• Biomolecules & Therapeutics
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• 제28권2호
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• pp.163-171
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• 2020

Silibinin exhibits antidiabetic potential by preserving the mass and function of pancreatic β-cells through up-regulation of estrogen receptor-α (ERα) expression. However, the underlying protective mechanism of silibinin in pancreatic β-cells is still unclear. In the current study, we sought to determine whether ERα acts as the target of silibinin for the modulation of antioxidative response in pancreatic β-cells under high glucose and high fat conditions. Our in vivo study revealed that a 4-week oral administration of silibinin (100 mg/kg/day) decreased fasting blood glucose with a concurrent increase in levels of serum insulin in high-fat diet/streptozotocin-induced type 2 diabetic rats. Moreover, expression of ERα, NF-E2-related factor 2 (Nrf2), and heme oxygenase-1 (HO-1) in pancreatic β-cells in pancreatic islets was increased by silibinin treatment. Accordingly, silibinin (10 μM) elevated viability, insulin biosynthesis, and insulin secretion of high glucose/palmitate-treated INS-1 cells accompanied by increased expression of ERα, Nrf2, and HO-1 as well as decreased reactive oxygen species production in vitro. Treatment using an ERα antagonist (MPP) in INS-1 cells or silencing ERα expression in INS-1 and NIT-1 cells with siRNA abolished the protective effects of silibinin. Our study suggests that silibinin activates the Nrf2-antioxidative pathways in pancreatic β-cells through regulation of ERα expression.

• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.155-161
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• 1992

Although glycosylated liposomes have attracted much attention as targeting delivery systems (DDS) of drugs to specific organs which have glycoside receptors, physical instability of liposomes greatly limits their practical application. In this case, proliposomes might be a potential answer to solve this problem. Utilizing the proliposomes as tageting DDS has been a goal of our series of works; we have tried to develop DDS which form liposomes uppon adding water and can deliver drugs to specific target organs/cells such as hepatocytes. In this paper, preparation of glycosylated liposomes and binding of the liposomes with lectin (agglutinin RCA 120) was studied. Asialoletuin (AF) was selected as a model compound which has galactose terminal and is favorable for binding with galactose receptor on the surface of hepatocytes. AF was obtained by splitting the terminal N-acetylneuraminic acid (NANA) of fetuin. Small unilamellar AF-liposomes were prepared by mixing aqueous solution of AF-palmitate with thin film of phosphatidyl choline and cholesterol (30:10 w/w) formed on the innersurface of the round bottomed flask. They were successively extruded through polycarbonate membranes (0.45 mm). Palmitoyl-AF not incorporated into the liposomal bilayer was separated from liposomes by a Sepharose 4B column equilibrated with 10 mM Tris-HCI buffered saline. Lectin (agglutinin RCA 120) was added to the suspension of AF-liposomes and incubated at $37^{\circ}C$ for 2 hr. After centrifugation, the unbound lectin in the supernatant was assayed for protein. The binding of the lectin to AF-liposomes (AF content 2.8 nmole) at $37^{\circ}C$ was linear at least upto 35 mg of lectin indicating high affinity association of the lectin to AF molecules of the liposomes.

• Journal of Pharmaceutical Investigation
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• 제41권6호
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• pp.331-336
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• 2011

The instability of hirsutenone (HST), a potential therapeutic candidate for the treatment of atopic dermatitis (AD) and ovarian carcinoma, is one of the main concerns for the development of drug product. In the present study, aqueous stability of HST was investigated by kinetic analysis, and the effect of several factors covering temperature, nitrogen gas ($N_2$) flushing, and selection of proper antioxidant was compared. Cosolvent system composed of distilled water and methanol (9:1 v/v) was used as a vehicle to dissolve HST at the concentration of $200{\mu}g/mL$. Samples of aqueous solution were prepared under the absence or presence of antioxidants, such as ascorbic acid (AA), sodium edetate (EDTA), and ascorbyl palmitate (AP), and subjected for stability test. The degradation of HST in aqueous solution was followed by the first order kinetics with an extremely short half life of less than a week at room temperature, and was accelerated as the temperature increased. $N_2$ flushing brought a little enhancement in stability compared to control solution, but the effect was insufficient. The addition of AA and EDTA (0.1%) significantly enhanced the stability of HST at $40^{\circ}C$, but the addition of AP (0.01%) was limited due to its water insolubility and revealed no promising result. The stability of HST was increased proportionally by the amount of AA added, showing the difference in degree of stabilization as an order of magnitude. Finally, we conclude that HST was stabilized by the addition of a suitable antioxidant, suggesting AA as the most effective stabilizer.

