• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.190-190
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• 1998

$_2$(5,7-dipropoxychrysin), $B_1$(chrysin7-O-toluate), $T_{0}$(5-hydroxy-7-butoxy-chrysin), and $O_1$(5- hydroxy-7 -octoxychrysin) are chrysin derivatives which have isolated from Mori Cortex Radicis. They exhibited strong hypoglycemic effect, so they can be developed for hypoglycemic agents. In this study, we evaluated the acute toxicity of $P_2$, $B_1$, $T_{0}$, and $O_1$ by a single oral administration in rats and mice. The male SD rats and the male ICR mice were divided into 5 groups, and each group was treated orally with 500mg/kg $P_2$, $B_1$, $T_{0}$, and $O_1$, and control respectively. 500mg/kg is the highest dosage which can be administered to mouse. Each group of mice were subdivided as the dosage, 5mg/kg, 20mg/kg, l00mg/kg, and 500mg/kg. After oral administration, we examined food consumption, clinical signs and mortality of each group for 12 days. We also examined body weight increment of animals before and after treatment. Then organ weights were examined on 13th day. There was no toxic effect in mortality, body weight changes, food consumption, clinical signs and organ weights. We found out that the $LD_{50}$ of $P_2$, $B_1$, $T_{0}$, and $O_1$ is more than 500mg/kg in rats.

• 디지털융복합연구
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• 제17권5호
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• pp.399-405
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• 2019

본 연구 목적은 유산소운동과 크리신섭취가 고지방식이동물의 간 조직에서 비만억제 효과를 규명하는데 있다. 집단은 정상식이, 고지방식이, 고지방식이와 크리신섭취, 고지방식이와 유산소운동 4집단으로 하였다. 크리신은 체중당 50mg/kg을 구강투여 하였고, 유산소운동은 트레드밀운동으로 주5회 60분 16주간 실시하였다. SPSS(20.0)프로그램을 이용해 일원변량분석(One-way ANOVA)을 하였고, 사후분석은 LSD로 하였다. 연구결과 간 조직에서 대식세포 마커 F480와 M1대식세포 마커 CD11c는 정상식이 그룹과 비교해 고지방식이, 크리신투여 그룹에서 유의하게 증가했고 운동집단에서는 유의하게 감소하였다. 지방분해 마커 PRDM은 정상식이집단과 비교해 고지방식이, 크리신투여 집단에서 유의하게 감소했으나 운동집단에서만 유의하게 증가하였다. 결론적으로 고지방식이와 중강도 운동은 간 조직에서 발생되는 대사적불균형을 억제하는데 효과적인 것으로 나타났다. 하지만 고지방식이와 크리신 섭취는 비만억제 기능이 미비한 것으로 나타났다. 따라서 향후 기능성식품을 이용한 비만개선 연구는 투여용량, 기간 등을 고려해 다양한 분자적 기전을 살펴보는 연구가 보강되어야 할 것이다.

• Environmental Analysis Health and Toxicology
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• 제10권3_4호
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• pp.29-40
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• 1995

To investigate and evaluate the scavenging and antioxidative effects of various ftavonoids on paraquat induced pulmonary toxicity, in vivo and vitro tests of eight flavonoids(catechin, epicatechin, flayone, chrysin, apigenin, quercetin, morin and biochanin A) were carried out. In vitro test, inhibitory and antioxidative effects of lipoxygenase dependent lipidperoxidation, NADPH dependent cytochrome p-450 reductase to liver and lung microsome and superoxide anion production in rat peritoneal exudated macrophage were studied. In vivo test, biochemical parameters and cell population in bronchoalveolar lavage fluid(BALF) in mouse and rats after administration of paraquat and flavonoids were tested. The results are summerized as follows; 1. All flavonoids tested inhibited on NADPH dependent cytochrome p-450 reductase in liver and lung microsome. 2. All flavonoids tested showed the inhibitory effects on the superoxide anion production in rat peritoneal exudated macropharge. 3. Lactate dehydrogenase, acid phosphatase and total protein in BALF of mouse which increased by the administration of paraquat, decreased significantly by catechin, chrysin, morin and biochanin A. 4. Numbers of alveolar macropharge and PMN in BALF of rats which increased by the administration of paraquat decreased by all the tested flavonoids. Therefore, all flavonoids tested showed the useful compounds for scavenger and antioxidant on paraquat induced pulmonary toxicity.

