Mono-Feruloyl-R, R-(+)-Tartaric Acid from Salvia chinensis

报道了用半合成方法和光谱分析确证从华鼠尾草(Salvia chinensis Benth.)中分离的单阿魏酰-R,R-(+)-酒石酸的化学结构和绝对构型;合成了其 S,S-(-)-和 R,S-(meso)-酒石酸的衍生物,并分析了其间的光谱差异。

Inhibitory effect of schisandrin B on free fatty acid-induced steatosis in L-02 cells

AIM:To investigate the effects of schisandrin B (Sch B) on free fatty acid (FFA)-induced steatosis in L-02 cells.METHODS:Cellular steatosis was induced by incubating L-02 cells with a FFA mixture (oleate and palmitate at the ratio of 2:1) for 24 h.Cytotoxicity and apoptosis were evaluated by 3-(4,5-dmethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and Annexin V/propidium iodide staining,respectively.Cellular total lipid was determined using a photocolorimetric method after Nile red staining,and triglyceride content was measured using an enzymatic kit.To study the effects of Sch B on steatosis,L-02 cells were treated with Sch B (1-100 μmol/L) in the absence or presence of 1 mmol/L FFA for 24 h,and cellular total lipid and triglyceride levels were measured.To explore the mechanisms of action of Sch B in the steatotic L-02 cells,mRNA levels of several regulators of hepatic lipid metabolism including adipose differentiation related protein (ADRP),sterol regulatory element binding protein 1 (SREBP-1),peroxisome proliferator-activated receptor (PPAR)-α and PPAR-γ were measured by quantitative real-time polymerase chain reaction (PCR),and protein levels of ADRP and SREBP-1 were measured by immunoblotting.RESULTS:Treatment with 1 mmol/L FFA for 24 h induced intracellular lipid accumulation in L-02 cells comparable to that in human steatotic livers without causing apparent apoptosis and cytotoxicity.Sch B mitigated cellular total lipid and triglyceride accumulations in the steatotic L-02 cells in a dose-dependent manner.Quantitative real-time PCR and Western blot analyses revealed that treatment of L-02 cells with 100 μmol/L Sch B reverted the FFA-stimulated up-regulation of ADRP and SREBP-1.CONCLUSION:Sch B inhibits FFA-induced steatosis in L-02 cells by,at least in part,reversing the up-regulation of ADRP and SREBP-1.

Synthesis of d,l-α-Tocopherol Catalyzed by Heteropoly Acids

,d,l-a-Tocopherol (vitamin E) isfound to be synthesized by condensingtrimethylhydroquinone with isophytol catalyzed by heteropoly acids (HPA) H3:PW12O40 andH3PMo12O40 at room temperature. These HPA are efficient catalysts for the synthesis of d l-a-Tocopherol and can easily be separated from the reaction mixture and roused,

Microwave-assisted Polycondensation of L-2-Hydroxy-3-phenylpropanoic Acid

Amorphous poly (L-2-hydroxy-3-phenylpropanoic acid) (PLHPPA) was synthesized by the microwave-assisted polycondensation of L-2-hydroxy-3-phenylpropanoic acid (LHPPA). The weight average molar mass (Mw) of PLHPPA ranged from 3600 to 5300 and polydispersity index (Mw/Mn) from 1.0 to 1.4 when the reaction mixture was irradiated by microwave at 255, 340 and 510 w for 1 to 10 h, respectively.

Free fatty acids, glucose, and insulin in type 2 diabetes mellitus

Xu et al used the HOMA2 model to estimate theβ-cell function and insulin resistance levels in an individual from simultaneously measured fasting plasma glucose and fasting plasma insulin levels.This method is based on the assumption that the glucose-insulin axis is central for the metabolic activities,which led to type 2 diabetes.However,significant downregulation of both the NKX2-1 gene and the TPD52L3 gene force an increase in the release of free fatty acids(FFAs)into the blood circulation,which leads to a marked reduction in membrane flexibility.These data favor a FFA-glucose-insulin axis.The authors are invited to extend their study with the introduction of the saturation index(number of carbon-carbon double bonds per 100 fatty-acyl chains),as observed in erythrocytes.

