In Vitro Antifungal Activities of D11-2040, a β-1,6-Glucan Inhibitor, with or without Currently Available Antifungal Drugs
We recently reported our discovery of small molecule β-1,6-glucan inhibitor named D75-4590 and the anti-Candida activity of its derivatives D11-2040 and D21-6076. In this study, we further evaluated the antifungal profile of D11-2040. It alone strongly inhibited the vegetative growth and/or hyphal d...
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| Veröffentlicht in: | Biological & pharmaceutical bulletin 2010/02/01, Vol.33(2), pp.192-197 |
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| container_title | Biological & pharmaceutical bulletin |
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| creator | Kitamura, Akihiro Someya, Kazuhiko Okumura, Ryo Hata, Masato Takeshita, Hiroshi Nakajima, Ryohei |
| description | We recently reported our discovery of small molecule β-1,6-glucan inhibitor named D75-4590 and the anti-Candida activity of its derivatives D11-2040 and D21-6076. In this study, we further evaluated the antifungal profile of D11-2040. It alone strongly inhibited the vegetative growth and/or hyphal development of various Candida species, but no significant activity was observed against Cryptococcus neoformans or any of the filamentous fungi tested. Synergism was detected for C. albicans in the interaction of D11-2040 and caspofungin by the chequerboard method and in that of D11-2040 and fluconazole by the time-kill method. Slight but positive interactions were observed in several combinations for C. neoformans and Aspergillus fumigatus as well. These results suggested that β-1,6-glucan inhibitors have promising potential as single drugs as well as concomitants. |
| doi_str_mv | 10.1248/bpb.33.192 |
| format | Article |
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In this study, we further evaluated the antifungal profile of D11-2040. It alone strongly inhibited the vegetative growth and/or hyphal development of various Candida species, but no significant activity was observed against Cryptococcus neoformans or any of the filamentous fungi tested. Synergism was detected for C. albicans in the interaction of D11-2040 and caspofungin by the chequerboard method and in that of D11-2040 and fluconazole by the time-kill method. Slight but positive interactions were observed in several combinations for C. neoformans and Aspergillus fumigatus as well. 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These results suggested that β-1,6-glucan inhibitors have promising potential as single drugs as well as concomitants.</description><subject>Animals</subject><subject>Antifungal Agents - administration & dosage</subject><subject>Antifungal Agents - pharmacology</subject><subject>antifungal susceptibility</subject><subject>Aspergillus fumigatus - drug effects</subject><subject>Aspergillus fumigatus - physiology</subject><subject>Benzimidazoles - pharmacology</subject><subject>beta-Glucans - antagonists & inhibitors</subject><subject>beta-Glucans - metabolism</subject><subject>Candida - drug effects</subject><subject>Candida - physiology</subject><subject>cell wall</subject><subject>combination</subject><subject>Cryptococcus neoformans - drug effects</subject><subject>Cryptococcus neoformans - physiology</subject><subject>Drug Therapy, Combination</subject><subject>Female</subject><subject>Mice</subject><subject>Microbial Sensitivity Tests - methods</subject><subject>Pyridines - pharmacology</subject><subject>synergy</subject><subject>β-1,6-glucan</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpNkM1uEzEQgC0EoqFw4QGQb0goG8Z_-3NCUUpLpEpcgKtlO-PElbMbbG-rirfiQXimLqSNuMwc5tM30kfIWwYLxmX70R7sQogF6_gzMmNCNpXiTD0nM-hYW9VMtWfkVc43ANAAFy_JGQfGWiW6Gfm17umPUNJAl30Jfuy3JtKlK-E2lICZDp5eMFZxkDCnhv75XbF5XV3F0ZmervtdsKEMaU7vQtnRIf3bw1joakwJ-xLv6fLWhGhsxP8_XKRxm1-TF97EjG8e9zn5fvn52-pLdf31ar1aXldO1m2pOi9Np0Bh1zjEjUJneS1rBdKzFjygVWA8iMbxlgtwGyudM6JpwFnw3Ipz8v7oPaTh54i56H3IDmM0PQ5j1o2QvOZNzSbyw5F0acg5odeHFPYm3WsG-m9rPbXWQuip9QS_e9SOdo-bE_oUdwI-HYGbXMwWT4BJJbiITy5-HJPydHE7kzT24gGVrJCv</recordid><startdate>20100201</startdate><enddate>20100201</enddate><creator>Kitamura, Akihiro</creator><creator>Someya, Kazuhiko</creator><creator>Okumura, Ryo</creator><creator>Hata, Masato</creator><creator>Takeshita, Hiroshi</creator><creator>Nakajima, Ryohei</creator><general>The Pharmaceutical Society of Japan</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>20100201</creationdate><title>In Vitro Antifungal Activities of D11-2040, a β-1,6-Glucan Inhibitor, with or without Currently Available Antifungal Drugs</title><author>Kitamura, Akihiro ; Someya, Kazuhiko ; Okumura, Ryo ; Hata, Masato ; Takeshita, Hiroshi ; Nakajima, Ryohei</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c468t-9f4a9505e97ceed5ecb2646504f180f0eb50af037c28230cdb4cca3770cb0f2b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Animals</topic><topic>Antifungal Agents - administration & dosage</topic><topic>Antifungal Agents - pharmacology</topic><topic>antifungal susceptibility</topic><topic>Aspergillus fumigatus - drug effects</topic><topic>Aspergillus fumigatus - physiology</topic><topic>Benzimidazoles - pharmacology</topic><topic>beta-Glucans - antagonists & inhibitors</topic><topic>beta-Glucans - metabolism</topic><topic>Candida - drug effects</topic><topic>Candida - physiology</topic><topic>cell wall</topic><topic>combination</topic><topic>Cryptococcus neoformans - drug effects</topic><topic>Cryptococcus neoformans - physiology</topic><topic>Drug Therapy, Combination</topic><topic>Female</topic><topic>Mice</topic><topic>Microbial Sensitivity Tests - methods</topic><topic>Pyridines - pharmacology</topic><topic>synergy</topic><topic>β-1,6-glucan</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kitamura, Akihiro</creatorcontrib><creatorcontrib>Someya, Kazuhiko</creatorcontrib><creatorcontrib>Okumura, Ryo</creatorcontrib><creatorcontrib>Hata, Masato</creatorcontrib><creatorcontrib>Takeshita, Hiroshi</creatorcontrib><creatorcontrib>Nakajima, Ryohei</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>Biological & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kitamura, Akihiro</au><au>Someya, Kazuhiko</au><au>Okumura, Ryo</au><au>Hata, Masato</au><au>Takeshita, Hiroshi</au><au>Nakajima, Ryohei</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In Vitro Antifungal Activities of D11-2040, a β-1,6-Glucan Inhibitor, with or without Currently Available Antifungal Drugs</atitle><jtitle>Biological & pharmaceutical bulletin</jtitle><addtitle>Biol Pharm Bull</addtitle><date>2010-02-01</date><risdate>2010</risdate><volume>33</volume><issue>2</issue><spage>192</spage><epage>197</epage><pages>192-197</pages><issn>0918-6158</issn><eissn>1347-5215</eissn><abstract>We recently reported our discovery of small molecule β-1,6-glucan inhibitor named D75-4590 and the anti-Candida activity of its derivatives D11-2040 and D21-6076. 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| source | J-STAGE Free; MEDLINE; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals Antifungal Agents - administration & dosage Antifungal Agents - pharmacology antifungal susceptibility Aspergillus fumigatus - drug effects Aspergillus fumigatus - physiology Benzimidazoles - pharmacology beta-Glucans - antagonists & inhibitors beta-Glucans - metabolism Candida - drug effects Candida - physiology cell wall combination Cryptococcus neoformans - drug effects Cryptococcus neoformans - physiology Drug Therapy, Combination Female Mice Microbial Sensitivity Tests - methods Pyridines - pharmacology synergy β-1,6-glucan |
| title | In Vitro Antifungal Activities of D11-2040, a β-1,6-Glucan Inhibitor, with or without Currently Available Antifungal Drugs |
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