Band 67, Heft 5-6

Six new compounds, comprising three flavonoid glycosides and their respective coumaroyl esters, have been isolated and characterized from the methanol extract of the leaves of Campylospermum calanthum, along with three known flavonoid aglycones, 7-O-methyl apigenin (1), 7-O-methyl luteolin (2), and 7-O-methyl quercetin (3). Their structures were elucidated based on chemical evidence as well as spectroscopic analysis including 1D and 2D NMR ( 1 H- 1 H COSY, HSQC, HMBC, and NOESY) spectroscopy and by comparing their spectral data with those reported for related compounds

Volatile compounds of healthy and insect-damaged stems of Hippophae rhamnoides sinensis were analysed using dynamic headspace and thermal-desorption cold-trap injector gas chromatography/mass spectroscopy (TCT-GC/MS). Sixteen compounds, belonging to alkanes, alcohols, aldehydes, esters, ketones, and ethers, were identified in the stems of healthy H. rhamnoides sinensis; the compounds in H. rhamnoides sinensis occurring naturally or cultivated in plantations were similar, but the relative contents were significantly different. In plants damaged by Holcocerus hippophaecolus, the nature and content of the volatile compounds were greatly changed. Butanedione and butyl glyoxylate were newly generated after damage by the pest, and the relative levels of pentanal, heptanal, eucalyptol, terpineol, and camphor were sharply increased in both naturally occurring and plantation-grown plants. n-Decane, trans-2-nonen-1-ol, and n-hexadecane levels increased in plants cultivated in the plantation and decreased in natural forests, whereas the levels of other types were reduced. Thus, both the nature and the content of volatile compounds of H. rhamnoides sinensis are affected by H. hippophaecolus damage, providing a theoretical basis to identify the mechanism of pest destruction

Propolis, a natural bee product widely used for its antimicrobial activity, was tested against isolates of Enterococcus from humans, pig-tailed macaques, isolates of refractory endodontic treatment cases, and isolates from Lactobacillus-containing food supplements. Typification of the propolis was performed by high-performance liquid chromatography (HPLC) by which prenylated compounds, cinnamic acid derivatives, and fl avonoids were detected as the main constituents. Minimum inhibitory concentrations (MIC) were determined using the agar dilution method. All human and animal Enterococcus isolates demonstrated MIC values of 1600 μg/mL. Enterococcal species of human and animal origin were inhibited by propolis. Particularly, human isolates of E. faecium and E. faecalis of refractory endodontic treatment cases were susceptible to propolis of Brazilian origin

New 3(2H)-pyridazinone derivatives containing a N’-benzyliden-acetohydrazide moiety at position 2 were synthesized. The structures of these newly synthesized compounds were confi rmed by IR, 1 H NMR, and MS data. These compounds were tested for their antibacterial, antifungal, antimycobacterial, and cytotoxic activities. The compounds 2-[4-(4-chlorophenyl)- 6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-tert-butylbenzyliden)acetohydrazide and 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-chlorobenzyliden) acetohydrazide exhibited activity against both Gram-positive and Gram-negative bacteria. Most of the compounds were active against E. coli ATCC 35218. The preliminary results of this study revealed that some target compounds exhibited promising antimicrobial activities

The sulforhodamine B (SRB) assay was used to assess the cytotoxicity of the aqueous (AqEx) and ethanolic (AlEx) extracts, respectively, of the aerial parts of Cleome droserifolia (Forssk.) Del. against two human cancer cell lines, breast (MCF7) and colon (HCT116) adenocarcinoma. AqEx exhibited higher cytotoxic activity, thus its four subfractions, namely n-hexane (HxFr), chloroform (ClFr), ethyl acetate (EtFr), and n-butanol (BuFr) fractions, were also tested. Purifi cation of the more active ClFr and EtFr yielded nine compounds. Six terpenoids, guai-7(11),8-diene (C 1 ), 1-hydroxy-guai-3,10(14)-diene (C 2 ), 18-hydroxydollabela- 8(17)-ene (C 3 ), (24E)-stigmasta-5,8-dien-3β-ol (C 4 ), teucladiol [1α,5β-guai-10(14)- ene-4β,6β-diol] (C 5 ), and buchariol (4,10-epoxy-6α-hydroxyguaiane) (C 6 ), were isolated from ClFr and three fl avonol glycosides, isorhamnetin-3-O-β-D-glucoside (F 1 ), quercetin- 3`-methoxy-3-O-(4``-acetylrhamnoside)-7-O-α-rhamnoside (F 2 ), and kaempferol-4`-methoxy- 3,7-O-dirhamnoside (F 3 ), were isolated from EtFr. Compounds C 3 and F 2 are new in nature. The isolated compounds were identifi ed using various spectroscopic methods (UV, IR, 1H NMR,13C NMR, HMQC, HMBC, and COSY). Compounds C 1 , C 3 , F 2 , and F 3 showed significant cytotoxic activities against the two tested cell lines comparable to those of the anticancer drug doxorubicin ® . The new compound C 3 was the most active as it had the lowest IC 50 values, (1.9 ± 0.08) and (1.6 ± 0.09) μg/ml corresponding to 6.5 and 5.4 μM, against MCF7 and HCT116 cells, respectively

