陈河如

发布时间:2014-07-18 发布单位:药学院


陈河如,男,博士,教授,博士/硕士生导师。1989年毕业于中山大学化学系,获理学学士学位及优秀毕业生称号;1995年毕业于中国科学院上海有机化学研究所并获理学硕士学位;1999年赴香港大学化学系进行合作研究,任助理研究员;2002年毕业于香港科技大学化学系并获哲学(化学)博士学位,同年赴加拿大蒙特利尔临床研究院(Clinical Research Institute of MontrealCanada)进行合作研究,任博士后研究员。2007年赴德国Wuppertal大学进行学术访问,20082月回国。1989.7-2008.2期间,曾断续在汕头大学工作,历任助教、讲师、副教授、汕头大学多学科研究中心顾问等职。2008.3至今,任暨南大学药学院药物化学教授, 博士生导师。多年来从事天然产物的结构修饰、药物合成、有机合成、多肽科学及生物有机化学等领域的研究工作。已经主持和参加多项国家自然科学基金项目、广东省自然科学基金重点及面上项目、广东省科技厅社会发展重点项目、广东省高等院校自然科学研究重点项目和多项其它基金,已在国际及国内重要刊物发表论文120多篇,获授权中国国家发明专利20项、国际发明专利8项。

 

研究方向

 

天然产物的结构修饰及全合成、新药设计/合成/作用机理研究、药物合成工艺研究

 

主持科研项目

 

1. 主持国家自然科学基金面上项目《FAP-alpha酶激活长春花碱类前体化合物的设计合成及抗肿瘤机理研究》(No. 81172982

2. 主持广东省自然科学基金重点研究项目《抗耐药环肽的设计合成及抗菌作用机理研究》(No. 2015A030311012

3. 主持广东省自然科学基金面上项目《天然来源RSV融合蛋白抑制剂的结构优化及其作用机制研究》(No. 2020A1515010857

 

代表性著作

(A) Anti-cancer and the mechanism investigation

1. Minfeng Chen, Xueping Lei, Changzheng Shi, Baojian Wu, Zhengqiu li, Bin Du, Weili Han, Jianyang Hu, Qiulin Nie, Zhenjian Zhuo, Weiqian Mai, Maohua Huang, Nan Ma, Nanhui Xu, Xinyi Zhang, Liangping Luo, Ande Ma, HongSheng Li, Qiang Yu,Heru Chen*, Dongmei Zhang*, Wencai Ye*. Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents.J Clin Invest. 2017, doi:10.1172/JCI94258 (IF 12.78).

2. Jing Zheng, Lijuan Deng, Minfeng Chen, Xuzhi Xiao, Shengwei Xiao, Cuiping Guo, Gaokeng Xiao, Liangliang Bai, Wencai Ye, Dongmei Zhang*, Heru Chen*. Elaboration of thorough simplified vinca alkaloids as antimitotic agents based on pharmacophore similarity.Eur J Med Chem, 2013, 65, 158-167 (IF 3.5)

3. Rikang Wang, Chao Zhang, Chaojun Zheng, Huilan Li, Xinshu Xie, Yi Jin, Zhijun Liu, Heru Chen*. Introduction of Z-GP scaffold into procarbazine reduces spermatoxicity and myelosuppression.Bioorganic Chemistry2019, 83, 461-467 (IF 3.9).

4. Jie Liu, Chao Zhang, Huailin Wang, Jianrun Zhang, Lei Zhang, Zhenlei Jiang, Jianrun Zhang, Zhijun Liu, Heru Chen*. Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity.Eur. J. Med. Chem.2018, 151, 158-172 (IF 4.816).

5. Jie Liu, Fan Zhou, Lei Zhang, Huailin Wang, Jianrun Zhang, Chao Zhang, Zhenlei Jiang, Yanbing Li, Zhijun Liu, Heru Chen*. DMXAA-pyranoxanthone hybrids enhance inhibition activities against human cancer cells with multi-target functions.Eur. J. Med. Chem.2018, 143, 1768-1778 (IF 4.816).

