Volume 66, Issue 3-4

Six isoflavonoid derivatives among which three are new have been isolated from the stem heartwood of Lophira alata. The structures were elucidated from spectroscopic and chemical evidences. Two have unusual carbon skeletons, possibly resulting from a variant of isoflavonoid biogenesis. The two compounds form the first members of a new subclass of flavonoid compounds which we call "isobiflavonoids". The presence of these isoflavonoid compounds in this plant of the Ochnaceae family has important chemotaxonomic implications since it modifies the botanic distribution of isoflavonoid compounds in non-leguminous plants

Benzothiophene carboxamide derivatives of aminobenzophenone, aminopyridine, aminobenzimidazole, and aniline derivatives (compounds 1 - 9) were synthesized and compounds 3, 6, 7, 8, and 9 tested in vivo for their hypolipidemic activity. Compounds 1 - 8 were prepared adopting the fusion process at 130 - 150°C between benzothiophene-2-carbonyl chloride and aminobenzophenones, aminopyridine, and anilines, respectively, and were obtained in high yield, while compound 9 was obtained from the reaction of benzothiophene acyl chloride with aminobenzimidazole in DMF at 160°C. At a dose of 15 mg/kg body weight compounds 6, 7, and 9 significantly reduced plasma triglyceride levels in Triton WR-1339-induced hyperlipidemic rats in comparison to control rats. Furthermore, they significantly increased high-density lipoprotein levels. It is therefore reasonable to assume that compounds 6, 7, and 9 may have a promising potential in the treatment of hyperlipidemia and atherosclerosis

The antimicrobial activity of twenty two synthetic flavonoids is reported. Among them three 3-arylideneflavanones, 2b, 2c, and 2i, were shown to be highly active against Staphylococcus aureus, S. epidermidis, and Enterococcus faecalis reference strains, with MIC (minimal inhibitory concentration) values ranging from 4.68 μg/ml (14.3 μM) to 37.5 μg/ml (119.7 μM). The synergy of oxacillin and vancomycin with 2c, evaluated as fractional inhibitory concentration index (FICI) was shown (against planktonic culture of S. aureus A3 and E. faecium 138/09 clinical strains). The presence of 2c in the culture medium diminished the initial adhesion of bacteria to an abiotic surface. Such an effect resulted in a decrease in biofilm formation during prolonged culture. Unfortunately, 2c failed to eradicate the S. aureus mature biofilm which was already preformed, however, decreased the number of live biofilm cells. The biofilm of E. faecalis was more susceptible to the action of 3-arylideneflavanone 2c than the S. aureus biofilm. The finding that 3-arylideneflavanones are lipophilic, cause bacterial aggregation, and influence the integrity of membranes making them permeable to SYTO 9/propidium iodide dyes may implicate the cytoplasmic membrane as a target site for these compounds activity

The chemical study of Laennecia schiedeana afforded three sterols, five diterpenes, five flavonoids, three caffeoyl derivatives of quinic acid, and two triterpenes. Evaluation of the cytotoxic activity of the extracts and isolated metabolites showed that 15-methoxy-16-oxo- 15,16H-strictic acid was the most active compound [(15.05 ± 2.2) μg/mL against U-251 cells]. In antibacterial assays the acetonic extract of leaves was the only active extract exhibiting its highest effect against the multiresistant Staphylococcus epidermidis (MIC 0.25 mg/mL). The anti-inflammatory activity observed was mild in the extracts and not relevant in the isolated compounds

This study reports the antibacterial activity of an oligosaccharide, prepared by partial acid hydrolysis of a native Paecilomyces sp. exopolysaccharide, and of its aminoglycosylated derivative, prepared by reductive alkylation of the oligosaccharide, against E. coli and S. aureus

