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Active Principle (active + principle)
Selected AbstractsSt John's Wort and its Active Principles in Depression and AnxietyFOCUS ON ALTERNATIVE AND COMPLEMENTARY THERAPIES AN EVIDENCE-BASED APPROACH, Issue 1 2006DJ Kroll [source] Withanoside IV and its active metabolite, sominone, attenuate A,(25,35)-induced neurodegenerationEUROPEAN JOURNAL OF NEUROSCIENCE, Issue 6 2006Tomoharu Kuboyama Abstract At the present, medication of dementia is limited to symptomatic treatments such as the use of cholinesterase inhibitors. To cure dementia completely, that is regaining neuronal function, reconstruction of neuronal networks is necessary. Therefore, we have been exploring antidementia drugs based on reconstructing neuronal networks in the damaged brain and found that withanoside IV (a constituent of Ashwagandha; the root of Withania somnifera) induced neurite outgrowth in cultured rat cortical neurons. Oral administration of withanoside IV (10 µmol/kg/day) significantly improved memory deficits in A,(25,35)-injected (25 nmol, i.c.v.) mice and prevented loss of axons, dendrites, and synapses. Sominone, an aglycone of withanoside IV, was identified as the main metabolite after oral administration of withanoside IV. Sominone (1 µm) induced axonal and dendritic regeneration and synaptic reconstruction significantly in cultured rat cortical neurons damaged by 10 µm A,(25,35). These data suggest that orally administrated withanoside IV may ameliorate neuronal dysfunction in Alzheimer's disease and that the active principle after metabolism is sominone. [source] Study and description of hydrogels and organogels as vehicles for cosmetic active ingredientsINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 4 2010M. E. Morales J. Cosmet. Sci., 60, 627,636 (November/December 2009) Synopsis Cellulite, a clinical syndrome mainly affecting women, involves specific changes in conjunctive dermic and subcutaneous tissue, leading to vascular and hypertrophic alterations in adipose tissues and the consequent alteration of tissue structure. This paper describes the design of hydrogels and pluronic-lecithin organogels elaborated as vehicles of Aloe vera (Aloe vera linné) and Hydrocotyle asiatica (Centella asiatica) for the treatment of cellulite. The objective of this work was to carry out a complete evaluation of the proposed formulae through the study of the organoleptic and rheological properties of the formulae. Our work revealed that, in appearance, hydrogels show better organoleptic characteristics than organogels. On the other hand, from a rheological point of view, both hydrogels and organogels display a plastic behavior. However, the main difference between the two is that the more complex internal structure of the organogel bestows it with more viscosity. Finally, in vitro tests with Franz-type diffusion cells revealed that the release of cosmetic active principle from the tested excipients was appropriate, both in terms of magnitude and velocity. [source] Analysis of low content drug tablets by transmission near infrared spectroscopy: Selection of calibration ranges according to multivariate detection and quantitation limits of PLS modelsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 12 2008Manel Alcalà Abstract The content uniformity of low dose products is a major concern in the development of pharmaceutical formulations. Near infrared spectroscopy may be used to support the design and optimization of potent drug manufacturing processes through the analysis of blends and tablets in a relatively short time. A strategy for the selection of concentration ranges in the development of multivariate calibration is presented, evaluating the detection and quantitation limits of the obtained multivariate models. The strategy has been applied to the determination of an active principle in pharmaceutical tablets of low concentration (0,5%, w/w), using Fourier Transform Near Infrared (FT-NIR) transmission spectroscopy. The quantitation and detection limits decreased as the upper concentration level of the calibration models was reduced. The results obtained show that the selection of concentration ranges is a critical aspect during model design. The selection of wide concentration ranges with high levels is not recommended for the determination of analytes at minor levels (<1%, w/w), even when the concentration of interest is within the range of the model. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:5318,5327, 2008 [source] Antioxidant effect of 2-hydroxy-4-methoxy benzoic acid on ethanol-induced hepatotoxicity in ratsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 3 2007Nadana Saravanan Alcoholic liver disease (ALD) is one of the most common diseases in society. A large number of studies are in progress to identify natural substances that are effective in reducing the severity of ALD. 2-Hydroxy-4-methoxy benzoic acid (HMBA), the active principle of Hemidesmus indicus, an indigenous Ayurvedic medicinal plant in India, is expected to significantly inhibit the development of liver injury in ethanol administration. It is expected to reduce the severity of liver damage in terms of body weight, hepatic marker enzymes, oxidative stress, antioxidant status and histological changes in ethanol-induced hepatotoxic rats. Hepatotoxicity was induced by administering 20% ethanol (5 g kg,1 daily) for 60 days to male Wistar rats, which resulted in significantly decreased body weight and an increase in liver-body weight ratio. The liver marker enzymes aspartate transaminase, alanine transaminase, alkaline phosphatase, ,-glutamyl transpeptidase and lactate dehydrogenase were elevated. In