Three quinolizidine dimers from the seeds of Sophora alopecuroides and their hepatoprotective activities

Sophoralines A–C,three novel[2+2]cycloaddition dimers of matrine-based alkaloids with an unprecedented 6/6/6/6/4/6/6/6/6 nonacyclic skeleton containing 11 stereogenic centers,were isolated from Sophora alopecuroides.Their structures were determined by spectroscopic methods,and the absolute configurations were further determined by single-crystal X-ray diffraction analysis for 1 and quantum chemical calculations of electronic circular dichroism(ECD)spectra for 2 and 3.Moreover,1 exhibited excellent hepatoprotective activities in acetaminophen-induced liver injury in vitro and in vivo.

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(CCL_4 treated) group.Group 3 served as positive control(Silyntarin) group,and Group 4.S and ft served as(73,150 and 300 nig/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 COL_4 treated rats when compared with the control group(P<0.05).But the L.racemosa leaf extract treated rats showed maximum reduction of SGOT[(210.16±19.63)IU/L].SGPT[(82.37±13.87) IU/L].ALP[(197.63±23.4.3)IU/L],bilurubilt[(2.13 ±0.84) mg/dL].cholesterol[(163.83± 13.63) mg/dL].sugar[(93.00±7.63) 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/ kgbw) of leaf extract treated rats except few mild necrosis.The IC_(50) 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 SOL) 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.

Hepatoprotective activity of Sapindus mukorossi and Rheum emodi extracts: In vitro and in vivo studies

AIM: To study the hepatoprotective capacity of Sapindus mukorossi (S. mukorossi) and Rheum emodi (R. emodi) extracts in CCl4 treated male rats. METHODS: The dried powder of S. mukorossi and R. emodi was extracted successively with petroleum ether, benzene, chloroform, and ethanol and concentrated in vacuum. Primary rat hepatocyte monolayer cultures were used for in vitro studies. In vivo, the hepatoprotective capacity of the extract of the fruit pericarp of S. mukorossi and the rhizomes of R. emodi was analyzed in liver injured CCl4-treated male rats. RESULTS: In vitro: primary hepatocytes monolayer cultures were treated with CCl4 and extracts of S. mukorossi & R. emodi. A protective activity could be demonstrated in the CCl4 damaged primary monolayer culture. In vivo : extracts of the fruit pericarp of S. mukorossi (2.5 mg/mL) and rhizomes of R. emodi (3.0 mg/mL) were found to have protective properties in rats with CCl4 induced liver damage as judged from serum marker enzyme activities. CONCLUSION: The extracts of S. mukorossi and R. emodi do have a protective capacity both in vitro on primary hepatocytes cultures and in in vivo in a rat model of CCl4 mediated liver injury.

Hepatoprotective Activity of the Ethanol Extract of Sarcopyramis Nepalensis

The present study examined the protective effect of the ethanol extract of Sarcopyramis nepalensis (EESN) on agents-induced hepatotoxicity in mice and the possible mechanism. Acute liver injury was induced by administration of either CCl4 or D-GalN. The animals were divided into 5 groups in terms of different treatment: normal group, CCl4 or D-GalN group, silymarin or bifendate group, low dose EESN group (10 mg/kg) and high dose EESN group (30 mg/kg). Liver function was evaluated by detecting the levels of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST). The oxidize stress markers were measured, including malondialdehyde (MDA), glutathione peroxidase (GSH) and superoxide dismutase (SOD). Liver tissues were histopathologically examined by hematoxy-lin-eosin (H&E) staining. The acute toxicity study revealed that there was no toxicity of EESN at the dose of 5 g/kg in mice. The levels of ALT and AST in serum, and the MDA level in live tissues were significantly increased and the activities of SOD and GSH substantially decreased in mice after CCl4 or D-GalN treatment. These biochemical and oxidize stress markers were profoundly improved after treatment with EESN at different doses, which was similar to the results of silymarin or bifendate treatment. The histophathological examination revealed the significant improvement in the pathological changes of the liver in EESN-treated mice as compared to those in CCl4 or D-GalN group. It was concluded that EESN possesses potential antioxidant and hepatoprotective properties and has therapeutic potential for liver diseases.

Hepatoprotective and antioxidant capacity of Melochia corchorifolia extracts

Objective:To evaluate bepato protective and antioxidant capacity of Melochia corchorifolia （M.corchorifolia）aerial part extracts.Methods:Antioxidant activitywas evaluated by using three free radicals（Superoxide,Hydroxyl and DPPH） and hepatoprotective activity was assessed against CCl4 induced liver intoxication in ruts.Results:The extracts produced concentration dependent percentage protection in decrease of serum enzymes and percentage inhibition on free radicals.Among all extracts methanol extract showed better activity with percentage protection of SGOT（78.98%）,SGPT（79.65%）,ALP（82.48%） and total bilirubin（80.0%）levels against CCl4 liver intoxication and also methanolic extract showed better activity with IC50 values on superoxide. hydroxyl and DPPH radicals were 127μg.240μg and 179μg.Conclusions:From the results obtained during the study it could be concluded that M.corchorifolia aerial part extracts have antioxidant and hepaloprotective components.Further study is necessary for isolation and characterization of bioactive molecules which are responsible for hepatoprotective and antioxidant activity.

Evaluation of the hepatoprotective and antioxidant activities of Rubus parvifolius L.

