cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.11453145.v1
title: Antimicrobial activity of actinomycetes and characterization of actinomycin-producing strain KRG-1 isolated from Karoo, South Africa

description: In the present study we reported the antimicrobial activity of actinomycetes isolated from aridic soil sample collected in Karoo, South Africa. Eighty-six actinomycete strains were isolated and purified, out of them thirty-four morphologically different strains were tested for antimicrobial activity. Among 35 isolates, 10 (28.57%) showed both antibacterial and antifungal activity. The ethyl acetate extract of strain KRG-1 showed the strongest antimicrobial activity and therefore was selected for further investigation. The almost complete nucleotide sequence of the 16S rRNA gene as well as distinctive matrix-assisted laser desorption/ionization-time-of-flight/mass spectrometry (MALDI-TOF/MS) profile of whole-cell proteins acquired for strain KRG-1 led to the identification of Streptomyces antibioticus KRG-1 (GenBank accession number: KX827270). The ethyl acetate extract of KRG-1 was fractionated by HPLC method against the most suppressed bacterium Staphylococcus aureus (Newman). LC//MS analysis led to the identification of the active peak that exhibited UV-VIS maxima at 442 nm and the ESI-HRMS spectrum showing the prominent ion clusters for [M-H2O+H]+ at m/z 635.3109 and for [M+Na]+ at m/z 1269.6148. This information could be assigned to chromopeptide lactone antibiotic - actinomycin. Our results suggest that unexplored soils could be an interesting source for exploring antibacterial secondary metabolites.
DOI: 10.6084/m9.figshare.11453142
title: Evaluation of triterpenes derivatives in the viability of Leishmania amazonensis and Trichomonas vaginalis

description: Trichomonas vaginalis and Leishmania spp. are protozoal species responsible for millions of cases of parasitic diseases worldwide. Considering the potential of natural products and the need for more effective and less toxic alternatives to treat trichomoniasis and leishmaniasis, this study aimed to evaluate the effect of two series of triterpenes derivatives with different modifications at C-3 and C-28 positions of the ursolic acid (UA) and betulinic acid (BA) against trophozoites of Trichomonas vaginalis and promastigotes forms of Leishmania (L.) amazonensis. The compounds modified just at C-3 were the most active. The 3β-acetyl betulinic acid (1b) reduced the trophozoites viability of T. vaginalis at 74%, followed by the 3-oxo ursolic acid and 3-oxo betulinic acid (3a and 3b) compounds (55% of reduction). The compound 3β-isobutyl ursolic acid (7a) inhibited the viability of L. amazonensis promastigotes by 55%. Therefore, analyzing the structure-activity relationship and the data of literature, it is possible to suppose that the inclusion of polar groups in the skeletons could improve the antiprotozoal activity. Overall, further studies are necessary to develop triterpenic derivatives with more powerful trichomonicidal and leishmanicidal properties.
DOI: 10.6084/m9.figshare.11453142.v1
title: Evaluation of triterpenes derivatives in the viability of Leishmania amazonensis and Trichomonas vaginalis

description: Trichomonas vaginalis and Leishmania spp. are protozoal species responsible for millions of cases of parasitic diseases worldwide. Considering the potential of natural products and the need for more effective and less toxic alternatives to treat trichomoniasis and leishmaniasis, this study aimed to evaluate the effect of two series of triterpenes derivatives with different modifications at C-3 and C-28 positions of the ursolic acid (UA) and betulinic acid (BA) against trophozoites of Trichomonas vaginalis and promastigotes forms of Leishmania (L.) amazonensis. The compounds modified just at C-3 were the most active. The 3β-acetyl betulinic acid (1b) reduced the trophozoites viability of T. vaginalis at 74%, followed by the 3-oxo ursolic acid and 3-oxo betulinic acid (3a and 3b) compounds (55% of reduction). The compound 3β-isobutyl ursolic acid (7a) inhibited the viability of L. amazonensis promastigotes by 55%. Therefore, analyzing the structure-activity relationship and the data of literature, it is possible to suppose that the inclusion of polar groups in the skeletons could improve the antiprotozoal activity. Overall, further studies are necessary to develop triterpenic derivatives with more powerful trichomonicidal and leishmanicidal properties.
DOI: 10.6084/m9.figshare.20039433
title: Development and characterization of photoprotective formulations containing keratin particles

