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Chinese Journal of Natural Medicines 2019年第2期17卷 155-160页

作者： XIONG Lei CHEN Chang-Fa MIN Tao-Ling HU Hai-Feng state key lab of new drug&pharmaceutical process Shanghai Institute of Pharmaceutical Industry China State Institute of Pharmaceutical Industry

Romipeptides A and B(1 and 2),two new romidepsin derivatives,and three known compounds,chromopeptide A(3),romidepsin(4)and valine-leucine dipeptide(5)were isolated from the fermentation broth of Chromobacterium violaceum *** structures were elucidated by interpretation of their UV,HR-ESI-MS and NMR *** absolute configuration of compound 1 and 2 were established by single crystal X-ray diffraction *** 1–5 were evaluated for their anti-proliferative activities against three human cancer cell lines,SW620,HL60,and *** results showed most of these compounds exhibited antitumor activities in vitro,in which compound 2 displayed potent cytotoxicity to SW620,HL60 and A549 cell lines,with IC_(50) of 12.5,6.7 and 5.7 nmol·L^(–1),respectively.

关键词： Chromobacterium violaceum Romidepsin derivatives Cytotoxicity

Synthesis,Configuration Judgment and Potentiation Activity of (2S,3S,E)-4-(3,4-Dihydroxybenzylidene)-3-(3,4-dihydroxyphenyl)-5-oxotetrahydrofuran-2-carboxylic Acid

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Chinese Journal of Structural Chemistry 2017年第9期36卷 1418-1424页

作者：张骏良吕志良钟家亮陈代杰李默影张建斌 state key laboratory of new drug and pharmaceutical process Shanghai Institute of Pharmaceutical IndustryChina State Institute of Pharmaceutical Industry Zhangjiang Branch Institute of China state Institute of pharmaceutical Industry Shanghai Institute of pharmaceutical Industry

The title compound（2S,3S,E）-4-（3,4-dihydroxybenzylidene）-3-（3,4-dihydroxyphenyl）-5-oxotetrahydrofuran-2-carboxylic acid was synthesized and the 2D structure was characterized by ^1H-NMR ^13C-NMR and LCMS. The absolute configuration was determined by single-crystal X-ray diffraction of the key intermediate（2S,3S,E）-ethyl 4-（3,4-dimethoxybenzylidene）-3-（3,4-dimethoxyphenyl）-5-oxotetrahydrofuran-2-carboxylate. The crystal belongs to tetragonal system, space group P41 with a = 13.0665（2）, b = 13.0665（2）, c = 13.4735（2）A, V = 2300.4（6） A^3, Z = 4, Dc = 1.278 g/cm^3, μ（CuKα） = 0.801 mm^-1, F（000） = 936, S = 1.050, R = 0.0364 and wR（I 〉 2σ（I）） = 0.1071. X-ray diffraction results showed that the molecular structure is stabilized totally by Van der Waals force. The antibacterial activity tests showed that the title compound possesses slight synergistic effect against MRSA and Acinetobacter baumanii.

关键词： total synthesis crystal structure potentiation activity traditional Chinese medicine synergistic effect

new phenylbutenoids and terpene glycosides from Ginkgo biloba leaves

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Chinese Journal of Natural Medicines 2024年第2期22卷 161-170页

作者： SUN Zeshi LIN Shan WU Zhi-Li DONG Hong-Yuan XU Xi-Ke LI Hui-Liang WANG Jinxin School of Pharmacy Second Military Medical UniversityShanghai 200433China state key laboratory of new drug and pharmaceutical process Shanghai Institute of Pharmaceutical IndustryChina State Institute of Pharmaceutical IndustryShanghai 201203China

Our continued works on the chemical constituents of Ginkgo biloba(***)leaves has led to the isolation of two novel phenylbutenoids(1,2),along with five previously unidentified terpene glycosides(3−7).Among them,compounds 1 and 2 represent unique(Z)-phenylbutenoids,3−6 are megastigmane glycosides,and 7 is identified as a rare bilobanone glycoside(Fig.1).This study marks the first reported isolation of phenylbutenoid and bilobanone glycoside from *** chemical structures of these compounds were elucidated through extensive spectroscopic analysis,including HR-ESI-MS and various 1D and 2D NMR ***,the absolute configurations of these molecules were determined using Mosher’s method,ECD experiments,and Cu-KαX-ray crystallographic analyses.

