The Proton Pump Inhibitor, Omeprazole, but Not Lansoprazole or
... omeprazole does cause clinically significant inhibition of CYP2C19. This apparent discrepancy could be explained if omeprazole, but not lansoprazole, were an irreversible inhibitor of CYP2C19. In support of this possibility, we presented preliminary in vitro evidence for metabolism-dependent inhibit ...
... omeprazole does cause clinically significant inhibition of CYP2C19. This apparent discrepancy could be explained if omeprazole, but not lansoprazole, were an irreversible inhibitor of CYP2C19. In support of this possibility, we presented preliminary in vitro evidence for metabolism-dependent inhibit ...
Role of the glutamine transaminase-m-amidase
... Evidence for the operation of the glutamine transaminase-cu-amidase pathway in mammalian cells has been amply documented by Cooper & Meister (1977). In this pathway, glutamine is transaminated to yield different amino acids and 2-oxoglutaramate through the participation of a glutamine transaminase; ...
... Evidence for the operation of the glutamine transaminase-cu-amidase pathway in mammalian cells has been amply documented by Cooper & Meister (1977). In this pathway, glutamine is transaminated to yield different amino acids and 2-oxoglutaramate through the participation of a glutamine transaminase; ...
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... bacterial growth showed the reduction of resazurin caused by bacterial metabolism, which was observed after two days of incubation. The MIC (minimum inhibitory concentration) was expressed as the lowest concentration of the drug that inhibited Mtb-growth or prevented change in color of the resazurin ...
... bacterial growth showed the reduction of resazurin caused by bacterial metabolism, which was observed after two days of incubation. The MIC (minimum inhibitory concentration) was expressed as the lowest concentration of the drug that inhibited Mtb-growth or prevented change in color of the resazurin ...
Pharmacology of platelet inhibition in humans: implications of the
... FIGURE 1. Prevention by salicylate of aspirin inhibition of arachidonic acid-induced platelet aggregation. Rat platelet aggregation was induced by threshold concentrations of arachidonic acid (AA 0.5 mM). Aspirin (100 jM) preincubation (1 min) with PRP completely prevented aggregation, whereas sodiu ...
... FIGURE 1. Prevention by salicylate of aspirin inhibition of arachidonic acid-induced platelet aggregation. Rat platelet aggregation was induced by threshold concentrations of arachidonic acid (AA 0.5 mM). Aspirin (100 jM) preincubation (1 min) with PRP completely prevented aggregation, whereas sodiu ...
Advances in Pharmacological Research of Eugenol
... The development and application of natural drugs have been done for thousands of years. As a type of plant extract, eugenol has a very long application history. In recent years, given its low toxicity and less residual activity, eugenol has been widely used in agriculture, forestry, animal husbandry ...
... The development and application of natural drugs have been done for thousands of years. As a type of plant extract, eugenol has a very long application history. In recent years, given its low toxicity and less residual activity, eugenol has been widely used in agriculture, forestry, animal husbandry ...
Potential medicinal benefits of Cosmos caudatus (Ulam Raja): A
... Anti-diabetic activity A previous study on obese, C. caudatus extract-treated rats showed a significant reduction in plasma blood glucose as compared to the control rats after one month of C. caudatus extract supplementation.[17] Acarbose, an alpha-glucosidase inhibitor, is widely used to treat type ...
... Anti-diabetic activity A previous study on obese, C. caudatus extract-treated rats showed a significant reduction in plasma blood glucose as compared to the control rats after one month of C. caudatus extract supplementation.[17] Acarbose, an alpha-glucosidase inhibitor, is widely used to treat type ...
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... the oral absorption of vancomycin and teicoplanin is very low so they must be administered intravenously to control systemic infections, which is not the preferred route of administration for many patients (Andre et al., 2010). Oxazolidinones are a novel class of synthetic antimicrobials with potent ...
... the oral absorption of vancomycin and teicoplanin is very low so they must be administered intravenously to control systemic infections, which is not the preferred route of administration for many patients (Andre et al., 2010). Oxazolidinones are a novel class of synthetic antimicrobials with potent ...
