Journal articles: 'Antigiardial'

1

Plummer, S., J. Harris, and D. Lloyd. "Antigiardial drugs." Applied Microbiology and Biotechnology 57, no. 5-6 (December 1, 2001): 614–19. http://dx.doi.org/10.1007/s002530100720.

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Tejman-Yarden, Noa, Yukiko Miyamoto, David Leitsch, Jennifer Santini, Anjan Debnath, Jiri Gut, James H. McKerrow, Sharon L. Reed, and Lars Eckmann. "A Reprofiled Drug, Auranofin, Is Effective against Metronidazole-Resistant Giardia lamblia." Antimicrobial Agents and Chemotherapy 57, no. 5 (February 12, 2013): 2029–35. http://dx.doi.org/10.1128/aac.01675-12.

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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.

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Kaur Bhatia, Richa. "Anti-Protozoal Potential of Heterocyclic Compounds Against Giardiasis." Current Bioactive Compounds 15, no. 3 (May 7, 2019): 280–88. http://dx.doi.org/10.2174/1573407214666180201154009.

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The aim of this literature review is to compile data of heterocyclic antigiardial agents. The importance is to analyze the structural requirements for improved antigiardial activity, to overcome resistance and enhance the bioavailability of the compounds under study. Though, nitroimidazoles/ imidazoles and benzimidazoles are major classes, other heterocyclic scaffolds viz. oxoindolinylidene, dioxodihydroisobenzofuran-5-carboxamide, fluoroquinolone, thieno[2,3-b]pyridine- 5-carbonitrile, α-amino-phosphonate analogs of polyoxins, nitazoxanide benzologue, thiazole and triazolyl- quinolone chalcone also possess activity against Giardia species. Heterocyclic phytoconstituents are also included to have a deep idea of antigiardial activity of herbs possessing heterocyclic constituents.

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Wright, Janelle M., Linda A. Dunn, Peter Upcroft, and Jacqueline A. Upcroft. "Efficacy of antigiardial drugs." Expert Opinion on Drug Safety 2, no. 6 (November 2003): 529–41. http://dx.doi.org/10.1517/14740338.2.6.529.

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ElSohly, H., A. Joshi, and A. Nimrod. "Antigiardial Isoflavones fromMachaerium aristulatum." Planta Medica 65, no. 05 (June 1999): 490. http://dx.doi.org/10.1055/s-2006-960825.

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Langford, T. Dianne, Michael P. Housley, Marianne Boes, Jianzhu Chen, Martin F. Kagnoff, Frances D. Gillin, and Lars Eckmann. "Central Importance of Immunoglobulin A in Host Defense against Giardia spp." Infection and Immunity 70, no. 1 (January 2002): 11–18. http://dx.doi.org/10.1128/iai.70.1.11-18.2002.

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ABSTRACT The protozoan pathogen Giardia is an important cause of parasitic diarrheal disease worldwide. It colonizes the lumen of the small intestine, suggesting that effective host defenses must act luminally. Immunoglobulin A (IgA) antibodies are presumed to be important for controlling Giardia infection, but direct evidence for this function is lacking. B-cell-independent effector mechanisms also exist and may be equally important for antigiardial host defense. To determine the importance of the immunoglobulin isotypes that are transported into the intestinal lumen, IgA and IgM, for antigiardial host defense, we infected gene-targeted mice lacking IgA-expressing B-cells, IgM-secreting B-cells, or all B-cells as controls with Giardia muris or Giardia lamblia GS/M-83-H7. We found that IgA-deficient mice could not eradicate either G. muris or G. lamblia infection, demonstrating that IgA is required for their clearance. Furthermore, although neither B-cell-deficient nor IgA-deficient mice could clear G. muris infections, IgA-deficient mice controlled infection significantly better than B-cell-deficient mice, suggesting the existence of B-cell-dependent but IgA-independent antigiardial defenses. In contrast, mice deficient for secreted IgM antibodies cleared G. muris infection normally, indicating that they have no unique functions in antigiardial host defense. These data, together with the finding that B-cell-deficient mice have some, albeit limited, residual capacity to control G. muris infection, show that IgA-dependent host defenses are central for eradicating Giardia spp. Moreover, B-cell-dependent but IgA-independent and B-cell-independent antigiardial host defenses exist but are less important for controlling infection.

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Bahadur, Vijay, Daniela Mastronicola, Hemandra Kumar Tiwari, Yogesh Kumar, Micol Falabella, Leopoldo Paolo Pucillo, Paolo Sarti, Alessandro Giuffrè, and Brajendra Kumar Singh. "O2-Dependent Efficacy of Novel Piperidine- and Piperazine-Based Chalcones against the Human Parasite Giardia intestinalis." Antimicrobial Agents and Chemotherapy 58, no. 1 (November 11, 2013): 543–49. http://dx.doi.org/10.1128/aac.00990-13.

