Wyniki wyszukiwania - Biblioteka Nauki

1

Gastroprotective effects of Prunus laurocerasus L. fruit extracts against the oxidative stress induced by indomethacin in rats

100%

Aydin Berktas O. , Keskin A. , Gulec Peker E. G.

European Journal of Clinical and Experimental Medicine

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2022

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nr 3

284-289

EN

Introduction and aim. Prunus laurocerasus L. is a perennial plant belonging to the Rosaceae family and is grown on the shores of the Black Sea Region. In the current study, the effect of P. laurocerasus fruits was investigated in the ulcer model created by the application of indomethacin to rats. Material and methods. Rats divided into five groups: fruit water extract (200 mg/kg), fruit ethanol-water extract (200 mg/kg), lansoprazole agent (LAN, 25 mg/kg), and indomethacin (IND, 25 mg/kg). All administrations were given to animals by oral gavage. At the end of the experiment, macroscopic and biochemical measurements were made in rats. Results. The lipid peroxidation was quite high in rat stomach tissues given IND. The applied LAN and extracts reduced this increase to almost a healthy rate. On the other hand, the amount of glutathione, catalase, and superoxide dismutase activities were found very low in IND applied tissues. The LAN and fruit extracts treatments tried to show their protective feature by increasing this decreased antioxidant level in their own groups. Conclusion. The data obtained determined that both enzyme and non-enzyme antioxidant markers measured in fruit extracts had a protective effect almost as strong as lansoprazole.

2

FORMULATION AND EVALUATION OF INDOMETHACIN LOADED NANOSPONGES FOR ORAL DELIVERY

88%

Abbas N. , Sarwar K. , Irfan M. , Hussain A. , Mehmood R. , Arshad M. S. , Shah P. A.

Acta Poloniae Pharmaceutica - Drug Research

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2018

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tom 75

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nr 5

1201-1213

EN

Nanosponges (NS) loaded sustained release tablet formulations of a non-steroidal anti-inflammatory drug; Indomethacin were successfully developed and evaluated for their pharmaceutical properties. Twelve nanosponge formulations were fabricated by solvent diffusion method by using different ratios of drug and polymers (ethyl cellulose and polyvinyl alcohol). Particle size of all the formulations was in the nano range of 221 to 625 nm and it was found dependent on the polymer concentration. Drug loading and entrapment efficiency was ranged in 32.2 to 59.4 % and 30.1 to 64.8 %, respectively. Formulations with equal proportion of drug and polymer resulted in higher values of drug loading and entrapment efficiency. Percent yield was also found dependent on the relative drug polymer ratio with highest value of 51 % was achieved for the formulation having same drug to polymer ratio. SEM results confirmed the formation of spherical and porous structures. Structural analysis by Fourier transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) showed the absence of any interaction between drug and polymer. In comparison to pure drug, NS formulations showed a linear intrinsic dissolution rate (IDR) profile depicting a controlled release profile. Diffusion studies of NS formulations performed by Franz diffusion cell and dialysis bag methods showed comparable results in terms of precision and linearity of diffusion profile. Tablets prepared from the drug loaded NS showed acceptable values for hardness, friability and drug content. Release of drug from NS tablets was confirmed as sustained release behaviour.

3

RELEASE AND PERMEATION OF INDOMETHACIN FROM PHOSPHOLIPID COMPLEX FILM GENERATED FROM SPRAY FORMULATIONS

88%

Buatong W. , Nakpheng T. , Dechraksa J. , Saisamuth S.-a. , Kongkhao W. , Srichana T.

Acta Poloniae Pharmaceutica - Drug Research

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2019

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tom 76

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nr 2

329-339

EN

An indomethacin topical spray was prepared using lecithin and a cholesterol derivative as a phospholipid complex in a film. Polyvinylpyrrolidone (PVP) was used as a film-forming agent. Drug penetration through keratinocytes was evaluated as well as cytotoxicity to the keratinocytes and fibroblast cells. The results reveal that the PVP concentration provided fine droplets under a microscope with a low contact angle (12.07°-22.53°). Incorporating PVP in the formulation reduced the hydrodynamic radius or size by 20 times. The SEM and TEM results showed smoother surfaces of the thin film for larger quantities of the PVP film-forming agent in the formulations. It also gave the highest drug penetration when the PVP was 0.5%. However, the film-forming agent can also act as a control release barrier. The percent viabilities of the human keratinocytes and fibroblasts were higher in the indomethacin spray phospholipid complex thin film formulation than the pure drug.

