Volume 70, Issue 9-10

Hymenocrater longiflorus was collected from northern Iraq, and the chemical composition and antioxidant and cytotoxic activities of this plant were investigated. Ten compounds detected by HPLC-ESI/MS were identified as flavonoids and phenolic acids. The free radical scavenging activity of the 70% methanol extract was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The antioxidant activities of the extract may be attributed to its polyphenolic composition. The cytotoxicity of the plant extract against the osteosarcoma (U2OS) cell line was assessed with the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. The extract significantly reduced the viability of cells in a concentration- and time-dependent manner. Cells were arrested during the S-phase of the cell cycle, and DNA damage was revealed by antibodies against histone H2AX. The apoptotic features of cell shrinkage and decrease in cell size were also observed. Western blot analysis revealed cleavage of poly (ADP-ribose)-polymerase 1 (PARP-1), in addition to increases in the proteins p53, p21, and γ-H2AX. Collectively, our findings demonstrate that the H. longiflorus extract is highly cytotoxic to U2OS cells, most likely due to its polyphenolic composition.

The protective effects of the total glycosides from Ligustri Lucidi Fructus against nonalcoholic fatty liver (NAFL) in mice were investigated. Liver injury was induced by the administration of high fat diet for 60 days. During this period, the model group received high fat diet only; the treatment groups received various drugs plus high fat diet. Compared with the model group, the total glycosides significantly decreased the contents of triglyceride (TG) and cholesterol (TC), as well as the activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum. Moreover, the contents of TG and TC in liver tissue and the liver index were reduced. Histological findings also confirmed antisteatosis. Compared with the model group, total glycosides significantly reduced the levels of the sterol regulatory element binding protein-1c (SREBP-1c) and liver X receptor-a (LXR-α) protein, and down-regulated the expression of SREBP-1c, LXR-α and interleukin-6 (IL-6) mRNA in the liver. These results suggest that the total glycosides are effective in the treatment of NAFL of mice. Their mode of action is associated with inhibiting SREBP-1c, LXR-α and IL-6 mRNA, reducing lipid synthesis factor SREBP-1c and LXR-α protein and gene expression, suppressing inflammatory responses, then decreasing serum lipid and hepatic lipid.

Five novel Pt(II) complexes with some 2-cycloalkyl-substituted benzimidazole carrier-ligands were synthesized and evaluated for their in vitro cytotoxic activities against HeLa and OVCAR-3 cell lines. A cell viability test revealed that [dichloro-bis(2-cycloheptylbenzimidazole) platinum(II)] is less cytotoxic than cisplatin, and its cytotoxic effect can be compared with that of carboplatin. Flow cytometric analysis revealed that this complex at 117 μM concentration causes apoptosis in approx. 72 % of the OVCAR-3 cell population. In addition, the complex was found to cause an increase in the SubG1 population of both OVCAR-3 and HeLa cells and to cause less apoptosis in HeLa cells than cisplatin.

Antimicrobial peptides (AMPs) are small peptides found in many organisms defending themselves against pathogens. AMPs form the first line of host defence against pathogenic infections and are key components of the innate immune system of amphibians. In the current study, cDNAs of precursors of four novel antimicrobial peptides in the skin of Paa spinosa were cloned and sequenced using the 3′-RACE technique. Mature peptides, named spinosan A–D, encoded by the cDNAs were chemically synthesized and their chemical properties were predicted. The antimicrobial, antioxidative, cyotoxic and haemolytic activities of these four AMPs were determined. While the synthesised spinosans A–C exhibited no activity towards any of the bacterial strains tested, spinosan-D exhibited weak but broad-spectrum antimicrobial activities against Gram-positive and Gram-negative bacteria. All peptides were weakly haemolytic towards rabbit erythrocytes, had a strong antioxidative activity, and a low cytotoxic activity against HeLa cells. These findings provide helpful insights that may be useful in the future design of anti-infective peptide agents.

Astragali radix (AR), known in China as huangqi, is commonly used in traditional Chinese medicine. Water soluble extractive (WSE) values play an important role in the quality evaluation of herbal drugs. In this study, WSE of wild and cultivated AR were compared systematically. The WSE value of cultivated AR was significantly higher than that of the wild AR, and their UV-absorbance in the range of 250–400 nm was also different. The chemical compositions of different WSE were further compared by 1 H NMR spectroscopy combined with multivariate analysis. Results from the principal component analysis and the hierarchical cluster analysis showed a clear separation between the WSEs of wild and cultivated AR. The differential metabolites responsible for the separation were identified by orthogonal projections to latent structures discriminant analysis and recursive support vector machine. The WSE of wild AR contained more arginine, valine, threonine, asparagine, succinate, and glutamine, while the cultivated AR contained more sucrose. Thus, the WSE can be used as a simple and reliable method for discrimination of wild and cultivated ARs, and the results obtained in this study extend the potential use of WSE in the quality evaluation of herbal drugs.

Tree mortality caused by bark beetles has increased in recent decades in both Europe and North America. In a large recent outbreak in central Sweden the bark beetle Polygraphus poligraphus was often found together with the spruce bark beetle Ips typographus in killed trees. To increase the understanding of the aggregation behavior of P. poligraphus we used solid phase microextraction (SPME) to collect volatile organic compounds (VOCs) released from single P. poligraphus males, with and without added females, colonizing Norway spruce stem sections and analyzed the sampled compounds by combined gas chromatography and mass spectrometry (GC-MS). High amounts of terpinen-4-ol, a substance found in the hindguts of P. poligraphus males in earlier studies, were released by colonizing males. The emission of both enantiomers of terpinen-4-ol was monitored by GC-MS over time as the males aged in the absence and presence of females. Single males emitted ( R )-(–)-terpinen-4-ol for up to 60 days in high enantiomeric purity but the enantiomeric excess (ee) varied between males, and also for the same individual, over time from 96.3% to 99.3% ee. In the presence of females, males also emitted terpinen-4-ol for up to 50 days but now in lower amounts and with lower enantiomeric purity varying from 67.7% ee to 99.3% ee. Small quantities of other volatile compounds were emitted from the colonizing beetles including cis - and trans -4-thujanol, both of which were previously shown to be present in the hindguts of males. In earlier studies frontalin was found to attract P. poligraphus , but in our study it was not identified among emitted compounds from colonizing beetles.

Essential oils (EOs) obtained from two crops and populations of thujone-free cultivated Artemisia absinthium were tested against two nematode models, the mammalian parasite Trichinella spiralis , and the plant parasitic root knot nematode Meloidogyne javanica . The EOs were characterized by the presence of ( Z )-epoxyocimene and chrysanthenol as major components and showed time and population dependent quantitative and qualitative variations in composition. The EOs showed a strong ex vivo activity against the L1 larvae of the nematode Trichinella spiralis with a reduction of infectivity between 72 and 100% at a dose range of 0.5–1 mg/ml in absence of cytotoxicity against mammalian cells. Moreover, the in vivo activity of the EO against T. spiralis showed a 66% reduction of intestinal adults. However, these oils were not effective against M. javanica.