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Mefloquine hydrochloride

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Mefloquine hydrochloride is a synthetic antimalarial drug. It is a white, crystalline powder that is soluble in water and alcohol. The compound is used in the treatment and prevention of malaria.

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Lab products found in correlation

Artesunate, by Merck Group (3 mentions) Amodiaquine dihydrochloride dihydrate, by Merck Group (2 mentions) Chloroquine diphosphate, by Merck Group (2 mentions) Atovaquone, by Merck Group (2 mentions) Chloroquine diphosphate salt, by Merck Group (2 mentions) Amodiaquin dihydrochloride dihydrate, by Merck Group (2 mentions) Artemisinin, by Merck Group (2 mentions) Penicillin streptomycin, by Thermo Fisher Scientific (2 mentions) Quinine hemisulfate, by Merck Group (1 mentions) Primaquine phosphate, by Merck Group (1 mentions) Pyronaridine tetraphosphate, by Merck Group (1 mentions) Praziquantel, by Merck Group (1 mentions) Doxycycline hyclate, by Merck Group (1 mentions) Methylene blue, by Merck Group (1 mentions) Clindamycin, by Merck Group (1 mentions) Ferroquine, by Sanofi (1 mentions) In vitro toxicology assay kit, by Merck Group (1 mentions) Prism 5, by GraphPad (1 mentions) Ponatinib, by Selleck Chemicals (1 mentions) Rpmi medium, by Thermo Fisher Scientific (1 mentions)

17 protocols using mefloquine hydrochloride

1

Antimalarial Compounds Preparation Protocol

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Artesunate, mefloquine hydrochloride, amodiaquine dihydrochloride dihydrate, chloroquine diphosphate, primaquine phosphate, quinine hemisulfate, atovaquone, methylene blue, pyronaridine tetraphosphate, doxycycline hyclate, clindamycin and praziquantel were purchased from Sigma-Aldrich. Ferroquine was obtained from Sanofi-Synthelabo, proguanil and cycloguanil from Jacobus Pharmaceutical Company, tigecycline from Wyeth, and mirincamycin hydrochloride enantiomers from Maldevco [45 (link)]. All compounds were dissolved in sterile DMSO except for quinine for which methanol was used and pure M199 medium (without additives) was used to dissolve proguanil, cycloguanil, clindamycin, and pyronaridine. The stock concentration was 50 mM for Artesunate, amodiaquine, chloroquine, atovaquone, quinine, and primaquine, and 100 mM for praziquantel, proguanil, cycloguanil, methylene blue, pyronaridine, clindamycin, doxycycline, and mirincamycin enantiomers, respectively. Mefloquine was dissolved to 24 mM and Ferroquine to 12.5 mM. All stocks were freshly prepared for the study and stored at -20°C. Maximum concentration of the solvent (DMSO, methanol) in the in vitro assays did not exceed 0.8% and did not interfere with parasite viability.
Koehne E., Zander N., Rodi M., Held J., Hoffmann W., Zoleko-Manego R., Ramharter M., Mombo-Ngoma G., Kremsner P.G, & Kreidenweiss A. (2021). Evidence for in vitro and in vivo activity of the antimalarial pyronaridine against Schistosoma. PLoS Neglected Tropical Diseases, 15(6), e0009511.
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2

Cell Viability Assay for Antimalarial Drugs

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Cells were plated at semi-confluency in 96 well plates. NCH644 were attached on ECM Cell-Tak (VWR, Leuven, Belgium) precoated plates. Increasing concentrations of tested compounds (chloroquine diphosphate (Sigma, Overijse, Belgium; C6628) and mefloquine hydrochloride (Sigma, M2319)) were applied for 72 h. Induction of cell death was measured after 72 h with the Sulforhodamine (SRB) assay (In Vitro Toxicology Assay Kit, Sigma). The optical density was measured at 540 nm. The percentage inhibition of cell mass was determined as: % cell mass reduction=(Mean ODcontrol−mean ODsample) × 100/Mean ODcontrol. IC50 was determined with the GraphPad Prism 5 (GraphPad Software, La Jolla, CA, USA).
Abdul Rahim S.A., Dirkse A., Oudin A., Schuster A., Bohler J., Barthelemy V., Muller A., Vallar L., Janji B., Golebiewska A, & Niclou S.P. (2017). Regulation of hypoxia-induced autophagy in glioblastoma involves ATG9A. British Journal of Cancer, 117(6), 813-825.
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3

