cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.7420868.v1
title: Effects of Cinnamomum cassia extract on oxidative stress, immunreactivity of iNOS and impaired thoracic aortic reactivity induced by type II diabetes in rats

description: Type II diabetes is known to cause neuropathy, nephropathy and retinopathy. However, cardiovascular disorders associated with diabetes have been ignored. In traditional medicine, cinnamon (Cinnamomum cassia) bark has been used for its abilities to relieve fever, inflammation and chronic bronchitis. In the present study, the effect of Cinnamomum cassia extract (CN) on the thoracic aorta in an experimental type II diabetes model was investigated. In rats administered with nicotinamide + streptozotocin, significant endothelial dysfunction and oxidative stress were characterised by increased inducible nitric oxide synthase (iNOS) and decreased insulin/proinsulin levels. This impairment was prevented by administering 1000 mg/kg metformin or 500-1000-1500 mg/kg CN. CN administration attenuated the inflammatory response by decreasing the levels of malondialdehyde (MDA), Nitric oxide (NO) and increasing Glutathione peroxidase (GPx), glutathione (GSH). In addition, CN administration was shown to cause down-regulating effects on iNOS in thoracic aorta. These findings reveal that CN could prevent chronic complications of experimentally induced type II diabetes by attenuating inflammation, oxidant/antioxidant imbalance, and normalised contraction and relaxion responses in the thoracic aorta.
DOI: 10.6084/m9.figshare.7419692
title: Cytotoxic and apoptotic potential of Myristica fragrans Houtt. (mace) extract on human oral epidermal carcinoma KB cell lines

description: Several studies have revealed that certain naturally occurring medicinal plants inhibit the growth of various cancers. The present study was conducted to evaluate cytotoxicity and apoptotic induction potential of Myristica fragrans Houtt mace extract. The cytotoxic activity of the Myristica fragrans Houtt mace acetone extract was assayed by MTT assay on human oral epidermal carcinoma KB cell lines. KB cells were incubated with different concentration of mace extract ranging from 25 to 125 μg/mL for 24hrs. The apoptotic induction potential was also studied by the analysis of Bcl-2 protein and gene expression in mace extract incubated KB cell lines using western blotting technique and real-time polymerase chain reaction. The mace extract exhibited cytotoxicity and anticancer effect against KB cell lines and it also suppressed the growth of cancer cells, therefore growth inhibitory effect was noted in extract treated cell lines. The apoptotic potential of mace extract was accompanied by reduced gene expression of Bcl-2 compared to the untreated KB cells. The mace extract shows the cytotoxic activity and induced the apoptosis through the modulation of its target genes Bcl-2 in the KB cell lines, suggesting the potential of mace as a candidate for oral cancer chemoprevention. This can be further investigated in vivo for its anticancer potential.
DOI: 10.6084/m9.figshare.7419692.v1
title: Cytotoxic and apoptotic potential of Myristica fragrans Houtt. (mace) extract on human oral epidermal carcinoma KB cell lines

description: Several studies have revealed that certain naturally occurring medicinal plants inhibit the growth of various cancers. The present study was conducted to evaluate cytotoxicity and apoptotic induction potential of Myristica fragrans Houtt mace extract. The cytotoxic activity of the Myristica fragrans Houtt mace acetone extract was assayed by MTT assay on human oral epidermal carcinoma KB cell lines. KB cells were incubated with different concentration of mace extract ranging from 25 to 125 μg/mL for 24hrs. The apoptotic induction potential was also studied by the analysis of Bcl-2 protein and gene expression in mace extract incubated KB cell lines using western blotting technique and real-time polymerase chain reaction. The mace extract exhibited cytotoxicity and anticancer effect against KB cell lines and it also suppressed the growth of cancer cells, therefore growth inhibitory effect was noted in extract treated cell lines. The apoptotic potential of mace extract was accompanied by reduced gene expression of Bcl-2 compared to the untreated KB cells. The mace extract shows the cytotoxic activity and induced the apoptosis through the modulation of its target genes Bcl-2 in the KB cell lines, suggesting the potential of mace as a candidate for oral cancer chemoprevention. This can be further investigated in vivo for its anticancer potential.
DOI: 10.6084/m9.figshare.7419716.v1
title: Protective effect of luteolin on the transgenic Drosophila model of Parkinson’s disease

