Статті в журналах: "HCT 116 Carcinoma"

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Apaydin Yildirim Betul. "Anti-cancer, antiproliferative activity of active anionic H2O8 oxygen solution on HCT-116 cancer cell." World Journal of Advanced Research and Reviews 12, no. 2 (November 30, 2021): 179–84. http://dx.doi.org/10.30574/wjarr.2021.12.2.0560.

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HCT116 cells are adherent epithelial cells derived from the human colorectal carcinoma cell line commonly used to study inflammatory responses in colonic epithelial cells. In this study, it was aimed to evaluate the effects of active anionic H2O8 oxygen solution, which is a very strong antiviral and antimicrobial agent, on HCT-116 human colorectal cancer cell line. Cell viability was determined by MTT analysis. Antiproliferative activity of the anionic H2O8 was investigated on HCT 116 (human colorectal carcinoma) cancer cells. Anionic H2O8 displayed the outstanding activities for MTT test, IC50= 9.44 for 24th hour was calculated as IC50= 11.73 for 48th hour on HCT 116 cell line. It is thought that it can serve as an agent with strong potential to be used in treatment.

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Leong, Lek Mun, Kok Meng Chan, Asmah Hamid, Jalifah Latip, and Nor Fadilah Rajab. "Herbal Formulation C168 Attenuates Proliferation and Induces Apoptosis in HCT 116 Human Colorectal Carcinoma Cells: Role of Oxidative Stress and DNA Damage." Evidence-Based Complementary and Alternative Medicine 2016 (2016): 1–12. http://dx.doi.org/10.1155/2016/2091085.

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The use of herbal formulations has gained scientific interest, particularly in cancer treatment. In this study, the herbal formulation of interest, denoted as C168, is a mixture of eight genera of plants. This study aims to investigate the antiproliferative effect of C168 methanol extract (CME) on various cancer cells and its underlying mechanism of action on the most responsive cell line, namely, HCT 116 cells. CME exerted antiproliferative activities on HCT 116 colorectal carcinoma cells and HepG2 hepatocellular carcinoma cells but not on CCD-841-CoN normal colon epithelial cells, Jurkat E6.1 lymphoblastic leukemic cells, and V79-4 Chinese hamster lung fibroblasts. Further investigation on HCT 116 cells showed that CME induced G2/M cell-cycle arrest and apoptosis. Treatment of CME induced oxidative stress in HCT 116 cells by increasing the superoxide anion level and decreasing the intracellular glutathione. CME also increased tail moment value and H2AX phosphorylation in HCT 116 cells, suggesting DNA damage as an early signal of CME induced apoptosis. Loss of mitochondrial membrane potential in CME-treated cells also indicated the involvement of mitochondria in CME induced apoptosis. This study indicated the selectivity of CME toward colon cancer cells with the involvement of oxidative damage as its possible mechanism of action.

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Leischner, Christian, Markus Burkard, Anja Michel, Susanne Berchtold, Heike Niessner, Luigi Marongiu, Christian Busch, Jan Frank, Ulrich M. Lauer, and Sascha Venturelli. "Comparative Analysis of the Antitumor Activity of Cis- and Trans-Resveratrol in Human Cancer Cells with Different p53 Status." Molecules 26, no. 18 (September 14, 2021): 5586. http://dx.doi.org/10.3390/molecules26185586.

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Resveratrol, a natural plant phytoalexin, is produced in response to fungal infection or− UV irradiation. It exists as an isomeric pair with cis- and trans-conformation. Whereas multiple physiological effects of the trans-form, including a pronounced anti-tumoral activity, are nowadays elucidated, much less knowledge exists concerning the cis-isomer. In our work, we analyzed the antiproliferative and cytotoxic properties of cis-resveratrol in four different human tumor entities in direct comparison to trans-resveratrol. We used human cell lines as tumor models for hepatocellular carcinoma (HCC; HepG2, Hep3B), colon carcinoma (HCT-116, HCT-116/p53(−/−)), pancreatic carcinoma (Capan-2, MiaPaCa-2), and renal cell carcinoma (A498, SN12C). Increased cytotoxicity in all investigated tumor cells was observed for the trans-isomer. To verify possible effects of the tumor suppressor p53 on resveratrol-induced cell death, we used wild type and p53-deleted or -mutated cell lines for every tested tumor entity. Applying viability and cytotoxicity assays, we demonstrated a differential, dose-dependent sensitivity towards cis- or trans-resveratrol among the respective tumor types.

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Chandrani, Jeenkal P., and Kalpesh J. Ganatra. "An Efficient And Catalytically Free Chemical Transformation of Pyrimidin-2(1H)-one to 2-(N-Arylamino)pyrimidines and their in vitro Cytotoxicity Evaluation." Asian Journal of Organic & Medicinal Chemistry 5, no. 2 (2020): 133–37. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p260.

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With the aim to develop an efficient strategy to synthesize pyrimidine derivatives bearing diversely substituted amines involves four step linear protocols started with Biginelli multi-component reaction leading to dihydropyrimidines which passing throug multistep sequantial process containing oxidation, chlorination and catalytically free transformation of pyrimidin-2(1H)-one to 2-(N-arylamino)pyrimidines, were evaluated for cytotoxicity study against human cancer lines HCT-116, Hep-G2 and QG-56. Compound 4j exhibit significant anticancer activity showed against: human hepato carcinoma (Hep-G2) and human colon carcinoma (HCT-116) serve as a excellent lead molecule for the generation of various promising targets.

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Tan, Maria Carmens, Glenn G. Oyong, Chien Chang Shen, and Consolacion Y. Ragasa. "CYTOTOXIC LABDANE DITERPENOIDS FROM ANDROGRAPHIS PANICULATA (BURM.F.) NEES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 12 (December 1, 2017): 99. http://dx.doi.org/10.22159/ajpcr.2017.v10i12.19194.

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Objective: The primary objective of this study was to probe the cytotoxic capacity of the labdane diterpenoids andrographolide (1), 14-deoxyandrographolide (2), 14-deoxy-12-hydroxyandrographolide (3), and neoandrographolide (4) on mutant and wild-type immortalized cell lines.Methods: Breast adenocarcinoma (MCF-7), colon carcinomas (HCT-116 and HT-29), small cell lung carcinoma (H69PR), human acute monocytic leukemia (THP-1), and wild-type primary normal human dermal fibroblasts - neonatal cells (HDFn) were incubated with 1-4, and the degree of cytotoxicity was analyzed by employing the in vitro PrestoBlue® cell viability assay. Working solutions of 1-4 were prepared in complete cell culture medium to a final non-toxic dimethyl sulfoxide concentration of 0.2%. The plates were incubated at 37°C with 5% CO2 in a 98% humidified incubator throughout the assay. Nonlinear regression and statistical analyses were done to extrapolate the half maximal inhibitory concentration 50% (IC50). One-way ANOVA (p<0.05) and multiple comparison, Tukey’s post hoc test (p<0.05), were used to compare different pairs of data sets. Results were considered statistically significant at p<0.05.Results: The highest cytotoxicity index was exhibited by the H69PR and 1 trials which displayed the lowest IC50 value of 3.66 μg/mL, followed by HT-29 treated with 2, HCT-116 and 1 trials, and H69PR treated with 4 (IC50=3.81, 3.82, and 4.19 μg/mL, respectively). Only 1 and 4 were detrimental toward MCF-7, while 1, 3, and 4 were degenerative against H69PR. Tukey’s post hoc multiple comparison indicated no significant difference in the cytotoxicity of 1-4 on HCT-116 cells which afforded IC50 values ranging from 3.82 to 5.12 μg/mL. Evaluation of the two colon carcinoma cell lines showed that HCT-116 was categorically more susceptible to cellular damage caused by treatments with 1-4 than was HT-29. Cytotoxicity was not detected in THP-1 and HDFn cells (IC50>100 μg/mL).Conclusion: Diterpenoids 1-4 isolated from the dichloromethane extract of the leaves of A. paniculata exhibited different cytotoxic activities against MCF-7, HCT-116, HT-29, and H69PR. All constituents had comparable action on HCT-116 cells but were not found to be cytotoxic to normal HDFn cells and mutant THP-1 cells.

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Budu, Oana, Christian Dragos Banciu, Codruta Soica, Daniel Florin Lighezan, Andreea Milan, Alexandra Prodea, Alexandra Mioc, Marius Mioc, Gabriel Mardale, and Laurentiu Sima. "Lacticaseibacillus rhamnosus—A Promising Tool for Colorectal Cancer Treatment." Processes 11, no. 3 (March 6, 2023): 781. http://dx.doi.org/10.3390/pr11030781.

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Probiotic strains such as Lactobacillus spp. are already known for their beneficial effect on human health and new research supports their role in colon cancer prevention and treatment. The current study reports the effect of different concentrations of Lacticaseibacillus rhamnosus (LGG, 106–109 CFU/mL), alone or in association with 5-fluorouracil (5-FU, 10 μM), tested against normal HaCaT cells, HT-29 colorectal adenocarcinoma and HCT-116 colorectal carcinoma cell lines. The underlying cytotoxic effect was further investigated. LGG treatment of HT-29 and HCT-116 cells caused a variety of apoptotic-related nuclear morphological changes, as revealed by DAPI staining. ELISA studies showed that LGG treatment increased caspase-3 activity and pro-apoptotic BAX protein levels while decreasing anti-apoptotic Bcl-2 protein levels and the proto-oncogene Cyclin D1. A more detailed examination of the mitochondrial function revealed that high concentrations of LGG can impair mitochondrial function in HT-29 and HCT-116 cancer cells. All of these findings suggest that LGG has a pro-apoptotic, mitochondrial-targeted, cytotoxic effect on both colon cancer cell lines studied.

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Vaziri, S. A., A. Al-Hazzouri, D. R. Grabowski, M. K. Ganapathi, R. M. Bukowski, and R. Ganapathi. "Sorafenib treatment of clear-cell renal cell carcinoma (CCRCC) and colorectal carcinoma (CRC) cells: Differential effects on gene expression and cell death pathways." Journal of Clinical Oncology 25, no. 18_suppl (June 20, 2007): 15612. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.15612.

