Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.06.025
Savita G. Ghule , Vinayak K. Deshmukh , Sanjay R. Chaudhari
Aim
The benzothiazole, pyrimidine and piperazine nucleuses having outstanding biological activates which prompted us to synthesis of substituted derivatives of N-(1,3-benzothiazol-2-yl)-2-[4-(5-cyano-6-imino-2-oxo1,2,3,4-tetrahydropyrimidin-4-yl)piperazin-1-yl]acetamide and to evaluate for anticancer and anti-inflammatory activity.
Method
Benzothiazole linked by acetamido bridge to 4-Imino-2 oxo-6-(piperazin-1-yl)1,2,3,4-tetrahydropyrimidine -5-carbonitrile to afforded a series of substituted N-(1,3-benzothiazol-2-yl)-2-[4-(5-cyano-6-imino-2-oxo1,2,3,4-tetrahydropyrimidin 4-yl)piperazin-1-yl]acetamide in good yield.
Results and discussion
The structures of compounds were in agreement with IR, 1H NMR, and MASS spectral data. Three compounds were screened for in-vitro anticancer activity at the national cancer institute for anticancer activity against a panel of 60 different human tumor cell lines derived from nine neoplastic cancer types at NCI, and for in vitro anti-inflammatory activity by albumin denaturation technique. The compound (4b) with 6-chloro substitution was showed selective influence on cancer cell lines and compounds (4h), (4i), (4j) exhibited excellent anti-inflammatory activity.
Conclusion
New derivatives having significant in-vitro anti-inflammatory activity showed remarkable inhibitory effects against cancer. This observation may promote a further development of this novel series that may lead to compounds with better anticancer and anti-inflammatory profile.
{"title":"Design, synthesis and pharmacological activity of substituted 1,2,3,6-tetrahydropyrimidine-5-carbonitrile","authors":"Savita G. Ghule , Vinayak K. Deshmukh , Sanjay R. Chaudhari","doi":"10.1016/j.jopr.2013.06.025","DOIUrl":"10.1016/j.jopr.2013.06.025","url":null,"abstract":"<div><h3>Aim</h3><p>The benzothiazole, pyrimidine and piperazine nucleuses having outstanding biological activates which prompted us to synthesis of substituted derivatives of <em>N</em>-(1,3-benzothiazol-2-yl)-2-[4-(5-cyano-6-imino-2-oxo1,2,3,4-tetrahydropyrimidin-4-yl)piperazin-1-yl]acetamide and to evaluate for anticancer and anti-inflammatory activity.</p></div><div><h3>Method</h3><p>Benzothiazole linked by acetamido bridge to 4-Imino-2 oxo-6-(piperazin-1-yl)1,2,3,4-tetrahydropyrimidine -5-carbonitrile to afforded a series of substituted <em>N</em>-(1,3-benzothiazol-2-yl)-2-[4-(5-cyano-6-imino-2-oxo1,2,3,4-tetrahydropyrimidin 4-yl)piperazin-1-yl]acetamide in good yield.</p></div><div><h3>Results and discussion</h3><p>The structures of compounds were in agreement with IR, <sup>1</sup>H NMR, and MASS spectral data. Three compounds were screened for in-vitro anticancer activity at the national cancer institute for anticancer activity against a panel of 60 different human tumor cell lines derived from nine neoplastic cancer types at NCI, and for in vitro anti-inflammatory activity by albumin denaturation technique. The compound (<strong>4b</strong>) with 6-chloro substitution was showed selective influence on cancer cell lines and compounds (<strong>4h</strong>), (<strong>4i</strong>), (<strong>4j</strong>) exhibited excellent anti-inflammatory activity.</p></div><div><h3>Conclusion</h3><p>New derivatives having significant <em>in-vitro</em> anti-inflammatory activity showed remarkable inhibitory effects against cancer. This observation may promote a further development of this novel series that may lead to compounds with better anticancer and anti-inflammatory profile.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 600-605"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.025","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90294593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.013
José Ramón Montejano-Rodríguez , Georgina Almaguer-Vargas , Juan Antonio Gayosso-De-Lucio , María Esther Ocharan Hernández , Reyna Erika Moreno Martínez , Marta Elena Hernández Caballero , J.J. Martín Torres-Valencia , José Alfredo Sierra Ramírez
Background
Although Geranium seemannii Peyr. is widely used in Mexican traditional medicine, there is as yet no scientific study to explore the validity of this practice. Therefore, the aim of the present study was to evaluate the diuretic activity of the ethanolic extract of G. seemannii Peyr. to provide evidence about its effect.
