Inhibition of 17beta-hydroxysteroid dehydrogenases by
... converting steroids at positions 3, 5, 11, 17 and 20 of the steroid backbone [40–43]. The subject of this review is the influence of phytoestrogens on 17beta-hydroxysteroid dehydrogenases (17-HSD) in comparison to other steroid metabolising enzymes. By conversion at position 17 of the steroid molec ...
... converting steroids at positions 3, 5, 11, 17 and 20 of the steroid backbone [40–43]. The subject of this review is the influence of phytoestrogens on 17beta-hydroxysteroid dehydrogenases (17-HSD) in comparison to other steroid metabolising enzymes. By conversion at position 17 of the steroid molec ...
3.5 MB
... oestrus); (2) catabolic (metoestrus and dioestrus (Bronson et aZ. 1966). During the anabolic phase there is synthesis and growth of the uterine and glandular epithelia. At this period the uterus is under the influence of oestrogen and there is evidence that uterine ALP in the mouse is oestrogen-depe ...
... oestrus); (2) catabolic (metoestrus and dioestrus (Bronson et aZ. 1966). During the anabolic phase there is synthesis and growth of the uterine and glandular epithelia. At this period the uterus is under the influence of oestrogen and there is evidence that uterine ALP in the mouse is oestrogen-depe ...
Cytochrome P450 Inhibition
... concentration is there likely to be CYP inhibition? greater than 10times than Cmax. When concentration greater than Ki 3.Why was Saldane removed from the market? because its metabolism at CYP3A4 was inhibited by 3A4 inhibitor. Such as erythromycin. ...
... concentration is there likely to be CYP inhibition? greater than 10times than Cmax. When concentration greater than Ki 3.Why was Saldane removed from the market? because its metabolism at CYP3A4 was inhibited by 3A4 inhibitor. Such as erythromycin. ...
Effects of monosulfuron-ester on metabolic processes of nitrogen
... In general, cyanobacteria are very sensitive to herbicides because they possess many characteristics of higher plants.9 Previous study showed that cyanobacteria had different degrees of sensitivity to herbicides.10 However, the effect of monosulfuron-ester on nitrogen-fixing cyanobacteria that may p ...
... In general, cyanobacteria are very sensitive to herbicides because they possess many characteristics of higher plants.9 Previous study showed that cyanobacteria had different degrees of sensitivity to herbicides.10 However, the effect of monosulfuron-ester on nitrogen-fixing cyanobacteria that may p ...
CHAPTER 7 DETERMINATION OF THE ANTIMYCOBACTERIAL ACTIVITY OF THE FRACTIONS AND ISOLATED COMPOUNDS
... 6 week of infection, cell-mediated immunity (CMI) develops, and there is an influx of lymphocytes and activated macrophages into the lesion resulting in granuloma formation. The exponential growth of the bacilli is checked and dead macrophages form a caseum. The bacilli are contained in the caseous ...
... 6 week of infection, cell-mediated immunity (CMI) develops, and there is an influx of lymphocytes and activated macrophages into the lesion resulting in granuloma formation. The exponential growth of the bacilli is checked and dead macrophages form a caseum. The bacilli are contained in the caseous ...
PDF hosted at the Radboud Repository of the Radboud University
... inhibition of HDAC activity (19). However, HDAC inhibition did not influence the spontaneous cytokine production of RA synovial macrophages or intact synovial tissue explants. Interestingly, HDACi induced apoptosis in RA synovial macrophages by suppressing antiapoptotic Bfl-1 protein (19). It has be ...
... inhibition of HDAC activity (19). However, HDAC inhibition did not influence the spontaneous cytokine production of RA synovial macrophages or intact synovial tissue explants. Interestingly, HDACi induced apoptosis in RA synovial macrophages by suppressing antiapoptotic Bfl-1 protein (19). It has be ...
(embelin)-a second solid gold of india
... antifertility and antimicrobial. The present review exemplifies the collective knowledge on therapeutic, pharmacological and medicinal applications of embelin. The development of this knowledge with perspectives of conservation, efficacy, safety and quality this will help not only to preserve this t ...
... antifertility and antimicrobial. The present review exemplifies the collective knowledge on therapeutic, pharmacological and medicinal applications of embelin. The development of this knowledge with perspectives of conservation, efficacy, safety and quality this will help not only to preserve this t ...
