• Title/Summary/Keyword: 대사 억제제

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Inhibition of Tyrosinase by Metabolites Originating from Thrichoderma atroviride (Thrichoderma atroviride 배양액의 tyrosinase 억제제에 관한 연구)

  • Kang, Dong Woo;Kim, Kyu-Min;Kim, Ye-Seong;Seo, Yu-Jin;Song, Da-Yeong;Oh, Da-Yun;Choi, Si-On;Hwang, Ju-Hyeon;Kim, Sam Woong;Bang, Kyu Ho;Gal, Sang Wan
    • Journal of Life Science
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    • v.31 no.1
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    • pp.47-51
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    • 2021
  • In today's society, functional whitening cosmetics are important to beauty. Fungi are known to produce a variety of whitening-related metabolites. In this study, we searched for tyrosinase inhibitors with metabolic products derived from Trichoderma atroviride supernatant in order to apply a material for whitening functional cosmetics. In addition, the inhibitory effect was compared to arbutin, which has already been approved as a whitening raw material by the Korea Ministry of Food and Drug Safety (KMFDS). The metabolites from the T. atroviride supernatant showed higher tyrosinase inhibitory activity than that of arbutin. Some of the tyrosinase inhibitors were stable to heat, whereas some were unstable. The heat unstable material was exhibited in the case of samples treated with little amounts, such as 0.02~0.2%. They were very unstable in acidic and alkali pHs, especially under acidic conditions. However, it was found that a weakly-acidic to neutral pH range was the optimal working pH, especially neutral pH. Since the activity of the inhibitory substances in the T. atroviride supernatant was maintained regardless of proteinase K treatment, it was assumed that the metabolites, but not the bioactive peptides, were involved in the activity. In summary, we propose that the metabolites derived from T. atroviride supernatant have strong potential as whitening raw material.

Solid Medium pH-Dependent Antifungal Activity of Streptomyces sp. Producing an Immunosuppressant, Tautomycetin (면역억제제 Tautomycetin을 생산하는 방선균의 고체배지 pH에 따른 항진균 활성)

  • Hur, Yoon-Ah;Choi, Si-Sun;Chang, Yong-Keun;Hong, Soon-Kwang;Kim, Eung-Soo
    • Microbiology and Biotechnology Letters
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    • v.35 no.1
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    • pp.26-29
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    • 2007
  • Tautomycetin (TMC), which is produced by Streptomyces sp. CK4412, is a novel activated T cell-specific immunosuppressive compound with an ester bond linkage between a terminal cyclic anhydride moiety and a linear polyketide chain bearing an unusual terminal alkene. Antifungal activity against Aspergillus niger and TMC productivity assayed by HPLC using culture extracts from Streptomyces sp. CK4412 grown on solid medium adjusted at various pH were measured. The cells cultured at acidic pH (pH 4-5) medium exhibited much stronger antifungal activity as well as higher TMC productivity than those cultured at neutral pH medium, implying that the acidic pH-shock should be an efficient strategy to induce the productivity of secondary metabolites in Streptomyces culture.

The Effect of Ginseng Saponins on the Biosynthesis of Prostaglandins (인삼 Saponin이 Prostaglandin 대사에 미치는 영향)

