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Phytochemical and pharmacological studies on the acetonic extract of Marrubium globosum ssp. libanoticum.

A new natural labdane diterpene, marrulibanoside, was isolated from the acetonic extract of aerial parts of M. globosum Montbr. et Auch. ex Benth. ssp. libanoticum Boiss. (Lamiaceae). Its structure was determined by spectroscopic methods such as 1D and 2D NMR and mass spectrometry. Pharmacological studies have shown that the extract of M. globosum exerts anti-inflammatory effects in the rat paw oedema induced by carrageenin resulting in reduced paw swelling. This activity, which seems due to marrulibanoside, is a consequence of iNOS and COX-2 activities inhibition.

Animals↗

Influence of the obligate parasite Cuscuta campestris on growth and biomass allocation of its host Mikania micrantha.

As a means of biologically controlling Mikania micrantha H.B.K. in South China, the influence of the obligate parasite Cuscuta campestris Yuncker on its growth and biomass allocation was studied using pot trials. The effect of C. campestris on M. micrantha became greater with time, such that the host biomass was only 1.8% of the control after 60 d of parasitism and by day 72 almost all the aerial parts of the host plants had died. Afterwards, the hosts and the remnant parasite shoots re-grew but the total biomass of the hosts was still significantly lower than that of the controls. The infection by C. campestris greatly increased the shoot:root dry weight ratio and the allocation to stems of the infected plants from 40 to 50 d after parasitization, but decreased their relative growth rate and unit leaf rate starting from 20 d after parasitization and their leaf area ratio from 30 to 60 d after parasitization. Cuscuta campestris significantly reduced the total biomass, changed the biomass allocation patterns, and completely inhibited the flowering of the infected M. micrantha plants. These results indicate that the use of C. campestris could be a potentially effective way of controlling M. micrantha.

Asteraceae↗

Antifungal activity of some Brazilian Hypericum species.

Crude methanolic extracts and fractions from the aerial parts of seven species of Hypericum (H. caprifoliatum Cham. and Schltdl., H. carinatum Griseb., H. connatum Lam., H. ternum A. St.-Hil., H. myrianthum Cham. and Schltdl., H. piriai Arechav. and H. polyanthemum Klotzsch ex Reichardt) growing in southern Brazil were analyzed for their in vitro antifungal activity against a panel of standardized and clinical opportunistic pathogenic yeasts and filamentous fungi, including dermatophytes, by the agar dilution method. Chloroform and hexane extracts of H. ternum showed the greatest activity among extracts tested.

Antifungal Agents↗

Anti-inflammatory and anti-nociceptive activities of Pluchea quitoc (DC.) ethanolic extract.

Pluchea quitoc DC. (Asteraceae), a plant widely distributed throughout Brazil and popularly known as "quitoco", "madre-cravo" or "tabacarana", is used in traditional medicine for the treatment of inflammation, as well as of digestive and respiratory diseases. The anti-inflammatory and anti-nociceptive activities of the ethanolic extract (EE) from aerial parts of this plant were evaluated in mice and rats. Oral treatment with the EE (1-2g/kg, p.o.) decreased the paw oedema induced by carrageenan in rats, showed anti-nociceptive effects on the tail-flick test and on acid-induced writhing in mice, and inhibited both phases of pain (neurogenic and inflammatory) of the formalin test in rats. Topical application (EE 1.25, 2.5 and 5.0mg) inhibited the ear oedema induced by croton oil in mice. The results support the folkloric use of the plant in inflammatory processes.

Acetic Acid↗

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↗

Dual inhibition of cyclooxygenase-1 and 5-lipoxygenase by aerial part of Bupleurum fruticescens methanol extract.

The effect of the methanol extract from aerial parts of Bupleurum fruticescens on the release of eicosanoids and hydrolytic enzymes was determined on in vitro cell systems. The extract had a significant effect on 5-lipoxygenase (5-LOX) activity, inhibiting both LTB4 and 5(S)-HETE production with IC50 values of 112 microg/ml and 95 microg/ml, respectively. At concentrations of 200 microg/ml, the extract also inhibited cyclooxygenase-1 (90%) and elastase activities (54%). The 12-LOX activity in intact platelets was not affected; a fact, which suggests that phospholipase A2 (PLA2) activity, is not modified by the extract.

