Over the past two decades a significant increase in fungal infections has been observed (1). More than any other antifungal class, the azoles have been steadily refined and improved upon over the course of almost 50 years. These antifungal compounds are chemically either an imidazole or a triazole group joined to carbon atom as their functional pharmacophore and working through blocking the act...

3,5-Bis(trifluoromethyl)pyrazole derivative (BTP2) or N-[4–3, 5-bis(trifluromethyl)pyrazol-1-yl]-4-methyl-1,2,3-thiadiazole-5carboxamide (YM-58483) is an immunosuppressive compound that potently inhibits both Ca influx and interleukin-2 (IL-2) production in lymphocytes. We report here that BTP2 dosedependently enhances transient receptor potential melastatin 4 (TRPM4), a Ca -activated nonselect...

A 5-year-old, neutered male domestic shorthair cat was referred for evaluation of suspected hypothyroidism. In the previous 2 months, the owner reported mild lethargy, weight gain with decreased appetite, unkempt hair coat, and an episode of bilateral external otitis that temporarily improved after a 10-day treatment with ear medications containing gentamicin, betamethasone, and clotrimazole; t...

Characteristics of pituitary adenylate cyclase-activating polypeptide (PACAP)-induced increase of Ca entry and catecholamine (CA) release were studied in bovine adrenal medullary chromaffin cells. PACAP induced intracellular free Ca concentration ([Ca ]i), showing an initial transient [Ca ]i rise followed by a sustained rise and CA release, which were not blocked by the blocking agents for nico...

nitrate is a widely used antifungal agent, but its use in topical formulations is not efficacious because deepseated fungal infections are difficult to treat with conventional topical formulations. The entrapment of a drug in liposomes can facilitate localized delivery of the drug, and improved availability by means of a controlled-release pattern can advance the treatment of deep fungal infect...

R.J. Hay, Department of Dermatology, Guys Hospital, London SE1 9RT, London, UK The present comprehensive range of antifungal drugs used in the treatment of superficial mycoses is by no means ideal. There are, for instance, certain infections which are refractory to existing therapy such as chronic tinea pedis due to Trichophyton rubrum, which has a 60–70% relapse rate whatever the primary thera...

Objective: Transdermal patch is a promising approach that allows continuous input of drugs with short biological half-lives. 18 β-Glycyrrhitic acid (GA) is chemically pentacyclic triterpenoid which possess powerful antiinflammatory action. The present study was designed to formulate GA reservoir-type transdermal patches using piperine as bioenhancer. Method: Transdermal Patch of GA was prepared...

Disturbances of endoplasmic reticulum (ER) Ca homeostasis or protein processing can lead to ER stress-induced cell death. Increasing evidence suggests that oxidative stress (OS) plays an important role in a variety of cell death mechanisms. To investigate the role of OS in ER stress, we measured OS in response to three ER stress agents: econazole (Ec), which stimulates ER Ca release and blocks ...

Rapidly growing global populations mandate greater crop productivity despite increasingly scarce natural resources, including freshwater. The adoption of sustainable agricultural practices seek to address such issues, but an unintended consequence is the exposure soils and associated biota emerging contaminants azole pharmaceutical antifungals. We show that environmentally relevant three common...

The effect of 3-[1-(p-chlorobenzyl)-5-(isopropyl)-3-tert-butylthioindol-2-yl]-2, 2-dimethylpropanoic acid (MK-886), a leukotriene biosynthesis inhibitor, on Ca mobilization in MadinDarby canine kidney cells has been examined by fluorimetry using fura-2 as a Ca indicator. MK-886 at 0.5 to 25 mM concentration dependently increased [Ca]i. The [Ca ]i increase comprised an immediate initial rise and...