2.SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors.
Wen-Wen YIN ; Zheng CHEN ; Yan-Bo TANG ; Fei YE ; Jin-Ying TIAN ; Zhi-Yan XIAO
Acta Pharmaceutica Sinica 2014;49(5):632-638
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
Humans
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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antagonists & inhibitors
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Structure-Activity Relationship
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Sulfathiazoles
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chemistry
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pharmacology
3.Research and practice about risk control of shenfu injection.
Zhi-Fei WANG ; Da-Li TIAN ; Wen ZHANG ; Yan-Ming XIE
China Journal of Chinese Materia Medica 2014;39(18):3641-3644
Shenfu injection is developed by improving dosage form of ancient prescription "Shenfu Tang" and is mainly derived from extracts of both traditional Chinese medicine red ginseng and prepared lateral root of monkshood with polysorbate 80 as auxiliary material. Shenfu injection may be administered through intramuscular injection, intravenous drip or intravenous injection. It produces good effects in restoring Yang and rescuing patients from collapse, tonifying Qi and preventing exhaustion. It is mainly used to treat not only syncope and prostration resulting from sudden Yang collapse (infectious, hemorrhagic and water depletion shock etc), but also pavor, palpitation, dyspnea with cough, stomachache, diarrhea and arthralgia etc caused by deficiency of Yang (deficiency of vital energy). Research group has audited the monitored hospitals and has carried out postmarketing study of Shenfu solution from many aspects including literature review, spontaneous reporting system (SRS) and hospital information system (HIS) data analysis etc. A summary is shown below.
Drugs, Chinese Herbal
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administration & dosage
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adverse effects
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Humans
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Injections
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Medicine, Chinese Traditional
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methods
4.Methods of HPV detection in exfoliated cells and tissue specimens approved by the United States Food and Drug Administration.
Cheng-quan ZHAO ; Huai-tao YANG ; Zhi-dan TIAN ; Wen-bin HUANG
Chinese Journal of Pathology 2012;41(12):855-857
Cervical Intraepithelial Neoplasia
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diagnosis
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virology
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DNA, Viral
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isolation & purification
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Female
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Human papillomavirus 16
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genetics
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isolation & purification
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Human papillomavirus 18
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genetics
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isolation & purification
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Humans
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Molecular Diagnostic Techniques
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methods
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Papillomaviridae
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genetics
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isolation & purification
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Papillomavirus Infections
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diagnosis
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virology
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RNA, Messenger
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metabolism
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United States
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United States Food and Drug Administration
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Uterine Cervical Neoplasms
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diagnosis
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virology
5.Dynamic infusion cavernosometry and cavernosography for the diagnosis and classification of venous erectile dysfunction.
Tao SONG ; Yun CHEN ; You-feng HAN ; Wen YU ; Zhi-peng XU ; Yu-tian DAI
National Journal of Andrology 2015;21(6):504-509
OBJECTIVETo explore the procedures of dynamic infusion cavernosometry and cavernosography (DICC) and their application in the diagnosis and classification of venous erectile dysfunction (VED).
METHODSThis study included 103 ED patients, aged 20 to 43 years, highly suspected of VED, with disease courses of 4 months to 6 years. DICC was performed and analyses were made on the results, especially the parameters of flow-to-maintain (FTM) and pressure decay (PD) in the corpus cavernosum.
RESULTSBased on the parameters of FTM and PD, 21 of the patients were normal, 5 were suspected of VED, 39 had mild VED, 25 had moderate VED, and 13 had severe VED. Penile subcutaneous hematoma was found in 4 of the patients, all recovered after 3 to 5 days, with no other complications.
CONCLUSIONDICC is a reliable, safe and minimally invasive method for the diagnosis and classification of VED.
Diagnostic Techniques, Urological ; adverse effects ; Hematoma ; etiology ; Humans ; Impotence, Vasculogenic ; classification ; diagnosis ; Male ; Penile Diseases ; etiology ; Penis ; blood supply ; diagnostic imaging ; Radiography ; Veins
8.Effects of hypertonic saline against focal cerebral ischemia-reperfusion injury in rats and the mechanism
Rong-Zhi HE ; Huan-Sen HUANG ; Wen-Zhi TIAN ; Ye-Tian CHANG
Chinese Journal of Neuromedicine 2009;8(6):560-562,566
Objective To investigate the effect of hypertonic saline on cerebral water content, tumor necrosis factor-α (TNF-α) level and neuronal apoptosis following focal cerebral ischemia-reperfusion (IR) injury in rats and explore the mechanisms involved. Methods Ninety-six rats were randomized equally into 4 groups, namely the shame-operated group, untreated IR injury group, and 4.2% and 7.5% hypertonic saline groups (HS-A and HS-B groups, respectively). In the latter 3 groups, cerebral ischcmia was induced by middle cerebral artery occlusion for 2 h followed by administration of the corresponding treatments. Serum sodium concentration was measured at 5 min before and at 30, 60 and 90 min after the reperfilsion. At 22 h of rcperfusion, the rats were sacrificed after neurological deficit evaluation, and brain edema was assessed by measuring the wet-to-dry weight ratio of the brain tissue. TNF-α expression in the ischemic brain tissue was measured by enzyme-linked immunosorbent assay (ELISA), and the neuronal apoptosis was analyzed using TUNEL assay. Results In the saline-treated rats, serum sodium level increased significantly after saline administration, lasting for 60 min before recovering the normal levels in HS-A group and for over 90 min in HS-B group. Compared with that in the sham-operated group, the brain water content in rats of the IR group increased in both of the hemispheres, but more obviously in the ischemic hemisphere. In the two saline-treated groups, the water content decreased significantly in the bilateral hemispheres, which was especially obvious in the ischemic hemisphere;administration of 7.5% saline resulted in greater water content reduction in the ischemic hemisphere than 4.2% saline. Compared with the IR group, the two saline-treated groups showed significant reduction in TNF-α levels and apoptotic cells in the brain along with decreased neurological deficits. Conclusion Hypertonic saline can ameliorate cerebral focal IR injury by decreasing the cerebral water content, TNF-α level and neuronal apoptosis following the injury.
