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Synthesis and antitussive evaluation of verticinone-cholic acid salt,a novel and potential cough therapeutic agent

Acta Pharmacologica Sinica 2007年第10期28卷 1591-1596页

作者： Fang-zhou XU~(2,3),Chang CHEN~2,Yong-hui ZHANG~2,Han-li RUAN~2,Hui-fang PI~2,Pong ZHANG~2,Ji-zhou WU~(2,4)~2 Faculty of Pharmaceutical Sciences,Tongji Medical College,Huazhong university of Science and Technology,Wuhan 430030,china~3 department of Pharmacy,peking university.shenzhen hospital,shenzhen 518036,china Faculty of Pharmaceutical Sciences Tongji Medical College Huazhong University of Science and Technology Wuhan China department of Pharmacy Peking University Shenzhen Hospital Shenzhen China

Aim:To seek a novel and potent antitussive drug based on Shedan-Chuanbeipowder,a complex of traditional Chinese medicine preparation for cough ***:Verticinone-cholic acid (Ver-CA) salt,a novel,salifying derivative ofverticinone and cholic acid,both of which are the major bioactive components inShedan-Chuanbei powder,was *** then evaluated the antitussiveactivity and the acute toxicity of the ***:The new compound,with goodsolubility in water,has much more potent antitussive activity in comparison withthe same dose of single verticinone and single cholic *** administration 3mg/kg of Ver-CA could result in over 50% reduction of a citric acid-induced *** with naloxone (0.8 mg/kg,ip) can only partially antagonize its anti-tussive *** the other hand,glybenclamide (3 mg/kg,ip),an ATP-sensitiveK~+ channel blocker,can also significantly reduce the antitussive effect of Ver-CA.A further acute toxicity study showed that the LD50values of Ver-CA were 3 timesthat of ***:Based on the studies of pharmacology and acutetoxicity,the salt has a synergic and attenuated toxicity compared with singleverticinone and cholic ***,the present study also suggests that Ver-CA,a potential novel antitussive agent,may exert its antitussive effect via boththe peripheral (modulated by ATP-sensitive K~+ channels) and central mechanisms(modulated by the opioid receptor).

关键词： verticinone-cholic acid salt Shedan-Chuanbei powder,cholic acid verticinone antitussive effect ATP-sensitive K~+ channels

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Effectiveness of Combined Testosterone Undecanoate with Tamoxifen Citrate Treatment in Men with Idiopathic Azoospermia or Serious Oligozoospermia

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Journal of Reproduction and Contraception 2012年第4期23卷 254-258页

作者： Bo SONG Wei-ping QIAN Guangdong Key Lab. Male Reproductive medicine & Genetics Reproductive Medicine Department Shenzhen Hospital Peking University

Objective To assess the effect of treatment with a combination of the tamoxifen citrate and testosterone undecanoate on sperm variables in men with idiopathic azoospermia or oIigozoospermia. Methods Four men with idiopathic azoospermia and 8 men with idiopathic oligozoospermia were collected in this retrospective and self control trial. All patients were treated with testosterone undecanoate of 80 mg/d and tamoxifen citrate of 20 mg/d. Sperm characteristics and pregnancy incidence were measured every month during 4 months medication. Results Tamoxifen citrate plus testosterone undecanoate treatment produced a satisfactory improvement of total sperm number, motility after 2 and 3 months whereas serum FSH, LH levels increased after 2 or 3 months. Conclusion The combination of tamoxifen citrate with testosterone undecanoate could improve significantly sperm count. The combination could be used in men with idiopathic azoospermia or serious oligozoospermia.

关键词： testosterone tamoxifen citrate oligozoospermia azoospermia

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Human papillomavirus DNA and P16～(INK4A) expression in concurrent esophageal and gastric cardia cancers

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World Journal of Gastroenterology 2010年第46期16卷 5901-5906页

作者： Guang-Cheng Ding,Tao Guo,department of Gastroenterology,The First Affiliated hospital and The Fifth Affiliated hospital,Zhengzhou university,Zhengzhou 450052,Henan Province,china Jing-Li Ren,Xin Song,Sheng-Li Zhou,Zong-Min Fan,LiDong Wang,Henan Key laboratory for Esophageal Cancer Research,department of Gastroenterology,The First Affiliated hospital,College of Basic medicine,Zhengzhou university,Zhengzhou 450052,Henan Province,china Fu-Bao Chang,department of Thoracic Surgery,Linzhou Center hospital,Linzhou 456500,Henan Province,china Ji-Lin Li,department of pathology,Yaocun Esophageal Cancer hospital,Linzhou 456500,Henan Province,china Ling Yuan,department of Oncoradiotherapy,Henan Province Tumor hospital,Zhengzhou 450003,Henan Province,china Yi Zeng,Institute of Virology,Chinese Academy of Preventive medicine,Beijing 100052,china Henan Key laboratory for Esophageal Cancer Research Department of Gastroenterology The First Affiliated Hospital College of Basic Medicine Zhengzhou University Zhengzhou 450052 Henan Province China.

