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In vitro studies on the mode of action of quassinoids with activity against chloroquine-resistant Plasmodium falciparum.

Abstract：

:Using the incorporation of [3H]isoleucine or [3H]hypoxanthine into acid-insoluble products as indices of protein- and nucleic acid-synthetic activity, respectively, it was shown that seven plant-derived quassinoids with differing chemical substitutions all inhibited protein synthesis more rapidly than nucleic acid synthesis in human erythrocytes infected with Plasmodium falciparum, in vitro. Five quassinoids (ailanthinone, bruceantin, bruceine B, glaucarubinone and holacanthone) were effective within 30 min at doses 10 times their 48 hr in vitro IC50 values. Chaparrin and glaucarubol differed in that they did not inhibit protein synthesis during the time course of these experiments when applied at 10 times their in vitro IC50 values. When these compounds were used at 209 and 114 times their respective IC50 values, their observed effects were identical to those of the other quassinoids studied. The time (t50) at which nucleic acid synthesis was reduced to 50% of control was directly proportional to the t50 for protein synthesis, suggesting that failure of nucleic acid synthesis is a consequence of inhibition of protein synthesis. It is concluded that in the malaria parasite, as in eukaryote models, quassinoids are rapid and potent inhibitors of protein synthesis, and that this is most likely due to effects upon the ribosome, rather than upon nucleic acid metabolism.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Kirby GC,O'Neill MJ,Phillipson JD,Warhurst DC

doi

10.1016/0006-2952(89)90644-8

subject

Has Abstract

pub_date

1989-12-15 00:00:00

pages

4367-74

issue

24

eissn

0006-2952

issn

1873-2968

pii

0006-2952(89)90644-8

journal_volume

38

pub_type

杂志文章

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