共查询到20条相似文献,搜索用时 62 毫秒
1.
Preparation and Sonodynamic Antitumor Effect of Protohemin‐Conjugated Multiwalled Carbon Nanotubes Functionalized with Carboxylic Group 下载免费PDF全文
Preclinical Research |
2.
V. Motilva C. Alarcn De La Lastra M. J. Martín 《The Journal of pharmacy and pharmacology》1994,46(2):91-94
Abstract— This study was designed to determine the cytoprotective properties of naringenin and the involvement of endogenous prostaglandins on mucosal injury produced by absolute ethanol. Gastric glands were also histologically analysed. Oral pretreatment with the highest dose of naringenin (200 mg kg?1), 240 min before absolute ethanol, was the most effective in ulcer prevention. Subcutaneous administration of indomethacin (10 mg kg?1) to the animals treated with naringenin (200 mg kg?1) partially inhibited the gastric protection but there was no increase in prostaglandin E2. All treated groups showed a marked increase in gastric mucus, although this increase was less in animals pretreated with indomethacin. Total proteins and hexosamine content decreased in the groups receiving indomethacin. Histomorphometric evaluation of the gastric damage, with the highest dose of naringenin (200 mg kg?1), confirmed a significant increase of mucus production accompanied by a parallel reduction of gastric lesion. 相似文献
3.
J. V. ESPLUGUES M. D. BARRACHINA M. A. MARTÍNEZ-CUESTA S. CALATAYUD L. MORENO A. FERNANDEZ J. PUIG J. ESPLUGUES 《The Journal of pharmacy and pharmacology》1995,47(2):128-130
The study was designed to analyse the protective effects of almagate on a model of gastric injury, ethanol-induced mucosal damage, in which acid plays little, if any, role. Pretreatment with almagate dose-dependently reduced the level of gastric damage induced by oral administration of 1mL 100% ethanol. Administration of 12 μmol kg?1 almagate 30 min before ethanol significantly reduced the area of mucosal damage by 65 ± 10%, and the maximum level of inhibition (74 ± 11%) was obtained with 150 μmol kg?1 almagate. Administration of higher doses of almagate (200–250 μmol kg?1) did not result in any further increase in the level of protection against ethanol-induced gastric damage. Administration of 1 mL 100% ethanol induces substantial damage to the gastric mucosa, with nearly 40% of the length of the section evaluated exhibiting deep necrotic and haemorrhagic damage. Pretreatment with almagate caused a significant diminution in all parameters of histological damage, whereas damage to the epithelial cell layer was only significantly reduced by pretreatment with the highest doses evaluated (25, 50 and 150 μmol kg?1). Administration of aluminium hydroxide did not modify ethanol-induced mucosal damage, even at doses containing concentrations of aluminium higher than those present in gastroprotective doses of almagate. Pretreatment with sucralfate, another aluminium containing compound, at doses of 250 μmiol kg?1 protected the mucosa, although lower doses did not. The present study has shown that almagate prevents ethanol-induced gastric mucosal damage. This protective effect seems independent of any antacid activity, related to its content in magnesium, and mediated by an increase in gastroprotective prostaglandins in the mucosa of the stomach. 相似文献
4.
Schisandrae Fructus Inhibits IL‐1β‐Induced Matrix Metalloproteinases and Inflammatory Mediators Production in SW1353 Human Chondrocytes by Suppressing NF‐κB and MAPK Activation 下载免费PDF全文
Jin‐Woo Jeong Hye Hyeon Lee Eun‐Ok Choi Ki Won Lee Ki Young Kim Sung Goo Kim Su Hyun Hong Gi‐Young Kim Cheol Park Ho Kyoung Kim Young Whan Choi Yung Hyun Choi 《Drug development research》2015,76(8):474-483
Preclinical Research |
5.
