scholarly journals In vivo Studies of the Effect of a Herbal Preparation on Pharmacokinetic Properties of Rifampicin in Male Swiss Albino Rats and Computer Mediated Mechanism of Interaction

2018 ◽  
Vol 3 (4) ◽  
Author(s):  
Kolawole Jacob
Keyword(s):  
In Vivo Studies ◽  
Albino Rats ◽  
Herbal Preparation ◽  
Computer Mediated ◽  
Pharmacokinetic Properties ◽  
Mechanism Of Interaction

scholarly journals Development of a Phototoxicity Testing Strategy for Accurate Photosafety Evaluation of Pharmaceuticals Based on the Assessment of Possible Melanin-Binding Effects

2018 ◽  
Vol 37 (4) ◽  
pp. 296-307
Author(s):  
Jelle Reinen ◽  
Pieter van Sas ◽  
Ton van Huygevoort ◽  
Leticia Rubio ◽  
Kevin Scase ◽  
...  
Keyword(s):  
Cellular Damage ◽  
In Vivo Studies ◽  
Brown Norway ◽  
Albino Rats ◽  
Guidance Document ◽  
High Affinity ◽  
Drug Concentrations ◽  
Melanin Binding

Drug-induced phototoxicity occurs when drugs absorb natural sunlight, leading to chemical reactions causing cellular damage. Distribution to light-exposed tissues is critical and is enhanced by binding to melanin. The International Council on Harmonization S10 guidance document on photosafety evaluation of pharmaceuticals states that although nonpigmented skin tends to be more sensitive than pigmented skin, pigmented skin models should be considered for drugs that bind significantly to melanin. In this study, an in vitro melanin-binding assay was evaluated as prescreening tool for animal model selection. Binding of various structurally diverse phototoxic drugs to synthetic melanin was investigated in vitro and the high-affinity binder sparfloxacin (SPX), moderate-affinity binder 8-methoxypsoralen (8-MOP), and low-affinity binder pirfenidone (PIF) were selected for in vivo studies. Pigmented Brown Norway (BN) rats were compared with nonpigmented Wistar Albino rats to evaluate their sensitivity for the assessment of phototoxicity and skin concentrations of the drugs were measured. For SPX, the onset of phototoxic symptoms was faster for BN rats and drug concentrations were significantly higher in skin of BN rats. For 8-MOP, both models showed comparable sensitivity and skin concentrations did not differ. For the low-affinity binder PIF, no phototoxic effects were observed and skin concentrations in both models were similar. A combined in vitro/in vivo approach was developed that can be applied for accurate photosafety evaluation of pharmaceuticals based on the assessment of possible melanin-binding effects. In view of the presented data, the pigmented model could be considered for compounds showing a high-affinity binding capacity in vitro.

scholarly journals Boosting GSH Using the Co-Drug Approach: I-152, a Conjugate of N-acetyl-cysteine and β-mercaptoethylamine

Nutrients ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 1291 ◽  
Author(s):  
Rita Crinelli ◽  
Carolina Zara ◽  
Michaël Smietana ◽  
Michele Retini ◽  
Mauro Magnani ◽  
...  
Keyword(s):  
Cell Cultures ◽  
In Vivo Studies ◽  
In Vivo Metabolism ◽  
Pharmacokinetic Properties ◽  
Immunomodulatory Properties ◽  
Acetyl Cysteine ◽  
High Doses ◽  
The Brain

Glutathione (GSH) has poor pharmacokinetic properties; thus, several derivatives and biosynthetic precursors have been proposed as GSH-boosting drugs. I-152 is a conjugate of N-acetyl-cysteine (NAC) and S-acetyl-β-mercaptoethylamine (SMEA) designed to release the parent drugs (i.e., NAC and β-mercaptoethylamine or cysteamine, MEA). NAC is a precursor of L-cysteine, while MEA is an aminothiol able to increase GSH content; thus, I-152 represents the very first attempt to combine two pro-GSH molecules. In this review, the in-vitro and in-vivo metabolism, pro-GSH activity and antiviral and immunomodulatory properties of I-152 are discussed. Under physiological GSH conditions, low I-152 doses increase cellular GSH content; by contrast, high doses cause GSH depletion but yield a high content of NAC, MEA and I-152, which can be used to resynthesize GSH. Preliminary in-vivo studies suggest that the molecule reaches mouse organs, including the brain, where its metabolites, NAC and MEA, are detected. In cell cultures, I-152 replenishes experimentally depleted GSH levels. Moreover, administration of I-152 to C57BL/6 mice infected with the retroviral complex LP-BM5 is effective in contrasting virus-induced GSH depletion, exerting at the same time antiviral and immunomodulatory functions. I-152 acts as a pro-GSH agent; however, GSH derivatives and NAC cannot completely replicate its effects. The co-delivery of different thiol species may lead to unpredictable outcomes, which warrant further investigation.

