scholarly journals Oceanapia magna Sponge Presents Dual Effect on the Gastrointestinal Motility of Rodents: In Vitro and In Vivo Assays

2020 ◽  
Vol 11 ◽  
Author(s):  
Joedna Cavalcante Pereira ◽  
Indyra Alencar Duarte Figueiredo ◽  
Filipe Rodolfo Moreira Borges de Oliveira ◽  
Sarah Rebeca Dantas Ferreira ◽  
Giulyane Targino Aires Moreno ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Guinea Pig ◽  
Gastrointestinal Motility ◽  
Gastrointestinal Transit ◽  
Ethanolic Extract ◽  
Guinea Pig Ileum ◽  
Dual Effect ◽  
Marine Products

Oceanapia magna Santos-Neto, Nascimento, Cavalcanti and Pinheiro sponges are distributed across tropical worldwide seas. Some studies of marine products have shown interesting activities in smooth muscle models. Hence, we assessed the effect of the ethanolic extract of Oceanapia magna. (OC-EtOH) on acute toxicity and gastrointestinal motility (in vitro and in vivo) in rodent models. On guinea pig ileum, OC-EtOH induced a concentration dependent contraction on basal tonus, which was not inhibited by atropine, but in the presence of pyrilamine or verapamil, the effect was antagonized. Contrastingly, on KCl- or histamine-induced contractions, OC-EtOH presented a transient contraction followed by a concentration-dependent relaxation. Moreover, OC-EtOH presented a relaxant profile on cumulative curves to CaCl2 and tonic contraction induced by S-(-)-BayK8644, through Cav blockade. The acute toxicity assay showed that OC-EtOH (2,000 mg/kg, p.o.) did not present any sign of toxicity in female mice. Additionally, OC-EtOH presented antidiarrheal effect in mice, increased the intestinal normal transit and reduced the castor oil-induced intestinal transit. Thus, OC-EtOH presented a dual effect on guinea pig ileum promoting contraction through activation of H1 and CaV, and relaxation through CaV blockade, besides the effect on upper gastrointestinal transit in mice, showing a potential medicinal use of this sponge in intestinal diseases such as diarrhea.

scholarly journals ACUTE TOXICITY STUDY OF THE LEAVES ETHANOLIC EXTRACT OF PICRIA FEL-TERRAE LOUR.

2018 ◽  
Vol 11 (13) ◽  
pp. 55
Author(s):  
Popi Patilaya ◽  
Dadang Irfan Husori ◽  
Imam Bagus Sumantri ◽  
Simon Sihombing
Keyword(s):  
Acute Toxicity ◽  
Plant Extract ◽  
Aspartate Aminotransferase ◽  
Alanine Aminotransferase ◽  
Ethanolic Extract ◽  
Male Mice ◽  
Plant Leaves ◽  
Liver And Kidney

 Objective: Picria fel-terrae belongs to family Linderniaceae is also known as Pugun tano by Indonesian people. The ethanolic extract of plant leaves has several potential pharmacological activities including antidiabetic, anthelmintic, and antioxidant. However, the toxicity of the plant extract is rarely explored. This work was to investigate toxicity of the leaf ethanolic extract of P. fel-terrae on Artemia salina and male mice.Methods: Acute toxicity of the plant extract was studied by in vitro and in vivo methods. In vitro study was carried out by exposing nauplii to the plant extract at concentrations of 10, 100, 200, 500, and 1000 μg/ml for 48 h. In vivo study was performed on male mice that divided into four groups. Groups I, II, III, and IV were treated with sodium carboxymethyl cellulose 0.5%, the ethanolic extract of plant leaves at doses of 1000, 2000, and 5000 mg/kg bw, respectively. The animal toxic symptoms were observed every day for 14 days. On day 15, the blood of mice was collected to measure alanine aminotransferase, aspartate aminotransferase, and creatinine levels. The effects of plant extract on vital animal organs such as heart, liver, and kidney were also studied. Statistical analysis of data was performed using analysis of variance and followed by Tukey post hoc.Results: The results showed that the leaf ethanolic extract of P. fel-terrae to have weakly toxicity on A. salina with the LC50 of 768.07 μg/ml. At in vivo studies, the toxic symptoms of mice were not identified during experiment with all doses of the plant extract for 14 days. In addition, aspartate aminotransferase and creatinine levels were no significantly different between control and all treatment groups (p>0.05). However, alanine aminotransferase level changed when mice were exposed by the plant extract at the doses of 2.000 and 5.000 mg/kg bw. Although the mice were not dead during experiment, the animal organs such as heart, liver, and kidney were histologically changed.Conclusion: This study suggests that the ethanolic extract of P. fel-terrae leaves has weakly toxicity on A. salina and causes histological changes on male mice organs at the high doses.

