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2.
Steroids ; 136: 22-31, 2018 08.
Artículo en Inglés | MEDLINE | ID: mdl-29772243

RESUMEN

Steroidal hormones progesterone and testosterone play a vital role in breast and prostate cancers. In this research, we have synthesized and characterized a total of thirty-one (31) new nitrogenous derivatives of progesterone and testosterone. The synthesized derivatives (1-31) were screened for their anti-cancer potential against MCF-7 and PC-3 cell lines of breast using MTT assay. The compounds 1-31exhibited significant inhibitory potentials against MCF-7 and PC-3 cell lines. In MCF-7 assay, compound 17 displayed IC50 value of 04 ±â€¯0.02 µM while compound 18 was leading in PC-3 assay with IC50 of 03.14 ±â€¯0.4 µM. Tamoxifen was used as positive control which exhibited an IC50of 0.12 ±â€¯0.03 and 0.26 ±â€¯0.01 µM against MCF-7 and PC-3 respectively. The compounds also showed good anti-inflammatory activity according to oxidative burst inhibition by chemiluminescence technique where ibuprofen was used as positive control with 73.2 ±â€¯1.4% ROS inhibition. The compounds showed the percent ROS inhibition between 23.2 ±â€¯0.2 and -3.2 ±â€¯4.1. The results of the compounds were compared with the positive control ibuprofen. Molecular docking correlations suggest that the compounds exerted their inhibitory activity by binding to the active of the enzyme.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Simulación del Acoplamiento Molecular , Progesterona/síntesis química , Progesterona/farmacología , Testosterona/síntesis química , Testosterona/farmacología , Antineoplásicos/química , Antineoplásicos/metabolismo , Técnicas de Química Sintética , Ensayos de Selección de Medicamentos Antitumorales , Receptor alfa de Estrógeno/química , Receptor alfa de Estrógeno/metabolismo , Humanos , Células MCF-7 , Células PC-3 , Progesterona/química , Progesterona/metabolismo , Conformación Proteica , Testosterona/química , Testosterona/metabolismo
3.
Front Chem ; 6: 55, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29594100

RESUMEN

In thecurrent research work,eleven metal complexes were synthesized from the hydrazide derivative of ursolic acid. Metal complexes of tin, antimony and iron were synthesized and characterized by FT-IR and NMR spectroscopy. The antibacterial and antioxidant activities were performed for these complexes, which revealed that the metal complexes synthesized are more potent than their parent compounds. We observed that antioxidant activity showed by triphenyltin complex was significant and least activity have been shown by antimony trichloride complex. The synthesized metal complexes were then evaluated against two Gram-negative and two Gram-positive bacterial strains. Triphenyl tin complex emerged as potent antibacterial agent with MIC value of 8 µg/ml each against Shigellaspp, Salmonella typhi and Staphylococcus aureus. While, the MIC value against Streptococcus pneumoniae is 4 µg/ml. Computational docking studies were carried out on molecular targets to interpret the results of antioxidant and antibacterial activities. Based on the results, it may be inferred that the metal complexes of ursolic acid are more active as compared to the parent drug and may be proved for some other pharmacological potential by further analysis.

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