Animals↗

Fascinating metabolic pools of Pelargonium sidoides and Pelargonium reniforme, traditional and phytomedicinal sources of the herbal medicine Umckaloabo.

The metabolic pools of Pelargonium sidoides DC and Pelargonium reniforme CURT, associated with the origin of the herbal medicine Umckaloabo, exhibit remarkable diversity and complexity. They comprise a variety of phenolic and polyphenolic compounds, a notable wealth of highly oxygenated simple coumarins and a number of miscellaneous uncommon metabolites. Noteworthy, the roots of both species express conspicuously distinct coumarin variations that facilitate their identification. Of the range of coumarins identified the titled species shared the ubiquitous scopoletin and the unique members 6,7,8-trihydroxycoumarin and 8-hydroxy-5,6,7-trimethoxycoumarin merely. Furthermore, the current data on the coumarin profiles suggest the occurrence of coumarin sulphates and coumarin glycosides to be apparently confined to P. sidoides, while the occurrence of conventional proanthocyanidins was a common chemical feature. An unprecedented diterpene, designated as reniformin, was encountered in the roots of P. reniforme, possessing a novel diterpene skeleton linked to a unique p-oxyphenethansulfonic moiety. Coumarins were less abundant in the aerial parts of both species. These were rich in flavonoids and hydrolysable tannins including a unique series of O-galloyl-C-glucosylflavones (P. sidoides and P. reniforme) and novel ellagitannins with a (1)C(4) glucopyranose core in P. reniforme, trivially named pelargoniins, accompanied by the new 4-allyl-2,5-dimethoxyphenol-1-beta-D-glucoside. These Pelargoniums have thus represented an attractive source of fascinating secondary metabolites. A proprietary extract of the roots of P. sidoides, EPs 7630, has been developed from this traditional herbal medicine and introduced into modern phytotherapy in Europe. Structural examination of EPs 7630 constituents showed excellent agreement of the profile with that of P. sidoides.

Coumarins↗

A mechanical analysis of the relationship between free oscillations of Pinus pinaster Ait. saplings and their aerial architecture.

The aim of this study was to investigate the influence of aerial architecture on the dynamic characteristics of young maritime pines (Pinus pinaster Ait.) using a mechanistic approach. For this purpose, three 4-year-old saplings with prominent differences in their branching patterns were submitted to free oscillation tests. The tests were carried out with different methods and directions of mechanical loading in order to initiate the movement of each sapling. The oscillations of the different architectural elements, i.e. stem and branches of different topological order, were measured with inclinometers and strain gauges fixed to saplings. Successive pruning of the architectural elements was carried out to evaluate their relative influence on the dynamic characteristics of the trees. The aerial systems were digitized before the mechanical tests in order to use 3D visualization techniques and to make architectural analyses of the crown structure. Two distinct modes of deformation were detected during free oscillations. The natural swaying frequency ranged from 0.6-0.8 Hz for the saplings tested at the same period of the year. The frequency variations were partly explained by the morphological differences of the experimental subjects. The motions of the axes were found to depend on their topology, i.e. the movement of the axes of a given branching order was forced by the movement of their respective bearing axis. The axes of third branching order had a significant and negative effect on the damping of the natural deformation mode. Results point out the major role played by foliage, qualitatively and quantitatively, on the damping of tree motions and on coupling the motions of the crown components.

Biomechanical Phenomena↗

Anti-anxiety activity studies of various extracts of Turnera aphrodisiaca Ward.

Turnera aphrodisiaca Ward (Turneraceae) has been used traditionally for treatment of anxiety neurosis and as an aphrodisiac. Yet, the plant has never been subjected to systematic biological investigation. In the present investigation, petroleum ether (60-80 degrees C), chloroform, methanol, and water extracts of T. aphrodisiaca aerial parts were evaluated for anti-anxiety activity in mice using elevated plus-maze apparatus. Among all the extracts, only methanol exhibited significant anti-anxiety activity at a dose of 25 mg/kg with respect to control as well as standard (diazepam, 2 mg/kg). The bioactive methanol extract was shaken with petroleum ether, chloroform, and n-butyl alcohol, and all the shakings as well as the remaining methanol extract (RME) were further evaluated for anxiolytic activity. Butanol fraction and RME were found to exhibit anxiolytic activity in mice at the dose of 10 mg/kg and 75 mg/kg, respectively.

