The assessment of toxic and pharmacological properties of snake venoms and their components is based predominantly on the animal experiments. Several modifications using fewer animals than the classical LD50 assay have been published. Using these methods an Approximate LD50 can be determined, the precision of and reproducibility of which is sufficient for most purposes of lethality testing. The pharmacological studies of the saw-scaled viper help us to locate and work on the components in the venom responsible for bringing these changes in the victims. So far in Pakistan the toxicity of snake venoms has been evaluated only through the classical LD50. The present work comprises the estimation of the toxicity of crude venom of Echis carinatus (saw-scaled viper) by evaluation of its Approximate LD50 in mice. This study has been taken as a model for the venom bioassays of snakes from other proximate species. The subsequent portion comprises the characterization of pharmacological effects of the crude venom of the said snake in mice.
{"title":"Evaluation of Approximate LD50 and pharmacological effects of Echis carinatus (Saw-scaled viper) venom from Central Punjab, Pakistan","authors":"A. Feroze, S. Malik, M. Nawaz","doi":"10.5580/1e90","DOIUrl":"https://doi.org/10.5580/1e90","url":null,"abstract":"The assessment of toxic and pharmacological properties of snake venoms and their components is based predominantly on the animal experiments. Several modifications using fewer animals than the classical LD50 assay have been published. Using these methods an Approximate LD50 can be determined, the precision of and reproducibility of which is sufficient for most purposes of lethality testing. The pharmacological studies of the saw-scaled viper help us to locate and work on the components in the venom responsible for bringing these changes in the victims. So far in Pakistan the toxicity of snake venoms has been evaluated only through the classical LD50. The present work comprises the estimation of the toxicity of crude venom of Echis carinatus (saw-scaled viper) by evaluation of its Approximate LD50 in mice. This study has been taken as a model for the venom bioassays of snakes from other proximate species. The subsequent portion comprises the characterization of pharmacological effects of the crude venom of the said snake in mice.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"70 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86141344","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}
Amphibians have been occupying a wide range of habitats since they evolved around 363 million-years-ago. Along with legs and lungs, skin played an important role in survival of amphibians and made it possible for them to exploit diverse ecological conditions. Amphibian skin not only helps in avoiding desiccation but also helps in imposing defense against predators as well as pathogens. Amphibian skin possesses wide variety of chemical compounds, which have potential significance in pharmacology and therapeutics. Toads especially those belonging to genus Bufo, are outstanding source of useful granulargland secretions. Compounds derived from toad skin-secretions can be used as analgesics, painkillers and as medicine against cardiac-problems, multi-drug resistant bacteria, HIV and Cancer.
{"title":"Toad skin-secretions: Potent source of pharmacologically and therapeutically significant compounds","authors":"Abhishek D Garg, R. Hippargi, Amit N. Gandhare","doi":"10.5580/18b6","DOIUrl":"https://doi.org/10.5580/18b6","url":null,"abstract":"Amphibians have been occupying a wide range of habitats since they evolved around 363 million-years-ago. Along with legs and lungs, skin played an important role in survival of amphibians and made it possible for them to exploit diverse ecological conditions. Amphibian skin not only helps in avoiding desiccation but also helps in imposing defense against predators as well as pathogens. Amphibian skin possesses wide variety of chemical compounds, which have potential significance in pharmacology and therapeutics. Toads especially those belonging to genus Bufo, are outstanding source of useful granulargland secretions. Compounds derived from toad skin-secretions can be used as analgesics, painkillers and as medicine against cardiac-problems, multi-drug resistant bacteria, HIV and Cancer.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81475756","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}
Under reporting of Adverse Drug Reactions (ADRs) is a common problem in pharmacovigilance programs. Previous studies conducted out side Nepal acknowledged a poor Knowledge, Attitude and Practices (KAP) among the healthcare professionals regarding ADR monitoring and pharmacovigilance programs. Similar data is lacking in Manipal Teaching hospital (MTH) where pharmacovigilance program was started two years ago. Hence we studied the demographic details of the healthcare professionals and analyzed their knowledge, attitude and practices of healthcare professionals regarding adverse drug reactions and pharmacovigilance. A survey was carryout among healthcare professionals. A KAP questionnaire was developed (Cronbach alpha value 0.72) and given to 24 healthcare professionals (10 doctors, 2 pharmacists and 12 nurses) working at MTH. The KAP questionnaire had a total of 25 questions. Each correct/positive answer was given a score of '1' whereas the negative/wrong answers were given a score of '0'. The total score is 25. Nearly two third (66.7%) of the respondents were in the age group of 20-30 years old. The median duration of service of the respondents was 17 months. The mean ± SD total score was 11.3 ±4 .1 for nurses, 13.6 ± 3.7 for doctors and 13.0±7.1 for pharmacists. The study identified the KAP scores to be low and recommended educational and managerial intervention. It is expected that though these programs the KAP and awareness among the healthcare professionals will improve.
