Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.030
Yatharth Anand , Sunil Pande , Dilip Gore
Aim
To develop vaccine leads by reverse vaccinology approach for Shigella sonnei.
Materials and methods
Study screened the coding proteins of S. sonnei as vaccine targets collected from NCBI website and filtered as cell surface proteins using programs such as SignalP 4.1, TMHMM, LipoP 1.0, PsortB and BLASTP.
Observation and results
In recent years due to rapid development in genome sequencing technology vaccine development program has achieved defined specificity and success. In our study, in total 63 cell surface proteins as vaccine leads were searched which are highly conserved among genus Shigella.
Conclusion
Study successfully used reverse vaccinology in search of vaccine leads in S. sonnei.
{"title":"Reverse vaccinology: An approach to search vaccine leads of Shigella sonnei","authors":"Yatharth Anand , Sunil Pande , Dilip Gore","doi":"10.1016/j.jopr.2013.07.030","DOIUrl":"10.1016/j.jopr.2013.07.030","url":null,"abstract":"<div><h3>Aim</h3><p>To develop vaccine leads by reverse vaccinology approach for <em>Shigella sonnei</em>.</p></div><div><h3>Materials and methods</h3><p>Study screened the coding proteins of <em>S. sonnei</em> as vaccine targets collected from NCBI website and filtered as cell surface proteins using programs such as SignalP 4.1, TMHMM, LipoP 1.0, PsortB and BLASTP.</p></div><div><h3>Observation and results</h3><p>In recent years due to rapid development in genome sequencing technology vaccine development program has achieved defined specificity and success. In our study, in total 63 cell surface proteins as vaccine leads were searched which are highly conserved among genus Shigella.</p></div><div><h3>Conclusion</h3><p>Study successfully used reverse vaccinology in search of vaccine leads in <em>S. sonnei</em>.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 576-581"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.030","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82460488","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}
To develop a stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method for the determination of related substances in Metoclopramide bulk drugs and pharmaceutical dosage form.
Method
The chromatographic separation was achieved using a Waters X-terra RP18 (150 × 4.6 mm), 3.5 μm particle size column using the gradient program with mobile phase consisting of solvent A: 30 mM monobasic sodium phosphate and 2.3 mM of pentane-1-sulphonic acid sodium salt (pH 3.0 buffer) and solvent-B (Acetonitrile). A flow rate of 1.2 mL/min and UV detector at 273 nm was used. The runtime was 18 min within which Metoclopramide and its four impurities, ACETYLMETO, ACMA, CLEE and ACME were well separated.
Results and discussion
The drug was subjected to stress conditions such as oxidative, acid & base hydrolysis, thermal and photolytic degradation. Metoclopramide was found to degrade significantly in photolytic, oxidative & thermal stress conditions and stable in acid, base, hydrolytic & humidity stress conditions. The major degradation impurities in oxidation and photolytic degradation were identified by LCMS. The degradation products were well resolved from the main peak and its impurities, thus proved the stability-indicating power of the method.
Conclusion
The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. The calibration curves obtained for the four impurities were linear over the range 0.062–3.040 μg/mL.
