• 대한약학회:학술대회논문집
• /
• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
• /
• pp.78-79
• /
• 2001

• Journal of Pharmaceutical Investigation
• /
• 제36권2호
• /
• pp.137-142
• /
• 2006

A bioequivalence of Daewoong $Alendronate^{TM}$ (Daewoong Pharmaceutical Co., Ltd., Korea) and $Fosamax^{TM}$ tablets (MSD Korea) was evaluated according to the guideline of Korea Food and Drug Administration (KFDA). A single 70 mg dose of sodium alendronate of each medicine was administered orally to 56 healthy male volunteers. This study was performed in a $2\;{\time}\;2$ crossover design. Concentrations of alendronate in the urine were monitored by a high-performance liquid chromatography (HPLC). $A_{et}$ (cumulative urinary excreted amount from time 0 to last sampling interval) was calculated by the accumulation of the urinary excreted alendronate. $U_{max}$ (maximum urinary excretion rate) and $T_{max}$ (time to reach $U_{max}$) were compiled from the urinary excretion rate - time data. Analysis of variance was performed using logarithmically transformed $A_{et}$ and $U_{max}$. No significant sequence effect was found for all of the bioavailability parameters. The 90% confidence intervals of the $A_{et}$ and $U_{max}$ for Daewoong $Alendronate^{TM}/Fosamax^{TM}$ were 0.89-1.12 and 0.82-1.02, respectively. This study demonstrated the bioequivalence of Daewoong $Alendronate^{TM}$ and $Fosamax^{TM}$ with respect to the rate and extent of absorption.

• Journal of Pharmaceutical Investigation
• /
• 제41권3호
• /
• pp.147-151
• /
• 2011

This paper demonstrates the development of a method for preparing micropatterned microdiscs in order to increase contact area with cells and to change the release pattern of drugs. The microdiscs were manufactured with hot embossing, where a polyurethane master structure was pressed onto both solid and porous microparticles made of polylactic-co-glycolic acid at various temperatures to form a micropattern on the microdiscs. Flat microdiscs were formed by hot embossing of porous microparticles; the porosity allowed space for flattening of the microdiscs. Three types of micro-grooves were patterned onto the flat microdiscs using prepared micropatterned molds: (1) 10 ${\mu}M$ deep, 5 ${\mu}M$ wide, and spaced 2 ${\mu}M$ apart; (2) 10 ${\mu}M$ deep, 9 ${\mu}M$ wide, and spaced 5 ${\mu}M$ apart; and (3) 10 ${\mu}M$ deep, 50 ${\mu}M$ wide, and spaced 50 ${\mu}M$ apart. This novel microdisc preparation method using hot embossing to create micropatterns on flattened porous microparticles provides the opportunity for low-cost, rapid manufacture of microdiscs that can be used to control cell adhesion and drug delivery rates.

• 대한약침학회지
• /
• 제25권3호
• /
• pp.242-249
• /
• 2022

Objectives: The aim of this work is to evaluate the in vitro antioxidant, hypoglycemic, and antiobesity effects of Euphorbia resinifera extracts and investigate the phenolic constituents and the toxicity of these extracts. Methods: Phytochemical screening was performed to detect polyphenols and flavonoids. Antioxidant activity was evaluated by four methods (DPPH, ABTS, H₂O₂, and xanthine oxidase inhibition). The hypoglycemic effect was determined by the inhibition of α-amylase and α-glucosidase enzymes in vitro and via a starch tolerance study in normal rats. The antiobesity effect was estimated by in vitro inhibition of lipase. Results: Phytochemical screening revealed that the ethanolic extract was rich in polyphenols (99 ± 0.56 mg GEA/g extract) and tannins (55.22 ± 0.17 mg RE/g extract). Moreover, this extract showed higher antioxidant activity in different tests: the DPPH assay (IC₅₀ = 53.81 ± 1.83 ㎍/mL), ABTS assay (111.4 ± 2.64 mg TE/g extract), H₂O₂ (IC₅₀ = 98.15 ± 0.68 ㎍/mL), and xanthine oxidase (IC₅₀ = 10.26 ± 0.6 ㎍/mL). With respect to hypoglycemic effect, the aqueous and ethanolic extracts showed IC₅₀ values of 119.7 ± 2.15 ㎍/mL and 102 ± 3.63 ㎍/mL for α-amylase and 121.4 ± 1.88 and 56.6 ± 1.12 ㎍/mL for α-glucosidase, respectively, and the extracts lowered blood glucose levels in normal starch-loaded rats. Additionally, lipase inhibition was observed with aqueous (IC₅₀ = 25.3 ± 1.53 ㎍/mL) and ethanolic (IC₅₀ = 13.7 ± 3.03 ㎍/mL) extracts. Conclusion: These findings show the antioxidant, hypoglycemic, and hyperlipidemic effects of E. resinifera extracts, which should be investigated further to validate their medicinal uses and their pharmaceutical applications.

