• Title/Summary/Keyword: Biological Synthesis

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Study on the Effects of Phenyldiazenylanilines on the Activation of Arylhydrocarbon Receptor (Phenyldiazenylaniline 유도체가 방향족탄화수소 수용체의 활성에 미치는 영향)

  • Lee, Hyosung
    • Journal of the Korea Convergence Society
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    • v.10 no.1
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    • pp.285-290
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    • 2019
  • AHR regulates the expression of xenobiotics metabolizing enzymes (XMEs) as a transcription fact upon binding of ligands that are mainly aryl hydrocarbons. The role of AHR in human physiology has been intensively investigated for the past decades, however our understanding on AHR yet to be elucidated largely due to the lack of proper chemical agents. It has been demonstrated that AHR correlates to pathogenesis for some diseases in recent studies suggesting that the study on the AHR may provide a valid therapeutic target. Classical antagonists in current use are reported to be partially agonistic whereas a pure antagonist is yet to be found. In this study, phenyldiazenylaniline has been designed based on the structure of two known AHR antagonist, Resveratrol and CH223191. The derivatives of phenyldiazenylaniline have been prepared and subjected to assessment as an AHR antagonist in order to optimize the AHR antagonistic activity of the designed structure by means of convergence study of organic synthesis and molecular biology.

The application of multifunctional metal oxide for wastewater treatment: Adsorption and disinfection (다기능 금속산화물의 하수처리 적용-흡착 및 살균)

  • Kim, Heegon;Park, Duckshin;An, Byungryul
    • Journal of Korean Society of Water and Wastewater
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    • v.33 no.4
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    • pp.251-258
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    • 2019
  • The physical treatment such as chemical precipitation or adsorption was usually added after biological treatment in wastewater treatment process since it was enforced to reduce the concentration of phosphate for wastewater effluent to 0.2 mg/L as P which was well known as one of main nutrient causing eutrophication in waterbody. Therefore, the new material functioned for both adsorption and disinfection was prepared with Fe and Cu, and $TiO_2$, respectively, by changing the ratio of concentration referred to tri-metal (TM). According to SEM-EDS, $TiO_2$ was 30~40% composition for any TM regardless of any synthesis condition. However, the ratio of composition for Fe and Cu was dependent on the initial Fe and Cu concentration, respectively. The removal efficiency of phosphate was obtained to 15% at low initial concentration and the maximum uptake (Q) was calculated to ~11 mg/g through Langmuir isotherm model using TM1 which was synthesized at 1000 mg/L, 1000 mg/L, and 2 g (10 g/L) for $Fe(NO_3)_3$, $Cu(NO_3)_2$, $TiO_2$, respectively. In disinfection test, the efficiency of virus removal using TM was increased with increase of dosage of TM and can be reached 98% at 0.2 g.

Synthesis and biological evaluation of tricarbonyl technetium labeled 2-(4-chloro)phenyl-imidazo[1,2-a]pyridine analog (99mTc-CB257) as a TSPO-binding ligand

  • Choi, Ji Young;Jung, Jae Ho;Song, In Ho;Moon, Byung Seok;Lee, Byung Chul;Kim, Sang Eun
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.4 no.2
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    • pp.73-79
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    • 2018
  • In our previous study, tricarbonyl $^{99m}Tc$-labeled TSPO-binding ligand, named $^{99m}Tc$-CB256, having positively charge (+1) was investigated but did not show promising results in in vivo environment despite of a nanomolar binding affinity for TSPO. Because the overall positively charge of $^{99m}Tc$-CB256 would likely interrupt its target protein uptake, we herein designed the neutral tricarbonyl-$^{99m}Tc$ labeled TSPO-binding ligand ($^{99m}Tc$-CB257, 1). $^{99m}Tc$-CB257 was prepared by the facile incorporation of the $[^{99m}Tc(CO)_3]^+$ into a N-(hydroxycarbonylmethyl)-2-picoly moiety in CB257. The radiochemical yield of $^{99m}Tc$-CB257 after HPLC purification was $54.1{\pm}2.4%$ (decay corrected, n = 3). The authentic Re-CB257 (2) was synthesized by using $(NEt_4)_2[Re(CO)_3Br_3]$ in 69.0% yield. The binding affinity of 2 for TSPO was measured in leukocyte and showed approximately 280 times higher than that observed for the positively charged (+1) ligand, Re-CB256 ($K_i=0.57{\pm}0.06nM$ versus $159.3{\pm}8.7nM$, respectively). Our results indicated that 1 can be considered potentially as a new SPECT radiotracer for TSPO-rich cancer and provides the foundation for further in vivo evaluation related with abnormal TSPO-overexpression environments.

