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Discovery of a potential bladder cancer inhibitor CHNQD-01281 by regulating EGFR and promoting infiltration of cytotoxic T cells

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Marine Life Science & Technology 2024年第3期6卷 502-514页

作者： Jian-Yu Liu Yao-Yao Jiang Peng-Jie Li Bo Yao Yi-Jing Song Ji-Xiu Gao Gulab Said Yang Gao Jun-Yu Lai chang-lun shao Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Department of Critical Care Medicine the Affiliated Hospital of Qingdao UniversityQingdao 266003China Department of Chemistry Women University SwabiSwabi 23430Pakistan Laoshan Laboratory Qingdao 266237China Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education College of Chemistry and Chemical EngineeringHainan Normal UniversityHaikou 571158China

As one of the common malignancies that threaten human life,bladder cancer occurs frequently with a high mortality rate in the world,due to its invasion,recurrence and drug *** products from marine microorganisms are becoming the hotspots in discovery of new candidate drug entities,especially in the area of *** A(BFA)is a natural Arf-GEFs inhibitor,but due to the low aqueous solubility,strong toxicity,and poor bioavailability,it is urgent to conduct structural optimization ***,a new BFA pyridine acrylate derivative CHNQD-01281 with improved solubility was prepared and found to exert moderate to strong antiproliferative activity on a variety of human cancer cell *** was noteworthy that CHNQD-01281 was most sensitive to two bladder cancer cell lines T24 and J82(IC50=0.079 and 0.081μmol/L)with high selectivity index(SI=14.68 and 14.32),suggesting a superior safety to *** vivo studies revealed that CHNQD-01281 remarkably suppressed tumor growth in a T24 nude mice xenograft model(TGI=52.63%)and prolonged the survival time(ILS=68.16%)in an MB49 allogeneic mouse model via inducing infiltration of cytotoxic T *** mechanism exploration indicated that CHNQD-01281 regulated both EGFR/PI3K/AKT and EGFR/ERK pathways and mediated the chemotactic effect of chemokines on immune effector ***,CHNQD-01281 may serve as a potential therapeutic agent for bladder cancer through multiple mechanisms.

关键词： Bladder cancer Marine natural products Brefeldin A EGFR/PI3K/AKT EGFR/ERK T-cell infiltration

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Metabolites from marine invertebrates and their symbiotic microorganisms: molecular diversity discovery, mining, and application

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Marine Life Science & Technology 2019年第1期1卷 60-94页

作者： Lu Liu Yao-Yao Zheng chang-lun shao chang-Yun Wang Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Laboratory for Marine Drugs and Bioproducts Qingdao National Laboratory for Marine Science and TechnologyQingdao 266237China Single-Cell Center CAS Key Laboratory of Biofuels and Shandong Key Laboratory of Energy GeneticsQingdao Institute of Bioenergy and Bioprocess TechnologyChinese Academy of SciencesQingdao 266101China Institute of Evolution and Marine Biodiversity Ocean University of ChinaQingdao 266003China

Metabolites from marine organisms have proven to be a rich source for the discovery of multiple potent bioactive moleculeswith diverse structures. In recent years, we initiated a program to investigate the diversity of the secondary metabolites frommarine invertebrates and their symbiotic microorganisms collected from the South China Sea. In this review, representativecases are summarized focusing on molecular diversity, mining, and application of natural products from these marineorganisms. To provide a comprehensive introduction to the field of marine natural products, we highlight typical moleculesincluding their structures, chemical synthesis, bioactivities and mechanisms, structure-activity relationships as well as biogenesis. The mining of marine-derived microorganisms to produce novel secondary metabolites is also discussed through theOSMAC strategy and via partial chemical epigenetic modification. A broad prospectus has revealed a plethora of bioactivenatural products with novel structures from marine organisms, especially from soft corals, gorgonians, sponges, and theirsymbiotic fungi and bacteria.

