• Applied Chemistry for Engineering
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• v.26 no.1
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• pp.111-115
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• 2015

Two new analogs of bestatin were prepared from $\small{D}$-leucine and $\small{D}$-valine in a stereoselective and efficient way. An aminopeptidase inhibitor bestatin shows significant biological effects on immunomodulation and is marketed for the treatment of acute myelocytic leukemia. The key intermediates, trans-oxazolidine methyl esters 2a and 2b, were obtained with more than 20 to 1 stereoselectivity in a one-pot procedure by the three cascade reactions between N-hydroxymethyl protected ${\alpha}$-amino aldehydes (4a and 4b) and phenylsulfonylnitromethane ($PhSO_2CH_2NO_2$) and the following in-situ ozonolysis. Basic hydrolysis of 2a and 2b, and then the peptide coupling with $\small{L}$-Leu-OMe produced the protected derivatives of two new bestatin analogs, 3a and 3b, respectively. The new isobutyl and isopropyl analogs of bestatin (1a and 1b) were produced in overall 51% and 38% yields, respectively, with high stereoselectivity from the corresponding protected ${\alpha}$-amino aldehydes 4 in a six-step process.

• Biomolecules & Therapeutics
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• v.30 no.2
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• pp.170-178
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• 2022

The airway epithelium is equipped with the ability to resist respiratory disease development and airway damage, including the migration of airway epithelial cells and the activation of TLR3, which recognizes double-stranded (ds) RNA. Primary cilia on airway epithelial cells are involved in the cell cycle and cell differentiation and repair. In this study, we used Beas-2B human bronchial epithelial cells to investigate the effects of the TLR3 agonist polyinosinic:polycytidylic acid [Poly(I:C)] on airway cell migration and primary cilia (PC) formation. PC formation increased in cells incubated under serum deprivation. Migration was faster in Beas-2B cells pretreated with Poly(I:C) than in control cells, as judged by a wound healing assay, single-cell path tracking, and a Transwell migration assay. No changes in cell migration were observed when the cells were incubated in conditioned medium from Poly(I:C)-treated cells. PC formation was enhanced by Poly(I:C) treatment, but was reduced when the cells were exposed to the ciliogenesis inhibitor ciliobrevin A (CilioA). The inhibition of Beas-2B cell migration by CilioA was also assessed and a slight decrease in ciliogenesis was detected in SARS-CoV-2 spike protein (SP)-treated Beas-2B cells overexpressing ACE2 compared to control cells. Cell migration was decreased by SP but restored by Poly(I:C) treatment. Taken together, our results demonstrate that impaired migration by SP-treated cells can be attenuated by Poly(I:C) treatment, thus increasing airway cell migration through the regulation of ciliogenesis.

• Applied Chemistry for Engineering
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• v.26 no.1
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• pp.86-91
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• 2015

The MPPO (3-methyl-1-phenyl-2-phospholene-1-oxide) was prepared by using various polymerization inhibitors such as BHT (2,6-di-tert-butyl-4-methylphenol), TBC (4-tert-butylcatechol), and copper stearate. The MPPO was confirmed by the analysis using FTIR, $^1H$-NMR, and GC/MS regardless of the type of inhibitors. The yield of MPPO increased with the increase of reaction time, whereas the purity of MPPO decreased slightly. The yield and purity of MPPO increased with temperature, but the MPPO prepared by using copper stearate as a polymerization inhibitor exhibited no changes in the purity. The amount of inhibitors had no effect on the yield of MPPO. The purity of MPPOs increased with the amount of inhibitors, but the MPPO prepared by using BHT showed no changes of the purity. We found that the MPPO prepared by using copper stearate exhibited the highest catalytic activity for diphenylcarbodiimide synthesis.

• KSBB Journal
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• v.11 no.2
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• pp.125-131
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• 1996

In this study, Bucillus amyloliquefaciens was adopted as bacterial source to investigate the concentration of carbon source by adding inhibitors in the batch culture. By adding acetic acid at $10g/\ell$ of initial glucose concentration, maximum dry cell density was obtained with the highest value of /$\3.9gell$ at $1.0g/\ell$ of initial acetic acid concentration. By adding acetic acid al 10g/$\ell$ of initial glucose concentration, maximum ${\alpha}$-amylase production was obtained with 331.55unit/m1 at $2.0g/\ell$ of initial acetic acid concentration. ${\alpha}$-Amylase production was decreased with the increase of initial acetic acrid concentration. By adding acetic acid to the medium, cell growth and ${\alpha}$-amylase production was higher in glucose than in maltose. By adding lactic acid to the medium, cell growth was decreased.

