bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effects of essential oils from certain Ziziphora species on swimming performance in mice
Authors: Öztürk Yusuf , Aydm Süleyman , Tecik Bahar , Başer K. Hüsnü Can 
Published: October 2006

AbstractIn Turkish folk medicine, Ziziphora species have been used as an infusion for various purposes such as for the sedative, stomachic, carminative, activities etc. Since some of the folkloric uses may be related to antistress (adaptogenic) activity or central nervous system depression, the effects of essential oils obtained from Z. tenuior, Z. taurica ssp. taurica and Z. taurica ssp. cleonioides on mice swimming performance were investigated. Acute lethal toxicities of these three Ziziphora oils were also studied. On the basis of our findings obtained, these essential oils from the Ziziphora species decreased the swimming time suggesting a central nervous system depressant activity.
Effects of leaf and root extracts of Nauclea latifolia on purinergic neurotransmission in the rat bladder
Authors: Udoh Francis V. 
Published: October 2006

AbstractThe leaf and root parts or their combination of Nauclea latifolia were separately extracted and their pharmacological effects on purinergic transmission in the bladder investigated. The leaf extract was very potent in potentiating purinergic neurotransmission by potentiating ATP induced contractions. These actions were more pronounced than the depression of potassium chloride evoked contraction of the bladder. The root extract depressed purinergic contraction of the bladder by a direct depressant action on the bladder smooth muscle since it did not modify ATP induced contractions. The leaf and root extracts antagonized each other when combined together. It is concluded that the leaf and root extracts of N. latifolia possess interesting pharmacological actions on the bladder.
Antiviral activity of Achyrocline flaccida Wein DC aqueous extract
Authors: Garcia G. , Cavallaro L. , Broussalis A. , Ferraro G. , Martino V. , De Torres R. , Coussio J. , Campos R. 
Published: October 2006

AbstractAqueous extracts (AE) of chyrocline flaccida exhibit true antiviral activity in vitro against different members of the Herpesvirus family (herpes simplex virus type 1 and 2, human cytomegalovirus, bovine herpesvirus and lower activity with pseudorabies virus). The extract had no activity against some RNA (naked and enveloped) viruses and adenoviruses. The extract was not virucidal but its antiviral index (AI) was sufficiently high to justify further analysis. A preliminary characterization indicates that an early step of viral replication was affected by the aqueous extract.
Biological screening of Italian medicinal plants for antibacterial activity
Authors: Izzo A. A. , di Carlo G. , Biscardi D. , de Fusco R. , Mascolo N. , Borrelli F. , Capasso F. , Fasulo M. P. , Autore G. 
Published: October 2006

AbstractSome 68 plant extracts from 65 species belonging to 25 families were investigated for antibacterial activity against eight gram‐positive and gram‐negative bacteria. Of the 68 extracts, 64 (94.1%) exhibited inhibitory effects against one or more microorganisms. Furthermore, among the active extracts, 12 from 11 species exhibited a broad spectrum of activity. Discussion on the probable chemical components responsible for this activity is included.
Pharmacological evaluation of the dichloromethanol extract from Inula crithmoides L.
Authors: Barrachina M. D. , Bello R. , Esplugues J. , Sanz I. , Yúfera E. Primo 
Published: October 2006

AbstractThe pharmacological effect of the dichloromethanol extract of Inula crithmoides L. was analysed in in vitro and in vivo models. The extract dose‐dependently decreased arterial blood pressure and furthermore it showed low acute toxicity, CNS depressor activity and analgesic and antiinflammatory effects. Preincubation of the guineapig ileum and rat duodenum (100 μg/mL) produced a significant reduction in the contractile effects of histamine and acetylcholine and a concentration‐related inhibition of the effects of serotonin. Following further fractionation the methylene chloride/acetone (50/50) fraction caused a significant decrease in motor activity and significantly reduced the threshold of pain chemical stimulus.
Antibacterial activity of diosquinone and plumbagin from the root of Diospyros mespiliformis (Hostch) (Ebenaceae)
Authors: Lajubutu B. A. , Pinney R. J. , Roberts M. F. , Odelola H. A. , Oso B. A. 
Published: October 2006

