GİRİŞ ve AMAÇ: Anadolu’da “Sığır kuyruğu” olarak adlandırılan Verbascum L. (Scrophulariaceae) cinsi, ülkemizde 193’ü endemik olmak üzere 248 tür ile temsil edilmektedir. Çiçekleri müsilaj, uçucu yağ ve glikozitler taşır. Bazı Verbascum türleri halk arasında göğüs yumuşatıcı ve balgam söktürücü olarak, adet sancısını gidermede, yatıştırıcı, romatizma ağrılarını giderici ve ayrıca hayvan yaralarını tedavi etmekte kullanılmaktadır. Verbascum pestalozzae Boiss. ve Verbascum pycnostachyum Boiss. & Heldr. türlerinin kök, gövde ve yaprak anatomik yapıları ilk kez bu çalışmada verilmiştir. Araştırmalar sonucunda türlerin gövde ve yaprak anatomik özellikleri belirlenmiş ve veriler detaylı fotoğraflarla desteklenmiştir. Gen merkezi Anadolu olmasına rağmen Verbascum ile ilgili yeterli çalışmaların bulunmaması ve taşıdığı sekonder metabolitler ile potansiyel bir tıbbi bitki olması çalışmanın önemini artıracaktır.
YÖNTEM ve GEREÇLER: V. pestalozzae ve V. pycnostachyum'a ait örnekler C3 Antalya'dan toplanmış, Akdeniz Üniversitesi Biyoloji Bölümü ve Anadolu Üniversitesi Eczacılık Fakültesi Herbaryumuna konulmuştur. Türlerin teşhisi Türkiye Florası ve Doğu Ege Adaları kullanılarak belirlenmiştir. Anatomik çalışmalar için, örnekler doğal habitatlardan toplanmış ve% 70 alkolde tutulmuştur. Araştırmada, olgun ve çiçekli bitkilerin kök, gövde ve yaprakları kullanılmıştır. Kök, çiçekli gövde ve yaprak kesitleri üzerinde incelemeler yapılmış. Salgı e örtü tüylerinin anatomik yapıları Leitz SM-LUX binoküler mikroskop kullanılarak çizimler yapılmıştır. Kesitler gliserin jelatin ile daimileştirilip, Sartur reaktifiyle boyanmış ve fotoğraflar ışık mikroskobu (Olympus BX51T) ile çekilmiştir.
BULGULAR: V. pestalozzae ve V. pycnostachyum'un kök, gövde ve yapraklarından alınan kesitler incelenmiş ve bu bitkilere ait anatomik özellikler belirlenerek şekil 4-12 ve Tablo 1'de ayrıntılı olarak verilmiştir.
TARTIŞMA ve SONUÇ: İki türe ait anatomik özellikler genellikle Metcalfe ve Chalk (20) ve diğerlerinde (21-24) belirtilen diğer bulgularla uyumludur. Sonuçlarımızın, taksonomistlere ek kanıt sağlamak için gerçekleştirildiğine ve türlerin ayrılmasına yardımcı olabileceğine inanıyoruz. Türler üzerinde taksonomik, morfolojik ve anatomik bir çalışma olmaması, araştırmanın sistematik olarak tanıtımı için önemli hale getirmiştir.

INTRODUCTION: The genus Verbascum L. (Scrophulariaceae) known as “sığır kuyruğu” in Anatolia is represented by 248 species, 193 of them are endemic. The flowers contain essential oil, musilage and glycosides. Some species’ of Verbascum have some folkloric usages as expectorant, sedative and the treatment of dysmenorrhoea and rheumatalgia. It was also notified the usage for healing wounds in animal care. In this study, anatomical structures of root, stem and leaves of Verbascum pestalozzae Boiss. and Verbascum pycnostachyum Boiss. & Heldr. are given for the first time. According to the results, some of the differences between stem and leaf anatomical features of these species were described and the data were supported by detailed photographs. Although, Anatolia is the center of the Verbascum genes, there is not enough studies about Verbascum species. It will increase the importance of this project that being potential medicinal plant and has secondary metabolites.
METHODS: species have been collected from C3 Antalya: Voucher specimens of V. pestalozzae and V. pycnostachyum are deposited in the Herbarium of the Biology Department, Akdeniz University in Antalya, Turkey and Herbarium of the Faculty of Pharmacy, Anadolu University in Eskisehir (ESSE), Turkey. The materials were identified as V. pestalozzae and V. pycnostachyum using Flora of Turkey and the East Aegean Islands. For anatomical studies, samples have been collected from the irnatural habitats and kept in 70% alcohol. In the research, root, stem and leaves of mature and flowered plants have been used. Investigations were performed on the cross-sections of the root, the flowering stem and the leaf. The anatomical structures of glandular and covering hairs were drawn by using Leitz SM-LUX binocular microscope. All sections were embedded in glycerin jelatine and stained by Sartur reactive and photographs were taken through a light microscope (Olympus BX51T).
RESULTS: The cross sections taken from root, stem and leaves of V. pestalozzae and V. pycnostachyum are examined and the anatomic features belonging to these plants are determined, compared and showed in Figs. 4-12 and in Table 1.
DISCUSSION AND CONCLUSION: The anatomical properties belonging to two species have generally compatible with findings of Metcalfe and Chalk (20) and others signified in the genus (21-24). We believe that our results were carried out to provide additional evidence for taxonomists and it can be help to separate of species. The lack of a taxonomic, morphological and anatomical study on the species made it important for the systematic introduction of the research.

GİRİŞ ve AMAÇ: Diyabet, vücudumuzun fizyolojisini etkileyen, kronik bir hastalıktır. Tedavi edilmeyen Diabetes mellitus, diyabetik retinopati, diyabetik nefropati ve diyabetik nöropati, oto bağışıklık hastalıkları, Ployuria, Polidipsia, kilo kaybı ve kardiyovasküler hastalıklar gibi hastalıklara neden olur. Diabetes mellitus tedavisinde kullanılan ilaçlar, uzun süreli kullanımda yan etkilere neden olur, bazen ölüme yol açar. Günümüzde araştırmacılar, yan etkileri düşük veya hiç olmayan bitkilerden yeni anti diyabet ilaçları keşfediyorlar. Bu açıdan, bu çalışma Zornia gibobosa'nın anti-diyabetik etkinliğini değerlendirmek için yapıldı.
YÖNTEM ve GEREÇLER: Akut toksisite çalışması OECD kılavuzlarına göre Z. gibbosa etil asetat ve etanol (%70 v/v) ekstreleri için yürütülmüştür. Seçilen bitki ekstraktlarının anti diyabetik aktivitesi, sıçanlar modelinde alloksanla indüklenen diyabet kullanılarak test edildi.
BULGULAR: Uygulanan Zornia gibobosa özütlerinin dozunda herhangi bir ölüm görülmedi. Test edilen özütler, alloksana bağlı şekerli diyatermeler nedeniyle oluşan fizyolojik değişiklikleri önemli ölçüde (P≤0.01) eski haline getirdi. 500 mg / kg vücut ağırlığında hidroalkolik özütler standart ilaç (Glibenclamide) ile birlikte daha fazla aktivite gösterdi. Zornia gibobosa, glikoz konsantrasyonunu önemli ölçüde düşürdü ve şeker hastalığının farklı organlara hasar vermesiyle değişmiş enzim düzeylerini geri kazandırdı.
TARTIŞMA ve SONUÇ: Z. gibbosa önemli antidiyabetik aktiviteye sahiptir (Glükoz düşürücü). Bu nedenle, diabet tedavisinde allopatik tıp ile birlikte geç komplikasyonları yanında adjuvan bir ilaç olarak da kullanılabilir.

