Design, Synthesis and Biological Evaluation of Novel Gypsogenin Derivatives as Potential Anticancer and Antimicrobial Agents.
Chem Biodivers
; 21(6): e202400471, 2024 Jun.
Article
en En
| MEDLINE
| ID: mdl-38594210
ABSTRACT
Natural compounds are important sources for the treatment of chronic disorders such as cancer and microbial infectious disorders. In this research, Gypsogenin and its derivatives (2 a-2 f) have been tested against different cancer cell lines (MCF-7, HeLa, Jurkat and K562â
cell lines) and further analyzed for cell proliferation, cell death type, and for act of the mechanism. Cell proliferation was determined by the MTT method and cell death types were analyzed with HO/PI staining. Fibroblast Growth Factor 1 (FGF-1), Interleukin 1 (IL-1), Interleukin 6 (IL-6), and Tumor Necrosis Factor Alpha (TNF-α), key players in breast cancer development and progression, were determined by Elisa kits. Results showed that compoundâ
2 e inhibited the MCF-7â
cell line proliferation with an IC50 value of 0.66±0.17â
µM with 93.38 % apoptosis rate. Compoundâ
2 e also decreased FGF-1, IL-1, IL-6, and TNF-α levels. Molecular docking studies performed in the binding site of FGFR-1 indicated that compoundâ
2 e formed key hydrogen bonding with Arg627 and Asn568. Besides, compoundsâ
2 a-2 f were evaluated for their antimicrobial activities against gram-negative and gram-positive bacteria and C. albicans via the microdilution method. Overall, compoundâ
2 e stands out as a potential anticancer agent for future studies.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ensayos de Selección de Medicamentos Antitumorales
/
Diseño de Fármacos
/
Pruebas de Sensibilidad Microbiana
/
Proliferación Celular
/
Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
Chem Biodivers
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2024
Tipo del documento:
Article
País de afiliación:
Turquía
Pais de publicación:
Suiza