NF-魏B Inhibitors from Eurycoma longifolia

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• 作者：Thi Van Anh Tran ; Clemens Malainer ; Stefan Schwaiger ; Atanas G. Atanasov ; Elke H. Heiss ; Verena M. Dirsch ; Hermann Stuppner
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：March 28, 2014
• 年：2014
• 卷：77
• 期：3
• 页码：483-488
• 全文大小：259K
• 年卷期：v.77,no.3(March 28, 2014)
• ISSN：1520-6025

文摘

The roots of Eurycoma longifolia have been used in many countries of Southeast Asia to alleviate various diseases including malaria, dysentery, sexual insufficiency, and rheumatism. Although numerous studies have reported the pharmacological properties of E. longifolia, the mode of action of the anti-inflammatory activity has not been elucidated. Bioguided isolation of NF-魏B inhibitors using an NF-魏B-driven luciferase reporter gene assay led to the identification of a new quassinoid, eurycomalide C (1), together with 27 known compounds including 11 quassinoids (2鈥?b>12), six alkaloids (13鈥?b>18), two coumarins (19, 20), a squalene derivative (21), a triterpenoid (22), and six phenolic compounds (23鈥?b>28) from the extract of E. longifolia. Evaluation of the biological activity revealed that C₁₉-type and C₂₀-type quassinoids, 尾-carboline, and canthin-6-one alkaloids are potent NF-魏B inhibitors, with IC₅₀ values in the low micromolar range, while C₁₈-type quassinoids, phenolic compounds, coumarins, the squalene derivative, and the triterpenoid turned out to be inactive when tested at a concentration of 30 渭M. Eurycomalactone (2), 14,15尾-dihydroklaieanone (7), and 13,21-dehydroeurycomanone (10) were identified as potent NF-魏B inhibitors with IC₅₀ values of less than 1 渭M.