Kidjoranin (1), one of the major C-steroidal aglycones isolated from Cynanchum otophyllum in our previous work, was used as the substrate for the preparation of a series of 3β-O-neoglycoside derivatives via the CdCO-mediated Koenigs-Knorr reaction. The resulting compounds were evaluated for cytotoxicity against a panel of human cancer cell lines (MCF-7, HCT-116, HeLa, and HepG2). Among them, compounds 2b, 2l, and 4a displayed significant cytotoxic effects, with IC values ranging from 6.00 to 9.41 μM, 2.58 to 3.20 μM, and 3.02 to 4.48 μM, respectively. Preliminary mechanistic studies revealed that compound 4a could induce apoptosis and lead to cell cycle arrest at the S phase in a dose-dependent manner. Furthermore, exploratory molecular docking was also performed to probe possible binding modes of 4a with PI3Kα, STAT3, and Cyclin D1. Collectively, these findings indicate that C-3 glycosylation of kidjoranin may represent a viable approach for developing new anticancer candidates.

Eugenia gracillima Kiaersk. is traditionally used in the treatment of urinary tract infections, respiratory disorders, and skin conditions, and its essential oil (EgEO) from leaves has shown antioxidant, anti-protozoal, analgesic, and anti-inflammatory effects, although its pharmacological potential remains insufficiently studied. This work aimed to evaluate the hemolytic, cytotoxic, toxicological, and antifungal properties of EgEO. The oil was extracted by hydrodistillation and chemically characterized by GC/MS, revealing 39 sesquiterpenes representing 97.02 % of the total composition. Hemolytic activity was assessed via spectrophotometric quantification of hemoglobin released from human erythrocytes, while cytotoxicity was evaluated using the MTT assay in HL-60, MCF-7, and HT-29 cell lines, showing significant cytotoxicity, particularly against HL-60 (IC₅₀ = 10.8 μg/mL). Contact toxicity was tested on Tenebrio molitor larvae, pupae, and adults, with pupae being the most susceptible (LD₅₀ = 4.55 mg/mL), followed by adults and larvae. Sublethal doses (2.3 and 4.6 mg/mL) injected into larvae caused no morphological abnormalities. Antifungal activity against standard and multidrug-resistant strains of Candida glabrata was evaluated through broth microdilution, with MICs ranging from 0.11 to 3.69 mg/mL and MFCs from 0.92 to 3.69 mg/mL. Time-kill assays indicated that EgEO at MIC had fungistatic activity, while at 2 × MIC it was fungicidal. In vivo efficacy, assessed using T. molitor as an infection model, demonstrated that EgEO at a sublethal dose (2.302 mg/mL) was effective against the standard C. glabrata strain. Overall, EgEO showed low hemolytic activity, significant antitumor effects, and notable antifungal efficacy, with low toxicity in vivo, particularly at sublethal concentrations. These results support the therapeutic potential of E. gracillima essential oil as a natural agent with antifungal and anticancer properties.

Eight lignans and four phenylpropanoids were isolated and identified from the roots of Rosmarinus officinalis, three of which were previously unreported compounds. Their structures were elucidated through comprehensive spectroscopic analyses, including HRESIMS, NMR, UV, IR, and ECD calculations. The new compounds were designated as rosmarinicols A-C (1-3). The anti-inflammatory activities of all the compounds were assessed using an LPS-induced RAW264.7 mouse macrophage model. The results showed that compounds 3, 5, 8, 9, 11, and 12 inhibited the production of NO in a dose-dependent manner at concentrations of 2.5, 5, and 10 μM, with IC values of 21.98, 5.01, 6.91, 4.43, 12.65, and 7.11 μM, respectively. This study demonstrates that the roots of Rosmarinus officinalis are rich in lignans with promising anti-inflammatory lignans properties, providing a scientific basis for further research and potential development.

