Eczacılık Meslek Bilimleri Bölümü Makale Koleksiyonu

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https://hdl.handle.net/20.500.12713/100

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Design, Synthesis, and Biological Evaluation of Some Novel Retinoid Derivatives
(Bentham Science Publishers, 2024) Konyar, Dilan; Foto, Egemen; Foto, Fatma Zilifdar; Büyükbingöl, Mehmet Erdem
Background: As cancer stands as a significant global health concern, many heterocyclic compounds that are more effective in cancer cells than healthy cells are being investigated for their selective anticancer potentials. One such compound is fenretinide, a synthetic derivative of retinoic acid that has a broad spectrum of cytotoxic activity against primary tumor cells, cell lines, and/or xenografts of various cancers. In this context, bexarotene and its derivatives, synthesized from hybridization of the fenretinide, are expected to possess a potential anticancer activity. Objective: The objective of the present study was to investigate the synthesis of novel amid-derived and bexarotene-based compounds, as well as to assess their cytotoxic effects in different cancer cell lines. Methods: This study involved the synthesis of twelve novel retinoid derivatives (6-17) in a six-step process. The cytotoxic activities of these compounds were assessed against various cancer cell lines, such as A549 (human lung carcinoma), HeLa (human cervical cancer), MCF7 (human breast adenocar-cinoma), and WiDr (human colon adenocarcinoma). The chemical structures of these compounds were elucidated through their elemental analysis, mass spectrometry (ESI+, ESI-), as well as1H-NMR and13C-NMR spectroscopic data. Results: The obtained cell toxicity results indicated that compounds 6, 8, 11, 12, 13, 14, and 17 were found to exhibit the strongest cytotoxic activity in above mentioned cancer cell lines. The IC50 values for active compounds, 11 and 12, were determined as 2.38µM and 2.29µM, respectively. Remarkably, these compounds displayed higher cytotoxic activity in the WiDr cell line related to positive control, camptothecin (CPT). Moreover, compounds 14 and 17 demonstrated very similar level of cytotoxic activity to CPT, indicating their potential for antitumoral applications upon further studies. Conclusion: While compounds 11, 12, 14, and 17 indicated a very comparable anticancer activity to CPT, compounds 6, 8, 11 and 12 showed more selective anticancer effect against cancer cells than non-cancerous cells. In accordance with the findings of the present study, they can be evaluated as primary candidates for further studies, specifically as RXRα-targeted anticancer agents. © 2024 Bentham Science Publishers.
Metal Oxide Nanoparticles Exhibit Anti-Acanthamoeba castellanii Properties by Inducing Necrotic Cell Death
(Springer Science and Business Media Deutschland GmbH, 2024) Ahmed, Usman; Gew, Lai Ti; Siddiqui, Ruqaiyyah; Khan, Naveed Ahmed; Alharbi, Ahmad M.; Alhazmi, Ayman; Anwar, Ayaz
Purpose: The treatment of amoebic infections is often problematic, largely due to delayed diagnosis, amoebae transformation into resistant cyst form, and lack of availability of effective chemotherapeutic agents. Herein, we determined anti-Acanthamoeba castellanii properties of three metal oxide nanoparticles (TiO2, ZrO2, and Al2O3). Methods: Amoebicidal assays were performed to determine whether metal oxide nanoparticles inhibit amoebae viability. Encystation assays were performed to test whether metal oxide nanoparticles inhibit cyst formation. By measuring lactate dehydrogenase release, cytotoxicity assays were performed to determine human cell damage. Hoechst 33342/PI staining was performed to determine programmed cell death (apoptosis) and necrosis in A. castellanii. Results: TiO2-NPs significantly inhibited amoebae viability as observed through amoebicidal assays, as well as inhibited their phenotypic transformation as evident using encystation assays, and showed limited human cell damage as observed by measuring lactate dehydrogenase assays. Furthermore, TiO2-NPs altered parasite membranes and resulted in necrotic cell death as determined using double staining cell death assays with Hoechst33342/Propidium iodide (PI) observed through chromatin condensation. These findings suggest that TiO2-NPs offers a potential viable avenue in the rationale development of therapeutic interventions against Acanthamoeba infections. © The Author(s), under exclusive licence to Springer Nature Switzerland AG 2024.
