A colorimetric method for the evaluation of anti-giardial drugs in vitro

Hounkong, Kruawan; Sawangjaroen, Nongyao; Phongpaichit, Souwalak

doi:10.1016/j.exppara.2010.09.006

Cited by 8 publications

(7 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The in vitro assays were performed according to Bénéré et al (2007) and Hounkong et al (2011) with modifications. All compounds were dissolved and serially diluted in 1:1vol ethanol/DMSO.…”

Section: Methodsmentioning

confidence: 99%

The FAD-dependent glycerol-3-phosphate dehydrogenase of Giardia duodenalis: an unconventional enzyme that interacts with the g14-3-3 and it is a target of the antitumoral compound NBDHEX

et al. 2015

View full text Add to dashboard Cite

The flagellated protozoan Giardia duodenalis is a worldwide parasite causing giardiasis, an acute and chronic diarrheal disease. Metabolism in G. duodenalis has a limited complexity thus making metabolic enzymes ideal targets for drug development. However, only few metabolic pathways (i.e., carbohydrates) have been described so far. Recently, the parasite homolog of the mitochondrial-like glycerol-3-phosphate dehydrogenase (gG3PD) has been identified among the interactors of the g14-3-3 protein. G3PD is involved in glycolysis, electron transport, glycerophospholipids metabolism, and hyperosmotic stress response, and is emerging as promising target in tumor treatment. In this work, we demonstrate that gG3PD is a functional flavoenzyme able to convert glycerol-3-phosphate into dihydroxyacetone phosphate and that its activity and the intracellular glycerol level increase during encystation. Taking advantage of co-immunoprecipitation assays and deletion mutants, we provide evidence that gG3PD and g14-3-3 interact at the trophozoite stage, the intracellular localization of gG3PD is stage dependent and it partially co-localizes with mitosomes during cyst development. Finally, we demonstrate that the gG3PD activity is affected by the antitumoral compound 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol, that results more effective in vitro at killing G. duodenalis trophozoites than the reference drug metronidazole. Overall, our results highlight the involvement of gG3PD in processes crucial for the parasite survival thus proposing this enzyme as target for novel antigiardial interventions.

show abstract

Section: Methodsmentioning

confidence: 99%

The FAD-dependent glycerol-3-phosphate dehydrogenase of Giardia duodenalis: an unconventional enzyme that interacts with the g14-3-3 and it is a target of the antitumoral compound NBDHEX

et al. 2015

View full text Add to dashboard Cite

show abstract

“…1. This method is convenient and reliable and has been used previously to assess the antigiardial activity of drugs (Busatti et al 2009;Hounkong et al 2011). side effects and non-negligible failure rates (Gardner and Hill, 2001;Müller and von Allmen, 2005).…”

Section: Discussionmentioning

confidence: 99%

“…The plate was washed and incubated for 20 min with HCl 0·1M, the dye removed and the absorbance was determined at 655 nm (Hounkong et al . 2011). Growth inhibition was calculated as a percentage by comparison with negative controls (Rufino-González et al .…”

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

In vitro activity of ‘Mexican Arnica’ Heterotheca inuloides Cass natural products and some derivatives against Giardia intestinalis

et al. 2014

View full text Add to dashboard Cite

Giardiasis is a gastrointestinal disease that affects humans and other animals caused by parasitic protists of the genus Giardia. Giardia intestinalis (Syn. Giardia lamblia; Giardia duodenalis) infections can cause acute or chronic diarrhoea, dehydration, abdominal discomfort and weight loss. Metronidazole is the most widely used drug for treating giardiasis. Although effective, metronidazol has undesirable secondary effects. Plants used in traditional medicine as antidiarrhoeals or antiparasitics may represent alternative sources for new compounds to treat giardiasis. Heterotheca inuloides Cass. (Asteraceae/Compositae) plant is widely used in Mexican traditional medicine. The following secondary metabolites were isolated from H. inuloides flowers: 7-hydroxy-3,4-dihydrocadalene (1), 7-hydroxycadalene (2), 3,7-dihydroxy-3(4H)-isocadalen-4-one (3), 1R,4R-hydroxy-1,2,3,4-tetrahydrocadalen-15-oic acid (4), quercetin (5), quercetin-3,7,3'-trimethyl ether (6), quercetin-3,7,3',4'-tetramethyl ether (7) and eriodictyol-7,4'-dimethyl ether (8). The activity of these compounds against Giardia intestinalis trophozoites was assessed in vitro as was the activity of the semisynthetic compounds 7-acetoxy-3,4-dihydrocadalene (9), 7-benzoxy-3,4-dihydrocadalene (10), 7-acetoxycadalene (11), 7-benzoxycadalene (12), quercetin pentaacetate (13) and 7-hydroxycalamenene (14). Among these, 7-hydroxy-3,4-dihydrocadalene (1) and 7-hydroxycalamenene (14) were the most active, whereas the remaining compounds showed moderate or no activity. The G. intestinalis trophozoites exposed to compound 1 showed marked changes in cellular architecture along with ultrastructural disorganization. The aim of this study was to evaluate the giardicidal activity of selected H. inuloides metabolites and some semisynthetic derivatives using an in vitro experimental model of giardiasis.

show abstract

“…Metronidazole has been determined in various pharmaceutical preparations, blood plasma and urine by gas chromatography mass spectrometry [3], liquid chromatography [4], high performance liquid chro matography [5][6][7], packed column supercritical fluid chromatography [8], amperometric [9], colorimetric [10], ultra performance liquid chromatography mass spectrometry [11], nuclear magnetic resonance spec troscopy [12], short wavelength near infrared spec troscopy [13], and spectrophotometry [14,15]. A few electrochemical studies have been conducted on the electrochemical behavior and determination of metronidazole in pharmaceuticals and biological sam ples by voltammetric techniques.…”

Section: Introductionmentioning

confidence: 99%

Voltammetric sensitive determination of metronidazole at poly(p-aminobenzene sulfonic acid)-modified glassy carbon electrode

Sağlikoğlu

2015

Russ J Electrochem

View full text Add to dashboard Cite

A glassy carbon electrode (GCE) was modified with electropolymerized film of p aminobenzene sulfonic acid (p ABSA) in pH 7.0 phosphate buffer solution (PBS). The polymer film showed excellent elec trocatalytic activity for the reduction of metronidazole. The DPV technique proposed was successfully applied to the detection of metronidazole in tablet dosage forms. Precision and accuracy of the developed technique were checked by recovery studies.

show abstract

A colorimetric method for the evaluation of anti-giardial drugs in vitro

Cited by 8 publications

References 22 publications

The FAD-dependent glycerol-3-phosphate dehydrogenase of Giardia duodenalis: an unconventional enzyme that interacts with the g14-3-3 and it is a target of the antitumoral compound NBDHEX

The FAD-dependent glycerol-3-phosphate dehydrogenase of Giardia duodenalis: an unconventional enzyme that interacts with the g14-3-3 and it is a target of the antitumoral compound NBDHEX

In vitro activity of ‘Mexican Arnica’ Heterotheca inuloides Cass natural products and some derivatives against Giardia intestinalis

Voltammetric sensitive determination of metronidazole at poly(p-aminobenzene sulfonic acid)-modified glassy carbon electrode

Contact Info

Product

Resources

About