1.Recent developments of drug eluting stent coatings.
Wen-ping CHEN ; Hong-bing ZHAN
Acta Pharmaceutica Sinica 2011;46(11):1301-1307
Drug eluting stents (DESs) have revolutionized the interventional cardiology over the past decade since the first DES became commercially available in Europe in 2002. Compared to bare metal stents that are deployed to keep the vessel open by mechanical force, DESs have an additional function of reducing restenosis by the action of the drug on the target site. Coatings on the stent surface which ensure the maximum delivery of therapeutic agents to the target site with minimal systematic toxicity, also play an important role in adjusting the drug release profile. Coating material and technology not only affect the surface biocompatibility and the integrity maintenance during the implanting process, but also decide the way of drug delivering and transmitting from the coating. This paper reviews the basic principles of DES coating design, the categories of DES coatings, the commonly used clinical DES coatings and their efficiency in reducing restenosis, and finally provides the future perspectives for DES coatings.
Biocompatible Materials
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Drug Carriers
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Drug Delivery Systems
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Drug-Eluting Stents
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Lactic Acid
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Phosphorylcholine
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Polyethylenes
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Polyglycolic Acid
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Prosthesis Design
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Titanium
2.The pathogenesis of cartilage erosion of rheumatoid arthritis and the development of animal model by engraftment of RA synovium and normal human cartilage under the kidney capsule of the SCID mice
Zhan-Guo SHI ; Ping ZHU ; Jun-Feng JIA ; Ning LU ; Jin-Kang ZHAO ; Hong-Ming LI ; Yan-Hong WANG ; Chun-Mei FAN ; Li-Bing XIAO
Chinese Journal of Rheumatology 2003;0(08):-
Objective To develop the humanized animal model for RA cartilage erosion,and study the mechanisms of its pathogenesis.Methods RA synovium and normal human cartilage under the kidney cap- sule of the SCID mice were engrafted,and were maintained for 4~16 weeks.In addition,mice underwent simi- lar surgery except the engraftment served as controls.After 4,8,12 or 16 weeks,the mice were killed and the grafts were harvested and the cartilage destruction was assessed histologically by haematoxylin/eosin-stained paraffin sections.Results Histological examination revealed the presence of infiltration of RA synovium cells into the cartilage after 4 weeks and the cartilage was destructed evidently.These studies demonstrated that the RA-SCID model maintained many of the phenotypic and functional features of RA.Conclusion This RA-SCID mouse is a useful animal model for study of the pathogenesis and the development of new drugs for RA patients.
3.Derivatization of berberine based on its synergistic antifungal activity with fluconazole against fluconazole-resistant Candida albicans.
Shu-Juan TIAN ; Yue GAO ; Cheng-Xu ZANG ; Zhan CAI ; Ting-jun-hong NI ; Shan-Lun TAN ; Yong-Bing CAO ; Yuan-Ying JIANG ; Da-Zhi ZHANG
Acta Pharmaceutica Sinica 2014;49(11):1563-1568
Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole. Preliminary SAR of berberine needs to be studied for the possibility of investigating its target and SAR, improving its drug-likeness, and exploring new scaffold. In this work, 13-substitutited benzyl berberine derivatives and N-benzyl isoquinoline analogues were synthesized and characterized by 1H NMR and MS. Their synergetic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The 13-substitutited benzyl berberine derivatives 1a-1e exhibited comparable activity to berberine, which suggested that the introduction of functional groups to C-13 can maintain its activity. The N-benzyl isoquinolines, which were designed as analogues of berberine with its D ring opened, exhibited lower activity than berberine. However, compound 2b, 2c, and 4b showed moderate activity, which indicated that berberine may be deconstructed to new scaffold with synergistic antifungal activity with fluconazole. The results of our research may be helpful to the SAR studies on its other biological activities.
Antifungal Agents
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pharmacology
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Berberine
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pharmacology
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Candida albicans
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drug effects
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Drug Resistance, Fungal
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Drug Synergism
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Fluconazole
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pharmacology
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Isoquinolines
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pharmacology
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Microbial Sensitivity Tests
4.D-limonene induces apoptosis of gastric cancer cells.
Xiao-guang LU ; Bing-an FENG ; Li-bin ZHAN ; Zhi-hong YU
Chinese Journal of Oncology 2003;25(4):325-327
OBJECTIVETo investigate the apoptosis effect induced by D-limonene on BGC-823 gastric cancer cells.
