bluuebunny/crossref_metadata_2025_split huggingface dataset:
The effect of papaverine on acute opiate withdrawal in guinea pig ileum
Authors: Capasso Anna , Loizzo Alberto 
Published: August 2003

AbstractIn the present work the effect of papaverine, a non speciﬁc smooth muscle relaxant, was investigated on the naloxone‐precipitated withdrawal contracture of the acute morphine‐dependent guinea‐pig ileum in vitro. Furthermore, the effect of papaverine was also considered on DAGO (highly selective µ‐agonist) and U50‐488H (highly selective k‐agonist) withdrawal to test whether the possible interaction of papaverine on opioid withdrawal involves µ‐ and/or k‐opioid receptors. Following a 4 min in vitro exposure to opioid agonist, the guinea‐pig isolated ileum exhibited a strong contracture after the addition of naloxone. Papaverine treatment (1 × 10−7 − 5 × 10−7 − 1 × 10−6 M) before or after the opioid agonists was able of both preventing and reversing the naloxone‐induced contracture after exposure to µ (morphine and DAGO) or k (U50‐488H) opiate agonists in a concentration‐dependent fascion. Both acetylcholine response and electrical stimulation were not affected by papaverine treatment whereas the ﬁnal opiate withdrawal was still reduced.The results of the present study indicate that papaverine was able to produce signiﬁcative inﬂuence on the opiate withdrawal in vitro and papaverine was able to exert its effect both at µ and k opioid agonists. Copyright © 2003 John Wiley & Sons, Ltd.
The hepatoprotective effects of Limonium sinense against carbon tetrachloride and β‐D‐galactosamine intoxication in rats
Authors: Chaung Shang‐Shing , Lin Chun‐Ching , Lin Julian , Yu Kuo‐Ho , Hsu Yu‐Fang , Yen Ming‐Hong 
Published: August 2003

AbstractIn the present study, the hepatoprotective action of Limonium sinense (Plumbaginaceae) was evident after carbon tetrachloride (CCl4) and β‐D‐galactosamine (D‐GalN), respectively, challenge in rats. The plant materials were divided into two parts: (1) the roots extracted with water (WRE) and (2) the leaves extracted with methanol and fractionated with chloroform (CLE). Both WRE and CLE were extremely ﬂavonoid‐enriched extracts.In an CCl4‐induced acute liver damage study, pretreatment with WRE at 300 mg/kg i.p. and CLE at 100 mg/kg i.p. signiﬁcantly reduced the amino‐transaminases levels of SGOT (p < 0.01) and SGPT (p < 0.01) previously increased by CCl4 intoxication. In D‐GalN‐induced acute liver damage study, administration of WRE (300 and 500 mg/kg) or CLE (100 mg/kg) p.o. also signiﬁcantly reduced the SGOT (p < 0.01) and SGPT (p < 0.01) levels previously increased by D‐GalN intoxication. Furthermore, the serum triglyceride level was increased after pretreatment with WRE or CLE previously reduced by D‐GalN intoxication. All of the liver function proﬁles were conﬁrmed to have improvement of liver lesion in histopathological obsvervation.In an acute toxicity test on ICR mice, the LD50 of WRE was 777.6 mg/kg i.p. An in vitro study showed that CLE possessed a more potent cytotoxicity to human hepatocellular carcinoma cells (Hep3B) (EC50 = 43.1 µg/mL) than the other organic fractions, which were fractionated from methanol extracts of the leaves of L. sinense. The present results conclude that L. sinense possesses a hepatoprotective efﬁcacy, and is relatively safe in rats. Copyright © 2003 John Wiley & Sons, Ltd.
Smooth muscle contraction induced by Indigofera dendroides leaf extracts may involve calcium mobilization via potential sensitive channels
Authors: Amos S. , Binda L. , Kunle O. F. , Okafor I. , Emeje M. , Akah P. A. , Wambebe C. , Gamaniel K. 
Published: August 2003

