Статті в журналах: "Curcumine – Analogues"

1

Al-Asadi, Ali M., Salah S. Al-Luaibi, Basil A. Saleh, Mohammed A. Baashen, and Gamal A. El-Hiti. "Antioxidant Properties of Curcumin Analogues to Inhibit Thermal Degradation of Low-Density Polyethylene: Experimental and DFT Study." Journal of Chemistry 2022 (June 20, 2022): 1–6. http://dx.doi.org/10.1155/2022/5391296.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Curcumin can be isolated from plants (Curcuma longa) and it belongs to the ginger family. It exhibits many useful properties and acts as an antioxidant. The aim of the current study was to prepare eight curcumin analogues and investigate their antioxidant activities to inhibit the thermal degradation of low-density polyethylene (LDPE). The carbonyl index (CI) was measured to test the effectiveness of the curcumin analogues. Various doses (0.5, 1, 2, 4, and 6% wt/wt) of a mixture containing LDPE and curcumin analogues were prepared, and the CI was measured. The eight curcumin analogues were found to have good to excellent antioxidant activity against the degradation of LDPE. It was clear that the curcumin analogue derived from vanillin and acetone has the highest antioxidant activity. The density functional theory study was conducted for the eight curcumin analogues to test their reactivity and stability. Again, the global reactivity descriptors analysis showed that compound derived from vanillin and acetone was the most reactive compound to inhibit thermal degradation of LDPE.

2

Nocito, Marta Claudia, Arianna De Luca, Francesca Prestia, Paola Avena, Davide La Padula, Lucia Zavaglia, Rosa Sirianni, et al. "Antitumoral Activities of Curcumin and Recent Advances to ImProve Its Oral Bioavailability." Biomedicines 9, no. 10 (October 14, 2021): 1476. http://dx.doi.org/10.3390/biomedicines9101476.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Curcumin, a main bioactive component of the Curcuma longa L. rhizome, is a phenolic compound that exerts a wide range of beneficial effects, acting as an antimicrobial, antioxidant, anti-inflammatory and anticancer agent. This review summarizes recent data on curcumin’s ability to interfere with the multiple cell signaling pathways involved in cell cycle regulation, apoptosis and the migration of several cancer cell types. However, although curcumin displays anticancer potential, its clinical application is limited by its low absorption, rapid metabolism and poor bioavailability. To overcome these limitations, several curcumin-based derivatives/analogues and different drug delivery approaches have been developed. Here, we also report the anticancer mechanisms and pharmacokinetic characteristics of some derivatives/analogues and the delivery systems used. These strategies, although encouraging, require additional in vivo studies to support curcumin clinical applications.

3

Yi, Yau Xin, Anand Gaurav, and Gabriel A. Akowuah. "Docking Studies of Curcumin and Analogues with Various Phosphodiesterase 4 Subtypes." Current Drug Discovery Technologies 17, no. 2 (June 19, 2020): 248–60. http://dx.doi.org/10.2174/1570163815666181017091655.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Introduction: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identify the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity. Materials and Methods: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the targets. A data set comprising 18 analogues of curcumin, was used as ligands for docking of PDE4 subtypes. Curcumin was used as the standard for comparison. Docking was performed using AutoDock Vina 1.1.2 software integrated in LigandScout 4.1. During this process water molecules were removed from proteins, charges were added and receptor structures were minimised by applying suitable force fields. The docking scores were compared, and the selectivity of compounds for PDE4B over PDE4D was calculated as well. Results: All curcumin analogues used in the study showed good binding affinity with all PDE4 subtypes, with evident selectivity towards PDE4B subtype. Analogue A11 provides the highest binding affinity among all ligands. Conclusion: Curcumin and analogues have moderate to strong affinity towards all PDE4 subtypes and have evident selectivity towards PDE4B. The Oxygen atom of the methoxy group plays a key role in PDE4B binding and any alterations could interfere with the binding. Tetrahydropyran side chain and heterocyclic rings are also suggested to be helpful in PDE4B binding.

4

Cheng, Yatian, Jian Zhang, Yan Shao, Yixiang Xu, Haixia Ge, Boyang Yu, and Weiwei Wang. "Enzyme-Catalyzed Glycosylation of Curcumin and Its Analogues by Glycosyltransferases from Bacillus subtilis ATCC 6633." Catalysts 9, no. 9 (August 29, 2019): 734. http://dx.doi.org/10.3390/catal9090734.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Curcumin is a naturally occurring polyphenolic compound that is commonly used in both medicine and food additives, but its low aqueous solubility and poor bioavailability hinder further clinical applications. For assessing the effect of the glycosylation of curcumin on its aqueous solubility, two glycosyltransferase genes (BsGT1 and BsGT2) were cloned from the genome of the strain Bacillus subtilis ATCC 6633 and over-expressed in Escherichia coli. Then, the two glycosyltransferases were purified, and their glycosylation capacity toward curcumin and its two analogues was verified. The results showed that both BsGT1 and BsGT2 could convert curcumin and its two analogues into their glucosidic derivatives. Then, the structures of the derivatives were characterized as curcumin 4′-O-β-D-glucoside and two new curcumin analogue monoglucosides namely, curcumoid-O-α-D-glucoside (2a) and 3-pentadienone-O-α-D-glucoside (3a) by nuclear magnetic resonance (NMR) spectroscopy. Subsequently, the dissolvability of curcumin 4′-O-β-D-glucoside was measured to be 18.78 mg/L, while its aglycone could not be determined. Furthermore, the optimal catalyzing conditions and kinetic parameters of BsGT1 and BsGT2 toward curcumin were determined, which showed that the Kcat value of BsGT1 was about 2.6-fold higher than that of BsGT2, indicating that curcumin is more favored for BsGT2. Our findings effectively apply the enzymatic approach to obtain glucoside derivatives with enhanced solubility.

5

Muhammad, Imran, Nadeem Muhammad, Khan Muhammad Asif, Ahmed Sheraz, Imran Ali, Amir Rai Muhammad, Arshad Muhammad Umair, et al. "Curcumin and its allied analogues: epigenetic and health perspectives – a review." Czech Journal of Food Sciences 35, No. 4 (August 30, 2017): 285–310. http://dx.doi.org/10.17221/584/2015-cjfs.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Curcumin (diferuoyl methane) is a yellow active ingredient present in turmeric. It is a homodimer of feruloylmethane that comprises a hydroxyl and methoxy group (heptadiene with two Michael acceptors), and α-, β-diketone. It contains various metabolites, i.e. hexahydrocurcumin (HHC), tetrahydrocurcumin (THC), octahydrocurcumin (OHC), dihydrocurcumin (DHC), curcumin sulphate, and curcumin glucuronide. Curcumin has been proven the most effective histone deacetylase (HDAC) inhibitor in HeLa nuclear extracts. It has the ability to affect the Akt, growth factors, NF-kB, and metastatic and angiogenic pathways. Curcumin has a strong therapeutic or preventive potential against several major human ailments, i.e. suppression of inflammation, cardiovascular, diabetes, tumorigenesis, chronic fatigue, antidepressant and neurological activities, depression, loss of muscle and bone, and neuropathic pain. In future, higher utilisation of curcumin as an active agent in food based products is required to curtail the human health disorders.

6

Athipornchai, Anan, Nattisa Niyomtham, Wachirachai Pabuprapap, Vachiraporn Ajavakom, Maria Duca, Stéphane Azoulay, and Apichart Suksamrarn. "Potent Tyrosinase Inhibitory Activity of Curcuminoid Analogues and Inhibition Kinetics Studies." Cosmetics 8, no. 2 (May 4, 2021): 35. http://dx.doi.org/10.3390/cosmetics8020035.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Natural tyrosinase inhibitors from herbal plants are promising therapeutic agents for skincare and cosmetic products. Natural curcuminoids exhibit weak antityrosinase properties. The structural modification of curcumin, the major curcuminoid from Curcuma longa, gave 14 analogues. The tyrosinase inhibitory activity of the natural curcuminoids and the modified analogues on both L-tyrosine and DOPA substrates were evaluated. The inhibition kinetics were also undertaken. For analogues with potent activity on the L-tyrosine substrate, the isoxazole analogue 12 and two reduced analogues, hexahydrocurcumin (16) and the α,β-unsaturated analogue 17, showed IC50 values of 8.3, 14.6 and 9.4 µM, and were 20.9-, 11.9- and 18.4-fold more active, respectively, than kojic acid, the reference compound. For the analogues with potent antityrosinase on DOPA substrate, the dimethylated analogue 5 exhibited the strongest antityrosinase activity against the DOPA substrate, with the IC50 value of 8.0 µM, which was 16.6-fold more active than kojic acid. The inhibition kinetics revealed that curcuminoid 5 could bind with both free enzyme and with the enzyme–substrate complex. It acted as a competitive–uncompetitive mixed-II type inhibitor. Curcuminoid 17 could bind with both free enzyme and the enzyme–substrate complex. The results indicated that 17 acted as a competitive–uncompetitive mixed-I type inhibitor, while curcuminoid 12 was a noncompetitive inhibitor which bound with both free enzymes and the enzyme–substrate complex. These potent analogues might serve as new potential tyrosinase inhibitors for the prevention and treatment of skin pigmentation disorders.