Administration, Oral↗

Hypoglycaemic effect of Calamintha officinalis Moench. in normal and streptozotocin-induced diabetic rats.

The purpose of this study was to investigate the effects of a water extract from the aerial parts of Calamintha officinalis Moench., after either a single dose or daily oral administration for 15 days, on plasma blood glucose concentrations and basal insulin levels in normal and streptozotocin-induced diabetic rats (STZ diabetic rats). The results clearly demonstrated the hypoglycaemic effect of this plant extract in both normal and STZ diabetic rats. In addition, no changes were observed in basal plasma insulin concentrations after treatment with this plant in normal or STZ diabetic rats, indicating that the underlying mechanism of the plant's pharmacological action seems to be independent of insulin secretion. We conclude that the aqueous C. officinalis extract exhibits a significant hypoglycaemic effect in normal and STZ diabetic rats without affecting basal plasma insulin concentrations, and supports, therefore, its traditional use by the Moroccan population.

Animals↗

Phytochemical constituents of Cirsium setidens Nakai and their cytotoxicity against human cancer cell lines.

Five terpenes (1-5), three fatty acids (6-8), two sterols (9 and 11), and a monogalactosyldiacyl glycerol (10) were isolated from the methylene chloride extract of the aerial part of Cirsium setidens. Their chemical structures were determined to be alpha-tocopherol (1), 25-hydroperoxycycloart-23-en-3beta-ol (2), 24-hydroperoxycycloart-25-en-3beta-ol (3), mokko lactone (4), transphytol (5), 9,12,15-octadecatrienoic acid (6), 9,12-octadecadienoic acid (7), hexadecanoic acid (8), acylglycosyl beta-sitosterol (9), (2R)-1,2-O-(9z,12z,15z-dioctadecatrienoyl)-3-O-beta-D-galactopyranosyl glycerol (10) and beta-sitosterol glucoside (11) by spectral evidences. Compound 3 exhibited significant cytotoxic activity against five human cancer cell lines with its ED50 values ranging from 2.66 to 11.25 microM.

Cirsium↗

Inhibition of intestinal motility and secretion by extracts of Epilobium spp. in mice.

Ethanol extracts of the fresh aerial parts of various Epilobium species were tested to elucidate the mechanism of their gastrointestinal activity in animals. The methods of charcoal meal, castor oil-induced diarrhoea, and enteropooling assay were used to evaluate their effect on mouse gut at various dose levels. The extracts were found to have a significant activity in all models. Moreover, the extracts resulted to possess very little toxicity. Thus, it can be concluded that Epilobium possesses anti-diarrhoeal, anti-motility, and anti-secretory activities and can prove beneficial in the treatment of gastrointestinal disorders.

Animals↗

Chemical constituents of Euphorbia marschalliana Boiss.

Acetone extract of aerial parts of Euphorbia marschalliana collected from Iran has been subjected to different chromatography techniques for fractionation and purification. The stereo-structures of the myrsinol esters 15-O-acetyl-3-O-propionyl-5-O-butanoyl-7-O-nicotinoylmyrsinol (1) and 15-O-acetyl-3,5-O-dibutanoyl-7-O-nicotinoylmyrsinol (2) have been probed using ROESY spectroscopy and modified for the stereochemistry at C-6, C-12 and C-13. Beta-sitosterol (3), 29-norcycloart-5-ene (4), 5,8-lanostadiene-3beta-ol (5), 3beta,24(S),25-trihydroxycycloartane (6), 3beta,24(R),25-trihydroxycycloartane (7) and 24-methylenecycloartan-3beta-ol (8) were identified for the first time in this plant.

Acetone↗

Cytotoxic constituents of Achillea clavennae from Montenegro.

Examination of the aerial parts of Achillea clavennae afforded eight guaianolides (1-8), three bisabolenes (9-11), four flavonols (12-15), sesamin (lignan) and isofraxidin (coumarin). The structures of the new compounds (2, 4, 5, 7 and 10) were determined by spectroscopic methods. The antiproliferative action of 2, 8, 9 and 12 were tested to HeLa, K562 and Fem-X human cancer cell lines. Guaianolides 2 (9alpha-acetoxyartecanin) and 8 (apressin) showed significant cytotoxic effects to all tested lines and inducumenone (9) exhibited a moderate activity. The most active was flavonol centaureidin (12), already known as cytotoxic compound.

