WEKO3
アイテム
{"_buckets": {"deposit": "821371cd-2792-45d5-9a48-835e2cb99a87"}, "_deposit": {"created_by": 2, "id": "3732", "owners": [2], "pid": {"revision_id": 0, "type": "depid", "value": "3732"}, "status": "published"}, "_oai": {"id": "oai:nagasaki-u.repo.nii.ac.jp:00003732", "sets": ["28"]}, "author_link": ["15207", "15205", "15204", "15206"], "item_2_biblio_info_6": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2015-12-22", "bibliographicIssueDateType": "Issued"}, "bibliographicPageStart": "1453", "bibliographicVolumeNumber": "6", "bibliographic_titles": [{"bibliographic_title": "Frontiers in Microbiology"}]}]}, "item_2_description_4": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using Candida albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC1280TM) using an antifungal susceptibility test (AST). To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF) cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by \u003e50%. Of these, 26 compounds had fungistatic effects and nine compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration. Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal candidiasis.", "subitem_description_type": "Abstract"}]}, "item_2_description_63": {"attribute_name": "引用", "attribute_value_mlt": [{"subitem_description": "Frontiers in Microbiology, 6, 1453; 2015", "subitem_description_type": "Other"}]}, "item_2_publisher_33": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "Frontiers Media S. A."}]}, "item_2_relation_12": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type": "isIdenticalTo", "subitem_relation_type_id": {"subitem_relation_type_id_text": "10.3389/fmicb.2015.01453", "subitem_relation_type_select": "DOI"}}]}, "item_2_rights_13": {"attribute_name": "権利", "attribute_value_mlt": [{"subitem_rights": "c 2015 Watamoto, Egusa, Sawase and Yatani. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms."}]}, "item_2_source_id_8": {"attribute_name": "EISSN", "attribute_value_mlt": [{"subitem_source_identifier": "1664302X", "subitem_source_identifier_type": "ISSN"}]}, "item_2_version_type_16": {"attribute_name": "著者版フラグ", "attribute_value_mlt": [{"subitem_version_resource": "http://purl.org/coar/version/c_970fb48d4fbd8a85", "subitem_version_type": "VoR"}]}, "item_creator": {"attribute_name": "著者", "attribute_type": "creator", "attribute_value_mlt": [{"creatorNames": [{"creatorName": "Watamoto, Takao"}], "nameIdentifiers": [{"nameIdentifier": "15204", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Egusa, Hiroshi"}], "nameIdentifiers": [{"nameIdentifier": "15205", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Sawase, Takashi"}], "nameIdentifiers": [{"nameIdentifier": "15206", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yatani, Hirofumi"}], "nameIdentifiers": [{"nameIdentifier": "15207", "nameIdentifierScheme": "WEKO"}]}]}, "item_files": {"attribute_name": "ファイル情報", "attribute_type": "file", "attribute_value_mlt": [{"accessrole": "open_date", "date": [{"dateType": "Available", "dateValue": "2020-12-21"}], "displaytype": "detail", "download_preview_message": "", "file_order": 0, "filename": "Fmicb6_1453.pdf", "filesize": [{"value": "783.4 kB"}], "format": "application/pdf", "future_date_message": "", "is_thumbnail": false, "licensetype": "license_free", "mimetype": "application/pdf", "size": 783400.0, "url": {"label": "Fmicb6_1453.pdf", "url": "https://nagasaki-u.repo.nii.ac.jp/record/3732/files/Fmicb6_1453.pdf"}, "version_id": "2089abb1-cb8c-400e-be1d-430ff9b23e85"}]}, "item_keyword": {"attribute_name": "キーワード", "attribute_value_mlt": [{"subitem_subject": "drug discovery", "subitem_subject_scheme": "Other"}, {"subitem_subject": "antifungal drug", "subitem_subject_scheme": "Other"}, {"subitem_subject": "biofilm", "subitem_subject_scheme": "Other"}, {"subitem_subject": "Small molecules", "subitem_subject_scheme": "Other"}, {"subitem_subject": "Candida albicans", "subitem_subject_scheme": "Other"}]}, "item_language": {"attribute_name": "言語", "attribute_value_mlt": [{"subitem_language": "eng"}]}, "item_resource_type": {"attribute_name": "資源タイプ", "attribute_value_mlt": [{"resourcetype": "journal article", "resourceuri": "http://purl.org/coar/resource_type/c_6501"}]}, "item_title": "Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms"}]}, "item_type_id": "2", "owner": "2", "path": ["28"], "permalink_uri": "http://hdl.handle.net/10069/36916", "pubdate": {"attribute_name": "公開日", "attribute_value": "2016-10-28"}, "publish_date": "2016-10-28", "publish_status": "0", "recid": "3732", "relation": {}, "relation_version_is_last": true, "title": ["Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms"], "weko_shared_id": -1}
Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms
http://hdl.handle.net/10069/36916
http://hdl.handle.net/10069/369162b8490d2-d740-4aef-8d87-ec32d00f8a97
名前 / ファイル | ライセンス | アクション |
---|---|---|
Fmicb6_1453.pdf (783.4 kB)
|
|
Item type | 学術雑誌論文 / Journal Article(1) | |||||
---|---|---|---|---|---|---|
公開日 | 2016-10-28 | |||||
タイトル | ||||||
タイトル | Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | drug discovery | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | antifungal drug | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | biofilm | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Small molecules | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Candida albicans | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Watamoto, Takao
× Watamoto, Takao× Egusa, Hiroshi× Sawase, Takashi× Yatani, Hirofumi |
|||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using Candida albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC1280TM) using an antifungal susceptibility test (AST). To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF) cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by >50%. Of these, 26 compounds had fungistatic effects and nine compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration. Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal candidiasis. | |||||
書誌情報 |
Frontiers in Microbiology 巻 6, p. 1453, 発行日 2015-12-22 |
|||||
出版者 | ||||||
出版者 | Frontiers Media S. A. | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 1664302X | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.3389/fmicb.2015.01453 | |||||
権利 | ||||||
権利情報 | c 2015 Watamoto, Egusa, Sawase and Yatani. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Frontiers in Microbiology, 6, 1453; 2015 |