RESUMO
Blueberries (Vaccinium corymbosum L.) are cultivated worldwide and are among the best dietary sources of bioactive compounds with beneficial health effects. This study aimed to investigate the components of Peruvian blueberry using high-performance liquid chromatography coupled to electrospray ionization and quadrupole time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS/MS), identifying 11 compounds. Furthermore, we assessed in vitro the antioxidant activity and in vivo the antidepressant effect using a rat model and protective effect on lipid peroxidation (in the serum, brain, liver, and stomach). We also conducted molecular docking simulations with proteins involved in oxidative stress and depression for the identified compounds. Antioxidant activity was assessed by measuring total phenolic and flavonoid contents, as well as using 1,1-diphenyl-2-picrylhydrazin (DPPH), 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid (ABTSâ¢+), and ferric-reducing antioxidant power (FRAP) assays. Peruvian blueberries demonstrated higher antioxidant activity than Vaccinium corymbosum fruits from Chile, Brazil, the United States, Turkey, Portugal, and China. The results showed that oral administration of Peruvian blueberries (10 and 20 mg/kg) for 28 days significantly (p < 0.001) increased swimming and reduced immobility in the forced swimming test (FST). Additionally, at doses of 40 and 80 mg/kg, oxidative stress was reduced in vivo (p < 0.001) by decreasing lipid peroxidation in brain, liver, stomach, and serum. Molecular docking and absorption, distribution, metabolism, excretion, and toxicity (ADMET) predictions were performed. In the molecular docking studies, quercitrin and 3,5-di-O-caffeoylquinic acid showed the best docking scores for nicotinamide adenine dinucleotide phosphate (NADPH) oxidase, superoxide dismutase, and xanthine oxidase; while 3,5-dicaffeoylquinic acid methyl ester and caffeoyl coumaroylquinic acid had the best docking scores for monoamine oxidase and serotonin receptor 5-HT2. In summary, our results suggest that the antidepressant and protective effects against lipid peroxidation might be related to the antioxidant activity of Peruvian Vaccinium corymbosum L.
RESUMO
The purpose of this work was to evaluate the antioxidant capacity of Prosopis pallida (Fabaceae) fruits "algarrobo", in addition to determine their main chemical components. Fruit purified extracts from the regions of Tumbes, Piura, Lambayeque, and La Libertad (Peru) were evaluated using infusion, decoction, and alcoholic extraction at concentrations of 45, 70 and 96%. To measure the antioxidant capacity of the extracts, the determination of total phenolics content was performed, followed by the antioxidant evaluation using DPPH, FRAP and ABTS. The chemical identification was carried out through UHPLC-UV-MS/MS. The results showed that the decoction of the sample from the region of La Libertad, as well as the ethanol extracts at 45% of the samples from Tumbes and Lambayeque presented greater antioxidant capacity. Moreover, ten major substances of these extracts were identified: nine phenolic derivatives (vicenin II as the main constituent of the extracts) and one diterpene (7-oxodehydroabietic acid).
El propósito de este trabajo fue evaluar la capacidad antioxidante de frutos de Prosopis pallida (Fabaceae) "algarrobo", además de determinar sus principales componentes químicos. Se estudiaron extractos purificados de frutos de las regiones de Tumbes, Piura, Lambayeque y La Libertad (Perú), mediante infusión, decocción y extracción alcohólica en concentraciones de 45, 70 y 96%. Para medir la capacidad antioxidante de los extractos, se realizó la determinación del contenido de fenoles totales, seguida de la evaluación antioxidante mediante DPPH, FRAP y ABTS. La identificación química se realizó mediante UHPLC-UV-MS/MS. Los resultados mostraron que la decocción de la muestra de la región de La Libertad, así como los extractos de etanol al 45% de las muestras de Tumbes y Lambayeque presentaron mayor capacidad antioxidante. Además, se identificaron diez sustancias principales de estos extractos: nueve derivados fenólicos (vicenin II como componente principal de los extractos) y un diterpeno (ácido 7-oxodehidroabiético).
