Objective To investigate the mechanism of Xuezhikang Capsules (血脂康胶囊) in intervening coronary microvascular dysfunction (CMD) in ApoE^−/− mice based on non-targeted metabolomics. Methods After seven weeks of high-fat diet feeding, SPF-grade ApoE^−/− mice were injected with sodium laurate via tail vein to establish CMD model. The mice were then randomly divided into model group, atorvastatin (6 mg/kg) group, Xuezhikang low-, medium-, and high-dose (90, 180, 360 mg/kg) groups, another 12 C57BL/6J mice were selected as the control group. After eight weeks of drug intervention, the morphology and pathological changes of myocardial tissue and myocardial microvessels in mice were detected using hematoxylin-eosin (HE), Carstairs and Heidenhain staining. Cardiac functional injury was evaluated by echocardiography. Oil red O staining was used to evaluate the degree of lipid accumulation in the aorta. Lipid levels, myocardial injury and endothelial function-related indicators were detected by biochemical assays, ELISA, immunohistochemistry and immunofluorescence. The changes in fecal metabolites were analyzed using non-targeted metabolomics, and differential metabolites and significantly enriched metabolic pathways were identified. Western blotting was used to detect silent information regulator 1 (SIRT1), peroxisome proliferator activated receptor γ coactivator-1α (PGC-1α), p-p65 and p65 protein expressions in myocardial tissue. Results Compared with model group, Xuezhikang Capsules significantly reduced the levels of triglycerides, total cholesterol, low-density lipoprotein cholesterol, as well as the degree of myocardial and endothelial injury in serum of mice (P < 0.05, 0.01), and significantly improved the degree of microthrombus, myocardial ischemia and heart function decline in mice (P < 0.01). Non-targeted metabolomics identified 14 differentially expressed metabolites and 15 enriched pathways (P < 0.05). Western blotting results showed that compared with model group, Xuezhikang Capsules significantly up-regulated the protein expressions of SIRT1 and PGC-1α in myocardial tissue (P < 0.01), and down-regulated the protein expression of p-p65/p65 (P < 0.01). Conclusion Xuezhikang Capsules could regulate blood lipids, improve endothelial dysfunction and inflammatory response, thereby effectively improving cardiac function and reducing myocardial structural damage in CMD model mice. Its mechanism may be related to the regulation of arginine-proline-α-ketoglutarate metabolic axis and eNOS/SIRT1/PGC-1α signaling pathway.

Objective To investigate the existing states of Panax notoginseng total saponins in complex solution systems and elucidate the micellar association behavior of total saponins based on their ultrafiltration separation characteristics. Methods A total saponins solution of P. notoginseng was used as the research subject, with notoginsenoside R₁ and ginsenoside Rg₁, Rb₁, Rd selected as representative analytes. Ultrafiltration rejection rate, permeation rate, and micellar compositional ratio were employed as evaluation indices to analyze how key parameters—including inorganic salt concentration, temperature, and saponin concentration—affect saponin molecular states and ultrafiltration behavior. Results Owing to their amphiphilic structures, the saponins readily form micelles in aqueous solution, and their ultrafiltration performance is regulated by multiple environmental factors. Inorganic salts modulate micellar stability through ionic effects and salting-out actions: the divalent anion SO₄²⁻ disrupts hydration layers and strengthens hydrophobic interactions, thereby promoting micelle formation and precipitation, with salting-out intensity ranked as Na₂SO₄ > MgSO₄ > KCl. Monovalent salts such as KCl facilitate micellar association at low concentrations via charge shielding, whereas high concentrations intensify salting-out. Dammarane-type saponins, particularly Rb₁ and Rd, showed higher participation in salt-induced micelles, indicating a structure-driven association preference. Increasing temperature enhances molecular motion, weakens hydrophobic interactions and intermolecular hydrogen bonding within micelles, thereby promoting micelle dissociation, increasing permeation rates, and reducing rejection. Elevating saponin concentration strengthens hydrophobic and aggregative interactions among solute molecules, facilitating micelle assembly. By fitting the relationship between ultrafiltration rejection and membrane pore size at different solute concentrations, the molecular weight of micelles at 90% rejection and the internal compositional ratio of characteristic saponins were estimated. The results showed that at 10—20 mg/mL, micelles mainly consisted of diol-type saponins, but their association degree remained limited at low concentrations. At 30—60 mg/mL, the micellar molecular mass increased markedly, indicating that higher solute concentrations promote the formation of hybrid micelles. Conclusion This study elucidates the mechanisms by which pharmaceutical processing parameters regulate the micellar structure and ultrafiltration efficiency of P. notoginseng total saponins, providing theoretical and practical guidance for quality control and purification process optimization in saponin‑based traditional Chinese medicine formulations.