Irreversible Inhibitors of Serine, Cysteine, and Threonine Proteases
... new clan (CD) of cysteine proteases.23,24 Structural differences between clans and families of proteases of the same class should be useful for the design of specificity into inhibitor structures. The 20S proteasome is a 6500 amino acid protein with an active site N-terminal threonine (Thr 1). It pl ...
... new clan (CD) of cysteine proteases.23,24 Structural differences between clans and families of proteases of the same class should be useful for the design of specificity into inhibitor structures. The 20S proteasome is a 6500 amino acid protein with an active site N-terminal threonine (Thr 1). It pl ...
EFFECTS OF POMEGRANATE JUICE ON HUMAN CYTOCHROME
... the injection of pomegranate juice. These data suggest that pomegranate juice component(s) impairs the function of enteric but not hepatic CYP3A. Thus, we discovered that a component(s) of pomegranate inhibits the human CYP3A-mediated metabolism of carbamazepine. Furthermore, pomegranate juice alter ...
... the injection of pomegranate juice. These data suggest that pomegranate juice component(s) impairs the function of enteric but not hepatic CYP3A. Thus, we discovered that a component(s) of pomegranate inhibits the human CYP3A-mediated metabolism of carbamazepine. Furthermore, pomegranate juice alter ...
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... at 0–0.3–1.8–1.9–3.0 minute marks, respectively, in which the mobile phases A and B were water and methanol (both containing 0.1% formic acid), respectively, at a flow rate of 0.6 ml/min and injection volume of 5 ml. The mass spectrometer was operated under the positive ion detection mode using the ...
... at 0–0.3–1.8–1.9–3.0 minute marks, respectively, in which the mobile phases A and B were water and methanol (both containing 0.1% formic acid), respectively, at a flow rate of 0.6 ml/min and injection volume of 5 ml. The mass spectrometer was operated under the positive ion detection mode using the ...
The Role of N- and C-terminal Amino Acids to
... The fundamental link between the primary amino acid sequence and the functional protein has long been an area of interest with much still to be discovered. The goal of studying protein folding is to ultimately predict the folded structure and the function of a protein from its primary sequence. Anfi ...
... The fundamental link between the primary amino acid sequence and the functional protein has long been an area of interest with much still to be discovered. The goal of studying protein folding is to ultimately predict the folded structure and the function of a protein from its primary sequence. Anfi ...
Antiatherogenic Properties of Naringenin, a Citrus Flavonoid
... plasma (3,29) following oral doses of pure naringin (3,50) or grapefruit juice (3,29,64,92). Hesperetin has been detected also in human urine (3,92) and plasma (3) following doses of pure compound or orange juice. These results showed that naringenin and hesperetin can be absorbed from the diet. In ...
... plasma (3,29) following oral doses of pure naringin (3,50) or grapefruit juice (3,29,64,92). Hesperetin has been detected also in human urine (3,92) and plasma (3) following doses of pure compound or orange juice. These results showed that naringenin and hesperetin can be absorbed from the diet. In ...
Synopsis of Some Recent Tactical Application of Bioisosteres in
... range but conferred time-dependent CYP P450 inhibition, a phenomenon well-known with cyclopropylamines.58 A fluoroethyl substituent performed similarly, but 23 was dealkylated in rat liver microsomes (RLM) as the major metabolic pathway to afford 24 and fluoroacetaldehyde, which was oxidized to fluo ...
... range but conferred time-dependent CYP P450 inhibition, a phenomenon well-known with cyclopropylamines.58 A fluoroethyl substituent performed similarly, but 23 was dealkylated in rat liver microsomes (RLM) as the major metabolic pathway to afford 24 and fluoroacetaldehyde, which was oxidized to fluo ...
IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) e-ISSN: 2278-3008, p-ISSN:2319-7676.
... wide range of pharmacological activities. The whole plant has its own medicinal value. Papaya is a powerhouse of nutrients and is available throughout the year. It is a rich source of threes powerful antioxidant vitamin C, vitamin A and vitamin E; the minerals, magnesium and potassium; the B vitamin ...