Pharmacists's knowledge, attitude, and practices towards pharmaceutical and patient-centred care in asthma management: a national study
(Elsevier, 2024) Çakmak, Dilan; Bektay, Muhammed Yunus; Al-Taie, Anmar; Jadoo, Saad Ahmed Ali; İzzettin, Fikret Vehbi
Background: Asthma, a chronic respiratory disease, is effectively managed with medications, yet many patients struggle due to irregular treatment and poor adherence. Pharmacists play a crucial role in improving asthma care through pharmaceutical care (PC) services. This study aims to assess pharmacists' knowledge, attitudes, and behaviors regarding asthma PC in T & uuml;rkiye. Methods: This cross-sectional study in T & uuml;rkiye evaluated community (CP) and hospital pharmacists' (HP) knowledge level, attitudes, and behaviors regarding asthma care. A validated Asthma Pharmaceutical Care Knowledge (APCL) and Asthma Attitudes and Behaviors (AAB) questionnaires were used to assess their knowledge levels and attitudes toward asthma pharmaceutical care. Results: Out of 400 pharmacists participated the questionnaire, the majority were CP (297, 74.25 %). Both CP and HP demonstrated adequate knowledge scores, 79.39 +/- 12.32 and 80.66 +/- 12.25, respectively. APCL mean scores of CP and HP were 4.22 +/- 0.523 and 4.29 +/- 0.383. No statistically significant difference in asthma knowledge levels was observed between CP and HP. Both groups reported positive attitudes and behaviors toward asthma care, with CP scoring 4.71 +/- 0.446 and HP scoring 4.74 +/- 0.330 on the AAB questionnaire. Conclusions: This study revealed that both CP and HP have sufficient knowledge about asthma and they have positive attitudes towards providing asthma PC. Pharmacists have crucial role in asthma care with leveraging their expertise, patient interactions, and ability to referral capabilities.
Drug modifications: graphene oxide-chitosan loading enhanced anti-amoebic effects of pentamidine and doxycycline
(SPRINGER, 28.11.2024) Jabri, Tooba; Daalah, Meshal; Alawfi, Bader S.; Gul, Jasra; Ahmed, Usman; Shah, Muhammad Raza; Khan, Naveed Ahmed; Siddiqui, Ruqaiyyah; Ying, Tan Yee; Tong, Yeo Jia; Anwar, Ayaz
Acanthamoeba castellanii is the causative pathogen of a severe eye infection, known as Acanthamoeba keratitis and a life-threatening brain infection, named granulomatous amoebic encephalitis. Current treatments are problematic and costly and exhibit limited efficacy against Acanthamoeba parasite, especially the cyst stage. In parallel to drug discovery and drug repurposing efforts, drug modification is also an important approach to tackle infections, especially against neglected parasites such as free-living amoebae: Acanthamoeba. In this study, we determined whether modifying pentamidine and doxycycline through chitosan-functionalized graphene oxide loading enhances their anti-amoebic effects. Various concentrations of doxycycline, pentamidine, graphene oxide, chitosan-functionalized graphene oxide, and chitosan-functionalized graphene oxide loaded with doxycycline and pentamidine were investigated for amoebicidal effects against pathogenic A. castellanii belonging to the T4 genotype. Lactate dehydrogenase assays were performed to determine toxic effects of these various drugs and nanoconjugates against human cells. The findings revealed that chitosan-functionalized graphene oxide loaded with doxycycline demonstrated potent amoebicidal effects. Nanomaterials significantly (p < 0.05) inhibited excystation and encystation of A. castellanii without exhibiting toxic effects against human cells in a concentration-dependent manner, as compared with other formulations. These results indicate that drug modifications coupled with nanotechnology may be a viable avenue in the rationale development of effective therapies against Acanthamoeba infections.
A systematic review of improper eye drop application and role of pharmacists for patient education
(Taylor and Francis Ltd., 2025) Al-Taie, Anmar
The application of eye drop is encountered with many technique errors, which can lead to decreased therapeutic response and treatment failure. Community pharmacists can play a pivotal role in providing appropriate knowledge and counselling services for the proper and effective use of eye drop. The aim of this systematic review was to assess the most important aspects of technique errors regarding eye drop application, along with the important role and impact of community pharmacist-led interventions towards the provision of patient education and counselling regarding the proper application of this topical preparation in clinical practice. PRISMA criteria were used to conduct a systematic search on the administration of eye drop through different databases, including Scopus, Web of Science, and PubMed between the years 1990 and 2023. A total of 22 articles were included in this study. Nearly three-quarters of the studies discussed the improper technique and non-adherence for eye drop instillation (77.3%). Five studies discussed the interventions by health care professionals for proper eye drop instillation technique (22.7%). Two studies discussed the intervention by community pharmacist in patient education and improved training on the correct instillation of eye drop. There are different aspects of application errors encountered by patients while using eye drop, particularly in glaucoma elderly patients, and polypharmacy. These application errors could lead to a diverse range of complications, such as poor medication, ocular infections, increased health care expenses, reduced treatment effectiveness, and lower health outcomes. There is a potential role of pharmacist-led interventions in minimising procedures associated with improper technique and application of eye drops to avoid decreased therapeutic response and treatment failure. © 2025 Optometry Australia.
