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Journal of Biomolecular Structure &... 2022Edifenphos (EDF) is an organophosphorus pesticide with antifungal and anti-insecticidal properties. However, EDF accumulates in various agricultural products and causes...
Edifenphos (EDF) is an organophosphorus pesticide with antifungal and anti-insecticidal properties. However, EDF accumulates in various agricultural products and causes potential hazards to human health. Although numerous reports have indicated EDF accumulation in agricultural products, toxic effects on cellular system is poorly understood. In the present study, we investigated the cytotoxicity and genotoxicity of EDF in rat hepatocytes and its amelioration by apigenin (a dietary flavonoid). Results showed that EDF inhibited the cell viability, induced oxidative stress, DNA damage, loss of mitochondrial membrane potential (ΔΨm) and caspase-9/-3 activation in rat hepatocytes. Incubation of hepatocytes with N-acetyl cysteine (ROS scavenger) significantly abrogated the ROS generation and apoptosis caused by EDF. In addition, this study also showed that apigenin significantly suppressed the toxic effects of EDF by quenching ROS production thereby abrogating the caspase-9/-3 and apoptosis activation in hepatocytes. Taken together, the findings of this study demonstrate that EDF induces cytotoxicity and DNA damage in hepatocytes, and apigenin can be considered as an effective dietary anti-oxidant regimen against EDF- induced toxicity in cellular system.Communicated by Ramaswamy H. Sarma.
Topics: Humans; Rats; Animals; Apigenin; Caspase 9; Membrane Potential, Mitochondrial; Reactive Oxygen Species; Organophosphorus Compounds; Pesticides; DNA Damage; Apoptosis
PubMed: 33998977
DOI: 10.1080/07391102.2021.1926325 -
International Journal of Molecular... May 2024Neuroinflammation, a hallmark of various central nervous system disorders, is often associated with oxidative stress and neuronal or oligodendrocyte cell death. It is... (Review)
Review
Neuroinflammation, a hallmark of various central nervous system disorders, is often associated with oxidative stress and neuronal or oligodendrocyte cell death. It is therefore very interesting to target neuroinflammation pharmacologically. One therapeutic option is the use of nutraceuticals, particularly apigenin. Apigenin is present in plants: vegetables (parsley, celery, onions), fruits (oranges), herbs (chamomile, thyme, oregano, basil), and some beverages (tea, beer, and wine). This review explores the potential of apigenin as an anti-inflammatory agent across diverse neurological conditions (multiple sclerosis, Parkinson's disease, Alzheimer's disease), cancer, cardiovascular diseases, cognitive and memory disorders, and toxicity related to trace metals and other chemicals. Drawing upon major studies, we summarize apigenin's multifaceted effects and underlying mechanisms in neuroinflammation. Our review underscores apigenin's therapeutic promise and calls for further investigation into its clinical applications.
Topics: Apigenin; Humans; Animals; Neuroinflammatory Diseases; Anti-Inflammatory Agents; Oxidative Stress; Inflammation
PubMed: 38732259
DOI: 10.3390/ijms25095041 -
Biomedicine & Pharmacotherapy =... Aug 2023Prolonged exposure to UV light can lead to photo-ageing of the skin. Therefore, the development and application of anti-photoaging drugs is urgent. In this study, we...
Prolonged exposure to UV light can lead to photo-ageing of the skin. Therefore, the development and application of anti-photoaging drugs is urgent. In this study, we co-loaded apigenin (Apn) and doxycycline (Doc), a broad-spectrum inhibitor of matrix metalloproteinases (MMPs), into flexible liposomes to exert anti-photoaging effects by combating oxidative stress, anti-inflammation, reducing the activation of MMPs and preventing collagen loss. The results showed that we prepared a flexible liposome (A/D-FLip) containing Apn and Doc. Its appearance, particle size and Zeta potential were normal and it had good encapsulation efficiency, drug loading, in vitro release and transdermal efficiency. In cellular experiments, A/D-FLip could inhibit oxidative stress damage, reduce inflammatory factors and decrease the activation of MMPs in Human immortalized keratinocytes (HaCaT) cells; in animal experiments, A/D-FLip could inhibit skin damage and reduce skin collagen loss by decreasing the activation of MMPs, thus inhibiting skin photoaging in mice. In conclusion, A/D-FLip has good anti-photoaging effects and it has the potential to become an effective skin care product or drug against UV damage and skin photoaging in the future.
