Preparation of quercetin-human serum albumin-nanoparticles and its inhibitory effects against NASH-induced liver fibrosis in vivo and in vitro
- VernacularTitle:槲皮素-白蛋白纳米粒的制备及其对NASH肝纤维化的体内外抑制作用
- Author:
Ziying CHEN
1
;
Wei ZHANG
1
;
Ping QIN
1
;
Yongmiao CHEN
2
;
Chuanping ZHANG
3
;
Junwei LI
3
;
Ali CHEN
1
Author Information
1. School of Chemistry and Chemical Engineering，Guangdong Pharmaceutical University，Guangzhou 510006，China
2. Dept. of Pharmacy，the First Affiliated Hospital of Guangdong Pharmaceutical University，Guangzhou 501080，China
3. Hutchison Whampoa Guangzhou Baiyunshan Chinese Medicine Company Limited，Guangzhou 510515，China
- Publication Type:Journal Article
- Keywords:
quercetin;
quercetin-human serum albumin-
- From:
China Pharmacy
2022;33(8):930-936
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To prepare quercetin-human serum albumin-nanoparticles （Que-HSA-NPs），and to evaluate the in vivo and in vitro inhibitory effects of Que-HSA-NPs on hepatic fibrosis of non-alcoholic steatohepatitis （NASH）. METHODS Que-HSA-NPs were prepared by desolvation-chemical cross-linking method ，their appearance characteristics were observed ，and their particle size ，polydispersity index （PDI），Zeta potential and drug loading were detected. Quercetin （Que）and Que-HSA-NPs were applied to murine HSC-T 6 cells. The effects of them on survival rate of HSC-T 6，mRNA expression of transforming growth factor β（TGF-β），Type Ⅰ collagen α1（COL1A1）and α-smooth muscle actin （α-SMA）were compared. Que and Que-HSA-NPs were applied to mice fed with low methionine and choline deficient high-fat diet. The serum levels of liver injury indexes ，liver pathological characteristics ，mRNA expressions of TGF-β，COL1A1 and α-SMA，protein expression of α-SMA in liver tissue were determined to evaluate the improvement effects of them on hepatic fibrosis of NASH in mice. RESULTS The prepared Que-HSA-NPs was spherical ，the particle size was （172.9±2.2）nm，the PDI was 0.233，the Zeta potential was －29.2 mV，and the drug loading was 2.99％. Que and Que-HSA-NPs were nontoxic to HSC-T 6 at concentrations of 0-250 μg/mL. Both of them could significantly decrease mRNA expressions of TGF-β，COL1A1 and α-SMA，especially Que-HSA-NPs （P＜0.05）. They also could significantly decrease the serum levels of liver inju ry index ，relieve liver injury and down-regulate mRNA expressions of TGF-β，COL1A1 and α-SMA and protein expression of α-SMA， especially Que-HSA-NPs （P＜0.05）. CONCLUSIONS Que- HSA-NPs is successfully prepared ，and confirm that its anti- NASH hepatic fibrosis effect is better than that of Que .
