Eczacılık Fakültesi Eczacılık Meslek Bilimleri Bölümü Koleksiyonu

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Cytotoxicity of endemic Haplophyllum megalanthum Bornm. and its newly isolated alkaloids and lignans
(Elsevier Ltd, 2024) Demir, Serhat; Petersen, Malene Johanne; Kjaerulff, Louise; Somer, Nehir Unver; Staerk, Dan
In this study, two previously unreported lignans [4′-O-demetylsuchilactone-8′-ol (1), 7-O-(3-methyl-2,3-dihydroxy-butyl)isodaurinol] (2), four new alkaloids (haplomegalanthine (3), megalantin (4), megalanthamide (5), glycoisohaplopine (6) and thirty-five known compounds (7–41) were isolated from Haplophyllum megalanthum Bornm. (Rutaceae). Pinoresinol (23), epipinoresinol (24), indole-3-carbaldehyde (29), N-[2-(4-hydroxyphenyl)ethyl]-3-methylbut-2-enamide (34), 7,8-dimethoxyfuroquinoline-4-one (35), cis-khellactone (36), 4,4′-dihydroxy-3,3′,9-trimethoxy-9,9′-epoxylignan (37), ulopterol (39) and trans-decursidinol (40) were identified for the first time in the genus Haplophyllum. Also, 4′-O-demethylsuchilactone (16) and N-(4-hydroxyphenethyl)benzamide (32) were found for the first time within the family Rutaceae. Structures of the compounds were elucidated by the use of HRMS, UHPLC-MS and 1D/2D NMR analyses. Furthermore, cytotoxic activity of the crude extract and previously unreported compounds (1–3, 5, 6) on colon cancer cell line HT29 were tested by the MTT method. IC50 values were determined for these five compounds and the crude extract as 18.48 ± 0.94 μg/ml, 52.62 ± 7.27 μg/ml, 23.15 ± 6.70 μg/ml, 21.45 ± 2.48 μg/ml, 5.06 ± 0.19 μg/ml and 2.82 ± 0.012 μg/ml, respectively. The present report is the first detailed phytochemical investigation of the title plant pointing out that it comprises a rich source of diverse chemical constituents including new compounds with promising cytotoxic activity.
Some heterocycles connected to substituted piperazine by 1,3,4-oxadiazole linker: Design, synthesis, anticholinesterase and antioxidant activity
(Elsevier B.V., 2025) Kurt, Zuhal Kılıç; Konyar, Dilan; Okur, Hayati; Kaplan, Alevcan; Boǧa, Mehmet
AD is a multifactorial neurodegenerative disease that has caused morbidity and mortality on a global scale. Currently, there are only a few drugs used in the treatment of AD. Although many compounds that aim at new targets have reached clinical trials, none have been approved. However, discovering efficient drugs for AD treatment is one of the biggest challenges for pharmaceutical research and requires strong support. In this paper, we aim to design a series of indole, benzothiophene, and thiophene bearing 1,3,4-oxadiazole linker to the piperazine basic center and evaluate for their antioxidant and inhibitory activity against both cholinesterase enzymes. Among the compounds, 6a, 7b, and 8b exhibited moderate cationic radical scavenging activities with IC50 values ranging from 20.39 to 30.10 μM. The inhibitory activity results revealed that compounds 5c (IC50 for AChE = 53.91 μM and for BChE = 55.81 μM) and 6c (IC50 for AChE = 54.42 μM and BChE = 45.82 μM) bearing 2-fluorophenyl piperazine moiety showed both AChE and BChE inhibition with moderate IC50 values. To explore the binding properties of the target compounds into the active site of the enzyme, a molecular docking study was carried out using MOE software. The docking study showed that compound 6c targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE/BChE and formed important interactions with key residues. Moreover, theoretical physicochemical properties of the best active compound 6c were calculated by the SwissADME web service. It obeyed Lipinski's rule of five and had high GI absorption (gastrointestinal absorption) and good permeating to the blood-brain barrier (BBB). The compound 6c can be considered a promising compound and provides us directions for further research of anti-AD agent development.
