Salvia leriifolia Benth (Lamiaceae) extract demonstrates in vitro antioxidant properties and cholinesterase inhibitory activity

The object of the present study was to investigate the in vitro antioxidant properties and cholinesterase inhibitory activity of Salvia leriifolia Benth extracts and fractions. The functional role of herbs and spices and their constituents is a hot topic in food-related plant research. Salvia species have been used since ancient times in folk medicine for cognitive brain function and have been subjected to extensive research. Thus, we hypothesize that S leriifolia, because of its functional properties, would be a good candidate to use as a nutraceutical product for improving memory in the elderly or patients affected by Alzheimer disease (ad). To test this hypothesis, we examined the cholinesterase inhibitory activity using the modified colorimetric Ellman's method against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The n-hexane exhibited the highest activity, with inhibitory concentration 50% (IC₅₀) values of 0.59 and 0.21 mg/mL, for AChE and BChE, respectively. This extract was fractionated, and 9 of these fractions (A-I) were obtained and tested. Fraction G, characterized by the presence of sesquiterpenes as major components, was the most active against AChE (IC₅₀ = 0.05 mg/mL). Because oxidative stress is a critical event in the pathogenesis of AD, we decided to screen the antioxidant activity (AA) using 2,2-diphenyl-1-picrylhydrazyl test, β-carotene bleaching test, and bovine brain peroxidation (thiobarbituric acid) assay. The ethyl acetate extract showed the highest activity, with IC₅₀ values of 2 and 33 μg/mL on β-carotene bleaching test and thiobarbituric acid test, respectively. These results suggest potential health benefits of S leriifolia extracts. However, this finding requires additional investigation in vivo.     

Antioxidant and cyclooxygenase inhibitory activity of sorrel (Hibiscus sabdariffa)

The antioxidant activity of the hexane, ethyl acetate and methanol extracts of three varieties of sorrel (Hibiscus sabdariffa), as well as their potential for reducing blood viscosity, were studied in vitro. The samples screened were two red [(traditional red (TRED) and early bearing red (ERED)] and one white (WHTE) mature Hibiscus varieties. Antioxidant activity was measured by fluorescence spectroscopy using a model liposome system. Cyclooxygenase inhibitory activity was measured using cyclooxygenase (COX-1 and COX-2) enzymes by monitoring the rate of oxygen uptake in prostaglandin synthesis. Antioxidant activity was the highest overall in the red varieties compared to the white. The methanol extract from the three varieties had the highest activity. The methanol and ethyl acetate extracts of the three varieties of sorrel showed higher COX-1 enzyme inhibition than COX-2 and therefore had high potential to decrease blood viscosity. There was no COX-1 or COX-2 inhibition in the hexane extract. These findings support the ethnomedicinal use of H. sabdariffa in Africa and the Caribbean for the treatment of cardiovascular disease and hypertension.     

Synthesis and antimalarial activity of new atovaquone derivatives

In this paper we describe the design and synthesis of 18 derivatives of the antimicrobial atovaquone which were substituted at the 3-hydroxy group by ester and ether functions. The compounds were evaluated in vitro for their activity against the growth of Plasmodium falciparum, the malaria causing parasite. All the compounds showed potent activity, with IC₅₀ values in the range of 1.25–50 nM, comparable to those of atovaquone and much higher than chloroquine or quinine.     

Determination of total phenol content, antioxidant activity and acetylcholinesterase inhibition in selected mushrooms from Turkey

In the present study, we investigated the acetylcholinesterase (AChE) inhibitory activity of the ethanolic extracts of a number of mushroom species growing in Turkey, including mainly Polyporus species (Polyporus gilvus, Polyporus sulphureus, Polyporus annosus, Polyporus radiatus, Polyporus pinicola, Polyporus volvatus, Polyporus fomentarius, Polyporus stevenii, Polyporus badius), as well as Cantharellus cibarius, Lactarius deliciosus, and Trametes versicolor. The analyses were carried out using the spectrophotometric method of Ellman in ELISA microplate reader at 500 μg/ml. Since Alzheimer's disease (AD) is associated with oxidative degeneration of cells, several methods of antioxidant activity were applied to the mushroom extracts such as 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, ferrous ion-chelating effect, ferric-reducing antioxidant power (FRAP), and beta-carotene bleaching tests. Total phenol contents of the extracts were also determined by Folin-Ciocalteu reagent. In anti-AChE assay, the most active one was P. sulphureus having 31.44% of inhibition. P. voluatus showed the best scavenging effect against DPPH, while all of the extracts exerted low capacity in chelating ferrous ions and reducing ferric ion.     

