pentacyclic triterpene杀马特是什么意思思

中国药科大学药学院药物化学孙宏斌教授、博士生导师
孙宏斌 ,男, 1966 年 12 月出生,教授、博士生导师。现任中国药科大学新药研究中心主任、 江苏省药学会药物化学专业委员会副主任委员、 中国药科大学校学位评定委员会和学术委员会委员、江苏省药品监督管理局新药审评专家。担任 Recent Patents on Anti-Ca
孙宏斌,男,1966年12月出生,教授、博士生导师。现任中国药科大学新药研究中心主任、江苏省药学会药物化学专业委员会副主任委员、中国药科大学校学位评定委员会和学术委员会委员、江苏省药品监督管理局新药审评专家。担任&Recent Patents on Anti-Cancer Drug Discovery& (SCI期刊)地区编委、&Drug Discoveries & Therapeutics&、&中国药物化学杂志&、&药物化学进展&(丛书)和&中国药科大学学报&编委。
&&&&&&&& 1989年毕业于吉林大学化学系获理学学士学位,同年考取中国药科大学药物化学专业研究生,并于1995年获得理学博士学位。年在中科院上海有机化学研究所从事博士后研究;年在德国亚琛工业大学有机化学研究所从事博士后研究;年在美国佛罗里达大学化学系做访问学者;年在美国加州Metabolex公司任新药研发科学家,其间所参与研制的I类抗糖尿病新药MBX-2044已进入II期临床研究阶段。2003年8月回国任中国药科大学教授,2005起年任中国药科大学新药研究中心主任,2008年10月兼任法国Cachan高等师范学院Visiting Professor.
&&&& 目前主要从事药物化学、有机合成化学和新药研究,研究内容包括&基于天然产物的新药发现&和&药物再发现&导向的创新药物研究。以类天然产物库的构建、活性评价、多靶点机制研究和成药性研究为主线,开展了五环三萜、生物碱、前列腺素和脱氧果糖等天然产物的合成及结构修饰研究,获得了1000 多个化合物,并从中筛选出抗脑缺血候选新药MA。此外,基于&药物再发现&策略所研制的抗血栓新药SJQ-1已进入临床前研究阶段。在国内外期刊发表论文110多篇,其中SCI论文55篇,单篇最高影响因子为9.2;申请专利36项,其中6项获授权;参编著作3部。自2003年回国以来,已培养毕业博士生11人,其中1人获2009年度中国药学会-施维雅青年药物化学奖,并获得全国优秀博士论文提名论文奖;毕业硕士生12人。目前承担博士生课程《药物立体化学》、硕士生课程《药物化学选论》和本科生课程《药物设计》的教学工作。
主要奖励、荣誉
教育部&新世纪优秀人才&(2005年);
中国药学会&施维雅青年药物化学奖&(2006年);
EFSD(European Foundation for the Study of Diabetes) Grant Awardsfor Collaborative DiabetesResearch between China and Europe(2007年);
江苏省&333高层次人才培养工程&首批中青年科学技术带头人(2007年);
江苏省 &六大人才高峰&计划(A类)(2005年);
&&Bioorganic and Medicinal Chemistry Letters& Most Cited Paper
Award(2009年)。
近年主持的科研基金和人才计划项目
&国家自然科学基金面上项目(No.);
&国家&重大新药创制&科技重大专项(候选药物)(No.-093);
&2007年度&欧洲糖尿病研究基金&(EFSD)(由施贵宝公司资助);
&国家自然科学基金重大研究计划(培育项目)(No.);
&国家自然科学基金面上项目(No.);
&教育部科技创新工程重大项目培育基金(No.706030);
&教育部&2005年度新世纪优秀人才&支持计划(No.NCET-05-0495);
&高等学校博士学科点专项科研基金(No.);
&江苏省自然科学基金(No.BK2005101);
&中国与匈牙利政府间科技合作项目(No.CHN-7/2006)。
近年代表性论文
1.Huaming Sheng, Hongbin Sun.* Synthesis, Biology and Clinical Significance of Pentacyclic Triterpenes: a Multi-target Approach to Prevention and Treatment of Metabolic and Vascular Diseases. Natural Product Reports 2011, 28, 543-593. (IF 9.202)
2.Zhangyu Yao, Xueying Wei, Xiaoming Wu, Jonathan L. Katz, Theresa Kopajtic, Nigel H. Greig, Hongbin Sun.*Preparation and Evaluation of Tetrabenazine Enantiomers and All Eight Stereoisomers of Dihydrotetrabenazine as VMAT2 Inhibitors. European Journal of Medicinal Chemistry2011, 46, 1841 (IF 3.269)
3.Zhongjie Liang, Liying Zhang, Lianchun Li, Jun Liu, Honglin Li, Luyong Zhang,Keguang Cheng, Xiaoan Wen, Pu Zhang, Jia Hao, Yanchun Gong, Xia Zhang, Jun Chen, Hong Liu, Cheng Luo, Hualiang Jiang,Hongbin Sun.* Pentacyclic Triterpenes Derivatives as Potent Inhibitors against Glycogen Phosphorylase: the Receptor-Based 3D-QSAR Guided Inhibitor Optimization. European Journal of Medicinal Chemistry 2011, 46, . (IF 3.269)
4.Yong Wu, Chen Shi, Xiaowei Sun, Xiaoming Wu, Hongbin Sun.* Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3& site of rennin.Bioorganic & Medicinal Chemistry2011 (IF 3.108), 19, .
