1.Effect of CYP3A5 and CYP3A4 on pharmacokinetics of Tacrolimus in renal transplantation recipients
Ling LIN ; Wenli SONG ; Zhongyang SHEN ; Yi ZHANG
Chinese Journal of Organ Transplantation 2012;33(4):220-224
Objective To retrospectively investigate the effects of CYP3A5 * 3,CYP3A4 * 18B and CYP3A5-CYP3A4 phenotype on the C0,D and C0/D of tacrolimus (Tac) in renal transplantation recipients.Methods The CYP3A5 * 3 and CYP3A4 * 18B genotypes of the 61 patients were detected by DNA direct sequencing,and the C0 was detected by ELISA.The differences of C0,D and C0/D on the day 14,and month 1,2 and 3 after transplantation were compared among different genotypes of recipients treated with Tac.Results The frequency of the CYP3A5 * 3 and CYP3A4 * 18B was 74.6% and 26.2% respectively.When the D of the recipients with CYP3A5 * 1 ( * 1/* 1 + * 1/* 3)was 1.3-1.6 times to theCYP3A5*3/*3,theC0 of *3/*3 group was 1.1-1.5 times to the * 1group,and the C0/D was 1.8 2.4 times to the CYP3A5 * 1.For CYP3A4,the D of CYP3A4 * 18B group ( * 1/* 18B+ * 18B/* 18B) was 1.2-1.5 times to the CYP3A5 * 1/* 1,but the C0 of 1/* 1was 1.2-1.4 times to the * 18B,the C0/D was 1.5-1.8 times to the * 18B.For the CYP3A5 CYP3A4 phenotype,the D of the recipients with AAAA was 1.3-1.7 times to the GG-GG,the C0 of GG-GG was 1.5-2 times to the AA-AA,the C0/D of the recipients with G@GG was 2.5-3 times to the AA-AA.In the recipients with C0/D above or below the median of C0/D,the distribution of CYP3A5,CYP3A4 and CYP3A5-CYP3A4 phenotypes was different significantly.Conclusion There is a significant correlation between the CYP3A5,CYP3A4 and pharmacokinetics of Tac.It's more powerful evaluating the CYP3A5-CYP3A4 phenotype rather than just one genotype of the recipients.So detecting the CYP3A5 * 3 and CYP3A4 * 18B genotypes prior to transplantation is meaningful for us to determine an appropriate initial and long-time dosage of Tac.
3.Research progress of chemical composition of taxane in Taxus canadensis and medicine source crisis solution.
Chun YANG ; Ling-Yi KONG ; Jun-Song WANG
China Journal of Chinese Materia Medica 2014;39(11):1961-1971
Taxus canadensis distributed mainly in North America, such as northern Minnesota, Newfoundland, south to Wisconsin and Pennsylvania. Its composition has been shown to be very different from other species, and in recent years, some new skeletons also have been found in Canada yew. Through analysis of the taxanes content on various Taxus plants containing taxanes, the results showed a higher content of taxol in T. canadensis. Based on the current research on T. canadensis (from the research results of the author in recent years, as well as from studies of scholars in the field), the paper outlined the research progress in recent years on the chemical constituents of taxane of T. canadensis and the spectral characteristics of various types of compounds. Besides, this paper analyzed the present research about solutions for the taxol drug source crisis.
