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Journal of Analysis and Testing 2024年第2期8卷 237-244页

作者： Fei Yu Yue Wang Caiyuan Yu Wei Zhang Xuefeng Bai state key laboratory of quality research in chinese medicines Macao Institute for Applied Research in Medicine and HealthMacao University of Science and TechnologyTaipaMacao999078China Baotou Cancer Hospital Baotou014040Inner MongoliaChina

miR-18a has been identified as a significantly expressed microRNA(miRNA)in non-small cell lung cancer(NSCLC)and plays a vital role in cancer cell transformation,metastasis,and ***,a pair of binary probes from numerous probe pairs based on single nucleotide polymorphism analyses of miR-18a and miR-18b was first designed and screened to develop a Y-shaped ratio biosensor for accurate detection of serum miR-18a in *** special structure of the binary probes combined with the hairpin showed strong specificity for miR-18a,which was confirmed by polyacrylamide gel electrophoresis assay and square wave voltammetry ***,it is beneficial to immobilize single-stranded DNA(ssDNA)probes due to the large specific surface area of nanoporous gold,thereby improving the sensitivity of the *** Y-shaped ratio biosensor exhibited a wide detection range and can quantify the concentration of miR-18a in the range of 10 fmol/L–100 pmol/L,with a limit of detection of 0.211 fmol/L(S/N=3).Moreover,it exhibits excellent detection capabilities in serum samples since the biosensor showed a high selectivity toward the coexistence of miR-18a and ***,the prepared Y-shaped ratio biosensor is a highly sensitive and specific miR-18a detection tool,capable of identifying microscopic amounts of miR-18a in serum samples,providing great potential for early screening of NSCLC.

关键词： Nanoporous gold Y-shaped biosensor miR-18a NSCLC

Feasible Synthesis of N,O-Bidentate Difluoroboron Chromophores through Direct Functionalization of Quinoxalin-2(1H)-ones with Ketones in One Shot

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chinese Journal of Chemistry 2024年第13期42卷 1481-1486页

作者： Shuaichen Zhang Jing Zhang Xiang Ling Yifan Zhao Yue Ma Peng Sun state key laboratory for quality Ensurance and Sustainable Use of Dao-di Herbs Artemisinin Research Center and Institute of Chinese Materia MedicaChina Academy of Chinese Medical SciencesBeijing 100700China Department of Pharmaceutics School of PharmacyChina Pharmaceutical UniversityState Key Laboratory of Natural MedicinesNanjingJiangsu 210009China

Organic difluoroboron complexes are a kind of potential platforms for a wide range of applications owing to their excellent photophysical ***,we have explored a simple and direct synthesis methodology for a library of N,O-bidentate difluoroboron complexes from quinoxalin-2(1H)-ones and ketones in one *** photophysical properties of the generated complexes were evaluated and the application potential of these compounds on subcellular imaging was also explored.

关键词： N,O-Bidentate difluoroboron Chromophores Quinoxalin-2(1H)-ones Ketones/Green chemistry Synthetic method C-CcouplingI Boron

Chemical derivatization strategies for enhancing the HPLC analytical performance of natural active triterpenoids

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Journal of Pharmaceutical Analysis 2024年第3期14卷 295-307页

作者： Xiao-Feng Huang Ying Xue Li Yong Tian-Tian Wang Pei Luo Lin-Sen Qing Chengdu Institute of Biology Chinese Academy of SciencesChengdu610041China state key laboratory for quality research in chinese medicines Macao University of Science and TechnologyMacaoChina Sichuan Center for Disease Control and Prevention Chengdu610041China University of chinese Academy of Sciences Beijing100049China

Triterpenoids widely exist in nature,displaying a variety of pharmacological *** triterpenoids in different matrices,especially in biological samples holds great ***-performance liquid chromatography(HPLC)has become the predominant method for triterpenoids analysis due to its exceptional analytical ***,due to the structural similarities among botanical samples,achieving effective separation of each triterpenoid proves challenging,necessitating significant improvements in analytical ***,triterpenoids are characterized by a lack of ultraviolet(UV)absorption groups and chromophores,along with low ionization efficiency in mass ***,routine HPLC analysis suffers from poor *** derivatization emerges as an indispensable technique in HPLC analysis to enhance its *** the structural characteristics of triterpenoids,various derivatization reagents such as acid chlorides,rhodamines,isocyanates,sulfonic esters,and amines have been employed for the derivatization analysis of *** review comprehensively summarized the research progress made in derivatization strategies for HPLC detection of ***,the limitations and challenges encountered in previous studies are discussed,and future research directions are proposed to develop more effective derivatization methods.

