Iraqi Journal of Pharmaceutical Sciences
Iraqi Journal of Pharmaceutical Sciences (IJPS) is the official journal of the College of Pharmacy, University of Baghdad. The IJPS is a biannual specialized scientific journal which was first founded in 1979. The aim of this journal is to support scientific knowledge and encourage scientific research and publications. The IJPS provides a forum for reporting innovations, production methods, technologies, initiatives and the application of scientific knowledge to all aspects of pharmaceutical sciences, including advanced drug delivery systems, drug targeting, pharmacodynamics, pharmacokinetics, pharmacogenomics, biopharmaceutics, drug and prodrug design, pharmaceutical analysis, drug stability, quality control, pharmaceutical engineering, and pharmacy practice . The journal has issued thirty volumes and fifty three issues from 1979 until December of 2021. Iraqi Journal of Pharmaceutical Sciences (IJPS) is an open access peer-reviewed journal. Open access (OA) refers to a free and unrestricted online access to journal articles. The OA content is open to all with no access fees. For more information on Creative Commons license and the benefits of publishing an open access article
University of Baghdad- College of Pharmacy
Understanding Medicine Need Estimation within the Public Healthcare System in Iraq: A Review Article
The Iraqi medication management system comprises five key pillars: selection, need estimation, procurement, storage and distribution, and use. Despite the diligent efforts of pharmacists to accurately estimate medication needs, Iraqi public health institutions sometimes experience medication shortages due to inadequate budget allocations and procurement challenges. This review examines current practices, legislation, and challenges in the need estimation of medications. Indeed, there is significant collaboration among Iraqi health authorities responsible for medication approval, regulation, procurement, and dispensing. Key stakeholders, including the Directorate of Technical Affairs/Department of Need Estimation, Department of Pharmacy, KIMADIA, health directorates, and pharmacy and therapeutics committees in public health institutions collaborate to estimate annual medication needs. The methods for calculating needs include consumption, morbidity, and proxy methods, each with distinct advantages and limitations. The article highlights how morbidity data, medication consumption records, and medical employed protocols influence medication estimation processes. Obstacles hindering accurate estimation include inadequate electronic systems, inconsistent supply, expiring medications, population displacement, health crises (e.g., COVID-19), insurance implementation, and changes in prescribing practices. In conclusion, estimating medication needs in the public health sector is crucial for sustainable supply, but it is a complex task with multiple protocols and challenges. To enhance the effectiveness of medication, and need estimation in Iraq, the health system must prioritize electronic documentation and allocate sufficient budgets. By addressing these challenges, sustainable medication supply can be achieved in public healthcare settings.
Copyright (c) 2026 Iraqi Journal of Pharmaceutical Sciences https://creativecommons.org/licenses/by/4.0
The Potential for Enhanced Systemic Delivery of Nimodipine Loaded Polymeric Nanoparticles via Bilayer Dissolving Microneedles
Nimodipine (NID) is used for the prevention of ruptured intracranial aneurysms and subarachnoid haemorrhage (SAH). The objective of study using the benefits of a combined approach of polymeric nanoparticles and microneedles to fabricate NID as polymeric nanoparticles (NID-NPs) loaded in a bilayer dissolving microneedle (bDMNs) patch to enhance the delivery of drugs through skin layers as a promising noninvasive and painless delivery system, improving poor solubility and lower oral bioavailability (5–10%) owing to first-pass metabolism, which leads to frequent dosing, inconsistent clinical responses, and poor patient compliance. The NID-NPs formula was fabricated with a (1:8) drug to polymer, Soluplus®, w/w ratio and 0.25% polyvinylpyrrolidone K15 (PVPK15) using nanoprecipitation technique. Formulas were characterized by measuring particle size (PS), polydisperse index (PDI), and entrapment efficiency (%EE). It exhibits a PS (81.78 nm) and PDI (0.046), zeta potential (-18.96 mV), and aspherical shape examined by transmission electron microscopy (TEM) with improved NID release. Moreover, the formula was designed as bilayer dissolved microneedles (bDMNs) using micromolding technique in polydimethylsiloxane (PDMS) molds. Eight microneedle (MN1-MN8) patches of polymers such as hyaluronic acid (HA), polyvinylpyrrolidone (PAPK30), polyvinyl alcohol (PVA), carboxymethylcellulose (CMC), and Pullulan (Pu) employ two plasticizers, glycerin (Gly) and polyethylene glycol 400 (PEG). The optimised formula MN2 with 10% PVA and 5% glycerin as amatrix was evaluated by measuring drug content, % moisture absorbance (%MA), weight variation, surface pH, and maximum mechanical needle strength for all MNs. Ex-vivo permeation study displayed that 80% of NID permeated in less than 2hr with a lag time of 2-3min. Insertion and mechanical studies show high resistance. Morphological study by field emission scanning electron microscopy (FE-SEM) was studied before and after the insertion into the skin, which displays sharp, strong, and uniform MNs. As a result, NP-bDMNs achieved an improvement in both solubility and drug release for transdermal drug delivery, reduced dose frequency, fewer side effects, and improved patient compliance.