scholarly journals The Effects of Using Chemicals to Remove Slime from African Giant Land Snails Flesh during Processing on Some Nutritional and Biochemical Parameters

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Agbor Esther Etengeneng ◽  
Lamye Glory Moh ◽  
Suffo Kamela Arnaud Landry
Keyword(s):  
Biochemical Parameters ◽  
Relative Weight ◽  
Hdl Cholesterol ◽  
Land Snails ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Protein Ratio ◽  
Crude Lipid ◽  
Hematological Indices

The effects of chemicals commonly used in Cameroon to eliminate slime from the flesh of the African giant land snail, Archachatina marginata, during processing on some nutritional and biochemical parameters were investigated. Groups of snails were processed with these chemicals at three different concentrations. Proximate analysis of all the treated snail groups was carried out, and groups with the highest concentration of each chemical were used to compose diets for experimental rats. Thirty weanling male Wistar albino rats ( 31.25 ± 3.09   g ) aged 21days old were distributed into four groups and fed with 10% protein based diets of A. marginata named D1 (washed with only water), D2 (lime C-treated), D3 (alum C-treated), and D4 (salt C-treated). The crude protein contents of the treated groups reduced significantly when compared with the control (CW), with lime C-treated (LC) having the least here and in crude fiber, but higher (LC, LB, and LA) in dry matter. There was a significant reduction in the crude lipid of alum C-treated (AC) and salt A-treated (SA). In vivo studies showed a general decrease in food consumption, weight gained, efficiency of feed utilization (EFU), true protein digestibility (TD) (except D2), and hematological indices (RBCs (red blood cells), PCV (packed cell volume) of the treated groups (D2, D3, D4) when compared to the control (D1). On the other hand, an increase in the relative weight of the liver (RWL), aspartate aminotransferase (AST), alanine aminotransferase (ALT), and total cholesterol was observed with some of the treated diets; meanwhile, protein efficiency ratio (PER), net protein ratio (NPR), relative weight of the kidneys (RWK), HDL cholesterol, and triglycerides were not affected by these diets. These chemicals should only be used at low concentrations or not at all because of its toxicity at high concentrations.

NITROGEN METABOLISM IN COLD-EXPOSED RATS

1963 ◽  
Vol 41 (5) ◽  
pp. 1169-1179 ◽  
Author(s):  
John R. Beaton ◽  
T. Orme ◽  
J. Laufer ◽  
A. Turner
Keyword(s):  
Food Intake ◽  
Cold Exposure ◽  
Body Weight Gain ◽  
Urine Volume ◽  
Nitrogen Retention ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Period 2

In these studies, male albino rats were exposed to cold (2–3 °C) for a 7-day period. In vivo studies included the daily measurement of body weight gain, food intake, urine volume, body and liver composition, and nitrogen retention. In vitro, the activities of the following liver enzymes were measured: aspartic acid transaminase, alanine transaminase, arginase, glutamic acid dehydrogenase, and phosphate-activated glutaminase. The results of these experiments demonstrate that exposure of rats to cold increases amino acid catabolism, in part at least to meet increased energy requirements, and reduces protein synthesis as a consequence in the period 2–5 days inclusive, despite a marked increase in food intake. Cold exposure was without effect upon protein absorption but, after 24 hours in the cold, the nitrogen which appeared in the urine increased from about 55% (at 22 °C) to about 76% of the amount that had been absorbed. No effect of cold exposure on nitrogen retention was apparent in the first 24 hours of cold exposure. The subsequent decreased nitrogen retention, on a time basis, appears to bear a relationship to changes in liver enzyme activities, particularly to the increased activities of liver transaminases and arginase.

scholarly journals Biocompatible Nanoparticles as a Platform for Enhancing Antitumor Efficacy of Cisplatin–Tetradrine Combination

