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반코마이신 내성 장구균 감염에 대한 quinupristin-dalfopristin 치료 경험
추은주,최상호,조영환,정선미,김백남,김남중,김미나,김양수,우준희,류지소 대한화학요법학회 2002 대한화학요법학회지 Vol.20 No.1
VRE 감염이 중환자에서 급속히 증가하고 있으나 이에 대한 확실한 치료제가 없어 새로운 항생제에 대한 활발한 연구가 있는데 그 중 하나가 quinupristin/dalfopristin이고, 저자들은 중증 환자들의 VRE 감염에 대해 quinupristin/dalfopristin를 투여하여 치료한 임상적 경험을 하였기에 문헌고찰과 함께 보고하는 바이다. Vancomycin-resistant enterococci (VRE) was first recognized in 1992 in Korea. VRE infection have been increasingly reported in immunosuppressed patients over the past decade and have become one of major nosocomial pathogens. Clinicians carings for patients with VRE infections face severe constraints in the selection of treatment. Quinupristin/dalfopristin is active in vitro againt vancomycin-resistant E. faecium (VREF), with a MIC_(90) of 1.0㎍/mL. We studied the clinical efficacy and safety of this agent in the treatment of VREF infection. Patients were included if they had signs and symptoms of active infection including bacteremia, intra-abdominal infection, and wound infection. A total of 13 patients with VREF infection were enrolled. A favorable clinical response (cure or improvement) occured in 10 of 11 evaluable patients. The only adverse events related to quinupristin/dalfopristin were arthralgia and myalgia, which occurred in 2 of 13 patients. These results suggest that quinupristin/dalfopristin is effective and safe as treatment for VREF infections in critically ill patients with serious underlying conditions.
Anticancer Activity of Asparagus cochinchinensis Extract and Fractions in HepG2 Cells
( Mi Kyung Park ),( Myeong Sook Cheon ),( Seong Hwan Kim ),( Jin Mi Chun ),( A Yeong Lee ),( Byeong Cheol Moon ),( Tae Sook Yoon ),( Byung Kil Choo ),( Ho Kyoung Kim ) 한국응용생명화학회 2011 Applied Biological Chemistry (Appl Biol Chem) Vol.54 No.2
Asparagus cochinchinensis Merrill (Liliaceae) has been traditionally used for the treatment of cancer in Korea and China, but its anticancer activity and underlying mechanism remain to be defined. Anticancer activities were investigated on fractions obtained from A. cochinchinensis 70% ethanol extract (ACE-EtOH) in human hepatocellular carcinoma HepG2 cells. Ethylacetate fraction from A. cochinchinensis extract (ACE-EA), more effective than other fractions, induced apoptosis of HepG2 (IC50=72.33±0.34 μg/mL), as revealed by apoptotic feature observation, increased capase-3 activity and Poly ADP ribose polymerase cleavage, and decreased expression of X-linked inhibitor of apoptosis protein in a dose-dependent manner. Protein levels of autophagy-related molecules, microtubule-associated protein 1 light chain 3 α and beclin 1, appeared to be induced by ACE-EA, suggesting ACE-EA exhibits anti-cancer activity with induction via both apoptosis and autophagy signaling pathways in HepG2 cells.