Phenolic content and antioxidant capacity of Philippine potato (Solanum tuberosum) tubers

Four potato (Solanum tuberosum) varieties – Bengueta, Ganza, Igorota and 125411.22 – were analyzed for total phenolic content and antioxidant activities to provide baseline data for Philippine potato varieties. Bengueta had the highest phenolic content with 50.0 ± 1.5 mg gallic acid equivalent (GAE)/100 g (dry basis, DB). It also had the highest DPPH radical scavenging activity with an EC₅₀ value of 30.6 ± 3.6 mg/mL (DB). The potato variety125411.22 had the highest reducing power with EC₅₀ equal to 66.2 ± 1.6 mg/mL (DB), while Igorota had the highest iron-chelating capacity with an EC₅₀ of 11.0 ± 3.2 mg/mL (DB) and the best inhibitory action against linoleic acid oxidation at 95.4 ± 2.2% at 50 mg/mL sample concentration. Methanolic potato extracts had better antioxidant activity than α-tocopherol and better iron chelating capacity than ethylenediamine tetraacetic acid (EDTA). Significant (^*P < 0.05) negative correlation (R = −0.542) was observed between total phenolic content and the EC₅₀ values for DPPH radical scavenging activity, but none between total phenolic content and reducing power, iron-chelating capacity and total antioxidant activity.     

Phenolic composition and radical scavenging activity of commercial Greek white wines from Vitis vinifera L. cv. Malagousia

Seven commercial white wine samples of the Malagousia cultivar were investigated for the first time with regard to their phenolic composition and radical scavenging activity. Total phenol content, corrected for ascorbic acid contribution (0–47 mg gallic acid equivalents/L of wine), ranged between 241 and 336 mg gallic acid equivalents/L of wine. On the other hand, the range for total hydroxycinnamates was 51.5–122.4 mg chlorogenic acid equivalents/L of wine and that for total flavanols 19.6–68.8 mg catechin equivalents/L wine. Fifteen phenolic compounds were identified and quantified by gas chromatography/mass spectrometry in the selective ion monitoring and high-performance liquid chromatography coupled with diode array detector. Tyrosol, caftaric, caffeic and 2-S-glutathionyl caffeoyl tartaric (GRP) acids were the major phenolics in all samples with mean concentrations of 12.32, 10.71, 10.17 and 4.79 mg/L wine, respectively. Catechin (3.75 mg/L) and p-coumaric acid (3.04 mg/L) followed in abundance. Variations in the values of GRP/caftaric (0.1–4.6) and caffeic/caftaric (0.4–4.2) acid concentrations, suggested differences in the degree of oxidation on one hand and hydrolytic processes during production and bottling on the other. Despite these variations, the radical scavenging activity of samples examined with DPPH and ABTS⁺ assays (mean value 0.85 and 3.45 mmol Trolox equivalents/L of wine) indicated a high efficiency in comparison to literature data on native and foreign white wines. The present findings can be useful for both technological and nutritional purposes.     

Antioxidant and free radical scavenging capacity of the underutilized legume, Vigna vexillata (L.) A. Rich

The raw and processed seeds of the underutilized legume, Vigna vexillata (L.) A. Rich were extracted with 70% acetone and used for the evaluation of its antioxidant potential. The different heat treatments included dry heating, soaking followed by autoclaving with 0.1% sodium bicarbonate, soaking followed by autoclaving and autoclaving without soaking. The raw seed extract contained higher levels of total phenolics (11.7 g/100 g) and tannins (5.9 g/100 g) than the processed seed extracts. The extracts were further evaluated for their antioxidant activities using FRAP, Fe²⁺ chelation, phosphomolybdenum reduction, DPPH and ABTS⁺ radical scavenging, antihemolytic and β-carotene/linoleic acid emulsion systems. In general, the raw seed extracts were the most potent antioxidant suppliers and free radical scavengers. Interestingly, among the various processing methods, acetone extract of dry heated seed sample registered higher antihemolytic activity (86.2%) at the concentration of 500 μg/ml, whereas, in β-carotene/linoleic acid emulsion system, the extracts of raw seeds and the presoaked seeds followed by autoclaving with 0.1% sodium bicarbonate exhibited higher and comparable activity than other processed seed extracts.     

Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro

The synthesis of novel 1,3-diaryl propenone derivatives and their antimalarial activity in vitro against asexual blood stages of human malaria parasite, Plasmodium falciparum, are described. Chalcone derivatives were prepared via Claisen-Schmidt condensation of substituted aldehydes with substituted methyl ketones. Antiplasmodial IC(50) (half maximal inhibitory concentration) activity of these compounds ranged between 1.5 and 12.3 microg/ml. The chloro-series, 1,2,4-triazole substituted chalcone was found to be the most effective in inhibiting the growth of P. falciparum in vitro while pyrrole and benzotriazole substituted chalcones showed relatively less inhibitory activity. This is the first report on antiplasmodial activity of chalcones with azoles on acetophenone ring.     

Leishmania species identification using FTA card sampling directly from patients' cutaneous lesions in the state of Lara, Venezuela

A molecular epidemiological study was performed using FTA card materials directly sampled from lesions of patients with cutaneous leishmaniasis (CL) in the state of Lara, Venezuela, where causative agents have been identified as Leishmania (Viannia) braziliensis and L. (Leishmania) venezuelensis in previous studies. Of the 17 patients diagnosed with CL, Leishmania spp. were successfully identified in 16 patients based on analysis of the cytochrome b gene and rRNA internal transcribed spacer sequences. Consistent with previous findings, seven of the patients were infected with L. (V.) braziliensis. However, parasites from the other nine patients were genetically identified as L. (L.) mexicana, which differed from results of previous enzymatic and antigenic analyses. These results strongly suggest that L. (L.) venezuelensis is a variant of L. (L.) mexicana and that the classification of L. (L.) venezuelensis should be reconsidered.     

Synthesis and in vitro leishmanicidal activity of 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-substituted-1,3,4-thiadiazole derivatives

A series of 2-(1-methyl-5-nitroimidazol-2-yl)-5-(1-piperazinyl, 1-piperidinyl and 1-morpholinyl)-1,3,4–thiadiazoles (3a–g) were synthesized and evaluated for in vitro leishmanicidal activity against Leishmania major promastigotes. The leishmanicidal data revealed that compounds 3a–g had strong and much better leishmanicidal activity than the reference drug pentostam. Compound 3c (piperazine analog) was the most active compound (IC₅₀ = 0.19 μM).     

In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity

The taxane diterpneoid 2-deacetoxytaxinine J (2-DAT-J) 1 has been isolated from the bark of Himalayan yew, Taxus baccata L. spp. wallichiana in a reasonably good yield (0.1%) and its anticancer activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human kidney epithelial cell line (HEK-293) has been studied. 2-DAT-J (1) showed significant in vitro activity against breast cancer cell line at a concentration of 20 μM and 10 μM in MCF-7 and MDA-MB-231 respectively. Few novel taxoids were derived (7, 8 and 10–13) from the naturally occurring 2-DAT-J (1) and screened for their anticancer activity. The structure–activity relationship studies indicated that the cinnamoyl group on C-5 and acetyl group on C-10 are essential for the anticancer activity. 2-DAT-J (1) was also tested for its in vivo activity on DMBA-induced mammary tumors in virgin female Sprague Dawley rats at a dose of 10 mg/kg body weight orally for 30 days and showed significant regression in mammary tumors as compared to vehicle treated group (p < 0.05).     

Search for new pharmacophores for antimalarial activity. Part III: Synthesis and bioevaluation of new 6-thioureido-4-anilinoquinazolines

Syntheses and in vitro antimalarial evaluation of 42 new thioureidoquinazolines have been carried out. Several analogs showed promising antimalarial effect in the in vitro investigation against chloroquine-sensitive 3D7 strain of Plasmodium falciparum whereas one of the compounds shows 50% curative effect in the mouse model at an oral dose of 100 mg/kg × 4 days against multidrug resistant Plasmodium yoelii nigeriensis.     

