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1

Martín-Pérez, Tania, Irene Heredero-Bermejo, Cristina Verdú-Expósito, and Jorge Pérez-Serrano. "In Vitro Evaluation of the Combination of Melaleuca alternifolia (Tea Tree) Oil and Dimethyl Sulfoxide (DMSO) against Trophozoites and Cysts of Acanthamoeba Strains. Oxygen Consumption Rate (OCR) Assay as a Method for Drug Screening." Pathogens 10, no. 4 (April 19, 2021): 491. http://dx.doi.org/10.3390/pathogens10040491.

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Ameobae belonging to the genus Acanthamoeba are responsible for the human diseases Acanthamoeba keratitis (AK) and granulomatous amoebic encephalitis (GAE). The treatment of these illnesses is hampered by the existence of a resistance stage (cysts). In an attempt to add new agents that are effective against trophozoites and cysts, tea tree oil (TTO) and dimethyl sulfoxide (DMSO), separately and in combination, were tested In Vitro against two Acanthamoeba isolates, T3 and T4 genotypes. The oxygen consumption rate (OCR) assay was used as a drug screening method, which is to some extent useful in amoebicide drug screening; however, evaluation of lethal effects may be misleading when testing products that promote encystment. Trophozoite viability analysis showed that the effectiveness of the combination of both compounds is higher than when either compound is used alone. Therefore, the TTO alone or TTO + DMSO in combination were an amoebicide, but most of the amoebicidal activity in the combination’s treatments seemed to be caused mainly by the TTO effect. In fact, DMSO alone seems to be a non-amoebicide, triggering encystment. Regarding cytotoxicity, these compounds showed toxicity in human corneal epithelial cells (HCEpiC), even at low concentrations when tested in combination. In conclusion, the use of TTO and DMSO, in combination or alone, cannot be recommended as an alternative for AK treatment until more cytotoxicity and cyst adhesion tests are performed.
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Beugelmans, René, Michèle Bois-Choussy, Philippe Gayral, and Marie Christine Rigothier. "Synthèse par SRN1 et évaluation de l'activité amoebicide de nouveaux dérivés quinoléiniques." European Journal of Medicinal Chemistry 23, no. 6 (November 1988): 539–46. http://dx.doi.org/10.1016/0223-5234(88)90097-9.

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3

Toledano-Magaña, Yanis, Ruth Meléndrez-Luévano, Marisol Navarro-Olivarria, Juan Carlos García-Ramos, Marcos Flores-Alamo, Luis Ortiz-Frade, Lena Ruiz-Azuara, and Blanca M. Cabrera-Vivas. "Synthesis, characterization and evaluation of the substituent effect on the amoebicide activity of new hydrazone derivatives." Med. Chem. Commun. 5, no. 7 (2014): 989–96. http://dx.doi.org/10.1039/c4md00075g.

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4

Santos, André L., Regina M. Takeuchi, Nelson R. Stradiotto, Ana Paula Esteves, and Maria José Medeiros. "Study of the electrochemical reduction of amoebicide teclozan and its amperometric determination in pharmaceutical formulations." Journal of the Brazilian Chemical Society 19, no. 6 (2008): 1144–52. http://dx.doi.org/10.1590/s0103-50532008000600014.

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5

García-Ramos, Juan Carlos, Yanis Toledano-Magaña, Luis Gabriel Talavera-Contreras, Marcos Flores-Álamo, Vanessa Ramírez-Delgado, Emmanuel Morales-León, Luis Ortiz-Frade, et al. "Potential cytotoxic and amoebicide activity of first row transition metal compounds with 2,9-bis-(2′,5′-diazahexanyl)-1,1-phenanthroline (L1)." Dalton Transactions 41, no. 34 (2012): 10164. http://dx.doi.org/10.1039/c2dt30224a.

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6

Tomita, Shinichi, Chie Suzuki, Hitomi Wada, Miya Nomachi, Masaki Imayasu, and Kaoru Araki-Sasaki. "Effects of lactoferrin on the viability and the encystment of Acanthamoeba trophozoites." Biochemistry and Cell Biology 95, no. 1 (February 2017): 48–52. http://dx.doi.org/10.1139/bcb-2016-0054.