INTRODUCTION: Diabetes mellitus is a chronic disease, lifelong condition that affects our body physiology. The untreated Diabetes mellitus causes diseases like diabetic retinopathy, diabetic nephropathy and diabetic neuropathy, auto immune diseases, Ployuria, Polydipsia, loss of weight and cardiovascular diseases. The use of medications for treatment of diabetes mellitus causes the side effects on long term use, sometimes leads to death. Today, researchers are working in the discovery of new anti-diabetes drugs from plants with low or no side effects. In this point of view, the present work was carried out to evaluate the anti-diabetic activity of Zornia gibbosa Span.
METHODS: The acute toxicity study was conducted for ethyl acetate and ethanol (70%v/v) extracts of Z. gibbosa as per OECD guidelines. The anti diabetic activity of selected plant extracts were tested using alloxan induced diabetes in rats model.
RESULTS: There was no mortality observed in the administered doses of Zornia gibbosa Span extracts. The tested extracts significantly (P≤0.01) restored the physiological changes occurred due to the alloxan-induced diabetes mellitus. The hydroalcoholic extracts at 500 mg/kg body weight concentration showed more activity compared to other extracts at different concentrations along with standard drug (Glibenclamide). Zornia gibbosa has significantly decreased the glucose concentration and restored the altered enzymes levels by different organs damage by diabetes.
DISCUSSION AND CONCLUSION: The results of present study indicates that, Z. gibbosa has significant anti-diabetic activity. Therefore, it be capable of be use as an alternate medicine along with allopathic medicine in treatment of diabetes as well as its health problems.

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GİRİŞ ve AMAÇ: Bu çalışmanın amacı, sumatriptanın iskemi reperfüzyonun (IR) sıçanlarda neden olduğu kardiyak hasar ve iskemik ön-koşullamanın (IPC) oluşturduğu koruyuculuk üzerine etkisini incelemek.
YÖNTEM ve GEREÇLER: Sıçanlar rastgele olarak gruplara bölündü: IR, Sumatriptan IR (SUM-IR), IPC ve Sumatriptan IPC (SUM-IPC) grupları. Ortalama arteriyel kan basıncı ve kalp atım hızı, basınç hız ürününü (PRP) hesaplamak için kaydedildi. Aritmi parametrelerini değerlendirmek için standart elektrokardiyogramlar kaydedildi.
BULGULAR: SUM-IPC grubundaki PRP değerleri, SUM-IR grubundakilerden reperfüzyon başlangıcında anlamlı olarak daha düşüktü (p<0.05). IPC, SUM-IR ve SUM-IPC gruplarındaki ventriküler taşikardi (VT) insidansı, IR grubundakinden anlamlı olarak daha düşüktü (p<0.05). Ventriküler fibrilasyon (VF) sadece IR grubunda gözlendi.
TARTIŞMA ve SONUÇ: Sumatriptan’ın IPC’ nin koruyucu etkisi kadar olmasa da, kalbi IR hasarına karşı koruduğu gözlenmiştir. Sumatriptan VT’ye karşı IPC’nin oluşturduğu koruyuculuğu kısmen azaltsa da, VF’ye karşı önleyici etkisi iskemik koşullarda kalp için koruyucu olabilir.

INTRODUCTION: The aim of this study was to investigate the effect of sumatriptan in cardiac injury caused by ischemia-reperfusion (IR) in rats and its effect on ischemic preconditioning (IPC)-induced protection.

METHODS: The rats were randomly divided in groups: IR, Sumatriptan IR (SUM-IR), IPC and Sumatriptan IPC (SUM-IPC) groups. Mean arterial blood pressure and heart rate were recorded to calculate pressure rate product (PRP). Standard limb lead II electrocardiograms were recorded to evaluate arrhythmia parameters.

RESULTS: The PRP values in the SUM-IPC group were significantly lower than SUM-IR group at the beginning of reperfusion (p<0.05). The incidence of ventricular tachycardia (VT) in the IPC, SUM-IR and SUM-IPC groups were significantly lower than the IR group (p<0.05). The ventricular fibrillation (VF) was only observed in the IR group.

DISCUSSION AND CONCLUSION: Sumatriptan protects the heart against IR injury but not as protective as IPC alone. Although sumatriptan diminishes IPC-induced protection against VT, the preventive effect of sumatriptan against VF may be predictive for cardioprotection in the ischemic conditions.

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GİRİŞ ve AMAÇ: Son yıllarda, medisinal kimyada farmakolojik olarak aktif halkaların moleküler hibridizasyonuna dayalı antikolinesteraz ajanlar tasarlamak ilgi çekmektedir. Bu amaçla, burada tiyazol ve pirazolin halkalarının moleküler hibridizasyonuna dayalı antikolinesteraz ajanlar tasarlamayı ve sentezlemeyi hedefledik.
YÖNTEM ve GEREÇLER: 3-(2-Furil)-5-(1,3-benzodioksol-5-il)-1-tiyokarbamoil-4,5-dihidro-1H-pirazolün fenaçil bromürlerle halka kapanma reaksiyonu ile yeni tiyazolil-pirazolin türevleri sentezlendi. Bileşikler, Ellman'ın spektrofotometrik yönteminin bir modifikasyonu kullanılarak asetilkolinesteraz (AChE) ve bütirilkolinesteraz (BuChE) üzerindeki inhibe edici etkileri bakımından araştırıldı. Bu çalışmanın bir parçası olarak, bileşiklerin Lipinski'nin beş kuralına uyumluluğu değerlendirildi. Fizikokimyasal parametreler (log P, TPSA, nrotb, molekül ağırlığı, hidrojen bağı donörlerinin ve alıcılarının sayısı, molekül hacmi) Molinspirasyon yazılımı kullanılarak hesaplandı.
BULGULAR: Bu seride, 2-[5-(1,3-benzodioksol-5-il)-3-(2-furil)-4,5-dihidro-1H-pirazol-1-il]-4-(4-florofenil)tiyazol en güçlü BuChE inhibitörü (%43.02±2.71) olarak bulunurken, 2-[5-(1,3-benzodioksol-5-il)-3-(2-furil)-4,5-dihidro-1H-pirazol-1-il]-4-(naftalen-2-il)tiyazolün en etkili AChE inhibitörü (%38.5±2.85) olduğu bulundu. Bu bileşikler, sadece Lipinski'nin beş kuralının bir parametresini ihlal etti. Lipinski'nin kuralına dayanarak, makul oral biyoyararlanımına sahip olmaları beklenir.
TARTIŞMA ve SONUÇ: Bu çalışmanın ışığında, etkinliği arttırılmış yeni kolinesteraz inhibitörlerinin üretilmesi için tanımlanmış bileşiklerin yapısal modifikasyonu devam etmektedir.