description: This work deals with development and evaluation of MFQ protective formulation, which contains two organic filters, namely: octyl-p-methoxycinnamate (OMC) and benzophenone-3 (BP-3); a photostabilizing agent called ethylhexylmethoxycrylene (EHMCR) and keratin particles. The MFQ formulation was evaluated in order to measure its pH, spin-spin lattice relaxation time (T2H), occlusivity factor, formulation efficacy, photostability and skin permeation, as well as keratin particle properties. Keratin particle size increased when incorporated to formulation, however, it did not affect pH. The MFQ formulation was found to be photostable and photoprotective, as evidenced by sunlight photostability test, sun protection factor (SPF), UVA/UVB ratio and critical wavelength. Interaction between keratin particles and active substances (OMC, BP-3 and EHMCR) was evidenced by T2H measurements. Evidences suggest that keratin reduces the permeation of both UV filters employed along this study, therefore, it can be stated that keratin has a promising potential for use in sunscreen formulations.
DOI: 10.6084/m9.figshare.20039433.v1
title: Development and characterization of photoprotective formulations containing keratin particles

description: This work deals with development and evaluation of MFQ protective formulation, which contains two organic filters, namely: octyl-p-methoxycinnamate (OMC) and benzophenone-3 (BP-3); a photostabilizing agent called ethylhexylmethoxycrylene (EHMCR) and keratin particles. The MFQ formulation was evaluated in order to measure its pH, spin-spin lattice relaxation time (T2H), occlusivity factor, formulation efficacy, photostability and skin permeation, as well as keratin particle properties. Keratin particle size increased when incorporated to formulation, however, it did not affect pH. The MFQ formulation was found to be photostable and photoprotective, as evidenced by sunlight photostability test, sun protection factor (SPF), UVA/UVB ratio and critical wavelength. Interaction between keratin particles and active substances (OMC, BP-3 and EHMCR) was evidenced by T2H measurements. Evidences suggest that keratin reduces the permeation of both UV filters employed along this study, therefore, it can be stated that keratin has a promising potential for use in sunscreen formulations.
DOI: 10.6084/m9.figshare.11453052
title: Effect of lesimarin against thioacetamide-induced liver cirrhosis in rat

description: Liver cirrhosis is one of chronic liver diseases with high disability and mortality accompanying fibrosis, hepatocyte damage, and liver dysfunction. In this study, the hepatoprotective and the antifibrotic properties of lesimarin(lecithin - silymarin - Artemisia messerschmitiana Besser(AMB) extract complex at 11:3:6 ratio) on rat hepatic fibrosis induced by thioacetamide (TAA) was investigated. Rats were divided into seven groups: control, lesimarin, TAA, TAA+lesimarin, TAA+lecithin, TAA+silymarin, TAA+AMB. Rats were administered with TAA at a dose of 200 mg/kg body weight intraperitoneally twice a week for three months. Lesimarin, lecithin, silymarin and AMB were administered at a dose of 1.0, 1.0, 0.5, 1.0g/kg body weight orally daily for three months, respectively. TAA administration resulted in hepatic fibrosis, significant decrease in body weight, albumin level and A/G ratio and increase in plasma transaminase, GGT(γ-glutamyltransferase) and ALP(alkaline phosphatase) activities as well as hepatic hydroxyproline content, which were attenuated by lesimarin administration. Lesimarin was found to decrease AST, ALT and GGT, ALP and bilirubin, hydroxyproline levels and increase albumin level and A/G ratio and its effect is more prominent than those of individual constituents. These results suggest this new drug, lesimarin, might be a promising drug to be used for chronic liver diseases.
DOI: 10.6084/m9.figshare.11453052.v1
title: Effect of lesimarin against thioacetamide-induced liver cirrhosis in rat