4

Inhibitory effects of indomethacin on growth and proliferation of gastric carcinoma cells Kato III

88%

Fujiwara Y. , Tarnawski A. , Fujiwara K. , Arakawa T. , Kobayashi K.

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nr 2

5

Anti-inflammatory activity of Turkey source pumpkin seed oil in rat oedema model

75%

Arslanbaş E. , KARA H. , KARAYİĞİT M. Ö. , DOĞAN H. O. , YILDIZ Ş. N.

Acta Poloniae Pharmaceutica - Drug Research

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2020

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tom 77

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nr 2

305-312

EN

This study aimed to determine the effects of Turkey-sourced pumpkin seed oil (PSO), administered orally to rats in different dosages, to research its anti-inflammatory effect in rat oedema model, induced by carrageenan, based on different dosages, and to evaluate its effects comparatively with indomethacin. The study was conducted on 42 rats in total, divided into 7 groups (control, carr, PSO40, PSO100, PSO40+carr, PSO100+carr and indo+carr). In the study, doses of 40 and 100 mg/kg of PSO were found to significantly suppress rat paw oedema in time, and it was observed that this effect was more pronounced in the fourth hour. It was found that MDA and cytokine (TNF-α, IL-6, IL-1β) levels were inhibited, and GPX and SOD activities were enhanced in groups that received PSO and indo+carr groups. Histopathological examinations also support these findings. As a result of the study, the significant anti-inflammatory effect of Turkey-sourced PSO was attributed to the existence of unsaturated fatty acids and enriched phytochemical compounds.

6

Effects of indomethacin and rofecoxib on gastric mucosal damage in normal and Helicobacter pylori - infected Mongolian gerbils

75%

Kanatani K. , Ebata M. , Murakami M. , Okabe S.

Journal of Physiology and Pharmacology

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2004

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tom 55

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nr 1,2

EN

This study examined the effects of indomethacin and rofecoxib on normal and Helicobacter pylori (H. pylori)-infected gastric mucosa of Mongolian (M.) gerbils. M. gerbils (6-wk-old) were orally administered H. pylori (ATCC43504, 2×108 CFU/ml) after fasting for 24 hours. Beginning 3 mo after inoculation, indomethacin (2 mg/kg, s.c) or rofecoxib (10 mg/kg, p.o.) was administered once daily for 2 wk to the gerbils. At autopsy, gastric mucosal ulcer area, myeroperoxidase (MPO) activity, prostaglandin (PG) E2 synthesis, and H. pylori viability were determined. Histamine-stimulated gastric acid secretion was measured with the acute gastric fistula method. Histological study was performed with H&E staining. H. pylori infection caused severe mucosal damage and production of lymphoid follicles in the gastric submucosa. In H. pylori-infected gerbils, indomethacin aggravated the gastric mucosal damage induced by H. pylori infection. Furthermore, indomethacin by itself induced gastric ulcers at an incidence of 6/10. In contrast, rofecoxib did not aggravate the H. pylori-induced mucosal damage. Indomethacin and rofeocoxib significantly reduced H. pylori viability. MPO activity was significantly increased in H. pylori-infected gerbils compared with H. pylori-uninfected gerbils. Indomethacin and rofecoxib reduced MPO activity in H. pylori-infected gerbils. PGE2 synthesis was markedly increased in H. pylori-infected gerbils (approximately 3-times) compared with the normal gerbils. Indomethacin significantly inhibited PGE2 synthesis in the gastric mucosa, both in normal and H. pylori-infected gerbils. Rofecoxib did not reduce PGE2 synthesis in normal gerbils, however, PGE2 synthesis was reduced to normal levels in H. pylori-infected gerbils. In H. pylori-infected gerbils, histamine-stimulated gastric acid secretion was reduced compared with normal gerbils. Indomethacin significantly increased histamine-stimulated gastric acid secretion and rofecoxib tended to increase secretion in H. pylori-infected gerbils. It was concluded that indomethacin enhances development of gastric mucosal damage in normal gerbils and aggravates H. pylori-induced gastric damage, resulting in gastric ulcers. Rofecoxib did not induce gastric damage in normal gerbils and did not aggravate damage in H. pylori-infected gerbils, suggesting that rofecoxib is less damaging to the stomach than indomethacin.

