Al Mustansiriyah Journal of Pharmaceutical Sciences

quality of life, metastatic colorectal cancer, EORTC QLQ-C30, bevacizumab, Global- health status

In this review, we examined studies through 2023 with particular attention to the cases listed below. by investigate the potential of acyloxyalkyl carbamates for the amine-containing drug in order to overcome problems associated with medication transport and pharmacological activity of these drugs by improving drug delivery and penetration for amine drugs.

This review explores how the esterase enzymes can generate effective parent drugs to give pharmacological action.

The findings focus on two main concepts. The first is activating enzymes and targeting their effects. The second concept focuses on creating pro-moieties that can achieve the intended outcome efficiently and how selecting the appropriate pro-moieties is crucial for creating stable compounds that do not produce any toxic byproducts. The review highlights the importance of enhancing drug solubility and permeability, particularly for amino-group prodrugs.

Polycystic ovary syndrome (PCOS) is the most prevalent disorder, establishing the single most common endocrine-metabolic disorder in women of reproductive age. Currently there are four recognized phenotypes of PCOS: 1) hyperandrogenism + oligo-anovulation + polycystic ovarian morphology; 2) hyperandrogenism + oligo-anovulation; 3) hyperandrogenism + polycystic ovarian morphology; and 4) oligo-anovulation + polycystic ovarian morphology, each having different long-term effects and metabolic consequences.

The histology of ovarian PCOS patients demonstrates that PCOS ovaries showed multiple ovarian cysts with a lack of corpus luteum, growing follicles, oocytes, granulosa, and theca cell layers. Chromium picolinate Chromium picolinate is a salt of the trace metallic element chromium (Cr). It is effectively treating hyperinsulinemia and hyperlipidemia.

This study aimed to investigate the effects of different doses of trichromium picolinate on the ovary histopathologic changes.

Methods: Forty-eight female albino rats were divided into six groups, with eight animals in each group. All groups were given testosterone enanthate 100 mg/kg/day by subcutaneous injection for 28 days, while the control group was given sesame oil 0.5 ml for 28 days. In the treatment stage, trichromium picolinate (1 mg, 2 mg, and 4 mg/kg/day) was given to groups III, IV, and V, respectively, for 42 days, and cyproterone acetate was given to group VI for comparison. At the same time, control and induction groups were treated with distilled water 0.5 mL orally for 42 days. In the current study, ovary histopathological changes were examined by hematoxylin and eosin staining.

Results: The control group showed apparently normal histology of ovarian rat’s tissue with all types of follicles at different stages of maturation. Furthermore, the oocyte was intact, surrounded by granulosa and visible theca cell layers with numbers of corpus luteum. Conversely, the induction group confirmed PCOS in ovarian rat’s tissue, which exhibited numerous cystic follicles and atretic follicles, granulosa, and theca layer hyperplasia with a decrease in the number of developing follicles and the absence of corpus luteum. Histopathological examination of the treatment groups with different doses of trichromium picolinate demonstrated dose-dependent manner. Treatment with trichromium picolinate (1 mg/kg) mildly improved the histopathological changes of the ovary. When the dose was increased to 2 mg/kg, the score improved additionally, with the ovarian tissue resolving at 4 mg/kg of trichromium picolinate as in the cyproterone acetate group.

Conclusions: Trichromium picolinate can improve histopathological changes in the ovarian tissue of female rats.

Vasculitis is an inflammation in the blood vessel wall, with variation in severity and the system affected. Vasculitis pathogenesis is caused by three possible mechanisms, including autoantibodies anti-neutrophil cytoplasmic antibodies, activation of T lymphocyte cells, and immune complexes.Various pathogens stimulate innate and adaptive immune systems, modulating the expression of pro-inflammatory cells, cytokines, and the complement system, that have a role in vasculitis progression. Ivermectin is an anti-parasitic drug, effective in treating parasitic infections. Thirty-three male albino rats were used for the experiment and divided into five groups. The disease was induced in all groups except group A (control), rats received the vehicles used in dissolving drug and chemicals. Group B (induction group) received Ovalbumin and Lipopolysaccharide. Group C, group D, and group E (Ivermectin groups) received 0.5mg/kg, 1 mg/kg and 1.5 mg/kg of Ivermectin, respectively, for seven days. All doses were injected by intraperitoneal route. Results of histopathological evaluation of lung sections of Ivermectin groups show a decrease in the inflammation severity, alveolar destruction, and vascular congestion and dilatation, with the absence of: hemorrhage, thrombi, and fibrinoid wall necrosis in comparison to the disease group. Therefore, the Ivermectin drug might have a protective effect against vasculitis.

Background: liver-related side effects can occur with numerous medications, with effects ranging from a mild effect to death. While statins in general, especially atorvastatin, are not usually associated with liver damage, reports recently have been suggesting otherwise.

