Pub Date : 2000-08-01DOI: 10.1211/146080800128736196
M. Mirzaei, A. Foroumadi
Background and the purpose of the study: Fluoroquinolones are an important group of antimicrobial agents that are used widely in the treatment of various infectious diseases. The purpose of the present study was to synthesize new N-piperazinyl quinolone derivatives with 5-chloro-2-theinyl group having possible antimicrobial activity. Methods: Reaction of ciprofloxacin (1), norfloxacin (2) and enoxacin (3) with α-bromoketone 10 or α-bromooxime derivatives 11a-c in DMF, in the presence of NaHCO3 at room temperature, afforded corresponding ketones 4a-c or oxime derivatives 5-7(a-c), respectively. Results and major conclusion: The synthesized compounds were tested against a series of Grampositive and Gram-negative bacteria. The results of MIC tests against both Gram-positive and Gram-negative bacteria revealed that ciprofloxacin derivatives (compounds 4a, 5a, 6a and 7a) were more active than norfloxacin and enoxacin analogues. Compound 5a, containing N-[2-(5-chlorothiophen-2-yl)-2-hydroxyiminoethyl] residue provided a high in vitro antibacterial activity against Gram-positive bacteria, with MIC of 0.06, 0.125, 0.5 and 0.125 µg/mL against S. aureus, S. epidermidis, E. feacalis and B. subtilis, respectively. Its activity was found to be 4 to 8 times better than reference drug (ciprofloxacin) against all
{"title":"Synthesis and In‐vitro Antibacterial Activity of N‐Piperazinyl Quinolone Derivatives with a 2‐Thienyl Group","authors":"M. Mirzaei, A. Foroumadi","doi":"10.1211/146080800128736196","DOIUrl":"https://doi.org/10.1211/146080800128736196","url":null,"abstract":"Background and the purpose of the study: Fluoroquinolones are an important group of antimicrobial agents that are used widely in the treatment of various infectious diseases. The purpose of the present study was to synthesize new N-piperazinyl quinolone derivatives with 5-chloro-2-theinyl group having possible antimicrobial activity. Methods: Reaction of ciprofloxacin (1), norfloxacin (2) and enoxacin (3) with α-bromoketone 10 or α-bromooxime derivatives 11a-c in DMF, in the presence of NaHCO3 at room temperature, afforded corresponding ketones 4a-c or oxime derivatives 5-7(a-c), respectively. Results and major conclusion: The synthesized compounds were tested against a series of Grampositive and Gram-negative bacteria. The results of MIC tests against both Gram-positive and Gram-negative bacteria revealed that ciprofloxacin derivatives (compounds 4a, 5a, 6a and 7a) were more active than norfloxacin and enoxacin analogues. Compound 5a, containing N-[2-(5-chlorothiophen-2-yl)-2-hydroxyiminoethyl] residue provided a high in vitro antibacterial activity against Gram-positive bacteria, with MIC of 0.06, 0.125, 0.5 and 0.125 µg/mL against S. aureus, S. epidermidis, E. feacalis and B. subtilis, respectively. Its activity was found to be 4 to 8 times better than reference drug (ciprofloxacin) against all","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77623842","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-08-01DOI: 10.1211/146080800128736204
M. Grover, M. Gulati, Bhupinder Singh, Saranjit Singh
The rates of degradation of 16 different penicillins have been determined at 35°C in borate buffer, pH9.2, by use of stability-indicating HPLC assay procedures. The best-fit was sought between pseudo first-order hydrolytic rate constants and different types of structural descriptor. Constitutional, topological, geometric and electrostatic descriptors were calculated using WHIM-3D/QSAR and CODESSA software. Advanced semi-empirical and ab-initio calculations were performed using AMPAC software. CODESSA was used to develop (multi)linear correlation models, perform cluster analysis of the experimental data and molecular descriptors, and interpret the developed models. The best correlations with the rates of hydrolysis of the drugs were found for topological, electrostatic and quantum-chemical descriptors.
