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In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-administered with Western drugs as a part of integrative medicine practice. Carboxylesterase 1 (CES1) plays a pivotal role in the metabolisms of pro-drugs. Since (S)-2-(2-(6-dimethylamino)-benzothiazole)-4,5-dihydro-thiazole-4-carboxylate (NLMe) has recently been identified by us as a selective CES1 bioluminescent sensor, we developed a rapid method using this substrate for the direct measurement of CES1 activity in rats. This bioluminescence assay was applied to determine CES1 activity in rat tissues after a two-week oral administration of each of the four herbs noted above. The results demonstrated the presence of CES1 enzyme in rat blood and all tested tissues with much higher enzyme activity in the blood, liver, kidney and heart than that in the small intestine, spleen, lung, pancreas, brain and stomach. In addition, the four herbs showed tissue-specific effects on rat CES1 expression. Based on the CES1 biodistribution and its changes after treatment in rats, the possibility that Danshen, Gegen and Danggui might alter CES1 ac-tivities in human blood and kidney should be considered. In summary, a selective and sensitive biolu-minescence assay was developed to rapidly evaluate CES1 activity and the effects of orally administered TCMs in rats.
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Mammalian carboxylesterases (CEs) are key enzymes from the serine hydrolase superfamily. In the human body, two predominant carboxylesterases (CES1 and CES2) have been identified and extensively studied over the past decade. These two enzymes play crucial roles in the metabolism of a wide variety of endogenous esters, ester-containing drugs and environmental toxicants. The key roles of CES in both human health and xenobiotic metabolism arouse great interest in the discovery of potent CES modulators to regulate endobiotic metabolism or to improve the efficacy of ester drugs. This review covers the structural and catalytic features of CES, tissue distributions, biological functions, genetic polymorphisms, substrate specificities and inhibitor properties of CES1 and CES2, as well as the significance and recent progress on the discovery of CES modulators. The information presented here will help pharmacologists explore the relevance of CES to human diseases or to assign the contribution of certain CES in xenobiotic metabolism. It will also facilitate medicinal chemistry efforts to design prodrugs activated by a given CES isoform, or to develop potent and selective modulators of CES for potential biomedical applications.
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OBJECTIVE:To compare the effects of dezocine and nalbuphine on patient-controlled intravenous analgesia(PCIA) in patients undergoing cesarean section. METHODS:A total of 97 patients undergoing selective cesarean section were selected from our hospital during Jun. 2015 to Mar. 2017. They were divided into dezocine group(52 cases)and nalbuphine group(45 cases) according to lottery. Both groups received cesarean section under combined spinal-epidural anesthesia,and then given PCIA pump immediately after surgery. The pump of dezocine group was Dezocine injection 0.5 mg/kg+Tropisetron hydrochloride injection 10 mg;that of nalbuphine group was Nalbuphine hydrochloride injection 2 mg/kg+Tropisetron hydrochloride injection 10 mg. Both groups of analgesic drugs were diluted 100 mL with 0.9% sodium chloride injection,constant infusion of liquid medicine at rate of 2 mL/h,adding 0.5 mL additionally each time,for consecutive 48 h. VAS score and Ramsay sedation score of resting pain, dynamic pain and uterine contraction pain were performed in 2 groups 4,8,12,24,48 h after surgery. The serum levels of PRL were determined 30 min before surgery and 24,48 h after surgery. The initial time of lactation and ADR were recorded in 2 groups. RESULTS:VAS score of resting pain and uterine contraction pain at 4,8,12 h after operation and that of dynamic pain at 4,8,12, 24 h after operation were significantly lower in dezocine group than nalbuphine group,with statistical significance (P＜0.05). There was no statistical significance in VAS score between 2 groups at other time points(P＞0.05). As time went on,the VAS scores of the two groups decreased significantly at each time point,and the difference was statistically significant(P＜0.05). The serum levels of PRL in 2 groups 24 and 48 h after operation were significantly higher than 30 min before operation,with statistical significance(P＜0.05). There was no statistical significance in serum level of PRL between 2 groups at same time point(P＞0.05). There was no statistical significance in Ramsay score, initial time of lactation or the incidence of ADR between dezocine group and nalbuphine group (P＞0.05). CONCLUSIONS:Both dezocine and nalbuphine are effective analgesia drugs of PCIA in patients undergoing cesarean section. Early postoperative analgesic effect of dezocine is superior to nalbuphine. They have similar effects on long-term analgesia and postoperative sedative,serum level of PRL,initial time of lactation,as well as safety.
