- The synthesis and hepatoprotective activity of esters of the lupane group triterpenoids
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Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, and p-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bishemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.
- Flekhter,Karachurina,Poroikov,Nigmatullina,Baltina,Zarudii,Davydova,Spirikhin,Baikova,Galin,Tolstikov
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- Synthesis of phthalates of betulinic acid and betulin with cytotoxic activity
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Synthesis of 3β-O-phthalic esters from betulinic acid and its esters and synthesis of phthalic esters from betulin and its monoacetates using classical acylation procedure with phthalic anhydride. The evaluation of cytotoxicity of the prepared compounds was using numbers of tumor cell lines in MTT test. It was discovered that hemiphthalic esters had better cytotoxicity than starting compounds as betulinic acid or quite inactive betulin.
- Kvasnica, Miroslav,Sarek, Jan,Klinotova, Eva,Dzubak, Petr,Hajduch, Marian
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p. 3447 - 3454
(2007/10/03)
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