Opuntia ficus-indica (L.) Mill. fruit as source of betalains with antioxidant, cytoprotective, and anti-angiogenic properties.

The aim of this work was to investigate the phytochemical profile and biological properties of different colours of betalain cactus pear extracts, evaluating their antioxidant, cytoprotective, and anti-angiogenic properties by cell-free, cell-based, and in vivo assays. A QuEChERS extraction method followed by RP-LC-DAD-MS/MS analysis showed that indicaxanthin and betanin were the main compounds (≥94.32% and ≥96.95%, respectively). Orange cactus pear extracts exert the best antioxidant activity in all assays carried out, in particular into ORAC (17,352.55 ± 987.407 mg trolox equivalents/100 g dry weight) and ß-carotene bleaching (60.35%) assays. The red ones, instead, showed the best cytoprotective activity decreasing the cell mortality, LDH, and Caspase-3 release ranging from 4.0 to 55%. According to antioxidant results, the orange cactus pear extracts showing also the highest anti-angiogenic activity (IC50 19.31 µg/ml), followed by the red (IC50 23.55 µg/ml) and the yellow ones (IC50 33.97 µg/ml). In light of the results and correlation analysis, the behaviour of these molecules varies a lot according to their structure and physicochemical features and synergistic activity between betalain classes may be postulated; so the plant complex could be of greater interest compared with the isolated molecules for potential nutraceutical and pharmaceutical uses.

Evaluation of antioxidant, antiinflammatory, and gastroprotective properties of Rubus fruticosus L. fruit juice.

The juice of R. fruticosus (RFJ) fruits grown in Sicily was analysed for polyphenol compounds and tested to evaluate in vitro antioxidant and in vivo antiinflammatory and gastroprotective effects. RFJ, containing mainly anthocyanins, such as cyanidin derivatives, significant amounts of phenolic acids, and smaller amounts of flavonoids, showed significant antioxidant activity in DPPH (2,2-diphenyl-1-picrylhydrazyl radical) (4,147.194 ± 17.199 mg trolox equivalent [TE]/100 ml), TE antioxidant capacity (8,312.444 ± 43.055 mg TE/100 ml), ferric reducing antioxidant power (2,177.830 ± 21.015 mg TE/100 ml), oxygen radical absorbance capacity (95,377.674 ± 616.194 µmol TE/100 ml juice), and ß-carotene bleaching (72% ± 4.58) assay. In vivo studies showed that RFJ inhibit significantly the carrageenan-induced paw oedema (63-71%) in rats and possess antiinflammatory effects particularly significant in association with phenylbutazone (94-96%). In addition, RFJ pretreatment was able to prevent the ethanol-induced ulcerogenic effect in rats. All in vivo results were corroborated by histopathological observations and are in good agreement with antioxidant activity, confirming the relationships between biological effects observed and radical scavenging properties of RFJ.

Endogenous reverse transcriptase as a mediator of ursolic acid's anti-proliferative and differentiating effects in human cancer cell lines.

Ursolic acid (UA) is a pentacyclic triterpenoid compound that is widely distributed in the plant kingdom and has a broad range of biological effects. Here, we examined the effects of UA on the proliferation and differentiation of human tumor cell lines from melanoma (A375), glioblastoma (U87) and thyroid anaplastic carcinoma (ARO), and on the proliferation of a non-transformed human fibroblast cell line (WI-38). The results show that UA inhibits tumor cell proliferation in a dose- and time-dependent manner. Consistent with this finding, UA treatment promotes differentiation of all of the analyzed tumor cell lines. Interestingly, we found that UA inhibits the endogenous reverse transcriptase (RT) activity in tumor cells, which has recently been shown to be involved in the control of proliferation and differentiation of neoplastic cells. Considering these findings, we suggest that the observed anti-proliferative and differentiating effects of UA may be related to this target.

Antioxidant Phytochemicals of Opuntia ficus-indica (L.) Mill. Cladodes with Potential Anti-spasmodic Activity.

