{"title":"Opioid Peptides: Pharmaceutical Significance and Formulation Approaches","authors":"Demet Engi̇n, S. Timur, Stela Muçaj, R. N. Gürsoy","doi":"10.52794/hujpharm.1109147","DOIUrl":"https://doi.org/10.52794/hujpharm.1109147","url":null,"abstract":"Opioidler, kendi reseptörlerine bağlanarak gösterdikleri ağrı kesici etkisi nedeniyle, binlerce yıldır ağrı tedavisinde kullanılmaktadır. Günümüzde kullanımları daha kontrollü olarak hala devam etmektedir. Ancak yan etkileri ve bağımlılık potansiyelleri nedeniyle hastaların izlenmesi gerekmektedir. Araştırmacılar tarafından, insan vücudunda doğal olarak sentezlenen ve opioid benzeri etkilere yol açan endojen opioid peptidleri bulunmuştur. Bu peptidlerin sentetik analogları da sentezlenmektedir. Bu bileşikler kimyasal yapılarından dolayı hidrofiliktir, yük taşırlar ve oral olarak uygulanmaları kısıtlıdır. Bu nedenle formülasyon için farklı yaklaşımlar geliştirilmiştir. Peptid tabanlı hidrojel sentezlenmesi ve bileşiğin hidrojele konjuge edilmesi, peptidin kumarinik asit temelli siklik bir ön ilaca dönüştürülmesi yaklaşımları stabil olmayan opioid peptidleri enzimatik parçalanmadan korur. Peptidin bir nanopartiküle yüklenmesi ve lipozomal nanotaşıyıcıların kullanılmasında nanoteknolojiden yararlanılmıştır. Multiveziküler lipozomlar (DepoFoam) kullanılarak cerrahi sonrası ağrı yönetiminde peptid temelli ilaç uygulanması mümkündür. Opioid peptidler, tedavide faydalanılabilecek birçok endikasyona sahiptir. Peptidlerin formülasyonunda çok çeşitli teknolojiler kullanılmaktadır ve bu çalışmalardan umut verici sonuçlar elde edilmiştir.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"47 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73816330","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Dapagliflozinin Diyabetik Sıçanlarda Sub-akut Maruziyet Sonrası Renal Etkilerinin Değerlendirilmesi","authors":"Tuğçe Boran, Bahar ULUS KARACA, Ayça KARAGÖZ KÖROĞLU, Feriha Ercan, Gülcan Özhan","doi":"10.52794/hujpharm.1171489","DOIUrl":"https://doi.org/10.52794/hujpharm.1171489","url":null,"abstract":"Dapagliflozin (DAPA), a sodium glucose co-transporter 2 (SGLT2) inhibitor, is a therapy option for the treatment of type 2 diabetes. Although several studies have demonstrated its protective effects on the kidney, the FDA warns about the risk of DAPA-induced nephrotoxicity. SGLT2 inhibitors may induce oxidative stress and inflammation in the kidney due to their mechanism of action. In the present study, it was aimed to clarify the molecular effects of DAPA on the kidney. Streptozotocin (STZ)-induced diabetes was initiated by single injection of STZ (35 mg/kg b.w.) after a two-week high-fat diet in male rats. Diabetic rats were administered with DAPA at 10 mg/kg b.w., by oral gavage for 28 days. The oxidative stress, inflammation and apoptosis induction potentials of DAPA were evaluated in kidney homogenates. The morphological changes and apoptosis were investigated by histological examinations. It was observed that DAPA treatment reduced oxidative parameters. The inflammatory mediators increased in diabetic control group, however, this increase was slightly inhibited by DAPA treatment. According to the histological examinations, DAPA ameliorated the diabetes-induced changes and apoptosis. As a result, DAPA showed a protective effect on the kidney by alleviating oxidative stress and inhibiting inflammation and apoptosis. However, further studies are needed to determine the long-term effects of DAPA on the kidney in diabetics by focusing on different mechanisms and individual differences.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"225 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83126307","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hasan Memi̇ş, Ahmet Çakir, Nesligül Özdemi̇r, Zeynep Ülkü Gün
