Latest ArticlesThe methods for determination of freezing point include cooling curve cryoscopy and air humidity cryoscopy. These methods are usually influenced by many factors, such as instrumentation, environment and operators. Despite the numerous experimental methods, precise freezing point values are challenging to obtain due to time-consuming procedures, limited sample size and extensive manual work. In this study, a semi-empirical hydration model (SEHM) was developed to calculate freezing point of NaH2PO4-K2HPO4 mixed electrolyte solution. According to SEHM, the water activity of mixed electrolyte solution was calculated by molality of solutes. Then the freezing point of solution was calculated. The calculated results were compared with those obtained by cooling curve cryoscopy and air humidity cryoscopy. The results indicate that the SEHM calculations are comparable to the measurements of cooling curve cryoscopy and air humidity cryoscopy.
Cichorium glandulosum has been used to treat non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes mellitus (T2DM) in Uyghur folk medicine. The mechanism of Cichorium glandulosum (CG) on type 2 diabetes mellitus accompanied with non-alcoholic fatty liver disease (T2DM-NAFLD) remains unclear. The effect of CG extraction on T2DM-NAFLD was determined in animal experiments here (all the experiments here were approved by the Animal Care Committee of the First Affiliated Hospital of the Medical College, Shihezi University). The mechanism of CG for treatment of T2DM-NAFLD was predicted and verified based on systems pharmacology. Based on the active compounds of CG on T2DM-NAFLD, T2DM and NAFLD-related targets, pathways and diseases were screened and predicted. Active compounds-targets, compounds-targets-pathways and compounds-targets-diseases were constructed and analyzed. The results of animal experiments showed that CG extraction can reduce the levels of blood glucose and blood lipid in T2DM-NAFLD rats. In addition, it can improve the glucose tolerance and relieve liver injury. Total 29 active compounds and 198 targets were screened by systems pharmacology, of which 106 targets were involved in T2DM, 88 were involved in NAFLD, and 56 targets were common between T2DM and NAFLD, mainly related to insulin resistance and inflammation. These 198 targets include those in metabolic pathways, calcium pathway, PI3K/Akt pathway, cAMP pathway, and MAPK pathway. Our study confirmed that CG can be potential phytomedicine for treatment of T2DM-NAFLD. This work provides a reference for studying the treatment of multiple diseases using multiple-targets phytomedicine in systems pharmacology.
An HPLC fingerprint and multi-component determination method of Leonurus japonicus was established for comprehensive evaluation and quality control of Leonurus japonicus. The sample was incubated in 70% ethanol in a water bath for 2 h, and the extract was analyzed by HPLC using Kromasil C18 column (250 mm×4.6 mm, 5 μm). The mobile phase consisted of acetonitrile-0.1% formic acid with gradient elution. The flow rate was 1.0 mL·min-1. The temperature of column was 30℃. The detection wavelength was 280 nm. HPLC fingerprint of characteristic components of Leonurus japonicus was established. There were 12 common peaks among 25 batches of samples, and 5 of them were identified and determined. Syringic acid, leonurine hydrochloride, rutin, hyperoside or isoquercitrin showed a good linearity in the ranges of 0.426 1-85.22 ng (r=0.999 9), 7.948-1 590 ng (r=0.999 3), 10.20-2 040 ng (r=1.000 0), 2.018-403.6 ng (r=0.999 9), or 8.704-1 741 ng (r=0.999 9), respectively. The average recoveries were 99.0%, 97.6%, 97.4%, 96.9% and 98.5% with RSD of 1.1%, 1.8%, 1.4%, 1.5% and 1.3%, respectively. The HPLC characteristic fingerprint of Leonurus japonicus was specific, and this method can simultaneously determine the content of 5 components.
Tumor, especially malignant tumor has become one of the major diseases, a serious threat to the health of people around the world. Modern clinical practice shows that the natural active products extracted from traditional Chinese medicine, marine medicine and other natural drugs, such as terpenes, alkaloids, polysaccharides, volatile oils and peptides, can effectively inhibit the growth of tumor cells. In this paper, the active components of natural antitumor products in recent years were summarized and their related mechanism was elucidated, so as to provide theoretical basis for the further development of natural antitumor drugs.
Provirus Integration in Maloney murine leukemia virus (PIM) represents a novel class of unique Ser/Thr kinase, which has been identified to be over-expressed in multiple hematological malignancies and some solid tumors, and the expression quantity correlates with malignant grade and poor prognosis in patients with cancer. PIM kinase plays important roles in regulation of cell proliferation and differentiation through the phosphorylation of its protein substrates, and it has become the emerging target for cancer treatment. A large number of highly active PIM kinase inhibitors have been reported by domestic and foreign research institutions, and the research progress will be summarized according to affiliations in this review.
