期刊
MOLECULES
卷 27, 期 10, 页码 -出版社
MDPI
DOI: 10.3390/molecules27103067
关键词
sesquiterpenes; antiproliferative activity; Asteraceae; tessaric acid; ilicic acid; ilicic alcohol; Trypanosoma cruzi
资金
- Tricontinental Talent Program of the Canary Islands CEI: Tricontinental Atlantic Campus
- EU Social Fund (FSE)
- Canary Islands ACIISI [TESIS2020010055]
This study evaluated the antiproliferative activity of natural compounds and their derivatives against different cancer cell lines and their effect on a parasite. The results showed that some derivatives exhibited promising antitumor and antiparasitic activities.
Cancer is one of the most important causes of death worldwide. Solid tumors represent the vast majority of cancers (>90%), and the chemotherapeutic agents used for their treatment are still characterized by variable efficacy and toxicity. Sesquiterpenes are a group of natural compounds that have shown a wide range of biological activities, including cytotoxic and antiparasitic activity, among others. The antiproliferative activity of natural sesquiterpenes, tessaric acid, ilicic acid, and ilicic alcohol and their semisynthetic derivatives against HeLa, T-47D, WiDr, A549, HBL-100, and SW1573 cell lines were evaluated. The effect of the compounds on Trypanosoma cruzi epimastigotes was also assessed. The selectivity index was calculated using murine splenocytes. Derivatives 13 and 15 were the most antiproliferative compounds, with GI(50) values ranging between 5.3 (+/- 0.32) and 14 (+/- 0.90) mu M, in all cell lines tested. The presence of 1,2,3-triazole groups in derivatives 15-19 led to improvements in activity compared to those corresponding to the starting natural product (3), with GI(50) values ranging between 12 (+/- 1.5) and 17 (+/- 1.1) mu M and 16 being the most active compound. In relation to the anti-T. cruzi activity, derivatives 7 and 16 obtained from tessaric acid and ilicic acid were among the most active and selective compounds with IC50 values of 9.3 and 8.8 mu M (SI = 8.0 and 9.4), respectively.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据