addition, the levels of plasma, erythrocyte and hepatic thiobarbituric acid reactive substances, hydroperoxides and conjugated dienes were also elevated in ethanol-fed rats as compared with those of the experimental control rats. Decreased activity of superoxide dismutase, catalase, glutathione peroxidase, reduced glutathione, vitamin C and ,-tocopherol was also observed on alcohol administration as compared with experimental control rats. HMBA was co-administered at a dose of 200 ,gkg,1 daily for the last 30 days of the experiment to rats with alcohol-induced liver injury, which significantly increased body weight, significantly decreased the liver-body weight ratio, transaminases, alkaline phosphatase, ,-glutamyl transpeptidase and lactate dehydrogenase, significantly decreased the levels of lipid peroxidative markers, significantly elevated the activity of enzymic and non-enzymic antioxidants in plasma, erythrocytes and liver and also increased levels of plasma and liver vitamin C and ,-tocopherol at the end of the experimental period as compared with untreated ethanol-administered rats. The histological changes were also in correlation with the biochemical findings. The results suggest that HMBA administration may afford protection against ethanol-induced liver injury in rats. [source] Anti-leukaemic and Anti-mutagenic Effects of Di(2-ethylhexyl)phthalate Isolated from Aloe vera LinneJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 5 2000KEYONG HO LEE Extracts of Aloe vera Linne have been found to exhibit cytotoxicity against human tumour cell lines. This study examines the anti-tumour effects of di(2-ethylhexyl)phthalate (DEHP) isolated from Aloe vera Linne, in human and animal cell lines. Its anti-mutagenic effects were examined using Salmonella typhimurium TA98 and TA100 strains. Growth inhibition was specifically exerted by DEHP against three leukaemic cell lines at concentrations below 100 ,g mL,1. At 100 ,g mL,1 DEHP, K562, HL60 and U937 leukaemic cell lines showed growth inhibition of 95, 97 and 95%, respectively. DEHP exhibited an inhibitory activity of 74, 83 and 81%, respectively, in K562, HL60 and U937 cell lines at a concentration of 10 ,g mL,1. At a concentration of 1 ,g mL,1, DEHP exerted an inhibitory activity of 50, 51 and 52%, respectively, in K562, HL60 and U937. In a normal cell line, MDBK, DEHP exerted 30% growth inhibition at a concentration of 100 ,g mL,1, and showed no inhibitory activity at concentrations below 50 ,g mL,1. It was found that DEHP exerted anti-mutagenic activity in the Salmonella mutation assay. The number of mutant colonies of Salmonella typhimurium strain TA98 upon exposure to AF-2 (0.2 ,g/plate) decreased in a concentration-dependent manner in the presence of different DEHP concentrations (decreasing to 90.4, 83.9, 75.4, 69.6 and 46.9%, respectively, for DEHP concentrations of 100, 50, 10, 5 and 1 ,g/plate). In the case of Salmonella typhimurium strain TA100, DEHP reduced AF-2-induced mutagenicity at 1, 5, 10, 50 and 100 ,g/plate to 57.4, 77.5, 80.0, 89.0 and 91.5%, respectively. The isolated compound from Aloe vera Linne, DEHP, was considered to be the active principle responsible for anti-leukaemic and anti-mutagenic effects in-vitro. [source] Fourier transform Raman spectroscopy of drugs: quantitative analysis of 1-phenyl-2,3-dimethyl-5-pyrazolone-4-methylaminomethane sodium sulfonate: (dipyrone)JOURNAL OF RAMAN SPECTROSCOPY, Issue 10 2003Antônio O. Izolani Abstract Several drugs provided by the pharmaceutical industry and containing dipyrone as the active principle have different mass percentages of the letter. We describe a procedure for the quantitative analysis of several tablets containing dipyrone (or other solid active principles). The results of Fourier transform Raman band analysis (band area and band height) agree well with the stated contents of dipyrone in the tablets. Copyright © 2003 John Wiley & Sons, Ltd. [source] Instrumental planar chromatographic method for determination of carbamazepine in human serumJOURNAL OF SEPARATION SCIENCE, JSS, Issue 9 2009Sigrid Mennickent Abstract An instrumental planar chromatographic (HPTLC) method for quantification of carbamazepine in human serum was developed using liquid-liquid extraction with dichloromethane, fluorescence activation with perchloric acid 60%/ethanol/water (1:1:1, v/v) and fluorescence detection. Planar chromatographic separation was performed on precoated silica gel F254 HPTLC plates using a mixture of ethyl acetate/toluene/methanol/acetic acid glacial (5:4:0.5:0.5, v/v) as mobile phase. Densitometric detection was done at 366 nm. The method was validated for linearity, precision and accuracy. Linear calibration curves in the range of 3 and 20 ng/,L showed correlation coefficient of 0.998. The intra-assay and inter-assay precision, expressed as the RSD, were in the range of 0.41,1.24% (n = 3) and 2.17,3.17% (n = 9), respectively. The LOD was 0.19 ng, and the LOQ was 0.57 ng. Accuracy, calculated as percentage recovery, was between 98.98 and 101.96%, with a RSD not higher than 1.52%. The method was selective for the active principle tested. In conclusion, the method is useful for quantitative determination of carbamazepine in human serum. [source] Pharmacokinetic interaction of single dose of piperine with steady-state carbamazepine in epilepsy patientsPHYTOTHERAPY RESEARCH, Issue 9 2009Smita Pattanaik Abstract Piperine, the active principle of piper species, is commonly used as a spice and adjuvant in various traditional systems of medicine. It has been known as a bioavailability-enhancer. The present study aimed at evaluating the effect of piperine on the steady-state pharmacokinetics of a single dose of