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Synthesis and anti-HIV activities of phorbol derivatives

Chinese Journal of Natural Medicines 2024年第2期22卷 146-160页

作者： HUANG Xiaolei TANG Chengrun HUANG Xusheng YANG Yun LI Qirun MA Mengdi ZHAO Lei YANG Liumeng CUI Yadong ZHANG Zhenqing ZHENG Yongtang ZHANG Jian College of Pharmaceutical Science Soochow UniversitySuzhou 215123China Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province Kunming Institute of ZoologyChinese Academy of SciencesKunming 650223China Kunming College of Life Science University of Chinese Academy of SciencesKunmingYunnan 650204China

In this study,37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated,building upon our previous synthesis of 51 phorbol derivatives.12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out,demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia *** derivatives exhibited a higher safety index compared with the positive control *** them,12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol,designated as compound 3c,exhibited the most potent anti-HIV-1 activity(EC_(50)2.9 nmol·L^(−1),CC50/EC_(50)11117.24)and significantly inhibited the formation of syncytium(EC_(50)7.0 nmol·L^(−1),CC50/EC_(50)4891.43).Moreover,compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase *** titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C(PKC).Therefore,compound 3c emerges as a potential candidate for developing new anti-HIV drugs.

关键词： Phorbol esters Anti-HIV-1 activity Syncytia formation 12-(Trans-4-fluorocinnamoyl)-13-decanoyl phorbol safety index HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator

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Mechanical performances of shield tunnel segments under asymmetric unloading induced by pit excavation

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Journal of Rock Mechanics and Geotechnical Engineering 2023年第6期15卷 1547-1564页

作者： Gang Wei Feifan Feng Chengbao Hu Jiaxuan Zhu Xiao Wang Department of Civil Engineering Hangzhou City UniversityHangzhou310015China Key Laboratory of Safe Construction and Intelligent Maintenance for Urban Shield Tunnels of Zhejiang Province Hangzhou310015China Zhejiang Engineering Research Center of Intelligent Urban Infrastructure Hangzhou310015China College of Civil Engineering and Architecture Zhejiang UniversityHangzhou310058China

To explore the stress and deformation responses,as well as the failure characteristics of the shield tunnel segment of Hangzhou Metro under the influences of pit excavation and other surrounding projects,a self-developed“shield tunnel segment hydraulic loading system”was used to carry out full-scale loading tests on the three-ring staggered assembled *** structural performances and failure process of the tunnel segment under step-by-step asymmetric unloading were studied.A safety index was proposed to describe the bearing capacity of the ***,a finite element model(FEM)was established to analyze the bearing capacity of segment using the test ***,the effect of reinforcement with a steel plate on the deformation and bearing capacity of the segment was *** results showed that under asymmetric unloading,the peak value and amplitude of the bending moment on the near unloading side converged with a greater value than those on the far *** concrete internal force exhibited a directional transformation at different load *** first appeared at the 180inner arc surface of the bottom standard block and then expanded to both sides,while the rate of crack propagation of the outer arc surface was relatively *** bearing capacity of the segments can be evaluated by the combination of the factors,*** residual bearing capacity coefficient,moment transfer coefficient,and characterization *** segments approaching failure can facilitate the increase in the residual bearing capacity coefficient by more than 50%.This can provide guidance for the service assessment of metro tunnel operations.

关键词： Shield tunnel segment Full-scale test Asymmetric unloading Stress and deformation safety index

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safety and Efficacy of Artisan Aphakia Iris-Claw Intraocular Lens in Tertiary Hospital in Indonesia

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Open Journal of Ophthalmology 2021年第1期11卷 25-35页

作者： Emmy Dwi Sugiarti Azalia Latuasan Andrew M. H. Knoch Budiman Budiman Cataract and Refractive Surgery Unit National Eye Centre Cicendo Eye Hospital Bandung Indonesia Ophtalmology Department Faculty of Medicine Universitas Padjadjaran Bandung Indonesia

Introduction: Iris-claw Intraocular Lens (IOL) is one of the alternatives to correct aphakia without sufficient capsular support. This technique is preferred because it has a simple procedure. Iris-claw IOL was originally designed to be fixated on the anterior chamber. The use of retropupillary fixation is increasing because the location is more physiologic and it shows less risk to corneal endothelial damage. Purpose: To describe safety and efficacy of iris-claw Artisan IOL in correcting aphakia without sufficient capsular support. Methods: This is a descriptive retrospective study of patients with aphakic iris-claw Artisan IOL implantation in National Eye Center Cicendo Eye Hospital, Indonesia from July 2017-July 2019. Patients were divided into prepupillary and retropupillary group. The Uncorrected Visual Acuity (UCVA), Best-Corrected Visual Acuity (BCVA), safety index (SI), Efficacy index (EI), and complications were recorded. The procedure is safe if SI value ≥ 1.0 and effective if EI value ≥ 1.0. Results: There were 54 eyes in the retropupilary group and 17 eyes in the prepupillary group. In the prepupillary group, there were 94.11% eyes with SI ≥ 1.0, the mean SI was 1.79 ± 1.02, 50% of eyes with EI ≥ 1.0, and the mean EI was 0.77 ± 0.20. In the retropupillary group, there were 96.29% eyes with SI ≥ 1.0, the mean SI was 2.49 ± 2.23, 74.07% of eyes with EI ≥ 1.0, and the mean EI was 1.75 ± 1.64. Postoperative UCVA and BCVA were improved significantly compared to preoperative visual acuity in both groups (p Conclusion: Prepupillary and retropupillary iris-claw IOL implantation are safe. Retropupillary fixation technique is more effective in improving visual acuity.

关键词： Iris-Claw Aphakia safety index Efficacy index

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Risk Assessment of Quality safety of Nonlocal Red Bayberry in Cixi City

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Plant Diseases and Pests 2014年第4期5卷 31-34页

作者： Wang Dongqun Hu Yinxia Fei Wei Ma Jinjin Su Tong Hu Shimeng Ma Yan Hua Xiaoxia Cixi Agricultural Supervising and Testing Center Cixi Agriculture Bureau

The nonlocal red bayberry sold in Cixi City were quantitatively analyzed for consecutive four years from 2010 to 2013, in order to understand their pesti- cide pollution. The results showed that the detectable rate of pesticide was 55.56%, and the pesticide detectable rate of samples was 59.09% in red bayberry. The exceeding standard rate of pesticides was 15.87%. In terms of safety index, the risk and safety state of all pesticides were within an acceptable range except cyhalothrin. In terms of risk coefficient, omethoate, triazophos and isocarbophes were at high-risk state, and the remaining 19 kinds of pesticides were at low-risk state.

关键词： Red bayberry Pesticide residue safety index Risk coefficient Cixi

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