于沛

博士/教授/博士生导师

通讯地址:               暨南大学药学院,广州市黄埔大道西601号,邮编:510632
E-mail:                     pennypeiyu@163.com
 

教育经历:                                                                              
1984 - 1988             武汉大学化学系,学士
1988 - 1991             武汉大学分析测试中心,硕士
1991 - 1997             香港中文大学化学系,博士
                                师从化学系首席教授、中科院院士、香港中文大学副校长黄乃正教授
1998 - 1999             英国诺丁汉大学化学系, 博士后
                                师从国际著名科学家、英国皇家院士、诺丁汉大学副校长G.Pattenden 教授
 
工作经历:     
2018 - 至今             暨南大学药学院,教授, 硕士生、博士生导师;国际学院常务副院长
2007 - 2018             暨南大学药学院, 教授, 硕士生、博士生导师,曾任新药研究所副所长,药学系主任
2000 - 2007             广州白云山制药股份有限公司技术中心副主任; 广州白云山化学药创新中心副主任;
                                兼白云山化学药厂研究所所长
1991 – 1994            广州白云山制药股份有限公司 质量研究
 
研究方向:       
中药天然产物的结构修饰及活性筛选,抗神经退行性疾病的新药设计、发现和应用开发。
 
研究成果:
在国内外学术期刊上发表学术论文70余篇,申请或授权发明专利40余项,主持国家科技部科技计划、国家“十一五”和“十三五”新药创制重大专项、广东省、广州市各类科研项目近30项,开发新产品新技术10多项,其中包括广州白云山制药的拳头产品国家抗菌新药“头孢硫脒(仙力素)”荣获2006年度国家发明二等奖;“枸橼酸西地那非(金戈)”全国首家上市,目前年销售8亿;在暨南大学团队一起开发的1.1类化学新药“硝酮嗪” 已经进入II期临床研究。
 
 

发表的部分论文 (English)

 

1. Sun, Y.; Jiang, J.; Zhang, Z.; Yu, P.; Wang, L.; Xu, C.; Liu, W.; Wang, Y. Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke. Bioorg. Med. Chem. 16, 8868–8874, 2008.

2. Jiang, X.;  Yu, P.; Jiang, J.;  Zhang, Z.; Wang, Z.; Yang, Z.; Tian, Z.; Wright, S. C.; Larrick, J. W.; Wang, Y. Synthesis and evaluation of antibacterial activities of andrographolide analogues. Eur. J. Med. Chem. 44, 2936–2943, 2009.

3. Chen, J-X.; Xue, H-J.; Ye, W-C.; Fang, B-H., Liu, Y-H., Yuan, S-H., Yu, P.; Wang, Y. Activity of andrographolide and its derivatives against influenza virus in vivo and in vitro. Biol. Pharm. Bull. 32, 1385–1391, 2009.

4. Wang, Z.; Yu, P.; Zhang, G.; Xu, L.; Wang, D.; Wang, L.; Zeng, X.; Wang, Y. Design, synthesis and antibacterial activity of novel andrographolide derivatives. Bioorg. Med. Chem. 18, 4269–4274, 2010.

5. Sun, H.; Xu, L.; Yu, P.; Jiang, J.; Zhang, G.; Wang, Y. Synthesis and preliminary evaluation of neuroprotection of celastrol analogues in PC12 cells. Bioorg. Med. Chem. Lett. 20, 3844–3847, 2010.

6. Zhang, Z.; Li, S.; Jiang, J.; Yu, P.; Liang, J.; Wang, Y. Preventive effects of Flos puerariae lobatae water extract and its active ingredient puerarin in acute and chronic alcohol treated rat and mice model. Chinese Med. 5:36, 2010.

7. Cui, Q.; Zhang, G.; Yu, P.; Wang, Y. Synthesis and preliminary evaluation of anti-HIV agent AZT prodrug. Yao Xue Xue Bao. 46, 1015–1018, 2011.

8. Lu, X.; Wan, S.; Jiang, J.;  Jiang, X.; Yang, W.; Yu, P.; Xu, L.; Zhang, Z.; Zhang, G.; , Zaijun Z.; Shan, L.; Wang, Y. Synthesis and biological evaluations of novel apocynin analogues. Eur. J. Med. Chem. 46, 2691–2698. 2011.

9. Cui, Q.; Zhang, G.; Yu, P.; Wang, Y. Synthesis and preliminary evaluation of anti-HIV agent AZT prodrug.  Acta Pharmaceutica Sinica, 46, 1015–1018, 2011.

10. Yao, H.; Li, S.; Yu, P.; Tang, X.; Jiang, J.; Wang, Y. Reaction characteristics of andrographolide and its analogue AL-1with GSH as a simple chemical simulation of NF-κB Inhibition. Molecules 17, 728–739, 2011.