{"title":"Correlation of Penicillin Structure with Rate Constants for Basic Hydrolysis","authors":"M. Grover, M. Gulati, Bhupinder Singh, Saranjit Singh","doi":"10.1211/146080800128736204","DOIUrl":"https://doi.org/10.1211/146080800128736204","url":null,"abstract":"The rates of degradation of 16 different penicillins have been determined at 35°C in borate buffer, pH9.2, by use of stability-indicating HPLC assay procedures. The best-fit was sought between pseudo first-order hydrolytic rate constants and different types of structural descriptor. Constitutional, topological, geometric and electrostatic descriptors were calculated using WHIM-3D/QSAR and CODESSA software. Advanced semi-empirical and ab-initio calculations were performed using AMPAC software. CODESSA was used to develop (multi)linear correlation models, perform cluster analysis of the experimental data and molecular descriptors, and interpret the developed models. The best correlations with the rates of hydrolysis of the drugs were found for topological, electrostatic and quantum-chemical descriptors.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78139413","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-08-01DOI: 10.1211/146080800128736150
H. Aoyama, P. S. Melo, P. Granjeiro, M. Haun, C. Ferreira
Protein phosphorylation and dephosphorylation mediate signal transduction events that control several important cellular processes. The aim of this work was to determine some kinetic properties of a protein phosphatase obtained from non-metabolizing V79 Chinese hamster cells. The effect of okadaic acid, a tumour promoter, on these cell cultures was also determined. Phosphatase activity was assayed in V79 cells which were lysed with 0.1 M imidazole buffer (pH7.4). Enzyme activity was determined using p-nitrophenylphosphate and tyrosine phosphate (TyrP) as substrates. Maximum phosphatase activity was obtained at pH 7.4. The apparent Km (Michael's constant) and specificity constant for TyrP were 0.06 nM and 57, respectively. Phosphatase activity was inhibited by 100 μM pCMB (p-chloro-mercuribenzoate; 70%), 10 mM fluoride (30%), 10 mM phosphate (40%), 100 μM m-vanadate (80%) and 100 μM o-vanadate (90%). Tartrate (5 mM) had no effect. The low Km value for TyrP and the high level of inhibition by vanadate suggest that the V79 phosphatase is a protein tyrosine phosphatase. The cytotoxic effect of okadaic acid was evaluated and the IC50 was 15, 20, 35 and 45 nM for nucleic acid content, neutral red uptake, MTT and protein phosphatase assays, respectively. These results agree with the kinetic data, indicating that the V79 phosphatase is a protein tyrosine phosphatase, as enzyme activity was stimulated when the cells were treated with okadaic acid. Serine/threonine protein phosphatases are completely inhibited by okadaic acid. The phosphatase enzyme system may be useful for studying cellular adaptation to apoptosis, oxidative stress and other conditions.
{"title":"Cytotoxicity of Okadaic Acid and Kinetic Characterization of Protein Tyrosine Phosphatase Activity in V79 Fibroblasts","authors":"H. Aoyama, P. S. Melo, P. Granjeiro, M. Haun, C. Ferreira","doi":"10.1211/146080800128736150","DOIUrl":"https://doi.org/10.1211/146080800128736150","url":null,"abstract":"Protein phosphorylation and dephosphorylation mediate signal transduction events that control several important cellular processes. The aim of this work was to determine some kinetic properties of a protein phosphatase obtained from non-metabolizing V79 Chinese hamster cells. The effect of okadaic acid, a tumour promoter, on these cell cultures was also determined. \u0000 \u0000 \u0000 \u0000Phosphatase activity was assayed in V79 cells which were lysed with 0.1 M imidazole buffer (pH7.4). Enzyme activity was determined using p-nitrophenylphosphate and tyrosine phosphate (TyrP) as substrates. Maximum phosphatase activity was obtained at pH 7.4. The apparent Km (Michael's constant) and specificity constant for TyrP were 0.06 nM and 57, respectively. Phosphatase activity was inhibited by 100 μM pCMB (p-chloro-mercuribenzoate; 70%), 10 mM fluoride (30%), 10 mM phosphate (40%), 100 μM m-vanadate (80%) and 100 μM o-vanadate (90%). Tartrate (5 mM) had no effect. The low Km value for TyrP and the high level of inhibition by vanadate suggest that the V79 phosphatase is a protein tyrosine phosphatase. The cytotoxic effect of okadaic acid was evaluated and the IC50 was 15, 20, 35 and 45 nM for nucleic acid content, neutral red uptake, MTT and protein phosphatase assays, respectively. These results agree with the kinetic data, indicating that the V79 phosphatase is a protein tyrosine phosphatase, as enzyme activity was stimulated when the cells were treated with okadaic acid. Serine/threonine protein phosphatases are completely inhibited by okadaic acid. \u0000 \u0000 \u0000 \u0000The phosphatase enzyme system may be useful for studying cellular adaptation to apoptosis, oxidative stress and other conditions.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74835671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-08-01DOI: 10.1211/146080800128736187
T. Mariappan, Baljinder Singh, Saranjit Singh
A liquid-chromatographic reversed-phase method employing a C18 column has been developed for simultaneous analysis of rifampicin, isoniazid and pyrazinamide in 0.1 M hydrochloric acid dissolution medium and in simulated gastric fluid. Good separations were achieved by employing a gradient prepared from methanol and 0.01M sodium dihydrogen orthophosphate buffer containing 0.05% w/v tetramethylammonium chloride (pH adjusted to 3.5). The detection wavelength was 254 nm. The method was validated for linearity, accuracy, precision and ruggedness. It was found to work well for analysis of the three drugs in the presence of degradation products and even for samples containing ethambutol, which does not interfere because of lack of UV absorption.
