• Title/Summary/Keyword: Biological Synthesis

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THE STUDY ON EFFECTS OF THE PLATELET-DERIVED GROWTH FACTOR-AA, BB ON THE CELLULAR ACTIVITY OF THE HUMAN PERIODONTAL LIGAMENT CELLS (Platelet-derived growth factor-AA, BB가 치주인대세포의 세포활성에 미치는 영향에 대한 연구)

  • Oh, Sang-Deok;Lee, Jae-Mok;Suh, Jo-Young
    • Journal of Periodontal and Implant Science
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    • v.24 no.2
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    • pp.303-320
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    • 1994
  • Current acceptable methods For promotin gperiodontal regeneration are base on removal of diseased soft tissue, root treatment, guided tissue regeneration, inteoduction of new graft materials and biological mediators. Platelet-derived growth factor(PDGF) is one of polypeptide growth factor. PDGF has been reported as a biological mediator which regulates activities of wound healing process including the cell proliferation, migration and metabolism. The purposes of this study is to evaluate the effects of PDGF-AA, BB on the periodontal ligament cells to use as a regeneration promoting agent of periodontal tissue. Human periodontal ligament cells were prepared from the first premolar tooth extracted for the orthodontic treatment and were cultured in DMEM/10% FBS at the $37^{\circ}C$, 5% $CO_2$ incubator. Author measured the DNA synthesis, total protein, collagen and noncollagenous protein synthesis and alkaline phosphatase activity according to the concentration of PDGF-AA and BB(0, 0.1, 1, 10, 100ng/ml). The results were as follows : The DNA synthetic activity was increased dose dependently by PDGF-AA and BB. The maximum mitogenic effect was at the 100ng/ml of PDGF-AA and 10ng/ml of PDGF-BB. The total protein, collagen and noncollagen systhesis was increased dose dependently by PDGF-AA and BB. The % of collagen was slightly decresed according to the concentration of PDGF-AA and BB. The effect of PDGF-AA and BB were not specific for collagen synthesis since it also increased noncollagenous protein synthesis. The effect of PDGF-AA and BB on alkaline phosphatase activity did not show any significant, meanwhile the alkaline phosphatase activity of 14 days group showed significnat increase. In conclusion, PDGF-AA and BB may have important roles in stimulation of DNA synthesis in human periodontal ligament cells, which means an increase in collagen-synthesizing cells, and may be useful for clinical application in periodontal regenerative procedures.

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Phenotypic Suppression of Rad53 Mutation by CYC8 (CYC8에 의한 rad53 돌연변이의 표현형 억제에 대한 연구)

  • Park, Kyoung-Jun;Choi, Do-Hee;Kwon, Sung-Hun;Kim, Joon-Ho;Bae, Sung-Ho
    • Korean Journal of Microbiology
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    • v.46 no.2
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    • pp.122-126
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    • 2010
  • RAD53 functions as an effector kinase of checkpoint pathways in Saccharomyces cerevisiae, which plays a central role to regulate many downstream cellular processes in response to DNA damage. It also involves in transcriptional activation of various genes including RNR genes which encode the key enzyme required for dNTP synthesis. In this study, we identified CYC8 as a suppressor for the hydroxyurea sensitivity of $rad53{\Delta}$ mutation. $Rad53{\Delta}$ mutant transformed with a multi-copy plasmid containing CYC8 showed increased hydroxyurea resistance. In contrast, TUP1 which forms a complex with CYC8 did not function as a suppressor. In the case of mutations, both $cyc8{\Delta}$ and $tup1{\Delta}$ suppressed hydroxyurea sensitivity of $rad53{\Delta}$. Since CYC8 can propagate as a prion in yeast, overexpression of CYC8 induced misfolding of the normal CYC8 proteins, resulting in dominant cyc8-phenotype. Therefore, it is suggested that CYC8 can act as a multi-copy suppressor due to its prion property. It was observed that the levels of RNR transcription were increased in the yeast strains containing either multi-copies of CYC8 gene or $cyc8{\Delta}$ mutation, suggesting that the increased level of RNR will elevate the intracellular pools of dNTPs, which, in turn, suppress the phenotype of $rad53{\Delta}$ mutation.

Synthesis and Biological Evaluation of Novel 2-[Substituted acetly]-amino-5-alkyl]-amino-5-alkyl-1,3,4-thiadiazoles

  • Shakya, Ashok K.;Mishra, Pradeep;Patnaik, G.K.;Shukla, Rakesh;Srimal, R.C.
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.753-758
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    • 1998
  • Sixteen novel 2-substituted acetyl amino-5-alkyl-1,3,4-thiadiazol were synthesized and screened for their pharmacological activities. A few of the compounds namely 11, 12 and 16 showed anti-inflammatory activities comparable to phenylbutazone. Compound 12 also showed significan non-specific spasmolytic activity. Diuretic activity of compound 15 at a dose level of 90mg/kg p.o. was two fold higher compared to 50mg/kg p.o. of furosemide. Comparable diuresis was aso produced by compounds 9, 10, and 16.