description: In the present study we have studied the effect of 25, 50, 75 and 100 µM of luteolin on the transgenic Drosophila expressing human alpha synuclein. The doses of luteolin were established in diet and the PD flies were allowed to feed on it for 24 days. After 24 days of exposure the flies were assayed for climbing assay, oxidative stress markers, caspase-3 & 9 activity and dopamine content. The immunohistochemistry was also performed on the brain sections for the activity of tyrosine hydroxylase. The exposure of luteolin showed a dose dependent delay in the loss of climbing ability and activity, reduction in oxidative stress markers, caspase-3&9 activities and results in an increase in the dopamine content. The results obtained for the immunohistochemistry also supports the protective role of luteolin against the damage of the dopaminergic neurons.
DOI: 10.6084/m9.figshare.7419716
title: Protective effect of luteolin on the transgenic Drosophila model of Parkinson’s disease

description: In the present study we have studied the effect of 25, 50, 75 and 100 µM of luteolin on the transgenic Drosophila expressing human alpha synuclein. The doses of luteolin were established in diet and the PD flies were allowed to feed on it for 24 days. After 24 days of exposure the flies were assayed for climbing assay, oxidative stress markers, caspase-3 & 9 activity and dopamine content. The immunohistochemistry was also performed on the brain sections for the activity of tyrosine hydroxylase. The exposure of luteolin showed a dose dependent delay in the loss of climbing ability and activity, reduction in oxidative stress markers, caspase-3&9 activities and results in an increase in the dopamine content. The results obtained for the immunohistochemistry also supports the protective role of luteolin against the damage of the dopaminergic neurons.
DOI: 10.6084/m9.figshare.7419518.v1
title: Hypoglycemic activity of Capparis ovata desf. var. palaestina zoh. methanol extract

description: Caper (Capparis ovata Desf. and Capparis spinosa L.) is naturally widespread in Turkey. Traditionally, buds, fruits, seeds and roots of this plant are used as tonic, diuretic, anti-rheumatic, expectorant, antidiabetic, and antifungal. The aim of this study is to evaluate potential hypoglycemic effect of C. ovata var. palaestina extracts in alloxan-induced diabetic mice. For this purpose; diabetic mice were administered with 100, 300, 500 mg/kg (i.p.) doses of methanol extract of bud and fruit. Blood glucose levels were screened 60, 120, 240 and 360 min. after treatment. Furthermore, high resolution mass spectrometry (HRMS) analysis, ABTS and DPPH free radical scavenging activity test, and phenolic and flavonoid compounds analysis of extracts were carried out. The data obtained from in vivo study revealed that fruit-methanol 500 mg/kg (FM3), bud-methanol 300 mg/kg (BM2), bud-methanol 500 mg/kg (BM3) extracts showed significant hypoglycemic activity. All extracts indicated significant antioxidant activity, however bud-methanol (BM) extract demonstrated the most potent antioxidant activity. Moreover high levels of phenolic substances and flavonoids were involved in all extracts, but the highest levels were found in FM extract. HRMS study showed that rutin, quercetin 3-O-glucoside (isoquercitrin) and stachydrine substances had seen in BM extract. The results of this study showed that the C. ovata var. palaestina extracts which, indicate hypoglycemic, antioxidant activities, might provide additional support in diabetes.
DOI: 10.6084/m9.figshare.7419518
title: Hypoglycemic activity of Capparis ovata desf. var. palaestina zoh. methanol extract

