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Seco-cyclic phorbol derivatives and their anti-HIV-1 activities

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Chinese Journal of Natural Medicines 2024年第4期22卷 365-374页

作者： HUANG Xiaolei HUANG Xusheng LI Qirun ma mengdi CUI Yadong YANG Liumeng WANG Haibo LUO Ronghua CHEN Jinglei YANG Jingxuan LIN Jinrong LI Duxin 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 SciencesKunming 650204China College of Traditional Chinese Medicine Yunnan University of Chinese MedicineKunming 650500China

Phorbol esters are recognized for their dual role as anti-HIV-1 agents and as activators of protein kinase C(PKC).The efficacy of phorbol esters in binding with PKC is attributed to the presence of oxygen groups at positions C20,C3/C4,and C9 of ***,the lipids located at positions C12/C13 are essential for both the anti-HIV-1 activity and the formation of the PKC-ligand *** influence of the cyclopropane ring at positions C13 and C14 in phorbol derivatives on their anti-HIV-1 activity requires further *** research entailed the hydrolysis of phorbol,producing seco-cyclic phorbol *** anti-HIV-1 efficacy of these derivatives was assessed,and the affinity constant(Kd)for PKC-δprotein of selected seco-cyclic phorbol derivatives was determined through isothermal titration *** findings suggest that the chemical modification of cyclopropanols could affect both the anti-HIV-1 activity and the PKC binding ***,compound S11,with an EC_(50) of 0.27μmol·L^(−1) and a CC_(50) of 153.92μmol·L^(−1),demonstrated a potent inhibitory effect on the intermediate products of HIV-1 reverse transcription(ssDNA and 2LTR),likely acting at the viral entry stage,yet showed no affinity for the PKC-δ*** results position compound S11 as a potential candidate for further preclinical investigation and for studies aimed at elucidating the pharmacological mechanism underlying its anti-HIV-1 activity.

关键词： seco-Cyclic phorbol derivatives Hydrolysis reaction Cyclopropane ring Esterification Anti-HIV-1 agent

Synthesis and anti-HIV activities of phorbol derivatives

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Chinese Journal of Natural Medicines 2024年第02期 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 University 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 Zoology Chinese Academy of Sciences Kunming College of Life Science University of Chinese Academy of Sciences

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 formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-（trans-4-fluorocinnamoyl）-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity(EC502.9 nmol·L-1, CC50/EC5011 117.24) and significantly inhibited the formation of syncytium(EC507.0 nmol·L-1, CC50/EC504891.43). Moreover, compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor. Isothermal 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.

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Seco-cyclic phorbol derivatives and their anti-HIV-1 activities

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Chinese Journal of Natural Medicines 2024年第04期 365-374页

作者： HUANG Xiaolei HUANG Xusheng LI Qirun ma mengdi CUI Yadong YANG Liumeng WANG Haibo LUO Ronghua CHEN Jinglei YANG Jingxuan LIN Jinrong LI Duxin ZHENG Yongtang ZHANG Jian College of Pharmaceutical Science Soochow University 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 Zoology Chinese Academy of Sciences Kunming College of Life Science University of Chinese Academy of Sciences College of Traditional Chinese Medicine Yunnan University of Chinese Medicine

Phorbol esters are recognized for their dual role as anti-HIV-1 agents and as activators of protein kinase C （PKC）.The efficacy of phorbol esters in binding with PKC is attributed to the presence of oxygen groups at positions C20,C3/C4,and C9 of ***,the lipids located at positions C12/C13 are essential for both the anti-HIV-1 activity and the formation of the PKC-ligand *** influence of the cyclopropane ring at positions C13 and C14 in phorbol derivatives on their anti-HIV-1 activity requires further *** research entailed the hydrolysis of phorbol,producing seco-cyclic phorbol *** anti-HIV-1efficacy of these derivatives was assessed,and the affinity constant （Kd） for PKC-δ protein of selected seco-cyclic phorbol derivatives was determined through isothermal titration *** findings suggest that the chemical modification of cyclopropanols could affect both the anti-HIV-1 activity and the PKC binding ***,compound S11,with an EC50 of 0.27μmol·L-1and a CC50of 153.92μmol·L-1,demonstrated a potent inhibitory effect on the intermediate products of HIV-1 reverse transcription （ss DNA and 2LTR）,likely acting at the viral entry stage,yet showed no affinity for the PKC-δ *** results position compound S11 as a potential candidate for further preclinical investigation and for studies aimed at elucidating the pharmacological mechanism underlying its anti-HIV-1 activity.

