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  • Ting-liang LIU, Tian-tian WANG, Wen-lin ZHENG, Jia-zheng WU, Shi-yun DU, Zhen-dan HE, Yan WU
    Acta Pharmaceutica Sinica. 2026, 61(5): 1769-1776.

    Thirteen compounds were isolated from the twigs and leaves of Meiogyne hainanensis (Merr.) N. T. Ban by silica gel column chromatography, sephadex LH-20, and preparative HPLC. Their structures were respectively determined as chienhainanin N (1), (S)-15, 16-didehydrocoriolic acid methyl ester (2), 13-hydroxy-9Z, 11E, 15E-octadecatrienoic acid (3), (S)-coriolic acid (4), 13-oxo-(9Z, 11E)-octadecadienic acid (5), 13-oxo-(9E, 11E)-octadecadienic acid (6), 9-oxo-(10E, 12Z)-octadecadienic acid (7), 9-oxo-(10E, 12E)-octadecadienic acid (8), α-tocopherol (9), vitamin E quinone (10), α-tocospiro A (11), 17c-ethoxypheaophorbide A (12), mustakone (13) by spectral data analysis. Among them, compound 1 is a new compound, compounds 2, 3, 5-8, 10-12 are isolated from Annonaceae plants for the first time, and compounds 4, 9 and 13 are isolated from the genus Meiogyne for the first time. Their antimicrobial activities were evaluated by the broth microdilution method. Compounds 2, 3, 5-7 showed weak antimicrobial effect against MRSA with MIC values from 64 to128 μg·mL-1, respectively. Compound 13 showed weak antimicrobial effects against Cryptococcus neoformans with the MIC value of 128 μg·mL-1.

  • Ya-ru QIN, Yu-yao LI, Yang-rui-xuan LIU, Yuan-yuan LI, Yan NI, Zhen-yu LI
    Acta Pharmaceutica Sinica. 2026, 61(5): 1777-1786.

    This study investigated cultivated Astragalus from three major production regions-Shanxi, Neimenggu, and Gansu-using a pseudo-targeted metabolomics approach based on UHPLC-Q-TRAP-MS. After systematic optimization of collision energy (CE) and declustering potential (DP) parameters, relative quantification of 109 compounds in 16 batches was performed. Combined with multivariate statistical analysis, chemical differences among samples from different origins were assessed. The results revealed certain differences in the overall chemical composition among the three origins. Approximately 60% of the detected components showed no significant content differences across regions, while the differential compounds-primarily secondary metabolites-were mainly observed between Shanxi Astragalus and samples from Neimenggu and Gansu. Compared to Neimenggu and Gansu samples, Shanxi Astragalus was characterized by higher contents of acylated flavonoid glycosides and flavonoid glycosides, along with lower levels of flavonoid aglycones. Thus, the flavonoid glycoside/aglycone ratio can serve as a reliable indicator to distinguish Shanxi Astragalus. These characteristic differences may serve as potential markers for geographical traceability and authenticity evaluation of cultivated Astragalus, providing a scientific basis for constructing a quality assessment system.

  • Tian-tian ZUO, Chang LIAO, Jing LIU, Hong-yu JIN, Xian-long CHENG, Feng WEI, Feng-guo XU, Yong-qiang LIN
    Acta Pharmaceutica Sinica. 2026, 61(5): 1787-1792.

    To investigate the oral bioaccessible contents of lead (Pb) and arsenic (As) in the animal-derived traditional Chinese medicine earthworm and to assess the associated health risks, the contents of Pb and As in earthworm were determined by inductively coupled plasma mass spectrometry (ICP-MS). An in vitro digestion/intestinal organ-on-a-chip model suitable for the matrix of traditional Chinese medicine was established for the first time to simulate the gastrointestinal digestion and absorption processes of Pb and As from earthworm, and their bioaccessible contents was determined. The health risks were assessed using the hazard index (HI) method based on both the total contents and the bioavailable contents of the heavy metals. The results indicated that the total contents of Pb and As in 9 batches of earthworm ranged from 0.16-12.10 and 0.15-1.20 mg·kg-1, respectively. After transported by the intestinal organ-on-a-chip, the bioavailable concentrations ranged from 0.02-0.92 mg·kg-1 for Pb and 0.01-0.09 mg·kg-1 for As. The risk assessment based on total contents revealed that the HI for Pb and As in multiple batches exceeded 1, indicating an unacceptable risk. In contrast, the HI values based on bioavailable concentrations were all below 1, suggesting an acceptable risk. The in vitro digestion/intestinal organ-on-a-chip model established in this study for the first time can more accurately reflect the actual exposure risk of heavy metals in traditional Chinese medicine following oral intake, providing a methodological foundation for the safety evaluation and standard setting of traditional Chinese medicines.

