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皮肤提取物通过抑制钠/氢ATP酶的抗疟功效。

Antimalarial efficacy of skin extract via inhibition of Na/H ATPase.

作者信息

Bagwe Akshay D, D'Souza Roshan C, Sharma Bharatbhushan B

机构信息

Department of Zoology, Sophia College for Women (Autonomous), Mumbai, Maharashtra 400 026 India.

Department of Zoology, KET's V. G. Vaze College of Arts, Science and Commerce (Autonomous), Mumbai, Maharashtra 400 081 India.

出版信息

J Parasit Dis. 2024 Dec;48(4):831-848. doi: 10.1007/s12639-024-01716-9. Epub 2024 Aug 2.

DOI:10.1007/s12639-024-01716-9
PMID:39493482
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11527857/
Abstract

UNLABELLED

Malaria remains a major health issue worldwide that affects many people, particularly in developing nations. Since, the malarial parasite has developed resistance against nearly every antimalarial drug now in use, it is imperative to search for novel antimalarial medications. Toxins produced by skin glands of toads have been shown to possess antiparasitic properties against a variety of protozoan parasites because of the bufadienolides they contain. Even though several studies have been conducted to show that toad skin secretions have antimalarial properties, very little information is known about the precise mechanism by which they work against infection. Thus, the goal of this study was to evaluate the antiplasmodial activity of crude skin extracts from Common Asian Toads, , of different sizes and illustrate how they work against 3D7 cells. The findings demonstrated a negative correlation between the toad size and percent yield of the extracts. HPTLC and UPLC-MS/MS analysis of the extracts exhibited varied composition of bufadienolides depending on the size of the animal. The extract obtained from small toads containing resibufagin and marinobufagin lactate demonstrated highest antiplasmodial activity and showed lowest cytotoxicity on peripheral blood mononuclear cells. It was discovered that the extract was effective against the trophozoite stage of the parasite. The extract was reported to inhibit Na/H ATPase of by binding to sodium-enzyme complex at ATP binding site. The study offers baseline data that can be used to assess the antimalarial potential of individual components in the skin extract derived from small toads.

SUPPLEMENTARY INFORMATION

The online version contains supplementary material available at 10.1007/s12639-024-01716-9.

摘要

未标注

疟疾仍然是一个影响全球许多人的重大健康问题,尤其是在发展中国家。由于疟原虫已对目前使用的几乎每种抗疟药物产生耐药性,因此寻找新型抗疟药物势在必行。蟾蜍皮肤腺体产生的毒素因其所含的蟾蜍二烯羟酸内酯而对多种原生动物寄生虫具有抗寄生虫特性。尽管已经进行了多项研究表明蟾蜍皮肤分泌物具有抗疟特性,但关于它们对抗感染的确切作用机制知之甚少。因此,本研究的目的是评估不同大小的亚洲普通蟾蜍粗皮肤提取物的抗疟活性,并说明它们如何作用于3D7细胞。研究结果表明蟾蜍大小与提取物的百分产率呈负相关。提取物的高效薄层色谱(HPTLC)和超高效液相色谱-串联质谱(UPLC-MS/MS)分析显示,取决于动物大小,蟾蜍二烯羟酸内酯的组成各不相同。从小蟾蜍中获得的含有脂蟾毒配基和乳酸海蟾蜍精的提取物表现出最高的抗疟活性,并且对外周血单核细胞的细胞毒性最低。发现该提取物对寄生虫的滋养体阶段有效。据报道,该提取物通过在ATP结合位点与钠酶复合物结合来抑制疟原虫的钠/氢ATP酶。该研究提供了基线数据,可用于评估从小蟾蜍皮肤提取物中各成分的抗疟潜力。

补充信息

在线版本包含可在10.1007/s12639-024-01716-9获取的补充材料。

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