AbstractDiosquinone and plumbagin isolated from the root of Diospyros mespiliformis (Hostch), a common Ingredient in several folk medicines and foods, have been shown to have antibacterial activity against a wide range of organisms. The minimum inhibitory concentrations (MICs) of diosquinone against Staphylococcus aureus NCTC 6571 and S. aureus E3T ranged from 3 to 30 μg/mL, while those against Escherichia coli KL16 and Pseudomonas aeruginosa NCTC 6750 ranged from 15 to 16 μg/mL. MICs were found to increase with the concentration of cells used in the inoculum. Bacterial studies showed that S. aureus NCTC 6571 exhibited a paradoxical biphasic response to dioquinone in nutrient broth, whereas bacterial activity against E. coli KL16 increased with concentration up to the highest concentration of dioquinone tested. Activity against E. coli KL16 was more pronounced in phosphate‐buffered saline than in nutrient broth.
The immunomodulatory effect of saikosaponin derivatives and the root extract of Bupleurum kaoi in mice
Authors: Yen Ming‐Hong , Lin Chun‐Ching , Yen Chuan‐Min 
Published: October 2006

AbstractThe saikosaponins ‐a(SSa), ‐d(SSd), ‐f(SSf), crude saponin mixture (CSM) and H2O‐layer components (HLC) which were isolated from the root of Bupleurum kaoi Liu, Chao et Chuang (Umbelliferae), demonstrated an immunomodulatory effect. Mice of the BALB/c strain were injected peritoneally with drugs to assess immune responses weekly over a 4 week period. The results showed that the mean ratio of thymus weight to body weight increased during week 1 but declined gradually thereafter; the ratio of helper T‐cells to suppressor T‐cells (Th/Ts) from mice treated with SSf and HLC gradually increased; however, in mice treated with SSa, SSd and CSM, the ratio rose to a maximum at week 3 and then decreased; the IL‐2 level of treated mice was significantly higher than that of the control group throughout the test period; the ratio of spleen weight to body weight in all drug treated groups increased weekly; the activity of B‐cell stimulation in mice was promoted week by week; levels of IgA, IgG and IgM in serum of SSd and SSa treated animals increased. An in vitro study, involving stimulation of IL‐1 demonstrated the following order of potency: SSd<SSa, 23‐O‐AcSSa and CSM<SSf and HLC.
In vitro and in vivo antimalarial activity of cryptolepine, a plant‐derived indoloquinoline
Authors: Kirby G. C. , Paine A. , Warhurst D. C. , Noamese B. K. , Phillipson J. D. 
Published: October 2006

AbstractCryptolepine is an indoloquinoline, high yields of which may be extracted from the roots of the West African shrub Cryptolepis sanguinolenta. The use of this plant as a traditional treatment for malaria is widespread in Ghana and is reported to be clinically effective. We have tested cryptolepine for in vitro antiplasmodial activity against the multidrug resistant (K1) strain of Plasmodium falciparum and found it to be highly active with an IC50 value of 0.031±0.0085 (SE) μg/mL, equivalent to 0.134±0.037 μM (n = 3). In a 4‐day suppression test there was, however, no significant reduction in parasitaemia in P. berghei‐infected mice treated subcutaneously with cryptolepine (7–113 mg/kg/d×4), when compared with untreated controls. Like 9‐aminoacridine, this compound appears to intercalate with DNA and this may explain the high degree of antimalarial activity demonstrated in vitro.
Antiinflammatory activity and effects on isolated smooth muscle of extracts from different Teucrium species
Authors: Barrachina M. D. , Bello R. , Martínez‐Cuesta M. A. , Esplugues J. , Primo‐Yúfera E. 
Published: October 2006

