A.S.M. Anisuzzaman - Academia.edu (original) (raw)
Papers by A.S.M. Anisuzzaman
Serum glutamic oxaloacetic transaminase
The present work carried out the study to investigate the antihyperglycemic, oral glucose toleran... more The present work carried out the study to investigate the antihyperglycemic, oral glucose tolerance test (OGTT) and glycogenesis effects of the different fractions (Petroleum ether, ethyl acetate and chloroform) of ethanolic extract of Brassica oleracea. The different fractions of the extract were administered intraperitoneally as a single dose of 150 mg/kg body weight to alloxan induced as well as glucose induced diabetic rats and found to reduce blood glucose level significantly (p<0.05). The different fractions of Brassica oleracea to the alloxaninduced diabetic rats resulted in the significant elevation of liver glycogen content which was decreased by 49% in diabetic control. The plant fractions also improve the glucose tolerance in the glucose induced rats. The effects of plant fractions were compared with standard drug metformin. The phytochemical screening tests indicated that the different constituents such as saponins, tannins, triterpenes, alkaloids and flavonoids etc. ...
Pleurotus osteratus (family: Pleurotaceae) and Ganoderma lucidum (family: ganodermataceae) are co... more Pleurotus osteratus (family: Pleurotaceae) and Ganoderma lucidum (family: ganodermataceae) are common edible mushrooms in Bangladesh. Ethyl acetate extract of Pleurotus osteratus and Ganoderma lucidum were used to find out their hypolipidemic and hepatoprotective activity in alloxan induced diabetic mice and normal mice. Lipid profile namely LDL, TG and TC level significantly reduced after 24 hours by the intraperitoneal administration of these extracts in normal and diabetic mice whereas equipotently increased HLD level in both cases. Further, diabetic condition increases alanine aminotransferase ALT/SGPT and aspartate aminotransferase AST/SGOT enzyme level in liver. Present treatment also showed that both the oyster and reishi has significantly inhibited the rise of both serum liver enzymes in the treated mice compared to controls.
The Journal of Phytopharmacology
In this study we have evaluated the nutritional analysisand mineral content of two varieties of m... more In this study we have evaluated the nutritional analysisand mineral content of two varieties of mushroom species include oyster (Pleurotus ostreatus) and Reshii (Ganoderma lucidum). The mushroom varieties were harvested and dried, then taken to the laboratory for proximate and mineral analysis by standard assay methods. For both mushrooms the nutritional composition was analyzed namely pH, moisture content, crude fibre, ash, water soluble protein, total lipid, total soluble sugar, reducing sugar, non-reducing sugar and starch content. However ten mineral elements were analyzed: potassium, calcium, magnesium, sodium, phosphorus, sulfur, cupper, iron, manganese and zinc having no significance difference in values of both mushroom species. Based on the result these mushrooms have high nutrient potentials hence it will serve as a good means of reducing the incidence and high prevalence of malnutrition in Bangladesh since it is a cheap food source that is within the reach of the poor.
The Journal of Phytopharmacology
Ethyl acetate extracts of the reishi (Ganoderma lucidum) and oyster (Pleurotus ostreatus) mushroo... more Ethyl acetate extracts of the reishi (Ganoderma lucidum) and oyster (Pleurotus ostreatus) mushrooms were tested for their in vitro growth inhibitory activity against a panel of microorganisms of reference strains. Antimicrobial effects of both mushrooms were monitored in the dose of 400 micro gm /disc by disc diffusion method using five Gram-positive bacteria, five Gram-negative bacteria and three fungi as well. Present study showed that ethyl acetate extract of Pleurotus ostreatus has moderate and Ganoderma lucidum has only mild antibacterial effect in comparison with standard Kanamycin (30 gm. /disc). However, both mushrooms had no antifungal activity on the experimental fungi compared with standard drug Nystatin at the dose of 30 gm. /disc.
