• 한국식품영양학회지
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• 제14권6호
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• pp.591-595
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• 2001

참깨 탈지박에 다량존재하는 수용성 lignan화합물을 $\beta$-glucosidase로 처리하여 얻어진 참깨박 추출물의 항산화 효과 및 기존 항산화제들과의 상승효과를 비교, 검토하고자 하였다. 참깨박 추출물 중에서도 sesamin 및 sesamolin이 peak가 확인되었으며, 각각 8.32%(8,315.4mg/100g) 및 0.28%(2,824.5mg/100g)의 함량을 나타냈다. Sesamin과 sesamolin은 배당체의 aglycone으로서 탈지박 중에 존재하는 것으로 나타났다. 참깨박 추출물의 항산화효과는 첨가농도가 증가함에 따라 증가되었으며, 이들의 효과는 같은 농도(100ppm)의 $\alpha$-tocopherol이나 ascorbyl palmitate 첨가구보다 항산화효과가 우수하였으나 BHA보다는 다소 약한 효과를 보였다. 또한 가수분해 물은 $\alpha$-tocopherol과 강한 상승 작용을 보여주었으나 ascorbyl palmitate와는 비교적 약한 상승작용을 나타내었다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.211-211
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• 1994

항종양성 화합물의 개발을 지향한 해양생물 유래의 생물활성 물질의 화학적 연구의 일환으로써 다양한 종류의 생물활성 (즉, 항균작용, 혈중콜레스테롤 저하작용)등을 나타내며, 구입수가 용이한 홍조 꼬시래기 (Gracilaria verrucosa) 및 갈조 지충이 (Sargassum thunbergii)의 아세톤 및 메탄올 엑스를 EtOAc 및 n-BuOH로 분획한후 각 분획을 SiO$_2$ column, TSK gel(Toyo pearl HW-40F), $\mu$-Bondapak column 및 HPLC등으로 분리 정제하여, 새로운 glyceroglycolipid(GV-5, -6, ST-6) 및 glycerylglycoside(GV-12)를 얻었다. 이렇게 분리된 화합물의 물리화학적 성질, 화학반응 및 분광학적 data를 종합 검토한 결과 GV-5, -6, -12, 및 ST-6은 각각 1,2-diacyl-3-0-($\alpha$-D-galactopyranosyl) glycerol (acyl : palmitate-oleate-arachidonate 4: 1 : 9) (1), 1,2-diacyl -3-0-〔$\alpha$-D-galactopyranosyl -(1 "$\longrightarrow$6')-0-$\beta$-D-galactopyranosyl〕 glycerol (acyl : palmitate-oleate-arachidonate(5:1:4)(3), 2-0-($\alpha$-D-galactopyranosyl) glycerol (5), 및 sodium salt of 1-acyl-3-0-(6'-sulfo-$\alpha$-D-quinovopyranosyl) glycerol(acyl:palmitate-oleate 96:4)(8) 이라는 것이 판명되었다. 그리고 GV-5 및 -6은 마우스 백혈병세포 (L1210)에 대한 세포독성 ($IC_{50}$/ of GV-5, and -6:8.0$\mu\textrm{g}$/ml and 10.8$\mu\textrm{g}$/ml )외에, 사람의 상피암세포에 대한 성장억제효과 [growth inhibitor(%) in 20$\mu\textrm{g}$/m1 :GV-5(39.9%), GV-6(16.7%)를 나타내었으며, 한편, GV-5, GV-6, -12 및 ST-6은 각각 쥐의 F9 기형암종 세포의 분화유도 활성을 나타내어 항종양제로의 개발에 많은 흥미가 기대된다.기대된다.

• Journal of Pharmaceutical Investigation
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• 제36권6호
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• pp.355-361
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• 2006

Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.

• 대한화장품학회지
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• 제25권4호
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• pp.145-154
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• 1999

A novel retinol derivative, polyethoxylated retinamide(Medimin A) was synthesized, as an anti-aging agent. Collagen synthesis, skin permeation, stability, and toxicity of Medimin A were evaluated and compared with those of retinol and retinyl palmitate. In vitro collagen synthesis was evaluated by quantitative assay of $[^3H]-proline$ incorporation into collagenase sensitive protein in fibroblast cultures. For in vitro skin permeation experiments, Franz diffusion cells(effective diffusion area: 1,766 $cm^2$) and the excised skin of female hairless mouse aged 8 weeks were used, The stabilities of retinoids were evaluated at two different temperature($25^{\circ}C\;and\;40^{\circ}C$) and under UV in solubilized state and in O/W emulsion. To estimate the safety, acute oral toxicity, acute dermal toxicity, primary skin irritation, acute eye irritation and human patch test were performed. The effect of Medimin A on collagen synthesis was similar to that of retinol. The skin permeability of Medimin A was higher than those of retinol and retinyl palmitate. The Medimin A was more stable than retinol and retinyl palmitate. Medimin A was nontoxic in various toxicological tests. These results suggest that Medimin A would be a good anti-aging agent for enhancing bioavailability and stability.