This review systematically examines the scientific literature on the genus Erica (heathers), with a focus on their phytochemical diversity and pharmacological potential. The objective is to critically analyze how extraction methods and species origin influence the profiles of bioactive compounds responsible for therapeutic effects. A comprehensive evaluation of phytochemical data is presented for widely studied species, including Erica arborea, Erica andevalensis, Erica australis, Erica manipuliflora, Erica cinerea, Erica verticillata, Erica carnea, Erica scoparia, Erica spiculifolia, Erica multiflora, and Erica mannii. Evidence indicates that extraction techniques and solvent polarity strongly affect the yield and diversity of secondary metabolites such as phenolic acids, flavonoids, and terpenoids, which are associated with antioxidant, anti-inflammatory, antimicrobial, diuretic, and anticancer activities. Importantly, this review highlights pronounced taxonomic and geographic sampling biases: most studies focus on European and Mediterranean Erica species, with very limited representation from Africa despite its exceptional species richness. These findings emphasize the need to optimize extraction protocols and expand research to underrepresented taxa. Overall, this synthesis underscores the therapeutic promise of Erica species and provides a foundation for future drug discovery efforts guided by phytochemical characterization and bioactivity screening.

This study investigates the chemical constituents and biological activities of the stems of the Mongolian medicinal plant Syringa oblata Lindl. ("Alashan-Agaru"). Through chromatographic separation and spectroscopic analysis, 34 compounds were isolated from the ethyl acetate fraction, including four new and ten first-reported in Syringa species. Using an LPS-induced RAW264.7 macrophage model, several compounds significantly inhibited NO production. It is known that compound 34 significantly reduced the levels of interleukin - 1β, interleukin - 6 and CD14. In addition, among the 23 lignans detected by the DPPH method, five showed strong antioxidant activity, with half - maximal inhibitory concentration (IC₅₀) values lower than that of vitamin C. These results provide a scientific basis for the medicinal use of the stems of Syringa reticulata var. amurensis.

Poria cocos is a prominent traditional fungal medicine that has been utilized in China for over a millennium. Its major bioactive constituents include triterpenes and polysaccharides, along with other minor components such as steroids, histidine, choline, amino acids, and essential minerals, which exhibit diverse pharmacological mechanisms, including antitumor, antibacterial, immunomodulatory, anti-aging, antioxidant, anti-inflammatory, hepatoprotective, neuroprotective, and cardioprotective effects. Globally, cancer remains a leading cause of mortality, accounting for approximately nine million deaths annually. Despite advances in current conventional therapies, complete tumor eradication remains elusive, and these treatments are often accompanied by severe adverse effects. To comprehensively evaluate the therapeutic potential of poria cocos, publications from 2002 to 2025 were systematically reviewed from PubMed, Web of Science, ScienceDirect, and Google Scholar. This review elucidates the antitumor properties of poria cocos on various cancers, including lung, colorectal, breast, and gastric cancers. Furthermore, it highlights its adjuvant role in enhancing the efficacy of chemotherapeutic agents through multiple mechanisms, such as inhibition of cellular proliferation and metastasis, induction of apoptosis and cell cycle arrest, and modulation of immune, inflammatory, and oxidative signaling pathways. Collectively, these findings demonstrate the promising antitumor and adjuvant potential of poria cocos in cancer therapy. Nevertheless, further investigations are required to determine optimal dosages, toxicity profiles, and clinical efficacy. Rigorous quality control, standardization, and well-designed clinical trials are essential to validate its safety and effective clinical application.

Stomach heat syndrome (SHS) is a common clinical digestive system disease, which seriously affects people 's quality of life. Kouchi Liuxiang Fang (KLF) has a significant effect in the clinical treatment of SHS. However, its potential therapeutic mechanism is not fully understood. The purpose of this study is to explore the potential mechanism in improving SHS by integrating multi-omics through network pharmacology. The in vitro and in vivo components of KLF were identified by UHPLC-Orbitrap Exploris/MS technology. Network pharmacology was used to predict the potential core pathways of KLF to improve SHS. The protective effect of KLF on SHS-induced gastric mucosal injury was evaluated in vitro and in vivo. Finally, the multi-omics strategies of network pharmacology, 16S rRNA sequencing and metabolomics were integrated to explore the mechanism of KLF in improving SHS. UHPLC-Orbitrap Exploris/MS identified 117 chemical components and 53 prototype components in KLF. In vitro and in vivo experiments showed that KLF had a good protective effect on SHS. Integrated multi-omics analysis (network pharmacology, 16S rRNA sequencing, metabolomics) revealed KLF improves SHS by restoring gut flora balance and activating the PI3K-Akt pathway, confirmed by Western Blot and RT-qPCR analysis. This study provides a basis for the mechanism of KLF in improving SHS, and provides a solid foundation for drug development and clinical application of SHS prevention and treatment.

