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桑色素从白桑中提取,抑制动脉血栓形成,调节血小板激活,用于治疗心血管疾病。

Morusinol extracted from Morus alba inhibits arterial thrombosis and modulates platelet activation for the treatment of cardiovascular disease.

机构信息

Department of Pharmacology, College of Pharmacy & Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon, Korea.

出版信息

J Atheroscler Thromb. 2012;19(6):516-22. doi: 10.5551/jat.10058. Epub 2012 Apr 4.

Abstract

UNLABELLED

Morus alba (white mulberry) has been used in traditional Chinese medicine as an anti-headache, diuretic, expectorant, and anti-diabetic agent. In previous studies, extracts of Morus alba demonstrated favorable biological properties, such as antioxidant activity, suppression of lipoxygenase (LOX)-1, cytotoxicity against cancer cells, and inhibition of the invasion and migration of cancer cells.

AIM

This study further evaluated the effects of morusinol, a flavonoid derived from Morus alba root bark, on platelet aggregation and thromboxane B(2) (TXB(2) formation in vitro and thrombus formation in vivo.

METHODS

The antiplatelet potential of morusinol was measured using in vitro rabbit platelet aggregation and TXB(2) formation assays. Arterial thrombus formation was investigated using an in vivo ferric chloride (FeCl(3)-induced thrombosis model.

RESULTS

Morusinol significantly inhibited collagen- and arachidonic acid-induced platelet aggregation and TXB(2) formation in cultured platelets in a concentration-dependent manner. Thrombus formation was reduced by 32.1, 42.0, and 99.0% for collagen-induced TXB(2) formation, and 8.0, 24.1, and 29.2% for arachadonic acid-induced TXB(2) formation, with 5, 10, and 30 µg/mL morusinol, respectively. Moreover, oral morusinol (20 mg/kg) or aspirin (20 mg/kg) for three days significantly increased the time to occlusion in vivo by 20.3±5.0 or 6.8±2.9 min, respectively, compared with the control (1% CMC, carboxymethyl cellulose).

CONCLUSION

Taken together, these results indicate that morusinol may significantly inhibit arterial thrombosis in vivo due to antiplatelet activity. Thus, morusinol may exert beneficial effects on transient ischemic attacks or stroke via the modulation of platelet activation.

摘要

目的

本研究进一步评估从桑白皮中提取的类黄酮——桑色醇对血小板聚集和血栓烷 B2(TXB2)形成的体外作用,以及体内血栓形成的影响。

方法

采用体外兔血小板聚集和 TXB2 形成试验测定桑色醇的抗血小板作用。采用体内三氯化铁(FeCl3)诱导的血栓形成模型研究动脉血栓形成。

结果

桑色醇可浓度依赖性地抑制胶原和花生四烯酸诱导的培养血小板聚集和 TXB2 形成。5、10 和 30μg/ml 的桑色醇对胶原诱导的 TXB2 形成的抑制率分别为 32.1%、42.0%和 99.0%,对花生四烯酸诱导的 TXB2 形成的抑制率分别为 8.0%、24.1%和 29.2%。此外,连续 3 天口服桑色醇(20mg/kg)或阿司匹林(20mg/kg)可使体内闭塞时间分别延长 20.3±5.0 和 6.8±2.9min,与对照组(1%CMC,羧甲基纤维素)相比。

结论

综上所述,这些结果表明桑色醇可能通过抗血小板作用显著抑制体内动脉血栓形成。因此,桑色醇可能通过调节血小板激活对短暂性脑缺血发作或中风产生有益作用。

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