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Lactoferrin (LF) is an iron-binding basic glycoprotein that has an antimicrobial effect against certain microbes. The purpose of this study is to evaluate the amoebicidal effect of bovine milk LF (bLF) against Acanthamoeba clinical-isolate trophozoites, which cause severe keratitis. Most of the risk factor for Acanthamoeba keratitis is from wearing soft contact lenses (SCLs). Acanthamoeba trophozoites were incubated in bovine LF (bLF) solution, and the ratios of viability and encystment were determined with microscopic analysis of cyst formation. The amoebicidal effect of bLF was assessed by Trypan blue assay. The ratios of viable cells in the presence of iron-free bLF (apo-bLF), native-bLF, and iron-saturated bLF (Fe-bLF) at the concentration of 10 μmol/L for 60 min were 7.7% ± 4.6%, 80.7% ± 10.1%, and 97.3% ± 1.5%, respectively. Apo-bLF showed potent amoebicidal effect against Acanthamoeba trophozoites, but Fe-bLF did not have this effect. After treating with apo-bLF, most dead cells were nonglobular forms of trophozoites but not cystic forms. Encystment of Acanthamoeba was assessed by the sarkosyl-calcofluor white assay. The encystment ratios treated with 0.5% propylene glycol (positive control) and 10 μmol/L apo-bLF for 24 h were 96.12% ± 10.6% and 0.47% ± 0.5%, respectively. These results suggest that the amoebicidal effect of apo-bLF without encystment might lead to the prevention of contamination of Acanthamoeba in SCL stock cases.
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7

Venugopalan, B., B. Patel, PJ Karnik, NJ de Souza, DK Chatterjee, and N. Iyer. "Synthesis of diphenyl bisamidines as potential amoebicides." European Journal of Medicinal Chemistry 31, no. 6 (January 1996): 485–88. http://dx.doi.org/10.1016/0223-5234(96)85169-5.

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8

Anwar, Ayaz, Mohammad Ridwane Mungroo, Simal Khan, Itrat Fatima, Rafaila Rafique, Kanwal, Khalid Mohammed Khan, Ruqaiyyah Siddiqui, and Naveed Ahmed Khan. "Novel Azoles as Antiparasitic Remedies against Brain-Eating Amoebae." Antibiotics 9, no. 4 (April 17, 2020): 188. http://dx.doi.org/10.3390/antibiotics9040188.

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Balamuthia mandrillaris and Naegleria fowleri are opportunistic protozoan pathogens capable of producing infection of the central nervous system with more than 95% mortality rate. Previously, we have synthesized several compounds with antiamoebic properties; however, synthesis of compounds that are analogues of clinically used drugs is a highly desirable approach that can lead to effective drug development against these devastating infections. In this regard, compounds belonging to the azole class possess wide range of antimicrobial properties and used clinically. In this study, six novel benzimidazole, indazole, and tetrazole derivatives were synthesized and tested against brain-eating amoebae. These compounds were tested for their amoebicidal and static properties against N. fowleri and B. mandrillaris. Furthermore, the compounds were conjugated with silver nanoparticles and characterized. The synthetic heterocyclic compounds showed up to 72% and 65% amoebicidal activities against N. fowleri and B. mandrillaris respectively, while expressing up to 75% and 70% amoebistatic activities, respectively. Following conjugation with silver nanoparticles, amoebicidal activities of the drugs increased by up to 46 and 36% versus B. mandrillaris and N. fowleri. Minimal effects were observed when the compounds were evaluated against human cells using cytotoxicity assays. In summary, azole compounds exhibited potent activity against N. fowleri and B. mandrillaris. Moreover, conjugation of the azole compounds with silver nanoparticles further augmented the capabilities of the compounds against amoebae.
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9

Derda, Monika, Edward Hadaś, and Barbara Thiem. "Plant extracts as natural amoebicidal agents." Parasitology Research 104, no. 3 (December 3, 2008): 705–8. http://dx.doi.org/10.1007/s00436-008-1277-9.

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10

Baig, Abdul Mannan, Junaid Iqbal, and Naveed Ahmed Khan. "In VitroEfficacies of Clinically Available Drugs against Growth and Viability of an Acanthamoeba castellanii Keratitis Isolate Belonging to the T4 Genotype." Antimicrobial Agents and Chemotherapy 57, no. 8 (May 13, 2013): 3561–67. http://dx.doi.org/10.1128/aac.00299-13.

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ABSTRACTThe effects of clinically available drugs targeting muscarinic cholinergic, adrenergic, dopaminergic, and serotonergic receptors; intracellular calcium levels and/or the function of calcium-dependent biochemical pathways; ion channels; and cellular pumps were tested against a keratitis isolate ofAcanthamoeba castellaniibelonging to the T4 genotype.In vitrogrowth inhibition (amoebistatic) assays were performed by incubatingA. castellaniiwith various concentrations of drugs in the growth medium for 48 h at 30°C. To determine amoebicidal effects, amoebae were incubated with drugs in phosphate-buffered saline for 24 h, and viability was determined using trypan blue exclusion staining. For controls, amoebae were incubated with the solvent alone. Of the eight drugs tested, amlodipine, prochlorperazine, and loperamide showed potent amoebicidal effects, as no viable trophozoites were observed (>95% kill rate), while amiodarone, procyclidine, digoxin, and apomorphine exhibited up to 50% amoebicidal effects. In contrast, haloperidol did not affect viability, but all the drugs tested inhibitedA. castellaniigrowth. Importantly, amlodipine, prochlorperazine, and loperamide showed compelling cysticidal effects. The cysticidal effects were irreversible, as cysts treated with the aforementioned drugs did not reemerge as viable amoebae upon inoculation in the growth medium. Except for apomorphine and haloperidol, all the tested drugs blocked trophozoite differentiation into cysts in encystation assays. Given the limited availability of effective drugs to treat amoebal infections, the clinically available drugs tested in this study represent potential agents for managing keratitis and granulomatous amoebic encephalitis caused byAcanthamoebaspp. and possibly against other meningoencephalitis-causing amoebae, such asBalamuthia mandrillarisandNaegleria fowleri.
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11