Apoptosis and inhibition of human epithelial cancer cells by ZnO nanoparticles synthesized using plant extract

  • Koutu, Vaibhav;Rajawat, Shweta;Shastri, Lokesh;Malik, M.M.
    • Advances in nano research
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    • v.7 no.4
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    • pp.233-240
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    • 2019
  • The present research work reports in-vitro anti-cancer activity of biologically synthesized ZnO nanoparticles (ZnO NPs) against human carcinoma cells viz SCC-40, SK-MEL-2 and SCC-29B using Sulforhodamine-B (SRB) Assay. ZnO NPs were synthesized by a unique and novel biological route using Temperature-gradient phenomenon where the extract of combination of Catharanthus roseus (L.) G. Don (C. roseus), Azadirachta indica (A. indica), Ficus religiosa (F. religiosa) and NaOH solution were used as synthesis medium. The morphology of the ZnO NPs was characterized by Transmission Electron Microscopy (TEM). TEM images reveal that particle size of the samples reduces from 76 nm to 53 nm with the increase in reaction temperature and 68 nm to 38 nm with the increase in molar concentration of NaOH respectively. XRD study confirms the presence of elements and reduction in crystallite size with increase in reaction temperature and NaOH concentration. The diffraction peaks show broadening and a slight shift towards lower Bragg angle ($2{\theta}$) which represents the reduction in crystallite size as well as presence of uniform strain. The FTIR spectra of the extract show transmittance peak fingerprint of Zn-O bond and presence of bioactive molecules These NPs exhibit inhibition greater than 50% for SCC-40, SK-MEL-2 and SCC-29B cell lines and more than 50% cell kill for SCC-29B cells at concentrations < $80{\mu}g/ml$. Nanoparticles with smallest size have shown better anti-cancer activity and peculiar cell-selectivity. The combination of extracts of these plants with ZnO NPs can be used in targeted drug delivery as an effective anti-cancer agent, a potential application in cancer treatment.

Korean Red Ginseng and Portulaca oleracea Extracts Attenuate Lipopolysaccharide-induced Inflammation via Downregulation of Nuclear Factor Kappa-B and the Mitogen-activated Protein Kinase Signaling Pathway in Macrophage Cell Line RAW 264.7

  • Ullah, HM Arif;Kim, Tae-Hwan;Saba, Evelyn;Kim, Sung Dae;Rhee, Man Hee
    • Biomedical Science Letters
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    • v.27 no.2
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    • pp.51-58
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    • 2021
  • Korean red ginseng (Panax ginseng Meyer) is a well-known traditional medicine, with numerous biological functions in the body. Portulaca oleracea (P. ole) belongs to the Portulacaceae family and has bioactive potential as a traditional medicine. This study aimed to determine the anti-inflammatory effects of Korean red ginseng extract (RGE) and P. ole extract on lipopolysaccharide (LPS)-treated RAW 264.7 cells. The combination of RGE (50 ㎍/mL) and P. ole (6.25 ㎍/mL) extracts significantly suppressed LPS-induced nitric oxide synthesis. The expression of proinflammatory mediators, including inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and proinflammatory cytokines, including interleukin-1β, interleukin-6, and tumor necrosis factor-α, were markedly decreased by the combined treatment with RGE (50 ㎍/mL) and P. ole (6.25 ㎍/mL). Moreover, iNOS and COX-2 protein expression levels were also significantly reduced in the combined treatment compared to the LPS-stimulated group. In addition, the nuclear translocation of phosphorylated nuclear factor kappa-B was suppressed by the treatment with RGE and P. ole. Moreover, the mitogen-activated protein kinase pathway was also partially inhibited by the combination treatment with RGE and P. ole. Our results demonstrate that the treatment mixture with RGE and P. ole could be used as functional food and therapeutic herbal medicine in various inflammatory diseases.

