Bombesin: a possible role in wound repair.

During tissue regeneration and wound healing of the skin, migration, proliferation and differentiation of keratinocytes are important processes. Here we assessed the effect of a neuropeptide, bombesin, on keratinocytes during regeneration from scratch wounding. Bombesin purified from amphibian skin, is homologous of mammalian gastrin-releasing peptide and is active in mammals. Its pharmacological effects mediate various physiological activities: hypertensive action, stimulating action on gastric secretion, hyperglycemic effect or increased insulin secretion. In vitro it shows a hyperproliferative effect on different experimental models and is involved in skin repair. The aim of this study was to elucidate the effect of Bombesin in an in vitro experimental model on a mechanically injured human keratinocyte monolayer. We evaluated different mediators involved in wound repair such as IL-8, TGFbeta, IL-1, COX-2, VEGF and Toll-like receptors 2 and 4 (TLR2 and TLR4). We also studied the effects of bombesin on cell proliferation and motility and its direct effect on wound repair by observing the wound closure after mechanical injury. The involvement of the bombesin receptors neuromedin receptor (NMBR) and gastrin-releasing peptide receptor (GRP-R) was also evaluated. Our data suggest that bombesin may have an important role in skin repair by regulating the expression of healing markers. It enhanced the expression of IL-8, TGFbeta, COX-2 and VEGF. It also enhanced the expression of TLR2, while TLR4 was not expressed. Bombesin also increased cell growth and migration. In addition, we showed that NMBR was more involved in our experimental model compared to GRP-R.

Anti-ulcer, anti-inflammatory and antioxidant activities of the n-butanol fraction from Pteleopsis suberosa stem bark.

Pteleopsis suberosa Engl. et Diels (Combretaceae) is a tree distributed in many African countries. The decoction from the stem bark is orally administered for the treatment of gastric ulcers in traditional medicine. Previous pharmacological studies reported the anti-ulcer activity of extracts from P. suberosa stem bark. In the present study, the anti-ulcer and anti-inflammatory effects of the n-butanol fraction (RBuOH) obtained from a methanol extract of P. suberosa bark were investigated on ethanol-induced gastric ulcers in rats and carrageenan-induced paw oedema in mice. Misoprostol (0.50 mg/kg, p.o.) and indomethacin (8.00 mg/kg, p.o.) were used as positive controls for anti-ulcer and anti-inflammatory activities, respectively. Results showed that RBuOH treatment significantly reduced the incidence of gastric lesions (50 mg/kg, P<0.05; 100 and 200 mg/kg, P<0.01) and restored the decreased levels of total sulfhydryl groups (T-SH) and non-protein sulfhydryl groups (NP-SH) (50, 100 mg/kg, P<0.05; 200 mg/kg, P<0.01) in the stomach homogenate. Moreover, RBuOH treatment attenuated MDA levels as index of lipid peroxidation in gastric mucosa. Administration of RBuOH at the same dosage (50, 100 and 200 mg/kg) reduced significantly (P<0.01) carrageenan-induced paw oedema in dose-dependent manner (from 42.81% to 87.81% inhibition, 5h after carrageenan injection). The anti-inflammatory effect of RBuOH at 200 mg/kg was comparable with that of indomethacin. Finally, RBuOH proved to possess elevated free radical scavenger capacity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay (IC(50) 23.48 microg/ml) which may contribute to the observed anti-ulcer and anti-inflammatory activities.

Exploring the design of a lightweight, sustainable and comfortable aircraft seat.

