椭圆叶花锚的化学成分研究

目的:对龙胆科Gentianaceae花锚属植物椭圆叶花锚Halenia elliptica的干燥全草进行化学成分研究.方法:椭圆叶花锚的干燥全草用90%乙醇提取,依次用石油醚、乙酸乙酯、正丁醇萃取,对乙酸乙酯萃取部分采用各种柱色谱进行分离纯化,通过波谱数据分析(1H-NMR,13C-NMR,MS)进行结构鉴定.结果:从乙酸乙酯萃取部分分离鉴定了12个化合物,其中5个(口山)酮,1个裂环烯醚萜苷,以及6个其他类化合物.分别鉴定为8-羟基-2-甲基色原酮(8-hydroxy-2-methylchromone,1),5-羟基-2-甲基色原酮(5-methoxy-2-methylchromone,2),7-表断马钱子苷半缩醛内酯(7-epi-vogeloside,3),松柏醛(coniferl aldehyde,4),芥子醛(sinapaldehyde,5),norbellidifolin(6),1-羟基-2,3,4,6-四甲氧基(口山)酮(1-hydroxyl-2,3,4,6-tetramethoxyxanthone,7),1-羟基-2,3,4,7-四甲氧基(口山)酮(1-hydroxyl-2,3,4,7-tetramethoxyxanthone,8),1-羟基-2,3,5-三甲氧基(口山)酮(1-hydroxyl-2,3,5-trimethoxyxanthone,9),壬二酸(azelaic acid,10),β-谷甾醇(β-sitosterol,11),齐墩果酸(oleanolic acid,12).结论:其中化合物1,2为新的天然产物,化合物3～6,10为首次从椭圆叶花锚中分离得到,化合物6显示较好的抗HBsAg和HBeAg活性,其IC50分别为0.77 mmol·L-1和＜0.62 mmol·L-1.     

In vitro and in vivo hepatoprotective and antioxidant activity of ethanolic extract from Meconopsis integrifolia (Maxim.) Franch

Ethnopharmacological relevance

Meconopsis integrifolia (Maxim.) Franch is a high mountain endemic species used as a traditional Tibetan and Mongolian herb to treat hepatitis, pneumonia, and edema. This study aims to investigate the hepatoprotective and antioxidant effects of Meconopsis integrifolia ethanolic extract (MIE) in vitro and in vivo.

Materials and methods

The in vitro antioxidant property of MIE was investigated by employing various established systems. Rats with carbon tetrachloride (CCl₄)-induced liver injury were used to assess the hepatoprotective and antioxidant effect of MIE in vivo. The level or activity of alkaline phosphatase (ALP), glutamate pyruvate transaminase (ALT), aspartate aminotransferase (AST), and total bilirubin (TB) in the blood serum and thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) in the liver and kidney of the rats were assayed using standard procedures.

Results

MIE exhibited strong antioxidant ability in vitro. In the rats with CCl₄-induced liver injury, the groups treated with MIE and silymarin showed significantly lower levels of ALT, AST, ALP, and TB. MIE demonstrated good antioxidant activities in both the liver and kidney of the rats in vivo.

Conclusions

MIE exhibits excellent hepatoprotective effects and antioxidant activities in vitro and in vivo, supporting the traditional use of Meconopsis integrifolia in the treatment of hepatitis.     

Hepatoprotective and in vivo antioxidant effects of Byrsocarpus coccineus Schum. and Thonn. (Connaraceae)

Ethnopharmacological relevance

The leaf decoction of Byrsocarpus coccineus (Connaraceae) is drunk for the treatment of jaundice in West African traditional medicine.

Aim of the study

To investigate the hepatoprotective and in vivo antioxidant effects of Byrsocarpus coccineus in carbon tetrachloride (CCl₄)-induced hepatotoxicity in rats.

Materials and methods

Group allotment in this study included vehicle, CCl₄, Byrsocarpus coccineus 1000 mg/kg alone, Byrsocarpus coccineus 200, 400, and 1000 mg/kg + CCl₄ and Livolin^® 20 mg/kg + CCl₄, and treatment was carried out accordingly. On the 7th day, rats were sacrificed and blood was withdrawn by cardiac puncture. The levels and activities of serum biochemical parameters and antioxidant enzymes were then assayed using standard procedures.

