Esterification of Ginsenoside Rh2 Enhanced Its Cellular Uptake and Antitumor Activity in Human HepG2 Cells

2015 ◽  
Vol 64 (1) ◽  
pp. 253-261 ◽  
Author(s):  
Fang Chen ◽  
Ze-Yuan Deng ◽  
Bing Zhang ◽  
Zeng-Xing Xiong ◽  
Shi-Lian Zheng ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cellular Uptake ◽  
Hepg2 Cells ◽  
Ginsenoside Rh2

Improved Method for Obtaining of Arctigenin from Arctium Lappa L. and its Antiproliferative Effect on Human Hepatocarcinoma HepG2 Cells

2020 ◽  
Vol 16 (3) ◽  
pp. 358-362
Author(s):  
Renan S. Teixeira ◽  
Paulo H.D. Carvalho ◽  
Jair A.K. Aguiar ◽  
Valquíria P. Medeiros ◽  
Ademar A. Da Silva Filho ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Crude Extract ◽  
Hepg2 Cells ◽  
Liver Carcinoma ◽  
Adhesion Assay ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Arctium Lappa ◽  
Nih 3T3

Background: Arctigenin is a lignan found in Arctium lappa L. (Asteraceae) that displays anti-inflammatory activities. Previous studies showed that the crude extract of A. Lappa has antitumor activity in human liver carcinoma, lung and stomach cancer cells. The aim of this study was to obtain arctigenin from A. lappa L., as well as to evaluate its antiproliferative effects in cells of liver carcinoma (HepG2) and fibroblasts (NIH/3T3). Methods: Arctigenin was obtained from the hydrolysis of arctiin, which was isolated from the crude extract of A. lappa. The effects of arctigenin and arctiin on HepG2 cell viability and cell adhesion were analyzed by MTT method. Adhesion assay was also carried out to evaluate the antitumor activity. Results: Our results showed that the analytical process to obtain arctigenin was fast and easy. In vitro experiments showed that arctigenin (107-269 μM) decreased HepG2 cells viability and did not cause cytotoxicity on NIH/3T3 cells. Arctigenin (27-269 μM) demonstrated anti-adhesion in HepG2 cells in a concentration-dependent manner, when compared with control. Conclusion: These results suggest a promising pharmacological activity for arctigenin as an antiproliferative compound.

Specific modification and self-transport of porphyrins and their multi-mechanism cooperative antitumor studies

2021 ◽  
Vol 9 (14) ◽  
pp. 3180-3191
Author(s):  
Shuxin Jia ◽  
Shaochen Wang ◽  
Shanshan Li ◽  
Peng Hu ◽  
Shuling Yu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cellular Uptake ◽  
Treatment Effect ◽  
Specific Modification ◽  
Tumor Region

The introduction of TPGS increases the cellular uptake and antitumor activity of TAPP-TPGS. TAPP-TPGS/PTX with small size increases the enrichment of drug and photosensitizer in tumor region and has excellent biocompatibility and synergistic treatment effect of TPGS, chemotherapy and PDT.

The Effect and Mechanism of Apoptosis Induced by Desacetylcinobufotalin (DEBF) in Human Hepatocellular Carcinoma HepG2 Cells

2013 ◽  
Vol 395-396 ◽  
pp. 587-590
Author(s):  
Xu Chao ◽  
Lin Dang ◽  
Min Hui Wei
Keyword(s):  
Hepatocellular Carcinoma ◽  
Antitumor Activity ◽  
Western Blot ◽  
Hepg2 Cells ◽  
Human Hepatocellular Carcinoma ◽  
Inhibition Effect ◽  
Marked Inhibition ◽  
Mitochondria Pathway

The cytotoxicity of Desacetylcinobufotalin (DEBF) and apoptosis induced by DEBF was measured. Additionally the mechanism of Apoptosis induced by DEBF was studied through Western blot. The results show DEBF displayed the marked inhibition effect to HepG2 cells and the IC50value is 0.0279μmol/ml. The expression of Bax was significantly increased and the expression of Bcl-2 was markedly decreased, compared to the control. The data suggest DEBF had significant antitumor activity through induction apoptosis via mitochondria pathway.

scholarly journals Epigallocatechin Gallate-Gold Nanoparticles Exhibit Superior Antitumor Activity Compared to Conventional Gold Nanoparticles: Potential Synergistic Interactions

Nanomaterials ◽  
2019 ◽  
Vol 9 (3) ◽  
pp. 396 ◽  
Author(s):  
Suhash Chavva ◽  
Sachin Deshmukh ◽  
Rajashekhar Kanchanapally ◽  
Nikhil Tyagi ◽  
Jason Coym ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Nuclear Translocation ◽  
Epigallocatechin Gallate ◽  
Drug Carriers ◽  
Water Soluble ◽  
Tetrazolium Salt ◽  
Uptake Studies