BACKGROUND: Making a lightweight seat that is also comfortable can be contradictory because usually comfort improvement means adding a feature (e.g. headrest, adjustable lumbar support, movable armrests, integrated massage systems, etc.), which makes seats heavier. OBJECTIVE: This paper explores the design of an economy class aircraft seat that aims to be lightweight, comfortable and sustainable. METHODS: Theory about comfort in seats, ergonomics, lightweight design, Biomimicry and Cradle to cradle was studied and resulted in a list of requirements that the new seat should satisfy. RESULTS: The design process resulted in a new seat that is 36% lighter than the reference seat, which showed that a significant weight reduction can be achieved. This was completed by re-designing the backrest and seat pan and integrating their functions into a reduced number of parts. Apart from the weight reduction that helps in reducing the airplane's environmental impact, the seat also satisfies most of the other sustainability requirements such as the use of recyclable materials, design for disassembly, easy to repair. A user test compared the new seat with a premium economy class aircraft seat and the level of comfort was similar. CONCLUSIONS: Strong points of the new design were identified such as the lumbar support and the cushioning material, as well as shortcomings on which the seat needs to be improved, like the seat pan length and the first impression. Long term comfort tests are still needed as the seat is meant for long-haul flights.

Flavonoids from Aconitum napellus subsp. neomontanum.

Three flavonol glycosides quercetin 7-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (1), kaempferol 7-O-(6-trans-caffeoyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (2), and kaempferol 7-O-(6-trans-p-coumaroyl)-beta-glucopyranosyl-(1-->3)-alpha-rhamnopyranoside-3-O-beta-glucopyranoside (3), together with the known beta-3,4-dihydroxyphenethyl beta-glucopyranoside, were isolated from the flowers of Aconitum napellus subsp. neomontanum. Their structures were elucidated by spectroscopic methods, including 2D NMR spectral techniques.

Molluscicidal and piscicidal activities of Venezuelan Chrysobalanaceae plants.

Extracts of increasing polarity of 6 Venezuelan plants belonging to the Chrysobalanaceae family were tested for possible letal toxicity against Biomphalaria glabrata Say, a snail intermediate hosts of Schistosoma mansoni Sambon. The piscicidal toxicity of the active extracts was also evaluated with the aim of findings compounds without toxicity in nontarget organisms, principally fishes and humans.

New metabolites from onopordum illyricum

A phytochemical investigation of Onopordum illyricum afforded, in addition to several known compounds, two new eudesmane sesquiterpenes (1 and 2), two new elemane sesquiterpenes (3 and 4), and one new neolignan derivative (5). The structure elucidation of all compounds was based on their (1)H and (13)C NMR spectral data, including those derived from 1D TOCSY, 2D NMR, COSY-DQF, HSQC, and HMBC experiments, as well as extensive 1D ROESY studies.

A new phenolic compound from Nigella damascena seeds.

A new phenolic ester has been isolated from the seeds of Nigella damascena and the structure was established as 1-O-(2,4-dihydroxy)phenylacetyl glycerol (1) by 1H and 13C-NMR spectral data and EI-MS analysis.

Flavonol glycosides from Aconitum vulparia.

The isolation of five flavonol glycosides (1-5) from the flowers of Aconitum vulparia is reported, together with the 1H- and 13C-NMR spectral data in CD(3)OD of compound 3 and 5.

Triterpenes from Licania licaniaeflora.

Nine triterpenoids with lupane, oleanane, and ursane skeleton have been isolated and characterized from the leaves of Licania licaniaeflora. The structural identification was based on (1)H and (13)C-NMR spectral data.

Myricetin glycosides from Licania densiflora.

Dried leaves of Licania densiflora yielded five myricetin glycosides: myricetin 3'-methylether-3-O-glucoside (1), myricetin 3'-methylether-3-O-galactoside (2), myricetin 4'-methylether-3-O-rhamnoside (3), myricetin 3',5'-dimethylether-3-O-glucoside (4), and myricetin 3',5'-dimethylether-3-O-rhamnoside (5). Their structures were elucidated by spectroscopic methods including mono- and bi-dimensional NMR techniques.

Effect of sesquiterpene lactone coronopilin on leukaemia cell population growth, cell type-specific induction of apoptosis and mitotic catastrophe.

