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Science China Life Sciences 2025年第1期68卷 300-302页

作者： Ze-Min Lin Mai Xiang Wen-Hui Wei Shu-Hui Fan Li Chen Jie Wang Xiao-Qian yang chun-hao yang Shi-Jun He Jian-Ping Zuo Laboratory of Immunopharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy University of Chinese Academy of Sciences School of Pharmacy Nanjing University of Chinese Medicine State Key Laboratory of Drug Research Department of Medicinal ChemistryShanghai Institute of Materia MedicaChinese Academy of Sciences Innovation Research Institute of Traditional Chinese Medicine Shanghai University of Traditional Chinese Medicine Experiment Center for Science and Technology Shanghai University of Traditional Chinese Medicine

Dear Editor, Phenotypic drug discovery, which observes compound effects on physiology,has given way to targeting specific molecules, but has revived by using modern methods to find drugs based on therapeutic outcomes in disease models(Vincent et al., 2022). Osteoarthritis(OA) is a prevalent chronic joint disorder, primarily affecting knee joints, with osteoclast activation due to low-grade inflammation resulting in increased bone resorption and structural changes in the joint(Katz et al.,2021).

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Synthesis and Characterization of Thermoplastic Poly(Ester Amide)s Elastomer (TPEaE) Obtained from Recycled PET

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Journal of Renewable Materials 2021年第5期9卷 867-880页

作者： Zhi-Yu yang Yi-Ling Chou hao-chun yang Chin-Wen Chen Syang-Peng Rwei Institute of Organic and Polymeric Materials Research and Development Center of Smart Textile TechnologyNational Taipei University of TechnologyTaipei10608Taiwan

A series of thermoplastic polyester elastomer (TPEE) and thermoplastic poly(ester amide)s elastomer (TPEaE)copolymers were obtained by depolymerizing PET (polyethylene terephthalate) by which the waste PET canbe efficiently recovered and recycled into value-added products from a practical and economical point of *** structure of TPEE and TPEaE was identified using nuclear magnetic resonance (NMR) and Fourier transforminfrared spectroscopy (FT-IR). Differential scanning calorimetry (DSC) data showed that the melting temperature(Tm) decreased with the amide content increased. The glass transition temperature (Tg) was increased as introducingthe amide group, and the formation of amide-ester and amide-amide hydrogen bonds increased the intermolecularchain force. The intrinsic viscosity (η) showed the tendency of increment from TPEE (0.53 dL g^(−1)) to TPEaE-5%(0.72 dL g^(−1)) due to the reinforcement of hydrogen bond and chain entanglement.

关键词： Recycle polyethylene terephthalate(r-PET) depolymerization thermalplastic poly(ester amide)s copolymer(TPEaE)

Catechol-Bisphosphonate Conjugates: New Potential Chelating Agents for Metal Intoxication Therapy

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Chinese Chemical Letters 2004年第12期15卷 1403-1406页

作者： Guang Yu XU chun hao yang Bo LIU Xi Han WU Yu Yuan XIE State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Shanghai 201203 State Key Lab. of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biol. Sci. Shanghai 201203 China

In a quest for better chelating therapy drugs for the treatment of intoxication by Fe, Al, oractinides, two new series of mixed catechol-bisphosphonate through amide linkage were synthesized.Benzyl group was used as protecting group to avoid the breakage of amide by acid hydrolysis orimcomplete reaction in silylation-dealkylation using bromotrimethylsilane.

关键词： Bisphosphonates catechol chelating agents metal intoxication therapy.

Unbiased screening reveals that blocking exportin 1 overcomes resistance to PI3Kαinhibition in breast cancer

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Signal Transduction and Targeted Therapy 2019年第1期4卷 211-213页

作者： Xue-Ling Liu Bo-Bo Wang Yi Wang Yu-Xiang Wang chun-hao yang Cun Tan Xi Zhang Qiao-jun He Jian Ding Ling-Hua Meng Division of Anti-Tumor Pharmacology Shanghai Institute of Materia MedicaChinese Academy of Sciences501 Haike RoadShanghai201203China Zhejiang Province Key Laboratory for Drug Evaluation and Clinical Research First Affiliated HospitalSchool of MedicineZhejiang University79 Qingchun RoadHangzhou310003China Zhejiang Province Key Laboratory of Anti-Cancer Drug Research College of Pharmaceutical SciencesZhejiang University866 Yuhangtang RoadHangzhou310058China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing100049China Department of Medicinal Chemistry Shanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203China Division of Anti-Tumor Pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203China