Topics: Animals; Mice; Humans; Liposomes; Apigenin; Doxycycline; Skin; Collagen; Skin Aging; Matrix Metalloproteinases; Ultraviolet Rays
PubMed: 37301137
DOI: 10.1016/j.biopha.2023.114998 -
Chemico-biological Interactions Jul 2022Tumor angiogenesis inhibitors such as Bevacizumab, Ramucirumab and Endostar have been applied to the therapy of non-small cell lung carcinoma (NSCLC) patients,...
Tumor angiogenesis inhibitors such as Bevacizumab, Ramucirumab and Endostar have been applied to the therapy of non-small cell lung carcinoma (NSCLC) patients, especially for lung adenocarcinoma (LUAD). However, several safe concerns such as neutropenia, febrile neutropenia and hypertension pulmonary hemorrhage limit their further development. And they often showed poor efficacy and serious side effect for lung squamous cell carcinoma (LUSC) patient. Thus, identification of effective and safe tumor angiogenesis inhibitor for NSCLC therapy is warranted. Apigenin is a bioflavonoid with potential anti-tumor effect and perfect safety, but its effect on tumor angiogenesis and underlying mechanism are still unclear. Herein, we found that apigenin not merely suppressed endothelial cells related motilities but also reduced pericyte coverage. Further research showed that apigenin had strong suppressive activity against HIF-1α expression and its downstream VEGF-A/VEGFR2 and PDGF-BB/PDGFβR signaling pathway. Apigenin also reduced microvessel density and pericyte coverage on the xengraft model of NCI-H1299 cells, leading to suppression of tumor growth. Moreover, apigenein showed perfect anti-angiogenic effect in xengraft model of LUSC cell NCI-H1703 cells, indicating it may be developed into a potential angiogenesis inhibitor for LUSC patient. Collectively, our study provides new insights into the anti-tumor mechanism of apigenin and suggests that apigenin is a safe and effective angiogenesis inhibitor for NSCLC therapy.
Topics: Angiogenesis Inhibitors; Apigenin; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Endothelial Cells; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; Lung Neoplasms; Neovascularization, Pathologic; Vascular Endothelial Growth Factor A
PubMed: 35513012
DOI: 10.1016/j.cbi.2022.109966 -
Dental Materials : Official Publication... Apr 2021The aim of this in vitro study was to incorporate two anti-caries agents, Apigenin and tt-Farnesol, to resin composite and resin cement to reduce the virulence of...
OBJECTIVES
The aim of this in vitro study was to incorporate two anti-caries agents, Apigenin and tt-Farnesol, to resin composite and resin cement to reduce the virulence of Streptococcus mutans around dental restorations.
METHODS
Apigenin (Api, 5 mM) and tt-Farnesol (Far, 5 mM) were added alone, together, and combined with fluoride (F). Biofilm of S. mutans was grown on composite discs, and the dry-weight, bacterial viability, and the polysaccharides (alkali-soluble, intracellular and water-soluble) were quantified. CLSM images of the S. mutans biofilm were obtained after three years of water-storage. The effect of the additions on the physicochemical properties and the composite colorimetric parameters were also analyzed.
