• Title/Summary/Keyword: Analogues

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Development of Rapid Analytical Method of Forbidden Medicines in Dietary Supplements Using LC-ESI-Tandem MS (LC-ESI-tandem MS를 이용한 기능성표방식품 중 부정유해물질 신속검사체계 개발)

  • Kim, Hee-Yun;Jang, Young-Mi;Joo, Hyun-Jin;Jung, Young-Hyun;Lee, Myoung-Sook;Park, Jong-Seok;Lee, Kwang-Ho;Lee, Hwa-Mi
    • Korean Journal of Food Science and Technology
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    • v.39 no.4
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    • pp.372-379
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    • 2007
  • A high-performance liquid chromatography-electrospray ionization (HPLC-ESI) tandem MS was developed for the rapid and simultaneous determination of forbidden medicines in dietary supplements. Thirteen medicinal components such as PDE-5 inhibitors and their analogues, and the newly identified dimethylsildenafil and xanthoanthrafil, were included in this study. After tentative standardization of molecular ions in both polarities using thirteen references on the mass spectrometer, with ESI-continuous infusion via the syringe pump method, the relative intensity of the ions present in the resulting spectra was quantitatively compared. From the results, the ion mode was selected depending on each reference's characteristics. A HPLC method coupled with the ESI mode was developed considering the matrix effect and interference depending on the type of sample. The validation test of the developed method was followed by carrying out precision, accuracy, recovery, sensitivity and linearity, etc. The method showed sufficiently high sensitivity, reproducibility, and specificity, and produced 4 times faster results when compared with the existing HPLC/UV method for the determination of forbidden compounds in dietary supplements.

The Synthesis of the Stable IVDU Derivative for Imaging HSV-1 TK Expression (체내 안정형 HSV1-tk (Herpes Simplex Virus Type-1 Thymidine Kinase) 영상용 IVDU 유도체의 합성)

  • Kim, Eun-Jung;Choi, Tae-Hyun;Ahn, Soon-Hyuk;Kim, Byoung-Soo;Park, Hyun;Cheon, Gi-Jeong;Rhee, Hak-June;An, Gwang-Il
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.5
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    • pp.478-486
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    • 2009
  • Purpose: 5-iododeoxyuridine analogues have been exclusively developed for the potential antiviral and antitumor therapeutic agents. In this study, we synthesized carbocyclic radioiododeoxyuridineanalogue (ddIVDU) and carbocyclic intermediate as efficient carbocyclic radiopharmaceuticals. Materials and Methods: The synthesis is LAH reduction, hetero Diels-Alder reaction as key reactions including Pd(0)-catalyzed coupling reaction together with organotin. MCA-RH7777 (MCA) and MCA-tk (HSV1-tk positive) cells were treated with various concentration of carbocyclic ddIVDU, and GCV. Cytotoxicity was measured by the MTS methods. For in vitro uptake study, MCA and MCA-tk cells were incubated with 1uCi of [$^{125}I$]carbocyclic ddIVDU. Accumulated radioactivity was measured after various incubation times. Results: The synthesis of ddIVDU and precursor for radioiodination were achieved from cyclopentadiene in good overall yield, respectively. The radioiododemetallation for radiolabeling gave more than 80% yield with > 95% radiochemical purity. GCV was more toxic than carbocyclic ddIVDU in MCA-tk cells. Accumulation of [$^{125}I$]carbocyclic ddIVDU was higher in MCA-tk cells than MCA cells. Conclusion: Biological data reveal that ddIVDU is stable in vitro, less toxic than ganciclovir (GCV), and selective in HSV1-tk expressed cells. Thus, this new carbocyclic nucleoside, referred to in this paper as carbocyclic 2',3'-didehydro-2',3'-dideoxy-5- iodovinyluridine (carbocyclic ddIVDU), is a potential imaging probe for HSV1-tk.

