Effect of HIV protease inhibitors and Orlistat on mycobacterial ES-31 serine protease, a potential drug target in Mycobacterium tuberculosis
Mycobacterial excretory secretory-31 (SEVA TB ES-31) antigen is shown to possess protease and lipase activities. To study the effect of commonly used HIV-protease inhibitors and lipase inhibitor Orlistat if any on mycobacterial ES-31 serine protease in vitro enzyme activity and on the growth of M.tb...
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| Veröffentlicht in: | Indian journal of tuberculosis 2011-01, Vol.58 (1), p.4-10 |
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| creator | Majumdar, Anindita Wankhade, Gauri Kamble, Pranita D Harinath, B C |
| description | Mycobacterial excretory secretory-31 (SEVA TB ES-31) antigen is shown to possess protease and lipase activities.
To study the effect of commonly used HIV-protease inhibitors and lipase inhibitor Orlistat if any on mycobacterial ES-31 serine protease in vitro enzyme activity and on the growth of M.tb H37Ra bacilli in axenic culture.
Effect of HIV-protease inhibitors namely Ritonavir, Lopinavir and Indinavir and Orlistat on protease activity of ES-31 was assessed using azocasein assay and on bacillary growth in axenic culture of Mycobacterium tuberculosis H37Ra. The concentration of ES-31 antigen in culture filtrate was determined by sandwich peroxidase ELISA using anti ES-31 antibody and the growth of bacilli by CFU count.
HIV-protease inhibitors such as Ritonavir, Lopinavir and Indinavir and lipase inhibitor Orlistat inhibited serine protease activity by 41.3 - 69.7% in vitro. These inhibitors also showed decreased bacterial growth in axenic culture and further confirmed by decreased concentration of ES-31 serine protease secretion in the culture fluid. Ritonavir showed maximum inhibition of 77% on the growth of the bacilli in axenic culture while anti obesity drug Orlistat showed 61% inhibition.
SEVA TB ES-31 with serine protease and lipase activities may be a potential drug target in tuberculosis management. |
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To study the effect of commonly used HIV-protease inhibitors and lipase inhibitor Orlistat if any on mycobacterial ES-31 serine protease in vitro enzyme activity and on the growth of M.tb H37Ra bacilli in axenic culture.
Effect of HIV-protease inhibitors namely Ritonavir, Lopinavir and Indinavir and Orlistat on protease activity of ES-31 was assessed using azocasein assay and on bacillary growth in axenic culture of Mycobacterium tuberculosis H37Ra. The concentration of ES-31 antigen in culture filtrate was determined by sandwich peroxidase ELISA using anti ES-31 antibody and the growth of bacilli by CFU count.
HIV-protease inhibitors such as Ritonavir, Lopinavir and Indinavir and lipase inhibitor Orlistat inhibited serine protease activity by 41.3 - 69.7% in vitro. These inhibitors also showed decreased bacterial growth in axenic culture and further confirmed by decreased concentration of ES-31 serine protease secretion in the culture fluid. Ritonavir showed maximum inhibition of 77% on the growth of the bacilli in axenic culture while anti obesity drug Orlistat showed 61% inhibition.
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To study the effect of commonly used HIV-protease inhibitors and lipase inhibitor Orlistat if any on mycobacterial ES-31 serine protease in vitro enzyme activity and on the growth of M.tb H37Ra bacilli in axenic culture.
Effect of HIV-protease inhibitors namely Ritonavir, Lopinavir and Indinavir and Orlistat on protease activity of ES-31 was assessed using azocasein assay and on bacillary growth in axenic culture of Mycobacterium tuberculosis H37Ra. The concentration of ES-31 antigen in culture filtrate was determined by sandwich peroxidase ELISA using anti ES-31 antibody and the growth of bacilli by CFU count.
HIV-protease inhibitors such as Ritonavir, Lopinavir and Indinavir and lipase inhibitor Orlistat inhibited serine protease activity by 41.3 - 69.7% in vitro. These inhibitors also showed decreased bacterial growth in axenic culture and further confirmed by decreased concentration of ES-31 serine protease secretion in the culture fluid. Ritonavir showed maximum inhibition of 77% on the growth of the bacilli in axenic culture while anti obesity drug Orlistat showed 61% inhibition.