RESULTS
The additions did not affect bacterial viability. Api alone and combined with Far or combined with Far and F decreased the bacterial dry-weight, alkali-soluble and intracellular polysaccharides. After three years, the composites containing the additions presented a greater EPS matrix on the top of biofilm. Statistical difference was obtained for the degree of conversion; however, the maximum polymerization rate and curing kinetics were unaffected by the additions. No difference was observed for the water-soluble polysaccharides, flexural strength, and elastic modulus. Api increased the yellowness of the composites.
SIGNIFICANCE
Api, alone and combined, reduced the expression of virulence of S. mutans without jeopardizing the physicochemical properties of the composites.
Topics: Apigenin; Biofilms; Cariostatic Agents; Composite Resins; Dental Caries; Farnesol; Humans; Streptococcus mutans; Virulence
PubMed: 33422299
DOI: 10.1016/j.dental.2020.12.005 -
Inflammopharmacology Aug 2022Apigenin is a member of the flavonoid family that can regulate various biological processes, which is characterized as a treatment of different inflammatory disorders... (Meta-Analysis)
Meta-Analysis Review
The effects of apigenin administration on the inhibition of inflammatory responses and oxidative stress in the lung injury models: a systematic review and meta-analysis of preclinical evidence.
BACKGROUND/OBJECTIVE
Apigenin is a member of the flavonoid family that can regulate various biological processes, which is characterized as a treatment of different inflammatory disorders and pathological problems associated with oxidative stress (OS). Recent research has focused on apigenin immunomodulatory properties as a potential treatment for different types of lung injuries. This meta-analysis was designed to determine the impact of apigenin treatment on inflammatory markers and OS parameters in animal models of lung injuries.
METHODS
The comprehensive literature search was conducted using electronic databases such as Google Scholar, PubMed, Web of Science, Scopus, and Embase up to August 2021. To assess apigenin's effect on inflammatory mediators and OS biomarkers in lung injury animal models, we used the I statistic to determine the heterogeneity. We then pooled data as standardized mean difference (SMD) with a 95% confidence interval (CI).
RESULTS
Our meta-analysis of the pooled data for inflammatory biomarkers demonstrated that the apigenin administration significantly decreased the NF-κB expression (SMD - 1.60, 95% CI [- 2.93 to - 0.26]; I = 89.0%, p < 0.001), IL-1β (SMD - 4.30, 95% CI [- 6.24 to - 2.37]; I = 67.3%, p = 0.047), IL-6 (SMD - 4.10, 95% CI [- 5.04 to - 3.16]; I = 72.6%, p < 0.001), TNF-α (SMD - 3.74, 95% CI [- 4.67 to - 2.82]; I = 84.1%, p < 0.001), and TNF-α gene expression (SMD - 3.44, 95% CI [- 4.44 to - 2.43]; I = 0.0%, p = 0.622). This study also indicated the efficacy of apigenin in increasing the level of CAT (SMD 4.56, 95% CI [3.57 to 5.55]; I = 15.3%, p = 3.15), GSH (SMD 5.12, 95% CI [3.53 to 6.70]; I = 77.6%, p < 0.001), and SOD (SMD 3.45, 95% CI [2.50 to 4.40]; I = 79.2%, p < 0.001), and decreasing the level of MDA (SMD - 3.87, 95% CI [- 5.25 to - 2.49]; I = 80.3%, p < 0.001) and MPO (SMD - 4.02, 95% CI [- 5.64 to - 2.40]; I = 88.9%, p < 0.001), TGF- β (SMD - 3.81, 95% CI [- 4.91 to - 2.70]; I = 73.4%, p = 0.001) and W/D level (SMD - 3.22, 95% CI [- 4.47 to - 1.97]; I = 82.1%, p < 0.001) than control groups.
CONCLUSION
Overall, our findings showed the immunomodulatory potential of apigenin as an alternative treatment for the suppression of inflammatory responses and OS in different types of lung injury diseases. Nevertheless, due to the paucity of clinical studies, reliable preclinical models, and clinical settings, evaluating the influence of apigenin on lung injury is required in the future. Before conducting large-scale clinical trials, detailed human pharmacokinetic studies are also needed to establish dosage ranges and determine the initial safety and tolerability of apigenin.
