Dietary phytosterols have been successfully used for lowering cholesterol levels, which correlates with the fact that some phytosterols are able to act as liver X receptor (LXR) agonists. Sargassum fusiforme is an edible marine seaweed well-known for its antiatherosclerotic function in traditional Chinese medicine. In this study, seven phytosterols including fucosterol (1), saringosterol (2), 24-hydroperoxy-24-vinyl-cholesterol (3), 29-hydroperoxy-stigmasta-5,24(28)-dien-3β-ol (4), 24-methylene-cholesterol (5), 24-keto-cholesterol (6), and 5α,8α-epidioxyergosta-6,22-dien-3β-ol (7) were purified and evaluated for their actions on LXR-mediated transcription using a reporter assay. Among these phytosterols, 2 was the most potent compound in stimulating the transcriptional activities of LXRα by (3.81±0.15)-fold and LXRβ by (14.40±1.10)-fold, respectively. Two epimers of 2, 24(S)-saringosterol (2a) and 24(R)-saringosterol (2b), were subsequently separated by semipreparative high-performance liquid chromatography. Interestingly, 2a was more potent than 2b in LXRβ-mediated transactivation ((3.50±0.17)-fold vs (1.63±0.12)-fold) compared with control. Consistently, 2a induced higher expression levels of LXR target genes including key players in reverse cholesterol transport in six cell lines. These data along with molecular modeling suggested that 2a acts as a selective LXRβ agonist and is a potent natural cholesterol-lowering agent. This study also demonstrated that phytosterols in S. fusiforme contributed to the well-known antiatherosclerotic function.

BackgroundA newly isolated L. acidophilus strain has been reported to have potential anti-inflammatory activities against lipopolysaccharide (LPS) challenge in piglet, while the details of the related inflammatory responses are limited. Here we aimed to analysis the ability of L. acidophilus to regulate inflammatory responses and to elucidate the mechanisms involved in its anti-inflammatory activity.ResultsThe ETEC (enterotoxigenic Escherichia coli) K88-induced up-regulations of IL-1β, IL-8 and TNF-α were obviously inhibited by L. acidophilus while IL-10 was significantly increased. Moreover, L. acidophilus down-regulated pattern recognition receptors TLR (Toll-like receptor) 2 and TLR4 expression in both spleen and mesenteric lymph nodes of ETEC-challenged piglets, in accompanied with the reduced phosphorylation levels of nuclear factor kappa B (NF-κB) p65 and mitogen-activated protein kinase (MAPK) p38 as well in spleen of ETEC-infected piglets. Furthermore, L.acidophilus significantly increased the expression of the negative regulators of TLRs signaling, including Tollip, IRAK-M, A20 and Bcl-3 in spleen of ETEC-challenged piglets.ConclusionsOur findings suggested that L. acidophilus regulated inflammatory response to ETEC via impairing both NF-κB and MAPK signaling pathways in piglets.

The Wittig reaction involving direct olefination of triphenylphosphonium ylides (Ph(3)P horizontal lineCHR) with aldehydes is arguably the most often used method for alkene synthesis, but in general it yields mixtures of Z- and E-alkenes for semistabilized triphenylphosphonium ylides (R = aryl or vinyl). We have developed a simple and efficient protocol to improve the stereoselectivity significantly by replacing the aldehydes used in the Wittig reaction with N-sulfonyl imines, which possess distinct electronic and steric properties relative to aldehydes. A broad range of aromatic, alpha,beta-unsaturated, and aliphatic imines bearing appropriate N-sulfonyl groups smoothly undergo olefination reaction with various benzylidenetriphenylphosphoranes or allylidenetriphenylphosphoranes under mild reaction conditions to afford an array of both Z- and E-isomers of conjugated alkenes in good to excellent yields and with greater than 99:1 stereoselectivity. Moreover, this tunable protocol has been successfully applied to the highly stereoselective synthesis of two anticancer agents, DMU-212 and its Z-isomer.

