4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic

The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N^’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to  physical, chemical characterization, spectral characterization (IR, ¹H NMR, ¹³C NMR and Mass spectra),hydro

Calendula officinalis L. (Asteraceae) known as marigold is known to have several pharmacological activities and used for the treatment of several diseases as measles, jaundice, constipation and several inflammations. Marigold flowers contain several chemical constituents mainly flavonoids, triterpenoids and essential oil. In this study marigold flowers cultivated in Iraq had been investigated for its flavonoids content. The study revealed the presence of quercetin and kaempferol glycosides and the absence of myricetin glycosides. The flowers were extracted with ethanol 70% fractionated with different solvent and the flavonoids were isolated by preparative HPLC. The isolated flavonoids were identified by measuring melting points, UV, IR,

Lignans are natural products widely distributed in the plant kingdom. They are composed of two β-β-linked phenylpropane (shikimate-derived biogenetic subunits). Although the backbone of lignans is composed of phenylpropane units, there is enormous diversity in the structure of lignans leading to different classes of lignans, such as γ-butyrolactone derivatives, eg. Hymatairesinol, bicyclooctadiene derivatives, e.g. pinoresinol, tetrahydrofuran derivatives e.g.lariciresinol, di-arylbutandiol derivatives, e.g. secoisolariciresinol. Introduction of a further carbon –carbon linkage leads to a class of lignans collectively known as cyclolignans such as tetrahydro-naphthalene derivatives, for example podophyllotoxin. Lignans ha

There is a continuous and massive need for newer cephalosporins that should have resistance against β-lactamases and can be used orally. An approach of using cephalexin, as a well-studied and potent antibacterial compound is considered to prepare new designed derivatives.  These derivatives include the incorporation of amino acid moiety linked through an amide bond with the α-amino group of cephalexin. Certain aliphatic amino acids were used, such as glycine, alanine, valine and proline. The chemical structures of these derivatives were confirmed by IR spectroscopy and elemental analyses. All the synthesized compounds were subjected for preliminary evaluation of antimicrobial activity using well diffusion method, against certa

To assess the total hip replacement patients’ knowledge of home – care regarding pain management, medication therapy, wound care, mobility limitation and complications may occur in the post hip replacement surgery, and to assess relationship between some variables such as, age level of education, sex & marital status with home- care knowledge. A descriptive study was used to assess the hip-replacement patient home-knowledge, a purposive sampling of (60) hip-replaced –patients were selected from Gazy Alhariri Hospital  (central of surgical profession ) and Alwasity Hospital ( plastic surgery) , the questionnaire  obtains two parts , part one, which included socio-demographical characteristics of the samp

Therapeutic contact lenses TCLs is an approach used to enhance corneal residence time and reduce frequent instillation, which is a problem with eye drops.  The problem with CLs is loading of hydrophobic drugs. In this research the CLs were prepared with molecular imprinting MI to enhance the loading of itraconazole, which is used as antifungal drug for fungal keratitis. CLs using different  concentration of hydroxyethyl methacrylate HEMA and methacrylic acid MAA were prepared with and without MI using PEGDA (25 μL) and AIBN (37 mg) as crosslinker and initiator respectively. All the prepared CLs were clear and have good folding endurance. MICLs had significantly higher drug loading compared to conventional CLs. The release of i

Asthma is a chronic in?ammatory respiratory disease associated with the changes of asthmatic airway structural that result from interact remodeling and in?ammatory processes lead to obstruction of airway. Guggulsterone (GS) is a bioactive compound and plant steroid present in  guggul gum of Commiphora wightii, which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-inflammatory activity of gugglsterone in improvement of asthma. Forty eight healthy albino male rats divided to six groups, Group I: Control group (distal water), Group II: Positive control group (distal water) with sensitization, Group III: Guggulsterone (25 mg/kg/day) with sens

The treatment of migraine headache targets the neurovascular mechanism and involves the use of serotonin receptor antagonists. Some of these drugs are used for the treatment of acute attacks; while others are effective as prophylactic measures to decrease the duration and frequency of attacks. Pizotifen, a 5-HT_A antagonist, is one of the prophylactic drugs for which the clinical use resulted in low outcomes in reducing migraine symptoms. Melatonin, a serotonin derived neurohormone, was reported to exert many functions like sleep induction, anti-inflammatory, neurovascular regulation, cytoprotection and modulation of neurotransmitter release.  In the view of the involvement of serotonin in the pathophysiology of migraine a

