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Background: Panax ginseng has been used as a traditional medicine for various pathological conditions. Ginsenoyne C (GSC) is a polyacetylene, minor constituent. Objective: The objective of the present study was to determine the anti-inflammatory activities of GSC for the protection of inflammation. Materials and Methods: The effects of GSC on cell viability and nitric oxide (NO) production in lipopolysaccharide (LPS)–induced RAW 264.7 cells were investigated through MTT assay and the Griess reaction, respectively. The levels of inflammatory cytokines such as interleukin (IL-1β) and IL-6 and inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2), and pERK were measured using enzyme-linked immunosorbent assay and Western blot analysis, respectively. Results: GSC suppressed NO production in LPS-induced RAW 264.7 cells. GSC suppressed the production of inflammatory mediators through downregulating phosphorylation of extracellular regulated kinases signaling in LPS-induced RAW 264.7. Conclusion: GSC has a potential therapeutic agent for protection of inflammation. Abbreviation used: CCK: Cell counting kit; COX-2: Cyclooxygenase-2; ELISA: Enzyme linked-immunosorbent assay; ERK: Extracellular regulated kinases; FBS: Fetal bovine serum; FEG: Fermented ginseng extract; GSC: Ginsenoyne C; IL: Interleukin; iNOS: Inducible nitric oxide synthase; LPS: Lipopolysaccharide; MAPK: Mitogen-activated protein kinases; NO: Nitric oxide; PVDF: Polyvinylidene difluoride; SDS-PAGE: Sodium dodecyl sulfate-polyacrylamide gel electrophoresis [ABSTRACT FROM AUTHOR]

Morus bombycis Koidzumi, commonly known as silkworm mulberry, is a plant belonging to family Moraceae. It has been used in Asian countries as a traditional medicine for treating hypertension, diabetes, and inflammatory disorders. In this study, we isolated eleven compounds from the cortex of M. bombycis and evaluated their inhibitory effects on nitric oxide (NO) production as an indicator of their anti-inflammatory activities using lipopolysaccharide (LPS)-stimulated murine macrophages. Compound 4 showed the most potent inhibitory activity on NO production. It was identified as mulberrofuran K (MFK). Anti-inflammatory activity of MFK was then carried out using LPS-stimulated RAW264.7 cells. MFK suppressed the production of NO, reactive oxygen species (ROS), and proinflammatory cytokines (interleukin (IL)-1β, IL-6 and tumor necrosis factor alpha (TNF-α)) in a concentration-dependent manner. Western blot analysis revealed that MFK treatment inhibited expression levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). MFK also inhibited transcriptional activation of nuclear factor-κB (NF-κB) and extracellular-regulated kinases (ERK) 1/2 in LPS-stimulated murine macrophages. These results suggest that MFK, an anti-inflammatory constituents of M. bombycis cortex, has potential as a therapeutic candidates for preventing and treating inflammatory diseases. [ABSTRACT FROM AUTHOR]

Abstract: Two bioactive phloroglucinol derivatives, dioxinodehydroeckol (DHE) and phlorofucofuroeckol A (PFF-A) were isolated from edible marine brown alga, Ecklonia stolonifera, and evaluated for effects on cell surface FcεRI expression in KU812F cells. DHE and PFF-A were found to reduce the cell surface expression, and total cellular protein and mRNA levels for the FcεRI α chain. Moreover, both compounds exerted inhibitory effects against the elevation of intracellular calcium concentration [Ca2+] i and histamine release from anti-FcεRI α chain antibody (CRA-1)-stimulated cells. These inhibitory effects were stronger for PFF-A than for DHE. These results show that two phloroglucinol derivatives, DHE and PFF-A, may exert anti-allergic effects via the inhibition of FcεRI expression, calcium influx, and degranulation in basophils, and contributes to the pharmacological activities of marine brown alga, including E. stolonifera. [Copyright &y& Elsevier]