Immobilization of Lactobacillus rhamnosus TISTR108 on Crude Pectin of Krung Kha Mao Leaves （Cissampe/os pareira L.） to Produce Lactic Acid in Longan Juice

L-（＋）-lactic acid production was studied by immobilized Lactobacillus rhamnosus T1STR108 on crude pectin from Krung Kha Mao Leaves. Central composite design was employed to determine the maximum lactic acid production of 42.88 g L-1 in predicted model with the factors at 4.11 g L1 of pectin, 6.05 mLLl inoculum and 1.09 mm of bead diameter. Statistical analyses demonstrated very high significance for the regression model, since the F-value computed 116.09 was much higher than the tabulated F-value 2.08 for the lactic acid production at 5% level for linear and quadratic polynomial regression models. The highest experimental lactic acid production was 43.57 g L^-1 at 96 h of fermentation, 1.58% higher than the predicted value.

Lactic Acid Production from Longan Juice （Euphora Iongana Lam.） by Crude Pectin of Immobilized Lactobacillus rhamnosus TISTRI08

L-（＋）-lactic acid production was studied by immobilized Lactobacillus rhamnosus TISTR108 on crude pectin from Krung Kha Mao （Cissampelospareira L.） leaves. Central composite design was employed to determine the maximum lactic acid production of 45.40 g/L in predicted model （Y = 43.98 - 2.43X1 ＋ 1.02X2 ＋ 2.96X3 - 8.72X1^2 - 3.99X2^2 - 1.74X3^2） with the factors at 5.9 of cultural medium pH, 37.6 ℃ of process temperature and 202 rpm of liquid agitation. Statistical analyses demonstrated very high significance for the regression model fitted the data adequately and explained the lactic acid production, since the F-value computed 54.89 was much higher than the tabulated F-value 2.08 for the lactic acid production at 5% level for linear and quadratic polynomial regression models. The highest experimental lactic acid production was 46.91 g/L at 72 h of fermentation.

Synthesis of the C5-C10 Segment of Taurospongin A

Stereoselective synthesis of C5-C10 segment 3 of taurospongin A (1) has been developed successfully from L-(-)-malic acid.

Drug discovery based on the structure of FKBP12: Design, synthesis and evaluation of L-1,4-thiazane-3-carboxylic acid derivatives as neuroimmunophilin ligands

By choosing neuroimmunophilin FKBP12 as a therapeutical target, we have attempted to discover a new structural drug for treating neurodegenerative disease. This drug should possess neurotrophic activity and not affect the immune system. Based on the crystal structure of FKBP12, FK506 and Calcineurin complex, a series of small organic molecules were designed. These molecules were to have the ability of binding to FKBP12 in a virtual screening. By using a solution parallel synthetic method, these compounds were synthesized. The neuroprotective and neuroregenerative activities of these compounds were evaluated by binding assays, PC12 cells survival and neurite outgrowth model, chick dorsal root ganglion cultures (DRG) and 6-OHDA lesioned mice sympathetic nerve endings model. The evaluation results of these compounds showed that compound N308 has great promise as a candidate for a neuroprotective and neuroregenerative agent.

Standard Enthalpies of Formation for Solid Complexes of Chromium Chloride with L-α-Amino Acids

The solid complexes of Cr(AA) 2Cl 3·nH 2O of CrCl 3 with L-α-amino acids (AA=Val, Leu, Thr, Met, Arg, Phe, Try and His) have been prepared in 95% EtOH medium, and characterized structurally by elemental analysis, chemical analysis, IR spectra and TG-DTG. The constant-volume combustion energies of the complexes have been determined by RBC-II type rotating-bomb calorimeter. The standard enthalpies of formation of the complexes have been calculated as well, which are ( -2543.16± 3.71) (Val), ( -2561.32± 4.06) (Leu), ( -2284.02± 2.95) (Thr), ( -1418.77± 4.60) (Met), ( -3218.91± 4.67) (Arg), ( -2643.90± 5.02) (Phe), ( -1707.18± 3.23) (Try) and ( -2838.05±3.45) (His) kJ/ mol, respectively.

