咖啡酸异戊酯是一种治疗利什曼病的有效药物:硅学和体内研究

IF 3.6 Q2 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Current Research in Biotechnology Pub Date : 2024-01-01 DOI:10.1016/j.crbiot.2024.100209
Wanessa S. Mota , Simone S.C. Oliveira , Matheus M. Pereira , Damião P. Souza , Mayara Castro , Pollyanna S. Gomes , Herbert L.M. Guedes , Vinícius F. Souza , André L.S. Santos , Ricardo L.C. Albuquerque-Junior , Juliana C. Cardoso , Cristina Blanco-Llamero , Sona Jain , Eliana B. Souto , Patrícia Severino
{"title":"咖啡酸异戊酯是一种治疗利什曼病的有效药物:硅学和体内研究","authors":"Wanessa S. Mota ,&nbsp;Simone S.C. Oliveira ,&nbsp;Matheus M. Pereira ,&nbsp;Damião P. Souza ,&nbsp;Mayara Castro ,&nbsp;Pollyanna S. Gomes ,&nbsp;Herbert L.M. Guedes ,&nbsp;Vinícius F. Souza ,&nbsp;André L.S. Santos ,&nbsp;Ricardo L.C. Albuquerque-Junior ,&nbsp;Juliana C. Cardoso ,&nbsp;Cristina Blanco-Llamero ,&nbsp;Sona Jain ,&nbsp;Eliana B. Souto ,&nbsp;Patrícia Severino","doi":"10.1016/j.crbiot.2024.100209","DOIUrl":null,"url":null,"abstract":"<div><p>Leishmaniasis is recognised as the second largest parasitic disease worldwide and yet a neglected disease. The current pharmacological treatments are associated with significant challenges, including high toxicity, high cost and parasitic resistance. Considering the potential of isopentyl caffeate (ICaf) as an anti-leishmanial agent, the present work evaluated the <em>in vivo</em> toxicity of ICaf and the absorption, distribution, metabolism, and excretion (ADME) properties <em>in silico</em>, aiming at the treatment of <em>Leishmania amazonensis</em>. For the <em>in vivo</em> toxicity testing, Swiss mice (<em>Mus musculus</em>) were treated with a single dose of ICaf. During the 14-day evaluation period, the animals underwent assessments including hippocratic screening, weight measurement, as well as histological and hematological evaluations. Analysis of ADME properties of ICaf was conducted to evaluate its pharmacokinetic characteristics and bioavailability. Characteristics, such as molar refractivity through Lipinski's Rule of Five, were identified. The <em>in silico</em> results showed that ICaf is considered to have good oral bioavailability and has potential to be considered as a new drug. From the <em>in vivo</em> toxicity testing, none of the evaluated parameters revealed toxicity of ICaf to the animals when treated intraperitoneally. The <em>in vivo</em> treatment reduced the lesion and the parasite load at the tested doses, corroborating the assumption that ICaf may be a potential pharmacological alternative against <em>L. amazonensis</em>.</p></div>","PeriodicalId":52676,"journal":{"name":"Current Research in Biotechnology","volume":null,"pages":null},"PeriodicalIF":3.6000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590262824000352/pdfft?md5=34b6b52f6490ccae56027b2ac7ff33f1&pid=1-s2.0-S2590262824000352-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Isopentyl caffeate as a promising drug for the treatment of leishmaniasis: An in silico and in vivo study\",\"authors\":\"Wanessa S. Mota ,&nbsp;Simone S.C. Oliveira ,&nbsp;Matheus M. Pereira ,&nbsp;Damião P. Souza ,&nbsp;Mayara Castro ,&nbsp;Pollyanna S. Gomes ,&nbsp;Herbert L.M. Guedes ,&nbsp;Vinícius F. Souza ,&nbsp;André L.S. Santos ,&nbsp;Ricardo L.C. Albuquerque-Junior ,&nbsp;Juliana C. Cardoso ,&nbsp;Cristina Blanco-Llamero ,&nbsp;Sona Jain ,&nbsp;Eliana B. Souto ,&nbsp;Patrícia Severino\",\"doi\":\"10.1016/j.crbiot.2024.100209\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Leishmaniasis is recognised as the second largest parasitic disease worldwide and yet a neglected disease. The current pharmacological treatments are associated with significant challenges, including high toxicity, high cost and parasitic resistance. Considering the potential of isopentyl caffeate (ICaf) as an anti-leishmanial agent, the present work evaluated the <em>in vivo</em> toxicity of ICaf and the absorption, distribution, metabolism, and excretion (ADME) properties <em>in silico</em>, aiming at the treatment of <em>Leishmania amazonensis</em>. For the <em>in vivo</em> toxicity testing, Swiss mice (<em>Mus musculus</em>) were treated with a single dose of ICaf. During the 14-day evaluation period, the animals underwent assessments including hippocratic screening, weight measurement, as well as histological and hematological evaluations. Analysis of ADME properties of ICaf was conducted to evaluate its pharmacokinetic characteristics and bioavailability. Characteristics, such as molar refractivity through Lipinski's Rule of Five, were identified. The <em>in silico</em> results showed that ICaf is considered to have good oral bioavailability and has potential to be considered as a new drug. From the <em>in vivo</em> toxicity testing, none of the evaluated parameters revealed toxicity of ICaf to the animals when treated intraperitoneally. The <em>in vivo</em> treatment reduced the lesion and the parasite load at the tested doses, corroborating the assumption that ICaf may be a potential pharmacological alternative against <em>L. amazonensis</em>.</p></div>\",\"PeriodicalId\":52676,\"journal\":{\"name\":\"Current Research in Biotechnology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S2590262824000352/pdfft?md5=34b6b52f6490ccae56027b2ac7ff33f1&pid=1-s2.0-S2590262824000352-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Research in Biotechnology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2590262824000352\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOTECHNOLOGY & APPLIED MICROBIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Research in Biotechnology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2590262824000352","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOTECHNOLOGY & APPLIED MICROBIOLOGY","Score":null,"Total":0}
引用次数: 0

