• Title/Summary/Keyword: q-analogue

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Cytotoxic Activity and Quantitative Structure Activity Relationships of Arylpropyl Sulfonamides

  • Hwang, Yu Jin;Park, Sang Min;Yim, Chul Bu;Im, Chaeuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.3
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    • pp.237-243
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    • 2013
  • B13 is a ceramide analogue and apoptosis inducer with potent cytotoxic activity. A series of arylpropyl sulfonamide analogues of B13 were evaluated for their cytotoxicity using MTT assays in prostate cancer PC-3 and leukemia HL-60 cell lines. Some compounds (4, 9, 13, 14, 15, and 20) showed stronger activities than B13 in both tumor cell lines, and compound (15) gave the most potent activity with $IC_{50}$ values of 29.2 and 20.7 ${\mu}M$, for PC-3and HL-60 cells, respectively. Three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed to build highly reliable and predictive CoMSIA models with cross-validated $q^2$ values of 0.816 and 0.702, respectively. Our results suggest that long alkyl chains and a 1R, 2R configuration of the propyl group are important for the cytotoxic activities of arylpropyl sulfonamides. Moreover, the introduction of small hydrophobic groups in the phenyl ring and sulfonamide group could increase biological activity.

The Relative Effectiveness of Liquid Methionine Hydroxy Analogue Compared to DL-methionine in Broilers

  • Yao, J.H.;Li, S.Q.;Zhong, L.L.;Huang, S.X.;Zhang, W.J.;Xi, H.B.
    • Asian-Australasian Journal of Animal Sciences
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    • v.19 no.7
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    • pp.1026-1032
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    • 2006
  • The present experiment was conducted to assess the efficacy of liquid methionine hydroxy analogue-free acid (MHA-FA) in comparison to DL-methionine (DL-Met) in broilers. 567 day-old Avian chicks were divided into 7 treatments with 5 replicates of 16 birds each. During the 35d (7-42 d) experimental periods chicks were given two basal diets. From 7 to 21d of age, a starting basal diet containing 19.5% protein and 0.33% methionine was supplemented with two graded levels of DL-Met (0.070 and 0.160%) or four levels of MHA-FA (0.118, 0.143, 0.221 and 0.268%). From 22 to 42d of age DL-Met (0.050 and 0.080%) or MHA-FA (0.071, 0.074, 0.112 and 0.140%) were added to a finishing basal diet with 18.0% protein and 0.28% methionine. Chicks fed on supplemental DL-Met or MHA-FA had significantly higher (p<0.05) body weight gain and feed conversion ratio (FCR) than the control group from 7-21d of age. During the finishing phase (22-42 d), body weight and weight gain of chicks in DL-Met or MHA-FA treatments were similar to those in the control, but FCR was improved (p<0.05) with supplementation of DL-Met or MHA-FA. Breast yield was higher (p<0.05) on DL-Met or MHA-FA supplemented than un-supplemented diets. The thigh meat yields emanating from diets with DL-Met or MHA-FA were lower (p<0.05) than that in control. Abdominal fat was also higher in broilers fed the control diet than in DL-Met or MHA-FA supplemented treatments. Methionine requirement of broilers was calculated to be 0.44 and 0.35% and cystine requirement was 0.35 and 0.31% for the starting (7-21 d) and finishing phase (22-42 d), respectively. The efficacy of MHA-FA in comparison to DL-Met for weight gain was 64 and 85% and for FCR was 55 and 60% at 7-21 and 22-42 d of age, respectively, while it was 74, 72, 52 and 48% for breast yield, thigh meat production, body energy content and energy deposition ratio at 42 d of age, respectively. In conclusion, in practical diet formulation for broiler chicks the average bioavailability of MHA-FA relative to DL-Met could be considered as 60 and 73% for 7 to 21d and 22 to 42 d of age, respectively.

Schedule-Dependent Effects of Kappa-Selenocarrageenan in Combination with Epirubicin on Hepatocellular Carcinoma

