Chlorpyrifos stimulates ABCC-mediated transport in the intestine of the rainbow trout Oncorhynchus mykiss.

The organophosphorus pesticide chlorpyrifos, detected in water and food worldwide, has also been found in the Río Negro and Neuquén Valley, North Patagonia, Argentina, where the rainbow trout, Oncorhynchus mykiss, is one of the most abundant fish species. We analyzed whether chlorpyrifos affects the transport activity of the ATP-binding cassette protein transporters from the subfamily C (ABCC), which are critical components of multixenobiotic resistance. We exposed ex vivo O.

Synthesis, antitumor activity, 3D-QSAR and molecular docking studies of new iodinated 4-(3)-quinazolinones 3-substituted.

A novel series of 6-iodo-2-methylquinazolin-4-(3)-one derivatives, 3a-n, were synthesized and evaluated for their cytotoxic activity. Compounds 3a, 3b, 3d, 3e, and 3h showed remarkable cytotoxic activity on specific human cancer cell lines when compared to the anti-cancer drug, paclitaxel. Compound 3a was found to be particularly effective on promyelocytic leukaemia HL60 and non-Hodgkin lymphoma U937, with IC values of 21 and 30 μM, respectively.

Consecutive emamectin benzoate and deltamethrin treatments affect the expressions and activities of detoxification enzymes in the rainbow trout (Oncorhynchus mykiss).

Rainbow trout (Oncorhynchus mykiss) subjected to three consecutive, alternating treatments with emamectin benzoate (EMB) and deltamethrin (DM) during outbreaks of Caligus rogercresseyi in a farm located in southern Chile (Hornopiren, Chiloé), were studied to determine the effects of these treatments on the protein and enzymatic activity levels of cytochrome P450 1A (CYP1A), flavin-containing monooxygenase (FMO) and glutathione S-transferase (GST) in different tissues. Consecutive and alternating EMB/DM treatments resulted in a 10-fold increase and 3-fold decrease of CYP1A protein levels in the intestine and gills, respectively. Notably, CYP1A activity levels decreased in most of the analyzed tissues.

P-glycoprotein expression and pharmacological modulation in larval stages of Echinococcus granulosus.

P-glycoprotein (Pgp) is an ATP-dependent transporter involved in the efflux of a wide variety of lipophilic substrates, such as toxins and xenobiotics, out of cells. Pgp expression level is associated with the ineffective therapeutic treatment of cancer cells and microbial pathogens which gives it high clinical importance. Research on these transporters in helminths is limited.

2-[2-(4-Acetyl-phen-yl)hydrazinyl-idene]-1,3-diphenyl-propane-1,3-dione.

In the title compound, C(23)H(18)N(2)O(3), the inter-planar angle between the benzoyl units is 80.51 (6)° while the dihedral angles between the hydrazinyl-idene and benzoyl groups are 43.43 (6) and 54.

[Study of resistance to chemotherapy mediated by ABC transporters in biopsies of glioblastoma multiforme].

Background: Mortality rate is dramatically high in high grade brain tumors. The presence of multiple drug resistance transporters in glioblastoma multiforme, has contributed largely to the poor efficacy of targeted therapy against cancer in the central nervous system.

Aim: To analyze the percentage of survival and mortality of patients with glioblastoma multiforme in a cohort of patients in Chile and to co-rrelate the chemo-resistance of these cells with the expression level of multiple drug resistance transporters.

A second monoclinic polymorph of 2-[2-(4-meth-oxy-phen-yl)hydrazinyl-idene]-1,3-diphenyl-propane-1,3-dione.

The title compound, C(22)H(18)N(2)O(3) is the second monoclinic polymorph (P2(1)/c) of the compound, the first being reported in space group P2(1) [Bertolasi et al. (1993 ▶). J.

2-[2-(3-Chloro-phen-yl)hydrazinyl-idene]-1,3-diphenyl-propane-1,3-dione.

The mol-ecular structure of the title compound, C(21)H(15)ClN(2)O(2), features one strong intra-molecular N-H⋯O resonance-assisted hydrogen bond (RAHB). In the crystal, mol-ecules form inversion-related dimers via pairs of weak inter-molecular N-H⋯O contacts. These dimers are further stabilized via three weak C-H⋯O contacts, developing the three-dimensional structure.

2-[2-(4-Bromo-phen-yl)hydrazinyl-idene]-1,3-diphenyl-propane-1,3-dione.

The conformation of the title mol-ecule, C(21)H(15)BrN(2)O(2), is stabilized by a weak intra-molecular C-H⋯N hydrogen bond and a strong resonance-assisted N-H⋯O intra-molecular hydrogen bond. In the crystal, the mol-ecules are linked by weak inter-molecular C-H⋯O inter-actions, forming zigzag chains along the b axis.

Combined use of anticancer drugs and an inhibitor of multiple drug resistance-associated protein-1 increases sensitivity and decreases survival of glioblastoma multiforme cells in vitro.

Glioblastoma multiforme (GBM) is a brain tumour characterised by a remarkably high chemoresistance and infiltrating capability. To date, chemotherapy with temozolomide has contributed only poorly to improved survival rates in patients. One of the most important mechanisms of chemoresistance comes about through the activity of certain proteins from the ATP-binding cassette superfamily that extrudes antitumour drugs, or their metabolites, from cells.

Effect of tacrolimus on activity and expression of P-glycoprotein and ATP-binding cassette transporter A5 (ABCA5) proteins in hematoencephalic barrier cells.

Tacrolimus is an agent used in clinical immunosuppressive drug therapies. A wide spectrum of adverse effects has been reported in association with this immunosuppressor, including neurotoxic effect. The upper limit of therapeutic blood concentrations of tacrolimus has been described as 30 ng/ml in immunosuppressed patients.