-
Oncology Reports Jan 2016Alterations in cellular metabolism are among the most consistent hallmarks of cancer. Herein, after a comprehensive metabolic phenotype characterization of MCF7 and ZR75...
Alterations in cellular metabolism are among the most consistent hallmarks of cancer. Herein, after a comprehensive metabolic phenotype characterization of MCF7 and ZR75 breast cancer cells, we investigated the activity of bergapten (Bg), a plant-derived compound, against breast cancer. The study of different biochemical pathways involved in cell metabolism revealed that the two cell lines have different bioenergetic phenotypes: MCF7 cells express a glycolytic phenotype only partially oxidative, while ZR75 cells mainly have an oxidative phenotype. In both cell lines, Bg blocked glycolysis and significantly decreased glucose-6-phosphate dehydrogenase (G6PDH) activity promoting glucose accumulation; modulated bioenergetic requirements altering the expression of oxidative phosphorylation (OXPHOS) complexes and ATP production; and induced a lipid-lowering effect since an increased lipase activity concomitantly to a reduction in triglyceride levels was observed. Quantitative data of different metabolites and enzymatic activities were presented. Treatment with Bg resulted in an alteration in different metabolic pathways inducing death in the cells. We report a novel action of the natural product Bg on breast cancer, since it induced metabolic reprogramming by disrupting the interconnected network of different metabolic mechanisms. Bg can be used in combination with other forms of targeted chemotherapy to improve cancer treatment outcomes.
Topics: 5-Methoxypsoralen; Breast Neoplasms; Cell Line, Tumor; Energy Metabolism; Female; Gene Expression Regulation, Neoplastic; Glucosephosphate Dehydrogenase; Glycolysis; Humans; Lipase; MCF-7 Cells; Methoxsalen
PubMed: 26459431
DOI: 10.3892/or.2015.4327 -
Annales de Dermatologie Et de... 1976
Clinical Trial
Topics: Clinical Trials as Topic; Humans; Long-Term Care; Methoxsalen; Psoriasis; Ultraviolet Therapy
PubMed: 827968
DOI: No ID Found -
Biomedical Mass Spectrometry Nov 1980Methoxsalen, administered orally shows a strong, albeit saturable first-pass effect, as demonstrated by classical dose linearity testing and by a new method, using...
Methoxsalen, administered orally shows a strong, albeit saturable first-pass effect, as demonstrated by classical dose linearity testing and by a new method, using stable isotopes and gas chromatographic mass spectrometric analysis. The therapeutic consequences of the first-pass effect are discussed.
Topics: Adult; Biological Availability; Deuterium; Gas Chromatography-Mass Spectrometry; Humans; Male; Methoxsalen; Time Factors
PubMed: 7225539
DOI: 10.1002/bms.1200071123 -
Lancet (London, England) Jun 1979
Topics: Humans; Methoxsalen; Photochemotherapy; Psoriasis; Skin Neoplasms
PubMed: 87765
DOI: 10.1016/s0140-6736(79)92263-3 -
Photochemical & Photobiological... Oct 2021PUVA is a treatment that combines oral methoxypsoralen (8-MOP) with ultraviolet radiation A (UVA). It is used for severe psoriasis and the early stages of T-cell...
PUVA is a treatment that combines oral methoxypsoralen (8-MOP) with ultraviolet radiation A (UVA). It is used for severe psoriasis and the early stages of T-cell lymphoma. X-rays are an effective treatment for skin cancers. Both treatments are in higher doses used to treat skin malignancies and simultaneously increase the risk of keratinocyte cancer. The main objective of this study was to test whether a few PUVA or X-ray treatments could delay the development of ultraviolet radiation (UVR)-induced skin tumors in a well-established hairless mouse model. Three groups of immunocompetent mice (total, N = 75) were included in the study. All groups were UVR-exposed during the study period. In addition, one group was treated with PUVA and another group was treated with X-rays at days 45, 52, 90 and 97. A control group was treated with UVR only. We recorded when the first, second and third skin tumors were induced in each mouse. Skin tumors developed significantly earlier in both the PUVA and X-ray groups (median, 188 days) than in the control mice (median, 215 days; p < 0.001). Therefore, a few X-ray and PUVA treatments both significantly accelerated the development of skin tumors in hairless mice, compared to UVR controls. Neither treatment showed a delay of UVR-induced skin tumors and caution should be exercised before applying these treatments to sun-damaged skin.
