Genotoxic activity of 4,4?,5?-trimethylazapsoralen on plasmid DNA

Lagatolla, Cristina; Dolzani, Lucilla; Granzotto, Marilena; Monti‐Bragadin, C.

doi:10.1002/(sici)1520-6866(1998)18:5<239::aid-tcm4>3.0.co;2-v

Cited by 6 publications

(4 citation statements)

References 14 publications

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“…Administration of photochemically treated 100% plasma did not cause maternal or fetal developmental toxicity. These results were consistent with, and supplemented the teratology study conducted with, photochemically treated 35% plasma [29,30]. Additionally, for the photochemically treated 35% plasma studies, a complete series of reproductive toxicology studies was conducted, which included male and female fertility studies in rats, an additional teratology study in the rabbit, and a peri-postnatal reproductive development study in the rat, none of which resulted in any reproductive toxicity as a result of administration of photochemically treated 35% plasma administered at 25 ml/kg.…”

Section: Reproductive Toxicitysupporting

confidence: 88%

“…Addition of chemicals to blood products for the inactivation of contaminants is a potential cause for concern because of the possible risks associated with the introduction of chemical agents into therapeutic preparations that will be administered to patients. With respect to psoralens [23], the combination of some compounds in this class and UV light has been associated with genotoxicity, carcinogenicity, phototoxicity and other adverse effects [24][25][26][27][28][29][30].…”

Section: Intercept Blood System For Plasmamentioning

confidence: 99%

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Preclinical safety profile of plasma prepared using the INTERCEPT Blood System

et al. 2003

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Section: Reproductive Toxicitysupporting

confidence: 88%

Section: Intercept Blood System For Plasmamentioning

confidence: 99%

Preclinical safety profile of plasma prepared using the INTERCEPT Blood System

et al. 2003

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“…On the contrary, other reports have indicated that psoralen (lethal dose 50 = 615 mg/kg), might possess genotoxicty, phototoxicity, or act as ovarian toxicants, or could inactivate cytochrome P-450 2B1 in the liver. [ 14 15 ] Furthermore, in-depth studies will be required to find in vivo potential of psoralen to become potential therapeutic phytoconstituents in the treatment of cognitive dysfunction. At the same time, efforts should be directed toward reducing toxicity and avoiding photosensitivity of psoralen.…”

Section: Resultsmentioning

confidence: 99%

In vitro acetylcholinesterase inhibition by psoralen using molecular docking and enzymatic studies

Somani¹,

Kulkarni²,

Shinde³

et al. 2015

J Pharm Bioall Sci

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Introduction:Alzheimer's disease (AD) has increased at an alarming rate and is now a worldwide health problem. Inhibitors of acetylcholinesterase (AChE) leading to inhibition of acetylcholine breakdown constitute the main therapeutic strategy for AD. Psoralen was investigated as inhibitor of AChE enzyme in an attempt to explore its potential for the management of AD.Materials and Methods:Psoralen was isolated from powdered Psoralea corylifolia fruits. AChE enzyme inhibitory activity of different concentrations of psoralen was investigated by use of in vitro enzymatic and molecular docking studies. Further, the enzyme kinetics were studied using Lineweaver-Burk plot.Results:Psoralen was found to inhibit AChE enzyme activity in a concentration-dependent manner. Kinetic studies showed psoralen inhibits AChE in a competitive manner. Molecular docking study revealed that psoralen binds well within the binding site of the enzyme showing interactions such as π-π stacking and hydrogen bonding with residues present therein.Conclusion:The result of AChE enzyme inhibitory activity of the psoralen in this study is promising. It could be further explored as a potential candidate for further development of new drugs against AD.

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“…On one hand, there are reports indicating that they do not exhibit any observable toxicity upon administration to various experimental animals (Chang & But 1986;Wall et al 1988;Sethi et al 1992). On the contrary, other reports have indicated that these compounds might possess genotoxic activities (Lagatolla et al 1998), or might act as ovarian toxicants (Diawara et al 1999), or could inactivate cytochrome P-450 2B1 in the liver (Koenigs & Trager 1998). Furocoumarins were reported to possess antiproliferative activity (Song & Tapley 1978) due to their ability to bind DNA upon ultraviolet A light (UVA) irradiation (Ben-Hur & Song 1984).…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Rat Brain Monoamine Oxidase Activities by Psoralen and Isopsoralen: Implications for the Treatment of Affective Disorders

Kong¹,

Tan²,

Woo³

et al. 2001

Pharmacol Toxicol

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Psoralen and isopsoralen, furocoumarins isolated from the plant Psoralea corylifolia L., were demonstrated to exhibit in vitro inhibitory actions on monoamine oxidase (MAO) activities in rat brain mitochondria, preferentially inhibiting MAO‐A activity over MAO‐B activity. This inhibition of enzyme activities was found to be dose‐dependent and reversible. For MAO‐A, the IC50 values are 15.2±1.3 μM psoralen and 9.0±0.6 μM isopsoralen. For MAO‐B, the IC50 values are 61.8±4.3 μM psoralen and 12.8±0.5 μM isopsoralen. Lineweaver‐Burk transformation of the inhibition data indicates that inhibition by both psoralen and isopsoralen is non‐competitive for MAO‐A. The Ki values were calculated to be 14.0 μM for psoralen and 6.5 μM for isopsoralen. On the other hand, inhibition by both psoralen and isopsoralen is competitive for MAO‐B. The Ki values were calculated to be 58.1 μM for psoralen and 10.8 μM for isopsoralen. These inhibitory actions of psoralen and isopsoralen on rat brain mitochondrial MAO activities are discussed in relation to their toxicities and their potential applications to treat affective disorders.

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Genotoxic activity of 4,4?,5?-trimethylazapsoralen on plasmid DNA

Cited by 6 publications

References 14 publications

Preclinical safety profile of plasma prepared using the INTERCEPT Blood System

Preclinical safety profile of plasma prepared using the INTERCEPT Blood System

In vitro acetylcholinesterase inhibition by psoralen using molecular docking and enzymatic studies

Inhibition of Rat Brain Monoamine Oxidase Activities by Psoralen and Isopsoralen: Implications for the Treatment of Affective Disorders

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