Topics: Animals; Apigenin; Biomarkers; Humans; Lung Injury; Oxidative Stress; Tumor Necrosis Factor-alpha
PubMed: 35661071
DOI: 10.1007/s10787-022-00994-0 -
Food Research International (Ottawa,... Aug 2023The production and use of ozone micro-nano bubble water (O-MNBW) is an innovative technology that prolongs the reactivity of aqueous-phase ozone and maintains the...
The production and use of ozone micro-nano bubble water (O-MNBW) is an innovative technology that prolongs the reactivity of aqueous-phase ozone and maintains the freshness and quality of fruits and vegetables by removing pesticides, mycotoxins, and other contaminants. The quality of parsley treated with different concentrations of O-MNBW was investigated during storage at 20 ℃ for 5 d, and found that a ten-minute exposure of parsley to 2.5 mg·L O-MNBW effectively preserved the sensory quality of parsley, and resulted in lower weight loss, respiration rate, ethylene production, MDA levels, and a higher level of firmness, vitamin C, and chlorophyll content, relative to untreated parsley. The O-MNBW treatment also increased the level of total phenolics and flavonoids, enhanced peroxidase and ascorbate peroxidase activity, and inhibited polyphenol oxidase activity in stored parsley. Five volatile signatures identified using an electronic nose (W1W, sulfur-compounds; W2S, ethanol; W2W, aromatic- and organic- sulfur compounds; W5S, oxynitride; W1S, methane) exhibited a significant decrease in response to the O-MNBW treatment. A total of 24 major volatiles were identified. A metabolomic analysis identified 365 differentially abundant metabolites (DMs). Among them, 30 and 19 DMs were associated with characteristic volatile flavor substance metabolism in O-MNBW and control groups, respectively. The O-MNBW treatment increased the abundance of most DMs related to flavor metabolism and reduced the level of naringin and apigenin. Our results provide insight into the mechanisms that are regulated in response to the exposure of parsley to O-MNBW, and confirmed the potential use of O-MNBW as a preservation technology.
Topics: Petroselinum; Apigenin; Ascorbic Acid; Chlorophyll; Coloring Agents
PubMed: 37316085
DOI: 10.1016/j.foodres.2023.113020 -
Natural Product Research Mar 2021Three new biflavones, apigenin-(3',8″)-chrysin (), (2)-2,3-Dihydroametoflavone 5,4'-dimethyl ether (), and...
Three new biflavones, apigenin-(3',8″)-chrysin (), (2)-2,3-Dihydroametoflavone 5,4'-dimethyl ether (), and (2)-5″,7″-Dihydroxy-2″-phenoxychromonyl-(4'″,3')-naringenin (), together with seven known biflavones () were isolated from the 75% EtOH extract of . The structures of new compounds were established by application of spectroscopic methods, including 1D and 2D NMR, HRMS, and CD measurements. In addition, all new compounds were evaluated for their cytotoxic potential against three human cancer cell lines A549, MCF-7, and SMMC-7721 . Compound exhibited potent cytotoxic activity with IC values ranging from 6.35 to 10.18 μM.
Topics: Antineoplastic Agents; Apigenin; Cell Death; Cell Line, Tumor; Flavanones; Flavones; Flavonoids; Humans; Magnetic Resonance Spectroscopy; Plant Extracts; Selaginellaceae
PubMed: 31109181
DOI: 10.1080/14786419.2019.1611813 -
The American Journal of Chinese Medicine 2024The stimulator of interferon genes (STING) signaling pathway is crucial for the pathogenesis of autoimmune and inflammatory disorders, including acute lung injury (ALI)....
