bluuebunny/crossref_metadata_2025_split huggingface dataset:
Antiinflammatory, antitumour and antifertility effects in rodents of two nor‐cucurbitacin glucosides from Wilbrandia species
Authors: Almeida F. R. C. , Rao V. S. N. , Matos M. E. O. 
Published: October 2006

AbstractThe purified fraction (PF) of the rhizome of Wilbrandia sp. (Cucurbitaceae) that contained two nor‐cucurbitacin glucosides (WG1 and WG2) demonstrated potent antiinflammatory, antitumour and antifertility effects in rats and mice at oral doses ranging from 50 to 200 mg/kg. In rat, it significantly inhibited carrageenan‐induced hind paw oedema and granulomatous lesion, while in mice the increased vascular permeability induced by acetic acid was markedly reduced. The PF exhibited an antitumour effect in rats bearing Walker 256 carcinosarcoma and also demonstrated cytotoxic action against KB cells in vitro. In regularly cycling mice, PF treatment suppressed the incidence of the oestrus phase of the reproductive cycle suggesting a possible antiovulatory effect. The rats that received PF from days 1 to 7 of pregnancy showed either a total absence or a reduced number of implantations in utero. The PF failed to exhibit abortifacient, oestrogenic or antioestrogenic actions. The results indicate that the nor‐cucurbitacin glucosides of Wilbrandia sp. possess a novel spectrum of pharmacological activity different from that of cucurbitacins described earlier from other plants of this family.
Oligo‐ and macrocyclic diterpenes in thymelaeaceae and euphorbiaceae occurring and utilized in Yunnan (Southwest China). 2. Ingenane type diterpene esters from Euphorbia nematocypha Hand.‐Mazz
Authors: Dagang Wu , Sorg B. , Adolf W. , Seip E. H. , Hecker E. 
Published: October 2006

AbstractThe highly irritant new Euphorbia factors N1 and N2 were isolated as a mixture from latex of E. nematocypha Hand.‐Mazz., by a combination of counter current distribution and chromatographic methods. Spectroscopic and chemical analyses revealed their structures to be 3‐0‐(2,4,6,8‐tetradecatetraenoyl)ingenol (1) and 3‐0‐(2,4,6,8‐pentadecatetraenoyl)ingenol (2), respectively.
Biota (Po‐Tzu‐Jen), a traditional Chinese medicine, ameliorates the memory acquisition disorder induced by amygdala lesion in mice
Authors: Nishiyama Nobuyoshi , Yuan‐Liang Wang , Kaimori Jun'Ya , Ishihara Akane , Saito Hiroshi 
Published: October 2006

AbstractThe effects of Biota orientalis (L.) Endl. (biota), a traditional Chinese medicine on learning performances were investigated. Nine weeks old male ddY mice recieved bilaterial amygdala lesions by delivery of a radiofrequency current. Biota (250 and 500 mg/kg/day) was administered orally from the day of the lesion until the end of the experiment. From 15 days after surgery, a step‐down type passive avoidance test was performed daily for 12 days. Lesioned animals showed severe impairment in the acquisition and retention processes. Biota ameliorated the memory acquisition deficit. The number of step‐down events in the acquisition and in the first testing trial was significantly decreased. Moreover, the mean number of days required to reach the memory acquisition criterion was markedly earlier in biota treated groups than in the lesioned control and almost similar to that in the naive control. Biota did not, however, alter the memory retention, choline acetyltransferase activity in the cortex, hippocampus and hypothalamus, and microscopic pathological changes induced by amygdala lesion. These results indicate that the memory acquisition enhancing effect of biota may not be due to a direct activation of cholinergic transmission in those areas nor to a mitigation of the pathological damage of the lesioned site but due to other unknown mechanisms.
Antifertility activity of the floral buds of Jasminum officinale var. grandiflorum in rats
Authors: Iqbal M. , Ghosh A. K. M. , Saluja A. K. 
Published: October 2006

