欢迎访问云南西力生物技术股份有限公司!证券代码:871574
首页 成 果 源于西力产品的客户论文
Antitumor Effect of Sikokianin C, a Selective Cystathionine β-Synthase Inhibitor, against Human Colon Cancer in Vitro and in Vivo. Med. Chem. Commun., 2018, 9: 113–120.
发布时间:2018-01-29 阅读数:1407 来源:Med. Chem. Commun.
分享到:

Abstract:

Cystathionineβ-synthase (CBS)overexpression is related to the proliferation and migration of human coloncancers. Targeted therapy thatinhibits CBS has achieved promising effectsin colon cancer treatments, butno selective inhibitor of CBS is available. In our previous study,a natural biflavonoid compound,sikokianinC,was identified as a potent and selective inhibitor of CBS. However, the mode of action of this compoundand its antitumor efficacyin vivoremain unknown. In the present study, we have demonstrated thatsikokianin C selectivelyinhibits CBS activity in a competitive manner, and the five key residues involved inthe binding of sikokianin C to the substrate channel ofCBS protein were identified via a combination ofmolecular docking and site-directed mutagenesis. Additionally, we analyzed the antitumor efficacy ofsikokianin C against human colon cancer cellsin vitroandin vivo. Sikokianin C greatly suppressed the proliferationof HT29 colon cancer cells with an IC50value of 1.6μM, and CBS is the target of sikokianin C inmammalian cells, as evidenced by CBS knockdown analyses. Moreover, sikokianin C induced the apoptosisof HT29 cancer cells in a dose dependent manner. Treating mice with sikokianin C dramatically reducedthe tumor volume and the weight of the colon cancer xenograftin vivo. These results indicate that the selectiveCBS inhibitor sikokianin C can potentially be used for the treatment of colon cancer.


ewm.jpg 微信公众号
11.jpg 移动官网
特别声明:禁止在未经同意情况下转载本网站信息,BioBioPha品牌产品均由西力生物独家生产与销售,仅用于科学研究或企业研发!
版权所有 2024-2025 云南西力生物技术股份有限公司 BioBioPha 滇ICP备09000810号-1滇公安备案号 53019002000069号
技术支持:奥远科技

联系客服