Background: The phytochemical composition, antioxidant, cytotoxic, and antimicrobial activities of a methanol extract from Glycyrrhiza glabra L. (Ge), a 50% ethanol (in water) extract from Paeonia lactiflora Pall. (Pe), and a 96% ethanol extract from Eriobotrya japonica (Thunb.) Lindl. (Ue) were investigated. Methods: The phytochemical profiles of the extracts were analyzed by LC-MS/MS. Antioxidant activity was evaluated by scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals and reducing ferric complexes, and the total phenolic content was tested with the Folin–Ciocalteu method. Cytotoxicity was determined with a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in murine macrophage RAW 264.7 cells. Antimicrobial activity of the three plant extracts was investigated against six bacterial strains with the broth microdilution method. Results: Only Pe showed high antioxidant activities compared to the positive controls ascorbic acid and (−)-epigallocatechin gallate (EGCG) in DPPH assay; and generally the antioxidant activity order was ascorbic acid or EGCG > Pe > Ue > Ge. The three plant extracts did not show strong cytotoxicity against RAW 264.7 cells after 24 h treatment with IC50 values above 60.53 ± 4.03 μg/mL. Ue was not toxic against the six tested bacterial strains, with minimal inhibitory concentration (MIC) values above 5 mg/mL. Ge showed medium antibacterial activity against Acinetobacter bohemicus, Kocuria kristinae, Micrococcus luteus, Staphylococcus auricularis, and Bacillus megaterium with MICs between 0.31 and 1.25 mg/mL. Pe inhibited the growth of Acinetobacter bohemicus, Micrococcus luteus, and Bacillus megaterium at a MIC of 0.08 mg/mL. Conclusions: The three extracts were low-cytotoxic, but Pe exhibited effective DPPH radical scavenging ability and good antibacterial activity; Ue did not show antioxidant or antibacterial activity; Ge had no antioxidant potential, but medium antibacterial ability against five bacteria strains. Pe and Ge could be further studied for their potential to be developed as antioxidant or antibacterial candidates.
Alzheimerʼs disease is a rising threat for modern societies as more and more people reach old age. To date, there is no effective treatment for this condition. In this study, we investigated the potential of Glycyrrhiza uralensis to counteract amyloid-β toxicity, one of the key features of Alzheimerʼs disease. An LC-MS/MS analysis revealed glycyrrhizic acid and glycosylated forms of isoliquiritigenin and liquiritigenin as major constituents of water and methanol extracts of G. uralensis. These extracts and the pure compounds were tested for their activity in two Caenorhabditis elegans models of amyloid-β aggregation and amyloid-β toxicity, respectively. The number of amyloid-β aggregates decreased by 30 % after treatment with isoliquiritigenin, the methanol extract could reduce the number by 14 %, liquiritigenin and glycyrrhizic acid by 15 %, and the aglycon of glycyrrhizic acid, glycyrrhetinic acid, by 20 %. Both extracts and isoliquiritigenin also showed significant activity against acute amyloid-β toxicity in transgenic C. elegans that express human amyloid-β peptides, delaying the paralysis in this model by 1.8 h and 1.1 h, respectively. We conclude that secondary compounds of G. uralensis may become interesting drug candidates for the treatment of Alzheimerʼs disease, which, however, need further analysis in other model systems.
Carlina acaulis is a medicinal plant that has shown antioxidant activity in in vitro studies, but to date no corresponding in vivo data is available. Therefore, in the present study the antioxidant activity and its impact in counteracting Aβ toxicity were studied in the Caenorhabditis elegans model. A dichloromethane extract of the roots of C. acaulis was prepared and characterised via gas-liquid-chromatography/mass-spectrometry (GLC-MS). The in vitro antioxidant activity was confirmed via 2,2-diphenyl-1-picrylhydracyl assay. The extract was further separated by thin layer chromatography into two fractions, one of which was a fraction of the dichloromethane extract of C. acaulis containing mostly Carlina oxide (CarOx). Different strains of C. elegans were employed to study the expression of hsp-16.2p::GFP as a marker for oxidative stress, delocalisation of the transcription factor DAF-16 as a possible mechanism of antioxidant activity, the effect of the drug under lethal oxidative stress, and the effect against beta-amyloid (Aβ) toxicity in a paralysis assay. The C. acaulis extract and CarOx showed high antioxidant activity (stress reduction by 47% and 64%, respectively) in C. elegans and could activate the transcription factor DAF-16 which directs the expression of anti-stress genes. In paralysis assay, only the total extract was significantly active, delaying paralysis by 1.6 h. In conclusion, in vivo antioxidant activity was shown for C. acaulis for the first time in the C. elegans model. The active antioxidant compound is Carlina oxide. This activity, however, is not sufficient to counteract Aβ toxicity. Other mechanisms and possibly other active compounds are involved in this effect.
In a context of rising demand for sustainable antiaging interventions, fruit processing by-products are a promising source of bioactive compounds for the production of antiaging dietary supplements. Piquiá (Caryocar villosum) is a native Amazonian fruit consisting of 65% nonedible shells. In the present study, the phytochemical profile of a hydroalcoholic extract of piquiá shells (CV) was characterized by LC-MS/MS analysis. Its antioxidant and antiaging activities were investigated using the nematode Caenorhabditis elegans as an in vivo model. CV is mainly composed by hydrolysable tannins and triterpenoid saponins. The extract enhanced stress resistance of wild-type and mutant worms by reducing the intracellular levels of reactive oxygen species (ROS) and by increasing their survival against a lethal dose of the prooxidant juglone. These effects involved the upregulation of sod-3 and downregulation of gst-4 and hsp-16.2, studied through the GFP fluorescent reporter intensity and at the transcriptional level by qRT-PCR analysis. CV extended the lifespan of wild-type worms in a DAF-16/FoxO- and SKN-1/Nrf-dependent manner. Taken together, our findings indicate piquiá shells as potential candidates for nutraceutical applications. Further studies are needed to validate the relevance of our findings to antiaging interventions in humans.
Drosophila suzukii (Diptera: Drosophilidae), is native to southeastern Asia and invaded Europe during the past decade. It causes serious economic damage in cherries and soft fruits. Control strategies rely on few insecticides with varying success. Due to environmental concern, the use of synthetic chemicals is restricted. Therefore, research effort is put into the quest for alternative substances applicable in chemical pest control. In laboratory assays, we tested 17 volatile plant compounds from different chemical classes for their contact toxicity, feeding modification, and oviposition repellency. Toxicity through contact with treated surfaces was evaluated after 1 h, 4 h, and 24 h; effects on food uptake were observed with capillary feeding (CAFE)—tests and oviposition trials compared egg numbers laid in raspberry medium with or without treated filter paper. Cinnamon oil and its components had the highest contact toxicity with an LC90 = 2–3%, whereas lemongrass oil, its main components, and farnesol were less toxic (LC90 = 7–9%), and geraniol was the least toxic. In CAFE tests, feeding stimulation was observed through 0.1% and 1% solutions of citronellol, lemongrass oil and farnesol. Cinnamon oil, cinnamaldhyde, and ethyl cinnamate were not consumed at a concentration of 1%. In the presence of citral, eugenol, and lemongrass oil, oviposition was reduced, and in the presence of limonene, no eggs were deposited. The natural products found most efficient in either bioassay will be further tested under field conditions.