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Chinese Journal of Chemistry 2022年第2期40卷 209-214页

作者： Yu Teng Hong Yang Xiang Li Yongcheng Wang dali yin Yulin Tian State Key Laboratory of Bioactive Substances and Function of Natural Medicine Beijing Key Laboratory of Active Substances Discovery and Drugability EvaluationInstitute of Materia MedicaPeking Union Medical College and Chinese Academy of Medical Sciences1st Xian Nong Tan StreetBeijing 100050China

A nitrone-modified 1,8-naphthalimide was desig ned as a novel bioorthog on alactivated turn-on probe based on strain-promoted alkyne-nitrone cycloadditio n(SPANC).The bioorthog onal cycloadducts were subseque ntly tran sformed into fluoresce nt rearra nge-ment products by photo-accelerati on,which exhibited sign ificant fluoresce nee enhan ceme nt,large stokes shift,and high fluores-cence qua ntum yield.DFT calculati ons were performed to elucidate the fluoresce nee OFF-ON mecha nism.This fluoroge nic strategy was successfully applied to labeling of proteins and visualizing mitochondria in live cells in real time.

关键词： Bioorthogonal reaction Fluorescence Naphthalimide Imaging agents Cycloaddition

A general strategy for in situ assembly of light-up fluorophores via bioorthogonal Suzuki-Miyaura cross-coupling

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Chinese Chemical Letters 2022年第9期33卷 4223-4228页

作者： Xiang Li Hong Yang Yu Teng Yongcheng Wang dali yin Yulin Tian Key Laboratory of Bioactive Substances and Function of Natural Medicine Beijing Key Laboratory of Active Substances Discovery and Drugability EvaluationInstitute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

Herein we presented a general strategy for in situ assembly of intramolecular charge-transfer(ICT)-based light-up fluorophores via bioorthogonal Suzuki-Miyaura cross-coupling reaction.By introducing iodo group at the appropriate position,five fluorophores with different scaffolds including naphthalimide,coumarin,naphthalene sulfonate,nitrobenzoxadiazole,and acetonaphthone,were designed as bioorthogonal multicolor fluorogenic probes,which could produce significant fluorescence enhancement and high fluorescence quantum yield after Suzuki-Miyaura reaction with aryl boronic acid or boronate.Manipulating the substituents andπscaffold in the fluorophores allows fine-tuning of their photophysical properties.With this strategy,we succeeded in peptide conjugation,no-wash fluorogenic protein labeling,and mitochondria-selective bioorthogonal imaging in live cells.

关键词： Bioorthogonal reaction Suzuki-Miyaura cross-coupling Fluorogenic probes Naphthalimide Live-cell imaging

Synthesis of tetrahydroisoquinolines through TiCl4-mediated cyclization and Et3SiH reduction

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Chinese Chemical Letters 2020年第3期31卷 729-732页

作者： Zeyu Shi Qiong Xiao dali yin State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia MedicaPeking Union Medical College and Chinese Academy of Medical SciencesBeijing 100050China Department of Medicinal Chemistry Beijing Key Laboratory of Active Substances Discovery and Drugability EvaluationInstitute of Materia MedicaPeking Union Medical College and Chinese Academy of Medical SciencesBeijing 100050China

A versatile and efficient telescoped reaction sequence for the synthesis of tetrahydroisoquinolines(THIQs)is reported that uses TiCl4 to promote cyclization of a benzylaminoacetal derivative and Et3SiH for reduction of the intermediate 4-hydroxy-THIQ.This method is complimentary to the classical Pomeranz-Fritsch and related reactions since it tolerates electron-withdrawing substituents and allows access to 8-substituted THIQs.

关键词： Tetrahydroisoquinoline TiCl4 Cyclization Et3SiH Telescoped reaction

A facile synthesis of goodyeroside A from (S)-malic acid

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Science China Chemistry 2009年第12期52卷 2176-2179页

作者： Feng Zhang Jun Wei dali yin HaiHong Huang YanHong Zhang Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 China National Engineering Research Center for the Development of New Drugs Beijing 102600 China

Goodyeroside A 1,a natural product with hepatoprotective activity,was efficiently synthesized in a total yield of 47% in five steps starting from (S)-malic acid. The spectral data of the target compound 1 is identical... 详细信息

关键词： goodyeroside A esterification protecting group glycoside lactonization

Design and synthesis of selective sphingosine-1-phosphate receptor 1 agonists with increased phosphorylation rates

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Acta Pharmaceutica Sinica B 2020年第6期10卷 1134-1142页

作者： Qiong Xiao Minwan Hu Si Chen Yifan Tang Zeyu Shi Jing Jin Jinping Hu Ping Xie dali yin Department of Medicinal Chemistry State Key Laboratory of Bioactive Substance and Function of Natural MedicinesBeijing Key Laboratory of Active Substances Discovery and Druggability EvaluationInstitute of Materia MedicaPeking Union Medical CollegeChinese Academy of Medical SciencesBeijing 100050China Departments of Drug Metabolism Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD StudyInstitute of Materia MedicaPeking Union Medical CollegeChinese Academy of Medical SciencesBeijing 100050China Beijing Union Pharmaceutical Factory Beijing 102600China Department of Pharmacology State Key Laboratory of Bioactive Substance and Function of Natural MedicinesInstitute of Materia MedicaPeking Union Medical CollegeChinese Academy of Medical SciencesBeijing 100050China

