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Métodos Terapéuticos y Terapias MTCI
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1.
J Enzyme Inhib Med Chem ; 36(1): 257-269, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33322969

RESUMEN

A series of Plectranthus spp. plant extracts (aqueous, acetonic, methanolic and ethyl acetic) obtained from eight different species, and previously isolated compounds (ranging from polyphenols, diterpenes and triterpenes), were assayed for in vitro inhibition of the skin-related enzymes tyrosinase, collagenase and elastase, and for studying their antioxidant properties. The ethyl acetic extracts of P. grandidentatus and P. ecklonii registered the highest antioxidant activity, whereas acetonic, methanolic and ethyl acetic extracts of P. ecklonii, P. grandidentatus, P. madagascariensis and P. saccatus concerning the enzymatic inhibition assays revealed high anti-tyrosinase and anti-collagenase activities. From the isolated compounds tested, abietane diterpenes and triterpenes were highly active against tyrosinase and elastase activity. Overall, the experimental results showed the powerful antioxidant and inhibitory action on skin-related enzymes tyrosinase, collagenase and elastase of Plectranthus spp. extracts and/or isolated compounds, supporting their further research as bioactive metabolites against skin sagging and hyperpigmentation in cosmetic and pharmaceutical formulations.


Asunto(s)
Antioxidantes/farmacología , Colagenasas/metabolismo , Monofenol Monooxigenasa/antagonistas & inhibidores , Elastasa Pancreática/antagonistas & inhibidores , Extractos Vegetales/farmacología , Plectranthus/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Humanos , Conformación Molecular , Monofenol Monooxigenasa/metabolismo , Elastasa Pancreática/metabolismo , Picratos/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Piel/efectos de los fármacos , Piel/metabolismo , Especificidad de la Especie , Relación Estructura-Actividad
2.
Oxid Med Cell Longev ; 2019: 9165784, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31737178

RESUMEN

Menyanthes trifoliata L. is a valuable medical plant found in Europe, North America, and Asia, which grows on peat bogs and swamps. It has long been used in folk medicine as a remedy for various ailments. This is the first report to demonstrate the protective antioxidant and anti-inflammatory properties of aqueous methanolic extracts derived from the aerial parts (MtAPV) and roots (MtRV) of in vitro grown plants on human umbilical vein endothelial cells (HUVECs). It describes the influence of the tested extracts on the expression of antioxidant (HO-1, NQO1, NRF2, kEAP1, and GCLC) and inflammation-related genes (IL-1α, IL-1ß, IL-6, TNF-α, and IFN-γ) in cells stimulated with H2O2 or LPS, respectively. In addition, M. trifoliata extracts were found to moderately affect the growth of certain bacterial and fungal pathogens, with the strongest antibacterial effect found against Pseudomonas aeruginosa and Enterococcus faecalis. M. trifoliata extracts demonstrated protective effects against mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) damage caused by ROS, decreasing the numbers of mtDNA lesions in the ND1 and ND2 genes and nDNA damage in the TP53 and HPRT1 genes and reducing cleavage in PARP1- and γ-H2A.X-positive cells. The root extract of in vitro M. trifoliata (MtRV) appears to have better anti-inflammatory, antioxidant, antimicrobial, and protective properties than the extract from the aerial part (MtAPV). These differences in biological properties may result from the higher content of selected phenolic compounds and betulinic acid in the MtRV than in the MtAPV extract.


Asunto(s)
Antiinfecciosos/farmacología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , ADN Mitocondrial/fisiología , Endotelio Vascular/efectos de los fármacos , Enterococcus faecalis/fisiología , Inhibidores de Crecimiento/farmacología , Magnoliaceae/química , Extractos Vegetales/farmacología , Pseudomonas aeruginosa/fisiología , Citocinas/metabolismo , Endotelio Vascular/patología , Enterococcus faecalis/efectos de los fármacos , Inhibidores de Crecimiento/química , Células Endoteliales de la Vena Umbilical Humana , Humanos , Oxidación-Reducción , Extractos Vegetales/química , Raíces de Plantas , Pseudomonas aeruginosa/efectos de los fármacos , Proteína p53 Supresora de Tumor/genética
3.
Future Med Chem ; 10(14): 1677-1691, 2018 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-29957070

RESUMEN

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 × 105 CFU/mL), with an effect similar to the antitubercular drugs ethambutol (2.0 × 105 CFU/mL) and isoniazid (1.2 × 105 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.


Asunto(s)
Antiinflamatorios/química , Antituberculosos/química , Productos Biológicos/química , Plectranthus/química , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Antituberculosos/aislamiento & purificación , Antituberculosos/farmacología , Productos Biológicos/aislamiento & purificación , Productos Biológicos/farmacología , Supervivencia Celular/efectos de los fármacos , Leucocitos Mononucleares/citología , Leucocitos Mononucleares/efectos de los fármacos , Leucocitos Mononucleares/metabolismo , Lipopolisacáridos/farmacología , Macrófagos/citología , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Óxido Nítrico/química , Óxido Nítrico/metabolismo , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Plectranthus/metabolismo , Células RAW 264.7
4.
Future Med Chem ; 10(10): 1177-1189, 2018 05 01.
Artículo en Inglés | MEDLINE | ID: mdl-29749759

RESUMEN

AIM: 6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis. METHODS/RESULTS: Different extraction parameters were tested, and its extraction optimization was accomplished with a Clevenger apparatus-based hydrodistillation. After isolation, its effect on microtubules, P-glycoprotein and caspases was assessed on several cell lines and the compound was coupled with hybrid nanoparticles. The results show that DHR does not interfere with microtubule formation, but evades the resistance mechanisms of P-glycoprotein. Strong activation of caspases-3 and -9 indicates that DHR is able to induce apoptosis by triggering the intrinsic cell death pathway. Moreover, the assembly of DHR with hybrid nanoparticles was able to potentiate the effect of DHR in cancer cells. CONCLUSION: DHR seems to be a promising starting material with anticancer properties to further be explored.


Asunto(s)
Abietanos/química , Antineoplásicos Fitogénicos/química , Subfamilia B de Transportador de Casetes de Unión a ATP/química , Subfamilia B de Transportador de Casetes de Unión a ATP/metabolismo , Abietanos/aislamiento & purificación , Abietanos/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Caspasas/metabolismo , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Humanos , Nanopartículas/química , Aceites Volátiles/química , Extractos Vegetales/química , Plectranthus/química , Plectranthus/metabolismo
5.
Future Sci OA ; 4(4): FSO283, 2018 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-29682318

RESUMEN

The worldwide interest in the use of medicinal plants has been growing, and its beneficial effects being rediscovered for the development of new drugs. Based on their vast ethnopharmacological applications, which inspired current research in drug discovery, natural products can provide new and important leads against various pharmacological targets. This work pioneers an extensive and an updated literature review on the current state of research on Rosmarinus officinalis L., elucidating which compounds and biological activities are the most relevant. Therefore, a search was made in the databases PubMed, ScienceDirect and Web of Science with the terms 'rosemary', 'Rosmarinus officinalis', 'rosmarinic acid' 'carnosol' and 'carnosic acid', which included 286 articles published since 1990 about rosemary's pharmacological activities and their isolated compounds. According to these references, there has been an increasing interest in the therapeutic properties of this plant, regarding carnosic acid, carnosol, rosmarinic acid and the essential oil. The present manuscript provides an updated review upon the most reported activities on R. officinalis and its active constituents.

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