Structure–activity relationships of flavanones, flavanone glycosides, and flavones in anti-degranulation activity in rat basophilic leukemia RBL-2H3 cells

Abstract

The incidence of type I allergies, which are associated with mast cell degranulation and local inflammation, is increasing, and new treatments are needed. To date, structure–activity relationships of flavonoids in their degranulation-inhibiting activity have not been systematically characterized. In the current study, the degranulation-inhibiting activity of a series of flavonoids was evaluated. The following three observations were made: (1) the activity disappears when a sugar moiety is introduced into the A ring of the flavanone; (2) the activity depends on the number of hydroxyl groups on the B ring; (3) the activity is markedly enhanced when a double bond is introduced into the C ring. The information obtained in the current study may guide the development of a therapy for type I allergies.

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Acknowledgements

The authors would like to thank Editage (http://www.editage.jp) for English language editing.

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Correspondence to Toshiro Noshita or Akihiro Tai.

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Noshita, T., Miura, K., Ikeda, K. et al. Structure–activity relationships of flavanones, flavanone glycosides, and flavones in anti-degranulation activity in rat basophilic leukemia RBL-2H3 cells. J Nat Med 72, 551–556 (2018). https://doi.org/10.1007/s11418-017-1169-3

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Keywords

  • Flavonoids
  • Anti-degranulation
  • Type I allergy
  • Structure–activity relationship
  • Rat basophilic leukemia RBL-2H3 cell