7

Effect and mechanism of sucralfate on healing of acetic acid-induced gastric ulcers in rats

75%

Ogihara Y. , Okabe S.

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nr 2

8

The influence of indomethacin on the ACTH secretion induced by central stimulation of adrenergic receptors

75%

Glod R. , Gadek-Michalska A. , Bugajski J.

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nr 2

9

Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity

75%

Kocaoglu S. , Karan A. , Berkan T. , Basdemir G. , Akpinar R.

Archivum Immunologiae et Therapiae Experimentalis

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1997

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tom 45

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nr 1

10

Effects of sucralfate and its components on indomethacin-induced damage to cultured rabbit gastric mucosal cells

75%

Takahashi S. , Okabe S.

Journal of Physiology and Pharmacology

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1996

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tom 47

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nr 4

11

Oenothera paradoxa defatted seeds extract containing pentagalloylglucose and procyanidins potentiates the cytotoxicity of vincristine

63%

Jaszewska E. , Kosmider A. , Kiss A. K. , Naruszewicz M.

Journal of Physiology and Pharmacology

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2010

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tom 61

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nr 5

12

Role of prostaglandins in heme-induced fever

63%

Walentynowicz K. , Szefer M. , Wojtal B. , Terlecki P. , Wrotek S. , Kozak W.

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nr 8

73-82

EN

Brain stroke is often accompanied by a high fever, which is insensitive to a blockade with classic antipyretic drugs known to inhibit the synthesis of prostaglandin E2 (PGE2), a proximal mediator of fever associated with infection. The molecular mechanism of fever associated with stroke is mostly unknown, and has not been thoroughly investigated. One characteristics of the stroke is an extravasation of the erythrocytes into the brain tissue followed by a release of hemoglobin and free heme. In the present study we have tested the hypothesis that free heme itself can induce fever after releasing into the brain. The study was conducted on Sprague Dawley rats instrumented with biotelemetry devices to monitor deep body temperature, and implanted with brain cannulae projected to the lateral ventricle. We demonstrate that heme-L-lysinate microinfused intraventricularly (icv) induces a dose-dependent fever lasting ca. 8 hours. Injection of heme-L-lysinate provoked a significant elevation of PGE2 in the rat cerebro-spinal fluid collected 3 hours post-injection. The fever induced by heme-L-lysinate was blocked by an icv injection of anti- PGE2 antibody. It was not affected, however, by intraperitoneal administration of indomethacin, a cyclooxygenase inhibitor. We conclude that heme-induced fever may underlie the stroke fever.

13

Vulnerability of gastric and small intestinal mucosa to ulcerogenic action of indomethacin in C57/BL6/J mice and transient receptor potential channel vanilloid type 1 knockout mice

63%

Yarushkina N. I. , Sudalina M. N. , Punin Y. M. , Filaretova L. P.

Journal of Physiology and Pharmacology

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2018

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tom 69

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nr 6

14

Role of COX inhibition in pathogenesis of NSAID-induced small intestinal damage

63%

Takeuchi K. , Tanaka A. , Ohno R. , Yokota A.

