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Synergistic Effects of the Combination of 20-Hydroxyecdysone with Ampicillin and Gentamicin Against Methicillin-Resistant Staphylococcus aureus

  • Kim, Eun-Sook;Jeong, Seung-Il;Kim, Jung-Hoon;Park, Channy;Kim, Shin-Moo;Kim, Jin-Kyung;Lee, Kang-Min;Lee, Sang-Heon;So, Hong-Seob;Park, Ra-Kil
    • Journal of Microbiology and Biotechnology
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    • v.19 no.12
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    • pp.1576-1581
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    • 2009
  • The emergence of methicillin-resistant Staphylococcus aureus (MRSA) has led to an urgent need for the discovery and development of new antibacterial agents. As part of an ongoing investigation into the antibacterial properties of natural products, 20-hydroxyecdysone (20E), isolated from the roots of Achyranthes japonica Nakai, was found to be active against MRSA, either alone or in combination with ampicillin (AM) or gentamicin (GM), via checkerboard assay. This study investigated the antibacterial activity of 20E, which exhibited poor antibacterial activity ($MIC=250-500\;{\mu}g/ml$) against MRSA tested. The combined activity of AM or GE plus 20E against MRSA resulted in fractional inhibitory concentractions (FICs) ranging from 4.00 to $0.031\;{\mu}g/ml$, respectively. Meanwhile, the FIC index ranged from 0.16-4.50, indicating a marked synergistic relationship between AM, GE, and 20E against MRSA. Time-kill assays also showed a remarkable decrease between the combination and the more active compound. Therefore, this study demonstrated that AM, GE, and 20E can act synergistically in inhibiting MRSA in vitro.

Synergistic Effect of Flavonoids from Artocarpus heterophyllus Heartwoods on Anticancer Activity of Cisplatin Against H460 and MCF-7 Cell Lines

  • Daud, Nik Nurul Najihah Nik Mat;Septama, Abdi Wira;Simbak, Nordin;Bakar, Nor Hidayah Abu;Rahmi, Eldiza Puji
    • Natural Product Sciences
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    • v.25 no.4
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    • pp.311-316
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    • 2019
  • Artocarpus heterophyllus has been used as traditional medicine. This plant is one of the sources of flavonoid. Flavonoid compounds possessed a wide range of biological properties including anticancer. This study was performed to investigate the cytotoxic effect of flavonoids from A. heterophyllus on H460 and MCF-7 cell lines. The interaction of flavonoids and cisplatin against tested cancer cells was also evaluated. MTT assay was used to determine the cytotoxic effect of flavonoid. Isobologram analysis was selected to evaluate the synergistic effect between flavonoid and cisplatin, their interaction was then confirmed using AO/PI staining method. Amongst of flavonoid compounds, artocarpin exhibited strong cytotoxic effect on both MCF-7 and H460 cell lines with IC50 values of 12.53 ㎍/mL (28.73 μM) and 9.77 ㎍/mL (22.40 μM), respectively. This compound enhanced anticancer activity of cisplatin against H460 and MCF-7. The combination produced a synergistic effect on H460 and MCF-7 cell lines with a combination index (CI) values of 0.2 and 0.18, respectively. The AO/PI stained demonstrated that the combination of artocarpin and cisplatin caused morphological changes that indicated apoptosis. Moreover, artocarpanone also significantly increased cytotoxic effect of cisplatin compared to its single concentration with CI below than 1. This result suggested the potency of flavonoid named artocarpin to enhance the anticancer activity of cisplatin on H460 and MCF-7 cell lines.

Discovery of Epinastine-NSAID Hybrids as Potential Anti-inflammatory Agents: Synthesis and In Vitro Nitric Oxide Production Inhibitory Activity Study

  • Woo, Hyeong Ryeol;Damodar, Kongara;Lee, Yeontaek;Lim, Soon-sung;Jeon, Sung Ho;Lee, Jeong Tae
    • Journal of the Korean Chemical Society
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    • v.64 no.2
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    • pp.79-83
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    • 2020
  • A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC50) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC50), cytotoxicity concentration (CC50) and in vitro efficacy index (iEI), 6 (IC50 = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC50 = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.