Abstract: Basophils and mast cells express FcεRI, a high-affinity receptor for IgE, on the cell surface and act as effector cells in allergic reactions. In this study, we investigated the inhibitory effect of Ecklonia cava (EC) methanolic extract on the expression of FcεRI in human basophilic KU812F cells. Flow cytometric analysis revealed that EC extract caused a concentration-dependent reduction in the cell surface expression of FcεRI. The extract was also capable of reducing the binding between IgE or serum IgE and cell surface FcεRI. RT–PCR analysis revealed that EC extract reduced the mRNA expression of total cellular FcεRI α-chain. Moreover, data obtained by fluorescence spectrophotometry showed that the extract inhibited the FcεRI-mediated release of histamine in a concentration-dependent manner. These results suggest that EC extract may exert its anti-allergic activity through negative-regulation of FcεRI expression and a decrease in histamine release. [Copyright &y& Elsevier]

Siegesbeckia glabrescens (Compositae), an annual herb indigenous to Korean mountainous regions and has been eaten as a food in Korea. This study investigated ABTS, DPPH and nitric oxide (NO) radical-scavenging activities, and melanin production and TYR inhibitory effects-guided fractionation to identify therapeutic phytochemicals from S. glabrescens that can attenuate oxidation and melanogenesis in murine melanoma B16F10 cells. Nine compounds with inhibitory effects on melanin production, and TYR activity, and ABTS, DPPH, and NO radical scavenging activity were isolated from the 100% ethanol fraction from S. glabrescens. Among the nine compounds, kirenol (K), methyl ent-16α, 17-dihydroxy-kauran-19-oate (MDK) had strong inhibitory effects on melanin production and TYR activity with antioxidant effects. Western blot analysis revealed that K and MDK suppressed tyrosinase-related protein (TYRP)-1, TYRP-2 and microphthalmia-associated transcription factor (MITF) expression. Moreover, these two compounds inhibited intracellular reactive oxygen species (ROS) level in tert-butyl hydroperoxide (t-BHP)-treated B16F10 cells. Our results suggest that S. glabrescens containing active compounds such as K and MDK, which has antioxidant and antimelanogenesis effects, is the potent therapeutic and functional material for the prevention of oxidation-induced hyperpigmentation. [ABSTRACT FROM AUTHOR]

• Compounds were isolated from Osmanthus fragrans var. aurantiacus leaves. • Compounds inhibited NO production and pro-inflammatory cytokines. • Compounds inhibited the expression of iNOS, COX-2, NF-ΚB and ERK 1/2 pathway. • Compounds could be as potential therapeutic agents to treat inflammatory diseases. Osmanthus fragrans var. aurantiacus has been used for the treatment of menopausal pain, foul breath, and intestinal bleeding. Four phenylpropyl triterpenoids, 3- O -trans- p -coumaroyltormentic acid (1), 3 β -trans- p -coumaroyloxy-2 α -hydroxyl-urs-12-en-28-oic acid (2), 3 β -cis- p -coumaroyloxy-2 α -hydroxyl-urs-12-en-28-oic acid (3), 3- O -cis-coumaroylmaslinic acid (4), were isolated from the leaves of O. fragrans var. aurantiacus and the inhibitory effect on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced macrophages were evaluated. Among them, compounds 2 – 4 concentration dependently showed NO production inhibitory effects. To determine the signaling factors involved in the inhibition of NO production by compounds 2 – 4 , we assessed anti-inflammatory activity. Western blot analysis revealed compounds 2 – 4 significantly decreased the expression of LPS-stimulated protein, inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, nuclear factor-kappa B (NF-κB) and phosphorylated extracellular regulated kinase (pERK)1/2. Also, compounds 2 – 4 downregulated tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and IL-8 levels in LPS-induced macrophages and colonic epithelial cells. This study demonstrated that phenylpropyl triterpenoids 2 – 4 isolated from O. fragrans var. aurantiacus leaves can be used as potential candidates for the prevention and treatment of inflammatory bowel disease. [ABSTRACT FROM AUTHOR]

