scholarly journals Pharmacokinetics of Photogem Using Fluorescence Spectroscopy in Dimethylhydrazine-Induced Murine Colorectal Carcinoma

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Raduan Hage ◽  
Juliana Ferreira ◽  
Vanderlei Salvador Bagnato ◽  
José Dirceu Vollet-Filho ◽  
Hélio Plapler
Keyword(s):  
Photodynamic Therapy ◽  
Colorectal Carcinoma ◽  
Fluorescence Spectroscopy ◽  
Wistar Rats ◽  
Fluorescence Spectra ◽  
Target Organ ◽  
Hematoporphyrin Derivative ◽  
Spectroscopy Technique ◽  
Normal Colon

This study aimed to investigate the pharmacokinetics of a hematoporphyrin derivative in colonic tumors induced by dimethylhydrazine and adjacent normal colon in Wistar rats using anin vivofluorescence spectroscopy technique. In conventional clinical application of photodynamic therapy, the interval between photosensitizer (PS) administration and lesion illumination is often standardized without taking into account variations due to the type or localization of the tumor and intrinsic differences in the microcirculation and vascular permeability of each target organ. The analysis of the fluorescence spectra was based on the intensity of porphyrin emission band centered at around 620 nm in normal colon and colon tumors. The photosensitizer fluorescence intensity rapidly grew for carcinoma and normal colon, reaching the maximum values 1 and 3 hours after PS injection, respectively. Data presented here allow us to verify that the best compromise between selectivity and drug concentration for colon carcinoma in rats took place in the interval between 1 to 4 h after PS injection.

The Photodynamic Therapy (PDT) Anticancer Activity of a Range of Porphyrin Dimers and Related Compounds Derived from Hematoporphyrin

2004 ◽  
Vol 57 (11) ◽  
pp. 1091 ◽  
Author(s):  
Christopher J. Byrne ◽  
Mathew A. Cooper ◽  
Prudence A. Cowled ◽  
Robert A. W. Johnstone ◽  
Lorraine Mackenzie ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Anticancer Activity ◽  
Side Chains ◽  
Hematoporphyrin Derivative ◽  
Synthetic Compounds ◽  
Photofrin Ii ◽  
Photodynamic Activity ◽  
Related Compounds ◽  
Porphyrin Dimers

The synthesis of diporphyrins and analogous compounds related to those present in the oligomeric fraction (Photofrin II) obtained from hematoporphyrin derivative (HPD) is described. The photodynamic activity of these compounds, in vivo, varies from inactive to as active as Photofrin II. Factors that are important in determining this anticancer activity of the synthetic compounds are the presence of hydrophobic side chains, as well as the propionic acid side chains of the hematoporphyrin derived materials, and the nature of the linking group between the porphyrins.

Ruthenium Complexes for 1- and 2-Photon Photodynamic Therapy: From In Silico Prediction to In Vivo Applications

2020 ◽  
Author(s):  
Johannes Karges ◽  
Shi Kuang ◽  
Federica Maschietto ◽  
Olivier Blacque ◽  
Ilaria Ciofini ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
In Silico ◽  
Aqueous Solubility ◽  
The Body ◽  
Photon Absorption ◽  
Multicellular Tumor Spheroids ◽  
Spectral Window ◽  
Photon Excitation ◽  
Polypyridine Complexes

<div>The use of photodynamic therapy (PDT) against cancer has received increasing attention overthe recent years. However, the application of the currently approved photosensitizers (PSs) is somehow limited by their poor aqueous solubility, aggregation, photobleaching and slow clearance from the body. To overcome these limitations, there is a need for the development of new classes of PSs with ruthenium(II) polypyridine complexes currently gaining momentum. However, these compounds generally lack significant absorption in the biological spectral window, limiting their application to treat deep-seated or large tumors. To overcome this drawback, ruthenium(II) polypyridine complexes designed in silico with (E,E’)-4,4´-bisstyryl 2,2´-bipyridine ligands showed impressive 1- and 2-Photon absorption up to a magnitude higher than the ones published so far. While non-toxic in the dark, these compounds were found phototoxic in various 2D monolayer cells, 3D multicellular tumor spheroids and be able to eradicate a multiresistant tumor inside a mouse model upon clinically relevant 1-Photon and 2 Photon excitation.</div>