Monitoring of Forbidden Medicines as Adulterants in Dietary Supplements Marketed Online by HPLC and ESI-tandom Mass Spectrometry (HPLC 및 ESI-tandom Mass Spectrometry를 이용한 인터넷에서 판매되는 기능성표방식품 중 부정유해물질 모니터링)

  • Lee, Yong-Cheol;Kim, Bog-Soon;Yun, Eun-Sun;Kim, Sung-Dan;Chang, Min-Su;Park, Young-Ae;Shin, Young;Jung, Sun-Ok;Lee, Jae-In;Chae, Young-Zoo
    • Korean Journal of Food Science and Technology
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    • v.44 no.2
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    • pp.148-154
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    • 2012
  • It was carried out to detect anti-impotence drug-like compounds, sibutramine and their analogues in dietary supplements, which are doubtful whether they include illegal compounds. A total of 51 food products were bought online and have been investigated. The separation was achieved on a C18 column, with the mobile phase made up of water (5 mM sodium hexanesulfonate and 0.1% phosphoric acid) and 95% acetonitrile, at a flow rate of 1.2 mL/min with gradient elution using by HPLC-DAD. The UV signals were monitored at 220 nm and 291 nm. LC-ESI-tandom MS was utilized to confirm that detected compounds in samples are the same as the reference materials. Two nutrient supplement foods and ginseng products were found to contain 1.3-82.1 mg of sildenafil, dimethylthiolsildenafil and pseudovardenafil per serving size. In addition, two other processed products were detected to contain 1.7 and 2.2 mg of didesmethylsibutramine, derived from sibutramine per serving size.

Effects of Vegetable Peptones on Promotion of Cell Proliferation and Collagen Production (Vegetable Peptones의 세포증식 및 콜라겐생성 촉진효과)

  • Jung, Eun-Sun;Lee, Jong-Sung;Lee, Jienny;Huh, Sung-Ran;Kim, Young-Soo;Hwang, Wang-Taek;Park, Deok-Hoon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.1
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    • pp.65-72
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    • 2009
  • Skin aging appears to be principally attributed to a decrease in both levels of Type I collagen and regeneration ability of dermal fibroblasts. It is important to introduce an efficient and safe agent for effective management of skin aging. To this end, we performed screening for anti-ageing agents and then found that vegetable peptones (pea and wheat) promoted cell proliferation of adult stem cells. Vegetable peptones may be considered as useful medium additives because it can supply nutrients, peptides, amino acids or growth factor analogues. This study was designed to investigate effects of vegetable peptones on cell proliferation/collagen production and their possible mechanisms in human dermal fibroblasts. In cell proliferation assay, vegetable peptones significantly promoted cell proliferation in a concentration-dependent manner. In addition, human COL1A2 promoter luciferase and type I procollagen synthesis assays showed that vegetable peptones induce type I procollagen production through the activation of COLlA2 promoter. In both TGF-${\beta}1$ luciferase reporter and ELISA assays, vegetable peptones was found to induce TGF-${\beta}1$ production, suggesting that vegetable peptones induce type I procollagen production through the activation of TGF-${\beta}1$. When applied topically in a human skin twice a day for an 4-week period of time, vegetable peptones did not induce any adverse reactions. Theretore, based on these results, we suggest the possibility that vegetable peptones may be considered as an attractive, wrinkle-reducing candidate for topical application.

Insecticidal Activity of Cinnamon Essential Oils, Constituents, and (E)-Cinnamaldehyde Analogues against Metcalfa pruinosa Say (Hemiptera: Flatidae) Nymphs and Adults (미국선녀벌레(Metcalfa pruinosa Say)에 대한 계피 정유 유래 물질의 살충 활성)

  • Kim, Jun-Ran;Jeong, In-Hong;Lee, Young Su;Lee, Sang-Guei
    • Korean journal of applied entomology
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    • v.54 no.4
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    • pp.375-382
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    • 2015
  • The insecticidal activity of the constituents of cinnamon essential oils and structurally related compounds against both the nymphs and adults of the citrus flatid planthopper Metcalfa pruinosa was examined using a direct-contact application. The toxicity of the cinnamon oil constituents and 21 (E)-cinnamaldehyde related compounds regarding the nymphs of M. pruinosa was evaluated using a leaf-dipping bioassay. Based on 24 h $LC_{50}$ values, hydro-cinnamic acid ($1.55mg/cm^2$) is the most toxic compound, followed by geranic acid ($1.59mg/cm^2$). The $LC_{50}$ values of 11 of the compounds including cinnamaldehyde are between $1.60mg/cm^2$ and $4.94mg/cm^2$. Low toxicities and no toxicity were observed with the other 15 ($5.24mg/cm^2$ to $13.47mg/cm^2$) and two compounds, respectively. Also, the toxicities of the cinnamon oil constituents and 21 cinnamaldehyde related compounds regarding the M. pruinosa adults were evaluated using a direct-spray method. The toxicity of eugenol (10.81 mg) is the most toxic compound for the adults of M. pruinosa, followed by geranic acid (30.68 mg). The $LC_{50}$ values of nine of the compounds including cinnamaldehyde are between 59.16 mg and 96.70 mg. Low toxicities and no toxicity were observed with the other 15 (105.44 mg to 255.76 mg) and three compounds, respectively. The spray formulations that comprise cinnamon bark and cinnamon green leaf oils resulted in 82.3% and 82.9% mortalities, respectively, toward the M. pruinosa adults in a ginseng field. Global efforts to reduce the level of highly toxic synthetic insecticides in agricultural environments justify further studies on cinnamon oils to ascertain whether the corresponding active principles can act as insecticides, when they are applied as a direct spray with contact action, for the control of M. pruinosa populations.