Journal of Scientific Research, 2014
Six marketed oral antidiabetic metformin tablets in Bangladesh have been studied for their drug c... more Six marketed oral antidiabetic metformin tablets in Bangladesh have been studied for their drug content, release profile and glucose lowering capacities. This sort of study is a good indicator for in vivo evaluation of the quality of an oral antidiabetic preparation. Marketed preparations of metformin-HCl from different manufacturers were randomly chosen for this study. The drug content was within the United State Pharmacopoeia (USP) specified limit (95-105%) in all cases. The blood glucose levels were investigated in streptozotocin-induced diabetic rats (SIDRs) after 5 hours of single dose (110 mg/kg body weight) treatment of the products; significantly (p<0.05) reduced blood glucose level by 58.1, 53.2, 50.8, 77.0, 72.9 and 49.1%, respectively; which were consistent with antihyperglycemic effects of standard metformin-HCl (71.3%). All the products were found to be qualified in lowering blood glucose level. It may be inferred that the metformin-HCl tablets of Bangladeshi manufac...
African Journal of Clinical and Experimental Microbiology, 2012
Body odour caused by bacterial growth is of great concern to those affected. To ameliorate this, ... more Body odour caused by bacterial growth is of great concern to those affected. To ameliorate this, deodorants, which are substances applied to avert body odour, are designed and used. These deodorants are claimed to have antibacterial activities. This work was therefore, carried out to determine the antibacterial activities of the deodorants marketed in Owerri municipality. Owerri is the capital of Imo State of Nigeria. To determine this, twenty (20) deodorants from ten (10) different manufacturers made up of fourteen (14) roll-on and six (6) sprays were assessed using punch-hole plate diffusion technique on nutrient agar plates. The deodorants were purchased from Ekeonunwa market, New market, Relief market, and some supper markets, all in Owerri Municipality. These deodorants were tested against Laboratory isolates of Staphylococcus epidermidis, Pseudomonas aeruginosa, Escherichia coli and Proteus mirabilis obtained from Federal Medical Centre (FMC) and Modesty Medical Laboratory Owerri and reconfirmed using morphological and biochemical tests. Out of the twenty (20) deodorants tested, 18 (90%) were active against the organisms, 17 (85%) were active against Staphylococcus epidermidis, 15 (75%) against P. mirabilis, 11 (55%) against E. coli and 10 (50%) against P. aeruginosa. It was also observed that deodorants "roll-on" were more active 14 (100%) than the deodorants "sprays" 4 (66.6%). From this study, it was observed that the deodorants tested had antibacterial activities.
Journal of Medical Sciences(Faisalabad), 2001
![Research paper thumbnail of Characterization and in vitro Antimicrobial Activity of 17-jS-hydroxy-14, 20-epoxy-1-oxo-[22R]-3/J-[0-j3-d-glucopyranosyl]-5, 24-withadienolide from Venda …](https://attachments.academia-assets.com/83858480/thumbnails/1.jpg)
](aseanbiodiversity.info, 2001
British Journal of Pharmacology, 2009
Background and purpose: The expression of multiple pharmacological phenotypes including a1L-adren... more Background and purpose: The expression of multiple pharmacological phenotypes including a1L-adrenoceptor has recently been reported for a1-adrenoceptors. The purpose of the present study was to identify a1-adrenoceptor phenotypes in the irises of pigmented and albino rabbits. Experimental approach: Radioligand binding and functional bioassay experiments were performed in segments or strips of iris of pigmented and albino rabbits, and their pharmacological profiles were compared. Key results: [ 3 H]-silodosin at subnanomolar concentrations bound to intact segments of iris of pigmented and albino rabbits at similar densities (approximately 240 fmol•mg-1 protein). The binding sites in the iris of a pigmented rabbit were composed of a single component showing extremely low affinities for prazosin, hydrochloride [N-[2-(2cyclopropylmethoxyphenoxy)ethyl]-5-chloro-a,a-dimethyl-1H-indole-3-ethamine hydrochloride (RS-17053)] and 5-methylurapidil, while two components with high and low affinities for prazosin, RS-17053 and 5-methylurapidil were identified in irises from albino rabbits. In contrast, specific binding sites for [ 3 H]-prazosin were not clearly detected because a high proportion of non-specific binding and/or low affinity for prazosin occurred. Contractile responses of iris dilator muscle to noradrenaline were antagonized by the above ligands, and their antagonist affinities were consistent with the binding estimates at low-affinity sites identified in both strains of rabbits. Conclusions and implications: A typical a1L phenotype with extremely low affinity for prazosin is exclusively expressed in the iris of pigmented rabbits, while two distinct phenotypes (a1A and a1L) with high and moderate affinities for prazosin are co-expressed in the iris of albino rabbits. This suggests that a significant difference in the expression of phenotypes of the a1-adrenoceptor occurs in the irises between the two strains of rabbits.