• Journal of Pharmaceutical Investigation
• /
• 제34권6호
• /
• pp.505-511
• /
• 2004

A bioequivalence study of $Bestidine^{TM}$ tablets (Choong Wae Pharma. Corp., Korea) to Dong-A $Gaster^{TM}$ (Dong-A Pharmaceutical Co., Ltd., Korea) tablets was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korean volunteers received each medicine at the famotidine dose of 40 mg in a $2{\times}2$ crossover study. There was a one-week wash out period between the doses. Plasma concentrations of famotidine were monitored by a high-performance liquid chromatography for over a period of 12 hours after the administration. $AUC_t$ (the area under the plasma concentration-time curve from time zero to 12 hr) was calculated by the linear trapezoidal rule method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t$ and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the Cmax ratio for $Bestidine^{TM}/Gaster^{TM}$ were log 0.90-log 1.06 and log 0.98-log 1.20, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the bioequivalence of $Bestidine^{TM}$ and $Gaster^{TM}$ with respect to the rate and extent of absorption.

• Fisheries and Aquatic Sciences
• /
• 제17권3호
• /
• pp.275-290
• /
• 2014

The marine ecosystem represents a vast and dynamic array of bio-resources attributed with its huge diversity and considered as potential untapped reservoirs for the development of functional foods for future health markets. Basically, marine microorganisms, sponges, algae, invertebrates such as crustaceans and mollusks along with marine fish species can be considered as marine bio-resources, which can be utilized to obtain different health benefits for humans, directly or after processing. Most of the bio-molecular components, such as lipids and proteins from these marine bio-resources, which can be extracted in large scale using the modern and advanced biotechnological approaches, are suitable drug candidates for the pharmaceutical industry as well as functional food ingredients for the food industry. Moreover, the furtherance of high throughput molecular biological techniques has already been incorporated with identification, mining and extraction of molecular components from marine bio-resources. In this review, potential marine bio-resources with respect to their extractable bio-molecules were described in details, while explaining the present and prospective methods of identification and extraction, which are integrated with advanced techniques in modern biotechnology. In addition, this provides an overview of future trends in marine biotechnology.

• Journal of Microbiology and Biotechnology
• /
• 제9권6호
• /
• pp.839-846
• /
• 1999

An extracellular chitinase-producing bacterial strain induced by colloidal chitin was isolated from sea sand and was identified to be a member of the genus Cytophaga. The chitinase was purified successively by 30-60% ammonium sulfate fractionation, and DEAE-Bio gel A column, Octyl-Sepharose CL-4B column, and DEAE-Bio gel A column chromatographies. The enzyme had a molecular mass of 59.75 kDa, and the amino terminal amino acid sequence was ATPNAPVISW MPTDXXLQNXS. The enzyme acted better on colloidal chitin as a substrate than on chitosan. For colloidal chitin and chitosan (Degree of Acetylation, 15-25%), $K_{cat}$ values were 0.60U/mg and 0.08U/mg, respectively. HPLC analysis of the enzymatic reaction products showed that the chitinase produced mostly N-acetyl-D-glucosarnine and di-N-acetylchitobiose. The optimum temperature and pH for the enzyme were $50^{\circ}C$ and 4.0, respectively. N-Bromosuccinimide and $Hg^{2+}$ inhibited the chitinase activity as much as 90%, and $Sb^{3+}$, diethylpyrocarbonate, and $Ag^{+}$ inhibited it by 50-70%.

