SYNTHESIS OF ALLENIC NAPHTHALENE DERIVATIVES

Propargylic alcohol of naphthalene derivatives were synthesized and converted to the corresponding propargylic acetate using acetic anhydride. Reduction of the propargylic acetates by SmI2 afforded allenes and acetylenes. Base-promoted isomerisation of acetylene formed allene in high yield. KEY WORDS: Isomerisation, Allenic derivatives of naphthalene Bull. Chem. Soc. Ethiop. 2007, 21(2), 241-247

Fatty acid constituents and anticancer activity of Cladophora fracta (OF Müller ex Vahl) Kützing

Purpose: To determine the fatty acid constituents and anticancer effect of Cladohora fractaMethods: Cladophora fracta (O.F. Müller ex Vahl) Kützing was collected from natural ponds in Tokat, Turkey. Antiproliferative and cytotoxic effects of methanol and hexane extracts of C. fracta were investigated on human colon carcinoma (HT29) and non-tumorigenic African green monkey kidney (Vero) cell lines using BrdU cell proliferation enzyme-linked Immunosorbent assay (ELISA) and lactate dehydrogenase (LDH) test, respectively. The fatty acid composition of hexane extract was analyzed by gas chromatography-mass spectrometry (GC-MS).Results: Oleic acid, palmitic acid, gamma-linoleic acid and linoleic acid were the main constituents of C. fracta. The methanol extract exhibited strong antiproliferative activity on HT29 and Vero cell lines (p < 0.05). The hexane extract revealed its good antiproliferative activity at high concentrations on both cell lines. Cytotoxicity results showed that both methanol and hexane extract had low effect on HT29 cell at low concentrations.Conclusion: Due to the strong antiproliferative effect of C. fracta methanol extract on HT29 and Vero cell lines, it has potential anticancer properties and recommended for further development as such.Keywords: Cladophora fracta, Antiproliferative activity, Anti-cancer, Cytotoxic effect, Fatty aci

Galanthus woronowii (amaryllidaceae)'nin antioksidan aktivitesi ve toplam fenolik içeriği

Plants have been used for medicinal purpose since ancient times. Due to the including bioactive secondary metabolites, plants have gained the great interest for drug discovery and development process. In this work, Galanthus woronowii was extracted with hexane, dichloromethane and ethyl acetate sequentially. After removing of the solvent by rotary evaporator, crude extracts were yielded. Antioxidant activity including 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3- ethylbenzothiazoline-6-sulphonic acid) (ABTS) and reducing power assays were executed on corresponding extracts. In addition, total phenolic content was presented. Ethyl acetate extract included the most phenolic compounds and also it revealed the most antioxidant activity. Hence, this plant could be considered as a promising antioxidant agent.Bitkiler eski çağlardan beri tıbbi amaçlarla kullanılmaktadır. İçerdikleri biyoaktif sekonder metabolitlerden dolayı, bitkiler ilaç keşfi ve gelişimi için oldukça fazla ilgi görmektedir. Bu çalışmada, Galanthus woronowii türüne ait bitki materyalleri sırasıyla hekzan, diklorometan ve etil asetat ile ekstrakte edilmiştir. Çözücü dönerli buharlaştırıcı ile uzaklaştırıldıktan sonra ham ekstraktlar elde edilmiştir. Ekstraktların DPPH serbest radikal giderme, ABTS radikal katyon giderme ve indirgeme gücü aktiviteleri değerlendirilmiştir. Ayrıca toplan fenolik içerik belirlenmiştir. Etil asetat ekstraktının en çok fenolik içerdiği ve en yüksek antioksidan aktivite gösterdiği belirlenmiştir. Bu nedenlerle, bu bitki ümit verici antioksidan ajan olarak kabul edilebilir

Galanthus krasnovii (amaryllidaceae)'nin toplam fenolik içeriği ile antioksidan kapasitenin değerlendirilmesi

Natural products have gained the great interest due to their broad spectrum of biological activities. Galanthus krasnovii was dried at shade then extracted with hexane, dichloromethane, and ethyl acetate successively. After removing of solvent by reduced pressure, crude extracts of each solvent were yielded. Antioxidant activity including 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical cation and reducing power assays were carried out for each extract. Moreover, total phenolic content was determined. Total phenolic content of hexane-, dichloromethane-, and ethyl acetate extracts were found as 60.95 mg GAE/g extract, 71.90 GAE/g extract and 58.90 GAE/g extract respectively. Dichloromethane and ethyl acetate extract revealed the moderate antioxidant activity.Doğal ürünler geniş spektrumlu biyolojik aktivite göstermelerinden dolayı yoğun ilgi görmektedirler. Galanthus krasnovii gölgede kurutulduktan sonra sırasıyla hekzan, diklorometan ve etil asetat ile ekstrakte edildi. Düşük basınçta çözücü uzaklaştırıldıktan sonra her bir çözücünün ekstraktı elde edildi. Her bir ekstraktın, 1,1-difenil-2- pikralhidrazil(DPPH) radikal, 2,2'-azino-bis(3- etilbenzotiazolin-6- sülfirik asit) (ABTS) radikal katyon ve indirgeme gücü antioksidan çalışmaları gerçekleştirildi. Ayrıca, ekstraktların toplam fenolik içerikleri belirlendi. Hekzan-, diklorometan- ve etil asetat ekstraktlarının toplam fenolik içerikleri sırasıyla 60.95 mg GAE/g ekstrakt, 71.90 GAE/g ekstrakt ve 58.90 GAE/g ekstrakt olarak belirlendi. Diklorometan ve etil asetat ekstraktları orta derece aktivite gösterdi