Lorenzo-Morales, Jacob, Ana R. Díaz-Marrero, Francisco Cen-Pacheco, Ines Sifaoui, María Reyes-Batlle, María L. Souto, Antonio Hernández Daranas, José E. Piñero, and José J. Fernández. "Evaluation of Oxasqualenoids from the Red Alga Laurencia viridis against Acanthamoeba." Marine Drugs 17, no. 7 (July 19, 2019): 420. http://dx.doi.org/10.3390/md17070420.

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Acanthamoeba genus is a widely distributed and opportunistic parasite with increasing importance worldwide as an emerging pathogen in the past decades. This protozoan has an active trophozoite stage, a cyst stage, and is dormant and very resistant. It can cause Acanthamoeba keratitis, an ocular sight-threatening disease, and granulomatous amoebic encephalitis, a chronic, very fatal brain pathology. In this study, the amoebicidal activity of sixteen Laurencia oxasqualenoid metabolites and semisynthetic derivatives were tested against Acanthamoeba castellanii Neff. The results obtained point out that iubol (3) and dehydrothyrsiferol (1) possess potent activities, with IC50 values of 5.30 and 12.83 µM, respectively. The hydroxylated congeners thyrsiferol (2) and 22-hydroxydehydrothyrsiferol (4), active in the same value range at IC50 13.97 and 17.00 µM, are not toxic against murine macrophages; thus, they are solid candidates for the development of new amoebicidal therapies.
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12

Aqeel, Yousuf, Ruqaiyyah Siddiqui, Ayaz Anwar, Muhammad Raza Shah, and Naveed Ahmed Khan. "Gold Nanoparticle Conjugation Enhances the Antiacanthamoebic Effects of Chlorhexidine." Antimicrobial Agents and Chemotherapy 60, no. 3 (December 14, 2015): 1283–88. http://dx.doi.org/10.1128/aac.01123-15.

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Acanthamoebakeratitis is a serious infection with blinding consequences and often associated with contact lens wear. Early diagnosis, followed by aggressive topical application of drugs, is a prerequisite in successful treatment, but even then prognosis remains poor. Several drugs have shown promise, including chlorhexidine gluconate; however, host cell toxicity at physiologically relevant concentrations remains a challenge. Nanoparticles, subcolloidal structures ranging in size from 10 to 100 nm, are effective drug carriers for enhancing drug potency. The overall aim of the present study was to determine whether conjugation with gold nanoparticles enhances the antiacanthamoebic potential of chlorhexidine. Gold-conjugated chlorhexidine nanoparticles were synthesized. Briefly, gold solution was mixed with chlorhexidine and reduced by adding sodium borohydride, resulting in an intense deep red color, indicative of colloidal gold-conjugated chlorhexidine nanoparticles. The synthesis was confirmed using UV-visible spectrophotometry that shows a plasmon resonance peak of 500 to 550 nm, indicative of gold nanoparticles. Further characterization using matrix-assisted laser desorption ionization-mass spectrometry showed a gold-conjugated chlorhexidine complex atm/z699 ranging in size from 20 to 100 nm, as determined using atomic force microscopy. To determine the amoebicidal and amoebistatic effects, amoebae were incubated with gold-conjugated chlorhexidine nanoparticles. For controls, amoebae also were incubated with gold and silver nanoparticles alone, chlorhexidine alone, neomycin-conjugated nanoparticles, and neomycin alone. The findings showed that gold-conjugated chlorhexidine nanoparticles exhibited significant amoebicidal and amoebistatic effects at 5 μM. Amoebicidal effects were observed by parasite viability testing using a Trypan blue exclusion assay and flow-cytometric analysis using propidium iodide, while amoebistatic effects were observed using growth assays. In contrast, chlorhexidine alone, at a similar concentration, showed limited effects. Notably, neomycin alone or conjugated with nanoparticles did not show amoebicidal or amoebistatic effects. Pretreatment ofA. castellaniiwith gold-conjugated chlorhexidine nanoparticles reduced amoeba-mediated host cell cytotoxicity from 90% to 40% at 5 μM. In contrast, chlorhexidine alone, at similar concentrations, had no protective effects for the host cells. Similarly, amoebae treated with neomycin alone or neomycin-conjugated nanoparticles showed no protective effects. Overall, these findings suggest that gold-conjugated chlorhexidine nanoparticles hold promise in the improved treatment ofA. castellaniikeratitis.
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13

Ávila-Blanco, Manuel Enrique, Martín Gerardo Rodríguez, José Luis Moreno Duque, Martin Muñoz-Ortega, and Javier Ventura-Juárez. "Amoebicidal Activity of Essential Oil ofDysphania ambrosioides(L.) Mosyakin & Clemants in an Amoebic Liver Abscess Hamster Model." Evidence-Based Complementary and Alternative Medicine 2014 (2014): 1–7. http://dx.doi.org/10.1155/2014/930208.

