• 대한화장품학회지
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• 제39권1호
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• pp.75-81
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• 2013

Chrysin (5,7-dihydroxyflavone)은 프로폴리스, 꿀 같은 음식과 다양한 식물에 존재하는 천연 플라보노이드이다. Chrysin은 항산화, 항노화, 항염, 항암 효과 등 다양한 생물학적 효과를 가진다고 알려져 있다. 이 연구에서, 우리는 사람의 각질형성세포에서 chrysin이 VDR을 통한 transcriptional activity에 미치는 영향을 dual-luciferase assay을 통하여 살펴보았다. Chrysin은 농도 의존적으로 VDR을 통한 transcriptional activity를 증가시켰다. Quantitative real time PCR을 통해 chrysin이 사람의 각질형성세포에서 VDR mRNA의 발현을 증가시킴을 확인하였다. 또한, chrysin이 각질형성세포의 분화 마커인 keratin 10, involucrin 그리고 filaggrin의 mRNA 발현을 증가시킴을 확인하였다. 이러한 연구 결과는 chrysin이 VDR을 통한 transcriptional activity를 조절하여 각질형성세포의 분화를 촉진시킬 수 있다는 것을 시사한다.

• Biomolecules & Therapeutics
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• 제24권4호
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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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• 제26권8호
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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.

• 생명과학회지
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• 제31권10호
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• pp.929-936
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• 2021

본 연구에서는 시판하는 천연물 library (Selleckchem, L1400)로부터 암세포 항 성장 활성을 보여주는 천연물을 선별하였다. 즉, 인간 대장암 세포주인 HCT116에 50 μM의 각 천연물을 처리한 후 세포 생존율을 측정하였다. 1차 선별과정을 통하여 5종의 천연물(chrysin, diosmetin, emodin, piperlongumine, tanshinone I)을 선별하였다. 5종의 천연물에 의한 NAG-1 단백질의 발현을 확인한 결과 chrysin과 emodin에 의해서 발현이 현저하게 증가하였다. 또한, chrysin과 emodin은 농도의존적으로 세포 생존율을 감소시켰으며, chrysin과 emodin은 항암 단백질인 NAG-1의 발현을 농도 및 시간 의존적으로 증가시켰다. 게다가, chrysin과 emodin 처리에 의해 증가된 PARP cleavage가 NAG-1 siRNA transfection에 의해서 감소됨을 확인함으로써, chrysin과 emodin에 의한 세포사멸과 NAG-1의 발현 증가가 직접적인 관련이 있음을 증명하였다. 따라서, 본 연구결과는 암세포 항 성장 활성을 보여주는 천연물 선별에 대한 기초 데이터를 제공해 주며, chrysin과 emodin에 의한 암세포 항 성장 활성 및 세포사멸의 기전을 이해하는 데 도움을 줄 것으로 판단된다.

• Toxicological Research
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• 제21권1호
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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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• 제25권5호
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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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• 제73권4호
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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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• 제16권18호
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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.

• 약학회지
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• 제55권6호
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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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• 제8권3호
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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.