Inhibitory Effect of Carnosolic Acid on HIV-1 Protease in Cell-Free Assays
| Autor: | Marko Pukl, B Strukelj, Alenka Pariš, Andrej Umek, V Turk, B.D. Korant, M. Renko |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Pharmacology
chemistry.chemical_classification Protease biology medicine.medical_treatment Organic Chemistry Pharmaceutical Science Carnosic acid biology.organism_classification Molecular biology Carnosol Rosmarinus Analytical Chemistry chemistry.chemical_compound Enzyme Complementary and alternative medicine chemistry HIV-1 protease Biochemistry Enzyme inhibitor Drug Discovery biology.protein medicine Molecular Medicine HIV Protease Inhibitor |
| Zdroj: | Journal of Natural Products. 56:1426-1430 |
| ISSN: | 1520-6025 0163-3864 |
| DOI: | 10.1021/np50098a031 |
| Popis: | In order to find new effective HIV protease inhibitors, two diterpenes (carnosic acid [1] and carnosol [5]) were isolated from rosemary (Rosmarinus officinalis L.), and rosmanol [2] and semisynthetic derivatives (7-O-methylrosmanol [3], 7-O-ethylrosmanol [4], and 11,12-O,O-dimethylcarnosol [6]) were prepared. The inhibitory activity of all six compounds against HIV-1 protease was tested. The carnosic acid [1] showed the strongest inhibitory effect (IC90 = 0.08 micrograms/ml). The same compound was also assayed against HIV-1 virus replication (IC90 = 0.32 micrograms/ml). The cytotoxic TC90 on H9 lymphocytes was 0.36 micrograms/ml, which is very close to the effective antiviral dose. Additionally, the tested compounds did not inhibit cellular aspartic proteases cathepsin D and pepsin at the concentration range up to 10 micrograms/ml [corrected]. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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