{"title":"A Validated Reversed‐Phase (C18) HPLC Method for Simultaneous Determination of Rifampicin, Isoniazid and Pyrazinamide in USP Dissolution Medium and Simulated Gastric Fluid","authors":"T. Mariappan, Baljinder Singh, Saranjit Singh","doi":"10.1211/146080800128736187","DOIUrl":"https://doi.org/10.1211/146080800128736187","url":null,"abstract":"A liquid-chromatographic reversed-phase method employing a C18 column has been developed for simultaneous analysis of rifampicin, isoniazid and pyrazinamide in 0.1 M hydrochloric acid dissolution medium and in simulated gastric fluid. Good separations were achieved by employing a gradient prepared from methanol and 0.01M sodium dihydrogen orthophosphate buffer containing 0.05% w/v tetramethylammonium chloride (pH adjusted to 3.5). The detection wavelength was 254 nm. The method was validated for linearity, accuracy, precision and ruggedness. It was found to work well for analysis of the three drugs in the presence of degradation products and even for samples containing ethambutol, which does not interfere because of lack of UV absorption.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86897478","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-08-01DOI: 10.1211/146080800128736169
T. Hino, S. Shimabayashi, Atsushi Nakai
Scoured silk fibre was dissolved in a solution of calcium chloride in water and ethanol. After dialysis against purified water, theophylline as model drug was added to the solution. Silk microspheres prepared after spray-drying were round but somewhat wrinkled; their diameter was 5 μm (approx.). According to powder X-ray diffractometry, and FTIR and Raman spectroscopy, fibroin and theophylline were amorphous in the microsphere. The microspheres formed gels immediately after soaking in purified water and in Japanese Pharmacopoeia XIII solutions 1 (pH 1.2) and 2 (pH 6.8); the gels dissolved slightly in these aqueous media. In this way we have developed a new drug carrier for sustained release without the use of poisonous organic solvents or glutaraldehyde.
{"title":"Silk Microspheres Prepared by Spray‐drying of an Aqueous System","authors":"T. Hino, S. Shimabayashi, Atsushi Nakai","doi":"10.1211/146080800128736169","DOIUrl":"https://doi.org/10.1211/146080800128736169","url":null,"abstract":"Scoured silk fibre was dissolved in a solution of calcium chloride in water and ethanol. After dialysis against purified water, theophylline as model drug was added to the solution. Silk microspheres prepared after spray-drying were round but somewhat wrinkled; their diameter was 5 μm (approx.). According to powder X-ray diffractometry, and FTIR and Raman spectroscopy, fibroin and theophylline were amorphous in the microsphere. The microspheres formed gels immediately after soaking in purified water and in Japanese Pharmacopoeia XIII solutions 1 (pH 1.2) and 2 (pH 6.8); the gels dissolved slightly in these aqueous media. In this way we have developed a new drug carrier for sustained release without the use of poisonous organic solvents or glutaraldehyde.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75428085","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-07-01DOI: 10.1211/146080800128736079
S. Hoag, R. Nair, F. Muller
A novel slotted-web transducer design concept for the measurement of die-wall stress in a compaction simulator has been developed and optimized by use of computer-aided design procedures. The optimized design was then built and tested. Geometric optimization of the novel design configuration and determination of strain-gauge placement were performed so that the transducer could withstand the high die-wall pressures encountered in a compaction simulator. Stress analysis was performed with Algor, a finite-element analysis software package. A model prototype was constructed with 4140 alloy steel and heat treated to a hardness of 43 Rockwell C. This prototype had a linear calibration curve (r2 = 0.99) at three different punch settings with no hysteresis. Radial stress versus axial stress transmission curves, and results from measurement of residual die-wall stress for dibasic calcium phosphate dihydrate, mannitol, sodium chloride, paracetamol and starch were consistent with literature data, which indicates satisfactory transducer performance.