Abstract 

    Oxidative stress has a significant impact on the etiology of type 1 diabetes mellitus (T1DM). However, associations of adipokines with oxidative stress biomarkers have yet to be investigated. Therefore, the present study aimed to investigate the estimation of serum apelin, chemerin, and omentin levels in induced TIDM and their correlations with oxidative stress markers. The study included sixty male albino rats divided into two groups. The first group (n = 30) was diabetic (TIDM induced with an intraperitoneal injection of 40mg/kg STZ). The non-diabetic control group was the second (n: 30). The enzyme-linked immunosorbent (ELISA) test was used to quantify the serum levels of apel

This study concerned with phytochemical investigation and methods of extraction and separation of active constituents from Valeriana officinalis plant cultivated in Iraq. Due to the large number of active constituents in Valeriana officinalis, it was necessary to make analytical study of its constituents to determine the chemical nature of these constituents and then determine the main classes (terpenes and iridoids) using chemical reagents specific for each class. Different organic solvents like ethanol (70%) used in soxhlet apparatus and hexane, ethyl acetate and methanol were used separately to extract the main active constituents by maceration. Through comparison between these solvents using thin layer chromatograph

Anaemia is a crucial issue among cancer patients and need to be treated properly. High incidence of anaemia in patients with cancer have been associated with several physiological manifestations, leading to decreased quality of life (QOL).

The current study aimed to assess the severity of anaemia, evaluate the current treatment guideline of anaemia, and to determine the association between the level of anaemia and its treatment on quality of life of breast cancer patients in Malaysia. This prospective study conducted among breast cancer patients in multicancer centers in Malaysia including three follow ups after receiving their chemotherapy. Clinical data were collected from their medical records and at each follow up, they asked

Rituximab (RTX) is one of the biological medications that has been used in the treatment of autoimmune diseases and cancer. However, a high percentage of patients may experience resistance to RTX therapy. The study aims to investigate the potential association of serum levels of the complement decay accelerating factor (DAF), as well as the pro-inflammatory cytokines, tumour necrosis factor-alpha (TNF-α) and interleukin-1 Beta (IL-1β); with response to RTX treatment in rheumatoid arthritis patients. A cross-sectional study was conducted under specialized physician supervision in the Specialized Center of Rheumatology at Baghdad Teaching Hospital in Baghdad/Iraq. Ninety adult patients who were already d

Plumbago auriculata is a perennial plant belong to Plumbaginaceae family. It is an endemic genus of 18 species in South Africa. All plant parts have many phytochemical compounds appearing several pharmacological activities. The study was aimed to isolate and identify of the bioactive phenolic compounds (luteolin and ferulic acid) from Plumbago auriculata cultivated in Iraq by various chromatographic and spectroscopic techniques. The plant materials were defatted with n-hexane solvent by maceration for 48hr, and extracted by soxhlet apparatus using 85% methanol solvent, then fractionated with the solvents of petroleum ether, chloroform, and ethyl acetate. High performance liquid chromatography (HPLC) was used to identify

Nuclear factor erythroid-2-related factor-2 (NFE2L-2) is one important endogenous anti -oxidative stress signal pathway. Single nucleotide polymorphism (SNP) or genetic variants of NFE2L-2 may be accountable for the genesis of diabetic retinopathy. Glyoxalase-1 (Glo-1) is the rate-limiting enzyme in the detoxification of methylglyoxal (MG) into D-lactate. The activity of GLO1 is regulated by the transcription factor NFE2L2.The goal of this study is to ascertain whether there is an association between the rs6706649 of NFE2L2 gene variant with serum GLO-1 levels in a group of Iraqi diabetic patients diagnosed with diabetic retinopathy (DR). This study included ninety patients diagnosed wi

Chronic kidney disease patients undergoing hemodialysis are frequently suffering from uremic pruritus, which can be quite uncomfortable. Uremic pruritus affects over 40% of hemodialysis patients. Bile acids have been implicated in the pathogenesis of pruritus; especially in conditions associated with cholestasis. The purpose of the study is to investigate the serum levels of total bile acids in chronic kidney disease patients on hemodialysis, with and without uremic pruritus. Ninety adults, chronic kidney disease patients who were on chronic hemodialysis at the hemodialysis unit at Al-Fallujah Teaching Hospital in Fallujah City, Iraq, were involved. Patients were grouped equally in two groups; according to the presence or absence of prur