Biocompatibility and toxicity challenges of nanomaterials
(Elsevier, 2024) Yaşayan, Gökçen; Alarçin, Emine; Avcı Adalı, Meltem; İpek, Tuba Çanak; Nejati, Omid; Özcan Bülbül, Ece; Karslı, Seher; Öztürk, Ayça Bal; Mostafavi, Ebrahim
Cancer is one of the most challenging diseases to treat and is one of the leading reasons for human death worldwide. In cancer research, nanomaterials are evaluated as an encouraging system due to their promising properties, consisting of nanoscale sizes and chemical and physical configurations that can be functionalized for the final application. Although much effort has been extended to efficient cancer research, the biocompatibility and toxicity of nanomaterials remain the main challenges. Cellular reactions are correlated with the physicochemical characteristics of nanomaterials. There are several structural parameters on which nanotoxicological reactions depend, such as size, charge, surface chemistry, and morphology. Notably, understanding the challenges is highly desirable to take full advantage of the benefits provided by nanomaterials. Therefore, this chapter covers the latest biocompatibility and toxicity findings from cancer studies using nanomaterials. Moreover, this chapter demonstrates the experiences learned and challenges faced by a group of leading scientists in this discipline. Also, it covers the physical, chemical, and biological strategies to make nanomaterials more biocompatible and nontoxic.
Antikanser Adayı ve Potansiyel hEGFR İnhibitörü Olarak Yeni 1,2,4-Triazol Bileşiklerinin Sentezi ve Biyokimyasal Özelliklerinin İncelenmesi
(TÜBİTAK, 01.06.2021) Kolcuoğlu, Yakup; Şanlıer, Şenay; Akdemir, Atilla; Türe, Aslı; Bekircan, Olcay; Ustalar, Narin; Fazlı, Hilal
Çağımızın en ölümcül hastalıklarından olan kanserle baş edebilmek için, tümör hücrelerine karşı seçici olarak hedeflenmiş ilaçlar geliştirilmektedir. Bu alanda, büyük umut vadeden hedeflerden biri EGFR?dir. EGFR protein yapıda, hücre yüzeyinde bulunan bir reseptördür. Aktifleştiğinde hücre içinde sinyal iletimine ve bunun sonucunda hücre içi değişikliklere yol açar. Protein tirozin kinaz reseptörlerinden biri olan EGFR, sadece hücrenin canlılığı için gerekli biyolojik olayları kontrol etmekle kalmaz, aynı zamanda tümör büyümesi ve metastazı için gerekli olan anjiyojeneze de yardımcı olur. EGFR?yi hedef alan ajanlar kolorektal kanser, baş-boyun kanseri, akciğer kanseri, meme kanseri başta olmak üzere çeşitli kanserlerin tedavisinde yerini almış başarılı ilaçlardır. Çalışma kapsamında, in slico yöntemlerle yapılan çalışmalar sonucunda hEGFR üzerinde etkili olabilecek iskelet ve substitue gruplar belirlenerek tasarlanmış ve belirlenen bu moleküller sentezlenerek yapıları aydınlatılmıştır. Sentezlenen moleküllerin anti-hEGFR özelliklerinin incelenebilmesi için ticari olarak satın alınan enzimin optimum reaksiyon şartları belirlenmiştir. Yapılan kinetik çalışmalarla sentezlenen her bir molekül için IC50 değeri bulunmuştur. Bu moleküller içerisinden en iyi IC50 değerine sahip olan moleküller için ise inhibisyon türü araştırılmış ve bu moleküllerin Ki değerleri hesaplanmıştır. En iyi inhibisyon etkisine sahip moleküllerin ayrıca, biyouyumluluk testleri A549, CRL-5807, WI-38, OVCAR3 ve SKOV3 hücreleri üzerinde sitotoksisite çalışmaları ile belirlenmiştir.
