Latest ArticlesWith the development of polymeric materials and nanotechnology, the potential application of nanoscaled drug delivery system (NDDS) is gradually manifested in the field of pharmaceutics. Especially, NDDS has the obvious advantages in the delivery of gene or drug. Comparing to the delivery system of single-drug, co-delivery system of gene and drug can significantly improve the therapeutic effects by enhancing transfection efficiency of gene and reversing multidrug resistance, etc. The co-delivery systems of gene and drug, which had the triggered release characteristics in the inner and outer of tumor, could be constructed by introducing the environment-responsive (pH-responsive, redox-responsive and light-responsive, etc) groups into the co-delivery system. The antitumor activity was further improved. In the present paper, the environment-responsive delivery systems in the application of co-delivery gene and drug in recent years were reviewed, and their remarkable properties in the antitumor activity were analyzed and summarized.
Strategies and techniques are extremely important to improve the evaluation efficiency and fully guarantee the consistency of dosage forms. For preparations with a structural feature as solid dosage forms and particulate dispersion systems, the structures of dosage forms are the outcome of the specific formulation and production process, which determine the drug delivery behaviors as well as the pharmacokinetics of the dosage forms. Conventional techniques failed to quantitatively determine the structures of dosage forms. Synchrotron radiation micro-computed tomography is a new generation of structural quantitative characterization technology in revealing the internal structure of dosage forms with unprecedented capability for quantitative characterization of the static and dynamic structures of dosage forms, enabling to reversely analyze the production process and identify the structure differences between the generics and brand products. Based on synchrotron radiation micro-computed tomography methodology researches and applications in static structures (powders, particulate systems, tablets, films, membranes, etc.), dynamic structures (hydration) and de-formulation of production process, we have classified the structures of dosage forms into four levels from macro-scope to molecular level as dosage forms, granular intermediates for formulation, dynamic structure and molecular structures, and proposed dosage form structure based new strategy for consistency evaluation. Along with conventional dissolution/ release behavior similarity, the internal structure consistency ensures high consistency between the brand product and the generics.
Thirty-three compounds were designed and synthesized directly from three-component, one-pot condensation of 1-(4-methylphenyl) ethanone and aromatic amines with some aromatic aldehydes. The chemical structures of the Mannich bases were confirmed by 1H NMR, IR and MS. The screening results of bioactivity indicated that all of these title compounds possessed the inhibitory activity at the concentration of 1×10-4 mol·L-1. Among them, the compound TM33 displayed the strongest bioactivity with the inhibition percentage of 60.3% against P338 cancer cell line at the concentration of 1×10-8 mol·L-1, and the value of the half maximal inhibitory concentration (IC50) was as low as 0.45 nmol·L-1. This study suggests a new type of potential anti-leukemia molecules.
The aim of the present study was to explore a sensitive, stable and reliable method for evaluating the phagocytosis, in which RAW264.7 macrophages engulfed GFP-Escherichia coli was tested by high-content screening technology. The study was conducted to optimize the method in evaluation of traditional Chinese medicine in the promotion of macrophage function. By testing macrophages at different ratio of bacteria to cells (multiplicity of infection, MOI), and at different incubation time, we optimized a high content screening method and the experimental parameters to determine the impact of bacteria in macrophages (fluorescence intensity index = be swallowed bacteria/macrophages). The method was used to determine whether Dendrobium moniliforme (DM) have effects on macrophage phagocytosis. The results show that the index has a positive relationship with MOI values, and the highest index was observed at incubation time of 1.5 h. The optimized conditions was 1×104 cells/well with a MOI of 50:1 (bacteria:cells) with incubation of 1.5 h. Under this condition, the relative standard deviation (RSD) was less than 10% in the precision test. Using the method to detect DM regulating macrophage phagocytosis experiment results showed that in 0.31-2.50 g·L-1 concentration range, DM has a dose-response effect in promoting phagocytosis. We successfully established the method for evaluation of macrophage phagocytosis, and proved the activity of DM in promotion of macrophage phagocytosis.
