scholarly journals Study of the Inhibitory Effects of Enteral Nutrition Formula on Indomethacin-Induced Gastric Lesions in Mice

Nutrients ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 3058
Author(s):  
Takeshi Yoshimi ◽  
Yoshiaki Yamagishi ◽  
Issei Kanegawa ◽  
Megumi Suda ◽  
Rei Saiki ◽  
...  
Keyword(s):  
Enteral Nutrition ◽  
Treated Group ◽  
Gastric Ulcers ◽  
Gastric Lesions ◽  
Inhibitory Effects ◽  
Significant Difference ◽  
Time Courses ◽  
Dose Dependent Decrease ◽  
Dose Dependent ◽  
Comparable Time

We investigated the effects of enteral nutrition formula on non-steroidal anti-inflammatory drug (NSAID)-induced gastric lesions in mice. Male ICR mice aged 7–9 weeks old were fasted, then orally given either purified water, Mermed® One, or 2-fold diluted Terumeal® 2.0α as enteral nutrition (25 or 50 mL/kg each). Indomethacin (IND) was orally administered at 20 mg/kg after 30 min, and the stomach was removed 6 h later and fixed in formalin. The number and area of lesions in the stomachs of the mice given enteral nutrition showed a significant, dose-dependent decrease compared to the purified water-treated group, and no significant difference was seen between the two enteral nutrition-treated groups. Comparable time courses of plasma IND concentrations suggest that enteral nutrition does not inhibit gastrointestinal absorption of IND. Our findings indicate that administering enteral nutrition could inhibit the onset of NSAID-induced gastric ulcers.

scholarly journals Effect of Bee Venom Pharmacopuncture on Inflammation in Mouse Model of Induced Atopic Dermatitis

2020 ◽  
Vol 37 (2) ◽  
pp. 123-127
Author(s):  
Kyeong Ju Park ◽  
Ho-Sueb Song
Keyword(s):  
Atopic Dermatitis ◽  
Mouse Model ◽  
Treated Group ◽  
Bee Venom ◽  
Related Protein ◽  
Griess Reaction ◽  
Cox 2 ◽  
Dose Dependent Decrease ◽  
Dose Dependent ◽  
Inflammatory Effect

Background: This study was designed using a mouse model of atopic dermatitis [phthalic anhydride (PA)-treated mice], to investigate the anti-inflammatory effect of bee venom pharmacopuncture (BVP) in keratinocytes.Methods: Western blot analysis was performed to investigate inflammation related protein expression of iNOS, COX-2, phospho-ERK (p-ERK), and ERK, in LPS (1 μg/mL)-activated keratinocytes, following BVP treatment, and in PA-treated mice, after BVP treatment. Griess reaction was performed to investigate NO concentration. Enzyme-linked immunosorbent assays were used to determine the concentrations of interleukin (IL)-4+, IL-17A+, IL-13 and IL-4 in PA-treated mice after BVP treatment. In addition, monocyte, macrophage, neutrophil, and eosinophil counts were measured to observe the changes in white blood cell infiltration.Results: The keratinocytes of the BVP-treated group showed a decreased expression of iNOS, COX-2, ERK at 5 OX-2, ERK E, and p-ERK at 1, 2 and 5 RKRK ERK ERK, and a dose-dependent decrease in NO concentration at 2 and 5 ntrationof s. In the BVP-treated groups (0.1 μ.1-trea μ.1-treated gr), PA-treated mice showed recovery after 4 weeks which was dose-dependent, showing a significant decrease in clinical scores for AD, and a decreased concentration of IL-13 and IL-4 with BV treatment. There was a dose-dependent decrease in the infiltration of eosinophils, neutrophils, monocytes, macrophages, and a decreased thickness of the epidermis due to inflammation, and decreased expressions of iNOS, COX-2, p-ERK, ERK, especially in the 0.1 μ0/mL BVP-treated group,<br>Conclusion: These results suggest that BVP may be an effective alternative treatment for atopic dermatitis.

