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Design,Synthesis and Molecular Docking of a Novel Small-molecule Inhibitor of Caspase-3

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Chemical Research in Chinese Universities 2010年第2期26卷 256-258页

作者： ZHANG Jin-liang GUO Yang-hong GAO Chao-hui wang en-si Ren Zhong-yuan FANG Xue-xun wang Ji-dong College of Life Science School of Pharmaceutical Sciences College of Chemistry Jilin University Changchun 130021 P. R. China

4,5-Dihydro-3-methylbenzo[1,2-b]furan-4,5-dione（4） was identified as a novel and potent inhibitor of caspase-3 through structural modification of an existing drug, sodium tanshinone IIA sulfonate（STS）. Compound 4 showed high potency against caspase-3 in vitro（ICso=0. 13μmol/L）. Molecular docking study further provided an insight into the interaction of compound 4 with activated caspase-3. Hence, this small-molecule caspase-3 inhibitor could be a oromising theraoeutic candidate against diseases caused by abnormally up-regulated apptosis.

关键词： Caspase-3 Inhibitor Docking simulation

Development of re-crosslinkable dispersed particle gels for conformance improvement in extremely high-temperature reservoirs

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Petroleum Science 2022年第6期19卷 2922-2931页

作者： Dao-Yi Zhu Run-Tian Luo Yang Liu Jun-hui Qin Qi Zhao Hong-Jun Zhang Wan-Sheng wang Zi-Yuan wang Meng-en Zhu Yi-Peng wang Peng-Bo Li China University of Petroleum-Beijing at Karamay Karamay 834000XinjiangChina

Micro-scale and nano-scale dispersed gel particles(DPG)are capable of deep migration in oil reservoirs due to their deformability,viscoelasticity,and suitable particle ***,it has been widely studied and applied in reservoir conformance control in recent ***,for highly permeable channels,their plugging performance is still *** addition,conventional in situ cross-linked polymer gels(ISCPGs)have fast gelation time under extremely high-temperature conditions,which often causes problems such as difficulty in ***,a re-cross linkable dispersed particle gel(RDPG)system applied for conformance control in highly permeable channels of extremely high-temperature petroleum reservoirs was *** particle size distribution,gelation time,gel strength,injection performance,and perfo rmance strength in po rous media were investigated using a laser particle size meter,the Sydansk bottle test method,rheometer,and core displacement experiments,*** show that the RDPG suspension can be stable for more than 6 months at room temperature with storage modulus G’much lower than 10 *** can pass through the pore throat by elastic deformation effect and does not cause strong ***,it can undergo re-crosslinking reaction at 150℃to form a strong bulk *** gel strength G’of re-crosslinked RDPG can be as high as 69.3 Pa,which meets the strength requirement of conformance *** RDPG suspension has the properties of easy injection,and it also has strong plugging,and high-temperature resistance after re-crosslinked in the core,which can be a very promising material for conformance improvement in extremely high-temperature reservoirs.

关键词： Dispersed particle gel Re-crosslinking Conformance improvement High-temperature petroleum reservoir Injection performance

Equilibrium sediment transport in lower Yellow River during later sediment-retaining period of Xiaolangdi Reservoir

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Water Science and engineering 2015年第1期8卷 78-84页

作者： Shao-lei Guo Dong-po Sun en-hui Jiang Peng Li College of Water Conservancy North China University of Water Resources and Electric Power Yellow River Institute of Hydraulic Research Yellow River Henan Bureau Yellow River Conservancy Commission

The Xiaolangdi Reservoir has entered the later sediment-retaining period, and new sediment transport phenomena and channel re-estab- lishing behaviors are appearing. A physical model test was used to forecast the scouring and silting trends of the lower Yellow River. Based on water and sediment data from the lower Yellow River during the period from 1960 to 2012, and using a statistical method, this paper analyzed the sediment transport in sediment-laden flows with different discharges and sediment concentrations in the lower Yellow River. The results show that rational water-sediment regulation is necessary to avoid silting in the later sediment-retaining period. The combination of 3 000 m^3/s 〈 Q 〈 4 000 m^3/s and 20 kg/m^3 〈 S 〈 60 kg/m^3 （where Q is the discharge and S is the sediment concentration） at the Huayuankou section is considered an optimal combination for equilibrium sediment transport in the lower Yellow River over a long period of time.

