Activation of Caspase-3 by Terpenoids and Flavonoids in Different Types of Cancer Cells
| Autor: | Suaib Luqman, Vijaya Dubey, Nusrat Masood |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Caspase 3
Cell Line HeLa Terpene 03 medical and health sciences 0302 clinical medicine Drug Discovery Gene expression Transcriptional regulation Humans 030304 developmental biology Flavonoids 0303 health sciences Biological Products biology Activator (genetics) Chemistry Terpenes General Medicine biology.organism_classification Antineoplastic Agents Phytogenic Terpenoid Biochemistry Cell culture 030220 oncology & carcinogenesis |
| Zdroj: | Current topics in medicinal chemistry. 20(21) |
| ISSN: | 1873-4294 |
| Popis: | Background: Caspase-3 is accountable for the execution of apoptosis. Recently, it has gained attention as a promising target for the discovery of natural products as anticancer agents. Methods: We examined the efficacy of two different sets of natural products (terpenoids and flavonoids) towards caspase-3 activity adopting in silico, cell-free and cell-based activity and real-time gene expression analysis. Results: It was observed that terpenes activate caspase-3 activity in both the cell-free and cell-based systems, which was supported by the gene expression analysis, binding energy and activation constant. Flavonoids’ action, however, was limited to the cell-based system and transcriptional regulation suggesting their indirect association, which enhanced the enzyme activity and up-regulated the expression of mRNA levels in the cells. Among the tested natural products, (+) carvone was observed to be the best activator of caspase-3 in K562 (34.4 μM), WRL-68 (22.3 μM), HeLa (18.7 μM), MCF-7 (39.4 μM) and MDA-MB-231 cell lines (45.1 μM). Conclusion: Overall, terpenoids have a persistent activation of caspase-3 in all the investigated systems, while flavonoids circuitously affect the enzyme activity. |
| Databáze: | OpenAIRE |
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