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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)

Novel Pt(IV) complex OAP2 induces STING activation and pyroptosis via mitochondrial membrane remodeling for synergistic chemo-immunotherapy

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Acta Pharmaceutica Sinica B 2024年第4期14卷 1742-1758页

作者： Renming Fan Ruizhuo Lin Shuo Zhang Aohua Deng Yongrui Hai Junyan Zhuang Yang Liu Maosheng Cheng Gaofei Wei Institute of Medical Research Northwestern Polytechnical UniversityXi'an 710072China Research&Development Institute of Northwestern Polytechnical university in Shenzhen Shenzhen 518057China Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationSchool of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Mitochondrial membrane remodeling can trigger the release of mitochondrial DNA (mtDNA), leading to the activation of cellular oxidative stress and immune responses. While the role of mitochondrial membrane remodeling in promoting inflammation in hepatocytes is well-established, its effects on tumors have remained unclear. In this study, we designed a novel Pt(IV) complex, OAP2, which is composed of oxaliplatin (Oxa) and acetaminophen (APAP), to enhance its anti-tumor effects and amplify the immune response. Our findings demonstrate that OAP2 induces nuclear DNA damage, resulting in the production of nuclear DNA. Additionally, OAP2 downregulates the expression of mitochondrial Sam50, to promote mitochondrial membrane remodeling and trigger mtDNA secretion, leading to double-stranded DNA accumulation and ultimately synergistically activating the intracellular cGAS-STING pathway. The mitochondrial membrane remodeling induced by OAP2 overcomes the limitations of Oxa in activating the STING pathway and simultaneously promotes gasdermin-D-mediated cell pyroptosis. OAP2 also promotes dendritic cell maturation and enhances the quantity and efficacy of cytotoxic T cells, thereby inhibiting cancer cell proliferation and metastasis. Briefly, our study introduces the first novel small-molecule inhibitor that regulates mitochondrial membrane remodeling for active immunotherapy in anti-tumor research, which may provide a creative idea for targeting organelle in anti-tumor therapy.

关键词： Anti-tumor drug Prodrug Platinum Chemo-immunotherapy Mitochondrial membrane modeling STING Pyroptosis mtDNA

UV,five wavelengths fusion and electrochemical fingerprints combined with antioxidant activity for quality control of antiviral mixture

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Asian Journal of Traditional Medicines 2024年第3期19卷 119-136,151页

作者： Kaining Zhou Zini Tang Guoxiang Sun Ping Guo Lili Lan College of pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

Aiming to ensure the consistency of quality control of Traditional Chinese Medicines(TCMs),a combination method of high-performance liquid chromatography(HPLC),ultraviolet(UV),electrochemical(EC)was developed in this study to comprehensively evaluate the quality of Antiviral Mixture(AM),and Comprehensive Linear Quantification Fingerprint Method(CLQFM)was used to process the *** analysis of three active substances in TCM was conducted.A fivewavelength fusion fingerprint(FWFF)was developed,using second-order derivatives of UV spectral data to differentiate sample levels *** combination of HPLC and UV spectrophotometry,along with electrochemical fingerprinting(ECFP),successfully evaluated total active ***,a multidimensional profiling analytical system for TCM was developed.

关键词： TCM antiviral mixture five-wavelength fusion fingerprint(FWFF) Comprehensive Linear Quantification Fingerprint Method(CLQFM) quantization fingerprint antioxidant activity profilling

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

2-APQC,a small-molecule activator of Sirtuin-3(SIRT3),alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis

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Signal Transduction and Targeted Therapy 2024年第6期9卷 2748-2764页

作者： Fu Peng Minru Liao Wenke Jin Wei Liu Zixiang Li Zhichao Fan Ling Zou Siwei Chen Lingjuan Zhu Qian Zhao Gu Zhan Liang Ouyang Cheng Peng Bo Han Jin Zhang Leilei Fu West China school of pharmacy and Department of Biotherapy Cancer Center and State Key Laboratory of BiotherapyWest China HospitalSichuan UniversityChengdu 610041China Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs School of Life Science and EngineeringSouthwest Jiaotong UniversityChengdu 610031China State Key Laboratory of Southwestern Chinese Medicine Resources Hospital of Chengdu University of Traditional Chinese MedicineSchool of PharmacyChengdu University of Traditional Chinese MedicineChengdu 611137China school of pharmaceutical Sciences Health Science CenterShenzhen UniversityShenzhen 518060China school of Traditional Chinese Materia Medica Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China

