GİRİŞ ve AMAÇ: p90 Ribozomal kinazlar serin/treonin protein kinaz ailesindendir ve kanser hücrelerinin çoğalmasında rol aldıkları saptanmıştır.
YÖNTEM ve GEREÇLER: Yüksek seçiciliğe sahip inhibiötlerin ve aynı zamanda bu inhibitörlerin mekanizmalarına ait yapısal bilgilerin eksikliği, bu alanda ilerlemeyi kısıtlamaktadır. Uygun bir RSK kristal yapısı olmadan yapılan in siliko protein-inhibitör çalışmalarında da yanlış sonuçlara varıldığı söylenmiştir.
BULGULAR: Bu çalışmada, yeni çözümlenen, en etkili ve seçici RSK inhibitörlerinden LJH685 ile kompleks halinde olan, yüksek çözünürlükteki RSK2 kristal yapısı kullanılarak, RSK2'ye ait ilk efarmakofor modeli oluşturulmuştur. Büyük veri tabanlarının (144 milyondan fazla konformasyona sahip yaklaşık 7 milyon bileşik) sanal taraması, ardından bir dizi moleküler kenetleme çalışması ve kritik bağlanma modlarının görsel olarak incelenmesi çalışmalarının birleştirilmesi ile 12 bileşik umut vaat eden etkili ve seçici inhibitörler olarak önerilmiştir.
TARTIŞMA ve SONUÇ: Bu bileşikler arasından 5777208 ve 5919607'nin kayda değer kenetlenme skorlarının ve bağlanma etkileşimlerinin olduğu bulunmuştur.

INTRODUCTION: The p90 ribosomal S6 kinases (RSK) are a family of serine/threonine protein kinases and are shown to
be involved in cancer cell proliferation.
METHODS: The lack of highly selective inhibitors and also the lack of structural information regarding the mechanism of those inhibitors restricts the progress in this field. It has also been reported that without a proper crystal structure of RSK, the protein-inhibitor interactions in silico studies had been erroneously concluded.
RESULTS: The first e-pharmacophore model for RSK2 has been generated in this study using recently resolved high resolution crystal structure of RSK2 in complex with LJH685 that is amongst the most potent and selective RSK inhibitors to date. 12 compounds have been suggested as promising potent and selective RSK inhibitors after the combination of virtual screening of a large database (ca. 7 million compounds with more than 144 million conformations), followed by a series of molecular docking work flow and visual inspection of all hits for critical binding modes.
DISCUSSION AND CONCLUSION: Amongst those hits, 5777208 and 5919607 have been found to have remarkable docking score and binding interactions.

Plantago lanceolata L. bitkisi, Türk Halk Tıbbında yara iyileştirici amaçla kullanılmaktadır. Bu çalışmada, P. lanceolata’nın sulu ve metanollü ekstrelerinin yara iyileştrici ve anti-enflamatuvar etkilerinin araştırılması amaçlanmıştır. Bitkinin yara iyileştirici etkisinin değerlendirilmesi için fare ve sıçanlarda in vivo eksizyon ve insizyon yara modelleri kullanılmıştır. Ekstrelerin asetik asit-nedenli kapiller permeabilite artışını inhibe edici etkileri Whittle Yöntemi kullanılarak araştırılmıştır. Bununla beraber, dokulardaki tiyobarbitürik asit reaktifleri (TBARs), glutatyon (GSH), total tiyol grupları (TSH) ve hidroksiprolin (HP) seviyeleri ile iz elementlerin (Zn+2 ve Cu+2) miktarları analiz edilmiştir. P. lanceolata’nın sulu ekstresinin insizyon ve eksiyon yara modellerinde yara iyileştirici etkiye sahip olduğu tespit edilmiştir. Histopatolojik incelemeler sonucunda elde edilen veriler de bu sonuçları desteklemektedir. Bitkinin her iki ekstresinin de anlamlı derecede anti-enflamatuvar etkiye sahip olduğu belirlenmiştir. P. lanceolata’nın oksidatif stresin bir göstergesi olan TBARs seviyesini anlamlı derecede düşürdüğü, diğer taraftan, GSH, TSH ve HPseviyelerini arttırdığı tespit edilmiştir. Buna ek olarak, bitkinin, yara iyileşmesi ve kolajen sentezi sürecinde önemli rolleri olan Zn+2 ve Cu+2 seviyelerinde artış sağladığı belirlenmiştir. Sonuçlar, Türkiye’de halk arasında yara iyileştirici amaçla kullanılan, flavonoit içeriği bakımından zengin ve antioksidan etkisiyle bilinen P. lanceolata’nın yara iyileşmesi sürecinde de etkili olduğunu göstermiştir. Bitki üzerinde, etki mekanizmasının aydınlatılmasına yönelik ileri çalışmalara ihtiyaç duyulmaktadır.