A comprehensive study on chemical and biological investigation of thymus brachychilus jalas: A rich source of ursolic and oleanolic acids
(Taylor & Francis Inc, 2023) Akdeniz, Mehmet; Yiğitkan, Serkan; Yılmaz, Mustafa Abdullah; Yener, İsmail; Varhan Oral, Elif; Fırat, Mehmet; Orhan, İlkay Erdoğan
The significance of Thymus species in the scientific community is growing steadily due to their extensive utilization in traditional medicine, food industry, and pharmaceutical sector, owing to their abundance in essential oil and phytochemical content, rendering them commercially significant species. The current work focuses on conducting a comprehensive analysis of the ethanol extract and essential oil derived from the root and aerial portions of Thymus brachychilus Jalas, an endemic species that has not been previously investigated. Additionally, a novel GC-MS (gas chromatography-mass spectrometry) technique was developed to quantify the levels of triterpenoids, which are frequently found in many plants, particularly those belonging to the Lamiaceae family. The approach was then used to assess the triterpenoid content of the species. While the phenolic content of the species was determined by LC-MS/MS (liquid chromatography-tandem mass spectrometry), the chemical composition of triterpenoid, essential oil and flavor (aroma) of the plant was determined by GC-MS. Eucalyptol was the primary ingredient in both the essential oil and the flavor, accounting for 11.05% and 12.35%, respectively. In the DPPH and ABTS radical scavenging techniques, the root ethanol extract exhibited the greatest antioxidant activity with IC50 values of 26.70 +/- 0.23 and 19.16 +/- 0.11 mu g/mL, respectively. There was a high level of urease (59.54 +/- 1.67% at 100 mu g/mL) inhibitory activity observed in the root ethanol extract in enzyme inhibition assays, as well as angiotensin (94.80 +/- 0.56%), elastase (40.19 +/- 0.39%), and collagenase (48.26 +/- 0.12%) inhibition in the aerial ethanol extract. Moreover, the MCF-7 cell line for breast cancer had a strong cytotoxic impact when exposed to the essential oil of the species (vitality%: 1.45 +/- 0.01 at 200 mu g/mL. The LC-MS/MS and GC-MS studies revealed that the roots had a significant concentration of rosmarinic acid (15,801 mu g analyte/g extract), but the aerial portions had a substantial quantity of ursolic acid (152,374 mu g analyte/g extract). The plant exhibits potential in the food, cosmetic, and pharmaceutical sectors on account of its elevated levels of rosmarinic and ursolic acid, superior antioxidant capacity, and angiotensin and urease inhibitory effect.
Hypoglycemic potential of 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives
(Dicle University, 2023) Bingül, Murat; Şahin, Hasan
The hybrid molecules, derived from biologically active compounds, have been an open target for the medical researchers due to the possible enhanced biological properties. Hybridization of biologically active compounds for the determination of new possible candidates for drug development has been an attractive idea and allow to detect new successful compounds for drug discovery. With respect to this idea, previously synthesized dimethoxyindole based thiosemicarbazones have been chosen as hybrid molecules derived from indole backbone and thiosemicarbazides which have heavily been used for biological studies and evaluated for inhibition of α-amylase and α-glucosidase to exhibit the hypoglycemic potential. The targeted molecules were found to be potent candidates for α-glucosidase enzyme inhibition compared to the standard. The inhibition potential for α-amylase was not comparable with the acarbose with the studied concentration, however, it was determined that the targeted compounds could be selective candidates for glucosidase enzyme inhibition and the future studies were directed for the identification new compounds for this purpose.
The computational and biological investigation of indole and quinoline based thiosemicarbazones towards ?-glucosidase enzyme inhibition
(Gaziantep University, 2022) Bingül, Murat; Şahin, Hasan
Thiosemicarbazones are important classes of Schiff base ligands due to the presence of conjugated N-N-S system providing an important therapeutic potential and have been the subject of many structural and medicinal studies via the interactions of biomolecules. A wide variety of heterocyclic systems have been used for the structural modifications of new thiosemicarbazone based compounds. Due to the presence of the indole and quinoline structures in many natural products, studies have been directed towards investigations of the biological properties of natural indolic and quinolic compounds, and a range of medical uses has been identified. In the present work, the synthetic procedures and chemical characterization of the targeted compounds derived from indole-3-carbaldehyde and 2-chloroquinoline-3-carbaldehyde systems with a range of thiosemicarbazides. The final compounds have been subjected to α-glucosidase enzyme inhibition assay to investigate the antidiabetic efficiency. A complementary study was carried out with the molecular docking study of targeted compounds on the catalytic side of the designated enzyme. The biological aspect of the study revealed that the indole-based compounds possessed more promising potency compared to the quinoline derivatives.
In-vitro anti-alzheimer activity of kırktekesakalı (Scorzonera pygmaea Sibth.&Sm.)
