N-(对乙烯基)苯磺酰氨基酸的合成

以对乙烯基苯磺酸钠为原料，经酰卤化和酰氨化两步合成Ｎ－（对乙烯基）苯磺酰氨基酸，转化率达５０％以上．

安磺灵合成工艺研究

本文对新型除草剂安磺灵的合成工艺进行了研究。改进了中间体3,5-二硝基-4-二正丙胺基苯磺酰氯和最终产品安磺灵的合成方法,使之更适合于工业生产的要求。安磺灵的总收率在55%以上。

IMMOBILIZED ASPERGILLUS ORYZAE CELLS AND THEIR ACTIVITIES

Aminoacylase was immobilized on the mycelium cells of Aspergillus oryzae by using ethylenediamine, gelatin and glutylalhyde. The proper immobilized condition was studied by orthogonal experimental design. The immobilized cells with excellent activity and stability for optically resoluting N acetyl DL alanine were obtained. The effects of pH, temperature, ion concentration and substrate concentration on the reactive activity of immobilized cells were studied. The continuous optical resolution of N acetyl DL alanine was investigated respectively in an immobilized cells column (ICC) and in a novel couple immobilized cells bed & membrane reactor(CICBMR). The results indicate that the immobilized cells are suitable for industrial applications.

Photoelectrochemical degradation of acetaminophen and valacyclovir using nanoporous titanium dioxide

Electrochemically treated nanoporous TiO2 was employed as a novel electrode to assist in the pho- toelectrochemical degradation of acetaminophen and valacyclovir. The prepared electrode was characterized by scanning electron microscopy （SEM） and energy dispersive spectroscopy （EDS）. Cyclic voltammetry （CV）, Mott-Schottky plots, ultraviolet-visible light （UV-vis） absorbance spec- troscopy, and a total organic carbon （TOC） analyzer were employed to investigate the photoelec- trochemical degradation of acetaminophen and valacyclovir. The results indicated no obvious re- moval of acetaminophen and valacyclovir over 3 h when separate photochemical degradation and electrochemical oxidation were employed. In contrast, acetaminophen and valacyclovir were rapid- ly eliminated via photoelectrochemical degradation. In addition, electrochemically treated nanopo~ rous TiO2 electrodes significantly enhanced the efficacy of the photoelectrochemical degradation of acetaminophen and valacyclovir, by 86.96% and 53.12%, respectively, when compared with un- treated nanoporous TiO2 electrodes. This enhanced performance may have been attributed to the formation of Ti3~, Ti2~, and oxygen vacancies, as well as an improvement in conductivity during the electrochemical reduction process. The effect of temperature was further investigated, where the activation energy of the photoelectrochemical degradation of acetaminophen and valacyclovir was determined to be 9.62 and 18.42 kJ/mol, respectively.

N-acetylcysteine attenuates alcohol-induced oxidative stress in the rat

AIM: There is increasing evidence that alcohol-induced liverdamage may be associated with increased oxidative stress.We aimed to investigate free-radical scavenger effect of n-acetylcysteine in rats intragastrically fed with ethanol.METHODS: Twenty-four rats divided into three groups werefed with ethanol (6 g/kg/day, Group 1), ethanol and n-acetylcysteine (1 g/kg, Group 2), or isocaloric dextrose(control group, Group 3) for 4 weeks. Then animals weresacrificed under ether anesthesia, intracardiac blood andliver tissues were obtained. Measurements were performedboth in serum and in homogenized liver tissues.Malondialdehyde (MDA) level was measured by TBARSmethod. Glutathione peroxidase (GSH-Px) and superoxidedismutase (SOD) levels were studied by commercial kits.Kruskal-Wallis test was used for statistical analysis.RESULTS: ALT and AST in Group 1 (154 U/Land 302 U/L,respectively) were higher than those in Group 2 (94 U/L and155 U/L) and Group 3 (99 U/L and 168 U/L) (P＝0.001 forboth). Serum and tissue levels of MDA in Group 1 (1.84 nmol/mL and 96 nmol/100 mg-protein) were higher than Group 2(0.91 nmol/mL and 64 nmol/100 mg-protein) and Group 3(0.94 nmol/mL and 49 nmol/100 mg-protein) (P＜0.001 forboth). On the other hand, serum GSH-Px level in Group 1(8.21 U/g-Hb) was lower than Group 2 (16 U/g-Hb) andGroup 3 (16 U/g-Hb) (P＜0.001). Serum and liver tissue levelsof SOD in Group 1 (11 U/mL and 26 U/100 mg-protein)were lower than Group 2 (18 U/mL and 60 U/100 mg-protein)and Group 3 (20 U/mL and 60 U/100 mg-protein) (P＜0.001for both).CONCLUSION: This study demonstrated that ethanol-induced liver damage is associated with oxidative stress,and co-administration of n-acetylcysteine attenuates thisdamage effectively in rat model.