Plantago lanceolata L. has been used for wound healing in Turkish traditional medicine. In the present study the wound healing and anti-inflammatory effects of the aqueous and methanol extract of P. lanceolata was investigated.In vivo excision and incision wound models were applied on mice and rats for the evaluation of the wound healing effect of P. lanceolata. Inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was assessed by using Whittle Method. Moreover, the levels of thiobarbituric acid reactive substances (TBARs), glutathione (GSH), total thiols (TSH), hydroxyproline (HP), and tissue trace elements (Zn+2 and Cu+2) were analysed.The aqueous extract of P. lanceolata was found to have wound healing activity in both incision and excision wound models. The results obtained from histopathological analysis also supported the data. Significant anti-inflammatory activity was also detected for both extracts. P.lanceolata significantly reduced the levels of TBARs which is one of the indicators of oxidative stress on the wounded tissue and increased the levels of GSH, TSH and HP. Additionally, P. lanceolata was found to have capacity to increase the levels of tissue Zn+2and Cu+2, both of which are important indicators in the process of wound healing and collagen synthesis. The results indicated that P. lanceolata which is used in the treatment of wounds in addition to many illnesses in traditional medicine and is rich in terms of flavanoids has a powerful antioxidant effect and so it has a positive assistance in healing process. More advanced studies are needed to illuminate the mechanism accurately.

Abstract | Full Text PDF

The objective of this study was to investigate the relationship between the genetic polymorphism of the serotonin transporter gene-linked polymorphic region (5-HTTLPR)and the response to citalopram treatment and side effects in Turkish patients with major depressive disorder. The study involved 51 patients who received 10-40 mg/day of citalopram for 4 to 6 weeks. Clinical symptoms were evaluated by the 17-item Hamilton Depression Rating (HAMD-17) scale, Clinical Global Impression (CGI) and UKU side effect rating scale (UKU) at weeks 4 and/or 6. The 5-HTTLPRL/S polymorphism was determined by slowdown-polymerase chain reaction method. Of the fifty-one patients, 13 (26%) were the LL genotype, 21 (41%) were the LS genotype, 17 (33%) were the SS genotype. L allele seems to be associated withbetter response due to odds ratio for L allele versus S allele despite statistically insignificant. In terms of CGI-Severity scale, The LL genotype versus the LS genotype had a higher risk at the week 6 (P<0.05).On the other hand, apart from this comparison, there is no significant difference in CGI-Severity and Improvement and UKU scales according to the distribution of genotypes at week 4 and/or 6. However, these findings surely need further investigation and confirmation.

The objective of this study was to investigate the relationship between the genetic polymorphism of the serotonin transporter gene-linked polymorphic region (5-HTTLPR)and the response to citalopram treatment and side effects in Turkish patients with major depressive disorder. The study involved 51 patients who received 10-40 mg/day of citalopram for 4 to 6 weeks. Clinical symptoms were evaluated by the 17-item Hamilton Depression Rating (HAMD-17) scale, Clinical Global Impression (CGI) and UKU side effect rating scale (UKU) at weeks 4 and/or 6. The 5-HTTLPRL/S polymorphism was determined by slowdown-polymerase chain reaction method. Of the fifty-one patients, 13 (26%) were the LL genotype, 21 (41%) were the LS genotype, 17 (33%) were the SS genotype. L allele seems to be associated withbetter response due to odds ratio for L allele versus S allele despite statistically insignificant. In terms of CGI-Severity scale, The LL genotype versus the LS genotype had a higher risk at the week 6 (P<0.05).On the other hand, apart from this comparison, there is no significant difference in CGI-Severity and Improvement and UKU scales according to the distribution of genotypes at week 4 and/or 6. However, these findings surely need further investigation and confirmation.

