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.

Chlorophyll-a derivatives in photodynamic therapy: effect of position of heptyl ether side-chains on in vivo photosensitizing activity

1996 ◽  
Vol 6 (1) ◽  
pp. 105-110 ◽  
Author(s):  
Ravindra K. Pandey ◽  
Scott Constantine ◽  
Dane A. Goff ◽  
Andrei N. Kozyrev ◽  
Thomas J. Dougherty ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Chlorophyll A ◽  
Side Chains ◽  
Therapy Effect

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 Preparation of Analogs of the Ether-Linked Dimer and Oligomer Components of Hematoporphyrin Derivative

1991 ◽  
Vol 44 (3) ◽  
pp. 411 ◽  
Author(s):  
CJ Byrne ◽  
AD Ward
Keyword(s):  
Anticancer Drugs ◽  
Biological Properties ◽  
Side Chain ◽  
Side Chains ◽  
Hematoporphyrin Derivative ◽  
Porphyrin Dimers

The preparation of ether-linked porphyrin dimers and oligomers which are analogues of those present in the anticancer drugs hematoporphyrin derivative and Photofrin IIR is described. These materials are prepared from the appropriately substituted porphyrins containing a 1-hydroxyethyl or a vinyl side chain through an intermediate 1-bromoethyl derivative. Ether-linked porphyrin dimers with ethyl, formyl , hydroxymethyl and 1-alkoxyethyl side chains were prepared, together with trimers and tetramers containing ethyl side chains. Some of the spectroscopic and biological properties of these compounds are discussed.

The Effects of Some Synthetic Compounds on In Vitro Fibrinolytic Activity Measured by Different Methods and the Relevance to Activity In Vivo

1972 ◽  
Vol 28 (03) ◽  
pp. 351-358
Author(s):  
A.J Baillie ◽  
A. K Sim
Keyword(s):  
Inhibitory Activity ◽  
Substrate Concentration ◽  
Fibrinolytic Activity ◽  
Synthetic Compounds ◽  
In Vitro Methods ◽  
Narrow Concentration Range

SummaryThe activity of several synthetic compounds, rated from good to poor (or inactive) fibrinolytic activators, has been assessed by two different commonly-used in vitro methods. Compounds shown to be active over a narrow concentration range in the hanging clot test were shown to be inhibitors of plasmin and trypsin in the casein-olytic test. The inhibitory activity of these compounds was shown to increase with increasing substrate concentration and apparent activity in the hanging clot test. Possible explanations and relevance of these observations are discussed.

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>

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Potential for Treatment of Neurodegenerative Diseases with Natural Products or Synthetic Compounds that Stabilize Microtubules

2020 ◽  
Vol 26 (35) ◽  
pp. 4362-4372
Author(s):  
John H. Miller ◽  
Viswanath Das
Keyword(s):  
Natural Products ◽  
Neurodegenerative Diseases ◽  
In Vivo Models ◽  
Synthetic Compounds ◽  
Stabilizing Agents ◽  
Animal Models Of Disease ◽  
Model Studies ◽  
Models Of Disease

No effective therapeutics to treat neurodegenerative diseases exist, despite significant attempts to find drugs that can reduce or rescue the debilitating symptoms of tauopathies such as Alzheimer’s disease, Parkinson’s disease, frontotemporal dementia, amyotrophic lateral sclerosis, or Pick’s disease. A number of in vitro and in vivo models exist for studying neurodegenerative diseases, including cell models employing induced-pluripotent stem cells, cerebral organoids, and animal models of disease. Recent research has focused on microtubulestabilizing agents, either natural products or synthetic compounds that can prevent the axonal destruction caused by tau protein pathologies. Although promising results have come from animal model studies using brainpenetrant natural product microtubule-stabilizing agents, such as paclitaxel analogs that can access the brain, epothilones B and D, and other synthetic compounds such as davunetide or the triazolopyrimidines, early clinical trials in humans have been disappointing. This review aims to summarize the research that has been carried out in this area and discuss the potential for the future development of an effective microtubule stabilizing drug to treat neurodegenerative disease.

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