Effect of Cynomorium total flavone on depression model of perimenopausal rat

PurposeTo observe the effect of cynomorium total flavone on the depression model of perimenopausal rat and to analyze the action characteristics of cynomorium total flavone on depression of rat with perimenopausal syndrome.MethodDuplicate the model of rat with perimenopausal depression based on the combined method of incomplete castration and chronic stimulation, and keep drug administration for 35d. And then measure related behavior indicators and the change of biochemical index level in serum and brains; measure the estrogen/androgen receptor (ER/AR) in related tissues and the ERmRNA expression in hypothalamus.ResultIt can be seen that cynomorium total flavone can significantly improve the behavior indicators of rat with perimenopausal depression; obviously or significantly change the level of related biomedical indexes in serum and brains of perimenopausal depressed rat; obviously or significantly increase the expression of ER/AR in related tissues of perimenopausal depressed rat; obviously or significantly increase the ERmRNA expression in hypothalamus.ConclusionCynomorium total flavone can adjust hypothalamic-pituitary-gonadal axis by increasing E2, and make related biomedical indexes and hormone receptors tend to be normal, so as to relieve perimenopausal syndrome and perimenopausal syndrome with depression.     

The effects of unilateral antennectomy on the flight behaviour of male Heliothis virescens in a pheromone plume

Abstract .Unilaterally antennectomized Heliothis virescens (F.) males flying close to the central axis of a plume of sex pheromone display no significant differences in behaviour compared to sham-operated males in course angles, track angles, airspeed and groundspeed. This demonstrates that right/left antennal information is not necessary for normal orientation movements in response to pheromone, but rather that it is 'blended' within the moth's central nervous system before pheromone-mediated manoeuvres are made. However, some unilaterally antennectomized moths (36%) make repetitive, asymmetrical, saw-tooth-shaped tracks during pheromone-mediated upwind progress, whereas control moths never make such tracks. Unilaterally antennectomized moths made such tracks on the side of the plume contralateral to the missing antenna. We hypothesize that these occasional asymmetrical tracks in unilaterally ablated males are the result of reiterative asymmetrical pheromone stimulation of a higher probability on track legs going toward rather than away from the long axis of the plume on males with a single antenna remaining on the 'away from axis' side. Combined with a greater propensity for treated moths to lock onto the plume away from the central axis on one side rather than the other, repetitive successive asymmetrical track legs (resulting in a saw-tooth-shaped track) are commonly observed in these moths. Control moths do also make asymmetric successive track legs but they rarely are repeated and thus are not readily observed.     

A novel Golgi mannosidase inhibitor: Molecular design,synthesis, enzyme inhibition,and inhibition of spheroid formation

Effective chemotherapy for solid cancers is challenging due to a limitation in permeation that prevents anticancer drugs from reaching the center of the tumor, therefore unable to limit cancer cell growth. To circumvent this issue, we planned to apply the drugs directly at the center by first collapsing the outer structure. For this, we focused on cell–cell communication (CCC) between N-glycans and proteins at the tumor cell surface. Mature N-glycans establish CCC; however, CCC is hindered when numerous immature N-glycans are present at the cell surface. Inhibition of Golgi mannosidases (GMs) results in the transport of immature N-glycans to the cell surface. This can be employed to disrupt CCC. Here, we describe the molecular design and synthesis of an improved GM inhibitor with a non-sugar mimic scaffold that was screened from a compound library. The synthesized compounds were tested for enzyme inhibition ability and inhibition of spheroid formation using cell-based methods. Most of the compounds designed and synthesized exhibited GM inhibition at the cellular level. Of those, AR524 had higher inhibitory activity than a known GM inhibitor, kifunensine. Moreover, AR524 inhibited spheroid formation of human malignant cells at low concentration (10 µM), based on the disruption of CCC by GM inhibition.     

A comparative study of sex pheromone reception in the Hadeninae (Lepidoptera: Noctuidae)

Abstract A comparative study of the olfactory responses to pheromone compounds was performed in twenty-four species of Hadeninae. Electroantennograms (EAG) were recorded on male moths in response to thirty compounds and the response profiles of each species were analysed by factorial correspondence analysis. A limited number of molecules were found active and the most effective stimuli were Z9 tetradecenes and Z11 hexadecenes. The species of the Mythimna genus were most sensitive to aldehydes. Tholera decimalis did not respond to any of the molecules tested. The species belonging to the Mamestra and the Orthosia genera responded to a variety of molecules and no simple correlation was found between the genus and the EAG sensibility. Pheromone reception is discussed in relation to the taxonomy and the evolution of olfactory communication in Hadeninae.     