{"title":"Novel validated stability-indicating UPLC method for the determination of Metoclopramide and its degradation impurities in API and pharmaceutical dosage form","authors":"Prathyusha Sowjanya , Palani Shanmugasundaram , Petla Naidu , Sanjeev Kumar Singamsetty","doi":"10.1016/j.jopr.2013.07.004","DOIUrl":"10.1016/j.jopr.2013.07.004","url":null,"abstract":"<div><h3>Aim</h3><p>To develop a stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method for the determination of related substances in Metoclopramide bulk drugs and pharmaceutical dosage form.</p></div><div><h3>Method</h3><p>The chromatographic separation was achieved using a Waters X-terra RP18 (150 × 4.6 mm), 3.5 μm particle size column using the gradient program with mobile phase consisting of solvent A: 30 mM monobasic sodium phosphate and 2.3 mM of pentane-1-sulphonic acid sodium salt (pH 3.0 buffer) and solvent-B (Acetonitrile). A flow rate of 1.2 mL/min and UV detector at 273 nm was used. The runtime was 18 min within which Metoclopramide and its four impurities, ACETYLMETO, ACMA, CLEE and ACME were well separated.</p></div><div><h3>Results and discussion</h3><p>The drug was subjected to stress conditions such as oxidative, acid & base hydrolysis, thermal and photolytic degradation. Metoclopramide was found to degrade significantly in photolytic, oxidative & thermal stress conditions and stable in acid, base, hydrolytic & humidity stress conditions. The major degradation impurities in oxidation and photolytic degradation were identified by LCMS. The degradation products were well resolved from the main peak and its impurities, thus proved the stability-indicating power of the method.</p></div><div><h3>Conclusion</h3><p>The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. The calibration curves obtained for the four impurities were linear over the range 0.062–3.040 μg/mL.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 765-773"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81469690","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.2013.07.009
Acharya Nagarjun Pyde , P. Nagaraja Rao , Aditya Jain , Divya Soni , Shailesh Saket , Sheaza Ahmed , Sugunakar Vuree , Anuraj Nayarisseri
Aim
Listeria monocytogenes acts as a pathogen for humans and animals, mainly causing, neonatal sepsis, abortions in pregnant females and severe infections such as septicemia and meningoencephalitis in susceptible hosts. Current study was aimed to identify novel strains of L. monocytogenes from retail chicken, beef meat and seafood samples.
Methods
In order to identify the strain, extraction and amplification of genomic DNA, 16S rRNA sequence analysis was carried out. Phylogenetic trees were constructed using dnapars and dnaml available in Phylip. The secondary structures of 16S rRNA gene sequence were predicted using UNAFOLD, a Linux based software.
Results
The results obtained were found to be a novel foodborne pathogens, which was further named L. monocytogenes strain Pyde1 and L. monocytogenes strain Pyde2, after characterization the sequence of isolate was deposited in GenBank with accession numbers ‘KC852899’ and ‘KC852900’ respectively. The Gibb's free energy of the secondary structures of L. monocytogenes strain Pyde1 and Pyde2 were −275.60 and −282.20 kcal/mol seems to be more stable in the present investigation.
Conclusion
The described results of phylogenetic distinctiveness and phenotypic disparities indicate that strain 2b represents a novel strain of foodborne pathogens within L. monocytogenes species, for which the name L. monocytogenes strain Pyde1 and L. monocytogenes strain Pyde2 is proposed.
{"title":"Identification and characterization of foodborne pathogen Listeria monocytogenes strain Pyde1 and Pyde2 using 16S rRNA gene sequencing","authors":"Acharya Nagarjun Pyde , P. Nagaraja Rao , Aditya Jain , Divya Soni , Shailesh Saket , Sheaza Ahmed , Sugunakar Vuree , Anuraj Nayarisseri","doi":"10.1016/j.jopr.2013.07.009","DOIUrl":"10.1016/j.jopr.2013.07.009","url":null,"abstract":"<div><h3>Aim</h3><p><em>Listeria monocytogenes</em> acts as a pathogen for humans and animals, mainly causing, neonatal sepsis, abortions in pregnant females and severe infections such as septicemia and meningoencephalitis in susceptible hosts. Current study was aimed to identify novel strains of <em>L. monocytogenes</em> from retail chicken, beef meat and seafood samples.</p></div><div><h3>Methods</h3><p>In order to identify the strain, extraction and amplification of genomic DNA, 16S rRNA sequence analysis was carried out. Phylogenetic trees were constructed using dnapars and dnaml available in Phylip. The secondary structures of 16S rRNA gene sequence were predicted using UNAFOLD, a Linux based software.</p></div><div><h3>Results</h3><p>The results obtained were found to be a novel foodborne pathogens, which was further named <em>L. monocytogenes</em> strain <em>Pyde1</em> and <em>L. monocytogenes</em> strain <em>Pyde2</em>, after characterization the sequence of isolate was deposited in GenBank with accession numbers ‘KC852899’ and ‘KC852900’ respectively. The Gibb's free energy of the secondary structures of <em>L. monocytogenes</em> strain <em>Pyde1</em> and <em>Pyde2</em> were −275.60 and −282.20 kcal/mol seems to be more stable in the present investigation.</p></div><div><h3>Conclusion</h3><p>The described results of phylogenetic distinctiveness and phenotypic disparities indicate that strain 2b represents a novel strain of foodborne pathogens within <em>L. monocytogenes</em> species, for which the name <em>L. monocytogenes</em> strain <em>Pyde1</em> and <em>L. monocytogenes</em> strain <em>Pyde2</em> is proposed.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 736-741"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.009","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88070963","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}
Cuscuta reflexa Roxb., (Convolvulaceae), is well known medicinal plant in Indian System of Medicine for various ailments. We have explored antiproliferative properties of Cuscuta reflexa (whole plant).