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ABSTRACTGiardia intestinalisis the most frequent protozoan agent of intestinal diseases worldwide. Though commonly regarded as an anaerobic pathogen, it preferentially colonizes the fairly oxygen-rich mucosa of the proximal small intestine. Therefore, when testing new potential antigiardial drugs, O2should be taken into account, since it also reduces the efficacy of metronidazole, the gold standard drug against giardiasis. In this study, 46 novel chalcones were synthesized by microwave-assisted Claisen-Schmidt condensation, purified, characterized by high-resolution mass spectrometry,1H and13C nuclear magnetic resonance, and infrared spectroscopy, and tested for their toxicity againstG. intestinalisunder standard anaerobic conditions. As a novel approach, compounds showing antigiardial activity under anaerobiosis were also assayed under microaerobic conditions, and their selectivity against parasitic cells was assessed in a counterscreen on human epithelial colorectal adenocarcinoma cells. Among the tested compounds, three [30(a), 31(e), and 33] were more effective in the presence of O2than under anaerobic conditions and killed the parasite 2 to 4 times more efficiently than metronidazole under anaerobiosis. Two of them [30(a) and 31(e)] proved to be selective against parasitic cells, thus representing potential candidates for the design of novel antigiardial drugs. This study highlights the importance of testing new potential antigiardial agents not only under anaerobic conditions but also at low, more physiological O2concentrations.

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Chabra, Aroona, Bahman Rahimi-Esboei, Emran Habibi, Taha Monadi, Mohammad Azadbakht, Taher Elmi, Hossein Keshavarz valian, Javad Akhtari, Mahdi Fakhar, and Farshad Naghshvar. "Effects of some natural products from fungal and herbal sources on Giardia lamblia in vivo." Parasitology 146, no. 9 (April 22, 2019): 1188–98. http://dx.doi.org/10.1017/s0031182019000325.

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AbstractGiardia lamblia (G. lamblia) is the most widely known protozoan parasite that causes human gastrointestinal infection worldwide. Some natural compounds exhibited pivotal effects against different infectious diseases. In this research, the antigiardial activity and cytotoxicity of fungal chitosan, nano-chitosan, Rhamnus cathartica (R. cathartica) and emodin were evaluated in Balb/c mice. Genotyping of G. lamblia was assessed by PCR-RFLP technique. Different concentrations of mentioned compounds were used to check their antigiardial and cytotoxicity effects on human intestinal epithelial cells (HT-29) after 24, 48 and 72 h. The G. lamblia strain used in the current work was genotyped and revealed as an AII assemblage. All the concentration showed acceptable activity against G. lamblia cysts and trophozoites in comparison to the negative and positive controls (furazolidone and metronidazole) in vitro (P < 0.05). Giardia lamblia cysts were susceptible after treatment in all experiments in vivo in comparison to negative control (P < 0.05). Approximately, in most of the concentration, nano-chitosan and emodin were more effective than chitosan and R. cathartica, respectively (P < 0.05). The effects of exposure times in antigiardial and cytotoxicity effects were not statistically significant (P > 0.05). The maximum mortality rate (100%) was achieved at 100 and 50 µg kg−1 concentrations after 48 and 72 h of exposure time, respectively. Our results provide significant information about the new antigiardial agent and proposed the nano-chitosan and emodin for the development of new drugs against G. lamblia in the future.

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Khan, I. A., M. A. Avery, C. L. Burandt, D. K. Goins, J. R. Mikell, T. E. Nash, A. Azadegan, and L. A. Walker. "Antigiardial Activity of Isoflavones fromDalbergia frutescensBark." Journal of Natural Products 63, no. 10 (October 2000): 1414–16. http://dx.doi.org/10.1021/np000010d.

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10

Inge, P. M. G., and M. J. G. Farthing. "A radiometric assay for antigiardial drugs." Transactions of the Royal Society of Tropical Medicine and Hygiene 81, no. 2 (January 1987): 345–47. http://dx.doi.org/10.1016/0035-9203(87)90260-4.

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11

Reynoldson, J. A., R. C. A. Thompson, and R. J. Horton. "Albendazole as a future antigiardial agent." Parasitology Today 8, no. 12 (December 1992): 412–14. http://dx.doi.org/10.1016/0169-4758(92)90193-6.

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12

Riches, Andrew G., Christopher J. S. Hart, Matthieu Schmit, Emmanuel A. Debele, Snigdha Tiash, Erin Clapper, Tina S. Skinner-Adams, and John H. Ryan. "Structural reassignment of a dibenz[." Australian Journal of Chemistry 75, no. 10 (November 10, 2022): 839–45. http://dx.doi.org/10.1071/ch22184.

