2010年8月
In Vitro Leishmanicidal Activity of Benzophenanthridine Alkaloids from Bocconia pearcei and Related Compounds
CHEMICAL & PHARMACEUTICAL BULLETIN
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- 巻
- 58
- 号
- 8
- 開始ページ
- 1047
- 終了ページ
- 1050
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1248/cpb.58.1047
- 出版者・発行元
- PHARMACEUTICAL SOC JAPAN
Leishmanicidal activities of benzophenanthridine alkaloids isolated from fruits of Bocconia pearcei and their derivatives were examined. Seven benzophenanthridine compounds were isolated from the methanolic extracts of B. pearcei. Among them, dihydrosanguinarine showed the most potent leishmanicidal activities (IC50 value: 0.014 mu g/ml, respectively). To examine the structure activity relationship of the benzophenanthridine skeleton, the leishmanicidal activities for 32 synthetic samples were examined. The existence of bulky groups at the C-7-C-8 position was found to enhance the activity. On the other hand, the bulkiness at the C-2-C-3 position on the D-ring, a carbonyl group at C-6, substitution at C-6 and cleavage or saturation of the C-5-C-6 bond reduced activity. A methyl group on nitrogen of the C-ring was thought to be necessary for significant activity.
- リンク情報
- ID情報
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- DOI : 10.1248/cpb.58.1047
- ISSN : 0009-2363
- PubMed ID : 20686258
- Web of Science ID : WOS:000280373800009