7

Morais de Lima, Ednilza, Gabriel Antônio dos Santos, Khaled Hayek, José Jardes Da Gama Bitencourt, and Carolina Passarelli Gonçalves. "Biossíntese Dirigida pelo Precursor de Curcumina pela Curcuma longa L." Ensaios e Ciência C Biológicas Agrárias e da Saúde 25, no. 3 (September 29, 2021): 357–60. http://dx.doi.org/10.17921/1415-6938.2021v25n3p357-360.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

O composto (E,E)-1,7-bis(4-hidroxi-3-metoxifenil)-1,6-heptadieno-3,5-diona, conhecido popularmente como curcumina, é um composto fitoquímico encontrado nos rizomas da Curcuma longa L. Esta substância já demonstrou diversas atividades terapêuticas importantes, como anti-inflamatória, antioxidante, antibacteriana, antiviral e antitumoral, por exemplo. Entretanto, apesar de ser o composto majoritário da via biossintética da Curcuma longa L. é descrito que apenas de 2 a 8% do peso total do rizoma, corresponde à quantidade de curcumina que pode ser extraída. Com o objetivo de estimular a biossíntese da curcumina, este trabalho utilizou a biossíntese dirigida por precursores, que combina síntese química com transformações enzimáticas naturais, e permite que materiais de partida não nativos sejam incorporados às vias biossintéticas. Utilizando essa abordagem foi estabelecido um sistema in vitro de cultura do rizoma suplementado com o precursor, ácido ferúlico e dois análogos. Os dois análogos sintetizados são sais de potássio solúveis em água e foram obtidos com alto grau de pureza e rendimentos consideráveis. A incorporação de diferentes concentrações do precursor e seus análogos ocasionou, em algumas concentrações, um aumento de até 40% da biossíntese da curcumina. O método desenvolvido, validado, utiliza a espectroscopia UV/VIS para quantificar as concentrações de curcumina, através da análise de seus extratos alcoólicos, nos extratos obtidos a partir dos rizomas suplementados. Palavras-chave: Curcumina. Rizoma. Biossíntese Dirigida pelo Precursor. Ácido Ferúlico. Sais Potássicos. Abstract The compound (E,E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, popularly known as curcumin, is a phytochemical found in the rhizomes of Curcuma longa L. This substance has already demonstrated several important therapeutic activities, such as anti-inflammatory, antioxidant, antibacterial, antiviral and antitumor, for example. However, despite being the major compound of the Curcuma longa L. biosynthetic pathway, it is described that only from 2 to 8% of the total weight of the rhizome corresponds to the amount of curcumin that can be extracted. In order to stimulate the curcumin biosynthesis, this work used the precursor-directed biosynthesis, which combines chemical synthesis with natural enzymatic transformations, and allows that non-native starting materials to be incorporated into the biosynthetic pathways. Using this approach, an in vitro rhizome culture system supplemented with the precursor, ferulic acid and two analogs was established. The two synthesized analogs are water-soluble potassium salts and were obtained with a high degree of purity and considerable yields. The incorporation of different precursor concentrations and its analogues caused, in some concentrations, an increase of up to 40% in curcumin biosynthesis. The method was developed, validated, and uses UV/VIS spectroscopy to quantify curcumin concentrations, through the analysis of its alcoholic extracts, in extracts obtained from supplemented rhizomes. Keywords: Curcumin. Rhizome. Precursor-Directed Biosynthesis. Ferulic Acid. Potassium Salts.

8

R, Thirumalaisamy. "Comparative Anti–Alzheimer’s Potential Evaluation of Curcumin and Curcumin Analogues obtained from ZINC Database: An in-Silico Validation." TEXILA INTERNATIONAL JOURNAL OF PUBLIC HEALTH 9, no. 4 (December 28, 2021): 269–83. http://dx.doi.org/10.21522/tijph.2013.09.04.art023.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Curcumin and its eleven analogues obtained from the ZINC database were screened for its anti-Alzheimer’s potential validated through in silico approach. Curcumin, eleven curcumin analogues from the ZINC database, and six standard anti-Alzheimer’s drugs were obtained from SWISS ADME and Pub chem database. All obtained molecules were subjected to drug-likeness, molecular docking, and ADMET analysis. Curcumin and eleven curcumin analogues show no violations against five drug-likeness rules, whereas 2 standard drugs (CID¬_11269353, CID_46883536) out of 5 screened standard drug molecules shows violations in drug likeness property. Curcumin and curcumin analogues possess docking scores in the range of -7.5 to 9.9 Kcal/mol, whereas reference standard drugs docking score lies in the range of -6.4 to -11.0 Kcal/mol against all three Alzheimer’s disease molecular targets. Finally, our present study has proven that curcumin analogues possess some novel anti-Alzheimer’s properties over curcumin and standard reference drug. It needs to be validated and commercialized after in vivo preclinical trials.

9

Ahsan, Mohamed Jawed, Kavita Choudhary, Amena Ali, Abuzer Ali, Faizul Azam, Atiah H. Almalki, Eman Y. Santali, Md Afroz Bakht, Abu Tahir, and Salahuddin. "Synthesis, DFT Analyses, Antiproliferative Activity, and Molecular Docking Studies of Curcumin Analogues." Plants 11, no. 21 (October 25, 2022): 2835. http://dx.doi.org/10.3390/plants11212835.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

With 19.3 million new cases and almost 10 million deaths in 2020, cancer has become a leading cause of death today. Curcumin and its analogues were found to have promising anticancer activity. Inspired by curcumin’s promising anticancer activity, we prepared three semi-synthetic analogues by chemically modifying the diketone function of curcumin to its pyrazole counterpart. The curcumin analogues (3a–c) were synthesized by two different methods, followed by their DFT analyses to study the HOMO/LUMO configuration to access the stability of compounds (∆E = 3.55 to 3.35 eV). The curcumin analogues (3a–c) were tested for antiproliferative activity against a total of five dozen cancer cell lines in a single (10 µM) and five dose (0.001 to 100 µM) assays. 3,5-Bis(4-hydroxy-3-methoxystyryl)-1H-pyrazole-1-yl-(phenoxy)ethanone (3b) and 3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazole-1-yl-(2,4-dichlorophenoxy)ethanone (3c) demonstrated the most promising antiproliferative activity against the cancer cell lines with growth inhibitions of 92.41% and 87.28%, respectively, in a high single dose of 10 µM and exhibited good antiproliferative activity (%GIs > 68%) against 54 out of 56 cancer cell lines and 54 out of 60 cell lines, respectively. The compound 3b and 3c demonstrated the most potent antiproliferative activity in a 5-dose assay with GI50 values ranging between 0.281 and 5.59 µM and 0.39 and 0.196 and 3.07 µM, respectively. The compound 3b demonstrated moderate selectivity against a leukemia panel with a selectivity ratio of 4.59. The HOMO-LUMO energy-gap (∆E) of the compounds in the order of 3a > 3b > 3c, was found to be in harmony with the anticancer activity in the order of 3c ≥ 3b > 3a. Following that, all of the curcumin analogues were molecular docked against EGFR, one of the most appealing targets for antiproliferative activity. In a molecular docking simulation, the ligand 3b exhibited three different types of interactions: H-bond, π-π-stacking and π-cationic. The ligand 3b displayed three H-bonds with the residues Met793 (with methoxy group), Lys875 (with phenolic group) and Asp855 (with methoxy group). The π-π-stacking interaction was observed between the phenyl (of phenoxy) and the residue Phe997, while π-cationic interaction was displayed between the phenyl (of curcumin) and the residue Arg841. Similarly, the ligand 3c displayed five H-bonds with the residue Met793 (with methoxy and phenolic groups), Lys845 (methoxy group), Cys797 (phenoxy oxygen), and Asp855 (phenolic group), as well as a halogen bond with residue Cys797 (chloro group). Furthermore, all the compound 3a–c demonstrated significant binding affinity (−6.003 to −7.957 kcal/mol) against the active site of EGFR. The curcumin analogues described in the current work might offer beneficial therapeutic intervention for the treatment and prevention of cancer. Future anticancer drug discovery programs can be expedited by further modifying these analogues to create new compounds with powerful anticancer potentials.

