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Background In sustainable agriculture, the use of farmyard manure (FYM) is of great interest to environmental security and is effective as a good nitrogen source for sustainable crop production. Therefore, determining the effective doses of FYM that will be an alternative to chemical fertilizers, is also important to improve soil fertility and produce healthy products. This study aimed to determine the effects of FYM and ammonium nitrate (AN) fertilizers on the biological value and essential oil content of dill (Anethum graveolens L.). Methods Different doses FYM (7.5, 10, 12.5 and 15 t ha−1) and AN (30, 60, 90 and 120 kg ha−1) were applied by sowing and compared to a control group (no manure). We evaluated the chemical constituents as well as the biological activities of dill herbs and seeds growing at various doses of FYM and AN fertilizers. Results The most abundant components of essential oils were found to be dill apiole (11.96 ± 0.83 and 18.65 ± 1.89%) and carvotanacetone (15.90 ± 2.34 and 21.76 ± 1.62%) in the leaves and seeds, respectively. Limonene (9.01 ± 1.11%), 4-isopropyltoluen (8.24 ± 0.89%), dill ether (9.13 ± 1.12%) and mycrene (7.44 ± 0.68%) were major essential oils components in herbs. The highest concentration of the essential oil components was determined as 12.5–15 t ha−1 in FYM and 90 AN applications. From the effective concentration (EC50) of the samples, it was seen that 60 kg ha−1 AN infusion, 120 kg ha−1 AN decoction as well as 7.5 t ha−1 FYM and 10 t ha−1 FYM essential oils had the highest DPPH, ABTS+ and superoxide anion radical scavenging activity as shown by the lowest value of EC50 compared to the control. Although the antioxidant activities of the samples were significantly lower than those of the reference antioxidant gallic acid, it was evident that they did show the antioxidative potential for hydrogen and a single electron donor activities, thus could serve as free radical scavengers, and act as reductant. In particular, the highest total phenolic content (18.36 ± 0.35 mg g−1) was found in the infusion extract after applying the 60 kg ha−1 AN fertilizer. Essential oils extracted from the seeds also exhibited strong antibacterial activity against Staphylococcus epidermidis, Enterococcus faecalis, and Pseudomonas aeruginosa. The highest antibacterial activity against all tested microbial species was observed with the 10 t ha−1 FYM application. Conclusion The findings of the study suggest that the application of FYM has promising effects on dill leaf, seed, and herb and can be considered as a suitable substitute for chemical fertilizers when growing dill, a plant with increasing importance and demand. more...

Background: 2-Indolinone-based hydrazinecarbothioamides carrying a 3-phenylsulfonamide moiety (7–9) were designed by replacement of donepezil's pharmacophore group indanone with a 2-indolinone ring. Method: Compounds 7–9 were synthesized by reaction of N-(3-sulfamoylphenyl)hydrazinecarbothioamide (6) with 1 H-indolin-2,3-diones (1–3). Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory effects of compounds 7–9 were assayed. Molecular modeling studies of 5-chloro-1,7-dimethyl-substituted compound 8e were carried out to determine the possible binding interactions at the active site of AChE. Results: Compound 8e showed the strongest inhibition against AChE ( Ki = 0.52 ± 0.11 μM) as well as the highest selectivity (SI = 37.69). The selectivity for AChE over BuChE of compound 8e was approximately 17-times higher than donepezil and 26-times higher than galantamine. Conclusion: Further development of compounds 7–9 may present new promising agents for Alzheimer's treatment. more...

Scorzonera L. (Asteraceae) species are widespread and utilised as traditional medicine and edible plant. A phytochemical study on ethyl acetate fraction obtained from the ethanol extract of Scorzonera hieraciifolia Hayek (an endemic species of Turkey) roots resulted in isolation of nine compounds; 5-O-feruloyl quinic acid methyl ester (1), 1,5-di-O-feruloylquinic acid (2), chlorogenic acid methyl ester (3), 3-O-caffeoylquinic acid methyl ester (4), 1,3-di-O-caffeoylquinic acid methyl ester (5), 3,5-di-O-caffeoylquinic acid methyl ester (6), 4,5-di-O-caffeoylquinic acid methyl ester (7), caffeic acid (8), 3-(4’-Hydroxyphenyl)-2-propenoic acid (4″-carboxyl)-phenyl ester (9). Structures of the compounds were determined using spectral methods. All substances were isolated for the first time from this species and compound 9 is new for the family Asteraceae. In vitro antioxidant, anti-inflammatory and antimicrobial activities of petroleum ether, chloroform, ethyl acetate and n-butanol fractions were evaluated. Ethyl acetate fraction showed the highest amount of total phenolic content and antioxidant capacity. No significant antimicrobial activity was determined against tested bacteria and fungi. COX inhibition test was employed for anti-inflammatory studies, all fractions showed low inhibitory effect on both COX-1 and COX-2 enzymes in comparison with indomethacin. more...