INTRODUCTION: In recent years, the design of anticholinesterase agents based on molecular hybridization of pharmacologically active scaffolds has attracted a great deal of interest in medicinal chemistry. For this purpose, herein we aimed to design and synthesize anticholinesterase agents based on molecular hybridization of thiazole and pyrazoline scaffolds.
METHODS: New thiazolyl-pyrazoline derivatives were synthesized via the ring closure reaction of 3-(2-furyl)-5-(1,3-benzodioxol-5-yl)-1-thiocarbamoyl-4,5-dihydro-1H-pyrazole with phenacyl bromides. The compounds were investigated for their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) using a modification of Ellman’s spectrophotometric method. As a part of this study, the compliance of the compounds to the Lipinski’s rule of five was evaluated. The physicochemical parameters (log P, TPSA, nrotb, molecular weight, number of hydrogen bond donors and acceptors, molecular volume) were calculated using Molinspiration software.
RESULTS: 2-[5-(1,3-Benzodioxol-5-yl)-3-(2-furyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(naphthalen-2-yl)thiazole was found to be the most effective AChE inhibitor (38.5±2.85%), whereas 2-[5-(1,3-benzodioxol-5-yl)-3-(2-furyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(4-fluorophenyl)thiazole was found as the most potent BuChE inhibitor (43.02±2.71%) in this series. These compounds only violated one parameter of Lipinski’s rule of five. On the basis of Lipinski’s rule, they were expected to have reasonable oral bioavailability.
DISCUSSION AND CONCLUSION: In the view of this study, the structural modification of the identified compounds is on-going for the generation of new cholinesterase inhibitors with enhanced efficacy.

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INTRODUCTION: Levosulpiride is a widely used gastroprokinetic agent in the treatment of various gastric disorders however its short half-life and increased dosage frequency leads to non-compliance and possible adverse effects. The prime objective of the current study was to develop a sustained release formulations of Levosulpiride incorporating bioresorbable cellulose derivatives.
METHODS: The sustained release formulations of Levosulpiride were prepared through Direct compression method using various cellulose derivatives like Carboxymethyl cellulose sodium, Hydroxypropyl cellulose and Hydroxypropyl methyl cellulose in different polymer to drug weight ratios as release modifying polymers. The powders blend as well as compressed tablets were then subjected to pre-compressional and post-compressional evaluation as well as FTIR analysis. The in-vitro release studies were carried out for all formulations of the model drug in buffer solution of pH 6.8 at a wave length of 214nm by using UV/Visible spectrophotometer.
RESULTS: The FTIR results confirmed that the interaction between components was physical and out of the different kinetic models data the release profile was best expressed by Higuchi model as the results shows high linearity. The results also shown formulation F9 to be the ideal one among the developed formulations exhibiting sustained release behavior.
DISCUSSION AND CONCLUSION: Levosulpiride sustained release matrices were prepared successfully utilizing CMC Sodium, HPC and HPMC as release retarding polymer/carrier.

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INTRODUCTION: Response surface methodology coupled with statistically designed experiment has been found to be very useful in optimising multivariable processes. The aim of this study is to evaluate the influence of two independent variables, a ratio of permeation enhancers/antioxidants (Transcutol and ethanolic extract of Tetracarpidium conophorum EETC) and stirring rate, on the flux and permeation of gentamicin hydrogel.
METHODS: A modification of free radical initial polymerization was utilized to formulate the gentamicin hydrogel. A 3² factorial central composite design (CCD) was then utilized to investigate the effect of independent variables of permeation enhancer Transcutol: EETC (X1), Stirring speed (X2) via 14 formulation batches which were evaluated for dependent variables Flux (Y1) and amount of drug permeated after 12 hours (Y2) ex-vivo.
RESULTS: The results of analysis of variance (ANOVA) carried out to determine the fit of the models revealed that the models were statistically significant (p < 0.05) and did not show lack of fit (R2 > 0.80). The regression equation generated for flux was Y1 = 19.35 – 25.82X1 – 0.044X2 + 0.0097X1X2 + 11.86X21 and for cumulative permeation of gentamicin in 12 hours Y2= 315.50 – 189.67X1 + 0.28X2 -1.29X1X2 + 123.55X21. The validity of the statistical models used for predicting flux and drug permeation was confirmed by carrying out three confirmation experimental runs at the identified optimum conditions. The results showed that there was no significant difference between the experimental results and those predicted by the statistical models.
DISCUSSION AND CONCLUSION: The excellent correlation between the predicted and measured values shows the validity of statistical models (R2= 0.95). Utilization of antioxidant and permeation enhancer has been used for the first time to investigate the influence on dependent variables. Optimization of gentamicin hydrogel using central composite statistical design is valid for prediction of drug permeation and flux utilizing variables in formulation.

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GİRİŞ ve AMAÇ: Bu çalışmanın amacı; Türkiye'de halk arasında yaygın olarak kullanılan bitkilerden elde edilen uçucu yağların antimikrobiyal etkilerini araştırmak ve bu etkilerden yola çıkarak ağız enfeksiyonlarında kullanılmak üzere gargara formülasyonu hazırlamaktır.
YÖNTEM ve GEREÇLER: Uçucu yağlar, bitkilerden (Origanum vulgare L. ssp. hirtum, Rosmarinus officinalis L., Laurus nobilis L., Salvia fruticosa Mill.) su distilasyonu metodu ile Clevenger apareyi kullanılarak elde edilmiştir. Elde edilen uçucu yağlar ve % 4.5 ve % 9.0 oranlarında uçucu yağların karışımını içeren gargara formülasyonlarının antimikrobiyal aktiviteleri disk difüzyon metodu ve mikrobroth dilüsyon metodu ile araştırılmıştır.
BULGULAR: Bu çalışmada antimikrobiyal aktivite disk difüzyon metodu ve mikrobroth dilüsyon metoduyla değerlendirilmiştir. İnhibisyon zon çaplarının 7-59 mm arasında değişkenlik gösterdiği belirlenmiştir. Uçucu yağlar, mikroorganizmalar üzerine saf olarak uygulandığında statik ve sidal etkinliğin genellikle % 50 ve % 50’ nin üzerinde olduğu gözlenmiştir. % 4.5 oranında uçucu yağ karışımı içeren F2 formülasyonunun Staphylococcus aureus ATCC 25923 üzerindeki minimum bakterisidal etkisinin % 6.25 olduğu ve diğer tüm mikroorganizmalar üzerinde minimum inhibitör konsantrasyon ve minimum bakterisidal konsantrasyonunun % 3.125 olduğu bulunmuştur. Uçucu yağ örneklerinin mikroorganizmalar üzerine saf olarak uygulandığında gösterdikleri antimikrobiyal etkinin, gargara formülasyonlarına göre daha düşük olduğu; ayrıca % 4.5 oranında uçucu yağ karışımı içeren F2 formülasyonunun, % 9.0 oranında uçucu yağ karışımı içeren F1 formülasyonuna göre test edilen tüm mikroorganizmalar üzerine daha yüksek antimikrobiyal etkiye sahip olduğu bulunmuştur.
TARTIŞMA ve SONUÇ: Elde edilen sonuçlar uçucu yağların karışımı ile hazırlanan F1 ve F2 formülasyonlarının, test edilen mikroorganizmalara karşı antimikrobiyal etkiye sahip olduğunu ortaya koymuştur. Ayrıca çalışma sonucunda F2 formülasyonunun test edilen mikroorganizmalar üzerinde önemli oranda antimikrobiyal aktiviteye sahip olduğu rapor edilmiştir.