10

Chen, Jian, Linlin Zhang, Yilai Shu, Liping Chen, Min Zhu, Song Yao, Jiabing Wang та ін. "Curcumin Analogue CA15 Exhibits Anticancer Effects on HEp-2 Cells via Targeting NF-κB". BioMed Research International 2017 (2017): 1–10. http://dx.doi.org/10.1155/2017/4751260.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Laryngeal carcinoma remains one of the most common malignancies, and curcumin has been proven to be effective against head and neck cancers in vitro. However, it has not yet been applied in clinical settings due to its low stability. In the current study, we synthesized 34 monocarbonyl analogues of curcumin with stable structures. CA15, which exhibited a stronger inhibited effect on laryngeal cancer cells HEp-2 but a lower toxicity on hepatic cells HL-7702 in MTT assay, was selected for further analysis. The effects of CA15 on cell viability, proliferation, migration, apoptosis, and NF-κB activation were measured using MTT, Transwell migration, flow cytometry, Western blot, and immunofluorescence assays in HEp-2 cells. An NF-κB inhibitor, BMS-345541, as well as curcumin was also tested. Results showed that CA15 induced decreased toxicity towards HL-7702 cells compared to curcumin and BMS-345541. However, similar to BMS-345541 and curcumin, CA15 not only significantly inhibited proliferation and migration and induced caspase-3-dependent apoptosis but also attenuated TNF-α-induced NF-κB activation in HEp-2 cells. These results demonstrated that curcumin analogue CA15 exhibited anticancer effects on laryngeal cancer cells via targeting of NF-κB.

11

Mora, Enda, Adel Zamri, Hilwan Y. Teruna, Neni Frimayanti, Ihsan Ikhtiarudin, Putri Rizki Rahmadani, and Vella kurnia Wahyuni. "Sintesis Dan Studi Molecular Docking Senyawa Pirazolo-Piridin Turunan Analog Kurkumin Monoketon Sebagai Inhibitor Enzim COX-2." Jurnal Penelitian Dan Pengkajian Ilmiah Eksakta 1, no. 2 (July 28, 2022): 126–32. http://dx.doi.org/10.47233/jppie.v2i1.799.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

The new pyrazolo-pyridine compounds derived from monoketone curcumin analogues (P4Cl and P2CL) were synthesized in two stages. The first stage was the synthesis of curcumin monoketone (Cs) analogue through the Claisen-Schmidt reaction in the heating method using reflux. The second step was the synthesis of P2CL and P4Cl through nucleophilic addition and intramolecular cyclization in the heating method using a Monowave 50 apparatus. The structures of the compounds P2CL and P4Cl were confirmed by spectroscopic analysis including UV-Vis, FT-IR, 1H-NMR and HRMS. Based on molecular docking studies, the compounds P2Cl and P4Cl have weak potential as COX-2 enzyme inhibitors with a binding free energy value of -4.02 kcal/mol and an RMSD of 1.19.

12

Kim, Mi Kyoung, Jun Cheol Park, and Youhoon Chong. "Aromatic Hydroxyl Group Plays a Critical Role in Antibacterial Activity of the Curcumin Analogues." Natural Product Communications 7, no. 1 (January 2012): 1934578X1200700. http://dx.doi.org/10.1177/1934578x1200700120.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

The aim of this study was to investigate the role of the aromatic substituents of the curcumin scaffold on the antibacterial activity of the resulting curcumin analogues. Six curcumin analogues with different aromatic substituents were prepared and their antibacterial activities were evaluated against two Gram-positive and four Gram-negative bacteria. The structure-activity relationship study demonstrated that antibacterial activity of the curcumin analogues was critically dependent upon the aromatic hydroxyl group. Thus, hydroxycurcumin with an additional aromatic hydroxyl group on the curcumin scaffold showed antibacterial activity against all six pathogens tested and it remained effective even against ampicillin-resistant Enterobacter cloacae. Along with the previously reported antioxidative effect, the broad-spectrum antibacterial activity of the hydroxycurcumin warrants further investigation of its biological activity as well as extensive structure-activity relationship study of the curcumin analogues with various aromatic substituents.

13

Hussain, Haya, Shujaat Ahmad, Syed Wadood Ali Shah, Abid Ullah, Mazen Almehmadi, Osama Abdulaziz, Mamdouh Allahyani, Ahad Amer Alsaiari, Mustafa Halawi, and Edrous Alamer. "Investigation of Antistress and Antidepressant Activities of Synthetic Curcumin Analogues: Behavioral and Biomarker Approach." Biomedicines 10, no. 10 (September 24, 2022): 2385. http://dx.doi.org/10.3390/biomedicines10102385.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Depression is a serious psychiatric disorder that affects millions of individuals all over the world, thus demanding special attention from researchers in order to investigate its effective remedies. Curcumin, along with its synthetic derivatives, is recognized for its incredible pharmacological activities. In this study, methyl, methoxy and chloro-substituent synthetic curcumin analogues C1–C3 were respectively tested for free radical-scavenging activity. Behavioral studies were performed using chemical-induced and swimming endurance tests as stress models, and forced swim tests (FSTs) and tail suspension tests (TSTs) as depression mice models. Biochemical examinations were performed after a scopolamine-induced stress model by decapitating the mice, and brain tissues were isolated for biochemical assessment of catalase (CAT), superoxide dismutase (SOD), glutathione (GSH), and malondialdehyde (MDA). The curcumin analogue C2 exhibited higher DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2′-azinobis-3-ethylbenzothiazo-line-6-sulphonate) free radical-scavenging potential, having IC50 values of 45.18 µg/mL and 62.31 µg/mL, respectively, in comparison with reference curcumin and tocopherol. In the chemical-induced test, C2 (80.17%), C3 (72.79%) and C1 (51.85%) revealed higher antistress responses by significantly reducing the number of writhes, whereas the immobility time was significantly reduced by C2 and C3 in the swimming endurance test, indicating excellent antistress potential. Similarly, C2 and C3 significantly reduced the immobility times in FST and TST, demonstrating their antidepressant properties. The biomarkers study revealed that these compounds significantly enhanced hippocampus CAT, SOD and GSH, and reduced MDA levels in the scopolamine-induced stress mice model. These findings suggest the potential of curcumin analogues (C2 and C3) as antistress and antidepressant agents.

14

Mardianis, Yunia, Chairil Anwar, and Winarto Haryadi. "Synthesis of Curcumin Analogues Monoketone from Cinnamaldehyde and their Inhibition Assay against Alpha-Glucosidase Enzyme." Materials Science Forum 901 (July 2017): 110–17. http://dx.doi.org/10.4028/www.scientific.net/msf.901.110.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

The synthesis of curcumin analogues monoketone as target compounds from cinnamaldehyde and inhibition assay against alpha-glucosidase enzyme had been performed. The stepwise of synthesis was performed by aldol condensation Claisen-Schmidt reaction andused ketones variation to give curcumin analogues monoketone. The antidiabetic activity of curcumin analogues was carried out by inhibition test against alpha-glucosidase enzyme isolated from rotten rice (Oryza sativa). The first step of synthesis was started by reacting cinnamaldehyde and monoketones such as acetone (curcumin analog A [(1E,3E,6E,8E)-1,9-diphenyl-1,3,6,8-nanotetraen-5-one]), cyclopentanone (curcumin analog B [(2E,5E)-2,5-bis ((E)-3-phenylallylidene) cyclopentanone], and cyclohexanone (curcumin analog C [(2E,6E)-2,6-bis [(E)-3-phenylallylidene] cyclohexanone]) in ethanol as solvent. The synthesis was carried out in base condition (KOH) by stirring at 52 °C for 50 minutes. The structures of all products were identified by using FTIR, direct inlet-MS, 1H-and 13C-NMR. Futhermore, the activity of curcumin analogues was tested against with alpha-glucosidase enzyme inhibition. The results show that the curcumin analogues (A-C) were yielded in 85.57; 72.15; and 82.97%, respectively as yellow solid. The melting point of curcuminanalogues (A-C) were at 116.60-122.40; 196.20-200.10; and 142.30-148.10 °C, respectively. The inhibition of alpha-glucosidase enzyme indicated that the curcumin analog B was potential to inhibit alpha-glucosidase enzyme with the highest activity by giving inhibition percentage of about 70.71% at 2.5 mM.

