Secondary Metabolites and Their Biological Evaluation from the Aerial Parts of Sibth. & Sm. (Asteraceae).

Phytochemical investigation of Sibth. & Sm. resulted in the isolation of twenty-two natural products: eleven sesquiterpene lactones, artemorin (), tamirin (), tanachin (), reynosin (), baynol C (), desacetyl-β-cyclopyrethrosin (), 1β-hydroxy-4α-methoxy-5α,7α,6β-eudesm-11(13)-en-6,12-olide (), 1β,4α,6α-trihydroxyeudesm-11-en-8α,12-olide (), 1β-hydroxy-arbusculin A (), methyl-1β,4α,6α-trihydroxy-5α,7αH-eudesm-11(13)-en-12-oate () and methyl-1β,6α,8α-trihydroxy-5α,7αH-eudesma-4(15),11(13)-dien-12-oate (); one lignan, pinoresinol (); one norisoprenoid, loliolide (); six flavonoids (four genins and two glycosides), hispidulin (), nepetin (), jaceosidin (), eriodictyol (), eriodictyol-3'-O-β-D-glucoside () and eriodictyol-7-O-β-D-glucuronide (); and three phenolic derivatives (one phenolic acid and two phenolic glucosides), protocatechuic acid (), arbutin () and nebrodenside A ().

Chemical Constituents and Anticancer Activities of the Extracts from × Rech. f. ( × ).

The present work is the first report on the ingredients of the × hybrid, a plant of the genus . So far, thirty substances have been isolated by various chromatographic techniques and identified by spectroscopic methods, such as UV/Vis, NMR, GC-MS and LC-MS. The compounds are classified as flavonoids: naringenin, eriodyctiol, eriodyctiol-7-O--D-glucoside, luteolin, luteolin-7-O--D-glucoside, apigenin, apigenin-7-O--D-glucoside, diosmetin-7-O--D-glucoside, quercetin, hesperetin and quercetin-3-O--D-glucoside; phenylpropanoids: martynoside, verbascoside, forsythoside B, echinacoside and allysonoside; chromene: 5,7-dihydroxychromone; phenolic acids: caffeic acid, -hydroxybenzoic acid, chlorogenic acid, chlorogenic acid methyl ester, gallic acid, -coumaric acid and vanillic acid; aliphatic hydrocarbon: docos-1-ene; steroids: brassicasterol and stigmasterol; a glucoside of allylic alcohol, 3-O--D-apiofuranosyl-(1→6)-O--D-glucopyranosyl-oct-1-ene-3-ol, was fully characterized as a natural product for the first time.

Biological Activities of Pod and Seed Extracts: A Comparative Analysis of Two Cretan Cultivars.

L., commonly known as the carob tree, appears in most Mediterranean countries, often cultivated for the collection of its fruits to be used as food for humans and animals. This study was aimed at the phytochemical characterization of two common Cretan cultivars and the biological evaluation of deseeded pod and seed extracts regarding their putative use in cosmetics.

Enantioselective synthesis of a costic acid analogue with acaricidal activity against the bee parasite .

One major disease of the pupae and the adult bee is the so-called that is owing to the bee parasite . It is an ectoparasite of bees, causing significant losses in the bee population needed for honey production as well as for pollination in agriculture. Costic acid is a sesquiterpene-carboxylic acid present in the plant .

The Synthetic Microneurotrophin BNN27 Affects Retinal Function in Rats With Streptozotocin-Induced Diabetes.

BNN27, a C17-spiroepoxy derivative of DHEA, was shown to have antiapoptotic properties via mechanisms involving the nerve growth factor receptors (tropomyosin-related kinase A [TrkA]/neurotrophin receptor p75 [p75]). In this study, we examined the effects of BNN27 on neural/glial cell function, apoptosis, and inflammation in the experimental rat streptozotocin (STZ) model of diabetic retinopathy (DR). The ability of BNN27 to activate the TrkA receptor and regulate p75 expression was investigated.

Use of costic acid, a natural extract from , for the control of , a parasite of the European honey bee.