Methods
Three extracts (95% alcoholic, 50% hydro-alcoholic and aqueous) and four fractions (n-hexane, chloroform, n-butanol and aqueous) were prepared. In vitro cytotoxicity was observed by using SRB assay and in vivo antitumor activity was also performed using murine models.
Results
The alcoholic extract and its chloroform fraction were found to be most potent among three extracts and four fractions of alcoholic extract. It showed maximum cytotoxicity against human breast (MCF-7) cancer cell lines. The alcoholic extract showed significant (p < 0.05) tumor growth inhibition at 40 mg/kg which were 42.62% and 25.96% for Ehrlich tumor and Sarcoma −180 solid tumor model respectively. Similarly, chloroform fraction of alcoholic extract showed significant tumor growth inhibition of 48.98% and 44.11% for Ehrlich tumor and Sarcoma-180 solid tumor model at 10 mg/kg respectively.
Conclusion
This study indicates that the cytotoxic potential of Cuscuta reflexa lies in its alcoholic extract and chloroform fraction of alcoholic extract of the whole plant due to interference in cell proliferation.
{"title":"In vitro and in vivo antiproliferative potential of Cuscuta reflexa Roxb.","authors":"Madhulika Bhagat , Jatinder Singh Arora , Ajit Kumar Saxena","doi":"10.1016/j.jopr.2013.06.005","DOIUrl":"10.1016/j.jopr.2013.06.005","url":null,"abstract":"<div><h3>Background</h3><p><em>Cuscuta reflexa</em> Roxb., (Convolvulaceae), is well known medicinal plant in Indian System of Medicine for various ailments. We have explored antiproliferative properties of <em>Cuscuta reflexa</em> (whole plant).</p></div><div><h3>Methods</h3><p>Three extracts (95% alcoholic, 50% hydro-alcoholic and aqueous) and four fractions (n-hexane, chloroform, n-butanol and aqueous) were prepared. <em>In vitro</em> cytotoxicity was observed by using SRB assay and <em>in vivo</em> antitumor activity was also performed using murine models.</p></div><div><h3>Results</h3><p>The alcoholic extract and its chloroform fraction were found to be most potent among three extracts and four fractions of alcoholic extract. It showed maximum cytotoxicity against human breast (MCF-7) cancer cell lines. The alcoholic extract showed significant (<em>p</em> < 0.05) tumor growth inhibition at 40 mg/kg which were 42.62% and 25.96% for Ehrlich tumor and Sarcoma −180 solid tumor model respectively. Similarly, chloroform fraction of alcoholic extract showed significant tumor growth inhibition of 48.98% and 44.11% for Ehrlich tumor and Sarcoma-180 solid tumor model at 10 mg/kg respectively.</p></div><div><h3>Conclusion</h3><p>This study indicates that the cytotoxic potential of <em>Cuscuta reflexa</em> lies in its alcoholic extract and chloroform fraction of alcoholic extract of the whole plant due to interference in cell proliferation.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 690-695"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91193475","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.2013.07.005
Md. Saifuzzaman , Md. Sarowar Jahan Shamim , Kamanashis Mahaldar , Eunus Sheemul Ali , Md. Amirul Islam
Background
Persicaria acuminata Sach. (Family – Polygonaceae) commonly known as Bishkathali is a Bangladeshi native plant which is traditionally used in painful conditions.
