Turkish Journal of Pharmaceutical Sciences最新文献

Objectives: Maclura pomifera (Rafin.) Schneider is a widespread species all around the world, which is also frequently cultured for ornamental purposes. Previous studies revealed that M. pomifera fruits are rich in prenylated isoflavonoids, exhibit noteworthy biological activities, and have probable benefits, particularly, when applied topically. Considering that phenolic compounds are important sources in the development of anti-aging cosmetic products, this study investigated the anti-aging potential of M. pomifera 80% methanolic extract (MPM) by evaluating antioxidant and extracellular matrix degrading enzymes inhibiting activity.

Materials and methods: For this study, the inhibitory potential of 80% MPM against different enzymes associated with the aging process was evaluated. Given the unequivocal role of oxidative stress in aging, in vitro antioxidant tests were employed as well. Moreover, osajin was determined as the major bioactive isoflavonoid of the sample by high performance thin layer chromatography analysis.

Results: Results of the mechanistically different antioxidant assays exhibited notable antioxidant potential of the extract. Inhibition potential of MPM against hyaluronidase, collagenase, and elastase enzymes, which are directly linked to acceleration of the aging process, was investigated and results revealed that MPM inhibited the aforementioned enzymes explicitly. MPM had notable phenolic and flavonoid content; 113.92 ± 2.26 mg gallic acid equivalent/g and 66.41 ± 0.74 mg QE/g, respectively. When total antioxidant capacity assays were considered, it is possible to suggest that MPM is a promising anti-aging agent.

Conclusion: As a result, this study discloses that extracts of fruits of M. pomifera have significant anti-aging potential and may be used for this purpose.

Objectives: Tanacetum L. belongs to Asteraceae family and is represented by 46 species in Türkiye. Tanacetum genus is known for its insecticide and insect repellent effect. T. argyrophyllum contains sesquiterpene lactone derivatives. These compounds are responsible for its various activities, especially cytotoxic, antitumor, phytotoxic, antimicrobial, antiviral, and antifungal activity. There are not enough biological activity studies on the plant that are likely to have a wide variety of activities in terms of the compounds it contains. The aim of the present study is to evaluate various biological activities of 80% aqueous methanol extract prepared from aerial parts of T. argyrophyllum (K. Koch) Tzvelev var. argyrophyllum collected from Sivas province of Turkey.

Materials and methods: Antioxidant activity of the methanol extract was determined by 2,2'-diphenyl-1-picryl-hydrazyl and 2,2-azinobis (3-ethyl benzothiazoline-6-sulfonic acid) radical scavenging activity, total phenolic, and total flavonoid content tests. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities were investigated via Ellman's spectrometric method.

Results: Total phenolic content was found as 71.67 mg/gallic acid equivalent g and total flavonoid content was 25.225 mg/quercetin equivalent g on a dry extract weight basis. In this work, AChE, BChE, and α-glycosidase enzymes were inhibited by the extract of T. argyrophyllum var. argyrophyllum. IC₅₀ values for these enzymes were found as 266.79 µg/mL for AChE and 176.91 µg/mL for BChE. Also, the α-glycosidase activity exhibited a dose-dependent manner with increasing concentration.

Conclusion: According to the results, T. argyrophyllum var. argyrophyllum can be used as an ingredient of functional foods as well as herbal products for diabetic and Alzheimer's disease patients.

Objectives: Colorectal cancer (CRC) remains a crucial health problem due to the toxicity of 5-Fluorouracil (5-FU) as first-line chemotherapy agent for treating CRC. The anticancer effects of boron and its compounds have been shown in various cell lines. This study aimed to examine the cytotoxic and apoptotic effects of borax (sodium tetraborate) alone or along with 5-FU on human CRC cells, DLD-1.

Materials and methods: Cytotoxicity and apoptosis were determined by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay, 4',6-diamidino-2-phenylindole and annexin V/propidium iodide staining.

