Antimicrobial, antiproliferative and proapoptotic activities of extract, fractions and isolated compounds from the stem of Erythroxylum caatingae plowman

Int J Mol Sci. 2012;13(4):4124-4140. doi: 10.3390/ijms13044124. Epub 2012 Mar 29.

Abstract

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6β-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 μg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis.

Keywords: Erythroxylum caatingae; antimicrobial activity; apoptosis; cytotoxic activity; hemolytic activity.

MeSH terms

  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology
  • Animals
  • Anti-Infective Agents / isolation & purification
  • Anti-Infective Agents / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival
  • Drug Discovery
  • Erythrocytes / drug effects
  • Erythroxylaceae / metabolism*
  • Female
  • Fungi / drug effects
  • Gram-Positive Bacteria / drug effects
  • Hemolysis / drug effects
  • Hep G2 Cells
  • Humans
  • Leukemia / drug therapy
  • Membrane Potential, Mitochondrial / drug effects
  • Mice
  • Microbial Sensitivity Tests
  • Mitochondrial Membranes / drug effects
  • Plant Extracts / pharmacology
  • Plant Stems / metabolism*

Substances

  • Alkaloids
  • Anti-Infective Agents
  • Antineoplastic Agents
  • Plant Extracts