Objective To investigate the correlation between MEX3A and differentiation characteristics of gastric cancer and intestinal metaplasia,and its combination with caudal-related homeobox transcription factor 2(CDX2)and mucin 2(MUC2)and mucin 5AC(MUC5AC)to determine the role of carcinogenic intestinal metaplasia.Methods From January 2010 to December 2014,a total of 410 cases of gastric cancer and paracarcinoma paraffin-embedded tissue samples were selected from the Central Hospital Affiliated to Shenyang Medical College and the Second Hospital Affiliated to Shenyang Medical College.According to pathological diagnosis,they were divided into control group(mild superficial gastritis,79 cases),intestinal metaplasia group(149 cases)and gastric cancer group(182 cases).The expressions of MEX3A,CDX2,MUC2 and MUC5AC were detected by immunohistochemistry.Results MEX3A was highly expressed in gastric cancer group and intestinal metaplasia group,especially diffuse gastric cancer,poorly differentiated gastric cancer and type Ⅲ intestinal metaplasia(P<0.05).CDX2 and MUC2 were highly expressed in gastric cancer group and intestinal metaplasia group,especially intestinal type gastric cancer,highly and moderately differentiated gastric cancer,type Ⅰ and type Ⅱ intestinal metaplasia(P<0.05).The expression of MUC5AC was high in control group and low in gastric cancer group and intestinal metaplasia group,especially in intestinal type gastric cancer,type Ⅰ and type Ⅲ intestinal metaplasia(P<0.05).Gastric cancer and intestinal metaplasia differentiation were negatively correlated with MEX3A and MUC5AC expression,but positively correlated with CDX2 and MUC2 expression(P<0.05).MEX3A was negatively correlated with the expression of CDX2 and MUC2,and positively correlated with the expression of MUC5AC in gastric cancer(P<0.05).MEX3A was negatively correlated with the expression of CDX2 and MUC2 in intestinal metaplasia(P<0.05),while CDX2 was positively correlated with the expression of MUC2(P<0.05).Conclusion MEX3A is negatively correlated with gastric cancer and intestinal metaplasia differentiation.Gastric cancer is characterized by high MEX3A expression and low CDX2 and MUC2 expression.

The package leaflet is a legal document relevant with drug information, which plays an important role for instructing the rational use of the medicinal product for the patient population. During the registration application in the EU countries, the patient readability test on package leaflet is the essential requirement to ensure the leaflet information easy-to-understand and avoid any risk caused by misunderstanding. The readability research on package leaflet can improve its quality and drug use safety to patients. Currently, CFDA does not publish any regulation/guidance on the drug application in China. By the successful case of registration application of Danshen Capsule as the herbal medicine in the EU, this paper not only discusses the relevant requirements of readability test in the EU, but also offers the regulatory advice on future regulations of readability research of the pharmaceutical products in China.

Polygalae Radix used as Chinese materia medica has a long history. The main chemical constituents include triterpenoid saponins, xanthones, oligosaccharide esters, and so on. The study shows that Polygalae Radix has a wide range of pharmacological activities, such as sedative hypnotic, anticonvulsant, antiaging, antidementia, brain protection, cough expectorant, antidepressant, antibacterial, and anticancer. In this paper, through referring to the domestic and foreign relevant literatures on Polygalae Radix systematically, we summarize the chemical composition, pharmacological activity, and structure activity relationship of Polygalae Radix, which could provide the reference for the further investigation and development of this plant.

To provide the reference for selecting the research and development trend and direction of new drug in Chinese materia medica (CMM). We sorted out the new drugs of CMM approved by the China Food and Drug Administration (CFDA) during 2010-2014 through database retrieval, analyzed their indications, declared period and approval rates, then discuss and suggest the predominance of CMM for research and development. In recent five years, among the new drugs of CMM approved by CFDA, their main indications are those for cardiovascular system, respiratory system, and urogenital system. The declared period from short to long is gynaecology system, respiratory system, and urogenital system. From the point of approval rates, urogential system and pediatric system are higher than others. Comprehensive the above three factors, we get that cardiovascular system is a classic indication for CMM; Urogenital system, pediatrics system and gynecologic system will be the potential fields for CMM research and development.

Objective: To separate antitumor constituent AD-1 [20(R)-25-OCH3-protopanoxadiol (PPD)] from non-racemic enatiomeric mixture. Methods: A crystallization method has been developed to separate AD-1 from 25-OCH3-PPD non-racemic enatiomeric mixture, the sorts and amount of solvent and crystallization temperature were optimized to obtain the best separative conditions, and the relationship between the S/R percentage of 25-OCH3-PPD non-racemic enantiomeric mixture and dielectric constant of the solvent was discussed. Results: Under the optimized conditions (acetone 26 mL, 4°C), the yield and purity of AD-1 crystals are 38.76% and 97.83% from 25-OCH3-PPD non-racemic enatiomeric mixture (R: 59.34%; S: 38.35%), respectively. Conclusion: The ε values of solvents are about 20.7, and an unsaturated solution and low temperature are beneficial to the separation of AD-1 from 25-OCH3-PPD non-racemic enatiomeric mixture.

