Enhanced activity of mefloquine and artesunic acid against Plasmodium falciparum in vitro and P. berghei in mice by combination with ciprofloxacin

Andrade, Aron José Pazin de; Varotti, Fernando de Pilla; Freitas, Isabela O.; Souza, Marcus V. N. de; Vasconcelos, Thatyana R. A.; Boechat, Núbia; Krettli, Antoniana U.

doi:10.1016/j.ejphar.2006.11.061

Cited by 31 publications

(37 citation statements)

References 23 publications

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“…Our findings are in agreement with previous study by Andrade et al 14 which showed that combination of mefloquine or artesunic acid with ciprofloxacin were experimentally active against P. falciparum.…”

Section: Effect Of 7 Mg/kg Ciprofloxacin On Artesunateamodiaquine Clesupporting

confidence: 83%

“…Ciprofloxacin forms complexes with multivalent cations that impair its oral absorption. Previous study 14 showed that combination of mefloquine or artesunic acid with ciprofloxacin was experimentally active against P. falciparum. Likewise, a study carried out by Ejikeme and her colleague 15 , showed that 12.9 mg/kg body weight of quinine with 15 mg/kg body weight of ciprofloxacin achieved 87 % reduction in parasitaemia level and significantly reduced mortality in the infected animals compared with other treatment groups Clinically important interactions may occur between ACTs drugs and ciprofloxacin compromising the treatment of either infection.…”

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confidence: 99%

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2016

IJPSR

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This study evaluates the effect of ciprofloxacin (CIP) on the antimalarial activity of artesunate (AS), artemether-lumefantrine (AL) and artesunate-amodiaquine using animal model. Some 120 albino mice infected with chloroquine sensitive Plasmodium berghei NK65 strain were used. The study was carried out in three phases. Phase 1 consisted of eleven groups treated with different doses of either AS, AL, ASAQ or CIP alone. Phase 2 consisted of nine groups treated with 7 mg/kg of CIP (CIP1) combined with different doses of AS, AL, ASAQ. Phase 3 consist of ten groups treated with 14 mg/kg of CIP (CIP2) with different doses of AS, AL, ASAQ. Thin blood films were used to assess parasitemia level daily after administration of drugs for 72 h. Results were analyzed using student t-test and analysis of variance (ANOVA). CIP alone showed antimalarial activity with 63 % parasitemia reduction. Antimalarial activities of AS and AL were significantly enhanced by both 7 and 14 mg/kg of CIP. The antimalarial effect of ASAQ was enhanced but not statistically significant. Low dose ciprofloxacin significantly enhanced the antimalarial activities of Artesunate, ArtemetherLumefanthrine and Artesunate-Amodiaquine This combination may be beneficial in the management of Plasmodium falciparum infection or coinfection with salmonellosis.

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Section: Effect Of 7 Mg/kg Ciprofloxacin On Artesunateamodiaquine Clesupporting

confidence: 83%

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confidence: 99%

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2016

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“…For background information on the pharmacological activity of quinoline derivatives, see: Elslager et al (1969); Font et al (1997); Kaminsky & Meltzer (1968); Musiol et al (2006); Nakamura et al (1999); Palmer et al (1993); Ridley (2002); Sloboda et al (1991); Tanenbaum & Tuffanelli (1980); Warshakoon et al (2006). For recent studies on quinoline-based anti-malarials, see: Andrade et al (2007); Cunico et al (2006); da Silva et al (2003); de Souza et al (2005). For a related crystallographic study on a neutral species related to the title compound, see: Kaiser et al (2009).…”

Section: Related Literaturementioning

confidence: 99%

“…It affects mainly those living in tropical and subtropical areas with an incidence of 500 million cases per year globally (Snow et al, 1999;Breman, 2001;World Health Organization, 1999). As part of our studies (de Souza et al, 2005;Andrade et al, 2007;da Silva et al, 2003;Cunico et al, 2006) of drugs for neglected diseases, various quinoline derivatives with potential antimalarial activities have been investigated. It was during this study that the the title salt hydrate, (I), was characterized.…”

Section: S1 Commentmentioning

confidence: 99%

4-[(2-Chloroethyl)amino]quinolinium chloride monohydrate

et al. 2009

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Key indicators: single-crystal X-ray study; T = 120 K; mean (C-C) = 0.003 Å; R factor = 0.032; wR factor = 0.065; data-to-parameter ratio = 17.8.In the title salt hydrate, C 11 H 12 ClN 2 + ÁCl À ÁH 2 O, the quinolinium core is essentially planar (r.m.s. deviation = 0.027 Å ) with the chloroethyl side chain being almost orthogonal to the core [C-N-C-C torsion angle = À80.0 (3) ]. In the crystal packing, the water molecule bridges three species, forming donor interactions to two chloride anions and accepting a hydrogen bond from the quinolinium H atom. The chloride anion accepts a hydrogen bond from the amine N atom with the result that a two-dimensional supramolecular array is formed in the ac plane. A C-HÁ Á ÁCl interaction also occurs. Related literature

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“…The antimalarial evaluation was done using method described by Andradea et al [17]. Plasmodium berghei (NK 65) strain was used for in vivo evaluation of antimalarial activity in Lacca mice.…”

Section: Evaluation Of Antimalarial Activity Of Quinine Sulphate and mentioning

confidence: 99%

Identification, Characterization and Evaluation of Crystal Forms of Quinine Sulphate

Karan¹,

Chadha²,

Chadha³

et al. 2012

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Crystal engineering concept has been utilized to modify the physico-chemical parameters of a naturally occurring alkaloid, quinine sulphate, by exploring its H-bond interactions to generate different forms. Quinine sulphate is found to exist in four different crystal forms. The Forms I and II depict endo/exo events suggesting conversion of metastable low melting forms to higher melting and stable form indicated by sharp melting endotherms. The low melting form I L is found to be monotropically related to high melting Form I H while low melting Form II L is enantiotropically related to high melting Form II H . The Form III and IV showed broad endotherms accompanied by mass loss in TGA prior to melting indicating the existence of solvatomorphism. The solvent molecules are tightly bound in the crystal lattice of the drug molecules which is shown by high values of the binding energies of the solvents in these two forms. The enthalpy of solution was found to be endothermic for all the forms which followed the order: Form O > Form II > Form III > Form I > Form IV and is further related to the lattice energy suggesting Form II to be least crystalline. The solubility for Form II was found to be highest with maximum release rate in dissolution studies. The effectiveness of new polymorphic forms was confirmed by performing in vivo antimalarial activity against P. berghei infection. The studies have shown an increase in antimalarial activity of Form IV concluding a successful development of new polymorphic form.

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Enhanced activity of mefloquine and artesunic acid against Plasmodium falciparum in vitro and P. berghei in mice by combination with ciprofloxacin

Cited by 31 publications

References 23 publications

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4-[(2-Chloroethyl)amino]quinolinium chloride monohydrate

Identification, Characterization and Evaluation of Crystal Forms of Quinine Sulphate

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