Turkish journal of pharmaceutical sciences最新文献

Objectives: This study aims to investigate the duration required for endothelium dysfunction to develop in the fructose drinking-induced hypertension and examine the relative contributions of endothelium-dependent relaxing factors to changes in mesenteric arterial reactivity in male Wistar Albino rats.

Materials and methods: Metabolic parameters (water intake and food consumption) and hemodynamic parameters systolic blood pressure (SBP) and diastolic blood pressure (DBP)-were monitored in vivo. Vascular reactivity was examined in the isolated organ bath. Endothelium-dependent relaxation (EDR) to acetylcholine was observed in the absence and presence of pharmacological inhibitors of endothelial nitric oxide (NO) synthase, cyclooxygenase, and KCa2.3 channels. Contractile responses to phenylephrine and relaxation of sodium nitroprusside (SNP) were also determined.

Results: A significant increase in daily water intake and decrease in food consumption were typically observed in rats treated with 10% fructose for 4 weeks (p < 0.05). SBP and DBP increased significantly as early as 2 weeks of induction and continued to rise gradually throughout the induction period (p < 0.05). Fructose consumption significantly impaired EDR at week 3 and worsened at week 4 (p < 0.05). Impairment of the KCa3.1 channel-mediated component of endothelium-dependent hyperpolarisation (EDH)-type relaxation contributed to worsening EDR, whereas the contribution of NO-mediated relaxation was not apparent compared with the controls. The reduction in EDH-type relaxation in fructose-fed rats appears to be partially compensated by increased NO sensitivity in the smooth muscle region, as fructose induction increased SNP relaxation compared with the control.

Conclusion: These data provide evidence of early endothelial dysfunction developing concurrently with increased blood pressure in 10% fructose-fed rats. Decreased KCa3.1-mediated part of EDH-type relaxation appears to contribute to the impairment of endothelium-dependent vasorelaxation over time in this model.

Objectives: The increase in epidemic diseases and frequent use of alcoholic disinfectants, despite their side effects, prompt scientists to develop new sterilization products that do not contain alcoholic materials. The aim of this study was to develop, prepare, and evaluate a nanoemulgel skin sanitizer using essential oils (EOs) as active substances.

Materials and methods: A microwave-based technique was used to prepare nanoemulsion. The pseudo-ternary phase plots were constructed to contain three ingredients: EOs, polyoxyethylene (80) sorbitan monooleate, and a propylene glycol mixture (1:0:75) % (w/w) and double distilled. Five samples of nanoemulsion (NE1-NE5) were selected for the characterization and preparation of nanoemulgel (HN1-HN5). Blank gel (HN6) was also prepared to compare the antibacterial activity against HN1-HN5 formulations. Various evaluation processes were achieved for HN1-HN6 formulations. The statistical test was a One-Way analysis of variance at p ≤ 0.05 as significant data.

Results: The characterization process indicates that NE1-NE5 formulations had nanosized droplets, a homogenous distribution, and an acceptable charge. The evaluation process for HN1-HN6 formulations indicates clear, homogenous, with distinctive EO odor and no phase separation, slightly acidic pH, spreadability (128.22 to 124.22 g cm/sec), plastic rheological flow, no skin lesions after application, and conspicuous antimicrobial activity.

Conclusion: Laboratory characterization and evaluation demonstrated the existence of a promising product for sanitizing human skin and could be a successful alternative to alcoholic products based on the growing demand for EO products.

Objectives: Drug utilization studies are tools for determining the effectiveness of drug use. The aim of the study was to evaluate drug usage patterns in ear, nose, and throat (ENT) outpatient settings by incorporating established benchmarks and World Health Organization (WHO) indicators.

Materials and methods: A cross-sectional study on drug utilization evaluation (DUE) was conducted on 800 patients from the ENT outpatient department. We gathered data on currently prescribed medications and identified any discrepancies with a thorough analysis. Continuing educational activities such as "dear doctor" letters and personal consultations were used to rectify any irrational prescribing patterns among physicians. The WHO/International Network for Rational Use of Drugs core drug use indicators, specifically prescribing and patient care indicators, and established benchmarks were applied to encourage rational prescribing.

