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Design, synthesis and anti-MRSA activities of cycloberberine derivatives with a novel chemical scaffold
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Tian-yun FAN, Xin-xin HU, Yan-xiang WANG, Sheng TANG, Xue-fu YOU, Dan-qing SONG*
Acta Pharmaceutica Sinica | 2018, 53(6) : 887 - 894
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Acta Pharmaceutica Sinica | 2018, 53(6): 887-894
• SPECIAL REPORTS •
Design, synthesis and anti-MRSA activities of cycloberberine derivatives with a novel chemical scaffold
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Tian-yun FAN, Xin-xin HU, Yan-xiang WANG, Sheng TANG, Xue-fu YOU, Dan-qing SONG*
Affiliations
  • Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2018-06-12 doi: 10.16438/j.0513-4870.2018-0141
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9-Acetoxycycloberberine (1) with a unique skeleton was first identified to display a potent antimicrobial profile against methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 1-16 μg·mL-1. Taking the compound as a lead, 14 target cycloberberine analogues with diverse structures, such as berberine and chelerythrine derivatives, were synthesized and evaluated for their anti-bacterial activities. Analysis of the structure-activity relationship revealed that:① ring E was essential for the activity; ② the removing of ring B decreased the activity against MRSA. However, the antimicrobial activity against vancomycin-resistant Enterococcus faecium (VRE) was improved; ③ the introduction of a suitable rigid substituent at the 9-position was beneficial for the activity. Among them, compound 9a showed the most potential activity against methicillin-sensitive Staphylococcus aureus (MSSA) and MRSA isolates with MIC values of 0.5-1 μg·mL-1, suggesting a different mechanism from clinical drugs. It displayed higher stability in blood. Therefore, we consider 9a worthy of further investigation. The results provide key scientific evidence for development of such compounds into a new type of anti-MRSA candidates.

cycloberberine  /  chelerythrine  /  antibacterial  /  MRSA  /  drug resistance  /  structure-activity relationship
Tian-yun FAN, Xin-xin HU, Yan-xiang WANG, Sheng TANG, Xue-fu YOU, Dan-qing SONG. Design, synthesis and anti-MRSA activities of cycloberberine derivatives with a novel chemical scaffold[J]. Acta Pharmaceutica Sinica, 2018 , 53 (6) : 887 -894 . DOI: 10.16438/j.0513-4870.2018-0141
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doi: 10.16438/j.0513-4870.2018-0141
  • Receive Date：2018-02-07
  • Online Date：2026-01-15
  • Published：2018-06-12
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  • Received：2018-02-07
  • Revised：2018-03-01
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    Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, 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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