Aconitum species are known to produce variously substituted diterpene alkaloids (DAs), many of which exhibit high toxicity and a broad spectrum of pharmacological effects. A research programme dealing with Aconitum species native to the Carpathian Basin has been started at the Department of Pharmacognosy, University of Szeged, in 2001. As a part of this still ongoing comprehensive phytochemical project, the alkaloid composition of Aconitum anthora and A. moldavicum was investigated. Besides the above the herein work reports the semisynthesis and purification of a series of lipo-alkaloids (LAs) derived from aconitine and the evaluation of the in vitro anti-inflammatory activity of these LAs, and the hERG and Nav1.2 channel activities of previously or newly isolated DAs; and the quantitative determination of toxic diester DAs in authentic processed A. carmichaelii and A. kusnezoffii samples. With the worldwide increasing spread of the Far Eastern traditional medicinal systems, and with the increasing public interest towards phytomedicines, pharmacological and phytoanalytical studies on aconite drugs are of growing importance and may be of interest for all who work in these fields.