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A novel marine-derived anti-acute kidney injury agent targeting peroxiredoxin 1 and its nanodelivery strategy based on ADME optimization

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3232-3250页

作者： Ping Yu Tanwei Gu Yueyang Rao Weimin Liang Xi Zhang Huanguo Jiang Jindi Lu Jianglian She Jianmin Guo Wei Yang Yonghong Liu Yingfeng Tu Lan Tang Xuefeng Zhou guangdong Provincial Key Laboratory of New Drug Screening Guangdong-Hong Kong-Macao Joint Laboratory for New Drug ScreeningSchool of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China CAS Key Laboratory of Tropical Marine Bio-Resources and Eco.ogy Guangdong Key Laboratory of Marine Materia MedicaSouth China Sea Institute of OceanologyChinese Academy of SciencesGuangzhou 510301China NMPA Key Laboratory for research and Evaluation of Drug Metabolism School of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China guangdong lewwin pharmaceutical research institute co. Ltd.Guangdong Provincial Key Laboratory of Drug Non-Clinical Evaluation and ResearchGuangdong Engineering Research Center for Innovative Drug Evaluation and ResearchGuangzhou 510990China

Insufficient therapeutic strategies for acute kidney injury(AKI)necessitate precision therapy targeting its *** study reveals the new mechanism of the marine-derived anti-AKI agent,piericidin glyco.ide S14,targeting peroxiredoxin 1(PRDX1).By binding to Cys83 of PRDX1 and augmenting its peroxidase activity,S14 alleviates kidney injury efficiently in Prdx1-overexpression(Prdx1-OE)***,S14 also increases PRDX1 nuclear translocation and directly activates the Nrf2/HO-1/NQO1 pathway to inhibit ROS *** to the limited druggability of S14 with low bioavailability(2.6%)and poor renal distribution,a pH-sensitive kidney-targeting dodecanaminechitosan nanoparticle system is co.structed to load S14 for precise treatment of AKI.L-Serine co.jugation to chitosan imparts specificity to kidney injury molecule-1(Kim-1)-overexpressed *** developed S14-nanodrug exhibits higher therapeutic efficiency by improving the in vivo behavior of S14 *** encapsulation with micelles,the AUC_(0-t),half-life time,and renal distribution of S14 increase 2.5-,1.8-,and 3.1-fold,*** main factors co.tributing to the improved druggability of S14 nanodrugs include the lower metabolic elimination rate and UDPglyco.yltransferase(UGT)-mediated *** summary,this study identifies a new therapeutic target for the marine-derived anti-AKI agent while enhancing its ADME properties and druggability through nanotechnology,thereby driving advancements in marine drug development for AKI.

关键词： Acute kidney injury Piericidin glyco.ide Peroxiredoxin 1 Nanodrug Kim-1 targeted ADME Marine drug Druggability

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Zhuangyao Jianshen pill(壮腰健肾丸) ameliorates testosterone-induced benign postatic hyperplasia in rats

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Journal of Traditional Chinese Medicine 2024年第4期44卷 694-702页

作者： ZHENG Jingrui CHEN Weijian YE Binbin MO Ziyao DU Qunqun QIN Renan NIE Ke School of Chinese Materia Medica Guangdong Pharmaceutical UniversityGuangzhou 510006China Modern Chinese Medicine research institute Guangzhou Baiyunshan Chenliji Pharmaceutical Factory Co.Ltd.Guangzhou 510228China

OBJECTIVE:To determine the therapeutic effects of the Zhuangyao Jianshen pill(壮腰健肾丸,ZYJSP)against benign prostatic hyperplasia(BPH)and investigate the underlying ***:Forty-eight male Sprague-Dawley rats were randomly divided into six groups:co.trol group,BPH model group,finasteride-treated group,ZYJSP low,medium and high dose *** for the co.trol group,40 rats were castrated and injected with testosterone propionate(TP)for 28 co.secutive day to induce ***,the co.responding drugs were administered by *** prostate wet weight,prostate index(PI),and the histopathological changes in the prostate were measured as the basis for examining the efficacy of ZYJSP against *** of the serum sex hormones,oxidative stress markers,inflammatory markers,renal function markers,growth factors,and Cyclin D1 expression in prostate were measured to characterize the therapeutic mechanism of ZYJSP against ***:ZYJSP administration significantly reduced prostate wet weight and PI and ameliorated histological changes of the prostate in TP-treated castrated *** markedly increased the levels of creatinine,blood urea nitrogen and growth factors in the serum as well as the expression of the Cyclin D1 in the *** of these markers were significantly decreased by *** significantly restored the dysregulation of testosterone,estradiol,and dihydrotestosterone caused by ***,ZYJSP relieved TP-induced prostate injury and exhibited both anti-inflammatory and anti-oxidant activity by decreasing interleukin-6,interleukin-8,and malondialdehyde levels and increasing the activity of superoxide dismutase in the ***:These findings indicate that ZYJSP can effectively ameliorate BPH induced by TP in castrated rats,and the underlying mechanism might be related to regulating sex hormone balance,reducing oxidative stress,and inhibiting the inflammatory response.

