[Inhibitory activity of allene cholesteryl derivatives on the biosynthesis of ecdysone].
Prothoracic glands of the migratory locust Locusta migratoria during the postembryonnic development, are the biosynthetic source of ecdysone. The production of ecdysone by these glands in vitro has been used to evaluate the inhibitory activity of four cholesteryl derivatives with an allenic function on the side chain at C-22. These molecules were devised as potential inhibitors of hydroxylation at C-22 which is an obligate step in the biosynthesis of ecdysone. Three of the four molecules tested induce a marked depressory effect of the production of ecdysone. The effect of the compound with the higher activity was dose dependent and irreversible.
Roussel
J P
JP
Laboratoire de Biologie Générale, UA CNRS 672, Université Louis Pasteur, Strasbourg, France.
Burger
A
A
Hetru
C
C
D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004440:Ecdysone / Q000096:biosynthesis*; D006110:Grasshoppers / Q000378:metabolism*; D006900:Hydroxylation; D013897:Thoracic Duct / Q000187:drug effects / Q000378:metabolism*
D000924:Anticholesteremic Agents; D004440:Ecdysone
Etude de l'activité inhibitrice de dérivés allénques du cholestérol sur la biosynthèse de l'ecdysone.