AIM:To investigate the relationship between human papillomavirus (HPV) infection and concurrent esophagus and gastric cardia cancer from the same patient (CC) and examine the significance of P16 INK4A protein ***:Polymerase chain reaction was used to detect the presence of HPV type16 (HPV16).The expression of P16 INK4A protein was detected using ***:Among the CC specimens,HPV16-DNA was found in eight cases of esophageal squamous cell carcinoma (ESCC) and five cases of gastric cardia adenocarcinoma (GCA),respectively (47% vs 29%),and two of both ESCC and GCA.P16 INK4A was highly expressed in both ESCC and *** the HPV-associated positive CC,higher P16 INK4A expression was observed in the GCA than in the ESCC (75% vs 25%,P 5).CONCLUSION:HPV16 as a correlated risk factor may play an important role in the development of ESCC and GCA.P16 INK4A may be a screening index in the HPVassociated carcinoma of gastric cardia.

关键词： Esophageal squamous cell carcinoma Gastric cardia adenocarcinoma Human papillomavirus Polymerase chain reaction Immunohistochemistry

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Chemokine RANTES is upregulated in monocytes from patients with hyperhomocysteinemia

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Acta Pharmacologica Sinica 2005年第11期26卷 1317-1321页

作者： Wei SUN~(2,5), Guang WANG~(3,5), Zhen-min ZHANG~4, Xiao-kun ZENG~2, Xian WANG~(2,4,6) ~2 Institute of Vascular medicine ~3 department of Gerontology, peking university Third hospital ~4 department of Physiology and Pathophysiology, Key laboratory of Molecular Cardiovascular Science, Ministry of Education, Basic Medical College, peking university, Beijing 100083, china Institute of Vascular medicine Peking University Third Hospital Beijing China department of Gerontology Peking University Third Hospital Beijing China department of Physiology and Pathophysiology Key Laboratory of Molecular Cardiovascular Science Ministry of Education Basic Medical College Peking University Beijing China

Aim: To investigate the changes in plasma level of the chemokine RANTES (regulated upon activation, normal T cells expressed and secreted) and the responsiveness of lipopolysaccharide (LPS)-induced RANTES secretion from monocytes in patients with hyperhomocysteinemia (HHcy). Methods: The plasma levels of homocysteine (Hcy), folate, and RANTES were measured in 38 control patients with normal Hcy levels and 40 patients with HHcy and the mRNA synthesis of RANTES in isolated human monocytes was determined by RNase protection assays. Results: The plasma level of RANTES was elevated in HHcy patients compared with controls (median 5.3 vs 3.5 ng/mL, P<0.01). LPS-induced RANTES production from monocytes of HHcy patients was also increased significantly. In addition, Hcy directly increased the mRNA level of RANTES in isolated normal human monocytes in a time- and dose-dependent manner. Conclusion: Upregulated RANTES from monocytes in HHcy patients may be involved in the atherogenesis of HHcy-induced atherosclerosis.

关键词： homocysteine monocytes RANTES folic acid atherosclerosis humans

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Evidence-based expert consensus on clinical management of safety of Bruton’s tyrosine kinase inhibitors(2024)

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Chinese Journal of Cancer Research 2024年第3期36卷 240-256页

