Cytotoxicity screening of some Turkish plants against renal cancer cells

In this contribution, we performed cytotoxicity screening of 51 extracts from 17 plant species, representing 14 families growing in Turkey. Cytotoxic activities of the dichloromethane, ethyl acetate, and methanol extracts of the plants were investigated against the renal (A498 and U031) cancer cell lines. 28 extracts exhibited more than 50% growth inhibition at a 25 ug/mL concentration on both renal cancer A498 and UO31 cell lines. The extracts showed higher activity against UO31 cells than A498 cells. The dichloromethane extract of the aerial parts of Scabiosa columbaria ssp. columbaria showed the highest cytotoxic activity with 64% inhibition at a 25 ug/mL concentration on the renal cancer UO31 cell line. The methanol extract of the aerial parts of Epilobium minutiflorum showed the highest cytotoxic activity with 63% inhibition at a 25 ug/mL concentration on the renal cancer A498 cell line

Assessment of Centella Asiatica Extract Containing Dual-crosslinked Gel-MA/Pec Hydrogels as Wound Dressing

In the present work, 3D-printed wound dressings containing different amounts of Centella Asiatica extract were synthesized via dual-crosslinking method. Methacrylic anhydride modified gelatin (Gel-MA) and pectin (Pec) were chosen as the base material for dressings. A dual crosslinked network was formed with Gel-MA photo-crosslinking using Irgacure 2959 and Pectin (Pec) psychical-crosslinking using Ca++ ions. Meanwhile, the developed dual-crosslinked hydrogel dressings were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, and mechanical, swelling, in vitro degradation as well as ex vivo bioadhesion tests. It has been observed that the preapred dressings provide good bioadhesion on the chicken skin. Moreover, MTT assay revealed cell viability of Gel-MA/Pec hydrogel dressings containing Centella Asiatica extract. The results presented the dressings as a promising biomaterial to be used for wound healing purposes, which should be further investigated in future

Pharmacognosıc Researches On Petroedmondıa Syrıaca (Boıss.) Tamamsch

Çalışmamızda, Petroedmondia syriaca (Boiss.) Tamamsch. (Apiaceae) bitkisinin sitotoksik aktivite yönünden incelenmesi ve bu aktiviteden sorumlu bileşiklerin belirlenmesi amaçlanmıştır. Bitkinin kökünden izole edilip saflaştırılan kumarinler fiziksel ve spektral özelliklerinden yararlanılarak 3′-isobutiriloksi marmesin asetat, 3′-α-angeloiloksi deltoin, smyrnioridin, deltoin, marmesin asetat, skoparon, bergapten, psoralen, kolladonin, 14′- asetoksi badrakemin, marmesin ve 14′-hidroksi badrakemin olarak teşhis edilmiştir. Bitkinin köklerinden toplam on üç bileşik izole edilmiştir. Üç bileşik ilk kez bu çalışmada izole edilmiştir. Diğer bileşikler ise daha önce bilinmekle beraber bu bitkiden ilk defa izole edilmiştir. Ekstreler, MCF-7 hücre hattında MTT yöntemi ile sitotoksisite yönünden değerlendirilmiştir. Bitkiden elde edilen bileşiklerin ve kumarin karışımının sitotoksik aktivitesi araştırılmış, sitotoksik aktivitesi kayda değer bulunmuştur. Bitki kumarin türevi bileşikler ve sitotoksik aktivite açısından ilk kez tarafımızdan incelenmiştir.The aim of this study is to investigate the cytotoxic activity of Petroedmondia syriaca (Boiss.) Tamamsch. (Apiaceae) and to determine the responsible compounds from this activity. The isolated and purified 12 coumarins from the roots of the plant were identified as 3'-isobutyryloxymarmesin acetate, 3′-α-angeloyloxydeltoin, smyrnioridine, deltoin, marmesin acetate, scoparone, bergapten, psoralen, colladonin, 14'-acetoxybadrakemin, marmesin and 14'-hydroxybadrakemin using their physical and spectral characteristics. Three compounds of them were isolated for the first time in this study. The extracts (hexan,CH2Cl2 etc.) were evaluated for cytotoxicity by the MTT method using MCF-7 cell line. The cytotoxic activity of the compounds obtained and the coumarin mixture were investigated and the cytotoxic activity was found to be significant. This is the first report on the chemical composition and cytotoxic activity of the roots of P. syriaca. The cytotoxic activity of the coumarin mixture was found to be significant

Determination of parthenolide in tanacetum argenteum (lam.) willd. subsp. argenteum

