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Praxis Jan 2001
Topics: 5-Methoxypsoralen; Breast Neoplasms; Dermatitis, Contact; Diagnosis, Differential; Female; Humans; Methoxsalen; Photosensitivity Disorders; Plants, Toxic; Tamoxifen
PubMed: 11219211
DOI: No ID Found -
Journal of Photochemistry and... Jun 1990There is good evidence that 8-methoxypsoralen is photocarcinogenic in psoriatic patients undergoing long-term photochemotherapy (PUVA) in the U.S.A. However, this... (Review)
Review
There is good evidence that 8-methoxypsoralen is photocarcinogenic in psoriatic patients undergoing long-term photochemotherapy (PUVA) in the U.S.A. However, this conclusion has not been supported by two major European studies which have indicated that PUVA is a tumour promoter of damage initiated by other agents. Variation in PUVA treatment protocols in the U.S.A. and Europe may partly account for the different conclusions. There is much interest in the therapeutic potential of monofunctional psoralens. It is hoped that these may reduce long-term risk. Monofunctional and cross-linking psoralens have been shown to be photocarcinogenic in mouse skin. The relative risk of different compounds may be assessed in the mouse, but it is important to base comparisons on dose protocols that have been shown to be therapeutically effective.
Topics: Animals; Carcinogens; Furocoumarins; Humans; Methoxsalen; Photochemotherapy; Skin Neoplasms
PubMed: 2121937
DOI: 10.1016/1011-1344(90)85093-c -
Archives of Dermatological Research 1981The kinetics of migration of radiolabeled 8-methoxypsoralen into human cataract lenses were investigated in 12 patients undergoing operation. Lenses were examined from...
The kinetics of migration of radiolabeled 8-methoxypsoralen into human cataract lenses were investigated in 12 patients undergoing operation. Lenses were examined from 2.5 - 72 h after intake of 3H-labeled 8-methoxypsoralen by mouth. Demonstrable amounts of activity was only found in two of three lenses studied 24 h after intake. The aqueous humor contained less 8-methoxypsoralen than serum. The results of the study may add support to the opinion that a less rigorous sunglass regimen than that recommended by certain PUVA centers may be justified.
Topics: Aged; Aqueous Humor; Cataract; Cataract Extraction; Humans; Methoxsalen; Middle Aged; Tritium
PubMed: 7283466
DOI: 10.1007/BF00403782 -
Food and Chemical Toxicology : An... May 20115-methoxypsoralen (bergapten) has been used in the treatment of psoriasis and vitiligo, and as a sun tanning accelerator. While low plasma concentrations have previously...
OBJECTIVE AND DESIGN
5-methoxypsoralen (bergapten) has been used in the treatment of psoriasis and vitiligo, and as a sun tanning accelerator. While low plasma concentrations have previously been detected, there is no data on its dermatopharmacokinetics.
MATERIALS AND METHODS
Three rhesus monkeys were used as a model for human skin. [14C]-5-methoxypsoralen, as a parenteral excretion control, was injected in propylene glycol with an activity of 1.12 uCi/ml at a concentration of 80 mcg/ml and urine was collected at 4, 8, 12, 24h, and then daily for a total of 6 days. [14C]-5-methoxypsoralen was then applied topically in acetone with a dose of 1.19 mc (72 mcg) and urine was collected at 4 and 24h and then daily for a total of 7 days. The amount excreted was corrected for the previously determined parenteral excretion kinetics.
RESULTS
Intramuscular [14C]-5-methoxypsoralen had an average of 71.87±7.77% of excretion and percutaneously applied [14C]-5-methoxypsoralen had an average of 58.4±11.8% of excretion.
CONCLUSION
A high percentage of the administered 5-methoxypsoralen was absorbed. This provides a foundation of methodology to evaluate the efficacy of other delivery vehicles for 5-methoxypsoralen and serves as part of its dermatotoxic profile.