Daisy Carbajal Vivian Molina Suria Valds Lourdes Arruzazabala Idania Rodeiro Rosa Ms Juan Magraner 《The Journal of pharmacy and pharmacology》1996,48(8):858-860
D?002 is an anti-ulcerogenic product, isolated from beeswax, which consists of a well-defined mixture of higher primary aliphatic alcohols. It is highly effective against ethanol-induced ulcers. This study was designed to determine if D-002 shows cytoprotective properties on gastric mucosa in ethanol-induced ulcers. The involvement of endogenous prostaglandins in the protective effect of D?002 was also investigated. When a subulcerogenic dose of indomethacin (10 mg kg?1) was injected simultaneously with oral administration of ethanol, oral pre-treatment with D-002 (5?100 mg kg?1) partially inhibited the gastric protection. D-002 (5 and 25 mg kg?1) administered to normal rats significantly increased the soluble mucus content and also prevented its reduction in rats with ethanol-induced ulcers. In addition, D-002 administered at 5 and 25 mg kg?1 prevented the increase of vascular permeability induced by ethanol (60%) and reduced the concentration of thromboxane B2 (TXB2) in gastric mucosa of rats with ethanol-induced ulcers. These results support the hypothesis that the anti-ulcerogenic properties of D-002 could be related to a cytoprotective mechanism. 相似文献
6.
Carvedilol Attenuates Inflammatory Biomarkers and Oxidative Stress in a Rat Model of Ulcerative Colitis 下载免费PDF全文
Amal J. Fatani Khaled A. Al‐Hosaini Mohammed M. Ahmed Hatem M. Abuohashish Mihir Y. Parmar Salim S. Al‐Rejaie 《Drug development research》2015,76(4):204-214
Preclinical Research |
7.
ARNALDO WILLAIN FILHO EDUARDO BREVIGLIERI VALDIR CECHINEL FILHO ADAIR R. S. SANTOS 《The Journal of pharmacy and pharmacology》1997,49(8):823-827
The analgesic effect of the hydroalcoholic extract of the stems of Bauhinia splendens (Leguminosae) has been investigated in chemical and thermal models of nociception in mice. The hydroalcoholic extract of B. splendens, 3–60 mg kg? intraperitoneally or 50–400 mg kg? orally, caused dose-related, and long-lasting (up to 3 h) inhibition of acetic acid-induced abdominal constriction in mice, with ID50 values of 3.2 and 177.6 mg kg? and maximum inhibition of 95 ± 2 and 61 ± 6%, respectively. In the formalin test, the extract given intraperitoneally (1.60 mg kg?) or orally (50–400 mg kg?) caused graded inhibition of both phases of formalin-induced pain, being about 5- to 6-fold more potent in attenuating the second phase of pain. The calculated mean ID50 values for the first and the second phases were 11.5 and 2.5 mg kg?, respectively, for intraperitoneal administration and > 200 and 70 mg kg?, respectively, for oral administration; the percentages of maximum inhibition for the first and the second phases were 68 ± 6 and 99 ± 1, respectively, for intraperitoneal administration and 37 ± 6 and 69 ± 9, respectively, for oral administration. However, at the same doses the extract did not significantly affect the oedematogenic response induced by formalin. The treatment of animals with naloxone (5 mg kg?, i.p.) completely reversed the analgesic effect caused by morphine (5 mg kg?, s.c), but had no effect against the antinociceptive effect of the hydroalcoholic extract of B. splendens (60 mg kg?, i.p.) when assessed against acetic acid-induced abdominal constrictions. Furthermore, the extract, in contrast with morphine, had no analgesic effect in the hot-plate test. These data show that the hydroalcoholic extract of B. splendens has significant analgesic action when assessed against several models of pain. The mechanism underlying its analgesic effect still remains unknown, but seems to be unrelated to interaction with opioid systems. 相似文献
8.
Angel Josabad Alonso‐Castro Julia Pérez‐Ramos Ernesto Sánchez‐Mendoza Cuauhtemoc Pérez‐González Salud Pérez‐Gutiérrez 《Drug development research》2015,76(4):185-193
Preclinical Research |
9.
β‐Ecdysterone Suppresses Interleukin‐1β‐Induced Apoptosis and Inflammation in Rat Chondrocytes via Inhibition of NF‐κB Signaling Pathway 下载免费PDF全文
Preclinical Research |
10.