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Fangcen Liu ◽  
Xinyue Wang ◽  
Qin Liu ◽  
Huan Zhang ◽  
Li Xie ◽  
...  
Keyword(s):  
Side Effects ◽  
Double Emulsion ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Pet Ct ◽  
Pharmacokinetic Properties ◽  
Metabolic Activities ◽  
Fdg Pet Ct

AbstractCombination therapy has been a standard strategy in the clinical tumor treatment. We have demonstrated that combination of Tetradrine (Tet) and Cisplatin (CDDP) presented a marked synergistic anticancer activity, but inevitable side effects limit their therapeutic concentration. Considering the different physicochemical and pharmacokinetic properties of the two drugs, we loaded them into a nanovehicle together by the improved double emulsion method. The nanoparticles (NPs) were prepared from the mixture of poly(ethyleneglycol)–polycaprolactone (PEG–PCL) and polycarprolactone (HO-PCL), so CDDP and Tet can be located into the NPs simultaneously, resulting in low interfering effect and high stability. Images from fluorescence microscope revealed the cellular uptake of both hydrophilic and hydrophobic agents delivered by the NPs. In vitro studies on different tumor cell lines and tumor tissue revealed increased tumor inhibition and apoptosis rates. As to the in vivo studies, superior antitumor efficacy and reduced side effects were observed in the NPs group. Furthermore, 18FDG-PET/CT imaging demonstrated that NPs reduced metabolic activities of tumors more prominently. Our results suggest that PEG–PCL block copolymeric NPs could be a promising carrier for combined chemotherapy with solid efficacy and minor side effects.

scholarly journals Production and Evaluation of Nutritional Contents of Traditional Couscous from Sprouted Wheat Fortified with Glycine max (L.) merr (Soya Bean) and Cucurbita pepo (Pumpkin) Seeds

2020 ◽  
Vol 4 (2) ◽  
pp. p1
Author(s):  
Raihanatu MB ◽  
Falmata AS ◽  
Bintu BP ◽  
Maryam BK ◽  
Hadiza Ahmed Ali ◽  
...  
Keyword(s):  
Glycine Max ◽  
Cucurbita Pepo ◽  
Protein Quality ◽  
Soya Bean ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Nutritional Requirement ◽  
Pumpkin Seeds

The study was carried to process, produce, and evaluate nutritional contents of traditional couscous from sprouted wheat (Triticum aestivum), fortified with Soya bean (Glycine max) and Pumpkin (Cucurbita pepo) seeds. The composite couscous blends were traditionally produced and compared with commercial couscous. The sprouted wheat couscous blends were blended in different ratios, they include; unprocessed (Raw wheat, 100), blend 1 (sprouted wheat mixed with soya bean and pumpkin seeds, 70:20:10), blend 2 (sprouted wheat mixed with soya bean, 60:40) and blend 3 (sprouted wheat mixed with pumpkin seeds, 60:40). Traditional wheat couscous blends were fed to experimental albino rats of wister strain weighing between (35 g and 45 g) for a period of 28 days. The nutritional and physiochemical analysis were determined using standard laboratory methods. The Statistical Package for Social Sciences (SPSS), version 20.0 was used to analyze the data collected which were expressed as means ± SE. One way analysis of variance (ANOVA) and Duncan’s multiple range tests were used to compare the means obtained after each experiment. Differences were considered significant at p < 0.05. Processing (Sprouting) decreases the levels of anti-nutrients, mineral elements and vitamins. Supplementation with soya bean and pumpkin seeds increased the nutritional composition of the sprouted wheat couscous blends. Results of chemical composition showed that blend 2, recorded high protein (29.95%), fat (8.95%) and low carbohydrate content (49.56%), followed by blend 1 and then blend 3, while commercial couscous crude protein, fat and carbohydrate were 12.53%, 1.42% and 75.10% respectively. There was improved level of in vitro protein digestibility at 1 hour (76.64% to 98.59%) and at 6 hours (96.80% to 99.33%). Results of in vivo studies showed that raw wheat couscous recorded protein quality when compared with spouted wheat couscous blends produced. The biological values of the composite couscous blends range from 95.04% to 95.73% and blend 2, recorded high net protein utilization (98.57%). In terms of sensory evaluation using hedonic method, blend 2 was most acceptable and differ significantly (p < 0.05) with other sprouted wheat couscous blends and commercial couscous. The cost of producing sprouted wheat couscous blends is cheaper than the commercial couscous. The study has therefore, revealed that with proper selection of locally available cereal, it is possible to produce nutritious complementary couscous blends that would be acceptable and nutritionally adequate to meet up the nutritional requirement for both children and adults. It also compares favourably with the commercial couscous in terms of nutrient contents.