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A screen for compounds with antigiardial activity in the Compounds Australia Scaffolds library identified SN00797640 (supplied structure being 8-acylaminodibenzoxazepinone 1) as a hit compound with potent anti-parasitic activity (concentration for 50% growth inhibition of Giardia duodenalis, IC50 0.18 μM). To further explore the structure–activity relationships in this series, compound 1 and analogues, including its 7-acylaminodibenzoxazepinone regioisomer (2), were synthesized and assessed for anti-Giardia activity. While regioisomer 2 demonstrated antigiardial activity, resynthesized 1 and other 8-acylaminodibenzoxazepinone analogues were inactive. Comparison of spectroscopic and physical properties demonstrated the correct structure of SN00797640 to be 7-acylamino regioisomer 2. These results highlight the importance of independent synthesis in verifying the structure and activity of screening hits.

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13

Mohammed, Seif Eldin A., Ahmed S. Kabashi, Waleed S. Koko, and M. Kamran Azim. "Antigiardial activity of glycoproteins and glycopeptides fromZiziphushoney." Natural Product Research 29, no. 22 (January 14, 2015): 2100–2102. http://dx.doi.org/10.1080/14786419.2014.986659.

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14

Miller, Richard L., Donald J. Nelson, Stephen W. LaFon, Wayne H. Miller, and Thomas A. Krenitsky. "Antigiardial activity of guanine arabinoside mechanism studies." Biochemical Pharmacology 36, no. 15 (August 1987): 2519–25. http://dx.doi.org/10.1016/0006-2952(87)90525-9.

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15

Eligio-García, Leticia, Elida Pontifez-Pablo, Salúd Pérez-Gutiérrez, and Enedina Jiménez-Cardoso. "Antigiardial Effect of Kramecyne in Experimental Giardiasis." Evidence-Based Complementary and Alternative Medicine 2017 (2017): 1–7. http://dx.doi.org/10.1155/2017/6832789.

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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.

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Voravuthikunchai, Supayang P., Tripetch Kanchanapoom, Nongyao Sawangjaroen, and Nongporn Hutadilok-Towatana. "Antioxidant, antibacterial and antigiardial activities ofWalsura robustaRoxb." Natural Product Research 24, no. 9 (May 20, 2010): 813–24. http://dx.doi.org/10.1080/14786410902819152.

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17

Calzada, Fernando, Mariana Meckes, and Roberto Cedillo-Rivera. "Antiamoebic and Antigiardial Activity of Plant Flavonoids**." Planta Medica 65, no. 01 (February 1999): 78–80. http://dx.doi.org/10.1055/s-2006-960445.

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18

de Almeida, Igor, Daniela Sales Alviano, Danielle Pereira Vieira, Péricles Barreto Alves, Arie Fitzgerald Blank, Angela Hampshire C. S. Lopes, Celuta Sales Alviano, and Maria do Socorro S. Rosa. "Antigiardial activity of Ocimum basilicum essential oil." Parasitology Research 101, no. 2 (March 7, 2007): 443–52. http://dx.doi.org/10.1007/s00436-007-0502-2.

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19

Hernández-Ochoa, Beatriz, Saúl Gómez-Manzo, Adrián Sánchez-Carrillo, Jaime Marcial-Quino, Luz María Rocha-Ramírez, Araceli Santos-Segura, Edson Jiovany Ramírez-Nava, et al. "Enhanced Antigiardial Effect of Omeprazole Analog Benzimidazole Compounds." Molecules 25, no. 17 (September 1, 2020): 3979. http://dx.doi.org/10.3390/molecules25173979.

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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.

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Mena-Rejón, Gonzalo J., Aida R. Pérez-Espadas, Rosa E. Moo-Puc, Roberto Cedillo-Rivera, I. L. Bazzocchi, I. A. Jiménez-Diaz, and Leovigildo Quijano. "Antigiardial Activity of Triterpenoids from Root Bark ofHippocratea excelsa‖." Journal of Natural Products 70, no. 5 (May 2007): 863–65. http://dx.doi.org/10.1021/np060559y.

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21

Hernández-Bolio, Gloria Ivonne, Luis Wiliunfo Torres-Tapia, Rosa Moo-Puc, and Sergio Rubén Peraza-Sánchez. "Antigiardial activity of flavonoids from leaves of Aphelandra scabra." Revista Brasileira de Farmacognosia 25, no. 3 (May 2015): 233–37. http://dx.doi.org/10.1016/j.bjp.2015.04.004.

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22

Farthing, M. J. G., and P. M. G. Inge. "Antigiardial activity of the bile salt-like antibiotic sodium fusidate." Journal of Antimicrobial Chemotherapy 17, no. 2 (1986): 165–71. http://dx.doi.org/10.1093/jac/17.2.165.

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23

Kyere-Davies, G., C. Agyare, A. Debnath, C. Caffrey, and J. Mckerrow. "Antigiardial activity of some plant extracts and fractions from Ghana." Planta Medica 81, S 01 (December 14, 2016): S1—S381. http://dx.doi.org/10.1055/s-0036-1596354.