11. Sun, Y.; Zhang, G.; Zhang, Z.; Yu, P.; Zhong, H.; Du, J.; Wang, Y. Novel multi-functional nitrones for treatment of ischemic stroke. Bioorg. Med. Chem. 20, 3939–3945, 2012.

12. Yu, P.; Xia, L.; Zhao, J.; Zhang, G.; Zhang, Z,; Lang, M.; Wang, Y. Synthesis and preliminary anticancer evaluation of 10-hydroxycamptothecin analogs. Biol. Pharm. Bull. 35, 1295–1299, 2012.

13. Cui, G.; Hung, M.; Shan, L.; Lei, S.; Choi, I.; Zhang, Z.; Hoi, M. P.; Yu, P.; Wang, Y.; Lee, S. M. A novel danshensu derivative confers cardioprotection via PI3K/Akt and Nrf2 pathways. Intl. J. Cardio. 168, 1349–1359, 2013.

14. Cui, Q.; Shan, L.; Zhu, H.;  Yu, P.; Wang, Y. Synthesis and preliminary evaluation of Danshensu derivatives modified at hydroxyl group. J. Intl. Pharm. Res. 40, 795–800, 2013.

15. Sun, Y.; Liao, K.; Li, S.; Zhang, Z.; Yu, P.; Wang, Y. Pharmacokinetic analysis of bis-nitrone tetramethylpyrazine (TN-2) in rats and its protein binding in vitro. Lett. Drug Design and Discov. 11, 770–777, 2014.

16. Wu, H.; Li, W.; Sun, Y.; Xu, L.; Yu, P.; Wang, Y.; Zhang, Z. Determination of AL-1 in rat plasma and tissues by high-performance liquid chromatography and tts application in AL-1 pharmacokinetic study. J. Pharm. Biomed. Sci., 4, 573–580, 2014.

17. Lang, M.; Yan, R.; Wang, Y.; Yu, P. A selective O- and N-acylation protocol for carbamyl chloride. Chin. J. Org. Chem. 34(6):1227, 2014.

18. Cui, Q.; Chen, Y.; Zhang, M.; Shan, L.; Sun, Y.; Yu, P.; Zhang, G.; Wang, D.; Zhao, Z.; Xu, Q.; Xu, B.; Wang, Y. Design, synthesis and preliminary cardioprotective effect evaluation of Danshensu derivatives. Chem. Biol. & Drug Des. 84, 282–291, 2014.

19. Xu, L.; Li, Y.; Wan, S.; Wang, Y.; Yu, P. Apocynin nitrone protects rats from LPS-mediated acute lung injury via inhibition of NADPH oxidase. Intl. Immunopharmacol. 20, 377–382, 2014.

20. Liang, Z.; Du, E.; Xu, L.; Sun, Y.; Zhang, G.; Yu, P.; Wang, Y. Synthesis and preliminary biologic activity evaluation of nitric oxide-releasing andrographolide analogues. Chem. Pharma. Bull. 62, 519–523, 2014.

21. Sun, Y.; Tan, Z.; Liang, Z.; Wang, L.; Shan, L.; Yu, P.; Wang, Y. Synthesis and relationship of stability and biological activity of new DSS and TMP conjugates. MedChemComm. 6, 586–591, 2014.  

22. Fu, P.; Li, Z.; Wang, Y.; Yu, P. Wang, Y. Yu, P. Synthesis of 3-(5H-pyrazolyl)-cyclobutanone derivatives. Asia J. Chem. 27(7): 2545–2547, 2015.

23. Lang, M.; Yao, H.; Fu, P.; Cai, W., Wang, Y.; Yu, P. An unexpected replacement of a methyl with an amino in the tetramethylpyrazine system.  Res. Chem. Intermed. 41: 5621–5626, 2015.

24. Li, Y.; Yan, H.; Zhang, Z.; Zhang, G.; Sun, Y.; Yu, P.; Wang, Y.; Xu, L. Andrographolide derivative AL-1 improves insulin resistance through down-regulation of NF-κB signaling pathway. Br. J. Pharmacol. 172(12):3151–8, 2015.

25. Cui, G.; Shan, L.; Guo, L.; Chu, I. K.; Li, G.; Quan, Q.; Zhao, Y.; Chong, C.; Zhang, Z.; Yu, P.; Hoi, P. M.; Wang, Y.; Lee, S. M. Y. Novel anti-thrombotic agent for modulation of protein disulfide isomerase family member ERp57 for prophylactic therapy. Sci. Rep. 5:10353, 2015.

26. Li, S.; Shan, L.; Zhang, Z.; Li, W.; Liao, K.; Li, S.; Yu, P.; Wang, Y. Pharmacokinetic and metabolism studies of ADTM, a novel Danshensu derivative confers cardioprotection by HPLC-UV and LC-MS/MS.  J. Chromatogr. Sci. 53(6):872–8, 2015.

