Asymmetric α-Allylation of N-Unprotected Amino Acid Esters with 1,3-Disubstituted Allyl Acetates Enabled by Chiral-Aldehyde/Palladium Catalysis.

A chiral aldehyde/palladium catalysis-enabled asymmetric α-allylation of NH2-unprotected amino acid esters with 1,3-disubstituted allyl acetates is described in this work. With the utilization of different chiral phosphine ligands, both the anti- and syn-selective allylation reactions are achieved enantioselectively. A series of α,α-disubstituted amino acid esters bearing two adjacent chiral centers are produced in moderate-to-excellent yields, diastereoselectivities, and enantioselectivities.

A Seroepidemiological Survey of Toxoplasma gondii and Chlamydia Infection in Chickens, Ducks, and Geese in Jilin Province, Northeastern China.

Toxoplasma gondii and Chlamydia are common protozoan pathogens, which can pose health risks to people around the world and cause considerable economic losses. Although information on the seroprevalence of T. gondii and Chlamydia in chickens can be found in China, knowledge on the infection of these two diseases in rural chickens, ducks, and geese is limited. Therefore, blood samples from 377 chickens, 268 ducks, and 379 geese were taken from rural areas in seven cities in northeastern China, and their seropositivity was analyzed by the indirect hemagglutination antibody (IHA) test with a cutoff titer of 1:64. The overall seroprevalence of T. gondii and Chlamydia was 10.6% and 21.0%, respectively. Moreover, the free-range poultry (20.75% and 30.55%) have significantly higher seroprevalences than caged poultry (5.47% and 15.66%) (p < 0.001). Moreover, the seroprevalence of T. gondii in older and younger poultry was found to be 5.48% and 12.89%, and those in Chlamydia were 23.53% and 15.16%, respectively. There were significant differences between different ages (p < 0.05). But regarding the prevalence of both, it is not clear in this way which one is the prevalence for younger and older for each specific pathogen. Logistic regression analysis suggested that geography were considered as a risk factor for T. gondii infection in this study. Our study is the first report on the seroprevalence of T. gondii and Chlamydia in poultry in rural areas of Jilin Province, China. These data reflect that T. gondii and Chlamydia are widespread in poultry in northeastern China, leading to a risk of infection in human health. Therefore, the prevention and control of Toxoplasma and Chlamydia infection in poultry, other animals, and humans should be strengthened.

Stereoselective binding of doxazosin enantiomers to plasma proteins from rats, dogs and humans in vitro.

AIM: (±)Doxazosin is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms. In this study we investigated the stereoselective binding of doxazosin enantiomers to the plasma proteins of rats, dogs and humans in vitro. METHODS: Human, dog and rat plasma were prepared. Equilibrium dialysis was used to determine the plasma protein binding of each enantiomer in vitro. Chiral HPLC with fluorescence detection was used to measure the drug concentrations on each side of the dialysis membrane bag. RESULTS: Both the enantiomers were highly bound to the plasma proteins of rats, dogs and humans [(-)doxazosin: 89.4%-94.3%; (+)doxazosin: 90.9%-95.4%]. (+)Doxazosin exhibited significantly higher protein binding capacities than (-)doxazosin in all the three species, and the difference in the bound concentration (Cb) between the two enantiomers was enhanced as their concentrations were increased. Although the percentage of the plasma protein binding in the dog plasma was significantly lower than that in the human plasma at 400 and 800 ng/mL, the corrected percentage of plasma protein binding was dog>human>rat. CONCLUSION: (-)Doxazosin and (+)doxazosin show stereoselective plasma protein binding with a significant species difference among rats, dogs and humans.

Relationship between urinary nephrin and urinary albumin changes in diabetic rats and effects of yiqiyangyinhuayutongluo recipe.

OBJECTIVE: To investigate the dynamic changes of urinary nephrin, and the relationship between it and urinary albumin excretion rate (UAER) in a diabetic rat model, as well the effects of yiqiyangyinhuayutongluo recipe. METHODS: Diabetic model was induced by high fat diet combined with low-dose Streptozotocin (STZ) in rats. Normal group (NG), model group (MG), and yiqiyangyinhuayutongluo recipe treated group (YHTG) were set. Gastrointestinal Yiqiyangyi-nhuayutongluo recipe was administered once daily for 32 w. At the end of the 2nd w (2 w), 8 w, 16 w, and 32 w, fasting blood glucose (FBG), UAER and 24h urinary nephrin (U-nephrin) were detected. RESULTS: Compared with NG, FBG in MG increased notably (P < 0.05). Compared with MG, FBG of YHTG (P < 0.05) since 16 w. U-nephrin and UAER in MG increased significantly from 2 w, peaked at 16 w, lessened in different degree at 32 w, but were still higher than NG. The correlation analysis showed that there was a significant positive correlation between U-nephrin and UAER at different time, the correlation coefficient as r > 0.9, and P < 0.05. Compared with MG, U-nephrin and UAER in YHTG decreased markedly (P < 0.05) except for U-nephrin at 8 w. CONCLUSIONS: U-nephrin and UAER in diabetic rat model have a positive linear correlation. Yiqiyangyinhuayutongluo recipe can reduce UAER markedly, and preventing the lose of nephrin in urine maybe one of the mechanisms.

{Mu-N,N'-bis[2-(dimethylamino)ethyl]oxamidato(2-)-kappa(6)N,N',O':N'',N''',O}bis[(2,2'-bipyridine-kappa2N,N')copper(II)] bis(perchlorate).

