Amarogentin, a naturally occurring secoiridoid glycoside and a newly recognized inhibitor of topoisomerase I from Leishmania donovani.
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.
Ray
S
S
Indian Institute of Chemical Biology, Calcutta, India.
Majumder
H K
HK
Chakravarty
A K
AK
Mukhopadhyay
S
S
Gil
R R
RR
Cordell
G A
GA
D000818:Animals; D016054:DNA, Protozoan / Q000737:chemistry / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology*; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D007194:India; D039823:Iridoids; D007893:Leishmania donovani / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D010946:Plants, Medicinal / Q000737:chemistry*; D011714:Pyrans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D059004:Topoisomerase I Inhibitors
D016054:DNA, Protozoan; D004791:Enzyme Inhibitors; D005960:Glucosides; D039823:Iridoids; D011714:Pyrans; D059004:Topoisomerase I Inhibitors; C102609:amarogentin