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Amebiasis is a parasitic disease that extends worldwide and is a public health problem in developing countries. Metronidazole is the drug recommended in the treatment of amebiasis, but its contralateral effects and lack of continuity of treatment induce low efficiency, coupled with the appearance of resistant amoebic strains. Therefore, the search of new compounds with amoebicidal activity is urgent and important. In this study, we evaluated the in vitro and in vivo antiamoebic activity of the essential oilDysphania ambrosioides(L.) Mosyakin & Clemants. It exhibited an IC50= 0.7 mg/mL against trophozoites. The oral administration of essential oil (8 mg/kg and 80 mg/kg) to hamster infected withEntamoeba histolyticareverted the infection. Ascaridole was identified as the main component of essential oil ofD. ambrosioides. The identification of amoebicidal activity of Ascaridole gives support to the traditional use. Further studies with Ascaridole will be carried out to understand the mechanism involved.
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14

Buck, Sally L., Ruth A. Rosenthal, and Barry A. Schlech. "Amoebicidal Activity of Multipurpose Contact Lens Solutions." Eye & Contact Lens: Science & Clinical Practice 31, no. 2 (March 2005): 62–66. http://dx.doi.org/10.1097/01.icl.0000146322.63546.50.

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15

Boost, Maureen V., Guang-Sen Shi, Sindy Lai, and Pauline Cho. "Amoebicidal Effects of Contact Lens Disinfecting Solutions." Optometry and Vision Science 89, no. 1 (January 2012): 44–51. http://dx.doi.org/10.1097/opx.0b013e31823ac85e.

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16

Sauvey, Conall, Gretchen Ehrenkaufer, Da Shi, Anjan Debnath, and Ruben Abagyan. "Antineoplastic kinase inhibitors: A new class of potent anti-amoebic compounds." PLOS Neglected Tropical Diseases 15, no. 2 (February 8, 2021): e0008425. http://dx.doi.org/10.1371/journal.pntd.0008425.

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Entamoeba histolytica is a protozoan parasite which infects approximately 50 million people worldwide, resulting in an estimated 70,000 deaths every year. Since the 1960s E. histolytica infection has been successfully treated with metronidazole. However, drawbacks to metronidazole therapy exist, including adverse effects, a long treatment course, and the need for an additional drug to prevent cyst-mediated transmission. E. histolytica possesses a kinome with approximately 300–400 members, some of which have been previously studied as potential targets for the development of amoebicidal drug candidates. However, while these efforts have uncovered novel potent inhibitors of E. histolytica kinases, none have resulted in approved drugs. In this study we took the alternative approach of testing a set of twelve previously FDA-approved antineoplastic kinase inhibitors against E. histolytica trophozoites in vitro. This resulted in the identification of dasatinib, bosutinib, and ibrutinib as amoebicidal agents at low-micromolar concentrations. Next, we utilized a recently developed computational tool to identify twelve additional drugs with human protein target profiles similar to the three initial hits. Testing of these additional twelve drugs led to the identification of ponatinib, neratinib, and olmutinib were identified as highly potent, with EC50 values in the sub-micromolar range. All of these six drugs were found to kill E. histolytica trophozoites as rapidly as metronidazole. Furthermore, ibrutinib was found to kill the transmissible cyst stage of the model organism E. invadens. Ibrutinib thus possesses both amoebicidal and cysticidal properties, in contrast to all drugs used in the current therapeutic strategy. These findings together reveal antineoplastic kinase inhibitors as a highly promising class of potent drugs against this widespread and devastating disease.
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Rangel-Castañeda, Itzia Azucena, José Manuel Hernández-Hernández, Armando Pérez-Rangel, Sirenia González-Pozos, Pilar Carranza-Rosales, Claudia Lisette Charles-Niño, Gabriela Tapia-Pastrana, Mario Alberto Ramírez-Herrera, and Araceli Castillo-Romero. "Amoebicidal activity of curcumin on Entamoeba histolytica trophozoites." Journal of Pharmacy and Pharmacology 70, no. 3 (February 6, 2018): 426–33. http://dx.doi.org/10.1111/jphp.12867.

