Anti-inflammatory activity of a lipid fraction (lyprinol) from the NZ green-lipped mussel

Abstract  A lipid-rich extract, preparared by supercritical fluid extraction of fresh stabilized mussel powder (Lyprinol), showed significant anti-inflammatory (AI) activity given therapeutically and prophylactically po to Wistar and Dark Agouti rats developing either (a) adjuvant-induced polyarthritis or (b) collagen(II)-induced autoallergic arthritis, with ED50≤15 mg/kg; c.f. naproxen≥25 mg/kg or various therapeutic oils (flaxseed, evening primrose, fish)≥1800 mg/kg given orally. Lyprinol showed little or no activity in acute irritation assays (carrageenan, kaolin, histamine) indicating it is not mimicking rapid-acting NSAIDs. Incorporating Lyprinol into arthritigenic adjuvants composed of heat-killed Mycobacterium. tuberculosis suspended in olive oil or squalane, effectively prevented arthritis development at a dose of 5 mg/rat. By contrast, ‘dummy adjuvants’ prepared with Mycobacterium tuberculosis and flaxseed, evening primrose or fish oils were still arthritigenic in Dark Agouti rats (doses of oil=90 mg/rat).

Antifeedants in the Feces of the Pine Weevil Hylobius abietis: Identification and Biological Activity

Abstract  Egg-laying females of the pine weevil, Hylobius abietis (L.), regularly deposit feces adjacent to each egg. Egg cavities are gnawed in the bark of roots of recently dead conifer trees. After egg deposition, the cavity is sealed by feces and a plug of bark fragments. Root bark containing egg cavities with feces is avoided as food by pine weevils, which indicates the presence of natural antifeedants. Here we present the first results of the isolation and chemical analyses of antifeedant compounds in the feces of H. abietis. In feeding bioassays, methanol extracts of the feces revealed strong antifeedant properties. Methanol extracts were fractionated by medium-pressure liquid chromatography and the antifeedant effects were mainly found in the fractions of highest polarity. Volatile compounds in the active fractions were identified by gas chromatography–mass spectrometry (GC–MS) and the nonvolatile compounds were characterized by pyrolysis–GC–MS. Based on mass spectra, a number of compounds with various chemical structures were selected to be tested for their antifeedant properties. Antifeedant effects were found among compounds apparently originating from lignin: e.g., a methylanisol, guaiacol, veratrol, dihydroxybenzenes, and dihydroconiferyl alcohol. A weak effect by fatty acid derivatives was found. The types of naturally occurring antifeedant compounds identified in this study may become useful for the protection of planted conifer seedlings against damage by H. abietis.

Antifeedant activity and toxicity of leaf extracts from Porteresia coarctata Takeoka and their effects on the physiology of Spodoptera litura (F.)

Abstract  Antifeeding and toxic effects of chemical extracts from Porteresia coarctata Takeoka on the insect pest Spodoptera litura (F.) were investigated in the laboratory. Hexane extracts of P. coarctata leaves were re-dissolved in dimethyl sulfoxide and applied in water to leaves of Ricinus communis L. (castor). A concentration of 1,000 and 2,000 ppm extract exhibited significant antifeeding and toxic effects to third instar larvae when compared to the same concentration of dimethyl sulfoxide in water as control. One day after feeding on extract-treated castor leaves, the mortality of S. litura larvae was 50%. Mortality increased to 95% after 11 days at a dosage of 2,000 ppm. Compared to the control, third instar larvae fed on castor leaves treated with P. coarctata leaf extract at different concentrations showed significant reduction in protein and DNA content in the fat body and midgut tissues. Results demonstrate the insecticidal and antifeedant properties of P. coarctata leaf extract against the generalist pest S. litura leading to biochemical changes in the insect body. Thus, P. coarctata contains phytochemicals, and the extract, in crude and pure form, has potential as a botanical insecticide in alternative control strategies against Lepidoptera pests.

