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1.
Asian-Australas J Anim Sci ; 28(2): 280-9, 2015 Feb.
Article in English | MEDLINE | ID: mdl-25557826

ABSTRACT

Anaerobic digestion is an efficient and renewable energy technology that can produce biogas from a variety of biomasses such as animal manure, food waste and plant residues. In developing countries this technology is widely used for the production of biogas using local biomasses, but there is little information about the value of these biomasses for energy production. This study was therefore carried out with the objective of estimating the biogas production potential of typical Vietnamese biomasses such as animal manure, slaughterhouse waste and plant residues, and developing a model that relates methane (CH4) production to the chemical characteristics of the biomass. The biochemical methane potential (BMP) and biomass characteristics were measured. Results showed that piglet manure produced the highest CH4 yield of 443 normal litter (NL) CH4 kg(-1) volatile solids (VS) compared to 222 from cows, 177 from sows, 172 from rabbits, 169 from goats and 153 from buffaloes. Methane production from duckweed (Spirodela polyrrhiza) was higher than from lawn grass and water spinach at 340, 220, and 110.6 NL CH4 kg(-1) VS, respectively. The BMP experiment also demonstrated that the CH4 production was inhibited with chicken manure, slaughterhouse waste, cassava residue and shoe-making waste. Statistical analysis showed that lipid and lignin are the most significant predictors of BMP. The model was developed from knowledge that the BMP was related to biomass content of lipid, lignin and protein from manure and plant residues as a percentage of VS with coefficient of determination (R-square) at 0.95. This model was applied to calculate the CH4 yield for a household with 17 fattening pigs in the highlands and lowlands of northern Vietnam.

2.
Bioorg Med Chem ; 9(5): 1185-95, 2001 May.
Article in English | MEDLINE | ID: mdl-11377177

ABSTRACT

The interaction of P1 and P3 side chains with the combining S1 and S3 hydrophobic subsites of HIV and FIV proteases has been explored using asymmetric competitive inhibitors. The inhibitors evaluated contained (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid (allophenylnorstatine) as the hydroxymethylcarbonyl isostere, (R)-5,5-dimethyl-1, 3-thiazolidine-4-carbonyl as P1', Val as P2 and P2' residues, and a variety of amino acids at the P3 and P3' positions. All inhibitors showed competitive inhibition of both enzymes with higher potency against the HIV protease in vitro. Within this series, 31 (VLE776) is the most effective inhibitor against FIV protease, and it contains Phe at P3, but no P3' residue. VLE776 also exhibited potent antiviral activities against the drug-resistant HIV mutants (G48V and V82F) and the TL3-resistant HIV mutants. Explanation of the inhibition activities was described. In addition, a new strategy was described for development of bifunctional inhibitors, which combine the protease inhibitor and another enzyme inhibitor in one molecule.


Subject(s)
Aspartic Acid Endopeptidases/antagonists & inhibitors , HIV Protease/drug effects , Phenylbutyrates/chemistry , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , Thiazoles/chemistry , Thiazoles/pharmacology , Aspartic Acid Endopeptidases/metabolism , Drug Resistance/genetics , HIV Protease/metabolism , HIV Protease Inhibitors/chemistry , HIV Protease Inhibitors/metabolism , HIV Protease Inhibitors/pharmacology , Inhibitory Concentration 50 , Mutagenesis/genetics , Oligonucleotides/chemistry , Oligonucleotides/metabolism , Oligonucleotides/pharmacology , Phenylbutyrates/metabolism , Phenylbutyrates/pharmacology , Protease Inhibitors/metabolism , Structure-Activity Relationship
3.
Bioorg Med Chem Lett ; 11(2): 219-22, 2001 Jan 22.
Article in English | MEDLINE | ID: mdl-11206463

ABSTRACT

A series of norstatine-based HIV/FIV protease inhibitors incorporating a 15-membered macrocycle as a mimic of the tripeptide (Ala-Val-Phe), a motif with a small P3' residue elective against the FIV protease and the drug-resistant HIV proteases, has been synthesized. It was found that the macrocycle is important to the overall activity of the inhibitors. Certain inhibitors were developed expressing low nanomolar inhibitory activity against the HIV/FIV proteases and they are also effective against some drug-resistant as well as TL3-resistant HIV proteases.


