Delivery of Oligonucleotides to the Liver with GalNAc – From Research to Registered Therapeutic Drug

Scientists highlight some of the recent chemistry and preclinical advances in this space leading to this large number of clinical candidates against a diverse range of targets in liver hepatocytes.
[Molecular Therapy]
Bae, M., Lee, Y., Pham, T. X., Hu, S., Park, Y.-K., & Lee, J.-Y. (2020). Astaxanthin inhibits the reduction of glycolysis during the activation of hepatic stellate cells. Life Sciences, 256, 117926. https://doi.org/10.1016/j.lfs.2020.117926 Cite
AbstractGraphical Abstract
Bookmark

No account yet? Register

0
Share

Astaxanthin Inhibits the Reduction of Glycolysis during the Activation of Hepatic Stellate Cells

Compared with quiescent hepatic stellate cells (HSCs), activated HSCs (aHSCs) had significantly lower expression of glucose transporter 1, the major glucose transporter in HSCs, and its transcription factor hypoxia-inducible factor 1α, which was markedly increased by astaxanthin in aHSCs.
[Life Sciences]
Bae, M., Lee, Y., Pham, T. X., Hu, S., Park, Y.-K., & Lee, J.-Y. (2020). Astaxanthin inhibits the reduction of glycolysis during the activation of hepatic stellate cells. Life Sciences, 256, 117926. https://doi.org/10.1016/j.lfs.2020.117926 Cite
Abstract
Bookmark

No account yet? Register

0
Share

Hydrazinocurcumin and 5-Fluorouracil Enhance Apoptosis and Restrain Tumorigenicity of HepG2 Cells via Disrupting the PTEN-Mediated PI3K/Akt Signaling Pathway

Scientists investigated the role and mechanism of hydrazinocurcumin (HZC) in regulating HepG2 cell apoptosis and tumorigenicity, and its synergistic effects with 5-fluorouracil (5-Fu). HepG2 cells were treated with HZC and/or 5-Fu to analyze the possible synergistic effects on cell proliferation, apoptosis and cell cycle distribution in vitro using EdU staining.
[Biomedicine & PharmacoTherapy]
Zhou, Y., Zhang, M., Zhang, Z., Jia, Y., Zhang, C., & Peng, L. (2020). Hydrazinocurcumin and 5-fluorouracil enhance apoptosis and restrain tumorigenicity of HepG2 cells via disrupting the PTEN-mediated PI3K/Akt signaling pathway. Biomedicine & Pharmacotherapy, 129, 109851. https://doi.org/10.1016/j.biopha.2020.109851 Cite
Full ArticleGraphical Abstract
Bookmark

No account yet? Register

0
Share

SOX9 Enhances Sorafenib Resistance through Upregulating ABCG2 Expression in Hepatocellular Carcinoma

The authors found that sorafenib treatment increased the proportion of SOX9 positive cells in hepatocellular carcinoma (HCC) cell lines. Overexpression of exogenous SOX9 in HCC increased sorafenib resistance both in vitro and in vivo, whereas down-regulation led to inhibition of sorafenib resistance.
[Biomedicine & PharmacoTherapy]
Wang, M., Wang, Z., Zhi, X., Ding, W., Xiong, J., Tao, T., Yang, Y., Zhang, H., Zi, X., Zhou, W., & Huang, G. (2020). SOX9 enhances sorafenib resistance through upregulating ABCG2 expression in hepatocellular carcinoma. Biomedicine & Pharmacotherapy, 129, 110315. https://doi.org/10.1016/j.biopha.2020.110315 Cite
Full ArticleGraphical Abstract
Bookmark

No account yet? Register

0
Share

Anti-Inflammatory, Hepatoprotective and Antioxidant Activity of Ellagitannin Isolated from Melaleuca styphelioides

The hepatoprotective activity of styphelioidin was tested using the CCl4-challenged HepG2 cell model by measuring alanine aminotransferase and aspartate aminotransferase levels in HepG2 cells treated with styphelioidin for one hour followed by 40 mM CCl4.
[Phytochemistry]
Al-Sayed, E., Korinek, M., Esmat, A., Chen, G.-Y., Cheng, Y.-B., Hsieh, P.-W., Chen, B.-H., & Hwang, T.-L. (2020). Anti-inflammatory, hepatoprotective and antioxidant activity of ellagitannin isolated from Melaleuca styphelioides. Phytochemistry, 177, 112429. https://doi.org/10.1016/j.phytochem.2020.112429 Cite
AbstractGraphical Abstract
Bookmark

No account yet? Register

0
Share

Asiatic Acid Ameliorates Acute Hepatic Injury by Reducing Endoplasmic Reticulum Stress and Triggering Hepatocyte Autophagy

Researchers investigated the effects and underlying mechanisms of Asiatic acid from Potentilla chinensis on acute liver injury (ALI). The model of ALI in mice was induced by administration with Lipopolysaccharide/D-Galactosamine.
[Biomedicine & PharmacoTherapy]
Pang, X., Qiao, Q., Vonglorkham, S., Feng, Z., Pang, L., Chen, S., Wang, D., Lao, L., Lin, X., & Wei, J. (2020). Asiatic acid ameliorates acute hepatic injury by reducing endoplasmic reticulum stress and triggering hepatocyte autophagy. Biomedicine & Pharmacotherapy, 129, 110375. https://doi.org/10.1016/j.biopha.2020.110375 Cite
Full Article
Bookmark

