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Biomedical subjects

Ivano Morelli

Publications and source records attributed to Ivano Morelli.

At least 37 records · Page 2Linked to original sources

Vasodilator activity of Michelia figo Spreng. (Magnoliaceae) by in vitro functional study.

The methanolic extract of leaves of Michelia figo Spreng. (Magnoliaceae), as well as several purified fractions, showed a concentration-dependent vasorelaxing effect on aortic rings endothelium-deprived and pre-contracted by norepinephrine (NE). For further pharmacological investigation on the mechanism of action, the fraction S4 was selected, since it showed the best vasodilator properties. The pharmacological effect was not produced through the stimulation of cyclooxygenase, adenyl cyclase, or guanylyl cyclase, since selective inhibitors did not prevent the fraction S4-induced effects. Moreover, the vasorelaxing effect of the fraction was resistant to the block of nifedipine-sensitive Ca(2+) channels. The fraction S4 (10(-4) g/ml) produced a shift towards the right of the concentration-contractile response curve to NE, in normal conditions, and the shift was more evident in Ca(2+)-free Tyrode solution, suggesting an action on intracellular Ca(2+)-channels. The vasodilator action of fraction S4 on NE pre-contracted rings was not prevented by cyclopiazonic acid (blocker of Ca(2+)/ATPase), which excludes a role for mechanisms involving the storage of Ca(2+) in the sarcoplasmic reticulum. The reduction of the contraction elicited by caffeine, an opener of ryanodine-sensitive receptors, suggests that the fraction S4 of Michelia figo leaves could produce the vasorelaxing response by the blockade of ryanodine-sensitive Ca(2+) channels of the sarcoplasmic reticulum.

Animals↗

Furostanol saponins and quercetin glycosides from the leaves of Helleborus viridis L.

Phytochemical analysis of the polar extracts of the leaves of Helleborus viridis (Ranunculaceae) resulted in the isolation of two new furostanol saponins (25R)-26-[(alpha-L-rhamnopyranosyl)oxy]-22alpha-methoxyfurost-5-en-3beta-yl O-beta-D-glucopyranosyl-(1-->3)-O-[6-acetyl-beta-D-glucopyranosyl-(1-->3)]-O-beta-D-glucopyranoside (1) and (25R)-26-[(alpha-L-rhamnopyranosyl)oxy]-22alpha-methoxyfurost-5-en-3beta-yl O-beta-D-glucopyranosyl-(1-->3)-O-beta-D-glucopyranosyl-(1-->3)-O-beta-D-glucopyranoside (2) and three new quercetin glycosides, quercetin 3-O-(2-E-caffeoyl)-alpha-L-arabinopyranosyl-(1-->2)-beta-D-galactopyranoside-7-O-beta-d-glucopyranoside (3), quercetin 3-O-(2-E-caffeoyl)-alpha-L-arabinopyranosyl-(1-->2)-beta-D-galactopyranoside (4), and quercetin 3-O-alpha-L-arabinopyranosyl-(1-->2)-beta-D-galactopyranoside (5). The structures of the new compounds were determined by spectroscopic analysis, including 2D NMR data and mass spectrometry.

Helleborus↗

Structure of kaurane-type diterpenes from Parinari sprucei and their potential anticancer activity.

Twenty-three kaurane-type diterpenes 1 - 23, including twenty new natural products 1 - 20, have been isolated from the leaves of Parinari sprucei and their structures elucidated by spectroscopic and chemical analysis. The isolated compounds were tested for their cytotoxic activity towards a panel of cancer cell lines. Compounds 9 and 10 showed activity against all cell lines with ED (50) values in the range of 10 - 20 microg/mL. The previously known 13-hydroxy-15-oxozoapatlin 21 was evaluated in an in vivo hollow fiber test, and found to be active with KB and LNCaP cells at the concentrations used.

Antineoplastic Agents, Phytogenic↗

Phenolic compounds from Baseonema acuminatum leaves: isolation and antimicrobial activity.