27. Chen, H.; Xu, D.; Tan, G.; Cai, W.; Zhang, G.; Cui, W.; Wang, J.; Long, C.; Sun, Y.; Yu, P.; Tsim, K.; Zhang, Z.; Han, Y.; Wang, Y. A Potent multifunctional neuroprotective derivative of tetramethylpyrazine.  J. Mol. Neurosci. 56(4):977–87, 2015.

28. Zhu, L.; Sun, Y.; Zhang, G.; Yu, P.; Wang, Y.; Zhang, Z. Radical-scavenging and anti-oxidative activities of TBN in cell-free system and murine H9c2 cardiomyoblast cells. J. Antioxid. Activity 1:1–55, 2015.

29. Zhou, X.; Zhu, L.; Wang, L.; Guo, B.; Zhang, G.; Sun, Y.; Zhang, Z.; Lee, M-Y.; Yu, P.; Wang, Y. Protective effect of edaravone in primary cerebellar granule neurons against iodoacetic acid-induced cell injury, Oxidat. Med. Cell. Longev. 2015:606981, 2015.

30. Yan, H.; Li, Y.; Yang, Y.; Zhang, Z.; Zhang, G.; Sun, Y.; Yu, P.; Wang, Y.; Xu, L. Protective effects of andrographolide derivative AL-1 on high glucose-induced oxidative stress in RIN-m cells. Curr. Pharm. Des. 22(4):499–505, 2016.   

31. Wang, L.; Zhang, X.; Chan, J.; Shan, L.; Cui, Q.; Wang, Y.; Li, J.; Chen, H.; Zhang, Q.; Yu, P.; Han, Y.; Wang, Y.; Lee, S-M. A novel danshensu derivative prevents cardiac dysfunction and improves the chemotherapeutic efficacy of doxorubicin in breast cancer cells" J. Cell. Biochem. 117, 94–105, 2016.

32. Li, X.; Liu, Z.; Wu, L.; Zhang, Z.; Wang, Y.; Sun, Y.; Yu, P. Synthesis and biological evaluation of tetramethylpyrazine nitrates as potential anti-ischemic agents. Asia. J. Chem., 28, 2085–2088, 2016.

33. Jiang, X.; Yang, J.; Zhang, F.; Yu, P.; Sun, Y,; Wang, Y. Facile synthesis of 3-halobenzo-heterocyclic-2-carbonyl compounds via in situ halogenation-oxidation. Adv. Synth. Catal. 358, 2678–2683, 2016.

34. Jiang, X.; Yang, J.; Zhang, F.; Yu, P.; Sun, Y,; Wang, Y. Synthesis of quaternary 3,3-disubstituted 2-oxindoles from 2-substituted indole using selectfluor. Org. Lett. 18, 3154–3157, 2016.

35. Yang, Y.; Yan, H.; Jing, M.; Zhang, Z.; Zhang, G.; Sun, Y.; Shan, L.; Yu, P.; Wang, Y.,  Xu, L. Andrographolide derivative AL-1 ameliorates TNBS-induced colitis in mice: involvement of NF-кB and PPAR-γ signaling pathways. Sci. Rep. 6:29716, 2016.

36. Li, X.; Liu, Z.; Wu, L.; Zhang, Z.; Wang, Y.; Yu, P. Synthesis and biological evaluation of tetramethylpyrazine nitrates as potential anti-ischemic stroke agent.  Asia. J. Chem. spacer28(9): 2085–2088, 2016.

37. Zhang, G.; Zhang, F.;  Zhang, T.; Gu, J.;  Li, C.; Sun, Y.; Yu, P.; Zhang, Z.; Wang, Y. Tetramethylpyrazine nitrone improves neurobehavioral functions and confers neuroprotection on rats with traumatic brain injury. Neurochem. Res. 41(11):2948–2957, 2016.

38. Zhang, Z.; Zhang, G.; Sun, Y.; Szeto, S. S.; Law, H. C.; Quan, Q.; Li, G.; Yu, P.; Sho, E.; Siu, M. K.; Lee,  S. M.;  Chu, I. K.; Wang. Y. Tetramethylpyrazine nitrone, a multifunctional neuroprotective agent for ischemic stroke therapy. Sci. Rep. 6:37148, 2016.

39. Liu, Z.; Yang, S.; Jin, X.; Zhang, G.; Guo, B.; Chen, H.; Yu, P.; Sun, Y.; Zhang, Z.; Wang, Y. Synthesis and biological evaluation of memantine nitrates as potential treatment for neurodegenerative diseases. MedChemComm. 6, 586–591, 2016.  

