Journal of Advanced Pharmaceutical Technology & Research最新文献

Fatigue is a prevalent symptom experienced by individuals diagnosed with multiple sclerosis (MS), which greatly affects their daily activities and causes frustration and depression, thus affecting their lives and society. This can be prevented through the use of medicines such as L-carnitine and modafinil. The study aimed to examine the effect of L-carnitine and modafinil on fatigue and which one is better for MS patients. This was a clinical trial. This clinical trial was conducted in cooperation between Al-Kut University College and an MS consultant at Al-Zahraa Teaching Hospital in addition to the private neurological clinic from October 1, 2022, to March 15, 2023. Forty participants were split into two groups; both of which were almost identical characteristics regarding age, disease duration, and degree of fatigue. Group I (n = 20): relapsing-remitting MS patients with fatigue received modafinil. Group II (n = 20): relapsing-remitting MS patients with fatigue received L-carnitine. Fatigue was evaluated according to the Modified Fatigue Impact Scale (MFIS). The statistical work was done in SPSS (IBM Corp., Chicago, IL, USA, version 24). P values were calculated by the t-test. Significant data have P = 0.05. After 2 months of treatment, the results show a significant decrease in MFIS in both groups with a higher reduction in patients who use L-carnitine. Both modafinil and L-carnitine show a significant influence on fatigue in MS patients, and these effects are more in L-carnitine.

[This retracts the article on p. S117 in vol. 13, PMID: 36643137.].

A series of eight novels' 1,3-diazetidin-2-ones have been proposed to assess their potential activities. They are intended to examine antiproliferative effects through inhibition of epidermal growth factor receptor (EGFR) expression. These eight compounds strongly interact with the EGFR protein, responsible for the activity. As part of a present study, these compounds were docked to the crystal structure of the EGFR (Protein Data Bank code: 1 M17) to determine their binding affinity at the active site. Based on computer predictions, two compounds were demonstrated high scores of 80.80 and 85.89. After analyzing ADME properties, these compounds were found to have significant potential for binding. Consequently, the abilities of gefitinib, erlotinib, imatinib, and sorafenib were selected for comparison as controls. Computational methods were performed to predict the critical disposition of eight novels' 1,3-diazetidin-2-one derivatives to the EGFR. Moreover, a docking technique employing the Genetic Optimization for Ligand Docking program was conducted. Compounds 2 and 7 demonstrate a high docking peace-wise scoring function (PLP) fitness of 85.89 and 80.80, respectively. They fulfilled the Lipinski's rule, topological descriptors, and fingerprints of drug-like molecular structure keys. These compounds can be used as lead compounds to develop novel antiproliferative agents. The outcome of applying this study is novel series of 1,3-diazetidin-2-one compounds as new analogs were designed and evaluated for their antiproliferative activity with a higher potency profile and binding affinity within the active sites of EGFR.

[This retracts the article on p. S112 in vol. 13, PMID: 36643134.].

Lung cancer is the most common malignancy worldwide, with approximately 1.8 million new cases yearly. Cytotoxic drugs are frequently used in cancer treatment. Even though the medicine enhances patients' quality of life, several drawbacks diminish its efficacy. Drug resistance and many disadvantages associated with chemotherapeutic drug side effects continue to be significant factors limiting the efficiency of cancer treatment. This necessitates developing new effective strategies that target tumors with minimal adverse effects. This research aims to overcome these issues by synthesizing a new series of compounds with an isoxazole ring attached by Schiff bases and azo bonds based on molecular docking with the (Genetic Optimization of Ligand Docking) program and estimating the pharmacokinetic properties with the Swiss ADME. The greatest-fitting compounds were then manufactured and verified by spectral analysis (FT-IR, ¹H NMR, and ¹³C NMR), in vitro MTT assay for assessment of antiproliferative activities against A549 lung cancer cell lines showed that compounds 5a and 5b had an inhibitory concentration half-maximal inhibitory concentration (IC₅₀) (17.34 and 18.32 μM), respectively, which was significantly lower than the inhibitory concentration of erlotinib (IC₅₀ = 25.06 μM).

In diabetes, microvascular damage often targets the kidney, making them the most crucial organ affected. Due to the disease itself or other accompanying health issues such as hypertension and nephron loss due to aging, a significant number of patients end up with kidney disease. The current research aimed to analyze the concentration of cytokines in the serum (Interleukin [IL]-18, IL-17a and transforming growth factor-beta (TGF-β) in Iraqi adult patients with diabetic kidney disease (DKD). The current investigation was carried out in Tikrit Teaching Hospital/Salahaddin governorate for the time from October 2022 to January 2023. Sixty blood specimens were obtained from patients with DKD. Serum levels of IL-18, IL-17a, and TGF-β markers in the samples were subjected to measurement by enzyme-linked immunosorbent assay. Results of the present study showed significant differences (P < 0.05) among different age categories of clinical populations with 51-60 and >60 years scoring highest (28% and 33%), whereas 21-30 and 31-40 years scored (8.3% and 13.3%). The concentration of IL-18, IL-17a, and TGF-β markers was high in patients (200.30 ± 59.50, 102.13 ± 50.82, and 57.15 ± 18.90) than in healthy individuals (104.50 ± 31.01, 42.90 ± 10.55, and 31.90 ± 8.83). Based on the Pearson's correlation results, IL-17a had a significant negative correlation with TGF-β (r = -0.270* Sig. =0.037). Moreover, the receiver operating characteristic curve showed the IL-18, IL-17a, and TGF-β markers scored the highest sensitivity (98%, 96%, and 87%) and specificity (94%, 97%, and 80%), respectively, in screening patients with DKD. Based on the analysis, it could be inferred that disease intensity generally tends to worsen with an increase in age. IL-18, IL-17a, and TGF-β are good prognostic markers in screening patients with DKD. These cytokines present a promising target for therapeutic interventions in DKD therapy.

