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1.
Pharmaceuticals (Basel) ; 17(1)2023 Dec 29.
Artículo en Inglés | MEDLINE | ID: mdl-38256897

RESUMEN

Pimenta dioica L. is one the most recognized species with diverse biological activities. In this study, in vitro activity and in vivo efficacy of essential oil from P. dioica (EO-Pd) was evaluated. The main compound was also included in the animal studies and its in silico prediction related to biological activities, molecular ligands, drug likeness, and ADME (absorption, distribution, metabolism, and excretion) properties are listed. The chemical composition analyzed by GC-MS retrieved 45 components, which the most abundant compound was the eugenol (80.1%). The EO-Pd was able to inhibit the growth of L. amazonensis (IC50 = 9.7 ± 0.7 and 11.3 ± 2.1 µg/mL, promastigotes and amastigotes, respectively). The cytotoxicity assay showed a CC50 of 104.5 ± 0.9 µg/mL and a selectivity index of 9. In the model of cutaneous leishmaniasis in BALB/c mice, the effect of EO-Pd and eugenol was observed after treatment at 30 mg/kg by intralesional route with 5 administrations every 4 days. In the in silico predictions, some targets that justified the antileishmanial activity of eugenol and good drug like properties for this compound, were obtained. This study showed for first time the potential of EO-Pd to inhibit L. amazonensis, which could be linked to the activity of major compound eugenol.

2.
Molecules ; 24(8)2019 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-31022871

RESUMEN

Essential oils (EOs) have gained increasing attention due to their pharmacological effectiveness, and they also constitute some of the most popular natural products. In this study, we present the chemical characterization of the EO from Phania matricarioides and the in vitro activity/selectivity against a wide panel of bacteria, fungi and parasitic protozoa. Forty-five compounds were identified in the studied EO, of which lavandulyl acetate (40.1%) and thymyl isobutyrate (13.9%) were the major components. The EO did not inhibit bacterial or fungal growth at the maximum concentration tested (64 µg/mL), although it displayed activity on all evaluated protozoa (IC50 values ranging from 2.2 to 56.6 µg/mL). In parallel, the EO demonstrated a noteworthy cytotoxic activity against peritoneal macrophages (CC50 values of 28.0 µg/mL). The most sensitive microorganism was Trypanosoma cruzi, which had a superior activity (IC50 = 2.2 µg/mL) and selectivity (SI = 13) in respect to other parasitic protozoa and the reference drug (p < 0.05). Further in vivo studies are needed to evaluate the potential use of this EO and the main compounds as antitrypanosomal agents. To our knowledge, this is the first report of chemical characterization and antimicrobial assessment of the EO from P. matricarioides.


Asunto(s)
Asteraceae/química , Proliferación Celular/efectos de los fármacos , Macrófagos Peritoneales/efectos de los fármacos , Aceites Volátiles/química , Antiinfecciosos/química , Antiinfecciosos/aislamiento & purificación , Antiinfecciosos/farmacología , Antiparasitarios/química , Antiparasitarios/aislamiento & purificación , Antiparasitarios/farmacología , Hongos/efectos de los fármacos , Hongos/patogenicidad , Humanos , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/aislamiento & purificación , Aceites Volátiles/farmacología , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/patogenicidad , Trypanosoma cruzi/efectos de los fármacos , Trypanosoma cruzi/patogenicidad
3.
Plants (Basel) ; 7(4)2018 Dec 14.
Artículo en Inglés | MEDLINE | ID: mdl-30558108

RESUMEN

Phania matricarioides (Spreng.) Griseb. is a traditionally used plant with various pharmacological properties. However, there are only scarce reports about the phytochemistry and biological activity of this plant. In this work, P. matricarioides was collected from three different localities of Cuba: PmB (collected in Bauta, Artemisa), PmC (collected in Cangrejeras, Artemisa), and PmI (collected in La Lisa, Havana), extracted with aqueous ethanol, and analyzed macroscopically and microscopically. The extracts were screened for phytochemical contents, analyzed by TLC and HPLC, and screened for antioxidant activity using the FRAP and DPPH assays. Macroscopic analysis showed similar results for all samples; however, microscopic, physicochemical and phytochemical studies showed appreciable differences. In particular, the total solid of PmC extract was higher (1.94 ± 0.03%) than the other samples. In HPLC profiles, quercetin was identified in the three samples and a greater similarity between samples PmB and PmI was observed. All samples demonstrated radical-scavenging antioxidant activity by the DPPH assay, which PmC also demonstrated the smaller (p < 0.05) value (IC50 = 27.4 ± 0.1 µg/mL), but was statistically superior (p < 0.05) to vitamin C (IC50 = 23.7 ± 0 µg/mL). Also, in the FRAP assay, a higher vitamin C equivalent of PmC was significantly superior (p < 0.05) to the other extracts at the evaluated concentrations, which is likely due to a higher concentration of quercetin. In conclusion, P. matricarioides could constitute a potential resource in the field of phytotherapeutic products, and the results obtained can contribute to the development of the quality control norms for this species.

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