• Title/Summary/Keyword: HMG2

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Serum ${\beta}$-endorphin during Human Menopausal Gonadotropin-Hyperstimulated Menstrual Cycles (Human Menopausal Gonadotropin으로 과배란유도된 월경주기에서의 혈청 ${\beta}$-endorphin에 과한 연구)

  • Kim, Jung-Gu;Mun, Shin-Yong;Chang, Yoon-Seok;Lee, Jin-Yong
    • Clinical and Experimental Reproductive Medicine
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    • v.17 no.2
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    • pp.159-165
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    • 1990
  • It has been reported that endogenous opioid peptides play a role in the control of the reproductive function. The goal of this study was to evaluate changs in the serum levels of ${\beta}$-endorphin during hyperstimulated menstrual cycle and their relationship to serum prolactin levels. Serum ${\beta}$-endorphin and prolactin levels were measured during menstrual cycles of 10 normal cylic women hyperstimulated by human menopausal gonadotropin (HMG) and of 10 women by clomiphene/HMG among in vitro fertilization candidates. The results were summarized as follows. 1. In clomiphene/HMG hyperstimulated menstrual cycle the mean serum ${\beta}$-endorphin level insignificantly on 2 day before aspiration of oocyte compared to basal level and reached maximum level on 1 day after aspiration. 2. There was a significant peak of the mean serum ${\beta}$-endorphin level on 1 day before aspiration in HMG hyperstimulated menstrual cycle. 3. On the same day from aspiration, there was no significant differences in the mean serum ${\beta}$-endorphin levels between HMG and clomiphene/HMG hyperstimulated cycles. 4. No significant correlation was noted between serum ${\beta}$-endorphin levels and prolactin levels.

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Screening of Phenolic Compounds with Inhibitory Activities against HMG-CoA Reductase (페놀 화합물로부터 HMG-CoA reductase 저해 활성 물질 탐색)

  • Son, Kun Ho;Lee, Ju Yeon;Lee, Jeong Soon;Kang, Sam Sik;Sohn, Ho Yong;Kwon, Chong Suk
    • Journal of Life Science
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    • v.27 no.3
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    • pp.325-333
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    • 2017
  • High level of plasma cholesterol is strongly associated with the development of atherosclerosis and coronary heart disease. Clinical trials designed to reduce plasma cholesterol level by diet or pharmacological intervention have resulted in marked reduction of disease incidence. The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which reduces cholesterol biosynthesis in the liver is the key enzyme of the mevalonate pathway that produces cholesterol. In this study, 71 naturally occurring phenolic compounds were tested for inhibitory activities against HMG-CoA reductase. Eleven compounds out of 71 showed inhibitory activities: three hydrolyzable tannin (geraniin, acetonyl geraniin and pentagalloyl ${\beta}-D-glucose$), four benzoic acid derivatives (benzoic acid, trans-cinnamic acid, 2,4-dihydroxybenzoic acid and 2,5-dihydroxybenzoic acid), and four naphthoquinone derivatives (1,2-naphthoquinone, 1,4-naphthoquinone, plumbagin and shikonin). At the concentration of $10{\mu}g/ml$, 1,4-naphthoquinone inhibited HMG-CoA reductase by 99.4%, and then plumbagin 91.4%, pentagalloyl ${\beta}-D-glucose$ 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonyl geraniin 30.2%, benzoic acid 28.5%, geraniin 28.3% and 2,5-dihydroxybenzoic acid 22.3%, respectively. $IC_{50}$ values of 1,4-naphthoquinone and plumbagin was $2.1{\mu}g/ml$ and $5.8{\mu}g/ml$, respectively.

Synthesis and biological activity of 4,5-polymethylenepyrazole-derived HMG-CoA reductase inhibitors

  • Kim, Jin-Il;Choi, Young-Hee;Yurngdong Jahng
    • Archives of Pharmacal Research
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    • v.20 no.2
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    • pp.158-170
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    • 1997
  • New HMG-CoA reductase inhibitors, in which 3-substituted 4, 5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor $(11cc, IC_{50}=0.01{\mu}M)$ is 4-fold more potent than lovastatin.