Assuntos
Extratos Vegetais/farmacologia , Extratos Vegetais/química , Prosopis/química , Antioxidantes/farmacologia , Peru , Plantas Medicinais , Medicina TradicionalRESUMO
Leishmaniasis is caused by protozoan parasites belonging to the genus Leishmania and includes cutaneous, mucocutaneous and visceral clinical forms. Drugs currently available for leishmaniasis treatment present high toxicity, and development of parasite resistance. Plants constitute an important source of compounds with leishmanicidal potential. This study aimed to evaluate the anti-Leishmania amazonensis activity of the terpenoid fraction of Eugenia pruniformis leaves (TF-EpL). TF-EpL was active against the promastigote and intracellular amastigote forms of L. amazonensis with IC50(24h) value of 43.60µg/mL and 44.77µg/mL, respectively. TF-EpL altered the cell cycle of the parasite, increasing 2.32-fold the cells in the Sub-G0/G1 phase. TF-EpL also changed the ΔΨm and increased ROS and the number of annexin-V-PI positive promastigotes, which suggests incidental death. ß-sitosterol, ursolic acid, corosolic acid and asiatic acid were isolated from TF-EpL. The results showed the antileishmanial activity of E. pruniformis terpenoids and its potential for further studies as a source of new drugs for leishmaniasis.
Assuntos
Antiprotozoários , Eugenia , Leishmania mexicana , Leishmania , Antiprotozoários/farmacologia , Folhas de Planta , Terpenos/farmacologiaRESUMO
The chemical composition of Mangifera indica L. cv. "Kent" leaves was determined by HPLC-ESI-QTOF-MS/MS. Polyphenolic compounds characterized as benzophenone derivatives were the main components found in extracts (1, maclurin 3-C-(2-O-galloyl)-D- glucoside isomer; 2, maclurin 3-C-ï¢--D-glucoside; 3, iriflophenone 3-C-ï¢--D-glucoside; 5, maclurin 3-C-(2,3-di-O-galloyl)-ï¢--D-glucoside; 6, iriflophenone 3-C-(2-O-galloyl)-ï¢--D-glucoside; 7, methyl-iriflophenone 3-C-(2,6-di-O-galloyl)-ï¢--D-glucoside) and xanthones (4, mangiferin and 8, 6-O-galloyl-mangiferin). The estrogenic and antioxidant effects of aqueous extracts from Mangifera indica L. cv. "Kent" leaves on ovariectomized rats were determined by uterotrophic assay and malondialdehyde (MDA) levels in erythrocytes, bone, liver, and stomach. We conclude that the polyphenolic compounds from extracts act as exogenous antioxidant agents against oxidative damage in ovariectomized rats.
La composicioÌn quiÌmica de las hojas de Mangifera indica L. cv. "Kent" se determinoÌ por HPLC-ESI-QTOF-MS/MS. Compuestos polifenoÌlicos caracterizados como derivados de benzofenona fueron los componentes principales encontrados en los extractos (1, isoÌmero de la maclurina 3-C-(2-O-galoyil)-D-glucoÌsido; 2, maclurina 3-C-ß-D-glucoÌsido; 3, iriflofenona 3-C-ß-D-glucoÌsido; 5, maclurina 3-C-(2,3-di-O-galloiÌl)-ß-D-glucoÌsido; 6, iriflofenona 3-C-(2-O-galloil)-ß-D-glucoÌsido; 7, metil-iriflofenona 3-C-(2,6-di-O- galloyl)-ß-D-glucoÌsido) y xantonas (4, mangiferina y 8, 6-O-galoyil-mangiferina). Los efectos estrogeÌnicos y antioxidantes de los extractos acuosos de hojas de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas se determinaron mediante ensayo uterotroÌfico y la medicioÌn de los niveles de malondialdehiÌdo (MDA) en eritrocitos, huesos, hiÌgado y estoÌmago. Concluimos que los compuestos polifenoÌlicos de los extractos actuÌan como agentes antioxidantes exoÌgenos contra el danÌo oxidativo en ratas ovariectomizadas.
Assuntos
Animais , Feminino , Ratos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Ovariectomia , Mangifera/química , Estrogênios/farmacologia , Antioxidantes/farmacologia , Estômago/efeitos dos fármacos , Benzofenonas/química , Osso e Ossos/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Espécies Reativas de Oxigênio , Ratos Sprague-Dawley , Folhas de Planta/química , Espectrometria de Massas por Ionização por Electrospray , Etanol , Espectrometria de Massas em Tandem , Fígado/efeitos dos fármacos , Malondialdeído , Antioxidantes/químicaRESUMO
ABSTRACT Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.
Assuntos
Humanos , Fenóis/análise , Flavonoides/análise , Myrtaceae/química , Proliferação de Células/efeitos dos fármacos , Antioxidantes/farmacologia , Picratos , Compostos de Bifenilo , Brasil , Linhagem Celular Tumoral , Capacidade de Absorbância de Radicais de Oxigênio , Indicadores e Reagentes , Acetatos/farmacologia , Acetatos/químicaRESUMO
Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.