2.Recent studies on the natural products with xanthine oxidase inhibitory effect
Nan JIANG ; Xiao-lin ZHANG ; Jin-ying TIAN ; Fei YE
Acta Pharmaceutica Sinica 2021;56(5):1229-1237
Xanthine oxidase (XOD), catalyzing purine metabolism, is the key enzyme in uric acid (UA) biosynthesis, and becomes an important target for hyperuricemia treatment. The inhibition on XOD plays an important role in the treatment of hyperuricemia-related diseases, such as gout, as well as oxidative stress-induced tissue injury. Here, studies on the natural products with XOD inhibition are reviewed.
3.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
4.Synthesis of diethylenetriamine polydentate ligands and their DNA-cleaving activity.
Xiao-Fei ZHU ; Yan-Hong LIU ; Yong YE
Acta Pharmaceutica Sinica 2012;47(3):380-384
A series of multinuclear diethylenetriamine ligands were synthesized and used as artificial nuclease enzyme model. Target compounds were characterized by 1H NMR, 13C NMR, IR and ESI-MS. Preliminary studies on the cleavage of pUC19 DNA in the presence of metal complexes have also been performed and the results revealed that these complexes could act as powerful catalysts for the cleavage of pUC19 DNA after 48 h under physiological conditions. The hydrolytic cleavage mechanism of DNA plasmid by title compound was confirmed by T4 DNA ligase experiment.
DNA
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metabolism
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DNA Cleavage
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Ligands
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Magnetic Resonance Spectroscopy
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Polyamines
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chemical synthesis
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chemistry
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Spectrometry, Mass, Electrospray Ionization
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Spectrophotometry, Infrared
5.Polypropylene mesh for testicular prothesis implantation: A report of 57 cases.
Jie AN ; Ye LIU ; Zong-min ZHANG ; Chun-xiao YU ; Yong-qiang XIA ; Peng-fei WANG
National Journal of Andrology 2015;21(9):816-818
OBJECTIVETo search for an optimum method for testicular prothesis implantation in the treatment of testis loss.
METHODSWe retrospectively analyzed the surgical methods and outcomes of 53 cases of terminal prostate cancer and 4 cases of unilateral testicular torsion treated by implantation of testicular prothesis with the polypropylene mesh.
RESULTSThe 57 male patients all received testicular prothesis with the polypropylene mesh. All the patients were satisfied with the appearance and size of the scrotum after surgery. No scrotal hematoma, prosthesis infection, or autoimmune disease occurred postoperatively.
CONCLUSIONTestis loss is not a rare condition clinically, for the treatment of which surgical implantation of testicular prothesis with the polypropylene mesh can achieve both a fine tissue compatibility and a desirable scrotal appearance.
Humans ; Male ; Polypropylenes ; Prostatic Neoplasms ; surgery ; Prostheses and Implants ; Retrospective Studies ; Scrotum ; Spermatic Cord Torsion ; surgery ; Surgical Mesh ; Testis
6.Therapeutic observation of Gao's nape acupuncture plus swallowing training for pharyngeal deglutition disorder after stroke
Xiao-Ping LIU ; Fei-Yu CHEN ; Jia-Mei CHU ; Ye-Hua BAO
Journal of Acupuncture and Tuina Science 2019;17(1):37-43
Objective:To observe the clinical efficacy of Gao's nape acupuncture plus swallowing training in treating pharyngeal deglutition disorder after stroke.Methods:One hundred patients with post-stroke pharyngeal deglutition disorder were randomized into a treatment group and a control group,with 50 cases in each group.The two groups both received routine neurological intervention.In addition,the treatment group was given Gao's nape acupuncture plus swallowing training,while the control group was intervened by swallowing training alone.After eight-week treatment,the two groups were observed in terms of the changes in repetitive saliva swallowing test (RSST),modified water swallowing test (MWST),standardized swallowing assessment (SSA) and swallowing-related quality of life (SWAL-QOL).The clinical efficacies of the two groups were also compared.Results:After treatment,the RSST grading,and scores of MWST,SSA and SWAL-QOL changed significantly in both groups (P<0.05 or P<0.01).The RSST grading,and scores of MWST,SSA and SWAL-QOL in the treatment group were significantly different from those in the control group after treatment (P<0.05 or P<0.01).The total effective rate and markedly effective rate were respectively 100.0% and 72.3% in the treatment group,versus 97.9% and 34.0% in the control group.There was a significant difference in the markedly effective rate between the two groups (P<0.01).The difference in the clinical efficacy between the two groups was statistically significant (P<0.01).Conclusion:Gao's nape acupuncture plus swallowing training is an effective approach for post-stroke pharyngeal deglutition disorder.Its therapeutic efficacy is more significant than that of swallowing training alone.
