从远志中分离鉴定出一种多巴胺受体活性化合物

ISOLATION AND IDENTIFICATION OF TETRAHYDRO-COLUMBAMINE AS A DOPAMINE RECEPTOR LIGAND FROM POLYGALA TENUIFOLIA WILLD

摘要: 从中药远志中提出一种多巴胺受体的配基,四氢非州防己胺。此化合物在体外可抑制³HSCH23390和³H螺哌隆与大鼠纹状体膜的结合,IC₅₀值分别为0.75±0.08μmol·L^-1和0.92±0.10μmol·L^-1。它在体外还能抑制³H哌唑嗪和大鼠脑皮质细胞膜结合(IC₅₀值为46μmol·L^-1),但不能改变³HQNB及³Hmuscimol对膜的结合。Scatchandplot分析显示此化合物对³HSCH23390和³H螺哌隆与膜结合的抑制作用是通过竞争性与非竞争性混合机制而实现的。

Abstract: The isolation and purification of a dopamine receptor ligand ,tetrahydro-columbamine from Polygala tenuifolia Willd is described. Tetrahydrocolumbamine was shown to inhibitthe binding of³H-SCH23390 and³H-spiroperidol to rat striatum membranes in vitro with IC₅₀values of 0.75 ± 0.08μmol·L^-1 and 0.92 ± 0. 10μmol·L^-1, respectively.The compoundinhibited the binding of³H-prazosin(IC₅₀ value of 46μmol·L^-1),while it did not change thebinding of the ligands,³H-QNB and³H-muscimol to rat cortex in vitro. Scatchard plot analysisshowed a mixture of competitive and non-competitive inhibition by the compound on both³H-SCH23390 and³H-spiroperidol binding to membranes from rat striatum.