Aim: Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents. Materials & 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 × 10 5 CFU/mL), with an effect similar to the antitubercular drugs ethambutol (2.0 × 10 5 CFU/mL) and isoniazid (1.2 × 10 5 CFU/mL). Conclusion: 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. © 2018 Newland press.

Antitubercular and anti-inflammatory properties screening of natural products from Plectranthus species / Andrade, J. M.; Custódio, L.; Romagnoli, A.; Reis, C. P.; Rodrigues, M. J.; Garcia, C.; Petruccioli, E.; Goletti, D.; Faustino, C.; Fimia, G. M.; Rijo, P.. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - 10:14(2018), pp. 1677-1691. [10.4155/fmc-2018-0043]

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

Fimia, G. M.;
2018

Abstract

Aim: Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents. Materials & 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 × 10 5 CFU/mL), with an effect similar to the antitubercular drugs ethambutol (2.0 × 10 5 CFU/mL) and isoniazid (1.2 × 10 5 CFU/mL). Conclusion: 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. © 2018 Newland press.
2018
1,6 di o acetyl 9 deoxyforskolin; 1,6 di o acetylforskolin; 11 acetoxyhalima 5,13 dien 15 oic acid; 11 acetoxyhalima 5,13 dien 15 oic acid methyl ester; 15 butyryloxyhalima 5,13 dien 11 ol; 6,7 dehydroroyleanon; 6beta,7alpha,12alpha 19 tetrahydroxy 13beta 16 cyclo 8 abietene 11,14 dione; alpha amyrin; antiinflammatory agent; antimycobacterial agent; beta amyrin; halima 5,13 diene 11,15 diol; natural product; nitric oxide; plectrornatine C; rosmarinic acid; sitosterol; stigmasterol; toll like receptor 4; unclassified drug; antiinflammatory agent; biological product; lipopolysaccharide; nitric oxide; tuberculostatic agent, animal cell; antiinflammatory activity; antitubercular activity; Article; bacterial strain; colony forming unit; controlled study; drug activity; drug determination; drug effect; drug screening; drug structure; human; human cell; IC50; in vitro study; macrophage; minimum inhibitory concentration; Mycobacterium tuberculosis; nonhuman; phytochemistry; Plectranthus; Plectranthus ecklonii; Plectranthus grandidentatus; Plectranthus madagascariensis; Plectranthus neochilus; Plectranthus ornatus; Plectranthus porcatus; Plectranthus prostratus; priority journal; quantitative analysis; RAW 264.7 cell line; animal; cell survival; chemistry; cytology; isolation and purification; medicinal plant; metabolism; microbial sensitivity test; mononuclear cell; mouse; Plectranthus, Animals; Anti-Inflammatory Agents; Antitubercular Agents; Biological Products; Cell Survival; Leukocytes, Mononuclear; Lipopolysaccharides; Macrophages; Mice; Microbial Sensitivity Tests; Mycobacterium tuberculosis; Nitric Oxide; Plants, Medicinal; Plectranthus; RAW 264.7 Cells; anti-inflammatory; Mycobacterium tuberculosis; Plectranthus spp.; SNAP; terpenoids; tuberculosis
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Antitubercular and anti-inflammatory properties screening of natural products from Plectranthus species / Andrade, J. M.; Custódio, L.; Romagnoli, A.; Reis, C. P.; Rodrigues, M. J.; Garcia, C.; Petruccioli, E.; Goletti, D.; Faustino, C.; Fimia, G. M.; Rijo, P.. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - 10:14(2018), pp. 1677-1691. [10.4155/fmc-2018-0043]
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