The Development and Trend of Eco-Friendly Water-Dispersible Polyurethane Field. (친환경 수분산 폴리우레탄 분야의 개발과 발전 동향)

  • Lee, Joo-Youb
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.6
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    • pp.1533-1542
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    • 2021
  • Eco-friendly polyurethane can be defined as a highly utilized material used in various fields. The various structural properties of the synthesis of isocyanates and polyols provide versatility and customization for use in the manufacturing field. The characteristics of polyurethane vary widely from soft touch coatings to hard building materials like rocks. These mechanical, chemical and biological properties and ease of alignment are drawing tremendous attention not only in the field of research but also in related industries. In order to improve the performance of water-dispersible polyurethane materials, it can be derived through processes such as adjusting the blending of raw materials and adding additives and nanomaterials. This study highlights the basic chemical structure of eco-friendly water-dispersible polyurethane in the fields of medical science, automobiles, coatings, adhesives, paints, textiles, marine industries, wood composite materials, and clothing.

Anti-Melanogenic Effect of Thymol, a Major Odorant in Essential Oils of Family Lamiaceae (꿀풀과 식물 정유의 주성분인 Thymol의 미백활성에 관한 연구)

  • Choi, Deok-Gyun;Park, Chan Ik;Lee, Sun-Mi;Baek, Jeong-In
    • The Korea Journal of Herbology
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    • v.34 no.4
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    • pp.19-25
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    • 2019
  • Objectives : Thymol (2-isopropyl-5-methylphenol), a natural monoterpenoid phenol, is one of the major odorant constituents found in natural essential oils of various herbal plants, such as Thymus quinquecostatus and Thymus vulgaris. Multiple biological activities of thymol, including antioxidative, antimicrobial, and anti-inflammatory effects, have been reported in numerous in vitro studies, and recently it was suggested that thymol may could inhibit oxidization of L-dihydroxyphenylalanine (L-DOPA) to dopaquinone required in melanogenesis pathway, as an antioxidant. Methods : MTT assay was performed to test the cytotoxic effect of thymol in B16F10 cells. Inhibitory effect of thymol to tyrosinase activities were examined using both mushroom tyrosinase and intracellular tyrosinase. Expression level of tyrosinase in B16F10 cells were investigated by western blot analysis. Results : The cell viability was decreased by thymol treatment in dose-dependant manner, leading significant cytotoxicity in 500 and $1000{\mu}M$ thymol-treated groups. In the alpha-melanocyte stimulating hormone (${\alpha}$-MSH)-induced melanogenesis, administration of thymol significantly decreased extracellular (secreted) melanin content in dose-dependent manner. Cellular tyrosinase activity assay and western blot analysis of intracellular tyrosinase showed that thymol has a strong anti-melanogenic effect by inhibition of tyrosinase activity and by decreasing expression of tyrosinase that contribute to melanin synthesis in the B1610 cells. Conclusions : As the first functional study that prove anti-melanogenic effect of thymol and its underlying mechanism in the living cells, our study suggests the applicability of fragrance as the functional materials of cosmetics or health supplement, not as just an additive.

Synthesis of Hyaluronic Acid Microsphere Crosslinked with Polyethylene Glycol Diglycidyl Ether Prepared by A Simple Fluidic Device

