• 제목/요약/키워드: $H^+/K^+-ATPase$

Search Result 236, Processing Time 0.024 seconds

Stability Improvement of Esomeprazole Magnesium Dihydrate Enteric-Coated Tablet by Adding Alkalizing Agents (에스오메프라졸 마그네슘 이수화물을 함유하는 장용성 제제의 안정성 개선)

  • Cho, Young Ho;Jeon, Hyo Bin;Lee, Jong-Hwa;Lee, Gye Won
    • KSBB Journal
    • /
    • v.32 no.2
    • /
    • pp.108-116
    • /
    • 2017
  • Omeprazole, a benzimidazole derivative, suppresses gastric acid secretion by inhibiting $H^+/K^+$ ATPase in gastric parietals cells, and by reducing $H^+$ concentration. To improve stability of esomeprazole magnesium dihydrate (ESMD), enteric-coated preperation was composed of core tablet, subcoating and enteric coating layer. We were evaluated in vitro dissolution characteristics between test and reference ESMD preparation and stability. We could prepare enteric-coated formulation of ESMD by controlling disintegrating agent and coating ratio which could rapidly dissolved in neutral or alkali medium. The formulation D5 with crospovidone of 1.25% and coating ratio of 16.25% had a similar dissolution behavior compare to reference preparation. Difference factor ($f_1$) and similarity factor ($f_2$) were 0~15 and 50~100 and there was no significant difference in bioequivalence between formulations. The content and dissolution rate of formulation D5 were $96.54{\pm}0.21$ and $78.56{\pm}0.87%$ without change of color in accelerated condition ($40^{\circ}C$, RH 75%, high density polyethylene (HDPE) container) for 6 months. This study concluded that our enteric coated preparation of ESMD could be an useful method to improve stability of unstable drug without direct contact with coating material.

Characterization of the Ryanodine Receptor and SERCA in Fetal, Neonatal, and Adult Rat Hearts

  • Ramesh, Venkat;Kresch, Mitchell J.;Park, Woo-Jin;Kim, Do-Han
    • BMB Reports
    • /
    • v.34 no.6
    • /
    • pp.573-577
    • /
    • 2001
  • The mammalian heart is known to undergo significant mechanical changes during fetal and neonatal development. The objective of this study was to define the ontogeny of the ryanodine receptor/$Ca^{2+}$ release channel and SERCA that play the major roles in excitation-contraction coupling. Whole ventricular homogenates of fetal (F) (19 and 22 days in gestation), postnatal (N) (1 and 7 days postnatal), and adult (A) (5 weeks postnatal) Sprague-Dawley rat hearts were used to study [$^3H$]ryanodine binding and oxalate-supported $^{45}Ca^{2+}$ uptake. For the ryanodine receptor, the major findings were: (1) The ryanodine receptor density, as determined by maximal [$^3H$]ryanodine binding ($B_{max}$), increased 3 fold between the F22 and A periods ($0.26{\pm}0.1$ vs. $0.73{\pm}0.07$ pmoles/mg protein, p<0.01), whereas there was no significant change during the F22 and N1 development phases ($0.26{\pm}0.1$ vs. $0.34{\pm}0.01$). (2) Affinity of the ryanodine receptor to ryanodine did not significantly change, as suggested by the lack of change in the $K_d$ during the development and maturation. For SERCA, changes started early with an increased rate of $Ca^{2+}$ uptake in the fetal periods (F19: $8.1{\pm}1.1$ vs. F22: $19.3{\pm}2.2$ nmoles/g protein/min; p<0.05) and peaked by 7 days (N7) of the postnatal age ($34.9{\pm}2.1$). Thus, we conclude that the quantitative changes occur in the ryanodine receptor during myocardial development. Also, the maturation of the $Ca^{2+}$ uptake appears to start earlier than that of the $Ca^{2+}$ release.

  • PDF

Reproductive cycle and Maturation Induction of Oocytes in Rana rugosa (옴개구리의 생식주기와 난자의 성숙유도)

