• Title/Summary/Keyword: p-derivative

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Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana

  • Kim, Mi Seon;Lee, Yunmi;Sung, Gi-Ho;Kim, Ji Hye;Park, Jae Gwang;Kim, Han Gyung;Baek, Kwang Soo;Cho, Jae Han;Han, Jaegu;Lee, Kang-Hyo;Hong, Sungyoul;Kim, Jong-Hoon;Cho, Jae Youl
    • Biomolecules & Therapeutics
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    • v.23 no.4
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    • pp.367-373
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    • 2015
  • Cordyceps species including Cordyceps bassiana are a notable anti-cancer dietary supplement. Previously, we identified several compounds with anti-cancer activity from the butanol fraction (Cb-BF) of Cordyceps bassiana. To expand the structural value of Cb-BF-derived anti-cancer drugs, we employed various chemical moieties to produce a novel Cb-BF-derived chemical derivative, KTH-13-amine-monophenyl [4-isopropyl-2-(1-phenylethyl) aniline (KTH-13-AMP)], which we tested for anti-cancer activity. KTH-13-AMP suppressed the proliferation of MDA-MB-231, HeLa, and C6 glioma cells. KTH-13-AMP also dose-dependently induced morphological changes in C6 glioma cells and time-dependently increased the level of early apoptotic cells stained with annexin V-FITC. Furthermore, the levels of the active full-length forms of caspase-3 and caspase-9 were increased. In contrast, the levels of total forms of caspases-3, caspase-8, caspase-9, and Bcl-2 were decreased in KTH-13-AMP treated-cells. We also confirmed that the phosphorylation of STAT3, Src, and PI3K/p85, which is linked to cell survival, was diminished by treatment with KTH-13-AMP. Therefore, these results strongly suggest that this compound can be used to guide the development of an anti-cancer drug or serve as a lead compound in forming another strong anti-proliferative agent.

Prediction of Internal Quality for Cherry Tomato using Hyperspectral Reflectance Imagery (초분광 반사광 영상을 이용한 방울토마토 내부품질 인자 예측)

  • Kim, Dae-Yong;Cho, Byoung-Kwan;Kim, Young-Sik
    • Food Engineering Progress
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    • v.15 no.4
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    • pp.324-331
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    • 2011
  • Hyperspectral reflectance imaging technology was used to predict internal quality of cherry tomatoes with the spectral range of 400-1000 nm. Partial least square (PLS) regression method was used to predict firmness, sugar content, and acid content. The PLS models were developed with several preprocessing methods, such as normalization, standard normal variate (SNV), multiplicative scatter correction (MSC), and derivative of Savitzky Golay. The performance of the prediction models were investigated to find the best combination of the preprocessing and PLS models. The coefficients of determination ($R^{2}_{p}$) and standard errors of prediction (SEP) for the prediction of firmness, sugar content, and acid content of cherry tomatoes from green to red ripening stages were 0.876 and 1.875kgf with mean of normalization, 0.823 and $0.388^{\circ}Bx$ with maximum of normalization, and 0.620 and 0.208% with maximum of normalization, respectively.

Antioxidant effect of ergothioneine on in vitro maturation of porcine oocytes

  • Ji-Young Jeong;Lian Cai;Mirae Kim;Hyerin Choi;Dongjin, Oh;Ali Jawad;Sohee Kim;Haomiao Zheng;Eunsong Lee;Joohyeong Lee;Sang-Hwan, Hyun
    • Journal of Veterinary Science
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    • v.24 no.2
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    • pp.24.1-24.13
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    • 2023
  • Background: Ergothioneine (EGT) is a natural amino acid derivative in various animal organs and is a bioactive compound recognized as a food and medicine. Objectives: This study examined the effects of EGT supplementation during the in vitro maturation (IVM) period on porcine oocyte maturation and subsequent embryonic development competence after in vitro fertilization (IVF). Methods: Each EGT concentration (0, 10, 50, and 100 μM) was supplemented in the maturation medium during IVM. After IVM, nuclear maturation, intracellular glutathione (GSH), and reactive oxygen species (ROS) levels of oocytes were investigated. In addition, the genes related to cumulus function and antioxidant pathways in oocytes or cumulus cells were investigated. Finally, this study examined whether EGT could affect embryonic development after IVF. Results: After IVM, the EGT supplementation group showed significantly higher intracellular GSH levels and significantly lower intracellular ROS levels than the control group. Moreover, the expression levels of hyaluronan synthase 2 and Connexin 43 were significantly higher in the 10 μM EGT group than in the control group. The expression levels of nuclear factor erythroid 2-related factor 2 (Nrf2) and NAD(P)H quinone dehydrogenase 1 (NQO1) were significantly higher in the oocytes of the 10 μM EGT group than in the control group. In the assessment of subsequent embryonic development after IVF, the 10 μM EGT treatment group improved the cleavage and blastocyst rate significantly than the control group. Conclusions: Supplementation of EGT improved oocyte maturation and embryonic development by reducing oxidative stress in IVM oocytes.