Phytochemical composition of ethyl acetate fraction and total phenolic content, in vitro antioxidant, anti-inflammatory, antimicrobial activities of petroleum ether, chloroform, ethyl acetate and n-butanol fractions of the ethanol extract obtained from the subaerial parts of Scorzonera pygmaea Sibth. & Sm. (Asteraceae) were investigated. Nine compounds; scorzopygmaecoside (1), scorzonerol (2), cudrabibenzyl A (3), thunberginol C (4), scorzocreticoside I (5) and II (6), chlorogenic acid (7), chlorogenic acid methyl ester (8), 3,5-di-O-caffeoylquinic acid (9) were isolated and identified using spectroscopic methods. All substances were isolated for the first time from this species. Compounds 1 and 2 are new. The fractions showed high antioxidant capacity correlated with their phenolic content and no significant antimicrobial activity against tested bacteria and fungi. COX inhibition test was used to evaluate the anti-inflammatory activity and all the fractions showed low inhibition in comparison with indomethacin. more...

A series of novel indole-based hydrazide-hydrazone derivatives were synthesized and evaluated for their AChE and BuChE inhibitory activities. The structural elucidations of the novel compounds (2a–k) were performed by IR, 1H-NMR, 13C-NMR, mass, and elemental analysis. The inhibitory potential of the novel compounds on AChE (from electric eel) and BuChE (from equine serum) enzymes were carried out using in vitro modified Ellman's spectrophotometric method. Compounds 2f and 2d displayed the highest AChE inhibitory activity. Furthermore, 2d displayed the best BuChE inhibitory activity which was comparable with Galantamine. In addition to the in vitro analysis, docking studies targeting AChE (PDB ID: 1EVE ) and BuChE (PDB ID: 4BDS ) were performed to understand the possible interactions of these compounds with the enzymes. Structure-activity relationships, as well as in silico ADME studies, were performed and a relationship between biological, electronic, and physicochemical qualifications of the title compounds was determined. more...

This study was conducted to evaluate the chemical composition, antioxidant and anti-acetylcholinesterase (anti-AChE) activities of methanolic extracts of H. neurocalycinum and H. malatyanum, two endemic species of the Turkish flora. HPLC-DAD analysis indicated that two naphthodianthrones (pseudohypericin and hypericin) together with chlorogenic acid, rutin, hyperoside, isoquercitrin, kaempferol, quercitrin, quercetin, amentoflavone and hyperforin are the main compounds present in the methanol extracts. The extracts were tested in vitro for their antioxidant activities including, inhibition of lipid peroxidation in liposomes, induced by Fe3 +/ascorbate system, scavenging effect on DPPH and superoxide anion radicals, and ferric ion reducing antioxidant power (FRAP). H. neurocalycinum demonstrated stronger antioxidant properties than H. malatyanum due to higher activity on scavenging DPPH (EC50 = 2.49 ± 0.09 mg/mL) and superoxide anion radicals (EC50 = 0.613 ± 0.05 mg mg/mL), and inhibition of lipid peroxidation (EC50 = 2.49 ± 0.09 mg/mL). This difference in activity seems to be due to the presence of higher amounts of the antioxidant compounds (flavonoids) such as rutin, quercetin and kaempferol in H. neurocalycinum extract. The antioxidant activities of the extract may be attributed to their reducing capabilities. At 5 mg/mL H. neurocalycinum (FRAP value = 2.39 ± 0.039 mM Fe2 +) and H. malatyanum (FRAP value = 2.23 ± 0.013 mM Fe2 +) showed high ability to reduce Fe3 + to Fe2 +. The extracts were tested also for their in vitro AChE inhibitory activities. H. neurocalycinum inhibited 72.24 ± 0.39% of AChE activity at a concentration of 5 mg/mL. It was concluded that H. neurocalycinum is more effective AChE inhibitor and antioxidant than H. malatyanum. more...

