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Activity of (-)-Camphene Derivatives Against Mycobacterium tuberculosis in Acidic pH
Medicinal Chemistry ( IF 2.3 ) Pub Date : 2021-05-31 , DOI: 10.2174/1573406415666191106124016
Hayalla Corrêa de Carvalho 1 , Andressa Lorena Ieque 2 , Tamires Leite Valverde 2 , Vanessa Pietrowski Baldin 1 , Jean Eduardo Meneguello 1 , Paula Aline Zanetti Campanerut-Sá 2 , Fábio Vandresen 3 , Luciana Dias Ghiraldi Lopes 2 , Mariana Regina Passos Souza 4 , Nathally Claudiane de Souza Santos 1 , Vera Lucia Dias Siqueira 1 , Katiany Rizzieri Caleffi-Ferracioli 1 , Regiane Bertin Lima Scodro 2 , Rosilene Fressatti Cardoso 1
Affiliation  

Background: For more than 60 years, the lack of new anti-tuberculosis drugs and the increase of resistant Mycobacterium tuberculosis lineages exhibit a therapeutic challenge, demanding new options for the treatment of resistant tuberculosis.

Objective: Herein, we determined the (i) activities of (-)-camphene and its derivatives and (ii) combinatory effect with pyrazinamide (PZA) against Mycobacterium tuberculosis in acidic pH and (iii) cytotoxicity on VERO cells.

Methods: The activity of (-)-camphene and its 15 derivatives was determined in M. tuberculosis H37Rv in culture medium at pH 6.0 by Resazurin Microtiter Assay Plate (REMA). The activity and combinatory study of three (-)-camphene derivatives with PZA was carried out on seven multidrugresistant (MDR) clinical isolates by REMA and Checkerboard, respectively. The assay of 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) bromide in VERO cells was used to determine the derivatives’ cytotoxicity.


中文翻译:

(-)-Camphene衍生物在酸性pH下对结核分枝杆菌的活性

背景:60多年来,缺乏新的抗结核药物和耐药结核分枝杆菌谱系的增加显示出治疗上的挑战,要求治疗耐药结核的新选择。

目的:在本文中,我们确定了(i)-(-)-camp烯及其衍生物的活性,以及​​(ii)吡嗪酰胺(PZA)在酸性pH下对结核分枝杆菌的联合作用和(iii)对VERO细胞的细胞毒性。

方法:采用刃天青微量滴定板(REMA)测定pH 6.0时在培养基中的结核分枝杆菌H37Rv中(-)-樟脑及其15种衍生物的活性。分别通过REMA和Checkerboard对7种多药耐药(MDR)临床分离株进行了三种(-)-樟脑衍生物与PZA的活性和组合研究。用VERO细胞中3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑(MTT)溴化物的测定来确定衍生物的细胞毒性。
更新日期:2021-05-24
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