  • 유명식;나철호
    • The Korean Journal of Zoology
    • /
    • v.38 no.1
    • /
    • pp.96-105
    • /
    • 1995
  • 본 연구는 옴개구리(Rana rugosa)의 생식주기를 파악하고 이들 난자들의 체외 성숙조건을 구하기 위하여 수행하였다 개구리들의 gonadosomatic index(G51)는 4월에서 8월사이에는 비교적 낮았고 9월에서 이듬해 3월까지는 높았다 여포들의 성장은 주로 6월에서 9월 사이에 이루어지는데 난소내에서도 여포들의 성장 속도는 일부 다른 것으로 나타났다. 야외 관찰에서 이 개구리들은 서식지의 온도에 따라 4월에서 7월 사이에 산란을 한다는 것과 10월에서 이듬해 3월까지 동면을 한다는 것을 말았다. 산란기에 취한 여포 난자들은 생체외 배양에서 progesterone에 성숙반응(germinal vesicle breakdown(GVBD))을 일으키지 않았다. 그러나 protein klnase C(PKC)의 촉진제인 12-O-tetradecanoylphorbol 13-acetate(TPA) 혹은 Na+/K+ ATPase의 저해제인 ouabain을 progesterone과 동시에 처리했을 때에는 성숙반응을 일으켰다(각각 86%와 80%). TPA 로 핵붕괴를 일으킨 난자의 세포질을 미성숙 난자에 주입하면 미성숙 난자의 핵붕괴를 유도하였으며 성숙된 다른 종의 난자들의 세포질도 이와 같은 효과를 나타내었다. TPA의 성숙유도 효과는 5분의 노출 기간으로도 충분하였으며 PKC의 저해제인 H-7을 처리하면 그 효과가 없어졌다 이러한 결과들은 옴개구리의 난자는 호르몬에 성숙반응을 일으킨지 않으나 PKC 활성화 이후 단계는 정상이라는 것을 의미한다.

  • PDF

Screening of Natural Product Libraries for the Extension of Cell Life-span through Immune System (면역시스템을 통한 세포수명연장 천연물질 스크린)

  • Yoo, Bo-Kyung;Kwon, Kisang;Ko, Young Hwa;Kim, Hong Geun;Lee, Seokhyun;Park, Kwan-Ho;Choi, Ji-Young;Kwon, O-Yu
    • Journal of Life Science
    • /
    • v.26 no.3
    • /
    • pp.359-363
    • /
    • 2016
  • We have screened four natural products against 640 single compounds, which shows more two folds gene expression for both endoplasmic reticulum aminopeptidase 1 (ERAP1) and FOXO-family transcription factor (FOXO1). The results were as follows. (±)-Car-3-ene-2,5-dione from Asarum sieboldii Miq. is C10H12O2 molecular formula and the 164 kDa molecular weight. Cinobufagin from Bufonis Venennum is C26H34O6 molecular formula and 442 kDa molecular weight. So far reported main biological function is Na+/K+-ATPase inhibition. Corilagin from Euphorbia pekinensis is C27H22O18 molecular formula and 634 kDa molecular weight. Carbonic anhydrase inhibition is well known its biological function. Corydaline from Corydalis turtschaninovii is C22H27NO4 molecular formula and 369 kDa molecular weight. The main biological function is acetylcholinesterase inhibition. In the short future, four types of natural products will be used in longevity experiments with insects. The results may give one of the clues for studying new drug development candidates of the longevity.

Isolation and Characterization of Paramyosins of Marine Gastropods (해산복족류(海産腹足類)의 Paramyosin의 분리(分離) 및 그 특성(特性)에 관(關)한 연구(硏究))

  • Pyeun, Jae-Hyeung
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.2 no.1
    • /
    • pp.1-21
    • /
    • 1973
  • The muscle of abalone, Notohaliotis discus (REEVE), and top-shell, Turbo cornutus Solander, were examined for protein composition. Then paramyosins which are known as one of the important structural protein of the muscle fibrils were isolated from the both muscle and their physico-chemical properties such as solubility, salting-out behaviour, intrinsic viscosity, ATPase activity, etc. involving amino acid composition and N-terminal amino acid residues were investigated to elucidate phylogenie characteristics more intensively from the viewpoint of comparative biochemistry. The analysis of protein composition resulted in the following estimations: abalone muscle; water-soluble protein of 22 %, salt-soluble protein, 34%, alkali-soluble protein, 20%, and stroma protein, 24%, and top-shell muscle; water-soluble protein of 16%, salt-soluble protein, 30%, alkali-soluble protein, 29%, and stroma protein, 25%, respectively. It is demonstrated in sedimentation analysis that paramyosin and myosin-actomyosin account for approximately 65% and 35% of the salt-soluble protein of abalone, and that the composition of both sediments in top-shell was approximately 70% and 30%, respectively. The ultracentrifugally homogenous paramyosins isolated essentially according to Bailey's ethanol-dried method from both of the muscle showed a $S^{\circ}_{20,w}$ of 3. 14s for abalone and a $S^{\circ}_{20,w}$ of 3.50s for top-shell. The both paramyosins were commonly rich in arginine, aspartic acid, and glutamic acid, while scarcely contained proline and tryptophan, in rough accord with the other paramyosins thus far reported. It is clear that these gastropod paramyosins showed of having the characteristic N-terminal amino acid residues such as N-aspartic acid, N-valine, N-serine, and N-threonine in common. The abalone paramyosin completely salted in with KCl beyond $0.35{\mu}$ and the top-shell paramyosin beyond $0.30{\mu}$. The abalone paramyosin was salted-out between 18% and 30% saturation of ammonium sulphate and the top-shell paramyosin between 22% and 29% saturation. The intrinsic viscosities at abalone and top-shell paramyosins at $25^{\circ}C$ were estimated respectively to be 3.1 dl/g and 2.6 dl/g showing somewhat higher than the values for some other paramyosins from lamellibranchs. In regard with the ATPase activity, the para myosin specimens did not exhibit any significant activity over through the pH conditions of 5 to 9.5. irrespective of the presence of $Ca^{++}$ or $Mg^{++}$. So was the case with the abalone paramyosin prepared by a slightly modified Bailey's wet-extraction method.