Objective To establish an objective endpoint criterion for the nine cycles of steaming and sun-drying in the processing of Shudihuɑng (Rehmanniae Radix Praeparata, RRP), to quantitatively characterize the dynamic changes in “morphology, color, and taste”, and to elucidate the correlation between chemical component transformations and the Maillard reaction. Methods Samples subjected to one through nine cycles of conventional steaming and wine-assisted steaming were prepared. An integrated analytical approach combining electronic tongue, electronic nose, electronic eye, mass spectrometry imaging, and infrared spectroscopy was employed to obtain quantitative parameters related to taste, odor, and chromaticity. These data were used to analyze the spatial distribution and dynamic variation of chemical constituents, as well as the migration patterns of characteristic functional groups. Results The electronic sensory data exhibited strong concordance with the results of manual sensory evaluation and demonstrated high discriminative capability among RRP samples subjected to varying cycles of re-hydration and re-drying. A pronounced shift in taste profile was observed at the third cycle of re-hydration and re-drying, identified as the critical inflection point for sensory deterioration. Concurrently, the color value decreased progressively with increasing reprocessing cycles—a trend consistent with the traditional quality benchmark “black as lacquer, sweet as honey”, wherein darker coloration correlates with superior quality. Volatile propane-type compounds were identified as key odor discriminants across treatment groups. Mass spectrometry imaging revealed that with increasing processing intensity, the levels of iridoid compounds, amino acids, and non-reducing sugars progressively declined, whereas those of reducing sugars and 5-hydroxymethylfurfural increased steadily. In contrast, phenethyl alcohol exhibited a triphasic trend—initially increasing, subsequently decreasing, and finally rising again. Fourier-transform infrared (FTIR) spectroscopy further demonstrated characteristic shifts in absorption peaks corresponding to sugar-derived hydroxyl groups and conjugated carbonyl moieties, consistent with hallmark spectral features of the Maillard reaction. Notably, organic acids present in the wine-steaming medium exerted a catalytic effect, advancing the onset of quality inflection points by one steaming cycle relative to the clear-steaming control group; However, no statistically significant difference in final product quality was observed between the two processing modalities. Conclusion The proposed multi-dimensional evaluation system objectively captures the evolutionary patterns of “morphology, color, and taste” throughout the nine-cycle steaming and sun-drying process of processed RRP. These findings provide a quantitative foundation for determining the optimal processing endpoint and offer a technical framework for quality control in the production of steamed and sun-dried traditional Chinese medicines.

