Metal Fluoride Inhibition of a P-type H+ Pump

Abstract

Background:Plasma membrane H ϩ -ATPase proton pumps exist in basal and activated states.

Fluoride contributes to the shaping of microbial community in high fluoride groundwater in Qiji County, Yuncheng City, China

“…As a toxic element, fluoride can inhibit or kill microbes by affecting bacterial metabolism through a set of actions with fundamentally different mechanisms 21,26,27,29 . For example, Al-F or Mg-F, the major metal-fluoride complexes present in high fluoride groundwater, were responsible for fluoride inhibition of phosphate transfer enzymes under laboratory conditions 66 .…”

“…Based on the previous studies, the antimicrobial activity of fluoride is mediated via three major effects of fluoride: (i) enzyme inhibition. The direct inhibition of the F-ATPase enzyme by fluoride was found to be dependent on cations 21,22 , and fluoride is a potent inhibitor of enolase, catalase, phosphatases and other enzymes of many organisms 23–25 ; (ii) fluoride was found to alter the proton movement through cell membranes and inhibit intracellular acid production 26,27 ; (iii) fluoride can inhibit certain microbes in the ingestion, transformation and utilization of certain nutrients, affecting the synthesis of extracellular polysaccharides and the storage of intracellular polysaccharides 28–30 .…”

LEGO‐Inspired Drug Design: Unveiling a Class of Benzo[d]thiazoles Containing a 3,4‐Dihydroxyphenyl Moiety as Plasma Membrane H+‐ATPase Inhibitors

“…The precipitate was filtered and washed (3 10 mL) with CH 3 CN, EtOH, hot acetone, followed by recrystallization in EtOH to afford clean 1-15 as hydrochloride salts. General synthetic procedure for compounds [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30].Am ixture of 1-(substituted phenyl)ethan-1-one (1 equiv), copper(II) bromide (1 equiv), and 8mLo famixture of ethyl acetate/dichloromethane (1:1) was added to a2 0mLm icrowave reaction vial (Biotage). The vial was sealed and irradiated in am icrowave apparatus at 60 8C, high absorption for 15 min.…”

“…The crude product above was dissolved in 20 mL of CH 3 CN and the appropriately substituted heterocyclic thiol (1 equiv) was added and stirred at room temperature for 30 min until the appearance of as olid precipitate. The precipitate was then filtered and fast washed (3 10 mL) with each of CH 3 CN, EtOH, and hot acetone, followed by recrystallization in EtOH to afford clean [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30] [1,4]dioxin-6-yl)-2-(quinolin-2-ylthio)ethan-1-one (16) Synthesis of 32-46:C ompounds 32-46 were synthesized using the same procedure as described for 1-15 from 31 a-o using microwave methodology (exception to workup procedure:a cidified to pH 4b yc onc. HBr instead of HCl, and products were collected as hydrobromide salts).…”

“…Proton transport measurement:P reparation of lecithin liposomereconstituted Pma1p and proton transport assay were performed as previously described [23] by monitoring fluorescence quenching of 9-amino-6-chloro-2-methoxyacridine (ACMA). The assay was conducted at 22 8Ci nt otal volumes of 1mLw ith am edium buffer containing 20 mm MES-KOH, pH 6.0, 40 mm K 2 SO 4 ,2m m ATP, 1 mm ACMA and 60 nm valinomycin.…”