scholarly journals Antigiardial Activity of Podophyllotoxin-Type Lignans from Bursera fagaroides var. fagaroides

Molecules ◽  
2017 ◽  
Vol 22 (5) ◽  
pp. 799 ◽  
Author(s):  
Filiberto Gutiérrez-Gutiérrez ◽  
Ana Puebla-Pérez ◽  
Sirenia González-Pozos ◽  
José Hernández-Hernández ◽  
Armando Pérez-Rangel ◽  
...  
Keyword(s):  
Antigiardial Activity

scholarly journals Antigiardial activity of novel triazolyl-quinolone-based chalcone derivatives: when oxygen makes the difference

2015 ◽  
Vol 6 ◽  
Author(s):  
Vijay Bahadur ◽  
Daniela Mastronicola ◽  
Amit K. Singh ◽  
Hemandra K. Tiwari ◽  
Leopoldo P. Pucillo ◽  
...  
Keyword(s):  
Chalcone Derivatives ◽  
Antigiardial Activity ◽  
The Difference

Antigiardial activity of glycoproteins and glycopeptides fromZiziphushoney

2015 ◽  
Vol 29 (22) ◽  
pp. 2100-2102 ◽  
Author(s):  
Seif Eldin A. Mohammed ◽  
Ahmed S. Kabashi ◽  
Waleed S. Koko ◽  
M. Kamran Azim
Keyword(s):  
Antigiardial Activity

scholarly journals Antigiardial Effect of Kramecyne in Experimental Giardiasis

2017 ◽  
Vol 2017 ◽  
pp. 1-7
Author(s):  
Leticia Eligio-García ◽  
Elida Pontifez-Pablo ◽  
Salúd Pérez-Gutiérrez ◽  
Enedina Jiménez-Cardoso
Keyword(s):  
Side Effects ◽  
High Efficiency ◽  
Morphological Changes ◽  
Lethal Dose ◽  
Expression Of Genes ◽  
Antigiardial Activity ◽  
Resistant Strains ◽  
Polymerase Chain

A variety of drugs are used in giardiasis treatment with different levels of efficiency, presence of side effects, and even formation of resistant strains, so that it is important to search new only-one-dose treatments with high efficiency and less side effects. Kramecyne, an anti-inflammatory compound isolated from methanolic extract ofKrameria cytisoides, does not present toxicity, even at doses of 5,000 mg/kg. The objective was to determine the antigiardial effect of kramecyne overGiardia intestinalis in vitroandin vivoand analyze the expression of genes ERK1, ERK2, and AK on kramecyne treated trophozoites by Real Time Polymerase Chain Reaction (RTPCR). The median lethal dose (LD50) was 40 μg/mL and no morphological changes were observed by staining with blue trypan and light microscopy; experimental gerbil infection was eliminated with 320 μg/Kg of weight. After treatment there were no differences between intestines from treated and untreated gerbils. Kramecyne did not have significant effect over ERK1 and AK, but there are differences in ERK2 expression (p=0.04). Results show antigiardial activity of kramecyne; however the mode of action is still unclear and the evaluation of ultrastructural damage and expressed proteins is an alternative of study to understand the action mechanism.

Antigiardial Activity of Isoflavones fromDalbergia frutescensBark

2000 ◽  
Vol 63 (10) ◽  
pp. 1414-1416 ◽  
Author(s):  
I. A. Khan ◽  
M. A. Avery ◽  
C. L. Burandt ◽  
D. K. Goins ◽  
J. R. Mikell ◽  
...  
Keyword(s):  
Antigiardial Activity

scholarly journals A Reprofiled Drug, Auranofin, Is Effective against Metronidazole-Resistant Giardia lamblia

2013 ◽  
Vol 57 (5) ◽  
pp. 2029-2035 ◽  
Author(s):  
Noa Tejman-Yarden ◽  
Yukiko Miyamoto ◽  
David Leitsch ◽  
Jennifer Santini ◽  
Anjan Debnath ◽  
...  
Keyword(s):  
Protein Function ◽  
Giardia Lamblia ◽  
Diarrheal Disease ◽  
Significant Inhibition ◽  
Chemical Library ◽  
Content Type ◽  
Antigiardial Activity ◽  
Resistant Strains ◽  
Human Use

ABSTRACTGiardiasis is one of the most common causes of diarrheal disease worldwide. Treatment is primarily with 5-nitro antimicrobials, particularly metronidazole. Resistance to metronidazole has been described, and treatment failures can occur in up to 20% of cases, making development of alternative antigiardials an important goal. To this end, we have screened a chemical library of 746 approved human drugs and 164 additional bioactive compounds for activity againstGiardia lamblia. We identified 56 compounds that caused significant inhibition ofG. lambliagrowth and attachment. Of these, 15 were previously reported to have antigiardial activity, 20 were bioactive but not approved for human use, and 21 were drugs approved for human use for other indications. One notable compound of the last group was the antirheumatic drug auranofin. Further testing revealed that auranofin was active in the low (4 to 6)-micromolar range against a range of divergentG. lambliaisolates representing both human-pathogenic assemblages A and B. Most importantly, auranofin was active against multiple metronidazole-resistant strains. Mechanistically, auranofin blocked the activity of giardial thioredoxin oxidoreductase, a critical enzyme involved in maintaining normal protein function and combating oxidative damage, suggesting that this inhibition contributes to the antigiardial activity. Furthermore, auranofin was efficaciousin vivo, as it eradicated infection with differentG. lambliaisolates in different rodent models. These results indicate that the approved human drug auranofin could be developed as a novel agent in the armamentarium of antigiardial drugs, particularly against metronidazole-resistant strains.