scholarly journals Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Xin Tian ◽  
Zhen-Yu Cheng ◽  
Han Jin ◽  
Jie Gao ◽  
Hai-Ling Qiao
Keyword(s):  
Liver Microsomes ◽  
Flavonoid Compound ◽  
Rat Liver Microsomes ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Concentration Dependent Manner ◽  
Dose Dependent Decrease ◽  
Induced Changes ◽  
Regulatory Properties ◽  
Dose Dependent

Baicalin, a flavonoid compound isolated fromScutellaria baicalensis, has been shown to possess antiinflammatory, antiviral, antitumour, and immune regulatory properties. The present study evaluated the potential herb-drug interaction between baicalin and midazolam in rats. Coadministration of a single dose of baicalin (0.225, 0.45, and 0.90 g/kg, i.v.) with midazolam (10 mg/kg, i.v.) in rats resulted in a dose-dependent decrease in clearance (CL) from 25%  (P<0.05)to 34%  (P<0.001)with an increase inAUC0−∞from 47%  (P<0.05)to 53%  (P<0.01). Pretreatment of baicalin (0.90 g/kg, i.v., once daily for 7 days) also reduced midazolam CL by 43%  (P<0.001), with an increase inAUC0−∞by 87%  (P<0.01). Multiple doses of baicalin decreased the expression of hepatic CYP3A2 by approximately 58%  (P<0.01)and reduced midazolam 1′-hydroxylation by 23%  (P<0.001)and 4′-hydroxylation by 21%  (P<0.01)in the liver. In addition, baicalin competitively inhibited midazolam metabolism in rat liver microsomes in a concentration-dependent manner. Our data demonstrated that baicalin induced changes in the pharmacokinetics of midazolam in rats, which might be due to its inhibition of the hydroxylation activity and expression of CYP3A in the liver.

scholarly journals Gastroprotective Effect of Enteral Nutrition Formula in Mice Injected Subcutaneously with Indomethacin

Nutrients ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 3297
Author(s):  
Yoshiaki Yamagishi ◽  
Rei Saiki ◽  
Takeshi Yoshimi ◽  
Toshiyuki Kudo ◽  
Kiyomi Ito
Keyword(s):  
Gastrointestinal Tract ◽  
Enteral Nutrition ◽  
Oral Administration ◽  
Protective Effect ◽  
Direct Interaction ◽  
Gastric Lesions ◽  
Icr Mice ◽  
Gastroprotective Effect ◽  
Time Courses

We have previously shown that two enteral nutrition formulas suppressed gastric lesions induced by the oral administration of indomethacin (IND) in mice. However, the mechanism of their protective effect is unknown. In this study, the effect of the two enteral nutrition formulas on gastric lesions induced by subcutaneous IND injection was investigated, with the objective of exploring the possibility that they may interact directly with IND in the gastrointestinal tract. Ten-week-old, male, ICR mice were fasted, then orally given either purified water, Mermed® One, or 2-fold diluted Terumeal® 2.0α as enteral nutrition formula (25 mL/kg). IND was injected subcutaneously at 20 mg/kg after 30 min, and the stomach was removed 6 h later and fixed in formalin. The number and area of lesions in the stomachs of mice given enteral nutrition formula was reduced to 56–89% and 34–61%, respectively, compared with the mice given purified water. The time courses of plasma IND concentrations were comparable among the three groups. These results suggested that the effect of these enteral nutrition formulas on gastric lesions did not originate from their direct interaction with IND in the gastrointestinal tract or their effect on the disposition of IND.

scholarly journals ANTIPLASMODIAL ACTIVITY OF CAESALPINIA CRISTA SEED EXTRACTS

2018 ◽  
Vol 8 (5) ◽  
pp. 354-357
Author(s):  
M. Swapna Reddy ◽  
B. Ramya Kuber
Keyword(s):  
Wistar Rats ◽  
Treated Group ◽  
Antiplasmodial Activity ◽  
Toxicity Tests ◽  
Alcoholic Extract ◽  
Antimalarial Agents ◽  
Dose Dependent Decrease ◽  
Dose Dependent ◽  
Oral Acute Toxicity ◽  
Seed Extracts

