Biological assay of a novel quinoxalinone with antimalarial efficacy on Plasmodium yoelii yoelii

详细信息    查看全文

• 作者：Norma Rivera (1)
  Yovani Marrero Ponce (2)
  Vicente J. Arán (3)
  Cecilia Martínez (1)
  Filiberto Malagón (1)
  
• 刊名：Parasitology Research
• 出版年：2013
• 出版时间：April 2013
• 年：2013
• 卷：112
• 期：4
• 页码：1523-1527
• 全文大小：127KB
• 参考文献：1. Arora K, Srivastava AK (2005) Antimalarial efficacy of methylene blue and menadione and their effect on glutathione metabolism of / Plasmodium yoelii-infected mice. Parasitol Res 97:521-26 CrossRef
  2. Argotte RR, Ramírez AG, Rodríguez GMC et al (2006) Antimalarial 4-phenylcoumarins from the stem bark of / Hintonia latiflora. J Nat Prod 69:1442-444 CrossRef
  3. Baird JK, Rieckmann KH (2003) Can primaquine therapy for vivax malaria be improved? Trends Parasitol 19(3):115-20 CrossRef
  4. Becker DE (2006) Drug therapy in dental practice: general principles. Part 1—pharmacokinetic considerations. Anesth Prog 53:140-46 CrossRef
  5. Giha H (2010) Artemisinin derivatves for treatment of uncomplicated / Plasmodium falciparum malaria in Sudan: too early for too much hope. Parasitol Res 106:549-52 CrossRef
  6. Goulart HR, Kimura EA, Peres VJ et al (2004) Terpenes arrest parasite development and inhibit biosynthesis of isoprenoids in / Plasmodium falciparum. Antimicrob Agents Chemoter 48:2502-509 CrossRef
  7. H?fle G, B??hlendorf B, Fecker T, Sasse F, Kunze B (2008) Semisynthesis and antiplasmodial activity of the quinoline alkaloid aurachin. J Nat Prod 71(11):1967-969 CrossRef
  8. Jensen M, Mehlhorn H (2009) Seventy-five years of Resochin in the fight against malaria. Parasitol Res 105:609-27 CrossRef
  9. Kaur K, Jain M, Reddy RP, Jain R (2010) Quinolines and structurally related heterocycles as antimalarials. Eur J Med Chem 45(8):3245-264 CrossRef
  10. Lorke D (1983) A new approach to practical acute toxicity testing. Arch Toxicol 54:275-87 CrossRef
  11. Marrero-Ponce Y, Castillo GJ, Olazabal E et al (2004) TOMOCOMD-CARDD, a novel approach for computer-aided ‘rational-drug design: I theoretical and experimental assessment of a promising method for computational screening and in silico design of new anthelmintic compounds. J of Computer-Aided Mol Des 18:615-34 CrossRef
  12. Moneriz C, Marín-García P, Bautista JM, Diez A, Puyet A (2011) Parasitostatic effect of maslinic acid. II. Survival increase and immune protection in lethal / Plasmodium yoelii-infected mice. Malar J 25:10-03
  13. Montero A, García RN, Marrero-Ponce Y et al (2006) Non-stochastic quadratic fingerprints and LDA-based QSAR models in hit and lead generation through virtual screening: theoretical and experimental assessment of a promising method for the discovery of new antimalarial compounds. Eur J Med Chem 41:483-93 CrossRef
  14. Muregi FW, Kirira PG, Ishih A (2011) Novel rational drug design strategies with potential to revolutionize malaria chemotherapy. Curr Med Chem 18(1):113-43 CrossRef
  15. Murray CJL, Rosenfeld L, Lim SS et al (2012) Global malaria mortality between 1980 and 2010: a systematic analysis. Lancet 379:413-43 CrossRef
  16. Peters W, Robinson BL (1992) The chemotherapy of rodent malaria. XLVII. Studies on pyronaridine and other Mannich base antimalarials. Ann Trop Med Parasitol 86(5):455-65
  17. Qiu W-W, Shen Q, Yang F et al (2009) Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase. Bioorg Med Chem Lett 19:6618-622 CrossRef
  18. Quéré L, Wenger R, Schramm HJ (1996) Triterpenes as potential dimerization inhibitors of HIV-1 protease. Biochem Biophys Res Commun 227:484-88 CrossRef
  19. Rangisetty JB, Gupta CN, Prasad AL et al (2001) Synthesis of new arylaminoquinoxalines and their antimalarial activity in mice. J Pharm Pharmacol 53(10):1409-413 CrossRef
  20. Rivera O, Marrero-Ponce Y, Meneses A et al (2009) Discovery of novel trichomonacidals using lda-driven qsar models and bond-based bilinear indices as molecular descriptors. QSAR Com Sci 1:9-6 CrossRef
  21. Schlitzer M (2008) Antimalarial drugs—what is in use and what is in the pipeline. Arch Pharm 341:149-63 CrossRef
  22. Sharma A, Mishra NC (1999) Inhibition of a protein tyrosine kinase activity in / Plasmodium falciparum by chloroquine. Indian J Biochem Biophys 36(5):299-04
  23. Turner VP, Brabb T, Pekow C, Vasbinder M (2011) Administration of substances to laboratory animals: routes of administration and factors to consider. J Am Assoc Lab Anim Sci 50(5):600-13
  24. Vega MC, Montero A, Marrero Y et al (2006) New ligand-based approach for the discovery of antitrypanosomal compounds. Bioorg Med Chem Lett 16:1898-904 CrossRef
  25. Zhang Y, Qi J, Li J et al (2012) A new antimalarial antigen produces partial protection against / Plasmodium yoelii challenge. Parasitol Res 110:1337-345 CrossRef
  