OBJECTIVES: The aim of this study was to investigate anti-leukaemic potential of coronopilin, a sesquiterpene lactone from Ambrosia arborescens, and to characterize mechanism(s) underlying its activity. MATERIALS AND METHODS: The study was conducted on Jurkat and U937, two leukaemia-derived cell lines. Apoptosis and impairment of cell cycle progression were evaluated by flow cytometry and by microscopic analysis. Changes in protein expression and activation were evaluated by western blot analysis. Coronopilin-tubulin covalent adducts were demonstrated by mass spectrometry. RESULTS: Coronopilin inhibited (IC(50) ≤ 20 µm) leukaemia cell population growth, but displayed poor cytotoxicity to normal white blood cells. On Jurkat cells, coronopilin exerted cell population growth inhibition activity, mainly by triggering caspase-dependent apoptosis. Conversely, in U937 cells, coronopilin's primary response was a robust arrest in G(2) /M. Marked increase in mitotic index and presence of activated cyclin B1/Cdk1 complex, phosphorylated histone H3 at Ser10, and hyperpolymerized tubulin indicated that cells accumulated in mitosis. Prolonged mitotic arrest ultimately resulted in U937 mitotic catastrophe, and dying cells exhibited the features of non-caspase-dependent death. CONCLUSIONS: This study demonstrated that coronopilin efficiently inhibited leukaemia cell population growth by triggering cell type-specific responses. Moreover, coronopilin-mediated cell population expansion inhibition was specific to neoplastic cells, as normal white blood cell viability was not significantly affected. Thus, coronopilin may represent an interesting new chemical scaffold upon which to develop new anti-leukaemic agents.

Extracts and constituents of Lavandula multifida with topical anti-inflammatory activity.

The topical anti-inflammatory activity of the ethanol and aqueous extracts from the aerial parts of Lavandula multifida L. (Lamiaceae), used in the Moroccan traditional medicine, was investigated by inhibition of the Croton oil-induced ear edema in mice. The biological assay revealed a dose-dependent anti-inflammatory activity for the ethanol extract, while the aqueous one was less active. Bioassay-guided fractionation of the ethanol extract led to identify four triterpenic acids of oleanane series, four pimarane and one iso-pimarane diterpenes, as well as the phenolic monoterpene carvacrol and its glucoside. Some of these compounds revealed an anti-inflammatory activity comparable to that of indomethacin.

Screening of Mediterranean Rosaceae plants for their molluscicidal and piscicidal activities.

Extracts of increasing polarity of 13 plants belonging to Mediterranean Rosaceae were tested for possible lethal toxicity against Biomphalaria glabrata Say, a snail intermediate host of Schistosoma mansoni Sambon. Due to the search for compounds without toxicity in nontarget organisms, principally fish and humans, the piscicidal toxicity of the active extracts was also evaluated.

Antimicrobial triterpenoids from Licania heteromorpha.

Six triterpenoids having a lupane and oleane skeleton were isolated from the leaves and young branches of Licania heteromorpha Bentham var. heteromorpha and were identified as: betulinic acid 1, alphitolic acid 2, 3 beta-O-trans-p-coumaroyl alphitolic acid 3, 3 beta-O-cis-p-coumaroyl alphitolic acid 4, 3 beta-O-trans-p-coumaroyl maslinic acid 5, 3 beta-O-cis-p-coumaroyl maslinic acid 6. The antimicrobial activity of these compounds was evaluated in vitro on clinically isolated microorganisms employing a microdilution method. Compounds 2, 3, 5, and 6 showed antimicrobial activity on Gram-positive bacteria and yeasts, whereas none of the six triterpenoids were active against Gram-negative organisms.

New prenylated anthraquinones and xanthones from Vismia guineensis.