(Asos Yayınevi, 2021) Şahin, Hasan; Boğa, Mehmet; Sarı, Aynur
Scorzonera L. cinsinin 50‘den fazla türü Türkiye‘de doğal olarak yetiĢmektedir. Asteraceae familyasına ait bu cinsin üyeleri dünyanın birçok bölgesinde hem gıda hem de halk ilacı olarak kullanılmaktadır. Bu çalıĢmada Türkiye‘nin endemik bitkilerinden olan Scorzonera pygmaea Sibth.&Sm. türünün anti-Alzheimer aktivitesi konu edilmiĢtir. Bitkinin kök (SPR) ve toprak üstü (SPH) kısımlarından elde edilen etanol ekstresi artan polariteye dayalı olarak sırasıyla petrol eteri (PE), kloroform (CH), etil asetat (EA) ve n-butanol (BU) ile tüketilmiĢtir. Elde edilen bu ekstrelerin in-vitro asetilkolin esteraz (AChE) ve butirilkolin esteraz (BChE) enzimlerini inhibisyonları Ellman yöntemi ile araĢtırılmıĢtır. Her iki enzim için pozitif standart olarak galantamin (G) kullanılmıĢtır. Hem AChE hem de BChE inhibisyonunda en potent ekstre sırasıyla % 59,72 (G: % 88,21) ve % 64,10 (G: % 81,80) inhibisyon ile SPR-CH olarak bulunmuĢtur. Ayrıca CH ekstreleri BChE‘a karĢı az da olsa daha spesifik iken kalan tüm ekstrelerin daha çok AChE‘a karĢı daha aktif olduğu gözlenmiĢtir. Bunlar içinde özellikle PE ekstrelerinin bu iki enzime karĢı olan afinitelerindeki fark kayda değerdir. Ayrıca bitkiden yaklaĢık 5 yıl önce elde edilmiĢ olan aynı ekstrelerin 4-8 °C‘deki stabilitelerini test etmek için yeni hazırlanan ekstrelerle beraber eski ekstrelerin de AChE inhibisyonları ölçülmüĢtür. Yeni ekstrelerin aksine bunların hiçbirinin aktivite göstermediği belirlenmiĢtir. Bu bağlamda bitkinin kurutulmuĢ halde, oda sıcaklığında, nem, ısı ve ıĢıktan korunarak saklanmasının AChE inhibisyonu açısında daha uygun olduğu anlaĢılmıĢtır. Sonuç olarak bitki orta derecede AChE, BChE inhibitör aktivitesine sahiptir ve bu etkilerden sorumlu bileĢiklerin tespit edilmesi için CH ekstreleri üzerinde ileri fitokimyasal çalıĢmalara ihtiyaç duyulmaktadır.
Uçucu yağlarda güvenlik riskleri: Aromaterapide madalyonun diğer yüzü
(Dicle Üniversitesi, 2022) Şahin, Hasan; Doğan, Nesrin
Uçucu yağlar bitkilerin farklı kısımlarından elde edilen aromatik ve uçucu sıvılardır. Genelde distilasyon ile elde edilen bu sıvılar terpenik, aromatik bileşikler, azot ve kükürt taşıyan bileşikler, fenilpropan türevleri gibi sekonder metabolitler taşırlar. İnsanlık tarihi boyunca bu yağların kullanımına büyük ilgi gösterilmiştir. Günümüzde uçucu yağların başta aromaterapi kapsamında farmasötik endüstride olmak üzere gıda, parfümeri, kozmetik ve temizlik endüstrilerinde geniş kullanım alanı bulunmaktadır. Son yıllarda doğal terapötiklere olan ilgi artışı aromaterapi ve uçucu yağlara da yansımıştır. Hem bu yoğun ilgi hem de konu ile ilgili yasal düzenlemelerdeki eksiklikler insanların uçucu yağlarla ilişkili güvenlik risklerine maruz kalma ihtimallerini arttırmıştır. Bu çalışmada Türkiye‘deki eczanelerde, aktarlarda, çevrimiçi platformlarda aromaterapi kapsamında en sık yararlanıldığı bildirilen 50 uçucu yağın güvenlik riskleri yapılan literatür taraması ile araştırılmıştır. Cilt hassasiyeti başta olmak üzere, kanserojenite, fototoksisite, teratojenite, nörotoksisite ve solunum depresyonunu içeren 60’tan fazla güvenlik riski tespit edilmiştir. Neredeyse tüm uçucu yağların subkronik ve kronik toksisite çalışmalarının olmadığı, yaygın olarak kullanılan limon otu, tarçın, ıtır, paçuli, zencefil, mayıs papatyası gibi uçucu yağların birçok ilaç ile etkileşim potansiyeli taşıdığı da belirlenmiştir. Bu bildirinin, aromaterapinin yasal boyutunun güçlendirilmesi, etkin ve güvenli bir biçimde uygulanması için eczacılık, tıp, hemşirelik gibi meslek gruplarının ortak çalışmasına bir çağrı niteliğinde olması ümit edilmektedir
Diyarbakır ili Kulp ilçesinde yaygın olarak kullanılan yenilebilir yabani bitkiler
(Kriter Yayınevi, 2023) Subaşı, Fatoş Şekerciler; Şahin, Hasan; Demir, Serhat
Diyarbakır ili Kulp ilçesinde yürütülen bu etnobotanik çalışma ile 18 farklı familyaya ait toplamda 37 yenilebilir yabani bitki türü kayıt altına alınmıştır. Belirlenen türlerin bilimsel botanik bilgileri, yöresel ve Türkçe isimleri, kullanılan kısımları ile kullanım yolları Tablo 1’de verilmiştir. Belirlenen türler arasında herhangi bir endemik bitkiye rastlanmamıştır. Bitkilerin büyük kısmının Rosaceae (%19), Asteraceae (%11), Apiaceae (%8) ve Lamiaceae (%8) familyalarına ait oldukları görülmekle beraber tüm bitkilerin familya dağılımı Şekil 1’de verilmiştir. Bitkilerin çoğunlukla bahar aylarında ortaya çıkan taze toprak üstü kısımları kullanılmaktadır. Bununla beraber, yaprak, tohum, meyve, gövde, çiçek, yumru, soğan gibi kısımlarından da yararlanılmaktadır. Yöre halkının bu bitkileri yemek, salata, börek, turşu, sirke, peynir yapımında ve baharat, çerez, çay, kahve, sakız olarak kullandıkları görülmüştür. Yemek yapımında sıklıkla kullanılan yöntemler haşlama, kavurma, haşladıktan sonra kavurma, sarma, pilav ya çorbalara ekleme şeklindedir.
