• Korean Journal of Clinical Pharmacy
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• v.15 no.2
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• pp.160-164
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• 2005

수마트립탄은 뇌혈관에 분포되어 있는 5-HT1B/1D수용체에 특이적이고 선택적으로 작용하여 뇌혈관 수축 작용을 나타내어 편두통의 치료에 널리 쓰이는 약물이다. 본 연구는 수마트립탄 제제인 이미그란(50 mg tablet, GSK사)을 대조약으로 하여 시험약인 명인 제약의 수마트란 50mg정의 생물학적 동등성 평가를 하기 위해 22명의 건강한 지원자를 모집하였다. 지원자를 두 군으로 나누어 1정씩 투여하였고 $2{\times}2$ 교차시험을 실시하였다. 수마트립탄의 혈장 중의 농도를 정량하기 위하여 발리데이션된 HPLC/FD를 사용하였다. 채혈 시간은 투약 전 및 투약 후 0.5, 1, 1.5, 2, 2.5, 3,4, 5, 7, 9, 12시간에 걸쳐 총 12시점에 걸쳐 시행하였다. 생물학적 동등성을 판정하기 위한 파라미터로 12시간까지의 혈장 중 농도 곡선 하 면적$(AUC_{12hr})$ 최고 혈중 농도$(C_{max})$를 사용하였다. $AUC_{12hr}$의 평균은 $137.87ng{\cdot}ml/hr$(시험약)과 $130.12ng{\cdot}ml/hr$(대조약)으로 나타났다. $C_{max}$의 경우 각 각 29.30 ng/ml(시험약)과 29.25ng/m1(대조약)으로 관찰되었다. $AUC_{12hr}$의 경우 로그변환 한 평균치 차의 90% 신뢰구간이 log0.95-log1.24이었고, $C_{max}$의 경우 log0.90-log1.149로 계산되 어 두 항목 모두 log0.8-log1.25이어야 한다는 식품의 약품 안전청 과 FDA의 기준을 모두 만족시켰다. 이상의 결과를 종합하면 시험약 수마트란 정 50 mg은 대조약 이미그란 정 50 mg에 대하여 생물학적으로 동등한 것으로 판정되었다.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.10
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• pp.5131-5136
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• 2012

Cancer is one of the major health problems worldwide and its current treatments have a number of undesired adverse side effects. Natural compounds may reduce these. Currently, a few plant products are being used to treat cancer. In this study, goniothalamin, a natural occurring styryl-lactone extracted from Goniothalamus macrophyllus, was investigated for cytotoxic properties against cervical cancer (HeLa), breast carcinoma (MCF-7) and colon cancer (HT29) cells as well as normal mouse fibroblast (3T3) using MTT assay. Fluorescence microscopy showed that GTN is able to induce apoptosis in HeLa cells in a time dependent manner. Flow cytometry further revealed HeLa cells treated with GTN to be arrested in the S phase. Phosphatidyl serine properties present during apoptosis enable early detection of the apoptosis in the cells. Using annexin V/PI double staining it could be shown that GTN induces early apoptosis on HeLa cells after 24, 48 and 72 h. It could be concluded that goniothalamin showing a promising cytotoxicity effect against several cancer cell lines including cervical cancer cells (HeLa) with apoptosis as the mode of cell death induced on HeLa cells by Goniothalamin was.

• Proceedings of the Korean Vacuum Society Conference
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• 2014.02a
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• pp.343-343
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• 2014