Highly Potent rhenium(I) Tricarbonyl Complexes with Dual Anticancer and Anti-Angiogenic Activity Against Colorectal Carcinoma

2020 ◽  
Author(s):  
Joachim Delasoie ◽  
Aleksandar Pavic ◽  
Noémie Voutier ◽  
Sandra Vojnovic ◽  
Aurélien Crochet ◽  
...  
Keyword(s):  
Colorectal Carcinoma ◽  
Anticancer Drugs ◽  
Xenograft Model ◽  
Therapeutic Window ◽  
Low Doses ◽  
Sunitinib Malate ◽  
Angiogenic Activity ◽  
Antimetastatic Activity ◽  
Clinical Drugs

Synthesized and characterized a series of rhenium(I) trycarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity <i>in vivo</i> (zebrafish-human CRC xenograft model), being effective at very low doses (1-3 µM). At doses as high as 250 µM the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). The two compounds exceed the antiproliferative and anti-angiogenic potency of clinical drugs cisplatin and sunitinib-malate, and display a large therapeutic window.

Oral in vivo Bactofection in Dextran Sulfate Sodium Treated Female Wistar Rats

2010 ◽  
Vol 58 (3) ◽  
pp. 171-176 ◽  
Author(s):  
Roland Pálffy ◽  
Michal Behuliak ◽  
Roman Gardlík ◽  
Peter Jáni ◽  
L'udevít Kádaši ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Dextran Sulfate ◽  
Dextran Sulfate Sodium ◽  
Female Wistar Rats

scholarly journals Effects of systemic glycine on accumbal glycine and dopamine levels and ethanol intake in male Wistar rats

2020 ◽  
Author(s):  
Yasmin Olsson ◽  
Helga Höifödt Lidö ◽  
Klara Danielsson ◽  
Mia Ericson ◽  
Bo Söderpalm
Keyword(s):  
Wistar Rats ◽  
In Vivo Microdialysis ◽  
Ethanol Intake ◽  
Water Model ◽  
Glycine Transporter 1 ◽  
Improved Outcomes ◽  
Male Wistar Rats ◽  
Treatment Principle ◽  
Reward Pathway

AbstractApproved medications for alcohol use disorder (AUD) display modest effect sizes. Pharmacotherapy aimed at the mechanism(s) by which ethanol activates the dopamine reward pathway may offer improved outcomes. Basal and ethanol-induced accumbal dopamine release in the rat involve glycine receptors (GlyR) in the nucleus accumbens (nAc). Glycine transporter 1 (GlyT-1) inhibitors, which raise extracellular glycine levels, have repeatedly been shown to decrease ethanol intake in the rat. To further explore the rational for elevating glycine levels in the treatment of AUD, this study examined accumbal extracellular glycine and dopamine levels and voluntary ethanol intake and preference in the rat, after systemic treatment with glycine. The effects of three different doses of glycine i.p. on accumbal glycine and dopamine levels were examined using in vivo microdialysis in Wistar rats. In addition, the effects of the intermediate dose of glycine on voluntary ethanol intake and preference were examined in a limited access two-bottle ethanol/water model in the rat. Systemic glycine treatment increased accumbal glycine levels in a dose-related manner, whereas accumbal dopamine levels were elevated in a subpopulation of animals, defined as dopamine responders. Ethanol intake and preference decreased after systemic glycine treatment. These results give further support to the concept of elevating central glycine levels to reduce ethanol intake and indicate that targeting the glycinergic system may represent a pharmacologic treatment principle for AUD.