• 생명과학회지
• /
• 제20권12호
• /
• pp.1807-1811
• /
• 2010

갈조류에서 에스트로겐 활성소재를 평가하기 위하여 in vitro 검출시스템을 사용하여 에스트로겐 효과를 가지는 분획을 검증하였다. 각각의 갈조류의 분획물들은 에탄올 추출로부터 물, 헥산, 부탄올 그리고 메탄올의 용매를 이용한 분획과정을 통해 제조하였다. 갈조류들의 수층 분획물에서 가장 높은 에스트로겐 활성을 보였다. 미역과 다시마의 수층 분획물들은 $500\;{\mu}g/ml$의 농도에서 $10^{-7}\;M$의 표준물질($17{\beta}$-estradiol)과 비슷한 활성을 보였으며, 곰피와 돌자반의 수층 분획물들은 $500\;{\mu}g/ml$의 농도에서 $10^{-8}\;M$의 표준물질보다 높은 활성을 보였다. 이 연구의 결과로 갈조류인 미역, 다시마, 곰피 및 돌자반의 수층 분획물에 에스트로겐 대체 작용을 할 수 있는 성분이 포함되어 있는 것을 확인하였으며, 이를 이용하여 폐경기 장애를 예방할 수 있는 에스트로겐 활성소재의 개발이 가능할 것으로 기대된다.

• 대한화장품학회지
• /
• 제49권1호
• /
• pp.59-65
• /
• 2023

사이자이지움 클래비플로룸(Syzygium claviflorum (Roxb.) Wall. ex A.M. Cowan & Cowan, S. claviflorum)의 추출물 (잎, 줄기, 열매, 꽃)의 화장품 소재로써 활용되기 위한 생리활성 능력을 검증하였다. 첫번째로, S. claviflorum 추출물은 DPPH와 ABTS assay법을 이용한 항산화 실험에서 다양한 농도로 처리한 결과, 약 80% 이상의 자유 라디칼을 제거하였다. 사람 피부 표피 각질형성세포(human epidermal keratinocytes)를 이용한 세포독성 실험에서는 S. claviflorum 추출물은 낮은 세포독성을 보였다. 또한, S. claviflorum 추출물은 각질형성세포의 분화인자 (keratin (KRT)1, KRT2, KRT9, KRT10)와 피부장벽의 기능 유지에 중요한 involucrin (IVL), loricrin (LOR), filaggrin (FLG)과 claudin1 (CLDN1) 유전자의 발현을 현저히 증가시켰다. 특히, in vitro 아토피 피부염 실험에서 interleukin (IL)-4/IL-13에 의해 억제된 FLG 단백질 발현이 S. claviflorum 추출물에 의해 회복되었다. 따라서, 뛰어난 항산화 효능과 피부장벽 개선 기능을 보유한 S. claviflorum 추출물은 향후 아토피 피부염 치료제 및 화장품 개발에 유용한 소재가 될 것이다.

• The Korean Journal of Physiology and Pharmacology
• /
• 제26권5호
• /
• pp.367-375
• /
• 2022

Gastric cancer stem cells (GCSCs) are a major cause of radioresistance and chemoresistance in gastric cancer (GC). Therefore, targeting GCSCs is regarded as a powerful strategy for the effective treatment of GC. Atorvastatin is a widely prescribed cholesterol-lowering drug that inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase, a rate-limiting enzyme in the mevalonate pathway. The anticancer activity of atorvastatin, a repurposed drug, is being investigated; however, its therapeutic effect and molecular mechanism of action against GCSCs remain unknown. In this study, we evaluated the anticancer effects of atorvastatin on MKN45-derived GCSCs. Atorvastatin significantly inhibited the proliferative and tumorsphere-forming abilities of MKN45 GCSCs in a mevalonate pathway-independent manner. Atorvastatin induced cell cycle arrest at the G0/G1 phase and promoted apoptosis by activating the caspase cascade. Furthermore, atorvastatin exerted an antiproliferative effect against MKN45 GCSCs by inhibiting the expression of cancer stemness markers, such as CD133, CD44, integrin α6, aldehyde dehydrogenase 1A1, Oct4, Sox2, and Nanog, through the downregulation of β-catenin, signal transducer and activator of transcription 3, and protein kinase B activities. Additionally, the combined treatment of atorvastatin and sorafenib, a multi-kinase targeted anticancer drug, synergistically suppressed not only the proliferation and tumorsphere formation of MKN45 GCSCs but also the in vivo tumor growth in a chick chorioallantoic membrane model implanted with MKN45 GCSCs. These findings suggest that atorvastatin can therapeutically eliminate GCSCs.