Objective: this study investigates the effects of various doses of hesperidin against hepatotoxicity caused by atorvastatin in rat model.

Method: Thirty apparently healthy male Wister rats were randomly and equally divided into five groups, each group containing six rats, each group was subjected to certain dose of medication for the entire time of the experiment that lasted for twenty days.

Results: atorvastatin caused numerous liver related toxicity while hesperidin demonstrated dose related hepatoprotective effects.

Conclusion: the characteristic protective features of hesperidin, most likely as an antioxidant, is able to provide protection against atorvastatin hepatotoxicity, however this protective effect is directly affected by the right dose.

Abstract:Chronic kidney disease occurs when a disease or condition impairs kidney function, causing kidney damage to worsen over several months or years. Anemia is an important complication of chronic kidney disease (CKD), with increasing prevalence in the more advanced stages of the disease. The etiology of anemia in CKD is multifactorial, and the key mechanisms involve relative deficiency of erythropoietin (EPO), iron deficiency and maldistribution, and shortened erythrocyte life span.

Objective: To determine the most effective method for inducing chronic kidney disease (CKD) with anemia in male rats by administering adenine and folic acid and comparing the outcomes of four different models.

First, folic acid was intraperitoneally injected into rats at a dose of 250mg/kg per week. Second, folic acid was also intraperitoneally injected into rats at a dose of 250mg/kg every 2 weeks. Third, adenine was intraperitoneally injected into rats at a dose of 250mg/kg/ per week. Finally, adenine was intraperitoneally injected into rats at a dose of 250mg/kg every 2 weeks.

Methods: Thirty male Wistar albino rats were divided into five groups, with n=6 in each group. Group I, the healthy control group, received a weekly intraperitoneal injection of normal saline for four weeks. Group II, the Adenine model group, received a weekly intraperitoneal injection of adenine at 250 mg/kg. Group III, also part of the adenine model group, received an intraperitoneal injection of adenine at a dose of 250 mg/kg every two weeks for four weeks. Group IV, the Folic acid model group, received a weekly intraperitoneal injection of folic acid at 250 mg/kg for four weeks. Lastly, Group V, also part of the folic acid model group, received an intraperitoneal injection of folic acid at 250 mg/kg every two weeks for four weeks. After a 28-day induction period, the rats were sedated and euthanized. Blood samples were obtained, and the serum was collected for further biomarker testing using ELISA kits.



Results: Upon comparing the rats' body weight at the start and end of the experiment, no group showed a statistically significant change. The dosage of folic acid per week was the most important factor in the increase of relative kidney weight, while there was a significant variation in relative kidney weight across the analyzed groups. After measuring kidney function tests (urea, creatinine), hematological parameters (hematocrit, ferritin), it was found that the folic acid model (250 mg/kg/wk, IP for 4 weeks) was significantly the best to induce renal anemia in male rats, it caused a critical increase in the levels of urea and creatinine, which indicates the occurrence of chronic kidney failure. The aforementioned model also caused a decrease in the hematocrit rate and a reduction in the level of ferritin in the blood, which gives the impression of renal anemia. The adenine model, in the same dose and duration, came second in ranking of the optimal induction model.

Conclusion: Compared to the other rat models, the folic acid model group (250 mg/Kg/wk) is more effective in producing anemia associated with chronic renal disease. Due to the observed alterations in many parameters including kidney function, oxidative stress markers, and inflammatory markers, the weekly dosage of folic acid demonstrated its superiority in the context of renal anemia. This will be useful in the future for discovering innovative drugs and understanding the renal anaemia process.

Background: Acne vulgaris is a widespread, long-term inflammatory skin disorder that commonly starts in adolescence. Hormonal influences are crucial in determining both the development and severity of the condition.

Aim: This study aims to evaluate the relationship between prolactin and total testosterone levels and the occurrence and severity of acne vulgaris.

Methods: The study included 119 Sudanese females diagnosed with acne vulgaris and 85 age-matched non-acne controls. Serum levels of total testosterone and prolactin were measured in both groups.

Results: Acne vulgaris predominantly affects individuals aged 20 to 25 years (70.5%). Patients with acne had a significantly higher mean testosterone level compared to the control group (patients: mean ± SD 64.0 ± 28.0 ng/dl; controls: 38.5 ± 15.2 ng/dl, P = 0.001). In contrast, there was no significant difference in mean prolactin levels between the two groups (patients: mean ± SD 15.6 ± 13.0 ng/dl; controls: 11.0 ± 5.2 ng/dl, P = 0.065). Prolactin levels were significantly associated with the severity of acne (P = 0.043), whereas testosterone levels were not (P = 0.403).
Conclusion: Total testosterone levels tend to be higher in individuals with acne vulgaris, whereas prolactin levels show no significant variation when compared to controls. However, acne severity appears to be more closely linked to prolactin levels than to testosterone.