Objective: To evaluate antiplasmodial activity of Caesalpinia crista seed extracts Methods:  Antiplasmodial activity of the seed extracts of Caesalpinia crista against rodent malaria infections in chloroquine sensitive Plasmodium falcipuram strain was investigated, and oral acute toxicity of seed extracts of Caesalpinia crista was also evaluated. Results: The findings of this study revealed significant (P < 0.05) and dose dependent decrease in parasitaemia in the parasitized groups treated with varying doses of the extract (50-200 mg/kg p.o.) in both suppressive and curative tests. There was also significant decrease in parasitaemia density in the chloroquine treated group. The alcoholic extract was found no toxicity in wistar rats and the oral LD50 was determined to be greater than 5000 mg/kg. Conclusion: Seed extracts of Caesalpinia crista extract possesses potent antiplasmodial activity and may therefore, serve as potential sources of new antimalarial agents Keywords: Plasmodium falcipuram, Caesalpinia crista, Plant extracts, Phytochemicals, Toxicity tests, malaria.

scholarly journals Effect of Caulerpa Cylindracea Extract on Histopathology Depiction of Male Rattus Norvegicus Gaster Mucosa Induced by Indomethacin

2021 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
FITRI HANDAJANI ◽  
Adya Hidayatullah ◽  
Nita Pranitasari
Keyword(s):  
Rattus Norvegicus ◽  
Mucosal Damage ◽  
Gastric Mucosal Damage ◽  
Male Rats ◽  
Gastric Ulcers ◽  
Gastric Lesions ◽  
Flavonoid Content ◽  
Experimental Animals ◽  
Significant Difference ◽  
Group 2

ABSTRACT Background: A lot of food can repair gastric mucosal damage. For example, sea grapes or the Caulerpa cylindracea with its flavonoid content. Anti-inflammatory and anti-ulcer effect can reduce gastric lesions due to ulcerogenic agents. Indomethacin is used to induce gastric ulcers in experimental animals. Based on this background, this study was conducted to analyze the effect of Caulerpa cylindracea extract, on the histopathological picture of gastric mucosal damage of Rattus norvegicus male rats.   Method: 32 male Rattus norvegicus rats were divided into 4 groups, (1) Group K(-), the untreated group, (2) Group K(+) induced by indomethacin 30mg/kgBB per head (3) Group P1 induced by indomethacin 30 mg/kgBB and Caulerpa cylindracea extract 1gr/100grBB per head, (4) Group P2, induced by indometacin 30mg/kgBB and 2gr/100grBB of Caulerpa cylindracea extract per head.   Result: There was a significant difference (p = 0.001) between the degree of gastric mucosal damage in group K(+) given only indomethacin and group P1 given Indomethacin and 1gr/100grBB Caulerpa cylindracea extract. There was a significant difference (p = 0.001) between group K(+) and group P2 that given Indomethacin and 2g/100grBB Caulerpa cylindracea extract. There was a significant difference (p = 0.004) between group P1 and group P2. Data revealed on group K(-) without any treatment did not obtain significant results (p = 0.060) with group P2.    Conclusion: Giving Caulerpa cylindracea extract with 1 gr/100grBB dose and 2gr/100grBB dose can repair mucosal damage in Rattus norvegicus male rats induced by indomethacin.   

Investigation of antiulcer activity of Pergularia extensa Linn

2020 ◽  
Vol 9 (2) ◽  
pp. 23-26
Author(s):  
Pavani C H
Keyword(s):  
Cardiac Glycosides ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Antiulcer Activity ◽  
Acute Oral Toxicity ◽  
Gastric Lesions ◽  
Oral Toxicity ◽  
Control Groups ◽  
Dose Dependent

This study was based on determination of the antiulcer activity from methanol extract was prepared by using barks of pergularia extensa linn.. Priliminary investigations showed presence of saponins, terpenes, cardiac glycosides, alkaloids and sterols. Based on OECD-423 Guidelines, the pharmacology and acute oral toxicity studies were conducted by using methanolic extract. Ulcer development was prevented by Tannins because of their vasoconstriction effects and due to protein precipitation. Similarly, the Methanolic extract of Pergularia extensa Linn shows triterpenoids and saponins. The phytoconstituents are present in the extract and these could be possible agents which are involved in order to prevent gastric lesions induced by aspirin. When compared to ulcerative control groups, this Pergularia extensa Linn., shows a dose dependent curative ratio. The extracts exhibited an inhibition percentage of 27.18, 45.47 and 61.28 at doses of 100, 200 and 400mg/kg doses respectively. 