scholarly journals Phytopharmacological Evaluation of Alcoholic Extract of Berberis aristata Leaf in the Treatment of Gastric Ulcer

2020 ◽  
Vol 13 (1) ◽  
pp. 1-5
Author(s):  
Ratnaker Singh ◽  
Y. Trilochana
Keyword(s):  
Acute Toxicity ◽  
Crude Extract ◽  
Antioxidant Activities ◽  
Ethanolic Extract ◽  
Total Phenolic ◽  
Antiulcer Activity ◽  
Alcoholic Extract ◽  
Dose Dependent

For over a century, peptic ulcer has been one of the most common gastrointestinal tract (GIT) disorder. There are number of drugs are now available for treatment. Drugs of herbal origin reduce the offensive factors and have proved to be safe, clinically effective, relatively less expensive, globally competitive, and with better patient tolerance.This study was performed to assess the anti-ulcer activity on different parts of B.aristata. Apart from that, acute toxicity, qualitative chemical analysis, total phenolic content (TPC), total flavonoid content(TFC) and in vitro antioxidant activities were evaluated. The potentially active plant part was selected for screening as gastro protective, in vivo antioxidant and antisecretory activities in ulcerated rats.The 50% ethanolic extract of B. aristata were subjected to preliminary phytochemical screening, estimation of TFC and TPC. The crude extract from the leaves of B. aristata gave best antiulcer activity among flower and stem. In acute toxicity studies, the administration of the crude extract of B. aristata leaves did not reveal any adverse effects or toxicity in rats at fourteen days observations.The results of these studies have shown that ethylexract of B.aristata leaf (EEBAL) produced a significant dose dependent ulcerprotective, antioxidant and antisecretory activity by blocking the activity of proton pump, protecting from antioxidants produced during stress induced ulcer and by enhancing glycoprotein levels.

scholarly journals Exploration of Anti-Diabetic, Anti-Diarrheal, Gastrointestinal Motility and Acute Toxicity of Different Extracts of Citrus Assamensis Leaf

2018 ◽  
Vol 42 (2) ◽  
pp. 111-120
Author(s):  
Mohammad Shahriar ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Sohel Rana
Keyword(s):  
Acute Toxicity ◽  
Gastrointestinal Motility ◽  
Treated Group ◽  
Chloroform Extract ◽  
Leaf Extracts ◽  
Ethanol Extracts ◽  
Academy Of Sciences ◽  
Vehicle Treated Group

Citrus assamensis (Family: Rutaceae), commonly known as Satkara, is a pharmacologically diverse medicinal plant. In the present study, the leaf extracts of C. assamensis were subjected to evaluate in vitro anti-diabetic as well as in vivo anti-diarrheal, gastrointestinal motility and acute toxicity activity on Swiss albino mice by using standard protocol. Ethanol and chloroform extracts showed significant inhibitory potentials (**p<0.01) against in vitro α-amylase enzyme at the concentration of 80μg/mL. Significant (*p<0.05, **p<0.01, ***p<0.001) reduction in the number of wet feces and percentage inhibition of diarrheal activity over three hours was observed with all the test doses of the extract compared with the vehicle treated group. Both doses of methanol and ethanol extracts (*p<0.05) and chloroform extract at doses of 100 mg/kg significantly reduced the number of wet feces compared to the control. None of the extracts showed any significant in vivo acute toxicity effect on mice. Journal of Bangladesh Academy of Sciences, Vol. 42, No. 2, 111-120, 2018

Sila-Pharmaka, 24. Mitt. [1]. Sila-Analoga von Nifedipin-ähnlichen 4-Aryl-2.6-dimethyl-1.4-dihydropyridin- 3.5-dicarbonsäure-dialkylestern, II. / Sila-Drugs, 24th Communication [1]. Sila-Analogues of Nifedipine-Like Dialkyl 4-Aryl-2,6-dimethyl-1,4-dihydropyridine- 3,5-dicarboxylates, II.

