Campomanesia adamantium Peel Extract in Antidiarrheal Activity: The Ability of Inhibition of Heat-Stable Enterotoxin by Polyphenols

• Published in: PloS one 2016-10, Vol.11 (10), p.e0165208
• Main Authors: Lescano, Caroline Honaiser, de Oliveira, Ivan Pires, Zaminelli, Tiago, Baldivia, Débora da Silva, da Silva, Luan Ramos, Napolitano, Mauro, Silvério, Camila Bitencourt Mendes, Lincopan, Nilton, Sanjinez-Argandoña, Eliana Janet
• Format: Article
• Language: English
• Subjects: Acids; Analysis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Anti-inflammatory agents; Antibacterial activity; Antidiarrheals - chemistry; Antidiarrheals - pharmacology; Antimicrobial agents; Assaying; Biology and Life Sciences; Cancer; Cell Line, Tumor; Cell proliferation; Cell Proliferation - drug effects; Computer simulation; Cyclic GMP; Cyclooxygenase 1 - chemistry; Cyclooxygenase 1 - metabolism; Cyclooxygenase 2 - chemistry; Cyclooxygenase 2 - metabolism; Cyclooxygenase-1; Cyclooxygenase-2; Cytotoxicity; Developing countries; Diarrhea; E coli; Enterotoxins - antagonists & inhibitors; Enterotoxins - metabolism; Escherichia coli; Fever; Flavonoids; Flavonoids - analysis; Fruit - chemistry; Fruit - metabolism; Fruits; Gallic acid; Gallic Acid - chemistry; Gallic Acid - metabolism; Heat; Herbal medicine; Hot Temperature; Humans; Hydrogen Bonding; Hypercholesterolemia; Inflammation; Inhibition; Kinases; LDCs; Medical treatment; Medicinal plants; Medicine and Health Sciences; Microorganisms; Molecular dynamics; Molecular Dynamics Simulation; Myrtaceae; Myrtaceae - chemistry; Myrtaceae - metabolism; Oils & fats; Penicillin; Pharmacology; Phenolic compounds; Phenols; Phenols - analysis; Physical Sciences; Plant Extracts - chemistry; Polyphenols; Polyphenols - chemistry; Polyphenols - metabolism; Research and analysis methods; Rodents; Salmonella typhimurium - drug effects; Sodium; Thermal stability; Toxicity
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0165208

Campomanesia adamantium (Myrtaceae) is a medicinal plant distributed in Brazilian Cerrado. Different parts of this plant are used in popular medicine for treatment of several diseases like fever, diarrhea, hypercholesterolemia and rheumatism. The aim of this work was to evaluate the inhibition of heat-stable enterotoxin type A (STa) by gallic acid present in the peel of C. adamantium fruit and assays to assess the antidiarrheal activity, anti-inflammatory and cytotoxic properties of peel extract using the T84 cell line model. The possible inhibition exerted by the gallic acid of the peel extract on the STa peptide was inferred by molecular dynamics simulations. The antidiarrheal effects were investigated measuring cGMP accumulation in cells after stimulation by STa toxin and antibacterial activity was assessed. The anti-inflammatory activity was assessed by inhibition of COX-1 and COX-2. MTT and LDH assays were used to evaluate any possible cytotoxic action while the CyQUANT test was used to investigate the effect on cell proliferation. A representation showing how the possible interactions between STa and the gallic acid of the extract might reduce the action of the enterotoxin is presented. C. adamantium peel extract significantly decreased the levels of cGMP in T84 cells. However, no effect on the species of microorganisms was observed. The extract also inhibited COX-1 (IC50 255.70 ± 0.04 ng/mL) and COX-2 (IC50 569.50 ± 0.11 ng/mL) enzymes. Cytotoxicity assay have shown significant changes in cells treated with the extract, which inhibited the cell proliferation until 72 hours of treatment. Direct interactions of phenolic compounds present in the extract with the STa toxin may limit its activity. Curative effect in the diarrhea treatment and its anti-inflammatory action is based on the pharmacological properties, mechanism of action of the C. adamantium peel extract, and no toxic effects of the peel extract presented on this work.