关键词： Ginkgo biloba Phenylbutenoid Megastigmane glycoside Bilobanone glycoside

Two kinds of ketoprofen enteric gel beads(CA and CS-SA) using biopolymer alginate

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Asian Journal of pharmaceutical Sciences 2018年第2期13卷 120-130页

作者： Bingchao Cheng Dongyang Li Qiye Huo Qianqian Zhao Qi Lan Mengsuo Cui Weisan Pan Xinggang Yang Department of Pharmaceutics School of Pharmaceutical Sciences Shenyang Pharmaceutical University state key laboratory of new-tech for Chinese Medicine pharmaceutical process

To obtain expected rapid-release and sustained-release of ketoprofen gel beads, this paper adopted biopolymer alginate to prepare alginate beads and chitosan-alginate gel beads. Formulation factors were investigated and optimized by the single factor test. The release of ketoprofen from calcium alginate gel beads in pH 1.0 hydrochloric acid solution was less than 10% during 2 h, then in pH6.8 was about 95% during 45 min, which met the requirements of rapid-release preparations. However, the drug release of chitosan-alginate gel beads in pH1.0 was less than 5% during 2 h, then in pH6.8 was about 50% during 6 h and reached more than 95% during 12 h, which had a good sustained-release behavior. In addition, the release kinetics of keteprofen from the calcium alginate gel beads fitted well with the Korsmeyer–Peppas model and followed a case-II transport mechanism. However, the release of keteprofen from the chitosan-alginate gel beads exhibited a non-Fickian mechanism and based on the mixed mechanisms of diffusion and polymer relaxation from chitosanalginate beads. In a word, alginate gel beads of ketoprofen were instant analgesic, while chitosan-alginate gel beads could control the release of ketoprofen during gastrointestinal tract and prolong the drug's action time.

关键词： Gel beads Enteric rapid-release Enteric sustained-release Ketoprofen

A review of structural modification and biological activities of oleanolic acid

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Chinese Journal of Natural Medicines 2024年第1期22卷 15-30页

作者： YANG Huali DENG Minghui JIA Hongwei ZHANG Kaicheng LIU Yang CHENG Maosheng XIAO Wei state key laboratory of new-tech for Chinese Medicine pharmaceutical process Jiangsu Kanion Pharmaceutical Co.Ltd.Lianyungang 222001China key laboratory of Structure-Based drug Design&Discovery of Ministry of Education School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Oleanolic acid(OA),a pentacyclic triterpenoid,exhibits a broad spectrum of biological activities,including antitumor,antiviral,antibacterial,anti-inflammatory,hepatoprotective,hypoglycemic,and hypolipidemic *** its initial isolation and identification,numerous studies have reported on the structural modifications and pharmacological activities of OA and its *** this,there has been a dearth of comprehensive reviews in the past two decades,leading to challenges in subsequent research on *** on the main biological activities of OA,this paper comprehensively summarized the modification strategies and structureactivity relationships(SARs)of OA and its derivatives to provide valuable reference for future investigations into OA.