In Silico Study, Synthesis and Evaluation of New Indole-Hydrazones as Potential Antibacterial Agents
Because pathogenic bacteria have gained resistance, bacterial illnesses are difficult to treat. Every year, a huge number of studies aimed at creating novel antibacterials are released. Shiff bases are an important field in organic synthesis due to their biological activities. Schiff bases also possessing an important range of pharmacological activities. Hybridization-combing two pharmacophores [heterocycle from starting molecule and synthesized hydrazones] to form one molecule-is the important method in designing new drugs. The new compounds [hydrazones] derivatives were created using a multi-step process including synthesis of indomethacin hydrazide by coupling agent reaction (EDC.HCL,HOBt) and then reaction with defferent aldehydes to form hydrazones , and thin-layer chromatography, ATR-FTIR, and 1HNMR spectroscopy were used to characterize them. Our objective is to create compounds with appropriate ADMET qualities that can be manufactured and employed in the future, as well as antibacterial activity based on molecular docking. Utilizing the fast resazurin micro titer assay MIC (minimum inhibitory concentration) method, the novel compounds' antibacterial properties were assessed. some compounds (IIIC) showed comparable activities to ciprofloxacin against S. aureus and comparable activity of ( IIIC , IIID ) against K. pneumonia other (IIIB) showed more potent against K. pneumonia, and in general all new compounds show good activities against E. coli, k .pneumonia , S. pyogenes and S. aureus.
Antibacterial, Bacterial infections, Heterocycles
Hepatoprotective Potential of Apigenin versus Vitexin: A Comparative Study in an Acetaminophen-Induced Acute Liver Injury Rat's Model
Background: Paracetamol poisoning is a global issue that results in severe liver failure and permanent liver damage, necessitating the need for liver transplantation. The objective of our study was to assess and compare the preventive effects of Apigenin and vitexin against paracetamol-induced liver damage in rats. Methods: Rats were divided into four groups and treated for seven consecutive days. Group I received 0.5% DMSO, Group II received a single paracetamol dose, and Groups III-IV received 10 mg/kg Apigenin or 40 mg/kg vitexin i.p for 7 days. On the seventh day, all groups except the Group I received a single oral dosage of 3000 mg/kg paracetamol three hours after their final Apigenin or vitexin dose. After 24 hours of paracetamol administration, the animals were sacrificed and their blood and livers were taken for biochemical and histopathological examination. Results: The results demonstrated that paracetamol treatment led to notable increases (p < 0.05) in blood biochemical markers (ALT, AST, and ALP), in contrast to the negative control groups. However, after receiving Apigenin, rats exhibited a notable decrease (p<0.05) in the level of these biomarkers. After vitexin pretreatment, the levels of these enzymes were reduced, but this reduction was statistically significant only for the ALP level when compared to the paracetamol group. (p<0.05). Furthermore, Apigenin pretreatment was able to restore normal liver histopathology, while vitexin was not. Conclusion: our research validated the hepatoprotective properties of Apigenin against paracetamol hepatotoxicity and provided insight into potential distinctions in the effects of a flavonoid and its glycosylated form.
Apigenin, vitexin, hepatoprotection, paracetamol, liver damage
Paracetamol hepatotoxicity and role of flavonoids
Investigate the Factors Influencing the Formulation of Aceclofenac-Loaded Nanosponges Based on Eudragit L100
Among the many NSAIDs generated from phenyl acetic acid is Aceclofenac, or ACE. Its antipyretic, analgesic, and anti-inflammatory effects are noteworthy. However, the substance's delayed dissolution, limit permeability, and inadequate bioavailability are caused by its low solubility in water, which hinders its usefulness. Nanosponges (NS) are tiny particles with nanoscale holes and a distinctive three-dimensional nanostructure. The incorporation of both water-soluble and fat-soluble molecules into these hollow spaces enhances the efficacy and safety of medication delivery. This study aims to improve and advance the formulation of ACE-containing nanosponges. The emulsion solvent diffusion procedure is used to prepare the nanosponges that are based on Eudragit L100. The effect of the amounts of polyvinyl alcohol (PVA) and the drug-to-polymer ratio on nanosponge properties are explored. Particle size, product yield, and ACE trapped inside nanosponge percentages are the aspects that be considered during characterization. The results indicated that the product yield and drug entrapment % were significantly reduced as the concentration of Eudragit L100 was increased, while the particle size was significantly increased. A significant change was seen in product yield and entrapment percentage as the PVA content was increased. It also caused a notable increase in particle size. It could be concluded that Eudragit L100 can be used as a polymer matrix to incorporate ACE. In future investigations, ACE would be manufactured as a topical gel.
Comparative Carvedilol Nanomicelle Preparation Method: Thin-Film Hydration and Direct Dissolution using Soluplus and PVP K-25
The present work aims to formulate carvedilol as nanomicelle and study variables effect on the particle size of nanomicelle, and on the entrapment efficiency (EE%). The formulations were performed by two methods; thin film hydration method and direct dissolution method using soluplus® and polyvinylpyrrolidone (PVP K-25) as polymers. The results revealed that formulations prepared by direct dissolution method exhibits lower size and higher EE% as compared with thin film hydration method, it was found that soluplus® produces larger size of nanomicelle and lower EE% as compared with PVP K-25, it was found that as the amount of polymer raised, the size of nanomicelle increased in both polymers, the effect of solvent indicates that methanol solvent produced lower particle size as compared with ethanol. From all the results obtained, we conclude that the direct dissolution was the best method for preparation of carvedilol nanomicelle and PVP K-25 in a concentration of 1:5 considered the best polymer that gave the best result for preparation concerning nanomicelle size, and EE%.