Abstract | Full Text PDF

Inula viscosa (L.) Aiton çiçeklerinde bir flavon bileşiği olan hispidulin (4´,5,7-trihidroksi-6-metoksiflavon) miktarı Yüksek Performans Sıvı Kromatografisi (YPSK) ile tayin edilmiş, ayrıca I. viscosa çiçeklerinin metanolik ekstresinin Yüksek Performans İnce Tabaka Kromatografisi (YPİTK) parmakizi kromatogramı da verilmiştir. Her iki yöntem de biyo-işaret bileşen olan hispidulinin belirlenmesi için hızlı ve kolay yaklaşımlar sağlamaktadır. Bu çalışmada küçük bir flavonoit bileşiği olan hispidulinin teşhis ve miktar tayinini gerçekleştirmek amacıyla I. viscosa çiçeklerinin YPİTK ve YPSK profilleri ortaya konmuştur. Sonuçlar, I. viscosa çiçeklerinin önemli ölçüde (0.151±0.007 g/100g kuru ağırlık) hispidulin içerdiğini göstermektedir.

The flavone hispidulin (4´,5,7-trihydroxy-6-methoxyflavone) in the flowers of Inula viscosa (L.) Aiton was quantified by using High Performance Liquid Chromatography (HPLC), and also High Performance Thin-Layer Chromatography (HPTLC) fingerprint of the methanolic I. viscosa flower extract was presented. Both methods provided a rapid and easy approach for determination of the bio-marker hispidulin. In the present study HPTLC and HPLC profiles of Inula viscosa flowers were presented to detect and quantify the small flavonoid hispidulin. The results reveal that I. viscosa flowers contain serious amount (0.151± 0.007 g/100g dry weight) of hispidulin.

Abstract | Full Text PDF

Suyun kalitesi halk sağlığı için çok önemlidir. Ancak sulardaki nitrit ve nitrat düzeyleri hala önemli bir kontaminasyon problemidir. Bu çalışmanın amacı İstanbul’un farklı bölgelerinden toplanan musluk ve çeşme sularında toplam nitrit ve nitrat düzeylerini tespit etmektir.Bu amaçla çeşitli bölgelerden musluk suyu örnekleri Kasım 2013’den Mart 2014’e kadar toplanmış ve değerlendirilmiştir. Su örneklerinde ortalama toplam nitrit ve nitrat düzeyleri Kasım, Aralık 2013 ve Şubat 2014 le karşılaştırıldığında Mart 2014’de en yüksektir. ABD Çevre Koruma Ajansına göre, musluk sularından 2’si ve kuyu sularından 3 tanesi toplam nitrat ve nitrit için maksimum kabul edilebilir konsantrasyonu (10 ppm) aşmaktadır. Ayrıca, yıllar arası değişimi saptamak için, bir önceki yıla ait su örnekleri de değerlendirilmiştir. Sonuçlar Aralık 2013-Şubat 2014 döneminde toplam nitrit ve nitrat düzeylerinin Aralık 2012-Şubat 2013 dönemine göre %2, 10 ve 18 oranında azalma göstermiştir. Sonuçlarımıza göre,mevsimsel değişim göz önüne alınarak, halk sağlığının korunması için sularda nitrit ve nitrat düzeyleri rutin olarak kontrol edilmelidir.

Water quality has a major importance for public health. However, nitrite and nitrate levels in water are still an important contamination issue in the world. This study aimed to determine the levels of total nitrite and nitrate in tap and wellwaters from different districts of Istanbul city and to evaluate the seasonal variation from November 2013 to March 2014. The average levels in tap waters were highest in March 2014 compared with November, December 2013 and February 2014. Two of the tap water and three of the well water samples exceed the maximum acceptable concentration according to the U.S. Environmental Protection Agency (10 ppm).Also, in order to determine the annual variation, tap water samples were collected between December 2012 and February 2013 and evaluated for total nitrite and nitrate levels. Results showed that total nitrite and nitrate levels during December 2013 and February 2014 were decreased in the ratio of 2, 10 and 18% compared to the same months during December 2012 and February 2013.In conclusion, our results suggested that due to seasonal and annual variations, nitrite and nitrate levels of waters should be routinely controlled to prevent various health hazards.

