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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.
The anticholinesterase perspective of dimethoxyindole based benzenesulfonamides: Synthesis, biological investigation and molecular docking applications
(John Wiley and Sons Inc., 2024) Bingül, Murat; Ercan, Selami; Boǧa, Mehmet; Arslan, Zehra; Tuneğ, Muhammed; Akocak, Süleyman; Bingül, Alev Arslantürk; Şengül, İbrahim Fazıl; Şahin, Hasan
Due to the well-known biological potential of benzenesulfonamides for the inhibition of specific enzymes, here in, we propose to investigate anticholinesterase efficiencies of five newly synthesized benzenesulfonamides incorporating dimethoxyindole tails. The targeted compounds were synthesized through the C7 position of the methyl 4,6-dimethoxy-1H-indole-2-carboxylate via Schiff-base reaction. The biological study was directed to identify the acetylcholinesterase (ACh) and butyrylcholinesterase (BCh) enzyme inhibitions. The molecular docking studies were also carried out to determine the possible poses of ligands 8 a–e in binding sites of enzymes and ligand-residue interactions. Molecular dynamics simulations, RMSD and RMSF plots, hydrogen bond analysis, per-residue energy decomposition and MM-PB(GB)/SA calculations were carried out investigate the potentials of the compounds towards the designated enzymes. It is important to note that all the synthesized compounds were found to be selective towards the BChE inhibition with a range of efficiencies. In addition to that the compound 8 a exhibited more potency than the standard Galanthamine with the value of 87.75 % for the same enzyme. The results could be valuable for the determination of new targets which are highly selective for BChE inhibition. The formation of hydrogen bonds and hydrophobic interactions with the residues located on the compounds were responsible for the binding free energy scores. The stability of all the compounds proved by molecular dynamics simulations were also promising for the further directions of the study.
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.
Biological and computational evaluation of carbazole-based bis-thiosemicarbazones: A selective enzyme inhibition study between ?-amylase and ?-glucosidase
(Istanbul University, 2023) Şahin, Hasan; Bingül, Alev Arslantürk; Şengül, İbrahim Fazıl; Bingül, Murat
Background and Aims: Carbazole heterocyclic systems are an important class of chemicals that have been reported as valuable antidiabetic agents in the literature. Uncoincidentally, the ayurvedic antidiabetic plant Murraya koenigii Spreng (Curry tree) was the source of the first carbazole alkaloids. Another important class of chemicals in terms of antidiabetic activity is thiosemicarbazones. The hybridization of these fragments can create new potential inhibitors for α-amylase and α-glucosidase enzyme inhibitions, which is one approach controlling post-prandial hyperglycemia in type 2 diabetes patients. Methods: The four carbazole-based thiosemicarbazone compounds (4a-d) have been selected from the group library and α-amylase and α-glucosidase inhibition potencies have been evaluated. A molecular modelling study has also been carried out to provide a complementary study on how the molecules behave in terms of the enzymes’ catalytic properties. . Results: All compounds showed higher potencies than the standard acarbose in terms of α-glucosidase inhibition and very low inhibitions toward α-amylase compared to acarbose. Having the number of hydrophobic interactions determine the potency of the compounds was crucial with compound 4a being shown to provide the highest number of conventional H bonds and the highest percentage of inhibition values for both enzymes. Conclusion: Carbazole-based thiosemicarbazone compounds have been found to be promising candidates in terms of both their potency and relative selectivity for developing new inhibitors that lack the usual side effects of current drugs.
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
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.
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.
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.
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.
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.
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
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.
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.
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.
