Substance P/NK1R antagonistic effect of 17-Trifluoromethyl phenyl trinor prostaglandin F2α in Breast cancer

17-Trifluoromethyl phenyl trinor prostaglandin F2α (17-TPGF2α) is extracted from Zinc data base, but its value for inhibiting breast cancer through SP/NK1R system remains unknown. This study was designed to investigate the potential antagonist effect of 17-TPGF2α through NK1Receptor. The effect of 17-TPGF2α on the proliferation and apoptosis of breast cancer cell lines were determined through invitro cell lines. Based on invitro results we planned to investigate anticancer activity in Female Balb/c and used SC injection of DMBA for cancer induction. Oral administration of 17-TPGF2α significantly suppress the tumor volume as compared with an untreated group. The serum parameters like ALP, AST and ALT and haematological parameters were normalized in test treated group. Histological examination revealed normal histoarchitecture of mammary gland and focal areas showed minimal inflammatory cell infiltration. There is no necrosis is seen both test treated and standard treated group when compared with Disease group. All these findings concluded that 17-TPGF2α may have potential as a novel antitumor candidate for breast cancer.

Chitosan and Lemon Extract Applied during Giuncata Cheese Production to Improve the Microbiological Stability

In this study, lemon extract and chitosan were used as antimicrobial agents during Giuncata cheese production in order to assess whether the natural compounds would improve the cheese’s microbial quality. In particular, the viable cell concentration of the main spoilage microbial growth (Pseudomonas spp. and total coliforms) was monitored during refrigerated storage at 4 °C. A central composite design (CCD) was adopted to highlight a possible synergic effect of the two selected compounds. The results showed that a decrease in the cell growth rate of the monitored spoilage microorganisms was observed for all cheese samples added with active agents, when compared with the control cheese. Despite the recorded antimicrobial activity, an antagonist effect was detected when the two compounds were combined at the highest concentrations. In fact, the best performance was obtained when the lemon and the chitosan were used individually at concentrations of 500 and 60 ppm, respectively.

Influence of Molybdenum in Drinking Water or Feed on Copper Metabolism in Cattle—A Review

The majority of Mo research has focused on the antagonist effect of Mo, alone or in combination with elevated dietary S, on Cu absorption and metabolism in ruminants. Diets containing both >5.0 mg of Mo/kg DM and >0.33% S have been reported to reduce the Cu status in cattle and sheep. Therefore, due to the potential for inducing Cu deficiency, Mo and S concentrations in the diet should be monitored and kept within appropriate values. Elevated sulfate concentrations in drinking water can also be detrimental to livestock production, especially in ruminants. High concentrations of sulfate in water have been extensively studied in cattle because high-sulfate water induces polioencephalomalacia in ruminants. However, little research has been conducted investigating the impact of Mo in water on Cu metabolism in ruminants. Based on the limited number of published experiments, it appears that Mo in drinking water may have a lower antagonistic impact on the Cu status in cattle when compared to Mo consumed in the diet. This response may be due to a certain percentage of water bypassing the rumen when consumed by ruminants. Therefore, the objective of this review was to examine the impact of Mo in drinking water on cattle performance and Mo and Cu metabolism.

In Vitro and In Silico Characterization of G-Protein Coupled Receptor (GPCR) Targets of Phlorofucofuroeckol-A and Dieckol

Phlorotannins are polyphenolic compounds in marine alga, especially the brown algae. Among numerous phlorotannins, dieckol and phlorofucofuroeckol-A (PFF-A) are the major ones and despite a wider biological activity profile, knowledge of the G protein-coupled receptor (GPCR) targets of these phlorotannins is lacking. This study explores prime GPCR targets of the two phlorotannins. In silico proteocheminformatics modeling predicted twenty major protein targets and in vitro functional assays showed a good agonist effect at the α2C adrenergic receptor (α2CAR) and an antagonist effect at the adenosine 2A receptor (A2AR), δ-opioid receptor (δ-OPR), glucagon-like peptide-1 receptor (GLP-1R), and 5-hydroxytryptamine 1A receptor (5-TH1AR) of both phlorotannins. Besides, dieckol showed an antagonist effect at the vasopressin 1A receptor (V1AR) and PFF-A showed a promising agonist effect at the cannabinoid 1 receptor and an antagonist effect at V1AR. In silico molecular docking simulation enabled us to investigate and identify distinct binding features of these phlorotannins to the target proteins. The docking results suggested that dieckol and PFF-A bind to the crystal structures of the proteins with good affinity involving key interacting amino acid residues comparable to reference ligands. Overall, the present study suggests α2CAR, A2AR, δ-OPR, GLP-1R, 5-TH1AR, CB1R, and V1AR as prime receptor targets of dieckol and PFF-A.

A Comparative Study of Human and Zebrafish Pregnane X Receptor Activities of Pesticides and Steroids Using In Vitro Reporter Gene Assays

The nuclear receptor pregnane X receptor (PXR) is a ligand-dependent transcription factor that regulates genes involved in xenobiotic metabolism in mammals. Many studies suggest that PXR may play a similar role in fish. The interaction of human PXR (hPXR) with a variety of structurally diverse endogenous and exogenous chemicals is well described. In contrast, little is known about the zebrafish PXR (zfPXR). In order to compare the effects of these chemicals on the PXR of these two species, we established reporter cell lines expressing either hPXR or zfPXR. Using these cellular models, we tested the hPXR and zfPXR activity of various steroids and pesticides. We provide evidence that steroids were generally stronger activators of zfPXR while pesticides were more potent on hPXR. In addition, some chemicals (econazole nitrate, mifepristone, cypermethrin) showed an antagonist effect on zfPXR, whereas no antagonist chemical has been identified for hPXR. These results confirm significant differences in the ability of chemicals to modulate zfPXR in comparison to hPXR and point out that zfPXR assays should be used instead of hPXR assays for evaluating the potential risks of chemicals on aquatic species.

Indoor pet allergen exposures modify the effects of chemical air pollutants on respiratory symptoms

SETTING: Indoor volatile organic compound (VOC) levels, which are generally correlated with each other, may have an additive or synergistic effect on health. VOC synergy with allergens is a suspected mechanism affecting respiration.OBJECTIVE: To determine the effect of exposure to interactions between VOCs and allergens on respiratory symptoms in individuals aged ≥15 years.DESIGN: A national cross‐sectional survey measured 20 VOCs and dog and cat aeroallergens in 490 main residential dwellings in France. A standardised questionnaire was used to elicit responses on respiratory conditions in 1012 inhabitants. Four VOC factor scores (linear combinations of VOCs) were generated using principal component analysis. In order to take into account the phenomenon of multi‐pollution, marginal models were used to model the relationships between exposure to VOC mixture and respiratory conditions. Stratified models were used to examine the interaction between allergens and VOCs.RESULTS: The aromatic hydrocarbon score was associated with rhinitis and wheezing, the aliphatic hydrocarbon score with asthma and cough, the halogenated hydrocarbons with asthma, wheezing and rhinitis. Aldehydes and Can f1 had a significant synergistic effect on wheezing and rhinitis. Aliphatic hydrocarbons had an antagonist effect with Can f1 on wheezing.CONCLUSION: Our data support evidence of adverse effects of exposure to VOC mixture on respiratory conditions; this effect is aggravated in the presence of pet allergens.