Three new phenolic compounds, 1-galloyl-beta-D-glucopyranosyl-(1-->4)-beta-D-galactopyranoside (1), 2-methoxy-5-(1 '2 3'-trihydroxypropyl)-phenyl- 1-0-(6"-galloyl)-beta-D-glucopyranoside (2),and 2-methoxy-5-hydroxymethyl-phenyl-1-O-(6"-galloyl)-beta-D-glucopyranoside (3), together with the known compounds benzyl 6'-O-galloyl-beta-D-glucopyranoside (4), 1,6-di-O-galloyl-beta-D-glucopyranose (5), myrciaphenone B (6), kaempferol 3-0-(6"-galloyl)-beta-D-glucopyranoside (7), quercetin 3-0-(6"-galloyl)-beta-D-glucopyranoside (8), vomifoliol 9-O-beta-D-apiofuranosyl-(1-->6)-beta-D-glucopyranoside, 2,3-dihydrobenzofuran-2-(4'-hydroxy-3'-methoxyphenyl)-3-alpha-L-rhamnopyranosyloxymethyl-7-methoxy-5-propanol, and benzyl-O-alpha-L-rhamnopyranosyl-(1-->6)-Beta-D-glucopyranoside were isolated from the leaves of Baseonema acuminatum P. Choux (Asclepiadaceae). Their structures were determined by 1D- and 2D-NMR spectroscopy and by ESI-MS analysis. The antimicrobial activity of all compounds was evaluated in vitro against bacteria (Staphylococcus aureus two strains, Bacillus cereus, Bacillus subtilis, Escherichia coli, Salmonella thyphimurium) and three strains of Candida albicans. The new compounds 2 and 3, together with the known compound 4, showed antifungal activity against two clinically isolated Candida albicans strains and against C. albicans ATCC 2091; MIC values were in the range of 25-100 microg/mL. Compound 5 was active against the two clinically isolated strains of C. albicans with MICs of 12.5 microg/mL and 25 microg/mL. Compounds 1, 6, 7, and 8 inhibited only one strain of C albicans at the maximum concentration used. None of the phenolic compounds tested was active against the bacteria studied.

Anti-Infective Agents↗

Cytotoxic saponins from Schefflera rotundifolia.

Eight new oleanane and lupane saponins (1-8) as well as two new benzyl glycosides (9 and 10) were isolated from the aerial parts of Schefflera rotundifolia (Ten) Frodin (Araliaceae) together with two known benzyl glycosides. Their structures were established using 1D- and 2D-NMR spectroscopy and mass spectrometry. The antiproliferative activity of all compounds was evaluated using three continuous murine and human culture cell lines J774.A1, HEK-293, and WEHI-164. Compounds 7 and 8, having betulinic acid as aglycone, were the most active constituents.

Animals↗

Chemical composition and antioxidant activity of phenolic compounds from wild and cultivated Sclerocarya birrea(Anacardiaceae) leaves.

A quantitative study of the phenolic constituents of wild and cultivated leaves of Sclerocarya birrea(Anacardiaceae) was carried out by HPLC-UV/PDA and LC-MS. Phytochemical analysis of the methanol extract of wild plants led to the isolation of one new flavonol glycoside, quercetin 3-O-alpha-l-(5' '-galloyl)-arabinofuranoside (1), and eight known phenolic compounds; two epicatechin derivatives were also isolated from the same extract of the cultivated species. The antioxidant activity of all isolated compounds was determined by measuring free radical scavenging effects using the Trolox equivalent antioxidant capacity assay and the coupled oxidation of beta-carotene and linoleic acid (autoxidation assay).

Anacardiaceae↗

Essential oils from Mediterranean lamiaceae as weed germination inhibitors.

