Статті в журналах з теми "In vitro biological evaluation"

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1

Morais, Shabna Roupal, R. Ram Narayanan, K. P. Sushmitha, N. Suchithra, Shruti Shankar, and M. Sugumar. "In vitro Biological Evaluation of Acanthophora spicifera." Research Journal of Pharmacy and Technology 13, no. 10 (2020): 4777. http://dx.doi.org/10.5958/0974-360x.2020.00840.9.

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2

Sheema, Sheema, Salman Zafar Salman Zafar, Nazif Ullah Nazif Ullah, Ishaq khan Ishaq khan, and and Ghias ud din and Ghias ud din. "Phytochemical and In Vitro Biological Evaluation of Roots of Malvastrum coromandelianum (L.) Garcke." Journal of the chemical society of pakistan 45, no. 6 (2023): 568. http://dx.doi.org/10.52568/001399/jcsp/45.06.2023.

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Malvastrum coromandelianum (L.) Garcke is a medicinal plant, employed traditionally for the treatment of different human illnesses. This study has been planned to study the chemical and biological aspects of the roots of the plant, using chemical and instrumental analytical techniques. Standard reported protocols were used for phytochemical screening of the crude extract, indicating the presence of terpenoids, steroids, flavonoids, and alkaloids classes of compounds. The extract was analyzed through Gas Chromatography-Mass Spectrometry (GC-MS) to confirm the presence of specific phytochemicals. The extract exhibited biological activities at good to moderate levels and was found to be non-toxic. Moderate inhibitory potential was observed against Aspergillus niger, Fusarium solani, Candida albicans, Klebsiella pneumoniae, Bacillus subtilis, Proteus mirabilis, Escherichia coli, and Staphylococcus aureus. At a concentration of 1000 μg/ml the crude extract showed 67 % inhibition of the Leishmania tropica promastigotes. The extract also displayed moderate radical scavenging activity. Interestingly, it showed lower red blood cell hemolysis (28%) at the highest concentration. The biological potential of the crude extract may be credited to these metabolites, as most of them have been previously reported to have the same activities.
3

Yusuf, Abdullah, Jiang-Yu Zhao, Paruke Aibibula, Ju-Bao Zhang, Guo-Zheng Huang, and Haji Akber Aisa. "Synthesis and in vitro Biological Evaluation of Cananodine." HETEROCYCLES 102, no. 3 (2021): 506. http://dx.doi.org/10.3987/com-20-14394.

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4

Halik, Paweł K., Przemysław Koźmiński, Joanna Matalińska, Piotr F. J. Lipiński, Aleksandra Misicka, and Ewa Gniazdowska. "In Vitro Biological Evaluation of Aprepitant Based 177Lu-Radioconjugates." Pharmaceutics 14, no. 3 (March 10, 2022): 607. http://dx.doi.org/10.3390/pharmaceutics14030607.

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Currently, the search for promising NK1R-positive tumor-targeting radiopharmaceuticals based on the structure of small molecular antagonists of neurokinin-1 receptor can be observed. Following this trend, we continued our evaluation of aprepitant-based 177Lu-radioconjugates in terms of future oncological applications. For this purpose, three novel aprepitant homologues were synthesized to broaden the previously obtained derivative portfolio, functionalized with the DOTA chelator and labeled with 68Ga and 177Lu. The newly evaluated radioconjugates showed the intended significant increase in lipophilicity compared to the previous ones, while maintaining stability in the human serum. Then, in a receptor binding study to the human NK1 receptor, we compared the two series of 177Lu-radioconjugates of aprepitant with each other and with the reference Substance P derivative currently used in glioblastoma therapy, clearly indicating the high affinity and better binding capacity of the novel radioconjugates. The in vitro experimental results included in the presented study, supported by labeling optimization, radioconjugate characterization and docking modeling of new aprepitant-derived radioagents, confirm our assumptions about the usefulness of aprepitant as a NK1R targeting vector and point out the perspectives for the forthcoming first in vivo trials.
5

Yi, Jiling, Zheng Zhao, Shipu Li, Yixia Yin, and Xinyu Wang. "In vitro biological evaluation of graphene on neuronal cells." Journal of Wuhan University of Technology-Mater. Sci. Ed. 31, no. 4 (July 30, 2016): 925–30. http://dx.doi.org/10.1007/s11595-016-1469-6.

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6

Rafaat, Mahmood Sherzad, Arzu Karatepe, Serhat Keser, Şule İnci, and Semih Dalkılıc. "In vitro Biological Evaluation of 1,2,4-triazole Mannich Base." BioMed Target Journal 1, no. 2 (December 30, 2023): 22–30. http://dx.doi.org/10.59786/bmtj.123.

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Biological evaluation of a 1,2,4-triazole mannich base that has been synthesized for interesting behavior in medicinal chemistry, so it’s interesting to synthesize triazole derivatives and investigate their biological properties to evaluate their capacity in medicine. The aim of this study evaluate the antimicrobial, anticancer, and antioxidant activities of a 1,2,4-triazole Mannich base derivative and its power in the treatment of diseases. For antimicrobial activity four bacterial strains and one fungal strain based on the agar disc diffusion. While used two cancer cell lines for anticancer activity which are known as Hep-G2 and MCF-7; the antioxidant activity of the compound used three different radical species include OH•, ABTS•+, and DPPH•, and also determine the antioxidant activity of the compound after extracting vitamins A, C, E, and MDA in the S. cerevisiae yeast cell by HPLC. The results of this study show the positive role of a derivative 1,2,4-triazole mannich base as antimicrobial and antiradical assays, particularly when treated with C. albicans and OH• radical that significantly reduced growth of the fungal and the radical compared to others. In addition, it didn’t exhibit any cytotoxicity to reduce both cancer cell lines. In conclusion, the compound's ability is different from one assay to another, increasing its concentration efficiency affects the radical scavenging, and inhibits microorganism growth.
7

Ourhzif, El-Mahdi, Caroline Decombat, Isabelle Abrunhosa-Thomas, Laetitia Delort, Mostafa Khouili, Mohamed Akssira, Florence Caldefie-Chezet, Pierre Chalard, and Yves Troin. "Synthesis and Biological Evaluation of New Naphthoquinones Derivatives." Current Organic Synthesis 17, no. 3 (June 9, 2020): 224–29. http://dx.doi.org/10.2174/1570179417666200212111956.

