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Aging Jun 2019The naturally occurring compound apigenin has many biological effects, including anti-inflammatory, antioxidative and anticancer effects. Although hypertrophic scar...
The naturally occurring compound apigenin has many biological effects, including anti-inflammatory, antioxidative and anticancer effects. Although hypertrophic scar formation is a common surgical complication, there is still no good treatment for it. In the present study, we examined the effect of apigenin on hypertrophic scar. After isolating fibroblasts from human hypertrophic scars, we assess the effects of apigenin on fibroblast cell survival, apoptosis and migration. The results showed that apigenin dose-dependently inhibited the growth and migration of hypertrophic scar fibroblasts. By inhibiting FAK kinase activity and FAK phosphorylation, apigenin also inhibited activation of the FAK signaling pathway. Apigenin thus appears to inhibit the growth and migration of hypertrophic scar fibroblasts by inhibiting FAK signaling. This suggests apigenin could potentially provide a new option for the treatment of hypertrophic scars.
Topics: Adult; Apigenin; Apoptosis; Cell Movement; Cell Proliferation; Cell Survival; Cicatrix, Hypertrophic; Female; Fibroblasts; Focal Adhesion Kinase 1; Humans; Male; Middle Aged; Phosphorylation; Signal Transduction
PubMed: 31170089
DOI: 10.18632/aging.102006 -
Frontiers in Bioscience (Landmark... Jan 2011The development of head and neck squamous cell carcinomas (HNSCCs) is a multistep process progressing from precancerous lesions to highly malignant tumors. A critical...
The development of head and neck squamous cell carcinomas (HNSCCs) is a multistep process progressing from precancerous lesions to highly malignant tumors. A critical role in HNSCCs development and progression is played by EGFR family members including EGFR and ErbB2. The aim of this study was to investigate the effect of apigenin, a low molecular weight flavonoid contained in fruits and vegetables, on growth and survival and on EGFR/ErbB2 signaling in cell lines derived from HNSCCs of the tongue (CAL-27, SCC-15) or pharynx (FaDu). Using sulforhodamine B assay, FACS analysis and activated caspase-3 detection by immunofluorescence, we here demonstrate that apigenin dose-dependently inhibits survival and induces apoptosis of HNSCC cells. Further, by performing western blotting with antibodies specific for phosphorylated EGFR, ErbB2, Erk1/2 and Akt we demonstrate that apigenin reduces ligand-induced phosphorylation of EGFR and ErbB2 and impairs their downstream signaling. On the whole, our results suggest that apigenin properties might be exploited for chemoprevention and/or therapy of head and neck carcinomas.
Topics: Apigenin; Apoptosis; Carcinoma; Carcinoma, Squamous Cell; Cell Line, Tumor; ErbB Receptors; Head and Neck Neoplasms; Humans; Neoplasms, Squamous Cell; Pharyngeal Neoplasms; Receptor, ErbB-2; Signal Transduction; Squamous Cell Carcinoma of Head and Neck; Tongue Neoplasms
PubMed: 21196218
DOI: 10.2741/3735 -
Journal of Integrative Neuroscience May 2023Apigenin has been reported to exhibit anti-inflammatory and anti-oxidative activities. This study aimed to investigate the protective role of Apigenin on...
BACKGROUND
Apigenin has been reported to exhibit anti-inflammatory and anti-oxidative activities. This study aimed to investigate the protective role of Apigenin on chemotherapy-induced peripheral neuropathy (CIPN).
METHODS
CIPN mouse model was established using Paclitaxel treatment. Hot plate and tail prick latency tests were performed to examine the allodynia and hyperalgesia behaviors. Anti-inflammatory and anti-oxidative effects of Apigenin on CIPN were determined by enzyme-linked immunosorbent (ELISA) assay, Western blot, and qRT-PCR. Nuclear recruitment of nuclear factor erythroid 2-related factor 2 (NRF2) was analyzed to evaluate the underlying mechanisms of the protective effects of Apigenin.