Results

CCl₄ significantly (P < 0.05) increased the levels of ALT and AST and reduced total protein. In CCl₄ treated animals, Byrsocarpus coccineus (200, 400, and 1000 mg/kg) dose-dependently and significantly decreased ALT, AST and ALP levels with peak effect produced at the highest dose. Conversely, Byrsocarpus coccineus produced significant increases in albumin and total protein levels. The standard drug produced significant effects in respect of ALT (↓), albumin (↑), and total protein (↑). CCl₄ also produced significant (P < 0.05) reductions in the activity of catalase, SOD, peroxidase and GSH, and conversely increased MDA level. Byrsocarpus coccineus produced significant and dose-dependent reversal of CCl₄-diminished activity of the antioxidant enzymes and reduced CCl₄-elevated level of MDA. The standard drug also significantly increased CCl₄-diminished antioxidant enzymes activity and reduced CCl₄-elevated MDA level. In general, the effects of the standard drug were comparable and not significantly different from those of Byrsocarpus coccineus.

Conclusion

The results obtained in this study suggest that the aqueous leaf extract of Byrsocarpus coccineus possesses hepatoprotective and in vivo antioxidant effects. This finding justifies the use of this preparation in West African traditional medicine for the treatment of liver disease.     

In vitro and in vivo antioxidant effects of the ethanolic extract of Swertia chirayita

Ethnopharmacological relevance

Swertia chirayita, a medicinal herb endemic to the Tibetan region, is used as a special remedy for liver disorders. The hepatoprotective activity of its plant extracts has been associated with its antioxidant activity. This paper aims to investigate the in vitro and in vivo antioxidant effects of Swertia chirayita extracts (SCE).

Materials and methods

Antioxidant ability of Swertia chirayita was investigated by employing several established in vitro methods. In vivo antioxidant activity was tested against CCl₄-induced toxicity in mice. The levels and activities of malondialdehyde (MDA) and antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH), were then assayed using standard procedures.

Results

SCE exhibited strong antioxidant ability in vitro. The liver and kidney of CCl₄-intoxicated animals exhibited a significant (p < 0.001) decrease in SOD, CAT, and GSH levels. Additionally, these organs exhibited a significant (p < 0.001) increase in MDA level. CCl₄ did not exhibit toxicity on mice treated with SCE and Vitamin E. The effects of Swertia chirayita (three dosages) were comparable to those of Vitamin E, except in MDA level in the liver and GSH level in the kidney (p < 0.05).

Conclusion

This study suggests that the ethanolic extract of Swertia chirayita possesses in vitro and in vivo antioxidant effects. This supports the traditional use of Swertia chirayita in Tibetan medicine to cure liver diseases.     

In vitro and in vivo antioxidant activity of the ethanolic extract from Meconopsis quintuplinervia

Aims of the study

Meconopsis quintuplinervia, a medicinal herb endemic to the Tibetan region, is used to treat hepatitis. The aim of this study is to evaluate the antioxidant potential of the ethanolic extract of this herb using different assays.

Materials and methods

The antioxidant capacity of Meconopsis quintuplinervia was investigated using various established in vitro systems. An in vivo study of carbon tetrachloride (CCl₄)-induced antioxidant activity in mice was also conducted by examining the levels of malondialdehyde (MDA) and the activities of antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH).

Results

The extract showed strong in vitro antioxidant ability. In the in vivo study, CCl₄-induced oxidative stress caused significant decreases in the SOD, CAT, and GSH levels and a significant increase in the MDA level, most of which were significantly reversed (except for SOD in the liver.) by treatment with the extract and standard Vitamin E.

Conclusion

This study clearly indicates that the ethanolic extract of Meconopsis quintuplinervia is a valuable source of natural antioxidants. These findings provide scientific support for the traditional use of this herb as a Tibetan medicine for liver diseases.     

Hepatoprotective and antioxidant activity of Phaseolus trilobus,Ait on bile duct ligation induced liver fibrosis in rats

Ethnopharmacological relevance

Phaseolus trilobus Ait (Fabaceae) is extensively used by tribal people of Nandurbar district (Maharashtra, India) in the treatment of Jaundice and other liver disorders.