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: New substituted 1,4-naphthoquinones have been prepared in good overall yields through the naphthol route. The cytotoxicity of these compounds was tested in vitro on MCF-7 breast tumor cells. The most active compound 14 displayed an IC50 of 15μM. Objective: To investigate the cytotoxicity of new naphthoquinones derivatives on MCF-7 cells. Methods: Synthesis of new naphtoquinones derivatives and in vitro evaluation of their cytotoxicity on MCF-7 cells (rezasurin cell-based assay). Results: Starting from Ethyl 4-hydroxy-6,7-dimethoxy-2-naphthoate, four naphthoquinones were prepared and exhibited substantial cytotoxicity against MCF-7 cells. Conclusion: Preliminary studies of the structure-activity relationship have shown the influence of the structural parameters and, in particular, the nature of the naphthoquinone side chain.
8

Abdul-Rida, Nabeel A., and Kawther M. Talib. "NEW CHALCONE DERIVATIVES AS ANTICANCER AND ANTIOXIDANT AGENTS: SYNTHESIS, MOLECULAR DOCKING STUDY AND BIOLOGICAL EVALUATION." Chemical Problems 22, no. 2 (2024): 177–86. http://dx.doi.org/10.32737/2221-8688-2024-2-177-186.

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In this approach, a series of new chalcone derivatives bearing baclofen drug were synthesized via Claisen-Schmidt condensation and evaluated in vitro as anticancer and antioxidant agents. The newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR spectra, and elemental analysis. All products were screened in vitro against both cell lines HdFn and MCF-7. The cytotoxicity assay results revealed that derivatives 5a and 5d exhibited good inhibition for cell lines MCF-7 with IC50 values 32.5 and 37.6 µM, respectively while 5a and 5c exhibited acceptable inhibition for HdFn with IC50 values 76.7 and 78.6 µM, respectively, compared to the Tamoxifen drug. Molecular docking study of the target compounds confirmed the results of the cytotoxicity test. In addition, results of the DPPH investigation revealed good antioxidant activity for derivatives 5a, 5c and 5d with inhibition percentages 86.62, 81.38, and 76.42%, respectively, compared to ascorbic acid.
9

Niesyto, Katarzyna, Wiktoria Łyżniak, Magdalena Skonieczna, and Dorota Neugebauer. "Biological In Vitro Evaluation of PIL Graft Conjugates: Cytotoxicity Characteristics." International Journal of Molecular Sciences 22, no. 14 (July 20, 2021): 7741. http://dx.doi.org/10.3390/ijms22147741.

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In vitro cytotoxicity of polymer-carriers, which in the side chains contain the cholinum ionic liquid units with chloride (Cl) or pharmaceutical anions dedicated for antituberculosis therapy, i.e., p-aminosalicylate (PAS) and clavulanate (CLV), was investigated. The carriers and drug conjugates were examined, in the concentration range of 3.125–100 μg/mL, against human bronchial epithelial cells (BEAS-2B) and adenocarcinomic human alveolar basal epithelial cells (A549) as an experimental model cancer cell line possibly coexisting in tuberculosis. The cytotoxicity was evaluated by MTT test and confluency index, as well as by the cytometric analyses, including Annexin-V FITC apoptosis assay. The polymer systems showed supporting activity towards the normal cells and no tumor progress, especially at the highest concentration (100 μg/mL). The analysis of cell death did not show meaningful changes in the case of the BEAS-2B, whereas in the A549 cell line, the cytostatic activity was observed, especially for the drug-free carriers, causing death in up to 80% of cells. This can be regulated by the polymer structure, including the content of cationic units, side-chain length and density, as well as the type and content of pharmaceutical anions. The results of MTT tests, confluency, as well as cytometric analyses, distinguished the polymer systems with Cl/PAS/CLV containing 26% of grafting degree and 43% of ionic units or 46% of grafting degree and 18% of ionic units as the optimal systems.
10

Hashimoto, Akiko, Takeji Takamura‐Enya, and Yoshimitsu Oda. "Synthesis and In Vitro Biological Evaluation of Psoralen‐Linked Fullerenes." Photochemistry and Photobiology 95, no. 6 (August 30, 2019): 1403–11. http://dx.doi.org/10.1111/php.13138.

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11

Alam, Fiaz, and Qazi Najam us Saqib. "Evaluation of Zanthoxylum armatum Roxb for in vitro biological activities." Journal of Traditional and Complementary Medicine 7, no. 4 (October 2017): 515–18. http://dx.doi.org/10.1016/j.jtcme.2017.01.006.

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12

Zhang, Yaling, Ying Zhang, Juan Liu, Li Chen, Lijun Zhao, Baolin Li, and Wei Wang. "Synthesis and in vitro biological evaluation of novel quinazoline derivatives." Bioorganic & Medicinal Chemistry Letters 27, no. 7 (April 2017): 1584–87. http://dx.doi.org/10.1016/j.bmcl.2017.02.027.