  • Park C.W.;Lee S.H.
    • Proceedings of the Ginseng society Conference
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    • 1988.08a
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    • pp.77-80
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    • 1988
  • The effects of ginseng saponins and some phenolic acids on the in vitro biosynthesis of prostaglandins was examined in order to identify the role of some ginseng components on the regulaion of arachidonic acid metabolism. The productions of prostaglandin $E_2(PGE_2).$ prostaglandin $F_2{\alpha}(PGF_2{\alpha}).$ thromboxane $B_2(TxB_2)$ and 6-keto-prostaglandin $F_1{\alpha}(6-keto-PGF_1{\alpha})$ from $[^3H]-arachidonic$ acid were evaluated with rabbit kidney microsome. human platelet homogenate and bovine aortic microsome. The amounts of the total cyclooxy-genase products from arachidonic acid did't show significant changes in the presence of ginseng saponins. Panaxadiol. panaxatriol and all of the ginsenosides used in these experiments reduced the formation of $TxB_2.$ while increased the $6-keto-PGF_1{\alpha}$ production dose dependently. Ginseng saponins did't inhibit the ADP($10{\mu}M$) induced platelet aggregation. but sodium arachidonate (0.5 mM) induced platelet aggregation. but sodium arachidonate (0.5 mM) induced platelet aggregation was signiticantly inhibited. These findings suggest that ginseng saponins seem to playa role in the regulation of the arachidonate metabolism. probably by affecting the divergent biosynthetic pathway of prostaglandins from endoperoxide.

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Pregnenolone Metabolism in the Ovarian Thecal Layers of the Rainbow Trout, Oncorhynchus mykiss: in vitro Inhibitory Effects of Cyanoketone and Trilostane (무지개송어 (Oncorhynchus mykiss)의 난소내 협막층(theca layers)에서의 Pregnenolone 대사: cyanoketone과 trilostane의 저해 효과)

  • BAEK Hea-Ja;FOSTIER Alex
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.28 no.4
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    • pp.469-474
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    • 1995
  • The effects of sperific inhibitors of $3\beta-hydroxy-\Delta^5-steroid\;dehydrogenase$ $(3\beta-HSD;\;an\;enzyme\;catalyzing\;conversion\;of \Delta^5\;steroids\;to\;\Delta^4 steroids),$ cyanoketone and trilostane, on $^3H-pregnenolone$ metabolism in isolated ovarian thecal layers have been investigated in vitro. At all doses of cyanoketone $(10^{-5}\;and\;10^{-4}\;M)$ and trilostane $(10^{-5}\;and\;10^{-4}\;M)$ $(3\beta-HSD$ enzyme activity that transforms pregnenolone to $17\alpha-hydroxyprogesterone$ was inhibited in the thecal layers. Trilostane appeared to be more efficient than cyanoketone. Trilostane at doses of $10^{-8},\;10^{-7},\;10^{-6},\;and\;10^{-5},\;M/ml$ caused a dose-response inhibition of $\Delta^4$ steroids accumulation in the medium from pregnenolone, but not completely blocked the conversion of $\Delta^5\;to\;\Delta^4$ steroids.

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Pathophysiological Functions of Deubiquitinating Enzymes in Obesity and Related Metabolic Diseases (탈유비퀴틴화 효소 DUBs의 비만 및 대사 관련 질환에서 병태생리학적 기능)

  • Lee, Seul Gi;Kwon, Taeg Kyu
    • Journal of Life Science
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    • v.32 no.6
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    • pp.476-481
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    • 2022
  • Ubiquitin signaling regulates virtually all aspects of eukaryotic biology and dynamic processes in which protein substrates are modified by ubiquitin. To regulate these processes, deubiquitinating enzymes (DUBs) cleave ubiquitin or ubiquitin-like proteins from these substrates. DUBs have been implicated in the pathogenesis of cancer, leading to the development of increasing numbers of small-molecule DUB inhibitors. On the other hand, recent studies have focused on the function of DUBs in metabolic diseases such as obesity, diabetes, and fatty liver diseases. DUBs play a positive or negative role in the progression and development of metabolic diseases. Their involvement in cell pathology and regulation of major transcription factors in metabolic syndrome has been examined in vitro and in animal and human biopsies. UCH, USP7, and USP19 were linked to adipocyte differentiation, body weight gain, and insulin resistance in genetic or diet-induced obesity. CYLD, USP4, and USP18 were found to be closely associated with fatty liver diseases. In addition, these liver diseases were accompanied by body weight change in certain cases. Collectively, in this review, we discuss the current understanding of DUBs in metabolic diseases with a particular focus on obesity. We also provide basic knowledge and regulatory mechanisms of DUBs and suggest these enzymes as therapeutic targets for metabolic diseases.

