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Effects of fisetin on virulence of Actinobacillus Pleuropneumoniae.

Porcine infectious pleuropneumonia (PCP), caused by Actinobacillus pleuropneumoniae (APP), is a highly infectious respiratory disease of pigs, resulting in significant economic losses to the industry. Apx toxins are cytolytic virulence factors produced by APP. The natural flavonoid fisetin has a variety of biological activities, including antioxidant and anti-inflammatory properties. This study aimed to investigate the protective effects of fisetin against APP. Fisetin was found to effectively inhibit the hemolytic activity of both APP culture supernatants and the purified toxins, and blood ag

Fisetin administration improves LPS-induced acute otitis media in mouse in vivo.

Acute otitis media is one of the most common infectious diseases worldwide in spite of the widespread vaccination. The present study was conducted to explore the effects of fisetin on mouse acute otitis media models. The animal models were established by lipopolysaccharide (LPS) injection into the middle ear of mice via the tympanic membrane. Fisetin was administered to mice for ten days through intragastric administration immediate after LPS application. Hematoxylin and eosin (H&E) staining was performed and the pro-inflammatory cytokines, including interleukin-1β (IL-1β), tumor necrosis fact

Dihydromyricetin Alleviates Non-Alcoholic Fatty Liver Disease by Modulating Gut Microbiota and Inflammatory Signaling Pathways.

Non-alcoholic fatty liver disease (NAFLD) is a prevalent chronic liver condition that is strongly linked to gut microbiota imbalance and chronic inflammation. This study aims to explore the preventive effects of dihydromyricetin (DHM) on NAFLD by modulating the intestinal flora and the TLR4/NF-κB signaling pathway. Fifty male C57BL/6J mice were randomly assigned to five groups: a normal control group, a model group, and three DHM treatment groups receiving low (500 mg/kg), medium (750 mg/kg), and high doses (1,000 mg/kg). NAFLD was induced using a high-fat diet, and DHM was administered for 8

Fisetin mitigates letrozole-induced polycystic ovarian syndrome in rats: crosstalk of AMPK/PI3K/AKT-mediated-Nrf2 antioxidant defense mechanism and the inflammasome NLRP3/NF-κB P65/IL-1β signaling pathways.

Polycystic ovarian syndrome (PCOS) is a highly prevalent condition affecting reproductive-aged women, causing insulin resistance, hyperandrogenism, weight gain, and menstrual problems. The present study intended to investigate the potential role of fisetin (FT) in letrozole (LZ)-induced PCOS in adult female rats and the possible mechanism underlying its action. PCOS was induced by oral administration of LZ (1 mg/kg) for 21 days. Treated rats received FT (1.25 or 2.5 mg/kg) orally once daily for 14 consecutive days. Following the experimental duration, blood samples and ovary tissues were isola

Senolytics reduce coronavirus-related mortality in old mice.

The COVID-19 pandemic has revealed the pronounced vulnerability of the elderly and chronically ill to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-induced morbidity and mortality. Cellular senescence contributes to inflammation, multiple chronic diseases, and age-related dysfunction, but effects on responses to viral infection are unclear. Here, we demonstrate that senescent cells (SnCs) become hyper-inflammatory in response to pathogen-associated molecular patterns (PAMPs), including SARS-CoV-2 spike protein-1, increasing expression of viral entry proteins and reducing antivir

Kaempferol's Therapeutic Applications and Mechanistic Insights in Ocular Diseases: Current Progress, Challenges, and Translational Opportunities.

Kaempferol is a natural flavonol compound widely present in various single-herb remedies and compound formulations used for the treatment of ocular diseases. Despite its inherent pharmaceutical limitations, accumulating evidence indicates that kaempferol exerts broad protective effects against diverse ocular disorders through multiple biological pathways, highlighting its potential as a multi-target therapeutic candidate in ophthalmology. However, current evidence regarding kaempferol-based ophthalmic applications remains fragmented across different ocular diseases and mechanistic investigatio

Chrysosplenetin acts as a homeostasis stabilizer with dual-function in shattering Plasmodium berghei K173 resistance to artemisinin driven by both ABC transporters and heme-ROS/GSH axis.

BACKGROUND: Chrysosplenetin (CHR), a polymethoxy flavonol co-occurring with artemisinin (ART) in Artemisia annua L., reverses ART resistance in Plasmodium berghei K173 potentially by downregulating intestinal P-glycoprotein (P-gp, encoded by Mdr1a) expression. In the present study, we further elaborated on the mechanism by comparing differences in antimalarial activity and resistance-associated molecular expression profiles between ART alone and combination therapy in blood and tissues of Mdr1a wild-type (WT) and knockout (KO) mice infected with either sensitive or resistant malarial parasites

Intake of dietary flavonoids in relation to overactive bladder among U.S. adults: a nutritional strategy for improving urinary health.

