Antihepatotoxic activity of p-methoxy benzoic acid from Capparis spinosa.

p-Methoxy benzoic acid isolated from the methanolic soluble fraction of the aqueous extract of Capparis spinosa L. (Capparidaceae) was found to possess significant antihepatotoxic activity against carbontetrachloride and paracetamol induced hepatotoxicity in vivo and thioacetamide and galactosamine induced hepatotoxicity in isolated rat hepatocytes, using in vitro technique. The compound was characterized through physicochemical and spectral studies. Isolation, identification and antihepatotoxic activity of the compound is reported for the first time in the plant. HPTLC analysis of methanol soluble fraction indicated that the compound constitutes 33% w/w of the active fraction.     

Antihepatotoxic actions of Formosan plant drugs

One hundred twenty-nine samples of Formosan plants were screened for antihepatotoxic activity in primary cultured hepatocytes to reveal that 19 and 26 plants exhibited more than 50% inhibition against cytotoxicity produced by carbon tetrachloride and D-galactosamine, respectively. Plants which disclosed significant antihepatotoxic activity in both assay methods are: Wedelia chinense, Mallotus repandus, Phyllantus urinaria, Loranthus parasiticus, Ludwigia octovalvis, Onychium japonicum, Tamarix chinensis and Ampelopsis brevipedunculata.     

Preliminary studies on antihepatotoxic effect of Physalis peruviana Linn. (Solanaceae) against carbon tetrachloride induced acute liver injury in rats

Physalis peruviana is a medicinal herb used by Muthuvan tribes and Tamilian native who reside in the shola forest regions of Kerala, India against jaundice. It was evaluated for its antihepatotoxic, phytochemical analysis and the acute toxicity of the most promising extract in rats. Water, ethanol and hexane extracts of Physalis peruviana (500mg/kg body weight) showed antihepatotoxic activities against CCl(4) induced hepatotoxicity. The ethanol and hexane extracts showed moderate activity compared to water extract, which showed activity at a low dose of 125mg/kg. The results were judged from the serum marker enzymes. Histopathological changes induced by CCl(4) were also significantly reduced by the extract. Further, the extract administration to rats resulted in an increase in hepatic GSH and decrease in MDA. Preliminary phytochemical analysis revealed the presence of various components in the crude aqueous extract. The extract was found to be devoid of any conspicuous acute toxicity in rats.     

Antihepatotoxic actions of Cochlospermum tinctorium rhizomes

The antihepatotoxic activity of the rhizomes of Cochlospermum tinctorium was investigated using carbon tetrachloride- and galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Because the methanol and ethanol extracts of C. tinctorium rhizomes exhibited antihepatotoxic effects, the former was fractionated in order to elucidate the active constituents. Polyphenol compounds (gallic and ellagic acids) were detected in the active fractions and may account for much of the antihepatotoxic activity. Carotenoids could also be implicated in the activity of the total extracts.     

Antihepatotoxic activity of Swertia chirata on paracetamol and galactosamine induced hepatotoxicity in rats

The extracts of Swertia chirata were evaluated for antihepatotoxic activity using paracetamol and galactosamine models. The methanol extract of the whole plant was found active at a dose of 100 mg/kg i.p. On fractionating this extract into chloroform soluble and butanol soluble fractions, the activity was retained in the chloroform soluble fraction which was most active at a dose level of 25 mg/kg i.p. with overall protection of 81% and 78% against paracetamol and galactosamine, respectively. The butanol soluble fraction, rich in bitter secoiridoids, was devoid of significant activity. The protective effect observed against these two hepatotoxins which are different in their mechanisms of inducing hepatotoxicity, suggests broader and non-specific protection of the liver against these two toxins by non-bitter components of Swertia chirata.     

Further studies on the antihepatotoxic activity of Phyllanthus maderaspatensis Linn

Phyllanthus maderaspatensis (whole plant extracts) was evaluated for its antihepatotoxic and choleretic activities in rats. The plant extracts (200 mg/kg, n-hexane, ethyl alcohol or water) showed a remarkable hepatoprotective activity against acetaminophen-induced hepatotoxicity as judged from the serum marker enzymes. The water and ethyl alcohol extracts showed moderate activity compared to the n-hexane extract, which showed activity at a dose as low as 1.5 mg/kg. The antihepatotoxicity of the hexane extract was found to be better than silymarin, a standard hepatoprotective herbal drug. The effect of n-hexane extract was found to be concentration-dependent. This extract also exhibited choleretic activity in normal rats, and in vitro hydroxyl radical scavenging activity and inhibition of lipid peroxidation.     