Abstract | Full Text PDF

Endemik bir tür olan Ferulago blancheana Post. türünün hidrodistilasyon yöntemiyle toprak üstü, çiçek ve köklerinden uçucu yağları elde edilmiştir. GC ve GC/MS analizleriyle ana bileşenleri sırasıyla toprak üstü kısmında bornil asetat (%11.7) ve β-karyofillen (%10.2); çiçekte sabinen (%23.2), mirsen (%17.5) ve kökte (E)-2-desenal (%20.3), karyofillen oksit (%17.8) olarak saptanmıştır. Elde edilen uçucu yağların biyootografi yöntemi kullanılarak Pseudomonas aeruginosa ATCC 13388, Escherichia coli NRRL, Staphylococcus aureus ATCC BAA 1026 ve Candida albicans ATCC 24433 suşlarına karşı antimikrobiyal etkisi araştırılmıştır. Toprak üstü, çiçek ve köklerden elde edilen uçucu yağların S. aureus ve C. albicans’a karşı etkili olduğu tespit edilmiş, buna karşın toprak üstü ve köklerden elde edilen uçucu yağların S. aureus’a karşı nispeten az etkili olduğu görülmüştür. P. aeruginosa’ya karşı antimikrobiyal etki saptanmamıştır.

Volatile oils from the aerial parts, flowers and roots of an endemic species Ferulago blancheana Post were obtained by hydrodistillation and analyzed by GC and GC/MS. Main components were found to be bornyl acetate (11.7%) and β-caryopyllene (10.2%); sabinene (23.2%), myrcene (17.5%); (E)-2-decenal (20.3%), caryopyllene oxide (17.8%) for the aerial parts, flowers and roots, respectively. Antimicrobial activity study with bioautography method was performed against three different microorganisms; Pseudomonas aeruginosa ATCC 13388, Escherichia coli NRRL, Staphylococcus aureus ATCC BAA 1026, and Candida albicans ATCC 24433. The results showed that essential oils obtained from the aerial parts, flowers and roots were active against S. aureus and C. albicans, however essential oils obtained from the aerial parts and roots were found to be less effective against S.aureus. In addition, no antibacterial effects were observed against P. aeruginosa.

Abstract | Full Text PDF

Cydonia oblonga Mill. (ayva) yaprakları, Helianthus tuberosus L. (yer elması) yumruları ve Allium porrum L. (pırasa) soğan ve yapraklarının in-vivo antidiabetik etkileri daha önceki çalışmamızda tespit edilmiştir. Bu bitkiler geleneksel olarak kan glukoz seviyelerini düşürmek için kullanılmaktadır. Bu sebeple, etki mekanizmalarını aydınlatmak için; ayva yaprakları, yer elması yumruları, pırasa soğan ve yapraklarının karbonhidrat sindiren enzimler (α-glukozidaz ve α-amilaz) üzerindeki inhibitör etkileri incelenmiştir. Diğer yandan, antioksidan aktiviteleri, total fenol ve flavonoit içerikleri incelenmiştir. En yüksek ABTS süpürücü aktivite, total antioksidan aktivite ve indirgeyici güç, C. oblonga yaprak etanol ekstresinde bulunmuştur. Ekstrelerin, total fenol ve flavonoit içerikleri sırasıyla 7.91-163.33 mg gallik asit eşdeğer/g ve 27.26-29.60 mg kersetin/g aralığında bulunmuştur. Sonuç olarak, bu üç bitkinin etki mekanizmasının α-amilaz ve α-glukozidaz enzimlerinin inhibisyonu ile ilgili olmadığı tespit edilmiştir.

