• Title/Summary/Keyword: Cholesterol synthesis

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Synthesis and Optimization of Cholesterol-Based Diquaternary Ammonium Gemini Surfactant (Chol-GS) as a New Gene Delivery Vector

  • Kim, Bieong-Kil;Doh, Kyung-Oh;Bae, Yun-Ui;Seu, Young-Bae
    • Journal of Microbiology and Biotechnology
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    • v.21 no.1
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    • pp.93-99
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    • 2011
  • Amongst a number of potential nonviral vectors, cationic liposomes have been actively researched, with both gemini surfactants and bola amphiphiles reported as being in possession of good structures in terms of cell viability and in vitro transfection. In this study, a cholesterol-based diquaternary ammonium gemini surfactant (Chol-GS) was synthesized and assessed as a novel nonviral gene vector. Chol-GS was synthesized from cholesterol by way of four reaction steps. The optimal efficiency was found to be at a weight ratio of 1:4 of lipid:DOPE (1,2-dioleoyl-L-${\alpha}$- glycero-3-phosphatidylethanolamine), and at a ratio of between 10:1~15:1 of liposome:DNA. The transfection efficiency was compared with commercial liposomes and with Lipofectamine, 1,2-dimyristyloxypropyl-3-dimethylhydroxyethylammonium bromide (DMRIE-C), and N-[1-(2,3-dioleoyloxy)propyl]-N,N,N-trimethylammonium chloride (DOTAP). The results indicate that the efficiency of Chol-GS is greater than that of all the tested commercial liposomes in COS7 and Huh7 cells, and higher than DOTAP and Lipofectamine in A549 cells. Confirmation of these findings was observed through the use of green fluorescent protein expression. Chol-GS exhibited a moderate level of cytotoxicity, at optimum concentrations for efficient transfection, indicating cell viability. Hence, the newly synthesized Chol-GS liposome has the potential of being an excellent nonviral vector for gene delivery.

Effect of Green Tea Extract on Lipid Synthesis in Human Sebocyte Cell Line (녹차추출물이 인체 피지선세포주에서 지질 생성에 미치는 효과)

  • Park, Si-Jun;Jeon, Byoung-Kook;Kim, Dae-Sung;Lee, Ghang-Tai;Mun, Yeun-Ja;Lee, Kun-Kuk;Woo, Won-Hong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.4
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    • pp.608-613
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    • 2011
  • The aqueous Green tea comes to be used with the Oriental medicine plant, it has the numerous health benefits, including antioxidant, anti-inflammatory, and anti- carcinogenic properties. Epidermal progenitor cells give rise to multiple skin lineages: hair follicle, sebaceous gland and the overlying interfollicular epidermis. Sebocytes are the cells of the sebaceous gland, which synthesize and accumulate lipid dropolets. In order to determine the effect of Green tea on lipid production, several experiments were performed in SZ95 cells (sebocytes). We found that Green tea increased lipid droplets compared with control in a dose-dependent manner. Human sebaceous glands produce sebum, a lipid mixture of squalene, wax esters, triglycerides, cholesterol esters, and free fatty acids that is secreted onto the skin. Therefore, to investigate the effects of Green tea on intracellular lipid levels, we treated SZ95 cells with Green tea, and then examined cholesterol and triglyceride levels. After treatment of the cells with Green tea, the cholesterol and triglyceride levels of SZ95 cells were increased significantly in a dose-dependent manner.

The comparative study on the anti-obesity effect of Arctium lappa L. roots with and without microwave processing (마이크로파 처리 유무에 따른 우엉뿌리의 항비만 효과 비교 연구)