Abstract— The protective mechanisms of paracetamol against ethanol-induced gastric mucosal damage have been examined. The antiulcer action of subcutaneously (s.c.)-injected paracetamol, 250 mg kg?1, was attenuated by either subdiaphragmatic vagotomy or s.c. injection of N-ethylmaleimide, 10 mg kg?1. This attenuation was not seen in rats given paracetamol by the oral route (p.o.). Indomethacin pretreatment, 5 mg kg?1, did not influence the lesion-preventing action of paracetamol given s.c. or p.o. The findings suggest that the antiulcer effect of s.c.-administered paracetamol results from an action involving the vagal nerve and tissue sulfhydryls, but not prostaglandins. On the other hand, the protective mechanism of paracetamol p.o. is independent of the vagal system or tissue sulfhydryls and prostaglandins. It seems that paracetamol given p.o. exerts its antiulcer effect by acting directly on the mucosal cell to strengthen mucosal integrity. 相似文献
11.
RAFAEL O. P. DE CAMPOS NIRALDO PAULINO CLIO H. M. DA SILVA AMARILIS SCREMIN JOO B. CALIXTO 《The Journal of pharmacy and pharmacology》1998,50(10):1187-1193
Propolis, or bee glue, which contains a complex mixture of secondary metabolites, has long been used in many countries for the management of several diseases. The purpose of this study was to evaluate, by means of several pharmacological models, the anti-hyperalgesic effect of propolis collected in the south of Brazil. The abdominal constrictions induced in mice by intraperitoneal injection of acetic acid (0.6%), kaolin (50 mg kg?1) or zymosan (40 mg kg?1) were inhibited to different extents by an extract of propolis (1–60 mg kg?1) administered intraperitoneally 30 min earlier; mean ID50 (concentrations resulting in 50% inhibition) values were 2.7, 10.8 and 10.7 mg kg?1, respectively, and maximum inhibition was 58 ± 5, 57 ± 10 and 51 ± 5%, respectively. Given orally (25–200 mg kg?1, 1 h previously) propolis also inhibited the abdominal constrictions induced by acetic acid (maximum inhibition 43 ±5%). When injected intraperitoneally (3–60 mg kg?1, 30 min previously), propolis attenuated both the neurogenic (first phase) and inflammatory (second phase) pain responses and paw oedema caused by intraplantar injection of formalin (2.5%); maximum inhibition was 32 ±5, 43 ±6 and 19 ±2%, respectively. Oral administration of propolis (25–200 mg kg?1, 1 h previously) inhibited both phases and reduced the oedema formation associated with the second phase of the formalin test (maximum inhibition 22±5, 33 ±6 and 26±3%) and extract of propolis (3–30 mg kg?1 i.p. or 25–100 mg kg?1 p.o., respectively 30 min and 1 h previously) significantly inhibited capsaicin-induced pain with maximum inhibition of 39±8 and 41 ±8%, respectively. When assessed in the Randall–Sellito test of pain, the extract of propolis (3–30 mg kg?1, i.p., 30 min previously) significantly reversed the hyperalgesia induced by intraplantar injection of bradykinin (3 nmol per paw) in rats (P < 0.01). In contrast with morphine the extract of propolis (. 100 mg kg?1, 30 min previously) was ineffective when assessed in the tail-flick and hot-plate thermal assays. Naloxone (5 mg kg?1 i.p.) reversed (P < 0.01) the effect of morphine (5 mg kg?1 s.c.) by 70 and 94% respectively in the first and second phases of the formalin test, but did not interfere with the analgesic effect of propolis (10 mg kg?1 i.p., 30 min previously). These results show that ethanolic extract of propolis, given systemically, has significant anti-hyperalgesic action when assessed in chemical, but not thermal, models of nociception in mice and rats. Its analgesic action seems to be unrelated to release or activation of the opioid system. 相似文献
12.
Combination of Diacerhein and Antiepileptic Drugs After Local Peripheral,and Oral Administration in the Rat Formalin Test 下载免费PDF全文
Angel Zúñiga‐Romero Martha Karina Ponce‐Chávez Marcia Yvette Gauthereau‐Torres Luis Fernando Ortega‐Varela 《Drug development research》2014,75(8):510-520
Preclinical Research |
13.