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13

Soni, Love Kumar, Tamanna Narsinghani, and Anand Sethi. "Anti-microbial benzimidazole derivatives: synthesis and in vitro biological evaluation." Medicinal Chemistry Research 21, no. 12 (January 18, 2012): 4330–34. http://dx.doi.org/10.1007/s00044-012-9976-2.

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14

Kainthan, Rajesh Kumar, Samuel R. Hester, Elena Levin, Dana V. Devine, and Donald Elliott Brooks. "In vitro biological evaluation of high molecular weight hyperbranched polyglycerols." Biomaterials 28, no. 31 (November 2007): 4581–90. http://dx.doi.org/10.1016/j.biomaterials.2007.07.011.

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15

Ventura, Cinzia Anna, Carmela Cannavà, Rosanna Stancanelli, Donatella Paolino, Donato Cosco, Antonio La Mantia, Rosario Pignatello, and Silvana Tommasini. "Gemcitabine-loaded chitosan microspheres. Characterization and biological in vitro evaluation." Biomedical Microdevices 13, no. 5 (May 24, 2011): 799–807. http://dx.doi.org/10.1007/s10544-011-9550-6.

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16

Baranyai, Zsuzsa, Martin Krátký, Rudolf Vosátka, Eleonóra Szabó, Zsuzsanna Senoner, Sándor Dávid, Jiřina Stolaříková, Jarmila Vinšová, and Szilvia Bősze. "In vitro biological evaluation of new antimycobacterial salicylanilide-tuftsin conjugates." European Journal of Medicinal Chemistry 133 (June 2017): 152–73. http://dx.doi.org/10.1016/j.ejmech.2017.03.047.

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17

Smit, Frans J., Riëtte A. van Biljon, Lyn-Marie Birkholtz, and David D. N'Da. "Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters." European Journal of Medicinal Chemistry 90 (January 2015): 33–44. http://dx.doi.org/10.1016/j.ejmech.2014.11.016.

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18

Vaesken, Antoine, Christian Pidancier, Nabil Chakfe, and Frederic Heim. "Hybrid textile heart valve prosthesis: preliminary in vitro evaluation." Biomedical Engineering / Biomedizinische Technik 63, no. 3 (June 27, 2018): 333–39. http://dx.doi.org/10.1515/bmt-2016-0083.

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Abstract Transcatheter aortic valve implantation (TAVI) is nowadays a popular alternative technique to surgical valve replacement for critical patients. Biological valve tissue has been used in these devices for over a decade now with over 100,000 implantations. However, material degradations due to crimping for catheter insertion purpose have been reported, and with only 6-year follow-up, no information is available about the long-term durability of biological tissue. Moreover, expensive biological tissue harvesting and chemical treatment procedures tend to promote the development of synthetic valve leaflet materials. Textile polyester (PET) material is characterized by outstanding folding and strength properties combined with proven biocompatibility and could therefore be considered as a candidate to replace biological valve leaflets in TAVI devices. Nevertheless, the material should be preferentially partly elastic in order to limit water hammer effects at valve closing time and prevent exaggerated stress from occurring into the stent and the valve. The purpose of the present work is to study in vitro the mechanical as well as the hydrodynamic behavior of a hybrid elastic textile valve device combining non-deformable PET yarn and elastic polyurethane (PU) yarn. The hybrid valve properties are compared with those of a non-elastic textile valve. Testing results show improved hydrodynamic properties with the elastic construction. However, under fatigue conditions, the interaction between PU and PET yarns tends to limit the valve durability.
19

Venkateshwarlu, R., B. Chinnababu, U. Ramulu, K. Purushotham Reddy, M. Damoder Reddy, P. Sowjanya, P. Venkateswara Rao, and S. Aravind. "Synthesis and biological evaluation of (−)-kunstleramide and its derivatives." MedChemComm 8, no. 2 (2017): 394–404. http://dx.doi.org/10.1039/c6md00606j.

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20

Ju liu, Ju liu, Jun Li Jun Li, Jian tao Shi Jian tao Shi, Jie Li Jie Li, Xue chen Hao Xue chen Hao, Duang zheng Song Duang zheng Song, Yang Wang Yang Wang, and Shi Ding and Ye Chen Shi Ding and Ye Chen. "Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives." Journal of the chemical society of pakistan 42, no. 4 (2020): 564. http://dx.doi.org/10.52568/000659.

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A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.
21

Ju liu, Ju liu, Jun Li Jun Li, Jian tao Shi Jian tao Shi, Jie Li Jie Li, Xue chen Hao Xue chen Hao, Duang zheng Song Duang zheng Song, Yang Wang Yang Wang, and Shi Ding and Ye Chen Shi Ding and Ye Chen. "Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives." Journal of the chemical society of pakistan 42, no. 4 (2020): 564. http://dx.doi.org/10.52568/000659/jcsp/42.04.2020.

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A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.
22

Mishra, Shweta, Debashree Das, Adarsh Sahu, Shailendra Patil, Ram Kishore Agrawal, and Asmita Gajbhiye. "Phosphonate Derivatives of 3,5-bis(arylidene)-4-piperidone: Synthesis and Biological Evaluation." Anti-Infective Agents 18, no. 3 (September 11, 2020): 245–54. http://dx.doi.org/10.2174/2211352517666190820143735.

