Salvinal is a natural lignan isolated from the roots of Bunge (Danshen). Previous studies have demonstrated its anti-proliferative activity in both drug-sensitive and -resistant cancer cell lines, with IC 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 displayed excellent anticancer activity, with IC 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 showed depolymerization activity in a dose-dependent manner. Our findings indicate that compound is a promising anticancer agent with depolymerization activity that has potential for the management of malignance.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10093915 | PMC |
http://dx.doi.org/10.3390/ijms24076386 | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!