Zang Bao-Xia, Jin Ming, Wu Wei, Chen Wen-Mei, Piao Yong-Zhe, Li Jin-Rong
Department of Pharmacology, Beijing Institute of Heart, Lung and Blood Vessel Diseases-Anzhen Hospital, Beijing 100029, China.
Zhongguo Zhong Yao Za Zhi. 2004 Aug;29(8):789-91.
To observe the platelet activating factor (PAF) antagonistic effect of kaempferol.
The specific binding of [3H] PAF to rabbit platelet receptor was investigatedwith radio ligand binding assay (RLBA). Platelet adhesion induced by PAF was measured with spectrophotometry. The elevation of inner free calcium concentration in rabbit polymorphonuclear leukocytes (PMNs) induced by PAF was determined with Fura-2 fluorescent technique.
The 1, 2 or 4 nmol x L(-1) [3H]PAF specific binding to rabbit platelet receptor was inhibited by Kae dosage dependently and the IC50 were 30.8, 74.6 and 92.0 micro mol x L(-1), respectively. The PAF induced reactions of rabbit platelet adhesion and PMNs inner free calcium concentration elevation were inhibited by Kae in a dose-dependent manner. The IC50 of Kae to inhibit platelet adhesion was 65 micromol x L(-1).
Kae is effective in inhibiting the action of PAF and it is a new PAF receptor antagonist.
观察山柰酚对血小板活化因子（PAF）的拮抗作用。
采用放射性配体结合分析法（RLBA）研究[3H]PAF与兔血小板受体的特异性结合。用分光光度法测定PAF诱导的血小板黏附。用Fura-2荧光技术测定PAF诱导的兔多形核白细胞（PMN）内游离钙浓度的升高。
1、2或4 nmol·L（-1）的[3H]PAF与兔血小板受体的特异性结合被山柰酚剂量依赖性抑制，IC50分别为30.8、74.6和92.0 μmol·L（-1）。山柰酚剂量依赖性抑制PAF诱导的兔血小板黏附反应和PMN内游离钙浓度升高。山柰酚抑制血小板黏附的IC50为65 μmol·L（-1）。
山柰酚能有效抑制PAF的作用，是一种新型PAF受体拮抗剂。
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