Antinociception of petroleum ether fraction derived from crude methanol extract of Melastoma malabathricum leaves and its possible mechanisms of action in animal models
- PMID: 27899097
- PMCID: PMC5129229
- DOI: 10.1186/s12906-016-1478-1
Antinociception of petroleum ether fraction derived from crude methanol extract of Melastoma malabathricum leaves and its possible mechanisms of action in animal models
Abstract
Background: Melastoma malabathricum L. (family Melastomaceae) has been traditionally used as remedies against various ailments including those related to pain. The methanol extract of M. malabathricum leaves has been proven to show antinociceptive activity. Thus, the present study aimed to determine the most effective fraction among the petroleum ether- (PEMM), ethyl acetate- (EAMM) and aqueous- (AQMM) fractions obtained through successive fractionation of crude, dried methanol extract of M. malabathricum (MEMM) and to elucidate the possible mechanisms of antinociception involved.
Methods: The effectiveness of fractions (100, 250 and 500 mg/kg; orally) were determine using the acetic acid-induced abdominal constriction test and the most effective extract was further subjected to the hot plate- or formalin-induced paw licking-test to establish its antinociceptive profile. Further elucidation of the role of opioid and vanilloid receptors, glutamatergic system, and nitric oxide/cyclic guanosine phosphate (NO/cGMP) pathway was also performed using the appropriate nociceptive models while the phytoconstituents analyses were performed using the phytochemical screening test and, HPLC-ESI and GCMS analyses.
Results: PEMM, EAMM and AQMM significantly (p < 0.05) attenuated acetic acid-induced nociception with the recorded EC50 of 119.5, 125.9 and 352.6 mg/kg. Based on the EC50 value, PEMM was further studied and also exerted significant (p < 0.05) antinociception against the hot plate- and formalin-induced paw licking-test. With regards to the mechanisms of antinociception,: i) PEMM significantly (p < 0.05) attenuated the nociceptive action in capsaicin- and glutamate-induced paw licking test.; ii) naloxone (5 mg/kg), a non-selective opioid antagonist, failed to significantly (p < 0.05) inhibit PEMM's antinociception iii) L-arginine (a nitric oxide precursor), but not NG-nitro-L-arginine methyl esters (L-NAME; an inhibitor of NO synthase), methylene blue (MB; an inhibitor of cGMP), or their respective combination, significantly (p < 0.05) reversed the antinociception of PEMM. Phytochemical analyses revealed the presence of several antinociceptive-bearing bioactive compounds, such as triterpenes and volatile compounds like oleoamide and palmitic acid. The presence of low flavonoids, such as gallocatechin and epigallocatechin, saponins and tannins in PEMM might synergistically contribute to enhance the major compounds antinociceptive effect.
Conclusion: PEMM exerted a non-opioid-mediated antinociceptive activity at the central and peripheral levels via the inhibition of vanilloid receptors and glutamatergic system, and the activation of NO-mediated/cGMP-independent pathway. Triterpenes, as well as volatile oleoamide and palmitic acid, might be responsible for the observed antinociceptive activity of PEMM.
Keywords: Antinociceptive activity; Crude methanol extract; Fraction; Glutamatergic system; Mechanisms of antinociception; Melastoma malabathricum; NO-mediated/cGMP-independent pathway; Non-opioid system; Vanilloid receptors.
Figures
![Fig. 1](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig1_HTML.gif)
![Fig. 2](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig2_HTML.gif)
![Fig. 3](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig3_HTML.gif)
![Fig. 4](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig4_HTML.gif)
![Fig. 5](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig5_HTML.gif)
![Fig. 6](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig6_HTML.gif)
![Fig. 7](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig7_HTML.gif)
![Fig. 8](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig8_HTML.gif)
![Fig. 9](https://www.ncbi.nlm.nih.gov/pmc/articles/instance/5129229/bin/12906_2016_1478_Fig9_HTML.gif)
Similar articles
-
Methanol Extract of Dicranopteris linearis Leaves Attenuate Pain via the Modulation of Opioid/NO-Mediated Pathway.Biomolecules. 2020 Feb 12;10(2):280. doi: 10.3390/biom10020280. Biomolecules. 2020. PMID: 32059475 Free PMC article.
-
Antinociceptive activity of petroleum ether fraction obtained from methanolic extract of Clinacanthus nutans leaves involves the activation of opioid receptors and NO-mediated/cGMP-independent pathway.BMC Complement Altern Med. 2019 Apr 2;19(1):79. doi: 10.1186/s12906-019-2486-8. BMC Complement Altern Med. 2019. PMID: 30940120 Free PMC article.
-
A Review on the Pharmacological Activities and Phytochemicals of Alpinia officinarum (Galangal) Extracts Derived from Bioassay-Guided Fractionation and Isolation.Pharmacogn Rev. 2017 Jan-Jun;11(21):43-56. doi: 10.4103/phrev.phrev_55_16. Pharmacogn Rev. 2017. PMID: 28503054 Free PMC article. Review.
-
Mechanisms of α-mangostin-induced antinociception in a rodent model.Biol Res Nurs. 2015 Jan;17(1):68-77. doi: 10.1177/1099800414529648. Epub 2014 Apr 3. Biol Res Nurs. 2015. PMID: 25504952
-
Central antinociceptive effects of non-steroidal anti-inflammatory drugs and paracetamol. Experimental studies in the rat.Acta Anaesthesiol Scand Suppl. 1995;103:1-44. Acta Anaesthesiol Scand Suppl. 1995. PMID: 7725891 Review.
Cited by
-
Lysionotin exerts antinociceptive effects in various models of nociception induction.Heliyon. 2023 Apr 18;9(4):e15619. doi: 10.1016/j.heliyon.2023.e15619. eCollection 2023 Apr. Heliyon. 2023. PMID: 37151635 Free PMC article.
-
Ceratonia siliqua leaves ethanol extracts exert anti-nociceptive and anti-inflammatory effects.Heliyon. 2022 Aug 24;8(8):e10400. doi: 10.1016/j.heliyon.2022.e10400. eCollection 2022 Aug. Heliyon. 2022. PMID: 36090223 Free PMC article.
-
LC-ESI-IT-MS/MS and MALDI-TOF Approach: Identification of Natural Polymers from Rhizophora mangle Barks and Determination of Their Analgesic and Anti-inflammatory Properties.Nat Prod Bioprospect. 2019 Jan;9(1):23-34. doi: 10.1007/s13659-018-0192-8. Epub 2018 Nov 14. Nat Prod Bioprospect. 2019. PMID: 30430388 Free PMC article.
References
-
- Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson G. Pharmacology. 7. Edinburg: Els Chur Livingstone; 2011.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Medical
Miscellaneous