OBJECTIVE: To optimize the formulation of the lutein thermosensitive in situ gels by using central composite design-response surface methodology, and study the drug release in vitro. METHODS: Gelation temperature was served as the indicator. The influences of the amounts of Poloxamer 407 and Poloxamer 188 on the gelation temperature were investigated. Central composite design-response surface method was used to optimize the prescription. The drug release profile of the preparation was investigated with a membrane-less dissolution model. RESULTS: The amounts of Poloxamer 407 and Poloxamer 188 had quantitative relationships with the gelation temperature. The optimum prescription was as follows: the mass concentration of P407 was 0.21 g · mL-1, and the mass concentration of P188 was 0.03 g · mL-1. The dissolution and drug release of the gels followed zero-order kinetics equation. CONCLUSION: Central composite design-response surface methodology can be applied to optimize the formulation of the lutein thermosensitive in situ gels.

A commercial albumin-bound paclitaxel nano-formulation has been considered a gold standard against breast cancer. However, its application still restricted unfavorable pharmacokinetics and the immunogenicity of exogenous albumin carrier. Herein, we report an albumin-bound tumor redox-responsive paclitaxel prodrugs nano-delivery strategy. Using diverse linkages (thioether bond and disulfide bond), paclitaxel (PTX) was conjugated with an albumin-binding maleimide (MAL) functional group. These pure PTX prodrugs could self-assemble to form uniform and spherical nanoparticles (NPs) in aqueous solution without any excipients. By immediately binding to blood circulating albumin after intravenous administration, NPs are rapidly disintegrated into small prodrug/albumin nanoaggregates

The surface hydrophobicity of nanoparticles plays an important role in drug delivery process. The aim of this study was to verify the feasibility of using self-assembly method to prepare drug-loaded nanoparticles with tunable surface hydrophobicity. Here, Soluplus was selected as the polymeric carrier to prepare panobinostat (PNB) loaded micelles. Three different monoglycerides, glycerly monooleate (GMO), glycerly linoleate (GML) and glycerly linolenate (GMLO), were used to modify the surface of PNB-Soluplus micelles to prepare polymer-lipid hybrid nanoparticles (PLHNs). The effect of monoglyceride type and amount on the physico-chemical properties of PNB-loaded PLHNs was investigated, and the surface hydrophobicity of PLHNs was characterized by Rose Bengal (RB) binding method and mucin particle method. The results suggested that compared with the PNB-Soluplus micelles (particle size 77.97 ± 0.78 nm, zeta potential 0.44 ± 0.29 mV, entrapment efficiency 99.45% ± 1.47%, the RB binding constant (K) value 0.008 ± 0.002, the increased particle size after mixing with mucin particles 7.90 ± 1.41 nm), surface hydrophobicity of the PLHNs increased significantly when modified by GMO, GML, GMLO, with K values of 0.055 ± 0.010, 0.050 ± 0.011 and 0.058 ± 0.008, respectively. The increased particle sizes after mixing with mucin particles were 17.37 ± 4.48 nm, 22.60 ± 2.10 nm and 25.13 ± 3.89 nm, respectively. Among them, the physico-chemical properties of the GMLO modified PNB-loaded PLHNs (particle size 81.60 ± 4.52 nm, zeta potential 0.77 ± 0.03 mV, entrapment efficiency 99.59% ± 0.20%) kept constant, thus GMLO was selected to further investigate the effect of GMLO mass ratio (1%-3%) to Soluplus on the properties of the nanoparticles. While no statistical significant difference in particle size, zeta potential, entrapment efficiency or in vitro release behavior was found when GMLO ratio increased, the surface lipophilicity of the PLHNs, as characterized by K values and the increased particle sizes after mixing with mucin particles, increased almost linearly with the increase of GMLO amount. In conclusion, we demonstrated that drug-loaded PLHNs based on Soluplus and GMLO can be prepared by self-assembly method, and the surface hydrophobicity was tunable by modifying the mass ratio of GMLO to Soluplus. This approach could be used for related basic science research aiming to elucidate the effect of surface hydrophobicity on in vivo behavior of drug-loaded system.

Recently, the incidence and mortality of cancer has raised. More and more cytotoxic drugs and molecular targeted medicines have been used in clinic. However, most drugs just display a short-term anti-tumor effect. If patients received treatment for a long time, it would arise resistance to chemotherapy frequently. One of its important reasons is the accumulation of drug induced cancer cells. Thus, this paper emphasizes on biological character of drug induced cells, including cell biological phenotype, the change of gene and protein, variation of metabolism, dynamic change of signal transduction pathway and so on. Meanwhile, according to the characteristics of drug induced cells, we propose some strategies to inhibit drug induced cells, which would provide the foundation of clinical therapy and novel anti-tumor drug research and development.

Due to the limited self-repair ability of neurons after injury, there has been a lack of effective treatments for nerve injury in clinical practice. So, to find drugs that promote the repair after nerve injury has become a research hotspot. Schwann cells and neurons play an important role in regeneration of the peripheral nerves after injury. This review summarizes the classification of peripheral nerve injury, the signaling pathways related to peripheral nerve regeneration in Schwann cells and neurons as well as diseases related to peripheral nerve injury, and provides a basis for further exploration of the regeneration mechanism after peripheral nerve injury.