... wide range of pharmacological activities. The whole plant has its own medicinal value. Papaya is a powerhouse of nutrients and is available throughout the year. It is a rich source of threes powerful antioxidant vitamin C, vitamin A and vitamin E; the minerals, magnesium and potassium; the B vitamin ...
International Journal of Ayurveda and Pharma Research
... of streptozotocin induced diabetic rats both in short term and long term study and also had renoprotective activity[71,72]. Oral administration of 75% methanolic extract of T. chebula (100 mg/kg body weight) reduced the blood sugar level in normal and alloxan diabetic rats significantly within 4 h ...
... of streptozotocin induced diabetic rats both in short term and long term study and also had renoprotective activity[71,72]. Oral administration of 75% methanolic extract of T. chebula (100 mg/kg body weight) reduced the blood sugar level in normal and alloxan diabetic rats significantly within 4 h ...
A review on pharmacological property of Mimusops elengi Linn.
... made from the dried flowers induces nasal discharge and relieves headache [6]. Fruits are used as astringent, coolant and anthelmintic. The tender stems are used as tooth brushes, and in cystorrhea, diarrhea and dysentery [5]. Flowers are brain tonic and are useful as snuff to relieve cephalalgia [7 ...
... made from the dried flowers induces nasal discharge and relieves headache [6]. Fruits are used as astringent, coolant and anthelmintic. The tender stems are used as tooth brushes, and in cystorrhea, diarrhea and dysentery [5]. Flowers are brain tonic and are useful as snuff to relieve cephalalgia [7 ...
Madhuca Indica JF Gmel. (Sapotaceae): An Overview
... saponins, Flavonoids and glycosides. M. indica is reported to possess antioxidant, anti-inflammatory, antimicrobial, hepatoprotective, antiulcer, antihyperglycaemic activity, antinociceptive and antidiarrhoeal activities. This work gives an overview of the phytochemical and pharmacological evidence ...
... saponins, Flavonoids and glycosides. M. indica is reported to possess antioxidant, anti-inflammatory, antimicrobial, hepatoprotective, antiulcer, antihyperglycaemic activity, antinociceptive and antidiarrhoeal activities. This work gives an overview of the phytochemical and pharmacological evidence ...
Review On The Medicinial Plant - Aerva Lanata
... Diuretic and anti-inflammatory activities of Aerva lanata in Rats: Male Albino rats were used for studying the diuretic activity of Aerva lanata, while the alcoholic extract of Aerva lanata increased the urine volume of rats moderately; this was equivalent to that of acetzolamide. The Na+ and K+ rat ...
... Diuretic and anti-inflammatory activities of Aerva lanata in Rats: Male Albino rats were used for studying the diuretic activity of Aerva lanata, while the alcoholic extract of Aerva lanata increased the urine volume of rats moderately; this was equivalent to that of acetzolamide. The Na+ and K+ rat ...
The activity and kinetic properties of cellulases in substrates
... The first two enzymes in this category act directly on cellulose, yielding mainly cellobiose and glucose as reaction products, and then the cellobiose is hydrolyzed into glucose by cellobiase [3,6]. Although the crude cellulase has a lower specific activity than pure cellulase containing only one of ...
... The first two enzymes in this category act directly on cellulose, yielding mainly cellobiose and glucose as reaction products, and then the cellobiose is hydrolyzed into glucose by cellobiase [3,6]. Although the crude cellulase has a lower specific activity than pure cellulase containing only one of ...
Oxidized low density lipoprotein inhibits the hemolytic activity of Asp
... phospholipids followed by the conversion of phosphatidylcholine to lysophosphatidylcholine [13]. Lysophosphatidylcholine is known to be a hemolytic agent. However, Sambrano et al. reported that oxidized LDL containing lysophosphatidylcholine caused erythrocyte crenation, but not hemolysis [9]. It is ...