INTRODUCTION: The aim of this study was to prepare pharmaceutical formulations of mouthwashes and examine the antimicrobial activities of essential oils obtained from plants used traditionally in Turkey for oral infections.
METHODS: Essential oils were obtained from herbal drugs with water distillation method using of Clevenger apparatus. Antimicrobial capacities of mouthwash formulations containing mixture of essential oils with proportions of 4.5 % and 9.0 % were examined by disc diffusion method and microbroth dilution method.
RESULTS: In study, antimicrobial activity was evaluated by disc diffusion method and microbroth dilution method. The inhibition zone diameters were determined to vary between 7-59 mm. It has been observed that the static and cidal activity was generally 50% and greater than 50%, when pure essential oil samples were applied on microorganism specimens. Formulation F2 containing mixture of essential oils with proportions of 4.5%, showed 6.25 % minimum bactericidal effect on Staphylococcus aureus ATCC 25923 and 3.125 % the minimum inhibitor concentration and minimum bactericidal concentration on all other microorganisms. It is found that the antimicrobial effect of pure essential oil samples applied on microorganisms, was lower than mouthwashes formulations; the antimicrobial effect of F2 formulation containing mixture of essential oils with proportions of 4.5% was higher than formulation F1 containing mixture of essential oils with proportions of 9%.
DISCUSSION AND CONCLUSION: The results obtained by these methods allow us to conclude that the essential oils and prepared F1 and F2 mouthwash formulations exert activity against microorganisms affecting the oral cavity. It has also been reported that the F2 formulation has significantly antimicrobial activity on the tested microorganisms.

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GİRİŞ ve AMAÇ: Bu çalışmanın amacı, farklı bitkisel zayıflama ürünlerinde arbutin ve hidrokinonun gaz kromatografisi-kütle spektrometresi yöntemiyle, eşzamanlı olarak belirlenmesi için basit, hassas ve spesifik bir yöntem geliştirmektir.


YÖNTEM ve GEREÇLER: Türkiye'de bulunan dokuz bitkisel zayıflama ürününün sulu ve metanolik ekstreleri, arbutin ve hidrokinon analizi için gaz kromatografisi-kütle spektrometresi yöntemi ile değerlendirilmiştir.
BULGULAR: Arbutin ve hidrokinon için alıkonma zamanları sırasıyla 11.32 ve 5.44 dakika olarak bulunmuştur. Geliştirilen yöntemin doğrusallık aralığı arbutin ve hidrokinon için 5-500 ng/mL’dir. Kalite kontrol numunelerinden belirlenen ve bağıl standart sapma olarak ifade edilen gün-içi ve günler-arası kesinlik, arbutin ve hidrokinon için sırasıyla %1.94 ve %2.73'ten düşüktür. Bağıl hataya göre doğruluk değerleri arbutin ve hidrokinon için sırasıyla %1.13 ve %2.56 arasındadır. Gözlenebilme ve miktar tayin sınırı arbutin için sırasıyla 0.555 ve 1.665 ng/mL, hidrokinon için 0,031 ve 0,093 ng/mL’ dir.
TARTIŞMA ve SONUÇ: Geliştirilen yöntem, farklı bitkisel zayıflama ürünlerinde arbutin ve hidrokinonun rutin kalite kontrol analizleri için kullanılabilir.

INTRODUCTION: The aim of our study was to development of simple, precise, sensitive and specific method for the simultaneous determination of arbutin and hydroquinone in different herbal slimming products by gas chromatography-mass spectrometry method.


METHODS: The methanol and aqueous extracts of nine herbal slimming products in Turkey were evaluated for analysis of arbutin and hydroquinone by gas chromatography-mass spectrometry method.
RESULTS: The retention times of arbutin and hydroquinone were found 11.32 and 5.44 min, respectively. The linear ranges in this developed method were 5-500 ng/mL for arbutin and hydroquinone, respectively. The intra- and inter-day precisions, expressed as the relative standard deviation, were less than 1.94 and 2.73%, determined from quality control samples for arbutin and hydroquinone, and accuracy was within 1.13 and 2.56% in terms of relative error, respectively. Limit of detection and quantification for arbutin were 0.555 and 1.665 ng/mL, for hydroquinone 0.031 and 0.093 ng/mL, respectively.
DISCUSSION AND CONCLUSION: The developed method can be used for routine quality control analysis of arbutin and hydroquinone in different herbal slimming products.

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GİRİŞ ve AMAÇ: Bu çalışmada Temozolomid’in farmasötik formundan tayini için doğru, kesin ve basit bir yüksek basınçlı sıvı kromatografi yöntemi geliştirilmiştir.
YÖNTEM ve GEREÇLER: DAD dedektörlü HPLC yöntemi ICH kurallarına göre valide edilmiştir. C18 kolon (150x4.6 mm. i.d., 5 µm tanecik boyutu) ve hareketli faz olarak sulu asetat tampon (0.02 M)- asetonitril (90: 10, h/h) (pH 4.5) karışımı kullanılmıştır.
BULGULAR: Doğrusal aralık ve LOD değerleri sırası ile 5-100 µg/mL and 0,02 µg/mL’dir. Yöntemin doğruluğu geri kazanım yöntemi ile belirlenmiş ve %98.8-100.3 olarak bulunmuştur. Bu çalışmaların yanı sıra bozunma çalışmaları yapılmıştır. Bozunma çalışmaları asidik, bazik, oksidatif ve termal bozunma şartlarında gerçekleştirilmiştir.
TARTIŞMA ve SONUÇ: Önerilen metot ilacın miktar tayini ve bozunma çalışması için başarı ile uygulanmıştır.

INTRODUCTION: In the present study, an accurate, precise and simple method has been developed for the determination of Temozolomide (TMZ) in its pharmaceutical form by using high-performance liquid chromatography (HPLC).
METHODS: HPLC method with diode array detector (DAD) was validated according to ICH guidelines. A C18 column (150x4.6 mm. i.d., 5 µm particle size) and an aqueous acetate buffer (0.02 M)–acetonitrile (90: 10, v/v) (pH 4.5) as a mobile phase were used.
RESULTS: The linear range and LOD value were 5-100 µg/mL and 0,02 µg/mL, respectively. The accuracy of the method was determined by recovery test and found to be 98.8-100.3%. In addition, forced degradation studies of the drug were also performed in bulk drug samples to demonstrate the specificity and stability-indicating. The degradation studies under acidic, basic, oxidative and thermal degradation conditions were applied.
DISCUSSION AND CONCLUSION: Proposed method could be applied successfully for the determination and the identification of degradation of the drug.

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INTRODUCTION: The aim of present study was to obtained crystallo-co-agglomerates of ritonavir to improve the solubility, dissolution rate and other physicochemical properties.