British Journal of Pharmacology, 2012
British Journal of Pharmacology, 2008
Background and purpose: The a 1L-adrenoceptor has pharmacological properties that distinguish it ... more Background and purpose: The a 1L-adrenoceptor has pharmacological properties that distinguish it from three classical a 1-adrenoceptors (a 1A , a 1B and a 1D). The purpose of this was to identify a 1L-adrenoceptors in mice and to examine their relationship to classical a 1-adrenoceptors. Experimental approach: Radioligand binding and functional bioassay experiments were performed on the cerebral cortex, vas deferens and prostate of wild-type (WT) and a 1A-, a 1B-and a 1D-adrenoceptor gene knockout (AKO, BKO and DKO) mice. Key results: The radioligand [ 3 H]-silodosin bound to intact segments of the cerebral cortex, vas deferens and prostate of WT, BKO and DKO but not of AKO mice. The binding sites were composed of two components with high and low affinities for prazosin or RS-17053, indicating the pharmacological profiles of a 1A-adrenoceptors and a 1L-adrenoceptors. In membrane preparations of WT mouse cortex, however, [ 3 H]-silodosin bound to a single population of prazosin high-affinity sites, suggesting the presence of a 1A-adrenoceptors alone. In contrast, [ 3 H]-prazosin bound to two components having a 1A-adrenoceptor and a 1B-adrenoceptor profiles in intact segments of WT and DKO mouse cortices, but AKO mice lacked a 1A-adrenoceptor profiles and BKO mice lacked a 1B-adrenoceptor profiles. Noradrenaline produced contractions through a 1L-adrenoceptors with low affinity for prazosin in the vas deferens and prostate of WT, BKO and DKO mice. However, the contractions were abolished or markedly attenuated in AKO mice. Conclusions and implications: a 1L-Adrenoceptors were identified as binding and functional entities in WT, BKO and DKO mice but not in AKO mice, suggesting that the a 1L-adrenoceptor is one phenotype derived from the a 1A-adrenoceptor gene.
British Journal of Pharmacology, 2008
alpha(1)-Adrenoceptors in the rabbit prostate have been studied because of their controversial ph... more alpha(1)-Adrenoceptors in the rabbit prostate have been studied because of their controversial pharmacological profiles in functional and radioligand binding studies. The purpose of the present study is to determine the native profiles of alpha(1)-adrenoceptor phenotypes and to clarify their relationship. Binding experiments with [3H]-silodosin and [3H]-prazosin were performed using intact tissue segments and crude membrane preparations of rabbit prostate and the results were compared with alpha(1)-adrenoceptor-mediated prostate contraction. [3H]-Silodosin at subnanomolar concentrations bound specifically to intact tissue segments of rabbit prostate. However, [3H]-prazosin at the same range of concentrations failed to bind to alpha(1)-adrenoceptors of intact segments. Binding sites of [3H]-silodosin in intact segments were composed of alpha(1L) phenotype with low affinities for prazosin (pKi=7.1), 5-methyurapidil and N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha,alpha-dimethyl-1H-indole-3-ethamine hydrochloride (RS-17053), and alpha(1A)-like phenotype with moderate affinity for prazosin (pKi=8.8) but high affinity for 5-methyurapidil and RS-17053. In contrast, both radioligands bound to a single population of alpha(1)-adrenoceptors in the membrane preparations at the same density with a subnanomolar affinity, showing a typical profile of &amp;#39;classical&amp;#39; alpha(1A)-adrenoceptors (pKi for prazosin=9.8). The pharmacological profile of alpha(1)-adrenoceptor-mediated prostate contraction was in accord with the alpha(1L) phenotype observed by intact segment binding approach. Three distinct phenotypes (alpha(1L) and alpha(1A)-like phenotypes in the intact segments and a classical alpha(1A) phenotype in the membranes) with different affinities for prazosin were detected in rabbit prostate. It appears that the three phenotypes are phenotypic subtypes of alpha(1A)-adrenoceptors, but are not genetically different subtypes.