关键词： testosterone ameliorate hyperplasia

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A novel dual serotonin transporter and M-channel inhibitor D01 for antidepression and co.nitive improvement

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1457-1466页

作者： Yaqin Wei Xiangqing Xu Qiang Guo Song Zhao Yinli Qiu Dongli Wang Wenwen Yu Yani Liu KeWei Wang School of Pharmacy Xuzhou Medical UniversityXuzhou 221004China institute of pharmaceutical research Jiangsu Nhwa Pharmaceutical Co.Ltd.&Jiangsu Key Laboratory of Central Nervous System Drug Research and DevelopmentXuzhou 221116China Department of Pharmaco.ogy School of PharmacyQingdao University Medical CollegeQingdao 266073China institute of Innovative Drug Qingdao UniversityQingdao 266021China Center for Brain Science and Brain-Inspired Intelligence Guangdong-Hong Kong-Macao Greater Bay AreaGuangzhou 510515China

co.nitive dysfunction is a co.e symptom co.mon in psychiatric disorders including depression that is primarily managed by antidepressants lacking efficacy in improving *** this study,we report a novel dual serotonin transporter and voltage-gated potassium Kv7/KCNQ/M-channel inhibitor D01(a 2-methyl-3-aryloxy-3-heteroarylpropylamines derivative)that exhibits both anti-depression effects and improvements in co.nition.D01 inhibits serotonin transporters(K_(i)=30.1±6.9 nmol/L)and M channels(IC_(50)=10.1±2.4μmol/L).D01 also reduces the immobility duration in the mouse FST and TST assays in a dose-dependent manner without a stimulatory effect on *** administrations of D01(20 and 40 mg/kg)can significantly shorten the immobility time in a mouse model of chronic restraint stress(CRS)-induced depression-like ***,D01 dose-dependently improves the co.nitive deficit induced by CRS in Morris water maze test and increases the exploration time with novel objects in normal or sco.olamine-induced co.nitive deficits in mice,but not ***,D01 reverses the long-term potentiation(LTP)inhibition induced by *** together,our findings demonstrate that D01,a dual-target serotonin reuptake and M channel inhibitor,is highly effective in the treatment-resistant depression and co.nitive deficits,thus holding potential for development as therapy of depression with co.nitive deficits.

关键词： SERT 5-HT Kv7/KCNQ/M current D01 Depression co.nition

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Bioactive co.ponents,pharmaco.ogical properties and underlying mechanism of Ganoderma lucidum spore oil:A review

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Chinese Herbal Medicines 2024年第3期16卷 375-391页

作者： Jianying Liu Binzhi Zhang Leqi Wang Shasha Li Qinqiang Long Xue Xiao guangdong Metabolic Diseases research Center of Integrated Chinese and Western Medicine(institute of Chinese Medicine) Guangdong Pharmaceutical UniversityGuangzhou 510006China The Seco.d Clinical co.lege of Guangzhou University of Chinese Medicine Guangzhou Higher Education Mega CenterGuangzhou 510120China NMPA Key Laboratory for Rapid Testing Technology of Drugs Guangdong Institute for Drug ControlGuangzhou 510525China

Ganoderma lucidum is a Chinese medicinal fungus with a long history of use in healthcare and disease *** spores(GLS)are tiny germ cells released from the mushroom cap during the mature stage of *** co.tain all the genetic active substances of *** spore oil(GLSO)is a lipid co.ponent extracted from broken-walled Ganoderma spores using supercritical co.(2)extraction *** co.tains fatty acids,Ganoderma triterpenes,sterols and other bioactive *** studies have demonstrated that GLSO has a wide range of pharmaco.ogical properties,including anti-tumor,anti-aging,neuroprotection,immunomodulation,hepatoprotection and modulation of metabolic *** review summarizes the research progress of GLSO over the past two decades in terms of its bioactive co.ponents,extraction and processing techniques,pharmaco.ogical effects and safety *** provides a solid foundation for further research and application of GLSO.

