Laboratory of Parasitology, Butantan Institute, São Paulo 05503-000, SP CEP, Brazil.
Biochemistry Department, Chemistry Institute, USP-Universidade de São Paulo, São Paulo 05508-00, SP, Brazil.
Mar Drugs. 2022 Jan 29;20(2):111. doi: 10.3390/md20020111.
Schistosomiasis has been controlled for more than 40 years with a single drug, praziquantel, and only one molluscicide, niclosamide, raising concern of the possibility of the emergence of resistant strains. However, the molecular targets for both agents are thus far unknown. Consequently, the search for lead compounds from natural sources has been encouraged due to their diverse structure and function. Our search for natural compounds with potential use in schistosomiasis control led to the identification of an algal species, , whose extracts demonstrated significant activity toward both parasites and their intermediate host snails . In the present study, three seaweed-derived halogenated sesquiterpenes, (-)-elatol, rogiolol, and obtusol are proposed as potential lead compounds for the development of anthelminthic drugs for the treatment of and pesticides for the environmental control of schistosomiasis. The three compounds were screened for their antischistosomal and molluscicidal activities. The screening revealed that rogiolol exhibits significant activity toward the survival of adult worms, and that all three compounds showed activity against cercariae and embryos. Biomonitored fractioning of extracts indicated elatol as the most active compound toward cercariae larvae and snail embryos.
血吸虫病在过去 40 多年里一直通过一种药物吡喹酮和唯一一种杀螺剂氯硝柳胺进行控制，这引发了人们对可能出现耐药菌株的担忧。然而，到目前为止，这两种药物的分子靶点还不清楚。因此，由于天然产物结构和功能的多样性，鼓励从天然来源寻找先导化合物。我们寻找具有控制血吸虫病潜力的天然化合物，发现了一种藻类物种，其提取物对寄生虫及其中间宿主蜗牛均表现出显著的活性。在本研究中，三种源自海藻的卤代倍半萜烯(-)-艾洛醇、罗乔醇和 obtusol 被提议作为开发抗蠕虫药物治疗血吸虫病和杀螺剂控制血吸虫病的潜在先导化合物。对这三种化合物进行了抗血吸虫和杀螺活性筛选。筛选结果表明，罗乔醇对成虫的存活具有显著的活性，而且这三种化合物对尾蚴和 胚胎均具有活性。生物监测的提取物分馏表明，艾洛醇对尾蚴幼虫和蜗牛胚胎的活性最高。
