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Bergapten

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P. Ph. D. Forlot – One of the best experts on this subject based on the ideXlab platform.

  • Toxicological & pharmacological properties of Bergapten
    , 2000
    Co-Authors: P. Ph. D. Forlot

    Abstract:

    Since almost two decades, 8-MOP (8-methoxypsoralen) and 5-MOP (5-Methoxypsoralen, Bergapten) are largely used for the treatment of psoriasis and vitiligo and are recognized as routine therapy for several psoriasis (Photochemiotherapy). Toxicity From experimental toxicological studies on animals (acute, subacute, subchronic & teratogenic potential) as well as from the available pharmaco-toxicological data there is no evidence of important systemic manifestations after clinicai utlization except some very idiosynchratic hepatic reactions. The only observed reactions were limited to the gastro-intestinal tract (nausea, vomiting) and the skin in case of excessive irradiations (Photototoxicity). Intensity and frequency of reactions are much lower with 5-MOP. Psoralens are carcinogenic in hairless mice using prolonged irradiation with UVA sources and at high intraperitoneal doses. In humans, there is a dose-related increased incidence of squamous cell carcinoma (SCC) occuring in U.S. patients with risk factors treated with 8-MOP However, there is a discrepancy in this incidence between the European and the American experience, and the incidence is even lower with 5-MOP. Pharmacology The absorption of 5-MOP (Bergapten) is variable and depends on a number of factors, including the dosage form, physical form of the drug and intake of food with drug administration. Biological properties: UV-related:5-MOP is specially activated by longwave ultraviolet radiations (UVA: 340-400 nm) depending on cellular and macromolecular conditions. The biologic effects observed are: -Inhibition of cellular proliferation due to the intercalation of 5-MOP in cellular DNA(Photochemotherapy of psoriasis, T-Cell cutaneous lymphoma). -Immunomodulation of Langerhans cells and other immunocompetent cutaneous cells ( Lupus erythematosus, atopic dermatitis…). -Stimulation of skin pigmentation ( Photochemotherapy of vitiligo). -Phototoxic elimination of microorganisms and viruses (extracorporeal photochemotherapy of AIDS, photodecontamination of transfusion blood). UV-non related: two recently discovered pharmacological properties of 5-MOP will be discussed: -Inhibition of melatonin catabolism in human ( depression, jet-lag, migraine) -selective blocking of K-channels in myelin ( possible use in symptomatic treatment of demyelinating diseases such multiple sclerosis).

  • toxicological pharmacological properties of Bergapten
    Essenze e derivati agrumari, 2000
    Co-Authors: P. Ph. D. Forlot

    Abstract:

    Since almost two decades, 8-MOP (8-methoxypsoralen) and 5-MOP (5-Methoxypsoralen, Bergapten) are largely used for the treatment of psoriasis and vitiligo and are recognized as routine therapy for several psoriasis (Photochemiotherapy). Toxicity From experimental toxicological studies on animals (acute, subacute, subchronic & teratogenic potential) as well as from the available pharmaco-toxicological data there is no evidence of important systemic manifestations after clinicai utlization except some very idiosynchratic hepatic reactions. The only observed reactions were limited to the gastro-intestinal tract (nausea, vomiting) and the skin in case of excessive irradiations (Photototoxicity). Intensity and frequency of reactions are much lower with 5-MOP. Psoralens are carcinogenic in hairless mice using prolonged irradiation with UVA sources and at high intraperitoneal doses. In humans, there is a dose-related increased incidence of squamous cell carcinoma (SCC) occuring in U.S. patients with risk factors treated with 8-MOP However, there is a discrepancy in this incidence between the European and the American experience, and the incidence is even lower with 5-MOP. Pharmacology The absorption of 5-MOP (Bergapten) is variable and depends on a number of factors, including the dosage form, physical form of the drug and intake of food with drug administration. Biological properties: UV-related:5-MOP is specially activated by longwave ultraviolet radiations (UVA: 340-400 nm) depending on cellular and macromolecular conditions. The biologic effects observed are: -Inhibition of cellular proliferation due to the intercalation of 5-MOP in cellular DNA(Photochemotherapy of psoriasis, T-Cell cutaneous lymphoma). -Immunomodulation of Langerhans cells and other immunocompetent cutaneous cells ( Lupus erythematosus, atopic dermatitis…). -Stimulation of skin pigmentation ( Photochemotherapy of vitiligo). -Phototoxic elimination of microorganisms and viruses (extracorporeal photochemotherapy of AIDS, photodecontamination of transfusion blood). UV-non related: two recently discovered pharmacological properties of 5-MOP will be discussed: -Inhibition of melatonin catabolism in human ( depression, jet-lag, migraine) -selective blocking of K-channels in myelin ( possible use in symptomatic treatment of demyelinating diseases such multiple sclerosis).

P. Agache – One of the best experts on this subject based on the ideXlab platform.

  • Citropten and Bergapten suction blister fluid concentrations after solar product application in man.
    Skin Pharmacology and Physiology, 2009
    Co-Authors: P. Treffel, S. Makki, Philippe Humbert, B. Faivre, D. Blanc, P. Agache

    Abstract:

    Citropten (5,7-dimethoxycoumarin) and Bergapten (5-methoxypsoralen) are present in bergamot oil which is used as a cosmetic tanning product. The aim of this study was to quantify, using HPLC, the amou

  • High-performance liquid chromatographic determination of citropten and Bergapten in suction blister fluid after solar product application in humans
    Journal of Chromatography B: Biomedical Sciences and Applications, 1991
    Co-Authors: S. Makki, P. Treffel, Philippe Humbert, P. Agache

    Abstract:

    Citropten (5,7-dimethoxycoumarin) and Bergapten (5-methoxypsoralen) are present in bergamot oil which is used as a tanning cosmetic product. The aim of this study was to quantify, using high-performance liquid chromatography, the amount of citropten and Bergapten in the skin after suntan products application (an emulsion and an oil formulation). A suction blister technique performed of the anterior aspect of the forearm permitted the collection of these two accumulated molecules. Fluorometric and ultraviolet detections were used for citropten and Bergapten determinations, respectively.

L. A. Martinez – One of the best experts on this subject based on the ideXlab platform.

  • Toxicity of linear furanocoumarins toSpodoptera exigua: Evidence for antagonistic interactions
    Journal of Chemical Ecology, 1993
    Co-Authors: M. M. Diawara, J. T. Trumble, K. K. White, W. G. Carson, L. A. Martinez

    Abstract:

    The linear furanocoumarins psoralen, Bergapten, and xanthotoxin were tested for toxicity to the beet armyworm Spodoptera exigua (Hübner) under short ultraviolet (UVB) radiation. Increased dietary concentrations of each furanocoumarin significantly decreased insect larval weight, extended generation time, and induced higher mortality. Xanthotoxin was the most toxic, followed by psoralen and Bergapten. Combining psoralen with Bergapten, xanthotoxin, or both resulted in significantly antagonistic effects on insect mortality. The combination of Bergapten and xanthotoxin, however, produced additive effects. The implications of these observations for S. exigua resistance in the wild plant accession of Apium prostratum and the enigma the findings represent for plant-insect relationships are discussed.