Objective To identify the genome-wide family members of type III polyketide synthase (PKS III) and conduct bioinformatics analysis and expression profile analysis and clarify the relationship between their expression and the content of active components of Huzhang (Polygonum cuspidatum). Methods Based on the genome data of P. cuspidatum, the members of PKS III gene family were identified. Subsequently, the characteristics of these members were analyzed, including the physicochemical properties of their encoded proteins, secondary structure, phylogeny, and conserved motifs. Transcriptome data were further used to analyze their expression profiles, and the correlation between the expression levels of these PKS III genes and the active components was investigated. Results A total of 73 PKS III members were identified in the whole genome of P. cuspidatum, which were unevenly distributed on 20 chromosomes. Subcellular localization prediction indicated that most PKS III members were localized in the cytoplasm, while a small portion were localized on the plasma membrane. Phylogenetic analysis revealed that they were clustered into three major groups, and members within the same group shared identical conserved domains. Analysis of promoter cis-acting elements demonstrated that the PKS III genes contained various elements responsive to hormones, light, and growth and development. Expression profile analysis showed significant differences in the expression of PKS III genes among five tissues of roots and rhizomes of P. cuspidatum. Specifically, the expression levels of PKS32 and PKS42 were significantly higher than those of other genes in all tissues, with the highest expression detected in the rhizome pith. Correlation analysis indicated that PKS3, PKS8, PKS21, PKS44, PKS58, and PKS61 exhibited a significant positive correlation with the contents of polydatin and physcion, and PKS27, PKS56, and PKS69 showed a significant positive correlation with the contents of resveratrol and emodin; and PKS32 and PKS42 displayed a significant positive correlation with the content of physcion. Conclusion A total of 73 PKS III family members were identified, and the expression levels of some members correlated significantly with the contents of active components in P. cuspidatum roots and rhizomes. This study provides a foundation for subsequent research on the functions of PKS III genes and for elucidating the biosynthetic mechanisms of anthraquinones, stilbenes, and flavonoids in P. cuspidatum.

Objective Reactive oxygen species (ROS)-responsive co-loaded elemene (Ee) and chlorin e6 (Ce6) liposomes (Ee-Ce6-L) were prepared, characterization of their physicochemical properties, and evaluated for their inhibitory effects on bladder cancer 5637 cells. Methods The synergistic ratio of elemene and Ce6 (Ee + Ce6) was screened using the MTT assay. Ee-Ce6-L was prepared via the thin-film hydration method and characterized for morphology, particle size, encapsulation efficiency, drug loading capacity, stability, ROS generation capacity, and in vitro release rate. MTT assays evaluated the cytotoxicity of Ee-Ce6-L against 5637 cells. Annexin V-FITC/PI double staining was used to study the apoptotic effects of Ee-Ce6-L on cells. Fluorescence microscopy and a fluorometer were employed to examine its impact on ROS generation capacity and mitochondrial membrane potential (MMP). Western blotting analysis was conducted to investigate the expression of apoptosis pathway-related proteins. Results Ee + Ce6 exhibited synergistic effects across the 40:1 to 200:1 concentration range, with optimal synergy observed at 120:1; Ee-Ce6-L exhibited good stability and dispersibility. After irradiation with 660 nm laser, the particle size changed from (194.27 ± 0.20) nm to (390.97 ± 2.76) nm, and the ζ potential shifted from (−19.06 ± 0.07) mV to (−6.30 ± 0.34) mV. In vitro release experiments demonstrated that Ee-Ce6-L exhibits dual functions of sustained release and light-controlled drug release; the encapsulation efficiencies of elemene and Ce6 were (94.02 ± 0.38)% and (96.95 ± 0.70)%, respectively, while the drug loading capacities of Ee and Ce6 were (11.51 ± 0.46)% and (2.32 ± 0.01)%; Ee-Ce6-L exhibited strong singlet oxygen generation capacity; In vitro cell experiments demonstrated that Ee-Ce6-L promoted apoptosis in 5637 cells by increasing ROS production and reducing MMP, as well as by decreasing B-cell lymphoma-2 (Bcl-2) protein expression while increasing Bcl-2-associated X protein (Bax), cleaved poly ADP-ribose polymerase (cleaved PARP), and cleaved cystein-asparate protease-3 (cleaved Caspase-3) protein expression. Conclusion Ee-Ce6-L exhibits ROS-responsive release properties and synergistically inhibits 5637 cell proliferation and induces apoptosis through the combined effects of traditional Chinese medicine and phototherapy.

