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Liquid chromatography/tandem mass spectrometry method for quantitative estimation of solutol HS15 and its applications

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Journal of Pharmaceutical Analysis 2015年第2期5卷 120-129页

作者： V.Vijaya Bhaskar Anil Middha Pratima Srivastava Sriram Rajagopal dmpk Laboratory (Biology Division) GVK BIO department of Pharmacy Jagadishprasad Jhabermal Tibrewala University

A rapid, sensitive and selective pseudo MRM（p MRM）-based method for the determination of solutol HS15（SHS15） in rat plasma was developed using liquid chromatography/tandem mass spectrometry（LC–MS/MS）. The most abundant ions corresponding to SHS15 free polyethyleneglycol（PEG）oligomers at m/z 481, 525, 569, 613, 657, 701, 745, 789, 833, 877, 921 and 965 were selected for p MRM in electrospray mode of ionization. Purity of the lipophilic and hydrophilic components of SHS15 was estimated using evaporative light scattering detector（ELSD）. Plasma concentrations of SHS15 were measured after oral administration at 2.50 g/kg dose and intravenous administration at 1.00 g/kg dose in male Sprague Dawley rats. SHS15 has poor oral bioavailability of 13.74% in rats. Differences in pharmacokinetics of oligomers were studied. A novel proposal was conveyed to the scientific community,where formulation excipient could be analyzed as a qualifier in the analysis of new chemical entities（NCEs） to address the spiky plasma concentration profiles.

关键词： SHS15 LC–MS/MS Spiky profiles Validation

Identification of human cytochrome P450 and UGT enzymes involved in the metabolism of ferulic acid, a major bioactive component in traditional Chinese medicines

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Chinese Journal of Natural Medicines 2017年第9期15卷 695-702页

作者： ZHUANG Xiao-Mei CHEN Lin TAN Yan YANG Hai-Ying LU Chuang GAO Yue LI Hua State Key Laboratory of Toxicology and Medical Countermeasures Beijing Institute of Pharmacology and Toxicology Beijing100850 China Institute of Radiation Medicine Beijing 100850 China Department of DMPK Biogen USA

Ferulic acid(FA) is an active component of herbal medicines. One of the best documented activities of FA is its antioxidant property. Moreover, FA exerts antiallergic, anti-inflammatory, and hepatoprotective effects. However, the metabolic pathways of FA in humans remain unclear. To identify whether human CYP or UGT enzymes are involved in the metabolism of FA, reaction phenotyping of FA was conducted using major CYP-selective chemical inhibitors together with individual CYP and UGT Supersomes. The CYPand/or UGT-mediated metabolism kinetics were examined simultaneously or individually. Relative activity factor and total normalized rate approaches were used to assess the relative contributions of each major human CYPs towards the FA metabolism. Incubations of FA with human liver microsomes(HLM) displayed NADPH-and UDPGA-dependent metabolism with multiple CYP and UGT isoforms involved. CYPs and UGTs contributed equally to the metabolism of FA in HLM. Although CYP1 A2 and CYP3 A4 appeared to be the major contributors in the CYP-mediated clearance, their contributions to the overall clearance are still minor(< 25%). As a constitute of many food and herbs, FA poses low drug-drug interaction risk when co-administrated with other herbs or conventional medicines because multiple phase I and phase II enzymes are involved in its metabolism.

关键词： Ferulic 酸植物药相互作用反应 phenotyping 人的肝微体

High degree of pharmacokinetic compatibility exists between the five-herb medicine XueBiJing and antibiotics comedicated in sepsis care

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Acta Pharmaceutica Sinica B 2019年第5期9卷 1035-1049页

作者： Jian Li Olajide E.Olaleye Xuan Yu Weiwei Jia Junling Yang Chuang Lu Songqiao Liu Jingjing Yu Xiaona Duan Yaya Wanga Kai Dong Rongrong He Chen Cheng Chuan Li State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences University of Chinese Academy of Sciences Department of DMPK department of Critical Care Medicine Zhongda HospitalSchool of MedicineSoutheast University School of Pharmacy University of Washington Tianjin Chasesun Pharmaceutical Co.Ltd.

