Chemical composition and protective effect of oregano (Origanum heracleoticum L.) ethanolic extract on oxidative damage and on inhibition of NO in LPS-stimulated RAW 264.7 macrophages.

The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid content, showed a significant radical-scavenging activity (IC(50) value of 12.8 μg/mL) using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) test and an interesting antioxidant activity with the β-carotene bleaching test (IC(50) values of 12.9 and 14.1 μg/mL at 30 and 60 min of incubation, respectively). The test for the inhibition of NO production, performed using the murine monocytic macrophage RAW 264.7 cell line, showed that the extract had significant activity with an IC(50) value of 108.5 μg/mL. The cytotoxic effect of O. heracleoticum extract in presence of lipopolysaccharide (LPS) (1 μg/mL) was evaluated but found to be negligible

Natural Products as Gastroprotective and Antiulcer Agents: Recent Developments:

Peptic ulcer, one of the most common gastrointestinal diseases, is a chronic inflammatory disease characterized by ulceration in the regions of the upper gastrointestinal tract where parietal cells are found and where they secrete hydrochloric acid and pepsin. The anatomical sites where ulcer occurs commonly are stomach and duodenum, causing gastric and duodenal ulcer, respectively. Physiopathology of ulcer is due to an imbalance between aggressive factors, such as acid, pepsin, Helicobacter pylori and non-steroidal anti-inflammatory agents, and local mucosal defensive factors, such as mucus bicarbonate, blood flow and prostaglandins. Several drugs are widely used to prevent or treat gastro-duodenal ulcers. These include H2-receptor antagonists, proton pump inhibitors and cytoprotectives. Due to problems associated with recurrence after treatment, there is therefore the need to seek alternative drug sources against ulcers. In recent years, a widespread search has been launched to identify new gastroprotective drugs from natural sources. The aim of the present review is to highlight the recent advances in current knowledge on natural products as gastroprotective and antiulcer agents and consider the future perspectives for the use of these compounds

Quantitative determination of Amaryllidaceae alkaloids from Galanthus reginae-olgae subsp. vernalis and in vitro activities relevant for neurodegenerative diseases.

In the present work the qualitative and quantitative analysis of Amaryllidaceae-type alkaloids in the aerial parts and bulbs of Galanthus reginae-olgae Orph. subsp. vernalis Kamari is presented for the first time using GC-MS analysis. The alkaloids galanthamine, lycorine, and tazettine were identified in both extracts while crinine and neronine were found only in the bulbs. The yield of alkaloid fraction from bulbs (36.8%) is very high compared to the yield from aerial parts (9.34%). Lycorine was the major component in both fractions. The antioxidant potential was determined by three complementary methods. The preparations to reduce the stable free radical DPPH to the yellow-colored 1,1-diphenyl-2-picrylhydrazyl with IC(50) values of 39 and 29 mug/mL for MeOH extracts from aerial parts and bulbs, respectively. The higher activity was given by EtOAc fraction of aerial parts with IC(50) of 10 mug/mL. This activity is probably due to the presence in EtOAc fraction of polar compounds such as polyphenols. The fraction exhibited a significant antioxidant capacity also in the beta-carotene-linoleic acid test system. A higher level of antioxidant activity was observed for EtOAc fraction from bulbs with IC(50) of 10 mug/mL after 30 min and 9 mug/mL after 60 min of incubation. In contrast, the fraction from bulbs performed poorly in the lipid peroxidation liposomes assay. Significant activity was obtained for dichloromethane fraction from aerial parts (IC(50) of 74 mug/mL). The major abundance of alkaloid in dichloromethane fraction may be responsible of the bulbs anti-cholinesterase highest activity (38.5%) at 0.5 mg/mL

Antioxidant and anti-cholinesterase activity of Globularia meridionalis extracts and isolated constituents.