{"title":"Force‐transducer‐design Optimization for the Measurement of Die‐wall Stress in a Compaction Simulator","authors":"S. Hoag, R. Nair, F. Muller","doi":"10.1211/146080800128736079","DOIUrl":"https://doi.org/10.1211/146080800128736079","url":null,"abstract":"A novel slotted-web transducer design concept for the measurement of die-wall stress in a compaction simulator has been developed and optimized by use of computer-aided design procedures. The optimized design was then built and tested. Geometric optimization of the novel design configuration and determination of strain-gauge placement were performed so that the transducer could withstand the high die-wall pressures encountered in a compaction simulator. Stress analysis was performed with Algor, a finite-element analysis software package. A model prototype was constructed with 4140 alloy steel and heat treated to a hardness of 43 Rockwell C. This prototype had a linear calibration curve (r2 = 0.99) at three different punch settings with no hysteresis. Radial stress versus axial stress transmission curves, and results from measurement of residual die-wall stress for dibasic calcium phosphate dihydrate, mannitol, sodium chloride, paracetamol and starch were consistent with literature data, which indicates satisfactory transducer performance.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82235715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-07-01DOI: 10.1211/146080800128736132
K. Cimanga, Y. Li, T. Bruyne, S. Apers, P. Cos, P. Bakana, K. Kambu, L. Tona, L. Pieters, D. Berghe, A. Vlietinck
Cryptolepis sanguinolenta (Lindl.) Schlechter (Periplocaceae) is a medicinal plant used in some African countries against infectious and parasitic diseases. Six of its constituent alkaloids have been isolated from the root bark, identified spectroscopically as cryptoquindolinine (1), quindoline (2), neocryptolepine (3), cryptolepine (4), 11-hydroxycryptolepine (5) and biscryptolepine (6), and their interaction with the xanthine-xanthine oxidase enzyme system has been tested. Compound 5 has been shown to inhibit xanthine oxidase and act as a scavenger of superoxide anions. Alkaloids 1–4 and 6 were devoid of effect in both assays at the highest test concentration of 100 mM. These findings suggest the importance, in the manifestation of both activities, of the hydroxyl group present in 5 but not in the other alkaloids.
{"title":"Inhibitors of Xanthine Oxidase and Scavengers of Superoxide Anions from Cryptolepis sanguinolenta (Lindl.) Schlechter (Periplocaceae)","authors":"K. Cimanga, Y. Li, T. Bruyne, S. Apers, P. Cos, P. Bakana, K. Kambu, L. Tona, L. Pieters, D. Berghe, A. Vlietinck","doi":"10.1211/146080800128736132","DOIUrl":"https://doi.org/10.1211/146080800128736132","url":null,"abstract":"Cryptolepis sanguinolenta (Lindl.) Schlechter (Periplocaceae) is a medicinal plant used in some African countries against infectious and parasitic diseases. Six of its constituent alkaloids have been isolated from the root bark, identified spectroscopically as cryptoquindolinine (1), quindoline (2), neocryptolepine (3), cryptolepine (4), 11-hydroxycryptolepine (5) and biscryptolepine (6), and their interaction with the xanthine-xanthine oxidase enzyme system has been tested. Compound 5 has been shown to inhibit xanthine oxidase and act as a scavenger of superoxide anions. Alkaloids 1–4 and 6 were devoid of effect in both assays at the highest test concentration of 100 mM. \u0000 \u0000 \u0000 \u0000These findings suggest the importance, in the manifestation of both activities, of the hydroxyl group present in 5 but not in the other alkaloids.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89538988","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-07-01DOI: 10.1211/146080800128736114
P. Arivazhagan, C. Panneerselvam
The effects of dietary DL-α-lipoic acid supplementation on lipid peroxidation and antioxidant status have been evaluated in the brain of young and aged rats. In aged rats, antioxidant status was low whereas levels of thiobarbituric acid-reactive substances were high. Intraperitoneal administration of DL-α-lipoic acid to experimental rats at 100 mgkg−1 day−1 for 7 and 14 days resulted in a duration-dependent reduction in lipid peroxidation and an elevation in the levels and activity of antioxidants. DL-α-Lipoic acid supplementation can increase the activity of brain antioxidants during ageing and minimize free radical-induced age-associated disorders in the brain.