AbstractThe effect of an aqueous extract of fresh floral buds of Jasminum officinale var. grandiflorum Linn. has been studied on female fertility in rats. Parameters included effects on the oestrus cycle, implantation, fetal loss, abortion, teratogenicity and serum progesterone levels on days 5, 12 and 20 of pregnancy. The extract at oral doses of 250 and 500 mg/kg produced a dose dependent significant antiimplantation effect, but failed to produce complete infertility. Treatment of animals during day 8 to day 12 to day 20 of pregnancy did not produce any significant abortifacient activity. There was no significant change in the weight and length of the fetuses delivered by rats treated with extract and no abnormalities were seen in the organs of the offspring. The extract produced a significant decrease in serum progesterone levels on day 5 of pregnancy which may be responsible for the antiimplantation effect observed in this study.
Ultraviolet radiation‐induced lipid peroxidation in liposomal membrane: Modification by capsaicin
Authors: De A. K. , Ghosh J. J. , Mandal T. K. 
Published: October 2006

AbstractUltraviolet‐radiation has been reported to cause lipid peroxidation in the liposomal membrane. In the present study, treatment with capsaicin, (8‐methyl‐n‐vanillyl‐6‐nonenamide), the pungent principle of red hot pepper, was shown to modify UV‐induced lipid peroxidation in the liposomal membrane. Treatment with low doses of capsaicin (less than 0.1 μg/mL of phosphatidyl choline liposome) produced a significant increase in UV‐induced lipid peroxidation, while high doses (0.1–0.5 μg/mL of PC liposome) caused a significant decrease of UV‐induced peroxidation. These pro‐oxidant and antioxidant activities of capsaicin over UV‐induced liposomal lipid peroxidation were also comparable to experiments modulated with standard pro‐oxidant ferrous sulphate and antioxidant sodium azide. The observed dual nature of capsaisin's action on the UV‐induced lipid peroxidation of the liposomal membrane may be attributed to the previously reported “activation” followed by “desensitization” action of capsaicin on other membrane lipid systems.
Antiprotozoal activity of dehydrozaluzanin C, a sesquiterpene lactone isolated from Munnozia maronii (asteraceae)
Authors: Fournet Alain , Muñoz Victoria , Roblot François , Hocquemiller Reynald , Cavé André , Gantier Jean‐Charles 
Published: October 2006

AbstractThe petroleum ether extract of the leaves of Munnozia maronii was found to inhibit in vitro the growth of promastigote forms of Leishmania and epimastigote forms of Trypanosoma cruzi with an IC90 of 25 μg/mL. Activity‐guided fractionation of the extract by chromatography identified the sesquiterpene lactone 1 of the guaiane series. The complete structure of 1 was elucidated using 1H and 13C NMR experiments at high field. The isolated compound was shown to be a new natural guaianolid, dehydrozaluzanin C, previously known as synthetic oxidative derivative of zaluzanin C (Romo de Vivar et al., 1967). This compound inhibited, in vitro, the growth of 12 strains of Leishmania and 15 strains of T. cruzi at concentrations between 50 and 2.5 μg/mL. The leishmanicidal activity of dehydrozaluzanin C was tested on BALB/c mice infected with amastigote forms of Leishmania amazonensis. Dehydrozaluzanin C reduced the severity of L. amazonesis lesions in BALB/c mice but was less active than the reference compound Glucantime.
Effects of standardized extracts GK501, from Ginkgo biloba L., G115 from Panax ginseng C. A. Meyer, and their combination, gincosan® (PHL‐00701), on the brain levels of biogenic monoamines and on the serum content of prolactin, growth hormone and ACTH
Authors: Petkov V. D. , Hadjiivanova C. , Petkov V. V. , Milanov S. , Visheva N. , Boyadjieva N. 
Published: October 2006

