Inhibitory Activities of Phenolic Compounds Isolated from Adina rubella Leaves Against 5α-Reductase Associated with Benign Prostatic Hypertrophy

Molecules. 2016 Jul 7;21(7):887. doi: 10.3390/molecules21070887.

Abstract

Adina rubella Hance (AR), a plant native to Korea, has been used as traditional medicine for dysentery, eczema, intoxication, and external hemorrhages. Previous phytochemical studies of AR have reported several components, including terpenoids, phenolics, and alkaloids. The current study evaluated the anti-oxidative and anti-inflammatory activities and 5α-reductase inhibition of isolated compounds of AR leaves to find a potential therapeutic agent for benign prostatic hypertrophy (BPH). Repeated chromatographic isolation of an 80% acetone extract of AR leaves yielded seven phenolic compounds: caffeic acid (1), chlorogenic acid (2), methyl chlorogenate (3), quercetin-3-rutinoside (4), kaempferol-3-O-α-l-rhamnopyranosyl-(1→6)-β-d-glucopyranoside (5), hyperoside (6), and grandifloroside (7). Compound 7 is a novel compound in AR. Caffeoyl derivatives 1-3 and 7 showed good anti-oxidative activities. In particular, caffeic acid (1) and grandifloroside (7) showed potent anti-inflammatory activities, and 7 also exhibited potent inhibitory activity against TNF-α and 5α-reductase. Our results show that the extract and grandifloroside (7) from leaves of AR might be developed as a source of potent anti-oxidative and anti-inflammatory agents and therapeutic agent for BPH.

Keywords: 5α-reductase; Adina rubella Hance; anti-inflammatory; anti-oxidative; benign prostatic hypertrophy.

MeSH terms

  • 5-alpha Reductase Inhibitors / chemistry*
  • 5-alpha Reductase Inhibitors / isolation & purification
  • 5-alpha Reductase Inhibitors / pharmacology*
  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Cell Line
  • Cytokines / biosynthesis
  • Enzyme Activation / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Male
  • Mice
  • Molecular Structure
  • Phenols / chemistry*
  • Phenols / isolation & purification
  • Phenols / pharmacology*
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plant Leaves / chemistry*
  • Prostatic Hyperplasia / drug therapy
  • Prostatic Hyperplasia / metabolism
  • Prostatic Hyperplasia / pathology
  • Rubiaceae / chemistry*

Substances

  • 5-alpha Reductase Inhibitors
  • Anti-Inflammatory Agents
  • Antioxidants
  • Cytokines
  • Phenols
  • Plant Extracts