論文 - 詳細
| RRC ID | 45265 |
|---|---|
| 著者 | Tung NH, Suzuki M, Uto T, Morinaga O, Kwofie KD, Ammah N, Koram KA, Aboagye F, Edoh D, Yamashita T, Yamaguchi Y, Setsu T, Yamaoka S, Ohta N, Shoyama Y. |
| タイトル | Anti-trypanosomal activity of diarylheptanoids isolated from the bark of Alnus japonica. |
| ジャーナル | Am J Chin Med |
| Abstract |
The crude extract of Alnus japonica bark exhibited a strong effect on the growth of Trypanosoma brucei. Subsequent chromatographic separation resulted in the isolation of two novel diarylheptanoids, known as alnuside C (2) and alnuside D (3), and three known compounds, 1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)-heptan-3(R)-O-β-D-glucopyranoside (1), oregonin (4) and hirsutanone (5). The structures of the isolates were elucidated based on the use of extensive spectroscopic and chemical methods. Among the isolated diarylheptanoids, oregonin (4) (a major component of plant bark) and hirsutanone (5) exhibited potent in vitro inhibitory activity against T. brucei growth in the bloodstream with IC50 values of 1.14 and 1.78 μM, respectively. We confirmed that oregonin (4) and hirsutanone (5) were not toxic to human normal skin fibroblast cells (NB1RGB) and colon cancer cells (HCT-15) at a concentration of 50 μM; however, lower levels of toxicity were observed for leukemia cells. To determine the structure activity relationships of the isolated components, we performed Conformation Search and found that the 3-oxo function of the heptane chain in the diarylheptanoid molecule is required for their trypanocidal activity. |
| 巻・号 | 42(5) |
| ページ | 1245-60 |
| 公開日 | 2014-1-1 |
| DOI | 10.1142/S0192415X14500785 |
| PMID | 25178281 |
| MeSH | Alnus* Animals Cells, Cultured Colonic Neoplasms / pathology Diarylheptanoids / chemistry Diarylheptanoids / isolation & purification Diarylheptanoids / pharmacology* Dose-Response Relationship, Drug Fibroblasts / drug effects Humans In Vitro Techniques Leukemia / pathology Plant Bark Plant Extracts / chemistry Plant Extracts / pharmacology* Plant Extracts / toxicity Skin / cytology Structure-Activity Relationship Trypanocidal Agents* Trypanosoma brucei brucei / drug effects* Trypanosoma brucei brucei / growth & development* Tumor Cells, Cultured |
| IF | 3.682 |
| 引用数 | 10 |
| WOS 分野 | INTEGRATIVE & COMPLEMENTARY MEDICINE |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Policy sources |
| 各媒体での言及数の合計 | 2 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | Jurkat U937 HL60(RCB0041) THP-1(RCB1189) NB1RGB(RCB0222) |