Results: The results showed that combined treatment revealed a significant time- and concentration-dependent cytotoxic effect on DLD-1 cells compared with borax or 5-FU treatment alone. The combination of borax and 5-FU induced a clear increase in the early apoptotic cell percentage, compared to the cells treated with monotherapies. Additionally, a significant increase in condensed and fragmented nuclei was detected in DLD-1 cells treated with the combination treatment compared with borax or 5-FU alone.

Conclusion: Our current findings suggest that the combination of borax with 5-FU has a strong cytotoxic and apoptotic effect on the human CRC DLD-1 cells.

Objectives: Recently, N-nitrosamines were unexpectedly detected in valsartan and other generic sartan products. Taking into this account, we developed a sensitive and stable multiple reaction monitoring mode-based "gas chromatography-tandem mass spectrometry (GC-MS/MS)" approach for the quantification of "four N-nitrosamines" in valsartan, especially, N-nitrosodiisopropylamine, N-nitroso ethyl isopropylamine, N-nitrosodiethylamine, and N-nitrosodimethylamine.

Materials and methods: GC and MS conditions were optimized with specificity, sensitivity, linearity, precision, and accuracy of the parameters. The approach was validated as per the "International Council for Harmonization" recommendations.

Results: The identification limits and limits of quantification of N-nitrosamines in valsartan varied between 0.02 and 0.03 ppm, and 0.06-0.09 ppm, respectively. The obtained values were satisfactory with limits established by the United States Food and Drug Administration for sensitivity requirements. The regression coefficients greater than 0.999 for four N-nitrosamines in the calibration curve demonstrated the strong linearity of the process. The retrievals of "N-nitrosamines" in valsartan between 91.9-122.7%. For the intra-day and inter-day accuracy studies, the (relative standard deviation) was less than 9.15%.

Conclusion: The proposed approach has rapid analysis capability, high precision, accuracy, and good sensitivity, which give a reliable approach for N-nitrosamines quality control in valsartan.

Objectives: Divalproex sodium (DS), being a hygroscopic drug, requires low humidity during product manufacturing. This study aims to develop a hygroscopicity controlled sustained release formulation of DS that can be manufactured in relatively high humid conditions in facilities lacking dehumidifiers.

Materials and methods: This study focuses on the role of polyethylene glycol (PEG-8000) and hydroxypropyl methylcellulose (HPMC K100M) as polymers of choice to control hygroscopicity and retard release of DS using solid dispersion technique. In this study, homogeneous solid dispersions containing various ratios of PEG-8000, HPMC K100M, and DS were obtained via melt granulation technique. Fifteen different solid dispersions were prepared based on Box-Behnken experimental design created in MiniTab software. The obtained solid dispersions were separately broken down into granules and their hygroscopic properties were determined via moisture uptake studies. Granular solid dispersions were then compressed into tablets and their sustained release dissolution profiles were studied as per the United States Pharmacopoeia (USP) monograph of DS extended-release tablets. Dissolution profiles of all fifteen formulations were then analyzed in Box-Behnken experimental design under MiniTab software to determine an optimized formulation having low hygroscopic properties as well as required multipoint drug release as per USP monograph. The final optimized formulation was prepared and subjected to moisture uptake study to determine its hygroscopicity, dissolution study to determine drug release kinetics and fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) analysis to determine molecular interactions between drug and polymers.

Result: Optimized final formulation yielded granular solid dispersion with 28% less hygroscopicity compared to DS and tablets with an excellent release profile in accordance with USP monograph. FTIR and DSC analysis did not show any significant interaction between DS and components of the solid dispersion.

Conclusion: Optimized formulation from this study can be used to manufacture divalproex extended-release tablets inside facilities lacking dehumidifiers.

Objectives: The "safe if natural" perception of herbal products may have several undesirable side effects. It is important to raise awareness in public order to change this perception and ensure safer use of herbal products. The role of pharmacists is to supply herbal medicines safely and to provide accurate information to the patients about herbal products. The aim of this study was to analyze the perspective, knowledge, attitude, and behavior of community pharmacists about phytovigilance.

