• Title/Summary/Keyword: Skin concentration

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Quercetin Inhibits ${\alpha}3{\beta}4$ Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes

  • Lee, Byung-Hwan;Hwang, Sung-Hee;Choi, Sun-Hye;Shin, Tae-Joon;Kang, Ji-Yeon;Lee, Sang-Mok;Nah, Seung-Yeol
    • The Korean Journal of Physiology and Pharmacology
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    • v.15 no.1
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    • pp.17-22
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    • 2011
  • Quercetin mainly exists in the skin of colored fruits and vegetables as one of flavonoids. Recent studies show that quercetin, like other flavonoids, has diverse pharmacological actions. However, relatively little is known about quercetin effects in the regulations of ligand-gated ion channels. In the previous reports, we have shown that quercetin regulates subsets of homomeric ligand-gated ion channels such as glycine, 5-$HT_{3A}$ and ${\alpha}7$ nicotinic acetylcholine receptors. In the present study, we examined quercetin effects on heteromeric neuronal ${\alpha}3{\beta}4$ nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding bovine neuronal ${\alpha}3$ and ${\beta}4$ subunits. Treatment with acetylcholine elicited an inward peak current ($I_{ACh}$) in oocytes expressing ${\alpha}3{\beta}4$ nicotinic acetylcholine receptor. Co-treatment with quercetin and acetylcholine inhibited $I_{ACh}$ in oocytes expressing ${\alpha}3{\beta}4$ nicotinic acetylcholine receptors. The inhibition of $I_{ACh}$ by quercetin was reversible and concentration-dependent. The half-inhibitory concentration ($IC_{50}$) of quercetin was $14.9{\pm}0.8\;{\mu}M$ in oocytes expressing ${\alpha}3{\beta}4$ nicotinic acetylcholine receptor. The inhibition of $I_{ACh}$ by quercetin was voltage-independent and non-competitive. These results indicate that quercetin might regulate ${\alpha}3{\beta}4$ nicotinic acetylcholine receptor and this regulation might be one of the pharmacological actions of quercetin in nervous systems.

Involvement of $Cu^{++}$-Catalyzed Peroxidation in Degradation of Collagen and Protective Mechanism of Sodium Salicylate on this Peroxidative Reaction ($Cu^{++}$ 촉매작용에 의한 과산화 현상이 Collagen 손상에 관여함과 Sodium Salicylate에 의한 보호 작용)

  • Kim, Yong-Sik
    • The Korean Journal of Pharmacology
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    • v.23 no.1
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    • pp.25-31
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    • 1987
  • The present study examines firstly, the inhibition of collagen gelation to explore the possible involvement of $Cu^{++}$-catalyzed peroxidation in rheumatoid arthritis and secondly, the effect of sodium salicylate on this peroxidative reaction to provide a possible explanation for its mechanism of anti-inflammatory action. Incubation of collagen obtained from rat skin with $Cu^{++}$ and $H_2O_2$ resulted in the inhibition of gelation in terms of maximal turbidity and lag phase, but either $Cu^{++}$ or $H_2O_2$ alone essentially gave no effect in the collagen gelation. In the presence of sodium salicylate the inhibited gelation of collagen induced by $Cu^{++}$ and $H_2O_2$ was reversed with the dependency of the concentration of sodium salicylate. Moreover, the rate of $H_2O_2$ decomposition by $Cu^{++}$ was accelerated by sodium salicylate and this decomposition of $H_2O_2$ was found to be saturable in terms of concentration of this drugs. Thus it can be expected that $Cu^{++}$ -catalyzed peroxidation attacks collagen resulting in change of structural or functional integrity of collagen, and sodium salicylate may act on this peroxidative process, possibly through the enhancement of catalatic action of $Cu^{++}$. From these results $Cu^{++}$-catalyzed peroxidation can be in part responsible for degradation of joint tissue in rheumatoid arthritis and sodium salicylate may exert its anti-inflammatory action by this peroxidative reaction.