Intermediate formation enabled regioselective access to amide in the Pd-catalyzed reductive aminocarbonylation of olefin with nitroarene

An efficient route for the palladium-catalyzed reductive aminocarbonylation of olefins with nitroarenes was developed using carbon monoxide(CO)as both reductant and carbonyl source,which enables facile access to amides with excellent regioselectivity and broad substrate scope.It is found that the counter anions of the Pd catalyst precursors significantly affect the reaction chemoselectivity and amide regioselectivity.Branched amides were mainly obtained with K2PdCl4 as the metal catalyst,and phosphine ligands had no influence on the regioselectivity but affected the catalytic reactivity.However,phosphine ligands had significant effects on aminocarbonylation regioselectivity when Pd(CH3CN)4(OTf)2 was used;monodentate phosphines tended to form branched amides,and bidentate phosphines mainly formed linear amides.Trapping experiments,primary kinetic studies,and control reactions with all possible N-species reduced from nitroarene indicated that the catalytic synthesis of branched and linear amides produced nitrene(further converted to enamide)and aniline,respectively,different from the previous ligand-controlled regioselective synthesis of amides via the aminocarbonylation of olefins with amines.Furthermore,the proposed synthesis route could be applied in the synthesis of gram-scale propanil under mild conditions.

N-acetylcysteine attenuates oxidative stress and liver pathology in rats with non-alcoholic steatohepatitis

AIM: To evaluate attenuating properties of N-acetylcysteine (NAC) on oxidative stress and liver pathology in rats with non-alcoholic steatohepatitis (NASH). METHODS: Male Sprague-Dawley rats were randomly divided into three groups. Group 1 (control, n = 8) was free accessed to regular dry rat chow (RC) for 6 wk. Group 2 (NASH, n = 8) was fed with 100% fat diet for 6 wk. Group 3 (NASH + NAC20, n = 9) was fed with 100% fat diet plus 20 mg/kg per day of NAC orally for 6 wk. All rats were sacrificed to collect blood and liver samples at the end of the study. RESULTS: The levels of total glutathione (GSH) and hepatic malondialdehyde (MDA) were increased significantly in the NASH group as compared with the control group (GSH; 2066.7 ± 93.2 vs 1337.5 ± 31.5 μmol/L and MDA; 209.9± 43.9 vs 3.8 ±1.7 μmol/g protein, respectively, P < 0.05). Liver histopathology from group 2 showed moderate to severe macrovesicular steatosis, hepatocyte ballooning, and necroinflammation. NAC treatment improved the level of GSH (1394.8 ± 81.2 μmol/L, P < 0.05), it did not affect MDA (150.1 ± 27.0 μmol/g protein), but led to a decrease in fat deposition and necroinflammation. CONCLUSION: NAC treatment could attenuate oxidative stress and improve liver histology in rats with NASH.

