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Effects of the New Phosphodiesterase Inhibitor Griseolic Acid on Insulin Release in Rat Pancreatic Islets

Effects of the New Phosphodiesterase Inhibitor Griseolic Acid on Insulin Release in Rat Pancreatic Islets

N Hashimoto, H Makino, A Kanatsuka, M Yamazaki, S Yoshida

Arzneimittelforschung. 1990 Oct;40(10):1098-101.

PMID: 1705426

Abstract:

A new cyclic AMP phosphodiesterase inhibitor, griseolic acid (CAS 79030-08-3), in a dose-dependent manner increased insulin release and cyclic AMP level in rat pancreatic islets in the presence of 5.5 mmol/l glucose. Griseolic acid (0.26 mmol/l) or 3-isobutyl-1-methylxanthine (IBMX) (1 mmol/l) enhanced insulin release and cyclic AMP level both in the presence of 5.5 and 16.7 mmol/l glucose (no significant difference). In perifusion system, 45Ca++ efflux and insulin release showed a monophasic increase when the islets were exposed to 1.3 mmol/l griseolic acid or 1 mmol/l IBMX in the presence of 5.5 mmol/l glucose (no significant difference). In a cell-free system, griseolic acid had a stronger inhibitory effect on cyclic AMP phosphodiesterase activity than IBMX, has a stimulatory effect on insulin release through an increase of cyclic AMP by inhibiting phosphodiesterase in pancreatic islets, but it might not cross the plasma membrane easily.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP28822584	3-Isobutyl-1-methylxanthine - CAS 28822-58-4		28822-58-4	Price

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