OBJECTIVE To establish the fingerprints of 50 batches of Arnebiae Radix and the methods for determination of the contents of six components. METHODS A high performance liquid chromatographic (HPLC) method was used for the determination of 50 batches of Arnebiae Radix on an Agilent 5 TC-C₁₈(2) column, with acetonitrile-0.05% formic acid aqueous solution as the mobile phase, gradient elution at a flow rate of 1 mL·min^-1, detection wavelength of 275 nm, and column temperature of 30 ℃. The contents of six naphthoquinone components, i.e., alkannin, acetylshikonin, deoxyshikonin, β-acetoxyisovalerylshikonin, isobutyryl alkannin, and β,β'-dimethylacrylalkannin were determined. The fingerprints of the herbs were established by HPLC fingerprinting combined with the “Chinese Medicine Chromatographic Fingerprint Similarity Evaluation System (Version 2012A)” to evaluate the similarity and confirm the common peaks. RESULTS The methodological validation results showed that the peak areas of the six components had good linear relationships in the corresponding concentration ranges, and the contents of the six components ranged from 0.006%-0.237%, 0.009%-1.759%, 0.001%-0.129%, 0.002%-0.625%, 0.011%-0.609%, and 0.016%-1.712%, respectively. The HPLC fingerprints of Arnebiae Radix were established, and a total of nine common peaks were calibrated. The similarity fitting was performed by using the TCM fingerprinting software, and it was found that the similarity of the 50 batches of Arnebiae Radix varied greatly. CONCLUSION The HPLC fingerprint of Arnebiae Radix established in this study and the method of simultaneous determination of the contents of six components are simple, stable, accurate, reliable, and reproducible, which can provide a basis for the quality study of Arnebiae Radix.

OBJECTIVE To establish critical quality attributes analysis method for recombinant human collagen Ⅲ. METHODS The recombinant human collagen Ⅲ molecular weight (MW) distribution was determined by matrix-assisted laser desorption ionization time of flight mass spectrometry (MALDI-TOF MS) and size exclusion chromatography with multi-angle light scattering (SEC-MALS). Capillary electrophoresis-sodium dodecyl sulfate (CE-SDS) and size exclusion high performance liquid chromatography (SE-HPLC) were used for purity analysis. Ion exchange chromatography and capillary zone electrophoresis (CZE) were used to separate and analyze charge isomers. The “double” enzyme digestion peptide mapping method was used for identification and sequence coverage analysis. RESULTS The recombinant human collagen Ⅲ MW distribution measured by MALDI-TOF was 45.01×10³. The MW of monomer recombinant human collagen Ⅲ determined by SEC-MALS was 45.17×10³ (±0.226%). CE-SDS analysis showed that the purity of recombinant human collagen Ⅲ was 98.77% and that of other ingredients was 1.23%. The SE-HPLC purity was 98.07%, and that of other component was 1.93% (dimer). A total of 14 charge isomers were identified through strong cation exchange, and the acidic peak was 52.08%, the main peak was 26.22%, and the basic peak was 21.70%. Eight charge isomers were identified by CZE, including 52.10% acidic peak, 25.27% main peak, and 22.63% basic peak. Two identification methods for charge isomers have consistent distribution patterns. The “double” enzyme digestion peptide mapping method was used for identification and sequence coverage analysis, achieving 100% coverage of the recombinant human collagen Ⅲ sequence. CONCLUSION A series of critical quality attributes analysis methods for recombinant human collagen Ⅲ have been established. These methods provide a reference basis for the quality control of recombinant human collagen Ⅲ in China.