carbamazepine in poorly controlled epilepsy patients on carbamazepine monotherapy. Patients (n = 10 each) receiving either 300 mg or 500 mg dose of carbamazepine twice daily were selected. After administration of carbamazepine, venous blood samples were collected at 0, 0.5, 1, 2, 4, 6, 9, 12 h. Subsequently, piperine (20 mg p.o.) was administered along with carbamazepine and samples were collected similarly. The pharmacokinetic parameters were compared by Students t -test. Piperine significantly increased the mean plasma concentrations of carbamazepine at most of the time points in both dose groups. There was a significant increase in AUC0-12hr (p < 0.001), average Css (p < 0.001), t1\2el (p < 0.05) and a decrease in Kel (p < 0.05), in both the dose groups, whereas changes in Ka and t1\2a were not significant. Cmax (p < 0.01) and tmax (p < 0.01) were increased significantly following piperine administration in the 500 mg dose group; however, these parameters were not significant in the lower dose group. Piperine could significantly enhance the oral bioavailability of carbamazepine, possibly by decreasing the elimination and/or by increasing its absorption. Copyright © 2009 John Wiley & Sons, Ltd. [source] Nimbidin suppresses functions of macrophages and neutrophils: relevance to its antiin,ammatory mechanismsPHYTOTHERAPY RESEARCH, Issue 5 2004Gurpreet Kaur Abstract Nimbidin is a mixture of tetranortriterpenes and is the major active principle of the seed oil of Azadirachta indica A. Juss (Meliaceae) possessing potent antiin,ammatory and antiarthritic activities. The present study revealed that nimbidin signi,cantly inhibited some of the functions of macrophages and neutrophils relevant to the in,ammatory response following both in vivo and in vitro exposure. Oral administration of 5,25 mg/kg nimbidin to rats for 3 consecutive days signi,cantly inhibited the migration of macrophages to their peritoneal cavities in response to in,ammatory stimuli and also inhibited phagocytosis and phorbol-12-myristate-13-acetate (PMA) stimulated respiratory burst in these cells. In vitro exposure of rat peritoneal macrophages to nimbidin also inhibited phagocytosis and PMA stimulated respiratory burst in these cells. Nimbidin also inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS) stimulated macrophages following in vitro exposure, whereas interleukin 1 (IL-1) was only weakly inhibited. Probing the mechanism of NO inhibition revealed that nimbidin ameliorated the induction of inducible NO synthase (iNOS) without any inhibition in its catalytic activity. In addition, nimbidin also attenuated degranulation in neutrophils assessed in terms of release of , -glucuronidase, myeloperoxidase and lysozyme. The results suggest that nimbidin suppresses the functions of macrophages and neutrophils relevant to in,ammation. Thus nimbidin can be valuable in treating in,ammation/in,ammatory diseases. Copyright © 2004 John Wiley & Sons, Ltd. [source] Activity of Zanthoxylum clava-herculis extracts against multi-drug resistant methicillin-resistant Staphylococcus aureus (mdr-MRSA)PHYTOTHERAPY RESEARCH, Issue 3 2003Simon Gibbons Abstract In a continuing search for compounds with antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA) possessing multidrug ef,ux systems, we have demonstrated activity associated with extracts from Southern prickly ash bark, Zanthoxylum clava-herculis. Bioassay-guided isolation of an alkaloid extract led to the characterization of the benzo[c]phenanthridine alkaloid chelerythrine as the major active principle. This compound exhibited potent activity against strains of MRSA, which were highly resistant to clinically useful antibiotics via multidrug ef,ux mechanisms. Copyright © 2003 John Wiley & Sons, Ltd. [source] Effects of tanshinone I isolated from Salvia miltiorrhiza Bunge on arachidonic acid metabolism and in vivo inflammatory responsesPHYTOTHERAPY RESEARCH, Issue 7 2002Sung Young Kim Abstract Arachidonic acid (AA) mainly released from the cell membrane by phospholipase A2 (PLA2) is converted to eicosanoids by the action of cyclooxygenase (COX) and lipoxygenase (LO). In order to find the specific inhibitors of AA metabolism especially PLA2 and COX-2, 300 plant extracts were evaluated for their inhibitory activity on PGD2 production from cytokine-induced mouse bone marrow-derived mast cells in vitro. From this screening procedure, the methanol extract of Salvia miltiorrhiza was found to inhibit PGD2 production and the ethyl,acetate subfraction gave the strongest inhibition of five subfractions tested. From this ethyl,acetate subfraction, an activity-guided isolation finally gave tanshinone I as an active principle. This investigation deals with the effects of tanshinone I on AA metabolism from lipopolysaccharide (LPS)-induced RAW 264.7 cells and in vivo antiinflammatory activity. Tanshinone I inhibited PGE2 formation from LPS-induced RAW macrophages (IC50,=,38,,M). However, this compound did not affect COX-2 activity or COX-2 expression. Tanshinone I was found to be an inhibitor of type IIA human recombinant sPLA2(IC50,=,11,,M) and rabbit recombinant cPLA2 (IC50,=,82,,M). In addition, tanshinone I showed in vivo antiinflammatory activity in rat carrageenan-induced paw oedema and adjuvant-induced arthritis. Copyright © 2002 John Wiley & Sons, Ltd. [source] A comparative study of different crude extracts of Ocimum sanctum on noise stressPHYTOTHERAPY RESEARCH, Issue 6 2002R. Archana Abstract Our previous studies have shown that the ethanolic extract of Ocimum sanctum (OS) leaves was effective in alleviating the noise stress induced changes. Hence in this study, we have investigated the effectiveness of different types