The JPJDF has Synergistic Effect with Fluoropyrimidine in the Maintenance Therapy for Metastatic Colorectal Cancer

2020 ◽  
Vol 15 (3) ◽  
pp. 257-269
Author(s):  
Xiaoling Fu ◽  
Yanbo Zhang ◽  
Lisheng Chang ◽  
Dengcheng Hui ◽  
Ru Jia ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Synergistic Effect ◽  
Maintenance Therapy ◽  
Metastatic Colorectal Cancer ◽  
Maintenance Treatment ◽  
Advanced Colorectal Cancer ◽  
Treated Group ◽  
Induction Treatment ◽  
Chemotherapeutic Regimen ◽  
Significant Difference

Background: Maintenance chemotherapeutic regimen with low toxicity is needed for metastatic colorectal cancer. A recent patent has been issued on the spleen-strengthening and detoxification prescription (JPJDF), a traditional Chinese herbal medicinal formula with anti-angiogenesis effect. The clinical effect of JPJDF on the maintenance treatment of advanced colorectal cancer has not been evaluated. Objective: This study aims to evaluate the effectiveness and safety of JPJDF in combination with fluoropyrimidine compared to fluoropyrimidine alone as maintenance therapy for metastatic colorectal cancer. Methods: We applied a prospective, randomized, double-blinded, single center clinical study design. A total of 137 patients with advanced colorectal cancer were recruited. Patients received either Fluoropyrimidine (Flu-treated group, n = 68), or Fluoropyrimidine plus JPJDF (Flu-F-treated group, n = 69) as maintenance treatment after 6-cycle of FOLFOX4 or FOLFORI induction treatment. The primary endpoints were Progression-Free Survival (PFS) and Overall Survival (OS). The secondary endpoints were safety, Performance Status (PS) score and other symptoms. Results: The endpoint of disease progression was observed in 91.7% of patients. The PFS was 5.0 months and 3.0 months in the Flu-F-treated and Flu-treated groups, respectively. The OS was 15.0 months and 9.0 months in the Flu-F-treated and Flu-treated groups, respectively. Some common symptoms, such as hypodynamia, anepithymia, dizziness and tinnitus and shortness of breath, were improved in the Flu-F-treated group. There was no significant difference in the common adverse reactions between the two groups. Conclusion: JPJDF and fluoropyrimidine have synergistic effect in the maintenance treatment of mCRC.

Interaction between amrinone and parathyroid hormone on bone in culture

1982 ◽  
Vol 243 (6) ◽  
pp. E499-E504
Author(s):  
N. S. Krieger ◽  
P. H. Stern
Keyword(s):  
Parathyroid Hormone ◽  
Bone Resorption ◽  
Direct Interaction ◽  
Inhibitory Effects ◽  
Dihydroxyvitamin D3 ◽  
Basal Bone ◽  
Cardiotonic Agent ◽  
Neonatal Mouse Calvaria ◽  
Dose Dependent ◽  
Stimulation Of

The cardiotonic agent amrinone has been postulated to directly affect Na-Ca exchange. Because stimulated bone resorption has been proposed to require Na-Ca exchange, we examined the effects of amrinone on bone. Amrinone inhibited release of Ca from neonatal mouse calvaria in organ culture stimulated by parathyroid hormone (PTH), 1,25-dihydroxyvitamin d3, or prostaglandin E2. Inhibition was dose dependent and maximal at 2 X 10(-4) M. The effect of amrinone differed from the inhibitory effects of calcitonin, ouabain, or nigericin in that 1) 6-h exposure to amrinone alone prevented the effect of subsequently added PTH; 2) amrinone was only partially effective if added after resorption was initiated by 24-h treatment with PTH; 3) coincubation with amrinone and PTH during the first 48 h of culture allowed for a response to PTH after amrinone was removed; no such protection by a stimulator occurred with ouabain or nigericin. Also submaximal concentrations of amrinone plus calcitonin, ouabain, or nigericin gave greater than additive inhibition of Ca release. Amrinone had no effect on basal bone cAMP or on the acute stimulation of cAMP by PTH. The results suggest that amrinone could have a more direct interaction with the pathway involved in stimulated bone resorption than the other inhibitors.