15

Krishnamurthy, Geeta, Lairikyengbam Deepti Roy, Jyotsna Kumar, Pooja Gour, Shivanjali Esther Arland, Manikanda Prabu, Srinivasa GR, and Shreenivas MT. "STUDY OF In-silico ADMET, MOLECULAR DOCKING, AND STABILITY POTENTIAL OF SYNTHESIZED NOVEL TETRAZOLE BEARING CURCUMIN DERIVATIVES AND EVALUATION OF THEIR ANTICANCER POTENTIAL ON PANC-1 CELL LINES." RASAYAN Journal of Chemistry 16, no. 01 (2023): 335–54. http://dx.doi.org/10.31788/rjc.2023.1618114.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Amplified expression of mutations in proteins is an important hallmark of malignant cancer. In all RAS-mutant human cancers, pancreatic ductal adenocarcinoma (PDAC) is considered the most RAS-fanatic cancer, with a frequency of 100% KRAS (Kirsten rat sarcoma virus) mutation. In the present work, curcumin, a dietary phytochemical, was used to design a series of novel curcumin analogues aiming to regulate KRAS protein. The molecular docking study revealed the ligand efficacy and binding affinity of designed curcumin analogues against target proteins. Drug-like behaviour and ADMET (absorption, distribution, metabolism, excretion, and toxicity) prediction of identified molecules were done, and most of the pharmacokinetic parameters were found to be quite satisfactory and within an acceptable range. Three of the most potent drug candidates have been synthesized and characterized by FTIR, 1HNMR, and LC-MS spectral analysis. Results of the in vitro anti-proliferative activities of curcumin analogues showed persuasive anticancer activity against the PANC-1 cell lines. The present study will be helpful in exploring the new series of cogent curcumin analogues as anticancer agents.

16

Tedesco, Serena, Morena Zusso, Laura Facci, Annalisa Trenti, Carlotta Boscaro, Federica Belluti, Gian Paolo Fadini, et al. "Bisdemethoxycurcumin and Its Cyclized Pyrazole Analogue Differentially Disrupt Lipopolysaccharide Signalling in Human Monocyte-Derived Macrophages." Mediators of Inflammation 2018 (2018): 1–13. http://dx.doi.org/10.1155/2018/2868702.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Several studies suggest that curcumin and related compounds possess antioxidant and anti-inflammatory properties including modulation of lipopolysaccharide- (LPS-) mediated signalling in macrophage cell models. We here investigated the effects of curcumin and the two structurally unrelated analogues GG6 and GG9 in primary human blood-derived macrophages as well as the signalling pathways involved. Macrophages differentiated from peripheral blood monocytes for 7 days were activated with LPS or selective Toll-like receptor agonists for 24 h. The effects of test compounds on cytokine production and immunophenotypes evaluated as CD80+/CCR2+ and CD206+/CD163+ subsets were examined by ELISA and flow cytometry. Signalling pathways were probed by Western blot. Curcumin (2.5–10 μM) failed to suppress LPS-induced inflammatory responses. While GG6 reduced LPS-induced IκB-α degradation and showed a trend towards reduced interleukin-1β release, GG9 prevented the increase in proinflammatory CD80+ macrophage subset, downregulation of the anti-inflammatory CD206+/CD163+ subset, increase in p38 phosphorylation, and increase in cell-bound and secreted interleukin-1β stimulated by LPS, at least in part through signalling pathways not involving Toll-like receptor 4 and nuclear factor-κB. Thus, the curcumin analogue GG9 attenuated the LPS-induced inflammatory response in human blood-derived macrophages and may therefore represent an attractive chemical template for macrophage pharmacological targeting.

17

Santoso, Broto. "3D-MOLECULAR SCREENING OF DIKETOPIPERAZINE DERIVATES ON Staphylococcus aureus DEHYDROSQUALENE SYNTHASE USING VINA." Pharmacon: Jurnal Farmasi Indonesia 13, no. 1 (January 27, 2015): 24–29. http://dx.doi.org/10.23917/pharmacon.v13i1.23.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Dehydrosqualene synthase enzyme has been used as protein target model for exploring docking simulation of pyrazoline analogues. One of diketopiperazine derivates that have similar structure to pyrazoline has antibacterial activity against Staphylococcus aureus (S. aureus). Vina is AutoDock- improved program that capable for molecular screening based on free-energy and binding conformation prediction between ligand and protein target. The aim of these studies is to screen diketopiperazine derivates on dehydrosqualene synthase of S. aureus using Vina. Diketopiperazine derivates, curcumin analogues, curcumin, pentagammavunon derivates (PGV-0 and PGV-1) were calculated for their geometry optimization energy using Gaussian-Density Functional Theory method. 3D-optimized ligands along with reference ligands were screened for their binding energy with dehydrosqualene synthase (2ZCO) by docking using Vina. The lowest values of binding energy were analyzed with statistic method. The results showed that top thirteen ligands of docking binding energy with receptor are diketopiperazine derivates (31%), curcumin analogues (31%), and reference ligands (38%). The new compounds of diketopiperazine derivates and curcumin analogues have better potency of binding energy than curcurmin as lead compound. Keywords: diketopiperazine, Vina, docking, Staphylococcus aureus, curcumin.

18

Bonaccorsi, Paola Maria, Manuela Labbozzetta, Anna Barattucci, Tania Maria Grazia Salerno, Paola Poma, and Monica Notarbartolo. "Synthesis of Curcumin Derivatives and Analysis of Their Antitumor Effects in Triple Negative Breast Cancer (TNBC) Cell Lines." Pharmaceuticals 12, no. 4 (October 26, 2019): 161. http://dx.doi.org/10.3390/ph12040161.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

We analyzed antitumor effects of a series of curcumin analogues. Some of them were obtained by reaction of substitution involving the two phenolic OH groups of curcumin while the analogues with a substituent at C-4 was prepared following an original procedure that regards the condensation of benzenesulfenic acid onto the nucleophilic central carbon of the curcumin skeleton. We analyzed cytotoxic effects of such derivatives on two TNBC (triple negative breast cancer) cell lines, SUM 149 and MDA-MB-231, but only three of them showed an IC50 in a lower micromolar range with respect to curcumin. We also focused on these three derivatives that in both cell lines exhibited a higher or at least equivalent pro-apoptotic effect than curcumin. The analysis of molecular mechanisms of action of the curcumin derivatives under study has highlighted that they decreased NF-κB transcriptional factor activity, and consequently the expression of some NF-κB targets. Our data confirmed once again that curcumin may represent a very good lead compound to design analogues with higher antitumor capacities and able to overcome drug resistance with respect to conventional ones, even in tumors difficult to treat as TNBC.

19

Sowa-Kasprzak, Katarzyna, Dorota Olender, Jacek Kujawski, Lucjusz Zaprutko, and Anna Pawełczyk. "Synthesis of curcumin derivatives containing non-steroidal anti-inflammatory drugs." Acta Poloniae Pharmaceutica - Drug Research 80, no. 2 (June 29, 2023): 289–304. http://dx.doi.org/10.32383/appdr/161972.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Synthesis and biological evaluation of hybrid molecules combining naturally occurring antioxidant active structures with anti-inflammatory agents has been a strong trend in medicinal chemistry. This study focuses on modulating the structure of curcumin derivatives or their analogues with the use of non-steroidal anti-inflammatory drugs (NSAIDs). The combinations of curcumin, its keto-blocked derivatives and monocarbonyl analogues with selected non-steroidal anti-inflammatory drugs (ibuprofen, naproxen) were obtained and characterized. The pyrazole, isoxazole, benzylidene derivatives as well as curcumin monocarbonyl analogues were used as substrates in the reactions with selected NSAIDs. As a result of the esterification of curcumin-type diphenol, the corresponding mono- and diester-type derivatives were also obtained and characterized. Moreover, the estimated values of binding affinities and the binding sites of docked derivatives were deduced from modeling studies were very favorable. Results obtained show the binding potential of curcumin and its analogs to the host-targeted proteins nucleocapsid phosphoprotein (PDB ID: 6VYO) structure. Additionally, with the use of selected methods of computational chemistry (Molinspiration Cheminformatics and Osiris Property Explorer) the molecular parameters of the relevant molecules were calculated.

20

Krówczyński, Adam, Anna Zep, Katarzyna Kuć, Tomasz Deptuła, Mirosław Salamończyk, Ewa Górecka, and Jadwiga Szydłowska. "Liquid crystalline analogues of curcumin." Liquid Crystals 41, no. 5 (January 10, 2014): 685–93. http://dx.doi.org/10.1080/02678292.2013.875227.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

21

Mock, Charlotta D., Brian C. Jordan, and Chelliah Selvam. "Recent advances of curcumin and its analogues in breast cancer prevention and treatment." RSC Advances 5, no. 92 (2015): 75575–88. http://dx.doi.org/10.1039/c5ra14925h.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

22

Mustika, Chessy Rima, Endang Astuti, and Muhammad Idham Darussalam Marjan. "Molecular Docking, Synthesis and <i>In Vitro</i> Antiplasmodium Assay of Monoketone Curcumin Analogous from 2-Chlorobenzaldehyde." Indonesian Journal of Chemistry 24, no. 3 (June 1, 2024): 638. http://dx.doi.org/10.22146/ijc.81122.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

This research aimed to develop new curcumin analogous as antiplasmodium candidates. Six curcumin analogous (1-6) were proposed and docked against three Plasmodium falciparum receptors, namely PfENR, PfLDH, and PfATP6. The docking studies were carried out to predict the interaction among the compounds and receptors as well as their binding affinity. Three curcumin analogous (3, 4, and 6), which displayed specific interactions with the target receptors and possessed the lowest binding affinity were further proceeded to synthesis and in vitro antiplasmodium assay. Synthesis of the analogous 3, 4, and 6 was carried out from 2-chlorobenzadehyde via aldol condensation reaction and the products were obtained in good yields. Their in vitro antiplasmodium activities were then evaluated against P. falciparum FCR3 and 3D7 strains. The results showed that analogous 3, 4, and 6 were active against both strains with low levels of resistance. The in silico evaluation of the physicochemical and pharmacokinetic parameters showed that curcumin analogous displayed a better ADMET profile than curcumin, demonstrating the great potential of the developed curcumin analogous as antiplasmodium candidates.