关键词： Triterpenoid HPLC Derivatization Quantification

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

MicroRNAs modulation in lung cancer: exploring dual mechanisms and clinical prospects

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BIOCELL 2024年第3期48卷 403-413页

作者： SHAHID HUSSAIN HABIB BOKHARI XINGXING FAN SHAUKAT IQBAL MALIK SUNDAS IJAZ MUHAMMAD ADNAN SHEREEN AIMAN FATIMA Department of Biotechnology Kohsar University MurreeMurreePakistan Macao University of Science and Technology state key laboratory of quality research in chinese medicines TaipaMacao Department of Bioinformatics and Biosciences Capital University of Science and TechnologyIslamabadPakistan Department of Microbiology Kohsar University MurreeMurreePakistan

The global incidence of lung cancer is marked by a considerably elevated mortality ***(miRNAs)exert pivotal inﬂuence in the intricate orchestration of gene regulation,and their dysregulation can precipitate dire consequences,notably *** this context,miRNAs encapsulated in exosomes manifest a diversiﬁed impact on the landscape of lung cancer,wherein their actions may either foster angiogenesis,cell proliferation,and metastasis,or counteract these *** comprehensive review article discerns potential targets for the prospective development of therapeutic agents tailored for lung ***-suppressive miRNAs,such as miR-204,miR-192,miR-30a,miR-34a,miR-34b,miR-203,and miR-212,exhibit heightened expression and demonstrate the capacity to inhibit cellular proliferation and ***,the deleterious effects of tumor-promoting miRNAs like miR-21,miR-106a,miR-155,miR-205,and miR-210 can be attenuated through the application of their respective *** miRNAs selectively target various oncogenes,including NUAK Family Kinase 1(NUAK1),Snail Family Transcriptional Repressor 1(Snai1),Astrocyte elevated gene-1(AEG-1),Vimentin,Proliferation and apoptosis adaptor protein 15(PEA-15/PED),Hypoxia-inducible factor 1-alpha(HIF1),as well as tumor suppressor genes such as phosphatase and tensin homolog(PTEN),Suppressor of cytokine signaling 1(SOCS1),Tumor protein P53 binding protein 1(TP53BP1),and PH Domain and Leucine Rich Repeat Protein Phosphatase 2(PHLP22).This investigative approach proves invaluable in elucidating the speciﬁc miRNAs implicated in the deregulation of crucial genes pivotal to the pathogenesis of cancer.

关键词： miRNAs Oncogenes Tumor suppressive genes Lung cancer therapy

Formulation,characterization and in vivo and in vitro evaluation of aloe-emodin-loaded solid dispersions for dissolution enhancement

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Journal of Traditional chinese Medicine 2024年第1期44卷 54-62页

作者： LI Xiuyan LUO Yuting WANG Jinhui DU Zhimin key laboratory of Basic and Application research of Beiyao Heilongjiang University of Chinese MedicineMinistry of EducationHarbin 150040China College of Pharmacy Harbin Medical UniversityHarbin 150081China Institute of Clinical Pharmacology the Second Affliated Hospital of Harbin Medical University(University Key aboratory of Drug ResearchHeilongjiang Province)Harbin 150086China Department of Clinical Pharmacology College of Pharmacy Harbin Medical UniversityHarbin 150081China state key laboratory of quality research in chinese medicines Macao University of Science and TechnologyMacao 999078China

OBJECTIVE:To prepare aloe-emodin solid dispersion(AE-SD)and determine the metabolic process of AE and AE-SD in ***:AE-SD was prepared via solvent evaporation or solvent melting using PEG-6000 and PVP-K30 as *** analysis,X-ray diffraction spectroscopy,differential scanning calorimetry,Fourier transform infrared spectroscopy and scanning electron microscopy were used to identify the physical state of *** prescriptions were screened via the dissolution degree determination *** Phoenix software,AE suspension and AE-SD were subjected to a pharmacokinetic comparison study analyzing the alteration of behavior in vivo after AE was prepared as a solid *** toxicity was assessed in mice,and the physiological toxicity was used as the determination criterion for ***:AE-SD showed that AE existed in the carrier in an amorphous *** with polyethylene glycol,polyvinylpyrrolidone(PVP)inhibited AE crystallization,causing the drug to transform from a dense crystalline state to an amorphous form and increasing the degree of drug ***,it was more suitable as a carrier material for *** addition of poloxamer(POL)was more beneficial to the stability of solid dispersions and could reduce the amount of *** dissolution test confirmed that the optimal ratio of AE to the composite vector AE-PVP-POL was 1:2:2,and its dissolution effect was also *** on the pharmacokinetic comparison,the drug absorption was faster and quickly reached the peak of blood drug concentration in AE-SD compared to AE,the Cmax of AE-SD was greater than that of AE,and t1/2 and mean residence time of AE-SD were less than *** results showed that the drug metabolism in AE-SD was better,and the residence time was *** toxicology study showed that both AE and AE-SD had no ***:This paper established that the solubility of the drug could be increased after preparing a solid dispersion,