{"title":"Evaluation of the knowledge, attitude and practices on adverse drug reactions and pharmacovigilance among healthcare professionals in a Nepalese hospital: a preliminary study","authors":"P. Subish, M. Izham, P. Mishra","doi":"10.5580/271a","DOIUrl":"https://doi.org/10.5580/271a","url":null,"abstract":"Under reporting of Adverse Drug Reactions (ADRs) is a common problem in pharmacovigilance programs. Previous studies conducted out side Nepal acknowledged a poor Knowledge, Attitude and Practices (KAP) among the healthcare professionals regarding ADR monitoring and pharmacovigilance programs. Similar data is lacking in Manipal Teaching hospital (MTH) where pharmacovigilance program was started two years ago. Hence we studied the demographic details of the healthcare professionals and analyzed their knowledge, attitude and practices of healthcare professionals regarding adverse drug reactions and pharmacovigilance. A survey was carryout among healthcare professionals. A KAP questionnaire was developed (Cronbach alpha value 0.72) and given to 24 healthcare professionals (10 doctors, 2 pharmacists and 12 nurses) working at MTH. The KAP questionnaire had a total of 25 questions. Each correct/positive answer was given a score of '1' whereas the negative/wrong answers were given a score of '0'. The total score is 25. Nearly two third (66.7%) of the respondents were in the age group of 20-30 years old. The median duration of service of the respondents was 17 months. The mean ± SD total score was 11.3 ±4 .1 for nurses, 13.6 ± 3.7 for doctors and 13.0±7.1 for pharmacists. The study identified the KAP scores to be low and recommended educational and managerial intervention. It is expected that though these programs the KAP and awareness among the healthcare professionals will improve.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87348584","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}
O. M. Salam, S. M. Nofal, S. El-Shenawy, Nermeen M. Shaffie
Thirty-six rats with biliary obstruction induced by double ligation and section of the common bile duct were randomly and blindly assigned to receive subcutaneous injection of interferon alpha (INF-alpha at 6750 or 13500 IU/kg) three times weekly alone, a combination of INF-alpha and silymarin (25 mg/kg once a day orally) or saline, starting one day after surgery and continued for one month. At the end of the treatment period, rats were killed and analyzed for blood biochemistry, liver and bone histopathology. The administration of INF-alpha at 6750 IU/kg increased plasma aspartate aminotransferase by 60.6%. Serum alkaline phosphatase, alanine aminotransferase and aspartate aminotransferase activities were markedly raised after INF-alpha 13500 U/kg by 74.6%, 89% and 109%, respectively. Such elevations in liver enzymes were not observed in rats treated with a combination of INF-alpha and silymarin. Serum bilirubin decreased by 30.8 and 36.1% after treatment with INF-alpha at 6750 and 13500 IU/kg and by 23.7 and 20.8% after treatment with INF-alpha at 6750 or 13500 IU/kg combined with silymarin, respectively. Calcium levels in plasma were not significantly altered by INF-alpha alone or combined with silymarin. On histology, INF-alpha at 6750 IU/kg failed to prevent fibrosis in liver of BDL rats, although many of the hepatocytes appeared normal, while the higher dose of resulted in some improvement in the degree of fibrosis, oedema and lymphocytic infiltration. The addition of silymarin to interferon did not result in further histological improvement. In contrast to observations in the liver, thickness of bone tissue at the diaphysis of tibia was reduced in BDL rats, but restored to normal values by treatment with INFalpha alone or by the combination of INF-alpha and silymarin. The high dose of interferon either alone or accompanied with silymarin made much improvement in the bone changes that resulted from bile duct legation These results suggest that INFalpha alone or co-administered with silymarin is of limited value in this model of cholestatic liver injury, but appear to prevent bone alterations in obstructive jaundice INF-alpha is likely to exert antifibrotic effects distinct from its antiviral properties. The study also indicates that bile duct ligation is a reliable and efficient model for producing osteoporosis in rats for the assessment of different drugs and pathophysiologic mechanisms involved.