This paper was prepared to analyze and discuss the main content of the Botanical Drug Development Guidance for Industry by United States FDA's (the draft version of the 2015), especially focused on the guidelines for clinical research (mainly in late-stage clinical studies) recommendations and requirements sectiones. The key and difficult issues in the late clinic study were analyzed and discussed, and a series of countermeasures were proposed in this paper. At the same time, combined with the case of approved botanical drug products, analysis of the guidelines for the development of plant drug regulations, the enlightenment were presented in the last part, to guide the research and development of traditional Chinese medicine and the internationalization of Chinese medicine.
The 26S proteasome is a 2.5 MDa complex of the protease family members and is central to a vast array of vital cellular processes including cell-cycle progression and antigen presentation. It has been proven to be a target for therapeutic agents in the treatment of cancers and autoimmune diseases. Most inhibitors are designed to target the 20S proteolytic core complex while the efforts to target the 19S regulatory particle subunits are less successful so far. This is, in part, due to the complexity of molecular architecture and poor understanding of the mechanism of this subcomplex. This review attempts to summarize the development of inhibitory molecules that target both the 20S and 19S subunits of the proteasome, especially highlight the recent progress in the proteasome structure and development of the new inhibitors.
This study was designed to investigate the microRNA expression profile in human embryonic lung fibroblast 2BS cells upon salidroside (SAL) treatment, and predict the target genes of miRNAs and related pathways delaying cellular senescence. Samples were divided into three groups: young control (28 PD), old control (50 PD), and old+SAL (50 PD with SAL), RNA from three groups was used for miRNA microarray analysis. In late PD cells, 43 miRNAs were found significantly changed relatively to those in young cells, and 58 miRNAs were regulated by SAL. The miRNAs including hsa-let-7c, hsa-let-7e and hsa-mir-3620 were significantly down-regulated in late PD cells which could be reversed by SAL treatment. However, hsa-mir-411, hsa-mir-24-2-5p and hsa-mir-485-3p exhibited an opposite trend. Gene Ontology and Pathway analysis revealed that target genes were significantly enriched in 31 GO and 11 pathways. The microarray data was further validated with qRT-PCR. This research provides new clues regarding the underlying mechanisms of SAL on cellular senescence through miRNAs regulation.
NMR-based metabolomics technique has been applied to botanical studies in recent years. The plant metabolites are complicated and various, metabolomics method can detect the global metabolomic profile of the plant to track valuable metabolites, and provide information for the research of plant physiology, metabolic pathways and functional genes. This paper reviews the application of NMR-based metabolomics technique in medicinal plants, including the biosynthetic mechanism and production of secondary metabolites, the improvement of yield or quality of medicinal plants, the development of effective active ingredient, the identification of medicinal plant species, and the quality control of herbal medicine. In addition, the potential development of this technique in future is discussed.
Neural stem cells (NSCs) posse the specialty of tumor tropism and be able to migrate specifically to tumor cells. NSCs are also cross the blood brain barrier. NSCs keep in touch with tumor cells preferentially under the tumor microenvironment, and surround the target cells. Based on these characteristics, NSCs can be used as a carrier for therapeutic virus, enzymes/prodrugs, genes or suicide genes, etc. which are selectively delivered to the glioma cells. NSCs may be modified by a variety of different genes to establish a reliable, safe and effective therapy for glioma.
L-Glutamate is an important amino acid in protein. It has many physiological functions, such as nutrient metabolism, energy supply, immune response, oxidative stress, and signaling pathways regulation. Recent studies have found that glutamate prevents gastrointestinal damage induced by non-steroidal anti-inflammatory drugs (NSAIDs) and promotes the healing of the lesions. It can inhibit colonization of Helicobacter pylori and cell apoptosis caused by NH3. Hence, it has a potential value in protection of gastrointestinal from damage caused by NSAIDs and Helicobacter pylori. This article provides a review of the metabolism and physiological function of glutamate and its protective mechanisms of gastrointestinal injury caused by NSAIDs and Helicobacter pylori, which may serve as a reference in the study of glutamate in drug development.
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