Siddiqui Ruqaiyyah, Syed Abdul, Tomas Salvador, Prieto-Garcia Jose, Khan Naveed Ahmed
School of Veterinary Medicine and Science, University of Nottingham, Sutton Bonington LE12 5RD, UK.
School of Biological and Chemical Sciences, Birkbeck College, University of London, London, UK.
J Med Microbiol. 2009 Mar;58(Pt 3):327-330. doi: 10.1099/jmm.0.006494-0.
Acanthamoeba is an opportunistic protozoan pathogen that can cause blinding keratitis and a rare but fatal encephalitis involving the central nervous system with a very poor prognosis. This is due to limited availability of effective anti-acanthamoebic drugs. Here, we tested whether the use of liposomes can improve the potency of pentamidine isethionate, an anti-amoebic compound. The liposomes consisted of l-alpha-phosphatidylcholine and cholesterol or ergosterol in a molar ratio of 1 : 5. Pentamidine isethionate was incorporated to achieve a final drug to lipid ratio of 1 : 5. At a drug concentration of 10 microg ml(-1), the liposomal drug was >12 times more effective than the free drug at preventing Acanthamoeba binding to human cells and significantly more effective in reducing parasite-mediated human cell cytopathogenicity, compared with the drug alone. Both the free and liposomal drug blocked Acanthamoeba encystation.
棘阿米巴是一种机会性原生动物病原体，可导致致盲性角膜炎以及一种罕见但致命的涉及中枢神经系统的脑炎，预后极差。这是由于有效的抗棘阿米巴药物供应有限。在此，我们测试了脂质体的使用是否能提高抗阿米巴化合物乙磺半胱氨酸戊烷脒的效力。脂质体由摩尔比为1:5的l-α-磷脂酰胆碱和胆固醇或麦角固醇组成。加入乙磺半胱氨酸戊烷脒以达到最终药物与脂质的比例为1:5。在药物浓度为10微克/毫升时，与游离药物相比，脂质体药物在防止棘阿米巴与人类细胞结合方面的效果高出12倍以上，并且在降低寄生虫介导的人类细胞细胞致病性方面明显更有效。游离药物和脂质体药物均能阻断棘阿米巴的包囊形成。
