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肝靶向纳米颗粒提高黄芩苷的体外和体内生物利用度及抗乙肝病毒疗效。

Liver-Targeted Nanoparticles Facilitate the Bioavailability and Anti-HBV Efficacy of Baicalin In Vitro and In Vivo.

作者信息

Xu Weiming, Niu Yijun, Ai Xin, Xia Chengjie, Geng Ping, Zhu Haiyan, Zhou Wei, Huang Hai, Shi Xunlong

机构信息

Department of Biological Medicines & Shanghai Engineering Research Center of Immunotherapeutics, Fudan University School of Pharmacy, Shanghai 201203, China.

Department of Chemistry, Fudan University, 220 Han Dan Road, Shanghai 200433, China.

出版信息

Biomedicines. 2022 Apr 14;10(4):900. doi: 10.3390/biomedicines10040900.

DOI:10.3390/biomedicines10040900
PMID:35453650
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9025464/
Abstract

The anti-hepatitis B virus (HBV) efficacy of baicalin (BA) is mediated by HBV-related hepatocyte nuclear factors (HNFs). However, this efficacy is severely limited by the low bioavailability of BA. Therefore, a novel liver-targeted BA liposome was constructed to promote the bioavailability and antiviral ability of BA. The results showed that apolipoprotein A1 (ApoA1)-modified liposomes (BAA1) significantly enhanced BA's cellular uptake and specific distribution in the liver. Furthermore, the substantial inhibitory effects of BAA1 on HBsAg, HBeAg, HBV RNA, and HBV DNA were assessed in HB-infected cells and mice. Western blotting, co-immunoprecipitation, and transcriptomics analysis further revealed that the enhanced anti-HBV efficacy of BAA1 was attributed to the interaction between hepatocyte nuclear factors (HNFs) and estrogen receptors (ERs). Based on the findings, we propose that the ApoA1-modified liposomes aid BA in inhibiting HBV transcription and replication by augmenting its bioavailability and the HNFs-ERs axis.

摘要

黄芩苷（BA）的抗乙型肝炎病毒（HBV）功效由HBV相关的肝细胞核因子（HNFs）介导。然而，BA的低生物利用度严重限制了这种功效。因此，构建了一种新型的肝脏靶向BA脂质体，以提高BA的生物利用度和抗病毒能力。结果表明，载脂蛋白A1（ApoA1）修饰的脂质体（BAA1）显著增强了BA在细胞中的摄取以及在肝脏中的特异性分布。此外，在HB感染的细胞和小鼠中评估了BAA1对HBsAg、HBeAg、HBV RNA和HBV DNA的显著抑制作用。蛋白质免疫印迹法、免疫共沉淀法和转录组学分析进一步揭示，BAA1增强的抗HBV功效归因于肝细胞核因子（HNFs）与雌激素受体（ERs）之间的相互作用。基于这些发现，我们提出ApoA1修饰的脂质体通过提高BA的生物利用度以及HNFs-ERs轴来帮助BA抑制HBV转录和复制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/93ff8ad6905a/biomedicines-10-00900-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/5bc7154f30b3/biomedicines-10-00900-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/4c5a7e03033e/biomedicines-10-00900-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/cbca079db6c9/biomedicines-10-00900-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/a969be63e9e1/biomedicines-10-00900-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/144f70b67a87/biomedicines-10-00900-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/15aea4a73657/biomedicines-10-00900-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/633213a7eacb/biomedicines-10-00900-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/ebcbe02cc6a5/biomedicines-10-00900-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/93ff8ad6905a/biomedicines-10-00900-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/5bc7154f30b3/biomedicines-10-00900-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/4c5a7e03033e/biomedicines-10-00900-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/cbca079db6c9/biomedicines-10-00900-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/a969be63e9e1/biomedicines-10-00900-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/144f70b67a87/biomedicines-10-00900-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/15aea4a73657/biomedicines-10-00900-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/633213a7eacb/biomedicines-10-00900-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/ebcbe02cc6a5/biomedicines-10-00900-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eec2/9025464/93ff8ad6905a/biomedicines-10-00900-g009.jpg

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Research Progress of in the Treatment of Gastrointestinal Cancer.在胃肠道癌症治疗中的研究进展。
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