The genus Taraxacum Wigg. is a member of the family Asteraceae. This genus is represented by about 49 species in Turkey. Taraxacum species are commonly used as a diuretic and for the treatment of various diseases such as dyspepsia, reflux, spleen and liver disorders, and anorexia. Compounds from the group of sesquiterpene lactones, triterpenes, phytosterols, flavonoids, lignans, coumarins, phenolic acids, beta-carboline alkaloids, indole alkaloids, and carotenoids have been reported from Taraxacum species. In this study, ethyl acetate and chloroform fractions of methanol extract obtained from root and aerial parts of Taraxacum farinosum Hausskn. & Bornm., an endemic species to Turkey, were investigated in terms of total phenol compound amounts and antioxidant potentials. The highest total phenolic compounds and antioxidant activity were determined in ethyl acetate fractions.. more...

WOS:000605357000022 Abstract Background and Aims: Scorzonera L. genus contains several medicinal and edible plants. Both roots and aerial parts of Scorzonera species are used. S. pygmaea is endemic to Turkey. in a previous study, nine phenolic compounds were reported from the roots of the plant alongside certain biological activities. The current study was designed to investigate the aerial parts of the plant in the same manner and compare the potentials of the two parts. Methods: Chromatographic and spectroscopic methods were used to isolate and identify the phenolics. Total phenolic contents were determined by Folin-Ciocalteu method. FRAP assay, anti-LPO, scavenging DPPH, ABTS and superoxide radicals were employed to evaluate the antioxidant activity. COX inhibition test and micro broth dilution technique were used for anti-inflammatory and antimicrobial activities, respectively. Results: Seven phenolic compounds; thunberginol C (1), protocatechuic acid (2), chlorogenic acid methyl ester (3), cudrabibenzyl A (4), scorzocreticin (5), scorzocreticoside I (6) and II (7) were purified. All the compounds are new for the aerial parts of the plant and 2 is new for the genus. The aerial parts showed a high antioxidant capacity which correlated with its phenolic content. COX inhibitory activity was found to be lower compared to Indomethacin. Weak antimicrobial activity was determined against Staphylococcus aureus and S. epidermidis. Conclusion: Aerial parts possess significant/infrequent phenolics and the ethyl acetate (EtOAc) fraction of the ethanol extract is the most promising fraction for isolating these compounds. Phenolic compositions of aerial parts and roots are very similar. However, aerial parts can be a better rich source of natural antioxidants with protocatechuic acid and higher antioxidant potential. more...

In the present work we carried out a phytochemical and biological investigation on three endemic Hypericum species, i.e. Hypericum thymbrifolium (H. thymbrifolium), Hypericum spectabile (H. spectabile) and Hypericum pseudolaeve (H. pseudolaeve) from Anatolia in order to discover new sources of natural compounds for the treatment of inflammatory and neurodegenerative disorders. HPLC-DAD analysis indicated that two naphthodianthrones (pseudohypericin and hypericin) together with chlorogenic acid, rutin, hyperoside, isoquercitrin, kaempferol, quercitrin, quercetin, amentoflavone, and hyperforin are the main compounds present in the methanol extracts. After chemical characterization, all extracts were in-vitro biologically assayed for antioxidant potential by lipid peroxidation inhibitory activity, DPPH, FRAP assays, and superoxide radical scavenging activity, for AChE inhibitory activity by Ellman’s method, for COX inhibitory activity by using enzyme immunoassay (EIA) kit, for cytotoxic activity on HeLa and NRK-52E cell lines by MTT assay. The superoxide radical scavenging activity and lipid peroxidation inhibitory activity of H. spectabile (EC50 = 0.430 mg/mL) were more remarkable than that of H. thymbrifolium and H. pseudolaeve. The extracts showed moderate inhibitory activity on AChE (from 49.37% to 63.41%). The best inhibitory activity against COX-1 (71.77% and 77.04%, respectively) and COX-2 ( 64.14% and 72.23%, respectively) were shown by H. thymbrifolium and H. spectabile, which may be due to their richest chlorogenic acid content (0.29576% and 0.23567%, respectively). Cytotoxicity screening results showed that the extracts did not demonstrate significant cytotoxic activity. It was concluded that the most promising extract with antioxidant, anti-inflammatory, and AChE inhibition potential is H. spectabile. more...