In the crystal structure of the title complex, [Cu(2)(C(10)H(20)N(4)O(2))(C(10)H(8)N(2))(2)](ClO(4))(2), the deprotonated dmaeoxd(2-) ligand {H(2)dmaeoxd is N,N'-bis[2-(dimethylamino)ethyl]oxamide} occupies an inversion centre at the mid-point of the central C-C bond and is thus in a trans conformation. The two Cu(II) atoms are located in slightly distorted square-based pyramidal environments. The binuclear units interact with each other via pi-pi interactions to form a one-dimensional chain extending in the c direction.

[Effects of Zhikeping on aortic oxyradical and the expression of ICAM-1 in a rat model of experimental early atherosclerosis].

OBJECTIVE: To investigate the effects of Zhikepingon the oxyradical andintercellular adhesion molecule-1 (ICAM-1) of experimental early atherosclerosis. METHOD: The model of SD rat early atherosclerosis was induced by cholesterol diet. The suspension of Zhikeping and simvastatin were administered intragastrically, respectively. After 10 weeks, the serum lipids, superoxide dismutase (SOD) and maleic dialdehyde (MDA) were detected by automatic biochemistry analyzer. ICAM-1 and its expression of mRNA in aortic wall were detected- by immunohistochemistry and RT-PCR, respectively. Aortic histomorphology was cbserved by HE stainning. RESULT: The results showed that the serum lipids, superoxide dismutase (SOD) and maleic dialdehyde (MDA) of treated groups were obviously improved as compared with those of the control group. The tissue pathological damage was improved indifferent degree, and ICAM-1 and its expression of mRNA was decreased obviously. CONCLUSION: It is suggested the mechanism of anti-atherosclerosis of Zhikeping have close relationship with the function of its anti-oxidizing and anti-adhesiveness that can protect aortic endothelial cell.

[Protective effects of Chailing Guiqi Decoction combined with lumbrukinase on renal function in rats with adriamycin nephropathy].

OBJECTIVE: To study the protective efffects of Chailing Guiqi Decoction (CLGQD) combined with lumbrukinase on renal function in rats with adriamycin nephropathy. METHODS: Thirty-six SD rats were randomly divided into four groups: normal control group, untreated group, simvastatin-treated group and CLGQD -treated group. Adriamycin nephropathy was induced by intravenous injection with 5 mg/kg adriamycin. After seven-day treatment, quantitative measurement of 24-h urine protein was determined with trichloroacetic acid, and serum total protein (TP), albumin (Alb), total cholesterol (TC), triglycerides (TG), high-density lipoprotein (HDL), low-density lipoprotein (LDL), creatinine (Cr) and blood urea nitrogen (BUN) were assessed using automatic biochemistry analyzer. The pathomorphological changes of renal tissues were observed with light and electron microscopes. RESULTS: In the untreated group, the 24-h urine protein excretion, serum TC, TG, LDL, Cr and BUN were significantly higher than those in the normal control group (P<0.05 or P<0.01), while the serum TP, Alb, HDL were significantly lower than those in the normal control group (P<0.01). In the CLGQD-treated group, the 24-h urine protein excretion, serum TC, TG, LDL, Cr and BUN were significantly lower as compared with those in the untreated group (P<0.05 or P<0.01), while the serum TP, Alb and HDL were significantly higher as compared with those in the untreated group (P<0.05 or P<0.01). The pathomorphological findings of the renal tissues under the light microscope in the untreated group showed focal segmental glomerulosclerosis in a few of glomerulus, degenerated and swelled proximal tubular epithelial cells, proteins in cast formation in some renal tubules and scattered fibrosis in interstitial tissues of the kidney, while the electron microscope images showed the fusion of foot processes in glomerular epithelial cells. The pathomorphological changes in the CLGQD-treated group were slighter than those in the untreated group. CONCLUSION: CLGQD combined with lumbrukinase can reduce proteinuria, regulate lipid metabolism, protect renal function, and delay progressive renal damage in rats.

[Experimental study of the specific immunoresponse induced by p53 modified dendritic cells].

OBJECTIVE: To explore the specific cytotoxic T lymphocyte (CTL) induced by dendritic cells (DC), which were transfected by the plasmid pC53-SN3 encoding p53 gene. METHODS: DC derived from HLA-A2(+) mononuclear cells of the 24-lung cancer patients was transfected with the plasmid pC53-SN3 by lipofectamine and then co-cultured with auto-unpurified T cells to induce potent CTL (T-pC53-SN3). The cytolysis of specific CTL against Calu-6, a HLA-A2(+) human lung cancer cell line, was measured by using lactate dehydrogenase (LDH) releasing assay. RESULTS: The expression of CD(1a) and CD(83), the correlative markers of DC, increased apparently after transfected with plasmid pC53-SN3, the expression rate was (5.45 +/- 0.89)% and (3.26 +/- 0.47)% versus (52.15 +/- 11.56)% and (25.78 +/- 12.35)%. CD(14) decreased apparently, but other DC correlative markers of CD(1a), CD(40), CD(86), and HLA-DR remained almost the same as that before transfection. Compared with T-IL-2, the CTL derived from PBMNC stimulated by IL-2 (100 U/ml), the cytolytic activity of T-pC53-SN3 against Calu-6 cell line showed a significant increase, but cytolytic activity was 56.79 +/- 15.67 and 39.33 +/- 9.88, respectively, when effect cells: target cells was 10:1. The expression of the CD(8), CD(69), and CD(45)RO/CD(8) of T-pC53-SN3 cells increased significantly, but that of CD(3), CD(4), CD(86), ect, was not significantly different from those of T-pCMV-neo. CONCLUSIONS: It showed that DC transfected by p53 gene could induce potent HLA-A(2) restrictive CTL to kill tumor cell efficiently.