关键词： Lower Yellow River Xiaolangdi Reservoir Water-sediment regulation Equilibrium sediment transport Later sediment-retaining period

Fibrin sealant for closure of mucosal penetration at the cardia during peroral endoscopic myotomy: A retrospective study at a single center

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World Journal of Gastroenterology 2017年第9期23卷 1637-1644页

作者： Wen-Gang Zhang en-Qiang Linghu hui-Kai Li Departmen of Gastroenterology Chinese PLA General HospitalBeijing 100853China

AIM To assess the efficacy and safety of fibrin sealant for closure of mucosal penetration at the cardia during peroral endoscopic myotomy(POEM).METHODS Twenty-four patients who underwent POEM and experienced mucosal injury of the cardia during the procedure were retrospectively identified. Of the 24 patients, 21 had mucosal penetration and 3 had only slight mucosal damage without penetration. The 21 patients with mucosal penetration received fibrin sealant for closure at the site of penetration. Penetration-related characteristics, treatment, and recovery were reviewed for all 21 patients to assess the efficacy and safety of fibrin sealant for closure of mucosal penetration at the cardia. Clinical data, including general characteristics, procedure-related parameters, Eckardt scores, lower esophageal sphincter pressures (LESP), and esophagogastroduodenoscopy(EGD) results, were analyzed to determine their influence on treatment success after mucosal penetration during *** All 21 patients had a solitary mucosal penetration in the cardia (12 in esophageal region of the cardia, 9 in the stomach region of the cardia, and 1 in both the esophageal and stomach regions). Twelve had ahole-like penetration and 9 had a linear penetration. For those with a hole-like penetration, the mean size was 0.14 cm2 (0.02-0.32 cm2). For those with a linear penetration, the median size was 0.37 cm (0.10-1.00 cm). Closure of the mucosal penetration using fibrin sealant was performed successfully in all 21 patients(two patients required 5 m L fibrin sealant, and the remaining 19 patients required 2.5 mL). Two patients had a nasogastric tube placed for five days after POEM; the remaining 19 patients were kept fasting for 3 d. All 21 patients were discharged after a median of 5 d(range: 5-7 d) postoperatively. During a median 42 mo (range: 9-62 mo) follow-up, all 21 patients with a mucosal penetration successfully healed without the occurrence of infection, ulcer, or esophagitis. Furth

关键词： Fibrin sealant Mucosal penetration Peroral endoscopic myotomy Efficacy Safety

endoscopic submucosal tunnel dissection for largesuperficial esophageal squamous cell neoplasms

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World Journal of Gastroenterology 2016年第1期22卷 435-445页

作者： Ya-Qi Zhai hui-Kai Li en-Qiang Linghu Department of Gastroenterology and Hepatology Chinese People’s Liberation Army General HospitalBeijing 100853China

endoscopic submucosal dissection(ESD)is a wellestablished treatment for superficial esophageal squamous cell neoplasms(SESCNs)with no risk of lymphatic ***,for large SESCNs,especially when exceeding two-thirds of the esophageal circumference,conventional ESD is time-consuming and has an increased risk of adverse *** on the submucosal tunnel conception,endoscopic submucosal tunnel dissection(ESTD)was first introduced by us to remove large SESCNs,with excellent *** from different centers also reported favorable *** with conventional ESD,ESTD has a more rapid dissection speed and R0 resection *** in China,ESTD for large SESCNs is an important part of the digestive endoscopic tunnel technique,as is peroral endoscopic myotomy for achalasia and submucosal tunnel endoscopic resection for submucosal tumors of the muscularis ***,not all patients with SESCNs are candidates for ESTD,and postoperative esophageal strictures should also be taken into consideration,especially for lesions with a circumference greater than *** this article,we describe our experience,review the literature of ESTD,and provide detailed information on indications,standard procedures,outcomes,and complications of ESTD.

关键词： endoscopic submucosal tunnel dissection Esophageal squamous cell neoplasms Digestiveendoscopic tunnel technique endoscopic submucosaldissection

CRISPR/Cas9-mediated Tyrosine hydroxylase knockout resulting in larval lethality in Agrotis ipsilon

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Insect Science 2018年第6期25卷 1017-1024页

作者： Yang Yang Yao-hui wang Xi-en Chen Di Tian Xia Xu Kai Li Yong-Ping Huang Lin He School of Life Science East China Normal UniversityShanghaiChina Key Laboratory of Insect Developmental and Evolutionary Biology Institute of Plant Physiology and EcologyShanghai Institutes for Biological SciencesChinese Academy of SciencesShanghaiChina Hubei Key Laboratory of Insect Resource Application and Sustainable Pest Control College of Plant Science &TechnologyHuazhong Agricultural UniversityWuhanChina

Tyrosine hydroxylase (TH)is involved in insect melanin and the catecholamine biosynthesis *** as an enzyme catalyzing the conversion of tyrosine to 3,4- dihydroxyphenylalanine is the first step reaction in the *** TH has been proven to affect the pigmentation of the epidermis and development in many insects,there is no report about physiological function of the THgene inAgrotis *** we cloned the TH gene from ***-quantitative real-time polymerase chain reaction (PCR) analysis showed that AiTH was expressed at all development ***,its high expression levels in the head and epidermis suggest that it is mainly related to pigment deposition and insect ***,we used the clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein 9system to target the AiTH gene:deletion events were detected at the target *** with the control group,a few mutants with the phenomenon of narrowing in the egg shell and embryos can develop but cannot hatch;the other hatched embryos were seriously dehydrated after hatching and died within the first *** real-time PCR analysis revealed that THwas down-regulated ***,our work demonstrated thatAiTHplays an important role in growth and development of newly hatched larvae;meanwhile,it would be a promising target to explore a control strategy for ***.

