• Title/Summary/Keyword: Chemical-induced inhibition

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Physicochemical Characteristics and Biological Activities of Monascus-fermented Angelica gigas Nakai by Origin (산지별 홍국발효 참당귀의 이화학적 특성 및 생리활성)

  • Park, Kyu-Rim;Kim, Young-Wan;Kim, Tae-Hoon;Ahn, Hee-Young;Sim, So-Yeon;Kim, Jung-Wook;Cho, Young-Su
    • Journal of Life Science
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    • v.27 no.8
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    • pp.919-929
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    • 2017
  • This study investigated the biological activities and chemical characteristics of Monascus-fermented Angelica gigas Nakai (A. gigas) with a view to the development of health foods. We also investigated the effect of the cultivation region of three A. gigas cultivars, namely Sancheong, Pyeongchang, and Jecheon. After fermentation, the content of decursin and decursinol angelate was increased compared to non-fermentation; the highest content of decursin and decursinol angelate was found in non-fermentation Pyeongchang A. gigas (PA) at 615.504, 326.742 ppm and fermented Pyeongchang A. gigas (FPA) at 792.610, 429.500 ppm, respectively. The highest content of phenolic compounds, flavonoids, and minerals was found in the FPA group, in which DPPH (${\alpha},{\alpha}^{\prime}-diphenyl-{\beta}-picrylhydrazyl$) radical scavenging activity and Fe/Cu reducing power were stronger in fermented than in non-fermented A. gigas. The FPA group in particular showed the highest activity. We measured nitric oxide (NO) production from lipopolysaccharide-induced RAW 264.7 cells and the inhibition of cancer cell proliferation. The inhibition of activity of NO production and cancer cell (MCF-7 and Hep3B) viability was significantly decreased in the FPA group. The results suggest that FPA may be highly useful as a health food. Overall, the study provides basic data for understanding the biological activities and chemical characteristics of A. gigas fermented by Monascus purpureus for the development of health foods.

Influence of Endogenous Catecholamines on Guanabenz- lnduced Inhibition of Micturition Reflex in Rats (Guanabenz 투여에 의한 흰쥐의 배뇨반사억제작용에 미치는 내인성 Catecholamines의 영향)

  • Park, Sang-Yeoul;Sohn, Uy-Dong;Kim, Choong-Young
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.67-74
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    • 1989
  • The effect of guanabenz on volume-induced micturition reflex contraction (VIMRC) in urethane-anethetized female rats was examined under adrenalectomy, chemical-sympathectomy, ganglionectomy, alpha-1, or alpha-2 blockade. Intracerbroventricular administration of guanalberz had little effect on VIMRC, but topical application suppressed amplitude and frequency of VIMRC. Guanabenz intravenous injection dose-dependently suppressed amplitude and frequency of VIMRC, with complete inhibition at dose of $100\;{\mu}g/kg$, but phenylephrine had no effect on VIMRC. Intravesicular peak pressure and amplitude of VIMRC were increased by 6-hydroxydopamine (6-OHDA) treatment when compared with control value, but yohimbine-, prazosin-hexamethonium-treatment and adrenalectomy did not show changes in VIMRC. Dose-response curve of guanabenz on amplitude and frequency of VIMRC shifted significantly to the right by treatment of yohimbine and 6-OHDA, and adrenalectomy. Median inhibitory dose $({\mu}g/kg)$ of guanabenz to amplitude of VIMRC showed 27.3 in control group, 381.6 in yohimbine, 294.1 in 6-OHDA and 54.1 in hexamethonium, and 38.8 in prazosin. Those of guanabenz to frequency of VIMRC showed 41.7 in control group, 571.1 in yohimbine, 410.8 in 6-OHDA, 141.4 in adrenalectomy, 59.6 in hexamethoinum and 31.4 in prazosin. These results suggest that guanabenz inhibits VIMRC through alpha-2 receptor stimulation rather than alpha-1 receptor stimulation and that catecholiamines released from sympathetic nerve ending and adrenal gland play a role in the inhibition.

