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The incubation mixture contained a methanol soluble fraction prepared from the powder of each herbal water extract (equivalent to 1.65 mg of extract powder per mL). Thirty-one herbal extracts inhibited over 50% of human liver microsomal erythromycin N-demethylation, a marker reaction of CYP3A4 activity. Among the 31 herbal extracts, 8 of them (Angelica Dahurica Root, Cassia Bark, Clove, Incised Notopterygium Rhizome, Moutan Bark, Rhubarb, Sappan Wood, Schisandra Fruit) inhibited N-demethylation by over 90%. Among the herbal extracts examined, the strongest inhibition of CYP3A4 was noted with Sappan Wood, which had an IC_\u003c50\u003e value of 43 mg/mL. Rhubarb, Schisandra Fruit, Incised Notopterygium Rhizome, and Angelica Dahurica Root had IC_\u003c50\u003e values of 77, 127, 144, and 185 μg/mL, respectively. Further, 28 of the herbal extracts inhibited over 50% of human liver microsomal dextromethorphan O-demethylation, which is a marker of CYP2D6 activity. Among the 28 herbal extracts, 13 (Cassia Bark, Clove, Coptis Rhizome, Ephedra Herb, Gambir Plant, Incised Notopterygium Rhizome, Magnolia Bark, Moutan Bark, Phellodendron Bark, Rhubarb, Sappan Wood, Sinomenium Stem, Zanthoxylum Fruit) inhibited O-demethylation by over 90%. The strongest inhibition of CYP2D6 was noted with Phellodendron Bark, which had an IC_\u003c50\u003e value of 4 μg/mL. Coptis Rhizome, Sinomenium Stem, Sappan Wood, and Rhubarb showed IC_\u003c50\u003e values of 14, 40, 52, and 64 μg/mL, respectively. These results indicate that many herbal extracts have an inhibitory effect on CYP3A4 and CYP2D6.\n 78種の生薬エキスについて,ヒト薬物代謝酵素シトクロムP450 3A4(CYP3A4)およびP450 2D6(CYP2D6)に対する阻害作用を調べた。生薬エキス粉末からメタノール可溶性画分を調製し,添加量1.65mg/mLで反応を行った。CYP3A4の指標として用いたヒト肝ミクロソーム中のエリスロマイシンN-脱メチル化活性に対して50%以上の阻害を示した生薬は31種であり,その中の8種(白芷,桂皮,丁子,羌活,牡丹皮,大黄,蘇木,五味子)が阻害率90%以上を示した。CYP3A4活性に対する阻害の強さは,蘇木,大黄,五味子,羌活,白芷の順であり,IC_\u003c50\u003e値は,それぞれ43,77,127,144および185μg/mLであった。一方,CYP2D6の指標として用いたヒト肝ミクロソーム中のデキストロメトルファンO-脱メチル化活性に対して50%以上の阻害を示した生薬は28種であり,その中の13種(桂皮,丁子,黄連,麻黄,釣藤鈎,羌活,厚朴,牡丹皮,黄柏,大黄,蘇木,防巳,山椒)が阻害率90%以上を示した。CYP2D6活性に対する阻害の強さは,黄柏,黄連,防巳,蘇木,大黄の順であり,IC_\u003c50\u003e値は各々4,14,40,52および64μg/mLであった。これらの結果から,CYP3A4あるいはCYP2D6に対する阻害活性を示す生薬が複数存在することが明らかとなった。", "subitem_description_type": "Abstract"}]}, "item_2_description_40": {"attribute_name": "資源タイプ(DSpace)", "attribute_value_mlt": [{"subitem_description": "Article", "subitem_description_type": "Other"}]}, "item_2_full_name_3": {"attribute_name": "著者別名", "attribute_value_mlt": [{"nameIdentifiers": [{"nameIdentifier": "159053", "nameIdentifierScheme": "WEKO"}], "names": [{"name": "手塚, 康弘"}]}]}, "item_2_publisher_33": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "和漢医薬学会"}]}, "item_2_rights_13": {"attribute_name": "権利", "attribute_value_mlt": [{"subitem_rights": "rights: 