生物活性

• 描述Acetylcysteine is a thiol-containing antioxidant that has been shown to inhibit the binding activity of NF-κB in response to multiple agonists in various cell types. Preincubation of human umbilical vein endothelial cells with acetylcysteine (0 – 40mM) for 1h dose-dependently inhibited IL-1-induced monocytic cell adhesion. The IC50 value of acetylcysteine was 20mM, and the 95% inhibition was observed at 40mM. Acetylcysteine treatment also resulted in a reduction in surface expression of E-selectin and VCAM-1 of 56% and 70%, respectively, in endothelial cells^[4]. In addition, acetylcysteine promoted long-term survival of serum-deprived PC12 cells with an ED50 value of around 30nM. It dose-dependently prevented internucleosomal DNA cleavage at the doses of 10 – 80mM. The presence of acetylcysteine also promoted the survival of neonatal rat sympathetic neurons. In PC12 cells, the thymidine incorporation and proliferation were almost completely blocked by 60mM acetylcysteine with an ED50 value of approximately 30mM^[5]. Administration of SAMP8 mice with acetylcysteine (100mg/kg, once daily, s.c.) for four weeks improved their cognition in both the T‐maze footshock avoidance paradigm and the lever press appetitive task when compared to mice treated with saline^[6].
• 作用机制Acetylcysteine is a thiol and mucolytic agent that acts as an antioxidant by maintaining the balance of intracellular glutathione. The free sulfhydryl group allows acetylcysteine to reduce disulphide bonds, thereby decreasing mucus viscosity and facilitating mucociliary clearance^[7].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  HUVEC cells	5 mM	Function assay	4 h	Antioxidant activity in HUVEC cells assessed as reduction in H2O2-induced GSH activity at 5 mmol/L incubated 4 hrs prior to H2O2 challenge measured after 12 hrs	22841280
  HUVEC cells	5 mM	Function assay	4 h	Inhibition of H2O2-induced cytotoxicity in HUVEC cells assessed as cell viability at 5 mmol/L incubated 4 hrs prior to H2O2 challenge measured after 12 hrs by MTT assay	22841280
  rat PC12 cells	-	Function assay	24 h	Inhibition of hydrogen peroxide induced cytotoxicity in rat PC12 cells pretreated for 24 hrs assessed as elevation of intracellular glutathione level	17158454

• 动物研究
  剂量	Mice: 1000 mg/kg[3] (i.v., MLD)
  给药途径	i.v.
  动物药代数据	Animal Rats[3] Dose 800 mg/kg Administration i.v. AUC0→24h 737350 ng·h/ml (male) 717854 ng·h/ml (female) T1/2 6.42 h (male) 8.67 h (female) Tmax 8.0 h (male) 12.0 h (female) Cmax 295 ng/ml (male) 443 ng/ml (female)

• 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
  NCT00374088	Transposition of Great Vessels... more >> Congenital Heart Disease Collapse <<	Phase 2	Completed	-	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48109-0204 Collapse <<
  NCT00374088	-	-	Completed	-	-
  NCT01878695	Stage 0/1 Breast Cancer ... more >> Post Biopsy Pre-surgery Collapse <<	Phase 1	Completed	-	United States, Pennsylvania ... more >> Jefferson Myrna Brind Center for Integrative Medicine Philadelphia, Pennsylvania, United States, 19107 Collapse <<

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• 参考文献

• [1] Alvirez-Freites EJ, Carter JL, Cynamon MH. In vitro and in vivo activities of gatifloxacin against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2002 Apr;46(4):1022-5.

  [2] Tsai JC, Jain M, et al. Induction of apoptosis by pyrrolidinedithiocarbamate and N-acetylcysteine in vascular smooth muscle cells. J Biol Chem. 1996 Feb 16;271(7):3667-70.

  [3] ACETYLCYSTEINE

  [4] Faruqi RM, Poptic EJ, Faruqi TR, De La Motte C, DiCorleto PE. Distinct mechanisms for N-acetylcysteine inhibition of cytokine-induced E-selectin and VCAM-1 expression. Am J Physiol. 1997 Aug;273(2 Pt 2):H817-26.

  [5] Ferrari G, Yan CY, Greene LA. N-acetylcysteine (D- and L-stereoisomers) prevents apoptotic death of neuronal cells. J Neurosci. 1995 Apr;15(4):2857-66. doi: 10.1523/JNEUROSCI.15-04-02857.1995.

  [6] Farr SA, Poon HF, Dogrukol-Ak D, Drake J, Banks WA, Eyerman E, Butterfield DA, Morley JE. The antioxidants alpha-lipoic acid and N-acetylcysteine reverse memory impairment and brain oxidative stress in aged SAMP8 mice. J Neurochem. 2003 Mar;84(5):1173-83.

  [7] Santus P, Corsico A, Solidoro P, Braido F, Di Marco F, Scichilone N. Oxidative stress and respiratory system: pharmacological and clinical reappraisal of N-acetylcysteine. COPD. 2014 Dec;11(6):705-17.

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