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Synthesis and Antibacterial Evaluation of Some Novel 1,3,4-oxadiazol Derivatives Incorporated with Quinoline Moiety (Quinoline moiety를 가지고 있는 1,3,4-oxadiazol 유도체의 합성 및 항균활성)

  • Mandhane, Priyanka G.;Joshi, Ratnadeep S.;Khan, Wajid;Gill, Charansingh H.
    • Journal of the Korean Chemical Society
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    • v.55 no.4
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    • pp.656-661
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    • 2011
  • 5-(3,4,5-Triethoxyphenyl)-1,3,4-oxadiazole-2-thiol 6 on treatment with substituted 3-(bromomethyl)-2-chloroquinoline or 2-(p-tolyloxy)-3-(bromomethyl)quinoline 4a-j afforded the corresponding 3-((5-(3,4,5-triethoxyphenyl)-1,3,4-oxadiazol-2-ylthio)methyl)-2-chloroquinoline or 3-((5-(3,4,5-triethoxyphenyl)-1,3,4-oxadiazol-2-ylthio)methyl)-2-(p-tolyloxy)quinoline 7a-j, in the presence of $K_2CO_3$ and DMF under stirring at ambient temperature. All the synthesized compounds were further screened for their antibacterial activities. Some of our compounds showed excellent antibacterial activities against test organisms and reference standard.

The Corneal Base Curve, Astigmatism, and Power of Women College Students (여대생들의 각막기본 곡률, 난시, 굴절력)

  • Kim, Douk-Hoon;Choi, Ho-Seong
    • Journal of Korean Ophthalmic Optics Society
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    • v.6 no.2
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    • pp.53-57
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    • 2001
  • The corneal structure and function changes somewhat with aging. We were performed the analysis of women college students on the base curve, power, and astigmatism axis of the cornea by keratometer. All women subjects were between the ages of 19 and 20 years. On the corneal base curve. the right eye of the ages of 19 was 7.64 mm in vertical and 7.81 mm in horizontal. But, the left eye was 7.65 mm in vertical and 7.83 mm in horizontal on the other hand, the right and left eye of the ages of 20 was 7.72 mm in vertical and 7.75 mm in horizontal. On the corneal diopter power, the right eye of the ages of 19 was 44.21 diopter in vertical and 43.32 diopter in horizontal. But, the left eye was 44.23 diopter in vertical and 43.24 diopter in horizontal. On the other hand, the right eye of the ages of 20 was 43.67 diopter in vertical and 43.62 diopter in horizontal. But, the left eye was 43.73 diopter in vertical and 43.6 diopter in horizontal. According to the corneal astigmatism axis style, the right eye of the ages of 19 have 83% positive for with the rule astigmatism, and 16% positive for against the rule astigmatism. But, the left eye of the ages of 19 have 86% positive for with the rule astigmatism, and 12% positive for against the rule astigmatism. On the other hand, the right eye of the ages of 19 have 56% positive for with the rule astigmatism, and 44 % positive for against the rule astigmatism. But, the left eye of the ages of 20 have 56% positive for with the rule astigmatism, and 41% positive for against the rule astigmatism. According to the diopter power of corneal astigmatism. The right eye of the ages of 19 have 36% positive for behind 1 diopter and left eye have 31%. But, the right and left eye of the ages of 20 have 37.5%. The right and left eye of the ages of 19 have 42% positive for 1 diopter, and the right eye of the ages of 20 have 34.4% positive for 1 diopter and the left eye have 43.8%. The right eye of the ages of 19 have 12% positive for 2 diopter and left eye have 22%. But, the right eye of the ages of 20 have 15.6% positive for 2 diopter and the left eye have 12%. The right eye of the ages of 19 have 4% positive for 3 diopter and left eye have 3%. But, the left eye of the ages of 20 have 3% positive for 3 diopter and the left eye have 6%. On the other hand, the right eye of ages of 19 have 6% positive over 4 diopter, and the left eye have 2%. But, the right eye of ages of 20 have only 9% positive over 4 diopter.