• 대한한의학방제학회지
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• 제24권2호
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• pp.100-107
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• 2016

Objectives : The purpose of this study is to evaluate the anti-lipogenic effect of Sobuncheong-eum on non-alcoholic fatty liver disease in free fatty acid induced cellular model. Methods : HepG2 cells were treated with palmitate for 24h to overload intracellular triglyceride (TG) content in the presence or absence of Sobuncheong-eum extract. After palmitate treatment, Intracellular TG content was measured with TG assay kit. Several lipogenesis related markers, including AMP-activated protein kinase (AMPK), sterol regulatory element-binding transcription factor-1c (SREBP-1c), acetyl-CoA carboxylase (ACC), and fatty acid synthase (FAS), were assessed using Western-blot analyses and RT-PCR. Results : Palmitate markedly increased intracellular TG in HepG2 cells, and which were alleviated by coadministered Sobuncheong-eum extract. Sobuncheong-eum extract activated AMPK, which plays a key role in reducing hepatic lipid accumulation, and reduced lipogenic fators, SREBP-1c, ACC, and FAS. Conclusions : Taken together, it is conceivable that Sobuncheong-eum has an potential to alleviate steatosis, and which may be mediated by activating AMPK at least in part.

• Journal of Pharmaceutical Investigation
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• 제31권4호
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• pp.225-232
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• 2001

The present study was carried out to observe the effect of liposome dispersed gel formulation (Lipogel) on topical delivery of ascorbyl palmitate (AsP). Neutral and negatively charged MLV liposomes containing AsP were prepared with dimyristoylphosphadtidylcholine (DMPC) and dicetyl phosphate (DCP), and dispersed to poloxamer gel matrix. In the hydrolysis study in rat's skin homogenates, AsP hydrolyzed to ascorbic acid (AsA) according to the first-order kinetics with the rate constant of $2.46{\times}10^{-2}\;min^{-1}$. In the passive skin penetration study using Franz diffusion cell, lipogel systems exhibited the greater values in the flux $(J_s)$ and the amount penetrated $(Q_p)$ compared to control hydrogels containing diethyleneglycol monoethyl ether $(Transcutol^{\circledR})$ as a solubilizing agent and a penetration enhancer for AsP. The total amount penetrated $(Q_{Total})$, which is expressed as a summation of $Q_P\;and\;Q_L$, for lipogel system was about 1.4 times higher in average than that of control hydrogel. However the amount localized in the skin $(Q_L)$ was similar in both formulations. As a result, lipogel system enhanced the skin penetration of AsP, possibly due to the increase in local concentration of AsP by preferential adsorption of liposome to the skin and the enhancing effect of phospholipid in liposome composition. Moreover it was expected that the penetrated AsP would generate AsA during skin penetration by the skin esterase. In conclusion, lipogel formulation was considered as a good candidate for topical delivery of AsP.

• The Korean Journal of Physiology and Pharmacology
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• 제17권3호
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• pp.197-201
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• 2013

The purpose of this study was to examine the anti-oxidative activity of pectin and other polysaccharides in order to develop a cosmeceutical base having anti-oxidative effects towards retinyl palmitate (RP). The anti-oxidative stabilizing effects of pectin and other polysaccharides on RP were evaluated by DPPH assay and then the stabilizing effect of pectin on RP was examined as a function of time. Among the polysaccharides we examined, pectin exhibited a considerably higher anti-oxidative activity, with an approximately 5-fold greater DPPH radical scavenging effect compared to other polysaccharides. The DPPH radical scavenging effect of pectin increased gradually with increasing concentrations of pectin. At two different RP concentrations, 0.01 and 0.1% in ethanol, addition of pectin improved the stability of RP in a concentration dependent manner. The stabilizing effect of pectin on RP was more effective for the lower concentration of RP (0.01%, v/v). Further, degradation of RP was reduced following the addition of pectin as measured over 8 hours. From the results obtained, it can be suggested that pectin may be a promising ingredient for cosmeceutical bases designed to stabilize RP or other pharmacological agents subject to degradation by oxidation.

