A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models
Abstract New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis . Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis...
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| Veröffentlicht in: | Biomedicine & pharmacotherapy 2017-04, Vol.88, p.603-609 |
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| creator | Gao, Chao Ye, Ting-Hong Peng, Cui-Ting Shi, Yao-jie You, Xin-Yu Xiong, Lu Ran, Kai Zhang, Li-Dan Zeng, Xiu-Xiu Wang, Ning-Yu Yu, Luo-Ting Wei, Yu-Quan |
| description | Abstract New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis . Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis H37Rv infection mouse models, SKLB-TB1001 significantly attenuated the mycobacterial load in lungs and spleens. The colony forming unit counts and histological examination of lungs from H37Rv infected mice revealed that the benzothiazinethione analogue SKLB-TB1001 as a higher dose level was as effective as isoniazid. Moreover, in a multidrug-resistant (MDR)-TB mouse model, SKLB-TB1001 showed significant activity in a dose-dependent manner and was more effective than streptomycin. These results suggested that SKLB-TB1001 could be an antitubercular drug candidate worth further investigation. |
| doi_str_mv | 10.1016/j.biopha.2017.01.098 |
| format | Article |
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Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis H37Rv infection mouse models, SKLB-TB1001 significantly attenuated the mycobacterial load in lungs and spleens. The colony forming unit counts and histological examination of lungs from H37Rv infected mice revealed that the benzothiazinethione analogue SKLB-TB1001 as a higher dose level was as effective as isoniazid. Moreover, in a multidrug-resistant (MDR)-TB mouse model, SKLB-TB1001 showed significant activity in a dose-dependent manner and was more effective than streptomycin. These results suggested that SKLB-TB1001 could be an antitubercular drug candidate worth further investigation.</description><identifier>ISSN: 0753-3322</identifier><identifier>EISSN: 1950-6007</identifier><identifier>DOI: 10.1016/j.biopha.2017.01.098</identifier><identifier>PMID: 28142116</identifier><language>eng</language><publisher>France: Elsevier Masson SAS</publisher><subject>Animals ; Antitubercular Agents - pharmacology ; Colony Count, Microbial ; Disease Models, Animal ; Female ; H37Rv ; Internal Medicine ; Lung - drug effects ; Lung - microbiology ; Lung - pathology ; MDR-TB ; Medical Education ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; Murine models ; Mycobacterium tuberculosis ; Mycobacterium tuberculosis - drug effects ; SKLB-TB1001 ; Survival Analysis ; Thiadiazoles - chemical synthesis ; Thiadiazoles - chemistry ; Thiadiazoles - pharmacology ; Thiadiazoles - therapeutic use ; Treatment Outcome ; Tuberculosis - drug therapy ; Tuberculosis - microbiology ; Tuberculosis - pathology</subject><ispartof>Biomedicine & pharmacotherapy, 2017-04, Vol.88, p.603-609</ispartof><rights>Elsevier Masson SAS</rights><rights>2017 Elsevier Masson SAS</rights><rights>Copyright © 2017 Elsevier Masson SAS. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-c5f04b841cdab473f1c182e2dd4114245263dfea64a68257e64526e3bfc459d13</citedby><cites>FETCH-LOGICAL-c417t-c5f04b841cdab473f1c182e2dd4114245263dfea64a68257e64526e3bfc459d13</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.biopha.2017.01.098$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3549,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28142116$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Gao, Chao</creatorcontrib><creatorcontrib>Ye, Ting-Hong</creatorcontrib><creatorcontrib>Peng, Cui-Ting</creatorcontrib><creatorcontrib>Shi, Yao-jie</creatorcontrib><creatorcontrib>You, Xin-Yu</creatorcontrib><creatorcontrib>Xiong, Lu</creatorcontrib><creatorcontrib>Ran, Kai</creatorcontrib><creatorcontrib>Zhang, Li-Dan</creatorcontrib><creatorcontrib>Zeng, Xiu-Xiu</creatorcontrib><creatorcontrib>Wang, Ning-Yu</creatorcontrib><creatorcontrib>Yu, Luo-Ting</creatorcontrib><creatorcontrib>Wei, Yu-Quan</creatorcontrib><title>A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models</title><title>Biomedicine & pharmacotherapy</title><addtitle>Biomed Pharmacother</addtitle><description>Abstract New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis . Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis H37Rv infection mouse models, SKLB-TB1001 significantly attenuated the mycobacterial load in lungs and spleens. The colony forming unit counts and histological examination of lungs from H37Rv infected mice revealed that the benzothiazinethione analogue SKLB-TB1001 as a higher dose level was as effective as isoniazid. Moreover, in a multidrug-resistant (MDR)-TB mouse model, SKLB-TB1001 showed significant activity in a dose-dependent manner and was more effective than streptomycin. These results suggested that SKLB-TB1001 could be an antitubercular drug candidate worth further investigation.</description><subject>Animals</subject><subject>Antitubercular Agents - pharmacology</subject><subject>Colony Count, Microbial</subject><subject>Disease Models, Animal</subject><subject>Female</subject><subject>H37Rv</subject><subject>Internal Medicine</subject><subject>Lung - drug effects</subject><subject>Lung - microbiology</subject><subject>Lung - pathology</subject><subject>MDR-TB</subject><subject>Medical Education</subject><subject>Mice, Inbred BALB C</subject><subject>Mice, Inbred C57BL</subject><subject>Murine models</subject><subject>Mycobacterium tuberculosis</subject><subject>Mycobacterium tuberculosis - drug effects</subject><subject>SKLB-TB1001</subject><subject>Survival Analysis</subject><subject>Thiadiazoles - chemical synthesis</subject><subject>Thiadiazoles - chemistry</subject><subject>Thiadiazoles - pharmacology</subject><subject>Thiadiazoles - therapeutic use</subject><subject>Treatment Outcome</subject><subject>Tuberculosis - drug therapy</subject><subject>Tuberculosis - microbiology</subject><subject>Tuberculosis - pathology</subject><issn>0753-3322</issn><issn>1950-6007</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFUcFu1DAUjBCILoU_QMhHLgl-juNkL0htBbRiJQ4tZ8uxX6gXx17sZKXdr8dRCgcunN7T07wZzUxRvAVaAQXxYV_1NhweVcUotBWFim67Z8UGtg0tBaXt82JD26Yu65qxi-JVSntKaSPq7mVxwTrgDEBsivMV8eGIjvToz2F6tOpsPeYZPBLllQs_ZiT3X3fX5cM1UArE2HRw6pTIIUzopwya7HjSoVd6wmiVI3mxRztZTMR6okjK57yHgYxzzOxkDAZdel28GJRL-OZpXhbfP396uLktd9--3N1c7UrNoZ1K3QyU9x0HbVTP23oADR1DZgyH7II3TNRmQCW4Eh1rWhTLCet-0LzZGqgvi_cr7yGGXzOmSY42aXROeQxzktCJuqWCdjxD-QrVMaQUcZCHaEcVTxKoXFKXe7mmLpfUJQWZU89v754U5n5E8_fpT8wZ8HEFZNt4tBhl0ha9RmMj6kmaYP-n8C-BdtZbrdxPPGHahznmrrIXmZik8n5pfik-a6_OfgNh-arA</recordid><startdate>20170401</startdate><enddate>20170401</enddate><creator>Gao, Chao</creator><creator>Ye, Ting-Hong</creator><creator>Peng, Cui-Ting</creator><creator>Shi, Yao-jie</creator><creator>You, Xin-Yu</creator><creator>Xiong, Lu</creator><creator>Ran, Kai</creator><creator>Zhang, Li-Dan</creator><creator>Zeng, Xiu-Xiu</creator><creator>Wang, Ning-Yu</creator><creator>Yu, Luo-Ting</creator><creator>Wei, Yu-Quan</creator><general>Elsevier Masson