5.Yanchun Gong, Sandrine Peyrat, Hongbin Sun, Juan Xie. Synthesis of nucleoside aminooxy acids. Tetrahedron 2011(IF 3.011), 67, .
6.Pu Zhang, Li Xu, Keduo Qian, Jun Liu, Luyong Zhang, Kuo-Hsiung Lee, Hongbin Sun.* Efficient synthesis and biological evaluation of epiceanothic acid and related compounds. Bioorganic & Medicinal Chemistry Letters 2011, 21, 338-341. (IF 2.65)
7.Jun Xia , Jianfei Song, Le Zhen, Xiuling Zhang, Xiantao Lei, Lina Zheng, Qiujuan Wang, Hongbin Sun.* Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists. Bioorganic & Medicinal Chemistry Letters 2011, 21, . (IF 2.65)
8.Li Xu, Hongbin Sun.* Pharmacological Manipulation of Brain Glycogenolysis as a Therapeutic Approach to Cerebral Ischemia. Mini Review in Medicinal Chemistry10, 1188-93. (IF 3.06)
9.Jun Liu, Ting He, Qian Lu, Jing Shang,Hongbin Sun,* Luyong Zhang. Asiatic acid preserves beta mass and mitigates hyperglycemia in streptozocin-induced diabetic rats. Diabetes Metabolism Research and Reviews2010, 26, 448-454 (IF 2.762)
10.Keguang Cheng, Jun Liu, Hongbin Sun,*, 34, 1-15. (IF 2.937)&
11.Keguang Cheng,Jun Liu, Hongbin Sun, Juan Xie. Synthesis of nucleoside conjugates as potential inhibitors of glycogen phosphorylase. Synthesis, 2010, 6,
(IF 2.447) &
12.Huaming Sheng, Ben Niu, Hongbin Sun.*Metabolic targeting of cancers: from molecular mechanisms to therapeutic strategies. Current Medicinal Chemistry 2009, 16, . (IF 4.708)
13.Jia Hao, Xueli Zhang, Pu Zhang, Jun Liu, Luyong Zhang, Hongbin Sun.* Efficient Access to Isomeric 2, 3-Dihydroxy Lupanes: First Synthesis of Alphitolic Acid. Tetrahedron 2009, 65,
(IF 3.219)
14.Pu Zhang, Jia Hao, Jun Liu, Qian Lu, Huaming Sheng, Luyong Zhang,Hongbin Sun.*Synthesis and biological evaluation of 3-deoxy-pentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. Journal of Natural Products2009, 72,
(IF 3.159)
15.Yanchun Gong, Hongbin Sun, Juan Xie. Synthesis of oligosaccharide mimetics with glycoaminoxy acids. European Journal of Organic Chemistry 2009, 34, (IF 3.016) .
