Hesperetin was able to inhibit both epinephrine- and theophylline-indu
ced lipolysis in rat adipocytes. At concentrations of 125 muM and 250
muM, it could augment the inhibitory effect of low insulin concentrati
on (17 muU/2ml) on epinephrine-induced lipolysis. The basal cyclic AMP
levels and phosphodiesterase activities in intact adipocytes were una
ltered by hesperetin. The antilipolytic action of hesperetin in adenos
ine deaminase pretreated adipocytes was abolished. Hesperetin could on
ly prevent lipolysis but not reverse the initial lipolytic activity st
imulated through the adenosine deaminase pretreatment of the adipocyte
s. In pertussis or cholera toxin (PT or CT) pretreated adipocytes, the
antilipolytic action of hesperetin was unaffected. From the data obta
ined it is possible to conclude that the antilipolytic action of hespe
retin is not mediated through the inhibition of cyclic AMP level nor t
hrough CT- or PT-sensitive G proteins. However, the involvement of hes
peretin in preventing the accessibility of cellular receptors to the a
ctions of lipolytic agents may be implicated.