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Structure modification and antimicrobial activity of novel cationic melittin analogues
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A-long CUI, He-xian YANG, Si-tu XUE, Lian-qi SUN, Jie JIN, Hong YI, Zhuo-rong LI*
Acta Pharmaceutica Sinica | 2021, 56(5) : 1424 - 1428
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Acta Pharmaceutica Sinica | 2021, 56(5): 1424-1428
• Original Articles •
Structure modification and antimicrobial activity of novel cationic melittin analogues
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A-long CUI, He-xian YANG, Si-tu XUE, Lian-qi SUN, Jie JIN, Hong YI, Zhuo-rong LI*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2021-05-12 doi: 10.16438/j.0513-4870.2021-0190
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Melittin exhibits high antibacterial potency against drug-resistant bacteria. However, the clinical utility of melittin is limited by its serious hemolytic activity. Thus, the need for developing novel melittin analogues with high antimicrobial activity and low hemolytic activity has grown. We designed, synthesized, and evaluated 20 novel melittin analogues with varying hydrophobic, polar or positively charged amino acids. The results showed that 8 compounds had antimicrobial activity (MIC: 1-4 μg·mL-1) against gram-positive pathogens equal to or better than that of melittin, and 16 compounds had low hemolytic activity (HC50 ≥ 11.9 μg·mL-1). Compounds 13 (MIC: 2-4 μg·mL-1) and 15 (MIC: 1-2 μg·mL-1) showed equal or better antimicrobial activity against both susceptible and resistant strains of Staphylococcus aureus and Enterococcus faecium compared to melittin (MIC: 4 μg·mL-1). Compound 13 (HC50: 24.0±4.3 μg·mL-1) displayed noticeably decreased hemolytic activity compared to melittin (HC50: 5.3±0.4 μg·mL-1). This work established a base for further study on the structure-activity relationships and structure-toxicity relationships of melittin.

gram-positive pathogen  /  melittin  /  novel analogue  /  antimicrobial activity  /  hemolytic activity
A-long CUI, He-xian YANG, Si-tu XUE, Lian-qi SUN, Jie JIN, Hong YI, Zhuo-rong LI. Structure modification and antimicrobial activity of novel cationic melittin analogues[J]. Acta Pharmaceutica Sinica, 2021 , 56 (5) : 1424 -1428 . DOI: 10.16438/j.0513-4870.2021-0190
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doi: 10.16438/j.0513-4870.2021-0190
  • Receive Date：2021-02-05
  • Online Date：2025-12-18
  • Published：2021-05-12
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  • Received：2021-02-05
  • Revised：2021-03-09
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    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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