Materials and methods: A cross-sectional analysis was performed using community pharmacists (n= 879) using face-to-face surveys between April-June 2019 in Istanbul. For statistical analysis, student's t-test and one-way ANOVA were used to compare the mean values of the groups.

Results: It was determined that 58.1% of the pharmacists heard phytovigilance for the first time and 93.5% of them had not reported any safety-related herbal medicine reported so far. Among the reasons for not reporting, well-known adverse reactions were found to be 24.2% and the difficulty of reporting was found to be 21.8%. 84.6% of pharmacists have never received training related to phytovigilance. It was found that pharmacists with a working experience of more than 20 years primarily selected herbal products provided in their pharmacy based on the manufacturing company primarily, whereas others selected based on the efficacy of the products.

Conclusion: The results of this study have revealed the necessity to increase training on the safety of herbal medicines to cover all stakeholders and to give due importance to phytovigilance. The phytovigilance systems established in some countries for public health should be expanded to other countries. There is a need for a more user-friendly reporting system to increase adverse reaction reporting by pharmacists and other healthcare professionals. In the future, plan to perform studies to raise awareness in the public and promote reporting with digital technologies.

Parkinson's disease (PD) is a type of movement disorder that affects the ability to perform daily activities. It is considered that 1 million people in the U.S. and more than 10 million people worldwide live with PD. It is a chronic and progressive disease, so symptoms worsen over the time. Patients experience motor symptoms such as tremors, stiffness and slow motion, and non-motor symptoms such as sleep problems, constipation, anxiety, depression and fatigue. Dopaminergic drugs are critical for treating motor symptoms in PD. Levodopa (L-DOPA) is the "gold standard" medication for the control of motor symptoms. Because of the progression of the disease, the effectiveness of oral L-DOPA decreases over time and motor fluctuations such as "delayed ON", "no ON" and unpredictable "ON-OFF" periods appear. These motor fluctuations affect the quality of life of the patient at a high rate and the patient has problems in fulfilling his daily morning routines. Gastrointestinal (GI) problems, as the common non-motor symptom, are the most important cause of motor fluctuations that occur because of inadequate oral treatment with the progression of PD. When oral treatments are not sufficient, non-oral treatments that are not affected by GI problems are required. In this review, the treatment strategies, developed and approved non-oral drug delivery systems in the early and advanced stages of PD are emphasized.

Objectives: Passiflora incarnata L., commonly called folk medicine declaredly used for an enormous range of therapeutic purposes, one such is antioxidant potency. The study prioritized to determine the phytochemical analysis of total phenolics, flavonoids, alkaloids, and tannins contents as well as the antioxidant properties through 1,1-diphenyl-2-picrylhydrazyl (DPPH) quenching assay, 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation decolorization test, superoxide, and hydrogen peroxide radical scavenging assays of ethanol extract of P. incarnata leaves.

Materials and methods: The organoleptic characteristics such as color, odor, appearance, taste, and other characters such as drying range and fiber contents were analyzed as preliminary data. Analytical parameters like total phenolic content, total tannins, total alkaloid content, and total flavonoid with multiple antiradical scavenging activity (DPPH, ABTS, superoxide and H₂O₂ scavenging assays) with IC₅₀ (μg/mL) in terms of inhibition percentage with various concentrations of the ethanolic extract studied.

Results: P. incarnata possessed a high radical scavenging activity with a phenolic content of 2.48 mg gallic acid equivalent/g of extract in leaves, whereas the total flavonoid content was 2.1, respectively.

Conclusion: High antioxidant activity was noticed in P. incarnata extract, in which might be of higher levels of flavonoids and phenols. Findings in the studies revealed that P. incarnata is a veritable source for antioxidant drug bioprospecting in scientific research and pharmaceutical industries.