Institute of Chinese Materia Medica, Henan University, Kaifeng, 475004, China; Kaifeng Key Laboratory of Functional Components in Health Food, Kaifeng, 475004, China.
Institute of Chinese Materia Medica, Henan University, Kaifeng, 475004, China.
Food Chem Toxicol. 2018 Sep;119:326-333. doi: 10.1016/j.fct.2018.02.049. Epub 2018 Feb 26.
Flowers of Malus halliana (M. halliana) Koehne have been used as a Chinese traditional medicine to treat metrorrhagia and in our study, its chemical composition and anticoagulant effect were investigated. Five compounds were isolated and identified from M. halliana flowers, including limocitrin-3-O-glucoside (1), baohuoside Ⅱ (2), kaempferol-3-O-α-L-furan arabinoside (3), phloretin-4'-O-glycosidase (4) and afzeloside (5). Compound 1-3 were isolated for the first time from this genus. The anticoagulant effect of the compounds and extracts of M. halliana flowers were evaluated by APTT, PT, TT and FIB on plasma of rabbit in vitro. The results indicated that several fractions of M. halliana flowers and compounds 2-5 exhibited anticoagulant activity in vitro. Subsequently, afzeloside (5), the abundant component in M. halliana flowers, was investigated further for its antithrombotic effect in vivo and its antithrombotic mechanisms were evaluated on rats acute blood-stasis model. The antithrombotic effect was evaluated by WBV, PV, HCT, ESR, APTT, PT, TT, FIB, 6-keto-PGF1α, TXB2, ET-1 and eNOS in vivo. Afzeloside demonstrated inhibitory effect of thrombus formation, and its underlying antithrombotic mechanism was found to be related to the regulation of vascular endothelium active substance, activating blood flow and anticoagulant effect. Hence, we postulate that flavonoids may be the active ingredients of the plant.
苹果属华西花的花被用作中药来治疗月经过多，在本研究中，研究了华西花的化学成分和抗凝作用。从华西花的花中分离并鉴定了 5 种化合物，包括 limocitrin-3-O-葡萄糖苷（1）、宝藿苷 Ⅱ（2）、山柰酚-3-O-α-L-呋喃阿拉伯糖苷（3）、根皮苷-4'-O-葡萄糖苷（4）和芹菜素-7-O-新橙皮糖苷（5）。化合物 1-3 是首次从该属中分离得到的。通过兔血浆体外 APTT、PT、TT 和 FIB 评估华西花的化合物和提取物的抗凝作用。结果表明，华西花的几个部位和化合物 2-5 具有体外抗凝活性。随后，进一步研究了华西花中丰富的成分芹菜素-7-O-新橙皮糖苷（5）的体内抗血栓作用及其在大鼠急性血瘀模型中的抗血栓机制。通过 WBV、PV、HCT、ESR、APTT、PT、TT、FIB、6-酮-PGF1α、TXB2、ET-1 和 eNOS 评价体内抗血栓作用。芹菜素-7-O-新橙皮糖苷显示出抑制血栓形成的作用，其潜在的抗血栓机制与调节血管内皮活性物质、激活血流和抗凝作用有关。因此，我们推测类黄酮可能是该植物的活性成分。