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Study on Cosmeceutical Activities and Anti-inflammatory Activities of Magnolia biondii Extracts (신이화(辛夷花, Magnoliae Flos)추출물의 화장품약리활성 및 항염증효과에 관한 연구)

  • Kim, Young-Hun;Sung, Ji-Yeon;Seo, Kyo-Seong;Shin, Jae-Cheon;Kim, Byung-So;Yeum, Jeong-Hyun;Lee, Jin-Tae
    • Journal of Life Science
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    • v.22 no.6
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    • pp.730-735
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    • 2012
  • Existing pharmaceutical studies show that Magnolia biondii is effective in treating rhinitis and in reducing cholesterol, given its endogenous, volatile ingredients. The study herein seeks to assess the cosmeceutical activities and anti-inflammatory activities of Magnolia biondii extracts for possible application as cosmetic ingredients. The cosmeceutical and anti-inflammatory activities were investigated using hydroxyl radical scavenging, superoxide dismutase (SOD)-like activity, xanthine oxidase (XO) inhibition, cell viability, nitric oxide (NO) inhibition, and inducible nitric oxide synthase (iNOS) expression by Western blotting. Magnolia biondii extracts were identified to have antioxidant activities in hydroxyl free radical scavenging, SOD-like activity, and XO inhibition. In testing the anti-inflammatory activities of the extracts, NO production was inhibited in a dose-dependent manner. Additionally, in a dose-dependent manner, the Magnolia biondii extracts were able to suppress iNOS expression in LPS-stimulated RAW 264.7 macrophage cells. From these results, Magnolia biondii showed adequate potential for application in cosmetic production and related industries as well as a functional material.

Effects of Cheongyeolyunbu-tang on DNFB-induced Allergic Dermatitis (청열윤부탕(淸熱潤膚湯)이 DNFB로 유발된 알레르기 피부염에 미치는 효과)

  • Lee, Kyung-Ki;Kim, Jin-Ju;Jung, Hee-Jae;Jung, Sung-Ki
    • The Journal of Internal Korean Medicine
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    • v.29 no.3
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    • pp.730-741
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    • 2008
  • Objective : To examine the efficacy of CY, the improvement of atopy dermatitis(AD)-like lesions on the rostral back of the NC/Nga mice, which took CY orally and were treated with a chemical substance called DNFB, the inhibition of ear swelling, and the inhibition of inflammatory response of the ear tissue of the mice were observed and compared, and the inhibition of the serum IgE count and the IL-4 and IFN-${\gamma}$ count produced by CD4+ T cells of the lymph node were observed and compared. Materials and Methods : For measurement of ear thicknesses, 0.15% DNFB $25{\mu}l$ mixed with acetone/olive oil(3:1) was applied to the right ear and dorsal skin of the NC/Nga mice 5 times at an interval of 7 days. Ear thickness was measured every day over a five-week period after the first application of DNFB. The total serum IgE count was measured with ELISA by taking blood samples 24 hours after the fifth application of DNFB. To measure the IL-4 and IFN-${\gamma}$ count, the lymph node was cut off, and the CD4+ T cells were purified and stimulated to activate the T cells, and then the IL-4 and IFN-${\gamma}$ count was measured with ELISA. Results : Continuous oral administration of CY improved the AD-like skin lesions on the rostral back and inhibited the ear swelling in NC/Nga mice treated with DNFB and inhibited the inflammatory response in the NC/Nga mice treated with DNFB NC/Nga mice. Continuous oral administration of CY did not significantly inhibit the serum IgE count and failed to significantly reduce the IL-4 count generated after TCR stimulation in the CD4+ T cells of the NC/Nga mice treated with DNFB. Continuous oral administration of CY significantly reduced the IFN-${\gamma}$ count generated after TCR stimulation in the CD4+ T cells of the NC/Nga mice treated with DNFB.