AbstractIn experiments on old (26 months old) rats, we found that the extracts of Panax ginseng (G115), Ginkgo biloba (GK501) and their combination Gincosan® (PHL‐00701) administered orally at two doses for 7 days induced changes in the levels of biogenic monoamines in some brain regions (frontal cerebral cortex, hippocampus, striatum, hypothalamus and pons). The most characteristic change was the increase produced by the two extracts and their combination in the serotonin level in all brain structures except for pons compared with controls. In the hippocampus G115, GK501 and their combination decreased the noradrenaline level. The same doses of G115, GK501 and their combination applied for 7 days to young (3 months old) and old (26 months old) rats caused significant changes in the blood level of prolactin (PRL), growth hormone (GH) and ACTH compared with age‐matched controls: both G115 and GK501 decreased the serum level of PRL compared with age‐matched controls; the hormone level being high in old controls, in extract‐treated rats it became equal to that in young controls; G115 and PHL‐00701 greatly increased the serum level of ACTH in both age groups compared with age‐matched controls. Under conditions of induced immobilization and cold stress in young rats, the 7‐day pretreatment with G115, GK501 and their combination led to significant changes in the blood levels of PRL, GH and ACTH compared with control untreated stressed and unstressed rats.
Hepatoprotective effects of Pluchea indica (less) extract in experimental acute liver damage in rodents
Authors: Sen T. , Basu A. , Ray R. N. , Nag Chaudhuri A. K. 
Published: October 2006

AbstractThe methanol fraction of the extract of Pluchea indica roots exhibited significant hepatoprotective activity against experimentally induced hepatotoxicity by carbon tetrachloride in rats and mice. The extract caused significant reduction of the elevated serum enzyme levels (AST, ALT, LDH and serum alkaline phosphatase) and serum bilirubin content in acute liver injury. A significant increase of reduced serum total protein, albumin and albumin/globulin ratio was also observed on extract treatment. The extract significantly reduced the prolonged pentobarbitone‐induced sleeping time and also caused a significant reduction of plasma prothrombin time in comparison with CCl4‐treated animals. The extract caused significant reduction of the increased bromosulphalein retention by CCl4‐treatment. These findings are suggestive of a potent hepatoprotective effect of the extract under investigation.
In vitro inhibition of mycobacteria by Rwandese medicinal plants
Authors: van Puyvelde L. , Ntawukiliyayo J. D. , Portaels F. , Hakizamungu E. 
Published: October 2006

AbstractA series of 15 Rwandese medicinal plants used by traditional healers to treat pulmonary diseases were screened for anti‐Mycobacterium tuberculosis activity. Three plant extracts showed activity at 1000 μg/mL: Bidens pilosa (leaves), Pentas longiflora (roots) and Tetradenia riparia (leaves). These plant extracts were studied further against several mycobacterial species: M. tuberculosis, M. avium complex, M. simiae and a new simiae like Mycobacterium species (SLM). None of the plant extracts showed activity against M. avium and SLM at 1000 μg/mL. M. simiae was sensitive to T. riparia and P. longiflora extracts (1000 μg/mL) and M. tuberculosis towards T. riparia (500 μg/mL) and B. pilosa (100 μg/mL). The active principle of T. riparia, 8(14), 15‐sandaracopimaradiene‐7α, 18‐diol, was also evaluated for its antimycobacterial activity and the concentration required for inhibiting M. tuberculosis ranged from 25 μg/mL to 100 μg/mL. The extract of the leaves of T. riparia can be used as a differentiation test (at 1000 μg/mL in the medium) for M. simiae and SLM.
Hypotensive and diuretic effect of Equisetum bogotense and Fuchsia magellanica and micropropagation of E. bogotense
Authors: Rodriguez J. , Pacheco P. , Razmilic I. , Loyola J. I. , Schmeda‐Hirschmann G. , Theoduloz C. 
Published: October 2006

