广山楂炭止血活性部位药效学筛选及作用机制初步研究

目的: 确定广山楂炭的止血活性部位,初步探讨其止血作用的机制。方法: 以昆明小鼠为研究对象,分为石油醚、氯仿、醋酸乙酯、正丁醇、水部位高、低剂量组,云南白药组和空白组。采用断尾法、毛细管法和玻片法测定各组小鼠出血、凝血时间。以 SD 大鼠为研究对象,分为石油醚高、低剂量组,醋酸乙酯高、低剂量组,模型组,云南白药组和空白组。除空白组外,其余组采用皮下注射盐酸肾上腺素加冰浴法复制血瘀出血大鼠模型,测定各组凝血四项、血液流变学、红细胞参数及血小板参数,探讨其止血作用机制。结果: 仅有广山楂炭的石油醚部位与醋酸乙酯部位能缩短小鼠出血、凝血时间;与模型组比较,石油醚组、醋酸乙酯组均缩短活化部分凝血酶原时间、凝血酶时间,延长凝血酶原时间,降低纤维蛋白原含量;升高血小板计数与平均血小板体积,降低血小板压积与血小板平均分布、红细胞计数、血红蛋白浓度、红细胞压积值和血浆黏度,以及高、中、低各切变率下的全血黏度值(P＜0.05)。结论: 石油醚部位、醋酸乙酯部位为广山楂炭的止血有效部位,其机制可能是通过内源性和外源性凝血系统两大途径发挥止血作用。

Pharmacodynamic screening and action mechanism of the hemostatic active site of Charred Fructus Mali

OBJECTIVE To determine the main active parts with hemostatic effect in Charred Fructus Mali, and to explore its hemostatic mechanism.METHODS Kunming mice were divided into high and low dose groups of petroleum ether, chloroform, ethyl acetate, n-butanol and water parts of Charred Fructus Mali, Yunnan Baiyao group and normal group. The bleeding time (BT) and coagulation time (CT) of mice were determined by the end-tail method, capillary method and glass slide method. SD rats were divided into high and low dose groups of petroleum ether and ethyl acetate parts of Charred Fructus Mali, model group, Yunnan Baiyao group and blank group. Except the normal group, the other groups were with the blood stasis and hemorrhage model rats, which were established by subcutaneous injection of epinephrine hydrochloride and ice bath. The hemostatic mechanism was studied by detecting the blood coagulation, hemorheology and red blood cell parameters after the treatment with the active parts of Charred Fructus Mali.RESULTS Both the petroleum ether and ethyl acetate fractions of Charred Fructus Mali could shorten the bleeding and coagulation time of mice. Compared with the model group, the high and low dose groups of petroleum ether and ethyl acetate parts could shorten activated partial thomboplastin time and thombin time significantly, while prolong prothrombin time and decrease fibrinogen level. Platelet count and mean platelet volume were increased, while platelet volume, mean platelet distribution, red blood cell, hemoglobin, hematocrit, plasma viscosity and whole blood viscosity at high, medium and low shear rates were decreased significantly(P＜0.05).CONCLUSION Petroleum ether and ethyl acetate fractions are effective hemostatic parts of Charred Fructus Mali, and its mechanism may play a role in hemostasis through two major pathways: endogenous and exogenous coagulation systems.