Journal of Asian Natural Products Research最新文献

Three new neo-clerodane diterpenoids, named scuregeliolides A-C (1-3), were isolated from the whole plant of Scutellaria regeliana. Their chemical structures, including absolute stereochemical configurations, were fully elucidated by means of integrated spectroscopic techniques and Electronic Circular Dichroism (ECD) calculations. In vitro, three undescribed neo-clerodane diterpenoids showed significant anti-inflammatory activities due to inhibiting the release of TNF-α, IL-6 and IL-1β in the LPS-induced RAW264.7 cells, as well as preventing the release of β-glucuronidase from the PAF-stimulated PMNs.

Glutinol (GT), a major triterpenoid component of Orostachys japonica, suppresses TGF-β-induced epithelial-mesenchymal transition (EMT) in human cancer cells. GT treatment restored epithelial characteristics by upregulating E-cadherin and downregulating Snail, thereby reducing cancer cell migration and invasion in A549 and MCF-7 cells. In vivo, GT significantly inhibited lung metastasis of TGF-β-treated A549-luc cells in mice. These findings demonstrate that GT exerts potent anti-metastatic effects through modulation of the TGF-β/Snail/E-cadherin signaling axis, highlighting its potential as a natural therapeutic agent against cancer metastasis.

Rutin, a dietary flavonoid, can relieve insulin resistance to improve hyperglycemia, while the precise mechanism remains unclear. In this study, we found that rutin bound well to the insulin receptor, alleviated glucosamine-induced insulin resistance in HepG2 cells and observably increased glucose consumption and glucose uptake in vitro. Furthermore, rutin increased the levels of IRS-1, IRS-2, PI3K, p-AKT, p-GSK3β and p-FOXO1 and decreased the expression of p-IRS-1, p-GS, PEPCK and G6Pase, indicating that rutin could promote glycogen synthesis and inhibit gluconeogenesis via the IRS/PI3K/Akt signaling pathway. Overall, the findings confirmed that rutin potentially mitigates glucosamine-induced insulin resistance in hepatocytes via activation of IRS/PI3K/Akt pathways.

Two previously undescribed macrocyclic diterpenoids, cycloserratol (1) and isopapyrifuranol A (2) were isolated from the gum resin of Boswellia seratta. Compound 1 was confirmed as trihydroxy substituted 12-membered macrocyclic cembrane-type diterpenoid skeleton and 2 was a new 1,12-oxygen fused trihydroxy cembrane skeleton. The structures of these new metabolites were characterized by HRESIMS, 1D NMR and 2D NMR analysis.

N-(4-Guanidinobutyl)-2-(4-hydroxyphenyl)-2-oxoacetamide (C1), a marine-derived leonurine analogue, was synthesized via a six-step route with 38% total yield. Biological evaluation demonstrated potent anticoagulant activity through significant prolongation of APTT (20 mM) and PT (5 mM). C1 dose-dependently (100-200 μM) suppressed LPS-induced NO production in RAW 264.7 macrophages without cytotoxicity and modulated phagocytosis. In LPS-induced acute lung injury rats, C1 reduced proinflammatory cytokines in BALF. These findings highlight C1's dual anticoagulant and anti-inflammatory properties as a promising lead compound.

Multiple sclerosis (MS) is an autoimmune-mediated, heterogeneous, multifactorial central nervous system degenerative disease influenced by genetics and environment. Ferroptosis, an iron-dependent lipid peroxidation/reactive oxygen species-induced programmed cell death, exacerbates MS pathology. Glutathione peroxidase 4 (GPX4) regulates ferroptosis by clearing peroxides to sustain cells. Targeting GPX4-mediated ferroptosis, especially via safe, potent natural compounds, is a promising MS treatment. This review explores GPX4-dependent ferroptosis's role in MS progression and summarizes natural compounds for MS therapy.

Two new (1-2) and five known (3-7) dihydro-β-agarofuran derivatives were isolated from the roots of Tripterygium wilfordii. The structures of new compounds were elucidated by spectroscopic techniques, such as UV, IR, HRESIMS and NMR. And the structure of compound 1 was confirmed by X-ray crystallographic. Cytotoxic activity assays against four human tumor cell lines (SK-MEL-2, HCC1806, HUH-7, PANC-1) were assessed for compounds 1-7. Compound 2 exhibited pronounced cytotoxicity against SK-MEL-2 cells with an IC₅₀ value of 9.18 μM. Additionally, compound 5 showed significant cytotoxic effects on SK-MEL-2 and HCC1806 cells with IC₅₀ values of 4.59 μM and 8.14 μM, respectively.

Four new compounds (1-4), along with 22 known metabolites (5-26), were isolated from the fungus Biscogniauxia sp. 8703. The structures of the new compounds were elucidated based on NMR, MS, and ECD analysis. Compounds 1 and 2 were identified as heliannuol D analogs, which exhibited anti-inflammatory activity by inhibiting NO production in LPS-induced RAW 264.7 cell, with IC₅₀ values of 7.14 and 25.25 μM, respectively.

Two novel polyacetylenic compounds were successfully separated from the dichloromethane extract of the aerial parts of Bidens parviflora Willd., known for its ethnomedicinal use in traditional Dai medicine. These compounds were structurally elucidated and identified as (2R)-trideca-3E,5Z,11E-triene-7,9-diyne-1,2,13-triol (1), and (2R)-trideca-11E-ene-5,7,9-triyne-1,2,13-triol (2). Their chemical structures were confirmed through a comprehensive analysis involving ultraviolet (UV) spectroscopy, infrared (IR) spectroscopy, high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), as well as detailed one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) spectroscopic data, and measurements of specific optical rotation.

A newly discovered chloroisosulochrin derivative, involving demethychloroisosul (1), and a novel chromone metabolite, reduchromone (2), were extracted from Penicilium sp., an endophytic fungus residing in Rhododendron molle. The structures of these compounds were elucidated through a comprehensive analysis of their 1D and 2D NMR and HRESIMS data. In addition, the X-ray diffraction analysis of demethychloroisosul (1) is the first example to confirm the structure of chloroisosulochrin by single-crystal data. Notably, demethychloroisosul (1) exhibited moderate cytotoxic efficacy against HepG2 liver cancer cells, with a half-maximal inhibitory concentration value of 30.18 μM.