METHODS: Ritonavir agglomerates were prepared by crystallo-co-agglomeration (CCA) technique. Acetone–water containing HPMC K-15, PEG-6000, PVP K-30 was used as the crystallization medium. The agglomerates were evaluated for saturation solubility, micromeritic properties, yield and drug content. The agglomerates were also characterized by Fourier Transforms Infra-red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRPD) and Scanning Electron Microscopy (SEM).
RESULTS: The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to the fragmentation which occurred during compression. DSC and XRD studies showed that ritonavir particles crystallized in the presence of HPMC, PEG-6000, PVP K-30 and diluents did not undergo structural modifications. The dissolution rate of ritonavir from the agglomerates could be controlled by the amount of included diluents, being enhanced as the latter was increased. Moreover, the results showed that when the diluents were included both intra-granularly and extra-granularly during agglomeration of ritonavir particles.
DISCUSSION AND CONCLUSION: Thus the crystallo-co agglomeration was successfully applied to improve the physicochemical properties of ritonavir.

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Amaç: Bu çalışmada V. mucronatum Lam.’ın sekonder metabolitlerinin belirlenmesi ve antimikrobiyal aktivitelerinin değerlendirilmesi amaçlanmıştır.
Gereç ve Yöntemler: İzole edilen metabolitlerin, bakteri (Escherichia coli ATCC 25922, Enterococcus faecalis ATCC 29212, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 29213) ve mantarlara (Candida albicans ATCC 90028, C. krusei ATCC 6258, C. parapsilosis ATCC 90018) karşı antimikrobiyal aktiviteleri sıvı mikrodilüsyon yöntemiyle belirlenmiştir.
Bulgular: Verbascum mucronatum Lam.’ın çiçekli kısımlarının metanol ektresinin suda çözünen kısımlarından, dört iridoit glikoziti, ajugol (1), okubin (2), lasiantozit I (3), katalpol (4); iki triterpenik saponin, ilvensisaponin C (5), ilvensisaponin A (= mimengozit A) (6) ve bir feniletanoit glikoziti, verbaskozit (= akteozit) (7) izole edilmiştir.
Sonuç: Elde edilen bileşikler içinde ajugol ve ilvensisaponin A, özellikle mantarlara karşı zayıf antimikrobiyal aktivite göstermiştir.

Objectives: Determination of secondary metabolites from Verbascum mucronatum Lam. and evaluation of their antimicrobial activity were aimed in this study.
Materials and Methods: Antimicrobial activities of the isolated metabolites were determined by broth microdilution method against the bacteria (Escherichia coli ATCC 25922, Enterococcus faecalis ATCC 29212, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 29213) and the fungi (Candida albicans ATCC 90028, C. krusei ATCC 6258, C. parapsilosis ATCC 90018).
Results: Four iridoid glycosides; ajugol (1), aucubin (2), lasianthoside I (3), catalpol (4), two triterpenic saponins; ilwensisaponin C (5), ilwensisaponin A (= mimengoside A) (6), and one phenylethanoid glycoside; verbascoside (= acteoside) (7) were isolated from the water soluble parts of the methanolic extract gained flowery parts of Verbascum mucronatum Lam.
Conclusion: Within the obtained compounds, ajugol and ilwensisaponin A showed moderate antimicrobial activity especially against fungi.

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INTRODUCTION: Background/Aim The impaired wound healing is a major complication. Few factors like blood glucose level, poor circulation, Immune System Deficiency, and Infection are the root cause of impaired wound healing. Thus the present study aims at bio-synthesizing copper nanoparticles with potential antibacterial activity against wound associated pathogens.
METHODS: Materials and Methods: The copper nanoparticles were fabricated utilizing sol gel method with the mixing of Syzigium cumini leaf extract in metal salt solution. The particles were then later chararacterized by utilizing UV spectroscopy, SEM, TEM, FTIR, XRD etc. and evaluation for their antibacterial activity and its MIC against four wound associated pathogens.
RESULTS: Results: The results obtained from TEM, SEM and XRD characterization showed the particle size i.e. below 100nm and of spherical shape. The FTIR analysis showed the possibility of various bio molecules which have role in capping and stabilization of the copper nanoparticles. The particles synthesized showed antibacterial activity against four wound associated pathogens i.e. P. mirabilis, S. saprophyticus, S. pyogenes, and P. aeroginosa.
DISCUSSION AND CONCLUSION: Conclusion: The Biosynthesized copper nanoparticles showed potent antimicrobial activity, thus the antibacterial activity of the synthesized copper nanoparticles could be utilized in several biomedical applications additionally they can be exploited as a better therapeutic agent for treating infection seen in impaired diabetic wounds etc. Withal, the particles synthesized by biological route are eco-amicable, less toxic, feasible and cost efficacious.

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GİRİŞ ve AMAÇ: Amaç: Yeni antibakteriyel ilaç geliştirilme çalışmalarında indol ve türevleri önemli bir bileşik sınıfı oluşturmaktadır. Ayrıca azoller ve türevlerinin antibakteriyel ve antifungal gibi biyolojik aktivite gösterdikleri dikkat çekmektedir. Bu çalışmada 1,2,4-triazol, 1,3,4.tiyadiazol ve hidrazinkarbotiyoamid ile sübstitüe edilmiş indol türevi yeni bileşiklerin, antimikrobiyel etkinlikleri araştırılarak değerlendirilmiştir
YÖNTEM ve GEREÇLER: Gereç ve Yöntemler: Yeni bileşiklerin antimikrobiyal etkinlikleri, 2-kat seri dilüsyon yöntemi kullanılarak, Staphylococcus aureus, Methicillin-Resistant-Staphylococcus aureus (MRSA), Escherichia coli, Bacillus subtilis, Candida albicans ve Candida krusei’ye karşı araştırılarak değerlendirilmiştir.
BULGULAR: Bulgular: Yeni sentezlenen bileşiklerin Minimum İnhibisyon Konsantrasyonu (MİK), sultamisilin, ampisilin, flukonazol ve siprofloksasin gibi standart referans bileşiklere karşı belirlenmiştir.
TARTIŞMA ve SONUÇ: Sonuç: Bileşikler test edilen mikroorganizmalara karşı 3.125-50 µg/Ml gibi geniş spektrum aralığında MİK değerleri göstermişlerdir. Bu çalışmada değerli veriler elde edilmiş ve indol-triazol türevi olan 3d bileşiği antibakteriyal ve antifungal lider bileşik olarak ileri çalışmalar için gelecek vadetmektedir.

INTRODUCTION: Objectives: In new antimicrobial drug development studies, indole and its derivatives create an important class of compounds. In addition azoles and their derivatives were recognized to be associated with a variety of biological activities such as antibacterial and antifungal. In this study antimicrobial activities of some indole derivatives mainly substituted with 1,2,4-triazole, 1,3,4-thiadiazole and hydrazinecarbothioamide were investigated to evaluate their efficacy.