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18

Reyes-Batlle, Mura-Escorche, Sifaoui, Otero-Ruiz, Alfaro-Sifuentes, López-Arencibia, Rocha-Cabrera, et al. "In Vitro Evaluation of Combined Commercialized Ophthalmic Solutions Against Acanthamoeba Strains." Pathogens 8, no. 3 (July 25, 2019): 109. http://dx.doi.org/10.3390/pathogens8030109.

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Acanthamoeba is a free-living amoebae genus which is present worldwide in natural and artificial environments. These amoebae are clinically important as causative agents of diseases in humans and other animals such as a fatal encephalitis or a sight threatening Acanthamoeba keratitis (AK). Lately; studies have focused on the search of novel therapeutic options for AK but also to prevent infections. Furthermore; the evaluation of commercialized products seems to be an option for this case since not clinical assays would be required. Thus; we aimed to test the amoebicidal activity of different mixtures of two commercial ophthalmic solutions: Systane® Ultra; which has already shown anti-Acanthamoeba properties; and Naviblef® Daily Care. In addition, we tested their cytotoxic effect against murine macrophages. At the individual level; Naviblef® Daily Care showed to be the most active product against Acanthamoeba spp. Nevertheless; the combinations of Systane® Ultra and Naviblef® Daily Care; showed an improvement in the activity against trophozoites and cysts of Acanthamoeba castellanii Neff. Moreover; the concentration necessary to generate cytotoxic effect against murine macrophages (J774.1) was much higher than the required for the amoebicidal and cysticidal effect achieved in the most effective mixtures.
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19

Sunoto, Sunoto, S. H. Pudjiadi, Suharjono Suharjono, and Z. Sulaiman. "Tiberal (Ro 7-0207-Roche) in the Treatment of Intestinal Amoebiasis - Part II." Paediatrica Indonesiana 16, no. 9-10 (September 18, 2019): 403–11. http://dx.doi.org/10.14238/pi16.9-10.1976.403-11.

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Twenty-four intestinal amoebiasis patients have been treated with a new amoebicid tiberal (Roche) or metronidazole as a control in a dosage of 15- 30 mg/kg body weight per day for 5 consecutive days. The results show that both drugs achieve a 100% cure rate. No side effects or signs of drug toxicity as evaluated from the results of the safety tests were observed. No signs of clinical or parasitological relapses were seen (after discharge. In comparison with the previous trial with a lower dosage (7~ - 15 mg.) and longer course (7 days) the results were even better, e.g. clinical improvement and parasitological disappearance were achieved in a shorter time.
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Bhopale, K. K., K. S. Pradhan, K. B. Masani, and C. L. Kaul. "A comparative study of experimental caecal amoebiasis and the evaluation of amoebicides." Annals of Tropical Medicine & Parasitology 89, no. 3 (June 1995): 253–59. http://dx.doi.org/10.1080/00034983.1995.11812950.

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21

Fabres, Laura Führich, Fabiany da Costa Gonçalves, Eliane Oliveira Salines Duarte, Francisco Kercher Berté, Débora Kélen Si lva da Conceição, Leonildo Alves Ferreira, Henri Stephan Schrekker, and Marilise Brittes Rott. "In Vitro Amoebicidal Activity of Imidazolium Salts Against Trophozoites." Acta Parasitologica 65, no. 2 (January 14, 2020): 317–26. http://dx.doi.org/10.2478/s11686-019-00161-6.

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22

Jung, Jae Woo, Jong Heon Lee, Sung Hee Park, Hak Sun Yu, Yoon Kyung Kim, and Ji-Eun Lee. "Amoebicidal Effect of Nephrite-containing Contact Lens Storage Case." Journal of the Korean Ophthalmological Society 58, no. 5 (2017): 509. http://dx.doi.org/10.3341/jkos.2017.58.5.509.

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Meza-Menchaca, Thuluz, Jorge Suárez-Medellín, Christian Del Ángel-Piña, and Ángel Trigos. "The Amoebicidal Effect of Ergosterol Peroxide Isolated fromPleurotus ostreatus." Phytotherapy Research 29, no. 12 (September 22, 2015): 1982–86. http://dx.doi.org/10.1002/ptr.5474.

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Leon-Sicairos, N., F. Lopez-Soto, M. Reyes-Lopez, D. Godinez-Vargas, C. Ordaz-Pichardo, and M. de la Garza. "Amoebicidal Activity of Milk, Apo-lactoferrin, sIgA and Lysozyme." Clinical Medicine & Research 4, no. 2 (June 1, 2006): 106–13. http://dx.doi.org/10.3121/cmr.4.2.106.

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Reyes-Batlle, M., I. Rodríguez-Talavera, I. Sifaoui, R. L. Rodríguez-Expósito, P. Rocha-Cabrera, J. E. Piñero, and J. Lorenzo-Morales. "In vitro amoebicidal effects of arabinogalactan-based ophthalmic solution." International Journal for Parasitology: Drugs and Drug Resistance 16 (August 2021): 9–16. http://dx.doi.org/10.1016/j.ijpddr.2021.04.005.