of crude OS extracts on some of the stress parameters after noies stress. The results of this study has shown that the active pinciple responsible for antistressor effect of ethanolic extract is also present in cold homogenised leaf extract of OS also. Hot extracts slightly decrease the potency of the active principle in normalizing corticosteroid level. Copyright © 2002 John Wiley & Sons, Ltd. [source] The effect of capsaicin on blood glucose, plasma insulin levels and insulin binding in dog modelsPHYTOTHERAPY RESEARCH, Issue 5 2001I. Tolan Abstract Capsicum frutescens has been used to treat diabetes mellitus by traditional healers in Jamaica. This study was designed to identify any hypoglycaemic principle(s) and to determine the mechanism of action. Purification experiments employing thin layer chromatography (TLC) and high performance liquid chromatography (HPLC) led to the extraction of the active principle, capsaicin. Capsaicin caused a decrease in blood glucose levels of 4.91,±,0.52 (n,=,6),mmol/dL versus 6.40,±,0.13,mmol/dL (n,=,6) for the control (p,<,0.05) at the 2.5,h time interval when the oral glucose tolerance test (OGTT) was performed on dogs treated with capsaicin and compared with the control. Plasma insulin levels measured at the 2.5,h time interval showed that there was an increase in plasma insulin levels of 5.78,±,0.76,µIU/mL (n,=,6) for the capsaicin treated dogs versus 3.70,±,0.43,µIU/mL (n,=,10) for the control (p,<,0.05). Insulin receptor studies, using a modification of the method of Gambhir et al. done on monocytes obtained from blood at the 2.5,h time interval showed that there was a decrease in the percentage receptor binding for the capsaicin treated dogs when compared with the control. Insulin affinity results showed that there was a decrease of 2.4,×,10,4 in monocytes for the capsaicin treated dogs versus 8.77,×,10,4 for the control (p,<,0.05). Also, insulin receptor calculations showed a decrease in number, 2.63,×,108,±,5.73,×,107, compared with 8.77,×,108,±,1.47,×,108 for the control. In conclusion it can be stated that capsaicin is responsible for the hypoglycaemic episodes seen in the dogs and that it also causes an increase in insulin secretion which leads to a reduction of insulin binding on the insulin receptors. Copyright © 2001 John Wiley & Sons, Ltd. [source] Complete bioavailability and lack of food-effect on pharmacokinetics of gliclazide 30 mg modified release in healthy volunteersBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 4 2002P. Delrat Abstract A new modified release (MR) formulation containing 30 mg of gliclazide was developed to obtain a better predictable release of the active principle and to allow once-daily dosing regimen. An absolute bioavailability study was carried out to characterise the performance of the new formulation and the food-effect was also investigated in a separate study. Both studies were single dose, randomised, open label, two way cross over studies with a wash out period between doses. For the bioavailability study, each volunteer received 30 mg of gliclazide given either as a 1 h intravenous infusion or as a 30 mg MR tablet. For the food-effect study, the treatment was given either fasted or 10 min after the start of a standardised Melander breakfast. Blood samples were collected up to 72 h after administrations and plasma samples assayed for gliclazide concentrations using a reverse-phase HPLC method with UV detection. Mean absolute bioavailability of gliclazide was 97% and ranged between 79 and 110% showing complete absorption. A similar moderate to low variability was observed after IV and oral administration showing the MR formulation did not add to the overall variability which is solely due to the disposition parameters, in particular metabolism of gliclazide. No significant difference was observed in tmax, t1/2z, Cmax and AUC of gliclazide after administration of the 30 mg MR tablet under fasted and fed conditions. In conclusion, after single oral administration of a 30 mg MR tablet, gliclazide was completely absorbed both under fasted and fed conditions. A consistent and optimal release of gliclazide from this formulation leads to a low to moderate overall variability of its pharmacokinetic parameters. Diamicron 30 mg MR can be given without regards to meals i.e. before, during or after breakfast. Copyright © 2002 John Wiley & Sons, Ltd. [source] Expression of a plant-derived peptide harboring water-cleaning and antimicrobial activitiesBIOTECHNOLOGY & BIOENGINEERING, Issue 1 2003M. Suarez Abstract Drinking water is currently a scarce world resource, the preparation of which requires complex treatments that include clarification of suspended particles and disinfection. Seed extracts of Moringa oleifera Lam., a tropical tree, have been proposed as an environment-friendly alternative, due to their traditional use for the clarification of drinking water. However, the precise nature of the active components of the extract and whether they may be produced in recombinant form are unknown. Here we show that recombinant or synthetic forms of a cationic seed polypeptide mediate efficient sedimentation of suspended mineral particles and bacteria. Unexpectedly, the polypeptide was also found to possesses a bactericidal activity capable of disinfecting heavily contaminated water. Furthermore, the polypeptide has been shown to efficiently kill several pathogenic bacteria, including antibiotic-resistant isolates of Staphylococcus, Streptococcus, and Legionella species. Thus, this polypeptide displays the unprecedented feature of combining water purification and disinfectant properties. Identification of an active principle derived from the seed