Topical anti-inflammatory phytomedicine based on Sphagneticola trilobata dried extracts

Pharm Biol. 2016 Nov;54(11):2465-2474. doi: 10.3109/13880209.2016.1160249. Epub 2016 Apr 5.

Abstract

Context: The aerial parts of Sphagneticola trilobata (L.) Pruski (Asteraceae) are popularly used to treat topical inflammation, but have not been fully investigated.

Objective: To identify polar compounds in S. trilobata extracts and develop a new topical phytomedicine based on the kaurenoic acid (KA) content while monitoring and demonstrating its topical anti-inflammatory activity.

Materials and methods: Ethanol spray-dried extract of S. trilobata was analysed by LC-MS while the KA content from semisolid was analysed by LC-UV. The extent of ear edema induced by applying 20 μL of croton oil (2.5%), arachidonic acid (AA; 2 mg/ear) and decanoylphorbol-13-acetate (TPA; 2.5 mg/ear) in mice was used to evaluate the biological activity of the semisolids, which were applied 30 min before the phlogistic agents.

Results: Eight phenylpropanoids and four oleanane-type triterpenoid saponins were identified, majority of them reported for the first time in this species, in addition to KA. The semisolid containing 1.0% of dried extract reduced the ear edema induced by croton oil [77.2 ± 4.5%; ID50 = 0.49 (0.28-0.87%)], TPA (81.5 ± 2.4%) and AA (39.1 ± 6.9%), with decreasing effect at higher KA concentrations. This was accompanied by neutrophil migration inhibition as investigated by biochemical and histological assays.

Discussion and conclusion: The anti-inflammatory effects were (at least in part) due to the interference in protein kinase C (PKC) activation, AA-cascade products and neutrophil migration inhibition, demonstrating the efficacy of the folk topical usage of this plant. The results support the development of a novel topical anti-inflammatory phytomedicine properly standardized to treat inflammatory dermatological diseases.

Keywords: Ear edema; LC-MS; LC-UV; kaurenoic acid; topical phytomedicine.

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Asteraceae* / chemistry
  • Cell Movement / drug effects
  • Diterpenes / analysis
  • Diterpenes / pharmacology
  • Male
  • Mice
  • Neutrophils / drug effects
  • Neutrophils / physiology
  • Oleanolic Acid / analysis
  • Phytotherapy*
  • Plant Extracts / analysis
  • Plant Extracts / pharmacology*
  • Protein Kinase C / metabolism

Substances

  • Anti-Inflammatory Agents
  • Diterpenes
  • Plant Extracts
  • kaurenoic acid
  • Oleanolic Acid
  • Protein Kinase C