• 제목/요약/키워드: q-analogue

검색결과 70건 처리시간 0.019초

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
    • /
    • 제17권3호
    • /
    • pp.237-243
    • /
    • 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
    • /
    • 제19권7호
    • /
    • pp.1026-1032
    • /
    • 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
    • /
    • 제15권8호
    • /
    • pp.3651-3657
    • /
    • 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.

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

  • 오종서
    • 한국콘텐츠학회논문지
    • /
    • 제9권4호
    • /
    • pp.154-161
    • /
    • 2009
  • 방송과 통신의 융합으로 인해, 전 세계의 TV와 라디오 방송사들은 전면적인 디지털 방송화를 위해 매진하고 있다. 이러한 흐름 속에서 우리나라는 아날로그 방송신호를 전면 중단해야만 하는 디지털 전환정책을 2012년까지 완수하여야 한다. 보고서에 따르면 현재 대략 30%정도의 디지털 전환률을 보이고 있다고는 하지만, 그 조차도 관련 기관의 공식적인 집계는 아니다. 이에 비해 우리나라와 같은 해인 2012년 디지털 전환을 완료해야 하는 영국의 경우 2008년 2분기 현재 88%의 디지털 전환률을 보이고 있는 것은 비교될 만하다. 현재 상태로 우리나라의 디지털 전환은 장밋빛 미래를 기대하기 힘들 뿐 아니라, 위태로운 지경에 놓여 있다고 볼 수 있다. 본 연구는 미래학적인 관점에서 우리나라의 디지털 전환의 미래를 예측하여 보고, 시청 행태에 영향을 미칠 수 있는 가능성을 찾고자 한다. 분석을 위해서는 미래 예측에서 유용하게 활용되는 퓨처스휠 기법을 적용하였다. 결론에서는 우리나라의 급박한 디지털 전환에 대처하는 몇 가지 시나리오를 제시하였다.

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
    • /
    • 제42권4호
    • /
    • pp.116-124
    • /
    • 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.

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

  • 오강오;이상열
    • PNF and Movement
    • /
    • 제17권2호
    • /
    • pp.311-319
    • /
    • 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.

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

  • 배성제;김완수;강수경;어규식;홍정표;전양현
    • Journal of Oral Medicine and Pain
    • /
    • 제38권4호
    • /
    • pp.339-356
    • /
    • 2013
  • 이 연구에서는 말초 opioid 수용체를 이용한 저작근 통증 조절 시 성별 효과의 차이를 확인하고자 RDC/TMD로 진단된 지원자 남성 20명, 여성 20명을 saline 주사군, lidocaine 주사군, morphine 1.5 mg 주사군, morphine 3 mg 주사군 각각 5명씩 배정하였다. 통증부위에 주사 전, 주사 후 1시간, 24시간, 48시간에 각각 주관적인 통증 평가인 시각유추척도평가, 맥길통증설문지 평가, 통증부위표시평가 그리고 객관적인 통증 평가인 압력통증역치평가와 압력통증한계평가를 실시하였다. 검사 후 평가된 자료를 통계 처리하여 다음과 같은 결과를 얻었다. 1. 시각유추척도평가에서는 남녀 모두가 morphine 3 mg군에서 통계학적으로 유의성 있는 효과가 있었다. (male: p<0.05, female: p<0.05) 2. 맥길통증설문지 평가에서는 남녀 모두가 morphine 1.5 mg군 보다 morphine 3 mg군에서 더 통계학적으로 유의성 있는 효과가 있었다. (male: p<0.001, female: p<0.01) 3. 통증부위표시평가와 압력통증역치평가에서는 남성이 morphine 3 mg군에서 통계학적으로 유의성 있는 효과가 있었다. (PD: p<0.001, PPT: p<0.05) 이상의 연구 결과로 저작근 통증을 조절하기 위해서 morphine 3 mg을 통증부위에 주사한 경우 객관적인 통증 평가에서 여성 환자보다 남성 환자에게 더 효과가 있다는 것을 알 수 있었으며, 앞으로 시간에 따른 그리고 용량에 따른 남녀 치료효과의 차이에 관한 연구가 더 필요 할 것으로 생각된다.