Metabolizing analysis according to the sawdust media of Pleurotus ostreatus (산겨릅나무와 옻나무 톱밥배지에서 재배한 느타리버섯의 함유성분 분석)

  • Shin, Yu-Su;Yang, Bo-Hyun;Kang, Bo-Yeon;Kim, Hyun-Soo;Lee, Ji-Hyun;Hong, Yoon-Pyo;Lee, Sang-Won;Lee, Chan-Jung;Kim, Seung-Yoo
    • Journal of Mushroom
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    • v.9 no.4
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    • pp.194-197
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    • 2011
  • The transitivity of Chemical constituents by Pleurotus ostreatus cultivated in different raw sawdusts, which are Acer tegmentosum MAX, Rhus verniciflura, was investigated. The HPLC chromatography patterns on the chemical constituents of P. ostreatus showed the similar chromatography patterns in the different raw sawdusts and control sawdust. The unknown chemical constituents of P. ostreatus cultivated in the mixed medium added 10 %, 20% raw sawdusts, respectively, were increased. But the significance results in the mixed medium added 50% raw sawdusts were not showed. The chromatography patterns of mycelia grown in media added the 80% MeOH extracts of A. tegmentosum and R. verniciflura showed the similar patterns in comparison with control mycelia. In the results, the secondary metabolites of functional media were not degrade and changed to other derivatives compounds by P. ostreatus.

Clinical Efficacy of Belotecan (CKD-602), Newly Developed Camptothecin Analog, in the 2nd Line Treatment of Relapsed Small Cell Lung Cancer (재발된 소세포폐암환자에서 이차 약제로 사용되는 Belotecan (CKD-602)의 임상적 효용성)

  • Ban, Hee-Jung;Oh, In-Jae;Kim, Kyu-Sik;Ju, Jin-Yung;Kwon, Yong-Soo;Kim, Yu-Il;Lim, Sung-Chul;Kim, Young-Chul
    • Tuberculosis and Respiratory Diseases
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    • v.66 no.2
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    • pp.93-97
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    • 2009
  • Background: Belotecan (Camtobell, CKD-602, Chongkundang Pharm., Korea), a camptothecin derivative, has anticancer effects by inhibiting topoisomerase I such as topotecan. This study observed the response, survival and toxicity of belotecan monotherapy after the failure of etoposide and platinum (EP). Methods: Forty nine small cell lung cancer (SCLC) patients (M/F=41/8; age, 64.5${\pm}$7.6 (mean${\pm}$SD) years), who failed in their first line chemotherapy were enrolled in this study. Twenty one SCLC patients showed relapsed lung cancer more than 90 days after their priorEP chemotherapy (sensitive relapse group, SR) and 28 patients relapsed within 90 days (refractory relapse group, RR). Results: The response rate was 25%. Eleven patients showed partial responses and 5 patients could not be checked. The response rate of the SR and RR patients was similar. The relative dose intensity was lower in the responders (78${\pm}$15%) than non-responders (83${\pm}$13%, p=0.03). The median survival time (MST) was 10.3 months (290 days). The MST of the non-responders and responders was 186 days (95% CI; 67-305) and 401 days (95% CI; 234-568, p=0.07), respectively. The median progression free survival (MPFS) was similar in the SR (79 days) and RR (67 days) patients. Grade 3-4 neutropenia, anemia, and thrombocytopenia were observed in 59.6%, 12.8% and 23.4% of patients, respectively. Conclusion: The efficacy and survival were demonstrated in the second-line setting. However, a randomized comparative trial with topotecan will be needed.

Consideration of the Usefulness of 18F-FET Brain PET/CT in Brain Tumor Diagnosis (뇌종양진단에 있어 18F-FET Brain PET/CT의 유용성에 대한 고찰)

