Chemical Constituents with Proprotein Convertase Subtilisin/Kexin Type 9 mRNA Expression Inhibitory Activity from Dried Immature Morus alba Fruits

J Agric Food Chem. 2017 Jul 5;65(26):5316-5321. doi: 10.1021/acs.jafc.7b02088. Epub 2017 Jun 26.

Abstract

Phytochemical investigation for a chloroform-soluble extract of dried Morus alba fruits, selected by proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression monitoring assay in HepG2 cells, led to the isolation of a new benzofuran, isomoracin D (1), and a naturally occurring compound, N-(N-benzoyl-l-phenylalanyl)-l-phenylalanol (2), along with 13 known compounds (3-15). All of the structures were established by NMR spectroscopic data as well as MS analysis. Of the isolates, moracin C (7) was found to inhibit PCSK9 mRNA expression with an IC50 value of 16.8 μM in the HepG2 cells.

Keywords: Morus alba fruits; N-(N-phenzoyl-l-phenylalanyl)-l-phenylalanol; PCSK9 mRNA expression; isomoracin D; moracin C.

MeSH terms

  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / isolation & purification
  • Fruit / chemistry
  • Hep G2 Cells
  • Humans
  • Molecular Structure
  • Morus / chemistry*
  • PCSK9 Inhibitors*
  • Plant Extracts / chemistry*
  • Plant Extracts / isolation & purification
  • Proprotein Convertase 9 / chemistry
  • Proprotein Convertase 9 / genetics*
  • Proprotein Convertase 9 / metabolism
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism

Substances

  • Enzyme Inhibitors
  • PCSK9 Inhibitors
  • Plant Extracts
  • RNA, Messenger
  • Proprotein Convertase 9