1982 ◽  
Vol 37 (4) ◽  
pp. 443-450 ◽  
Author(s):  
R. Tacke ◽  
A. Bentlage ◽  
W. S. Sheldrick ◽  
L. Ernst ◽  
R. Towart ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Antihypertensive Effect ◽  
Substitution Effects ◽  
X Ray Diffraction ◽  
Guinea Pig Ileum ◽  
X Ray ◽  
Renal Hypertensive Rat ◽  
Dihydropyridine Derivatives

In the course of systematic studies on sila-substituted drugs the nifedipine-like 1.4-dihydropyridine derivatives 4a, 4b and 4c were prepared and investigated with respect to sila-substitution effects. By X-ray diffraction analyses 4a, 4b and 4c were found to be isostructural. The C/Si-analogues exhibit similar spasmolytic activities (in vitro, guinea pig ileum), comparable with that of nifedipine. However, the compounds differ substantially in their in vivo activity, as measured by the antihypertensive effect on the renal-hypertensive rat. The experimental results are discussed with respect to the carbon/silicon exchange.

Bioactive peptide derived from in vitro proteolysis of bovine β-lactoglobulin and its effect on smooth muscle

1997 ◽  
Vol 64 (1) ◽  
pp. 149-155 ◽  
Author(s):  
ANNE PIHLANTO-LEPPÄLÄ ◽  
ILARI PAAKKARI ◽  
MERJA RINTA-KOSKI ◽  
PIRKKO ANTILA
Keyword(s):  
Guinea Pig ◽  
Proteolytic Enzymes ◽  
Whey Proteins ◽  
Casein Hydrolysate ◽  
Milk Proteins ◽  
Biologically Active ◽  
Guinea Pig Ileum ◽  
Β Lactoglobulin

Milk proteins have largely been considered as providing essential amino acids, but oligopeptides derived from milk proteins have been shown to possess biological functions. In vitro, opioid activity was first reported in bovine β-casein hydrolysate by Brantl et al. (1979). Precursors of biologically active peptides have been demonstrated in vivo after digestion of milk (Scanff et al. 1992). Peptides that inhibit platelet aggregation (Fiat et al. 1989), stimulate the immune system (Migliore-Samour et al. 1989), inhibit angiotensin I converting enzyme (Maruyama & Suzuki, 1982) and are involved in intestinal Ca solubilization and absorption (Sato et al. 1986) have also been isolated from bovine casein hydrolysates.Bioactive peptides from whey proteins and their physiological effects have received less attention than those from casein. Peptides with opiate-like activity include the lactorphins, residues 50–53 in bovine and human α-lactalbumin and 102–105 in bovine β-lactoglobulin (β-lg) (Chiba & Yoshikawa, 1986; Yoshikawa et al. 1986; Antila et al. 1991). Yamauchi (1992) has reported that a peptide derived from β-lg induced contraction of guinea pig ileum longitudinal muscle in the absence of electric stimulation and agonist. The fragment, containing residues 146–149 of β-lg (His–Ile–Arg–Leu), was called β-lactotensin.The purpose of this study was to determine whether β-lactotensin was released from bovine β-lg by in vitro proteolysis using different proteolytic enzymes. The pharmacological activity of this tetrapeptide was characterized in guinea pig ileum in vitro using a synthetic fragment.

scholarly journals Antidiarrhoeal potentials of methanol bark extract of Hymenocardia Acida Tul (Euphorbiaceae) in laboratory animals

2021 ◽  
Vol 45 (1) ◽  
Author(s):  
Abba Musab Usman ◽  
Nuhu Muhammad Danjuma ◽  
Jamilu Ya’u ◽  
Muslim Muhammad Ahmad ◽  
Zakariyya Alhassan ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Lethal Dose ◽  
Stem Bark ◽  
Laboratory Animals ◽  
Bark Extract ◽  
Intestinal Fluid ◽  
Guinea Pig Ileum ◽  
Rabbit Jejunum

