Polyprezinc VS Rebamipide
- Categories:Stomach healthy
- Time of issue:2020-12-04
Polyprezinc VS Rebamipide
- Categories:Stomach healthy
- Time of issue:2020-12-04
Stomach ulcers are caused by an imbalance between aggressive factors (gastric acid) and protective factors (bicarbonate and prostaglandins). In recent years, many studies have focused on new methods to improve the resistance of the gastric mucosa to injury. Various defense mechanisms have been developed to protect the mucosa from acid-induced damage. The gastric epithelium secretes mucosal barrier substances composed of mucin glycoprotein, water, bicarbonate and other factors. Mediators such as prostaglandins, NO and lipoprotein A4 protect the gastric mucosa through epithelial remodeling. Many protein mediators, such as antioxidants, anti-inflammatory cytokines, and growth factors, can regulate defense mechanisms to protect and repair.
Polyprezinc (Polaprezinc, PZ) is a chelate composed of L-carnosine and zinc ions, and is clinically used to treat gastric ulcers. Studies have shown that L-carnosine can promote the growth of granulation tissue and accelerate the healing of ulcers; zinc ions can effectively protect the gastric mucosa from damage. PZ has anti-inflammatory and antioxidant effects and protects the gastric mucosa. Rebamide (RM) is also a drug commonly used clinically for gastric mucosal protection. So, is there any difference between the protective effects of polyprezinc and rebamipide on gastric mucosa? In order to more clearly understand the healing process induced by each drug, we conducted a comparative study to compare the effects of polyprezinc and rebamipide on inflammatory cytokines, antioxidants, growth factors and The effect of heat shock protein expression.
Materials and Method
Male SD rats weighing about 250g were selected for 8 weeks and kept in an environment of 22±1°C and 40-60% relative humidity. They were adapted to the environment at least one week before the experiment and fasted for 24 hours before inducing ulcers.
Alcoholic gastric ulcer
After fasting for 24 hours, 70 rats were randomly divided into 7 groups with 10 rats in each group (Figure 1). Oral normal saline for rats, polyprezinc (PZ 5, 10 and 30 mg/kg) and rebamipide (RM 10, 30 and 100 mg/kg); all rats are given 100% alcohol (1mL/200g) by gavage . They were sacrificed 1 hour later, and the stomach tissue was taken out for observation, and the ulcer index (UI) was calculated.
Figure 1 Animal grouping diagram
Ulcer Index (UI)
The ulcer index was measured according to the Joseph scoring method. The sum of the length (mm) of all gastric hemorrhagic lesions is used as the ulcer index, and the defense percentage is calculated using the formula: [(control group UI-treatment group UI)/control group UI] × 100. Analyze the image with Axiovision software (version 4.8) and detect each hemorrhagic lesion.
Take gastric ulcer mucosal specimens, and determine the total protein content by Bradford protein assay. The same amount of protein in each lane was separated by SDS polyacrylamide gel electrophoresis, transferred to a polyvinyl fluoride membrane under 400mA, 2h conditions, blocked with a blocking solution for 1h at room temperature, and incubated with monoclonal antibodies for 2h at room temperature. After washing the membrane 4 times in 20 phosphate buffered saline (PBS-T) within 1 hour, incubate for 1 hour at room temperature with the corresponding secondary antibody horseradish peroxidase. Using chemiluminescence to make the protein bands visible, and through image scanning analysis, each band is compared with the internal reference protein β-actin.
Statistical analysis was performed using SPSS 18.0, and Duncan multiple range test and Tukey test were used for analysis of variance (ANOVA) to evaluate the difference between the experimental group and the control group. P<0.05 has a significant difference.
