2.Application of methyl in drug design.
Jie LIAN ; Jiang WANG ; Haifeng SUN ; Daizong LIN ; Hong LIU
Acta Pharmaceutica Sinica 2013;48(8):1195-208
The methyl group plays an important role in the rational drug design. Introducing methyl into small molecules has become an important strategy of lead compound optimization. The application of methyl in drug design is reviewed in this paper. Methyl can modulate the physicochemical, pharmacodynamic, and pharmacokinetic properties by ortho effect, inductive effect, and conformational effect. It also improves the metabolic stability as a soft metabolic point. In addition, introducing methyl into drug molecules can also be applied as a strategy in new uses of old drugs and generate me-too drugs.
3.Selection of Different Occluders in Transcatheter Closure of Congenital Ventricular Septal Defect in Children
lei, GAO ; mi-lin, ZHANG ; shi-jie, CUI ; qi-lian, XIE ; zhen, WANG ; hui-lian, TAN ; xiao-li, ZHU
Journal of Applied Clinical Pediatrics 1986;0(01):-
Objective To discuss the methods of selecting different shapes occluder and to evaluate the feasibility,safety and efficacy of them in transcatheter closures of congenital ventricular septal defect (VSD) in children.Methods Transcatheter closures were performed in 226 children with congenital VSD,age ranging from 2 to 14 years(mean 5.62 years) under the guidance of transthoracic echocardiography(TTE) and fluoroscopy.There were 14 patients with intracristal VSD,209 patients with perimembranous VSD and 3 patients with muscular VSD.Left ventriculography and transthoracic echocardiography were performed repeatedly after the procedure to assess the effect of occlusion.The echocardiography and electrocardiography were scheduled before discharge,1,6 and 12 months for the follow-up.Results The occluders were deployed successfully in 211 patients.The successful rate was 93.4%.Thin waist shape occluders,were deployed in 7 patients;equal side shape occluders,were deployed in 191 patients;eccentric shape occluders were deployed in 12 patients,and muscular defect occluders were deployed in 1 patient.There were no complications encountered during or after closure.Conclusions It is very important in transcatheter closure of congenital in children to select different shape occluder according to pathologic characteristics.In general,equal side shape occluder is suita-ble for a large number of defect and it is easy for deployment.In some conditions,the other shape occluder may be necessary.
4.Vertebroplasty with bone cement in the treatment of osteoporotic vertebral compression fractures A 6-year follow-up
Lian REN ; Zhizhong LI ; Jie SUI ; Yongxin LIN ; Genlong JIAO ; Guodong SUN
Chinese Journal of Tissue Engineering Research 2012;16(12):2110-2114
BACKGROUND: Percutaneous vertebroplasty for osteoporotic vertebral compression fractures has achieved very good results, but its long-term efficacy as well as impact on patients has been rarely reported so far.OBJECTIVE: To investigate the long-term effect of vertebroplasty with bone cement on osteoporotic vertebral compression fractures through a follow-up.METHODS: Thirty-four patients with osteoporotic vertebral compression fractures who had undergone percutaneous vertebroplasty were recruited. Visual analogue scale scoring was measured and compared as well as lesioned vertebral height and kyphosis angle shown on lateral X-ray examination prior to, 1 week and 6 years after percutaneous vertebroplasty.RESULTS AND CONCLUSION: The kyphosis angle was improved 1 week and 6 years after percutaneous vertebroplasty, and it changed insignificantly during the follow-up period. The vertebral height was also improved significantly after percutaneous vertebroplasty (P < 0.01); however, there was no obvious variation in the vertebral height at 1 week and 6 years after percutaneous vertebroplasty. The visual analogue scale exhibited an improvement after percutaneous vertebroplasty (P < 0.01); however, with time going by, the scoring on the visual analogue scale had an increased tend. All the parameters remained stable and had no large fluctuations. It is proved that the percutaneous vertebroplasty is effective and safe to treat osteoporotic vertebral compression fractures with an excellent long-term effect.
5.Research on the training strategy of medical research ability based on the practice ability
Yan LIN ; Haiying DONG ; Wei XIAO ; Li JIN ; Bo LI ; Jie LIAN ; Haijun MU ; Xiaojie ZHANG
Chinese Journal of Medical Education Research 2016;15(11):1098-1100,1101
Practice abilityoriented professional quality training is an important part of thethree orientation talent training mode in Qiqihar Medical School, and it is the key link of the reform and inno-vation of talent training mode. This article mainly expounds the connotation of training mode in the three orientation under the guidance of medical personnel and medical research ability, and the training objec-tives cover innovative thinking ability and scientific research ability, including five aspects of training strat-egy such as reforming the teaching mode of the traditional theory course, setting up scientific research related courses, carrying out academic lecture, reforming the teaching mode of experiment course and con-structing the scientific research team of teachers and students by the scientific research project as well as seven aspects of the evaluation system, such as the literature review, the title of the report, academic report and research application writing, scientific research (comprehensive) experiment report, thesis writing and comprehensive performance, and deeply analyzes the close relationship between the practice ability and the medical research ability of medical students.
6.Effects of "three ways" method of acupuncture on serum levels of tumor necrosis factor-alpha and interleukin-1beta patients with acute ischemic cerebrovascular diseases.
Jie JI ; Hui-lin LIU ; Jin-lian CHENG
Chinese Journal of Integrated Traditional and Western Medicine 2006;26(6):500-503
OBJECTIVETo observe the effect of "Three ways" method of acupuncture on serum levels of tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) in patients with acute ischemic cerebrovascular diseases (ICVD).