The aerial parts of Teucrium sandrasicum L. (Lamiaceae), an endemic species of the Turkish flora, are widely used in the daily diet. The plant is also valued as a traditional medicine and is used for diuretic, diaphoretic, tonic, antipyretic, antidiabetic, antispasmodic, and cholagogic purposes. This study investigated a methanolic extract of aerial parts of T. sandrasicum for its antioxidant and anti-inflammatory effects, inhibition of thioredoxin reductase, and protection against DNA damage. The extract showed inhibitory activity against FeCl3/ascorbic acid induced phosphatidylcholine liposome oxidation (EC50 = 1.49 ± 0.03 mg/mL), quenched stable DPPH (EC50= 1.05 ± 0.03 mg/mL), superoxide anion (EC50 = 1.20 ± 0.06 mg/mL), and ABTS cation radicals (EC50 = 1.73 ± 0.01 mg/mL). The extract also acted as a reductant, as determined by the FRAP value (2.66 ± 0.21 mM/L Fe2+), indicating its potential as an antioxidant. The T. sandrasicum species was determined to be a rich source of flavonoids (104.39 ± 1.37 mg/g), which are likely to serve as antioxidant, anti-inflammatory, and cancer chemoprevention agents. The extract was strongly inhibitory against both cyclooxygenase-2 (COX-2) (EC50 = 1.18 ± 0.03 mg/mL) and thioredoxin reductase (0.90 ± 0.02 mg/mL), and it significantly and dose-dependently decreased the amount of nicked DNA, as well as increased the natural form of DNA. more...

The antioxidant, anti-inflammatory, acetylcholinesterase (AChE) inhibitory and antimicrobial activities of extract from the Centaurea antiochia Boiss. var. praealta (Boiss. & Bal.) Wagenitz, an endemic plant species from Turkey, were investigated. The results indicated that the extract inhibits FeCl3/ascorbic acid-induced phosphatidylcholine liposome oxidation, scavenges stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radicals, and reduces Fe3+ to Fe2+ in the ferric-reducing antioxidant power (FRAP) assay. The extract inhibited AChE and both cyclooxygenase (COX)-1 and COX-2, which suggests this species might be a potential source of plant-derived anti-inflammatory and anti-AChE substances. The extract may also act as an antimicrobial agent because it inhibited the growth of Gram-positive and Gram-negative bacteria as well as yeast. These findings may scientifically explain some uses of this species in Turkish folk medicine as an antimicrobial, anti-inflammatory and wound healing agent. Practical Applications The Centaurea species are known by the vernacular name “peygamber cicegi” in Turkish folk medicine. Ethnobotanical reports indicate the Centaurea species have antidiabetic, anti-inflammatory, wound healing, digestive, stomachic, diuretic, astringent, hypotensive, antipyretic, laxative, analgesic, tonic, hemostatic and antibacterial properties. Considering the important role oxidative stress and inflammation play in the pathogenesis of neurological diseases, C. antiochia var. praealta may be used as a medicinal plant to treat Alzheimer's disease. This study also confirms the efficacy of this plant as a natural antimicrobial agent. more...

DOI : 10.5152/IstanbulJPharm.2018.382627 Thioredoxin reductase (TrxR, EC 1.6.4.5) is a ubiquitous flavoenzyme that is present from Archaea to humans, and it is the only enzyme capable of catalyzing the reduction of thioredoxin (Trx) by nicotinamide adenine dinucleotide phosphate (NADPH). Although TrxR has been purified and characterized from different bacteria, plants, and mammalian organisms, a survey of the literature revealed no studies on the purification and characterization of TrxR from the mussel Mytilus galloprovincialis Lam. In this study, TrxR was purified to homogeneity from the hepatopancreatic tissue of M. galloprovincialis Lam. by extraction, ammonium sulfate precipitation, and DEAE-Sepharose CL-6B anion and 2’,5‘-ADP-agarose chromatographies, and some of its kinetic properties were examined. Molar mass determined by sodium dodecyl sulfate polyacrylamide gel electrophoresis revealed only a single protein band corresponding to a molecular weight of 35 kDa. Optimum pH and temperature were found to be 7.0 and 60°C, respectively. Km and Vmax values for NADPH were found to be 85 µmol and 4.82 µmol/min/mg, respectively. For 5,5ʹ-dithiobis (2-nitrobenzoic) acid (DTNB), the Km and Vmax values were 193 µmol and 1.32 µmol/min/mg, respectively. Increasing the knowledge on the kinetic properties of TrxR will significantly increase the prospects of enzyme application as an oxidative stress biomarker in mussels and fishes for monitoring contamination in coastal environments. more...

