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  • Ge-ge ZHAO, Ying-ying SI, Yan-zhi WANG
    Acta Pharmaceutica Sinica. 2026, 61(8): 3111-3115.

    Three new eudesmane sesquiterpenoids (oxyphylleudnes K-M) were separated and purified from the ethyl acetate fraction of Alpinia oxyphylla Fructus, by using various column chromatography methods such as MCI Gel CHP-20, YMC GEL ODS-A, and silica gel columns, combined with preparative thin-layer and semi-preparative liquid chromatography methods. Their structures were identified by modern spectroscopic techniques (1D and 2D NMR, UV, IR and MS) and with computational NMR and ECD methods. Among them, there are two nor-eudesmane sesquiterpenes (1, 2) and one seco-eudesmane sesquiterpene (3).

  • Ling ZHANG, Jing LIU, Cheng-tian TAO, Pan-deng WANG, Yong-xian CHENG
    Acta Pharmaceutica Sinica. 2026, 61(8): 3116-3122.

    Anti-renal fibrosis activity screening was performed on the extracts of Liquidambar formosana via the activity-tracing approach, which led to the identification of the bioactive fractions. Subsequent separation and purification afforded seven abietane-type diterpenoids, including one new diterpenoid, liquidformosane A (1) and six known ones. The planar structure of the new compound was established by nuclear magnetic resonance spectroscopy (NMR), and its stereoconfiguration was confirmed by quantum chemical calculations for simulation and prediction of electronic circular dichroism (ECD) spectra. The Western blot method was used to evaluate the in vitro anti-renal fibrosis activity of compounds 1-7, and the results showed that compounds 5-7 all exhibited significant anti-renal fibrosis activity.

  • You-min YING, Ji-geng CAO, Ting TIAN, Jing TANG, Shi-lei WANG, Wei-guang SHAN
    Acta Pharmaceutica Sinica. 2026, 61(8): 3123-3128.

    The chemical constituents of Stellera chamaejasme L. were separated by comprehensive column chromatography on MCI, ODS C-18, Toyopearl HW-40C, and silica gels. Structures of the isolated compounds were determined by NMR (nuclear magnetic resonance), MS (mass spectrometry), IR (infrared spectroscopy), and quantum chemical calculations. Nine compounds were isolated from the chloroform fraction 95% ethanol extract of the titled plant and identified as chamaejaslactone A (1), stelleranoid A (2), stelleranoid D (3), stelleranoid E (4), wikstronone A (5), wikstronone C (6), chamaejasmone D (7), daphnauranol A (8), and holosericin B (9), respectively. Among them, compound 1 was characterized as the first example of a sesquiterpenoid with an unprecedented 7,8-seco-guaiane skeleton. In the in vitro bioassay, compound 1 exhibited moderate inhibitory activity against Escherichia coli-originated β-glucuronidase with an IC50 value of 51.79 ± 3.21 μmol·L-1.

  • Cai-ying PENG, Xiao-jun PAN, Jian-qun LIU, Hui-lian HUANG, Ji-cheng SHU
    Acta Pharmaceutica Sinica. 2026, 61(8): 3129-3136.

    The ethanol extract of Pteris multifida was isolated and purified using various column chromatographic methods, including silica gel, Sephdex LH-20 and semi-preparative HPLC. Based on the physicochemical properties of the isolated compounds, their structures were elucidated by spectroscopic data such as MS, NMR, and CD. From the ethyl acetate fraction of P. multifida,18 terpenoids were isolated, including 14 sesquiterpenoids possessing a 1H-inden-1-one nucleus (1-14) and four nortriterpenoids with a megastigmane skeleton (15-18). They were identified as (2S,3S)-2,5,7-trimethyl-3-hydroxyl-6-carboxyl-indan-1-one (ptemulic A) (1), (2S,3S)-2,7-dimethyl-5,6-dihydroxymethyl-indan-1-one (ptemulinol A) (2), dehydropterosin B (3), 6-(1,2-dihydroxyethyl)-2,5,7-trimethyl-indan-1-one (4), pterosin D (5), (3R)-pterosin (6), pterosin D 3-O-β-D-glucopyranoside (7), (3R)-pteroside W (8), (3R)-pteroside D (9), 14-acetyl-pterosin A (10), pterosin A (11), 11-acetyl-pterosin A (12), pterosin A2 (13), (2S,3S)-pterosin C 3-O-β-D-glucopyranoside (14), dearabinosyl pneumonanthoside (15), grasshopper ketone (16), vomifoliol (17), roseoside Ⅰ (18). Compounds 1 and 2 were new compounds, while compounds 3, 4, 10-13, 16 and 18 were isolated from this plant for the first time. New compounds 1 and 2 showed anti-inflammatory activity by inhibiting the production of nitric oxide (NO), with IC50 values of 36.7 and 61.2 μmol·L-1, respectively.