7.Expression of Pentraxin 3 in Children with Henoch-Sch?enlein Purpura
Fengying WANG ; Lusheng HUANG ; Kang XU ; Linhua YE ; Yun HUANG ; Fei XIAO
Journal of China Medical University 2017;46(2):156-159
Objective Henoch-Sch?nlein purpura(HSP)is a common multisystemic vasculitis in children ,but the exact pathogenesis remains unknown. Pentraxin 3(PTX3),a new kind of inflammatory cytokines,has a strong inflammatory effect,and is involved in occurrence and develop-ment of a variety of autoimmune diseases. The objective of this study is to evaluate the expression of PTX3,interleukin-8(IL-8),tumor necrosis fac-tor-α(TNF-α)and high sensitivity C-reactive protein(hs-CRP)in children with HSP,and explore the clinical significance of PTX3 in HSP devel-opment. Methods Thirty-six children(HSP group)and 17 healthy children(control group)were enrolled in the study. Serum levels of PTX3,IL-8 and TNF-α were detected by enzyme-linked immunosorbent assay. Serum hs-CRP levels were measured by automatic biochemical analyzer. Re-sults The serum levels of PTX3,IL-8,TNF-α,and hs-CRP were up-regulated in HSP group compared with the control group(P<0.05). The levels of PTX3,IL-8,TNF-α,and hs-CRP in patients with joint symptoms,or/and gastrointestinal symptoms,or/and kidney injury were significant-ly higher than those patients without joint symptoms,or/and gastrointestinal symptoms,or/and kidney injury(P<0.05). The expression of PTX3 was positively correlated with the expression of IL-8 and TNF-α(r=0.514,0.833,all P<0.05),but there was no correlation between PTX3 and hs-CRP(r=0.292,P>0.05). The expression of PTX3,IL-8,TNF-α and hs-CRP in HSP patients had no gender difference(all P>0.05). Con-clusion The high expression of PTX3 is related to the degree of inflammation in children with HSP. The up-regulated expression of PTX3 may play an important role in pathogenesis of HSP in children.
8.The correlation between the OATP1B1 521T > C genetic polymorphism and essential hypertension
Lili YE ; Jian QIU ; Shujin ZHAO ; Changjiang HONG ; Fei XIAO ; Yuhai ZOU
Chinese Journal of Primary Medicine and Pharmacy 2012;19(5):646-648
Objective To study the relationship between the OATP1B1 521T > C genetic polymorphism and essential hypertension.Methods 164 essential hypertension subjects and 159 normotensive subjects were detected by the TaqMan-MGB probe real-time fluorescence quantitative PCR,and the results were compared with those of DNA sequencing.Results The frequencies of T/C genotype and C allele of OATP1B1 521T > C gene of the essential hypertension subjects were obviously lower than those of the normotensive subjects(T/C genotype:0.16 vs 0.25,P <0.05 ;C allele:0.10 vs 0.17,P <0.05),The difference was significant.Binary logistic stepwise regression analysis was used for evaluatine the risk factors of essential hypertension,there was significant relationship between OATP1 B1 52IT > C gene polymorphism and essential hypertension.Conclusion The SLCO1 B1 521T > C variant was common in Chinese essential hypertension population,but the difference of frequency of SLCO1B1 52IT > Cmuton between the essential hypertension patients and the normotensive controls was of obviously statistical significance,which indicates that the SLCO1B1521T > C variant maybe associate with essential hypertension.
9.Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors.
Xin DU ; Shuen ZHANG ; Junzheng LIU ; Feilin NIE ; Fei YE ; Jinying TIAN ; Zhiyan XIAO
Acta Pharmaceutica Sinica 2012;47(3):367-73
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.
10.SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors.
Wenwen YIN ; Zheng CHEN ; Yanbo TANG ; Fei YE ; Jinying TIAN ; Zhiyan XIAO
Acta Pharmaceutica Sinica 2014;49(5):632-8
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.