effects of cytochrome p450 enzyme inhibitors and inducers
... The human body eliminates foreign compounds primarily by metabolizing them to hydrophilic forms to facilitate effective excretion through the kidneys. Cytochrome P450 (CYP) enzymes in the liver and intestine contribute to the metabolism of many drugs. Pharmacokinetic drugdrug interactions occur if t ...
... The human body eliminates foreign compounds primarily by metabolizing them to hydrophilic forms to facilitate effective excretion through the kidneys. Cytochrome P450 (CYP) enzymes in the liver and intestine contribute to the metabolism of many drugs. Pharmacokinetic drugdrug interactions occur if t ...
In vitro and in vivo studies of artemisinin endoperoxides
... shown to exert cytotoxic effects, and lately, considerable attention has been focused on the demonstrated anticancer properties of these compounds [6-7]. ...
... shown to exert cytotoxic effects, and lately, considerable attention has been focused on the demonstrated anticancer properties of these compounds [6-7]. ...
Charles University in Prague Faculty of Pharmacy in Hradec Králové
... drug will be not toxic. The first-pass effect can be avoided either changing the route of drug administration or via structural modifications approaches in drug design. Once the drug has reached its site of action and achieved the desired objective, should be metabolized and eliminated at a reasonab ...
... drug will be not toxic. The first-pass effect can be avoided either changing the route of drug administration or via structural modifications approaches in drug design. Once the drug has reached its site of action and achieved the desired objective, should be metabolized and eliminated at a reasonab ...
Uses
... Cyclic peptides antibiotics The usual physiologically significant peptides are linear. Several bacterial species, however, produces antibiotic mixtures of cyclic peptides some with uncommon amino acids and some with common amino acids but with the D absolute stereochemistry. These cyclic substance ...
... Cyclic peptides antibiotics The usual physiologically significant peptides are linear. Several bacterial species, however, produces antibiotic mixtures of cyclic peptides some with uncommon amino acids and some with common amino acids but with the D absolute stereochemistry. These cyclic substance ...
TECTONA GRANDIS Research Article NEHA KHERA
... Lapachol isolated from Tectona grandis demonstrated highly significant activity against cancerous tumors in rats[37].Its antitumor property alone and in combination with radiation was evaluated in female Swiss albino mice, 6-8 weeks old, bearing sarcoma-180 (S-180) ascetic tumor cells. In female mic ...
... Lapachol isolated from Tectona grandis demonstrated highly significant activity against cancerous tumors in rats[37].Its antitumor property alone and in combination with radiation was evaluated in female Swiss albino mice, 6-8 weeks old, bearing sarcoma-180 (S-180) ascetic tumor cells. In female mic ...
SHOREA ROBUSTA EXPERIMENTALLY INDUCED ULCER MODELS Research Article
... S. robusta resin has been reported to contain several mono-, sesquiand tri-terpenoids includes ursolic acid, tri and tetrahydroxy ursenoic acid, asiatic acid, α and β-amyrin, α –amyrenone, mangiferonic acid, benthamic acid and uvaol [35]. In general triterpenoids like ursolic acid and amyrin are wel ...
... S. robusta resin has been reported to contain several mono-, sesquiand tri-terpenoids includes ursolic acid, tri and tetrahydroxy ursenoic acid, asiatic acid, α and β-amyrin, α –amyrenone, mangiferonic acid, benthamic acid and uvaol [35]. In general triterpenoids like ursolic acid and amyrin are wel ...
An Introduction to Medicinal Chemistry
... Drugs are grouped depending on the biological effect they have, e.g. analgesics, antipsychotics, antihypertensives, antiasthmatics, antibiotics, etc. This is useful if one wishes to know the full scope of drugs available for a certain ailment. However, it should be emphasized that such groupings con ...
... Drugs are grouped depending on the biological effect they have, e.g. analgesics, antipsychotics, antihypertensives, antiasthmatics, antibiotics, etc. This is useful if one wishes to know the full scope of drugs available for a certain ailment. However, it should be emphasized that such groupings con ...
sertraline is metabolized by multiple cytochrome p450 enzymes
... 5 mM; sertraline, 2 to 200 M; and UDPGA, 5 mM. Incubations were conducted in a Lucite container submerged in a heated water bath that permitted the continuous flow of CO2. The CO2 was passed through a gas warmer to prevent cooling of the incubations. After 45 min, incubations were terminated by the ...
... 5 mM; sertraline, 2 to 200 M; and UDPGA, 5 mM. Incubations were conducted in a Lucite container submerged in a heated water bath that permitted the continuous flow of CO2. The CO2 was passed through a gas warmer to prevent cooling of the incubations. After 45 min, incubations were terminated by the ...
