{"created":"2023-06-20T16:49:16.246802+00:00","id":21449,"links":{},"metadata":{"_buckets":{"deposit":"cb512675-6259-4e84-a7bc-ce2de567252a"},"_deposit":{"created_by":3,"id":"21449","owners":[3],"pid":{"revision_id":0,"type":"depid","value":"21449"},"status":"published"},"_oai":{"id":"oai:kindai.repo.nii.ac.jp:00021449","sets":["14:2667:4613"]},"author_link":["43308"],"control_number":"21449","item_8_biblio_info_21":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2020","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"8","bibliographicPageStart":"1","bibliographic_titles":[{"bibliographic_title":"科学研究費助成事業研究成果報告書 (2019)"}]}]},"item_8_description_25":{"attribute_name":"リンクURL","attribute_value_mlt":[{"subitem_description":"https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-17K08377/","subitem_description_type":"Other"}]},"item_8_description_33":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"研究成果の概要（和文）：アーユルベーダ薬物”サラシア”から単離された,強力なα-グルコシダーゼ阻害剤、サラシノール (1), ネオコタラノール (2) の効率的大量合成を目的として、チオ糖とエポキシド との S-アルキル化を鍵反応とするスルホニウム塩構築法のジアステレオ選択的合成法を確立した (dr,α/β=約26/1)。また、本手法を用いて、高活性誘導体[３-O-(一置換ベンジル）体]の合成を行い、in vitroでヒト小腸由来マルターゼに対して糖尿病治療薬、アカルボース、ボグリボース以上のIC50値をしめすことを明らかにした。さらに、これら誘導体のマウスへの投与で食後過血糖の上昇が著しく阻害されることも判明した。研究成果の概要（英文）：A facile and highly diastereoselective approach toward the synthesis of potent salacinol-type α-glucosidase inhibitors, originally isolated from plants of the genus “ Salacia”, was developed using the S-alkylation of thiosugars with epoxides in HFIP (約;90%, dr, α /β = 約 26/1). The dr ratio of the product was significantly improved by the protocol as compared to that of the conventional S-alkylation of thiosugars (dr, α/β = 約 8/1). The protocol could be used for gram scale synthesis of the desired compounds. The 3′-O-benzylated salacinol analogs, which are the most potent in vitro inhibitors to date, were synthesized and evaluated in vivo; all analogs suppressed blood glucose levels in maltose－loaded mice, at levels comparable to those of the antidiabetic agent, voglibose.","subitem_description_type":"Abstract"}]},"item_8_description_36":{"attribute_name":"内容記述","attribute_value_mlt":[{"subitem_description":"研究種目：基盤研究(C);  研究期間：2017～2019;   課題番号：17K08377;   研究分野：有機合成、構造活性相関;   科研費の分科・細目：","subitem_description_type":"Other"}]},"item_8_description_37":{"attribute_name":"資源タイプ(WEKO2)","attribute_value_mlt":[{"subitem_description":"Research Paper","subitem_description_type":"Other"}]},"item_8_description_41":{"attribute_name":"フォーマット","attribute_value_mlt":[{"subitem_description":"application/pdf","subitem_description_type":"Other"}]},"item_8_publisher_14":{"attribute_name":"出版者 名前","attribute_value_mlt":[{"subitem_publisher":"近畿大学"}]},"item_8_text_10":{"attribute_name":"著者 役割","attribute_value_mlt":[{"subitem_text_value":"研究代表者"}]},"item_8_text_7":{"attribute_name":"著者(英)","attribute_value_mlt":[{"subitem_text_language":"en","subitem_text_value":"Tanabe, Genzoh"}]},"item_8_text_8":{"attribute_name":"著者 所属","attribute_value_mlt":[{"subitem_text_value":"近畿大学薬学部; 教授"}]},"item_8_text_9":{"attribute_name":"著者所属(翻訳)","attribute_value_mlt":[{"subitem_text_value":"Kindai University"}]},"item_8_version_type_12":{"attribute_name":"版","attribute_value_mlt":[{"subitem_version_resource":"http://purl.org/coar/version/c_be7fb7dd8ff6fe43","subitem_version_type":"NA"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"田辺, 元三"},{"creatorName":"タナベ, ゲンゾウ","creatorNameLang":"ja-Kana"}],"nameIdentifiers":[{"nameIdentifier":"43308","nameIdentifierScheme":"WEKO"},{"nameIdentifier":"40217104","nameIdentifierScheme":"NRID","nameIdentifierURI":"https://nrid.nii.ac.jp/ja/search/?kw=40217104"}]}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2021-03-15"}],"displaytype":"detail","filename":"17K08377seika.pdf","filesize":[{"value":"314.1 kB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"17K08377seika.pdf","url":"https://kindai.repo.nii.ac.jp/record/21449/files/17K08377seika.pdf"},"version_id":"866b04a9-bd05-4f97-87bb-956f70836f06"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"salacinol","subitem_subject_language":"en","subitem_subject_scheme":"Other"},{"subitem_subject":"neokotalanol","subitem_subject_language":"en","subitem_subject_scheme":"Other"},{"subitem_subject":"α-glucosidase inhibitor","subitem_subject_language":"en","subitem_subject_scheme":"Other"},{"subitem_subject":"Salacia","subitem_subject_language":"en","subitem_subject_scheme":"Other"},{"subitem_subject":"SAR study","subitem_subject_language":"en","subitem_subject_scheme":"Other"},{"subitem_subject":"Diabetes","subitem_subject_language":"en","subitem_subject_scheme":"Other"}]},"item_language":{"attribute_name":"言語","attribute_value_mlt":[{"subitem_language":"jpn"}]},"item_resource_type":{"attribute_name":"資源タイプ","attribute_value_mlt":[{"resourcetype":"research report","resourceuri":"http://purl.org/coar/resource_type/c_18ws"}]},"item_title":"サラシノールをシードとする新規ジカチオン型高活性食後過血糖改善薬の合成と活性評価","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"サラシノールをシードとする新規ジカチオン型高活性食後過血糖改善薬の合成と活性評価","subitem_title_language":"ja"},{"subitem_title":"Synthesis and evaluation of di-cationic sulfonium-type alpha-glucosidase inhibitors based on the structure of salacinol","subitem_title_language":"en"}]},"item_type_id":"8","owner":"3","path":["4613"],"pubdate":{"attribute_name":"PubDate","attribute_value":"2021-03-15"},"publish_date":"2021-03-15","publish_status":"0","recid":"21449","relation_version_is_last":true,"title":["サラシノールをシードとする新規ジカチオン型高活性食後過血糖改善薬の合成と活性評価"],"weko_creator_id":"3","weko_shared_id":-1},"updated":"2023-09-13T05:52:20.734123+00:00"}