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Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo

Introduction: Pain is a major global health issue, where its pharmacotherapy prompts unwanted side effects; hence, the development of effective alternative compounds from natural derivatives with lesser side effects is clinically needed. Chalcone; the precursors of flavonoid, and its derivatives hav...

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Main Authors: Noor Azlina, Abu Bakar, Mohd Roslan, Sulaiman, Nordin, Lajis, Akhtar, Muhammad Nadeem, Azam Shah, Mohamad
Format: Article
Language:English
Published: Wolters Kluwer Medknow Publications 2020
Subjects:
TP Chemical technology
Online Access:http://umpir.ump.edu.my/id/eprint/31005/1/Evaluation%20of%20antinociceptive%20profile%20of%20chalcone%20derivative%20.pdf
http://umpir.ump.edu.my/id/eprint/31005/
https://doi.org/10.4103/jpbs.JPBS_344_19
https://doi.org/10.4103/jpbs.JPBS_344_19
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spelling my.ump.umpir.310052021-05-17T07:21:18Z http://umpir.ump.edu.my/id/eprint/31005/ Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo Noor Azlina, Abu Bakar Mohd Roslan, Sulaiman Nordin, Lajis Akhtar, Muhammad Nadeem Azam Shah, Mohamad TP Chemical technology Introduction: Pain is a major global health issue, where its pharmacotherapy prompts unwanted side effects; hence, the development of effective alternative compounds from natural derivatives with lesser side effects is clinically needed. Chalcone; the precursors of flavonoid, and its derivatives have been widely investigated due to its pharmacological properties. Objective: This study addressed the therapeutic effect of 3- (2,5- dimethoxyphenyl)-1-(5-methyl furan-2-yl) prop-2-en-1-one (DMPF-1); synthetic chalcone derivative, on antinociceptive activity in vivoMaterials and Methods: The antinociceptive profile was evaluated using acetic-acid-induced abdominal writhing, hot plate, and formalin induced paw licking test. Capsaicin, phorbol 12-myristate 12 acetate (PMA), and glutamate induced paw licking test were carried out to evaluate their potential effects toward different targets. Results: It was shown that the doses of 0.1, 0.5, 1, and 5 mg/kg of DMPF-1 given via intraperitoneal injection showed significant reduction in writhing responses and increased the latency time in hot-plate test where reduced time spent on licking the injected paw in formalin and dose contingency inhibition was observed. The similar results were observed in capsaicin, PMA, and glutamate-induced paw licking test. In addition, the challenge with nonselective opioid receptor antagonist (naloxone) aimed to evaluate the involvement of the opioidergic system, which showed no reversion in analgesic profile in formalin and hot-plate test. Conclusion: Collectively, this study showed that DMPF-1 markedly inhibits both peripheral and central nociception through the mechanism involving an interaction with vanilloid and glutamatergic system regardless of the activation of the opioidergic system. Wolters Kluwer Medknow Publications 2020-11 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/31005/1/Evaluation%20of%20antinociceptive%20profile%20of%20chalcone%20derivative%20.pdf Noor Azlina, Abu Bakar and Mohd Roslan, Sulaiman and Nordin, Lajis and Akhtar, Muhammad Nadeem and Azam Shah, Mohamad (2020) Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo. Journal of Pharmacy and Bioallied Sciences, 12 (6). pp. 711-717. ISSN 0975-7406 https://doi.org/10.4103/jpbs.JPBS_344_19 https://doi.org/10.4103/jpbs.JPBS_344_19
institution Universiti Malaysia Pahang
building UMP Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaysia Pahang
content_source UMP Institutional Repository
url_provider http://umpir.ump.edu.my/
language English
topic TP Chemical technology
spellingShingle TP Chemical technology
Noor Azlina, Abu Bakar
Mohd Roslan, Sulaiman
Nordin, Lajis
Akhtar, Muhammad Nadeem
Azam Shah, Mohamad
Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
description Introduction: Pain is a major global health issue, where its pharmacotherapy prompts unwanted side effects; hence, the development of effective alternative compounds from natural derivatives with lesser side effects is clinically needed. Chalcone; the precursors of flavonoid, and its derivatives have been widely investigated due to its pharmacological properties. Objective: This study addressed the therapeutic effect of 3- (2,5- dimethoxyphenyl)-1-(5-methyl furan-2-yl) prop-2-en-1-one (DMPF-1); synthetic chalcone derivative, on antinociceptive activity in vivoMaterials and Methods: The antinociceptive profile was evaluated using acetic-acid-induced abdominal writhing, hot plate, and formalin induced paw licking test. Capsaicin, phorbol 12-myristate 12 acetate (PMA), and glutamate induced paw licking test were carried out to evaluate their potential effects toward different targets. Results: It was shown that the doses of 0.1, 0.5, 1, and 5 mg/kg of DMPF-1 given via intraperitoneal injection showed significant reduction in writhing responses and increased the latency time in hot-plate test where reduced time spent on licking the injected paw in formalin and dose contingency inhibition was observed. The similar results were observed in capsaicin, PMA, and glutamate-induced paw licking test. In addition, the challenge with nonselective opioid receptor antagonist (naloxone) aimed to evaluate the involvement of the opioidergic system, which showed no reversion in analgesic profile in formalin and hot-plate test. Conclusion: Collectively, this study showed that DMPF-1 markedly inhibits both peripheral and central nociception through the mechanism involving an interaction with vanilloid and glutamatergic system regardless of the activation of the opioidergic system.
format Article
author Noor Azlina, Abu Bakar
Mohd Roslan, Sulaiman
Nordin, Lajis
Akhtar, Muhammad Nadeem
Azam Shah, Mohamad
author_facet Noor Azlina, Abu Bakar
Mohd Roslan, Sulaiman
Nordin, Lajis
Akhtar, Muhammad Nadeem
Azam Shah, Mohamad
author_sort Noor Azlina, Abu Bakar
title Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
title_short Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
title_full Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
title_fullStr Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
title_full_unstemmed Evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (DMPF-1) in vivo
title_sort evaluation of antinociceptive profile of chalcone derivative (3-(2,5-dimethoxyphenyl)-1-(5- methylfuran-2-yl) prop-2-en-1-one (dmpf-1) in vivo
publisher Wolters Kluwer Medknow Publications
publishDate 2020
url http://umpir.ump.edu.my/id/eprint/31005/1/Evaluation%20of%20antinociceptive%20profile%20of%20chalcone%20derivative%20.pdf
http://umpir.ump.edu.my/id/eprint/31005/
https://doi.org/10.4103/jpbs.JPBS_344_19
https://doi.org/10.4103/jpbs.JPBS_344_19
_version_ 1701163149161398272
score 13.211869

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