Anti-inflammatory and immunomodulatory effects of RDV-8 [C18H22N2O2S (ethyl 1-butyl-6-methyl-2-phenyl-4-thioxo-1,4-dihydropyrimidi
详细信息 查看全文
- 作者：Marcos Schuch Azambuja (1)
Adroaldo Lunardelli (1)
Robson Henrich Amaral (1)
Fernanda Bordignon Nunes (1)
Eduardo Caberlon (1)
Vinicius Lorini da Costa (1)
Márcio Vinícius Fagundes Donadio (1) (2)
Daniela Nunes Vitor (3)
Denizar Alberto da Silva Melo (1) (2)
Silvio Cunha (3)
Jarbas Rodrigues de Oliveira (1) - 关键词：RDV ; 8 ; Pleurisy ; Anti ; inflammatory ; Immunomodulatory ; Nitric oxide
- 刊名：Inflammopharmacology
- 出版年：2011
- 出版时间：June 2011
- 年：2011
- 卷：19
- 期：3
- 页码：145-153
- 全文大小：420KB
- 参考文献：1. Anjos JV, Mendon?a FJB Jr, Costa-Silva JH et al (2008) Estudo preliminar da toxicidade aguda e das atividades anti-edematogênica e anti-nociceptiva da 3, 4-diidro-2-fenil-6-para-flúor-fenil-4-oxo-pirimidina-5-carbonitrila. Latin Am J Pharm 27(3):339-44
2. Biber K, Zuurman MW, Dijkstra IM et al (2002) Chemokines in the brain: neuroimmunology and beyond. Curr Opin Pharmacol 2(1):63-8 CrossRef
3. Boschi ES, Leite CE, Saciura VC et al (2008) Anti-inflammatory effects of low-level laser therapy (660?nm) in the early phase in carrageenan-induced pleurisy in rat. Lasers Surg Med 40:500-08 CrossRef
4. Christopherson K 2nd, Hromas R (2001) Chemokine regulation of normal and pathologic immune responses. Stem Cells 19(5):388-96 CrossRef
5. Cocco MT, Congiu C, Onnis V et al (2001) Synthesis and antitumor evaluation of 6-thioxo-, 6-oxo- and 2, 4-dioxopyrimidine derivatives. Il Farmaco 56(10):741-48 CrossRef
6. Cunha S, Bastos RM, Silva PO et al (2007) Synthesis and structural studies of 4-thioxopyrimidines with antimicrobial activities. Monatshefte für Chemie/Chem Mon 138(2):111-19 CrossRef
7. Curran RD, Billiar TR, Stuehr DJ et al (1989) Hepatocytes produce nitrogen oxides from l -arginine in response to inflammatory products from Kupffer cells. J Exp Med 170(5):1769-774 CrossRef
8. D’Ambrosio D, Panina-Bordignon P, Sinigaglia F (2003) Chemokine receptors in inflammation: an overview. J Immunol Methods 273(1-):3-3 CrossRef
9. Fujisawa H, Nakagawa S, Ohkubo Y et al (2005) Local and systemic expression of inducible nitric oxide synthase in comparison with that of cyclooxygenase-2 in rat carrageenin-induced pleurisy. Nitric Oxide 12(2):80-8 CrossRef
10. Goldsby RA, Kindt TJ, Kuby J et al (2002) Immunology, 5th edn. W. H. Freeman, New York
11. Gualillo O, Eiras S, Lago F et al (2000) Elevated serum leptin concentrations induced by experimental acute inflammation. Life Sci 67(20):2433-441 CrossRef
12. Habashy RR, Abdel-Naim AB, Khalifa AE et al (2005) Anti-inflammatory effects of jojoba liquid wax in experimental models. Pharmacol Res 51(2):95-05 CrossRef
13. Kumar A, Prasad R, Gupta VK (2004) Fabrication of PVC based membrane using nickel porphyrazine as ionophore in the screening of thiocyanate ion in aqueous and real samples. Comb Chem High Throughput Screen 7(4):367-74
14. Lopes RP, Lunardelli A, Preissler T et al (2006) The effects of fructose-1,6-bisphosphate and dexamethasone on acute inflammation and T-cell proliferation. Inflamm Res 55:354-58 CrossRef
15. Lunardelli A, Leite CE, Pires MGS et al (2006) Extract of the bristles of / Dirphia sp. increases nitric oxide in a rat pleurisy model. Inflamm Res 55:129-35 CrossRef
16. Madhavan GR, Chakrabarti R, Vikramadithyan RK et al (2002) Synthesis and biological activity of novel pyrimidinone containing thiazolidinedione derivatives. Bioorg Med Chem 10(8):2671-680 CrossRef
17. Modica M, Santagati M, Santagati A et al (2000) Synthesis of new [1, 3, 4]thiadiazolo[3, 2-a]thieno[2, 3-d]pyrimidinone derivatives with antiinflammatory activity. Pharmazie 55(7):500-02
18. Nunes FB, Graziottin CM, Alves Filho JCF et al (2003a) An assessment of fructose-1, 6-bisphosphate as an antimicrobial and anti-inflammatory agent in sepsis. Pharmacol Res 47(1):35-1 CrossRef
19. Nunes FB, Graziottin CM, Alves-Filho JCF et al (2003b) Immunomodulatory effect of fructose-1, 6-bisphosphate on T-lymphocytes. Int Immunopharmacol 3:267-72 CrossRef
