• Title/Summary/Keyword: 6R-1

Search Result 14,688, Processing Time 0.052 seconds

ER stress and unfolded protein response (UPR) signaling modulate GLP-1 receptor signaling in the pancreatic islets

  • Yurong Gao;Hanguk Ryu;Hyejin Lee;Young-Joon Kim;Ji-Hye Lee;Jaemin Lee
    • Molecules and Cells
    • /
    • v.47 no.1
    • /
    • pp.100004.1-100004.11
    • /
    • 2024
  • Insulin is essential for maintaining normoglycemia and is predominantly secreted in response to glucose stimulation by β-cells. Incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide, also stimulate insulin secretion. However, as obesity and type 2 diabetes worsen, glucose-dependent insulinotropic polypeptide loses its insulinotropic efficacy, whereas GLP-1 receptor (GLP-1R) agonists continue to be effective owing to its signaling switch from Gs to Gq. Herein, we demonstrated that endoplasmic reticulum (ER) stress induced a transition from Gs to Gq in GLP-1R signaling in mouse islets. Intriguingly, chemical chaperones known to alleviate ER stress, such as 4-PBA and TUDCA, enforced GLP-1R's Gq utilization rather than reversing GLP-1R's signaling switch induced by ER stress or obese and diabetic conditions. In addition, the activation of X-box binding protein 1 (XBP1) or activating transcription factor 6 (ATF6), 2 key ER stress-associated signaling (unfolded protein response) factors, promoted Gs utilization in GLP-1R signaling, whereas Gq employment by ER stress was unaffected by XBP1 or ATF6 activation. Our study revealed that ER stress and its associated signaling events alter GLP-1R's signaling, which can be used in type 2 diabetes treatment.

R&D Intensity and Regulation Fair Disclosure

  • Park, Jin-Ha;Shim, Hoshik
    • The Journal of Asian Finance, Economics and Business
    • /
    • v.6 no.1
    • /
    • pp.281-288
    • /
    • 2019
  • This study examines the relationship between R&D intensity and disclosure. R&D activities are essential in bringing innovation to companies. However, R&D activities are naturally uncertain and increase information asymmetry. Thus, firms with high R&D activities are more likely to have the incentive to communicate the potential of R&D investment to the market through voluntary disclosure and, concurrently, resolve information asymmetry. Meanwhile, incentives to less voluntary disclosure exist because of the proprietary cost and the risk of competitiveness loss. Furthermore, the uncertainties inherent in R&D activities caused the possible decrease in the information accuracy. For the two opposing views, this study investigates the relationship between R&D intensity and disclosure frequency using the Regulation Fair Disclosure data in Korea. Moreover, the relationship between R&D intensity and usefulness of the information disclosed is also examined. Using firm sample listed in the 2011-2016 Korea Stock Market, results show that firms with high R&D intensity make disclosures more frequent. Subsequently, the analysis using forecast sample shows that management forecast error is higher in firms with high R&D intensity. This research contributes to the existing literature by presenting evidence that R&D intensity is a significant factor affecting manager's disclosure behavior and information usefulness.

Changes in chemical characteristics of cellulase-treated wheat germ extract (효소 처리 밀 배아 추출물의 화학적 특성 변화)

  • Lee, Jae-Kang;Jang, Davin;Kang, Dongwoo;Lee, Jeonghoon;Kum, Hyeim;Choi, Yonghyoun;Kang, Hee;Choi, Yong-Seok;Kim, Dae-Ok
    • Korean Journal of Food Science and Technology
    • /
    • v.51 no.2
    • /
    • pp.97-102
    • /
    • 2019
  • Wheat germ, which is rich in nutrients and phytochemicals, is a by-product during the milling process of wheat kernel. In this study, we aimed to increase the amount of bioactive 2,6-dimethoxy-1,4-benzoquinone (2,6-DMBQ) in wheat germ using the cell-wall-degrading enzyme cellulase (Celluclast 1.5L). The amounts of organic acids, free sugars, and 2,6-DMBQ in wheat germ treated with Celluclast 1.5L were evaluated at various reaction times and temperatures. The results of reversed-phase high-performance liquid chromatography of Celluclast 1.5L-treated wheat germ revealed 2,6-DMBQ, four organic acids (tartaric, acetic, lactic, and succinic acids), and three free sugars (sucrose, fructose, and glucose). As reaction time and temperature of the mixture of wheat germ and Celluclast 1.5L increased, the contents of four organic acids, glucose, fructose, and 2,6-DMBQ increased, but that of sucrose decreased. Taken together, these results suggest that Celluclast 1.5L-treated wheat germ containing increased amounts of 2,6-DMBQ serves as a source of functional ingredients in food industry.

