Synthesis，anti-melanoma activity and acute toxicity of aporphine alkaloids in zebrafish
10.11665/j.issn.1000-5048.20210503
- VernacularTitle:阿朴菲类生物碱的合成、抗黑色素瘤活性及其斑马鱼急性毒性评价
- Author:
Yili WAN
1
;
Hui ZHONG
;
Li CHEN
;
Jianbo SUN
Author Information
1. 中国药科大学中药学院
- Publication Type:Journal Article
- Keywords:
aporphine alkaloids;
synthesis;
melanoma;
safety evaluation;
structure activity relationship
- From:
Journal of China Pharmaceutical University
2021;52(5):529-535
- CountryChina
- Language:Chinese
-
Abstract:
In this study, 10 aporphine alkaloids were synthesized with 1, 2-methylenedioxy substituent in ring A and 9, 10, 11-position with different substituents in ring D. Their structures were determined by ESI-MS,13C NMR and 1 H NMR.The potencial antitumor activity of these compounds against B16F10 melanoma cells were evaluated by MTT assay, and their structure-activity relationship was further analyzed.Meanwhile, zebrafish acute toxicity test was conducted to evaluate the safety of the active compounds.The results showed that some compounds had strong inhibitory activity on tumor cells, and could significantly inhibit the proliferation of B16F10 melanoma cells.Compound IVa has the best anti-melanoma activity with wide safety range, and can be used as a lead compound for further study on anti-proliferation of B16F10 melanoma cells.
