摘要
L-薄荷醇(LM)是薄荷中含量最高的有效成分,属于单环萜烯,具有芳香气味,LM具有疏肝解郁,上清头目的功效,因此认为LM具有抗抑郁作用。试验通过LM与有机酸(苯甲酸,α-硫辛酸,糠酸,油酸)的酯化合成了4种化合物,经过NMR鉴定其化学结构。采用强迫游泳试验(FST)筛选LM及其衍生物抗抑郁活性,发现苯甲酸薄荷酯(LM 1)的抗抑郁效果最佳。其次有效剂量(1 mg/kg)联合氟西汀[5 mg/kg,腹腔注射给药(i.p.)],噻奈普汀(15 mg/kg,i.p.)和瑞波西汀(2.5 mg/kg,i.p.)可显著缩短累积不动时间(P<0.01)。LM1在剂量为30 mg/kg可极显著缩短游泳不动时间(P<0.001),使用荷包牡丹碱(竞争性γ-氨基丁酸拮抗剂,4 mg/kg,i.p.),N-甲基-D-天冬氨酸(NMDA,谷氨酸的激动剂,75 mg/kg),昂丹司琼(高选择性5-HT3受体拮抗剂,8 mg/kg,i.p.)和氟哌啶醇(非选择性D2受体拮抗剂,0.2 mg/kg,i.p.)可逆转LM1[30 mg/kg,灌胃给药(i.g.)]的抗抑郁作用。结果表明:LM1是通过作用于谷氨酸能,γ-氨基丁酸能,5-羟色胺能和多巴胺能介导发挥的抗抑郁作用。
L-Menthol(LM)is the highest active ingredient in peppermint,belonging to monocyclic terpenes with aromatic odor.LM has sparse,supernatant purpose of the head.Therefore,we believe that LM has anti-depressant effect.In this experiment,four compounds were synthesized by esterification of LM with organic acids(benzoic acid,α-lipoic acid,furoic acid and oleic acid).Its chemical structure was identified by NMR.Forced swimming test(FST)was used to screen antidepressant activities of LM and its derivatives,and found that antidepressant effect of menthyl benzoate(LM1)was the best.Its sub-effective dose(1 mg/kg)combined with Fluoxetine(5 mg/kg,i.p.),tianeptine(15 mg/kg,i.p.)and reboxetine(2.5 mg/kg,i.p.)can significantly shorten immobility time in FST(P<0.01).LM1 significantly reduces swimming immobility at a dose of 30 mg/kg(P<0.001).Using bicuculline(a competitiveγ-aminobutyric acid antagonist,4 mg/kg,i.p.),NMethyl-D-aspartic acid(NMDA,glutamate agonist,75 mg/kg,i.p.),ondansetron(a highly selective 5-HT3 receptor antagonist,8 mg/kg,i.p).and haloperidol(Non-selective D2 receptor antagonist,0.2 mg/kg,i.p.)can reverse antidepressant effect of LM1(30 mg/kg,i.g.).The results show that LM1 acts on glutamatergic,γ-aminobutyric acid,serotonergic and dopamine-mediated antidepressant effects.
作者
姜圆圆
赵岩
王士杰
郜玉钢
杨鹤
张连学
JIANG Yuanyuan;ZHAO Yan;WANG Shijie;GAO Yugang;YANG He;ZHANG Lianxue(College of Chinese Medicinal Materials,Jilin Agricultural University,Changchun 130118,China;College of Traditional Chinese Medicine,Jilin Agricultural Science and Technology University,Jilin 132101,China)
出处
《吉林农业大学学报》
CAS
CSCD
北大核心
2020年第3期300-308,共9页
Journal of Jilin Agricultural University
基金
国家农业部公益性行业科研专项(201303111)
吉林省科技发展计划项目(20150204049YY,20140204013YY,20140311050YY)
