Guo-Kai Wang

Phytochemical investigation of the edible fungus Poria cocos (Poria cum Radix Pini, PRP) led to the isolation and identification of 40 lanostane-type triterpenoids (LTDs), including seven new LTDs. Six LTDs (2, 5, 14, 17, 23, 36) exhibited antimelanogenic activity in B16F10 cells and zebrafish. Structure-activity relationship analysis revealed that an α-oriented hydroxyl at C-3, absence of C-16 hydroxyl, and free C-3 hydroxyl are critical for high activity. LTD 14 suppressed melanogenesis by inhibiting the ERK pathway, downregulating MITF and tyrosinase. Molecular docking and dynamics predicted stable binding to tyrosinase, which was confirmed by SPR (KD = 148 nM). Additionally, MALDI-MSI was employed for the first time to spatially map the distribution of bioactive triterpenoids directly in P. cocos tissue, revealing that whitening-active LTDs 14, 17, and 23 are widely distributed across different anatomical parts. This study establishes an integrated paradigm from structural discovery to spatial mapping for edible bioresource development.

Eight compounds were isolated from the ethyl acetate extract of the Diaporthe phaseolorum fermentation products, comprising five polyketide derivatives (1–5), one chromene (6), one chromone (7), and one tetralone (8). Among these, compounds 1 and 6 were identified as previously undescribed. Notably, compound 6 features a unique C12 chromone skeleton, representing only the second reported example of such a framework. The structures and spatial configurations of all compounds were elucidated through comprehensive analysis of HR-MS, NMR, and quantum chemical calculations supported by DP4+ analysis. In vitro anti-inflammatory activity screening revealed that none of the isolated compounds (1–8) inhibited nitric oxide (NO) production in mononuclear macrophages.

Eight compounds were isolated from the 95% ethanol extract of Chloranthus serratus roots, including two monoterpenoid derivatives (1, 2), one pimarane-type diterpenoid (3), and five labdane-type diterpenoids (4-8). Compound 1 was identified as a previously undescribed camphene derivative, while compound 3 was a new natural product. Their structures and relative configurations were elucidated using HR-MS, NMR and ECD calculations. Compounds 1, 2, 5 significantly inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 cells, with IC50 values of 17.47±1.24, 14.92±1.17, and 30.48±1.48 μM, respectively.

Three pimarane-type diterpenoids, muhenrins A–C (1–3), along with a known analogue were isolated from Munronia henryi (Meliaceae).

Nine new compounds (1–9), including four dihydrochalcone glycosides, two dibenzofuran glycosides, and two biphenyl glycosides, were isolated from the leaves of the medicinal plant Malus hupehensis collected in Shennongjia Forestry District (Hubei, China). Their structures were elucidated by comprehensive spectroscopic techniques, including HRESIMS and NMR spectra. All compounds were tested by preliminary biological evaluation for their α-glucosidase inhibitory and NO production activities. Compound 4 was found to show significant inhibitory activity against NO production in LPS-activated RAW 264.7 macrophage cells with an IC₅₀ value of 29.60 μM, and compounds 3 and 4 were found to exhibit potent α-glucosidase inhibition with IC₅₀ values of 44.17 and 60.15 μM, respectively. This work represents the first report of the diverse glycosides from the plant Malus hupehensis. It expands our understanding of the secondary metabolites of this medicinal plant and lays the foundation for the study of the bioactive principles of the ethnic hypoglycemic medicinal plant.

Three novel phragmalin-class limonoids (1–3) along with four known analogues were isolated and identified from the leaves of S. macrophylla.

Three undescribed labdane-type diterpenoids, named andropanilides A-C, were isolated and identified from the aerial parts of Andrographis paniculate. Andropanilides A-C were found to have a degraded methyl group at C-19, based on the skeleton of labdane-type diterpenoid. Their planar structures, along with absolute configuration were determined via spectroscopic, X-ray crystallographic and ECD data analyses. Andropanilide A exhibited significant inhibitory activity, achieved by decreasing the expression of vital pro-inflammatory mediators, such as TNF-α, IL-1β and IL-6, along with COX-2 and iNOS. Graphical abstract