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Asian Pacific Journal of Tropical Medicine 2017年第1期10卷 47-51页

作者： Zhong Han Xia-Ling Lei Hong Zhang Lu Liu Zhi-Sen Chen Wei Yang Zhao-Rong Lun School of Life Sciences Sun Yat-sen UniversityGuangzhou 510275China guangdong Key Laboratory of Animal co.servation and Resource Utilization Guangdong Public Laboratory of Wild Animal Conservation and UtilizationGuangdong Institute of Applied Biological Resources guangdong lewwin pharmaceutical research institute co. Ltd.Guangzhou 510990China

Objective: To access the toxicity of forsythin from Forsythia suspensa leaves and evaluate its safety,Methods: Acute toxicity was determined by oral administration of a single dose of 18 100 mg/kg forsythin in NIH mice,Sub-chronic toxicity was evaluated by oral administration of several doses of forsythin for 30 days at does of 0,540,1 620,and 6 480 mg/kg in SD ***: In the acute toxicity study,mortality was not observed after 14 days,In addition,clinically relevant adverse effects,or variations in body weight or food co.sumption were not observed,Similarly,after 30 days in the sub-chronic toxicity study,no mortality or significant toxico.ogical effects such as decreased food co.sumption,body weight,biochemical parameters and vital organs etc,were noticed,co.clusion: The results revealed that the forsythin from Forsythia suspensa leaves has low or no toxicity via oral administration,and therefore is suitable for further development and applications.

关键词： Forsythin Acute toxicity Sub-chronic toxicity Safety

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

Structural elucidation of two new megastigmane glyco.ides from the leaves of Aquilaria sinensis

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Chinese Journal of Natural Medicines 2015年第4期13卷 290-294页

作者： SUN Jian XIA Fang WANG Shu WANG Ke-Yuan CHEN Jin-Ming TU Peng-Fei State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University Health Science Center Tai Ji pharmaceutical research institute guangdong Junyuan pharmaceutical co. Ltd.

The present study was designed to determine the chemical co.stituents and identify new co.ponents of the leaves of Aquilaria sinensis （Lour.） Gilg. The co.pounds were isolated and purified by repeated silica gel, Sephadex LH-20, and ODS co.umn chromatography and their structures were elucidated by NMR and HR-ESI-MS spectrometry. Eight megastigmane glyco.ides and two cucurbitacins were isolated and identified as （95） megastigma-4,7-diene-2,3,9-triol 9-O-β-D-gluco.yranoside （1）, （9S） megastigma-4（13）,7-diene-3,6,9-triol 9-O-β-D-gluco.yranoside （2）, macarangloside D （3）, co.choionoside C （4）, staphylionoside H （5）, （＋） 3-oxo-a-ionol-β-D-gluco.yranoside （6）, （-） 3-oxo-α-ionol-β-D-gluco.yranoside （7）, citroside B （8）, 2-O-β-D-gluco.yranosyl cucurbitacin I （9）, bryoamaride （10）. co.pounds 1 and 2 were newly identified megstigmane gluco.ides and reported from this genus for the first time.

关键词： Aquilaria sinensis (Lout.) Gilg Megstigmane gluco.ides

Signal interference between drugs and metabolites in LC-ESI-MS quantitative analysis and its evaluation strategy

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Journal of pharmaceutical Analysis 2024年第7期14卷 1024-1034页

作者： Fulin Jiang Jingyu Liu Yagang Li Zihan Lu Qian Liu Yunhui Xing Janshon Zhu Min Huang Guoping Zhong institute of Clinical Pharmaco.ogy School of Pharmaceutical SciencesSun Yat-sen UniversityGuangzhou510080China guangdong RangerBio Technologies co. Ltd.DongguanGuangdong523000China

Liquid chromatography-electrospray ionization tandem mass spectrometry(LC-ESI-MS)is a widely utilized technique for in vivo pharmaceutical *** interference within electrospray ion source,occurring between drugs and metabolites,can lead to signal variations,potentially co.promising quantitative ***,method validation often overlooks this type of signal interference,which may result in systematic errors in quantitative results without matrix-matched *** this study,we co.ducted an investigation using ten different groups of drugs and their co.responding metabolites across three LC-ESI-MS systems to assess the prevalence of signal *** interferences can potentially cause or enhance nonlinearity in the calibration curves of drugs and metabolites,thereby altering the relationship between analyte response and co.centration for ***,we established an evaluation scheme through a step-by-step dilution assay and employed three resolution methods:chromatographic separation,dilution,and stable labeled isotope internal standards *** above strategies were integrated into the method establishment process to improve quantitative accuracy.

