Synthesis and biological evaluation of the glycoside (25R)-3β,16β-diacetoxy-22-oxocholest-5-en-26-yl β-d-glucopyranoside: a selective anticancer agent in cervicouterine cell lines
| Autor: | B. Mario Pinto, Moisés López-Dávila, María A. Fernández-Herrera, Hugo López-Muñoz, Sankar Mohan, José M.V. Hernández-Vázquez, Jesús Sandoval-Ramírez, María L. Escobar-Sánchez, Luis Sánchez-Sánchez |
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| Rok vydání: | 2011 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Uterine Cervical Neoplasms Antineoplastic Agents DNA Fragmentation Mass Spectrometry HeLa Glucosides Cell Line Tumor Drug Discovery Cytotoxic T cell Humans Lymphocytes Cell Proliferation Pharmacology chemistry.chemical_classification biology Molecular Structure Chemistry Cell growth Caspase 3 Organic Chemistry Cell Cycle Glycoside General Medicine Cell cycle biology.organism_classification Cholesterol Biochemistry Apoptosis Cell culture Cancer cell Female |
| Zdroj: | European journal of medicinal chemistry. 46(9) |
| ISSN: | 1768-3254 |
| Popis: | The synthesis and biological evaluation of the new cholestane glycoside (25R)-3β,16β-diacetoxy-22-oxocholest-5-en-26-yl β-d-glucopyranoside starting from diosgenin is described. This compound showed selective antiproliferative activity against CaSki, ViBo, and HeLa cervicouterine cancer cells. Its effect on the cell-cycle was determined. The cytotoxic effects of the title compound on cervicouterine cancer cell lines and human lymphocytes indicate that the main cell death process is not necrosis; hence it is not cytotoxic. The title compound induced apoptosis in cervicouterine cancer cells. Importantly, the antiproliferative activity on tumor cells did not affect the proliferative potential of peripheral blood lymphocytes. The title compound showed selective antitumor activity and greater antiproliferative activity than its aglycon, and therefore serves as a promising lead candidate for further optimization. |
| Databáze: | OpenAIRE |
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