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Characterization and Purification of a Microsomal 3-Hydroxy-3-Methylglutaryl-CoA Reductase in Rice Seedling (벼 HMG-CoA 환원효소의 특성연구)

  • Kim, Jai-Hyun;Paik, Young-Ki;Kim, Jong-Bum;Kim, Jong-Guk;Hwang, Young-Soo;Ha, Sun-Hwa
    • Applied Biological Chemistry
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    • v.41 no.1
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    • pp.47-52
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    • 1998
  • 3-Hydroxy-3-methylglutaryl-CoA reductase (HMGR) catalyzes the conversion of HMG-CoA to mevalonic acid, the first intermediate of isoprenoid biosynthetic pathway in plants. The enzyme was solubilized with 0.4% Brij (polyoxyethylene ether) W-1 from a microsomal fraction of etiolated rice seedlings (Oryza sativa L.) in which its maximal activity was observed on the fourth day after germination. HMGR was purified to near homogeneity by employing $(NH_4)_2SO_4$ fractionation plus chromatographic procedures including DEAE-Sephadex A-50 and HMG-CoA-hexane-agarose affinity column. The size of the purified enzyme was estimated to be 55 kDa when judged by SDS-PAGE analysis with silver staining method. The apparent $K_m$ and $V_{max}$ values for HMG-CoA were determined to be $180\;{\mu}M$ and 107 pmol/min/mg, and those for NADPH were $810\;{\mu}M$ and 32.1 pmol/min/mg, respectively.

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Inhibitory Effects of Bile Acids on the Cholesterol Biosynthesis in Cultured Hepatocytes (배양 간세포내에서의 콜레스테롤 합성에 대한 담즙산의 저해효과)

  • Kim, Sung-Wan
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.21 no.5
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    • pp.496-501
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    • 1992
  • The present work tested the inhibitory effects of bile acids on the cholesterol biosynthesis and the activity of HMG-CoA reductase in cultured rat hepatocytes. The uptake of bile acids in hepatocytes were increased in according to the different bile acid concentrations and culture times. The rate of cholesterol synthesis in cells were inversely decreased to the bile acid concentrations and culture times. As expected, insulin injection (4 units/100g body weight) showed an enhancing effect of the cholesterol synthesis and the HMG-CoA reductase activity. The addition of bile acids in medium of insulin-treated hepatocytes also showed the suppressing effect. This effect was directly confirmed in isolated hepatic icrosomes by the test of HMG-CoA reductase activity. In the test of $Na^+$,$K^+$-ATPase activity in the isolated hepatocyte membrane, only the cholic acid did not stimulate the enzyme system. The reason of such difference is not obvious, but this result indicates that the cholic acid could be absorbed by simple diffusion.

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Effect of Perilla Oil on the Fatty Acid Composition, ACAT and HMG-CoA Reductase in Microsomes, or Cholesterol and Protein in Serum of Rabbits (들깨기름이 토끼의 혈청단백질, Cholesterol 과 간장속의 ACAT, HMG-CoA reductase 및 지방산 조성에 미치는 영향)

  • Nam, Hyun-Keun
    • Journal of the Korean Society of Food Culture
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    • v.4 no.2
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    • pp.185-189
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    • 1989
  • Effect of perilla oil on the fatty acid composition, ACAT and HMG-CoA reductase in the liver microsomes, or cholesterol and protein in serum of rabbit were examined. 1. The content of total protein in serum was almost same amount of both groups, but ${\alpha_1}-globulin$ and r-globuline were incresed or ${\beta}-globulin$ was decresed compared with control. 2. The content of high density lipoprotein incresed, and the content of low density lipoprotein decresed in lipoprotein. 3. Total cholesterol and triglyceride were decresed, and the content of phospholipid was incresed. 4. Perilla oil did not effect for changing blood glucose and $Na^+,\;K^+$ electrolytes. 5. Perilla oil did not effect for changing serum GOT and GPT in rabbit. 6. The activity of ACAT decresed and the activity of HMG-CoA reductase incresed. The activity of ACAT and HMG-CoA reductase in liver microsomes were reciprocal. 7. There were arachidonic acid 20:4, eicosapentaenoic acid 20:5, and docosahexaenoic acid 22:6 in the liver microsomes of rabbits. These highly polyunsaturated fatty acids were convented from linolenic acid 18:3 n-3.

