Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica

	Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica
	Li, L; Shen, YM ; Yang, XS ; Zuo, GY ; Shen, ZQ ; Chen, ZH ; Hao, XJ
	2002-08-02
发表期刊	EUROPEAN JOURNAL OF PHARMACOLOGY
卷号	449 期号:1-2 页码:23-28
摘要	Six diterpene alkaloids with an atisine-type C-20-skeleton isolated from the Chinese herbal medicines Spiraea japonica var. acuta and S. japonica var. ovalifolia, as well as eight derivatives of spiramine C and spiradine F were evaluated for the ability to inhibit aggregation of rabbit platelets induced by arachidonic acid, ADP, and platelet-activating factor (PAF) in vitro. The results showed that 12 of the 14 atisine-type diterpene alkaloids significantly inhibited PAF-induced platelet aggregation in a concentration-dependent manner, but had no effect on ADP- or arachidonic acid-induced aggregation, exhibiting a selective inhibition. It is the first report that C-20-diterpene alkaloids inhibit PAF-induced platelet aggregation. However, spiramine C1 concentration-dependently inhibited platelet aggregation induced by PAF, ADP and arachidonic acid with IC50 values of 30.5 +/- 2.7, 56.8 +/- 8.4 and 29.9 +/- 9.9 muM, respectively, suggesting a non-selective antiplatelet aggregation action. The inhibitory effect of spiramine C1 on arachidonic acid was as potent as that of aspirin. Primary studies of the structure-activity relationships for inhibition of PAF-induced aggregation showed that the oxygen substitution at the C-15 position and the presence of an oxazolidine ring in spiramine alkaloids were essential to their antiplatelet aggregation effects. These results suggest that the atisine-type alkaloids isolated from S. japonica are a class of novel antiplatelet aggregation agents. (C) 2002 Elsevier Science B.V All rights reserved.
关键词	Atisine-type Diterpene Alkaloid Platelet Aggregation Arachidonic Acid Adenosine-5 '-diphosphate Paf (Platelet-activating Factor) Structure-activity Relationship
学科领域	Pharmacology & Pharmacy
收录类别	SCI
语种	英语
WOS记录号	WOS:000177717600003
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/14627
专题	植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.Chinese Acad Sci, Kunming Inst Bot, Kunming 650204, Yunnan, Peoples R China 2.Kunming Med Coll, Yunnan Pharmacol Labs Nat Prod, Kunming 650031, Yunnan, Peoples R China 3.Key Lab Chem Nat Prod Guizhou Province, Guiyang 550002, Guizhou, Peoples R China 4.Chinese Acad Sci, Guiyang 550002, Guizhou, Peoples R China
推荐引用方式 GB/T 7714	Li, L,Shen, YM,Yang, XS,et al. Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2002,449(1-2):23-28.
APA	Li, L.,Shen, YM.,Yang, XS.,Zuo, GY.,Shen, ZQ.,...&Hao, XJ.(2002).Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica.EUROPEAN JOURNAL OF PHARMACOLOGY,449(1-2),23-28.
MLA	Li, L,et al."Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica".EUROPEAN JOURNAL OF PHARMACOLOGY 449.1-2(2002):23-28.

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