Results and observations
Polyprezinc significantly improves ulcer index
The ulcer indexes of rats after pretreatment were: control group (80.86±1.43%), PZ5 (51.56±6.73%), PZ10 (20.08±3.80%), PZ30 (7.54±2.17%), RM10 (67.57±7.99%) ), RM30 (48.73±2.95%) and RM100 (18.00±5.15%) (P<0.005). The pathological ulcer index of the PZ group and RM group was significantly lower than that of the control group (Figure 2 and Figure 3). The anti-ulcer effect of PZ is better than that of RM. PZ protects gastric mucosa in a dose-dependent manner. UI decreases with increasing PZ dose.
Figure 2 Macro photos of gastric injury after administration of PZ group and RM group in the alcohol-induced gastric mucosal injury model in rats
Figure 3 Pathological ulcer index
(Ulcer index: lesion area/total area×100)
Polyprezinc reduces levels of inflammatory cytokines
Alcohol-induced ulcers caused the overexpression of all inflammatory cytokines in the gastric mucosa. After PZ treatment, the expression of IL-1β, IL-6, IL-8 and TNF-α in the gastric mucosa decreased in a dose-dependent manner (P<0.05) (Figure) 4). It shows that polyprezinc has anti-inflammatory effects. The anti-inflammatory effect of RM is similar to that of PZ, and PZ is better than RM in reducing inflammatory factors.
Figure 4 (a) Rat gastric mucosa IL-1β, IL-6, IL-8 and TNF-α expression levels; (b) Western blot to detect the expression of inflammatory cytokines, *Compared with the control group, P<0.05
Polyprezinc has significant antioxidant effect
Compared with the control group, after PZ treatment, the expressions of SOD-1, SOD-2, HO-1, GST, PRXI, and PRXV in the gastric mucosa increased significantly (P<0.05) (Figure 5), indicating that Polyprezinc has Anti-oxidize effect. The antioxidant effect of PZ is better than that of RM.
Figure 5 (a) The expression levels of SOD-1, SOD-2, HO-1, GST, PRXI and PRXV in the gastric mucosa of rats; (b) Western blot to detect the expression of antioxidant enzymes, *Compared with the control group P<0.05
Polyprezinc significantly promotes growth factor expression
Compared with the control group, after PZ treatment, the expression of NGF, VEGF and PDGFB in the gastric mucosa increased significantly (P<0.05) (Figure 6).
Figure 6 (a) The expression level of growth factors in the gastric mucosa of rats; (b) The expression of growth factors detected by western blot, *Compared with the control group, P<0.05
Polyprezinc significantly upregulates HSPs protein expression
After PZ treatment, the expressions of HSP90, HSP70, HSP60, HSP27, and HSP10 in the gastric mucosa of rats were significantly increased, and the expression of HSP70 increased in a dose-dependent manner (P<0.05) (Figure 7), which shows that PZ can cause alcohol-induced gastric mucosal damage Has a protective effect.
Figure 7 (a) HSP90, HSP70, HSP60, HSP27 and HSP10 expression levels in the gastric mucosa of rats; (b) Western blot to detect the expression of HSPs, *Compared with the control group, P<0.05
In this study, we compared the healing effects of polyprezinc and rebamipide on ulcer healing. Rebamipide is a gastroprotective drug with multiple effects, including the induction of cyclooxygenase-2 (COX-2) and prostaglandin. However, polyprezinc has a cytoprotective effect that does not depend on prostaglandins. Studies have shown that polyprezinc can significantly improve alcohol-induced mucosal damage, by reducing the level of inflammatory factors, increasing the expression of antioxidant enzymes and up-regulating the expression of growth factors to exert mucosal effects Protective effect; in addition, polyprezinc also exerts a cytoprotective effect by up-regulating heat shock proteins; at the same time, we found that antioxidant activity is an important mechanism for polyprezinc to exert its effects, and the effects of gastrointestinal protection and ulcer healing are derived from this.
Therefore, polyprezinc is a multi-target mucosal protective agent with dual mechanisms of protection and repair. Relaisen (Polyprezinc Granules) is a safe and effective mucosal protective agent that can be widely used in clinical practice.
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