Coagulant Effects and Mechanism of Schefflera heptaphylla (L.) Frodin.

Xuqiang Liu,Xuqiang Liu,Zhenhua Liu,Qiongxin Liang,Hui-Min David Wang,Ruian Xu,Ruian Xu,Wenyi Kang,Jing Dong

doi:10.3390/molecules24244547

Abstract

Schefflera heptaphylla (L.) Frodin, are commonly used in anti-inflammatory, analgesic, traumatic bleeding and hemostasisas. In this paper, the coagulation effect of the ethanol extract (Set), ethyl acetate phase (Sea) and n-butanol phase (Sbu) was evaluated by prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen content (FIB) assays in vitro. Then, Three main lupanine triterpenes (compounds A–C) were isolated and identified from Sea and Sbu by a bioassay-guided method and their structure were identified as 3α-Hydroxy-lup-20(29)-ene-23, 28-dioic acid, betulinic acid 3-O-sulfate and 3α-Hydroxy-lup-20(29)-ene-23, 28-dioic acid 28-O-(α-l-rhamnopyranosyl(1→4)-O-β-d-glucopyranosyl(1→6))-β-d-glucopyranoside) by spectroscopic data analysis. Among of them, compound B was confirmed to have significant coagulant effect in vitro. Furthermore, the pro-coagulation mechanism of S. heptaphylla extracts and compound B were investigated by measuring whole blood viscosity (WBV), plasma viscosity (PV), erythrocyte sedimentetion rate (ESR), pack cell volume (PCV), APTT, PT, TT, and FIB in vivo. Meanwhile, the levels of thromboxane B2 (TXB2), 6-keto prostaglandin F1α (6-keto-PGF1α), endothelial nitric oxide synthase (eNOS) and (endothelin-1) ET-1 were detected. The bleeding time (BT) was tested by tail bleeding method, which proved the traumatic bleeding and hemostasis activities of S. heptaphylla. The pharmacology experiments showed that the Set, Sea, Sbu and compound B has significant pro-coagulation effect. In addition, compound B might be the main constituent of pro-coagulation in S. heptaphylla These results could support the fact that S. heptaphylla could be used traditionally to cure traumatic bleeding, and the pro-coagulation effects were associated with the regulation of vascular endothelium active substance and hemorheology parameters.

Highlights

As we all known, blood is an important substance of the human body
Considering the traditional uses in traumatic bleeding and hemostasis of leaves of S. heptaphylla, we evaluated the pro-coagulation effect of Set, Sea and Sbu by Plasma coagulation parameters (PT, activated partial thromboplastin time (APTT), thxrombin time (TT), FIB) assay in vitro
The results showed that heparin had weaker and pro-coagulation effects of them maybe were associated with the regulation of Thromboxane A2 (TXA2) and PGI

Summary

Introduction

Blood is an important substance of the human body. If the disease of bleeding is not stopped timely and effectively, it will cause blood loss and lead to weakness of the body and even endanger life, such as clinical hemorrhage, traumatic bleeding and so on. Many hemostatic drugs are widely used in clinical practice, including vitamin K1, vitamin K3, vitamin K4 as activating coagulant factor; carbazochrome sodium sulfonate (CCSS), Carbazochrome as reduce capillary permeability and aminocaproic acid, aminomethylbenzoic acid as antifibrinolytic. Hemostatic drugs, traditionally used in medical practice, are not always effective to reduce blood loss which is dangerous due to the development of hemorrhagic shock, dilutional coagulopathy, or thrombosis and thromboembolic complications [1]. It is important to develop new hemostatic drugs with high efficiency and low side effects. Much more researchers focus on natural products, and had found some natural products with effective pro-coagulation [2,3]

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