Response of the sandfly Lutzomyia longipalpis to an oviposition pheromone associated with conspecific eggs

Response of female Lutzomyia longipalpis Lutz & Neiva (Diptera: Psychodidae) to an oviposition attractant and/or stimulant associated with conspecific eggs was investigated in the laboratory. Females of two populations laid significantly higher mean number of eggs on sites with 160 eggs already present than on bare control sites. This response was lost when eggs placed on test sites were previously washed in organic solvents and distilled water. Age of eggs placed on test sites, 1-6 days after being laid, did not seem to affect the oviposition response of the females. Comparing effects of different numbers of eggs, positive responses were obtained when 80, 160 or 320 eggs were placed on test sites. No significant differences between mean egg numbers laid on test sites and controls were detected when batches of only 20 or 40 eggs were used.     

Early environment influences later performance in fishes

Conditions fish encounter during embryogenesis and early life history can leave lasting effects not only on morphology, but also on growth rate, life‐history and behavioural traits. The ecology of offspring can be affected by conditions experienced by their parents and mother in particular. This review summarizes such early impacts and their ecological influences for a variety of teleost species, but with special reference to salmonids. Growth and adult body size, sex ratio, egg size, lifespan and tendency to migrate can all be affected by early influences. Mechanisms behind such phenotypically plastic impacts are not well known, but epigenetic change appears to be one central mechanism. The thermal regime during development and incubation is particularly important, but also early food consumption and intraspecific density can all be responsible for later life‐history variation. For behavioural traits, early experiences with effects on brain, sensory development and cognition appear essential. This may also influence boldness and other social behaviours such as mate choice. At the end of the review, several issues and questions for future studies are given.     

Deposition and longevity of oviposition-deterring pheromone in the cabbage seed weevil

Abstract The cabbage seed weevil ( Ceutorhynchus assimilis Payk.) lays eggs singly into pods of oilseed rape ( Brassica napus L.) through punctures bored with the mouthparts, preferring pods not recently used for oviposition. A simple new choice test has been used to test individual components of egg-laying behaviour for their effect on oviposition site selection. It is confirmed that an oviposition-deterring pheromone (ODP) is deposited during abdomen brushing of the pod which follows egg-laying. Neither pin punctures, weevil feeding punctures, oviposition punctures nor eggs had any deterrent effect. Pods walked on by female weevils were not avoided by those laying eggs. Observations suggest that the ODP is sensed by contact chemoreceptors on the antennae. The deterrent effect lasted only 1–2 h. The implications of these findings on the adaptive significance of the pheromone and its possible use in pest control are discussed.     

The influence of age and sex on phagocyte chemiluminescence

The process of ageing is associated with increased susceptibility to infection. Phagocytes form the primary defence mechanism against infecting microorganisms, but the influence of ageing on phagocyte function remains controversial. In this study we have applied a microtitre plate phagocyte chemiluminescence (CL) assay suitable for clinical use to compare phagocyte oxidative metabolism in younger healthy subjects (age 20–60 years) and healthy older (60–70 years) subjects. Polymorphonuclear leukocytes (PMNL) and monocytes were stimulated using phorbol myristate acetate (PMA), serum opsonized zymosan (SOZ), and non-opsonized zymosan (ZYM) in the presence of both lucigenin and luminol. Monocytes showed a higher luminolenhanced CL response to PMA in males compared with females in the younger age group. No PMNL differences were observed between the sexes. Although no difference were found in relation to age when cells were stimulated with PMA and SOZ, significantly lower background (unstimulated) CL was obtained from PMNL with luminol. PMNL luminol-enhanced CL responses were also lower in response to ZYM. The findings suggest a reduced response of PMNL from older subjects to minimal stimulation. This could be related to abnormalities in the triggering of the respiratory burst or myeloperoxidase release due to ageing. The influence of age and sex should be taken into account in clinical studies of phagocyte CL.     

Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk

The non-receptor tyrosine kinase Syk (spleen tyrosine kinase) is a pharmaceutical relevant target because its over-activation is observed in several autoimmune diseases, allergy, and asthma. Here we report the identification of two novel inhibitors of Syk by high-throughput docking into a rare C-helix-out conformation published recently. Interestingly, both compounds are slightly more active on ZAP70 (Zeta-chain-associated protein kinase 70), which is the kinase closest to Syk in the phylogenetic tree of human kinases. Taken together, the docking pose and experimental results suggest that the higher affinity of the inhibitors for ZAP70 than Syk originates from a more populated C-helix-out conformation in ZAP70. The latter observation is congruent with the 100-fold lower intrinsic activity of ZAP70 than Syk, as the C-helix-out conformation is inactive. The pharmacophore features of DFG-in, C-helix-out compounds are analyzed in relation to DFG-out inhibitors.