Yin Zhenhua, Zhang Yong, Zhang Juanjuan, Wang Jinmei, Kang Wenyi
Zhengzhou Key Laboratory of Medicinal Resources Research, Huanghe Science and Technology College, Zhengzhou, 450063, China.
Henan Joint International Research Laboratory of Drug Discovery of Small Molecules, Zhengzhou, 450063, China.
Chem Cent J. 2018 Dec 3;12(1):126. doi: 10.1186/s13065-018-0490-6.
The flowers of Malus pumila Mill (Rosaceae) is rich in resources, but lack of medicinal value research. Chemical constituents of the same family M. pumila have coagulatory activity. Considering the coagulatory activity could be beneficial for various cardiovascular diseases, the aim of this study is to evaluate coagulatory active constituents of M. pumila flowers.
Chemical constituents of M. pumila flowers were isolated by various column chromatographies, and their coagulatory activity were evaluated by activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT) and fibrinogen (FIB) in vitro.
Nine compounds were isolated from M. pumila flowers, and identified as kaempferol-3-O-β-D-glucopyranoside (1), kaempferol-7-O-β-D-glucopyranoside (2), kaempferol-3-O-α-L-arabinofuranoside (3), phloridzin (4), kaempferol (5), phloretin (6), β-sitosterol (7), lupeol (8) and pyracanthoside (9). Compounds 1-9 were isolated from the flowers for the first time, compounds 1, 2 and 9 were isolated from the genus for the first time. Compound 2 could significantly shorten APTT, TT and PT, but significantly decrease the content of FIB. Compound 3 could shorten PT. Compound 4 could significantly shorten TT and PT, but significantly decrease the content of FIB. Compound 5 shortened APTT. Compound 6 and 7 could significantly shorten APTT and PT. Compound 9 was able to prolong TT and decrease the content of FIB, but shorten PT.
Compounds 2-7 possessed significant procoagulant activity in vitro, compound 9 had anticoagulant activity in vitro, which showed coagulation potential of compounds from M. pumila flowers, as a new source of bioactive molecules for therapeutic purposes.
苹果花（蔷薇科）资源丰富，但缺乏药用价值研究。同科植物苹果的化学成分具有凝血活性。鉴于凝血活性可能对多种心血管疾病有益，本研究旨在评估苹果花的凝血活性成分。
采用多种柱色谱法分离苹果花的化学成分，并通过活化部分凝血活酶时间（APTT）、凝血酶原时间（PT）、凝血酶时间（TT）和纤维蛋白原（FIB）体外评估其凝血活性。
从苹果花中分离出9种化合物，分别鉴定为山奈酚-3-O-β-D-吡喃葡萄糖苷（1）、山奈酚-7-O-β-D-吡喃葡萄糖苷（2）、山奈酚-3-O-α-L-阿拉伯呋喃糖苷（3）、根皮苷（4）、山奈酚（5）、根皮素（6）、β-谷甾醇（7）、羽扇豆醇（8）和火棘苷（9）。化合物1-9首次从花中分离得到，化合物1、2和9首次从该属植物中分离得到。化合物2可显著缩短APTT、TT和PT，但显著降低FIB含量。化合物3可缩短PT。化合物4可显著缩短TT和PT，但显著降低FIB含量。化合物5缩短APTT。化合物6和7可显著缩短APTT和PT。化合物9可延长TT并降低FIB含量，但缩短PT。
化合物2-7在体外具有显著的促凝血活性，化合物9在体外具有抗凝血活性，这表明苹果花中的化合物具有凝血潜力，可作为治疗目的的生物活性分子新来源。
