Hepatoprotective and antioxidant activity of a mangrove plant Lumnitzera racemosa

Objective

To identify the hepatoprotective and in vitro antioxidant activity of Lumnitzera racemosa (L. racemosa) leaf extract.

Methods

Animals in Group 1 served as vehicle control, Group 2 served as hepatotoxin (CCL₄ treated) group, Group 3 served as positive control (Silymarin) group, and Group 4, 5 and 6 served as (75, 150 and 300 mg/kg bw p.o.) L. racemosa leaf extract treated groups. Moreover, in vitro antioxidant DPPH, hydroxyl radical scavenging activity (HRSA), NO, ferric reducing antioxidant power (FRAP), lipid hydroperoxide (LPO) and super oxide dismutase (SOD) were also analyzed for the leaf extract.

Results

The levels of the serum parameters such as serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), alkaline phosphatase (ALP), bilirubin, cholesterol (CHL), sugar and lactate dehydrogenase (LDH) were significantly increased in CCL₄ treated rats when compared with the control group (P<0.05). But the L. racemosa leaf extract treated rats showed maximum reduction of SGOT [(210.36±19.63) IU/L], SGPT [(82.37±13.87) IU/L], ALP [(197.63±23.43) IU/L], bilurubin [(2.15±0.84) mg/dL], cholesterol [(163.83±15.63) mg/dL], sugar [(93.00±7.65) mg/dL] and LDH [(1134.00±285.00) IU/L] were observed with the high dose (300 mg/kg bw) of leaf extract treated rats. Histopathological scores showed that, no visible changes were observed with high dose (300 mg/kg bw) of leaf extract treated rats except few mild necrosis. The IC₅₀ values were observed as (56.37±4.87) µg/mL, (57.68±1.98) µg/mL, (64.15±2.90) µg/mL, (61.94±3.98) µg/mL, (94.53±1.68) µg/mL and (69.7±2.65) µg/mL for DPPH, HRSA, NO, FRAP, LPO and SOD radical scavenging activities, respectively.

Conclusions

In conclusion, the hepatoprotective effect of the L. racemosa leaf extract might be due to the presence of phenolic groups, terpenoids and alkaloids and in vitro antioxidant properties.     

Synthesis and biological evaluation of novel dimethyl[1,1'-biphenyl]-2,2'-dicarboxylate derivatives containing thiazolidine-2,4-dione for the treatment of concanavalin A-induced acute liver injury of BALB/c mice

In this paper, we reported the synthesis of bifendate derivatives and evaluation of anti-inflammatory activity by detecting the production of the Nitric Oxide (NO) in the lipopolysaccharide(LPS)-stimulated RAW 264.7 cell lines. Among the newly derivatives, compound 7k was the most potent one and two other compounds (7e and 7f) also exhibited greater anti-inflammatory activity than bifendate. Further in vivo studies confirmed that 7k significantly and dose-dependently inhibited carrageenan-induced paw edema and decreased the serum levels of alanine aminotransaminase, and aspartate aminotransaminase in concanavalin A-induced hepatitis model. Histopathological evaluation demonstrated that 7k has better hepatoprotective effect on acute liver injury induced by concanavalin A than bifendate, suggesting that 7k is a potential drug candidate for the treatment of hepatic injuries.     

La cafeína atenúa daño hepático y mejora signos neurológicos en un modelo de encefalopatía hepática con ratas

Introduction and aimsCirrhosis is the common outcome of liver diseases. It can be decompensated and lead to the development of complications, such as encephalopathy. Hyperammonemia that develops due to liver dysfunction is etiopathologically related to hepatic encephalopathy. Caffeine increases the activity of the urea cycle in the liver, augmenting ammonia degradation. By antagonizing adenosine receptors, it also has a hepatoprotective effect, impeding the formation of fibrosis, as well as having a stimulating effect on the central nervous system. The present study analyzed the effects of caffeine on the progression of cholestatic liver fibrosis and hepatic encephalopathy.Materials and methodsAn experimental model of cholestatic liver fibrosis, through common bile duct ligature, and of hepatic encephalopathy, through the administration of a high-protein diet, was constructed. Male Wistar rats (n = 32) were equally divided into 4 groups. The experiment lasted 28 days, with the administration of 50 mg/kg/day of caffeine. Laboratory tests, histologic analyses of the liver and encephalon, open field tests (OFTs), and daily behavioral analyses were carried out.ResultsThe ligated animals treated with caffeine had lower mean transaminase levels and improved histologic aspects of the liver and encephalon. The untreated ligated animals were clearly lethargic and apathetic at the last week of the experiment, confirmed by reduced exploratory activity during the OFT.ConclusionCaffeine improved the microarchitecture of the liver and encephalon of the cirrhotic animals and prevented the decrease in exploratory behavior of the animals during the OFT.     