40. Chen, H.; Tan, G.; Cao, J.; Jiang, J.; Yi, P.; Yu, P.; Sun, Y.; Zhang, Z.; Wang, Y. Design, synthesis, and biological evaluation of novel tetramethylpyrazine derivatives as potential neuroprotective agents. Chem. Pharma. Bull. 65, 56–65, 2017.

41. Jiang, X.; Zhang, F.; Yang, J.; Yu, P.; Yi, P.; Sun, Y.; Wang, Y. Fluorination-oxidation of 2-hydroxymethylindole. Adv. Synth. Catal. 359, 853–858, 2017.

42. Liu, Z.; Cai, W.; Lang, M.; Yan, R.; Li, Z.; Zhang, G.; Yu, P.; Wang, Y.; Sun, Y.; Zhang, Z. Neuroprotective effects and mechanisms of action of multifunctional agents targeting free radicals, monoamine oxidase B and cholinesterase in Parkinson’s disease model. J. Mol. Neurosci. 61(4):498–510, 2017.

43. Zhang, X.; Hu, H.; Luo, J.; Deng, H.; Yu, P.; Zhang, Z.; Zhang, G.; Shan, L.; Wang. Y. A novel danshensu-tetramethylpyrazine conjugate DT-010 provides cardioprotection through the PGC-1α/Nrf2/HO-1 pathway. Bio. Pharm. Bull. 40(9):1490–1498, 2017.

44. Wang, Y.; Zhang, X.;  Xu, C.; Zhang, G.; Zhang, Z.; Yu, P.; Shan, L.; Sun, Y.; Wang, Y. Synthesis and Biological Evaluation of Danshensu and Tetramethylpyrazine Conjugates as Cardioprotective Agents. Chem. Pharm. Bull. 65(4):381–388, 2017.

45. Zhang, T.; Gu, J.; Wu, L.; Li, N.’ Sun, Y.; Yu, P.; Wang, Y.; Zhang, G.;  Zhang. Z. Neuroprotective and axonal outgrowth-promoting effects of tetramethylpyrazine nitrone in chronic cerebral hypoperfusion rats and primary hippocampal neurons exposed to hypoxia. Neuropharmacology. 118:137–147, 2017.

46. Zhang, X.; Luo, J.; Huang, Y.; Deng, H.; Hu, H.; Yu, P.; Sun, Y.; Shan, L.; Wang, Y. A novel danshensu-tetramethylpyrazine conjugate DT-018 provides cardioprotection by preserving mitochondrial function through the MEF2D/PGC-1α pathway. Curr. Pharm. Des. 23(39):6062–6070, 2017.

47. Zhang, G.; Zhang, T.; Li, N.; Wu, L.; Gu, J.; Li, C.; Zhao, C.; Liu, W.; Shan, L.; Yu, P.; Yang, X.; Tang, Y.; Yang, G.; Wang, Y.; Sun, Y.; Zhang, Z. Tetramethylpyrazine nitrone activates AKT/CREB pathway through increasing BDNF expression to promote post-ischemic neuroregeneration and recovery of neurological functions in rats. Br. J. Pharmacol. 175(3):517–531, 2018.

48. Jiang, X.; Liu, S.; Yang, S.; Jiang, M.; Xu, L.; Yu, P.; Wang, Y.; Yeung, Y. Enantioselective Bromolactonization of Deactivated Olefinic Acids. Org. Lett. 20(11): 3259–3262, 2018.

49. Li, N.; Song, X.; Wu, L.; Zhang, T.; Zhao, C.; Yang, X.; Shan, L; Yu, P; Sun, Y.; Wang, Y.; Zhang, G.; Zhang. Z. Miconazole stimulates post-ischemic neurogenesis and promotes functional restoration in rats. Neurosci. Lett. 687:94–98, 2018.

50. Chen, H.; Cao, J.; Zhu, Z.; Zhang, G.; Shan, L.; Yu, P.; Wang, Y.; Sun, Y.; Zhang, Z. A Novel tetramethylpyrazine derivativeprotects against glutamate-induced cytotoxicity through PGC1α/Nrf2 and PI3K/Akt signaling pathways. Front Neurosci.12:567, 2018.

51. Jiang, J.; Jian, Q.; Jing, M.; Zhang, Z.; Zhang, G.; Shan, L.; Yu, P.; Wang, Y.; Xu, L. The novel N-methyl-d-aspartate receptor antagonist MN-08 ameliorates lipopolysaccharide-induced acute lung injury in mice. Int. Immunopharmacol. 66:109–118, 2019.

52. Wu, L.; Su, Z.; Zha, L.; Zhu, Z.; Liu, W.; Sun, Y.; Yu, P.; Wang, Y.; Zhang, G.; Zhang, Z. Tetramethylpyrazine nitrone reduces oxidative stress to alleviate cerebral vasospasm in experimental subarachnoid hemorrhage models. Neuromolecular Med. 2019 May 27. doi: 10.1007/s12017-019-08543-9.

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