BACKGROUND: The increasing influence of overactive bladder (OAB) on physical as well as mental health of individuals is becoming more pronounced annually, as evidenced by the urge urinary incontinence and nocturia. Symptoms in OAB patients may be influenced by inflammation and oxidative stress. Flavonoids are recognized as significant anti-inflammatory and antioxidant agents, which are commonly available in fruits, tea, vegetables, etc. Previous research has demonstrated the therapeutic potential of flavonoids and their subclasses in treating inflammation, and oxidative stress. Despite this, t

Medicinal plants as a potential source of Phosphodiesterase-5 inhibitors: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: The prevalence and distress caused by erectile dysfunction (ED) to both male and female partners are increasing at a steady rate. ED has now become the most treated sexual disorder for men among young and old age groups due to varying physical and psychological factors. The treatment with synthetic Phosphodiesterase-5 (PDE5) inhibitors are cost-effective but due to adverse effects such as priapism, loss of vision, heart attack and syncope, the daily life patterns of these patients are distressed and hence the need for alternative medicaments or sources are of ut

Anti-inflammatory action of an alkaloid, fraction and extract from Alchornea glandulosa in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Alchornea glandulosa (Euphorbiaceae) has traditionally been used in medicine for treating immune-mediated inflammatory diseases. AIM OF STUDY: This work aimed to evaluate the anti-inflammatory effects of a methanolic extract of leaves from A. glandulosa (MEAG), as well as the ethyl acetate fraction (EAFAG) and isolated compound guanidine alkaloid N-1, N-2, N-3-triisopentenylguanidine (AG-1), in experimental in vivo models of inflammation in mice. We also investigated this extract's phenols, flavonoids and flavonol compounds. MATERIALS AND METHODS: MEAG (extrac

Nutritional and Physicochemical Characteristics of Innovative High Energy and Protein Fruit- and Date-Based Bars.

With the increasing global nutritional bar market, developing and formulating innovative high-energy and protein bars to compensate for nutr … the FBB was significantly higher in total phenolic content (TPC), total flavonoids (TF), and total flavonols (TFL) contents and scavenging activity against DPPH and ABTS free radicals than the DBB. The DBB and the FBB showed positive a* values, indicating a reddish color. The b* values were 27.81 and 28.54 for the DBB and the FBB, respectively. The DBB is …

A novel anti-acute lung injury mechanism of astilbin: inhibition of epithelial cells ferroptosis by targeting NRF2 activation via binding Val608 site of NRF2.

OBJECTIVE AND DESIGN: Astilbin (ATB) is a newly discovered natural compound with anti-inflammatory and immunomodulatory effects. However, its effects and underlying mechanisms in acute lung injury (ALI) remain unclear. MATERIAL OR SUBJECTS: An ALI model was established by intratracheal injection of lipopolysaccharide (LPS) into the trachea of C57BL/6 mice. In vitro, MLE-12 cells were stimulated with LPS. ATB was administered as a pretreatment to C57BL/6 mice and MLE-12 cells. RESULTS: ATB significantly alleviated ALI and suppressed the inflammatory response induced by LPS. Further data sugge

Consumption of ellagic acid and dihydromyricetin synergistically protects against UV-B induced photoaging, possibly by activating both TGF-β1 and wnt signaling pathways.

Ellagic acid (EGA) and dihydromyricetin (DHM) are both found in fruits and vegetables are used for anti-aging treatment for the skin. The anti-photoaging efficacy of EGA and DHM was investigated in UV-B irradiated skin in vivo and the involvement of transforming growth factor (TGF)-β1 and wnt signaling pathways were examined in vitro. HaCaT cells were treated with either 50μM EGA, 50μM DHM or 25μM EGA+25μM DHM before 100mJ/cm2 UV-B exposure, and then oxidative stress and inflammation was measured. The involvement of TGF-β1 and wnt signaling was measured using their inhibitors, respectively, in

ERK activation by the polyphenols fisetin and resveratrol provides neuroprotection in multiple models of Huntington's disease.

Huntington's disease (HD) is an inherited, progressive and ultimately fatal neurodegenerative disorder that is characterized by psychiatric, cognitive and motor symptoms. Among the pathways implicated in HD are those involving mitogen-activated protein kinase signaling and particularly the Ras-extracellular signal-regulated kinase (ERK) cascade. Studies in both cells and animal models suggest that ERK activation might provide a novel therapeutic target for the treatment of HD but compounds that specifically activate ERK are few. To test the hypothesis that pharmaceutical activation of ERK migh

Nanoemulsion formulation of fisetin improves bioavailability and antitumour activity in mice.

