Inula viscosa (L.) Aiton leaves and flower buds: Effect of extraction solvent/technique on their antioxidant ability, antimicrobial properties and phenolic profile.

This study was designed to establish the most effective solvent/technique for extracting antioxidant phytoconstituents from leaves and flower buds of Inula viscosa (L.) Aiton (Asteraceae) grown wild in Morocco. Maceration and hot extraction with methanol or water and Soxhlet ethanol extraction were utilized. The antioxidant potential was evaluated in vitro by DPPH, reducing power, and ferrous ions chelating activity assays. I. viscosa leaf and flower bud extracts displayed the strongest effect in the DPPH test, being the Soxhlet ethanol the most active ones (IC50 = 54.24 ± 0.21 µg/mL and 39.77 ± 0.23 µg/mL); thus, they were selected for further investigations. The antimicrobial efficacy of the Soxhlet ethanol extracts against ATCC and food isolates strains was assayed; the leaf extract showed the best activity, and Candida albicans was the most sensitive strain (MIC = 125 µg/mL). The extracts resulted non-toxic against Artemia salina. Among the phenolics characterised by HPLC-PDA-ESI-MS, hispidulin hexoside, patuletin and spinacetin were identified for the first time.

Phenolic composition and biological activities of Juniperus drupacea Labill. berries from Turkey.

The present study was designed to define the phenolic profile and the biological potential of berries methanol extract of Juniperus drupacea Labill. from Turkey. The total phenolic content (Folin-Ciocalteau assay) was 48.06±0.99mgGAE/g extract. The HPLC-DAD-ESI-MS analysis allowed the determination of the complete phenolic profile of J. drupacea berries. Phenolic acids represented more than 60% of the total phenolics, and tyrosol was the major one (1324±0.64µg/g extract); within the flavonoids amentoflavone was detected as the main constituent (927±0.35µg/g extract). The extract exhibited good antioxidant properties, as determined by different in vitro models: DPPH test (IC(50) 0.38±0.02mg/mL), reducing power (12.63±0.14ASE/mL), Fe(2+) chelating ability (IC(50) 2.26±0.06mg/mL), and TBA test (IC(50) 2.47±1.13µg/mL). Cytotoxicity against Artemia salina was highlighted (LC(50) 489.47±27.8µg/mL), and a significant decrease (p⩽0.05; p⩽0.01) in HepG2 cells viability was observed at the higher concentrations (5-10µg/mL). The extract displayed good antibacterial activity towards Gram-positive bacteria and in particular Staphylococcus aureus was the most susceptible strain (MIC 78.12µg/mL).

Antiinflammatory and antioxidant activity of Hypericum rumeliacum Boiss. subsp. apollinis (Boiss. & Heldr.) Robson & Strid methanol extract.

Plants of the genus Hypericum are widely used in folk medicine for the treatment of gastric ailments (including pectic ulcers), burns, swelling, inflammation, anxiety, as well as for bacterial and viral infections. The aerial parts of Hypericum rumeliacum Boiss. subsp. apollinis (Boiss. & Heldr.) Robson & Strid (Guttiferae), a perennial herb growing wild in Greece, were subjected to biological and phytochemical studies. The H. rumeliacum methanol extract showed, on the DPPH test, antioxidant activity (IC(50) = 23.61 microg/mL). The antiinflammatory activity of the extract (70 mg/kg, i.p.), in the carrageenan-induced paw oedema in rat, was studied. In this experimental model an inhibition of paw oedema, significant from the first to third hour, was observed. The histological examination confirmed resolution of the inflammatory process observed in vivo. Through HPLC analysis of the H. rumeliacum methanol extract, the naphthodianthrones hypericin, pseudohypericin and some polyphenol compounds, such as chlorogenic acid, rutin and isoquercitrin, were identified and quantified. The antioxidant activity of H. rumeliacum could be chiefly related to polyphenol compounds that are well known as the main contributors to the free radical-scavenging effects. The antiinflammatory effect of the methanol extract of the aerial parts could be due to the synergic action both of hypericin and polyphenol compounds.

Ursolic acid plays a role in Nepeta sibthorpii Bentham CNS depressing effects.

The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing test and the hot plate test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the hot plate test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the hot plate test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound.

Opuntia ficus indica (L.) Mill. mucilages show cytoprotective effect on gastric mucosa in rat.

Opuntia ficus indica cladodes possess a protective action against ethanol-induced ulcer in the rat. The major components of cladodes are carbohydrate polymers, mainly mucilages and pectin. To clarify the cytoprotective effects of cladodes on experimental ethanol-induced ulcer in rat, mucilages and pectin were extracted and were administered instead of cladodes. The above mentioned effects induced by cladodes may be attributed to mucilages, and not significantly to pectin.

Opuntia ficus indica (L.) Mill. fruit juice protects liver from carbon tetrachloride-induced injury.