METHODSSixty patients with acute cerebral infarction were randomly divided into the treated group treated by "Three ways" method of acupuncture and the control group by hand and foot acupuncture on acupoints of the hands and feet. Serum levels of TNF-alpha and IL-1beta were detected with radioimmunoassay before treatment and at the 6th, 12th and 28th days of treatment. Neurological deficit score (NDS) and Barthel Index (BI) were also observed in the same time.
RESULTSAfter treatment, serum levels of TNF-alpha and IL-1beta in both groups decreased significantly (P < 0.05), approaching the normal range at the 28th day of treatment, which were even lower in the treated group than those in the control group, and the decreasing trend were significantly different (P < 0.05). Compared with the control group, the effect in decreasing NDS and increasing BI in the treated group was better than that in the control group (P < 0.05).
CONCLUSION"Three ways" method of acupuncture could reduce serum levels of TNF-alpha and IL-1beta, alleviate injury of nervous function so as to improve the daily life ability, superior to hand and foot acupuncture.
Acupuncture Therapy ; methods ; Adult ; Aged ; Cerebral Infarction ; blood ; therapy ; Female ; Humans ; Interleukin-1beta ; blood ; Male ; Middle Aged ; Tumor Necrosis Factor-alpha ; blood
7.Application of methyl in drug design.
Jie LIAN ; Jiang WANG ; Hai-Feng SUN ; Dai-Zong LIN ; Hong LIU
Acta Pharmaceutica Sinica 2013;48(8):1195-1208
The methyl group plays an important role in the rational drug design. Introducing methyl into small molecules has become an important strategy of lead compound optimization. The application of methyl in drug design is reviewed in this paper. Methyl can modulate the physicochemical, pharmacodynamic, and pharmacokinetic properties by ortho effect, inductive effect, and conformational effect. It also improves the metabolic stability as a soft metabolic point. In addition, introducing methyl into drug molecules can also be applied as a strategy in new uses of old drugs and generate me-too drugs.
Drug Design
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Hydrophobic and Hydrophilic Interactions
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Lipid Metabolism
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Methylation
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Pharmaceutical Preparations
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chemical synthesis
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chemistry
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metabolism
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Solubility
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Stereoisomerism
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Structure-Activity Relationship
8.Langerhans cell sarcoma of talus: report of a case.
Ya-li LIAN ; Hui-ying HE ; Song-lin LIAO ; Li-jun YIN ; Zhi-hui HAN ; Jie ZHENG
Chinese Journal of Pathology 2006;35(11):697-698
Bone Neoplasms
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metabolism
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pathology
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surgery
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Diagnosis, Differential
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Female
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Humans
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Immunohistochemistry
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Langerhans Cell Sarcoma
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metabolism
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pathology
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surgery
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Middle Aged
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S100 Proteins
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metabolism
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Talus
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Vimentin
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metabolism
9.Resveratrol alleviates ISO-induced cardiomyocyte hypertrophy in rat
Jun WANG ; Wei XIAO ; Bo LI ; Li JIN ; Xiuwen YU ; Jie LIAN ; Mengyao LI ; Xinpeng LI ; Jinyu ZHOU ; Yan LIN
Basic & Clinical Medicine 2017;37(9):1226-1230
Objective To explore the role of resveratrol (RES) on cardiomyocyte hypertrophy of rat induced by isoproternol (ISO) and the effect of Res on the expression of GRP78 and GRP94 in endoplasmic reticulum stress of cardiomyocyte hypertrophy.Methods Hypertrophic model of cardiomyocytes was induced by ISO.Cardiomyocytes was divided into four group: control group, the model group, RES+ISO group and RES group.Hypertrophy status of cardiomyocytes was determined by Leica 2Q500 image analysis system measuring the cell surface area and the gene expression of ANP.The content of LDH and MDA was measured in different groups, and the protein expressions of GRP78 and GRP94 were detected by Western blot.Results Compared with control group, ISO induced cardiomyocytes hypertrophy, endoplasmic reticulum stress related factors GRP78 and GRP94 protein expression were increased, compared with ISO group, RES intervention effectively suppressed the cardiomyocytes hyper-trophy induced by ISO, reduced the protein expression of GRP78 and GRP94, at the same time, reduced lactate dehydrogenase (LDH) and malondialdehyde (MDA) release in cell medium.Conclusions Treatment of RES may protect cardiomyocytes hypertrophy, which is partially mediated by inhibiting the expression of ERS factors GRP78 and GRP94.
10.Anti-feeding activity of total ginsenoside from Panax ginseng to 4th-instar Mythimna separata larvae.
Shi-qiang TAN ; Lin MA ; Yong-hua XU ; Feng-jie LEI ; Ai-hua ZHANG ; Lian-xue ZHANG
China Journal of Chinese Materia Medica 2015;40(14):2787-2791
This paper is in order to study the anti-feeding and growth inhibition activity of toatal ginsenoside of ginseng stems and leaves against 4th-instar Mythimna separata larvae. Simulating natural growing condition indoors, on the base, To study the anti-feeding and growth inhibition activity of toatal ginsenoside against 4th-instar M. separata larvae by leaf disc test. The toatal ginsenoside appeared to be of significant antifeeding activity against 4th-instar M. separata larvae. The 4th-instar M. separata larvae fed on the leaves of Sorghum bicolor treated with 20, 10, 5 g · L(-1) toatal ginsenoside. At 8 h, non-selective anti-feeding rate were 88.67%, 64.40% and 47.36%, and selective anti-feeding rate were 62.49% , 44.29% and 34.19%; Compared with the photographic, The toatal ginsenoside conld make the development period had prolonged 13h in treated group. The toatal ginsenoside had significant inhibition effect on feeding and growth and development against 4th-instar M. separata larvae, and inhibition effect increases as the increase of concentration ginsenoside.
Animals
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Ginsenosides
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pharmacology
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Insecticides
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pharmacology
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Larva
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Moths
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growth & development
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Panax
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chemistry