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Synthesis and anti-HCC activity of full 2ʹ-F/OMe-siRNA encapsulated with neutral cytidinyl/cationic lipid
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Yu-jing GAO1, Xi-xian WANG2, Yu-fei PAN2, Quan-xin WANG2, Yue-jie ZHU2, De-lin PAN1, *, Zhu GUAN2, Zhen-jun YANG2, *
Acta Pharmaceutica Sinica | 2023, 58(6) : 1634 - 1640
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Acta Pharmaceutica Sinica | 2023, 58(6): 1634-1640
Original Articles
Synthesis and anti-HCC activity of full 2ʹ-F/OMe-siRNA encapsulated with neutral cytidinyl/cationic lipid
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Yu-jing GAO1, Xi-xian WANG2, Yu-fei PAN2, Quan-xin WANG2, Yue-jie ZHU2, De-lin PAN1, *, Zhu GUAN2, Zhen-jun YANG2, *
Affiliations
  • 1. School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
  • 2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Published: 2023-06-12 doi: 10.16438/j.0513-4870.2022-1345
Outline
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A variety of full 2ʹ-F/OMe-modified siRNAs were designed and synthesized, and the activity against hepatocellular carcinoma Huh-7 and HepG2 cells was evaluated. K&A DNA/RNA H-8 synthesizer was used to synthesize siRNAs, and neutral cytidinyl lipid DNCA mixed with cationic lipid CLD were used to transfect siRNA. By RT-qPCR and CCK-8 assay, the target gene silence and the proliferation of Huh-7 and HepG2 cells were detected. The siRNAs loading into Ago2 protein was detected by RNA-binding protein immunoprecipitation. Drug uptake and cell apoptosis were detected by flow cytometry, and the expression of PLK1 protein was detected by Western blot. Partial full 2ʹ-F/OMe modified siRNAs, especial siPLK1A3, increased the uptake of Huh-7 cells, enhanced their binding to Ago2 and gene silencing activity, down-regulated PLK1 protein, as well as induced more Huh-7 cell apoptosis and proliferation inhibition activity. It provides important data for the development of novel siRNA modification patterns and anti-HCC formulations.

siRNA  /  full 2ʹ-modification  /  anti-HCC  /  Ago2  /  DNCA/CLD
Yu-jing GAO, Xi-xian WANG, Yu-fei PAN, Quan-xin WANG, Yue-jie ZHU, De-lin PAN, Zhu GUAN, Zhen-jun YANG. Synthesis and anti-HCC activity of full 2ʹ-F/OMe-siRNA encapsulated with neutral cytidinyl/cationic lipid[J]. Acta Pharmaceutica Sinica, 2023 , 58 (6) : 1634 -1640 . DOI: 10.16438/j.0513-4870.2022-1345
Year 2023 volume 58 Issue 6
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Article Info
doi: 10.16438/j.0513-4870.2022-1345
  • Receive Date:2022-12-07
  • Online Date:2025-11-21
  • Published:2023-06-12
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History
  • Received:2022-12-07
  • Revised:2023-01-13
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Affiliations
    1. School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
    2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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