{"title":"The Effect Of Interferon Alone Or Combined With Silymarin On Liver And Bone Parameters In Bile Duct Ligated Rats","authors":"O. M. Salam, S. M. Nofal, S. El-Shenawy, Nermeen M. Shaffie","doi":"10.5580/2753","DOIUrl":"https://doi.org/10.5580/2753","url":null,"abstract":"Thirty-six rats with biliary obstruction induced by double ligation and section of the common bile duct were randomly and blindly assigned to receive subcutaneous injection of interferon alpha (INF-alpha at 6750 or 13500 IU/kg) three times weekly alone, a combination of INF-alpha and silymarin (25 mg/kg once a day orally) or saline, starting one day after surgery and continued for one month. At the end of the treatment period, rats were killed and analyzed for blood biochemistry, liver and bone histopathology. The administration of INF-alpha at 6750 IU/kg increased plasma aspartate aminotransferase by 60.6%. Serum alkaline phosphatase, alanine aminotransferase and aspartate aminotransferase activities were markedly raised after INF-alpha 13500 U/kg by 74.6%, 89% and 109%, respectively. Such elevations in liver enzymes were not observed in rats treated with a combination of INF-alpha and silymarin. Serum bilirubin decreased by 30.8 and 36.1% after treatment with INF-alpha at 6750 and 13500 IU/kg and by 23.7 and 20.8% after treatment with INF-alpha at 6750 or 13500 IU/kg combined with silymarin, respectively. Calcium levels in plasma were not significantly altered by INF-alpha alone or combined with silymarin. On histology, INF-alpha at 6750 IU/kg failed to prevent fibrosis in liver of BDL rats, although many of the hepatocytes appeared normal, while the higher dose of resulted in some improvement in the degree of fibrosis, oedema and lymphocytic infiltration. The addition of silymarin to interferon did not result in further histological improvement. In contrast to observations in the liver, thickness of bone tissue at the diaphysis of tibia was reduced in BDL rats, but restored to normal values by treatment with INFalpha alone or by the combination of INF-alpha and silymarin. The high dose of interferon either alone or accompanied with silymarin made much improvement in the bone changes that resulted from bile duct legation These results suggest that INFalpha alone or co-administered with silymarin is of limited value in this model of cholestatic liver injury, but appear to prevent bone alterations in obstructive jaundice INF-alpha is likely to exert antifibrotic effects distinct from its antiviral properties. The study also indicates that bile duct ligation is a reliable and efficient model for producing osteoporosis in rats for the assessment of different drugs and pathophysiologic mechanisms involved.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73150995","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}
B. Semwal, K. Shah, Nagendra Singh Chauhan, R. Badhe, K. Divakar
Object: To evaluate antidiabetic activity of stem bark of Berberis aristata D.C. (Berberdiaceae) in alloxan induced diabetic rats. Materials and Method: Male Wistar albino rats (150–250 g) were taken and study for glucose tolerance test and alloxan induced diabetic rats. The ethanolic extract of B. aristata were selected for antidiabetic activity. Blood glucose levels were estimated in all groups on 1st, 4th, 7th and 15th day of the treatment with B. aristata. The biochemical parameters and body weight were estimated all treated groups and compared against diabetic control group. Results: The ethanolic extract of stem bark of B. aristata showed a significant hyperglycemic effect in alloxan induced diabetic rats. It reduces blood glucose level 60.4% and & 75.46 % at the dose of 25 mg/kg and 50 mg/kg in diabetic rats. B. aristata has a significant antidiabetic activity in glucose tolerance test Conclusion: The results justify the traditional use of bark in the treatment of diabetes.