Costic acid has been isolated from the plant and its efficacy against , a parasite of , the European honey bee, has been studied. Costic acid exhibited potent in vivo acaricidal activity against the parasite. Initial experiments showed that the compound is not toxic for human umbilical vein endothelial cells (HUVEC) at concentrations of up to 230 micromolar (μM), indicating that costic acid could be used as a safe, low-cost and efficient agent for controlling varroosis in honey bee colonies.

Chemical and genetic characterization of Phlomis species and wild hybrids in Crete.

The genus Phlomis is represented in the island of Crete (Greece, Eastern Mediterranean) by three species Phlomis cretica C. Presl., Phlomis fruticosa L.

Reporting effectiveness of an extract of three traditional Cretan herbs on upper respiratory tract infection: results from a double-blind randomized controlled trial.

Ethnopharmacological Relevance: Observations from the island of Crete, Greece suggest that infusions of traditional Cretan aromatic plants, well known for their ethnopharmacological use in Eastern Mediterranean region and Near East, could be effective in the prevention and treatment of upper respiratory tract infections, including viral-induced infections. The aim of this study was to report the effectiveness of an essential-oil extract of three Cretan aromatic plants in the treatment of cases with an upper respiratory tract infection.

Materials And Methods: A double blind randomized controlled trial was implemented between October 2013 and February 2014.

Fullerene-coumarin dyad as a selective metal receptor: synthesis, photophysical properties, electrochemistry and ion binding studies.

A coumarin derivative with a malonate unit has been synthesized and used for the preparation of a fullerene-coumarin dyad through the Bingel cyclopropanation method. The newly synthesized dyad is soluble in organic solvents and has been fully characterized with traditional spectroscopic techniques. Electronic interactions between the two components of the dyad were probed with the aid of UV/Vis spectroscopy, fluorescence emission, and electrochemistry measurements.

A "turn-on" coumarin-based fluorescent sensor with high selectivity for mercury ions in aqueous media.

The synthesis and spectral profile of a "turn-on" fluorescent sensor selective for Hg(2+) ions in aqueous media is described.

Coumarin-based ratiometric fluorescent indicators with high specificity for lead ions.

Total syntheses and spectral properties of fluorescent Pb(2+) indicators are reported.

ICPBCZin: a red emitting ratiometric fluorescent indicator with nanomolar affinity for Zn2+ ions.

A new fluorescent Zn2+ indicator, namely, ICPBCZin was synthesized and the spectral profile of its free and Zn2+ bound forms was studied. The newly synthesized zinc indicator incorporates as chromophore the chromeno [3',2':3,4]pyrido[1,2a] [1,3]benzimidazole moiety and belongs to the dicarboxylate-type of zinc probes. The compound is excited with visible light, exhibits high selectivity for zinc in the presence of calcium and other common biological ions, and its Zn2+ dissociation constant is 4.

Anti-inflammatory and antioxidant activity of coumarins designed as potential fluorescent zinc sensors.

A series of coumarin analogs, designed and synthesised as potential fluorescent zinc probes were evaluated for their biological activity as anti-inflammatory and antioxidant agents. The effect of the synthesised compounds on inflammation, using the carrageenin-induced rat paw oedema model, was studied. In general, the compounds were found to be potent anti-inflammatory agents (26.

Quercetin exhibits a specific fluorescence in cellular milieu: a valuable tool for the study of its intracellular distribution.

The elaboration of novel techniques for flavonoid intracellular tracing would elucidate the compounds' absorption and bioavailability and assist molecular and pharmacological approaches, as they are promising candidates for drug development. This study exploited the properties of quercetin (3,3',4',5,7-pentahydroxyflavone), found in high concentrations in the majority of edible plants. Through the use of UV-vis spectroscopy, confocal microscopy, and HPLC-ESI-MS, native quercetin, at physiologically relevant concentrations, was found to exhibit a specific fluorescence (488 nmex/500-540 nmem) upon internalization.

ICPBC and C12-ICPBC: two new red emitting, fluorescent Ca2+ indicators excited with visible light.

