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The inhibition mechanism of the uptake of lamivudine via human organic anion transporter 1 by Stellera chamaejasme L. extracts

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Chinese Journal of Natural Medicines 2019年第9期17卷 682-689页

作者： PAN Lan-Ying zeng Kui LI Li LOU Yan zeng su Institute of Drug Metabolism and Pharmaceutical Analysis Zhejiang Province Key Laboratory of Anti-Cancer Drug ResearchCollege of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China Laboratory of Natural Medicine School of Forestry and Bio-technologyZhejiang A&F UniversityHangzhou 311300China The First Affiliated hospital College of MedicineZhejiang UniversityHangzhou 310000China

Stellera chamaejasme L.is a traditional Chinese medicine with a long history to treat stubborn skin ulcer,and it also has antiviral and antitumor effects.Neochamaejasmine B(NCB),Neochamaejasmine A(NCA)and Chamaechromone(CMC)are the major components in dried roots of Stellera chamaejasme L..Our studies suggested that NCB,NCA and CMC are inhibitors of Organic anion transporter 1(OAT1).OAT1 is encoded by solute carrier family 22 member 6 gene(SLC22 A6)in humans and plays a critical role in the organic anion drug uptake and excretion in the kidney.Lamivudine is the typical substrate of OAT1 and is frequently used in combination with other antiviral drugs in clinical antiviral treatments.The aim of this study is to investigate the interaction and its mechanism between these bi-flavone components in Stellera chamaejasme L.and lamivudine via OAT1 both in vitro and in vivo.In vitro,the uptake studies in Madin-Darby canine kidney(MDCK)cells overexpressing OAT1 suggested that NCB inhibited the uptake of 6-CFL and lamivudine.Similar results were obtained for NCA and CMC.NCB was a noncompetitive and competitive inhibitor interaction with OAT1.IC50 values of NCB,NCA and CMC for inhibiting OAT1-mediated lamivudine transport were 2.46,8.35 and 0.61μmol·L^–1,respectively.In vivo,the pharmacokinetic results of lamivudine in rats showed that the mean area under the plasma concentration-time curve(AUC0-∞)and maximal plasma concentration(Cmax)of lamivudine after co-administration is increased 2.94-fold and 1.87-fold,respectively,compared to lamivudine administration alone.The results of interactions between lamivudine and these bi-flavone components in Stellera chamaejasme L.extracts via OAT1 in vivo are consistent with studies in vitro.The inhibition of OAT1-mediated uptake of lamivudine by NCB,NCA and CMC is the possible mechanism for Stellera chamaejasme L.extracts improving the oral bioavailability of lamivudine in rats.

关键词： Lamivudine Neochamaejasmine B Neochamaejasmine A Chamaechromone OAT1 Inhibition

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浙江大学药学院四次停办的历史追溯

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高等药学教育研究 2024年第1期 80-85页

作者：曾苏浙江大学药学院浙江杭州310058

目的追溯浙江大学药学院四次停办的历史成因。方法查阅相关历史档案、文献和数据库,考证和分析关联性。结果1928年,由于政府整顿专门学校等原因,浙江公立医药专门学校停办;1931年,改组为浙江省立医药专科学校;1939年抗日战争期间,浙江... 详细信息

目的追溯浙江大学药学院四次停办的历史成因。方法查阅相关历史档案、文献和数据库,考证和分析关联性。结果1928年,由于政府整顿专门学校等原因,浙江公立医药专门学校停办;1931年,改组为浙江省立医药专科学校;1939年抗日战争期间,浙江高校迁往内地,为支持浙江省新办大学而停办,改组为英士大学医学院药学系;上世纪五十年代,国家两次高等院校院系调整,1952年,浙江大学理学院药学系停办,合并到上海医学院药学院;1955年,浙江医学院药学系停办,支援全国药学两院三系建设;1962年,国家自然灾害困难时期,浙江医科大学药学系停止招生。结论浙江大学药学院四次停办都有其历史的烙印,可供研究我国高等药学教育事业发展历史借鉴。

