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GC-MS Analysis, Antioxidant, Antidiabetic Activity, and ADMET Study of Diospyros mespiliformis Hochst. Ex A. DC. Ebenaceae Stembark

The present study carried out GC-MS analysis, antioxidant, antidiabetic, and ADMET study of the crude ethanol extract (CRE), ethyl acetate (EAF), and aqueous (AQF) fractions of Diospyros mespiliformis (DM). Grandiflorenic (25.36%) and cis, cis-linoleic (27.13%) acids were the most abundant of the 59 and 40 compounds identified in the EAF and AQF, respectively. The EAF and CRE exhibited total antioxidant capacity of 77.78 ±0.01 ascorbic acid equivalent (mg AAE/g extract) and 60.20 ±0.01 mg AAE/g extract, respectively, significantly (p < 0.05) than the AQF (29.63 ±0.01 mg AAE/g extract). Furthermore, the EAF (38.27% ±2.44) exhibited a significantly (p < 0.05) higher percentage inhibition via the ferric thiocyanate assay than the CRE (17.45% ±2.18) and AQF (15.91% ±2.11). All the extracts showed significantly (p < 0.05) lower malondialdehyde concentrations than AA in the thiobarbituric acid assay. Additionally, the AQF exhibited a significantly higher percentage of H2O2 scavenging than the AA and EAF at 100 µg/ml. Diazoprogesterone (compound III) identified in the EAF exhibited the lowest respective binding affinity and inhibition constant, interacting with myeloperoxidase (-9 kcal/mol and 0.25 µM), xanthine oxidase (-9.9 kcal/mol and 0.05 µM), 11-β-hydroxysteroid dehydrogenase (-10 kcal/mol and 0.05µM), and sirtuin 6 (-10 kcal/mol and 0.05 µM). The molecular dynamics simulations showed residue fluctuations of the diazoprogesterone-docked complexes with the highest observed at Ser42 (5.14 Å), Cys1325 (8.96 Å), Ser281 (7.71 Å), and Leu78 (3.91 Å) for myeloperoxidase, xanthine oxidase, 11-β-hydroxysteroid dehydrogenase, and sirtuin 6, respectively compared to the undocked targets. Moreover, diazoprogesterone was predicted to possess good ADMET properties. Conclusively, DM possesses significant antioxidant and antidiabetic potential, containing compounds that might be a source of novel therapeutics against oxidative stress and diabetes.

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Effectiveness of Biological Assays as an Alternative Method to Determine the Potency of Antibiotics: A Review

In this review, chemical and biological assays performed in the pharmaceutical industry to determine the potency and bioactivity of antibiotics are discussed. Though commonly employed chemical methods can measure the potency of antibiotics, inefficiency to estimate the bioactivity is one of their major limitations. Due to their sensitivity and cost-effectiveness, common microbiological assays can serve as alternative methods. Several factors like doses of antibiotics, homogeneity of agar medium, inoculum concentration, chemical composition of agar media, size and solubility of samples or drug molecules, pH, relative humidity and exposure time can influence microbiological assays. Based on specific requirement and experimental targets, agar diffusion assays are designed focusing on their costs, errors, accuracy and simplicity. To avoid the misuse and overuse of antibiotics that leads to drug-resistance, parameters like zone of inhibition, minimum inhibitory concentration, minimum bactericidal concentration, mutation prevention concentration and critical concentration are also conversed in this study. Finally, microbiological and high-performance liquid chromatography methods were specifically compared for their sensitivity, accuracy and assessment of biological activity with minimal cost. Due to their advantages and disadvantages, parallel use of both bioassays and chemical methods are suggested to precisely determine the potency of antibiotics.

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Study Of The Stress-Protective Effect Of Sodium 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetate

The aim was to study the stress-protective effect of sodium 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetate. The analysis of the effect of the sample on the behavior and psycho-emotional state of animals, physiological parameters, antioxidant-prooxidant system was studied. Studies of stress-protective properties were performed on white outbred rats. As a comparison drug was used a Mebicar (Adaptol®) (reference sample). One hour after the simulation of immobilization 6-hour stress, the animals were subjected to a series of tests: "Open Field", "Light and Dark Chamber", "Morris Water Labyrinth". Behavioral tests were performed according to generally accepted methods in simplified modifications. Serum and liver homogenate were used to determine the content of markers of the antioxidant-prooxidant system: quantitative content of diene conjugates (DC), thiobarbituric acid reactants (TBA reactants), as well as catalase and superoxide dismutase (SOD) activity. Based on complex behavioral tests data, Catalase, TBA reactants, DC, SOD data in the serum and in the liver homogenate it can be concluded the presence of stress-protective properties of sodium 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetate in the model of acute immobilization stress.

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Systematic Scrutinization of Vital factors for the Development of Efficient Cisplatin-Quercetin Loaded Bionanomicelles

The present work aims to optimize and assess the Cisplatin (CIS) and Quercetin (QCT)-loaded biodegradable polymeric nanomicelles (PNM). The development of a quantitative method for the estimation of CIS and QCT in pharmaceutical dosage form was another objective. The aluminum plates coated with silica gel F254 used for separation of both the drugs employing Toluene: Methanol: Ethyl acetate: DMF: Triethylamine (5:0.5:3.5:1:1 drop % v/v/v/v/v) as mobile phase. Results of the validation parameter indicate that the developed method was precise, accurate, and robust. CIS and QCT-loaded PNM formulated using solvent evaporation technique employing poly lactic-co-glycolic acid (PLGA) 50:50. The Quality by Design (QbD) was accomplished to identify the critical manufacturing attributes and critical process parameters. Optimization of the formulation was performed by central composite design using particle size and % encapsulation efficiency as dependent variables. The amount of PLGA and Span selected as independent variables. Statistically substantial variables identified using regression analysis and analysis of variance. A diffusion study revealed that optimized nanomicelles were capable to sustain the drug release up to 8h. Zeta sizer, TEM confirmed the stability and nano-sized nanoparticles. CIS-QCT PNM was found to be an alternate route to systemic treatment.

