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Ten alkaloids ( 1 – 10 ), with sophoridine ( 1 ) as the most abundant component, were obtained from the whole plants of Oxytropis ochrocephala Bunge. Furthermore, eight new sophoridine derivatives ( 11 – 16 , 20 , 21 ), with modification on the C-14 position of 1 were synthesized. All compounds ( 1 – 16 , 20 , 21 ) were evaluated for antiproliferative activity against five human tumor cell lines. Among them, the newly synthesized derivative 20 exhibited the best inhibitory activity against the tested cell lines. Its activity was increased by more than fourfold as compared with parent compound 1 . [ABSTRACT FROM AUTHOR]

Little information has been reported on the antitumor effects of the diterpenoid alkaloid constituents of Aconitum plants, used in the herbal drug ‘bushi’. This study was aimed at determining the antitumor activities of Aconitum C 19 -and C 20 -diterpenoid alkaloids and synthetic derivatives against lung (A549), prostate (DU145), nasopharyngeal (KB), and vincristine-resistant nasopharyngeal (KB-VIN) cancer cell lines. Newly synthesized C 20 -diterpenoid alkaloid derivatives showed substantial suppressive effects against all human tumor cell lines tested. In contrast, natural and derivatized C 19 -diterpenoid alkaloids showed only a slight or no effect. Most of the active compounds were hetisine-type C 20 -diterpenoid alkaloids, specifically kobusine and pseudokobusine analogs with two different substitution patterns, C-11 and C-11,15. Notably, several C 20 -diterpenoid alkaloids were more potent against multidrug-resistant KB subline KB-VIN cells. Pseudokobusine 11-3′-trifluoromethylbenzoate ( 94 ) is a possible promising new lead meriting additional evaluation against multidrug-resistant tumors. [ABSTRACT FROM AUTHOR]