The essential oils obtained from rosemary (Rosmarinus officinalis L.), thyme (Thymus vulgaris L.), and savory (Satureja montana L.) and the four monoterpenes that are their major constituents have been analyzed by GC and GC-MS and tested for their allelopathic properties on the seeds of three different annual weeds (Chenopodium album, Portulaca oleracea, and Echinochloa crus-galli) and three crops (Raphanus sativus, Capsicum annuum, and Lactuca sativa), with the aim to evaluate in vitro their potential as germination inhibitors. The essential oil composition varied with the species, thymol being the main constituent (44%) of thyme and carvacrol (57%) that of savory oil. Differences in essential oil composition were observed within two different rosemary ecotypes, type A, with alpha-pinene (37%) and 1,8-cineole (23%), and type B, characterized by a 2-fold content of 1,8-cineole (47%). This latest essential oil inhibited completely the germination of weeds while concurrently displaying little effect on pepper. The other two oils showed less selective action. S. montana essential oil, with 57% carvacrol, is the most active compound, completely inhibiting germination both of crops and weeds. Borneol, one of the main constituents of the oil of rosemary type B, showed an activity comparable to that of the whole oil. Crop and weed seeds treated with 1,8-cineole showed germination values that were not significantly different from controls, even if a slowing of the germination process expressed in terms of a significant increase in mean germination time was observed. Monoterpene compounds also present in the essential oils mainly represented the volatile fraction released from the crops and their residues into the soil.

Chromatography, Gas↗

Composition of the essential oil of Mentha microphylla from the Gennargentu Mountains (Sardinia, Italy).

The essential oil obtained by hydrodistillation of the fresh aerial parts of Mentha microphylla C. Kock (Lamiaceae) collected on the Gennargentu Mountains (Sardinia, Italy) has been investigated by gas chromatography (GC) and GC/mass spectrometry (MS). The main constituents that resulted were pulegone (34.1%), piperitenone oxide (32.9%), and piperitenone (11.3%). The presence of small amounts of compounds such as ethyl hexanoate, 1-octen-3-ol, nonanal, and ethyl 2-methylbutanoate could justify the particular odorous profile of the plant, resembling the aroma of milk and other dairy products such as mozzarella.

Chromatography, Gas↗

Use of solid-phase micro-extraction as a sampling technique in the determination of volatiles emitted by flowers, isolated flower parts and pollen.

The volatiles emitted by fresh whole flowers or isolated flower parts of mandarin, Citrus deliciosa Ten. (Rutaceae), were sampled using solid-phase micro-extraction (SPME). This technique offers several advantages over dynamic headspace sampling techniques used in previous investigations. In particular, SPME requires smaller sample sizes and very short sampling times, which can minimize the formation of artifacts due to damage to the plant, and contaminations or loss of compounds. This was especially applicable to the collection of volatiles from pollen.

Gas Chromatography-Mass Spectrometry↗

Differences in the fragrances of pollen, leaves, and floral parts of garland (Chrysanthemum coronarium) and composition of the essential oils from flowerheads and leaves.

Headspace analyses of pollen, whole flowerheads, ligulate and tubular florets, flower buds, involucral bracts, and leaves have been performed on the food plant Chrysanthemum coronarium L. (Asteraceae). The analyses permitted differences in the pattern of volatiles emitted by the different floral parts to be observed and the site and phenological stage of emission of these chemicals to be verified. Camphor and cis-chrysanthenyl acetate were emitted mainly by ligulate and tubular florets; the production of myrcene and (Z)-ocimene was higher in the flower buds, whereas beta-caryophyllene, (E,E)-alpha-farnesene, and (E)-beta-farnesene seemed attributable mainly to the involucral bracts. The leaves showed a quite different volatile profile, with (Z)-ocimene as the main constituent. Pollen showed a completely different composition of its volatiles, with perilla aldehyde, cis-chrysanthenyl acetate, and camphor among the principal compounds; many carbonylic compounds and linear hydrocarbons have been detected exclusively in pollen. Furthermore, the essential oils obtained from flowerheads and leaves have been studied. These samples showed mainly quantitative differences. Camphor (22.1%) and cis-chrysanthenyl acetate (19.9%) were the main constituents of the oil from flowers, whereas the oil from the leaves contained mainly (Z)-ocimene (45.4%) and myrcene (28.2%).