6. Jie Liu, Jianrun Zhang, Huailin Wang, Zhijun Liu, Chao Zhang, Zhenlei Jiang, Heru Chen*. Synthesis of xanthone derivatives and the studies on the inhibition against cancer cells growth and synergistic effects of them.Eur. J. Med. Chem.2017, 133, 50-61 (IF 4.816).

7. 肖胜伟,刘志军,柳杨,陈河如*.抗癌药物达卡巴嗪的合成工艺优化.有机化学2015, 35(5), 1161-1165.

8. 张潮,刘志军,李艳冰,何业谱,林晓洪,陈河如*.靶向抗肿瘤药N-(Nꞌ-苄氧羰基甘氨酰脯氨酰)丙卡巴肼 (Z-GP-Pcb)的环境友好合成以及透过血脑屏障活性评价.有机化学2020, 40, 536-540 (IF 1.392).

(B) Anti-neurodegeneration disease and the mechanism investigation

9. Rongtian Lin, Shuwen Rao, Yanbing Li, Lei Zhang, Liyu Xu, Yepu He, Zhijun Liu, Heru Chen*. Conjugation of tacrine with genipin derivative not only enhances effects on AChE but also leads to autophagy against Alzheimer’s disease.Eur J Med Chem2021, 211, 113067 (IF 5.2).

10. Yepu He, Liyu Xu, Yanbing Li, Yinying Tang, Shuwen Rao, Rongtian Lin, Zhijun Liu, Heru Chen*. Synergistic Integration of Dihydro-artemisinin with -Aminobutyric Acid Results in a More Potential Anti-depressant.Bioorg. Chem.2021, 110, 104769 (IF 4.3).

11. Wang, R., Yang, J., Peng, L., Zhao, J., Mu, N., Huang, J., Lazarovici, P., Chen, H.*, and Zheng, W.* Gardenamide A attenuated cell apoptosis induced by serum deprivation via ERK1/2 and PI3K/Akt signaling pathways.Neuroscience2015, 286, 242-250. (IF3.3)

12. Rikang Wang, Jiaqiang Zhao, Lei Zhang, Xinyi Zhang, Wenhua Zheng*, and Heru Chen*. Genipin Derivatives Protect RGC-5 from Sodium Nitroprusside-Induced Nitrosative Stress.Int. J. Mol. Sci.2016, 17(1), 117;doi: 10.3390/ijms 17010117 (IF 3.15).

13. Jiaqiang Zhao, Lizhi Peng, Rikang Wang, Lei Zhang, Xinyi Zhang, Jian Yang, Wenhua Zheng*, Heru Chen*. Chemically Bonding of Amantadine with Gardenamide A Enhances the Neuroprotective Effects Against Corticosterone-Induced Insults in PC12 Cells.Int. J. Mol. Sci.2015, (IF2.8)

14. Rikang Wang, Lizhi Peng, Jiaqiang Zhao, Laitao Zhang, Cuiping Guo, Wenhua Zheng*, Heru Chen*. Gardenamide A Protects RGC-5 Cells from H2O2-induced Oxidative Stress Insults by Activating PI3K/Akt/eNOS Signaling Pathway.Int. J. Mol. Sci.2015, (IF2.8)

15. Wang, R., Yang, J., Zhang, L., Xiao, G., Luo, J., Liao, S., Chen, H.*, and Zheng W.* Stereoselective Reduction of 1-O-Isopropyloxygenipin Enhances Its Neuroprotective Activity against Apoptosis in PC12 Cells Induced by Sodium Nitroprusside.ChemMedChem2014,9(7), 1397-1401. (IF 3.15)

16. Huan-huan Zheng, Cui-ting Luo, Heru Chen*, Juan-na Lin, Chun-lin Ye, Shuang-shuang Mao, Yu-lin Li.Xanthones from Swertia mussotii as multi-target-directed anti-diabetic agents. ChemMedChem2014, 9(7), 1378-1386.(IF 3.15)

17. Luo, J., Wang, R. –K., Huang, Z., Yang, J., Yao, X. –S., Chen, H. R.*, Zhen, W. –H.* Synthesis of Stable Derivatives from Genipin and Studies of Their Neuroprotective Activity in PC12 Cells.ChemMedChem2012, 7(9), 1661-1668IF 3.15

18. Lei Zhang, Xinyi Zhang, Laitao Zhang, Lizhi Peng, Jie Liu, Cuiping Guo, Cheng Luo, Heru Chen *. Incorporation of Dihydroartemisinin into Memantine through A Propriate Spacer Makes the Hybrid with Enhancing Effects to Protect PC12 Cells from Corticosterone–Caused Impairments.高等学校化学研究2017, 33(4), 611-622 (IF 1.248) .

