| Autor: |
Chi-I Chang, Cheng-Chih Hsieh, Yung-Shung Wein, Ching-Chuan Kuo, Chi-Yen Chang, Jrhau Lung, Jong-Yuh Cherng, Po-Chen Chu, Jang-Yang Chang, Yueh-Hsiung Kuo |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
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| Zdroj: |
International Journal of Molecular Sciences; Volume 24; Issue 7; Pages: 6386 |
| ISSN: |
1422-0067 |
| DOI: |
10.3390/ijms24076386 |
| Popis: |
Salvinal is a natural lignan isolated from the roots of Salvia mitorrhiza Bunge (Danshen). Previous studies have demonstrated its anti-proliferative activity in both drug-sensitive and -resistant cancer cell lines, with IC50 values ranging from 4–17 µM. In this study, a series of salvinal derivatives was synthesized and evaluated for the structure–activity relationship. Among the twenty-four salvinal derivatives, six compounds showed better anticancer activity than salvinal. Compound 25 displayed excellent anticancer activity, with IC50 values of 0.13–0.14 µM against KB, KB-Vin10 (overexpress MDR/Pgp), and KB-7D (overexpress MRP) human carcinoma cell lines. Based on our in vitro microtubule depolymerization assay, compound 25 showed depolymerization activity in a dose-dependent manner. Our findings indicate that compound 25 is a promising anticancer agent with depolymerization activity that has potential for the management of malignance. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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