Jiangsu Kanion Pharmaceutical Co., Ltd.

Natural terpenes found in essential oils (EOs) have shown promise as penetration enhancers (PEs) in pharmaceutical and cosmetic formulations. This study compared the skin penetration enhancement properties of sesquiterpenes and monoterpenes from galangal EO (GEO), e.g. δ-cadinene, β-caryophyllene, caryophyllene oxide (CPO), 4-terpineol, β-pinene, and 1,8-cineole. Results indicated that the sesquiterpenes, particularly δ-cadinene, significantly improved the skin permeation of rhodamine B compared to monoterpenes. Electrical resistance measurements of the skin, DSC and XRD analysis revealed that the sesquiterpenes notably disturbed the ordered arrangement of stratum corneum (SC) components including lipids and keratins. Additionally, the results of molecular docking also revealed that sesquiterpenes were easily combined with transient receptor potential vanilloid 4 (TRPV4) ion channel. The cutaneous TRPV4 ion channel, which played a role in tight junction (TJ) formation in keratinocytes, were abundantly expressed in rat abdominal skin. δ-Cadinene, specifically, exhibited an agonistic effect on the cutaneous TRPV4 ion channel, significantly enhancing its SC retention and facilitating in vivo skin permeation of rhodamine B. In summary, the penetration enhancement mechanism of sesquiterpenes from GEO, particularly δ-cadinene, includes acting on SC components and activating the cutaneous TRPV4 ion channel.

Four previously unreported phenylpropanoid glycosides (1-4), together with four known analogues (5-8), were isolated from the leaves of Illicium dunnianum. The structures of these new compounds were elucidated based on spectroscopic analysis (HR-ESI-MS, NMR, IR, UV) and chemical methods. In addition, the neuroprotective activities of all the isolates were evaluated by measuring their cell viability in H₂O₂-induced OLN-93 cell injury model.

A novel acidic polysaccharide, ATP-4, was isolated from Amomum tsao-ko and demonstrated immunomodulatory potential in the immunosuppressed mouse model and cellular assays. Structural characterization via monosaccharide analysis and gel permeation chromatography revealed ATP-4 as a heteropolysaccharide (4.23 × 10⁴ Da), composed of Rha, GalA, Glc, Gal, Xyl, and Ara in a molar ratio of 9.03:52.37:7.89:12.34:6.47:11.89. Integrated analysis of conventional techniques (PMP-HPLC, GC-MS, and NMR) and UPLC-Orbitrap-MS/MS profiling of free radical-degraded components (AO-1/2/3) elucidated its unique repeating units, which are characteristic of a novel polysaccharide assembled through specific patterns between the HG regions and branched domains such as GRP, RGP, etc. In vitro and in vivo studies demonstrated ATP-4's dual mechanisms: direct immune cell activation and indirect gut microbiota modulation. Notably, active structural domains AO-2 (the nonlinear branched region of ATP-4) significantly induced cytokine production at a lower concentration, guiding activity-directed enzymatic modification of ATP-4. The optimized derivative, ATP-4e, maintained a nonlinear branching structure while demonstrating enhanced immunoregulatory capacity, improved conformational flexibility, and superior physicochemical properties compared to the native ATP-4. This study establishes an integrated degradation-analysis-modification paradigm for polysaccharide research and provides a methodological framework for elucidating structure-activity relationships of traditional Chinese medicine polysaccharides.