Sporicidal activity of sodium dichloroisocyanurate, peroxygen and glutaraldehyde disinfectants against Bacillus subtilis

The activity of sodium dichloroisocyanurate (NaDCC), peroxygen and glutaraldehyde disinfectants against spores of Bacillus subtilis NCTC 10073 was evaluated using suspension tests. The activity of aqueous solutions of NaDCC disinfectants increased with the level of available chlorine (av.Cl) but was considerably reduced by low levels of blood. Five percent Titan Sanitizer (1200 ppm av.Cl) achieved a > 10⁵-fold reduction in spore count (kill) in 3 h in the absence of blood but no kill in 3 h with 2% blood present. One percent Presept (3180 ppm av.Cl) achieved a > 10⁵-fold kill in 1 h in the absence of blood and in 2 h with 2% blood present. One percent Haz-Tab (5750 ppm av.Cl) achieved a >10⁵-fold kill in 5 min in the absence of blood and in 30 min with 2% blood present. One percent Virkon (peroxygen) achieved a 10⁵-fold kill in 2–3 h in the absence of blood but little kill in 3 h with 2% blood present. Nu-Cidex (peracetic acid) was rapid in action and tolerant of organic matter. A 24 h old solution achieved a > 10⁵-fold kill in 5 min with 10% serum present. Cidex Long-Life (glutaraldehyde) worked much slower; a 28-day-old solution achieved a >10⁵-fold kill in 2 h with 4% blood present. Neat sporicidin (glutaraldehyde-phenate) was slightly superior to Cidex Long-Life but in a 1 in 8 dilution exhibited markedly reduced activity; a 30-day-old solution achieved a 10⁴-fold kill in 10 h in the absence of blood but only a 10²-fold kill in 10 h with 2% blood present.     

Low genetic diversity and epidemiological significance of Listeria monocytogenes isolated from wild animals in the far east of Russia

The causative agent of listeriosis, a serious disease of humans and animals, Listeria monocytogenes is a ubiquitous bacterium that inhabits both anthropogenic and pristine environments. We report L. monocytogenes isolation from wild animals, humans, food and the environment of a far eastern region of Russia. In total, 654 samples of internal organs of small rodents belonging to the Muridae and Cricetidae families, and 986 samples of the liver and muscles of mollusks and fish were examined to obtain 7 and 14 independent L. monocytogenes isolates, respectively. The wild animal isolates were compared with human (n=9), food (n=8) and environmental (n=3) isolates obtained in the same region. Twenty of the 21 wild animal isolates belonged to the serovar 4b. The serovars 4b, 1/2a, 1/2b, and 4b, 1/2a, 1/2b, 1/2c were found between human and food isolates, respectively. All isolates were characterized into molecular subtypes by DNA sequencing of the 618 bp internal fragment of the house keeping gene prs and 621 bp internal fragment of the virulence gene inlB. Sequence analysis revealed 4 and 13 alleles for prs and inlB fragments, respectively. Distinct prs and inlB alleles clustered into two groups consistently with established phylogenetic lineages. Among isolates of every lineage, the nucleotide diversity of the prs fragment was low; the nucleotide diversity of the inlB fragment was low among wild animal isolates and higher among human isolates. All rodent isolates and 10 of 14 marine organism isolates carried the same allele of the inlB fragment, which was also found among environmental (two of three), food (two of eight) and human (two of nine) isolates.     

Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds

A series of nitroaromatic compounds was synthesized and evaluated as potential antileishmanial and trypanocidal agents. Five compounds exerted significant anti-leishmanial activity in vitro against promastigotes forms of Leishmania (L.) amazonensis, with IC₅₀ in the range of 23–59 μmol L⁻¹, but none were active against amastigotes intracellular forms of Trypanosoma cruzi. In vitro cytotoxicity on the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated with phytohemaglutinin (PHA) was also evaluated. Two compounds, 6 and 7, were found to present a promising anti-leishmanial activity with IC₅₀ values of 59.5 and 50.6 μM, respectively, without affecting the lymphocyte proliferation in PBMCs (selectivity index of 16.1 and 21.7, respectively), indicating low toxicity to human cells.     