• 作者单位：Norma Rivera (1)
  Yovani Marrero Ponce (2)
  Vicente J. Arán (3)
  Cecilia Martínez (1)
  Filiberto Malagón (1)
  
  1. Laboratorio de Malariología, Departamento de Microbiología y Parasitología, Facultad de Medicina, Universidad Nacional Autónoma de México, México, DF, 04510, Mexico
  2. Unit of Computer-Aided Molecular “Biosilico-Discovery and Bioinformatic Research, Faculty of Chemistry-Pharmacy, Universidad Central “Marta Abreu-de Las Villas, Santa Clara, 54830, Villa Clara, Cuba
  3. Instituto de Química Médica, CSIC, c/ Juan de la Cierva 3, 28006, Madrid, Spain
  
• ISSN：1432-1955

文摘

Compound 1-methyl-7-nitro-4-(5-(piperidin-1-yl)pentyl)-3,4-dihydroquinoxalin-2(1H)-one (VAM2-6) was evaluated against a blood-induced infection with chloroquine-sensitive Plasmodium yoelii yoelii lethal strain in CD1 mice in a 4-day test scheme. LD50 of the compound was 56.51?mg/kg and LD10 was 20.58?mg/kg (taken as the highest dose). Animals were treated by oral gavage of 20, 10, and 5?mg/kg. Mice in the untreated control group showed a progressively increasing parasitemia leading to mouse death on 6?days post-infection; in this group, all mice showed parasites in the blood on the fifth day of sampling; the mean parasitemia on that day was 19.4?%. A 4-day dosage of 20?mg/kg of VAM2-6 showed a 97?% chemosuppression of total parasitemia on the fifth day, a 28?days survival time, and 20?% of cured animals. A 4-day dosage of 10 and 5?mg/kg showed 85 and 37?%, respectively, chemosuppression of total parasitemia on the fifth day; but all mice died from days 6 to 9 post-infection with increasing parasitemia. Mice treated with chloroquine at 5?mg/kg survived during the experiment. The results obtained in this study showed that the infection outcome of P. yoelii yoelii-infected mice is affected by VAM2-6 compound by slowing down the parasite replication, retarding the patency time, and increasing their survival time. Although compound VAM2-6 was active at higher doses than chloroquine, these results leaves a door open to the study of its structure in order to improve its antimalarial activity.