Ferulago W. Koch is a genus in the Apiaceae family comprising 34 species, of which 18 are endemic in Turkey. Ferulago species have been known since the time of Dioscorides and have been used in folk medicine for their sedative, tonic, digestive, carminative, and aphrodisiac effects, as well as for the treatment of intestinal worms and hemorrhoids. This study was conducted to evaluate the polyphenolic contents and antioxidant activities of methanol extracts of the aerial parts (HFT) and rhizomes (RFT) of Ferulago trojana E. Akalin & Pimenov by measuring their ability to inhibit lipid peroxidation induced by Fe3+-ascorbate, their DPPH· and ABTS·+ scavenging activities, and their ferric reducing antioxidant power (FRAP value). The methanol extracts were also examined for their antimicrobial activity using the microbroth dilution technique. Results showed that the methanol extracts of the aerial parts of the plant, containing the highest amount of total phenolic content and flavonoids, exhibited antioxidative potential for the chain-breaking inhibition of lipid peroxidation and showed the strongest hydrogen and single electron donor activities, which could thus serve as a free radical scavenger, act as a reductant, and provide protection against oxidative stress. Although the methanol extract of rhizomes did not exhibit any inhibitory effect on lipid peroxidation, it is possible that it might also have protective effects against oxidative damage by scavenging free radicals and acting as a reductant. While both the methanol extracts of the aerial parts and rhizomes of F. trojana were effective against Staphylococcus aureus, Methicillin-resistant S. aureus (MRSA), and S. epidermidis, the extracts showed no activity against Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. In addition, the methanol extract of rhizomes of F. trojana exhibited antibacterial activity against Proteus mirabilis and antifungal activity against the yeast Candida albicans. more...

The chemical composition of methanolic extract of Hypericum pamphylicum (HPM) was analyzed by using high performance liquid chromatography–diode array detector (HPLC-DAD). The plant contained hypericin (0.00002 ± 0.000001%), hyperforin (trace), chlorogenic acid (5.58 ± 1.59%), hyperoside (0.46 ± 0.05%), isoquercitrin (0.134 ± 0.02%) and quercetin (0.087 ± 0.008%). The antioxidant activity of HPM was evaluated by using several antioxidant tests. HPM exhibits inhibitory capacity against phosphatidylcholine liposome peroxidation, induced with iron and ascorbic acid, scavenge DPPH and superoxide radicals and act as reductants. The cytotoxic activity of HPM was also determined by using MTT cell viability assay on HeLa and NRK-52E cell lines. HPM demonstrated no cytotoxicity against HeLa and NRK-52E cell lines with IC50 values of 1.89 mg/ml and 1.05 mg/ml, respectively. The different crude extracts of H. pamphylicum were analyzed using a microdilution assay for antimicrobial activity against several microorganisms. The most active extract was HPM which showed activity against Staphylococcus aureus. It is observed that nearly all extracts showed activity against Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella thypi, Shigella flexneri, Proteus mirabilis and Candida albicans. more...

3H-Spiro[1,3-benzothiazole-2,3'-indol]-2'(1'H)-ones 3a-c and 4a-e were synthesized from treating the 5-substituted 1H-indole-2,3-diones with 2-aminothiophenol in ethanol. The structures were confirmed by elemental analyses, spectrometry (IR, (1)H NMR, (13)C NMR, HSQC-2D and LCMS-APCI) and single crystal X-ray analysis. The new compounds were screened for their antioxidant activities such as the Fe(3+)/ascorbate system induced inhibition of lipid peroxidation (LP) in liposomes, trolox equivalent antioxidant capacity (TEAC), scavenging effect on diphenylpicryl hydrazine (DPPH*), and reducing power. These compounds showed potent scavenging activities against DPPH* and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS*(+)) radicals, reducing powers, and strong inhibitory capacity on lipid peroxidation. Compound 4a incorporating methyl both at R(1) and R(2) was found to be the most potent antioxidant described in this study. Compounds 3b and 4b were selected as representative compounds by the National Cancer Institute for screening against anticancer activity and these compounds were found to be cytotoxic against CNS cancer cell line SNB-75 in the primary screen. more...