Geleneksel/tamamlayıcı tıp ve tıbbi çaylar
(Orient, 2022) Şahin, Hasan
Hastalıklar insanlık için her zaman bir sorun olmuştur. Zira güncel bilim bizlere hastalık etkeni mikroorganizmaların insandan önce de dünyada bulunduğunu göstermektedir. Bu durumda ilk insan dahi hastalıklarla mücadele etmek zorunda kalmış olmalıdır. Bu anlamda tedavi uygulamaları tarihinin insanlık tarihi ile eş zamanlı olduğu söylenebilir. Bu uygulamaların önceleri iç güdüsel ve mistik daha sonra ise ilk ikisi ile karışık ampirik olarak yapıldığı düşünülmektedir. Özellikle ampirik dönemdeki uygulamaları yapan kişiler bir anlamda tıp ve eczacılığın da ilk nüvesini oluşturmuşlardır. Bu nüvenin oluşumuna dair ilk verilerin elde edilebildiği en eski tarih ise şimdilik M.Ö. 55.000 olarak görünmektedir. Bu tarihe ait olduğu düşünülen ve günümüzde Irak’ın kuzeyinde bulunan Şanidar Mağarası’ndaki ondan fazla Neandertal kalıntının çevresinde birçok farklı tıbbi bitkinin polen kalıntılarına rastlanmıştır. Bu durum o topluluk içerisinde çevrede yetişen tıbbi bitkilerden faydalanıldığını düşündürmektedir
Diyarbakır’dan toplanan Tragopogon longirostris Bisch. ex Schultz Bip. türü üzerinde farmakognozik araştırmalar
(Bitkisel İlaç Hammaddeleri Toplantısı, 2022) Şahin, Hasan
Asteraceae familyasına ait Tragopogon L. cinsi dünya üzerinde yaklaşık 150 tür ile temsil edilmekte olup dünyanın farklı bölgelerinde ‘salsify’ adı altında sebze olarak tüketilmektedir. Türkiye’de 25 taksonu yetişen bu cinsin üyeleri Türkçe ’de genel olarak Yemlik veya Teke Sakalı olarak bilinirler. Diyarbakır ve çevresinde “sıpıng” olarak adlandırılan T. longirostris Bisch. ex Schultz Bip. türünün taze sürgünlerinden hem sebze hem de geleneksel ilaç olarak yararlanılmaktadır[1-3]. Bu çalışmada Diyarbakır’dan toplanan bu türün toprak üstü kısmı etanol kullanılarak perkolasyon yöntemi ile ekstre edilmiştir. Elde edilen EtOH ekstresi ise sırasıyla petrol eteri (PE), etil asetat (EA) ve n-butanol (BuOH) kullanılarak fraksiyonlandırılmıştır. Drogun terpenik bileşiklerinin araştırılması amacıyla PE fraksiyonu GC-MS yöntemi ile incelenmiş ve Lup-20(29)-en-3-ol-asetat-(3β)- majör olmak üzere; Stearik asit-3-(oktadesiloksi)-propil ester, Lup-20(29)-en-3-ol-(3β)-, α-amyrin, 13,27-sikloursan-3-ol-asetat-(3β, 13β, 14β)-, 9,19-siklolanost-24-en-3-ol-asetat, pregnane-3,11,20-trion-(5β)-, androstan-17-ol-asetat-(5α, 17β)-, Lup-20(29)-en-3,28-diol-(3β)- varlığı tespit edilmiştir. Bu cinste antidiyabetik amaçlı geleneksel kullanımın yaygın olması göz önüne alınarak fraksiyonların α-amilaz ve α-glukozidaz enzim inhibitör aktiviteleri in-vitro kolorimetrik yöntemlerle ölçülmüştür. Akarbozun (IC50 – Amilaz - 0,063 µg/mL, IC50 – Glukozidaz - 667,4 µg/mL) pozitif kontrol olarak kullanıldığı bu çalışmada 500 µg/mL konsantrasyona kadar herhangi bir aktivite gözlenmemiştir. Bu durum potent α-glukozidaz inhibitörü triterpen olarak bildirilen oleanolik asit ve türevlerinin[4] PE fraksiyonunda tespit edilememesi ile uyumlu görünmektedir. Türün fenolik bileşiklerinin aydınlatılması için EA fraksiyonu üzerinde yürütülen izolasyon çalışması ile preliminer biyoaktivite (tripsin, lipoksijenaz, üreaz, tirozinaz, asetil/butiril kolin esteraz enzim inhibisyonları) çalışmaları devam etmektedir. Anahtar Kelimeler: Tragopogon longirostris, sekonder metabolit, biyoaktivite, terpenik bileşik, α-amilaz, α-glukozidaz Kaynaklar 1 Gültepe M., Coşkunçelebi K., Makbul S., Güzel M.E., Contribution to the taxonomy of little known Tragopogon species endemic to Turkey, Nord. J. Bot. 2021; 39. 2 Abdalla M.A., Zidorn C., The genus Tragopogon (Asteraceae): A review of its traditional uses, phytochemistry, and pharmacological properties, J. Ethnopharmacol. 2020; 250, 112466. 3 Altundag E., Ozturk M., Ethnomedicinal studies on the plant resources of east Anatolia, Turkey, Procedia Soc Behav Sci. 2011: 19, 756-777. 4 Teng H., Yuan B., Gothai S., Arulselvan P., Song X., Chen L., Dietary triterpenes in the treatment of type 2 diabetes: To date, Trends Food Sci Technol. 2018; 72, 34-44.