Aim

of the present study was to assess the medicinal claim of Phaseolus trilobus as hepatoprotective and antioxidant.

Material and methods

The hepatoprotective activity of methanol and aqueous extract of Phaseolus trilobus was evaluated by bile duct ligation induced liver fibrosis and antioxidant activity was evaluated using in vitro and in vivo antioxidant models viz anti-lipid peroxidation assay, super oxide radical scavenging assay and glutathione estimation in liver. Liver function tests were carried out to detect hepatoprotective activity, which was further supported by histopathological examination.

Results

Methanol and aqueous extracts of Phaseolus trilobus reduced elevated level of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), bilirubin and hydroxyproline significantly (p < 0.01) in bile duct ligated Wistar rats, proving hepatoprotective activity comparable with Silymarin. Both the extracts were found to reduce the elevated levels of serum thiobarbituric acid reactive substance (TBARS) and elevate superoxide scavenging radical activity proving antioxidant activity comparable with ascorbic acid. The reduced level of glutathione was found to be elevated in liver proving antioxidant activity comparable with Silymarin.

Conclusion

Phaseolus trilobus posses hepatoprotective property and is effective in oxidative stress induced cholestatic hepatic injury.     

Hepatoprotective and antioxidant effects of Cuscuta chinensis against acetaminophen-induced hepatotoxicity in rats

Tu-Si-Zi, the seeds of Cuscuta chinensis Lam. (Convolvulaceae), is a traditional Chinese medicine that is commonly used to nourish and improve the liver and kidney conditions in China and other Asian countries. As oxidative stress promotes the development of acetaminophen (APAP)-induced hepatotoxicity, the aim of the present study was to evaluate and compare the hepatoprotective effect and antioxidant activities of the aqueous and ethanolic extracts of C chinensis on APAP-induced hepatotoxicity in rats. The C chinensis ethanolic extract at an oral dose of both 125 and 250mg/kg showed a significant hepatoprotective effect relatively to the same extent (P<0.05) by reducing levels of glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT), and alkaline phosphatase (ALP). In addition, the same ethanolic extract prevented the hepatotoxicity induced by APAP-intoxicated treatment as observed when assessing the liver histopathology. Regarding the antioxidant activity, C chinensis ethanolic extract exhibited a significant effect (P<0.05) by increasing levels of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), and by reducing malondialdehyde (MDA) levels. In contrast, the same doses of the aqueous extract of C chinensis did not present any hepatoprotective effect as seen in the ethanolic extract, and resulted in further liver deterioration. In conclusion, these data suggest that the ethanolic extract of Cuscuta chinensis can prevent hepatic injuries from APAP-induced hepatotoxicity in rats and this is likely mediated through its antioxidant activities.     

Hepatoprotective effect of Hypericum japonicum extract and its fractions

OBJECTIVE: To investigate the hepatoprotective activity of different parts of Hypericum japonicum against carbon tetrachloride(CCl(4))-induced hepatitis and alpha-naphthyl-isothiocyanate (ANIT)-induced cholestasis. MATERIALS AND METHODS: Mice were divided into groups and then administrated orally with solutions extracted from herbs before they were modeled in the experiments. Levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin (T-BIL) in serum were evaluated. HPLC fingerprint was used for phytochemical analysis of the extracts. RESULTS: The total aqueous extract of Hypericum japonicum had an obvious effect on the decreasing of AST, ALT and T-BIL levels in serum. The isolated fraction IV (F4) exhibited a preferable activity of ameliorating cholestasis, while Fraction V (F5) was more efficacious in protecting liver from injury. Chemical fingerprint indicated that F5 contained several flavonoids which might be the active chemicals against hepatotoxicity. CONCLUSION: Different fractions of Hypericum japonicum manifest different effect, indicating their different potentials as candidacies of new drugs.     

Studies on the antioxidant and hepatoprotective activities of polysaccharides from Talinum triangulare

Ethnophamacological relevancy

The whole plant of Talinum triangulare (Family: Portulacaceae) is used in variety of diseases including hepatic ailments in Africa and Taiwan of China.