A crude acetone extract and oil of ripe fruits from Melia azedarach L. were evaluated against the 2 nd and 4 th instar larvae of Spodoptera littoralis (Boisd.) (Lepidoptera: Noctuidae). Both oil and extract exhibited highly significant growth inhibition at all concentrations tested, while the oil of M. azedarach recorded higher insecticidal activity against both instars than the crude extract. GC-MS analysis of the oil revealed the presence of linoleic acid methyl ester, oleic acid methyl ester, and free oleic acid as the main components in addition to hexadecanol, palmitic acid, methyl esters of stearic acid and myristic acid. Fatty acids and their esters were not only the main constituents of essential oil from the ripe fruits of M. azedarach, but also mainly responsible for the insecticidal and growth inhibition activity against S. littoralis

A quantitative structure-activity relationship model for Morita-Baylis-Hillman adducts with leishmanicidal activities was developed which correlates molecular orbital energy and dipole with percentage in the promastigote stage

The aerial parts of Pituranthos tortuosus (Desf.) Benth and Hook (Apiaceae), growing wild in Egypt, yielded 0.8%, 0.6%, and 1.5% (v/w) of essential oil when prepared by hydrodistillation (HD), simultaneous hydrodistillation-solvent (n-pentane) extraction (Lickens- Nickerson, DE), and conventional volatile solvent extraction (preparation of the “absolute”, SE), respectively. GC-MS analysis showed that the major components in the HD sample were β-myrcene (18.81%), sabinene (18.49%), trans-iso-elemicin (12.90%), and terpinen- 4-ol (8.09%); those predominent in the DE sample were terpinen-4-ol (29.65%), sabinene (7.38%), γ-terpinene (7.27%), and β-myrcene (5.53%); while the prominent ones in the SE sample were terpinen-4-ol (15.40%), dill apiol (7.90%), and allo-ocimene (4E,6Z) (6.00%). The oil prepared in each case was tested for its cytotoxic activity on three human cancer cell lines, i.e. liver cancer cell line (HEPG2), colon cancer cell line (HCT116), and breast cancer cell line (MCF7). The DE sample showed the most potent activity against the three human cancer cell lines (with IC 50 values of 1.67, 1.34, and 3.38 μg/ml against the liver, colon, and breast cancer cell lines, respectively). Terpinen-4-ol, sabinene, γ-terpinene, and β-myrcene were isolated from the DE sample and subjected to a similar evaluation of cytotoxic potency; signifi cant activity was observed

The lipid profiles of Synechococcus sp. PCC7002 and two related 16S rDNA (99% identity) strains were established by a new method of high-performance liquid chromatography coupled to electrospray-mass spectrometry (HPLC-MS). Lipids were analysed in the positive and negative ionization mode, and fragmentation patterns are reported. No differences in the lipid profi le between the three strains could be observed, but the relative content of some species differed. Major lipid species were found to be 1-octadecatrienoyl- 2-hexadecanoyl-3-(6’-sulfo-α-D-quinovosyl)-sn-glycerol [SQDG (18:3/16:0)] and 1-octadecatrienoyl-2-hexadecenoyl-3-β-D-monogalactosyl-sn-glycerol [MGDG (18:3/16:1)]. Ten species of SQDG, six species of PG (phosphatidyl-glycerol), seven species of MGDG, and two species of DGDG (digalactosyl-diacyl-glycerol) were detected. A PG species (m/z 761) containing hydroxylinolenic acid or oxophytodienoic acid acyl ester (C18H32O3), and SQDG species containing C17:1 and C17:3 fatty acyl esters are reported for the first time in cyanobacteria. The method also allowed the separation of two pairs of closely related isobaric MGDG species (m/z 770 and m/z 772 in positive ionization)

In contrast to differentiated leaves, the regulatory mechanisms of chloroplast gene expression in darkened cotyledons have not been elucidated. Although some results have been reported indicating accelerated senescence in Arabidopsis upon reillumination, the capacity of cotyledons to recover after dark stress remains unclear. We analysed the effect of twodays dark stress, applied locally or at the whole-plant level, on plastid gene expression in zucchini cotyledons. Our results showed that in the dark the overall chloroplast transcription rate was much more inhibited than the nuclear run-on transcription. While the activities of the plastid-encoded RNA polymerase (PEP) and nuclear RNA polymerase II were strongly reduced, the activities of the nuclear-encoded plastid RNA polymerase (NEP) and nuclear RNA polymerase I were less affected. During recovery upon reillumination, chloroplast transcription in the cotyledons was strongly stimulated (3-fold) compared with the naturally senescing controls, suggesting delayed senescence. Northern blot and dot blot analyses of the expression of key chloroplast-encoded photosynthetic genes showed that in contrast to psbA, which remained almost unaffected, both the transcription rate and mRNA content of psaB and rbcL were substantially decreased