METHODS: Materials and Methods: Efficacy of new compounds were evaluated using the 2-fold serial dilution technique against Staphylococcus aureus, Methicillin-Resistant-Staphylococcus aureus (MRSA), Escherichia coli, Bacillus subtilis, Candida albicans and Candida krusei.
RESULTS: Results: The minimum inhibitory concentration (MIC) was determined for test compounds and for the reference standards sultamicillin, ampicillin, fluconazole and ciprofloxacin.
DISCUSSION AND CONCLUSION: Conclusion: Compounds possessed a broad spectrum of activity having MIC values of 3.125–50 µg/mL against the tested microorganisms. This study provides valuable evidence that indole-triazole derivative compound 3d has significant promise as a novel antibacterial and antifungal lead compound.

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INTRODUCTION: Aim of the study is to develop sintered floating tablets of Cefpodoxime proxetil using locust bean gum as release controlling material. Cefpodoxime proxetil [CP] is an orally administered, extended spectrum, semi-synthetic antibiotic of cephalosporin class.
METHODS: CP has short elimination half-life, possesses high solubility, chemical, enzymatic stability and absorption profiles in acidic pH, makes it suitable candidate for formulating it as gastro retentive dosage form for improved bioavailability. Camphor was used to get the desired floating properties. The prepared Cefpodoxime proxetil floating tablets were subjected to sintering technique, where the cross linkage within the polymeric structure was increased by exposing tablets to acetone vapors. Advantage with sintering is that prolong drug release can be attained at low hardness and low concentrations of polymers.
RESULTS: The prepared tablets were evaluated and found to have acceptable physicochemical properties. Formulation S2 containing locust bean gum: drug [0.3: 1.0] and camphor [10% w/w], which was exposed to acetone vapors for a period of 6 hrs has shown optimum floating properties and better dissolution profile i.e. 97.3% in 12 hrs. Hence, S2 formulation was considered as optimized formulation. The in vitro release data of optimized formulation was treated with mathematical equations and was concluded that drug release followed zero order kinetics [0.9599] with anomalous transport mechanism [0.5331].
DISCUSSION AND CONCLUSION: Based on the results, it can be concluded that sintered floating matrix tablets of Cefpodoxime proxetil containing locust bean provides a better choice for controlled release.

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GİRİŞ ve AMAÇ: Üre ve karbohidrazit türevleri önemli sitotoksik etkinlik gösteren bileşiklerdir. Bu çalışmada, bir yeni seri piridin halkası taşıyan üre ve karbohidrazit türevleri sentezlenmiş ve sitotoksik etkileri araştırılmıştır.
YÖNTEM ve GEREÇLER: Sentezlenen bileşiklerin önerilen yapıları elemental analiz, IR, 1H-NMR spektroskopik yöntemleriyle doğrulanmıştır. Sentezlenen bileşiklerin sitotoksik etki güçleri, 3-(4,5-dimetiltiyazol-2-il)-2,5-difeniltetrazolyum bromür (MTT) kullanılarak BRCA mutasyonu taşıyan HCC1937 ve Capan-1 hücre hatları olan MCF7, HeLa ve MRC5 hücreleri üzerinde tespit edilmiştir.
BULGULAR: 3a, 3b, 3c ve 3d tüm kanser hücre hatlarına karşı sitotoksik etki göstermiştir.
TARTIŞMA ve SONUÇ: Verilerimiz, 3a-d bileşiklerinin kanser hücrelerinde tümoral olmayan fibroblastlarla kıyaslandığında daha seçici olduğunu, ancak bu bileşiklerin BRCA-1 mutant homolog rekombinasyonal (HR) DNA onarımı hatalı hücrelerde ise daha fazla etkili olmadığını göstermektedir.

INTRODUCTION: Urea and carbohydrazide derivatives are important compounds exhibiting cytotoxic activities. In this study, a series of new urea and carbohydrazide derivatives containing an pyridine ring were synthesized and evaluated for cytotoxic activity.
METHODS: The proposed structures of the synthesized compounds were confirmed using elemental analysis, IR and 1H-NMR spectroscopic techniques. The cytotoxic potencies of synthesized compounds were determined by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT) on BRCA mutant carrying HCC1937 and Capan-1 cell lines as well as on MCF7, HeLa and MRC5 cells.
RESULTS: 3a, 3b, 3c and 3d showed cytotoxic activity against all cancer cell lines.
DISCUSSION AND CONCLUSION: Our data indicate that compounds 3a-3d are more selective to cancer cells compared to nontumoral fibroblasts, however these compounds are not more potent on HR defective cells with BRCA mutants.

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INTRODUCTION: Creation of new effective drugs based on plant material is relevant and a priority direction of modern pharmacy. Herbal origin preparations have recently become very popular due to the variety of therapeutic effects, provided by both individual substances and complex compounds found in plant material.
METHODS: Study of antidepressant properties of SBDE, SBRP, "Scutex" and "Scutella" drugs and reference drug conducted by mice tail suspension test (despair behavior).Antihypoxic effect was evaluated on the model of normobaric hypoxic hypoxia with hypercapnia. The impact of the studied substances on the physical endurance of mice was studied by a test of swimming with the load.
RESULTS: The obtained results indicate that SBDE at a dose of 50 mg/kg increases latent time of freezed mice. Action of SBDE exceeded the effect of reference drug "Bilobil". So SBDE possesses antidepressant action.All drugs of SB- SBDE, SBRP, "Scutex" tablets, "Scutella" capsules as well as "Bilobil" did not affect the physical endurance of mice in the test of swimming to exhaustion. So SBRP at a dose of 260 mg/kg has the most significant antihypoxic effect in terms of normobaric hypoxic hypoxia with hypercapnia and exceeds the effect of comparison drug, and at a dose of 173 mg/kg SBRP acts at the level of reference drug.
DISCUSSION AND CONCLUSION: SBDE at a dose 50 mg/kg shows antidepressant activity. SBRP at doses 173 mg/kg and 260 mg/kg does not show antidepressant action, as well as tablets "Scutex" and capsules "Scutella." SBDE, SBRP, tablets "Scutex" and capsules "Scutella" do not affect the physical endurance of mice. SBDE at a dose 50 mg/kg and SBRP at a dose of 173 mg/kg and 260 mg/kg exhibit antihypoxic activity exceeding the activity of the reference drug "Bilobil." "Scutex" tablets show no antihypoxic action and "Scutella" capsules cause probable antihypoxic action.

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GİRİŞ ve AMAÇ: Bu çalışmanın amacı, sıklıkla kullanılan tıbbi bitkilerde kurşun, kadmiyum ve okratoksin A (OTA) seviyelerinin araştırılmasıdır.
YÖNTEM ve GEREÇLER: Toplam 21 adet ıhlamur, papatya ve adaçayı örnekleri 2016 yılının bahar ve yaz aylarında İstanbul (Türkiye)’da geleneksel Pazar ve marketlerden satın alındı. Örnekler mikrodalga parçalama yöntemi uygulanarak hazırlandı ve kurşun ve kadmiyum analizi indüktif eşleşmiş plazma optik emisyon spektrometre (ICP-OES) cihazı kullanılarak gerçekleştirildi. OTA tayini immünoafinite kolonu ile temizlemenin ardından floresan detektör donanımlı yüksek performanslı sıvı kramatografisi (HPLC-FLD) ile gerçekleştirildi.
BULGULAR: OTA sadece 1 adet papatya örneğinde düşük konsantrasyonda (0,034 µg/kg) tayin edildi. ICP-OES analizi sonuçlarına göre; ıhlamur, papatya ve adaçayı örneklerinde sırasıyla kurşun 4.125-6.487 mg/kg, 3.123-5.769 mg/kg ve 3.229-5.985 mg/kg konsantrasyon aralığında; kadmiyum 0.324-0.524 mg/kg, 0.365-0.51 ve mg/kg 0.321-0.474 mg/kg konsantrasyon aralığında bulundu.
TARTIŞMA ve SONUÇ: Tıbbi bitkilerde Pb ve OTA seviyeleri maksimum izin verilen seviyelerin altında bulunmuş olup, yüksek seviyelerde bulunan Cd seviyelerinin yapılan maruziyet değerlendirmesine göre tüketici sağlığında risk oluşturmayacağı gösterilmektedir. Bununla birlikte, tıbbi bitkilerde diğer mikotoksinler ve ağır metal seviyelerinin dikkatle izlenmesi gerektiği önerilmektedir.

