Antiplatelet aggregation and antithrombotic benefits of terpenes and flavones from hawthorn leaf extract isolated using the activity-guided method†,Food & Function

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Antiplatelet aggregation and antithrombotic benefits of terpenes and flavones from hawthorn leaf extract isolated using the activity-guided method†
Food & Function ( IF 5.1 ) Pub Date : 2019-01-09 00:00:00 , DOI: 10.1039/c8fo01862f
Pinyi Gao _{1,

2,

3,

4,

5} , Shuangshuang Li _{1,

2,

3,

4,

5} , Kechun Liu _{6,

7,

8} , Chen Sun _{6,

7,

8} , Shaojiang Song _{1,

2,

3,

4,

5} , Lingzhi Li _{1,

2,

3,

4,

5}

Affiliation

Hawthorn is a well-known functional food; at present, increasing attention has been given to hawthorn leaf due to its numerous functional and nutritional properties. In this study, the antithrombotic properties of hawthorn leaves were evaluated using the activity-guided isolation process and high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS). A crude extract prepared in 75% ethanol was fractionated using macroporous resin D101 and polyamide chromatography to obtain three active fractions (Fr.C, Fr.C-1 and Fr.C-2). Thereafter, the inhibitory activities of these fractions were examined by platelet aggregation and antithrombus assays using a zebrafish model. Using the HPLC-QTOF-MS technique, we identified 25 compounds in the active fraction (Fr.C). The structures of these compounds were identified by comparing the retention time (t_R) and mass spectral data from the previous reports and 19 reference compounds. Based on the analysis, 21 peaks were detected in the mass spectrum of Fr.C-1 and 8 peaks were detected in Fr.C-2, we found that 11 compounds in Fr.C-1 exhibited potent inhibitory effects on platelet aggregation, including nine monoterpenoids, one diterpenoid and one flavanone. Accordingly, monoterpenoids are suggested as the main anti-platelet aggregation constituents from hawthorn leaves. Particularly, compounds 10 and 24 inhibited ADP-induced platelet aggregation and delayed FeCl₃-induced thrombus in zebrafish. Furthermore, interactions between compounds 10 and 24 with two ADP receptors P2Y₁ and P2Y₁₂, serving as the target for key regulators of antiplatelet aggregative activity, were investigated via molecular modeling. In addition, five flavones were obtained from the active fraction (Fr.C-2). These results indicated that monoterpenoid glycosides and some flavones were responsible for the antithrombotic activity of hawthorn leaves. Moreover, this study shows that the activity-guided isolation is a fast, efficient and systematic separation method for the identification of active compounds in natural products.

中文翻译：

活性指导方法从山楂叶提取物中提取的萜烯和黄酮的抗血小板凝集作用和抗血栓形成作用†

山楂是一种著名的功能食品。目前，由于山楂叶的许多功能和营养特性，它已经引起了越来越多的关注。在这项研究中，使用活性导向的分离过程和高效液相色谱-四极杆飞行时间质谱（HPLC-QTOF-MS）对山楂叶的抗血栓性质进行了评估。使用大孔树脂D101和聚酰胺色谱法分馏在75％乙醇中制得的粗提物，获得三个活性馏分（Fr.C，Fr.C-1和Fr.C-2）。此后，通过使用斑马鱼模型的血小板聚集和抗血栓测定法检查了这些级分的抑制活性。使用HPLC-QTOF-MS技术，我们在活性级分（Fr.C）中鉴定出25种化合物。t _R）和先前报告和19种参考化合物的质谱数据。通过分析，在Fr.C-1的质谱图中检测到21个峰，在Fr.C-2的质谱图中检测到8个峰，我们发现Fr.C-1中的11种化合物对血小板聚集具有有效的抑制作用，包括9种单萜，一种二萜和一种黄烷酮。因此，建议将单萜类化合物作为山楂叶的主要抗血小板聚集成分。特别地，化合物10和24抑制斑马鱼中ADP诱导的血小板凝集并延迟FeCl ₃诱导的血栓。此外，化合物10和24与两个ADP受体P2Y的相互作用通过分子模型研究了作为抗血小板聚集活性关键调节剂的靶标₁和P2Y₁₂。此外，从活性级分（Cr.C-2）中获得了五个黄酮。这些结果表明，单萜类糖苷和一些黄酮是山楂叶的抗血栓形成活性的原因。此外，这项研究表明，活性引导分离是一种快速，有效和系统的分离方法，用于鉴定天然产物中的活性化合物。

更新日期：2019-01-09

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