Research in Pharmaceutical Sciences

BACKGROUND AND PURPOSE: Since insulin and pramlintide cooperate in glucose hemostasis, co-administration and quantitation of them in pharmaceutical preparations are imperative. A simple, rapid, sensitive, and isocratic RP-HPLC method was developed and validated for simultaneous quantitation of insulin and pramlintide in loading and in-vitro release studies of a glucose-responsive system to improve the control of hyperglycemic episodes in diabetic patients. EXPERIMENTAL APPROACH: The isocratic RP-HPLC separation was achieved on a C18 µ-Bondopak column (250 mm × 4...

Background and purpose: Hypoxia-inducible factors (HIFs) are transcription factors that get activated and stabilized in the heterodimerized form under hypoxic conditions. many studies have reported the importance of the HIF-1α and HIF-2α activity in biological pathways of hypoxic cancer cells. However, the importance of HIF-3α in a variety of cancers remains unknown. Experimental approach: The expression profile of 13 different types of cancer samples from the Cancer Genome Atlas (TCGA) database were subjected to normalization, and differential gene expression analysis was performed using computational algorithms by R programming...

Background and purpose: Yam bean ( Pachyrhizus erosus ) is a potent medicinal plant exerting therapeutical effects against diseases. However, investigations on the health benefits of its fiber remain limited. This study aimed to investigate the potential of yam bean fiber (YBF) against a high-fat diet (HFD)-induced metabolic diseases, inflammation, and gut dysbiosis. Experimental approach: Adult male mice were assigned to four groups (8 each), namely a normal diet-fed group (ND), HFD-fed group, and HFD supplemented with YBF groups (HFD + YBF) at a dose of 2...

Background and purpose: Osteoarthritis is a degenerative joint disease without definite treatment. It is characterized by intra-articular inflammation, cartilage degeneration, subchondral bone remodeling, and joint pain. The objective of the current study was to assess the anti-osteoarthritic effect and the possible underlying mechanism of action of Crataegus sinaica extract (CSE). Experimental approach: Intra-articular injection of monosodium iodoacetate in the right knee joint of all rats was done except for the sham group...

Background and purpose: One of the most noteworthy methods to slow down multiple sclerosis (MS) progress is a decrease of lymphocyte cells via S1P1 receptor modulating. Here, a series of S1P1 receptor modulators were designed and investigated for their ability to decrease lymphocytes in a rat model. Experimental approach: Molecular docking was performed to compare the binding mode of desired compounds 5a-f with fingolimod to the active site of the S1P1 receptor, theoretically...

Background and purpose: Quantum dots (QDs) are semiconductor nanocrystals that are widely used in biology due to their good optical properties. QDs, especially cadmium-based QDs, play an important role in the diagnosis and treatment of cancer due to their intrinsic fluorescence. The aim of the present study was the evaluation of the cellular uptake mechanisms of CdTe QDs in ovarian cancer cell lines. Experimental approach: In this study, we used CdTe QDs coated with thioglycolic acid...

Background and purpose: Ferula gummosa ( F. gummosa ), a potent medicinal herb, has been shown to possess anticancer activities in vitro . The present examination evaluated the cytotoxic and apoptogenic impacts of F. gummosa gum on the U87 glioblastoma cells. Experimental approach: MTT assay to determine the cell viability, flow cytometry by annexin V/FITC-PI to apoptosis evaluation, reactive oxygen species (ROS) assay, and quantitative RT-PCR were performed. Findings / Results: The results revealed that F...

Background and purpose: Prolonging the drug release can be a suitable approach to overcome the challenges related to topical ophthalmic administration of drugs especially the ones prescribed for chronic ailments. The sustained delivery of the drug would reduce the required frequency of administration which could extremely improve patient compliance and feeling of well-being. This study aimed to develop nanofibrous inserts for sustained ophthalmic delivery of timolol maleate (TIM) for the treatment of glaucoma...

Background and purpose: Histone deacetylation is one of the essential cellular pathways in the growth and spread of cancer, so the design of histone deacetylase (HDAC) inhibitors as anticancer agents is of great importance in pharmaceutical chemistry. Here, a series of indole acylhydrazone derivatives of 4-pyridone have been introduced as potential histone deacetylase inhibitors. Experimental approach: Seven indole-acylhydrazone-pyridinone derivatives were synthesized via simple, straightforward chemical procedures...

BACKGROUND AND PURPOSE: Garcinia mangostana , simply known as mangosteen, has long been used by Thai traditional medicine because of its reported antibacterial and anti-inflammatory activities for the treatment of skin infections. In this study, mangosteen pericarps were developed into a hydrogel patch to eradicate acne-inducing bacteria. EXPERIMENTAL PROCEDURE: The G. mangostana extract was investigated for bactericidal activity. A hydrogel patch containing the extract was examined for mechanical properties, antibacterial activity, in vitro release, skin permeation, and a phase I clinical study of skin irritation and allergic testing by a closed patch test...

