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Future Medicinal Chemistry 2018-Jul

Antitubercular and anti-inflammatory properties screening of natural products from Plectranthus species.

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Krækjan er vistuð á klemmuspjaldið
Joana M Andrade
Luísa Custódio
Alessandra Romagnoli
Catarina P Reis
Maria J Rodrigues
Catarina Garcia
Elisa Petruccioli
Delia Goletti
Célia Faustino
Gian M Fimia

Lykilorð

Útdráttur

OBJECTIVE

Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents.

METHODS

Compounds previously isolated from Plectranthus spp. were studied for their anti-inflammatory activity using the SNAP assay and RAW 264.7 cells, by the quantification of nitric oxide. An halimane diterpene and its derivatives were tested in infected macrophages with M. tuberculosis H37Rv, using CFU counts assay, at their minimum inhibitory concentration values. Results: The isolated compounds tested at noncytotoxic concentrations, did not reveal nitric oxide scavenging in the S-nitroso-N-acetylpenicillamine and the cellular assays. On the other hand, promising results were obtained regarding one semisynthetic halimane derivative (11R*,13E)-halima-5,13-diene-11,15-diol), previously prepared (2.1 × 105 CFU/mL), with an effect similar to the antitubercular drugs ethambutol (2.0 × 105 CFU/mL) and isoniazid (1.2 × 105 CFU/mL).

CONCLUSIONS

The present report demonstrates the relevance of Plectranthus spp. in medicinal chemistry drug development for TB and other infective respiratory complaints. Also, this work suggests that further studies involving other inflammatory mediators are needed to validate the anti-inflammatory use of these medicinal plants.

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