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Kim, Byung Chan,Kim, Hyerim,Lee, Hye Soo,Kim, Su Hyun,Cho, Do-Hyun,Jung, Hee Ju,Bhatia, Shashi Kant,Yune, Philip S.,Joo, Hwang-Soo,Kim, Jae-Seok,Kim, Wooseong,Yang, Yung-Hun The Korean Society for Microbiology and Biotechnol 2022 Journal of microbiology and biotechnology Vol.32 No.6
Methicillin-resistant Staphylococcus aureus (MRSA) causes severe infections and poses a global healthcare challenge. The utilization of novel molecules which confer synergistical effects to existing MRSA-directed antibiotics is one of the well-accepted strategies in lieu of de novo development of new antibiotics. Thymol is a key component of the essential oil of plants in the Thymus and Origanum genera. Despite the absence of antimicrobial potency, thymol is known to inhibit MRSA biofilm formation. However, the anti-MRSA activity of thymol analogs is not well characterized. Here, we assessed the antimicrobial activity of several thymol derivatives and found that 4-chloro-2-isopropyl-5-methylphenol (chlorothymol) has antimicrobial activity against MRSA and in addition it also prevents biofilm formation. Chlorothymol inhibited staphyloxanthin production, slowed MRSA motility, and altered bacterial cell density and size. This compound also showed a synergistic antimicrobial activity with oxacillin against highly resistant S. aureus clinical isolates and biofilms associated with these isolates. Our results demonstrate that chlorinated thymol derivatives should be considered as a new lead compound in anti-MRSA therapeutics.
사구체신염에서 N-acetyl-β-D-glucosaminidase의 예후 인자로서의 유용성
김혜영,김미경,오동진,김범,김대중,오하영,김윤구,허우성 대한신장학회 1999 Kidney Research and Clinical Practice Vol.18 No.4
Backgrounds:N-acetyl-β-D-glucosaminidase (NAG) is one of many enzymes that exist in the renal proximal tubular cells. It is said that functional impairment of renal tubule can be detected by checking NAG in the urine. But, it has never been known whether urinary NAG value can be used as a predictor for the prognosis of patients with glomerulonephritis. In this study, we evaluated the relationship between urinary NAG level and the degree of injury in cortical interstitium which has been known to influence the prognosis of renal function in glomerulonephritis closely. Methods:Before renal biopsy was performed in each patient, urinary NAG(isoenzyme A and B), urinary β2-microglobulin, serum blood urea nitrogen (BUN), serum creatinine, serum albumin, creatinine clearance and 24 hour urinary protein excretion were measured. Then, we calculated volume density of cortical interstitium〔Vv(i/c)〕 in each specimen using point count morphometry method after getting a confirmative diagnosis from pathologist. Simple coation analysis and multivariate regression analysis were carried out. Results:The number of total patients was 32(male:16), whose median age was 60(32-80). Vv (i/c) had significant correlation with serum creatinine, creatinine clearance and serum BUN. But it was not correlated well with urinary NAG and urinary β2-microglobulin. Urinary NAG concentration(2.131 2.549unit/mmol Cr) was higher than that of normal control and showed significant correlation with urinary β2-microglobulin, serum albumin and 24 hour urinary protein excretion in patients. Conclusion:Urinary NAG had no significant correlation with Vv(i/c) that has been known as an important prognostic factor for the renal function in glomerulonephritis, but had significant correlation with urinary protein excretion. We concluded that urinary NAG was not regarded to be an appropriate marker for predicting the prognosis of renal function in patient with glomerulonephritis.