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24

Carvalho, Thais Batista de, Teresa Cristina Goulart Oliveira-Sequeira, and Semiramis Guimaraes. "In vitro ANTIGIARDIAL ACTIVITY OF THE CYSTEINE PROTEASE INHIBITOR E-64." Revista do Instituto de Medicina Tropical de São Paulo 56, no. 1 (January 2014): 43–47. http://dx.doi.org/10.1590/s0036-46652014000100006.

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The quest for new antiparasitic alternatives has led researchers to base their studies on insights into biology, host-parasite interactions and pathogenesis. In this context, proteases and their inhibitors are focused, respectively, as druggable targets and new therapy alternatives. Herein, we proposed to evaluate the in vitro effect of the cysteine protease inhibitor E-64 on Giardia trophozoites growth, adherence and viability. Trophozoites (105) were exposed to E-64 at different final concentrations, for 24, 48 and 72 h at 37 °C. In the growth and adherence assays, the number of trophozoites was estimated microscopically in a haemocytometer, whereas cell viability was evaluated by a dye-reduction assay using MTT. The E-64 inhibitor showed effect on growth, adherence and viability of trophozoites, however, its better performance was detected in the 100 µM-treated cultures. Although metronidazole was more effective, the E-64 was shown to be able to inhibit growth, adherence and viability rates by ≥ 50%. These results reveal that E-64 can interfere in some crucial processes to the parasite survival and they open perspectives for future investigations in order to confirm the real antigiardial potential of the protease inhibitors.

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Birdi, TannazJ, S. Brijesh, PoonamG Daswani, and Pundarikakshudu Tetali. "In vitro antigiardial and antirotaviral activity of Psidium guajava L. leaves." Indian Journal of Pharmacology 43, no. 5 (2011): 616. http://dx.doi.org/10.4103/0253-7613.84990.

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26

Gutiérrez-Gutiérrez, Filiberto, Ana Puebla-Pérez, Sirenia González-Pozos, José Hernández-Hernández, Armando Pérez-Rangel, Laura Alvarez, Gabriela Tapia-Pastrana, and Araceli Castillo-Romero. "Antigiardial Activity of Podophyllotoxin-Type Lignans from Bursera fagaroides var. fagaroides." Molecules 22, no. 5 (May 13, 2017): 799. http://dx.doi.org/10.3390/molecules22050799.

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27

Abraham, Rebecca J., Mark O'Dea, Bertha Rusdi, Stephen W. Page, Ryan O'Handley, and Sam Abraham. "Giardia duodenalis mouse model for the development of novel antigiardial agents." Journal of Microbiological Methods 145 (February 2018): 7–9. http://dx.doi.org/10.1016/j.mimet.2017.11.025.

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28

Tripathi, D. M., N. Gupta, V. Lakshmi, K. C. Saxena, and A. K. Agrawal. "Antigiardial and immunostimulatory effect ofPiper longum on giardiasis due toGiardia lamblia." Phytotherapy Research 13, no. 7 (November 1999): 561–65. http://dx.doi.org/10.1002/(sici)1099-1573(199911)13:7<561::aid-ptr479>3.0.co;2-w.

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29

Morales-Luna, Laura, Beatriz Hernández-Ochoa, Víctor Martínez-Rosas, Gabriel Navarrete-Vázquez, Daniel Ortega-Cuellar, Yadira Rufino-González, Abigail González-Valdez, et al. "Giardia lamblia G6PD::6PGL Fused Protein Inhibitors Decrease Trophozoite Viability: A New Alternative against Giardiasis." International Journal of Molecular Sciences 23, no. 22 (November 18, 2022): 14358. http://dx.doi.org/10.3390/ijms232214358.

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Treatments to combat giardiasis have been reported to have several drawbacks, partly due to the drug resistance and toxicity of current antiparasitic agents. These constraints have prompted many researchers to investigate new drugs that act against protozoan parasites. Enzyme inhibition is an important means of regulating pathogen metabolism and has recently been identified as a significant alternative target in the search for new treatments. Glucose-6-phosphate dehydrogenase and 6-phosphogluconolactonase (G6PD::6PGL) is a bifunctional enzyme involved in the pentose phosphate pathway (PPP) in Giardia lamblia (G. lamblia). The G. lamblia enzyme is unusual since, unlike the human enzyme, it is a fused enzyme. Here, we show, through inhibition assays, that an in-house chemical library of 120 compounds and four target compounds, named CNZ-7, CNZ-8, CMC-1, and FLP-2, are potent inhibitors of the G. lamblia G6PD::6PGL fused enzyme. With a constant (k2) of 2.3, 3.2, and 2.8 M−1 s−1, respectively, they provoke alterations in the secondary and tertiary protein structure and global stability. As a novel approach, target compounds show antigiardial activity, with IC50 values of 8.7, 15.2, 15.3, and 24.1 µM in trophozoites from G. lamblia. Moreover, these compounds show selectivity against G. lamblia, since, through counter-screening in Caco-2 and HT29 human cells, they were found to have low toxicity. This finding positions these compounds as a potential and attractive starting point for new antigiardial drugs.