60 yıldır yayınlanan bir eczacılık dergisi ve mesleğimize katkısı
(Mersin Üniversitesi, 2014) Şahin, Hasan; Mat, Afife
Tüm meslek tarihlerinde olduğu gibi eczacılık tarihinde de meslek dergileri önemli bir yere sahiptir. Türkiye’de bu dergilerden önemli bazılarını; Resimli Eczacı Gazetesi (1924-1926), Türk Eczacı Âlemi (1927-1931), Farmakolog (1931-1954), Folia Pharmaceutica (1949-1968) şeklinde sıralayabiliriz. Bu çalışmada ise İstanbul Üniversitesi Eczacılık Fakültesi’nde Prof. Dr. Kasım Cemal Güven tarafından 1954 yılından bu yana yayınlanmakta olan ve yayın hayatı boyunca; Eczacılık Bülteni, Eczacılık Mecmuası, Acta Pharmaceutica Turcica, Acta Pharmaceutica Scientia isimlerini alan, meslek dergisi konu edilmiştir. Dergide, bilimsel çalışmaların yanında, eczacılıkta mesleki örgütlenme, etik, dönemin eczanelerinin durumu, ilaç reklamları, fiyat listeleri, eczacılık açısından önemli şahsiyetler, eczacılıkla ilgili yasal düzenleme ve değişiklikler, meslekte uluslararası gelişmeler gibi başlıklar da bulunmaktadır. Türkiye’nin en uzun süreli bu meslek dergisi yıllar içinde geçirdiği değişimler ve Türk eczacılık tarihine sağlayabileceği katkılar açısından incelenmiştir.
Chamazulene content and hypoglycemic potential of matricaria chamomilla L. samples collected from six different localities of Diyarbakır/Türkiye
(Adıyaman Bilimsel Araştırmalar Derneği, 2023) Şahin, Hasan; Tunç, Ramazan; Subaşı, Fatoş Şekerciler
Chamomile (Matricaria chamomilla L.) is one of the oldest and most widely known medicinal plants belonging to Asteraceae family. An artifact named chamazulene forms from the sesquiterpene structured lactones such as matricin during the hydro-distillation of flowering tops of chamomile. These compounds are associated with the anti-inflammatory potential of chamomile along with flavonoids, other sesquiterpenoids, and essential oil of the plant. However, not all M. chamomilla specimens grown in different regions or species known and used as chamomile contains sesquiterpene lactone components. Thus, chamazulene content of chamomile has become a pharmaceutical interest. A traditional and well-established indication of the plant is diabetes. Protective and beneficial effects of chamomile on diabetic complications and glycemic control have been proposed by several studies. However, the mechanism of action is yet to be elucidated. Flowering tops of chamomile samples were collected from six different localities of Diyarbakır/Türkiye. Essential oils (EOs) were obtained by hydro-distillation. Petroleum ether (PE), ethyl acetate (EA), methanol (Me), and infusion (INF) extracts were prepared. Qualitative analysis of the EOs resulted in no chamazulene content. Bismil district might be eligible for medicinal chamomile culture with its high essential oil yield. In-vitro hypoglycemic potentials of the extracts and EOs were evaluated by α-glucosidase inhibitory assay. All EOs and EA extracts (except M4-Bismil samples) showed the highest inhibitory activities comparable to that of standard acarbose. α-Glucosidase inhibition might be a significant mechanism of action contributing to the antidiabetic effects of chamomile
Chemical and Biological Perspectives of Monoterpene Indole Alkaloids From Rauwolfia species
(Elsevier, 2018) Boğa, Mehmet; Bingül, Murat; Özkan, Esra Eroğlu; Şahin, Hasan
The biosynthesis of monoterpene indole alkaloids (MIAs) starts with a geraniol for the terpenoid portion. Secologanin, a secoiridoid glycoside, is derived from 10-hydroxygeraniol, produced in the presence of geraniol 10-hydroxylase. The indole portion of MIAs contain tryptamine, produced by the decarboxylation of tryptophan. Conjugation of secologanin with tryptamine is achieved with strictosidine synthase to produce strictosidine. Over 2500 known MIAs found in many plants from several families, such as Apocynaceae, Loganiaceae, Rubiaceae, and Nyssaceae, are produced by modification of strictosidine. A number of pharmacologically active compounds, namely, reserpine, ajmalicine, ajmaline, serpentine, and yohimbine, isolated from different Rauwolfia species, are examples of MIAs
