Latest ArticlesSerotonin (5-hydroxytryptamine, 5-HT) is an endogenous molecule playing key roles in life activity. In the treatment of metabolic diseases such as obesity, the traditional paradigm of appetite suppression by serotonin in the central nervous system has some limitations. In recent years, great progress has been made in the study of the regulation of energy metabolism by peripheral serotonin system. Recent studies revealed that peripheral serotonin plays an important role in regulation of adipogenesis and energy expenditure in adipose tissues, insulin secretion in pancreatic β-cell and glycogen synthesis in liver, etc. This review summarizes the recent advances in the function of serotonin in the peripheral organs of energy metabolism. We propose that peripheral serotonin system may serve as an attractive new therapeutic target for the treatment of metabolic diseases in the near future.
Transient receptor potential (TRP) channels are non-selective and cation-permeable channels in the cell membrane, widely distributed in tissues and organs of human body. As biosensors, TRP channels can regulate the functions of vision, hearing, taste, pain, and touch, etc. So far, more than 100 different kinds of natural modulators targeting TRP channels have been identified from 70 species of plants or animals. In this review article, we attempt to summarize the effect of known natural active compounds on TRP channels with focuses on their sources, structures, action features and mechanisms. Hopefully this review can provide some useful information that can facilitate discovery of more specific natural modulators, and development of innovative therapeutic drugs targeting TRP channels.
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.
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.
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.
The aim of this research is to investigate the inhibitory effects of calpain inhibitors (ALLN and calpain inhibitor Ⅳ) on mammary epithelial-mesenchymal transition (EMT) of MCF-10A cells induced by fibronectin (FN). After FN treatment of MCF-10A cells for 48 h, cell migration and invasion were determined by scratch repair assay and matrigel coated transwell assay, respectively. Vimentin, E-cadherin, snail and calpain-2 protein expression were measured by Western blot. The results suggest that FN induced morphological changes in MCF-10A cells, significantly increased the migration and invasion abilities of MCF-10A cells, upregulated the expression of calpain-2, vimentin and snail, and downregulated the expression of E-cadherin. All such changes by FN were reversed with ALLN and calpain inhibitor Ⅳ. In conclusion, the upregulation of calpain-2 was involved in FN-induced EMT of MCF-10A mammary epithelial cells, which may be inhibited by ALLN and calpain inhibitor Ⅳ.
Plumbagin (Plumbago zeylanica L.) has a wide spectrum of anticancer activity with a relatively lower toxicity. The molecular mechanisms of proliferation inhibition and apoptosis induction by plumbagin on esophageal squamous carcinoma cell lines may be important for the structure modification and clinical application of plumbagin. After treatment of KYSE-30, KYSE-70 and KYSE-140 cells with 0-20 μmol·L-1 of plumbagin for 24, 48, 72 h, CCK8 was used to examine the proliferation, Annexin V and PI immunofluorescence staining for apoptosis, real-time PCR and Western blot for FoxM1 mRNA and protein expression, dual-luciferase reporter gene assay for the transcriptional activity of FoxM1, respectively. In addition, the relationship between anti-tumor effect of plumbagin and FoxM1 was investigated in vivo. Plumbagin significantly inhibited proliferation and induced apoptosis of esophageal squamous carcinoma cell in vitro and in vivo. Moreover, plumbagin down-regulated the expression of FoxM1 through suppression of its gene transcription. Our findings suggest that plumbagin may inhibit the proliferation of esophageal squamous carcinoma cell in vivo and in vitro through down-regulating the expression of FoxM1.
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.
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