  • PDF

Crystal structure of CodW in Bacillus Subtilis - the first N-terminal serine pretense

  • Park, Seong-Hwan;Park, Hyun-Ho;Lim, Young-Jun;Kang, Min-Suk;Lim, Byung-Kook;Seong, Ihn-Sik;Jimin Wang;Chung, Chin-Ha;Eom, Soo-Hyun
    • Proceedings of the Korea Crystallographic Association Conference
    • /
    • 2002.11a
    • /
    • pp.25-25
    • /
    • 2002
  • CodWX, encoded by the cod operon in Bacillus subtilis, is a member of the ATP-dependent protease complex family, and is homologous to the eukaryotic 26S proteasome. It consists of two multimeric complexes: two hexameric ATPase caps of CodX and a protease chamber consisting of CodW dodecamer. Prior structural studies have shown that the N-terminal threonine residue is solely functional as a proteolytic nucleophile in ATP-dependent proteases such as HslV and certain β-type subunits of 20S proteasome, which have a primary sequence similarity of -50% and -20% with CodW respectively. Here we present a 3.0 Å resolution crystal structure of CodW, which is the first N-terminal serine protease among the known proteolytic enzymes. In spite of the same fold and the conserved contacts between subunits with HslV in E. coli and H. influenza, this structure shows the five additional residues extending from conserved Thr1 among the other ATP-dependent pretense and extraordinary basic proteolytic chamber.

  • PDF

Cloned Placenta of Korean Native Calves Died Suddenly at Two Months after Birth Displays Differential Protein Expression

  • Kim Hong Rye;Kang Jae Ku;Lee Hye Ran;Yoon Jong Taek;Seong Hwan Hoo;Jung Jin Kwan;Park Chang Sik;Jin Dong Il
    • Reproductive and Developmental Biology
    • /
    • v.29 no.2
    • /
    • pp.63-68
    • /
    • 2005
  • Cloned calves derived from somatic cell nuclear transfer (SCNT) have been frequently lost by sudden death at 1 to 3 month following healthy birth. To address whether placental anomalies are responsible for the sudden death of cloned calves, we compared protein patterns of 2 placentae derived from SCNT of Korean Native calves died suddenly at two months after birth and those of 2 normal placentae obtained from AI fetuses. Placental proteins were separated using 2-Dimensional gel electrophoresis. Approximately 800 spots were detected in placental 2-D gel stained with coomassie-blue. Then, image analysis of Malanie III (Swiss Institute for Bioinformatics) was performed to detect variations in protein spots between normal and SCNT placentae. In the comparison of normal and SCNT samples, 8 spots were identified to be up-regulated proteins and 24 spots to be down-regulated proteins in SCNT placentae, among which proteins were high mobility group protein HMG1, apolipoprotein A-1 precursor, bactenecin 1, tropomyosin beta chain, $H^+-transporting$ ATPase, carbonic anhydrase II, peroxiredoxin 2, tyrosine-rich acidic matrix protein, serum albumin precursor and cathepsin D. These results suggested that the sudden death of cloned calves might be related to abnormal protein expression in placenta.

Structure and action mechanism of humic substances for plant stimulations

  • Jeon, Jong-Rok;Yoon, Ho Young;Shin, Gyeong-Im;Jeong, Song Yi;Cha, Joon-Yung;Kim, Woe-Yeon
    • Journal of The Korean Society of Grassland and Forage Science
    • /
    • v.38 no.3
    • /
    • pp.175-179
    • /
    • 2018
  • Humic substances that can be obtained from coal resources such as leonardite in a bulk scale have been employed as crop stimulators and soil conditioners. The polymeric organics containing a variety of aromatic and aliphatic structures are known to activate plants in a multifunctional way, thus resulting in enhanced germination rate and abiotic stress resistance concomitant with induction of numerous genes and proteins. Although detailed structural-functional relationship of humic substances for plant stimulations has not been deciphered yet, cutting-edge analytical tools have unraveled critical features of humic architectures that could be linked to the action mechanisms of their plant stimulations. In this review article, we introduce key findings of humic structures and related biological functions that boost plant growth and abiotic stress resistance. Oxygen-based functional groups and plant hormone-like structures combined with labile and recalcitrant carbon backbones are believed to be critical moieties to induce plant stimulations. Some proteins such as HIGH-AFFINITY $K^+$ TRANSPORTER 1, phospholipase A2 and $H^+$-ATPase have been also recognized as key players that could be critically involved in humic substance-driven changes in plant physiology.