Aims of the study

The study was aimed to evaluate the antioxidant and hepatoprotective activity of polysaccharides from T. triangulare (TTP).

Materials and methods

The TTP was extracted using boiling water, and removed protein by Sevag method. 40%, 60% and 80% ethanol precipitating TTP (40%, 60%, 80% TTP) were gained by the successive addition of absolute ethanol. The antioxidant activities of 40%, 60%, 80% and crude TTP were evaluated using three different models in vitro, including reducing power, hydroxyl radicals, superoxide anion. To investigate the hepatoprotective potential, mice were treated with crude polysaccharides (50, 100 and 200 mg/kg, p.o.) for 7 days. Liver injures were induced by CCl₄ (0.1% in arachis oil, 10 mg/kg, i.v.) 1 h after the drug administration on day 7. Mice were sacrificed at 24 h after the CCl₄ injection. The levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT) in serum, and glutathione (GSH), superoxide dismutase (SOD), malondialdehyde (MDA) in liver tissues were measured. Histopathological examinations were carried out to supplement the biochemical results.

Results and conclusions

In vitro assays, TTP showed remarkably different degrees of antioxidant activities in dose-dependent manners. The crude TTP demonstrated a relatively strong antioxidant activity, while the 40% TTP showed the strongest antioxidant activity, and the 60% TTP had the weakest antioxidant ability. In vivo assay, pretreatment with TTP had significantly decreased the levels of AST, ALT and MDA against CCl₄ injures, and restored the activities of defense antioxidant substances SOD and GSH towards normalization. These results supported the effect of T. triangulare in fork use with scientific evidence.     

Antimicrobial activity of the methanolic extract and compounds from Morus mesozygia stem bark

Aim of the study

This study was aimed at investigating the antimicrobial activity of the methanolic extract (MMB) and compounds isolated from the stem bark of Morus mesozygia, namely 3β-acetoxyurs-12-en-11-one (1), moracin Q (2), moracin T (3), artocarpesin (4), cycloartocarpesin (5), moracin R (6), moracin U (8), moracin C (9), and moracin M (10).

Materials and Methods

The liquid microdilution assay was used in the determination of the minimal inhibitory concentration (MIC) and the minimal microbicidal concentration (MMC), against nine bacterial and two fungal species.

Results

The results of the MIC determination showed that the compounds 3, 4, 8 and 9 were able to prevent the growth of all tested microbial species. All other samples showed selective activities. Their inhibitory effects were noted on 90.9% studied organisms for the crude extract, 81.8% for compound 6, 72.7% for compound 10, 63.6% for compound 1, 54.5% for compound 5, and 45.5% for compound 2. The lowest MIC value of 39 μg/ml was obtained with the crude extract against Escherichia coli. The corresponding value for compounds (5 μg/ml) was registered with compound 9 on Shigella dysenteriae and compound 3 on E. coli, S. dysenteriae, Pseudomonas aeruginosa, Salmonella typhi and Bacillus cereus. The lowest MIC value (39 μg/ml) observed with the crude extract (on E. coli) was only eightfold greater than that of gentamycin used as reference antibiotic (RA) while the corresponding value (5 μg/ml) recorded with compounds 3 and 9 was equal to that of RA on the corresponding microorganisms.

Conclusions

The obtained results highlighted the interesting antimicrobial potency of M. mesozygia as well as that of the studied compounds, and provided scientific basis for the traditional use of this species.     

The hepatoprotective and antifibrotic effects of Saururus chinensis against carbon tetrachloride induced hepatic fibrosis in rats

Ethnopharmacological relevance

Saururus chinensis (Lour.) Baill (Saururaceae) has been used in Chinese folk medicine for treatment of various diseases, such as edema, jaundice, gonorrhea, antipyretic, diuretic, and antiinflammatory agents.

Aim of the study

Our aim was to evaluate the hepatoprotective and antifibrotic effects of Saururus chinensis extract (SC-E) in carbon tetrachloride (CCl₄) induced liver fibrosis rats.