Attitudes and perceptions of pharmacy students toward pharmacognosy and related competencies of the national core education program in Türkiye
(İstanbul Üniversitesi, 2023) Şahin, Hasan; Gökkaya, İçim; Yazıcı, Nurdan
Background and Aims: Competency-based education (CBE) and the use of natural health products have been increasingly discussed in pharmacy. The national core education program of Türkiye has 108 mandatory competencies. This study investigated pharmacy students’ thoughts about pharmacognosy and their preparedness to provide related competencies. Methods: A descriptive online survey consisting of a 35-item questionnaire was administered to pharmacy students in Türkiye between June and July 2023. A 3-point Likert scale was used to assess students’ opinions. Data were analyzed using SPSS 23.0 (P < 0.05). Results: A total of 404 students in the third, fourth, and fifth years from 19 different faculties participated in the study. The interest in pharmacognosy was high, and students attributed significant value and importance to the field. Most of the students believed that their pharmacognosy education (67.1%) is sufficient, particularly on herbal medicinal plants (62.4%) and traditional and complementary medicine (59.2%). However, their satisfaction rates with education on marine pharmacognosy (10.4%) and drugs sourced from animals (30.2%) and microorganisms and minerals (32.2%) were low. Students rated their preparedness toward related competencies at concerning levels. The lowest value was observed in homeopathy (21.0%). Students felt more confident in academic and industrial practices (52.4%) than in community and hospital pharmacy requirements (35.3%). The impacts of national accreditation status and the education model of the faculties were found to be limited. Conclusion: An overall review may be needed to adapt the field to outcome-based education or CBE.
Comparative phytochemical and bioactivity studies on two related Scorzonera L. species: A chemotaxonomic contribution
(Elsevier, 2023) Şahin, Hasan; Demir, Serhat; Boğa, Mehmet; Sarı, Aynur; Makbul, Serdar; Gültepe, Mutlu
Scorzonera L. (Asteraceae) is considered a taxonomically difficult genus with its more than 160 species. Scorzonera bella (SB) and S. veratrifolia (SV) species have been treated as synonyms since 1975. Recent botanical studies suggested the separation of the two taxa based on phenetic dissimilarities. Isolation, LC-MS/MS (including 53 phytochemicals as standard), and GC-MS (followed by library search) analyzes were conducted on the aerial parts of the plants to compare their phytochemical compositions and contribute to the classification of the two taxa. While flavonoid profile of SB was dominated by flavones, the majority of SV consisted of flavonols, among the analyzed standards. Nicotiflorin, the most abundant compound of SV, was the most notable difference which was not determined in SB. Kaempferol glycosides might be chemotaxonomic markers for the classification at subgenus levels. Caffeoylquinic acid esters were in common and similar amounts according to profiling and isolation results. Phytochemical compositions of nonpolar fractions of the plants differed significantly in phthalic acid esters, ursane, and hopane type triterpenoids which were only determined in SV. Phytochemical findings supported the separation of the two taxa. Antioxidant, anti-diabetic, anti-Alzheimer, and anti-hyperpigmentation potentials of the plants were evaluated in-vitro.
