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Synthetic cryptolepine inhibits DNA binding of NF-kappaB.

Olajide, Olumayokun A, Heiss, Elke H, Schachner, Daniel, Wright, Colin W, Vollmar, Angelika M and Dirsch, Verena M (2007) Synthetic cryptolepine inhibits DNA binding of NF-kappaB. Bioorganic & medicinal chemistry, 15 (1). pp. 43-49. ISSN 0968-0896

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The alkaloid cryptolepine is thought to mediate the anti-inflammatory effects of the climbing shrub, Cryptolepis sanguinoleta. The underlying mechanism of action, however, is largely unknown. In the present study, we show that the synthetic cryptolepine-hydrochloride (2.5-10microM) dose-dependently inhibits lipopolysaccharide (LPS)-induced nitric oxide production in the murine macrophage cell line RAW 264.7. We furthermore demonstrate a strong inhibition of nuclear factor (NF)-kappaB, a transcription factor primarily involved in inflammatory and immune responses, by cryptolepine (2.5-10microM) using a luciferase reporter gene assay in human HEK 293 cells. Examining the individual steps of NF-kappaB activation in the presence of cryptolepine we could exclude an inhibitory effect on degradation of IkappaB or nuclear translocation of NF-kappaB by the alkaloid. However, EMSA of nuclear extracts from LPS-activated RAW cells revealed reduced DNA binding activity of NF-kappaB by cryptolepine in vivo and in vitro. This indicates that cryptolepine may exhibit its anti-inflammatory action by blocking DNA binding of activated NF-kappaB and thus transcription of NF-kappaB-regulated proinflammatory proteins.

Item Type: Article
Subjects: R Medicine > RM Therapeutics. Pharmacology
Schools: School of Applied Sciences
Related URLs:
Depositing User: Olumayokun Olajide
Date Deposited: 10 Nov 2010 10:21
Last Modified: 28 Aug 2021 11:01


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