Neem--an omnipotent plant: a retrospection

Neem (Azadirachta indica A. Juss.) has universally been accepted as a wonder tree because of its diverse utility. Multidirectional therapeutic uses of neem have been known in India since the Vedic times. Besides its therapeutic efficacies, neem has already established its potential as a source of naturally occurring insecticide, pesticide and agrochemicals. Safe and economically cheaper uses of different parts of neem in the treatment of various diseases and in agriculture are discussed in this article. It further deals with the active chemical constituents of various neem formulations. Commercially available neem products are also mentioned along with their respective applications. Furthermore, evaluation of safety aspects of different parts of neem and neem compounds along with commercial formulations are also taken into consideration. Systematic scientific knowledge on neem reported so far is thus very useful for the wider interests of the world community.     

Transport of surface-modified nanoparticles through cell monolayers

We synthesized three peptides, a D-polyarginyl peptide (r8(FITC)), a Tat peptide (Tat(FITC)), and a control peptide (Cp(FITC)) and attached each to amino-CLIO, a nanoparticle 30 nm in diameter. We then examined the effective permeability, Peff, of all six materials through CaCo-2 monolayers. The transport of peptide-nanoparticles was characterized by a lag phase (0-8 h) and a steady-state phase (9-27 h). The steady-state Peff values for peptides were in the order r8(FITC)>Tat(FITC)=Cp(FITC). When r8(FITC) and Tat(FITC) peptides were attached to the nanoparticle, they conferred their propensity to traverse cell monolayers onto the nanoparticle, whereas Cp(FITC) did not. Thus, when the r8(FITC) peptide was attached to the amino-CLIO nanoparticle, the resulting peptide-nanoparticle had a Peff similar to that of this poly-D-arginyl peptide alone. The Peff of r8(FITC)-CLIO (MW approximately 1000 kDa) was similar to that of mannitol (MW=182 Da), a poorly transported reference substance, with a far lower molecular weight. These results are the first to indicate that the modification of nanoparticles by attachment of membrane-translocating sequence-based peptides can alter nanoparticle transport through monolayers. This suggests that the surface modification of nanoparticles might be a general strategy for enhancing the permeability of drugs and that high-permeability nanoparticle-based therapeutics can be useful in selected pharmaceutical applications.     

微波消解-电感耦合等离子体质谱法测定原料药中的残留钯

建立了一种微波消解-电感耦合等离子体质谱法(ICP-MS)测定利奥西呱原料药中残留钯含量的方法。方法:对样品进行微波消解前处理,优化调谐仪器参数后,以相对稳定的铑(1 03 Rh)作在线内标校准,采用ICP-MS法对样品中的钯元素进行定量测定分析。结果表明,原料药中钯元素标准曲线的线性范围为0~60.0μg/L,相关系数r为0.9996;7次重复性测试的相对标准偏差RSD为0.85%;加标回收率为90.14%~101.3%,相对标准偏差RSD为2.17%~2.44%。表明该方法简便快速、灵敏度高,准确可靠,适用于利奥西呱原料药中残留钯含量的测定。     

Quinone‐Fused Pyrazoles through 1,3‐Dipolar Cycloadditions: Synthesis of Tricyclic Scaffolds and in vitro Cytotoxic Activity Evaluation on Glioblastoma Cancer Cells

A novel and straightforward synthesis of highly substituted isoquinoline‐5,8‐dione fused tricyclic pyrazoles is reported. The key step of the synthetic sequence is a regioselective, Ag₂CO₃ promoted, 1,3‐dipolar cycloaddition of C‐heteroaryl‐N‐aryl nitrilimines and substituted isoquinoline‐5,8‐diones. The broad functional group tolerability and mild reaction conditions were found to be suitable for the preparation of a small library of compounds. These scaffolds were designed to interact with multiple biological residues, and two of them, after brief synthetic elaborations, were analyzed by molecular docking studies as potential anticancer drugs. In vitro studies confirmed the potent anticancer effects, showing promising IC₅₀ values as low as 2.5 μm against three different glioblastoma cell lines. Their cytotoxic activity was finally positively correlated to their ability to inhibit PI3K/mTOR kinases, which are responsible for the regulation of diverse cellular processes in human cancer cells.     

