生物活性

• 描述Dequalinium chloride (DECA), a cationic, lipophilic mitochondrial poison, selectively targets the mitochondrial membrane of certain epithelial carcinoma cells, in which it inhibits cellular energy production. After a single ip administration, we found a maximum tolerated dose of 15 mg/kg and a lethal dose (LD50) of 18.3 mg/kg. Single ip doses of 20 and 25 mg/kg produced > 50% mortality^[3]. The compound antagonized M3 mACHRs (M3 muscarinic receptor) with an IC50 of 0.27 μM for dequalinium chloride^[4]. Dequalinium chloride (DQC) is an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity. Vaginal DQC (Fluomizin vaginal tablets) has been shown to have equal clinical efficacy as clindamycin in the treatment of BV(bacterial vaginosis)^[5]. Dequalinium chloride inhibits and kills clinical isolates of A. vaginae at concentrations similar to those of clindamycin and lower than those of metronidazole^[6].
• 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
  NCT02242695	Vulvovaginal Candidiasis	Phase 4	Completed	-	Thailand ... more >> Siriraj Gynaecologic ID and Female STD Unit, Department of Obstetrics & Gynaecology, Faculty of Medicine Siriraj Hospital, Mahidol University Bangkok, Bangkok Noi district, Thailand, 10700 Collapse <<
  NCT01125410	Bacterial Vaginosis	Phase 3	Completed	-	Belgium ... more >> AZ Imelda Ziekenhuis Bonheiden, Belgium AZ St. Dimpna Geel, Belgium AZ Ziekenhuis Oost-Limburg Genk, Belgium AZ Heilig Hart Tienen, Belgium Czech Republic Centrum Ambulantni gynekologie a prodnictvi Brno, Czech Republic Faculty Hospital Brno Brno, Czech Republic University Hospital Hradec Kralove Hradec Kralove, Czech Republic Charles University Prague, Czech Republic Fakultni nemocnice Na Bulovce Prague, Czech Republic Ambulance pro gynekologie a prodnictvi Telc, Czech Republic Germany LMU Munich Munich, Germany Slovakia JLF UK a MFN Martin, Slovakia Switzerland University Hospital of Geneva and Faculty of Medicine Geneva, Switzerland CHUV Lausanne, Switzerland Collapse <<

• 参考文献

• [1] Dunn PM. Dequalinium, a selective blocker of the slow afterhyperpolarization in rat sympathetic neurones in culture. Eur J Pharmacol. 1994 Feb 3;252(2):189-94.

  [2] Manetta A, Emma D, et al. Failure to enhance the in vivo killing of human ovarian carcinoma by sequential treatment with dequalinium chloride and tumor necrosis factor. Gynecol Oncol. 1993 Jul;50(1):38-44.

  [3] Gamboa-Vujicic G, Emma DA, Liao SY, Fuchtner C, Manetta A. Toxicity of the mitochondrial poison dequalinium chloride in a murine model system. J Pharm Sci. 1993 Mar;82(3):231-5

  [4] Bugay V, Wallace DJ, Wang B, Salinas I, Chapparo AP, Smith HR, Dube PH, Brooks EG, Berg KA, Brenner R. Bis-Quinolinium Cyclophane Blockers of SK Potassium Channels Are Antagonists of M3 Muscarinic Acetylcholine Receptors. Front Pharmacol. 2020 Sep 16;11:552211

  [5] Mendling W, Weissenbacher ER, Gerber S, Prasauskas V, Grob P. Use of locally delivered dequalinium chloride in the treatment of vaginal infections: a review. Arch Gynecol Obstet. 2016 Mar;293(3):469-84

  [6] Lopes dos Santos Santiago G, Grob P, Verstraelen H, Waser F, Vaneechoutte M. Susceptibility testing of Atopobium vaginae for dequalinium chloride. BMC Res Notes. 2012 Mar 19;5:151

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