Materials and methods

The SC-E (70 mg/kg) was administrated via gavage once a day starting from the onset of CCl₄ treatment (14 weeks) for subsequent 8 weeks. Evaluated with liver index, serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), hyaluronic acid (HA), hepatic malondialdehyde (MDA) content, and superoxide dismutase (SOD) activity, total cholesterol (TC), triglyceride (TG), total lipoprotein (TP), albumin (ALB), hydroxyproline (HYP), total antioxidant capacity (T-AOC), laminin (LN), type III collagen terminal peptide (PC-IIINP), and type IV collagen (IV-C), as well as with histopathologic changes of liver.

Results

SC-E effectively reduced the elevated levels of liver index, serum ALT, AST, HA, and hepatic MDA contents, enhance the reduced hepatic SOD activity in CCl₄-treated rats. The histopathological analysis suggested that SC-E obviously alleviated the degree of liver fibrosis induced by CCl₄.

Conclusions

Those results suggest SC-E has protective and therapeutic effects on liver fibrosis induced by CCl₄.     

Beneficial effects of Aesculus hippocastanum L. seed extract on the body's own antioxidant defense system on subacute administration

Aim of the study

Seeds of Aesculus hippocastanum L. have long been used in European phytotherapy to treat inflammatory and vascular problems. In Turkish folk medicine, tea prepared from the crushed seeds was used to pass kidney stone and against stomach ache, while a fraction of seed was swallowed to alleviate hemorroids symptoms.In order to evaluate the in vivo effects of escin mixture from Aesculus hippocastanum seed on the blood and tissue antioxidant defense systems in standard pellet diet (SPD) and in high-fat diet (HFD) consumed male mice.

Materials and methods

Escin mixture was obtained from the ethanol extract of seeds. Escin mixture was administered orally to male mice fed either standard pellet diet (SPD) or high-fat diet (HFD) at 100 mg/kg doses daily for 5 weeks and the tissue (liver, kidney and heart) and blood samples were collected at the end of experimental period. The effect of escin mixture on the plasma antioxidant activity; blood and tissue malondialdehyde (MDA) and reduced glutathione (GSH) levels; erythrocyte and tissue superoxide dismutase (SOD) and catalase activity (CAT) in SPD and HFD consumed animals were experimentally studied.

Results

Escin mixture prohibited the adverse effects of oxidative stress and showed a protective effect on the liver architecture both in SPD and HFD consumed male mice. Escin mixture prohibited the adverse effects of oxidative stress and showed a protective effect on the liver architecture both in SPD and HFD consumed male mice. Combined administration of high-fat diet with escin mixture decreased blood (p < 0.01), liver (p < 0.01), kidney (p < 0.05), and heart (p < 0.05) of MDA, liver SOD (p < 0.01) and CAT (p < 0.05) levels and increased blood (p < 0.01) and liver GSH (p < 0.001) levels in mice.

Conclusion

The present results indicate that Aesculus hippocastanum increase the antioxidative defense system of the body and prevent HFD-induced lipid peroxidation in male mice.     

Antihyperlipidemic effect of the methanolic extract from Lagenaria siceraria Stand. fruit in hyperlipidemic rats

Ethnopharmacological relevance

Lagenaria siceraria Stand. (Cucurbitaceae) fruits have been used, traditionally, in the treatment of hyperlipidemia and atherosclerotic impasse and considered as cardioprotective and cardiotonic drug.

Aim of the study

The present work was undertaken to investigate the effects of methanolic extract from Lagenaria siceraria in experimentally induced hyperlipidemia in rats.

Materials and methods

Methanolic extract of Lagenaria siceraria fruits (LSFE) (100, 200 and 300 mg/kg; p.o.) was administered to the high fat-diet-induced hyperlipidemic rats for 30 days to evaluate its antihyperlipidemic activity. Atorvastatin (10 mg/kg; p.o.) was used as a standard drug.