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15612 Background: The von Hippel Lindau gene (VHL) is often mutated in CCRCC and leads to loss of VHL protein (pVHL) expression. Sorafenib is a TKI with clinical activity in metastatic CCRCC. Studies to define mechanisms governing anti-tumor activity of this agent in CCRCC or CRC cell lines that express wild-type pVHL were conducted. Methods: We evaluated CAKI-1 (CCRCC) and HCT- 116/p53 +/+ (CRC) cell lines as model systems expressing wild-type pVHL. Cells were treated at 37°C in an atmosphere of normoxia (21% O2) or hypoxia (1% O2), 5% CO2 and the remainder N2 in the absence (control) or presence of sorafenib (2.5–20 μM) for 24–96 hours. Expression of target angiogenesis, apoptotic and anti-apoptotic genes was determined by real-time RT- PCR. Fluorescence microscopy following staining with Hoechst 33342 plus propidium iodide was used to analyze cell death by apoptosis and/or necrosis. Caspase-3 activity was measured using the target substrate DEVD-AFC. Results: In CAKI-1 and HCT-116 cells, exposure to 1% O2 relative to 21% O2, led to increased expression (2 to 6-fold) of angiogenesis (VEGF) and anti-apoptosis (TNFAIP3 & MCF2) genes. However, in an atmosphere of 1% O2 relative to 21% O2, a decreased (>2-fold) and increased (>3-fold) expression of the apoptotic (TNFRSF25) gene was observed in CAKI-1 cells and HCT-116 cells. Sorafenib treatment (7.5 μM) of CAKI-1 cells in 1% O2 led to a >3–4-fold decrease in expression of the VEGF and TNFAIP3 and a 3-fold increase TNFRSF25 genes. Following treatment with 10 μM sorafenib for 48h, cell death was >80% by necrosis in CAKI-1 cells and >95% by apoptosis in HCT-116 cells. Apoptotic cell death in the HCT-116 was also confirmed by increased caspase-3 activity in cell extracts following sorafenib treatment. Apoptotic cell death or necrotic cell death induced by sorafenib was unaffected by normoxia or hypoxia. Conclusions: In contrast to CCRCC cells, hypoxia led to upregulation of the apoptotic gene TNFRSF25 in the CRC cells. Anti- proliferative effects of sorafenib were primarily by necrosis in CCRCC cells and by apoptosis in CRC cells. No significant financial relationships to disclose.

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Khulud M Alshehr and Madeha O I Ghobashy. "Antitumor, Antimicrobial activities and Phytochemicals Constituent of different Extracts of Pulicaria undulata (Forssk.) Oliver. Grown Naturally in Saudi Arabia." International Journal of Research in Pharmaceutical Sciences 11, no. 3 (August 11, 2020): 4889–901. http://dx.doi.org/10.26452/ijrps.v11i3.2790.

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Antitumor and antimicrobial resistance are a habitual global issue, which continually demands finding new natural compounds to encounter the resistance. Pulicaria undulata (Forssk.) Oliver. (Asteraceae family) has numerous promising medicinal properties. The recent work aimed at determination of antitumor effects of three extracts of P. undulata on three types of human carcinoma; HEPG-2 hepatocellular carcinoma, MCF-7 breast carcinoma and HCT-116 colon carcinoma cell lines. Anticancer activity was assessed through studying the viability of the cancer cells and apoptotic pathway. Also, antimicrobial potency of different extracts was assessed against studied human pathogens (five Gram negative bacteria, two Gram positive bacteria and yeast). The results reveal that chloroform extract has different levels of cytotoxicity toward the three types of cancer cell lines. A considerable decline in cancer cell rates has been linked to increasing in concentration of plant extract. The half maximal inhibitory concentration IC 50 value was 3.01 µg/ mL for the HepG-2, 16.4 µg/mL for the MCF-7, and 7.4 µg/ mL for HCT-116. Followed by the ethyl acetate extract which showed strong cytotoxic activity against HEPG2 with IC 50 = 12.2 µg ∕ml and moderate activities against MCF7 and HCT 116 and recorded (IC 50 = 26.7 and 26.4 µg ∕ml, respectively). While the crude methanol extract recorded the lowest cytotoxic effect against HEPG2, MCF7 and HCT 116 with (IC 50 = 51.4, 105.1 and 86.7 µg ∕ ml, respectively). Chloroform and ethyl acetate extracts have a high antimicrobial activity more than methanol extract against the pathogens being studied. HPLC and GCMs Analysis identified numerous chemical compounds of P. undulata extracts with various therapeutic benefits. In conclusion, P. undulata has the potential to act as an antimicrobial agent against various pathogenic microbes and is a promising wild herb for the treatment of cancer.

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Kanti Das, Sabuj, Snehasis Mishra, Krishnendu Manna, Utpal Kayal, Supratim Mahapatra, Krishna Das Saha, Sasanka Dalapati, G. P. Das, Amany A. Mostafa та Asim Bhaumik. "A new triazine based π-conjugated mesoporous 2D covalent organic framework: itsin vitroanticancer activities". Chemical Communications 54, № 81 (2018): 11475–78. http://dx.doi.org/10.1039/c8cc07289b.

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Jacinto, Sonia D., Eunice Alexis C. Chun, Anthony Sebastian Montuno, Chien-Chang Shen, Dinah L. Espineli, and Consolacion Y. Ragasa. "Cytotoxic Cardenolide and Sterols from Calotropis Gigantea." Natural Product Communications 6, no. 6 (June 2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600614.

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The dichloromethane extract from the leaves of Calotropis gigantea Linn. was strongly cytotoxic against non-small cell lung carcinoma (A549), colon carcinoma (HCT 116) and hepatocellular carcinoma (Hep G2), and non toxic to Chinese hamster ovary (AA8). The extract afforded uscharin (1), 3,5,8-trihydroxy-24-methylcholest-6,22-diene (2), a mixture of (24R)-3β-hydroxy-24-ethylcholest-5-en-7-one (3a) and 6β-hydroxy-24-ethylcholest-4,22-dien-3-one (3b), and another mixture of (24R)-24-ethylcholest-4-en-3-one (4a) and (24S)-24-ethylcholest-4,22-dien-3-one (4b). Cardenolide 1 exhibited extreme toxicity to A549, HCT 116 and Hep G2 with IC50 values of 0.003 μg/mL, 0.013 μg/mL, and 0.018 μg/mL, respectively, while sample 3 exhibited an IC50 of 1.35 μg/mL, 4.46 μg/mL, and 3.83 μg/mL, respectively.

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Rajendrasozhan, Saravanan. "In vitro cytotoxicity analysis of Zizyphus spina-christi stem bark extract on human cancer cell lines." Bioinformation 17, no. 5 (May 31, 2021): 583–92. http://dx.doi.org/10.6026/97320630017583.

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Zizyphus spina-christi (Rhamnaceae family) is an edible plant used in folk medicine. Therefore, it is of interest to report the cytotoxic effects of Z. spina-christi bark crude extract on human cell lines. Crude ethanol extract of Z. spina-christi bark was fractionated with increasing polarity (diethyl ether, chloroform, ethyl acetate and butanol fractions). The fractions were examined for their cytotoxicity against human colon cancer (HCT-116 and CACO-2), cervical cancer (HeLa and HEp-2), lung carcinoma (A-549), hepatocellular carcinoma (HepG-2), breast cancer (MCF-7) and prostate cancer (PC-3) cell lines using viability assay. Diethyl ether fraction of Z. spina-christi showed the highest cytotoxic effects among the four extracts of Z. spina-christi. The IC50 of diethyl ether fraction was 7.14, 11.2, 11.6, 15.4, 39.8, 42.2, 84.2 and 153.8 Ĵg/ml on HepG-2, A-549, CACO-2, HCT-116, MCF-7, PC-3, HeLa, and HEp-2 cell lines, respectively. Data shows that the diethyl ether fraction of Z. spina-christi showed effective cytotoxic effects in colon, lung and hepatocellular cancer cell lines.

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Jalique, Shella Mae. "ID2010 Cytotoxicity of aqueous and ethanolic bark extracts of Pithecellobium dulce against human carcinoma cells." Biomedical Research and Therapy 4, S (September 5, 2017): 44. http://dx.doi.org/10.15419/bmrat.v4is.253.

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Cancer cases continue to increase and kill humans. In this paper, we report a study based on anticancer properties of the aqueous and ethanolic bark extracts of Pithecellobium dulce. Anticancer activities were assayed with standard MTT colorimetric procedure against three human cancer cell lines namely breast (MCF-7), colon (HCT-116), and hepatocellular (HepG2) in different concentrations. The aqueous extract of the plant revealed the highest toxicity on hepatocellular carcinoma (HepG2) cancer cell line with cell viability of 1.71 percent. On the other hand, its ethanol extracts has the highest toxicity on colon carcinoma (HCT-116) with a percent viability of 6.05 percent. Based on the results, the bark of the plant can be used to prepare anticancer drug with proper standardization methods

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Nurashikin Nordin, Anis, Irmanisha Ibrahim, Ahmad Fairuzabadi Mohd Mansor, Yumi Zuhanis Has-Yun Hashim, and Ioana Voiculescu. "Content Cytotoxicity Studies of Colorectal Carcinoma Cells Using Printed Impedance Sensors." Bulletin of Electrical Engineering and Informatics 6, no. 4 (December 1, 2017): 317–26. http://dx.doi.org/10.11591/eei.v6i4.851.