关键词：浙江大学药学院停办恢复办学

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The metabolism and hepatotoxicity of ginkgolic acid(17:1) in vitro

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Chinese Journal of Natural Medicines 2018年第11期16卷 829-837页

作者： YAO Qing-Qing LI Li XU Ming-Cheng HU Hai-Hong ZHOU Hui YU Lu-Shan zeng su Institute of Drug Metabolism and Pharmaceutical Analysis Zhejiang Province Key Laboratory of Anti-Cancer Drug Research College of Pharmaceutical Sciences Department of Pharmacy & Geriatrics Institute of Zhejiang Province Zhejiang Hospital

Pharmacological activities and adverse side effects of ginkgolic acids(GAs), major components in extracts from the leaves and seed coats of Ginkgo biloba L, have been intensively studied. However, there are few reports on their hepatotoxicity. In the present study, the metabolism and hepatotoxicity of GA(17:1), one of the most abundant components of GAs, were investigated. Kinetic analysis indicated that human and rat liver microsomes shared similar metabolic characteristics of GA(17:1) in phase I and II metabolisms. The drug-metabolizing enzymes involved in GA(17:1) metabolism were human CYP1 A2, CYP3 A4, UGT1 A6, UGT1 A9, and UGT2 B15, which were confirmed with an inhibition study of human liver microsomes and recombinant enzymes. The MTT assays indicated that the cytotoxicity of GA(17:1) in HepG2 cells occurred in a time-and dose-dependent manner. Further investigation showed that GA(17:1) had less cytotoxicity in primary rat hepatocytes than in HepG2 cells and that the toxicity was enhanced through CYP1 A-and CYP3 A-mediated metabolism.

关键词： Ginkgolic acid(17) Cytotoxicity Liver microsomes Recombinant enzyme Hepatotoxicity

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Screening and verifying potential NTCP inhibitors from herbal medicinal ingredients using the LLC-PK1 cell model stably expressing human NTCP

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Chinese Journal of Natural Medicines 2016年第7期14卷 549-560页

作者： SHEN Zhuo-Wei LUO Meng-Yue HU Hai-Hong ZHOU Hui JIANG Hui-Di YU Lu-Shan zeng su Institute of Drug Metabolism and Pharmaceutical Analysis Zhejiang Province Key Laboratory of Anti-Cancer Drug ResearchCollege of Pharmaceutical Sciences Zhejiang University

NTCP is specifically expressed on the basolateral membrane of hepatocytes, participating in the enterohepatic circulation of bile salts, especially conjugated bile salts, to maintain bile salts homeostasis. In addition, recent studies have found that NTCP is a functional receptor of HBV and HDV. Therefore, it is important to study the interaction between drugs and NTCP and identify the inhibitors/substrates of NTCP. In the present study, a LLC-PK1 cell model stably expressing human NTCP was established, which was simple and suitable for high throughput screening, and utilized to screen and verify the potential inhibitors of NTCP from 102 herbal medicinal ingredients. The results showed that ginkgolic acid(GA)(13 : 0), GA(15 : 1), GA(17 : 1), erythrosine B, silibinin, and emodin have inhibitory effects on NTCP uptake of TCNa in a concentration-dependent manner. Among them, GA(13 : 0) and GA(15 : 1) exhibited the stronger inhibitory effects, with IC_(50) values being less than 8.3 and 13.5 mmol·L^(-1), respectively, than the classical inhibitor, cyclosporin A(CsA)(IC_(50) = 20.33 mmol·L^(-1)). Further research demonstrated that GA(13 : 0), GA(15 : 1), GA(17 : 1), silibinin, and emodin were not substrates of NTCP. These findings might contribute to a better understanding of the disposition of the herbal ingredients in vivo, especially in biliary excretion.