Results

At the 30th day, most significant reduction in lipid levels in the LSFE treated rats as compared to the rats fed with high-fat diet at the 0th day were: total cholesterol 290.14 ± 18.42 mg/dl vs. 228.58 ± 16.38 mg/dl, low-density lipoprotein cholesterol 195.14 ± 8.86 mg/dl vs. 120.57 ± 8.11 mg/dl, triglyceride 232.41 ± 15.22 mg/dl vs. 181.79 ± 15.68 mg/dl, very low-density lipoprotein cholesterol 46.48 ± 3.04 mg/dl vs. 36.35 ± 3.13 mg/dl (P < 0.0001). Conversely, high-density lipoprotein cholesterol levels were significantly (P < 0.0001) increased from 48.52 ± 6.52 to 71.66 ± 5.14 mg/dl. The increase in weight in rats administered with LSFE was less when compared to rats fed with high-fat diet. Moreover, LSFE also exhibited significant increase in excretion of bile acids.

Conclusion

The results demonstrate that the LSFE has a definite antihyperlipidemic potential. There is also a valid scientific basis for consuming it in the treatment of coronary artery diseases in India.     

Antidiabetic and antioxidant effects of Annona muricata (Annonaceae), aqueous extract on streptozotocin-induced diabetic rats

Ethnopharmacological relevance

The leaves of Annona muricata are used in Cameroon to manage diabetes and its complications. The aim of this study was to evaluate the antidiabetic, antioxidant activities and the potential toxicity of aqueous extract of Annona muricata in streptozotocin-induced diabetic rats.

Material and methods

Oral administration of Annona muricata aqueous extract (100 mg/kg or 200 mg/kg) was studied in normal and streptozotocin-induced diabetic rats. In long term treatment, 2 weeks after streptozotocin-induced diabetic rats, animals received plant extract during 28 consecutive days. For a protective effect, extract was administered 3 days prior to streptozotocin exposure and animals were observed 2 weeks without treatment.

Results

The plant extract was not effective in normal rats. In diabetic rats, single administration of the extract significantly reduced blood glucose levels by 75% and 58.22% respectively at the dose of 100 mg/kg and 200 mg/kg as compared to the initial value. Treatment of normal rats 3 days prior to diabetes induction showed that, Annona muricata extract has no effect within 72 h following STZ injection. However, after 14 days post-treatment, the extract at the dose of 100 mg/kg significantly reduced blood glucose levels as compared with initial value and diabetic control rats. Immunohistochemical staining of pancreatic β-cells of diabetic rats treated with the dose of 100 mg/kg expressed strong staining for β-cell compared to diabetic control. In a long-term study daily administration of Annona muricata aqueous extract for 28 days to diabetic rats, reduced blood glucose levels, serum creatinine, MDA, AST, ALT activity, and nitrite levels LDL-cholesterol. Total cholesterol, triglycerides, SOD, and CAT activity contents were restored.

Conclusion

These different results show that the antidiabetic activity of Annona muricata aqueous extract can be explained by its hypolipidaemic effect, its antioxidant and protective action on pancreatic β-cells, which in turn improve glucose metabolism.     

Antioxidant and hepatoprotective activity of ethanol extract of Arachniodes exilis (Hance) Ching

Aim of the study

The study was aimed to investigate the ethanol extract of Arachniodes exilis for the antioxidant and hepatoprotective activity.

Materials and methods

Antioxidant activity was evaluated by different assays, including reducing power, lipid peroxidation, 2, 2′-diphenyl-1-picrylhydrazyl (DPPH), 2, 2′-azinobis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), superoxide anion, hydroxyl radicals and hydrogen peroxide. The hepatoprotective activity of ethanol extract was studied on mice liver damage induced by CCL₄ by monitoring biochemical parameters.

Results

The extract showed potent activities on reducing power, lipid peroxide, DPPH, ABTS, superoxide anion, hydroxyl radical and hydrogen peroxide. And oral administration of Arachniodes exilis at different doses resulted in significant improvement on the levels of glutamate oxaloacetate transaminase, glutamate pyruvate transaminase, malondialchehyche and superoxidedismutase.

Conclusion

The results indicate that this plant possesses potential antioxidant and hepatoprotective properties and has therapeutic potential for the treatment of liver diseases.     

Hepatoprotective and antioxidant activity of Amaranthus spinosus against CCl4 induced toxicity

Aim

50% ethanolic extract (ASE) of Amaranthus spinosus (whole plant) was evaluated for in vitro antioxidant and hepatoprotective activity.

