Potential of the bitter melon Momordica charantia as a source of anthelmintics

翻译后摘要：寄生线虫（PN）感染仍然是全球人类健康的主要威胁。超过1.5 10亿人感染了PN，儿童，孕妇和老年人特别容易感染 线虫感染的发病率。控制策略仅限于定期驱虫， 这是有限的快速再感染率和抗药性蠕虫的不可避免的发展 人口。目前没有可用于人PN感染的疫苗。因此，有一个明确的和 迫切需要新的药物来治疗PN感染，以防止耐药菌株的出现。PNs的 感染人类的钩虫，由于它们贪婪的吸血活动，可以说是最重要的。 疾病控制和预防中心估计，钩虫目前感染5.76 - 7.4亿 世界各地的人们。感染可能引起贫血和蛋白质缺乏，引起肠胃健康 一般问题，并阻碍儿童的生长和认知发展。苦瓜 charantia在钩虫流行地区广泛种植，并被用作传统药物 寄生虫感染和其他疾病。M. Charantia（MCE） 已显示抑制感染性钩虫幼虫（L3）的进食，并杀死成虫和L4钩虫， 体外，以及其他几种线虫。生物活性物质的化学鉴定和表征 这些成分可能导致开发治疗钩虫和其他PN感染的药物。在这里我们建议 从M.利用钩虫死亡率的charantia 锡兰钩虫筛选级分。在目标1中，我们将使用天然产物化学来分离 从植物材料的其余部分中提取活性成分，并进行生物测定以鉴定活性驱虫剂 MCE中的化合物。在目标2中，我们将确定分离的驱虫剂是否能成功治疗 体内钩虫感染。确定MCE的活性成分，这些成分负责植物的 显着的驱虫活性和确认其体内活性可能导致开发一种新的 治疗钩虫和其他PN的驱虫药。

Abstract: Parasitic nematode (PN) infections remain a major threat to human health globally. More than 1.5 billion people are infected with PNs, with children, pregnant women, and the elderly especially susceptible to morbidity from nematode infection. Control strategies are restricted to periodic de-worming of infected individuals, which is limited by rapid re-infection rates and the inevitable development of drug resistant worm populations. There are currently no vaccines available for human PN infections. Therefore, there is a clear and pressing need for new drugs to treat PN infections to forestall the emergence of resistant isolates. Of the PNs infecting humans, hookworms are arguably the most important due to their voracious blood feeding activities. The Center for Disease Control and Prevention estimates that hookworm currently infects 576-740 million people worldwide. Infection may cause anemia and protein deficiency, causing gastrointestinal health problems generally and retarded growth and cognitive development in children. The bitter melon Momordica charantia is widely grown in areas where hookworm is endemic, and has been used as a traditional medicine for parasitic infections and other disease in developing countries. Aqueous extracts of M. charantia (MCE) have been shown to inhibit feeding of infective hookworm larvae (L3) and to kill adult and L4 hookworm in vitro, as well as several other nematodes. Chemical identification and characterization of the biologically active component(s) may lead to development of a drug to treat hookworm and other PN infections. Here we propose to isolate the active anthelmintic compound(s) from M. charantia using mortality of the hookworm Ancylostoma ceylanicum to screen fractions. In Aim 1, we will use natural product chemistry to separate the active component(s) from the rest of the plant material and a bioassay to identify the active anthelmintic compund(s) within MCE. In Aim 2, we will determine if the isolated anthelmintic can successfully treat hookworm infections in vivo. Identifying the active components of MCE that are responsible for the plant’s remarkable anthelmintic activity and confirming its in vivo activity may lead to the development of a new anthelmintic for the treatment of hookworm and other PNs.