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Lee, Soyoung,Nam, Kyu-Yeol,Oh, Jaeseong,Lee, SeungHwan,Cho, Sang-Min,Choi, Youn-Woong,Cho, Joo-Youn,Lee, Beom-Jin,Hong, Jang Hee Dove Medical Press 2018 Drug design, development and therapy Vol.12 No.-
<P><B>Background</B></P><P>Levodropropizine is a non-opioid antitussive agent that inhibits cough reflex by reducing the release of sensory peptide in the peripheral region. To improve patients’ compliance, a controlled-release (CR) tablet is under development. The aim of this study was to compare the pharmacokinetic (PK) profiles of the CR and immediate-release (IR) tablets of levodropropizine. In addition, the effect of food on the PK properties of levodropropizine CR tablet in healthy subjects was evaluated.</P><P><B>Subjects and methods</B></P><P>A randomized, open-label, multiple-dose, three-treatment, three-period, six-sequence, crossover study was conducted on 47 healthy subjects. All subjects were randomly assigned to one of the six sequences, which involve combinations of the following three treatments: levodropropizine IR 60 mg three times in the fasted state (R), levodropropizine CR 90 mg two times in the fasted state (T), and levodropropizine CR 90 mg two times in the fed state (TF). Serial blood samples were collected up to 24 h after the first dose. Tolerability was assessed based on the vital signs, adverse events (AEs), and clinical laboratory tests.</P><P><B>Results</B></P><P>Levodropropizine CR showed lower maximum drug concentration (<I>C</I><SUB>max</SUB>) and similar total exposure compared to levodropropizine IR. The geometric mean ratios (GMRs) (90% confidence intervals [CIs]) of T to R for the <I>C</I><SUB>max</SUB> and area under the concentration–time curve from the 0 to 24 h time points (AUC<SUB>0–24h</SUB>) were 0.80 (0.75–0.85) and 0.89 (0.86–0.93), respectively. In the fed group, levodropropizine CR showed exposure similar to that in the fasted group. The GMRs (90% CIs) of TF to T for the <I>C</I><SUB>max</SUB> and AUC<SUB>0–24h</SUB> were 0.90 (0.85–0.97) and 1.10 (1.05–1.14), respectively. No serious AEs occurred with both levodropropizine CR and IR tablets.</P><P><B>Conclusion</B></P><P>Total systemic exposure for levodropropizine was similar in subjects receiving the CR and IR formulations in terms of the AUC. Although food delayed the absorption of levodropropizine CR, systemic exposure was not affected.</P>
Synthesis and HIV-1 Integrase Inhibitory Activities of 4-Hydroxy-5-azacoumarin 3-Carboxamides
Lee, Seung-Uk,Park, Jang-Hyun,Kwon, Tae-Hoon,Yoo, Yeong-Jae,Lee, Jae-Yeol,Shin, Cha-Gyun,Yoo, Kyung-Ho,Lee, Yong-Sup Korean Chemical Society 2007 Bulletin of the Korean Chemical Society Vol.28 No.9
Recently, it has been reported that the inhibition of the strand transfer function of HIV-1 integrase is necessary to obtain significant antiviral activity. Accordingly, several compounds typified by aryl 1,3-diketo acids that can inhibit strand transfer reaction of HIV-1 IN have been identified. In this work, we synthesized new 4- hydroxy-5-azacoumarin-3-carbox(thio)amides (1a-h) and evaluated for the inhibition of HIV-1 IN strand transfer reaction with a brief SAR. Among synthesized, compound 1e was the most potent HIV-1 IN inhibitor with equipotent activity to that of L-708,906. Therefore, the 4-hydroxy-5-azacoumarin ring can be considered as a new scaffold in designing more potent of HIV-1 IN inhibitors for treatment of AIDS.