Abstract Background The plant Hymenocardia acida (Euphorbiaceae) is utilized as herbal preparation against diarrhoea, dysentery and other diseases. We aimed to determine the antidiarrhoeal potentials of Hymenocardia acida (MEHA) stem bark in vivo and in vitro. Preliminary phytochemical contents, as well as the acute toxicity effect of the extract, were investigated based on standard experimental methods. The antidiarrhoeal properties of the MEHA at 150, 300 and 600 mg/kg were studied against diarrhoea induced by castor oil, intestinal fluid accumulation, as well as intestinal movement tests using distilled water (10 ml/kg) and loperamide/atropine sulphate as the control groups. Besides, the in vitro effects of the extract (8 × 10−2–640 × 10−2 mg/ml) on the rabbit jejunum and guinea-pig ileum were evaluated. Results Phytochemical screening showed alkaloids, glycoside, saponins, tannins, triterpenes, flavonoids and steroids in the MEHA. The median lethal dose (LD50) of the MEHA after oral administration was approximately greater than 2000 mg/kg. The MEHA declined the diarrhoea onset and remarkably decreased the number of watery stools in the group that received 300 and 600 mg/kg. It also elicited a remarkable and non-dose-dependent reduction in the intestinal fluid volume. At 1000 mg/kg, the MEHA significantly inhibited the charcoal movement. In addition, the MEHA (8 × 10−2–640 × 10−2 mg/ml) elicited a remarkable decrease in the contractility of the rabbit jejunum over time and relaxed the guinea pig ileum. Besides, it showed concentration-dependent attenuation of the acetylcholine and histamine-induced contraction. Conclusion The extract under investigation revealed promising antidiarrhoeal properties that justified its traditional claim for use against diarrhoea.

Inhibition of Human and Animal Platelet Adhesiveness to Glass Bead Columns by Adenosine, Dipyridamole, Chlorpromazine and Acetylsalicylic Acid

1976 ◽  
Vol 36 (02) ◽  
pp. 401-410 ◽  
Author(s):  
Buichi Fujttani ◽  
Toshimichi Tsuboi ◽  
Kazuko Takeno ◽  
Kouichi Yoshida ◽  
Masanao Shimizu
Keyword(s):  
Guinea Pig ◽  
Acetylsalicylic Acid ◽  
Guinea Pigs ◽  
Glass Bead ◽  
Animal Species ◽  
Inhibitory Effect ◽  
Rabbit Platelet ◽  
Platelet Adhesiveness

SummaryThe differences among human, rabbit and guinea-pig platelet adhesiveness as for inhibitions by adenosine, dipyridamole, chlorpromazine and acetylsalicylic acid are described, and the influence of measurement conditions on platelet adhesiveness is also reported. Platelet adhesiveness of human and animal species decreased with an increase of heparin concentrations and an increase of flow rate of blood passing through a glass bead column. Human and rabbit platelet adhesiveness was inhibited in vitro by adenosine, dipyridamole and chlorpromazine, but not by acetylsalicylic acid. On the other hand, guinea-pig platelet adhesiveness was inhibited by the four drugs including acetylsalicylic acid. In in vivo study, adenosine, dipyridamole and chlorpromazine inhibited platelet adhesiveness in rabbits and guinea-pigs. Acetylsalicylic acid showed the inhibitory effect in guinea-pigs, but not in rabbits.

Evaluation of the In Vivo Acute Toxicity and In Vitro Hemolytic and Immunomodulatory Activities of the Moringa oleifera Flower Trypsin Inhibitor (MoFTI)

2020 ◽  
Vol 27 ◽  
Author(s):  
Leydianne Leite de Siqueira Patriota ◽  
Dayane Kelly Dias do Nascimento Santos ◽  
Bárbara Rafaela da Silva Barros ◽  
Lethícia Maria de Souza Aguiar ◽  
Yasmym Araújo Silva ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Trypsin Inhibitor ◽  
Hemolytic Activity ◽  
Moringa Oleifera ◽  
Biological Activities ◽  
Hematological Parameters ◽  
Behavioral Alterations ◽  
Female Mice

