生物活性

• 描述Benzethonium Chloride (BZN), a FDA-approved drug for anti-infective, was found to markedly induce apoptosis and inhibit proliferation and colony formation ability of lung cancer cells in dose- and time-dependent manners. BZN also enhanced the sensitivity of lung cancer cells to gefitinib, the first-line treatment strategy for selected lung cancer patients. Furthermore, BZN significantly delayed the growth of tumor xenografts in nude mice by increasing apoptosis and decreasing Ki-67 proliferation index, without obvious toxic effects to the vital organs of animals^[3]. Benzethonium chloride was identified as a novel cancer-specific compound. For benzethonium (48-hour incubation), the dose required to reduce cell viability by 50% was 3.8 micromol/L in FaDu, 42.2 micromol/L in NIH 3T3, 5.3 micromol/L in C666-1, and 17.0 micromol/L in GM05757. In vitro, this compound did not interfere with the effects of cisplatin, 5-fluorouracil, or gamma-irradiation. Benzethonium chloride induced apoptosis and activated caspases after 12 hours. Loss of mitochondrial membrane potential (DeltaPsiM) preceded cytosolic Ca2+ increase and cell death. In vivo, benzethonium chloride ablated the tumor-forming ability of FaDu cells, delayed the growth of xenograft tumors, and combined additively with local tumor radiation therapy^[4]. The benzethonium chloride wipe can reduce the influence on the semen collection process and does not affect the semen parameters^[5]. Both menadione and benzethonium chloride foliar spray (15 and 5 mM, respectively) and soil drench (5 and 25 mM, respectively) treatments were equally effective in reducing PD symptoms by 54 to 59% and revealed that the effects of both chemical treatments became systemic^[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
  NCT02018068	Injury of Foot, Shoulder or Kn... more >>ee Perineural Analgesia Pain, Postoperative Collapse <<	Not Applicable	Terminated	-	France ... more >> Department of Anesthesiology and critical care, Lapeyronie University Hospital Montpellier, France, 34295 Anesthesia Réanimation Department, Hôpital Saint Roch Nice, France, 06001 Netherlands A Schweitzer Hospital Dordrecht, Netherlands United Arab Emirates Rachid Hospital Dubaï, United Arab Emirates Collapse <<
  NCT03311191	-	-	Recruiting	June 6, 2019	United States, Massachusetts ... more >> Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Kathryn Hall, MS,APC-BC,NE-BC       KHALL7@PARTNERS.ORG    Contact: Joan Braley, RN,BSN,MSM       JBRALEY@mgh.harvard.edu Collapse <<

• 参考文献

• [1] Coates KM, Flood P. Ketamine and its preservative, benzethonium chloride, both inhibit human recombinant alpha7 and alpha4beta2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes. Br J Pharmacol. 2001 Oct;134(4):871-9.

  [2] Zaman Z, Speeleveld E, et al. Inhibition of acetylcholine esterase and choline esterase by benzethonium chloride and avoidance of the benzethonium chloride carry-over inhibitory effect. Eur J Clin Chem Clin Biochem. 1997 Aug;35(8):603-7.

  [3] Huang XH, Wang Y, Hong P, et al. Benzethonium chloride suppresses lung cancer tumorigenesis through inducing p38-mediated cyclin D1 degradation. Am J Cancer Res. 2019;9(11):2397‐2412. Published 2019 Nov 1

  [4] Yip KW, Mao X, Au PY, et al. Benzethonium chloride: a novel anticancer agent identified by using a cell-based small-molecule screen. Clin Cancer Res. 2006;12(18):5557‐5569

  [5] Wang ZQ, Pan LJ, Wei XZ, et al. Zhonghua Nan Ke Xue. 2018;24(7):613‐617

  [6] Zhang S, Jain M, Fleites LA, Rayside PA, Gabriel DW. Identification and Characterization of Menadione and Benzethonium Chloride as Potential Treatments of Pierce's Disease of Grapevines. Phytopathology. 2019;109(2):233‐239

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