  • Ji, Yu-Bin;Ling, Na;Zhou, Xiao-Jun;Mao, Yun-Xiang;Li, Wen-Lan;Chen, Ning
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.8
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    • pp.3651-3657
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    • 2014
  • Hepatocellular carcinoma (HCC) has a relatively higher incidence in many countries of Asia. Globally, HCC has a high fatality rate and short survival. Epirubicin, a doxorubicin analogue, may be administered alone or in combination with other agents to treat primary liver cancer and metastatic diseases. However, the toxic effects of epirubicin to normal tissues and cells have been one of the major obstacles to successful cancer chemotherapy. Here, we investigated the effects of epirubicin in combination with kappa-selenocarrageenan on mice with H22 implanted tumors and HepG-2 cell proliferation, immune organ index, morphology, cell cycle and related protein expressions in vivo and in vitro with sequential drug exposure. The inhibitory rate of tumor growth in vivo was calculated. Drug sensitivity was measured by MTT assay, and the King's principle was used to evaluate the interaction of drug combination. Morphological changes were observed by fluorescent microscopy. Cell cycle changes were analyzed by flow cytometry. Expression of cyclin A, Cdc25A and Cdk2 were detected by Western blotting. In vivo results demonstrated that the inhibitory rate of EPI combined with KSC was higher than that of KSC or EPI alone, and the Q value indicated an additive effect. In addition, KSC could significantly raise the thymus and spleen indices of mice with H22 implanted tumors. In the drug sensitivity assay in vitro, exposure to KSC and EPI simultaneously was more effective than exposure sequentially in HepG-2 cells, while exposure to KSC prior to EPI was more effective than exposure to EPI prior to KSC. Q values showed an additive effect in the simultaneous group and antagonistic effects in the sequential groups. Morphological analysis showed similar results to the drug sensitivity assay. Cell cycle analysis revealed that exposure to KSC or EPI alone arrested the cells in S phase in HepG-2 cells, exposure to KSC and EPI simultaneously caused accumulation in the S phase, an effect caused by either KSC or EPI. Expression of cyclin A, Cdc25A and Cdk2 protein was down-regulated following exposure to KSC and EPI alone or in combination, exposure to KSC and EPI simultaneously resulting in the lowest values. Taken together, our findings suggest that KSC in combination with EPI might have potential as a new therapeutic regimen against HCC.

Scenario Planning after Digital Switchover in S. Korea: The Use of Futures Wheel (디지털전환의 미래 예측 시나리오: 퓨처스휠 기법을 중심으로)

  • Oh, Jong-Sir
    • The Journal of the Korea Contents Association
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    • v.9 no.4
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    • pp.154-161
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    • 2009
  • Thanks to the circumstance of digital convergence, most of the world TV and radio stations are gearing up for digitalisation of broadcasting. In this flux, digital switchover in South Korea should be completed by 2012 when transmission of analogue broadcasting signal will be ceased. According to the report, it shows only over 30% take up roughly so far, but there is no official survey from relevant organisation. It is very comparable with British digital switchover which is same year as S. Korea and has been reported 88% take up as of 2008 Q2. Yet the digital switchover in S. Korea inferred from this current is not a rosy future and even seems to be perilous. The purpose of this paper is to predict the media future of S. Korea at the view point of futurology and draw out the possibilities which enable to affect viewing behavior. In order to analyse it applies the futures wheel which is one of useful tools for future work. Consequently it suggests a number of scenarios how to cope with the impending situation in S. Korea.

Antidiuretic Hormone Levels in Men with Burning Mouth Syndrome: A Pilot Study

  • Lee, Yeon-Hee;Hwang, Mi-Jin;Chon, Suk;Auh, Q-Schick
    • Journal of Oral Medicine and Pain
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    • v.42 no.4
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    • pp.116-124
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    • 2017
  • Purpose: Burning mouth syndrome (BMS) is a disabling pain that mostly occurs in elderly women, but rarely in men. It is characterized by an unremitting oral burning sensation and pain without detectable oral mucosal changes. We investigated the clinical and hematologic features of middle-aged men with BMS, and compared the results to those of men with oral mucositis. Methods: Five men with BMS ($48.60{\pm}6.19years$) and five age-matched controls with oral mucositis ($49.80{\pm}15.26years$) underwent clinical and psychological evaluations and blood tests. Psychological status was evaluated using the Symptom Checklist-90-Revised. Cortisol, estradiol, progesterone, testosterone, follicle-stimulating hormone (FSH), luteinizing hormone (LH), adrenocorticotropic hormone (ACTH), and antidiuretic hormone (ADH) levels and erythrocyte sedimentation rate (ESR) were determined from the blood samples. Results: ADH level was significantly lower in men with BMS than in the controls. ADH levels correlated with testosterone (p<0.01), and ACTH levels strongly correlated with ESR (p<0.05). Progesterone level positively correlated with FSH and LH levels. Pain intensity on a visual analogue scale correlated with estradiol level only in men with BMS. Among psychological factors, the obsessive-compulsive disorder, interpersonal-sensitivity, and anxiety scores were higher in men with BMS than in the controls (p<0.05). However, no correlations were observed between the psychological and hematologic factors in both groups. The BMS symptoms presented only on the tongue, with the lateral border being the most prevalent area. Conclusions: Men with BMS may experience dysregulated endocrinologic or psychoneuroendocrinologic interactions, which might affect oral BMS symptoms, aggravating the severity of the burning sensation.