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GS28 Protects Neuronal Cell Death Induced by Hydrogen Peroxide under Glutathione-Depleted Condition

  • Lee, Hwa-Ok;Byun, Yu-Jeong;Cho, Kyung-Ok;Kim, Seong-Yun;Lee, Seong-Beom;Kim, Ho-Shik;Kwon, Oh-Joo;Jeong, Seong-Whan
    • The Korean Journal of Physiology and Pharmacology
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    • v.15 no.3
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    • pp.149-156
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    • 2011
  • Golgi SNAP receptor complex 1 (GS28) has been implicated in vesicular transport between intra-Golgi networks and between endoplasmic reticulum (ER) and Golgi. Additional role(s) of GS28 within cells have not been well characterized. We observed decreased expression of GS28 in rat ischemic hippocampus. In this study, we examined the role of GS28 and its molecular mechanisms in neuronal (SK-N-SH) cell death induced by hydrogen peroxide ($H_2O_2$). GS28 siRNA-transfected cells treated with $H_2O_2$ showed a significant increase in cytotoxicity under glutathione (GSH)-depleted conditions after pretreatment with buthionine sulfoximine, which corresponded to an increase of intracellular reactive oxygen species (ROS) in the cells. Pretreatment of GS28 siRNA-transfected cells with p38 chemical inhibitor significantly inhibited cytotoxicity; we also observed that p38 was activated in the cells by immunoblot analysis. We confirmed the role of p38 MAPK in cotransfected cells with GS28 siRNA and p38 siRNA in the cell viability assay, flow cytometry, and immunoblot. Involvement of apoptotic or autophagic processes in the cells was not shown in the cell viability, flow cytometry, and immunoblot analyses. However, pretreatment of the cells with necrostatin-1 completely inhibited $H_2O_2$-induced cytotoxicity, ROS generation, and p38 activation, indicating that the cell death is necroptotic. Collectively these data imply that $H_2O_2$ induces necroptotic cell death in the GS28 siRNA-transfected cells and that the necroptotic signals are mediated by sequential activations in RIP1/p38/ROS. Taken together, these results indicate that GS28 has a protective role in $H_2O_2$-induced necroptosis via inhibition of p38 MAPK in GSH-depleted neuronal cells.

Phytoecdysones from the Roots of Achyranthes japonica Nakai and their Anti-atopy Activity (우슬의 뿌리로부터 Phytoecdysones의 분리와 항 아토피 효과)

  • Kim, Ki Ohk;Ku, Chang-Sub;Kim, Min-Jin;Park, Yhun Jung;Ryu, Hyung Won;Song, Hyuk-Hwan;Kim, Jung Hee;Oh, Sei-Ryang
    • Journal of Applied Biological Chemistry
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    • v.58 no.1
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    • pp.13-19
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    • 2015
  • The roots of Achyranthes japonica Nakai were extracted with 100% aqueous and concentrated subfraction was separated with ultra-performance liquid chromatography-based activity profiling. Three compounds were isolated from the subfraction 5 through the repeated prep- high performance liquid chromatography column chromatography. According to the results of physico-chemical and spectroscopic data including NMR and MS, the chemical structures of the compounds were determined as ecdysterone (1), 25S-inokosterone (2), and 25R-inokosterone (3). Three phytoecdysones were showed weak inhibitory activity for thymus and activation-regulated chemokine expression levels in tumor necrosis factor (TNF)-${\alpha}$ plus IFN-${\gamma}$ induced HaCaT cells, respectively. However, those compounds 1-3 were exhibited the most potent inhibition (80-95% at $200{\mu}g/mL$) against TNF-${\alpha}$ expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells. As result, 100% aqueous extract of A. japonica has an excellent anti-atopy activity. It could be used to a large range of functional anti-atopy cosmetics.

Effect of mixtures of gibberellic acid and several herbicides on the herbicidal activity against wild oat (Avena fatua L.) (Gibberellic acid와 여러 가지 제초제와의 혼합처리가 메귀리에 대한 제초활성에 미치는 영향)

