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Design, synthesis and evaluation of anti-inflammatory effect of novel berberine derivatives on IL-6/STAT signaling pathway
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Qing-xuan ZENG, Na ZHANG, Hong-bin DENG, Dan-qing SONG, Jian-dong JIANG, Yan-xiang WANG*
Acta Pharmaceutica Sinica | 2017, 52(12) : 1895 - 1902
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Acta Pharmaceutica Sinica | 2017, 52(12): 1895-1902
• ORIGINAL ARTICLES •
Design, synthesis and evaluation of anti-inflammatory effect of novel berberine derivatives on IL-6/STAT signaling pathway
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Qing-xuan ZENG, Na ZHANG, Hong-bin DENG, Dan-qing SONG, Jian-dong JIANG, Yan-xiang WANG*
Affiliations
  • Institute of Medicinal Biotechnology, China Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2017-12-12 doi: 10.16438/j.0513-4870.2017-0835
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Interleukin-6 (IL-6)/signal transducers and activators of transcription (STAT) signaling pathway is closely related to the development and progression of atherosclerosis (AS). Taking Chinese natural product berberine (BBR) as the leading compound, a series of novel BBR analogues defined on different types of substituents on position 3 or/and 9 were designed, synthesized and evaluated for their inhibitory activities on phosphorylation of STAT-1 and STAT-3 induced by IL-6. The structure-activity relationship indicated that introduction of rigid fragment on position 3 or 9 was beneficial for enhancing their activities. Among them, compounds 2b and 9 exhibited the most satisfactory potency. The study revealed that the compounds 2b and 9 exhibit anti-inflammatory potencies via activating AMPK, and down-regulation of phosphorylation of STAT1 and STAT3 induced by IL-6 in HUVEC cells. These results suggest that BBR derivatives may inhibit the inflammatory response mediated by the IL-6/STAT signaling pathway through regulation of AMPK, which provides useful insight into the development of BBR derivatives for treatment of atherosclerosis.

berberine  /  atherosclerosis  /  structure-activity relationship  /  IL-6  /  STAT-1/3
Qing-xuan ZENG, Na ZHANG, Hong-bin DENG, Dan-qing SONG, Jian-dong JIANG, Yan-xiang WANG. Design, synthesis and evaluation of anti-inflammatory effect of novel berberine derivatives on IL-6/STAT signaling pathway[J]. Acta Pharmaceutica Sinica, 2017 , 52 (12) : 1895 -1902 . DOI: 10.16438/j.0513-4870.2017-0835
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Year 2017 volume 52 Issue 12
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Article Info
doi: 10.16438/j.0513-4870.2017-0835
  • Receive Date：2017-08-28
  • Online Date：2026-01-14
  • Published：2017-12-12
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  • Received：2017-08-28
  • Revised：2017-09-27
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    Institute of Medicinal Biotechnology, China Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, 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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