  • Kyu-Ho Yeon; Jae-Kwang Ryu
    • The Korean Journal of Nuclear Medicine Technology
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    • v.28 no.1
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    • pp.41-47
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    • 2024
  • Purpose: 18F-FET, a radiopharmaceutical based on a Tyrosine amino acid derivative using the Sodium-Potassium Pump-independent Transporter (System L) for non-invasive evaluation of primary, recurrent, and metastatic brain tumors, exhibits distinct characteristics. Unlike the widely absorbed 18F-FDG in both tumor and normal brain tissues, 18F-FET demonstrates specific uptake only in tumor tissue while almost negligible uptake in normal brain tissue. This study aims to compare and evaluate the usefulness of 18F-FDG and 18F-FET Brain PET/CT quantitative analysis in brain tumor diagnosis. Materials and Methods: In 46 patients diagnosed with brain gliomas (High Grade: 34, Low Grade: 12), Brain PET/CT scans were performed at 40 minutes after 18F-FDG injection and at 20 minutes (early) and 80 minutes (delay) after 18F-FET injection. SUVmax and SUVpeak of tumor areas corresponding to MRI images were measured in each scan, and the SUVmax-to-SUVpeak ratio, an indicator of tumor prognosis, was calculated. Differences in SUVmax, SUVpeak, and SUVmax-to-SUVpeak ratio between 18F-FDG and 18F-FET early/delay scans were statistically verified using SPSS (ver.28) package program. Results: SUVmax values were 3.72±1.36 for 18F-FDG, 4.59±1.55 for 18F-FET early, and 4.12±1.36 for 18F-FET delay scans. The highest SUVmax was observed in 18F-FET early scans, particularly in HG tumors (4.85±1.44), showing a slightly more significant difference (P<0.0001). SUVpeak values were 3.33±1.13 for 18F-FDG, 3.04±1.11 for 18F-FET early, and 2.80±0.96 for 18F-FET delay scans. The highest SUVpeak was in 18F-FDG scans, while the lowest was in 18F-FET delay scans, with a more significant difference in HG tumors (P<0.001). SUVmax-to-SUVpeak ratio values were 1.11±0.09 for 18F-FDG, 1.54±0.22 for 18F-FET early, and 1.48±0.17 for 18F-FET delay scans. This ratio was higher in 18F-FET scans for both HG and LG tumors (P<0.0001), but there was no statistically significant difference between 18F-FET early and delay scans. Conclusion: This study confirms the usefulness of early and delay scans in 18F-FET Brain PET/CT examinations, particularly demonstrating the changes in objective quantitative metrics such as SUVmax, SUVpeak, and introducing the SUVmax-to-SUVpeak ratio as a new evaluation metric based on the degree of tumor malignancy. This is expected to further contributions to the quantitative analysis of Brain PET/CT images.

Synthesis and Characterization of Thermally Cross-linkable Hole Transporting Material Based on Poly(p-phenylenevinylene) Derivative (열경화가 가능한 poly(p-phenylenevinylene)계 정공전달 물질의 합성 및 특성)

  • Choi, Jiyoung;Lee, Bong;Kim, Joo Hyun
    • Applied Chemistry for Engineering
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    • v.19 no.3
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    • pp.299-303
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    • 2008
  • A thermally cross-linkable polymer, poly[(2,5-dimethoxy-1,4-phenylenevinylene)-alt-(1,4-phenylenevinylene)] (Cross-PPV), was synthesized by the Heck coupling reaction. In order for the polymer to be cross-linkable, 20 mol% excess divinylbenzene was added. The chemical structure of Cross-PPV and thermally crosslinked Cross-PPV were confirmed by FT-IR spectroscopy. From the FT-IR, UV-Vis, and PL spectral data, thermally crosslinked Cross-PPV was insoluble in common organic solvents. The HOMO and LUMO energy level of thermally cross-linked Cross-PPV were estimated -5.11 and -2.56 eV, respectively, which were determined by the cyclic voltammetry and UV-Vis spectroscopy. From the energy level data, one can easily notice that thermally crosslinked Cross-PPV can be used for hole injection layer effectively. Bilayer structured device (ITO/crosslinked Cross-PPV/PM-PPV/Al) was fabricated using poly(1,4-phenylenevinylene-(4-dicyanomethylene-4H-pyran)-2,6-vinylene-1,4-phenylenevinylene-2,5-bis(dodecyloxy)-1,4-phenylenevinylene (PM-PPV) as the emitting layer, which have HOMO and LUMO energy levels of -5.44 eV and -3.48 eV, respectively. The bilayered device had much enhanced the maximum efficiency (0.024 cd/A) and luminescence ($45cd/m^2$) than those of a single layer device (ITO/PM-PPV/Al, 0.003 cd/A, $3cd/m^2$). The enhanced performance originated from that fact that cross-linked Cross-PPV facilitatse the hole injection to the emissive layer and the injected hole and electron from ITO and Al are recombined in emitting layer (PM-PPV) effectively.