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Monitoring the effectiveness of drugs on cancer cells is crucial for chemotherapeutics studies. In-vitro cell-based biosensors can be used as an alternative for characteristic studies of cells’ response to drugs. Cell-based sensors provide real-time measurements and require smaller sample volumes compared to conventional T-flask measurement methods. This paper presents a biosensor that detects in real-time, impedance variations of human colon cancer, HCT-116 cells when treated with anti-cancer agent, 5-Fluorouracil (5-FU). Two different extracellular matrix (ECM); polyaniline and gelatin were tested and evaluated in terms of attachment quality. Polyaniline was found to provide the best attachment for HCT-116 cells and was used for cytotoxicity studies. Cytokinetic behavior indicated that 5-FU inhibited HCT-116 cells at IC50 of 6.8 µg/mL. Trypan blue exclusion method for testing cell viability was used to validate the impedance measurements, where the cancer cell concentrations were reduced to ~35% when treated with 2.5 µg/mL, and 50% when treated with 6.8 µg/mL. The results generated by the microfabricated impedance biosensor are comparable to the Trypan blue method since both gave similar cell growth trend. It can be concluded that the impedance biosensor has potential to be used as an alternative method in drug testing applications.

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Atchudan, Raji, Suguna Perumal, Thomas Nesakumar Jebakumar Immanuel Edison, Ashok K. Sundramoorthy, Sambasivam Sangaraju, Rajendran Suresh Babu, and Yong Rok Lee. "Sustainable Synthesis of Bright Fluorescent Nitrogen-Doped Carbon Dots from Terminalia chebula for In Vitro Imaging." Molecules 27, no. 22 (November 21, 2022): 8085. http://dx.doi.org/10.3390/molecules27228085.

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In this study, sustainable, low-cost, and environmentally friendly biomass (Terminalia chebula) was employed as a precursor for the formation of nitrogen-doped carbon dots (N-CDs). The hydrothermally assisted Terminalia chebula fruit-derived N-CDs (TC-CDs) emitted different bright fluorescent colors under various excitation wavelengths. The prepared TC-CDs showed a spherical morphology with a narrow size distribution and excellent water dispensability due to their abundant functionalities, such as oxygen- and nitrogen-bearing molecules on the surfaces of the TC-CDs. Additionally, these TC-CDs exhibited high photostability, good biocompatibility, very low toxicity, and excellent cell permeability against HCT-116 human colon carcinoma cells. The cell viability of HCT-116 human colon carcinoma cells in the presence of TC-CDs aqueous solution was calculated by MTT assay, and cell viability was higher than 95%, even at a higher concentration of 200 μg mL−1 after 24 h incubation time. Finally, the uptake of TC-CDs by HCT-116 human colon carcinoma cells displayed distinguished blue, green, and red colors during in vitro imaging when excited by three filters with different wavelengths under a laser scanning confocal microscope. Thus, TC-CDs could be used as a potential candidate for various biomedical applications. Moreover, the conversion of low-cost/waste natural biomass into products of value promotes the sustainable development of the economy and human society.

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Hegazy, Marwa GA, Amal M. Imam, and Bassem E. Abdelghany. "Evaluation of cytotoxic and anticancer effect of Orobanche crenata methanolic extract on cancer cell lines." Tumor Biology 42, no. 5 (May 2020): 101042832091868. http://dx.doi.org/10.1177/1010428320918685.

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We aimed to assess the antitumor activity of Orobanche crenata methanolic extract and evaluate its cytotoxic effect on different cancer cell lines to develop an effective natural anticancer drug. Components of O. crenata methanolic extract were analyzed using gas chromatography–mass spectrometry. The extract’s antioxidant activity was assessed by 2,2-diphenyl-1-picrylhydrazyl and ferric reducing antioxidant power procedures and cytotoxicity of the extract was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase assays. Caspase-3 activity was also estimated. O. crenata methanolic extract shows powerful antioxidant activity. The extract inhibited the propagation of human hepatocellular carcinoma (HepG2), human prostate cancer (PC3), human breast adenocarcinoma (MCF-7), and human colon carcinoma (HCT-116) in a dose-dependent manner. O. crenata–treated cells displayed obvious morphological structures distinctive of apoptosis. MTT assay exposed that the extract presented prevention of cell persistence in a dose-dependent means and revealed extremely cytotoxic activity against HepG2, PC3, MCF-7, and HCT-116 with 50% inhibitory concentration values 30.3, 111, 89.6, and 28.6 µg/mL, respectively, after 24 h of incubation. In addition, treatment of HCT-116 with various concentrations of the extract caused the release of lactate dehydrogenase and induction of caspase-3 activity in a dose-dependent way. In conclusion, our findings suggested that the O. crenata extract possesses potent antioxidant, cytotoxic activity, and anticancer properties which are possibly due to the principal bioactive phytochemical composites existing in this plant. These results can be used to develop new drugs for cancer treatment.

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El Azab, Islam H., and Nadia A. A. Elkanzi. "An Efficient Synthetic Approach Towards Benzo[b]pyrano[2,3-e][1,4]diazepines, and Their Cytotoxic Activity." Molecules 25, no. 9 (April 28, 2020): 2051. http://dx.doi.org/10.3390/molecules25092051.

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In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1H-benzo[b][1,4]diazepin-2(3H)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. In vitro investigation of 11 compounds of this series, using a panel of two human tumor cell lines namely; human breast adenocarcinoma (MCF-7), and human colorectal carcinoma (HCT-116), revealed promising cytotoxic activities. Among all synthesized compounds, analogue 9 displayed maximum cytotoxicity with IC50 values of 16.19 ± 1.35 and 17.16 ± 1.54 μM against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin.

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Dogan Tuba, Ozturk Serdar, and Apaydin Yildirim Betul. "In vitro anticancer and antiproliferative activity of crocin on HCT-116 cells." World Journal of Advanced Research and Reviews 15, no. 3 (September 30, 2022): 290–97. http://dx.doi.org/10.30574/wjarr.2022.15.3.0919.

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One of the world’s main causes of cancer-related fatalities worldwide is colorectal cancer. The adherent epithelial cells known as HCT116 (human colorectal carcinoma) are frequently employed to examine inflammatory responses in colonic epithelial cells. They are derived from the human colorectal cancer cell line. Crocin, a potent antioxidant, anticarcinogenic was tested in this study to see how it affected the HCT-116 human colorectal cancer cell line. MTT analysis was used to assess cell viability. Crocin's antiproliferative activity to inhibit the proliferation of HCT 116 cancer cells was examined. Crocin displayed the outstanding activities for MTT test, IC50= 10.57 μL/mL for 24 hours was calculated as IC50= 3.29 μL/mL for 48 hours on HCT 116 cell line. Total antioxidant status (TAS) and total oxidant status (TOS) in the prepared cell lysate were determined by using commercial kits. Crocin is thought to be a high potential agent to be used in treatment.

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Sabbah, Dima A., Ameerah H. Ibrahim, Wamidh H. Talib, Khalid M. Alqaisi, Kamal Sweidan, Sanaa K. Bardaweel, Ghassan A. Sheikha, et al. "Ligand-Based Drug Design: Synthesis and Biological Evaluation of Substituted Benzoin Derivatives as Potential Antitumor Agents." Medicinal Chemistry 15, no. 4 (May 20, 2019): 417–29. http://dx.doi.org/10.2174/1573406414666180912111846.

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Background: Phosphoinositide 3-kinase α (PI3Kα) has emerged as a promising target for anticancer drug design. Objectives: Target compounds were designed to investigate the effect of the p-OCH3 motifs on ligand/PI3Kα complex interaction and antiproliferative activity. Methods: Synthesis of the proposed compounds, biological examination tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, along with Glide docking studies. Results: A series of 1,2-bis(4-methoxyphenyl)-2-oxoethyl benzoates was synthesized and characterized by means of FT-IR, 1H and 13C NMR, and by elemental analysis. Biological investigation demonstrated that the newly synthesized compounds exhibit antiproliferative activity in human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines possibly via inhibition of PI3Kα and estrogen receptor alpha (ERα). Additionally, results revealed that these compounds exert selective inhibitory activity, induce apoptosis, and suppress VEGF production. Compound 3c exhibited promising antiproliferative activity in HCT-116 interrogating that hydrogen bond-acceptor mediates ligand/PI3Kα complex formation on m- position. Compounds 3e and 3i displayed high inhibitory activity in MCF-7 and T47D implying a wide cleft discloses the o-attachment. Furthermore, compound 3g exerted selective inhibitory activity against T47D. Glide docking studies against PI3Kα and ERα demonstrated that the series accommodate binding to PI3Kα and/or ERα. Conclusion: The series exhibited a potential antitumor activity in human carcinoma cell lines encoding PI3Kα and/or ERα.

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Elsayed, Shadia A., Entsar A. Saad, and Sahar I. Mostafa. "Development of New Potential Anticancer Metal Complexes Derived from 2-Hydrazinobenzothiazole." Mini-Reviews in Medicinal Chemistry 19, no. 11 (July 10, 2019): 913–22. http://dx.doi.org/10.2174/1389557518666181017143548.

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Background: Due to the side effects of clinically approved anticancer drugs there is a great need to explore and develop new metal-based anticancer drug molecules of high efficiency with less or no side effects. Objective: To synthesize new metal complexes of 2-hydrazinobenzothiazole (hbt) and to investigate their potential anticancer characteristics. Methods: New five complexes; [VO(hbt)2SO4].4H2O (1), [Ru(hbt)2Cl3(H2O)] (2), [M(hbt)2Cl2] [M(II) = Pd (3), Pt (4)] and [Ag(hbt)2].NO3 (5) were prepared and their structure was investigated by means of FTIR, 1H NMR, ESI-MS and UV-Vis spectra, elemental and thermal analysis, magnetic and molar conductance measurements. The ligand and its complexes were examined as anticancer agents against Ehrlich ascites carcinoma (EAC) and human cancer cells (hepatocellular carcinoma Hep-G2, mammary gland breast cancer MCF-7 and colorectal carcinoma HCT-116). This feature is further supported by the DNAmetal complexes binding ability. In addition, anti-oxidation activity of the complexes was investigated. Results: Complex (5) shows the highest anticancer activity with IC50 of 5.15, 9.9, 13.1 and 17.7 µg/mL for EAC, HePG-2, MCF-7 and HCT-116, respectively. Complexes (2) and (3) show promising cytotoxicity against EAC and HePG-2 cells with IC50 5.49 and 16.2 µg/mL, respectively. While, complexes (1) and (4) show optimistic cytotoxicity against EAC with IC50 of 9.63 and 11.25 µg/mL, respectively. The order of DNA binding ability of the complexes is (5) > (3) > (2) > (1) > (4). Among the five complexes, complex (5) shows the best anti-oxidation activity. Conclusion: Complex (5) showed the highest DNA binding ability, anti-oxidation and anticancer activities.