• BMB Reports
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• 제42권5호
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• pp.265-270
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• 2009

Due to their multiple biological activities, flavonoids have gained attention as potentially useful therapeutics for a variety of diseases including cancer, cardiovascular diseases, and autoimmune diseases. In this study, we demonstrated that several flavonoids, including kaempferol, quercetin, fisetin, and chrysin block TNF-$\alpha$ induced IL-8 promoter activation and gene expression in HEK 293 cells. In addition, phosphorylation and degradation of $I{\kappa}B{\alpha}$ and translocation of NF-${\kappa}B$ p65 were inhibited by these flavonoids in TNF-$\alpha$-stimulated HEK 293 cells. Furthermore, generation of reactive oxygen species (ROS) in response to TNF-$\alpha$ was reduced by the flavonoids. Moreover, although pretreatment with fisetin, quercetin, or chrysin decreased cell viability, kaempferol did not. Taken together, these findings suggest that kaempferol would be useful for the treatment of TNF-$\alpha$-induced inflammatory diseases.

• Environmental Analysis Health and Toxicology
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• 제10권1_2호
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• pp.47-54
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• 1995

To investigate and evaluated the scavenging and antioxidative effects of various flavonoids on paraquat induced toxicity, in vivo and vitro tests of eight flavonoids (catechin, epocatechin, flavone, chrysin, apigenin, quercetin, morin and biochanin A) were carried out. The generation of reactive oxygen substances(ROS) in PMS-NADH system $H_2O_2$ induced hemolysis and lipidperoxidation to blood, NADPH dependent lipidperoxidation to liver and lung microsome by paraquat were studied.The results are summerized as follows; 1) In the concentration ranges from 3.3 to 9.8$\mu$M of catechin,epicatechin, quercetin and biochanin A removed the 50% of DPPH radical scavenging effects. 2) In the concentration ranges from 0.60 to 1.86 mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on superoxide anion which gernerated in PMA-NADH system. 3) In the concentration ranges from 0.12 to 0.49mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on H202 which generated in PMA-NADH system. 4) In the concentration ranges from 0.6 x10$^{-5}$ to 6.3 x 10$^{-5}$mM of catechin, epicatechin, flavone, chrysin, quercetin and morin showed the inhibitory and antioxidative activity on $H_2O_2$ induced hemolysis to blood 5) All flavonoids tested exhibited inhibitory and antioxidative effects on paraquat induced liver and tung microsomal lipidperoxidation. Therefore, all flavonoids evaluated showed the useful compounds for scavenger and antioxidant on paraquat induced toxicity.

• 약학회지
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• 제59권1호
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• pp.12-16
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• 2015

Several 8-cycloalkoxychrysin analogs were synthesized from 6-benzyloxy-5,8-dihydroxyflavone and cycloalkanols in 2 steps and we evaluated their inhibitory activities against NO production from LPS-induced RAW 264.7 cells. Among tested analogs, two analogs with cyclopentyl substructure (796 and 798) showed strong inhibitory activity against NO production.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.247.3-248
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• 2000

• Archives of Pharmacal Research
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• 제16권1호
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• pp.18-24
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• 1993

In this inverstigation, the various flavonoid aglycones were evaluated for their inhibitory activities against croton-oil or arachidonic acid induced mouse ear edema by oral or topical administration. The compounds tested were thirteen derivatives of flavan-3-ol(catechin and epicatechin), flavanone (flavanone and naringenin), flavone (flavone, chrysin and apigenin), flavonol(favonol, galangin, quercetin and morin) and isoflavone (biochanin A and 2-carbethoxy-5,7-dihydroxy-4'-methoxyisoflavone), along with hydrocortisone, indomethacin, 4-bormophenacyl bromide, nordihydroguaiaretic acid and phenidone as positive controls. A(isoflavone) were found to show broad inhibitoty activities (14-52%) against croton-oil or arachidonic acid induced ear edema by oral or topical application at the dose of 2 mg/mouse, although they showed less activity than hydrocortisone (26-88%) or indomethacin (36-80%). Flavonoid agtlycones tested showed higher activity when aplied topically than by the oral administration. It was also found that they inhibited arachidonic acid induced edema more profoundly than croton-oil induced edema by topical application. In arachidonic acid induced edema when applied topically, flavone derivatives such as flavone, chrysin and apigenin were revealed to be the good inhibitory agents in addition to flavonols and isoflavones. When quercetin and biochanin. A were selected for evaluating in carrageenan induced rat pleurisy and biochanin both flavonoids showed antiinflammatory activity at the dose of 70 mg/kg by the oral adminis-tration. All of these results revealed that flavonoid aglycones, especially 5,7-dihydroxy-flavonols having hydroxyl group(s) in B-ring and biochanin A (isoflavone) possessed in vivo antiinflammatory activity.