Methods
G. seemannii Peyr. was orally administered to adult male Wistar rats at 25 and 50 mg/kg, and its diuretic activity was evaluated and compared to the reference drug furosemide (20 mg/kg, administered intraperitoneally). Acute toxicity and lethality (LD50) of the extract were assessed.
Results
Compared to control rats, there was significantly higher urinary output, as well as sodium, potassium and chloride ion excretion, in animals administered the ethanolic extract of G. seemannii Peyr. This effect was dose dependent, and there was no evidence of either acute toxicity or lethality with twice the maximum dose employed.
Discussion
The diuretic activity of some plants has been attributed to the presence of flavonoids, and G. seemannii Peyr. has a relatively large concentration of ellagitannins. This could be responsible for the effect demonstrated herein, which was similar to that produced by the reference drug furosemide. The mechanism of action of furosemide is by inducing a loss of water through the inhibition of NaCl reabsorption. The results suggest that this receptor-mediated mechanism may account for the diuretic effect of G. seemannii Peyr. as well.
Conclusion
The findings in the present work support the possible use of G. seemannii Peyr as a diuretic agent and, representing the first report of the diuretic activity of this specie.
{"title":"Evaluation of the diuretic activity of the ethanolic extract of Geranium seemannii Peyr. in Wistar rats","authors":"José Ramón Montejano-Rodríguez , Georgina Almaguer-Vargas , Juan Antonio Gayosso-De-Lucio , María Esther Ocharan Hernández , Reyna Erika Moreno Martínez , Marta Elena Hernández Caballero , J.J. Martín Torres-Valencia , José Alfredo Sierra Ramírez","doi":"10.1016/j.jopr.2013.07.013","DOIUrl":"10.1016/j.jopr.2013.07.013","url":null,"abstract":"<div><h3>Background</h3><p>Although <em>Geranium seemannii</em> Peyr. is widely used in Mexican traditional medicine, there is as yet no scientific study to explore the validity of this practice. Therefore, the aim of the present study was to evaluate the diuretic activity of the ethanolic extract of <em>G. seemannii</em> Peyr. to provide evidence about its effect.</p></div><div><h3>Methods</h3><p><em>G. seemannii</em> Peyr. was orally administered to adult male Wistar rats at 25 and 50 mg/kg, and its diuretic activity was evaluated and compared to the reference drug furosemide (20 mg/kg, administered intraperitoneally). Acute toxicity and lethality (LD<sub>50</sub>) of the extract were assessed.</p></div><div><h3>Results</h3><p>Compared to control rats, there was significantly higher urinary output, as well as sodium, potassium and chloride ion excretion, in animals administered the ethanolic extract of <em>G. seemannii</em> Peyr. This effect was dose dependent, and there was no evidence of either acute toxicity or lethality with twice the maximum dose employed.</p></div><div><h3>Discussion</h3><p>The diuretic activity of some plants has been attributed to the presence of flavonoids, and <em>G. seemannii</em> Peyr. has a relatively large concentration of ellagitannins. This could be responsible for the effect demonstrated herein, which was similar to that produced by the reference drug furosemide. The mechanism of action of furosemide is by inducing a loss of water through the inhibition of NaCl reabsorption. The results suggest that this receptor-mediated mechanism may account for the diuretic effect of <em>G. seemannii</em> Peyr. as well.</p></div><div><h3>Conclusion</h3><p>The findings in the present work support the possible use of <em>G. seemannii</em> Peyr as a diuretic agent and, representing the first report of the diuretic activity of this specie.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 709-713"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.013","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72668693","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present study was aimed to investigate the potent antifungal, and larvicidal phytochemical compounds from crude leaf organic solvent extracts of Ceriops decandra against phytopathogenic fungi and larvicidal activity against 3rd and 4th instar larvae of Spodoptera litura and Aedes aegypti.