• Childhood Kidney Diseases
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• v.16 no.2
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• pp.132-137
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• 2012

Microscopic polyangiitis (MPA) is systemic small vessel vasculitis that is very rare in childhood. MPA is characterized by pauci-immune necrotizing small vessel vasculitis without clinical or pathological evidence of necrotizing granulomatous inflammation. Approximately 90% of patients have glomerulonephritis that is accompanied by a variety of other organ involvement. A 10-year-old girl visited our clinic with clinical manifestations suggestive Henoch-Sch$\ddot{o}$nlein purpura nephritis such as purpuric skin rash, abdominal pain, arthralgia on both knees, massive proteinuria and microscopic hematuria. So initially we suspected Henoch-Sch$\ddot{o}$nlein purpura nephritis. However, later her perinuclear-antineutrophil cytoplasmic antibodies(p-ANCA) test was positive, and her renal biopsy was consistent with microscopic polyangiitis. We began steroid therapy, combined with cyclophosphamide, ACE inhibitor. Currently she is a 12-year old, and until now she has been regularly examined in the outpatient. We report a case of microscopic polyangiitis initially suspected with Henoch-Sch$\ddot{o}$nlein purpura nephritis.

• Korean Journal of Microbiology
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• v.46 no.1
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• pp.9-14
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• 2010

In this study, lactic acid bacteria with high angiotensin converting enzyme inhibitor activity were isolated from Korean fermented food, such as kimchi and salted seafood. The strain HLJ59, isolated from salted shrimp showed the highest angiotensin converting enzyme inhibitor activity in DeMan Rogosa Sharpe broth. Optimum growth temperature of Lactobacillus brevis HLJ59 was at $34^{\circ}C$. Acid treatment at pH 3.0 for 1.5 h decreased cell viability from $9.9{\times}10^8$ CFU/ml to $3.11{\times}10^4$ CFU/ml. The bile extract concentration of 0.3%, 0.5%, and 1.0% in MRS broth did not inhibit the growth of HLJ59. Isolated strain HLJ59 showed more sensibility to amikacin, gentamycin, neomycin, streptomycin, kanamycin, cefmetazole, cephalothin, ampicillin, ticarcillin, sulbactam+ampicillin, amoxicillin+clavulanic acid (AMC), tetracycline, and sulfamethoxazole+trime thoprim (SXT) as compare to other 7 different antibiotics. However, it showed more resistance to cefoxatin, ceftnaxone, penicillin, ciprofloxacin, nalidixic acid, lincomycin, and chloramphenicol.

• Applied Chemistry for Engineering
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• v.32 no.6
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• pp.647-652
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• 2021

In this study, Saussurea Lappa roots were extracted using ethanol and n-hexane, and also the effects on proliferation of human hair dermal papilla cells and fibroblast and related signaling pathway were evaluated. 3-[4, 5-dimethylthiazol-2-yl]-2, 5 diphenyl tetrazolium bromide (MTT) assay was conducted for cell proliferation effect of Saussurea Lappa root extract, and extracellular signal-related kinase (ERK), serine/threonine protein kinase (Akt), wingless-related integration site (Wnt)/𝛽-catenin signaling pathway, and 5𝛼-reductase expression through western blot analysis were measured. Saussurea Lappa root extract significantly increased human hair dermal papilla cells and propagation of fibroblast, promoted phosphorylation of ERK and Akt that get involved in cell proliferation. Additionally, Saussurea Lappa root extract significantly decreased promotion of Akt phosphorylation and cell proliferation by MEK/ERK inhibitor PD98059 and PI3K/Akt inhibitor LY294002. Also, Saussurea Lappa root extract induced intranuclear 𝛽-catenin accumulation by promoting phosphorylation of 𝛽-catenin (Ser552, 675) through phosphorylation of GSK-3𝛽 (Ser9), and suppressed activation of 5𝛼-reductase type I and II. Overall, Saussurea Lappa root induces cell proliferation through vitalization of ERK and Akt route of human hair dermal papilla cells and fibroblast and apoptosis defense mechanism, and can be helpful in hair loss prevention and hair growth by vitalizing the 𝛽-catenin signaling pathway and inhibiting activation of 5𝛼-reductase, which can be used as a potential hair care products.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.6
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• pp.667-674
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• 2017

