• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.1
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• pp.75-81
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• 2013

Chrysin (5,7-dihydroxyflavone) is a natural flavonoid found in various plants and foods such as propolis and honey. It has been reported that chrysin has various biological effects including antioxidant, anti-aging, anti-inflammatory and anti-cancer. In this study, we investigated the effect of chrysin on the transcriptional activity of VDR in human epidermal keratinocytes by performing dual-luciferase assay. Chrysin significantly induced the transcriptional activity of VDR in a concentration-dependent manner. The VDR mRNA expression was investigated by quantitative real time PCR and chrysin increased the VDR mRNA expression in normal human epidermal keratinocytes. We also found that chrysin increased the expression of keratinocyte differentiation markers such as keratin 10, involucrin and filaggrin. Therefore, the results suggest that chrysin can stimulate the differentiation of human keratinocytes by increasing transcriptional activity of VDR.

• Biomolecules & Therapeutics
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• v.24 no.4
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• pp.446-452
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• 2016

Pharmacokinetic interaction of chrysin, a flavone present in honey, propolis and herbs, with caffeine was investigated in male Sprague-Dawley rats. Because chrysin inhibited CYP1A-selective ethoxyresorufin O-deethylase and methoxyresorufin O-demethylase activities in enriched rat liver microsomes, the pharmacokinetics of caffeine, a CYP 1A substrate, was studied following an intragastric administration with 100 mg/kg chrysin. In addition to the oral bioavailability of chrysin, its phase 2 metabolites, chrysin sulfate and chrysin glucuronide, were determined in rat plasma. As results, the pharmacokinetic parameters for caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) were not changed following chrysin treatment in vivo, despite of its inhibitory effect on CYP 1A in vitro. The bioavailability of chrysin was found to be almost zero, because chrysin was rapidly metabolized to its sulfate and glucuronide conjugates in rats. Taken together, it was concluded that the little interaction of chrysin with caffeine might be resulted from the rapid metabolism of chrysin to its phase 2 metabolites which would not have inhibitory effects on CYP enzymes responsible for caffeine metabolism.

• Archives of Pharmacal Research
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• v.26 no.8
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• pp.581-584
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• 2003

Vinylated and allylated chrysin analogues were prepared as congeners of prenylated flavonoids and evaluated their anti-inflammatory activity. 8-Substituted chrysin analogues were prepared from 2 -hydroxy-3 -iodo-4 ,6 -dimethoxyacetophenone in 3 steps. 3-Allylated chrysin analogues were prepared from chrysin in 3 steps. Synthesized chrysin analogues (4, 5 and 8) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.

• Journal of Life Science
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• v.31 no.10
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• pp.929-936
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• 2021

In the present study, we screened candidate natural compounds which possess the strong anti-proliferative effects on human colorectal HCT116 cells using the commercial natural product library (Selleckchem, L1400) based on cell viability assay. Human colorectal cancer HCT116 cells were incubated with 50 μM of each compound from the natural product library, and then cell viability was measured by MTT assay. From the first screening, five different kinds of natural products (chrysin, diosmetin, emodin, piperlongumine, and tanshinone I) were selected based on cell viability assay in HCT116 cells and commercial availability. All selected natural products significantly decreased cell viabilities in HCT116 cells, whereas pro-apoptotic protein NAG-1 is strongly induced by chrysin or emodin treatment. Chrysin and emodin decreased cell viability in a dose-dependent manner. Moreover, chrysin and emodin increased the expression of pro-apoptotic NAG-1 protein in a dose- and time-dependent manner. In addition, PARP cleavage induced by chrysin or emodin was recovered in part by the transfection of NAG-1 siRNA indicating that NAG-1 may be one of the genes responsible for apoptosis induced by chrysin or emodin. Overall, our findings may provide basic screening data on natural products which possess anti-proliferative activities and may help to understand the molecular mechanisms of anti-proliferative and pro-apoptotic activities mediated by chrysin and emodin.

• Toxicological Research
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• v.21 no.1
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• pp.71-75
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• 2005

Chrysin (5,7-dihydroxyflavone) is a flavonoid compound contained in many fruits, vegetables and honey. In our experiment, we investigated genotoxicity of chrysin using bacterial reverse mutation assay, chromosomal aberration test, in vivo micronucleus test. In bacterial reverse mutation assay, chrysin did not induce mutagenicity in Salmonella typhimurium TA98, TA100, TA1535, TA1537, TA102 with and without metabolic activation. In chromosome aberration test, chrysin did not also induce structural and numerical abberations regardless of metabolic activation in Chinese hamster lung fibroblast cells. In mouse micronucleus test, no significant increase in the occurrence of micronucleated polychromatic erythrocytes (MNPCE) was observed in ICR male mice orally administered with chrysin at the dose of 0.5, 1.0, 2.0 g/kg body weight. Taken together these results, chrysin has no mutagenic potential in our experiment.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.613-616
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• 2002

