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

[11] Emerging roles of caspase-3 in apoptosis [J].

Porter, AG ;

Jänicke, RU .

CELL DEATH AND DIFFERENTIATION, 1999, 6 (02) :99-104

[12]

[任晓 REN Xiao], 2007, [中国药学杂志, Chinese Pharmaceutical Journal], V42, P907

[13] Auto-redox reaction:: Tin(II) chloride-mediated one-step reductive cyclization leading to the synthesis of novel biheterocyclic 5,6-dihydro-quinazolino[4,3-b]quinazolin-8-ones with three-point diversity [J].

Roy, AD ;

Subramanian, A ;

Roy, R .

JOURNAL OF ORGANIC CHEMISTRY, 2006, 71 (01) :382-385

[14] Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis [J].

Scott, CW ;

Sobotka-Briner, C ;

Wilkins, DE ;

Jacobs, RT ;

Folmer, JJ ;

Frazee, WJ ;

Bhat, RV ;

Ghanekar, SV ;

Aharony, D .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2003, 304 (01) :433-440

[15] Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads [J].

Ullman, BR ;

Aja, T ;

Chen, N ;

Diaz, JL ;

Gu, X ;

Herrmann, J ;

Kalish, VJ ;

Karanewsky, DS ;

Kodandapani, L ;

Krebs, JJ ;

Linton, SD ;

Meduna, SP ;

Nalley, K ;

Robinson, ED ;

Roggo, SP ;

Sayers, RO ;

Schmitz, A ;

Ternansky, RJ ;

Tomaselli, KJ ;

Wu, JC .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (15) :3632-3636

[16] MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity [J].

Yang, W ;

Guastella, J ;

Huang, JC ;

Wang, Y ;

Zhang, L ;

Xue, D ;

Tran, M ;

Woodward, R ;

Kasibhatla, S ;

Tseng, B ;

Drewe, J ;

Cai, SX .

BRITISH JOURNAL OF PHARMACOLOGY, 2003, 140 (02) :402-412

[17] Isoquinoline-1,3,4-trione and its derivatives attenuate β-amyloid-induced apoptosis of neuronal cells [J].

Zhang, Ya-Hui ;

Zhang, Hua-Jie ;

Wu, Fang ;

Chen, Yi-Hua ;

Ma, Xue-Qin ;

Du, Jun-Qin ;

Zhou, Zhong-Liang ;

Li, Jing-Ya ;

Nan, Fa-Jun ;

Li, Jia .

FEBS JOURNAL, 2006, 273 (21) :4842-4852

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