Porphyrin-lipid nanovesicles (Porphysomes) are effective photosensitizers for photodynamic therapy

Nanophotonics ◽  
2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Keegan Guidolin ◽  
Lili Ding ◽  
Juan Chen ◽  
Brian C. Wilson ◽  
Gang Zheng
Keyword(s):  
Photodynamic Therapy ◽  
Tumor Growth ◽  
Intrinsic Structure ◽  
Therapeutic Applications ◽  
Positron Emission ◽  
Theranostic Agents ◽  
Negative Controls ◽  
And Control ◽  
Complete Tumor

Abstract Porphysomes (PS) are liposome-like nanoparticles comprising pyropheophorbide-conjugated phospholipids that have demonstrated potential as multimodal theranostic agents for applications that include phototherapies, targeted drug delivery and in vivo fluorescence, photoacoustic, magnetic resonance or positron emission imaging. Previous therapeutic applications focused primarily on photothermal therapy (PTT) and suggested that PSs require target-triggered activation for use as photodynamic therapy (PDT) sensitizers. Here, athymic nude mice bearing subcutaneous A549 human lung tumors were randomized into treatment and control groups: PS-PDT at various doses, PS-only and no treatment negative controls, as well as positive controls using the clinical photosensitizer Photofrin. Animals were followed for 30 days post-treatment. PS-PDT at all doses demonstrated a significant tumor ablative effect, with the greatest effect seen with 10 mg/kg PS at a drug-light interval of 24 h. By comparison, negative controls (PS-only, Photofrin-only, and no treatment) showed uncontrolled tumor growth. PDT with Photofrin at 5 mg/kg and PS at 10 mg/kg demonstrated similar tumor growth suppression and complete tumor response rates (15 vs. 25%, p = 0.52). Hence, porphysome nanoparticles are an effective PDT agent and have the additional advantages of multimodal diagnostic and therapeutic applications arising from their intrinsic structure. Porphysomes may also be the first single all-organic agent capable of concurrent PDT and PTT.

scholarly journals Site-Specific Dual-Labeling of a VHH with a Chelator and a Photosensitizer for Nuclear Imaging and Targeted Photodynamic Therapy of EGFR-Positive Tumors

Cancers ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 428
Author(s):  
Emma Renard ◽  
Estel Collado Camps ◽  
Coline Canovas ◽  
Annemarie Kip ◽  
Martin Gotthardt ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Fluorescence Imaging ◽  
Ex Vivo ◽  
Growth Factor Receptor ◽  
Nuclear Imaging ◽  
A431 Cells ◽  
Site Specific ◽  
Variable Domains ◽  
Diagnostic Probe

Variable domains of heavy chain only antibodies (VHHs) are valuable agents for application in tumor theranostics upon conjugation to both a diagnostic probe and a therapeutic compound. Here, we optimized site-specific conjugation of the chelator DTPA and the photosensitizer IRDye700DX to anti-epidermal growth factor receptor (EGFR) VHH 7D12, for applications in nuclear imaging and photodynamic therapy. 7D12 was site-specifically equipped with bimodal probe DTPA-tetrazine-IRDye700DX using the dichlorotetrazine conjugation platform. Binding, internalization and light-induced toxicity of DTPA-IRDye700DX-7D12 were determined using EGFR-overexpressing A431 cells. Finally, ex vivo biodistribution of DTPA-IRDye700DX-7D12 in A431 tumor-bearing mice was performed, and tumor homing was visualized with SPECT and fluorescence imaging. DTPA-IRDye700DX-7D12 was retrieved with a protein recovery of 43%, and a degree of labeling of 0.56. Spectral properties of the IRDye700DX were retained upon conjugation. 111In-labeled DTPA-IRDye700DX-7D12 bound specifically to A431 cells, and they were effectively killed upon illumination. DTPA-IRDye700DX-7D12 homed to A431 xenografts in vivo, and this could be visualized with both SPECT and fluorescence imaging. In conclusion, the dichlorotetrazine platform offers a feasible method for site-specific dual-labeling of VHH 7D12, retaining binding affinity and therapeutic efficacy. The flexibility of the described approach makes it easy to vary the nature of the probes for other combinations of diagnostic and therapeutic compounds.

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