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In this study, a variety of Japanese traditional herbal medicine (\u0027Kampo\u0027) were examined for their potential anti-malarial activities. METHODS: A comprehensive screening methods were designed to identify novel anti-malarial drugs from a library of Kampo herbal extracts (n?=?120) and related compounds (n?=?96). The anti-malarial activity was initially evaluated in vitro against chloroquine/mefloquine-sensitive (3D7) and-resistant (Dd2) strains of Plasmodium falciparum. The cytotoxicity was also evaluated using primary adult mouse brain cells. After being selected through the first in vitro assay, positive extracts and compounds were examined for possible in vivo anti-malarial activity. RESULTS: Out of 120 herbal extracts, Coptis rhizome showed the highest anti-malarial activity (IC50 1.9 μg/mL of 3D7 and 4.85 μg/mL of Dd2) with a high selectivity index (SI)?\u003e?263 (3D7) and?\u003e?103 (Dd2). Three major chlorinated compounds (coptisine, berberine, and palmatine) related to Coptis rhizome also showed anti-malarial activities with IC50 1.1, 2.6, and 6.0 μM (against 3D7) and 3.1, 6.3, and 11.8 μM (against Dd2), respectively. Among them, coptisine chloride exhibited the highest anti-malarial activity (IC50 1.1 μM against 3D7 and 3.1 μM against Dd2) with SI of 37.8 and 13.2, respectively. Finally, the herbal extract of Coptis rhizome and its major active compound coptisine chloride exhibited significant anti-malarial activity in mice infected with Plasmodium yoelii 17X strain with respect to its activity on parasite suppression consistently from day 3 to day 7 post-challenge. The effect ranged from 50.38 to 72.13% (P?\u003c?0.05) for Coptis rhizome and from 81 to 89% (P?\u003c?0.01) for coptisine chloride. CONCLUSION: Coptis rhizome and its major active compound coptisine chloride showed promising anti-malarial activity against chloroquine-sensitive (3D7) and -resistant (Dd2) strains in vitro as well as in vivo mouse malaria model. 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Anti-malarial activity of traditional Kampo medicine Coptis rhizome extract and its major active compounds
http://hdl.handle.net/10069/40070
http://hdl.handle.net/10069/400708eb09c39-b793-4bfd-94e3-0a00b48278e9
名前 / ファイル | ライセンス | アクション |
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MalJou16_204.pdf (1.5 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2020-06-29 | |||||
タイトル | ||||||
タイトル | Anti-malarial activity of traditional Kampo medicine Coptis rhizome extract and its major active compounds | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Herbal medicine | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Kampo | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Antimalarial | |||||
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 |
Teklemichael, Awet Alem
× Teklemichael, Awet Alem× Mizukami, Shusaku× Toume, Kazufumi× Mosaddeque, Farhana× Kamel, Mohamed Gomaa× Kaneko, Osamu× Komatsu, Katsuko× Karbwang, Juntra× Huy, Nguyen Tien× Hirayama, Kenji |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | BACKGROUND: Herbal medicine has been a rich source of new drugs exemplified by quinine and artemisinin. In this study, a variety of Japanese traditional herbal medicine ('Kampo') were examined for their potential anti-malarial activities. METHODS: A comprehensive screening methods were designed to identify novel anti-malarial drugs from a library of Kampo herbal extracts (n?=?120) and related compounds (n?=?96). The anti-malarial activity was initially evaluated in vitro against chloroquine/mefloquine-sensitive (3D7) and-resistant (Dd2) strains of Plasmodium falciparum. The cytotoxicity was also evaluated using primary adult mouse brain cells. After being selected through the first in vitro assay, positive extracts and compounds were examined for possible in vivo anti-malarial activity. RESULTS: Out of 120 herbal extracts, Coptis rhizome showed the highest anti-malarial activity (IC50 1.9 μg/mL of 3D7 and 4.85 μg/mL of Dd2) with a high selectivity index (SI)?>?263 (3D7) and?>?103 (Dd2). Three major chlorinated compounds (coptisine, berberine, and palmatine) related to Coptis rhizome also showed anti-malarial activities with IC50 1.1, 2.6, and 6.0 μM (against 3D7) and 3.1, 6.3, and 11.8 μM (against Dd2), respectively. Among them, coptisine chloride exhibited the highest anti-malarial activity (IC50 1.1 μM against 3D7 and 3.1 μM against Dd2) with SI of 37.8 and 13.2, respectively. Finally, the herbal extract of Coptis rhizome and its major active compound coptisine chloride exhibited significant anti-malarial activity in mice infected with Plasmodium yoelii 17X strain with respect to its activity on parasite suppression consistently from day 3 to day 7 post-challenge. The effect ranged from 50.38 to 72.13% (P?<?0.05) for Coptis rhizome and from 81 to 89% (P?<?0.01) for coptisine chloride. CONCLUSION: Coptis rhizome and its major active compound coptisine chloride showed promising anti-malarial activity against chloroquine-sensitive (3D7) and -resistant (Dd2) strains in vitro as well as in vivo mouse malaria model. Thus, Kampo herbal medicine is a potential natural resource for novel anti-malarial agents. | |||||
書誌情報 |
Malaria Journal 巻 19, 号 1, p. 204, 発行日 2020-06-08 |
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出版者 | ||||||
出版者 | BioMed Central Ltd. | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 14752875 | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1186/s12936-020-03273-x | |||||
権利 | ||||||
権利情報 | c The Author(s) 2020. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated in a credit line to the data. | |||||
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 | Malaria journal, 19(1), p.204; 2020 |