Methods
The phytochemical constituents of three organic solvent (methanol, chloroform, and ethanol) extracts of the leaves of C. decandra were analyzed by GC–MS. Larvicidal activity of the crude extracts of C. decandra leaves was determined by topical application to early 3rd and 4th instar larvae of S. litura. Lethality was estimated by applying different concentrations (100–5000 μg/mL) of the crude extracts.
Results and discussion
The principle phytochemical constituents present in the chloroform extracts are triterpenes, Lupeol (66.95%) and α-amyrin (6.68%) are the major constituents. Chloroform extracts of C. decandra leaves showed strong antifungal against Pythium aphanidermatum, Rhizoctonia solani, Pyricularia oryzae, Curvularia oryzae and Fusarium oxysporum with zone of inhibition diameter (IZD) of 29 mm, 27 mm, 28 mm, 28 mm and 28 mm, respectively at a concentration of 500 μg/mL. Ethanolic extracts showed poor antifungal activity against the test fungi. The 3rd and 4th instar larvae of S. litura is more susceptible to the chloroform extracts of C. decandra with a LD50 value of 328.5% and 498.6% respectively. The LD50 value of chloroform extract was 251.2% and 309.7% against 3rd and 4th instar larvae of A. aegypti. Chloroform extracts of C. decandra showed a marked significant activity against 3rd and 4th instar larvae of S. litura and A. aegypti.
Conclusion
This investigation demonstrates the potency of organic solvent extracts of leaves of C. decandra in controlling the wide spreading of fungal diseases and larvae and thus contributes as an affordable way to control phytopathogenic fungi, S. litura and A. aegypti.
{"title":"Differential biological activities of the solvent extracts of Ceriops decandra (Griff.) and their phytochemical investigations","authors":"Vundru Anil Kumar , Kandru Ammani , Busi Siddhardha , Uppalapati Sreedhar , Gudapati Aravind Kumar","doi":"10.1016/j.jopr.2013.05.024","DOIUrl":"10.1016/j.jopr.2013.05.024","url":null,"abstract":"<div><h3>Objective</h3><p>The present study was aimed to investigate the potent antifungal, and larvicidal phytochemical compounds from crude leaf organic solvent extracts of <em>Ceriops decandra</em> against phytopathogenic fungi and larvicidal activity against 3rd and 4th instar larvae of <em>Spodoptera litura</em> and <em>Aedes aegypti</em>.</p></div><div><h3>Methods</h3><p>The phytochemical constituents of three organic solvent (methanol, chloroform, and ethanol) extracts of the leaves of <em>C. decandra</em> were analyzed by GC–MS. Larvicidal activity of the crude extracts of <em>C. decandra</em> leaves was determined by topical application to early 3rd and 4th instar larvae of <em>S. litura</em>. Lethality was estimated by applying different concentrations (100–5000 μg/mL) of the crude extracts.</p></div><div><h3>Results and discussion</h3><p>The principle phytochemical constituents present in the chloroform extracts are triterpenes, Lupeol (66.95%) and α-amyrin (6.68%) are the major constituents. Chloroform extracts of <em>C. decandra</em> leaves showed strong antifungal against <em>Pythium aphanidermatum</em>, <em>Rhizoctonia solani</em>, <em>Pyricularia oryzae</em>, <em>Curvularia oryzae</em> and <em>Fusarium oxysporum</em> with zone of inhibition diameter (IZD) of 29 mm, 27 mm, 28 mm, 28 mm and 28 mm, respectively at a concentration of 500 μg/mL. Ethanolic extracts showed poor antifungal activity against the test fungi. The 3rd and 4th instar larvae of <em>S. litura</em> is more susceptible to the chloroform extracts of <em>C. decandra</em> with a LD<sub>50</sub> value of 328.5% and 498.6% respectively. The LD<sub>50</sub> value of chloroform extract was 251.2% and 309.7% against 3rd and 4th instar larvae of <em>A. aegypti</em>. Chloroform extracts of <em>C. decandra</em> showed a marked significant activity against 3rd and 4th instar larvae of <em>S. litura</em> and <em>A. aegypti</em>.</p></div><div><h3>Conclusion</h3><p>This investigation demonstrates the potency of organic solvent extracts of leaves of <em>C. decandra</em> in controlling the wide spreading of fungal diseases and larvae and thus contributes as an affordable way to control phytopathogenic fungi, <em>S. litura</em> and <em>A. aegypti</em>.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 654-660"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.05.024","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75157550","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present work was carried out to evaluate the hepatoprotective activity of Marrubium vulgare against paracetamol toxicity in Wistar rats.