关键词： Herbal medicinal ingredients Human NTCP Inhibitor Transport Biliary excretion

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Mechanism for ginkgolic acid(15：1)-induced MDCK cell necrosis： Mitochondria and lysosomes damages and cell cycle arrest

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Chinese Journal of Natural Medicines 2017年第5期15卷 375-383页

作者： YAO Qing-Qing LIU Zhen-Hua XU Ming-Cheng HU Hai-Hong ZHOU Hui JIANG Hui-Di YU Lu-Shan zeng su Institute of Drug Metabolism and Pharmaceutical Analysis Zhejiang Province Key Laboratory of Anti-Cancer Drug Research College of Pharmaceutical Sciences Zhejiang University Hangzhou 310058 China

Ginkgolic acids(GAs), primarily found in the leaves, nuts, and testa of ginkgo biloba, have been identified with suspected allergenic, genotoxic and cytotoxic properties. However, little information is available about GAs toxicity in kidneys and the underlying mechanism has not been thoroughly elucidated so far. Instead of GAs extract, the renal cytotoxicity of GA(15 : 1), which was isolated from the testa of Ginkgo biloba, was assessed in vitro by using MDCK cells. The action of GA(15 : 1) on cell viability was evaluated by the MTT and neutral red uptake assays. Compared with the control, the cytotoxicity of GA(15 : 1) on MDCK cells displayed a time-and dose-dependent manner, suggesting the cells mitochondria and lysosomes were damaged. It was confirmed that GA(15 : 1) resulted in the loss of cells mitochondrial trans-membrane potential(ΔΨm). In propidium iodide(PI) staining analysis, GA(15 : 1) induced cell cycle arrest at the G0/G1 and G2/M phases, influencing on the DNA synthesis and cell mitosis. Characteristics of necrotic cell death were observed in MDCK cells at the experimental conditions, as a result of DNA agarose gel electrophoresis and morphological observation of MDCK cells. In conclusion, these findings might provide useful information for a better understanding of the GA(15 : 1) induced renal toxicity.

关键词： Ginkgolic acids(15) Cytotoxicity Mechanism Necrosis

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新型生物活性玻璃对乳牙根尖周炎常见细菌抗菌效果评价

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上海口腔医学 2024年第1期33卷 49-53页

作者：方颖黄文燕苗国厚孟斯彭博曾素娟广州医科大学附属口腔医院儿童口腔科广东省口腔组织修复与重建工程技术研究中心广州市口腔再生医学基础与应用研究重点实验室广东广州510182 广州医科大学附属口腔医院广东省口腔组织修复与重建工程技术研究中心广州市口腔再生医学基础与应用研究重点实验室广东广州510182

目的:研究不同浓度新型生物活性玻璃(bioactive glass,BG)对乳牙根尖周炎常见细菌的抗菌效果。方法 :采用纸片扩散法检测并观察新型BG处理粪肠球菌、牙龈卟啉单胞菌和具核梭杆菌后形成的抑菌环直径(mm),同时测定粪肠球菌、牙龈卟啉单胞... 详细信息

目的:研究不同浓度新型生物活性玻璃(bioactive glass,BG)对乳牙根尖周炎常见细菌的抗菌效果。方法 :采用纸片扩散法检测并观察新型BG处理粪肠球菌、牙龈卟啉单胞菌和具核梭杆菌后形成的抑菌环直径(mm),同时测定粪肠球菌、牙龈卟啉单胞菌和具核梭杆菌的最小抑菌浓度(minimal inhibitory concentration,MIC)、最小杀菌浓度(minimal bactericidal concentration,MBC)和最小菌斑清除浓度(minimal biofilm eradication concentration,MBEC),20、40、60、80 mg/mL新型BG处理3种菌的混合菌斑24 h,于激光共聚焦显微镜(confocal laser scanning microscopy,CLSM)下摄片观察新型BG对混合菌斑的抑菌效果。采用GraphPad Prism 10.0软件对数据进行统计学分析。结果:新型BG对乳牙根尖周炎常见细菌显示出很强的抗菌潜力;新型BG对菌斑的MBEC显著大于对粪肠球菌、牙龈卟啉单胞菌和具核梭杆菌的MIC和MBC。随着新型BG浓度加大,混合菌斑死菌数量显著增加,与空白对照组有显著差异(P<0.05)。结论:新型BG对乳牙根尖周炎常见细菌粪肠球菌、牙龈卟啉单胞菌和具核梭杆菌具有显著抗菌功效。

