Daurichromenic Acid from the Chinese Traditional Medicinal Plant Rhododendron dauricum Inhibits Sphingomyelin Synthase and Aβ Aggregation

• HADAY, Virupaksha Deepak

• MAHADEVA, M. M. Swamy

• MURAI, Yuta

• SUGA, Yoshiko

• ANETAI, Masaki

• YO, Takuro

• KURAGANO, Masahiro

• UWAI, Koji

• TOKURAKU, Kiyotaka

• MONDE, Kenji

Abstract

Species of the genus Rhododendron have been used in traditional Chinese medicine, with the medicinal herb “Manshanfong” used as an expectorant and for the treatment of acute bronchitis. Daurichromenic acid (DCA), a constituent of Rhododendron dauricum, is a meroterpenoid with antibacterial, anti-HIV, and anti-inflammatory activities. However, the mechanisms underlying these pharmacologic activities are poorly understood. To develop new drugs based on DCA, more information is required regarding its interactions with biomolecules. The present study showed that DCA inhibits the activity of the enzyme sphingomyelin synthase, with an IC50 of 4 µM. The structure–activity relationships between DCA and sphingomyelin synthase were evaluated using derivatives and cyclized hongoquercin A. In addition, DCA was found to inhibit amyloid β aggregation. These results may help in the design of effective drugs based on DCA.

Journal

• Molecules

  Molecules 25 (18), 4077-, 2020

  MDPI

Keywords

• daurichromenic acid
• sphingomyelin synthase
• dual inhibitor
• lipid-related disease

Details

• CRID: 1051130853454006912
• NII Article ID: 120006900321
• DOI: 10.3390/molecules25184077
• ISSN: 14203049
• HANDLE: 10258/00010314
• Web Site: https://muroran-it.repo.nii.ac.jp/records/10373
• Web Site: https://www.mdpi.com/1420-3049/25/18/4077/pdf
• Text Lang: en
• Article Type: journal article
• Data Source:
  • IRDB
  • Crossref
  • CiNii Articles
  • KAKEN