Mangosteen contains lead compounds for histamine & |
serotonin receptor antagonists |
1: Nippon Yakurigaku Zasshi. 1997 Oct;110 Suppl 1:153P-158P. Related Articles, Links [Novel types of receptor antagonists from the medicinal plant Garcinia mangostana] [Article in Japanese] Furukawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y. Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan. PMID: 9503424 [PubMed - indexed for MEDLINE] |
![]() On the basis of physicochemical data, the active substances were identified as alpha-mangostin and gamma-mangostin. To define the pharmacological properties of alpha-mangostin, the effect of alpha-mangostin on both histamine H1 and H2 receptors were examined by monitoring the mechanical responses of smooth muscles and measuring the radioligand binding to cultured vascular smooth muscle cells. The results suggest that alpha-mangostin acts as a selective and competitive histamine H1 receptor antagonist. The pharmacological actions of gamma-mangostin on 5-HT receptors were also investigated by using contractile response of vascular smooth muscle, platelet aggregation and radioligand binding studies. The results provide the evidence that gamma-mangostin is a selective and competitive 5-HT2A receptor antagonist. It is of great interest that the structures of alpha-mangostin and gamma-mangostin free from nitrogen atom are not resemble to the common structures of histamine and serotonin receptor antagonists. alpha-Mangostin and gamma-mangostin may become novel types of lead compounds for histamine and serotonin receptor antagonists. |