Inhibition of calcium and calmodulin-dependent phosphodiesterase activity in rats by capsaicin.

Abstract:

:Capsaicin, reported to elevate hormone sensitive lipase (HSL), is also found to inhibit the Ca++ and calmodulin-dependent cAMP phosphodiesterase (PDE) activity in adipose tissue of rats, fed high fat diet. The dependence of the enzyme activity on Ca++ and calmodulin in vitro, in control rats, is shown by its substantial lowering in the presence of EGTA and inhibition by trifluoperazine (TFP) (IC50 between 10-20 microM). This enzyme activity is also inhibited by both red pepper extract (80% inhibition with 50 microliter) and capsaicin (IC50 between 0.3-1 microM) in a dose dependent manner. Capsaicin has been found to inhibit Ca++-dependent PDE activity by 60% in the test rats. Enzyme inhibition in vivo, due to capsaicin, was overcome by addition of calmodulin to the assay system. Inclusion of fluphenazine or capsaicin in assay inhibited not only the calmodulin-restored enzyme activity from test rats but also that of control rats. These results suggest a possible mechanism for the stimulation of lipolytic activity by capsaicin in vivo.

authors

Salimath BP,Satyanarayana MN

doi

10.1016/0006-291x(87)91109-0

subject

Has Abstract

pub_date

1987-10-14 00:00:00

pages

292-9

issue

1

eissn

0006-291X

issn

1090-2104

pii

0006-291X(87)91109-0

journal_volume

148

pub_type

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