16.Pu Zhang, Jia Hao, Jun Liu, Luyong Zhang, Hongbin Sun.* Efficient synthesis of morolic acid and related triterpenes starting from betulin. Tetrahedron 2009, 65, . (IF 3.219)
17.Xiaoan Wen, Hongbin Sun,* Jun Liu, et al. Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships and X-ray Crystallographic Studies. Journal of Medicinal Chemistry 2008, 51, . (IF 4.802)
18.Jia Hao, Pu Zhang, Xiaoan Wen, Hongbin Sun.* Efficient Access to 2-Isobetulinic Acid, 2-Isooleanolic Acid and 2-Isoursolic Acid. Journal of Organic Chemistry 2008, 73, . (IF 4.219)
19.Keguang Cheng, Pu Zhang, Jun Liu, Juan Xie, Hongbin Sun.* Practical Synthesis of Bredemolic Acid, a Natural Inhibitor of Glycogen Phosphorylase. Journal of Natural Products2008, 71, . (IF 3.159)
20.Xiaoan Wen, Pu Zhang, Jun Liu, Luyong Zhang, Xiaoming Wu, Peizhou Ni, Hongbin Sun.*(IF 2.65) (&Bioorganic and Medicinal Chemistry Letters& Most Cited Paper
Award) Pentacyclic Triterpenes. Part 2: Synthesis and biological activity of maslinic acid derivatives as inhibitors of glycogen phosphorylase. Bioorganic & Medicinal Chemistry Letters 2006, 16, 722-726.
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):1135-46. doi: 10.-011-3467-0. Epub
2011 Jul 22.A new Bacillus megaterium whole-cell catalyst for the hydroxylation of the pentacyclic triterpene 11-keto-β-boswellic acid (KBA) based on a recombinant cytochrome P450 system.1, , , , , .1Department of Biochemistry, Saarland University, Campus, B 2.2, 66123 Saarbrücken, Germany.AbstractThe use of cytochromes P450 for the regio- and stereoselective hydroxylation of non-activated carbon atoms in biotechnological applications reflects an efficient and cost-effective alternative in comparison to classical organic chemistry. The prokaryotic cytochrome P450 CYP106A2 from Bacillus megaterium ATCC 13368 hydroxylates a variety of 3-oxo-Δ? steroids and recently it was identified to carry out a one-step regioselective allylic hydroxylation of the diterpene abietic acid. The anti-inflammatory pentacyclic triterpene 11-keto-β-boswellic acid (KBA) was found to be a further substrate of CYP106A2, being the first report of a pentacyclic triterpene conversion by a prokaryotic P450. The reaction products were analyzed by HPLC and the corresponding kinetic parameters were investigated. Structure determination of the main product by NMR revealed a 15α-hydroxylation of this substrate. In order to overcome the inability of a recombinant P450 whole-cell system in E. coli for the uptake of acids with terpene structure, we developed for the first time an expression system for cytochromes P450 in B. megaterium (strains MS941 and ATCC 13368). Interestingly, CYP106A2 was only successfully expressed in the plasmid-less B. megaterium strain MS941 but not in ATCC13368. This recombinant system, with the co-expressed heterologous redox chain of the P450, bovine adrenodoxin reductase (AdR), and bovine adrenodoxin (Adx), was applied for the whole-cell conversion of KBA. The formation of 15α-hydroxy-KBA was increased 15-fold in comparison with the naturally CYP106A2-expressing B. megaterium strain ATCC 13368.PMID:
[PubMed - indexed for MEDLINE]
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Wu K J, Chen Q L, He C H*. Speed of sound of ionic Liquids: database, estimation, and its application for thermal conductivity prediction, AIChE J, ): .
Chen D X, OuYang X K, Wang Y G, Yang L Y, Wu K J, He C H*. Adsorption of caprolactam from aqueous solution by novel polysulfone microcapsules containing [Bmim][PF6], Colloids and Surfaces A: Physicochem Eng Aspects, : 72-76.
Zhou Y, Lin Z, Wu K J, Xu G H, He C H*. A group contribution method for the correlation of static dielectric constant of ionic liquids, Chinese J Chem Eng, ):79-88.
Zhu Z W, Xu G H*, An Y, He C H. Construction of octadecyltrichlorosilane self-assembled monolayer on stainless steel 316L surface, Colloids and Surfaces A: Physicochem Eng Aspects, : 408-413.
朱志文,徐国华*,安越,何潮洪. 辛基三乙氧基硅烷/十八烷基三氯硅烷均相混合自组装单分子膜的表征及其形成机制,物理化学学报,2014, 30(8): .
