Дорно дахины уламжлалт анагаах ухаан, 2012, 2(3)
EUPHORBIA SPECIES AS PROMISING SOURCE OF DRUG DISCOVERY AND DEVELOPMENT: FROM TRADITIONAL KNOWLEDGE TO MODERN MEDICINE
( Тойм өгүүлэл )
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Абстракт
Euphorbia is the largest genus in the family Euphorbiaceae, comprising about 2000
species worlwide. Plants of Euphorbia genus have a long history of use in the
traditional medicine, especially for the treatment of different tumors, warts and cancers.
Euphorbiaceae species are well known for the chemical diversity of their isoprenoid
constituents. Among isoprenoids, highly esterified diterpenoids are of particular interest
because of their restricted occurrence and broad structural diversity. Diterpenoid
polyesters, which often are accumulated in relatively large amounts and generally occur
in complex mixtures, are based on the acylation of many different skeletons (e.g.
ingenane, tigliane, lathyrane, jatrophane and daphnane) with different aliphatic and
aromatic acids. Previous studies indicated that these types of diterpenes have a wide
variety of biological activities, such as skin-irritant, antitumor, antiviral effect and
multi-drug resistance (MDR) modulating activities.
In the course of our current interest in the chemistry and pharmacology of the genus
Euphorbia, we have investigated the secondary metabolites of E. mongolica, E.
platyphyllos and E. esula. The compounds were isolated from the CHCl3 extract of the
aerial parts by means of multistep chromatographic purification. The structure
elucidation was carried out by extensive spectroscopic analysis, including 1D and 2D
NMR and HRESIMS experiments. The compounds were identified as jatrophane
polyester acylated with acetic, propanoic, butyric, isobutyric, 2-methylbutyric, nicotinic
and benzoic acids.
The isolated compounds were tested for its MDR-reversing activity on mouse
lymphoma cells using the standard functional assay with Rhodamine 123, and found
many of them to be effective in modulating the efflux-pump activity. Moreover, the
antiproliferative activities of the diterpenes were also tested on different human tumour
cell lines. This assay revealed moderate antitumor activity of some compounds.
Acknowledgements: This publication is supported by the European Union and cofinanced
by the European Social Fund. Project title: “Creating the Center of Excellence
at the University of Szeged”. Project number: TÁMOP-4.2.1/B-09/1/KONV-2010-
0005.
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