• The Korean Journal of Physiology and Pharmacology
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• 제19권1호
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• pp.59-64
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• 2015

Retinyl palmitate (RP)-loaded pectinate micro- and nano-particles (PMP and PNP) were designed for stabilization of RP that is widely used as an anti-wrinkle agent in anti-aging cosmeceuticals. PMP/PNP were prepared with an ionotropic gelation method, and anti-oxidative activity of the particles was measured with a DPPH assay. The stability of RP in the particles along with pectin gel and ethanolic solution was then evaluated. In vitro release and skin permeation studies were performed using Franz diffusion cells. Distribution of RP in each skin tissue (stratum corneum, epidermis, and dermis) was also determined. PMP and PNP could be prepared with mean particle size diameters of $593{\sim}843{\mu}m$ (PMP) and 530 nm (i.e., $0.53{\mu}m$, PNP). Anti-oxidative activity of PNP was greater than PMP due largely to larger surface area available for PNP. The stability of RP in PMP and PNP was similar but much greater than RP in pectin bulk gels and ethanolic solution. PMP and PNP showed the abilities to constantly release RP and it could be permeated across the model artificial membrane and rat whole skin. RP was serially deposited throughout the skin layers. This study implies RP loaded PMP and PNP are expected to be advantageous for improved anti-wrinkle effects.

• Journal of Ginseng Research
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• 제46권3호
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• pp.444-453
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• 2022

Background: Compound K (CK) is among the protopanaxadiol (PPD)-type ginsenoside group, which produces multiple pharmacological effects. Herein, we examined the effects of CK on muscle atrophy under hyperlipidemic conditions along with its pro-myogenic effects. Further, the molecular pathways underlying the effects of CK on skeletal muscle have been justified. Methods: C2C12 myotubes were treated with palmitate and CK. C2C12 myoblasts were differentiated using CK for 4-5 days. For the in vivo experiments, CK was administered to mice fed on a high-fat diet for 8 weeks. The protein expression levels were analyzed using western blotting analysis. Target protein suppression was performed using small interfering (si) RNA transfection. Histological examination was performed using Jenner-Giemsa and H&E staining techniques. Results: CK treatment attenuated ER stress markers, such as eIF2a phosphorylation and CHOP expression and impaired myotube formation in palmitate-treated C2C12 myotubes and skeletal muscle of mice fed on HFD. CK treatment augmented AMPK along with autophagy markers in skeletal muscle cells in vitro and in vivo experiments. AMPK siRNA or 3-MA, an autophagy inhibitor, abrogated the impacts of CK in C2C12 myotubes. CK treatment augmented p38 and Akt phosphorylation, leading to an enhancement of C2C12 myogenesis. However, AMPK siRNA abolished the effects of CK in C2C12 myoblasts. Conclusion: These findings denote that CK prevents lipid-induced skeletal muscle apoptosis via AMPK/autophagy-mediated attenuation of ER stress and induction of myoblast differentiation. Therefore, we may suggest the use of CK as a potential therapeutic approach for treating muscle-wasting conditions associated with obesity.

• 대한조현병학회지
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• 제21권2호
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• pp.74-80
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• 2018

Objectives : This study investigated whether long-acting injectable (LAI) paliperidone is different from its oral form in terms of the effect on cognitive function in schizophrenia spectrum and other psychotic disorders. Methods : We reviewed the medical records of patients in Seoul National University Bundang Hospital who were diagnosed as having schizophrenia and/or other psychotic disorders based on DSM-5 from 2016 to 2017. Seven patients were treated with oral paliperidone and 11 were treated with paliperidone palmitate. All patients underwent clinical and neuropsychological assessment, including the Korean version of the MATRICS Consensus Cognitive Battery (MCCB) at their first visit or within one month of their initial treatment. MCCB was repeated within three to 12 months after the initial assessment. Results : There was no significant difference between the two groups in most cognitive domains including speed of processing, attention and vigilance, working memory, verbal learning, visual learning and reasoning and problem solving domain. However, patients treated with paliperidone palmitate showed better improvement in social cognition domain than those taking oral paliperidone. The standardized values of social cognition domain scores had significantly improved over time in patients under paliperidone palmitate, demonstrating a significant time-by-group interaction. Conclusion : Our results show that long-acting injectable paliperidone could be helpful in some aspects of improving cognitive function in schizophrenia spectrum and other psychotic disorders. Further studies with other antipsychotics are necessary to generalize the results.