关键词： anti-aging anti-tumor bioactive co.ponents Ganoderma lucidum spore oil hepatoprotection immune regulation pharmaco.ogical properties

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Generic Interpretable Reaction co.dition Predictions with Open Reaction co.dition Datasets and Unsupervised Learning of Reaction Center

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research 2024年第2期2023卷 773-794页

作者： Xiaorui Wang Chang-Yu Hsieh Xiaodan Yin Jike Wang Yuquan Li Yafeng Deng Dejun Jiang Zhenxing Wu Hongyan Du Hongming Chen Yun Li Huanxiang Liu Yuwei Wang Pei Luo Tingjun Hou Xiaojun Yao Dr.Neher's Biophysics Laboratory for lnnovative Drug Disco.ery State Key Laboratory of Quality Research in Chinese MedicineMacao Institute for Applied Research in Medicine and HealthMacao University of Science and TechnologyMacao999078China innovation institute for Artificial Intelligence in Medicine of Zhejiang University College of Pharmaceutical SciencesZhejiang UniversityHangzhou310058China Faculty of Applied Sciences Macao Polytechnic UniversityMacao999078China co.lege of Chemistry and Chemical Engineering Lanzhou UniversityLanzhou730000China Carbon Silico. AI Technology co. LtdHangzhouZhejiang 310018China Center of Chemistry and Chemical Biology Guangzhou Regenerative Medicine and Health Guangdong LaboratoryGuangzhou 510530China co.lege of Pharmacy Shaanxi University of Chinese MedicineXianyangShaanxi712044China

Effective synthesis planning powered by deep learning(DL)can significantly accelerate the disco.ery of new drugs and ***,most DL-assisted synthesis planning methods offer either none or very limited capability to reco.mend suitable reaction co.ditions(RCs)for their reaction ***,the prediction of RCs with a DL framework is hindered by several factors,including:(a)lack of a standardized dataset for benchmarking,(b)lack of a general prediction model with powerful representation,and(c)lack of *** address these issues,we first created 2 standardized RC datasets co.ering a broad range of reaction classes and then proposed a powerful and interpretable Transformer-based RC predictor named *** careful design of the model architecture,pretraining method,and training strategy,Parrot improved the overall top-3 prediction accuracy on catalysis,solvents,and other reagents by as much as 13.44%,co.pared to the best previous model on a newly curated ***,the mean absolute error of the predicted temperatures was reduced by about 4℃.Furthermore,Parrot manifests strong generalization capacity with superior cross-chemical-space prediction *** analysis indicates that Parrot effectively captures crucial chemical information and exhibits a high level of interpretability in the prediction of *** proposed model Parrot exemplifies how modern neural network architecture when appropriately pretrained can be versatile in making reliable,generalizable,and interpretable reco.mendation for RCs even when the underlying training dataset may still be limited in diversity.

关键词： versatile absolute generalization

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Deciphering the high-carbonization-temperature triggered enzymatic activity of wool-derived N,S-co.doped carbon nanosheets

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Chinese Chemical Letters 2024年第3期35卷 182-188页

作者： Jiachen Zhao Deshuai Yu Jianmin Chen Shihao Lin Yonghua Tang Chaoyu Fan Dongfang Zhou Youhui Lin Department of Physics Research Institute for Biomimetics and Soft MatterFujian Provincial Key Laboratory for Soft Functional Materials ResearchXiamen UniversityXiamen 361005China School of Pharmacy and Medical Technology Putian UniversityPutian 351100China Key Laboratory of Mental Health of the Ministry of Education NMPA Key Laboratory for Research and Evaluation of Drug Metabolism&Guangdong Provincial Key Laboratory of New Drug ScreeningSchool of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China Key Laboratory of pharmaceutical Analysis and Laboratory Medicine(Putian University) Fujian Province UniversityPutian 351100China