  • Yu-xin LIU, Qiu-xia NONG, Yu-fei HOU, Fang YUAN, Shu-mei WANG, Xiong LI, Jian-chun MA, Yuan-yuan XIE
    Acta Pharmaceutica Sinica. 2026, 61(8): 3137-3149.

    Fufang E jiao Jiang (FFEJ), a Chinese patent medicine with the effects of tonifying Qi and nourishing blood, as well as nourishing Yin and moistening dryness, is clinically used as an adjuvant therapy for tumor patients and has been proven to possess certain anti-tumor activity. To identify the material basis for its anti-tumor efficacy, this study employed the cell counting kit-8 (CCK-8) assay to screen the anti-tumor active fractions of FFEJ on Lewis cells, and validated their activity through cell cloning, apoptosis, invasion, and migration assays. Ultra-high performance liquid chromatography coupled with quadrupole-Orbitrap high-resolution mass spectrometry (UHPLC-Q-Exactive-Orbitrap-MS), integrating network pharmacology analysis was used to systematically analyze the chemical components and potential action mechanisms of the active fractions. The results showed that the n-hexane (F2) and ethyl acetate (F3) extracts were the main anti-tumor active fractions of FFEJ. Both fractions dose-dependently inhibited Lewis cell colony formation, induced cell apoptosis, significantly reduced the horizontal and vertical migration abilities of Lewis cells, and suppressed their invasion and distant metastasis. F2 was dominated by primary metabolites such as organic acids and sugars, while F3 was rich in secondary metabolites including ginsenosides and iridoids. Network pharmacology analysis indicated that 60 key active components in F3 act on core targets such as proto-oncogene tyrosine-protein kinase Src (SRC), signal transducer and activator of transcription 3 (STAT3), and RAC-alpha serine/threonine-protein kinase (AKT1), regulating signaling pathways closely related to tumor apoptosis, migration, and invasion, including phosphatidylinositol 3-kinase/protein kinase B (PI3K/AKT), interleukin-17 (IL-17), tumor protein 53 (p53), and hypoxia-inducible factor-1 (HIF-1), thereby exerting synergistic anti-tumor effects. This study systematically elucidates the multi-component, multi-target, multi-pathway anti-tumor characteristics of FFEJ, identifies its active fractions and potential pharmacodynamic substances, and provides experimental evidence for the clinical application of FFEJ in adjuvant tumor therapy.

  • Teng-teng PENG, Long ZHAO, Guang-miao GAO, Bin FAN, Qu-huan MA, Xiao-feng SHI
    Acta Pharmaceutica Sinica. 2026, 61(8): 3150-3163.

    This study aims to analyze the components absorbed into the blood and brain after intragastric administration of Paeonia rockii pollen in rats, and to explore the pharmacodynamic material basis. The chemical constituents of Paeonia rockii pollen, as well as those in medicated serum and brain tissue, were investigated using ultra-performance liquid chromatography-electrospray ionization-triple quadrupole-linear ion trap mass spectrometry (UPLC-ESI-Q-TRAP-MS/MS) based on widely targeted metabolomics technology. Differential components were screened using principal component analysis and orthogonal partial least squares discriminant analysis, followed by functional annotation and pathway enrichment analysis, and the mass spectrometric fragmentation patterns of blood-brain barrier-penetrating components were deduced. A total of 340 components were identified from Paeonia rockii pollen, primarily including flavonoids, terpenoids, and phenolic acids. In the medicated serum, 38 prototype absorbed components such as methyl gallate, myricetin, trachelogenin, tyrosol, and albiflorin, along with two metabolites (inosine and hypoxanthine) were identified. In the brain tissue, 15 prototype components such as gallic acid, isorhamnetin, 4-hydroxycoumarin, resveratrol, and paeoniflorin were detected, and the plasma concentration was the highest after 2 h of intragastric administration. These components were mainly enriched in pathways such as longevity regulation, microbial metabolism in different environments, biosynthesis of secondary metabolites, flavonoid degradation, nicotinate and nicotinamide metabolism, and purine metabolism. The animal experiment protocol was approved by the Experimental Animal Ethics Review Committee of Lanzhou Institute of Food and Drug Control, Gansu Province (Approval No. 2023-010).