关键词： aloe-emodin solid dispersion solvent evaporation drug liberation pharmacokinetics

Mogroside IIE,an in vivo metabolite of sweet agent,alleviates acute lung injury via Pla2g2a-EGFR inhibition

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Food Science and Human Wellness 2024年第1期13卷 299-312页

作者： Weichao Lü Guoqing Ren Kuniyoshi Shimizu Renshi Li Chaofeng Zhang state key laboratory of Natural medicines School of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing 211198China Sino-Jan Joint lab of Natural Health Products research School of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing 211198China Faculty of Agriculture Kyushu UniversityFukuoka 819-0395Japan

In the face of increasingly serious environmental pollution,the health of human lung tissues is also facing serious *** IIE(M2E)is the main metabolite of sweetening agents mogrosides from the anti-tussive chinese herbal Siraitia *** study elucidated the anti-inflammatory action and molecular mechanism of M2E against acute lung injury(ALI).A lipopolysaccharide(LPS)-induced ALI model was established in mice and MH-S cells were employed to explore the protective mechanism of M2E through the western blotting,co-immunoprecipitation,and quantitative real time-PCR *** results indicated that M2E alleviated LPS-induced lung injury through restraining the activation of secreted phospholipase A2 type IIA(Pla2g2a)-epidermal growth factor receptor(EGFR).The interaction of Pla2g2a and EGFR was identified by *** addition,M2E protected ALI induced with LPS against inflammatory and damage which were significantly dependent upon the downregulation of AKT and m TOR via the inhibition of ***2g2a may represent a potential target for M2E in the improvement of LPS-induced lung injury,which may represent a promising strategy to treat ALI.

关键词： Mogroside IIE Acute lung injury Secreted phospholipase A2 type IIA(Pla2g2a) Epidermal growth factor receptor(EGFR)

Citrinsorbicillin A,a novel homotrimeric sorbicillinoid isolated by LC-MS-guided with cytotoxic activity from the fungus Trichoderma citrinoviride HT-9

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chinese Chemical Letters 2024年第8期35卷 299-303页

作者： Guo-Ping Yin Ya-Juan Li Li Zhang Ling-Gao Zeng Xue-Mei Liu Chang-Hua Hu Engineering research Center of Coptis Development and Utilization(Ministry of Education) College of Pharmaceutical Sciences and Chinese MedicineSouthwest UniversityChongqing 400715China state key laboratory of Natural medicines China Pharmaceutical UniversityNanjing 211198China NMPA key laboratory for quality Monitoring of Narcotic Drugs and Psychotropic Substances Chongqing Institute for Food and Drug ControlChongqing 401121China

Citrinsorbicillin A(1),a novel homotrimeric sorbicillinoid,along with two new monomers citrinsor-bicillins B(2)and C(3),were isolated from the Coptis chinensis endophyte Trichoderma citrinoviride HT-9 by liquid chromatograph mass spectrometer(LC-MS)-guided strategy.1 was the first trimeric-example from terrestrial fungi,which possessed a unique carbon skeleton with two bicyclo[2.2.2]octanedione ring connected through an enolated carbon forming by[4+2]*** structures were elucidated by spectroscopic analysis and X-ray diffraction.1 exhibited moderate cytotoxicity against human colon cancer HT29 cells,and it induced significant cell cycle arrest by reducing the protein expression of cyclin D1.