Insulin secretion and substrate homeostasis in prolonged hypothermia in rats

1988 ◽  
Vol 255 (6) ◽  
pp. R1035-R1040
Author(s):  
R. Hoo-Paris ◽  
M. L. Jourdan ◽  
L. C. Wang ◽  
R. Rajotte
Keyword(s):  
Insulin Secretion ◽  
Plasma Glucose ◽  
Low Temperatures ◽  
Plasma Insulin ◽  
Glucose Utilization ◽  
Exogenous Insulin ◽  
Metabolic Substrate ◽  
Endogenous Insulin ◽  
Dose Dependent Decrease ◽  
Dose Dependent

In hypothermia, impairment of metabolic substrate mobilization and utilization may be a factor limiting survival. By use of a newly developed technique, substrate profiles and their regulation by insulin were examined in hypothermic rats (body temperature 19 degrees C) over 24 h. Plasma glucose concentrations increased to approximately 300 mg/dl during cooling and remained high throughout the period of hypothermia. Free fatty acid (FFA) concentration was not altered during cooling or during the first 10 h of hypothermia (approximately 700 mu eq/l) but progressively decreased thereafter, reaching 420 mu eq/l by 20 h. Plasma insulin decreased dramatically during cooling and remained very low (9 +/- 2 microU/ml) during the whole period of hypothermia, reflecting the suppression of insulin secretion by isolated islets at low temperatures. To test he hypothesis that suppression of endogenous insulin secretion may hamper glucose utilization and thus limit survival in hypothermia, exogenous insulin was administered. At doses of 0.1, 0.5, and 1 U/kg intravenously, insulin slowly decreased plasma glucose and FFA. However, at 0.1 and 1 U/kg intraperitoneally, insulin resulted in a dose-dependent decrease in survival time in the hypothermic rat. It is possible that the antilipolytic effect of insulin may have outweighed any beneficial effect of improving glucose utilization in hypothermia.

scholarly journals A Reversible Shift of Driver Dependence from EGFR to Notch1 in Non-Small Cell Lung Cancer as a Cause of Resistance to Tyrosine Kinase Inhibitors

Cancers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 2022
Author(s):  
Francesca Iommelli ◽  
Viviana De Rosa ◽  
Cristina Terlizzi ◽  
Rosa Fonti ◽  
Rosa Camerlingo ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Epithelial Mesenchymal Transition ◽  
Parental Cell ◽  
Egfr Inhibitors ◽  
Simultaneous Increase ◽  
Adherent Cells ◽  
Binding Assays ◽  
Mesenchymal Transition ◽  
Dose Dependent Decrease ◽  
Dose Dependent

Notch1 plays a key role in epithelial-mesenchymal transition (EMT) and in the maintenance of cancer stem cells. In the present study we tested whether high levels of activated Notch1 in oncogene-driven NSCLC can induce a reversible shift of driver dependence from EGFR to Notch1, and thus causing resistance to EGFR inhibitors. Adherent cells (parental) and tumor spheres (TS) from NSCLC H1975 cells and patient-derived CD133-positive cells were tested for EGFR and Notch1 signaling cascade. The Notch1-dependent modulation of EGFR, NCID, Hes1, p53, and Sp1 were then analyzed in parental cells by binding assays with a Notch1 agonist, DLL4. TS were more resistant than parental cells to EGFR inhibitors. A strong upregulation of Notch1 and a concomitant downregulation of EGFR were observed in TS compared to parental cells. Parental cell exposure to DLL4 showed a dose-dependent decrease of EGFR and a simultaneous increase of NCID, Hes1, p53, and Sp1, along with the dislocation of Sp1 from the EGFR promoter. Furthermore, an enhanced interaction between p53 and Sp1 was observed in TS. In NSCLC cells, high levels of active Notch1 can promote a reversible shift of driver dependence from EGFR to Notch1, leading to resistance to EGFR inhibitors.

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