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Malyarenko, Olesya S., Tatiana I. Imbs, and Svetlana P. Ermakova. "In Vitro Anticancer and Radiosensitizing Activities of Phlorethols from the Brown Alga Costaria costata." Molecules 25, no. 14 (July 14, 2020): 3208. http://dx.doi.org/10.3390/molecules25143208.

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The anticancer and radiosensitizing effects of high-molecular-weight phlorethols CcPh (Mw = 2520 Da) isolated from the brown algae of Costaria costata on human colorectal carcinoma HCT 116 and HT-29 cells were investigated. Phlorethols CcPh possessed cytotoxic activity against HT-29 (IC50 = 92 μg/mL) and HCT 116 (IC50 = 94 μg/mL) cells. CcPh at non-toxic concentrations inhibited the colony formation in colon cancer cells and significantly enhanced their sensitivity to low non-toxic X-ray irradiation. The combinatory effect of radiation and CcPh was synergistic (Combination index < 0.7). Algal phlorethols might be prospective candidates as radiosensitizers to improve the scheme of radiotherapy.

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Tsai, Cheng-Chih, Kuan-Jung Huang, and Pei-Pei Lin. "Lactobacillus spp. inhibits the growth of HCT-116 and reduces IL-8 secretion by Salmonella typhimurium-infected HCT-116 colorectal carcinoma cells." International Journal of Food Studies, no. 2 (October 18, 2022): 307–19. http://dx.doi.org/10.7455/ijfs/11.2.2022.a5.

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Salmonella typhimurium causes symptoms resembling typhoid fever and gastroenteritis in humans. Its toxicity is due to an outer membrane consisting largely of lipopolysaccharides (LPS) which is responsible for the host immune response. The aim of this study is to evaluate the antimicrobial, anti-apoptotic ability of Lactobacillus plantarum and reduce Salmonella-induced pro-inflammatory cytokine IL-8 secretion. Adhesive tests were performed using lactobacilli co-cultured with the colon cancer cell line HCT-116 for 2 hours. The strains displaying the highest adhesion were selected for downstream 3- (4, 5- Dimethylthiazol -2-yl) -2, 5- diphenyltetrazolium bromide (MTT) tests to assess cytotoxicity. The supernatants of Lactobacillus cultured with HCT-116 cells for 24 and 48 h to evaluate the inhibitory effect. To determine Interleukin 8 (IL-8) secretion in colon cancer induced by S. typhimurium, we stimulated HCT-116 cells with S. typhimurium and co-cultured with lactobacilli for 24 h. Lactobacilli had the most significant inhibitory effects on cell growth, and their inhibitory effects were time-dependent. Strain No. 03-03-026 caused cancer cell deoxyribonucleic acid (DNA) fragmentation, and the anti-apoptosis protein (B-cell lymphoma 2) was reduced in the HCT-116 cells as determined. IL-8 production in colon cancer cells was significantly reduced by these lactobacilli. Our results suggested that lactobacilli maybe effectively reduce the numbers of S. typhimurium, IL-8 levels and the anti-apoptotic phosphorylated-p38 mitogen-activated protein kinase and B-cell lymphoma 2 proteins. Lactobacillus can be added to the diet as a food additive to prevent colorectal cancer and used to be the prophylactic agent against S. typhimurium.

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H. Al Rasheed, Hessa, Azizah M. Malebari, Kholood A. Dahlous, and Ayman El-Faham. "Synthesis and Characterization of New Series of 1,3-5-Triazine Hydrazone Derivatives with Promising Antiproliferative Activity." Molecules 25, no. 11 (June 11, 2020): 2708. http://dx.doi.org/10.3390/molecules25112708.

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A new series of s-triazine hydrazone derivatives was prepared based on the reaction of 6-hydrazino-2,4-disubstituted-s-triazine with p-substituted benzaldehyde derivatives using a straightforward synthetic pathway. The antiproliferative activity of all synthesized compounds was evaluated against two human cancer cell lines; breast cancer MCF-7 and colon carcinoma HCT-116 using MTT assay. Among all, 11 compounds have shown strong to moderate antiproliferative activity with IC50 values in the range 1.01–18.20 µM in MCF-7 and 0.97–19.51 µM in HCT-116. The best results were obtained with 4,4’-(6-(2-(pyridin-2-ylmethylene)hydrazinyl)-1,3,5-triazine-2,4-diyl) dimorpholine 11 (IC50 = 1.0 µM and 0.98 µM in MCF-7 and HCT-116 cell lines, respectively). The substituents on the s-triazine core as well as the substituent at the benzylidene moiety have a great effect on the antiproliferative activity. Whereas compounds containing dimorpholino-s-triazine derivatives 8a–e showed more potent antiproliferative in MCF-7 compared to their analogs 7a–f (compounds containing two-piperidine rings), compounds containing one piperidine and one morpholine ring 9a–f showed better IC50 values in the range 10.4–22.2 µM. On the other hand, compounds containing two-piperidine rings 7a–f showed more potent antiproliferative in HCT-116 (IC50 values in the range 8.8–19.5 µM) than their analogs 8a–e and 9a–f.

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Bae, Inho, Taeyu Grace Kim, Taeyeon Kim, Dohoon Kim, Doug-Hoon Kim, Jaewon Jo, Young-Ju Lee, and Young-Il Jeong. "Phenethyl Isothiocyanate-Conjugated Chitosan Oligosaccharide Nanophotosensitizers for Photodynamic Treatment of Human Cancer Cells." International Journal of Molecular Sciences 23, no. 22 (November 9, 2022): 13802. http://dx.doi.org/10.3390/ijms232213802.

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The aim of this study is to synthesize phenethyl-conjugated chitosan oligosaccharide (COS) (abbreviated as ChitoPEITC) conjugates and then fabricate chlorin E6 (Ce6)-incorporated nanophotosensitizers for photodynamic therapy (PDT) of HCT-116 colon carcinoma cells. PEITC was conjugated with the amine group of COS. Ce6-incorporated nanophotosensitizers using ChitoPEITC (ChitoPEITC nanophotosensitizers) were fabricated by dialysis method. 1H nuclear magnetic resonance (NMR) spectra showed that specific peaks of COS and PEITC were observed at ChitoPEITC conjugates. Transmission electron microscope (TEM) confirmed that ChitoPEITC nanophotosensitizers have spherical shapes with small hydrodynamic diameters less than 200 nm. The higher PEITC contents in the ChitoPEITC copolymer resulted in a slower release rate of Ce6 from nanophotosensitizers. Furthermore, the higher Ce6 contents resulted in a slower release rate of Ce6. In cell culture study, ChitoPEITC nanophotosensitizers showed low toxicity against normal CCD986Sk human skin fibroblast cells and HCT-116 human colon carcinoma cells in the absence of light irradiation. ChitoPEITC nanophotosensitizers showed a significantly higher Ce6 uptake ratio than that of free Ce6. Under light irradiation, cellular reactive oxygen species (ROS) production of nanophotosensitizers was significantly higher than that of free Ce6. Especially, PEITC and/or ChitoPEITC themselves contributed to the production of cellular ROS regardless of light irradiation. ChitoPEITC nanophotosensitizers showed significantly higher PDT efficacy against HCT-116 cells than that of free Ce6. These results indicate that ChitoPEITC nanophotosensitizers have superior potential in Ce6 uptake, ROS production and PDT efficacy. In the HCT-116 cell-bearing mice tumor-xenograft model, ChitoPEITC nanophotosensitizers efficiently inhibited growth of tumor volume rather than free Ce6. In the animal imaging study, ChitoPEITC nanophotosensitizers were concentrated in the tumor tissue, i.e., fluorescence intensity in the tumor tissue was stronger than that of other tissues. We suggest that ChitoPEITC nanophotosensitizers are a promising candidate for the treatment of human colon cancer cells.

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Jovankić, Jovana, Danijela Nikodijević, Stefan Blagojević, Nikola Radenković, Dragana Jakovljević, Filip Grbović, and Danijela Cvetković. "The biological activity of Ocimum minimum L. flowers on redox status parameters in HCT-116 colorectal carcinoma cells." Kragujevac Journal of Science, no. 44 (2022): 155–68. http://dx.doi.org/10.5937/kgjsci2244155j.

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Medicinal plants have widely been used as a natural source of remedies for treating several diseases, including colorectal cancer. Ocimum minimum L. is a very important dietary plant used in traditional and modern medicine, due to its health beneficial effect realized by cytotoxic, proapoptotic, antioxidant/prooxidant, antiviral and antimicrobial activity. The biological activity of O. minimum flowers has been evaluated in HCT116 colorectal carcinoma cells through antiproliferative activity by MTT assay, pro-apoptotic activity by AO/EB and concentrations of redox status parameters (O2∙ and lipid peroxidation) by colorimetric methods. The protein expression of iNOS was analyzed by immunocytochemistry, while the antimigratory effect was measured by xCELLigence system. The treatment with O. minimum shows the antiproliferative, proapoptotic, impact on redox status parameters and antimigratory effect on HCT-116 cells. Based on obtained results, the pharmacological effect of O. minimum is evident against HCT-116 colorectal carcinoma cells, suggesting that this plant may be good start material for future anticancer therapy investigation.

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Singh, Mahendra Pal, Ki Hun Park, Tejinder Pal Khaket, and Sun Chul Kang. "CJK-7, a Novel Flavonoid from Paulownia tomentosa Triggers Cell Death Cascades in HCT-116 Human Colon Carcinoma Cells via Redox Signaling." Anti-Cancer Agents in Medicinal Chemistry 18, no. 3 (June 4, 2018): 428–37. http://dx.doi.org/10.2174/1871520617666171026170009.