In-vivo antidiabetic activity of Cydonia oblonga Mill. (quince) leaves, Helianthus tuberosus L. (Jerusalem artichoke) tubers, and Allium porrum L. (leek) bulb and leaves was determined in our previous studies. These plants are traditionally used to lower blood glucose levels in Turkey. Therefore, inhibitory activities of quince leaves, Jerusalem artichoke tubers, leek bulbs and leaves on carbohydrate digestive enzymes (α-glucosidase and α-amylase) were investigated to enlighten the mechanism of action. On the other hand, their antioxidant activities, total phenol and flavonoid contents were investigated. The highest ABTS radical scavenging, total antioxidant activity and reducing power were found in C. oblonga leaf ethanol extract. Nevertheless, tested plant extracts did not inhibit α-amylase and α-glucosidase significantly. Total phenol and flavonoid contents of the extracts were found in the range of 7.91-163.33 mg gallic acid equivalent/g and 27.26-29.60 mg quercetin/g, respectively. Consequently, it is clearly seen that the mechanism of action of these three plants was not determined to be related to the inhibition of α-amylase and α-glucosidase enzymes.

Abstract | Full Text PDF

The study is aimed to investigate a novel approach for the preparation of multiparticulate drug delivery system using chitosan succinate a chitosan derivatives polymer. Herein the chitosan succinate multiparticulate pellets entrapped diclofenac sodium was prepared by extrusion and spheronization technique. FTIR results revealed that there were no interactions between the drug and polymer. The prepared pellets were with good spherical geometry and 1.02±0.40 mm as their mean diameter. Chitosan succinate showed pH dependent release profiles for the entrapped diclofenac sodium. Maximum drug release was observed at pH 7.4, whereas no drug release was observed at pH 1.2. The optimized formulation followed Higuchi kinetics while drug release mechanism was found to be anomalous type i.e controlled by diffusion through swollen matrix. These results may be concluded that a new pharmaceutical carrier which can capable of sustained release in oral drug delivery system.

The study is aimed to investigate a novel approach for the preparation of multiparticulate drug delivery system using chitosan succinate a chitosan derivatives polymer. Herein the chitosan succinate multiparticulate pellets entrapped diclofenac sodium was prepared by extrusion and spheronization technique. FTIR results revealed that there were no interactions between the drug and polymer. The prepared pellets were with good spherical geometry and 1.02±0.40 mm as their mean diameter. Chitosan succinate showed pH dependent release profiles for the entrapped diclofenac sodium. Maximum drug release was observed at pH 7.4, whereas no drug release was observed at pH 1.2. The optimized formulation followed Higuchi kinetics while drug release mechanism was found to be anomalous type i.e controlled by diffusion through swollen matrix. These results may be concluded that a new pharmaceutical carrier which can capable of sustained release in oral drug delivery system.

Abstract | Full Text PDF

Salvia virgata Jacq.’ın toprak üstü kısımlarının metanol ve su ekstresinin fenolik içeriği ve antioksidan özellikleri belirlenmiştir. Her iki ekstrenin de toplam fenolik, toplam flavonoit ve flavonol içeriği, kalitatif-kantitatif kompozisyonları (YBSK ile), serbest radikal süpürücü aktiviteleri (DPPH● ve ABTS●+), demir(II) ile şelat oluşumu ve TBA yöntemi ile peroksidasyon seviyeleri incelenmiştir. IC50 değeri olarak verilen antioksidan aktiviteler butil hidroksianisol, butil hidroksitoluen, rozmarinik asit, askorbik asit ve gallik asit standartları ile karşılaştırılmıştır. Metanol ekstresi DPPH● radikalini süpürücü etkide aktif bulunurken, su ekstresi ABTS●+ radikalini süpürücü etkide aktif bulunmuştur. Metanol ektresinin fenolik bileşiminin daha zengin olduğu ve her iki ekstrede de rozmarinik asitin ana bileşen olduğu tespit edilmiştir.

Methanol and water extracts of Salvia virgata Jacq. aerial parts were examined for its phenolic contents and antioxidant activities. Both extracts were investigated for their total phenolic contents, total flavonoids and flavonols, qualitative-quantitative compositions (by HPLC-PDA analysis). Free radical scavenging activities (using DPPH● and ABTS●+), iron(II) chelation activity and also the peroxidation level was determined by TBA method. The antioxidant activity of extracts were given as IC50 values and compared with standards; butylated hydoxyanisole, butylated hydoxytoluene, rosmarinic acid, ascorbic acid, and gallic acid. Methanol extract was found to be active for DPPH● radical scavenging activity where as water extract was more active for ABTS●+ radical scavenging. The methanol extract enriched in phenolic compound and rosmarinic acid as the main component in both extracts has been identified