作者： Zaiwei Song Dan Jiang Lingling Yu Yixuan Chen Daobin Zhou Yue Li Depei Wu Lingli Zhang Liyan Miao Jun Ma Jun Zhu Hongmei Jing Rongsheng Zhao the Steering Committee,the Consensus Panel and the Evidence Synthesis Group Evidence-based Pharmacy Professional Committee of Chinese Pharmaceutical Association(CPA) hospital Pharmacy Professional Committee of Chinese Pharmaceutical Association(CPA) Division of Therapeutic Drug Monitoring of Chinese Pharmacological Society(CPS) Expert Committee on Lymphoma of Chinese Society of Clinical Oncology(CSCO) Expert Committee on Leukemia of Chinese Society of Clinical Oncology(CSCO) Society of Integrative Cardio-Oncology of china Anti-Cancer Association(CACA) Chinese Society of Hematology of Chinese Medical Association(CMA) hospital Pharmacy Professional Committee of Cross-Straits medicine Exchange Association(SMEA) department of Pharmacy Peking University Third HospitalBeijing 100191China Institute for Drug Evaluation Peking University Health Science CenterBeijing 100191China Therapeutic Drug Monitoring and Clinical Toxicology Center Peking UniversityBeijing 100191China department of Pharmacy Administration and Clinical Pharmacy School of Pharmaceutical SciencesPeking UniversityBeijing 100191China department of Hematology Peking Union Medical College HospitalChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100005China department of Cardiology the First Affiliated HospitalHarbin Medical UniversityHarbin 150001China department of Hematology the First Affiliated Hospital of Soochow UniversitySuzhou 215006China department of Pharmacy Evidence-based Pharmacy CenterWest China Second HospitalSichuan UniversityChengdu 610041China department of Pharmacy the First Affiliated Hospital of Soochow UniversitySuzhou 215006China department of Hematology and Oncology Harbin Institute of Hematology and OncologyHarbin 150010China Key laboratory of Carcinogenesis and Translational Research(Ministry of Education/Beijing) Department of LymphomaPeking University Cancer Hospital&InstituteBeijing 100142China department of Hematology Peking University Third HospitalBeijing 100191China 不详

Bruton’s tyrosine kinase inhibitors(BTKis)have revolutionized the treatment of B-cell ***,safety issues related to the use of BTKis may hinder treatment continuity and further affect clinical efficacy.A comprehensive and systematic expert consensus from a pharmacological perspective is lacking for safety issues associated with BTKi treatment.A multidisciplinary consensus working group was established,comprising 35 members from the fields of hematology,cardiovascular disease,cardio-oncology,clinical pharmacy,and evidencebased *** evidence-based expert consensus was formulated using an evidence-based approach and the Delphi *** Joanna Briggs Institute Critical Appraisal(JBI)tool and Grading of Recommendations Assessment,Development,and Evaluation(GRADE)approach were used to rate the quality of evidence and grade the strength of recommendations,*** consensus provides practical recommendations for BTKis medication based on nine aspects within three domains,including the management of common adverse drug events such as bleeding,cardiovascular events,and hematological toxicity,as well as the management of drug-drug interactions and guidance for special *** multidisciplinary expert consensus could contribute to promoting a multi-dimensional,comprehensive and standardized management of BTKis.

关键词： Consensus BTK inhibitors safety adverse drug events drug-drug interactions

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Culture of Human Tendon Cell Transfected by Human Telomerase Reverse Transcriptase Plasmid and their Biological CharacteristicsIn Vitro

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生物医学工程学杂志 2005年第S1期22卷 173-174页

作者： Hui-Qi XIE~1 Zhi-Ming YANG~(1△) Fan LIN~1 Yi QU~21(Division of Stem Cell and Tissue Engineering, State Key laboratory of Biotherapy, sichuan university, chengdu 610041, china) 2(department of Biochemistry and Molecular Biology, west china School of Preclinical and Forensic medicine, sichuan university, chengdu 610041, china) Division of Stem Cell and Tissue Engineering State Key Laboratory of Biotherapy Sichuan University Chengdu 610041 China department of Biochemistry and Molecular Biology West China School of Preclinical and Forensic Medicine Sichuan University Chengdu 610041 China

1 IntroductionThe proliferative and functional characteristics of tendon cell are the key issue in the research of tissue engineered tendon. The standard tendon cell line, which has normal functional characteristics, and can be subcultured continuously and permanently, will not only meet the demands of seeding cell in tissue engineered tendon,but also control the variable of tendon cell. In our previous study, it showed that the proliferative ability of human tendon cell cultured in vitro is depressed gradually after subcultured to the 13th passage, which can not meet the demands of tendon tissue engineering. It has been proved that replicative senescence of cells was closely related to the activity of telomerase. We constructed pGRN145 plasmid which contain total human telomerase reverse transcriptase (hTERT) cDNA. We transfected it into human tendon cells to investigate the feasibility of life span extension by reconstitution of the telomerase activity.