INTRODUCTION: The aim of this study as to determine the levels of lead, cadmium and ochratoxin A (OTA) in frequently used medicinal plants.
METHODS: Totally twenty-one samples of linden, chamomile and sage were obtained during the spring and summer period of the year 2016 from local markets and traditional bazaars in Istanbul, Turkey. Microwave-assisted digestion was applied for the preparation of the samples and inductively coupled plasma technique with optical emission spectrometry (ICP-OES) was used for the determination of lead and cadmium. Determination of OTA was carried out using high performance liquid chromatography with fluorescence detector (HPLC-FLD) after immunoaffinity column clean-up.
RESULTS: OTA was detected in only one chamomile sample with a low concentration level of 0.034 µg/kg. According to the results of ICP-OES analysis, lead in the concentration range of 4.125-6.487 mg/kg, 3.123-5.769 mg/kg and 3.229-5.985 mg/kg and cadmium in the concentration range of 0.324-0.524 mg/kg, 0.365-0.51 mg/kg and 0.321-0.474 mg/kg was found in linden, chamomile and sage teas, respectively.
DISCUSSION AND CONCLUSION: We indicated that levels of Pb and OTA were found below the maximum permissible level whereas high levels of Cd were observed in medicinal plants which may not pose health risk for the consumers according to the exposure assessment. However, it is suggested that other mycotoxins and heavy metal content should be carefully considered in medicinal plants.

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INTRODUCTION: Treatment of diseases of the biliary system is one of the urgent problems of modern medicine
METHODS: For a complex treatment of diseases of the biliary system it was proposed the original pharmaceutical drug in the form of combined tablets «Lavaflam», which include the composition of herbal components of flamin (0.05 g) and lavender oil (0.02 g). Flamin is phytomedicine from the immortelle flowers (Helichrysum arenarium (L.) Moench, Asteraceae), which contains a complex of active substances from the group of flavonoids (salipurposide, isosalipurposide, kaempferol, luteolin, etc.). It is applied as a choleretic and anti-inflammatory agent in the case of cholecystitis, cholangitis and biliary dyskinesia. Tablets were prepared by pressing for separate granulation technology.
RESULTS: Lavender oil granulate is prepared by solid phase method, as an excipient substance was used β-cyclodextrin. Flamin granulate was prepared by mixing with spherical shape filler mannitol PARTECK M 200. On the basis of studies designed composition tablet excipients «Lavaflam»: β-cyclodextrin (0.27 g), mannitol PARTECK M 200 (0.20 g), croscarmellose sodium (0.03 g), potato starch (0,022 g), PEG 6000 (0.002 g), magnesium stearate (0.006 g). Assay of the main components of lavender oil with the reference into linalol and linalyl acetate was performed by gas chromatography. Assay of total flavonoids of flamin was performed by spectrophotometric method with reference into isosalipurposide.
DISCUSSION AND CONCLUSION: New phytomedicine tablets «Lavaflam» meets European Pharmacopoeia requirements on the following parameters: appearance, geometrical sizes, average weight, disintegration, friability, resistance of tablets to crushing, quantification.

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GİRİŞ ve AMAÇ: Bu çalışmanın amacı, Chrysophthalmum gueneri Aytac & Anderb.’nin tuzlu su karidesi üzerine olası toksisite, fitotoksisite ve insektisidal aktivitesinin incelenmesidir.
YÖNTEM ve GEREÇLER: C. gueneri’nin tüm bitki kısımlarından hazırlanan metanollü (% 80) ekstresi artan polaritede n-hekzan, kloroform ve n-butanol ile ardarda fraksiyonlanmıştır. C. gueneri’nin metanollü (% 80) ekstresi ve tüm fraksiyonları tuzlu su karidesi letalite testi, Lemna minor’e karşı fitotoksisite ile Rhyzopertha dominica ve Tribolium castaneum’a karşı insektisidal aktiviteleri olmak üzere in vitro tarama testleri kullanılarak biyolojik aktiviteleri bakımından incelenmiştir.
BULGULAR: Çalışmamızın bulguları bitkinin n-hekzan ve kloroform fraksiyonlarının 1000 μg/mL’de % 100 büyüme inhibisyonu (Bİ) ile L. minor’e karşı önemli fitotoksik aktiviteye sahip olduğunu göstermiştir. Bunun yanısıra, bitkinin metanol (%80) ekstresi (%53 Bİ) ve n-butanol fraksiyonu (%46.6 Bİ) 1000 μg/mL’de orta derecede fitotoksik aktiviteye sahip bulunmuştur. Diğer taraftan, tüm örnekler tuzlu su karidesi üzerinde toksisiteye sahip bulunmamıştır. Ayrıca kalan sulu fraksiyonu % 20 mortalite ile Tribolium castaneum’a karşı düşük insektisidal aktivite göstermiştir.
TARTIŞMA ve SONUÇ: Sonuçlarımız C. gueneri’nin n-hekzan ve kloroform fraksiyonlarının potansiyel fitotoksik etkiye sahip olduğunu ortaya koymuştur.

INTRODUCTION: The aim of this work was to investigate the probable toxicity on brine shrimp, phytotoxicity and insecticidal activity of Chrysophthalmum gueneri Aytac & Anderb.
METHODS: The MeOH (80 %) extract obtained from the whole plant of C. gueneri was fractionated through subsequent solvent extractions in increasing polarity with n-hexane, chloroform and n-butanol. The MeOH (80 %) extract and all fractions of C. gueneri were evaluated for their biological acitivities using in vitro screening bioassays such as brine shrimp lethality test and phytotoxicity against Lemna minor as well as insecticidal activity against Rhyzopertha dominica and Tribolium castaneum.
RESULTS: The research findings showed that the n-hexane and chloroform fractions of the plant had significant phytotoxic activities with 100 % growth inhibition (GI) at 1000 μg/ml against L. minor. Moreover, the MeOH (80%) extract (53 % GI) and n-butanol fraction (46.6 % GI) of the plant have moderate phytotoxic activities at 1000 μg/ml. Otherwise, all samples had no toxicity on the brine shrimps. In addition, the remaining water fraction had low insecticidal activity with 20 % of mortality against Tribolium castaneum.
DISCUSSION AND CONCLUSION: Our results exerted that the n-hexane and chloroform fractions of C. gueneri had potential phytotoxic effects.