23

Leslie, Kimberly K., Alex Goss, Jamie Padilla, and Lane E. Smith. "Abstract B016: Novel curcumin analogues as therapies for endometrial cancer with TP53 mutations." Clinical Cancer Research 30, no. 5_Supplement (March 1, 2024): B016. http://dx.doi.org/10.1158/1557-3265.endo24-b016.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Abstract The protein p53 is designated as the guardian of the genome because it is the principal tumor suppressor and functions to surveil the genome, enforce cell cycle checkpoints, and trigger apoptosis when genomic instability is beyond repair. Mutations in TP53 are found in >50% of human tumors and in 25% of the deadliest endometrial malignancies. Yet, few studies have targeted the mutant protein to restore its wild type (WT) tumor suppressor functions. Curcumin, a turmeric derivative, has been shown to help return WT function to mutant p53. However, curcumin is not bioavailable to most of the body because of its water insolubility, hydrophobic nature and rapid metabolization. Our laboratory is testing novel, more bioavailable analogs of curcumin including HO-3867 and AKT-100. In these studies, we tested these agents in preclinical models of serous endometrial cancer to assess their effects on cell growth and p53-dependent signaling. We used CyQUANT cell proliferation assay to identify IC50 values for HO-3867 and AKT-100 in ECC-1 and KLE endometrial cancer cell lines. We performed RNA sequencing to elucidate mechanisms of action and verified p53 expression changes via Western blotting. IC50 values ranged from 100 nanomolar (AKT-100) to low micromolar (HO-3867). RNA sequencing data revealed the re-enforcement of cell cycle checkpoints including the upregulation of CDKN1A (p21) and GADD45 (Gadd45). Proliferative signaling downstream of ATM, an important protein kinase stimulating cell growth, was downregulated by both agents. Western blotting confirmed the classic negative feedback loop of p53, where total p53 levels decreased after drug treatment. Taken together, our findings show that AKT-100 and HO-3867 are able to restore WT tumor suppressor function in otherwise oncogenic mutant p53 by reducing cell replication and promoting apoptosis. Thus, curcumin analogues such as AKT-100 and HO-3867 show promise in the treatment of a subset of endometrial tumors expressing mutant p53 by returning WT p53 functionality, and future studies will move to in vivo analyses of curcumin analogue function. Citation Format: Kimberly K. Leslie, Alex Goss, Jamie Padilla, Lane E. Smith. Novel curcumin analogues as therapies for endometrial cancer with TP53 mutations [abstract]. In: Proceedings of the AACR Special Conference on Endometrial Cancer: Transforming Care through Science; 2023 Nov 16-18; Boston, Massachusetts. Philadelphia (PA): AACR; Clin Cancer Res 2024;30(5_Suppl):Abstract nr B016.

24

Kurien, Biji T., Debashish Danda, and Robert H. Scofield. "Therapeutic potential of curcumin and curcumin analogues in rheumatology." International Journal of Rheumatic Diseases 18, no. 6 (July 2015): 591–93. http://dx.doi.org/10.1111/1756-185x.12753.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

25

Nalli, Marianna, Giorgio Ortar, Aniello Schiano Moriello, Vincenzo Di Marzo, and Luciano De Petrocellis. "Effects of curcumin and curcumin analogues on TRP channels." Fitoterapia 122 (October 2017): 126–31. http://dx.doi.org/10.1016/j.fitote.2017.09.007.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

26

Pantiora, Panagiota, Veronika Furlan, Dimitris Matiadis, Barbara Mavroidi, Fereniki Perperopoulou, Anastassios C. Papageorgiou, Marina Sagnou, Urban Bren, Maria Pelecanou, and Nikolaos E. Labrou. "Monocarbonyl Curcumin Analogues as Potent Inhibitors against Human Glutathione Transferase P1-1." Antioxidants 12, no. 1 (December 28, 2022): 63. http://dx.doi.org/10.3390/antiox12010063.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

The isoenzyme of human glutathione transferase P1-1 (hGSTP1-1) is involved in multi-drug resistance (MDR) mechanisms in numerous cancer cell lines. In the present study, the inhibition potency of two curcuminoids and eleven monocarbonyl curcumin analogues against hGSTP1-1 was investigated. Demethoxycurcumin (Curcumin II) and three of the monocarbonyl curcumin analogues exhibited the highest inhibitory activity towards hGSTP1-1 with IC50 values ranging between 5.45 ± 1.08 and 37.72 ± 1.02 μM. Kinetic inhibition studies of the most potent inhibitors demonstrated that they function as non-competitive/mixed-type inhibitors. These compounds were also evaluated for their toxicity against the prostate cancer cells DU-145. Interestingly, the strongest hGSTP1-1 inhibitor, (DM96), exhibited the highest cytotoxicity with an IC50 of 8.60 ± 1.07 μΜ, while the IC50 values of the rest of the compounds ranged between 44.59–48.52 μΜ. Structural analysis employing molecular docking, molecular dynamics (MD) simulations, and binding-free-energy calculations was performed to study the four most potent curcumin analogues as hGSTP1-1 inhibitors. According to the obtained computational results, DM96 exhibited the lowest binding free energy, which is in agreement with the experimental data. All studied curcumin analogues were found to form hydrophobic interactions with the residue Gln52, as well as hydrogen bonds with the nearby residues Gln65 and Asn67. Additional hydrophobic interactions with the residues Phe9 and Val36 as well as π–π stacking interaction with Phe9 contributed to the superior inhibitory activity of DM96. The van der Waals component through shape complementarity was found to play the most important role in DM96-inhibitory activity. Overall, our results revealed that the monocarbonyl curcumin derivative DM96 acts as a strong hGSTP1-1 inhibitor, exerts high prostate cancer cell cytotoxicity, and may, therefore, be exploited for the suppression and chemosensitization of cancer cells. This study provides new insights into the development of safe and effective GST-targeted cancer chemosensitizers.

27

Almayyahi, Muhanad T., Basil A. Saleh, and Baqer A. Almayyahi. "Synthesis and Characterization of Some New Copolyester from Curcumin Mono-Carbonyl Analogues." Biomedicine and Chemical Sciences 3, no. 1 (July 1, 2022): 147–59. http://dx.doi.org/10.48112/bcs.v1i3.179.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Nine copolyesters were prepared from a dicarboxylic acid, curcumin analogues (monocarbonyl) and phenophthalene dye in the mole ratio of 2:1:1 by direct polycondensation using triethylamine (Et3N) as the condensation agent. The dicarboxylic used is 2,6-Pyridine dicarbonyl dichloride acid. The curcumin analogues were prepared by acid catalyzed Aldol condensation reaction. These copolyesters were characterized by FT-IR. The fluorescence of the synthesized copolyesters was also investigated. Furthermore, Thermo gravimetric analysis (TGA) was used to investigate the thermal stability of these copolymers.

28

Aman, La Ode, Rahmana Emran Kartasasmita, and Daryono Hadi Tjahjono. "Virtual screening of curcumin analogues as DYRK2 inhibitor: Pharmacophore analysis, molecular docking and dynamics, and ADME prediction." F1000Research 10 (May 17, 2021): 394. http://dx.doi.org/10.12688/f1000research.28040.1.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Background: Curcumin reduces the proliferation of cancer cells through inhibition of the DYRK2 enzyme, which is a positive regulator of the 26S proteasome. Methods: In the present work, curcumin analogues have been screened from the MolPort database using a pharmacophore model that comprised a ligand-based approach. The result of the screening was then evaluated by molecular docking and molecular dynamics based on binding the free energy of the interaction between each compound with the binding pocket of DYRK2. The hit compounds were then confirmed by absorption, distribution, metabolism, and excretion (ADME) prediction. Results: Screening of 7.4 million molecules from the MolPort database afforded six selected hit compounds. By considering the ADME prediction, three prospective curcumin analogues have been selected. These are: 2‐[2‐(1‐methylpyrazol‐4‐yl)ethyl]‐1H,5H,6H,7H,8H‐imidazo[4,5‐c]azepin‐4‐one (Molport-035-369-361), methyl 4‐(3‐hydroxy‐1,2‐oxazol‐5‐yl)piperidine‐1‐carboxylate (Molport-000-004-273) and (1S)‐1‐[5‐(furan‐3‐carbonyl)‐4H,6H,7H‐pyrazolo[1,5‐a]pyrazin‐2‐yl]ethanol (MolPort-035-585-822). Conclusion: Pharmacophore modelling, combined with molecular docking and molecular dynamics simulation, as well as ADME prediction were successfully applied to screen curcumin analogues from the MolPort database as DYRK2 inhibitors. All selected compounds that have better predicted pharmacokinetic properties than that of curcumin are considered for further study.