Seven indole diketopiperazine-based hybrids, including four new compounds (1-4) and three known ones (5-7), were successfully isolated from the fungus Aspergillus sp. EGF 15-0-3. Comprehensive spectroscopic analyses, combined with single-crystal X-ray diffraction and electronic circular dichroism calculations, were employed to elucidate their structures, relative configurations, and absolute configurations. Biological evaluation revealed that all obtained compounds except 2 exhibited potential TDP1 inhibitory activity. Notably, compound 3 demonstrated unique dual inhibitory effects against both TDP1 and TDP2, highlighting its promising therapeutic potential.

Phytochemical investigation of Maclura fruticosa (Moraceae) yielded twelve flavonoids from its twigs and leaves, including six undescribed compounds: five prenylated isoflavones (maccosas G-K, 1-5) and one benzylated dihydroflavonol (maccosa L, 6), alongside six known analogues (7-12). Structural elucidation was accomplished through NMR, HRESIMS, and ECD analyses. The anti-inflammatory activity of all the isolated compounds was screened and three benzylated dihydroflavonols (6, 11 and 12) exhibited potent anti-inflammatory activities. Compound 6 decreased LDH level in a dose-dependent manner, showing IC value of 8.53 μM.

Veronica incana L. (Plantaginaceae), commonly known as silver speedwell, is a flowering plant native to eastern Europe and parts of Russia, Siberia, Mongolia, and northern China. This study aimed to isolate various iridoid glycosides and other phytochemicals from the n-BuOH fraction of V. incana, resulting in the identification of one new phenolic compound (1) along with three known phenolic compounds (2: 1-O-β-d-vanillyl-glucose, 3: isopungenin, and 4: pungenin), one tyrosol (5: salidroside), one flavonoid (6: apigenin), two megastigmane glucosides (7: [6R,9R] 3-oxo-α-ionol-β-d-glucoside and 8: [6R,9S] 3-oxo-α-ionol-β-d-glucoside), and ten iridoid glycosides (9: veronicoside, 10: catalposide, 11: 4'-methoxycatalposide, 12: verproside, 13: 6-O-veratroylcatalpol, 14: 6-vanilloylcatalpol, 15: 6-O-isovanilloylcatalpol, 16: verminoside, 17: longifolioside A, and 18: dolicocymboside D). The isolation of these compounds was achieved through solvent partitioning, open-column chromatography, and semi-preparative high-performance liquid chromatography. Their structures, including absolute configurations, were determined by 1D and 2D NMR spectroscopy, optical rotation [α], and electronic circular dichroism (ECD), and confirmed by comparison with reported data. Among the isolates, compounds 2-5, 7-9, 11, 13, and 16-18 were reported for the first time from this species, while compounds 2, 7, and 8 were newly reported from the genus Veronica. Notably, compound 3 was isolated for the first time from this plant family. To evaluate their potential anticancer activity, all isolated compounds except 3, 4, and 5 were tested for antiproliferative effects against DU-145 prostate cancer cells using the MTT assay. Compounds 10 and 11 demonstrated notable inhibitory activity in this assay.

Myocardial infarction (MI) is a multifactorial cardiovascular condition characterized by metabolic disturbances and inflammatory responses. QiShenYiQi dropping pills (QSYQ), a traditional Chinese medicine formula, have shown therapeutic potential through multi-component and multi-target mechanisms, yet their effects from the perspective of active compounds and metabolites remain underexplored. This study utilized phytochemical characterization, metabolomics, network pharmacology, molecular docking, and biological validation to investigate QSYQ's pharmacological mechanisms in MI treatment. Chemical constituents were identified via UHPLC-Q-Orbitrap HRMS, and plasma metabolites from MI rats were analyzed using UPLC-MS/MS. Network pharmacology and docking revealed 19 active components, 68 target proteins, and key pathways, including cAMP-Rap1 and PI3K-Akt, associated with QSYQ's effects. Experimental validation demonstrated that QSYQ significantly improved cardiac function, reduced myocardial fibrosis, and modulated key pathway proteins, including Cyclin D1. A two-week regimen proved more effective than one week. Enrichment analysis highlighted QSYQ's role in regulating cell proliferation and survival, supported by changes in 45 plasma metabolites. Molecular docking confirmed interactions between active components and targets, and biological validation reinforced the importance of cAMP-Rap1 and PI3K-Akt pathways. This study provides a systematic framework for understanding the therapeutic mechanisms of QSYQ, emphasizing its potential in addressing cardiac dysfunction and myocardial fibrosis in MI.