• Biomolecules & Therapeutics
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• 제7권4호
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• pp.362-370
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• 1999

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents(wax, flavonoids, phenolic compounds, etc.) and has been used in traditional medicines as early as 300 B.C. It was been demonstrated that ethanol, acetylsalicylic acid, ischemia reperfusion, non-steroidal antiin-flammatory drugs and stress induce gastric lesions by promoting the generation of reactive oxygen metabolites. Therefore, some drugs that are capable of scavenging or inhibiting the generation of reactive oxygen radicals might be expected to prevent the gastric mucosal injury. The aim of this study was 1) to examine the antiulcer effect of propolis, 2) to investigate the mechanism of action by determining gastric acid secretion, lipid per-oxidation, mucus content and proton pump ($H^+$/$K^+$-ATPase) activity on gastric mucus in varios experimental models, and finally, 3) to isolate and identify the pure compounds that exert antiulcer activity. Step 2-1 and 2-3 sub-sub fraction shoed a significant reduction of severity of gastirc damage at the dose of 25 mg/kg in various experimental models. We isolated 4 sub-sub-sub fractions by flash column chromatography of Step 2-1 sub-sub fraction and one sub-sub-sub fraction by recrystalization of Step 2-3 sub-sub fraction. The protective effects of propolis sub-sub-sub fraction manifested sifnificant effects in HCl-ethanol induced gastric erosion model and aspirin induced gastric ulcer model. These results showed that the gastric mucosal protective effect of propolis might result from the increase of mucus secretion, free radical scavenging effect as well as the reduction of acid secretion in accordance with the reduction of $H^+$/$K^+$-ATPase activitv. Three compounds were isolated and identified from sub-sub fraction of propolis which showed antiulcer effects. Subsequently, these compounds were identified as a flavonoid, namely, 2-acetoxy-5,7,-dihydroxy-flavanone, galangin and chrysin.

• 약학회지
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• 제43권1호
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• pp.16-22
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• 1999

Scutellaria baicalensis Georgi (Labiatae) has been extensively used in treatment of diarrhea, conjunctivitis, gastritis, enteritis and skin disease. As instructed in old description, the Scutellariae Radix should sometimes be processed before use. To 노디 light on the changes of chemical compositions by processing as well as processing method-activity relationships, Scutellariae Radix was heated at 16$0^{\circ}C$-20$0^{\circ}C$ for 30 min. in furnace or soaked with 20% EtOH (SPE) and boy's urine(SPU), respectively, which are one of processing methods and then heated at 17$0^{\circ}C$ for 30 min. To isolate the chemical components, Scutellariae Radix with/without processing were extracted with EtOH and EtOH extract was fractionated with ether, ethyl acetate and butanol to give respective fractions. Ether and EtOAc fractions obtained from the processed drug with urine (SPU) were subjected to chromatography to obtainsix components, oroxylin A, Wogonin, chrysin, baicalein, baicalein 7-O-$\beta$-D-glucopyranoside and $\beta$-sitosterol 3-O-$\beta$-D-glucopyranoside. All the isolated compounds were identified by means of physicochemical and spectroscopic methods (IR, $^1H-NMR,{\;}^13C-NMR$, Mass). By HPLC determination, the changes of the contents for each isolated components from SPE and SPU samples were observed. It was found that the content of nonglycosidic flavones such as oroxylin A, wogonin, chrysin and baicalein was increased markedly, whereas the content of baicalin and baicalein 7-O-$\beta$-D-glucopyranoside was significantly decreased in both samples as compared with those of Scutellariae Radix. When the sample was soaked with boy's urine, the total amount of nonglycosidic flavones was higher than that of processing with 20% EtOH.