The antioxidant and anti-cholinesterase properties of Globularia meridional (Podp.) O. Schwarz (Globulariaceae) were investigated. G. meridionalis aerial parts and roots were extracted with methanol, and the total extract successively partitioned with n-hexane. The methanol fraction of the roots showed the highest antioxidant activity with IC50 values of 8.0 and 2.1 μg/mL in the DPPH and β-carotene bleaching tests, respectively. From this fraction, three flavonoids, namely pectolinarigenin 7- O-β-glucoside, apigenin 7- O-β-glucoside and luteolin, and two phenylethanoids, namely acteoside and isoacteoside, were isolated. Potential anti-cholinesterase effects were assessed through the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes inhibition assay. The n-hexane fraction of the roots exhibited the highest activity against both AChE and BChE with IC50 values of 65.5 and 70.4 μg/mL, respectively

Acetyl-cholinesterase Inhibition by Extracts and Isolated Flavones from Linaria reflexa Desf. (Scrophulariaceae):

Extracts, linariin, isolinariin A and B obtained from Linaria reflexa Desf. (Scrophulariaceae) were tested for acetylcholinesterase inhibition activity using Ellman's method. A dose-response relationship was observed for all extracts and isolated compounds. Flavones exhibited IC50 values ranging from 0.27 μM to 0.30 μM. The structure-activity relationship was briefly discussed

Protective effect of Hypericum calabricum Sprengel on oxidative damage and its inhibition of nitric oxide in lipopolysaccharide-stimulated RAW 264.7 macrophages

The present study shows for the fi rst time the phenolic composition and the in vitro properties (antioxidant and inhibition of nitric oxide production) of Hypericum calabricum Sprengel collected in Italy. The content of hypericins (hypericin and pseudohypericin), hyperforin, fl avonoids (rutin, hyperoside, isoquercetrin, quercitrin, quercetin and biapigenin) and chlorogenic acid of H. calabricum, have been determined. The ethyl acetate fraction from the aerial parts of H. calabricum exhibited activity against the radical 1,1-diphenyl-2picrylhydrazyl (DPPH) with IC 50 value of 1.6 μg/ml. The test for inhibition of nitric oxide (NO) production was performed using the murine monocytic macrophage cell line RAW 264.7. The ethyl acetate fraction had signifi cant activity with an IC 50 value of 102 μg/ml and this might indicate that it would have an anti-infl ammatory effect in vivo

Estrazione ed identificazione di principi biologicamente attivi da piante endemiche

Dottorato di Ricerca in: Ambiente, Salute e Processi Ecosostenibili, Ciclo XXII, a.a. 2009Università della Calabria

Changes in the phenolic and lipophilic composition, in the enzyme inhibition and antiproliferative activity of Ficus carica L. cultivar Dottato fruits during maturation

Fruits of Ficus carica cultivar Dottato from Italy were examined to assess how the stage of ripeness influences their chemical composition, antioxidant activity, pancreatic lipase inhibition and antiproliferative properties on C32 melanoma cells. Fruits of the first harvest (June) showed a major content in furanocoumarins and pyranocoumarins whereas the fruits collected in September showed the highest polyphenolic content (11.9mg/g of dried material). The total 70% ethanol extracts were portioned between methanol/water and n-hexane, dichloromethane and ethyl acetate, successively. Coumarins and fatty acid esters were the most abundant components of the n-hexane fractions. The dichloromethane fractions showed as major components 2 furanocoumarins (rutarenin and pimpinellin). The total extracts of F. carica cv. Dottato exhibited a significant dose-dependent antiradical and inhibition of lipid peroxidation activity, particularly fruits of the first harvest (June) that showed the highest activity with IC 50 of 1.64mg/mL and 0.004mg/mL, respectively. Among single fractions, the ethyl acetate fraction from the second harvest (July) showed the highest antiradical activity with an IC 50 value of 0.05mg/mL while the dichloromethane fraction showed the best inhibition of lipid peroxidation with an IC 50 value of 0.02mg/mL. Dichloromethane fractions showed the highest photodynamic cytotoxicity with an IC 50<5μg/mL. © 2012 Elsevier Ltd.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

Protection against neurodegenerative diseases of Iris pseudopumila extracts and their constituents

The present study describes for the first time the in vitro properties of Iris pseudopumila flowers and rhizomes extracts and their constituents. The methanolic extract of rhizomes showed significant anti-inflammatory activity through inhibition of NO production in the murine monocytic macrophage cell line RAW 264.7. Among the isolated compounds, those which most effectively inhibited LPS-induced NO production were irisolidone and 7-methyl-tectorigenin-4′-O-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside], with IC50 values of 23.6 μM and 29.4 μM respectively. Isoorientin and isovitexin exhibited the most promising activity against AChE with IC50 of 26.8 μM and 36.4 μM, respectively. The same compounds exhibited also the higher activity against BChE