Characterization of CML Cell Lines

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Human CML cell lines, K562 (kind gift from Dr. Junia Melo), KU812 (kind gift from Dr. S Tiong Ong) and murine CML cell lines, 32Dp210 (kind gift from Dr. Brian Druker) and 32Dp210 T315I mutant (kind gift from Dr. James Griffin) were maintained in suspension in RPMI medium (Thermo Fisher Scientific, USA), supplemented with 10% fetal bovine serum, 4 mM L-glutamine (Hyclone, USA), 1% penicillin/streptomycin (Gibco, Thermo Fisher Scientific, USA). 32Dp210 and 32Dp210 T315I are murine hematopoietic 32D cells transfected with BCR-ABL1 and T315I mutant respectively [18] (link). The cell lines used in our study are validated with short tandem repeat (STR) profile analysis or Sanger sequencing analysis (Table S1 and Figure S1). Imatinib (LC Laboratories, USA) and ponatinib (Selleckchem, USA) were dissolved in sterile distilled water. Mefloquine hydrochloride (Sigma, US) and bafilomycin A1 (Cayman Chemicals, USA) were reconstituted in dimethylsulfoxide (DMSO; Sigma, USA). N-acetyl cysteine (NAC; Sigma, USA) was dissolved in sterile distilled water. α-Tocopherol (Sigma, USA) was dissolved in a mixture of DMSO and 30% ethanol.
Lam Yi H., Than H., Sng C., Cheong M.A., Chuah C, & Xiang W. (2019). Lysosome Inhibition by Mefloquine Preferentially Enhances the Cytotoxic Effects of Tyrosine Kinase Inhibitors in Blast Phase Chronic Myeloid Leukemia. Translational Oncology, 12(9), 1221-1228.
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4

Pharmacological Agents for Neuronal Studies

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D-AP5 (D-(-)−2-Amino-5-phosphopentanoic acid), SR 95531 (2–3-Carboxyprobyl)−3-amino-6(4-methoxyphenyl pyridazinium bromide), and QX-314 chloride were purchased from Abcam, Cambridge, UK. NBQX (2,3-Dioxo-6nitro-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide) was purchased from Tocris Bioscience, Bristol, UK. Alexa Fluor 488 and 594 were purchased from Life Technologies, Carlsbad, California, USA. Mefloquine hydrochloride and DMSO (Dimethyl sulfoxide) were bought from Sigma-Aldrich, St Louis, Missouri, USA.
Hoehne A., McFadden M.H, & DiGregorio D.A. (2020). Feed-forward recruitment of electrical synapses enhances synchronous spiking in the mouse cerebellar cortex. eLife, 9, e57344.
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5

Dissolving Mefloquine and Chloroquine

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Mefloquine hydrochloride and chloroquine diphosphate salt (Sigma-Aldrich. St Louis, MO) were dissolved in a solution of DMSO 50% (Sigma-Aldrich. St Louis, MO) prepared with saline solution. PTZ was dissolved in saline solution and administered with a dose of 70 mg/kg. All the solutions were made the same day of the experiment guarantying cleanliness and avoiding degradation. All the drugs were administered i.p. in a volume of 5 ml/kg. In accordance with Turner and collaborators [31 (link)]; in rats, the maximum amount to administrate for i.p route is 10 ml/kg. For this reason, 5 ml/kg is an ideal volume to facilitate the absorption of substances given i.p.
Franco-Pérez J., Ballesteros-Zebadúa P, & Manjarrez-Marmolejo J. (2015). Anticonvulsant effects of mefloquine on generalized tonic-clonic seizures induced by two acute models in rats. BMC Neuroscience, 16, 7.
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6

Mefloquine Pretreatment in Social Stress

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Mefloquine hydrochloride, Lot #111M4707V, (Sigma-Aldrich, St. Louis, Missouri) was dissolved in dimethyl sulfoxide (DMSO) for a 38mg/mL stock solution. Intraperitoneal injections (drug: 20 mg/kg mefloquine or 5 mg/kg mefloquine in 0.9% saline, or vehicle: 5% DMSO in 0.9% saline) were administered 20 minutes prior to stress. Direct cannula microinfusions (150 µM mefloquine or 1% DMSO in artificial cerebrospinal fluid; see Electrophysiology methods) were performed using a minipump (Harvard Apparatus, Holliston, Massachusetts) and internal cannula (Plastics One, Roanoke, Virginia) at a rate of 0.1 mL/minute for 5 minutes followed by a 5 minute rest period with the cannula still in place. Drug dosing was based on the doses used for malaria treatment (20 mg/kg) and prophylaxis (5 mg/kg) in humans, as well as previous literature using mefloquine to block gap junctions in mice (12 (link), 13 (link)). Since mefloquine has a long elimination half-life of approximately two to three weeks (14 (link)), the drug was given only once as a pretreatment prior to subthreshold social defeat stress. Subsequent behavioral tests were performed without additional drug administrations.
Heshmati M., Golden S.A., Pfau M.L., Christoffel D.J., Seeley E.L., Cahill M.E., Khibnik L.A, & Russo S.J. (2015). Mefloquine in the nucleus accumbens promotes social avoidance and anxiety-like behavior in mice. Neuropharmacology, 101, 351-357.
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7