Inflammatory cytokines suppress arylamine N-acetyltransferase 1 in cholangiocarcinoma cells

AIM： To evaluate the effect of inflammatory cytokines on arylamine N-acetyltransferase 1 （NAT1）, which is a phase-U enzyme involved in the biotransformation of aromatic and heterocyclic amines found in food, drugs and the environment. METHODS： Human cholangiocarcinoma KKU-100 cells were treated with a mixture of proinflammatory cytokines （interferon-7, interleukin-l and tumor necrosis factor-m） for 48 h, and the effect on NAT1 activity was assessed by high performance liquid chromatography, while NAT1 expression was determined by reverse-transcription polymerase chain reaction. The oxidative stress on the cells was examined by the formation of nitric oxide, superoxide anion and glutathione （GSH） levels. The cells were also treated with S-nitroso-glutathione （GSNO）, a nitric oxide donor, to see if the responses were similar to those obtained with the inflammatory cytokines. RESULTS： Cytokines suppressed NAT1 activity, reducing the Vmax without affecting the Am. Cytokines also had a significant impact on the induction of nitric oxide production and in reducing the redox ratios of glutathione （GSH） and GSH disulfide. Treatment with GSNO for 2-48 h reduced NAT1 activity without affecting the GSH ratio. Moreover, inflammatory cytokines and GSNO suppressed NAT1 mRNA expression. CONCLUSION： These findings indicate an association between inflammation and suppression of NAT1, which perhaps contributes to chemical-mediated toxicity and carcinogenesis,

Proline with or without Hydroxyproline Influences Collagen Concentration and Regulates Prolyl 4-Hydroxylase α(I) Gene Expression in Juvenile Turbot(Scophthalmus maximus L.)

This study was conducted to investigate the effect of dietary proline(Pro), and Pro and hydroxyproline(Hyp) in combination on the growth performance, total Hyp and collagen concentrations of tissues, and prolyl 4-hydroxylase α(I)(P4H α(I)) gene expression in juvenile turbot feeding high plant protein diets. A diet containing 50% crude protein and 12% crude lipid was formulated as the basal and control, on which other two protein and lipid contents identical experimental diets were formulated by supplementing the basal with either 0.75% Pro(Pro-0.75) or 0.75% Pro and 0.75% Hyp(Pro+Hyp). Four groups of fish in indoor seawater recirculating systems, 35 individuals each, were fed twice a day to apparent satiation for 10 weeks. The results showed that dietary Pro and Hyp supplementation had no significant effect on growth performance and feed utilization of juvenile turbot(P > 0.05). Total Hyp and collagen concentrations in muscle were significantly increased when dietary Pro and Hyp increased(P < 0.05), and fish fed diet Pro+Hyp showed significantly higher free Hyp content in plasma than those fed other diets(P < 0.05). The expression of P4 H α(I) gene in liver and muscle was significantly up regulated in fish fed diet Pro-0.75 in comparison with control(P < 0.05); however the gene was significantly down regulated in fish fed diet Pro+Hyp in muscle in comparison with fish fed diet Pro-0.75(P < 0.05). It can be concluded that supplement of crystal L-Pro and L-Hyp to high plant protein diets did not show positive effects on growth performance of juvenile turbot, but enhanced total collagen concentrations in muscle.

Immobilization of Aspergillus Oryzae Mycelium Pellets and Its Application in the Resolution of D, L-Alanine

Aspergillus oryzae 3042 mycelium pellets were immobilized by crosslinking method with reagents of gelatin and formaldehyde. An orthogonal design table was used to determine the optimal immobilization conditions. The L-aminoacylase activity of immobilized mycelium pellets under optimal conditions was assayed. The results show that the L-aminoacylase activity was 1350 U·g^-1 and the activity retention rate was 83%. The properties of the immobilized preparation were studied. Compared with free pellets, the appropriate pH of reaction system changed from 7.0 to 8.0, temperature changed from 52℃ to 63℃, and the ranges of the optimum reaction conditions were all improved. The effect of Co^2＋ on immobilized mycelium pellets was investigated and the favorable concentration was determined. When the immobilized preparation was used for the resolution of D, L-alanine in a packed bed reactor with 10 mm in diameter, 200 mm in height, the operational stability was increased, and the half-life period was 53 d. Thermal stability analysis shows that the immobilized pellets were more stable than the free pellets.

