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The discovery of molecules that can inhibit the action of phytopathogens is essential to find alternative to current pesticides. Pectin methylesterases (PME), enzymes that fine-tune the degree of methylesterification of plant cell wall pectins, play a key role in the pathogenicity of fungi or bacteria. Here we report the synthesis of new lactoside derivatives and their analysis as potential PME inhibitors using three plants and one fungal PME. Because of its structure, abundance and reduced cost, lactose was chosen as a case study. Lactoside derivatives were obtained by TEMPO-mediated oxidation of methyl lactoside, followed by an esterification procedure. Three derivatives were synthesized: sodium (methyl-lactosid)uronate, methyl (methyl-lactosid)uronate and butyl (methyl-lactosid)uronate. The inhibition of the plant and pathogen enzyme activities by lactoside derivatives was measured in vitro, showing the importance of the substitution on lactose: methyl (methyl-lactosid)uronate was more efficient than butyl (methyl-lactosid)uronate. These results were confirmed by docking analysis showing the difference in the interaction between lactoside derivatives and PME proteins. In conclusion, this study identified novel inhibitors of pectin remodeling enzymes.
This article was published in the following journal.
Name: International journal of biological macromolecules
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RP-G28 is being investigated for treatment of moderate to severe lactose intolerance and its potential to improve the tolerance of lactose (dairy products).
The hypothesis underlying this study is that failure to recognise the role of lactose intolerance among patients has led to inappropriate dietary advice and treatment with drugs that conta...
Ritter Pharmaceuticals, Inc. is developing RP G28 as a treatment for Lactose Intolerance. Lactose intolerance is a syndrome of gastrointestinal symptoms resulting from a deficiency in inte...
The hypothesis underlying this study is that failure to recognise the role of lactose intolerance among patients with ulcerative colitis has led to inappropriate dietary advice and treatme...
It is currently assumed that all patients are lactose intolerant post bone marrow transplantation. This pilot study is to assess what the incidence of lactose intolerance is after bone mar...
The condition resulting from the absence or deficiency of LACTASE in the MUCOSA cells of the GASTROINTESTINAL TRACT, and the inability to break down LACTOSE in milk for ABSORPTION. Bacterial fermentation of the unabsorbed lactose leads to symptoms that range from a mild indigestion (DYSPEPSIA) to severe DIARRHEA. Lactose intolerance may be an inborn error or acquired.
Plasmids which determine the ability of a bacterium to ferment lactose.
A measure of a patient's ability to break down lactose.
An enzyme of the transferase class that catalyzes the transfer of galactose from UDPgalactose to glucose, forming lactose. The enzyme is a complex of the enzyme N-ACETYLLACTOSAMINE SYNTHASE and alpha-lactalbumin; the latter protein is present in lactating mammary gland cells where it alters the usual specificity of the former to make lactose synthesis the preferred reaction. (Dorland, 28th ed) EC 220.127.116.11.
An enzyme which catalyzes the hydrolysis of LACTOSE to D-GALACTOSE and D-GLUCOSE. Defects in the enzyme cause LACTOSE INTOLERANCE.
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