British Journal of Pharmacology, 2012
a1-Adrenoceptors are involved in numerous physiological functions, including micturition. However... more a1-Adrenoceptors are involved in numerous physiological functions, including micturition. However, the pharmacological profile of the a1-adrenoceptor subtypes remains controversial. Here, we review the literature regarding a1-adrenoceptors in the lower urinary tract from the standpoint of a1L phenotype pharmacology. Among three a1-adrenoceptor subtypes (a1A, a1B and a1D), a1a-adrenoceptor mRNA is the most abundantly transcribed in the prostate, urethra and bladder neck of many species, including humans. In prostate homogenates or membrane preparations, a1A-adrenoceptors with high affinity for prazosin have been detected as radioligand binding sites. Functional a1-adrenoceptors in the prostate, urethra and bladder neck have low affinity for prazosin, suggesting the presence of an atypical a1-adrenoceptor phenotype (designated as a1L). The a1L-adrenoceptor occurs as a distinct binding entity from the a1A-adrenoceptor in intact segments of variety of tissues including prostate. Both the a1Land a1A-adrenoceptors are specifically absent from Adra1A (a1a) gene-knockout mice. Transfection of a1a-adrenoceptor cDNA predominantly expresses a1A-phenotype in several cultured cell lines. However, in CHO cells, such transfection expresses a1Land a1A-phenotypes. Under intact cell conditions, the a1L-phenotype is predominant when co-expressed with the receptor interacting protein, CRELD1a. In summary, recent pharmacological studies reveal that two distinct a1-adrenoceptor phenotypes (a1A and a1L) originate from a single Adra1A (a1a-adrenoceptor) gene, but adrenergic contractions in the lower urinary tract are predominantly mediated via the a1L-adrenoceptor. From the standpoint of phenotype pharmacology, it is likely that phenotype-based subtypes such as the a1L-adrenoceptor will become new targets for drug development and pharmacotherapy.
Journal of Scientific Research, 2009
Methocel K15 MCR (a modified hydroxypropylmethylcellulose) matrix tablets of pentoxifylline using... more Methocel K15 MCR (a modified hydroxypropylmethylcellulose) matrix tablets of pentoxifylline using microcrystalline cellulose (MCC), starch and lactose were prepared by wet granulation process. There was no significant difference in drug release between the hydrophilic matrices when the Methocel K15 MCR concentration was modified in low percentage. The release of pentoxifylline was influenced by the presence of microcrystalline cellulose, and by the different concentrations of starch and lactose. The data obtained proved that the formulation with 12.5% Methocel K15 MCR and 20% lactose is more useful for a controlled release pentoxifylline, due to the percentage released after 8 hours is nearly to 65%. There was no significant change on release profile after three months storage of tablets. The best-fit release kinetics was achieved with the Higuchi model, followed by the first-order plot.
Journal of Scientific Research, Dec 29, 2012
Ethanolic extracts of some fruits of Cucurbitaceae family such as Cucumis sativus (cucumber), Lag... more Ethanolic extracts of some fruits of Cucurbitaceae family such as Cucumis sativus (cucumber), Lagenaria siceraria (white pumpkin), Luffa acutangula (ridge gourd), Benincasa hispida (ash gourd), Citrullus lanatus (sweet melon) and Cucarbita maxima (pumpkin) have been studied for their hypoglycemic effects on alloxan induced diabetic rats (AIDRs). Screening results suggested that among the tested fruits the hypoglycemic potency follows: cucumber> white pumpkin> ridge gourd. These three fruit-extracts were further ...