description: Liver cirrhosis is one of chronic liver diseases with high disability and mortality accompanying fibrosis, hepatocyte damage, and liver dysfunction. In this study, the hepatoprotective and the antifibrotic properties of lesimarin(lecithin - silymarin - Artemisia messerschmitiana Besser(AMB) extract complex at 11:3:6 ratio) on rat hepatic fibrosis induced by thioacetamide (TAA) was investigated. Rats were divided into seven groups: control, lesimarin, TAA, TAA+lesimarin, TAA+lecithin, TAA+silymarin, TAA+AMB. Rats were administered with TAA at a dose of 200 mg/kg body weight intraperitoneally twice a week for three months. Lesimarin, lecithin, silymarin and AMB were administered at a dose of 1.0, 1.0, 0.5, 1.0g/kg body weight orally daily for three months, respectively. TAA administration resulted in hepatic fibrosis, significant decrease in body weight, albumin level and A/G ratio and increase in plasma transaminase, GGT(γ-glutamyltransferase) and ALP(alkaline phosphatase) activities as well as hepatic hydroxyproline content, which were attenuated by lesimarin administration. Lesimarin was found to decrease AST, ALT and GGT, ALP and bilirubin, hydroxyproline levels and increase albumin level and A/G ratio and its effect is more prominent than those of individual constituents. These results suggest this new drug, lesimarin, might be a promising drug to be used for chronic liver diseases.
DOI: 10.6084/m9.figshare.11452416.v1
title: Chemical composition and bioactivity of methanolic extract obtained from Lepista sordida

description: The present study aimed at the evaluation of chemical composition and bioactive potential of methanolic extract obtained from Lepista sordida in terms of antioxidative and antimicrobial efficacy. The macrofungus is recognized for its high nutritional value and medicinal properties. However, to the best of our knowledge bioactivity of its methanolic extract is yet to be explored. In this investigation, quantitative analysis of mycochemicals revealed the extract contained significant amount of phenolic compounds such as phenols and flavonoids. Ascorbic acid was found in higher amount than β carotene and lycopene which were present in vestigial amounts. A phenolic profile was also determined using high performance liquid chromatography that further confirmed the presence of 10 phenolic constituents in the extract. Furthermore, the extract was subjected for determining antioxidant potential in different in-vitro assays. The findings showed remarkable 2, 2-Diphenyl-1-picrylhydrazyl and ABTS radical scavenging ability which was evident by low EC50 values, 330 µg/mL and 30 µg/mL respectively. The extract also demonstrated good chelating and reducing ability, an important marker of antioxidant compounds. Antimicrobial screening displayed positive results against Staphylococcus aureus and Escherichia coli. Altogether, the observations recommend therapeutic application of this mycotaxon on a commercial basis.
DOI: 10.6084/m9.figshare.11452416
title: Chemical composition and bioactivity of methanolic extract obtained from Lepista sordida

description: The present study aimed at the evaluation of chemical composition and bioactive potential of methanolic extract obtained from Lepista sordida in terms of antioxidative and antimicrobial efficacy. The macrofungus is recognized for its high nutritional value and medicinal properties. However, to the best of our knowledge bioactivity of its methanolic extract is yet to be explored. In this investigation, quantitative analysis of mycochemicals revealed the extract contained significant amount of phenolic compounds such as phenols and flavonoids. Ascorbic acid was found in higher amount than β carotene and lycopene which were present in vestigial amounts. A phenolic profile was also determined using high performance liquid chromatography that further confirmed the presence of 10 phenolic constituents in the extract. Furthermore, the extract was subjected for determining antioxidant potential in different in-vitro assays. The findings showed remarkable 2, 2-Diphenyl-1-picrylhydrazyl and ABTS radical scavenging ability which was evident by low EC50 values, 330 µg/mL and 30 µg/mL respectively. The extract also demonstrated good chelating and reducing ability, an important marker of antioxidant compounds. Antimicrobial screening displayed positive results against Staphylococcus aureus and Escherichia coli. Altogether, the observations recommend therapeutic application of this mycotaxon on a commercial basis.
DOI: 10.6084/m9.figshare.11452419
title: Preformulation of a liquid dosage formulation of captopril for pediatric use: drug-excipient compatibility and stability studies