Water, methanol and ethyl acetate extracts from stems with leaves and flowers of Amaranthus lividus L., one of the most popular leafy vegetable consumed in the west Black Sea region of Turkey, were tested in vitro for their ability to inhibit peroxidation of phosphatidylcholine liposomes induced with Fe 3+ /ascorbate, to scavenge ABTS + , DPPH and hydroxyl radicals, to reduce Fe (III) to Fe (II) and to chelate Fe (II) ions. The results showed that amaranth vegetable contained naturally occuring antioxidant components and possessed antioxidant activity which may be attributed to its lipid peroxidation inhibitory, radical scavenging and metal chelating activities. The antioxidant activities of the water and ethyl acetate extracts were not concomitant with the development of their reducing power. It was concluded that A. lividus might be a potential source of antioxidants. more...

Smilax excelsa L. leaves are used widely in the Black Sea region of Turkey for consumption in the daily diet and in folk medicine for their medicinal properties. In the present study, different antioxidant tests were employed in order to evaluate the antioxidant activities of water, infusion, ethanol and ethyl acetate extracts of S. excelsa leaves. In addition, the results were compared with natural and synthetic antioxidants. The levels of total phenolics, total flavonoids and anthocyanins of the extracts were also determined. The extracts were found to have different levels of antioxidant properties in the test models used. All extracts had good total phenolic and flavonoid contents, inhibited lipid peroxidation, showed radical scavenging and iron-chelating activities. Therefore, the leaves of the plant could be considered as a significant natural antioxidant source. more...

Background: Because reactive oxygen species (ros) contribute to the pathogenesis of various acute and chronic liver diseases, dietary antioxidants and drugs from herbal origins have been proved to be beneficial as therapeutic agents in reversing hepatotoxicity and oxidative stress. The objective of this study was to investigate the protective effect of an aqueous extract from smilax excelsa l. Shoots and leaves against acute ccl4-induced liver injury as well as the changes in antioxidative defense system in female wistar albino rats.Materials and Methods: S. Excelsa extract was administered orally in doses of 100, 200 and 400 mg/kg body weight, once daily for 9 days. Acute hepatic toxicity was induced by intraperitoneal injection of ccl4 (1 ml/kg) on the 10th day. 24 h after ccl4 intoxication, biochemical and histopathological analyses were undertaken on sera and liver tissues.Results: Ccl4 challenge caused significant increases in the activities of liver enzymes as well as the levels of bilirubin, malondialdehyde and nitric oxide, while total serum protein levels and antioxidant defense system parameters were reduced significantly compared to the normal group. Administration of s. Excelsa extract at a dose of 400 mg/kg resulted in a suppression of ccl4-induced lipid peroxidation and altered oxidative stress parameters to nearly normal values in comparison to ccl4-treated rats. Nevertheless the extract did not reduce the extent of ccl4-induced mild liver injury, as seen by the histopathology of liver damage.Conclusion: The results of this study suggest that s. Excelsa could protect the liver tissues against ccl4-induced oxidative stress probably by increasing antioxidative defense activities.Keywords: Antioxidant enzymes, carbon tetrachloride, liver injury, smilax excelsa, hepatoprotective activity more...

The aim of this work was to investigate the effects of Aloe vera leaf pulp and gel extracts on the liver tissue of neonatal streptozotocin (n0STZ)-induced type-II diabetic rats. The diabetic rats were separated into four groups and each group was given the following samples by gavage, daily for 15 d: phosphate buffered saline (PBS; diabetic control), Aloe leaf pulp extract, Aloe leaf gel extract, glibenclamide. Liver tissues were examined histologically. The markers of oxidative stress: glutathione (GSH), non-enzymatic glycosylation (NEG) and lipid peroxidation (LPO), were determined in liver tissue. Biochemical parameters for liver function: serum alkaline phosphatase (ALP), and alanine transaminase (ALP) activities, were evaluated. All parameters were also determined in healthy (non diabetic) rats for comparison. In the diabetic control group, the degenerative changes in liver tissue were remarkable, while in the diabetic groups given Aloe pulp and gel extracts and glibenclamide, the damage to the liver tissue was decreased. The increase of GSH and the decrease of NEG and LPO in liver tissues with the treatment of Aloe gel extract, is consistent with the beneficial effect of Aloe. Serum ALP and ALT activities were also decreased in the groups given Aloe gel extract. It was concluded that Aloe gel extract has a protective effect comparable to glibenclamide against hepatotoxicity produced by diabetes if used in the treatment of type-II diabetes. more...