Abstract | Full Text PDF

Acyclovir loaded nanospheres embedded mucoadhesive film have been developed as potential drug delivery system and evaluated both ex vivo and in vivo. Poly (lactic-co-glycolic acid) nanospheres were formulated and impregnated in films prepared with varying concentrations of hydroxyethyl cellulose and eudragit RS PO. The prepared formulations (F1-F4) were evaluated by ex vivo permeation studies using rabbit mucosa in order to select the optimum formulation for further studies. In vivo studies were carried out in rabbits to assess the pharmacokinetic profile of acyclovir when delivered from mucoadhesive buccal films and its control. Ex vivo studies (6 h) indicate significant difference in permeation rate of acyclovir from mucoadhesive films (F3 > F4 > F2 > F1), suggesting the release and/or permeation of acyclovir is influenced by the film composition used. SEM images showed the nanospheres were embedded uniformly in the films. In vivo data demonstrated significant absorption (Cmax ~360.93 ng/mL; P<0.0001), prolonged duration (Tmax 6 h) and greater AUC0-α (~5 folds, P<0.0001) with buccal films in comparison to oral solution (control). The results showed

Acyclovir loaded nanospheres embedded mucoadhesive film have been developed as potential drug delivery system and evaluated both ex vivo and in vivo. Poly (lactic-co-glycolic acid) nanospheres were formulated and impregnated in films prepared with varying concentrations of hydroxyethyl cellulose and eudragit RS PO. The prepared formulations (F1-F4) were evaluated by ex vivo permeation studies using rabbit mucosa in order to select the optimum formulation for further studies. In vivo studies were carried out in rabbits to assess the pharmacokinetic profile of acyclovir when delivered from mucoadhesive buccal films and its control. Ex vivo studies (6 h) indicate significant difference in permeation rate of acyclovir from mucoadhesive films (F3 > F4 > F2 > F1), suggesting the release and/or permeation of acyclovir is influenced by the film composition used. SEM images showed the nanospheres were embedded uniformly in the films. In vivo data demonstrated significant absorption (Cmax ~360.93 ng/mL; P<0.0001), prolonged duration (Tmax 6 h) and greater AUC0-α (~5 folds, P<0.0001) with buccal films in comparison to oral solution (control). The results showed

Abstract | Full Text PDF

Bitki metabolitlerinin bir grubu olan fenolik bileşikler, antioksidan özellikleri nedeniyle oldukça fazla ilgi görmektedir. Sinapik asit fenolik bir bileşik olup çeşitli meyve ve sebzelerde yaygın bulunur. Antioksidan, antimikrobiyal, antikanser dahil pek çok farmakolojik etkiler gösterebildiği belirtilmektedir. Ancak sinapik asitin sitotoksisitesi hakkında yeterli veri bulunmamaktadır; mevcut veriler sınırlıdır. Bu çalışmanın amacı iki farklı hücre hattında; Çin hamster akciğer fibroblast (V79) ve insan serviks kanser (HeLa) hücreleri, sinapik asitin geniş bir konsantrasyon aralığında 18 saat maruziyetinde sitotoksik özelliklerini nötral kırmızı alım yöntemi ile değerlendirmektir. Sinapik asitin 500 µM ve 2000 µM’a kadar olan konsantrasyonları, sırasıyla V79 ve HeLa hücrelerinde, anlamlı bir etki göstermemiştir, ancak 1000 µM ve 5000 µM üzeri konsantrasyonlarında, sırasıyla V79 ve HeLa hücrelerinde hücre canlılıkları %50’nin altındadır. IC50 değerleri sırasıyla V79 ve HeLa hücreleri için 1860 µM ve 7248 µM olarak bulunmuştur. Bu çalışma sinapik asitin iki farklı hücre hattında genel olarak çok yüksek konsantrasyon haricinde sitotoksik etkilere sahip olmadığını göstermiştir.

