OBJECTIVE To establish a high-throughput qualitative analysis method for the Zhuang medicine Tongfeng Li'an Capsule use by Q-exactive orbitrap HRMS mass spectrometry. METHODS HPLC part on GOLD C₁₈ column(2.1 mm×100 mm,1.9 μm) and the gradient elution was performed with mobile phase consisting of 0.1% formic acid acetonitrile -0.1% formic acid aqueous solution. Flow velocity was 0.3 mL·min^-1, injection volume was 3 μL, column temperature was maintained at 35 ℃, mass spectrometry part used HESI ion source, Full MS/dd-MS² mode, ion scan range 100-1 500, vertex excitation for 2-8 s. RESULTS A total of 49 compounds were identified from Tongfeng Li'an Capsule by orbitrap HRMS, including 19 phenylpropanoids, 11 terpenes, 10 organic acids, 3 phenols, 2 anthraquinone, 2 alkaloids and vitamins, and 2 sugars and glycols. Among them, 46 compounds were identified for the first time from Tongfeng Li'an Capsule. CONCLUSION Data for high-resolution gather with orbitrap HRMS method was the first time comprehensive qualitative characterization conducted on Tongfeng Li'an Capsule, This provides a material basis and new scientific research basis and reference for its multi-component analysis application, quality standard improvement, and pharmacological research.

OBJECTIVE To prepare hydrogels containing antimicrobial peptide PMAP-24KK and evaluate antibacterial activity. METHODS The antimicrobial peptide PMAP-24KK was combined with sodium alginate, calcium carbonate, and gluconic acid-δ-lactone to form the PMAP-24KK hydrogel. Firstly, the formation time, swelling rate, moisture content, water retention rate, and release rate of PMAP-24KK hydrogel were analyzed. Then, the effect of PMAP-24KK hydrogel on the antibacterial activity in vitro, the sustained release, and the antibacterial barrier were determined by drug sensitivity test and skin wound healing in mice was analyzed. RESULTS The results showed that the PMAP-24KK hydrogel could form a gel state with network structure in about 2 min, and the swelling rate and moisture content reached equilibrium at 10 h, which were (158.83±3.26)% and (61.01±2.41)%, respectively. The water retention rate and release rate were about 55% and 81% after 24 h, respectively. The PMAP-24KK hydrogel showed the inhibitory effect on Staphylococcus aureus, Listeria monocytogenes, Salmonella choleraesuis, and Salmonella typhimurium. The sustained-release activity of PMAP-24KK hydrogel had no significant difference in 18 h, and gradually decreased after 18 h to 36 h without antibacterial activity. The PMAP-24KK hydrogel can effectively act as an antibacterial barrier and contribute to wound healing in mouse wound model. CONCLUSION Antimicrobial peptide PMAP-24KK hydrogel with good physicochemical properties and antibacterial activity is successfully prepared in this study, and it has good sustained-release and antibacterial barrier and promote wound healing, the study laid a foundation for further application research of antimicrobial peptide hydrogel.

OBJECTIVE To observe the effects of curcumin on the gastric tissue morphology and inflammatory microenvironment in mice with gastric epithelia dysplasia (GED), and to evaluate the preventive and therapeutic effects of curcumin on GED. METHODS Normal control group, model group, low, medium, and high dose groups of curcumin, and positive control group were set up. Except for the normal control group, all other groups were induced to establish GED animal models using a compound factor modeling method. After 8 weeks of modeling, the low, medium, and high dose groups of curcumin and the positive control group were respectively given curcumin at doses of 38, 75, 150 mg·kg^-1 and vitacoenzyme 350 mg/kg for intervention, continued for 8 weeks. At the end of the experiment, the gastric levels of pepsinogen PGⅠ, IFN-γ, IL-1β, IL-6, and the relative expression levels of p-JAK2, p-STAT3, Cyclin D1 in each experimental group were detected. HE staining and PCNA antibody immunohistochemistry were performed to observe the gastric mucosal tissue morphology and cell proliferation in each group. The pathological scores of GED and inflammatory cell infiltration were evaluated, and the proliferation index (PI) was calculated. RESULTS Compared with the normal control group, the serum concentration of PGⅠ in mice in the model group decreased, while the levels of IL-1β, IFN-γ, and IL-6 in gastric tissue increased (P<0.05). The scores of GED and gastric mucosal inflammatory cell infiltration, as well as the proliferation index (PI), all increased (P<0.01). Histopathological observations revealed changes such as epithelial dysplasia and inflammatory cell infiltration in the gastric mucosa, enhanced cell proliferation activity, and upregulation of p-JAK2, p-STAT3, and Cyclin D1 expression (P<0.05). Compared with the model group, the medium and high dose groups of curcumin showed an increase in serum PG1 concentration, a decrease in the inflammatory factors IFN-γ and IL-6 levels in gastric tissue (P<0.05), a decrease in GED and gastric mucosal inflammatory cell infiltration scores, as well as PI (P<0.05 or 0.01). The curcumin treatment alleviated gastric mucosal dysplasia and inflammatory cell infiltration, inhibited cell proliferation activity, and downregulated the expression of p-JAK2, p-STAT3, and Cyclin D1 (P<0.05). In the low dose group of curcumin, the expression of p-JAK2 protein was downregulated, and in the high dose group, IL-1β decreased (P<0.05). CONCLUSION Curcumin has a preventive and alleviating effect on the epithelial dysplasia of the gastric mucosa in mice, and can improve the tissue morphology of the gastric mucosa in GED mice. Its mechanism of action may be related to the downregulation of the JAK2/STAT3/Cyclin D1 pathway signaling, inhibiting excessive cell proliferation.