Jang-yeol Lee,Een- soon Yoo,Hyoun-chull Kim,Il-hae Park,Sang-chull Lee 대한치과이식임플란트학회 2006 The Korean Academy of Implant Dentistry Vol.25 No.2
서 론 : 상악동거상술시 골이식재로 자가골,동종골, 이종골, 합성골 혹은 이들 이식재료의 혼합형태를 사용 할수 있으며 이중자가골은다른 이식재료와 달리 골재형성이 빠르고 흡수율이 높은 것으로 알려져 있다. 골 이식을 위한자가골은구강내 악골 혹은구강외 장골 등에서 채취될 수 있으며,구강내 악골에서 채취된자가 골에 비해 장골의 경우보다빠른이식골의 흡수를 보이는 것으로 보고되고 있다. 이에 저자등은 상악골거상 술시 골이식재로써 하악지에서 채취된 골을 사용한 증례와 장골에서 채취된 골을 사용한 증례를 비교해 봄 으로써 채취된자가골의 기원에 따른흡수율 차이를 비교평가해보고자 한다. 재료 및 방법 : 리빙웰 치과병원에 내원하여 상악동거상술 및 자가골이식을 시행한 10증례 (24 임프란트 식립 부위)에 대하여 술후 파노라마방사선사진 및 1년뒤 파노라마방사선사진을 비교하여 흡수율을 비교해 보았 다. 5증례 (13 임프란트 식립부위)에 경우 이식재로 장골을 사용하였으며,5증례 (11 임프란트 식립부위)에 경 우 하악지에서 채취된 골을 사용하였고 각증례 모두에서 상악동거상술과 함께 임프란트 동시식립을 시행하 결 과 : 하악지에서 이식된 재료의 평균 흡수율은 2.6± 1.1 mm 로 나타났고, 장골의 경우 1.2±0.4 mm 로 측정되 어 장골의 경우 이식 재의 흡수율이 적은 것으로 나타났다. 토의 및 결론 : 자가골 이식의 경우 일반적으로 골형성의 기원이 다른 장골에서 흡수율이 높다고 알려져 있 다. 그러나 본 연구 결과 기존의 보고와는 다른 결과가 나타났는데 이는 장골에서 이식 재 채취시 수질골을 함 께 채취하여 사용함으로써 신속한 골형성을 도모하였고, Hydroxyapatite coated fixture를 사용한 동시식립에 의해 임프란트 주변의 골흡수율이 억 제된 결과로 사료된다.
GSH-dependent peroxidase activity of the rice (Oryza sativa) glutaredoxin, a thioltransferase
Lee, Kyun-Oh,Lee, Jung-Ro,Yoo, Ji-Young,Jang, Ho-Hee,Moon, Jeong-Chan,Jung, Bae-Gyo,Chi, Yong-Hun,Park, Soo-Kwon,Lee, Seung-Sik,Lim, Chae-Oh,Yun, Dae-Jin,Cho, Moo-Je,Lee, Sang-Yeol Plant molecular biology and biotechnology research 2002 Plant molecular biology and biotechnology research Vol.2002 No.-
Glutaredoxin (Grx) is a 12-kDa thioltransoferase that reduces disulfide bonds of other proteins and maintains the redox potential of cells. In addition to its oxidoreductase activity, we report here that a rice Grx(OsGrx) can also function as a GSH-dependent peroxidase. Because of this antioxidant activity, OsGrx protects glutamine synthetase from oxidative damage. Individually replacing the conserved Cys residues in OsGrx with Ser shows that Cys^(23), but not Cys^(26), is essential for the thioltransferase and GSH-de-pendent peroxidase activities. Kinetic Characterization of OsGrx reveals that the maximal catalytic efficiency (V_(max)/K_(m))is obtained with cumene hydroperoxide rather than H_(2)O_(2) or t-butyl hydroperoxide.
Lee, Sang Yeol,Lee, Kyun Oh,Jang, Ho Hee,Lee, Ji Yeun,Lee, Seung Sik,Jung, Bae Gyo,Chi, Yong Hun,Kang, Soon Suk,Park, Soo Kwon,Lee, Jung Ro,Yoo, Ji Young 생화학분자생물학회 1970 BMB Reports Vol.34 No.4
Even though three isotypes of thioredoxins (-f, -m and -h types) have been identified in a variety of plant cells, there are only a few reports on thioredoxin-h that were recently identified. In this study, a cDNA encoding a h-type of thioredoxin was isolated from a cDNA library of Chinese cabbage, and named here CTrx-h. An open reading frame of the gene contained a polypeptide of 133 amino acids with a conserved active center, WCGPC, which appeared in all of the thioredoxin proteins. A deduced amino acid sequence of the CTrx-h showed the highest sequence identity with those of Arabidopsis thioredoxin-h2 (75.2 %) and thioredoxin-h5 (46.6%) proteins, but it shared a low sequence homology to other isotypes of plant thioredoxinm and thioredoxin-f. The CTrx-h protein that is expressed in E. coli represented not only an insulin reduction activity, but also electron transferring activity from NADPH to thioredoxin-dependent peroxidase. A genomic Southern blot analysis using the cDNA insert of CTrx-h revealed that the gene consisted of a small multigene family in Chinese cabbage genome. On the contrary to other thioredoxin-h proteins that were widely distributed in most tissues of the plant, the CTrx-h was predominantly expressed in flowers. The expression was very low in other tissues. The data of the Northern blot analysis suggests that the CTrx-h may have other functions in flower development or differentiation, in addition to its defensive role.