Animals
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Bridged-Ring Compounds
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chemical synthesis
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chemistry
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pharmacology
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Humans
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Molecular Structure
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Plant Extracts
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chemical synthesis
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chemistry
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pharmacology
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Plants, Medicinal
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chemistry
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Taxoids
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chemical synthesis
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chemistry
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pharmacology
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Taxus
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chemistry
4.Diagnostic Value of Fluorescent Quantitative Polymerase Chain Reaction for Mycoplasma Pneumoniae Pneumoniae in Children with Mycoplasma Pneumoniae Pneumonia
yi, YUAN ; jin, FU ; ling, CAO ; ling-yun, GENG ; xiao-dai, CUI ; guo-wei, SONG
Journal of Applied Clinical Pediatrics 2003;0(10):-
Objective To evaluate the diagnostic value of fluorescent quantitative polymerase chain reaction(PCR) for Mycoplasma pneumoniae (MP) in children with MP pneumonia(MPP).Methods From Jun.2008 to Jan.2009,153 cases hospitalized with pneumonia were enrolled,and 30 cases without respiratory infection were enrolled as control group.Their respiratory secretion (including nasopharyngeal secretion,sputum,bronchialalveolar lavage fluid or pharyngeal swab) samples were collected for fluorescent quantitative PCR for MP.And their single or paired serums were collected for specific MP antibody detection.Results There were 123 cases confirmed with MPP by serology,among whom 114 cases were MP PCR positive.The quantitation of MP DNA was among 1.20?106-3.66?1010 gene copys/L. There were 30 cases with pneumonia negative with MP by the paired serum serology,among whom 2 cases were MP PCR positive,and the quantitation of MP DNA was (1.08-3.02)?107gene copys/L.All cases of control group were MP PCR negative.During the first and second weeks of the MPP onset,the sensitivity of MP-IgM from the first single blood samples were 66.7% and 83.9%,respectively.While the sensitivity and specificity of MP PCR were 92.7% and 93.3%,respectively.From the third week of the disease onset,the sensitivity of MP-IgM from the first single blood samples increased to 90.9%-100%.The clinical manifestations of MPP were nonspecific.Conclusions PCR is superior to serology for early diagnosis on MP infection.Combination of the 2 methods may be helpful to early and accurate diagnosis on MP infection.
5.Treatment values of precise target delineation of chest MRI for lung cancer
Zhenying YI ; Zhiqiao XU ; Ning LI ; Ling GAO ; Yan ZHANG ; Yongwei TIAN ; Zhibo SONG
The Journal of Practical Medicine 2016;32(18):2959-2962
Objective To investigate the treatment values of precise target delineation of chest MRI for lung cancer Methods From August 2011 to February 2015 , 45 non-small cell lung cancer patients were given chest CT scans and MRI scans before radiotherapy , and then active target tumor delineation , then related influencing factors were analyzed. Results All patients completed CT scans and MRI positioning. For patients that it was difficult to identify lung tissue lesions caused by lung cancer through CT , their MRI imaging showed high signal and the boundaries between the tumor and surrounding normal tissue became relatively clear. Meanwhile , 20 patients of borders were diagnosed by CT , while 25 by MRI; 36 patients with lymph node metastasis were diagnosed by CT while 40 by MRI. The difference was statistically significant (P<0.05). Univariate logistic regression analysis showed that pathological type and atelectasis were the influence factors for CT and MRI tumor target delineation differences (P<0.05), and multivariate logistic regression analysis showed the atelectasis was the main factor (P<0.05). Conclusion Compared with CT, breast MRI can precisely delineate target to improve the accuracy of target localization before radiotherapy. It can help determine lymph node metastasis and avoid the impact of atelectasis then ensure the accuracy of radiotherapy.
6.Evidence of perineural invasion on early-stage cervical cancer and prognostic significance
Guonan ZHANG ; Yan YANG ; Yi ZHU ; Ling CUI ; Shijun JIA ; Yu SHI ; Shuiqin SONG ; Shiqiang XU
Chinese Journal of Obstetrics and Gynecology 2015;(9):673-678
Objective To evaluate the incidence and significance of perineural invasion (PNI) in cervical cancer. Methods Retrospective chart review of patients with cervical cancer (stages Ⅰa2-Ⅱb) who underwent radical hysterectomy and pelvic lymphadenectomy from 2007 to 2012. To evaluate the incidence and significance of PNI in cervical and uterine tissues by microscopic examination. Results A total of 238 patients were included, 9.2% (22/238) patients with PNI in the cervical stroma. Patients with PNI were more likely to have adverse histopathologic features, including lymphoma vascular space invasion, parametrical invasion, depth of invasion, tomor size and lymph nodes metastases (all P<0.05). PNI were independent of age, international federation of gynecology and obstetrics (FIGO) stage, histopathology type and grade, and positive vaginal margin (all P>0.05). Patients with PNI had shorter disease-free and overall survival (P=0.002 and P=0.008, respectively). On multivariate analysis, risk factors for recurrence and death included parametrical invasion and depth of invasion (P<0.05). Similarly, risk factors for recurrence included lymph nodes metastases (P=0.024). However, PNI was not identified as an independent risk factor for either recurrence or death (P>0.05). Conclusions PNI exists in early cervical cancer. PNI is associated with tumor size, depth of invasion, parametrical invasion, lymphoma vascular space invasion and lymph nodes metastases. PNI represente a decreasing disease-free and overall survival in patients with early-stage cervical cancer, and is independently associated with multiple high-risk factors, which be informed management decisions regarding adjuvant therapy.