Topics: Animals; Immunocompromised Host; Kaplan-Meier Estimate; Methoxsalen; Mice; Mice, Hairless; Neoplasms, Radiation-Induced; Skin; Skin Neoplasms; Skin Pigmentation; Ultraviolet Rays; X-Rays
PubMed: 34559384
DOI: 10.1007/s43630-021-00105-y -
Prescrire International Feb 2009
Topics: Drug Approval; Extracorporeal Circulation; France; Humans; Lymphoma, T-Cell; Methoxsalen; PUVA Therapy; Photopheresis; Photosensitizing Agents
PubMed: 19388212
DOI: No ID Found -
Southern Medical Journal Feb 1980
Topics: Humans; Methoxsalen; Photochemotherapy; Psoriasis
PubMed: 7355305
DOI: 10.1097/00007611-198002000-00002 -
Chemical Biology & Drug Design May 2024Tyrosinase is a copper-containing enzyme involved in the biosynthesis of melanin pigment. While the excess production of melanin causes hyperpigmentation of human skin,...
Tyrosinase is a copper-containing enzyme involved in the biosynthesis of melanin pigment. While the excess production of melanin causes hyperpigmentation of human skin, hypopigmentation results in medical conditions like vitiligo. Tyrosinase inhibitors could be used as efficient skin whitening agents and tyrosinase agonists could be used for enhanced melanin synthesis and skin protection from UV exposure. Among a wide range of tyrosinase-regulating compounds, natural and synthetic derivatives of furochromenones, such as 8-methoxypsoralen (8-MOP), are known to both activate and inhibit tyrosinase. We recently reported a synthetic approach to generate a variety of dihydrofuro[3,2-c]chromenones and furo[3,2-c]chromenones in a metal-free condition. In the present study, we investigated these compounds for their potential as antagonists or agonists of tyrosinase. Using fungal tyrosinase-based in vitro biochemical assay, we obtained one compound (3k) which could inhibit tyrosinase activity, and the other compound (4f) that stimulated tyrosinase activity. The kinetic studies revealed that compound 3k caused 'mixed' type tyrosinase inhibition and 4f stimulated the catalytic efficiency. Studying the mechanisms of these compounds may provide a basis for the development of new effective tyrosinase inhibitors or activators.
Topics: Monophenol Monooxygenase; Enzyme Inhibitors; Kinetics; Humans; Methoxsalen; Enzyme Activators
PubMed: 38760181
DOI: 10.1111/cbdd.14539 -
Archives of Dermatology Apr 1979Analysis of standard fluorescent sunlamps (Westinghouse) indicates that in addition to UVB (290 to 320 nm), a considerable amount of UVA (320 to 400 nm) is also present...
Analysis of standard fluorescent sunlamps (Westinghouse) indicates that in addition to UVB (290 to 320 nm), a considerable amount of UVA (320 to 400 nm) is also present in their emissions. Since the benefits of topical psoralen administration and UVA have already been demonstrated, and prior experience by ourselves and others with UVB has indicated that some psoriasis benefited from UVB alone, localized areas and plaques of 20 patients were treated with topical administration of psoralens and fluorescent sunlamp bulbs to determine if such a light source with this emission spectrum would be advantageous. Results indicated a total resolution in 17 of 20 patients after an average of 18 treatments. Adverse blistering phototoxic reactions and excessive hyperpigmentation were not encountered. The UVB erythema response of normal skin served as the guide to light dosage in the same manner as administration of the Goeckerman regimen. Therefore, the use of psoralens was very effective when combined with fluorescent sunlamp irradiation; however, the potential risks of photocarcinogenicity makes this treatment experimental and should be reserved for recalcitrant cases.
Topics: Administration, Topical; Fluorescence; Humans; Male; Methoxsalen; Photochemotherapy; Psoriasis; Sunlight
PubMed: 434863
DOI: No ID Found -
Molecules (Basel, Switzerland) Oct 2018Eight alkaloids (⁻) were isolated from , and their herbicide activities were evaluated through in vitro, semivivo, and in vivo assays. The most relevant results were...
Eight alkaloids (⁻) were isolated from , and their herbicide activities were evaluated through in vitro, semivivo, and in vivo assays. The most relevant results were observed for Compounds and ⁻ at 150 μM, which decreased dry biomass by 20% and 23%, respectively. These are significant results since they presented similar values with the positive control, commercial herbicide 3-(3,4-dichlorophenyl)-1,1-dimethylurea (DCMU). Based on the performed assays, Compound (graveoline) is classified as an electron-transport inhibitor during the light phase of photosynthesis, as well as a plant-growth regulator. On the other hand, Compounds ⁻ inhibited electron and energy transfers, and are also plant-growth inhibitors. These phytotoxic behaviors based on acridone and quinolone alkaloids may serve as a valuable tool in the further development of a new class of herbicides since natural products represent an interesting alternative to replace commercial herbicides, potentially due their low toxicity.
Topics: Alkaloids; Biomass; Diuron; Electron Transport; Herbicides; Methoxsalen; Photosynthesis; Ruta
PubMed: 30347671
DOI: 10.3390/molecules23102693