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| Preparation and pharmaceutical properties research of silybin phenolate derivatives |
| Hits 443 Download times 323 Received:March 12, 2023 |
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| DOI
10.11656/j.issn.1672-1519.2023.07.18 |
| Key Words
silybin;rosmarinic acid;danshensu;condensation reaction;drug evaluation;chronic hepatitis;hepatic fibrosis |
| Author Name | Affiliation | E-mail | | LUO Xi | Pharmacy Department, Tianjin Chest Hospital, Tianjin 300051, China | | | AN Zizheng | TIPR New Drug Evaluation Center, Tianjin 300301, China | | | ZHOU Wen | School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory of Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin 300070, China | | | LI Shuo | Parmacy Department, Tianjin Hedong District Dawangzhuang Street Community Health Service Center, Tianjin 300171, China | 18622306770@qq.com。 | | ZHANG Mujun | School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory of Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin 300070, China | |
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| Abstract
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| [Objective] The molecular structure of silybin was modified by esterification and condensation reaction to produce salvianolic acid ester derivatives，and its drug property were preliminarily studied. [Methods] The silybin rosemary ester（RA-SLB） and silybin danshensu ester（DSS-SLB） were obtained by esterification Condensation reaction of silybin（SLB） with the active components of salvia miltiorrhiza（RA） and danshensu（DSS），respectively. The structure of salvianolic acid ester derivatives was confirmed by hydrogen spectrum，carbon spectrum and mass spectrum，and the solubility differences between salvianolic acid ester derivatives and silybin were compared，and their anti-liver injury effects and the evaluation of the protective effect of fatty liver were studied. [Results] Compared with silybin，the solubility of salvianolic acid ester derivatives is significantly improved，and the stability in water is good. Compared with the model group of acute immune liver injury caused by scalan globulin，the low-dose group of RA-SLB significantly reduced the content of serum alanine aminotransferase（ALT），aspartate aminotransferase（AST） and lactate dehydrogenase（LDH）（P<0.05）. The DSS-SLB group had a tendency to improve liver function in the experimental scheme of liver injury caused by scalan globulin，but there was no statistical difference compared with the model group（P>0.05）. Compared with DL-ethionine induced fatty liver model group，RA-SLB group can significantly reduce the content of triglyceride（TG） in liver tissue（P<0.05），while other administration groups have no significant effect on the increase of TG content（P>0.05）. [Conclusion] RA-SLB has a significant effect on protecting liver injury and improving the activity of fatty liver，and has a good prospect of patent medicine. |
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