Nyansah Wilson Bright, Koffuor George Asumeng, Asare Frederick, Gyanfosu Linda
Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.
J Intercult Ethnopharmacol. 2016 Mar 30;5(2):153-61. doi: 10.5455/jice.20160324054355. eCollection 2016 Mar-Apr.
Currently available therapeutic options for thromboembolic disorders are often very expensive and are associated with unfavorable side effects.
To establish the anticoagulant effect and safety profile of an extract made from of the root bark of Pseudocedrela kotschyi (Schweinf.) Harms and the aerial part of Adenia cissampeloides (Planch. ex Hook.) Harms (PAE).
PAE (0.5-2.0 g/L) effect on prothrombin time (PT) and activated partial thromboplastin time (aPTT) were evaluated on whole blood drawn from the marginal ear vein of New Zealand White rabbits. Effect of PAE (250-2000 mg/kg) on bleeding time (BT) and clotting time (CT) in Sprague-Dawley rats were also assessed. Histopathological, hematological, and liver function studies were also carried out to assess the safety for use of PAE (250-2000 mg/kg).
PAE had no significant effect (P > 0.05) on PT, but resulted in a significant increase (P ≤ 0.05-0.0001) in aPTT. The PAE treatment resulted in a significant increase (P ≤ 0.05-0.0001) in BT and CT in vivo compared with control. Safety studies indicated no deaths with PAE treatment with hematological and liver function tests being normal. Histological studies revealed pathological changes in the liver at a PAE treatment dose of 2000 mg/kg but all doses had no detrimental effect on kidney and stomach tissue. The no-observed-adverse-effect-level was <2000 mg/kg when given orally.
PAE has anticoagulant effect in vitro and is safe to use at oral doses <2000 mg/kg.
目前用于治疗血栓栓塞性疾病的治疗方案通常非常昂贵,且伴有不良副作用。
确定由柯氏假香椿(Schweinf.)Harms的根皮和腺叶藤(Planch. ex Hook.)Harms的地上部分制成的提取物(PAE)的抗凝作用和安全性。
在从新西兰白兔耳缘静脉采集的全血上评估PAE(0.5 - 2.0 g/L)对凝血酶原时间(PT)和活化部分凝血活酶时间(aPTT)的影响。还评估了PAE(250 - 2000 mg/kg)对Sprague - Dawley大鼠出血时间(BT)和凝血时间(CT)的影响。还进行了组织病理学、血液学和肝功能研究,以评估PAE(250 - 2000 mg/kg)使用的安全性。
PAE对PT无显著影响(P > 0.05),但导致aPTT显著增加(P≤0.05 - 0.0001)。与对照组相比,PAE治疗导致体内BT和CT显著增加(P≤0.05 - 0.0001)。安全性研究表明,PAE治疗无死亡情况,血液学和肝功能测试正常。组织学研究显示,在PAE治疗剂量为2000 mg/kg时肝脏出现病理变化,但所有剂量对肾脏和胃组织均无有害影响。口服时未观察到有害作用的剂量水平<2000 mg/kg。
PAE在体外具有抗凝作用,口服剂量<2000 mg/kg时使用安全。