OBJECTIVETo study the chemical constituents in the introduced Coleus forskohlii.

METHODThe chemical constituents were isolated by column chromato-graphy. The structures were elucidated on the basis of IR, MS, 1H-NMR and 13C-NMR experiments.

RESULTEight compounds were obtained, the structures of which were identified as cytochalasin B (1), N-benzoyl-L-phenylalaninol (2), 3,6-dibenzyl-2,5-dioxopiperazine (3), 2-furoic acid (4), vanillic acid (5), loliolide (6) and forskolin D (7).

CONCLUSIONCompounds 1-6 were isolated from the genus Coleus for the first time.

Coleus ; chemistry ; Plant Extracts ; chemistry

OBJECTIVETo study the chemical constituents in root of Coleusforskohlii.

METHODThe chemical constituents were isolated by column chromatography. The structures were elucidated on the basis of IR, MS, 1H-NMR, 13C-NMR and 2D-NMR experiments.

RESULTSix compounds were obtained and the structures were identified as 14-deoxycoleon U (1), demethylcryptojaponol (2), alpha-amyrin (3), betulic acid (4), alpha-cedrol (5) and beta-sitosterol (6).

CONCLUSIONCompounds 1 and 2 were isolated from the genus Coleus for the first time. Compounds 3 and 4 were isolated from C. forskohlii for the first time.

Coleus ; chemistry ; Diterpenes ; chemistry ; isolation & purification ; Oleanolic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Triterpenes ; chemistry ; isolation & purification

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.
Animals ; Chromatography, High Pressure Liquid ; Coleus ; chemistry ; Colforsin ; blood ; isolation & purification ; metabolism ; Cytochrome P-450 CYP3A ; metabolism ; Dogs ; Humans ; Macaca ; Metabolic Clearance Rate ; Microsomes, Liver ; metabolism ; Plants, Medicinal ; chemistry ; Rats ; Tandem Mass Spectrometry