Antiviral Compound Screening Protocol

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Oseltamivir carboxylate was purchased from MedChemexpress CO., Ltd, (Monmouth Junction, NJ). Lysosomotrophic agents amodiaquin dihydrochloride dihydrate, bafilomycin A from Streptomyces griseus, chloroquine diphosphate salt, quinacrine dihydrochloride, quinidine anhydrous, Mefloquine hydrochloride, and primaquine diphosphate were purchased from Sigma-Aldrich (St-Louis, MO). Quinine sulfate was obtained from Fisher (Fair Lawn, NJ). Calcium modulators calcimycin (A23187), capsaicin, 5-(N,N-Dimethyl) amiloride hydrochloride, and verapamil hydrochoride were purchased from Sigma-Aldrich whereas TMB-8 hydrochloride was purchased from Calbiochem (Mississauga, ON). Mefloquine, calcimycin, bafilomycin A, and capsaicin were dissolved in DMSO (Sigma-Aldrich) in order to have a final solvent concentration of less than 0.1%, whereas other compounds were dissolved in culture medium. At this concentration, DMSO showed no apparent toxicity in MDCK cells (less than 1%, data not shown).
Marois I., Cloutier A., Meunier I., Weingartl H.M., Cantin A.M, & Richter M.V. (2014). Inhibition of Influenza Virus Replication by Targeting Broad Host Cell Pathways. PLoS ONE, 9(10), e110631.
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8

Solubilizing Bioactive Compounds for Research

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Carbenoxolone disodium salt (CBX), glycyrrhizic acid (GCA), and mefloquine hydrochloride (MFQ) were purchased from Sigma-Aldrich. CBX was dissolved in saline (0.9%); GCA and MFQ were dissolved in DMSO initially and then further diluted to the final concentration with saline.
Xu Q., Cheong Y.K., Yang F., Tiwari V., Li J., Liu J., Raja S.N., Li W, & Guan Y. (2014). Intrathecal carbenoxolone inhibits neuropathic pain and spinal wide-dynamic range neuronal activity in rats after an L5 spinal nerve injury. Neuroscience letters, 563, 45-50.
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9

Enantioselective Purification of Mefloquine

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Mefloquine hydrochloride (reference PHR1705) was purchased from Sigma Aldrich (Saint Louis, MO, USA). The (11S, 12R)-mefloquine and (11R, 12S)-mefloquine enantiomers were purified by the laboratory [2 (link)].
Cavasol W7 HP pharma hydroxypropyl-β-cyclodextrin (HP-β-CD) and Cavasol W7 M pharma randomly methylated β-cyclodextrin (RAMEB) were produced by Wacker Chemie AG (Munich, Germany) and purchased from Ashland (Covington, KY, USA). Heptakis(2,6-O-dimethyl)beta-cyclodextrin (DIMEB) was purchased from Cis BIO (Gif sur Yvette, France).
Durand A., Mathiron D., Rigaud S., Djedaini-Pilard F, & Marçon F. (2023). Rapid Study on Mefloquine Hydrochloride Complexation with Hydroxypropyl-β-Cyclodextrin and Randomly Methylated β-Cyclodextrin: Phase Diagrams, Nuclear Magnetic Resonance Analysis, and Stability Assessment. Pharmaceutics, 15(12), 2794.
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10

Modulation of Autophagy Pathways

Cited 2 times
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Mefloquine hydrochloride (Sigma-Aldrich, M2319), Rapamycin (BioAustralis, BIA-R1183), PP242 hydrate (Sigma-Aldrich, P0037) and PI-103, Torin-1, NVP-BEZ-235 (Selleckchem, S1009) were dissolved in DMSO. Drug concentrations were around the doses (mefloquine 10µM and PI-103, Torin-1, NVP-BEZ-235; PP242, 5µM) previously published for analogous in vitro experiments (6 (link), 22 (link)). Established modulators of autophagy were used at a concentration previously reported in similar in vitro experiments: nocodazole, vinblastine (10µM) (23 (link)), PI-103 (5µM), PP242 (5µM), NH4Cl (10 to 20mM) (Sigma-Aldrich, A9434), and chloroquine (Sigma-Aldrich, C6628) (CQ, 5 to 25µM) (22 (link)–27 (link)). CQ,and NH4Cl, were dissolved in PBS (Biochrom, L1825), all the remaining reagents were dissolved in DMSO (Sigma-Aldrich, D8418). Z-Val-Ala-DL-Asp-fluoromethylketone (zVAD-fmk) was purchased from Bachem GmbH (Bachem GmbH, Germany) and used as previously described (28 (link)). Cellular viability remained unaffected even by the highest solvent concentration (DMSO 0.1%).
Shah H., Stankov M., Panayotova-Dimitrova D., Yazdi A., Budida R., Klusmann J.H, & Behrens G.M. (2023). Autolysosomal activation combined with lysosomal destabilization efficiently targets myeloid leukemia cells for cell death. Frontiers in Oncology, 13, 999738.
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