Abstract
Emodin (1) is the major bioactive compound of several herb species, which belongs to anthraquinone class of compound. As a part of our drug discovery program, large quantities of emodin (1) was isolated from the roots of Rheum emodi and a library of novel emodin derivatives 2–24 were prepared to evaluate their in-vitro antimalarial activity, among them, compound 17, 18 and 20 showed potent antimalarial activity against chloroquine resistant strain PfK1with the IC50 of 2.28, 2.49 and 2.48 μM respectively with a high safety index.
Highlights
IntroductionAnthraquinones are widely distributed secondary metabolites of plants (aloe, cascara sagrada, senna and rhubarb), microbes, lichens and insects, which possess various biological activities [1,2,3]
Anthraquinones are widely distributed secondary metabolites of plants, microbes, lichens and insects, which possess various biological activities [1,2,3]
We have synthesized a library of novel emodin derivatives 2-24 and their antimalarial activity was evaluated
Summary
Anthraquinones are widely distributed secondary metabolites of plants (aloe, cascara sagrada, senna and rhubarb), microbes, lichens and insects, which possess various biological activities [1,2,3]. As a part of our drug discovery program on antimalarial agents from Indian medicinal plants, we isolated large quantities of anthraquinone i.e. emodin (1) from the roots of Rheum emodi and planned to carry out chemical transformation to improve its therapeutic application. Chemical transformation of bioactive compounds of medicinal herbs is one of the most common approaches in drug discovery to improve the therapeutic properties. Towards this goal, we have synthesized a library of novel emodin derivatives 2-24 and their antimalarial activity was evaluated
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