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].
Acetylcysteine/乙酰半胱氨酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Neutrophils
1 mM
30 min
To assess the effect of NAC on NET formation, results showed that NAC reduced PMA-induced NET formation.
Blood Adv. 2020 Jan 28;4(2):312-321.
LS174T
2.5-40 mM
72 h
Acetylcysteine significantly inhibited the proliferation of LS174T cells, particularly at higher concentrations.
J Exp Clin Cancer Res. 2014 Nov 12;33(1):92.
HT29-5M21
1-75 mM
72 h
Acetylcysteine significantly inhibited the proliferation of HT29-5M21 cells, particularly at higher concentrations.
J Exp Clin Cancer Res. 2014 Nov 12;33(1):92.
HT29-5F12
1-75 mM
72 h
Acetylcysteine significantly inhibited the proliferation of HT29-5F12 cells, particularly at higher concentrations.
J Exp Clin Cancer Res. 2014 Nov 12;33(1):92.
KATO-III
1-100 mM
72 h
Acetylcysteine significantly inhibited the proliferation of KATO-III cells, particularly at higher concentrations.
J Exp Clin Cancer Res. 2014 Nov 12;33(1):92.
MKN45
1-100 mM
72 h
Acetylcysteine significantly inhibited the proliferation of MKN45 cells, particularly at higher concentrations.
J Exp Clin Cancer Res. 2014 Nov 12;33(1):92.
Panc-1 cells
1 mM
72 h
To evaluate the effect of NAC/Cu(II) on Panc-1 cells, it was found that NAC/Cu(II) significantly reduced cell viability.
Cancer Lett. 2010 Dec 8;298(2):186-94.
T47D cells
1 mM
72 h
To evaluate the effect of NAC/Cu(II) on T47D cells, it was found that NAC/Cu(II) significantly reduced cell viability.
Cancer Lett. 2010 Dec 8;298(2):186-94.
MDA-MB-231 cells
1 mM
72 h
To evaluate the effect of NAC/Cu(II) on MDA-MB-231 cells, it was found that NAC/Cu(II) significantly reduced cell viability.
Cancer Lett. 2010 Dec 8;298(2):186-94.
A2780 cells
1 mM
72 h
To evaluate NAC as a potential metal ionophore/shuttle, it was found that NAC is cytotoxic only in the presence of copper and inhibits cell growth by inducing apoptosis.
Cancer Lett. 2010 Dec 8;298(2):186-94.
CF sputum
2.5 mM
30 min
To compare the mucolytic effects of MUC-031 and NAC, MUC-031 was more effective in reducing the elastic modulus (G′) of sputum and acted faster. MUC-031 induced mucolysis in 69% of sputum samples within 15 min, compared to 25% for NAC.
Eur Respir J. 2023 May 25;61(5):2202022.
Acetylcysteine/乙酰半胱氨酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
JAK2V617F knockin mouse model
Oral
2 g/L
Starting from 4 to 6 weeks of age, replenished weekly, continuous administration.
To investigate the effect of NAC on thrombosis in MPN mice, results showed that NAC extended the lifespan of JAK2V617F mice and reduced thrombus formation.
Blood Adv. 2020 Jan 28;4(2):312-321.
Mice
ΒENaC-Tg mice
Intratracheal instillation (adult mice) or intranasal instillation (neonatal mice)
131 mg/mL
Three times in one day (acute experiment) or twice daily for two weeks (chronic experiment)
To evaluate the mucolytic efficacy of MUC-031 in βENaC-Tg mice. Acute treatment significantly reduced airway mucus plugging and inflammation; chronic treatment sustained these reductions and improved survival.
Eur Respir J. 2023 May 25;61(5):2202022.
BALB/c mice
Hind leg muscle model
Diet
5%
Daily for 14 days
To investigate the effect of dietary NAC on radical-induced structural changes in DNA, results showed that NAC significantly reduced the concentration of 8-OH-Gua and decreased the variance in the oxidative status of DNA.
Proc Natl Acad Sci U S A. 2002 Apr 30;99(9):5937-41
Rats and mice
Early-life stress (ELS) model and EAAC1 knockout mice
Intraperitoneal injection
50 mg/kg and 150 mg/kg
Once daily for 2 days
NAC injection alleviated depressive-like behaviors in NMS model rats and reduced oxidative stress and neuroinflammation. In EAAC1-/- mice, NAC improved depressive-like behaviors but not impulsive behaviors.
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
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