Candeias M F, Abreu P, Pereira A, Cruz-Morais J
Department of Chemistry, University of Evora, R. Romão Ramalho 59, 7000-671 Evora, Portugal.
J Ethnopharmacol. 2009 Jan 12;121(1):117-22. doi: 10.1016/j.jep.2008.08.032. Epub 2008 Nov 1.
Present study reports on the general bioactivity of strictosamide and on its effects on Na(+),K(+)-ATPase and Mg(2+)-ATPase activities of Charles River male mouse. Strictosamide is the main glycoalkaloid of Sarcocephalus latifolius (Rubiaceae) leaves and roots, used as medicinal plant in folk medicine. In this work, we studied the in vitro effects of various concentrations of strictosamide (0.25, 0.5, 1 or 2 mg/mL) and the in vivo effects of single doses (50, 100 or 200 mg/kg, i.p.) of this compound on kidney and brain Na(+),K(+)-ATPase and Mg(2+)-ATPase activities. Results of general study showed that strictosamide is slightly toxic to Charles River mouse (LD(50)=723.17 mg/kg), producing CNS depression and kidney toxicity, but the exact mechanism of these effects could not be defined. Strictosamide inhibited the in vitro and in vivo Mg(2+)-ATPase activity on kidney but had nonsignificant effect on brain. Furthermore, strictosamide had nonsignificant in vitro and in vivo effect on kidney Na(+),K(+)-ATPase activity but produced an in vivo increase of Na(+),K(+)-ATPase activity of brain, these findings suggesting that strictosamine may be related to the induction of alpha(2) isoform of Na(+),K(+)-ATPase and may account for the folk use of Sarcocephalus latifolius root infusion on hypertension.
本研究报道了士的宁酰胺的一般生物活性及其对查尔斯河雄性小鼠钠钾 - ATP酶和镁离子 - ATP酶活性的影响。士的宁酰胺是阔叶非洲帽柱木(茜草科)叶和根中的主要糖苷生物碱,在民间医学中用作药用植物。在本研究中,我们研究了不同浓度的士的宁酰胺(0.25、0.5、1或2 mg/mL)的体外作用以及该化合物单剂量(50、100或200 mg/kg,腹腔注射)对肾脏和大脑钠钾 - ATP酶及镁离子 - ATP酶活性的体内作用。综合研究结果表明,士的宁酰胺对查尔斯河小鼠有轻微毒性(半数致死量=723.17 mg/kg),可导致中枢神经系统抑制和肾脏毒性,但这些作用的确切机制尚不清楚。士的宁酰胺在体外和体内均抑制肾脏的镁离子 - ATP酶活性,但对大脑无显著影响。此外,士的宁酰胺在体外和体内对肾脏钠钾 - ATP酶活性无显著影响,但可使大脑钠钾 - ATP酶活性在体内增加,这些发现表明士的宁酰胺可能与钠钾 - ATP酶α2亚型的诱导有关,这可能解释了阔叶非洲帽柱木根煎剂在民间用于治疗高血压的原因。