BACKGROUND: Opuntia ficus-indica (OFI) (L.) Mill. (Cactaceae), a plant widespread in dry regions of the world, shows interesting biological activities (cicatrizant, antiulcer, anti-inflammatory, and hypolipidemic) and is widely used in traditional medicine. OBJECTIVES: Phytochemical analysis and antispasmodic effect of wild OFI cladodes were carried out. MATERIAL AND METHODS: Polyphenols and Vitamin E occurrence, in antioxidant pool of OFI cladodes, were quantified by high-performance liquid chromatography. The antispasmodic effect of OFI cladodes was assessed in isolated rabbit smooth muscle tissues. The experiments were carried out with preparations of rabbit jejunum and uterus with the spontaneous contractile activity, to evaluate the effect of cumulative concentrations of the extract on basal tone, amplitude, and frequency of contractions. RESULTS: Catechin, quercetin, kaempferol, isorhamnetin and chlorogenic, ferulic, and p-coumaric acid were identified. α-, ß-, and γ-tocopherols have been highlighted and α-tocopherol is the major component. OFI cladodes contain significant amount of polyphenols and tocopherols that are effective radical scavengers and inhibited ethanol 1,1-diphenyl-2-picrylhydrazyl formation by 50%. OFI cladodes caused a light inhibition of amplitude and frequency of spontaneous contractions and a marked decrease in muscle basal tone of rabbit jejunum preparations. On spontaneously contracting uterus preparations, the addition of increasing concentrations of cladode extract caused uterine muscle relaxation. CONCLUSION: The contraction of smooth muscle preparations depends on an increase in cytoplasmic free calcium ion concentration, which activates the contractile elements. The flavonoids may suppress the contractility of smooth myocytes, by an inhibition of availability of Ca2+ for muscle contraction. SUMMARY: Opuntia ficus-indica (OFI) cladodes contain significant amount of polyphenols and tocopherols that are effective radical scavengers and inhibited ethanol 1,1-diphenyl-2-picrylhydrazyl formation by 50%Polyphenols and Vitamin E complex occurrence in OFI cladodes were characterized by high-performance liquid chromatographyOFI cladodes exhibited significative antispasmodic activity. The antispasmodic effect was assessed in isolated rabbit smooth muscle tissues. The experiments were carried out with preparations of rabbit jejunum and uterus with the spontaneous contractile activity, to evaluate the effect of cumulative concentrations of the extract on basal tone, amplitude, and frequency of contractions. Abbreviations used: OFI: Opuntia ficus-indica, DPPH: Ethanol 1,1-diphenyl-2-picrylhydrazyl.

Chemical characterization and biological effects of Sicilian Opuntia ficus indica (L.) mill. Fruit juice: antioxidant and antiulcerogenic activity.

The juice of whole fruits of Sicilian cultivars of prickly pear (Opuntia ficus indica (L.) Mill.) was investigated, and the contents of ascorbic acid, total polyphenols, and flavonoids were determined. In the juice, ferulic acid was the chief derivative of hydroxycinnamic acid and the mean concentration of total phenolic compounds was 746 microg/mL. The flavonoid fraction, analyzed by high-performance liquid chromatography-diode array detection, consisted of rutin and isorhamnetin derivatives. The juice showed antioxidant activity in the DPPH(*) test, probably due to the phenolic compounds that are effective radical scavengers. The preventive administration of the juice inhibited the ulcerogenic activity of ethanol in rat. Light microscopy observations showed an increase in mucus production and the restoration of the normal mucosal architecture. The juice is nutritionally interesting, and its dietary intake could provide protection against oxidative damage.

Chemical composition and biological activities of Calamintha officinalis Moench essential oil.

Calamintha officinalis Moench essential oil is used in cooking as an aromatic herb and also to improve the flavor and fragrance of several pharmaceutical products. The essential oil, obtained by hydrodistillation (5 mL/kg), was analyzed by gas chromatography-mass spectrometry and gas chromatography-flame ionization detection. Sixty-four components were identified, constituting 99.7% of the total oil. The major component was found to be carvone (38.7%), followed by neo-dihydrocarveol (9.9%), dihydrocarveol acetate (7.6%), dihydrocarveol (6.9%), 1,8 cineole (6.4%), cis-carvyl acetate (6.1%), and pulegone (4.1%). The essential oil showed antifungal and antimicrobial activity against Gram-positive bacteria. In addition, it presented a very low toxicity both in vivo (50% lethal dose >100 mg/kg) and in vitro in the Artemia salina test (50% lethal concentration >500 µL/mL). C. officinalis essential oil, in rodents, produces the typical effects in behavior of a nonselective central nervous system-depressant drug; it potentiates the hypnotic effects of sodium pentobarbital, decreasing the induction time and enhancing the sleeping time. Moreover, it produces a decrease in body temperature and a protection against pentylenetetrazole-induced convulsions.

Anti-inflammatory effect of lemon mucilage: in vivo and in vitro studies.

The mucilage extracted from a lemon juice centrifugation pulp was studied for its anti-inflammatory effect in rat. In vivo the lemon mucilage significantly inhibited carrageenan-induced edema in rat paw from 59% to 73.5% showing the highest effect at the third hour. In vitro, at the doses of 10(-8), 10(-6), 10(-4) or 10(-2) mg/mL the lemon mucilage stimulated the superoxide anion production in rat testing neutrophils in whole blood but inhibited it in FMLP stimulated cells at the dose of 10(-2) mg/mL. The neutrophils of rats receiving p.o. the lemon mucilage for 21 days showed a significant decrease of 45.5% in O2- generation after FMLP stimulation, and a not-significant increase after phorbol-12-myristate-13-acetate (PMA) or zymosan stimulation. Since the activity on zymosan- and PMA-induced O2- production was not significant, the inhibition exerted by FMLP in rat neutrophils occurred mainly through the blockade of phospholipase D.