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Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives
Hea-Young, Park,Hee-Kyung, Rhee,Ji Hye, Yoo,Eun Young, Lee,Young Joo, Kwon,Hang-Rhan, Seo,Yun-Sil, Lee 梨花女子大學校 藥學硏究所 2012 藥學硏究論文集 Vol.- No.22
Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (Se, Sk, St. 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against Hela cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the GO/Gl phase by compounds Sk, Sv, Sm. 6c, and 6f in Hela cells. These compounds showed relatively high cytotoxicity in this cell type.
Cyclooxygenase-2 promotes cell proliferation, migration andinvasion in U2OS human osteosarcoma cells
Eun Jeong Lee,최은미,So Ra Kim,Jung Hea Park,Hyunsook Kim,Kwon Soo Ha,Young Myeong Kim,Sung Soo Kim,Myeon Choe,김종일,Jeong A Han 생화학분자생물학회 2007 Experimental and molecular medicine Vol.39 No.4
Osteosarcoma is the most comon primary bone tu-mor, but the pathogenesis is not well understood. While cyclooxygeanse-2 (COX-2) is known to be close-ly associated with tumor growth and metastasis in sev-eral kinds of human tumors, the function of COX-2 in osteosarcoma is unclear. Therefore, to investigate the function of COX-2 in osteosarcoma, we established stable cell lines overexpressing COX-2 in U2OS human osteosarcoma cells. COX-2 overexpression as well as prostaglandin E2 treatment promoted proliferation of U2OS cells. In addition, COX-2 overexpression enhanced mobility and invasiveness of U2OS cells, which was accompanied by increases of matrix metalloproteinase- 2 and -9 (MMP-2 and -9) activities. Selective COX-2 inhibitors, NS-398 and celecoxib, inhibited cell proliferation and abrogated the enhanced mobility, invasiveness and MMP activities induced by COX-2 overexpression. These results suggest that COX-2 is directly associated with cell proliferation, migrationand invasion in human osteosarcoma cells, and the therapeutic value of COX-2 inhibitors should be evaluated continuously.
( Hea Yon Lee ),( Jin Jin Kim ),( Eun Sil Ko ),( Sei Won Kim ),( Sang Haak Lee ),( Hyeon Hui Kang ),( Chan Kwon Park ),( Ki Ouk Min ),( Bae Young Lee ),( Hwa Sik Moon ),( Ji Young Kang ) 대한결핵 및 호흡기학회 2010 Tuberculosis and Respiratory Diseases Vol.69 No.4
We report the case of a 68-year-old man with a stromal tumor of uncertain malignant potential (STUMP), which had metastasized to the lung. The patient complained of an enlarged mass in the anterior chest. Chest computed tomography (CT) showed a sternal abscess with multiple nodules in both lungs. A thoracoscopic lung biopsy of the nodules and incision/drainage of the sternal mass were performed simultaneously. CT of the pelvis revealed an enlarged prostate with irregular cystic lesions in the pelvis. Prostate biopsy was done and demonstrated hypercellular stroma with minimal cytological atypia, a distinct pattern of STUMP. The sternal abscess proved to be tuberculosis and the lung lesion was consistent with STUMP, which had spread from the prostate. However, to our knowledge, the tuberculous abscess might not be assoicated with STUMP in the lung. The patient refused surgical prostatectomy and was discharged with anti-tuberculosis medication. On one-year follow up, the patient had no evidence of disease progression.
