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Specific blockade of muscle acetylcholine receptor by α-conotoxin MIA and MIB
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Xi-xi WU1, Liu-jun WANG1, Xiao-peng ZHU2, Dong-ting ZHANGSUN1, Yong WU2, *, Su-lan LUO1, 2, *
Acta Pharmaceutica Sinica | 2022, 57(3) : 724 - 730
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Acta Pharmaceutica Sinica | 2022, 57(3): 724-730
• Original Articles •
Specific blockade of muscle acetylcholine receptor by α-conotoxin MIA and MIB
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Xi-xi WU1, Liu-jun WANG1, Xiao-peng ZHU2, Dong-ting ZHANGSUN1, Yong WU2, *, Su-lan LUO1, 2, *
Affiliations
  • 1. Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou 570228, China
  • 2. School of Medicine, Guangxi University, Nanning 530004, China
Published: 2022-03-12 doi: 10.16438/j.0513-4870.2021-1434
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The α-conotoxins are peptide toxins that are identified from the venom of marine cone snails and they hold outstanding potency on various subtypes of nicotinic acetylcholine receptors (nAChRs). nAChRs have an important role in regulating transmitter release, cell excitability, and neuronal integration, so nAChR dysfunctions have been involved in a variety of severe pathologies. Four types of α-3/5 conotoxins MI, MIA, MIB and MIC have been found from Conus magus. Among them, the activity and selectivity of MIA and MIB have not been well studied. In this study, four α-3/5 conotoxins MI, MIA, MIB and MIC were synthesized by solid peptide synthesis method, and the bioactivities of them were screened by double electrode voltage clamp electrophysiology. The results showed that MIA and MIB selectively inhibited muscle type acetylcholine receptors with IC50 values of 14.45 and 72.78 nmol·L-1, respectively, which are slightly weaker than MI and MIC. Molecular docking results have shown MIA and MIB interact with muscle-type nAChRs with similar mechanism. The reasons for activity differences may relate to the size of the N-terminal amino acids. Together, the conotoxins MIA and MIB may have the potential to develop as a tool for detect the function of muscle type nAChRs, as well as the diagnosis or treat of related diseases.

Conus magus  /  α-conotoxin  /  solid phase synthesis of 9-fluorene methoxycarbonyl  /  oxidative folding  /  muscle type nAChRs  /  molecular docking
Xi-xi WU, Liu-jun WANG, Xiao-peng ZHU, Dong-ting ZHANGSUN, Yong WU, Su-lan LUO. Specific blockade of muscle acetylcholine receptor by α-conotoxin MIA and MIB[J]. Acta Pharmaceutica Sinica, 2022 , 57 (3) : 724 -730 . DOI: 10.16438/j.0513-4870.2021-1434
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Year 2022 volume 57 Issue 3
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Article Info
doi: 10.16438/j.0513-4870.2021-1434
  • Receive Date：2021-09-30
  • Online Date：2025-12-22
  • Published：2022-03-12
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History
  • Received：2021-09-30
  • Revised：2021-11-02
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Affiliations
    1. Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou 570228, China
    2. School of Medicine, Guangxi University, Nanning 530004, 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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