Dear Editor,Targeting PI3K is a promising approach for cancer therapy,and the PI3Kα-selective inhibitor alpelisib has been approved for breast cancer treatment.1,2,3 However,the development of acquired resistance poses a significant clinical *** of PTEN and activation of mTOR,CDK4/6,or PIM have been reported to mediate acquired resistance to alpelisib.4,5,6,7 The mechanisms leading to resistance to PI3Kαinhibitors appear to be different under different circumstances,and the aforementioned strategies may be beneficial for a particular group of *** strategies to overcome acquired resistance in a broad spectrum of patients need to be discovered.

关键词： PI3K breast cancer

LUNX mRNA作为肺癌微转移检测分子标志物的可行性研究

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药物生物技术 2015年第4期22卷 328-331页

作者：郝春阳王坤宇辽宁省鞍山市中心医院老2科辽宁鞍山114000

探讨LUNX m RNA作为肺癌微转移检测分子标志物的可行性。临床纳入20例确诊为可以进行手术治疗的中早期非小细胞肺癌(Non-small cell lung carcinoma,NSCLC)患者,分别于术前、术后即刻以及术后1 w采集患者的外周血液,使用逆转录聚合酶链... 详细信息

探讨LUNX m RNA作为肺癌微转移检测分子标志物的可行性。临床纳入20例确诊为可以进行手术治疗的中早期非小细胞肺癌(Non-small cell lung carcinoma,NSCLC)患者,分别于术前、术后即刻以及术后1 w采集患者的外周血液,使用逆转录聚合酶链反应(RT-PCR)法检测肺癌特异性基因LUNX的表达。此外,研究纳入10例肺部良性疾病患者,亦进行肺癌特异性基因LUNX表达的RT-PCR检测。20例中早期非小细胞肺癌患者中,有9例患者的外周血中检测到LUNX m RNA的表达;10例肺部良性疾病患者的外周血中,均未检测到LUNX m RNA的表达。采用RT-PCR法进行外周血LUNX m RNA表达的检测,是目前较为理想的诊断中早期非小细胞肺癌患者是否发生微转移的方法。手术治疗中早期非小细胞肺癌患者,能够减低患者术后远处转移的发生。手术操作可能促进肿瘤细胞向外周血的脱落。

关键词： LUNX mRNA 非小细胞肺癌微转移实时PCR

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基于多特征提取的合成射流涡流控制机理研究

工程力学 2024年第11期41卷 225-237页

作者：郝春阳董祥瑞蔡天意周骛蔡小舒上海理工大学能源与动力工程学院上海200093 上海市动力工程多相流传热重点实验室上海200093

在横流的底部施加倾斜角为60?的合成射流,并采用大涡模拟(LES)对其周期性涡运动过程进行了数值模拟,研究不同激励参数条件下合成射流与横流相互作用涡环结构的产生机理及演变规律。该文首先利用第三代涡识别方法(Liutex矢量法)对流场中... 详细信息

在横流的底部施加倾斜角为60?的合成射流,并采用大涡模拟(LES)对其周期性涡运动过程进行了数值模拟,研究不同激励参数条件下合成射流与横流相互作用涡环结构的产生机理及演变规律。该文首先利用第三代涡识别方法(Liutex矢量法)对流场中涡环的演变过程进行了运动跟踪,并且定量统计合成射流在不同驱动频率(S_(t)=0.25,0.5,0.75,1)和驱动振幅(A_(0)=1,1.5,2,2.5)下涡旋结构的旋转强度和涡核尺度。此外,采用本征正交分解法(proper orthogonal decomposition,POD)方法和动态模态分解(dynamic mode decomposition,DMD)对合成射流特定频率(S_(t)=0.25)及振幅(A_(0)=2.5)下流场速度场进行模态分解,提取影响流场的主特征模态。结果表明:振幅对旋转强度和涡核尺寸大小有正贡献,而频率对旋转强度和涡核尺寸大小有负贡献;合成射流在横流中的涡运动机理可以概括为,在低频低振幅条件下有利于顺时针涡结构的产生,而在高频高振幅条件下有利于逆时针涡结构的产生;基于各阶POD模态的空间结构及频谱特征等特性,流场主特征结构为脱落涡,脱落频率与射流驱动频率一致(S_(t)=0.25)。初级顺时针涡旋结构为涡流控制的主导结构,而每阶模态均为多频耦合;通过DMD对流场信息进行时空解耦,得到了剪切诱导、涡合并等动力特征。多种特征提取方法的结合更有助于合成射流涡流控制机理的深入研究。