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Background: Colon cancer is the second most common cancer to cause death worldwide. About half of colon cancers patients require adjuvant therapy to control relapse following surgical resection. Therefore, abolition of tumor cell progression using an effective chemotherapeutic agent holds a feasible approach to treat patients suffering from colon cancer. In the present study, we evaluated the effects of geranylated flavonoid CJK-7, isolated from Paulownia tomentosa on HCT-116 human colon carcinoma cells. Materials and Methods: The effects of CJK-7 as an active component on HCT-116 cells programmed cell death and its underlying molecular mechanism were examined by using MTT assay, morphological assessment, H2DCFDA staining, Fura-2AM staining, Hoechst-33342 staining, comet assay, Acridine orange staining, mitochondrial membrane potential (ΔΨm) assay and Western blot analyses. Results and Conclusion: The results revealed that, CJK-7 was capable of inducing caspase-dependent cell death events in cancer cells. Moreover, it was involved in up-regulation of autophagy signaling as evidenced by enhanced expression of LC3I/II. We also noticed stimulated expression of endoplasmic reticulum stress markers and phosphorylation of c-Jun NH2-terminal kinase (JNK), which was associated with up-regulated expression of p53, PUMA, Atg5 and Beclin-1, and down-regulation of Bcl-2, stressing the interaction of ROS on the aforementioned signaling. Furthermore, exposure to ROS scavengers (N-acetyl-l-cysteine (NAC), and JNK-specific inhibitor SP600125) significantly reversed the effects of CJK-7 by down-regulating apoptosis and autophagy signatures in HCT-116 cancer cells. Collectively our findings clarify the ROS-dependent regulatory effect of CJK-7 on programmed cell death signaling events in HCT-116 cancer cells while depicting its virile pro-oxidant capacity.

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Tomovic, Dusan Lj, Andriana M. Bukonjic, Aleksandar Kocovic, Milos V. Nikolic, Marina Z. Mijajlovic, Verica V. Jevtic, Zoran R. Ratkovic, et al. "Synthesis, Characterization, and Cytotoxicity of Binuclear Cooper(II)-Complexes with some S-Alkenyl Derivatives of Thiosalicyclic Acid." Serbian Journal of Experimental and Clinical Research 18, no. 1 (March 1, 2017): 13–18. http://dx.doi.org/10.1515/sjecr-2016-0071.

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Abstract New complexes of copper(II) with S-alkenyl derivatives of thiosalicylic acid (alkenyl = propenyl-(L1), isobutenyl-(L2)) have been synthesized and characterized by microanalysis, infrared spectra, magnetic measurements, and by NMR spectra. The cytotoxic activity of two newly synthesized precursor S-alkenyl derivatives of thiosalicylic acid were tested using an MTT colorimetric technique on HCT-116 human colon carcinoma cells. The cytotoxic effect of the copper(II)- complexes were higher compared to the cytotoxicity of the corresponding ligand (for concentrations from 31.25 to 250 μM). Copper(II)-complexes showed a slightly lower cytotoxicity compared to cisplatin. Complexes of copper(II) with S-alkenyl derivatives of thiosalicylic acid (at concentrations from 250 to 1000 μM) had a cytotoxic effect on HCT-116 cells compared to cisplatin.

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Staab, A., I. Müller, J. Rudner, V. Heinrich, M. Bamberg, and S. Huber. "135 HYPERTHERMIA RADIOSENSITIZES HYPOXIC HCT-116 HUMAN COLORECTAL CARCINOMA CELLS IN VITRO." Radiotherapy and Oncology 102 (March 2012): S60. http://dx.doi.org/10.1016/s0167-8140(12)70107-x.

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Feist, Peter E., Liangliang Sun, Xin Liu, Norman J. Dovichi, and Amanda B. Hummon. "Bottom-up proteomic analysis of single HCT 116 colon carcinoma multicellular spheroids." Rapid Communications in Mass Spectrometry 29, no. 7 (April 15, 2015): 654–58. http://dx.doi.org/10.1002/rcm.7150.

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Mirnajafizadeh, Fatemeh, Deborah Ramsey, Shelli McAlpine, Fan Wang, and John Stride. "Nanoparticles for Bioapplications: Study of the Cytotoxicity of Water Dispersible CdSe(S) and CdSe(S)/ZnO Quantum Dots." Nanomaterials 9, no. 3 (March 20, 2019): 465. http://dx.doi.org/10.3390/nano9030465.

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Semiconductor nanocrystals or quantum dots (QDs) have unique optical and physical properties that make them potential imaging tools in biological and medical applications. However, concerns over the aqueous dispersivity, toxicity to cells, and stability in biological environments may limit the use of QDs in such applications. Here, we report an investigation into the cytotoxicity of aqueously dispersed CdSe(S) and CdSe(S)/ZnO core/shell QDs in the presence of human colorectal carcinoma cells (HCT-116) and a human skin fibroblast cell line (WS1). The cytotoxicity of the precursor solutions used in the synthesis of the CdSe(S) QDs was also determined in the presence of HCT-116 cells. CdSe(S) QDs were found to have a low toxicity at concentrations up to 100 µg/mL, with a decreased cell viability at higher concentrations, indicating a highly dose-dependent response. Meanwhile, CdSe(S)/ZnO core/shell QDs exhibited lower toxicity than uncoated QDs at higher concentrations. Confocal microscopy images of HCT-116 cells after incubation with CdSe(S) and CdSe(S)/ZnO QDs showed that the cells were stable in aqueous concentrations of 100 µg of QDs per mL, with no sign of cell necrosis, confirming the cytotoxicity data.

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Al-Etaibi, Alya M., and Morsy Ahmed El-Apasery. "Dyeing Performance of Disperse Dyes on Polyester Fabrics Using Eco-Friendly Carrier and Their Antioxidant and Anticancer Activities." International Journal of Environmental Research and Public Health 16, no. 23 (November 20, 2019): 4603. http://dx.doi.org/10.3390/ijerph16234603.

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Both non eco- and eco-friendly carriers were utilized for accelerating the dyeing rate of polyethylene terephthalate fabrics (PET) dyed with disperse dyes at 100 °C. Fastness properties of the dyed fabrics showed good and excellent results. Finally, the prepared disperse dyes 1 and 2 showed potent anti-tumor cytotoxic activity in vitro using MCF-7 cells (human breast cancer cell line), HepG-2 cells (human Hepatocellular carcinoma), HCT-116 (colon carcinoma), A-549 cells (Lung carcinoma cell line), and anti-oxidant activities.

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El-Kahky, Dina, Magdy Attia, Saadia M. Easa, Nemat M. Awad, and Eman A. Helmy. "Interactive Effects of Biosynthesized Nanocomposites and Their Antimicrobial and Cytotoxic Potentials." Nanomaterials 11, no. 4 (April 1, 2021): 903. http://dx.doi.org/10.3390/nano11040903.

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The present study investigated the biosynthesis of silver (AgNPs), zinc oxide (ZnONPs) and titanium dioxide (TiO2NPs) nanoparticles using Aspergillusoryzae, Aspergillusterreus and Fusariumoxysporum. Nanocomposites (NCs) were successfully synthesized by mixing nanoparticles using a Sonic Vibra-Cell VC/VCX processor. A number of analytical techniques were used to characterize the synthesized biological metal nanoparticles. Several experiments tested biologically synthesized metal nanoparticles and nanocomposites against two types of human pathogenic bacteria, including Gram-positive Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative Escherichia coli and Pseudomonasaeruginosa. Additionally, the antitumor activity in HCT-116 cells (colonic carcinoma) was also evaluated. Significant antimicrobial effects of various synthesized forms of nanoparticles and nanocomposites against E. coli and P. aeruginosa bacteria were detected. Various synthesized biogenic forms of nanoparticles and nanocomposite (9.0 to 29 mm in diameter) had high antibacterial activity and high antitumor activity against HCT-116 cells (colonic carcinoma) with IC50 values of 0.7–100 µg/mL. Biosynthesized NPs are considered an alternative to large-scale biosynthesized metallic nanoparticles and nanocomposites, are simple and cost effective, and provide stable nanomaterials.

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Al Baroot, Abbad, Khaled A. Elsayed, Firdos Alam Khan, Shamsuddeen A. Haladu, Filiz Ercan, Emre Çevik, Q. A. Drmosh, and M. A. Almessiere. "Anticancer Activity of Au/CNT Nanocomposite Fabricated by Nanosecond Pulsed Laser Ablation Method on Colon and Cervical Cancer." Micromachines 14, no. 7 (July 20, 2023): 1455. http://dx.doi.org/10.3390/mi14071455.

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Gold nanoparticles (AuNPs) and carbon nanotubes (CNTs) are increasingly being investigated for cancer management due to their physicochemical properties, low toxicity, and biocompatibility. This study used an eco-friendly technique (laser synthesis) to fabricate AuNP and Au/CNT nanocomposites. AuNPs, Au/CNTs, and CNTs were tested as potential cancer nanotherapeutics on colorectal carcinoma cells (HCT-116) and cervical cancer cells (HeLa) using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. In addition, the non-cancer embryonic kidney cells HEK-293 were taken as a control in the study. The cell viability assay demonstrated a significant reduction in cancer cell population post 48 h treatments of AuNPs, and Au/CNTs. The average cell viabilities of AuNPs, Au/CNTs, and CNTs for HCT-116 cells were 50.62%, 65.88%, 93.55%, and for HeLa cells, the cell viabilities were 50.88%, 66.51%, 91.73%. The cell viabilities for HEK-293 were 50.44%, 65.80%, 93.20%. Both AuNPs and Au/CNTs showed higher cell toxicity and cell death compared with CNT nanomaterials. The treatment of AuNPs and Au/CNTs showed strong inhibitory action on HCT-116 and HeLa cells. However, the treatment of CNTs did not significantly decrease HCT-116 and HeLa cells, and there was only a minor decrease. The treatment of AuNPs, and Au/CNTs, on normal HEK-293 cells also showed a significant decrease in cell viability, but the treatment of CNTs did not produce a significant decrease in the HEK-293 cells. This study shows that a simplified synthesis technique like laser synthesis for the preparation of high-purity nanomaterials has good efficacy for possible future cancer therapy with minimal toxicity.