Two new, visible-excited and red-emitting fluorescent Ca(2+) indicators were synthesized and the spectral profiles of their free and Ca(2+) bound forms were studied. The fluorescent properties of these probes are due to the extended conjugation of the chromeno[3',2':3,4]pyrido[1,2a][1,3]benzimidazole chromophore incorporated in their BAPTA-type, Ca(2+) chelating structure. The compounds, namely ICPBC and its N-dodecyl analog C12-ICPBC exhibit Ca(2+) dissociation constants of 7.

Composition and insect attracting activity of the essential oil of Rosmarinus officinalis.

The essential oil and a number of extracts of Rosmarinus officinalis L. in solvents of increasing polarity were isolated, and their components identified and tested as pest control agents. Ethanol and acetone extracts attract grape berry moth Lobesia botrana.

Near-membrane iminocoumarin-based low affinity fluorescent Ca(2+) indicators.

Two new potential near-membrane iminocoumarin-based fluorescent Ca(2+) indicators were synthesized and the spectral profiles of their free and Ca(2+) bound forms were studied. The probes incorporate in their BAPTA-related structures, the 3-(benzimidazolyl)iminocoumarin or the 3-(benzothiazolyl)iminocoumarin moiety, substituted at the imino nitrogen with an n-dodecyl lipophilic chain. The compounds are excited with visible light and have Ca(2+) dissociation constant values of 5.

Polycarboxylate fluorescent indicators as ion concentration probes in biological systems.

A large number of techniques have been applied to monitor the function of free metal ions in biological systems. Fluorescent ion probes have evolved into an extremely useful tool for contemporary experimentalists. Polycarboxylate indicators are widely used in the determination of metal ion concentrations, especially due to their cell membrane permeability.

Iminocoumarin-based low affinity fluorescent Ca2+ indicators excited with visible light.

A series of iminocoumarin-based fluorescent Ca2+ indicators were synthesized and the spectral profiles of their free and Ca2+ bound forms were studied. The newly-synthesized compounds incorporate the Ca2+ chelating structure of BAPTA. The chromophore moieties are iminocoumarins substituted at the 3-position with benzothiazolyl, benzoxazolyl and benzimidazolyl groups.

Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.

In vitro assays on a series of cis- and trans-octahydrobenzo[g]quinolines indicated an unusual trend of affinities at the dopaminergic receptors and alpha adrenoceptors. The trans N-benzyl analogues exhibited affinity at the alpha2 as well as the D1-like receptors whereas their N-unsubstituted congeners showed a distinct preference for the alpha2 adrenoceptor. Enhanced activity for the alpha2 receptors was also exhibited by the cis N-benzylated isomers.

N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.

A series of N-(iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines was synthesized and assayed in vitro for their dopaminergic and alpha-adrenergic activity. Structure-activity relationship (SAR) analysis revealed that the tested benzoquinolines exhibited activity at the D1 rather than the D2 receptor sites in contrast to the D2 receptor subfamily activity reported for their aminotetralin congeners. N-Iodopropenyl substitution was apparently a decisive factor for D1 activity independent of ring substitution pattern.

Composition and antimicrobial activity of the essential oil of Cistus creticus subsp. eriocephalus.

The chemical composition of the essential oil of the leaves of Cistus creticus subsp. eriocephalus (Viv.) Greuter & Burdet, (Cistaceae), was investigated by GC/MS.

Detection of cardiovascular calcified deposits via tetracarboxylate ion dye (BTC) probing and laser-induced fluorescence spectroscopy.

In order to develop a reliable, laser-induced, fluorescence-guided, angioplasty system, fluorescence spectra were recorded during exposure of normal and atherosclerotic cadaveric aortic tissue to argon ion laser irradiation. A characteristic increase in the fluorescence signal in the 520-560 nm spectral region for atheromatous tissue was observed after treatment of the samples with a tetracarboxylate ion dye (BTC). This allowed the development of a simple algorithm (based on the intensity difference) and a subsequent index of discrimination between normal and atheromatous tissue.