Phenolic compounds, a group of plant metabolites, are of considerable interest because of their antioxidant properties. Sinapic acid, a phenolic compound, is widely distributed in various fruits and vegetables. It is suggested to show some pharmacological effects such as antioxidant, antimicrobial, and anticancer. However, there is not enough data about the cytotoxicity of sinapic acid; the available data are limited. This study was aimed to assess the cytotoxic profiles of sinapic acid in a wide range of concentrations for 18 h exposure in two different cell lines, Chinese hamster lung fibroblasts (V79) and human cervical carcinoma (HeLa) cells using Neutral Red Uptake assay. The concentrations up to 500 µM and 2000 µM had no significant effect on V79 and HeLa cells, respectively, but the cell viabilities decreased below 50 % at concentrations higher than 1000 µM and 5000 µM for V79 and HeLa cells, respectively. IC50 values were found to be 1860 µM and 7248 µM in V79 and HeLa cells, respectively. This study has shown that sinapic acid have no cytotoxic effects in two different cell lines except at very high concentrations.

Abstract | Full Text PDF

The antineoplastic drug Busulfan can lead to impaired antioxidant defense system. Silymarin as a natural herbal product has powerful antioxidant properties. In the present study, the effects of Busulfan and Silymarin on oxidative stress system were evaluated. For the study 48 rats were prepared and fed with special ration, then they were divided to 6 groups with 8 rats in each group: (C1): no drugs, (C2): 175 mg/kg/day Silymarin for 14 days as gavage, (C3): 20 mg/kg/day Busulfan for 14 days intra peritoneal, (T1): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 175 mg/kg/day Silymarin for 14 days as gavage, (T2): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 250 mg/kg/day Silymarin for 14 days as gavage, (T3): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 325 mg/kg/day Silymarin for 14 days as gavage. The amount of MDA, SOD and GPX in the different tissue extracts (liver, spleen, pancreas, testes, heart and kidneys) were measured. The results of this study showed that after Busulfan treatment, the activity of SOD and GPX in different tissues was significantly decreased. Silymarin in C1 could increase the activity of SOD and GPX compared to C3. In C3, the level of MDA in different tissues compared to other the groups was significantly increased. Silymarin in C1 could decrease the level of MDA compared to C3. It can be concluded that the use of Busulfan can induce oxidative stress and Silymarin had an antioxidant role along with decreasing the lipid peroxidation.

The antineoplastic drug Busulfan can lead to impaired antioxidant defense system. Silymarin as a natural herbal product has powerful antioxidant properties. In the present study, the effects of Busulfan and Silymarin on oxidative stress system were evaluated. For the study 48 rats were prepared and fed with special ration, then they were divided to 6 groups with 8 rats in each group: (C1): no drugs, (C2): 175 mg/kg/day Silymarin for 14 days as gavage, (C3): 20 mg/kg/day Busulfan for 14 days intra peritoneal, (T1): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 175 mg/kg/day Silymarin for 14 days as gavage, (T2): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 250 mg/kg/day Silymarin for 14 days as gavage, (T3): 20 mg/kg/day Busulfan for 14 days intra peritoneal and after 2 weeks 325 mg/kg/day Silymarin for 14 days as gavage. The amount of MDA, SOD and GPX in the different tissue extracts (liver, spleen, pancreas, testes, heart and kidneys) were measured. The results of this study showed that after Busulfan treatment, the activity of SOD and GPX in different tissues was significantly decreased. Silymarin in C1 could increase the activity of SOD and GPX compared to C3. In C3, the level of MDA in different tissues compared to other the groups was significantly increased. Silymarin in C1 could decrease the level of MDA compared to C3. It can be concluded that the use of Busulfan can induce oxidative stress and Silymarin had an antioxidant role along with decreasing the lipid peroxidation.

Abstract | Full Text PDF

In the whole world, a large number of plants have therapeutic potential and used in the treatment of various diseases in different populations. Heliotropium (Boraginaceae) is a widely spread genus of plants found in the temperate and the tropical regions of both hemispheres and used for the treatment of diseases from ancient times. In folk medicine history, the plants of genus Heliotropium include treatments of inflammations, gout, rheumatism, skin diseases, menstrual disorder, and poisonous bites. Phytochemical reports on genus Heliotropium revealed the presence of many bioactive components especially pyrrolizidine alkaloids, terpenoids and flavonoids. A large number of extracts and bioactive constituents of different species of genus Heliotropium revealed significant biological activities such as antimicrobial, antitumor, antiviral, anti-inflammatory, wound healing, cytotoxicity and phytotoxicity. Different parts of plants of genus Heliotropium are examined for valuable pharmacognostic properties.Although it’s medicinal importance is recognized worldwide, this review artifact will thus, comprehensively describes the various medicinal effects of the plants, isolation of a large number of secondary metabolites and important pharmacognostic characteristics of genus Heliotropium of Boraginaceae family.