AbstractThe present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan‐induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti‐inflammatory effect through the 24 h experimental period and reduced the Emax induced by histamine and serotonin in vitro on guinea‐pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and noradrenaline on rat vas deferens. The methanol extracts of T. pumillum (50 mg/kg, i.p.) and T. buxifolium (26 mg/kg, i.p.) exhibited significant antiinflammatory effects only in the acute phase of the oedema (2 h) without affecting the chronic phase (24 h). In guinea‐pig ileum, rat uterus and rat vas deferens, the methanol extract of T. pumillum reduced the maximal effect induced by histamine, serotonin and noradrenaline, respectively, whereas the methanol extract of T. buxifolium lacked any effect on the contractile activity induced by various agonists in vitro. When tested for antiinflammatory activity the methanol (200 mg/kg, i.p.) and dichloromethanol (200 mg/kg, i.p.) extracts of T. cartaginenses did not modify the oedematous response induced by carrageenan administration.
Effects of flavonoids on cytochrome P‐450 from rat liver microsomes: Inhibition of enzyme activities and protection against peroxidative damage
Authors: Ubeda A. , Esteve M. L. , Alcaraz M. J. , Cheeseman K. H. , Slater T. F. 
Published: October 2006

AbstractA series of flavonoids, able to inhibit non‐enzymic and enzymic lipid peroxidation, were investigated as inhibitors of cytochrome P‐450 mediated reactions (aminopyrine N‐demethylation and aniline hydroxylation) in rat liver microsomes. The most potent compounds were chrysin, luteolin, amentoflavone and eriodictyol (aminopyrine N‐demethylation) and apigenin, kaempferol and quercetin (aniline hydroxylation). Some structure‐activity relationships were established for inhibition of aminopyrine N‐demethylation and it was observed that the resorcinol configuration of the ring A is a determinant feature, whereas O‐glycosylation abolished the activity. Most of the compounds showed lower activity on aniline hydroxylation. The presence of these flavonoids during incubation of microsomes in a medium containing NADPH did not modify the cytochrome P‐450 concentration and protected against lipid peroxidation induced degradation of this cytochrome.
Investigation of korean plant extracts for potential phytotherapeutic agents against B‐virus hepatitis
Authors: Chung T. H. , Kim J. C. , Kim M. K. , Choi S. C. , Kim S. L. , Chung J. M. , Lee I. S. , Kim S. H. , Hahn K. S. , Lee I. P. 
Published: October 2006

AbstractThe present study was undertaken to identify potential phytotherapeutic agents among the aqueous extracts of 151 herbal medicinal plants of Korea. Extracts were assayed for (1) binding potency to hepatitis B‐virus surface antigen (HBsAg), and (2) inhibition of serum hepatitis B‐virus DNA polymerase activity. Of the 151 aqueous plant extracts tested, 33 demonstrated a positive precipitation reaction with HBsAg+ serum, and 15 of these specifically bound HBsAg in serum as well as recombinant HBsAg (Hepavax®). Nine extracts competitively inhibited >80% of anti‐HBsAg antibody binding to Hepavax® HBsAg. Furthermore, nine of these 15 plant extracts also exhibited greater than 25%—50% inhibition of hepatitis B‐virus (HBV) DNA polymerase activity, and also significantly stimulated production of the potent cytokine, tumour necrosis factor (TNF). None of the extract concentrations used altered liver function parameters of normal rats.
Wound healing effects ofAloegel and other topical antibacterial agents on rat skin
Authors: Heggers John P. , Kucukcelebi Ahmet , Stabenau Catherine J. , Ko Francis , Broemeling Lyle D. , Robson Martin C. , Winters Wendell D. 
Published: October 2006

AbstractThe effects of topical antibacterials were studied in an acute wound healing model. Sprague‐Dawley rats after appropriate anaesthesia received four 1.5 cm2dorsal defects through the skin and panniculus carnosus. Skin defects were treated for 14 days with 2% mupirocin ointment, 1% clindamycin cream, 1% silver sulfadiazine cream +Aloe veragel, and silver sulfadiazine combined withAloegel. An untreated group served as controls. Each group was comprised of 10 animals each to achieve statistical significance. Wound closure rate was assessed by serial planimetry. Following healing, the breaking strength of each resultant scar was determined. Wound half‐lives and overall healing rates were calculated by regressing the log of the areas of all wounds over time. Overall healing rates of all the treated groups were significantly different compared with control group (p<0.05). TheAloegroup had the shortest half‐life and healed faster than the control group. All the other treated groups had no longer half‐lives when compared with the control group. While silver sulfadiazine +Aloeincreased the breaking strength of the healed wound,Aloealone did not, but demonstrated an increase over the control. TopicalAloesignificantly enhances the rate of wound healing and when combined with silver sulfadiazine reverses the wound retardant effect observed with silver sulfadiazine. Clindamycin and mupirocin significantly delay wound closure. However mupirocin enhanced the breaking strength of the wound.
Effects of antiinflammatory plant extracts on ovoimplantation in rats
Authors: Rao V. S. N. , Silva J. C. R. , Medeiros F. C. 
Published: October 2006