{"title":"Anti-diabetic activity of stem bark of Berberis aristata D.C. in alloxan induced diabetic rats","authors":"B. Semwal, K. Shah, Nagendra Singh Chauhan, R. Badhe, K. Divakar","doi":"10.5580/90","DOIUrl":"https://doi.org/10.5580/90","url":null,"abstract":"Object: To evaluate antidiabetic activity of stem bark of Berberis aristata D.C. (Berberdiaceae) in alloxan induced diabetic rats. Materials and Method: Male Wistar albino rats (150–250 g) were taken and study for glucose tolerance test and alloxan induced diabetic rats. The ethanolic extract of B. aristata were selected for antidiabetic activity. Blood glucose levels were estimated in all groups on 1st, 4th, 7th and 15th day of the treatment with B. aristata. The biochemical parameters and body weight were estimated all treated groups and compared against diabetic control group. Results: The ethanolic extract of stem bark of B. aristata showed a significant hyperglycemic effect in alloxan induced diabetic rats. It reduces blood glucose level 60.4% and & 75.46 % at the dose of 25 mg/kg and 50 mg/kg in diabetic rats. B. aristata has a significant antidiabetic activity in glucose tolerance test Conclusion: The results justify the traditional use of bark in the treatment of diabetes.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"84 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83822354","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}
The present work is carried out to study the effect of Centratherum anthelminticum wild. kuntze (Asteaceae) on blood glucose level and antioxidant enzymes level in streptozotocin induced diabetic rats. Streptozotocin (STZ 50 mg/kg, i.p) induced diabetic rats were treated with methanolic extract of Centratherum anthelminticum (100 mg/kg; p.o.) for 28 days. Methanolic extract of Centratherum anthelminticum wild. Kuntze significantly prevented loss of body weight, decrease food and water intake. It showed significant prevention in elevation of glucose and significantly increased insulin level and showed prevention in increase in the cholesterol, triglyceride, LDL cholesterol, VLDL cholesterol levels in serum of diabetic rats. The treatment with methanolic extract of Centratherum anthelminticum also significantly prevented decrease in the HDL-cholesterol level and increase in urea and creatinine levels in diabetic rats compared to that of diabetic control. The chronic treatments with methanolic extract of CA significantly prevented the increase of malondialdehyde and prevent reduction of superoxide dismutase, catalase, and reduced glutathione levels. Histopathological study revealed that Centratherum anthelminticum extract provided significant protection against STZ induced degeneration in liver and kidney. This confirms the antidiabetic and antioxidant activity of Centratherum anthelminticum wild. kuntze in streptozotocin induced diabetic rats.
{"title":"Evaluation of Anti-diabetic and Anti-oxidant Activity of Centratherum anthelmintica in STZ – induced Diabetic Rats","authors":"J. Shah, M. S. Patel, K. Patel, T. Gandhi","doi":"10.5580/1b56","DOIUrl":"https://doi.org/10.5580/1b56","url":null,"abstract":"The present work is carried out to study the effect of Centratherum anthelminticum wild. kuntze (Asteaceae) on blood glucose level and antioxidant enzymes level in streptozotocin induced diabetic rats. Streptozotocin (STZ 50 mg/kg, i.p) induced diabetic rats were treated with methanolic extract of Centratherum anthelminticum (100 mg/kg; p.o.) for 28 days. Methanolic extract of Centratherum anthelminticum wild. Kuntze significantly prevented loss of body weight, decrease food and water intake. It showed significant prevention in elevation of glucose and significantly increased insulin level and showed prevention in increase in the cholesterol, triglyceride, LDL cholesterol, VLDL cholesterol levels in serum of diabetic rats. The treatment with methanolic extract of Centratherum anthelminticum also significantly prevented decrease in the HDL-cholesterol level and increase in urea and creatinine levels in diabetic rats compared to that of diabetic control. The chronic treatments with methanolic extract of CA significantly prevented the increase of malondialdehyde and prevent reduction of superoxide dismutase, catalase, and reduced glutathione levels. Histopathological study revealed that Centratherum anthelminticum extract provided significant protection against STZ induced degeneration in liver and kidney. This confirms the antidiabetic and antioxidant activity of Centratherum anthelminticum wild. kuntze in streptozotocin induced diabetic rats.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72923366","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}
In order to prevent and treat cardiac diseases, the author proposed strategies to invent cardiovascular drugs by cardiac gap junctions through summarizing the functions, physiology and pathophysiology of cardiac gap junctions. The 5 principle strategies to invent cardiovascular drugs are created. The 5 principle strategies to invent cardiovascular drugs have the great potentialities to be used as novel proposals to treat and prevent cardiac diseases. INTRODUCTION More and more studies have been done on the gap junctions' structure, functions, physiology and pathophysiology. The gap junctions as a pharmacological target for clinical treatments becomes a important topic in medical science. Lots of tissues have gap junctions. But the cardiac gap junctions are the most important gap junctions in the human body. The research on cardiac gap junctions' structure, functions, physiology and pathophysiology has reached good achievements. But the cardiac gap junctions' clinical applications as targets to invent cardiovascular drugs have not developed good results. There are no reports about the cardiac gap junctions' clinical applications as targets to invent cardiovascular drugs. Which is identified through a MEDLINE search of the Englishlanguage literature on “Strategies To Invent Cardiovascular Drugs by Cardiac Gap Junctions” and the key words of this paper or only on the title of the paper. According to cardiac gap junctions' structure, functions, physiology, pathophysiology characters and recently research achievements about cardiac gap junctions, the author summarized his ideas as following strategies that cardiac gap junctions should be targeted to invent cardiovascular drugs. 