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Reyes-Vivas, Horacio, Ignacio de la Mora-de la Mora, Adriana Castillo-Villanueva, Lilian Yépez-Mulia, Gloria Hernández-Alcántara, Rosalia Figueroa-Salazar, Itzhel García-Torres, et al. "Giardial Triosephosphate Isomerase as Possible Target of the Cytotoxic Effect of Omeprazole in Giardia lamblia." Antimicrobial Agents and Chemotherapy 58, no. 12 (September 15, 2014): 7072–82. http://dx.doi.org/10.1128/aac.02900-14.

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ABSTRACTGiardiasis is highly prevalent in the developing world, and treatment failures with the standard drugs are common. This work deals with the proposal of omeprazole as a novel antigiardial drug, focusing on a giardial glycolytic enzyme used to follow the cytotoxic effect at the molecular level. We used recombinant technology and enzyme inactivation to demonstrate the capacity of omeprazole to inactivate giardial triosephosphate isomerase, with no adverse effects on its human counterpart. To establish the specific target in the enzyme, we used single mutants of every cysteine residue in triosephosphate isomerase. The effect on cellular triosephosphate isomerase was evaluated by following the remnant enzyme activity on trophozoites treated with omeprazole. The interaction of omeprazole with giardial proteins was analyzed by fluorescence spectroscopy. The susceptibility to omeprazole of drug-susceptible and drug-resistant strains ofGiardia lambliawas evaluated to demonstrate its potential as a novel antigiardial drug. Our results demonstrate that omeprazole inhibits giardial triosephosphate isomerase in a species-specific manner through interaction with cysteine at position 222. Omeprazole enters the cytoplasmic compartment of the trophozoites and inhibits cellular triosephosphate isomerase activity in a dose-dependent manner. Such inhibition takes place concomitantly with the cytotoxic effect caused by omeprazole on trophozoites.G. lambliatriosephosphate isomerase (GlTIM) is a cytoplasmic protein which can help analyses of how omeprazole works against the proteins of this parasite and in the effort to understand its mechanism of cytotoxicity. Our results demonstrate the mechanism of giardial triosephosphate isomerase inhibition by omeprazole and show that this drug is effectivein vitroagainst drug-resistant and drug-susceptible strains ofG. lamblia.

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31

Domínguez-Vigil, Irma G., Benito D. Mata-Cárdenas, Patricia C. Esquivel-Ferriño, Francisco G. Avalos-Alanís, Javier Vargas-Villarreal, and María del Rayo Camacho-Corona. "Antigiardial Activity of Foeniculum vulgare Hexane Extract and Some of Its Constituents." Plants 11, no. 17 (August 26, 2022): 2212. http://dx.doi.org/10.3390/plants11172212.

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Foeniculum vulgare is used for the treatment of diarrhea in Mexican traditional medicine. Hexane extract showed 94 % inhibition of Giardia duodenalis trophozoites at 300 μg/mL. Therefore, 20 constituents of hexane extract were evaluated to determine their antigiardial activity. Interestingly, six compounds showed good activity toward the parasite. These compounds were (1R,4S) (+)-Camphene (61%), (R)(−)-Carvone (66%), estragole (49%), p-anisaldehyde (67%), 1,3-benzenediol (56%), and trans, trans-2,4-undecadienal (97%). The aldehyde trans, trans-2,4-undecadienal was the most active compound with an IC50 value of 72.11 µg/mL against G. duodenalis trophozoites. This aldehyde was less toxic (IC50 588.8 µg/mL) than positive control metronidazole (IC50 83.5 µg/mL) against Vero cells. The above results could support the use of F. vulgare in Mexican traditional medicine.

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32

Mahfouz, Nadia M., Tarek Aboul-Fadl, and Ahmed K. Diab. "Metronidazole twin ester prodrugs: synthesis, physicochemical properties, hydrolysis kinetics and antigiardial activity." European Journal of Medicinal Chemistry 33, no. 9 (September 1998): 675–83. http://dx.doi.org/10.1016/s0223-5234(98)80026-3.

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33

Meloni, B. P., R. C. A. Thompson, J. A. Reynoldson, and P. Seville. "Albendazole: a more effective antigiardial agent in vitro than metronidazole or tinidazole." Transactions of the Royal Society of Tropical Medicine and Hygiene 84, no. 3 (May 1990): 375–79. http://dx.doi.org/10.1016/0035-9203(90)90324-8.

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34

Harris, Janine C., Sue Plummer, Michael P. Turner, and David Lloyd. "The microaerophilic flagellate Giardia intestinalis: Allium sativum (garlic) is an effective antigiardial." Microbiology 146, no. 12 (December 1, 2000): 3119–27. http://dx.doi.org/10.1099/00221287-146-12-3119.

