Topical Apigenin Alleviates Cutaneous Inflammation in Murine Models

Dermatology Service, Veterans Affairs Medical Center and Department of Dermatology, University of California, San Francisco, 4150 Clement Street, San Francisco, CA 94121, USA.
Evidence-based Complementary and Alternative Medicine (Impact Factor: 1.88). 11/2012; 2012(11):912028. DOI: 10.1155/2012/912028
Source: PubMed


Herbal medicines have been used in preventing and treating skin disorders for centuries. It has been demonstrated that systemic administration of chrysanthemum extract exhibits anti-inflammatory properties. However, whether topical applications of apigenin, a constituent of chrysanthemum extract, influence cutaneous inflammation is still unclear. In the present study, we first tested whether topical applications of apigenin alleviate cutaneous inflammation in murine models of acute dermatitis. The murine models of acute allergic contact dermatitis and acute irritant contact dermatitis were established by topical application of oxazolone and phorbol 12-myristate 13-acetate (TPA), respectively. Inflammation was assessed in both dermatitis models by measuring ear thickness. Additionally, the effect of apigenin on stratum corneum function in a murine subacute allergic contact dermatitis model was assessed with an MPA5 physiology monitor. Our results demonstrate that topical applications of apigenin exhibit therapeutic effects in both acute irritant contact dermatitis and allergic contact dermatitis models. Moreover, in comparison with the vehicle treatment, topical apigenin treatment significantly reduced transepidermal water loss, lowered skin surface pH, and increased stratum corneum hydration in a subacute murine allergic contact dermatitis model. Together, these results suggest that topical application of apigenin could provide an alternative regimen for the treatment of dermatitis.

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Available from: Richard Sun, May 13, 2014
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    • "In the recent past, several studies reported the mitigation of matrix metalloproteinases (MMPs) expression by apigenin in target cells, which is induced by several agents such as carcinogens, ultraviolet A (UVA 320–400 nm), phorbol myristate acetate (PMA), interleukin-1 beta (IL-1β) and tumor necrosis factor-alpha (TNF-α) [18]–[21]. Further, inhibitory action of apigenin or apigenin structural analogues against cutaneous inflammation and infection-induced inflammation is also demonstrated [22], [23]. However, no study claims the SVMP inhibitory efficacy of apigenin or derivatives having apigenin nucleus. "
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    ABSTRACT: The classical antivenom therapy has appreciably reduced snakebite mortality rate and thus is the only savior drug available. Unfortunately, it considerably fails to shield the viper bite complications like hemorrhage, local tissue degradation and necrosis responsible for severe morbidity. Moreover, the therapy is also tagged with limitations including anaphylaxis, serum sickness and poor availability. Over the last decade, snake venom metalloproteases (SVMPs) are reported to be the primary component responsible for hemorrhage and tissue degradation at bitten site. Thus, antivenom inability to offset viper venom-induced local toxicity has been a basis for an insistent search for SVMP inhibitors. Here we report the inhibitory effect of compound 5d, an apigenin based molecule against SVMPs both in silico and in vivo. Several apigenin analogues are synthesized using multicomponent Ugi reactions. Among them, compound 5d effectively abrogated Echis carinatus (EC) venom-induced local hemorrhage, tissue necrosis and myotoxicity in a dose dependant fashion. The histopathological study further conferred effective inhibition of basement membrane degradation, and accumulation of inflammatory leucocytes at the site of EC venom inoculation. The compound also protected EC venom-induced fibrin and fibrinogen degradation. The molecular docking of compound 5d and bothropasin demonstrated the direct interaction of hydroxyl group of compound with Glu146 present in hydrophobic pocket of active site and does not chelate Zn2+. Hence, it is concluded that compound 5d could be a potent agent in viper bite management.
    PLoS ONE 09/2014; 9(9):e106364. DOI:10.1371/journal.pone.0106364 · 3.23 Impact Factor
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    • "Recently apigenin was demonstrated to possess healing effect in both acute irritant dermatitis and contact dermatitis models on topical application (Man et al., 2012). More recently Byun et al. (2013) showed that apigenin exerts potent chemopreventive activity against UVB-induced skin inflammations primarily by targeting Src-kinase. "
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    ABSTRACT: ETHNOPHARMACOLOGICAL RELEVANCE: In Turkish traditional medicine, the flowers of Helichrysum graveolens (Bieb.) Sweet (Asteraceae) has been used for the treatment of jaundice, for wound-healing and as a diuretic. AIM OF THE STUDY: In order to find scientific evidence for the traditional utilization of this plant in wound-healing, the effect of the plant extract was investigated by using in vivo and in vitro experimental models. Then through bioassay-guided fractionation procedures active wound-healing component(s) was isolated and its possible role in the wound-healing process was also determined. MATERIAL AND METHODS: The linear incision and the circular excision wound models were applied in order to evaluate in vivo wound-healing potential of H. graveolens. Anti-inflammatory and antioxidant activities, which are known to involve in wound-healing process, were also assessed by the Whittle method and the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical-scavenging assay, respectively. The total phenolic content of the crude extract and solvent fractions was estimated to find correlation between the phenolic content and the antioxidant activity. Combined application of the chromatographic separation techniques on sephadex and silica gel columns, and bioassay techniques have yielded the active wound-healing principle of H. graveolens. Moreover, in vitro inhibitory effect of active principle on hyaluronidase, collagenase and elastase enzymes were investigated to explore the activity pathways. RESULTS: The 85% methanol (MeOH) extract of H. graveolens flowers displayed significant wound-healing, anti-inflammatory and antioxidant activities. Then the crude extract was partitioned by successive solvent extractions, in increasing polarity, to give five solvent fractions. Among the solvent fractions, the ethyl acetate (EtOAc) fraction exerted the highest activity. The EtOAc fraction was further subjected to chromatographic separations to yield active constituent and its structure was elucidated to be apigenin by spectrometric methods. Further in vivo and in vitro assays revealed that apigenin was one of the components responsible for the wound-healing effect of the plant remedy and also found to possess significant anti-inflammatory, antioxidant, anti-hyaluronidase and anti-collagenase activities. CONCLUSION: Present study supported the traditional use of H. graveolens flowers for wound-healing and through bioassay-guided fractionation procedures from the crude extract apigenin was isolated as one of the active components.
    Journal of ethnopharmacology 06/2013; 149(1). DOI:10.1016/j.jep.2013.06.006 · 3.00 Impact Factor
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    • "Recently apigenin was demonstrated to possess healing effect in both acute irritant dermatitis and contact dermatitis models on topical application (Man et al., 2012). More recently Byun et al. (2013) showed that apigenin exerts potent chemopreventive activity against UVB-induced skin inflammations primarily by targeting Src-kinase. "
    Planta Medica 08/2011; 77(12). DOI:10.1055/s-0031-1282419 · 2.15 Impact Factor
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