RESULTS
Apigenin significantly alleviated CIPN-induced nociceptive behaviors of CIPN mice. It also decreased the TNF-α and IL-1β levels, suppressed oxidative stress and inflammation in the surgical spinal cord tissues. Mechanistically, Apigenin altered the pro-inflammatory and anti-inflammatory phenotypes ratio of microglia through promoting the nuclear recruitment of NRF2 and activating the NRF2/Antioxidant Response Element (ARE) signaling pathway.
CONCLUSIONS
In summary, Apigenin relieves CIPN by regulating microglia activation and polarization, which provides a potential therapeutic strategy for CIPN treatment.
Topics: Mice; Animals; Hyperalgesia; Apigenin; Microglia; NF-E2-Related Factor 2; Peripheral Nervous System Diseases; Anti-Inflammatory Agents; Antineoplastic Agents
PubMed: 37258427
DOI: 10.31083/j.jin2203064 -
Oral Surgery, Oral Medicine, Oral... Feb 2014Apigenin and kaempferol are plant flavonoids with reported chemopreventive activities. This study aimed to determine the effect of apigenin and kaempferol on cell...
OBJECTIVE
Apigenin and kaempferol are plant flavonoids with reported chemopreventive activities. This study aimed to determine the effect of apigenin and kaempferol on cell viability in cultured cells derived from the pharynx (FaDu cell line), an oral cavity carcinoma (PCI-13 cell line), and a metastatic lymph node (PCI-15B cell line) and in explanted FaDu cells.
STUDY DESIGN
The in vitro viability of FaDu, PCI-13, and PCI-15B cells treated with apigenin and kaempferol was determined. Tumor growth of FaDu explants was evaluated in athymic mice that were gavaged with either apigenin or kaempferol.
RESULTS
Although apigenin and kaempferol treatment decreased viability of cells in vitro, cell-type-dependent differences in responsiveness were observed. In vivo apigenin treatment significantly increased the tumor size of FaDu explants. Results obtained using kaempferol were similar.
CONCLUSIONS
The in vitro decrease in FaDu cell viability by apigenin and kaempferol was not observed in in vivo tumor explants using the conditions described in this study.
Topics: Animals; Apigenin; Cell Line, Tumor; Cell Survival; Female; Head and Neck Neoplasms; Humans; Kaempferols; Mice; Mice, Nude
PubMed: 24439916
DOI: 10.1016/j.oooo.2013.10.012 -
Molecules (Basel, Switzerland) Nov 2018Apigenin-7-O-glucoside is an active phenolic compound in Asteraceae flowers and possesses remarkable therapeutic applications. However, its high price and low abundance...
Apigenin-7-O-glucoside is an active phenolic compound in Asteraceae flowers and possesses remarkable therapeutic applications. However, its high price and low abundance in plants limit its use, meanwhile it would hydrolyze in the purification process. In this study, apigenin-7-O-glucoside extracted with ultrasound and purified with preparative HPLC from 'Huangju' was investigated, as well as its hydrolysis behavior and bioactivities. The optimized extraction conditions were: solid/liquid ratio: 1:20, extraction time: 35 min, temperature: 50 °C, and ultrasound power: 350 W. The content of apigenin-7-O-glucoside was up to 16.04 mg/g. Apigenin-7-O-glucoside was then purified with preparative HPLC from the extract, and confirmed by Q-TOF/MS. Apigenin-7-O-glucoside was partially hydrolyzed in acidic condition, and the hydrolysis rate depended on the pH value and temperature. The antioxidant activity increased as a result of the hydrolysis process. This study provided a green and effective way to obtain apigenin-7-O-glucoside and would be beneficial for further investigations into nutritional and functional aspects apigenin-7-O-glucoside and other glycosides.
