Inhibitor for FcεRI expression on mast cell from Verbasucum thapsus L

  • Bioorg Med Chem Lett. 2018 Nov 1;28(20):3342-3345. doi: 10.1016/j.bmcl.2018.09.007.
Satoru Tamura  1 ,  Kunichika Yoshihira  2 ,  Tomikazu Kawano  3 ,  Nobutoshi Murakami  2
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Osaka University, Japan; School of Pharmacy, Iwate Medical University, Japan. Electronic address: [email protected].
  • 2. Graduate School of Pharmaceutical Sciences, Osaka University, Japan.
  • 3. School of Pharmacy, Iwate Medical University, Japan.
PMID: 30217416 DOI: 10.1016/j.bmcl.2018.09.007
Abstract

We found out 2',3'-dihydroxypuberulin from South American medicinal plant, V. thapsus L., as a candidate of an anti-allergic lead which inhibits the expression of high-affinity receptor of IgE (FcεRI) on the surface of mast cells. Furthermore, the analysis of structure-activity relationship by using synthesized 2',3'-dihydroxypuberulin analogs revealed that both hydroxy groups in the side chain and both of methyl moieties on phenolic hydroxy groups were crucial for potent activity, but absolute configuration of C-3' position wasn't. The active principle, 2',3'-dihydroxypuberulin, was disclosed to down-regulate the mRNA level of β-chain of FcεRI, different from previous reported active natural product reducing γ-chain level.

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