Effects of Calcaneus Fixation Taping on Quadriceps Angle and Lower Limb Muscles During Stairway Gait of a Patient with Patellofemoral Pain (무릎넙다리통증증후군 환자의 계단보행 시 발뒤꿈치뼈 교정 테이핑이 슬개대퇴각과 하지근육에 미치는 영향)

  • Oh, Kang-O;Lee, Sang-Yeol
    • PNF and Movement
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    • v.17 no.2
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    • pp.311-319
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    • 2019
  • Purpose: This study was conducted to determine the structural change in knees caused by quadriceps angle and the muscle activity in lower limbs. Indirect intervention was provided by using taping for stability in the ankle joints, which affected patellofemoral pain. Methods: The subjects in this study were 20 patients with patellofemoral pain who visited ${\bigcirc}{\bigcirc}{\bigcirc} $ Hospital in Busan. The visual analogue scale measured the dynamic quadriceps angle and the degree of pain felt by the patients while walking down stairs, which was a known factor of patellofemoral pain. In addition, muscle activities in the rectus femoris, vastus lateralis, vastus medialis, tibialis anterior, peroneus longus, and biceps femoris, which affect the knees and ankles, were measured using surface electromyography. The muscle activities were converted into %RVC for this study. The data obtained in this study were analyzed with the Wilcoxon signed-rank test using the SPSS Ver. 25.0 statistical program. The significance level ${\alpha}$ was 0.05. Results: The study results showed that the pain and dynamic quadriceps angle were significantly reduced statistically when applying the calcaneus fixation taping (p<0.05). Muscle activity in the lower limbs was significantly decreased in the vastus medialis, vastus lateralis, and tibialis anterior (p<0.05). Conclusion: The summary of the study results verified that the calcaneus fixation taping reduced the pain and dynamic quadriceps angle by providing stability in the ankle joints. It also produced efficient movement due to the difference in lower-limb muscle activity.

Sex Differences in the Pain Control by the Peripheral Opioid (성별에 따른 말초 opioid의 통증조절)

  • Bae, Sung-Jae;Kim, Wan-Su;Kang, Soo-Kyung;Auh, Q-Schick;Hong, Jung-Pyo;Chun, Yang-Hyun
    • Journal of Oral Medicine and Pain
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    • v.38 no.4
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    • pp.339-356
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    • 2013
  • This study was designed to evaluate the sex differences in the pain control effect by morphine injection to masticatory muscle pain patients. Patients with masticatory muscle pain visited the Department of Oral Medicine, Kyung Hee University Dental Hospital were recruited to this study and diagnosed by RDC/TMD. Experimental group were divided into four group each from male (n=20) and female (n=20); saline injection group (n=5), lidocaine injection group (n=5), morphine 1.5 mg injection group (n=5) and morphine 3 mg injection group (n=5). Evaluation list was the subjective pain evaluation(visual analogue scale, Mc Gill pain questionnaire, pain drawing) and the objective pain evaluation(pressure pain threshold, pressure pain tolerance) and evaluation time was injection before, after 1 hour, 24 hour, 48 hour and then it was analyzed statistically. The results were as follows : 1. The male and female were significantly different statistically morphine 3 mg group in visual analogue scale evaluation. (male: p<0.05, female: p<0.05) 2. The male and female were more significantly different statistically morphine 3 mg group than morphine 1.5 mg group in McGill pain questionnaire evaluation. (male: p<0.001, female: p<0.01) 3. The male were significantly different statistically morphine 3 mg group in pain drawing evaluation and pressure pain threshold evaluation. (PD: p<0.001, PPT: p<0.05) Therefore, it was revealed that the morphine 3 mg injection for masticatory muscle pain was effective to pain control male patients and more effect than female patients in the objective pain evaluation.

Comparison between the Subjective Evaluation and the Objective Evaluation of the Effect of Pain Control in the Masticatory Muscle Pain