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Anwar, Ayaz, Ruqaiyyah Siddiqui, Abdul Hameed, Muhammad R. Shah, and Naveed A. Khan. "Synthetic Dihydropyridines as Novel Antiacanthamoebic Agents." Medicinal Chemistry 16, no. 7 (November 6, 2020): 841–47. http://dx.doi.org/10.2174/1573406415666190722113412.

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Background: Acanthamoeba is an opportunistic pathogen widely spread in the environment. Acanthamoeba causes excruciating keratitis which can lead to blindness. The lack of effective drugs and its ability to form highly resistant cyst are one of the foremost limitations against successful prognosis. Current treatment involves mixture of drugs at high doses but still recurrence of infection can occur due to ineffectiveness of drugs against the cyst form. Pyridine and its natural and synthetic derivatives are potential chemotherapeutic agents due to their diverse biological activities. Objective: To study the antiamoebic effects of four novel synthetic dihydropyridine (DHP) compounds against Acanthamoeba castellanii belonging to the T4 genotype. Furthermore, to evaluate their activity against amoeba-mediated host cells cytopathogenicity as well as their cytotoxicity against human cells. Methods: Dihydropyridines were synthesized by cyclic dimerization of alkylidene malononitrile derivatives. Four analogues of functionally diverse DHPs were tested against Acanthamoeba castellanii by using amoebicidal, encystation and excystation assays. Moreover, Lactate dehydrogenase assays were carried out to study cytopathogenicity and cytotoxicity against human cells. Results: These compounds showed significant amoebicidal and cysticidal effects at 50 μM concentration, whereas, two of the DHP derivatives also significantly reduced Acanthamoebamediated host cell cytotoxicity. Moreover, these DHPs were found to have low cytotoxicity against human cells suggesting a good safety profile. Conclusion: The results suggest that DHPs have potential against Acanthamoeba especially against the more resistant cyst stage and can be assessed further for drug development.
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Fürnkranz, Ursula, Markus Nagl, Waldemar Gottardi, Martina Köhsler, Horst Aspöck, and Julia Walochnik. "Cytotoxic Activity of N-Chlorotaurine on Acanthamoeba spp." Antimicrobial Agents and Chemotherapy 52, no. 2 (November 26, 2007): 470–76. http://dx.doi.org/10.1128/aac.00715-07.

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ABSTRACT Acanthamoeba spp. are the causative agents of Acanthamoeba keratitis (AK), which mainly occurs in contact lens wearers, and of skin lesions, granulomatous amoebic encephalitis (GAE), and disseminating diseases in the immunocompromised host. AK therapy is complex and irritating for the eye, skin lesions are difficult to treat, and there is no effective treatment for GAE. Therefore, new anti-Acanthamoeba drugs are needed. We investigated the anti-Acanthamoeba activity of N-chlorotaurine (NCT), an endogenous mild antiseptic. It was shown that NCT has amoebicidal qualities, both in phosphate-buffered saline (PBS) and in amoebic culture medium. After 6 h of treatment with 10 mM NCT in PBS, the levels of trophozoites of all strains investigated already showed at least a 2-log reduction. When the trophozoites were treated with 20 mM NCT in culture medium, they showed a 2-log reduction after 24 h. The addition of NH4Cl to NCT led to a faster decrease in the numbers of living cells, if tests were carried out in PBS. A delay of excystation was observed when cysts were treated with 55 mM (1%) NCT in culture medium. A complete failure of excystment was the result of treatment with 1% NCT plus 1% NH4Cl in PBS. Altogether, NCT clearly demonstrated amoebicidal activity at concentrations well tolerated by human tissues and might be useful as a topical drug for the treatment of Acanthamoeba infections. The addition of ammonium chloride can be considered to enhance the activity.
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Arrieta, J., B. Reyes, F. Calzada, R. Cedillo-Rivera, and A. Navarrete. "Amoebicidal and giardicidal compounds from the leaves of Zanthoxylum liebmannianun." Fitoterapia 72, no. 3 (March 2001): 295–97. http://dx.doi.org/10.1016/s0367-326x(00)00297-5.

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Alizadeh, Hassan, Sudha Neelam, and H. Dwight Cavanagh. "Amoebicidal Activities of Alexidine Against 3 Pathogenic Strains of Acanthamoeba." Eye & Contact Lens: Science & Clinical Practice 35, no. 1 (January 2009): 1–5. http://dx.doi.org/10.1097/icl.0b013e3181909ae6.

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Vijay, Ajay Kumar, Mahesh Bandara, Hua Zhu, and Mark Duncan P. Willcox. "Protamine as a Potential Amoebicidal Agent for Contact Lens Disinfection." Optometry and Vision Science 90, no. 2 (February 2013): 119–24. http://dx.doi.org/10.1097/opx.0b013e31827cdabc.

