Latest ArticlesCorona virus disease 2019 (COVID-19) is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. At present, there is no specific antiviral drug for this virus, and the main clinical treatment is support and symptomatic treatment. Direct targeting the virus and the host targets are two strategies for the development of antiviral drugs. At present, the research and development of COVID-19 therapeutic drugs has made some progress on both approaches. Here we review potential anti-SARS-CoV-2 drugs to discuss the antiviral mechanisms and potential of these drugs from the perspectives of virus and host. The role of traditional Chinese medicine in the treatment of COVID-19 is discussed along with the prospects for drug treatment strategies of COVID-19.
The injectable recombinant protein of exendin-4 and human serum albumin (HSA), E2HSA, is a long-acting glucagon like-peptide-1 (GLP-1) receptor agonist, which is in clinical research stage now. This study aimed to evaluate the protective effects of E2HSA on mouse islet β cell function in vitro and in vivo. In vitro, the mouse insulinoma cells NIT-1 were used to assay the effects of E2HSA on cell viability and proliferation. Besides, the water soluble cholesterol was adopted to induce cell injury, and then the effects of E2HSA on cell viability and apoptosis, as well as the mechanism, were studied. In vivo, the alloxan-induced hyperglycemic mice were repeatedly administered with E2HSA by subcutaneous injection, and the blood glucose, serum insulin, and content of insulin in islets were measured. All animal experiments were carried out with approval of the Experimental Animal Welfare Ethics Committee of the Institute of Materia Medica (Chinese Academy of Medical Sciences and Peking Union Medical College). The results showed that E2HSA significantly increased the viability of NIT-1 cells and the amount of bromodeoxyuridine (BrdU) incorporated in cells. Besides, the water soluble cholesterol significantly decreased the cell viability and induced apoptosis of NIT-1 cells, but E2HSA significantly reversed the injury of NIT-1 cells. Nevertheless, E2HSA significantly increased the expression of pancreatic duodenal homeobox-1 (PDX-1) and protein kinase B (PKB) of NIT-1 cells after injured by water soluble cholesterol. Furthermore, repeated injections of E2HSA significantly reduced the fasting and non-fasting blood glucose, increased the serum insulin level and raised the insulin content in β cells of alloxan-induced hyperglycemic mice. In conclusion, E2HSA could promote proliferation of NIT-1 cells, inhibit the water soluble cholesterol induced injury and apoptosis, and increase the insulin content in serum and islets of alloxan-induced hyperglycemic mice, suggesting the protective effects on pancreatic islet β cell function.
Huang-Kui-Si-Wu Formula (HKSWF) can reduce the accumulation of uremic toxin p-cresyl sulfate (PCS) and its precursor p-cresol (PC) in a rat model of chronic kidney disease (CKD) and delay the progression of CKD. However, the mechanism by which HKSWF decreases PC accumulation is not clear. This study investigated the effect of HKSWF on PC production in intestinal microbes as well as its mechanism of action. After CKD model rats were given HKSWF by intragastric administration, feces were collected to analyze the gut bacterial composition by 16S rDNA sequencing technology. All procedures were approved by the Institutional Animal Care and Use Committee of the Nanjing University of Chinese Medicine. The results showed that HKSWF inhibited PC production without decreasing the abundance of harmful bacteria. HPLC-UV-FLD was used to detect p-cresol. An in vitro anaerobic culture system was used to study the effect and mechanism of action of HKSWF on PC production in gut bacteria. The results show that food-derived tyrosine (Tyr) could significantly promote PC production in intestinal bacteria, and HKSWF (4000, 400, 40 μg·mL-1) could dose-dependently inhibit PC production in gut bacteria in vitro. HKSWF inhibited bacterial PC synthesis by two pathways: it decreased the oxidation pathway from 82.83% to 38.87%, and increased the reductive pathway from 17.17% to 61.13%. This result suggests that HKSWF could inhibit PC production by switching tyrosine metabolism from an oxidative pathway to a reductive pathway. Secondly, HKSWF could directly inhibit the oxidative pathway of tyrosine and decrease the decomposition of PHA, thereby inhibiting PC production. These results suggest that HKSWF could inhibit the formation of harmful uremic toxins by modulating the metabolic pathway of PC in gut microbiota and thereby delaying CKD progression.
The rapid development of antibiotic resistance among bacterial pathogens has threatened to take humans back to the "pre-antibiotic era". The New Delhi metallo-β-lactamase (NDM-1) hydrolyzes nearly all β-lactam antibiotics including carbapenems. Bacterial strains carrying blaNDM-1 gene are termed "superbugs" and clinical inhibitors of NDM-1 have not yet been identified. Discovery of novel NDM-1 inhibitors is a challenging but rewarding research area. This review focuses on the structural characteristics and catalytic mechanisms of NDM-1, and comprehensively summarizes the development of NDM-1 inhibitors in order to facilitate the further development of NDM-1 inhibitors.