Antihepatotoxic activity of Rosmarinus tomentosus in a model of acute hepatic damage induced by thioacetamide

R. tomentosus is a vegetal species closely related to the culinary rosemary (R. officinalis), a plant reported to contain antihepatotoxic agents. A dried ethanol extract of the aerial parts of Rosmarinus tomentosus (Lamiaceae) and its major fraction separated by column chromatography (fraction F19) were evaluated for antihepatotoxic activity in rats with acute liver damage induced by a single oral dose of thioacetamide. Silymarin was used as a reference antihepatotoxic substance. Pre-treatment with R. tomentosus ethanol extract, fraction F19 or silymarin significantly reduced the impact of thioacetamide toxicity on plasma protein and urea levels as well as on plasma aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase and gamma-glutamyl transpeptidase activities compared with thioacetamide-treated animals (group T). Pre-treatment with R. tomentosus ethanol extract significantly reduced the impact of thioacetamide damage on alkaline phosphatase and gamma-glutamyl transpeptidase activities compared with group T. Silymarin administration significantly reduced alkaline phosphatase and gamma-glutamyl transpeptidase activities compared with group T. Fraction F19 administration reduced only alkaline phosphatase activity compared with group T. According to these data, R. tomentosus extract shows promising antihepatotoxic activity, suggesting the need to isolate the chemical principles responsible for this activity and to study this activity in a model of thioacetamide-induced cirrhosis.     

Antioxidant and antihepatotoxic activities of Phellinus rimosus (Berk) Pilat

The antioxidant and antihepatotoxic activities of a wood inhabiting macrofungus, Phellinus rimosus were studied. The superoxide anion scavenging, Fe(2+)-ascorbate induced lipid peroxidation inhibiting, hydroxyl radical scavenging and nitric oxide scavenging activities of the ethyl acetate extract were determined. The results indicated that ethyl acetate extract of P. rimosus exhibited significant in vitro antioxidant activity. The ethyl acetate extract of P. rimosus also showed potent antihepatotoxic activity against carbontetrachloride-induced acute toxicity in rat liver. The amelioration of liver toxicity by the ethyl acetate extract was evident from its significant effect on the levels of serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and serum alkaline phosphatase (ALP). The results suggest that hepatoprotective effect of P. rimosus is possibly related to the free radical scavenging activity.     

Antihepatotoxic activity of Swertia chirata on carbon tetrachloride induced hepatotoxicity in rats

The methanol extract of Swertia chirata was evaluated for antihepatotoxic activity against carbon tetrachloride induced liver toxicity in experimental rats. The extract was found to be active and on fractionation into butanol soluble and chloroform soluble fractions, the activity was traced and found more profound in the chloroform soluble fraction. The butanol soluble bitter rich fraction showed marginal activity. The results based on biochemical estimations have been expressed statistically and are additionally supported by histopathological examination of the liver of experimental rats and pentobarbitone induced sleep time studies in mice.     

Hepatoprotective and antihyperliposis activities of in vitro cultured Anoectochilus formosanus

The pharmacological effects of an aqueous extract of the whole plants of in vitro cultured Anoectochilus formosanus were investigated experimentally for hepatoprotective and antihyperliposis activities. The extract showed significant antihepatotoxic activity against carbon tetrachloride induced cytotoxicity in primary cultured rat hepatocytes. In an assay for antihyperliposis using aurothioglucose-induced obese mice, the extract suppressed significantly the increase in the weights of body and liver, ameliorated triglyceride levels in the liver and serum, and also significantly reduced the deposition of adipose tissue.     

Assay method for antihepatotoxic activity using macrophage-mediated cytotoxicity in primary cultured hepatocytes

Conditions were examined to establish an in vitro assay method for antihepatotoxic activity using macrophage-mediated cytotoxicity in primary cultured mouse liver cells. Satisfactory assay procedure was achieved utilizing 3 h preincubated mouse hepatocytes and 18 h lipopolysaccharide-activated mouse peritoneal macrophages. Some natural products known to exert liver-protective effects in experimental liver damages were screened for antihepatotoxic activity by this assay method to reveal that cynarin, desoxypodophyllotoxin and silybin showed significant antihepatotoxic activity but at high concentrations cytotoxic effects were observed in desoxypodophyllotoxin and silybin. The utility of this assay method is discussed.     

Antihepatotoxic actions of gingerols and diarylheptanoids

The antihepatotoxic effects of gingerols, shogaols, diarylheptanoids and related analogues were assessed utilizing carbon tetrachloride- and galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Most congeners exhibited significant actions in these assay methods. The carbon tetrachloride assay appeared to be most useful in defining structure-activity relationships. The antihepatotoxic activity of gingerols and shogaols was dependent on the length of the side chain with the [7]- and [8]-companions eliciting the strongest activity. The gingerols exerted more intense activity than the corresponding shogaols. In the diarylheptanoids, introduction of hydroxyl groupings on the phenyl rings caused increased activity; however, the effect of the positions and number of hydroxyls on activity was variable depending on the carbon skeleton.     

Antihepatotoxic activity of bergenin, the major constituent of Mallotus japonicus, on carbon tetrachloride-intoxicated hepatocytes

To determine the antihepatotoxic activity of bergenin from Mallotus japonicus, carbon tetrachloride (CCl4)-induced cytotoxicity in primary cultured rat hepatocytes has been adopted as an assay system. Bergenin significantly reduced the activities of glutamic pyruvic transaminase and sorbitol dehydrogenase released from the CCl4-intoxicated hepatocytes. The antihepatotoxicity of bergenin was also evidenced by elevating the activities of glutathione S-transferase and glutathione reductase, and content of glutathione in the CCl4-intoxicated hepatocytes. From these results, it is assumed that bergenin exerted antihepatotoxicity against CCl4-induced cytotoxicity through glutathione-mediated detoxification as well as free radical suppressing activity.     

