• Title/Summary/Keyword: Ester

Search Result 2,593, Processing Time 0.033 seconds

Synthesis and Biological Evaluation of Water-Soluble Oleanolic Acid Derivatives for use as Melanogenesis Inhibitors (멜라닌 생합성 억제제로서 수용성 Oleanolic Acid 유도체의 합성 및 활성 평가)

  • An, Hyun-Jin;Yoon, Young-kyung;Lee, Jae-Duck;Jeong, Noh-Hee
    • Applied Chemistry for Engineering
    • /
    • v.31 no.6
    • /
    • pp.653-659
    • /
    • 2020
  • This study was focused on the synthesis of methoxy polyethylene glycol-oleanolic acid ester (mPEG-OA derivative) and investigation of its water solubility and anti-melanogenic effects. mPEG-OA derivative was identified by 1H and 13C NMR and FT-IR spectroscopic measurements. The water solubilities of mPEG-OA derivative and OA were found to be 13 and 0.013 mg/mL and that of mPEG-OA was found to be 1000-fold higher than that of OA. The effects of mPEG-OA derivative and OA on cell viability were measured using B16F10 melanoma cells. The viability of cells treated with mPEG-OA derivative (250 μM) increased 4-fold compared to that of cells treated with OA (62.5 μM). At mPEG-OA derivative and OA concentrations where the cell viability was unaffected, the inhibitory effect of mPEG-OA derivative and OA on the melanogenesis in B16F10 melanoma cells were 36 and 35% at 50 and 10 μM, respectively. The expression level of microphthalmia-associated transcription (MITF) was also reduced in B16F10 melanoma cells treated with mPEG-OA and OA. Overall, mPEG-OA derivative showed excellent water solubility and inhibitory effects of the melanogenesis, which could be used as a potential formulation for use in whitening functional cosmetic material.

Polymer Eyeglass Lens with Ultraviolet & High-Energy Visible Light Blocking Function for Eye Health (자외선 및 고에너지 가시광 차단 기능을 갖는 눈 건강을 위한 폴리머 안경렌즈)

  • Kim, Ki-Chul
    • Journal of the Korea Academia-Industrial cooperation Society
    • /
    • v.21 no.12
    • /
    • pp.10-15
    • /
    • 2020
  • Ultraviolet rays, which have wavelengths smaller than 400 nm, are very harmful to the eyes. Recently, high-energy visible light was also revealed to be harmful to retinal cells. Therefore, polymer eyeglass lenses that can block UV and high-energy visible light are needed for eye health. In this study, high-refractive-index polymer eyeglass lens, n=1.67, were manufactured using the injection-mold method with the m-xylene diisocyanate monomer, 2,3-bis((2-mercaptoethyl)thio)-1-propanethiol monomer, benzotriazole UV absorber, release of alkyl phosphoric ester, dye mixture of CI solvent violet 13, and catalyst of dibutyltin dichloride mixture. A multi-layer anti-reflection coating was applied to manufactured polymer eyeglass lenses for both sides using an E-beam evaporation system. The optical properties of the manufactured lenses with the UV and high-energy visible light-blocking function were analyzed by UV-visible spectrophotometry. As a result, the polymer eyeglass lens with a UV absorber of 0.5 wt. % blocked 99% of UV and high-energy visible light shorter than 411 nm. The average transmittance of the polymer eyeglass lens with a UV absorber of 0.5wt.% was 97.9% in the range of 460 ~ 660 nm for photopic eye sensitivity higher than 10%. Therefore, clear image acquisition in photopic vision is possible.