Terminalia chebula is a widely used medicinal herb in traditional phytotherapy, valued for its extensive range of therapeutic uses. In this study, the seed extract (TCS) was investigated for its potential against multidrug-resistant (MDR) pathogens associated with diabetic foot ulcer (DFU) infections. The clinical isolate Pseudomonas aeruginosa (DW07) was extremely resistant to standard antibiotics, reaffirming its MDR phenotype. Chemical profiling of TCS with liquid chromatography showed a dense phytochemical profile containing ellagic acid, chebulagic acid, punicalagin, corilagin, and chebulinic acid, which is all attributed to specific anti-pathogenic activities like quorum sensing inhibition, biofilm inhibition, efflux pump obstruction, and disrupting bacterial adhesion. The extract showed dose-dependent antibacterial activity with a minimum inhibitory concentration of 0.70 ppm, and was found to greatly inhibit biofilm formation to the extent of 87.57 %. Transcriptomic analysis also showed wide modulation of bacterial physiology as 54 genes were differentially expressed and significant downregulation of virulence-related proteins such as short-chain dehydrogenase oxidoreductase, histidine kinase, and PtxR. Gene Ontology classification identified functional effects on DNA binding, lipopolysaccharide biosynthesis, and major metabolic pathways. Overall, these findings indicate that the phytochemical variability of T. chebula seeds not only establishes a molecular foundation for its traditional application but also attests to its potential as a plant-based therapeutic approach in the phytomedical management of chronic wound infections due to MDR pathogens.

Ten non-limonoids type ingredients with four structural skeletons, including two cyclic peptide (1/3), a 5-hydroxymethylfurfural derivative (2), two monoterpenoid glycosides (4/5), and five coumarins (6-10), were discovered from Citrus medica var. Sarcodactylis fruits guided by single-node based CMN and feature-based molecular networking (FBMN) strategy. Among of them, the new cyclic heptapeptide 1 is with rare asparagine unit, and the new skeleton of 2 is formed between 5-hydroxymethylfurfural and malonic acid through aldol condensation, which were elucidated undoubtedly through NMR and single crystal diffraction. The cyclic dipeptide and monoterpenoid glycosides were also isolated from this plant for the first time. Bioactivities evaluation indicated that the cyclic heptapeptide 1 can significantly inhibit the production of IL-1β (IC 7.65 ± 0.04 μM) in THP-1 Cells and possess potential anti-inflammatory activity. This research provided further basis for clarification of its chemical constituents and development as natural medicine and food.

Traditional African medicine utilizes Annona muricata leaves and Telfairia occidentalis (fluted pumpkin) seeds for cancer management, though their mechanistic basis and potential enhancement through nanotechnology remain insufficiently characterized. This study evaluated the phytochemical composition, antioxidant capacity, and experimental chemotherapeutic efficacy of T. occidentalis seed and A. muricata leaf extracts, with a focus on the role of chitosan nanoparticle encapsulation in improving biological performance in a rat model of prostate carcinogenesis. Prostate tumors were induced in male Wistar rats using N-methyl-N-nitrosourea (MNU) and testosterone, followed by oral administration of crude or nanoparticle-encapsulated extracts for 21 days. GC-MS, HPLC, and qualitative phytochemical analyses revealed abundant terpenoids, sterols, fatty acids, flavonoids, and alkaloids. Treatment normalized hematological parameters, mitigated oxidative stress (decreased MDA; increased SOD, CAT, and GSH), and reduced tumor burden and prostate-specific antigen (PSA) levels. Nanoparticle formulations produced more pronounced effects, lowering serum PSA from 6.72 ± 0.24 ng/mL in untreated rats to 2.12 ± 0.16 ng/mL (p < 0.05), and suppressing Ki-67 immunoexpression. Histopathological examination showed decreased epithelial hyperplasia and improved glandular preservation in nanoparticle-treated animals relative to crude extracts. These findings corroborate previous reports that phytochemicals from A. muricata and T. occidentalis exhibit antioxidant and antiproliferative properties, while providing new experimental evidence that nanoencapsulation can potentiate these effects. Although further mechanistic and clinical investigations are warranted, the present study highlights the promise of biopolymer-based nanoparticle systems as a means of enhancing the therapeutic potential of African ethnobotanicals in prostate cancer research.