A comparative study on the accuracy of impression body according to the types of impression tray (임플란트 인상 채득 시 트레이 종류에 따른 인상체의 정확도에 관한 비교 연구)

  • Yi, Hyun-Jung;Lim, Jong-Hwa;Lee, Joon-Seok
    • The Journal of Korean Academy of Prosthodontics
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    • v.48 no.1
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    • pp.48-54
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    • 2010
  • Purpose: The objective of this study was to evaluate and compare the accuracy of impression body taking by the closed and the open tray impression technique with 3 types of impression tray. Individual tray, metal stock tray and polycarbonate tray were used. Materials and methods: Nine closed tray impressions were taken by individual tray, metal stock tray and polycarbonate stock tray, respectively with polyether impression material. 9 open tray impressions were also acquired by same manner. Precision analysis on the master models was performed by attaching the reference frameworks with alternate single screws and measuring the vertical fit discrepancy of respective analogues in working cast with a stereo microscope. Data were analyzed by 1 way ANOVA and independent t-test. Results: The average fit accuracy of impression bodies was calculated. With the closed tray impression technique, there were significant statistical differences in vertical fit discrepancy according to the types of tray. The individual tray group showed the lowest value and the polycarbonate stock tray group represented the highest. With the open tray impression technique, there was no significant difference in vertical fit discrepancy. Significant statistical difference in vertical fit discrepancy was found between the open and the closed impression technique with the polycarbonate stock tray. Conclusion: From the results above, more precise impressions could be acquired by the rigid individual tray compared with the polycarbonate stock tray. It was hard to get consistent accuracy impressions by the closed tray impression technique with polycarbonate stock trays.

Comparative accuracy of new implant impression technique using abutments as impression copings with an angulated implant model (경사지게 식립된 임플랜트 모형에서 지대주를 인상용 코핑으로 이용한 새로운 인상법의 정확성 비교 연구)

  • Lee, Hyeok-Jae;Kim, Chang-Whe;Lim, Young-Jun;Kim, Myung-Joo
    • The Journal of Korean Academy of Prosthodontics
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    • v.46 no.2
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    • pp.201-208
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    • 2008
  • Statement of problem: A new implant impression technique which use abutments as impression coping, and use resin cement as a splinting material was described. Accuracy of this technique was compared with conventional closed tray and resin splinted open tray technique for a $15^{\circ}$ angled 3-implant model Material and methods: A dental stone master model with 3 linearly positioned implant analogue and a reference framework which was passively fitted to it were fabricated. The center analogue was perpendicular to the plane of model and the outer analogues had a $15^{\circ}$angulation forward or backward. 10 closed tray impressions, 10 resin splinted open tray impressions, 10 abutment-resin framework cementation impressions and 10 abutment-metal framework cementation impressions were made with additional silicone material and poured with dental stone. A light microscope with image processing was used to record the vertical gap dimension between reference framework and analogue of duplicated cast made with each 4 impression techniques. Statistical analysis used one-way ANOVA with post-hoc tests Tukey test of .05 level of significance Results: Significant difference in the vertical gap dimension was found between closed tray technique; 74.3 (${\pm}33.4$)${\mu}m$ and resin splinted open tray technique, and two other new technique. (P<.05) Abutment-metal framework cementation technique;42.5 (${\pm}11.9$)${\mu}m$ was significantly different from resin splinted open tray technique. (P<.05) Abutmentresin framework cementation technique;51.0 (${\pm}14.1$)${\mu}m$ did not differ significantly from resin splinted open tray technique;50.3 (${\pm}16.9$)${\mu}m$. (P>.05) Conclusion: Within limitations of this study, the accuracy of implant level impressions of resin splinted open tray technique was superior to that of closed tray technique. A new technique using abutment and metal framework cementation was more accurate than resin splinted open tray technique.

