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Synthesis and hepatoprotective activity of Mannich base derivatives of silybin
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Bao-jun WANG1, 2, 3, Min HAN2, 3, Zhi-yao LI2, 3, Jing CAO2, 3, Gen-bei WANG2, 3, Yi HE2, 3, *, Zhong-yu DUAN1, *
Acta Pharmaceutica Sinica | 2018, 53(5) : 771 - 777
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Acta Pharmaceutica Sinica | 2018, 53(5): 771-777
• ORIGINAL ARTICLES·Medicinal Chemistry •
Synthesis and hepatoprotective activity of Mannich base derivatives of silybin
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Bao-jun WANG1, 2, 3, Min HAN2, 3, Zhi-yao LI2, 3, Jing CAO2, 3, Gen-bei WANG2, 3, Yi HE2, 3, *, Zhong-yu DUAN1, *
Affiliations
  • 1. School of Chemical Engineering, Hebei University of Technology, Tianjin 300131, China
  • 2. TCM Research Center, Tasly Group Co., Ltd., Tianjin 300410, China
  • 3. State Key Laboratory of Critical Technology in Innovative Chinese Medicine, Tasly Group Co. Ltd, Tianjin 300410, China
Published: 2018-05-12 doi: 10.16438/j.0513-4870.2017-1200
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Two novel Mannich base derivatives of silybin, SLB-DEA and DHSLB-PIP, were designed and synthesized. All the structures of new Mannich base derivatives of silybin were characterized by 1H NMR and HR-MS. Their protective action against CCl4-induced liver injury in mice were investigated. The changes of alanine aminotransferase (ALT), aspartate transaminase (AST), lactate dehydrogenase (LDH), total cholesterol (TC) and triglyceride (TG) were determined and the histopathological changes in liver tissues were examined. Pretreatment with a higher dosage of DHSLB-PIP (40 mg·kg-1) prevented CCl4-induced liver injury as indicated by the reduced levels of ALT, AST, LDH and TG. Meanwhile, liver histopathological improvement was observed in the model groups. The pharmacokinetics study in rats showed that the relative bioavailability of SLB-DEA and DHSLB-PIP were 172.5% and 259.8% compared with silybin. All the results suggest that SLB-DEA and DHSLB-PIP may protect liver against injury by CCl4 and the relative bioavailability was significantly increased, which is worth of further investigation for their druggability.

silybin derivatives  /  structure modification  /  Mannich reaction  /  biological activity  /  relative bioavailability
Bao-jun WANG, Min HAN, Zhi-yao LI, Jing CAO, Gen-bei WANG, Yi HE, Zhong-yu DUAN. Synthesis and hepatoprotective activity of Mannich base derivatives of silybin[J]. Acta Pharmaceutica Sinica, 2018 , 53 (5) : 771 -777 . DOI: 10.16438/j.0513-4870.2017-1200
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Article Info
doi: 10.16438/j.0513-4870.2017-1200
  • Receive Date：2017-12-04
  • Online Date：2026-01-15
  • Published：2018-05-12
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  • Received：2017-12-04
  • Revised：2018-01-29
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Affiliations
    1. School of Chemical Engineering, Hebei University of Technology, Tianjin 300131, China
    2. TCM Research Center, Tasly Group Co., Ltd., Tianjin 300410, China
    3. State Key Laboratory of Critical Technology in Innovative Chinese Medicine, Tasly Group Co. Ltd, Tianjin 300410, 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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