scholarly journals Antigiardial Activity of Acetylsalicylic Acid Is Associated with Overexpression of HSP70 and Membrane Transporters

2020 ◽  
Vol 13 (12) ◽  
pp. 440
Author(s):  
Verónica Yadira Ochoa-Maganda ◽  
Itzia Azucena Rangel-Castañeda ◽  
Daniel Osmar Suárez-Rico ◽  
Rafael Cortés-Zárate ◽  
José Manuel Hernández-Hernández ◽  
...  
Keyword(s):  
Acetylsalicylic Acid ◽  
Diarrheal Disease ◽  
Drug Repositioning ◽  
Biological Activities ◽  
Dependent Manner ◽  
Full Spectrum ◽  
Morphological Alterations ◽  
Antigiardial Activity ◽  
Low Toxicity ◽  
Ventral Disk

Giardia lamblia is a flagellated protozoan responsible for giardiasis, a worldwide diarrheal disease. The adverse effects of the pharmacological treatments and the appearance of drug resistance have increased the rate of therapeutic failures. In the search for alternative therapeutics, drug repositioning has become a popular strategy. Acetylsalicylic acid (ASA) exhibits diverse biological activities through multiple mechanisms. However, the full spectrum of its activities is incompletely understood. In this study we show that ASA displayed direct antigiardial activity and affected the adhesion and growth of trophozoites in a time-dose-dependent manner. Electron microscopy images revealed remarkable morphological alterations in the membrane, ventral disk, and caudal region. Using mass spectrometry and real-time quantitative reverse transcription (qRT-PCR), we identified that ASA induced the overexpression of heat shock protein 70 (HSP70). ASA also showed a significant increase of five ATP-binding cassette (ABC) transporters (giABC, giABCP, giMDRP, giMRPL and giMDRAP1). Additionally, we found low toxicity on Caco-2 cells. Taken together, these results suggest an important role of HSPs and ABC drug transporters in contributing to stress tolerance and protecting cells from ASA-induced stress.

Antigiardial activity of Ocimum basilicum essential oil

2007 ◽  
Vol 101 (2) ◽  
pp. 443-452 ◽  
Author(s):  
Igor de Almeida ◽  
Daniela Sales Alviano ◽  
Danielle Pereira Vieira ◽  
Péricles Barreto Alves ◽  
Arie Fitzgerald Blank ◽  
...  
Keyword(s):  
Essential Oil ◽  
Ocimum Basilicum ◽  
Antigiardial Activity

Antiamoebic and Antigiardial Activity of Clerodane Diterpenes from Mexican Salvia Species Used for the Treatment of Diarrhea

2015 ◽  
Vol 29 (10) ◽  
pp. 1600-1604 ◽  
Author(s):  
Fernando Calzada ◽  
Elihú Bautista ◽  
Lilian Yépez-Mulia ◽  
Normand García-Hernandez ◽  
Alfredo Ortega
Keyword(s):  
Clerodane Diterpenes ◽  
Antigiardial Activity

scholarly journals Enhanced Antigiardial Effect of Omeprazole Analog Benzimidazole Compounds

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3979
Author(s):  
Beatriz Hernández-Ochoa ◽  
Saúl Gómez-Manzo ◽  
Adrián Sánchez-Carrillo ◽  
Jaime Marcial-Quino ◽  
Luz María Rocha-Ramírez ◽  
...  
Keyword(s):  
Triosephosphate Isomerase ◽  
Tertiary Structure ◽  
Diarrheal Disease ◽  
Attractive Potential ◽  
Chemical Structures ◽  
Ht29 Cells ◽  
Starting Point ◽  
Nmr Techniques ◽  
Antigiardial Activity

Giardiasis is a diarrheal disease that is highly prevalent in developing countries. Several drugs are available for the treatment of this parasitosis; however, failures in drug therapy are common, and have adverse effects and increased resistance of the parasite to the drug, generating the need to find new alternative treatments. In this study, we synthesized a series of 2-mercaptobenzimidazoles that are derivatives of omeprazole, and the chemical structures were confirmed through mass, 1H NMR, and 13C NMR techniques. The in vitro efficacy compounds against Giardia, as well as its effect on the inhibition of triosephosphate isomerase (TPI) recombinant, were investigated, the inactivation assays were performed with 0.2 mg/mL of the enzyme incubating for 2 h at 37 °C in TE buffer, pH 7.4 with increasing concentrations of the compounds. Among the target compounds, H-BZM2, O2N-BZM7, and O2N-BZM9 had greater antigiardial activity (IC50: 36, 14, and 17 µM on trophozoites), and inhibited the TPI enzyme (K2: 2.3, 3.2, and 2.8 M−1 s−1) respectively, loading alterations on the secondary structure, global stability, and tertiary structure of the TPI protein. Finally, we demonstrated that it had low toxicity on Caco-2 and HT29 cells. This finding makes it an attractive potential starting point for new antigiardial drugs.

Antigiardial Activity of Triterpenoids from Root Bark ofHippocratea excelsa‖

2007 ◽  
Vol 70 (5) ◽  
pp. 863-865 ◽  
Author(s):  
Gonzalo J. Mena-Rejón ◽  
Aida R. Pérez-Espadas ◽  
Rosa E. Moo-Puc ◽  
Roberto Cedillo-Rivera ◽  
I. L. Bazzocchi ◽  
...  
Keyword(s):  
Root Bark ◽  
Antigiardial Activity
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