AbstractEquisetum bogotense (Equisetaceae) and Fuchsia magellanica (Onagraceae) were used by the Mapuche Amerindians as diuretics. Intravenous administration of hydroalcoholic extracts to rats elicited a hypotensive response of −29.0% ±4.5% and −24.2% ±0.5% respectively in the mean blood pressure of normotensive animals at a dose of 5 mg crude extract/kg body weight. The activity was found to be related with polar compounds. For Fuchsia, the active principles are related to tannins. A single oral dose of 500 mg/kg body weight Equisetum extract produced a significant increase (p < 0.05) in the urine output in rats, while in Fuchsia a reduction in diuresis was observed. The diuretic effect of the Equisetum extract was weak compared with hydrochlorothiazide at 25 mg/kg body weight. The data presented support the use of E. bogotense in Chilean traditional medicine. A micropropagation method for E. bogotense was established by culturing shoot tips in Murashige‐Skoog medium with macro and micronutrients diluted 4‐fold and containing 0.1 mg/L thiamine, 100 mg/L myoinositol, 1.0 mg/L NAA and 0.1 mg/L BAP.
Hepatoprotective effects of Taiwan folk medicine: Alternanthera sessilis on liver damage induced by various hepatotoxins
Authors: Lin Song‐Chow , Lin Yun‐Ho , Shyuu Shyh‐Jong , Lin Chung‐Ching 
Published: October 2006

AbstractThe hepatoprotective effects of the Taiwanese herb ‘Horngtyan‐wu’ (Alternanthera sessilis (L.) DC.) were investigated in three kinds of experimental animal model. Acute hepatitis was induced by various chemicals such as carbon tetrachloride (31.25 μL/kg, i.p.) or acetaminophen (paracetamol; 600 mg/kg, i.p.) in mice and D(+)‐galactosamine (188 mg/kg, i.p.) in rats. When treated with A. sessilis (300 mg/kg, p.o.) at 2, 6 and 10 h, a reduction in elevation of serum glutamate oxaloacetic transaminase (SGOT) and glutamate pyruvic transaminase (SGPT) levels could be observed at 24 h after administration of the three hepatotoxins. These serological observations were also confirmed by histopathological examinations including centrilobular necrosis, eosinophilic bodies, pyknotic nuclei, microvesicular degeneration of hepatocytes and others. The liver microscopic examination showed a noted improvement in groups receiving A. sessilis. All pharmacological and histopathological effects were compared with observations using the hepatoprotective Chinese herb, Bupleurum chinense (Family Umbelliferae). It was confirmed that A. sessilis has hepatoprotective effects against liver injuries induced by hepatotoxins with different mechanisms.
An approach to the genus Tanacetum L. (Compositae): Phytochemical and pharmacological review
Authors: Abad M. J. , Bermejo P. , Villar A. 
Published: October 2006

AbstractIn view of the importance in folk medicine of some species of Tanacetum L. (Compositae), e.g. T. parthenium, this paper reviews reports of the past two decades on their phytochemistry and pharmacological actions. The facets of phytochemical composition to be reviewed concern mainly the compounds with a chemosystematic interest in the tribe: terpenoids, especially sesquiterpenes and sesquiterpene lactones and flavonoids. The pharmacological activities which make it possible to corroborate their use as a herbal remedy have also been reviewed.
Palbinone, a novel terpenoid from Paeonia albiflora: A potent inhibitory activity on human monocyte interleukin‐1β
Authors: Kadota Shigetoshi , Basnet Purusotam , Terashima Satoshi , Li Jian‐Xin , Namba Tsuneo , Kageyu Akira 
Published: October 2006