We reported on the electrical, optical, structural and morphological properties fabricated by co-sputtering for use as an anode for organic solar cells (OSCs). By adjusting RF and DC power of $MoO_3$ and IZO targets during co-sputtering, we fabricated the $MoO_3$-IZO electrode with graded content of the $MoO_3$ on the IZO films. At optimized $MoO_3$ thickness of 20 nm, the $MoO_3$ graded IZO electrode showed a higher mobility ($33cm^2/V-Sec$) than directly deposited $MoO_3$ on IZO film ($26cm^2/V-Sec$). At visible range (400nm~800nm), optical transmittance of the $MoO_3$ graded IZO electrode is higher than that of directly deposited $MoO_3$ on IZO film. High mobility of $MoO_3$ graded on IZO is attributed to less interface scattering between $MoO_3$ and IZO. To investigate the feasibility of $MoO_3$ graded IZO films, we fabricated conventional P3HT:PCBM based OSCs with $MoO_3$ graded IZO as a function of MoO3 thickness. The OSC fabricated on the $MoO_3$ graded IZO anode showed a fill factor of 66.53%, a short circuit current of $8.121mA/cm^2$, an open circuit voltage of 0.592 V, and a power conversion efficiency of 3.2% comparable to OSC fabricated on ITO anode and higher than directly deposited $MoO_3$ on IZO film. We suggested possible mechanism to explain the high performance of OSCs with a $MoO_3$ graded IZO.

• Proceedings of the Korean Vacuum Society Conference
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• 2014.02a
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• pp.257.1-257.1
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• 2014

We investigated characteristics of ITO/Ag-Pd-Cu (APC)/ITO multilayer electrodes prepared by direct current magnetron sputtering for use as an anode in organic solar cells (OSCs). To optimize electrical properties of ITO/APC/ITO multilayer, we fabricated the ITO/APC/ITO multilayer at a fixed ITO thickness of 30 nm as a function of APC thickness. Compare to the surface of Ag layer on ITO, the APC had a smooth surface morphology. At optimized APC thickness of 12 nm, the ITO/APC/ITO multilayer exhibited a sheet resistance of $6{\Omega}/square$ and optical transmittance of 84.15% at a wavelength of 550 nm which is comparable to conventional ITO/Ag/ITO multilayer. However, the APC-based ITO multilayer showed a higher average transmittance in a visible region than the Ag-based ITO multilayer. The higher average transmittance of ITO/APC/ITO multilayer indicated the multilayer is suitable anode for organic solar cells with P3HT:PCBM active layer. OSCs fabricated on the optimized ITO/ACP/ITO multilayer exhibited a better performance with a fill factor of 64.815%, a short circuit current of $8.107mA/cm^2$, an open circuit voltage of 0.59 V, and power conversion efficiency (3.101%) than OSC with ITO/Ag/ITO multilayer (2.8%).

• Fisheries and Aquatic Sciences
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• v.21 no.6
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• pp.16.1-16.7
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• 2018

Background: Matrix metalloproteinases (MMPs) are linked with several complications such as metastasis of cancer progression, oxidative stress, and hepatic fibrosis. Brown seaweeds are being extensively studied for their bioactive molecule content against cancer progression. In this context, Sargassum horneri was reported to possess various bioactivities including antiviral, antimicrobial, and anti-inflammatory partly due to its phenolic compound content. Methods: In this study, potential of S. horneri was evaluated through anti-MMP effect in HT1080 fibrosarcoma cells. S. horneri crude extract was fractionated with organic solvents, namely, water ($H_2O$), n-buthanol (n-BuOH), 85% aqueous methanol (85% aq. MeOH), and n-hexane. The non-toxicity of fraction samples (Sargassum horneri solvent-partitioned extracts (SHEs)) was confirmed by cell-viability assay. SHEs were tested for their ability to inhibit MMP enzymatic activity through gelatin digestion evaluation and cell migration assay. Expressions of MMP-2 and MMP-9 and tissue inhibitors of MMP (TIMPs) were evaluated by reverse transcription and Western blotting. Results: All fractions inhibited the enzymatic activities of MMP-2 and MMP-9 according to gelatin zymography. Except $H_2O$ fraction, fractions hindered the cell migration significantly. All tested fractions suppressed both mRNA and protein levels of MMP-2, MMP-9, TIMP-1, and TIMP-2. Conclusion: Overall, current results suggested that S. horneri has potential to be a good source for anti-MMP agents, and further investigations are underway for better understanding of the action mechanism and isolation and elucidation of the bioactive molecules.

