The synthesis and cytotoxic activity of derivatives of 4β-hydroxywithanolide E

Wen-Juan Xu; Qin Xiao; Chen-Lei Lian; Chong Zhang; Jie-Qing Liu

doi:10.1016/j.steroids.2020.108776

The synthesis and cytotoxic activity of derivatives of 4β-hydroxywithanolide E

Steroids. 2021 Feb:166:108776. doi: 10.1016/j.steroids.2020.108776. Epub 2020 Dec 15.

Authors

Wen-Juan Xu¹, Qin Xiao¹, Chen-Lei Lian¹, Chong Zhang¹, Jie-Qing Liu²

Affiliations

¹ School of Medicine, Huaqiao University, Quanzhou 362021, PR China.
² School of Medicine, Huaqiao University, Quanzhou 362021, PR China. Electronic address: liujieqing@hqu.edu.cn.

PMID: 33338476
DOI: 10.1016/j.steroids.2020.108776

Abstract

4β-Hydroxywithanolide E, which can be obtained in large amounts from the Physalis genus, possessed anti-proliferative effects on a variety of human cancer cell lines. For discussing its anti-tumor structure-activity relationship, a series of 4β-hydroxywithanolide E derivatives (1-17) were synthesized and evaluated for their antitumor activity in vitro towards acute promyelocytic leukemia NB4 cell line by the Alarma blue assay. Cytotoxicity data revealed that the enone structure and C-4 hydroxyl substituents of ring A, together with the side chain (C-20-C-28) play an important effect on the cytotoxicity.

Keywords: 4β-Hydroxywithanolide E; Cytotoxic activity; Structure modification.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents, Phytogenic
Apoptosis / drug effects
Drug Screening Assays, Antitumor
Humans
Physalis
Structure-Activity Relationship
Withanolides*

Substances

4-hydroxywithanolide E
Antineoplastic Agents, Phytogenic
Withanolides