... phospholipids followed by the conversion of phosphatidylcholine to lysophosphatidylcholine [13]. Lysophosphatidylcholine is known to be a hemolytic agent. However, Sambrano et al. reported that oxidized LDL containing lysophosphatidylcholine caused erythrocyte crenation, but not hemolysis [9]. It is ...
trimethoprim and sulfamethoxazole are selective inhibitors of cyp2c8
... drug metabolism (i) can be predicted by the Ki value and the concentration of the inhibitor [I] around the metabolic enzyme in the liver using the following scaling model: i ⫽ [I]/([I] ⫹ Ki), assuming that the substrate concentration is much lower than its Km value (von Moltke et al., 1998). After o ...
... drug metabolism (i) can be predicted by the Ki value and the concentration of the inhibitor [I] around the metabolic enzyme in the liver using the following scaling model: i ⫽ [I]/([I] ⫹ Ki), assuming that the substrate concentration is much lower than its Km value (von Moltke et al., 1998). After o ...
Advances in and applications of proteasome inhibitors
... With the recent US Food and Drug Administration approval of bortezomib (Velcade1) for the treatment of relapsed multiple myeloma, the proteasome has emerged as a new therapeutic target with diverse pathology. Drug discovery programs in academia and the pharmaceutical industry have developed a range ...
... With the recent US Food and Drug Administration approval of bortezomib (Velcade1) for the treatment of relapsed multiple myeloma, the proteasome has emerged as a new therapeutic target with diverse pathology. Drug discovery programs in academia and the pharmaceutical industry have developed a range ...
Structural and Functional Basis of
... heterocycle inhibitors celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] and rofecoxib (4-[4-(methylsulfonyl)phenyl]-3-phenyl-2(5H)-furanone).13,14 In addition to their reduced gastrointestinal toxicity profiles, several in vitro, in vivo, and clinical studies have demonstrated t ...
... heterocycle inhibitors celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] and rofecoxib (4-[4-(methylsulfonyl)phenyl]-3-phenyl-2(5H)-furanone).13,14 In addition to their reduced gastrointestinal toxicity profiles, several in vitro, in vivo, and clinical studies have demonstrated t ...
Journal home page: http://www.iajpr.com/index.php/en/ INDO
... Tremendous approved pharmacological activity of Aegle marmelos Antidiabetic activity Diabetes mellitus is metabolic disorder which independent risk factor for coronary artery disease, hypertension, myocardial infaraction & hyperlipidemia. Diabetes & its related complication are closely related with ...
... Tremendous approved pharmacological activity of Aegle marmelos Antidiabetic activity Diabetes mellitus is metabolic disorder which independent risk factor for coronary artery disease, hypertension, myocardial infaraction & hyperlipidemia. Diabetes & its related complication are closely related with ...
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... As well as other nanocarriers, the use of CD can increase drug solubility, bioavailability, safety, and stability of drug formulations [60]. Polymers provide even more versatility in nanocarriers engineering, being nanoparticles (NP), nanocapsules (NC), dendrimers and copolymer micelles among the nu ...
... As well as other nanocarriers, the use of CD can increase drug solubility, bioavailability, safety, and stability of drug formulations [60]. Polymers provide even more versatility in nanocarriers engineering, being nanoparticles (NP), nanocapsules (NC), dendrimers and copolymer micelles among the nu ...
Development of analogs of thalidomide
The development of analogs of thalidomide was precipitated by the discovery of the anti-angiogenic and anti-inflammatory properties of the drug yielding a new way of fighting cancer as well as some inflammatory diseases after it had been banned in 1961. The problems with thalidomide included; teratogenic side effects, high incidence of other adverse reactions, poor solubility in water and poor absorption from the intestines.In 1998 thalidomide was approved by the US Food and Drug Administration (FDA) for use in newly diagnosed multiple myeloma (MM) under strict regulations. This has led to the development of a number of analogs with fewer side effects and increased potency which include; lenalidomide, (currently marketed), pomalidomide and apremilast (currently marketed), all of which are manufactured by Celgene.