SAS</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20170401</creationdate><title>A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models</title><author>Gao, Chao ; Ye, Ting-Hong ; Peng, Cui-Ting ; Shi, Yao-jie ; You, Xin-Yu ; Xiong, Lu ; Ran, Kai ; Zhang, Li-Dan ; Zeng, Xiu-Xiu ; Wang, Ning-Yu ; Yu, Luo-Ting ; Wei, Yu-Quan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-c5f04b841cdab473f1c182e2dd4114245263dfea64a68257e64526e3bfc459d13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Animals</topic><topic>Antitubercular Agents - pharmacology</topic><topic>Colony Count, Microbial</topic><topic>Disease Models, Animal</topic><topic>Female</topic><topic>H37Rv</topic><topic>Internal Medicine</topic><topic>Lung - drug effects</topic><topic>Lung - microbiology</topic><topic>Lung - pathology</topic><topic>MDR-TB</topic><topic>Medical Education</topic><topic>Mice, Inbred BALB C</topic><topic>Mice, Inbred C57BL</topic><topic>Murine models</topic><topic>Mycobacterium tuberculosis</topic><topic>Mycobacterium tuberculosis - drug effects</topic><topic>SKLB-TB1001</topic><topic>Survival Analysis</topic><topic>Thiadiazoles - chemical synthesis</topic><topic>Thiadiazoles - chemistry</topic><topic>Thiadiazoles - pharmacology</topic><topic>Thiadiazoles - therapeutic use</topic><topic>Treatment Outcome</topic><topic>Tuberculosis - drug therapy</topic><topic>Tuberculosis - microbiology</topic><topic>Tuberculosis - pathology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gao, Chao</creatorcontrib><creatorcontrib>Ye, Ting-Hong</creatorcontrib><creatorcontrib>Peng, Cui-Ting</creatorcontrib><creatorcontrib>Shi, Yao-jie</creatorcontrib><creatorcontrib>You, Xin-Yu</creatorcontrib><creatorcontrib>Xiong, Lu</creatorcontrib><creatorcontrib>Ran, Kai</creatorcontrib><creatorcontrib>Zhang, Li-Dan</creatorcontrib><creatorcontrib>Zeng, Xiu-Xiu</creatorcontrib><creatorcontrib>Wang, Ning-Yu</creatorcontrib><creatorcontrib>Yu, Luo-Ting</creatorcontrib><creatorcontrib>Wei, Yu-Quan</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Biomedicine & pharmacotherapy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gao, Chao</au><au>Ye, Ting-Hong</au><au>Peng, Cui-Ting</au><au>Shi, Yao-jie</au><au>You, Xin-Yu</au><au>Xiong, Lu</au><au>Ran, Kai</au><au>Zhang, Li-Dan</au><au>Zeng, Xiu-Xiu</au><au>Wang, Ning-Yu</au><au>Yu, Luo-Ting</au><au>Wei, Yu-Quan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models</atitle><jtitle>Biomedicine & pharmacotherapy</jtitle><addtitle>Biomed Pharmacother</addtitle><date>2017-04-01</date><risdate>2017</risdate><volume>88</volume><spage>603</spage><epage>609</epage><pages>603-609</pages><issn>0753-3322</issn><eissn>1950-6007</eissn><abstract>Abstract New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis . 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| source | Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE |
| subjects | Animals Antitubercular Agents - pharmacology Colony Count, Microbial Disease Models, Animal Female H37Rv Internal Medicine Lung - drug effects Lung - microbiology Lung - pathology MDR-TB Medical Education Mice, Inbred BALB C Mice, Inbred C57BL Murine models Mycobacterium tuberculosis Mycobacterium tuberculosis - drug effects SKLB-TB1001 Survival Analysis Thiadiazoles - chemical synthesis Thiadiazoles - chemistry Thiadiazoles - pharmacology Thiadiazoles - therapeutic use Treatment Outcome Tuberculosis - drug therapy Tuberculosis - microbiology Tuberculosis - pathology |
| title | A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models |
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