Antileishmanial Evaluation of the Leaf Latex of , Aloin A/B, and Its Semisynthetic Derivatives against Two Species.

Evid Based Complement Alternat Med

Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, College of Health Sciences, Addis Ababa University, P.O. Box 1176, Addis Ababa, Ethiopia.

Published: February 2019

The currently available antileishmanial drugs are either toxic or too expensive for routine use in developing countries where the disease is most common. Local people in the Somalia region of Ethiopia use the leaves of Todaro for the treatment of malaria, jaundice, and skin diseases. In our ongoing search for new, efficient, and safe antileishmanial drugs, we investigated the leaf latex of and its acid-hydrolyzed product aloin A/B (), as well as the semisynthesized derivatives of aloin A/B, namely, aloe-emodin () and rhein () against promastigotes and axenically cultured amastigotes of and clinical isolates. Activity study was carried out based on the fluorescence characteristic of resazurin added to drug-treated cultures. Oxidative hydrolysis of aloin A/B by ferric chloride and concentrated hydrochloric acid afforded aloe-emodin (), which was further oxidized using sodium nitrite and concentrated sulfuric acid to furnish rhein (). Cytotoxicity study of test substances was performed against human cell line Alamar Blue and cell viability was measured fluorometrically. The test compounds showed lower activity (IC = 6.7 to 12.1 M for promastigotes and IC = 3.6 to 10.2 M for axenic amastigotes) than the reference drug amphotericin B (IC = 1.3 to 2.7 M). However, amphotericin B (LC = 11.1 M) was much more toxic than the test compounds (LC = 369.2 - 611.6 M) towards human monocytic cell line (THP-1) despite its efficiency. As demonstrated in the current study, high selectivity indices (SIs) of the test compounds represent a remarkable advantage over the reference drug and highlight their potential use as templates for further development of safe leishmanicidal drugs.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409032PMC
http://dx.doi.org/10.1155/2019/4736181DOI Listing

Publication Analysis

Top Keywords

aloin a/b
16
test compounds
12
leaf latex
8
antileishmanial drugs
8
reference drug
8
antileishmanial evaluation
4
evaluation leaf
4
aloin
4
latex aloin
4
a/b
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!