Dube Anuradha, Singh Nasib, Saxena A, Lakshmi V
Division of Parasitology, Central Drug Research Institute, Lucknow, 226 001, India.
Parasitol Res. 2007 Jul;101(2):317-24. doi: 10.1007/s00436-007-0469-z. Epub 2007 Feb 10.
In this study, we are reporting antileishmanial activity of a marine sponge Haliclona exigua, belonging to phylum Porifera. The crude methanol extract and its three fractions were tested both in vitro and in vivo. The crude extract exerted almost complete inhibition of promastigotes at 50 microg/ml and 76.4 +/- 6.5% inhibition of intracellular amastigotes at 100 microg/ml concentration with IC50 values of 18.6 microg/ml and 47.2 microg/ml, respectively. When administered to Leishmania donovani infected hamsters at a dose of 500 mg/kg x 5, p.o., it resulted in 72.2 +/- 10.4% inhibition of intracellular amastigotes. At a lower dose (250 mg/kg), it exhibited 43.9 +/- 5.1% inhibition. Among the fractions, highest antileishmanial activity both in vitro (>90%) and in vivo (60.9 +/- 18.3%) was observed in n-butanol (soluble) fraction with IC50 values of 8.2 mug/ml and 31.2 microg/ml against promastigotes and intracellular amastigotes, respectively. Hexane fraction also showed comparatively good activity against both the stages of parasites in vitro but was moderately active in leishmania-infected hamsters. Chloroform fraction resulted in 45 +/- 10.2% inhibition in vivo at a dose of 500 mg/kg x 5, p.o., whereas it was inactive in vitro. n-Butanol (insoluble) fraction was inactive both in vitro and in vivo. Araguspongin C, an alkaloid isolated from n-butanol (soluble) fraction exhibited moderate inhibition of promastigotes and intracellular amastigotes at 100 microg/ml but showed weak antileishmanial action in vivo. Our findings indicate that this marine sponge has the potential to provide new lead toward development of an effective antileishmanial agent and, hence, calls for more exhaustive studies for exploiting the vast world of marine resources to combat the scourge of several parasitic diseases.
在本研究中,我们报告了属于多孔动物门的一种海洋海绵——微小Haliclona海绵的抗利什曼原虫活性。对其粗甲醇提取物及其三个馏分进行了体外和体内测试。粗提取物在50微克/毫升时对前鞭毛体几乎有完全抑制作用,在100微克/毫升浓度时对细胞内无鞭毛体有76.4±6.5%的抑制作用,IC50值分别为18.6微克/毫升和47.2微克/毫升。当以500毫克/千克×5的剂量口服给予感染杜氏利什曼原虫的仓鼠时,它对细胞内无鞭毛体的抑制率为72.2±10.4%。在较低剂量(250毫克/千克)时,其抑制率为43.9±5.1%。在这些馏分中,正丁醇(可溶)馏分在体外(>90%)和体内(60.9±18.3%)均表现出最高的抗利什曼原虫活性,对前鞭毛体和细胞内无鞭毛体的IC50值分别为8.2微克/毫升和31.2微克/毫升。己烷馏分在体外对寄生虫的两个阶段也显示出相对较好的活性,但在感染利什曼原虫的仓鼠中活性中等。氯仿馏分在500毫克/千克×5的剂量口服时,体内抑制率为45±10.2%,而在体外无活性。正丁醇(不溶)馏分在体外和体内均无活性。从正丁醇(可溶)馏分中分离出的一种生物碱——阿拉古海绵素C在100微克/毫升时对前鞭毛体和细胞内无鞭毛体有中等抑制作用,但在体内表现出较弱的抗利什曼原虫作用。我们的研究结果表明,这种海洋海绵有可能为开发有效的抗利什曼原虫药物提供新的先导化合物,因此,需要进行更详尽的研究,以开发广阔的海洋资源来对抗几种寄生虫病的祸害。