The cause of the worldwide coronavirus disease-2019 (COVID-19) pandemic is the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). It is known to employ the same entry portal as SARS-CoV, which is the type 1 transmembrane angiotensin-converting enzyme 2 (ACE2) receptor. The receptor-binding domain (RBD) is located on the spike S-protein's S1 subunit of the spike glycoprotein. The most important and effective therapy method is inhibiting the interaction between the ACE2 receptor and the S-spike RBD. An aptamer is a small, single-chain oligonucleotide that binds strongly to the target molecule. Recently, a CoV-2-RBD-1C aptamer-based system with a 51-base hairpin structure was discovered to have substantial binding affinity against the SARS-CoV-2RBD with similar binding sites at ACE. In the current study, we will study the aptamer's effect as a SARS-CoV-2 spike blocker and inhibit its ACE2 receptors' binding by studying the toxicity of aptamer for this cell line by calcein assay and the inhibition test of CoV-2-RBD-1C aptamers on spike RBD-ACE2 binding. The results show the half-maximum inhibitory concentration of CoV-2-RBD-1C aptamer is 0.08188 μM. The inhibition effect of CoV-2-RBD-1C aptamer on spike RBD-ACE2 binding was determined at half-maximal effective concentration of 0.5 μM concentration. The percentage of spike-ACE2 binding inhibition in A549-hACE2 cells in the D614G variant after 30 s was 77%. This percentage is higher than D614 and N501Y and equals 55% and 65%, respectively, at 0.15 μM of CoV-2-RBD-1C aptamer. The CoV-2-RBD-1C aptamer prevents virus entrance through spike inhibition, which results in a 90% reduction in spike D614 virus transduction at 1.28 μM. In conclusion, the CoV-2-RBD-1C aptamer might be an effective treatment against COVID-19 infection because it directly affects the virus by blocking the S-spike of SARS-CoV-2 and preventing ACE2 receptor binding.

An accurate and sensitive determination procedure has been established for the quantification of cefdinir in pure and pharmacological formulas. The approach was dependent on derivatizing cefdinir with sodium anthraquinone-2-sulfonate (SAS) in an alkaline medium to produce a magenta-colored derivative with a maximum absorbance at 517 nm against the reagent blank. Different factors affecting the interaction of cefdinir with SAS were studied carefully and optimized, such as the buffer value, medium acidity, the duration of hydrolysis, and the reagent percentage. Under optimized conditions, a linear calibration curve with a correlation coefficient of R² = 0.9995 was obtained over the concentration range of cefdinir 0.5-100 μg/mL. The values of the parameters that represented the sensitivity of the method were satisfactory, i.e., the limit of detection, the limit of quantification, as well as Sandell's sensitivity (л) were 0.1 μg/mL, 0.5 μg/mL, and 0.064 μg/cm²/0.001 Au, respectively. The relative standard deviation was below 1.35%, while the percentage recovery was 99.930%-102.257%. The mole ratio of the colored complex was estimated by following Job's method of continuous variation, which indicated that the cefdinir-SAS ratio was 1:1. The suggested approach was proven to be adequately accurate, precise, and without interfering with common excipients and additives. Thus, it could be implemented successfully for the standard determination of cefdinir in its pure and pharmaceutical forms.

Gout arthritis is an inflammatory condition that occurs suddenly in joints affected by high uric acid levels (hyperuricemia). The uric acid levels in this disease fluctuate throughout its various phases, resulting in frequent or recurrent attacks. This study aims to review some aspects of gout arthritis, such as its pathophysiology, treatment goals, and adverse drug reactions. This study employs review literature using articles published between 2017 and 2022 as the research methodology. Furthermore, articles under 2017 are used as references if they are relevant to the study's subject matter. The findings showed the importance of the pathogenesis of inflammation in the treatment of gout arthritis. It is also recommended to use anti-inflammatories such as colchicine and uric acid-lowering medications starting at a specific time to prevent unintended risks. Hence, pharmacotherapy management's adverse effects include nausea, vomiting, myalgia, neuropathy, and stomach pain.

The research aims to produce a local Pemberian makanan tambahan (PMT) biscuit formula that is nutritious, acceptable and has a good shelf life. Experimental research with RAL design used two factors and two treatments, namely the addition of anchovy flour (20% and 30%) and moringa leaf flour (20% and 30%) to 100 g of corn flour. The research was conducted in April-November 2022 with an analysis of nutritional content, and acceptability. Data were processed using SPSS with a statistical test One Way analysis of variance Test. The results of the analysis showed that the P4 product had a higher nutritional content difference, namely: 17.976 g of protein; fat 20.106 g; carbohydrates 60.644 g; minerals 3.632 μg; water content 3.999 aw; and energy 490.9 kcal with acceptance scores: Like-really like for 7 days at room temperature without standard packaging. Each serving portion for children of 2 pieces of biscuits or as much as 25 g/day gets a protein nutritional intake of 2.26 g or 11.3% of the Recommended dietary allowance (RDA); Fat of 2.66 or 5.9% of the RDA; Carbohydrates are 14.3 or 6.7% of the RDA and Energy is 615.23 kcal or 45.6% of the RDA. Product combination of 100 g of corn flour; 20 g of moringa flour; and 20 g of anchovy flour into the local therapeutic food "Iman" biscuit formulation which is very popular.