Implications of health care providers by physicians' and pharmacists' attitudes and perceptive barriers towards ınterprofessional collaborative practices
(Univ Sao Paulo, Conjunto Quimicas, 2022) Al-Taie, Anmar
The study was aimed at assessing and comparing physicians' and pharmacists' attitudes and experiences with collaborative practices, along with the extent of barriers toward interprofessional collaboration in Iraqi healthcare settings. A descriptive, cross-sectional study was conducted among physicians and pharmacists in different healthcare settings in Baghdad, Iraq through an interview using a structured 3-part questionnaire, assessing the demographic characteristics, attitudes and barriers to interprofessional collaborative practices. A total of 384 participants were enrolled in this study. The physicians and pharmacists reported a significant positive attitudes towards collaboration, such as ''pharmacists are qualified to assess and respond to patients' drug treatment needs'' (69.8%, vs. 89.6%,; P=0.001);''pharmacists have special expertise in counseling patients on drug treatment'' (59.9%, vs. 86%; P=0.001); ''physicians and pharmacists should be educated to establish collaborative relationships'' (80.7%, vs. 100%; P=0.001), respectively. However, 57.3% of the physicians agreed about lack or inadequate of pharmacists' time to provide direct and effective patient care because of medications dispensing duties'', while 56.8% of the pharmacists disagreed about this barrier (P=0.005). Both professions reported significant, positive attitudes and shared some barriers toward collaborative practices; however, there is a disagreement in some areas in which both professions would like more collaboration for better patient care.
Comprehensive estrogenic/anti-estrogenic, anticancer, mutagenic/anti-mutagenic, and genotoxic/anti-genotoxic activity studies on chemically characterized black poplar and eurasian aspen propolis types
(Elsevier B.V., 2023) Güzelmeriç, Etil; Sipahi, Hande; Helvacıoğlu, Sinem; Düz, Gamze; Akyıldız, İsmail Emir; Hazar, Merve; Dilsiz, Sevtap Aydın; Aydın, Ahmet; Yeşilada, Erdem; Özhan, Yağmur; Hamitoğlu, Muhammed; Helvacıoğlu, Sinem; Yaman, Beril Kadıoğlu
Propolis is mainly composed of plant resins, and its type is named according to the primary plant origin in its composition. Identification of propolis botanical origin is essential for predicting and repeating its pharmacological activity because of the variations in chemical composition. This study aimed to compare chemical composition of black poplar (Populus nigra L.) type-propolis (PR1 and PR2) and Eurasian aspen (P. tremula L.)-type propolis (PR3) by liquid chromatography-tandem mass spectrometry (LC-MS/MS) technique and to evaluate their biological activity profiles. According to LC-MS/MS results, in addition to marked caffeic acid phenethyl ester content in PR1 and PR2, flavonoid aglycones such as pinocembrin, chrysin, pinobanksin, and galangin were found to be dominant in these samples. On the other hand, PR3 contained relatively high concentrations of phenolic acids such as ferulic acid, p-coumaric acid, and trans-cinnamic acid. The anti-estrogenic activity test showed that PR2 exerted the highest anti-estrogenic activity by inhibiting cell proliferation by 44.6%. All propolis extracts showed anticancer activity, which was justified by decreasing activity on the 3D spheroid size in a concentration-dependent manner. Besides, all extracts showed moderate or potent antimutagenic activity in Salmonella typhimurium TA98 and TA100 strains with and without metabolic activation, respectively. In addition, the Comet assay results revealed that propolis extracts have a geno-protective effect against H2O2-induced DNA damage in CHO-K1 cells at 0.625 and 1.25 ?g/mL concentrations. Overall, the result of this study may help in preparing standardized propolis extracts and developing products with defined pharmacological benefits in the food supplements industry. © 2023 Elsevier B.V.