AbstractThe contractile effects of the aqueous extract of the leaves of Indigofera dendroides (ID) were studied on the gastrointestinal motility in mice and isolated smooth muscle preparations obtained from rats and guinea pigs. The contractile effects of 10−6 M acetylcholine, 80 mM KCl and 1.6 mg/ml ID were measured on the rat ileal smooth muscle exposed to calcium‐free buffer or physiological solution, to determine the calcium pools mobilized by extract for activation of contraction. Acute toxicity test (LD50) was also carried out in mice. The result showed that ID (0.05–3.2 mg/ml) produced a concentration‐dependent contraction of the guinea pig and rat ileum. These responses were not blocked by mepyramine (2.49 × 10−9 M), verapamil (8.14 × 10−9 M), or pirenzepine (4.7 × 10−7 M), but were blocked completely by atropine (2.92 × 10−9 M). A signi.cant increase in propulsion of gastrointestinal motility was observed. Acetylcholine, KCl and ID produced contractions in Ca2+ free media. The phasic components of the contractile responses to Ach as well as the tonic component of K+ and ID‐induced contractions were relatively resistant to short periods of calcium‐free exposure. Ach, K+ and ID still caused contractions in the presence of verapamil. The data revealed that ID‐induced contractions were not mediated by histaminergic receptors, calcium channels, M1 muscarinic receptors. It also suggests that Ach mobilize Ca from some tightly bound or intracellular pool, whereas high K+ and ID may mobilize Ca from some superficial or loosely‐bound pool. Copyright © 2003 John Wiley & Sons, Ltd.
Antifungal activity of Mahonia aquifolium extract and its major protoberberine alkaloids
Authors: Volleková Anna , Košt'álová Daniela , Kettmann Viktor , Tóth Jaroslav 
Published: August 2003

AbstractThe crude extract of Mahonia aquifolium (Berberidaceae) stem bark and its components berberine, palmatine and jatrorrhizine were screened for their inhibitory activity against a variety of dermatophytes and two Candida species of human origin using the in vitro dilution agar plate method. Jatrorrhizine was found to be the most effective against all fungal species tested (MIC ranges from 62.5 to 125 µg/mL), while the crude extract, berberine, and palmatine exhibited only marginal activity (MIC 500 to ≥ 1000 µg/mL). Dermatophytes were more susceptible to jatrorrhizine than yeasts, and Scopulariopsis brevicaulis appeared the least sensitive species to all the compounds tested. The effects of the alkaloids were compared with those of .uconazole and bifonazole for which the MIC ranges were 12.5 to >100 µg/mL. Our results suggest that jatrorrhizine may serve as a leading compound for further studies to develop new antifungal agents with highly potent antifungal activity and low host toxicity. Copyright © 2003 John Wiley & Sons, Ltd.
Exploring the consistency of logP estimation for substituted coumarins
Authors: Vrakas Demetris , Tsantili‐Kakoulidou Anna , Hadjipavlou‐Litina Dimitra 
Published: August 2003

AbstractThe lipophilicity of a series of substituted coumarins was investigated by experimental and calculative approaches. The compounds contain substituted amidoximes, or substituted heterocycles directly attached at position 4 of the coumarinic skeleton. The reliability of the predictions produced by 8 different calculation systems was evaluated considering the absolute differences and the correlation between experimental and calculated logP values. The calculation procedure based on electrotopological state indices provided better results than the fragmental and atomic contribution systems applied. The consistency of the predictions based on the fragmental or atomic contribution systems was further explored by comparing the contribution of certain structural characteristics, defined as special π constants, in the experimental and estimated logP values. Differences between the heterocyclic and the original benzene π constants were found to affect the predictions. They might be attributed to the contribution of electronic effects as further supported by the factorization of logP in bulk and electronic terms. The same factors were found to be significant for the calculated logP values derived on the basis of the Electrotopological State Indices.
3D‐QSAR and Docking Study of the Binding Mode of Steroids to Progesterone Receptor in Active Site
Authors: Chen HaiFeng , Li Qiang , Yao Xiaojun , Fan BoTao , Yuan ShenGang , Panaye A. , Doucet J. P. 
Published: August 2003