description: Currently, medications used in children are typically modified from pharmaceutical dosage forms designed for adults. Captopril is widely adapted to liquid formulations for use in hospitals. Its stability in the aqueous medium is reduced since it undergoes oxidation producing captopril disulfide (its main metabolite). The aim of this formulation study was to suggest favorable conditions for the development of a stable captopril formulation. The compatibility between the drug and excipients was evaluated by differential scanning calorimetry analysis (DSC). For studies in solution, different formulations were prepared according to a factorial design varying EDTA concentration, water purity and pH. The resultant formulations were stored at 60°C and analyzed over a twelve-day period using HPLC. The DSC curves obtained suggested, although not conclusive to elucidation, interactions of captopril with citric acid and sucralose. The stability study of these solutions revealed that the variables significantly influenced captopril content, which degraded at zero order kinetics and rates differing by a factor of up to 7 times, where pH proved the most influential factor. Interactions between variables were observed. Therefore, development of a stable captopril formulation is feasible provided EDTA and a buffering agent is used at suitable concentrations (0.08% and pH 3.85).
DOI: 10.6084/m9.figshare.11452419.v1
title: Preformulation of a liquid dosage formulation of captopril for pediatric use: drug-excipient compatibility and stability studies

description: Currently, medications used in children are typically modified from pharmaceutical dosage forms designed for adults. Captopril is widely adapted to liquid formulations for use in hospitals. Its stability in the aqueous medium is reduced since it undergoes oxidation producing captopril disulfide (its main metabolite). The aim of this formulation study was to suggest favorable conditions for the development of a stable captopril formulation. The compatibility between the drug and excipients was evaluated by differential scanning calorimetry analysis (DSC). For studies in solution, different formulations were prepared according to a factorial design varying EDTA concentration, water purity and pH. The resultant formulations were stored at 60°C and analyzed over a twelve-day period using HPLC. The DSC curves obtained suggested, although not conclusive to elucidation, interactions of captopril with citric acid and sucralose. The stability study of these solutions revealed that the variables significantly influenced captopril content, which degraded at zero order kinetics and rates differing by a factor of up to 7 times, where pH proved the most influential factor. Interactions between variables were observed. Therefore, development of a stable captopril formulation is feasible provided EDTA and a buffering agent is used at suitable concentrations (0.08% and pH 3.85).
DOI: 10.6084/m9.figshare.11452413
title: Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

description: This study evaluates various techniques for producing mesalamine (5ASA)-loaded particles employing chitosan as a biopolymer: (1) the polyelectrolyte complexation of chitosan with phthalate hypromelose (HP), (2) the chemical crosslinking of chitosan with genipin and (3) the water-in-oil emulsion method associated with chemical crosslinking with genipin. Systems were characterized by dynamic light scattering, zeta potential (ζ), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and a drug release profile. Method (1) was efficiently produced unloaded nanoparticles (491 nm, PdI=0.26 and ζ = 23.2), but the conditions for chitosan and HP cross-linking enhanced the precipitation of 5ASA. Method (2) caused the degradation of the drug. Method 3 produced sub-micron and microparticles, thereby varying the agitation method; 3 h magnetic agitation resulted in 2692 nm, Pdi = 0.6 and ζ = 46, while Ultra-Turrax, 5 min produced submicron particles (537 nm, PdI = 0.6). The percentage yield was approximately 50%, which is very satisfactory considering the impossibility of encapsulating 5ASA using other methods. FTIR showed the covalent interaction of chitosan and genipin. The drug release was rapid in acidic fluid, but in neutral pH a slower release was obtained in the initial stage, followed by rapid release, which may ensure the controlled release of 5ASA in the colon.
DOI: 10.6084/m9.figshare.11452413.v1
title: Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

description: This study evaluates various techniques for producing mesalamine (5ASA)-loaded particles employing chitosan as a biopolymer: (1) the polyelectrolyte complexation of chitosan with phthalate hypromelose (HP), (2) the chemical crosslinking of chitosan with genipin and (3) the water-in-oil emulsion method associated with chemical crosslinking with genipin. Systems were characterized by dynamic light scattering, zeta potential (ζ), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and a drug release profile. Method (1) was efficiently produced unloaded nanoparticles (491 nm, PdI=0.26 and ζ = 23.2), but the conditions for chitosan and HP cross-linking enhanced the precipitation of 5ASA. Method (2) caused the degradation of the drug. Method 3 produced sub-micron and microparticles, thereby varying the agitation method; 3 h magnetic agitation resulted in 2692 nm, Pdi = 0.6 and ζ = 46, while Ultra-Turrax, 5 min produced submicron particles (537 nm, PdI = 0.6). The percentage yield was approximately 50%, which is very satisfactory considering the impossibility of encapsulating 5ASA using other methods. FTIR showed the covalent interaction of chitosan and genipin. The drug release was rapid in acidic fluid, but in neutral pH a slower release was obtained in the initial stage, followed by rapid release, which may ensure the controlled release of 5ASA in the colon.
DOI: 10.6084/m9.figshare.11452404.v1
title: Protective effect of citrus lemon on inflammation and adipokine levels in acrylamide-induced oxidative stress in rats