Hwang, Jin Ho,Han, Seung Seok,Huh, Wooseong,Park, Su-Kil,Joo, Dong Jin,Kim, Myoung Soo,Kim, Yu Seun,Min, Sang-Il,Ha, Jongwon,Kim, Sang Joon,Kim, Suhnggwon,Kim, Yon Su Springer International ; Oxford University Press 2012 Nephrology, dialysis, transplantation Vol.27 No.6
<P>Idiopathic focal segmental glomerulosclerosis (FSGS) occurring at young age is known to predispose to poor graft outcome, but the outcome of adulthood-onset FSGS (A-FSGS) has not been thoroughly investigated. Here, we compared the graft outcomes between kidney recipients with A-FSGS and childhood-onset FSGS (C-FSGS).</P>
Dithiocarbamate chitosan as a potential polymeric matrix for controlled drug release
Kim, Youn Taeg,Yum, Soohwan,Heo, Jeong Soon,Kim, Wooseong,Jung, Yunjin,Kim, Young Mi Informa Healthcare USA, Inc. 2014 Drug development and industrial pharmacy Vol.40 No.2
<P><I>Objective</I>: To develop a polymer matrix for controlled release of drugs, chitosan, a linear aminopolysaccharide, was chemically modified to dithiocarbamate chitosan (DTCC) to afford a matrix where metal-drug complexes could be attached and released in a controlled manner depending on the binding nature between the drugs and the metals.</P><P><I>Materials and methods</I>: DTCC was treated with metal-tetracycline (Tc) complexes to prepare DTCC-Ca(II)-Tc, DTCC-Mg(II)-Tc, DTCC-Cu(II)-Tc and DTCC-Zn(II)-Tc.</P><P><I>Results</I>: The binding amount of Tc was in the order of DTCC-Zn(II)-Tc ≈ DTCC-Mg(II)-Tc ≈ DTCC-Ca(II)-Tc > DTCC-Cu(II)-Tc. The biphasic binding profiles, where Tc binding increased initially and then decreased, were shown for DTCC-Cu(II)-Tc and DTCC-Zn(II)-Tc. In a flow method, Tc was released slowly from DTCC-metal-Tc complexes except for DTCC-Cu(II)-Tc compared with Tc release from DTCC-Tc. In parallel with the results of the release experiment, DTCC-metal-Tc complexes except for DTCC-Cu(II)-Tc presented a prolonged antibacterial activity in an antibacterial test. The antibacterial activity of DTCC-Ca(II)-, -Mg(II)- and -Zn(II)-Tc complexes lasted for 28-44 days, while free Tc and DTCC-Tc lasted for 7-12 days.</P><P><I>Discussion and conclusion</I>: Taken together, our data suggest that DTCC could be used for a polymeric matrix for controlled release of drugs such as Tc, which possess functional groups for ionic and/or coordinate bond with metals.</P>
Kim, Wooseong,Yang, Yejin,Kim, Dohoon,Jeong, Seongkeun,Yoo, Jin-Wook,Yoon, Jeong-Hyun,Jung, Yunjin Dove Medical Press 2017 Drug design, development and therapy Vol.11 No.-
<P>Metronidazole (MTDZ), the drug of choice for the treatment of protozoal infections such as luminal amebiasis, is highly susceptible to colonic metabolism, which may hinder its conversion from a colon-specific prodrug to an effective anti-amebic agent targeting the entire large intestine. Thus, in an attempt to control the colonic distribution of the drug, a polymeric colon-specific prodrug, MTDZ conjugated to dextran via a succinate linker (Dex-SA-MTDZ), was designed. Upon treatment with dextranase for 8 h, the degree of Dex-SA-MTDZ depolymerization (%) with a degree of substitution (mg of MTDZ bound in 100 mg of Dex-SA-MTDZ) of 7, 17, and 30 was 72, 38, and 8, respectively, while that of dextran was 85. Depolymerization of Dex-SA-MTDZ was found to be necessary for the release of MTDZ, because dextranase pretreatment ensures that de-esterification occurs between MTDZ and the dextran backbone. In parallel, Dex-SA-MTDZ with a degree of substitution of 17 was found not to release MTDZ upon incubation with the contents of the small intestine and stomach of rats, but it released MTDZ when incubated with rat cecal contents (including microbial dextranases). Moreover, Dex-SA-MTDZ exhibited prolonged release of MTDZ, which contrasts with drug release by small molecular colon-specific prodrugs, MTDZ sulfate and <I>N</I>-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-<SMALL>D</SMALL>,<SMALL>L</SMALL>-glycine. These prodrugs were eliminated very rapidly, and no MTDZ was detected in the cecal contents. Consistent with these in vitro results, we found that oral gavage of Dex-SA-MTDZ delivered MTDZ (as MTDZ conjugated to [depolymerized] dextran) to the distal colon. However, upon oral gavage of the small molecular prodrugs, no prodrugs were detected in the distal colon. Collectively, these data suggest that dextran conjugation is a potential pharmaceutical strategy to control the colonic distribution of drugs susceptible to colonic microbial metabolism.</P>