AbstractPalbinone, a novel terpenoid from the roots of Paeonia albiflora, has a very strong inhibitory activity on the reduced form of nicotinamide adenine dinucleotide phosphate (NADPH) linked 3α‐hydroxysteroid dehydrogenase (3α‐HSD) of rat liver cytosol and showed a significant inhibitory activity on human monocyte interleukin‐1β, a polypeptide which is though to play an important role in inflammation. In contrast the enzymes cyclooxygenase (CO), thromboxane A synthase (TX) and 5‐lipoxygenase (LO) were not significantly inhibited by palbinone when it was compared with tenokisicum, indomethacin, imidazole and 2, 3, 5‐trimethyl‐6‐(12‐hydroxy‐5, 10‐dodecadiynyl)‐1, 4‐benzoquinone (AA‐861) as positive controls under similar experimental conditions. The activity of palbinone was highly selective since it inhibited strongly only human monocyte interleukin‐1β and did not show any significant activity on CO, TX and LO.
Studies on the effects of capsaicin on leakage in egg lecithin (Phosphatidyl Choline) liposome membranes in vitro
Authors: Mandal T. K. , Chakraborty B. , De A. K. 
Published: October 2006

AbstractCapsaicin (8‐methyl‐n‐vanillyl‐6‐nonenamide), caused a concentration dependent leakage of chromate through an egg lecithin (phosphatidyl choline) liposomal preparation. Capsaicin treatment of liposomal suspensions caused a maximum leakage of marker chromate at 20 min and then attained a plateau from 30 min onward. Treatment of liposomes with various concentrations of capsaicin (μg/mL loposomal suspensions) showed that lower concentrations of capsaicin (< 0‐0.1 μg/mL) caused greater chromate leakage than higher concentrations (0.1‐0.5 μg/mL). This dual effect of capsaicin on liposome membrane was accompanied by an increased amount of malondialdehyde formed (an important end product of lipid peroxidation) at lower concentrations (<0.10 μg/mL) than at higher concentrations (0.1‐0.5 μg/mL).
Effects of Olea europaea L. extract on the rat isolated ileum and trachea
Authors: Fehri Badreddine , Mrad Samira , Aiache Jean‐Marc , Lamaison Jean‐Louis 
Published: October 2006

AbstractThe effects of an Olea europaea L. dried leaf extract containing 3.2% of oleuropein were investigated on the rat isolated ileum and trachea. On basal tone rat isolated ileum, Olea europaea L. extract was shown to produce a dual effect characterized by a contraction at low doses (10−7‐10−4g/mL) and a relaxation at high doses (3.10−4‐10−3g/mL). The extract induced contractile effect was found to involve at least histamine, 5‐hydroxytryptamine and thromboxane A2. On precontracted rat isolated ileum, the extract only induced a relaxation that was not modified by nifedipine, diltiazem, dipyridamone, verapamil or papaverine (10−6 M). The effects of the extract were also studied on the rat isolated trachea. On basal tone organs, Olea europaea L. extract did not produce any effect, whereas, when basal tone was raised by acetylcholine (ACh 10−3 M), the drug caused a relaxation (maximal effect 39.01% ± 5.40%) of the response to theophylline; (3.10 ± 10−3M n = 15). It is suggested that the induced relaxation is consecutive to an increase of intracellular 3′5′ cAMP.
Screening of tropical medicinal plants for antiinflammatory activity
Authors: Recio M. C. , Giner R. M. , Mánez S. , Rios J. L. , Marston A. , Hostettmann K. 
Published: October 2006

AbstractThe antiinflammatory activity of different extracts from 16 tropical plant species belonging to 15 different families has been determined. They were administered topically on TPA‐induced mouse ear oedema and orally on carrageenan‐induced mouse paw oedema. In the latter, extracts from Diospyros leucomelas, Erythrospermum monticolumn, Ficus polita, Heteromorpha trifoliata, Hypericum lalandii, Kirkia acuminata, Pterocarpus angolensis and Zanha africana significantly reduced the oedema 3 h after carrageenan injection. All the extracts were considerably active when assayed topically with only three exceptions.
Multivariate Parametrization of Amino Acid Properties by Thin Layer Chromatography
Authors: Eriksson Lennart , Jonsson Jörgen , Sjöström Michael , Wold Svante 
Published: October 2006