Insights into patterns of knowledge, practices, and safety use of energy drinks: a cross-sectional observational study
(Wolters Kluwer Medknow Publications, 2022) Arueyingho, Oritsetimeyin; Al-Taie, Anmar
Background: Energy drinks (EDs) are largely consumed by adolescents and sports youths without understanding safety precautions and associated side effects. The aim of this study was to assess the knowledge, practices, and safety use, including the occurrence of side effects of EDs among adolescents and sports youths in Kyrenia, Northern Cyprus. Methods: This was a descriptive, cross-sectional study conducted among adolescents and sports youths in Kyrenia province, Northern Cyprus, using a structured three-part questionnaire, consisting of 22 items to assess the knowledge, practices, and safety use of EDs. Results: The most common reported adverse effects were insomnia and palpitations (24%), diuresis (18.7%), headache (17.7%), and stress (15.6%). The study participants reported a statistically significant low knowledge about the ingredients of EDs (P < 0.0001) and side effects of EDs (P = 0.05). Although statistically nonsignificant, the study participants also reported a low knowledge about ED intake during the COVID-19 pandemic. Conclusions: There is still a lack of knowledge regarding ED consumption among the adolescents and sports youths in Northern Cyprus reported by low level of knowledge about the ingredients of EDs, their potential effects, and incidence of side effects along with correct consumption during the COVID-19 pandemic which creates a barrier to healthy dietary patterns.
Synthesis, characterization, in vitro cytotoxicity of novel metallo phthalocyanines with four methylpropiophenonyl clusters and their effects on caenorhabditis elegans thermotolerance
(SPRINGER INT PUBL AG, 2022) Şenoğlu, Sema; Güleç, Meltem; Yavuz Dokgöz, Elif; Bal Öztürk, Ayça; İzbudak, Burçin; Salih, Bekir; Olgun, Abdullah; Ceyhan, Tanju
Phthalocyanines (Pcs) have the potential to be used in many medical applications. Novel Zn (II), Co (II), and Cu (II) phthalocyanines (Pcs) 4, 5, and 6, respectively, containing four methylpropiophenonyl units at the peripheral positions were described. Pcs were synthesized by cyclotetramerization of the previously prepared precursor 2-hydroxy-4'-[2-(3,4-dicyanophenoxyethoxy)]-2-methylpropiophenone 3 with the presence of metal salts under nitrogen atmosphere. The compounds were characterized by elemental analysis, IR (Infrared spectroscopy), UV-visible spectroscopy, and Laser Desorption ionization time-of-flight mass spectroscopy (LDI-TOF-MS) methods. The compounds were tested for in vitro cytotoxicity in cultured human cells, and thermotolerance in Caenorhabditis elegans (C. elegans). Standard MTT assays were carried out for cytotoxicity testing using HeLa and L929 cells. Results showed that there was no significant decrease in the cell viability with zinc (II), cobalt (II), and copper (II) phthalocyanines (ZnPc, CoPc, and CuPc) at 0.25 mu M concentration. C. elegans survival assay with ZnPc, CoPc, and CuPc under heat stress showed that although a dose-dependent statistically significant toxicity was observed for ZnPc and CuPc, CoPc was not toxic at all concentrations tested and even increased the survival of worms at the 0.050-0.250 mu M concentration range. Therefore, CoPc can be a lead compound for further preclinical studies for its potential in photodynamic therapy (PDT) and anti-aging purposes.
Reported knowledge and practices towards the proper use of patient information leaflet among university students
(INTERNATIONAL PHARMACEUTICAL FEDERATION, 2022) Al-Taie, Anmar
Background: A patient information leaflet (PIL) is a valuable tool that can convey basic information about the disease conditions and the recommended medication enabling both the patients and the health care professional to get rapid, easy, and precise access to the treatment process.Objective: To evaluate the level of knowledge and practices for appropriate and useful use of PIL among final-year medical and non-medical undergraduate university students in Baghdad, Iraq.Method: A descriptive, cross-sectional study was conducted among final-year undergraduate university students with different academic disciplines, including medical (pharmacy, dentistry) and non-medical disciplines (law, media) in Baghdad, Iraq, using a structured questionnaire to evaluate the level of knowledge and practices towards the proper use of PIL.Result: A total of 384 students enrolled in this study and the majority were medical students (59.1%). The proportion of non-medical students who read the PILs was lower than that of medical students (82.2% vs. 91.6%, p<0.0001). According to participants' responses, 84.6% (p=0.03) of the medical students stated that reading PIL was useful for accurate medication use, while 60.5% of the non-medical students reported that the language of PIL was difficult to understand. Instructions for proper medication intake were significantly higher among the medical students (78%, p<0.0001).Conclusion: An acceptable level of knowledge along with several different practices toward the proper use of PIL while taking medicines was reported among medical and non-medical undergraduate university students.