Background: Protease inhibitors have been isolated from plants and present several biological activities, including immunomod-ulatory action. Objective: This work aimed to evaluate a Moringa oleifera flower trypsin inhibitor (MoFTI) for acute toxicity in mice, hemolytic activity on mice erythrocytes and immunomodulatory effects on mice splenocytes. Methods: The acute toxicity was evaluated using Swiss female mice that received a single dose of the vehicle control or MoFTI (300 mg/kg, i.p.). Behavioral alterations were observed 15–240 min after administration, and survival, weight gain, and water and food consumption were analyzed daily. Organ weights and hematological parameters were analyzed after 14 days. Hemolytic activity of MoFTI was tested using Swiss female mice erythrocytes. Splenocytes obtained from BALB/c mice were cultured in the absence or presence of MoFTI for the evaluation of cell viability and proliferation. Mitochondrial membrane potential (ΔΨm) and reactive oxygen species (ROS) levels were also determined. Furthermore, the culture supernatants were analyzed for the presence of cytokines and nitric oxide (NO). Results: MoFTI did not cause death or any adverse effects on the mice except for abdominal contortions at 15–30 min after administration. MoFTI did not exhibit a significant hemolytic effect. In addition, MoFTI did not induce apoptosis or necrosis in splenocytes and had no effect on cell proliferation. Increases in cytosolic and mitochondrial ROS release, as well as ΔΨm reduction, were observed in MoFTI-treated cells. MoFTI was observed to induce TNF-α, IFN-γ, IL-6, IL-10, and NO release. Conclusion: These results contribute to the ongoing evaluation of the antitumor potential of MoFTI and its effects on other immunological targets.

Chemosensitizing Activity of Histone Deacetylases Inhibitory Cyclic Hydroxamic Acids for Combination Chemotherapy of Lymphatic Leukemia

2018 ◽  
Vol 18 (4) ◽  
pp. 365-371 ◽  
Author(s):  
Denis V. Mishchenko ◽  
Margarita E. Neganova ◽  
Elena N. Klimanova ◽  
Tatyana E. Sashenkova ◽  
Sergey G. Klochkov ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Acute Toxicity ◽  
Histone Deacetylases ◽  
Hydroxamic Acids ◽  
Water Soluble ◽  
Male Rat ◽  
Hybrid Male ◽  
Cyclic Hydroxamic Acids

Background: Anti-tumor effect of hydroxamic acid derivatives is largely connected with its properties as efficient inhibitors of histone deacetylases, and other metalloenzymes involved in carcinogenesis. Objective: The work was aimed to (i) determine the anti-tumor and chemosensitizing activity of the novel racemic spirocyclic hydroxamic acids using experimental drug sensitive leukemia P388 of mice, and (ii) determine the structure-activity relationships as metal chelating and HDAC inhibitory agents. Method: Outbreed male rat of 200-220 g weights were used in biochemical experiments. In vivo experiments were performed using the BDF1 hybrid male mice of 22-24 g weight. Lipid peroxidation, Fe (II) -chelating activity, HDAC fluorescent activity, anti-tumor and anti-metastatic activity, acute toxicity techniques were used in this study. Results: Chemosensitizing properties of water soluble cyclic hydroxamic acids (CHA) are evaluated using in vitro activities and in vivo methods and found significant results. These compounds possess iron (II) chelating properties, and slightly inhibit lipid peroxidation. CHA prepared from triacetonamine (1a-e) are more effective Fe (II) ions cheaters, as compared to CHA prepared from 1- methylpiperidone (2a-e). The histone deacetylase (HDAC) inhibitory activity, lipophilicity and acute toxicity were influenced by the length amino acids (size) (Glycine < Alanine < Valine < Leucine < Phenylalanine). All compounds bearing spiro-N-methylpiperidine ring (2a-e) are non-toxic up to 1250 mg/kg dose, while compounds bearing spiro-tetramethylpiperidine ring (1a-e) exhibit moderate toxicity which increases with increasing lipophility, but not excite at 400 mg/kg. Conclusion: It was shown that the use of combination of non-toxic doses of cisplatin (cPt) or cyclophosphamide with CHA in most cases result in the appearance of a considerable anti-tumor effect of cytostatics. The highest chemosensitizing activity with respect to leukemia Р388 is demonstrated by the CHA derivatives of Valine 1c or 2c.

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