Chemical constituents of Buddlejae officinalis and their bioactivities / 中草药

ABSTRACT

Object To investigate the chemical constituents of Buddlejae officinalis Maxim. , the relationship between their bioactivities, and the medicinal application of the herb. Methods Various chro-matographic techniques were employed for the isolation and purification of the constituents, including silica gel, Sephadex LH-20, and pre-HPLC. The structures of 11 isolated chemical compounds were elucidated by chemical and spectral analysis (NMR, IR, UV, and MS). The aldose reductase inhibiting test and test on DNA topoisomerase Ⅳ inhibitory effect were applied to evaluate the bioactivity of both the purified compounds and the crude fraction. Results Eleven compounds were isolated from the extracts of B. offic-inalis. They are four flavones and their glycosides; apigenin (Ⅰ), linarin (Ⅱ), apigenin-7-O-?-L-rhamnopyranosyl (1-6)-?-D-glucopyranoside (Ⅲ), and luteolin-7-O-?-D-glucoside (Ⅶ); four phenylen-thanoid glycosides: verbascoside (Ⅴ), isoacteoside (Ⅵ), cistanoside F, a and b (Ⅶ-1 and 2), campneo-side Ⅱ , a and b (Ⅷ-1 and 2); three triferpenoid saponins: mimengoside A (Ⅸ), mimengoside B (Ⅹ), songaroside A (Ⅺ). Some of the them (such as Ⅱ ,Ⅲ , and Ⅵ) showed the aldose reductase inhibitory activities with a higher inhibitory rate than that of quercetin (the positive control), others (such as Ⅰ,Ⅱ , Ⅴ, Ⅵ, and Ⅺ) displayed the inhibititory activities against the DNA topoisomerase Ⅳ . Conclusion Among all the isolated compounds, Ⅲ , Ⅶ-1 and 2, Ⅷ-1 and 2, and Ⅺ are separated for the first time both from the plant and the genus. Their bioactivities of bacteriostatic and against aldose reductase with DNA topoisomerase Ⅳ as target are tested for the first time and are related to the medicinal application of B. officinalis.