Carvedilol, Nanomicelle, preparation method, PVP K-25, Soluplus.
The Anti-Inflammatory Effect of Chromium Picolinate in Doxorubicin Induced Cardiotoxicity in Rats
Doxorubicin is a potent anthracycline antibiotic used to treat many types of human neoplasms. The long-term adverse effect is cardiomyopathy, which is primarily caused by the extensive production of reactive oxygen species, which relates to several events related to nucleic acid metabolism and the activation of the immune system. Chromium is a trace element mostly utilized to regulate glucose levels and enhance the body's response to insulin, particularly in people with diabetes. Chromium picolinate often contains Chromium in its trivalent state, coupled with picolinic acid. The current study aims to evaluate the anti-inflammatory effect of chromium picolinate in doxorubicin-induced cardiotoxicity of rats. Twenty eight Wister male rats were used in this study and divided into 4 groups. Group I (Control group): Rats were given distilled water orally for 8 days. The rats were euthanized on the ninth day. Group II (Doxorubicin group): Rats were given distilled water orally for 7 days, followed by a single dose of doxorubicin (25 mg/kg) IP. The rats were euthanized on the ninth day. Group III (Chromium 2 mg/kg): Rats were given chromium picolinate at a dose (2 mg /kg) orally for 7 days, followed by a single dose of doxorubicin (25 mg/kg) IP. The rats were euthanized on the ninth day. Group IV (Chromium 4 mg/kg): Rats were given chromium picolinate at a dose (4 mg /kg) orally for 7 days, followed by a single dose of doxorubicin (25 mg/kg) IP. The rats were euthanized on the ninth day. The outcome of this study indicated that single IP dose of doxorubicin (25mg/kg) resulted in a significant elevation in cardiac creatine kinase MB, lactate dehydrogenase, and inflammatory cytokines (Interleukin1β and Tumor necrosis factor α) in group 2 compared to group 1 (P<0.05). Interestingly, co administration of chromium picolinate at dose (2mg/kg) and (4mg/kg) caused a significant decrease in cardiac biomarkers and inflammatory cytokines in groups 3 and 4 compared to group 2 (P<0.05).This current research indicated that Chromium picolinate have a potential role in reducing cardiac injury and inflammation in patients treated with doxorubicin.
Effect of Saxagliptin on Oxidative and Apoptotic Biomarkers in Doxorubicin- Induced Cardiac Injury in Comparison with Telmisartan Treated Rats
One of the most potent and effective drugs in the field of chemotherapy is doxorubicin. It has shown remarkable efficacy against multiple cancer targets. Despite the effectiveness of this treatment, an important drawback is the cardiotoxicity caused by doxorubicin. This limitation has led oncologists to explore potential ways to prevent or reduce this toxic side effect. We will investigate in this study whether saxagliptin and telmisartan have any protective effects on heart tissue. We will study their effects on oxidative stress and apoptotic indicators in particular. There were a total of 28 rats, with 7 animals in each of the four groups: First group(control group): seven rats in good health were given distilled water for fourteen days in a row before being sacrificed on the fifteenth day.Group 2 (positive group): Seven rats were given a 20 mg/kg intraperitoneal dose of doxorubicin HCl as a single dose. The rats were sacrificed after twenty-four hours. In the third group, rats took 10 mg/kg of saxagliptin orally for 14 days in a row. They received a single dosage of 20 mg/kg of Doxorubicin IP on day 15, and after 24 hours, they were slaughtered .In Group 4, seven rats were given 10 mg/kg of Telmisartan orally for 14 days in a row. Doxorubicin was administered intraperitoneally once at a dosage of 20 mg/kg on the fifteenth day. The rats were sacrificed after a day. Glutathione (GSH), malondialdehyde (MDA), creatinine kinase (CK-mb), and caspase 3 levels were quantified in several groups in this investigation. The doxorubicin treated group had a significantly lower GSH level compared to the saxagliptin and telmisartan groups (p<0.05). Likewise, when contrasted with the doxorubicin-treated group, the saxagliptin and telmisartan groups exhibited a substantial decrease in MDA levels (p<0.05). The doxorubicin treated group had significantly higher CK-mb levels compared to the saxagliptin and telmisartan groups (p<0.05). Finally, when comparing the groups treated with doxorubicin to those treated with saxagliptin and telmisartan, there was a substantial drop in caspase 3 levels (p<0.05). It is clear from our in vivo enzymatic analysis that saxagliptin and telmisartan show promise as doxorubicin cardiotoxicity protectants. Further research into their effects on cardiac biomarkers and anti-inflammatory capabilities, as well as further prospective preventative measures, should be undertaken in a long-term study.