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Background: 3,5-Bis(arylidene)-4-piperidinones (BAP) belong to a wide class of cross conjugated dienones. The 1,5-diaryl-3-oxo-1,4-pentadienyl fragment of the BAP moiety is responsible for the molecule's anti-tumor, antioxidant, antimicrobial and anti-inflammatory manifestations. In the present study, we present combinations of phosphonate and 3,5-bis(arylidene)-4- piperidone pharmacophores. The anti-inflammatory, anti-oxidant potential, anti-proliferative, cytotoxic potential and antimicrobial of the title compounds were evaluated in in-vitro bioassay paradigms. Methods: A novel class of phosphonate linked 3,5-Bis(aryl methylene)-4-piperidone derivatives were synthesized from simple, versitalie and efficient synthetic methodology. All of the synthesized compounds were screened for their in vitro anti-inflammatory, in vitro anti-oxidant potential, in vitro anti-proliferative, in vitro cytotoxic potential and in vitro antimicrobial activity. Amongst all the synthesized compounds in series, phosphonate derivatives of 3,5-Bis(arylmethylene)-4- piperidone containing 4-hydroxy-3-methoxyphenyl curcumin like prototype were more active than phenyl substituted compounds. Results: The results of the screening revealed that compounds 5e, 5f, 5g, 5h were more active candidates as compared to 5a, 5b, 5c and 5d, however 5d can be readily endorsed as the most active compound of the series. Structure- activity relationship of the synthesized series suggested that structural resemblance of the synthesized compounds with that of curcumin was enormously accountable for the compounds anti-inflammatory, antioxidant and cytotoxic potential activity. Conclusion: The in-vitro biological spectrum indicated that the substitution of groups at third and fourth position and alkyl phosphonates substitution potentiates the activity as compared to curcumin.
23

Liu, Gai-Zhi, Yan-Bin Guan, Ya Wu та Hong-Min Liu. "Synthesis and Biological Evaluation of Novelγ-Alkylidene Butenolides". Journal of Chemistry 2013 (2013): 1–8. http://dx.doi.org/10.1155/2013/926723.

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Three new series of 4-substituted-5-alkylidene-2,5-dihydrofuran-2-ones were synthesized. The in vitro activity test results showed that some of them exhibited good antibacterial and cytotoxic activities. Among them compound5cshowed the most potent antibacterial activity againstEscherichia coliwith the MIC value of 20.00 μg/mL. Compound9cshowed good cytotoxic activity against Ec9706 cells withIC50value of 19.39 μM, better than that of the reference compound fluorouracil (IC50=37.74 μM).
24

Kumar Baba, N. H., D. Ashok, Boddu Ananda Rao, Sarasija Madderla, and N. Y. S. Murthy. "Microwave-assisted synthesis and biological evaluation of thiazole-substituted dibenzofurans." Heterocyclic Communications 24, no. 3 (June 27, 2018): 171–76. http://dx.doi.org/10.1515/hc-2017-0247.

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AbstractNew thiazole-substituted dibenzofurans 7a–j were synthesized from dibenzofuran derivatives 5a–b and substituted thiosemicarbazones 6a–h under conventional and microwave irradiation conditions. The structures of all products were established on the basis of analytical and spectral data. The synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative strains. Compounds 7b, 7d and 7h are active against Bacillus subtilis (+ve), and compound 7i displays good activity against Pseudomonas aeruginosa (-ve) strain. Compounds 7a–j were also evaluated for their in vitro antimycobacterial activity, and compound 7b shows antimycobacterial activity against Mycobacterium bovis strain.
25

M. Hassan, M. Hassan, Zafar Iqbal Zafar Iqbal, Fazli Nasir Fazli Nasir, Ismail Khan Ismail Khan, Fahim U. Khan Fahim U. Khan, Farhad Ullah Farhad Ullah, and Saifullah Khan and Nabeela Niaz Saifullah Khan and Nabeela Niaz. "Simultaneous Determination of Etoposide and Paclitaxel in Biological and Pharmaceutical Samples by RP-HPLC; Method Development." Journal of the chemical society of pakistan 41, no. 5 (2019): 874. http://dx.doi.org/10.52568/000790/jcsp/41.05.2019.

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A simple, rapid and sensitive RP-HPLC-UV method was developed for quantification of paclitaxel (PTX) and etoposide (ETO) in biological and pharmaceutical samples. Optimization of experimental conditions were performed and standard guidelines were used for the validation of the method. Analytes were separated on Pruospher® Star RP- 18e (250mm × 4.6mm, 5µm) column using ACN and TFA (0.025%) as mobile phase in the ratio of (60:40V/V) with a flow rate of 1 mL/min and detector set at 235 nm. Protein precipitation method was applied for the extraction of analytes from biological samples. The method was applied to in-vitro and in-vivo evaluation of polymeric nanoparticles of etoposide. Solvent evaporation technique was used for the preparation of polymeric nanoparticles (NPs) using polymer PLGA (75:25) and poloxamer as surfactant. The linearity of the method is in the range of 14-500 ng / mL for paclitaxel and 12-1000 ng/mL for etoposide. The LLOD were 5 and 6 ng/mL while the LLOQ were 12 and 14 ng/mL for etoposide and paclitaxel, respectively. The developed method was precise and its intra and inter day co-efficient of variance was below 1%. The method was used for in-vitro and in-vivo evaluation of PLGA polymeric nanoparticles of etoposide. In-vitro evaluation included determination of drug content and drug release while in-vivo evaluation consisted of pharmacokinetic evaluation.
26

Godwin, Lisa A., Divya Sukumar, Sarah Moreno, Matthew Giedd, Connie Chung, Michelle Massee, Heather Bara, Thomas J. Koob, and John Harper. "Biological Evaluation of a Native Amniotic Membrane Allograft." Foot & Ankle Orthopaedics 7, no. 4 (October 2022): 2473011421S0067. http://dx.doi.org/10.1177/2473011421s00672.