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Alminderej, Elganzory, El-Bayaa, Awad, and El-Sayed. "Synthesis and Cytotoxic Activity of New 1,3,4-Thiadiazole Thioglycosides and 1,2,3-Triazolyl-1,3,4-Thiadiazole N-glycosides." Molecules 24, no. 20 (October 16, 2019): 3738. http://dx.doi.org/10.3390/molecules24203738.

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New 1,3,4-thiadiazole thioglycosides linked to substituted arylidine systems were synthesized via glycosylation of the prepared 1,3,4-thiadiazole thiol compounds. Click strategy was also used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycosides by reaction of the acetylenic derivatives with different glycosyl azids followed by deacetylation process. The cytotoxic activities of the prepared compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds 2 and 3, the triazole glycosides linked to p-methoxyarylidine derivatives 14 and 15 in addition to the free hydroxyl glycoside 20 were found potent in activity comparable to the reference drug doxorubicin against MCF-7 human cancer cells. The acetylenic derivative 2 and glycoside 20 were also found highly active against HCT-116 cell lines.

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Zorc, Branka, Zrinka Rajić, and Ivana Perković. "Antiproliferative evaluation of various aminoquinoline derivatives." Acta Pharmaceutica 69, no. 4 (December 1, 2019): 661–72. http://dx.doi.org/10.2478/acph-2019-0048.

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Abstract Four classes of aminoquinoline derivatives were prepared: primaquine ureas 1a–f, primaquine bis-ureas 2a–f, chloroquine fumardiamides 3a–f and mefloquine fumardiamides 4a–f. Their antiproliferative activities against breast adeno-carcinoma (MCF-7), lung carcinoma (H460) and colon carcinoma (HCT 116 and SW620) cell lines were evaluated in vitro, using MTT cell proliferation assay. The results revealed a low activity of primaquine urea and bis-urea derivatives and high activity of all fumardiamides, with IC50 values in low micromolar range against all tested cancer cell lines.

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Sabbah, Dima A., Bayan Hishmah, Kamal Sweidan, Sanaa Bardaweel, Murad AlDamen, Haizhen A. Zhong, Reema Abu Khalaf, et al. "Structure-Based Design: Synthesis, X-ray Crystallography, and Biological Evaluation of N-Substituted-4-Hydroxy-2-Quinolone-3-Carboxamides as Potential Cytotoxic Agents." Anti-Cancer Agents in Medicinal Chemistry 18, no. 2 (April 19, 2018): 263–76. http://dx.doi.org/10.2174/1871520617666170911171152.

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Background: Oncogenic potential of phosphatidylinositol 3-kinase (PI3Kα) has been highlighted as a therapeutic target for anticancer drug design. Objective: Target compounds were designed to address the effect of different substitution patterns at the N atom of the carboxamide moiety on the bioactivity of this series. Methods: Synthesis of the targeted compounds, crystallography, biological evaluation tests against human colon carcinoma (HCT-116), and Glide docking studies. Results: A new series of N-substituted- 4-hydroxy-2-quinolone-3-carboxamides was prepared and characterized by means of FT-IR, 1H and 13C NMR, and elemental analysis. In addition, the identity of the core nucleus 5 was successfully characterized with the aid of X-ray crystallography. Biological activity of prepared compounds was investigated in vitro against human colon carcinoma (HCT-116) cell line. Results revealed that these compounds inhibit cell proliferation and induce apoptosis through an increase in caspase-3 activity and a decrease in DNA cellular content. Compounds 7, 14, and 17 which have H-bond acceptor moiety on p-position displayed promising PI3Kα inhibitory activity. On the other hand, derivatives tailored with bulky and hydrophobic motifs (16 and 18) on o- and m-positions exhibited moderate activity. Molecular docking studies against PI3Kα and caspase-3 showed an agreement between the predicted binding affinity (ΔGobsd) and IC50 values of the derivatives for the caspase-3 model. Furthermore, Glide docking studies against PI3Kα demonstrated that the newly synthesized compounds accommodate PI3Kα kinase catalytic domain and form H-bonding with key binding residues. Conclusion: The series exhibited a potential PI3Kα inhibitory activity in HCT-116 cell line.

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Zubair, Muhammad Sulaiman, Walied Mohamed Alarif, Mohamed Ali Ghandourah, Syariful Anam та Ibrahim Jantan. "Cytotoxic Activity of 2-O-β-glucopyranosil Cucurbitacin D from Benalu Batu (Begonia sp.) Growing in Morowali, Central Sulawesi". Indonesian Journal of Chemistry 20, № 4 (10 червня 2020): 766. http://dx.doi.org/10.22146/ijc.43626.

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Benalu batu (Begonia sp.) had been used traditionally as an anticancer medicinal plant by Wana tribe in Morowali, Central Sulawesi, This study aims to evaluate the cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D, isolated from the ethyl acetate soluble fraction of Benalu batu (Begonia sp.) and to determine its action on apoptosis induction. Benalu batu (Begonia sp.) herb was extracted by maceration using ethanol 96% as a solvent. Vacuum liquid column chromatography and preparative thin layer chromatography have been applied on fractionation and isolation of the compound. The structure elucidation was performed by extensive analysis of 1D/2D nuclear magnetic resonance (NMR) and Mass Spectrophotometer (MS). Cytotoxic activity against human breast adenocarcinoma (MCF-7) and human colon colorectal carcinoma (HCT-116) cell lines were performed by 5-diphenyltetrazolium bromide (MTT) method. Annexin V-FITC assay was employed to determine the apoptosis induction. 2-O-β-glucopyranosil cucurbitacin D showed potent cytotoxic activity against MCF-7 and HCT-116 with the IC50 of 19.913 and 0.002 μg/mL, respectively. Annexin V-FITC assay clearly exhibited the cytotoxic mechanism on MCF-7 and HCT-116 via apoptosis induction with a significant percentage of early and late apoptosis of 75.8 and 78.4%, respectively. This study reveals the potential cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D isolated from Benalu batu and its mechanism via apoptosis induction.

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Shen, Le, Xuewei Zhu, Yan Wang, Wuwei Zeng, Gang Wu, Hong Xue, and Baosheng Chen. "Secreted human apolipoprotein(a) kringle IV-10 and kringle V inhibit angiogenesis and xenografted tumor growth." Biological Chemistry 389, no. 2 (February 1, 2008): 135–41. http://dx.doi.org/10.1515/bc.2008.016.

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Abstract Angiogenesis plays an important role in normal physiology of blood vessel growth, but can contribute to the pathogenesis of diseases, such as cancer. A new anti-angiogenic recombinant kringle protein, composed of the fused domains of human apolipoprotein(a) carboxyl-terminal kringle IV-10 and kringle V, was expressed in Pichia pastoris and human colorectal carcinoma (HCT 116) cells to investigate its influence on angiogenesis and tumor growth. The mature recombinant protein exhibited the characteristic features of kringle-containing proteins (glycosylation and disulfide bond formation) and, when added to cultures of human umbilical vein endothelial cell, resulted in a 31% decrease in proliferation relative to untreated controls (p<0.05). The neo-angiogenesis was diminished by 63% in chick embryos treated with 10 μg recombinant protein compared with 7% for phosphate buffer solution-treated embryos (p<0.01). Transfection of a kringle IV-10-kringle V fusion protein construct into HCT 116 cells decreased tumorigenesis and inhibited tumor growth in vivo without affecting tumor cell proliferation. HCT 116 cells that expressed recombinant protein displayed a much lower relative growth ratio of 8% (p<0.01) against the control tumor cells. From these results, we conclude that human apolipoprotein(a) carboxyl-terminal kringle IV-10-kringle V fusion protein is an effective inhibitor of angiogenesis and angiogenesis-dependent tumor growth.

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Surti, Malvi, Mitesh Patel, Alya Redhwan, Lamya Ahmed Al-Keridis, Mohd Adnan, Nawaf Alshammari, and Mandadi Narsimha Reddy. "Ilimaquinone (Marine Sponge Metabolite) Induces Apoptosis in HCT-116 Human Colorectal Carcinoma Cells via Mitochondrial-Mediated Apoptosis Pathway." Marine Drugs 20, no. 9 (September 18, 2022): 582. http://dx.doi.org/10.3390/md20090582.

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Ilimaquinone (IQ), a metabolite found in marine sponges, has been reported to have a number of biological properties, including potential anticancer activity against colon cancer. However, no clear understanding of the precise mechanism involved is known. The aim of this study was to examine the molecular mechanism by which IQ acts on HCT-116 cells. The anticancer activity of IQ was investigated by means of a cell viability assay followed by the determination of induction of apoptosis by means of the use of acridine orange–ethidium bromide (AO/EB) staining, Annexin V/PI double staining, DNA fragmentation assays, and TUNEL assays. The mitochondrial membrane potential (ΔΨm) was detected using the JC-1 staining technique, and the apoptosis-associated proteins were analyzed using real-time qRT-PCR. A molecular docking study of IQ with apoptosis-associated proteins was also conducted in order to assess the interaction between IQ and them. Our results suggest that IQ significantly suppressed the viability of HCT-116 cells in a dose-dependent manner. Fluorescent microscopy, flow cytometry, DNA fragmentation and the TUNEL assay in treated cells demonstrated apoptotic death mode. As an additional confirmation of apoptosis, the increased level of caspase-3 and caspase-9 expression and the downregulation of Bcl-2 and mitochondrial dysfunction were observed in HCT-116 cells after treatment with IQ, which was accompanied by a decrease in mitochondrial membrane potential (ΔΨm). Overall, the results of our studies demonstrate that IQ could trigger mitochondria-mediated apoptosis as demonstrated by a decrease in ΔΨm, activation of caspase-9/-3, damage of DNA and a decrease in the proportion of Bcl-2 through the mitochondrial-mediated apoptosis pathway.

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39

Coşkun, Göknil, Teodora Djikic, Taha Hayal, Nezaket Türkel, Kemal Yelekçi, Fikrettin Şahin, and Ş. Küçükgüzel. "Synthesis, Molecular Docking and Anticancer Activity of Diflunisal Derivatives as Cyclooxygenase Enzyme Inhibitors." Molecules 23, no. 8 (August 6, 2018): 1969. http://dx.doi.org/10.3390/molecules23081969.

