Asset Details
Do you wish to reserve the book?
Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library
Do you wish to request the book?
Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library
2025
Overview
Visceral leishmaniasis caused by Leishmania donovani is one of the major neglected tropical diseases attributable to parasitic protozoa. In the absence of an effective vaccine, chemotherapy remains the only available therapeutic option. However, current treatments rely on a limited number of drugs that are largely obsolete, highly toxic or require intravenous administration, and their extensive use has led to the emergence of drug resistance. Consequently, the discovery of new antileishmanial agents is an urgent priority. In this study, a commercial library of 449 alkaloids in a high-throughput screening format was evaluated against both axenic bone marrow-derived amastigotes and intramacrophagic amastigotes from mice infected with L. donovani IRFP, a strain engineered to emit infrared fluorescence in its viable form. Six isoquinoline-type alkaloids showed the best antileishmanial efficacy against intramacrophagic amastigotes while exhibiting minimal cytotoxicity toward RAW 264.7 and HepG2 cell lines, with a promising selective index higher than four, and good mouse intestinal tolerance in mouse organoids. Among these compounds, the protoberberine scaffold emerged as the most promising candidate for further drug development.
Publisher
MDPI AG,Multidisciplinary Digital Publishing Institute (MDPI)
Subject
/ Animals
/ Antiprotozoal Agents - chemistry
/ Antiprotozoal Agents - pharmacology
/ Cancer
/ High-Throughput Screening Assays
/ Humans
/ Leishmania donovani - drug effects
/ Leishmaniasis, Visceral - drug therapy
/ Leishmaniasis, Visceral - parasitology
/ Mice
/ phenotypic high-throughput screening
/ Small Molecule Libraries - chemistry
/ Small Molecule Libraries - pharmacology
/ Toxicity
/ Vaccines