description: Caper (Capparis ovata Desf. and Capparis spinosa L.) is naturally widespread in Turkey. Traditionally, buds, fruits, seeds and roots of this plant are used as tonic, diuretic, anti-rheumatic, expectorant, antidiabetic, and antifungal. The aim of this study is to evaluate potential hypoglycemic effect of C. ovata var. palaestina extracts in alloxan-induced diabetic mice. For this purpose; diabetic mice were administered with 100, 300, 500 mg/kg (i.p.) doses of methanol extract of bud and fruit. Blood glucose levels were screened 60, 120, 240 and 360 min. after treatment. Furthermore, high resolution mass spectrometry (HRMS) analysis, ABTS and DPPH free radical scavenging activity test, and phenolic and flavonoid compounds analysis of extracts were carried out. The data obtained from in vivo study revealed that fruit-methanol 500 mg/kg (FM3), bud-methanol 300 mg/kg (BM2), bud-methanol 500 mg/kg (BM3) extracts showed significant hypoglycemic activity. All extracts indicated significant antioxidant activity, however bud-methanol (BM) extract demonstrated the most potent antioxidant activity. Moreover high levels of phenolic substances and flavonoids were involved in all extracts, but the highest levels were found in FM extract. HRMS study showed that rutin, quercetin 3-O-glucoside (isoquercitrin) and stachydrine substances had seen in BM extract. The results of this study showed that the C. ovata var. palaestina extracts which, indicate hypoglycemic, antioxidant activities, might provide additional support in diabetes.
DOI: 10.6084/m9.figshare.7419521
title: Determination of phytoconstituents of n-hexane extract of leaves of Morus nigra and evaluation of their effects on biochemical and histopathological parameters in paracetamol intoxicated mice liver

description: In-vitro investigation of Morus nigra L. (Moraceae) has demonstrated the evidence of several antioxidant compounds. Current study was aimed to determine the phytoconstituents and hepatoprotective potential of n-hexane extract of Morus nigra. Swiss albino mice were divided into five groups: normal control, paracetamol control, silymarin control, 250 mg/kg p.o. extract for 7 days plus paracetamol 3 h later, 500 mg/kg p.o. extract for 7 days plus paracetamol 3 h later. Serum levels of liver enzymes and total bilirubin were assessed and compared between the groups by using one-way ANOVA to confirm hepatoprotective activity. HPLC analysis revealed the presence quercetin, oleanolic acid, luteolin, apigenin, vitamin C and kuwanon C. n-hexane extract of Morus nigra at dose of 250 mg/kg reduced elevated ALT by 54.3% (p&lt;0.001), AST by 55.1% (p&lt;0.01), ALP by 28.5% (p&lt;0.01) and TBR by 56.4% (p&lt;0.01) as compared to paracetamol control. The dose of 500 mg/kg of the extract reduced the ALT levels by 62.9% (p&lt;0.001), AST by 56.7% (p&lt;0.01), ALP by 33.6% (p&lt;0.01) and TBR by 54.5% (p&lt;0.01), as compared to paracetamol group. However, the reduction of liver enzymes and total bilirubin after administration of extract was comparable to the silymarin. Current study demonstrated potential hepatoprotective activity of n-hexane extract of Morus nigra.
DOI: 10.6084/m9.figshare.7419521.v1
title: Determination of phytoconstituents of n-hexane extract of leaves of Morus nigra and evaluation of their effects on biochemical and histopathological parameters in paracetamol intoxicated mice liver

description: In-vitro investigation of Morus nigra L. (Moraceae) has demonstrated the evidence of several antioxidant compounds. Current study was aimed to determine the phytoconstituents and hepatoprotective potential of n-hexane extract of Morus nigra. Swiss albino mice were divided into five groups: normal control, paracetamol control, silymarin control, 250 mg/kg p.o. extract for 7 days plus paracetamol 3 h later, 500 mg/kg p.o. extract for 7 days plus paracetamol 3 h later. Serum levels of liver enzymes and total bilirubin were assessed and compared between the groups by using one-way ANOVA to confirm hepatoprotective activity. HPLC analysis revealed the presence quercetin, oleanolic acid, luteolin, apigenin, vitamin C and kuwanon C. n-hexane extract of Morus nigra at dose of 250 mg/kg reduced elevated ALT by 54.3% (p&lt;0.001), AST by 55.1% (p&lt;0.01), ALP by 28.5% (p&lt;0.01) and TBR by 56.4% (p&lt;0.01) as compared to paracetamol control. The dose of 500 mg/kg of the extract reduced the ALT levels by 62.9% (p&lt;0.001), AST by 56.7% (p&lt;0.01), ALP by 33.6% (p&lt;0.01) and TBR by 54.5% (p&lt;0.01), as compared to paracetamol group. However, the reduction of liver enzymes and total bilirubin after administration of extract was comparable to the silymarin. Current study demonstrated potential hepatoprotective activity of n-hexane extract of Morus nigra.
DOI: 10.6084/m9.figshare.20039325
title: Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations

description: The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03-PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
DOI: 10.6084/m9.figshare.20039325.v1
title: Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations

description: The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03-PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
DOI: 10.6084/m9.figshare.7974983.v1
title: Impact of a drug dispensing model at a Community Pharmacy in Goiânia, Goiás, Brazil

description: Although dispensing of medication has been addressed by theoretical models, studies that confirm the impact of this service are still needed. The objective was to evaluate the impact of a new model of medicine dispensing system on patients’ medication knowledge, adherence to treatment and satisfaction. One hundred and four patients attending the dispensing service of a community pharmacy between 21 January 2013 and 20 April 2013 were included in this intervention study. The impact of the service on patients’ medication knowledge, adherence to treatment and satisfaction was assessed by using validated questionnaires at two time points: at the moment of medication dispensing and 30 days thereafter by telephone contact. Statistical analysis was performed by McNemar’s test, and a p&lt;0.05 was set as statistically significant. The number of patients showing insufficient knowledge about medications decreased by 50% (p &lt; 0.05), and the number of those showing sufficient knowledge was three times greater (p &lt; 0.05) after medicine dispensing. A high level of satisfaction was observed. Improvement of medication adherence, however, was not observed. The proposed system model for drug dispensing improved patients’ knowledge about medication and satisfaction.
DOI: 10.6084/m9.figshare.7974983
title: Impact of a drug dispensing model at a Community Pharmacy in Goiânia, Goiás, Brazil

description: Although dispensing of medication has been addressed by theoretical models, studies that confirm the impact of this service are still needed. The objective was to evaluate the impact of a new model of medicine dispensing system on patients’ medication knowledge, adherence to treatment and satisfaction. One hundred and four patients attending the dispensing service of a community pharmacy between 21 January 2013 and 20 April 2013 were included in this intervention study. The impact of the service on patients’ medication knowledge, adherence to treatment and satisfaction was assessed by using validated questionnaires at two time points: at the moment of medication dispensing and 30 days thereafter by telephone contact. Statistical analysis was performed by McNemar’s test, and a p&lt;0.05 was set as statistically significant. The number of patients showing insufficient knowledge about medications decreased by 50% (p &lt; 0.05), and the number of those showing sufficient knowledge was three times greater (p &lt; 0.05) after medicine dispensing. A high level of satisfaction was observed. Improvement of medication adherence, however, was not observed. The proposed system model for drug dispensing improved patients’ knowledge about medication and satisfaction.
DOI: 10.6084/m9.figshare.7974992
title: Synthesis of some novel pyrimidine, thiophene, coumarin, pyridine and pyrrole derivatives and their biological evaluation as analgesic, antipyretic and anti-inflammatory agents

description: Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities.
DOI: 10.6084/m9.figshare.7974992.v1
title: Synthesis of some novel pyrimidine, thiophene, coumarin, pyridine and pyrrole derivatives and their biological evaluation as analgesic, antipyretic and anti-inflammatory agents

description: Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities.
DOI: 10.6084/m9.figshare.20039326.v1
title: Effect of wet mass on dextromethorphan hydrobromide matrix pellets

description: Dextromethorphan hydrobromide (DM) sustained release matrix pellets containing 10% w/w drug were prepared by an extrusion/spheronization technique. The effect of mixing different concentrations of ethyl cellulose (EC), hydroxypropyl methylcellulpse (HPMC K10), and Carbopol 934 with Avicel PH101 on the rheological properties of pellet wet mass was evaluated using mixer torque rheometry (MTR). The prepared pellets were characterized for size, drug content, and in-vitro DM release rate. The results showed that increasing the concentration of the hydrophobic polymer (EC) with Avicel PH101 decreased wet mass consistency, represented by mass mean line torque. Lower binder ratio was required for optimum wet massing, while mixing with swellable polymers (HPMC and Carbopol) caused a noticeable increase in both mean line torque and binder ratio. Combinations of HPMC and Carbopol at higher concentrations resulted in controlled in vitro release of DM from the prepared pellets. Furthermore, mathematical treatment of the in vitro release data of DM from the prepared pellets showed that all formulations except those containing 5% Carbopol plus 5% HPMC (F10) follow first order release. n values of these formulation were in the range of 0.09-0.40, which support an anomalous non-Fickian release.