AbstractAutodock 3.0 was applied to the search for the binding mode of a set of steroids with progesterone receptor (PR). The results of docking investigation show that oxygen atom of 3‐keto forms three hydrogen bonds with the residues Gln725 and Arg766 respectively. This is consistent with the reported work of S. P. Williams et al. (Nature, 1998, 393, 392–396). Moreover, we have studied in particular the most affinitive compound, steroid with a para alkylthio substituent of benzene at position 11. We find that there is a deep cavity around this substituent and a wide cavity around the substituent on position 17. This result could help us to select substituents to improve the PR‐binding affinity of steroids. The most probable aligned conformers were selected by a docking‐guided conformation selection method, and all‐orientation and all‐placement searches were applied to optimize CoMFA and CoMSIA models. Stable and highly predictive 3D‐QSAR models were built with cross‐validated coefficients q2 0.773 and 0.699 respectively for CoMFA and CoMSIA. The predictive ability of these models was validated using a test set. The results agree with those obtained from the docking investigations.
Evaluation of Vitreous and Starchy Syrian Durum (Triticum Durum) Wheat Grains: The Effect of Amylose Content on Starch Characteristics and Flour Pasting Properties
Authors: El‐Khayat Ghassan H. , Samaan Jihad , Brennan Charles S. 
Published: August 2003

AbstractThe physiochemical composition of durum wheat cultivars was studied in order to investigate the influence of vitreousness on the chemical composition of starch and its thermal and pasting properties. Six durum wheat lines were chosen and grown in northern Syria. Grains of each cultivar were visually sorted according to the degree of vitreousness into fully vitreous and fully starchy fractions. Amylose/amylopectin ratio and total starch was determined using Megazyme methods, while thermal and pasting properties were determined using DSC and RVA. Starchy kernels were higher in total starch than vitreous kernels but showed a decreased amylose content. Negative linear relations were found between amylose content, and both peak viscosity and breakdown. Trends in variation of gelatinisation characteristics were observed between vitreous and starchy kernels from the same cultivar, with higher total enthalpy being associated with starchy grains compared with vitreous grains of the same line.
Cross dating (Th/U-14C) of calcite covering prehistoric paintings in Borneo
Authors: Plagnes Valérie , Causse Christiane , Fontugne Michel , Valladas Hélène , Chazine Jean-Michel , Fage Luc-Henri 
Published: August 2003

AbstractWe present the first application of cross-dating (Th/U measured by thermo-ionization mass spectrometry (TIMS) and 14C measured by accelerator mass spectrometry (AMS)) of calcite covering prehistoric paintings. Th/U age estimates of cave drapery range from 9800 to 27,300 yr B.P. while conventional 14C age is estimated between 9900 and 7610 yr B.P. depending on the dead carbon correction. The age discrepancy is attributed to a disturbance of Th/U and/or 14C geochemical systems, showing the limits of the geochronological approach applied to this kind of material. For the Th/U system, the poor consistency of U data (U content, 234U/238U activity ratios) and apparent ages argue for open system conditions. For 14C system, variation of the dead carbon fraction (dcf) and a possible mixing of successive generations of calcite could account for age discrepancy. Nevertheless, one sample shows concordant ages for the two methods. Compatible ages through corrections for open system conditions are assumed for other samples. Then, the cross-dating suggests 9900 yr as the minimum age of the piece of drapery; the underlying painting must be older. This study of rock art demonstrates the presence of a Pleistocene population before 9900 yr in the southeast of Borneo, whereas previously the only population in evidence in this area was of Austronesian type from ∼5000 to 6000 yrs ago.
The effects of therapeutic vs. high‐intensity ultrasound on the rabbit growth plate
Authors: Lyon Roger , Liu Xue C. , Meier Joshua 
Published: August 2003

