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Lipidation of polyethylenimine-based polyplex increases serum stability of bioengineered RNAi agents and offers more consistent tumoral gene knockdown in vivo
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Qian-Yu Zhang, Pui Yan Ho, Mei-Juan Tu, Joseph L. Jilek, Qiu-Xia Chen, Su Zeng, Ai-Ming YuAbstractRecently we have established a novel approach to produce bioengineered noncoding RNA agents (BERAs) in living cells that carry target RNAi molecules (e.g., siRNA and miRNA) and thus act as “prodrugs”. Using GFP-siRNA-loaded BERA (BERA/GFP-siRNA) as a model molecule, this study was to define the in vitro and in vivo knockdown efficiency of BERAs delivered by liposome-polyethylenimine nanocomplex (lipopolyplex o...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Hispidulin inhibits hepatocellular carcinoma growth and metastasis through AMPK and ERK signaling mediated activation of PPAR γ
Publication date: July 2018 Source:Biomedicine & Pharmacotherapy, Volume 103 Author(s): Mei Han, Hui Gao, Ping Ju, Ming-quan Gao, Yin-ping Yuan, Xue-hong Chen, Kai-li Liu, Yan-tao Han, Zhi-wu Han Hispidulin, a phenolic flavonoid, exerts potent cytotoxicity towards a variety of human cancers. However, the effects of hispidulin on hepatocellular carcinoma (HCC) and underlying molecular mechanisms of its action remain elusive. The present study investigated the effect of hispidulin on HCC in experimental models, including tumor cell lines and mouse tumor xenograft. Results demonstrated that hispidulin was cytotoxic a...
Source: Biomedicine and Pharmacotherapy - April 25, 2018 Category: Drugs & Pharmacology Source Type: research

LINC00963 promotes hepatocellular carcinoma progression by activating PI3K/AKT pathway.
CONCLUSIONS: Our data revealed that LINC00963 was upregulated in HCC, which significantly extended the G0/G1 phase of HCC cells by activating PI3K/AKT pathway and promoting the proliferative ability of HCC cells. LINC00963 may be involved in the HCC development. PMID: 29630107 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - April 10, 2018 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

E4bp4 Regulates Carboxylesterase 2 Enzymes through Repression of the Nuclear Receptor Rev-erb α in Mice.
In conclusion, E4bp4 regulates Ces enzymes through inhibition of the transrepression activity of Rev-erbα, thereby impacting the metabolism and pharmacokinetics of Ces substrates. PMID: 29653076 [PubMed - as supplied by publisher]
Source: Pharmacological Reviews - April 10, 2018 Category: Drugs & Pharmacology Authors: Zhao M, Zhang T, Yu F, Guo L, Wu B Tags: Biochem Pharmacol Source Type: research

Reversal effect of quercetin on multidrug resistance via FZD7/ β-catenin pathway in hepatocellular carcinoma cells
Conclusion : Overall, these data suggested the effectiveness of using quercetin, at least in part, via inhibiting FZD7 to combat chemoresistance and showed that quercetin could be developed into an efficient natural sensitizer for resistant human hepatocellular carcinoma. Graphical abstract
Source: Phytomedicine - March 20, 2018 Category: Drugs & Pharmacology Source Type: research

Cisplatin induces apoptosis of hepatocellular carcinoma LM3 cells via down-regulation of XIAP.
CONCLUSIONS: Downregulation of XIAP enhanced the proapoptotic effect of cisplatin on LM3 cells, suggesting that XIAP might be used as a potential target in the treatment of liver cancer. PMID: 29424923 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - February 11, 2018 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

Chelerythrine inhibits human hepatocellular carcinoma metastasis in vitro.
In this study, we investigated the effects of Chelerythrine on the migration and invasion of the human hepatocellular carcinoma cell line Hep3B. MTT, wounding healing, transwell migration and invasion assays and cytoskeleton staining demonstrated that CHE could inhibit the migration and invasion of Hep3B cells in a dose-dependent manner with change of cell structure. RNA interference studies made a knockdown of MMP (matrix metalloproteinase)-2/9 respectively in Hep3B cells. And the results of wounding healing and transwell invasion assay with the treatment of siRNA investigated that MMP-2/9 are positively associated with H...
Source: Biological and Pharmaceutical Bulletin - October 31, 2017 Category: Drugs & Pharmacology Authors: Zhu Y, Pan Y, Zhang G, Wu Y, Zhong W, Chu C, Qian Y, Zhu G Tags: Biol Pharm Bull Source Type: research

