111In–L–LDL and 153Gd–L–LDL as radiotracers for detection of AR4‐2J rat pancreatic tumors

Pancreatic cancer has an extremely poor prognosis, due, in part, to lack of methods for early diagnosis. The present study was designed to evaluate the potential of labeling low‐density lipoprotein (LDL) with a radionuclide using a lipid chelating agent, bis(stearylamide) of diethylenetriaminepentaacetic acid (L), to detect pancreatic tumors by gamma‐scintigraphy. Previous studies indicated that the difficulty of visualization of pancreatic tumors was due to their poor vascularization. This study compares the ability of two radiotracers, ¹¹¹In–L–LDL and ¹⁵³Gd–L–LDL to target highly vascularized rat pancreatic tumors (AR4‐2J) implanted in nude mice. Biodistribution studies showed that the tumor uptake of ¹¹¹In–L–LDL and ¹⁵³Gd–L–LDL tracers was twofold and fivefold higher respectively than with the controls (¹¹¹In citrate and ¹⁵³Gd citrate respectively). These tracers would thus be suitable for scintigraphic imaging. We show here that LDL could be employed as a delivery system for tracers such as ¹¹¹In or ¹⁵³Gd when these two radionuclides are complexed by a lipid‐chelating anchor, and that ¹¹¹In–L–LDL and ¹⁵³Gd–L–LDL enabled better visualization of the pancreatic tumor tissues, with a better result with ¹⁵³Gd–L–LDL. Copyright © 2004 John Wiley & Sons, Ltd.     

胰腺腺泡细胞胞浆游离钙浓度的测定及药物作用的研究

本文建立了用荧光指示利Fura－2测定胰腺腺泡细胞胞浆游离Ca2＋浓度（［Ca2＋］i）的实验技术,包括：胰腺腺泡的分离制备;Fura—2／AM的负载;腺泡悬液的荧光光谱测量等．测定了胰腺腺泡细胞［Ca2＋］i。的静息值和卡巴可促腺泡细胞［Ca2＋］i升高的剂量—效应关系及动力学过程,并研究了柴胡总皂甙对胰腺腺泡细胞［Ca2＋i］的影响．发现0．01mg／ml浓度的柴胡总皂甙使胰腺腺泡细胞［Ca2＋］。明显升高,0．1mg／ml浓度时可使［Ca2＋］。升高到静息值的3倍,提示柴胡总皂甙的促酶分泌作用是通过胞内［Ca2＋］i升高介导的．     

核糖核酸酶A在DAB-环乙烷溶液中的活性和构象

The activity and conformation of ribonuclerse A (RNaseA) solubilized in cyclohexane via dodecylammonium butyrate(DAB) reverse micelles were investigated. The activity of RNaseA was studied using the cytidine 2’,3’ -phosphate as the substrate, and it was found that kcat increases significantly with respect to that in water attended by an increased Km•FT-IR spectra of RNaseA in reverse micellar solution were investigated as a function of w0(= [H2O]/ [DAB]), and it was noted that the structure of RNaseA became losser in reverse micelles campared to that in aqueous solution. The relation between activity and conformation was discussed.     

Comparison of Transcriptomic Profiles of MiaPaCa-2 Pancreatic Cancer Cells Treated with Different Statins

Statins have been widely used for the treatment of hypercholesterolemia due to their ability to inhibit HMG-CoA reductase, the rate-limiting enzyme of de novo cholesterol synthesis, via the so-called mevalonate pathway. However, their inhibitory action also causes depletion of downstream intermediates of the pathway, resulting in the pleiotropic effects of statins, including the beneficial impact in the treatment of cancer. In our study, we compared the effect of all eight existing statins on the expression of genes, the products of which are implicated in cancer inhibition and suggested the molecular mechanisms of their action in epigenetic and posttranslational regulation, and in cell-cycle arrest, death, migration, or invasion of the cancer cells.     

Betulinic Acid Affects the Energy-Related Proteomic Profiling in Pancreatic Ductal Adenocarcinoma Cells

Pancreatic ductal adenocarcinoma (PDAC) is an aggressive disease with a 5-year survival rate of <8%. Therefore, finding new treatment strategies against PDAC cells is an imperative issue. Betulinic acid (BA), a plant-derived natural compound, has shown great potential to combat cancer owing to its versatile physiological functions. In this study, we observed the impacts of BA on the cell viability and migratory ability of PDAC cell lines, and screened differentially expressed proteins (DEPs) by an LC-MS/MS-based proteomics analysis. Our results showed that BA significantly inhibited the viability and migratory ability of PDAC cells under a relatively low dosage without affecting normal pancreatic cells. Moreover, a functional analysis revealed that BA-induced downregulation of protein clusters that participate in mitochondrial complex 1 activity and oxidative phosphorylation, which was related to decreased expressions of RNA polymerase mitochondrial (POLRMT) and translational activator of cytochrome c oxidase (TACO1), suggesting that the influence on mitochondrial function explains the effect of BA on PDAC cell growth and migration. In addition, BA also dramatically increased Apolipoprotein A1 (APOA1) expression and decreased NLR family CARD domain-containing protein 4 (NLRC4) expression, which may be involved in the dampening of PDAC migration. Notably, altered expression patterns of APOA1 and NLRC4 indicated a favorable clinical prognosis of PDAC. Based on these findings, we identified potential proteins and pathways regulated by BA from a proteomics perspective, which provides a therapeutic window for PDAC.     

MR Imaging of metastatic pancreatic VIPoma

The MR findings in a 32-year-old man with pancreatic VIPoma and liver metastases are described. A 2-cm mass was present in the region of the tail of the pancreas that was best shown on T₁-weighted fat-suppressed images as a low-signal intensity mass. Multiple liver metastases were present that showed intense peripheral ring enhancement on immediate post gadolinium spoiled gradient echo images.     

碳酸钙固定化猪胰脂肪酶的制备及活性研究

本文利用市售普通碳酸钙(general calcium carbonate,GCC)作为猪胰脂肪酶(PPL)固定化的载体材料,研究了不同固定化条件对所制备的固定化酶活性的影响.结果显示PPL固定化于GCC上的最佳制备工艺为:将20 mL酶液与1.50 g GCC放入置于摇床内的三角瓶中,摇床温度设为40℃,摇床转速设为...     

Biocatalysis for C–S bond formation: Porcine pancreatic lipase (PPL) catalysed thiolysis/hydrothiolation reactions in sole water

In this paper, a biocatalytic route is described wherein PPL, lipase from porcine pancreas, in conjunction with water on reaction with different thiophenols and styrene oxides undergo thiolysis with C-S bond formation without the use of any metal catalysts, oxidants, bases, additives or organic solvents towards formation of β-hydroxysulfides in good to excellent yields with high regioselectivity at room temperature. Furthermore, PPL also facilitates thiophenols to undergo hydrothiolation with styrenes or phenylacetylenes in sole water and thus forming linear thioethers or vinylsulfides respectively via C–S bond formation. In addition to the straightforward and atom-efficient protocol, a gram-scale synthesis of β-hydroxysulfide and recyclability for three consecutive cycles without decrease in efficiency of PPL make our biocatalytic protocol for constructing C–S bond highly valuable from both environmental and economic viewpoints than traditional chemical practices.