  • Kim, Jin-Seog;Choi, Jung-Sup;Hong, Kyung-Sik;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.2 no.3
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    • pp.107-116
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    • 1998
  • Based on the differential growth response to exogenous gibberellic acid ($GA_{3}$) between semi-dwarf wheat(Triticum aestivum) and wild oat(Avena fatua), we examined the possibility of improving the selective performance of several herbicides by $GA_{3}$ application and the physiological background of $GA_{3}$-induced increase in herbicidal activity. Growth of wild oat was 4 to 5 times higher than that of wheat by $GA_{3}$ treatment. Pretreatment of wild oat seed with 300 ppm $GA_{3}$ increased the herbicidal activities of trifluralin and isoproturon by soil-surface application, but not of alachor and metsulfuron-methyl. $GA_{3}$ applied simultaneously with post-emergence herbicides resulted in a significant or moderate improvement of the efficacy of such herbicides as tralkoxydim, fenoxaprop-ethyl, metsulfuron-methyl, metribuzine and isoproturon, but not in the mixtures of oxyfluorfen or paraquat with $GA_{3}$. In the sequencial treatment of tralkoxydim and $GA_{3}$ at interval of one-day, $GA_{3}$ applied prior to tralkoxydim significantly increased a chlorosis and desiccation of leaf without affecting the growth inhibition by tralkoxydim. Tralkoxydim followed by $GA_{3}$ application had lower herbicidal activity than that of $GA_{3}$ followed by tralkoxydim treatment. Electrolyte leakage response of $GA_{3}$-pretreated or $GA_{3}$-untreated wild oat leaf against several compounds inducing membrane. peroxidation was compared. Differencial responses were observed in oxyfluorfen and isoproturon treatments with an increased electrolyte leakage in $GA_{3}$-pretreated tissue, but not in paraquat and rose bengal treatments. These results suggest that $GA_{3}$-induced increase in herbicidal activity is likely to be dependent on a herbicide type and may be due to activation of a metabolic ability related with herbicidal reponse as well as an increase in the herbicide absorbtion and translocation, rather than due to membrane and cell wall extention induced by $GA_{3}$, which in turn makes the herbicides easily enter.

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The Effect of Vitamin A Derivatives on the Activity of Drug-metabolizing Enzyme in Rat Liver (Vitamin A 유도체로 인한 간의 약물대사효소 변동)

  • Lee, H.W.;Ryu, K.Z.;Ro, J.Y.;Hong, S.S.
    • The Korean Journal of Pharmacology
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    • v.18 no.1
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    • pp.65-72
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    • 1982
  • It has been known that retinoids are intrinsically of critical importance for control of premalignant epithelial cell differentiation. In the absence of retinoids, normal cellular differentiation and growth does not occur in epithelia such as those of trachea and bronchi. Furthermore, it was also reported that retinoid deficiency enhanced susceptibility to chemical carcinogenesis in the respiratory system, in the bladder, and in the colon of the experimental animal. In 1974, Bollag examined the effects of synthetic retinoids in prevention of development of cancer and demonstrated synthetic retinoids to have more favorable therapeutic index than retinoic acid for causing regression of skin papilloma in mice. Therefore, it was assumed that this anticarcinogenic effect of vitamin A derivatives could be due to modification of the metabolism of the carcinogenic polycyclic hydrocarbon, which must first be activated to exert their effect. Hill and Shih reported that vitamin A compounds and analogs had inhibitory effect on drug metabolizing enzyme from liver and lung tissue of mouse and hamster. Lucy suggested that the chemoprevention effect of vitamin A derivatives is due to reaction with molecular oxygen, and it is possible that inhibition of hydroxybenzpyrene formation is a result of this property. On the other hand, butylated hydroxytoluene which is a potent antioxidant strongly inhibited the formation of mammary tumor induced by dimethylbenranthracene. Also, it was observed that this antioxidant inhibited cancer induction in rats by N-2-fluo-renylacetamide. The purpose of this experiment was to investigate the effect of vitamin A derivatives such as retinoic acid and retinoid on drug-metabolizing enzyme and to determine whether riboflavin tetrabutylate or vitamin E could prevent of modify any changes induced by vitamin A delivatives in the rats. The results obtained were as followings. 1) Body weight was significantly reduced by retinoic acid, but not by retinoid. 2) Retinoic acid markedly increased liver weight while retincid showed no effect on liver weight. Treatment of riboflavin tetrabutylate did not affect retinoic acid-induced change in both body weight and liver weight. 3) Both retinoic acid and retinoid remarkably decreased the activity of aminopyrine demethylase. Pretreatment of riboflavin tetrabutylate, however, prevented inhibitory effect of retinoic acid on the enzyme activity. 4) No significant effect of vitamin E on aminopyrine demethylase was observed in both groups treated with retinoic acid and retinoid.