In this study, 5-chloro-3H-spiro-[1,3-benzothiazole-2,3'-indole]-2'(1'H)-one derivatives 3a-l were synthesized by the reaction of 1H-indole-2,3-diones 1a-l with 2-amino-4-chlorothiophenol 2 in ethanol. 3a-l were tested for their abilities to inhibit lipid peroxidation (LP), scavenge DPPH(•) and ABTS(•+) radicals, and to reduce Fe(3+) to Fe(2+). Most of the tested compounds exhibited potent scavenging activities against ABTS(•+) radical, reducing powers and strong inhibitory capacity on LP. 3 a, 3 d, 3 e, 3h, 3 j and 3 k chosen as prototypes were evaluated in the National Cancer Institute's in vitro primary anticancer assay. The greatest growth inhibitions were observed against a non-small cell lung cancer cell line HOP-92 for R1-fluoro substituted 3 d and a renal cancer cell line RXF-393 for R-chloro substituted 3 e in the primary screen. more...

WOS: 000300921100086, This study was conducted to evaluate the essential oil composition and antioxidant activity of methanolic extracts from fruits and flowers of Hypericum lydium Boiss., a wild growing species of the Turkish flora. The antioxidant activities were determined through several biochemical assays. Both extracts showed an inhibitory effect against the formation of TBARS in a phosphatidylcholine liposome model system, moderate scavenging effect on DPPH center dot and superoxide radicals, prominent reducing power and inhibitory effect on deoxyribose degradation in both the nonsite and site-specific assay, but a greater hydroxyl radical scavenging activity was observed in the non-site specific assay, suggesting that the extracts were better at scavenging hydroxyl radicals than at chelating iron. Correlation analysis indicated that there was a linear relationship between antioxidant potency, free-radical scavenging activity, reducing power and the content of flavonoids of fruits and flowers extracts. The essential oils obtained by hydrodistillation were analyzed by GC and GC-MS. In total forty-three compounds were identified. The most abundant components were monoterpenes hydrocarbons represented principally by alpha-pinene. The tested oil showed no antioxidant activity, Scientific Research Foundation of Istanbul University [7069], This work is supported by the Scientific Research Foundation of Istanbul University (Project no: 7069). more...

In recent years, the role of free radical damage consequent to oxidative stress is widely discussed in diabetic complications. In this aspect, the protection of cell integrity by trace elements is a topic to be investigated. Vanadium is a trace element believed to be important for normal cell function and development. The aim of the present study was to investigate the effect of vanadyl sulfate supplementation on the antioxidant system in the muscle tissue of diabetic rats. Diabetes was induced by intraperitoneal injection of streptozotocin (STZ, 65 mg/kg body weight) to male Swiss albino rats. The rats were randomly divided into 4 groups: Group I, control; Group II, vanadyl sulfate control; Group III, STZ-diabetic untreated; Group IV, STZ-diabetic treated with vanadyl sulfate. Vanadyl sulfate (100 mg/kg) was given daily by gavage for 60 days. At the last day of the experiment, rats were killed, muscle tissues were taken, homogenized in cold saline to make a 10% (w/v) homogenate. Body weights and blood glucose levels were estimated at 0, 30 and 60th days. Antioxidant enzymes, superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR), glutathione peroxidase (GPx), glutathione-S-transferase (GST), as well as carbonic anhydrase (CA), myeloperoxidase (MPO) activities and protein carbonyl content (PCC) were determined in muscle tissue. Vanadyl sulfate administration improved the loss in body weight due to STZ-induced diabetes and decreased the rise in blood glucose levels. It was shown that vanadium supplementation to diabetic rats significantly decrease serum antioxidant enzyme levels, which were significantly raised by diabetes in muscle tissue showing that this trace element could be used as preventive for diabetic complications. more...

In this work we report the isolation and characterisation of seven flavonoids, the levels of total phenolics, flavonoids and proanthocyanidins, and the antioxidant activity of the leaf extract of Rosa agrestis Savi (Rosaceae). The results showed that the R. agrestis leaf extract exhibited significant antioxidative activity as measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) (EC(50) = 47.4 microg mL(-1)), inhibited both beta-carotene bleaching and deoxyribose degradation, quenched a chemically generated superoxide anion in vitro and showed high ferrous ion chelating activity. Reactivity towards 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) radical cation and ferric-reducing antioxidant power (FRAP) values were equivalent to 2.30 mM L(-1) Trolox, the water soluble alpha-tocopherol analogue, and 1.91 mM L(-1) Fe(2+), respectively. The high antioxidant activity of the extract appeared to be attributed to its high content of total phenolics, flavonoids and proanthocyanidins. The flavonoids isolated from R. agrestis leaves were diosmetin, kaempherol, quercetin, kaempherol 3-glucoside (astragalin), quercetin 3-rhamnoside (quercitrin), quercetin 3-xyloside and quercetin 3-galactoside (hyperoside). Diosmetin (5,7,3'-trihydroxy-4'-methoxyflavone) was isolated for the first time from Rosa species. more...