It is well-established that high carbonization temperature will trigger the enzyme-like activity of carbon-based ***,the catalytic mechanism is still ambiguous,which hinders the further rational design of nanomaterials as enzyme ***,N,S-rich carbonized wool nanosheets(CWs)were synthesized at different pyrolysis *** expected,only CWs treated with high-temperature possess intrinsic oxidase-and peroxidase-like ***,density functional theory(DFT)calculations demonstrate that graphitic nitrogen and the co.existence of nitrogen and sulfur in the carbon matrix serve as the active sites for the enzyme-like *** importantly,co.bining theoretical calculations and experimental observations,the high-temperature triggered catalytic mechanism can be ascribed to the fact that an appropriate high-temperature maximizes the graphitization degree to a certain extent,at which most of the catalytic active sites are well retained rather than ***,co.pling with excellent photothermal co.version efficiency and catalytic performance,CWs can be applied to photothermal-catalytic cancer therapy under near-infrared region(NIR)light *** believe this work will co.tribute to understanding the catalytic mechanism of carbon-based nanozymes and promote the development of new biomedical and pharmaceutical applications.

关键词： Carbon-based nanozyme Catalytic mechanism Density functional theory High-temperature carbonization

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Efficient Photolytic Halogenation and Oxidation of Unactivated Alkyl sp^(3) C—H Bonds with Iodine(III)

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Chinese Journal of Chemistry 2024年第5期42卷 505-510页

作者： Hao Jia Nan Li Chunmei Tang Yajuan Wang Yonghao Xi Rongbao Liao Wei Xu Fufang Wu Xiaobao Shen Hongbin Zhai Biomass Oligosaccharides Engineering Technology research Center of Anhui Province Engineering Research Center of Biomass Conversion and Pollution Prevention of Anhui Educational InstitutionsFuyang Normal UniversityFuyangAnhui236037 China institute of Marine Biomedicine Shenzhen PolytechnicShenzhenGuangdong518055 China State Key Laboratory of Chemical Onco.enomics Shenzhen Engineering Laboratory of Nano Drug Slow-ReleasePeking University Shenzhen Graduate SchoolShenzhenGuangdong518055 China

A metal-free,green,and sustainable functionalization of unactivated alkyl sp^(3) C—H bonds is reported using iodine(III)as a feasible dehydrogenation agent under visible light or KBr,and alkyl chlorides,bromides,alco.ols,and ketones co.ld be co.structed by addition of different co.pling *** and safe iodobenzene diacetate was used to form a radical to activate the alkyl sp^(3) C—H bond in a highly efficient manner,which can co.struct different alkylation products by adding co.responding co.pling reagents.

关键词： Alkyl sp^(3)C—H bonds Chlorination Bromination Oxidation Iodine(III) C—H activation Radical Photocatalysis

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Advancements in the application of natural extracts for atopic dermatitis treatment

Journal of dermatologic science and cosmetic technology

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Journal of dermatologic science and co.metic technology 2024年第2期1卷 45-52页

作者： Yi Peng Miaohong Yang Ju Wen Huixiong Chen Weihua Shen Ling Jiang Yi Li Li Lin Zhiyun Du Xinjiang Technical institute of Physics and Chemistry Chinese Academy of SciencesUrumqi 830011China School of Biomedical and pharmaceutical Sciences Guangdong University of TechnologyGuangzhou 510006China Foshan Allan co.ney Biotechnology co. LtdFoshan 523281China guangdong co.metics Association Guangzhou 510006China University of Chinese Academy of Sciences Beijing 100049China Department of Dermatology Guangdong Second People's HospitalGuangzhou 510317China Laboratory of Pharmaco.ogic and Toxico.ogic Chemistry and Biochemistry UMR 8601 CNRSParis Descartes UniversityParis 75006France

Atopic dermatitis,a co.mon chronic inflammatory skin disease,has an unclear etiology and may involve multiple factors such as genetic predisposition,immune abnormalities,and impaired skin barrier ***,there is no specific medication available for the co.plete cure of atopic *** current treatment approaches mainly focus on symptom relief and co.trol rather than curative *** co.monly used medications for atopic dermatitis,such as topical co.tico.teroids and immunosuppressants,may have certain adverse reactions and side *** review summarizes the research progress on natural extracts in the treatment of atopic dermatitis,aiming to provide a foundation for the development of safe and side-effectfree medications.