Bu çalışmada, Kayseri-Binboğa dağlarından toplanan şimdiye kadar partenolit içeriği yönünden araştırılmamış ve Türkiye için endemik olan Tanacetum argenteum subsp. argenteum bitkisinin yaprak, çiçek ve gövde kısımlarının partenolit içeriği HPLC/LC-MS yöntemi ile tayin edilmiştir. Bitkinin gövde (%0,129) ve çiçeklerindeki (%1,585) partenolit miktarı literatürlerde121-124 Tanacetum parthenium için belirtilen değerler (%0,1-1,68) arasındadır. Yapraklarda bulunan partenolit miktarı (%2.261) ise çok daha yüksek olup Avrupa Farmakopesin de126 ve ESCOP da127 T. parthenium bitkisinin topraküstü kısımları için istenmiş olan miktarın (%0,2) da çok üzerindedir.In this study, the leaves, flowers and stems of endemic Tanacetum argenteum subsp. argenteum collected from Kayseri-Binboğa mountains were analyzed for their parthenolide content by using HPLC/LCMS method. There were no reports in the literature on the parthenolide content of Tanacetum argenteum subsp. argenteum. Parthenolide amount in the stems (%0,129) and flowers (%1,585) of Tanacetum argenteum subsp. argenteum are in accordance with the reported amount for Tanacetum parthenium in the literature (%0.1-1.68). Parthenolide amount of the leaves of Tanacetum argenteum subsp. argenteum (%2.261) is much higher than the required amount for the aerial parts of Tanacetum parthenium (%0,2) in European Pharmacopoeia and ESCOP Monographs

Biological activities of the natural coumarins from apiaceae plants

Nineteen natural coumarins; badrakemin (1), colladonin (2), 14'-acetoxybadrakemin (3), anatolicin (4), 14'-hydroxycolladonin (5), badrakemone (6), karatavicinol (7), 14'-acetoxybadrakemone (8), 14'-acetoxycolladonin (9), colladonin acetate (10), deltoin (11), smyrnioridin (12), isoimperatorin (13), oxypeucedanin (14), bergapten (15), osthol (16), 4'-senecioyloxyostol (17), neopapillarine (18), and scoparone (19) were tested against U87MG, A549, and PC3 cancer cell lines as well as against healthy human embryonic kidney cell line, HEK293. Colladonin (2) was found to have IC50 values of 12.6 and 11.58 µM in A549 and PC3 cell lines, respectively. Deltoin (11) and 14'-acetoxybadrakemin (3) were found to have an IC50 value of 9.92 µM and 11.85 µM against the U87MG cell line, respectively. Remarkably, these compounds show very low cytotoxicity against the healthy human embryonic kidney cell line, HEK293. In addition to the cytotoxic activity, nineteen natural coumarins were tested for their inhibitory activity against 5-LOX, collagenase, and elastase enzymes

Butyrylcholinesterase-inhibiting natural coumarin molecules as potential leads

Seventeen natural coumarin derivatives; badrakemin (1), 14′-acetoxybadrakemin (2), badrakemone (3), 14′-acetoxybadrakemone (4), colladonin (5), colladonin acetate (6), 14′-acetoxycolladonin (7), karatavicinol (8), deltoin (9), smyrnioridin (10), marmesin (11), osthol (12), oxypeucedanin (13), oxypeucedanin hydrate (14), isoimperatorin (15), scopoletin (16), and umbelliprenin (17), were tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the sister enzymes that play a critical role in the pathology of Alzheimer’s disease as well as tyrosinase (TYR) as the target for Parkinson’s disease. The tested coumarins were more selective against BChE, where the coumarins 2, 5, 8, and 15 (IC50 = 30.3 μM, 29.2 μM, 37.2 μM, and 50.1 μM, respectively) displayed higher BChE inhibition than the reference (galanthamine, IC50 = 60.2 μM) at 100 μg/mL. Only four coumarins (2, 5, 9, and 15) showed inhibition against AChE. Binding conformations of the coumarins (2, 5, 8, 9, and 15) within the active sites of AChE and BChE were explored via molecular docking experiments. The docked compounds were oriented by the interactions with the oxyanion hole and the peripheral anionic site residues of AChE/BChE. The coumarin derivatives 1–17 was found to have no or low inhibition (2.03 ± 0.92 %–12.91 ± 0.40 %) against TYR at 100 μg/mL. Our findings revealed that coumarins could be promising lead compounds for designing novel anti-Alzheimer drug candidates

Butyrylcholinesterase-inhibiting natural coumarin molecules as potential leads

Seventeen natural coumarin derivatives; badrakemin (1), 14′-acetoxybadrakemin (2), badrakemone (3), 14′-acetoxybadrakemone (4), colladonin (5), colladonin acetate (6), 14′-acetoxycolladonin (7), karatavicinol (8), deltoin (9), smyrnioridin (10), marmesin (11), osthol (12), oxypeucedanin (13), oxypeucedanin hydrate (14), isoimperatorin (15), scopoletin (16), and umbelliprenin (17), were tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the sister enzymes that play a critical role in the pathology of Alzheimer's disease as well as tyrosinase (TYR) as the target for Parkinson's disease. The tested coumarins were more selective against BChE, where the coumarins 2, 5, 8, and 15 (IC50 = 30.3 μM, 29.2 μM, 37.2 μM, and 50.1 μM, respectively) displayed higher BChE inhibition than the reference (galanthamine, IC50 = 60.2 μM) at 100 μg/mL. Only four coumarins (2, 5, 9, and 15) showed inhibition against AChE. Binding conformations of the coumarins (2, 5, 8, 9, and 15) within the active sites of AChE and BChE were explored via molecular docking experiments. The docked compounds were oriented by the interactions with the oxyanion hole and the peripheral anionic site residues of AChE/BChE. The coumarin derivatives 1–17 was found to have no or low inhibition (2.03 ± 0.92 %–12.91 ± 0.40 %) against TYR at 100 μg/mL. Our findings revealed that coumarins could be promising lead compounds for designing novel anti-Alzheimer drug candidates