S Theophylline again? Reasons for believing EDITORIAL
... individual doses to achieve this therapeutic range in our clinical practice. Interestingly, we now know that theophylline is in fact a weak bronchodilator, with an effective concentration giving a 50% response of 1.5610-4 M in vitro, which equates to a plasma concentration of 67 mg?L-1 assuming 60% ...
... individual doses to achieve this therapeutic range in our clinical practice. Interestingly, we now know that theophylline is in fact a weak bronchodilator, with an effective concentration giving a 50% response of 1.5610-4 M in vitro, which equates to a plasma concentration of 67 mg?L-1 assuming 60% ...
Optical isomerism - DrBravoChemistry
... • Chiral molecules often react differently with other chiral molecules. • This is like the idea that a right hand does not fit a left handed glove – the molecule must be the correct shape to fit the molecule it is reacting with. • Many natural molecules are chiral and most natural reactions are af ...
... • Chiral molecules often react differently with other chiral molecules. • This is like the idea that a right hand does not fit a left handed glove – the molecule must be the correct shape to fit the molecule it is reacting with. • Many natural molecules are chiral and most natural reactions are af ...
Beili B24 25 Insulin
... phenylalanine residues at positions B24 and B25 in insulin. The analogs were successfully prepared by SPPS from individual A and B chains, in total yields that varied between 1 and 10%. The relative binding affinity of this group of insulin analogs for the insulin receptor was determined to differ b ...
... phenylalanine residues at positions B24 and B25 in insulin. The analogs were successfully prepared by SPPS from individual A and B chains, in total yields that varied between 1 and 10%. The relative binding affinity of this group of insulin analogs for the insulin receptor was determined to differ b ...
O R I G I N A L A R T I C L E
... > tianeptine > moclobemide, cocaine >> lithium, valproate. MAO-B was inhibited by the following drugs: pargyline > clorgyline > iproniazid > fluoxetine > venlafaxine > amitriptyline > olanzapine > citalopram > desipramine > reboxetine > imipramine > tianeptine > mirtazapine, cocaine >> moclobemide, ...
... > tianeptine > moclobemide, cocaine >> lithium, valproate. MAO-B was inhibited by the following drugs: pargyline > clorgyline > iproniazid > fluoxetine > venlafaxine > amitriptyline > olanzapine > citalopram > desipramine > reboxetine > imipramine > tianeptine > mirtazapine, cocaine >> moclobemide, ...
Phyto Lec 16
... Colchicine is an effective treatment for acute attacks, but it is very toxic, and this restricts its general use. Colchicine binds to tubulin in the mitotic spindle, preventing polymerization and assembly into microtubules >>> potential anticancer activity. But the therapeutic index is very narrow, ...
... Colchicine is an effective treatment for acute attacks, but it is very toxic, and this restricts its general use. Colchicine binds to tubulin in the mitotic spindle, preventing polymerization and assembly into microtubules >>> potential anticancer activity. But the therapeutic index is very narrow, ...
Synthesis, Molecular Docking, and Biological Evaluation of Some
... some kidney and liver malfunctions were observed (2). The rise of selective COX-2 inhibitors reduced the risk of some of these side-effects (3), but other side-effects were also observed, and the most serious one was the capability of some drugs of causing cardiac arrest in some patients (4). But al ...
... some kidney and liver malfunctions were observed (2). The rise of selective COX-2 inhibitors reduced the risk of some of these side-effects (3), but other side-effects were also observed, and the most serious one was the capability of some drugs of causing cardiac arrest in some patients (4). But al ...
Bioisosterism: A Rational Approach in Drug Design
... instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review was to demonstrate the opportunities that one has in employing bioisosteres to gain more specif ...
... instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review was to demonstrate the opportunities that one has in employing bioisosteres to gain more specif ...
Enzyme
... b) carboxylases need ATP for their function c) kinases transfer a phosphate from an energy rich compound to a substrate d) hydroxylases catalyze oxidation of a substrate ...
... b) carboxylases need ATP for their function c) kinases transfer a phosphate from an energy rich compound to a substrate d) hydroxylases catalyze oxidation of a substrate ...
Lack of Susceptibility of Bicyclic Nucleoside Analogs, Highly Potent
... The separation of the BCNAs and their respective bases was performed by a linear gradient from 98% buffer B (50 mM NaH2PO4 ⫹ 5 mM heptane sulfonic acid, pH 3.2) ⫹ 2% buffer C (acetonitrile) to 20% buffer B ⫹ 80% buffer C. After injection of the samples, 98% buffer B ⫹ 2% buffer C was run for 2 min b ...