20. Paul EL, Lunardelli A, Caberlon E et al (2009) Anti-inflammatory and immunomodulatory effects of / Baccharis trimera aqueous extract on induced pleurisy in rats and lymphoproliferation in vitro. Inflammation 32(6):419-25 CrossRef
21. Puneet P, Moochhala S, Bhatia M (2005) Chemokines in acute respiratory distress syndrome. Am J Physiol Lung Cell Mol Physiol 288(1):3-5 CrossRef
22. Pype JL, Dupont LJ, Menten P et al (1999) Expression of monocyte chemotactic protein (MCP)-1, MCP-2, and MCP-3 by human airway smooth-muscle cells. Modulation by corticosteroids and T-helper 2 cytokines. Am J Respir Cell Mol Biol 21(4):528-36
23. Sakaguchi Y, Shirahase H, Kunishiro K et al (2006) Effect of combination of nitric oxide synthase and cyclooxygenase inhibitors on carrageenan-induced pleurisy in rats. Life Sci 79(5):442-47 CrossRef
24. Saladino R, Ciambecchini U, Maga G et al (2002) A new and efficient synthesis of substituted 6-[(2-dialkylamino)ethyl] pyrimidine and 4- / N, / N-dialkyl-6-vinyl-cytosine derivatives and evaluation of their anti-rubella activity. Bioorg Med Chem 10(7):2143-153 CrossRef
25. Salimbeni A, Canevotti R, Paleari F et al (1995) / N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists. J Med Chem 38(24):4806-820 CrossRef
26. Santos RCV, Lunardelli A, Caberlon E et al (2010) Anti-inflammatory and immunomodulatory effects of / Ulomoides dermestoides on induced pleurisy in rats and lymphoproliferation in vitro. Inflammation 33(3):173-79 CrossRef
27. Shimizu M, Oh-Hashi F, Tsukagoshi S et al (1995) In vitro and in vivo antitumor activity of the interferon inducer bropirimine. Anticancer Drugs 6(1):158-62 CrossRef
28. Spiller F, Alves MK, Vieira SM et al (2008) Anti-inflammatory effects of red pepper ( / Capsicum baccatum) on carrageenan- and antigen-induced inflammation. J Pharm Pharmacol 60:473-78 CrossRef
29. Temple DL, Yevich JP, Covington C et al (1979) Synthesis of 3, 4-dihydro-4-oxothieno(2, 3-d)pyrimidine-2-carboxylates, a new series of orally active antiallergy agents. J Med Chem 22(5):505-10 CrossRef
30. White DC, Greenwood TD, Downey AL et al (2004) Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido(2, 3-d)pyrimidinones. Bioorg Med Chem 12(21):5711-717 CrossRef - 作者单位：Marcos Schuch Azambuja (1)
Adroaldo Lunardelli (1)
Robson Henrich Amaral (1)
Fernanda Bordignon Nunes (1)
Eduardo Caberlon (1)
Vinicius Lorini da Costa (1)
Márcio Vinícius Fagundes Donadio (1) (2)
Daniela Nunes Vitor (3)
Denizar Alberto da Silva Melo (1) (2)
Silvio Cunha (3)
Jarbas Rodrigues de Oliveira (1)
1. Laboratório de Pesquisa em Biofísica Celular e Inflama??o, Pontifícia Universidade Católica do Rio Grande do Sul (PUCRS), Avenida Ipiranga 6681, Prédio 12, Bloco C, Sala 263, CEP 90.619-00, Porto Alegre, Rio Grande do Sul, Brazil
2. Faculdade de Enfermagem Nutri??o e Fisioterapia, Pontifícia Universidade Católica do Rio Grande do Sul (PUCRS), Porto Alegre, Rio Grande do Sul, Brazil
3. Instituto de Química, Universidade Federal da Bahia (UFBA), Salvador, Bahia, Brazil - ISSN：1568-5608
文摘
RDV-8 [C18H22N2O2S (ethyl 1-butyl-6-methyl-2-phenyl-4-thioxo-1,4-dihydropyrimidine-5-carboxylate)] is derived from the 4-thioxopyrimidine, and presents important clinical effects. The present study explored the RDV-8 effects in the proliferation of human peripheral blood mononuclear cells (PBMCs), as well as in a pleurisy-induced rat model. PBMCs were directly plated in four different RDV-8 concentrations (0.0125, 0.025, 0.05 and 0.1?mg/mL). RDV-8 decreased cell proliferation and monocyte chemotactic protein 1 synthesis. The interleukin 1 levels and the cytotoxic effect were not significantly affected by RDV-8 treatment. In the carrageenan-induced pleurisy model, the RDV-8 (3?mg/kg) treatment induced a significant reduction in the exudate volume, in the polymorphonuclear leukocyte migration and in the pleural exudate NO levels. The results indicate that RDV-8 may have an immunomodulatory effect, as well as anti-inflammatory actions suggesting that it could represent a new strategy in the inflammatory response modulation.