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七叶树提取物的静脉张力调节作用、血管保护作用、抗炎作用及自由基清除特性。

Veinotonic effect, vascular protection, antiinflammatory and free radical scavenging properties of horse chestnut extract.

作者信息

Guillaume M, Padioleau F

机构信息

Lipha Group, Department of Pharmacology, Suresnes, France.

出版信息

Arzneimittelforschung. 1994 Jan;44(1):25-35.

PMID:8135874
Abstract

Horse chestnut extract (HCE), containing 70% escin, is the main active component of Veinotonyl 75. The aim of this work was to investigate pharmacological properties attempting to elucidate the efficacy of HCE in chronic venous insufficiency. Veinotonic and lymphagogue properties: HCE dose dependently contracts the canine saphenous isolated vein (cumulative doses 5 x 10(-8) to 5 x 10(-4) g/ml). Its action lasts more than 5 h. In the perfused canine saphenous vein, HCE (25-50 mg in bolus) increases the venous pressure of the normal vein and the pathological vein stenosed 8 days before, and the contractile response to noradrenaline is significantly potentiated. Moreover, during the perfusion in inverse direction of the blood stream, a clear contracting effect on the valves is also obtained with HCE. In the anaesthetized dog, HCE in situ improves the femoral vein compliance and opposes the venous distension obtained during clamping in a carotido-femoral perfusion with constant flow. In other respects, HCE significantly increases femoral venous pressure and flow, together with thoracic lymphatic flow, while respecting the arterial parameters (2.5 and 5 mg/kg i.v.). Vasculotropic action: HCE dose dependently diminishes the cutaneous capillary hyperpermeability induced either by injections of phlogistic agents as histamine and serotonin in the rat (100 to 400 mg/kg p.o.), or by an irritative agent (chloroform) application in the rabbit (50 to 300 mg/kg p.o. and 2.5 to 5 mg/kg i.v.). It significantly increases the vascular resistance in the guinea pig fed a scorbutigenic diet as measured by the petechia method (50 to 400 mg/kg p.o.). Antiedema and antiinflammatory properties: HCE decreases the formation of edemas induced in the rat's hind paw, one of lymphatic origin, the other of inflammatory origin (200 to 400 mg/kg p.o.). In an experimental model of pleurisy in the rat HCE suppresses plasmatic extravasation and leucocytes emigration into the pleural cavity (200 to 400 mg/kg p.o.; 1 to 10 mg/kg i.v.). It decreases the connective tissue formation in the subchronic model of inflammatory granuloma in the rat (400 mg/kg p.o. and 5-10 mg/kg s.c.). Antiradical mechanism of action both in vitro and in vivo: HCE dose dependently inhibits both enzymatic and non-enzymatic in vitro lipid peroxidation (5 x 10(-6) to 5 x 10(-4) g/ml).(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

七叶树提取物(HCE),含70%七叶皂苷,是脉络宁75的主要活性成分。本研究旨在探讨其药理特性,以阐明HCE在慢性静脉功能不全中的疗效。静脉张力调节和促淋巴回流特性:HCE能使犬隐静脉离体标本剂量依赖性收缩(累积剂量5×10⁻⁸至5×10⁻⁴g/ml)。其作用持续超过5小时。在灌注的犬隐静脉中,HCE(单次推注25 - 50mg)可使正常静脉及8天前已狭窄静脉的静脉压升高,且对去甲肾上腺素的收缩反应显著增强。此外,在血流逆向灌注时,HCE对瓣膜也有明显收缩作用。在麻醉犬中,原位给予HCE可改善股静脉顺应性,并对抗在恒定流量的颈总动脉 - 股动脉灌注中夹闭时出现的静脉扩张。在其他方面,HCE显著增加股静脉压力和血流量以及胸导管淋巴流量,同时保持动脉参数不变(静脉注射2.5和5mg/kg)。血管趋向性作用:HCE能剂量依赖性降低大鼠因注射组胺和5 - 羟色胺等炎症介质(口服100至400mg/kg)或兔因涂抹刺激性物质(氯仿)(口服50至300mg/kg及静脉注射2.5至5mg/kg)所诱导的皮肤毛细血管通透性增高。通过瘀点法测定,HCE能显著增加喂饲致坏血病饮食的豚鼠的血管阻力(口服50至400mg/kg)。抗水肿和抗炎特性:HCE可减少大鼠后爪因淋巴源性及炎症源性因素所诱导的水肿形成(口服200至400mg/kg)。在大鼠胸膜炎实验模型中,HCE可抑制血浆渗出及白细胞向胸腔内迁移(口服200至400mg/kg;静脉注射1至10mg/kg)。在大鼠炎症性肉芽肿亚慢性模型中,HCE可减少结缔组织形成(口服400mg/kg及皮下注射5 - 10mg/kg)。体外和体内的抗自由基作用机制:HCE能剂量依赖性抑制体外酶促及非酶促脂质过氧化(5×10⁻⁶至5×10⁻⁴g/ml)。(摘要截选至400字)

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