Mechanisms of Action of Uncaria rhynchophylla Ethanolic Extract for Its Vasodilatory Effects

被引:25
|
作者
Loh, Yean Chun [1 ]
Ch'ng, Yung Sing [1 ]
Tan, Chu Shan [1 ]
Ahmad, Mariam [1 ]
Asmawi, Mohd Zaini [1 ]
Yam, Mun Fei [1 ]
机构
[1] Univ Sains Malaysia, Sch Pharmaceut Sci, Dept Pharmacol, Minden 11800, Penang, Malaysia
关键词
anti-hypertension; Chinese medicine; signaling; mechanism pathways; traditional vasodilation; Uncaria rhynchophylla; GEISSOSCHIZINE METHYL-ETHER; INDOLE ALKALOIDS; IN-VITRO; VASORELAXANT; HOOK; ENDOTHELIUM; INHIBITION; PRINCIPLES;
D O I
10.1089/jmf.2016.3804
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Uncaria rhynchophylla is one of the major components included in Traditional Chinese Medicine prescriptions for hypertensive treatment. Previous studies have suggested that U. rhynchophylla might contain vasodilation-mediating active compounds, especially indole alkaloids. Hence, this study was carried out to determine the vasodilatory effects of U. rhynchophylla, which was extracted by different solvents. The most effective extract was then further studied for its signaling mechanism pathways. The authenticity of U. rhynchophylla was assured by using modernized tri-step Fourier transform infrared (FTIR), including conventional 1D FTIR, second derivative scanning combined with 2D-correlated IR spectroscopy. Results obtained proved that the fingerprint of U. rhynchophylla used was identical to the atlas. Isolated aortic rings frommale Sprague-Dawley rats were preconstricted with phenylephrine (PE) followed by cumulative addition of U. rhynchophylla extracts. The signaling mechanism pathways were studied by incubation with different receptor antagonists before the PE precontraction. In conclusion, the 95% ethanolic U. rhynchophylla extract (GT100) was found to be most effective with an EC50 value of 0.028 +/- 0.002 mg/mL and an R-max value of 101.30% +/- 2.82%. The signaling mechanism pathways employed for exerting its vasodilatory effects included nitric oxide/soluble guanylyl cylcase/cyclic guanosine monophosphate (NO/sGC/cGMP) and PGI(2) (endothelium-derived relaxing factors), G protein-coupled M-3- and beta 2 receptors, regulation of membrane potential through voltage-operated calcium channel, intracellular Ca2+ released from inositol triphosphate receptor (IP3R), and all potassium channels except the Kca channel.
引用
收藏
页码:895 / 911
页数:17
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