关键词： Marine invertebrates Symbiotic microorganisms Marine natural products Molecular diversity Bioactivities Marine drugs

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The intriguing chemistry and biology of sulfur-containing natural products from marine microorganisms(1987-2020)

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Marine Life Science & Technology 2021年第4期3卷 488-518页

作者： Yang Hai Mei-Yan Wei chang-Yun Wang Yu-Cheng Gu chang-lun shao Key Laboratory of Marine Drugs School of Medicine and PharmacyThe Ministry of Education of ChinaOcean University of ChinaQingdao 266003China Laboratory for Marine Drugs and Bioproducts Pilot National Laboratory for Marine Science and Technology(Qingdao)Qingdao 266237China College of Food Science and Engineering Ocean University of ChinaQingdao 266003China Syngenta Jealott’s Hill International Research Centre BracknellBerkshire RG426EYUK

Natural products derived from marine microorganisms have received great attention as a potential resource of new compound entities for drug *** unique marine environment brings us a large group of sulfur-containing natural products with abundant biological functionality including antitumor,antibiotic,anti-inflammatory and antiviral *** reviewed all the 484 sulfur-containing natural products(non-sulfated)isolated from marine microorganisms,of which 59.9%are thioethers,29.8%are thiazole/thiazoline-containing compounds and 10.3%are sulfoxides,sulfones,thioesters and many others.A selection of 133 compounds was further discussed on their structure-activity relationships,mechanisms of action,biosynthesis,and *** is the first systematic review on sulfur-containing natural products from marine microorganisms conducted from January 1987,when the first one was reported,to December 2020.

关键词： Sulfur-containing natural products Marine microorganisms Molecular diversity Bioactivities Marine drugs

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Co-culture:stimulate the metabolic potential and explore the molecular diversity of natural products from microorganisms

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Marine Life Science & Technology 2021年第3期3卷 363-374页

作者： Xiao-Yue Peng Jin-Tao Wu chang-lun shao Zhi-Yong Li Min Chen chang-Yun Wan Key Laboratory of Marine Drugs The Ministry of Education of ChinaSchool of Medicine and PharmacyInstitute of Evolution and Marine BiodiversityOcean University of ChinaQingdao266003China Marine Science and Technology Institute College of Environmental Science and EngineeringYangzhou UniversityYangzhou225127China Laboratory for Marine Drugs and Bioproducts Qingdao National Laboratory for Marine Science and TechnologyQingdao266237China State Key Laboratory of Microbial Metabolism School of Life Sciences and BiotechnologyShanghai Jiao Tong UniversityShanghai201100China

Microbial secondary metabolites have long been considered as potential sources of lead compounds for medicinal use due to their rich chemical diversity and extensive biological ***,many biosynthetic gene clusters remain silent under traditional laboratory culture conditions,resulting in repeated isolation of a large number of known *** co-culture strategy simulates the complex ecological environment of microbial life by using an ecology-driven method to activate silent gene clusters of microorganisms and tap their metabolic potential to obtain novel bioactive secondary *** this review,representative studies from 2017 to 2020 on the discovery of novel bioactive natural products from co-cultured microorganisms are summarized.A series of natural products with diverse and novel structures have been discovered successfully by co-culture strategies,including fungus-fungus,fungus-bacterium,and bacterium-bacterium co-culture *** novel compounds exhibited various bioactivities including extensive antimicrobial activities and potential cytotoxic activities,especially when it came to disparate marine-derived species and cross-species of marine strains and terrestrial *** could be concluded that co-culture can be an effective strategy to tap the metabolic potential of microorganisms,particularly for marine-derived species,thus providing diverse molecules for the discovery of lead compounds and drug candidates.