Objective
The aim of the present study was to evaluate antinociceptive effect of the plant and to prove the scientific basis of traditional use.
Methods
The ethanolic extracts of leaf and stem of the plant were investigated using acetic acid induced writhing method on animal model.
Results
Oral administration of both leaf and stem extracts at the doses of 250 and 500 mg/kg body weight showed significant and dose-dependent inhibition of writhing response.
Conclusion
The study signifies the antinociceptive activity of the plant and supports its popular folkloric use in the management of pain.
{"title":"Antinociceptive activity of the ethanolic extract of Persicaria acuminata Sach.","authors":"Md. Saifuzzaman , Md. Sarowar Jahan Shamim , Kamanashis Mahaldar , Eunus Sheemul Ali , Md. Amirul Islam","doi":"10.1016/j.jopr.2013.07.005","DOIUrl":"10.1016/j.jopr.2013.07.005","url":null,"abstract":"<div><h3>Background</h3><p><em>Persicaria acuminata</em> Sach. (Family – Polygonaceae) commonly known as Bishkathali is a Bangladeshi native plant which is traditionally used in painful conditions.</p></div><div><h3>Objective</h3><p>The aim of the present study was to evaluate antinociceptive effect of the plant and to prove the scientific basis of traditional use.</p></div><div><h3>Methods</h3><p>The ethanolic extracts of leaf and stem of the plant were investigated using acetic acid induced writhing method on animal model.</p></div><div><h3>Results</h3><p>Oral administration of both leaf and stem extracts at the doses of 250 and 500 mg/kg body weight showed significant and dose-dependent inhibition of writhing response.</p></div><div><h3>Conclusion</h3><p>The study signifies the antinociceptive activity of the plant and supports its popular folkloric use in the management of pain.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 753-755"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87569666","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.2013.07.011
Sarita Pawar , Akhilesh Roy , Sanjay Wagh
Aim
In the present study ten dibenzothiazepines with a methylene bridge between tricyclic nucleus and the substituent at C-11 were synthesized in order to investigate their antipsychotic activity. Some of the derivatives showed significant activity.
Methods
The title compounds were synthesized by condensation of 11-piperazinyl-dibenzothiazepine with the substituted benzyl halides in presence of triethylamine and 1,4-dioxane. The structures of the derivatives were elucidated by spectral analysis. The antipsychotic activity of the synthesized derivatives was evaluated using haloperidol induced catalepsy and lithium induced head twitches.
Results
In SSP-9 treated group, maximum catalepsy was noted 30 min after haloperidol. Lithium induced 40.2 ± 1.655 head twitches in 1 h. Clozapine (5 mg per kg) and SSP-9 (5 mg per kg) reduced the number of head twitches to 10 ± 0.7071 and 14.8 ± 0.8602, respectively.
Conclusion
The results demonstrated that the derivative SSP-9 possesses significant in vitro antipsychotic activity when compared with standard clozapine. Therefore, compound SSP-9 prototype could be considered as novel antipsychotic agent for further developing new atypical antipsychotics.
