Investigation of the inhibitory properties of some phenolic standards and bee products against human carbonic anhydrase I and II (original) (raw)
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Phenolic Composition and Antioxidant Properties of Anzer Bee Pollen
Journal of Food Biochemistry, 2013
Anzer honey is produced on the Anzer plateau, known for its rich flora, in the Eastern Black Sea region of Turkey. It is well known across the world, and is believed to be of high medical value. This study is the first detailed research in which the polyphenolic profiles responsible for the bioactive properties of Anzer honey was determined, melissopalynological analysis was performed, and in which total phenolic contents (TPC), total flavonoid contents (TFC), and total antioxidant activities were identified. The ferric (III) reducing antioxidant power (FRAP) assay and 1,1-diphenyl-2picrylhydrasil (DPPH) free radical scavenging test were used to determine antioxidant activity. The total mean phenolic content of Anzer honey was 26.92 GAE/100 g, and the total flavonoid content was 2.79 mgQE/100g. Anzer honeys' mean FRAP and DPPH values were 110.11 μmoLTrolox/100g and 49,12 mg/mL, respectively. The phenolic acids and flavonoids of Anzer honey were determined using highperformance liquid chromatography (HPLC). Of the 19 standard compounds used in the analysis, pinocembrin, hesperidin, chrysin, protocatechuic acid, p-coumaric acid, catechin, caffeic acid phenyl ester (CAPE), p-OH benzoic acid, and caffeic acid as major compounds, while myricetin, luteolin, rutin, resveratrol, epicatechin, t-cinnamic acid, ferulic acid, and gallic acid were identified as minor compounds. Daidzein and syringic acid were not detected. Based on these findings, Anzer is a flower honey noteworthy for the rich variety of its polyphenols.
Journal of Enzyme Inhibition and Medicinal Chemistry, 2012
Different natural products and secondary metabolites from mushrooms, teas, honeys, mosses, plants and seaweeds were investigated for their in vitro inhibitory effects on human carbonic anhydrase (hCA, E.C.4.2.1.1) isoforms I and II. Inhibition data were correlated with the total phenol content in the extract and investigated with the pure compounds believed to be responsible for this activity. Methanolic extracts were prepared for 17 such pure chemicals present in the natural products and for 41 diverse natural products. The IC 50 values were in the range of 0.11-66.50 μg/mL against hCA I and of 0.09-54.54 μg/mL against hCA II, respectively. The total phenol content was in the range of 0.02-1318.96 (as milligrams of gallic acid equivalents) per gram of sample. These data offer new insights on possible novel classes of CA inhibitors based on natural products, possessing a range of chemical structures not present in the classical inhibitors with pharmacological applications, such as the sulfonamides and sulfamates.
Chemistry & biodiversity, 2017
Plant phenolics are known to display many pharmacological activities. In the current study, eight phenolic compounds [e.g. luteolin 5-O-β-glucoside (1), methyl rosmarinate (2), apigenin (3), vicenin 2 (4), lithospermic acid (5), soyasaponin II (6), rubiadin 3-O-β-primeveroside (7), 4(3,4dihydroxybenzoyloxymethyl)phenyl-O-β-D-glucopyranoside (8)] isolated from various plant species were tested at 0.2 mM against carbonic anhydrase-II (CA-II) and urease using microtiter assays. Urease inhibition rate for compounds 1-8 ranged between 5.0 - 41.7%, while only compounds 1, 2, and 4 showed a considerable inhibition over 50% against CA-II with the IC50 values of 73.5 ± 1.05, 39.5 ± 1.14, and 104.5 ± 2.50 μM, respectively, where IC50 of the reference (acetazolamide) was 21.0 ± 0.12 μM. In silico experiments were also performed through two docking softwares (Autodock Vina and i-GEMDOCK) in order to find out interactions between the compounds and CA-II. Actually, compounds 6 (30.0%) and 7 (42.0...