Formulation and Evaluation of Lercanidipine HCL Loaded Nanomicelles
Among the strong calcium channel blockers, lercanidipine hydrochloride (LER) has been shown to be useful in reducing blood pressure by acting on L-type calcium channels. Nevertheless, the main drawback of lercanidipine is that it is a BCS class II medication with poor solubility and a 10% oral bioavailability because of significant first pass metabolism. The goal of this study is to use the thin film hydration process to generate and assess lercanidipine nanomicelles utilizing soluplus in conjugation with other surfactants/polymers at different ratios in order to boost the solubility of virtually insoluble LER. Six formulations were prepared and analyzed for their micelles size, polydispersity index (PDI), encapsulation efficiency (EE%), and in-vitro release. The optimum formula was determined to be the one prepared using soluplus, poloxamer188 and tween80(50mg). Micelle size was found to be 62.26 nm, with PDI 0.233 and EE (88.8%). An in-vitro release study was conducted, and the results showed that the chosen formula (solu/p188/tween50) released the entire dose of drug in 75 minutes with 94% release, compared to only 53% for pure drug.These findings indicate the strong potential of employing LER HCl micelles in dosage form formulation.
Optimization of Processing Parameters for the Preparation of Nimodipine-Loaded Transferosomes by Solvent Evaporation-Hydration Method
Nimodipine is a vasodilator medicinal agent approved for the prevention of cerebral vasospasm, a major risk factor that causes deaths in patients diagnosed with subarachnoid hemorrhage. The current marketed products of this drug are associated with challenges such as frequent dosing orally, or continuous infusion through central vein. Therefore, transdermal delivery of nimodipine via transferosomes can overcome these difficulties. Solvent evaporation-hydration method followed by sonication was applied for the preparation of transferosomes. The aim of present study is to investigate and optimize the processing parameters of this method through the utilization of Design-Expert software. Box-Behnken statistical design was selected for this purpose to study the hydration temperature, speed of rotation, and hydration time as independent variables, each at three levels. The vesicles sizes (VS), polydispersity index (PDI), and entrapment efficiency (EE) of nimodipine were the dependent variables. After statistical analysis of the obtained data, a batch was formulated according to the selected, optimized variables, and then the responses were compared to those predicted by the software. This batch was subjected to further characterization by transmission electron microscopy (TEM), degree of deformability and permeation through an excised skin of rat. The study showed that transferosomal formulations were within the nanoscale for VS of 95.4 - 914.0 nm with PDI of 0.0897 – 0.624% and EE was 65.2 - 98.3%. The chosen response ranges to optimize the processing parameters were 200.0 - 250.0 nm for VS, 0.1 – 0.4% for PDI and 80.0 - 100.0% for EE. The resulted values of the batch formulation were comparable as 197.0 nm, 0.01% and 91.4%, respectively. In addition, TEM revealed bilayer vesicular structure, degree of deformability was 0.98 and permeation calculated as the flux of nimodipine was 513 μg/cm2/h. In summary, this study demonstrates that in addition to addressing qualitative and quantitative concerns, optimizing the processing parameters can yield nimodipine-loaded transferosomes to achieve the desired properties of the transferosomes.
Transferosomes, nimodipine, Box-Behenken design, solvent evaporation-hydration
Molecular Docking, ADMET Study, Synthesis, Characterization, and Anti-proliferative Activity Study of Novel Schiff Base Derivatives of N'-benzylidene-4H-benzo[b][1,4]thiazine-3-carbohydrazide Against Lung Cancer Cell Line.
Epidermal growth factor receptor tyrosine kinase (EGFR-TK) is a vastly fascinating epigenetic target for medicine treatment. EGFR-TK is overexpressed in several diseases, including cancers. In this study, we designed new EGFR-TK inhibitors with the same consists of erlotinib (approved anticancer drug) with longer linker and substituted hydrophobic moiety using Ligand Designer from Glide (Schrodinger LLC). By experimenting with different amide and Schiff base residues, the linker was optimized. Using licensed Schrodinger modeling software, the probable inhibition over EGFR-TK for the best-designed items was virtually assessed. The findings demonstrated that there is a possibility of an acceptable level of fitness interaction between the hydroxylated substitution hydrophobic moiety and the EGFR-TK active site. To forecast the final drugs' pharmacokinetic characteristics, an ADMET analysis was conducted. Good predicted drug-like characteristics were displayed by the final compounds. Recrystallization was used to successfully manufacture and purify the intermediates and final chemicals. FTIR, 1HNMR, and 13CNMR spectroscopy were used to characterize the chemical structure of the intermediates and final products. Using MTT technique; all synthesized compounds (SH1-SH6) exposed a reassuring antiproliferative activity in A504 lung tumor cells lines with IC50 of 10.24 μM, 5.47 μM, 19.98 μM, 4.18 μM, 13.13 μM, and 3.88 μM respectively, and inhibition percentage of 82.3%, 88.2%, 70.5%, 82.3%, 82.3%, and 94.1% respectively, which is comparable to erlotinib IC50 of 3.86 μM and inhibition percentage of 94.7%. The compound SH6 was the most promising one (IC50=3.88µM and a percentage of inhibition=94.1%), compared with erlotinib, a reference authorized anticancer drug.