Mathematical Simulation of Blood Purification for Leukemia by Immobilized L-asparaginase

Plasma was purified in an immobilized L-asparaginase column. The predicted results are in good agreement with experimental data. It is indicated that the mathematical model is suitable for the mass transfer and reaction of blood purification.

N-acetylcysteine attenuates alcohol-induced oxidative stess in rats

AIM:To investigate free-radical scavenger effect of n- acetylcysteine in rats intragastrically fed with ethanol. METHODS:Twenty-four rats divided into three groups were fed with ethanol (6 g/kg/day,Group 1),ethanol and n- acetylcysteine (1 g/kg,Group 2),or isocaloric dextrose (control group,Group 3) for 4 weeks.Then animals were sacrificed under ether anesthesia,and intracardiac blood and liver tissues were obtained.Measurements were made in both serum and homogenized liver tissues. Malondialdehyde (MDA) level was measured by TBARS method.Glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) levels were studied by commercial kits. Kruskal-Wallis test was used for statistical analysis. RESULTS:ALT and AST in Group 1 (154 U/L and 302 U/L, respectively) were higher than those in Group 2 (94 U/L and 155 U/L) and Group 3 (99 U/L and 168 U/L) (P=0.001 for both).Serum and tissue levels of MDA in Group 1 (1.84 nmol/mL and 96 nmol/100 mg-protein) were higher than that in Group 2 (0.91 nmol/mL and 64 nmol/100 mg protein) and Group 3 (0.94 nmol/ml and 49 nmol/100 mg-protein) (P<0.001 for both).On the other hand,serum GSH-Px level in Group 1 (8.21 U/g Hb) was lower than that in Group 2 (16 U/g Hb) and Group 3 (16 U/g-Hb) (P<0.001).Serum and liver tissue levels of SOD in Group 1 (11 U/mL and 26 U/100 rag-protein) were lower than that in Group 2 (18 U/ mL and 60 U/100 mg protein) and Group 3 (20 U/mL and 60 U/100 rag-protein) (P<0.001 for both). CONCLUSION:Ethanol-induced liver damage was associated with oxidative stress,and co-administration of n-acetylolsteine attenuates this damage effectively in rat model.

Catalytic role of Cu(I) species in Cu_2O/CuI supported on MWCNTs in the oxidative amidation of aryl aldehydes with 2-aminopyridines

Cu2O and Cul were supported on multiwalled carbon nanotubes （MWCNTs） using a wet impregna- tion method, and the resulting materials were fully characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy with energy dispersive X-ray spectroscopy, transmission electron microscopy, and temperature-programmed desorption with ammonia analysis. The results of these experiments revealed that Cu2O and CuI were deposited on the MWCNTs in the cubic and γ phases, respectively. These results also showed that the Cu-containing MWCNTs exhibited weak to strong electron-accepting （Lewis acidic） properties. The catalytic activities of these materials were studied for the synthesis of biologically significant N-（pyridin-2-yl）benzamides via the oxidative amidation of aryl aldehydes with 2-aminopyridines. The yields of the products were in the range 50%-95% with 100% selectivity. Notably, the CuI/MWCNT catalyst was much more effective than the Cu2O/MWCNT catalyst with respect to the isolated yield of the product, although the latter of these two catalysts exhibited much better recyclability. A preferential interaction was observed between the polar nature of the acid-activated MWCNTs and the ionic Cu2O compared with covalent CuL The differences in these interactions had a significant impact on the rate of the nucleophilic attack of the amino group of 2-aminopyridine substrate on the carbonyl group of the aryl aldehyde.

