Latest ArticlesGlioblastoma is a malignant tumor in central nervous system, which has strong invasion, poor prognosis and short survival time. At present, the main treatment strategy of glioblastoma is surgical excision, supplemented by radiotherapy and chemotherapy. However, due to incomplete resection and high recurrence rate, it is urgent to find novel therapeutic method for glioblastoma. Photodynamic therapy, as a promising non-surgical treatment, provides a new strategy for postoperative adjuvant therapy of glioblastoma. This review summarizes the mechanism and clinical application of photodynamic therapy mediated by various photosensitizers in glioblastoma, in order to provide help for the treatment of glioblastoma.
Twenty compounds were isolated from the ethyl acetate extract of Smilax glabra by using various chromatographic techniques, including macroreticular resin, silica gel, Sephadex LH-20 and semi-preparative HPLC. Their structures were elucidated by physicochemical properties, MS and spectroscopic data. These compounds were elucidated as glabraside A (1), glabraone A (2), 5-hydroxy-3ʹ, 4ʹ, 7-trimethoxy-flavanone (3), naringenin (4), quercetin 7-O-α-L-rhamnoside (5), neoastilbin (6), neoisoastilbin (7), isoastilbin (8), eriodictyol-7-O-β-D-glucopyranoside (9), naringenin-7-O-α-L-rhamnoside (10), kaempferol 3-O-[4′′′′′-O-acetyl-α-L-rhamnosyl-(1→6)]-[β-D-glucopyranosyl-(1→2)]-β-D-glucopyranoside (11), 5-hydroxymaltol (12), 3, 4, 5-trimethoxyphenyl-1-O-β-D-glucopyranoside (13), 2-(3′, 4′-dihydroxyphenyl)-1, 3-benzodioxole-5-aldehyde (14), kompasinol A (15), (+)-syringaresinol (16), cis-resveratrol (17), trans-resveratrol (18), flufuran (19) and 5-hydroxymethyl-furaldehyde (20). Two new compounds (1 and 2) showed inhibitory activity toward nitric oxide (NO) production, with IC50 values of 56.8 and 29.5 μmol·L-1, respectively.
The high mortality of tumor is one of the most urgent problems to be solved. However, the current clinical trials provide limited quantitative descriptions on dynamic changes of drug efficacy, which restrict the selection of dosing regimens. Quantitative systems pharmacology (QSP) is a new approach for precise treatment of tumors. It quantifies the network relationship between drug action and diseases by integrating the tumor growth and molecules, cells in vivo, thereby predicting the efficacy, toxicity, and mechanism of antitumor drugs as well as identifying predictive biomarkers. In this review, we provide an overview of definition of QSP, current approaches and typical applications in research of antitumor drugs to enhance our understanding of QSP.
Silk fibroin is a natural polymer with certain water solubility, structural modification, good biocompatibility and biodegradability, which can be used as a drug delivery carrier material. As a promising drug delivery system, drug-loaded silk fibroin nanoparticles can control drug release, reduce toxicity and improve therapeutic effects. In this paper, the basic characteristics of silk fibroin, the preparation methods of drug-loaded silk fibroin nanoparticles and the application of silk fibroin in nanoparticulate drug delivery systems are reviewed, and on this basis, the further development of drug-loaded silk fibroin nanoparticles is prospected.
The MYC gene, one of the most common dysregulated driver genes in human cancers, is composed of three paralogous genes C-MYC, N-MYC and L-MYC. It is abnormally activated in more than half of cancer types. Since MYC plays an important role in the formation, maintenance and progression of cancer, targeting MYC is an effective strategy for cancer treatment. As a potential anti-cancer target, MYC is considered "undruggable" because it lacks a suitable pocket for accommodating small molecule inhibitors. Recently, under the guidance of protein structure information and many computational tools, many indirect strategies to inhibit MYC have emerged and shown favorable anti-cancer effects in tumor models. In this paper, the recent small molecules that indirectly target MYC are divided into inhibitors acting on the protein-protein interaction (PPI) among MYC and other proteins, and targeting inhibitors regulating MYC action. Additionally, the introduction and assessment towards compounds with different mechanisms are summarized to provide reference for the further research of MYC inhibitors.