Achillea↗

In vitro antiplasmodial activity of abietane and totarane diterpenes isolated from Harpagophytum procumbens (devil's claw).

The development of drug resistance and resurgence of malaria has highlighted the need for new chemically diverse antimalarial drugs. This study investigates Harpagophytum procumbens DC. as a source of antiplasmodial hit compounds. The roots of wild harvested plants as well as the aerial sections, seeds and roots of cultivated H. procumbens were evaluated for in vitro antiplasmodial activity. Bioassay-guided fractionation of the petroleum ether root extract yielded two diterpenes, (+)-8,11,13-totaratriene-12,13-diol (1) and (+)-8,11,13-abietatrien-12-ol (2). Compounds 1 and 2 displayed significant (IC50 < 1 microg/mL) in vitro antiplasmodial activity against a chloroquine-resistant (K1) and -sensitive (D10) strain of Plasmodium falciparum, and low cytotoxicity (SI > 65) against two mammalian cell lines (CHO and HepG2). It was found that 1 and 2 did not modify the erythrocyte shape, which in conjunction with the cytotoxicity results, indicates selective antiplasmodial activity.

Animals↗

Neuropharmacological profile of Barleria lupulina Lindl. Extract in animal models.

Barleria lupulina Lindl. is a popular medicinal plant distributed in mountains of southern and western India. In the present work, the effect of methanolic extract of aerial parts of B. lupulina on CNS activity has been evaluated. The CNS activity was tested in several experimental models, in mice and rats: general behavior, exploratory behavior, muscle relaxant activity, conditioned avoidance response and phenobarbitone sodium-induced sleeping time tests. The aerial parts of the plant B. lupulina was extracted with methanol and the solvent was removed by vacuum distillation. The methanol extract (100, 200 and 300 mg/kg) showed reduction in general behavioral pattern (spontaneous activity, alertness, awareness, pain response and touch response) in a dose dependent manner. The extract was found to produce a significant reduction of the exploratory behavioral profile (Y-maze test, head dip test) and conditioned avoidance response with all the tested doses. The methanolic extract showed significant motor incoordination and muscle relaxant activity. The extract also potentiated phenobarbitone sodium induced sleeping time. Preliminary investigation showed that the methanol extract of B. lupulina has significant psychopharmacological activity.

Acanthaceae↗

Mitogenic and comitogenic activities of polysaccharides from some European herbaceous plants.

From the leaves of Plantago lanceolata, the green parts of Rudbeckia fulgida, the aerial parts of Salvia officinalis and the roots of Valeriana officinalis, crude polysaccharides have been isolated by extraction with water and further purified and fractionated by various techniques. The water-soluble polysaccharides obtained were examined for their immunomodulatory activities using the in vitro mitogenic and comitogenic rat thymocyte tests. The results indicate that in spite of the considerable differences in chemical composition and structural properties, the tested polysaccharides exhibited similar significant immunomodulatory properties with a particularly high adjuvans activity in the case of the Rudbeckia and Salvia polysaccharides. The pectic polysaccharide-rich complex from Valeriana was shown to also stimulate the immune function of bone marrow cells.

Adjuvants, Immunologic↗

ci21A/Asr1 expression influences glucose accumulation in potato tubers.

Asr genes are exclusively found in the genomes of higher plants. In many species, this gene family is expressed under abiotic stress conditions and during fruit ripening. The encoded proteins have nuclear localisation and consequently a transcription factor function has been suggested. Interestingly, yeast-one-hybrid experiments revealed that a grape ASR binds to the promoter of a hexose transporter gene (VvHT1). However, the role of these proteins in planta is still elusive. By using a reverse genetics approach in potato we found that modification of Asr1 expression has no incidence on the aerial phenotype of the plant but exerts a dramatic effect in tuber. Asr1 antisense potatoes displayed decreased tuber fresh weight whereas Asr1 overexpressors had a diminished number of tubers. Moreover, overexpression lines showed lower transcript levels of a plasma membrane hexose transporter and a concomitant decrease in glucose content in parenchyma cells of potato tubers. On the same hand glucose uptake rate was also reduced in one of the overexpressing lines. It thus seems likely that Asr1 is involved in the control of hexose uptake in heterotrophic organs. In addition, the transgenic plants were characterized by several other changes in steady state metabolite levels. Results presented here support a role for ci21A/Asr1 in glucose metabolism of potato tuber.

DNA Primers↗