Some variables Affecting Preparation of Nanosuspension-based Gel of Paliperidone
An intranasal drug delivery system offers a non-invasive, effective, reliable, direct, and alternative route to the CNS via the neural connections between the nasal mucosa and the brain. Paliperidone (PAL) is mainly used to treat schizophrenia and disorder. It’s practically insoluble in water class II with low bioavailability 28%. Therefore the aim of preparation of nano nasal suspension gel is in order to target PAL to brain via neural connections of nasal mucosa and the brain, and then enhance the uptake and bioavailability of the drug near and at the site of action. Different variables were investigated in this study, in order to recognize the best formula that aims the drug to deliver by the brain through the nasal administration.Among these variables are, polymers types soluplus®, PVP (plasdone), HPMC ,and Poloxamer 188, besides to drug-polymer ratios, and stirring speed .The prepared suspension nano particles, were evaluated according to their particles sizes, poly dispersity index (PDI), and dissolution behavior in simultaneous nasal fluid pH 6.5.The in-vitro results of the study revealed that, lowest particle size diameter was with the drug loaded by soluplus® of (1:3), (71.28 nm), compared with PVP (plasdone) of (1:3), (146.2 nm.), Poloxamer188 of (1:3), (393.1nm.), and HPMC of (1:3), (251.2 nm.), respectively. Furthermore the poly dispersity index (PDI) demonstrates that soluplus® was the lowest (0.031), compared with PVP (0.163), Polyxamer188 (0.2428), and HPMC (0.309), respectively. While the calculated entrapment efficiency (EE) % of the all PAL prepared nano particles were ranged from 81.94% to 99.99 %. According to the particle size diameter, the formula F6 loaded by soluplus® of (1:3), was chosen for dissolution behavior of PAL in simultaneous nasal fluid pH 6.5, it gave 98% drug released, and estimated time for 50%, and 75% PAL released at 40.3 and 73.2 minutes, respectively
Inducing Selective Starvation of Cancer Cells through Synergistic Inhibition of glycolysis using Mannoheptulose and 2-Deoxy-D-Glucose
The unique opportunity lies in targeting tumor cells through glycolysis, a pathway that compensates for decreased ATP production by increasing sugar consumption. This strategy allows for the development of a novel therapeutic approach, targeting malignant cells with selective pharmacological inhibitors of glycolysis without harming normal cells. In this study, hexokinase, glycolytic enzyme, was targeting to selectively inhibit energy production pathways in cancer cells without harming normal cells. The anticancer mechanisms of 2 Deoxy-D-Glucose (2DG) and Mannoheptulose (MH) in esophagus adenocarcinoma (SK-GT-4) and HBL-100 normal cell lines were investigated using MTT and wound healing assays to assess their cytotoxic effects and cellular proliferation. The apoptosis effect was detected using the AO/EB assay. To confirm the effect of agents on cell energy metabolism, the levels of ATP, pyruvate, and hexokinase were assessed as glycolysis parameters. The results showed significant cytotoxic effects of 2DG and MH on the growth of cancer cells, with a strong synergistic effect when used in combination, especially in SK-GT-4 cells. The IC50 values for 2DG and MH were 278 and 440 µg/mL, respectively, in SK-GT-4 cells, while HBL-100 cells did not reach IC50 values. Wound healing outcomes indicated a decrease in proliferation and invasion of cancer cells. Measurements of ATP and pyruvate levels showed that the combined use of the two drugs more effectively reduces cellular energy compared to using them independently, suggesting a synergistic effect against cancer cells and potential for a more effective treatment approach in the future
Design, Synthesis, and Anticancer Activity Study of several New Schiff Base Imidyl Sulfa Drug Derivatives based on N-(Sulfamethoxazole-4-yl)-4-Aminomethylbenzylidene
In this research, a series of new (Schiff base imidly sulfa drug) derivatives were designed and synthesized via many steps. In the first step, a sulfa drug (sulfamethoxazole) was chosen as a bioactive starting material and introduced in a condensation reaction with 4-amino acetophenone under microwave irradiation producing compound [1] N-(sulfamethoxazole-4\-yl)-4-amino methyl benzylidene. Subsequently, in the second step, compound [1] was introduced in reaction with three cyclic anhydrides, namely (succinic, maleic, and phthalic) anhydrides producing amic acid compounds [2-4], and these, inturn, introduced in the third step in a dehydration reaction via treatment with acetic anhydride and sodium acetate under reflux producing the target corresponding cyclic imide [5-7]. The work also involved a synthesis of other (Schiff base imidyl sulfa drug) derivatives (quinazoline) [8-10] via treatment of compounds [5-7] with anthranilic acid, while treatment of compound [5-7] with phthalic anhydride afforded other new derivatives (oxazepin) [11-13]. Since molecules of the newly synthesized compound contain three biologically active segments, two of them are sulfa drug and cyclic imide. At the same time, the third segment is Schiff base in compounds [5-7], quinazoline in compounds [8-10], and oxazepin in compounds [11-13]. They are expected to possess high biological activity. Thus, the work involved also studying the anticancer activity of the prepared compounds against breast cancer, and the results are promising.
