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藿香的化学成分与凝血活性

Chemical constituents and coagulation activity of Agastache rugosa.

作者信息

Cao Pengran, Xie Pingyao, Wang Xuebiao, Wang Jinmei, Wei Jinfeng, Kang Wen-Yi

机构信息

Institute of Chinese Materia Medica, Henan University, Kaifeng, 475004, China.

Kaifeng Key Laboratory of Functional Components in Health Food, Kaifeng, 475004, China.

出版信息

BMC Complement Altern Med. 2017 Feb 6;17(1):93. doi: 10.1186/s12906-017-1592-8.

Abstract

BACKGROUND

In the Chinese traditional medicine, plant of Agastache rugosa (Fisch. & C.A. Mey.) Kuntze (A. rugosa) has been used to treat nausea, vomiting and dispel damp. However, currently, few reports about the chemical constituents, especially the non-volatile components of A. rugosa are available.

METHODS

Through separation with various column chromatographies to elucidate the chemical constituents of A. rugosa, the biological activities of the major constituents were investigated. The extracts and main constituents of A. rugosa were evaluated for their anticoagulant effects by assaying the activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT) and fibrinogen (FIB) in vitro.

RESULTS

Seven known compounds (namely compounds 1-7) were isolated from the aerial parts of A. rugosa. They were identified as methyl hexadecanoate (1), β-sitosterol (2), acacetin (3), ursolic acid (4), apigenin (5), protocatechuic acid (6) and tilianin (7), respectively. Compounds 1 and 6 were isolated from the genus Agastache for the first time, and compound 4 was obtained from the plants for the first time. The results showed that the extract of A. rugosa had a significant procoagulant activity by shortening the time of PT (P < 0.001) and increasing FIB content (P < 0.001), as compared with Vitamin K. While its major constituents acacetin and tilianin exhibited significant anticoagulant activities by prolonging the times of PT, APTT, TT and reducing FIB content (P < 0.001), as compared with blank control group.

CONCLUSIONS

The total extract of A. rugosa possessed significant procoagulant activity, while its main components, acacetin and tilianin possessed significant anticoagulant activities. Further investigation should be pursued to find out the bioactivity components responsible for the procoagulant action of the plant.

摘要

背景

在中国传统医学中,藿香(Agastache rugosa (Fisch. & C.A. Mey.) Kuntze)已被用于治疗恶心、呕吐和祛湿。然而,目前关于藿香化学成分,尤其是非挥发性成分的报道较少。

方法

通过各种柱色谱分离方法阐明藿香的化学成分,并研究主要成分的生物活性。通过体外测定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),评估藿香提取物和主要成分的抗凝作用。

结果

从藿香地上部分分离得到7个已知化合物(即化合物1 - 7)。它们分别被鉴定为十六烷酸甲酯(1)、β-谷甾醇(2)、金合欢素(3)、熊果酸(4)、芹菜素(5)、原儿茶酸(6)和田蓟苷(7)。化合物1和6首次从藿香属植物中分离得到,化合物4首次从该植物中获得。结果表明,与维生素K相比,藿香提取物通过缩短PT时间(P < 0.001)和增加FIB含量(P < 0.001)具有显著的促凝血活性。而其主要成分金合欢素和田蓟苷与空白对照组相比,通过延长PT、APTT、TT时间和降低FIB含量(P < 0.001)表现出显著的抗凝活性。

结论

藿香总提取物具有显著的促凝血活性,而其主要成分金合欢素和田蓟苷具有显著的抗凝活性。应进一步研究以找出导致该植物促凝血作用的生物活性成分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ee0/5294890/d1466c1ddc30/12906_2017_1592_Fig1_HTML.jpg

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