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FISCHER-STENGER, KRISTA, GUY A. CABRAL, and FRANCINE MARCIANO-CABRAL. "Separation of Soluble Amoebicidal and Tumoricidal Activity of Activated Macrophages." Journal of Protozoology 39, no. 1 (January 1992): 235–41. http://dx.doi.org/10.1111/j.1550-7408.1992.tb01307.x.

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32

Chiboub, Olfa, Leila Ktari, Ines Sifaoui, Atteneri López-Arencibia, Maria Reyes-Batlle, Mondher Mejri, Basilio Valladares, Manef Abderrabba, José E. Piñero, and Jacob Lorenzo-Morales. "In vitro amoebicidal and antioxidant activities of some Tunisian seaweeds." Experimental Parasitology 183 (December 2017): 76–80. http://dx.doi.org/10.1016/j.exppara.2017.10.012.

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García-Davis, Sara, Ines Sifaoui, María Reyes-Batlle, Ezequiel Viveros-Valdez, José Piñero, Jacob Lorenzo-Morales, José Fernández, and Ana Díaz-Marrero. "Anti-Acanthamoeba Activity of Brominated Sesquiterpenes from Laurencia johnstonii." Marine Drugs 16, no. 11 (November 11, 2018): 443. http://dx.doi.org/10.3390/md16110443.

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Focused on our interest to develop novel antiparasistic agents, the present study was aimed to evaluate the biological activity of an extract of Laurencia johnstonii collected in Baja California Sur, Mexico, against an Acantamoeba castellanii Neff strain. Bioassay-guided fractionation allowed us to identify the amoebicidal diastereoisomers α-bromocuparane (4) and α-isobromocuparane (5). Furthermore, bromination of the inactive laurinterol (1) and isolaurinterol (2) yielded four halogenated derivatives, (6)–(9), which improved the activity of the natural sesquiterpenes. Among them, the most active compound was 3α-bromojohnstane (7), a sesquiterpene derivative which possesses a novel carbon skeleton johnstane.
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Perrine, D., J. P. Chenu, P. Georges, J. C. Lancelot, C. Saturnino, and M. Robba. "Amoebicidal efficiencies of various diamidines against two strains of Acanthamoeba polyphaga." Antimicrobial Agents and Chemotherapy 39, no. 2 (February 1, 1995): 339–42. http://dx.doi.org/10.1128/aac.39.2.339.

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Gomart, Gabrielle, Julie Denis, Tristan Bourcier, Anne Dory, Ahmed Abou-Bacar, Ermanno Candolfi, and Arnaud Sauer. "In Vitro Amoebicidal Activity of Titanium Dioxide/UV-A Combination AgainstAcanthamoeba." Investigative Opthalmology & Visual Science 59, no. 11 (September 14, 2018): 4567. http://dx.doi.org/10.1167/iovs.18-25003.

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36

Stapleton, Fiona, Najat Harmis, Rajesh Deshpande, and David Tran. "Preliminary studies on the amoebicidal efficacy of contact lens disinfection systems." Australian and New Zealand Journal of Ophthalmology 26 (May 1998): S44—S46. http://dx.doi.org/10.1111/j.1442-9071.1998.tb01369.x.

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Cleary, S. F., and F. Marciano-Cabral. "Soluble amoebicidal factors mediate cytolysis of Naegleria fowleri by activated macrophages." Cellular Immunology 101, no. 1 (August 1986): 62–71. http://dx.doi.org/10.1016/0008-8749(86)90186-3.

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38

Sauter, Ismael Pretto, Guilherme Evaldt Rossa, Aline Machado Lucas, Samuel Paulo Cibulski, Paulo Michel Roehe, Luiz Antônio Alves da Silva, Marilise Brittes Rott, Rubem Mário Figueiró Vargas, Eduardo Cassel, and Gilsane Lino von Poser. "Chemical composition and amoebicidal activity of Piper hispidinervum (Piperaceae) essential oil." Industrial Crops and Products 40 (November 2012): 292–95. http://dx.doi.org/10.1016/j.indcrop.2012.03.025.

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Üstüntürk, Miray, and Zuhal Zeybek. "Amoebicidal efficacy of a novel multi-purpose disinfecting solution: First findings." Experimental Parasitology 145 (November 2014): S93—S97. http://dx.doi.org/10.1016/j.exppara.2014.05.011.

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Sauter, Ismael Pretto, Jaqueline Campiol dos Santos, Miriam A. Apel, Samuel Paulo Cibulski, Paulo Michel Roehe, Gilsane Lino von Poser, and Marilise Brittes Rott. "Amoebicidal activity and chemical composition of Pterocaulon polystachyum (Asteraceae) essential oil." Parasitology Research 109, no. 5 (April 27, 2011): 1367–71. http://dx.doi.org/10.1007/s00436-011-2383-7.