关键词： Agrotis ipsilon CRISPR/Cas9system larvae lethal Tyrosine hydroxylase

One-year outcomes of intravitreal conbercept combined rescue therapy for polypoidal choroidal vasculopathy in a Chinese population: a real-life clinical data

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International Journal of Ophthalmology(english edition) 2019年第1期12卷 51-57页

作者： hui-Jun Qi en-Zhong Jin Ming-Wei Zhao Department of Ophthalmology Ophthalmology & Optometry CenterPeking University People’s HospitalBeijing Key Laboratory of Diagnosis and Therapy of Retinal and Choroid Diseases

AIM: To evaluate the real-life clinical outcomes of intravitreal injection of conbercept combined rescue therapy for polypoidal choroidal vasculopathy(PCV). METHODS: This was an open label, single center, and interventional study. All enrolled patients were treated initially with three consecutive monthly intravitreal conbercept injections(0.5 mg). Additional conbercept injections were administered upon substantial polyp regression with improved visual acuity(VA). Eyes with partial or no polyp regression and poor VA were rescue treated with photodynamic therapy(PDT) for subfoveal polyps or thermal laser photocoagulation for extrafoveal polyps. Best-corrected visual acuity(BCVA), central foveal thickness(CFT) and polyp regression were observed as primary outcomes. Side effects were also collected during the follow-up period. RESULTS: A total of 56 eyes(56 patients) with PCV were included. BCVA increased significantly from the baseline of 43.52±24.21 letters to 55.88±21.94 letters(Pents showed polyp regression. Twenty-three eyes achieved complete polyp regression after the three initial injections, which increased to 44 eyes at 12 mo. Seventeen eyes underwent rescue therapy, among which 2 eyes treated with PDT and 15 eyes treated with laser photocoagulation. A mean of 4.30±1.43 injections were given per eye. No intraocular inflammation, retinal or vitreous hemorrhage, or systemic complication occurred. CONCLUSION: Conbercept is an effective and safe option for the treatment of PCV in Chinese population. The treatment regimen of three initial conbercept injections followed by additional injections or rescue therapies is efficacious for treating PCV.

关键词： conbercept anti-vascular endothelial growth factor polypoidal choroidal vasculopathy intravitreal injection laser photocoagulation photodynamic therapy

The microRNA miR-184 regulates the CYP303A1 transcript level to control molting of Locusta migratoria

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Insect Science 2021年第4期28卷 941-951页

作者： Yan-Li wang Li-Xian Wu hui-Yong Li Xue-Qin Wen en-Bo Ma Kun-Yan Zhu Jian-Zhen Zhang Research Institute of Applied Biology Shanxi UniversityTaiyuanShanxiChina College of Life Science Shanxi UniversityTaiyuanShanxiChina Department of entomology Kansas State UniversityManhattanKSUSA

Cytochrome P450 monooxygenases(CYPs)play essential physiological functions in ***303A1 is highly conserved in insect species studied to date,and shows an indispensable role for adult eclosion in both Locusta migratoria and Drosophila ***,how CYP303A1 is regulated to control insect developmental processes remains *** this study,we discovered functional binding sites for miR-184 in the coding sequence of *** luciferase reporter assay showed that miR-184 could target LmCYP303A1 and regulate its expression in ***,overexpression of miR-184 through microinjection of agomir to locusts reduced the transcripts of LmCYP303A1 and led to abnormal molting,which is similar to the phenotype of silencing LmCYP303A1 by direct injection of dsLmCYP303A1 to ***,down-regulation of miR-184 by injection of antagomir increased the LmCYP303A1 transcript and caused molting *** findings suggested that miR-184 could target LmCYP303A1 to regulate the molting process in ***,which might be considered as a novel target for pest control.

关键词： CYP303A1 gene regulation insect molting Locusta migratoria miR-184

The effect of chelating agent on hydrodesulfurization reaction of ordered mesoporous alumina supported Ni Mo catalysts

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Petroleum Science 2022年第1期19卷 321-328页

作者： Di Hu hui-Ping Li Jin-Lin Mei Cheng-Kun Xiao en-Hua wang Xi-Yue Chen Wen-Xin Zhang Ai-Jun Duan State Key Laboratory of Heavy Oil Processing China University of Petroleum-BeijingBeijing102249China

In this paper,ordered mesoporous alumina(OMA)support with the high surface area(328 m^(2)g^(-1))and the large pore volume 0.74(cm^(3)·g^(-1))was synthesized by homogeneous precipitation *** the influence of EDTA on the physical and chemical properties of the modified catalysts was also *** characteristic results showed that the addition of EDTA could adjust the metal-support interaction and improved the acidity of the corresponding *** with the catalytic performance results,the EDTA-modified Ni Mo E(1.0)/OMA catalyst displays the highest DBT hydrodesulfurization conversion(97.7%).

关键词： Chelating agent Hydrodesulfurization Ordered mesoporous alumina