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Objective To determine the diagnostic value of plain CT in tuberous goiter and thyroid papillary carcinoma.Methods The CT images including 63 lesions from 58 patients with thyroid papillary carcinoma and 103 lesions from 86 patients with tuberous goiter proven by pathology were reviewed retrospectively.The analyses were mainly focus on the internal density,the presence of calcification, andthe relation of the lesion with the normal thyroid and adjacent tissue.Results There were statistically significant differences in the internal density,the morphology of calcification and the relation of the lesion with normal thyroid and adjacent tissue between the papillary carcinoma and tuberous goiter lesions.The common CT appearances of papillary carcinoma included uniform density,crab pattern change,micro calcifications and unclear boundaries of the lesion.Focal necrosis and cystic changes were also occasionally found in papillary carcinoma and usually occured at the peripheral area.Tuberous goiters usually manifested as mixed density with macro or eggshell calcifications as well as clear boundaries both with normal thyroid tissue and adjacent tissue.Conclusion The plain CT helps for the preliminary distinction of tuberous goiter and thyroid papillary carcinoma.
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Objective To investigate the value of MR T2* in evaluation of liver iron overload caused by long term blood transfusion.Methods Thirty one patients with long term blood transfusion were collected.Both serum ferritin(SF)and CRP levels were measured and the adjusted serum ferritin(ASF)concentration was calculated.MRI of the maximum cross-sectional liver was performed using a 1.5T scanner (Siemens Avanto).The T2* value of the liver was measured,and the correlation analysis was carried out.Twenty one normal volunteers served as controls.The transfusion group was divided into iron overload group and non overload group,and differences between groups were analyzed.Results The correlation coefficient in 31 patients between liver T2* value and SF,ASF and blood transfusion volume was-0.695,-0.728 and -0.657 respectively,and the difference was statistically significant(P<0.05).The correlation coefficient between SF and blood transfusion volume was 0.518,and the difference was statistically significant(P<0.05).There was difference in T 2* value between three groups.Conclusion MR T2* has some practical value in the evaluation of liver iron overload in patients with long term blood transfusion.
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Objective To analyze the relationship between the measured diameters of pituitary gland on MRI and peak-stimulated growth hormone(GH) in children with growth hormone deficiency (GHD).Methods A total of 46 children with GHD were included in this study, and 30 healthy children who were admitted to the hospital for health check-up were acted as the control group during the same period.The measured diameters of pituitary gland on MRI were compared between the two groups and the correlation between the diameters of pituitary gland on MRI and peak-stimulated GH were analyzed.Results ① The coronary and sagittal heights of pituitary gland on MRI were greater in children aged 7-10 years old and older than 10 years in control group and in children older than 10 years in observation group than those in children younger than 6 years (P<0.05).The anteroposterior diameter of pituitary gland on sagittal MRI in the control group was increased (P<0.05).The coronal height, sagittal anteroposterior diameter and sagittal height were lower in the observation group compared with age-and gender-matched controls(P<0.05).②The peak-stimulated growth hormone levels were higher in children aged 7-10 years old and older than 10 years in both groups compared with children younger than 6 years old (P<0.05).The peak-stimulated GH were lower in observation group compared with age-and gender-matched controls(P<0.05).③ The heights of pituitary gland on coronary and sagittal MRI in children with GHD were positively related to the peak-stimulated GH, and coronary height had the highest correlation(P<0.05).Conclusion The heights of pituitary gland on coronary and sagittal MRI in children with GHD are positively related to the peak-stimulated GH.The growth and development of children can be predicted by monitoring the changes of GH levels.
