Simple equilibrium dialysis-high-performance liquid chromatographic method for the in vitro assessment of 5-methoxypsoralen bound to human albumin

Makki, S.; Muret, Patrice; Renaud, Alexis; Agache, P; Magnin, P

doi:10.1016/s0021-9673(01)83953-4

Cited by 6 publications

(2 citation statements)

References 6 publications

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“…Dialysis 5-MOP binding to human isolated proteins as well as to serum was studied by equilibrium dialysis using a Dianorm apparatus (München, FRG) with Teflon ma cro-1 cells (2 X 1.15ml) separated by Diachema mem branes (cut-off 10,000). The dialysis experiments were described in a previous work [5]. Briefly, they were car ried out at 37 °C, pH 7.4 for 2 h with a constant stir ring of 12 rpm.…”

Section: -Mop Was Supplied By Bergadcrm Laboratories (Rungis Francementioning

confidence: 99%

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Binding of 5-Methoxypsoralen to Blood Fractions

Muret

Makki

Urien

et al. 1993

Skin Pharmacol Physiol

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The binding of 5-methoxypsoralen (5-MOP) to human serum and blood fractions was studied by equilibrium dialysis associated to high-performance liquid chromatography. 5-MOP serum binding was 95% and kept constant in the range of therapeutic concentrations. Albumin was the main binding protein with one class of binding sites (n = 2.05) and with a moderate affinity constant (K_a = 10,270 M^-1). Free fatty acids (FFA) enhanced 5-MOP binding to albumin. Binding to other proteins, α₁-acid glycoprotein, gamma-globulins and lipoproteins (LDL, HDL, VLDL) also occurred, but was negligible. 5-MOP bound to red blood cells (RBCs) with a binding index (ratio of intra- to extra-globular 5-MOP concentrations) of 3.84 and 1.48 in buffer and plasma, respectively. 5-MOP distribution in blood was simulated. The free fraction of 5-MOP in blood could be increased in hypoalbuminemia, unchanged in acute inflammation, and decreased by FFA.

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Section: -Mop Was Supplied By Bergadcrm Laboratories (Rungis Francementioning

confidence: 99%

“…For the higher concentrations, an adequate dilution was per formed before assessment. Although 8-MOP has a lower absorption coefficient than 5-MOP, it was used as an internal standard, allowing us to obtain short time chromatograms with an acceptable peak separa tion [5],…”

Section: -Mop Was Supplied By Bergadcrm Laboratories (Rungis Francementioning

confidence: 99%

Binding of 5-Methoxypsoralen to Blood Fractions

Muret

Makki

Urien

et al. 1993

Skin Pharmacol Physiol

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Serum free 5-methoxypsoralen fraction in health and psoriasis: relationship with human serum albumin concentration

et al. 1993

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Human serum albumin is known to be the main carrier of 5-methoxypsoralen (5-MOP) in serum. As hypoalbuminaemia may occur in psoriasis with inflammatory syndrome, variability of the free 5-MOP fraction in serum can be expected. The free 5-MOP fraction was determined by equilibrium dialysis in serum samples obtained from 18 psoriatic patients and 18 control subjects. The median free 5-MOP fraction was not significantly different in the psoriatic group (fu = 4.75%) than in the control group (fu = 5%). However, there was a significantly larger variability of the free fraction in the psoriatic group (2.7 to 8.6%) than in the healthy group (3.2 to 6.8%) (p = 0.002). The binding index of 5-MOP (ratio of bound to free concentrations) was correlated with human serum albumin level (r = 0.784). This work confirms that the 5-MOP fraction in human serum is principally serum albumin dependent, as has been described with in vitro models. Free drug monitoring of 5-MOP is discussed.

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Treatment of psoriasis with a new micronized 5-methoxypsoralen tablet and UVA radiation

Aubin¹,

Makki

Humbert³

et al. 1994

Arch Dermatol Res

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Since 1974, phototherapy with psoralen and ultraviolet A (UVA) has been used successfully for the treatment of psoriasis. However, undesirable side effects, including phototoxicity, nausea, stomach pain and headaches, have led investigators to develop new psoralen compounds. 5-Methoxypsoralen (5-MOP) has thus been introduced as an alternative to 8-MOP because of its less pronounced side effects. Since the absorption kinetics and bioactivity of 5-MOP are known to be variable, a new micronized tablet form (5-MOPm) has been developed. In an open randomized study, oral treatments with 5-MOP or 5-MOPm plus UVA radiation were compared in 22 psoriatic patients. Skin type and initial psoriasis area severity index did not differ significantly between treatment groups. Serum concentrations were significantly higher (320 vs 85.82 ng/ml) and occurred earlier (51.8 vs 229.09 min) with 5-MOPm. In addition, a reduction in PASI of more than 90% was achieved sooner (10.63 vs 17.27 treatments) and with a lower cumulative UVA dose (145.89 vs 232.11 J/cm2), in the group treated with 5-MOPm. No side effects were observed with 5-MOPm. Our data indicate that 5-MOPm has a higher bioavailability, clinical efficacy and tolerability than the commonly used 5-MOP.

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Simple equilibrium dialysis-high-performance liquid chromatographic method for the in vitro assessment of 5-methoxypsoralen bound to human albumin

Cited by 6 publications

References 6 publications

Binding of 5-Methoxypsoralen to Blood Fractions

Binding of 5-Methoxypsoralen to Blood Fractions

Serum free 5-methoxypsoralen fraction in health and psoriasis: relationship with human serum albumin concentration

Treatment of psoriasis with a new micronized 5-methoxypsoralen tablet and UVA radiation

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