Bergapten

14,000,000 Leading Edge Experts on the ideXlab platform

Scan Science and Technology

Contact Leading Edge Experts & Companies

Scan Science and Technology

Contact Leading Edge Experts & Companies

The Experts below are selected from a list of 297 Experts worldwide ranked by ideXlab platform

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.

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.

Zi-long Zhang - One of the best experts on this subject based on the ideXlab platform.

  • Bergapten exerts inhibitory effects on diabetes related osteoporosis via the regulation of the pi3k akt jnk mapk and nf κb signaling pathways in osteoprotegerin knockout mice
    International Journal of Molecular Medicine, 2016
    Co-Authors: Zhe Zhu, Si-lin Han, Zi-long Zhang
    Abstract:

    Diabetes, as a serious metobolic disorder, poses global threat to human health. It is estimated that over 50 million individuals are already affected by diabetes. Currently, diabetes-related osteoporosis has been a research hotspot due to its high incidence rate in older individuals. Osteoprotegerin, as an important protein for the prevention of osteoporosis, has been proven to be key to the suppression of osteoporosis. Hence, the loss of function of osteoprotegerin may promote the development of osteoporosis. Bergapten, as a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils, and grapefruit juice, has been proven to have the ability to attenuate a number of metabolic disorders. In view of these findings, in this study, we used a high-fat diet to construct a mouse model of diabetes-related osteoporosis and a mouse model of diabetes-related osteoporosis using osteoprotegerin knockout mice. Enzyme-linked immunosorbent assay (ELISA), qPCR, western blot analysis, immunohistochemical assay, H&E staining, Oil Red O staining, Masson's staining and other biochemical analyses were used to evaluate the related signaling pathways involved in the development of diabetes-related osteoporosis. We also examined the role of osteoprotegerin in the activation of these pathways and in the development of osteoporosis, as well as the protective effects of Bergapten against diabetes-related osteoporosis and on the activation of related signaling pathways. Our results revealed that in diabetes-related osteoporosis, the phosphoinositide 3-kinase (PI3K)/AKT, c-Jun N-terminal kinase (JNK)/mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB) signaling pathways were activated and the expression levels of related indicators were increased. At the same time, osteoprotegerin knockout further promoted the activation of these pathways. By contrast, Bergapten exerted effects similar to those of osteoprotegerin. Bergapten exhibited the ability to significantly inhibit RANKL-RANK signaling transduction, and to suppress the activation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways, thus protecting trabecular structure and decreasing osteoclastogenic differentiation.

  • Bergapten exerts inhibitory effects on diabetes-related osteoporosis via the regulation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways in osteoprotegerin knockout mice
    International Journal of Molecular Medicine, 2016
    Co-Authors: Zhe Zhu, Si-lin Han, Zi-long Zhang
    Abstract:

    Diabetes, as a serious metobolic disorder, poses global threat to human health. It is estimated that over 50 million individuals are already affected by diabetes. Currently, diabetes-related osteoporosis has been a research hotspot due to its high incidence rate in older individuals. Osteoprotegerin, as an important protein for the prevention of osteoporosis, has been proven to be key to the suppression of osteoporosis. Hence, the loss of function of osteoprotegerin may promote the development of osteoporosis. Bergapten, as a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils, and grapefruit juice, has been proven to have the ability to attenuate a number of metabolic disorders. In view of these findings, in this study, we used a high-fat diet to construct a mouse model of diabetes-related osteoporosis and a mouse model of diabetes-related osteoporosis using osteoprotegerin knockout mice. Enzyme-linked immunosorbent assay (ELISA), qPCR, western blot analysis, immunohistochemical assay, H&E staining, Oil Red O staining, Masson's staining and other biochemical analyses were used to evaluate the related signaling pathways involved in the development of diabetes-related osteoporosis. We also examined the role of osteoprotegerin in the activation of these pathways and in the development of osteoporosis, as well as the protective effects of Bergapten against diabetes-related osteoporosis and on the activation of related signaling pathways. Our results revealed that in diabetes-related osteoporosis, the phosphoinositide 3-kinase (PI3K)/AKT, c-Jun N-terminal kinase (JNK)/mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB) signaling pathways were activated and the expression levels of related indicators were increased. At the same time, osteoprotegerin knockout further promoted the activation of these pathways. By contrast, Bergapten exerted effects similar to those of osteoprotegerin. Bergapten exhibited the ability to significantly inhibit RANKL-RANK signaling transduction, and to suppress the activation of the PI3K/AKT, JNK/MAPK and NF-κB signaling pathways, thus protecting trabecular structure and decreasing osteoclastogenic differentiation.

M. M. Diawara - 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.