关键词： Cell Culture of Human Tendon Cell Transfected by Human Telomerase Reverse Transcriptase Plasmid and their Biological CharacteristicsIn Vitro

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Clinical value of ^(18)F-FDG PET/CT in assessing suspicious relapse after rectal cancer resection

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World Journal of Gastrointestinal Oncology 2009年第1期1卷 55-61页

作者： Long Sun,Wei-Min Pan,Zuo-Ming Luo,Ji-Hong Wei,Long Zhao,Hua Wu,Minnan PET Center and department of Nuclear medicine,the First hospital of Xiamen university,Xiamen 316003,Fujian Province,china Yong-Song Guan,State Key laboratory of Biotherapy,west china Medical School,sichuan university,Gaopeng Street,Keyuan Road 4,chengdu 610041,sichuan Province,china Long Sun Wei-Min Pan Zuo-Ming Luo Ji-Hong Wei Long Zhao Hua Wu Minnan PET Center and Department of Nuclear Medicine the First Hospital of Xiamen University Xiamen 316003 Fujian Province China.

AIM:To evaluate the value of 18F-fluorodeoxyglucose positron emission tomography/computed tomography(18F-FDG PET/CT) in the restaging of resected rectal ***:From January 2007 to Sep 2008,21 patients who had undergone curative surgery resection for rectal carcinoma with suspicious relapse in conventional imaging or clinical findings were retrospectively enrolled in our *** patients underwent 28 PET/CT scans(two patients had two scans,one patient had three and one had four scans).Locoregional recurrences and/or distant metastases were confirmed by histological analysis or clinical and imaging ***:Final diagnosis was confirmed by histopathological diagnosis in 12 patients(57.1) and by clinical and imaging follow-up in nine patients(42.9).Eight patients had extrapelvic metastases with no evidence of pelvic *** patients had both pelvic recurrence and extrapelvic metastases,and two patients had pelvic recurrence only.18F-FDG PET/CT was negative in two patients and positive in 19 patients.18F-FDG PET/CT was true positive in 17 patients and false positive in *** accuracy of 18F-FDG PET/CT was 90.5,negative predictive value was 100,and positive predictive value was *** patients with perirectal recurrence underwent 18F-FDG PET/CT image guided tissue core biopsy.18F-FDG PET/CT also guided surgical resection of pulmonary metastases in three patients and monitored the response to salvage chemotherapy and/or radiotherapy in four ***:18F-FDG PET/CT is useful for evaluating suspicious locoregional recurrence and distant metastases in the restaging of rectal cancer after curative resection.

关键词： 18F-fluorodeoxyglucose Positron emission tomography/computed tomography Rectal cancer Follow-up Restaging Locoregional recurrence Distant metastases

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Investigation on Azoospermia Factor (AZF) Microdeletion and Sex-determining Region Y (SRY) of the Y Chromosome in Male Infertility

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Journal of Reproduction and Contraception 2013年第2期24卷 88-94页

作者： Li-hua LU Fei-xue HU Song GE laboratory of Genetics Deptment of Laboratory Medicine Peking University Shenzhen Hospital

Objective To determine the incidence of azoospermia faetor （AZF） microdeletions of Y chromosome in male infertility and to investigate the mechanism of sex-determining region Y （SRY） in sex differentiation. Methods The mierodeletion of AZF was detected by multiplex polymerase chain reaction （PCR） using Y-chromosome specific sequence tagged sites （STSs）, and SRY was analyzed by PCR and sequencing. Results There were 100 cases with AZF microdeletion and the ratio of AZF microdeletion was 6.8% over all 1 474 cases. The ratios of AZF microdeletion of azoospermia group and severe oligozoospermia group were 9.0% and 7.1%, respectively, which was significantly different from oligozoospermia group （P〈 0. 05）. There were 67 cases with 5 STSs mierodeletion of sY152, sY239, sY243, sY254 and sY255. There were 20 cases with long fragment deletion more than 10 STSs, and the patterns of AZF microdeletion in other 13 cases were rare. In all 9 patients with disorders of sex differentiation, there were 6patients with SRY-absent and AZF-absent. There was no mutation of SRY gene by sequencing in other 3 patients with SRY-positive. Conclusion Deletions in AZF region of Y chromosome are specific with diagnoses with spermatogenesis disorder. Deletions of sY152, sY239, sY243, sY254 and sY255 occur the most frequently. SRY was an important candidate gene of testis-determining factor （TDF） gene.