关键词：生物活性玻璃粪肠球菌牙龈卟啉单胞菌具核梭杆菌抗菌效果

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Current developments of bioanalytical sample preparation techniques in pharmaceuticals

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Journal of Pharmaceutical Analysis 2022年第4期12卷 517-529页

作者： Rahul G.Ingle su zeng Huidi Jiang Wei-Jie Fang Institute of Drug Metabolism and Pharmaceutical Analysis College of Pharmaceutical SciencesZhejiang UniversityHangzhou310058China Hangzhou Institute of Innovative Medicine Zhejiang UniversityHangzhou310016China

Sample preparation is considered as the bottleneck step in bioanalysis because each biological matrix has its own unique challenges and complexity.Competent sample preparation to extract the desired analytes and remove redundant components is a crucial step in each bioanalytical approach.The matrix effect is a key hurdle in bioanalytical sample preparation,which has gained extensive consideration.Novel sample preparation techniques have advantages over classical techniques in terms of accuracy,automation,ease of sample preparation,storage,and shipment and have become increasingly popular over the past decade.Our objective is to provide a broad outline of current developments in various bioanalytical sample preparation techniques in chromatographic and spectroscopic examinations.In addition,how these techniques have gained considerable attention over the past decade in bioanalytical research is mentioned with preferred examples.Modern trends in bioanalytical sample preparation techniques,including sorbent-based microextraction techniques,are primarily emphasized.

关键词： Bioanalysis Biological matrices Matrix effect Microextraction Sample preparationtechnique

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Potential use of a dried saliva spot(DSS)in therapeutic drug monitoring and disease diagnosis

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Journal of Pharmaceutical Analysis 2022年第6期12卷 815-823页

作者： Yu Han Xi-Ling Li Minghui Zhang Jing Wang su zeng Jun Zhe Min Key Laboratory of Natural Medicines of the Changbai Mountain Ministry of EducationDepartment of Pharmaceutical AnalysisCollege of PharmacyYanbian UniversityYanjiJilin133002China Institute of Drug Metabolism and Pharmaceutical Analysis Zhejiang Province Key Laboratory of Anti-Cancer Drug ResearchCollege of Pharmaceutical SciencesZhejiang UniversityHangzhou310058China

In recent years,scientific researchers have increasingly become interested in noninvasive sampling methods for therapeutic drug monitoring and disease diagnosis.As a result,dried saliva spot(DSS),which is a sampling technique for collecting dried saliva samples,has been widely used as an alternative matrix to serum for the detection of target molecules.Coupling the DSS method with a highly sensitive detection instrument improves the efficiency of the preparation and analysis of biological samples.Furthermore,dried blood spots,dried plasma spots,and dried matrix spots,which are similar to those of the DSS method,are discussed.Compared with alternative biological fluids used in dried spot methods,including serum,tears,urine,and plasma,saliva has the advantage of convenience in terms of sample collection from children or persons with disabilities.This review aims to provide integral strategies and guidelines for dried spot methods to analyze biological samples by illustrating several dried spot methods.Herein,we summarize recent advancements in DSS methods from June 2014 to March 2021 and discuss the advantages and disadvantages of the key aspects of this method,including sample preparation and method validation.Finally,we outline the challenges and prospects of such methods in practical applications.

