Evaluation of Biological Activity of Mastic Extracts Based on Chemotherapeutic Indices

In Vivo. 2017 Jul-Aug;31(4):591-598. doi: 10.21873/invivo.11099.

Abstract

Background: Most previous mastic investigators have not considered its potent cytotoxicity that may significantly affect the interpretation of obtained data. In the present study, we re-evaluated several biological activities of mastic extracts, based on chemotherapeutic indexes.

Materials and methods: Pulverized mastic gum was extracted with n-hexane and then with ethyl acetate or independently with methanol or n-butanol. Tumor specificity (TS) of the extracts was determined by their cytotoxicity against human malignant and non-malignant cells. Antibacterial activity was determined by their cytotoxicity against bacteria and normal oral cells. Antiviral activity was determined by their protection of viral infection and cytotoxic activity. Cytochrome P-450 (CYP) 3A4 activity was measured by β-hydroxylation of testosterone.

Results: Ethyl acetate extract showed slightly higher tumor specificity (TS=2.6) and one order higher antibacterial activity (selectivity index (SI)=0.813) than other extracts (TS=1.4-2.5; SI=0.030-0.063). All extracts showed no anti-human immunodeficiency virus (HIV) activity, but some anti-herpes simplex virus (HSV) activity, which was masked by potent cytotoxicity. They showed strong inhibitory activity against CYP3A4.

Conclusion: Ethyl acetate extraction following the removal of cytotoxic and CYP3A4 inhibitory substances by n-hexane can enhance antitumor and antibacterial activity of mastic.

Keywords: CYP3A4 inhibition; Mastic; anti-HIV; anti-HSV; antibacterial; ethyl acetate extraction; fractionation; tumor specificity.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Bacteria / drug effects*
  • Bacteria / pathogenicity
  • Cell Proliferation / drug effects
  • Cytochrome P-450 CYP3A / genetics
  • HIV / drug effects
  • HIV / pathogenicity
  • Hexanes / chemistry
  • Humans
  • Mastic Resin / chemistry
  • Mastic Resin / pharmacology*
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Pistacia / chemistry
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Simplexvirus / drug effects
  • Simplexvirus / pathogenicity

Substances

  • Anti-Bacterial Agents
  • Antiviral Agents
  • Hexanes
  • Mastic Resin
  • Plant Extracts
  • n-hexane
  • Cytochrome P-450 CYP3A