Insights into disease and pharmacotherapy knowledge of Alzheimer's disease among community pharmacists: a cross-sectional study
(TAYLOR & FRANCIS LTD, 2022) Al-Taie, Anmar; Yılmaz, Zekiye K.; Dahman, Hasan; Yardımcı, Turay
Objective To assess the knowledge level and awareness of Alzheimer's disease, including knowledge about the disease, pharmacotherapy, provision of patient education and associated factors among community pharmacists across Turkey and Northern Cyprus. Methods This was a descriptive, cross-sectional study conducted among community pharmacists working in Turkey (Group A) and Northern Cyprus (Group B). Disease and pharmacotherapy knowledge of AD were assessed using AD Knowledge Scale (ADKS), and drug treatment (KADT) scale, respectively. Results Both groups reported a moderate level of knowledge of AD, especially medically-oriented domains, with no significant difference regarding the mean ADKS domains (18.8 +/- 2.8 vs. 18.9 +/- 3.4; p = .98). Nevertheless, participants from both groups reported a good level of KADT knowledge about AD treatment (p = .03). Group A reported a statistically significant higher level of knowledge about drug interactions compared with Group B (54.6% vs. 45.8%; p = .01), and knowledge about proper information (79.6% vs. 31.8%; p = .02). There was a statistically significant KADT difference correlated with gender, those having a Master degree, more than 5 years of work experience, and those taking AD training courses. Conclusion There is still a lack of knowledge regarding AD reported by moderate ADKS score, especially in medically-oriented domains, which creates a barrier to early provision of care and preventing AD, noted with no difference among community pharmacists across Turkey and Northern Cyprus.
The potential chemo-preventive roles of Malus domestica against the risk of colorectal cancer: A suggestive insight into clinical application
(Elsevier Ltd, 2022) Köseoğlu, Aygül; Al-Taie, Anmar
Biologically active compounds in fruit-derived ingredients, particularly phytochemicals, have significant potential to modulate and mitigate many pathological processes in the development of disease conditions, including cancer. Colorectal cancer (CRC) remains a major public health issue. Nonetheless, prevention is an important step in lowering the rate of mortality from this cancer. Currently, the link between apple consumption and improved health is becoming remarkably evident and is reported to be beneficial for human health. Phytochemicals, such as flavonoids and other polyphenol compounds extensively available in apple fruits, have well-known positive effects on health outcomes and the potential to combat and prevent the development of CRC, including antioxidant, anti-proliferative, and anti-carcinogenic effects. This review describes the bioactive compounds derived from apple fruits, particularly the polyphenols and flavonoids, their proposed mechanisms responsible for their bioactive properties and health-promoting attributes that could provide potential chemo-preventive effects against the risk of CRC development. The conclusion of the review provides insights into the potential effects of apple-derived bioactive compounds and proposes the need for more clinical studies in large trials for future strategies regarding the valuable effects of apple phytochemicals, which might be therapeutic candidates in the campaign against CRC.
Antioxidant, antimicrobial, anti-urease and cytotoxic activities of various extracts from Scutellaria sibthorpii endemic to Cyprus
(NATL INST SCIENCE COMMUNICATION-NISCAIR, 2022) Toplan, Gizem Gülsoy; Taşkın, Turgut; Öztaş, Ezgi; Hacıoğlu, Mayram; Tufan, Selin; Sarıyar, Günay; Mat, Afife
Lamiaceae is one of the largest families in the plant kingdom. Including the genus Scutellaria whose species are used in traditional medicine in various countries for prevention and also the treatment of several disorders. In vitro biological activities of the various extracts of the aerial parts from Scutellaria sibthorpii were investigated in the present study. Antioxidant activity of the extracts was measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS assays and ferric reducing antioxidant power (FRAP) assays. Cytotoxic potential and anti-urease activities of the extracts were also determined. Spectrophotometric analysis was used to establish the total phenol content of the extracts. The antibacterial activities of extracts were assessed by minimal inhibitory concentration (MIC) against seven bacteria and Candida albicans. Regarding the results, infusion showed considerable antioxidant properties in three method (IC50 value 0.133 +/- 0.0005(DPPH), 26.54 +/- 0.05 mM trolox/mg extract(ABTS), 8.76 +/- 0.1 mM Fe+2/mg extract (FRAP)). Other extracts exhibited high-to-moderate antioxidant effects. Among the studied samples, the infusion had the highest total phenolic content (0.0295 +/- 0.0002 mg GAE/mg extract). According to cytotoxicity results, n-hexane extract had strong cytotoxic effects against PC-3 and NIH/3T3 cell line with IC50 values of 330.40 mu g/mL and 340.85 mu g/mL, respectively. In the antibacterial activity screening, the ethyl acetate extract showed higher activity against Enterecocus facecalis, Klebsiella pneumoniae, Proteus mirabilis with 625 mu g/mL MIC value. According to the research carried out, it would seem that this is the first study on screening biological activities of extracts from Scutellaria sibthorpii. These findings indicate that these endemic species from Cyprus could be used in phytopharmaceutical preparation.