Computerized Image Analysis of Micronucleated Reticulocytes in Mouse Bone Marrow (컴퓨터 이미지 분석법을 이용한 마우스 골수세포에서 소핵의 계수)

  • 권정;홍미영;고우석;정문구;이미가엘
    • Toxicological Research
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    • v.18 no.4
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    • pp.369-374
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    • 2002
  • The present study was performed to validate an automated image analysis system (Loats Automated Micronucleus Scoring System) for the mouse bone marrow micronucleus assay, comparing with conventional microscopic scoring. Two studies were conducted to provide slides for a comparison of micro-nucleated polychromatic erythrocytes (MNPCEs) values collected manually to those collected by the auto-mated system. Test article A was used as an example of a compound negative for the induction of micronuclei and test article B was wed as a micronucleus-inducing agent to elicit a positive response. Cyclophosphamide was included to provide an positive control in two studies. Bone marrow samples were collected 24 h after administration of test article A and B in male ICR mice. The cells were fixed with absolute methanol and stained with May-Grunwald and Giemsa. The number of MNPCEs was determined by the analysis of 1000 total PCEs per bone marrow sample. In addition to micronucleus scoring, an index of bone marrow toxicity based on PCE ratio (% of PCEs to total erythrocytes) was determined for each sample. The automated and manual scoring was similar when the MNPCEs incidence induced by each test article was less than 10. However manual scoring was able to effectively enumerate micronucleated PCEs in mouse bone marrow when MNPCEs incidence was more than 10, such as cyclophosphamide treatment. Conversely, PCE ratio was superior in computer-assisted image analysis. Taken together, it is suggested that improvement of the automated image analysis may be necessary to render the automatic scoring as sensitive as manual scoring for routine counting of micronuclei, especially because it is superior in objectivity and high throughput scoring.

The Quantitative Changes of Major Compounds from Aster koraiensis Nakai Essential Oil by Harvesting Time (수확 시기에 따른 벌개미취 정유의 주요 화합물 함량 변화)

  • Choi, Hyang-Sook
    • The Korean Journal of Food And Nutrition
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    • v.27 no.2
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    • pp.194-202
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    • 2014
  • This study investigates the chemical compositions of Aster koraiensis Nakai essential oils and the quantitative changes of major terpene compounds according to various harvesting times. The essential oils obtained by hydrodistillation from the aerial parts of Aster koraiensis Nakai are being analyzed by GC and GC-MS. The essential oil compositions of Aster koraiensis Nakai are characterized byhigher contents of sesquiterpene compounds. Ninety-seven volatile flavor compounds are being identified in the essential oils from Aster koraiensis Nakai harvested in 2010, and caryophyllene oxide (8.38%), aristolene (7.08%), epiglobulol (5.57%), and ethyl furanone (4.73%) are the most abundant compounds. Ninety-five compounds are identified in the essential oils from the plants harvested in 2011, and aristolene (11.56%), calarene (9.33%), phytol (8.28%), ethyl furanone (7.63%), and epiglobulol (7.18%) are the most abundant compounds. Ninety-five compounds are being identified in the essential oils from the plants harvested in 2012, and calarene (15.3%), aristolene (14.24%), ethyl furanone (7.21%), phytol (6.98%) are the major compounds. The contents of aristolene, ${\alpha}$-caryophyllene, ${\alpha}$-muurolene, ${\alpha}$-calacorene, aromadendrene oxide, and calarene increase significantly from 2010 to 2012. The contents of ${\alpha}$-cubebene, isocaryophyllene, and diepi-${\alpha}$-cedrene epoxide decrease significantly from 2010 to 2012. The quantitative changes of aristolene and calarene according to harvesting time can be served as a quality index of the Aster koraiensis Nakai essential oils.