extracts points to a range of potential for drinking water treatment or skin and mucosal disinfection in clinical settings. © 2002 Wiley Periodicals, Inc. Biotechnol Bioeng 81: 13,20, 2003. [source] Pharmacological characterization of a novel investigational antimuscarinic drug, fesoterodine, in vitro and in vivoBJU INTERNATIONAL, Issue 8 2008Peter Ney OBJECTIVE To investigate the primary pharmacology of fesoterodine (a novel antimuscarinic drug developed for treating overactive bladder) and SPM 7605 (its active metabolite, considered to be the main pharmacologically active principle of fesoterodine in man) against human muscarinic receptor subtypes, and to investigate in vitro and in vivo functional activity of these agents on the rat bladder compared with existing standard agents. MATERIALS AND METHODS The displacement of radioligand binding by fesoterodine, SPM 7605 and standard agents in membrane preparations of Chinese hamster ovary (CHO) cells expressing the different human muscarinic receptors (M1,M5) was characterized. Agonistic and antagonistic activities were studied using different CHO cell lines stably expressing the human recombinant muscarinic receptor subtypes. The effects of fesoterodine and SPM 7605 on isolated bladder strips contracted by carbachol or electrical field stimulation (EFS) were investigated. In vivo the effects of fesoterodine and SPM 7605 on micturition variables were assessed using continuous cystometry in conscious female Sprague-Dawley rats, and compared to those of oxybutynin and atropine. RESULTS In vitro SPM 7605 potently inhibited radioligand binding at all five human muscarinic receptor subtypes with equal affinity across all five. Fesoterodine had a similar balanced selectivity profile but was less potent than SPM 7605. Both substances were competitive antagonists of cholinergic agonist-stimulated responses in human M1-M5 cell lines and had a similar potency and selectivity profile to the radioligand-binding studies. In rat bladder strips, fesoterodine and SPM 7605 caused a rightward shift of the concentration-response curve for carbachol with no depression of the maximum, and concentration-dependently reduced contractions induced by EFS. The potency of both drugs was similar to that of atropine and oxybutynin. In the presence of the esterase inhibitor neostigmine, the concentration-response curve of fesoterodine was shifted to the right, suggesting that part of the activity was caused by metabolism to SPM 7605 by tissue enzymes. In vivo, low doses (0.01 mg/kg) of fesoterodine and SPM 7605 reduced micturition pressure and increased intercontraction intervals and bladder capacity, but did not affect residual volume. CONCLUSIONS Fesoterodine and its active metabolite, SPM 7605, are nonsubtype selective, competitive antagonists of human muscarinic receptors, but SPM 7605 has greater potency than the parent compound. Pharmacodynamic studies in the rat bladder in vitro confirm the competitive muscarinic antagonist profile of these agents in a native tissue preparation, and in vivo studies in the rat showed effects on bladder function consistent with a muscarinic antagonist profile. [source] Fast Batch to Continuous Transposition: Application to the Extraction of Andrographolide from PlantsCHEMICAL ENGINEERING & TECHNOLOGY (CET), Issue 3 2006L. Prat Abstract A fast development method for batch to continuous process transposition is proposed. This method is based on transient regime experiment analyses and is applied to a solid-liquid extraction. The application under consideration is the extraction of an active principle from a plant in a non-sinusoidal pulsed column. Typically, the proposed signal is composed of two different periods: firstly, a classical sinusoidal pulsation step is used to mix the liquid and solid phases in the active part of the column and allow an optimal mass transfer and, secondly, an impulsion phase, used generally for the transport of solids. The extraction is carried out in a disc and doughnut column of 54,mm diameter and 3.5,m height. Liquid and solid are flowing co-currently and downwardly. This technological improvement has been implemented to solve the difficulties due to the significant heterogeneity of the matter: one part tends to float and other to sink, which always leads to a definitive flooding in classical operations. The effects of the solid flow rate and the solvent characteristics on the hydrodynamic behavior of the column are studied. The mean residence time and the total solid holdup are calculated by using a transient regime mass balance on the experimental results. These experiments allow the identification and quantification of opposite effects of the operating parameters. Mass transfer experiments have been performed and the results fit calculated values obtained by coupling the hydrodynamic and batch extraction results. Despite the simplifications made, this validates the fast development method proposed to help batch to continuous transposition. [source] In vitro antioxidant activities of mouthrinses and their componentsJOURNAL OF CLINICAL PERIODONTOLOGY, Issue 5 2002M. Battino Abstract Objectives: Several forms of periodontal diseases (PD) are often associated with activated phagocytosing leukocytes and contemporary free radical production. Host antioxidant defenses could benefit from mouthrinses used as adjuncts to counteract plaque-associated bacteria. The aim of the present study was to determine possible antioxidant activity (AA) of a number of antiseptic mouthrinses and of their stated active principles (AP), regardless of their efficacy as antimicrobial agents. Material and Methods: The antioxidant activities of 11 mouthrinses and their