THE RELATIONSHIP BETWEEN THE N-GLYCOSYLATION OF ACETYLGLUCOSAMINYLTRANSFERASE V AND ITS ACTIVITY

Objective. The goal of this paper is to investigate the relationship between the N-glycosylation of acetylglucosaminyltransferase V(Glc NAcT-V) and its activity and to know which site among the 6 N-glycosylation sites in the GlcNAcT-V gene is the most important. Methods.Wild type of GlcNAcTV was transfected into COS7 cells and its activity was measured 48 h later. The first site (Asn 110) was mutated with sitedirected mutagenesis and transfected into COS7 cells. Results. It was found that after the cells were added tunicamycin(TM, 1 μ g/ml), the activity was 117% of the wild type. The activity of the cells with mutating GlcNAcTV was about 120% of the wild type RTPCR showed that there was no significant change in mRNA expression among the three groups. Conclusion.The Nglycosylation is important for its activity. Our results suggest that the Nlinked carbohydrates on GlcNAcTV are required for the posttranscriptional activity of the enzyme.

Antifibrotic effect of N-acetyl-seryl-aspartyl-lysyl-proline on bile duct ligation induced liver fibrosis in rats

AIM:To investigate the preventive effect of N-acetyl-seryl-aspartyl-lysyl-proline (AcSDKP) on bile duct ligation (BDL)induced liver fibrosis in rats. METHODS:Liver fibrosis in rats was induced by BDL and AcSDKP was infused subcutaneously for 2 wkvia a osmotic minipump (Alzet 2ML4) immediately after BDL operation. After scarifying, serum and liver specimens were collected. Hematoxylin and eosin staining, Sirius red staining, enzyme linked immunosorbent assay, Western blot or real-time polymerase chain reaction were used to determinate liver functions, histological alterations, collagen deposition, mRNA expression of markers for fibroblasts, transforming growth factor-β1 (TGF-β1) and bone morphogenetic protein-7 (BMP-7). RESULTS:When compared to model rats, chronic exogenous AcSDKP infusion suppressed profibrogenicTGF-β1 signaling, α-smooth muscle actin positivity (α-SMA), fibroblast specific protein-1 (FSP-1) staining and collagen gene expression. Col Ⅰ, Col Ⅲ, matrix metalloproteinase-2, tissue inhibitors of metallopro-teinase-1 and tissue inhibitors of metalloproteinase-2 mRNA expressions were all significantly downregulated by AcSDKP infusion (2.02 ± 1.10vs 14.16 ± 6.50, 2.02 ± 0.45vs 10.00 ± 3.35, 2.91 ± 0.30vs 7.83 ± 1.10, 4.64 ± 1.25 vs 18.52 ± 7.61, 0.46 ± 0.16 vs 0.34 ± 0.12, respectively, P < 0.05). Chronic exogenous AcSDKP infusion attenuated BDL-induced liver injury, inflammation and fibrosis. BDL caused a remarkable increase in alanine transaminase, aspartate transaminase, total bilirubin, and prothrombin time, all of which were reduced by AcSDKP infusion. Mast cells, collagen accumulation, α-SMA, TGF-β1, FSP-1 and BMP-7 increased. The histological appearance of liver specimens was also improved. CONCLUSION:Infusion of exogenous AcSDKP attenu-ated BDL-induced fibrosis in the rat liver. Preservation of AcSDKP may be a useful therapeutic approach in the management of liver fibrosis.

PURIFICATION OF L-METHIONINE AND N-ACETYL-D-METHIONINE FROM THE MIXTURE OF ENZYMATICALLY DEACYLATED N-ACETYL-DL-METHIONINE

N-acetyl-D-methionine, NaAc and the remains of N-acetyl-L-methionine dramatically affect the purification of L-methionine when purified from the mixture of enzymatically deacylated N-acetyl-DL-methionine, leading to a low yield conventionally. Here, this paper reports a successful separation and purification of both L-methionine and N-acetyl-D-methionine by an H ion-exchange column. The pH, L-Met concentration and the ratio between the content of sodium cation and the ion-exchange capacity were optimized to obtain the maximum yield. Experimental results indicate that, under the optimized conditions, the yields of L-methionine and N-acetyl-D-methionine can reach as high as 85% and 75%, respectively.