A scoping systematic assessment for post-marketing abuse drug withdrawal
(OXFORD UNIV PRESS, 2022) Al-Taie, Anmar; Büyük, Ayşe Şeyma; Şardaş, Semra
Objectives The aim of this study was to identify the post-marketing withdrawal of medicines due to their adverse drug reactions (ADRs)-related abuse effects and to examine the types of evidence, mechanisms and patterns for the withdrawal decisions after their approval across different geographical regions. Methods By searching through different databases that focused on withdrawn drugs due to their ADRs-related abuse effects between 1930 and 2021 that could provide findings of evidence used in making withdrawal decisions based on the tools of the Oxford Centre for Evidence-Based Medicine (OCEBM) criteria alongside sources derived from authorities based on their withdrawal. The outcomes were categorized, and the average time between the launch date of exposure and withdrawal was calculated and stratified. Key findings A total of 33 abused withdrawn drugs. The withdrawals occurred between 1961 and 2007. Psychostimulant drugs accounted for most of the abuse withdrawals (42.4%). Most of the withdrawals occurred between 1981 and 1990 (n = 18, 54.5%). Most withdrawn drugs were in Europe (41, 46.6%) with a minimum withdrawal period of 5 years and an average time of withdrawal of 28.8 years. Conclusions Psychostimulant drugs presented the most abuse withdrawals based on the evidence of case-control studies, and the most withdrawals were in Europe. The duration of withdrawn drugs was different from region to region in different continents. More intensive research is required to further reduce the time duration between drug marketing and withdrawal, which will help improve decision-making processes with favourable benefit-risk ratio outcomes.
The long view on COVID-19 theranostics and oral antivirals: living with endemic disease and lessons from molnupiravir
(Atypon, 2022) Al-Taie, Anmar; Denkdemir, Fatma Rana; Büyük, Ayşe Şeyma; Şardaş, Semra
The long view on living with COVID-19 as an endemic disease calls for expanding the planetary health inter-vention toolbox. We will need a battery of vaccines, small molecule oral antiviral drugs, and biomarkers toforecast antiviral drug efficacy and safety. In this context, theranostics refers to fusion of therapeutics and diag-nostics. We examine here emerging pathways to theranostics innovation for COVID-19 oral antiviral drugs,with molnupiravir as a case study. With new virus variants (1) variations in the molnupiravir efficacy target,viral RNA-dependent RNA polymerase, (2) variability in pharmacokinetics and exposure to molnupiravir activemoiety in fluids on virus entry points to the host (e.g., saliva, tears, and nasal secretions), (3) variability intransformation from prodrug molnupiravir to its active form, and (4) variability in putative adverse effects onhuman/host cells, all warrant attention for prospects and challenges vis a`vis theranostics innovation forCOVID-19 oral antivirals. The emerging lessons from molnupiravar are of interest to future design of COVID-19theranostic research with other oral antiviral medications. Regulatory agencies, the pharmaceutical industry,research funders, governments, and ministries of health around the world have important stewardship roles toadvance the subpopulation level analyses of clinical trial data on oral antiviral drugs for COVID-19. This wouldremedy the current lag in clinically relevant multiomics theranostics for oral antivirals in the battle againstCOVID-19.