Chrysanthemum zawadskii var. latilobum (CZL) has been used in Eastern medicine for the treatment of various diseases, such as pneumonia, bronchitis, cough, the common cold, pharyngitis, bladder-related disorders, gastroenteric disorders, and hypertension. In the present study, we isolated two strong antiallergic compounds from CZL, namely, eriodictyol-7-O-β-d-glucuronide (EDG) and 5,7-dihydroxy-4-chromene (DC), and investigated their antiallergic effects in FcεRI-mediated human basophilic KU812F cells. EDG and DC downregulated the protein and messenger RNA (mRNA) expression of FcεRI on the cell surface. Moreover, Western blotting analysis showed that EDG and DC inhibited the expression of protein tyrosine kinases such as Syk and Lyn, and extracellular-regulated kinases (ERK) 1/2. These results suggested that EDG and DC, antiallergic constituents of CZL, are potential therapeutic candidates for protection against and for the treatment of allergic disorders. [ABSTRACT FROM AUTHOR]

Selaginella tamariscina (S. tamariscina) (Beauv.) Spring (Selaginellaceae) has been used in oriental medicine for the treatment of dysmenorrhea, chronic hepatitis, hyperglycemia, amenorrhea, hematuria, prolapse of the anus and metrorrhagia. In the present study, we isolated two strong anti-inflammatory compounds, the biflavonoids hinokiflavone (H) and 7′-O-methyl hinokiflavone (mH), from S. tamariscina and examined their anti-inflammatory activities in lipopolysaccharide (LPS)-mediated murine macrophages (RAW 264.7) and colon epithelial cells (HT-29). H and mH suppressed the production of the inflammatory mediators nitric oxide (NO), interleukin (IL)-6, IL-8, and tumor-necrosis factor (TNF)-α, which are most highly activated in inflammatory bowel disease (IBD). In addition, Western blot analysis revealed that H and mH suppressed the LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, and the activation of nuclear factor-κB (NF-κB) and extracellular regulated kinases (ERK) 1/2. These results suggest that H and mH are compounds having potent anti-inflammatory effects that could be used to treat such diseases as IBD. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) remains a significant global health concern, and targeting inflammation has emerged as a promising approach for its prevention and treatment. Medicinal plants and phytochemicals have garnered attention for their potential efficacy against inflammation with minimal toxicity. Osmanthus fragrans var. aurantiacus Makino (O. fragrans) has a history of traditional use in Korea and China in treating various inflammation-related conditions, but its potential use for CRC has not been uncovered. This study aims to explore the potential anti-proliferative and pro-apoptotic properties of O. fragrans , focusing on its impact on CRC treatment. By investigating O. fragrans , we aim to uncover its anti-proliferative and apoptotic effects in human CRC cells, potentially paving the way for effective and well-tolerated therapeutic strategies for CRC patients. Ethanol (EtOH) extracts of O. fragrans leaf and flower, along with specific fractions (n -hexane, ethyl acetate (EtOAc), n -butanol, and the aqueous residue) were evaluated for their anti-proliferative effects in human CRC cells using MTT assays, and compared to normal colon cells. Mechanistic insights and chemical profiling were obtained through flow cytometry, colorimetric assays, western blotting, and molecular docking, and high-performance liquid chromatography (HPLC) system. Both flower and leaf EtOH extracts of O. fragrans exhibited significant anti-proliferative effects in human CRC cells, with the leaf extract demonstrating higher potency. The EtOAc fraction from the leaf extract displayed the strongest anti-CRC cell proliferative effects while no cytotoxic effects in normal colon cells. Chemical profiling of these fractions identified triterpenoids as significant components in the EtOAc fractions. The leaf EtOAc fraction caused cell cycle arrest and apoptosis, accompanied by elevating intracellular reactive oxygen species and mitochondrial dysfunction in CRC cells. Additionally, it inhibited NF-κB and ERK1/2 signaling, leading to reduced COX2 expression. Notably, two triterpenoids isolated from the leaf EtOAc fraction, maslinic acid and corosolic acid, displayed potent anti-cancer activity in CRC cells without affecting normal colon cells. Corosolic acid exhibited a strong binding affinity to COX2 and reduced its expression, supporting its role in the anti-inflammatory and anti-cancer effects. Our findings suggest that O. fragrans , particularly its triterpenoid-rich EtOAc fraction, holds promise as a novel therapeutic agent for CRC prevention and therapy. These results provide valuable insights into the potential application of O. fragrans and its bioactive compounds in combating CRC. [Display omitted] • Osmanthus fragrans var. aurantiacus (O. fragrans) inhibits proliferation of colorectal cancer (CRC) cells. • The leaf EtOAc fraction of O. fragrans promotes apoptosis in CRC cells by inducing mitochondrial dysfunction. • Triterpenoids from the leaf EtOAc fraction display strong anti-CRC cell proliferation activity with induction of apoptosis. • The leaf EtOAc fraction and triterpenoids exhibit anti-CRC cell proliferation effects by inhibiting NF-κB and COX2. • These results underscore the therapeutic potential of O. fragrans and its bioactive compounds against CRC. [ABSTRACT FROM AUTHOR]