(C) Anti-diabetic and the mechanism investigation

19. Laitao Zhang#, Yifang Li#, Sheng Yuan#, Shijie Zhang, Huanhuan Zheng, Jie Liu, Pinghua Sun, Yijun Gu, Hiroshi Kurihara, Rongrong He*, Heru Chen*. Bioactivity Focus of -Cyano-4-hydroxycinnamic acid (CHCA) Leads to Effective Multifunctional Aldose Reductase Inhibitors. Sci Report2016, 6, 24942, doi: 10.1038/srep24942 (IF 5.28).

20. Zhihua Wang, Sheng Yuan, Yanbing Li, Zhe Zhang, Wei Xiao, Dan Tang, Kaihe Ye, Zhijun Liu, Congcong Wang, Yixiong Zheng, Hong Nie*, Heru Chen*. Regulation on SIRT1-PGC-1α/Nrf2 pathway together with selective inhibition of aldose reductase makes compound hr5F a potential agent for the treatment of diabetic complications.Biochem Pharmacology2018, 150, 54-63. https://doi.org/10.1016/j.bcp.2018.01.034 (IF 4.235).

21. Fu-xiang Jiang, Qiao-zhen Liu, Dan Zhao, Cui-ting Luo, Cui-ping Guo, Wen-cai Ye, Cheng Luo, Heru Chen*. A concise synthesis of N-substituted fagomine derivatives and the systematic exploration of their -glycosidase inhibition.Eur J Med Chem2014, 77, 211-222.IF 3.9

22. Huan-huan Zheng, Cui-ting Luo, Heru Chen*, Juan-na Lin, Chun-lin Ye, Shuang-shuang Mao, Yu-lin Li.Xanthones from Swertia mussotii as multi-target-directed anti-diabetic agents. ChemMedChem2014, 9(7), 1378-1386.(IF 3.15)

23. Cui-ting Luo, Huan-huan Zhen, Shuang-shuang Mao, Mao-xun Yang, Cheng Luo, Heru Chen*. Xanthones from Swertia mussotii and their -glycosidase inhibitory activities.Planta Medica2014, 80, 201-208 (IF 2.23)

24. Cui-ting Luo, Shuang-shuang Mao, Fang-lan Liu, Mao-xun Yang, Hiroshi Kurihara, Yulin Li, Heru Chen*. Antioxidant Xanthones from Swertia mussotii, a High Altitude Plant.Fitoterapia2013, 91, 140-147 (IF 2.15)

(D) Others

25. Yinying Tang, Jie Liu, Huailing Wang, Yanbing Li, Zhijun Liu, Heru Chen*. 1,3,5,8-Tetrahydroxy-9H-xanthen-9-one exerts anti-ageing effect through the regulation of stress-response genes and MAPKs signaling pathway. Arch Pharm Chem Life Sci.2019, 352: 1900100. DOI: 10.1002/ardp.201900100

26. Yanbing Li, Chao Zhang, Huailing Wang, Fan Zhou, Jie Liu, Yinying Tang, Zhenlei Jiang, Zhijun Liu, Heru Chen*. The Synthesis and Anti-ageing Property of Antioxidant Pseudopeptides Designed Based on Bioisostere Principle.Arch Pharm Chem Life Sci.2019, 352: e1800354, DOI:10.1002/ardp.201800354

27. 许男徽,陈河如*. (1aRS,7aRS)-7-羟基氨亚基-1,1a,7,7a-4H-丙环骈[b]色烯-1a-甲酸乙酯及其衍生物的有效全合成.有机化学2015, 35(5), 1033-1039.

28. Heru Chen*, Cao Zhang, Zhenlei Jiang, Jiu Liu. Structural modification based on natural products leads to more drug-like candidates.结构化学2017, 36(12), 1947-1960 (综述) (IF 0.659).

