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
;
Protein Tyrosine Phosphatase, Non-Receptor Type 1
;
antagonists & inhibitors
;
Structure-Activity Relationship
;
Sulfathiazoles
;
chemistry
;
pharmacology
3.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
;
diagnosis
;
virology
;
DNA, Viral
;
isolation & purification
;
Female
;
Human papillomavirus 16
;
genetics
;
isolation & purification
;
Human papillomavirus 18
;
genetics
;
isolation & purification
;
Humans
;
Molecular Diagnostic Techniques
;
methods
;
Papillomaviridae
;
genetics
;
isolation & purification
;
Papillomavirus Infections
;
diagnosis
;
virology
;
RNA, Messenger
;
metabolism
;
United States
;
United States Food and Drug Administration
;
Uterine Cervical Neoplasms
;
diagnosis
;
virology
4.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
;
administration & dosage
;
adverse effects
;
Humans
;
Injections
;
Medicine, Chinese Traditional
;
methods
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.Colour stabilities of three types of orthodontic clear aligners exposed to staining agents
Liu CHEN-LU ; Sun WEN-TIAN ; Liao WEN ; Lu WEN-XIN ; Li QI-WEN ; Jeong YUNHO ; Liu JUN ; Zhao ZHI-HE
International Journal of Oral Science 2016;8(4):246-253
The aim of this study was to evaluate and compare the colour stabilities of three types of orthodontic clear aligners exposed to staining agents in vitro. Sixty clear orthodontic aligners produced by three manufacturers (Invisalign, Angelalign, and Smartee) were immersed in three staining solutions (coffee, black tea, and red wine) and one control solution (distilled water). After 12-h and 7-day immersions, the aligners were washed in an ultrasonic cleaner and measured with a colourimeter. The colour changes (ΔE*) were calculated on the basis of the Commission Internationale de I’Eclairage L*a*b*colour system (CIE L*a*b*), and the results were then converted into National Bureau of Standards (NBS) units. Fourier transformation infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM) were conducted to observe the molecular and morphologic alterations to the aligner surfaces, respectively. The three types of aligners exhibited slight colour changes after 12 h of staining, with the exception of the Invisalign aligners stained with coffee. The Invisalign aligners exhibited significantly higherΔE*values (ranging from 0.30 to 27.81) than those of the Angelalign and Smartee aligners (ΔE*values ranging from 0.33 to 1.89 and 0.32 to 1.61, respectively, Po0.05). FT-IR analysis confirmed that the polymer-based structure of aligners did not exhibit significant chemical differences before and after the immersions. The SEM results revealed different surface alterations to the three types of aligner materials after the 7-day staining. The three types of aesthetic orthodontic appliances exhibited colour stability after the 12-h immersion, with the exception of the Invisalign aligners stained by coffee. The Invisalign aligners were more prone than the Angelalign and Smartee aligners to pigmentation. Aligner materials may be improved by considering aesthetic colour stability properties.
9.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.
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