Methods
Hepatoprotective properties of the methanol extract of whole plant were evaluated on paracetamol induced hepatotoxicity. Hepatotoxicity was induced in albino Wistar rats by the administration of paracetamol (2 g/kg), p.o. for 7 days. Methanol extract of Marrubium vulgare was administered at the doses 100 and 200 mg/kg/day, p.o. for 7 days. Serum analysis was performed to estimate the levels of ALT, AST, ALP, albumin, total bilirubin, and triglycerides. The liver was solated and homogenized for the estimation of glutathione and malondialdehyde. Histopathology studies were also performed on the catalase liver samples.
Results
The toxic effects of paracetamol were significantly controlled in the extract treated groups which was manifested by the restoration of serum biochemical parameters to near normal levels.
Conclusions
From the study it was concluded that M. vulgare possess significant hepatoprotective properties.
{"title":"Hepatoprotective activity of Marrubium vulgare against paracetamol induced toxicity","authors":"Nayeema Akther , A.S. Shawl , Sarwat Sultana , B.K. Chandan , Mymoona Akhter","doi":"10.1016/j.jopr.2013.06.023","DOIUrl":"10.1016/j.jopr.2013.06.023","url":null,"abstract":"<div><h3>Aim</h3><p>The present work was carried out to evaluate the hepatoprotective activity of <em>Marrubium vulgare</em> against paracetamol toxicity in Wistar rats.</p></div><div><h3>Methods</h3><p>Hepatoprotective properties of the methanol extract of whole plant were evaluated on paracetamol induced hepatotoxicity. Hepatotoxicity was induced in albino Wistar rats by the administration of paracetamol (2 g/kg), p.o. for 7 days. Methanol extract of <em>Marrubium vulgare</em> was administered at the doses 100 and 200 mg/kg/day, p.o. for 7 days. Serum analysis was performed to estimate the levels of ALT, AST, ALP, albumin, total bilirubin, and triglycerides. The liver was solated and homogenized for the estimation of glutathione and malondialdehyde. Histopathology studies were also performed on the catalase liver samples.</p></div><div><h3>Results</h3><p>The toxic effects of paracetamol were significantly controlled in the extract treated groups which was manifested by the restoration of serum biochemical parameters to near normal levels.</p></div><div><h3>Conclusions</h3><p>From the study it was concluded that <em>M. vulgare</em> possess significant hepatoprotective properties.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 565-570"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.023","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78067942","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The study was undertaken to assess the pharmacokinetic and pharmacodynamic correlation of Lamotrigine (LMT) was determined following oral administration to prove that there was a direct relationship between daily dose, plasma level of LMT and analgesic effects.
Methods
Neuropathic pain was induced by chronic constriction injury of the sciatic nerve. This technique allows consecutive measurements of the paw withdrawal thresholds and paw withdrawal duration on hyperalgesia and allodynia respectively. Increase in threshold and decrease in the duration of paw withdrawals was used as an analgesic effect against neuropathy.
Results and discussion
The results demonstrate that there was a positive correlation between plasma correlation and pharmacodynamic effects in neuropathic pain.
Conclusion
Since there was a positive correlation between plasma correlation and pharmacodynamic effects in neuropathic pain, the plasma levels of Lamotrigine are good indicators of efficacy of the same in animal models of neuropathic pain.