 

授权中国国家发明专利

 

1. 陈河如,叶文才,张冬梅,陈敏锋,肖绪枝,许男徽,雷雪萍,胡坚杨.一种吲哚生物碱加合物及其制备方法和在制备抗肿瘤药物中的应用.中国发明专利,ZL201310138241.8

2. 陈河如,李怡芳,何蓉蓉.一种-氰基-4-羟基肉桂酸衍生物及其制备方法和用途.中国发明专利,ZL201410723116.8

3. 陈河如,张来涛,彭丽芝.二氢青蒿素-美金刚二联体化合物及其合成方法和用途.中国国家发明专利, ZL 20160061614.X,授权日2017.12.12.

4. 叶文才,陈河如,张冬梅,陈敏峰,许男徽.长春碱类衍生物及其制备方法和应用.中国发明专利, ZL201480022198.1,授权日2018.02.02.

5. 叶文才,张冬梅,陈河如,陈敏峰,肖绪枝,许男徽,雷雪萍,胡坚杨.长春碱及其类似物的新应用.中国发明专利, ZL201310738860,授权日2018.10.30.

6. 王日康,陈河如,张磊,张潮.一种靶向FAP-alpha酶的抗肿瘤化合物及其制备方法和应用.中国国家发明专利, ZL20161118043.5,申请日 2016.12.07,授权日2019.05.14.

7. 陈河如,王日康,赵家强,张磊.一种栀子酰胺A-他克林二联体化合物及其制法和应用.中国国家发明专利, ZL 201610946374.1,申请日 2016.11.03,授权日2019.08.02.

8. 陈河如,张磊,张潮.一种CHR20/21-他克林杂合体化合物及其制备方法和应用.中国国家发明专利, ZL 201710751799.1,申请日期 2017.08.28授权日2019.09.17.

9. 陈河如, 袁盛, 李艳冰, 李怡芳, 何蓉蓉. 一种具有醛糖还原酶抑制活性的肉桂酸衍生物及其制备方法和应用. 中国国家发明专利, ZL 201710372369.9, 申请日2017.05.24, 授权日2019.11.08.

10.陈河如,刘杰,王怀玲,刘志军,张磊.一种Xanthone-NO供体化合物的制备方法和在抗肿瘤药物中的应用.中国国家发明专利, ZL 201710751106.9,申请日 2017.08.28,授权日2019.12.24.

11. 陈河如,刘杰,王怀玲,刘志军.一种DMXAA-Pyranoxanthone杂合体化合物及其制备方法与用途.中国国家发明专利, ZL 201710545200.9,申请日 2017.07.06,授权日2020.02.07.

12. 陈河如,彭丽芝,李艳冰,张潮,李怡芳,何蓉蓉,张磊.一种金刚烷胺-栀子酰胺A杂合体化合物在治疗帕金森疾病药物中的应用.中国国家发明专利, ZL201711054870.7,申请日 2017.11.01,授权日2020.02.07.

13. 杨懋勋, 陈河如, 曹文强, 赵柏松. 一种植物根茎榨汁装置. 中国国家实用新型专利, ZL201921423331.0, 申请日2019.08.29, 授权日2020.06.19.

14. 陈河如,刘杰,周帆,王怀玲.一种线性假多肽及其制备方法以及其在抗肿瘤药物中的应用.中国国家发明专利, ZL201810711204.4,申请日2018.07.03,授权日2020.09.04.

15. 陈河如,周帆.李艳冰.一种线性假多肽及其制备方法以及在抗菌药物中的应用.中国国家发明专利, ZL 201810711202.5,申请日期 2018.07.03,授权日2020.11.13.

 

授权国际发明专利

 

1. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. PCT/2014/000192.

2. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. United States Patent, US14/785,547

3. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. European Patent, EP2987794.

4. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. UK Patent, EP2987794.

5. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. French Patent, FR2987794.

6. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. Germany Patent, DE602014026358.5.

7. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. Australia Patent, AU2014253584 B2.

8. Ye Wencai, Chen Heru, Zhang Dongmei, Chen Minfeng, Xu Nanhui. Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof. Japan Patent, JP6250710.

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