关键词： Atopic dermatitis Natural extracts Treatment

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Enco.ing and display technologies for co.binatorial libraries in drug disco.ery:The co.ing of age from biology to therapy

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Acta Pharmaceutica Sinica B 2024年第8期14卷 3362-3384页

作者： Yu Fan Ruibing Feng Xinya Zhang Zhen-Liang Wang Feng Xiong Shuihua Zhang Zhang-Feng Zhong Hua Yu Qing-Wen Zhang Zhang Zhang Yitao Wang Guodong Li Macao Centre for research and Development in Chinese Medicine State Key Laboratory of Quality Research in Chinese MedicineInstitute of Chinese Medical SciencesUniversity of MacaoMacao SAR 999078China State Key Laboratory of Quality research in Chinese Medicine Institute of Chinese Medical SciencesUniversity of MacaoMacao SAR 999078China International co.perative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development Ministry of Education(MoE)of People’s Republic of ChinaCollege of PharmacyJinan UniversityGuangzhou 510632China Zhuhai UM Science and Technology research institute Zhuhai 519031China Department of Pharmacy Guangzhou Red Cross HospitalFaculty of Medical ScienceJinan UniversityGuangzhou 510632China Geriatric Medicine First People’s Hospital of XinXiang and the Fifth Affiliated Hospital of Xinxiang Medical CollegeXinxiang 453100China Shenzhen Innovation Center for Small Molecule Drug Disco.ery co. Ltd.Shenzhen 518000China

Drug disco.ery is a sophisticated process that inco.porates scientific innovations and cuttingedge *** to traditional bioactivity-based screening methods,enco.ing and display technologies for co.binatorial libraries have recently advanced from proof-of-principle experiments to promising tools for pharmaceutical hit disco.ery due to their high screening efficiency,throughput,and resource *** review systematically summarizes the development history,typology,and prospective applications of enco.ing and displayed technologies,including phage display,ribosomal display,mRNA display,yeast cell display,one-bead one-co.pound,DNA-enco.ed,peptide nucleic acidenco.ed,and new peptide-enco.ed technologies,and examples of preclinical and clinical *** discuss the progress of novel targeted therapeutic agents,co.ering a spectrum from small-molecule inhibitors and nonpeptidic macrocycles to linear,monocyclic,and bicyclic peptides,in addition to *** also address the pending challenges and future prospects of drug disco.ery,including the size of screening libraries,advantages and disadvantages of the technology,clinical translational potential,and market *** review is intended to establish a co.prehensive high-throughput drug disco.ery strategy for scientific researchers and clinical drug developers.

关键词： Drug screening Phage display DNA-enco.ed chemical libraries Peptide-enco.ed chemical libraries Clinical drugs

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ACQ到CIE转化:水合作用诱导的姜黄素晶体发光及可调热致变色用于体内药物追踪（英文）

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Science China Materials 2024年

作者：申欢石鹏刘二刚方月飞许史杰龚俊波黄永焯 Zhongshan institute for Drug Disco.ery Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai institute of Materia Medica Chinese Academy of Sciences School of Chemical Engineering and Technology Tianjin University SINOPEC research institute of Petroleum Processing co. Ltd. co.lege of Chemical Engineering and Materials Science Tianjin University of Science and Technology NMPA Key Laboratory for Quality research and Evaluation of pharmaceutical Excipients Shanghai

目前固态材料在受刺激时能够切换发光性质仍然是一个挑战,特别是对于有机材料而言.晶体中的水分子极大地影响有机晶体的吸收光谱,但是否可以系统地通过水分子调控有机发光材料的发射光谱尚不清楚.在本研究中,我们成功地制备了姜黄素一...

目前固态材料在受刺激时能够切换发光性质仍然是一个挑战,特别是对于有机材料而言.晶体中的水分子极大地影响有机晶体的吸收光谱,但是否可以系统地通过水分子调控有机发光材料的发射光谱尚不清楚.在本研究中,我们成功地制备了姜黄素一水合物(Ⅹ型),它是一种结晶诱导发光(CIE)的通道型水合物,在608 nm处发出橙色荧光,与传统的聚集诱导荧光猝灭(ACQ)形式有所不同.经过热处理后,姜黄素水合物释放出水分子,形成了新的无水合物(Ⅳ型),其发出黄绿色荧光,且最佳发射波长为575 nm.该方法可用于追踪皮下或肌肉注射后姜黄素晶体的吸收.水合物介导的单晶到单晶转变(SCSC)及其相关的发光转变是可逆的,并且对温度敏感,可为合成和设计基于聚集诱导发射(AIE)的智能发光装置提供一种环保的途径,也可用于检测空气湿度或示踪药物吸收.

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