This study aims to synthesize fluorinated hyperbranched poly(amido amine)s for the delivery of influenza DNA vaccine. Hyperbranched poly(amido amine)s (HP) were synthesized by using Michael-type polyaddition and then fluorinated to obtain fluorinated polymers (F-HP). The target gene was amplified by designing specific primers to construct the eukaryotic expression plasmid of influenza viral PR8 nucleoprotein (NP) gene as DNA vaccines. Then the polyplexes (F-HP/NP) were prepared by the electrostatic interactions between polymers and plasmid. The results suggested that the molecular weight of HP was 59.7 kDa and polydispersity index (PDI) was 2.67. The fluorine content in F-HP was found to be 20% (w/w). Transmission electron microscopy (TEM) revealed that the polyplexes had spherical shapes with sizes around 100 nm (w/w 5-10) and decreased with increasing w/w ratios. F-HP polyplexes showed improved cell uptake, lysosomal escape and elevated expression levels of NP in vitro than polyplexes based on HP. Finally, the in-vivo immunization by F-HP/NP polyplexes triggered improved CD8+ T cell responses. This study suggests that fluorinated hyperbranched poly (amido amine)s represent one of the effective carriers for DNA vaccine delivery. The animal experiments were approved by the Experimental Animal Ethics Committee of Yangzhou University.
The paper aims to study and compare the effects of Scutellaria baicalensis leaves (SLE) and Scutellaria baicalensis tea (STE) water extracts on the lifespan of Drosophila melanogaster, and explore their anti-aging mechanism through metabolomics. Lifespan, food intake and fertility were measured after administering different doses of SLE and STE to a Drosophila natural aging model, and the metabolic profile of Drosophila was analyzed by metabolomics and multivariate statistical methods. The results showed that SLE and STE (1, 3 g·L-1) could significantly prolong the average lifespan, median life and maximum lifespan of male Drosophila, improve the fertility of Drosophila, and had no effect on the food intake. Through metabolomics technology, 14 differential metabolites related to aging were found, involving a total of five metabolic pathways. All differential metabolites were reversed after STE intervention, while 13 differential metabolites were reversed after SLE intervention. The results suggest that SLE and STE can delay aging of Drosophila, and the anti-aging mechanism is related to energy metabolism.
Chaetomium globosum WQ, an endophyte derived from Imperata cylindrical, can produce abundant cytochalasan compounds through solid state fermentation. Based on previous research and guided by 1H NMR spectrum and TLC, a new cytochalasan compound was isolated from the ethyl acetate extract of a solid culture of C. globosum WQ using silica gel column chromatography, gel filtration over Sephadex LH-20 and HPLC. The new compound was characterized as 20-iso-chaetoglobosin E (1) by a combination of spectroscopic (HR-MS, 1D and 2D NMR) analyses.
To identify major bioactive components and metabolites of Gandou decoction (GDD) in urine of normal and copper-laden rats, an integrative approach that ultra-performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MSE) coupled with xenometabolomics analytical platform was established. Mass spectral data information about retention time, accurate m/z and ionic strength of rat urine samples was performed under positive and negative ion modes. Unsupervised principal components analysis (PCA) and supervised orthogonal partial least-squared discriminant analysis (OPLS-DA) were used to reveal the differential ions. As a result, a total of 77 compounds including 45 prototypes and 32 metabolites in urine were detected. Results indicated that anthraquinones, alkaloids and tetracyclic triterpenoids and flavonoids were the main chemical components of GDD in rat urine; the main metabolic pathways of these compounds in rat urine mainly include hydroxyl, methylation, sulfating, glucuronidation, and so on. UPLC-QTOF-MSE coupled with xenometabolomics analytical platform is fast and efficient so that facilitates authentication of the material basis of Chinese herb compound in vivo, can also be used as an effective tool for ascertaining trace bioactive components in vivo. The animal experiments were approved by the Experimental Animal Ethics Committee of Anhui University of Chinese Medicine (No. 2019025).
Qualitative and relatively quantitative methods were used to study the quality of cultivated Epimedium sagittatum (Sieb. et Zucc.) Maxim., Epimedium myrianthum Stearn, and Epimedium pubescens Maxim by ultra high-performance liquid chromatography coupled with photo-diode array and quadrupole time-of-flight mass spectrometry (UHPLC-PDA-Q-TOF/MSE). Thirty-two compounds in cultivated and wild samples of E. sagittatum, E. myrianthum and E. pubescens were identified using UHPLC-Q-TOF/MSE combined with the UNIFI data analysis platform. Principal component analysis (PCA) was used to compare the cultivated and wild samples of these three species. The results show that the chemical compositions of cultivated samples were consistent with the corresponding wild samples. UHPLC-PDA was used to determine the relative content of 12 flavonoids as well as total flavonoids in all samples. The results show that the relative chemical content of these flavonoids in cultivated and wild samples is similar and the quality of cultivated Epimedium is more stable. These qualitative and relatively quantitative methods using UHPLC-PDA-Q-TOF/MSE combined with the UNIFI data analysis platform and PCA can be used to study the quality of cultivated Herba Epimedii. This research provides a scientific basis for the cultivation and rational development and utilization of Epimedium medicinal materials.
A collaborative inter-laboratory validation was carried out using a reporter gene assay to measure the bioactivity of anti-PD-1 monoclonal antibody, in order to study the applicability and transferability of the method. In this study, two collaborative schemes were designed to measure the precision, linearity and accuracy of the method. The results showed that the 95% confidence interval (CI) of the intra-assay precision was (1.72-16.89)%, inter-assay precision was (2.63-17.67)%, inter-laboratory precision was (9.00-14.26)%, all linear correlation coefficients were greater than 0.99, and the 95% CI for the accuracy at different potency levels was (91.83-104.40)% at 50%, (90.40-101.40)% at 75%, (94.71-105.60)% at 100%, (94.00-102.00)% at 125%, and (96.73-104.30)% at 150%. The collaborative validation results proved that the reporter gene assay for the bioactivity determination of anti-PD-1 monoclonal antibody has good precision, linearity and accuracy, and could be applied to the release and stability analysis of anti-PD-1 monoclonal antibodies in different laboratories.
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