Bridged Bicyclo Compounds↗

Volatile fractions from three cultivars of Olea europaea L. collected in two different seasons.

The chemical composition of the volatile fractions from leaves of three Olea europaea L. cultivars (Leccino, Frantoio, and Cipressino) harvested at two different times of the year were examined by GC and GC-MS. The results showed a high content of aliphatic aldehydes in the three cultivars during both harvesting periods and an increase of (E)-2-hexenal (an aldehyde with high antimicrobial properties) percentage from July to November.

Aldehydes↗

Volatiles from leaves, fruits, and virgin oil from Olea europaea Cv. Olivastra Seggianese from Italy.

The volatiles produced by leaves and fruits of Olea europaea cv. Olivastra Seggianese have been analyzed in two different phenological stages. Furthermore, the volatiles of the virgin olive oil obtained from ripe fruits has been characterized. The volatiles were sampled by means of two different techniques: hydrodistillation and SPME. Differences were observed between the two different collection times, the different organs, and sampling techniques. The major constituents were often aldehydes, particularly (E)-2-hexenal (9.8-48.0%); however, also many terpenoids have been identified, mainly (E,E)-alpha-farnesene (0.2-27.0%), linalool (0-3.6%), beta-caryophyllene (0-8.1%), and valencene (0-2.5%). This is the first investigation on this cultivar.

Aldehydes↗

Further constituents from Caralluma negevensis.

Two new megastigmane glycosides (1 and 2) and two new flavone glycosides (3 and 4) were isolated from the methanol extract of the whole plant of Caralluma negevensis Zohary (Asclepiadaceae). The structures of the isolated compounds were characterized as (9R)-2beta,9-dihydroxymegastigma-4,7-dien-3-one-9-O-alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside (1), 2beta,9-dihydroxymegastigma-4-en-3-one 9-O-alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside (2), luteolin 3'-O-beta-D-glucopyranoside-4'-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside (3), and luteolin 3',4'-di-O-beta-D-glucopyranoside (4). The structures of the isolated compounds were established on the basis of spectral evidence and chemical transformation.

Apocynaceae↗

Antioxidant and free radical scavenging activity of flavonol glycosides from different Aconitum species.

Bioassay-guided fractionation by 1,1-diphenyl-2-dipicrylhydrazyl (DPPH) radical scavenging test of polar extracts of some Italian Aconitum species (A. napellus subsp. tauricum, A. napellus subsp. neomontanum, A. paniculatum, A. vulparia) led to the isolation of 13 flavonol glycosides: quercetin 3-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->2)-beta-glucopyranoside-7-O-alpha-rhamnopyranoside (1), kaempferol 3-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->2)-beta-glucopyranoside-7-O-alpha-rhamnopyranoside (2), quercetin 3-O-(6-trans-p-coumaroyl)-beta-glucopyranosyl-(1-->2)-beta-glucopyranoside-7-O-alpha-rhamnopyranoside (3), kaempferol 3-O-(6-trans-p-coumaroyl)-beta-glucopyranosyl-(1-->2)-beta-glucopyranoside-7-O-alpha-rhamnopyranoside (4), quercetin 7-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (5), kaempferol 7-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (6), kaempferol 7-O-(6-trans-p-coumaroyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (7), kaempferol 3-O-beta-(2"-acetyl)galactopyranoside (8), kaempferol 3-O-beta-(2"-acetyl)galactopyranoside-7-O-alpha-arabinopyranoside (9), quercetin 3-O-beta-(2"-acetyl)galactopyranoside-7-O-alpha-arabinopyranoside (10), quercetin 3,7-di-O-alpha-rhamnopyranoside (11), kaempferol 3,7-di-O-alpha-rhamnopyranoside (12) and quercetin 3-O-beta-glucopyranoside-7-O-alpha-rhamnopyranoside (13). Their antioxidant activity (AA) was determined by measuring free radical scavenging activity by DPPH test and the coupled oxidation of beta-carotene and linoleic acid assay. The results showed that 5 is the most active compound in the DPPH free-radical scavenging test (IC(50) 1.9 microM) while in the coupled oxidation of beta-carotene and linoleic acid assay compound 1 has the highest inhibitory ratio after 1h (58.9%). Some structure-activity relationships on the AA were obtained.

