Benzamides and Quinazolines from a Mangrove Actinomycetes Streptomyces sp (No. 061316) and Their Inhibiting Caspase-3 Catalytic Activity in Vitro

被引：19

作者：

Chen, Guodong ^{[1
]}

Gao, Hao ^{[1
,3
]}

Tang, Jinshan ^{[1
]}

Huang, Yuanfan ^{[1
]}

Chen, Ying ^{[1
]}

Wang, Ying ^{[1
]}

Zhao, Huinan ^{[1
]}

Lin, Haipeng ^{[2
]}

Xie, Qingyi ^{[2
]}

Hong, Kui ^{[2
]}

Li, Jia ^{[3
]}

Yao, Xinsheng ^{[1
]}

机构：

[1] Jinan Univ, Inst Tradit Chinese Med & Nat Prod, Jinan Univ Coll Pharm, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China

[2] Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Haikou 571101, Peoples R China

[3] Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2011年 / 59卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Streptomyces sp; benzamide; quinazoline; Caspase-3; APOPTOSIS;

D O I：

10.1248/cpb.59.447

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

One new benzamide,, 3-hydroxyl-2-N-iso-butyryl-anthranilamide (1), together with two known benzamides (2, 3) and three known quinazolines (4-6), was isolated from a mangrove actinomycetes Streptomyces sp. (No. 061316), which displayed inhibiting Caspase-3 activity in vitro. The structure of 1 was elucidated by electrospray ionization (ESI)-MS, NMR spectroscopies and X-ray crystal diffraction. After evaluation of all compounds for their inhibitory effect on,Caspase-3 in vitro, 3-hydroxyl-anthranilamide (2) and 8-hydroxyl-2,4-dioxoquinazoline (6) showed activity against Caspase-3 with IC50 values of 32 and 36 mu M, respectively.

引用

页码：447 / 451

页数：5

共 17 条

[1] Caspase inhibitor affords neuroprotection with delayed administration in a rat model of neonatal hypoxic-ischemic brain injury [J].