From the roots of Vismia guineensis 23 structurally related compounds were isolated and identified. Ten of them are new constituents, namely 3-O-(2-hydroxy-3-methylbut-3-enyl)-emodin (1); 3-O-(2-methoxy-3-methylbut-3-enyl)-emodin (2); 1, 8-dihydroxy-3-(2-methoxy-3-methylbut-3-enyloxy)-6-methylx anthone (3); 1,8-dihydroxy-3-geranyloxy-6-methylxanthone (4); 1, 8-dihydroxy-3-isoprenyloxy-6-methylxanthone (5); 1,8-dihydroxy-3-(3, 7-dimethyl-7-methoxyoct-2-enyloxy)-6-methylxanthone (6); 3-O-(E-3-hydroxymethylbut-2-enyl)-emodin (7); 3-O-(3-hydroxymethyl-4-hydroxybut-2-enyl)-emodin (8); 1, 8-dihydroxy-3-(E-3-hydroxymethylbut-2-enyloxy)-6-methylxa nthone (9); and 1, 8-dihydroxy-3-(3-hydroxymethyl-4-hydroxybut-2-enyloxy)-6- methylxantho ne (10). Their structures were established by means of EIMS and a combination of homonuclear and heteronuclear 2D NMR techniques. Furthermore, an in vitro preliminary screening of antimitotic activity of all the isolated compounds was also evaluated.

New flavonol glycosides from the flowers of Aconitum napellus ssp. tauricum.

From the methanolic extract of the flowers of A. napellus spp. tauricum four new 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), and kaempferol 3-O-(6-trans-p-coumaroyl)-beta-glucopyranosyl-(1-->2)-beta- glucopyranoside-7-O-alpha-rhamnopyranoside (4), together with the known beta-3,4-dihydroxyphenethyl beta-glucopyranoside were isolated. The structural elucidation of all compounds was deduced on the basis of 1H- and 13C-NMR spectral data, including those derived from 2D-NMR, as well as on HPLC-MS results.

Antioxidant principles from Bauhinia tarapotensis.

A new cyclohexenone (1) and a new caffeoyl ester derivative (2), together with the known compounds (-)-isolariciresinol 3-alpha-O-beta-D-glucopyranoside (3), (+)-1-hydroxypinoresinol 1-O-beta-D-glucopyranoside (4), isoacteoside (5), luteolin 4'-O-beta-D-glucopyranoside (6), and indole-3-carboxylic acid (7), were isolated from the leaves of Bauhinia tarapotensis. The structures of these new compounds were determined by spectroscopic data analysis. The antioxidant activities of 1-7 were determined by measuring their free radical scavenging effects, using the 1,1-diphenyl-2-dipicrylhydrazyl free radical (DPPH) and Trolox equivalent antioxidant activity (TEAC) methods, and the coupled oxidation of beta-carotene and linoleic acid. Compounds 3-5 showed good activities in the DPPH and TEAC tests, while compounds 1 and 2 were active in the coupled oxidation of beta-carotene and linoleic acid bioassay.

Flavonol glycosides from the flowers of Aconitum paniculatum.

Three new acetylated flavonol glycosides-kaempferol 3-O-beta-(2' '-acetyl)galactopyranoside (1), kaempferol 3-O-beta-(2' '-acetyl)galactopyranoside-7-O-alpha-arabinopyranoside (2), and quercetin 3-O-beta-(2' '-acetyl)galactopyranoside-7-O-alpha-arabinopyranoside (3)-were isolated from the flowers of Aconitum paniculatum. Their structures were elucidated by 1D and 2D NMR studies ((1)H-(1)H COSY, HSQC, HMBC) as well as by HPLC-MS.

Topical anti-inflammatory activity of Bauhinia tarapotensis leaves.

The topical anti-inflammatory properties of Bauhinia tarapotensis Benth. (Leguminosae) leaves have been studied by the inhibition of the croton oil-induced ear edema in mice. A bioassay-guided fractionation showed an interesting anti-inflammatory activity of the chloroform extract, that justifies the activity of the whole herbal drug. The main anti-inflammatory principles of B. tarapotensis leaves are triterpenic acids of ursane and oleanane series. The antiphlogistic activity of mixtures constituted of two ursane and oleanane isomers with different hydroxylation pattern, in the ratio 2:1, is comparable to that of indomethacin (ID50 ranging from 95 to 147 microg/cm2 and 93 microg/cm2, respectively).