{"title":"Relationship between plasma levels and the anti-neuropathic pain effect of Lamotrigine in rat model","authors":"Hema Veesam , Prameela Rani Avula , Siva Reddy Challa , Gangadhar Matharasala , Yogeeswari Perumal , Sriram Dharmarajan","doi":"10.1016/j.jopr.2013.07.006","DOIUrl":"10.1016/j.jopr.2013.07.006","url":null,"abstract":"<div><h3>Background</h3><p>The study was undertaken to assess the pharmacokinetic and pharmacodynamic correlation of Lamotrigine (LMT) was determined following oral administration to prove that there was a direct relationship between daily dose, plasma level of LMT and analgesic effects.</p></div><div><h3>Methods</h3><p>Neuropathic pain was induced by chronic constriction injury of the sciatic nerve. This technique allows consecutive measurements of the paw withdrawal thresholds and paw withdrawal duration on hyperalgesia and allodynia respectively. Increase in threshold and decrease in the duration of paw withdrawals was used as an analgesic effect against neuropathy.</p></div><div><h3>Results and discussion</h3><p>The results demonstrate that there was a positive correlation between plasma correlation and pharmacodynamic effects in neuropathic pain.</p></div><div><h3>Conclusion</h3><p>Since there was a positive correlation between plasma correlation and pharmacodynamic effects in neuropathic pain, the plasma levels of Lamotrigine are good indicators of efficacy of the same in animal models of neuropathic pain.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 780-784"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77718580","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.023
Saurav Panda , N.D. Jayakumar , M. Sankari , Sheeja. S. Varghese , Puneet Mehta
Background
For complete periodontal regeneration, delivery of growth factors in a local environment holds a great deal in adjunct to bone grafts. Platelet rich fibrin (PRF) is considered as second generation platelet concentrate, consisting of viable platelets, releasing various growth factors like PDGF, VEGF, TGF, IGF, EGF and bFGF. Hence, this case report aims to investigate the clinical and radiological (bone fill) effectiveness of autologous platelet rich fibrin (PRF) along with use of alloplastic bone mineral in the treatment of intra bony defects.
Methods
Intrabony defect was treated with autologous platelet rich fibrin (PRF) along with use of alloplastic bone mineral.
Results
A decrease in probing pocket depth, gain in clinical attachment level and significant bone fill was observed at end of 6 months.
Discussion
The result obtained with the use of Platelet Rich Fibrin may be attributed to the sustained and simultaneous release of various growth factors over a period of 7 days.
Conclusion
According to the results obtained in this case report, it could be concluded that the positive clinical impact of additional application of PRF with alloplastic graft material in treatment of periodontal intrabony defect.
{"title":"Platelet rich fibrin and alloplast in treatment of intrabony defect","authors":"Saurav Panda , N.D. Jayakumar , M. Sankari , Sheeja. S. Varghese , Puneet Mehta","doi":"10.1016/j.jopr.2013.07.023","DOIUrl":"10.1016/j.jopr.2013.07.023","url":null,"abstract":"<div><h3>Background</h3><p>For complete periodontal regeneration, delivery of growth factors in a local environment holds a great deal in adjunct to bone grafts. Platelet rich fibrin (PRF) is considered as second generation platelet concentrate, consisting of viable platelets, releasing various growth factors like PDGF, VEGF, TGF, IGF, EGF and bFGF. Hence, this case report aims to investigate the clinical and radiological (bone fill) effectiveness of autologous platelet rich fibrin (PRF) along with use of alloplastic bone mineral in the treatment of intra bony defects.</p></div><div><h3>Methods</h3><p>Intrabony defect was treated with autologous platelet rich fibrin (PRF) along with use of alloplastic bone mineral.</p></div><div><h3>Results</h3><p>A decrease in probing pocket depth, gain in clinical attachment level and significant bone fill was observed at end of 6 months.</p></div><div><h3>Discussion</h3><p>The result obtained with the use of Platelet Rich Fibrin may be attributed to the sustained and simultaneous release of various growth factors over a period of 7 days.</p></div><div><h3>Conclusion</h3><p>According to the results obtained in this case report, it could be concluded that the positive clinical impact of additional application of PRF with alloplastic graft material in treatment of periodontal intrabony defect.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 621-625"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.023","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85062406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.028
Sindhujaa Vajravel, Poornima Saravanan
Aim
To assess the effects of different concentrations of chromium (25; 50; 100; 150 mg/l) in the plant, Alternanthera philoxeroides.
Method
Different concentrations of chromium (25; 50; 100; 150 mg/l) were applied for 12 days and assessed by measuring changes in the growth; photosynthetic pigments activities; and antioxidative enzymes: catalase (CAT); peroxidase (POD); ascorbate peroxidase (APX) and total soluble protein changes. Metabolic responses to chromium (Cr) exposure and metal uptake were also experimentated.