Antihepatotoxic activity of seeds of Cichorium intybus

The different fractions of alcoholic extract and one phenolic compound AB-IV of seeds of Cichorium intybus Linn were screened for antihepatotoxic activity on carbon tetrachloride (CCl(4))-induced liver damage in albino rats. The degree of protection was measured using biochemical parameters like aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALKP), and total protein (TP). The methanol fraction and compound AB-IV were found to possess a potent antihepatotoxic activity comparable to the standard drug Silymarin (Silybon-70). The histopathological study of the liver was also carried out, wherein the methanolic fraction and compound AB-IV showed almost complete normalization of the tissues as neither fatty accumulation nor necrosis was observed.     

Antioxidant and hepatoprotective effects of punicalagin and punicalin on acetaminophen-induced liver damage in rats

Punicalagin and punicalin were isolated from the leaves of Terminalia catappa L., a Combretaceous plant distributed throughout tropical and subtropical beaches, which is used for the treatment of dermatitis and hepatitis. Our previous studies showed that both of these compounds exert antioxidative activity. In this study, the antihepatotoxic activity of punicalagin and punicalin on acetaminophen-induced toxicity in the rat liver was evaluated. After evaluating the changes of several biochemical functions in serum, the levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were increased by acetaminophen administration and reduced by punicalagin and punicalin. Histological changes around the hepatic central vein and oxidative damage induced by acetaminophen were also recovered by both compounds. The data show that both punicalagin and punicalin exert antihepatotoxic activity, but treatment with larger doses enhanced liver damage. These results suggest that even if punicalagin and punicalin have antioxidant activity at small doses, treatment with larger doses will possibly induce some cell toxicities.     

Antihepatotoxic properties of picroliv: an active fraction from rhizomes of Picrorhiza kurrooa.

The hepatoprotective activity of picroliv, the irridoid glycoside mixture from Picrorhiza kurrooa, was determined in adult male albino rats. Pretreatment with picroliv prevented the hepatotoxic effects of paracetamol and galactosamine as evidenced by various biochemical and histopathological observations. Maximum hepatoprotective effect was observed with daily oral doses of 6 and 12 mg/kg for 7 or 8 days. The antihepatotoxic action of picroliv seems likely due to an alteration in the biotransformation of the toxic substances resulting in decreased formation of reactive metabolites.     

Evaluation of hepatoprotective effect of Pistacia lentiscus,Phillyrea latifolia and Nicotiana glauca

The hepatoprotective effect of the boiled and non-boiled aqueous extracts of Pistacia lentiscus, Phillyrea latifolia, and Nicotiana glauca, that are alleged to be effective in the treatment of jaundice in Jordanian folk medicine, was evaluated in vivo using carbon tetrachloride (CCl(4)) intoxicated rats as an experimental model. Plant extracts were administrated orally at a dose of 4 ml/kg body weight, containing various amounts of solid matter. Only total serum bilirubin level was reduced by treatment with non-boiled aqueous extract of N. glauca leaves, while the boiled and non-boiled aqueous extracts of the N. glauca flowers were non effective. Bilirubin level and the activity of alkaline phosphatase (ALP) were both reduced upon treatment with boiled aqueous extract of P. latifolia without reducing the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Aqueous extract of P. lentiscus (both boiled and non-boiled) showed marked antihepatotoxic activity against CCl(4) by reducing the activity of the three enzymes and the level of bilirubin. The effect of the non-boiled aqueous extract was more pronounced than that of the boiled extract.     

Radical scavenger and antihepatotoxic activity of Ganoderma formosanum,Ganoderma lucidum and Ganoderma neo-japonicum

The free radical scavenging and antihepatotoxic activity from Ganoderma lucidum, Ganoderma formosanum and Ganoderma neo-japonicum were studied. Treatment with the water extract of Ganoderma lucidum, Ganoderma formosanum and Ganoderma neo-japonicum caused a marked decrease in the CCl₄-induced toxicity in rat liver, made evident by their effect on the levels of glutamic oxaloacetic transaminase (GOT) and lactic dehydrogenase (LDH) in the serum. The scavenging potency of the water extracts of the crude drugs was evaluated in terms of their ability to reduce the peaks of spin adducts using electron spin resonance (ESR) spin-trapping techniques. The results indicated that Ganoderma formosanum showed the greatest antihepatotoxic activity and the greatest free radical scavenging activity.     

生、炒决明子及其煎剂中部分活性成分的比较

采用高效液相色谱法对生、炒决明子及其煎剂中游离大黄酚、结合大黄酚及保肝成分进行了比较。与生品比较，炒决明子游离大黄酸含量升高，结合大黄酸含量下降；而煎剂中结果则相反。炒决明子保肝类成分含量下降，但煎剂中含量反而略高。对上述实验结果进行了分析。本文为决明子炮制研究提供了方法和数据。