Kim, Hyunjeong,Kim, Wooseong,Yum, Soohwan,Hong, Sungchae,Oh, Jeong-Eun,Lee, Ji-Woo,Kwak, Mi-Kyoung,Park, Eun Ji,Na, Dong Hee,Jung, Yunjin Elsevier 2013 FREE RADICAL BIOLOGY AND MEDICINE Vol.65 No.-
<P><B>Abstract</B></P> <P>Caffeic acid phenethyl ester (CAPE) is a polyphenolic natural product that possesses numerous biological activities including anti-inflammatory effects. CAPE-mediated nuclear factor-erythroid 2 p45 (NF-E2)-related factor 2 (Nrf2) activation is likely responsible for some of its biological effects. CAPE was chemically modified to yield CAPE analogues that were subjected to experiments examining cellular Nrf2 activity. CAPE and the CAPE analogue with a catechol moiety, but not the other analogues, activated the Nrf2 pathway. In addition, only biotin-labeled CAPE analogues with the catechol moiety precipitated Kelch-like ECH associated protein 1 (Keap1) when incubated with cell lysates and streptavidin agarose beads. Sodium hypochlorite (NaOCl) oxidation of the catechol moiety in CAPE produced an oxidized, electrophilic form of CAPE (Oxi-CAPE) and greatly enhanced the ability of CAPE to activate Nrf2 and to bind to Keap1. Rectal administration of CAPE ameliorated 2,4,6-trinitrobenzene sulfonic acid-induced rat colitis and activated the Nrf2 pathway in the inflamed colon, and incubation of CAPE in the lumen of the inflamed distal colon generated Oxi-CAPE. However, these biological effects and chemical change of CAPE were not observed in the normal colon. Our data suggest that CAPE requires the catechol moiety for the oxidation-enhanced activation of the Nrf2 pathway and has potential as a pathologically targeted Nrf2-activating agent that is exclusively activated in pathological states with oxidative stress such as colonic inflammation.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The catechol moiety in caffeic acid phenethyl ester (CAPE) is required for CAPE activation of Nrf2. </LI> <LI> Oxidized CAPE (most likely an electrophilic <I>o</I>-quinone form) is responsible for the biological activity of CAPE. </LI> <LI> CAPE ameliorates experimental rat colitis and generates the oxidized form of CAPE in the inflamed colonic tissues. </LI> <LI> CAPE activates the Nrf2 pathway in the inflamed colonic tissues but not in the normal colonic tissues. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Kim, Wooseong,Nam, Joon,Lee, Sunyoung,Jeong, Seongkeun,Jung, Yunjin American Chemical Society 2016 MOLECULAR PHARMACEUTICS Vol.13 No.6
<P>To improve the anticolitic efficacy of 5-aminosalicylic acid (5-ASA), a colon-specific mutual prodrug of 5-ASA was designed. 5-ASA was coupled to procainamide (PA), a local anesthetic, via an azo bond to prepare 5-(4-{[2-(diethylamino)ethyl]carbamoyl}phenylazo)salicylic acid (5-ASA-azo-PA). 5-ASA-azo-PA was cleaved to 5-ASA and PA up to about 76% at 10 h in the cecal contents while remaining stable in the small intestinal contents. Oral gavage of 5-ASA-azo-PA and sulfasalazine, a colon-specific prodrug currently used in clinic, to rats showed similar efficiency in delivery of 5-ASA to the large intestine, and PA was not detectable in the blood after 5-ASA-azo-PA administration. Oral gavage of 5-ASA-azo-PA alleviated 2,4,6-trinitrobenzenesulfonic acid-induced rat colitis. Moreover, combined intracolonic treatment with 5-ASA and PA elicited an additive ameliorative effect. Furthermore, combined treatment with 5-ASA and PA additively inhibited nuclear factor-kappaB (NF kappa B) activity in human colon carcinoma cells and inflamed colonic tissues. Finally, 5-ASA-azo-PA administered orally was able to reduce inflammatory mediators, NF kappa B target gene products, in the inflamed colon. 5-ASA-azo-PA may be a colon-specific mutual prodrug acting against colitis, and the mutual anticolitic effects occurred at least partly through the cooperative inhibition of NF kappa B activity.</P>