VE和L-肌肽对大菱鲆幼鱼生长、抗氧化、非特异性免疫及血清生化指标的影响

实验以大菱鲆（Scophthalmus maximus）幼鱼[（14.00±0.02）g]为研究对象，采用2×4双因素设计，设2个VE水平（0和75 mg/kg）和4个L-肌肽水平（0、50、100和200 mg/kg），研究VE和L-肌肽对其生长、抗氧化、非特异性免疫及血清生化指标的影响。实验共分8组，每组3个重复，每个重复46尾鱼，实验周期为8周。结果显示:（1）在饲料中添加75 mg/kg VE显著提高了大菱鲆幼鱼增重率（WGR）和特定生长率（SGR）（P < 0.05），L-肌肽添加量≤100 mg/kg对实验鱼生长性能无显著影响（P>0.05），添加量为200 mg/kg时鱼体WGR、SGR和蛋白质效率（PER）显著降低，饲料系数（FCR）显著升高（P < 0.05）；（2）VE和L-肌肽对血清谷胱甘肽过氧化物酶（GSH-PX）、过氧化氢酶（CAT）活性和丙二醛（MDA）含量及肝脏总抗氧化能力（T-AOC）、超氧化物歧化酶（SOD）活性和MDA含量均具有显著的交互作用（P < 0.05），在VE 75 mg/kg水平下，L-肌肽添加量为50和100 mg/kg时血清GSH-PX活性最高，L-肌肽添加量为100和200 mg/kg时血清CAT活性最高且与添加量为50 mg/kg差异不显著（P>0.05），添加100 mg/kg肝脏T-AOC和SOD活性达到最高且50 mg/kg组的SOD与100 mg/kg组差异不显著（P>0.05），主效应结果显示，VE显著提高了血清T-AOC、SOD及肝脏CAT活性（P < 0.05），L-肌肽显著提高了血清T-AOC（P < 0.05）；（3）VE和L-肌肽对血清补体C3和LZM活性交互作用显著，在75 mg/kg VE水平下，L-肌肽添加量为50 mg/kg时，补体C3水平最高（P < 0.05），主效应显示，VE和L-肌肽对血清总蛋白（TP）影响均不显著（P>0.05）；（4）添加VE显著降低了血清总胆固醇（TCHO）和甘油三酯（TG）含量（P < 0.05），添加L-肌肽显著降低了血清TG含量，且在L-肌肽50 mg/kg时达到最低。综合考虑大菱鲆幼鱼[（14.00-39.43）g]的生长性能、抗氧化性能、非特异性免疫及血清生化指标得出，在实验配方条件下（鱼油70 g/kg，大豆卵磷脂10 g/kg），添加VE 75 mg/kg时，L-肌肽的适宜添加量为50 mg/kg。     

Identification of phytochemical components from Aerva lanata (Linn.) medicinal plants and its in-vitro inhibitory activity against drug resistant microbial pathogens and antioxidant properties

This study aimed to determine the phytochemical components, microbial inhibitory effectiveness and antioxidant properties of Aerva lanata plant extracts. The whole plant showed various medicinal applications in folklore and traditional medicine in various parts of the world. The organic extracts such as ethanol, ethyl acetate, chloroform, acetone, water and methanol were subjected for various phytochemical analysis and confirmed for the existence of flavonoids, glycosides, terpenoids and alkaloid containing components. Alternatively, the extracts were performed for the antibacterial activities against the microbial pathogens and antioxidant properties. Results indicated that, the solvent extracts showed prominent activity against the tested strains. The MIC concentrations of plant were detected from 5 mg/ml to 40 mg/ml. The plant extract was highly effective against E. coli and E. aerogenes and the MIC was 5 mg/ml. In addition, the extracts noted promising antioxidant activities. The antioxidant activities were dose dependent manner. In conclusion, A. lanata extracts showed that significant major phytochemicals and effective antioxidant and anti-microbial properties.     

