Coumarins from Artemisia

Yang, S.-L. Roberts, M. R Phillipson, J. D. Methoxylated flavones and coumarins from Artemisia annua. Phytochemistry, 1989, 28(5) 1509-1511. 

The Laboratory of Lactones, Coumarins, and Terpenoids (headed by Prof. G.P Sidyakin) studied various plants for lactone content, particularly for the lactones leucomisine and austricine, which were isolated from Artemisia leucodes. Both lactones possess pronounced anti-inflammatory action. As a compound possessing pronounced angio-protective, hypolipidemic, hypo-cholesterolemic, and anti-inflammatory actions, leucomisine has passed medical tests and has been introduced into medical practice under the preparation name Oligvon. Since 1970, systematic studies of chemical compounds found in various species of the genus Ferula, which grows in the territory of Uzbekistan and adjacent republics, have been conducted. As a result, more than 50 species of Ferula have been investigated, from which more than 250 new terpenoids, coumarins, and esters have been isolated and their chemical structures determined. Natural esters of mono- and sesquiterpene alcohols with aromatic acids were discovered for the first time in this lab (Kurmukov and Akhmedkhodzhaeva 1994). 

Among the coumarins isolated from species of Artemisia (Asteraceae), esculetin (6,7-dihydroxycoumarin) and its dimethyl-ether scoparone were known to be antiproliferative on vascular smooth muscle cells. This activity was further found in some very simple mono-substituted coumarins, which were even more potent than esculetin, although less effective. In an attempt to verify its mechanism of action, esculetin was tested for interactions with PTK and PKC. The induction of membrane PTK activity by either foetal calf serum or platelet-derived growth factor (PDGF) was moderately reduced by esculetin, whereas no effect was observed against PKC [56]. 

Capillarisin Cirsimaritin Rhamno-citrin Artemisia Capillari Spica/Compositae Whole plant Three flavonoids and two coumarins, scoparone and scopoletin, were isolated from the ethyl acetate extract of A. capillari. These compounds have been tested for their inhibitory effect on bovine lens aldose reductase (bovine-LAR) and rabbit platelet aggregation. Increased aldose reductase activity and platelet aggregation are considered as two causes of diabetic complications. Capillarisin exhibited a potent inhibitory effect on bovine-LAR. Scoparone showed strong inhibitory effect on rabbit platelet aggregation [25],... 

The compound 6,7-dimethoxycoumarin or scoparone isolated from the herb Artemisia scoparia possesses vasodilator and hypolipidemic effects and has been tested in rabbits with hyperhpidemia and diabetogenic condition. Administration of this coumarin for a week was able to reduce total cholesterol and triglycerides to normal values. Furthermore, scoparone treatment retarded the characteristic pathomorphological changes associated with hyperlipidemia such as intimal thickening or accumulation of fatty streaks and foam cells [264]. 

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