Results
It was found that chromium was accumulated in shoots and roots of A. philoxeroides. The shoots accumulated 111.27 mg Cr/g of their dry weight at 150 mg/l Cr concentration, while the roots accumulated 751.71 mg Cr/g. The photosynthetic pigment contents increased with the higher concentration of Cr. Both in shoots and roots Cr could induce rise of the activity of CAT; POD and APX. The total soluble protein contents also increased with the increased concentration of Cr.
Conclusion
The results from the present experiments suggest that high concentrations of Cr cause oxidative damage as evidenced by increased antioxidative enzymes, photosynthetic pigments and changes in total soluble protein content. Induction of antioxidative enzymes could the reason for tolerating higher levels of metals by A. philoxeroides plants.
{"title":"Accumulation of chromium and its effects on physiological and biochemical parameters of Alternanthera philoxeroides seedlings","authors":"Sindhujaa Vajravel, Poornima Saravanan","doi":"10.1016/j.jopr.2013.07.028","DOIUrl":"10.1016/j.jopr.2013.07.028","url":null,"abstract":"<div><h3>Aim</h3><p>To assess the effects of different concentrations of chromium (25; 50; 100; 150 mg/l) in the plant, <em>Alternanthera philoxeroides</em>.</p></div><div><h3>Method</h3><p>Different concentrations of chromium (25; 50; 100; 150 mg/l) were applied for 12 days and assessed by measuring changes in the growth; photosynthetic pigments activities; and antioxidative enzymes: catalase (CAT); peroxidase (POD); ascorbate peroxidase (APX) and total soluble protein changes. Metabolic responses to chromium (Cr) exposure and metal uptake were also experimentated.</p></div><div><h3>Results</h3><p>It was found that chromium was accumulated in shoots and roots of <em>A. philoxeroides</em>. The shoots accumulated 111.27 mg Cr/g of their dry weight at 150 mg/l Cr concentration, while the roots accumulated 751.71 mg Cr/g. The photosynthetic pigment contents increased with the higher concentration of Cr. Both in shoots and roots Cr could induce rise of the activity of CAT; POD and APX. The total soluble protein contents also increased with the increased concentration of Cr.</p></div><div><h3>Conclusion</h3><p>The results from the present experiments suggest that high concentrations of Cr cause oxidative damage as evidenced by increased antioxidative enzymes, photosynthetic pigments and changes in total soluble protein content. Induction of antioxidative enzymes could the reason for tolerating higher levels of metals by <em>A. philoxeroides</em> plants.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 633-639"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.028","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86026748","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.06.026
Santhosh Kumar Chinnaiyan , Mohan Raj Subramanian , S. Vinoth Kumar , Atul N. Chandu , Karthikeyan Deivasigamani
Rationale
Resistance against antibiotics of numerous bacteria is accumulating. Therefore, searches for innovative substances with antimicrobial activity have become an insistent necessity. Medicinal plants are recurrently used in popular medicine as remedies for many infectious diseases.
Aim
This study aimed to determine the in-vitro antimicrobial and anti-HIV activity of Canthium coromandelicum leaf extract against bacteria, fungi and viral component.
Methods
The plant extract screened for their antimicrobial activity against ten bacterial strains including Gram negative, Gram-positive bacteria, and six fungal strains using agar well diffusion, and microbroth dilution assays. The in-vitro anti-HIV assay was performed by reverse transcriptase (RT) and gp120 binding inhibition assay.
Results
The methanolic extract showed the broad spectrum antimicrobial activity. The minimum inhibitory concentration of 64, 124 μg/ml showed against Salmonella typhi and Candida albicans respectively. The methanolic extract exhibit highest inhibition on HIV reverse transcriptase 78.67 ± 0.13 and glycoprotein 120 binding 72.52 ± 0.13.
Conclusion
The overall results provide information for the possible use of C. coromandelicum leaf extract in the control of microbial and HIV infections.
