Efficient One-Pot Synthesis of Benzimidazoles Under Solvent-Free Conditions

A green, efficient method for the synthesis of various 2-aryl-benzimidazoles in the presence of hypervalent iodine as the oxidant at room temperature under solvent-free conditions is reported. The salient features of this method include mild conditions, short reaction times (3–5 min), excellent yields, and simple procedure.     

某鸡场鸡传染性法氏囊病弱毒疫苗饮水免疫后发生的一次鸡病的诊断

１９９１年４月上旬，四川某鸡场对３５７０只１３日龄依莎雏鸡作法氏囊病弱毒疫苗饮水免疫，１４日龄时发病死亡９只，到２３日龄９天内共死亡８１４只，病死率达２２．８％。对２０只送检病死鸡的沙门氏菌分离率为１／２０株（５％）．但病料人工感染小白鼠试验为阴性，证明非病原菌所致，用病料与新城疫血清（抑制价１：６４０）作用后接种非免疫健康鸡１组的存活率为７５％，直接接种未与新城疫血清作用病料的２组存活率为５０％，剖检回归本动物试验自然死亡和人为处死的病鸡发现了较为典型的法氏囊病变，由此认为：法氏囊弱毒疫苗饮水免疫是引起鸡群发病死亡的主要原因。     

鸡ND—IBD二联高免卵黄抗体的研制与应用

应用秦皇岛市流行的IBDV,配合ND弱毒疫苗免疫蛋鸡制备出ND—IBD高免卵黄抗体,经各项检验、初步应用符合治疗和预防ND、IBD的要求,具有特异、快速、成本低、易制备的特点。     

胚期接种IBD疫苗对雏鸡ND4倍剂量免疫接种效果之影响

为了研究用IBD疫苗进行鸡胚免疫的可行性，探讨了胚期接种IBD疫苗对雏鸡ND4倍剂量免疫接种效果的影响．将IBD中等毒力疫苗接种18日龄鸡胚，出壳后采用4倍剂量ND疫苗进行免疫，通过抗体水平、免疫细胞数量及功能和免疫保护力等的检测，结果表明：胚期接种IBD中等毒力疫苗对雏鸡4倍剂量免疫仍具有免疫抑制作用．     

Chrysophanol Attenuates Manifestations of Immune Bowel Diseases by Regulation of Colorectal Cells and T Cells Activation In Vivo

Inflammatory bowel disease (IBD) is an immune disorder that develops due to chronic inflammation in several cells. It is known that colorectal and T cells are mainly involved in the pathogenesis of IBD. Chrysophanol is an anthraquinone family member that possesses several bioactivities, including anti-diabetic, anti-tumor, and inhibitory effects on T cell activation. However, it is unknown whether chrysophanol suppresses the activity of colorectal cells. In this study, we found that chrysophanol did not induce cytotoxicity in HT-29 colorectal cells. Pre-treatment with chrysophanol inhibited the mRNA levels of pro-inflammatory cytokines in tumor necrosis factor-α (TNF-α)-stimulated HT-29 cells. Western blot analysis revealed that pre-treatment with chrysophanol mitigates p65 translocation and the mitogen-activated protein kinase (MAPK) pathway in activated HT-29 cells. Results from the in vivo experiment confirmed that oral administration of chrysophanol protects mice from dextran sulfate sodium (DSS)-induced IBD. Chrysophanol administration attenuates the expression of pro-inflammatory cytokines in colon tissues of the DSS-induced IBD model. In addition, we found that oral administration of chrysophanol systemically decreased the expression of effector cytokines from mesenteric lymph nodes. Therefore, these data suggest that chrysophanol has a potent modulatory effect on colorectal cells as well as exhibiting a beneficial potential for curing IBD in vivo.     

(Poly)phenols in Inflammatory Bowel Disease and Irritable Bowel Syndrome: A Review

(Poly)phenols (PPs) may have a therapeutic benefit in gastrointestinal (GI) disorders, such as irritable bowel syndrome (IBS) or inflammatory bowel disease (IBD). The aim of this review is to summarise the evidence-base in this regard. Observational evidence does not give a clear indication that PP intake has a preventative role for IBD or IBS, while interventional studies suggest these compounds may confer symptomatic and health-related quality of life improvements in known patients. There are inconsistent results for effects on markers of inflammation, but there are promising reports of endoscopic improvement. Work on the effects of PPs on intestinal permeability and oxidative stress is limited and therefore conclusions cannot be formed. Future work on the use of PPs in IBD and IBS will strengthen the understanding of clinical and mechanistic effects.     