AbstractThe effects of five antiinflammatory plant extracts on ovoimplantation was investigated in albino rats. Rats treated with plant extracts from days 4 to 6 (periimplantation) of pregnancy showed either a total absence (20%–40%) or a considerably reduced number of implantations in utero. The observation suggests that the use of antiinflammatory plant extracts during the periimplantation period impairs fertility probably by reducing the vascular permeability which is an obligate accompaniment of normal implantation.
Hypoglycaemic activity of Nelumbo nucifera gaertn. (Fam. Nymphaeaceae) rhizome (methanolic extract) in streptozotocin‐induced diabetic rats
Authors: Mukherjee Pulok Kumar , Pal Saroj K. , Saha Kakali , Saha B. P. 
Published: October 2006

AbstractThe hypoglycaemic effect of the rhizome extract of Nelumbo nucifera was studied in streptozotocin‐induced diabetic rats. A methanol extract of the plant obtained by soxhlet extraction from finely pulverized rhizomes was used. The LD50 of the extract was found to be 2 g/kg. The extract (300 mg/kg and 600 mg/kg, orally) caused a reduction of blood glucose levels in streptozotocin‐induced diabetic rats by 53% (p<0.001) and 55% (p<0.001) respectively at the end of 12 h. The results of this study indicate that the methanol extract of the rhizome possesses favourable hypoglycaemic activity in hyperglycaemic animals taking chlorpropamide as a standard.
Castanospermine, an HIV inhibitor from tissue cultures of Castanospermum australe
Authors: Roja G. , Heble M. R. 
Published: October 2006

AbstractTree species are important sources of phytotherapeutics. The seeds of the tree Castanospermum australe contain alkaloids effective against HIV. Unorganized callus cultures were established from the leaves of the mature tree on a chemically defined nutrient medium of Murashige and Skoog supplemented with 2,4‐dichlorophenoxyacetic acid and benzyladenine. The alkaloids were separated and identified by gas liquid chromatographic analysis. The cultures synthesized castanospermine (0.004% F.W.) indicating that the biosynthetic ability of the highly differentiated seeds of the tree is expressed in the unorganized cells.
Effects of Sclerocarya birroea Hochst. extract on some metabolic activities in the rat
Authors: Trovato A. , Kirjavainen S. , Galati E. M. , Forestieri A. M. , Iauk L. 
Published: October 2006

AbstractThe decoction of Sclerocarya birroea Hochst. shows hypoglycaemic effects, an increase in plasma IRI in normal rats and an incremented oral‐glucose tolerance. The decoction is also active against diet‐induced hypercholesterolaemia.
Catechols and quercetin reduce MTT through iron ions: A possible artefact in cell viability assays
Authors: Habtemariam Solomon 
Published: October 2006

AbstractThe reduction of MTT (d‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) by mitochondrial enzymes to its blue formazan product is a widely used colorimetric assay method to determine the viability of cells in culture. In the present study the reduction of MTT by several agents in the absence of living cells was investigated. Several catechols and the flavonoid quercetin were found to reduce MTT in serum‐supplemented Dulbecco's modified Eagle's medium. All the agents tested failed to reduce MTT in Hank's balanced salt solution, but supplementing this buffer with serum or iron ions resulted in MTT reduction. The involvement of an iron‐catalysed redox reaction in the reduction of MTT induced by catechols and flavonoids was demonstrated. Caution is needed in using MTT in cell viability assays involving such chemicals.
Free Wilson Analysis. Theory, Applications and its Relationship to Hansch Analysis
Authors: Kubinyi Hugo 
Published: October 2006

