三肽 Phe-Trp-Leu-NH2 作为 TSPO 的假定内源配体：分子建模、合成和药理活性

IF 1.8 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Mendeleev Communications Pub Date : 2024-09-01 DOI:10.1016/j.mencom.2024.09.018

Olga A. Deeva , Andrey S. Pantileev , Oxana Yu. Kravtsova , Sergey V. Nikolaev , Nikolay A. Zefirov , Polina Yu. Povarnina , Tatiana A. Antipova , Tatiana A. Gudasheva , Vladimir L. Dorofeev

{"title":"三肽 Phe-Trp-Leu-NH2 作为 TSPO 的假定内源配体：分子建模、合成和药理活性","authors":"Olga A. Deeva , Andrey S. Pantileev , Oxana Yu. Kravtsova , Sergey V. Nikolaev , Nikolay A. Zefirov , Polina Yu. Povarnina , Tatiana A. Antipova , Tatiana A. Gudasheva , Vladimir L. Dorofeev","doi":"10.1016/j.mencom.2024.09.018","DOIUrl":null,"url":null,"abstract":"<div><div>The putative endogenous tripeptide ligand of the translocator protein (TSPO) l-phenylalanyl-l-tryptophanyl-l-leucine amide was obtained using the drug-based peptide design strategy and molecular modeling. This tripeptide demonstrated anxiolytic activity in the elevated plus-maze test and antidepressant-like activity in the forced swimming test in BALB/c mice at the doses of 10 mg kg<sup>−1</sup> (<em>i.p</em>.) and also showed neuroprotective activity in the concentration range of 10<sup>−5</sup>–10<sup>−7</sup> m <em>in vitro</em> under conditions of oxidative stress using HT-22 neuronal cell line.</div></div>","PeriodicalId":18542,"journal":{"name":"Mendeleev Communications","volume":"34 5","pages":"Pages 682-684"},"PeriodicalIF":1.8000,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Tripeptide Phe-Trp-Leu-NH2 as a putative endogenous ligand of TSPO: molecular modeling, synthesis and pharmacological activity\",\"authors\":\"Olga A. Deeva , Andrey S. Pantileev , Oxana Yu. Kravtsova , Sergey V. Nikolaev , Nikolay A. Zefirov , Polina Yu. Povarnina , Tatiana A. Antipova , Tatiana A. Gudasheva , Vladimir L. Dorofeev\",\"doi\":\"10.1016/j.mencom.2024.09.018\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>The putative endogenous tripeptide ligand of the translocator protein (TSPO) l-phenylalanyl-l-tryptophanyl-l-leucine amide was obtained using the drug-based peptide design strategy and molecular modeling. This tripeptide demonstrated anxiolytic activity in the elevated plus-maze test and antidepressant-like activity in the forced swimming test in BALB/c mice at the doses of 10 mg kg<sup>−1</sup> (<em>i.p</em>.) and also showed neuroprotective activity in the concentration range of 10<sup>−5</sup>–10<sup>−7</sup> m <em>in vitro</em> under conditions of oxidative stress using HT-22 neuronal cell line.</div></div>\",\"PeriodicalId\":18542,\"journal\":{\"name\":\"Mendeleev Communications\",\"volume\":\"34 5\",\"pages\":\"Pages 682-684\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2024-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Mendeleev Communications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0959943624002578\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Mendeleev Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0959943624002578","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}

引用次数: 0

摘要

通过基于药物的多肽设计策略和分子建模，获得了转运蛋白（TSPO）的推定内源性三肽配体-l-苯丙氨酰-l-色氨酰-l-亮氨酸酰胺。这种三肽在高架迷宫试验中表现出抗焦虑活性，在BALB/c小鼠强迫游泳试验中表现出抗抑郁样活性，剂量为10 mg kg-1（i.p.）；在体外氧化应激条件下，利用HT-22神经细胞系，在10-5-10-7 m浓度范围内表现出神经保护活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Tripeptide Phe-Trp-Leu-NH2 as a putative endogenous ligand of TSPO: molecular modeling, synthesis and pharmacological activity

查看原文本刊更多论文

Tripeptide Phe-Trp-Leu-NH2 as a putative endogenous ligand of TSPO: molecular modeling, synthesis and pharmacological activity

The putative endogenous tripeptide ligand of the translocator protein (TSPO) l-phenylalanyl-l-tryptophanyl-l-leucine amide was obtained using the drug-based peptide design strategy and molecular modeling. This tripeptide demonstrated anxiolytic activity in the elevated plus-maze test and antidepressant-like activity in the forced swimming test in BALB/c mice at the doses of 10 mg kg⁻¹ (i.p.) and also showed neuroprotective activity in the concentration range of 10⁻⁵–10⁻⁷ m in vitro under conditions of oxidative stress using HT-22 neuronal cell line.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Mendeleev Communications 化学-化学综合

CiteScore

3.00

自引率

21.10%

发文量

226

审稿时长

4-8 weeks

期刊介绍： Mendeleev Communications is the journal of the Russian Academy of Sciences, launched jointly by the Academy of Sciences of the USSR and the Royal Society of Chemistry (United Kingdom) in 1991. Starting from 1st January 2007, Elsevier is the new publishing partner of Mendeleev Communications. Mendeleev Communications publishes short communications in chemistry. The journal primarily features papers from the Russian Federation and the other states of the former USSR. However, it also includes papers by authors from other parts of the world. Mendeleev Communications is not a translated journal, but instead is published directly in English. The International Editorial Board is composed of eminent scientists who provide advice on refereeing policy.