关键词： Oleanolic acid Derivatives Pentacyclic triterpenoid Structural modification Biological activities

Abietane diterpenoids and iridoids from Caryopteris mongolica

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Chinese Journal of Natural Medicines 2023年第12期21卷 927-937页

作者： ZHANG Shanshan MAO Xudong XU Hongtao WEI Xiaohui CHOU Guixin Institute of Chinese Materia Medica Shanghai University of Traditional Chinese MedicineShanghai 201203China Shanghai R&D Center for Standardization of Chinese Medicines Shanghai 201203China state key lab of new drug and pharmaceutical process Shanghai Institute of Pharmaceutical IndustryChina State Institute of Pharmaceutical IndustryShanghai 201203China

Six new abietane diterpenoids(1−6)and five undescribed iridoids(7−11)have been isolated from the aerial parts of Caryopteris *** intricate structural characterization of these compounds was meticulously undertaken using an array of advanced spectroscopic *** process was further enhanced by the application of DP4+probability analyses and electronic circular dichroism(ECD)*** isolation and structural elucidation,the cytotoxicity of these compounds was *** them,compound 3 stood out,displaying significant cytotoxic activity against HeLa cells with an IC50 value of 7.83±1.28μmol·L^(−1).Additionally,compounds 1,2,4,9,and 10 manifested moderate cytotoxic effects on specific cell lines,with IC50 values ranging from 11.7 to 20.9μmol·L^(−1).

关键词： Caryopteris mongolica Abietane diterpenoids Spectroscopic analysis Cytotoxicity

Discovery of proqodine A derivatives with antitumor activity targeting NAD(P)H:quinone oxidoreductase 1 and nicotinamide phosphoribosyltransferase

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Chinese Journal of Natural Medicines 2024年第1期22卷 75-88页

作者： SONG Jiangzhou ZOU Guiqing ZHAO Zhou ZHU Ya XUE Jiayu AO Lanjia SUN Huiyong HAO Haiping ZHANG Bo XU Xiaowei state key laboratory of Natural Medicines Key Lab of Drug Metabolism and PharmacokineticsChina Pharmaceutical UniversityNanjing 210009China state key laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009China

NAD(P)H:quinone oxidoreductase 1(NQO1)is a flavin protease highly expressed in various cancer ***1 catalyzes a futile redox cycle in substrates,leading to substantial reactive oxygen species(ROS)*** ROS generation results in extensive DNA damage and elevated poly(ADP-ribose)polymerase 1(PARP1)-mediated consumption of nicotinamide adenine dinucleotide(NAD^(+)),ultimately causing cell *** phosphoribosyltransferase(NAMPT),the rate-limiting enzyme in the NAD^(+)salvage synthesis pathway,emerges as a critical target in cancer *** concurrent inhibition of NQO1 and NAMPT triggers hyperactivation of PARP1 and intensive NAD+*** this study,we designed,synthesized,and assessed a novel series of proqodine A derivatives targeting both NQO1 and *** these,compound T8 demonstrated potent antitumor ***,T8 selectively inhibited the proliferation of MCF-7 cells and induced apoptosis through mechanisms dependent on both NQO1 and *** discovery offers a promising new molecular entity for advancing anticancer research.

关键词： NQO1 ROS NAMPT NAD^(+) T8

Recent progress in tumor photodynamic immunotherapy

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Chinese Chemical Letters 2020年第7期31卷 1709-1716页

作者： Lijun Shen Tianjiao Zhou Yatong Fan Xin Chang Yi Wang Jianguo Sun Lei Xing Hulin Jiang state key laboratory of Natural Medicines Department of PharmaceuticsChina Pharmaceutical UniversityNanjing 210009China Jiangsu key laboratory of druggability of Biopharmaceuticals China Pharmaceutical UniversityNanjing 210009China Jiangsu key laboratory of drug Screening China Pharmaceutical UniversityNanjing 210009China Jiangsu key laboratory of drug Discovery for Metabolic Diseases China Pharmaceutical UniversityNanjing 210009China key lab of drug Metabolism and Pharmacokinetics State Key Laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjing 210009China

Photodynamic therapy(PDT)is a promising alternative approach for effective cancer treatment,which can directly destroy local tumor cells due to the generation of cytotoxic singlet oxygen and reactive oxygen species(ROS)in the tumor ***,PDT-mediated cell death is also associated with anti-tumor immune *** r,immunosuppre s sion of tumor microe nvironment is able to limit the immune response induced by PDT,it is therefore necessary to combine with immunocheckpoint inhibitor and immunoadjuvant for synergistic treatment of ***,the recent advances of PDT,immunotherapy,and photodynamic immunotherapy are reviewed.

