Natural Compounds Department, National Research Center, Giza, Egypt.
Pharm Biol. 2012 Apr;50(4):490-6. doi: 10.3109/13880209.2011.615842. Epub 2011 Dec 2.
Praziquantel (PZQ) is the drug available for the treatment of schistosomiasis. The reported reduced cure rates, the failure of treatment after PZQ administration in patients and the existence of resistant parasite strains, reinforce the need to rapidly discover new effective molecules against Schistosoma parasite.
To screen the methanol extracts of 79 marine organisms for their schistosomicidal activities against Schistosoma mansoni adult worms in vitro and perform bio-assay directed chromatography for the most active extracts to isolate the active compounds.
Screening of the marine organisms and bio-assay directed chromatography of the most active extracts together with identification of the active isolates using 1D and 2D NMR analysis, were investigated.
RESULTS indicated that the isolates echinosides A and B from the sea cucumbers Actinopyga echinites Jaeger and Holothuria polii Delle Chiaie (Holothuriidae) were highly active. Their LC(50) values were equal to 0.19 μg/ml and 0.27 μg/ml, respectively. Detailed (1)HNMR data for echinosides A and B are reported here for the first time.
These findings demonstrate that the isolated echinosides possess potential in vitro schistosomicidal activity against S. mansoni adult worms. Therefore, echinosides are promising as lead compounds for the development of new schistosomicidal agents.
吡喹酮（PZQ）是治疗血吸虫病的药物。据报道，PZQ 治疗后患者的治愈率降低，治疗失败以及存在耐药寄生虫株，这都加强了我们对迅速发现针对血吸虫寄生虫的新有效分子的需求。
对 79 种海洋生物的甲醇提取物进行筛选，以评估其对曼氏血吸虫成虫的杀血吸虫活性，并对最有效的提取物进行生物活性导向色谱分离，以分离活性化合物。
研究了海洋生物的筛选和最有效的提取物的生物活性导向色谱分离，以及使用 1D 和 2D NMR 分析鉴定活性分离物。
结果表明，来自海参 Actinopyga echinites Jaeger 和 Holothuria polii Delle Chiaie（海参科）的echinosides A 和 B 具有很高的活性。它们的 LC50 值分别为 0.19μg/ml 和 0.27μg/ml。这里首次报道了 echinosides A 和 B 的详细 1HNMR 数据。
这些发现表明，分离出的echinosides 对曼氏血吸虫成虫具有潜在的体外杀血吸虫活性。因此，echinosides 有望成为开发新型杀血吸虫药物的先导化合物。