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Silent Adenomas of Pituitary Gland : It's Immunohistochemical Features and Clinical Characteristics

  • Shim, Jae-Hyone;Song, Young-Jin;Kim, Dae-Chul;Park, Mi-Kyung;Choi, Sun-Seob;Kim, Ki-Uk
    • Journal of Korean Neurosurgical Society
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    • v.40 no.5
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    • pp.330-335
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    • 2006
  • Objective : The aim of the study was to review the clinical and radiological findings of those non-functioning adenomas[NFAs] with positive immnoreactivity for anterior pituitary hormones. Methods : Sixty patients with pituitary adenoma were treated at the author's institution between January 2000 and July 2005. All consecutive patients were underwent transsphenoidal surgery by same operator. In addition to the routine histopathological examination, surgical specimen was examined by immunohistochemical staining against adenohypophyseal cells. And clinical analysis was performed by retrospective review of medical records, neuroimaging examinations and immunohistochemical technique. We classified these pituitary adenomas into functioning adenomas [group F], immuno-positive NFAs [group S, so-called silent adenoma] and immuno-negative NFAs [group N], and compared clinical and radiological differences between group F, N, and S. Results : Of the 60 cases, group F was 25, group S was 25, and group N was 10. Among the group S, 5 cases showed reactivity against PRL, 1 against GH, 1 against both PRL and GH, 1 against TSH and GH, 2 against ACTH, 11 against FSH and 4 against both LH and FSH. Radiologically, invasiveness was noted in 8 in group S, compared to 3 in group N and 1 in group F [p = 0.02]. Intratumoral bleeding was noted in 7 of group S, 2 of group N and 2 of group F [p >0.05]. Conclusion : Silent adenomas were thought to behave more aggressive than other subgroups of pituitary adenomas. And so we suggest the immunohistochemical study against adenohypophyseal cells may be helpful for evaluating clinical course of pituitary adenoma, expecially for, NFAs.

Antibacterial Effect of Bacteria Isolated from the Plant Rhizosphere against Pathogenic Bacteria of Fish (식물근권에서 분리한 세균의 어류질병세균에 대한 항균활성 효과)

  • Jeong, Ji-Woon;Park, So-Hyun;Kim, Dong-Hwi;Jeun, Yong-Chull;Heo, Moon-Soo
    • Journal of Life Science
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    • v.24 no.7
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    • pp.757-761
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    • 2014
  • Olive flounder (Paralichthys olivaceus) is an important aquaculture fish species in Jeju Island, South Korea. Due to the intensification of flounder fish farming, huge amounts of chemical antibiotics are used against several fish diseases. This has many harmful side effects on fish, as well as human consumers. Hence, an alternative to chemical antibiotic agents is needed for disease control. In this study, three strains of rhizobacteria (BRH433-2, TRH415-2, and THJ609-3) were isolated from the rhizosphere of plants. Assays of their antibacterial activity against fish pathogens, such as S. iniae, S. parauberis, V. anguillarum, and E. tarda, were performed with untreated broth culture (without cell separation), supernatant, and precipitated pellets separated by centrifugation. Among these, the cell suspension prepared from the precipitated pellet showed significant antimicrobial activity when compared with that of the untreated broth culture and centrifugal supernatant. These results indicate that the three isolated rhizobacterial strains exhibit antibacterial activity. Analysis of the 16S rDNA sequences of the BRH-433-2, THJ609-3, and TRH415-2 strains showed the highest similarity to Burkholderia gladioli (99.5%), Pseudomonas baetica (97.7%), and P. koreensis and P. baetica (98.4%), respectively. We suggest that the strains hold promise in disease management of fish.