Actions of bufalin and cinobufotalin, two bufadienolides respectively
... recently cinobufotalin has been reported to be less active than ouabain on this enzyme [8]. Ouabain is not the most toxic of the cardiac glycosides, but many studies have related activity of other molecules to that of ouabain, especially in relation to inhibition of Na+/K+-ATPase and the inhibition ...
... recently cinobufotalin has been reported to be less active than ouabain on this enzyme [8]. Ouabain is not the most toxic of the cardiac glycosides, but many studies have related activity of other molecules to that of ouabain, especially in relation to inhibition of Na+/K+-ATPase and the inhibition ...
Min2008 online
... inhibition of GSK3 (Jope, 2003; Phiel and Klein, 2001). Lithium directly inhibits GSK3, and this direct action is amplified in vivo by a subsequent increase in the inhibitory serine-phosphorylation of GSK3 (De Sarno et al., 2002). Several selective small molecule ATP-competitive inhibitors of GSK3 ha ...
... inhibition of GSK3 (Jope, 2003; Phiel and Klein, 2001). Lithium directly inhibits GSK3, and this direct action is amplified in vivo by a subsequent increase in the inhibitory serine-phosphorylation of GSK3 (De Sarno et al., 2002). Several selective small molecule ATP-competitive inhibitors of GSK3 ha ...
Simvastatin
... particle contains one molecule of apolipoprotein B, and since little apolipoprotein B is found in other lipoproteins, this strongly suggests that simvastatin does not merely cause cholesterol to be lost from LDL, but also reduces the concentration of circulating LDL particles. As a result of these c ...
... particle contains one molecule of apolipoprotein B, and since little apolipoprotein B is found in other lipoproteins, this strongly suggests that simvastatin does not merely cause cholesterol to be lost from LDL, but also reduces the concentration of circulating LDL particles. As a result of these c ...
Antiangiogenic Activity of N-substituted and
... phthalimido ring is crucial but not sufficient for potent angiogenesis and TNF-␣ inhibitory actions. Being a polar isostere of CPS49, the lack of biological activity of CPS48 might be attributed to its decreased lipophilicity. Niwayama et al. (21) reported that the increase in potency of the tetrafl ...
... phthalimido ring is crucial but not sufficient for potent angiogenesis and TNF-␣ inhibitory actions. Being a polar isostere of CPS49, the lack of biological activity of CPS48 might be attributed to its decreased lipophilicity. Niwayama et al. (21) reported that the increase in potency of the tetrafl ...
QA84_3_Folic_acid_methotrexate
... Methotrexate is a first line disease-modifying-anti-rheumatic-drug (DMARD) for rheumatoid arthritis (1,2); It is an antifolate agent with a chemical structure similar to that of folic acid and folinic acid (3), but its exact mechanism of action in treating this condition is unclear (3, 4, 5). Admini ...
... Methotrexate is a first line disease-modifying-anti-rheumatic-drug (DMARD) for rheumatoid arthritis (1,2); It is an antifolate agent with a chemical structure similar to that of folic acid and folinic acid (3), but its exact mechanism of action in treating this condition is unclear (3, 4, 5). Admini ...
Interactions between the cytochrome P450 system and
... 48.5% inhibition of clozapine metabolism; 42.0% inhibition was observed with the chemical CYP1A2 furafyline. Similarly, Olesen and Linnet42 noted significant inhibition of clozapine demethylation in vitro after incubation with fluvoxamine, a reaction catalyzed in vitro by CYP1A2, CYP2C9, CYP2C19, CY ...
... 48.5% inhibition of clozapine metabolism; 42.0% inhibition was observed with the chemical CYP1A2 furafyline. Similarly, Olesen and Linnet42 noted significant inhibition of clozapine demethylation in vitro after incubation with fluvoxamine, a reaction catalyzed in vitro by CYP1A2, CYP2C9, CYP2C19, CY ...
Prodrug Strategies of Antiviral Nucleotides
... For being just tiny simple particles, made up only of genetic material coated with protein, viruses cause a full spectrum of diseases from common cold to highly severe states, such as cancer. Vaccination is an effective method in preventing many viral infections. National vaccination programs give p ...
... For being just tiny simple particles, made up only of genetic material coated with protein, viruses cause a full spectrum of diseases from common cold to highly severe states, such as cancer. Vaccination is an effective method in preventing many viral infections. National vaccination programs give p ...
SUPERGEN INC (Form: DEFA14A, Received: 04/12
... Product License & Sub-license for Dacogen Executed worldwide (all indications) license agreement with MGI Pharma during 2004: 20-year license on a territory by territory basis from date of regulatory approval. During 2006, Dacogen approved by FDA and sub-license executed between MGI and JNJ. MGI wa ...
