Research in Pharmaceutical Sciences

BACKGROUND AND PURPOSE: The present study aimed to obtain a taste-masked oral disintegrating tablet (ODT) containing tolterodine tartrate (TT) intercalated into montmorillonite (MMT). EXPERIMENTAL APPROACH: The TT-MMT hybrid was prepared by ion exchange reaction. The effect of the initial concentration of TT, MMT, temperature, and pH on the encapsulation efficiency (EE) % of the drug in MMT was evaluated. The selected TT-MMT hybrid was characterized by X-ray diffraction (XRD), Fourier transforms infrared (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM)...

BACKGROUND AND PURPOSE: Lactobacillus , the most popular probiotic, has recently gained more attention because it is a potential reservoir of antibiotic resistance. This review summarized and discussed the phenotypic-genotypic characteristics of antibiotic resistance. EXPERIMENTAL APPROACH: Google Scholar, PubMed, Web of Science, and Scopus were searched up to February 2022. The inclusion criteria were all studies testing antibiotic resistance of probiotic Lactobacillus strains present in human food supplementation and all human/animal model studies in which transferring antibiotic-resistant genes from Lactobacillus strains to another bacterium were investigated...

BACKGROUND AND PURPOSE: Several attempts have been made to synthesize and investigate modified flavonoids to improve their potential anticancer efficacy. This study aimed to determine the in vitro anti-viability, anti-migration, and anti-invasive effects of two novel hesperidin glycosides, hesperidin glucoside (HG1) and hesperidin maltoside (HG2), compared to original hesperidin and diosmin. EXPERIMENTAL APPROACH: Inhibitory effects on normal (MRC5) and cancer (A549) cell viability of hesperidin glycosides were investigated by the trypan blue and MTS assays...

BACKGROUND AND PURPOSE: Primary and metastatic breast cancers still represent an unmet clinical need for improved chemotherapy and hormone therapy. Considerable attention has been paid to natural anticancer compounds, especially lignans. The study aimed to evaluate the activity of several lignans against breast cancer cells and assess the effect of leading lignans on signaling pathways in combination with metformin. EXPERIMENTAL APPROACH: Human breast cancer cell lines MCF7 (hormone-dependent), MDA-MB-231, and SKBR3 (hormone-independent) were used...

BACKGROUND AND PURPOSE: P-glycoprotein (P-gp) is an adenosine triphosphate (ATP)-dependent membrane efflux pump for protecting cells against xenobiotic compounds. Unfortunately, overexpressed P-gp in neoplastic cells prevents cell entry of numerous chemotherapeutic agents leading to multidrug resistance (MDR). MDR cells may be re-sensitized to chemotherapeutic drugs via P-gp inhibition/modulation. Side effects of synthetic P-gp inhibitors encouraged the development of natural products...

BACKGROUND AND PURPOSE: The use of fluoxetine raises the risk of pancreatic beta-cell dysfunction. However, the specific mechanism behind its mechanism of action in beta cells is unknown. This study investigated the cellular response of MIN6 cells to fluoxetine using untargeted cell-based metabolomics. EXPERIMENTAL APPROACH: Metabolic profiling of MIN6 cells was performed using liquid chromatography-high resolution mass spectrometry (LC-HRMS) analysis on samples prepared under optimized conditions, followed by principal component analysis, partial least squares-discriminant analysis, and pair-wise orthogonal projections to latent structures discriminant analyses...

BACKGROUND AND PURPOSE: Renal hemodynamics is influenced by renal sympathetic nerves and the renin-angiotensin system. On the other hand, renal sympathetic denervation impacts kidney weight by affecting renal hemodynamics. The current study evaluated the role of the Mas receptor on renal hemodynamic responses under basal conditions and in response to angiotensin II (Ang II) in chronic renal sympathectomy in female and male rats. EXPERIMENTAL APPROACH: Forty-eight nephrectomized female and male rats were anesthetized and cannulated...

BACKGROUND AND PURPOSE: Biomaterials, scaffold manufacturing, and design strategies with acceptable mechanical properties are the most critical challenges facing tissue engineering. EXPERIMENTAL APPROACH: In this study, polycaprolactone (PCL) scaffolds were fabricated through a novel three-dimensional (3D) printing method. The PCL scaffolds were then coated with 2% agarose (Ag) hydrogel. The 3D-printed PCL and PCL/Ag scaffolds were characterized for their mechanical properties, porosity, hydrophilicity, and water absorption...

BACKGROUND AND PURPOSE: Enzyme engineering is the process of raising enzyme efficiency and activity by altering amino acid sequences. Kallikrein 6 (KLK6) enzyme is a secreted serine protease involved in a variety of physiological and pathological activities. The increased expression of KLK6 plays a key role in various diseases. Instability and spontaneous activation and deactivation are major challenges in the study of this enzyme. This study aimed to create a stable pro-KLK6 enzyme by enzyme engineering, designing a specific cleavage site for enterokinase, and using Pichia pastoris GS115 as a host cell...

BACKGROUND AND PURPOSE: The current study aimed to study the therapeutic effects of lupeol as a nutritional triterpene on non-alcoholic fatty liver disease (NAFLD) and polycystic ovarian syndrome (PCOS) disorders in separate and concurrent models. EXPERIMENTAL APPROACH: This study was performed in three sets and each set contained 4 groups of female mice (n = 6), including control, NAFLD or PCOS and/or NAFLD/PCOS, lupeol, and metformin (MET). The treatment groups following the induction of disorders were treated with lupeol (40 mg/kg, orally) or MET (500 mg/kg, orally) for 28 days...