{"title":"Antimicrobial and anti-HIV activity of extracts of Canthium coromandelicum (Burm.f.) Alston leaves","authors":"Santhosh Kumar Chinnaiyan , Mohan Raj Subramanian , S. Vinoth Kumar , Atul N. Chandu , Karthikeyan Deivasigamani","doi":"10.1016/j.jopr.2013.06.026","DOIUrl":"10.1016/j.jopr.2013.06.026","url":null,"abstract":"<div><h3>Rationale</h3><p>Resistance against antibiotics of numerous bacteria is accumulating. Therefore, searches for innovative substances with antimicrobial activity have become an insistent necessity. Medicinal plants are recurrently used in popular medicine as remedies for many infectious diseases.</p></div><div><h3>Aim</h3><p>This study aimed to determine the <em>in-vitro</em> antimicrobial and anti-HIV activity of <em>Canthium coromandelicum</em> leaf extract against bacteria, fungi and viral component.</p></div><div><h3>Methods</h3><p>The plant extract screened for their antimicrobial activity against ten bacterial strains including Gram negative, Gram-positive bacteria, and six fungal strains using agar well diffusion, and microbroth dilution assays. The <em>in-vitro</em> anti-HIV assay was performed by reverse transcriptase (RT) and gp120 binding inhibition assay.</p></div><div><h3>Results</h3><p>The methanolic extract showed the broad spectrum antimicrobial activity. The minimum inhibitory concentration of 64, 124 μg/ml showed against <em>Salmonella typhi</em> and <em>Candida albicans</em> respectively. The methanolic extract exhibit highest inhibition on HIV reverse transcriptase 78.67 ± 0.13 and glycoprotein 120 binding 72.52 ± 0.13.</p></div><div><h3>Conclusion</h3><p>The overall results provide information for the possible use of <em>C. coromandelicum</em> leaf extract in the control of microbial and HIV infections.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 588-594"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.026","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74425770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.022
Jitendra D. Bhosale , Amey R. Shirolkar , Umesh D. Pete , Chetan M. Zade , Dipesh P. Mahajan , Chakradhar D. Hadole , Sharad D. Pawar , Umesh D. Patil , Rajesh Dabur , R.S. Bendre
Aim
Synthesis of some novel formazan derivatives from condensation of aniline diazonium salt with a variety of Schiff bases of 3,4-dimethyl-1H-pyrrole-2-carbohydrazide moiety and evaluate their potential antimicrobial and antioxidant activities.
Methods
Novel substituted formazans (2a-j) were prepared from Schiff bases of 3,4-dimethyl-1H-pyrrole-2-carbohydrazide (1a-j) by condensation with aniline diazonium chloride in pyridine (Scheme 1). All the formazan derivatives were characterized by IR, 1H NMR, 13C NMR and Mass spectroscopy.
Results
These molecules (2a-j) exhibits moderate to good antimicrobial and antioxidant activities some of which are comparable to standards used in this study.
Conclusion
The results of preliminary bioassays of derivatisation of Schiff bases to formazan indicate that a number of these molecules exhibits moderate to good antibacterial, antifungal and antioxidant activities some of which are comparable to standard used in this study. The outcome indicates that there is a good scope for evaluation of this class of compounds as potential leads towards antimicrobial and antioxidant agents.
{"title":"Synthesis, characterization and biological activities of novel substituted formazans of 3,4-dimethyl-1H-pyrrole-2-carbohydrazide derivatives","authors":"Jitendra D. Bhosale , Amey R. Shirolkar , Umesh D. Pete , Chetan M. Zade , Dipesh P. Mahajan , Chakradhar D. Hadole , Sharad D. Pawar , Umesh D. Patil , Rajesh Dabur , R.S. Bendre","doi":"10.1016/j.jopr.2013.07.022","DOIUrl":"10.1016/j.jopr.2013.07.022","url":null,"abstract":"<div><h3>Aim</h3><p>Synthesis of some novel formazan derivatives from condensation of aniline diazonium salt with a variety of Schiff bases of 3,4-dimethyl-1<em>H</em>-pyrrole-2-carbohydrazide moiety and evaluate their potential antimicrobial and antioxidant activities.</p></div><div><h3>Methods</h3><p>Novel substituted formazans <strong>(2a-j)</strong> were prepared from Schiff bases of 3,4-dimethyl-1<em>H</em>-pyrrole-2-carbohydrazide <strong>(1a-j)</strong> by condensation with aniline diazonium chloride in pyridine (<span>Scheme 1</span>). All the formazan derivatives were characterized by IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR and Mass spectroscopy.</p></div><div><h3>Results</h3><p>These molecules <strong>(2a-j)</strong> exhibits moderate to good antimicrobial and antioxidant activities some of which are comparable to standards used in this study.</p></div><div><h3>Conclusion</h3><p>The results of preliminary bioassays of derivatisation of Schiff bases to formazan indicate that a number of these molecules exhibits moderate to good antibacterial, antifungal and antioxidant activities some of which are comparable to standard used in this study. The outcome indicates that there is a good scope for evaluation of this class of compounds as potential leads towards antimicrobial and antioxidant agents.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 582-587"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.022","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79291828","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.029
Pradeepa V. Samaga, V. Ravishankar Rai
Background
Phenolic content of the plants and their associated bioactivities depend upon the geographical regions where they grow. Therefore antimicrobial, antioxidant activities and phenolic profile of Hypericum japonicum collected from Western Ghats of Karnataka, India had been evaluated in this study.