关键词：流体力学流动控制特征提取方法横流合成射流 Liutex矢量涡脱落主频率

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舒利迭治疗慢性阻塞性肺疾病临床疗效观察

实用医技杂志 2007年第17期14卷 2279-2280页

作者：郝春阳鞍山市中心医院辽宁鞍山114000

目的:观察舒利迭治疗慢性阻塞性肺疾病(COPD)的疗效。方法:我院呼吸科就诊的COPD患者120例,随机分为治疗组和对照组。对照组给予常规治疗,治疗组在此基础上给予吸入舒利迭。结果:治疗组的总有效率显著高于对照组,两组疗效比较差异有显... 详细信息

目的:观察舒利迭治疗慢性阻塞性肺疾病(COPD)的疗效。方法:我院呼吸科就诊的COPD患者120例,随机分为治疗组和对照组。对照组给予常规治疗,治疗组在此基础上给予吸入舒利迭。结果:治疗组的总有效率显著高于对照组,两组疗效比较差异有显著性意义(P<0.01);治疗组的氧分压(PaO2)治疗后显著高于对照组(P<0.05);二氧化碳分压(PaCO2)则显著低于对照组(P<0.05);治疗组的FEV1、FVC治疗后显著高于对照组(P<0.05)。舒利迭无明显的毒副作用。结论:应用舒利迭治疗COPD在临床上能显著改善动脉血气指标,使用安全,值得在临床上推广。

关键词：舒利迭慢性阻塞性肺疾病疗效

灯盏花注射液对慢性阻塞性肺疾病急性加重期肺动脉高压的疗效观察

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实用医技杂志 2007年第15期14卷 1974-1975页

作者：郝春阳鞍山市中心医院辽宁鞍山114000

目的:探讨灯盏花注射液对慢性阻塞性肺疾病(COPD)急性加重期肺动脉高压的疗效。方法:COPD急性加重期患者共100例,分为试验组48例和对照组52例,对照组采用常规综合治疗,试验组除常规综合治疗外,加用灯盏花注射液50mg溶于生理盐水250ml中... 详细信息

目的:探讨灯盏花注射液对慢性阻塞性肺疾病(COPD)急性加重期肺动脉高压的疗效。方法:COPD急性加重期患者共100例,分为试验组48例和对照组52例,对照组采用常规综合治疗,试验组除常规综合治疗外,加用灯盏花注射液50mg溶于生理盐水250ml中静脉滴注,1次/d,共7d。结果:试验组肺动脉收缩压治疗后显著低于治疗前(P<0.05),也显著低干对照组(P<0.05);试验组肺功能指标(FEV1,FEV1/FVC)较用药前显著增加,但与对照组比较无明显差异;试验组血浆D-二聚体含量显著低于用药前,也显著低于对照组(P<0.05);两组动脉血气指标中的PO2和PCO2在治疗后较治疗前有所改善,差异有高度显著性(试验组,P<0.01;对照组,P<0.05)。两组均无明显不良反应。结论:灯盏花注射液治疗COPD急性加重期肺动脉高压疗效好,对患者预后可能产生积极影响。

关键词：灯盏花注射液慢性阻塞性肺疾病肺动脉高压

Deciphering fungal metabolon coupling tandem inverse-electrondemand Diels-Alder reaction and semipinacol rearrangement for the biosynthesis of spiro polycyclic alkaloids