{"title":"Yoğun Bakım Hastalarında Antimikrobiyal İlaç Dozajlarının Uygunluğunun Değerlendirilmesi","authors":"Hasan Memi̇ş, Ahmet Çakir, Nesligül Özdemi̇r, Zeynep Ülkü Gün","doi":"10.52794/hujpharm.1302724","DOIUrl":"https://doi.org/10.52794/hujpharm.1302724","url":null,"abstract":"The purpose of this study was to investigate the factors that required dose adjustments of antimicrobial drugs in intensive care unit (ICU) patients and to identify the drugs that required the most dose adjustments. \u0000The 26-bed reanimation ICU of a university-affiliated hospital hosted this study from September to December 2022. Two clinical pharmacists on duty examined patients' antimicrobial drug dosages daily. The acceptance status of the recommendations and the patients' demographic information were recorded. \u0000The study involved 133 ICU patients, and antimicrobial drug recommendations were made for 48 patients, 31 (64.6%) of whom were male. The median (IQR) age of the 48 patients was 67 (54–77). The number of recommendations was 94, and all of them were accepted by the physician. The recommendation rates according to the causes were: inappropriate dosages based on renal functions (71.3%), presence of continuous renal replacement therapy (11.7%), indication (10.6%), body weight (4.3%), and loading dose (2.1%). \u0000The top 3 drugs for which recommendations were made the most were colistin (21.3%), meropenem (18.1%), and piperacillin-tazobactam (12.8%). The most troublesome drug was colistin, which is frequently used to treat Acinetobacter pneumonia. Clinical pharmacist and physician collaboration may help rationalize ICU antimicrobial drug use.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89406941","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of anti-inflammatory activity and identification of a monoterpenoidhydroxylactone (-)-loliolide from Tribulus terrestris L.: In-vivo and In-silico Approaches","authors":"Shaza SHANTİER, Wadah OSMAN, Mona MOHAMED","doi":"10.52794/hujpharm.1179460","DOIUrl":"https://doi.org/10.52794/hujpharm.1179460","url":null,"abstract":"The present study aimed to determine the anti-inflammatory effects of Tribulusterrestris L (aerial parts) and to identify the anti-inflammatory agents from active extracts and fractions together with in silico prediction of their mechanism of action, pharmacokinetics, and toxicity profile. The anti-inflammatory activity was evaluated for Dichloromethane, methanol, and its fractions (chloroform, ethyl acetate, n-butanol by Carrageenan induced rat paw edema. The phytoconstituents of the anti-inflammatory active fraction (chloroform fraction of methanol extract) was identified using Thermo Scientific TM DFS high-resolution GC-MS. The GC-MS analysis revealed 13 compounds from which (-)-loliolide was the most abundant compound by peak area. It was docked, using Autodock 4.0 onto three Key enzymes involved in the inflammatory cascade (Cyclooxygenase (COX-1 &2) and 5-lipooxygenase (5-LOX)). It displayed binding energies; -6.98 kcal/mole (COX-1) compared to -6.83kcal/mole for standard, -6.64 kcal/mole (COX-2) compared to -6.88 kcal/mole for standard and -5.25 kcal/mole (5-LOX) compared to -6.89 kcal/mole for standard. Toxicity risks, drug likeliness, and pharmacokinetic properties were studied by different online open-source programs. Good binding energy, drug-likeness, and efficient pharmacokinetic parameters of (-)-loliolide suggest it as a good inhibitor, however, further research is needed.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"18 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135840911","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Migren Araştırmalarında Kullanılan Güncel Hayvan Modelleri","authors":"Melih Zeki KAYA, Sibel BOZDAĞ PEHLİVAN, Levent ÖNER","doi":"10.52794/hujpharm.1332342","DOIUrl":"https://doi.org/10.52794/hujpharm.1332342","url":null,"abstract":"Hayvan modelleri, insana zarar verme riski olmadan insanda görülen hastalıkların incelenmesinde ve yeni terapötik yaklaşımların geliştirilmesinde kullanılan önemli araştırma araçlarıdır. Hayvan modellerinde gözlenen biyolojik aktivite ile insanda elde edilen arasında her zaman birebir benzerlik olmasa da insan hastalıkları için birçok ilaç ve tedavi hayvan modellerinin rehberliğinde geliştirilmektedir. Bu kapsamda, son yıllarda baş ağrısı ve migren mekanizmalarını incelemek için hayvan modelleri yoğun bir şekilde geliştirilmiş ve bunun sonucu olarak migrenin anlaşılmasında ve anti migren tedavilerin geliştirilmesinde önemli adımlar atılmıştır. Bu modeller arasında, genetik modifikasyonlarla oluşturulan fare ve sıçan modelleri, trigeminal sinir sistemi aktivasyonunu taklit eden modeller ve inflamatuar ajanlarla baş ağrısı indüklenen modeller