• The Journal of Korean Physical Therapy
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• v.14 no.4
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• pp.454-474
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• 2002

Vasoactive intestinal peptide (VIP) is a very potent dilatator and a nonadrenergic, noncholinergic (NANC) neurotransmitter or neuromodulator in the peripheral and the central nervous systems. The mechanisms of action of VIP were examined in aortic circular and in uterine longitudinal smooth muscle strips of the rat. The effects of sympathetic neurotransmitter were investigated in gastric and aortic circular muscle strips of the mouse and the rat. The effects of silver spike point, SSP, low frequency electrical stimulations of VIP, sympathetic neurotransmitter and $\beta$-endorphin were examined in plasma, serum and 24h urine from the healthy volunteer. In gastric smooth muscle strips from the mouse, adrenergic neurotransmitter norepinephrine was inhibitory effected, followed by caused phasic and tonic contraction to the, muscrine receptor agonist carbachol and acetylcholine, respectively. In urine from the healthy volunteer, both norepinephrine and epinephrine were significantly decreased in continue type and low frequency (3 Hz) of SSP electrical stimulations. The contractile responses to S-HT in uterine longitudinal smooth muscle strips of the rats were completely decreased by a VIP 1 $\mu$M. The contractile responses to PGF2$\alpha$ were not decreased by a VIP. In plasma and serum from the healthy volunteer, both VIP and $\beta$-endorphin were significantly increased in continue type and low frequency (3 Hz) of SSP electrical stimulations. Therefore, this study demonstrate that VIP has the capacity to relax vascular or gastric smooth muscles in part by stimulating the generation of NO, and silver spike point low frequency electrical stimulation has the capacity both to decrease sympathetic neurotransmitters and to increase VIP, $\beta$-endorphin.

• Biomolecules & Therapeutics
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• v.20 no.5
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• pp.470-476
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• 2012

Resveratrol, a chemopreventive agent, is rapidly metabolized in the intestine and liver via glucuronidation. Thus, the pharmacokinetics of resveratrol limits its efficacy. To improve efficacy, the activity of resveratrol was investigated in the context of sphingolipid metabolism in human gastric cancer cells. Diverse sphingolipid metabolites, including dihydroceramides (DHCer), were tested for their ability to induce resveratrol cytotoxicity. Exposure to resveratrol ($100{\mu}M$) for 24 hr induced cell death and cell cycle arrest in gastric cancer cells. Exposure to the combination of resveratrol and dimethylsphingosine (DMS) increased cytotoxicity, demonstrating that sphingolipid metabolites intensify resveratrol activity. Specifically, DHCer accumulated in a resveratrol concentration-dependent manner in SNU-1 and HT-29 cells, but not in SNU-668 cells. LC-MS/MS analysis showed that specific DHCer species containing C24:0, C16:0, C24:1, and C22:0 fatty acids chain were increased by up to 30-fold by resveratrol, indicating that resveratrol may partially inhibit DHCer desaturase. Indeed, resveratrol mildly inhibited DHCer desaturase activity compared to the specific inhibitor GT-11 or to retinamide (4-HPR); however, in SNU-1 cells resveratrol alone exhibited a typical cell cycle arrest pattern, which GT-11 did not alter, indicating that inhibition of DHCer desaturase is not essential to the cytotoxicity induced by the combination of resveratrol and sphingolipid metabolites. Resveratrol-induced p53 expression strongly correlated with the enhancement of cytotoxicity observed upon combination of resveratrol with DMS or 4-HPR. Taken together, these results show that DHCer accumulation is a novel lipid biomarker of resveratrol-induced cytotoxicity in human gastric cancer cells.