OBJECTIVE To analyze the influencing factors of tacrolimus (FK506) blood concentration non-attainment in renal transplant patients and construct a risk prediction column-line diagram model. METHODS Two hundred patients admitted to the hospital from June 2020 to June 2023 who were treated with FK506 after renal transplantation and whose blood concentration was monitored for 30 d were selected for the study, and according to the monitoring results, they were categorized into 126 cases in the group of meeting the standard (5-15 μg·L^-1) and 74 cases in the group of failing to meet the standard (<5 μg·L^-1 or>15 μg·L^-1), and the clinical data were collected, and independent risk factors for failing to meet the standard of FK506 were screened and fit into a predictive model by single-factor and multifactorial logistic regression analysis. Clinical data of the two groups were collected, and the independent risk factors for FK506 blood concentration non-compliance were screened by single-factor and multifactor logistic regression analyses, according to which, a prediction model for the risk of FK506 blood concentration non-compliance was constructed with a line graph and tested for goodness-of-fit. RESULTS Of the 1 200 FK506 concentration monitoring sessions in 200 patients within 30 d after surgery, the number of sessions in which the target concentration of 5-15 μg·L^-1 was reached was 756, with an attainment rate of 63.0%. A total of 126 patients reached the target concentration (target group), and 74 patients did not reach the target concentration (non-target group). The proportion of patients with age >60 years, male, intravenous, fasting blood glucose (FPG) >7 mmol·L^-1, total bilirubin (TB) >20 μmol·L^-1, white blood cell count (WBC)≤4×10⁹·L^-1, and blood creatinine (Cr) >133 μmol·L^-1 was higher in the non-attainment group than in the attainment group, and the difference was statistically significant (P<0.05). Multifactorial logistic regression analysis was performed, and the results showed that age >60 years, male, FPG>7 mmol·L^-1, TB>20 μmol·L^-1, and Cr>133 μmol·L^-1 were independent risk factors for substandard FK506 blood concentration in renal transplant patients (all P<0.05). The AUC of the constructed column-line graph model reached 0.859 (0.795-0.924), the model calibration curve validation C-index was 0.836, and the H-L deviation test χ²=4.203, P=0.516, the calibration curve was basically the same as the ideal curve trend, with a good degree of precision and differentiation. DCA analysis showed that the column-line graph prediction model displayed a large range of threshold probabilities (0.05 to 0.95), which corresponded to the largest area of the red curve to the gray curve and the horizontal axis, indicating a better clinical utility value of the model. CONCLUSION Age >60 years, male, FPG >7 mmol·L^-1, TB >20 μmol·L^-1, and Cr >133 μmol·L^-1 are the risk factors for substandard FK506 blood concentration in renal transplantation patients, and the column-line graph model constructed accordingly can effectively predict the degree of risk for substandard FK506 blood concentration in renal transplantation patients.

Hippophae rhamnoides L. is a high-quality medicinal and edible plant with rich nutritional values and a wide range of biological activities. It has been used to improve hyperglycemia, hyperlipidemia, liver injury and prevent cardiovascular diseases. Sea buckthorn polysaccharides (SBPs) are one of the most important bioactive components of Hippophae rhamnoides L.. The preperation methods of SBPs include hot water extraction, ultrasonic-assisted extraction, microwave-assisted extraction, and flash extraction. Different preperation methods lead to different configurations and biological activities of SBPs. Furthermore, these biological activities are related to the chemical structure of SBPs, including the relative molecular weight, monosaccharide composition, glycosidic bond and three-dimensional structure. Modern pharmacological studies have demonstrated that SBPs possess various activities, including hepatoprotective, anti-inflammatory, immunomodulatory, anti-tumor, antioxidant activity, as well as the regulation of blood sugar and lipid metabolism disorder, which will exhibit excellent development value in functional food and medicament. However, few studies on the structure-function relationship of SBPs have been reported. In this paper, the preperation methods, structure characterization, pharmacological activities and the utilization of SBPs were systematically reviewed, the structure-activity relationship and application prospect were discussed, which will provide a theoretical basis for a further research and development and utilization of SBPs.

Central nervous system (CNS) diseases are a serious threat to human health. However, due to the existence of blood-brain barrier (BBB), there is a lack of effective technology to deliver drugs to the brain, which seriously affects the success rate of drug development related to CNS diseases, resulting in treatment results that are often unsatisfactory. Therefore, a new technology is urgently needed to solve the above problems. Brain targeted peptide-drug conjugates, which consist of a brain targeted peptide, a linker, and a payload, have become a promising CNS drug by enabling bioactive molecules to cross the BBB and reach the brain parenchyma by using biologically relevant endogenous transport mechanisms. In this review, the types and characteristics of brain targeting peptides, linkers, and payloads are briefly introduced, and some common brain targeting peptide-drug conjugates are listed, as well as the challenges faced by such drugs and the improvement methods, in order to provide ideas for the design and development of drugs for CNS diseases.

OBJECTIVE To systematically study the micro-characteristics and microscopic characteristics of 9 commercially available Epimedium leaves, summarize more exclusive and practical features and provide reference for effective identification of Epimedii Folium on market. METHODS Using the character identification, micro-character identification, microscopic identification and combining with the technique of depth synthesis, high definition feature images of 9 species of Epimedium leaves were obtained. Some of the feature maps were extracted digitally and analyzed by SPSS 26.0 software. RESULTS The micro-characteristics of petiole hair, leaf margin spines, nipple and hairs on lower surface, parenchyma number on the base of leaf main vein transverse section, cuticle on the surface of leaf, as well as the microscopical characters of upper epidermal cell wave depth, non-glandular hair and nipple surface morphology, all of that can be regarded as specific features of 9 species of Epimedium leaves in classification and identification. There was statistically significant difference in the angle of thorns at the edge of leaves, the proportion of wave depth in upper epidermal cells and the density of nipple among all samples (P<0.05). CONCLUSION Nine kinds of Epimedium leaves could be distinguished through the micro-characteristics and micro-identification methods. The quantitative analysis and statistical analysis of micro-property will make up for the deficiency of traditional experience identification by subjective factors. The results of this study will provide a reference for the circulation, inspection, clinical medication and standard drafting and so on.