The natural flavonoid fisetin (3,3',4',7-tetrahydroxyflavone) has shown antitumour activity but its administration is complicated by its low water solubility. Our aim was to incorporate fisetin into a nanoemulsion to improve its pharmacokinetics and therapeutic efficacy. Solubility and emulsification tests allowed to develop an optimal nanoemulsion composed of Miglyol 812N/Labrasol/Tween 80/Lipoid E80/water (10%/10%/2.5%/1.2%/76.3%). The nanoemulsion had an oil droplet diameter of 153 ± 2 nm, a negative zeta potential (-28.4 ± 0.6 mV) and a polydispersity index of 0.129. The nanoemulsion was s

[Ginkgo biloba extract (EGb 761). State of knowledge in the dawn of the year 2000].

EGb 761 is a standardized extract of dried leaves of Ginkgo biloba containing 24% ginkgo-flavonol glycosides, 6% terpene lactones such as ginkgolides A, B, C, J and bilobalide. Its broad spectrum of pharmacological activities allows it to be in adequacy to the numerous pathological requirements--hemodynamic, hemorheological, metabolic--which occur in cerebral, retinal, cochleovestibular, cardiac or peripheral ischemia. Moreover, EGb 761 has direct effects against necrosis and apoptosis of neurons and improves neural plasticity as evidenced in vestibular compensation. At the molecular and the c

Ethnopharmacological uses, phytochemistry, biological activities, and therapeutic applications of Clinacanthus nutans (Burm. f.) Lindau: A comprehensive review.

ETHNOPHARMACOLOGICAL RELEVANCE: Clinacanthus nutans (Burm. f.) Lindau, a widely used medicinal plant, is extensively grown in tropical Asia … esence of two glycerolipids, four sulfur-containing compounds, six known flavones, a flavanol, four flavonols, two phytosterols, one polypeptide, and various phenolics and fatty acids largely influences its diverse bioactivities. Numerous reports justify the ethnomedicinal use of C. nutans as an antiviral agent in treating herpes simplex virus and varicella …

Effect of fisetin supplementation on inflammatory factors and matrix metalloproteinase enzymes in colorectal cancer patients.

A growing body of evidence indicates that inflammation is associated with tumorigenesis, metastasis and chemotherapeutic resistance in patients with colorectal cancer (CRC). Natural flavonoids are promising agents for inflammation-related tumor progression in patients with CRC. This study aimed to assess the efficacy of flavonoid fisetin supplementation on the inflammatory status and matrix metalloproteinase (MMP) levels in these patients. In this double-blind, randomized placebo-controlled clinical trial, 37 CRC patients undergoing chemotherapy were assigned to receive either 100 mg fisetin (

Anticancer effects of Ekebergia capensis Sparrm: cytotoxicity on human breast cancer cells and genotoxicity on Allium cepa L. roots.

ETHNOPHARMACOLOGICAL RELEVANCE: Cancer is a global threat that affects people regardless of sex, race, or age. In the ongoing search for nov … (66.39 mg quercetin equivalent (QE)/g DW), tannins (58.47 mg tannic acid equivalent (TAE)/g DW) and flavonols (29.13 mg QE/g DW). It is non-toxic with LD50 greater than 5000 mg/kg. It exhibited potent antioxidant capacity (IC50 of 0.54 μg/mL and 17.68 μg/mL with ABTS+ and DPPH, respectively and a FRAP of 12797.5). The extract showed moderate cytotoxic effec …

Current Perspectives of the Applications of Polyphenols and Flavonoids in Cancer Therapy.

The development of anticancer therapies that involve natural drugs has undergone exponential growth in recent years. Among the natural compounds that produce beneficial effects on human health, polyphenols have shown potential therapeutic applications in cancer due to their protective functions in plants, their use as food additives, and their excellent antioxidant properties. The possibility of combining conventional drugs-which are usually more aggressive than natural compounds-with polyphenols offers very valuable advantages such as the building of more efficient anticancer therapies with l

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… Flavonols Flavonols are a class of flavonoids based on the backbone 3-hydroxyflavone. There is a wide variety of flavonols, which depend on positions that can be hydroxylated ( Figure 4 ). … Kaempferol and quercetin are the main flavonols studied in medicine. Nevertheless, other flavonols such as herbacetin, myricetin, and fisetin have also been investigated as anticancer drugs [ 68 , 69 ]. …