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Design, synthesis, and activity study of α-conotoxin[A10L]PnIA fluorescent probe
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Yao TAN1, Yi-shuai YANG1, Zhao-li CHU1, Dong-ting ZHANGSUN1, Xiao-peng ZHU1, 2, *, Su-lan LUO1, 2, *
Acta Pharmaceutica Sinica | 2021, 56(8) : 2252 - 2259
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Acta Pharmaceutica Sinica | 2021, 56(8): 2252-2259
• Original Articles •
Design, synthesis, and activity study of α-conotoxin[A10L]PnIA fluorescent probe
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Yao TAN1, Yi-shuai YANG1, Zhao-li CHU1, Dong-ting ZHANGSUN1, Xiao-peng ZHU1, 2, *, Su-lan LUO1, 2, *
Affiliations
  • 1. Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Life and Pharmaceutical Sciences, Hainan University, Haikou 570228, China
  • 2. Medical School, Guangxi University, Nanning 530004, China
Published: 2021-08-12 doi: 10.16438/j.0513-4870.2021-0528
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α7 nicotinic acetylcholine receptor (nAChR) is widely distributed in the central and peripheral nervous systems, and is closely related to a variety of neurological diseases and inflammation response. α-Conotoxin[A10L]PnIA, as an antagonist targeting α7 nAChR, plays an important role in studying the physiological and pathological processes involved in α7 nAChR.[A10L]PnIA was labeled with fluorescein 5-carboxytetramethylrho-damine, and the active peptide ([A10L]PnIA-F) was obtained by a two-step oxidative folding procedure in vitro. The Xenopus oocyte expression system and the two-electrode voltage clamp technique were used to identify the potency of[A10L]PnIA-F fluorescent peptide, and its cytotoxicity was detected by mouse macrophages and CCK8 method. The molecular weight of[A10L]PnIA-F fluorescent peptide was identified by mass spectrometry as 2 077.28 Da, which was consistent with the theoretical value. Electrophysiological determination of its halfmaximal inhibitory concentration (IC50) for α7 nAChR is 17.32 nmol·L-1, which is consistent with[A10L]PnIA (IC50, 13.84 nmol·L-1). The cytotoxicity test results showed that within the concentration range of 5 nmol·L-1 to 10 μmol·L-1, there was no significant inhibition on the growth of mouse macrophages. The results showed that the α-conotoxin fluorescent probe[A10L]PnIA could provide pharmacological tools for the research of α7 nAChRrelated neurophysiological and pathological mechanisms.

α7 nicotinic acetylcholine receptor  /  α-conotoxin[A10L]PnIA  /  fluorescent probe  /  electrophysio-logical activity
Yao TAN, Yi-shuai YANG, Zhao-li CHU, Dong-ting ZHANGSUN, Xiao-peng ZHU, Su-lan LUO. Design, synthesis, and activity study of α-conotoxin[A10L]PnIA fluorescent probe[J]. Acta Pharmaceutica Sinica, 2021 , 56 (8) : 2252 -2259 . DOI: 10.16438/j.0513-4870.2021-0528
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Article Info
doi: 10.16438/j.0513-4870.2021-0528
  • Receive Date：2021-04-12
  • Online Date：2025-12-18
  • Published：2021-08-12
Article Data
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History
  • Received：2021-04-12
  • Revised：2021-05-06
Funding
Affiliations
    1. Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Life and Pharmaceutical Sciences, Hainan University, Haikou 570228, China
    2. Medical School, 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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