Preparation and evaluation of chitosan/β‐cyclodextrin magnetic nanoparticles as a photodegradable and hydrophobic drug delivery carrier

In this study, novel tumor targeting nanocarriers comprised of chitosan (CS)/β‐cyclodextrin (β‐CD) magnetic nanoparticles were prepared to improve the photodegradable stability and bioavailability of hydrophobic drug. Resveratrol (Res) with photodegradable and hydrophobic properties was selected as a model drug. The photodegradation rate of Res in Fe₃O₄ nanoparticles solution was 7.8 times lower than that in the ethanol solution_. In addition, the value of the saturation magnetization of CS/β‐CD nanoparticles was found to be 19.56 emu/g with characteristic of superparamagnetism. Approximately 90% Res was entrapped into the CS/β‐CD magnetic nanoparticles with the size distribution ranging from 200 to 359 nm, and the nanoparticles were spherical in shape with high zeta potentials. Furthermore, the formation of CS/β‐CD nanoparticles showed a sustained release in vitro. These results indicated that the obtained CS/β‐CD magnetic nanoparticles were a promising magnetic targeting carrier for photodegradable and hydrophobic drugs. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134, 45076.     

消化性溃疡药物治疗的现状

对治疗消化性溃疡药物进行了综述，文中叙述了降低胃酸及胃蛋白酶活性药物；增强胃粘膜抵抗力药物；促进胃排空药物；抗忧郁药物；胃肠激素类药物等。对这些药物的研究近年来都有很大进展，这些药物在治疗消化性溃疡方面取得了显著成绩，只要根据患者的病情和具体条件给以合理的治疗，消化性溃疡的治愈率可达９０％以上。     

Molecularly imprinted polymer-high performance liquid chromatography for the determination of tetracycline drugs in animal derived foods

In this study, a molecularly imprinted polymer solid phase extraction method combining high performance liquid chromatography was developed to determine the residues of tetracycline drugs in animal derived foods. The polymer was synthesized with chlortetracycline as template molecule, methacrylic acid as functional monomer at template/monomer ratio of 1:4. The prepared solid phase extraction column was able to capture four tetracyclines simultaneously with high adsorption capacities (3560–4700 ng) and high recoveries (>87%), and was able to be reused for at least thirty times. The limits of detection were in a range of 20–40 ng/g, and the recoveries from fortified blank samples (milk, egg and pork) were in a range of 74%–93%. Furthermore, the polymer-based column achieved better purification effect than three commercial solid phase extraction columns. This is the first study reporting the use of chlortetracycline based molecularly imprinted polymer for determination of tetracyclines in animal derived foods.     

Preparation and characterization of an oridonin nanosuspension for solubility and dissolution velocity enhancement

This study describes the preparation of an oridonin (ORI) nanosuspension by high-pressure homogenization (HPH). The aim was to obtain a stable nanosuspension with an increased drug saturation solubility and dissolution velocity. The homogenization procedure was optimized in regard to particle size and long-term stability. The characteristics of the oridonin nanosuspension, such as particle size, size distribution, shape, and zeta potential, were evaluated following the water removal. The solubility and dissolution experiments were performed to verify the obvious improvement of the dissolution behavior compared with commercial ORI. Finally, crystalline state evaluation before and following the formulation was performed through differential scanning calorimetry (DSC) and powder X-ray (PXRD).     

论化工行业易制毒化学品

在分析我省易制毒化学品生产及管理工作的特点与难点后,提出若干改进工作的建议,可为我省禁毒工作者提供参考。