No account yet? Register

0
Share

MicroRNA200a Enhances Antitumor Effects in Combination with Doxorubicin in Hepatocellular Carcinoma

Scientists investigated the effects of specific microRNA-200a (miR-200a) on hepatocellular carcinoma (HCC) tumor cell growth and effect of doxorubicin-mediated cytotoxicity. Their results showed miR-200a to be downregulated in human HCC and HCC tumor cell lines.
[Translational Oncology]
Cui, X., Zhou, D., Du, Q., Wan, P., Dong, K., Hou, H., & Geller, D. A. (2020). MicroRNA200a Enhances Antitumor Effects in Combination with Doxorubicin in Hepatocellular Carcinoma. Translational Oncology, 13(10), 100805. https://doi.org/10.1016/j.tranon.2020.100805 Cite
Full Article
Bookmark

No account yet? Register

0
Share

Plasma Membrane Vesicles of Human Umbilical Cord Mesenchymal Stem Cells Ameliorate Acetaminophen-Induced Damage in HepG2 Cells: A Novel Stem Cell Therapy

PMVs from human umbilical cord (hUC) MSCs were prepared with an improved procedure including a chemical enucleation step followed by a mechanical extrusion. Plasma membrane vesicles of hUCMSCs were characterized and supplemented to hepatocyte cultures.
[Stem Cell Research & Therapy]
Lin, M., Li, S., Yang, L., Ye, D., Xu, L., Zhang, X., … Wei, C. (2020). Plasma membrane vesicles of human umbilical cord mesenchymal stem cells ameliorate acetaminophen-induced damage in HepG2 cells: a novel stem cell therapy. Stem Cell Research & Therapy, 11(1), 225. https://doi.org/10.1186/s13287-020-01738-z Cite
Full Article
Bookmark

No account yet? Register

0
Share

Inventiva’s Lanifibranor Meets the Primary and Key Secondary Endpoints in the Phase IIb NATIVE Clinical Trial in Non-Alcoholic Steatohepatitis (NASH)

Inventiva are developing oral small molecule therapies for the treatment of non-alcoholic steatohepatitis (NASH), mucopolysaccharidoses and other diseases with significant unmet medical need. They have announced positive topline results from the Phase IIb NAsh Trial to Validate IVA337 Efficacy (NATIVE) clinical trial evaluating lanifibranor for the treatment of NASH.
[Inventiva]
Inventiva’s lanifibranor meets the primary and key secondary endpoints in the Phase IIb NATIVE clinical trial in non-alcoholic steatohepatitis (NASH Paris Stock Exchange:IVA. (n.d.). Retrieved June 17, 2020, from https://www.globenewswire.com/news-release/2020/06/15/2048284/0/en/Inventiva-s-lanifibranor-meets-the-primary-and-key-secondary-endpoints-in-the-Phase-IIb-NATIVE-clinical-trial-in-non-alcoholic-steatohepatitis-NASH.html Cite
Full ArticlePress Release
Bookmark

No account yet? Register

0
Share

Simulating the Human Colorectal Cancer Microenvironment in 3D Tumor-Stroma Co-Cultures In Vitro and In Vivo

Researchers successfully converted three in-house-derived primed human PSC lines to a naive state and an expanded pluripotent stem cell (EPS) state. Primed, naive and EPS cells displayed state-specific morphologies and expressed pluripotent markers.
[Scientific Reports]
Devarasetty, M., Dominijanni, A., Herberg, S., Shelkey, E., Skardal, A., & Soker, S. (2020). Simulating the human colorectal cancer microenvironment in 3D tumor-stroma co-cultures in vitro and in vivo. Scientific Reports, 10(1), 9832. https://doi.org/10.1038/s41598-020-66785-1 Cite
Full Article
Bookmark

No account yet? Register

0
Share

Roseotoxin B Alleviates Cholestatic Liver Fibrosis through Inhibiting PDGF-B/PDGFR-β Pathway in Hepatic Stellate Cells

Roseotoxin B was shown to possess an improving effect on cholestatic liver fibrosis in bile duct–ligated mice, as proved by histochemical and immunohistochemical staining, hepatic biochemical parameters, and TUNEL apoptotic cell detection in tissue sections.
[Cell Death & Disease]
Wang, X., Gao, Y., Li, Y., Huang, Y., Zhu, Y., Lv, W., Wang, R., Gou, L., Cheng, C., Feng, Z., Xie, J., Tian, J., & Yao, R. (2020). Roseotoxin B alleviates cholestatic liver fibrosis through inhibiting PDGF-B/PDGFR-β pathway in hepatic stellate cells. Cell Death & Disease, 11(6), 1–13. https://doi.org/10.1038/s41419-020-2575-0 Cite
Full Article
Bookmark

No account yet? Register

0
Share
Share