Phyllanthus has been widely used in traditional medicine as an antipyretic, a diuretic, and to treat liver diseases and viral infections. Correct genotype identification of medicinal plant material remains important for the botanical drug industry. Limitations of chemical and morphological approaches for authentication have generated the need for newer methods in quality control of botanicals. In the present study, attempts were made to identify species- diagnostic markers for ten Phyllanthus species using the inter simple sequence repeat-polymerase chain reaction (ISSR-PCR) fingerprinting method. PCR amplification using seven ISSR primers resulted in significant polymorphism among the populations from different species. P. angustifolius and P. urinaria showed monomorphic frequency of maximum (63.88%) and minimum (20.64%), respectively. Seventeen species-diagnostic markers were identified for seven species (P. acidus, P. emblica, P. fraternus, P. urinaria, P. rotundifolius, P. amarus, and P. angustifolius) while no marker was detected for P. reticulatus, P. nivosus, and P. virgulatus. A maximum of six species-diagnostic markers were identified for P. acidus and a minimum of only one of 755 bp was available for P. amarus. Among the seventeen markers, nine were present in all individuals of particular species. The speciesspecific differences in fragment numbers and sizes could be used as diagnostic markers to distinguish the Phyllanthus species quickly

The response surface methodology (RSM) involving central composite design (CCD) was employed to optimize the fermentation medium for the cell growth and schizophllan production by Schizophyllum commune CGMCC 5.113 in submerged culture at pH 6.5 and 26°C. The four variables involved in this study were glucose, yeast extract, ammonium nitrate, and magnesium sulfate. The statistical analysis of the results showed that, in the range studied, glucose and yeast extract had a highly significant effect on schizophyllan production. The optimal medium for schizophyllan production calculated from the regression model of RSM was as follows: glucose, 18 g/l; yeast extract, 0.5 g/l; NH 4 NO 3 , 0.48 g/l; and MgSO 4 , 0.05 g/l, with a predicted maximum schizophyllan production of 11.74 g/l. These predicted values were experimentally validated. The excellent correlation between predicted and measured values justifies the validity of the response model. The results of bioreactor fermentation also show that the optimized medium enhanced schizophyllan production (12.80 g/l) by S. commune in a 5-l fermenter

A previous work suggested that peptides from the histidine-containing copper-binding motifs in human prion protein (PrP) function as peroxidase-like biocatalysts catalyzing the generation of superoxide anion radicals in the presence of neurotransmitters (aromatic monoamines) and phenolics such as tyrosine and tyrosyl residues on proteins. In this study, using various phenolic substrates, the phenol-dependent superoxide-generating activities of PrP-derived peptide sequences were compared. Among the peptides tested, the GGGTH pentapeptide was shown to be the most active catalyst for phenol-dependent reactions. Based on these results, we designed a series of oligoglycyl-histidines as novel peroxidative biocatalysts, and their catalytic performances including kinetics, heat tolerance, and freezing tolerance were analysed

Metabolites, the end products of gene expression in living organisms, are tightly correlated with an organism’s development and growth. Thus, metabolic profiling is a potentially important tool for understanding the events that have occurred in cells, tissues, and individual organisms. Here, we present a method for predicting the developmental stage of zebrafish embryos using novel metabolomic non-target fingerprints of “single-embryos”. With this method, we observed the rate of development at different temperatures. Our results suggest that this method allows us to analyse the condition, or distinguish the genotype, of singleembryos before expression of their ultimate phenotype