Compounds from Polyphaga plancyi and their inhibitory activities against JAK3 and DDR1 kinases

被引：22

作者：

Zhu, Hong-Jie ^{[1
,2
]}

Yan, Yong-Ming ^{[2
]}

Tu, Zheng-Chao ^{[3
]}

Luo, Jin-Feng ^{[3
]}

Liang, Rui ^{[3
]}

Yang, Tong-Hua ^{[4
]}

Cheng, Yong-Xian ^{[2
]}

Wang, Shu-Mei ^{[1
]}

机构：

[1] Guangdong Pharmaceut Univ, Guangzhou 510006, Guangdong, Peoples R China

[2] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China

[3] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China

[4] First Peoples Hosp Yunnan Prov, Dept Hematol, Kunming 650032, Peoples R China

来源：

FITOTERAPIA | 2016年 / 114卷

关键词：

Polyphaga plancyi Bolivar; Insect; Computational methods; JAK3; DDR1; POLYRHACHIS-DIVES; INSECT; DERIVATIVES; COX-1;

D O I：

10.1016/j.fitote.2016.09.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Plancyamides A (1) and B (3), plancypyrazine A (2), and plancyols A (4) and B (5), five new compounds (1-5), and three known ones (6-8), were isolated from the whole bodies of Polyphaga plancyi Bolivar. Their structures were elucidated by a combination of spectroscopic analyses including 1D and 2D NMR, and HRESIMS. Among them, compound 3 is racemic, chiral HPLC separation afforded its respective enantiomers. The absolute configuration of 1 was assigned by computational methods. Biological evaluation of all the compounds with exception of 7 and 8 discloses that compounds 2 and 4 could inhibit JAK3 kinase with IC50 values of 12.6 and 5.0 mu M, respectively. In addition, compound 4 exhibit inhibitory activity towards DDR1 kinase with IC50 value of 4.87 mu M. (C) 2016 Elsevier B.V. All rights reserved.

引用

页码：163 / 167

页数：5

共 18 条

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