Jul 2026· Fitoterapia· Vol 193, pp.
107402
· 0 citations
Medicine
TL;DR
It is demonstrated that diarylheptanoids are the major anti-inflammatory components in A. maximum fruits, which not only validates the ethnopharmacological use of this herb, but also provides new anti-inflammatory agents derived from natural products.
Abstract
The fruits of Amomum maximum Roxb. (Zingiberaceae), traditionally used for gastrointestinal disorders, have been less phytochemically investigated compared to its rhizomes. In this study, four undescribed compounds (1-3,12) together with 15 known compounds were isolated from a 75% ethanol extract of A. maximum fruits, including eleven diarylheptanoids and eight labdane diterpenes. Their structures were unequivocally elucidated by spectroscopic methods, including NMR spectroscopy, computational NMR methods, and ECD. Compounds 1, 3-6, 10, and 11 significantly inhibited the release of NO, IL-6, and TNF-α in LPS/IFN-γ-stimulated RAW 264.7 macrophages. Furthermore, the integration of network pharmacology, molecular docking, and molecular dynamics simulations identified compounds 1, 3-6, 10, and 11 as promising candidates, demonstrating favorable binding affinity and stability with the active target AKT1. This study demonstrates that diarylheptanoids are the major anti-inflammatory components in A. maximum fruits, which not only validates the ethnopharmacological use of this herb, but also provides new anti-inflammatory agents derived from natural products.
Ligusticum wallichii Franch., an oriental medicinal herb widely used throughout East Asian countries, is well recognized for its therapeutic potential in treating cardiovascular, inflammatory, and neurodegenerative diseases. In this study, phytochemical investigation of the methanol extract of L. wallichii roots led to the isolation and structural elucidation of four previously undescribed compounds (1-4), and eight known analogues (5-12). Their structures were determined through extensive spectroscopic analyses, including 1D and 2D NMR, HR-ESI-MS, and CD spectroscopy, supported by quantum chemical ECD calculations. All isolated compounds were evaluated for anti-inflammatory and cytotoxic activities. Compounds 1, 3, 7, 9, and 12 significantly inhibited nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages. Regarding pro-inflammatory cytokine modulation, compounds 1, 9 and 12 significantly reduced both TNF-α and IL-6 levels by more than 40% at 10 μM. Moreover, compounds 2, 3, 5-7, and 9 showed significant cytotoxic activity with IC50 values ranging from 2.8 to 13.2 μM. Mechanistic investigations in PC9 cells revealed that the cytotoxic effects of selected compounds (2, 3, 5-7, 9) were mediated via apoptosis induction. Their dual functional properties position them as promising anti-inflammatory and anti-cancer agents, which prompt further research and potential following development step in targeting inflammation-associated cancer.
Ninh Khac Thanh Tung, Nguyễn Thị Tú Oanh, T. H. Giáp et al.· Phytochemistry· 0 citations
Vaccinium macrocarpon (American Cranberry) fruit is processed to make juice, supplements, and other edible products, leaving pomace as a sidestream that contains secondary metabolites with potential anti-inflammatory and anti-proliferative activities. Ultrasound-assisted extraction and chromatographic methods were developed to prepare an extract (POM-ACE) and fractions rich in pentacyclic triterpenoids and phytosterols for bioactivity evaluation. These were characterized using UPLC-MS and GC-MS. Anti-inflammatory effects were assessed in a human monocyte (THP-1) model, identifying several fractions containing triterpenoids and sitosterol that significantly inhibited IL-1β expression. Molecular docking indicated favorable interactions of these components with NLRP3, suggesting a possible modulation of inflammasome. Fractions rich in ursolic acid (UA) and oleanolic acid (OA) and their p-hydroxycinnamic acid (HCA) esters also showed mild concentration-dependent inhibition of lipoxygenase (LOX) activity. Pearson correlation analysis identified strong positive correlations between UA, OA, and their trans-HCA esters with LOX inhibition. Anti-proliferative activity was assessed in HT-29 colon adenocarcinoma cells using MTT, with several fractions exhibiting moderate concentration-dependent activity (IC50 = 12–17 µg/mL). PLS regression analysis supported significant contributions by UA, OA, and their HCA esters. Flow cytometry experiments demonstrated that cell death occurs in part through apoptosis; the role of apoptosis was further supported by favorable molecular docking interactions between pomace triterpenoids and caspases-3 and -9. These findings suggest that cranberry pomace is a promising source of triterpenoids and phytosterols with anti-inflammatory and anti-proliferative properties.
