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Design, synthesis and biological evaluation of the novel ligustrazine derivatives
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Yang ZHANG1, 2, Yu YANG1, 2, Jia-ming LI1, 2, *, Xiao-dong MA1, 2, Yan-chun ZHANG1, 2, Yu-jun WANG1, 2, Pan-hu ZHU1, 2
Acta Pharmaceutica Sinica | 2017, 52(11) : 1722 - 1730
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Acta Pharmaceutica Sinica | 2017, 52(11): 1722-1730
ORIGINAL ARTICLES
Design, synthesis and biological evaluation of the novel ligustrazine derivatives
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Yang ZHANG1, 2, Yu YANG1, 2, Jia-ming LI1, 2, *, Xiao-dong MA1, 2, Yan-chun ZHANG1, 2, Yu-jun WANG1, 2, Pan-hu ZHU1, 2
Affiliations
  • 1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038, China
  • 2. Department of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230038, China
Published: 2017-11-12 doi: 10.16438/j.0513-4870.2017-0323
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Using ligustrazine as the leading compound, we designed and synthesized ten novel ligustrazine derivatives, whose structures were determined by 1H NMR, 13C NMR and MS. Inhibitory effects of the new compounds on the proliferation of A549, A549/DDP and HBE cells were detected by MTT assay. The inhibi-tory activity of the synthesized compounds on migration and invasion of A549 cells were evaluated through scratch assay and transwell assay. Mechanism of the inhibition on migration and invasion was investigated by Western blotting. In addition, the cell cycle was analyzed with flow cytometry. The results showed that, both compounds Z8 and Z10 have an anti-proliferative activity, and the potencies of inhibition of tumor-cell migration and invasion were attributed to the down-regulation of MMP-2 and MMP-9. The compounds Z8 and Z10 could also enhance G2/M arrest in A549 cell as revealed by cell cycle analysis.

ligustrazine derivative  /  migration  /  invasion  /  cell cycle
Yang ZHANG, Yu YANG, Jia-ming LI, Xiao-dong MA, Yan-chun ZHANG, Yu-jun WANG, Pan-hu ZHU. Design, synthesis and biological evaluation of the novel ligustrazine derivatives[J]. Acta Pharmaceutica Sinica, 2017 , 52 (11) : 1722 -1730 . DOI: 10.16438/j.0513-4870.2017-0323
Year 2017 volume 52 Issue 11
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Article Info
doi: 10.16438/j.0513-4870.2017-0323
  • Receive Date:2017-04-07
  • Online Date:2026-01-14
  • Published:2017-11-12
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  • Received:2017-04-07
  • Revised:2017-06-07
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Affiliations
    1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038, China
    2. Department of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230038, 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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