7.Effects of Bushen Huoxue Prescription on Granulosa Cell Apoptosisi of Premature Ovarian Failure Mice
Huiping LIU ; Yi XIAO ; Ling LI ; Peng QI ; Yan SONG ; Jiajun LI ; Haiqing YI ; Chao KE ; Guomin ZHANG
Chinese Journal of Information on Traditional Chinese Medicine 2015;(4):47-50
Objective To discuss Bushen Huoxue Prescription mechanism of action on follicular granulosa cell apoptosis of premature ovarian failure (POF) mice. Methods The mouse zona pellucida 3 as the antigen, multi-point injection of subcutaneous immunization BALB/c to female mice was used to establish autoimmune POF model. Forty clean female mice were randomly divided into blank group, model group, Estradiol Valerate group and Bushen Huoxue Prescription group. All medicine groups were given relevant medicine for gavage, while model and blank groups were given normal saline with the same amount for gavage for 15 days. After the treatment, ovary, uterus, and thymus were weighed, and the viscera index was calculated. An ovarian slice was taken and HE staining was used to observe granulosa cell apoptosis. The levels of E2, LH, and FSH were detected by using the radioimmunoassay method. RT-PCR was used to analyze Fas and Fas-L mRNA expressions in ovarian granulosa cells. Results Compared with blank group, the weight of ovary, thymus, and uterus decreased significantly (P<0.05, P<0.01);Serum E2 level dropped (P<0.01);levels of FSH and LH, and expressions of Fas and Fas-L mRNA increased significantly (P<0.01). Compared with model group, granulosa cell apoptosis significantly decreased, and ovary index, uterus index, and thymus index increased (P<0.05);serum E2 level increased (P<0.01);levels of FSH and LH, and expressions of Fas and Fas-L mRNA significantly decreased (P<0.05). Conclusion Bushen Huoxue Prescription can decrease expressions of Fas and Fas-L mRNA to inhibit cell apoptosis by adjusting the hormone level of hypothalamus-pituitary-ovarianaxis.
8.Two new phragmalin-type limonoid orthesters from Chukrasia tabularis var. velutina.
Jun LUO ; Jun-song WANG ; Ling-bo WANG ; Ling-yi KONG
Acta Pharmaceutica Sinica 2011;46(2):183-187
As a part of our ongoing research program to isolate novel phragmalin limonoids from the stem bark of Chukrasia tabularis var. velutina, two new phragmalin limonoids orthesters, tabularin Q (1) and tabulalide O (4), along with two known compounds tabularin C (2) and tabularin H (3) were isolated. Their structures were elucidated by means of extensive 1D and 2D spectroscopic analyses which included HSQC, HMBC, and ROESY experiments and HR-ESI-MS.
Limonins
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chemistry
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isolation & purification
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Meliaceae
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chemistry
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Molecular Structure
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Plant Bark
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chemistry
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Plants, Medicinal
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chemistry
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Spectrometry, Mass, Electrospray Ionization
9.Nutritional risk screening and nutrition assessment for gastrointestinal cancer patients.
Yan-ping DU ; Ling-ling LI ; Qing HE ; Yun LI ; Hu SONG ; Yi-jia LIN ; Jun-sheng PENG
Chinese Journal of Gastrointestinal Surgery 2012;15(5):460-463
OBJECTIVETo investigate the nutritional status, and provide evidence for nutritional treatment option.
METHODSA total of 452 patients with gastrointestinal cancer were selected, including 156 gastric cancer,117 colon cancer, and 180 rectal cancer. The nutritional risk screening 2002(NRS2002) was applied to grade the nutritional risk. A multi-frequency bioelectrical impedance analysis was used to measure the patients' body composition. Albumin (Alb), prealbumin(PA), transferring(Tf), retinol binding protein(RBP), red blood cell(RBC), hemoglobin (Hb), haematocrit(Hct) were measured after fasting.