Objective To elucidate the dynamic changes in moisture, color, and index components during the “sweating” process of Danshen (Salviae Miltiorrhizae Radix et Rhizoma, SMRR) and preliminarily explore the correlation between moisture migration, color evolution, and changes in index components. Methods SMRR samples from Shandong underwent the “sweating” process, low-field nuclear magnetic resonance (LF-NMR) and magnetic resonance imaging (MRI) were employed to analyze moisture migration and distribution characteristics. The high-performance liquid chromatography (HPLC) and colorimeter were used to determine the contents of salvianolic acid B, tanshinone II_A, tanshinone I, cryptotanshinone and chromaticity values (L^*,a^*, b^*, and ΔE) of SMRR at different “sweating” degrees, respectively, followed by Pearson correlation analysis. Results The “sweating” process mainly involved free water loss, with relaxation peak gradually shifting leftward. MRI results indicated that moisture migrated from the core to the exterior of the roots. The cross-sectional color transitioned from the outer to inner layers, changing from yellowish-white to brown and finally to purplish-brown, with the L^* decreasing while a^*, b^*, and ΔE increasing continuously. The contents of salvianolic acid B and tanshinones initially increased and then decreased, reaching the highest values in lightly sweated SMRR (SD3, 47.38 mg/g) and moderately sweated SMRR (SD7, 4.62 mg/g) respectively. The content of salvianolic acid B exhibited a significant correlation with L^*, a^*, b^* and ΔE (P < 0.01). Conclusion By clarifying the characteristics of moisture migration and distribution during the “sweating” process of SMRR, this study scientifically validates the traditional view that “sweating promotes the outward diffusion of internal moisture in medicinal materials”. It reveals the dynamic changes in color and index components during “sweating” and preliminarily explores the role of moisture in driving the color deepening from the outside to the inside and changes in salvianolic acid B content, providing a reference for optimizing the “sweating” process of SMRR.

Objective To investigate the effect and mechanism of Yaobitong Capsules (腰痹通胶囊, YBT) on deep vein thrombosis (DVT). Methods Multi-scale evaluation of the effect of YBT was conducted using a rat lower limb deep vein ligation model, a zebrafish blood stasis model induced by phenylhydrazine, and an oxygen glucose deprivation (OGD)-induced human umbilical vein endothelial cell (HUVEC) injury model. In the rat lower limb deep vein ligation model, the ratio of thrombus weight to length and hematoxylin-eosin (HE) staining were used to evaluate the pathological changes of thrombus. Six coagulation parameters, plasma tissue factor (TF), endothelin-1 (ET-1), soluble vascular cell adhesion molecule-1 (sVCAM-1), interleukin-6 (IL-6), IL-1β, tumor necrosis factor-α (TNF-α), superoxide dismutase (SOD), malondialdehyde (MDA), hypoxia inducible factor-1α (HIF-1α) and other indicators were detected. In the zebrafish blood stasis model, the stasis of red blood cells and platelet aggregation were assessed via o-dianisidine staining and confocal microscopy, respectively. qRT-PCR was employed to measure the expressions of coagulation-related genes (fga, fgb, fgg, f2). In the OGD induced HUVEC cell injury model, qRT-PCR, Western blotting and immunofluorescence were used to detect the expressions of TF, VCAM-1, ET-1, HIF-1α, as well as the phosphorylation and nuclear translocation of nuclear factor-κB (NF-κB) p65. Results In the rat model of deep vein ligation of the lower limbs, YBT could reduce the ratio of thrombus weight to length, improve histopathological changes (P < 0.05), prolong activated partial thromboplastin time (APTT) (P < 0.001), reduce fibrinogen (FIB), D-dimer, fibrinogen and fibrin degradation products (FDP), TF, ET-1, sVCAM-1, IL-6, IL-1β, TNF -α, MDA and HIF-1α levels (P < 0.01, 0.001), and increase SOD activity (P < 0.05, 0.01). In the zebrafish blood stasis model, YBT could significantly increase cardiac erythrocyte staining intensity and circulating platelet number (P < 0.001), and down-regulate the expressions of coagulation related genes (P < 0.01, 0.001). In the OGD induced HUVEC cell injury model, YBT could down-regulate the mRNA expressions of TF, VCAM-1, ET-1 and HIF-1α (P < 0.05, 0.01, 0.001), down-regulate the protein expressions of TF and HIF-1α (P < 0.05, 0.01, 0.001), inhibit the phosphorylation and nuclear translocation of NF-κB p65 (P < 0.05, 0.01). Conclusion YBT may effectively inhibit DVT by inhibiting HIF-1α/NF-κB p65/TF axis (down-regulating HIF-1α expression, inhibiting NF-κB p65 phosphorylation and nuclear translocation, thereby reducing TF overexpression), alleviating the hypoxia inflammation cascade, protecting endothelial function, and improving hypercoagulability.

