Isolation of Arginase Inhibitors from the Bioactivity-Guided Fractionation of Byrsonima coccolobifolia Leaves and Stems
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- 作者：Lorena Ramos Freitas de Sousa ; Suelem Demuner Ramalho ; Marcela Carmen de Melo Burger ; Liliane Nebo ; Jo茫o Batista Fernandes ; Maria F谩tima das Gra莽as Fernandes da Silva ; M么nica Rosas da Costa Iemma ; Caroindes Julia Corr锚a ; Dulce Helena Ferreira de Souza ; Maria In锚s Salgueiro Lima ; Paulo Cezar Vieira
- 刊名：Journal of Natural Products
- 出版年：2014
- 出版时间：February 28, 2014
- 年：2014
- 卷：77
- 期：2
- 页码：392-396
- 全文大小：255K
- 年卷期：v.77,no.2(February 28, 2014)
- ISSN：1520-6025
文摘
Byrsonima coccolobifolia leaf and stem extracts were studied in the search for possible leishmanicidal compounds using arginase (ARG) from Leishmania amazonensis as a molecular target. Flavonoids 1b, 1e鈥?b>1g, 2a, 2b, and 2d鈥?b>2f showed significant inhibitory activity, with IC50 values ranging from 0.9 to 4.8 渭M. The kinetics of the most active compounds were determined. Flavonoids 1e, 1f, 2a, 2b, and 2e were characterized as noncompetitive inhibitors of ARG with dissociation constants (Ki) ranging from 0.24 to 3.8 渭M, demonstrating strong affinity. Structure鈥揳ctivity relationship studies revealed some similarities in the structural features of flavonoids related to ARG activity.