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The Effect of Bangpungtongsung-san Extracts on Adipocyte Metabolism (추출방식에 따른 방풍통성산(防風通聖散)이 지방세포 대사에 미치는 영향)

  • Lee, Sang-Min;Kim, Byoung-Woo;Rhim, Tae-Jin;Kim, Dong-Heui;Kwon, Ki-Rok
    • Journal of Pharmacopuncture
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    • v.11 no.1
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    • pp.163-176
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    • 2008
  • Objective : The purpose of this study is to investigate the effects of Bangpungtongsung-san extracts on the preadipocytes proliferation, of 3T3-L1 cell line. lipolysis of adipocytes in rat's epididymis and localized fat accumulation of porcine by extraction methods(alcohol and water). Methods : Diminish 3T3-L1 proliferation and lipogenesis do primary role to reduce obesity. So, 3T3-L1 preadipocyte and adipocytes were performed on cell cultures, and using Sprague-Dawley rats for the lipogenesis, and treated with 0.01-$1mg/m{\ell}$ Bangpungtongsung-san Extracts depend on concentrations. Porcine skin including fat tissue after treated Bangpungtongsung-san Extracts by means of the dosage dependent variation are investigated the histologic changes after injection of these extracts. Results : Following results were obtained from the 3T3-L1 preadipocyte proliferation and lipolysis of adipocyte in rats and histologic investigation of fat tissue. 1. Bangpungtongsung-san extracts were showed the effect of decreased preadipocyte proliferation on the high dosage($1.0mg/m{\ell}$). 2. Bangpungtongsung-san extracts were showed the effect of decreased the activity of glycerol-3-phosphate dehydrogenase(GPDH) on the high dosage($1.0mg/m{\ell}$) and Specially, alcohol extract of Bangpungtongsung-san was clear as time goes by high concentration. 3. Bangpungtongsung-san extracts were showed tries to compare the effect of lipolysis, alcohol extract of Bangpungtongsung-san on the high dosage($1.0mg/m{\ell}$) was observed the effect is higher than water extract. 4. Investigated the histological changes in porcine fat tissue after treated Bangpungtongsung-san extracts, we knew that water extract of Bangpungtongsung-san was showed the effect of lipolysis on the high dosage($10.0mg/m{\ell}$) and alcohol extract of Bangpungtongsung-san was showed significant activity to the lysis of cell membranes in all concentration. Conclusion : These results suggest that Bangpungtongsung-san efficiently induces diminish proliferation of preadipocyte and lipolysis in adipose tissue.

Antibacterial Activity of Graviola extract to inhibit the Staphylococcus epidermidis (Staphylococcus epidermidis를 억제하는 Graviola 추출물의 항균활성)

  • Choi, Jong-Hwa;Ohk, Seung-Ho
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.5
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    • pp.667-673
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    • 2017
  • This study was carried out to verify the antimicrobial effect of Graviola leaves against pathogenic bacteria for the purpose of developing an antibacterial material. The extraction conditions of graviola leaves were $60^{\circ}C$, $80^{\circ}C$ and $98^{\circ}C$, and graviloa leaves werewater extracted at $60^{\circ}C$, $80^{\circ}C$ and $98^{\circ}C$.The extraction yields and extraction conditions were determined. The antimicrobial activity against S. epidermidis, S. aureus and E. coli TOP10 was evaluated by agar diffusion method. The extraction yields were 3.02%, 14.73% and 20.76% at $60^{\circ}C$, $80^{\circ}C$ and $98^{\circ}C$, respectively. The antimicrobial activity against S. epidermidis, S. aureus and E. coli TOP10 was found in S. epidermidis.In the samples extracted at $98^{\circ}C$, a clear zone of 13 mm was observed at 200 mg/mL and of 20 mm at 500 mg/mL. The MIC was 100 mg/mL. The higher the extraction temperature and concentration, the better was the growth inhibition effect. As a result, the natural antimicrobial activity contained in natural materials can solve the problem of resistance to antibiotics. It is considered that antimicrobial activity against S. epidermidis in skin is highly applicable to basic cosmetics and cosmetic materials.

Anti-inflammaory effects of the Gamroeum in vivo and in vitro (감로음(甘露飮)의 항염증 효과에 대한 실험적 연구)

