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Design and Synthesis of Novel 2'(β)-Fluoro-3'(α)-hydroxy-threose Nucleosides: Iso-FMAU Analogues as Potent Antiviral Agents

  • Kim, Seyeon;Jee, Jun-Pil;Hong, Joon Hee
    • Journal of Integrative Natural Science
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    • v.8 no.2
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    • pp.99-106
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    • 2015
  • Novel 2'(${\beta}$)-fluoro-3'(${\alpha}$)-hydroxy-threose nucleosides (iso-FMAU) as antiviral agents were designed and racemically synthesized from Solketal. Condensation successfully proceeded from a glycosyl donor 9 under $Vorbr{\ddot{u}}ggen$ conditions yielded the nucleoside analogues. Ammonolysis and hydrolysis of isopropylidene protection group gave the desired nucleoside analogues 12, 15, 18, and 19. The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2 and HCMV. Compound 12 displayed some anti-HCMV activity ($EC_{50}=24.7{\mu}g/ml$) without exhibiting any cytotoxicity up to $100{\mu}M$.

Effect of Mixed Extract of Panax Notoginseng, Rehmanniae Radix and Acanthopanacis Cortex (AIF) on Experimentally Induced Osteoarthritis

  • Park, Shin-Ae;Kim, Jae-Hoon;Ahn, Jeong-Taek;Kim, Won-Tae;Park, Chull-Gyu;Jeong, Man-Bok;Yi, Sun-Shin;Yoon, Yeo-Sung;Yoon, Jung-Hee;Kim, Hyung-Gun;Seo, Kang-Moon
    • Biomolecules & Therapeutics
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    • v.18 no.4
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    • pp.426-432
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    • 2010
  • The objective of the present study was to evaluate the effect of a mixed extract of three herbs, Panax Notoginseng, Rehmanniae Radix and Acanthopanacis cortex (AIF), for the treatment of horses with experimentally induced osteoarthritis. Twelve healthy male horses were included in this study. Horses were assigned to one of two groups: the AIF group (n=6) or the control group (n=6). Osteoarthritis was induced in all horses by intraarticular injection of sodium monoiodoacetate (0.12 mg/kg). Horses in the AIF group received 3 g of AIF with food daily, and those in the control group received food only. Treatment began on the day of intraarticular injection. Clinical and radiographic evaluations were performed every 2 weeks. At week 12, horses were euthanatized, and postmortem gross pathologic and histologic examinations of the middle carpal joint were performed. There were no significant differences in clinical values between the two groups. Radiographic evaluation revealed that the percentages of narrowness of joint space width in the control group were significantly higher than those in the AIF group (p<0.02). On gross pathologic examination, the mean total dimensions of articular cartilage erosions and fibrillations in the control group ($101.5{\pm}41.5mm^2$) were significantly wider than those in the AIF group ($29.3{\pm}39.7mm^2$; p<0.01). On histopathologic evaluation, significantly higher grades of staining intensity and lower empty lacunae (EL) ratios were found in the AIF group (p<0.03). The present study revealed that AIF had significant disease modifying effects in horses with experimentally induced osteoarthritis.

Water Extract of Ecklonia cava Protects against Fine Dust (PM2.5)-Induced Health Damage by Regulating Gut Health

  • Park, Seon Kyeong;Kang, Jin Yong;Kim, Jong Min;Kim, Min Ji;Lee, Hyo Lim;Moon, Jong Hyun;Jeong, Hye Rin;Kim, Hyun-Jin;Heo, Ho Jin
    • Journal of Microbiology and Biotechnology
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    • v.32 no.7
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    • pp.927-937
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    • 2022
  • To confirm the therapeutic effect of the water extract from Ecklonia cava (WEE) against PM2.5 induced systemic health damage, we evaluated gut health with a focus on the microbiota and metabolites. Systemic damage in mice was induced through PM2.5 exposure for 12 weeks in a whole-body chamber. After exposure for 12 weeks, body weight and food intake decreased, and WEE at 200 mg/kg body weight (mpk) alleviated these metabolic efficiency changes. In addition, PM2.5 induced changes in the length of the colon and fecal water content. The administration of the WEE at 200 mpk oral dose effectively reduced changes in the colon caused by PM2.5 exposure. We also attempted to confirm whether the effect of the WEE is mediated via regulation of the microbiota-gut-brain axis in mice with PM2.5 induced systemic damage. We examined changes in the fecal microbiota and gut metabolites such as short-chain fatty acids (SCFAs) and kynurenine metabolites. In the PM2.5 exposed group, a decrease in the abundance of Lactobacillus (Family: Lactobacillaceae) and an increase in the abundance of Alistipes (Family: Rikenellaceae) were observed, and the administration of the WEE showed a beneficial effect on the gut microbiota. In addition, the WEE effectively increased the levels of SCFAs (acetate, propionate, and butyrate). Furthermore, kynurenic acid (KYNA), which is a critical neuroprotective metabolite in the gut-brain axis, was increased by the administration of the WEE. Our findings suggest that the WEE could be used as a potential therapeutic against PM2.5 induced health damage by regulating gut function.