{"title":"Synthesis and pharmacological evaluation of some new dibenzo [b, f] [1, 4]thiazepines","authors":"Sarita Pawar , Akhilesh Roy , Sanjay Wagh","doi":"10.1016/j.jopr.2013.07.011","DOIUrl":"10.1016/j.jopr.2013.07.011","url":null,"abstract":"<div><h3>Aim</h3><p>In the present study ten dibenzothiazepines with a methylene bridge between tricyclic nucleus and the substituent at C-11 were synthesized in order to investigate their antipsychotic activity. Some of the derivatives showed significant activity.</p></div><div><h3>Methods</h3><p>The title compounds were synthesized by condensation of 11-piperazinyl-dibenzothiazepine with the substituted benzyl halides in presence of triethylamine and 1,4-dioxane. The structures of the derivatives were elucidated by spectral analysis. The antipsychotic activity of the synthesized derivatives was evaluated using haloperidol induced catalepsy and lithium induced head twitches.</p></div><div><h3>Results</h3><p>In SSP-9 treated group, maximum catalepsy was noted 30 min after haloperidol. Lithium induced 40.2 ± 1.655 head twitches in 1 h. Clozapine (5 mg per kg) and SSP-9 (5 mg per kg) reduced the number of head twitches to 10 ± 0.7071 and 14.8 ± 0.8602, respectively.</p></div><div><h3>Conclusion</h3><p>The results demonstrated that the derivative SSP-9 possesses significant in vitro antipsychotic activity when compared with standard clozapine. Therefore, compound SSP-9 prototype could be considered as novel antipsychotic agent for further developing new atypical antipsychotics.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 756-760"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.011","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87720282","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.2013.04.020
S.K. Kushwaha , A. Dashora , N. Dashora , J.R. Patel , M.L. Kori
Objectives
To determine the acute toxicity of standardized methanolic extract of Phyllanthus amarus in vivo in female albino rats.
Methods
Treated group of animals were administrated 300, 600, 2000 and 5000 mg/kg body weight of extract orally and the control group received standard laboratory diet and water ad libitum following OECD guideline 423 with some modifications. All animals were sacrificed after 14 days of treatment.
Results
The extract was standardized by HPLC to contain phyllanthin and hypophyllanthin. No mortality was noted and the study exhibited no significant changes in general behavior, body weight, gross appearance of internal organs, hematological and biochemical parameters and the histological profile of liver also indicated the nontoxic nature of this drug. Biochemical studies showed no significant change in the levels of ALT, AST, albumin, triglycerides, cholesterol and albumin. There were no evidence found about congestion of sinusoids, hemorrhage, hepatocytes, fatty changes, centrilobular necrosis and the changes in number of Kupffer cells in the liver. There was no increase of blood pressure and does not induce any nephrotoxicity and acute severe hepatotoxicity.
Conclusion
The present study provides pivotal evidences for ascertaining the safety of the standardized MEPA (LD50 > 5000 mg/kg) that could be used as tonic or food supplement in folklore medicine.
{"title":"Acute oral toxicity studies of the standardized methanolic extract of Phyllanthus amarus Schum & Thonn","authors":"S.K. Kushwaha , A. Dashora , N. Dashora , J.R. Patel , M.L. Kori","doi":"10.1016/j.jopr.2013.04.020","DOIUrl":"10.1016/j.jopr.2013.04.020","url":null,"abstract":"<div><h3>Objectives</h3><p>To determine the acute toxicity of standardized methanolic extract of <em>Phyllanthus amarus in vivo</em> in female albino rats.</p></div><div><h3>Methods</h3><p>Treated group of animals were administrated 300, 600, 2000 and 5000 mg/kg body weight of extract orally and the control group received standard laboratory diet and water <em>ad libitum</em> following OECD guideline 423 with some modifications. All animals were sacrificed after 14 days of treatment.</p></div><div><h3>Results</h3><p>The extract was standardized by HPLC to contain phyllanthin and hypophyllanthin. No mortality was noted and the study exhibited no significant changes in general behavior, body weight, gross appearance of internal organs, hematological and biochemical parameters and the histological profile of liver also indicated the nontoxic nature of this drug. Biochemical studies showed no significant change in the levels of ALT, AST, albumin, triglycerides, cholesterol and albumin. There were no evidence found about congestion of sinusoids, hemorrhage, hepatocytes, fatty changes, centrilobular necrosis and the changes in number of Kupffer cells in the liver. There was no increase of blood pressure and does not induce any nephrotoxicity and acute severe hepatotoxicity.</p></div><div><h3>Conclusion</h3><p>The present study provides pivotal evidences for ascertaining the safety of the standardized MEPA (LD<sub>50</sub> > 5000 mg/kg) that could be used as tonic or food supplement in folklore medicine.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 720-724"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.04.020","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86615106","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.2013.07.001
Syamsudin Abdillah , Awik Puji Dyah Nurhayati , Sri Nurhatika , Edwin Setiawan , Wan Lelly Heffen
Objective
A study on the cytotoxic and antioxidant activities of Sponges collected from Pecaron Bay Pasir Putih Situbondo was conducted. This study aimed at screening the hydro-ethanolic extracts of 7 sponge species: Callyspongia sp, Acanthella sp and Xestospongia sp colleted at the Pecaron Situbondo, East Java, Indonesia for antiproliferative and antioxidant activities.