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Category: Basic Sciences/Biologics; Other Introduction/Purpose: Placental tissue allografts have long been used as effective wound dressings for hard to heal wounds and are demonstrating increasing utility in the field of foot and ankle surgeries. Previous observations of the PURION-processed dehydrated amnion/chorion membrane (dHACM) demonstrated retention of regulatory proteins inherent to amniotic tissues and preservation of the bioactivity to stimulate cellular activities. Novel and patent-pending processing techniques have been developed to introduce a thicker and more robust allograft, as compared to dHACM. Lyophilized human amnion chorion membrane (LHACM) will confer versatility to clinicians with improved handling while maintaining the natural tissue composition and intrinsic biological activities. This study characterizes the biological properties of LHACM which may support the healing cascade. Methods: LHACM was processed using a modified PURION process which incorporates an optimized cleansing process, enabling retention of the intermediate layer, and lyophilization. Tissue architecture was visualized with hematoxylin and eosin staining. The hygroscopic contribution of the intermediate layer was appraised with absorbency measurements. Cleansing efficiency was determined through quantification of residual hemin remaining in the tissue. Regulatory proteins were quantified using a multiplex ELISA. The cellular response to LHACM treatment was assessed using multiple in vitro assays targeting cellular proliferation and analysis of signaling pathways. Adult dermal fibroblasts (HDFs) cultured over a 3-day period in LHACM eluates were assessed for cellular proliferation. In vitro models were developed to assess the regulation of relevant signaling pathways, including TGF-β1 and Wnt/β-catenin for fibrotic and proliferative processes, respectively. Cellular responses were evaluated through quantitative PCR and cell reporter lines. Results: Histological evaluation showed that processing maintains the tissue structure. Absorption testing demonstrated LHACM is more hygroscopic than dHACM. Hemin analysis demonstrated low levels of residual hemin which were comparable for LHACM and dHACM allografts. Screening for regulatory proteins indicate that LHACM contains a diverse array of regulatory proteins, inherent to amniotic membranes. In vitro treatment of primary cells with LHACM eluates promoted dermal fibroblast proliferation as well as regulation of elevated TGFβ- and Wnt/β-catenin signaling. Conclusion: The processing method of LHACM maintains the intrinsic properties of amniotic membranes with similar levels of biological activity as compared to dHACM, while providing an option for a thicker allograft with alternative handling characteristics. LHACM represents a novel product concept which increases versatility of amniotic membrane application in varied outpatient and surgical uses.
27

Marcinčáková, D., N. Červeňáková, and M. Miłek. "In vitro Evaluation of Biological Effects of Dandelion (Taraxacum officinale) Extracts." Folia Veterinaria 62, no. 3 (September 1, 2018): 36–40. http://dx.doi.org/10.2478/fv-2018-0025.

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Abstract Dandelion (Taraxacum officinale) of the Asteraceae family is known for its pharmacological effects and has been used in therapy for centuries. Currently extracts of all parts of this plant are used — root, leaves and flowers. The extracts are prepared using various extraction agents that may significantly affect the effectiveness and therapeutic spectrum of the extracts. The aim of this study was to use three different solvents for the preparation of the extracts from dandelion (Taraxacum officinale) leaves and flowers, namely triton X-100 (2 %), nonidet P-40 (2 %) and acetone (30 %). After extraction, the extractants were evaporated and the dried extracts were dissolved in water to obtain a series of solutions of the concentrations: 125, 250, 500 and 1000 µg.ml–1. The biological effects of the extracts were investigated by means of the MTT test of cell viability. Rabbit kidney epithelial cells (RK13) exposed to the extracts for 24 and 48 hours were used as a model cell line. We observed that the acetone extract of dandelion leaves and flowers at lower concentrations caused an increase in the viability of the treated cells in comparison with the control cells which were not exposed to the extracts (P < 0.05). At the same time, we observed a significant effect of the solvent used for the preparation of the dry extracts on the viability of the cells. The residues of the extractants caused a decrease in the cell viability almost to zero, which in fact means the death of the cells. The selection of the correct extractant for the preparation of the extracts is essential regarding the use of extracts in the pharmaceutical or cosmetic industries.
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Ceyhan Güvensen, Nur, Mehlika Alper, and Aylin Taşkaya. "Evaluation of Biological Activities of Exopolysaccharide from Rhodococcus pyridinivorans In vitro." European Journal of Research and Development 2, no. 2 (June 7, 2022): 491–504. http://dx.doi.org/10.56038/ejrnd.v2i2.46.

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Microbial exopolysaccharides (EPSs) are biopolymers in the form of carbohydrates produced by many microorganisms and secreted into the external environment. EPS protects the microorganism from drying, phagocytosis, and phage effects, and acts as a barrier in stress environments such as heat, light and sound. EPSs produced for industrial purposes are generally used in areas such as food, cosmetics, petroleum and chemistry. This study was aimed to investigate in addition to basic physical and chemical properties of R. pyridinovorans EPS, in vitro its biological activities such as antioxidant properties and antiproliferative activity. The antioxidant properties of EPS were determined by DPPH and hydroxyl radical elimination. The antiproliferative activity of EPS on HT-29 and MCF-7 cell lines was determined by MTT assay. The results of study indicate that EPS from R. pyridinovorans have important biological activities. Further studies on structural and mechanism elucidation of the bacterial EPSs are still needed being carried out.
29

Pacholak, P., J. Krajewska, P. Wińska, J. Dunikowska, U. Gogowska, J. Mierzejewska, K. Durka, K. Woźniak, A. E. Laudy, and S. Luliński. "Development of structurally extended benzosiloxaboroles – synthesis and in vitro biological evaluation." RSC Advances 11, no. 41 (2021): 25104–21. http://dx.doi.org/10.1039/d1ra04127d.

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30

이인철, Kim Dae Yong, 문지영, 박병권, and 김정미. "In Vitro Evaluation of Biological Activities of Jeju Island Plants Mixture." Journal of Investigative Cosmetology 14, no. 1 (March 2018): 39–45. http://dx.doi.org/10.15810/jic.2018.14.1.005.