  • Li-fang GUAN, Sai-yu LI, Yi-jing DONG, Ming-zhe ZHANG, Qian ZHANG, Hua-rong XU, Qing LI, Yi-wen ZHANG
    Acta Pharmaceutica Sinica. 2026, 61(5): 1793-1803.

    This study aims to investigate the potential active components and mechanism of action of "Ginseng-Schisandra" herb pair in the treatment of hepatocellular carcinoma (HCC). The blood-entering components of the "Ginseng-Schisandra" herb pair were identified using high pressure liquid chromatography-quadrupole-time of flight mass spectrometry (HPLC-QTOF/MS). The alterations of bile acid (BA) levels in the plasma, liver, and feces of HCC rats following intervention with the "Ginseng-Schisandra" herb pair were comprehensively analyzed by LC-MS. The biomarkers of HCC were screened by integrating orthogonal partial least squares-discriminant analysis (OPLS-DA) and Student's t-test. Finally, the key pharmacodynamic substances of "Ginseng-Schisandra" herb pair in the treatment of HCC were identified based on correlation analysis and further verified through molecular docking. The animal experiments were approved by the Ethics Committee of Shenyang Pharmaceutical University (approval No.: CSE202106002). As a result, 22 blood-entering prototype components of the "Ginseng-Schisandra" herb pair were identified. This study demonstrated that the "Ginseng-Schisandra" herb pair markedly restored dysregulated BA metabolism in the plasma, liver, and feces of HCC rats, and 9 bile acids were successfully characterized as HCC biomarkers. Correlation analysis and molecular docking demonstrated that ginsenoside Rb1 and schisandrin A, which exhibited strong binding affinities to key BA regulatory proteins [farnesoid X receptor (FXR), cytochrome P450 family 7 subfamily A member 1 (CYP7A1), bile salt export pump (BSEP), and organic anion transporting polypeptide 1B1 (OATP1B1)], were crucial pharmacodynamic constituents of the "Ginseng-Schisandra" herb pair in the treatment of HCC. Collectively, this study established a scientific foundation for the clinical application of the "Ginseng-Schisandra" herb pair in the treatment of HCC.

  • Yu HAN, Yue-yue LUO, Sheng-ru HUANG, Shu-lan SU, Pei LIU, Er-xin SHANG, Yong-qi LIU, Jin-ao DUAN
    Acta Pharmaceutica Sinica. 2026, 61(5): 1804-1818.

    Ultra-high performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UPLC-QTOF-MS/MS) was used to analyze and identify the chemical components of Dabufei Decoction (DBFT). Combined with network pharmacology, the mechanism of action of DBFT in the stable phase of chronic obstructive pulmonary disease (COPD) was explored. Under positive and negative ion modes, the chemical components of DBFT were identified based on information such as the accurate molecular weight of compounds, MS/MS fragmentation rules, and literature-reported data. Then, combined with the TCMSP database and literature mining, the active components and action targets of DBFT were obtained. Targets related to the stable phase of COPD were retrieved from the OMIM and Gene Cards databases. The overlapping targets between drug targets and disease targets were screened out, imported into the STRING database and Cytoscape 3.10.3 to construct a protein-protein interaction (PPI) network, and Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses of core targets were performed using the Metascape database. The results showed that a total of 132 chemical components were identified in DBFT, among which 87 components were derived from the "Yong" group of herbs, 49 from the "Ti" group of herbs, 4 from the "Hua" group of herbs, and 8 components were shared by the "Ti" and "Yong" groups of herbs. A total of 84 potential active components of DBFT were screened out based on the Swiss ADME gastrointestinal absorption and five principles of druggability. There were 294 common targets with the stable phase of COPD, and 87 core targets were obtained through calculation using Cytoscape. The KEGG-enriched pathways mainly included the PI3K-AKT signaling pathway, HIF-1α signaling pathway, AGE-RAGE signaling pathway, EGFR tyrosine kinase inhibitor resistance, and MAPK signaling pathway, which played a role in the treatment of the stable phase of COPD. Among them, the "Ti" group of herbs mainly acted on the C-type lectin receptor signaling pathway, the "Yong" group of herbs acted on the PI3K-AKT signaling pathway, and the "Hua" group of herbs acted on the differentiation process of Th17 cells. The research results provide a scientific basis and support for the clinical application and in-depth study of this prescription.