关键词： Liquid chromatography-electrospray ionization tandem mass spectrometry(LCESI-MS) Drugs Metabolites Ionization interference Quantitative analysis

Influence of physical properties of carrier on the performance of dry powder inhalers

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Acta Pharmaceutica Sinica B 2016年第4期6卷 308-318页

作者： Tingting Peng Shiqi Lin Boyi Niu Xinyi Wang Ying Huang Xuejuan Zhang Ge Li Xin Pan Chuanbin Wu School of pharmaceutical Sciences Sun Yat-Sen University Guangzhou Neworld Pharm. co. Ltd. guangdong research Center for Drug Delivery Systems

Dry powder inhalers(DPIs) offer distinct advantages as a means of pulmonary drug delivery and have attracted much attention in the field of pharmaceutical science. DPIs co.monly co.tain micronized drug particles which, because of their co.esiveness and strong propensity to aggregate, have poor aerosolization performance. Thus carriers with a larger particle size are added to address this problem. However, the performance of DPIs is profoundly influenced by the physical properties of the carrier, particularly their particle size, morphology/shape and surface roughness. Because these factors are interdependent, it is difficult to co.pletely understand how they individually influence DPI *** purpose of this review is to summarize and illuminate how these factors affect drug–carrier interaction and influence the performance of DPIs.

关键词： Carrier Particle size Morphology Surface roughness Performance Dry powder inhaler

Ganoderma lucidum spore oil(GLSO),a novel antioxidant,extends the average life span in Drosophila melanogaster

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Food Science and Human Wellness 2021年第1期10卷 38-44页

作者： Yi Zhang Hongfei Cai Zhu Tao Cheng Yuan Zhaojian Jiang Juyan Liu Hiroshi Kurihara Wendong Xu institute of Integrated Chinese and Western Medicine Postdoctoral research Station Jinan UniversityGuangzhou 510632China Postdoctoral research Station of Guangzhou pharmaceutical Holdings Limited Guangdong 510130China institute of National Engineering research Center for Modernization of Extraction and Separation Process of Traditional Chinese Medicine Hanfang Pharmaceutical Co.LtdGuangdong 510240China Guangzhou pharmaceutical Holdings Ltd Guangdong 510130China institute of Traditional Chinese Medicine and Natural Products Jinan University601Huangpu Avenue WestGuangzhou510632China

In ancient China,Ganoderma lucidum was believed to be a medical fungus that co.ld increase ***,pharmaco.ogic studies have found that polysaccharide peptides and triterpenoids extracted from Ganoderma lucidum have various physiological effects as active ***,the effects of spore oil isolated from Ganoderma lucidum remains *** this study,the biological effects of Ganoderma lucidum spore oil(GLSO)were evaluated using a Drosophila melanogaster *** with untreated groups,groups treated with GLSO had significantly longer average and maximum lifespan in both normal co.ditions and under oxidative *** activities of various antioxidant enzymes were measured to determine the antioxidant effect of *** treatment markedly enhanced total superoxide dismutase(SOD)and catalase(CAT)activity and decreased levels of malondialdehyde(MDA).Further,we found dose-dependent increases in the mRNA expression of Cu,Zn-SOD,Mn-SOD,and CAT in GLSO-treated *** results suggest that GLSO may effectively eliminate free radicals and extend lifespan in *** work should investigate the value of GLSO as a functional food for the prevention of aging in larger animal models.

关键词： Ganoderma lucidum spore oil Antioxidant activity Drosophila melanogaster Anti-aging

Pt-co.single atom alloy catalysts: Accelerated water dissociation and hydrogen evolution by strain regulation

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Journal of Energy Chemistry 2022年第6期31卷 44-53,I0002页

作者： Rendian Wan Mi Luo Jingbo Wen Shilong Liu Xiongwu Kang Yong Tian School of Pharmacy Guangdong Pharmaceutical UniversityGuangzhou 510006GuangdongChina New Energy research institute School of Environment and EnergySouth China University of TechnologyHigher Education Mega CenterGuangzhou 510006GuangdongChina

The alkaline hydrogen evolution reaction(HER) on Pt-based catalysts is largely limited by the slow water dissociation kinetics. Pt-based single atom alloy catalysts(SAAC) with water dissociation sites have been demonstrated as excellent alkaline HER catalysts. However, the regulation of their activity and stability at the atomic scale is still a great challenge. Herein, the kinetic and stability issues are successfully resolved via engineering the electronic structure of Pt-co.SAAC by Au-induced tensile strain. The atomic dispersion of co.into the Pt shell was co.firmed by extended X-ray absorption fine structure and the electronic structure and catalytic HER performance was modulated by the tensile strain induced by the Pt shell thickness. An inverse volcano-type relation between HER activity and surface strain was *** functional theory(DFT) calculations reveal that the Au-induced tensile strain on Pt-co.shell can not only boost the adsorption and dissociation kinetics of water at co.site by upshifting the dband and promoting the electron transfer, but also downshift the d-band center of Pt in Pt-co.shell, leading to optimized H* adsorption/desorption. The champion catalyst provides an overpotential of only 14 m V at the current density of 10 mA cm^(-2). This work not only provides an effective strategy for the co.struction of single-atom alloy electrocatalysts for high performance toward alkaline HER but also sheds light on the understanding of the reaction mechanism at the atomic level.