Methods
After collection, the species were immediately immersed in ethanol and stored at low temperatures (−20 °C) until use. Cytotoxic assay was conducted using MTT methods for some cancerous cells, including T47D, Casky and HT-29 meanwhile antioxidant assay was conducted using DPPH method.
Results
the extracts from species A. suberitoides has the highest toxicity compare to another species which valued level on tumor cell lines (HT-29, T47D and Casky). Antioxidant assay using DPPH method found that only Aaptos suberitoides that had been identified to show strong activity due to IC50 value of <30 μg/mL; meanwhile Fascaplysinopsis reticulata, Acanthella sp, Petrosia contignata and Xestospongia exigua showed moderate antioxidant activity with a IC50 < 100 μg/mL. Xestospongia sp, Callyspongia sp showed a value of IC50 > 100 μg/mL.
Conclusion
The study showed that Xestospongia sp, Fascaplysinopsis reticulata, Callyspongia sp, Petrosia contignata, Aaptos suberitoides were highly potential to develop for isolation of bioactive compounds as anticancer and antioxidant agents.
{"title":"Cytotoxic and antioxidant activities of marine sponge diversity at Pecaron Bay Pasir Putih Situbondo East Java, Indonesia","authors":"Syamsudin Abdillah , Awik Puji Dyah Nurhayati , Sri Nurhatika , Edwin Setiawan , Wan Lelly Heffen","doi":"10.1016/j.jopr.2013.07.001","DOIUrl":"10.1016/j.jopr.2013.07.001","url":null,"abstract":"<div><h3>Objective</h3><p>A study on the cytotoxic and antioxidant activities of Sponges collected from Pecaron Bay Pasir Putih Situbondo was conducted. This study aimed at screening the hydro-ethanolic extracts of 7 sponge species: <em>Callyspongia</em> sp, <em>Acanthella</em> sp and <em>Xestospongia</em> sp colleted at the Pecaron Situbondo, East Java, Indonesia for antiproliferative and antioxidant activities.</p></div><div><h3>Methods</h3><p>After collection, the species were immediately immersed in ethanol and stored at low temperatures (−20 °C) until use. Cytotoxic assay was conducted using MTT methods for some cancerous cells, including T47D, Casky and HT-29 meanwhile antioxidant assay was conducted using DPPH method.</p></div><div><h3>Results</h3><p>the extracts from species <em>A. suberitoides</em> has the highest toxicity compare to another species which valued level on tumor cell lines (HT-29, T47D and Casky). Antioxidant assay using DPPH method found that only <em>Aaptos suberitoides</em> that had been identified to show strong activity due to IC<sub>50</sub> value of <30 μg/mL; meanwhile <em>Fascaplysinopsis reticulata</em>, <em>Acanthella</em> sp, <em>Petrosia contignata</em> and <em>Xestospongia exigua</em> showed moderate antioxidant activity with a IC<sub>50</sub> < 100 μg/mL. <em>Xestospongia</em> sp<em>, Callyspongia</em> sp showed a value of IC<sub>50</sub> > 100 μg/mL.</p></div><div><h3>Conclusion</h3><p>The study showed that <em>Xestospongia</em> sp<em>, Fascaplysinopsis reticulata, Callyspongia</em> sp, <em>Petrosia contignata</em>, <em>Aaptos suberitoides</em> were highly potential to develop for isolation of bioactive compounds as anticancer and antioxidant agents.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 685-689"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74629095","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.2013.07.024
Elizabeth M. Mathew , Kingston Rajiah , Krishana Kumar Sharma
Aim
Printed education materials are often used to augment healthcare professional's verbal information to consumers so it serves as an important component of symptom management. They also enhance the teaching process and can be used by consumers as a home reference. This study was aimed to interpret consumers' perception on Consumer Medical Information Leaflets (CMILs) on obesity and lipid lowering drugs, according to the standard formulae such as Flesch Reading Ease (FRE), Flesch–Kincaid Grade Level (FK-GL).
