Antiplatelet aggregation activity of diterpene alkaloids from Spiraea japonica
Li, L; Shen, YM; Yang, XS; Zuo, GY; Shen, ZQ; Chen, ZH; Hao, XJ
AbstractSix 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.
KeywordAtisine-type Diterpene Alkaloid Platelet Aggregation Arachidonic Acid Adenosine-5 '-diphosphate Paf (Platelet-activating Factor) Structure-activity Relationship
Subject AreaPharmacology & Pharmacy
Indexed BySCI
WOS IDWOS:000177717600003
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Document Type期刊论文
Affiliation1.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
Recommended Citation
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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