• Journal of Microbiology and Biotechnology
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• 제24권8호
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• pp.1123-1132
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• 2014

This study evaluated the growth and nutrient removal ability of an indigenous algal consortium on real untreated municipal wastewater in a high rate algal pond (HRAP). The HRAP was operated semicontinuously under different hydraulic retention times (HRT: 2, 4, 6, and 8 days). The average removal efficiencies of chemical oxygen demand, and total nitrogen and phosphate of real municipal wastewater were maintained at $85.44{\pm}5.10%$, $92.74{\pm}5.82%$, and $82.85{\pm}8.63%$, respectively, in 2 day HRT. Algae dominated the consortium and showed high settling efficiency (99%), and biomass and lipid productivity of $0.50{\pm}0.03g/l/day$ and $0.103{\pm}0.0083g/l/day$ (2day HRT), respectively. Fatty acid methyl ester analysis revealed a predominance of palmitate (C16:0), palmitoleate (C16:1), linoleate (C18:2), and linolenate (C18:3). Microalgal diversity analyses determined the presence of Chlorella, Scenedesmus, and Stigeoclonium as the dominant microalgae. The algal consortium provides significant value not only in terms of energy savings and nutrient removal but also because of its bioenergy potential as indicated by the lipid content (20-23%) and FAME profiling.

• 한국응용과학기술학회지
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• 제17권2호
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• pp.67-75
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• 2000

Cosmetic industries have recently developed sun-block products, which are composed of W/O or O/W emulsion system. It was very difficult for waterproofing product to show the stability in W/O emulsion with $TiO_{2}$. To enhance the stability of W/O emulsion, it needs to be combined with the water and oil soluble components as the gelling agents. The emulsifiers used in W/O were 3.0% of cetyl dimethicone copolyol, 2.0% of sorbitan sesquioleate as the basic emulsifiers, and 0.6% of quaternium-18 bentonite and 1.5% of dextrin palmitate as stabilizer were used. The content of titanium dioxide was optimized up to 8.0%. Titanium dioxide was used as the UV scattering powder coated with $Al_{2}O_{3}$(UV-sperse T40/TN). The sunscreen cream prepared with W/O emulsion system by using QB and DP showed higher stability than that of W/O emulsion system by using each QB and DP. W/O emulsion from Formula 3 for passing one year was very durable more than F1 and F2. Within W/O emulsion by observing F1, F2 and F3 for one year, F3 was more excellent than F2 and F3 when they were observed at RT, $4^{\circ}C$, $40^{\circ}C$, because F3 used the mixed QB and DP in W/O emulsion. The zeta potential for F1, F2, and F3 after one year were 21, 30 and 43, respectively. From these result F3 was found best stable emulsion. The in-vitro SPF value for F3 was 35 for the initial product at room temperature and also, the in-vitro SPF values of F3 was 32 for after one year. Finally, the mean in-vivo SPF value of 10 volunteers for F3 was 27.3 by the Korea cosmetic association made the rules of SPF.

• Journal of Microbiology and Biotechnology
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• 제23권11호
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• pp.1569-1576
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• 2013

In mice, supplementation of t10,c12 conjugated linoleic acid (CLA) increases liver mass and hepatic steatosis via increasing uptake of fatty acids released from adipose tissues. However, the effects of t10,c12 CLA on hepatic lipid synthesis and the associated mechanisms are largely unknown. Thus, we tested the hypothesis that gut microbiota-producing t10,c12 CLA would induce de novo lipogenesis and triglyceride (TG) synthesis in HepG2 cells, promoting lipid accumulation. It was found that treatment with t10,c12 CLA ($100{\mu}M$) for 72 h increased neutral lipid accumulation via enhanced incorporation of acetate, palmitate, oleate, and 2-deoxyglucose into TG. Furthermore, treatment with t10,c12 CLA led to increased mRNA expression and protein levels of lipogenic genes including SREBP1, ACC1, FASN, ELOVL6, GPAT1, and DGAT1, presenting potential mechanisms by which CLA may increase lipid deposition. Most strikingly, t10,c12 CLA treatment for 3 h increased phosphorylation of mTOR, S6K, and S6. Taken together, gut microbiota-producing t10,c12 CLA activates hepatic de novo lipogenesis and TG synthesis through activation of the mTOR/SREBP1 pathway, with consequent lipid accumulation in HepG2 cells.

• BMB Reports
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• 제45권1호
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• pp.26-31
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• 2012

TRIM72 is known to play a critical role in skeletal muscle membrane repair. To better understand the molecular mechanisms of this protein, we carried out an in vitro binding study with TRIM72. Our study proved that TRIM72 binds various lipids with dissociation constants ($K_d$) ranging from 88.2 ${\pm}$ 9.9 nM to 550.5 ${\pm}$ 134.5 nM. In addition, the intrinsic fluorescence of TRIM72 exponentially decreased when the protein was diluted with stirring. The time-resolved fluorescence decay occurred in a concentration-independent manner. The fluorescence-decayed TRIM72 remained in its secondary structure, but its binding properties were significantly reduced. The dissociation constants ($K_d$) of fluorescence-decayed TRIM72 for palmitate and stearate were 159.1 ${\pm}$ 39.9 nM and 355.4 ${\pm}$ 106.0 nM, respectively. This study suggests that TRIM72 can be dynamically converted by various stimuli. The results of this study also provide insight into the role of TRIM72 in the repair of sarcolemma damage.