Results: The three most common diagnoses were pharyngitis (51.49%), allergic rhinitis (25.11%), and acute suppurative otitis media (21.17%). Montelukast, in combination with levocetirizine (13.77%) and amoxicillin in combination with clavulanic acid (8.81%), was the most frequently prescribed medication. The average number of drugs per prescription was 4.2% (±1.1), with low usage of generic names (33.0%) and suboptimal reliance on the essential drugs list (76.7%). Furthermore, patient care indicators demonstrated room for improvement, particularly concerning consultation times (6 minutes), dispensing times (30 seconds), and drug labeling practices (0% labeled). The DUE improved the prescribing rate of first-line drugs for five diseases and few aspects of prescribing and patient care indicators.

Conclusion: There is an overuse of prescribed drugs, a need for more utilization of generic names, and less than optimal use of the essential drugs list. Additionally, shortcomings in patient care were observed, including issues in consultation, drug dispensing times, and labeling. However, DUE effectively improved WHO patient care metrics and the prescription of first-line drugs warranting its implementation.

Objectives: This study examined how vitamin D supplementation based on daily dietary intake affects biomarkers in obese women with 25-hydroxyvitamin D deficiency.

Materials and methods: Group D (n= 14) used vitamin D supplements daily for 2 months, and Group C (n= 16) did not receive supplements. Three blood samples were collected from the volunteers during the initial phase of the study. In this study, blood was collected from the volunteers: first measurement (M1), second measurement (M2), and third measurement (M3).

Results: Compared with Group C, Group D had lower high-density lipoprotein (HDL) levels at M2 and fasting serum glucose (FSG) levels at M3 (p < 0.05), and lower HDL levels at M2 and FSG levels in normal-weight individuals at M3 (p < 0.05). In addition, 25-hydroxyvitamin D levels were higher in normal-weight women than in obese women according to M3 (p= 0.043). There was a higher negative correlation between HDL-C in M1 and FSG in Group D (r= -0.710, p= 0.004). 25-hydroxyvitamin D was moderately positively correlated with dietary vitamin D in M2 in Group D (r= 0.559, p= 0.038). Significant positive correlations were observed between iodine intake and triiodothyronine (T3) levels, whereas no significant difference was observed between thyroid-stimulating hormone and T3 levels.

Conclusion: Vitamin D intake improves HDL levels in normal-weight individuals and causes an effect on FSG to be at the desired low level, whereas in individuals with obesity, although serum 25-hydroxyvitamin D levels increased in the last measurement, no effect was observed. Women with normal vitamin D levels have higher serum 25-hydroxyvitamin D levels than those who are obese.

Objective: This study aimed to investigate whether Mitragyna inermis (Willd.) Otto Kuntze organic and aqueous extracts are able to control seizures induced by pentylenetetrazol (PTZ) in mice based on flavonoid fingerprints and alkaloidal contents.

Materials and methods: Ethanolic extract and decoction-derived fractions from roots, leaves, and stems were subjected to chromatographic fingerprinting using AlCl₃ and screening for their antiseizure effects using PTZ-induced acute seizure model. From the fractions that showed potent bioactivities, plausible antiseizure alkaloids were isolated using thin layer chromatography, and their structures were elucidated using ¹H NMR, 2D NMR, ¹³C NMR, and FAB-HR (+ve or -ve).

Results: All fractions, with the exception of the dichloromethane and hexane fractions, revealed remarkable flavonoid fingerprints. An acute PTZ-induced seizure test revealed that ethanolic extract of stem bark [500 mg/kg body weight (bw)], ethyl acetate extract of stem bark (500 mg/kg bw), and aqueous extract of leaves (300 mg/kg bw) significantly delayed the occurrence of hind limb tonic extension (HLTE); however, a non-significant delay was observed in the onset of first myoclonic jerk compared with control animals. Isolation yielded four main alkaloids: that are, pteropodine (1), isopteropodine (2), mitraphylline (3) and corynoxeine (4). Corynoxeine is a new compound derived from M. inermis.

