生物活性

• 描述Mefloquine (Hydrochloride) is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. Mefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. Mefloquine can prolong cardiac repolarization, especially when coadministered with halofantrine, an antagonist of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Using patch-clamp electrophysiology we found that mefloquine inhibited KvLQT1/minK channel currents with an IC50 value of approximately 1 microM^[2]. Mefloquine possesses activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria^[3]. The anti-malarial mefloquine was previously shown to be active against E. multilocularis metacestodes in vitro, and in mice infected by intraperitoneal inoculation of metacestodes when administered at 100 mg/kg by oral gavage twice a week for 12 weeks. After 12 weeks of treatment, the presence of parasite lesions was assessed in a liver squeeze chamber and by PCR, and a significantly reduced parasite load was found in mefloquine-treated animals^[4]. Mefloquine (MQ) has a highly selective cytotoxicity that inhibits PCa (prostate cancer) cell growth. MQ also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS (reactive oxygen species) generation^[1].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01976325	Malaria	Not Applicable	Unknown	November 2015	Canada, Ontario ... more >> National Capital Region Occupational Health Clinic Recruiting Ottawa, Ontario, Canada, K1A 0K9 Contact: Louise J Levesque, RN, BScN    613-946-5533    louise.j.levesque@hc-sc.gc.ca    Contact: Lisa Taras, MD, CCFP    613-946-6583    lisa.taras@hc-sc.gc.ca    Ottawa Hospital Research Institute Recruiting Ottawa, Ontario, Canada, K1Y 4E9 Contact: Charde A Morgan, MScPH    613-737-8899 ext 72424    cmorgan@ohri.ca    Contact: Anne E McCarthy, MD    613-737-8899 ext 78184    amccarthy@toh.on.ca    Principal Investigator: Anne E McCarthy, MD, MSc          Sub-Investigator: Charde A Morgan, MScPH          International Association for Medical Assistance to Travellers Recruiting Toronto, Ontario, Canada, M6K 3E3 Contact: Tullia Marcolongo    416-652-0137    tullia@iamat.org Collapse <<
  NCT00902811	Uncomplicated Falciparum Malar... more >>ia Collapse <<	Phase 4	Unknown	December 2009	Myanmar ... more >> Dabhine and Mingan Clinic Recruiting Sittwe, Rakhine, Myanmar Contact: Pyay Phyo Aung       frank_smithuis@yahoo.com    Principal Investigator: Pyay Phyo Aung, MD          Myit Kyi Nar Clinic Recruiting Kachin, Myanmar Contact: Mya Nee Nyo       frank_smithuis@yahoo.com    Principal Investigator: Mya Nee Nyo, MD          Myothugyi Rural Health Center, Bu Thee Daung Recruiting Maungdaw, Myanmar Contact: Arkar Linn Naing       frank_smithuis@yahoo.com    Principal Investigator: Arkar Linn Naing, MD          Lashio Clinic Recruiting Shan, Myanmar Contact: Naing Nyo, MD          Principal Investigator: Naing Zaw, MD Collapse <<
  NCT01107145	Plasmodium Vivax Malaria	Phase 4	Terminated(Extremely slow enro... more >>llment) Collapse <<	-	Brazil ... more >> Hospital Geral Maternidade de Cruzeiro do Sul Cruzeiro do Sul, Acre, Brazil Hospital Municipal Teonila Alves Anajas, Para, Brazil Centro de Pesquisa em Patologias Tropicais Porto Velho, Rondonia, Brazil Collapse <<

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• 参考文献

• [1] Yan KH, Yao CJ, Hsiao CH, et al. Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Oncol Lett. 2013;5(5):1541‐1545

  [2] Kang J, Chen XL, Wang L, Rampe D. Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG. J Pharmacol Exp Ther. 2001;299(1):290‐296

  [3] da Silva Araújo A, Moraes AM, Lourenço MCS, Pessoa CO, da Silva ET, de Souza MVN. Synthesis and Antibacterial Activity of Mefloquine-Based Analogs Against Sensitive and Resistant Mycobacterium tuberculosis Strains. Curr Top Med Chem. 2019;19(9):683‐689

  [4] Rufener R, Ritler D, Zielinski J, et al. Activity of mefloquine and mefloquine derivatives against Echinococcus multilocularis. Int J Parasitol Drugs Drug Resist. 2018;8(2):331‐340