title: Compounds from Polyphaga plancyi and their inhibitory activities against JAK3 and DDR1 kinases.
abstract: 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 IC50values of 12.6 and 5.0μM, respectively. In addition, compound 4 exhibit inhibitory activity towards DDR1 kinase with IC50value of 4.87μM.
authors.affiliation: Guangdong Pharmaceutical University, Guangzhou 510006, PR China; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
authors.forename: Hong-Jie
authors.initials: HJ
authors.lastname: Zhu
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
authors.forename: Yong-Ming
authors.initials: YM
authors.lastname: Yan
authors.affiliation: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, PR China.
authors.forename: Zheng-Chao
authors.initials: ZC
authors.lastname: Tu
authors.affiliation: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, PR China.
authors.forename: Jin-Feng
authors.initials: JF
authors.lastname: Luo
authors.affiliation: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, PR China.
authors.forename: Rui
authors.initials: R
authors.lastname: Liang
authors.affiliation: Department of Hematology, First People's Hospital of Yunnan Province, Kunming 650032, PR China.
authors.forename: Tong-Hua
authors.initials: TH
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China. Electronic address: yxcheng@mail.kib.ac.cn.
authors.forename: Yong-Xian
authors.initials: YX
authors.lastname: Cheng
authors.affiliation: Guangdong Pharmaceutical University, Guangzhou 510006, PR China. Electronic address: shmwang@sina.com.
authors.forename: Shu-Mei
authors.initials: SM
authors.lastname: Wang
mesh_terms: D000818:Animals; D001688:Biological Products / Q000737:chemistry* / Q000302:isolation & purification; D001517:Coleoptera / Q000737:chemistry*; D000070819:Discoidin Domain Receptor 1 / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D053616:Janus Kinase 3 / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D001688:Biological Products; D004791:Enzyme Inhibitors; D000070819:Discoidin Domain Receptor 1; D053616:Janus Kinase 3
keywords: Computational methods; DDR1; Insect; JAK3; Polyphaga plancyi Bolivar