Piperbetol, methylpiperbetol, piperol A and piperol B: A new series of highly specific PAF receptor antagonists from Piper betle

doi:10.1055/s-2006-957685

	Piperbetol, methylpiperbetol, piperol A and piperol B: A new series of highly specific PAF receptor antagonists from Piper betle
	Zeng, HW ; Jiang, YY; Cai, DG ; Bian, J ; Long, K ; Chen, ZL
刊名	PLANTA MEDICA
	1997-08
卷号	63 期号:4 页码:296-298
关键词	platelet activating factor PAF antagonist platelet aggregation piperbetol methylpiperbetol piperol A piperol B Piper betle Piperaceae
ISSN号	0032-0943
DOI	10.1055/s-2006-957685
文献子类	Article
英文摘要	Piperbetol, methylpiperbetol, piperol A, and piperol B, isolated from Piper betle, selectively inhibited the washed rabbit platelet aggregation induced by platelet activating factor (PAF) in a concentration-dependent manner. The IC50 values of piperbetol, methylpiperbetol, piperol A, piperol B, and ginkgolide B were about 18.2, 10.6, 114.2, 11.8, and 4.8 mu mol/l, respectively. The inhibitory potency of ginkgolide B was about 2.8, 1.2, 22.8, and 1.4 times higher than those of piperbetol, methylpiperbetol, piperol A, and piperol B, The concentration-response curve of PAF-induced platelet aggregation was shifted to the right by 50 mu mol/l of piperbetol, methylpiperbetol, piperol A, piperol B, and ginkgolide B. The EC50 of PAF was increased by these compounds from 1.5 nmol/l to 14.3, 23.1, 2.4, 20.6, and 47.2 mol/l, respectively. The compounds also inhibited the binding of [H-3]-PAF to washed rabbit platelets with IC50 values of 8.7, 5.3, 88, 6.2, and 1.8 mu mol/l. Correlating with the inhibitory potency for platelet aggregation, the inhibitory potency of ginkgolide B for binding of PAF was about 3.8, 1.9, 48, and 2.4 times higher than those of piperbetol, methylpiperbetol, piperol A, and piperol B. However, the aggregation of washed rabbit platelets induced by threshold ADP and arachidonic acid were unaffected by piperbetol, methylpiperbetol, piperol A, and piperol B. Furthermore, piperbetol, methylpiperbetol, piperol A, and piperol B had no effects on the cAMP contents in rest washed rabbit platelets, In conclusion, these data indicate that piperbetol, methylpierbetol, piperol A, and piperol B are effective PAF receptor antagonists in vitro.
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:A1997XQ45200002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274893]
专题	中国科学院上海药物研究所
作者单位	1.ACAD SINICA, SHANGHAI INST MAT MED, SHANGHAI 200031, PEOPLES R CHINA 2.PHARM CTR NAVY, SHANGHAI 200081, PEOPLES R CHINA 3.Second Mil Med Univ, COLL PHARM, DEPT PHARMACOL, SHANGHAI 200433, PEOPLES R CHINA
推荐引用方式 GB/T 7714	Zeng, HW,Jiang, YY,Cai, DG,et al. Piperbetol, methylpiperbetol, piperol A and piperol B: A new series of highly specific PAF receptor antagonists from Piper betle[J]. PLANTA MEDICA,1997,63(4):296-298.
APA	Zeng, HW,Jiang, YY,Cai, DG,Bian, J,Long, K,&Chen, ZL.(1997).Piperbetol, methylpiperbetol, piperol A and piperol B: A new series of highly specific PAF receptor antagonists from Piper betle.PLANTA MEDICA,63(4),296-298.
MLA	Zeng, HW,et al."Piperbetol, methylpiperbetol, piperol A and piperol B: A new series of highly specific PAF receptor antagonists from Piper betle".PLANTA MEDICA 63.4(1997):296-298.