Journal of Physiology and Pharmacology. Supplement

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2003

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tom 54

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nr 4

165-182

EN

Nonsteroidal antiinflammatory drugs (NSAIDs) such as indomethacin decrease mucosal PGE2 production by inhibiting cyclooxygenase (COX) activity and produce damage in the small intestine. The development of intestinal lesions as induced by indomethacin was accompanied by increases in intestinal motility, enterobacterial invasion, and myeloperoxidase (MPO) as well as inducible nitric oxide synthase (iNOS) activity, together with the up-regulation of COX-2 and iNOS mRNA expression. Neither the selective COX-1 inhibitor, SC-560, nor the selective COX-2 inhibitor, rofecoxib, alone caused intestinal damage, but their combined administration produced lesions. SC-560, but not rofecoxib, caused intestinal hypermotility, bacterial invasion and the expression of COX-2 as well as iNOS mRNAs, yet the iNOS and MPO activity was increased only when rofecoxib was administered together with SC-560. Although SC-560 inhibited the PG production, the level of PGE2 was recovered, in a rofecoxib-dependent manner. The intestinal hypermotility response to indomethacin was prevented by both 16,16-dimethyl PGE2 and atropine but not ampicillin, yet all these agents inhibited not only the bacterial invasion but also the expression of COX-2 as well as the iNOS activity in the intestinal mucosa following indomethacin treatment, resulting in preventing the intestinal lesions. These results suggest that inhibition of COX-1, despite causing intestinal hypermotility, bacterial invasion and iNOS expression, up-regulates the expression of COX-2, and the PGE2 derived from COX-2 counteracts deleterious events caused by COX-1 inhibition and maintains the mucosal integrity. These sequences of events explain why intestinal damage occurs when both COX-1 and COX-2 are inhibited.

15

Assessment of neurotoxicity of pharmacological compounds during early neural development of human embryonic stem cells

63%

Kang H. Y. , Hong E. J. , Kang H. S. , Ahn C. , Jeung E. B.

Journal of Physiology and Pharmacology

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2017

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tom 68

|

nr 2

16

Leukotrienes in mucosal damage and protection

63%

Peskar B. M.

Journal of Physiology and Pharmacology

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1991

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tom 42

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nr 2

EN

Exposure of the rat gastric mucosa to ethanol stimulates the generation of leukotriene (LTC₄) and 15-hydroxyeicosatetraenoic acid, hut not of thromboxanes and prostaglandins. Lipoxygenase activation is not found with other topical irritants or nonsteroidal anti-inflammatory drugs. A number of gastroprotective drugs dose-dependently inhibit the stimulatory action of ethanol on mucosal LTC₄ formation closely parallel to their protective activity suggesting that ethanol-induced damage and activation of lipoxygenases may involve common targets which are simultaneously counteracted by certain types of protective agents. Selective inhibition of 5-lip- oxygenase, however, does not confer protection against gastric mucosal damage caused by topical irritants or non-steroidal anti-inflammatory drugs. Thus, although leukotrienes may mediate certain reactions elicited by gastric ulcerogens such as submucosal venular constriction and mucosal micro vascular engorgement, they do not appear to be major mediators of ulcerogen-induced tissue necrosis. The contribution of other products of the various pathways of arachidonic acid metabolism to gastric mucosal injury and the mechanism underlying the close interrelationship between protection and inhibiton of LTC₄ formation observed with certain compounds remains to be investigated.

17

Effects of stress preconditioning on vulnerability of gastric and small intestinal mucosa to ulcerogenic action of indomethacin in rats

63%

Yarushkina N. I. , Filaretova L. P.

Journal of Physiology and Pharmacology

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2019

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tom 70

|

nr 6

18

Comparison of prostaglandin and cimetidine in protection of isolated gastric glands against indomethacin injury

63%

Brzozowski T. , Tarnawski A. , Hollander D. , Sekhon S. , Krause W. J. , Gergely H.

