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4-羟基苯甲醇衍生物及其镇静催眠活性。

4-Hydroxybenzyl alcohol derivatives and their sedative-hypnotic activities.

作者信息

Zhu Hong-Yan, Zhang Di, Zhang Qi, Zhao Yan, He Zhong-Mei, Gao Yu-Gang, Zhang Lian-Xue

机构信息

College of Chinese Medicinal Materials, Jilin Agricultural University Changchun 130118 Jilin China

The Fiftieth Middle School of Daqing Daqing 163000 China.

出版信息

RSC Adv. 2018 May 29;8(35):19539-19550. doi: 10.1039/c8ra01972j. eCollection 2018 May 25.

DOI:10.1039/c8ra01972j
PMID:35540981
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9080670/
Abstract

4-Hydroxybenzyl alcohol (HBA), one of the characteristic active components of , exhibits obvious effects on the human central nervous system. In order to acquire compounds with superior bioactivity, 10 derivatives of HBA were synthesized from HBA and carboxylic acids. The sedative effects of the 10 HBA derivatives were evaluated using a spontaneous locomotor activity test (SLT) in mice, and their hypnotic effects were determined to be synergistic with pentobarbital-induced sleep. The results showed that 4-hydroxybenzyl alcohol 3-furancarboxylic acid diester (2FHBA, 10 mg kg) exhibited the strongest sedative-hypnotic activity among HBA and its derivatives, and 2FHBA could reverse the insomnia caused by -chlorophenylalanine (CPA), flumazenil (FLU) and thiosemicarbazide (TSC). Meanwhile, 2FHBA and 5-hydroxytryptophan (5-HTP) showed a synergistic effect. The results suggested that 2FHBA might be a potential agent against insomnia, which might be mediated by the serotonergic and GABAergic systems.

摘要

4-羟基苯甲醇（HBA）是[具体物质]的特征性活性成分之一，对人体中枢神经系统具有明显作用。为了获得具有更优生物活性的化合物，以HBA和羧酸为原料合成了10种HBA衍生物。采用小鼠自主活动试验（SLT）对这10种HBA衍生物的镇静作用进行评估，确定它们的催眠作用与戊巴比妥诱导的睡眠具有协同性。结果表明，4-羟基苯甲醇3-呋喃羧酸二酯（2FHBA，10毫克/千克）在HBA及其衍生物中表现出最强的镇静催眠活性，且2FHBA可逆转由对氯苯丙氨酸（CPA）、氟马西尼（FLU）和氨基硫脲（TSC）引起的失眠。同时，2FHBA与5-羟色氨酸（5-HTP）表现出协同作用。结果提示，2FHBA可能是一种潜在的抗失眠药物，其作用可能由5-羟色胺能和γ-氨基丁酸能系统介导。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/5a2ab2c0f274/c8ra01972j-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/cdadfc6d6c30/c8ra01972j-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/203ec760d17b/c8ra01972j-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/28d78daaf103/c8ra01972j-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/ef249b2feaec/c8ra01972j-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/e28f0680e51c/c8ra01972j-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/5a2ab2c0f274/c8ra01972j-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/cdadfc6d6c30/c8ra01972j-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/203ec760d17b/c8ra01972j-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/28d78daaf103/c8ra01972j-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/ef249b2feaec/c8ra01972j-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/e28f0680e51c/c8ra01972j-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/149b/9080670/5a2ab2c0f274/c8ra01972j-f8.jpg

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