Xanthine Oxidase Inhibitors from Garcinia esculenta Twigs

doi:10.1055/s-0034-1383193

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	Xanthine Oxidase Inhibitors from Garcinia esculenta Twigs
	Zhu, Lun-Lun 1,2; Fu, Wen-Wei 1,2; Watanabe, Shimpei 3; Shao, Yi-Nuo 1,2; Tan, Hong-Sheng 1,2; Zhang, Hong 1,2; Tan, Chang-Heng4 ; Xiu, Yan-Feng 1,2; Norimoto, Hisayoshi 3; Xu, Hong-Xi 1,2
刊名	PLANTA MEDICA
	2014-12
卷号	80 期号:18 页码:1721-1726
关键词	Garcinia esculenta Clusiaceae xanthine oxidase inhibitor 1,3,6,7-tetrahydroxy-xanthone griffipavixanthone
ISSN号	0032-0943
DOI	10.1055/s-0034-1383193
文献子类	Article
英文摘要	The EtOAc-soluble portion of the 80% (v/v) EtOH extract from the twigs of Garcinia esculenta exhibited strong xanthine oxidase inhibition in vitro. Bioassay-guided purification led to the isolation of 1,3,6,7-tetrahydroxyxanthone (3) and griffipavixanthone (8) as the main xanthine oxidase inhibitors, along with six additional compounds (1, 2, 4-7), including two new compounds (1 and 2). This enzyme inhibition was dose dependent with an IC50 value of approximately 1.2 mu M for 3 and 6.3 mu M for 8. The inhibitory activity of 3 was stronger than the control allopurinol (IC50 value: 5.3 mu M). To our knowledge, compound 8 is the first bixanthone that demonstrated potent XO inhibitory activity in vitro. The structures of the new compounds were established by spectroscopic analysis, and the optical properties and absolute stereochemistry of racemic (+/-) esculentin A (2) were further determined by the calculation of the DP4 probability and analysis of its MTPA ester derivatives.
WOS关键词	BIOASSAY-GUIDED ISOLATION ; XANTHONES ; ACYLPHLOROGLUCINOLS ; SPECTROSCOPY ; DERIVATIVES ; LANCILIMBA ; PREDICTION ; CHEMISTRY ; DISCOVERY ; CELLS
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种	英语
出版者	GEORG THIEME VERLAG KG
WOS记录号	WOS:000346411300009
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276812]
专题	天然药物化学研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Xu, Hong-Xi
作者单位	1.Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China; 2.Shanghai Coll TCM New Drug Discovery, Engn Res Ctr, Shanghai, Peoples R China; 3.Kracie Pharma Ltd, Kampo Res Labs, Takaoka, Toyama, Japan; 4.Chinese Acad Sci, Shanghai Inst Biol Sci, State Key Lab Drug Res, Inst Mat Med, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Zhu, Lun-Lun,Fu, Wen-Wei,Watanabe, Shimpei,et al. Xanthine Oxidase Inhibitors from Garcinia esculenta Twigs[J]. PLANTA MEDICA,2014,80(18):1721-1726.
APA	Zhu, Lun-Lun.,Fu, Wen-Wei.,Watanabe, Shimpei.,Shao, Yi-Nuo.,Tan, Hong-Sheng.,...&Xu, Hong-Xi.(2014).Xanthine Oxidase Inhibitors from Garcinia esculenta Twigs.PLANTA MEDICA,80(18),1721-1726.
MLA	Zhu, Lun-Lun,et al."Xanthine Oxidase Inhibitors from Garcinia esculenta Twigs".PLANTA MEDICA 80.18(2014):1721-1726.