关键词： Hydrogen evolution reaction Single atom alloy Strain DFT calculation d-band

Five new benzophenone glyco.ides from the leaves of Aquilaria sinensis(Lour.) Gilg

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Chinese Chemical Letters 2014年第12期25卷 1573-1576页

作者： Jian Sun Shu Wang Fang Xia Ke-Yuan Wang Jin-Ming Chen Peng-Fei Tu State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University Health Science Center Department of Medicinal Chemistry and pharmaceutical Analysis Logistics College of Chinese People's Armed Police Forces Taiji pharmaceutical research institute guangdong Junyuan pharmaceutical co Ltd.

Phytochemical investigation on the ethanol extract from the leaves of Aquitaria sinensis led to the isolation of five new benzophenone glyco.ides,aquilarinensides A-E（1-5）.Their structures were elucidated by a co.bi... 详细信息

关键词： Thymelaeaceae Aquilaria sinensis Benzophenone glyco.ides

research Progress on Prevention and Treatment of Gluco.ipid Metabolic Disease with Integrated Traditional Chinese and Western Medicine

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Chinese Journal of Integrative Medicine 2017年第6期23卷 403-409页

作者： GUO Jiao guangdong Metabolic Disease research Center of Integrated Chinese and Western Medicine guangdong Key Laboratory of Metabolic Disease Prevention and Treatment of Traditional Chinese Medicine Key Unit of Modulating Liver in Treating Hyperlipidemia SACM Institute of Traditional Chinese Medicine Research InstituteGuangdong Pharmaceutical UniversityGuangzhou 510006China

Hyperlipidemia, type 2 diabetes mellitus, nonalco.olic fatty liver and many other metabolic disorder are frequently co.existing in patients. In addition, these diseases are closely related in pathophysiological settings. However, increasing of the disease incidence, lacking of co.prehensive prevention and co.trol measurements against the key pathology point co.co.itant occurrence with the pattem of the single disease, single target therapy, that is leading therapeutic strategy for these metabolic disorders in the setting of Western medicine （WM）. On the basis of the co.bination of the advantages of integrated Chinese medicine （CM） and WM, with unified understanding of such diseases, the new co.cept of gluco.ipid metabolic disease （GLMD） is introduced. In this new co.cept, disorders in gluco.e and lipid metabolism are reco.nized as the key trigger and major driving force for the progress of GLMD. The key points of pathology included dysfunction of neuronal-endocrine-immune system,insulin resistance, oxidative stress, inflammation and intestinal flora imbalance. In the co.e pathogenic perspective of CM, it can be explained as ＂Gan （Liver） Shi Shu Xie＂（dysfunction of Gan in metabolism and emotion regulation） that will lead to the occurence/production of endogenous dampness and phlegm, blood stasis and turbid. This leads to the new co.cept of ＂Liver-based regulatory system for metabolic homeostasis＂ to be introduced further. The co.prehensive prevention and co.trol strategy ＂Tiao Gan Qi Shu Hua Zhuo＂（modulating Gan, trigging key metabolic system to resolve pathogenic factors such as phlegm retention and dampness）. Its representative formula Fufang Zhenzhu Tiaozhi Capsule （复方贞术调脂胶囊） is innovated under such rationales. co.ment for some co.monly-used CM GLMD therapeutic drugs was presented. High-level evidence-based and epidemiological and mechanism studies should be carded out to further interpret and explain of the scientific co.notation of GLMD.

关键词： gluco.ipid metabolic disease liver-based regulatory system for metabolic homeostasis Tiao Gan (Liver) Qi Shu Hua Zhuo (modulating Gan trigging key metabolic system to resolve pathogenic factors such as phlegm retention and dampness) Chinese medicine

Preparation and evaluation of sustained-release solid dispersions co.loading gastrodin with borneol as an oral brain-targeting enhancer

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Acta Pharmaceutica Sinica B 2014年第1期4卷 86-93页

作者： Zheng Cai Xiaolu Lei Zhufen Lin Jie Zhao Feizhen Wu Zhaoxiang Yang Junxue Pu Zhongqiu Liu School of pharmaceutical Sciences Southern Medical UniversityGuangzhou 510515China institute of pharmaceutical research Kunming Pharmaceutical Co.Kunming 650100China International institute for Translational Chinese Medicine Guangzhou University of Chinese MedicineGuangzhou 510006China

Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the ***,stomach irritation may occur when high doses of borneol are *** the present work,gastrodin,the main bioactive ingredient of the traditional Chinese drug“Tianma”(Rhizoma Gastrodiae)was used as a model drug to explore reasonable application of ***-release solid dispersions(SRSDs)for co.loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a *** dispersion state of drug within the SRSDs was analyzed by using scanning electron microsco.y,differential scanning calorimetry,and powder X-ray *** results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous *** of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi ***,gastric muco.a irritation and the brain targeting of the SRSDs were *** with the free mixture of gastrodin and borneol,brain targeting of SRSDs was slightly weaker(brain targeting index:1.83 vs.2.09),but stomach irritation obviously ***-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

关键词： Borneol Gastrodin Oral drug delivery Brain-targeting Gastric muco.a irritation Sustained-release