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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)
B13 analogues are being considered as therapeutic agents for cancer cells, since B13 is a ceramide analogue and inhibits ceramidase to promote apoptosis in cancer cells. B13 sulfonamides are assumed to have biological activity similar to B13, since they are made by bioisosterically substituting the carboxyl moiety of B13 with sulfone group. Twenty B13 sulfonamides were evaluated for their in vitro cytotoxicities against human colon cancer HT-29 and lung cancer A549 cell lines using MTT assays.... -
Myoplasmic [Ca2＋], Crossbridge Phosphorylation and Latch in Rabbit Bladder Smooth Muscle
Young-DonKim, Min-HyungCho, Seong-ChunKwon 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2011, Vol.15 No.3 8 171-177 (7 pages)
Tonic smooth muscle exhibit the latch phenomenon: high force at low myosin regulatory light chains (MRLC) phosphorylation, shortening velocity (Vo), and energy consumption. However, the kinetics of MRLC phosphorylation and cellular activation in phasic smooth muscle are unknown. The present study was to determine whether Ca2＋-stimulated MRLC phosphorylation could suffice to explain the agonist- or high K＋-induced contraction in a fast, phasic smooth muscle. We measured myoplasmic [Ca2＋], MRLC... -
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)
B13, a ceramide analogue, is a ceramidase inhibitor and induces apoptosis to give potent anticancer activity. A series of thiourea B13 analogues was evaluated for their in vitro cytotoxic activities against human renal cancer Caki-2 and leukemic cancer HL-60 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,... -
Characterization of ETB Receptor-mediated Relaxation in Precontracted Mesenteric Artery from Streptozotocin-induced Diabetic Rats
YangKiEom, KoanHoiKim, ByungYongRhim 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 9 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2005, Vol.9 No.5 8 305-313 (9 pages)
Diabetes mellitus is associated with vascular complications, including an impairment of vascular function and alterations in the reactivity of blood vessels to vasoactive substances in various vasculature. In the present study, the authors have observed endothelin-B (ETB) receptor agonist-induced relaxation in precontracted mesenteric arterial segments from streptozotocin (STZ)-induced diabetic rats, which was not shown from control rats or in other arterial segments from diabetic rats.... -
Expression of Nitric Oxide Synthase and Endothelin-1 in Human Uterine Artery from Full-Term Pregnancies
Ook-HwanChoi, SunHeeLee, EunJinKim, KoanHoiKim, ByungYongRhim 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 8 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2005, Vol.9 No.3 6 165-172 (8 pages)
The aim of this study was to determine the roles of ET-1 and NO on uterine blood flow in pregnancy. Uterine arteries were isolated from 17 nonpregnant and 12 pregnant women. Nonpregnant group included patients with median age of 48.6⁑2.3 years who underwent hysterectomy, because of myoma. Pregnant group included patients with median age of 31.3⁑1.4 years undergoing cesarean delivery. ET-1 and ET-2 induced concentration-dependent contraction in isolated nonpregnant and pregnant... -
Cooperation of Gβ and Gαq Protein in Contractile Response of Cat Lower Esophageal Sphincter (LES)
UyDongSohnTaiSangLee 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2003, Vol.7 No.6 9 349-355 (7 pages)
We previously shown that LES contraction depends on M3 receptors linked to PTX insensitive Gq protein and activation of PLC. This results in production of IP3, which mediates calcium release, and contraction through a CaM dependent pathway. In the esophagus ACh activates M2 receptors linked to PTX sensitive Gi3 protein, resulting in activation of PLD, presumably, production of DAG. We investigated the role of PLC isozymes which can be activated by Gq or Gβ protein on ACh-induced contraction in... -
The Substates with Mutants That Negatively Charged Aspartate in Position 172 Was Replaced with Positive Charge in Murine Inward Rectifier Potassium Channel (Murine Kir2.1)
ISo, I.Ashmole, P.R.Stanfield 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2003, Vol.7 No.5 4 267-273 (7 pages)
the side chain or pKa with mutants (D172H, D172K and D172R), the more frequent the transitions between the fully open state and substate within an opening. The conductance of the substate also depended upon the pKa or the size of the side chain. The relative occupancy at substate SLC with monomer D172K (0.50) was less than that in K-H dimer (0.83). However, the relative occupancy at substate with D172R (0.79) was similar to that with R-N dimer (0.82). In the contrary to ROMK1, positive charge as... -
THI 52 Inhibits Inducible Nitric Oxide Synthase Gene Expression in RAW 264.7 Cells and Rat Lung Tissue by Lipopolysaccharide
BogKyuLee, MinKyuPark, HanGeukSeo, HyeSookYun-Choi, DuckHyungLee, KiChurlChang 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2001, Vol.5 No.5 10 443-449 (7 pages)
Previously we reported that THI 52 inhibits tumor necrosis factor (TNF)-α mRNA expression in mouse peritoneal macrophages exposed to LPS plus IFN-γ. In the present study, the effects of THI 52 on vascular reactivity ex vivo, and iNOS protein expression (rat lung) were investigated in LPS-treated rats. Treatment of THI 52 concentration-dependently reduced not only serum nitrite production but also the expression of iNOS protein in rat lung tissues. Thoracic aorta taken from LPS injected rat... -
Effect of Ethanol on Na+-Pi Uptake in Opossum Kidney Cells Role of Membrane Fluidization and Reactive Oxygen Species
InHoPark, MoonYoungHwang, JaeSukWoo, JinSupJung, YongKeunKim 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 10 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 1999, Vol.3 No.5 10 529-538 (10 pages)
a change in Vmax of Na-Pi uptake. Inhibitory effect of n-alcohols on Na-Pi uptake was dependent on the length of the hydrocarbon chain, and it resulted from the binding of one molecule of alcohol, as indicated by the Hill coefficient (n) of 0.8-1.04. Catalase significantly prevented the inhibition, but superoxide dismutase and hydroxyl radical scavengers did not alter the ethanol effect. A potent antioxidant DPPD and iron chelators did not prevent the inhibition. Pyrazole, an... -
Increased Activity of Large Conductance Ca2+-Activated K+ Channels in Negatively-Charged Lipid Membranes
JinBongParkPanDongRyu 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 11 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 1998, Vol.2 No.4 15 529-539 (11 pages)
The effects of membrane surface charge originated from lipid head groups on ion channels were tested by analyzing the activity of single large conductance Ca2-activated K (maxi K) channel from rat skeletal muscle. The conductances and open-state probability (Po) of single maxi K channels were compared in three types of planar lipid bilayers formed from a neutral phosphatidylethanolamine (PE) or two negatively-charged phospholipids, phosphatidylserine (PS) and phosphatidylinositol...