{"title":"Effect of Dietary DL‐α‐Lipoic Acid Supplementation on Peroxidative Antioxidant Status in the Brain of Aged Rats","authors":"P. Arivazhagan, C. Panneerselvam","doi":"10.1211/146080800128736114","DOIUrl":"https://doi.org/10.1211/146080800128736114","url":null,"abstract":"The effects of dietary DL-α-lipoic acid supplementation on lipid peroxidation and antioxidant status have been evaluated in the brain of young and aged rats. \u0000 \u0000 \u0000 \u0000In aged rats, antioxidant status was low whereas levels of thiobarbituric acid-reactive substances were high. Intraperitoneal administration of DL-α-lipoic acid to experimental rats at 100 mgkg−1 day−1 for 7 and 14 days resulted in a duration-dependent reduction in lipid peroxidation and an elevation in the levels and activity of antioxidants. \u0000 \u0000 \u0000 \u0000DL-α-Lipoic acid supplementation can increase the activity of brain antioxidants during ageing and minimize free radical-induced age-associated disorders in the brain.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85914929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-07-01DOI: 10.1211/146080800128736105
G. Schmeda-Hirschmann, Jaime A. Rodríguez, J. I. Loyola, L. Astudillo, J. Bastida, F. Viladomat, C. Codina
Plants belonging to the Amaryllidaceae family have been shown to be a good source of biologically active alkaloids. The effect of 20 Amaryllidaceae alkaloids on the blood pressure of normotensive rats was assessed. The compounds evaluated belong to the lycorine, homolycorine, galanthamine, crinane, tazettine and miscellaneous skeletal types. At 1.5 mgkg−1, eight of the alkaloids assayed showed a significant effect on the arterial pressure of normotensive rats. Seven elicited a hypotensive response > 20%, with a lasting time ranging from 2.0 to 36.0 min while crinamine showed a hypertensive effect. These findings support the potential of Amaryllidaceae alkaloids as hypotensive drugs.
{"title":"Activity of Amaryllidaceae Alkaloids on the Blood Pressure of Normotensive Rats","authors":"G. Schmeda-Hirschmann, Jaime A. Rodríguez, J. I. Loyola, L. Astudillo, J. Bastida, F. Viladomat, C. Codina","doi":"10.1211/146080800128736105","DOIUrl":"https://doi.org/10.1211/146080800128736105","url":null,"abstract":"Plants belonging to the Amaryllidaceae family have been shown to be a good source of biologically active alkaloids. The effect of 20 Amaryllidaceae alkaloids on the blood pressure of normotensive rats was assessed. The compounds evaluated belong to the lycorine, homolycorine, galanthamine, crinane, tazettine and miscellaneous skeletal types. \u0000 \u0000 \u0000 \u0000At 1.5 mgkg−1, eight of the alkaloids assayed showed a significant effect on the arterial pressure of normotensive rats. Seven elicited a hypotensive response > 20%, with a lasting time ranging from 2.0 to 36.0 min while crinamine showed a hypertensive effect. These findings support the potential of Amaryllidaceae alkaloids as hypotensive drugs.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88812036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-07-01DOI: 10.1211/146080800128736141
H. P. Shaila, S. Udupa, A. Udupa
The hypocholesterolaemic activity of different fractions from Terminalia arjuna were tested on rats fed an atherogenic diet. In the control group the feeding of cholesterol led to a 97% increase in serum cholesterol levels at the end of three weeks. The alcoholic and aqueous fractions inhibited this rise in serum cholesterol. The faecal excretion of total bile acids in rats fed with these fractions was increased. The possible mechanism of action of the cholesterol-reducing activity of these fractions may be due to the rapid excretion of bile acids.
{"title":"Hypocholesterolaemic Activity in Rats of Different Fractions from Terminalia arjuna","authors":"H. P. Shaila, S. Udupa, A. Udupa","doi":"10.1211/146080800128736141","DOIUrl":"https://doi.org/10.1211/146080800128736141","url":null,"abstract":"The hypocholesterolaemic activity of different fractions from Terminalia arjuna were tested on rats fed an atherogenic diet. In the control group the feeding of cholesterol led to a 97% increase in serum cholesterol levels at the end of three weeks. The alcoholic and aqueous fractions inhibited this rise in serum cholesterol. The faecal excretion of total bile acids in rats fed with these fractions was increased. The possible mechanism of action of the cholesterol-reducing activity of these fractions may be due to the rapid excretion of bile acids.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86529262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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