AbstractSix of 6‐week‐old NZ rabbits underwent ultrasound treatment using a therapeutic dose (0.5 W/cm) and other six were treated with a higher dose (2.2 W/cm2) to the lateral aspect of the left knee joint for 20 min per day and a total of six weeks. The right knee joint served as a control. The goal of this study is to see if the therapeutic dose and high dose (approximately 45‐fold therapeutic dose) will have toxic effects on the physis. Histological review appeared normal growth plate in the therapeutic group. In the high dosage group three of six cases displayed flattening of the distal femoral epiphysis and wedging of the proximal tibial plateau and indistinct growth plate lines. It is of interest to note that there are opening radiolucent area in the lateral aspect on the femoral metaphysis in five of six cases, where bone resorption has taken place. Histological results showed that there are disordered arrays of the cartilaginous cells in the proliferative zone. The height of the lateral physis in the high dose group is not only greater than that in the therapeutic dose (1083.8 vs. 500.3 μm), but also greater than that in their contralateral control (530.7 μm) (P < 0.05). This short‐term study demonstrates that high dose ultrasound has profound pathologic effects in growing bone. Therapeutic doses of ultrasound do not have an adverse effect on bone growth in the short‐term follow‐up. © 2003 Orthopaedic Research Society. Published by Elsevier Science Ltd. All rights reserved.
Extracorporeal shock wave therapy for plantar fasciitis. A double blind randomised controlled trial
Authors: Speed C. A. , Nichols D. , Wies J. , Humphreys H. , Richards C. , Burnet S. , Hazleman B. L. 
Published: August 2003

AbstractBackground: Extracorporeal shock wave therapy (ESWT) is an increasingly popular therapeutic approach in the management of a number of tendinopathies. Benefit has been shown in calcific tendinitis of the rotator cuff, but evidence for its use in non‐calcific disorders is limited.Aims: To perform a double blind randomised controlled trial of moderate dose shock wave therapy in plantar fasciitis.Methods: Adults with plantar fasciitis for at least 3 months were randomised to receive either active treatment (0.12 mJ/mm) or sham therapy, monthly for 3 months. Pain in the day, nocturnal pain and morning start‐up pain were assessed at baseline, before each treatment and 1 and 3 months after completion of therapy.Results: Eighty‐eight subjects participated and no differences existed between the groups at baseline. At 3 months, 37% of the subjects in the ESWT group and 24% in the sham group showed a positive response (50% improvement from baseline) with respect to pain. Positive responses in night pain occurred in 41% and 31% in the ESWT and sham groups, respectively. Positive responses in start‐up pain occurred in 37% and 36% in the ESWT and sham groups, respectively. Both groups showed significant improvement over the course of the study, but no statistically significant difference existed between the groups with respect to the changes were seen in any of the outcome measures over the 6‐month period.Conclusions: There appears to be no treatment effect of moderate dose ESWT in subjects with plantar fasciitis. Efficacy may be highly dependent upon machine types and treatment protocols. Further research is needed to develop evidence based recommendation for the use ESWT in musculoskeletal complaints. © 2003 Orthopaedic Research Society. Published by Elsevier Science Ltd. All rights reserved.
PGE2 and IL‐6 production by fibroblasts in response to titanium wear debris particles is mediated through a Cox‐2 dependent pathway
Authors: Bukata Susan V. , Gelinas Jill , Wei Xiaochao , Rosier Randy N. , Puzas J. Edward , Zhang Xinping , Schwarz Edward M. , Song Xiao‐yu R. , Griswold Don E. , O'Keefe Regis J. 
Published: August 2003

AbstractAseptic loosening of orthopaedic implants is precipitated by wear debris‐induced osteolysis. Central to this process are the pro‐inflammatory mediators that are produced in response to wear by the fibroblastic cells, which comprise the majority of periprosthetic membranes. Since this pro‐inflammatory cascade is mediated by a plethora of factors with redundant functions, it is imperative to establish a hierarchy. Two well‐known fibroblast derived pro‐inflammatory factors that stimulate wear debris‐induced osteoclastic resorption are prostaglandin E2 (PGE2) and IL‐6. However, their relationship to each other in this process is poorly defined. Here we show immunohistochemistry of retrieval membranes indicating that COX‐2 is the principal cyclooxygenase responsible for PGE2 production in fibroblasts around failed implants. We also performed in vitro experiments with fibroblasts derived from wild‐type (WT), COX‐1 (–/–) and COX‐2 (–/–) mice, which demonstrated that COX‐2 is required for Ti wear debris‐induced PGE2 production. Interestingly, COX‐2 was also required for IL‐6 production in these assays, which could be rescued by the addition of exogenous PGE2 (10−6 M). Pharmacology studies that utilized the COX‐1 selective inhibitor SC 560, the COX‐2 selective inhibitor celecoxib, and the nonselective COX inhibitor indomethacin confirmed these results. Taken together, these results indicate that selective inhibition of prostaglandin signaling could favorably impact aseptic loosening beyond its direct effects on PGE2 synthesis, in that it inhibits downstream pro‐inflammatory/pro‐osteoclastic cytokine production. © 2003 Orthopaedic Research Society. Published by Elsevier Ltd. All rights reserved.
Protecting the Heart: Will studying the young save the old?
Authors: Strauss Evelyn 
Published: August 2003