SEVA TB ES-31 with serine protease and lipase activities may be a potential drug target in tuberculosis management.</description><subject>Antigens, Bacterial - drug effects</subject><subject>Antigens, Bacterial - metabolism</subject><subject>Bacterial Proteins</subject><subject>Enzyme-Linked Immunosorbent Assay</subject><subject>HIV Protease Inhibitors - therapeutic use</subject><subject>Humans</subject><subject>Lactones - therapeutic use</subject><subject>Lopinavir</subject><subject>Mycobacterium tuberculosis - drug effects</subject><subject>Mycobacterium tuberculosis - enzymology</subject><subject>Mycobacterium tuberculosis - isolation & purification</subject><subject>Pyrimidinones - therapeutic use</subject><subject>Ritonavir - therapeutic use</subject><subject>Serine Endopeptidases - drug effects</subject><subject>Serine Endopeptidases - metabolism</subject><subject>Tuberculosis - drug therapy</subject><subject>Tuberculosis - microbiology</subject><issn>0019-5707</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkMtOwzAURL0A0VL4BXR3bIhkx64TL1FVoFJRFzy2kZ3cFKO88GPRf-CjMaLAamakM6Ore0LmlDKVLQtazMi59--UckEFPyOznAmRF0rNyee6bbEOMLbwsHmFyY0BtUeww5s1NozOgx4a2LnO-qATN0B_qEej64DO6g7WTxln4FMY8K9-AxqmZIfwjTQu7iFot8eQduHxvx97CNGgq2M3eusvyGmrO4-XR12Ql7v18-oh2-7uN6vbbTaxfBmynEmtaKlQUs6MTJZqw7gpDNdNXghZtChNw5RWJTe1bCUvmWIS85oKJhVfkOuf3XTvR0Qfqt76GrtODzhGX5VLxakSgify6khG02NTTc722h2q3wfyL_m5bLI</recordid><startdate>201101</startdate><enddate>201101</enddate><creator>Majumdar, Anindita</creator><creator>Wankhade, Gauri</creator><creator>Kamble, Pranita D</creator><creator>Harinath, B C</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>201101</creationdate><title>Effect of HIV protease inhibitors and Orlistat on mycobacterial ES-31 serine protease, a potential drug target in Mycobacterium tuberculosis</title><author>Majumdar, Anindita ; Wankhade, Gauri ; Kamble, Pranita D ; Harinath, B C</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p125t-216a9089e6031b69080ab13b7b3ad27467fe6bd19a983bc6f6381916e2c041693</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Antigens, Bacterial - drug effects</topic><topic>Antigens, Bacterial - metabolism</topic><topic>Bacterial Proteins</topic><topic>Enzyme-Linked Immunosorbent Assay</topic><topic>HIV Protease Inhibitors - therapeutic use</topic><topic>Humans</topic><topic>Lactones - therapeutic use</topic><topic>Lopinavir</topic><topic>Mycobacterium tuberculosis - drug effects</topic><topic>Mycobacterium tuberculosis - enzymology</topic><topic>Mycobacterium tuberculosis - isolation & purification</topic><topic>Pyrimidinones - therapeutic use</topic><topic>Ritonavir - therapeutic use</topic><topic>Serine Endopeptidases - drug effects</topic><topic>Serine Endopeptidases - metabolism</topic><topic>Tuberculosis - drug therapy</topic><topic>Tuberculosis - microbiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Majumdar, Anindita</creatorcontrib><creatorcontrib>Wankhade, Gauri</creatorcontrib><creatorcontrib>Kamble, Pranita D</creatorcontrib><creatorcontrib>Harinath, B C</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Indian journal of tuberculosis</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Majumdar, Anindita</au><au>Wankhade, Gauri</au><au>Kamble, Pranita D</au><au>Harinath, B C</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of HIV protease inhibitors and Orlistat on mycobacterial ES-31 serine protease, a potential drug target in Mycobacterium tuberculosis</atitle><jtitle>Indian journal of tuberculosis</jtitle><addtitle>Indian J Tuberc</addtitle><date>2011-01</date><risdate>2011</risdate><volume>58</volume><issue>1</issue><spage>4</spage><epage>10</epage><pages>4-10</pages><issn>0019-5707</issn><abstract>Mycobacterial excretory secretory-31 (SEVA TB ES-31) antigen is shown to possess protease and lipase activities.
To study the effect of commonly used HIV-protease inhibitors and lipase inhibitor Orlistat if any on mycobacterial ES-31 serine protease in vitro enzyme activity and on the growth of M.tb H37Ra bacilli in axenic culture.
Effect of HIV-protease inhibitors namely Ritonavir, Lopinavir and Indinavir and Orlistat on protease activity of ES-31 was assessed using azocasein assay and on bacillary growth in axenic culture of Mycobacterium tuberculosis H37Ra. The concentration of ES-31 antigen in culture filtrate was determined by sandwich peroxidase ELISA using anti ES-31 antibody and the growth of bacilli by CFU count.
HIV-protease inhibitors such as Ritonavir, Lopinavir and Indinavir and lipase inhibitor Orlistat inhibited serine protease activity by 41.3 - 69.7% in vitro. These inhibitors also showed decreased bacterial growth in axenic culture and further confirmed by decreased concentration of ES-31 serine protease secretion in the culture fluid. Ritonavir showed maximum inhibition of 77% on the growth of the bacilli in axenic culture while anti obesity drug Orlistat showed 61% inhibition.
SEVA TB ES-31 with serine protease and lipase activities may be a potential drug target in tuberculosis management.</abstract><cop>India</cop><pmid>21442799</pmid><tpages>7</tpages></addata></record> |
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| ispartof | Indian journal of tuberculosis, 2011-01, Vol.58 (1), p.4-10 |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | Antigens, Bacterial - drug effects Antigens, Bacterial - metabolism Bacterial Proteins Enzyme-Linked Immunosorbent Assay HIV Protease Inhibitors - therapeutic use Humans Lactones - therapeutic use Lopinavir Mycobacterium tuberculosis - drug effects Mycobacterium tuberculosis - enzymology Mycobacterium tuberculosis - isolation & purification Pyrimidinones - therapeutic use Ritonavir - therapeutic use Serine Endopeptidases - drug effects Serine Endopeptidases - metabolism Tuberculosis - drug therapy Tuberculosis - microbiology |
| title | Effect of HIV protease inhibitors and Orlistat on mycobacterial ES-31 serine protease, a potential drug target in Mycobacterium tuberculosis |
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