Subject(s)
Aspartic Acid Endopeptidases/antagonists & inhibitors , HIV Protease Inhibitors/chemical synthesis , Peptides, Cyclic/pharmacology , Amino Acid Motifs , Aminocaproates/chemistry , Antiviral Agents/chemical synthesis , Antiviral Agents/pharmacology , Combinatorial Chemistry Techniques , Drug Design , Drug Resistance , HIV Protease Inhibitors/pharmacology , Immunodeficiency Virus, Feline/enzymology , Inhibitory Concentration 50 , Molecular Conformation , Molecular Mimicry , Peptides, Cyclic/chemical synthesis , Protease Inhibitors/chemical synthesis , Protease Inhibitors/pharmacology , Structure-Activity Relationship
4.
J Org Chem ; 65(8): 2399-409, 2000 Apr 21.
Article in English | MEDLINE | ID: mdl-10789452

ABSTRACT

The synthesis of 2'-substituted polyhydroxytetrahydropyrimidines as transition-state mimics of enzymatic glycosidic cleavage has been achieved by using guanylation and cyclization methodologies. The D-galacto type N-hydroxy cyclic guanidino-sugar 21 was synthesized in six steps from amine 7 and thiourea 14 in an overall yield of 59%. To further derivatize compound 21 to incorporate the leaving group moiety, we have synthesized 2-methylsulfanyl compounds 26-29 as key intermediates. The 2-methylsulfanyl group in 29 was displaced with amines, assisted by silver tetrafluoroborate as Lewis acid, to give protected cyclic guanidines 30-32 in moderate yields (60-67%). Removal of the protecting groups in 32 gave the D-galacto-type N-hydroxy cyclic guanidino-sugar 34. The key steps in the synthesis of the 6-deoxy-DL-galacto type N-hydroxy cyclic guanidino-sugars 49, 54, and 64-66 involve cyclization of the appropriate acetal intermediates (45, 50, and 58-60) followed by removal of the protecting groups.


Subject(s)
Glycoside Hydrolases/chemistry , Glycosides/chemistry , Pyrimidines/chemical synthesis , Crystallography, X-Ray , Cyclization , Glycoside Hydrolases/antagonists & inhibitors , Guanine/chemistry , Indicators and Reagents , Magnetic Resonance Spectroscopy , Molecular Conformation
5.
J Virol ; 74(10): 4710-20, 2000 May.
Article in English | MEDLINE | ID: mdl-10775609

ABSTRACT

Feline immunodeficiency virus (FIV) protease is structurally very similar to human immunodeficiency virus (HIV) protease but exhibits distinct substrate and inhibitor specificities. We performed mutagenesis of subsite residues of FIV protease in order to define interactions that dictate this specificity. The I37V, N55M, M56I, V59I, and Q99V mutants yielded full activity. The I37V, N55M, V59I, and Q99V mutants showed a significant increase in activity against the HIV-1 reverse transcriptase/integrase and P2/nucleocapsid junction peptides compared with wild-type (wt) FIV protease. The I37V, V59I, and Q99V mutants also showed an increase in activity against two rapidly cleaved peptides selected by cleavage of a phage display library with HIV-1 protease. Mutations at Q54K, I98P, and L101I dramatically reduced activity. Mutants containing a I35D or I57G substitution showed no activity against either FIV or HIV substrates. FIV proteases all failed to cut HIV-1 matrix/capsid, P1/P6, P6/protease, and protease/reverse transcriptase junctions, indicating that none of the substitutions were sufficient to change the specificity completely. The I37V, N55M, M56I, V59I, and Q99V mutants, compared with wt FIV protease, all showed inhibitor specificity more similar to that of HIV-1 protease. The data also suggest that FIV protease prefers a hydrophobic P2/P2' residue like Val over Asn or Glu, which are utilized by HIV-1 protease, and that S2/S2' might play a critical role in distinguishing FIV and HIV-1 protease by specificity. The findings extend our observations regarding the interactions involved in substrate binding and aid in the development of broad-based inhibitors.


Subject(s)
Aspartic Acid Endopeptidases/chemistry , Aspartic Acid Endopeptidases/metabolism , Immunodeficiency Virus, Feline/enzymology , Protease Inhibitors/pharmacology , Amino Acid Sequence , Animals , Aspartic Acid Endopeptidases/genetics , Cats , Fluorescent Dyes/metabolism , HIV Protease/chemistry , HIV Protease/genetics , HIV Protease/metabolism , HIV Reverse Transcriptase/metabolism , Humans , Inhibitory Concentration 50 , Kinetics , Models, Molecular , Molecular Sequence Data , Mutagenesis , Peptide Library , Peptides/metabolism , Retroviridae Proteins/metabolism , Substrate Specificity
6.
J Chir (Paris) ; 118(12): 725-38, 1981 Dec.
Article in French | MEDLINE | ID: mdl-7320100

ABSTRACT

An anatomical study, based essentially upon 38 dissections of formol-preserved specimens, was used to identify the different characteristics of the vagus nerve which might have an influence on different vagotomy techniques. The arrangement of the different vagal structures (principal and accessory) at the oesophageal orifice is described in full. The most criminal branches are pointed out with particular emphasis. Distribution branches unknown or poorly known up to the present have been demonstrated. The principal nerves of the lesser curvature and their endings are reviewed in the context of supraselective vagotomy. The discussion emphasis the most important anatomical details relevant to the achievement of adequate supraselective vagotomy.


Subject(s)
Vagotomy, Proximal Gastric , Vagotomy , Vagus Nerve/anatomy & histology , Adult , Humans , Stomach/innervation
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