9.Effect of gufuhuotang on hemorheology and lipid metabolism of hormonal necrosis of femoral head.
Wei-ming TIAN ; Wen-zhi WANG ; Xin-guo WANG
China Journal of Chinese Materia Medica 2002;27(10):769-771
OBJECTIVETo probe the of Gufuhuotang effect on hemorheology and lipid metabolism of hormonal necrosis of femoral head.
METHOD32 male rabbits of New Zealand were divided at random into pathological pattern group, normal control group, low-dosage of Gufuhuotang group and high-dosage group; models of osteocyte necrosis of head of femur were made with intragluteal injection of hydroprednisone acetate; the rabbits were observed weekly and killed 6 weeks later and HE pathological section was made to observe hemorheology index and blood-liquid content, and then analysis and comparison were made.
RESULTGufuhuotang could obviously decrease total blood low-shear viscosity, plasma viscosity, hemacocrit, serum cholesterol and triglyceride contents; under light microscope empty bone lacunas of femoral head were less, fat cells of medullary cavity were less and relatively small, and bone trabecula was sparse with no break.
CONCLUSIONGufuhuotang has a distinct preventive and curative effect on rabbits' hormonal necrosis of femoral head.
Animals ; Drug Combinations ; Drugs, Chinese Herbal ; isolation & purification ; therapeutic use ; Femur Head Necrosis ; blood ; chemically induced ; prevention & control ; Hemorheology ; drug effects ; Lipids ; blood ; Male ; Plants, Medicinal ; chemistry ; Prednisone ; Rabbits ; Random Allocation
10.Study on intersection and regulation mechanism of "efficacy-toxicity network" of aconite in combination environment of Sini decoction.
Zhi-yong LI ; Hong-juan BAO ; Shuo-feng ZHANG ; Tian-yuan YE ; Ce YANG ; Yan-wen LI
China Journal of Chinese Materia Medica 2015;40(4):733-738
OBJECTIVETo explore the intersection and regulation mechanism of "efficacy-toxicity network" of Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma and Aconiti Lateralis Radix Praeparata's action gene in the combination environment of Sini decoction with the network pharmacological method.
METHODThe gene interaction network of Aconiti Lateralis Radix Praeparata, Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma were mined and established with Cytoscape software and Agilent literature search plug-in. The "efficiency-toxicity network" intersection of Aconiti Lateralis Radix Praeparata was formed according to its effects in anti-heart failure, neurotoxicity and cardiotoxicity. The target genes were clustered with Clusterviz plug-in. And the possible pathways of the "efficacy-tox- icity network" intersection of Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma and Aconiti Lateralis Radix Praeparata were forecasted in DAVID database.
RESULTThere were five genes related to neurotoxicity, cardiotoxicity and anti-heart failure function of Aconiti Lateralis Radix Praeparata, namely AKT1, BAX, HCC, IL6 and IL8, which formed 47 nodes genes in the "efficiency-toxicity network" intersection of Aconiti Lateralis Radix Praeparata. There were 29 and 27 coincident genes in the "efficiency-toxicity network" of Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma and Aconiti Lateralis Radix Praeparata. There were 23 and 17 possible regulatory pathways.
CONCLUSIONIn the combination environment of Sini decoction, Glycyrrhizae Radix et Rhizoma and Zingiberis Rhizoma may regulate the efficiency-toxicity network of Aconiti Lateralis Radix Praeparata by influencing immune-inflammatory signaling pathway, apoptosis-autophagy signaling pathway, nerve cell and myocardial ischemia and hypoxia protection signaling pathways.
Aconitum ; chemistry ; toxicity ; Drugs, Chinese Herbal ; chemistry ; toxicity ; Gene Regulatory Networks ; drug effects ; Humans ; Rhizome ; chemistry ; toxicity