... Product License & Sub-license for Dacogen Executed worldwide (all indications) license agreement with MGI Pharma during 2004: 20-year license on a territory by territory basis from date of regulatory approval. During 2006, Dacogen approved by FDA and sub-license executed between MGI and JNJ. MGI wa ...
Clavulin - GlaxoSmithKline
... Activated charcoal may be administered to aid in the removal of unabsorbed drug. General supported measures are also recommended. Many patients have been asymptomatic following overdosage or have experienced primarily gastrointestinal symptoms including stomach and abdominal pain, vomiting, and diar ...
... Activated charcoal may be administered to aid in the removal of unabsorbed drug. General supported measures are also recommended. Many patients have been asymptomatic following overdosage or have experienced primarily gastrointestinal symptoms including stomach and abdominal pain, vomiting, and diar ...
Cytochrome P4502C9: an enzyme of major importance in human
... the CYP2C9 variants differ at only a few residues; the significance of the existence of allelic variants on CYP2C9 activity is discussed under ‘Pharmacogenetics’. The CYP2C9 cDNAs encode proteins of 490 amino acids which all have a calculated molecular mass of #55.6 KDa. Six substrate recognition si ...
... the CYP2C9 variants differ at only a few residues; the significance of the existence of allelic variants on CYP2C9 activity is discussed under ‘Pharmacogenetics’. The CYP2C9 cDNAs encode proteins of 490 amino acids which all have a calculated molecular mass of #55.6 KDa. Six substrate recognition si ...
PhD thesis
... adverse effects, is the aromatase enzyme (CYP19). CYP19 catalyses the conversion of androgens to estrogens and is vital for maintaining the sex steroid hormone balance. The aim of this thesis was to evaluate whether aromatase enzyme assays are useful as predictive tools for identify ...
... adverse effects, is the aromatase enzyme (CYP19). CYP19 catalyses the conversion of androgens to estrogens and is vital for maintaining the sex steroid hormone balance. The aim of this thesis was to evaluate whether aromatase enzyme assays are useful as predictive tools for identify ...
The challenge of selecting protein kinase assays
... human kinome [1]. As such, protein kinases represent the largest ‘druggable’ gene family within the human genome [2]. Overexpression and/or dysregulation of protein kinases result in many diseases, thus providing numerous targets for drug development [3]. Since 2001, the FDA has approved nine kinase ...
... human kinome [1]. As such, protein kinases represent the largest ‘druggable’ gene family within the human genome [2]. Overexpression and/or dysregulation of protein kinases result in many diseases, thus providing numerous targets for drug development [3]. Since 2001, the FDA has approved nine kinase ...
Full PDF - IOSR Journal of Pharmacy
... A medicinal plant is factually any plant which in one or more of its parts contains substances that can be used for therapeutic purposes or which are precursors for the synthesis of direct therapeutic purposes or which are precursors for the synthesis of direct therapeutic agents. At least 12,000 su ...
... A medicinal plant is factually any plant which in one or more of its parts contains substances that can be used for therapeutic purposes or which are precursors for the synthesis of direct therapeutic purposes or which are precursors for the synthesis of direct therapeutic agents. At least 12,000 su ...
- International Journal Of Pharmaceutical Sciences And
... Leaf-closing and leaf–opening substances were observed in several nyctinastic plants. Nyctinastic movement is regulated by a chemical substance that differs depending on the plant 2. Every family or subfamily of plants has its own leaf movement factor that is effective only for plants belonging to i ...
... Leaf-closing and leaf–opening substances were observed in several nyctinastic plants. Nyctinastic movement is regulated by a chemical substance that differs depending on the plant 2. Every family or subfamily of plants has its own leaf movement factor that is effective only for plants belonging to i ...
Lawsonia inermis Linnaeus - International Journal of
... inhibition in comparison with controls. Isoplumbagin showed significant anti- inflammatory activity similar to that of phenylbutazone. [68] Butanol and chloroform fractions showed more potent anti-inflammatory, analgesic and antipyretic effects than aqueous fraction of crude ethanol extract of L. in ...
... inhibition in comparison with controls. Isoplumbagin showed significant anti- inflammatory activity similar to that of phenylbutazone. [68] Butanol and chloroform fractions showed more potent anti-inflammatory, analgesic and antipyretic effects than aqueous fraction of crude ethanol extract of L. in ...
Asif, M., 2015. Pharmacological activities and
... the traditional use of these plants are discussed. Aegopodium podagraria showed only modest activity. Pure coumarins found in it, angelicin and apterin, failed to show any anti-inflammatory activity, and the total coumarin content was low, therefore the traditional use described in the literature as ...
... the traditional use of these plants are discussed. Aegopodium podagraria showed only modest activity. Pure coumarins found in it, angelicin and apterin, failed to show any anti-inflammatory activity, and the total coumarin content was low, therefore the traditional use described in the literature as ...