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The Meaning of Canalization of Human Cervical Mucus as an Ovulation Marker in the Induced Ovulatory Menstrual Cycles (배란유도주기에서 배란예측지표로서 자궁경관점액의 관강화(Canalization) 현상의 의의)

  • Shim, Hyun-Nam;Suh, Byung-Hee;Lee, Jae-Hyun
    • Clinical and Experimental Reproductive Medicine
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    • v.14 no.1
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    • pp.19-28
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    • 1987
  • 35 patients of normal reproductive age group (22-37 yrs) were selected for ovulation induction using $Clomid^{(R)}$ and HMG. Correlation between canalization of cervical mucus and estradiol level in plasma. morphological ovarian follicular change by ultrasonogram, Ferning and Spinnbarkeit were studied in the induced ovulatory menstrual cycles. By retrospective analysis, the results were following; 1. Canalization appeared on the eighth day of the menstrual cycle in $Clomid^{(R)}$ group, and seventh day of HMG group. And the number of the channels increased gradually until the ovulation time. 2. The mean number of channels increased from 12${\pm}$12 in $Clomid^{(R)}$ group, 19${\pm}$14 in HMG group (Day-6) to a maximum of 46${\pm}$22 in $Clomid^{(R)}$ group (Day-1). 3. The maximum plasma estradiol(E2) level was 812${\pm}$722pg/ml in $Clomid^{(R)}$ group (Day-1), 1792${\pm}$504 pg/ml in HMG group (Day-1), and there was a good statistical correlation between the number of channels and the plasma E2 level. 4. The maximal follicular diameter was 19.4${\pm}$6.7 mm in $Clomid^{(R)}$ Group (Day-1) 19.3${\pm}$4.6mm in HMG group (Day-1) and after than decreased. There was a good statistical correlation between the number of channels and the follicular diameter. 5. When grade of ferning was I, the number of channels were 19.4${\pm}$6.7 in $Clomid^{(R)}$ group, 38${\pm}$26 in HMG group. When grade of ferning was III, the number of channels were 54${\pm}$30 in $Clomid^{(R)}$ group, 71${\pm}$36 in HMG group. 6. The maximum score of Spinnbarkeit was 2.6${\pm}$0.5 in Clomid group (Day-0), 2.6${\pm}$0.5 in HMG group (Day-2). In conclusion, the phenomenon of cervical mucus canalization showed the value of the clinical use as an ovulatin marker.

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Insertion Mutation in HMG-CoA Lyase Increases the Production Yield of MPA through Agrobacterium tumefaciens-Mediated Transformation

  • Dong, Yuguo;Zhang, Jian;Xu, Rui;Lv, Xinxin;Wang, Lihua;Sun, Aiyou;Wei, Dongzhi
    • Journal of Microbiology and Biotechnology
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    • v.26 no.11
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    • pp.1924-1932
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    • 2016
  • Mycophenolic acid (MPA) is an antibiotic produced by Penicillium brevicompactum. MPA has antifungal, antineoplastic, and immunosuppressive functions, among others. ${\beta}-Hydroxy-{\beta}-methylglutaryl-CoA$ (HMG-CoA) lyase is a key enzyme in the bypass metabolic pathway. The inhibitory activity of HMG-CoA lyase increases the MPA biosynthetic flux by reducing the generation of by-products. In this study, we cloned the P. brevicompactum HMG-CoA lyase gene using the thermal asymmetric interlaced polymerase chain reaction and gene walking technology. Agrobacterium tumefaciens-mediated transformation (ATMT) was used to insert a mutated HMG-CoA lyase gene into P. brevicompactum. Successful insertion of the HMG-CoA lyase gene was confirmed by hygromycin screening, PCR, Southern blot analysis, and enzyme content assay. The maximum MPA production by transformants was 2.94 g/l. This was 71% higher than wild-type ATCC 16024. Our results demonstrate that ATMT may be an alternative practical genetic tool for directional transformation of P. brevicompactum.