关键词： Co-culture Microorganisms Secondary metabolites Chemical diversity

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Targeted isolation of antitubercular cycloheptapeptides and an unusual pyrroloindoline-containing new analog,asperpyrroindotide A,using LC–MS/MS-based molecular networking

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Marine Life Science & Technology 2023年第1期5卷 85-93页

作者： Yi-Qian Han Qun Zhang Wei-Feng Xu Yang Hai Rong Chao Cui-Fang Wang Xue-Mei Hou Mei-Yan Wei Yu-Cheng Gu chang-Yun Wang chang-lun shao Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources School of Chemistry and Pharmaceutical SciencesGuangxi Normal UniversityGuilin 541004China College of Food Science and Engineering Ocean University of ChinaQingdao 266003China Syngenta Jealott’s Hill International Research Centre BracknellBerkshire RG426EYUK Laboratory for Marine Drugs and Bioproducts Qingdao National Laboratory for Marine Science and TechnologyQingdao 266237China

Further insights on the secondary metabolites of a soft coral-derived fungus Aspergillus versicolor under the guidance of MS/MS-based molecular networking led to the isolation of seven known cycloheptapeptides,namely,asperversiamides A–C(1–3)and asperheptatides A–D(4–7)and an unusual pyrroloindoline-containing new cycloheptapeptide,asperpyrroindotide A(8).The structure of 8 was elucidated by comprehensive spectroscopic data analysis,and its absolute configuration was determined by advanced Marfey’s *** semisynthetic transformation of 1 into 8 was successfully achieved and the reaction conditions were ***,a series of new derivatives(10−19)of asperversiamide A(1)was semi-synthesized and their anti-tubercular activities were evaluated against Mycobacterium tuberculosis *** preliminary structure−activity relationships revealed that the serine hydroxy groups and the tryptophan residue are important to the activity.

关键词： Marine natural product MS/MS-based molecular networking Cycloheptapeptides Semi-synthesis Anti-tubercular activity

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Discovery of a natural small‑molecule AMP‑activated kinase activator that alleviates nonalcoholic steatohepatitis

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Marine Life Science & Technology 2023年第2期5卷 196-210页

作者： Jin Chen Li Xu Xue-Qing Zhang Xue Liu Zi-Xuan Zhang Qiu-Mei Zhu Jian-Yu Liu Muhammad Omer Iqbal Ning Ding chang-lun shao Mei-Yan Wei Yu-Chao Gu Key Laboratory of Marine Drugs the Ministry of EducationSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Laboratory for Marine Drugs and Bioproducts Laoshan LaboratoryQingdao 266237China College of Food Science and Engineering Ocean University of ChinaQingdao 266003China Key Laboratory of Glycoscience and Glycotechnology of Shandong Province Qingdao 266003China The Massachusetts General Hospital Cancer Center Harvard Medical SchoolBostonMA 02114USA

Non-alcoholic steatohepatitis(NASH)is a primary cause of cirrhosis and hepatocellular ***,there is no approved drug treatment for ***-activated kinase(AMPK)is an important metabolic sensor and whole-body *** has been proposed that AMPK activators could be used for treating metabolic diseases such as obesity,type 2 diabetes and *** this study,we screened a marine natural compound library by monitoring AMPK activity and found a potent AMPK activator,candidusin A(CHNQD-0803).Further studies showed that CHNQD-0803 directly binds recombinant AMPK with a K_(D) value of 4.728×10^(-8) M and activates AMPK at both molecular and intracellular *** then investigated the roles and mechanisms of CHNQD-0803 in PA-induced fat deposition,LPS-stimulated infammation,TGF-β-induced fbrosis cell models and the MCD-induced mouse model of *** results showed that CHNQD-0803 inhibited the expression of adipogenesis genes and reduced fat deposition,negatively regulated the NF-κB-TNFαinfammatory axis to suppress infammation,and ameliorated liver injury and *** data indicate that CHNQD-0803 as an AMPK activator is a novel potential therapeutic candidate for NASH treatment.