车圆圆, 周俊超, 毕纪葛, 何潮洪*. 改进CBY 桨搅拌釜内单相流体流动与传热特性研究,高校化学工程学报,2014,28(3): 489-496.
郭康斌, 钱超, 陈新发, 何潮洪*. 离子液体催化合成乙酰柠檬酸三丁酯,高校化学工程学报, ): 396-400.
Kou Z N, Zhi Z O, Xu G H*, An Y, He C H. Investigation of the performance and deactivation behavior of Raney-Ni catalyst in continuous dehydrogenation of cyclohexane under multiphase reaction conditions, Applied Catalysis A-General, : 196-201.
Kou Z N, Shen S H, Liu K, Xu G H*, An Y, He C H. Kinetic analysis of dehydrogenation reaction of cyclohexane catalyzed by Raney-Ni under multiphase reaction conditions, Int J Hydrogen Energy, 930-11936.
Chen Q L, Wu K J*, He C H. Thermal Conductivities of [EMIM][EtSO4], [EMIM][EtSO4] + C2H5OH, [EMIM][EtSO4] + H2O, and [EMIM][EtSO4] + C2H5OH + H2O at T =(283.15 to 343.15) K, J Chem Eng Data, 8&2064.
Xu L F, Huang J M,& Qian C, Chen X Z*, Feng L,& Chen Y B, He C H. The synthesis of N-ethyl-n-butylamine by amines disproportionation, Res Chem Intermed, 7-2704.
Zhou J C, Che Y Y, Wu K J*, Shen J, He C H. Thermal conductivity of DMSO + C2H5OH, DMSO + H2O, and DMSO + C2H5OH + H2O Mixtures at T = (278.15 to 338.15) K, J Chem Eng Data, ):663&670.&
Wu K J, Zhao C X, He C H*.& Development of a group contribution method for determination of thermal conductivity of ionic liquids, Fluid Phase Equilibria, : 10-14.
Chen D X, OuYang X K, Wang Y G, Yang L Y, He C H*. Liquid-liquid extraction of caprolactam from water using room temperature ionic liquids, Separation and Purification Technology, : 263-267.
黄捷, 罗能镇, 沈剑, 相咸高, 钱超, 徐义明, 周俊超, 何潮洪*. 二(2-乙基己基)磷酸钠对氨基葡萄糖盐酸盐的离子交换萃取与反萃, 高校化学工程学报, ): 960-966.
陈菡,罗能镇,沈剑,相咸高,何潮洪*,徐义明,陈新志. 野菊花总黄酮的提取及萃取精致研究,高校化学工程学报,2013, 27(3):393-398.
陈颍颍,沈剑,何潮洪*. 三辛胺络合萃取分离一氯乙酸和二氯乙酸,化工学报,2013, 64(2): 609-615.
, . Investigation of convective heat transfer with liquids in microtubes, Ind Eng Chem Res, 86-9395.
Wu K J, Zhao C X, He C H.
Che Y Y, Shen J, Zhou J C, He C H. Thermal conductivity and density of (NH4)2SO4 + H2O, NH4NO3 + H2O, and (NH4)2SO4 + NH4NO3 + H2O solutions at T = (278.15 to 333.15) K, J Chem Eng Data, ):.
Solubilities of 3-methoxy-N-phenylaniline and 3-(methylthio)-N-phenylaniline in five organic solvents (285 K to 333.75 K), J Chem Eng Data, ):
Chen X Z, Zhou S D, Chen Y H, Dong Z H, Gao Y Y, Qian C, He C H. Application of alkoxide in catalytic transfer hydrogenation of unsaturated nitrogen compounds, Res Chem Intermed, ):.
Chen X Z, Zhou S D, Qian C, He C H. Synthesis of 1H-indazole: a combination of experimental and theoretical studies, Res Chem Intermed, ): .
方樟彩,徐国华,钱超,何潮洪. 辣椒红色素制备新工艺研究,高校化学工程学报,): 105-111.
Zhao C X, He C H. Mass transfer and separation criteria for high-speed countercurrent chromatography, AIChE J, ): 359-372.
Fang S, He C H. A new one parameter viscosity model for binary mixtures, AIChE J, ): 517-524.