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41

Sarker, Imran, A. K. M. Motiur Rahman Bhuiyan, and Md Zilan Miah Sarker. "A middle aged man with Caroli's disease: A case report." Bangabandhu Sheikh Mujib Medical University Journal 9, no. 1 (July 28, 2016): 50. http://dx.doi.org/10.3329/bsmmuj.v9i1.28945.

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Caroli's disease (CD) is a rare congenital abnormality characterized by non-obstructive dilatation of intra hepatic bile ducts, which may be complicated by stone formation, recurrent cholangitis, biliary abscess and higher risk for biliary malignancy. We report a 37-year-old man with recurrent bouts of upper abdominal pain, high grade pyrexia, mild icterus with normal liver function tests who was diagnosed as a case of Caroli's disease. The laboratory studies confirmed Caroli' s disease with a SOL in liver suggestive of liver abscess and the patient received broad spectrum antibiotics with anaerobic and amoebicidal coverage. With 14 days course of antibiotics, he gradually recovered from his symptoms.
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Das, P., L. Narain, GP Dutta, S. Pal, and SC Pal. "IMPROVED METHOD OF PRODUCING AMOEBIC LIVER ABSCESSES IN HAMSTERS FOR SCREENING OF SYSTEMICALLY ACTIVE AMOEBICIDES." Australian Journal of Experimental Biology and Medical Science 63, no. 1 (February 1985): 85–89. http://dx.doi.org/10.1038/icb.1985.10.

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KALYANAM, N., M. A. LIKHATE, and S. G. MANJUNATHA. "ChemInform Abstract: Studies on Antiamoebic Compounds. Part 3. Synthesis and Evaluation of Terpyridines as Amoebicides." ChemInform 23, no. 44 (August 21, 2010): no. http://dx.doi.org/10.1002/chin.199244208.

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Lebbadi, M., A. Galvez, E. Valdivia, M. Martinez-Bueno, and M. Maqueda. "Biological activity of amoebicin m4-A from Bacillus licheniformis M-4." Antimicrobial Agents and Chemotherapy 38, no. 8 (August 1, 1994): 1820–23. http://dx.doi.org/10.1128/aac.38.8.1820.

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45

Reyes-López, M., S. Villa-Treviño, M. Arriaga-Alba, L. Alemán-Lazarini, M. Rodrı́guez-Mendiola, C. Arias-Castro, S. Fattel-Fazenda, and M. de la Garza. "The amoebicidal aqueous extract from Castela texana possesses antigenotoxic and antimutagenic properties." Toxicology in Vitro 19, no. 1 (February 2005): 91–97. http://dx.doi.org/10.1016/j.tiv.2004.06.005.

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Ghadirian, Esfandiar, and Michel Denis. "Entamoeba histolytica Extract and Interferon-Gamma Activation of Macrophage-Mediated Amoebicidal Function." Immunobiology 185, no. 1 (June 1992): 1–10. http://dx.doi.org/10.1016/s0171-2985(11)80312-8.

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47

Leos-Rivas, Catalina, M. Julia Verde-Star, Lidia Osuna Torres, Azucena Oranday-Cardenas, Catalina Rivas-Morales, M. Porfiria Barron-Gonzalez, Mario R. Morales-Vallarta, and Delia E. Cruz-Vega. "In vitro Amoebicidal Activity of Borage (Borago officinalis) Extract on Entamoeba histolytica." Journal of Medicinal Food 14, no. 7-8 (July 2011): 866–69. http://dx.doi.org/10.1089/jmf.2010.0164.

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48

Preet, Simran, Sanjay Bharati, Geeta Shukla, Ashwani Koul, and Praveen Rishi. "Evaluation of Amoebicidal Potential of Paneth Cell Cryptdin-2 against Entamoeba histolytica." PLoS Neglected Tropical Diseases 5, no. 12 (December 20, 2011): e1386. http://dx.doi.org/10.1371/journal.pntd.0001386.

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Borase, Hemant P., Chandrashekhar D. Patil, Ismael P. Sauter, Marilise B. Rott, and Satish V. Patil. "Amoebicidal activity of phytosynthesized silver nanoparticles and theirin vitrocytotoxicity to human cells." FEMS Microbiology Letters 345, no. 2 (July 1, 2013): 127–31. http://dx.doi.org/10.1111/1574-6968.12195.

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Hernández-Ayala, Luis Felipe, Yanis Toledano-Magaña, Luis Ortiz-Frade, Marcos Flores-Alamo, Rodrigo Galindo-Murillo, Miguel Reina, Juan Carlos García-Ramos, and Lena Ruiz-Azuara. "Heteroleptic NiII complexes: Synthesis, structural characterization, computational studies and amoebicidal activity evaluation." Journal of Inorganic Biochemistry 206 (May 2020): 111043. http://dx.doi.org/10.1016/j.jinorgbio.2020.111043.

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