Sirtuin 3(SIRT3)is well known as a conserved nicotinamide adenine dinucleotide^(+)(NAD^(+))-dependent deacetylase located in the mitochondria that may regulate oxidative stress,catabolism and ATP *** evidence has recently revealed that SIRT3 plays its critical roles in cardiac fibrosis,myocardial fibrosis and even heart failure(HF),through its deacetylation ***,discovery of SIRT3 activators and elucidating their underlying mechanisms of HF should be urgently ***,we identified a new small-molecule activator of SIRT3(named 2-APQC)by the structure-based drug designing strategy.2-APQC was shown to alleviate isoproterenol(ISO)-induced cardiac hypertrophy and myocardial fibrosis in vitro and in vivo rat ***,in SIRT3 knockout mice,2-APQC could not relieve HF,suggesting that 2-APQC is dependent on SIRT3 for its protective ***,2-APQC was found to inhibit the mammalian target of rapamycin(mTOR)-p70 ribosomal protein S6 kinase(p70S6K),c-jun N-terminal kinase(JNK)and transforming growth factor-β(TGF-β)/small mother against decapentaplegic 3(Smad3)pathways to improve ISO-induced cardiac hypertrophy and myocardial *** upon RNA-seq analyses,we demonstrated that SIRT3-pyrroline-5-carboxylate reductase 1(PYCR1)axis was closely assoiated with *** activating PYCR1,2-APQC was shown to enhance mitochondrial proline metabolism,inhibited reactive oxygen species(ROS)-p38 mitogen activated protein kinase(p38MAPK)pathway and thereby protecting against ISO-induced mitochondrialoxidative ***,activation of SIRT3 by 2-APQC could facilitate AMP-activated protein kinase(AMPK)-Parkin axis to inhibit ISO-induced ***,our results demonstrate that 2-APQC is a targeted SIRT3 activator that alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis,which may provide a new clue on exploiting a promising drug candidate for the future HF therapeutics.

关键词： SIRT3 homeostasis metabolism

Reversibly size-switchable polyion complex micelles for antiangiogenic cancer therapy

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Chinese Chemical Letters 2024年第7期35卷 377-382页

作者： Mengjuan Sun Muye Zhou Yifang Xiao Hailei Tang Jinhua Chen Ruitao Zhang Chunjiayu Li Qi Ya Qian Chen Jiasheng Tu Qiyue Wang Chunmeng Sun NMPA Key Laboratory for Research and Evaluation of pharmaceutical Preparations and Excipients China Pharmaceutical UniversityNanjing 210009China State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 211198China Department of Pharmaceutics School of PharmacyChina Pharmaceutical UniversityNanjing 211198China Jiangsu Provincial Key Laboratory of Drug Metabolism and Pharmacokinetics China Pharmaceutical UniversityNanjing 210009China school of pharmaceutical Science Nanjing Tech UniversityNanjing 211816China

Size is one of the most important characteristics of nanoparticles to influence their biodistribution and antitumoral *** with large sizes have difficulty in deep tumor penetration,while small particles are easily removed from tumor tissues due to the high tumor interstitial fluid *** address these issues,an intelligent core-crosslinked polyion complex micelle(cPCM)with a reversibly sizeswitchable feature was engineered in this *** micelles are consisting of methoxy poly(ethylene glycol)-poly(D,L-lactide)copolymer(mPEG-PLA),mPEG-PLA-(HE)6CC,and mPEG-PLA-(RG)6CC at an optimal mass ratio of 6:1:1 with an antiangiogenic compound,dabigatran etexilate(DE),*** net charge inside the micelles is switchable when exposed to different pH conditions,thereby leading to revisable size-change of ***-loaded micelles(DE@cPCM)can swell and release drugs at the tumor sites with a mildly acidic pH,while they shrink and protect the cargo from leaking into the blood circulation with a neutral *** indicated that DE@cPCM can inhibit tumor angiogenesis in vitro and in vivo,thereby efficiently restraining tumor growth in a 4T1-bearing mouse ***,the sizeswitchable cPCM is a promising nanoplatform for targeting delivery of anticarcinogens into the matrix of tumor tissues.