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DELLA proteins interact with FLC to repress flowering transition

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Journal of Integrative Plant Biology 2016年第7期58卷 642-655页

作者： Mingzhe Li Fengying An Wenyang Li mengdi ma Ying Feng Xing Zhang Hongwei Guo State Key Laboratory of Protein and Plant Gene Research College of Life Sciences Peking-Tsinghua Center for Life Sciences Peking University

Flowering is a highly orchestrated and extremely ct critical process in a plant＇s life cycle. Previous study has ademonstrated that SUPPRESSOR OF OVEREXPRESSION OF pCONSTANS 1（SOC1） and FLOWERING LOCUS T（FT） integrate m^-1 the gibberellic acid（GA） signaling pathway and vernalization higpathway in regulating flowering time, but detailed molecular Hmechanisms remain largely unclear. In GA signaling pathway,DELLA proteins are a group of master transcriptional regulators, while in vernalization pathway FLOWERING LOCUS C（FLC） is a core transcriptional repressor that down-regulates the expression of SOC1 and FT. Here, we report that DELLA proteins interact with FLC in vitro and in vivo, and the LHRI domains of DELLAs and the C-terminus of maDS domain of FLC are required for these *** and gene expression analysis showed that mutation of FLC reduces while over-expression of FLC enhances the GA response in the flowering process. Further,DELLA-FLC interactions promote the repression ability of FLC on its target genes. In summary, these findings report that the interaction between maDS box transcription factor FLC and GRAS domain regulator DELLAs may integrate various signaling inputs in flowering time control, and shed new light on the regulatory mechanism both for FLC and DELLAs in regulating gene expression.

关键词： Arabidopsis co-repressor DELLAs FLC flowering

不同方法改善口服清肠药口感及不良反应的研究进展

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华西医学 2024年第1期39卷 153-158页

作者：潘杰马梦迪林中华王瑶隋牮箐康复大学青岛医院(青岛市市立医院)消化内二科山东青岛266001

结肠镜检查是诊断、治疗结肠疾病及早癌筛查的金标准,良好的肠道准备质量,即肠道清洁度,是结肠黏膜病变及其细节充分可视化的前提条件。临床上使用较多的口服肠道清洁剂,如聚乙二醇、硫酸镁等口感差,服药量大,部分患者不能耐受,影响肠... 详细信息

结肠镜检查是诊断、治疗结肠疾病及早癌筛查的金标准,良好的肠道准备质量,即肠道清洁度,是结肠黏膜病变及其细节充分可视化的前提条件。临床上使用较多的口服肠道清洁剂,如聚乙二醇、硫酸镁等口感差,服药量大,部分患者不能耐受,影响肠道准备的效果。而口含辅助剂、清肠药加辅助剂、采用新型小容量或极低剂量聚乙二醇-抗坏血酸制剂等方法的出现可以降低患者恶心、呕吐等不良反应发生率,提高患者的耐受性、满意度等。该文对国内外改善清肠药口感、减轻不良反应的方法进行综述,为临床提供参考。

关键词：肠道准备结肠镜检查清肠药口感

FHY3 and FAR1 Integrate Light Signals with the miR156-SPL Module-Mediated Aging Pathway to Regulate Arabidopsis Flowering

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Molecular Plant 2020年第3期13卷 483-498页

作者： Yurong Xie Qin Zhou Yongping Zhao Quanquan Li Yang Liu mengdi ma Baobao Wang Rongxin Shen Zhigang Zheng Haiyang Wang Biotechnology Research Institute Chinese Academy of Agricultural SciencesBeijing 100081China Graduate School of Chinese Academy of Agriculturai Sciences Beijing 100081China State Key Laboratory of Crop Biology College of AgronomyShandong Agricultural UniversityTai’an 271018China State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources South China Agricultural UniversityGuangzhou 510642China Guangdong Laboratory for Lingnan Modern Agriculture Guangzhou 510642China

In response to competition for light from their neighbors,shade-intolerant plants flower precociously to ensure reproductive success and ***,the molecular mechanisms underlying this key developmental switch are not well ***,we show that a pair of Arabidopsis transcription factors essential for phytochrome A signaling,FAR-RED ELONGATED HYPOCOTYL3(FHY3)and FAR-RED IMPAIRED RESPONSE1(FAR1),regulate flowering time by integrating environmental light signals with the miR156-SPL module-mediated aging *** found that FHY3 and FAR1 directly interact with three flowering-promoting SQUAMOSA-PROMOTER BINDING PROTEIN-LIKE(SPL)transcription factors,SPL3,SPL4,and SPL5,and inhibit their binding to the promoters of several key flowering regulatory genes,including FRUITFUL(FUL),LEAFY(LFY),APETALA1(AP1),and MIR172C,thus downregulating their transcript levels and delaying *** simulated shade conditions,levels of SPL3/4/5 proteins increase,whereas levels of FHY3 and FAR1 proteins decline,thus releasing SPL3/4/5 from FHY3/FAR1 inhibition to allow activation of FUL,LFY,AP1,and MIR172C and,consequently,early *** together,these results unravel a novel mechanism whereby plants regulate flowering time by integrating environmental cues(such as light conditions)and an internal developmental program(the miR156-SPL module-mediated aging pathway).

