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Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Plants of the genus Hypericum are widely used in folk medicine for the treatment of gastric ailments, bums, inflammation, microbial infections, skin wounds and psycological disorders. Five endemic Hypericum species in Turkey (H. kotschyanum Boiss., H. scabroides Robson & Paulter, H. salsugineum Robson & Hub.-Mor, H. thymopsis Boiss. and H. uniglandulosum Hausskn. ex Bomm.) were tested in vitro for antioxidant activity. Methanol-acetone extracts of the aerial parts of H. salsugineum and H. scabroides possessed significant activity which may be attributed to their strong reducing power, DPPH and superoxide radicals scavenging, metal chelating and lipid peroxidation inhibitory activities. The superoxide radical scavenging activity of H. scabrides (EC50: 1.14 ± 0.046 mg/ml) and H. salsugineum (EC50: 1.09 ± 0.096 mg/ml) were more remarkable than that of other three species. The antimicrobial study was carried out by microbroth dilution technique. The extracts showed good antibacterial activity against Gram-positive bacteria but no antifungal activity. Chloroform extract of the aerial parts of H. scabroides showed antibacterial activity against Staphylococcus aureus with a MIC value of 39.06 µg/ml. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

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. [ABSTRACT FROM AUTHOR]

In this study, antioxidant, antiacetylcholinesterase, anti-inflammatory, and DNA protecting activities of the aerial parts of Glaucium grandiflorum var. grandiflorum were evaluated. The lyophilized methanolic extract of the aerial parts of G. grandiflorum var. grandiflorum was investigated for potential in-vitro antioxidant properties in thiobarbituric acid test using the lipid peroxidation of liposomes, ferric ion reducing antioxidant power (FRAP), 1,1-diphenyl- 2-picrylhydrazyl, 2, 2'-azinobis(3-ethylbenzothiazoline-6-sulphonate) free-radicals and hypochlorous acid scavenging assays. The extract demonstrated antioxidant activity in all the assays. The (AChE) inhibition capacity of the lyophilized methanolic extract at 320 µg/mL (80.75 ± 1.59%) was found to be strong and almost equal to the inhibition capacity of the positive control, galantamine (82.23 ± 2.21%) at 25 µg/mL. The significant AChE inhibitory activity suggests that the extract may be beneficial in the treatment of Alzheimer's disease. The extract also showed inhibitory activity against plasmid DNA damage (94%), as well as COX-2 69.05%, which is a target for many anti-inflammatory and cancer-preventive drugs. These results indicate that G. grandiflorum var. grandiflorum methanolic extract is an excellent source of compounds with antioxidant, anti-acetylcholinesterase and anti-inflammatory properties that prevent DNA damage. [ABSTRACT FROM AUTHOR]

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, antiinflammatory and wound healing agent. [ABSTRACT FROM AUTHOR]

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) (EC50 = 47.4 µg mL-1), inhibited both β-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 α-tocopherol analogue, and 1.91 mM L-1 Fe2+, 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. [ABSTRACT FROM AUTHOR]

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 (EC 50 = 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.

In this study, antioxidant, antiacetylcholinesterase, anti-inflammatory, and DNA protecting activities of the aerial parts of Glaucium grandiflorum var. grandiflorum were evaluated. The lyophilized methanolic extract of the aerial parts of G. grandiflorum var. grandiflorum was investigated for potential in-vitro antioxidant properties in thiobarbituric acid test using the lipid peroxidation of liposomes, ferric ion reducing antioxidant power (FRAP), 1,1-diphenyl-2-picrylhydrazyl,2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonate) free-radicals and hypochlorous acid scavenging assays. The extract demonstrated antioxidant activity in all the assays. The (AChE) inhibition capacity of the lyophilized methanolic extract at 320 μg/mL (80.75 ± 1.59%) was found to be strong and almost equal to the inhibition capacity of the positive control, galantamine (82.23 ± 2.21%) at 25 μg/mL. The significant AChE inhibitory activity suggests that the extract may be beneficial in the treatment of Alzheimer's disease. The extract also showed inhibitory activity against plasmid DNA damage (94%), as well as COX-2 69.05%, which is a target for many anti-inflammatory and cancer-preventive drugs. These results indicate that G. grandiflorum var. grandiflorum methanolic extract is an excellent source of compounds with antioxidant, anti-acetylcholinesterase and anti-inflammatory properties that prevent DNA damage.

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.

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., (Copyright (c) 2009 Elsevier Masson SAS. All rights reserved.)

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.

An extracellular alpha-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 alpha-galactosidase and invertase activities. The optimum pH and temperature were determined as 4.5-5.0 and 45 degrees C, respectively. The Km value for p-nitrophenyl-alpha-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 alpha-galactosidase., (Copyright 2003 John Wiley & Sons, Ltd.)