Constitutive Coexpression of Bacillus Endoxylanase and Trichoderma Endoglucanase Genes in Saccharomyces cerevisiae

  • Lee, Jae-Hyung;Lim, Myung-Ye;Kim, Mi-Jin;Heo, Sun-Yeon;Seo, Jin-Ho;Kim, Yeon-Hee;Nam, Soo-Wan
    • Journal of Microbiology and Biotechnology
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    • v.17 no.12
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    • pp.2076-2080
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    • 2007
  • The endoxylanase (GenBank Access No. U51675) of Bacillus spp. and endoglucanase (GenBank Access No. AY466436) of Trichoderma spp. were separately inserted downstream of the yeast constitutive ADHI promoter, resulting in three different plasmids (pAGX1, pAGX2, and pAGX3) according to the transcription direction of two genes. When the yeast transformants, S. cerevisiae SEY2102 harboring each expression plasmid, were grown on YPD medium, the total activities of the enzymes were approximately 3.01 unit/ml, 3.24 unit/ml, and 7.56 unit/ml for endoxylanase and 0.60 unit/ml, 0.54 unit/ml, and 0.39 unit/ ml for endoglucanase, in the following order: the pAGX1, pAGX2, and pAGX3. More than 70% of the endoxylanase and endoglucanase activities was found in the extracellular media.

Biochemical characterization of the lipid-binding properties of a broccoli cuticular wax-associated protein, WAX9D, and its application

  • Ahn, Sun-Young;Kim, Jong-Min;Pyee, Jae-Ho;Park, Heon-Yong
    • BMB Reports
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    • v.42 no.6
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    • pp.367-372
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    • 2009
  • In this study, we showed that WAX9D, a nonspecific lipid-transfer protein found in broccoli, binds palmitate (C16) and stearate (C18) with dissociation constants of 0.56 ${\mu}M$ and 0.52 ${\mu}M$, respectively. WAX9D was fused to thioredoxin protein by genetic manipulation to enhance its solubility. The data revealed strong interaction of Trx-WAX9D with palmitate and stearate. The dissociation constants of Trx-WAX9D for palmitate and stearate were 1.1 ${\mu}M$ and 6.4 ${\mu}M$, respectively. The calculated number of binding sites for palmitate and stearate was 2.5 to 2.7, indicating that Trx-WAX9D can bind three molecules of fatty acids. Additionally, Trx-WAX9D was shown to inhibit the apoptotic effect of palmitate in endothelial cells. Our data using Trx-WAX9D provide insight into the broad spectrum of its biological applications with specific palmitate binding.

Allergenicity of Hot Peppers Cultivated in Korea

  • Lee, Jeong-Ok;Kim, Eun-Jung;Ko, Yu-Jin;Lee, Sang-Il;Lee, Won-Sup;Ryu, Chung-Ho
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.317-322
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    • 2009
  • The proteins from 15 types of cultivar of hot peppers cultivated in Korea were extracted and its allergenicity was investigated by immunoblotting and enzyme-linked immunosorbent assay (ELISA). The immunoblotting of hot pepper proteins extracts (HPEs) against serum of hot pepper sensitized patients revealed dominant IgE binding to 14, 37, and 40 kDa molecules. The specific levels of IgE to HPEs sample No. 1, 3, and 7 were much higher than the other samples in patients. Also, IgE binding capacity of HPEs were not reduced by thermal processing and digestion in ELISA using human IgE antibody acquired from hot pepper sensitized patients. By means of Western blotting using anti-thaumatin IgY, thaumatin-like protein (TLP) acting as allergen in several plants and fruits was detected in tested hot peppers. This study demonstrates that the antigenic protein in hot peppers are present but are differently contained according to cultivars.