A Study on the Antilipidperoxidative Effects of Brazilin and Hematoxylin(I) (천연색소 Brazilin 및 Hematoxylin의 항지질 과산화활성에 관한 연구 (I))

  • 문창규;하배진;이수환;목명수
    • Journal of Food Hygiene and Safety
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    • v.2 no.1
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    • pp.35-40
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    • 1987
  • The antilipidperoxidative effects of Brazilin and Hematoxylin were investigated at the levels of liver~total homogenates, -microsomal fraction, -mitochondrial fraction and the sera of SD-rats intoxicated with $CCl_4$ and ethanol. Both natural dyes markedly inhibited the lipidperoxidation induced by $CCl_4$ and ethanol. Brazilin and Hematoxylin showed the inhibitory effects on the both enzymatic (NADPH-dependent) and nonenzymatic (Ascorbate-induced) lipidperoxidation pathways. but it is supposed that the antilipidperoxidative powers of them mainly result from the inhibition of the nonenzymatic lipidperoxidation.

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Application of HPLC with Electrochemical Detection to Assaying Tyrosine Hydroxylase Activity and Dopamine Content in Dissociated Cultures of Fetal Rat Brainstem (흰쥐 태 뇌간의 세포배양에서 HPLC-전기화학검출을 이용한 Tyrosine Hydroxylase 활성 및 Dopamine의 정량)

  • Song, Dong-Keun;Wie, Myung-Bok;Park, Chan-Woong;Kim, Yung-Hi
    • The Korean Journal of Pharmacology
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    • v.27 no.1
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    • pp.7-12
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    • 1991
  • We measured the developmental increase of tyrosine hydroxylase(TH) activity and dopamine content with high performance liquid chromatography with electrochemical detection(HPLC-EC) in dissociated cultures of fetal rat brainstem(E14). TH activity and dopamine content increased progressively upto 7 days in vitro, when the effects of various drugs on the dopamine contents were studied. ${\alpha}-Methyl-p-tyrosine$, a TH inhibitor and NSD-1015, an inhibitor of aromatic amiono acid decarboxylase effectively depleted dopamine contents. Dopamine contents were depleted by reserpine and increased by pargyline. When cultures grown for 1 week in control medium were then exposed to tetrodotoxin$(0.1\;{\mu}M$) for 7 days, exposure to tetrodotoxin markedly decreased TH activity. All the above results indicate that dopamine metabolism in the cultered cells reflect reliably the property of brain dopamine metabolism. We suggest that measuring TH activity and dopamine content in brainstem culture with HPLC-EC can be useful tool in the study of pharmacology as well as toxicology of the central dopaminergic system.

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Dichloroacetate Inhibits the Proliferation of a Human Anaplastic Thyroid Cancer Cell Line via a p53-independent Pathway (Dichloroacetate의 p53 비의존적 경로를 통한 인간 역분화 갑상선 암세포주의 성장억제 효과)

  • KC, Yam Bahadur;Poudel, Sunil;Jeon, Eon Ju;Shon, Ho Sang;Byun, Sung June;Jeoung, Nam Ho
    • Journal of Life Science
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    • v.28 no.12
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    • pp.1469-1476
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    • 2018
  • Occurrence of the Warburg effect in solid tumors causes resistance to cancer chemotherapy, and targeting energy metabolisms such as aerobic glycolysis is a potential strategy for alternative treatment. Dichloroacetate (DCA), an inhibitor of pyruvate dehydrogenase kinase (PDK), shifts glucose metabolism from aerobic glycolysis to oxidative phosphorylation (OxPhos) in many cancers. In this study, we investigated the anticancer effect of DCA on a human anaplastic thyroid cancer (ATC) cell line, 8505C. We found that DCA selectively inhibits cell proliferation of the 8505C line but not of a normal thyroid line. In 8505C, the cell cycle was arrested at the G1/S phase with DCA treatment as a result of decreased antiapoptotic proteins such as $HIF1{\alpha}$, PDK1, and Bcl-2 and increased proapoptotic proteins such as Bax and p21. DCA treatment enhanced the production of reactive oxygen species which consequently induced cell cycle arrest and apoptosis. Interestingly, DCA treatment not only reduced lactate production but also increased the expression of sodium-iodine symporter, indicating that it restores the OxPhos of glucose metabolism and the iodine metabolism of the ATC. Taken together, our findings suggest that PDK inhibitors such as DCA could be useful anticancer drugs for the treatment of ATC and may also be helpful in combination with chemotherapy and radiotherapy.

