• Biomolecules & Therapeutics
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• 제30권2호
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• pp.126-136
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• 2022

Liver fibrosis is part of the wound healing process to help the liver recover from the injuries caused by various liver-damaging insults. However, liver fibrosis often progresses to life-threatening cirrhosis and hepatocellular carcinoma. To overcome the limitations of current in vivo liver fibrosis models for studying the pathophysiology of liver fibrosis and establishing effective treatment strategies, we developed a new mouse model of liver fibrosis using polyhexamethylene guanidine phosphate (PHMG-p), a humidifier sterilizer known to induce lung fibrosis in humans. Male C57/BL6 mice were intraperitoneally injected with PHMG-p (0.03% and 0.1%) twice a week for 5 weeks. Subsequently, liver tissues were examined histologically and RNA-sequencing was performed to evaluate the expression of key genes and pathways affected by PHMG-p. PHMG-p injection resulted in body weight loss of ~15% and worsening of physical condition. Necropsy revealed diffuse fibrotic lesions in the liver with no effect on the lungs. Histology, collagen staining, immunohistochemistry for smooth muscle actin and collagen, and polymerase chain reaction analysis of fibrotic genes revealed that PHMG-p induced liver fibrosis in the peri-central, peri-portal, and capsule regions. RNA-sequencing revealed that PHMG-p affected several pathways associated with human liver fibrosis, especially with upregulation of lumican and IRAK3, and downregulation of GSTp1 and GSTp2, which are closely involved in liver fibrosis pathogenesis. Collectively we demonstrated that the PHMG-p-induced liver fibrosis model can be employed to study human liver fibrosis.

• 생명과학회지
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• 제24권5호
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• pp.558-566
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• 2014

카드뮴(Cd)에 의해 유도되는 담배의 생장과 rubisco/rubisco activase에 미치는 ESA (ethylsalicylic acid)의 효과 및 이에 대한 변성제의 효과를 연구하였다. 담배기내 배양에 대한 ESA의 최적 농도를 찾기 위해, $10^{-6}$-10 mM ESA를 처리하여 배양시킨 결과, $10^{-4}$ mM ESA에서 생장이 가장 높게 나타났다. 최적농도인 $10^{-4}$ mM ESA와 0.2 mM $CdCl_2{\cdot}2.5H_2O$를 사용하여, 대조구, Cd 처리구, ESA 처리구 및 Cd와 ESA 혼합구에서의 담배의 생장을 측정한 결과, ESA 처리구의 생장이 가장 좋았으며, Cd 처리구의 생장이 가장 저조하였다. Rubisco/rubisco activase의 함량과 활성을 측정한 결과, 두 가지의 함량과 활성 모두 Cd 처리구가 가장 낮았으며, ESA 처리구에서는 Rubisco와 rubisco activase의 함량이 감소되었고, 활성은 증가하였다. Guanidine-HCl 처리를 제외한 L-cysteine, urea, thiourea, ${\beta}$-mercaptoethanol, EDTA에 의해 rubisco의 활성이 억제되었으며, L-cysteine, urea, thiourea, guanidine-HCl 처리구에서는 rubisco activase 활성이 변화가 없었으나, ${\beta}$-mercaptoethanol과 EDTA는 활성을 증가시키는 것으로 나타났다. 결론적으로, ESA는 rubisco의 함량을 억제시키고 활성은 촉진시키며, rubisco activase의 함량은 촉진시키고 활성은 억제시켰다. 또한 Cd에 의해 저해된 rubisco와 rubisco activase의 활성이 변성제에 의해 저해되었으며, Cd에 의해 저해된 ESA의 회복이 변성제에 의하여 상실되었다.

• Bulletin of the Korean Chemical Society
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• 제35권7호
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• pp.2065-2071
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• 2014

${\beta}$-Secretase (beta-amyloid converting enzyme 1 [BACE1]) is involved in the first and rate-limiting step of ${\beta}$-amyloid ($A{\beta}$) peptides production, which leads to the pathogenesis of Alzheimer's disease(AD). Therefore, inhibition of BACE1 activity has become an efficient approach for the treatment of AD. Ligand-based and docking-based 3D-quantitative structure-activity relationship (3D-QSAR) studies of acyl guanidine analogues were performed with comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) to obtain insights for designing novel potent BACE1 inhibitors. We obtained highly reliable and predictive CoMSIA models with a cross-validated $q^2$ value of 0.725 and a predictive coefficient $r{^2}_{pred}$ value of 0.956. CoMSIA contour maps showed the structural requirements for potent activity. 3D-QSAR analysis suggested that an acyl guanidine and an amide group in the $R_6$ substituent would be important moieties for potent activity. Moreover, the introduction of small hydrophobic groups in the phenyl ring and hydrogen bond donor groups in 3,5-dichlorophenyl ring could increase biological activity.

• 한국미생물·생명공학회지
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• 제19권3호
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• pp.308-312
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• 1991

B.thuringiensis subsp. darmstadiensis 73E10-2의 내독소에 대한 화학적 처리에서 고농도의 중성염(4M NaBr), 유기용매(50% acetone), 변성제(4M urea) 및 중성 계면활성제(10% triton X-100)로 내독소를 처리하였을 때 모기유충에 대한 독력의 소실이 거의 나타나지 않았으나, guanidine HCL이나 $CCl_4$ 또는 양이온 및 음이온 계면활성제로 처리함으로써 그 독력이 크게 소실되었다. 또한, 내독소의 sulfhydryl기의 변형은 모기유충에 대한 독력에 영향을 나타내지 못하였으나, lysine기 변형으로 내독소의 독력이 거의 완전히 소실되었다.