Human Acyl-CoA: Cholesterol Acyltransferase Inhibitory Effect of Flavonoids from Roots of Glycine max (L.) Merr

  • Lee, Jin-Hwan;Seo, Woo-Duck;Jeong, Seong-Hun;Jeong, Tae-Sook;Lee, Woo-Song;Park, Ki-Hun
    • Journal of Applied Biological Chemistry
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    • v.49 no.2
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    • pp.57-61
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    • 2006
  • Isoflavones 1-3 and pterocarpans 4-8 were isolated from methanol extract of roots of Glycine max. In inhibitory effect against human acyl-CoA:cholesterol acytransferase (ACAT)-1 and ACAT-2, glyceollin I 5 showed potent hACAT-1 ($IC_{50}=299.0{\mu}M$) and hACAT-2 ($IC_{50}=82.7{\mu}M$) inhibitory activities.

Temperature variation of the outer skin above specific acupoints induced by controlling mind : Pilot Study (조심법(調心法)을 통한 혈위의 체표온도변화 관찰 : Pilot Study)

  • Lee, Hwa-Jin;Chae, Youn-Byoung;Park, Hi-Joon;Baik, You-Sang;Yi, Seung-Ho;Lee, Hye-Jung
    • Korean Journal of Acupuncture
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    • v.24 no.3
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    • pp.55-65
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    • 2007
  • Qi intention. Temperature variations on the outer skin above measured at acupuncture points, PC8, LI4, and ST7. Results : The change of temperature in PC8 of the Qigong trainees were significantly higher than that of non-trainees ($0.97{\pm}0.20$ vs. $0.45{\pm}0.10$ respectively, p< 0.05 ). The change of temperature of the other acupoints areas was not significantly different between the two groups. Conclusions : Qi intention resulted in temperature change at the outer skin on the specific acupoints.

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Purification and Characterization of a Major Fibrinolytic Enzyme from Bacillus amyloliquefaciens MJ5-41 Isolated from Meju

  • Jo, Hyeon-Deok;Lee, Hwang-A;Jeong, Seon-Ju;Kim, Jeong-Hwan
    • Journal of Microbiology and Biotechnology
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    • v.21 no.11
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    • pp.1166-1173
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    • 2011
  • Meju is a traditional Korean fermented soy product used as a key element for soy sauce and doenjang. Bacilli with antimicrobial activity were isolated from meju prepared by traditional methods at Sunchang county, Jeollabukdo, Korea. Six isolates were identified as Bacillus amyloliquefaciens by recA gene sequencing and RAPD-PCR. One isolate, B. amyloliquefaciens MJ5-41, showed the strongest fibrinolytic activity. A 27 kDa active fibrinolytic enzyme, AprE5-41, was purified from the culture supernatant of MJ5-41 grown on LB by chromatographic methods. The optimum pH and temperature for purified AprE5-41 were 7.0 and $45^{\circ}C$, respectively. AprE5-41 quickly degraded $A{\alpha}$ and $B{\beta}$ chains but not the ${\gamma}$-chain of fibrinogen. AprE5-41 exhibited the highest specificity for N-succinyl-Ala-Ala-Pro-Phe p-nitroanilide, a known substrate for ${\alpha}$-chymotrypsin, cathepsin G, and subtilisin BPN'. The structural gene, aprE5-41, was cloned by PCR and successfully expressed in B. subtilis.

Confirmed cases of severe fever with thrombocytopenia syndrome in companion cats with a history of tick exposure in the Republic of Korea

  • Sun-Woo, Han;Ju-Hyun, An;Ji-Min, Rim;Eunseok, Jeong;Sungjun, Noh;Myoungdai, Kang;Jun-Gu, Kang;Joon-Seok, Chae
    • Journal of Veterinary Science
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    • v.23 no.6
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    • pp.83.1-83.7
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    • 2022
  • Severe fever with thrombocytopenia syndrome (SFTS) is a zoonotic disease, and its clinical information and prevalence are important. This study was conducted on 22 feline patients from the Republic of Korea (ROK), suspected to suffer from a tick-borne disease. Four cats were positive for SFTS, and genotypes B-1, B-3, D, and F were identified. Clinical symptoms, such as anorexia, jaundice, thrombocytopenia, leukopenia, and hyperbilirubinemia, were detected. This is the first report of SFTS virus genotypes B-1, D, and F from cats in the ROK. Moreover, our results suggest that jaundice may be an indicator of SFTS in cats.