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Evaluation of the antiplasmodial efficacy of synthetic 2,5-diphenyloxazole analogs of compounds naturally derived from Oxytropis lanata
https://obihiro.repo.nii.ac.jp/records/2000201
https://obihiro.repo.nii.ac.jp/records/2000201be6a7fce-c6f2-4e20-8d03-361ab2da0e03
名前 / ファイル | ライセンス | アクション |
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Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||
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公開日 | 2024-05-20 | |||||||||||
タイトル | ||||||||||||
タイトル | Evaluation of the antiplasmodial efficacy of synthetic 2,5-diphenyloxazole analogs of compounds naturally derived from Oxytropis lanata | |||||||||||
言語 | en | |||||||||||
言語 | ||||||||||||
言語 | eng | |||||||||||
キーワード | ||||||||||||
言語 | en | |||||||||||
主題Scheme | Other | |||||||||||
主題 | 2,5-Diphenyloxazoles | |||||||||||
キーワード | ||||||||||||
言語 | en | |||||||||||
主題Scheme | Other | |||||||||||
主題 | Antiplasmodial | |||||||||||
キーワード | ||||||||||||
言語 | en | |||||||||||
主題Scheme | Other | |||||||||||
主題 | Plasmodium falciparum | |||||||||||
キーワード | ||||||||||||
言語 | en | |||||||||||
主題Scheme | Other | |||||||||||
主題 | Plasmodium yoelii | |||||||||||
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 |
Ariefta, Nanang R.
× Ariefta, Nanang R.× Narita, Koichi
× Murata, Toshihiro× 西川, 義文
WEKO
176
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抄録 | ||||||||||||
内容記述タイプ | Other | |||||||||||
内容記述 | The persistent prevalence and dissemination of drug-resistant malaria parasites continue to challenge the progress of malaria eradication efforts. As a result, there is an urgent need to search for and develop innovative therapies. In this study, we screened synthetic 2,5-diphenyloxazole analogs from Oxytropis lanata. Among 48 compounds, 14 potently inhibited the proliferation of P. falciparum strains 3D7 (chloroquine-sensitive) and K1 (multidrug-resistant) in vitro, exhibited IC50 values from 3.38 to 12.65 μM and 1.27–6.19 μM, respectively, and were toxic to human foreskin fibroblasts at 39.53–336.35 μM. Notably, Compounds 31 (2-(2′,3′-dimethoxyphenyl)-5-(2″-hydroxyphenyl)oxazole) and 32 (2-(2′,3′-dimethoxyphenyl)-5-(2″-benzyloxyphenyl)oxazole) exhibited the highest selectivity indices (SIs) against both P. falciparum strains (3D7/K1), with values > 40.20/>126.58 and > 41.27/> 59.06, respectively. In the IC50 speed and stage-specific assays, Compounds 31 and 32 showed slow action, along with distinct effects on the ring and trophozoite stages. Microscopy observations further revealed that both compounds impact the development and delay the progression of the trophozoite and schizont stages in P. falciparum 3D7, especially at concentrations 100 times their IC50 values. In a 72-h in vitro exposure experiment at their respective IC80 in P. falciparum 3D7, significant alterations in parasitemia levels were observed compared to the untreated group. In Compound 31-treated cultures, parasites shrank and were unable to reinvade red blood cells (RBCs) during an extended 144-h incubation period, even after compound removal from the culture. In vivo assessments were conducted on P. yoelii 17XNL-infected mice treated with Compounds 31 and 32 at 20 mg/kg administered once daily for ten days. The treated groups showed statistically significant lower peaks of parasitemia (Compound 31-treated: trial 1 12.7%, trial 2 15.8%; Compound 32-treated: trial 1 12.7%, trial 2 14.0%) compared to the untreated group (trial 1 21.7%, trial 2 28.3%). These results emphasize the potential of further developing 2,5-diphenyloxazoles as promising antimalarial agents. | |||||||||||
言語 | en | |||||||||||
書誌情報 |
en : International Journal for Parasitology: Drugs and Drug Resistance 巻 25, 発行日 2024-08 |
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出版者 | ||||||||||||
出版者 | Elsevier | |||||||||||
言語 | en | |||||||||||
ISSN | ||||||||||||
収録物識別子タイプ | EISSN | |||||||||||
収録物識別子 | 22113207 | |||||||||||
PubMed番号 | ||||||||||||
関連タイプ | isIdenticalTo | |||||||||||
識別子タイプ | PMID | |||||||||||
関連識別子 | 38676995 | |||||||||||
DOI | ||||||||||||
関連タイプ | isIdenticalTo | |||||||||||
識別子タイプ | DOI | |||||||||||
関連識別子 | https://doi.org/10.1016/j.ijpddr.2024.100540 | |||||||||||
権利 | ||||||||||||
言語 | en | |||||||||||
権利情報 | © 2024 The Authors | |||||||||||
フォーマット | ||||||||||||
内容記述タイプ | Other | |||||||||||
内容記述 | application/pdf | |||||||||||
言語 | en | |||||||||||
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 | |||||||||||
日本十進分類法 | ||||||||||||
言語 | ja | |||||||||||
主題Scheme | NDC | |||||||||||
主題 | 649 |