Vasorelaxant Effect of Prunus yedoensis leaf on Rat Aortic Rings (앵엽(櫻葉) 에탄올 추출물의 혈관이완 효능 및 작용기전에 대한 연구)

  • Lee, Kyungjin;Kim, Kwang-Woo;Heo, Heeseung;Ham, Inhye;Lee, Mi-Hwa;Kim, Bumjung;Bu, Youngmin;Kim, Hocheol;Choi, Ho-Young
    • The Korea Journal of Herbology
    • /
    • v.28 no.4
    • /
    • pp.63-69
    • /
    • 2013
  • Objectives : The purpose of present study was to investigate the vasorelaxant activities and mechanisms of action of the ethanol extract of P. yedoensis leaf (PYL) on isolated rat aortic rings. Methods : Dried P. yedoensis leaves were extracted 3 times with 100% ethanol for 3 h in a reflux apparatus. Isolated rat aortic rings were suspended in organ chambers containing 10 ml Krebs-Henseleit (K-H) solution. The rings were maintained at $37^{\circ}C$ and aerated with a mixture of 95% $O_2$ and 5% $CO_2$. Changes in their tension were recorded via isometric transducers connected to a data acquisition system. Results : PYL relaxed the contraction of aortic rings induced by phenylephrine (PE, 1 ${\mu}M$) or KCl (60 mM) in a concentration dependent manner. However, the vasorelaxant effects of PYL on endothelium-denuded aortic rings were lower than endothelium-intact aortic rings. And the vasorelaxant effects of PYL on endothelium-intact aortic rings were reduced by pre-treatment with $N{\omega}$-Nitro-L-arginine methyl ester (10 ${\mu}M$), methylene blue (10 ${\mu}M$), 1-H-[1,2,4]-oxadiazolo-[4,3-${\alpha}$]-quinoxalin-1-one (10 ${\mu}M$), tetraethylammonium (5 mM). In addition, PYL inhibited the contraction induced by extracellular $Ca^{2+}$ in endothelium-denuded aortic rings pre-contracted by PE or KCl in $Ca^{2+}$-free K-H solution. Conclusions : These results suggest that PYL exerts its vasorelaxant effects via the activation of Nitric Oxide (NO) formation by means of L-arginine and NO-cGMP pathways and via the blockage of receptor operated calcium channels, voltage dependent calcium channels and calcium-activated potassium channels.

Enhancing the Anti-cancer Activity of Non-steroidal Anti-inflammatory Drug and Down-regulation of Cancer Stemness-related Markers in Human Cancer Cells by DAPT and MHY2245 (DAPT 및 MHY2245의 비스테로이드소염제(NSAID)의 항암 활성 증강 및 종양줄기세포관련 표지자 발현 감소 활성에 대한 분자적 기전)

  • Moon, Hyun-Jung;Kang, Chi-Dug;Kim, Sun-Hee
    • Journal of Life Science
    • /
    • v.32 no.3
    • /
    • pp.210-221
    • /
    • 2022
  • This study investigated the mechanisms underlying the anti-cancer effects of non-steroidal anti-inflammatory drugs (NSAIDs) in human cancer cells in combination with either N-[N-(3, 5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester (DAPT), a γ-secretase inhibitor, or MHY2245, a new synthetic sirtuin 1 inhibitor. The results showed both DAPT and MHY2245 as novel chemosensitizers of human colon cancer KM12 and human hepatocellular carcinoma SNU475 cells to NSAIDs involving celecoxib and 2, 5-dimethyl celecoxib. The NSAID-induced cytotoxicity of these cells was significantly increased by DAPT and MHY2245 in a cyclooxygenase-2 independent manner. In addition, DAPT and MHY2245 reduced levels of p62, Notch1 intracellular domain, and multiple cancer stemness (CS)-related markers including Notch1, CD44, CD133, octamer-binding transcription factor 4, mutated p53 and c-Myc. However, the level of activating transcription factor 4 (ATF4) was enhanced, probably indicating the down-regulation of multiple CS-related markers by DAPT or MHY2245-mediated autophagy induction. Moreover, the NSAID-mediated reduction of p62/nuclear factor erythroid-derived 2-like 2 and CS-related marker proteins and the up-regulation of C/EBP homologous protein (CHOP)/ATF4 were accelerated by DAPT and MHY2245. As such, the combination of NSAID and either DAPT or MHY2245 resulted in higher cytotoxicity than NSAID alone by accelerating the down-regulation of multiple CS-related markers and PARP activation, indicating that both inhibitors promote NSAID-mediated autophagic cell death, possibly through the CHOP/ATF4 pathway. In conclusion, either combination strategy may be useful for the effective treatment of human cancer cells expressing CS-related markers.

