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Cytotoxicities and Quantitative Structure Activity Relationships of B13 Sulfonamides in HT-29 and A549 Cells
SeulKiChanLee, SangMinPark, ChaeukIm 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 8 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2011, Vol.15 No.6 14 423-430 (8 pages)
with IC50 values of 27 and 28.7ՌM for HT-29 and A549, respectively. The comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used to carry out QSAR molecular modeling of these compounds. The predictive CoMSIA models for HT-29 and A549 gave cross-validated q2 values of 0.703 and 0.830, respectively. From graphical analysis of these models, we suppose that the stereochemistry of 1,3-propandiol is not important for activity and that... -
The Protective Effect of Quercetin-3-O-β-D-Glucuronopyranoside on Ethanol-induced Damage in Cultured Feline Esophageal Epithelial Cells
JungHyunCho, SunYoungPark, HoSungLee, WanKyunnWhang, UyDongSohn 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 8 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2011, Vol.15 No.6 1 319-326 (8 pages)
Quercetin-3-O-Ղ-D-glucuronopyranoside (QGC) is a flavonoid glucoside extracted from Rumex Aquaticus Herba. We aimed to explore its protective effect against ethanol-induced cell damage and the mechanism involved in the effect in feline esophageal epithelial cells (EEC). Cell viability was tested and 2',7'-dichlorofluorescin diacetate assay was used to detect intracellular H2O2 production. Western blotting analysis was performed to investigate MAPK activation and interleukin 6 (IL-6)... -
Cytotoxic Activity and Structure Activity Relationship of Ceramide Analogues in Caki-2 and HL-60 Cells
YongJinKim, EunAeKim, UyDongSohn, ChulBuYim, ChaeukIm 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2010, Vol.14 No.6 14 441-447 (7 pages)
in the MTT assay. Some compounds (12, 15, and 16) showed stronger cytotoxicity than B13 and C6-ceramide against both tumor cell lines, and compound (12) gave the most potent activity with IC50 values of 36 and 9</SUB>ՌM, respectively. Molecular modeling of thiourea B13 analogues was carried out by comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). We obtained highly reliable and predictive CoMSIA models with cross-validated q2... -
Octyl Gallate Inhibits ATP-induced Intracellular Calcium Increase in PC12 Cells by Inhibiting Multiple Pathways
YujieGuo, YiJaeHong, Hyun-JongJang, Myung-JunKim, Duck-JooRhie, Yang-HyeokJo, SangJuneHahn, ShinHeeYoon 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 8 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2010, Vol.14 No.1 4 21-28 (8 pages)
Phenolic compounds affect intracellular free Ca2＋ concentration ([Ca2＋]i) signaling. The study examined whether the simple phenolic compound octyl gallate affects ATP-induced Ca2＋ signaling in PC12 cells using fura-2-based digital Ca2＋ imaging and whole-cell patch clamping. Treatment with ATP (100</SUP>ՌM) for 90 s induced increases in [Ca2＋]i in PC12 cells. Pretreatment with octyl gallate (100 nM to 20ՌM) for 10 min inhibited the ATP-induced [Ca2＋]i response in a... -
Block of hERG K＋ Channel by Classic Histamine H1 Receptor Antagonist Chlorpheniramine
Hee-KyungHong, Su-HyunJo 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2009, Vol.13 No.3 12 215-220 (6 pages)
Chlorpheniramine is a potent first-generation histamine H1 receptor antagonist that can increase action potential duration and induce QT prolongation in several animal models. Since block of cardiac human ether-a-go-go-related gene (hERG) channels is one of leading causes of acquired long QT syndrome, we investigated the acute effects of chlorpheniramine on hERG channels to determine the electrophysiological basis for its proarrhythmic potential. We examined the effects of chlorpheniramine on... -
Physiological, Pharmacological and Toxicological Implications of Heterodimeric Amino Acid Transporters
YoshikatsuKanaiHitoshiEndou 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 12 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2004, Vol.8 No.3 1 117-128 (12 pages)
may be damaging neurons leading to the exacerbation of brain damage after brain ischemia. Because of broad substrate selectivity, system L transporters such as LAT1 transport amino acid-related compounds including L-Dopa and function as a drug transporter. System L also interacts with some environmental toxins with amino acid-related structure such as cysteine-conjugated methylmercury. Therefore, these transporter would be candidates for drug targets based on new therapeutic strategies. -
Effects of Local Anesthetics on Rotational Mobility of n-(9-Anthroyloxy)stearic Acid in Neuronal Membranes
Hye-OckJang, ChangLee, Min-GakChoi, Sang-HunShin, In-KyoChung, IlYun 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2003, Vol.7 No.3 1 119-124 (6 pages)
To elucidate the molecular mechanism of pharmacological action of local anesthetics, we studied membrane actions of tetracaine, bupivacaine, lidocaine, prilocaine and procaine. Fluorescence polarization of n-(9-anthroyloxy)stearic acid (n-AS) was used to examine the effects of these local anesthetics on differential rotational mobility of different positions of the number of synaptosomal plasma membrane vesicle (SPMV) phospholipid carbon atoms. The four membrane components differed with respect... -
Assessment of Flavin-containing Monooxygenase (FMO) Activity by Determining Urinary Ratio of Theobromine and Caffeine in a Korean Population after Drinking a Cup of Coffee
Woon-GyeChung, , Ju-HeeKang, Hyung-KeunRoh, Kyung-HoonLee, Chang-ShinPark, Young-NamCha, 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 1999, Vol.3 No.2 11 207-213 (7 pages)
To examine individual variation in drug metabolism catalyzed by flavin-containing monooxygenase (FMO), 179 Korean volunteers' urinary molar concentration ratio of theobromine (TB) and caffeine (CA) was determined. Their urine was collected for 1 hr (between 4 and 5 hrs) after they drank a cup of coffee containing 115 mg CA and analyzed by an HPLC system. The lowest TB/CA ratio obtained was 0.40, the highest ratio was 15.17 (38-fold difference), and the median ratio for all subjects was 1.87.... -
Chlorpromazine의 유전적 안전성에 관한 연구
김한규, 손윤희, 이광헌, 윤태호, 남경수 대한신경정신의학회 신경정신의학 9 Pages
대한신경정신의학회 신경정신의학 2000, 제 39권 제 3호 14 629-637 (9 pages)
연구목적： 항 정신성약물로 사용빈도가 높은 chlorpromazine을 사용하여 이 약물의 돌연변이원성과 유전독성을 알 아보았다. 방 법： Bacillus subtilis을 사용한 DNA손상성검토(rec assay), Salmonella typhimurium을 이용한 돌연변이원 성실험(Ames test 및 SOS umu test) 그리고 생쥐에 chlorpromazine를 직접 주입하여 대사 후에 돌연변이 원성을 확인하는 host-mediated assay법을 각각 사용하였다. 결 과： Rec assay에서 chlorpromazine은 Bacillus subtilis의 DNA에는 별다른 영향을 미치지 않았으며, Salmonella typhomurium TA...
