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Design and synthesis of peptide-drug conjugates and fluorescent probe based on α-conotoxin ArIB[V11L,V16D]
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Xin SUN, Jiang-nan HU, Su-lan LUO, Shuai DONG*
Acta Pharmaceutica Sinica | 2023, 58(9) : 2727 - 2733
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Acta Pharmaceutica Sinica | 2023, 58(9): 2727-2733
Design and synthesis of peptide-drug conjugates and fluorescent probe based on α-conotoxin ArIB[V11L,V16D]
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Xin SUN, Jiang-nan HU, Su-lan LUO, Shuai DONG*
Affiliations
  • Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou, Hainan, 570228, China
Published: 2023-09-12 doi: 10.16438/j.0513-4870.2023-0577
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α-Conotoxin ArIB[V11L,V16D] is currently the most optimal selective inhibitor of α7 nicotinic acetylcholine receptor (nAChR) known. In order to explore chemical modification methods and enrich its application in targeting nAChR, this study utilized the linker to covalently connect camptothecin and 7-amino-4-methylcoumarin to the [2,4] disulfide bond of ArIB[V11L,V16D]. Therefore, two peptide-drug conjugates (PDCs), ArIB[V11L,V16D]-5 and ArIB[V11L,V16D]-6, and one fluorescent-labeled peptide, ArIB[V11L,V16D]-7 were constructed. Cytotoxicity evaluation showed that the IC50 values against non-small cell lung cancer cell line A549 of the two PDCs were respectively 1.3 and 4.1 times of camptothecin, indicating slight reduction in activity at the cellular level which was related to the linker structure. Fluorescence spectrum scanning revealed that the excitation and emission wavelength of the fluorescent-labeled peptide were 340 nm and 403 nm respectively, and the fluorescence features of 7-amino-4-methylcoumarin as a marker were retained without fluorescence quenching. This modification strategy laid a solid foundation for the further application of α-conotoxin ArIB[V11L,V16D] in PDCs and fluorescent probes.

α-conotoxin ArIB[V11L,V16D]  /  disulfide bond modification  /  peptide-drug conjugate  /  fluorescent probe
Xin SUN, Jiang-nan HU, Su-lan LUO, Shuai DONG. Design and synthesis of peptide-drug conjugates and fluorescent probe based on α-conotoxin ArIB[V11L,V16D][J]. Acta Pharmaceutica Sinica, 2023 , 58 (9) : 2727 -2733 . DOI: 10.16438/j.0513-4870.2023-0577
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doi: 10.16438/j.0513-4870.2023-0577
  • Receive Date：2023-05-06
  • Online Date：2025-11-21
  • Published：2023-09-12
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  • Received：2023-05-06
  • Revised：2023-06-15
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    Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou, Hainan, 570228, 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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