Preparation of Mg(OH)2 Dispersion and its Application to PET Non-woven Textile as Flame Retardant Coating (수산화마그네슘 분산상의 제조와 PET 부직포 섬유의 난연 코팅제 적용)

  • Lim, Hyung-Mi;Hyun, Mi-Kyung;Jeong, Sang-Ok;Lee, Dong-Jin;Lee, Seung-Ho
    • Journal of the Korean Ceramic Society
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    • v.48 no.6
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    • pp.537-542
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    • 2011
  • Magnesium hydroxide as a non-halogen flame retardant has increasing attention due to its non-toxicity, high decomposition temperature and smoke suppressant ability during combustion. For the application of magnesium hydroxide retardant to the textile by soaking and coating method, the prerequisite for the coating is a small particle size, stable dispersion, and adhesion to the textile. The dispersion of $Mg(OH)_2$ particles and stability of the coating was checked by monitoring the change of transmittance and backscattering by varying the types of dispersion agents, binder, solvent, and $Mg(OH)_2$ source, and their compositions in the coating. The $Mg(OH)_2$ dispersion coating was applied to PET(poly(ethylene terephthalate)) non-woven textile. The physical properties are characterized by surface morphology, amount of coating, particle dispersion, and adhesion test. The flame retardant $Mg(OH)_2$ coated textile has been compared by limited oxygen index(LOI) and thermal gravimetry and differential scanning calorimetry(TG-DSC). It was found that phosphorous additive may give synergistic effect on $Mg(OH)_2$ flame retardant coating to make the flame retardant PET non-woven textile.

Inhibitory Effects of Low-Dose Aloe-Emodin on the Development of Colorectal Tumors in Min Mice

  • Shimpo, Kan;Chihara, Takeshi;Kaneko, Takaaki;Beppu, Hidehiko;Wakamatsu, Kazumasa;Shinzato, Masanori;Yukitake, Jun;Sonoda, Shigeru
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.14
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    • pp.5587-5592
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    • 2014
  • Aloe-emodin (AE), a natural anthraquinone compound, has been reported to exhibit anticancer activity in various cancer cell lines and anti-inflammatory effects in murine macrophages. In the present study, we investigated the cancer chemopreventive effects of AE in an Apc-deficient Min mouse model. In the first experiment, male Min mice were fed a basal diet or diets containing 5 ppm AE and 10 ppm AE for 12 weeks. The dietary administration of 5 ppm AE significantly reduced the number of colorectal tumors. In a second experiment, we investigated the effects of AE on colitis-related colon carcinogenesis in Min mouse treated with dextran sodium sulfate (DSS). Female Min mice were administered 1% DSS in their drinking water for 7 days. AE was given to mice in their diet at a dose of 5 or 50 ppm for 5 weeks. Feeding with AE significantly reduced the number of colorectal tumors. When proliferation of cells in normal-appearing colonic mucosa was assessed by monoclonal anti-rat Ki-67 antibody (MIB-5) immunohistochemistry in experiments 1 and 2, the AE treatment significantly decreased the mean MIB-5-labeling index. These results suggest that the dietary administration of low-dose AE may have chemopreventive effects against development of colorectal tumors in Min mice, possibly in part by reducing cell proliferation in colorectal mucosa.

Cr-doped Tialite Pigments (크롬을 사용한 Tialite계 안료)

  • Kim, Yeon-Ju;Lee, Byung-Ha
    • Korean Journal of Materials Research
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    • v.21 no.9
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    • pp.515-519
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    • 2011
  • The purpose of this study was to determine the optimal firing condition and composition for $Al_2TiO_5$ crystal, which is suitable for stable coloration in glazes at high temperatures, using $Cr_2O_3$ as chromophore for the synthesis of $Al_2TiO_5$ system pigments. $Al_2TiO_5$ has a high refractive index and good solubility of chromophore in the $Al_2TiO_5$ lattice, making this structure a good candidate for the development of new ceramic pigments. Pigments were synthesized by using $Al_2O_3$ and $TiO_2$ mainly. Various amounts of $Cr_2O_3$ such as 0.01, 0.02, 0.03, 0.04 and 0.05 mole were also added. Each compound was synthesized at $1300^{\circ}C$, $1400^{\circ}C$, and $1500^{\circ}C$ for 2 hours and cooled naturally. The crystal structure, solubility limit, and color of the synthesized pigments were analyzed by XRD, SEM, Raman spectroscopy, UV and UV-vis. The changes in color as the result of applying 6 wt% of the synthesized pigments to lime barium glaze were expressed as CIE-L*a*b* values. A $Cr_2O_3$ 0.03 mole doped $Al_2TiO_5$ brown pigment was successfully synthesize at $1400^{\circ}C$, and the values of CIE-L*a*b* parameters were L* = 44.62, a* = 3.10, and b* = 17.25. In the case of the pigment synthesized at $1500^{\circ}C$, the brown color was obtained at 0.01 mole and 0.02 mole $Cr_2O_3$, and the CIE-L*a*b* values were 55.34, 1.73, 28.64, and 49.39, 0.51, 21.33, respectively. At $1500^{\circ}C$, the maximum limit of solid solution was 0.03 mole $Cr_2O_3$. The glazed sample showed green color, and the values of the CIEL* a*b* parameters were L* = 45.69, a* = -0.98, and b* = 20.38.