Estimation on the Coefficient of Repair & Maintenance Costs for Power Tiller (경운기의 수리비계수(修理費係數) 산정(算定)에 관한 연구(硏究))

  • Kang, C.H.;Park, N.J.;Jung, D.H.
    • Journal of Biosystems Engineering
    • /
    • v.15 no.2
    • /
    • pp.143-150
    • /
    • 1990
  • This study was conducted to estimate the ratio of Repair & Maintenance (R&M) costs to purchasing price that is one of the important factors for calculating the management costs of farm machinery. For this purpose, hour of use and R & M costs of power tiller and its attachments utilized results that were investigated with 400 sample units, 50 units by years of use from 1 to 8 years in 1988. The results obtained are summarized as follows; 1. The ratio of R & M costs per hours and annual R & M costs, accumulated R & M costs when sercice life of power tiller is 7 years were 0.017%, 5.50% and 38.52%, respectively. And in case of rotary, these ratio when its service life is 6 years were 0.072%, 7.16% and 43.0%, respectively. 2. The relationship between accumulated hours of use(t) and accumulated R & M costs(Y) of power tiller and its attachments were $Y=19.3t^{1.3}$ in power tiller, $Y=0.03t^{2.09}$ in plow, $Y=48.84t^{1.25}$ in rotary and $Y=7.45t^{1.15}$ in trailer. 3. The ratio of accumulated R & M costs to purchasing price when service life of power tiller is 7 years was 38.5%, and in case of rotary, this ratio when its service life is 6 years was 43.0%.

  • PDF

Overproduction of Bacterial Trypsin in Streptomyces - Optimization for Streptomyces griseus Trypsin Production by Recombinant Streptomyces (미생물을 이용한 트립신 과대 생산 연구 - Streptomyces용 숙주-벡터계를 이용한 트립신 유전자의 대량발현 최적화 -)

  • Kim, Jong-Hee;Hong, Soon-Kwang
    • Microbiology and Biotechnology Letters
    • /
    • v.36 no.1
    • /
    • pp.28-33
    • /
    • 2008
  • The expression vector (pWHM3-TR1R2) for sprT gene encoding Streptomyces griseus trypsin (SGT) followed by two regulatory genes, sgtR1 and sgtR2, was introduced into Streptomyces lividans TK24 and Streptomyces griseus IFO 13350. Various media with different compositions were used to maximize the productivity of SGT in the recombinant trains. he SGT productivity was best when the transformant of S. lividans TK24 was cultivated in R2YE medium (0.74 unit/mL) at 5 days of cultivation. C5/L (0.66 unit/mL) medium also gave a good productivity, but Livid (0.08 unit/mL) and NDSK (0.06 unit/mL) yielded poor productivities. S. griseus IFO 13350/pWHM3-TR1R2 produced SGT by 1.518 unit/mL (C5/L), 1.284unit/mL (R2YE),0.932 unit/mL (NDSK), and 0.295 unit/mL (Livid) at 7 days of cultivation, which was much higher than those from S. lividans TK24/TR1R2. The SGT protein was purified from the culture broth of S. griseus IFO 13350/pWHM3-TR1R2 in C5/L to homogeneity via ammonium sulfate fractionation, and CM-sepharose and SP-sepharose column chromatographies. The specific activity of purified SGT was 69,252 unit/mg, and the final purification fold and recovery yield were 6.5 and 1.4%, respectively.

Anti-Inflammatory Effects of the Mixture of Sorbus commixta, Urtica dioica, Phyllostachys nigra, and Rhus semialata Gall Extracts on LPS-induced Inflammation in HaCaT Cells (각질형성세포에서 LPS로 유도된 염증반응에 대한 마가목, 쐐기풀, 죽여 및 오배자 혼합추출물의 항염 효과)

  • Lee, Kyung-Eun;Nam, Jin-Ju;Kim, Seon-Mi;Kim, Han-Kon;Moon, Seong-Joon;Youm, Jong-Kyung
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.40 no.1
    • /
    • pp.45-54
    • /
    • 2014
  • Lipopolysaccharide (LPS)-induced inflammatory responses in the HaCaT keratinocyte cell line produce proinflammatory cytokines, such as interleukin-1${\alpha}$(IL-1${\alpha}$), tumor neurosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-6 (IL-6), and interleukin- 8 (IL-8) and also increase the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandins E2 (PGE2). In this study, we developed new natural ingredients for cosmetics that inhibit the pro-inflammatory responses induced by LPS in HaCaT cells. The mixture of Sorbus commixta (SC), Urtica dioica (UD), Phyllostachys nigra (PN), and Rhus semialata gall (RS) extracts blocked the increase of TNF-${\alpha}$ IL-1${\alpha}$ IL-6, and IL-8. The increase of COX-2, iNOS, and PGE2 were also blocked by it. Finally, the mixture inhibited skin irritation induced by sodium lauryl sulfate (SLS), when applied on skin through IQ chamber$^{(R)}$. In conclusion, these results show that the mixture of SC, UD, PN, and RS can be used as a primary ingredient to alleviate skin irritation when cosmeceutical products are developed for sensitive skin.