OBJECTIVE To investigate the effects of age, gender, body mass index (BMI), type of epilepsy, dosage and combined medication on the steady-state serum concentration of perampanel in children with epilepsy. METHODS A total of 95 serum samples from 4 to 14 years old children with epilepsy who were admitted to our hospital from 2019 to 2023 and took perampanel regularly were collected. The serum concentration was determined by high performance liquid chromatography. The influence of factors such as gender, BMI, dosage and combined medication on the concentration were analyzed. RESULTS The children aged 4.25-14 (7.25±3.99) years. The serum concentration of perampanel was 0.13-0.99(0.47±0.36)μg·mL^-1. There were no significant differences in the serum concentration and ratio of concentration dose (CDR) of perampanel among different age groups and gender groups (P>0.05). The CDRs of patients of 18.5≤BMI<24.0 group were significantly higher than those of BMI<18.5 group (t=-1.207, P<0.05). The combination of drug had no significant effects on the dosage, blood concentration and CDR of perampanel (P>0.05). The correlation between perampanel concentration and dose was poor (r=0.113). CONCLUSION In the course of using perampanel for the treatment of epilepsy in children, it is necessary to conduct therapeutic drug monitoring, so that the concentration can be controlled within the therapeutic range to ensure clinical efficacy and reduce the incidence of adverse reactions.

OBJECTIVE To establish a high performance liquid chromatography (HPLC) method for the detection of related substances in somatostatin for injection. METHODS The determination was performed on a C₁₈ column with mobile phases consisting of potassium dihydrogen phosphate solution and acetonitrile by gradient elution. The detection wavelength was set at 215 nm and the column temperature was maintained at 50 ℃. RESULTS The established method can effectively separate the main components and seven major degradation impurities. The peak area of somatostatin and 7 kinds of impurities had good linear relationships with the concentration (r≥0.999 1, n=8). Relative standard deviation (RSD) of precision, stability and repeatability tests of 7 kinds of impurities were all lower than 3.6%. The average recoveries of 7 kinds of impurities ranged from 100.0% to 104.4% (n=9). The impurity content determined by the established method is higher than that determined by the European Pharmacopoeia(EP) and Chinese Pharmacopoeia(Ch.P). CONCLUSION The method is simple, accurate and stable. It can control the impurities in somatostatin for injection and provide a basis for improving the standard of this drug.

Red yeast rice is a kind of traditional Chinese medicine(TCM) commonly used in China and all over the world in medicine, food additives, fermented food and other fields, but the research in this TCM is far from enough. Recently, the safety of red yeast rice health care product has aroused great concern around the world. This article reviews studies on the applied history, fermentation processing technology, material basis and quality control status of red yeast rice, aiming to clarify the factors that may lead to the risk of quality and safety of red yeast rice, and provide references for the safety quality control and risk prevention and control of red yeast and its products in China.