29

Anthwal, Amit, Kundan Singh, M. S. M. Rawat, Amit K. Tyagi, Bharat B. Aggarwal, and Diwan S. Rawat. "C5-curcuminoid-dithiocarbamate based molecular hybrids: synthesis and anti-inflammatory and anti-cancer activity evaluation." RSC Adv. 4, no. 54 (2014): 28756–64. http://dx.doi.org/10.1039/c4ra03655g.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

The C5-curcumin-dithiocarbamate analogues were synthesized in search of new molecules with anti-proliferation potential against cancer cells. These new compounds demonstrated higher anti-proliferation and anti-inflammatory activity against cancer cell lines in comparison to curcumin.

30

Muhanad T. Almayyahi, Basil A. Saleh, and Baqer A. Almayyahi. "Synthesis, Characterization and Thermal Study of Some new Copolyesters from mono-carbonyl analogues of Curcumin and Thymol blue dye." Journal of Kufa for Chemical Sciences 2, no. 9 (August 28, 2023): 569–81. http://dx.doi.org/10.36329/jkcm/2022/v2.i9.13322.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

A series of copolyesters were prepared from a dicarboxylic acid, curcumin analogues (monocarbonyl) and thymol blue dye in the mole ratio of 2:1:1 by direct polycondensation using triethylamine (Et3N) as the condensation agent. The dicarboxylic used is 2,6-Pyridine dicarbonyl dichloride acid. The curcumin analogues were prepared by acid catalyzed Aldol condensation reaction. These copolyesters were characterized by FT-IR. The fluorescence of the synthesized copolyesters was also investigated. Furthermore, Thermo gravimetric analysis (TGA) was used to investigate the thermal stability of these copolymers

31

Mainassy, Meillisa Carlen, Wasmen Manalu, Andri Yanto, Agus Oman Sudrajat, Imanuel Berly Delvis Kapelle, and Bambang Gunadi. "Suplementasi Analog Kurkumin Dapat Meningkatkan Kinerja Hati Untuk Mendukung Reproduksi Ikan Nila Merah (Oreochromis niloticus)." Jurnal Veteriner 23, no. 2 (June 30, 2022): 217–27. http://dx.doi.org/10.19087/jveteriner.2022.23.2.217.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Kualitas benih ikan sangat ditentukan oleh deposisi nutrien dalam oosit yang sedang berkembang dan diproduksi oleh hepatosit di bawah kendali hormon estrogen. Penelitian ini bertujuan untuk mengevaluasi peranan suplementasi analog kurkumin dalam meningkatkan kinerja hati untuk mendukung reproduksi ikan nila merah (Oreochromis niloticus). Rancangan yang digunakan adalah rancangan acak lengkap dengan tujuh perlakuan dan tiga kali ulangan, yaitu P0 (kontrol/0 mg kurkumin), P1 (analog kurkumin dosis 2,4 mg/100 g pakan), P2 (analog kurkumin dosis 4,8 mg/100 g pakan), P3 (tepung kunyit dosis 25 mg/100 g pakan), P4 (tepung kunyit dosis 50 mg/100 g pakan), P5 (kurkumin murni komersial dosis 2,4 mg/100 g pakan), dan P6 (kurkumin murni komersial dosis 4,8 mg/100 g pakan). Tiap ulangan terdiri dari 5 ekor ikan. Parameter yang diamati adalah kadar vitelogenin plasma, DNA, dan RNA jaringan hati, kadar serum glutamic pyruvic transaminase (SGPT), serum glutamic oxaloacetic transaminase(SGOT), malondialdehyde (MDA) dan superoxide dismutase (SOD) pada jaringan hati. Hasil penelitian menunjukkan bahwa suplementasi analog kurkumin dalam pakan dapat meningkatkan pertumbuhan jaringan hati ikan nila, terbukti dengan peningkatan konsentrasi DNA dan RNA jaringan hati pada kelompok ikan yang diberikan perlakuan. Peningkatan kinerja hati melalui penurunan konsentrasi MDA, SGPT, dan SGOT serta meningkatnya konsentrasi SOD. Suplementasi analog kurkumin dapat meningkatkan kapasitas hati untuk menyintesis vitelogenin yang akan disimpan dalam folikel yang sedang berkembang selama kematangan gonad.

32

Puentes, Neyder Contreras, Daimer Pérez Orozco та Fernando Camacho -Díaz. "Curcumin Analogues as Promissory Compounds for Inhibition of β-Secretase, γ-Secretase and GSK-3β Implicated at Alzheimer Disease: In Silico Study". Biomedical and Pharmacology Journal 15, № 1 (31 березня 2022): 445–52. http://dx.doi.org/10.13005/bpj/2384.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Aims: Alzheimer's disease is a disorder associated to dementia that widely affects to population. In the molecular study, key enzymes have been associated with the regulation of the amyloid pathway, which have a focus in the discovery of possible inhibitors. Likewise, the absence of specific treatments, has promoted the development of promising molecules from natural sources. Material and Methods: In this study was carried out an in-silico exploration of curcumin analogues against β-secretase, γ-secretase and GSK-3β. A virtual screening of 373 curcumin analogues against enzymes implicated in the pathology was implemented, using molecular docking simulations through Autodock-Vina based on PyRx 0.8. Followed by in-silico prediction of ADMET properties to molecules with higher affinity using SwissADME and GUSAR prediction. Results: It was obtained that the molecules of highest affinity were 92296662, 102584924, 92341226 for β-secretase, γ-secretase and GSK-3β, respectively. These were contrasted with selective inhibitors for enzymatic systems. Additionally, the predictions of the ADMET properties of the analogues showed a variability in terms of metabolism, non-permeation on blood–brain barrier and toxicity values according to reported in the literature. Thus, in-silico prediction indicated curcumin analogues as possible regulatory agents of the enzymatic activity associated to Alzheimer's disease.

33

Khisamova, A., та O. Gizinger. "The antitoxic and protective effects of Curcuma longa and it`s active agent, Curcumin: оverview". Terapevt (General Physician), № 6 (1 червня 2020): 66–72. http://dx.doi.org/10.33920/med-12-2006-09.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

In the modern world, where a person is exposed to daily stress, increased physical exertion, the toxic effect of various substances, including drugs. The task of modern science is to find antioxidants for the body. These can be additives obtained both synthetically and the active substances that we get daily from food. Such a striking example is turmeric, obtained from the plant Curcuma longa. Recently, it has been known that curcumin has an antioxidant, anti-inflammatory, anti-cancer effect and, thanks to these effects, plays an important role in the prevention and treatment of various diseases, in particular, from cancer to autoimmune, neurological, cardiovascular and diabetic diseases. In addition, much attention is paid to increasing the biological activity and physiological effects of curcumin on the body through the synthesis of curcumin analogues. This review discusses the chemical and physical characteristics, analogues, metabolites, the mechanisms of its physiological activity and the effect of curcumin on the body.

34

Ratan, Chameli, Arya Mangalath Arian, Rajalakshmi Rajendran, Rangasamy Jayakumar, Mar Masson, and Sabitha Mangalathillam. "Nano-based formulations of curcumin: elucidating the potential benefits and future prospects in skin cancer." Biomedical Materials 18, no. 5 (August 25, 2023): 052008. http://dx.doi.org/10.1088/1748-605x/acf0af.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Abstract Skin cancer refers to any malignant lesions that occur in the skin and are observed predominantly in populations of European descent. Conventional treatment modalities such as excision biopsy, chemotherapy, radiotherapy, immunotherapy, electrodesiccation, and photodynamic therapy (PDT) induce several unintended side effects which affect a patient’s quality of life and physical well-being. Therefore, spice-derived nutraceuticals like curcumin, which are well tolerated, less expensive, and relatively safe, have been considered a promising agent for skin cancer treatment. Curcumin, a chemical constituent extracted from the Indian spice, turmeric, and its analogues has been used in various mammalian cancers including skin cancer. Curcumin has anti-neoplastic activity by triggering the process of apoptosis and preventing the multiplication and infiltration of the cancer cells by inhibiting some signaling pathways and thus subsequently preventing the process of carcinogenesis. Curcumin is also a photosensitizer and has been used in PDT. The major limitations associated with curcumin are poor bioavailability, instability, limited permeation into the skin, and lack of solubility in water. This will constrain the use of curcumin in clinical settings. Hence, developing a proper formulation that can ideally release curcumin to its targeted site is important. So, several nanoformulations based on curcumin have been established such as nanogels, nanoemulsions, nanofibers, nanopatterned films, nanoliposomes and nanoniosomes, nanodisks, and cyclodextrins. The present review mainly focuses on curcumin and its analogues as therapeutic agents for treating different types of skin cancers. The significance of using various nanoformulations as well non-nanoformulations loaded with curcumin as an effective treatment modality for skin cancer is also emphasized.