Schiff base, cyclic imide, sulfamethoxazole drug and MDA assay
Effect of Physalis angulata Active Fraction on The Spermatogenic Cells, mRNA Expression of NFкB and TNF-α in Testicular Diabetic Rat Model
Hyperglycemia in diabetes mellitus (DM) induces oxidative stress, leading to inflammation, a decrease in the number of spermatogenic cells, and reduced testicular weight, which may affect reproduction and result in infertility. Ciplukan (Physalis angulata) contains flavonoid compounds that function as antioxidants to combat free radicals and exhibit protective and therapeutic effects on spermatogenic cells in diabetic rats. This study aims to investigate the protective effect of active fraction of P. angulata on the histology of spermatogenic cells, mRNA expression of NFkB and TNF-α, and testicular weight in a diabetic rat model. This study used a post-test-only control group design with 5 groups: control (K), DM group (K-DM), DM treated with active fraction of P. angulata at doses of 8.5, 34, and 136 mg/kg BW (KP-1, KP-2, KP-3, respectively). Each group consisted of 5 male Wistar rats (Rattus norvegicus). Testicular histology was analyzed with HE staining, mRNA expression of NFkB and TNF-α was measured using qPCR. To account for variations in body size, the testicular weight was normalized to tibia length, resulting in the testicular weight-to-tibia length ratio. Statistical analysis, including the Shapiro-Wilk normality test and ANOVA, was performed using SPSS. The number of spermatogenic cells, including spermatogonium, primary spermatocytes, and spermatids, in the treatment group given the active fraction of P. angulata was significantly higher, whereas the mRNA expression of NFкB and TNF-α were significantly lower than K-DM group. The ratio of testicle weight per tibia length in K-P1 (34.24±10.95 mg/mm), KP-2 (34.25±2.45 mg/mm) and KP-3 (39.5±2.69 mg/mm) groups were not significantly higher than DM (34.21±2.88 mg/mm) group.
Diabetes mellitus, Histology, Inflammation, NFкB, Physalis angulata, Testis, TNF-α
ADME Study, Molecular Docking, Synthesis, Characterization, and Preliminary Antimicrobial Activity Evaluation of New Glycine Derivatives of Sulfonamide
A novel glycine-based sulfonamide derivates were synthesized. This study presents the newly synthesized compounds (G1-G6) that exhibit promising DHPS inhibition activities, designed through a molecular docking analysis targeting the Yersinia pestis DHPS protein (PDB ID: 5JQ9). The docked compounds were subsequently subjected to ADME study to evaluate their pharmacokinetic properties. This work started with the synthesis of the glycine methyl ester HCL salt by esterification of the carbonyl group of the carboxylic acid functionality of glycine with thionyl chloride and methanol and the synthesis of 4-acetamidobenzene sulfonyl chloride from acetanilide, the reaction of the latter two intermediates using the TEA as base and neutralizing agent in DCM led to the synthesis of a sulfonamide-containing compound. This compound was then reacted with hydrazine hydrate to give the hydrazide, which was then reacted with various aldehydes using glacial acetic acid as a catalyst to give the final target compounds G1-6. The identification of these compounds was carried out using infrared spectroscopy (ATR-FTIR) and proton magnetic resonance. Using the well diffusion method, the antimicrobial activity of the final compounds was tested in vitro against two Gram-positive bacteria, two Gram-negative bacteria and one fungus in comparison with the standard drugs sulfamethoxazole, sulfadiazine and fluconazole. In general, all synthesized compounds have moderate to high antimicrobial activity, but compounds G5 and G6 with the highest activity had zone inhibition (ZI) ranging from 16 to 21 mm.
Evaluation of the Protective Effect of Echinacea purpurea on Iron Overload-Induced Multi-Organ Damage in Male Rats: In Comparison with Vitamin E
By producing reactive oxygen species, primarily reactive hydroxyl radicals, iron overload may contribute to cellular damage and change the integrity of essential organelles. Echinacea Purpura; a medical plant with a root liquid extract contains various biologically active phytochemical compounds. This study aimed to evaluate the protective effect of Echinacea Purpura on bone marrow suppression with liver and spleen cells apoptosis induced by iron overload. Fifty albino rats were divided into five groups: Group (I) [negative control] intraperitoneally injection with (0.2 ml) normal saline solution every 3 days; with daily oral gavage of (1 ml) normal saline for 4 weeks. Group (II) [Iron-overloaded]: Rats intraperitoneally injected with (200 mg/kg/day iron dextran every 3 days); with daily oral gavage of (1 ml) normal saline solution for 4 weeks. Group (III) Rats intraperitoneally injected with iron dextran (200 mg/kg/day every 3 days)+Echinacea (100mg/kg/day) orally administered for 4 weeks. Group (IV) Rats intraperitoneally injected with iron dextran (200 mg/kg/day every 3 days)+Echinacea (200mg/kg/day) orally administered for 4 weeks. Groups (V) Rats intraperitoneally injected with iron dextran (200 mg/kg/day every 3 days) and an oil solution of vitamin E (200mg/kg/day) orally administered for 4 weeks. Twenty-four hours following the treatment duration; the animals were euthanized, sacrificed and blood was drawn from the carotid artery in the neck of each male rat to be utilized for the estimation of serum Ferritin, and Hepcidin; liver tissue homogenate for malondialdehyde, superoxide dismutase2, and glutathione biomarkers estimation and liver histopathological examination; spleen tissue homogenate utilized to estimate Nuclear factor erythroid 2- related factor 2 and Caspase-3 protein expression. Echinacea Purpura in 200mg showed significant elevation (p<0.05) in the serum hepcidin and antioxidant superoxide dismutase2, glutathione, and Nuclear factor erythroid 2- related factor 2 protein expression levels; with a significant reduction in Ferritin and Malondialdehyde levels and a non-significant elevation in Caspase-3 level.