Conclusion: This study suggests that flavonoid fingerprints are tracers of M. inermis anticonvulsant ingredients. The stem bark ethanolic and ethyl acetate extracts and leaf aqueous extracts contain anticonvulsant bioactive principles that delay notifying the HLTE occurring in male naval medical research institute mice. Furthermore, alkaloidal contents also remain plausible bioactive anticonvulsant principles. All observations support the traditional use of M. inermis to manage epilepsy. However, further studies are needed to understand the effects of alkaloid fractions, flavonoids, and the isolated compounds as promising antiseizure agents derived from M. inermis in experimental animals.

Objectives: This study sought to examine the chemical profile, antioxidant, antimicrobial, antibiofilm, and anti-quorum sensing potential of two propolis ethanolic extracts (PEEs) collected from northeast Algeria.

Materials and methods: To achieve the main objectives of this study, multiple in vitro tests were employed. The phenolic and flavonoid contents were analyzed, and the chemical composition of both PEE was determined by high-performance liquid chromatography. The antioxidant properties of the propolis extracts were investigated using six complementary tests. The inhibitory effects of propolis extracts were evaluated against multidrug-resistant (MDR) clinical isolates using agar well diffusion and microdilution methods, whereas their antibiofilm and quorum-sensing disruption effects were determined by spectrophotometric microplate methods.

Results: The results demonstrated that phenolic and flavonoid contents were higher in propolis from the Guelma (PEEG) region (PEEG; 188.50 ± 0.33 μg GAE/mg E, 144.23 ± 1.03 μg QE/mg E), respectively. Interestingly, different components were identified, and cynarin was the major compound detected. The PEEG sample exhibited potential antioxidant effects in scavenging ABTS^•+ radicals with minimal inhibitory concentration values equal to 10.46 ± 1.40 µg/mL. Furthermore, the highest antibacterial activity was recorded by PEEG against Gram-positive Staphylococcus aureus MDR1. Similarly, PEEG effectively inhibited the biofilm formation of S. aureus MDR1 and the degradation of biofilm was up to 60%. In addition, quorum sensing disruption revealed that both extracts have a moderate capacity for violacein inhibition by the Chromobacterium violaceum ATCC 12472 strain in a concentration-dependent manner.

Conclusion: These findings indicate that propolis can be regarded as a natural therapeutic agent for health problems associated with MDR bacteria and oxidative stress.

Objectives: Colorectal cancer is one of the most common cancers worldwide. However, surgical intervention and chemotherapy provide only limited benefits for the recovery and survival of patients. The anticarcinogenic effect of genistein has attracted attention because epidemiological studies have shown that soybean consumption is associated with a decrease in the incidence of cancer. There are limited studies on the effects of genistein in colorectal carcinoma cells. We aimed to investigate the cytotoxic, genotoxic, and apoptotic effects of genistein in SW480 and SW620 colon adenocarcinoma cells treated with 5-fluorouracil, the basis of chemotherapy, and the tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) ligand, the mediator of apoptosis, both alone and in combination.

Materials and methods: Cytotoxicity and genotoxicity were determined by MTT and comet assays, respectively. The apoptotic effects were evaluated by reverse transcription-polymerase chain reaction assay, with the additional use of Annexin V FITC, mitochondrial membrane potential (MMP), caspase 3, 8, and 9 activity, and reactive oxygen species (ROS) assay kits.

Results: According to our findings, genistein, 5-fluorouracil, and TRAIL had synergistic apoptotic effects because of DR5 upregulation, ROS production, and DNA damage, which were mediated by increased caspase-8, and -9 activity and decreased MMP.

Conclusion: The applied combinations of these compounds may contribute to the resistance problem that may occur in treating colorectal cancer, with a decrease in DcR1 and XIAP genes.