Managing the dysregulated host response to infection remains a major challenge in sepsis care. Chinese treatment guideline recommends adding Xue Bi Jing, a five-herb medicine, to antibioticbased sepsis care. Although adding Xue Bi Jing further reduced 28-day mortality via modulating the host response, pharmacokinetic herbedrug interaction is a widely recognized issue that needs to be studied.Building on our earlier systematic chemical and human pharmacokinetic investigations of Xue Bi Jing, we evaluated the degree of pharmacokinetic compatibility for Xue Bi Jing/antibiotic combination based on mechanistic evidence of interaction risk. Considering both Xue Bi Jing-antibiotic and antibiotic-Xue Bi Jing interaction potential, we integrated informatics-based approach with experimental approach and developed a compound pair-based method for data processing. To reflect clinical reality, we selected for study Xue Bi Jing compounds bioavailable for drug interactions and 45 antibiotics commonly used in sepsis care in China. Based on the data of interacting with drug metabolizing enzymes and transporters, no Xue Bi Jing compound could pair, as perpetrator, with the antibiotics. Although some antibiotics could,due to their inhibition of uridine 50-diphosphoglucuronosyltransferase 2 B15, organic anion transporters1/2 and/or organic anion-transporting polypeptide 1 B3, pair with senkyunolide I, tanshinol and salvianolic acid B, the potential interactions(resulting in increased exposure) are likely desirable due to these Xue Bi Jing compounds’ low baseline exposure levels. Inhibition of aldehyde dehydrogenase by 7 antibiotics probably results in undesirable reduction of exposure to protocatechuic acid from Xue Bi Jing.Collectively, Xue Bi Jing/antibiotic combination exhibited a high degree of pharmacokinetic compatibility at clinically relevant doses. The methodology developed can be applied to investigate other drug combinations.

关键词： XueBiJing Antibiotic Combination drug therapy Sepsis Pharmacokinetic compatibility Herb-drug interaction

New Convenient Synthesis of 8-C-Methylated Homoisoflavones and Analysis of Their Structure by NMR and Tandem Mass Spectrometry

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International Journal of Organic Chemistry 2021年第1期11卷 46-54页

作者： Santosh Kumar Yadav department of Organic Chemistry & FDW Andhra University Visakhapatnam India dmpk Sai Life Sciences Ltd. Pune Maharashtra India

Homoisoflavonoids are in the subclass of the larger family of flavonoids having one more alkyl carbon than flavonoids. Among them, 8-C-Methylated homoisoflavones have not been extensively studied for synthesis and biological evaluation. Author’s current objective is to synthesize 8-C-Methylated homoisoflavones by the reaction of 3-C-methylated dihydrochalcones with N,N’-dimethyl (chloromethylene) ammonium chloride generated in situ from DMF and PCl5 for one carbon extension at about room temperature. The 3-C-methylated dihydrochalcones were synthesized by the reduction of 3-C-methylated chalcones, which were prepared from 3-C-methylated acetophenones and aromatic aldehydes in the presence of base. All the synthesized novel homoisoflavones’s structures were characterized by NMR and Tandem Mass Spectrometry.

关键词： 8-C-Methylated Homoisoflavones 3-C-Methylated Dihydrochalcones 3-C-Methylated Chalcones 3-C-Methylated Acetophenones Dimethylformamide BF3·Et2O PCl5

静脉注射给药的甘草酸易在由肝转运体OATP1B1/OATP1B3介导的药物相互作用中成为被影响药物

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中国临床药理学与治疗学 2020年第4期25卷 364-365页

作者：董佳佳 Olajide EOlaleye 姜蓉嵘李静吕闯杜飞飞徐方杨军令王凤清贾伟伟李川中国科学院上海药物研究所新药研究国家重点实验室中国上海201203 中国科学院大学中国北京100049 Department of DMPK SanofiCambridge美国MA 02451

随意使用天然产品可能严重干扰患者正在接受的化药治疗,此已引起国际广泛关注。中西医结合治疗疾病在中国很普遍,研究中药与化药合用时发生药代性质药物相互作用风险,对于保证临床用药的有效性和安全性十分重要。不同于美英等西方国家,... 详细信息

随意使用天然产品可能严重干扰患者正在接受的化药治疗,此已引起国际广泛关注。中西医结合治疗疾病在中国很普遍,研究中药与化药合用时发生药代性质药物相互作用风险,对于保证临床用药的有效性和安全性十分重要。不同于美英等西方国家,中国将中药作为药物来监管和使用,因此研究中药与化药合用的风险既涉及“中药影响化药”,也涉及“化药影响中药”。国际上围绕化药影响天然产物制品的研究还很少,这是因为与健康相关的天然产物制品在西方国家通常不具备药物身份,缺乏相应的药代动力学研究和技术。研究“化药影响中药”的风险首先应明确成分体内暴露改变能够影响中药的有效性或安全性,其重点是要搞清楚与化药合用能否通过某种机制改变这些中药成分的体内暴露。