• 한국미생물·생명공학회지
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• 제16권5호
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• pp.393-397
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• 1988

고도 호열성균의 Adenylate kinase가 phospho cellulose column의 adenosine-penta-phospho adenosine affinity elution으로부터 균일하게 정제되었다. 분자량은 SDS PAGE와 gel filtration으로부터 22,000의 단량체로 밝혀졌다. 효소반응의 최적온도는 8$0^{\circ}C$이였으며 정반응의 활성화 에너지는 22.4kcal/mole이었다. 본 효소는 6M guanidine-HCI에 활성을 잃지 않았으며 10$0^{\circ}C$에서 한시간에 75%의 활성을 유지하였다. AMP, ADP, ATP에 대한 Km치는 0.01mM, 0.017mM, 0.067mM이었다.

• 대한화학회지
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• 제37권1호
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• pp.131-135
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• 1993

2-Amino-3-cyano-6-chloromethylpyrazine으로부터 합성한 methotrexate(MTX) 중간 유도체의 모핵인 pteridine ring의 $C_2$-amino 대신 $HCH_3$기, 또는 $nH_2$기로 치환된 화합물 (7a),(7b)와 (7c)를 두 단계에 걸쳐 합성하였다. 출발물질인 dibenzyl 4,4'-dithiobisbenzoate(12)와 2-amino-3-cyano-6-chloromethylpyrazine으로부터 합성한 2-amino-3-cyano-6-[(S-p-carbenzyloxyphenyl)thiomethyl]-pyrazine(14)화합물을 formamidine HCl, acetamidine HCl과 guanidine HCl 등과 각각 반응시켜 cyclization시키고, 이 화합물을 ethanol 용매하에서 0.2N NaOH를 사용한 알칼리 가수분해로 pteroic acid유도체를 합성하였다.

• Bulletin of the Korean Chemical Society
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• 제30권4호
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• pp.913-916
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• 2009

Femtosecond vibrational spectroscopy was used to probe the dynamics of CO rebinding to hemoglobin (Hb), denatured by 4.0 M GdnHCl in $D_2O# at 283 K, after photolysis of HbCO. The stretching mode of $^{13}CO$ bound to the denatured $Hb^{13}CO$ showed a single band centered at 1922 $cm^{-1}$, indistinguishable from that of denatured $Mb^{13}CO$. Geminate rebinding of CO to the denatured Hb was accelerated more than 1000 times, suggesting that the native structure of the Hb is required to suppress efficient geminate rebinding of CO, as is the case in Mb. The geminate yield and rate for CO rebinding are almost the same in both the denatured Hb and Mb. Similarity in the equilibrium spectrum and rebinding dynamics of CO indicates that the state of the denatured Hb is very similar to that of the denatured Mb. In the denatured Hb, quaternary contact of the protein is likely severed, with the denatured protein existing as an independent subunit much like Mb.

• Bulletin of the Korean Chemical Society
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• 제31권12호
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• pp.3623-3631
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• 2010

We prepared several novel molecular transporters built on myo- and scyllo-inositol scaffolds with variations in the number of guanidine residues, linker chain lengths and patterns. Some of these transporters were found to localize in mitochondria, and the mitochondrial affinity seems to be substantially related to the scaffold stereochemistry.

• 농업생명과학연구
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• 제43권6호
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• pp.105-109
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• 2009

경산 묘목단지는 대단위 과수종묘를 생산하고 있어 경쟁력 강화를 위하여 무독묘 보증 생산이 요구되고 있다. 특히 생산규모가 큰 사과종묘에 대한 빠르고 정확한 바이러스 진단이 시급하다. 본 연구에서는 사과바이러스 진단을 위하여 다량의 시료를 동시 분쇄할 수 있는 bead beater를 이용하였으며 분쇄 bead는 저가의 산업용 glass bead (0.4 mm 직경)를 일회용으로 채택하였다. RNA추출을 위하여서는 guanidine thiocyanate 용액이 Trizol 용액보다 효과적인 것으로 나타났으며 silica membrane tube의 이용으로 RNA추출 간편성을 높일 수 있었다. 사과바이러스는 RT-PCR에 의하여 검증하였다.

• Journal of Industrial and Engineering Chemistry
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• 제68권
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• pp.153-160
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• 2018

An environmentally favorable (chlorine-free) solid oxidizer, guanidinium dinitramide [GDN; $NH_2C(NH_2)NH_2N(NO_2)_2$], was newly synthesized from guanidine carbonate [$NH_2C(=NH)NH_2{\cdot}1/2H_2CO_3$]. Two different crystalline forms (${\alpha}-type$ and ${\beta}-type$) appeared according to the applied solvents and synthesis conditions. Moisture, during extraction, might become trapped in a crystal between inner molecules. Therefore, despite having the same chemical composition, Raman-IR and TGA-DSC revealed different physical characteristics of the two forms. Peaks of Raman shift near $1000cm^{-1}$ implied different chemical structures. Thermal analysis revealed an exothermic temperature $155.7^{\circ}C$ for ${\alpha}-type$ but one of $191.6^{\circ}C$ for ${\beta}-type$. The caloric value of ${\alpha}-type$ was 536.4 J/g, which was 2.5 times larger than that of the ${\beta}-type$, which was 1310 J/g. While the synthesized GDN of ${\alpha}-type$ showed a steep exothermic decomposition, the ${\beta}-type$ was slowly decomposed after melting through an endothermic process. This work implied that despite of the same molecular formula some different core thermal properties would appear depending on synthesis conditions.