Anti-Termite Activity of Azadirachta excelsa Seed Kernel and Its Isolated Compound against Coptotermes curvignathus

  • Morina ADFA;Khafit WIRADIMAFAN;Ricky Febri PRATAMA;Angga SANJAYA;Deni Agus TRIAWAN;Salprima YUDHA S.;Masayuki NINOMIYA;Mohamad RAFI;Mamoru KOKETSU
    • Journal of the Korean Wood Science and Technology
    • /
    • v.51 no.3
    • /
    • pp.157-172
    • /
    • 2023
  • Azadirachta excelsa, is a plant belonging to the same genus as Indian neem (Azadirachta indica), and its use as a pesticide is reported by few studies. Despite being a different species, it is expected to have the same biopesticide potential as A. indica. Therefore, this study aims to investigate the anti-termite activity of n-hexane and methanol extracts of A. excelsa seed kernel at various concentrations against Coptotermes curvignathus. The methanol extract demonstrated greater termicidal activity than n-hexane at doses test of 2%, 4%, and 8%. It also showed 100% termite mortality on the third day of administering the 8% dose. According to the gas chromatography with mass spectrometry data, the putative main components of the n-hexane extract were hexadecanoic acid, ethyl ester (18.99%), 9,12-octadecadienoic acid (Z,Z)- (16.31%), and 9-octadecenal (16.23%). In contrast, the principal constituents of methanol extract were patchouli alcohol (28.1%), delta-guaiene (15.15%), and alpha-guaiene (11.93%). Furthermore, limonoids profiling of A. excelsa methanol extract was determined using Ultrahigh-performance liquid chromatography coupled with quadrupole-Orbitrap high-resolution mass spectrometry. The number of limonoids identified tentatively was fifteen, such as 6-deacetylnimbin, nimbolidin C, nimbolide, 6-acetylnimbandiol, 6-deacetyl-nimbinene, salannol, 28-deoxonimbolide, gedunin, nimbandiol, epoxyazadiradione, azadirone, 2',3'-dihydrosalannin, marrangin, nimbocinol, and azadirachtin. They were the same as those reported in the seed and leaves of A. indica, but its largest component in A. excelsa was 6-deacetylnimbin. As a result, the presence of these compounds may be responsible for the anti-termite activity of A. excelsa seed kernel extract. Additionally, column chromatography of methanol extract yielded 6-deacetylnimbin, which was found to be antifeedant and termiticide against C. curvignathus.

Properties of Liquid Crystalline Polyester/Poly(ethylene 2,6-naphthalate) Blend Fibers (액정 폴리에스테르/PEN 블렌드 섬유의 성질)

  • Kim, Won;Kim, Young-Yong;Son, Jung-Sun;Yun, Doo-Soo;Han, Chul;Choi, Jae-Kon;Jo, Byung-Wook
    • Elastomers and Composites
    • /
    • v.37 no.4
    • /
    • pp.244-257
    • /
    • 2002
  • A thermotropic liquid crystalline polymer(TLCP) which has flexible butylene/hexylene spacers in the main chain and a triad aromatic ester type mesogenic unit containing a naphthyl group was prepared by solution polycondensation. The in-situ composites based on poly(ethylene 2,6-naphthalate) (PEN) and a thermotropic liquid crystalline polymer(TLCP) were prepared and melt spun at different TLCP contents and different draw ratios to produce monofilaments. Blends of the TLCP with PEN were investigated in terms of thermal, mechanical properties and morphology. The TLCP synthesized showed nematic mesophasic behavior and its transition temperature to isotropic melt from mesophase was 249℃. The blends showed well dispersed TLCP phases in the PEN matrix without macroscopic phase separation. Inclusion of TLCP in the blends decreased the cold crystallization temperature of PEN in the blend, therefore, the TLCP acts as a nucleating agent in the blend and showed good interfacial adhesion between the dispersed LCP phases and PEN matrix with domain sizes 40~50 nm in diameter and well developed fibrillation in the monofilaments. The TLCP acted effectively as a reinforcing material in the PEN matrix at the 10wt% level, it led to an increase of initial modulus up to 270% and tensile strength by 235%, while the elongation rate increasing with higher draw ratios.