2,4-Dibromo-2,3-dihydro-1H-inden-1-yl acetate

In the title compound, C11H10Br2O2, the cyclo­pentene ring fused to the benzene ring adopts an envelope conformation, with the C atom attached to the Br atom as the flap. The crystal structure does not exhibit any classical hydrogen bonds. The mol­ecular packing is stabilized by van der Waals forces and π–π stacking inter­actions with a centroid–centroid distance of 3.811 (4) Å

5-Amino-4-bromo-2,3-dihydro-1H-inden-1-one

In the title compound, C9H8BrNO, the non-H-atom framework is essentially planar, with a maximum deviation of 0.087 (3) Å. In the crystal, mol­ecules are inter­connected into a three-dimensional network by C—H⋯O and N—H⋯O hydrogen bonds. In addition, C—H⋯π inter­actions and a π–π stacking inter­action, with a centroid–centroid distance of 3.5535 (19) Å, are also observed

Crystal structure and computational study of 3,4-dihydroxy-3-hydroxymethyl-9-methyl-6-methylidene-3a,4,5,6,6a,9,9a,9b-octahydroazuleno[4,5-b]furan-2,8(3H,7H)-dione

In the molecule of title compound, C15H20O6, also known as cynarinin A, the cyclopentane ring having twist conformation and a gamma-lactone ring assuming an envelope conformation are trans-and cis-fused, respectively, to a cycloheptane ring adopting a twist-chair conformation. In the crystal, O-H center dot center dot center dot O hydrogen bonds link neighbouring molecules, forming a three-dimensional network. Theoretical calculations of the molecular structure using the CNDO approximation and MOPAC PM3 geometry optimization are in satisfactory agreement with the results of the X-ray structure analysis

Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3beta of substituted quinolines.

A new series of fifteen 5-, 6-, and 8-appended 4-methylquinolines were synthesized and evaluated for their neural protective activities. Selected compounds were further examined for their inhibition of glycogen synthase kinase-3β (GSK-3β) and protein kinase C (PKC). Two most potent analogs, compounds 3 and 10, show nanomolar protective activities in amyloid β-induced MC65 cells and enzymatic inhibitory activities against GSK-3β, but poor PKC inhibitory activities. Using normal mouse model, the distribution of the most potent analog 3 in various tissues and possible toxic effects in the locomotors and inhibition of liver transaminases activities were carried out. No apparent decline of locomotor activity and no inhibition of liver transaminases were found. The compound appears to be safe for long-term use in Alzheimer’s disease mouse model

Bromination of 4-Bromoindanone and 5-Bromoindanone, Facile Synthetic Access to 3,5,10-tribromo-7H-benzo[c] fluoren-7-one

Bromination reactions of 4-bromoindanone and 5-bromoindanone were presented and optimum reaction conditions were introduced. 2,2,4-Tribromoindanone was synthesized by treatment of 4-bromoindanone with molecular bromine at room temperature in a high yield. Bromination of 4-bromoindanone with NBS, SiO2 and LiClO4 in PEG yielded the corresponding 2,4-dibromoindanone which was reduced to 1-hydroxy-2,4-dibromoindane. Acetylation of hydroxydibromoindane in pyridine gave the 1-acetoxy-2,4-dibromoindane in excellent yield. The radical bromination of 5-bromoindanone with NBS at 77 degrees C in CCl4 yielded the corresponding 3,5-dibromoindene-1-one which was converted to 3,5,10-tribromo-7H-benzo[c] fluoren-7-one by thermolysis

Effect of Salt and pH Stress of Bioactive Metabolite Production in Geitlerinema carotinosum

Cyanobacterial metabolites are natural products that have an important feature in pharmaceutical and medicinal industries. In this study, the presence of the secondary metabolite norharmane in the indole structure was determined in Geitlerinema carotinosum (Geitler) Anagnostidis isolated from Tokat Yesilirmak River and its production in salt stress and pH stress was investigated. In salt stress experiments, cyanobacterium was cultured for two weeks by adding NaCl to BG11 medium in erlenmayers of 0.5, 1.0, 3.0, 5.0 M. pH stress was executed at 5 and 9. Norharmane amount was determined by HPLC using C18 reverse phase column at a temperature of 40 °C and a flow rate of 1 ml / min. The amount of norharman metabolite (μg/g) was calculated according to the Gauss method by drawing a calibration curve over the absorbance value of the standard 247 nm wavelength. According to the analysis results, metabolite production was 0.612, 1.299, 0.011 at 0.5 M, 1.0 M, 3.0 M respectively. At 5 M, there was no norharmane production. The norharmane production is higher at pH 5 (1.293 μg /g) than that of the pH 9 (0.448 μg /g)