Antioxidative and antiapoptotic effects of （＋）-clausenamide on acetaminophen-induced nephrotoxicity in mice

Objective： （＋）-Clausenamide （（＋）-CLA）, the active ingredient of wampee, was isolated from the leaves of Clausena lansium （Lour.） Skeels. This study aimed to evaluate the protective potential of （＋）-CLA against acetaminophen （APAP）-induced nephrotoxicity in mice. Methods： Mice were divided into control, APAP, high-dose （＋）-CLA, and low-dose （＋）-CLA groups. Then, mice were preadministered （＋）-CLA （50 and 100 mg/kg） for 5 consecutive days. After the last treatment, the animals received a single intraperitoneal injection of APAP （600 mg/kg）. Renal histopathology was evaluated by staining with hematoxylin and eosin. The levels of malondialdehyde （MDA） and glutathione （GSH） and the activities of catalase （CAT） and superoxide dismutase （SOD） were determined using corresponding kits. Western blotting was used to analyze the expression of apoptosis-related proteins in renal tissue. Results： Administration of APAP increased serum creatinine and blood urea nitrogen levels in comparison with the control group. An increase in renal MDA level, depletion of GSH, and reductions in CAT and SOD activities in renal tissue indicated that APAP-induced kidney injury was mediated by oxidative stress. The expressions of Bax and caspase-3, cleavage of caspase-3, and cytoplasm cytochrome c levels were up-regulated in renal tissue, whereas Bcl-2 expression and mitochondrial cytochrome c levels were down-regulated in the APAP group, which revealed that APAP-induced kidney injury significantly increased cell apoptosis in renal tubules. The histopathology of kidney tissue supported these biochemical mechanisms. （＋）-CLA can reverse changes in most of the abovementioned parameters and nearly restore the normal structure of the kidney. Conclusion： Oxidative stress and apoptosis are considered to be the mechanisms underlying APAP-induced nephrotoxicity. （＋）-CLA could be a promising antidote for APAP-induced acute renal damage owing to its antioxidative and antiapoptotic effects.

Product selectivity controlled by manganese oxide crystals in catalytic ammoxidation

The performances of heterogeneous catalysts can be effectively tuned by changing the catalyst structures.Here we report a controllable nitrile synthesis from alcohol ammoxidation,where the nitrile hydration side reaction could be efficiently prevented by changing the manganese oxide catalysts.α-Mn_(2)O_(3)based catalysts are highly selective for nitrile synthesis,but MnO_(2)-based catalysts includingα,β,γ,andδphases favour the amide production from tandem ammoxidation and hydration steps.Multiple structural,kinetic,and spectroscopic investigations reveal that water decomposition is hindered onα-Mn2O3,thus to switch off the nitrile hydration.In addition,the selectivity-control feature of manganese oxide catalysts is mainly related to their crystalline nature rather than oxide morphology,although the morphological issue is usually regarded as a crucial factor in many reactions.