35

Din, Zia Ud, Alef dos Santos, Marilia Almeida Trapp, Danielle Lazarin-Bidóia, Francielle Pelegrin Garcia, Francieli Peron, Celso Vataru Nakamura, and Edson Rodrigues-Filho. "Curcumin inspired synthesis of unsymmetrical diarylpentanoids with highly potent anti-parasitic activities: in silico studies and DFT-based stereochemical calculation." MedChemComm 7, no. 5 (2016): 820–31. http://dx.doi.org/10.1039/c5md00599j.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

36

Nagy, L. I., L. Z. Fehér, G. J. Szebeni, M. Gyuris, P. Sipos, R. Alföldi, B. Ózsvári, et al. "Curcumin and Its Analogue Induce Apoptosis in Leukemia Cells and Have Additive Effects with Bortezomib in Cellular and Xenograft Models." BioMed Research International 2015 (2015): 1–11. http://dx.doi.org/10.1155/2015/968981.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Combination therapy of bortezomib with other chemotherapeutics is an emerging treatment strategy. Since both curcumin and bortezomib inhibit NF-κB, we tested the effects of their combination on leukemia cells. To improve potency, a novel Mannich-type curcumin derivative, C-150, was synthesized. Curcumin and its analogue showed potent antiproliferative and apoptotic effects on the human leukemia cell line, HL60, with different potency but similar additive properties with bortezomib. Additive antiproliferative effects were correlated well with LPS-induced NF-κB inhibition results. Gene expression data on cell cycle and apoptosis related genes, obtained by high-throughput QPCR, showed that curcumin and its analogue act through similar signaling pathways. In correlation with in vitro results similar additive effect could be obsereved in SCID mice inoculated systemically with HL60 cells. C-150 in a liposomal formulation given intravenously in combination with bortezomib was more efficient than either of the drugs alone. As our novel curcumin analogue exerted anticancer effects in leukemic cells at submicromolar concentration in vitro and at 3 mg/kg dose in vivo, which was potentiated by bortezomib, it holds a great promise as a future therapeutic agent in the treatment of leukemia alone or in combination.

37

Leslie, Kimberly K., Jamie L. Padilla, Geneva L. Williams, Hua-Ying Fan, Cristian G. Bologa, Eric R. Prossnitz, Jun-Yong Choe, et al. "Abstract 4641: Preclinical evaluation of the novel curcumin Analogue AKT-100 demonstrates therapeutic effectiveness in p53-mutated cancer cells." Cancer Research 84, no. 6_Supplement (March 22, 2024): 4641. http://dx.doi.org/10.1158/1538-7445.am2024-4641.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Abstract Among the myriad of molecular alterations associated with cancer, loss of the normal tumor suppressive functions of p53, the “guardian of the genome,” is the most consistent. Thus, the possibility of targeting oncogenic, mutant p53 proteins has long been a therapeutic goal. However, that aspiration has not been fully realized, leaving patients vulnerable to aggressive disease that is resistant to chemotherapy and to targeted agents such as PARP inhibitors and immunotherapy owing to the loss of wild type p53 functionality and the gain of new oncogenic functions when mutant p53 is expressed. An effective therapeutic strategy is urgently needed for p53 mutant cancers, and our team is developing novel analogues of curcumin with the potential to convert mutant p53 to a wild type conformation and restore its tumor suppressive functions. In this study, we investigated the effects of AKT-100, which was developed from the parent molecule and curcumin analogue HO-3867. Effects were compared to another drug believed to reactivate p53 functionality, APR-246, using CyQUANT IC50 cell proliferation assays and bulk and single cell RNA sequencing. Structural analyses are underway investigating the specific sites of interaction of AKT-100 with various mutant forms of p53. Our findings indicate that, first, AKT-100 exhibits impressive cell killing in multiple ovarian and serous endometrial cancer cells at concentrations ranging from 100-300 nM and is synergistic with the PARP inhibitor olaparib. Second, RNA sequencing demonstrates the reactivation of wild type p53 genes associated with normal cell cycle regulation (induction of CDKN1A encoding p21 and GADD45A), apoptosis (induction of PMAIP1 encoding Noxa and DR5 encoding Death Receptor 5), and the inhibition of DNA replication and multiple alternative mechanisms of DNA repair employed by malignant cells. Third, RNA sequencing indicates that AKT-100 acts through both p53-dependent and independent pathways to inhibit cancer cell proliferation. Gene expression is impacted in ways that portend a therapeutic effect as well as highlight potential resistance pathways (e.g. significant induction of PLK5 encoding polo like kinase 5) that can be further targeted to create synthetic lethal drug combinations with AKT-100 chosen specifically to target the various mutant forms of p53. Taken together, these results identify novel curcumin analogues in early development with the potential to improve therapy for p53 mutant cancers. Through this strategy it is also possible to identify and block resistance pathways that are activated by different forms of mutant p53 in response to AKT-100 and to create synthetic lethal precision drug combinations. Citation Format: Kimberly K. Leslie, Jamie L. Padilla, Geneva L. Williams, Hua-Ying Fan, Cristian G. Bologa, Eric R. Prossnitz, Jun-Yong Choe, Lane E. Smith, Alexander Goss, Robert J. Lake, Avinash D. Sahu. Preclinical evaluation of the novel curcumin Analogue AKT-100 demonstrates therapeutic effectiveness in p53-mutated cancer cells [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 4641.

38

Safitri, Cikra Ikhda Nur Hamidah, Ritmaleni Ritmaleni, Ning Rintiswati, Sardjiman Sardjiman, and Takushi Kaneko. "EVALUATION OF BENZYLIDENE-ACETONE ANALOGUES OF CURCUMIN AS ANTITUBERCULOSIS." Asian Journal of Pharmaceutical and Clinical Research 11, no. 4 (April 1, 2018): 226. http://dx.doi.org/10.22159/ajpcr.2018.v11i4.22991.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Objective: The objective of this research is to evaluate the effect of benzylideneacetone analog of curcumin against Mycobacterium tuberculosis (MTB) H37Rv.Method: The activity of benzylideneacetone analog of curcumin is evaluated using mycobacteria growth indicator tube (MGIT) method and microplate alamar blue assay (MABA) method. The compound of minimum inhibitory concentration (MIC) is defined as the minimum concentration of drugs which really inhibit the growth of MTB.Result: The MIC compound of 1,5-bis(3,4-dichlorophenyl)-1,4-pentadiene-3-one (C9) and 1,5-bis(3-chlorophenyl)-1,4-pentadiene-3-one (C10) can inhibit the bacteria of MTB at the concentration of 500 μg/ml using MGIT method. Based on MABA method, it can be obtained similar MIC value of C9 compound and C10 compound that are 187.5 μg/ml.Conclusion: C9 and C10 have antituberculosis activity. Benzylideneacetone analog of curcumin which has chlor moiety has a better activity in inhibiting MTB, but it still needs further research to make it become a potent antituberculosis drug.