In order to demonstrate whether the known biological effects ofAloe vera(L.) Burm. fil. could correlate with the antioxidant activity of the plant, the antioxidant activity of the aqueous leaf extract was investigated. The present study demonstrated that the aqueous extract fromA. veraleaves contained naturally occuring antioxidant components, including total phenols, flavonoids, ascorbic acid, β-carotene and α-tocopherol. The extract exhibited inhibitory capacity against Fe3+/ascorbic acid induced phosphatidylcholine liposome oxidation, scavenged stable DPPH•, ABTS•+and superoxide anion radicals, and acted as reductant. In contrast, the leaf inner gel did not show any antioxidant activity. It was concluded that the known beneficial effects ofAloe veracould be attributed to its antioxidant activity and could be related to the presence of phenolic compounds and antioxidant vitamins. more...

Background: Because reactive oxygen species (ros) contribute to the pathogenesis of various acute and chronic liver diseases, dietary antioxidants and drugs from herbal origins have been proved to be beneficial as therapeutic agents in reversing hepatotoxicity and oxidative stress. The objective of this study was to investigate the protective effect of an aqueous extract from smilax excelsa l. Shoots and leaves against acute ccl4-induced liver injury as well as the changes in antioxidative defense system in female wistar albino rats. Materials and Methods: S. Excelsa extract was administered orally in doses of 100, 200 and 400 mg/kg body weight, once daily for 9 days. Acute hepatic toxicity was induced by intraperitoneal injection of ccl4 (1 ml/kg) on the 10th day. 24 h after ccl4 intoxication, biochemical and histopathological analyses were undertaken on sera and liver tissues. Results: Ccl4 challenge caused significant increases in the activities of liver enzymes as well as the levels of bilirubin, malondialdehyde and nitric oxide, while total serum protein levels and antioxidant defense system parameters were reduced significantly compared to the normal group. Administration of s. Excelsa extract at a dose of 400 mg/kg resulted in a suppression of ccl4-induced lipid peroxidation and altered oxidative stress parameters to nearly normal values in comparison to ccl4-treated rats. Nevertheless the extract did not reduce the extent of ccl4-induced mild liver injury, as seen by the histopathology of liver damage. Conclusion: The results of this study suggest that s. Excelsa could protect the liver tissues against ccl4-induced oxidative stress probably by increasing antioxidative defense activities. more...

Significant degenerative changes were observed in the kidney tissue of untreated neonatal streptozotocin (n0STZ)-induced type-II diabetic rats. These degenerative changes were diminished in the kidney tissue of diabetic animals given glibenclamide and Aloe leaf gel and pulp extracts. Kidney lipid peroxidation levels were increased in diabetic rats compared to healthy rats; these levels were higher in rats treated with glibenclamide than in those which received Aloe extracts. Serum urea and creatinine levels were higher in diabetic rats in comparison to healthy rats. The administration of Aloe gel extract and glibenclamide decreased serum urea and creatinine levels in comparison to diabetic controls. Only A. vera leaf gel extract showed improvement both in histological and biochemical parameters suggesting a protective effect of A. vera on mild damage caused by type-II diabetes on kidney tissue. more...

An extracellular α-galactosidase from the culture filtrate of Aspergillus flavipes grown on melibiose as a carbon source was partially purified by hydroxylapatite and diethylaminoethylcellulose chromatographies. Electrophoretic analysis showed protein bands corresponding to α-galactosidase and invertase activities. The optimum pH and temperature were determined as 4.5–5.0 and 45°C, respectively. The Km value for p-nitrophenyl-α-d-galactopyranoside was found to be 1.89 mm. The results reported in this study indicate that Aspergillus flavipes is indeed an active source of extracellular α-galactosidase. Copyright © 2003 John Wiley & Sons, Ltd. more...