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31

Fonseca, Fernando L. A., Taiana C. Caetano, Carolina Z. P. Mecca, Roberta S. S. Yamaguchi, Leandro R. Bissoli, Beatriz da Costa A. Alves, and Izilda A. Bagatin. "In vitro Evaluation of Biological Effects of Metallic Compounds with Quinolines." Current Enzyme Inhibition 14, no. 1 (March 7, 2018): 18–25. http://dx.doi.org/10.2174/1573408013666170213152751.

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32

Erhabor, J. O., A. G. Omokhua, and L. J. McGaw. "In vitro biological activities and safety evaluation of Raphia hookeri (Arecaceae)." South African Journal of Botany 115 (March 2018): 284–85. http://dx.doi.org/10.1016/j.sajb.2018.02.036.

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33

Bettio, F., M. Canevari, C. Marzano, F. Bordin, A. Guiotto, F. Greco, R. Duncan, and F. M. Veronese. "Synthesis and Biological In Vitro Evaluation of Novel PEG−Psoralen Conjugates." Biomacromolecules 7, no. 12 (December 2006): 3534–41. http://dx.doi.org/10.1021/bm060760n.

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34

Hassan, Sadaf ul, Murtaza Hasan, Attia Firdous, and Muhammad Asim Farid. "Preparation, Characterization and In Vitro Biological Evaluation of Nano-Tubular Polyoxometalate." Journal of Nanoscience and Nanotechnology 17, no. 7 (July 1, 2017): 4882–87. http://dx.doi.org/10.1166/jnn.2017.13459.

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35

Bodiga, Vijaya Lakshmi, Sasidhar Reddy Eda, Saishashank Chavali, Nagasaisreelekha Nagavalli Revur, Anita Zhang, Sandhya Thokala, and Sreedhar Bodiga. "In vitro biological evaluation of glyburide as potential inhibitor of collagenases." International Journal of Biological Macromolecules 70 (September 2014): 187–92. http://dx.doi.org/10.1016/j.ijbiomac.2014.06.054.

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36

Napimoga, Marcelo Henrique, Ana Paula Dias Demasi, Christian Rado Jarry, Mauricio Cardoso Ortega, Vera Cavalcanti de Araújo, and Elizabeth Ferreira Martinez. "In vitro evaluation of the biological effect of SOFAT on osteoblasts." International Immunopharmacology 26, no. 2 (June 2015): 378–83. http://dx.doi.org/10.1016/j.intimp.2015.04.033.

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37

Xu, Yuanting, Li Li, Hao Wang, Xixun Yu, Zhipeng Gu, Chengcheng Huang, and Hong Peng. "In vitro cytocompatibility evaluation of alginate dialdehyde for biological tissue fixation." Carbohydrate Polymers 92, no. 1 (January 2013): 448–54. http://dx.doi.org/10.1016/j.carbpol.2012.09.096.

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38

Perdomo, F., R. Ech�vez-Badel, M. Alameda, and E. C. Schr�der. "In vitro evaluation of bacteria for the biological control ofMacrophomina phaseolina." World Journal of Microbiology & Biotechnology 11, no. 2 (March 1995): 183–85. http://dx.doi.org/10.1007/bf00704645.

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39

Tran, UyenPhuong, and Kelvin L. Billingsley. "Biological evaluation of indolactams for in vitro bryostatin 1-like activity." Bioorganic & Medicinal Chemistry Letters 97 (December 2023): 129570. http://dx.doi.org/10.1016/j.bmcl.2023.129570.

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40

Marionnet, Claire, and Françoise Bernerd. "In Vitro Skin Models for the Evaluation of Sunscreen-Based Skin Photoprotection: Molecular Methodologies and Opportunities." Current Medicinal Chemistry 26, no. 10 (June 20, 2019): 1874–90. http://dx.doi.org/10.2174/0929867324666170303124247.

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Identifying and understanding the biological events that occur following ultraviolet (UV) exposure are mandatory to elucidate the biological and clinical consequences of sun exposure, and to provide efficient and adequate photoprotection strategies. The main UVinduced biological features (markers related to sunburn, cancer, photoaging immunosuppression, pigmentation), characterized in human skin in vivo, could be reproduced in adapted models of reconstructed skin in vitro, attesting their high relevance in the field of photobiology. In turn, 3D skin models were useful to discover precise biological pathways involved in UV response and were predictive of in vivo situation. Although they did not follow a strict validation process for the determination of protection factors, they enabled to evidence important concepts in photoprotection. Indeed, the use of reconstructed skin model highlighted the importance of broad spectrum sunscreen use to protect essential cellular functions, and biologically proved that SPF value was not predictive of the level of protection in the UVA wavelength domain. New biological approaches, such as transcriptomic or proteomic studies as well as quantitative and qualitative determination of DNA damage, will indisputably increase the added value of such systems for sunscreen efficiency evaluation.
41

Ribeiro, Carlos J. A., Joana D. Amaral, Cecília M. P. Rodrigues, Rui Moreira, and Maria M. M. Santos. "Spirooxadiazoline oxindoles with promising in vitro antitumor activities." MedChemComm 7, no. 3 (2016): 420–25. http://dx.doi.org/10.1039/c5md00450k.

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42

Woźnica, Iwona, Wioletta Szeszel-Fedorowicz, Grzegorz Rosińskiand, and Danuta Konopińska. "Biological evaluation of analogues of an insect neuropeptide proctolin." Acta Biochimica Polonica 51, no. 1 (March 31, 2004): 115–19. http://dx.doi.org/10.18388/abp.2004_3602.

