RESUMO
As the safety and effectiveness of synthetic drugs remain in doubt, researchers are trying to develop natural medicines from medicinal plants. Herein, ethyl acetate, methanol and water extracts from the Heracleum humile plant were obtained by an ultrasonic-assisted extraction process and the aim was to evaluate some biological effects of the extracts due to the limited data on the pharmacological properties of Heracleum humile in the literature. Weak antibacterial activity was observed on tested bacterial species. The minimum inhibitory concentration and the minimum bactericidal concentration values ranged from 250 to 500â µg/mL. In addition, cytotoxic activity was determined using the MTT test. The strongest findings were determined for ethyl acetate extract on the MDA-MB-231 cell lines at the 48th â hour (IC50 :97.94â µg/mL), followed by the MCF-7 cell lines at the 24th â hour (IC50 :103.9â µg/mL). All extracts of Heracleum humile contained mainly flavonoids, phenolic acids and their derivatives, i. e., well-known compounds that possess numerous biological activities such as antioxidant, anti-inflammatory, anticancer, antimicrobial etc. The study results could provide important information that Heracleum humile could be a potential candidate as a natural enzyme inhibitor. It can be concluded that these extracts could be useful in the elementary step of improving novel plant-derived multifunctional pharmaceuticals.
Assuntos
Heracleum , Magnoliopsida , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Flavonoides/farmacologia , Testes de Sensibilidade Microbiana , Extratos Vegetais/farmacologiaRESUMO
Salvia species have been traditionally used to improve cognition and have been proved to be a potential natural treatment for Alzheimer's disease. Salvia fruticosa Mill. (Turkish sage or Greek sage) demonstrated to have anticholinergic effects in vitro. The aim of this study was to understand the mechanism underlying the neuroprotective effects of S. fruticosa infusion and its representative compound rosmarinic acid, which was detected by LC-DAD-ESI-MS/MS. The protective effects of the S. fruticosa infusion (SFINF) and its major substance rosmarinic acid (RA) on amyloid beta 1-42 -induced cytotoxicity on SH-SY5Y cells together with p-GSK-3ß activation were investigated. Their in vitro inhibitory effects against glycogen synthase kinase 3ß, ß-secretase, and casein kinase 1δ enzymes were also evaluated. The results showed that treatment with the all tested concentrations, SFINF significantly decreased Aß 1-42-induced cytotoxicity and exhibited promising in vitro glycogen synthase kinase 3ß inhibitory activity below 10 µg/mL (IC50 6.52 ± 1.14 µg/mL), in addition to ß-secretase inhibition (IC50 86 ± 2.9 µg/mL) and casein kinase 1δ inhibition (IC50 121.57 ± 4.00). The SFINF (100 µg/mL and 250 µg/mL) also activated the expression of p-GSK-3ß in amyloid beta 1-42 treated SH-SY5Y cells. The outcomes of this study demonstrated that the S. fruticosa infusion possessed activity to prevent amyloid beta 1-42 -induced neurotoxicity and provided proof that its mechanism may involve regulation of p-GSK-3ß protein.
RESUMO
Seseli L. is one of the largest genera of the Apiaceae family widely known for their traditional uses as herbal remedies. In the present study, the methanolic and water extracts of two Seseli species, S. gummiferum and S. transcaucasicum were evaluated for their bioactive contents and biological activities. The total phenolic and flavonoid contents in the extracts ranged from 19.09 to 24.33 mg GAE/g and from 0.45 to10.09 mg RE/g, respectively. Moreover, while narcissin was detected as the most abundant component in the methanolic extract of S. transcaucasicum (261.40 µg/g), chlorogenic acid was identified as the major component in all the other extracts, although a high amount was also present in the methanolic S. transcaucasicum extract (107.48-243.12 µg/g). The total antioxidant capacity was also determined by the phosphomolybdenum assay (0.66-1.18 mM TE/g). Other antioxidant assays such as the radical scavenging assays (DPPH: 5.51-11.45 mg TE/g; ABTS: 43.46-51.91 mg TE/g), reducing assays (CUPRAC: 41.67-53.20 mg TE/g; FRAP: 31.26-34.14 mg TE/g), as well as the metal chelating activity assay (14.38-38.57 mg EDTAE/g) were conducted. All the extracts showed inhibitory potential against the enzyme's amylase (0.12-0.78 mM ACAE/g), acetyl- and butyryl-cholinesterase (0.15-9.71 mg GALAE/g), while only the methanolic extracts acted as inhibitors of tyrosinase (107.15 and 109.37 mg KAE/g) and only the water extract of S. gummiferum displayed anti-glucosidase activity (0.13 mM ACAE/g). Interestingly, the methanolic extracts of both Seseli species showed lower cytotoxicity towards HaCaT cells (IC50: >500 µg/mL), compared to the water extracts (IC50: 267.8 and 321.41 µg/mL). Besides, only the methanolic extracts showed a slight wound healing effect (28.21 and 31.23%). All extracts showed antibacterial action against Staphylococcus lugdunensis (minimum inhibitory and bactericidal concentrations: 0.025-2 mg/mL). S. gummiferum methanolic extract, which exhibited the highest antibacterial potency was found to inhibit adhesion and invasion of S. lugdunensis to HaCaT cells as well. Taken together, this study demonstrated the two Seseli species to harbour interesting bioactive components, in particular polyphenolics and to exhibit several biological properties that could be further investigated for their potential exploitation as healing agents as supported by various traditional medicinal uses.