Journal of Physiology and Pharmacology. Supplement

|

2005

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tom 56

|

nr 5

75-88

EN

Prostaglandins can protect the in vivo gastric mucosa against necrosis produced by a variety noxious agents. Cimetidine has also been shown to have protective properties in humans and in some models of experimental injury. Whether prostaglandins or cimetidine may protect gastric mucosal cells directly in the absence of systemic factors remains controversial. In the present study, the potential protective actions of prostaglandin and cimetidine against indomethacin injury were assessed in isolated rat gastric glands. Gastric glands were pre-incubated in oxygenated medium with either placebo, 16,16 dimethyl prostaglandin E2 (dm PGE2) or cimetidine and incubated at 37°C in medium containing 0.5 mg/ml of indomethacin for 2, 4 and 6 hrs. Cell injury and protection was assessed by the Fast Green exclusion test (viability test), leakage of lactate dehydrogenase (LDH) into the medium, and by scanning and transmission electron microscopy. In addition, the generation of PGE2 by the gland cells was determined using RIA assay. Indomethacin by itself significantly reduced the viability of gastric glands, increased LDH release into the medium and produced prominent ultrastructural damage. In contrast to cimetidine, co-incubation of gastric glands with dm PGE2 added to indomethacin, significantly reduced indomethacin-induced injury, increased the number of viable cells, reduced LDH leakage and diminished the extent of ultrastructural damage. The dose of indomethacin (5 µg/ml) which significantly inhibited the generation of PGE2 (up to 90% inhibition) had no effect on cell viability nor LDH release. We conclude that 1) exogenous PGE2 exerts a potent protective activity in vitro which is independent on neural, vascular and hormonal factors; 2) inhibition of endogenous PGs may not the primary mechanism in the deleterious action of indomethacin against damage to gastric glandular cells and 3) indomethacin can exert a direct cytotoxic effect on the mucosal cells in gastric glands.

19

Influence of forced treadmill and voluntary wheel running on the sensitivity of gastric mucosa to ulcerogenic stimuli in male rats

63%

Yarushkina N. I. , Komkova O. P. , Filaretova L. P.

Journal of Physiology and Pharmacology

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2020

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tom 71

|

nr 6

20

Highly sensitive chemiluminescence method for determination of indomethacin using permanganate-formaldehyde system

63%

Fu Z. , Wang L.

Chemia Analityczna

|

2009

|

tom Vol. 54, No. 2

163-172

EN

A highly sensitive flow injection chemiluminescent method for determination of indomethacin has been proposed. During oxidation of indomethacin by KMnO4 in polyphosphoric acid medium, chemiluminescence emission was observed, which could be enhanced more than 100 times in the presence of 4% formaldehyde. The chemiluminescence mechanism was investigated and two emitters were identified. The proposed strategy allowed for sample assay rate of 100 per l h in an automatic mode in combination with flow injection analysis. Indomethacin could be determined over the concentration range 1.0x109-1.0x 10-1 g mL<-sub>-1 with the detection limit (3σ) of 6.0 x 10<-sub>-10 g mL<-sub>-1. The relative standard deviation for determination of 1.0 x 10<-sub>-8 g mL<-sub>-1 indomethacin (n = 11) was 2.3%. The proposed method has been successfully applied to the analysis of a commercial pharmaceutical formulation without any sample pretreatment and to biological samples after their clean-up by solidphase extraction.

PL

Do oznaczania indometacyny w przepływie zaproponowano wysoko czułą metodę wstrzy-kową wykorzystującą chemiluminescencję, obserwowaną podczas utleniania indometacyny przez KMnO4 w kwasie polifosforowym. Jej intensywność wzrastała w obecności 4% formaldehydu. Badano mechanizm powstawania chemiluminescencji i zidentyfikowano jej dwa źródła. Opracowana metoda pozwalała na zbadanie 100 próbek w ciągu godziny. Indome-tacynę można by ło oznaczy ć w zakresie stężeń 1.0x 109—1.0 x l.0<-sub>-6 g mL<-sub>-1. Granicę wykrywalności (3σ) określono jako 6.0 x l0<-sub>-9 g mL<-sub>-1. Zaproponowaną metodę zastosowano z powodzeniem do analizy handlowych preparatów farmaceutycznych bez potrzeby wstępnego przygotowania próbki. Zastosowano ją również do analizy próbek biologicznych po ich oczyszczeniu metodą ekstrakcji z fazy stałej.