Cytoprotective Effects of Schisandrin A against Hydrogen Peroxide-induced Oxidative Stress in SW1353 Human Chondrocytes (SW1353 인간 연골세포에서 산화적 스트레스에 대한 schisandrin A의 세포 보호 효과)

  • Jeong, Jin-Woo;Choi, Eun Ok;Kwon, Da Hye;Kim, Bum Hoi;Park, Dong Il;Hwang, Hye Jin;Kim, Byung Woo;Choi, Yung Hyun
    • Journal of Life Science
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    • v.27 no.9
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    • pp.1070-1077
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    • 2017
  • Chondrocyte apoptosis induced by reactive oxygen species (ROS) plays an important role in the pathogenesis of osteoarthritis. Schisandrin A, a bioactive compound found in fruits of the Schisandra genus, has been reported to possess multiple pharmacological and therapeutic properties. Although several studies have described the antioxidant effects of analogues of schisandrin A, the underlying molecular mechanisms of this bioactive compound remain largely unresolved. The present study investigated the cytoprotective effect of schisandrin A against oxidative stress (hydrogen peroxide [$H_2O_2$]) in SW1353 human chondrocyte cells. The results showed that schisandrin A preconditioning significantly inhibited $H_2O_2-induced$ growth inhibition and apoptotic cell death by blocking the degradation of poly (ADP-ribose) polymerase proteins and down-regulating pro-caspase-3. These antiapoptotic effects of schisandrin A were associated with attenuation of mitochondrial dysfunction and normalization of expression changes of proapoptotic Bax and antiapoptotic Bcl-2 in $H_2O_2-stimulated$ SW1353 chondrocytes. Furthermore, schisandrin A effectively abrogated $H_2O_2-induced$ intracellular ROS accumulation and phosphorylation of histone H2AX at serine 139, a widely used marker of DNA damage. Thus, the present study demonstrates that schisandrin A provides protection against $H_2O_2-induced$ apoptosis and DNA damage in SW1353 chondrocytes, possibly by prevention of ROS generation. Collectively, our data indicate that schisandrin A has therapeutic potential in the treatment of oxidative disorders caused by overproduction of ROS.

The comparison of predicted adult height change and height gain after gonadotropin-releasing hormone agonist and combined growth hormone treatment in girls with idiopathic central precocious puberty (진성 성조숙증으로 진단 받은 여아에서 gonadotropin-releasing hormone agonist 단독치료 및 growth hormone의 병합치료 시 예측 성인키의 변화 및 성장 획득의 비교)

  • Seo, Ji-Young;Yoon, In-Suk;Shin, Choong-Ho;Yang, Sei-Won
    • Clinical and Experimental Pediatrics
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    • v.49 no.3
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    • pp.305-311
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    • 2006
  • Purpose : GnRH analogues(GnRHa) are used to treat central precocious puberty(CPP). However, in some patients, the GV decrease is so remarkable that it impairs predicted adult height(PAH); and there fore, the addition of growth hormone(GH) is suggested. We analysed the growth changes during two years and final adult height(FAH) in girls with idiopathic CPP treated with combined therapy, compared with those of girls treated with GnRHa alone. Methods : For the analysis, we classified the patients, who was treated for longer than two years, into three groups depending on the initial PAH and combination of GH; PAH_L, treated with GnRHa and PAH less than midparental height(MPH) - 5 cm. PAH_H, treated with GnRHa and PAH greater than MPH - 5 cm. GnRHa+GH, combined GH treatment, regardless of PAH before treatment. We analysed the GV and PAH change during the first two years and FAH. Results : In PAH_L, the PAH(SDS) at first year of therapy was significantly increased to $153.5{\pm}6.5cm(-1.4{\pm}1.3)$ from $149.7{\pm}6.4cm(-2.1{\pm}1.3)$ before treatment(P=0.004). In PAH_H, there was no significant increase in PAH during the two years of treatment. During the first year of combination of GH and GnRHa, GV and PAH increased significantly. We observed significant increases in FAH, comparing to the initial PAH in the PAH_L and GnRHa+GH groups. The height gains(FAH - initial PAH) were significantly higher in the PAH_L and GnRHa+GH groups than that in the PAH_H group. Conclusion : This study suggests the FAH and height gains are improved in patients, whose predicted adult height before treatment was shorter than those with higher predicted adult height, with the treatment of GnRHa alone or in combination with GH. GH could not improve the final adult height, but compensated the growth in patients whose growth velocity was decelerated by GnRHa alone.