Home Journals Articles Updates About
CN
image
收藏切换
Anti-Helicobacter pylori activities of 9-substituted palmatine derivatives
收藏切换
PDF
Tian-yun FAN1, Jing PANG1, Qing-xuan ZENG1, Yan-xiang WANG1, 2, Xue-fu YOU1, Dan-qing SONG1, *
Acta Pharmaceutica Sinica | 2020, 55(6) : 1237 - 1244
Less
收藏切换
Acta Pharmaceutica Sinica | 2020, 55(6): 1237-1244
• Original Articles •
Anti-Helicobacter pylori activities of 9-substituted palmatine derivatives
Full
Tian-yun FAN1, Jing PANG1, Qing-xuan ZENG1, Yan-xiang WANG1, 2, Xue-fu YOU1, Dan-qing SONG1, *
Affiliations
  • 1. Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2020-06-12 doi: 10.16438/j.0513-4870.2020-0085
Outline
收藏切换

Fifteen 9-substituted palmatine (1) derivatives were synthesized and evaluated for their anti-Helicobacter pylori (Hp) activities in vitro. Structure-activity relationship studies revealed that introducing appropriate substituted secondary amino group at position 9 of lead 1 might be beneficial for potency. Among them, compound 5a showed the most potential activity against metronidazole (Met) resistant Hp isolates with minimal inhibitory concentrations (MICs) of 4 μg·mL-1, much better than that of lead 1. Compound 5a displayed satisfactory safety profile in acute toxicity assay. Molecular docking suggested that 5a might act on Hp urease. The results provided key scientific evidence for the development of 1 derivatives into a new class of anti-Hp component.

9-substitute palmatine  /  Helicobacter pylori  /  structure-activity relationship  /  molecular docking
Tian-yun FAN, Jing PANG, Qing-xuan ZENG, Yan-xiang WANG, Xue-fu YOU, Dan-qing SONG. Anti-Helicobacter pylori activities of 9-substituted palmatine derivatives[J]. Acta Pharmaceutica Sinica, 2020 , 55 (6) : 1237 -1244 . DOI: 10.16438/j.0513-4870.2020-0085
Appendix
Less
Year 2020 volume 55 Issue 6
PDF
143
48
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2020-0085
  • Receive Date：2020-02-05
  • Online Date：2026-01-21
  • Published：2020-06-12
Article Data
Affiliations
History
  • Received：2020-02-05
  • Revised：2020-03-02
Funding
Affiliations
    1. Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2020-0085
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House