2012~2014年武汉地区34家医院保肝药应用分析

摘 要 目的:对武汉地区2012~2014年保肝药物临床应用情况进行分析,为临床合理用药和科学管理提供参考。方法：采用世界卫生组织推荐的限定日剂量为指标的分析方法,对武汉地区2012~2014年34家样本医院保肝药总销售金额、用药频度（DDDs）、限定日费用（DDC）、排序比等进行回顾性统计分析。结果：武汉地区2012~2014年保肝药总体销售金额和用药频度逐年升高,排序前10 位的品种变化不大。每年均以异甘草酸镁销售金额最高,其次是鸟氨酸 门冬氨酸,核糖核酸,甘草甜素、半胱氨酸疏基丙氨酸复方制剂和多烯磷脂酰胆碱。2012～2013年用药频度居于前2位的是甘草甜素、半胱氨酸疏基丙氨酸复方制剂和水飞蓟素,2014年是促肝细胞生长素和苦参素。3年来,金额排名前30位的药品中,每年均有7个品种排序比小于0.5。结论：武汉地区保肝药的市场前景广阔,临床应用基本合理,但仍存在个别品种应用不合理的情况。     

Evaluation of hepatoprotective activity of Kyllinga nemoralis (Hutch & Dalz) rhizomes

Aim of study

In view of the use of rhizomes of Kyllinga nemoralis L., against hepatopathy in ethnomedicine the present study was aimed at evaluating the hepatoprotective activity of the rhizomes of Kyllinga nemoralis against carbon tetrachloride (CCl₄)-induced hepatotoxicity in rats.

Materials and methods

Hepatotoxicity was induced in male Wistar rats by carbon tetrachloride and olive oil (50%, v/v). i.p. ethanolic and petroleum ether extracts of Kyllinga nemoralis rhizomes were administered to the experimental rats (100 and 200 mg/kg, p.o. for seven days). The hepatoprotective effect of these extracts was evaluated by the assay of liver function biochemical parameters and histopathological studies of the liver compared with silymarin.

Results

Both extracts showed significant hepatoprotection when compared to control, similar to standard silymarin. Histology of liver sections also revealed that the extracts protected liver from injury.

Conclusions

The study identified a plant with potential hepatoprotective constituents which will be isolated and characterized in future.     

Phycocyanobilin accelerates liver regeneration and reduces mortality rate in carbon tetrachloride-induced liver injury mice

AIM: To investigate the hepatoprotective effects of phycocyanobilin(PCB) in reducing hepatic injury and accelerating hepatocyte proliferation following carbon tetrachloride(CCl4) treatment.METHODS: C57BL/6 mice were orally administered PCB 100 mg/kg for 4 d after CCl4 injection, and then the serum and liver tissue of the mice were collected at days 1, 2, 3, 5 and 7 after CCl4 treatment. A series of evaluations were performed to identify the curative effects on liver injury and recovery. Aspartate aminotransferase(AST), alanine aminotransferase(ALT), albumin and superoxide dismutase(SOD) were detected to indirectly assess the anti-inflammatory effects of PCB. Meanwhile, we detected the expressions of hepatocyte growth factor, transforming growth factor alpha(TGF-α), TGF-β, tumor necrosis factor-alpha(TNF-α) and interleukin-6(IL-6), the factors which are associated with inflammation and liver regeneration. The protein expressions of proliferating cell nuclear antigen(PCNA), TNF-α and cytochrome C were detected by western blot. Furthermore, the survivalrates were analyzed of mice which were administered a lethal dose of CCl4(2.6 mg/kg)with or without PCB.RESULTS:In our research,PCB showed a strongly anti-inflammatory effect on CCl4-induced liver injury in mice.The ALT was significantly decreased after CCl4 treatment from day 1(P0.01)and the AST was significantly decreased from day 2(P0.001).Both albumin and liver SOD were increased from day2(P0.001 and P0.01),but serum SOD levels did not show a significant increase(P0.05).PCB protected the structure of liver from the injury by CCl4.TUNEL assay showed that PCB dramatically reduced the number of apoptotic cells after CCl4 treatment compared to the control(101.0±25.4 vs 25.7±6.4,P0.01).The result of western blotting showed that PCB could increase PCNA expression,decrease TNF-αand cytochrome C expression.Furthermore,data shows that PCB could improve the survival rate of acute liver failure(ALF)mice which were injected with a lethal dose of CCl4(60.0%vs 20.0%).CONCLUSION:Our study indicated that PCB could be an ideal candidate for reversing acute liver injury or ALF.     

Hepatoprotective and antiviral properties of isochlorogenic acid A from Laggera alata against hepatitis B virus infection

Ethnopharmacological relevance

The aim of this study was to determine the anti-hepatitis B effect of isochlorogenic acid A isolated from Laggera alata (Asteraceae), a traditional Chinese herbal medicine.

Materials and methods

The anti-hepatitis B activity of isochlorogenic acid A was evaluated by the d-galactosamine (D-GalN)-induced HL-7702 hepatocyte damage model and the HBV-transfected HepG2.2.15 cells.

Results

Isochlorogenic acid A significantly improved HL-7702 hepatocyte viability and markedly inhibited the productions of HBsAg and HBeAg. The inhibitory rates of isochlorogenic acid A on the HBsAg and HBeAg expressions were 86.9% and 72.9%, respectively. In addition, isochlorogenic acid A declined markedly the content of hepatitis B virus covalently closed circular DNA (HBV cccDNA) and induced significantly the heme oxygenase-1 (HO-1) expression in HepG2.2.15 cells.

Conclusions

Isochlorogenic acid A was verified to possess the potent anti-hepatitis B activity. The anti-HBV target of isochlorogenic acid A is probably associated with blocking the translation step of the HBV replication. Overexpression of HO-1 may contribute to the anti-HBV activity of isochlorogenic acid A by reducing the stability of the HBV core protein and thus blocking the refill of nuclear HBV cccDNA. Additionally, the hepatoprotective effect of isochlorogenic acid A could be achieved by its antioxidative property and induction of HO-1.     

药食两用植物竹叶椒近五年药理活性研究进展

竹叶椒在我国是一种常见的花椒属药食两用植物,分布于我国大部分地区,结合近5年的文献资料,阐述竹叶椒药理活性研究成果,为深入研究该植物药理活性提供参考。