Determination of Enzyme Inhibition and Antioxidant Activity in Some Chestnut Honeys
Foods and Raw materials
Honey has always been seen as the main source of healthy natural food and folk medicines. It has been prized due to bioactive components that are responsible for different therapeutic effects. Phenolic compounds are one the parts of these components. It is claimed that these have been antioxidant agents. But it also has to be evaluated by different perspectives in biomechanics except antioxidative effects. A variety of diseases may be treated by the inhibition of some individual enzymes. A pharmaceutical drug and synthetic agents are used to treat and avert illness even though there is a potential risk named drug resistance. Nowadays, the most effective treatment seems to be the combined administration of natural foods. The study aims at investigating hyaluronidase (HYA), xanthine oxidase (XOD) and the urease enzyme inhibition of some chestnut honeys from different locations of Giresun and Ordu in Turkey. Moreover, the antioxidant activities of the prepared chestnut honey extracts were investigated by using different methods. The total phenolic (TP), total flavonoid (TF), FRAP, CUPRAC assays and DPPH, and ABTS inhibition potential were carried out using in vitro models. The enzyme IC 50 values in the samples ranged from 0.793 to 12.639 mg/ml for HYA; from 0.029 to 0.106 g/ml for XO; from 0.002 to 0.054 g/ml for urease, respectively. In conclusion, honey extracts exhibited good potentials towards the inhibition of activities of the studied enzymes, and the samples also suggest a practical value for surveying natural inhibitors for specific clinical purposes. Moreover, all results can provide a basis of future studies on the alternative medicinal application related to honey.
Journal of Enzyme Inhibition and Medicinal Chemistry, 2010
Three different honey extracts from the endemic plant in the Black Sea region Rhododendron ponticum, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), more precisely the human (h) isoforms hCA I and hCA II. Hexane, methanol, ethanol, and water solid-phase extractions (SPEs) showed inhibitory activity towards the two CA isozymes which were related to the total phenolic content. The highest inhibitory effects (0.036-0.039 mg/mL) were those of propolis methanolic extract. Among the three different samples investigated here, the aqueous extracts showed lower inhibitory effects compred to the organic solvent SPE extracts (in the range of 1.150-5.144 mg/ mL). The studied honey extracts constitute an interesting source of phenolic derivatives that might serve to identify lead compounds, targeting the physiologically relevant enzymes CA I and CA II.
phytochemical screening and anitoxidant activity of bee honeys
The present study aimed at elucidating the protective role of honeys produced by the five bee species that prevail in Kerala namely, Apis cerana indica F., Apis mellifera L., Apis dorsata F., Apis florea F. and Trigona iridipennis S. in their raw and processed form against oxidative stress and free radicals. The major phytochemicals screened were polyphenols, flavonoids, and flavonols. The antioxidant potency of the honeys was analyzed using in vitro antioxidant assays namely, 2, 2 diphenyl-1-picrylhydrazyl assay and nitric oxide scavenging assay. The results indicated that the honeys in pure form were having a higher rate of antioxidant activity compared to processed honeys as processing reduce the thermolabile phytochemicals.
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Bee pollen is regarded as a valuable source of bioactive substances. Honey enrichment with bee pollen seems to be the most popular way to introduce this bee product into a human diet. The aim of this study was to determine the influence of the addition of bee pollen to honey on the content of selected biologically active pollen components, antioxidant activity, and quality parameters, as well as sensory properties. On the basis of the obtained results, it was established that enriching honey with bee pollen resulted in a significant increase in the level of phenolics, including both flavonoids and phenolic acids, of which kaempferol and gallic acid were present in the highest level. As a result of increasing addition of bee pollen, an increase in the antioxidative, antiradical, and reducing activities of honey was observed. However, the addition of bee pollen to honey resulted in the deterioration of its sensory properties. A decrease in brightness, clarity, and uniformity of color,...
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Honey is a natural product consisting of multiple components which determine its dietary and medicinal properties. Honey of different botanical origin were analyzed for in vitro antioxidant capacity and physico-chemical properties. The aim of this study was to establish relationship between non-phenolic compounds (5-hydroxymethylfurfural (HMF) and glucose oxidase (GOD)) and antioxidant capacity considering botanical origin. Antioxidant capacity was measured by the scavenging of 2.2 azino-bis-3-3 ethylbenzothiazoline-6-sulfonic acid (ABTS) radical cations. The buckwheat honey showed the highest values of antioxidant scavenging activity, the rape honey-the lowest. HMF contribution to the antioxidant capacity was tested. It had doubtful influence on the antioxidant capacity. Bee secreted compounds (enzymes, proteins, etc.) in honey also might increase antioxidant capacity: it increased strongly in light-coloured honey, and slightly-in dark-coloured honey.