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
    • /
    • 제41권2호
    • /
    • pp.61-71
    • /
    • 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.

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

  • 유상훈;김민재;장주연;강수경;어규식;홍정표;전양현
    • Journal of Oral Medicine and Pain
    • /
    • 제37권3호
    • /
    • pp.169-182
    • /
    • 2012
  • 이 연구는 Morphine을 이용한 저작근통증의 조절 효과를 확인하기 위해서 시행되었으며, 경희대학교 치과대학병원 구강내과에 내원한 환자 중 RDC/TMD로 진단된 지원자를 saline 주사군, lidocaine 주사군, morphine 주사군 각각 10명씩 배정하였다. 통증부위에 주사 전, 주사 후 10분, 30분, 60분에 각각 주관적인 통증 평가인 시각유추척도검사, 맥길통증설문지검사 그리고 통증부위표시검사와 객관적인 통증 평가인 압력통증역치검사와 압력통증한계검사를 실시하였다. 검사 후 평가된 자료를 통계 처리하여 다음과 같은 결과를 얻었다. 1. 주관적인 통증 평가와 객관적인 통증 평가 모두 집단 내 효과가 있었다. (p<0.001) 2. 주관적인 통증 평가인 통증부위표시검사(p<0.001)에서 집단 간 효과가 있었다. 3. 객관적인 통증 평가인 압력통증역치검사(p=0.025)에서 집단 간 효과가 있었다. 4. 주관적인 통증 평가인 통증부위표시검사는 morphine 주사군(p=0.001)이 saline 주사군에 비해서 효과가 있었다. 이상의 연구결과로 저작근에 통증이 있는 환자에게 morphine 주사 시 60분 이내에는 주관적인 평가에서 통증 조절 효과가 있었으며, 향후 시간 연장에 따른 지속적인 추가 연구가 필요 할 것으로 생각된다.

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

  • 고석호;강수경;어규식;김은철;홍정표;전양현
    • Journal of Oral Medicine and Pain
    • /
    • 제38권2호
    • /
    • pp.161-174
    • /
    • 2013
  • 이 연구는 저작근 통증 환자에게 Morphine을 주사하였을 때의 조절 효과를 확인하기 위해서 시행되었으며, 경희대학교 치과대학병원 구강내과에 내원한 환자 중 RDC/TMD로 근막통증으로 진단된 환자들이 지원하였다. 실험군은 총 네 군으로 구성되었으며 saline 주사군, lidocaine 주사군, morphine 1.5mg 주사군, morphine 3.0 mg 주사군에 각각 10명씩 배정하였다. 통증부위에 주사 전, 주사 후 1시간, 24시간, 48시간에 각각 주관적인 통증 평가인 시각유추척도검사, 맥길통증설문지검사 그리고 통증부위표시검사와 객관적인 통증 평가인 압력통증역치검사와 압력통증한계검사를 실시하였다. 검사 후 평가된 자료를 통계 처리하여 다음과 같은 결과를 얻었다. 1. 주관적인 통증평가에서 morphine 3 mg 군은 48시간 후 통계학적으로 유의성 있는 효과가 있었다.(VAS: p<0.01, MGQ: p<0.001, PD: p<0.05) 2. 객관적인 통증평가에서 morphine 1.5 mg 군은 1시간 후 통계학적으로 유의성 있는 효과가 있었다.(PPT: p<0.01, PPTol: p<0.05) 3. 맥길통증설문지에서 lidocaine 군, morphine 1.5 mg 군 그리고 morphine 3 mg 군은 모두 처치 후 1시간부터 효과가 있었으나 상대적으로 morphine 3 mg 군에서 통계학적으로 유의성 있게 더 큰 효과가 있었다.(1h: p<0.01, 24h: p<0.01, 48h: p<0.001) 이상의 연구 결과로 저작근에 통증이 있는 환자에게 morphine 주사 시 주관적인 평가에서 48시간 후 통증 조절 효과가 있었고, morphine 3 mg이 더 효과가 있었으며, 향후 시간 연장에 따른 지속적인 추가 연구가 필요 할 것으로 생각된다.