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Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms.
J Ethnopharmacol. 2015 Dec 04; 175:378-89.JE

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Copaifera malmei Harms (Fabaceae) is a plant that occurs in the central region of Brazil, where the plant's leaves infusion is popularly used to treat gastric ulcer and inflammatory diseases. This study was aimed to investigate the gastroprotective activity and mode of action of the plants' leaves infusion in order to establish the scientific basis for such usage, and to assess its potential as a source of an anti-ulcer agent.

MATERIALS AND METHODS

Leaves infusion extract of the plant (SIECm) was prepared, freeze dried and lyophilised. Its qualitative and quantitative phytochemical constituents were investigated using TLC and HPLC techniques. The safety profile was evaluated on CHO-k1 epithelial cells viability using the Alamar blue assay, and by acute toxicity test in mice. The gastroprotection and anti-ulcer efficacy of the SIECm (25, 100 and 400mg/kg, p.o.) were tested using acute (acidified ethanol, piroxicam and water restrain stress), and chronic (acetic acid) experimental ulcer models. The plausible mode of action of the SIECm was assessed using gastric secretion, gastric barrier mucus, nitric oxide, and its antioxidant (myeloperoxidase and catalase) effects in mice and rats. The histopathological analyses of the ulcerated tissues as well as the extract's activity on Helicobacter pylori were also investigated.

RESULTS

Phytochemical tests indicated the presence of mainly phytosterols, phenolics and flavonoids. The SIECm exhibited no cytotoxic effects on the CHO-k1 cells, and no oral acute toxicity in mice. It prevented against the acute induced ulcerations by enhancing gastroprotection through gastric mucus production, NO modulation, antioxidant, reduced gastric secretion and enhanced chronic ulcers healing process, as shown by reduction/prevention of epithelial and vascular damage, in addition to reduction in leucocyte infiltration. The SIECm however did not exhibit activity against H. pylori.

CONCLUSION

The SIECm is safe, contain useful phytochemicals and exhibited significant gastroprotective/anti-ulcer effects. The results justify its folkloric usage, and provided scientific evidence of its potential as a source of new phytodrug to treat gastric ulcers.

Authors+Show Affiliations

Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil; Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development (NIPRD), Abuja, Nigeria.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Laboratório de Pesquisa em Produtos Naturais, Curso de Medicina, Universidade Federal do Tocantins (UFT), Palmas, Brazil.Laboratório de Pesquisa em Produtos Naturais, Curso de Medicina, Universidade Federal do Tocantins (UFT), Palmas, Brazil.Departamento da Biotecnologia, Universidade Federal do Tocantins (UFT), Gurupi, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Histologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil. Electronic address: taba@terra.com.br.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26408044

Citation

Adzu, Bulus, et al. "Evaluation of the Safety, Gastroprotective Activity and Mechanism of Action of Standardised Leaves Infusion Extract of Copaifera Malmei Harms." Journal of Ethnopharmacology, vol. 175, 2015, pp. 378-89.
Adzu B, Balogun SO, Pavan E, et al. Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms. J Ethnopharmacol. 2015;175:378-89.
Adzu, B., Balogun, S. O., Pavan, E., Ascêncio, S. D., Soares, I. M., Aguiar, R. W., Ribeiro, R. V., Beserra, Â. M., de Oliveira, R. G., da Silva, L. I., Damazo, A. S., & Martins, D. T. (2015). Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms. Journal of Ethnopharmacology, 175, 378-89. https://doi.org/10.1016/j.jep.2015.09.027
Adzu B, et al. Evaluation of the Safety, Gastroprotective Activity and Mechanism of Action of Standardised Leaves Infusion Extract of Copaifera Malmei Harms. J Ethnopharmacol. 2015 Dec 4;175:378-89. PubMed PMID: 26408044.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms. AU - Adzu,Bulus, AU - Balogun,Sikiru Olaitan, AU - Pavan,Eduarda, AU - Ascêncio,Sérgio Donizeti, AU - Soares,Ilsamar Mendes, AU - Aguiar,Raimundo Wagner Souza, AU - Ribeiro,Reginaldo Vicente, AU - Beserra,Ângela Márcia Selhorst e Silva, AU - de Oliveira,Ruberlei Godinho, AU - da Silva,Larissa Irene, AU - Damazo,Amílcar Sabino, AU - Martins,Domingos Tabajara de Oliveira, Y1 - 2015/09/25/ PY - 2015/06/23/received PY - 2015/09/12/revised PY - 2015/09/21/accepted PY - 2015/9/27/entrez PY - 2015/9/27/pubmed PY - 2016/9/28/medline KW - Acute toxicity KW - Copaifera malmei KW - Gastroprotection KW - Leaves infusion KW - Phytochemicals SP - 378 EP - 89 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 175 N2 - ETHNOPHARMACOLOGICAL RELEVANCE: Copaifera malmei Harms (Fabaceae) is a plant that occurs in the central region of Brazil, where the plant's leaves infusion is popularly used to treat gastric ulcer and inflammatory diseases. This study was aimed to investigate the gastroprotective activity and mode of action of the plants' leaves infusion in order to establish the scientific basis for such usage, and to assess its potential as a source of an anti-ulcer agent. MATERIALS AND METHODS: Leaves infusion extract of the plant (SIECm) was prepared, freeze dried and lyophilised. Its qualitative and quantitative phytochemical constituents were investigated using TLC and HPLC techniques. The safety profile was evaluated on CHO-k1 epithelial cells viability using the Alamar blue assay, and by acute toxicity test in mice. The gastroprotection and anti-ulcer efficacy of the SIECm (25, 100 and 400mg/kg, p.o.) were tested using acute (acidified ethanol, piroxicam and water restrain stress), and chronic (acetic acid) experimental ulcer models. The plausible mode of action of the SIECm was assessed using gastric secretion, gastric barrier mucus, nitric oxide, and its antioxidant (myeloperoxidase and catalase) effects in mice and rats. The histopathological analyses of the ulcerated tissues as well as the extract's activity on Helicobacter pylori were also investigated. RESULTS: Phytochemical tests indicated the presence of mainly phytosterols, phenolics and flavonoids. The SIECm exhibited no cytotoxic effects on the CHO-k1 cells, and no oral acute toxicity in mice. It prevented against the acute induced ulcerations by enhancing gastroprotection through gastric mucus production, NO modulation, antioxidant, reduced gastric secretion and enhanced chronic ulcers healing process, as shown by reduction/prevention of epithelial and vascular damage, in addition to reduction in leucocyte infiltration. The SIECm however did not exhibit activity against H. pylori. CONCLUSION: The SIECm is safe, contain useful phytochemicals and exhibited significant gastroprotective/anti-ulcer effects. The results justify its folkloric usage, and provided scientific evidence of its potential as a source of new phytodrug to treat gastric ulcers. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/26408044/Evaluation_of_the_safety_gastroprotective_activity_and_mechanism_of_action_of_standardised_leaves_infusion_extract_of_Copaifera_malmei_Harms_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(15)30152-5 DB - PRIME DP - Unbound Medicine ER -