International Journal
The antidiabetic effects of Ethyl acetate (Et Ac), Petroleum-ether (Pet ether), and Chloroform fr... more The antidiabetic effects of Ethyl acetate (Et Ac), Petroleum-ether (Pet ether), and Chloroform fractions from methanolic extract of the seeds of Entada phaseoloides were investigated in alloxan induced diabetic mice (AIDM). The effect of these fractions (200 mg ...
Serum glutamic oxaloacetic transaminase
The present work carried out the study to investigate the antihyperglycemic, oral glucose toleran... more The present work carried out the study to investigate the antihyperglycemic, oral glucose tolerance test (OGTT) and glycogenesis effects of the different fractions (Petroleum ether, ethyl acetate and chloroform) of ethanolic extract of Brassica oleracea. The different fractions of the extract were administered intraperitoneally as a single dose of 150 mg/kg body weight to alloxan induced as well as glucose induced diabetic rats and found to reduce blood glucose level significantly (p<0.05). The different fractions of Brassica oleracea to the alloxaninduced diabetic rats resulted in the significant elevation of liver glycogen content which was decreased by 49% in diabetic control. The plant fractions also improve the glucose tolerance in the glucose induced rats. The effects of plant fractions were compared with standard drug metformin. The phytochemical screening tests indicated that the different constituents such as saponins, tannins, triterpenes, alkaloids and flavonoids etc. ...
Pleurotus osteratus (family: Pleurotaceae) and Ganoderma lucidum (family: ganodermataceae) are co... more Pleurotus osteratus (family: Pleurotaceae) and Ganoderma lucidum (family: ganodermataceae) are common edible mushrooms in Bangladesh. Ethyl acetate extract of Pleurotus osteratus and Ganoderma lucidum were used to find out their hypolipidemic and hepatoprotective activity in alloxan induced diabetic mice and normal mice. Lipid profile namely LDL, TG and TC level significantly reduced after 24 hours by the intraperitoneal administration of these extracts in normal and diabetic mice whereas equipotently increased HLD level in both cases. Further, diabetic condition increases alanine aminotransferase ALT/SGPT and aspartate aminotransferase AST/SGOT enzyme level in liver. Present treatment also showed that both the oyster and reishi has significantly inhibited the rise of both serum liver enzymes in the treated mice compared to controls.
The Journal of Phytopharmacology
In this study we have evaluated the nutritional analysisand mineral content of two varieties of m... more In this study we have evaluated the nutritional analysisand mineral content of two varieties of mushroom species include oyster (Pleurotus ostreatus) and Reshii (Ganoderma lucidum). The mushroom varieties were harvested and dried, then taken to the laboratory for proximate and mineral analysis by standard assay methods. For both mushrooms the nutritional composition was analyzed namely pH, moisture content, crude fibre, ash, water soluble protein, total lipid, total soluble sugar, reducing sugar, non-reducing sugar and starch content. However ten mineral elements were analyzed: potassium, calcium, magnesium, sodium, phosphorus, sulfur, cupper, iron, manganese and zinc having no significance difference in values of both mushroom species. Based on the result these mushrooms have high nutrient potentials hence it will serve as a good means of reducing the incidence and high prevalence of malnutrition in Bangladesh since it is a cheap food source that is within the reach of the poor.
The Journal of Phytopharmacology
Ethyl acetate extracts of the reishi (Ganoderma lucidum) and oyster (Pleurotus ostreatus) mushroo... more Ethyl acetate extracts of the reishi (Ganoderma lucidum) and oyster (Pleurotus ostreatus) mushrooms were tested for their in vitro growth inhibitory activity against a panel of microorganisms of reference strains. Antimicrobial effects of both mushrooms were monitored in the dose of 400 micro gm /disc by disc diffusion method using five Gram-positive bacteria, five Gram-negative bacteria and three fungi as well. Present study showed that ethyl acetate extract of Pleurotus ostreatus has moderate and Ganoderma lucidum has only mild antibacterial effect in comparison with standard Kanamycin (30 gm. /disc). However, both mushrooms had no antifungal activity on the experimental fungi compared with standard drug Nystatin at the dose of 30 gm. /disc.