Antihypertensive effect of Ganjang (traditional Korean soy sauce) on Sprague-Dawley Rats

  • Mun, Eun-Gyung;Sohn, Hee-Sook;Kim, Mi-Sun;Cha, Youn-Soo
    • Nutrition Research and Practice
    • /
    • v.11 no.5
    • /
    • pp.388-395
    • /
    • 2017
  • BACKGROUND/OBJECTIVES: Although Korean fermented foods contain large amounts of salt, which is known to exacerbate health problems, these foods still have beneficial effects such as anti-hypertension, anti-cancer, and anti-colitis properties. We hypothesized that ganjang may have different effects on blood pressure compared to same concentrations of salt. MATERIALS/METHODS: Sprague-Dawley rats were divided into control (CT), NaCl (NC), and ganjang (GJ) groups and orally administered with 8% NaCl concentration for 9 weeks. The systolic blood pressure (SBP), serum chemistry, $Na^+$ and $K^+$ concentrations and renal gene expressions were measured. RESULTS: The SBP was significantly increased in the NC group compared to the GJ and CT groups. In addition, the $Na^+$ concentration in urine was higher in the GJ and NC groups than the CT group, but the urine volume was increased in the GJ group compared to the other groups. The serum renin levels were decreased in the GJ group compared to the CT group, while the serum aldosterone level was decreased in the GJ group relative to the NC group. The mRNA expression of the renin, angiotensin II type I receptor, and mineralocorticoid receptor were significantly lower in the GJ group compared to other groups. Furthermore, GJ group showed the lowest levels of genes for $Na^+$ transporter in kidney cortex such as $Na^+/K^+$ $ATPase{\alpha}1$ ($NKA{\alpha}1$), $Na^+/H^+$ exchanger 3 (NHE3), $Na^+/HCO_3{^-}$ co-exchanger (NBC), and carbonic anhydrases II (CAII). CONCLUSIONS: The decreased SBP in the GJ could be due to decreased renin and aldosterone levels in serum and increased urinary volume and excretion of $Na^+$ with its transporter gene alteration. Therefore, ganjang may have antihypertensive effect despite its high contents of salt.

The Effect of Juglandis Semen Extract Solution on Oxidant-Induced Alteration of Glutamate Uptake in Rabbit Brain Synaptosome (호도약침액(胡桃藥鍼液)이 가토(家兎) 뇌(腦)의 Synaptosome에서 Oxidant에 의한 물질이동계(物質移動系)의 장애(障碍)에 미치는 영향(影響))

  • Kim Tae-Kook;Youn Hyoun-Min;Jang Kyung-Jeon;Song Choon-Ho;Ahn Chang-Beohm
    • Korean Journal of Acupuncture
    • /
    • v.17 no.1
    • /
    • pp.179-190
    • /
    • 2000
  • This study was undertaken to determine whether Juglandis semen extract solution (JLS solution) exerts protective effect against oxidant-induced inhibition of glutamate uptake by synaptosomes. Synaptosome was prepared from rabbit brain cortex. Glutamate uptake increased by incubation time during 10 minutes, which was significantly inhibited by 1mM t-buthylhydroperoxide(t-BHP). JLS solution prevented t-BHP-induced inhibition of glutamate uptake in a dose-dependent manner. t-BHP reduced glutamate uptake in dose-dependent fashion, which was significantly prevented by 2% JLS solution. t-BHP(1mM) and $ascorbate/Fe^{2+}(50/1{\mu}M)$ increased lipid peroxidation in synaptosomes by 5-fold, and it was significantly prevented by 2% JLS solution. $HgCl_2(0.1mM)$ inhibited glutamate uptake and increased lipid peroxidation. These changes were prevented by 2% JLS solution. Synaptosomal Na-K-ATPase activity was inhibited by t-BHP(1mM) and $H_2O_2(50mM)$, which was prevented by 2% JLS solution. The results indicate that JLS solution prevents oxidant-induced inhibition of glutamate by synaptosomes, and this may result from inhibition of lipid peroxidation induced by oxidants.

  • PDF