Clofibrate Attenuates ROS Production by Lipid Overload in Cultured Rat Hepatoma Cells.
CONCLUSIONS: Characteristic cellular damage resulted from released ROS following a high fat load to hepatoma cells. The damage was attenuated through early treatment with clofibrate, which may act as a hepatoprotectant by inducing FABP1 expression and in this manner, suppress intracellular ROS levels. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page. PMID: 28810950 [PubMed - in process]
Source: Journal of Pharmacy and Pharmaceutical Sciences - August 18, 2017 Category: Drugs & Pharmacology Tags: J Pharm Pharm Sci Source Type: research

The study on expression of CIAPIN1 interfering hepatocellular carcinoma cell proliferation and its mechanisms.
CONCLUSIONS: CIAPIN1 played an important role in the proliferation of liver cancer cells through increasing the expressions of cell cycle related proteins Cyclin D1, CDK2, CDK4, and Cyclin E. PMID: 28742201 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - July 27, 2017 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

Hypoxia promotes epithelial-mesenchymal transition of hepatocellular carcinoma cells via inducing Twist1 expression.
CONCLUSIONS: Hypoxia promotes hepatocellular carcinoma cells SMMC-7721 EMT by upregulating the expression of Twist1. PMID: 28742200 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - July 27, 2017 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

Physcion 8-O- β-glucopyranoside suppresses tumor growth of Hepatocellular carcinoma by downregulating PIM1.
This study is aimed to investigate the anti-tumor activity of physcion 8-O-β-glucopyranoside (PG) in HCC. Our results have showed that PG significantly suppresses cell growth and induces apoptosis in vitro and in vivo. At molecular level, PG represses the expression of Pim family kinases 1 (PIM1), which is responsible for the anti-tumor effect of PG in HCC. Ectopic over-expression of PIM1 significantly abrogates the suppressing effect of PG on cell growth and inducing effect of PG on apoptosis. In contrast, knockdown of PIM1 by siRNA enhances the anti-tumor effect of PG in HCC cells. PMID: 28570979 [PubMed - as supplied by publisher]
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - May 29, 2017 Category: Drugs & Pharmacology Authors: Wang Q, Jiang Y, Guo R, Lv R, Liu T, Wei H, Ming H, Tian X Tags: Biomed Pharmacother Source Type: research

Protein phosphatase 2A regulation of markers of extracellular matrix remodelling in hepatocellular carcinoma cells: functional consequences for tumour invasion
Conclusion and ImplicationsOA increased MMP‐9 by decreasing PP2A activity and PP2Ac, through AP‐1 binding sites on the MMP‐9 promoter. The functional consequence of this and CIP2A overexpression was increased cell migration. Hence, PP2A inhibition induced a metastatic phenotype through alterations in MMP‐9 in Hep3B cells.
Source: British Journal of Pharmacology - April 7, 2017 Category: Drugs & Pharmacology Authors: M P Ward, J P Spiers Tags: RESEARCH PAPER Source Type: research

Guggulsterone sensitized drug-resistant human hepatocarcinoma cells to doxorubicin through a Cox-2/P-gp dependent pathway.
Abstract Previous researches indicated that cyclooxygenase-2 (Cox-2) might be involved in P-glycoprotein (P-gp)-mediated multidrug resistance in hepatocellular carcinoma cells. Doxorubicin-resistant hepatocellular carcinoma PLC/PRF/5 cells (PLC/PRF/5R) and HepG2 (HepG2R) cells were developed in the present study. The modulatory effect of guggulsterone on Cox-2 and P-gp in PLC/PRF/5R and HepG2R cells was investigated. Cells proliferation, Cox-2 and P-gp expression, and prostaglandin E2 release were examined using MTT, flow cytometry, western blot and ELISA assays. Small interfering RNA (siRNA) targeted against Cox-...
Source: European Journal of Pharmacology - March 23, 2017 Category: Drugs & Pharmacology Authors: Xu HB, Fu J, Huang F, Yu J Tags: Eur J Pharmacol Source Type: research

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