  • Seo, Seong-Wook;Kim, Min Ju;Kim, Kyoung;Chung, Dong-Min;Shin, Mi-Rae
    • The Korea Journal of Herbology
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    • v.37 no.4
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    • pp.17-29
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    • 2022
  • Objective : The present study comparatively analyzed the anti-obesity effect of Arctium lappa L. roots with and without microwave processing. Methods : Four HFD groups except for the Normal group (n=8) were allocated: Control, microwave-processed dried Arctium lappa L. roots (MAL) extract 400 mg/kg/d (MAL400), MAL extract 800 mg/kg/d (MAL800), and the dried Arctium lappa L. roots (DAL) extract 800 mg/kg/d (DAL800). The efficacy of MAL and DAL was confirmed in terms of the serum biochemical index, protein expressions related to the synthesis of triglyceride (TG) and total cholesterol (TC) and 𝛽-oxidation, and histopathological staining. Results : Both MAL and DAL treatments significantly reduced final body weight and body weight gain. MAL800 treatment significantly reduced serum TG, TC, low-density lipoprotein cholesterol, and leptin levels, but the serum high-density lipoprotein cholesterol and adiponectin concentrations were dramatically increased. In particular, leptin in the MAL800 group was reduced by 14.1% compared with the DAL800 group. Moreover, the MAL800 treatment showed an effect superior to the DAL800 treatment in the reduction of serum TC, the sirtuin 1 (Sirt1) activation, and the inhibition of 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMGCR) gene expression. In particular, unlike the DAL800 treatment, MAL treatment significantly led to the activation of peroxisome proliferator-activated receptor alpha (PPAR𝛼). Subsequently, PPAR𝛼 meaningfully regulated downstream proteins associated with 𝛽-oxidation. Conclusion : These findings suggest that Arctium lappa L. roots with microwave processing effectively ameliorate obesity through the regulation of leptin and TC and the promotion of 𝛽-oxidation compared with Arctium lappa L. roots without microwave processing.

Identification of Steroidogenic Acute Regulatory Protein mRNA in the Rat Ovary and Adrenal G land (흰쥐 난소 및 부신에서 Steroidogenic Acute Regulatory Protein mRNA의 발현에 관한 연구)

  • 김명옥
    • Development and Reproduction
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    • v.2 no.1
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    • pp.39-43
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    • 1998
  • The synthesis of steroid hormone starts from cholesterol. Steroidogenic acute regulatory protein(StAR) transfers cholesterol acutely from the outer mitochondrial membranes to the inner in the early step of steroidogenesis. Many kinds of steroid hormones are mainly synthesized in adrenal grand, ovary and testis. The purpose of this study is to determine the distribution of StAR mRNA in the rat ovary and adrenal gland and to confirm the functions of StAR in these organs. In the ovary, StAR mRNAs were strongly expressed in the corpus luteum, where progesterone is synthesized, and these were weakly expressed in the theca layer of follicles, where androgen is synthesized. However, StAR mRNAs were not detected in the estrogen producing granulosa cells of growing follicles. In the corpus luteum, StAR mRNAs were strongly loclized in the zona fasciculata and zona reticularis, where glucocorticoid is mainly synthesized. StAR mRNAs were weakly expressed in the zona gromerulosa, where mineralcorticoid is synthesized. StAR mRNAs were not detected in the adrenal medulla. In our results, StAR mRNAs were expressed differentially in the steroidogenic cells of ovary and adrenal gland according to the types of steroid hormones, and the statges of corpus luteum development. We conclude that StAR is involved in the steroidogenesis at the very early step of steroid synthesis cascade.

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Expression of steroidogenic acute regulatory protein mRNA in immature and adult rat testes (미성숙과 성숙한 흰쥐 고환에서의 Steroidogenic acute regulatory protein mRNA의 발현)

  • Koh, Phil-ok;Kwak, Soo-dong
    • Korean Journal of Veterinary Research
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    • v.40 no.2
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    • pp.229-236
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    • 2000
  • The synthesis of steroid hormone starts from cholesterol. Steroidogenic acute regulatory protein (StAR) acutely transfers cholesterol from the outer mitochondrial membrane to the inner in the early step of steroidogenesis. Many kinds of steroid hormone are mainly synthesized in adrenal grand, ovary, and testis. Among the steroid hormone, testosterone is synthesized in Leydig cells of the testis, the production of testosterone significantly increases in adult testis after puberty onset. Therefore, we think that the expression of StAR mRNA in testis will change according to the testicular development. The aim of this study is to determine the distribution of StAR mRNA in immature and adult rat testes and to confirm the functions of StAR in these testes. Thus, in situ hybridization was used in rat testes of the 2, 4, and 10 weeks of age. StAR mRNA was expressed in Leydig cells. Positive signals of StAR mRNA were weakly detected in Leydig cells of the 2 weeks of age. But, StAR mRNA was strongly expressed in Leydig cells of the 4 and 10 weeks of age, where steroidogenesis actively occur. In our results, the pattern of StAR mRNA expression was similar to the pattern of testosterone production in immature and adult rat testes. In conclusion, we can suggest that StAR acts as an important factor to regulate the synthesis of testosterone in Leydig cells of the rat testis.