关键词： NASH AMPK Infammation Lipid metabolism Fibrosis Marine drug

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Bioactive Diphenyl Ether Derivatives from a Marine-Derived Talaromyces ***

Bioactive Diphenyl Ether Derivatives from a Marine-Derived T...

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全国第九届海洋生物技术与创新药物学术会议

作者： Min Chen Lei Han chang-lun shao chang-Yun Wang Key Laboratory of Marine Drugs The Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of China

Marine-derived fungi have proven to be rich sources of structurally novel and biologically active secondary metabolites for drug *** have been an increasing number of reports of bioactive natural products from marine-derived *** ether derivatives,a class of fungal polyketide metabolites,have been reported to show a wide range of biological activities including antibacterial,antifungal,cytotoxic *** our ongoing research for bioactive metabolites from marine-derived fungi,a fungal strain,Talaromyces sp.,which was isolated from the gorgonian Subergorgia suberosa collected from the South China Sea,attracted our attention.A chemical investigation of the bioactive extract resulted in the isolation of three new diphenyl ether derivatives,purpactins D-F(1-3),together with 6 known analogues(4-9).The structures of the new compounds were determined by extensive NMR spectroscopic *** of the isolated metabolites(1-9)were evaluated for their cytotoxic and antifouling *** 4 exhibited pronounced cytotoxicity towards five human cell lines HepG2,Hep3B,MCF-7/ADR,PC-3,and HCT-116 with the ICvalues ranging from 2.8 to 5.1μg/*** 3,5,8 and 9 showed potent antifouling activity against the larval settlement of the barnacle Balanus amphitrite with ECvalues ranging from 2.2 to 4.8μg/mL.

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Structure modification,antialgal,antiplasmodial,and toxic evaluations of a series of new marine-derived 14-membered resorcylic acid lactone derivatives

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Marine Life Science & Technology 2022年第1期4卷 88-97页

作者： Wei-Feng Xu Na-Na Wu Yan-Wei Wu Yue-Xuan Qi Mei-Yan Wei Laura M.Pineda Michelle G.Ng Carmenza Spadafora Ji-Yong Zheng Ling Lu chang-Yun Wang Yu-Cheng Gu chang-lun shao Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of ChinaQingdao266003China Laboratory for Marine Drugs and Bioproducts Qingdao National Laboratory for Marine Science and TechnologyQingdao266237China State Key Laboratory for Marine Corrosion and Protection Luoyang Ship Material Research Institute(LSMRI)Qingdao266237China Center of Cellular and Molecular Biology of Diseases Instituto de Investigaciones Científcas y Servicios de Alta TecnologíaCity of KnowledgeClaytonApartado0816-02852Panama Syngenta Jealott’s Hill International Research Centre BracknellBerkshireRG426EYUK

Marine natural products play critical roles in the chemical defense of many marine organisms and are essential,reputable sources of successful drug ***-seven 14-membered resorcylic acid lactone derivatives 3–27 and 30–71 of the natural product zeaenol(1)isolated from the marine-derived fungus Cochliobolus lunatus were semisynthesized by chlorination,acylation,esterification,and acetalization in one to three *** structures of these new derivatives were established by HRESIMS and NMR *** the compounds(1–71)were evaluated for their antialgal and antiplasmodial *** them,14 compounds displayed antifouling activities against adhesion of the fouling *** particular,9 and 34 exhibited strong and selective inhibitory effects against the diatoms Navicula laevissima and Navicula exigua(EC50=6.67 and 8.55μmol/L),respectively,which were similar in efficacy to those of the positive control SeaNine 211(EC50=2.90 and 9.74μmol/L).More importantly,38,39,and 69–71 showed potent antiplasmodial activities against Plasmodium falciparum with IC50 values ranging from 3.54 to 9.72μmol/*** interestingly,the five antiplasmodial derivatives displayed non-toxicity in the cytotoxicity assays and the zebrafish embryos model,thus,representing potential promising antiplasmodial drug *** preliminary structure–activity relationships indicated that biphenyl substituent at C-2,acetonide at positions C-5′and C-6′,and tri-or tetra-substituted of acyl groups increased the antiplasmodial ***,combining evaluation of chemical ecology with pharmacological models will be implemented as a systematic strategy,not only for environmentally friendly antifoulants but also for structurally novel drugs.

