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A five-component one-pot synthesis of phosphatidylinositol pentamannoside(PIM_5)

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Chinese Chemical Letters 2018年第9期29卷 1340-1342页

作者： Dong Wang De-Cai Xiong Xin-Shan Ye state key laboratory of natural and Biomimetic drugs School of Pharmaceutical Sciences Peking University

A practical and efficient synthesis of phosphatidylinositol pentamannoside （PIM5） was achieved based on a five-component one-pot sequential glycosylation protocol with exclusive regio- and stereo-selectivity. Two regioselective sequential glycosylations on inositol and p-tolyl thioglycosides as the sole type of building blocks made this protocol to avoid the tedious protective group manipulations. This synthetic strategy provides access to other important glycolipids with similar structures.

关键词： Phosphatidylinositol pentamannoside Glycosylation Preactivation One-pot synthesis Thioglycoside

Copper-catalyzed enantioselective cyanation of benzylic C–H bonds via radical relay

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Science China Chemistry 2017年第1期60卷 105-106页

作者： Yujie Liang Ning Jiao state key laboratory of natural and Biomimetic drugs School of Pharmaceutical Sciences Peking University Beijing 100191 China

Direct methods that enable stereoselective functionalization of C（sp^3）–H bonds could facilitate efficient preparation of therapeutics and agrochemicals,and shall have a major effect on the discovery and development of new *** the transformations through C（sp^2）–H bond cleavage have been significantly developed in the past decades,the direct C（sp^3）–H functionalization,especially the asymmetric transformation is still a big challenge.

关键词： Carbon Copper Cyanides Drug products

Schisandrol A protects AGEs-induced neuronal cells death by allosterically targeting ATP6V0d1 subunit of V-ATPase

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Acta Pharmaceutica Sinica B 2022年第10期12卷 3843-3860页

作者： Xiaoqing Zhou Shaoyang Zhao Tingting Liu Lu Yao Meimei Zhao Xiaoming Ye Xiaowen Zhang Qiang Guo Pengfei Tu Kewu Zeng state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

Diabetes have been shown to cause progressive neuronal injury with pain and numbness via advanced glycation end-products(AGEs)-induced neuronal cell apoptosis;however, the valuable drug targets for diabetic neuropathy have been poorly reported so far. In this study, we discovered a natural small-molecule schisandrol A(SolA) with significant protective effect against AGEs-induced neuronal cell apoptosis. ATP6V0D1, a major subunit of vacuolar-type ATPase(V-ATPase) in lysosome was identified as a crucial cellular target of SolA. Moreover, SolA allosterically mediated ATP6V0D1 conformation via targeting a unique cysteine 335 residue to activate V-ATPase-dependent lysosomal ***, SolA-induced lysosome pH downregulation resulted in a mitochondrial-lysosomal crosstalk by selectively promoting mitochondrial BH3-only protein BIM degradation, thereby preserving mitochondrial homeostasis and neuronal cells survival. Collectively, our findings reveal ATP6V0D1 is a valuable pharmacological target for diabetes-associated neuronal injury via controlling lysosomal acidification, and also provide the first small-molecule template allosterically activating V-ATPase for preventing diabetic neuropathy.

关键词： Allosteric regulation Advanced glycation endproducts AGEs Lysosomal acidification Targets V-ATPase ATP6V0D1 Schisandrol A Diabetic neuropathy

Novel carbohydrate-triazole derivatives as potentialα-glucosidase inhibitors

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Chinese Journal of natural Medicines 2020年第10期18卷 729-737页

作者： ZHANG Zi-Pei XUE Wan-Ying HU Jian-Xing XIONG De-Cai WU Yan-Fen YE Xin-Shan state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

A series of novel pyrano[2,3-d]trizaole compounds were synthesized and theirα-glucosidase inhibitory activities were evaluated by in vitro enzyme *** experimental data demonstrated that compound 10 f showed up to 10-fold higher inhibition(IC5074.0±1.3μmol·L-1)than *** molecular docking revealed that compound 10 f could bind toα-glucosidase via the hydrophobic,π-πstacking,and hydrogen bonding *** results may benefit further structural modifications to find new and potentα-glucosidase inhibitors.

关键词： Pyrano[2,3-d]trizaole α-Glucosidase inhibitor Enzyme assay Molecular docking

Synthesis,physicochemical and biological properties of oligonucleotides incorporated with amino-isonucleosides

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Science China Chemistry 2012年第1期55卷 70-79页

作者： WANG Fang CHEN Yue HUANG Ye JIN Hong-Wei ZHANG Liang-Ren YANG Zhen-Jun ZHANG Li-He state key laboratory of natural and Biomimetic drugs School of Pharmaceutical Sciences Peking UniversityBeijing 100191China

Antisense oligonucleotides(ASONs) and siRNAs have been applied extensively for the regulation of cellular and viral gene expression,and RNAi is currently one of the most promising new approaches for anti-tumor and anti-viral *** order to improve bioactivity properties and physicochemical properties of siRNA,we synthesized a novel class of ASONs II-VII incorporated with amino-isonucleoside(isoA1 and isoA2) for investigation on basic physicochemical *** we designed amino-isonucleoside(isoA1,isoA2 and isoT1) incorporated siRNA *** meaningful results have been obtained from the physicochemical property experiments in *** RNAi potency experiments,we investigated RNAi potency of each strand of the *** amino-isonucleosides incorporated siRNAs showed promising bioactivity properties and had position *** off target effect from sense strand loading in siRNA application was observed.