Epigallocatechin gallate (EGCG) possesses significant antitumor activity and binds to laminin receptors, overexpressed on cancer cells, with high affinity. Gold nanoparticles (GNPs) serve as excellent drug carriers and protect the conjugated drug from enzymatic metabolization. Citrate-gold nanoparticles (C-GNPs) and EGCG-gold nanoparticles (E-GNPs) were synthesized by reduction methods and characterized with UV-visible spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering (DLS). Cytotoxicity of citrate, EGCG, C-GNPs, and E-GNPs was evaluated by the water-soluble tetrazolium salt (WST-1) assay. Nanoparticle cellular uptake studies were performed by TEM and atomic absorption spectroscopy (AAS). Dialysis method was employed to assess drug release. Cell viability studies showed greater growth inhibition by E-GNPs compared to EGCG or C-GNPs. Cellular uptake studies revealed that, unlike C-GNPs, E-GNPs were taken up more efficiently by cancerous cells than noncancerous cells. We found that E-GNP nanoformulation releases EGCG in a sustained fashion. Furthermore, data showed that E-GNPs induced more apoptosis in cancer cells compared to EGCG and C-GNPs. From the mechanistic standpoint, we observed that E-GNPs inhibited the nuclear translocation and transcriptional activity of nuclear factor-kappaB (NF-κB) with greater potency than EGCG, whereas C-GNPs were only minimally effective. Altogether, our data suggest that E-GNPs can serve as potent tumor-selective chemotoxic agents.

New approach for the synthesis, docking of new porphyrins and their antitumor activity

2019 ◽  
Vol 23 (03) ◽  
pp. 251-259 ◽  
Author(s):  
Eman H. Tawfik ◽  
Ahmed A. Fadda ◽  
Nanees N. Soliman ◽  
Laila Abou-Zeid ◽  
Amr Negm
Keyword(s):  
Molecular Docking ◽  
Antitumor Activity ◽  
Human Cell ◽  
Hepg2 Cells ◽  
Human Cell Lines ◽  
New Approach ◽  
Cytotoxicity Activity ◽  
Porphyrin Derivatives ◽  
New Compounds ◽  
Mcf 7

A new methodology for the synthesis of a new series of mesotetrakis[aryl]-21H,23H-porphyrin derivatives 5a–5d, 6a–6c, 7 and 8 is presented. Structures of new compounds were established based on both elemental and spectral data. Cytotoxicity activity of the newly synthesized compounds was investigated against two human cell lines MCF-7 and HepG2. Molecular docking was performed to investigate the binding between the most active porphyrin derivatives and Bcl-2 molecular biomarkers in HepG2 cells.

Controlled release of brefeldin A from electrospun PEG–PLLA nanofibers and their in vitro antitumor activity against HepG2 cells

2013 ◽  
Vol 33 (5) ◽  
pp. 2513-2518 ◽  
Author(s):  
Wanyun Liu ◽  
Junchao Wei ◽  
Ping Huo ◽  
Yunhua Lu ◽  
Yiwang Chen ◽  
...  
Keyword(s):  
Controlled Release ◽  
Antitumor Activity ◽  
Hepg2 Cells ◽  
Brefeldin A

scholarly journals Postprandial triglyceride-rich lipoproteins induce hepatic insulin resistance in HepG2 cells independently of their receptor-mediated cellular uptake

2011 ◽  
Vol 343 (1-2) ◽  
pp. 71-78 ◽  
Author(s):  
Tobias Tatarczyk ◽  
Christian Ciardi ◽  
Andreas Niederwanger ◽  
Michael Kranebitter ◽  
Josef R. Patsch ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Cellular Uptake ◽  
Hepg2 Cells ◽  
Hepatic Insulin Resistance ◽  
Postprandial Triglyceride

scholarly journals Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin–GnRH-III conjugates developed for targeted drug delivery

2018 ◽  
Vol 14 ◽  
pp. 756-771 ◽  
Author(s):  
Sabine Schuster ◽  
Beáta Biri-Kovács ◽  
Bálint Szeder ◽  
Viktor Farkas ◽  
László Buday ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Laser Scanning ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Dependent Manner ◽  
Binding Studies ◽  
Gnrh Receptors

Gonadotropin releasing hormone-III (GnRH-III), a native isoform of the human GnRH isolated from sea lamprey, specifically binds to GnRH receptors on cancer cells enabling its application as targeting moieties for anticancer drugs. Recently, we reported on the identification of a novel daunorubicin–GnRH-III conjugate (GnRH-III–[4Lys(Bu), 8Lys(Dau=Aoa)] with efficient in vitro and in vivo antitumor activity. To get a deeper insight into the mechanism of action of our lead compound, the cellular uptake was followed by confocal laser scanning microscopy. Hereby, the drug daunorubicin could be visualized in different subcellular compartments by following the localization of the drug in a time-dependent manner. Colocalization studies were carried out to prove the presence of the drug in lysosomes (early stage) and on its site of action (nuclei after 10 min). Additional flow cytometry studies demonstrated that the cellular uptake of the bioconjugate was inhibited in the presence of the competitive ligand triptorelin indicating a receptor-mediated pathway. For comparative purpose, six novel daunorubicin–GnRH-III bioconjugates have been synthesized and biochemically characterized in which 6Asp was replaced by D-Asp, D-Glu and D-Trp. In addition to the analysis of the in vitro cytostatic effect and cellular uptake, receptor binding studies with 125I-triptorelin as radiotracer and degradation of the GnRH-III conjugates in the presence of rat liver lysosomal homogenate have been performed. All derivatives showed high binding affinities to GnRH receptors and displayed in vitro cytostatic effects on HT-29 and MCF-7 cancer cells with IC50 values in a low micromolar range. Moreover, we found that the release of the active drug metabolite and the cellular uptake of the bioconjugates were strongly affected by the amino acid exchange which in turn had an impact on the antitumor activity of the bioconjugates.

Sign in / Sign up

Export Citation Format

Share Document