关键词： Arabidopsis FHY3/FAR1 SPL3/4/5 FUL/LFY/AP1 MIR172C flowering time

A Comprehensive Study of a Low-Grade Heat-Driven Cooling and Power System Based on Heat Current Method

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Journal of Thermal Science 2024年第4期33卷 1523-1541页

作者： ZHAO Tian XU Ronghong XIN Yonglin HE Kelun ma Huan YUAN mengdi CHEN Qun School of Energy Storage Science and Engineering North China University of TechnologyBeijing100144China Key Laboratory for Thermal Science and Power Engineering of Ministry of Education Department of Engineering MechanicsTsinghua UniversityBeijing100084China

Combined cooling and power(CCP)system driven by low-grade heat is promising for improving energy *** work proposes a CCP system that integrates a regenerative organic Rankine cycle(RORC)and an absorption chiller on both driving and cooling fluid *** system is modeled by using the heat current method to fully consider nonlinear heat transfer and heat-work conversion constraints and resolve its behavior *** off-design system simulation is performed next,showing that the fluid inlet temperatures and flow rates of cooling water as well as RORC working fluid strongly affect system *** off-design operation even becomes infeasible when parameters deviate from nominal values largely due to limited heat transfer capability of components,highlighting the importance of considering heat transfer constraints via heat current *** optimization aiming to minimize the total thermal conductance is also *** efficiency increases by 7.9%and decreases by 12.4%after optimization,with the hot fluid inlet temperature increase from 373.15 to 403.15 K and mass flow rate ranges from 10 to 30 kg/s,emphasizing the necessity of balancing system cost and performance.

关键词： combined cooling and power system organic Rankine cycle absorption chiller cascade heat utilization heat current method off-design analysis

Three-dimensional nanoscale vortex line visualization and chiral nanostructure fabrication of tightly focused multi-vortex beams via direct laser writing

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Photonics Research 2024年第1期12卷 70-77页

作者： mengdi LUO JISEN WEN PENGCHENG ma QIUYUAN SUN XIANMENG XIA GANGYAO ZHAN ZHENYAO YANG LIANG XU DAZHAO ZHU CUIFANG KUANG XU LIU Research Center for Intelligent Chips and Devices Zhejiang LabHangzhou 311100China State Key Laboratory of Extreme Photonics and Instrumentation College of Optical Science and EngineeringZhejiang UniversityHangzhou 310027China ZJU-Hangzhou Global Scientific and Technological Innovation Center Hangzhou 311200China

Optical singularity is pivotal in nature and has attracted wide interest from many disciplines nowadays,including optical communication,quantum optics,and biomedical *** vortex lines formed by phase singularities and fabricating chiral nanostructures using the evolution of vortex lines are of great *** this paper,we introduce a promising method based on two-photon polymerization direct laser writing(2PP-DLW)to record the morphology of vortex lines generated by tightly focused multi-vortex beams(MVBs)at the *** to Gouy phase,the singularities of the MVBs rotate around the optical axis and move towards each other when approaching the focal *** propagation dynamics of vortex lines are recorded by 2PP-DLW,which explicitly exhibits the evolution of the phase ***,the MVBs are employed to fabricate stable three-dimensional chiral nanostructures due to the spiral-forward property of the vortex *** of the obvious chiral features of the manufactured nanostructures,a strong vortical dichroism is observed when excited by the light carrying orbital angular momentum.A number of applications can be envisioned with these chiral nanostructures,such as optical sensing,chiral separation,and information storage.

关键词： vortex chiral singularity

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考虑应力比修正的应力梯度影响指数计算方法

航空动力学报 2019年第9期34卷 1888-1894页

作者：魏大盛马梦弟王延荣北京航空航天大学能源与动力工程学院北京100191 先进航空发动机协同创新中心北京100191

基于考虑应力梯度的寿命预测模型,深入研究了不同应力比对应力梯度影响指数的影响。通过引入新的参数,对模型进行修正,并以典型合金的试验数据为基础,进行寿命预测并考核计算精度。结果表明:修正后的模型能够更合理地考虑局部应力比对... 详细信息

基于考虑应力梯度的寿命预测模型,深入研究了不同应力比对应力梯度影响指数的影响。通过引入新的参数,对模型进行修正,并以典型合金的试验数据为基础,进行寿命预测并考核计算精度。结果表明:修正后的模型能够更合理地考虑局部应力比对应力梯度影响指数的影响,寿命预测结果相比于修正前更接近试验值,对TC4(200℃)、GH4169(500、650℃)缺口试件的疲劳寿命预测结果多在2.0倍分散带以内,部分数据的预测结果可在1.5倍分散带以内。

关键词：寿命预测缺口疲劳应力梯度应力比参数拟合