active principles were tested with a specific spectrophotometric method. Comet assay was used to test whether pure chemical antioxidant activity actually corresponded to prevention of in vitro DNA fragmentation. Results: Methylsalicylate-containing mouthrinses were the most effective. Several compounds, and some vehicles, behaved as antioxidants. Fibroblast DNA fragmentation was limited by preincubation with methylsalicylate-containing mouthrinse but was unaffected by treatment with chlorexidine. Conclusion: The results described herein indicate that several mouthrinses possess AA; such a property could be ascribed to either AP or vehicles or both. All the data were obtained in systems in vitro and the demonstration of in vivo AA is necessary. These findings could be useful in the treatment of some forms of PD and should be considered when arranging new mouthrinse formulations. Zusammenfassung In vitro antioxidative Aktivitäten von Mundwässern und ihren Komponenten Ziele:,Verschiedene Formen von parodontalen Erkrankungen (PD) sind häufig mit aktivierten phagozytierenden Leukozyten und gleichzeitiger Produktion von freien Radikalen verbunden. Die Antioxydantienabwehr des Wirtes könnte von Mundwässern genützt werden, die als Adjunktive zur Bekämpfung der plaque-assoziierten Bakterien verwendet werden. Das Ziel der vorliegenden Studie war die Bestimmung der möglichen Antioxydantienaktivität (AA) von einer Anzahl antiseptischer Mundwässer und ihrer angegebenen aktiven Prinzipien (AP), unabhängig von ihrer Effektivität als antimikrobielle Agentien. Material und Methoden:,Die antioxydative Aktivität von 11 Mundwässern und ihre Aktivitätsprinzipien wurden mit einer spezifischen Spektralphotometrie getestet. Ein Assay wurde für die Testung genutzt, ob die reine chemische antioxydative Aktivität tatsächlich mit der Prävention der in vitro DNA Fragmentation korrespondiert. Ergebnisse:,Methylsalicylat enthaltende Mundwässer waren am effektivsten. Verschiedene Bestandteile und einige Vehikel verhielten sich wie Antioxydantien. Fibroblasten DNA Fragmentation wurde durch Präinkubation mit Methylsalicylat enthaltende Mundwässer begrenzt, war aber unbeeinflusst durch Behandlung mit Chlorhexidin. Schlussfolgerung:,Die beschriebenen Ergebnisse zeigen, dass verschiedene Mundwässer über AA verfügen; solch eine Eigenschaft könnte entweder AP oder Vehikeln oder beiden zugeschrieben werden. Alle Daten sind in in vitro Systemen gewonnen worden, aber die Demonstration der in vivo AA ist notwendig. Diese Ergebnisse könnten in der Behandlung von einigen Formen der PD nützlich sein und sollten bei der Entwicklung neuer Mundwasserrezepte beachtet werden. Résumé Activité antioxydante in vitro des bains de bouche et de leurs composants Buts:,Plusieurs formes d'affections parodontales (periodontal diseases, PD) sont souvent associées à des leucocytes phagocytaires activés et à la production de radicaux libres contemporains. L'utilisation de bains de bouche comme adjuvants pourrait être bénéfique aux défenses antioxidantes de l'hôte pour lutter contre les bactéries de plaque. L'objectif de cette étude était de déterminer l'activité antioxydante (antioxidant activity, AA) potentielle d'un certain nombre de bains de bouche antiseptiques et de leurs principes actifs reconnus (active principles, AP), indifféremment de leur efficacité en tant qu'agents antimicrobiens. Matériaux et méthodes:,L'activité antioxydante de 11 bains de bouche et de leurs principes actifs a été testée à l'aide d'une méthode spectrophotométrique spécifique. Le test Comet a été utilisé pour voir si l'activité antioxydante chimique pure permet effectivement de prévenir la fragmentation de l'ADN in vitro. Résultats:,Les bains de bouche contenant du méthylsalicylate étaient les plus efficaces. Plusieurs composés et certains vecteurs se comportaient comme des antioxydants. La pré-incubation dans des bains de bouche contenant du méthylsalicylate limitait la fragmentation de l'ADN des fibroblastes, mais le traitement à la chlorhexidine ne l'affectait pas. Conclusion:,Les résultats décrits dans cette étude indiquent que plusieurs bains de bouche possèdent une AA, propriété qui pourrait être attribuée aux AP ou aux véhicules ou aux deux. Toutes les données ont été obtenues sur des systèmes in vitro, et l'AA in vivo reste à démontrer. Ces résultats pourraient s'avérer utiles pour le traitement de certaines formes de PD et devraient être pris en compte lors de l'élaboration de nouvelles formulations de bains de bouche. [source] Insect growth-reducing and antifeedant activity in Eastern North America hardwood species and bioassay-guided isolation of active principles from Prunus serotinaAGRICULTURAL AND FOREST ENTOMOLOGY, Issue 4 2000S. Omar Abstract 1 Thirty extracts of wood and bark of hardwood trees from Eastern North America were examined for insect growth-reducing activity in a bioassay with European corn borer, Ostrinia nubilalis, and an antifeedant bioassay with the rice weevil, Sitophilus oryzae. 2 Nine of the bark extracts and four of the wood extracts showed significant growth reducing effects at 0.5% in meridic diets, whereas only two bark extracts and one wood extract showed significant antifeedant effect at the same concentration. 