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Objective: Diclofenac exhibits limited solubility, low bioabsorption and gastric toxicity. The objective is to address above limitations and to design multiparticulate formulation for chronotherapy of Rheumatoid arthritis (RA).
Materials and methods: Solid dispersions of diclofenac (DC) with sodium starch glycolate (SSG) and guar gum (GG) were prepared. Uniform sized (~400 µm) non-pariel seeds were coated with solid dispersions to produce immediate release pellets (DMP-1 and DMP-2) and controlled release pellets (DMP-3 and DMP-4). The resultant controlled release pellets were further layered with methaacrylate polymers to obtain pulsatile release pellets (DMPP). Solubility, FTIR, DSC, micromeritics, SEM, drug content, drug release, pharmacokinetics and stability studies were performed for DMPP.
Results: Solubility of DC was improved by 164-folds due to presence of hydrophilic carries in the solid dispersions. No chemical and physical interactions were noticed in FTIR spectra and also in thermograms. Fluidized bed processor facilitated the production of high-quality, circular and regular pellets with angle of repose less than 19.5º and DC content in between 95.18-98.87%. Maximum drug was released from DMPP at the end of 12 hours. DMP-1 and DMP-2 pellets had 2 hrs of drug release and pulsatile controlled release pellets had 6 hrs lag phase followed by 12 hrs controlled release. Both DMP-1 and DMP-2 immediate had shown first-order release followed by Hixson-Crowell kinetics whereas DMPP pellets followed zero order release with Higuchi’s kinetics. Maximum concentration of DC in plasma was recognized as 400.8 ng/ml at 5 hr for DMP-2 and 381.1 ng/ml at 14 hr for DMPP-5. The solubility of DC was increased with the application of solid dispersion technique and in turn increased the pharmacokinetics. The pellets were plausibly stable above a time period. Thus, multiparticulate pulsatile systems of DC were as effective as chronotherapeutics in the treatment of circadian rhythm based ailments like RA.

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Meme kanseri kadınlarda en yüksek morbidite ve mortalite oranı oluşturan en yaygın kanser türlerinden biridir. Göğüs kanserinin mekanizmalarından biri, patogenezinde önemli rol oynayan oksidatif strestir. Oksitleyicilerin artmış üretimi ve / veya etkili olmayan atılımı, kansere yol açan doku hasarında çok önemli bir rol oynayabilir. Bu çalışmada tüm meme serumlarında malondialdehit (MDA) ve nitrik oksit (NO) düzeyleri ile birlikte kırmızı kan hücreleri süperoksit dismutaz (RBC-SOD) ve nitrik oksit sentaz (NOS) aktiviteleri anlamlı olarak yüksekti Kanserli hastalar kontrollere kıyasla. Bununla birlikte, meme kanseri hastalarında kontrollere kıyasla glutatyon (GSH) ve vitamin A, C, E düzeyleri ile bakır ve çinko glutatyon peroksidaz (GPx) ve katalaz (CAT) aktiviteleri azalmıştır. Serumda daha yüksek malondialdehit seviyesine sahip olan hastalar, serumda antioksidanların ve ağır metallerin eksikliğini göstermiştir. Zayıf bir diyet antioksidan durumu ve yüksek oksidan seviyeleri meme kanseri riski ile ilişkilidir, bu nedenle göğüs kanseri hastalarının, antioksidan ve oksidan seviyelerini dengelemek için besleyici takviyeleri almaları önerilir; daha iyi bir sonuç elde edilir.

Breast cancer is one of the most common types of cancer, which accounts for highest rate of morbidity and mortality in women. One of the mechanisms of breast cancer is the oxidative stress, which plays a crucial role in its pathogenesis. The increased production and/or ineffective scavenging of oxidants may play a crucial role in tissue damage leading to cancer. In this study, the levels of malondialdehyde (MDA) and nitric oxide (NO) as well as the activities of red blood cells-superoxide dismutase (RBC-SOD)(RBC-hemolysate) and nitric oxide synthase (NOS) were significantly higher in the sera of all breast cancer patients as compared to controls. However, the levels of glutathione (GSH) and vitamins A, C, E as well as the activities of copper and zinc glutathione peroxidase (GPx) and catalase (CAT) were decreased in patients of breast cancer when compared with controls. The patients who have shown higher level of malondialdehyde in the serum have shown deficiencies of antioxidants and heavy metals in the serum. A poor dietary antioxidant status and high oxidant levels are associated with the risk of breast cancer, thus suggesting that the breast cancer patients should take nutritive supplements to balance the antioxidant and oxidant levels for a the better outcome.

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Amaç: Pendimetalin ve trifluralin birçok ülkede, büyüme ve hücre bölünmesi üzerindeki inhibitör etkileri nedeniyle, geniş yapraklı yabani otları ve çimenli ot türlerini kontrol etmek amacıyla yaygın şekilde kullanmaktadır. Bu çalışmada, pendimetalin ve trifluralinin apoptotik ve anti-apoptotik potansiyelleri, A549 insan küçük olmayan akciğer kanseri hücreleri üzerinde çeşitli konsantrasyonlarda in vitro incelendi. Gereç ve Yöntem: Apoptoz ile ilişkili genler bcl-2, bax, casp3, casp9, tp53, birc ve ppia'nın ekspresyon seviyeleri, 24 saat 1, 10, 50, 100 ve 500 μM pendimetalin ve trifluralin uygulamasından sonra kantitatif gerçek zamanlı RT PCR ile incelendi. Bulgular: Çalışılan tüm konsantrasyonlarda pendimetalinin etkileri trifluralinin etkilerine kıyasla daha fazla baskıcılayıcı bulundu. 100μM pendimetalin ve trifluraline 24 saat boyunca maruz bırakılan hücrelerde gen ifadesi, apoptozu baskılayacak ve kanser hücrelerinin büyüme ve çoğalmasına yol açacak şekilde değişikliğe uğradı. Sonuç: Pendimethalin ve trifluralinin insanlar üzerindeki olası kanserojenik etkilerini azaltabilmek için, kullanımları sırasında izin verilen değerlerin ve gıdalar üzerindeki kalıntı limitlerinin aşılmamasına dikkat edilmelidir.

Objectives: Pendimethalin and trifluralin are commonly used in many countries to control broadleaf weeds and grassy weed species because of their inhibitor effects on growth and cell division. In this study, we examined the apoptotic and the anti-apoptotic potentials of pendimethalin and trifluralin on A549 human non-small lung cancer cells with several concentrations in vitro. Materials and Methods: The expression levels of apoptosis-related genes bcl-2, bax, casp3, casp9, tp53, birc and ppia were examined by quantitative RT PCR after 24h treatment of 1, 10, 50, 100 and 500 µM pendimethalin and trifluralin. Results: The effects of pendimethalin were found more repressive than trifluralin on all the studied concentrations. 24 hours of exposure with 100 µM pendimethalin and trifluralin altered the gene expressions in the way to suppress the apoptosis and lead cancer cells to grow and proliferate. Conlusion: Care should be taken not to exceed the permissible values and residue limits on the food during pendimethalin and trifluralin use in order to reduce the possible carcinogenic effects on humans.

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