The in vivo characteristics of four analogues of benzoporphyrin derivative (BPD) have been investigated. Biodistribution data obtained in DBA/2J mice with BPD-MA (monoacid ring A analogue) which had been tritiated or internally labelled with 14C showed that both labelled materials acted in an essentially identical manner during the period of study. Biodistribution and clearance studies showed that relative distribution in a variety of mouse tissues was similar for all BPD analogues. M1 tumour cells (rhabdomyosarcoma in DBA/2J mice) taken from tumours excised from animals treated 3 h earlier with BPD, and tested in vitro for photosensitivity provided evidence that significant levels of photosensitiser detected in tumour was both active and associated with tumour cells. The monoacid forms of BPD were found to be much more photodynamically active in this test than were the diacid analogues. The ability of the analogues to ablate tumours in mice by photodynamic therapy was also tested. Again, BPD-MA and BPD-MB proved to be measurably better than the diacid analogues. These findings are discussed in reference to structural and physical differences between the analogues.
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http://dx.doi.org/10.1038/bjc.1991.18 | DOI Listing |
Energy Fuels
September 2024
Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
A novel series of Zn--AB porphyrins and benzoporphyrins bearing phenyl and thiophene-based -substituents was successfully synthesized and characterized by spectroscopic and electrochemical techniques. Systematic comparison among the compounds in this series, together with the corresponding A analogs previously studied by our group, led to the understanding of the effects of π-conjugated system extension of a porphyrin core through β-fused rings, replacement of the phenyl with the thiophene-based -groups, and introduction of additional thiophene rings on thienyl substituents on photophysical and electrochemical properties. Oxidative electropolymerization through bithiophenyl units of both A and -AB analogs was achieved, resulting in porphyrin- and benzoporphyrin-oligothiophene conjugated polymers, which were characterized by cyclic voltammetry and absorption spectrophotometry.
View Article and Find Full Text PDFMolecules
September 2021
LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
In this study, we report the preparation of new mono-charged benzoporphyrin complexes by reaction of the appropriate neutral benzoporphyrin with (2,2'-bipyridine)dichloroplatinum(II) and of the analogs' derivatives synthesized through alkylation of the neutral scaffold with iodomethane. All derivatives were incorporated into polyvinylpyrrolidone (PVP) micelles. The ability of the resultant formulations to generate reactive oxygen species was evaluated, mainly the singlet oxygen formation.
View Article and Find Full Text PDFJ Hematol Oncol
June 2020
Department of Hematology, Shandong Provincial Hospital Affiliated to Shandong University, No.324, Jingwu Road, Jinan, 250021, Shandong, China.
Background: Hippo-Yes-associated protein (YAP) signaling is a key regulator of organ size and tumorigenesis, yet the underlying molecular mechanism is still poorly understood. At present, the significance of the Hippo-YAP pathway in diffuse large B-cell lymphoma (DLBCL) is ill-defined.
Methods: The expression of YAP in DLBCL was determined in public database and clinical specimens.
Cancer Res
March 2016
Wellman Center for Photomedicine, Massachusetts General Hospital (MGH) and Harvard Medical School, Boston, Massachusetts. Department of Dermatology, MGH, Boston, Massachusetts. Division of Health Sciences and Technology, Harvard University and Massachusetts Institute of Technology, Cambridge, Massachusetts.
The ability of tumor cells to adapt to therapeutic regimens by activating alternative survival and growth pathways remains a major challenge in cancer therapy. Therefore, the most effective treatments will involve interactive strategies that target multiple nonoverlapping pathways while eliciting synergistic outcomes and minimizing systemic toxicities. Nanoliposomal irinotecan is approved by the FDA for gemcitabine-refractory metastatic pancreatic cancer.
View Article and Find Full Text PDFMol Pharm
September 2015
Institute of Biomedical Optics , University of Lübeck, Peter-Monnik-Weg 4, 23562 Lübeck, Germany.
The selective inhibition of intracellular and nuclear molecules such as Ki-67 holds great promise for the treatment of cancer and other diseases. However, the choice of the target protein and the intracellular delivery of the functional agent remain crucial challenges. Main hurdles are (a) an effective delivery into cells, (b) endosomal escape of the delivered agents, and (c) an effective, externally triggered destruction of cells.
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