FTY720 and IMMH002,prodrugs for sphingosine-1-phosphate receptor 1(S1P1)agonists,show inadequate and inconsistent levels of phosphorylation in humans compared to that in rats.In this study,FTY720 or IMMH002 analogues(21-24)were designed and synthesized with modified head pieces to improve the biotransformation of the prodrugs to the active phosphorylated forms.Target compounds were synthesized via a convergent route using the key and optically pure building block 9,which was first synthesized via asymmetrically catalyzed amination.The phosphorylation rates of these analogues in rat or human blood were compared.The new methyl-substituted analogue compound 21 showed higher phosphorylation rates in both rats and humans than the parent compound,whereas compound 23 showed improvements in rats,but not in humans.In pharmacokinetics studies of rats,compounds 21 and 23 both had higher levels of phosphorylation than FTY720 and IMMH002.Thus,our study not only yielded new compounds with therapeutic potential,but also showed species differences between rats and humans in response to the structural modifications,which might be useful for predicting the biotransformation behavior and efficacy of this class of prodrugs in the clinic.

关键词： S1P1 agonist Prodrug Catalytic amination Phosphate formation rate Lymphocyte

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

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Acta Pharmaceutica Sinica B 2020年第2期10卷 276-288页

作者： Jing Jin Nina Xue Yuan Liu Rong Fu Mingjin Wang Ming Ji Fangfang Lai Jinping Hu Xiaojian Wang Qiong Xiao Xiaoying Zhang dali yin Liping Bai Xiaoguang Chen Shuan Rao State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia MedicaChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100050China Department of Thoracic Surgery Nanfang HospitalSouthern Medical UniversityGuangzhou 510515China State Key Laboratory of Quality Research in Chinese Medicine Macao Institutefor Applied Research in Medicine and HealthMacao University of Science and TechnologyTaipaMacao SAR 999078China

Psoriasis is characterized by abnormal proliferation of keratinocytes,as well as infiltration of immune cells into the dermis and epidermis,causing itchy,scaly and erythematous plaques of skin.The understanding of this chronic inflammatory skin disease remains unclear and all available treatments have their limitations currently.Here,we showed that IMMH002,a novel orally active S1 P1 modulator,desensitized peripheral pathogenic lymphocytes to egress signal from secondary lymphoid organs and thymus.Using different psoriasis animal models,we demonstrated that IMMH002 could significantly relieve skin damage as revealed by PAS I score and pathological injure evaluation.Mechanistically,IMMH002 regulated CD3+T lymphocytes re-distribution by inducing lymphocytes’homing,thus decreased T lymphocytes allocation in the peripheral blood and skin but increased in the thymus.Our results suggest that the novel SIP1 agonist,IMMH002,exert extraordinary capacity to rapidly modulate T lymphocytes distribution,representing a promising drug candidate for psoriasis treatment.

关键词： S1P1 S1P1 agonist IMMH002 Lymphocyte Psoriasis

Multi-scale analysis of carbon mineralization in lime-treated soils considering soil mineralogy

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Journal of Rock Mechanics and Geotechnical Engineering 2024年第6期16卷 2296-2309页

作者： Dhanalakshmi Padmaraj Chinchu Cherian dali Naidu Arnepalli Department of Civil Engineering Indian Institute of Technology MadrasChennai600036India University of Northern British Columbia Prince GeorgeBCV2N4Z9Canada

Mineral carbonation is emerging as a reliable CO_(2) capture technology that can mitigate climate change.In lime-treated clayey soils,mineral carbonation occurs through the carbonation of free lime and cementitious products derived from pozzolanic reactions.The kinetics of the reactions in lime-treated clayey soils are variable and depend primarily on soil mineralogy.The present study demonstrates the role of soil mineralogy in CO_(2) capture and the subsequent changes caused by carbon mineralization in terms of the unconfined compressive strength(UCS)of lime-treated soils during their service life.Three clayey soils(kaolin,bentonite,and silty clay)with different mineralogical characteristics were treated with 4%lime content,and the samples were cured in a controlled environment for 7 d,90 d,180 d,and 365 d.After the specified curing periods,the samples were exposed to CO_(2) in a carbonation cell for 7 d.The non-carbonated samples purged with N2 gas were used as a benchmark to compare the mechanical,chemical-mineralogical,and microstructure changes caused by carbonation reactions.Experimental investigations indicated that exposure to CO_(2) resulted in an average increase of 10%in the UCS of limetreated bentonite,whereas the strength of lime-treated kaolin and silty clay was reduced by an average of 35%.The chemical and microstructural analyses revealed that the precipitated carbonates effectively filled the macropores of the treated bentonite,compared to the inadequate cementation caused by pozzolanic reactions,resulting in strength enhancement.In contrast,strength loss in lime-treated kaolin and silty clay was attributed to the carbonation of cementitious phases and partly to the tensile stress induced by carbonate precipitation.In terms of carbon mineralization prospects,lime-treated kaolin exhibited maximum carbonation due to the higher availability of unreacted lime.The results suggest that,in addition to the increase in compressive strength,adequate calcium-bearing phases and macropores determine the effic