BACKGROUND AND PURPOSE: Previous studies highlighted that chemoprevention curcumin analog-1.1 (CCA-1.1) demonstrated an antitumor effect on breast, leukemia, and colorectal cancer cells. By utilizing immortalized MDA-MB-231 and HCC1954 cells, we evaluated the anticancer properties of CCA-1.1 and its mediated activity to promote cellular death. EXPERIMENTAL APPROACH: Cytotoxicity and anti-proliferation were assayed using trypan blue exclusion. The cell cycle profile after CCA-1...

BACKGROUND AND PURPOSE: The incidence of antibiotic resistance rapidly emerges over the globe. In the present study, the synthesis of thiourea derivatives as antibacterial agents and their biological evaluation are reported. EXPERIMENTAL APPROACH: Preliminary studies were done by molecular docking of four analogs of 1-allyl-3-benzoylthiourea, clorobiocin, and ciprofloxacin on the DNA gyrase subunit B receptor (PDB: 1KZN). The nucleophilic substitution reaction of benzoyl chloride analogs to the allylthiourea yielded four 1-allyl-3-benzoylthiourea analogs (Cpd 1-4)...

BACKGROUND AND PURPOSE: Prostate cancer is the second cause of death among men. Nowadays, treating various cancers with medicinal plants is more common than other therapeutic agents due to their minor side effects. This study aimed to evaluate the effect of taraxasterol on the prostate cancer cell line. EXPERIMENTAL APPROACH: The prostate cancer cell line (PC3) was cultured in a nutrient medium. MTT method and trypan blue staining were used to evaluate the viability of cells in the presence of different concentrations of taraxasterol, and IC50 was calculated...

BACKGROUND AND PURPOSE: The central nucleus of the amygdala (CeA) is one of the nuclei involved in the reward system. The aim of the current study was to investigate the electrical stimulation (e-stim) effect of the CeA in combination with dopamine D1 receptor antagonist on morphine-induced conditioned place preference (CPP) in male rats. EXPERIMENTAL APPROACH: A 5-day procedure of CPP was used in this study. Morphine was administered at an effective dose of 5 mg/kg, and SCH23390 as a selective D1 receptor antagonist was administrated into the CeA...

BACKGROUND AND PURPOSE: Bhamrung-Lohit (BRL) remedy is a traditional Thai medicine (TTM). There are few reports of biological activity, the activity of its constituent plants, or quantitative analytical methods for the content of phytochemicals. In this study, we investigated antioxidant, anti-inflammatory activity, and total phenolic and flavonoid content and validated a new analytical method for BRL. EXPERIMENTAL APPROACH: Antioxidant activity was evaluated by a 2,2-diphenyl-1-picrylhydrazyl (DPPH and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging...

BACKGROUND AND PURPOSE: One strategy to overcome methotrexate (MTX) resistance in acute lymphoblastic leukemia is suppressing MDR1 expression. It has been proved Astragalus polysaccharides (APS) exert their anticancer effect by reversing drug resistance. Due to the structural similarity of tragacanthin and bassorin with APS, we aimed to investigate the effects of the aforementioned polysaccharides on the expression of the MDR1 gene in the MTX-treated CCRF-CEM cells. EXPERIMENTAL APPROACH: Cytotoxicity of APS, bassorin, and tragacanthin on CCRF-CEM, CCRF-CEM/MTX (cells treated with MTX at IC50 ), and CCRF-CEM/R cells (CCRF-CEM cells resistant to MTX) was evaluated by MTT assay...

BACKGROUND AND PURPOSE: Acyl-CoA synthetase (ACS) enzymes play an important role in the activation of fatty acids. While many studies have found correlations between the expression levels of ACS enzymes with the progression, growth, and survival of cancer cells, their role and expression patterns in colon adenocarcinoma are still greatly unknown and demand further investigation. EXPERIMENTAL APPROACH: The expression data of colon adenocarcinoma samples were downloaded from the Cancer Genome Atlas (TCGA) database...

BACKGROUND AND PURPOSE: Though controversial, many clinical trials have been conducted to evaluate the efficacy of intravenous immunoglobulins (IVIG) in COVID-19 cases. Therefore, a systematic review and meta-analysis have been performed to evaluate the efficacy of IVIG in the treatment of COVID-19 patients. EXPERIMENTAL APPROACH: A systematic search was performed in electronic databases and preprint servers up to November 20, 2021. Since substantial heterogeneity was expected, a random-effects model was applied to pool effect size from included studies to calculate the standardized mean differences (SMDs) for the continuous variables and relative risks (RRs) for the dichotomous variable with 95% confidence intervals (CIs)...

BACKGROUND AND PURPOSE: The renin-angiotensin system activation, partial ischemia/reperfusion (IR) injury, and hypertension contribute to the development of acute kidney injury. The study aims to look at the vascular responses of angiotensin II (Ang II) during Ang II type 1 receptor (AT1R) blockade (losartan) or co-blockades of AT1R and Mas receptor (A779) in two kidneys one clip (2K1C) hypertensive rats which subjected to partial IR injury with and without ischemia preconditioning (IPC)...

BACKGROUND AND PURPOSE: Excitotoxicity in nerve cells is a type of neurotoxicity in which excessive stimulation of receptors (such as N-methyl-d-aspartate glutamate receptors (NMDAR)) leads to the influx of high-level calcium ions into cells and finally cell damage or death. This complication can occur after taking some of the plasminogen activators like tissue plasminogen activator and reteplase. The interaction of the kringle2 domain in such plasminogen activator with the amino-terminal domain (ATD) of the NR1 subunit of NMDAR finally leads to excitotoxicity...