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

• Published in: Molecules (Basel, Switzerland) Switzerland), 2020-09, Vol.25 (18), p.4077
• Main Authors: Deepak, Hadya Virupaksha, Swamy, Mahadeva M M, Murai, Yuta, Suga, Yoshiko, Anetai, Masaki, Yo, Takuro, Kuragano, Masahiro, Uwai, Koji, Tokuraku, Kiyotaka, Monde, Kenji
• Format: Article
• Language: English
• Subjects: Acids; Amyloid; Amyloid beta-Peptides - antagonists & inhibitors; Amyloid beta-Peptides - metabolism; amyloid β; Apoptosis; Biomolecules; Bronchitis; Cell growth; Chromans - chemistry; Chromans - pharmacology; daurichromenic acid; Disease; Dose-Response Relationship, Drug; Drug development; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacology; dual inhibitor; Enzyme Activation - drug effects; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Enzymes; Gram-positive bacteria; Herbal medicine; Inflammation; Ligands; lipid-related disease; Medicinal plants; Molecular Structure; Natural products; NMR; Nuclear magnetic resonance; Plants, Medicinal - chemistry; Protein Aggregates - drug effects; Quantum dots; Rhododendron; Rhododendron - chemistry; Sphingomyelin; sphingomyelin synthase; Staphylococcus infections; Transferases (Other Substituted Phosphate Groups) - antagonists & inhibitors
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules25184077

Species of the genus 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 , 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 IC 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.