Identification of plumbagin and sanguinarine as effective chemotherapeutic agents for treatment of schistosomiasis.
Identification of plumbagin and sanguinarine as effective chemotherapeutic agents for treatment of schistosomiasis.
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DOI：
10.1016/j.ijpddr.2012.12.001
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发表时间：
2013-12
影响因子：
4
通讯作者：
Coultas, Kristen A.
中科院分区：
文献类型：
--
作者：
Zhang, Si-Ming;Coultas, Kristen A.
►只有一种药物(吡喹酮)可用于治疗血吸虫病。►已证明两种化合物(白花黄素和血根碱)具有很强的抗血吸虫活性。►的体外抗血吸虫作用符合世界卫生组织控制血吸虫病的HIT化合物的标准。两种化合物处理后虫体的►形态变化和被膜变化有很大不同。血吸虫病是一种通过蜗牛传播的寄生虫病，影响着全球2亿多人。目前，血吸虫病的治疗依赖于吡喹酮的单一疗法，这是一种30多年前开发的药物。因此，迫切需要开发替代的抗血吸虫药物。在寻找新的抗血吸虫药物的过程中，我们检查了45个化合物的抗血吸虫活性，这些化合物已被报道具有抗微生物和/或抗寄生虫活性。从植物中提取的两个化合物，白花黄素和血根素，在体外被发现具有很强的抗血吸虫活性。对于这两种化合物，浓度为10μM(相当于白花蛇精的1.88g/ml和血根素的3.68g/ml)在48小时内可导致100%的死亡率，符合世界卫生组织控制血吸虫病的“Hit”化合物的标准。两种化合物处理后的虫体形态和外皮变化有很大不同。两种化合物处理后蠕虫的显著形态变化表明，这两种化合物针对不同的生物途径，都会导致寄生虫的死亡。这项研究提供了证据，表明白花丹和血根那林确实有潜力成为治疗血吸虫病的有效替代化疗药物。
► Only one drug (praziquantel) is available for treatment of schistosomiasis. ► Two compounds (plumbagin and sanguinarine) have shown to possess potent antischistosomal activity. ► In vitro antischistosomal effects meet the WHO’s criterion of “hit” compounds for the control of schistosomiasis. ► Morphological changes and tegumental alternations of worms treated by the two compounds are quite different. Schistosomiasis, a snail-borne parasitic disease, affects more than 200 million people worldwide. Currently the treatment of schistosomiasis relies on a single therapy of praziquantel, a drug developed over 30 years ago. Thus, there is an urgent need to develop alternative antischistosomal drugs. In the pursuit of novel antischistosomal drugs, we examined the antischistosomal activities of 45 compounds that had been reported to exhibit antimicrobial and/or antiparasitic activities. Two plant-derived compounds, plumbagin and sanguinarine, were found to possess potent antischistosomal activities in vitro. For both the compounds, a concentration of 10 μM (equivalent to 1.88 μg/ml for plumbagin and 3.68 μg/ml for sanguinarine) resulted in 100% mortality at 48 h, which meets the World Health Organization’s (WHO) criterion of “hit” compounds for the control of schistosomiasis. Morphological changes and tegumental alterations of the dead worms treated by the two compounds were quite different. The significant morphological changes of worms after treatment by the two compounds suggest the two compounds target different biological pathways, both of which result in parasite’s death. This study provides evidence to suggest plumbagin and sanguinarine have real potential as effective alternative chemotherapeutic agents for the treatment of schistosomiasis.
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影响因子：
15.8
作者：
Abdulla MH;Lim KC;Sajid M;McKerrow JH;Caffrey CR
通讯作者：
Caffrey CR
影响因子：
2
作者：
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作者：
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通讯作者：
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影响因子：
64.5
作者：
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通讯作者：
Su X
影响因子：
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作者：
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通讯作者：
Kolodziej, Herbert