The carboxylic acid group of quinolones was modified; so, we designed new quinolones derivatives with different antioxidants using Ligand Designer from Glide (Schrodinger LLC). The cap group and the linker were optimized through trying various aliphatic and aromatic residues. A new synthesized derivatives (IIa-Vb) were synthesized by esterification of (ciprofloxacin, gatifloxacin, nalidixic acid and norfloxacin) with antioxidants (a: vanillin, b: sesamol) through a glycol linker. Based on spectral data (NMR, ATR-FTIR) their structure were confirmed. The synthesized compounds were screened for their Pharmacological activities. In vivo, the anti-inflammatory effect of (IIa-Vb) compounds was estimated using a rat paw edema model and showed

Clozapine (CLZ) is a tricyclic dibenzodiazepine, classified as an atypical antipsychotic agent. It belongs to the Biopharmaceutical Classification System (BCS) class II drug (High Permeability, Low Solubility), with a high first-pass effect. The current study used a technique called the solvent-antisolvent method to prepare a nanosuspension of clozapine with different stabilizers and solvents in an effort to increase the drug's solubility and dissolution. (Soluplus®, HPMC E15, PVA, Poloxamer 188, Poloxamer 407, PVP K30, PVP K90, and Tween 40) were used to produce the formula. Evaluations were done on particle size, PDI, zeta potential, and in vitro dissolution investigations. According to the data, all developed clozapine formulations h

Abstract 

              The condition known as gestational diabetes mellitus (GDM) describes as an intolerance to glucoseThat first occur or progresses during pregnancy is the most common metabolic illness, and impacts up to25% of pregnant women.  It has been demonstrated that omentin-1, which originates from both human placental and adipose tissue can serve as an insulin resistance mediator. It was initially identified as a secretory factor specific to visceral fat and showed that recombinant omentin-1 administration increased insulin-stimulated glucose transport in vitro which may increase insulin sensitivity, both glucose and insulin can down regulate omentin-1 which reduces levels in o

Oral anticancer medicines are frequently administered to patients with cancer. Regrettably, many medications are administered without appropriate recommendations about handling practices. This study aims to assess the handling, storage, and disposal practices of oral anticancer medication among cancer patients at home. A cross-sectional study was conducted from December 2023 to February 2024 on adult cancer patients who were administered oral anticancer at the Hematology and Bone Marrow Transplant Center in Iraq using pre-validated questionnaire. In total, 300 patients were interviewed, with (57%) being male and approximately (47%) falling within the age range of 40 to 60 years. Regarding handling practices, most patients (96.7%) never w

          Murraya paniculata, sometimes known as orange Jessamine, is a significant decorative plant found in tropical and subtropical regions. It belongs to the Rutaceae family. The distribution of this species extends from South Asia to Australia. This plant possesses a multitude of applications in traditional medicine for the treatment of several ailments. The plant demonstrates an extensive array of pharmacological actions, involving antinociceptive, antioxidant, anti-diabetic, antibacterial, and analgesic effects. This study aims to conduct Preliminary Phytochemical Screening, Phytochemical investigation of some bioactive constituents, and isolation of new compounds from Iraqi Murray

Febuxostat (FEB) is a potent, non-purine-selective inhibitor of xanthine oxidoreductase used to manage gout. Gout is a type of arthritis that occurs due to the accumulation of uric acid crystals in the joints, leading to inflammation and pain. According to the Biopharmaceutical Classification System (BCS), FEB was classified under class II drugs. The low dissolution rate of the drug determines its bioavailability at approximately 49%. Drug nanosizing, such as Nanosuspensions (NS), represents an exciting and potentially beneficial method to improve the bioavailability of hydrophobic drugs. This study aimed to prepare and characterize FEB NS to increase the dissolution rate, which can enhance its oral bioavailability. Using solvent/anti-so

Obesity by multiple mechanisms can contribute not only to the development of type 2 diabetes mellitus (T2DM) but also by further worsening the patient’s condition. One of these mechanisms may include the disturbances of neuropeptide Y (NPY) serum level which is one of the most powerful orexigenic peptides, that’s produced in large amounts in the hypothalamus, as well as in peripheral adipose tissue. The present study aimed to assess the impact of obesity in type 2 diabetic patients on serum neuropeptide-Y level and its impact on fasting serum glucose and insulin levels. Eighty-seven T2DM patients attending the clinic of The National Center of Diabetes Treatment & Research/Baghdad, were included in this study, had been categorized