关键词： amino-isonucleoside antisense oligonucleotide siRNA

Supramolecular Assembly Models of siRNA Delivery Systems

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Chinese Journal of Chemistry 2015年第1期33卷 79-89页

作者： Jing Sun Jiancheng Wang Zhenjun Yang state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

Small interfering RNA(siRNA)technology,which could be able to silence specific targeted mRNAs rapidly and efficiently,has been regarded as a novel and potent gene therapeutic approach for diseases,such as cancers,in-fections,inflammations and neurological ***,some conspicuous intrinsic defects of siRNA including the poor cellular uptake,low biological stability,unfavorable pharmacokinetics and bio-distribution properties,have hindered further applications in ***,it is prerequisite to design safe and effective siRNA delivery systems for the successful development of siRNA-based various diseases *** review aims to analyze and summarize these supramolecular assembly models in the process of siRNA delivery,namely recent nanotech-nological strategies for carrying siRNA by using diverse non-viral vehicles such as cationic liposomes,stable nucleic acid lipid particles(SNALPs),cationic polymers,cationic dendrimers,inorganic nanoparticles and ***,it is concluded with future perspectives of siRNA therapeutics in the field of non-viral carriers.

关键词： siRNA delivery supramolecular assembly non-viral vectors nanocarriers

In vitro selection of G-rich RNA aptamers that target HIV-1 integrase

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Science China Chemistry 2008年第5期51卷 401-413页

作者： LIU YingChun ZHANG Yan YE GuoZhu YANG ZhenJun ZHANG LiangRen ZHANG LiHe state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100083China

Aptamers that interact with various HIV-1 proteins,such as reverse transcriptase,Rev,Tat protein,and nuclear capsule protein,have been prepared through SELEX (systematic evolution of ligands by ex-ponential enrichment) technique. However,there are few reports about the DNA or RNA aptamers that target HIV-1 integrase. In this investigation,we selected alternative RNA aptamers specific for the HIV-1 integrase by using a different binding buffer containing 10 mmol·L-1 MgCl2 and 100 mmol·L-1 KCl. Aptamer IN1,IN2,IN3 had similar and the highest Kd values from 145 to 239 nmol·L-1. Structural studies showed that they formed similar stem-loop structure. Deletion of any stem structure resulted in diminished affinity. In addition,structure probing study with antisense DNA indicated that the stem-loop structure in the random region was critical for integrase binding. Although aptamer IN1 failed to form G-quartet structure,it might directly interact with the DDE motif of integrase,which is the virus DNA-binding site,because G-quadruplex T40214 competitively inhibited the interaction between IN1 and integrase. Together,this study generated a novel RNA aptamer IN1,which could be useful in basic research and anti-HIV drug screening.

关键词： RNA aptamer HIV-1 integrase G-quadruplex

NO inhibitory constituents from Glycosmis craibii ***

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Chinese Journal of natural Medicines 2024年第11期22卷 1040-1046页

作者： CHEN Hongwei DING Meng LIN Jun YUAN Shuo ZENG Kewu TU Pengfei JIANG Yong state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

Six novel compounds,comprising three quinolones(1a,1b,and 2)and three flavanones(3-5),along with seven known analogs(6-13),were isolated from the 95%EtOH extract of the stems and leaves of Glycosmis craibii *** structures of the new compounds were elucidated using HR-ESI-MS,UV,and 1D and 2D nuclear magnetic resonance(NMR)data *** ab-solute configurations were determined through Mosher ester and electronic circular dichroism(ECD)spectral *** 2,6,9,and 10 demonstrated inhibition of nitric oxide(NO)production stimulated by lipopolysaccharide in BV-2 microglial cells,with IC50 values ranging from 13.5 to 20.1 μmol·L^(-1),comparable to the positive control,dexamethasone.

关键词： Glycosmis craibii var.glabra Quinolone Flavanone NO inhibition

Four new phenolic glycosides from Baoyuan decoction

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Acta Pharmaceutica Sinica B 2017年第2期7卷 173-178页

作者： Xiaoli Ma Xiaoyu Guo Mingbo Zhao Pengfei Tu Yong Jiang state key laboratory of natural and Biomimetic drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

Four new phenolic glycosides,including two flavonoid glycosides(1 and 2) and two lignan glycosides(3 and 4),were isolated from the traditional Chinese medicine formula,Baoyuan *** structures were established by detailed analysis of the NMR and HR-ESI-MS spectroscopic data and their absolute configurations were determined by the experimental electronic circular dichroism data as well as chemical ***,the sources of the four new compounds were determined by the UPLC-Qtrap-MS method,which proved that 1 and 2 are originated from Glycyrrhiza uralensis,and 3 and4 are from Cinnamomum cassia.

关键词： Baoyuan decoction Traditional Chinese med icine formula Flavonoid glycosides Lignan glycosides Electronic circular dichroism UPLC–Qtrap-MS