Indolyl imine compounds as multi-target agents; synthesis, antidiabetic, anticholinesterase, antioxidant activities and molecular modeling
(Elsevier B.V., 2024) Ceyhan, Sadık M.; Zengin, İrem Nur; Bingül, Murat; Şahin, Hasan; Boǧa, Mehmet; Sağlam, Mehmet F.; Kandemir, Hakan
A new range of indolyl imine system 3d-l has been successfully prepared from 4,6-dimethoxy-2,3-diphenyl-indole-7-carbaldehyde 2a and 4,6-dimethoxy-3-aryl-indole-7-carbaldehyde 2b-c via Schiff base reaction. The structure of targeted compounds was confirmed by 1H and 13C NMR, FT-IR, mass spectrometry and single crystal X-ray diffraction techniques. The indolyl imine derivatives were also subjected to in vitro antidiabetic activities employing ?-glucosidase and ?-amylase enzymes. In terms of antidiabetic investigation, the ?-glucosidase enzyme was found to be potential target due to the comparable inhibition concentrations with the standard acarbose and the compound 3e exhibited better potency than the standard. The anticholinesterase potency of the compounds was investigated towards the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The compounds displayed moderate efficiency against the BChE enzyme with the best inhibition concentration of 30.48 ?M by the compound 3h. The antioxidant properties of final compounds were determined by DPPH radical scavenging, ABTS Cation Radical Decolarization and CUPRAC Cupric Reducing Antioxidant Capacity assay methods. The ABTS cation scavenging assay provided the best responses for the compounds and the candidates 3k and 3l were determined as promising targets for the antioxidant activity. Plausible binding mode and interaction of ligands with the selected enzyme have been studied by molecular docking, supporting the experimental results. In silico ADME showed high drug likeness of the synthesized compounds. © 2024 Elsevier B.V.
Investigating the Pharmacological Potential of Micromeria myrtifolia Boiss. & Hohen.: Phenolic Profiling and Biological Activity Assessments
(ABADER (Adıyaman Bilimsel Arastırmalar Dernegi), 2024) Ersoy, Ezgi; Batal Yildizhan, Rumeysa; Yilmaz, Mustafa Abdullah; Yeşil Cantürk, Yeter; Şahin, Hasan; Eroğlu Özkan, Esra; Boğa, Mehmet
Micromeria myrtifolia Boiss. & Hohen. is a valuable medicinal plant in Türkiye, recognized for its extensive applications across the country. In this study, plant samples were collected from Muğla, Türkiye and extracts from both the aerial parts and roots were prepared using ethanol. To elucidate their phytochemical composition, a comprehensive LC-MS/MS analysis was conducted. The results revealed that both extracts were quite rich in phenolic compounds. Notably, nicotiflorin was the major constituent in both extracts (12878.31±355.44 μg/g extract in the aerial parts and 47512.4±1311.34 μg/g extract in the roots) along with significant phenolic acids such as rosmarinic acid and caffeic acid as well as flavonoids like hesperidin. Moreover, both extracts demonstrated substantial antioxidant activities compared to the synthetic antioxidant compounds as evaluated by DPPH free radical scavenging, ABTS cation radical scavenging, and CUPRAC activity assays. Both aerial parts and root extracts also exhibited meaningful anti-glucosidase activity with 73.03±0.16% and 47.06±0.41%, respectively, at 2 mg/mL concentration. The root extract also showed moderate butyrylcholinesterase inhibitory activity. This study contributes to the existing body of knowledge with valuable insights regarding the phytochemical profile and biological activities of M. myrtifolia, paving the way for future research aimed at exploring its medicinal properties and potential uses in traditional and modern medicine. © 2024, ABADER (Adıyaman Bilimsel Arastırmalar Dernegi). All rights reserved.
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.
