Charge Dependence of Cellular Uptake and Selective Antitumor Activity of Porphyrazines

2005 ◽  
Vol 48 (26) ◽  
pp. 8125-8133 ◽  
Author(s):  
Neal D. Hammer ◽  
Sangwan Lee ◽  
Benjamin J. Vesper ◽  
Kim M. Elseth ◽  
Brian M. Hoffman ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cellular Uptake ◽  
Charge Dependence

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.

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.

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.

Cellular uptake and antitumor activity of the new anthracycline analog DA-125 in human cancer cell lines

1997 ◽  
Vol 40 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Kyoung-Hwa Lim ◽  
Hun-Sik Kim ◽  
Yong-Man Yang ◽  
Sang-Deuk Lee ◽  
Won-Bae Kim ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cellular Uptake ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

scholarly journals Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin–GnRH-III bioconjugates

2012 ◽  
Vol 56 ◽  
pp. 155-165 ◽  
Author(s):  
Rózsa Hegedüs ◽  
Marilena Manea ◽  
Erika Orbán ◽  
Ildikó Szabó ◽  
Éva Kiss ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Antitumor Activity ◽  
Cellular Uptake ◽  
Short Chain Fatty Acid ◽  
Chain Fatty Acid ◽  
Short Chain

scholarly journals Pt(IV)-based nanoscale coordination polymers: Antitumor activity, cellular uptake and interactions with nuclear DNA

2018 ◽  
Vol 340 ◽  
pp. 94-102 ◽  
Author(s):  
N.N. Adarsh ◽  
Carolina Frias ◽  
T.M. Ponnoth Lohidakshan ◽  
Julia Lorenzo ◽  
Fernando Novio ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cellular Uptake ◽  
Coordination Polymers ◽  
Nuclear Dna ◽  
Nanoscale Coordination Polymers

In Vitro and In Vivo Evaluation of Novel DTX-Loaded Multifunctional Heparin-Based Polymeric Micelles Targeting Folate Receptors and Endosomes

2020 ◽  
Vol 15 (4) ◽  
pp. 341-359
Author(s):  
Moloud Kazemi ◽  
Jaber Emami ◽  
Farshid Hasanzadeh ◽  
Mohsen Minaiyan ◽  
Mina Mirian ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antitumor Activity ◽  
Cellular Uptake ◽  
Folate Receptor ◽  
Chemotherapeutic Agents ◽  
Water Soluble ◽  
Growth Monitoring ◽  
Tumor Bearing

Background: The development of biocompatible tumor-targeting delivery systems for anticancer agents is essential for efficacious cancer chemotherapy. Nanoparticles, as drug delivery cargoes for cancer therapy, are rapidly improving to overcome the limitations of conventional chemotherapeutic agents. Heparin–modified nanoparticles are currently being considered as one of the favorable carriers for the delivery of chemotherapeutics to cancer tissues. Objective: This study was aimed at evaluating the in vitro and in vivo antitumor activity of a novel targeted, pH-sensitive, heparin-based polymeric micelle loaded with the poorly water-soluble anticancer drug, docetaxel (DTX). The micelles could overcome the limited water solubility, non-specific distribution, and insufficient drug concentration in tumor tissues. Methods: DTX-loaded folate targeted micelles were prepared and evaluated for physicochemical properties, drug release, in vitro cellular uptake and cytotoxicity in folate receptor-positive and folate receptor-negative cells. Furthermore, the antitumor activity of DTX-loaded micelles was evaluated in the tumor-bearing mice. Some related patents were also studied in this research. Results: The heparin-based targeted micelles exhibited higher in vitro cellular uptake and cytotoxicity against folate receptor over-expressed cells due to the specific receptor-mediated endocytosis. DTX-loaded micelles displayed greater antitumor activity, higher anti-angiogenesis effects, and lower systemic toxicity compared with free DTX in a tumor-induced mice model as confirmed by tumor growth monitoring, immunohistochemical evaluation, and body weight shift. DTX-loaded targeting micelles demonstrated no considerable toxicity on major organs of tumor-bearing mice compared with free DTX. Conclusion: Our results indicated that DTX-loaded multifunctional heparin-based micelles with desirable antitumor activity and low toxicity possess great potential as a targeted drug delivery system in the treatment of cancer.

scholarly journals Cellular Uptake and Antitumor Activity of DOX-hyd-PEG-FA Nanoparticles

PLoS ONE ◽  
2014 ◽  
Vol 9 (5) ◽  
pp. e97358 ◽  
Author(s):  
Wei-liang Ye ◽  
Jiang-bo Du ◽  
Bang-le Zhang ◽  
Ren Na ◽  
Yan-feng Song ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cellular Uptake

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

Tumor-targeted co-delivery of mitomycin C and 10-hydroxycamptothecin via micellar nanocarriers for enhanced anticancer efficacy

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 23022-23033 ◽  
Author(s):  
Jinyan Lin ◽  
Yang Li ◽  
Hongjie Wu ◽  
Xiangrui Yang ◽  
Yanxiu Li ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Mitomycin C ◽  
Cellular Uptake ◽  
Anticancer Efficacy ◽  
Tumor Accumulation

Polymer–lipid hybrid micelles co-delivered hydrophilic mitomycin C and hydrophobic 10-hydroxycamptothecin showed improved cellular uptake and cytotoxicity in vitro and enhanced tumor accumulation and antitumor activity in vivo.

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