  • Wan-fang LI, Zhi-hua LIU, Yu FENG, Yan-min CHEN, Yuan-yuan LIU, Ting-ting WANG, Xue-qing XU, Yuan-yuan ZU, Xin-gang WANG, Hong-tao JIN, Yu-ling LIU
    Acta Pharmaceutica Sinica. 2026, 61(8): 3164-3173.

    This study comprehensively evaluated the reproductive safety of Ramulus Mori (Sangzhi) alkaloids (SZ-A) in rats, analyzed the toxicokinetics of the main active ingredient 1-deoxynojirimycin (DNJ) during embryo-fetal development, and determined the no-observed-adverse-effect level. Reproductive toxicity assessment was conducted in three stages (this study was reviewed and approved by the Institutional Animal Care and Use Committee of Beijing Union-Genius Pharmaceutical Technology Development Co., Ltd., ethics numbers: SN22072-DS, SN21288-DS, SN22074-DS). In stage Ⅰ, rats were orally administered SZ-A at doses of 100, 200 and 500 mg·kg-1 (calculated as total alkaloids) to evaluate its effects on fertility and early embryonic development, including sperm count and motility in males, as well as mating and pregnancy rates in females. In stage Ⅱ, pregnant rats were given SZ-A by gavage at 100, 200 and 500 mg·kg-1 to examine its impact on maternal health, embryo-fetal development, and fetal growth, while DNJ concentrations in maternal plasma, placenta and fetus were measured. In stage Ⅲ, pregnant rats were orally administered SZ-A at doses of 250, 500 and 750 mg·kg-1. Indicators were examined to evaluate perinatal safety, including maternal reproductive function; offspring growth and development, behavior and learning/memory function, reproductive function; and F2 embryonic development. The results showed that SZ-A had no adverse effects on fertility, early embryonic development in both male and female rats, and on embryo-fetal development in pregnant rats. The plasma exposure of DNJ in pregnant rats showed a linear relationship with the administered dose. However, only limited distribution of DNJ was observed in the placenta, and the drug was undetectable in whole fetal tissues. At all tested doses, SZ-A showed no reproductive toxicity. This was evidenced by normal sex ratio, growth and development, and reproductive function in the F1 generation; embryonic development of the F2 generation was also unaffected. The no-observed-adverse-effect level (NOAEL) of SZ-A over the entire reproductive cycle in rats was determined to be 500 mg·kg-1, indicating favorable safety. This finding provides essential reproductive safety data to support the potential clinical application of SZ-A in special populations such as diabetic patients of childbearing age, gestational diabetes mellitus (GDM), and patients with polycystic ovary syndrome (PCOS).

  • Run-lin SONG, Yue-lin FANG, Lin YANG, Xin-xin ZHANG
    Acta Pharmaceutica Sinica. 2026, 61(8): 3174-3185.

    As an important form of drug delivery, the transdermal drug delivery system has demonstrated unique advantages and potential in the treatment of various diseases such as chronic pain and skin diseases. However, in the prevention and treatment of skin photo-damage, it still faces issues like low transdermal efficiency and poor drug retention. Therefore, there is an urgent need to develop a highly efficient and safe drug delivery technology. In this study, solid lipid nanoparticles loaded with vitamin A palmitate (VAP-SLN) were designed and prepared to improve the encapsulation efficiency and stability of vitamin A palmitate (VAP), aiming to enhance the therapeutic effect of VAP on skin photodamage via transdermal drug delivery. The high-speed shearing and high-pressure homogenization method were used to prepare VAP-SLN. After prescription screening, it was determined that VAP-SLN was mainly composed of solid lipid glyceryl behenate and liquid lipid medium-chain triglycerides, phospholipids, Tween 80, alkyl polyglycosides and VAP. The prepared VAP-SLN had a particle size of approximately 200 nm, a spherical structure, and an encapsulation efficiency of 91.1%. Its phase transition temperature was 59.8 ℃. This characteristic endowed it with excellent thermal stability and significantly improved the stability of the encapsulated VAP. VAP-SLN exhibited the advantage of sustained-release characteristics and intradermal retention, which could significantly prolong the local drug action and enhance the transdermal drug delivery efficiency. At the cellular level, VAP-SLN exhibited good cellular uptake and retention ability in HaCaT cells, thereby enhancing the effect of VAP in alleviating cellular oxidative stress and inflammatory responses. In the mouse skin photodamage model, VAP-SLN could effectively improve the reduction of collagen fibers and the decrease in collagen volume in photodamaged skin, restore the epidermal thickness and morphology to a healthy level, and effectively prevent and treat ultraviolet-induced skin damage. The animal experiments were approved by the Institutional Animal Care and Use Committee of Yantai Institute of Materia Medica (Approval No.: 20250701-01). In conclusion, VAP-SLN significantly alleviates skin photodamage through antioxidant and anti-inflammatory mechanisms, providing a new strategy for the transdermal delivery of VAP and the prevention of skin photodamage.