Synthesis,biological activities,and molecular docking studies of 2-mercaptobenzimidazole based derivatives

A new series of N-acylhydrazone derivatives of 2-mercaptobenzimidazole (2-MBI) has been synthesized through S-alkylation with 1-bromotetradecane and N-alkylation with ethyl-2-chloroacetate. The resulting ester was synthetically modified through hydrazine hydrate to acyl hydrazide which was condensed with aromatic aldehydes to afford the title N-acylhydrazones (4-17). Chemical structures of the newly synthesized compounds have been confirmed through mass, FT-IR and ¹HNMR techniques. In vitro free radical scavenging and α-glucosidase inhibition activities of the compounds were investigated with reference to the standard ascorbic acid and acarbose, respectively. Amongst the target compounds, 13 showed the highest inhibition in DPPH scavenging assay (IC₅₀ = 131.50 µM) and α-glucosidase inhibition potential (IC₅₀ = 352 µg/ml). We extended our investigations to explore the mechanism of enzyme inhibition and conducted docking analysis by using Molecular Operating Environment (MOE 2016.08). A homology model for α-glucosidase was constructed and validated using Ramachandran plot. Docking studies were also carried out on human intestinal α-glucosidases. In view of the importance of the nucleus involved, the synthesized compounds might find extensive medicinal applications as reported in the literature.     

Expression of manganese superoxide dismutase is not altered in transgenic mice with elevated level of copper-zinc superoxide dismutase

In evaluating the relative expression of copper-zinc and manganese superoxide dismutase (CuZnSOD and MnSOD) in vivo in states like Down syndrome in which one dismutase is present at increased levels, we measured activities of both enzymes, in tissues of control and transgenic mice constitutively expressing increased levels of CuZnSOD, during exposure to normal and elevated oxygen tensions. Using SOD gel electrophoresis assay, CuZnSOD and MnSOD activities of brain, lung, heart, kidney, and liver from mice exposed to either normal (21%) or elevated (>99% oxygen, 630 torr) oxygen tensions for 120 h were compared. Whereas CuZnSOD activity was elevated in tissues of transgenic relative to control mice under both normoxic or hyperoxic conditions, MnSOD activities in organs of transgenic mice were remarkably similar to those of controls under both conditions. To confirm the accuracy of this method in quantitating MnSOD relative to CuZnSOD expression, two other methods were utilized. In lung, which is the organ exposed to the highest oxygen tension during ambient hyperoxia, a sensitive, specific ELISA for MnSOD was used. Again, MnSOD protein was not different in transgenic relative to control mice during exposure to air or hyperoxia. In addition, lung MnSOD protein was not changed significantly by exposure to hyperoxia in either group. In kidney, a mitochondrion-rich organ, SOD assay, before and after inactivation of CuZnSOD with diethyldithiocarbamate, was used. MnSOD activity was not different in organs from air-exposed transgenic relative to control mice. The data indicated that expression of MnSOD in vivo was not affected by overexpression of the CuZnSOD and, therefore, the two enzymes are probably regulated independently.     

Multifunctional liposomes for nasal delivery of the anti-Alzheimer drug tacrine hydrochloride

The purpose of this study was the development of multifunctional liposomes for nasal administration of tacrine hydrochloride. Liposomes were prepared using traditional excipients (cholesterol and phosphatidylcholine), partly enriched with α-tocopherol and/or Omega3 fatty acids. This approach was chosen in order to obtain at the same time two positive results: an enhanced drug permeation through nasal mucosa and a concomitant neuroprotective effect. Several liposome formulations were prepared using the Reverse Phase Evaporation technique followed by membrane filter extrusion. In particular, liposome capacity to enhance drug permeation was evaluated by means of membrane permeation and cellular uptake studies. Furthermore, liposome effect on neuronal viability and intracellular ROS production was evaluated as well as their cytoprotective effect against oxidative stress. All liposome formulations showed a mean diameter in the range of 175?nm to 219?nm with polydispersity index lower than 0.22, a lightly negative zeta potential and excellent encapsulation efficiency. Moreover, along with good mucoadhesive properties, multifunctional liposomes showed a markedly increase in tacrine permeability, which can be related to liposome fusion with cellular membrane, a hypothesis, which was also supported by cellular uptake studies. Finally, the addition of α-tocopherol without Omega3 fatty acids, was found to increase the neuroprotective activity and antioxidant properties of liposomes.     