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Cyclooxygenase enzymes play a vital role in inflammatory pathways in the human body. Apart from their relation with inflammation, the additional involvement of COX-2 enzyme with cancer activity was recently discovered. In some cancer types the level of COX-2 enzyme is increased indicating that this enzyme could be a suitable target for cancer therapy. Based on these findings, we have synthesized some new diflunisal thiosemicarbazides and 1,2,4-triazoles and tested them against androgen-independent prostate adenocarcinoma (PC-3), colon carcinoma (HCT-116), human breast cancer (T47D), breast carcinoma (MCF7) and human embryonic kidney (HEK-293) cell lines. Specifically, the diflunisal and thiosemicarbazide functionality are combined during the synthesis of original compounds anticipating a potency enhancement. Compounds 6, 10, 15 and 16 did not show cytotoxic effects for the HEK293 cell line. Among them, compounds 15 and 16 demonstrated anticancer activity for the breast cancer cell line T47D, whereas compounds 6 and 10 which are thiosemicarbazide derivatives displayed anti-tumourigenic activity against the PC-3 cell line, consistent with the literature. However, no activity was observed for the HCT-116 cancer cell line with the tested thiosemicarbazide derivatives. Only compound 16 displayed activity against the HCT-116 cell line. Therefore, it was speculated that the diflunisal and thiosemicarbazide functionalities potentiate anticancer activity on prostate cancer and the thiosemicarbazide functionality decreases the anticancer activity of diflunisal on colon cancer cell lines. In order to gain insight into the anticancer activity and COX-2 inhibition, molecular docking studies were carried out for COX-1 and COX-2 enzymes utilizing the newly synthesized compounds 15, and 16. Both 15 and 16 showed high selectivity and affinity toward COX-2 isozyme over COX-1, which is in agreement with the experimental results.

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Ahmed, Nermien Z., Shaimaa R. Ibrahim, and Omar A. Ahmed- Farid. "Quercetin and Apigenin of Cymbopogon citratus mediate inhibition of HCT-116 and PC-3 cell cycle progression and ameliorate Doxorubicin-induced testicular dysfunction in male rats." Biomedical Research and Therapy 5, no. 7 (July 27, 2018): 2466–79. http://dx.doi.org/10.15419/bmrat.v5i7.457.

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Introduction: This study aims to elucidate the possible ameliorative effect of Cymbopogon citratus (CC), i.e. lemon grass, in a Doxorubicin (Dox)-induced male testicular damage and infertility model. Moreover, the anticancer role of the main active constituents of CC (Apigenin and Quercetin) was evaluated on prostatic and colon cancer (PC-3 and HCT-116 carcinoma cell lines, respectively). Methods: In vitro studies of the cell lines were carried out to determine the IC50 of each active constituent of CC, in order to select the most suitable dose for in vivo studies. For the in vivo studies, 24 rats were divided into 4 groups: Group 1 received saline treatment (negative control), Group 2 received treatment with CC (300 mg/kg body weight (b.w.)), Group 3 received Dox treatment (25 mg/kg b.w. intraperitoneally (i.p.)) on day 9 of the study, and Group 4 received CC treatment followed by Dox treatment on day 9 of the study. All the treatments were administered orally for 10 consecutive days. Results: The data revealed that Apigenin and Quercetin (AQ) had greater potency against PC-3 cells than HCT-116 cells. In vivo studies demonstrated that Dox treatment induced testicular damage and increased nitrosative stress, inflammation, and cell death, while decreasing cell energy markers for testes. In contrast, rats treated with CC only, or in parallel with Dox, showed ameliorative responses against Dox; they also showed greater testicular activity than normal, which reflected the ability of CC to significantly improve reproductive health performance. Conclusion: In conclusion, CC inhibits the activity and growth of PC-3 and HCT-116 carcinoma cell lines and, moreover, the whole extract of CC ameliorates testicular dysfunction induced by Dox.

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Li, Tie-Ling, Hai-Feng Guo, Fu-Juan Li, Zhi-Guo Sun, and Heng-Chun Zhang. "Synthesis and biological evaluation of 6H-1-benzopyrano[4,3-b]quinolin-6-one derivatives as inhibitors of colon cancer cell growth." Bangladesh Journal of Pharmacology 10, no. 3 (August 1, 2015): 660. http://dx.doi.org/10.3329/bjp.v10i3.23645.

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<p class="Abstract">A convenient synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-one derivatives was reported using 4-chloro-2-oxo-2H-chromene-3-carbaldehyde with different aromatic amines using silica sulfuric acid. The compounds were tested for their anticancer activity against colon (HCT-116 and S1-MI-80), prostate (PC3 and DU-145), breast (MCF-7 and MDAMB-231) cancer cells. These com-pounds showed more selectivity and potent cytotoxic activity against colon cancer cells. 3c was tested against five other colon cancer cell lines (HT-29, HCT-15, LS-180, LS-174, and LoVo), which had similar cytotoxicity and selectivity. 3c did not induce PXR-regulated ABCB1 or ABCG2 transporters. In fact, 3c induced cytotoxicity in HEK293 cells over expressing ABCB1 or ABCG2 to the same extent as in normal HEK293 cells. It was cytotoxic approximately 3- and 5-fold to resistant colon carcinoma S1-MI-80 cells. 3c also produced concentration-dependent changes in HCT-116 colon cancer cells, in mitochondrial membrane potential, leading to apoptosis, and sub-micromolar concentrations caused chromosomal DNA fragmentation. </p><p> </p>

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Batubara, Irmanida, Arif Rakhman Hakim, Silmi Mariya, Suminar Setiati Achmadi, Valentina Sokoastri Valentina Sokoastri, Agustin Sri Mulyatni, and Rohayati Suprihatini. "The Potential of 9,10-Anthraquinone in Inhibiting Human Cancer Cells Growth." Indonesian Journal of Cancer 15, no. 1 (March 31, 2021): 19. http://dx.doi.org/10.33371/ijoc.v15i1.780.

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Background: 9,10-Anthraquinone (9,10-AQ) is a contaminant on some agricultural products and considered as carcinogenic based on EU Regulation No. 1146/2014. Except for little evidence on experimental rats, there is no strong proof regarding the carcinogenicity in humans. Therefore, it is essential to find a safe dose of this compound since the difference in 9,10-AQ levels will affect cancer cell growth. This research aims to find the 9,10-AQ concentration that does not proliferate the human cancer cells under in vitro study.Methods: In determining the 9,10-AQ concentration that does not proliferate the cancer cells growth, 0.01 to 500 mg/L 9,10-AQ was directly tested on four human cancer cells (colorectal carcinoma HCT 116, colon adenocarcinoma WiDr, breast cancer MCF-7, and cervical cancer HeLa), and the viability of the cells was counted via (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) assay. In the gene expression level, the effects on a selected cancer cell line were determined by qRT-PCR against BAX, BCL-2, PCNA, and P53.Results: The result indicates that 9,10-AQ up to 500 mg/L concentration does not proliferate the cell’s growth but instead inhibits those four cancer cells’ growths. The concentration of 9,10-AQ that inhibits 50% the cancer cells growth (IC50) value was 321.8 mg/L (1.55 mM) against HCT 116 and above 500 mg/L (above 2.40 mM) against WiDr, MCF-7, and HeLa. The 9,10-AQ at 500 mg/L (or 2.40 mM) increases BAX expression and acts as an apoptotic agent on HeLa cells.Conclusions: The investigation has shown that 9,10-AQ up to 500 mg/L concentration does not proliferate the cancer cell growth; instead, it inhibits the HCT 116 and HeLa cells growth. We have preliminary evidence regarding the apoptotic mechanism of 9,10-AQ by increasing BAX gene expression on HeLa cells.

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Tamang, Bunu, Qi Liang, Biju Balakrishnan, Su Peng, and Wei Zhang. "Astragalus Shiitake—A Novel Functional Food with High Polysaccharide Content and Anti-Proliferative Activity in a Colorectal Carcinoma Cell Line." Nutrients 14, no. 11 (June 2, 2022): 2333. http://dx.doi.org/10.3390/nu14112333.

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The chemical and nutritional constituents of mushrooms can alter significantly when grown on different substrates. Based on this fact, an approach was made to cultivate a new type of mushroom, Hengshan Astragalus Shiitake, by growing Shiitake mushrooms on beds supplemented with the roots of an edible herbal plant, Astragalus membranaceus. In this study, three green extraction techniques, including microwave-enzyme assisted (MEA), ultrasound-enzyme assisted (UEA) and microwave-ultrasound-enzyme assisted (MUEA) extractions, were used to compare both the yield and antiproliferative activity of the polysaccharide-rich extracts (PREs) from HAS in human colorectal carcinoma cells (HCT 116). Both HAS-A and HAS-B extracts contain significantly higher amounts of polysaccharides when compared to the control (Shiitake extract), regardless of the extraction methods. The PREs from HAS-B have significantly higher anti-proliferative activity in HCT 116 compared to the control when using the UEA extraction method. Our findings demonstrate that HAS-B can become a novel functional food with anti-proliferative activities and the optimization of UEA extraction would help to develop new active extract-based health products.

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Sananda Dey, Nensina Murmu, Mijanur R Molla, Sandeep K Dash, and Biplab Giri. "Parthenolide Induces Oxidative Stress and Impedes Cell Migration by Suppressing Wnt Pathway and Epithelial-Mesenchymal-Transition (EMT) in HCT-116 Metastatic Colorectal Cancer Cells." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 21, 2020): 2313–23. http://dx.doi.org/10.26452/ijrps.v11ispl4.4459.