METHODSThe expression of p53, bc1-2 in BGC-823 cells and qualitative, quantitative index of cell apoptosis were detected with MTT, electron microscopy, flow cytometry and immunohistochemical method.
RESULTSD-limonene could induce the formation of apoptotic bodies in a dose- and time-dependent manner. The expression of bcl-2 protein decreased and p53 protein increased in BGC-823 cells treated with D-limonene, compared with the control cells.
CONCLUSIOND-limonene exerts its cytotoxic effect on BGC-823 gastric cancer cells by inducing apoptosis.
Adenocarcinoma ; metabolism ; pathology ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacology ; Apoptosis ; drug effects ; Cell Line, Tumor ; Cyclohexenes ; Dose-Response Relationship, Drug ; Humans ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Stomach Neoplasms ; metabolism ; pathology ; Terpenes ; administration & dosage ; pharmacology ; Tumor Suppressor Protein p53 ; metabolism
5.Clinical effects of atorvastatin in patients with acute ischemic stroke
Hong-Xia ZHOU ; Xing-Yuan WANG ; Li-Juan FAN ; Shan-Jin YANG ; Hong-Bing CAO ; Zhan-Ao WU
The Chinese Journal of Clinical Pharmacology 2016;32(1):72-74
Objective To explore the clinical effects of two doses of atorvastatin in patients with acute ischemic stroke .Methods A total of 128 patients with acute ischemic stroke were randomly divided into two groups ,64 cases in each group .The patients in atorvastatin 20 mg group were given atorvastatin 20 mg daily , and the patients of the atorvastatin 10 mg group were given atorvastatin 10 mg daily.The treatment lasted for six months.Blood lipid , nerve function defect grading , atherosclerotic plaque area and adverse drug reactions were observed before and after six months.Results The total effective rate in the atorvastatin 20 mg group (98.4%) was significantly higher than that in the atorvastatin 10 mg group (84.4%) (P<0.05).Blood lipid, nerve function defect grading and atherosclerotic plaque area were obviously improved in two groups (P<0.05), and the atorvastatin 20 mg group had a better improvement against the atorvastatin 10 mg group ( P <0.05 ) . The incidence of adverse drug reactions in two groups were 4.7%, no statistical signifi-cance (P>0.05).Conclusion Aatorvastatin 20 mg can better improve the clinical symptoms , blood lipid level as well as atherosclerotic plaque area in patients with acute ischemic stroke , accordingly improve the quality of life in those patients .
6.Utilization of high-resolution melting analysis to screen patients with neonatal intrahepatic cholestasis caused by citrin deficiency.
Peng-qiang WEN ; Guo-bing WANG ; Zhan-ling CHEN ; Dong CUI ; Xiao-hong LIU ; Li-fang YING ; Ping SONG ; Quan YUAN ; Shu-li CHEN ; Jian-xiang LIAO
Chinese Journal of Medical Genetics 2012;29(2):167-171
OBJECTIVETo assess the feasibility of high-resolution melting (HRM) analysis for screening patients with neonatal intrahepatic cholestasis caused by citrin deficiency (NICCD).
METHODSBased on previous studies on SLC25A13 gene in Chinese patients with NICCD, four hotspot mutations (851del4, 1638ins23, IVS6+5G>A and IVS16ins3kb) were selected. Results of the HRM analysis was validated using 50 negative controls and 20 patients with NICCD whose genotypes were confirmed previously by direct sequencing. With the established protocol, 171 suspected patients were enrolled. Samples with abnormal melting curves were further validated by DNA sequencing.
RESULTSHRM analysis can accurately determine the genotypes of all negative controls and patients. The sensitivity and specificity of the technique reached 100% (70/70). The melting curves of samples with the same genotype were highly reproducible. In 171 suspected patients, seven NICCD patients were detected by HRM. Identified mutations have included one case of 851del4 homozygote, one case of IVS6+5G>A heterozygote, 3 cases of 851del4 heterozygotes, one case of [IVS6+5G>A]+[ 851del4] and one case of [1638ins23+IVS16ins3kb]+[1638ins23]. All mutations were subsequently confirmed by DNA sequencing.
CONCLUSIONHRM analysis is a convenient, high-throughput and rapid technique for the screening of NICCD patients.