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35

Blank, Arie Fitzgerald, Evanildes Menezes de Souza, Maria de Fátima Arrigoni-Blank, José Welton Azevedo de Paula, and Péricles Barreto Alves. "Maria Bonita: cultivar de manjericão tipo linalol." Pesquisa Agropecuária Brasileira 42, no. 12 (December 2007): 1811–13. http://dx.doi.org/10.1590/s0100-204x2007001200020.

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'Maria Bonita' é proveniente do acesso PI 197442, do Banco de Germoplasma North Central Regional PI Station, EUA. É uma cultivar de manjericão de copa arredondada, pétalas róseas e sépalas roxas, indicada para o Nordeste brasileiro. Apresenta hábito de crescimento ereto, o que favorece a colheita manual e mecanizada. A produtividade média de matéria seca de folhas e inflorescências foi de 20,97 g por planta, 26,34% superior à testemunha 'Genovese'. Possui teor de 4,96% de óleo essencial, e rendimento de 1,18 mL por planta. Seu componente principal é o linalol (78,12%). Seu óleo essencial possui atividades antinociceptiva e antigiardial.

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Palomo-Ligas, Lissethe, Filiberto Gutiérrez-Gutiérrez, Verónica Yadira Ochoa-Maganda, Rafael Cortés-Zárate, Claudia Lisette Charles-Niño, and Araceli Castillo-Romero. "Identification of a novel potassium channel (GiK) as a potential drug target in Giardia lamblia: Computational descriptions of binding sites." PeerJ 7 (February 27, 2019): e6430. http://dx.doi.org/10.7717/peerj.6430.

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Background The protozoan Giardia lamblia is the causal agent of giardiasis, one of the main diarrheal infections worldwide. Drug resistance to common antigiardial agents and incidence of treatment failures have increased in recent years. Therefore, the search for new molecular targets for drugs against Giardia infection is essential. In protozoa, ionic channels have roles in their life cycle, growth, and stress response. Thus, they are promising targets for drug design. The strategy of ligand-protein docking has demonstrated a great potential in the discovery of new targets and structure-based drug design studies. Methods In this work, we identify and characterize a new potassium channel, GiK, in the genome of Giardia lamblia. Characterization was performed in silico. Because its crystallographic structure remains unresolved, homology modeling was used to construct the three-dimensional model for the pore domain of GiK. The docking virtual screening approach was employed to determine whether GiK is a good target for potassium channel blockers. Results The GiK sequence showed 24–50% identity and 50–90% positivity with 21 different types of potassium channels. The quality assessment and validation parameters indicated the reliability of the modeled structure of GiK. We identified 110 potassium channel blockers exhibiting high affinity toward GiK. A total of 39 of these drugs bind in three specific regions. Discussion The GiK pore signature sequence is related to the small conductance calcium-activated potassium channels (SKCa). The predicted binding of 110 potassium blockers to GiK makes this protein an attractive target for biological testing to evaluate its role in the life cycle of Giardia lamblia and potential candidate for the design of novel antigiardial drugs.

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Quihui-Cota, Luis, Rocio León-Trujillo, Humberto Astiazarán-García, Julián Esparza-Romero, María del Refugio Robles, Ramón E. Robles-Zepeda, Rafael Canett, and Jesús Sánchez-Escalante. "Marked Antigiardial Activity ofYucca baccataExtracts: A Potential Natural Alternative for Treating Protozoan Infections." BioMed Research International 2014 (2014): 1–6. http://dx.doi.org/10.1155/2014/823492.

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Human Giardiosis is a public health problem in Mexico, where the national prevalence was estimated to be up to 68%. Misuse of antiprotozoal drugs may result in low effectiveness and undesirable side effects. Research on natural products is a good strategy for discovering more effective antiparasitic compounds. This study evaluated the antigiardial activity of extracts ofYucca baccata, which is native to northwestern Mexico. Forty-two gerbils (females) were weighed and orally inoculated with5×106Giardiatrophozoites. Two gerbils were selected at random to confirm infection. Forty living gerbils were randomly allocated into 5 treatment groups (8 per group). Gerbils were randomly assigned to be treated with 24.4 mg/mL, 12.2 mg/mL, and 6.1 mg/mL of extracts, metronidazole (2 mg/mL) or PBS, which were intragastrically administered once per day for 3 days. Nine gerbils died during the study course. On day 10 postinfection, gerbils were euthanized and trophozoites were quantified.Yuccaextracts reduced, albeit not significantly, the trophozoite counts in the duodenum segment. Only the high-extract concentration significantly reduced the trophozoite counts in the proximal segment and it was similar to that of metronidazole. Extracts ofY. baccatamay represent an effective and natural therapeutic alternative for human giardiosis.

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Cáceres-Castillo, David, Rubén M. Carballo, Ramiro Quijano-Quiñones, Gumersindo Mirón-López, Manlio Graniel-Sabido, Rosa E. Moo-Puc, and Gonzalo J. Mena-Rejón. "Synthesis, in vitro antigiardial activity, SAR analysis and docking study of substituted chalcones." Medicinal Chemistry Research 29, no. 3 (December 27, 2019): 431–41. http://dx.doi.org/10.1007/s00044-019-02492-5.