Methods

The total phenolics and reducing capacity of ASE was determined using standard curve of gallic acid (0–1.0 mg/ml) and butylated hydroxy anisole. In vitro antioxidant activity was determined by DPPH, superoxide, hydroxyl radicals, hydrogen peroxide and nitric oxide scavenging methods. The hepatoprotective activity of ASE was evaluated at 6, 7, 8, 9 and 10 μg/ml concentration against CCl₄ (1%) induced toxicity in freshly isolated rat hepatocytes and HepG2 cells.

Results

ASE was found to contain 336 ± 14.3 mg/g total polyphenolics expressed as gallic acid equivalent while the reducing capacity was 2.26 times of BHA. ASE showed significant antioxidant activity in DPPH assay (IC₅₀ 29 μg/ml), scavenges superoxide (IC₅₀ ∼ 66–70 μg/ml), hydrogen peroxide (IC₅₀ ∼120–125 μg/ml), hydroxyl radicals (IC₅₀ ∼140–145 μg/ml) and nitric oxide (IC₅₀ ∼ 135–140 μg/ml). ASE (6, 7, 8, 9 and 10 μg/ml) was able to normalise the levels of biochemical parameters in isolated rat hepatocytes intoxicated with CCl₄. A dose dependent increase in percentage viability was observed in CCl₄ intoxicated HepG2 cells.

Conclusions

ASE possesses significant hepatoprotective activity which might be due to antioxidant defence factors and phenolics might be the main constituents responsible for activity.     

Davilla elliptica and Davilla nitida: Gastroprotective,anti-inflammatory immunomodulatory and anti-Helicobacter pylori action

Ethnopharmacological relevance

Davilla elliptica and Davilla nitida are species commonly found in the Brazilian Cerrado biome.

Aim of the study

Based on ethnopharmacological and phytochemical analyses, methanolic extracts from leaves of Davilla elliptica (EDE) and Davilla nitida (EDN) were evaluated for their anti-ulcer, anti-inflammatory, immunological and anti-Helicobacter pylori activities.

Materials and methods

The gastroprotective action of both extracts was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated anti-inflammatory (carrageenin-induced rat hind paw edema), immunomodulatory (murine peritoneal macrophages) and antibacterial action of both extracts against a standard strain of Helicobacter pylori.

Results

EDE and EDN (500 mg/kg) were able to protect gastric mucosa against HCl/ethanol solution (EDE 63%; EDN 59%), absolute ethanol (EDE 95%; EDN 88%), and also against injurious effect of NSAID (EDE 77%; EDN 67%). When EDE and EDN were challenged with sulfhydryl depleter compound, the gastroprotective action of both extracts was completely abolished. EDE had gastroprotective effect related to increase of glutathione bioavailability and stimulated higher levels of NO, H₂O₂ and TNF-α production. Otherwise EDN showed better anti-Helicobacter pylori action than EDE. Neither extracts presented anti-inflammatory activity by oral route.

Conclusion

The phytochemical investigation showed that both extracts possess phenolic acid derivatives, acylglycoflavonoids and condensed tannins with evident quantitative variations that probably influenced the pharmacological differences between extracts.     

Antioxidant and hepatoprotective effect of swertiamarin from Enicostemma axillare against d-galactosamine induced acute liver damage in rats

Ethnopharmacological relevance

The whole plant of Enicostemma axillare Raynal (Family: Gentianaceae) is used in variety of diseases in traditional Indian system of medicine including hepatic ailments.

Aim of the study

Swertiamarin isolated from Enicostemma axillare Raynal was evaluated for antioxidant and hepatoprotective activity.

Materials and methods

Swertiamarin was isolated from successive ethyl acetate extract of the plant Enicostemma axillare belongs to the family Gentianaceae. The concentration of swertiamarin was determined by high performance thin layer chromatography (HPTLC). The hepatoprotective and antioxidant activity of swertiamarin (100 and 200 mg/kg body weight) was carried out against d-Galactosamine (d-GalN) (200 mg/kg body weight intraperitoneally i.p.) induced liver injury in rats.