Kwon, Oran,Lee, Sunho,Ban, Soonhyun,Im, Jooyeon J.,Lee, Doo Suk,Lee, Eun Hee,Kim, Joohee,Lim, Soo Mee,Lee, Sang Gon,Kang, Ilhyang,Kim, Kyung-Hee,Yoon, Sujung,Lee, Sun Hea The Korean Society of Biological Psychiatry 2015 생물정신의학 Vol.22 No.2
Objectives The combination extract of four kinds of herbs, Gastrodia elata, Liriope platyphylla, Dimocarpus longan, and Salvia miltiorrhiza, has shown to have memory improving effects in mice. The aim of this study was to investigate the efficacy and safety of the herbal mixture for improving working memory as well as microstructural changes in white matter integrity in individuals with subjective memory complaints. Methods Seventy-five individuals with subjective memory complaints were assigned to receive either placebo (n = 15) or herbal mixture (low-dose group, n = 30 and high-dose group, n = 30) supplementation in an 8-week, randomized, double-blind, placebo-controlled clinical trial. Changes in working memory performance and fractional anisotropy (FA) values reflecting white matter integrity from baseline to 8-week endpoint were assessed. Results The herbal mixture group showed an increase in working memory performance compared to the placebo group (p for interaction = 0.001). In addition, the herbal mixture group showed an increase in FA values in the temporo-parietal regions (corrected p < 0.05), which are crucially involved in working memory function and are among the most affected regions in patients with cognitive impairments. Conclusions Findings from this study indicate that the herbal mixture may be a promising therapeutic option for individuals with subjective memory complaints.
Inhibitory Effect of Nicardipine on hERG Channel
( Eun Jung Kim ),( Hea Young Cho ),( Hye Soo Kim ),( Eun Yong Chung ),( Su Hyun Jo ),( Ji Hun Cha ),( Kyoung Jin Kwon ),( Seol Hee Jeon ),( Hye Ju Chung ) 한국응용약물학회 2010 Biomolecules & Therapeutics(구 응용약물학회지) Vol.18 No.4
Drug-induced long QT syndrome is known to be associated with the onset of torsades de pointes (TdP), resulting in a fatal ventricular arrhythmia. QT interval prolongation can result from blocking the human ether-a-go-go-related gene (hERG) channel, which is important for the repolarization of cardiac action potential. Nicardipine, a Ca-channel blocker and antihypertensive agent, has been reported to increase the risk of occasional serious ventricular arrhythmias. We studied the effects of nicardipine on hERG K+ channels expressed in HEK293 cells and Xenopus oocytes. The cardiac electrophysiological effect of nicardipine was also investigated in this study. Our results revealed that nicardipine dose-dependently decreased the tail current of the hERG channel expressed in HEK293 cells with an IC50 of 0.43 μM. On the other hand, nicardipine did not affect hERG channel trafficking. Taken together, nicardipine inhibits the hERG channel by the mechanism of short-term channel blocking. Two S6 domain mutations, Y652A and F656A, partially attenuated (Y652A) or abolished (F656A) the hERG current blockade, suggesting that nicardipine blocks the hERG channel at the pore of the channel.
Dependence Potential of Propofol: Behavioral Pharmacology in Rodents
( Eun Jung Kim ),( Hea Young Cho ),( Eun Yong Chung ),( Hye Joo Chung ),( Jun Yeon Lee ),( Ho Sang Jeong ),( Hye Jin Cha ),( Ji Hun Cha ),( Kyoung-jin Kwon ),( Hye- Soo Kim ) 한국응용약물학회 2012 Biomolecules & Therapeutics(구 응용약물학회지) Vol.20 No.2
Propofol is an anesthetic commonly used to provide sedation or to induce and maintain an anesthetic stated. However, there are reports which indicate propofol may cause psychological dependence or be abused. In the present study, we used various behavioral tests including climbing test, jumping test, conditioned place preference, and self-administration test to assess the dependence potential and abuse liability of propofol compared to a positive control (methamphetamine) or a negative control (saline or intralipid). Among the tests, the conditioned place preference test was conducted with a biased method, and the selfadministration test was performed under a fl xed ratio (FR) 1 schedule, 1 h per session. No difference was found in the climbing test and jumping test, but propofol (30 mg/kg, i.p.) increased the rewarding effect in the conditioned place preference test, and it showed a positive reinforcing effect compared to the vehicle. These results indicate that propofol tends to show psychological dependence rather than physical dependence, and it seems not to be related with dopaminergic system.