Synthesis of the C_(11-16)+C_(27) Segment of Epothilone A

A chiral synthesis of the C11-16+C27 segment of epomilone A is described using inexpensive L-(-)-malic acid as staring materinal and using Sharpless asymmetric epoxidahon for introduction of the desired 12, 13 epoxide.

Women with Methylenetetrahydrofolate Reductase Gene Polymorphism and the Need for Proper Periconceptional Folate Supplementation

Maternal folate supplementation is critical for fetal development. Women with MTHFR （methylenetetrahydrofolate reductase） gene polymorphisms may not be getting the proper folate form to support fetal development. The objectives of this review were to： （1） undertake a comprehensive review on the association of MTHFR polymorphisms with the risk for various congenital diseases and other adverse pregnancy outcomes, （2） assess the efficacy and safety of current folic acid and other supplementations in women with the MTHFR polymorphism, and （3） provide guidance on the appropriate supplementation for women of childbearing potential with the MTHFR gene polymorphism in order to decrease these adverse pregnancy outcomes. Our assessments show that women with MTHFR gene polymorphism cannot efficiently convert folic acid to L-5-methyl-tetrahydofolate, the predominant active form of folic acid, due to reduced MTHFR enzymatic activity. L-5-methyl-tetrahydrofolate is currently commercially available under several brand names. Based on our comprehensive review and knowledge of the biochemistry of the folates, we recommend that L-5-methyltetrahydrofolate be given in combination with folic acid to women with MTHFR polymorphism that are pregnant or planning to become pregnant. Further study is needed to determine the optimal dose.

The Influence of Aziridine on the Aging of Composite Solid Rocket Propellant

Aging of a solid composite propellant containing HTPB/AP/AL was performed in order to validate the conformance of the accelerated aging data to the Arrhenius law. The main objective of the work was to examine the influence of the aziridine bonding agents family on the propellant aging. Aging of the prepared propellant samples was conducted as follows: 1. Four samples, one free of bonding agents, and three containing aziridine based bonding agents MAPO,HX-752, MAT4 were aged at 65°C. 2. Another four samples based on HX-752, MAT4 with different curing agents were aged at 65°C. The measured mechanical properties of the free bonding agent propellant samples were very far from the specifications and this illustrates the importance of the bonding agents in both the preparation and the aging phases.The prepared bonding agent 'MAT4' gave remarkable improvements of the mechanical properties comparing with HX-752 and MAPO. The aziridine bonding agents family inhibited the rate of decomposition of the propellant during the aging periods and supported the propellant matrix against decomposition at the elevate temperatures. Using of HMDI as curing agent gave slight better mechanical properties to the IPDI.

Synthesis of Novel Tartaric Acid-derived Chiral Phosphite Ligands and Their Application in the Cu-catalyzed Conjugate Addition of Diethylzinc to Cyclic Enones

Five novel tropos （3R,4R）- and/or （3S,4S）-N-benzyltartarimide-derived biphenylphosphite ligands were synthesized and applied in the Cu-catalyzed asymmetric conjugate addition of diethylzinc to cyclic enones with up to 75% e.e. Compared with the reported ligand 1-N-benzylpyrrolidine-3,4-bis[（R）-1,1＇-binaphthyl-2,2＇-diyl]phosphite- L-tartaric acid, the issue that L-（＋）-tartaric acid backbone and （R）-binaphthyl showed strong matched/mismatched character was solved with these tropos ligands. It was found that the enantioselectivity was mainly controlled by the absolute configuration of N-benzyltartarimide backbone, and both enantiomers of the addition products can be obtained by simply changing the configuration of N-benzyltartarimide substituent.

谷氨酸系列化合物专利

L-谷氨酸-5-甲酯的合成方法L-谷氨酸-5-甲酯（L—Glutamic acid 5-methyl ester）是合成多种氨基酸和氨基酸药物的重要原料。本发明以H2SO4为催化剂，在甲醇溶剂中对谷氨酸进行酯化，酯化反应结束后，用Ba（OH）2除去催化量的H2SO4，再回收甲醇，可获得含量98％以上的L-谷氨酸-5-甲酯产品。回收的95％甲醇溶剂可再用于酯化反应。本发明的合成工艺简单易行，