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Castillo-Villanueva, Adriana, Yadira Rufino-González, Sara-Teresa Méndez, Angélica Torres-Arroyo, Martha Ponce-Macotela, Mario Noé Martínez-Gordillo, Horacio Reyes-Vivas, and Jesús Oria-Hernández. "Disulfiram as a novel inactivator of Giardia lamblia triosephosphate isomerase with antigiardial potential." International Journal for Parasitology: Drugs and Drug Resistance 7, no. 3 (December 2017): 425–32. http://dx.doi.org/10.1016/j.ijpddr.2017.11.003.

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Leung, Alexander K. C., Amy A. M. Leung, Alex H. C. Wong, Consolato M. Sergi, and Joseph K. M. Kam. "Giardiasis: An Overview." Recent Patents on Inflammation & Allergy Drug Discovery 13, no. 2 (December 4, 2019): 134–43. http://dx.doi.org/10.2174/1872213x13666190618124901.

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Background: Giardiasis is an important cause of waterborne and foodborne diarrhea, daycare center outbreaks, and traveler's diarrhea. Objective: The study aimed to provide an update on the evaluation, diagnosis, and treatment of giardiasis. Methods: A PubMed search was completed in Clinical Queries using the key terms “giardiasis”, "Giardia lamblia", "Giardia duodenalis" and "Giardia intestinalis". The search strategy included metaanalyses, randomized controlled trials, clinical trials, observational studies, and reviews. The search was restricted to the English literature. Patents were searched using the key term “giardiasis” from www.freepatentsonline.com. Results: Giardiasis is caused by the protozoan parasite Giardia lamblia. The parasite is transmitted by the fecal-oral route, frequently through ingestion of contaminated water and food or person-to person transmission. Risk factors for infection include children in day-care settings, child-care workers, institutionalized individuals, travelers in endemic areas, ingestion of contaminated or recreational water, immunodeficiency, cystic fibrosis, and oral-anal sex. Approximately 50 to 75% of infected children are asymptomatic. Other children present acute or chronic diarrhea. Direct fluorescent antibody tests that detect intact organisms, enzyme immunoassays that detect soluble antigens, and multiplex real-time polymerase chain reaction assays that detect specific genes of the parasite in stool samples have improved sensitivity and specificity compared with microscopic examination of stool specimens for the detection of Giardia trophozoites or cysts. Drugs used in the treatment of symptomatic giardiasis are reviewed in this study. Moreover, recent patents related to the management of giardiasis are also discussed. Conclusion: Metronidazole, tinidazole, and nitazoxanide are drugs of choice. Resistance to common antigiardial drugs has increased in recent years, therefore, the search for new molecular targets for antigiardial drugs is urgently needed. In general, treatment of asymptomatic carriers is not recommended. Purification of water supply is an important preventive measure.

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Ochoa-Maganda, Verónica Yadira, Itzia Azucena Rangel-Castañeda, Daniel Osmar Suárez-Rico, Rafael Cortés-Zárate, José Manuel Hernández-Hernández, Armando Pérez-Rangel, Natalia Chiquete-Félix, et al. "Antigiardial Activity of Acetylsalicylic Acid Is Associated with Overexpression of HSP70 and Membrane Transporters." Pharmaceuticals 13, no. 12 (December 3, 2020): 440. http://dx.doi.org/10.3390/ph13120440.

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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.

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Ahmed, Abdelazim, Saad Howladar, Haidar Mohamed, and Sami Al-Robai. "Phytochemistry, Antimicrobial, Antigiardial and Antiamoebic Activities of Selected Plants from Albaha Area, Saudi Arabia." British Journal of Medicine and Medical Research 18, no. 11 (January 10, 2016): 1–8. http://dx.doi.org/10.9734/bjmmr/2016/29803.

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Pancholi, Bhaskaranand, and AC Rana. "Traditional Uses, Phytochemistry and Pharmacological Aspects of Rubus niveus thumb Plant – A Review." Journal of Phytopharmacology 9, no. 6 (December 30, 2020): 438–44. http://dx.doi.org/10.31254/phyto.2020.9610.

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Several plant species are utilized in extraordinary common remedy system around the globe and are viewed as doable marketers for the revelation of new medications. Traditional Chinese medication have a long history of flora therapeutically including multiple species of the genus Rubus (Rosaceae). The pharmacological effects of Rubus include antibacterial, antistress, anticancer, antiaging, antiinflammatory, antigastropathic, antirheumatic, antinocieptive, anxiolytic and antigiardial activities. In India, the roots of Rubus niveus (R. niveus) are utilized to treat women for excessive menstrual bleeding and its juice extract as an antidote of snake bite. R. niveus root helps to relieve rheumatoid pain, clear warmness, detoxify, clear wind damp and deal with dysentery. This review article is focused on the ethanopharmacological, phytochemical and pharmacognostical standardization and pharmacological activity of R. niveus.