Bronchial asthma, a multifaceted disease involving multiple cellular components, including airway epithelial cells, mast cells, and airway smooth muscle cells (ASMC). Our previous research has highlighted the crucial role of taste type 2 receptors (TAS2Rs) in alleviating airway inflammation, allergic responses, and abnormal ASMC proliferation in bronchial asthma. Ginkgo Biloba leaf, a traditional Chinese medicine with bitter properties, has demonstrated potential therapeutic value in bronchial asthma. The current study aimed to investigate the critical role of TAS2Rs in the alleviation of bronchial asthma by G. biloba leaf. In vitro cellular experiments revealed that the aqueous decoction of G. biloba leaf (GBLAD) significantly inhibits 16HBE inflammatory responses (assessed by LDH and TNF), RBL-2H3 degranulation (including IL-3, MCP-1, calcium influx, and F-actin reorganization), and ASMC proliferation (encompassing cell cycle and migration). Intracellular calcium assays revealed that GBLAD selectively activates TAS2R4, 14, and 38 receptors. Subsequent investigation revealed that blocking the Gβγ signaling pathway, specifically targeting SERCA, resulted in a marked reduction in the ability of GBLAD to stimulate TAS2Rs and its effectiveness in alleviating asthma. UPLC-Q-Exactive MS identified bilobalide, kaempferol, and quercetin as potential bioactive compounds that activate TAS2Rs to inhibit epithelial inflammation, cell degranulation, and ASMC proliferation. Notably, the downstream mechanisms of the compounds align with the overall action of G. biloba leaf, involving SERCA in the Gβγ pathway. Our findings provide significant insights and a theoretical framework for the application of G. biloba leaf in the treatment of bronchial asthma.

To investigate the complete chloroplast genome sequences and codon usage bias of "Shan Dou Gen" (Sophorae Tonkinensis Radix et Rhizoma) and its six easily confused species, analyze their evolutionary patterns, and evaluate the identification efficiency of four DNA barcodes combined with two machine learning methods for these seven plant species. Chloroplast gene structures of the seven species were aligned to construct phylogenetic trees. Codon usage bias was analyzed using CodonW and CUSP. Genetic distances were calculated based on the Kimura-2-Parameter model to assess the barcoding gap and reconstruct phylogenetic trees.Species discrimination capabilities of four DNA barcodes (ITS2, matK, psbA-trnH, and rbcL) were compared. Species identification was performed using BLOG and WEKA machine learning algorithms. Single-nucleotide SSRs predominated in chloroplast genomes, primarily composed of A/T bases. Complete species differentiation was achieved using cpDNA. Natural selection was the primary factor influencing codon usage bias, followed by mutation pressure. Among synonymous codons, A > T and G > C in base composition, with optimal codons ending in A/U at the third position across all seven species. All four DNA barcodes successfully discriminated Shandougen from its confusable species. The BLOG algorithm achieved >85 % identification accuracy, outperforming WEKA. This research provides a theoretical foundation for ensuring clinical medication safety, elucidating plant phylogeny, facilitating species identification, and guiding resource conservation and utilization of Shandougen and its analogues.

Three undescribed alkaloids, asperalkals A-C (1-3), as well as two known analogues (4 and 5), were isolated from Aspergillus sp. TJ507. Their structures were elucidated through comprehensive spectroscopic analysis, chemical derivatization, and ECD calculations. Subsequently, the immunosuppressive effects of these compounds were assessed in mouse lymphocytes stimulated with either anti-CD3/anti-CD28 monoclonal antibodies (mAbs) or concanavalin A (ConA). The results revealed that moderate immunosuppressive activity was observed for compounds 2-4, exhibiting IC values in the range of 13.77 ± 2.73 to 21.37 ± 3.33 μM, providing potential lead compounds for novel immunosuppressant development.