Reyes-Trejo B Sánchez-Mendoza ME Becerra-García AA Cedillo-Portugal E Castillo-Henkel C Arrieta J 《The Journal of pharmacy and pharmacology》2008,60(7):931-936
Croton reflexifolius H. B. K (Euphorbiaceae) is a very common medicinal plant in the Huastecan region of Mexico that, according to local folk medicine, is considered useful in the treatment of gastritis and gastric ulcer. We have aimed to test the validity of this practice by using the experimental model of an ethanol-induced gastric ulcer in male Wistar rats. The results showed that C. reflexifolius had gastroprotector activity, that the hexane extract had the highest protective activity (64.38+/-7.72%), and that polyalthic acid isolated from this extract was the main active gastroprotector agent. Rats treated orally with polyalthic acid showed a gastroprotective effect similar to that elicited by carbenoxolone. As with carbenoxolone, the effect elicited by polyalthic acid was attenuated by pretreatment with either N(G)-nitro-L-arginine methyl ester (70 mgkg(-1), i.p.), a nitric oxide (NO) synthase inhibitor, or N-ethylmaleimide (10 mgkg(-1), s.c.), a blocker of sulfhydryl groups. This suggested that the gastroprotective mechanism of this diterpenoid involved the participation of both NO and endogenous sulfhydryl groups. Contrary to carbenoxolone, the gastroprotective effect of polyalthic acid was not affected by the inhibition of prostaglandin synthesis with indometacin (10 mgkg(-1), s. c.). In conclusion, Croton reflexifolius contains compounds with gastroprotector activity. Polyalthic acid, which was isolated from this plant, was the main compound with gastroprotector activity, having effectiveness similar to that found with the use of carbenoxolone. Whereas NO and sulfhydryl groups were involved in the mechanisms of gastroprotective action of polyalthic acid, prostaglandins were not. 相似文献
14.
Preclinical Research |
15.
SAILENDRA GOSWAMI SUNITA JAIN DEVDAS SANTANI 《The Journal of pharmacy and pharmacology》1997,49(2):195-199
The effect of cromakalim, a potassium-channel opener, was studied on pylorus ligation-induced, aspirin-induced and water-immersion plus restraint stress-induced gastric ulcers in rats and on histamine-induced duodenal ulcer in guinea-pigs. Pretreatment with cromakalim (50–500 μg kg?1, p.o.) resulted in a significant reduction in the incidence of gastric and duodenal ulceration in each model. The anti-ulcer activity of cromakalim was comparable with that of cimetidine. Cromakalim at 100, 250 and 500 μg kg?1 caused a reduction in the volume of the gastric content in pylorus-ligated rats, and a dose of 250 μg kg?1 resulted in a significant reduction in total acidity (28.81 ± 11.73 mEq L?1, P < 0.02) in the pylorus ligation model. A significant reduction in total acid output was observed at doses of 250 μg kg?1 (84.27 ± 22.33 mEqH+, P < 0.02) and 500 μg kg?1 (120.17 ± 24.49 mEq H+, P < 001) in pylorus-ligated rats. A significant reduction in the ulcer index in pylorus-ligated rats was observed at all cromakalim doses: 50 μg kg?1 (0.23 ± 009, P < 0.05), 100 μg kg?1 (0.15 ± 0009, P < 0.02), 250 μg kg?1 (0.12 ± 0.05, P < 0.01) and 500 μg kg?1 (0.14 ± 0.03, P < 0.02). A significant reduction in the ulcer index of aspirin-treated rats was also observed at all cromakalim dose levels: 50 μg kg?1 (0.39 ± 0.03. P < 0.01), 100 μg kg?1 (0.28 ± 0.06, P < 0.01), 250 μg kg?1 (0.22 ± 0.04, P < 0.001) and 500 μg kg?1 (0.28 ± 0.03, P < 0.01). In the water-immersion plus restraint stress-induced gastric ulcer model, cromakalim significantly reduced gastric ulceration at all the dose levels: 50 μg kg?1 (28.2 ± 2.12, P < 0.001), 100 μg kg?1 (20.24 ± 1.71, P < 0.01), 250 μg kg?1 (19.95 ± 1.46, P < 0.001) and 500 μg kg?1 (21.61 ± 3.00, P < 0.001) but there was no consistent reduction of gastric bleeding. In addition to gastric ulcers, duodenal lesions were also reduced by pretreatment with cromakalim at all dose levels: 50 μg kg?1 (97.87 ± 20.03 mm2, P < 0.02). 100 μg kg?1 (70.72 ± 12.82 mm2, P < 0.02), 250 μg kg?1 (48.32 ± 8.42 mm2, P < 0.01) and 500 μg kg?1 (55.50 ± 12.50 mm2, P < 0.01). Cromakalim at a dose of 100 μg kg?1 also reduced total acidity (99.36 ± 9.12 mEq L?1, P < 0.02) and total acid output (172.22 ± 45.33 mEq of H+, P < 0.05) in this model. These findings demonstrate the anti-ulcer activity of cromakalim in different experimental models and suggest its potential use in ulcer therapy. 相似文献
16.