A high-performance liquid chromatographic method has been developed for the separation and quantification of chrysin and synthetic chrysin derivatives (12 chrysin alkyl and 7 chrysin acyl derivatives). The chromatography was performed using a $Nova-Pak^{\circledR}C_{18}$ column. A RP-HPLC was performed by using a binary mixture (MeOH-10 mM H$_3$PO$_4$) as a mobile phase, and the column temperature was maintained at room temperature. A flow rate was 1.0 ml/min, and the effluent was monitored at a wavelenth of 280 nm. The retention times for chrysin acyl and alkyl derivatives were within 10 minutes and 20 minutes, respectively. The absolute recovery of samples were all over 96%. The detection limits were 0.1~18 ng at S/N = 3 ratio.

• Tuberculosis and Respiratory Diseases
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• v.73 no.4
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• pp.204-209
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• 2012

Background: We investigated whether chrysin affected MUC5AC mucin production and gene expression induced by phorbol ester (phorbol 12-myristate 13-acetate, PMA) or epidermal growth factor (EGF) from human airway epithelial cells. Methods: Confluent NCI-H292 cells were pretreated with varying concentrations of chrysin for 30 minutes, and were then stimulated with PMA and EGF for 24 hours, respectively. MUC5AC mucin gene expression and mucin protein production were measured by reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay. Results: Concentrations of $10{\mu}M$ and $100{\mu}M$ chrysin were found to inhibit the production of MUC5AC mucin protein induced by PMA; A concentration of $100{\mu}M$ chrysin also inhibited the production of MUC5AC mucin protein induced by EGF; $100{\mu}M$ chrysin inhibited the expression of MUC5AC mucin gene induced by PMA or EGF. The cytotoxicity of chrysin was checked by lactate dehydrogenase assay, and there was no cytotoxic effect observed for chrysin. Conclusion: These results suggest that chrysin can inhibit mucin gene expression and the production of mucin protein by directly acting on airway epithelial cells.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.18
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• pp.8259-8263
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• 2016

Background: Nano-therapy has the potential to revolutionize cancer therapy. Chrysin, a natural flavonoid, was recently recognized as having important biological roles in chemical defenses and nitrogen fixation, with anti-inflammatory and anti-oxidant effects but the poor water solubility of flavonoids limitstheir bioavailability and biomedical applications. Objective: Chrysin loaded PLGA-PEG-PLGA was assessed for improvement of solubility, drug tolerance and adverse effects and accumulation in a gastric cancer cell line (AGS). Materials and Methods: Chrysin loaded PLGA-PEG copolymers were prepared using the double emulsion method (W/O/W). The morphology and size distributions of the prepared PLGA-PEG nanospheres were investigated by 1H NMR, FT-IR and SEM. The in vitro cytotoxicity of pure and nano-chrysin was tested by MTT assay and miR-34a was measured by real-time PCR. Results: 1H NMR, FT-IR and SEM confirmed the PLGA-PEG structure and chrysin loaded on nanoparticles. The MTT results for different concentrations of chrysin at different times for the treatment of AGS cell line showed IC50 values of 68.2, 56.2 and $42.3{\mu}M$ and 58.2, 44.2, $36.8{\mu}M$ after 24, 48, and 72 hours of treatment, respectively for chrysin itslef and chrysin-loaded nanoparticles. The results of real time PCR showed that expression of miR-34a was upregulated to a greater extent via nano chrysin rather than free chrysin. Conclusions: Our study demonstrates chrysin loaded PLGA-PEG promises a natural and efficient system for anticancer drug delivery to fight gastric cancer.

• YAKHAK HOEJI
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• v.55 no.6
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• pp.462-465
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• 2011

Chrysin analogs with 2-heteroaryl groups were synthesized and evaluated for their inhibitory activities against $PGE_2$ and NO production from LPS-induced RAW 264.7 cells. Chrysin analogs were synthesized from 2-hydroxy-4,6-dimethoxy-acetophenone and heteroaryl aldehydes in 3 steps. The tested chrysin analogs showed decreased inhibitory activity against $PGE_2$ and NO production than those of chrysin.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.223-227
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• 2000

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used for traditional medicines as early as 300 B .C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. To investigate activities of chrysin, one of propolis effective compounds for blood coagulation system was injected endotoxin (4000 EU/kg, i.v.) in rats at 1 hr after administered chrysin (20 mg/kg, p.o.). This study was resulted that chrysin has antiplatelet aggregation activity in vitro, delay of blood clotting time and prothrombin time, and reduction of fibrinogen and FDP in vivo. Chrysin has increased SOD activity, GSH content and GST activity, and decreased MDA content in liver. The result suggests that the antithrombosis effect of chrysin is suppressive activity for a blood coagulation system and antioxidative activity.