Irritable bowel syndrome (IBS) is one of the most prevalent functional digestive disorders, diagnosis of patients might be difficult because IBS can be confused with the symptoms of other organic gastrointestinal disorders such as diarrhea, microscopic colitis, celiac and inflammatory bowel disease.

The primary clinical symptoms of IBS included changed bowel habits, pains, and recurrent abdominal discomfort. The pathogenesis of IBS is very complicated, there was several factors like environment, heritability, genetic, diet or intestinal inflammation, social learning, and disorders in the neuroendocrine system (NES) of the gut. The treatment must be tailored to each patient specific symptomatology because may be difficult management of the disease, patients should be avoiding some foods such as fermentable saccharides that increase osmotic pressure that provide substrate for bacterial fermentation, which results in the production of gas, distension of the large intestine with pain and discomfort in the abdomen. Many studies approved the effect of probiotics by improvements of abdominal distension and flatulence, as well as a reduction in the composite IBS symptom. Probiotics bind to the epithelial cells, inhibit pathogens, and improve intestinal barrier function, also increase stabilization of the colonic microbiota and reduce colonic fermentation.

Hepatotoxicity is considered a primary cause of mortality induced by anticonvulsant medicines such as carbamazepine, which produce inflammation and oxidative stress in the liver; this impact is mitigated by Pentoxifylline, which has an anti-inflammatory and antioxidant action.

This study aims to assess Pentoxifylline's protective effect on liver function enzymes and its possible role in minimizing structural changes and cellular death in hepatocytes during Carbamazepine-induced liver injury in a rat model. Forty rats were randomly assigned to five groups. Each group contained eight rats. Group 1 (Control): rats were given 10ml of distilled water per kg body weight. Group 2 (induction): rats administered Carbamazepine 50 mg/kg body weight. In the other groups, rats were given Pentoxifylline 100 mg/kg of body weight, 200 mg/kg of body weight, and 300 mg/kg of body weight one hour before being given Carbamazepine 50 mg/kg of body weight. Orally for 28 days. A serum was obtained to measure alkaline phosphatase and Bilirubin, and small portions of liver tissue were removed and preserved in 10% buffered formalin, which was then used for histological examination. The results demonstrate a significant (P<0.001) reduction in alkaline phosphatase and Bilirubin with Pentoxifylline groups. The findings revealed that Pentoxifylline protects hepatocytes from Carbamazepine-induced liver damage by improving liver function enzymes and decreasing histological alterations in hepatocytes.

In this study, four Schiff base derivatives (S1-S4) were designed, synthesized and tested for biological activity. The synthesized compounds were analysed and described based on their physical and chemical properties, as well as through the use of NMR and FTIR techniques. The molecular docking investigation demonstrated the potential biological action of these molecules. The results demonstrated that these compounds exhibit antibacterial, antifungal, and anticancer properties. Compound S1 and S2 exhibited antibacterial efficacy against Staphylococcus aureus and Escherichia coli. Compounds S3 and S4 exhibited fungicidal properties against Aspergillus niger and Chaladra corda. Compound S3 demonstrated significant anticancer efficacy against breast cancer, as confirmed by MTT tests.

Nanotechnology has been introduced in several health-related aspects, particularly in therapy. Delivery therapeutic agents using nanoliposomes have approved several improvements in their physiochemical properties, selectivity, potency, and general pharmacokinetics and pharmacodynamics.

Antibiotic resistance is a major threat to the healthcare system in therapeutic and economic aspects. Developing systems of nano-sized antibacterial agents delivered by nano-liposomes shows a promising solution that would increase the effectiveness, decrease the required therapeutic doses, and save the health economy. Various types of nanoliposomes were incorporated including the cationic, anionic, and neutrally charged molecules, this technology targeted G-negative, G-positive, fungal strains, and other pathogens. Nanoliposomes could overcome the dilemma of biofilm formation and enhance selective targeting of the antibiotic agent.

Background: A woman's ovarian reserve and fertility may be affected by the long-term use of hormonal contraception. Anti-Mullerian hormone levels, the best available measure of ovarian reserve, were reduced by hormonal contraceptives methods, and were much lower in the majority of hormonal contraceptive methods, although this suppression effect is reversible.

Objective : The aim is to investigate the association between different types of contraceptives and ovarian reserve, probably affect fertility by measuring ovarian reserve parameters (Anti-Mullerian hormone, follicle-stimulating hormone).