Abstract48 amino acids (20 coded and 28 non‐coded) were multivariately characterized by seven thin layer chromatography variables and two theoretical variables (molecular weight and side chain van der Waals volume). Principal components analysis (PCA) of the original 48 × 9 data matrix, resulted in two significant principal components which together described 88% of the variance in the data. The relationship between these principal components and the earlier estimated z‐scales for coded amino acids was investigated. In addition, it was found that the principal components had a predictive capacity similar to the z‐scales, when compared in a peptide QSAR of a series of bradykinin potentiating pentapeptides modified with only coded amino acids. Thus it is shown that TLC is a rapid technique suitable for the parametrization of amino acids.
Inhibition of Carbonic Anhydrase by Substituted Benzenesulfonamides. A Reinvestigation by QSAR and Molecular Graphics Analysis
Authors: Carotti Angelo , Raguseo Cosima , Campagna Francesco , Langridge Robert , Klein Teri E. 
Published: October 2006

AbstractThe inhibition of Bovine Carbonic Anhydrase B (BCA‐B) by an appropriately designed set of meta‐ and para‐substituted benzenesulfonamides was studied. From the results the following quantitative structure‐activity relationship was derived: log 1/Ki = 0.95 σ + 0.54 π – 0.35 B5,3 + 6.29. In this equation Ki is the inhibition constant, σ is the Hammett constant, π is the hydrophobic parameter and B5,3 is the sterimol steric parameter for the meta substituents. Using this equation we designed, synthesized and successfully predicted Ki for a new congener intended to maximize the inhibitory potency (1/Ki). The interactions involved in the enzyme‐inhibitors binding as suggested by the correlation equation, have been tentatively interpreted using computer built 3‐D molecular models based on the published X‐ray crystallographic coordinates of the free and inhibitor‐bound carbonic anhydrase. The results from our analyses have been compared with those obtained in some previous QSAR analyses.
EVE, a Distance Based Approach for Discriminating Nonlinearly Separable Groups
Authors: Benigni Romualdo 
Published: October 2006

AbstractWe previously demonstrated that the Euclidian distances between objects provide a description of the data field, which is more flexible and versatile than the description provided by the original variables, from which the distances were calculated. In fact, the distance matrix also contains, together with the information carried by the original variables, information about the relationships between objects. These properties of the Euclidian distances permit the separation of both linearly and nonlinearly separable groups. In this paper, the findings of our previous work were implemented in a computer program (EVE), which permits: a) the identification of the variables that separate two classes; b) the construction of discriminant equations. The potential of EVE was demonstrated by applying it to a number of simulated cases, as well as to a real QSAR problem (antiparasitic activity of Praziquantel and its analogues), where the active chemicals are embedded in the group of the inactives.
ADMET Property Prediction: The State of the Art and Current Challenges
Authors: Gola Joelle , Obrezanova Olga , Champness Ed , Segall Matthew 
Published: October 2006

AbstractIn this article, we review recent developments in the prediction of Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) properties by Quantitative Structure–Activity Relationships (QSAR). We consider advances in statistical modelling techniques, molecular descriptors and the sets of data used for model building and changes in the way in which predictive ADMET models are being applied in drug discovery. We also discuss the current challenges that remain to be addressed. While there has been progress in the adoption of non‐linear modelling techniques such as Support Vector Machines (SVM) and Bayesian Neural Networks (BNNs), the full advantages of these ‘machine learning’ techniques cannot be realised without further developments in molecular descriptors and availability of large, high‐quality datasets. The largest pharmaceutical companies have developed large in‐house databases containing consistently measured compound properties. However, these data are not yet available in the public domain and many models are still based on small ‘historical’ datasets taken from the literature. Probably, the largest remaining challenge is the full integration of predictive ADMET modelling in the drug discovery process. Until in silico models are applied to make effective decisions in a multi‐parameter optimisation process, the full value they could bring will not be realised.