Coumarin Metabolism, Toxicity and Carcinogenicity: Relevance for Human Risk Assessment

Lake, Brian G.

doi:10.1016/s0278-6915(99)00010-1

Cited by 471 publications

(421 citation statements)

References 156 publications

Supporting

Mentioning

400

Contrasting

Unclassified

Order By: Relevance

“…For coumarin, half-lives (t 1/2 ) of between 60-240 h were found in humans and other species, such as rats (Lake, 1999).…”

Section: Discussionmentioning

confidence: 99%

“…This fact suggests that 6MC is rapidly eliminated from the systemic circulation (t 1/2 less than 2 hour and high apparent clearance) or extensively metabolized. Previous studies on the in vivo metabolism of coumarins reported that coumarins are metabolized mainly into two kinds of compounds: its hydroxyl derivatives, and its smaller acid derivatives, such as ortho-hydroxyphenyllactic acid, ortho-hydroxyphenylacetic acid and orthohydroxyphenylpropionic acid (Lake, 1999).…”

Section: Discussionmentioning

confidence: 99%

“…Another peak (Rt = 11.8, [M+H]+ (m/z) 657.3) was observed, but was not possible to propose a structure, because the molecular weight is not comparable with the common metabolites of coumarin structure. The conjugation with glutathione (GSH) is common for coumarin (Lake, 1999).…”

Section: Discussionmentioning

confidence: 99%

See 2 more Smart Citations

In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats

Cárdenas

Kratz

Hernández

et al. 2017

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo antiinflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (K e ) 0.0070 min -1 and a short life half time of (T

show abstract

“…For coumarin, half-lives (t 1/2 ) of between 60-240 h were found in humans and other species, such as rats (Lake, 1999).…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats

Cárdenas

Kratz

Hernández

et al. 2017

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

show abstract

“…: coumarin, 3,4-dihydrocoumarin, bergapten [3,4,11]. This particular group with coumarin as a main compound, is responsible for the specific sweet, cheery-like aroma of southern sweet-grass herb [17,18]. The content of coumarin in the raw material depends on the origin of the herb, developmental phase of plants during harvest, plant age, fertilization and drying conditions [3,4,10,14,15].…”

Section: Air Dry Mass Of Leaves [G × Plant -1 ]mentioning

confidence: 99%

Setting of southern sweet-grass plantation with stem cuttings obtained by division of maternal plants

et al. 2015

View full text Add to dashboard Cite

S u m m a r ySouthern sweet-grass (Hierochloë australis /Schrad./ Roem. & Schult.) is a perennial, wild growing tuft grass occurring in North-East Poland, Belarus and Finland. In Poland the species is under the partial legal protection. The raw material harvested from this plant are leaves rich in coumarins, mainly in coumarin responsible for specific sweet aroma of leaves. They are used mostly for the aromatization of alcohol and tobacco products. Due to high demand for the raw material and decrease in the natural resources of the species, it is advisable to introduce the plant into cultivation. In the presented study vegetative planting stock (1-, 2-, and 4-stem cuttings) were used to set the plantation of southern sweet-grass. The influence of the planting stock type on the mass of leaves and their quality in the first and second year of plant vegetation as well as the mass of seeds from two-year-old plants were investigated. The highest number of well rooted plants was obtained from 4-stem cuttings (74.07%) and the least -from 1-stem cuttings (47.53%). Both, on one-and two-year-old plantations the plants from 4-stem cuttings were characterized by the highest mass of leaves (7.73 and 24.65 g × plant -1 , respectively). The plants were also characterized by the highest number of generative shoots (40.71 pcs. × plant -1 ) and mass of seeds (4.62 g × plant -1 ). The total contents of coumarins and phenolic acids did not depend on the type of planting stock. The contents of these compounds was higher in two-year-old plants than in one-year-old ones, whereas the content of flavonoids was higher in one-year-old plants.

show abstract

“…Both natural as well as synthetic coumarins are in clinical trials for the treatment of various types of cancers because of their tendency to induce carcinoma cell apoptosis [14]. 5,7-Dimethoxycoumarin (Figure 1), a derivative of coumarin present in vegetables has shown potent anti-cancer activity through induction of DNA damage and inhibition of carcinoma cell proliferation [15,16].…”

Section: Introductionmentioning

confidence: 99%

5,7-Dimethoxycoumarin inhibits neuronal apoptosis by targeting caspase-3 expression in rats with acute cerebral infarction

Ma¹,

Wang²

2017

Trop. J. Pharm Res

View full text Add to dashboard Cite

show abstract

Coumarin Metabolism, Toxicity and Carcinogenicity: Relevance for Human Risk Assessment

Cited by 471 publications

References 156 publications

In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats

In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats

Setting of southern sweet-grass plantation with stem cuttings obtained by division of maternal plants

5,7-Dimethoxycoumarin inhibits neuronal apoptosis by targeting caspase-3 expression in rats with acute cerebral infarction

Contact Info

Product

Resources

About