Bioactive ent-kaurane diterpenoids from Isodon rubescens

Phytochemistry. 2017 Nov:143:199-207. doi: 10.1016/j.phytochem.2017.08.009. Epub 2017 Sep 1.

Abstract

Seven previously undescribed 7,20-epoxy-ent-kaurane diterpenoids, isojiangrubesins A-G, along with seventeen known ones, were isolated from the aerial parts of Isodon rubescens. Their structures were characterized on the basis of spectroscopic methods and signal-crystal X-ray diffraction. All of these compounds were evaluated for their in vitro cytotoxicity against five human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480). Four isolates exhibited significant inhibitory ability against all cell lines, with IC50 values ranging from 0.5 to 6.5 μM; They also strongly inhibited NO production in LPS-stimulated RAW264.7 cells.

Keywords: 7,20-Epoxy-ent-kaurane diterpenoids; Anti-inflammatory; Cytotoxicity; Isodon rubescens; Lamiaceae.

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Crystallography, X-Ray
  • Diterpenes, Kaurane / chemistry
  • Diterpenes, Kaurane / isolation & purification*
  • Diterpenes, Kaurane / pharmacology*
  • Drug Screening Assays, Antitumor
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / isolation & purification*
  • Drugs, Chinese Herbal / pharmacology*
  • HL-60 Cells
  • Humans
  • Isodon / chemistry*
  • Lipopolysaccharides / pharmacology
  • Macrophages / drug effects
  • Molecular Structure
  • Nitric Oxide / biosynthesis
  • Plant Components, Aerial / chemistry

Substances

  • Antineoplastic Agents, Phytogenic
  • Diterpenes, Kaurane
  • Drugs, Chinese Herbal
  • Lipopolysaccharides
  • Nitric Oxide