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[从石南藤和毛山蒌中分离与鉴定血小板活化因子抑制剂]

[The isolation and identification of PAF inhibitors from Piper wallichii (Miq.) Hand-Mazz and P. hancei Maxim].

作者信息

Han G Q, Wei L H, Li C L, Qiao L, Jia Y Z, Zheng Q T

出版信息

Yao Xue Xue Bao. 1989;24(6):438-43.

PMID:2609983
Abstract

Platelet activating factor (PAF) is a highly potent endogenous phospholipid mediator, involved in various inflammatory and cardiovascular disorders. As part of a research program dealing with PAF inhibitors isolated from Piper plant species, we have isolated kadsurenone (I), denudatin B (II), and N-isobutyl-deca-trans-2-trans-4-dienamide (III) from Piped wallichii (Miq.) Hand-Mazz. and P. hancei Maxim. In a continuing search for potential PAF inhibitor from plants, using PAF induced platelet aggregation as a guide, a new neolignan named hancinone D (IV) was isolated from P. hancei maxim. By X-ray analysis it was identified as a racemate. The X-ray analysis led to a revision of the previously made structure assignment of hancinone C. Another new neolignan named wallichinine (V), which was identified as an analogue of (IV), along with the known compounds hancinone C (VI), galgravin (VII), dihydropiperlonguminine (VIII) and crotepoxide (IX) were isolated from P. wallichii (Miq.) Hand-Mazz. The structure determination was based upon spectroscopic analysis. All of the compounds were for the first time obtained from both plants. In the test of platelet aggregation caused by PAF, I, II, V, VI, VII showed inhibitory activity, whereas III, IV, VII, IX showed no activity.

摘要

血小板活化因子(PAF)是一种高效的内源性磷脂介质,参与多种炎症和心血管疾病。作为从胡椒属植物中分离PAF抑制剂研究项目的一部分,我们已从华胡椒(Piper wallichii (Miq.) Hand-Mazz.)和海南胡椒(P. hancei Maxim.)中分离出了海风藤酮(I)、去甲环烯醚萜苷B(II)和N-异丁基-反-2-反-4-癸二烯酰胺(III)。在持续从植物中寻找潜在PAF抑制剂的过程中,以PAF诱导的血小板聚集为指导,从海南胡椒中分离出了一种名为汉辛酮D(IV)的新木脂素。通过X射线分析确定其为外消旋体。X射线分析导致了对之前确定的汉辛酮C结构的修正。从华胡椒中分离出了另一种名为瓦氏胡椒碱(V)的新木脂素,它被确定为(IV)的类似物,同时还分离出了已知化合物汉辛酮C(VI)、加拉格文(VII)、二氢胡椒碱(VIII)和巴豆环氧素(IX)。结构测定基于光谱分析。所有这些化合物均首次从这两种植物中获得。在PAF诱导的血小板聚集试验中,I、II、V、VI和VII显示出抑制活性,而III、IV、VIII和IX则无活性。

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