Chromatographic separation of the leaves of Sapium sebiferum afforded two previously undescribed dammarane-type triterpenoid glycosides, sapibisides A and B (1 and 2), together with 12 related known analogues (3-14). The structures of these compounds were elucidated by extensive analysis of HRESIMS, 1D and 2D NMR spectroscopic data and comparison with previously reported data. The inhibitory activities of compounds 1-14 against LPS-induced NO production in RAW264.7 macrophages were evaluated. Compounds 1, 3, 9, and 13 exhibited moderate inhibitory activity, with IC50 values ranging from 31.2 to 45.7 μM, compared to the positive control, dexamethasone, which showed an IC50 value of 13.6 μM.
This study investigates the therapeutic effects and mechanisms of Guomin decoction (GMJ) on atopic dermatitis (AD). Animal and cellular experiments revealed that GMJ reduces ear swelling and collagen loss in AD-affected mice, modulates inflammatory factors, and inhibits M1 polarization while promoting M2 polarization. Mechanistic studies indicate that GMJ restores the M1/M2 balance in macrophages by dual regulation of the MAPK/NF-κB and JAK-STAT pathways, thereby improving AD.
A new diketomorpholine, myromopholine A (1), was isolated from the wetland fungus Myrothecium gramineum (ZLW0801-19). Through extensive spectroscopic analyses, including IR, MS, NMR, and X-ray single crystal diffraction, the planar structure and absolute configuration of the compound were determined, revealing the presence of a rare D-phenyllactic acid moiety. The investigation represents the first reported isolation of a diketomorpholine compound from the genus Myrothecium. Furthermore, it is the first identification of a diketomorpholine bearing a D-phenyllactic acid unit from a natural source, challenging the conventional understanding that such natural products exist exclusively as L-form derivatives.
Sixteen compounds, including two undescribed bisabolane-type sesquiterpenoids (1, 2), four aromatic derivatives (3-6), two cyclopeptides (7, 8), two acyclic sesquiterpenes (9-10), four fatty acid esters (11-14) and two fatty acids (15-16), were separated from the endophytic fungus Penicillium herquei. Their structures were established by analysis of spectroscopic data, HRESIMS spectra, NMR data and comparison with data in relevant literature. It is the first time that all of these compounds were isolated from P. herquei. The in vitro cytotoxicity of all isolated was evaluated against four tumor cell lines (HCT116, A549, HeLa, and Hepg2 cells) by the MTT assay, and compounds 1, 2, 4, 7 and 8 exhibited cytotoxicity with IC50 values ranging from 9.7 ± 0.8 to 37.4 ± 2.5 μM.
ABETRACTThree previously undescribed steroidal alkaloids, 20α-N,N-dimethylamino-2β-hydroxy-3α-senecioylamino-5α-pregnane (1), 20α-N,N-dimethylamino-2β,4α-dihydroxy-3α-senecioylamino-5α-pregnane (2) and 20α-N,N-dimethylamino-2β,15α-dihydroxy-3α-senecioylamino-5α-pregn-16-ene (3), were isolated from the whole plants of Sarcococca ruscifolia. Their structures were determined through the analysis of physiochemical properties and spectroscopic data. Compound 1 showed a certain inhibitory effect on human glioma U251 cells with an IC50 value of 13.51 μM.
Liver fibrosis may develop into cirrhosis and liver cancer, lacking effective approved treatments. Breviscapine extracted from Erigeron breviscapus possesses low toxicity and favorable pharmacokinetics, yet its anti-fibrotic mechanisms remain unclear. This study verified its protective effects on cell and rat fibrosis models. It suppresses HSC activation and ECM accumulation by inhibiting TGF-β1/Smad3 pathway, reversing EMT. Breviscapine is a promising candidate for hepatic fibrosis therapy.
Eighteen C19 aconitine-type derivatives were designed and syn-thesized with the modification of core active and strong toxicity components, such as yunaconitine (YA), mesaconitine (MA), and hypaconitine (HA) in Fuzi through hydrolysis and demethylation reactions. Their structures were confirmed by MS,1H NMR and 13C NMR. Isolated frog heart perfusion assay demonstrated that compound 18 exhibited excellent anti-heart failure activity with a cardiotonic rate of 103.14%. Its cardiotonic effect could be completely antagonized by nonselective calcium channel blockers, suggesting that the pharmacological effect of this compound is closely related to the calcium ion influx mechanism.