Aims & BackgroundsAlthough inflammatory bowel diseases (IBD) are emerging and increasing in China, epidemiologic data are rarely available. This study was to investigate the epidemiological and clinical characteristics of IBD in Northern China.MethodsThis is a prospective, population-based study of incidence of IBD in Daqing,Heilongjiang province of Northern China from March 1, 2012 to February 28, 2013. All incident patients with IBD were clinically identified by IBD specialist group from five main General Hospitals covering the healthcare service for 1,343,364 residents in the urban areas of Daqing. IBD cases included in this study were followed-up for three months for diagnosis confirmation.ResultsA total of 27 new IBD cases including 25 cases of ulcerative colitis (UC) and 2 cases of Crohn's disease (CD) were identified. The population at risk was 1,343,364 person years. Age-adjusted incidence for total IBD, CD and UC were 1.77, 0.13, and 1.64 per 100,000population, respectively. A male predominance was found in CD patients (male to female ratio was 2∶0). In contrast, no obvious gender predominance was found in UC patients (male to female ratio was 1∶1.1). CD patients were diagnosed at an average age of 39.5 years. The main disease phenotypes of UC were distal colitis with a 24% of proctitis and 56% of left-sided colitis. The mean diagnostic age of UC patients was 48.9 years.ConclusionsThis is the first report on the incidence of IBD in the Northern Chinese population. A lower incidence of IBD, similar male predominance for CD, similar disease phenotype of UC, and lower disease activity was observed in Daqing compared to that in Southern China.

The novelty of this study lies in the beneficial effects of C. butyricum on intestinal health, likely by improving intestinal barrier function and alleviating inflammatory reactions.

A series of new halo-substituted aroylhydrazones have been prepared and structurally characterized by elemental analysis, 1H NMR, 13C NMR, and IR spectra, and single crystal X-ray diffraction. The compounds were evaluated for their antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence) and antifungal (Candida albicans and Aspergillus niger) activities by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. Among the tested compounds, N′-(2-chloro-5-nitrobenzylidene)-2-fluorobenzohydrazide showed the most effective antimicrobial activity with minimum inhibitory concentration values of 0.82, 2.5, 1.7, 15.2, and 37.5 μg mL–1 against B. subtilis, S. aureus, E. coli, P. fluorescence, and C. albicans, respectively. The biological assay indicated that the presence of the electron-withdrawing groups in the aroylhydrazones improved their antimicrobial activities.

Formyl groups at 6-and 2,6-positions initiated Knoevenagel reactions of the methyl groups at the 7, and 1,7-positions of 1,3,5,7-tetramethyl BODIPY dyes with aromatic aldehydes. Formation of vinyl bonds at the 7-, and 1,7-positions facilitates further Knoevenagel reactions of the methyl groups at the 3,5positions. This approach offers fast, facile and versatile ways to prepare potential novel building blocks of BODIPY dyes for conjugated oligomers, dendrimers, and highly water-soluble, near-infrared emissive sensing materials.

This study was conducted with a lipopolysaccharide (LPS)-challenged piglet model to determine the effects of diets containing Lactobacillus acidophilus on the performance, intestinal barrier function, rectal microflora and serum immune function. A total of 150 piglets (initial body weight (BW) 7.53 ± 0.21 kg) were allotted to one of the following diets, including a basal diet, a basal diet supplemented with 250 mg/kg Flavomycin, or basal diet plus 0.05, 0.1 or 0.2 % L. acidophilus. On day 28 of the trial, the pigs were given an intraperitoneal injection of LPS (200 μg/kg body weight) followed by blood collection 3 h later. Diets with either antibiotics, 0.1 or 0.2 % Lactobacillus increased (P < 0.05) the final BW and decreased (P < 0.05) feed gain ratio (F/G) compared with the control group. Pigs fed diets containing antibiotic or Lactobacillus had greater average daily gain (ADG) (P < 0.05) than pigs fed the control diet. The rectal content Lactobacillus counts for pigs fed diet containing Lactobacillus were significant higher (P < 0.01) than those fed antibiotic or control diet. Feeding the Lactobacillus diets decreased the Escherichia coli counts of rectal content (P < 0.01). Pigs fed diets containing 0.1 or 0.2 % Lactobacillus decreased serum DAO activity (P < 0.05) compared with pigs fed the control diet. Serum IL-10 concentration was enhanced in pigs fed the diet with Lactobacillus compared to pigs fed the control diet and antibiotic diet. Feeding a diet with Lactobacillus reduced (P < 0.05) IFN-γ concentration compared to the control diet. Inclusion of Lactobacillus in diets fed to pigs reduced TNF-α concentration compared with pigs fed no Lactobacillus (P < 0.05). These results indicate that feeding with L. acidophilus improved growth performance and protected against LPS-induced inflammatory status.