Topics: Antioxidants; Apigenin; Chromatography, High Pressure Liquid; Chrysanthemum; Glycosides; Hydrolysis; Phytochemicals; Plant Extracts; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
PubMed: 30424020
DOI: 10.3390/molecules23112933 -
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 -
International Journal of Molecular... Feb 2023The prominent flavonoids apigenin and chrysin have been demonstrated to have systemic benefits. Our previous work was first to establish the impact of apigenin and...
The prominent flavonoids apigenin and chrysin have been demonstrated to have systemic benefits. Our previous work was first to establish the impact of apigenin and chrysin on cellular transcriptome. In the current study, we have revealed the ability of apigenin and chrysin to alter the cellular metabolome based on our untargeted metabolomics. Based on our metabolomics data, both these structurally related flavonoids demonstrate diverging and converging properties. Apigenin demonstrated the potential to possess anti-inflammatory and vasorelaxant properties through the upregulation of intermediate metabolites of alpha-linolenic acid and linoleic acid pathways. Chrysin, on the other hand, exhibited abilities to inhibit protein and pyrimidine synthesis along with downregulation of gluconeogenesis pathways based on the altered metabolites detected. Chrysin-mediated metabolite changes are mostly due to its ability to modulate L-alanine metabolism and the urea cycle. On the other hand, both the flavonoids also demonstrated converging properties. Apigenin and chrysin were able to downregulate metabolites involved in cholesterol biosynthesis and uric acid synthesis, namely 7-dehydrocholesterol and xanthosine, respectively. This work will provide understanding regarding the diverse therapeutic potential of these naturally occurring flavonoids and help us in curbing an array of metabolic complications.
Topics: Apigenin; Flavonoids; Up-Regulation; Metabolomics
PubMed: 36835484
DOI: 10.3390/ijms24044066 -
International Journal of Biological... 2023Apigenin is the active ingredient in Ludangshen. Although previous studies reported the cardioprotective actions of apigenin against doxorubicin (Dox)-induced...
Apigenin is the active ingredient in Ludangshen. Although previous studies reported the cardioprotective actions of apigenin against doxorubicin (Dox)-induced cardiomyopathy, the underlying mechanisms remain incompletely understood. Since apigenin beneficially regulates various aspects of mitochondrial function and dynamics, we asked whether apigenin improves heart function in mice with Dox-induced cardiomyopathy by regulating the mitochondrial unfolded protein response (UPR). Co-administration of apigenin significantly restored heart function, reduced myocardial swelling, inhibited cardiac inflammation, increased cardiac transcription of UPR-related genes, and promoted cardiomyocyte survival in Dox-treated mice. In turn, blockade of UPR abolished the mito- and cytoprotective effects of apigenin, evidenced by decreased ATP production, suppressed mitochondrial antioxidant capacity, and increased apoptosis, in Dox-treated, cultured HL-1 cardiomyocytes. Furthermore, apigenin treatment prevented Dox-induced downregulation of Sirt1 and Atf5 expression, and the beneficial effects of apigenin were completely nullified in knockout (KO) mice or after siRNA-mediated knockdown . We thus provide novel evidence for a promotive effect of apigenin on UPR via regulation of the Sirt1/Atf5 pathway. Our findings uncover that apigenin seems to be an effective therapeutic agent to alleviate Dox-mediated cardiotoxicity.
Topics: Mice; Animals; Apigenin; Sirtuin 1; Myocytes, Cardiac; Cardiotoxicity; Cardiomyopathies; Mice, Knockout; Doxorubicin; Apoptosis; Oxidative Stress
PubMed: 37928261
DOI: 10.7150/ijbs.85204 -
International Journal of Molecular... Apr 2019Ultraviolet (UV) radiation, especially types A (UVA) and B (UVB), is one of the main causes of skin disorders, including photoaging and skin cancer. Ultraviolent...