Assessment of the Efficacy of Adhering to the Ketogenic Diet on Adipokines (Betatrophin, Endotrophin, and Meteorin-Like Protein) in Obese Women with Polycystic Ovary Syndrome
Obesity increases the detrimental effects on both reproductive and metabolic indicators of polycystic ovarian syndrome (PCOS). The ketogenic diet affects the outcomes of reproductive and metabolic characteristics in PCOS women. Adipose tissue is recognized as a novel gland by releasing diverse peptides called adipokines, like betatrophin, endorphin, and meteorite-like proteins. Although the ketogenic diet's impact on many adipokines in various diseases was examined, its effects on the adipokines level in PCOS have not yet been studied. Therefore, our paper attempts to investigate how the ketogenic diet affects the adipokines level in obese PCOS women. Because seventy obese women with PCOS did not follow our randomized clinical trial design, they were excluded, and only 50 obese women with PCOS completed and concluded the study. Adipokines (betatrophin, endotrophin, and meteorin-like protein) level was measured for all obese PCOS before and after adhering to 3 and 6 months of the ketogenic diet. From the baseline (before adhering to the ketogenic diet), betatrophin was significantly reduced by 15% and 27% when obese PCOS women adhered to 3 and 6 months of the ketogenic diet, respectively. Furthermore, endotrophin was significantly reduced by 19% and 34% when obese PCOS women adhered to 3 and 6 months of the ketogenic diet, respectively. Conversely, meteorin-like protein significantly surged by 10% and 19% when obese PCOS women adhered to 3 and 6 months of the ketogenic diet, respectively. Our findings suggested that the ketogenic diet and its advantageous impacts can serve as supplementary management to control PCOS complications.
Adipokines, Betatrophin, Endotrophin, Ketogenic Diet, Meteorin-Like Protein, Polycystic Ovary Syndrome
The reproductive, metabolic, and adipokines characteristics are improved when obese women with polycystic ovary syndrome adhering to the ketogenic diet.
Synthesis, Antimicrobial, Biocompatibility, Toxicity, and Osteogenic Properties of Nanofibrous Gelatin Scaffold Containing Meropenem/Vancomycin-Mesoporous Silica Nanoparticles (Mrp/Van-MSNPs)
Electrospinning scaffolds composed of antibiotics and natural polymers can be helpful in the simultaneous suppression of infectious procedures and inducing tissue healing in the treatment of bone infections. The present study was performed to prepare and determine antimicrobial effects, biocompatibility, and osteogenic effects of gelatin meropenem/vancomycin -mesoporous silica nanoparticles (Mrp/Van-MSNPs) prepared using an electrospinning procedure. The scaffolds were investigated for physicochemical features, antimicrobial, biocompatibility, and osteogenic properties. The scaffolds showed applicable mechanical features, slow drug release patterns, and showed antimicrobial effects for 21 days. Gelatin-Mrp/Van-MSNPs showed higher antimicrobial and bacterial adhesive effects than gelatin and gelatin-Mrp/Van. All prepared scaffolds exhibited in vitro favorable biocompatibility. Gelatin-Mrp/Van-MSNPs significantly induced the MSCs' attachment, viability, and proliferation. It also significantly triggered the alkaline phosphatase (ALP) activity and induced the expression of osteogenic genes in both the early and late stages of differentiation. Therefore, the gelatin scaffolds with Mrp/Van-MSNPs can be considered for treating osteomyelitis. The addition of MSNPs and antimicrobial drugs in gelatin was not significantly associated with unfavorable effects on gelatin properties. The MSNPs led to improved antimicrobial, biocompatibility, and increasing cellular proliferation, and induced osteogenesis properties of gelatin.
Gelatin, meropenem, mesoporous silica nanoparticles, osteomyelitis, vancomycin.