关键词： Cancer therapy Photodynamic therapy Immunotherapy Reactive oxygen species Singlet oxygen

A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer

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Acta Pharmaceutica Sinica B 2022年第11期12卷 4165-4179页

作者： Yan Li Ya Chu Guangjiang Shi Xiaobin Wang Wanli Ye Chun Shan Dajia Wang Di Zhang Wei He Jingwei Jiang Shuqian Ma Yuhong Han Zhili Zhao Shijia Du Zhen Chen Zhiyu Li Yong Yang Chen Wang Xi Xu Hongxi Wu Center for new drug Safety Evaluation and Research State Key Laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjing 211198China School of Life Science and Technology China Pharmaceutical UniversityNanjing 211198China School of Pharmacy China Pharmaceutical UniversityNanjing 211198China Jiangsu key lab of drug Screening China Pharmaceutical UniversityNanjing 211198China

Enzalutamide(ENZ) is a second-generation androgen receptor(AR) antagonist used for the treatment of castration-resistant prostate cancer(CRPC) and reportedly prolongs survival time within a year of starting therapy. However, CRPC patients can develop ENZ resistance(ENZR), mainly driven by abnormal reactivation of AR signaling, involving increased expression of the full-length AR(ARfl)or dominantly active androgen receptor splice variant 7(ARv7) and ARfl/ARv7 heterodimers. There is currently no efficient treatment for ENZR in CRPC. Herein, a small molecule LLU-206 was rationally designed based on the ENZ structure and exhibited potent inhibition of both ARfl and constitutively active ARv7 to inhibit PCa proliferation and suppress ENZR in CRPC. Mechanically, LLU-206 promoted ARfl/ARv7 protein degradation and decreased ARfl/ARv7 heterodimers through mouse double minute 2-mediated ubiquitination. Finally, LLU-206 exhibited favorable pharmacokinetic properties with poor permeability across the blood-brain barrier, leading to a lower prevalence of adverse effects, including seizure and neurotoxicity, than ENZ-based therapies. In a nutshell, our findings demonstrated that LLU-206 could effectively inhibit ARfl/ARv7-driven CRPC by dual-targeting of ARfl/ARv7 heterodimers and protein degradation, providing new insights for the design of new-generation AR inhibitors to overcome ARfl/ARv7-driven CRPC.

关键词： drug resistance Enzalutamide Castration-resistant prostate cancer Androgen receptorsplice variant7 Heterodimers Degradation

Enhanced production of shikimic acid using a multi-gene co-expression system in Escherichia coli

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Chinese Journal of Natural Medicines 2016年第4期14卷 286-293页

作者： LIU Xiang-Lei LIN Jun HU Hai-Feng ZHOU Bin ZHU Bao-Quan state key laboratory of new drug and pharmaceutical process Shanghai Institute of Pharmaceutical IndustryChina State Institute of Pharmaceutical IndustryShanghai 201203China

Shikimic acid(SA) is the key synthetic material for the chemical synthesis of Oseltamivir, which is prescribed as the front-line treatment for serious cases of influenza. Multi-gene expression vector can be used for expressing the plurality of the genes in one plasmid, so it is widely applied to increase the yield of metabolites. In the present study, on the basis of a shikimate kinase genetic defect strain Escherichia coli BL21(?aro L/aro K, DE3), the key enzyme genes aro G, aro B, tkt A and aro E of SA pathway were co-expressed and compared systematically by constructing a series of multi-gene expression vectors. The results showed that different gene co-expression combinations(two, three or four genes) or gene orders had different effects on the production of SA. SA production of the recombinant BL21-GBAE reached to 886.38 mg·L^(-1), which was 17-fold(P < 0.05) of the parent strain BL21(?aro L/aro K, DE3).

关键词： Shikimic acid Escherichia coli Multi-gene co-expression