AbstractThe Free Wilson model is a simple and efficient method for the quantitative description of structure activity relationships. It is the only numerical method which directly relates structural features with biological properties, in contrast to Hansch analysis, where physicochemical properties are correlated with biological activity values. Nevertheless both approaches are closely interrelated, not only from a theoretical point of view, but also in their practical applicability. In many cases both models can be combined to a mixed approach which includes Free Wilson type parameters to describe the activity contributions of certain structural modifications and physicochemical parameters to describe the effect of some other substituents on the biological activity. Many successful applications, especially from the work of Hansch and his group on the structure activity relationships of enzyme inhibitors, demonstrate that this combined model is the most powerful tool of classical QSAR.
Qualitative and Quantitative Structure‐Activity Relationships for Calcium Channel Modulating 1,4‐Dihydropyridine Derivatives: A Hypothetical Molecular Receptor Model
Authors: Höltje Hans‐Dieter , Marrer Stephan 
Published: October 2006

AbstractBased on force field methods, quantum chemical calculations and using molecular graphics a hypothetical receptor model for calcium antagonists and agonists from the 1,4‐dihydropyridine (DHP) series has been developed. In a previous study it could be shown, that calcium channel activating DHP's reduced the molecular electrostatic receptor potential, while this is increased by calcium channel blocking DHP's. These effects offer a possible explanation for the opposite behaviour of chiral dihydropyridines. In continuation of this work a quantitative structure‐activity study with a group of calcium channel blockers provided a three binding site model for the drug receptor interaction. Calculated interaction energies correlate well with biological potencies (r = 0.94, s = 0.28). The postulated receptor model shows structural similarities to segments of the very recently published amino acid sequence of the receptor for 1,4‐dihydropyridine calcium channel blockers.
The Effect of Molecular Structure on the Distribution and Elimination of Some Organic Acids in Rats
Authors: Lázniček Milan , Kvêtina Jaroslav 
Published: October 2006

AbstractThe pharmacokinetics and distribution of nine model acidic drugs (iodobenzoic, iodophenylacetic and iodohippuric acid derivatives) in rats were investigated following intravenous injection. The distribution volume of the central compartment increases linearly with increasing free drug fraction in plasma. Relatively weaker correlations were found between the distribution volume at steady‐state and lipophilicity or plasma protein binding. Even when a statistically relevant correlation between total plasma clearance and lipophilicity was found, this relation expresses rather the difference between individual acids. Comparing the individual position isomers, substitution of the aromatic ring with iodine in the para position leads to a strong decrease in the total plasma clearance value in contrast to a change in their lipophilicity. It shows that the total plasma clearance value is dependent not only on the lipophilicity, but on the geometry of drugs under study as well.
Viscosimetric Evaluation of Solvent Effects. II. Determination of the Range of the Applicability of the Method
Authors: Batko Anna , Mazurkiewicz Józef , Tomasik Piotr 
Published: October 2006

AbstractThe intrinsic viscosities of solutions of a naphthalene derivative series i.e. quinoline, isoquinoline, 2‐methoxynaphthalene, 2‐naphthyl acetate, 1‐nitronaphthalene, 1‐naphthol and 2‐naphthol were determined in a series of aromatic solvents like benzene, toluene, anisole, pyridine, chlorobenzene and nitrobenzene. These magnitudes were correlated with various parameters which characterize solvents and solvent – solute interactions, the Lewis acidity and basicity, the Kirkwood function, the dipol moment, the molar polarizability, the function of polarizability as well as the Večeřa parameters. The polar solvation seems to be the predominating component of the solvent – solute effect in the case of quinoline, isoquinoline, 2‐methoxynaphthalene and 2‐naphthyl acetate whereas other factors become more important in case of the remaining compounds studied. The viscosimetric method appears to be suitable for the quantitative study of the solvent effect even if mainly Van der Waals forces are involved in the solvent – solute interactions and molecular weight of solute reaches hardly about 130 a.m.u.
Principal Properties for Aromatic Substituents. A Multivariate Approach for Design in QSAR
Authors: Skagerberg Bert , Bonelli Daniela , Clementi Sergio , Cruciani Gabriele , Ebert Cynthia 
Published: October 2006

AbstractA set of a hundred aromatic substituents were multivariately characterized by nine descriptor variables taken from the literature. From the 9*100 data set were calculated four principal properties for the aromatic substituents as the four first dimensions in a principal components analysis, PCA. The first three principal properties were used to develop a strategy for selecting substituents from eight subgroups according to a factorial design.