  • Lim, In-Ho;Jung, Ho-Jun;Kim, Sang-Chan;Jee, Seon-Young
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.23 no.2
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    • pp.13-26
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    • 2010
  • Objectives : The present study was conducted to evaluate the anti-inflammatory effects of the Gamroeum water extracts (GRE) in vivo and in vitro. Methods : The effects of GRE on anti-inflammation were measured by production of NO, $PGE_2$ (Prostaglandin $E_2$), iNOS (inducible Nitric Oxide Synthase), COX-2, $NF{\kappa}B$ (Nuclear Factor kappa B), TNF-$\alpha$ (Tumor Necrosis Factor-alpha) and IL-$1{\beta}$ (Interleukin-$1{\beta}$), IL-6 in Raw 264.7 macrophage cells stimulated with LPS. Results : 1. In machrophage cells, LPS displayed significant stimulatory effects on the production of NO and $PGE_2$. However, GRE showed significant inhibitory effects on NO and $PGE_2$ release. The level of NO and $PGE_2$ was decreased by GRE in a concentration dependent manner as compared with LPS only group. 2. Immunoblot analysis verified that LPS stimulation significantly increased the iNOS and COX-2 protein level, but GRE suppressed the induction of iNOS and COX-2 protein at a concentration dependent manner. 3. GRE reduced the elevated production of TNF-$\alpha$, IL-$1{\beta}$ and IL-6 by LPS. Moreover, the inhibitory effects of GRE was occurred in a dose-dependent manner. 4. GRE significantly reduced the expression of NF-${\kappa}B$ protein in nuclear fraction. 5. GRE effectively inhibited the increases of hind paw skin thicknesses and inflammatory cell infiltrations induced by carrageenan treatment. It, therefore, considered that GRE will be favorably inhibited the acute edematous inflammations. Conclusions : These results indicated that GRE could have anti-inflammatory capacity by inhibiting the production of NO, $PGE_2$ and cytokines in vitro and by reducing the formation of carrageenan-induced paw edema in vivo. Moreover, inhibitory effects of GRE on the macrophage activation were attributable to the reduction of some of inflammatory factors by inhibiting iNOS and COX-2 through the suppression of NF-${\kappa}B$.

The influences of Phaseolus radiatus L.'s Ethanol Extracts and Fractions on Skin Whitening and Anti-inflammatory Effects (녹두(綠豆) 에탄올 추출물 및 분획물이 피부의 미백, 항염증 효과에 미치는 영향)

  • Lee, Yu-Lim;Choi, Jung-Hwa;Park, Soo-Yeon;Jeong, Min-Yeong;Lee, Ho-Chan;Song, Jie-Hye
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.31 no.3
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    • pp.39-49
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    • 2018
  • Objectives : This study is designed to clarify whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. Methods : In this experiment, we were intended to reveal whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. The whitening activity was confirmed by UV blocking activity, tyrosinase inhibiting activity, and melanin formation inhibiting activity. Anti-inflammatory activity is confirmed by measurement of cytotoxicity level by MTT assay and measurement of Cytokine expression, which is the main mediator of inflammation reaction. Results : As a results, overall activity was high in the ethyl acetate fraction. Tyrosinase inhibitory activity was less than 20% at all concentrations, but the activity to inhibit melanin self-production was higher than that of ethyl acetate fraction at $32.19{\pm}2.79%$ at $100{\mu}g/m{\ell}$. And ethyl acetate fraction had a relatively high UV blocking activity. In the anti-inflammatory test, the concentration-dependent activity was shown, and the chloroform and ethyl acetate fractions showed significant NO production inhibitory activity. Cytokine expression was superior to that of the final stage of B cell differentiation, and cell viability was over 80% except for the chloroform fraction at the concentration of $200{\mu}g/m{\ell}$. Conclusions : The results of this experiment confirmed the whitening effect and anti-inflammatory effect of Phaseolus radiatus L.'s extracts and fractions and report the possibility of application as external medicine.

Study on the Antioxidant Activity of Geranium nepalense subsp. thunbergii Extract (이질풀 추출물의 항산화 효능에 관한 연구)

  • Lee, Sun-Young;Kim, Hyun-Ju;Choi, Shin-Wook
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.1
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    • pp.61-66
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    • 2011
  • Antioxidant activity of Geranium nepalense subsp. thunbergii extract was evaluated by DPPH free radical scavenging assay. Geranium nepalense subsp. Thunbergii extract contains tannin, (-)epicatechin, kaempferitin, kaepferol -7-rhamnoside, brevifolin, corilagin, pyrogallol, ellagitannin, geraniin, gallic acid, succinic acid, quercetin, protocatechuic acid, etc. Geranium nepalense subsp. Thunbergii showed excellent antioxidant activity compared to positive control, quercetin. Geranium nepalense subsp. thunbergii extract showed a 98.33 % inhibition of DPPH radical at a concentration of $50\;{\mu}g/mL$. Quercetin showed a 78.05 % inhibition of DPPH radical at the same concentration. To investigate reactive oxygen species (ROS) scavenging activity, Geranium nepalense subsp. thunbergii extract was treated to human keratinocytes (HaCaT). $IC_{50}$ value of Geranium nepalense subsp. thunbergii extract was $43.22\;{\mu}g/mL$ and $IC_{50}$ value of quercetin was $102.35\;{\mu}g/mL$. Geranium nepalense subsp. thunbergii extract showed excellent antioxidant activity. Skin irritation test and cytotoxicity test suggested that Geranium nepalense subsp. thunbergii extract is a safe antioxidant ingredient for cosmetics.

