Abstract

Interest has developed in natural molecules due to their clinically proven effects on skin diseases. Flavanones display several biological activities, and recently have been the focus of studies due to their anti-inflammatory effect. To improve their pharmacological profile, four flavanones (A, B, C, and D) were synthesized by structural modification of one natural flavanone 1 (semi-systematic name: (2S)-5,7-dihydroxy-6-prenylflavanone) extracted from Eysenhardtia platycarpa. The hydroalcoholic flavanone solutions (FS) were assayed to investigate their anti-inflammatory effect on two in vivo cutaneous inflammation models. Materials and methods: the topical anti-inflammatory effects of FS were evaluated against models of 12-O-tetradecanoylphorbol acetate (TPA)-induced mouse ear edema and arachidonic acid (AA) in rat ear edema. Results: The vinylogous cyclized derivative (flavanone D) caused edema inhibition in the TPA-induced models with an inhibition of 96.27 ± 1.93%; equally effective and potent in inhibiting the mouse ear edema as indomethacin had been. In addition, the AA-induced increase in ear thickness was reduced the most by the topical application of modulated ether (flavanone B). Conclusions: The in vivo and histology results suggest that flavanones B and D are effective as topical anti-inflammatory agents in inflammatory processes. Thus, this new compound represents a promising agent for the management of skin diseases with an inflammatory component.

Highlights

  • Model of Mice Ear Inflammation Induced with tetradecanoylphorbol acetate (TPA)

  • The anti-inflammatory study results of the flavanones are depicted in Table 1 as mean values ± the standard deviation (SD)

  • The flavanone natural 1 revealed a significant reduction of the dermal edema with inhibition percentage of 66.67 ± 1.55

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Summary

Introduction

There are widespread dermatological diseases that include inflammatory responses in the skin and can present different ranges in severity. It is manifested by swelling, redness, heat, and pain in the affected tissue [1]. Natural products for human skin problems have been used since ancient times They have gathered considerable attention as new anti-inflammatory compounds because their long-established usage promises the development of safe and effective medicaments [3]. Flavanones have been the focus of much research and development due to their several biological activities, including anti-inflammatory effects [4] They have been a potential source in the search for lead compounds and biologically active components [5]. The therapeutic efficacy of flavanones was checked by 12-O-tetradecanoylphorbol acetate (TPA)

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