  • Xin-hong CHU, Rui-xuan ZHANG, Shi-yang SHEN, Hui WANG, Yu-jiao SUN, Ying-peng LI
    Acta Pharmaceutica Sinica. 2026, 61(5): 1819-1829.

    In this study, we employed astragalus polysaccharides (APS), derived from the traditional Chinese medicine Astragalus, as a natural carrier, and curcumol (CUL), a hydrophobic component with antitumor activity in the traditional Chinese medicine Curcuma longa, as a model drug, to construct a drug-loaded integrated nanoimmune drug delivery system, CUL@AHNP, and systematically evaluate its in vitro properties, oral absorption properties, and antitumor immune activity. The CUL@AHNP was prepared by high-pressure homogenization, resulting in a particle size of approximately 116.4 nm. It exhibited a spherical structure, a negatively charged surface, and good dispersion and stability. In vitro experiments demonstrated that CUL@AHNP could significantly enhance the inhibitory effect of CUL on breast cancer 4T1 cells and effectively induce immunogenic cell death (ICD) and activate anti-tumor immune responses. Assays measuring cellular uptake and tumor sphere penetration verified the sub stance's excellent transmembrane transport and tissue penetration ability. In vivo studies demonstrated that the oral administration of CUL@AHNP led to a substantial inhibition of tumor growth and an enhancement in the infiltration density of CD8+ and CD4+ T cells. The combination of CUL@AHNP and the chemotherapeutic drug doxorubicin (DOX) exhibited a certain degree of synergistic antitumor effect, without causing significant liver or kidney toxicity. All animal experiments had been approved by the Experimental Animal Ethics Committee of Tianjin University of Traditional Chinese Medicine (No. 2023114). In conclusion, this study constructed an oral nanoimmune drug delivery system based on astragalus polysaccharides, which provides a safer and more efficient therapeutic option for the treatment of breast cancer with traditional Chinese medicine.

  • Jiu-yang WANG, De-sheng WANG, Ri-qing CHENG, Hui-qing GUO, TANA, QIHERIMA, Chang-jin XU
    Acta Pharmaceutica Sinica. 2026, 61(5): 1830-1840.

    To achieve precise drug delivery responsive to the tumor microenvironment (TME), this study designed and constructed a multifunctional nanotherapeutic system. The system employs spherical manganese dioxide (MnO2) as the core, which is loaded with gold nanoparticles (Au nanoparticles, GNPs) and the chemotherapeutic drug 5-fluorouracil (5-FU). It successfully integrates the near-infrared photothermal effect of GNPs and the responsiveness of MnO2 to high glutathione concentration and acidic pH, enabling on-demand drug release under multiple stimuli. Experimental results demonstrate that the as-constructed MnO2/GNPs@5-FU nano-system exhibits high drug loading capacity, excellent photothermal conversion efficiency, and remarkable TME-dependent drug release behavior. In vitro cell experiments demonstrated that the system, by combining MnO2-mediated chemodynamic therapy and 5-FU chemotherapy, achieved a highly efficient synergistic killing effect against 4T1 tumor cells. This study provides preliminary in vitro experimental evidence and novel insights for the development of intelligent nanodrug delivery platforms for tumor-targeted therapy.

  • Na-na ZHANG, Yu-tong GAN, Tian-yi XIN, Zhi-jie SHI, Wen-jie XU, Jing-yuan SONG
    Acta Pharmaceutica Sinica. 2026, 61(5): 1841-1851.