In the whole world, a large number of plants have therapeutic potential and used in the treatment of various diseases in different populations. Heliotropium (Boraginaceae) is a widely spread genus of plants found in the temperate and the tropical regions of both hemispheres and used for the treatment of diseases from ancient times. In folk medicine history, the plants of genus Heliotropium include treatments of inflammations, gout, rheumatism, skin diseases, menstrual disorder, and poisonous bites. Phytochemical reports on genus Heliotropium revealed the presence of many bioactive components especially pyrrolizidine alkaloids, terpenoids and flavonoids. A large number of extracts and bioactive constituents of different species of genus Heliotropium revealed significant biological activities such as antimicrobial, antitumor, antiviral, anti-inflammatory, wound healing, cytotoxicity and phytotoxicity. Different parts of plants of genus Heliotropium are examined for valuable pharmacognostic properties.Although it’s medicinal importance is recognized worldwide, this review artifact will thus, comprehensively describes the various medicinal effects of the plants, isolation of a large number of secondary metabolites and important pharmacognostic characteristics of genus Heliotropium of Boraginaceae family.

Abstract | Full Text PDF

Rekombinant DNA teknolojisindeki ilerlemelerin doğal sonucu olarak, kalıtsal hastalıkların iyileştirilmesi için gen tedavisi gündeme gelmiştir. Gen tedavisinde amaç, vücuttan alınan hücreler içinde yeni genetik materyalin tanıtılmasıyla, enfeksiyon ve genetik hastalıkların tedavisidir. Çalışmamızın amacı, katı lipit nanopartiküler (KLN) sisteme, katyonik bir lipit yardımıyla katyonik özellik kazandırılarak, DNA’ya elektrostatik etkileşme ile bağlanabilecek yeni bir gen taşıyıcı sistem geliştirmektir. SLN’lerin hazırlanmasında lipit matris olarak mono-, di- ve trigliserid karışımı (Gelucire 50/13 Pastilles) ve gliserol distearat (Precirol ATO 5) olmak üzere farklı iki lipit seçilmiştir. Hazırlanan katyonik katı nanopartikülleri, partikül boyutu 50.55 nm ve 168.2 ± 0.35 nm aralığında bulunmuştur. Kararlılıkları için önemli özellik olan zeta potansiyelleri ise -50.2 ± 0.1 ile +37.1 ± 0.63 mV aralığında belirlenmiştir. Katyonik lipidin oranının arttırılması ile SLN’lerin zeta potansiyelinde ve 293 HEK hücrelerinde toksik özelliğinin arttığı gözlenmiştir. SLN’lerin DNA bağlama yetilerinin farklılık gösterdiği belirlenmiştir.

As a natural result of the progresses made in the recombinant DNA technology, the gene treatment has been brought forward for the improvement of genetic disorders. The purpose of the gene therapy is the treatment of the infection and genetic disorders with the introduction of new genetic materials among cells taken from the body. The objective of our study is to develop a new gene carrier system that can bind the DNA through electrostatic interaction by cationic solid lipid nanoparticulate (SLN) system with the help of a cationic lipid. In preparation of the SLNs, two different lipids including mono-, di- and triglyceride mixtures (Gelucire 50/13 Pastilles) and glycerol distearate (Precirol ATO 5) were selected as lipid matrixes. The particle sizes of the prepared cationic solid lipid particles were found to be between 50.55 ± 0.12 and 168.2 ± 0.35 nm. Their zeta potentials which constitute of an important characteristic for the stability were determined to be between -50.2 ± 0.16 and +37.1 ± 0.63 mV. Increasing the ratio of cationic lipids in SLN have been observed to increase the zeta potentials and the toxic properties on HEK 293 cells of SLNs. The DNA binding abilities of SLNs were found to be varied.

Abstract | Full Text PDF