Arnebiae Radix is a traditional Chinese medicine, and its active constituent shikonofuran exhibits a broad spectrum of pharmacological activities. In this study, shikonofuran derivatives were designed and synthesized, and their hepatoprotective effects were evaluated using the MTT assay in a HepG2 cell injury model. The results showed that compound 10b, bearing a lipoic acid moiety, displayed superior activity compared with the positive control bicyclol. This study provides experimental evidence for further investigation of these compounds and the development of hepatoprotective leads.

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.

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.

This study established a Caco-2/HT29 co-culture intestinal epithelial model to systematically investigate the intestinal absorption and transport mechanisms of cinnamic acid (CA). The results indicate that CA enhances intestinal barrier integrity by regulating the expression of tight junction proteins and promoting the secretion of neutral mucus, and significantly increases the intestinal absorption rates of alkaloids (sinomenine hydrochloride, SH), monoterpenes (paeoniflorin, PF), saponins (glycyrrhizic acid, GA), and flavonoids (liquiritin, LQ). These findings provide experimental evidence supporting the use of CA as a natural permeation enhancer to improve oral bioavailability.

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.

Four undescribed compounds, including one new sesquiterpene lactone (1, coriarilactone A), two new phenylpropanoid glycosides (2 and 3, corianosides A and B), and one new coumarin (4, coriacoumarin A), together with five known sesquiterpenes, were isolated from the leaves of the toxic medicinal plant Coriaria nepalensis. The structures of 1-4 were elucidated through a combination of extensive NMR spectroscopic analysis, HRESIMS, and X-ray crystallography. Notably, compounds 2-3 possess a rare heptose moiety, which were isolated from the Coriariaceae family for the first time. Compound 1 exhibited potential neuroprotective activity. All compounds showed no convulsant neurotoxicity and no remarkable inhibitory activity toward four human cancer cell lines.

Herein, we disclosed a concise total synthesis of indole alkaloid coerulescine via a novel copper(I)-catalyzed tandem reaction of chiral tert-butanesulfinyl amide o-iodoanilide derivative with methyl chloroformate as the electrophile reagent to afford the quaternary carbon stereocenter efficiently, followed by hydrolysis of the tert-butanesulfinyl group and a tandem ammonolysis process to give the key spiro[pyrrolidine-3,3'-oxindole] core of the coerulescine alkaloids.

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,[1]H NMR and [13]C 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.

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.

A new coumaronochromone (1), and 12 known compounds (2-13) were isolated from the ethyl acetate part of an aqueous EtOH extract of Suaeda glauca. Compounds 5-8 and 12 effectively ameliorated pericardial edema and venous congestion in zebrafish embryos induced by verapamil hydrochloride at 50 μM. Among these, 8 exhibited superior efficacy in reducing pericardial edema compared to the positive control, Digoxin. In contrast, 1-3 displayed significant lethality in zebrafish embryos, with LC50 values of 9.41, 39.59, and 24.47 μM, respectively. Furthermore, these three compounds showed potential cytotoxic effects on HCT116 cells at 30 and 50 μM.