Drug-induced cardiotoxicity is recently a major concern. Cardiotoxicity is the leading cause of drug withdrawal from the market. Long-QT syndrome is one of the most important manifestations of cardiotoxicity. hERG potassium channel is an important target of drug-induced arrhythmia and antiarrhythmia drugs. Traditional Chinese medicine is a traditional medicine in China with a long history and a wide range of clinical use. However, the multi-organ toxicity caused by traditional Chinese medicine is still a problem to be solved. Some traditional Chinese medicines already in clinical use have been withdrawn from the market because of their potential cardiotoxicity or severe arrhythmias. The cardiac toxicity of more than 50 kinds of traditional Chinese medicines causing arrhythmia was reported, while more than 20 of them are induced by affecting on the hERG potassium channels. Therefore, finding out the mechanism of drug-induced long-QT syndrome and the regulatory target of drug intervention is the key research goal in today's medical field. In this paper, we summarized the mechanisms of long-QT syndrome induced by traditional Chinese medicine with Ikr/hERG potassium channel as the main target. It provides a theoretical basis for the rational use of related traditional Chinese medicine in clinical practice, the avoidance of cardiac toxicity and the development of regulatory targets for drug intervention.
Chiral amino acid analysis is a sensitive, efficient and economical method for controlling racemic peptide impurities, especially for synthetic polypeptide drugs with complex composition of amino acids. Unexpected amino acid enantiomers in racemic peptides can be measured by chiral amino acid analysis coupled with mass spectrometry. The position of amino acid isomerization in the peptide segment can be accurately mapped by mass spectrometry, which lays a solid foundation for screening of racemic peptide impurities and rapid identification or quantification of trace racemic peptide impurities. Combination of the two techniques is vital for quality control of the synthetic polypeptide drugs and for research of polypeptide drugs based on chemical synthesis. The strategies of peptide hydrolysis have been summarized in this review. The latest chiral amino acid analysis based on mass spectrometry is briefly reviewed. Based on our knowledge, we have pointed to the direction of research and control of racemic peptide impurities in synthetic polypeptide drugs.
Benzoxaborole is a series of compounds with five member ring and boron atom. Since the approval of crisaborole and tavaborole by FDA, benzoxaborole gained lots of research interests and become widely used in current drug discovery. Specially, benzoxaborole derivatives were found to exhibit anti-bacterial, anti-fungal, anti-protozoal, anti-tumor and anti-inflammatory activities. Here, we will review the properties of benzoxaborole, structure activity relationships as well as the recent progress in the biological activity of benzoxaborole derivatives.
Drug-induced cardiotoxicity is a serious concern in recent years, and acquired long QT syndrome (LQTS) is an important manifestation of cardiotoxicity. hERG gene encodes the α subunit of the rapidly activated delayed rectifier potassium channel (Ikr), which plays an important role in action potential phase 3 repolarization. Drug inhibition of Ikr/hERG channel leads to prolonged QT interval, accompanied by Tdp malignant arrhythmia, which can cause sudden death. We studied the effect of berberines on the hERG K+ channels after combination with rosuvastatin and glibenclamide, and evaluated the cardiac safety of these drugs in combination. Whole cell patch clamp technique was used to detect the effect of the combinations of these drugs on hERG current on HEK293 cells stably expressing hERG gene. The results showed that the inhibitory effects of berberine or dihydroberberberine combined with rosuvastatin on hERG current were higher than single drug (P < 0.05), but the combination had no effect on the kinetics of hERG channel. Berberine or dihydroberberberine combined with glibenclamide had higher inhibitory effects on hERG current than the application of single drug (P < 0.05) while the time constant of hERG channel inactivation was shortened after the combination (P < 0.05). In addition, the combination of berberine and glibenclamide inhibited hERG channel activation (P < 0.05). In conclusion, our results demonstrated that the combination of berberine with rosuvastatin or glibenclamide significantly inhibited hERG current and the inhibition effects were higher than the application alone. Therefore, when the two drugs that have inhibitory effects on the hERG channel are combined, the risk of inducing prolonged QT interval is significantly increased, and therefore reducing cardiac safety.
With the significant breakthrough that programmed cell death 1 (PD-1)/programmed cell death 1 ligand 1 (PD-L1) antibody drugs achieved promising clinical outcomes across various tumor types, immunotherapy targeting immune checkpoint has been considered a promising way to treat cancer. However, most recently studies suggest that the hyperprogressive disease occurred frequently during the therapy of using PD-1/PD-L1 antibody drugs and has become an urgent problem to be solved. In this review, we summarize the progress and potential reasons of hyperprogressive disease caused by PD-1/PD-L1 blockade, and further discuss its application based on the rational use of biomarkers for searching the benefit patients.
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