Işgın (Rheum Ribes L.) bitkisinin hipoglisemik etkisi; Diyarbakır'da bir geleneksel tıp uygulaması
(Hayrullah Yazar, 2023) Şahin, Hasan; Üşenti, Berfin
Amaç: Rheum ribes L. (Polygonaceae) dünyanın birçok bölgesinde hem gıda hem de diyabet dahil birçok hastalığa karşı geleneksel bir ilaç olarak kullanılmaktadır. Bu çalışmada bitkinin hipoglisemik potansiyelinin ve Diyarbakır’daki geleneksel kullanımının araştırılması amaçlanmıştır. Metot: Bitkinin Diyarbakır pazarlarındaki satıcıları, rastgele seçilmiş kullanıcılar ve aktarlarla görüşmeler yapılmıştır. Hakkâri ve Muş (Şenyayla) illerinden toplanan bitkinin toprak üstü ve kök kısımlarından petrol eteri (PE), etil asetat (EA), metanol (Me) ve içme suyu (İnf) kullanılarak hazırlanan ekstrelerin invitro α-glukozidaz inhibisyon aktivitesi mikroplaka okuyucu kullanılarak kolorimetrik yöntemle ölçülmüştür. Bulgular: Bitkinin taze sürgünleri yöre halkı tarafından çiğ halde yenmektedir. Kökleri ise geleneksel olarak hem taze hem de kurutulmuş halde dil altına konularak ya da sabahları aç karnına tıbbi çay halinde kan glukoz seviyesini düşürme amaçlı kullanılmaktadır. Her iki örneğin tüm ekstreleri pozitif kontrol akarboza kıyasla yüksek potansiyel göstermişlerdir. Özellikle akarbozun 665,9 µg/mL IC50 değerine karşılık Muş örneklerinin kök metanol ve etil asetat ekstrelerinde ortaya çıkan sırasıyla 0,24 ve 0,33 µg/mL IC50 değerleri kayda değerdir. Sonuç: α-glukozidaz inhibisyonu bitkinin hipoglisemik aktivitesine önemli derecede katkı sağlayan bir etki mekanizması olabilir. Bu enzimin yeni ve potent inhibitörlerinin keşfi için bitkinin köklerinden etil asetat ya da metanol ile elde edilecek ekstreler üzerinde ileri fitokimyasal çalışmalar önerilebilir.
The Therapeutic potential of ethnomedicinally important Anatolian thyme species: A Phytochemical and biological assessment
(Frontiers, 09.06.2022) Özkan, Esra Eroğlu; Ersoy, Ezgi; Cantürk, Yeter Yeşil; Kara, Emel Mataracı; Çınar, Ercan; Şahin, Hasan; Karahan, Selim; Sancaktepe, Kübra Karaca; Yılmaz, Mustafa Abdullah; Boğa, Mehmet
Thyme has been used for various therapeutic purposes in many different cultures, which makes it one of the most riveting medicinal plants throughout history. From its beneficial effects on the respiratory tract or the gastrointestinal system, to its unique skin-related activities, the investigation of the medicinal properties of thyme has always been an alluring topic for researchers aiming to develop conventional medications from this traditional herb. With an incentive to contribute to the extensive thyme research, three Thymus L. species namely Thymus cariensis Hub-Mor. & Jalas (endemic), Thymus praceox subsp. grossheimii (Ronniger) Jalas, and Thymus pubescens Boiss. et Kotschy ex Celak from Turkey were deeply investigated within this study. The analysis of the phytochemical constituents of the extracts was conducted by LC-MS/MS. 12 biologically important secondary metabolites (p-coumaric acid, caffeic acid, salicylic acid, quinic acid, fumaric acid, vanillin, malic acid, rutin, apigenin, naringenin, and nicotiflorin) were detected in all extracts. Their total phenolic and flavonoid contents were calculated (11.15 ± 0.17—61.12 ± 2.59 μg PEs/mg extract, 2.53 ± 0.04—40.28 ± 0.92 μg QEs/mg extract, respectively), and the antioxidant potential of the extracts was evaluated by DPPH and ABTS radical scavenging and CUPRAC activity methods, accordingly, the extracts were shown to possess significant antioxidant activity. Among them, Thymus cariensis Hub-Mor. & Jalas was the most active with IC50 values of 34.97 ± 1.00 μg/ml and 9.98 ± 0.04 μg/ml regarding the DPPH and ABTS radical scavenging assays, respectively, and an A0.5 value of 5.80 ± 0.02 μg/ml according to CUPRAC activity method. Their anticholinesterase, antityrosinase, and antiurease activities were also tested, Thymus cariensis Hub-Mor. & Jalas (35.61 ± 1.20%) and Thymus pubescens Boiss. et Kotschy ex Celak aerial part extract (33.49 ± 1.39%) exhibited moderate antibutyrylcholinesterase activity at 200 μg/ml concentration. The results of the cell viability assay indicated that the extracts demonstrated moderate-to-low cytotoxicity on A498 human renal cell lines. Furthermore, all studied extracts exerted noteworthy antimicrobial activity, especially against Candida tropicalis (MIC values: 19.53—78.12 μg/ml). The presented data substantiates the use of thyme extracts as therapeutic agents in both ethnomedicine and conventional therapies.