Analysis of Mineral and Volatile Flavor Compounds in Pimpinella brachycarpa N. by ICP-AES and SDE, HS-SPME-GC/MS (ICP-AES와 SDE, HS-SPME-GC/MS를 이용한 참나물의 무기성분과 향기성분)

  • Chang, Kyung-Mi;Chung, Mi-Sook;Kim, Mi-Kyung;Kim, Gun-Hee
    • Journal of the Korean Society of Food Culture
    • /
    • v.22 no.2
    • /
    • pp.246-253
    • /
    • 2007
  • Mineral and volatile flavor compounds of Pimpinella brochycarpa N., a perennial Korean medicinal plant of the Umbelliferae family, were analyzed by inductively coupled plasma-atomic emission spectroscopy (ICP-AES) and simultaneous steam distillation extract (SDE)-gas chromatography mass spectrometry (GC/MS), head space solid phase micro-extraction (HS-SPME)-GC/MS. Mineral contents of the stalks and leaves were compared and the flavor patterns of the fresh and the shady air-dried samples were obtained by the electronic nose (EN) with 6 metal oxide sensors. Principal component analysis (PCA) was carried out using the data obtained from EN. The 1st principal values of the fresh samples have + values and the shady air-dried have - values. The essential oil extracted from the fresh and the shady air-dried by SDE method contain 58 and 31 flavor compounds. When HS-SPME method with CAR/PDMS fiber and PDMS fiber were used, 34 and 21 flavor compounds. The principal volatile components of Pimpinella brachycarpa N. were ${\alpha}$-selinene, germacrene D, and myrcene.

Purple perilla frutescens extracts containing α-asarone inhibit inflammatory atheroma formation and promote hepatic HDL cholesterol uptake in dyslipidemic apoE-deficient mice

  • Sin-Hye Park;Young Eun Sim;Min-Kyung Kang;Dong Yeon Kim;Il-Jun Kang;Soon Sung Lim;Young-Hee Kang
    • Nutrition Research and Practice
    • /
    • v.17 no.6
    • /
    • pp.1099-1112
    • /
    • 2023
  • BACKGROUND/OBJECTIVES: Dyslipidemia causes metabolic disorders such as atherosclerosis and fatty liver syndrome due to abnormally high blood lipids. Purple perilla frutescens extract (PPE) possesses various bioactive compounds such as α-asarone, chlorogenic acid and rosmarinic acid. This study examined whether PPE and α-asarone improved dyslipidemia-associated inflammation and inhibited atheroma formation in apolipoprotein E (apoE)-deficient mice, an experimental animal model of atherosclerosis. MATERIALS/METHODS: ApoE-deficient mice were fed on high cholesterol-diet (Paigen's diet) and orally administrated with 10-20 mg/kg PPE and α-asarone for 10 wk. RESULTS: The Paigen's diet reduced body weight gain in apoE-deficient mice, which was not restored by PPE or α-asarone. PPE or α-asarone improved the plasma lipid profiles in Paigen's diet-fed apoE-deficient mice, and despite a small increase in high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein (LDL)-cholesterol, and very LDL were significantly reduced. Paigen's diet-induced systemic inflammation was reduced in PPE or α-asarone-treated apoE-deficient mice. Supplying PPE or α-asarone to mice lacking apoE suppressed aorta atherogenesis induced by atherogenic diet. PPE or α-asarone diminished aorta accumulation of CD68- and/or F4/80-positive macrophages induced by atherogenic diet in apoE-deficient mice. Treatment of apoE-deficient mice with PPE and α-asarone resulted in a significant decrease in plasma cholesteryl ester transfer protein level and an increase in lecithin:cholesterol acyltransferase reduced by supply of Paigen's diet. Supplementation of PPE and α-asarone enhanced the transcription of hepatic apoA1 and SR-B1 reduced by Paigen's diet in apoE-deficient mice. CONCLUSIONS: α-Asarone in PPE inhibited inflammation-associated atheroma formation and promoted hepatic HDL-C trafficking in dyslipidemic mice.