关键词： AUC 静脉注射给药 OATP1B1/OATP1B3 甘草酸

血必净注射液联合抗生素治疗脓毒症:两类药物间高水平药代和谐

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中国临床药理学与治疗学 2020年第4期25卷 361-363页

作者：李坚 Olajide EOlaleye 余玄贾伟伟杨军令吕闯刘松桥于晶晶段小娜王亚亚董凯贺容容程晨李川中国科学院上海药物研究所新药研究国家重点实验室中国上海201203 中国科学院大学中国北京100049 Department of DMPK SanofiWaltham美国MA 02451 东南大学医学院附属中大医院中国江苏南京210009 School of Pharmacy University of WashingtonSeattle美国WA 98105 天津红日药业股份有限公司中国天津301700

联合用药既需要药物间药效协同互补,也需要药物间能够“药代和谐”(pharmacokinetic compatibility,PKC;不发生会影响药物有效性或安全性的药代性质药物相互作用)。当今世界天然产物制品与化药一同使用既大量存在,又充满争议。一方面,... 详细信息

联合用药既需要药物间药效协同互补,也需要药物间能够“药代和谐”(pharmacokinetic compatibility,PKC;不发生会影响药物有效性或安全性的药代性质药物相互作用)。当今世界天然产物制品与化药一同使用既大量存在,又充满争议。一方面,服用葡萄柚汁、圣约翰草制剂等能严重干扰同时进行的化药治疗,这使人们对天然产物制品与化药合用充满戒心;另一方面,越来越多严格的临床和基础研究证明,中药联合化药能更好地应对多因素疾病。脓毒症是一种由感染引起机体反应失调所导致危及生命的器官功能障碍,死亡率高、预后不良。

关键词：抗生素治疗天然产物联合用药注射液

Probing the Kinematic Signatures of Planet Formation in the Gas Disk of MWC 480

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Research in Astronomy and Astrophysics 2024年第6期24卷 112-120页

作者： Min Zhao Haochuan Yu Zhengxiang Li department of Astronomy Beijing Normal University Sub-department of Astrophysics Department of Physics University of Oxford

The disk around MWC 480 has shown multiple substructures in both dust and gas observations, possibly suggesting ongoing planet formation in situ. In this paper, we explore the gas kinematics of the MWC 480 disk by analyzing the archival Atacama Large Millimeter/submillimeter Array observations of12CO(J = 2-1),13CO(J = 2-1), and C18O(J = 2-1). By modeling the line-of-sight velocities, inferred from the Doppler shifts of the emission lines, we are able to decompose the three-dimensional(3D) velocity field of the disk into rotational,radial, and vertical components. Further analysis reveals the presence of large-scale gas flows in the(r, z) plane.Notably, we identify potential meridional flows across various heights as traced by all three CO isotopologues in the 80–120 au region, possibly associated with ongoing planet formation activities in this region. Moreover, we find upward flows near 200 au for all three CO isotopologues, which may point to the presence of disk winds.

关键词： planet-disk interactions planet-star interactions protoplanetary disks

Imaging mass spectrometry: a molecular microscope for studying the role of lipids in Parkinson's disease

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Neural Regeneration Research 2024年第6期19卷 1179-1180页

作者： Vinata Vedam-Mai Jacob M.Samuel Boone M.Prentice department of Neurology University of Florida department of Chemistry University of Florida

Parkinson’s disease–A lipidopathy? The histopathological hallmark of Parkinson’s disease(PD) and dementia with Lewy bodies are inclusions enriched in α-synuclein(α-syn), known as Lewy bodies, which are not only composed of proteins, but also a core of lipid species. PD has been thus far principally thought of as a “proteinopathy” caused by the misfolding of α-syn. However,

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Composites with high omnidirectional fracture toughness due to helical interlocking fasteners are found in gingko seed shells

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National Science Review 2023年第5期10卷 106-108页

作者： Nicholas A.Kotov department of Chemical Engineering Biointerfaces InstituteDepartment of Materials Science and EngineeringUniversity of Michigan department of Aeronautics Imperial College London

Engineering of composites mimicking load-bearing materials from living organisms is essential for sustainable economic development and successful resolution of current and future bottle-necks of chemical,automotive,av... 详细信息

关键词： POLYELECTROLYTE COMPOSITES