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Continuing our studies on proctolin (Arg-Tyr-Leu-Pro-Thr) we performed the synthesis and biological evaluation of 52 analogues substituted in position 2, 3, 4, and 5 of the peptide chain. The peptides were bioassayed for cardiotropic activity in vitro on Tenebrio molitor and myotropic activity on foregut of Schistocerca gregaria. Twenty analogues retained 20-80% of proctolin activity.
43

Reddy, Janardan K., M. Sambasiva Rao, and Anjana V. Yeldandi. "Peroxisome Proliferation: A Biological Marker for Toxicological Evaluation." Journal of the American College of Toxicology 11, no. 3 (May 1992): 349–52. http://dx.doi.org/10.3109/10915819209141874.

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Peroxisome proliferators constitute an important group of xenobiotics with therapeutic, societal, and agricultural importance. Because these agents induce liver tumors in rodents, but fail to exert the genotoxic or mutagenic effects directly in short-term in vitro test systems, they are considered a paradigm to investigate the mechanisms of nongenotoxic hepatocarcinogenesis. A concerted cell biological, biochemical, and molecular biological approach is essential to understand the relationship of xenobiotic-induced peroxisome proliferation to the eventual development of liver tumors. It is our intent to provide insight into the mechanisms responsible for tissue specificity and species differences in the biological responses to peroxisome proliferators.
44

Lad, Chaitali, Ishan Panchal, Ashish Patel, Afzal Nagani, Vruti Parikh, Harnisha Patel, and Bhargav Bhimani. "In silico analysis, synthesis and biological evaluation of DHFR inhibitors." Folia Medica 63, no. 5 (October 31, 2021): 745–59. http://dx.doi.org/10.3897/folmed.63.e56786.

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Introduction: Malaria is one of the varieties of fatal diseases caused by a protozoan parasite that is now considered to be the greatest global health challenge. A parasite of Plasmodium species triggers it transmitting the disease to humans by the bites of female Anopheles mosquitoes. Aim: To screen out designed molecules by molecular docking analysis and assess their pharmacokinetic properties using SwissADME. To synthesize the designed compounds. To characterize the synthesized compounds by TLC, melting point, IR spectroscopy, mass spectrometry, 1H NMR, and 13C NMR. To evaluate the synthesized compounds for antimalarial activity. Materials and methods: In silico analysis was performed with SWISSADME, and molecular docking was performed by AutoDock Vina version 4.2. In vitro antimalarial activity study was performed. Results: In-vitro studies of synthesized molecules showed that compounds C2 (IC50 1.23), C6 (IC50 0.48), C10 (IC50 0.79), and C14 (IC50&nbsp;0.19) possess good antimalarial activity. Conclusions: 7-chloroquinoline-piperazine derivatives exhibited potential antimalarial compounds for pf-DHFR inhibitors.
45

Świątek, Piotr, Katarzyna Gębczak, Tomasz Gębarowski, and Rafal Urniaz. "Biological Evaluation and Molecular Docking Studies of Dimethylpyridine Derivatives." Molecules 24, no. 6 (March 20, 2019): 1093. http://dx.doi.org/10.3390/molecules24061093.

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Cyclooxygenase inhibitors as anti-inflammatory agents can be used in chemoprevention. Many in vitro and in vivo studies on human and animal models have explained the mechanisms of the chemopreventive effect of COX inhibitors such as: induction of apoptosis, inhibition of neoplasia, angiogenesis suppression, induction of cell cycle inhibition and inhibition of the expression of peroxisome proliferator-activated receptors. Here, biological evaluation of twelve different Schiff base derivatives of N-(2-hydrazine-2-oxoethyl)-4,6-dimethyl-2-sulfanylpyridine- 3-carboxamide are presented. Their in vitro anti-COX-1/COX-2, antioxidant and anticancer activities were studied. The molecular docking study was performed in order to understand the binding interaction of compounds in the active site of cyclooxygenases. Compounds PS18 and PS33 showed a significant inhibitory activity on COX-1 at lower concentrations compared to meloxicam and piroxicam. The IC50 of COX-1 of these compounds was 57.3 µM for PS18 and 51.8 µM for PS33. Out of the tested compounds, the highest therapeutic index was demonstrated by PS18, PS19, PS33, PS40 and PS41. Lower molar concentrations of these compounds inhibit the growth of cancer cells while not inhibiting the healthy cells. Compounds PS18, PS19 and PS33 simultaneously demonstrated a statistically-significant inhibition of COX-1 or COX-2. This opens up the possibility of applying these compounds in the chemoprevention of cancer.
46

Mendoza, Manuel, Ryan Eom, Celeste Salas, Jeremy Haynes-Smith, and Kelvin L. Billingsley. "The Synthesis and Biological Evaluation of Indolactam Alkaloids." Synthesis 51, no. 23 (August 30, 2019): 4443–51. http://dx.doi.org/10.1055/s-0039-1690198.

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In this work, we execute a general synthetic strategy to access novel indolactam alkaloids, which are agonists of protein kinase C. This protocol allowed for the most efficient reported syntheses of indolactam V (ILV) stereoisomers, while also affording the large-scale production of natural product (–)-ILV. Structure–activity studies were conducted with these compounds to elucidate the elements necessary to promote PKC-mediated cellular response. EC50 measurements in leukemia and lymphoma cell lines, as well as molecular docking analyses with the PKCδ C1B domain, provided the foundation for these studies. A distinct correlation between in vitro activity and the conformation of the macrocyclic lactam ring was discovered, which can guide design efforts for therapeutics that target the PKC regulatory domain.
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Liu, Weihua, Donghai Zhao, Zhiwen He, Yiming Hu, Yuxia Zhu, Lingjian Zhang, Lianhai Jin, Liping Guan, and Sihong Wang. "Synthesis, Characterization and Biological Evaluation of Benzothiazole–Isoquinoline Derivative." Molecules 27, no. 24 (December 19, 2022): 9062. http://dx.doi.org/10.3390/molecules27249062.