Journal of Scientific Research, 2014
Six marketed oral antidiabetic metformin tablets in Bangladesh have been studied for their drug c... more Six marketed oral antidiabetic metformin tablets in Bangladesh have been studied for their drug content, release profile and glucose lowering capacities. This sort of study is a good indicator for in vivo evaluation of the quality of an oral antidiabetic preparation. Marketed preparations of metformin-HCl from different manufacturers were randomly chosen for this study. The drug content was within the United State Pharmacopoeia (USP) specified limit (95-105%) in all cases. The blood glucose levels were investigated in streptozotocin-induced diabetic rats (SIDRs) after 5 hours of single dose (110 mg/kg body weight) treatment of the products; significantly (p<0.05) reduced blood glucose level by 58.1, 53.2, 50.8, 77.0, 72.9 and 49.1%, respectively; which were consistent with antihyperglycemic effects of standard metformin-HCl (71.3%). All the products were found to be qualified in lowering blood glucose level. It may be inferred that the metformin-HCl tablets of Bangladeshi manufac...
African Journal of Clinical and Experimental Microbiology, 2012
Body odour caused by bacterial growth is of great concern to those affected. To ameliorate this, ... more Body odour caused by bacterial growth is of great concern to those affected. To ameliorate this, deodorants, which are substances applied to avert body odour, are designed and used. These deodorants are claimed to have antibacterial activities. This work was therefore, carried out to determine the antibacterial activities of the deodorants marketed in Owerri municipality. Owerri is the capital of Imo State of Nigeria. To determine this, twenty (20) deodorants from ten (10) different manufacturers made up of fourteen (14) roll-on and six (6) sprays were assessed using punch-hole plate diffusion technique on nutrient agar plates. The deodorants were purchased from Ekeonunwa market, New market, Relief market, and some supper markets, all in Owerri Municipality. These deodorants were tested against Laboratory isolates of Staphylococcus epidermidis, Pseudomonas aeruginosa, Escherichia coli and Proteus mirabilis obtained from Federal Medical Centre (FMC) and Modesty Medical Laboratory Owerri and reconfirmed using morphological and biochemical tests. Out of the twenty (20) deodorants tested, 18 (90%) were active against the organisms, 17 (85%) were active against Staphylococcus epidermidis, 15 (75%) against P. mirabilis, 11 (55%) against E. coli and 10 (50%) against P. aeruginosa. It was also observed that deodorants "roll-on" were more active 14 (100%) than the deodorants "sprays" 4 (66.6%). From this study, it was observed that the deodorants tested had antibacterial activities.
Journal of Medical Sciences(Faisalabad), 2001
aseanbiodiversity.info, 2001
British Journal of Pharmacology, 2009
Background and purpose: The expression of multiple pharmacological phenotypes including a1L-adren... more Background and purpose: The expression of multiple pharmacological phenotypes including a1L-adrenoceptor has recently been reported for a1-adrenoceptors. The purpose of the present study was to identify a1-adrenoceptor phenotypes in the irises of pigmented and albino rabbits. Experimental approach: Radioligand binding and functional bioassay experiments were performed in segments or strips of iris of pigmented and albino rabbits, and their pharmacological profiles were compared. Key results: [ 3 H]-silodosin at subnanomolar concentrations bound to intact segments of iris of pigmented and albino rabbits at similar densities (approximately 240 fmol•mg-1 protein). The binding sites in the iris of a pigmented rabbit were composed of a single component showing extremely low affinities for prazosin, hydrochloride [N-[2-(2cyclopropylmethoxyphenoxy)ethyl]-5-chloro-a,a-dimethyl-1H-indole-3-ethamine hydrochloride (RS-17053)] and 5-methylurapidil, while two components with high and low affinities for prazosin, RS-17053 and 5-methylurapidil were identified in irises from albino rabbits. In contrast, specific binding sites for [ 3 H]-prazosin were not clearly detected because a high proportion of non-specific binding and/or low affinity for prazosin occurred. Contractile responses of iris dilator muscle to noradrenaline were antagonized by the above ligands, and their antagonist affinities were consistent with the binding estimates at low-affinity sites identified in both strains of rabbits. Conclusions and implications: A typical a1L phenotype with extremely low affinity for prazosin is exclusively expressed in the iris of pigmented rabbits, while two distinct phenotypes (a1A and a1L) with high and moderate affinities for prazosin are co-expressed in the iris of albino rabbits. This suggests that a significant difference in the expression of phenotypes of the a1-adrenoceptor occurs in the irises between the two strains of rabbits.