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T. Mineno, Bentham Science Publisher, Bentham Science Publisher K.M. Stanford, Bentham Science Publisher L.A. Walker, and Bentham Science Publisher M.A. Avery. "Solution-Phase Parallel Synthesis of an Isoflavone Library for the Discovery of Novel Antigiardial Agents." Combinatorial Chemistry & High Throughput Screening 5, no. 6 (September 1, 2002): 481–87. http://dx.doi.org/10.2174/1386207023330138.

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Sahib, Ahmed, Imad Mohammed, and Saja Sloo. "Antigiardial effect of <i>Anethum graveolens </i>aqueous extract in children." Journal of Intercultural Ethnopharmacology 3, no. 3 (2014): 109. http://dx.doi.org/10.5455/jice.20140523104104.

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Humen, Martín A., Graciela L. De Antoni, Jalil Benyacoub, María E. Costas, Marta I. Cardozo, Leonora Kozubsky, Kim-Yen Saudan, et al. "Lactobacillus johnsonii La1 Antagonizes Giardia intestinalis In Vivo." Infection and Immunity 73, no. 2 (February 2005): 1265–69. http://dx.doi.org/10.1128/iai.73.2.1265-1269.2005.

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ABSTRACT This study describes the in vivo activity of Lactobacillus johnsonii La1 (NCC533) in Giardia intestinalis-infected gerbils (Meriones unguiculatus). Daily administration of lactobacilli in the drinking water from 7 days before inoculation with Giardia trophozoites efficiently prevented G. intestinalis strain WB clone C6 from infecting gerbils. More specifically, shedding of fecal Giardia antigens (GSA65 protein) was diminished in the La1-treated group, and resolution of infection was observed by 21 days postinoculation. Histology and analysis of enzymatic markers of microvillus membrane integrity revealed that probiotic administration also protected against parasite-induced mucosal damage. In addition, a cellular response to Giardia antigens was stimulated in spleen cells from La1-treated gerbils. Results show for the first time the antigiardial effect of probiotic lactobacilli in vivo and provide further insight into the antagonistic properties of lactic acid bacteria against protozoa involved in intestinal infections.

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Calzada, Fernando, Elihú Bautista, Lilian Yépez-Mulia, Normand García-Hernandez, and Alfredo Ortega. "Antiamoebic and Antigiardial Activity of Clerodane Diterpenes from Mexican Salvia Species Used for the Treatment of Diarrhea." Phytotherapy Research 29, no. 10 (July 16, 2015): 1600–1604. http://dx.doi.org/10.1002/ptr.5421.

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Shukla, Geeta, and Ramandeep Kaur Sidhu. "Lactobacillus casei as a probiotic in malnourished Giardia lamblia-infected mice: a biochemical and histopathological study." Canadian Journal of Microbiology 57, no. 2 (February 2011): 127–35. http://dx.doi.org/10.1139/w10-110.

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The study describes the in vivo activity of Lactobacillus casei in malnourished Giardia lamblia -infected BALB/c mice. By experimentation, it was found that daily administration of the probiotic 7 days before inoculation with Giardia trophozoites in malnourished mice efficiently reduced both the severity and duration of giardiasis. More specifically, excretion of Giardia cysts and trophozoites counts were reduced, while faecal lactobacilli counts increased significantly in probiotic-fed malnourished mice, compared with control mice. Interestingly, it was also observed that oral feeding of the probiotic to malnourished mice abrogated all the anthropometric and biochemical anomalies. Histologically, morphological and cellular alteration of microvillus membrane integrity revealed that probiotic administration ameliorated the mucosal damage in malnourished, probiotic-inoculated, Giardia-infected mice compared with the severe microvillus atrophy, œdematous and vacuolated epithelial cells, and ileitis in malnourished Giardia-infected mice. The results clearly show the antigiardial effect of the probiotic in vivo by modulating the gut cells to inhibit the colonization and multiplication of Giardia trophozoites, thus reducing the severity and duration of murine giardiasis.

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Bell, C. A., M. Cory, T. A. Fairley, J. E. Hall, and R. R. Tidwell. "Structure-activity relationships of pentamidine analogs against Giardia lamblia and correlation of antigiardial activity with DNA-binding affinity." Antimicrobial Agents and Chemotherapy 35, no. 6 (June 1, 1991): 1099–107. http://dx.doi.org/10.1128/aac.35.6.1099.

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Barbosa, Elizabeth, Fernando Calzada, and Rafael Campos. "Antigiardial activity of methanolic extracts from Helianthemum glomeratum Lag. and Rubus coriifolius Focke in suckling mice CD-1." Journal of Ethnopharmacology 108, no. 3 (December 2006): 395–97. http://dx.doi.org/10.1016/j.jep.2006.05.026.

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Journal articles on the topic 'Antigiardial'

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