Microphthalmia-associated transcription factor (MITF) is a master regulator of melanogenesis but remains undruggable. We designed anthraquinone-2-carboxylic acid-based PROTACs; EF4 exhibited the most potent degradation in A375B16-F10 cells with minimal cytotoxicity. CETSA and proteasome inhibition assays confirmed target engagement, and molecular docking revealed a stable MITF-EF4-CRBN ternary complex. ADMET profiling showed favorable properties (MW 564.6, logP 2.62, bioavailability 0.55). Compared to E6, EF4 had fewer drug-likeness violations, better skin permeability (log Kp = -7.76 cm/s), and superior synthetic accessibility. These findings highlight EF4 as a promising lead for skin-targeted MITF degraders.
To explore the chemical constituents of Selaginella tamariscina and their effects on cancer cells, this study employed multiple chromatographic techniques including polyamide, silica gel, and semi-preparative High-performance liquid chromatography for compound isolation. The structures of the compounds were elucidated based on physicochemical properties and spectroscopic data. A pair of epimeric lignan glycosides, 7'R-tamariscinol U 4-O-β-d-glucopyranoside (1), 7'S-tamariscinol U 4-O-β-d-glucopyranoside (2) were obtained, along with two known compounds 3,5,7-trimethoxyflavone-4'-O-β-d-glucopyranoside (3) and selapeptin B (4). 1 and 2 are new, while the spectral data of 3 and 4 in methanol-d4 are reported for the first time.
Two previously undescribed cassane diterpenoids, caesmimo C3 (1) and caesmimo C8 (2), were isolated from the seeds of Hultholia mimosoides. Their structures were established by comprehensive spectroscopic analysis, and the absolute configurations were assigned from the electronic circular dichroism spectrum. Bioactively, compounds 1 and 2 exhibited significant cytotoxicity, inhibiting the cell viability of NRK-52E cells at a concentration of 50 μM.
We established in vivo models of hippocampal oxidative injury to investigate the protective effect of Angelica dahurica polysaccharide (ADP) on the hippocampus. ADP alleviated ovariectomized/D-Galactose (OVX/D-Gal)-induced hippocampal damage and enhanced antioxidant capacity (increased SOD/GSH-Px, decreased MDA). Additionally, ADP activated the Nrf2 pathway (upregulated Nrf2, downregulated NQO1/HO-1) and inhibited apoptosis (upregulated Bcl-2, downregulated Bax/cleaved caspase-3). Untargeted metabolomics revealed that ADP reversed seven oxidative stress-related metabolites, and pathway analysis implicated glycerophospholipid metabolism in its antioxidant mechanism. These results demonstrated that ADP protects against OVX/D-Gal-induced hippocampal oxidative injury by activating Nrf2, enhancing antioxidant capacity, inhibiting apoptosis, and regulating glycerophospholipid metabolism.
Osteoporosis is characterized by excessive bone resorption due to aberrant osteoclast activation. This study investigated the effects of Lobelia chinensis extract (L.C.) on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis. L.C. significantly inhibited TRAP-positive multinucleated osteoclast formation from bone marrow-derived macrophages without cytotoxicity. Mechanistically, L.C. suppressed RANKL-induced phosphorylation of JNK, IκB, Btk, and PLCγ2, but not p38 or Akt, leading to down regulation of c-Fos, NFATc1, and osteoclast-specific genes (Trap, Oscar, Dcstamp, Itgb3, Atp6v0d2, Ctsk). L.C. did not affect mature osteoclasts function, indicating stage-specific inhibition. These findings suggest that L.C. as a potential anti-resorptive agent for osteoporosis.
In this study, the phytochemical profile of the roots of Nardostachys jatamansi was investigated, leading to the isolation of four iridoid glycosides, including three new compounds: 2"-acetyl-valerosidate (1), 3"-acetyl-valerosidate (2), 10-deoxy-sambucuside F-3"-acetyl (3), and one known compound: 7-deoxy-10-acetyl-loganic acid (4). Their structures were determined by UV, IR, HRESIMS, and NMR data. Screening for anti-hepatocyte injury activity was conducted, and compounds 1 and 3 exhibited significant protective activity.