Objective To investigate the chemical constituents of the taproots of Brassica rapa (Qiamagu) and evaluate their anti-inflammatory activity. Methods The chemical constituents were systematically isolated and purified using silica gel, ODS, Sephadex LH-20 column chromatography, and preparative HPLC. Their structures were elucidated by comprehensive spectroscopic analyses, including NMR, MS, and UV. The cytotoxicity of the isolates against RAW264.7 murine macrophages was assessed using the CCK-8 assay. The in vitro anti-inflammatory activity was evaluated via the Griess method. Results Twenty-five compounds were isolated from the 70% ethanol extract of B. rapa taproots and identified as 2-C-β-D-glucosyl-indole-3-acetonitrile (1), sinapic acid (2), p-coumaric acid (3), ferulic acid (4), methyl sinapate (5), methyl 4-hydroxycinnamate (6), trans-4-methoxycinnamic acid (7), dimethyl feruloyl malate (8), sinapoyl dimethyl malate (9), p-hydroxybenzaldehyde (10), phenylacetic acid (11), phenylethane-1, 2-diol (12), 3-phenylpropanamide (13), phenylethyl-β-D-glucoside (14), 4-(3-hydroxypropyl) phenyl β-D-glucopyranoside (15), idaeusinol B (16), syringaresinol-4-O-β-D-glucoside (17), equiselignan A (18), phaseic acid (19), abscisic acid (20), roseoside (21), bergapten (22), methylthioadenosine (23), 5-hydroxymethylfurfural (24), and rabdosia acid B (25). The CCK-8 assay demonstrated the cytotoxicity of compounds 16, 22, and 25. To evaluate the anti-inflammatory activity in vitro, the Griess method was employed. The results demonstrated that all tested compounds exhibited varying degrees of inhibitory activity. Conclusion Compound 1 is an indole glucosinolate; compounds 2—9 and 16—18 are phenylpropanoids, compounds 10—12, 14 and 15 are benzene ring derivatives, and compounds 13 and 23 are nitrogen-containing compounds. Among them, compounds 1, 6—9, 13, 15, 16, 18, 19, and 23 are isolated from B. rapa for the first time. In the anti-inflammatory assay, with compounds 8 and 9 demonstrating significant effects, yielding IC₅₀ values of 6.95 and 6.46 μmol/L.

