Pharmacological profile of apigenin, a flavonoid isolated from Matricaria chamomilla

Dried flowers of Matricaria chamomilla L. are largely used to provide sedat ive as well as spasmolytic effects. In the present study, we examined in pa rticular the pharmacological property of a fraction isolated from a methano lic extract of M. chamomilla, which was identified by HPLC-MS-MS analysis a s apigenin. By radioreceptor binding assays, we demonstrated the ability of the flavone to displace a specific radioligand, [H-3]Ro 15-1788, from the central benzodiazepine binding site. Electrophysiological studies performed on cultured cerebellar granule cells showed that apigenin reduced GABA (ga mma-aminobutyric acid)-activated Cl(-)currents in a dose-dependent fashion. The effect was blocked by co-application of Ro 15-1788, a specific benzodi azepine receptor antagonist. Accordingly, apigenin reduced the latency in t he onset of picrotoxin-induced convulsions. Moreover, apigenin injected i.p . in rats reduced locomotor activity, but did not demonstrate anxiolytic, m yorelaxant, or anticonvulsant activities. The present results seem to sugge st that the inhibitory activity of apigenin on locomotor behaviour in rats cannot be ascribed to an interaction with GABA(A)- benzodiazepine receptor but to other neurotransmission systems, since it is not blocked by Ro 15-17 88. BIOCHEM PHARMACOL 59;11:1387-1394, 2000. (C) 2000 Elsevier Science Inc.