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Objective To investigate the clinical feasibility of contrast?enhanced three dimensional T2WI turbo?spin?echo sequence with short?term inversion recovery and sampling perfection using different flip angle evolutions (3D STIR T2WI SPACE) sequence in the brachial plexus neurography. Methods Thirty two patients were prospectively chosen and performed with brachial plexus plain scanning on a 3.0 T MR scanner by using plain and contrast?enhanced 3D STIR T2WI SPACE sequence. Thirteen of them underwent plain scan, 9 of them underwent contrast?enhanced scan, and 10 of them underwent both plain scan and enhanced scan. The visibility of the brachial plexus were scored and contrast to noise ratio (CNR) were measured by two experienced radiologists. The results between plain and contrast?enhanced imaging were compared by t test. The 10 subjects received both enhance and plain imaging, were performed with paired t test. Results In 32 patients, the visibility score of brachial plexus nerve and CNR were 7.8 ± 1.3 and 24.97±3.41 in the plain scan group, and 13.1±1.7 and 38.49±4.95 in enhanced scan group, respectively. There were statistically significant differences in the two groups(t=-11.72,P<0.01;t=-10.47, P<0.01). In 10 cases with plain and enhanced brachial plexus imaging, the average score of the brachial plexus were 7.4 ± 1.7 and 13.3 ± 1.6, the average CNR were 26.23 ± 4.43 and 38.19 ± 5.03 respectively. There were statistically significant differences (t=- 8.22, P<0.01; t=- 5.64,P<0.01). The score results were analyzed for consistency. Plain images Kappa value was 0.684, which shows moderate consistency and enhanced images Kappa value= 0.822, which shows excelent consistency. Conclusions The contrast?enhanced 3D STIR T2WI SPACE sequences may suppress background tissue signals, which is helpful to display brachial plexus, therefore it is of important value for the early diagnosis of brachial plexus neuropathy.
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Objective To investigate the effects of exercise on knee cartilage tissue structure using quantitative MR T2 mapping. Methods Sagittal T2 maps of the knee joints of 26 healthy volunteers were obtained by using 3.0T MR before,immediately after, and 1 5 min after running.The original images were classified into three terms of knee cartilage T2 map after postreconstruction.The T2 values of regions of interest (ROC)(T2 pre ,T2 post ,T2 delay )in the superficial,middle and deep cartilage of femoral and tibial joint were measured.Statistical differences of cartilage T2 values of three terms after running were analyzed.Results For the tibial joint cartilage,the T2 pre ,T2 post ,T2 delay were (49.71 ± 1.95)ms,(44.30 ± 2.56)ms,(49.41 ± 1.62)ms in the superficial layer,respectively.The three terms T2 were (42.43 ± 2.23)ms,(39.01 ± 2.37)ms,(41.90±2.28)ms in the middle layer,respectively.The differences were statistically significant(F=55.673,16.759 respectively.P<0.001).While the three terms T2 were (19.39±2.13)ms,(19.20±2.22)ms, (19.49±2.05)ms in the deep layers cartilage,respectively.The differences were not statistically significant(F =0.122,P =0.886).And the differences between T2 pre and T2 post ,T2 post and T2 delay were statistically significant (all P <0.001)in superficial and middle alyers,but there were no significant difference between the T2 pre and T2 delay (P =0.610,0.403,respectively).For the femoral joint cartilage,the T2 pre ,T2 post ,T2 delay were (50.22 ± 1.47)ms,(45.60 ± 2.82)ms,(49.84 ± 1.84)ms in superficial layers,respectively.The three terms T2 were (42.67±2.23)ms,(39.36 ± 1.98)ms,(42.40 ± 2.57)ms in the middle layer,respectively.The differences were statistically significant (F=37.976,16.987 respectively,P<0.001).While the three terms T2 were (20.30±2.73)ms,(20.60±2.44)ms,(20.51± 2.24)ms in the deep layer,the differences were not statistically significant (F =0.098,P =0.907).And the differences between T2 pre and T2 post ,T2 post and T2 delay were statistically significant (all P <0.001)in superficial and middle layers,but there were no significant difference between the T2 pre and T2 delay (P=0.520,0.679,respectively). Spatial distribution of T2 values of articular cartilage from deep to superficial layers showed a ascending trend.T2 maps showed the spatial distribution trend of T2 value change.Conclusion T2 mapping can monitor quantitatively the changes of articular cartilage molecular structure after running.The change of articular cartilage T2 value after exercise is uneven and the change of articular cartilage structure after exercise is reversible.
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Objective To assess the value of the dynamic enhanced MR (DE-MRI)morphological features in diagnosis of non lac-tation mastitis.Methods We retrospectively studied the breast DE-MRI image data of 1 5 patients with non lactation mastitis con-firmed by pathology were retrospectively studies and the lesion morphological features and distribution were analyzed.Results Amonge 1 5 patients with non lactation mastitis,6 cases were the plasma cell mastitis,5 cases were granulomatous mastitis,2 cases were abscess,and 2 cases were cyst associated with inflammation.The typical features of non lactation mastitis on DE-MRI were fast wash-in,centrifugal enhancement sign,blur boundaries between lesions and normal breast tissue,increasing unilateral vessel sign in diseased breast.Conclusion Breast DE-MRI can show typical morphological features of non lactation mastitis.When dynam-ic information is obtained inconveniently,these are helpful in diagnosing and differential diagnosing non lactation mastitis.