Luo H, Xia W, Qian C, Chen X Z, He C H. The preparation of 8-[4-[4-(2-pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro[4,5] decane-7,9-dione hydrochloride, Res Chem Intermed, ):
Chen X Z, Luo H, Qian C, He C H. Research on the N-alkylation of morpholine with alcohols catalyzed by CuO-NiO/gamma-Al2O3, Reac Kinet Mech Cat, ): 163-171.
刘明,何潮洪,黄志尧,孟振振,周俊超,车圆圆,金伟光. 丁酮肟-丁酮、丁酮肟-正己烷体系导热系数的测定,高校化学工程学报,): 547-553.
Shen J, He C H. Isolation and Purification of Triptolide from the Leaves of Tripterygium wilfordii Hook F, Chinese J Chem Eng, ): 750-754.
郑博予,房升,何潮洪. 丁酮肟-丁酮、正己烷、环己烷二元体系密度和黏度的测定及关联,高校化学工程学报,): 911-916.
徐亚兰, 何潮洪.& 二(2-乙基己基)磷酸钠离子交换萃取氨基葡萄糖盐酸盐的研究,高校化学工程学报,): 554-561.
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Fang S, Zhu M Q, He C H. Moving window as a variable selection method in potentiometric titration multivariate calibration and its application to the simultaneous determination of ions in Raschig synthesis mixtures, J Chemometrics, -4): 117-123.
Fang S, Zhao C X, He C H, Liu J Q, Sun J H. Densities and viscosities of binary mixtures of tris(2-ethylhexyl) phosphate + cyclohexane or n-hexane at T= (293.15, 298.15, and 303.15) K and p=0.1MPa, J Chem Eng Data, 18-2720.
Fang S, Zhao C X, He C H. Densities and viscosities of binary mixtures of tri-n-butyl phosphate + cyclohexane, +n-heptane at T= (288.15, 293.15, 303.15, and 308.15) K, J Chem Eng Data, 44-2246.
Xu H N, Huang W N, He C H. Modeling for extraction of isoflavones from stem of Pueraria lobata (Willd.) Ohwi using n-butanol/water two-phase solvent system, Separation and Purification Technology, 0-595.
Xu H N, He C H. Separation and purification of puerarin with solvent extraction,Separation and Purification Technology, 7-400.
Xu H N, Zhang Y X, He C H. Ultrasonically Assisted Extraction of Isoflavones from Stem of Pueraria lobata (Willd.) Ohwi and its Mathematical Model, Chinese Journal of Chemical Engineering, ): 861-867.
Zhao C X, He C H. Solubility of atractylenolide III in hexane, ethyl acetate, diethyl ether, and ethanol from (283.2 to 323.2) K. Journal of Chemical & Engineering Data. 2007,52(4): .
OuYang X K, Jin M C, He C H. Preparative separation of four major alkaloids from medicinal plant of Tripterygium wilfordii Hook. F. using High speed countercurrent chromatography. Separation and Purification Technology, 9-324.
OuYang X K, Jin M C, He C H. Simultaneous determination of four sesquiterpene alkaloids in Tripterygium Wilfordii Hook. f. extracts by high-performance liquid chromatography, Phytochemical Analysis, 0-325.
Zhu, J.Q.; Yu, Y.S.; He, C.H. Calculation of solid&s solubilities in mixed liquid solvents by the lh equation using mixing rules,& Fluid Phase Equilibria, ): 85-94.
He, C.H.; Yu, Y.S. New equation for infinite-dilution diffusion coefficients in supercritical& and high-temperature liquid solvents,& Ind Eng Chem Res, 93-3798.&
何潮洪. 超临界溶剂中溶质的扩散系数关联, 高校化学工程学报,3-185.&&
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He, C.H.; Yu, Y.S. Prediction of the temperature dependence of liquid diffusion coefficients at& infinite dilution by a group contribution method, Chinese J Chem Eng, 7-370.&
毛磊,俞菁,何潮洪. 原油常压汽液平衡常数K的普遍关联式,石油化工, 4-535.
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何潮洪, 侯虞钧, 吴兆立. 纯气体在非挥发性溶剂中溶解度的关联,化工学报,3.
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何潮洪, 侯虞钧, 吴兆立. 二元低压汽液平衡 P、y、x 关系及其在加压中的近似应用,化工学报,2.
姓名:何潮洪
单位:化学工程与生物工程学系
职称:教授
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