Methods
Total phenolic and flavonol contents of H. japonicum methanolic extract was estimated spectrometrically. The extract was qualitatively screened for bioactive phytochemicals. Antimicrobial activity was assessed by disk diffusion and broth microdilution methods. The extract was tested for DPPH scavenging, molybdenum reduction, lipid peroxidation inhibition, DNA damage protection and β-carotene bleaching inhibition. Phenolic profiling of the extract was done by high performance liquid chromatography.
Results
The extract inhibited all tested bacteria except Pseudomonas aeruginosa. Total antioxidant activity of the extract was 37.28 ± 0.54 μg/mg. IC50 value for DPPH radical quenching was 77.7 ± 5.6 μg (P < 0.05). β-carotene bleaching and lipid peroxidation were inhibited by 83.18% and 95.38% respectively. The extract also protected the DNA from hydroxyl radical mediated damage. Chlorogenic acid, ferulic acid, vanillic acid, quercetin, epicatechin and phloroglucinol were profiled in the extract.
Conclusion
This is the first report on bioactivity and phenolic profile of H. japonicum growing in Western Ghats, Karnataka, India. The study evidently showed the potency of H. japonicum from Western Ghats to be used in the food and pharmaceutical industries as a dietary supplement of antioxidants and rich source of vital phenolic acids and flavonoids.
{"title":"Evaluation of pharmacological properties and phenolic profile of Hypericum japonicum Thunb. from Western Ghats of India","authors":"Pradeepa V. Samaga, V. Ravishankar Rai","doi":"10.1016/j.jopr.2013.07.029","DOIUrl":"10.1016/j.jopr.2013.07.029","url":null,"abstract":"<div><h3>Background</h3><p>Phenolic content of the plants and their associated bioactivities depend upon the geographical regions where they grow. Therefore antimicrobial, antioxidant activities and phenolic profile of <em>Hypericum japonicum</em> collected from Western Ghats of Karnataka, India had been evaluated in this study.</p></div><div><h3>Methods</h3><p>Total phenolic and flavonol contents of <em>H. japonicum</em> methanolic extract was estimated spectrometrically. The extract was qualitatively screened for bioactive phytochemicals. Antimicrobial activity was assessed by disk diffusion and broth microdilution methods. The extract was tested for DPPH scavenging, molybdenum reduction, lipid peroxidation inhibition, DNA damage protection and β-carotene bleaching inhibition. Phenolic profiling of the extract was done by high performance liquid chromatography.</p></div><div><h3>Results</h3><p>The extract inhibited all tested bacteria except <em>Pseudomonas aeruginosa</em>. Total antioxidant activity of the extract was 37.28 ± 0.54 μg/mg. IC<sub>50</sub> value for DPPH radical quenching was 77.7 ± 5.6 μg (<em>P</em> < 0.05). β-carotene bleaching and lipid peroxidation were inhibited by 83.18% and 95.38% respectively. The extract also protected the DNA from hydroxyl radical mediated damage. Chlorogenic acid, ferulic acid, vanillic acid, quercetin, epicatechin and phloroglucinol were profiled in the extract.</p></div><div><h3>Conclusion</h3><p>This is the first report on bioactivity and phenolic profile of <em>H. japonicum</em> growing in Western Ghats, Karnataka, India. The study evidently showed the potency of <em>H. japonicum</em> from Western Ghats to be used in the food and pharmaceutical industries as a dietary supplement of antioxidants and rich source of vital phenolic acids and flavonoids.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 626-632"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.029","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88390088","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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