The n-butanolic fraction of a methanolic extract (80%) from aerial parts of Ajuga chamaecistus ssp. tomentella was analysed using different chromatographic methods. Column (CC) and high-performance liquid chromatography (HPLC) were used for isolation and purifi cation. 13 C, 1H NMR, H-H COSY, HSQC, HMBC, and ESI-MS were employed for identifi cation of the compounds isolated from this fraction. The structures of the compounds were determined to be cis-melilotoside (1), trans-melilotoside (2), lavandulifolioside (3), 20-hydroxyecdysone (4), leonoside B (5), martynoside (6), ajugalactone (7), makisterone A (8), and 24-dehydroprecyasterone (9). This is the fi rst report on the presence of cis- and transmelilotoside in Ajuga species. Cytotoxic evaluation of the n-butanolic fraction, cis- and transmelilotoside against cancer (T47D, HT-29, and Caco-2) and normal (NIH 3T3) cell lines by the mitochondrial tetrazolium test (MTT) showed no cytotoxic effects up to 400 μg/mL. The results of this study suggest that melilotoside, phenylethyl glycosides, and phytoecdysteroids are the main constituents of the n-butanolic fraction of Ajuga chamaecistus ssp. tomentella

Antioxidant and antimicrobial activities of the essential oil and n-hexane (HEE), chloroform (CHE), ethyl acetate (EAE), and methanol (MEE) extracts, respectively, from the root of Saurauia lantsangensis Hu were investigated. The GC-MS analysis revealed 39 compounds representing 96.41% of the oil containing T-muurolol (13.85%), acetophenone (7.46%), α-cadinol (6.26%), methyl palmitate (5.36%), n-hexadecanoic acid (4.31%), torreyol (3.69%), and isospathulenol (3.48%) as major components. Antioxidant activities determined by three various testing systems, i. e. DPPH radical scavenging, superoxide anion radical scavenging, and reducing power assay, increased in the order: HEE < CHE < oil < MEE < EAE. CHE, EAE, MEE and oil exhibited a promising antimicrobial effect determined as the diameter of zones of inhibition (13.3 - 16.2, 16.5 - 20.4, 13.5 - 16.6, and 16.5 - 22.7 mm), respectively, along with their respective MIC values (500 - 1000, 125 - 500, 250 - 500, and 250 - 500 μg/ml) against Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli), Gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus), and a yeast (Hansenula anomala).

Five flavonoids (rutin, asebotin, 3-hydroxyasebotin, quercetin-3-O-β-D-xylopyranoside, and a racemic mixture of catechin) and caffeic acid were isolated and identified for the first time from seagrass, Thalassodendron ciliatum, collected from the Hurghada region in Egypt. The crude extract and the isolated pure compounds were evaluated for their cytotoxic activities against HCT-116, HEPG, MCF-7, and HeLa human cancer cell lines, for their antiviral activity against Herpes Simplex and hepatitis A viruses, and for their antioxidant activity

Doxorubicin (DOX) is an anthracycline antibiotic widely used as a chemotherapeutic agent in the treatment of several tumours. However, its cardiac toxicity limits its use at maximum therapeutic doses. Most studies implicated increased oxidative stress as the major determinant of DOX cardiotoxicity. The local Saudi flora is very rich in a variety of plants of quite known folkloric or traditional medicinal uses. Tribulus macropterus Boiss., Olea europaea L. subsp. africana (Mill.) P. S. Green, Tamarix aphylla (L.) H. Karst., Cynomorium coccineum L., Cordia myxa L., Calligonum comosum L’ Hér, and Withania somnifera (L.) Dunal are Saudi plants known to have antioxidant activities. The aim of the current study was to explore the potential protective effects of methanolic extracts of these seven Saudi plants against DOX-induced cardiotoxicity in rats. Two plants showed promising cardioprotective potential in the order Calligonum comosum > Cordia myxa. The two plant extracts showed potent in vitro radical scavenging and antioxidant properties. They significantly protected against DOX-induced alterations in cardiac oxidative stress markers (GSH and MDA) and cardiac serum markers (CK-MB and LDH activities). Additionally, histopathological examination indicated a protection against DOX-induced cardiotoxicity. In conclusion, C. comosum and C. myxa exerted protective activity against DOX-induced cardiotoxicity, which is, at least partly, due to their antioxidant effect

Environmental pollution by pesticide residues is a major environmental concern due to the extensive use of these substances in agriculture. The insecticide β-cyfluthrin is a synthetic pyrethroid widely used in agricultural and other domestic activities. The aim of the present study was to assess the genotoxic effects of a sublethal exposure of the fish Bryconamericus iheringii (Characidae) to a commercial formulation of β-cyfl uthrin using the comet assay. Fish were exposed to sublethal concentrations (4.2 and 5.6 μg/L) of β-cyfluthrin under static conditions during 24- and 48-h exposure periods. Fish in tap water were used as negative controls. Results obtained by the comet assay revealed genotoxic effects of the pyrethroid in the higher concentration and at the longer exposure period. The mean DNA damage index of fish exposed to 5.6 μg/L β-cyfluthrin for 48 h was significantly higher (145.9 ± 51.8) than in the control group (69.3 ± 39.5). These findings indicate that native fi sh species might be at risk for genotoxic damage in waters contaminated with β-cyfluthrin