关键词： sex-determining region Y (SRY) azoospermia factor (AZF) sex differentiation spermatogenesis

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Melatonin ameliorates experimental hepatic fibrosis induced by carbon tetrachloride in rats

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World Journal of Gastroenterology 2009年第12期15卷 1452-1458页

作者： Ru-Tao Hong,department of Geriatrics medicine,The First Affiliated hospital of Anhui Medical university,Hefei 230022,Anhui Province,china Ru-Tao Hong,Jian-Ming Xu,Qiao Mei,department of Gastroenterology,The First Affiliated hospital of Anhui Medical university,Hefei 230022,Anhui Province,china The Key laboratory of Digestive Diseases of Anhui Province,Hefei 230022,Anhui Province,china department of Geriatrics medicine The First Affiliated Hospital of Anhui Medical University Hefei 230022 Anhui Province China.

AIM:To investigate the protective effects of melatonin on carbon tetrachloride(CCl4)-induced hepatic fibrosis in experimental ***:All rats were randomly divided into normal control group,model control group treated with CCl4 for 12 wk,CCl4+NAC group treated with CCl4+NAC(100 mg/kg,i.p.)for 12 wk,CCl4+MEL-1 group treated with CCl4+melatonin(2.5 mg/kg)for 12 wk,CCl4+MEL-2 group treated with CCl4+ melatonin(5.0 mg/kg)for 12 wk,and CCl4+MEL-3 group treated with CCl4+melatonin(10 mg/kg).Rats in the treatment groups were injected subcutaneously with sterile CCl4(3 mL/kg,body weight)in a ratio of 2:3 with olive oil twice a *** in normal control group received hypodermic injection of olive oil at the same dose and frequency as those in treatment *** the end of experiment,rats in each group were anesthetized and *** and eosin(HE)staining and Van Gieson staining were used to examine changes in liver *** activities of alanine aminotransferase(ALT),aspartate aminotransferase(AST)and protein concentration weremeasured with routine laboratory methods using an ***(HYP)content in liver and malondialdehyde(MDA)and glutathione peroxidase(GPx)levels in liver homogenates were assayed by *** hyaluronic acid(HA),laminin(LN),and procollagenⅢN-terminal peptide(PⅢNP)were determined by ***:Pathologic grading showed that the fibrogenesis was much less severe in CCl4+MEL3 group than in model control group(u=2.172,P5),indicating that melatonin(10 mg/kg)can significantly ameliorate CCl4-induced hepatic fibrotic *** serum levels of ALT and AST were markedly lower in CCl4+MEL treatment groups(5,10 mg/kg)than in model control group(ALT:286.23 ±121.91 U/L vs 201.15±101.16 U/L and 178.67 ±103.14 U/L,P=0.028,P=0.007;AST:431.00 ±166.35 U/L vs 321.23±162.48 U/L and 292.42 ±126.23 U/L,P=0.043,P=0.013).Similarly,the serum laminin(LN)and hyaluronic acid(HA)levels and hydroxyproli

关键词： Melatonin Hepatic fibrosis Oxidativestress Hyaluronic acid Laminin Malondialdehyde Glutathione peroxidase

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Effectiveness of Testosterone Undecanoate Treatment in Men with Asthenospermia

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Journal of Reproduction and Contraception 2012年第2期23卷 119-126页

作者： Bo SONG Zhi-ming CAI Guangdong Key Lab Male Reproductive Medicine&GeneticsShenzhen HospitalPeking UniversityShenzhen 518036China

Objective To assess the effectiveness of testosterone undecanoate on sperm motility and pregnancy incidence in men with asthenospermia. Methods A clinical trial was performed. Fifty men with asthenospermia were included to receive placebo （control group, n=9） or T undecanoate 80 mg/d （study group, n=41）. Pregnancy incidence and sperm characteristics after 1, 2 and 3 months of medication and 3 months after the end of the trial were measured. Results Compared with the placebo, T undecanoate treatment produced a satisfactory improvement of seminal motility （F=55.904, P=0.000）. In study group, the incidence of pregnancy was 28.2% while the incidence of pregnancy in control group was 11.1%. In study group, 26patients took T undecanoate for more than 3 months. In the 3 months, semen volume showed no statistical difference （F=1.206, P=0.312） before and after treatment, sperm concentration （F=0.023, P=0.000） and motility a, b, a ＋b （P=0.000） showed statistical differences. Motility grade a showed significantly higher increment in 2 and 3 months after treatment than 1 month and there was no statistical difference between 2 and 3 months. So did grade b. Conclusion The results indicate that T undecanoate increases semjnal motility, leading to a higher incidence of pregnancy in couples with infertility related to asthenoaspermia.

关键词： testosterone undecanoate sperm motility asthenospermia

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