Effects of Asparagus cochinchinensis (Lour.) Merr. on the Stimulation of Osteoblast Differentiation and Inhibition of Osteoclast Generation (천문동 추출물에 의한 조골세포 분화 촉진 및 파골세포 생성 억제효과)

  • Lee, Seung-Youn;Kim, Si-Na;Kim, Jong-Keun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.1
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    • pp.16-19
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    • 2008
  • Bone mass in adults decreases with age because of the imbalance between the rate of bone formation and resorption. We performed this study to investigate whether Asparagus cochinchinensis (Lour.) Merr. (ACAE) plays a role in osteoblasts differentiation and osteoclasts formation. Ethanol extract of ACAE showed increase in the differentiation and alkaline phosphatase activity of osteoblasts. Also, it decreased the number of tartrate-resistant acid phosphatase (TRAP)-positive multinucleated cells (OCLs) and TRAP activity. Therefore, ACAE has the potential to prevent bone-related diseases such as osteoporosis by increasing the differentiation of osteoblasts and reducing both the number and activity of osteoclasts.

[ $^{14}CO_2$ ] Assimilation and Metabolism of $^{14}C-$Assimilates in Whole Plants of Spring Barley In Relation to Adult-Plant Resistance to Powdery Mildew (흰가루병에 대해 성체식물 저항성을 지닌 봄보리에서 $^{14}CO_2$ 동화와 $^{14}C-$동화산물의 대사)

  • Hwang Byung Kook;Ibenthal Wolf-Dieter;Heitefuss Rudolf
    • Korean Journal Plant Pathology
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    • v.2 no.1
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    • pp.22-30
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    • 1986
  • The effect of powdery mildew infection on the $^{14}CO_2$ assimilation and metabolism of $^{14}C-$assimilates was studied with spring barley cultivars, susceptible Peruvian and adult-plant resistant Asse at the four-leaf stage. No consistent differences between Peruvian and Asse were revealed in $^{14}CO_2$ assimilation and metabolism of $^{14}C-$assimilates in healthy whole plants. In the two cultivars, $^{14}CO_2$ assimilation and translocation of assimilates decreased as the number of infected leaves increased. Despite the same infection intensity, $^{14}CO_2$ assimilation was less inhibited in Asse than Peruvian. Infection reduced the fixation of $^{14}CO_2$ in noninfected fourth leaves of Peruvian more severely than that of Asse. Infection of the lower 3 leaves also inhibited the incorporation of 14 C into carbohydrates such as fructose and glucose in noninfected fourth leaves and their translocation into leaf sheathes, the inhibitions being greater in Peruvian than Asse. In the infected third leaves, there was a reduction of 14 C-activity in carbohydrates, more $^{14}C-$labeled fructose and glucose being retained in Peruvian. The stimulation of $^{14}C-$organic acid synthesis in all plant organs was more pronounced in Peruvian than Asse. Powdery mildew markedly increased the incorporation of $^{14}C$ into amino acids in infected third and noninfected fourth leaves, but reduced their translocation to the leaf sheathes. A greater rise of $^{14}C-$ activity in some amino acids in the two leaves was found in Peruvian than Asse.

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