Biopharmaceutics, pharmacokinetics and pharmacology of psoralens

Stolk, L. M. L.; Siddiqui, A. H.

doi:10.1016/0306-3623(88)90122-x

Cited by 18 publications

(14 citation statements)

References 18 publications

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“…In the liver, about 60% to 70% of psoralen was combined with glucuronic acid and sulfuric acid. The combination was excreted into the small intestine through bile duct and hydrolyzed, and then the prototype was regenerated and reabsorbed into blood (Stolk and Siddiqui, 1988). In this study, we found that after oral administration, the enterohepatic circulation of psoralen was quite obvious, the t max of its concentration-time curve was 2.4 and 4.1 h after dosing, but the enterohepatic circulation of isopsoralen was unobvious.…”

Section: Discussionmentioning

confidence: 61%

Pharmacokinetics, tissue distribution and excretion of coumarin components from Psoralea corylifolia L. in rats

2010

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Coumarin components from Psoralea corylifolia L. are novel drugs in which psoralen and isopsoralen are the active components. The pharmacokinetics, tissue distribution and excretion of the two compounds were studied by liquid chromatography-tandem mass spectrometry after intravenous administration to Wistar rats. The elimination half-lives of psoralen and isopsoralen were 4.88 and 5.35 h. After dosing, the area under the curves of the tissues decreased in the following order: liver > lung > heart > kidney > spleen > brain for psoralen; and kidney > lung > liver > heart > spleen > brain for isopsoralen. After dosing, 51.27% of psoralen and 56.25% of isopsoralen were excreted as prototype, and urine was the major excretion route. In addition, the pharmacokinetics of psoralen and isopsoralen after oral administration to Wistar rats were also studied. The elimination half-lives of psoralen and isopsoralen were 4.13 and 5.56 h, and their relative bioavailabilities were 61.45% and 70.35%. Overall, the results show that coumarin components from P. corylifolia L. have high oral bioavailability, they are rapidly and widely distributed into tissues after intravenous administration, but they are slowly cleared and excreted.

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Section: Discussionmentioning

confidence: 61%

Pharmacokinetics, tissue distribution and excretion of coumarin components from Psoralea corylifolia L. in rats

2010

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“…The MPD is defined as the dose of UVA required to induce a barely visible erythema on the skin and is proportional to the concentration of 8-MOP in the skin. MPD values following bathwater and oral administration of 8-MOP are comparable: 1–3 J/cm 2 UVA [19, 22;]our own clinical observations]. First results indicate that bath PUVA carried out at the current 8-MOP concentrations in bathwater could even have a somewhat stronger effect (i.e.…”

Section: Pharmacokinetics Of Bath Puva Versus Oral Puvamentioning

confidence: 62%

“…Thus, the systemic burden of 8-MOP is much lower following bath PUVA. Typically, plasma and serum concentrations of 8-MOP lie in the range of 10–30 ng/ml [16, 17, 18], whereas following oral administration concentrations of 100–200 ng 8-MOP/ml are observed [18, 19]. …”

Section: Pharmacokinetics Of Bath Puva Versus Oral Puvamentioning

confidence: 99%

“…Since noncovalently bound 8-MOP has a short half-life in the body (approx. 1 h in serum [19]), the risk of forming new carcinogenic monoadducts at this time would be small. However, the benefit of this second irradiation would have to be weighed against the risks of additional exposure to UVA, which is weakly carcinogenic in its own right [26, 27].…”

Section: Therapeutic and Carcinogenic Mechanismsmentioning

confidence: 99%

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Carcinogenic Risk of Bath PUVA in Comparison to Oral PUVA Therapy

Shephard

Panizzon

1999

Dermatology

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The potential carcinogenic risk of bath PUVA therapy was compared to that of systemic (oral) PUVA. An analysis of the epidemiological data on cancer risk following bath PUVA with trimethylpsoralen does not support the conclusion that bath PUVA per se is less carcinogenic than systemic PUVA with 8-methoxypsoralen (8-MOP). Pharmacokinetic studies indicate that both the concentration of 8-MOP in the target organ for PUVA carcinogenicity (skin) at the relevant time point (time point of UVA irradiation) and the extents of biological effects in the skin are comparable following bathwater or systemic 8-MOP administration. Furthermore, the therapeutic effects of PUVA arise from the same photochemical reaction mechanisms as do the carcinogenic effects. Theoretically, the ratio of (desired) cytotoxic versus (undesired) mutagenic effects could increase with increasing efficiency of the PUVA therapy itself. On the basis of the available evidence, it is concluded that all forms of PUVA therapy, independently of the route of 8-MOP administration, contribute to a small but dose-dependent increase in nonmelanoma skin cancer risk.

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“…Psoralens, extremely toxic to a wide variety of prokaryotic and eukaryotic organisms, are mainly extracted from the ripe fruit of Psoralea corylifolia (Leguminosae), an erect annual herb widely used in Ayurvedic medicine and traditional Chinese medicine. 8-methoxypsoralen (8-MOP) and 5-methoxypsoralen (5-MOP), or bergapten, are the psoralen compounds that occur in nature but several analogues have also been described [15][16][17][18][19][20] . These molecules cause cell damage by covalent binding to DNA after ultraviolet radiation A (UVA) irradiation.…”

Section: Topic Highlightmentioning

confidence: 99%

Effects of psoralens as anti-tumoral agents in breast cancer cells

Panno

Giordano

2014

WJCO

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Core tip: This review examines the biological properties of coumarins by considering their beneficial effects in the prevention of some diseases and as anti-cancer agents. The attention is mainly focused on the effects of psoralens on human breast cancer as they are able to influence many aspects of cell behavior. More recently, it has been reported that these drugs in breast cancer cells are capable of antagonizing some metabolizing enzymes, to affect estrogen receptor stability and to counteract cell invasiveness as well as cancer drug resistance.Panno ML, Giordano F. Effects of psoralens as anti-tumoral agents in breast cancer cells.

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Biopharmaceutics, pharmacokinetics and pharmacology of psoralens

Cited by 18 publications

References 18 publications

Pharmacokinetics, tissue distribution and excretion of coumarin components from Psoralea corylifolia L. in rats

Pharmacokinetics, tissue distribution and excretion of coumarin components from Psoralea corylifolia L. in rats

Carcinogenic Risk of Bath PUVA in Comparison to Oral PUVA Therapy

Effects of psoralens as anti-tumoral agents in breast cancer cells

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