The pharmacokinetic parameters of aristolochic acid-Ⅰ (AA-Ⅰ) and -Ⅱ (AA-Ⅱ) in rat serum after intragastrical administration of the crude drug powders of Radix Aristolochiae (RA) and Muskone containing equal amounts of RA were compared. The pharmacokinetic profiles of AA-Ⅰ and AA-Ⅱ could be fitted with a two-compartment model The elimination half time (T1/2β) of AA-Ⅰ in Muskone was 1573.2 min and that of AA-Ⅰ in RA was 475.8 min; T1/2β of AA-Ⅱ in Muskone was 2344.8 min and that of AA-Ⅱ in RA was 427.8 rain. The area under the concentration-time curve (AUC) of AA-Ⅰ in Muskone was 13.07 μg/h/mL and that of AA-Ⅰ in RA was 3.86 μg/h/mL; AUC of AA-Ⅱ in Muskone was 67.67 μg/h/mL and that of AA-Ⅱ in RA was 23.93 μg/h/mL. The bioavailabilities of AA-Ⅰ and AA-Ⅱ in Muskone were markedly increased compared with that in RA based on the elimination half-time and A UC values.
Chemical constituents of the whole herb of Saruma henryi Oliv. were investigated. The herbal extract was separated by repeated column chromatography over silica gel and celite. The structures were elucidated by spectroscopic analysis. Thirteen compounds were obtained and identified as 7-methoxyl-aristololactam Ⅳ (1), aristololactam Ⅱ (2), aristolochic acid Ⅰ (3), aristololactam AⅡ (4), daucosterol (5), aristololactam Ⅰa (6), N-trans-feruloyl tyramine (7), aristololactam Ⅰ (8), 4β,10β-aromadendranediol (9), aristololide (10), aristolic acid Ⅰ (11), meso-dihydroguaiaretic acid (12), and calopiptin (13). These compounds were obtained from the genus Saruma for the first time, and they provided chemical evidences for the chemotaxonomy of plants of the Aristolochiaceae family. Since aristolochic acids and aristololactams are toxic to kidney, the results of this investigation suggest that it should be cautious to use Saruma henryi as a medicine.
A new aristololactam, aristololactam Ⅶ (1), was isolated from the root and rhizome of Asarum maximum Hemsl. On the basis of spectroscopic analysis, its structure was identified as 10-amino-7,8-dimethoxy-3,4-methylenedioxy-phenanthrene-1- earboxylie acid laetam.