3 Slower growing tree species were more biologically active than fast growing ones. Isolation of the bioactive compounds in one of the active species, Prunus serotina, showed that naringenin, its derivative methoxynaringenin, and eriodictyol were responsible for the antifeedant effects. [source] Fourier transform Raman spectroscopy of drugs: quantitative analysis of 1-phenyl-2,3-dimethyl-5-pyrazolone-4-methylaminomethane sodium sulfonate: (dipyrone)JOURNAL OF RAMAN SPECTROSCOPY, Issue 10 2003Antônio O. Izolani Abstract Several drugs provided by the pharmaceutical industry and containing dipyrone as the active principle have different mass percentages of the letter. We describe a procedure for the quantitative analysis of several tablets containing dipyrone (or other solid active principles). The results of Fourier transform Raman band analysis (band area and band height) agree well with the stated contents of dipyrone in the tablets. Copyright © 2003 John Wiley & Sons, Ltd. [source] Absence of mutagenic effects of a particular Symphytum officinale L. liquid extract in the bacterial reverse mutation assayPHYTOTHERAPY RESEARCH, Issue 3 2010Birgit Benedek Abstract Comfrey (Symphytum officinale L.) root is traditionally used for the topical treatment of contusions, strains and sprains. Besides allantoin and rosmarinic acid, which are discussed as pharmacologically active principles, the drug contains pyrrolizidine alkaloids (PAs) known for their hepatotoxic, carcinogenic and mutagenic properties. The topical herbal medicinal products Kytta-Salbe® f and Kytta-Plasma® f contain a PA-free liquid extract from comfrey root as active substance. The aim of this study was to demonstrate the absence of genotoxic effects of this special extract in the bacterial reverse mutation assay (Ames test). Briefly, comfrey root liquid extract was investigated for its ability to induce gene mutations in Salmonella typhimurium strains TA 98, TA 100, TA 102, TA 1535 and TA 1537 with and without metabolic activation using the mammalian microsomal fraction S9 mix. Reference mutagens were used to check the validity of the experiments. Comfrey root fluid extract showed no biologically relevant increases in revertant colony numbers of any of the five tester strains, neither in the presence nor in the absence of metabolic activation. In conclusion, the comfrey root fluid extract contained in Kytta-Salbe® f and Kytta-Plasma® f was not mutagenic in the bacterial reverse mutation assay. Copyright © 2009 John Wiley & Sons, Ltd. [source] Bioassay-guided fractionation of lemon balm (Melissa officinalis L.) using an in vitro measure of GABA transaminase activityPHYTOTHERAPY RESEARCH, Issue 8 2009Rosalie Awad Abstract A novel pharmacological mechanism of action for the anxiolytic botanical Melissa officinalis L. (lemon balm) is reported. The methanol extract was identified as a potent in vitro inhibitor of rat brain GABA transaminase (GABA-T), an enzyme target in the therapy of anxiety, epilepsy and related neurological disorders. Bioassay-guided fractionation led to the identification and isolation of rosmarinic acid (RA) and the triterpenoids, ursolic acid (UA) and oleanolic acid (OA) as active principles. Phytochemical characterization of the crude extract determined RA as the major compound responsible for activity (40% inhibition at 100 µg/mL) since it represented approximately 1.5% of the dry mass of the leaves. Synergistic effects may also play a role. Copyright © 2009 John Wiley & Sons, Ltd. [source] Fatty acids profile and antiinflammatory activity of Nonea setosa R. et S.PHYTOTHERAPY RESEARCH, Issue 5 2006Massimo Curini Abstract In order to verify the antiinflammatory properties of Nonea setosa R. et S. (Fam. Boraginaceae) and to identify the relevant active principles, aerial parts of this plant were extracted with increasing polarity solvents. The antiinflammatory activity was investigated by a bioassay-oriented fractionation using the inhibition of the croton oil-induced ear oedema in mice as an experimental model of inflammation. GC-MS analysis of the most active fraction revealed the presence of high amounts of polyunsaturated fatty acids. Copyright © 2006 John Wiley & Sons, Ltd. [source] Inhibition of platelet phospholipase A2 activity by catuaba extract suggests antiin,ammatory propertiesPHYTOTHERAPY RESEARCH, Issue 11 2004Nádia R. Barbosa Abstract In the in,ammation process, phospholipase A2 (PLA2) catalyses the cleavage of the sn -2 ester-linked fatty acids from phospholipids, being the enzyme responsible for arachidonic acid (AA) release by cells for the biosynthesis of the prostaglandins and thromboxanes via the cyclooxygenase system, and the leukotrienes and eicosatetraenoids via the lipoxygenase pathway. AA mobilization by PLA2 and subsequent prostaglandins synthesis is considered to be a pivotal event in in,ammation. Therefore, drugs that inhibit PLA2, thus blocking the COX and LOX pathways in the AA cascade, may be effective in the treatment of in,ammatory processes. New strategies for the treatment of in,ammatory processes could be detected by a search for active principles of vegetal origin that control the lipid mediator production by inhibition of PLA2. The present data are part of a wide explorative investigation on the effects of Trichilia catigua (catuaba), which found that PLA2 activity was totally inhibited by catuaba at a concentration of 120 µg/mL, suggesting that this natural substance may have antiin,ammatory properties. Copyright © 2004 John Wiley & Sons, Ltd. [source] Suppressive effect of inducible nitric oxide synthase (iNOS) expression by the methanol extract of Actinodaphne lancifoliaPHYTOTHERAPY RESEARCH, Issue 10 2004Youngleem Kim Abstract Nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) has played a crucial role in various pathophysiological processes including in,ammation and carcinogenesis. Therefore, the inhibitors of NO synthesis or iNOS gene expression have been considered as potential anti-in,ammatory and cancer chemopreventive agents. In our continuous search for iNOS inhibitors from natural products we have evaluated indigenous Korean plant extracts using