  • Guang-yi XIANG, Hong-juan TANG, Hui-fang LI, Han-bing LI, Lin CHENG, Yong-gang ZHANG
    Acta Pharmaceutica Sinica. 2026, 61(8): 3186-3198.

    Oplopanax elatus Nakai is a deciduous shrub within the Araliaceae family and is classified as a first-class protected plant in Jilin Province. To elucidate the structural characteristics of its chloroplast genome and phylogenetic relationships, this study conducted chloroplast genome sequencing of one cultivated individual and five wild populations of O. elatus, followed by comparative chloroplast genomic and phylogenetic analyses with published congeneric species of Oplopanax and allied genera of Araliaceae deposited in GenBank. The results revealed that the chloroplast genomes of the six O. elatus accessions ranged from 156 108-156 193 bp in length, with a uniform GC content of 38.03%. A total of 129-133 genes were annotated, comprising 87-88 protein-coding genes, 6-8 rRNA genes, and 36-37 tRNA genes. The chloroplast genome of cultivated O. elatus contained one additional protein-coding gene compared to those of wild accessions. Using the chloroplast genome sequence of cultivated O. elatus as reference, sequence alignment against wild populations identified 36 single nucleotide polymorphism (SNP) loci and 10 insertion-deletion (InDel) loci. SNPs were distributed in both intergenic spacers and coding sequences (CDS), whereas all InDels were restricted to the large single-copy (LSC) region. Nucleotide diversity (Pi) analysis of the 13 chloroplast genomes detected two hypervariable regions, clpP1-exon3_clpP1-exon2 and ycf1, which are proposed as candidate DNA barcodes and molecular markers for O. elatus. Analysis of codon preference indicated that all 13 samples exhibited a preference for codons terminating in A or T. Discrepancies in codon numbers were observed between cultivated and wild O. elatus chloroplast genomes. A total of 545 simple sequence repeat (SSR) loci and 498 dispersed repeat sequences were identified within the 13 chloroplast genomes. Phylogenetic reconstruction based on branch support values and clustering patterns partitioned the eight Araliaceae genera into four clades. The genus Oplopanax formed a highly supported monophyletic lineage positioned centrally within the tree, diverging subsequently to Panax and constituting a sister group to the fourth major clade, with its closest affinity to Schefflera. This investigation advances the understanding of evolutionary dynamics within Oplopanax and allied genera, with the acquired genomic resources providing a foundation for DNA barcode screening and germplasm conservation of the genus.

  • Si-qi WU, Jia-yi REN, Jin-yong WANG, Bei-lei YU, Jun-gui DAI, Ri-dao CHEN
    Acta Pharmaceutica Sinica. 2026, 61(8): 3199-3206.

    Hyperforin is a key pharmacologically active constituent responsible for the antidepressant and other therapeutic effects of Hypericum perforatum. However, its content within medicinal materials varies significantly according to the harvest season and the plant organ, leading to inconsistencies in drug quality. To elucidate the dynamic patterns of hyperforin biosynthesis, this study systematically analyzed the accumulation of hyperforin and the expression levels of key biosynthetic genes in the roots, stems, leaves, and flowers of H. perforatum collected across different seasons. The results revealed that hyperforin accumulation exhibits distinct seasonal fluctuations and tissue specificity, following the order of flower > leaf > stem > root. Notably, the hyperforin content in leaves reached its peak in the second season. The expression patterns of key biosynthetic genes (e.g., HpPKS, HpPT1-4) were inconsistent with the accumulation trends of the final product in terms of both temporal (seasonal) and spatial (tissue) dynamics. Gene expression was predominantly active during the first season and was significantly high in roots, where hyperforin content was the lowest. These findings suggest that the regulation of hyperforin biosynthesis involves complex multi-level mechanisms, with an asynchronous regulatory relationship between gene expression and the accumulation of the final product. By dissecting the spatiotemporal characteristics of hyperforin biosynthesis from both the perspectives of metabolite accumulation and gene expression, this study not only provides a theoretical basis for further research into its regulatory mechanisms but also offers valuable insights for the quality control, metabolic regulation, variety breeding, and the development of science-based cultivation and harvesting strategies of H. perforatum.