Journal of Advanced Pharmaceutical Technology & Research最新文献

The Suk-Saiyasna remedy, an herbal treatment, was historically used but ceased due to its cannabis content. After a relaxation of drug control laws in Thailand, its use re-emerged. This study examines the Suk-Saiyasna remedy's impact on rodent behavior and its receptor effects. This study was conducted to assess the sedative-like effects of the remedy on mice. The mice were divided into groups receiving 0.6, 3, 30, and 60 mg/kg extracts, with negative controls for comparison. We also investigated the impact on receptors, utilizing negative controls and pretreatment with receptor blockers, followed by either a negative control or a 60 mg/kg extract. Furthermore, this study investigated the behavioral aspects of mice, including anxiolytic effects, antidepressant-like effects, and motor coordination, utilizing the elevated plus-maze, open-field, and rotarod performance tests. The Suk-Saiyasna remedy (P < 0.05) decreased significantly in the latent period and increased sleeping time in the treated groups. Moreover, the Suk-Saiyasna remedy also showed efficacy in reaction to GABAA receptors and cannabinoid CB1 receptors (P < 0.05). In addition, positive effects were observed regarding the animal behavior in the arena, as the animal activity, behavior, and muscle coordination were reduced (P < 0.05). The Suk-Saiyasna remedy may be involved in a sedative-hypnotic-like effect in rodents under normal conditions through the modulation of GABAergic neurons and induction of the cannabinoid CB1 receptor mechanism.

Skin damage and aging are potential health problems for woman agriculture workers. This study aimed to test the efficacy of Oxalis dehradunensis ethanol extract formulated in antiaging cream preparations as an aging treatment in women agriculture workers. The method carried out was an experimental study on woman agriculture workers who were willing to volunteer. The experimental scenario conducted related to the physical quality of antiaging cream products and the efficacy of creams on the skin as an antiaging treatment. Physical quality parameters of antiaging cream include organoleptic assessment, cream emulsion, homogeneity, viscosity, pH, distribution, and skin irritation test to evaluate potential side effects. Skin aging efficacy assessments were conducted on 12 subjects divided into four formula concentration groups. The physical skin identification parameters measured are moisture, pore size, pigmentation or spots, and wrinkles using a skin analyzer. The results found that O. dehradunensis leaf extract formulated as an antiaging cream can neutralize free radicals and is an effective countermeasure against premature skin aging. There were significant differences in the skin characteristics of woman agriculture workers who participated as samples. The formula with 5% concentrate and 7% extract of O. dehradunensis has provided a reaction and is more effective in continuous treatment. It provides skin moisture changes of more than 300%, disguises pore size and good pigmentation, and reduces wrinkles of farmers who are constantly exposed to chemicals and free radicals in their agricultural activities. The leaf extracts antiaging cream showed more significant changes in moisture and skin pigmentation. It was concluded that the use of O. dehradunensis leaf extract as the core ingredient of antiaging cream can be an innovation that is beneficial to the health of the farming community, especially among women agriculture workers.

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.

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. S117 in vol. 13, PMID: 36643137.].

[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.