  • Kim, Dong-Keun;Ahn, Chi-Hyuk;Hwang, Mi-Jin;Lee, Yeon-Hee;Kang, Soo-Kyung;Auh, Q-Schick;Hong, Jung-Pyo;Chun, Yang-Hyun
    • Journal of Oral Medicine and Pain
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    • v.41 no.2
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    • pp.61-71
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    • 2016
  • Purpose: This study was designed to evaluate the comparison between the subjective and the objective evaluation of pain control effect in masticatory muscle pain depending on time and dose change. Methods: The patients were recruited to this study and diagnosed according to the Research Diagnostic Criteria for Temporomandibular Disorders (RDC/TMD). Experimental group were divided into three groups; saline injection group (n=10), morphine 1.5 mg injection group (n=10), and morphine 3.0 mg injection group (n=10). Evaluation list was the subjective pain evaluation (visual analogue scale, McGill pain questionnaire) and the objective pain evaluation (pressure pain threshold [PPT], pressure pain tolerance [PTO]). The subjective and the objective pain evaluation were performed at the times of just before injection, 10 minutes, 30 minutes, 1 hour, 24 hours, and 48 hours after injection. Then, data were statistically analyzed. Results: The results were as follows: 1) There is no statistically significant difference between the results of the subjective and the objective pain evaluation with regard to the short-term (within 1 hour) analgesic effect of morphine sulfate. 2) However, after 1 hour of injection, while the subjective pain evaluation score still decreased, the objective pain evaluation didn't show significant changes in PPT and PTO (1 hour, p<0.05; 24 hours, p<0.01; 48 hours, p<0.001). 3) In comparison to changes in the dose, the McGill pain questionnaire was the most statistically effective method among the subjective pain evaluations (1.5 mg, p<0.05; 3 mg, p<0.01). Conclusions: Therefore, it was revealed that the subjective pain evaluation was more effective to evaluate long-term pain control, and that the McGill pain questionnaire could be an effective way to evaluate pain control depending on dose changes. It requires further investigations with time and dose extension.

Effect of Masticatory Muscle Pain Control by Morphine (Morphine에 의한 저작근 통증의 조절 효과)

  • Yoo, Sang-Hoon;Kim, Min-Jae;Chang, Joo-Yeon;Kang, Soo-Kyung;Auh, Q-Schick;Hong, Jung-Pyo;Chun, Yang-Hyun
    • Journal of Oral Medicine and Pain
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    • v.37 no.3
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    • pp.169-182
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    • 2012
  • This study was designed to evaluate the pain control effect by morphine injection to masticatory muscle pain patients. Patients with masticatory muscle pain visited the Department of Oral Medicine, Kyung Hee University Dental Hospital were recruited to this study and diagnosed by RDC/TMD. Experimental group were divided into three group; saline injection group(n=10), lidocaine injection group(n=10) and morphine injection group(n=10). Evaluation list was the subjective pain evaluation(visual analogue scale, Mc Gill pain questionnaire, pain drawing) and the objective pain evaluation(pressure pain threshold, pressure pain tolerance) and evaluation time was injection before, after 10min, 30min, 60min and then it was analyzed statistically. The results were as follows : 1. The subjective pain evaluation and the objective pain evaluation were significantly different statistically in within subject effects(p<0.001). 2. The subjective pain drawing evaluation(p<0.001) were significantly different statistically in between subject effects. 3. The objective pressure pain threshold evaluation(p=0.025) were significantly different statistically in between subject effects. 4. The morphine injection group(p=0.001) were more significantly different than the saline injection group statistically in the subject pain drawing evaluation. Therefore, it was considered that the morphine injection was effective to pain control for masticatory muscle pain patients within 60 minute.

Effect of Peripheral Opioid Receptor on Masticatory Muscle Pain Control (말초 opioid 수용체에 의한 저작근 통증의 조절 효과)

  • Ko, Seok-Ho;Kang, Soo-Kyung;Auh, Q-Schick;Kim, Eun-Cheol;Hong, Jung-Pyo;Chun, Yang-Hyun
    • Journal of Oral Medicine and Pain
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    • v.38 no.2
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    • pp.161-174
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    • 2013
  • This study was designed to evaluate the pain control effect by morphine injection to masticatory muscle pain patients. Patients with masticatory muscle pain visited the Department of Oral Medicine, Kyung Hee University Dental Hospital were recruited to this study and diagnosed by RDC/TMD. Experimental group were divided into four group; saline injection group (n=10), lidocaine injection group (n=10), morphine 1.5 mg injection group (n=10) and morphine 3 mg injection group (n=10). Evaluation list was the subjective pain evaluation(visual analogue scale, Mc Gill pain questionnaire, pain drawing) and the objective pain evaluation(pressure pain threshold, pressure pain tolerance) and evaluation time was injection before, after 1 hour, 24 hour, 48 hour and then it was analyzed statistically. The results were as follows : 1. The subjective pain evaluation were significantly different statistically in morphine 3 mg group after 48 hour. (VAS: p<0.01, MGQ: p<0.001, PD: p<0.05) 2. The objective pain evaluation were significantly different statistically in morphine 1.5 mg group after 1 hour. (PPT: p<0.01, PPTol: p<0.05) 3. The morphine 3 mg group were more significantly different than lidocaine group and morphine 1.5 mg group statistically in the McGill pain questionnaire evaluation. (1h: p<0.01, 24h: p<0.01, 48h: p<0.001) Therefore, it was revealed that the morphine 3 mg injection was effective to pain control for masticatory muscle pain patients within 48 hours and more effect than lidocaine injection.