In Vitro Leishmanicidal Activity of Benzophenanthridine Alkaloids from Bocconia pearcei and Related Compounds

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概要

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• 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–C3 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.

著者

• Fuchino Hiroyuki

  Research Center for Medicinal Plant Resources, National Institute of Biomedical Innovation

• Kawano Marii

  Faculty of Pharmaceutical Sciences, Josai International University

• Mori-Yasumoto Kanami

  Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokush

• Sekita Setsuko

  Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokush

• Satake Motoyoshi

  Institute of Environmental Science for Human Life, Ochanomizu University

• Ishikawa Tsutomu

  Faculty of Pharmaceutical Sciences, Chiba University

• Kiuchi Fumiyuki

  Faculty of Pharmacy, Keio University

• Kawahara Nobuo

  Research Center for Medicinal Plant Resources, National Institute of Biomedical Innovation

• Kuroyanagi M

  Fac. Of Pharmaceutical Sciences At Kagawa Campus Tokushima Bunri Univ.

• Fuchino H

  Sci. Univ. Tokyo Tokyo Jpn

• Fuchino Hiroyuki

  Research Center For Medicinal Plant Resources National Institute Of Biomedical Innovation

• Satake Motoyoshi

  Institute Of Environmental Science For Human Life Ochanomizu University

• Kiuchi Fumiyuki

  Faculty Of Pharmaceutical Sciences Kanazawa University

• Ishikawa Tsutomu

  Faculty Of Pharmaceutical Sciences Chiba University

• Fuchino Hiroyuki

  Res. Center For Medicinal Plant Resources National Inst. Of Biomedical Innovation

• Kuroyanagi Masanori

  Fac. Of Pharmaceutical Sciences At Kagawa Campus Tokushima Bunri Univ.

• Kimura Mariko

  Fac. Of Food Culture Dep. Of Nutrition Kurashiki Sakuyo Univ.

• Fuchino H

  Research Center For Medicinal Plant Resources National Institute Of Biomedical Innovation

• Sekita Setsuko

  Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University

• Mori-Yasumoto Kanami

  Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University

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