SIRT1 Inhibitory Diterpenoids from the Vietnamese Medicinal Plant Croton tonkinensis

被引:17
作者
Dao, Trong Tuan [1 ]
Le, Thi Van Thu [1 ]
Nguyen, Phi Hung [1 ]
Thuong, Phuong Thien [1 ]
Pham Thi Hong Minh [2 ]
Woo, Eun-Rhan [1 ]
Lee, Kwang Youl [3 ]
Oh, Won Keun [1 ]
机构
[1] Chosun Univ, Coll Pharm, Project Team BK21, Kwangju 501759, South Korea
[2] Vietnam Acad Sci & Technol, Inst Chem, Hanoi, Vietnam
[3] Chonnam Natl Univ, Coll Pharm, Kwangju, South Korea
基金
新加坡国家研究基金会;
关键词
Croton tonkinensis; Euphorbiaceae; SIRT1; ent-kaurane diterpenoid; ent-11; alpha-acetoxy-7; beta-hydroxykaur-16-en-15-one; DEACETYLASE; FAMILY; GAGNEP;
D O I
10.1055/s-0029-1240863
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of Croton tonkinensis resulted in the isolation of a new ent-kaurane diterpenoid (1) along with 11 known compounds (2-12). The structure of the new compound 1 was determined to be ent-11 alpha-acetoxy-7 beta-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 6-9, 11, and 12 exhibited SIRT1 inhibitory activity in an in vitro assay, with IC(50) values ranging from 16.08 +/- 0.11 to 44.34 +/- 2.32 mu M. This is the first report showing the potential of ent-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.
引用
收藏
页码:1011 / U74
页数:4
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