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Oral Drugs for Treatment of Dyslipidemia and Cardiovascular Disease Prevention (이상지질혈증 경구용 약제와 심혈관질환 예방효과)

  • Lee, Yun-Ah;Rho, JunSeung;Song, Sang-Wook;Jung, Su-Young;Kwon, Ji Young;Kang, Sung-Goo
    • Archives of Obesity and Metabolism
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    • v.1 no.1
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    • pp.14-25
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    • 2022
  • In 1971, Dr. Akira Endo succeeded in isolating a cholesterol synthesis inhibitor, compactin. Later, compactin was renamed mevastatin, meaning that it stops the synthesis of mevalonate, which is considered the first statin. However, mevastatin is not commercially released, whereas lovastatin, developed by Alfred Albert of Merk in 1979, was the first commercially developed statin. After the 4S study, the first largescale clinical trial with statins conducted in Scandinavia showed a dramatic secondary preventive effect against cardiovascular disease, and the effectiveness of statins in patients with dyslipidemia was repeatedly demonstrated. Subsequently, many oral drugs that affect blood lipid concentration; statins and ezetimibe aimed at reducing low-density lipoprotein (LDL)) cholesterol; fibrates and omega 3 formulations aimed at reducing triglycerides were widely developed and used in Korea. In this article, we review the results of clinical studies on representative cardiovascular diseases for four types of oral drugs for dyslipidemia, which are currently the most commonly used in Korea.

Effects of Eicosapentaenoic Acid during In Vitro Maturation of Porcine Oocytes: Hormone Synthesis and Embryonic Developmental Potential (에이코사펜타인산이 돼지난포란의 체외 성숙에 미치는 영향)

  • Kim, Kang-Sig;Park, Hum-Dai
    • Journal of Animal Reproduction and Biotechnology
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    • v.34 no.3
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    • pp.222-231
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    • 2019
  • Among fatty acid families, the polyunsaturated fatty acids were demonstrated to be mediators in various reproductive processes as precursor of steroid hormone (via cholesterol) and prostaglandins (via arachidonic acid), and in the last decade, major research was focused on the effects of omega-6 and especially omega-3 fatty acid. Eicosapentaenoic acid, the longest members of omega-3 fatty acid family, can be produced by a series of desaturation and elongation reactions from shorter member such as α-Linolenic acid. However, very few studies have provided detailed descriptions of Eicosapentaenoic acid effects and mechanisms of action in mammalian oocytes. The purpose of this study was to evaluate the effect of Eicosapentaenoic acid supplementation on in vitro maturation and developmental potential of porcine oocytes. Various concentrations of Eicosapentaenoic acid was added into in vitro maturation medium, and we evaluated the degree of cumulus expansion, nuclear maturation rate, blastocysts quality, and levels of prostaglandin E2, 17β-estradiol, progesterone in the spent medium. High doses (100 μM) of Eicosapentaenoic acid supplementation significantly inhibited cumulus expansion and oocyte nuclear maturation, and prostaglandin E2 synthesis also significantly decreased compared with other groups (p < 0.05). Supplementation of 50 μM Eicosapentaenoic acid showed higher quality blastocysts in terms of high cell numbers and low apoptosis when compared with other groups (p < 0.05), and synthesis ratio of E2/P4 also significantly increased compared with control group (p < 0.05). However, Supplementation of 100 μM Eicosapentaenoic acid showed high apoptosis when compared with other groups (p < 0.05), and synthesis ratio of 17β-estradiol/progesterone also significantly decreased compared with control group (p < 0.05). Our results indicated that supplementation with appropriate levels of Eicosapentaenoic acid beneficially affects the change of hormone synthesis for controlling oocyte maturation, leading to improved embryo quality. However, high doses of Eicosapentaenoic acid treatment results in detrimental effects.

Effects of Ethylacetate Fraction of Plantago asiatica L. on Hypercholesterolemia Induced by High Cholesterol Diet in Rats (질경이(Plantago asiatica L.) 에틸아세테이트분획이 흰쥐의 고콜레스테롤혈증에 미치는 효과)

