ABSTRACT
A total of twenty-two diterpenoid alkaloids, including ten unprecedented ones, namely refractines C-L, were isolated from the roots of Aconitum refractum (Finet et Gagnep.) Hand.-Mazz. Refractine C was the first example of a natural diterpenoid alkaloid wherein C-19 is linked to N position by an oxaziridine ring. Refractine L was a rare glycosidic diterpenoid alkaloid with fructofuranoside. Most of the isolated compounds obtained from a previous study were screened for their anti-inflammatory and myocardial protective activities. The autophagy-inducing effects of some of these compounds on RAW 264.7 cells were evaluated by assessing the expression of microtubule-associated protein 1 light chain 3 (LC3-II/LC3-I). Results revealed that some compounds exerted varying levels of inhibitory effects on the proliferative activity of RAW 264.7 cells.
Subject(s)
Aconitum , Alkaloids , Autophagy , Diterpenes , Aconitum/chemistry , Mice , Animals , Autophagy/drug effects , RAW 264.7 Cells , Alkaloids/pharmacology , Alkaloids/isolation & purification , Alkaloids/chemistry , Diterpenes/pharmacology , Diterpenes/chemistry , Diterpenes/isolation & purification , Cell Proliferation/drug effects , Molecular Structure , Structure-Activity Relationship , Dose-Response Relationship, Drug , Plant Roots/chemistryABSTRACT
Two unprecedented aconitine-type C19-diterpenoid alkaloids, refractines A-B (1-2), along with 12 known compounds (3-14) were isolated from the roots of Aconitum refractum (Finet et Gagnep.) Hand. -Mazz. Their structures were elucidated based on extensive spectroscopic analyses, including 1D and 2D NMR, IR, and HR-ESI-MS data. All compounds were tested for inhibitory activities against NO production in LPS induced RAW 264.7 macrophages, compounds 10 and 14 had slight inhibited NO production with rate of 29.4% and 22.1% at the concentration of 30 µM, respectively.