Micromeria myrtifolia Boiss. & Hohen. Bitkisinin Farmakolojik Potansiyelinin Araştırılması: Fenolik İçeriğinin ve Biyolojik Aktivitelerinin Belirlenmesi
(ABADER (Adıyaman Bilimsel Araştırmalar Derneği), 2024) Ersoy, Ezgi; Yıldızhan, Rümeysa Batal; Yılmaz, Mustafa Abdullah; Yeşil, Yeter; Şahin, Hasan; Özkan, Esra Eroğlu; Boğa, Mehmet
Micromeria myrtifolia Boiss. & Hohen., Türkiye'nin önemli tıbbi bitkilerindendir ve ülke genelinde farklı tıbbi amaçlarla oldukça yaygın olarak kullanılmaktadır. Bu çalışmada, M. myrtifolia örnekleri Muğla, Türkiye'den toplanmış hem topraküstü kısımlarından hem de köklerden ayrı ayrı etanol ekstreleri hazırlanmıştır. Ekstrelerin fitokimyasal içeriklerini belirlemek için detaylı bir LC-MS/MS analizi yapılmıştır. Analiz sonuçlarına göre her iki ekstrenin de fenolik bileşikler açısından oldukça zengin olduğu belirlenmiştir. Her iki ekstrede de ana bileşen olarak nikotiflorin öne çıkmış ve topraküstü kısımlarından hazırlanan ekstrede 12878.31±355.44 µg/g, kök ekstresinde ise 47512.4±1311.34 µg/g nikotiflorin tespit edilmiştir. Ayrıca ekstrelerde rozmarinik asit ve kafeik asit gibi önemli fenolik asitler ile hesperidin gibi flavonoitlerin varlığı da belirlenmiştir. Ekstrelerin antioksidan aktiviteleri DPPH serbest radikal giderici, ABTS katyon radikali giderici ve CUPRAC aktivitesi metotları ile değerlendirilmiş, buna göre her iki ekstre de sentetik antioksidan bileşiklere kıyasla anlamlı antioksidan aktiviteler sergilemiştir. Bunun yanı sıra ekstreler enzim inhibisyon aktiviteleri açısından değerlendirildiğinde, ekstrelerin 2 mg/mL konsantrasyonda %73.03±0.16 (topraküstü) ve %47.06±0.41 (kök) oranında anti-glukozidaz aktivite gösterdiği tespit edilmiştir. Kök ekstresi ayrıca orta düzeyde butirilkolinesteraz inhibe edici aktivite de göstermiştir. Bu çalışma, M. myrtifolia bitkisinin kimyasal içeriği ve biyolojik aktiviteleri konusunda mevcut literatüre önemli katkılarda bulunmakla birlikte, bitkinin geleneksel ve modern tıp uygulamalarındaki yeni ve potansiyel kullanım alanlarını keşfetmeye yönelik gelecek araştırmalara da zemin hazırlamaktadır.
Phenolic compounds and bioactivity of Scorzonera pygmaea Sibth. & Sm. aerial parts: In vitro antioxidant, anti-inflammatory and antimicrobial activities
(Istanbul University, 2020) Şahin, Hasan; Sarı, Aynur; Özsoy, Nurten; Çelik, Berna Özbek
Abstract Background and Aims: Scorzonera L. genus contains several medicinal and edible plants. Both roots and aerial parts of Scorzonera species are used. S. pygmaea is endemic to Turkey. in a previous study, nine phenolic compounds were reported from the roots of the plant alongside certain biological activities. The current study was designed to investigate the aerial parts of the plant in the same manner and compare the potentials of the two parts. Methods: Chromatographic and spectroscopic methods were used to isolate and identify the phenolics. Total phenolic contents were determined by Folin-Ciocalteu method. FRAP assay, anti-LPO, scavenging DPPH, ABTS and superoxide radicals were employed to evaluate the antioxidant activity. COX inhibition test and micro broth dilution technique were used for anti-inflammatory and antimicrobial activities, respectively. Results: Seven phenolic compounds; thunberginol C (1), protocatechuic acid (2), chlorogenic acid methyl ester (3), cudrabibenzyl A (4), scorzocreticin (5), scorzocreticoside I (6) and II (7) were purified. All the compounds are new for the aerial parts of the plant and 2 is new for the genus. The aerial parts showed a high antioxidant capacity which correlated with its phenolic content. COX inhibitory activity was found to be lower compared to Indomethacin. Weak antimicrobial activity was determined against Staphylococcus aureus and S. epidermidis. Conclusion: Aerial parts possess significant/infrequent phenolics and the ethyl acetate (EtOAc) fraction of the ethanol extract is the most promising fraction for isolating these compounds. Phenolic compositions of aerial parts and roots are very similar. However, aerial parts can be a better rich source of natural antioxidants with protocatechuic acid and higher antioxidant potential.

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