摘要
美人蕉_ _ Cannaceae 是一种有价值的植物,用于治疗多种疾病。然而,支持传统用途治疗心脏病的科学证据很少。基于先前报道的C. indica的抗血栓作用,本研究旨在从其己烷馏分中分离出纯化合物,并评估分离化合物的抗血小板和抗凝血活性。NMR 和 MS 光谱方法用于阐明化合物结构。采用比浊法测定抗血小板活性。通过测定凝血酶原时间、活化部分凝血活酶时间和凝血酶时间来检查抗凝作用。这是首次从C. indica中分离出 8 种已知化合物:24-亚甲基环阿坦-3β-ol ( 1 )、stigma-4-ene-3-one ( 2 )、stigmast-4-ene-3,6 -二酮 ( 3 )、6β-羟基豆油-4-en-3-酮 ( 4 )、β-谷甾醇、ent -kaur-15-ene-19-al-17-oic 酸 ( 5 )、16α-Hydro-19 -al- ent- kauran-17-oic 酸 ( 6 ) 和 16 α -Hydro-19-ol -ent -kauran-17-oic 酸 ( 7 )。β-谷甾醇和 16α-Hydro-19-al -ent- kauran-17-oic 酸先前已被证明具有抗血栓作用。该研究首次证明1、2、3、4和5表现出剂量依赖性抗血小板作用。此外,2对ADP诱导的血小板聚集具有最高的抑制作用(0.4 mg/ml,平均抑制百分比,77.27%),并通过延长活化的部分凝血活酶时间来影响内在凝血。化合物1对 ADP 诱导的血小板聚集具有非常轻微的影响。1、3、4、5和7没有观察到抗凝血活性。 _ C. indica根茎是治疗和预防心脏病的抗血栓化合物的潜在来源。应该进行进一步的研究以阐明抗血栓作用的机制并从该植物中鉴定出更多的生物活性化合物。
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Antithrombotic Activity of the Steroids and ent-Kaurane Diterpenoids from Canna indica Rhizomes
Abstract
Canna indica L. Cannaceae, is a valuable plant used for the treatment of many conditions. However, the scientific evidence to support the traditional use for treatment of heart diseases is scarce. Based on previously reported antithrombotic effect of C. indica, this study aimed to isolate pure compounds from its hexane fraction, and evaluate antiplatelet and anticoagulant activity of isolated compounds. NMR and MS spectroscopic methods were used to elucidate compound structures. The antiplatelet activity was tested by a turbidimetric method. The anticoagulant effect was examined by measuring prothrombin time, activated partial thromboplastin time and thrombin time. This is the first report on the isolation of 8 known compounds from C. indica: 24-methylenecycloartan-3β-ol (1), stigma-4-ene-3-one (2), stigmast-4-ene-3,6-dione (3), 6β-hydroxystigmast-4-en-3-one (4), β-sitosterol, ent-kaur-15-ene-19-al-17-oic acid (5), 16α-hydro-19-al-ent-kauran-17-oic acid (6) and 16α-hydro-19-ol-ent-kauran-17-oic acid (7). β-Sitosterol and 16α-hydro-19-al-ent-kauran-17-oic acid were previously documented to have antithrombotic effects. This study proved for the first time that 1, 2, 3, 4 and 5 showed dose-dependent antiplatelet effects. Furthermore, 2 exposed the highest inhibitory effect on ADP-induced platelet aggregation (at 0.4 mg/ml, mean percentage inhibition, 77.27%) and affected the intrinsic blood coagulation with prolonged activated partial thromboplastin time. Compound 1 had a very mild effect on ADP-induced platelet aggregation. No anticoagulant activity was observed for 1, 3, 4, 5 and 7. C. indica rhizome is a potential source of antithrombotic compounds for treating and preventing heart diseases. Further studies should be done to clarify the mechanisms of antithrombotic action and identify more bioactive compounds from this plant.
Graphical Abstract