本文データは学協会の許諾に基づきCiNiiから複製したものである"}]}, "item_2_source_id_10": {"attribute_name": "書誌レコードID", "attribute_value_mlt": [{"subitem_source_identifier": "AA12035198", "subitem_source_identifier_type": "NCID"}]}, "item_2_source_id_8": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "18801447", "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": "Iwata, Hiroshi"}], "nameIdentifiers": [{"nameIdentifier": "159047", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Tezuka, Yasuhiro"}], "nameIdentifiers": [{"nameIdentifier": "159048", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "USIA, Tepy"}], "nameIdentifiers": [{"nameIdentifier": "159049", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kadota, Shigetoshi"}], "nameIdentifiers": [{"nameIdentifier": "159050", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hiratsuka, Akira"}], "nameIdentifiers": [{"nameIdentifier": "159051", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Watabe, Tadashi"}], "nameIdentifiers": [{"nameIdentifier": "159052", "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": "2016-02-17"}], "displaytype": "detail", "download_preview_message": "", "file_order": 0, "filename": "wakan04-tezuka.pdf", "filesize": [{"value": "1.2 MB"}], "format": "application/pdf", "future_date_message": "", "is_thumbnail": false, "licensetype": "license_free", "mimetype": "application/pdf", "size": 1200000.0, "url": {"label": "wakan04-tezuka.pdf", "url": "https://toyama.repo.nii.ac.jp/record/5245/files/wakan04-tezuka.pdf"}, "version_id": "e3a9afda-68be-40d8-90f2-122d6972eb99"}]}, "item_keyword": {"attribute_name": "キーワード", "attribute_value_mlt": [{"subitem_subject": "herb", "subitem_subject_scheme": "Other"}, {"subitem_subject": "Kampo medicines", "subitem_subject_scheme": "Other"}, {"subitem_subject": "human liver microsomes", "subitem_subject_scheme": "Other"}, {"subitem_subject": "inhibition", "subitem_subject_scheme": "Other"}, {"subitem_subject": "CYP3A4", "subitem_subject_scheme": "Other"}, {"subitem_subject": "CYP2D6", "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": "Inhibition of human liver microsomal CYP3A4 and CYP2D6 by extracts from 78 herbal medicines", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Inhibition of human liver microsomal CYP3A4 and CYP2D6 by extracts from 78 herbal medicines"}]}, "item_type_id": "2", "owner": "3", "path": ["648"], "permalink_uri": "http://hdl.handle.net/10110/1395", "pubdate": {"attribute_name": "公開日", "attribute_value": "2007-12-18"}, "publish_date": "2007-12-18", "publish_status": "0", "recid": "5245", "relation": {}, "relation_version_is_last": true, "title": ["Inhibition of human liver microsomal CYP3A4 and CYP2D6 by extracts from 78 herbal medicines"], "weko_shared_id": -1}
Inhibition of human liver microsomal CYP3A4 and CYP2D6 by extracts from 78 herbal medicines
http://hdl.handle.net/10110/1395
http://hdl.handle.net/10110/1395982b9f3e-560f-47e4-b41b-b36379fd3beb
名前 / ファイル | ライセンス | アクション |
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wakan04-tezuka.pdf (1.2 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2007-12-18 | |||||
タイトル | ||||||
タイトル | Inhibition of human liver microsomal CYP3A4 and CYP2D6 by extracts from 78 herbal medicines | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | herb | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Kampo medicines | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | human liver microsomes | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | inhibition | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | CYP3A4 | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | CYP2D6 | |||||
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 |