• 공업화학
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• 제26권6호
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• pp.659-665
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• 2015

지용성 토코페롤(${\alpha}$-tocopherol)의 산화 안정성을 높이기 위하여 nanostructured lipid carrier (NLC)에 봉입을 시도하였다. 먼저 구성 성분과 혼합 비율을 달리한 여러 NLC를 만들고 각각의 특성을 살펴보았다. 고체 지질로 세틸 팔미테이트 또는 글리세릴 모노스테아레이트를 사용했을 때는 안정한 상태의 NLC 입자가 만들어지지만 스테아린 산으로 만든 NLC에서는 상분리가 일어났다. NLC 입자는 수백 나노미터 크기로 만들어지는데 지질대비 용매의 비율이 높을수록 입자크기가 작게 나타났다. 고급 지방알콜인 옥틸도데칸올을 고체 지질에 첨가하면 결정화도가 감소하면서 지질 매트릭스의 배열규칙성 이 약해짐을 DSC (Differential Scanning Calorimetry) 열차트와 anisotropy 측정을 통해서 확인하였다. 고온($45^{\circ}C$) 또는 UV 빛이 조사되는 조건에서 토코페롤이 NLC에 봉입되어 있으면 용액이나 에멀젼 상태로 있는 것에 비해 산화 안정성이 크게 향상됨을 DPPH 테스트와 과산화물가 측정으로 확인하였다.

• 한국식품조리과학회지
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• 제14권5호
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• pp.560-565
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• 1998

The purpose of this study was to investigate any differences in the efficiency of various antioxidants for the three types of substrates such as corn oil in water (O/W) emulsion, water in com oil (W/O) emulsion, and bulky corn oil. ${\alpha}$-Tocopherol (${\alpha}$-Toc) at 0.01 or 0.02%, ascorbic acid (AsA), ascorbyl palmitate (AP), and BHT at 0.02% were added separately to the prepared O/W emulsion, W/O emulsion, and bulk oil, and their antioxidative effects were compared. The mixture of ${\alpha}$-Toc ind AsA or AP at the level of 0.02% also was tested to observe any synergistic effect. Oxidation was made by storing at 42${\pm}$1$^{\circ}C$ for 25 days and the oxidative stability was determined by peroxide value and conjugated dienoic acid with time fluctuation of storage. The results were as follows: 1. In case of O/W emulsion, the order of antioxidative effect was AP> ${\alpha}$-Toc+AP>${\alpha}$-Toc+AsA>AsA>BHT. 2. In case of W/O emulsion, the order of antioxidative effect was AsA>AP>${\alpha}$-Toc+AsA>BHT. ${\alpha}$-Toc+AP mixture showed the prooxidant effect rather than synergistic effect. 3. In case of bulk oil, the order of antioxidative effect was AsA>AP>${\alpha}$-Toc+AsA>${\alpha}$-Toc+AP\ulcornerBHT. Therefore, AsA, a hydrophilic antioxidant, was more effective in W/O emulsion system than in O/W emulsion system, while the opposite trend was found in AP, a lipophilic antioxidant. AsA, a hydrophilic antioxidant, was more efficient in bulk oil of anhydrous substrate. ${\alpha}$-Toc showed prooxidant effects in all substrates.

• Asian-Australasian Journal of Animal Sciences
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• 제19권6호
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• pp.825-830
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• 2006

Status of blood minerals and their absorption by neonate calves as influenced by fat soluble vitamins supplementation in their respective mothers, mineral supplementation in calves themselves has been evaluated. The objective was to know the impact of antioxidant vitamin supplementation to advance pregnant buffaloes, on enhanced acquired immunity during first few hours after birth, in relation to weight gain in buffalo calves. Advance pregnant buffaloes (n = 30) consisting of average body weight of $550{\pm}15$ kg and of 4-6 parity were fed on 25 kg green (green Jawar-Sorghum bicolor), 2-3 kg wheat straw and 3-4 kg concentrate mixture individually per day. Intramuscular injections of vitamin triplex A $D_3$ E consisting of -2,500,000 IU of vit A -Palmitate; 2,500,000 IU of vitamin $D_3$ and 1,000 IU of vit E (dl-alpha tocopherol acetate) were given per dose, a month prior to parturition, twice at 15 days interval to 15 dams. Rest of the 15 pregnant buffaloes served as negative controls. Secretion of immune proteins, immunoglobulin (Ig) enhanced by 80% in colostrum. The blood serum levels of Zn, Cu, Ca, Mg were measured from birth to 90 days in calves. A significant (p<0.05) difference between the blood serum Zn levels of calves born to vitamin supplemented and non-supplemented dams was measured and a positive correlation between blood serum Zn levels and injections of vitamins was identified. Association of Zn and Cu with passive immunity status has been identified in these calves. A significant positive correlation between Zn and Cu was also identified which showed a change under the impact of vitamin supplementation in buffaloes. The study signifies the role of micronutrients supplementation in dams prior to parturition, in calf immunity development. The study indicates significant mineral - vitamins interactions during this process.