Production of hTPO Transgenic Chickens using Tetracycline-Inducible Expression System (Tetracycline-Inducible Expression System을 이용한 Human Thrombopoietin (hTPO) 형질전환 닭의 생산)

  • Kwon, M.S.;Koo, B.C.;Kim, D.H.;Kim, M.J.;Kim, T.
    • Korean Journal of Poultry Science
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    • v.36 no.2
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    • pp.177-186
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    • 2009
  • It is well-known that unregulated over-expression of foreign gene may have unwanted physiological or toxic effects in transgenic animals. To circumvent these problems, we constructed retrovirus vector designed to express the foreign gene under the control of the tetracycline-inducible promoter. However, gene expressions in the tetracycline-inducible expression system (Tet system) are not completely regulated but a little leaky due to the inherent defects in conventional Tet-based systems. A more tightly controllable regulatory system can be achieved when the advanced versions ($rtTA2^SM2$) of rtTA and a minimal promoter in responsive components (pTRE-tight) are used in combination therein. In this study, we tried to produce human thrombopoietin (hTPO) from various target cells and transgenic chickens using the retrovirus vector combined with Tet system. hTPO is the primary regulator of platelet production and has an important role in the survival and expansion of hematopoietic stem cells. In a preliminary experiment in vitro, higher hTPO expression and tighter expression control were observed in chicken embryonic fibroblast (CEF) cells. We also measured the biological activity of the hTPO using Mo7e cells whose proliferation is dependant on hTPO. The biological activity of the recombinant hTPO from CEF was higher than both its commercial counterpart and hTPO from other target cells. The recombinant retrovirus was injected beneath the blastoderm of non-incubated chicken embryos (stage X). Out of 138 injected eggs, 15 chicks hatched after 21 days of incubation. Among them, 8 hatched chicks were hTPO positive. When the Go transgenic chicken was fed doxycycline (0.5 mg per 1 gram of feed), a tetracycline derivative, hTPO concentration of the transgenic chicken blood was 200 ng/mL. Germline transmission of the transgene was confirmed in sperm of the Go transgenic roosters. These results are informative to establish transgenic chickens as bioreactors for the mass production of commercially valuable and biological active human cytokine proteins.

Clinical Efficacy of Erdosteine in Patients with Acute or Chronic Bronchitis -A Randomized, Double Blind, Comparative Study vs. Ambroxol- (급.만성 기관지염 환자에서 엘도스$^{(R)}$(Erdosteine)의 임상효과 -염산 암브록솔과의 무작위 이중맹검 비교시험-)

  • Kim, Seok-Chan;Lee, Sang-Hoak;Song, So-Hyang;Kim, Young-Kyoon;Moon, Hwa-Sik;Song, Jeong-Sup;Park, Sung-Hak
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.6
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    • pp.1296-1307
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    • 1997
  • Background : Erdosteine is a thiol derivative developed for the treatement of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine has mucomodulating and antioxidant properties and especially exhibits excellent gastrointestinal tolerability. Methods : The study was conducted as a prospective evaluation, with 2 comparative groups orally treated with erdosteine 300mg (bid.) or ambroxol 30mg (b.i.d.) for 7 days and the design of trial was double-blind. The treatments have been assigned randomly to patients (n=80) with acute or chronic bronchitis. The primary end-point used to determine efficacy in this study was subjective symptoms including expectorating frequence, expectoration volume, expectorating difficulty, expectoration viscosity, cough intensity and dyspnea. The secondary end-points of efficacy was the result of arterial blood gas analysis and pulmonary function test. Safety was evaluated with adverse drug reactions and laboratory tests monitoring. 61 patients was included in the efficacy analysis, due to the fact that 19 patients drop-out for different reasons. The obtained values have been analyzed with paired Hest., ANOVA test., multivariate $t^2$-test, repeated measures analysis of covariance, two sample t-test, loglinear-logit model analysis, Fisher's exact test. Results : 1) There was no significant difference on demographic data and vital signs between erdosteine and ambroxol treated groups. 2) The comparison between erdosteine and ambroxol treated groups showed no significant difference in improvement of each symptom in spite of the more favorable efficacy obtained with erdosteine. No difference on the contrary was observed for arterial blood gas analysis and pulmonary function test. 3) As safety is concerned, no clinical significant changes in laboratory test and symptom were induced in erdosteine and ambroxol treated group and two patients in ambroxol treated group drop-out for adverse reactions in symptom. 4) In the evaluation of final clinical efficacy, erdosteine improved more effectively patient's overall symptoms {very good effect (11/31), good effect (12/31), moderate effect (6/31), no effect (2/31), aggravation (0/31)} than ambroxol {very good effect (6/30), good effect (14/30), moderate effect (5/30), no effect (4/30), aggravation (2/30)}. And the probability of symptomatic improvement by erdosteine compared to ambroxol was 2.5 times. (p<0.05). Conclusion : This study showed that erdosteine was clinically effective and safe drug for treatment of acute and chronic bronchitis.

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