Phytoremediation of stable Cs from solutions by Calendula alata, Amaranthus chlorostachys and Chenopodium album

Uptake rate of ¹³³Cs, at three different concentrations of CsCl, by Calendula alata, Amaranthus chlorostachys and Chenopodium album plants grown outdoors was studied. These plants grow abundantly in semi-arid regions and their varieties exist in many parts of the world. When exposed to lowest Cs concentration 68 percent Cs was remediated by Chenopodium album.¹³³Cs accumulation in shoots of Amaranthus chlorostachys reached its highest value of 2146.2 mg kg⁻¹ at a ¹³³Cs supply level of 3.95 mg l⁻¹ of feed solution. The highest concentration ratio value was 4.89 for Amaranthus chlorostachys, whereas for the other tests it ranged from 0.74 to 3.33. Furthermore uptake of ¹³³Cs by all three species increased with increasing metal concentrations. The results also indicated that hydroponically grown Calendula alata, Amaranthus chlorostachys and Chenopodium album could be used as potential candidate plants for phytoremediation of solutions contaminated with Cs.     

The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its IC₅₀ values ranged from 47.1 to 210.5 µg/ml and IC₅₀ of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and 56.5 µg/ml, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.     

Hepatic glutathione S-transferase activity in flounder collected from contaminated and reference sites along the Polish coast

The aim of the present study was to examine the activity of hepatic glutathione S-transferase (GST) in flounder, Platichthys flesus, as a potential biomarker of exposure to xenobiotics present in the environment. The fish were collected along known pollution gradients and from areas regarded relatively free of anthropogenic input. GST was measured spectrophotometrically in each sampled specimen of flounder. The databases from the studies performed by two research institutes were compiled, and generalized linear models were used to analyze the dependence of the enzyme activity on the time and area of sampling and on selected biological parameters of the fish. Fish sex, sampling area, year, month, water temperature, and somatic indices (gonado-somatic index, hepato-somatic index) were significant in the model of GST activity. The three annual datasets showed that the biomarker activities exhibited in the Gulf of Gdansk were significantly different from those measured in the areas off the coast.     

热带假丝酵母菌临床分离株毒力表型特征研究

目的 描述临床分离的热带假丝酵母菌培养不同时间的天冬氨酰蛋白酶活性(蛋白酶活性)、磷脂酶活性和溶血活性,并分析不同感染部位分离菌的蛋白酶活性和溶血活性差异。方法 将分离自不同感染部位的热带假丝酵母菌鉴定后分别接种在牛血清蛋白培养基、卵黄琼脂培养基和羊血琼脂培养基上,培养不同时间(24、48和72 h)后检测蛋白酶活性、磷脂酶活性和溶血活性。结果 热带假丝酵母菌培养24、48和72 h时均具有蛋白酶活性和溶血活性,但未表现出磷脂酶活性;热带假丝酵母菌在48 和72 h时的蛋白酶活性高于其在24 h时的活性,在72 h范围内,溶血活性随培养时间延长持续增长;分离自不同感染部位的热带假丝酵母菌的蛋白酶活性(P=0.368)和溶血活性(P=0.985)差异无统计学意义。结论 我国热带假丝酵母菌临床分离株培养不同时间具有蛋白酶活性和溶血活性,但无磷脂酶活性。     

Comparison of the contents of bioactive compounds and the level of antioxidant activity in different kiwifruit cultivars

The aim of this investigation was to find the best among four different cultivars of kiwifruit (‘Hayward’, ‘Daeheung’, ‘Haenam’ and ‘Bidan’) for human consumption. The bioactive compounds and the level of antioxidant activity of these cultivars were determined and compared. The presence of polyphenols (flavonoids and phenolic acids) in the investigated samples was studied by Fourier transform infrared (FT-IR) spectroscopy. By far the highest levels (P < 0.05) of polyphenols and ascorbic acids were found in ‘Bidan’ (25.9 ± 1.3 mg GAE/g and 152 ± 10.4 mg/g DW, respectively), which also contained the highest levels of protocatechuic and vanillic acids. In addition, the level of antioxidant activity (μM TE/g DW) was significantly higher (P < 0.05) in ‘Bidan’ (121 ± 5.8, 109 ± 11.2, 102 ± 6.6 and 94 ± 4.7 for CUPRAC, ABTS, DPPH and FRAP radical scavenging assays, respectively). Pattern-recognition techniques (cluster analysis, principal component analysis, factor analysis, and canonical discriminant analysis) were used to compare the cultivars. A high correlation was found among the polyphenols (R² = 0.99), ascorbic acid (R² = 0.99+) and the antioxidant activity in the studied cultivars. In conclusion, the overall bioactivity of the cultivars was: ‘Bidan’ > ‘Haenam’ > ‘Daeheung’ = ‘Hayward’. ‘Bidan’, a relatively new cultivar, can be recommended for consumption.