Cytotoxic Effects of 1, 2-Hexanediol and 1, 2-Hexanediol Galactoside on HaCaT Cell (1, 2-Hexanediol과 1, 2-Hexanediol Galactoside의 HaCaT Cell에 대한 세포독성)

  • Kim, Jun-Sub;Jung, Kyung-Hwan
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.44 no.3
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    • pp.343-347
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    • 2018
  • We synthesized 1, 2-hexanediol galactoside (HD-Gal) from HD using Escherichia coli (E. coli) ${\beta}-galactosidase$ (${\beta}-gal$), in which the reaction is generally called as transgalactosylation (reverse hydrolysis). In this study, we investigated how much HD-Gal and HD had a cytotoxic effect on HaCaT cell, in order to compare HD-Gal with HD in terms of the cytotoxicity of human skin cell. Cell proliferation assay and phase-contrast microscope observation were used for investigating the cytotoxicity. As a result, HD-Gal had not cytotoxic effect on HaCaT cell in the concentration range from 42.2 to 211 mM. In addition, when we observed the cells using microscopy, there was no change in the cell morphology. Meanwhile, when 42.2 mM and 84.4 mM HD were treated on HaCaT cell, we did not observe the cytotoxicity; however, when 168.8 mM and 211 mM HD were on HaCaT cell, HD had a higher cytotoxic effect on HaCaT cell. In addition, when HD was treated on the cells regardless of the concentration of HD, there were obvious changes in cell morphology and cell number. It was expected hopefully that HD-Gal would be applicable as a substitute for HD as a less toxic preservative in views of safety, health, and well-being.

Evaluation for Antioxidant Effects and Water-holding Capacity of Rice Protein Extracts from Cheongwon Area (청원 지역 쌀단백질 추출물의 항산화 및 수분 보유력 평가)

  • Chio, Hyoung-Chul;Jung, Su-Hyun;Jeong, Noh-Hee
    • Applied Chemistry for Engineering
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    • v.31 no.4
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    • pp.398-403
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    • 2020
  • In this study, six kinds of rice grown in Cheongwon area were extracted using glycolytic and proteolytic enzymes, and also antioxidant effects and water holding capacity of rice protein extracts were compared and analyzed. Protein contents of rice cultivars protein extract showed that black rice (BR) extract was the highest at 4,900 ㎍/mL, and flavored brown rice (FBR) extract was the lowest at 3,700 ㎍/mL. 2,2-diphenyl-1-picryl-hydrazyl-hydrate free radical scavenging activity was confirmed the superior activity of more than 80.0% at a concentration of 2 mg/mL with BR and red brown rice (RBR) extracts. 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activity at a concentration of 2 mg/mL with BR and RBR extracts was more than 70.0% The water holding capacity for extracts using RBR, red-kerneled brown rice (RKBR), BR and FBR was more than 110.0%. Overall, the rice protein extract using BR has excellent antioxidant and water holding capacity which can be used as a potential skin moisturizer and antioxidant functional cosmetic material.

Study on the Anti-oxidant Effect of Pinus rigida Mill. inner Bark Extracts (리기다소나무(Pinus rigida Mill.) 내수피 추출물의 항산화효과에 관한 연구)

  • Jang, Min-Jung;An, Bong-Jeun;Lee, Chang-Eeon;Lee, Jin-Tae;Lee, Byung-Guen;Lee, Do-Hyung
    • Journal of Korean Society of Forest Science
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    • v.97 no.1
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    • pp.88-94
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    • 2008
  • The aim of the study was to assess the cosmeceutical activity of Pinus rigida Mill. and it is possible that can be used as a cosmetic ingredient for application of cosmetic industries. The concentration of total phenolic compound of P. rigida water soluble fraction and P. rigida ethyl acetate soluble fraction showed 47 mg/L and 601 mg/L respectively. In the result of DPPH scavenging radical activity, P. rigida ethyl acetate soluble fraction showed 86% and it was similar to BHA effect at 10 ppm concentration. Xanthine oxidase inhibition of P. rigida water soluble fraction and P. rigida ethyl acetate soluble fraction were 76.3% and 80.5% at 500 ppm, respectively. In the result of tyrosinase inhibition effect related to skin-whitening, P. rigida water and ethyl acetate soluble fraction showed 42%, 10.9% at a 1,000 ppm. In these results, P. rigida has a great potential as a cosmeceutical ingredient with a natural anti-oxidant source.