Method
The study was conducted over a period of 3 years in community pharmacy settings in Tamil Nadu, India. CMILs were interpreted by using the formulae such as Flesch Reading Ease (FRE) and Flesch–Kincaid Grade Level (FK-GL). Among the 1800 consumers, 300 consumers were excluded from the study due to lack of interest.
Results
Data revealed the consumer's perception on readability of Consumer Medical Information Leaflets on obesity and lipid lowering drugs based consumers rating.
Conclusions
Pharmaceutical companies (leaflets providers) are not taking the reading level of consumers into consideration which may not achieve the intended purpose. There is a need for developing CMILs having good readability score according to Indian set up.
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Pub Date : 2013-07-01DOI: 10.1016/j.jopr.2013.07.017
Sibi Narayanan , D. Velmurugan
Background
Cancer causes death to over 7.6 million people every year. The disease can be classified as cells' uncontrolled division. This uncontrolled division of cells or uncontrolled growth is caused by DNA damage. This eventually results in genes mutations, which encodes cell division controlling proteins. Histone deacetylase (HDAC) is one among the principal targets for the anticancer drugs.
Methods
Molecular docking studies of nearly 60 Trichostatin A, SuberoylAnilide Hydroxamic Acid and Sulfonamide anilides which show good inhibitory activity against HDAC were carried out using GLIDE program of Schrödinger Suite 2009. Comparison of docking scores of the compounds with their respective QSAR IC50 have also been made.
Results
From Trichostatin A and SuberoylAnilide Hydroxamic Acid analogues binding results, it was found that HDAC conformational changes are based on the ligand binding. C/N/O atoms present in the aliphatic chains of the analogues interacted well with the Zn2+ metal ion and active site amino acid residues to disrupt the enzymatic activity of target protein HDAC.
Conclusion
Analogue inhibition taken into study with the target protein HDAC assures to be an advantageous therapeutic approach in cancer treatment.
癌症每年导致超过760万人死亡。这种疾病可归类为细胞不受控制的分裂。这种不受控制的细胞分裂或不受控制的生长是由DNA损伤引起的。这最终导致基因突变，从而编码控制细胞分裂的蛋白质。组蛋白去乙酰化酶(HDAC)是抗癌药物的主要靶点之一。方法利用Schrödinger Suite 2009的GLIDE软件对近60种对HDAC具有良好抑制活性的曲古霉素A、亚羟肟酸和磺胺类苯胺进行分子对接研究。并将化合物的对接分数与其QSAR IC50进行了比较。结果从曲古霉素A与亚羟肟酸类似物的结合结果中发现，HDAC的构象变化是以配体结合为基础的。类似物的脂肪链上的C/N/O原子与Zn2+金属离子和活性位点氨基酸残基相互作用良好，破坏靶蛋白HDAC的酶活性。结论利用靶蛋白HDAC进行类似物抑制研究，有望成为治疗肿瘤的有效途径。
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