Antiproliferative Effects of and Venom Peptides on Glioblastoma Cell Lines.

This study explores the potential of natural bioactive peptides from animal venoms as targeted anti-cancer agents with reduced toxicity. Initially, we screened a broad collection of animal venoms for their antiproliferative activity against cancer cell lines. From this collection, we selected venoms from and due to their promising activity.

Screening of antimicrobial activity in venom: Exploring key parameters.

The escalating challenge of antibiotic resistance significantly threatens global health, underscoring the critical need for new antimicrobial agents. Venoms, increasingly recognized as reservoirs of bioactive compounds with diverse pharmacological effects, have been the focus of recent research. This work evaluates the use of various screening methodologies in assessing the antimicrobial activities of 185 venoms against some gram positive and gram negative bacteria, including E.

Myotoxin-3 from the Pacific Rattlesnake Venom Is a New Microtubule-Targeting Agent.

Microtubule targeting agents (MTA) are anti-cancer molecules that bind tubulin and interfere with the microtubule functions, eventually leading to cell death. In the present study, we used an in vitro microtubule polymerization assay to screen several venom families for the presence of anti-microtubule activity. We isolated myotoxin-3, a peptide of the crotamine family, and three isoforms from the venom of the Northern Pacific rattlesnake , which was able to increase tubulin polymerization.

Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.

Voltage-gated Na (Na) channels are significant therapeutic targets for the treatment of cardiac and neurological disorders, thus promoting the search for novel Na channel ligands. With the objective of discovering new blockers of Na channel ligands, we screened an In-House vegetal alkaloid library using fluorescence cell-based assays. We screened 62 isoquinoline alkaloids (IA) for their ability to decrease the FRET signal of voltage sensor probes (VSP), which were induced by the activation of Na channels with batrachotoxin (BTX) in GH3b6 cells.

Pharmacological Dissection of the Crosstalk between Na and Ca Channels in GH3b6 Cells.

Thanks to the crosstalk between Na and Ca channels, Na and Ca homeostasis interplay in so-called excitable cells enables the generation of action potential in response to electrical stimulation. Here, we investigated the impact of persistent activation of voltage-gated Na (Na) channels by neurotoxins, such as veratridine (VTD), on intracellular Ca concentration ([Ca]) in a model of excitable cells, the rat pituitary GH3b6 cells, in order to identify the molecular actors involved in Na-Ca homeostasis crosstalk. By combining RT-qPCR, immunoblotting, immunocytochemistry, and patch-clamp techniques, we showed that GH3b6 cells predominantly express the Na1.

Isolation of an Anti-Tumour Disintegrin: Dabmaurin-1, a Peptide Lebein-1-Like, from Venom.

In the soft treatment of cancer tumours, consequent downregulation of the malignant tissue angiogenesis constitutes an efficient way to stifle tumour development and metastasis spreading. As angiogenesis requires integrin-promoting endothelial cell adhesion, migration, and vessel tube formation, integrins represent potential targets of new therapeutic anti-angiogenic agents. Our work is a contribution to the research of such therapeutic disintegrins in animal venoms.

Gram-scale purification of aconitine and identification of lappaconitine in Aconitum karacolicum.

Aconitum karacolicum from northern Kyrgyzstan (Alatau area) contains about 0.8-1% aconitine as well as other aconite derivatives that have already been identified. In this paper, we compare several methods for the further purification of an Aconitum karacolicum extract initially containing 80% of aconitine.

ArgTX-636, a polyamine isolated from spider venom: A novel class of melanogenesis inhibitors.

To discover new molecules with an inhibitory activity of melanogenesis a hundred of scorpions, snakes, spiders and amphibians venoms were screened for their capacity to inhibit mushroom tyrosinase using 3,4-l-dihydroxyphenylalanine (l-DOPA) as substrate. The Argiope lobata spider venom proved to be the most active. HPLC fraction containing Argiotoxine-636 (ArgTX-636), a polyamine known for its numerous biological activities, was found to also show a good regulation activity of melanogenesis by inhibiting DOPA and 5,6-dihydroxyindole-2-carboxylic acid (DHICA) oxidases activities, wore by tyrosinase (TYR) and tyrosinase-related protein 1 (TRP-1), respectively.

Changes in endogenous urea recycling and the handling of renal urea in pregnant and lactating Sardi sheep kept on a constant feeding level.

The kinetics of endogenous urea were compared during the last month of pregnancy, lactation, and a nonpregnant, nonlactating control period in Sardi sheep kept on a constant feed level. Urea entry rate estimated by injections of [14C]urea rose by 36% during pregnancy. Renal urea excretion was reduced by 40% during pregnancy and by 28% during lactation.

An in vivo model for pharmacokinetic studies in the kidney.

In order to assess drug renal kinetics in vivo, the two kidneys of seven ewes were surgically placed under the skin. Through the use of renal function tests and a series of biopsies, we found that the kidneys remained normal in their subcutaneous location. Gentamicin renal kinetics were evaluated in conscious animals by a series of biopsies.

Prednisolone succinate and prednisolone acetate in cattle: pharmacokinetics and action on the adrenal gland.

The pharmacokinetics of prednisolone were studied in a group of 6 cows given prednisolone 21-sodium succinate IV and IM (600 micrograms/kg of body weight expressed as prednisolone alcohol) and prednisolone acetate IM (600 micrograms/kg of body weight expressed as prednisolone alcohol). After IV administration of prednisolone 21-sodium succinate, the half-life of elimination was 3.6 +/- 1.

Dexamethasone and prednisolone in the horse: pharmacokinetics and action on the adrenal gland.

Pharmacokinetics of dexamethasone and prednisolone were studied in 6 horses given dexamethasone alcohol (IV or IM) or dexamethasone 21-isonicotinate as a solution IV or IM (50 micrograms/kg of body weight), prednisolone 21-sodium succinate IV or IM (0.6 mg/kg of body weight), or prednisolone acetate IM (0.6 mg/kg of body weight).