British Journal of Pharmacology, 2012
British Journal of Pharmacology, 2008
Background and purpose: The a 1L-adrenoceptor has pharmacological properties that distinguish it ... more Background and purpose: The a 1L-adrenoceptor has pharmacological properties that distinguish it from three classical a 1-adrenoceptors (a 1A , a 1B and a 1D). The purpose of this was to identify a 1L-adrenoceptors in mice and to examine their relationship to classical a 1-adrenoceptors. Experimental approach: Radioligand binding and functional bioassay experiments were performed on the cerebral cortex, vas deferens and prostate of wild-type (WT) and a 1A-, a 1B-and a 1D-adrenoceptor gene knockout (AKO, BKO and DKO) mice. Key results: The radioligand [ 3 H]-silodosin bound to intact segments of the cerebral cortex, vas deferens and prostate of WT, BKO and DKO but not of AKO mice. The binding sites were composed of two components with high and low affinities for prazosin or RS-17053, indicating the pharmacological profiles of a 1A-adrenoceptors and a 1L-adrenoceptors. In membrane preparations of WT mouse cortex, however, [ 3 H]-silodosin bound to a single population of prazosin high-affinity sites, suggesting the presence of a 1A-adrenoceptors alone. In contrast, [ 3 H]-prazosin bound to two components having a 1A-adrenoceptor and a 1B-adrenoceptor profiles in intact segments of WT and DKO mouse cortices, but AKO mice lacked a 1A-adrenoceptor profiles and BKO mice lacked a 1B-adrenoceptor profiles. Noradrenaline produced contractions through a 1L-adrenoceptors with low affinity for prazosin in the vas deferens and prostate of WT, BKO and DKO mice. However, the contractions were abolished or markedly attenuated in AKO mice. Conclusions and implications: a 1L-Adrenoceptors were identified as binding and functional entities in WT, BKO and DKO mice but not in AKO mice, suggesting that the a 1L-adrenoceptor is one phenotype derived from the a 1A-adrenoceptor gene.
British Journal of Pharmacology, 2008
alpha(1)-Adrenoceptors in the rabbit prostate have been studied because of their controversial ph... more alpha(1)-Adrenoceptors in the rabbit prostate have been studied because of their controversial pharmacological profiles in functional and radioligand binding studies. The purpose of the present study is to determine the native profiles of alpha(1)-adrenoceptor phenotypes and to clarify their relationship. Binding experiments with [3H]-silodosin and [3H]-prazosin were performed using intact tissue segments and crude membrane preparations of rabbit prostate and the results were compared with alpha(1)-adrenoceptor-mediated prostate contraction. [3H]-Silodosin at subnanomolar concentrations bound specifically to intact tissue segments of rabbit prostate. However, [3H]-prazosin at the same range of concentrations failed to bind to alpha(1)-adrenoceptors of intact segments. Binding sites of [3H]-silodosin in intact segments were composed of alpha(1L) phenotype with low affinities for prazosin (pKi=7.1), 5-methyurapidil and N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha,alpha-dimethyl-1H-indole-3-ethamine hydrochloride (RS-17053), and alpha(1A)-like phenotype with moderate affinity for prazosin (pKi=8.8) but high affinity for 5-methyurapidil and RS-17053. In contrast, both radioligands bound to a single population of alpha(1)-adrenoceptors in the membrane preparations at the same density with a subnanomolar affinity, showing a typical profile of &amp;#39;classical&amp;#39; alpha(1A)-adrenoceptors (pKi for prazosin=9.8). The pharmacological profile of alpha(1)-adrenoceptor-mediated prostate contraction was in accord with the alpha(1L) phenotype observed by intact segment binding approach. Three distinct phenotypes (alpha(1L) and alpha(1A)-like phenotypes in the intact segments and a classical alpha(1A) phenotype in the membranes) with different affinities for prazosin were detected in rabbit prostate. It appears that the three phenotypes are phenotypic subtypes of alpha(1A)-adrenoceptors, but are not genetically different subtypes.