1. Cardiac gap junctions blockers or mediators for clinical usages. Research and select cardiac gap junctions blockers or mediators to mediate or block cardiac gap junction channels. So as to mediate or block the ions and small molecules flowing passage in cardiac gap junctions and electrical activation of the heart's cell-cell transfer of current via gap junctions. As the gap junction blocker had been invented for clinical prevention and treatment in the nervous system. The cardiac gap junctions mediators have a bright future. These strategies may be easy to do. 2. Modulating gap junction protein expression. As cardiac gap junction channels are predominantly composed of connexin40(Cx40) or connexin43(Cx43) proteins. Specially selected molecules to mediate connexin40 or connexin43 proteins expression, transcriptions, and translations or proteins catabolism are also bright ways to mediate cardiac gap junction channels' functions, physiology, pathophysiology activities. These strategies may affect gap junction conductance chronically. 3. Modulating protein kinases. Substances which activate protein kinase C, protein kinase A or protein kinase G may alter Cx43 gap junction conductance. Therefore, modulating protein kinase C, protein kinase A or protein kinase G may alter cardiac g
{"title":"Strategies To Invent Cardiovascular Drugs by Cardiac Gap Junctions","authors":"X. Han–You","doi":"10.5580/a79","DOIUrl":"https://doi.org/10.5580/a79","url":null,"abstract":"In order to prevent and treat cardiac diseases, the author proposed strategies to invent cardiovascular drugs by cardiac gap junctions through summarizing the functions, physiology and pathophysiology of cardiac gap junctions. The 5 principle strategies to invent cardiovascular drugs are created. The 5 principle strategies to invent cardiovascular drugs have the great potentialities to be used as novel proposals to treat and prevent cardiac diseases. INTRODUCTION More and more studies have been done on the gap junctions' structure, functions, physiology and pathophysiology. The gap junctions as a pharmacological target for clinical treatments becomes a important topic in medical science. Lots of tissues have gap junctions. But the cardiac gap junctions are the most important gap junctions in the human body. The research on cardiac gap junctions' structure, functions, physiology and pathophysiology has reached good achievements. But the cardiac gap junctions' clinical applications as targets to invent cardiovascular drugs have not developed good results. There are no reports about the cardiac gap junctions' clinical applications as targets to invent cardiovascular drugs. Which is identified through a MEDLINE search of the Englishlanguage literature on “Strategies To Invent Cardiovascular Drugs by Cardiac Gap Junctions” and the key words of this paper or only on the title of the paper. According to cardiac gap junctions' structure, functions, physiology, pathophysiology characters and recently research achievements about cardiac gap junctions, the author summarized his ideas as following strategies that cardiac gap junctions should be targeted to invent cardiovascular drugs. 1. Cardiac gap junctions blockers or mediators for clinical usages. Research and select cardiac gap junctions blockers or mediators to mediate or block cardiac gap junction channels. So as to mediate or block the ions and small molecules flowing passage in cardiac gap junctions and electrical activation of the heart's cell-cell transfer of current via gap junctions. As the gap junction blocker had been invented for clinical prevention and treatment in the nervous system. The cardiac gap junctions mediators have a bright future. These strategies may be easy to do. 2. Modulating gap junction protein expression. As cardiac gap junction channels are predominantly composed of connexin40(Cx40) or connexin43(Cx43) proteins. Specially selected molecules to mediate connexin40 or connexin43 proteins expression, transcriptions, and translations or proteins catabolism are also bright ways to mediate cardiac gap junction channels' functions, physiology, pathophysiology activities. These strategies may affect gap junction conductance chronically. 3. Modulating protein kinases. Substances which activate protein kinase C, protein kinase A or protein kinase G may alter Cx43 gap junction conductance. Therefore, modulating protein kinase C, protein kinase A or protein kinase G may alter cardiac g","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78901522","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}
Quantitative structure activity relationships (QSAR) and pharmacophore three-dimensional structure modelling provide possible methods for understanding the first pass metabolism of human cytochrome P450 substrates in the absence of reliable crystal structures of the human enzymes. The increasing need for alternative and objective methods of metabolism prediction has developed into computational approaches to the problem of understanding the enzyme and substrate behaviour. By analysis of the three-dimensional structure known to be catalysed by human P450 and comparison to other substrates involved in similar alkyl removal reactions, along with the alignment of molecular interaction potentials (MIP), a common template for specific dealkylations is proposed.