Effect of Lianshu preparation on lipopolysaccharide-induced diarrhea in rats

AIM： To investigate the effect of Lianshu preparation on lipopolysaccharide （LPS）-induced diarrhea in rats. METHODS： A diarrhea model was established in Sprague Dawley rats via injection of 1 mL of 30 mg/kg LPS. A total of 40 rats were randomly divided into normal group, LPS group, LPS ＋ Lianshu group, LPS ＋ berberine group （n = 10 in each group）. Their intestinal mucosal barrier and frequency of diarrhea were observed. Levels of glucose, serum Na^＋, K^＋, Cl and hematocrit, plasma nitrogen monoxide （NO）, diamine oxidase （DAO）, and D （-）-lactate were measured. The number of IgA＋ plasma cells in small intestine was detected and SIgA levels in the intestinal fluid were measured. The antipyretic activity of Lianshu preparation in rats was evaluated using Brewer＇s yeast-induced pyrexia （10 mL/kg of 20% aqueous suspension）. Acetaminophen （250 mg/kg, intragastric administration, bid） was comparison. Temperature used as a standard drug for was recorded 1 h before and 6 h after Brewer＇s yeast injection. Finally, small intestina transmission in mice treated with Lianshu was detected after intraperitoneal injection of methyl prostigmin （2 mg/kg）. Atropine （10 g/kg） was used as a control. The ink content in intestine was determined and the total length of intestine was measured. RESULTS： The frequency of diarrhea was higher in LPS group than in LPS ＋ Lianshu group and LPS ＋ berberine group （36.70± 5.23 vs 28.50 ±4.06 and 32.70±9.30 respectively, P 〈 0.01）, and lower in LP5 ＋ Lianshu group than in LPS ＋ berberine group （P = 0.03）. The levels of Na＋, glucose, Cl, K^＋ were significantly lower in LPS ＋ Lianshu group than in LPS ＋ berberine group （140.35±3.19 mmol/L vs 131.99±4.86 mmol/L, 8.49 ±1.84 mmol/L vs 6.54±2.30 mmol/L, 106.29± 4.41 mmol/L vs 102.5±1.39 mmol/L, 5.08±0.66 mmol/L vs 4.32 ± 0.62 mmol/L respectively, P 〈 0.05）. The level of hematocrit was lower in LPS ＋ Lianshu group than in LPS ＋ berberine group （0.50% ±0.07% vs 0.59%± 0.10% respectively, P 〈 0.05）. The plasma levels of NO, DAO and D （-）-lactate were higher in LPS group than in normal group （79.74 ± 7.39μmol/L vs 24.94 ± 3.38μmol/L, 2.48 ±0.42μ/mL vs 0.82 ±0.33 p/mL, 5.63± 0.85μg/mL vs 2.01 ±0.32 μg/mL respectively, P 〈 0.01）, and lower in LPS ＋ Lianshu group than in LP5 ＋ berberine group （48.59±4.70μmol/L vs 51.56 ±8.38 μmol/L, 1.43± 0.53μmol/mL vs 1.81 ±0.42 μmol/mL, 4.00± 0.54 μg/mL vs 4.88 ± 0.77 pg/mL respectively, P 〈 0.05）. The morphology of the intestinal mucosa showed destroyed villi in LPS group and atrophied intestinal mucosa in other groups. The pathological intestinal mucosal changes were less in LPS ＋ Lianshu group than in LPS group. The number of IgA＋ plasma cells and amount of SIgA were higher in LPS ＋ Lianshu group than in LPS group （1.16±0.19/μm^2 vs 1.09±0.28/μm^2, P = 0.026; 0.59 ±0.12 mg/L vs 0.15± 0.19 mg/L respectively, P = 0.000）. Lianshu had counteractive effects on yeast-induced pyrexia and enterokinesia in rats. CONCLUSION： Lianshu preparation has therapeutic effects on LPS-induced diarrhea and enterokinesia in rats.

The Hepatoprotective Effects of Solanum Incanum on Acetaminophen-lnduced Hepatotoxicity in Guinea Pigs

Solanum incanum, a shrubby herb, is widely distributed and used as analgesic, antitoxic, and antispasmodic in folk medicine. In the present study, the protective effects of aqueous extract of S. incanum against acetaminophen induced acute liver damage were evaluated in guinea pigs. Animals were orally administered with S. incanum extract （50 and 100 mg/ kg bw） and silymarin （ 100 mg / kg bw） respectively for 6 days followed by acetaminophen administration （2 g / kg bw） at the 7th day. The results showed that the treatment with S. incanum extract significantly lowered the acetaminophen-induced serum levels of hepatic marker enzymes （AST, ALT, and ALP）, Liver histopathology also showed that S. incanum extract reduced the incidence of liver lesions including the swelling of hepatic cells, lymphocytes infiltration, nucleus condensation, and hepatic necrosis induced by acetaminophen treatment in guinea pigs. The S. incanum extract at a dose of 100 mg / kg bw was more effective in suppressing the oxidative damage than the extract at a dose of 50 mg / kg bw. Therefore, the results of this study suggest that S. incanum extract could protect liver against the acetaminophen-induced oxidative damage.