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The Anti-Fibrogenic Effect of a Pharmaceutical Composition of[5-(2-Pyrazinyl)-4-methyl-1,2-dithiol-3-thione] (Oltipraz) and Dimethyl-4,4′-dimethoxy-5,6,5′,6′-dimethylene dioxybiphenyl-2,2′-dicarboxylate (DDB)

  • Kang, Keon-Wook;Kim, Yoon-Gyoon;Kim, Choon-Won;Kim, Sang-Geon
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.655-663
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    • 2002
  • Liver fibrosis is a prepathological state wherein damaged liver tissues in chronic liver diseases, such as hepatitis, are not repaired to normal tissues, but converted to fibrous tissue. 5-(2-Pyrazinyl)-4-methyl-1,2-dithiol-3-thione (oltipraz), a cancer chemopreventive agent, is effective against a wide variety of chemical carcinogens. Recently, we reported that oltipraz inhibits liver fibrogenesis (Kang et al., 2002). In the present study, the effects of oltipraz in combination with dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylene dioxybiphenyl-2,2'-dicarboxylate (DDb) on dimethylnitrosamine (DMN)-induced liver fibrogenesis were assessed in rats. Oltipraz (30 mg/kg body weight, po, 3 times per week for 4 weeks) was found to inhibit the increases in plasma ALT, AST and bilirubin by DMN, whereas DDB (30 mg/kg body weight, po, 3 times per week for 4 weeks) attenuated the increases in the plasma ALT and bilirubin. The lowered plasma protein and albumin contents in DMN-treated rats were completely restored by oltipraz, but not by DDB. DDB decreases liver cell injury and inflammation through inhibition of nuclear factor-kB. DMN increased the accumulation of liver collagen, as indicated by the increase in the 4-hydroxyproline content in liver homogenates, which was reduced by treatment with oltipraz, but not by DDB. Given the differential effect between oltipraz and DDB, the potential enhancement of antifibrotic efficacy by the drugs was assessed in the animal model. Despite the minimal effect of DDB on DMN-induced fibrogenesis, DDB (5-25 mg/kg), administered together with oltipraz (25-5 mg/kg), showed an additive protective effect against hepatotoxicity and fibrosis induced by DMN, which was shown by the blood chemistry parameters and histopathological analysis. The adequate composition ratio of oltipraz to DDB was 5:1. These results provide information on the pharmaceutical composition, comprising of oltipraz and DDB as the active components, for the treatment and/or prevention of liver fibrosis and cirrhosis.

Development of Peptides from the Germinated Black Rice and Applications as Cosmetics Ingredients (발아 흑미 유래 펩타이드의 개발과 화장품 응용에 대한 연구)

  • Dong-hwan, Lee;Jin-hwa , Kim;Jun-tae, Bae;Sung-min, Park;Hyeong-bae, Pyo;Tae-boo, Choe;Bum-chun, Lee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.241-246
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    • 2004
  • To develop novel anti-aging peptides from the germinated black rice, we treated with bromelain, papain and Pronase E. And we investigated the effects of the germinated black rice peptide (GBRP) as anti-aging cosmetic ingredients, and compared with the non-germinated black rice protein (NBRP). We investigated the effects on in vitro inhibition of matrix-metalloprotease (MMP), proliferation of human skin fibroblasts, stimulation of collagen synthesis and expression of UVA-induced MMPs in human skin fibroblasts, UVA induced MMP-1 expression and collagen contents in human skin fibroblasts were analyzed by enzyme-linked immunosorbent assay (ELISA). As a result, the molecular weight distributions of GBRP and NBRP were determined by gel permeation chromatography to be approximately 900 and 10,000 daltons. GBRP increased skin cell proliferation about 40% and reduced UVA-induced MMP-1 expression about 50%. Also the collagen protein level of cells, which were cultured with GBRP, was increased about 25%. These results suggest that the geminated plant seed peptides can be novel anti-aging ingredients for cosmetics.