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Science China Chemistry 2025年第1期68卷 288-296页

作者： Shuai Liu Wen-Qiang Xu Ying-Tong Di Man-Cheng Tang Ding-Kang Chen Ming-Ming Cao Yao-Wen Chang Hong-Yu Tang chun-Mao Yuan Jun-Bo yang Zhi-Li Zuo Han Guo Zi-Fei Xu Ying Zeng Yun-Dong Wu Xiao-Jiang hao Key Laboratory of Phytochemistry and Natural Medicines (Chinese Academy of Sciences) Kunming Institute of Botany Chinese Academy of Sciences University of Chinese Academy of Sciences Lab of Computational Chemistry and Drug Design State Key Laboratory of Chemical Oncogenomics Peking University Shenzhen Graduate School Shenzhen Bay Laboratory State Key Laboratory of Microbial Metabolism School of Life Sciences & Biotechnology Shanghai Jiao Tong University State Key Laboratory of Functions and Applications of Medicinal Plants Guizhou Medical University Molecular Biology Experimental Center Germplasm Bank of Wild Species in Southwest China Kunming Institute of Botany Chinese Academy of Sciences Yunnan Key Laboratory for Wild Plant Resources Kunming Institute of Botany Chinese Academy of Sciences Research Unit of Chemical Biology of Natural Anti-Virus Products Chinese Academy of Medical Sciences

In the intricate process of natural product biosynthesis, a metabolon can enhance metabolic flux by associating sequential enzymes. A fungal metabolon, comprising of flavin-dependent monooxygenase Spe F and P450 monooxygenase Spe G, is identified in the biosynthesis of spiro polycyclic alkaloids(+)-notoamide B and its diastereomer(+)-versicolamide B. Using notoamide E as a substance, Spe F/Spe G metabolon can control the stereoselectivity of its 2,3-epoxidation, followed by hydrogen atom ion at C-17 to generate reactive epoxide tau-m A with dienyl iminium unit. Subsequently,(+)-notoamide B and(+)-versicolamide B are produced via tandem nonenzymatic inverse-electron-demand Diels-Alder reaction and semipinacol rearrangement. This provides the first example of metabolon in the biosynthesis of spiro-prenylated indole alkaloids.

关键词： metabolon Diels-Alder reaction semipinacol rearrangement biosynthesis notoamides spiro polycyclic alkaloids

Chiral phosphoramidite ligand-modulated palladium auto-tandem catalysis for asymmetric dehydrogenative dienylation of imines with α-alkenes

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Science China Chemistry 2025年

作者： Zhong-Sheng Nong hao-Fan Qian Ying-chun Chen Pu-Sheng Wang Liu-Zhu Gong Hefei National Research Center for Physical Sciences at the Microscale and Department of Chemistry University of Science and Technology of China Key Laboratory of Drug Targeting and Drug Delivery System (Sichuan University) Ministry of Education and Sichuan Research Center for Drug Precision Industrial Technology West China School of Pharmacy Sichuan University School of Materials and Chemistry Southwest University of Science and Technology

The development of efficient processes allowing rapid access to complex chiral molecules from easily available alkenes is a long-term pursuit in the synthetic chemistry community. Transition metal-catalyzed asymmetric functionalization of allylic C–H bond represents a unique alternative toward this goal. However, enantioselective dehydrogenative transformation of olefins to value-added optically enriched molecules remains yet to be discovered. Here, we report a highly enantioselective dehydrogenative dienylation of imines with unactivated α-alkenes driven by the synergistic action of palladium complex and carboxylic acid. Chiral phosphoramidite ligands turned out to be superior in modulating the performance of palladium autotandem catalysis and allowed a broad range of α-alkenes and imines to be transformed into chiral dienylamines. Mechanistic studies suggest that the dienes could be in situ generated from α-alkenes through a palladium(0)-mediated dehydrogenative process in the presence of excess benzoquinone oxidants, and then participated in the Pd-chiral phosphoramidite-catalyzed intermolecular vinylogous-type addition to the imines activated by the carboxylic acid co-catalyst. Notably, the second β-H elimination occurring in the dienylation event might be the turnover-limiting step.

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