Anion Transport Proteins ; genetics ; Base Sequence ; Calcium-Binding Proteins ; deficiency ; China ; Citrullinemia ; diagnosis ; genetics ; metabolism ; DNA ; chemistry ; genetics ; Genetic Predisposition to Disease ; Genotype ; Humans ; Mitochondrial Proteins ; genetics ; Molecular Sequence Data ; Mutation ; Nucleic Acid Denaturation ; Organic Anion Transporters ; deficiency ; Sensitivity and Specificity
7.Resection of a giant renal angiomyolipoma in a solitary kidney with preoperative arterial embolization.
Wen-hao SHEN ; Jin-hong PAN ; Ju-nan YAN ; Zhi-wen CHEN ; Zhan-song ZHOU ; Gen-sheng LU ; Wei-bing LI
Chinese Medical Journal 2011;124(9):1435-1437
Renal angiomyolipoma is a type of benign tumor that occurs sporadically in addition to being associated with tuberous sclerosis. Preoperative embolization of large tumors is important to avoid excessive blood loss during surgery. We reported a patient with a 5505-g giant renal angiomyolipoma in a solitary kidney. The patient was treated with preoperative embolization and radical nephrectomy without complications. This type of treatment for an enormous angiomyolipoma can reduce the risk of uncontrolled hemorrhage caused by rupture of the tumor during the operation and should be considered for the treatment of similar tumors.
Adult
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Angiomyolipoma
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surgery
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Arteries
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surgery
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Embolization, Therapeutic
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methods
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Humans
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Kidney Neoplasms
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surgery
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Male
8.Analysis of clinical features and GCDH gene mutations in four patients with glutaric academia type I.
Peng -qiang WEN ; Guo-bing WANG ; Xiao-hong LIU ; Zhan-ling CHEN ; Yue SHANG ; Dong CUI ; Ping SONG ; Quan YUAN ; Shu-li CHEN ; Jian-xiang LIAO ; Cheng-rong LI
Chinese Journal of Medical Genetics 2012;29(6):642-647
OBJECTIVETo review clinical features of four male patients with glutaric academia type I and screen glutaryl-CoA dehydrogenase (GCDH) gene mutations.
METHODSThe 4 patients underwent brain computer tomography (CT) and magnetic resonance imaging (MRI) analyses. Blood acylcarnitine and urine organic acid were analyzed with tandem mass spectrometry and gas chromatographic mass spectrometry. Genomic DNA was extracted from peripheral blood samples. The 11 exons and flanking sequences of GCDH gene were amplified with PCR and subjected to direct DNA sequencing.
RESULTSAll patients have manifested macrocephaly, with head circumference measured 50 cm (14 months), 47 cm (9 months), 46 cm (5 months) and 51 cm (14 months), respectively. Imaging analyses also revealed dilation of Sylvian fissure and lateral ventricles, frontotemporal atrophy, subarachnoid space enlargement and cerebellar vermis abnormalities. All patients had elevated glutarylcarnitine (5.8 umol/L, 7.5 umol/L, 8.3 umol/L and 7.9 umol/L, respectively) and high urinary excretion of glutaric acid. Seven mutations were identified among the patients, among which c.146_149del4, IVS6-4_Ex7+4del8, c.508A>G (p.K170E), c.797T>C (p.M266T) and c.420del10 were first discovered.
CONCLUSIONMacrocephaly and neurological impairment are the most prominent features of glutaric academia type I. Blood tandem mass spectrometry and urine gas chromatographic mass spectrometry analysis can facilitate the diagnosis. The results can be confirmed by analysis of GCDH gene mutations.
Amino Acid Metabolism, Inborn Errors ; diagnosis ; genetics ; metabolism ; Amino Acid Sequence ; Base Sequence ; Brain Diseases, Metabolic ; diagnosis ; genetics ; metabolism ; Glutaryl-CoA Dehydrogenase ; deficiency ; genetics ; metabolism ; Humans ; Infant ; Male ; Molecular Sequence Data ; Mutation ; Sequence Alignment
9.Clinical investigation and mutation analysis of a child with citrin deficiency complicated with purpura, convulsive seizures and methioninemia.
Peng-qiang WEN ; Guo-bing WANG ; Zhan-ling CHEN ; Xiao-hong LIU ; Dong CUI ; Yue SHANG ; Cheng-rong LI
Chinese Journal of Medical Genetics 2013;30(6):649-653
OBJECTIVETo analyze the clinical features and SLC25A13 gene mutations of a child with citrin deficiency complicated with purpura, convulsive seizures and methioninemia.
