In vitro leishmanicidal activity of benzophenanthridine alkaloids from Bocconia pearcei and related compounds

Hiroyuki Fuchino, Marii Kawano, Kanami Mori-Yasumoto, Setsuko Sekita, Motoyoshi Satake, Tsutomu Ishikawa, Fumiyuki Kiuchi, Nobuo Kawahara

研究成果: Article査読

32 被引用数 (Scopus)

抄録

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 μg/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 C7-C8 position was found to enhance the activity. On the other hand, the bulkiness at the C2-C 3 position on the D-ring, a carbonyl group at C-6, substitution at C-6 and cleavage or saturation of the C5-C6 bond reduced activity. A methyl group on nitrogen of the C-ring was thought to be necessary for significant activity.

本文言語English
ページ(範囲)1047-1050
ページ数4
ジャーナルChemical and Pharmaceutical Bulletin
58
8
DOI
出版ステータスPublished - 2010 8

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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