Diterpenoids Isolated from Podocarpus macrophyllus Inhibited the Inflammatory Mediators in LPS-Induced HT-29 and RAW 264.7 Cells

Species of Podocarpus are used traditionally in their native areas for the treatment of fevers, asthma, coughs, cholera, chest pain, arthritis, rheumatism, and sexually transmitted diseases. To identify natural products having efficacy against inflammatory bowel disease (IBD), we identified a new, 16-hydroxy-4β-carboxy-O-β-D-glucopyranosyl-19-nor-totarol (4) together with three known diterpenoids from P. macrophyllus. Furthermore, all the extracts, fractions, and isolates 1–4 were investigated for their anti-inflammatory effects by assessing the expression on nitric oxide (NO) production and proinflammatory cytokines in lipopolysaccharide (LPS)-stimulated RAW 264.7 and HT-29 cells. Among them, nagilactone B (2) exhibited a potent anti-inflammatory effect against NO production on RAW 264.7 cells; therefore, nagilactone B was further assessed for anti-inflammatory activity. Western blot analysis revealed that nagilactone B significantly decreased the expression of LPS-stimulated protein, inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, and phosphorylated extracellular regulated kinase (pERK)1/2. In addition, nagilactone B downregulated tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-8 levels in LPS-induced macrophages and colonic epithelial cells. To our best knowledge, this is the first report on the inhibitory effect of nagilactone B (pure state) and rakanmakilactone G against NO production in LPS-stimulated RAW 264.7 cells. Thus, diterpenoids isolated from P. macrophyllus could be employed as potential therapeutic phytochemicals for IBD.     

Metabolism of the colonic mucosa in patients with inflammatory bowel diseases: an in vitro proton magnetic resonance spectroscopy study

Metabolism of the colonic mucosa of patients with ulcerative colitis (UC; n=31) and Crohn's disease (CD; n=26) and normal mucosa (control, n=26) was investigated using in vitro high-resolution proton magnetic resonance spectroscopy. Of the 31 UC patients, 20 were in the active phase and 11 were in the remission phase of the disease. Out of 26 CD patients, 20 were in the active phase, while 6 were in the remission phase of the disease. Twenty-nine metabolites were assigned unambiguously in the perchloric acid extract of colonic mucosa. In the active phase of UC and CD, significantly lower (P相似文献   

茶多酚对AOM/DSS诱导高脂饮食小鼠结直肠癌的影响

探讨茶多酚(TP)对长期高脂饮食小鼠结肠炎相关性结肠癌(CAC)发生发展的影响及其可能机制。将5周龄BALB/c小鼠50只随机分为对照组、HFD组、AOM/DSS组、HFD+AOM/DSS组和HFD+AOM/ DSS+TP组,采用三次循环腹腔注射氧化偶氮甲烷(AOM)以及饮用2%葡聚糖硫酸钠(DSS)建立CAC模型。通过实时荧光定量PCR检测TNF-α、IL-6、COX-2、 IL-4、IL-10、β-catenin和C-myc 的mRNA表达水平;通过Western Blotting 检测β-catenin、P-GSK3β和GSK3β蛋白表达量;通过HE染色观察结直肠形态结构,免疫细胞浸润程度。结果表明：与HFD+AOM/DSS组相比茶多酚上调了TNF-α、IL-6、COX-2、β-catenin和C-myc的表达(P<0.05),下调了IL-4、IL-10的表达(P<0.05),促进了β-catenin的降解,显著降低AOM/DSS诱导CAC小鼠模型结直肠肿瘤的发生、抑制了结直肠缩短、维护了肠道屏障的完整。说明茶多酚能缓解炎症反应并抑制了Wnt信号系统的活化,对CAC有明显抑制作用。     

Correcting for biases in affected sib-pair linkage analysis caused by uncertainty in sibling relationship

When there is uncertainty in sibling relationship,the classical affected sib-pair(ASP) linkage tests may be severely biased.This can happen,for example,if some of the half sib-pairs are mixed with full sib-pairs.The genomic control method has been used in association analysis to adjust for population structures.We show that the same idea can be applied to ASP linkage analysis with uncertainty in sibling relationship.Assuming that,in addition to the candidate marker,null markers that are unlinked to the disease locus are also genotyped,we may use the information on these loci to estimate the proportion of half sib-pairs and to correct for the bias and variance distortion caused by the heterogeneity of sibling relationship.Unlike in association studies,the null loci are not required to be matched with the candidate marker in allele frequency for ASP linkage analysis.This makes our approach flexible in selecting null markers.In our simulations,using a number of 30 or more null loci can effectively remove the bias and variance distortion.It is also shown that,even the null loci are weakly linked to the disease locus,the proposed method can also provide satisfactory correction.