关键词： Citrinsorbicillin A Trimeric sorbicillinoid Coptis chinensis endophyte Trichoderma citrinoviride [4+2]Cycloaddition Cytotoxic activity

Rapid Simultaneous Determination of Four Ganoderic Acids in Ganoderma(chinese Name:Lingzhi)by Direct Infusion-Multiple Reaction Monitoring Cubed

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Journal of Analysis and Testing 2024年第1期8卷 52-62页

作者： Nian Wu Bo Peng Ting Li Pengfei Tu Shengpeng Wang Bo Li Wenjing Liu Yuelin Song Modern research Center for Traditional chinese Medicine Beijing Research Institute of Chinese MedicineBeijing University of Chinese MedicineBeijing 100029China Amway(China)Botanical research Center Wuxi 214011China state key laboratory of quality research in chinese Medicine Institute of Chinese Medical SciencesUniversity of MacaoTaipa 999078China Amway(Shanghai)Innovation&Science Co. LtdShanghai 201508China School of Pharmacy Henan University of Chinese MedicineZhengzhou 450046China

Attributing to the rapid demand expansion for the edible medicinal materials in the market,the limited throughput of highperformance liquid chromatography-multiple reaction monitoring(HPLC-MRM)cannot fully address the measurement workload for a huge number of testing ***,it is urgent to pursue more efficient approaches for the quality *** of the greater selectivity of MRM cubed(MRM^(3))over MRM,there might be a chance to omit the time-intensive LC *** current study,we attempted to develop a direct infusion(DI)-MRM^(3) program,and the applicability was thereafter assessed through simultaneous determination of four ganoderic acids(GAs)in one of the most famous tonic herbal medicines namely Ganoderma(chinese name:Lingzhi).Primary parameters such as Q1>Q3>QLIT ion transitions,collision energy(CE),and excitation energy were optimized by programming online energy-resolved mass spectrometry with authentic compounds.A single DI-MRM measurement merely costed four minutes,and in spite of the wide occurrences of isomers,satisfactory selectivity was *** validation assays demonstrated the method to be sensitive,precise,accurate,and *** quantitative results from DI-MRM^(3) were also justified by conducting LC-MRM measurements in *** differences occurred for the content patterns between the two original sources namely Ganoderma lucidum and ***,and,moreover,either cultivar or harvest time showed dramatical influence on the quantitative features of the four targeted *** importantly,DI-MRM3 is a meaningful analytical option for rapid quantitative analysis of herbal medicines,because of the comparable reliability,nonetheless,less consumptions of both measurement time and solvent,compared with LC-MRM.

关键词： Direct infusion Multiple reaction monitoring cubed High-throughput quantitative analysis Ganoderic acids Ganoderma

Concise Synthesis of Lactococcus garvieae Lipoteichoic Acids Through an Additive-Modulated Preactivation Protocol and the Immunological Studies

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CCS Chemistry 2024年第2期6卷 403-414页

作者： Tianlu Li Tong Li Yue Yang Haoru Zhuang Jianwu Lv Ning Zhou Miaomiao Zhang Fengshan Wang Yiqun Geng Richard R.Schmidt Peng Peng National Glycoengineering research Center Shandong Key Laboratory of Carbohydrate Chemistry and GlycobiologyNMPA Key Laboratory for Quality Research and Evaluation of Carbohydrate Based MedicineShandong UniversityQingdao 266237 state key laboratory of Bioactive Substance and Function of Natural medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050 Department of Chemistry University of KonstanzD-78457 Konstanz

Lipoteichoic acids(LTAs)are macroamphiphiles composed of alditol,lipid,phosphate,and carbohydrate *** to their inherent complexity,it is a severe challenge to access LTAs with structural integrity from natural sources for biological or immunological ***,we describe the first total synthesis of Lactococcus garvieae LTA(type II LTA),containing five distinct 1,2-cis gluco/galactopyranosidic linkages,via a novel additive-modulated O-glycosyl trichloroacetimidate preactivation glycosidation *** strategy features(1)high glycosidation yields and excellent 1,2-cis stereoselectivities independent of the donor anomeric configuration,(2)common and inexpensive reagents as promoters and additives,(3)application to standard glycosyl imidate donors without resorting to participating protection,and(4)general application to reactive and less reactive glycosyl ***,via the precise stereocontrolled construction of three galactopyranosidic and two glucopyranosidic bonds on a multigram scale,a series of structurally well-defined LTA molecules were successfully *** evaluation of these type II synthetic LTAs showed a structure–activity relationship in the stimulation of a proinflammatory response.

关键词： 1,2-cis glycosidation stereoselectivity lipoteichoic acid total synthesis additive-modulated trichloroacetimidate glycosidation immune response