β-谷甾醇及其衍生物的溶解性特征及抗抑郁活性研究  

The solubility characteristics and antidepressant activity of β-sitosterol and its derivatives

作　　者：曹馨元 刘晓峰[1] 尹永霞 王波[1] 黄文华[1] CAO Xinyuan;LIU Xiaofeng;YIN Yongxia;WANG Bo;HUANG Wenhua(Department of Pharmacy,People’s Hospital of Ningxia Hui Autonomous Region,Yinchuan 750002,China;Chinese Medicine Material College,Jilin Agricultural University,Changchun 130118,China)

机构地区：[1]宁夏回族自治区人民医院药学部,宁夏银川750002 [2]吉林农业大学中药材学院,吉林长春130118

出　　处：《宁夏医学杂志》2021年第5期436-438,共3页Ningxia Medical Journal

基　　金：宁夏自然科学基金项目(2018AAC03273)。

摘　　要：目的β-谷甾醇(Sit)及其衍生物的溶解性特征及抗抑郁活性研究。方法分别测定Sit及其衍生物在溶剂石油醚、氯仿、二氯甲烷、乙酸乙酯、甲醇、乙醇、水中的溶解度及在正辛醇/水中的脂水分配系数;以瑞波西汀为阳性对照,考察Sit及其衍生物对小鼠悬尾应激和强迫游泳不动时间的影响。结果水杨酸-Sit酯(Sit-S)和山梨酸Sit酯(Sit-Sr)的溶解性和脂水分配系数(lg P)值均强于Sit及其他衍生物;Sit-S可显著缩短小鼠悬尾和强迫游泳不动时间(P<0.05)。结论对β-谷甾醇进行酯化衍生化处理可以增加其脂溶性,进一步提升其抗抑郁活性。ObjectiveTo study the solubility characteristics and antidepressant activity ofβ-sitosterol and its derivatives.MethodsThe solubility ofβ-sitosterol and its derivatives in petroleum ether,chloroform,dichloromethane,ethyl acetate,methanol,ethanol and lipid water distribution coefficient in N-octanol were determined respectively.Suspension and forced swimming test were applied to evaluate the antidepressant effects ofβ-sitosterol and its derivatives,and with reboxetine as the positive control.ResultsThe solubility and lgP values of sit-s and sit-sr were higher than those of Sit and other derivatives.Sit-s could significantly shorten the suspension time and forced swimming time(P<0.05).ConclusionEsterification ofβ-sitosterol can increase its lipid solubility and further improve its antidepressant activity.

关 键 词：Β-谷甾醇 衍生物 溶解性 抗抑郁 

分 类 号：R971[医药卫生—药品]