A little bit of a bad thing can be good for you--but this truism might not apply equally to the old and the young. A variety of minor biochemical and physical assaults on cells and organs can protect them later from more severe forms of the same--or even different--insults. Some drugs that exploit this phenomenon to protect animals and potentially people from permanent heart damage might not work as well in old organisms as in young ones, according to a new study. Schulman and colleagues subjected old rats to one of three drugs that shield younger ones from subsequent heart damage. Afterward, the team blocked blood supply to the heart for 35 minutes before allowing it to flow again. This treatment mimics heart attack and open-heart surgery, where physicians chemically stop the heart while working on it. The drugs significantly reduced the degree of destruction--as measured by the amount of dead heart tissue--in the young animals but not in the old ones. No one yet knows if these results apply to humans, but they raise questions about the wisdom of a common practice: proceeding from promising results in young animals to clinical studies in old humans, the population most affected by heart attacks and open-heart surgery.
--Evelyn Strauss; suggested by Kathy Rosewell

D. Schulman, D. S. Latchman, D. M. Yellon, Effect of aging on the ability of preconditioning to protect rat hearts from ischemia-reperfusion injury.
Am. J. Physiol. Heart Circ. Physiol.
281
, H1630-H1636 (2001).
[Abstract]
[Full Text]
Working Out the Kinks: Fly enzyme reverses protein damage, extends life-span (Protein damage)
Authors: Davenport R. John 
Published: August 2003

Getting bent out of shape isn't good for a person's blood pressure--or for proteins. Over time, cellular proteins accumulate chemical changes that can distort their shapes and disrupt their functions. Keeping these alterations at bay might help an aging organism maintain its youthful vigor. New results support that idea by indicating that extra doses of a protein-repairing enzyme help flies live longer, at least under certain conditions.
Two amino acids--aspartate and asparagine--can spontaneously undergo changes that convert them to another chemical form, called isoaspartate. The transformation reshuffles the carbon atoms in the amino acids. This perturbation puts a kink in the backbone of a protein that contains the amino acids, which distorts the shape of the protein and can prevent it from performing its cellular duties. To combat this affront, organisms carry an enzyme called protein carboxyl methyltransferase (PCMT), which converts isoaspartate back to aspartate and restores the backbone to its proper line.

Because isoaspartates accumulate as organisms age, Chavous and colleagues wondered whether supplementary PCMT would increase an animal's life-span. To find out, the researchers manipulated amounts of PCMT in the fruit fly
Drosophila melanogaster.
They engineered some flies to produce large amounts of PCMT all the time and other flies to produce extra protein only at higher than normal temperatures. They grew both sets of flies, along with a control group, at either room temperature or the elevated temperature and waited for the flies to die.

At the elevated temperature, both types of experimental flies lived about 35% longer on average than did control flies. At room temperature, however, neither set of test flies lived longer than normal. The results suggest that enhanced protein-repairing power can help flies endure, but only at elevated temperatures. It's not clear why supplemental PCMT doesn't extend the life-span of flies grown at room temperature. PCMT might require the assistance of heat shock proteins, whose amounts shoot up with temperature and which help cells maintain protein integrity. These proteins--which unfold and refold other proteins to help them maintain their proper shape--might help PCMT gain access to the altered amino acids. Alternatively, extra PCMT might make a measurable difference only when isoaspartates accumulate rapidly, as they do at higher temperatures. The work hints that keeping the kinks out of proteins--especially under stressful conditions such as high temperature--might stretch out an animal's life-span.
--R. John Davenport; suggested by Amir A. Sadighi Akha

D. A. Chavous, F. R. Jackson, C. M. O'Connor, Extension of the
Drosophila
lifespan by overexpression of a protein repair methyltransferase.
Proc. Natl. Acad. Sci. U.S.A.
98
, 14814-14818 (2001).
[Abstract]
[Full Text]