{"title":"The Identification of De-Alkylation Reactions Catalysed by Cytochrome P450 using Pharmacophore Three-dimensional Structure","authors":"L. L. Jones, B. Howlin, D. Povey","doi":"10.5580/140","DOIUrl":"https://doi.org/10.5580/140","url":null,"abstract":"Quantitative structure activity relationships (QSAR) and pharmacophore three-dimensional structure modelling provide possible methods for understanding the first pass metabolism of human cytochrome P450 substrates in the absence of reliable crystal structures of the human enzymes. The increasing need for alternative and objective methods of metabolism prediction has developed into computational approaches to the problem of understanding the enzyme and substrate behaviour. By analysis of the three-dimensional structure known to be catalysed by human P450 and comparison to other substrates involved in similar alkyl removal reactions, along with the alignment of molecular interaction potentials (MIP), a common template for specific dealkylations is proposed.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"35 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91189405","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}
S. Padi, Minakshi Gupta, J. Kehal, A. Aggarwal, Neeraj Kumar, R. Marwaha
The systemic use of non-steroidal anti-inflammatory drugs (NSAIDs) which act by inhibiting cyclooxygenase (COX) is severely hampered by gastric and peptic ulcers. The topical delivery of NSAIDs has the advantages of avoiding gastric and peptic ulcers and delivering the drug to the inflammation site. There are no studies that compared the pharmacological profile of gel formulations containing different NSAIDs. Therefore, attempt has been made to study the anti-inflammatory and antihyperalgesic effects of NIZER gel (nimesulide, a preferential COX-2 inhibitor, 1 mg per 100 mg gel) and VOVERAN Emulgel (diclofenac sodium, a nonselective COX (COX-1/2) inhibitor, 1 mg per 100 mg gel) in carrageenan-induced inflammation and hyperalgesia in rats. A 100 mg of NIZER gel or VOVERAN Emulgel when applied topically 30 min before inflammogen administration showed marked anti-inflammatory and antihyperlagesic effects against carrageenan-induced inflammation in rats with more significant effect was observed with NIZER gel. The results indicate that gels containing a preferential COX-2 inhibitor are better than a non-selective COX-1/2 inhibitor in alleviating inflammation and hyperalgesia.
{"title":"Evaluation of Topical Gels Containing Non-Steroidal Anti-Inflammatory Drugs on Inflammation and Hyperalgesia in rats","authors":"S. Padi, Minakshi Gupta, J. Kehal, A. Aggarwal, Neeraj Kumar, R. Marwaha","doi":"10.5580/1593","DOIUrl":"https://doi.org/10.5580/1593","url":null,"abstract":"The systemic use of non-steroidal anti-inflammatory drugs (NSAIDs) which act by inhibiting cyclooxygenase (COX) is severely hampered by gastric and peptic ulcers. The topical delivery of NSAIDs has the advantages of avoiding gastric and peptic ulcers and delivering the drug to the inflammation site. There are no studies that compared the pharmacological profile of gel formulations containing different NSAIDs. Therefore, attempt has been made to study the anti-inflammatory and antihyperalgesic effects of NIZER gel (nimesulide, a preferential COX-2 inhibitor, 1 mg per 100 mg gel) and VOVERAN Emulgel (diclofenac sodium, a nonselective COX (COX-1/2) inhibitor, 1 mg per 100 mg gel) in carrageenan-induced inflammation and hyperalgesia in rats. A 100 mg of NIZER gel or VOVERAN Emulgel when applied topically 30 min before inflammogen administration showed marked anti-inflammatory and antihyperlagesic effects against carrageenan-induced inflammation in rats with more significant effect was observed with NIZER gel. The results indicate that gels containing a preferential COX-2 inhibitor are better than a non-selective COX-1/2 inhibitor in alleviating inflammation and hyperalgesia.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"81 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82401066","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}