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Colorectal cancer (CRC) is a vital cause of cancer morbidity and mortality. 50% of CRC patients suffer from an aggressive metastatic disease which ultimately fallout in death. In metastatic cancer, tumour cells migrate, invade, and finally colonise to the distant organ by degrading their attachments with the extracellular matrix. Parthenolide (PTL) is a secondary metabolite of feverfew (Tanacetum parthenium) plant. It shows its cytotoxic effect towards cancer cells via different cellular signalling pathways like inhibition of NF-κB, STAT3, MAPK, JNK pathways, activation of p53 etc. In the present study, we have assessed anti-cancer and anti-metastatic potential of PTL against human HCT-116 metastatic colorectal cancer cells. Analysis of cellular oxidative status (GSH/GSSG) of PTL treated HCT-116 cells showed a significant decrease (p<0.05) in GSH level while GSSG level was increased significantly (p<0.05) on PTL treatment. PTL also increased the amount of intracellular reactive oxygen species. The qRT-PCR analysis revealed that PTL down-regulates c-fos, c-jun and N-cadherin expression and up-regulates E-cadherin expression indicating inhibition of cell migration and metastasis by EMT pathway. PTL inhibited the MMP-9 expression in a dose-dependent fashion and inhibited cancer cell migration by regulating Wnt/β-catenin signalling through the up-regulation of DKK-1 protein expression indicating PTL has a promising anti-cancer potential against HCT-116 metastatic colorectal carcinoma cells.

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Jin, GuiLin, Zhen Luo, Mingke Fen, and Lijun Xu. "Peiminine regulates the biological characteristics of colorectal cancer cells via P13K/Akt/mTOR and oxidative stress pathways." Tropical Journal of Pharmaceutical Research 21, no. 5 (June 16, 2022): 921–25. http://dx.doi.org/10.4314/tjpr.v21i5.2.

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Purpose: To investigate the influence of peiminine on biological characteristics of colorectal cancer cells, and the underlying mechanism.Methods: Two groups of cultured human colorectal cancer HCT-116 cells were used: peiminine and control groups. Peiminine group cells were exposed to the drug at a final concentration of 100 μmol/L. The effect of peiminine on cell proliferation was determined with CCK-8 method, while its effect on apoptosis was determined with flow cytometric method. Cell migration was determined with scratch test. The effect of peiminine on the expressions of proteins associated with the P13K/Akt/mTOR pathway and Wnt/β-catenin pathway in HCT-116 cells was determined with Western blotting assay.Results: Cell proliferation was markedly reduced in the peiminine group, relative to control (p < 0.05). There was higher percentage cell apoptosis in peiminine-treated cells than in control. Moreover, cell migration potential was significantly lower in the peiminine-treated cells. There were significantly downregulated levels of p-P13K, p-Akt and p-mTOR expressions in peiminine group, relative to the corresponding control expressions (p < 0.05). However, there were significantly higher relative expression of Wnt in peiminine group than in control cells, but β-catenin level was reduced, relative to the corresponding control level (p < 0.05).Conclusion: These data indicate that peiminine suppresses the proliferative, apoptotic and migratory potential of colorectal carcinoma HCT-116 cells via regulation of P13K/Akt/mTOR and oxidative stress pathways.

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ALBEDAIR, Lamia A. "Iron(III), gold(III), platinum(IV) and palladium(II) trimethoprim drug complexes: synthesis, spectroscopic, morphological and anticancer assessments." Revue Roumaine de Chimie 65, no. 12 (2021): 1145–52. http://dx.doi.org/10.33224/rrch.2020.65.12.09.

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Iron(III), gold(III), platinum(IV) and palladium(II) complexes of trimethoprim (TMP) drug were synthesized and well characterized using elemental analysis, conductance measurements, (UV-Vis, FTIR, 1HNMR and X-ray powder diffraction) spectroscopy. The Au(III), Pt(IV) and Pd(II) complexes have a four coordinate geometry comprising one molecules of the TMP drug and two coordinated chloride ions, while, iron(III) complex has an octahedral geometry containing one TMP, three chloride and one coordinated water molecules. The TMP drug acts as a bi-dentate chelate towards the metal ions through the nitrogen atoms of the two amino groups attached with pyrimidine ring, this was confirmed by spectroscopic analyses with the molecular formulas [Fe(TMP)Cl3(H2O)].4H2O, [Au(TMP)Cl2]Cl2H2O, [Pt(TMP)Cl2]Cl22H2O and [Pd(TMP)Cl2]. The transmission electron microscopy (TEM) and XRD analyses deduced that the gold(III) complex has a nano-scale range at ~ 10 nm. The [Au(TMP)Cl2]Cl2H2O complex was screened for its cytotoxicity evaluation against hepatocellular carcinoma (HepG2) and colon carcinoma (HCT-116) cell lines. It is showed that the IC50 of gold(III) complex are 7.46 µg/mL and 9.30 µg/mL against HepG2 and HCT-116 cancer cell lines, respectively.

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Park, Jong-Hwa, Yuan-Yuan Fu, In Sik Chung, Tae-Ryong Hahn, and Man-Ho Cho. "Cytotoxic property of ultraviolet-induced rice phytoalexins to human colon carcinoma HCT-116 cells." Journal of the Korean Society for Applied Biological Chemistry 56, no. 2 (February 28, 2013): 237–41. http://dx.doi.org/10.1007/s13765-012-3238-3.

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Mabkhot, Yahia N., H. Algarni, Abdulrhman Alsayari, Abdullatif Bin Muhsinah, Nabila A. Kheder, Zainab M. Almarhoon, and Faiz A. Al-aizari. "Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives." Molecules 24, no. 9 (April 26, 2019): 1654. http://dx.doi.org/10.3390/molecules24091654.

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A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing 1H-NMR, 13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.

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Al-Yousef, Hanan M., Wafaa H. B. Hassan, Sahar Abdelaziz, Musarat Amina, Rasha Adel, and May A. El-Sayed. "UPLC-ESI-MS/MS Profile and Antioxidant, Cytotoxic, Antidiabetic, and Antiobesity Activities of the Aqueous Extracts of Three Different Hibiscus Species." Journal of Chemistry 2020 (June 25, 2020): 1–17. http://dx.doi.org/10.1155/2020/6749176.

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The aqueous extracts of Hibiscus calyphyllus (HcA), Hibiscus micranthus (HmA), and Hibiscus deflersii (HdA) growing in Saudi Arabia did not receive enough attention in phytochemical and biological studies. This inspired the authors to investigate the phytochemicals of these extracts for the first time using UPLC-ESI-MS/MS in negative and positive ionization modes. The analysis afforded the tentative identification of 103 compounds including phenolic compounds, flavonoids, and anthocyanins. Moreover, in vitro evaluations of their cytotoxic, antioxidant, antidiabetic, and antiobesity activities were carried out. The results showed that aqueous extract of Hibiscus calyphyllus had the highest activity as an antioxidant agent (SC50 = 111 ± 1.5 μg/mL) compared with ascorbic acid (SC50 = 14.2 ± 0.5 μg/mL). MTT assay was used to evaluate cytotoxic activity compared to cisplatin. Hibiscus deflersii showed the most potent cytotoxic effect against A-549 (human lung carcinoma) with IC50 = 50 ± 5.1 μg/mL, and Hibiscus micranthus showed a close effect with IC50 = 60.4 ± 1.7 μg/mL. Hibiscus micranthus showed the most potent effect on HCT-116 (human colon carcinoma) with IC50 = 56 ± 1.9 μg/mL compared with cisplatin (IC50 = 7.53 ± 3.8 μg/mL). HcA and HdA extracts showed weak cytotoxic activity against A-549 and HCT-116 cell lines compared to the other extracts. Eventually, Hibiscus deflersii showed astonishing antidiabetic (IC50 = 56 ± 1.9 μg/mL) and antiobesity (IC50 = 95.45 ± 1.9 μg/mL) activities using in vitro α-amylase inhibitory assay (compared with acarbose (IC50 = 34.71 ± 0.7 μg/mL)) and pancreatic lipase inhibitory assay (compared with orlistat (IC50 = 23.8 ± 0.7 μg/mL)), respectively. In conclusion, these findings are regarded as the first vision of the phytochemical constituents and biological activities of different Hibiscus aqueous extracts. Hibiscus deflersii aqueous extract might be a hopeful origin of functional constituents with anticancer (on A-549 cell line), antidiabetic, and antiobesity activities. It might be a natural alternative remedy and nutritional policy for diabetes and obesity treatment without negative side effects. Isolation of the bioactive phytochemicals from the aqueous extracts of aerial parts of Hibiscus calyphyllus, Hibiscus micranthus, and Hibiscus deflersii and estimation of their biological effects are recommended in further studies.

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Sabbah, Dima A., Bara’a A. Al-Azaideh, Wamidh H. Talib, Rima Hajjo, Kamal Sweidan, Aya M. Al-Zuheiri, Ghassan Abu Sheikha, and Sawsan Shraim. "New derivatives of sulfonylhydrazone as potential antitumor agents: Design, synthesis and cheminformatics evaluation." Acta Pharmaceutica 71, no. 4 (April 3, 2021): 545–65. http://dx.doi.org/10.2478/acph-2021-0043.

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Abstract Phosphoinositide 3-kinase α (PI3Kα) is a propitious target for designing anticancer drugs. A series of new N’-(diphenylmethylene)benzenesulfonohydrazide was synthesized and characterized using FT-IR, NMR (1H and 13C), HRMS, and elemental analysis. Target compounds exhibited an antiproliferative effect against the human colon carcinoma (HCT-116) cell line. Our cheminformatics analysis indicated that the para-tailored derivatives [p-NO2 (3) and p-CF3 (7)] have better ionization potentials based on calculated Moran autocorrelations and ionization potentials. Subsequent in vitro cell proliferation assays validated our cheminformatics results by providing experimental evidence that both derivatives 3 and 7 exhibited improved antiproliferative activities against HCT-116. Hence, our results emphasized the importance of electron-withdrawing groups and hydrogen bond-acceptors in the rational design of small-molecule chemical ligands targeting PI3Kα. These results agreed with the induced-fit docking against PI3Kα, highlighting the role of p-substituted aromatic rings in guiding the ligand-PI3Kα complex formation, by targeting a hydrophobic pocket in the ligand-binding site and forming π-stacking interactions with a nearby tryptophan residue.

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