关键词： Clays Mineralogy Carbon capture Lime Strength Pore structure

Design, synthesis and in vitro antitumor evaluation of novel diaryl urea derivatives bearing sulfonamide moiety

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Science China Chemistry 2013年第11期56卷 1564-1572页

作者： LUO Can TANG Ke LI Yan yin dali CHEN XiaoGuang HUANG HaiHong Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation Institute of Materia Medica Peking Union Medical College & Chinese Academy of Medical Sciences

A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized.Their in vitro antitumor effect against human cancer cell lines MX-1,A375,HepG2,Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control.Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib.In particular,2,6-dimethyl-4-{6-[3-(4-chloro-3-(trifluoromethyl)phenyl)urea]naphthalen-2-yl}sulfonyl morpholine(10d)was found to be the most potent against A375,HepG2 and Ketr3 with IC50values of 0.65–0.97mol/L,which were 5–20-fold more potent than sorafenib.Compound 10d emerged as a valuable lead for further optimization.

关键词：体外抗肿瘤脲衍生物二芳基胺基团设计评价轴承合成

WNT7A promotes tumorigenesis of head and neck squamous cell carcinoma via activating FZD7/JAK1/STAT3 signaling

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International Journal of Oral Science 2024年第1期16卷 85-96页

作者： Qingling Huang Yi Xiao Ting Lan Youguang Lu Li Huang dali Zheng Department of Biochemistry and Molecular Biology School of Basic Medical SciencesFujian Medical UniversityFuzhouChina Fujian Key Laboratory of Oral Diseases School and Hospital of StomatologyFujian Medical UniversityFuzhouChina Department of Preventive Dentistry School and Hospital of StomatologyFujian Medical UniversityFuzhouChina Department of Dentistry The First Affiliated Hospital of Fujian Medical UniversityFuzhouChina

Wnt signaling are critical pathway involved in organ development, tumorigenesis, and cancer progression. WNT7A, a member of the Wnt family, remains poorly understood in terms of its role and the underlying molecular mechanisms it entails in head and neck squamous cell carcinoma (HNSCC). According to the Cancer Genome Atlas (TCGA), transcriptome sequencing data of HNSCC, the expression level of WNT7A in tumors was found to be higher than in adjacent normal tissues, which was validated using Real-time RT-PCR and immunohistochemistry. Unexpectedly, overexpression of WNT7A did not activate the canonical Wnt-β-catenin pathway in HNSCC. Instead, our findings suggested that WNT7A potentially activated the FZD7/JAK1/STAT3 signaling pathway, leading to enhanced cell proliferation, self-renewal, and resistance to apoptosis. Furthermore, in a patient-derived xenograft (PDX) tumor model, high expression of WNT7A and phosphorylated STAT3 was observed, which positively correlated with tumor progression.These findings underscore the significance of WNT7A in HNSCC progression and propose the targeting of key molecules within the FZD7/JAK1/STAT3 pathway as a promising strategy for precise treatment of HNSCC.

关键词： WNT squamous tumorigenesis

Characterization of ZnO Based Varistor Derived from Nano ZnO Powders and Ultrafine Dopants

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Journal of Materials Science & Technology 2005年第2期21卷 183-186页

作者： Weizhong YANG, dali ZHOU, Guangfu yin, Runsheng WANG and Yun ZHANG College of Material Science and Engineering, Sichuan University, Chengdu 610064, China Coll. of Mat. Sci. and Eng. Sichuan Univ. Chengdu 610064 China

Nanosized ZnO powders were prepared with a two-step precipitation method. The average size of ZnO particles was about 80 nm and their size distribution was narrow. Combining with ultrafine additive powders, ZnO base varistor was produced via an oxide mixing route. ZnO varistor derived from normal reagent grade starting materials was investigated for comparison purpose. Outstanding microstructure of the ZnO varistor derived from nanosize ZnO powders and ultrafine dopants was obtained: uniform distribution of fine ZnO grains (less than 3 microns), grain boundary and the dopant position. Higher varistor voltage (U=492 V/mm) and nonlinear coefficient (α=56.2) as well as lower leakage current (TL=1.5 μuA) were achieved. The better electrical properties were attributed to the uniform microstructure, which in turn led to stable and uniform potential barriers. Also this improved technique is more feasible for producing ZnO nanopowders and resulting varistor in large scales.

关键词： Zinc oxide (ZnO) Varistor Nanopowders Ultrafine dopants Two-step precipitation