摘要

利什曼病被认为是全球第二大寄生虫病,但也是一种被忽视的疾病。目前的药物治疗面临着巨大挑战,包括毒性大、成本高和寄生虫抗药性。考虑到咖啡酸异戊酯(ICaf)作为抗利什曼病药的潜力,本研究对 ICaf 的体内毒性以及吸收、分布、代谢和排泄(ADME)特性进行了硅学评估,旨在治疗亚马逊利什曼病。在体内毒性测试中,瑞士小鼠(Mus musculus)接受了单剂量 ICaf 的治疗。在为期 14 天的评估期间,对动物进行了海马筛选、体重测量以及组织学和血液学评估。对 ICaf 的 ADME 特性进行了分析,以评估其药代动力学特性和生物利用度。通过利宾斯基五法则确定了摩尔折射率等特性。硅学结果表明,ICaf 具有良好的口服生物利用度,有潜力被视为一种新药。从体内毒性测试来看,经腹腔注射治疗后,ICaf 的各项评估参数均未显示出对动物的毒性。在测试剂量下,体内治疗可减少病变和寄生虫量,这证实了 ICaf 可能是抗击 L. amazonensis 的潜在药理替代品的假设。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

摘要图片

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Isopentyl caffeate as a promising drug for the treatment of leishmaniasis: An in silico and in vivo study

Leishmaniasis is recognised as the second largest parasitic disease worldwide and yet a neglected disease. The current pharmacological treatments are associated with significant challenges, including high toxicity, high cost and parasitic resistance. Considering the potential of isopentyl caffeate (ICaf) as an anti-leishmanial agent, the present work evaluated the in vivo toxicity of ICaf and the absorption, distribution, metabolism, and excretion (ADME) properties in silico, aiming at the treatment of Leishmania amazonensis. For the in vivo toxicity testing, Swiss mice (Mus musculus) were treated with a single dose of ICaf. During the 14-day evaluation period, the animals underwent assessments including hippocratic screening, weight measurement, as well as histological and hematological evaluations. Analysis of ADME properties of ICaf was conducted to evaluate its pharmacokinetic characteristics and bioavailability. Characteristics, such as molar refractivity through Lipinski's Rule of Five, were identified. The in silico results showed that ICaf is considered to have good oral bioavailability and has potential to be considered as a new drug. From the in vivo toxicity testing, none of the evaluated parameters revealed toxicity of ICaf to the animals when treated intraperitoneally. The in vivo treatment reduced the lesion and the parasite load at the tested doses, corroborating the assumption that ICaf may be a potential pharmacological alternative against L. amazonensis.

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
Current Research in Biotechnology
Current Research in Biotechnology Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
6.70
自引率
3.60%
发文量
50
审稿时长
38 days
期刊介绍: Current Research in Biotechnology (CRBIOT) is a new primary research, gold open access journal from Elsevier. CRBIOT publishes original papers, reviews, and short communications (including viewpoints and perspectives) resulting from research in biotechnology and biotech-associated disciplines. Current Research in Biotechnology is a peer-reviewed gold open access (OA) journal and upon acceptance all articles are permanently and freely available. It is a companion to the highly regarded review journal Current Opinion in Biotechnology (2018 CiteScore 8.450) and is part of the Current Opinion and Research (CO+RE) suite of journals. All CO+RE journals leverage the Current Opinion legacy-of editorial excellence, high-impact, and global reach-to ensure they are a widely read resource that is integral to scientists' workflow.
期刊最新文献
Engineering yeast lipids for production of designer biodiesel Table of Contents Dolastatins and their analogues present a compelling landscape of potential natural and synthetic anticancer drug candidates Drug Discovery, Diagnostic, and therapeutic trends on Mpox: A patent landscape Life cycle and environmental impact assessment of vegetation-activated sludge process (V-ASP) for decentralized wastewater treatment
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1