Angiotensin II (Ang II) is metabolized from N-terminal by aminopeptidases and from C-terminal by Ang converting enzyme (ACE) to generate several truncated angiotensin peptides (Angs). The truncated Angs have different biological effects but it remains unknown whether Ang-(4-8) is an active peptide. The present study was to investigate the effects of Ang-(4-8) on hemodynamics and atrial natriuretic peptide (ANP) secretion using isolated beating rat atria. Atrial stretch caused increases in atrial contractility by 60% and in ANP secretion by 70%. Ang-(4-8) (0.01, 0.1, and $1{\mu}M$) suppressed high stretch-induced ANP secretion in a dose-dependent manner. Ang-(4-8) ($0.1{\mu}M$)-induced suppression of ANP secretion was attenuated by the pretreatment with an antagonist of Ang type 1 receptor ($AT_1R$) but not by an antagonist of $AT_2R$ or $AT_4R$. Ang-(4-8)-induced suppression of ANP secretion was attenuated by the pretreatment with inhibitor of phospholipase (PLC), inositol triphosphate ($IP_3$) receptor, or nonspecific protein kinase C (PKC). The potency of Ang-(4-8) to inhibit ANP secretion was similar to Ang II. However, Ang-(4-8) $10{\mu}M$ caused an increased mean arterial pressure which was similar to that by 1 nM Ang II. Therefore, we suggest that Ang-(4-8) suppresses high stretch-induced ANP secretion through the $AT_1R$ and $PLC/IP_3/PKC$ pathway. Ang-(4-8) is a biologically active peptide which functions as an inhibition mechanism of ANP secretion and an increment of blood pressure.

• Childhood Kidney Diseases
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• v.14 no.1
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• pp.94-99
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• 2010

Obesity-related glomerulopathy (ORG) is a secondary form of focal and segmental glomerulosclerosis (FSGS) manifesting as proteinuria and progressive renal dysfunction that results from maladaptive glomerular response to increasing adiposity. Reports of ORG progressing to end stage renal diseases in rare in the pediatric population. We report a 9-year-old boy with obesity (body mass index $35\;kg/m^2$) who was diagnosed with ORG presenting with proteinuria. He was diagnosed with obesity-related glomerulopathy based on the laboratory, urinary, and kidney biopsy finding. In spite of treatment with angiotensin- converting enzyme (ACE) inhibitor and/or, angiotensin-receptor blocking agent, the degree or amount of proteinuria increased and renal function declined continuously. His BMI did not decrease and eventually progressed to chronic renal failure. Consequently, obese patients should be monitored for proteinuria, which may be the first manifestation of FSGS, a lesion that may be associated with serious renal sequelae.

• Journal of Veterinary Clinics
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• v.23 no.3
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• pp.349-354
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• 2006

A 9-month-old, female Miniature Pinscher(MP) dog weighing 1.97kg was presented because of periodic syncopal episode for 5 months. This case was diagnosed as primary dilated cardiomyopathy based on respiratory distress history, weak femoral pulse, generalized cardiomegaly, pulmonary edema, marked dilation of left atrium(LA) and left ventricle(LV), decreased wall thickness of LV and interventricular septum(IVS), increased EPSS in echocardiography, and young age of onset in the absence of other cardiovascular disorders. The patient was stabilized by application of diuretics(Furosemide, 2 mg/kg, SC, q 1 hr) and venodilator(Nitroglycerine patch, 0.5 mg/kg, q 12 hrs). Clinical signs were improved with medical management of positive inotropic vasodilator(Pimobendan, 0.2 mg/kg, PO, q 12 hrs) and angiotensin-converting enzyme(ACE) inhibitor(benazepril, 0.5 mg/kg, PO, q 12 hrs), potassium gluconate gel(2 mEq/dog, PO, q 12 hrs) and, L-carnitine(50 mg/kg, PO, q 12 hrs). The dog still maintains stable clinical status 10 months after the first visit. We report the rare case of DCM in small breed dog, which corresponds to the diagnosis and treatment of typical DCM in large breed dog.