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罗布麻提取物对豚鼠离体心房的强心作用。

Cardiotonic effect of Apocynum venetum L. extracts on isolated guinea pig atrium.

作者信息

Irie Kaoru, Sato Takahiro, Tanaka Ippei, Nakajima Jun-ichiro, Kawaguchi Maiko, Himi Toshiyuki

机构信息

Faculty of Pharmacy and Research Institute of Pharmaceutical Sciences, Musashino University, 1-1-20 Shinmachi, Nishitokyo, Tokyo, Japan.

出版信息

J Nat Med. 2009 Apr;63(2):111-6. doi: 10.1007/s11418-008-0296-2. Epub 2008 Nov 11.

Abstract

The effects on guinea-pig heart muscle of extracts of Apocynum venetum L. leaf, root, stem, old stem and Venetron--a polyphenol-rich extract of leaves--were studied by recording the mechanical activity and heart rate of isolated right atria. Cymarin--a cardiac glycoside--was also determined in A. venetum extracts by LC-MS/MS analysis. All extracts examined here showed a weak cardiotonic effect, i.e., induced a contractile response of the isolated atria and increased the pulse at a concentration of 1 mg/mL, which was not inhibited by propranolol (1 microM)-a beta-adrenoceptor blocker. The cymarin content in extracts of A. venetum was ranked as follows: old stem >> stem > root > leaf >> Venetron. Since the cardiotonic effects of A. venetum extracts did not reflect the cymarin content, a possible mechanism other than that of cardiac glycosides was investigated. The inhibitory effects on phosphodiesterase 3 (PDE3) were studied in a cell-free enzyme assay; all extracts of various parts of A. venetum inhibited PDE purified from human platelets. These results suggest that PDE3 inhibition may contribute to the cardiotonic effects of A. venetum extracts.

摘要

通过记录离体右心房的机械活动和心率,研究了罗布麻叶、根、茎、老茎提取物以及罗布麻宁(一种富含多酚的叶提取物)对豚鼠心肌的影响。还通过液相色谱-串联质谱分析测定了罗布麻提取物中的毒毛旋花子苷元。此处检测的所有提取物均显示出微弱的强心作用,即在浓度为1mg/mL时可诱导离体心房产生收缩反应并加快脉搏,且该作用不受β-肾上腺素受体阻滞剂普萘洛尔(1μM)的抑制。罗布麻提取物中毒毛旋花子苷元的含量排序如下:老茎>>茎>根>叶>>罗布麻宁。由于罗布麻提取物的强心作用与毒毛旋花子苷元含量不相符,因此研究了除强心苷之外的可能机制。在无细胞酶测定中研究了对磷酸二酯酶3(PDE3)的抑制作用;罗布麻各部位的所有提取物均抑制了从人血小板中纯化的PDE。这些结果表明,抑制PDE3可能是罗布麻提取物产生强心作用的原因。

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