In vitro metabolism of forscolin isolated from Coleus forskohlii / 药学学报
Acta Pharmaceutica Sinica
;
(12): 383-389, 2013.
Artículo
en Chino
| WPRIM
| ID: wpr-235655
ABSTRACT
This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Plantas Medicinales
/
Sangre
/
Colforsina
/
Microsomas Hepáticos
/
Tasa de Depuración Metabólica
/
Química
/
Cromatografía Líquida de Alta Presión
/
Coleus
/
Citocromo P-450 CYP3A
/
Espectrometría de Masas en Tándem
Límite:
Animales
/
Humanos
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2013
Tipo del documento:
Artículo
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