New Targets for Growth Inhibition of Mycobacterium tuberculosis: Why Do Natural Terpenoids Exhibit Antitubercular Activity?
| Autor: | B. F. Garifullin, Vladimir E. Kataev, R. N. Khaybullin, R. R. Sharipova |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Tuberculosis biology 010405 organic chemistry Chemistry Organic Chemistry Phosphatase Virulence medicine.disease biology.organism_classification 01 natural sciences Biochemistry Cyclase Terpenoid 0104 chemical sciences Mycobacterium tuberculosis 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology medicine Growth inhibition Diterpene |
| Zdroj: | Russian Journal of Bioorganic Chemistry. 44:438-452 |
| ISSN: | 1608-330X 1068-1620 |
| DOI: | 10.1134/s1068162018040106 |
| Popis: | The article draws the attention of chemists to the literature data reporting the discovery of new targets for growth inhibition of Mycobacterium tuberculosis, namely, diterpene cyclase (Rv3377c) and tuberculosinol phosphatase (Rv3378c), which produce diterpenoids of tuberculosinols in the cell membrane of M. tuberculosis, and these diterpenoids ensure the pathogenicity and the virulence of M. tuberculosis. For the first time, by the example of diterpenoid of isosteviol, its binuclear derivatives, triterpenoid betulinic, oleanolic, and ursolic acids, it has been shown by the molecular docking method that the antitubercular activity of natural terpenoids is caused by their ability to bind to the active site of tuberculosinol phosphatase (Rv3378c) of M. tuberculosis. It is suggested that natural and semisynthetic terpenoids represent a promising platform for design of a new generation of antitubercular agents that affect this enzyme. |
| Databáze: | OpenAIRE |
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