Topics: 5-Methoxypsoralen; Administration, Cutaneous; Animals; Carbon Isotopes; Injections, Intramuscular; Macaca mulatta; Methoxsalen; Models, Animal; Oxidation-Reduction; Psoriasis; Skin; Skin Absorption; Vitiligo
PubMed: 21281688
DOI: 10.1016/j.fct.2011.01.018 -
Transactions of the American... 1979
Review
Topics: Adolescent; Adult; Aged; Animals; Aqueous Humor; Biological Assay; Cataract; Female; Humans; Lens, Crystalline; Male; Methoxsalen; Middle Aged; Photochemotherapy; Psoriasis
PubMed: 397661
DOI: No ID Found -
Clinical Immunology (Orlando, Fla.) Feb 2012
Topics: Cytokines; Female; Humans; Male; Methoxsalen; Photopheresis; Scleroderma, Systemic
PubMed: 22134055
DOI: 10.1016/j.clim.2011.11.003 -
Bioorganic & Medicinal Chemistry Jan 2020A novel series of graveolinine derivatives were synthesized and evaluated as potential anti-Alzheimer agents. Compound 5f exhibited the best inhibitory activity for...
A novel series of graveolinine derivatives were synthesized and evaluated as potential anti-Alzheimer agents. Compound 5f exhibited the best inhibitory activity for acetylcholinesterase (AChE) and had surprisingly potent inhibitory activity for butyrylcholinesterase (BuChE), with IC values of 0.72 μM and 0.16 μM, respectively. The results from Lineweaver-Burk plot and molecular modeling study indicated non-competitive inhibition of AChE by compound 5f. In addition, these derivatives showed potent self-induced β-amyloid (Aβ) aggregation inhibition. Moreover, 5f didn't show obvious toxicity against PC12 and HepG2 cells at 50 μM. Finally, in vivo studies confirmed that 5f significantly ameliorates the cognitive performances of scopolamine-treated ICR mice. Therefore, these graveolinine derivatives should be thoroughly and systematically studied for the treatment of Alzheimer's disease.
Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Behavior, Animal; Butyrylcholinesterase; Cell Survival; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Electrophorus; Hep G2 Cells; Horses; Humans; Male; Methoxsalen; Mice; Molecular Structure; PC12 Cells; Peptide Fragments; Rats; Structure-Activity Relationship
PubMed: 31744779
DOI: 10.1016/j.bmc.2019.115190 -
Archives of Dermatology Sep 1979Fluorescent sunlamp bulbs have been an effective light source for treatment of psoriasis when they are used in combination with crude coal tar. In addition to their... (Comparative Study)
Comparative Study
Fluorescent sunlamp bulbs have been an effective light source for treatment of psoriasis when they are used in combination with crude coal tar. In addition to their ultraviolet B (UVB) emission, the spectral output of these bulbs contains a substantial amount of ultraviolet A (UVA). Prior testing with this light source and topically applied methoxsalen achieved excellent results in psoriasis. This study compared topically applied methoxsalen to crude coal tar in 16 patients who had plaque-type psoriasis, using the same fluorescent sunlamp source of irradiation. Fourteen of 16 patients had complete clearing of plaques when they were treated with methoxsalen, compared with six patients who had complete clearing with the tar treatment. These results indicate that the use of methoxsalen and ultraviolet light may be more effective than tar, when used as they were in this study. The advantages of a clean, white, nonstaining topical agent also makes outpatient therapy more cosmetically acceptable.
Topics: Coal Tar; Humans; Male; Methoxsalen; Photochemotherapy; Psoriasis; Ultraviolet Therapy
PubMed: 485182
DOI: No ID Found -
Clinical Pharmacology and Therapeutics Apr 1979The correlation between serum concentration of methoxsalen (8-methoxypsoralen; 8-MOP) and phototoxic effect using long-wave ultraviolet light has been studied in 5...
The correlation between serum concentration of methoxsalen (8-methoxypsoralen; 8-MOP) and phototoxic effect using long-wave ultraviolet light has been studied in 5 psoriatic patients. The maximum serum concentration occurred between 0.5 and 2 hr after oral administration of 0.6 mg/kg of methoxsalen. The lowest value for the minimum phototoxic dose (MPD), i.e., highest photosensitivity, was obtained between 1 and 2 hr. There was a significant negative correlation between the logarithm of the serum concentration and minimum phototoxic dose (MPD) (r = 0.780). Hence, the degree of photosensitivity appears to be related to the serum level of methoxsalen.
Topics: Adult; Humans; Methoxsalen; Photosensitivity Disorders; Psoriasis; Time Factors
PubMed: 428192
DOI: No ID Found -
Anales de Medicina Interna (Madrid,... Aug 2003
Topics: Humans; Methoxsalen; Photopheresis
PubMed: 14516257
DOI: No ID Found