Feltenstein Matt W, Lambdin L Corinne, Ganzera M, Ranjith H, Dharmaratne W, Nanayakkara N P Dhammika, Khan Ikhlas A, Sufka Kenneth J
Department of Psychology, University of Mississippi, Oxford 38677, USA.
Phytother Res. 2003 Mar;17(3):210-6. doi: 10.1002/ptr.1107.
Piper methysticum extract (Kava kava) possesses anxiolytic properties. However, it is unknown whether these effects are best predicted by total kavalactone content or by one or more of its primary kavalactone constituents. Using the chick social separation-stress procedure as an anxiolytic bioassay, P. methysticum samples containing 12.8-100.0% total kavalactones (Exp. 1) and fractions containing 1-6 kavalactones of varying concentrations (0.1-67.5%; Exps. 2-3) were screened for activity and compared against a 5.0 mg/kg dose of chlordiazepoxide (CDP; Exp. 3). Eight-day-old chicks received IP injections of either vehicle or test compounds 30 min before being placed in the presence of two conspecifics or in isolation for a 3 min observation period. Dependent measures were ventral recumbency latency (sedation), distress vocalizations, and a measure of stress-induced analgesia (in Exps. 1 and 2 only). P. methysticum extract samples attenuated distress vocalizations in a concentration-dependent manner. The P. methysticum fraction that contained the highest concentration of dihydrokavain attenuated distress vocalizations in a manner equivalent to that of CDP. The extract samples and fractions that possessed anxiolytic properties did not possess the sedative properties found in CDP. Collectively, these findings suggest that dihydrokavain may be necessary and sufficient in mediating the anxiolytic properties of P. methysticum extract.
卡瓦胡椒提取物(卡瓦)具有抗焦虑特性。然而,尚不清楚这些作用是由总卡瓦内酯含量还是由其一种或多种主要卡瓦内酯成分能得到最佳预测。使用雏鸡社会隔离应激程序作为抗焦虑生物测定法,对总卡瓦内酯含量为12.8 - 100.0%的卡瓦胡椒样品(实验1)以及含有1 - 6种不同浓度(0.1 - 67.5%)卡瓦内酯的馏分(实验2 - 3)进行活性筛选,并与5.0 mg/kg剂量的氯氮卓(CDP;实验3)进行比较。8日龄雏鸡在与两只同种个体共处或单独隔离3分钟观察期前30分钟接受腹腔注射溶剂或测试化合物。相关测量指标为腹卧潜伏期(镇静作用)、痛苦叫声以及应激诱导镇痛指标(仅在实验1和2中)。卡瓦胡椒提取物样品以浓度依赖方式减轻痛苦叫声。含有最高浓度二氢卡瓦因的卡瓦胡椒馏分减轻痛苦叫声的方式与CDP相当。具有抗焦虑特性的提取物样品和馏分不具有CDP中发现的镇静特性。总体而言,这些发现表明二氢卡瓦因可能在介导卡瓦胡椒提取物的抗焦虑特性方面是必要且充分的。