Ultraviolet (UV) radiation, especially types A (UVA) and B (UVB), is one of the main causes of skin disorders, including photoaging and skin cancer. Ultraviolent radiation causes oxidative stress, inflammation, p53 induction, DNA damage, mutagenesis, and oxidation of various molecules such as lipids and proteins. In recent decades, the use of polyphenols as molecules with an antioxidant and anti-inflammatory capacity has increased. However, some of these compounds are poorly soluble, and information regarding their absorption and bioavailability is scarce. The main objective of this study was to compare the intestinal absorption and biological activity of apigenin and its more soluble potassium salt (apigenin-K) in terms of antioxidant and photoprotective capacity. Photoprotective effects against UVA and UVB radiation were studied in human keratinocytes, and antioxidant capacity was determined by different methods, including trolox equivalent antioxidant capacity (TEAC), ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC) assays. Finally, the intestinal absorption of both apigenins was determined using an in vitro Caco-2 cell model. Apigenin showed a slightly higher antioxidant capacity in antioxidant activity assays when compared with apigenin-K. However, no significant differences were obtained for their photoprotective capacities against UVA or UVB. Results indicated that both apigenins protected cell viability in approximately 50% at 5 J/m of UVA and 90% at 500 J/m of UVB radiation. Regarding intestinal absorption, both apigenins showed similar apparent permeabilities (), 1.81 × 10 cm/s and 1.78 × 10 cm/s, respectively. Taken together, these results suggest that both apigenins may be interesting candidates for the development of oral (nutraceutical) and topical photoprotective ingredients against UVA and UVB-induced skin damage, but the increased water solubility of apigenin-K makes it the best candidate for further development.
Topics: Antioxidants; Apigenin; Caco-2 Cells; Cells, Cultured; Humans; Intestinal Absorption; Keratinocytes; Sunscreening Agents
PubMed: 31052292
DOI: 10.3390/ijms20092148 -
Analytical Biochemistry Jul 2020Glucuronidation is one of the major metabolic pathways for flavonoids. However, quantification of flavonoid glucuronides in biological samples, especially in the bile,...
Development and validation of an LC-MS/MS method for the quantification of flavonoid glucuronides (wogonoside, baicalin, and apigenin-glucuronide) in the bile and blood samples: Application to a portal vein infusion study.
Glucuronidation is one of the major metabolic pathways for flavonoids. However, quantification of flavonoid glucuronides in biological samples, especially in the bile, is sometimes challenging due to signal suppression by bile acids. The purpose of this study is to establish a robust LC-MS/MS method for directly measuring flavonoid glucuronides in bile and blood. Wogonoside (wogonin-7-O-glucuronide), baicalin (baicalein-7-O-glucuronide) and apigenin-7-O-glucuronide were used as the model compounds and taurocholic acid (T-CA) were used as the model bile acid to establish the method. Bile samples were processed using solid phase extraction (SPE) and blood samples were prepared using protein precipitation method. The analytes were separated on a Resteck HPLC (50 mm × 2.1 mm ID, 1.7 μm) column using acetonitrile and 0.1% formic acid in water as the mobile phases. The mass analysis was performed in an AB Sciex 5500 Qtrap mass spectrometer via multiple reaction monitoring (MRM) in the positive mode. The results showed that the linear range of the above three analytes were 10 nM-5000 nM in the bile and 1.56 nM-4000 nM in the blood, respectively. The recoveries of three glucuronides were >85% and the matrix effects were <20% at low, medium and high concentrations in the bile and the blood. The results also showed that >90% of these bile acids were removed by the selected SPE procedure to facilitate glucuronide analysis. The validated method was successfully applied to a portal vein infusion study using rats to quantify baicalin, wogonoside, and apigenin-glucuronide in bile and blood samples.
Topics: Animals; Apigenin; Bile; Chromatography, High Pressure Liquid; Flavanones; Flavonoids; Glucosides; Male; Portal Vein; Rats; Rats, Wistar; Tandem Mass Spectrometry
PubMed: 32298642
DOI: 10.1016/j.ab.2020.113723