Aconitum↗

Antimicrobial diterpenes from the seeds of Cephalotaxus harringtonia var. drupacea.

Six diterpenes, including two new natural products, were isolated from the seeds of Cephalotaxus harringtonia. The new metabolites were characterised as 8 beta-hydroxy-9(11),13-abietadien-12-one and 5,6-didehydroferruginol, while the known compounds were identified as ferruginol, sugiol, 6,12-dihydroxyabieta-5,8,11,13-tetraen-7-one, and abieta-8,11,13-trien-7 beta-ol. These compounds were studied in vitro for their antimicrobial activity against clinically isolated bacteria and Candida strains. Ferruginol and 6,12-dihydroxyabieta-5,8,11,13-tetraen-7-one showed antimicrobial activity against Gram-positive bacteria. None of the six diterpenes was active against the Gram-negative organisms and yeasts tested.

Anti-Bacterial Agents↗

Cytotoxic saponins from Schefflera fagueti.

Six new lupane (1 - 4) and oleanane saponins (5 and 6) were isolated from the aerial parts of Schefflera fagueti Baill. (Araliaceae). Their structures were determined by 2D-NMR spectroscopy (DQF-COSY, 1D-TOCSY, 2D-HOHAHA, 1D-ROESY, HSQC, HMBC). The antiproliferative activity of compounds 1 - 6 and of their prosapogenins (1a - 6a) was evaluated using three continuous murine and human culture cell lines J774, HEK-293, WEHI-164. Oleanane saponins 5 and 6 were the most active, showing significant inhibitory effects on all cell lines, while their prosapogenins 5a and 6a demonstrated minor activity.

Animals↗

The xanthones gentiacaulein and gentiakochianin are responsible for the vasodilator action of the roots of Gentiana kochiana.

Gentiana kochiana Perr. et Song. (Gentianaceae), a plant used in the traditional medicine of Tuscany (Italy) as antihypertensive remedy, exerts a vasodilator action on in vitro aortic rings that is probably linked to the blocking of the ryanodine-sensitive Ca++ channels. In the present study, three known xanthones were isolated from the crude methanolic extract of the roots: gentiacaulein, gentiakochianin, and swertiaperennin. The first two showed a vasorelaxing activity in rat aortic preparations, pre-contracted by 3 microM norepinephrine (pIC50 = 5.00 +/- 0.032 for gentiacaulein, pIC50 = 4.95 +/- 0.068 for gentiakochianin), 20 mM KCl (pIC50 = 4.90 +/- 0.15 for gentiacaulein; 4.59 +/- 0.069 for gentiakochianin), or 5 mM caffeine; on the contrary, in the same conditions, swertiaperennin did not show any vasodilator effect. In conclusion, gentiacaulein and gentiakochianin seem to be the compounds responsible for the vasorelaxing properties of the crude extract of Gentiana kochiana roots.

Animals↗

New Pyrrolizidine Alkaloids and Glycosides from Anchusa strigosa.

Six new pyrrolizidine alkaloids, a new carboxylic acid, a new phenolic and a new oleanane glycoside, together with the known compounds 7,7'-bis-(4-hydroxy-3,5-dimethoxyphenyl)-8,8'-dihydroxymethyltetrahydrofuran 4'-O-beta-D-glucopyranoside, rosmarinic acid, caffeic acid, tormentic acid 28-O-beta- D-glucopyranoside, euscaphic acid 28-O-beta-D-glucopyranoside, euscaphic acid, and allantoin were isolated from Anchusa strigosa roots. Their structures were established by high resolution NMR, MS, elemental analysis, and chemical reactions.

Boraginaceae↗