yer almaktadır. Her bir modelin kendine özgü üstünlük ve sınırlaması olduğundan, ilaç etkinliğini değerlendirmek için uygun hayvan modelinin seçimi ve sonuçların değerlendirilmesi için en uygun deneysel yöntemin seçimi kritik bir parametredir. Bu derlemede son yıllarda üzerinde yoğun bir biçimde çalışılan in-vivo migren modelleri ve bu modellerden elde edilen en son bulgular üzerinde tartışılacaktır","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136163420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Yeni imidazol 2-amino pirimidin türevleri: Insilico çalışmaları, insan-CDK2'ye karşı kanser önleyici aktivitelerinin değerlendirilmesi","authors":"Navneetha Oleti̇, Hemalatha Sattu, Munı Sıreesha Sunkara, Pranitha Kurella, Sahithi Manchi","doi":"10.52794/hujpharm.1177687","DOIUrl":"https://doi.org/10.52794/hujpharm.1177687","url":null,"abstract":"In drug discovery process the identification of lead compounds by virtual screening is a novel approach. From the literature it is understood that imidazoles and pyrimidines have gained much importance among the medicinal chemists because of their flexible structure and varied pharmacological activities. In present study imidazole and 2-amino pyrimidine derivatives were designed, subjected to the structure based virtual screenings in order to find the novel anticancer agents against human CDK2 protein. The molecular properties and molecular toxicity prediction was done using various online softwares like Molinspiration, Molsoft, OSIRIS, pkCSM along with bioactivity properties. The derivatives which exhibited drug like property were further subjected to molecular docking studies using Autodock Vina. Hits are identified, the basic pharmacophoric features responsible for the anticancer activity were predicted. Based on docking results the compound 24, which exhibited highest binding interaction with receptor will be further synthesized and can be novel lead for the development of anticancer agents.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"47 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72404863","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of Neopterin Levels and Kynurenine Pathway in Acute Coronary Syndrome Patients","authors":"İbrahim KEMBER, Gözde GİRGİN, Terken BAYDAR","doi":"10.52794/hujpharm.1261037","DOIUrl":"https://doi.org/10.52794/hujpharm.1261037","url":null,"abstract":"Neopterin Düzeylerinin ve Kinürenin Yolağının Akut Koroner Sendrom Hastalarında Değerlendirilmesi
 Koroner arter hastalığının en önemli nedeni koroner aterosklerozdur. Aterosklerotik plağın yırtılması ile oluşan intrakoroner trombüs ise akut koroner sendomun temel nedenidir. Yırtılmaya hassas plakların daha fazla sayıda maktofaj ve T lenfosit içerdiği çeşitli çalışmalarda gösterilmiştir. Neopterin hücresel immün yanıtın önemli bir biyogöstergesidir. İnflamasyon, çeşitli enfeksiyonlar ve maligniteler de dahil olmak üzere çok çeşitli patolojilerde erken tanı ve prognoz için önemli bir biyomarkör olarak kabul edilir. Hücresel immün aktivasyonda neopterin salınımına ilave olarak triptofan yıkımında hız kısıtlayıcı basamağı katalizleyen indolamin 2,3-dioksijenaz (İDO) enzimi de aynı anda indüklenir. Kinürenin (Kyn) in triptofan (Trp) ’a oranlanmasıyla ifade edilebilien İDO aktivitesinin, immün değişkenlerle desteklenerek hücresel immünitenin düzenlenmesinde önemli bir gösterge olarak kullanılabileceği rapor edilmiştir. Bu derleme makalesinde, anjiyografik olarak ateroskleroz zemininde gelişen akut koroner sendrom (AKS) hastalarında, neopterin, C reaktif protein (CRP), İDO gibi biyokimyasal göstergelerin koroner arter hastalığı (KAH) tanısı, mortalite ve morbidite süreçlerindeki olası değişimlerin değerlendirilmesi hedeflenmiştir. Akut koroner sendrom hastalarında, neopterin düzeyleri ile kinürenin yolağı parametlerinin belirlenmesi ve biyomarkör olarak kullanılmaları anlamlı ve değerlidir.