The Search for Putative Hits in Combating Leishmaniasis:The Contributions of Natural Products Over the Last Decade  

作　　者：Patrick O.Sakyi Richard K.Amewu Robert N.O.A.Devine Emahi Ismaila Whelton A.Miller Samuel K.Kwofie 

机构地区：[1]Department of Chemistry,School of Physical and Mathematical Sciences,College of Basic and Applied Sciences,University of Ghana,P.O.BOX LG 56,Legon,Accra,Ghana [2]Department of Chemical Sciences,School of Sciences,University of Energy and Natural Resources,Box 214,Sunyani,Ghana [3]Department of Medicine,Loyola University Medical Center,Maywood,IL 60153,USA [4]Department of Molecular Pharmacology and Neuroscience,Loyola University Medical Center,Maywood,IL 60153,USA [5]Department of Chemical and Biomolecular Engineering,School of Engineering and Applied Science,University of Pennsylvania,Philadelphia,PA 19104,USA [6]Department of Biomedical Engineering,School of Engineering Sciences,College of Basic&Applied Sciences,University of Ghana,PMB LG 77,Legon,Accra,Ghana [7]Department of Biochemistry,Cell and Molecular Biology,West African Centre for Cell Biology of Infectious Pathogens,College of Basic and Applied Sciences,University of Ghana,P.O.Box LG 54,Accra,Ghana

出　　处：《Natural Products and Bioprospecting》2021年第5期489-544,共56页应用天然产物（英文）

摘　　要：Despite advancements in the areas of omics and chemoinformatics,potent novel biotherapeutic molecules with new modes of actions are needed for leishmaniasis.The socioeconomic burden of leishmaniasis remains alarming in endemic regions.Currently,reports from existing endemic areas such as Nepal,Iran,Brazil,India,Sudan and Afghanistan,as well as newly affected countries such as Peru,Bolivia and Somalia indicate concerns of chemoresistance to the classical antimonial treatment.As a result,effective antileishmanial agents which are safe and affordable are urgently needed.Natural products from both flora and fauna have contributed immensely to chemotherapeutics and serve as vital sources of new chemical agents.This review focuses on a systematic cross-sectional view of all characterized anti-leishmanial compounds from natural sources over the last decade.Furthermore,IC_(50)/EC_(50),cytotoxicity and suggested mechanisms of action of some of these natural products are provided.The natural product classification includes alkaloids,terpenes,terpenoids,and phenolics.The plethora of reported mechanisms involve calcium channel inhibition,immunomodulation and apoptosis.Making avail-able enriched data pertaining to bioactivity and mechanisms of natural products complement current efforts geared towards unraveling potent leishmanicides of therapeutic relevance.

关 键 词：CHEMOTHERAPEUTICS CHEMOINFORMATICS Natural products CYTOTOXICITY LEISHMANIASIS Phenotypic screening 

分 类 号：R285[医药卫生—中药学] R531.6[医药卫生—中医学]