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Chemistry for Sustainable Development

2010 year, number 4

Derivatives of Methyllambertianate as Promising Correctors of Cytostatics with Hepatoprotective and Hemostimulating Activity

I. V. Sorokina, T. G. Tolstikova, D. S. Baev, N. A. Zhukova, Y. V. Kharitonov
Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences
sorokina@nioch.nsc.ru
Keywords: methyllambertianate, hepatoprotective, antioxidant, hemostimulating activity
Pages: 419-424

Abstract

Results of the development of three original labdanum antioxidants based on the methyl ester of lambertianic acid, an available plant metabolite of Siberian pine Pinus sibirica R. Mayr. are presented. As a result of screening with the model of toxic CCl4-hepatitis induced in mice, the agents surpassing the known flavonoid dihydroquercetin in the anticytolytic and anticholestase action. It is shown that under the conditions of hemodepression caused by the introduction of cytostatic preparation cyclophosphane to rats, the compounds significantly decrease leukopenia by increasing the number of granulocytes and monocytes in blood. At the background of cyclophosphane, the derivatives of methyllambertianate exhibit higher antioxidant activity than dihydroquercetin does. The azlactone demonstrates pronounced anticholestase properties. The pharmacological properties discovered in the new derivatives of lambertianic acid allow considering them as potential correctors of chemotherapeutical preparations.