关键词： Marine natural product 14-Membered resorcylic acid lactone Zeaenol Semisynthesis Antialgal activity Antiplasmodial activity

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The Systematic Evolution and Functional Differentiation of Fungal PKS Product Template Domains for C2-C7 Cyclization

The Systematic Evolution and Functional Differentiation of F...

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第十二届海洋药物学术年会

作者： Lu Liu Zheng Zhang chang-lun shao Jin-Lan Wang Hong Bai chang-Yun Wang Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of China State Key Laboratory of Microbial Technology Shandong University School of Life Science Shandong University Institute of Evolution&Marine Biodiversity Ocean University of China

Objective The relationships between sequences,structures and functions of the fungal NR-PKS PT domains for C2-C7 cyclization were analyzed with all known fungal NR-PKS *** Bioinformatic methods,including phylogenetic analysis,structure modeling and evolutional conservation analysis,were applied to systematicly study the PT *** The C2-C7 catalytic pockets of PT domains were lack of the finger-like regions and the catalytic dyads located at the bottom of the pockets Comparing PT domains for C2-C7 cyclization in different groups,most of the cavity lining residue（CLR）sites were common,while the regional CLR site mutations resulted in the differentiations of the cavity shapes and volumes corresponding with structures of the representative *** The conservative residues in PT sequences for C2-C7 cyclization were responsible for the cyclization functions and the evolution of the key residues resulted in the differentiations of cyclization functions attributed tothe changes of the cavity *** findings may help to better understand the C2-C7 cyclization mechanisms of PT domains and even predict the structural types of the aromatic polyketide products.

关键词： fungal polyketide synthase non-reducing PKS C2-C7 cyclization PT domain

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Enhancement of low-temperature toughness of Fe-Mn-C-Al alloy by rare earth Ce-modified inclusions

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Journal of Iron and Steel Research International 2024年第1期31卷 157-173页

作者： Guang-kai Yang chang-ling Zhuang Yi-zhuang Li Chen Hu shao-bo Li College of Materials and Metallurgy Guizhou UniversityGuiyang550025GuizhouChina Department of Mechanical Engineering University of Hong KongHong Kong999077China The State Key Laboratory of Rolling and Automation Northeastern UniversityShenyang110819LiaoningChina State Key Laboratory of Public Big Data Guizhou UniversityGuiyang550025GuizhouChina

Fe-Mn-C-Al alloys have been recognized as promising materials for certain low-temperature applications due to their exceptional mechanical properties and ***,their limited low-temperature toughness restricts their large-scale applications in specific *** influence of trace amounts of rare earth cerium(Ce)on the low-temperature toughness of Fe-18Mn-0.6C-1.8Al alloys was *** addition of Ce effectively alters the inclu-sions in the alloy,transforming large-sized irregular inclusions into fine ellipsoidal rare earth *** leads to a significant reduction in both the proportion and average size of the inclusions,resulting in their effective dispersion throughout the matrix and improved cryogenic *** presence of Ce-containing inclusions within the matrix reduces stress concentration,thereby inhibiting microcrack formation and improving impact absorption ***-cally,the addition of rare earth Ce alters the fracture behavior of the material at room temperature and low temperature,changing from brittle cleavage fracture to a more ductile failure *** impact toughness of the Fe-Mn-C-Al alloy is significantly improved by the addition of 0.0048 wt.%Ce,particularly at-196℃where the impact toughness reaches 103.6 J/cm^(2),representing an impressive improvement of 87.3%.

关键词： Fe-Mn-C-Al alloy Rare earth Low-temperature toughness Inclusion Fracture

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