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Currently, no suitable clinical drugs are available for patients with neurodegenerative diseases complicated by depression. Based on a fusion technique to create effective multi–target–directed ligands (MTDLs), we synthesized a series of (R)–N–(benzo[d]thiazol–2–yl)–2–(1–phenyl–3,4–dihydroisoquinolin–2(1H)–yl) acetamides with substituted benzothiazoles and (S)–1–phenyl–1,2,3,4–tetrahydroisoquinoline. All compounds were tested for their inhibitory potency against monoamine oxidase (MAO) and cholinesterase (ChE) by in vitro enzyme activity assays, and further tested for their specific inhibitory potency against monoamine oxidase B (MAO–B) and butyrylcholinesterase (BuChE). Among them, six compounds (4b–4d, 4f, 4g and 4i) displayed excellent activity. The classical antidepressant forced swim test (FST) was used to verify the in vitro results, revealing that six compounds reduced the immobility time significantly, especially compound 4g. The cytotoxicity of the compounds was assessed by the MTT method and Acridine Orange (AO) staining, with cell viability found to be above 90% at effective compound concentrations, and not toxic to L929 cells reversibility, kinetics and molecular docking studies were also performed using compound 4g, which showed the highest MAO–B and BuChE inhibitory activities. The results of these studies showed that compound 4g binds to the primary interaction sites of both enzymes and has good blood–brain barrier (BBB) penetration. This study provides new strategies for future research on neurodegenerative diseases complicated by depression.
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Dmytrenko, Oleksandra, Maryna Arkhypova, Darya Starosyla, Svitlana Rybalko, Michael Gevorkyan, and Alexander Galkin. "Biological Evaluation of Medical Devices in the Form of Suppositories for Rectal and Vaginal Use." Innovative Biosystems and Bioengineering 5, no. 4 (December 26, 2021): 228–37. http://dx.doi.org/10.20535/ibb.2021.5.4.249082.

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Background. Programs of preclinical safety studies of the health care products depend on the regulatory status of the investigated products. The classification of such products, in particular suppositories for rectal and vaginal use, is a critical step of developing tactics for their biological evaluation. Adaptation of biological evaluation methods for the medical devices based on the combination of biologically active substances, as well as evaluation of the results of such studies is urgent task of biomedicine. Objective. To substantiate the regulatory status and to carry out a biological evaluation of medical devices in the form of vaginal suppositories based on octenidine dihydrochloride ("Prodexyn") and in the form of rectal suppositories based on Saw palmetto, Levisticum officinale and Calendula officinalis extracts ("Pravenor"). Methods. Biological evaluation was conducted according to the requirements of ISO 10993 standards using in vitro and in vivo biological test systems (cytotoxicity in cell culture and the MTT test, sensitizing and irritating effect in guinea pigs). Results. The cytotoxicity (СС50) of the medical device "Prodexyn" extract in Vero cell culture was 8.35 μg/ml calculated as octenidine dihydrochloride and 416.65 μg/ml calculated as dexpanthenol. "Pravenor" medical device was found to be non-toxic in Vero cell culture. According to the results of MMT assay CC50 for octenidine dihydrochloride was 1.67 μg/ml, and 83.33 μg/ml – for dexpanthenol. CC50 indicators calculated for the different active ingredients of the medical device "Pravenor" were the following: 50 mg/ml for the dwarf palm berries extract (Saw palmetto), 16.67 mg/ml for the lovage roots extract (Levisticum officinale), and 16.67 mg/ml for the calendula flowers extract (Calendula officinalis). No sensitizing or skin irritating effects were observed in guinea pigs. Conclusions. Biological evaluation of medical devices in the form of rectal suppositories "Pravenor" and vaginal suppositories "Prodexyn" performed using in vitro and in vivo biological systems. It was demonstrated an acceptable level of safety of the products. The MTT test was 5 times more sensitive than the Vero cell culture method in determination of cytotoxicity.
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Kumar, Vadlapudi. "Evaluation of In vitro Anti-inflammatory and Thrombolytic Activities of Anisomeles indica Kuntze." Indian Journal of Pure & Applied Biosciences 11, no. 2 (April 30, 2023): 61–71. http://dx.doi.org/10.18782/2582-2845.8981.

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Anisomeles indica Kuntze (A. indica) is among the most common aromatic plants with a heritage of being employed as an ethnomedicinal potential. The therapeutic efficacy of the plant is well known for being antioxidant, antifungal, antioxidant, and anti-inflammatory attributes. In this present study, solvent extraction was carried out by employing the soxhlet extraction method. The phytoconstituents analysis revealed the variation and diversification in the phytochemical content at the qualitative level. The phytochemical screening investigation of A. indica explores the occurrence of flavonoids, glycosides, alkaloids, phenolics, saponins, terpenoids, steroids, carbohydrates, and proteins. A. indica extracts were employed for TLC analysis and further employed to ascertain its biological activity, such as anti-inflammatory and thrombolytic activity. Among all extracts (methanol, hexane, chloroform, and ethyl acetate), the methanol extract of A. indica exhibits potent anti-inflammatory activity and also showed significant thrombolytic activity.
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El-Naggar, Mohamed, Hadia Almahli, Hany Ibrahim, Wagdy Eldehna, and Hatem Abdel-Aziz. "Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation." Molecules 23, no. 6 (June 15, 2018): 1459. http://dx.doi.org/10.3390/molecules23061459.

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