Polyethylene glycol (PEG) conjugation technology has been successfully applied to improve the performance of protein drugs. In this study, L-asparaginase was N-terminal sitespecifically modified by alkylating PEG with monomethoxy polyethylene glycol-propionaldehyde (mPEG-ALD 20000 ). The optimum reaction parameters were determined as pH 5.0, a molar ratio of mPEG-ALD 20000 to L-asparaginase of 10:1, a reaction time of 16 h and temperature of 25 °C. PEG-L-asparaginase (PEG-L-ASNase) was isolated and purified with consecutive anion-exchange (XK, 16 × 20 cm, Q Sepharose FF) and gel-filtration (Tricorn, 10 × 600 cm, Sephacryl S-300 HR) chromatography, respectively. PEG-L-ASNase retained 43.5% of its activity and the N-terminal amino groups were modified to an extent of 3.67%

We studied the metabolic fate of [carbonyl- 14 C]nicotinamide and [8- 14 C]adenine in segments taken from young and developing leaves, stem, hypocotyls, and roots of a shoot-root type emerging propagule of the mangrove plant Bruguiera gymnorrhiza. Thin-layer chromatography was used together with a bioimaging analyser system. During 4 h of incubation, incorporation of radioactivity from [carbonyl- 14 C]nicotinamide into NAD and trigonelline was found in all parts of the propagules; the highest incorporation rates into NAD and trigonelline were found in newly emerged stem and young leaves, respectively. Radioactivity from [8- 14 C]adenine was distributed mainly in the salvage products (adenine nucleotides and RNA), and incorporation was less in catabolites (allantoin, allantoic acid, and CO 2 ). Adenine salvage activity was higher in young leaves and stem than in hypocotyls and roots. Over a short time, the effect of 500 mM NaCl on nicotinamide and adenine metabolism indicated that NaCl inhibits both salvage and degradation activities in roots

Translation elongation factor 1A (eEF1A) is a factor critically involved in the process of protein synthesis. The activity of eEF1A has been shown by several studies to be regulated by post-translational modifi cations such as phosphorylation and dephosphorylation. However, until now less research has focused on other post-translational modifi cations of eEF1A, especially acetylation. In this report, we provide new evidence for the existence of eEF1A acetylation in PLC5 cells by immunoprecipitation and Western blotting. Using the histone deacetylase (HDAC) inhibitor trichostatin A (TSA), we found that the deacetylation of eEF1A is mainly attributable to classes I and II HDAC rather than class III HDAC, and, furthermore, that the antitumour agent etoposide phosphate (VP 16) enhances the acetylation of eEF1A in a synergistic way with TSA. Our data suggest the possibility that the increased acetylation of eEF1A could be a new mechanism for the antitumour effect of etoposide

Adults of Papilio protenor demetrius emit a faint odour; the male odour is notably stronger than that of the females. The extracts of whole individuals of each sex comprised 53 compounds regarded as cuticular lipid components, of which the 17 major compounds were straight-chain alkanes and alkenes with 23 - 31 carbon atoms, higher fatty acids, long-chain aliphatic ketones, squalene, and cholesterol. However, highly volatile compounds were not detected in the whole individual extracts. Eight of the 17 major compounds showed a significant sex difference in relative abundance per individual. Principal component analysis, using the major compounds as variables, revealed a marked sexual dimorphism in the chemical composition of cuticular lipids. From the extracts of 10 dissected individuals of each sex, 21 highly volatile compounds were identified in amounts of less than 200 ng/individual. Among them, linalool and 2,3-butanediol showed a significantly larger amount in males than in females, indicating that the adult odour is also sexually dimorphic. Moreover, both sexes shared several odoriferous compounds, such as heptanal, nonanal, methyl salicylate, benzyl alcohol, and benzoic acid. The faint odour of P. protenor adults, perceivable by the human nose, appears to originate from these volatile compounds

Cyclin-dependent kinases (CDKs) are serine/threonine kinases that play critical roles in the cell cycle regulation. Herein, we describe the identifi cation of a CDK gene from Apis cerana cerana, named AccCDK6. The full-length cDNA is 1,778 bp long, including an ORF of 1,380 bp that encodes a polypeptide of 459 amino acid residues. Multiple sequence alignment analysis showed that the predicted AccCDK6 sequence shares a high similarity with CDK6 genes of other species, and this protein may share an evolutionary predecessor with Drosophila CDK4. The expression patterns of the gene were also analysed, and the transcript was detected throughout the larval, pupal, and adult developmental stages. Furthermore, the expression level of the mRNA of the gene in adult workers was infl uenced by H 2 O 2 , ultraviolet (UV) light, temperature (42°C), HgCl 2 , and pyriproxyfen. These results indicate that AccCDK6 responds to multiple environmental stresses and may also participate in intracellular reactions of reactive oxygen species (ROS) and development processes in honey-bees