  • Lee Jae-Joon;Lee Jeong-Hwa;Jeong Chang-Ju;Choi Hyun-Sook;Lee Myung-Yul
    • Food Science and Preservation
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    • v.12 no.6
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    • pp.624-630
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    • 2005
  • Plantain was extracted with ethanol and fractionated systemically with n-hexane, chloroform, ethylacetate, n-butanol and water to study inhibitory effect on cholesterol synthesis in vitro. To screen the effect, inhibitory activities on 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase obtained from Saccharomyces cerevisiae were examined using the five fractions of Plantain. The HMG-CoA reductase activity was inhibited most by ehylacetate fraction among the fractions, although the all five fractions had the effect To see the hypocholesterolemic effect of the ethylacetate fraction of Plantanin (PAE) in vivo, male Sprague-Dawley rats were received 5 types of diets for 6 weeks: normal diet group (NOR), high cholesterol diet group($1\%$ cholesterol and $0.25\%$ sodium cholate, CON), normal diet and PAE 70 mg/kg administered group(S1), high cholesterol diet and PAE 140 mg/kg administrated group(S2), and high cholesterol diet and PAE 140 mg/kg administered group(S3). Body weight gains of the CON were significantly increased compared to those of S1, S2 and S3. Activities of serum AST and ALT were tended to be increased in CON compared with NOR and reduced by the PAE administration. Concentrations of serum total cholesterol, free cholesterol, LDL-cholesterol, triglyceride and the atherogenic index were tended to be decreased in the PAE administered groups compared with the CON. HDL-cholesterol and phospholipid concentrations were significantly decreased in the CON and markedly increased by the PAE administered groups. Taten together, it is suggested that the ethylacetate fraction of Plantanin exerts antiatherosclerotic effect by reducing serum cholesterol concentrations in rats fed high cholesterol diets.

The Effects of Ka-Mi-Chung-Gan-Tang on Rat with Alcoholic Fatty Liver (가미청간탕(加味淸肝場)이 Rat의 알콜성 지방간에 미치는 영향)

  • Zheng, Cheng-Xuan;Yim, Dong-Sool;Lee, Sook-Yeon
    • Korean Journal of Pharmacognosy
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    • v.35 no.3 s.138
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    • pp.229-232
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    • 2004
  • Chronical intake of alcohol can cause alcoholic fatty liver. Fatty liver is caused by fat infiltration: the state of high rate of fat in liver cells and by losing the balance between the synthesis and the secretion of fatty acid. It could be developed into liver necrosis and cirrhosis. Ka-Mi-Chung-Gan-Tang (KMCGT) is a decoction used for fatty liver as oriental medicines in China. The prescription is composed of Ginseng Radix, Bupleuri Radix, Scutellariae Radix, Pinelliae Tuber, Artemisiae capillaris Herba, Gardeniae Fructus, Zingiberis Rhizoma, Zizyphi Fructus and Glycyrrhizae Radix etc. We have induced alcoholic fatty liver by ethanol administration (6 g/kg, single dose/day, for a week) on rats and observed changes of triglyceride, cholesterol and lipid peroxidation in liver tissues of them. Also we checked the activities of GOT and GPT in blood of rats. KMCGT inhibited significantly the increase of triglyceride, cholesterol, lipid peroxidation level and effectively the increase of malondialdehyde (MDA).

Synthesis and Primary Screening for Growth Inhibitors of L1210 Cells of Cholesteryl p-[3-(2-chloroethyl)-3-nitrosoureido] Phenylthioacetate

  • Kim, Jack-C.;Kim, Min-Sook;Lee, Hyeon-Kyuy
    • Archives of Pharmacal Research
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    • v.6 no.2
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    • pp.115-121
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    • 1983
  • Cholesteryl p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioaccetate (2) was synthesized : an intermediate, p-[3(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid (1) is a congener of an antitumor chlorambucil which both the -CH$_{2}$CH$_{2}$-linkage and -N(CH$_{2}$CH$_{2}$Cl)$_{2}$ group of chlorambucil molecule is doubly modified into the respective -S-linkage and -NH-CO-NNO-CH$_{2}$CH$_{2}$CL group. The attackment of cholesterol moiety as a carrier group to p-[3-(2-chloroethyl-3nitrosoureido] phenylthioacetic acid was accomplished through the esterification of cholesterol with p-[3-(2-chloroethyl-3-nitrosoureido] phenylthioacetyl chloride which was obtained from the treatment of p-[3-(2-chloroethyl)-3-nitrosourei-do] phenylthioaceticacid with SOCL$_{2}$, p-[3-(2-chloroethyl)ureido]]-phenythioacetic acid was nitrosated with NaNO$_{2}$ IN 98-100% HCOOH to give exclusively p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid. Antitumor evaluation of compounds, 1 and 2 on L 1210 leukemia did show significant activity (ED$_{40}$ : 1.14.mu./ml and 8.4.mu.g/ml, repectively). Further studies were subjected..

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