Iwata, Hiroshi
× Iwata, Hiroshi× Tezuka, Yasuhiro× USIA, Tepy× Kadota, Shigetoshi× Hiratsuka, Akira× Watabe, Tadashi |
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著者別名 | ||||||
姓名 | 手塚, 康弘 | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The inhibitory effects of 78 herbal extracts on cytochrome P450 3A4 (CYP3A4) and P450 2D6 (CYP2D6) activity were investigated using human liver microsomes. The incubation mixture contained a methanol soluble fraction prepared from the powder of each herbal water extract (equivalent to 1.65 mg of extract powder per mL). Thirty-one herbal extracts inhibited over 50% of human liver microsomal erythromycin N-demethylation, a marker reaction of CYP3A4 activity. Among the 31 herbal extracts, 8 of them (Angelica Dahurica Root, Cassia Bark, Clove, Incised Notopterygium Rhizome, Moutan Bark, Rhubarb, Sappan Wood, Schisandra Fruit) inhibited N-demethylation by over 90%. Among the herbal extracts examined, the strongest inhibition of CYP3A4 was noted with Sappan Wood, which had an IC_<50> value of 43 mg/mL. Rhubarb, Schisandra Fruit, Incised Notopterygium Rhizome, and Angelica Dahurica Root had IC_<50> values of 77, 127, 144, and 185 μg/mL, respectively. Further, 28 of the herbal extracts inhibited over 50% of human liver microsomal dextromethorphan O-demethylation, which is a marker of CYP2D6 activity. Among the 28 herbal extracts, 13 (Cassia Bark, Clove, Coptis Rhizome, Ephedra Herb, Gambir Plant, Incised Notopterygium Rhizome, Magnolia Bark, Moutan Bark, Phellodendron Bark, Rhubarb, Sappan Wood, Sinomenium Stem, Zanthoxylum Fruit) inhibited O-demethylation by over 90%. The strongest inhibition of CYP2D6 was noted with Phellodendron Bark, which had an IC_<50> value of 4 μg/mL. Coptis Rhizome, Sinomenium Stem, Sappan Wood, and Rhubarb showed IC_<50> values of 14, 40, 52, and 64 μg/mL, respectively. These results indicate that many herbal extracts have an inhibitory effect on CYP3A4 and CYP2D6. 78種の生薬エキスについて,ヒト薬物代謝酵素シトクロムP450 3A4(CYP3A4)およびP450 2D6(CYP2D6)に対する阻害作用を調べた。生薬エキス粉末からメタノール可溶性画分を調製し,添加量1.65mg/mLで反応を行った。CYP3A4の指標として用いたヒト肝ミクロソーム中のエリスロマイシンN-脱メチル化活性に対して50%以上の阻害を示した生薬は31種であり,その中の8種(白芷,桂皮,丁子,羌活,牡丹皮,大黄,蘇木,五味子)が阻害率90%以上を示した。CYP3A4活性に対する阻害の強さは,蘇木,大黄,五味子,羌活,白芷の順であり,IC_<50>値は,それぞれ43,77,127,144および185μg/mLであった。一方,CYP2D6の指標として用いたヒト肝ミクロソーム中のデキストロメトルファンO-脱メチル化活性に対して50%以上の阻害を示した生薬は28種であり,その中の13種(桂皮,丁子,黄連,麻黄,釣藤鈎,羌活,厚朴,牡丹皮,黄柏,大黄,蘇木,防巳,山椒)が阻害率90%以上を示した。CYP2D6活性に対する阻害の強さは,黄柏,黄連,防巳,蘇木,大黄の順であり,IC_<50>値は各々4,14,40,52および64μg/mLであった。これらの結果から,CYP3A4あるいはCYP2D6に対する阻害活性を示す生薬が複数存在することが明らかとなった。 |
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書誌情報 |
和漢医薬学雑誌 = Journal of traditional medicines 巻 21, 号 1, p. 42-50, 発行日 2004-02 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 18801447 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA12035198 | |||||
権利 | ||||||
権利情報 | rights: 本文データは学協会の許諾に基づきCiNiiから複製したものである | |||||
フォーマット | ||||||
内容記述タイプ | Other | |||||
内容記述 | application/pdf | |||||
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 | |||||
スポンサー | ||||||
内容記述タイプ | Other | |||||
内容記述 | 21st Century COE Program, Toyama Medical and Pharmaceutical University | |||||
出版者 | ||||||
出版者 | 和漢医薬学会 | |||||
資源タイプ(DSpace) | ||||||
内容記述タイプ | Other | |||||
内容記述 | Article |