Bidie Alain Dit Philippe, Koffi Ernest, N'Guessan Jean-David, Djaman Allico Joseph, Guede-Guina Frédérique
Laboratoire de pharmacodynamie Biochimique, UFR Biosciences Université de Cocody, 22 BP 582 Abidjan 22, Côte d'Ivoire.
Afr J Tradit Complement Altern Med. 2008 Apr 10;5(3):294-301. doi: 10.4314/ajtcam.v5i3.31286.
Mitragyna ciliata (MYTA) (Rubiaceae) inhibits plasmodia activity. MYTA induces a cardiotonicity of the digitalic type on rat's isolated heart. In this work we studied the effect of MYTA on microsomal Na(+)/K(+) dependant ATPase (Na(+), K(+) ATPase) extracted from the heart of a rabbit since digitalics inhibit Na(+), K(+) ATPase. Our results revealed that the Na(+)/K(+) ATPase has an optimum pH of 7.4 and temperature of 37 degrees C respectively. There is a linear relationship between the organic phosphate formed and the incubation time over 25 mins incubation period. The ATP hydrolysis rate in the presence of MYTA was 0.775 microM/min. LINEWEAVER and BURK plots showed that MYTA did not alter K(M) (1.31 mM) but decreased V(MAX). This study shows that MYTA exerts a non-competitive inhibition on the microsomal Na(+)/K(+) ATPase extracted from rabbit heart with a Ci(50) of 48 microg/ml. We conclude that the mechanism of action of MYTA is linked to the inhibition of the Na(+)/K(+) ATPase like cardiotonics of the digitalic type.
纤毛帽柱木(MYTA)(茜草科)可抑制疟原虫活性。MYTA可使大鼠离体心脏产生洋地黄类强心作用。在本研究中,鉴于洋地黄类药物可抑制钠钾ATP酶,我们研究了MYTA对从兔心脏提取的微粒体钠钾依赖性ATP酶(钠钾ATP酶)的影响。我们的研究结果显示,钠钾ATP酶的最适pH值和温度分别为7.4和37摄氏度。在25分钟的孵育期内,生成的有机磷酸盐与孵育时间呈线性关系。在MYTA存在的情况下,ATP水解速率为0.775微摩尔/分钟。双倒数作图显示,MYTA并未改变米氏常数(1.31毫摩尔),但降低了最大反应速度。本研究表明,MYTA对从兔心脏提取的微粒体钠钾ATP酶具有非竞争性抑制作用,半数抑制浓度为48微克/毫升。我们得出结论,MYTA的作用机制与抑制钠钾ATP酶有关,类似于洋地黄类强心药物。