Review of Clinical Research about Herbal Medicine Treatment on Recurrent Respiratory Tract Infection in Children (소아 반복성 호흡기 감염의 한약 치료에 대한 임상 연구 동향: 중의학 논문을 중심으로)

  • Lee, Ji Hong;Lee, Eun Ju;Lee, Bo Ram;Chang, Gyu Tae
    • The Journal of Pediatrics of Korean Medicine
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    • v.30 no.2
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    • pp.82-95
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    • 2016
  • Objectives The purpose of this study is to investigate recent clinical studies on effect of herbal medicine treatment for recurrent respiratory tract infection in children. Methods We searched some clinical studies about recurrent respiratory tract infection in children from the China Academic Journal (CAJ) of China National Knowledge Infrastructure (CNKI) (January 2011 to December 2015). Results 50 papers were selected from 168 studies. The herbal decoction was main herbal medicine treatment for recurrent respiratory tract infection in children. Commonly used herbs were Atractylodis Rhizoma Alba, Glycyrrhizae Radix, Astragali Radix, Saposhnikovia Radix and Pseudostellariae Radix. Yupingfeng keli was the most frequently used herbal compound. Total effective rate was 66.4-100%, experimental group was significantly higher than control group in 45 papers (P<0.05). Immune index (in 22 papers) and curative effect of TCM syndrome (in 7 papers) were significantly higher than those of control group after treatment (p<0.05). Conclusions Herbal medicine has been shown as an effective treatment on recurrent respiratory tract infection in children. These research results can be utilized in other clinical studies and in treatment of recurrent respiratory tract infection for children.

Construction of Amylolytic Industrial Brewing Yeast Strain with High Glutathione Content for Manufacturing Beer with Improved Anti-Staling Capability and Flavor

  • Wang, Jin-Jing;Wang, Zhao-Yue;He, Xiu-Ping;Zhang, Bo-Run
    • Journal of Microbiology and Biotechnology
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    • v.20 no.11
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    • pp.1539-1545
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    • 2010
  • In beer, glutathione works as the main antioxidant compound, which also correlates with the stability of the beer flavor. In addition, high residual sugars in beer contribute to major nonvolatile components, which are reflected in a high caloric content. Therefore, in this study, the Saccharomyces cerevisiae GSH1 gene encoding glutamylcysteine synthetase and the Saccharomycopsis fibuligera ALP1 gene encoding ${\alpha}$-amylase were coexpressed in industrial brewing yeast strain Y31 targeting the ${\alpha}$-acetolactate synthase (AHAS) gene (ILV2) and alcohol dehydrogenase gene (ADH2), resulting in the new recombinant strain TY3. The glutathione content in the fermentation broth of TY3 increased to 43.83 mg/l as compared with 33.34 mg/l in the fermentation broth of Y31. The recombinant strain showed a high ${\alpha}$-amylase activity and utilized more than 46% of the starch as the sole carbon source after 5 days. European Brewery Convention tube fermentation tests comparing the fermentation broths of TY3 and Y31 showed that the flavor stability index for TY3 was 1.3-fold higher, whereas its residual sugar concentration was 76.8% lower. Owing to the interruption of the ILV2 gene and ADH2 gene, the contents of diacetyl and acetaldehyde as off-flavor compounds were reduced by 56.93% and 31.25%, respectively, when compared with the contents in the Y31 fermentation broth. In addition, since no drug-resistant genes were introduced to the new recombinant strain, it should be more suitable for use in the beer industry, owing to its better flavor stability and other beneficial characteristics.