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David R Rose - One of the best experts on this subject based on the ideXlab platform.

  • probing the intestinal α glucosidase enzyme specificities of Starch digesting maltase glucoamylase and sucrase isomaltase synthesis and inhibitory properties of 3 and 5 maltose extended de o sulfonated ponkoranol
    Chemistry: A European Journal, 2011
    Co-Authors: Razieh Eskandari, Kumarasamy Jayakanthan, David R Rose, Kyra Jones, Kongara Ravinder Reddy, Marcia M Chaudet, Mario B Pinto
    Abstract:

    The synthesis and glucosidase inhibitory activities of two C-3′- and C-5′-β-maltose-extended analogues of the naturally occurring sulfonium-ion inhibitor, de-O-sulfonated ponkoranol, are described. The compounds are designed to test the specificity towards four intestinal glycoside hydrolase family 31 (GH31) enzyme activities, responsible for the hydrolysis of terminal Starch Products and sugars into glucose, in humans. The target sulfonium-ion compounds were synthesized by means of nucleophilic attack of benzyl protected 1,4-anhydro-4-thio-D-arabinitol at the C-6 position of 6-O-trifluoromethanesulfonyl trisaccharides as alkylating agents. The alkylating agents were synthesized from D-glucose by glycosylation at C-4 or C-2 with maltosyl trichloroacetimidate. Deprotection of the coupled Products by using a two-step sequence, followed by reduction afforded the final compounds. Evaluation of the target compounds for inhibition of the four glucosidase activities indicated that selective inhibition of one enzyme over the others is possible.

  • new glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes structures and inhibition of human intestinal maltase glucoamylase with compounds from salacia reticulata
    Biochemistry, 2010
    Co-Authors: Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target α-amylases and intestinal glucosidases using α-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of α-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (Ki = 0.03 μM), some 2000-fold better than the compounds currently used in the clinic, and highlights the poten...

  • New glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes: structures and inhibition of human intestinal maltase-glucoamylase with compounds from Salacia reticulata.
    Biochemistry, 2010
    Co-Authors: Lyann Sim, Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target alpha-amylases and intestinal glucosidases using alpha-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of alpha-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (K(i) = 0.03 microM), some 2000-fold better than the compounds currently used in the clinic, and highlights the potential of the salacinol class of inhibitors as future drug candidates.

M S Brewer - One of the best experts on this subject based on the ideXlab platform.

  • effect of salmon type and presence absence of bone on color sensory characteristics and consumer acceptability of pureed and chunked infant food Products
    Journal of Food Science, 2010
    Co-Authors: F A Desantos, L Ramamoorthi, Peter J Bechtel, Scott Smiley, M S Brewer
    Abstract:

    Salmon-based infant food (puree) and toddler food (puree plus chunks) were manufactured from pink salmon, with and without bone, and from Sockeye salmon, with and without bone, to contain 45% salmon, 55% water, and 5% Starch. Products were retort processed at 118 to 121 degrees C for 55 min in a steam-jacketed still retort. A trained descriptive panel (n = 7) evaluated infant and toddler foods separately. Instrumental color, pH, and water activity were also determined. Infant and toddler foods were also evaluated by a consumer panel (n = 104) of parents for product acceptability. During the manufacturing process (cooking, homogenization, retort processing), salmon infant food from pink salmon lost much of its characteristic pink color while that from sockeye salmon retained a greater amount. Bitterness was more evident in samples with bones. In the toddler food formulation containing chunks, the odor and flavor characteristics were influenced primarily by the type of salmon. The presence of bone affected visual pink color and lightness, and salmon odor only. Consumers scored Products made with sockeye salmon as more acceptable despite the fact that they had more off-flavor than Products from pink salmon. The appearance and thickness of the pureed infant food was more acceptable than the toddler food with chunks despite the chunky toddler product having more acceptable salmon flavor. This indicates that the color and appearance of the prototypes were the main drivers for liking. Of the total number of parents surveyed, 73% would feed this salmon product to their children.