Antidiabetic effect of novel modulating peptides of G-protein-coupled kinase in experimental models of diabetes

AbstractAims/hypothesis  G-protein-coupled receptor kinases (GRKs) play a key role in agonist-induced desensitisation of G-protein-coupled receptors (GPCRs) that are involved in metabolic regulation and glucose homeostasis. Our aim was to examine whether small peptides derived from the catalytic domain of GRK2 and -3 would ameliorate Type 2 diabetes in three separate animal models of diabetes.

Antidiabetic actions of estrogen: Insight from human and genetic mouse models

Abstract  There is increasing evidence both in humans and rodents linking the endogenous estrogen 17β-estradiol (E2) to the maintenance of glucose homeostasis. Postmenopausal women develop visceral obesity and insulin resistance and are at increased risk for type 2 diabetes mellitus, but hormone replacement therapy leads to a reduction in the incidence of diabetes. In various spontaneous rodent models of type 2 diabetes, female rodents are protected against hyperglycemia unless they are ovariectomized, and E2 perfusion reverses diabetes in male rodents. Finally, the study of transgenic mice and mice with genetic alteration of E2 secretion or E2 action has shed light on the antidiabetic properties of E2 at a tissue-specific level. Thus, E2 secretion and action in rodents seems to be implicated 1) in adipose tissue biology and the prevention of obesity, 2) in the stimulation of liver fatty acid metabolism and suppression of hepatic glucose production, and 3) in the protection of pancreatic β-cell function/survival and insulin secretion in conditions of oxidative stress.

Anti-cyanobacterial fatty acids released from Myriophyllum spicatum

Abstract  This study was carried out to identify unknown allelochemicals released from Myriophyllum spicatum and to investigate their anti-cyanobacterial effects. A series of analyses of culture solutions and methanol extracts of M. spicatum using gas chromatograph equipped with a mass selective detector revealed that M. spicatum released fatty acids, specifically, nonanoic, tetradecanoic, hexadecanoic, octadecanoic, and octadecenoic acids. Nonanoic, cis-6-octadecenoic, and cis-9-octadecenoic acids significantly inhibited growth of Microcystis aeruginosa, whereas tetradecanoic, hexadecanoic, and octadecanoic acids did not show any effect. When the inhibitory effect of nonanoic acid was compared with those of 4 polyphenols and eugeniin, which are anti-cyanobacterial compounds previously reported to be released by M. spicatum, nonanoic acid was found to be the most inhibitory to M. aeruginosa. These results indicate that not only polyphenols and eugeniin but also fatty acids such as nonanoic acid must be studied to reveal how M. spicatum exerts its allelopathic effect on M. aeruginosa.

Antibacterial activity of a bacteriocin-like substance produced by Bacillus sp. P34 that targets the bacterial cell envelope

Abstract  The objective of this study was to investigate the mode of action of BLS P34, a bacteriocin-like substance (BLS) produced by a novel Bacillus sp. strain P34 isolated from the Amazon basin. The effect of the BLS was tested against Listeria monocytogenes, showing a bactericidal effect at 200 AU (activity units) ml−1, while no inhibition of spore outgrowth of Bacillus cereus was observed with a dose of 1,600 AU ml−1. Growth of Escherichia coli and Salmonella Enteritidis was inhibited, but only when the chelating agent EDTA was co-added with the BLS. The effect of BLS P34 on L. monocytogenes was also investigated by Fourier transform infrared spectroscopy. Treated cells showed an important frequency increase in 1,452 and 1,397 cm−1 and decrease in 1,217 and 1,058 cm−1, corresponding assignments of fatty acids and phospholipids. Transmission electron microscopy showed damaged cell envelope and loss of protoplasmic material. BLS P34 was bactericidal to Gram-positive, and also showed inhibitory effect against Gram-negative bacteria. There is evidence that its mode of action corresponds to that of a membrane-active substance. The knowledge about the mode of action of this BLS is essential to determine its effective application as an antimicrobial agent.