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首页> 美国卫生研究院文献>Proceedings of the National Academy of Sciences of the United States of America >Characterization of a platelet-activating factor receptor antagonist isolated from haifenteng (Piper futokadsura): specific inhibition of in vitro and in vivo platelet-activating factor-induced effects.
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Characterization of a platelet-activating factor receptor antagonist isolated from haifenteng (Piper futokadsura): specific inhibition of in vitro and in vivo platelet-activating factor-induced effects.

机译：从海芬藤（Piper futokadsura）分离的血小板活化因子受体拮抗剂的特征：体内和体外血小板活化因子诱导的作用的特异性抑制。

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摘要

Platelet-activating factor (PAF) is a potent lipid mediator of inflammation and asthma. Using a receptor preparation of rabbit platelet membranes, we identified a novel antagonist of PAF in the methylene chloride extract of a Chinese herbal plant, haifenteng (Piper futokadsura). The active antagonist, kadsurenone, was isolated and characterized in several in vitro and in vivo assays. It is a specific and competitive inhibitor of PAF binding to its receptor with a Ki of 5.8 X 10(-8) M vs. a Ki of 6.3 X 10(-9) M for PAF itself. It inhibits PAF-induced aggregation of rabbit platelets and human neutrophils at 2.4-24 microM, without showing any PAF agonistic activity. It potently inhibits PAF-induced degranulation of human neutrophils at 2.5-50 microM, also without any agonist activity. Kadsurenone is active orally at 25-50 mg/kg of body weight in blocking PAF-induced cutaneous permeability in the guinea pig. It also inhibits PAF-induced increases of hematocrit and circulating N-acetylglucosaminidase in the rat at greater than 10 mg/kg i.p. in a dose-dependent manner. Kadsurenone does not interfere with the function of several pharmacological mediators and receptors tested. Its structural specificity is evidenced by the poor PAF-antagonistic activities of three related structures isolated from the same haifenteng extract.
机译：血小板激活因子（PAF）是炎症和哮喘的有效脂质介体。使用兔血小板膜的受体制剂，我们在中草药植物海芬藤（Pifu futokadsura）的二氯甲烷提取物中鉴定了一种新型的PAF拮抗剂。分离了活性拮抗剂kadsurenone，并在几种体外和体内试验中进行了表征。它是PAF与其受体结合的特异性竞争抑制剂，KIF为5.8 X 10（-8）M，而PAF自身的Ki为6.3 X 10（-9）M。它在2.4-24 microM抑制PAF诱导的兔血小板和人中性粒细胞的聚集，而没有表现出任何PAF激动活性。它以2.5-50 microM的浓度有效抑制PAF诱导的人类嗜中性粒细胞脱粒，也没有任何激动剂活性。 Kadsurenone以25-50 mg / kg体重的口服活性可阻断豚鼠PAF诱导的皮肤通透性。它还以大于10 mg / kg i.p抑制大鼠PAF引起的血细胞比容和循环N-乙酰氨基葡萄糖苷酶的增加。以剂量依赖的方式。 Kadsurenone不会干扰所测试的几种药理介质和受体的功能。从同一海芬藤提取物中分离的三个相关结构的不良PAF拮抗活性证明了其结构特异性。

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