Cytotoxic Activity of the Inula japonica Extracts Against Several Human Cancer Cell Lines In Vitro (선복화 (Inula japonica)추출물의 암세포주에 대한 In Vitro 세포독성)

  • Cha, Mi-Ran;Kim, Ju-Young;Hwang, Ji-Hwan;Park, Hae-Ryong
    • Korean Journal of Pharmacognosy
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    • v.37 no.3
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    • pp.130-135
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    • 2006
  • The present study describes the preliminary evaluation of the cytotoxic activity of the extracts from Inula japonica. I. japonica was extracted with methanol, ethanol, acetone, and water, and then cytotoxic activity of these extracts were evaluated. The cytotoxic activity of each extract was assessed by the MTT-dye reduction assay. Both ethanol and acetone extracts from I. japonica showed the cytotoxic activity against the HT-29 human colon cancer cells. Furthermore, the ethanol extract was fractionated with n-hexane, diethyl ether, ethyl acetate, and water according to degree of Polarity, The diethyl ether fraction showed the highest cytotoxic activity against HT-29 cells, but the other fractions showed low cytotokic activity. In addition, diethyl ether layer also showed the cytotoxic activity against various tumor cells, such as human colon carcinoma SW620, human cervix adenocarcinoma HeLa, and human breast adenocarcinoma MCF-7 cells as well as HT-29 cells. These studies support that extracts of I. japonica may be a potential candidate as possible chemotherapeutic agent against human cancer.

Protective Effects of Bear Bile against Hepatotoxicity Induced by 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) in Mice (마우스에서 2,3,7,8-Tetrachlorodibenzo-p-dioxin(TCDD)에 의해 유발된 간독성에 대한 웅담의 방어효과)

  • Zhang, Hu-Song;Nam, Sang-Yoon;Kang, Jong-Koo
    • Korean Journal of Pharmacognosy
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    • v.32 no.2 s.125
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    • pp.121-127
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    • 2001
  • The effect of bear bile on 2,3,7,8-tetrachlorodibenzo- p-dioxin (TCDD)-induced hepatotoxicity was investigated in 6-week-old C57BL/6 male mice. Bear bile (100 mg/kg or 500 mg/kg) was administered orally daily for 4 weeks, respectively. From the second week, $10\;{\mu}g/kg$ of TCDD was administered to the bear bile-treated animals orally once a week for 3 weeks (a total of $30\;{\mu}g/kg$). There were no specific clinical findings and significant body weight changes in all groups. Although the livers in TCDD-treated mice appeared a severe hypertrophy and many necrotic foci, and changed to yellow-brown color in gross findings, these lesions were remarkably reduced by bear bile administration. The elevated serum activities of alanine transaminase, aspartate transaminase, alkaline phosphatase, and lactate dehydrogenase due to TCDD were significantly decreased by bear bile treatment (P<0.05). The lipid peroxidation induced by TCDD was significantly prevented by bear bile administration (P<0.05). In histological examinations, there were a moderate necrosis of hepatic cells around central veins, severe cytoplasmic vacuolizations, inflammatory cell infiltrations, and remarkable fatty changes in the liver of TCDD-treated animals. However, the lesions were dose-dependently inhibited by the bear bile treatments. These findings indicate that bear bile may have a protective effect against TCDD-induced hepatotoxicity in mice.

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Antifungal activities for derivatives of 4-isopropyl-3-methylphenol and 5-isopropyl-3-methylphenol against plant pathogenic fungi (4-Isopropyl, 5-isopropyl-3-methylphenol 유도체들의 합성과 식물 병원균에 대한 항균 활성)

  • Choi, Won-Sik;Jang, Soon-Ho;Jang, Do-Yeon;Choi, Kyoung-Gil;Lee, Byung-Ho;Kim, Tae-Jun;Jung, Bong-Jin
    • The Korean Journal of Pesticide Science
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    • v.10 no.4
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    • pp.249-261
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    • 2006
  • Fifty compounds such as ester, sulfonyl ester, carbamate, ether and phosphoyl ester derivatives of 4-isopropyl-3-methylphenol(I) and 5-isopropyl-3-methylphenol(II) were synthesized. These derivatives were identified by IR, GC/MS and $^1H$-NMR spectra. Their in vitro antifungal activities were tested against 10 plant pathogenic fungi. Among them, several compounds showed potent in vitro antifungal activity. The selected compounds showing potent in vitro antifungal activity were tested for their in vivo antifungal activities against 5 plant diseases such as rice blast, rice sheath blast, cucumber anthracnose, cucumber gray mold and tomato late blight. As a result, 4-isopropyl-3-methylphenyl(2-amino-thiazole-4-yl)methoxyiminoacetate(I-7a) showed a potent in vivo antifungal activity against rice blast. Both methyl (4-isopropyl-3-methylphenoxy)acetate(I-4d) and methyl (5-isopropyl-3-methylphenoxy)acetate(II-4d) effectively inhibited the development of cucumber gray mold.

Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.35 no.6
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    • pp.1681-1686
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    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Screening the Antibacterial Activities of Streptomyces Extracts against Phytopathogens Xanthomonas oryzae pathovar oryzae, Xanthomonas campestris pathovar vesicatoria, and Pectobacterium carotovorum pathovar carotovorum

  • Kim, Seung-Hwan;Cheng, Jinhua;Yang, Seung Hwan;Suh, Joo-Won;Song, Eun-Sung;Kang, Lin-Woo;Kim, Jeong-Gu
    • Journal of Applied Biological Chemistry
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    • v.58 no.3
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    • pp.253-258
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    • 2015
  • Xanthomonas oryzae pv. oryzae (Xoo), X. campestris pv. vesicatoria (Xcv), and Pectobacterium carotovorum pv. carotovorum (Pcc) are the causative agents of bacterial blight in rice, bacterial spot in pepper, and bacterial soft rot in carrot and cabbage, respectively. To isolate novel microbial extracts with antimicrobial activities against these bacteria, approximately 5,300 different Streptomyces extracts were prepared and tested. Microbial cultures from various Streptomyces strains isolated from the Jeju Island, Baekam, Mankyoung river, Jiri mountain etc. in Korea were extracted into three different factions -secreted hydrophobic, secreted hydrophilic, and mycelia- using ethyl acetate, water, and methanol. Initially, 34, 29, and 10 extracts were selected as having antibacterial activities against Xoo, Xcv, and Pcc, respectively. Extracts 1169G4, 1172E9, and 1172E10 had the highest growth inhibition activities against both Xoo and Xcv, and extracts 1151H7 and 1152H7 showed the highest growth inhibition activities against Pcc.

The Protective Effects of the Ethyl Acetate Fraction and Flavonoids from Taraxacum coreanum against Oxidative Stress in Neuronal Cells Induced by Hydrogen Peroxide and Amyloid Beta (흰민들레 Ethyl Acetate 분획물 및 Flavonoid 화합물의 Hydrogen Peroxide와 Amyloid Beta에 의한 신경세포의 산화적 스트레스 보호 효과)

  • Lee, Ah Young;Choi, Ji Myung;Lee, Sullim;Kim, Hyun Young;Lee, Sanghyun;Cho, Eun Ju
    • Korean Journal of Pharmacognosy
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    • v.44 no.3
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    • pp.263-268
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    • 2013
  • The protective role against oxidative stress under cellular system using C6 glioma cells was studied using the ethyl acetate (EtOAc) fraction, luteolin (1), and luteolin-7-glucoside (2) of Taraxacum coreanum. C6 glioma cells showed low cell viability and high generation of reactive oxygen species (ROS) by the treatment with generator of hydrogen peroxide ($H_2O_2$) and amyloid beta ($A{\beta}_{25-35}$). However, the treatment of the EtOAc fraction attenuated the cellular oxidative stress, resulting in significant elevation of cell viability. In addition, the production of ROS formation was also decreased by the treatment of the EtOAc fraction. Compounds 1 and 2 were isolated from the EtOAc fraction, and the protective effect was evaluated. Compounds 1 and 2 led to the increase of cell viability and decrease of production of ROS against oxidative stress by $H_2O_2$ and $A{\beta}_{25-35}$. The present study indicated that the EtOAc fraction, compounds 1 and 2 from T. coreanum demonstrated protective effects against oxidative stress, suggesting the preventive role against neurodegenerative diseases.