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Healthcare Services and Empathy: A Portrait of the Pharmacy Students on Determining the Empathy Levels

Empathy is defined as a fundamental tool to improve the healthcare professional-patient bond and understanding of both patient and other professionals which enhances the healthcare professional’s experience. The empathetic attitude of the pharmacist could be a key element in effective interaction and this skill can be improved with various methods. In this study, it is aimed to reveal whether pharmacy education has an effect on the level of empathy by comparing the opinions of the students and their empathy levels. The validated Turkish version of the Empathy Quotient (EQ) questionnaire was used to reveal the participants’ empathy level. 311 students participated the survey from 699 students and 306 of them were included for the analysis. According to the scale scores’ mean of student, a statistically significant difference was found only in terms of gender. Additionally, whether they had an internship or not did not make a significant difference on empathy levels. Pharmacy students' technical skills in providing therapeutic recommendations may be negatively affected by their inability to communicate or engage with patients due to their lack of empathy. To prevent this, empathy as a teachable ability could be involved in the pharmacy education curriculum with various practices and techniques.

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Bacteria Mediated Drug Delivery System for Cancer Therapy

Kanser tedavisine yönelik terapötiklerin ve tedavi yaklaşımlarının geliştirilmesine rağmen hastalık dünya çapında önde gelen ölüm nedenlerinden biridir. Spesifite eksikliği, sitotoksisite ve çoklu ilaç direnci gibi sınırlamalar nedeniyle kemoterapi, radyasyon terapisi ve immünoterapi gibi kanser tedavileri ile henüz istenen düzeyde başarı elde edilememiştir. Bu nedenle yan etkilerin azaltılarak etkin bir tedavinin gerçekleştirilebilmesi için hedefe yönelik tedavilerin geliştirilmesi büyük önem taşımaktadır. Ancak kanser mikroçevresi, vaskülarizasyonu ve hipoksik bölgeleri ile hedeflendirme için birçok fizyolojik engele sahiptir. 1800’lü yıllardan günümüze kadar yapılan araştırmalar, bakterilerin bu fizyolojik engelleri aşarak kanser dokusuna seçici olduğunu göstermiştir. Bakterilerin doğal olarak tümör dokularını hedefleme ve dokuda birikme özelliklerine sahip olduğunun keşfedilmesiyle birlikte araştırmacılar, bakteri destekli ilaç taşıyıcı sistemler üzerine yoğunlaşmıştır. Bakterilerin hareketlilik, immün yanıt oluşturma ve kolay modifikasyon özelliğiyle konvansiyonel ilaç taşıyıcı sistemlerden daha üstün olduğu bildirilmiştir. Bu derlemede kanser tedavisine yönelik bakteri destekli ilaç taşıyıcı sistemler konusunda literatürde yer alan en güncel gelişmeler değerlendirilmiştir.

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Nutritional Benefits of Shea Products and Medicinal Properties of Shea Butter

Karite Ürünlerinin Besinsel Faydaları ve Karite Yağının Tıbbi Özellikleri
 
 ÖZET
 Karite veya Shea ağacı, Vitellaria paradoxa (Syn: Butyrospermum paradoxum, B. paradoxa, B. parkii) (Sapotaceae), Batı Afrika’nın kuru savan kuşağında doğal olarak yetişir. V. paradoxa subsp. paradoxa ve V. paradoxa subsp. nilotica olmak üzere iki alt türü tanımlanmıştır. Ağaç farklı ülkelerde farklı isimlerle bilinir. Karite ağacının önemi yüzyıllar önce meyvesi, çekirdekleri ve yağı aracılığıyla anlaşılmıştır. Günümüzde ise karite ağacı büyük bir ekonomik potansiyele sahiptir. Geleneksel olarak bitkinin farklı kısımlarının çok çeşitli kullanımları kayıtlıdır. Yağ; gıda hazırlama, ilaç ve kozmetik endüstrisinde kullanılır. Yağın ve yağdan izole edilen bileşiklerin anti-inflamatuvar, antimikrobiyal, antioksidan, anti-diyareik, anti-arthritik, antitümör, UV-koruyucu, emoliyan, nemlendirici, yaşlanma karşıtı ve proteaz inhibisyon etkilerinin olduğu çeşitli araştırmalarda gösterilmiştir. Ayrıca yağın kolesterol ve protein metabolizması üzerine etkisi bildirilmiştir. Yağ sabunlaşmayan maddelerin yüksek yüzdesi nedeniyle uluslararası kozmetik endüstrisinde oldukça talep görmektedir. Bu çalışmada; karite ağacının yayılışı, geleneksel kullanımı, ağaçtan elde edile meyve, çekirdek ve yağın kimyasal içerikleri; besinsel faydaları ve yağın tıbbi özellikleri ve kullanım alanları ile ilgili güncel bilgiler derlenmiştir.
 Anahtar Kelimeler: Vitellaria paradoxa, karite yağı, doğal kozmetik, kimyasal içerik, yemeklik yağ

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