Methods: A total of 60 women were eligible for inclusion and were divided into two groups. Group 1 included 40 married women who had regularly used combined oral contraceptives (ethinyl estradiol 30 µg and 150 µg levonorgestrel) or medroxyprogesterone acetate injection for at least 6 months. 21 women used combined oral contraceptives, and 19 women used injectable form. Group 2 included 20 married women who didn't take any hormonal contraceptives. Both groups were investigated for serum anti-Mullerian and follicle-stimulating hormone levels on the third day of the menstrual cycle.

Results: Among women aged 26-30, the mean age was 30.8±3.3 years. There were statistically significant differences between cases and non-users regarding anti-mullerian hormone level (P-value=0.001), significantly lower level among women who were taking combined oral contraceptives compared to those who were receiving birth control injections (P-value =0.001) regarding the anti-mullerian hormone level. There were no significant differences between cases and non-users regarding follicle-stimulating hormone levels (P-value = 0.772).

Conclusion: Hormonal contraceptive methods, both oral and injectable, seem to reduce anti-mullerian hormone levels, but not follicle-stimulating hormone and anti-mullerian hormone levels were suppressed more by oral compared to injectable contraceptives. Further studies using ultrasound and other tests for example luteinizing hormone, sex hormones, and inhibin to check ovarian reserve changes during contraception.

Background: Rheumatoid arthritis is a chronic, damaging autoimmune disease identified by systemic inflammation; it initially impacts the joints. S100A8 is a calcium-binding protein and one of the S100 protein family, which is crucial for developing multiple inflammatory diseases, especially rheumatoid arthritis.

Objective: This study aims to estimate serum S100A8 levels in rheumatoid arthritis patients receiving infliximab therapy and its effect on disease activity.

Methods: A case-controlled study was conducted on 65 rheumatoid arthritis patients receiving infliximab infusion therapy and 25 healthy individuals as control. The enzyme-linked immunosorbent assay (ELISA) was applied to determine S100A8 levels. In addition, Clinical Disease Activity Index (CDAI) scores and erythrocyte sedimentation rate (ESR) were also assessed.

Results: The current study demonstrated that the levels of S100A8 in patients with rheumatoid arthritis were significantly higher than in healthy controls, with a p-value less than 0.0001. Also, it was useful for distinguishing individuals with rheumatoid arthritis from a healthy subject, with excellent Area Under the Curve (AUC) and very high sensitivity and specificity (95.38% and 100%, respectively). Furthermore, this study shows a weak positive correlation between S100A8 and the Clinical Disease Activity Index (CDAI) in rheumatoid arthritis patients (R = 0.087, p = 0.491).

Conclusion: This study concluded that, despite taking infliximab therapy, the levels of S100A8 remained higher in rheumatoid arthritis patients when compared with controls, indicating that it could be a marker for rheumatoid arthritis disease.

This study investigates the design, molecular docking, and ADME properties of thioimidazole-4-one derivatives as potential therapeutic agents targeting the A2A adenosine receptor for asthma treatment. Computational molecular docking was performed using the A2A receptor complexed with theophylline (PDB ID: 5MZJ), and the compounds were compared to theophylline to evaluate binding affinity. Docking results revealed that the synthesized compounds showed stronger binding affinities than theophylline, with several compounds (e.g., 5y and 3y) exhibiting superior PLP fitness scores. These compounds formed hydrogen bonds and hydrophobic interactions with key residues of the A2A receptor, such as ASN253, TYR271, and GLU169, suggesting their potential to modulate asthma-related mechanisms like airway constriction and inflammation. ADME analysis, conducted using the SwissADME server, indicated that compounds Y1–Y6 possessed favorable pharmacokinetic properties, including good gastrointestinal absorption, moderate bioavailability, and no P-glycoprotein interactions, making them suitable for oral administration. However, compounds Y7 and Y8 exhibited lower gastrointestinal absorption and increased polarity, suggesting the need for further structural optimization. The findings suggest that these thioimidazole-4-one derivatives are promising candidates for asthma therapy, with potential for further development based on their molecular docking results and ADME profiles.

Medicated lipsticks use active medicinal compounds in lipstick formulations to combine therapeutic advantages with cosmetic benefits such as hydrating, mending, and shielding the lips against infections, dryness, and chapping. A shed of light on the materials used, such as waxes, oils, and pigments.

Also, this review provided an overview of previous research that clarified the usage of various constituents in lipstick and the production methods. A focus on herbal and medicate lipsticks such as lipstick formulations of antifungal agents (e.g. ketoconazole), antiviral (e.g. acyclovir), sunscreens, vitamin D3, and moisturizers like vitamin E and lanolin. Lipstick’s effectiveness can be investigated through many studies, such as melting point, softening point, breaking point, thixotropy, the force of application, separability, pH meter, skin irritation, and stability. Additionally, metal contaminants are due to ingredients impurities and attention to the use of advanced analytical instruments to analyse the presence of lead and other metals in lipstick formulation based on their considerable impact on consumer health.