Glucose esters of α-methylene-γ-hydroxybutyrates known as tuliposides (Pos) are accumulated in tulip and are enzymatically converted to bioactive tulipalins (Pa) by a carboxylesterase, a tuliposide-converting enzyme. Herein, we evaluated the antibacterial and anti-yeast activities of naturally occurring variants of Pos and Pa, along with synthetic Pa analogs, including ring-opened hydroxy acids of Pa (PaA/B-acids) and their methyl esters, predicted PaB degradation products, and ring-expanded analogs of Pa, by determining their half-maximal inhibitory concentration values through turbidimetric assays. To enhance compound stability during the assay, we developed a modified minimal medium. PaA-forming (A-type) Pos (6-PosA, 1-PosA, PosD, PosG, and PosK-M) and PaA showed little or no antibacterial activity, whereas PaB-forming (B-type) Pos (6-PosB and PosF) and PaB showed markedly higher activity. Among the PaA/B-acids and methyl esters, only PaB-acid methyl ester showed activity, likely because of its ability to form active PaB. All tested PaB degradation products and their analogs exhibited no antibacterial activity. The activity trend of the ring-expanded analogs of PaA/B was similar to that of A- or B-type analogs. In anti-yeast assays, both PaA and PaB displayed weak and comparable activities, suggesting different modes of action against bacteria and yeast. These results enhance our understanding of the natural roles and potential applications of Pos, Pa, and their analogs as antimicrobial agents.

Candida (Candidozyma) auris is a multidrug-resistant fungal pathogen associated with high mortality and limited treatment options. Eugenia dysenterica, a medicinal plant from the Brazilian Cerrado traditionally used for gastrointestinal ailments, is rich in bioactive phenolics with potential therapeutic applications. To evaluate the chemical composition, antifungal activity, mechanisms of action, and in vivo effects of ethanolic leaf extract of E. dysenterica (Ed-EE) against C. auris. Ed-EE was analyzed for phenolic and flavonoid content. Its antifungal activity and interactions with amphotericin B (AmB) and fluconazole (FLC) were tested using microdilution and checkerboard assays. Mechanisms of action were explored through membrane integrity and efflux pump inhibition assays. Hemolysis assay was performed to assess hemocompatibility. In vivo toxicity and efficacy were evaluated using Tenebrio molitor larvae. Ed-EE exhibited fungistatic activity against C. auris, with a MIC of 32 μg/mL. When combined with AmB, a synergistic effect was observed (FICI = 0.5), reducing the MICs to 8 μg/mL for Ed-EE and 0.5 μg/mL for AmB. Mechanistic assays indicated moderate membrane disruption and efflux pump inhibition. Hemolysis and in vivo assays using T. molitor larvae showed survival rates above 80 %, confirming low toxicity. However, Ed-EE did not significantly inhibit biofilm formation at tested concentrations. Ed-EE exhibits promising antifungal activity against C. auris, particularly in synergy with AmB, and demonstrates a favorable safety profile as potential adjuvant therapy for resistant fungal infections.

The study of potential high-added-value waste materials is pivotal for their recycling and repurpose in the market. Walnut husks are a well-known source of bioactive natural products with potential applications in the antimicrobial and anticancer therapies or in the cardiovascular and neurodegenerative prevention, and as anti-inflammatory treatments. However, since the metabolic content of walnut husks is highly dependent on their variety, there is still a need for thorough systematic phytochemical investigations of this precious waste material of the food industry. Herein we report the anti-inflammatory evaluation and an NMR-based phytochemical profiling of the ethyl acetate fraction of husks obtained from Juglans regia var. Sorrento. Our study demonstrated that the extract exerts significant anti-inflammatory activity by reducing the NO and PGE production in LPS-stimulated cells in a concentration-dependent manner by inhibiting iNOS and COX-2 proteins. The phytochemical analysis of the bioactive fraction revealed the dominant presence of diarylheptanoids and triterpenoids and resulted in the discovery of the new ursane derivative huskol (15).