METHODSThe patient was subjected to physical examination and routine laboratory tests. Blood amino acids and acylcarnitines, and urine organic acids and galactose were analyzed respectively with tandem mass spectrometry and gas chromatographic mass spectrometry. SLC25A13 gene mutation screening was conducted by high resolution melt (HRM) analysis.
RESULTSThe petechiae on the patient's face and platelet count (27×10(9)/L, reference range 100×10(9)/L-300×10(9)/L) supported the diagnosis of immunologic thrombocytopenic purpura (ITP). Laboratory tests found that the patient have abnormal coagulation, cardiac enzyme, liver function and liver enzymes dysfunction. Tandem mass spectrometry also found methionine to be increased (286 μmol/L, reference ranges 8-35 μmol/L). The patient did not manifest any galactosemia, citrullinemia and tyrosinemia. Analysis of SLC25A13 gene mutation found that the patient has carried IVS16ins3kb, in addition with abnormal HRM result for exon 6. Direct sequencing of exon 6 revealed a novel mutation c.495delA. The same mutation was not detected in 100 unrelated healthy controls. Further analysis of her family has confirmed that the c.495delA mutation has derived from her farther, and that the IVS16ins3kb was derived from her mother.
CONCLUSIONThe clinical features and metabolic spectrum of citrin deficiency can be variable. The poor prognosis and severity of clinical symptoms of the patient may be attributed to the novel c.495delA mutation.
Amino Acid Metabolism, Inborn Errors ; genetics ; pathology ; Calcium-Binding Proteins ; deficiency ; genetics ; DNA Mutational Analysis ; methods ; Female ; Glycine N-Methyltransferase ; deficiency ; genetics ; Humans ; Infant ; Mitochondrial Membrane Transport Proteins ; genetics ; Organic Anion Transporters ; deficiency ; genetics ; Pedigree ; Purpura ; genetics ; pathology ; Seizures ; genetics ; pathology
10.Comparison of surgical treatment in single thoracolumbar-lumbar adolescent idiopathic scoliosis: anterior versus posterior surgery.
Shi-qiang ZHAN ; Yun-bing CHANG ; Shi-xing ZENG ; Yi-sheng WANG ; Yu-hong KE ; Yuan-chen MA
Chinese Journal of Surgery 2010;48(6):419-422
OBJECTIVETo retrospectively compare the clinical outcomes of anterior and posterior surgical treatment in single thoracolumbar-lumbar adolescent idiopathic scoliosis.
METHODSBetween January 2004 and August 2008, 22 female patients, averaged 14.5 years old (12 to 18 years), of thoracolumbar-lumbar adolescent idiopathic scoliosis were corrected by anterior correction and fusion. At the same time, 20 female patients, average 14.8 years old (11 to 19 years), were corrected by posterior segmental pedicle screw correction and fusion. Operation time, SRS-24 score, intraoperative blood loss, and coronal and sagittal plane correction were compared between the two groups.
RESULTSAll patients were followed up for 12 to 63 months, the mean follow-up time was 28.3 months. Operation time was (334 + or - 36) min in anterior group and (292 + or - 17) min in posterior group; intraoperative blood loose was (940 + or - 207) ml in anterior group and (596 + or - 227) ml in posterior group; fusion levels were (5.2 + or - 0.8) in anterior group and (6.7 + or - 1.2) in posterior group. There were statistically significant difference in operation time, intraoperative blood loss and fusion levels (P < 0.05). Coronal correction was (93 + or - 5)% in anterior group and (88 + or - 5)% in posterior group. SRS-24 scores averaged 98 in anterior group and averaged 94 in posterior group. There was no statistical difference in coronal correction or SRS-24 scores (P > 0.05).
CONCLUSIONSPosterior surgery has the same correction results compared with anterior surgery in treating thoracolumbar-lumbar adolescent idiopathic scoliosis. Posterior surgery takes less operation time, brings less trauma but has longer fusion levels.
Adolescent ; Child ; Female ; Follow-Up Studies ; Humans ; Lumbar Vertebrae ; surgery ; Retrospective Studies ; Scoliosis ; surgery ; Spinal Fusion ; methods ; Thoracic Vertebrae ; surgery ; Treatment Outcome ; Young Adult