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"66 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135286703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Review on Diabetic Foot Ulcers and Its Herbal Approach to Treatment","authors":"Het Talati̇, P. Bhatt","doi":"10.52794/hujpharm.1167357","DOIUrl":"https://doi.org/10.52794/hujpharm.1167357","url":null,"abstract":"Diabetes, a silent killer and globally renowned disease, has enormously afflicted most parts of the world causing serious health issues to an individual, many of which suffer financially. There are several outbreaks of this disease, but diabetic foot ulcer is a dreadful situation imparting harsh skin ailments to an individual’s feet. The etiology of these ulcers includes high glucose levels, improper foot hygiene, etc. The pathophysiology of diabetic foot ulcers involves oxidative stress to the nerve tissues and other complications leading to loss of sensation in the patient’s feet along with skin dryness. Many times, diabetes remains undiagnosed but the foot ulcers can be evaluated by the latest electro-diagnostic, radiological, or vascular studies. Once identified, they can be treated with several topical antibiotics and certain foot assistance methods. Besides allopathic medication, one can also opt for herbal treatment as many herbal species are still unnoticed having specific phytochemicals and ought to be an ultimate source for wound healing, some of them are Radix rehmanniae, Martynia annua, Cortex phellodendri, Angelica dahurica, and Moringa oleifera A few of these plant species possess anti-oxidant, anti-bacterial, and other potent therapeutic properties which enhance the wound healing process as per its physiology and with minimal side effects. Some Ayurvedic formulations like Jatyadi Ghrita also contribute efficiently to this ailment that can be applied to foot ulcers to gain positive results.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90477055","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Alzheimer Hastalığı ve Anti-Alzheimer Etkili Bileşiklerin Yapılarının Araştırılması","authors":"Özden Tari, Ramazan Yağmurtaşan","doi":"10.52794/hujpharm.1175099","DOIUrl":"https://doi.org/10.52794/hujpharm.1175099","url":null,"abstract":"Demansın en yaygın şekli olan Alzheimer hastalığı, hafıza kaybı ve diğer bilişsel problemler ile karakterize karmaşık bir hastalıktır. Artan prevalansa sahip olan Alzheimer hastalığının fizyopatolojisinin anlaşılması ve bu hastalığın tedavisinde etkin olan bileşiklerin yapılarının araştırılması, yeni etkin ilaç moleküllerinin geliştirilmesine yardımcı olacaktır. Bu anlamda hastalık üzerinde etkili olan hipotezlerin, etkin olan bileşiklerin yapısının ve etki mekanizmalarının araştırılması büyük önem taşımaktadır. Son yıllarda yapılan araştırmalarda, hastalığın patolojisinde etkili olan hipotezlerin birden fazlasını etkileyebilen daha güçlü bileşikler elde edilmeye odaklanıldığı görülmektedir. Bu derleme çalışmasında, Alzheimer hastalığının patolojisinde rol oynayan önemli hipotezler ile bu hipotezler üzerinden anti-Alzheimer etkinliği kanıtlanmış ilaç etken maddelerinin yapıları ortaya konulmuştur.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"152 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75095886","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Diazotizasyon ve Kuplaj Reaksiyonu ile Saf Form ve Farmasötik formülasyonlarda Mesalazin'in spektrofotometrik tayini","authors":"Aws Maseer, Moath Najem","doi":"10.52794/hujpharm.1129852","DOIUrl":"https://doi.org/10.52794/hujpharm.1129852","url":null,"abstract":"An accurate, simple, and precise spectrofluorimetric method is presented for the determination of Mesalazine (MZN) based on Diazotization in acidic medium through reaction it with Sodium nitrite (NaNO2) to result diazonium salt that Coupling Reaction in medium base with 2,7-Dihydroxynaphthalene (DHNP) to formed azo dye. The intensity of the dye was measured at 501 nm after optimization of the experimental parameters. Beer’s law was applied to the proposed method and it was valid within a concentration range of 0.25–10 μg/mL and the linear regression was R2 = 0.9974. The limit of quantitation was 0.0241 μg/mL, and the molar absorptivity coefficient 1.85x104 L.mol−1.cm−1. Sandal's sensitivity was 0.0082 μg.cm-2 There is no interference from excipients found in the tablet. The data were statistically compared with British Pharmacopoeia methods asstandard reference using Student's t-and F-test.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"59 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88118666","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}