Background and purpose: Ghrelin is known as a hunger hormone and plays a pivotal role in appetite, food intake, energy balance, glucose metabolism, and insulin secretion, making it a potential target for the treatment of obesity and type 2 diabetes. The essential maturation step of ghrelin to activate the GHS-R1a is the octanoylation of the Ser3, which is catalyzed by the ghrelin O-acyltransferase enzyme (GOAT) enzyme. Therefore, the inhibition of GOAT may be useful for treating ghrelin-related diseases...

BACKGROUND AND PURPOSE: Traditionally, Nigella sativa L. has been known as a medical intervention to treat numerous diseases. This study aimed at investigating the antihyperalgesic effect of black seed oil (BSO) in an experimental model of neuropathic pain. EXPERIMENTAL APPROACH: Chronic constriction injury (CCI) was performed under anesthesia. The sciatic nerve was ligated with four loose ties. Two separate protocols were used to administer BSO. In chronic treatment, rats were given daily doses of BSO (250, 500, and 1000 mg/kg p...

Background and purpose: Acinetobacter baumannii (A. baumannii) is known as a pathogen with antibiotic resistance, causing respiratory infections. PLGA has been approved for use in vaccines as well as drug delivery. This study was performed to evaluate PLGA nanoparticles containing the outer membrane proteins (OMPs) of A. baumannii in stimulating the mice's immune system and improving pneumonia. Experimental approach: Double emulsion solvent evaporation technique was used...

Background and purpose: Hepatic encephalopathy (HE) is a brain dysfunction caused by acute and chronic hepatic failure. The pathogenesis of HE is unknown, although small intestinal bacterial overgrowth associated with chronic liver damage, hyperammonemia, and oxidative stress are considered major factors for HE. Effective lowering of circulating ammonia and neuroinflammation is the main strategy for preventing and treating HE in cirrhosis. In the present study, the protective effect of probiotics (Lactobacillus plantarum and Bacillus clausii) and ascorbic acid in combination was assessed in bile duct ligation (BDL)-induced chronic HE in rats...

Background and purpose: Pomegranate seed extract (PSE) possesses anticancer activities and healing effects. Adipose-derived stem cells (ADSCs) are being considered a new candidate for cancer treatment. The purpose of this study was to investigate the effect of PSE on the cell cycle and apoptosis of the MCF-7 cell line in the co-culture condition with ADSCs. Experimental approach: MCF-7 and ADSC cells (ratio 1/1) were cultured in a transwell plate with and without PSE (PSE-co-culture and co-culture groups)...

Background and purpose: Epigenetics has been defined as the study of mitotically heritable alterations in gene expression that are not caused by changes in DNA sequence. Epigenetic-mediated silencing of a gene includes genomic imprinting, histone deacetylation, DNA methylation, and RNA-associated silencing. Cell growth and cell proliferation are inhibited by some histone deacetylase and histone inhibitors. This study was designed to investigate the effect of valproic acid (VPA) on extrinsic, intrinsic, and the Janus kinase (JAK)- signal transducer and activator of transcription (STAT) pathways in neuroblastoma and glioblastoma cell lines...

Background and purpose: Several pharmaceutical formulations were investigated to improve the solubility of 5-fluorouracil to enhance bioavailability and therapeutic efficacy. This study aimed to examine the potential use of cyclodextrin-based nanosponges for the incorporation of 5-fluorouracil and to investigate the use of different crosslinking agents on the properties of the resulting drug carrier. 5-Fluorouracil complexation with β-cyclodextrin was also studied to explain the unexpected results of weak 5-fluorouracil incorporation in nanosponge...

Background and purpose: Medicinal plants have been used to cure numerous diseases compared to orthodox medicines. The present study estimated the antidiabetic activity of ethanolic extract of Salvia tebesana Bunge in streptozotocin-induced diabetic rats. Experimental approach: In this study type 2 diabetes was induced in male rats by streptozotocin (65 mg/kg, i.p.). After diabetes induction, normal control groups were treated with distilled water, the positive control group received metformin (500 mg/kg), and the other groups were orally treated with ethanolic extracts of S...

Background and purpose: Cisplatin is a chemotherapeutic drug used to treat cancer, however, causes kidney toxicity. Harmine is a plant-derived alkaloid with a wide range of therapeutic applications. The effects of harmine on the renal side effects of cisplatin in mice were studied in this study. Experimental approach: Forty-eight male BALB/c mice were randomly divided into eight groups (n = 6). They were treated with saline, cisplatin (5.5 mg/kg), harmine (5, 10, and 15 mg/kg/day), cisplatin + harmine (5, 10, and 15 mg/kg/day), respectively...

Background and purpose: Inflammatory bowel disease (IBD) is a chronic and multifactorial disease with unknown etiology and a decisive cure. Salvia officinalis (sage) which has anti-inflammatory, anti-oxidative, and ulcer healing properties can be useful for the treatment of IBD. Therefore, the effect of S. officinalis ethanolic extract (SOEE) and methanolic partition (SOMP) was investigated on acetic acid-induced ulcerative colitis. Experimental approach: Male Wistar rats (180-220 g) were used...