RESUMO
This study presents the evaluation of biological activities and chemical profiling of Oenanthe aquatica (L.) Poir. and Oenanthe silaifolia M. Bieb. The phytochemical profile, antioxidant, enzyme inhibitory, cytotoxic and antiviral activities of the methanolic and aqueous extracts were investigated. The aqueous extract of O. aquatica possessing the highest content of phenolics (60.85 mg gallic acid equivalent/g extract), also exhibited the strongest radical scavenging potential against 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (79.46 and 148.66 mg Trolox equivalent/g extract, respectively), the highest reducing ability (207.59 and 107.27 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant activity, respectively), metal chelating potential (33.91 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant ability (1.60 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) permitted tentative identification of compounds from simple organic acids, phenolic acids, coumarins, flavonoids and their glycosides in O. aquatica and O. silaifolia extracts. The methanolic extract of O. aquatica substantially depressed acetylcholinesterase (3.67 mg galantamine equivalent/g extract), tyrosinase (126.66 mg kojic acid equivalent/g extract), and α-amylase (0.83 mmol acarbose equivalent/g extract) enzymes. The methanolic extract of O. silaifolia showed highest enzymatic inhibitory property against butyrylcholinesterase, and its aqueous extract depressed α-glucosidase activity (0.26 mmol acarbose equivalent/g extract). All tested extracts exerted selective toxicity towards cancer cell lines, and the highest anticancer potential was found for O. aquatica aqueous extract on FaDu and HeLa cells with CC50 of 57.36 and 47.16 µg/mL, respectively. Significant antiviral activity against HSV-1 (HHV-1) was found for both aqueous extracts in concentrations of 1000 µg/mL, which inhibited the HSV-1 cytopathic effect (CPE) in virus infected VERO cells and reduced the virus infective titer by more than 3 log (logCCID50/mL). This study has produced critical scientific data on O. aquatica and O. silaifolia, which are potential contenders for the development of novel phyto-pharmaceuticals.
RESUMO
Bunium species have been reported to be used both as food and in traditional medicines. The scientific community has attempted to probe into the pharmacological and chemical profiles of this genus. Nonetheless, many species have not been investigated fully to date. In this study, we determined the phenolic components, antimicrobial, antioxidant, and enzyme inhibitory activities of aerial parts of four Bunium species (B. sayai, B. pinnatifolium, B. brachyactis and B. macrocarpum). Results showed that B. microcarpum and B. pinnatifolium were strong antioxidants as evidenced in the DPPH, ABTS, CUPRAC, and FRAP assays. B. brachyactis was the most effective metal chelator, and displayed high enzyme inhibition against cholinesterase, tyrosinase, amylase, glucosidase, and lipase. The four species showed varied antimicrobial activity against each microorganism. Overall, they showed high activity against P. mirabilis and E. coli (MIC and MBC <1â¯mg mL-1). B. brachyactis was more effective against Aspergillus versicolor compared to the standard drug ketoconazole. B. brachyactis was also more effective than both ketoconazole and bifonazole against Trichoderma viride. B. sayai was more effective than ketoconazole in inhibiting A. fumigatus. B. sayai was most non-toxic to HEK 293 (cellular viabilityâ¯=â¯117%) and HepG2 (cellular viabilityâ¯=â¯104%). The highest level of TPC was observed in B. pinnatifolium (35.94â¯mg GAE g-1) while B. microcarpum possessed the highest TFC (39.21 mg RE g-1). Seventy four compounds were detected in B. microcarpum, 70 in B. brachyactis, 66 in B. sayai, and 51 in B. pinnatifolium. Quinic acid, chlorogenic acid, pantothenic acid, esculin, isoquercitrin, rutin, apigenin, and scopoletin were present in all the four species. This study showed that the four Bunium species are good sources of biologically active compounds with pharmaceutical and nutraceutical potential.