Objective To investigate the chemical constituents of Urtica cannabina and their hypoglycemic activity in vitro. Methods The compounds were isolated and purified by column chromatography of HPD-600 macroporous resin, silica gel, preparative TLC, and semi-preparative HPLC. Their structures were elucidated by physicochemical properties and spectral analyses. The hypoglycemic activity was evaluated in vitro through their inhibitory effects on α-glucosidase, sucrase, and maltase. Results Twenty compounds were isolated and identified from the 70% ethanol extract of U. cannabina, including cis-p-hydroxycinnamic acid (1), trans-p-hydroxycinnamic acid (2), dimethyl glansreginate (3), kaempferol 3-O-β-D-glucopyranoside (4), caffeic acid (5), chlorogenic acid methyl ester (6), 4-O-feruloylquinic methyl ester (7), hydroxycinnamic acid methyl ester (8), (E)-p-coumaroyl dimethyl malate (9), fraxidin (10), trans-caffeic acid methyl ester (11), trans-caffeic acid ethyl ester (12), 3,4-dihydroxy-acetophenone (13), 4-caffeoylquinic acid (14), 3-O-p-coumaroyl quinic acid methyl ester (15), 3-O-feruloylquinic methyl ester (16), hydroxybenzoic acid (17), phaseic acid (18), 5-O-p-coumaroylquinic methyl ester (19), 5-O-feruloylquinic methyl ester (20). The in vitro activity screening revealed that compounds 5 and 7 exhibited significant inhibitory activity against α-glucosidase, while compounds 5, 6, 11, 12 and 14 displayed considerable inhibitory effects on both sucrase and maltase. Conclusion Compounds 1, 2, 5—12, and 14—20 are phenolic acids, compound 4 is a flavonoid, and compound 13 is a ketophenol. Among these, compounds 3, 7, 9, 10, 13, 15, 16, and 18—20 were isolated from U. cannabina for the first time. Compound 5 demonstrated notable inhibitory activity against all three enzymes, suggesting that it may serve as the core pharmacophoric structure for the hypoglycemic effect. Structure-activity relationship analysis indicated that the catechol structure and the caffeic acid esterification motif collectively constitute the key structural basis for the glycosidase inhibitory activity of these phenolic acids.

Objective To investigate the different effects of carboxymethyl starch sodium (CMS) and polyvinylpyrrolidone (PVPP) on the structure, free surface energy, and key direct compression properties of composite particles produced by co-spray drying based on traditional Chinese medicines (TCM) extracts. Methods This study selected extracts of Fuling (Poria), Danggui (Angelicae Sinensis Radix), Huangqi (Astragali Radix), Danshen (Salviae Miltiorrhizae Radix et Rhizoma), and Jinyinhua (Lonicerae Japonicae Flos) (PC、AS、AM、SM、LJ) as model drugs, and CMS and PVPP as modifiers. The composite particles of TCM extracts (CP-PC/AS/AM/SM/LJ-CMS and CP-PC/AS/AM/SM/LJ-PVPP) were prepared via co-spray drying. The properties of the co-spray dring liquid, and structure, free surface energy and direct compression properties of composite particles were comprehensively characterized. The different effects of CMS and PVPP on these properties were analyzed by statistical analysis. Results The application of different modifiers led to differential variations in the properties of the co-spray dring liquid, as well as in the structural characteristics, free surface energy, and direct compression properties of the composite particles. Compared to PVPP, co-spray dried liquid containing CMS exhibited increased solid content and viscosity, and lower surface tension and hydrodynamic size (except for CP-SM/LJ-CMS); All composite particles exhibited spherical structures, and those containing CMS showed smoother surfaces and larger particle size than those containing PVPP; The composite particles containing CMS brightness values (except for CP-AM-CMS), hardness (except for CP-AS/AM-CMS), elasticity, and rebound property (except for CP-AS/AM-CMS) were lower; The cohesion (except for CP-PC/LJ-CMS), cohesion work (except for CP-SM/LJ-CMS), free surface energy (except for CP-SM/LJ-CMS), and polarity index (except for CP-SM -CMS) of composite particles containing CMS were relatively high; The Carr’s index, Hausner ratio, angle of repose (except for CP-SM-CMS), and disintegration time (except for CP-LJ-CMS) of composite particles containing CMS were all smaller, while composite particles containing PVPP demonstrated higher tensile strength. Conclusion The properties of TCM extract co-spray drying solutions, structures, free surface energy, and direct compression performance of composite particles containing CMS and PVPP were exhibited different effects. These findings provide valuable insights for advancing co-spray drying technology in TCM extracts and for preparing composite particles suitable for direct powder compression.