关键词： Polyion complex micelle Size-switchable Revisable size-change pH response Antiangiogenic cancer

Tumor-targeted metabolic inhibitor prodrug labelled with cyanine dyes enhances immunoprevention of lung cancer

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Acta Pharmaceutica Sinica B 2024年第2期14卷 751-764页

作者： Wen Li Jiali Huang Chen Shen Weiye Jiang Xi Yang Jingxuan Huang Yueqing Gu Zhiyu Li Yi Ma Jinlei Bian State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009China Department of Biomedical Engineering School of EngineeringChina Pharmaceutical UniversityNanjing 210009China Jiangsu Key Laboratory of Drug Design and Optimization Department of Medicinal ChemistrySchool of PharmacyChina Pharmaceutical UniversityNanjing 210009China

Recent progress in targeted metabolic therapy of cancer has been limited by the considerable toxicity associated with such *** address this challenge,we developed a smart theranostic prodrug system that combines a fluorophore and an anticancer drug,specifically 6-diazo-5-oxo-L-norleucine(DON),using a thioketal linkage(TK).This system enables imaging,chemotherapy,photodynamic therapy,and on-demand drug release upon radiation *** optimized prodrug,DON-TK-BM3,incorporating cyanine dyes as the fluorophore,displayed potent reactive oxygen species release and efficient tumor cell *** the parent drug DON,DON-TK-BM3 exhibited no toxicity toward normal ***,DON-TK-BM3 demonstrated high tumor accumulation and reduced side effects,including gastrointestinal toxicity,in *** study provides a practical strategy for designing prodrugs of metabolic inhibitors with significant toxicity stemming from their lack of tissue selectivity.

关键词： Smart prodrug system Glutamineantagonists Immunotherapy Photodynamictherapy Reactive oxygen species Metabolicinhibitor Cyaninedye Non-small-cell lung cancer(NSCLC)

Base-controlled NHC-Ru-catalyzed transfer hydrogenation andα-methylation/transfer hydrogenation of ketones using methanol

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Chinese Chemical Letters 2024年第7期35卷 276-280页

作者： Ming Huang Xiuju Cai Yan Liu Zhuofeng Ke school of pharmacy School of clinical pharmacyGuangdong Pharmaceutical UniversityGuangzhou 510006China school of Materials Science&Engineering PCFM LabSchool of ChemistrySun Yat-sen UniversityGuangzhou 510275China school of Chemical Engineering and Light Industry Guangdong University of TechnologyGuangzhou 510006China

Herein,we report the NHC-Ru catalyst system that realizes the chemo-selective transformation of ketones with *** simply changing the base,a broad range of structurally diverse ketones,could be selectively and efficiently converted to the correspondingβ-methylated secondary alcohols or secondary ***,this catalytic system was very effective for the synthesis of bio-related molecules and deuterated alcohols,as well as the three-component coupling between methyl ketones,primary alcohols,and *** reaction mechanism was further revealed by experiment and DFT mechanistic investigations.

关键词： Ru complexes Methanol Ketones β-Methylated secondary alcohols Transfer hydrogenation

Sodium cholesterol sulfate mediated mitoxantrone prodrug electrostatic nanocomplexes: achieving the therapeutic efficacy and safety of mitoxantrone

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Science China Chemistry 2024年

作者： Erwei Zhao Lingxiao Li Jingyi Zhang Yaqiao Li Rong Chai Bowen Zhang Jialin Xing Minglong Huang Lurong Zhang Xiaohui Pu Zhonggui He Bingjun Sun Department of Pharmaceutics Wuya College of Innovation Shenyang Pharmaceutical University Department of Bioengineering Graduate School of Engineering The University of Tokyo Peking Union pharmaceutical Factory Ltd. State Key Laboratory of Antiviral Drugs School of Pharmacy Henan University Joint International Research Laboratory of Intelligent Drug Delivery Systems Ministry of Education Shenyang Pharmaceutical University

Forming electrostatic nanocomplexes(ENCs) with counter-ions can improve the delivery efficiency of chemotherapy ***, water-soluble chemotherapy drugs like mitoxantrone(MTO), have limited affinity for counter-ions, posing challenges in the creation of stable ENCs. Herein, MTO was connected to fatty alcohols of varying chain lengths(C8, C12, C16) via disulfide bonds, forming hydrophobic prodrugs. We found that conjugating MTO to fatty alcohols significantly improved its affinity for the counter-ion sodium cholesterol sulfate(SCS). Among the designed prodrugs, conjugated to fatty alcohols with longer carbon chain lengths exhibited heightened affinity for SCS, resulting in the formation of more stable ENCs. However,extending the carbon chain also slowed the rate of drug release. Overall, compared with MTO solution, these ENCs demonstrated comparable therapeutic efficacy while causing minimal damage to healthy tissues, especially for MTO-SS-C16 ENCs. Our research provides new insights for constructing stable and safe ENCs for hydrophilic drugs like MTO.

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