Physalins from Witheringia solanacea as modulators off the NF-κB cascade

被引:49
作者
Jacobo-Herrera, NJ
Bremner, P
Márquez, N
Gupta, MP
Gibbons, S
Muñoz, E
Heinrich, M
机构
[1] Univ London, Sch Pharm, Ctr Pharmacognosy & Phytotherapy, London WC1N 1AX, England
[2] Univ Cordoba, Dept Biol Celular Fisiol & Inmunol, Cordoba, Spain
[3] Univ Panama, Fac Farm, CIFLORPAN, Panama City, Panama
来源
JOURNAL OF NATURAL PRODUCTS | 2006年 / 69卷 / 03期
关键词
D O I
10.1021/np050225t
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Crude extracts of Witheringia solanacea leaves showed inhibition of NF-KB activation at 100 mu g/mL induced by phorbol 12-myristate-13-acetate (PMA) in HeLa cells stably transfected with a luciferase reporter gene controlled by the IL-6 promoter. Three physalins were isolated from an active fraction, namely, physalins B (1), F (2), and D (3). Of these compounds, 1 and 2 demonstrated inhibitory activities on PMA-induced NF-KB activation at 16 and 8 mu M and induced apoptosis after 24 h in a cell-cycle analysis using a human T cell leukemia Jurkat cell line. Compound 2 also inhibited TNF-alpha-induced NF-KB activation at 5 mu M through the canonical pathway, but was inactive in the Tet-On-Luc assay, indicating specificity of action, although it interfered with Tet-On-Luc at higher concentrations. It is suggested that the presence of a double bond and an epoxy ring between carbons 5 and 6 in compounds 1 and 2, respectively (which are not present in compound 3), are related to their anti-inflammatory activity.
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页码:328 / 331
页数:4
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