• Journal of Life Science
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• v.14 no.1
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• pp.26-31
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• 2004

Redox factor-1 (Ref-1), known as a redox regulator, controls the DNA binding of AP-1 and is activated in HT29 colon cancer cells by hypoxia in vitro. REF-1 also increases tile DNA binding affinity of Hypoxia-inducible Factor-lalpha$ (HIF-lalpha$), HIF-like Factor (HLF) and early growth response-1 (Egr-1) which induce expression of the genes involved in angiogenesis, so that we speculate that REF-1 may play a role in hypoxia-induced angiogenesis. In this research we tried to detect novel proteins interacting with REF-1 using Yeast two-hybrid system using full-length REF-1 cDNA as bait. As result of such screening we detected 3 positive clones. DNA sequencing and GeneBank search revealed that one of the clones contained the same sequences as M.musculus cDNA for tioredoxin.

• Food Science of Animal Resources
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• v.38 no.3
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• pp.554-569
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• 2018

This study aimed to investigate the physiological characteristics and anti-obesity effects of Lactobacillus plantarum K10. The ${\alpha}-amylase$ inhibitory activity, ${\alpha}-glucosidase$ inhibitory activity, and lipase inhibitory activity of L. plantarum K10 was $94.66{\pm}4.34%$, $99.78{\pm}0.12%$, and $87.40{\pm}1.41%$, respectively. Moreover, the strain inhibited the adipocyte differentiation of 3T3-L1 cells ($32.61{\pm}8.32%$) at a concentration of $100{\mu}g/mL$. In order to determine its potential for use as a probiotic, we investigated the physiological characteristics of L. plantarum K10. L. plantarum K10 was resistant to gentamycin, kanamycin, streptomycin, ampicillin, ciprofloxacin, tetracycline, vancomycin, and chloramphenicol. It also showed higher Leucine arylamidase, Valine arylamidase, and ${\beta}-galactosidase$ activities. Moreover, it was comparatively tolerant to bile juice and acid, exhibiting resistance to Escherichia coli, Salmonella Typhimurium, Listeria monocytogenes, and Staphylococcus aureus with rates of 90.71%, 11.86%, 14.19%, and 23.08%, respectively. The strain did not produce biogenic amines and showed higher adhesion to HT-29 cells compared to L. rhamnosus GG. As a result of the animal study, L. plantarum K10 showed significantly lower body weight compared to the high-fat diet group. The administration of L. plantarum K10 resulted in a reduction of subcutaneous fat mass and mesenteric fat mass compared to the high-fat diet (HFD) group. L. plantarum K10 also showed improvement in gut permeability compared to the HFD positive control group. These results demonstrate that L. plantarum K10 has potential as a probiotic with anti-obesity effects.

• Korean Journal of Plant Resources
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• v.29 no.3
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• pp.297-304
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• 2016

The seed of safflower (Carthamus tinctorius L) has been reported to suppress human cancer cell proliferation. However, the mechanisms by which safflower seed inhibits cancer cell proliferation have remained nuclear. In this study, the inhibitory effect of the safflower seed (SS) on the proliferation of human colorectal cancer cells and the potential mechanism of action were examined. SS inhibited markedly the proliferation of human colorectal cancer cells (HCT116, SW480, LoVo and HT-29). In addition, SS suppressed the proliferation of human breast cancer cells (MDA-MB-231 and MCF-7). SS treatment decreased cyclin D1 protein level in human colorectal cancer cells and breast cancer cells. But, SS-mediated downregulated mRNA level of cyclin D1 was not observed. Inhibition of proteasomal degradation by MG132 attenuated cyclin D1 downregulation by SS and the half-life of cyclin D1 was decreased in SS-treated cells. In addition, SS increased cyclin D1 phosphorylation at threonine-286 and a point mutation of threonine-286 to alanine attenuated SS-mediated cyclin D1 degradation. Inhibition of ERK1/2 by PD98059 suppressed cyclin D1 phosphorylation and downregulation of cyclin D1 by SS. In conclusion, SS has anti-proliferative activity by inducing cyclin D1 proteasomal degradation through ERK1/2-dependent threonine-286 phosphorylation of cyclin D1. These findings suggest that possibly its extract could be used for treating colorectal cancer.