Results

Swertiamarin a secoiridoid glycoside was found to contain a major constituent of the extract. d-GalN caused significant hepatotoxicity by alteration of several hepatic parameters. It also caused significant lipid peroxidation and reduced the levels of antioxidant defense mechanisms. The treatment with swertiamarin at 100 and 200 mg/kg body weight when administered orally for 8 days prior to d-GalN caused a significant restoration of all the altered biochemical parameters due to d-GalN towards the normal, indicating the potent antioxidant and hepatoprotective nature of swertiamarin.

Conclusions

Swertiamarin isolated from Enicostemma axillare possesses significant antioxidant and hepatoprotective properties against d-GalN induced hepatotoxicity given at 100 and 200 mg/kg body weight orally for 8 days, which might be due to its in vitro antioxidant activity.     

Orofacial antinociceptive effect and antioxidant properties of the hydroethanol extract of Hyptis fruticosa salmz ex Benth

Ethnopharmacological relevance

Hyptis fruticosa is a plant native to Brazil with antinociceptive and antiinflamatory properties. This study evaluated the antinociceptive activity of the hydroethanol extract of the plant leaves (CHEE) against orofacial pain as well as its in vitro effect against lipid peroxidation.

Materials and methods

The antinociceptive activity was investigated in mice orally treated with different doses of the CHEE (50, 100, and 200 mg/kg) and morphine (5 mg/kg) using formalin, glutamate, and capsaicin orofacial pain models using. Lipoperoxidation was induced in egg yolk by AAPH and FeSO₄ in the absence and presence of the CHEE (5, 50, 100, and 150 μg/mL).

Results

CHEE (200 mg/kg) significantly reduced (ρ<0.001) the pain response in the first (69.6%) and second (81.8%) phases of the formalin test, while the nociception caused by capsaicin was significantly (ρ<0.001) reduced by up to 62% at 200 mg/kg of extract. When glutamate was used as algogen, a significant (ρ<0.001) nociception reduction of up to 85% at 200 mg/kg extract was observed. CHEE showed a higher protection against lipoperoxidation caused by FeSO₄ (82.3% TBARS inhibition) than AAPH (35.7% TBARS inhibition) at 150 μg/mL.

Conclusion

Hyptis fruticosa leaf CHEE is of pharmacological interest because it was able to inhibit the peripheral and central transmission of orofacial pain, while reducing the spreading of the inflammatory processes by neutralizing reactive oxygen species, which are by-products in the biosynthesis of pain mediators.     

Hepatoprotective potential of Aloe barbadensis Mill. against carbon tetrachloride induced hepatotoxicity

Aloe barbadensis Mill. Syn. Aloe vera Tourn. ex Linn.(Liliaceae) has been used in variety of diseases in traditional Indian system of medicine in India and its use for hepatic ailments is also documented. In the present study an attempt has been made to validate its hepatoprotective activity. The shade dried aerial parts of Aloe barbadensis were extracted with petroleum ether (AB-1), chloroform (AB-2) and methanol (AB-3). The plant marc was extracted with distilled water (AB-4). All the extracts were evaluated for hepatoprotective activity on limited test models as hexobarbitone sleep time, zoxazolamine paralysis time and marker biochemical parameters. AB-1 and AB-2 were observed to be devoid of any hepatoprotective activity. Out of two active extracts (AB-3 and AB-4), the most active AB-4 was studied in detail. AB-4 showed significant hepatoprotective activity against CCl4 induced hepatotoxicity as evident by restoration of serum transaminases, alkaline phosphatase, bilirubin and triglycerides. Hepatoprotective potential was confirmed by the restoration of lipid peroxidation, glutathione, glucose-6-phosphatase and microsomal aniline hydroxylase and amidopyrine N-demethylase towards near normal. Histopathology of the liver tissue further supports the biochemical findings confirming the hepatoprotective potential of AB-4. The present study shows that the aqueous extract of Aloe barbadensis is significantly capable of restoring integrity of hepatocytes indicated by improvement in physiological parameters, excretory capacity (BSP retention) of hepatocytes and also by stimulation of bile flow secretion. AB-4 did not show any sign of toxicity up to oral dose of 2 g/kg in mice.