British Journal of Pharmacology, 2012
a1-Adrenoceptors are involved in numerous physiological functions, including micturition. However... more a1-Adrenoceptors are involved in numerous physiological functions, including micturition. However, the pharmacological profile of the a1-adrenoceptor subtypes remains controversial. Here, we review the literature regarding a1-adrenoceptors in the lower urinary tract from the standpoint of a1L phenotype pharmacology. Among three a1-adrenoceptor subtypes (a1A, a1B and a1D), a1a-adrenoceptor mRNA is the most abundantly transcribed in the prostate, urethra and bladder neck of many species, including humans. In prostate homogenates or membrane preparations, a1A-adrenoceptors with high affinity for prazosin have been detected as radioligand binding sites. Functional a1-adrenoceptors in the prostate, urethra and bladder neck have low affinity for prazosin, suggesting the presence of an atypical a1-adrenoceptor phenotype (designated as a1L). The a1L-adrenoceptor occurs as a distinct binding entity from the a1A-adrenoceptor in intact segments of variety of tissues including prostate. Both the a1Land a1A-adrenoceptors are specifically absent from Adra1A (a1a) gene-knockout mice. Transfection of a1a-adrenoceptor cDNA predominantly expresses a1A-phenotype in several cultured cell lines. However, in CHO cells, such transfection expresses a1Land a1A-phenotypes. Under intact cell conditions, the a1L-phenotype is predominant when co-expressed with the receptor interacting protein, CRELD1a. In summary, recent pharmacological studies reveal that two distinct a1-adrenoceptor phenotypes (a1A and a1L) originate from a single Adra1A (a1a-adrenoceptor) gene, but adrenergic contractions in the lower urinary tract are predominantly mediated via the a1L-adrenoceptor. From the standpoint of phenotype pharmacology, it is likely that phenotype-based subtypes such as the a1L-adrenoceptor will become new targets for drug development and pharmacotherapy.
Journal of Scientific Research, 2009
Methocel K15 MCR (a modified hydroxypropylmethylcellulose) matrix tablets of pentoxifylline using... more Methocel K15 MCR (a modified hydroxypropylmethylcellulose) matrix tablets of pentoxifylline using microcrystalline cellulose (MCC), starch and lactose were prepared by wet granulation process. There was no significant difference in drug release between the hydrophilic matrices when the Methocel K15 MCR concentration was modified in low percentage. The release of pentoxifylline was influenced by the presence of microcrystalline cellulose, and by the different concentrations of starch and lactose. The data obtained proved that the formulation with 12.5% Methocel K15 MCR and 20% lactose is more useful for a controlled release pentoxifylline, due to the percentage released after 8 hours is nearly to 65%. There was no significant change on release profile after three months storage of tablets. The best-fit release kinetics was achieved with the Higuchi model, followed by the first-order plot.
Journal of Scientific Research, Dec 29, 2012
Ethanolic extracts of some fruits of Cucurbitaceae family such as Cucumis sativus (cucumber), Lag... more Ethanolic extracts of some fruits of Cucurbitaceae family such as Cucumis sativus (cucumber), Lagenaria siceraria (white pumpkin), Luffa acutangula (ridge gourd), Benincasa hispida (ash gourd), Citrullus lanatus (sweet melon) and Cucarbita maxima (pumpkin) have been studied for their hypoglycemic effects on alloxan induced diabetic rats (AIDRs). Screening results suggested that among the tested fruits the hypoglycemic potency follows: cucumber> white pumpkin> ridge gourd. These three fruit-extracts were further ...
International Journal
The antidiabetic effects of Ethyl acetate (Et Ac), Petroleum-ether (Pet ether), and Chloroform fr... more The antidiabetic effects of Ethyl acetate (Et Ac), Petroleum-ether (Pet ether), and Chloroform fractions from methanolic extract of the seeds of Entada phaseoloides were investigated in alloxan induced diabetic mice (AIDM). The effect of these fractions (200 mg ...