Comparative Studies on Essential Oil and Phenolic Content with In Vitro Antioxidant, Anticholinesterase, Antimicrobial Activities of Achillea biebersteinii Afan. and A. millefolium subsp. millefolium Afan. L. Growing in Eastern Turkey
(2022) Toplan, Gizem Gülsoy; Taskın, Turgut; Iscan, Gokalp; Goger, Fatih; Kurkçuoglu, Mine; Civas, Ayşe; Ecevit-Genc, Gulay; Mat, Afife; Baser, Kemal Husnu Can
The potential applications of Achillea species in various industries have encouraged the examination of their phytochemical components along with their biological potential. In the present study, phenolic contents and essential oil compositions together with the in vitro biological activities of the aerial parts from Achillea biebersteinii Afan. and Achillea millefolium subsp. millefolium Afan. collected from Turkey were evaluated. Different solvent extracts (n-hexane, chloroform, methanol, water) were prepared and their antimicrobial, anticholinesterase, and antioxidant activities were studied. The LC-MS/MS results revealed the presence of 16 different phenolic compounds, including chlorogenic acid, rutin, quercetin, and luteolin glycosides, in methanolic extracts. According to GC-FID and GC/MS results, the primary components of the oils were identified as 1,8-cineole (32.5%), piperitone (14.4%), and camphor (13.7%) in A. biebersteinii and 1,8-cineole (12.3%) and ?-eudesmol (8.9%) in A. millefolium subsp. millefolium. The infusion and methanolic extracts of both species were found to be rich in their total phenolic content as well as their antioxidant and anticholinesterase activity. In contrast, the n-hexane and chloroform extracts of both species showed strong antimicrobial activity with MIC values ranging from 15 to 2000 ?g/mL. Our findings suggest that the investigated Achillea species could be evaluated as potent natural agents, and further studies into the promising extracts are needed.
Phytochemical screening and biological evaluation of Salvia hydrangea Dc. ex Benth. growing in eastern Anatolia
(Elsevier B.V., 2022) Gülsoy Toplan, Gizem; Kürkçüoğlu, Mine; Göger, Fatih; Taşkın, Turgut; Civaş, Ayşe; İşcan, Gökalp; Ecevit Genç, Gülay; Mat, Afife; Başer, K.Hüsnü Can
Salvia species have lately gained significant interest as a result of their suitable utilization in various industries. In the current study, S. hydrangea, one of the most consumed sages in the eastern region of Turkey, has been evaluated for phytochemical composition as well as in vitro pharmacological potential comparatively for the first time. The phytochemical composition of S.hydrangea was investigated by LC-MS/MS, GC-FID, and GC/MS. To reveal its biological activities, antioxidant, antimicrobial, and also acetylcholinesterase activities of different solvent extracts such as water, n-hexane, chloroform, and methanol were determined. According to GC/MS analysis, the primary components of the oil were identified as camphor (46.0%), 1,8-cineole (7.5%), camphene (6.8%), limonene (6.5%), a-pinene (5.6%) and b-pinene (6.1%). Additionally, in the infusion and methanol extract, rosmarinic acid and luteolin glycoside were detected as predominant phenolics by LC-MS/MS. In DPPH·, CUPRAC, and FRAP test results of the samples indicated strong to moderate antioxidant ability in all samples studied, additionally, among them, the infusion exhibited significant acetylcholine inhibition properties comparable with galanthamine. With regard to antimicrobial activity, all of the tested microorganisms had MIC values ranging from 15 to 2000 µg/mL. Based on these findings, S. hydrangea may have promising properties for a variety of industrial applications in the pharmaceutical, food, and cosmetic industries. © 2022 SAAB
Phytochemical composition and pharmacological activities of Teucrium polium L. Collected from eastern Turkey
(TUBITAK, 2022) Gülsoy Toplan, Gizem; Göger, Fatih; Taşkın, Turgut; Ecevit-Genç, Gülay; Civaş, Ayşe; İşcan, Gökalp; Kürkçüoğlu, Mine; Mat, Afife; Başer, K. Hüsnü Can
Teucrium species that belong to the family Lamiaceae have been traditionally used for their medicinal properties. T. polium is one the most widespread members of the genus for its use in the treatment of several diseases. In this study, the essential oil and phenolic composition of the aerial parts from T. polium were assessed by GC-FID, GC/MS, and LC-MS/MS as well as for its total phenolic content. Several extracts such as n-hexane, chloroform, methanol, and infusion were prepared and their antimicrobial, antioxidant, and also acetylcholinesterase activities were studied. According to GC/MS results, ß -caryophyllene (8.8%), t-cadinol (6.2%), (E)-nerolidol (5%), ? -cadinol (5.4%), and a-pinene (4.7%) were identified as main constituents of the essential oil. LC MS/MS analysis of the infusion and the methanol extract showed the presence of 15 phenolic compounds. Moreover, the total phenolic content of each sample was also determined and the infusion had the highest percentage of phenolics. To evaluate the antioxidant properties, the samples were tested by using DPPH” free radical scavenging, FRAP, and CUPRAC activity methods. The infusion showed the strongest radical scavenging activity, whereas n-hexane and chloroform extracts exhibited considerable reducing power effects. The MIC values for all of the examined microorganisms ranged from 15 to 2000 µg/mL with respect to antimicrobial activities. © TÜBİTAK

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