Novel types of receptor antagonists from the medicinal plant Garcinia Mangostana

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A crude methanolic extract of the fruit hull of Garcinia mangostana L. inhibited the contraction of the isolated rabbit aorta induced by histamine and serotonin. The extract has been fractionated by silica gel chromatography, monitoring the pharmacological activity to give active compounds. On the basis of physicochemical data, the active substances were identified as amangostin and γ-mangostin. To define the pharmacological properties of α-mangostin, the effect of α-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 α-mangostin acts as a selective and competitive histamine H1 receptor antagonist. The pharmacological actions of γ-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 γ-mangostin is a selective and competitive 5-HT2A receptor antagonist. It is of great interest that the structures of α-mangostin and γ-mangostin free from nitrogen atom are not resemble to the common structures of histamine and serotonin receptor antagonists. α-Mangostin and γ-mangostin may become novel types of lead compounds for histamine and serotonin receptor antagonists.
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