Synthesis and biological evaluation of 6-nitro-1,2,4-triazoloazines containing polyphenol fragments possessing antioxidant and antiviral activity

Stable σ-adducts of azolo[5,1-c]triazines and azolo[1,5-a]pyrimidines with different polyphenols were synthesized and their antioxidant and antiviral activity were investigated. Their affinity to viral hemagglutinin was assessed using molecular modelling. The phloroglucinol-modified azolo-azines possessed the highest virus-inhibiting activity. According to the results of the study of antioxidant properties of compounds, the most promising ones exhibiting highest antioxidant capacity were adducts containing in their structure pyrogallol and catechol residues and 6-nitro-triazolotriazin-7-ol scaffold. No correlation between antioxidant and virus-inhibiting activity of compounds studied was detected. The most active compounds demonstrated the ability to prevent binding of viral hemagglutinin with cellular receptor as shown in hemagglutination inhibition assay. Our results demonstrate that polyphenol-modified azolo-azines are prospective for further optimization as potential antivirals and that their action is directed against viral hemagglutinin.     

Effects of exogenous salicylic acid on manganese toxicity, element contents and antioxidative system in cucumber

The effects of salicylic acid (SA) on manganese (Mn) toxicity in cucumber plants (Cucumis sativus L.) were studied by investigating the symptoms, plant growth, lipid peroxidation, antioxidative enzymes and antioxidants. Excess Mn caused serious chlorosis and inhibited the growth of cucumber plants, and dramatically increased accumulation of Mn in both shoots and roots, furthermore, inhibited the absorption of Ca, Mg and Zn. Addition of SA decreased the transport of Mn from roots to shoots, alleviated the inhibition of Ca, Mg and Zn absorption induced by excess Mn, reduced the toxicity symptoms and promoted the plant growth. The accumulation of reactive oxygen species (ROS) significantly increased in cucumber leaves exposed to excess Mn, and resulted in the lipid peroxidation, which was indicated by accumulated concentration of thiobarbituric acid-reactive substances (TBARS). Addition of SA significantly decreased the level of ROS and lipid peroxidation. Activities of antioxidant enzymes showed different changes, addition of SA inhibited catalase (CAT) and ascorbate peroxidase (APX) activities, while increased activities of superoxide dismutase (SOD), peroxidase (POD), dehydroascorbate reductase (DHAR) and glutathione reductase (GR) in cucumber leaves exposed to excess Mn. As important antioxidants, ascorbate and glutathione contents in cucumber leaves exposed to excess Mn were significantly increased by SA treatment.     

The chemotaxonomic and medicinal significance of phenolic acids in Arctopus and Alepidea (Apiaceae subfamily Saniculoideae)

The occurrence of (R)-3′-O-β-d-glucopyranosylrosmarinic acid, rosmarinic acid and caffeic acid in two important South African medicinal plants is reported for the first time. (R)-3′-O-β-d-Glucopyranosylrosmarinic acid and rosmarinic acid were isolated and identified in several samples from three species of the genus Arctopus L. (sieketroos) and three species of the genus Alepidea F. Delaroche (ikhathazo), both recently shown to be members of the subfamily Saniculoideae of the family Apiaceae. The compounds occur in high concentrations (up to 15.3 mg of (R)-3′-O-β-d-glucopyranosylrosmarinic acid per g dry wt) in roots of Arctopus. Our results provide a rationale for the traditional uses of these plants, as the identified compounds are all known for their antioxidant activity, with rosmarinic acid further contributing to a wide range of biological activities. Furthermore, we confirm the idea that (R)-3′-O-β-d-glucopyranosylrosmarinic acid is a useful chemotaxonomic marker for the subfamily Saniculoideae.