A Comprehensive study on a medicinal and edible plant scorzonera incisa DC., discussing the natural limits of phytochemical profiling
(Wiley, 2023) Şahin, Hasan; Demir, Serhat; Boğa, Mehmet; Sarı, Aynur; Makbul, Serdar; Coşkunçelebi, Kamil
Leaves of Scorzonera incisa DC. (Asteraceae) are eaten raw against diabetes and headache. Evaluation of medicinal, edible plants using profiling methods has become a common phenomenon. Petroleum ether (PE), ethyl acetate (EA), and nbutanol (BU) fractions were prepared from ethanol extract of the aerial parts of the plant. Isolation by HPLC and phenolic profiling by validated LC-MS/MS method with 53 compounds were conducted on the EA fraction. GC-MS method was used to profile the PE fraction. In-vitro inhibitory activities of all fractions against α-amylase, α-glucosidase, AChE, BChE, tyrosinase and urease enzymes were measured. Isoorientin, vitexin, cynaroside and chlorogenic acid were isolated and characterized from the EA fraction as major compounds. LC-MS/MS analysis quantified 36 compounds in the EA fraction. 20 compounds were tentatively determined in the PE fraction. Compounds with the same molecular and fragment ions, a low percentage of identified compounds, and very close polarities were revealed to be some limits of the nature for LC-MS/MS profiling. Particularly, the presence and amount of substances other than the standard compounds used in the profiling methods and possible misdetections should not be neglected in evaluating medicinal plants and establishing a correlation between compounds and bioactivity.
7-Acetoxyhorminone from Salvia multicaulis Vahl. as Promising Inhibitor of 3-Hydroxy-3-methylglutaryl Coenzyme A (HMG-CoA) Reductase
(MDPI, 2022) Yiğitkan, Serkan; Ertaş, Abdulselam; Salmas, Ramin Ekhteiari; Fırat, Mehmet; Orhan, İlkay Erdoğan
3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase is a key enzyme involved in cholesterol biosynthesis and one of the most important targets for the treatment of hy-percholesterolemia. A limited number of studies on the HMG-CoA reductase inhibitory potential of natural products are available. Thus, in the current study, we aimed to test the HMG-CoA re-ductase inhibitory capacity of extracts from the roots and aerial parts of Salvia multicaulis Vahl., through activity-guided isolation. Our findings revealed that the root extract prepared with di-chloromethane–acetone (1:1) showed the highest inhibition (71.97 ± 0.37%) at 100 µg/mL. The extract was then initially fractionated by column chromatography and the obtained fractions were monitored by thin layer chromatography. Fractions which were similar to each other were combined and a total of 15 fractions were obtained. Further conventional chromatographic studies were carried out on the active fractions. Based on these fractions, 10 known compounds, compris-ing 9 terpenes and 1 steroid derivative in total, were isolated and their structures were verified by a combination of IT-TOF-MS, and 1D and 2D NMR techniques. According to the enzyme inhibition data of the identified compounds, 7-acetoxyhorminone exerted the highest inhibition (84.15 ± 0.10%, IC50 = 63.6 ± 1.21 µg/mL). The molecular docking experiments on 7-acetoxyhorminone and horminone indicated that both compounds strongly bind to the active site of the enzyme.
In-vitro anti-diabetic, anti-Alzheimer, anti-tyrosinase, antioxidant activities of selected coumarin and dihydroisocoumarin derivatives
(İzzet Kara, 2023) Şahin, Hasan
Abstract: Benzo-α-pyrone structured coumarin derivatives are secondary metabolites first obtained from Coumarouna odorata in 1822. Coumarin and its structural isomer dihydroisocoumarin derivatives are found in many different sources in nature. Several different bioactivities of these compounds have been reported. In this study, preliminary activity screening and comparison of four purchased coumarin derivatives (esculetin, esculin monohydrate, umbelliferon, scoparone) and four previously isolated 3-phenyl-3,4-dihydroisocoumarin derivatives (thunberginol C, scorzocreticoside I, scorzocreticoside II, scorzopygmaecoside) from a medicinal plant were carried out by in-vitro methods. α-Glucosidase, acetylcholinesterase, butyrylcholinesterase, tyrosinase inhibitor activities and antioxidant potentials of the compounds were evaluated. Consequently, thunberginol C (free – not glycosylated form of 3,4dihydroisocoumarin structure) showed better potential in all enzyme inhibitory activities compared to coumarin structure. Particularly, α-glucosidase inhibitory activity of this compound with a very low IC50 value (94.76±2.98 µM) compared to standard acarbose (1036.2±2.70 µM) should be noted. Glycosylation and/or methoxy substitution of 3,4-dihydroisocoumarin structure resulted a significant decrease in all tested enzyme inhibitory activities. The structures of esculin MH, umbelliferone, scoparone, scorzocreticoside I, and scorzopygmaeceoside might be considered in further synthetic studies as selective acetylcholinesterase inhibitors. Thunberginol C has a promising potential in tyrosinase inhibitory activity. Esculetin and thunberginol C showed the best results with high potentials in antioxidant activity via 2,2-diphenyl-1-picryl-hydrazyl-hydrate free radical scavenging, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid cation radical decolorization, and cupric ion reducing antioxidant capacity assays compared to the standards.

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