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KD-64-A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist-Caffeine does not reduce diet-induced obesity in mice.
PLoS One. 2020; 15(6):e0229806.Plos

Abstract

The A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A2A adenosine receptor-KD-64 as compared to the known non-selective antagonist-caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A2A receptor antagonist was quite different from that of the non-selective.

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Authors+Show Affiliations

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacodynamics, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, Krakow, Poland.

Kieć-Kononowicz K

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

MeSH

Adenosine A2 Receptor AntagonistsAnimalsAnti-Inflammatory AgentsBody WeightCaffeineCapillary PermeabilityDietDiet, High-FatInsulin ResistanceInterleukin-6LocomotionMaleMiceObesityPeritoneumTumor Necrosis Factor-alpha

Pub Type(s)

Journal Article

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

Language

eng

PubMed ID

32555600

Citation

Kotańska, Magdalena, et al. "KD-64-A New Selective A2A Adenosine Receptor Antagonist Has Anti-inflammatory Activity but Contrary to the Non-selective antagonist-Caffeine Does Not Reduce Diet-induced Obesity in Mice." PloS One, vol. 15, no. 6, 2020, pp. e0229806.

Kotańska M, Dziubina A, Szafarz M, et al. KD-64-A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist-Caffeine does not reduce diet-induced obesity in mice. PLoS One. 2020;15(6):e0229806.

Kotańska, M., Dziubina, A., Szafarz, M., Mika, K., Reguła, K., Bednarski, M., Zygmunt, M., Drabczyńska, A., Sapa, J., & Kieć-Kononowicz, K. (2020). KD-64-A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist-Caffeine does not reduce diet-induced obesity in mice. PloS One, 15(6), e0229806. https://doi.org/10.1371/journal.pone.0229806

Kotańska M, et al. KD-64-A New Selective A2A Adenosine Receptor Antagonist Has Anti-inflammatory Activity but Contrary to the Non-selective antagonist-Caffeine Does Not Reduce Diet-induced Obesity in Mice. PLoS One. 2020;15(6):e0229806. PubMed PMID: 32555600.

* Article titles in AMA citation format should be in sentence-case

TY - JOUR T1 - KD-64-A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist-Caffeine does not reduce diet-induced obesity in mice. AU - Kotańska,Magdalena, AU - Dziubina,Anna, AU - Szafarz,Małgorzata, AU - Mika,Kamil, AU - Reguła,Karolina, AU - Bednarski,Marek, AU - Zygmunt,Małgorzata, AU - Drabczyńska,Anna, AU - Sapa,Jacek, AU - Kieć-Kononowicz,Katarzyna, Y1 - 2020/06/18/ PY - 2020/02/13/received PY - 2020/05/27/accepted PY - 2020/6/20/entrez PY - 2020/6/20/pubmed PY - 2020/8/22/medline SP - e0229806 EP - e0229806 JF - PloS one JO - PLoS One VL - 15 IS - 6 N2 - The A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A2A adenosine receptor-KD-64 as compared to the known non-selective antagonist-caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A2A receptor antagonist was quite different from that of the non-selective. SN - 1932-6203 UR - https://www.unboundmedicine.com/medline/citation/32555600/KD_64_A_new_selective_A2A_adenosine_receptor_antagonist_has_anti_inflammatory_activity_but_contrary_to_the_non_selective_antagonist_Caffeine_does_not_reduce_diet_induced_obesity_in_mice_ DB - PRIME DP - Unbound Medicine ER -