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors
Kim, Mi Kyoung,Shin, Heerim,Park, Kwang-su,Kim, Hyungmi,Park, Jiseon,Kim, Kangjeon,Nam, Joonwoo,Choo, Hyunah,Chong, Youhoon American Chemical Society 2015 Journal of medicinal chemistry Vol.58 No.18
<P>The Janus kinase (JAK) family comprises four members (JAK1, JAK2, JAK3, and Tyk2) that play a key role in mediating cytokine receptor signaling. JAK inhibition thus modulates cytokine-mediated effects. In particular, selective inhibition of JAK1 or JAK3 may provide an efficient therapeutic agent for the treatment of inflammatory diseases, with minimized side effects. In this study, as part of our continued efforts to develop a selective JAK1 inhibitor, a series of 1,2-disubstituted benzimidazole-5-carboxamide derivatives was prepared and their inhibitory activities against all four JAK isozymes were evaluated. A clear structure–activity relationship was observed with respect to JAK1 selectivity; this highlighted the importance of hydrogen bond donors at both <I>N</I><SUP>1</SUP> and R<SUB>2</SUB> positions located within a specific distance from the benzimidazole core. One of the synthesized compounds, 1-(2-aminoethyl)-2-(piperidin-4-yl)-1<I>H</I>-benzo[<I>d</I>]imidazole-5-carboxamide (<B>5c</B>), showed remarkable JAK1 selectivity (63-fold vs JAK2, 25-fold vs JAK3, and 74-fold vs Tyk2). Molecular docking revealed that the 2-aminoethyl and piperidin-4-yl substituents of <B>5c</B> function as probes to differentiate the ATP-binding site of JAK1 from that of JAK2, resulting in preferential JAK1 binding. A kinase panel assay confirmed the JAK1 selectivity of <B>5c</B>, which showed no appreciable inhibitory activity against 26 other protein kinases at 10 μM.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2015/jmcmar.2015.58.issue-18/acs.jmedchem.5b01263/production/images/medium/jm-2015-012639_0008.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm5b01263'>ACS Electronic Supporting Info</A></P>
Kim, Mi Kyoung,Kim, Yunyoung,Choo, Hyunah,Chong, Youhoon Elsevier 2017 Bioorganic & medicinal chemistry Vol.25 No.3
<P><B>Abstract</B></P> <P>Previously, we have reported remarkable effect of a quercetin-glutamic acid conjugate to reverse multidrug resistance (MDR) of cancer cells to a broad spectrum of anticancer agents through inhibition of P-glycoprotein (Pgp)-mediated drug efflux. Due to the hydrolysable nature, MDR-reversal activity of the quercetin conjugate was attributed to its hydrolysis product, quercetin. However, several lines of evidence demonstrated that the intact quercetin-glutamic acid conjugate has stronger MDR-reversal activity than quercetin. In order to evaluate this hypothesis and to identify a novel scaffold for MDR-reversal agents, we prepared quercetin conjugates with a glutamic acid attached at the 7-<I>O</I> position via a non-hydrolysable linker. Pgp inhibition assay, Pgp ATPase assay, and MDR-reversal activity assay were performed, and the non-hydrolysable quercetin conjugates showed significantly higher activities compared with those of quercetin. Unfortunately, the quercetin conjugates were not as effective as verapamil in Pgp-inhibition and thereby reversing MDR, but it is worth to note that the structurally modified quercetin conjugates with a non-cleavable linker showed significantly improved MDR-reversal activity compared with quercetin. Taken together, the quercetin conjugates with appropriate structural modifications were shown to have a potential to serve as a scaffold for the design of novel MDR-reversal agents.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
미추마취시 첨가한 Fentanyl 혹은 Clonidine 이 술후 진통과 요정체에 미치는 영향
김태환,김미운,안승원,김웅,추동훈,김형태 대한마취과학회 2001 Korean Journal of Anesthesiology Vol.40 No.5
Background: Caudal administration of local anesthetics, opioids, and the a2 adrenergic agonists is effective for postoperative pain. Intrathecal and epidural opioids may commonly result in urinary retention. The purpose of this study was to evaluate the effects of fentanyl or clonidine on postoperative analgesia and urinary retention. MethodsL: Forty patients undergoing a hemorrhoidectomy were randomly assigned to receive 20ml of 2% lidocaine and 1:200,000 epinephrine plus clonidine 100 ㎍(group C100,n=10), clonidine 150 ㎍(group C150,n=10), fentanyl 50 ㎍(group F50,n=10), or fentanyl 100 ㎍(group F100,n=10) for caudal anesthesia. Mean arterial pressure (MAP) and heart rate (HR) were measured before anesthesia and immediately postanesthesia, and every 5 min after caudal administration for 30 min. The following variables were recorded; onset time, analgesic time, voiding time, and urinary retention. Results: The MAP at 20, 25, and 30 min in group C150 (91±7, 91±6, and 90±7 mmHg, respectively) was less than in group F50 (99±4, 101±6, and 101±5 mmHg, respectively) (P<0.05). There was no difference in HR and onset time of anesthesia among the groups. Analgesic times in groups C150, F50, and F100 (270±22, 265±23, and 323±82 min, respectively) were longer than in group C100(207±59 min), (P<0.05). The number of patients using a urinary catheter to void was much higher in group F100 (7 patients) than in the groups C100, C150, or F50 (4, 5, and 3 patients, respectively) (P<0.05). The voiding time was longer in group C150 than in group C100 (369±122 min vs 266±83 min, P<0.05). No side effects were reported. Conclusions: We conclude that clonidine 150㎍ is adequate to provide effective analgesia and a low incidence of urinary retention during caudal anesthesia.