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Structure Determination and Biological Activities of Elaiophylin Produced by Streptomyces sp. MCY-846

  • LEE, SANG-YONG;MI-SOON KIM;HANG-SUB KIM;YOUNG-HO KIM;SOON-DUCK HONG;JUNG-JOON LEE
    • Journal of Microbiology and Biotechnology
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    • v.6 no.4
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    • pp.245-249
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    • 1996
  • A cytotoxic compound, 8461 was isolated from the culture of Streptomyces sp. strain MCY846 by its cytotoxicity against gastric cancer cell line SNU-l. The IR, UV and NMR spectra of 8461 were identical to those of elaiophylin. This compound showed moderate cytotoxicity against several cell lines and exerted strong inhibitory effect on the synthesis of nitric oxide in the lipopolysaccharide stimulated-Raw 264.7 cells.

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Designing Inhibitor against Phospholipases A2 Enzyme through Inslico-Molecular Docking Studies

  • Ganapathy, Jagadeesan;Govindhan, Suresh;Sanmargam, Aravindhan
    • Journal of Integrative Natural Science
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    • v.7 no.3
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    • pp.159-165
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    • 2014
  • Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

Solvent Free Microwave Accelerated Synthesis of Heterocyclic Thiazolidin-4-ones as Antimicrobial and Antifungal Agents

  • Sekhar, Kondapalli Venkata Gowri Chandra;Rao, Vajja Sambasiva;Reddy, Aravalli Satish;Sunandini, Ravada;Satuluri, V S A Kumar
    • Bulletin of the Korean Chemical Society
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    • v.31 no.5
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    • pp.1219-1222
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    • 2010
  • A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3-yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.

Polymeric Nano-materials: Applications & Research Trends (고분자 나노 소재의 응용 및 연구 현황)

  • 박영준
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.28 no.2
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    • pp.55-57
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    • 2002
  • The fabrication, characterization and manipulation of nanosystems brings together physics, chemistry, materials science and biology in an unprecedented way, Phenomena occurring in such systems are fundamental to the workings of electronic devices, but also to living organisms. The ability to fabricate nanostructures is essential in the further development of functional devices that incorporate nanoscale features. Even more essential is the ability to introduce a wide range of chemical and materials flexibility into these structures to build up more complex nanostructures that can ultimately rival biological nanosystems. In this respect, polymers are potentially ideal nanoscale building blocks because of their length scale, well-defined architecture, controlled synthesis, ease of processing and wide range of chemical functionality that can be incorporated. In this presentation, we will look at a number of promising polymer-based nanofabrication strategies that have been developed recently, with an emphasis on those techniques that incorporate nanostructured polymers into devices and that exploit intrinsic polymer properties.

Biological Activity of Multifunctional Oligopeptide Derivatives

  • Kim, Bo Mi
    • Journal of Integrative Natural Science
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    • v.9 no.2
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    • pp.86-93
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    • 2016
  • The peptide sequences, GHK(Gly-His-Lys) and KTTKS(Lys-Thr-Thr-Lys-Ser), using a collagen stimulator recently were manipulated at N-terminal as a multifunctional peptide derivative with PEG(polyethyleneglycol) linker connected to gallic acid which presents anti-inflammatory activity. The multifunctional peptide derivatives were obtained in a normal peptide preparation method through SPPS(solid phase peptide synthesis) using Fmoc chemistry and a carboxyl group insertion reaction of PEG-3,4,5-triacetoxy benzoate by using potassium tert-butoxide and ethyl bromoacetate, which was separated by Sephadex DEAE. It gave a good compromise to a cosmetic application for cell cytotoxicity, anti-wrinkle, and anti-inflammation.

Synthesis and Biological Evaluation of N-(Aminopyridine) Benzamide Analogues as Histone Deacetylase Inhibitors

  • Zhang, Qing-Wei;Li, Jian-Qi
    • Bulletin of the Korean Chemical Society
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    • v.33 no.2
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    • pp.535-540
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    • 2012
  • A series of benzamide-based histone deacetylases (HDACs) inhibitors possessing N-(aminopyridine) residue as the zinc binding site of HDAC were synthesized and evaluated. Among these derivatives, compounds with N-(2-amino-4-pyridine) benzamide moiety have been found as the most potent ones. Moreover, introduction of appropriate substituents on the terminal aryl group acting as the surface-recognition domain could significantly improve the antiproliferative activity. In particular, the compound 4k possessed favorable pharmacokinetic characteristics and exhibited potent antitumor activity on xenograft model in mice at well tolerated doses, thus suggesting a good therapeutic index.

Synthesis of Biologically Active Chalcones and their Anti-inflammatory Effects

  • Jeon, Jae-Ho;Kim, Si-Jun;Kim, Cheol-Gi;Kim, Jin-Kyung;Jun, Jong-Gab
    • Bulletin of the Korean Chemical Society
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    • v.33 no.3
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    • pp.953-957
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    • 2012
  • Chalcones have been reported to have various biological activities including antitumor, antiparasitic, antileishmanial, antioxidative, superoxide scavenging, antibacterial, and PTP1B activity. Due to the limited natural resources, we had to prepare sizable quantities of biologically active chalcones for bio-tests. Therefore, Claisen-Schmidt condensation between substituted acetophenones and corresponding aldehydes enabled us to prepare chalcones for inflammatory studies. Chalcones thus prepared showed significant suppression of nitric oxide (NO) production at $10{\mu}M$.