This study describes the isolation and identifi cation of apigenin-7-O-glucopyranoside, a fl avonoid isolated from the fl owers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The fl avonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.
Acute toxicity, antioxidant activity in vitro and general pharmacological effects of the fl ower crude ethanolic extract of Bellis perennis L., Asteraceae, a popular medicine used in South America, were investigated in mice. The oral route LD50 value was found 2.31 g/kg. Oral administration at doses 50, 100 and 150 mg/ kg of the extract neither caused significant changes in general behavior nor led to toxic symptoms. Anxiolytic-like properties were studied in the open fi eld test and the possible antidepressant-like actions were evaluated in the forced swimming test (FST). There is a signifi cant decrease in the number of crossings at all dosages mentioned above, but no sedative effects at any dosages when compared to controls. In the FST, the extract dosage of 150 mg/kg was effective in reducing immobility, along with a signifi cant increase in swimming time. The ethanolic extract showed strong antioxidant potential in vitro, through the removal capacity against hydroxyl radicals and nitric oxide as well as prevented the formation of reactive substances to thiobarbituric acid (TBARS). Together, these results indicate that the ethanolic extract has effect on central nervous system, which might due to its antioxidant property, as demonstrated in vitro methods used. These results suggest that some of the components in ethanolic extract of B. perennis, such as alkaloids, phenolic compounds and fl avonoids may have antioxidant, anxiolytic and antidepressant-like properties. Additional investigations are in progress.
This paper describes the anticholinesterase and antioxidant activities of Eugenia dysenterica DC. (O.Berg. (Myrtaceae) essential oils from leaves (EOED). EOED were obtained by hydrodistillation using a Clevenger-type apparatus and the products were analyzed by gas chromatography-mass spectrometry (GC-MS) and gas chromatography-flame ionization detector (GC-FID). The main constituents of EOED were caryophyllene oxide (66.3%), isoledene (3.9%), 1,3,8-p-menthatriene (3.5%), mustakone (3.46%), β-phellandrene (1.7%), and selin-11-en-4-α-ol (1.7%). The antioxidant assay was performed based on the formation of thiobarbituric acid reactive substances (TBARS), hydroxyl radical, and nitric oxide production. By performing the Ellman assay, it was observed that EOED was able to inhibit the enzyme acetylcholinesterase (AChE) with an IC 50 = 0.92 g.ml -1 promising better value when compared with the drug rivastigmine (IC 50 = 1.87 g.ml , it was found out that EOED prevented lipid peroxidation inhibiting amount of TBARS formed in a similar manner to ascorbic acid. In addition, there was a reduction in the production of hydroxyl radical as well as the production of nitric oxide. To the best of our knowledge, this is the first report on compounds from this species that have activity for potentially preventing neurodegenerative disorders.
The antioxidant and anti-inflammatory properties of Citrus flavonoids can play a key role in their activity against several degenerative diseases and particularly brain diseases. In Brazil promising studies deposited in the patents "pharmaceutical formulation" form was obtained from the inclusion of Citrus sinensis L. (orange) essential oil with β-cyclodextrin and Citrus limon (lemon) compounds and their applications in therapy of Alzheimer's disease. In this chapter, we report activities of active compounds present in the genus Citrus, which include antioxidant, anti-inflammatory, anxiolytic, insecticidal, and anticholinesterase activities. These activities are associated with some neurodegenerative diseases such as Alzheimer's disease (AD). Pharmaceutical formulations containing such compounds (for example, inhibitors such as acetylcholinesterase (AChE) of C. limon (5,8-dimethoxy-psoralen and 5,7-dimethoxycumarin) and essential oil from C. sinensis oils are reported in this chapter. These results indicate that the effects of the essential oil and substances of Citrus species are very interesting for further isolation of AChE inhibitors that can be used in the formulation of natural products for neurodegenerative diseases.
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