Comparison of the Effects of Ginseng Total Saponin, Ginsenoside-$Rb_1$, Ginsenoside-$Rb_2$ and Lovastatin on the Expression of mRNAs for HMG CoA reductase and LDL Receptor (인삼의 총사포닌, Ginsenoside-$Rb_1$, Ginsenoside-$Rb_2$와 Lovastatinul 의한 Hep G2 세포의 HMG CoA Reductase 및 LDL수용체 mRNA 발현 유발효과의 비교)

  • Noh, Yun-Hee;Lim, G-Rewo;Koo, Ja-Hyun
    • Journal of Ginseng Research
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    • v.20 no.3
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    • pp.241-247
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    • 1996
  • The effects of ginseng total saponin, ginsenoside-Rb, and -Rb, on the reduction of chmlesterol level and the myNA expression rates of HMG CoA reductase and LDL receptor in Hep G2 were investigated and compared with that of lovastatin, a competitive HMG CoA reductase Inhibitor. The amounts of cholesterol in Hep G2 decreased in total saponin-and ginsenoside-treated groups as compared with that of control group, while there was no significant reduction in lovastatin-treated group. The mRNA expression rates of HMG CoA reductase increased in total saponin and gin- senoside groups except for ginsenoside-Rb, (10-3%) group and decreased in lovastatin group com- pared with that of control group. The mRNA expression rates of LDL receptor generally increased In all of the test groups except for total saponin (10-5%) group compared with that of control group. Because the ginseng components tested were more effective in the reduction of cholesterol level in Hep G2 than lovastatin and induced the gene expression of LDL receptor, we suggest the possibility that they could be used as a replacement agent for lovastatin which can not be prescribed especially to patients with hepatic diseases.

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Study on Clomiphene Citrate with Single Human Menopausal Gonadotropin for Controlled Ovarian Hyperstimulation (체외수정시술시 과배란에 Clomiphene Citrate와 일회 Human Menopausal Gonadotropin 병합요법의 효용성에 관한 연구)

  • Lee, So-Young;Lee, Sang-Hoon;Bae, Do-Whan
    • Clinical and Experimental Reproductive Medicine
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    • v.22 no.2
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    • pp.123-130
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    • 1995
  • Many types of medication regimens have been used for controlled ovarian hyperstimulation for assisted reproductive technique(ART). Questions are now being raised regarding how to lower the escalating costs of assisted reproduction and decrease the extent of patient discomfort and disruption of life style without sacrificing success rates. In this investigation, from January 1994 through August 1994 patients presenting to the Chung-Ang university hospital, infertility clinic were offered the option of the clomiphene citrate (CC)/single Human Menopausal Gonadotropin(HMG) combination and conventional GnRH-agonist combination method. 60 patients (78 cycles) were given CC/single HMG combination as a study group, and 78 patients (102 cycles) were given conventional GnRH-a combined ultrashort protocol as a control group for IVF-ET program and the resulting number of oocyte retrieved, embryo produced, and pregnancy initiated were compared. There were no differences between the two groups in mean age, serum $E_2$, LH and FSH level on menstrual cycle day 2. HMG requirement was 2 ampules in study group and $24.2{\pm}6.8$ ampules in control group. On the day of HCG injection, serum LH and FSH levels were not significantly different, but serum $E_2$, was significantly higher in control group(p<0.001). There was relatively well endometrial quality in control group but not significant compare to study group. In control group, numbers of retrieved oocyte and transferred embryo were significantly more than study group(p<0.001). Fertilization rate was not significantly different in the two groups and pregnancy rates were 20.2% in study group 28.4% in control group(p<0.001). CC/single HMG protocol for IVF-ET is less expensive than GnRH-a combined ultrashort protocol and minimizes patients discomfort. In addition, CC/single HMG protocol produces acceptable pregnancy rate and represents an attractive alternative to select patients undergoing IVF-ET.

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