... The separation of the BCNAs and their respective bases was performed by a linear gradient from 98% buffer B (50 mM NaH2PO4 ⫹ 5 mM heptane sulfonic acid, pH 3.2) ⫹ 2% buffer C (acetonitrile) to 20% buffer B ⫹ 80% buffer C. After injection of the samples, 98% buffer B ⫹ 2% buffer C was run for 2 min b ...
Histamine and Antihistaminic Agents
... Possesses both antihistamine and antiserotonin. Antipruritic agent. Sedation as principal side effect. ...
... Possesses both antihistamine and antiserotonin. Antipruritic agent. Sedation as principal side effect. ...
DESIGN, SYNTHESIS AND MOLECULAR DOCKING STUDIES OF BENZOTHIAZOLE Research Article
... spectrum of biodynamic properties having potent clinical significance [4]. Schiff bases are currently been applied for the treatment of a number of disease condition. Though extensive research work has been reported on benzothiazole with Schiff base, relatively very little is known about the substit ...
... spectrum of biodynamic properties having potent clinical significance [4]. Schiff bases are currently been applied for the treatment of a number of disease condition. Though extensive research work has been reported on benzothiazole with Schiff base, relatively very little is known about the substit ...
Structure- Activity Relationships (SAR)
... In addition, the presence of a new group may introduce a new metabolic pathway for the analogue. • These changes will in turn affect the pharmacodynamic properties of the analogue. For example, they could result in an analogue with either increased or decreased • potency, duration of action, metabol ...
... In addition, the presence of a new group may introduce a new metabolic pathway for the analogue. • These changes will in turn affect the pharmacodynamic properties of the analogue. For example, they could result in an analogue with either increased or decreased • potency, duration of action, metabol ...
Thrombin = anticoagulant
... Total daily rivaroxaban doses of 5–20 mg had similar efficacy and safety to enoxaparin ...
... Total daily rivaroxaban doses of 5–20 mg had similar efficacy and safety to enoxaparin ...
Evaluation of anti-inflammatory potential of Nardostachys jatamansi
... Where Vc and Vt represent the mean increase in paw volume in control and treated groups, respectively. 2.4.1.2. Autacoids-induced hind paw oedema in rats This experiment was conducted as per the methodology used by Singh and Pandey[12]. The autacoids, viz., histamine (1 mg/mL), 5-HT (1 mg/mL), PGE2 ...
... Where Vc and Vt represent the mean increase in paw volume in control and treated groups, respectively. 2.4.1.2. Autacoids-induced hind paw oedema in rats This experiment was conducted as per the methodology used by Singh and Pandey[12]. The autacoids, viz., histamine (1 mg/mL), 5-HT (1 mg/mL), PGE2 ...
A conformationally restricted uniconazole analogue as a specific
... compounds are not ideal inhibitors of a specific enzyme. Azole inhibitors of P450 bind to the target P450 active site by both coordinating to the heme-iron atom and interacting with surrounding protein residues. Because heme coordination is a common property of azole inhibitors, their affinity and s ...
... compounds are not ideal inhibitors of a specific enzyme. Azole inhibitors of P450 bind to the target P450 active site by both coordinating to the heme-iron atom and interacting with surrounding protein residues. Because heme coordination is a common property of azole inhibitors, their affinity and s ...
- Journal of Pharmacognosy and Phytochemistry
... induced writhing test in Wistar rats for seven days orally and standard group rats were administered diclofenac sodium (10mg/kg per orally) one hour before study on seventh day. The drug showed significant analgesic activity when compared to standard drug (Saha et al, 2012) [17]. 6.8 Anti-allergic a ...
... induced writhing test in Wistar rats for seven days orally and standard group rats were administered diclofenac sodium (10mg/kg per orally) one hour before study on seventh day. The drug showed significant analgesic activity when compared to standard drug (Saha et al, 2012) [17]. 6.8 Anti-allergic a ...
Natural Products for the Treatment of Trachoma and Chlamydia
... settings of poverty, they are chronic conditions, they often disable rather than kill, they have existed for centuries, and they promote poverty through their debilitating effects [2]. Due to the complex social and economic factors related to these conditions, plans have been developed to address th ...
... settings of poverty, they are chronic conditions, they often disable rather than kill, they have existed for centuries, and they promote poverty through their debilitating effects [2]. Due to the complex social and economic factors related to these conditions, plans have been developed to address th ...
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.