  • effect of salmon type and presence absence of bone on color sensory characteristics and consumer acceptability of pureed and chunked infant food Products
    Journal of Food Science, 2010
    Co-Authors: F A Desantos, L Ramamoorthi, Peter J Bechtel, Scott Smiley, M S Brewer
    Abstract:

    :  Salmon-based infant food (puree) and toddler food (puree plus chunks) were manufactured from pink salmon, with and without bone, and from Sockeye salmon, with and without bone, to contain 45% salmon, 55% water, and 5% Starch. Products were retort processed at 118 to 121 °C for 55 min in a steam-jacketed still retort. A trained descriptive panel (n = 7) evaluated infant and toddler foods separately. Instrumental color, pH, and water activity were also determined. Infant and toddler foods were also evaluated by a consumer panel (n = 104) of parents for product acceptability. During the manufacturing process (cooking, homogenization, retort processing), salmon infant food from pink salmon lost much of its characteristic pink color while that from sockeye salmon retained a greater amount. Bitterness was more evident in samples with bones. In the toddler food formulation containing chunks, the odor and flavor characteristics were influenced primarily by the type of salmon. The presence of bone affected visual pink color and lightness, and salmon odor only. Consumers scored Products made with sockeye salmon as more acceptable despite the fact that they had more off-flavor than Products from pink salmon. The appearance and thickness of the pureed infant food was more acceptable than the toddler food with chunks despite the chunky toddler product having more acceptable salmon flavor. This indicates that the color and appearance of the prototypes were the main drivers for liking. Of the total number of parents surveyed, 73% would feed this salmon product to their children.

Kumarasamy Jayakanthan - One of the best experts on this subject based on the ideXlab platform.

  • probing the intestinal α glucosidase enzyme specificities of Starch digesting maltase glucoamylase and sucrase isomaltase synthesis and inhibitory properties of 3 and 5 maltose extended de o sulfonated ponkoranol
    Chemistry: A European Journal, 2011
    Co-Authors: Razieh Eskandari, Kumarasamy Jayakanthan, David R Rose, Kyra Jones, Kongara Ravinder Reddy, Marcia M Chaudet, Mario B Pinto
    Abstract:

    The synthesis and glucosidase inhibitory activities of two C-3′- and C-5′-β-maltose-extended analogues of the naturally occurring sulfonium-ion inhibitor, de-O-sulfonated ponkoranol, are described. The compounds are designed to test the specificity towards four intestinal glycoside hydrolase family 31 (GH31) enzyme activities, responsible for the hydrolysis of terminal Starch Products and sugars into glucose, in humans. The target sulfonium-ion compounds were synthesized by means of nucleophilic attack of benzyl protected 1,4-anhydro-4-thio-D-arabinitol at the C-6 position of 6-O-trifluoromethanesulfonyl trisaccharides as alkylating agents. The alkylating agents were synthesized from D-glucose by glycosylation at C-4 or C-2 with maltosyl trichloroacetimidate. Deprotection of the coupled Products by using a two-step sequence, followed by reduction afforded the final compounds. Evaluation of the target compounds for inhibition of the four glucosidase activities indicated that selective inhibition of one enzyme over the others is possible.

  • new glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes structures and inhibition of human intestinal maltase glucoamylase with compounds from salacia reticulata
    Biochemistry, 2010
    Co-Authors: Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target α-amylases and intestinal glucosidases using α-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of α-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (Ki = 0.03 μM), some 2000-fold better than the compounds currently used in the clinic, and highlights the poten...

  • New glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes: structures and inhibition of human intestinal maltase-glucoamylase with compounds from Salacia reticulata.
    Biochemistry, 2010
    Co-Authors: Lyann Sim, Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target alpha-amylases and intestinal glucosidases using alpha-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of alpha-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (K(i) = 0.03 microM), some 2000-fold better than the compounds currently used in the clinic, and highlights the potential of the salacinol class of inhibitors as future drug candidates.

F A Desantos - One of the best experts on this subject based on the ideXlab platform.

  • effect of salmon type and presence absence of bone on color sensory characteristics and consumer acceptability of pureed and chunked infant food Products
    Journal of Food Science, 2010
    Co-Authors: F A Desantos, L Ramamoorthi, Peter J Bechtel, Scott Smiley, M S Brewer
    Abstract:

