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Anti-Helicobacter pylori activities of 9-substituted palmatine derivatives
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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
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Acta Pharmaceutica Sinica | 2020, 55(6): 1237-1244
• Original Articles •
Anti-Helicobacter pylori activities of 9-substituted palmatine derivatives
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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
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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
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Article Info
doi: 10.16438/j.0513-4870.2020-0085
  • Receive Date：2020-02-05
  • Online Date：2026-01-21
  • Published：2020-06-12
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  • Received：2020-02-05
  • Revised：2020-03-02
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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
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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
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