Citric acid introduced into the stomach of mice at increasing concentrations of 0.1, 1 or 10% (4.8 M-0.48 mM; 95 mol/kg–9.5 mmol/kg, 0.5 ml) caused dose-dependent inhibition of abdominal constrictions induced 1 h later by i.p. acetic acid injection by –51% to -69.5%. When administered at 10% (0.48 mM, 0.5 ml) 15 min before nociceptive challenge, citric acid inhibited the nociceptive response by 96.8%. Inhibition of the acetic acid-induced abdominal constrictions was also observed when lower doses of citric acid were introduced into the stomach (0.2 ml of 0.1-1%; 38.1 mol/kg-0.38 mmol/kg). The effect was evident as early as 5 min after administration of citric acid into the stomach and with the maximal effect being at 15-30 min after dosing. Lidocaine given orally 5 min prior to citric acid (1%, 48 M; 0.38 mmol/kg, 0.2 ml) prevented antinociception by citric acid, but lidocaine given 15 min before oral introduction of citric acid enhanced the citric acid-induced inhibition of the nociceptive response to acetic acid. The antinociceptive effect of orally administered citric acid (1%, 48 M; 0.38 mmol/kg, 0.2 ml) was increased by pre-treatment with propranolol (4 mg/kg, s.c.), yohimbine (4 mg/kg, s.c.), guanethidine (32 mg/kg, s.c.), but reduced after treatment with atropine (3 mg/kg, s.c.), which itself increased the nociceptive behaviour. Similar inhibition of the acetic acid-induced nociceptive behavior was also observed when sodium citrate (pH 7.21) or 0.1 N HCl (pH 3) or 1% sucrose solution (0.2 ml) was intragastrically given. It is suggested that citric acid might act to stimulate sensory afferents and that transmission of nociceptive information centrally leads to the activation of descending antinociceptive mechanism to a noxious stimulus.
{"title":"Pharmacological Investigation Into The Effect Of Citric Acid On Visceral Pain Response In Mice","authors":"O. M. Salam, A. R. Baiuomy","doi":"10.5580/1108","DOIUrl":"https://doi.org/10.5580/1108","url":null,"abstract":"Citric acid introduced into the stomach of mice at increasing concentrations of 0.1, 1 or 10% (4.8 M-0.48 mM; 95 mol/kg–9.5 mmol/kg, 0.5 ml) caused dose-dependent inhibition of abdominal constrictions induced 1 h later by i.p. acetic acid injection by –51% to -69.5%. When administered at 10% (0.48 mM, 0.5 ml) 15 min before nociceptive challenge, citric acid inhibited the nociceptive response by 96.8%. Inhibition of the acetic acid-induced abdominal constrictions was also observed when lower doses of citric acid were introduced into the stomach (0.2 ml of 0.1-1%; 38.1 mol/kg-0.38 mmol/kg). The effect was evident as early as 5 min after administration of citric acid into the stomach and with the maximal effect being at 15-30 min after dosing. Lidocaine given orally 5 min prior to citric acid (1%, 48 M; 0.38 mmol/kg, 0.2 ml) prevented antinociception by citric acid, but lidocaine given 15 min before oral introduction of citric acid enhanced the citric acid-induced inhibition of the nociceptive response to acetic acid. The antinociceptive effect of orally administered citric acid (1%, 48 M; 0.38 mmol/kg, 0.2 ml) was increased by pre-treatment with propranolol (4 mg/kg, s.c.), yohimbine (4 mg/kg, s.c.), guanethidine (32 mg/kg, s.c.), but reduced after treatment with atropine (3 mg/kg, s.c.), which itself increased the nociceptive behaviour. Similar inhibition of the acetic acid-induced nociceptive behavior was also observed when sodium citrate (pH 7.21) or 0.1 N HCl (pH 3) or 1% sucrose solution (0.2 ml) was intragastrically given. It is suggested that citric acid might act to stimulate sensory afferents and that transmission of nociceptive information centrally leads to the activation of descending antinociceptive mechanism to a noxious stimulus.","PeriodicalId":22523,"journal":{"name":"The Internet Journal of Pharmacology","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2007-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88440119","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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