• Sargahydroquinoic acid, SHQA was isolated from marine algae, Sargassum serratifolium. • SHQA inhibited calcium influx, ROS and cytokines production, MAPK and NF- k B activation, degranulation in PMACI-induced KU812F cells. • SHQA inhibited the cytokines production and b -hexosaminidase release in com 48/80-induced RBL-2H3 cells. • SHQA inhibited the degranulation in IgE-mediated BMCMCs and PCA in mice. • SHQA isolated from Sargassum serratifolium could be used as potential therapeutic functional food materials for protection of allergic disorders. Basophils and mast cells are characteristic effector cells in allergic reactions. Sargahydorquinoic acid (SHQA), a compound isolated from Sargassum serratifolium (marine alga), possesses various biochemical properties, including potent antioxidant activities. The objective of the present study was to investigate inhibitory effects of SHQA on the activation of human basophilic KU812F cells induced by phorbol myristate acetate and A23187 (PMACI), a calcium ionophore. Furthermore, we confirmed the inhibitory effects of SHQA on the activation of rat basophilic leukemia (RBL)–2H3 cells induced by compound 48/80 (com 48/80), bone marrow-derived mast cells (BMCMCs) induced by anti-dinitrophenyl(DNP)-immunoglobulin E (IgE)/DNP-bovine serum albumin (BSA), DNP/IgE and on the reaction of passive cutaneous anaphylaxis (PCA) mediated by IgE. SHQA reduced PMACI-induced intracellular reactive oxygen species (ROS) and calcium levels. Western blot analysis revealed that SHQA downregulated the activation of ERK, p38, and NF-κB in a dose-dependent manner. Moreover, SHQA suppressed the production and gene expression of various cytokines, including interleukin (IL)-1 β, IL-4, IL-6, and IL-8 in PMACI-induced KU812F cells and IL-4 and tumor necrosis factor (TNF)- α in com 48/80-induced RBL-2H3 cells. It also determined the inhibition of PMACI, com 48/80- and IgE/DNP-induced degranulation by reducing the release of β -hexosaminidase. Furthermore, it attenuated the IgE/DNP-induced PCA reaction in the ears of BALB/c mice. These results suggest that SHQA isolated from S. serratifolium is a potential therapeutic functional food material for inhibiting effector cell activation in allergic reactions and anaphylaxis in animal model. [ABSTRACT FROM AUTHOR]