OBJECTIVE To explore the mechanism of Atractylodes macrocephala polysaccharide (AMP) in improving chronic unpredictable mild stress (CUMS) depression in mice by integrating metabolomics technology and gut microbiota analysis. METHODS CUMS depression mouse model was established. Low, medium and high dose AMP treatment were given at 0.062 5, 0.125, 0.250 g·kg^-1, respectively, fluoxetine was given at the dosage of 0.015 g·kg^-1, control group and model group were given 0.9% saline solution, and all groups were given at 5 mL·kg^-1·d^-1 of drug. The content of 5-hydroxytryptamine(5-HT) in the brain of mice was determined by enzyme-linked immunosorbent assay (ELISA), and the CUMS depression model was tested by combining sucrose preference test (SPT) results. The 16S rDNA amplicon sequencing technology was used to analyze the gut microbiota in the feces of mice in each group. LC-MS technology was used to perform non-targeted metabolomics determination of mouse serum. RESULTS Compared with the control group, the sucrose preference rate of CUMS model mice was significantly lower, and the content of 5-HT in the brain of mice was significantly reduced (P<0.01), indicating that the CUMS depression model was successfully established. After AMP treatment, the sucrose preference rate and 5-HT content of mice in each group increased (P<0.01), the gut microbiota of CUMS mice had a regulatory effect, serum metabolites were significantly changed, and 58 metabolites were significantly adjusted. Spearman correlation analysis showed that the changes in gut microbiota were significantly associated with the changes in metabolite levels. CONCLUSION AMP exerts intervention effects on CUMS depression model mice by regulating the stability of gut microbiota, upregulating the F-B ratio, and thereby regulating metabolic pathways.

OBJECTIVE To prepare a “sandwich” oral film (composed ofthe backing layer, sustained release layer, and adhesion layer) containing triamcinolone acetonide for the treatment of oral ulcers. METHODS Triamcinolone acetonide oral film was prepared by a tape casting process using ethyl cellulose (EC), hydroxypropyl methylcellulose (HPMC), and polyacrylic acid (PAA) as carrier materials. Taking the appearance, thickness, uniformity, adhesion, and mechanical strength of the film as indicators, the formulation of the backing layer, sustained release layer, and adhesion layer was optimized by a single factor study. The film's physicochemical properties and drug release in vitro were compared with the commercially available formulation Taisho^®. RESULTS The drug loading of the resulting triamcinolone acetonide three-layer oral film was 96.0%, and the film had good uniformity, mechanical strength, and adhesion. The designed oral film had a release curve similarity factor f₂ of 54.25 when compared to the commercially available formulation of Taisho^®. CONCLUSION The quality of triamcinolone acetonide oral film prepared by the tape casting process is consistent with that of Taisho^®. Moreover, the technology of this film is simple and feasible, with the potential for industrial conversion.

OBJECTIVE To prepare tetrahydropalmatine gel emulsion with Bletilla striata polysaccharide, and investigate its stability and dissolution characteristics in vitro. METHODS The nascent soap method combined with high pressure homogenization method were used to prepare tetrahydropalmatine gel emulsion. Using the particle size and polydispersity index (PDI) as evaluation indexes, the single factor response surface method was used to screen the optimal prescription, and the biological properties of tetrahydropalmatine gel emulsion were investigated. RESULTS The optimum formula was m(Bletilla striata polysaccharide)-m(konjac gum)=50∶1, triethanolamine mass fraction of 0.8%, stearic acid mass fraction of 2.0%. The gel emulsion of tetrahydropalmatine was milky white, fine, uniform and glossy, and had good moisturizing, coating and stability properties. The average particle size and PDI value were about (1.56±0.04) μm, (0.434±0.03), and the cumulative transmittance of the gel emulsion for 24 h was (915.23±85.55) μg·cm^-2. CONCLUSION The tetrahydropalmatine gel emulsion prepared in this experiment has good appearance, moisture retention, coating and stability, and good transdermal absorption rate. The research results can provide reference for the further development and utilization of tetrahydropalmatine.

OBJECTIVE To analyze the chemical components of Longzuan Tongbi Granules, a classical prescription of Zhuang medicine by liquid chromatography-tandem mass spectrometry (LC-MS/MS). METHODS The MS/MS data were collected in positive and negative ion mode after gradient elution of the test solution using an ACQUITY UPLC HSS T3 column (2.1 mm×100 mm, 1.8 μm) and a mobile phase system consisting of 0.1% formic acid water (A)-0.1% formic acid acetonitrile (B). RESULTS A total of 113 compounds, including 64 alkaloids, 20 flavonoids, 12 organic acids, 8 coumarins, 5 lignans and 4 others, were identified by high-resolution mass spectrometry data analysis, reference substance and database comparison, while referring to the mass fragmentation patterns of relevant components reported in the literature, and of which 109 secondary metabolites were attributed for recognition. CONCLUSION The material basis of Longzuan Tongbi Granules is rich, represented by alkaloids, and Toddalia asiatica is the important “main drug”. This information can provide a scientific basis for the pharmacodynamic mechanism study and rational clinical use of this formula.