    Salmon-based infant food (puree) and toddler food (puree plus chunks) were manufactured from pink salmon, with and without bone, and from Sockeye salmon, with and without bone, to contain 45% salmon, 55% water, and 5% Starch. Products were retort processed at 118 to 121 degrees C for 55 min in a steam-jacketed still retort. A trained descriptive panel (n = 7) evaluated infant and toddler foods separately. Instrumental color, pH, and water activity were also determined. Infant and toddler foods were also evaluated by a consumer panel (n = 104) of parents for product acceptability. During the manufacturing process (cooking, homogenization, retort processing), salmon infant food from pink salmon lost much of its characteristic pink color while that from sockeye salmon retained a greater amount. Bitterness was more evident in samples with bones. In the toddler food formulation containing chunks, the odor and flavor characteristics were influenced primarily by the type of salmon. The presence of bone affected visual pink color and lightness, and salmon odor only. Consumers scored Products made with sockeye salmon as more acceptable despite the fact that they had more off-flavor than Products from pink salmon. The appearance and thickness of the pureed infant food was more acceptable than the toddler food with chunks despite the chunky toddler product having more acceptable salmon flavor. This indicates that the color and appearance of the prototypes were the main drivers for liking. Of the total number of parents surveyed, 73% would feed this salmon product to their children.

  • effect of salmon type and presence absence of bone on color sensory characteristics and consumer acceptability of pureed and chunked infant food Products
    Journal of Food Science, 2010
    Co-Authors: F A Desantos, L Ramamoorthi, Peter J Bechtel, Scott Smiley, M S Brewer
    Abstract:

    :  Salmon-based infant food (puree) and toddler food (puree plus chunks) were manufactured from pink salmon, with and without bone, and from Sockeye salmon, with and without bone, to contain 45% salmon, 55% water, and 5% Starch. Products were retort processed at 118 to 121 °C for 55 min in a steam-jacketed still retort. A trained descriptive panel (n = 7) evaluated infant and toddler foods separately. Instrumental color, pH, and water activity were also determined. Infant and toddler foods were also evaluated by a consumer panel (n = 104) of parents for product acceptability. During the manufacturing process (cooking, homogenization, retort processing), salmon infant food from pink salmon lost much of its characteristic pink color while that from sockeye salmon retained a greater amount. Bitterness was more evident in samples with bones. In the toddler food formulation containing chunks, the odor and flavor characteristics were influenced primarily by the type of salmon. The presence of bone affected visual pink color and lightness, and salmon odor only. Consumers scored Products made with sockeye salmon as more acceptable despite the fact that they had more off-flavor than Products from pink salmon. The appearance and thickness of the pureed infant food was more acceptable than the toddler food with chunks despite the chunky toddler product having more acceptable salmon flavor. This indicates that the color and appearance of the prototypes were the main drivers for liking. Of the total number of parents surveyed, 73% would feed this salmon product to their children.

Sankar Mohan - One of the best experts on this subject based on the ideXlab platform.

  • new glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes structures and inhibition of human intestinal maltase glucoamylase with compounds from salacia reticulata
    Biochemistry, 2010
    Co-Authors: Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target α-amylases and intestinal glucosidases using α-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of α-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (Ki = 0.03 μM), some 2000-fold better than the compounds currently used in the clinic, and highlights the poten...

  • New glucosidase inhibitors from an ayurvedic herbal treatment for type 2 diabetes: structures and inhibition of human intestinal maltase-glucoamylase with compounds from Salacia reticulata.
    Biochemistry, 2010
    Co-Authors: Lyann Sim, Kumarasamy Jayakanthan, Sankar Mohan, Ravindranath Nasi, Blair D Johnston, B M Pinto, David R Rose
    Abstract:

    An approach to controlling blood glucose levels in individuals with type 2 diabetes is to target alpha-amylases and intestinal glucosidases using alpha-glucosidase inhibitors acarbose and miglitol. One of the intestinal glucosidases targeted is the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM), one of the four intestinal glycoside hydrolase 31 enzyme activities responsible for the hydrolysis of terminal Starch Products into glucose. Here we present the X-ray crystallographic studies of ntMGAM in complex with a new class of alpha-glucosidase inhibitors derived from natural extracts of Salacia reticulata, a plant used traditionally in Ayuverdic medicine for the treatment of type 2 diabetes. Included in these extracts are the active compounds salacinol, kotalanol, and de-O-sulfonated kotalanol. This study reveals that de-O-sulfonated kotalanol is the most potent ntMGAM inhibitor reported to date (K(i) = 0.03 microM), some 2000-fold better than the compounds currently used in the clinic, and highlights the potential of the salacinol class of inhibitors as future drug candidates.