Speaker
Ms
Maria Mayordomo Martinez
(Department of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, CTU Prague)
Description
Triterpenes are a group of natural compounds. They are studied for their wide spectrum of biological activities: antitumor, antimutagenic, antiinflammatory, antiallergy, endocrine, immunomodulatory, antiviral, hepatoprotective, cardioprotective, antithrombotic or activities on central nervous system.1
Nowadays the investigation of antitumor drugs is really important because over one million people get cancer each year and this quantity is increasing every year.
Some of the most important triterpenes are betulin andbetulinic acid and their derivatives2, which have demonstrated selective cytotoxicity against a number of specific tumor lines, HIV disseas, a variety of infectious agents such as malaria and bacteria, and the inflammatory process in general. The derivatives and potencial drugs from betulinic acid can be used to kill and/or inhibit multiplication of tumor cells. This type of drugs need to have high cytotoxic activity, low toxicity and have to be easily aviable.
We are focusing on the synthesis of semisynthetic derivatives of betulin and betulinic, heterobetulinic and morolic acids (lupane and taraxastane type) selectively labelled by deuterium, 2H and tritium 3H, carbon-13 and carbon-14.
That labelled compounds are essential for supporting of pharmacokinetic and toxicological evaluations which help with better understanding of methabolic pathways which are proceeding in investigated organism. We trust that labelled derivatives help us with investigation of mechanism of action and indentification of primary target.
All the synthesized compounds are tested on the board of tumors lines for their cytotoxic activity in vitro and in vivo in LEM, hoped to obtain new anticancer drugs.
References:
1.P. Dzubak, M. Hajduch, D. Vydra, A. Hustova, M. Kvasnica, D. Biedermann, L. Markova, M. Urban, J. Sarek, Nat. Prod. Rep., 2006, 23, 394-411.
2.E. R. Trumbull, E. Bianchi, D. J. Eckert, R. M. Wiedhopf, J. R. Cole, J. Pharm. Sci., 1976, 65, 1407-1408.
Primary author
Ms
Maria Mayordomo Martinez
(Department of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, CTU Prague)
Co-authors
Mr
Jan Sarek
(Department of Organic Chemistry, Faculty of Science, Palacky University, Trida 17. listopadu 12, 772 07 Olomouc, Czech Republic)
Ms
Marian Hajduch
(Laboratory of Experimental Medicine, Faculty of Medicine and Dentistry, Palacky University, Puskinova 6, 772 07 Olomouc, Czech Republic)
Mr
Martin Vlk
(Department of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, Czech Technical University, Brehova 7, 115 19 Prague 1, Czech Republic)
Mr
Tomas Elbert
(Laboratory of Radioisotopes, Institute of Organic Chemistry and Biochemistry, Academy of Sciences, Flemingovo n. 2, 166 10 Prague 6, Czech Republic)