Seven previously undescribed compounds comprising four diterpenoids (1-4), two sesquiterpenoids (5, 6), and one polyketide (7), together with four known diterpenoids (8-11), were isolated from Callicarpa longifolia Lamk. var. floccosa Schauer. Their structures and absolute configurations were established using HRESIMS, UV, IR, NMR and ECD calculations. All isolated compounds (1-11) were evaluated for anti-inflammatory activity by LPS-induced RAW264.7 cells. While all compounds inhibited nitric oxide (NO) release to varying degrees, callilongiflocin A (1) exhibited the most potent effects, significantly suppressing the production of NO, pro-inflammatory cytokines interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and the overexpression of inducible NO synthase (iNOS) in a concentration-dependent manner. Proteomics sequencing revealed that compound 1 modulates IL-17 and TNF signaling pathways. This regulation was further validated by Western blotting, demonstrating 1's inhibition of the common downstream mitogen-activated protein kinase (MAPK) pathway. Furthermore, in an IL-17A plus TNF-α-induced keratinocyte HaCaT model of psoriasis, compound 1 effectively suppressed the inflammatory cytokine IL-6, C-C motif chemokine ligand 20 (CCL-20), and the protein expression of intercellular cell adhesion molecule-1 (ICAM-1), suggesting its potential anti-psoriatic activity.
Ting Liu, Xiao-Lu Wu, Lianchun Li et al.· Phytochemistry· 0 citations
The genus
Pereskia
comprises leafy cacti with food and medicinal applications, notably
Pereskia aculeata
Miller, for which preclinical anti-inflammatory and immunomodulatory effects have been reported. This review summarizes the available evidence and integrates findings on phytochemicals and their mechanisms. Phytochemical investigations have reported phytosterols, flavonoids, phenolic acids, terpenoids, and polysaccharides in this species. Among the constituents reported in
P. aculeata
, β-sitosterol, stigmasterol, taraxasterol, and cynaroside are plausible contributors to the observed anti-inflammatory effects; however, their individual contributions within the extracts have not been fully established. A hexane fraction exhibited topical anti-inflammatory activity comparable to that of dexamethasone in specific cutaneous models, whereas ethanolic and petroleum ether extracts modulated the p38/MK2/TTP pathway and attenuated adjuvant-induced arthritis in rats. Cynaroside reduced IL-6 levels, COX-2 expression, and COX-2 enzymatic activity. Further studies using standardized preparations and clinically relevant models are warranted to confirm these effects and advance their therapeutic application.
L. L. Fernandes, Guilherme Otoni Francisco, Wilson R. Cunha et al.· Natural Product Communicatio...· 0 citations
A phytochemical investigation of Manglietia chevalieri (Magnoliaceae), an ornamental species has remained largely unexplored for its chemical constituents and pharmacological potential, led to the isolation and identification of 51 structurally diverse compounds. These include 20 phenylpropanoids, 12 terpenoids, and 19 alkaloids. Among them, 14 previously undescribed structures, named manglianins A-N (1-11, 12b, 13, 14), were characterized. Notably, the 3,3'-biphenyl neolignans 1-3 feature unprecedented fusions with an additional C2 or C3 unit, leading to the formation of dioxane or benzofuran rings. Compound 13 is the first sesquiterpenoid featuring a rare 3-oxabicyclo[3.3.0]octane ring. The undescribed structures and their absolute configurations were determined by extensive spectroscopic data analysis, computational calculations, and the modified Mosher's method. Given the role of chronic inflammation in driving idiopathic pulmonary fibrosis (IPF), all isolates were initially evaluated for their anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophages by measuring the mRNA expression levels of CCL-2, IL-1β, and IL-6. At 1 μM, 17 isolates reduced expression of the three cytokines by more than 50%. Notably, compounds 14, 15, 28, and 40 retained significant anti-inflammatory effect at concentrations as low as 0.1 μM. Subsequent anti-fibrotic assays evaluating the expression of fibrosis markers (collagen I, fibronectin, and α-SMA) identified compounds 14, 28, 31, 33, and 40-43 as potential anti-IPF agents.
Zi-Jie Long, Mao-Mao Zheng, Yuhang He et al.· Phytochemistry· 0 citations
A phytochemical investigation of the stems of Dendrobium nobile Lindl. led to the isolation of six nitrogen-containing compounds, including one previously undescribed quinoline–aspartic acid hybrid alkaloid, dendronobiline A (1), together with five known alkaloid-related constituents (2–6). The structure of compound 1 was elucidated by comprehensive spectroscopic analyses, including HRESIMS, 1D and 2D NMR experiments, and its absolute configuration was assigned by comparison of experimental and calculated ECD spectra. Structurally, compound 1 features a quinoline-derived unit connected to a dimethyl aspartate moiety through an amide linkage. All isolated compounds were evaluated for their inhibitory effects on LPS-induced nitric oxide production in RAW264.7 macrophages. Among them, compound 1 displayed the most potent anti-inflammatory activity, with an IC50 value of 9.05 ± 1.60 μM, comparable to that of the positive control dexamethasone. These findings enrich the chemical diversity of D. nobile alkaloids and suggest that its stems are a promising source of anti-inflammatory natural products.
Jing-Yi Yue, Yu-Jia Lu, Yang Yu et al.· Records of Natural Products· 0 citations
