Abstract
A MeOH extract of Swertia chirata found to inhibit the catalytic activity of topoisomerase I of Leishmania donovani was subjected to fractionation to yield three secoiridoid glycosides: amarogentin (1), amaroswerin (2), and sweroside (3). Amarogentin is a potent inhibitor of type I DNA topoisomerase from Leishmania and exerts its effect by interaction with the enzyme, preventing binary complex formation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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DNA, Protozoan / chemistry
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DNA, Protozoan / drug effects
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Enzyme Inhibitors / isolation & purification*
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Enzyme Inhibitors / pharmacology*
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Glucosides / chemistry
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Glucosides / isolation & purification*
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Glucosides / pharmacology
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India
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Iridoids*
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Leishmania donovani / enzymology*
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Magnetic Resonance Spectroscopy
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Plants, Medicinal / chemistry*
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Pyrans / chemistry
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Pyrans / isolation & purification*
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Pyrans / pharmacology
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Topoisomerase I Inhibitors*
Substances
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DNA, Protozoan
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Enzyme Inhibitors
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Glucosides
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Iridoids
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Pyrans
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Topoisomerase I Inhibitors
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amarogentin