39

Istyastono, Enade Perdana, Rr Sri Untari Siwi S.M.P, Andreas Asdi Utama, and Supardjan A.M. "SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0." Indonesian Journal of Chemistry 4, no. 3 (June 10, 2010): 180–85. http://dx.doi.org/10.22146/ijc.21850.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0). Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

40

Zhao, Chengguang, Zhiguo Liu, and Guang Liang. "Promising Curcumin-based Drug Design: Mono-carbonyl Analogues of Curcumin (MACs)." Current Pharmaceutical Design 19, no. 11 (February 1, 2013): 2114–35. http://dx.doi.org/10.2174/1381612811319110012.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

41

Zhao, Chengguang, Zhiguo Liu, and Guang Liang. "Promising Curcumin-based Drug Design: Mono-carbonyl Analogues of Curcumin (MACs)." Current Pharmaceutical Design 19, no. 11 (April 1, 2013): 2114–35. http://dx.doi.org/10.2174/138161213805289282.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

42

Afzal, Obaid, Mohammad Yusuf, Mohamed Jawed Ahsan, Abdulmalik S. A. Altamimi, Md Afroz Bakht, Amena Ali, and Salahuddin. "Chemical Modification of Curcumin into Its Semi-Synthetic Analogs Bearing Pyrimidinone Moiety as Anticancer Agents." Plants 11, no. 20 (October 16, 2022): 2737. http://dx.doi.org/10.3390/plants11202737.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Natural products (NPs) continue to provide a structural template for the design of novel therapeutic agents and expedite the drug discovery process. The majority of FDA-approved pharmaceuticals used in medical practice can be traced back to natural sources, and NPs play a significant role in drug development. Curcumin, one of the most well-studied chemicals among the NPs, is currently the subject of intense investigation for its biological effects, including the prevention and treatment of cancer. Cancer has overtaken all other causes of death in the world today, with 19.3 million new cases and nearly 10 million deaths predicted in 2020. In the present investigation, we reported the synthesis of three semi-synthetic analogues of curcumin-bearing pyrimidinone moiety by the chemical modification of the diketone function of curcumin followed by their characterization by analytical techniques including infrared (IR), nuclear magnetic resonance (NMR), and mass spectral data. According to the National Cancer Institute (NCI US) methodology, the curcumin analogues (C1-C3) were tested for their anticancer efficacy against 59 cancer cell lines in a single dose assay. 1-(2,6-Dichlorophenyl)-4,6-bis((E)-4-hydroxy-3-methoxystyryl)pyrimidin-2(1H)-one (C2) demonstrated the most promising anticancer activity with mean percent growth inhibition (%GIs) of 68.22 in single dose assay at 10 µM. The compound exhibited >68 %GIs against 31 out of 59 cancer cell lines and was found to be highly active against all leukemia and breast cancer cell lines. The compound C2 showed a lethal effect on HT29 (colon cancer) with %GI of 130.44, while 99.44 %GI was observed against RPMI-8226 (Leukemia). The compound C2 displayed better anticancer activity against the panels of CNS, melanoma, ovarian, prostate, and breast cancer cell lines than curcumin and other anti-EGFR agents gefitinib and imatinib in single dose assay. The compound C2 also demonstrated potent anticancer activity in a 5-dose assay (0.001 to 100 µM) with GI50 values ranging from 1.31 to 4.68 µM; however, it was found to be non-selective with SR values ranging from 0.73 to 1.35. The GI50 values of compound C2 were found to be better than that of the curcumin against all nine panels of cancer cell lines. All of the curcumin analogues were subsequently investigated for molecular docking simulation against EGFR, one of the most attractive targets for antiproliferative action. In molecular docking studies, all the ligands were found to accommodate the active site of EGFR and the binding affinity of ligand C2 was found to be −5.086 kcal/mol. The ligand C2 exhibited three different types of interactions: H-bond (Thr790 and Thr854), π-cationic (Arg841), and aromatic H-bond (Asn842). The curcumin analogues reported in the current investigation may provide valuable therapeutic intervention for the prevention and treatment of cancer and accelerate anticancer drug discovery programs in the future.

43

Changwichit, Kanokwan, Prapapan Temkitthawon, Nantaka Khorana, Apichart Suksamrarn, and Kornkanok Ingkaninan. "Curcumin Analogues as Lead for PDE5 Inhibitors." Open Conference Proceedings Journal 4, no. 1 (March 1, 2013): 210. http://dx.doi.org/10.2174/2210289201304010210.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

44

Bukhari, Syed Nasir Abbas, Ibrahim Bin Jantan, Malina Jasamai, Waqas Ahmad, and Muhammad Wahab Bin Amjad. "Synthesis and Biological Evaluation of Curcumin Analogues." Journal of Medical Sciences 13, no. 7 (September 15, 2013): 501–13. http://dx.doi.org/10.3923/jms.2013.501.513.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

45

Fuchs, James R., Bulbul Pandit, Deepak Bhasin, Jonathan P. Etter, Nicholas Regan, Dalia Abdelhamid, Chenglong Li, Jiayuh Lin, and Pui-Kai Li. "Structure–activity relationship studies of curcumin analogues." Bioorganic & Medicinal Chemistry Letters 19, no. 7 (April 2009): 2065–69. http://dx.doi.org/10.1016/j.bmcl.2009.01.104.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

46

Bukhari, Syed Nasir Abbas, Ibrahim Jantan, Endang Kumolosasi, and Malina Jasamai. "Immunomodulatory effects of diarylpentanoid analogues of curcumin." Medicinal Chemistry Research 24, no. 9 (July 2, 2015): 3405–11. http://dx.doi.org/10.1007/s00044-015-1387-8.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

47

Hosoya, Takahiro, Asami Nakata, Fumie Yamasaki, Faridah Abas, Khozirah Shaari, Nordin Hj Lajis, and Hiroshi Morita. "Curcumin-like diarylpentanoid analogues as melanogenesis inhibitors." Journal of Natural Medicines 66, no. 1 (August 10, 2011): 166–76. http://dx.doi.org/10.1007/s11418-011-0568-0.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

48

Anthwal, Amit, Bandana K. Thakur, M. S. M. Rawat, D. S. Rawat, Amit K. Tyagi та Bharat B. Aggarwal. "Synthesis, Characterization andIn VitroAnticancer Activity of C-5 Curcumin Analogues with Potential to Inhibit TNF-α-Induced NF-κB Activation". BioMed Research International 2014 (2014): 1–10. http://dx.doi.org/10.1155/2014/524161.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

In a search of new compounds active against cancer, synthesis of a series of C-5 curcumin analogues was carried out. The new compounds demonstrated good cytotoxicity against chronic myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Further, these compounds were found to have better potential to inhibit TNF-α-induced NF-κB activation in comparison to curcumin, which show their potential to act as anti-inflammatory agents. Some compounds were found to show higher cytotoxicity against cancer cell lines in comparison to curcumin used as standard.

49

Chainoglou, Eirini, and Dimitra Hadjipavlou-Litina. "Curcumin in Health and Diseases: Alzheimer’s Disease and Curcumin Analogues, Derivatives, and Hybrids." International Journal of Molecular Sciences 21, no. 6 (March 13, 2020): 1975. http://dx.doi.org/10.3390/ijms21061975.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

Worldwide, Alzheimer’s disease (AD) is the most common neurodegenerative multifactorial disease influencing the elderly population. Nowadays, several medications, among them curcumin, are used in the treatment of AD. Curcumin, which is the principal component of Curcuma longa, has shown favorable effects forsignificantly preventing or treating AD. During the last decade, the scientific community has focused their research on the optimization of therapeutic properties and on the improvement of pharmacokinetic properties of curcumin. This review summarizes bibliographical data from 2009 to 2019 on curcumin analogues, derivatives, and hybrids, as well as their therapeutic, preventic, and diagnostic applications in AD. Recent advances in the field have revealed that the phenolic hydroxyl group could contribute to the anti-amyloidogenic activity. Phenyl methoxy groups seem to contribute to the suppression of amyloid-β peptide (Aβ42) and to the suppression of amyloid precursor protein (APP) andhydrophobic interactions have also revealed a growing role. Furthermore, flexible moieties, at the linker, are crucial for the inhibition of Aβ aggregation. The inhibitory activity of derivatives is increased with the expansion of the aromatic rings. The promising role of curcumin-based compounds in diagnostic imaging is highlighted. The keto-enol tautomerism seems to be a novel modification for the design of amyloid-binding agents. Molecular docking results, (Q)SAR, as well as in vitro and in vivo tests highlight the structures and chemical moieties that are correlated with specific activity. As a result, the knowledge gained from the existing research should lead to the design and synthesis ofinnovative and multitargetedcurcumin analogues, derivatives, or curcumin hybrids, which would be very useful drug and tools in medicine for both diagnosis and treatment of AD.

50

Paulraj, Felicia, Faridah Abas, Nordin H. Lajis, Iekhsan Othman, and Rakesh Naidu. "Molecular Pathways Modulated by Curcumin Analogue, Diarylpentanoids in Cancer." Biomolecules 9, no. 7 (July 10, 2019): 270. http://dx.doi.org/10.3390/biom9070270.

Повний текст джерела

Стилі APA, Harvard, Vancouver, ISO та ін.

Анотація:

While curcumin has a range of therapeutic benefits, its potent anticancer activity remains an attractive avenue for anticancer research owing to the multifactorial nature of cancer itself. The structure of curcumin has thus been used as a lead to design more potent analogues, and diarylpentanoids in particular have shown improved cytotoxicity over curcumin. Investigations of diarylpentanoids have demonstrated that these compounds exert anti-cancer effects through several signalling pathways that are associated with cancer. This review focuses on selected diarylpentanoids and highlights molecular targets that modulate key pathways involved in cancer such as NF-κB, MAPK/ERK, and STAT signalling. Future research will need to focus on drug interactions to explore potential synergistic actions of diarylpentanoids and further establish the use of diverse animal models.

Статті в журналах з теми "Curcumine – Analogues"

Оформте джерело за APA, MLA, Chicago, Harvard та іншими стилями