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Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor
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Shao-bo RUAN, Qin HE, Hui-le GAO*
Acta Pharmaceutica Sinica | 2017, 52(11) : 1756 - 1762
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Acta Pharmaceutica Sinica | 2017, 52(11): 1756-1762
• ORIGINAL ARTICLES •
Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor
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Shao-bo RUAN, Qin HE, Hui-le GAO*
Affiliations
  • Key Laboratory of Drug Targeting and Drug Delivery Systems, West School of Pharmacy, Sichuan University, Chengdu 610041, China
Published: 2017-11-12 doi: 10.16438/j.0513-4870.2017-0847
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Legumain, a kind of asparaginyl endopeptidase, is overexpressed in highly metastatic and highly aggressive tumor, which can undergo an enzymatic hydrolysis of substrates. We proposed a legumain-responsive functional gold nanoparticle (GNP) drug delivery system (GNPs-A & C), which was consist of Ala-Ala-Asn-Cys-Lys (AK) modified GNPs (GNPs-AK) and 2-cyano-6-aminobenzothiazole (CABT) modified GNPs (GNPs-CABT). In the circulation system, the GNPs-A & C could passively target to the tumor site through the enhanced permeability and retention (EPR) effect. Then the overexpressed legumain specifically cleave the peptide to exposure the 1, 2-thiolamino group, which could take place click reaction with the cyano group of CABT, leading to the aggregation of two GNPs, these aggregates of GNPs with increased size were more likely to retain within tumor site. In vivo fluorescent imaging demonstrated GNPs-A & C could acquire an enhanced accumulation in legumain-overexpressed C6 tumor. Importantly, after tethering DOX, the GNPs-DOX-A & C showed an excellent anti-tumor effect with reduced cardiotoxicity.

legumain  /  metal nanoparticle  /  click chemistry  /  aggregation  /  retention
Shao-bo RUAN, Qin HE, Hui-le GAO. Legumain-responsive functional gold nanoparticles for drug targeting delivery and treatment of subcutaneous xenograft tumor[J]. Acta Pharmaceutica Sinica, 2017 , 52 (11) : 1756 -1762 . DOI: 10.16438/j.0513-4870.2017-0847
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Year 2017 volume 52 Issue 11
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doi: 10.16438/j.0513-4870.2017-0847
  • Receive Date：2017-08-29
  • Online Date：2026-01-14
  • Published：2017-11-12
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  • Received：2017-08-29
  • Revised：2017-09-07
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    Key Laboratory of Drug Targeting and Drug Delivery Systems, West School of Pharmacy, Sichuan University, Chengdu 610041, 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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