Isobolographic Analyses of Proglumide–Celecoxib Interaction in Rats with Painful Diabetic Neuropathy
《Drug development research》2017,78(2):116-123
Preclinical Research |
17.
Relationship Between Blood Levels and the Anti‐Hyperalgesic Effect of Ketoprofen in the Rat 下载免费PDF全文
José Carlos Aguilar‐Carrasco Juan Rodríguez‐Silverio Juan Miguel Jiménez‐Andrade Miriam del Carmen Carrasco‐Portugal Francisco Javier Flores‐Murrieta 《Drug development research》2014,75(3):189-194
Preclinical Research |
18.
《Drug development research》2017,78(8):403-410
Preclinical Research |
19.
Involvement of Nitric Oxide and ATP‐Sensitive Potassium Channels in the Peripheral Antinoceptive Action of a Tramadol–Dexketoprofen Combination in the Formalin Test 下载免费PDF全文
Mario A. Isiordia‐Espinoza Amaury Pozos‐Guillén José Pérez‐Urizar Daniel Chavarría‐Bolaños 《Drug development research》2014,75(7):449-454
Preclinical Research |
20.
This study investigated the anti-inflammatory effect of N, N′-bis(3-dimethylamino-1-phenyl-propylidene)hydrazine dihydrochloride, D1, on carrageenan-induced edema. In addition, its effect on hyaluronidase-induced vascular permeability was also tested. D1 was synthesized, and anti-inflammatory activity was determined by carrageenan-induced hind paw edema in rats (n?=?30) at 50, 100, and 200?mg kg?1 doses of D1 and also a 25?mg kg?1 dose of indomethacin. The effects of D1 and indomethacin on hyaluronidase-induced capillary permeability were investigated in rabbits (n?=?18) at a 100?mg kg?1 dose of D1 and 25?mg kg?1 dose of indomethacin. D1 inhibited carrageenan-induced inflammation by 40, 20, and 10% at 50, 100, and 200?mg kg?1 doses after 1?h. The inhibitions were 22.5, 32.7, 28.6% and 15.6, 33.4, 8.9% at 2?h and 3?h, respectively. The inhibitions due to indomethacin (25?mg kg?1 dose) were 67.5, 87.8, and 91.1%, at 1?h, 2?h, and 3?h, respectively. The subcutaneous spreading areas of Trypan blue at 1, 5, 30, and 60?min after subcutaneous injection of hyaluronidase were 172.6?±?41.6, 210.2?±?39.7, 363?±?50, and 400.2?±?46.7?mm2 in the D1 (100?mg kg?1) treated group. The spreading areas at these time periods were 38.8?±?3.7, 48.2?±?4.5, 100.6?±?6.9, and 119.8?±?22.5?mm2 in the indomethacin treated group. Our results showed that D1 inhibits carrageenan-induced inflammation in rats. A tendency to decrease the capillary permeability suggested that the mechanism of action of the anti-inflammatory effect of D1 may partly depend on inhibition of the hyaluronidase enzyme. 相似文献