scholarly journals A SYNERGISTIC INSULINOTROPIC EFFECT OF GREEN TEA EXTRACT AND POMEGRANATE EXTRACT WITH ROSIGLITAZONE: BOTH IN VIVO AND IN VITRO EXPERIMENT

2020 ◽  
pp. 96-99
Author(s):  
REKHA S ◽  
CHANDRASHEKHARA S
Keyword(s):  
Green Tea ◽  
Type Ii Diabetes ◽  
Body Weight Gain ◽  
Serum Insulin ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Type Ii ◽  
Insulinotropic Effect

Objective: Scientists have growing interest in traditional medicinal plants as they contain active ingredients for the treatment of various diseases. Tea is one of the most popular beverages worldwide. The variety of tea and tea extracts in the market has different polyphenol profiles, which are the bioactive chemical entities. We performed a direct comparison between Thea sinensis, green tea extracts (GTEs), and Punica granatum peel powder (PGPP), which have been chemically well characterized in a type II diabetic mouse model. Methods: We conducted both in vivo and in vitro experiments in the present paper. In vivo studies were carried out on male Swiss albino rats having type II diabetes, induced by single intravenous injection of streptozotocin (0.7 mg/Kg i.m.) and IDDM rats received either PGPP (200 mg/kg) or GTE (100 mg/kg) as a single oral dose. After the above result, the extracts were further subjected to know the effect of insulin secretion by RIN-5F cells providing confirmation of insulinotropic effect. Results: The results revealed that both PGPP and GTE substantially lowered blood glucose levels and ameliorated glucose intolerance, both were effective in antihyperglycemic activity and in lowering body weight gain. Serum insulin levels significantly increased in GTE group as well as in PGPP group, suggesting that they were exerting hypoglycemic effects through different pathways. Conclusion: Synergistic action of PGPP and GTE is an effective alternative for the treatment of type II diabetes through the regeneration of β cells of pancreas.

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies

2002 ◽  
Vol 103 (s2002) ◽  
pp. 112S-117S ◽  
Author(s):  
Jerry L. WESSALE ◽  
Andrew L. ADLER ◽  
Eugene I. NOVOSAD ◽  
Samuel V. CALZADILLA ◽  
Brian D. DAYTON ◽  
...  
Keyword(s):  
Amino Acid ◽  
Ex Vivo ◽  
In Vivo Studies ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Pressor Responses ◽  
Pharmacokinetic Properties ◽  
Isolated Arteries

Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ETA and ETB receptors. In this report, we compare the efficacy, potency and pharmacokinetic properties of these four antagonists, including potency in inhibiting ET-1- or Sarafotoxin 6c-induced vessel constriction in isolated arteries and efficacy in antagonizing ET-1-, big ET-1- or Sarafotoxin 6c-induced pressor responses in rats.

NITROGEN METABOLISM IN COLD-EXPOSED RATS

1963 ◽  
Vol 41 (1) ◽  
pp. 1169-1179 ◽  
Author(s):  
John R. Beaton ◽  
T. Orme ◽  
J. Laufer ◽  
A. Turner
Keyword(s):  
Food Intake ◽  
Cold Exposure ◽  
Body Weight Gain ◽  
Urine Volume ◽  
Nitrogen Retention ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Period 2

In these studies, male albino rats were exposed to cold (2–3 °C) for a 7-day period. In vivo studies included the daily measurement of body weight gain, food intake, urine volume, body and liver composition, and nitrogen retention. In vitro, the activities of the following liver enzymes were measured: aspartic acid transaminase, alanine transaminase, arginase, glutamic acid dehydrogenase, and phosphate-activated glutaminase. The results of these experiments demonstrate that exposure of rats to cold increases amino acid catabolism, in part at least to meet increased energy requirements, and reduces protein synthesis as a consequence in the period 2–5 days inclusive, despite a marked increase in food intake. Cold exposure was without effect upon protein absorption but, after 24 hours in the cold, the nitrogen which appeared in the urine increased from about 55% (at 22 °C) to about 76% of the amount that had been absorbed. No effect of cold exposure on nitrogen retention was apparent in the first 24 hours of cold exposure. The subsequent decreased nitrogen retention, on a time basis, appears to bear a relationship to changes in liver enzyme activities, particularly to the increased activities of liver transaminases and arginase.

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