    Citrus plants are economically and medicinally important crops worldwide. However, due to the highly complex genetic background of the genus, the accurate identification of medicinal species within this genus remains a major challenge. In this study, we employed the analysis of whole-GEnome (AGE), also known as the Shizhen Method, to conduct bioinformatics analysis on 49 genomes from 15 Citrus species, successfully constructing a candidate species-specific target sequence library that covers these species. The number of specific target sequences per species predominantly ranges from 10 000 to 100 000. From this candidate library, species-specific target sequences were selected for the corresponding species. Their high specificity was subsequently verified using Sanger sequencing and CRISPR-Cas12a technology, which confirmed their efficacy in identifying medicinal Citrus species. Based on this foundation, we established an AGE-based identification system for closely related Citrus species, which enabled the precise authentication of 30 commercial samples of Citri Reticulatae Semen and its decoction pieces. This study demonstrates that the AGE can be used for the accurate identification of medicinal Citrus species, which breaks through the bottlenecks of traditional methods and effectively resolves the identification challenges. It thereby provides technical support for quality control of Chinese herbal medicine and clinical medication safety.

  • Mi-mi TIAN, Ping XU, Xiao-ye ZHANG, Jun-zhe ZHOU, Mao-ying CUI, Guo-wei ZHENG
    Acta Pharmaceutica Sinica. 2026, 61(5): 1852-1860.

    To identify the key genes involved in the synthesis of polyphyllin within downstream pathways, this study employed high-performance liquid chromatography (HPLC) to quantify the content of eight types of polyphyllins in two groups of Paris polyphylla var. yunnanensis rhizomes, followed by transcriptome sequencing analysis. The results revealed significant differences in the content of the eight types of polyphyllins between the two groups. Specifically, the total saponin content in the high saponin content group (HS) was 24.81 mg·g-1, whereas that in the low saponin content group (LS) was 5.99 mg·g-1. Notably, polyphyllin Ⅱ, Ⅲ, and Ⅴ were undetectable in the LS group. The substantial difference in total saponin content between the two groups can be primarily attributed to the considerable accumulation of diosgenin-type saponins in the HS group. A total of 11 399 differentially expressed genes were identified through transcriptome sequencing, the comparison between HS and LS, with 5 708 genes exhibiting upregulation and 5 691 genes exhibiting downregulation. This study successfully screened seven candidate genes involved in the synthesis of polyphyllin and conducted protein structure prediction for these genes. Through interaction network analysis, 80 transcription factors with a correlation coefficient of 0.95 or higher with the candidate genes were identified, among which a total of 8 transcription factors were correlated with two or more candidate genes. The findings provide a theoretical foundation for predicting genes related to polyphyllin synthesis, exploring the biosynthetic pathway of polyphyllin, and understanding their accumulation patterns.

  • La-ha A MU, Zhi-fei ZHANG, Wen-qin CHEN, Xin WANG, Zhen-yu PENG, Bao-wei WANG, Can-can TONG, Zi-qi LIU, Xiao-hui WANG, Sheng-li WEI
    Acta Pharmaceutica Sinica. 2026, 61(5): 1861-1868.

    Fritillaria ussuriensis Maxim is a valuable medicinal plant in Northeast China. Based on previous chloroplast genome sequencing results, this study selected the chloroplast genome fragments atpF and petB as specific DNA barcodes to identify germplasm resources of commercially available F. ussuriensis. Additionally, the content of peiminine was analyzed using a UV spectrophotometer, aiming to clarify the main germplasm resources and quality of F. ussuriensis in the market. In this study, 74 samples of commercially available F. ussuriensis were collected from 52 cities across 23 provinces. Based on the combined analysis of atpF and petB sequences, a total of 10 haplotypes (h2, h3, h4, h5, h6, h11, h13, h16, h19, and h20) were identified, among which h19 and h20 were reported for the first time. Haplotype h4 was the predominant haplotype, accounting for 44.59% of the total samples, followed by haplotype h3. The content determination results showed that 60 batches (81.08%) of commercially available F. ussuriensis samples met the standards of the 2025 edition of the Pharmacopoeia of the People's Republic of China. The content of peiminine in the samples ranged from 0.044% to 0.075%, and the sample quality was uneven; among them, haplotype h16 had the highest average content of peiminine at 0.063%, while haplotype h6 had the lowest at 0.044%. Statistical analysis indicates that, overall, there is no statistically significant difference between haplotypes and the content of peiminine. Given its highest peiminine content, haplotype h16 shows potential value for selective breeding. This study is conducive to guiding the circulation of F. ussuriensis samples in the market and rational clinical use, and also provides a reference for protecting the genetic diversity of F. ussuriensis and for its sustainable development and utilisation.