Withaferin A (WA), a steroidal lactone from Withania somnifera, exerts multi-targeted anti-breast-cancer activity by modulating redox homeostasis, autophagy, and apoptosis. WA elevates reactive oxygen species, perturbs mitochondrial function, and suppresses NF-κB/STAT3 signaling, thereby inhibiting proliferation, epithelial-to-mesenchymal transition, metastasis, and breast cancer stem cell self-renewal. This review synthesizes preclinical and emerging clinical evidence from PubMed/MEDLINE, Scopus, Web of Science, Google Scholar, and ClinicalTrials.gov (January 2000-October 2025). Despite promising multi-pathway activity, limited oral bioavailability, model heterogeneity, and scarce human data hinder translation. Advanced nanoformulations and rigorously designed clinical trials are essential to realize WA's therapeutic potential.
Three undescribed compounds including (8S)-neonardochinone B (1), (2E,4E,6E)-4-methylocta-2,4,6-trienedioic acid (2) and narchinol D (3), along with three known sesquiterpenoids kanshone A (4), kanshone K (5) and kanshone L (6) were isolated from the roots of Nardostachys jatamansi. Their structures were elucidated by comprehensive spectroscopic analysis, including mass spectrometry (MS), infrared (IR) spectroscopy, and one- and two-dimensional nuclear magnetic resonance (NMR) spectroscopy. Notably, compounds 1, 2 and 6 demonstrated neuroprotective effects at 10 μM concentration against glutamate (Glu)-induced cytotoxicity in SH-SY5Y neuronal cells.
Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease lacking effective therapies. To investigate antifibrotic potential and mechanisms of kuwanon C, we evaluated its effects in bleomycin-induced IPF and TGF-β1-stimulated myofibroblast differentiation. Kuwanon C dose-dependently alleviated IPF, improved histopathological injury, reduced hydroxyproline accumulation and fibrotic marker expression, and suppressed TGF-β1-induced myofibroblast differentiation without cytotoxicity. Mechanistically, kuwanon C activated the Nrf2/HO-1/NQO-1 antioxidant pathway and attenuated oxidative stress, whereas Nrf2 silencing abolished these protective effects. These findings demonstrate that kuwanon C attenuates IPF by activating Nrf2 and inhibiting oxidative stress-driven fibroblast activation, highlighting its potential as a novel therapeutic candidate for IPF.
Phytochemical investigation of Ferula sinkiangensis K. M. Shen led to the isolation of 12 meroterpenoids, including three new compounds (1-3) and nine known compounds (4-12). Their structures were elucidated based on comprehensive spectroscopic data, including HRESIMS and 1D, 2D NMR analyses. All compounds were assayed in vitro for protective activities against acetaminophen (APAP)-induced hepatotoxicity at 10 μM. Compounds 2-6 and 9-12 experimentally exerted protective effects against APAP-induced HepG2 cell damage.
Clinacanthus nutans (CN), a traditional medicinal plant widely used in Southeast Asia, has gained attention as a potential nutraceutical and therapeutic agent due to its diverse phytochemical composition, including phenolics, flavonoids, terpenoids, phytosterols, and sulfur-containing compounds. Growing evidence indicates that CN modulates key molecular pathways related to oxidative stress, inflammation, immune regulation, and cellular metabolism, such as NF-κB, TLR4, Nrf2, and p38 MAPK. This review summarizes recent advances in its phytochemistry, extraction methods, and pharmacological activities. The therapeutic potential of CN is discussed in cancer, metabolic disorders, infections, and bone diseases. However, further studies on bioavailability, safety, and clinical validation are required.
Vascular dementia (VaD) is associated with chronic cerebral hypoperfusion, oxidative stress, mitochondrial dysfunction, and hippocampal neuronal senescence. Citronellal (CT) ameliorates cognitive impairment in 2VO-induced VaD rats. CT improved spatial learning and working memory, reduced in vivo oxidative stress, restored hippocampal dendritic spine density, upregulated hippocampal myelin basic protein (MBP), and decreased P-p53, p21, and SA-β-gal. CT also restored mitochondrial membrane potential and reduced Drp1/FIS1 expression. Mechanistically, CT suppressed TRPM2 and restored NMDAR1; TRPM2 deficiency weakened CT-mediated NMDAR1 regulation. These findings suggest that CT ameliorates VaD-related cognitive impairment by inhibiting hippocampal aging through TRPM2/NMDAR-associated oxidative stress-mitochondrial pathways.