OBJECTIVE To establish a method for identifying the authenticity of Artemisiae Argyi Folium suitable for use in drug regulatory work. METHODS The near-infrared spectra of samples of Artemisiae Argyi Folium and counterfeit were determined, and the experimental data was processed using feature engineering related techniques, such as feature screening and feature derivation. The training set and test set were divided randomly, and the logistic regression model, a classic model in the field of machine learning, was trained in 2-class mode and evaluated with the training set data and the test set data used, respectively. RESULTS The discrimination accuracy of the samples in the test set was 97%, and the other evaluation indicators were also above 92% with the logistic regression model. In addition, the results of discrimination between genuine and counterfeit mixed samples were also relatively accurate. Compared with traditional chemometrics methods, the machine learning used in the study had higher discrimination accuracy. CONCLUSION The logistic regression model established in this study can achieve the authenticity identification of Artemisiae Argyi Folium, providing technical support for actual drug regulatory work.

OBJECTIVE To prepare t he immobilized α-L-rhamnosidase on SBA 15 mesoporous silica to promote the efficient conversion of epimedin C to icariin. METHODS SBA-15 was modified through amination and aldehydeylation, and the α-L-rhamnosidase was covalently coupled onto SBA-15. The immobilization conditions were optimized using the enzyme loading capacity and relative enzyme activity as evaluation index. X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), N₂ adsorption-desorption analysis, scanning electron microscopy (SEM) and transmission electron microscope (TEM) were used to characterize the physicochemical properties of immobilized α-L-rhamnosidase. Using epimedin C as substrate and free α-L-rhamnosidase as control, the optimal enzymatic hydrolysis conditions, enzymatic kinetic parameters and recyclability of the immobilized α-L-rhamnosidase were investigated. RESULTS The optimal pH was 3.5, the optimal temperature was 35 ℃, the optimal immobilization time was 4 h and the optimal α-L-rhamnosidase concentration was 8 mg·mL^-1. The immobilized α-L-rhamnosidase showed a well-retained activity of 198.6 μmol·h^-1·g^-1 as well as a high enzyme loading capacity of 256.9 mg·g^-1 support. The optimum hydrolysis conditions were as follows: pH 4.5, conversion temperature 50 ℃, substrate concentration 0.5 mg·mL^-1, and transformation time 12 h. The V_max and K_m of the immobilized α-L-rhamnosidase was 0.505 μg·min^-1 and 0.787 mmol·L^-1, respectively. After four cycles of reuse, the residual relative enzyme activity of the immobilized α-L-rhamnosidase was more than 65%, which showed good stability. CONCLUSION The immobilized α-L-rhamnosidase has a high enzyme loading capacity, strong enzyme activity and good reusability, which can be used for efficient conversion of epimedin C to icariin.

Non-alcoholic steatohepatitis (NASH), a severe subtype of non-alcoholic fatty liver disease (NAFLD), is emerging as a major health threat worldwide. However, due to its complex pathogenesis, there are currently no marketed drugs for NASH. The disease is not only involved in fat accumulation, but also accompanied by inflammation and fibrosis processes, in which inflammation plays an important role in the progression of NASH, long-term inflammatory response, can promote liver fibrosis and lipid homeostasis imbalance. Therefore, inhibiting inflammation is of great significance in improving NASH. This review systematically reviews the mechanism of action of inflammatory signaling pathways such as mitogen-activated protein kinase(MAPK), nuclear factor-κB(NF-κB), inactive rhomboid-like protein 2(iRhom2) and inflammasome in the development of NASH, and the current research status of related drugs such as Selonsertib, SHR0302 and fisetin, and further discusses the research progress of new targets for the treatment of NASH. It aims to provide new ideas for the research and development of drugs for NASH.

OBJECTIVE To investigate the attribution of berberine hydrochloride in the biological pharmaceutics classification system (BCS) and to determine its taxonomic properties. METHODS The solubility of berberine hydrochloride was investigated in pH 1.0-8.0 medium; its absorption parameters related to the rat duodenum, jejunum, ileum and colon were derived from in-situ intestinal perfusion model in vivo to determine its permeability. RESULTS The solubility in different pH dissolution media with the value of drug metering number (D₀) and combined with the pharmacopoeia regulations found that berberine hydrochloride belonged to the low solubility drugs. From the results of permeability experiments, it was found that the permeability coefficient P_eff(rat) of berberine hydrochloride in each intestinal segments was exceeded than 5.0×10^-5 cm·s^-1 in rats, and the conversion into human absorption F_a(human) was exceeded than 85%, therefore, it was determined to be the high permeability drug. CONCLUSION The combination of solubility and permeability test results proves that berberine hydrochloride is a low solubility and high permeability drug, which belongs to BCS class Ⅱ.