Rheumatoid arthritis is a lifelong autoimmune arthritic disorder that mostly impacts the small joints, although it can also affect the larger joints. Infliximab is a chimeric monoclonal IgG antibody that specifically targets tumor necrosis factor, a crucial material associated with pathogenic processes. Remicade is an original medication of infliximab. Monitoring the trough level is essential for managing disease activity, while C-reactive protein (CRP) and Erythrocyte Sedimentation Rate (ESR) are utilized to detect inflammation and anticipate the drug's effectiveness. The study was designed to assess the impact of Remicade trough level on both disease activity and inflammatory biomarkers. A cross-sectional, observational research was ca

Histone deacetylases (HDACs) are a class of proteins that responsible of the hydrolysis of N-acetyl lysine residues in histones as well as non-histone protein substrates. This phenomenon may provide an explanation for the involvement of these enzymes in a wide range of clinical situations, encompassing cancer, metabolic, cardiovascular problems, and neurological diseases. Most of HDAC inhibitors are often used in clinical settings consist of a hydroxamate group (ZBG) that binds to zinc ion inside the active site. The poor selectivity and pharmacokinetic characteristics of numerous medicines belonging to the hydroxamates group have prompted the exploration of non-hydroximic ZBG HDAC inhibitors with a potential selectivity and potency prof

Hyperglycemia and hyperinsulinemia, two common metabolic disorders associated with type 2 diabetes mellitus, are the main causes of metabolic abnormalities that result in a wide range of complications, such as cardiac dysfunction, nephropathy, neuropathy, and retinopathy. Substance-P is an 11-amino acid neuropeptide that is highly conserved and secreted by sensory nerve endings as well as different types of non-neural cells. It was believed that substance P would reduce inflammation triggered on by diabetes, interrupting the development of complications associated with this disease. The current study aims to investigate whether serum levels of substance P are associated with glycemic measures &/or lipids profile in patients with type

Paclitaxel (Taxol) belongs to the initial taxane category and is employed for treating diverse types of cancers, including ovarian, lung, and breast cancers. Paclitaxel is associated with the highest prevalence of peripheral neuropathy. The detection of PIPN may necessitate a reduction in dosage or discontinuation of treatment, which can have consequences for cancer care. Activation of AT2R has shown neuroprotective effects in different rodent models. this study aims to assess the potential impact of candesartan in mitigating the deleterious effect on human neuron cells. The methods involved in Immunocytochemistry to characterize the neuron cells depend on the expression of the B tubulin III protein. WST-8 test was used on human neuron c

Olmesartan medoxomil (OLM) is a selective angiotensin II antagonist that effectively lowers blood pressure. It has a poor rate of absorption when taken orally, a maximum bioavailability of about 26%, and limited solubility in water. OLM is therefore categorized as class II in the Biopharmaceuticals Classification System (BCS), suggesting that it has high permeability and low solubility. By generating nanomicelles, this work attempts to increase the aqueous solubility and dissolution rate of OLM. Mixed polymeric nanomicelles made up of soluplus (SLP) with tween 80 (TWN80) and SLP with d-α tocopheryl polyethylene glycol 1000 succinate (TPGS), had been prepared in different gravimetric ratios. The nanomicelles holding OLM were developed us

The isatin molecule is present in many natural substances, like plants and animals, and it is utilized to prepare compounds with various biological activities. A series of Schiff and Mannich bases derived from isatin were synthesized in this research. First, acetylenic Mannich bases (IIa-e) were prepared by a reaction of isatin with propargyl bromide and different secondary amines (morpholine, piperidine, pyrrolidine, dimethylamine, and diphenylamine) separately, and cuprous chloride (CuCl) was used as a catalyst. Second, these Mannich bases were treated with 2-aminothiazole to obtain the desired final compounds (AM1-AM5). The synthesized compounds were characterized on the basis of their spectral (FT-IR

Abstract

Olanzapine (OLZ) is classified a typical antipsychotic drug, which utilized for treatment of schizophrenia. It possesses poor water solubility and high membrane permeability, so, OLZ classified as class II according to biopharmaceutical classification system (BCS). Its oral bioavailability is (60%) due to poor solubility and extensive first-pass hepatic metabolism. Hence, the objective of this study was to prepare and evaluate the nanoparticles of OLZ for transdermal delivery. Nanoprecipitation method was employed to formulate the nanoparticles, where methanol utilized to dissolve the drug and form organic phase, which was added to an aqueous phase that consist of deionized water and stabilizer at speed