The protective effects of the juice of Opuntia ficus indica fruit (prickly pear) against carbon tetrachloride (CCl(4))-induced hepatotoxicity were examined in rats. The animals were treated orally with the juice (3 mL/rat) 2 h after administration of the hepatotoxic agent. Preventive effects were studied by giving the juice (3 mL/rat) for 9 consecutive days. On day 9 the rats received the hepatotoxic agent. Morphological and biochemical evaluations were carried out 24, 48 and 72 h after induction of the hepatic damage. Data show that O. ficus indica fruit juice administration exerts protective and curative effects against the CCl(4)-induced degenerative process in rat liver. Histology evaluation revealed a normal hepatic parenchyma at 48 h; the injury was fully restored after 72 h. Moreover, a significant reduction in CCl(4)-induced increase of GOT and GPT plasma levels is evident; these data are in agreement with the functional improvement of hepatocytes. O. ficus indica fruit juice contains many phenol compounds, ascorbic acid, betalains, betacyanins, and a flavonoid fraction, which consists mainly of rutin and isorhamnetin derivatives. Hepatoprotection may be related to the flavonoid fraction of the juice, but other compounds, such as vitamin C and betalains could, synergistically, counteract many degenerative processes by means of their antioxidant activity.

Anti-inflammatory activity of extract and fractions from Nepeta sibthorpii Bentham.

Several species of Nepeta genus are utilized in folk medicine for treatment of contusions, rheumatic pains, fever, cutaneous eruptions. Some species are employed for their anti-inflammatory properties. In this paper, we report the results of phytochemical studies on aerial parts of Nepeta sibthorpii Bentham (Lamiaceae), an endemic plant of Greece. The bioassay-guided fractionation of methanol extract led to the isolation of ursolic acid and polyphenol fraction. By HPLC, we determined some phenolics: chlorogenic acid (0.315 mg/g) and the flavonoids rutin (0.091 mg/g), luteolin-7-O-glucoside (0.387 mg/g) and a luteolin derivative. We assayed the radical scavenging activity of Nepeta sibthorpii methanol extract by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. Moreover, we studied the anti-inflammatory activity of Nepeta sibthorpii methanol extract (50 mg/kg, os), ursolic acid and polyphenol fraction (dose corresponding to 50 mg/kg of methanol extract, os) in the carrageenan-induced paw oedema in rat. In this experimental model, we observed a significant inhibition of paw oedema. We suppose that the anti-inflammatory effect of methanol extract could be related to the free radical scavenging activity and that it depends on a synergic action of all the components of the methanol extract, even if ursolic acid can be considered the main responsible for this activity.

Chiral 3,3'-(1,2-ethanediyl)-bis[2-(3,4-dimethoxyphenyl)-4-thiazolidinones] with anti-inflammatory activity. Part 11: evaluation of COX-2 selectivity and modelling.

Anti-inflammatory/analgesic 3,3'-(1,2-ethanediyl)-bis[2-(3,4-dimethoxyphenyl)-4-thiazolidinones] 1, obtained as racemic mixtures (a) and mesoforms (b), have two equivalent stereogenic centres (C-2 and C-2') and exist as RR, SS and RS isomers. The enantioseparation of 1a provided the single enantiomers that displayed different in vitro cyclooxygenase-1/cyclooxygenase-2 selectivity ratios. In particular the dextrorotatory compound is a highly selective COX-2 inhibitor and the levorotatory one is moderately selective. Instead, RS-meso isomer (1b) exhibited similar levels of inhibitory activity on both COX isozymes. The diastereo- and enantioselectivity has been explained by molecular modelling of RR, SS and RS compounds into COX-1 and COX-2 binding sites. Theoretical results indicated SS>RS>RR affinity order towards COX-2 isoenzyme, in agreement with in vitro and previous in vivo pharmacological results.

Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10.

In this note, the synthesis and structure-activity relationships of a new series of 2R,2'R/2S,2'S and 2R,2'S-meso 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinones] are described. Antiinflammatory activity was investigated by the carrageenin-induced paw edema test and analgesic activity by acetic acid writhing and hot plate tests in rats. All compounds displayed ulcerogenic effects and acute toxicity much lower than indomethacin and phenylbutazone. Meso isomers (b) showed better pharmacological profiles than corresponding racemates (a). Methoxy substitution patterns of the aryls on stereogenic carbons are generally the most favorable on the pharmacological profile.

Anti-inflammatory and analgesic activity of Hypericum empetrifolium Willd. (Guttiferae).

A methanolic extract of Hypericum empetrifolium Willd. was evaluated for anti-inflammatory properties in rats (subplantar edema induced by carrageenan) and analgesic effects in mice (hot plate and writhing tests). Our results showed that the methanolic extract exhibits a significant anti-inflammatory activity and analgesic effects only in one of the experimental models (writhing test). Therefore, we may suppose that the methanolic extract of H. empetrifolium is active against inflammatory pain.