The mitochondrial enzyme glutaminase C (GAC) is highly expressed in a variety of cancer cells, resulting in increased glutamine metabolism and cancer development. Therefore, GAC has become a potential target for anti-tumor drug development. However, current GAC inhibitors shared similar structural characteristics, few new scaffolds were reported. By conducting a prokaryotic Escherichia coli expression system, human GAC protein of high-purity was obtained through lysozyme digestion combined with ultrasound dissociation, and cobalt magnetic beads purification, Moreover, we performed studies to validate interaction between small molecules and GAC protein through thermal shift assay, drug affinity responsive target stability assay, protein crosslinking and GAC enzyme activity detection. Meanwhile, a comprehensive small molecule-protein interaction confirmation and systematic pharmacodynamic study in vitro were carried out on compound C19, which was a reported GAC inhibitor screened from the Enamine database. Results showed that C19 directly bind to GAC protein, disturbed GAC tetramers formation, and inhibited its enzyme catalytic activity. By interfering GAC function, C19 dose-dependently suppressed GAC-mediated glutamine metabolism, reduced glutamate in cancer cells, and thus alleviated A549 and NCI-H1299 non-small cell lung cancer cell growth. Together, C19 was identified as a lead compound, providing a new strategy for the structural design of drugs targeting GAC.
In this study, chronic emotional stress-induced H1N1 influenza susceptibility model was employed to simulate the states of "emotional stagnation" and "liver fire invading lung", and the protective effect of Qinggan Xiefei Fang on viral pneumonia was investigated. Survival rate and morbidity rate of mice were observed within 21 days after H1N1 infection, the symptoms of viral pneumonia and the level of phospholipid peroxidation were detected in lungs of mice after 6-day infection. The experimental results showed that Qinggan Xiefei Fang could alleviate the decline of survival rate and morbidity rate of mice caused by chronic constraint stress loaded with H1N1, inhibit the replication of H1N1 and the production of inflammatory factors, reduce the level of phospholipid peroxidation, and improve the symptoms of pneumonia in mice. The results also showed that compound-target network of Qinggan Xiefei Fang contained 171 compounds and 260 corresponding targets involved in the signaling pathway of oxidative stress, inflammation and immunity. All the above results indicate that Qinggan Xiefei Fang protecting influenza virus pneumonia was related to the regulation of oxidative stress. The animal experimental protocol has been reviewed and approved by Laboratory Animal Ethics Committee of Jinan University, in compliance with the Institutional Animal Care Guidelines.
Four compounds were isolated from the 70% EtOH extract of Ardisia crispa by using various chromatographic techniques, including silica gel, ODS and semi-preparative HPLC. The structures of 1-4 were elucidated based on physicochemical properties and spectroscopic data. These compounds were defined as crispalactone A (1), (+)-pinoresinol (2), 3, 5-dimethoxy-4- hydroxyphenol-1-O-β-D-glucopyranoside (3) and (+)-schizandriside (4). Compound 1 is a new γ-valerolactone derivative, and compounds 2-4 are firstly isolated from Ardisia crispa.
Although current synthetic anti-gout drugs have significant therapeutic effects in reducing serum uric acid levels, they have serious side effects such as allergic reactions and liver and kidney damage. Natural products with a wide range of uric acid-lowering and high safety have played a critical role in anti-gout drug discovery and development. This paper reviews the natural products with uric acid-lowering or anti-gout pharmacological effects and the investigation on their mechanisms of action, to provide information for drug discovery and development.
This study was designed to obtain recombinant human thioredoxin (rhTXN) by gene cloning and prokaryotic expression, and evaluated its therapeutic effect in the mouse ulcerative colitis (UC) model induced by dextran sulfate sodium (DSS). The human thioredoxin gene TXN was cloned from the cDNA of Jurkat cells. The recombinant expression plasmid pCold TF-rhTXN was constructed by restriction enzyme digestion. After expression in E. coli BL21 (DE3), recombinant human thioredoxin was purified by a nickel column. Intact rhTXN recombinant protein was obtained after removal of the fusion partner-tag by enzyme digestion and the activity of disulfide reductase was detected by the insulin reduction method. The animal experiments in this study were performed in accordance with the ethical guidelines of the Laboratory Animal Welfare Ethical Review Committee of Nanjing University. Experiment ulcerative colitis was induced by providing mice with sterilized drinking water which contained 3% DSS. rhTXN was injected intraperitoneally. The therapeutic effect was studied by weight change, colon length and HE (hematoxylin and eosin) stained sections. In vivo imaging was used to study the targeting of rhTXN to DSS mice. The GSE107499 data set of GEO database was used to screen the hub genes at the lesional sites of UC and study the correlation with TXN. The experimental results showed that rhTXN was successfully expressed and purified with disulfide reductase activity. rhTXN (100 μg·kg-1) had a significant therapeutic effect on maintaining the weight change of mice (P = 0.000 5) and reducing intestinal injury (P < 0.000 1), and had a colon targeting effect on DSS mice. In GSE107499 data set, TXN in inflammatory sites of UC patients was significantly down regulated (P < 0.01) and negatively correlated with hub gene CD40 (P < 0.01) and positively correlated with hub gene fibronectin 1 (FN1) (P < 0.01). In this study, biologically active rhTXN was successfully prepared and proved to have a promising therapeutic effect on the DSS mouse model, and TXN gene was significantly correlated with the UC hub genes CD40 and FN1.
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