Nanofibrous Gelatin Scaffold Containing Mrp/Van-MSNPs
Phytochemical Screening and Potential Cytotoxic Activity of Iraqi Corchorus olitorius Leaves Ethyl acetate Extract against The Breast and The Esophageal Cancer Cell Lines
The Corchorus olitorius leaves, a popular 'healthier' meal in Iraq , provided cytotoxic effects against different cell lines. The main purpose of the research work was to assess the phytochemical composition and the cytotoxicity of the Corchorus olitorius leaf ethyl acetate extract. The Iraqi Corchorus olitorius leaves ethyl acetate extract was made and fractionated using the hot continuous soxhlet device technique.Following this, a number of general and specialized tests were used to qualitatively screen for the different phytochemical constitutions found within the plant extract. then the human Iraqi breast (AMJ13) and the esophagus (SKGT-4) were subjected to various ethyl acetate extract concentrations (31.2, 62.5 , 125 , 250, 500 and 1000 μg/ml) in order to perform The MTT assay, is also known as 3-(4,5 dimthylthiazol-2-yl)-2,5-dipheyltetrazolium bromide and the viability of the cell was subsequently evaluated 72 hours after the treatment .The Iraqi Corchorus olitorius leaf ethyl acetate extract exhibited cytotoxic activity against the AMJ 13 and SKGT-4 cell lines. It produced a dose-dependent action. For the AMJ13 and SKGT-4 cell lines, the values of the inhibitory concentrations at half- maximum (IC 50) were 139.5 µg / ml and 100.1 µg / ml, respectively. So from the results of the study conclude that the Iraqi Corchorus olitorius leaves ethyl acetate extract exhibited cytotoxic activity and decreased the viability of Iraqi human breast and esophageal cancer cell line. So that further research regarding this topic is required.
Keywords: Breast cancer; Iraqi Corchorus olitorius; and Phenolic compounds .
Keywords: Breast cancer; Iraqi Corchorus olitorius; Esophageal cancer; Flavonoids; Phenolic compounds.
Knowledge of medical cannabis use, cannabis in food, and health literacy among late-adolescent students in a Thai province
Cannabis is the most widely used illicit drug globally, with an increasing use for both medicinal and non-medical purposes. Despite evolving policies and regulations, knowledge gaps persist among the youth, particularly regarding cannabis use, its integration into food products, and associated health risks. Many adolescents rely on unverified sources such as social media and peer networks for cannabis-related information, thereby increasing the risk of misinformation and unsafe consumption. This cross-sectional descriptive study assessed knowledge levels with respect to medical cannabis use, cannabis in food, and health literacy among late adolescent students in educational institutions. Additionally, it examined factors influencing knowledge, experience, and willingness to try cannabis while exploring opinions on medical cannabis use and cannabis in food. Data were collected from 252 students aged 15 - 18 years, using self-administered questionnaires. Descriptive statistics were used to analyze participant characteristics, while the chi-square test was applied to assess relationships between demographic factors, knowledge, and health literacy. The Decision Tree method (CART Algorithm) identified key determinants, classified participants based on significant factors, and predicted cannabis use and abstinence. The findings revealed that 49.2% of the participants had low cannabis-related knowledge, whereas 62.3% demonstrated moderate health literacy. Gender and field of study significantly influenced knowledge and health literacy. Most of the participants acknowledged the benefits and risks of cannabis use. These results highlight the need for targeted educational interventions to enhance cannabis-related knowledge and health literacy among late adolescents, considering their unique contexts and experiences.
The Effectiveness of Topical Nanohydrogel Pegagan Leaf Extract in Healing of Excision Wounds in Hyperglycemic Wistar Rats
Individuals with diabetes are susceptible to complications from diabetic foot ulcers, making it crucial to explore natural product-based dosage forms as alternative treatments for diabetic wound healing. One such natural product is the Centella asiatica (L.) plant, known to contain asiatic acid compounds that promote wound healing. However, these compounds exhibit low bioavailability. This study aims to evaluate the wound healing effectiveness of a topical nanohydrogel of C. asiatica leaf extract in hyperglycemic rats. C. asiatica leaves were extracted with 96% ethanol for 72 hours and formulated into a nanohydrogel. The diabetes was induced with a single dose of nicotinamide 230 mg/kgBW 15 minutes before the induction of streptozotocin 65 mg/kgBW intraperitoneally. Two excision wounds on the back of the rat with a diameter of 6 mm. Treatment was carried out for 14 days and macroscopic observations. At the end of the study, histopathological examination was performed on skin samples and wound healing percentages were analyzed using One-way ANOVA. Molecular docking studies were carried out on the target receptors S. aureus, mitogen-activated protein kinase 3 (MAPK3), Nuclear Factor-κB (NF-κB), and the IL-6/IL-6Rα/IL-6Rβ complex. Formula 1 nanoemulsion matrix is an optimum matrix with a particle size of 20.3 ± 0.3 nm, PI 0.414 ± 0.203, zeta potential -31.0 ± 0.7, percent transmittance 89.507 ± 0.0, and particle size <50nm, as shown by TEM. Nanohydrogel 1% significantly accelerated diabetic wound healing compared to the negative control (p<0.05). Histological examination revealed that wounds treated with 1% nanohydrogel had a moderate collagen composition and were rich in macrophages, which are beneficial in wound healing. Asiatic acid has an affinity level of -8.4 kcal/mol (S. aureus), -8.3 kcal/mol (MAPK3), -6.9 kcal/mol (NF-κB), and -8.5 kcal/mol (IL-6/IL-6Rα/IL-6Rβ complex). Nanohydrogel 1% is biocompatible and accelerates wound healing in hyperglycemic rats.