关键词： Human saliva Dried saliva spot Therapeutic drug monitoring Disease diagnosis

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多参数MRI组学列线图模型预测子宫内膜样腺癌淋巴血管间隙侵犯

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复旦学报（医学版） 2024年第3期51卷 306-314,322页

作者：马晓亮沈敏花马凤华张国福周建军曾蒙苏强金伟复旦大学附属中山医院放射科上海200032 复旦大学附属妇产科医院放射科上海200090 复旦大学附属金山医院放射科上海200540

目的分析多参数磁共振成像(magnetic resonance imaging,MRI)组学列线图模型治疗前预测子宫内膜样腺癌(endometrial endometrioid adenocarcinoma,EEA)淋巴血管间隙侵犯(lymphovascular space invasion,LVSI)的可行性及价值。方法于2020年10月至2022年1月在复旦大学附属妇产科医院前瞻性收集205例EEA临床及MRI资料,按6∶4随机分为训练集(n=123)和验证集(n=82)。分别在T2加权成像、扩散加权成像(表观扩散系数图)及动态增强MRI序列勾画全肿瘤体积感兴趣区提取肿瘤影像组学特征。在训练集中,采用单变量分析及多变量Logistic回归分析筛选LVSI的独立预测因子,建立临床预测模型;采用最小绝对收缩和选择算法(least absolute shrinkage and selection operator,LASSO)进行特征筛选并建立影像组学标签;采用临床独立预测因子与组学标签构建临床-MRI组学列线图模型,并在验证集中进行模型验证。使用受试者操作特征曲线下面积(area under the receiver operating characteristic curve,AUC)评估模型效能,临床决策曲线评估模型临床应用价值。结果205例EEA中,LVSI(-)144例,LVSI(+)61例。患者绝经状态、CA125及CA199为LVSI(+)的临床独立预测因子,三者联合组成的临床预测模型AUC为0.714(训练集)和0.731(验证集)。从多参数MRI图像中共提取的8240个影像组学特征中筛选出5个最佳特征构建MRI组学标签,AUC为0.860(训练集)和0.759(验证集)。临床-MRI组学列线图模型AUC为0.887(训练集)和0.807(验证集),优于单独的临床模型及组学模型,且在较大的阈值概率范围内临床-MRI组学列线图模型可获得更大的临床净收益。结论基于多参数MRI组学的列线图模型可在治疗前有效预测EEA的LVSI状态,为临床管理决策提供有价值的参考,提高患者的临床获益。

关键词：影像组学磁共振成像子宫内膜癌淋巴血管间隙侵犯列线图

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Low-Rank Optimal Transport for Robust Domain Adaptation

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IEEE/CAA Journal of Automatica Sinica 2024年第7期11卷 1667-1680页

作者： Bingrong Xu Jianhua Yin Cheng Lian Yixin su Zhigang zeng IEEE the School of Automation Wuhan University of TechnologyWuhan 430070China Intelligent Transportation Systems Research Center Wuhan University of TechnologyWuhan 430063 Chongqing Research Institute Wuhan University of TechnologyChongqingChina the School of Artificial Intelligence and Automation Huazhong University of Science and TechnologyWuhan 430074 the Key Laboratory of Image Processing and Intelligent Control of Education Ministry of China Wuhan 430074China

When encountering the distribution shift between the source(training) and target(test) domains, domain adaptation attempts to adjust the classifiers to be capable of dealing with different domains. Previous domain adaptation research has achieved a lot of success both in theory and practice under the assumption that all the examples in the source domain are welllabeled and of high quality. However, the methods consistently lose robustness in noisy settings where data from the source domain have corrupted labels or features which is common in reality. Therefore, robust domain adaptation has been introduced to deal with such problems. In this paper, we attempt to solve two interrelated problems with robust domain adaptation:distribution shift across domains and sample noises of the source domain. To disentangle these challenges, an optimal transport approach with low-rank constraints is applied to guide the domain adaptation model training process to avoid noisy information influence. For the domain shift problem, the optimal transport mechanism can learn the joint data representations between the source and target domains using a measurement of discrepancy and preserve the discriminative information. The rank constraint on the transport matrix can help recover the corrupted subspace structures and eliminate the noise to some extent when dealing with corrupted source data. The solution to this relaxed and regularized optimal transport framework is a convex optimization problem that can be solved using the Augmented Lagrange Multiplier method, whose convergence can be mathematically proved. The effectiveness of the proposed method is evaluated through extensive experiments on both synthetic and real-world datasets.

关键词： Domain adaptation low-rank constraint noise corruption optimal transport

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