an assay for inhibition of nitric oxide formation on lipopolysaccharide (LPS)-activated mouse macrophage RAW 264.7 cells. As a result, the methanolic stem extract of Actinodaphne lancifolia showed an inhibitory activity of NO production in a dose-dependent manner (IC50 = 2.5 µg/ml). Additional study demonstrated that the extract of Actinodaphne lancifolia signi,cantly suppressed the iNOS protein and gene expression in a dose-dependent manner. These results suggest that Actinodaphne lancifolia could be a potential candidate for developing an iNOS inhibitor from natural products. Further elucidation of active principles for development of new cancer chemopreventive and/or anti-in,ammatory agents could be warranted. Copyright © 2004 John Wiley & Sons, Ltd. [source] Butanolides from Machilus thunbergii and their inhibitory activity on nitric oxide synthesis in activated macrophagesPHYTOTHERAPY RESEARCH, Issue 4 2003Nam Yi Kim Abstract In activated macrophages the inducible form of nitric oxide synthase (iNOS) generates high amounts of the toxic mediator, nitric oxide (NO), that contributes to the circulatory failure associated with septic shock. Three butanolides were isolated from Machilus thunbergii as active principles which inhibit the production of NO in lipopolysaccharide-activated RAW 264.7 cells, and their structures were identi,ed as litsenolide A2 (1), B1 (2) and B2 (3). They showed dose-dependent inhibition of NO syntheses and the IC50s were 3.36, 3.70 and 6.19 µm, respectively. These new inhibitors of iNOS may have potential in the treatment of endotoxaemia and in,ammation accompanied by the overproduction of NO. Copyright © 2003 John Wiley & Sons, Ltd. [source] Mutagenic and antimutagenic potential of the medicinal plants M. laevigata and C. xanthocarpaPHYTOTHERAPY RESEARCH, Issue 3 2003J. B. F. Fernandes Abstract Aqueous extracts of medicinal plants (Mikania laevigata and Campomanesia xanthocarpa) were screened for the presence of mutagenic activity in the Salmonella/microsome assay. The extracts of Campomanesia xanthocarpa showed frameshift (TA97a strain) signs of mutagenic activity without exogenous metabolism (S9 fraction). The infusions of Mikania laevigata, negative for mutagenic activity, showed high percentages of inhibition of mutagenesis induced by mutagens 2AF (2-amino,uorene), in the presence of exogenous metabolism (S9 fraction), for frameshift (TA98) and base pair substitution (TA100) lesions. In addition, these inhibitions were observed against mutagen SAZ (sodium azide) in assays with the TA100 strain, without exogenous metabolism (S9 fraction). A synergistic effect was also observed in frameshift mutagenic events, with direct action in the presence of 4NQO (4-oxide-1-nitroquinoline) and a tendency to a low percentage of action enhancement, in the presence of the 2AF mutagen. The variable responses observed in the extract assays show the potentials for interaction of the different active principles in genetic material. Copyright © 2003 John Wiley & Sons, Ltd. [source] Topographical and Wettability Effects of Post-Discharge Plasma Treatments on Macroporous Polystyrene-Divinylbenzene Solid FoamsPLASMA PROCESSES AND POLYMERS, Issue 10 2009Cristina Canal Abstract The aim of this study was to evaluate the morphological characteristics and wetting properties of polystyrene-divinylbenzene (PS-DVB) solid foams and their modification through post-discharge plasmas. The low-density solid foams are mainly macroporous, but show a small fraction of mesopores; their characterization revealed differences in topography between the smoother surface and the rougher bulk, while from the chemical point of view both regions of the PS-DVB solid foams are hydrophobic. The macroporous structure of these materials with high pore volume makes them interesting for the design of new drug delivery systems, but some active principles and the physiological media are hydrophilic; therefore, it would be of interest to modify the wettability of the materials via post-discharge plasma treatments. [source] Effect of tetramethylpyrazine on potassium channels to lower calcium concentration in cultured aortic smooth muscle cellsCLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 10 2003Kar-Lok Wong Summary 1.,Tetramethylpyrazine (TMP) is one of the active principles contained in Ligusticum chuanxiong Hort. (Umbelliferae), a herb that has been used widely in China to treat vascular disorders. 2.,In an attempt to elucidate the possible mechanisms of action of TMP, the effect of TMP on intracellular calcium concentrations ([Ca2+]i) was investigated in cultured vascular smooth muscle (A7r5) cells using the Ca2+ -sensitive dye Fura-2 as an indicator. 3.,The increase in [Ca2+]i in A7r5 cells produced by vasopressin (1 µmol/L) or phenylephrine (1 µmol/L) was attenuated by TMP in a concentration-dependent manner. Only inhibitors specific to ATP-sensitive potassium (KATP) channels or small conductance calcium-activated potassium (SKCa) channels attenuated the action of TMP (10 µmol/L) on [Ca2+]i. However, blockers of other K+ channels failed to modify the inhibitory action of TMP (10 µmol/L) on [Ca2+]i. 4.,The action of TMP on membrane potential in A7r5 cells was monitored by the fluorescence of bisoxonol. Tetramethylpyrazine caused a concentration-dependent inhibition of changes in membrane potential elicited by KCl (20 mmol/L) or phenylephrine (1 µmol/L), an effect that was totally reversed by glibenclamide (100 µmol/L) and apamin (100 nmol/L) in combination. 5.,The results obtained indicate that the decrease in [Ca2+]i in A7r5 cells produced by TMP is mediated mainly by opening of KATP and/or SKCa channels. [source] | |||||||||||||||||||