The hepatoprotective and antioxidant activities of the n-butanol extract of Rubus parvifolius L. （RPL）, a widely used medicinal plant, were evaluated. Results demonstrated that RPL extract possessed pronounced hepatoprotective effects against carbon tetrachloride （CCI4）-induced hepatic injury in mice, which was at least partially attributed to its strong antioxidant capacity. Treatment with RPL extract markedly attenuated the increases in serum alanine ami- notransferase （ALT） and aspartate aminotransferase （AST） levels caused by CCI4 intoxication. It also significantly prevented the decrease in superoxide dismutase （SOD） activity and the increase in malondialdehyde （MDA） content of liver tissue. Meanwhile, histopathological changes of hepatic damage were also remarkably ameliorated. Phytochemical analysis based on high-performance liquid chromatography/tandem mass spectrometry （HPLC-MS/MS） revealed the presence of various phenolic compounds, including caffeic acid conjugates, ellagic acid glycosides, and flavonol glycosides, which might be responsible for the hepatoprotective and antioxidant activities of RPL.

New triterpenoid saponins from the leaves of Ilex chinensis and their hepatoprotective activity

Seven new triterpenoid saponins,including five ursane-type saponins,ilexchinenosides R–V(1–5),and two oleananetype saponins,ilexchinenosides W–X(6–7),with four known triterpenoid saponins(8–11)were isolated from the leaves of Ilex chinensis.Their structures were elucidated by comprehensive spectroscopic 1 D and 2 D NMR and HR-ESI-MS data.Their sugar moieties were determined by HPLC analysis compared with standards after hydrolysis and derivatization.Compounds 1,2,4,9 and 10 exhibited potential hepatoprotective activity against N-acetyl-p-aminophenol(APAP)-induced Hep G2 cell injury in vitro.

Protection of Citrullus colocynthis Fruit Extracts on Carbon Tetrachloride-induced and Bacillus Calmette-Guerin plus Lipopolysaccharide-induced Hepatotoxicity in Mice

Objective To investigate the hepatoprotective activities of the extracts from Citrullus colocynthis(ECC),a native plant used as traditional Uigur Medicine on acute liver injury in mice.Methods The activities of ECC of petroleum ether(ECCPE),chloroform(ECCC),ethyl acetate(ECCEA),n-butyl alcohol(ECCBA),and water(ECCW) were evaluated in vivo using two experimental models,carbon tetrachloride(CCl4)- and bacillus calmette-guerin(BCG) plus lipopolysaccharide(LPS)-induced acute hepatotoxicity in mice.The contents of aspartate aminotransferase(AST) and alanine aminotransferase(ALT) in serum were determined and the liver histological examination was carried out,respectively.Results The pretreatment with ECC for 7 d obviously reduced the impact of CCl4toxicity on the serum markers of liver damage,ECCEA and ECCC with a significant difference of AST(P < 0.01,0.05,respectively) and ALT(P < 0.05,0.01,respectively).The protective activity was reconfirmed against BCG + LPS-induced injury and the serum enzymatic levels were obviously elevated,for ECCEA and ECCC with a significant difference of AST(P < 0.05,0.01,respectively) and ALT(P < 0.01,0.05,respectively).Conclusion That ECCEA and ECCC are the potent hepatoprotective extracts that could protect liver against the acute injury,and this ability might be attributed to their hepatoprotective potentials.

New phenolic constituents obtained from Polygonum multiflorum

Objective:To isolate the phenolic compounds obtained from the dried roots ofPolygonum multiflorum and investigate their pharmacological activities.Methods:The chemical constituents were isolated and purified by combining them with a macroporous resin(DM-8),MCI gel,and Sephadex LH-20 and by performing ODS column chromatography.Their structures were elucidated by 1D and 2D NMR analyses,as well as mass spectrometry.The isolated compounds were evaluated to determine their hepatoprotective andα-glucosidase inhibitory activities in vitro.Results:Two phenolic compounds,namely,polygonimitin E(1)and polygonimitin F(2),were isolated from the dried roots of P.multiflorum.Compound 2(10μmol/L)only showed moderate hepatoprotective activity against N-acetyl-p-aminophenol(APAP)-induced HepG2 cell damage.Unfortunately,these two compounds exhibited noα-glucosidase inhibitory activity.Conclusion:Compounds 1 and 2 were new compounds.Compound 2 could be one of the potential hepatoprotective constituents of P.multiflorum.

Two new phenylpropanoid glycosides from the aerial parts of Lespedeza cuneata

Two new phenylpropanoid glycosides named cuneataside E (1) and cuneataside F (2), were isolated from the aerial parts of Lespedeza cuneata (Dum. Cours.) G. Don, whose structures were E and Z isomer, respectively. Their structures were elucidated on the basis of comprehensive spectroscopic analysis (UV, IR, HR-ESI-MS, 1D and 2D NMR). In in vitro bioassays at 10 mu mol/L, compound 1 showed moderate hepatoprotective activity against N-acetyl-p-aminophenol (APAP)-induced toxicity in HeG2 cells. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND

Novel liver-specific nitric oxide(NO) releasing drugs with bile acid as both NO carrier and targeting ligand

Novel liver-specific nitric oxide（NO） releasing drugs with bile acid as both the NO carrier and targeting ligand were designed and synthesized by direct nitration of the hydroxyl group in bile acids or the 3-Ohydroxyl alkyl derivatives,with the intact 24-COOH being preserved for hepatocyte specific recognition.Preliminary biological evaluation revealed that oral administrated targeted conjugates could protect mice against acute liver damage induced by acetaminophen or carbon tetrachloride.The nitrate level in the liver significantly increased after oral administration of 1e while nitrate level in the blood did not significantly change.Co-administration of ursodeoxycholic acid（UDCA） significantly antagonized the increase of nitrate in the liver resulted by administration of 1e.