Natural Compound Cudraflavone B Shows Promising Anti-inflammatory Properties in Vitro

Abstract

Cudraflavone B (1) is a prenylated flavonoid found in large amounts in the roots of Morus alba, a plant used as a herbal remedy for its reputed anti-inflammatory properties. The present study shows that this compound causes a significant inhibition of inflammatory mediators in selected in vitro models. Thus, 1 was identified as a potent inhibitor of tumor necrosis factor α (TNFα) gene expression and secretion by blocking the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages derived from a THP-1 human monocyte cell line. The NF-κB activity reduction resulted in the inhibition of cyclooxygenase 2 (COX-2) gene expression. Compound 1 acts as a COX-2 and COX-1 inhibitor with higher selectivity toward COX-2 than indomethacin. Pretreatment of cells by 1 shifted the peak in an regulatory gene zinc-finger protein 36 (ZFP36) expression assay. This natural product has noticeable anti-inflammatory properties, suggesting that 1 potentially could be used for development as a nonsteroidal anti-inflammatory drug lead.

Therapeutic Impact of Berries (Morus Alba and Morus Rubra) Fruit Extract in the Regression of High-Fat Diet-Induced Cardiac Dysfunction in Rats

“…It was a powerful TNF-a inhibitor by preventing the NF-kB translocation from the cytoplasm to the nucleus. The NF-Kb inhibition activity leads to an inhibition in the gene expressions of COX-2 [40,41]. Resveratrol purified from MA inhibits a secretion of IL-8 by blocking phosphorylation of MAPK and activation of NF-kappa B in LPSinduced human monocytic cell line THP-1 [38,42].…”

C-Geranylated Flavanones from Paulownia tomentosa Fruits as Potential Anti-inflammatory Compounds Acting via Inhibition of TNF-α Production

“…Eriodictyol (24) and naringenin (25) were used as non-prenylated flavanones for anti-inflammatory potential testing and were obtained from Sigma-Aldrich, with declared purity exceeding 95%.…”

“…Its molecular formula was determined by HRESIMS to be C 25 , 441.1913). The signals of oxygen-bearing carbons (δ C 72.3 and 77.5) were again present, but the observed HMBC correlations indicated that oxidation took place in a different part of the chain than in compounds 1−3.…”

“…Its molecular formula was determined by HRESIMS to be C 25 The aromatic protons of the flavonoid ring B were represented by the presence of a singlet at δ H 6.79 (2H), indicating a 3′,4′,5′-trisubstituted ring. Two equal methoxy groups at δ H 3.88 (s, 6H) were assigned to carbons C-3′ and C-5′, respectively, on the basis of the NOESY cross-peak with H-2′ and H-6′, and the hydroxy group was assigned to C-4′.…”

“…The anti-inflammatory activity of flavonoids has long been well known. The production of a typical pro-inflammatory cytokine TNF-α in lipopolysaccharide (LPS)-stimulated macrophages was used to determine the ability of compounds 1−23 isolated from P. tomentosa, along with eriodictyol (24) and naringenin (25), to attenuate the production of this cytokine ( Figure 1). As can be seen, several compounds affected the production of TNF-α in a statistically significant manner (p < 0.001).…”