  • Yuk, Sujeong;Jeong, Dayeon;Lee, Yongjun;Lee, Deuk Yong
    • Journal of Biomedical Engineering Research
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    • v.42 no.6
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    • pp.251-258
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    • 2021
  • Hyaluronic acid (HA) microspheres (MSs) crosslinked with polyethylene glycol diglycidyl ether (PEGDE) are prepared using a simple fluidic device (SFD) to investigate the optimized parameters. A solution mixture of PEGDE in 2-methyl-1-propanol was prepared as a continuous phase in SFD. HA solutions of 1 wt% concentration were introduced into SFD as a discontinuous phase. The HA solution prepared by stirring for more than 48 h exhibited spherical MSs at the needle tip inside the ring cap. As the flow rate of the continuous phase increased from 0.7 to 1.9 mL/min, the diameter of the MS decreased from 173±36 ㎛ to 129±13 ㎛. Although the PEGDE concentration in the range of 0.2 to 1.8 vol% did not affect the diameter of the MS, the microstructure of MS, consisting of inner hollow void and wall, was changed. The inner void and wall size decreased and increased from 79.5 ㎛ to 57.2 ㎛ and from 10.3 ㎛ to 21.4 ㎛, respectively, with increasing PEGDE concentration from 0.2 vol% to 1.8 vol%. FT-IR peaks located around 2867 cm-1 and 1088 cm-1 indicated that the HA MS prepared at different PEGDE concentrations were chemically crosslinked. The HA MSs containing different PEGDE concentrations exhibited quantitative cell viability of more than 98%. L-929 cells adhered well to the HA MSs and proliferated continuously with increasing culture time to 48 h regardless of PEGDE concentration, implying that the HA MSs are clinically safe and effective.

Synthesis of Titanate Nanotubes Via A Hydrothermal Method and Their Photocatalytic Activities

  • Kim, Ye Eun;Byun, Mi Yeon;Lee, Kwan-Young;Lee, Man Sig
    • Clean Technology
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    • v.28 no.2
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    • pp.147-154
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    • 2022
  • Titanate nanotubes (TNTs) were synthesized via alkaline hydrothermal treatment using commercial TiO2 nanoparticles (P25). The TNTs were prepared at various TiO2/NaOH ratios, hydrothermal temperatures, and hydrothermal times. The synthesized catalysts were characterized by X-ray diffraction, field-emission scanning electron microscopy, N2 adsorption-desorption isotherms, field-emission transmission electron microscopy, and ultraviolet-visible spectroscopy. TNTs were generated upon a decrease in the TiO2/NaOH ratio due to the dissolution of TiO2 in the alkaline solution and the generation of new Ti-O-Ti bonds to form titanate nanoplates and nanotubes. The hydrothermal treatment temperature and time were important factors for promoting the nucleation and growth of TNTs. The TNT catalyst with the largest surface area (389.32 m2 g-1) was obtained with a TiO2/NaOH ratio of 0.25, a hydrothermal treatment temperature of 130 ℃, and a hydrothermal treatment time of 36 h. Additionally, we investigated the photocatalytic activity of methyl violet 2B (MV) over the TNT catalysts under UV irradiation and found that the degradation efficiencies of the TNTs were higher than that of P25. Among the TNT catalysts, the TNT catalyst that was hydrothermally synthesized for 36 h (TNT 36 h) exhibited a 96.9% degradation efficiency and a degradation rate constant that was 4.8 times higher than P25 due to its large surface area, which allowed for more contact between the MV molecules and TNT surfaces and facilitated rapid electron transfer. Finally, these results were correlated with the specific surface area.

Synthesis of a PEGylated tracer for radioiodination and evaluation of potential in tumor targeting

  • Abhinav Bhise;Sushil K Dwivedi;Kiwoong Lee;Jeong Eun Lim;Subramani Rajkumar;Woonghee Lee;Seong Hwan Cho;Jeongsoo Yoo
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.2
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    • pp.79-84
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    • 2021
  • Radiopharmaceuticals are important for tumor diagnosis and therapy. To deliver a radiotracer at the desired target excluding non-targeted tissues is difficult The development of a targeted tracer that has a good clearance profile while maintaining high biostability and biocompatibility is key to optimizing its biodistribution and transport across biological barriers. Improving the hydrophilicity of radiotracers by PEGylation can reduce serum binding, allowing the tracer to circulate without retention and reducing its affinity for non-targeted tissues. In this study, we synthesized a new benzamido tracer (SnBz-PEG36) with the introduction of a low molecular weight polyethylene glycol unit (PEG36, ~2,100 Da). The tumor targeting efficiency and biodistribution of [131I]-Bz-PEG36 or radiotracer-loaded liposomes were evaluated after their administration to normal mice or mouse tumor models including CT26 (xenograft) and 4T1 (xenograft and orthotopic). Most of the radiotracer was cleared out rapidly (1-24 h post-administration) through the kidney and there was little tumor uptake.