Rosmarinic Acid Inhibits Ultraviolet B-Mediated Oxidative Damage via the AKT/ERK-NRF2-GSH Pathway In Vitro and In Vivo

  • Mei Jing Piao;Pattage Madushan Dilhara Jayatissa Fernando;Kyoung Ah Kang;Pincha Devage Sameera Madushan Fernando;Herath Mudiyanselage Udari Lakmini Herath;Young Ree Kim;Jin Won Hyun
    • Biomolecules & Therapeutics
    • /
    • v.32 no.1
    • /
    • pp.84-93
    • /
    • 2024
  • Rosmarinic acid (RA) is a phenolic ester that protects human keratinocytes against oxidative damage induced by ultraviolet B (UVB) exposure, however, the mechanisms underlying its effects remain unclear. This study aimed to elucidate the cell signaling mechanisms that regulate the antioxidant activity of RA and confirm its cyto-protective role. To explore the signaling mechanisms, we used the human keratinocyte cell line HaCaT and SKH1 hairless mouse skin. RA enhanced glutamate-cysteine ligase catalytic subunit (GCLC) and glutathione synthetase (GSS) expression in HaCaT cells in a dose- and time-dependent manner. Moreover, RA induced nuclear factor erythroid-2-related factor 2 (NRF2) nuclear translocation and activated the signaling kinases protein kinase B (AKT) and extracellular signal-regulated kinase (ERK). Treatment with the phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002, the ERK inhibitor U0126, and small interfering RNA (siRNA) gene silencing suppressed RA-enhanced GCLC, GSS, and NRF2 expression, respectively. Cell viability tests showed that RA significantly prevented UVB-induced cell viability decrease, whereas the glutathione (GSH) inhibitors buthionine sulfoximine, LY294002, and U0126 significantly reduced this effect. Moreover, RA protected against DNA damage and protein carbonylation, lipid peroxidation, and apoptosis caused by UVB-induced oxidative stress in a concentration-dependent manner in SKH1 hairless mouse skin tissues. These results suggest that RA protects against UVB-induced oxidative damage by activating AKT and ERK signaling to regulate NRF2 signaling and enhance GSH biosynthesis. Thus, RA treatment may be a promising approach to protect the skin from UVB-induced oxidative damage.

[RETRACTED] Changes in the volatile aromatic compounds and amino acid contents of distilled soju using co-fermentation by Saccharomyces cerevisiae and Hanseniaspora uvarum yeasts ([논문철회] Saccharomyces cerevisiae 와 Hanseniaspora uvarum 효모 혼합발효를 이용한 증류식 소주의 휘발성 향기성분 및 아미노산 함량 변화)

  • Kyu-Taek Choi;Chun-Woo Park;Su-Hyun Lee;Ye-Na Lee;Ji-Yun Oh;Jun-Su Choi;Deokyeong Choe;Sae-Byuk Lee
    • Food Science and Preservation
    • /
    • v.30 no.6
    • /
    • pp.1029-1042
    • /
    • 2023
  • This study aimed to apply the technology of increasing the volatile aromatic compounds in wine through mixed fermentation of Saccharomyces cerevisiae and non-Saccharomyces yeasts to make distilled soju. The expectation was to induce changes in metabolites such as volatile aromatic compounds before the distillation process, followed by concentrating these compounds through distillation to enhance the odor property of distilled soju. Additionally, the study aimed to examine the impact of mixed fermentation with S. cerevisiae and non-Saccharomyces yeasts on distilled soju's free amino acid content. As a result, when Hanseniaspora uvarum yeast was used, there was an increase in the content of low molecular weight volatile aroma compounds, particularly esters. Distilled soju co-fermented with S. cerevisiae and H. uvarum SJ69 exhibited similar amino acid content to distilled soju single-fermented with S. cerevisiae. However, distilled soju co-fermented with S. cerevisiae and H. uvarum S6, a decrease in amino acid content. Sensory evaluation results indicated a higher odor score in distilled soju co-fermented with S. cerevisiae and H. uvarum S6, suggesting that the mixed fermentation technology utilizing H. uvarum could contribute to improving the quality of distilled soju in the future.