The stimulator of interferon genes (STING) signaling pathway is crucial for the pathogenesis of autoimmune and inflammatory disorders, including acute lung injury (ALI). Apigenin (4[Formula: see text],5,7-trihydroxyflavone) is a natural flavonoid widely found in fruits, vegetables, and Chinese medicinal herbs that exhibits a range of pharmacological effects, such as antibacterial and anti-inflammatory activities. However, the efficacy of apigenin in STING pathway-mediated diseases remains unclear. Accordingly, this study screened Chinese medicines to identify potent agents that reduced the synthesis of type I interferons (IFNs). The results revealed apigenin as a potent compound with low cytotoxicity that markedly reduced the synthesis of type I IFNs in response to STING pathway agonists. Besides, apigenin markedly suppressed innate immune responses triggered by the STING agonist SR-717. Mechanistically, apigenin downregulated IFN beta 1 (IFNB1) expression mediated by the STING pathway via dose-dependent inhibition of STING expression, reduction of dimerization, nuclear translocation of phosphorylated IRF3, and disruption of the association between STING and IRF3. Moreover, apigenin effectively mitigated pathological pulmonary inflammation and lung edema in lipopolysaccharide (LPS)-induced ALI in mice. Apigenin further strongly attenuated the hallmarks of immoderate inflammation (interleukin (IL)-6, IL-1[Formula: see text], and tumor necrosis factor [Formula: see text]) and innate immune responses (IFNB1, C-X-C motif chemokine ligand 10, and IFN-stimulated gene 15) by preventing the activation of the STING/IRF3 pathway both and . Importantly, SR-717 significantly reversed the inhibitory effects of apigenin in LPS-induced THP1-Blue ISG macrophages. Collectively, apigenin effectively alleviated innate immune responses and mitigated inflammation in LPS-induced ALI via inhibition of the STING/IRF3 pathway. These findings suggest the potential of apigenin as a prophylactic and therapeutic candidate for managing STING-mediated diseases.
Topics: Animals; Mice; Lipopolysaccharides; Apigenin; Membrane Proteins; Immunity, Innate; Inflammation; Interleukin-6
PubMed: 38480499
DOI: 10.1142/S0192415X24500204 -
Neurochemical Research Mar 2022Apigenin, as a natural flavonoid present in several plants is characterized with potential anticancer, antioxidant, and anti-inflammatory properties. Recent studies...
Apigenin, as a natural flavonoid present in several plants is characterized with potential anticancer, antioxidant, and anti-inflammatory properties. Recent studies proposed that apigenin affects depression disorder through unknown mechanistic pathways. The effects of apigenin's anti-depressive properties on streptozocin-mediated depression have been investigated through the evaluation of behavioral tests, oxidative stress, cellular energy homeostasis and inflammatory responses. The results demonstrated anti-depressive properties of apigenin in behavioral test including forced swimming and splash tests and oxidative stress biomarkers such as reduced glutathione, lipid peroxidation, total antioxidant power and coenzyme Q levels. Apigenin, also, demonstrated its regulatory potency in cellular energy homeostasis and immune system gene expression through inhibiting Nlrp3 and Tlr4 overexpression. Furthermore, failure in energy production as the key factor in various psychiatric disorders was reversed by apigenin modulating effect on AMPK gene expression. Overall, 20 mg/kg of apigenin was recognized as the dose suitable for minimizing the undesirable adverse effects in the STZ-mediated depression model proposed in this study. Our data suggested that apigenin could be able to adjust behavioral dysfunction, biochemical biomarkers and recovered cellular antioxidant level in depressed animals. The surprising results were achieved by raise in COQ level, which could regulate the overexpression of the AMPK gene in stressful conditions. The regulatory effect of apigenin in inflammatory signaling pathways such as Nlrp3, and Tlr4 gene expression was studied at the surface part of the hippocampus.
Topics: Animals; Antioxidants; Apigenin; Depression; Humans; Neuroprotective Agents; Oxidative Stress
PubMed: 34705188
DOI: 10.1007/s11064-021-03473-0