Analgesic Constituent from the Herba of Saururus chinensis ($L_{OUR.})B_{AILL.}$ (삼백초의 진통성분)

  • Park, Si-Kyung;Oh, Gab-Jin;Kim, Hyun-Tae;Kim, Hyun-Jong;Chung, Sun-Gan;Cho, Eui-Hwan
    • YAKHAK HOEJI
    • /
    • v.42 no.3
    • /
    • pp.238-242
    • /
    • 1998
  • For the investigation of bioactive natural products with analgesic activity, we have evaluated various extracts of Saururi Herba (Saururaceae), which has been used in traditiona l medicine for edema, beriberi, jaundice, turbid urine, carbuncle and furuncle. The diethylether extract of this plant was found to show a significant analgesic effect on writhing syndrome in mice. Using bioactivity-guided separation of the diethylether extract, analgesic constituent, (8S, 8`R, 7R, 6`R)-2'-oxo-4,5: 4',5'-bis(methylenedioxy)-${\Delta}^{1,3,5,3'}$-8.8', 7.6', 2.O.5'-neolignan(sauchinone) was isolated and structurally identified by physico-chemical properties and spectroscopic evidences. This compound has good analgesic activity with lower toxicity, as compared to other antipyretic-analgesic drug(acetaminophen).

  • PDF

Structure-activity relationships on the herbicidal activity of the 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl substituents in 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one derivatives (5-Benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one 유도체 중 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl 치환체들의 제초활성에 관한 구조-활성관계)

  • Sung, Nack-Do;Song, Jong-Hwan;Kim, Kyoung-Mahn
    • The Korean Journal of Pesticide Science
    • /
    • v.4 no.3
    • /
    • pp.34-39
    • /
    • 2000
  • A new fifteen 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl substituents in 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one derivatives as substrate were synthesized and their herbicidal activities against rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-galli) with post emergence were measured under submerged conditions. The $R_{1}$=methyl substituents, $1{\sim}8$ showed the higher herbicidal activity to the rice plant and barnyard grass. The structure-activity relationships (SARs) on tile herbicidal activity of $R_{1}$ and $OR_{2}$ groups on the azomethine bond in substrates were analysized. From tile results of dicussed SAR, the herbicide activities against rice plant would depend largely on the steric factor, Whereas, in case of barnyard grass, the activities were governed by the hydrophobicity factor. The conditions of selective herbicide activity between the two plant species are assumed that the substrates should nave optimal hydrophobicity ( $(logP)_{opt.}=6.0$), a $R_{1}$ groups of small and a long $OR_{2}$ groups.

  • PDF

Synthesis and structure of $[Cp^*Rh({\eta}^6-2,6-diisopropylaniline)](OTF)_2$

  • 백지영;한원석;이순원
    • Proceedings of the Korea Crystallographic Association Conference
    • /
    • 2002.11a
    • /
    • pp.29-29
    • /
    • 2002
  • Reaction of [$Cp^*Rh(NO_3)OTf$] (1) with 2,6-diisopropylaniline under argon led to the formation of $[Cp^*Rh({\eta}^6-2,6-diisopropylaniline)](OTF)_2$, (2). Compound 2 was characterized by NMR, IR, elemental analysis, and X-ray diffraction. Crystallrographc data for 2: orthorhombic, space group $Cmc2_1$, $a=19.850(16){\AA}$, $b=9.870(8){\AA}$, $c=15.774(13){\AA}$, Z = 4, $R(wR_2)=0.0362(0.0938)$.

  • PDF

Enhanced Bioavailability of Itraconazole in Liquid Preparation (난용성 항진균제 이트라코나졸의 액상제제화에 의한 생체이용율 개선)

  • Hwang, Woo-Sin;Kwon, Kwang-Il;Bang, Kyu-Ho
    • YAKHAK HOEJI
    • /
    • v.44 no.6
    • /
    • pp.528-533
    • /
    • 2000
  • This study was to develop an effective itraconazole liquid preparation which exhibits an enhanced bioavailability. The solubility of itraconazole was increased (72-fold) in itraconazole liquid preparation as compared with itraconazole powder. The dissolution rate of itraconazole was higher for itraconazole liquid preparation filled into a hard gelatin capsule with 90% release within 20 min as compared to 55% for $Sporanox^{\circledR}$capsules. The oral absorption of itraconazole liquid preparation and $Sporanox^{\circledR}$tablets were studied in the rat. The area under the concentration-time curve $(AUC_{0-24hr})$ of itraconazole liquid preparation ($90.25\;{\pm}\;8.36\;{\mu}g{\cdot}hr/ml$) increased by 6.2 times compared to that of Sporanox tablets ($14.58\;{\pm}\;1.26\;{\mu}g{\cdot}hr/ml$) after oral administration of itraconazole 15 mg/rat each. $C_{max}$ also increased to $6.87\;{\pm}\;1.15\;{\mu}g/ml$ after administration of liquid preparation $1.58\;{\pm}\;0.16\;{\mu}g/ml$ of $Sporanox^{\circledR}$tablets. These results indicate that in vivo bioavailability of itraconazole liquid preparation was significantly enhanced as compared with $Sporanox^{\circledR}$tablets.

  • PDF