RESULTSThe rate of patients with NRS2002 score more than 3 was 70.5%(110/156) for gastric cancer, 53.8%(63/117) for colon cancer, and 46.7%(86/180) for rectal cancer. The score for impaired nutritional status more than 1 for gastric cancer was higher than that for colorectal cancer(P<0.05), while patients with disease score more than 2 was less for gastric cancer(P<0.05). Body mass index(BMI), obesity degree, fat content, fat percentage, and arm circumference were lower in gastric cancer patients as compared to colorectal cancer patients(P<0.05); but protein percentage, muscle percentage, ratio of muscles of arm, and cell mass percentage were higher in gastric cancer patients(P<0.05). The proportions of patients with low Alb, PA, Tf, BC, Hb, Hct were higher for gastric cancer and colon cancer(P<0.05).
CONCLUSIONPatients with gastric cancer are prone to fat loss and therefore have a higher nutritional risk and malnutrition than those with colorectal cancer. Combination of body composition analysis and laboratory examination may achieve comprehensive evaluation of the nutritional status of patients, and provide the evidence of nutritional therapy by being combined with NRS2002 score.
Female ; Gastrointestinal Neoplasms ; Humans ; Male ; Middle Aged ; Nutrition Assessment ; Nutritional Status ; Risk Factors
10.Preparation of in situ gel systems for the oral delivery of ibuprofen and its pharmacokinetics study in beagle dogs.
Rui-ling WU ; Chun-shun ZHAO ; Jing-wen XIE ; Shao-ling YI ; Hong-tao SONG ; Zhong-gui HE
Acta Pharmaceutica Sinica 2008;43(9):956-962
The in situ gel systems can form gel in situ after administration to achieve sustained release, thus provides a promising strategy for drug delivery systems. The aim of this study was to design and prepare in situ gel systems for the oral delivery of ibuprofen (IBU-ISG) and study its pharmacokinetics in Beagle dogs. The characteristics of the basic material of gellan gum (Kelcogel, Kel) and sodium alginate (Manugel, M) were studied through investigating the complex viscosity of the Kel or M solution with or without different concentrations of calcium ion or sodium citrate to ascertain the amount range of the excipients. The measurement of complex viscosity of the solution (0. 5% Kel and 1% M) with different concentrations of sodium citrate and calcium ion was carried out to select the suitable proportion of calcium ion and sodium citrate. The formulation of binary IBU-ISG was optimized by monitoring the complex viscosity before gelling in vitro release property. The optimized formulation contains 1.0% sodium alginate, 0.5% gellan gum, 0. 21% sodium citrate and 0.056% calcium chloride. A single oral dose of IBU-ISG and reference formulation (IBU suspension) were given to each of the 6 healthy Beagle dogs, ibuprofen in plasma at different sampling times was determined by RP-HPLC. The pharmacokinetics parameters in 6 Beagle dogs were calculated. The Tmax of IBU-ISG and reference formulation were (1.8 +/- 0.6) and (0.4 +/- 0. 1) h. The Cmax values were (29.2 +/- 7.6) and (37.8 +/- 2.2) microg x mL(-1). The T(1/2) were (2.3 +/- 0.5) and (2.0 +/- 0.9) h, and the AUC(0-t) were (131.0 +/- 38.6) and (117.3 +/- 23.1) microg x mL(-1) x h, respectively. The binary IBU-ISG was successfully prepared.
Administration, Oral
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Alginates
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chemistry
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Analgesics, Non-Narcotic
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administration & dosage
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blood
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pharmacokinetics
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Animals
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Area Under Curve
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Calcium Chloride
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chemistry
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Citrates
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chemistry
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Delayed-Action Preparations
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Dogs
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Drug Compounding
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methods
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Drug Delivery Systems
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Excipients
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Female
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Glucuronic Acid
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chemistry
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Hexuronic Acids
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chemistry
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Ibuprofen
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administration & dosage
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blood
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pharmacokinetics
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Male
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Polysaccharides, Bacterial
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chemistry
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Viscosity