description: The high exposure to acrylamide (AA) due to smoking and increased consumption of processed and fast foods in recent years, has become one of the health threatening problems. This study examined the effect of lemon juice on inflammation and adipokines in acrylamide-induced oxidative stress in rats. Forty animals were divided into five groups. Toxicity was induced by AA (35mg/kg) for two weeks in all groups except normal control group. After that, lemon juice in three doses was administrated to treatment groups for 4 weeks. Serum levels of adipokines and inflammatory parameters and both serum and liver levels of oxidative stress parameters were measured. The results showed groups were received AA had significant higher levels of malondialdehyde, tumor necrosis factor alpha, leptin and C-reactive protein and lower levels of total antioxidant capacity compared to the negative control group. Lemon juice in all three doses significantly improved serum levels of TAC, MDA, TNFα and hs-CRP in treated groups. Also, 7.5 ml/kg lemon juice significantly decreased leptin levels. However, lemon juice had no significant effect on adiponectin levels. This study suggests lemon juice as a potential dietary alternative could attenuate leptin levels and manage oxidative and inflammatory damages in acrylamide- induced toxicity in rats.
DOI: 10.6084/m9.figshare.11452404
title: Protective effect of citrus lemon on inflammation and adipokine levels in acrylamide-induced oxidative stress in rats

description: The high exposure to acrylamide (AA) due to smoking and increased consumption of processed and fast foods in recent years, has become one of the health threatening problems. This study examined the effect of lemon juice on inflammation and adipokines in acrylamide-induced oxidative stress in rats. Forty animals were divided into five groups. Toxicity was induced by AA (35mg/kg) for two weeks in all groups except normal control group. After that, lemon juice in three doses was administrated to treatment groups for 4 weeks. Serum levels of adipokines and inflammatory parameters and both serum and liver levels of oxidative stress parameters were measured. The results showed groups were received AA had significant higher levels of malondialdehyde, tumor necrosis factor alpha, leptin and C-reactive protein and lower levels of total antioxidant capacity compared to the negative control group. Lemon juice in all three doses significantly improved serum levels of TAC, MDA, TNFα and hs-CRP in treated groups. Also, 7.5 ml/kg lemon juice significantly decreased leptin levels. However, lemon juice had no significant effect on adiponectin levels. This study suggests lemon juice as a potential dietary alternative could attenuate leptin levels and manage oxidative and inflammatory damages in acrylamide- induced toxicity in rats.
DOI: 10.6084/m9.figshare.11452122
title: The anti-obesity potential of Ilex paraguariensis: results from a meta-analysis

description: The dried leaves of Ilex paraguariensis, also known as yerba mate or chimarrão, are used to produce infusions consumed by over 1 million people worldwide, being a traditional drink in several South American countries, particularly, Argentina, Brazil, Uruguay, and Paraguay. The positive effects of I. paraguariensis in obesity have been described and observed in some clinical trials both in animals and in humans. The main goal of this work was to perform a systematic review, complying with the PRISMA (Preferred Reported Items for Systematic Reviews and Meta-Analysis) recommendations, followed by a meta-analysis and Trial Sequential Analysis (TSA), to summarize the results of the recent clinical trials, clarifying the anti-obesity potential of I. paraguariensis. The search for this systematic review was performed on several electronic databases (Pubmed, Web of Science, Scopus, SciELO and Cochrane Library) in July 2017. A total of 22 clinical trials were considered for the quantitative synthesis of the data, totalizing 726 patients enrolled. In conclusion, this systematic review demonstrated the positive effects of I. paraguariensis consumption on the reduction of body weight, body mass index (BMI), and waist circumference of patients, showing its anti-obesity potential.