Interleukin (IL)-33, a member of the IL-1 cytokine family, plays a vital role in immune system regulation and inflammation, with oxidative stress being implicated in its expression. During the search for compounds from natural sources with potential as therapeutic agents for allergic diseases via IL-33 signal modulation, we discovered significant IL-33 inhibitory activity in the methanol extract of Canavalia gladiata (sword bean) pods. Through chromatographic separation and liquid chromatography–mass spectrometry, we isolated 11 compounds (1–11) from the methanol extract. Furthermore, we assessed the inhibitory effects of these substances on IL-33/ST2 signaling in processes related to inflammatory and autoimmune diseases using an enzyme-linked immunosorbent assay. Among them, compounds 7, 10, and 11 exhibited substantial IL-33 inhibitory efficacy, with values reaching 78%, 86%, and 79% at 100 µM, respectively. Remarkably, compounds 7, 10, and 11 demonstrated significant and dose-dependent inhibition of IL-33 signaling at concentrations of 10, 50, and 100 µM. Computational molecular docking and dynamic simulations further elucidated the underlying mechanisms. These findings have promising pharmacological implications for allergy prevention and treatment associated with flavonoid glycosides derived from C. gladiata.
Gnetum formosum Markgr., a member of the Gnetaceae family, is distributed in Vietnam. This plant remains a botanical enigma with an unexplored diversity of chemical constituents and pharmacological effects. In this study, two new steroidal saponins, namely gnetumosides A (1) and B (2), were isolated from the aerial parts of G. formosum. Their chemical structures were elucidated using spectroscopic techniques, including high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) and NMR, along with chemical hydrolysis and comparison with the reported literature. The potential anti-inflammatory effects of the isolated compounds were evaluated by measuring lipopolysaccharide-stimulated nitric oxide (NO) production in murine macrophage cells. Notably, compound 1 exhibited the most potent inhibitory activity (IC50 = 14.10 ± 0.75 µM), comparable to dexamethasone. Additionally, the mechanisms underlying the observed anti-inflammatory effects were investigated through molecular docking and molecular dynamics simulations on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins. This study is the first to investigate the chemical constituents and pharmacological effects of G. formosum.
Polygala tenuifolia, known as Yuan Zhi in traditional Chinese medicine and Viễn Chí in Vietnamese medicine, is renowned for its cognitive-enhancing and anti-inflammatory properties. Phytochemical investigations of its roots have led to the isolation of four oleanane-type triterpenoid saponins (1–4). Using sophisticated analytical techniques, such as electrospray ionization mass spectrometry (ESI-MS) and both 1D and 2D nuclear magnetic resonance (NMR) spectroscopy, the structures of these compounds were elucidated. The identified compounds were polygalasaponin XXVIII (1), onjisaponin B (2), desacylsenegasaponin B (3), and platycodin D (4). The acetylcholinesterase (AChE) inhibitory activities of these compounds were tested, revealing that compound 1 exhibited an IC50 value of 12.3 ± 1.6 μM, which is relatively higher than that of the positive control, tacrine (IC50 = 3.2 ± 1.8 μM). To further investigate the underlying mechanisms of AChE inhibition, molecular docking studies were performed. These findings validate the potential of P. tenuifolia as an AChE inhibitor through its triterpenoid saponin constituents. However, in vivo studies are crucial to confirm its therapeutic potential and explore its clinical applications.
A special alkaloid compound known as capsaicin, which can only be found in the fruit of the Capsicum plant, was isolated and tested for its anti-inflammatory activity. The purpose of this work is to establish a simple and quick approach for capsaicin purification utilizing centrifugal partition chromatography (CPC) as well as an effective method - accelerated solvent extraction (ASE), for extracting capsaicin from Capsicum chinense. After purification, capsaicin was validated by HPLC-DAD at 281 nm to be > 90% purity. The in vivo anti-inflammatory activity of the isolated capsaicin was also investigated, and the IC50 value of the capsaicin was determined to be 57.61 µg/mL. The current work emphasizes how an ASE and CPC system may combine to extract high-purity capsaicin from Capsicum chinense, which have the anti-inflammatory activity, as we evaluated in the experiment.
27 June 2025 in Tạp chí Nghiên cứu Khoa học và Phát triển
Bitter melon (Momordica charantia) is a traditional medicinal and functional food highly valued for its diverse pharmacological properties, including anti-inflammatory, anti-diabetic, and antioxidant effects. Phytochemical studies of the fruits of M. charantia led to the isolation of three triterpenoid saponins (1-3). Their structures were elucidated using spectroscopic data, including HR-ESI-MS, 1D and 2D NMR, as well as comparison with reference compounds. In particular, their compounds were identified as 3β-malonyl-7β,23-dimethoxycucurbita-5,24-dien-19-al (1), 3β-malonyl-7β-hydroxy-25-methoxycucurbita-5,23-dien-19-al (2), and 3β-malonyl-7β,25-dihydroxycucurbita-5,23-dien-19-al (3), respectively. To evaluate the anti-inflammatory potential of these substances, the production of pro-inflammatory cytokines—IL-6, IL-12p40, and TNF-α—was tested in LPS-stimulated bone marrow-derived dendritic cells (BMDCs). The data showed that the activity of compound 1 was higher than that of the selected drug adezmapimod, which served as the positive control. The findings suggest the potential in vitro anti-inflammatory effects of secondary metabolites from M. charantia. However, further investigations, including in vivo and in silico studies, are necessary to verify the therapeutic anti-inflammatory potential of these chemical constituents.