Solid-State Form Characterization of Riparin I de Moura, Elisana Afonso; Terto, Márcio Vinícius Cahino; de Moura Mendonça, Elisângela Afonso ...
Molecules (Basel, Switzerland),
10/2017, Letnik:
22, Številka:
10
Journal Article
Recenzirano
Odprti dostop
Riparin I is an alkamide with potential anxiolytic activity in preclinical studies. The characterization and understanding of solid-state properties play an importance role in drug development. For ...this work, the solid state of five riparin I batches (RIP-1, RIP-2, RIP-3, RIP-4, and RIP-5), obtained by the same synthesis process, were characterized by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), DSC-photovisual, Thermogravimetry (TG), Fourier Transform Infrared (FTIR), Pyrolysis (Pyr-GC/MS), X-ray Powder Diffraction (PXRD), and Solid-State Nuclear Magnetic Resonance (ssNMR) techniques. Batches of riparin I with different crystal habits resulting in crystallization impurities were observed, which can be attributed to the presence of triethylamine. The main differences were observed by DSC, PXRD, and ssNMR analysis. DSC curves of RIP-2 and RIP-3 presented endothermic peaks at different temperatures of fusion, which can be attributed to the mixture of different crystalline forms. PXRD and ssNMR results confirmed crystallinity differences. The results offer evidence of the importance of controlling the reproducibility of the synthesis in order to obtain the adequate morphology for therapeutic efficacy and avoiding future problems in quality control of riparin I products.
Vogel (Leguminosae) is a species popularly known in Brazil as "urinária", "urinana", and "carrapicho", it is popularly used as a diuretic and in the treatment of venereal diseases. A specific ...methodology to obtain a saponin-enriched fraction and high-performance liquid chromatography coupled with diode array detection, ion trap mass spectrometry, and TOF-MS (HPLC-DAD-ESI-MS/MS) was applied for the analysis of triterpene saponins. The MS and MS/MS experiments were carried out by ionization in negative mode. Molecular mass and fragmentation data were used to support the structural characterization of the saponins. Based on retention times, high-resolution mass determination and fragmentation, 35 oleanane-triterpene saponins were tentatively identified in
.
Pharmacological studies show spasmolytic activity for various species of
. Thus, based on the taxonomy criteria, the aim of this study was to contribute to chemical and biological knowledge, ...especially regarding the evaluation of spasmolytic activity of the ethanolic extract from
leaves (VD-EtOH
) on rat aorta and trachea, guinea-pig ileum and rat uterus. Were used High and Medium Performance Liquid Chromatography. Wistar rats and guinea-pigs were used for pharmacological assays. All experimental protocols were approved by Animal Ethics Committee of UFPB (126/2017). Two chalcones (pinostrobin chalcone and gymnogrammene), five flavanones (pinocembrin, isosakuranetin, pinostrobin, sakuranetin 4'-methyl ether, naringenin) and a flavonoid glycosilated (astragalin) were identified based on data of
H and
C Nuclear Magnetic Resonance. This study also showed that VD-EtOH
has a non-selective spasmolytic activity, presenting greater relaxing potency in rat uterus, suggesting that flavonoids isolated from VD-EtOH
may be responsible for spasmolytic activity of this extract.
In the Amazon region of Brazil, the fruits of
Caesalpinia ferrea Martius (Brazilian ironwood) are widely used as an antimicrobial and healing medicine in many situations including oral infections. ...This study aimed to evaluate the antimicrobial activity of
Caesalpinia ferrea Martius fruit extract against oral pathogens.
Polyphenols estimation and spectral analysis (
1H NMR) of the methanol extract were carried out. The microorganisms
Candida albicans,
Streptococcus mutans,
Streptococcus salivarius,
Streptococcus oralis and
Lactobacillus casei were tested using the microdilution method for planktonic cells (MIC) and a multispecies biofilm model. Chlorhexidine was used as positive control.
Polyphenols in the extract were estimated at 7.3% and
1H NMR analysis revealed hydroxy phenols and methoxilated compounds. MIC values for
Candida albicans,
Streptococcus mutans,
Streptococcus salivarius,
Streptococcus oralis and
Lactobacillus casei were 25.0, 40.0, 66.0, 100.0, 66.0
μg/mL, respectively. For the biofilm assay, chlorhexidine and plant extract showed no growth at 10
−4 and 10
−5 microbial dilution, respectively. At 10
−4 and 10
−5 the growth values (mean
±
SD) of the negative controls (DMSO and saline solution) for
Streptococcus mutans,
Streptococcus sp. and
Candida albicans were 8.1
±
0.7, 7.0
±
0.6 and 5.9
±
0.9
×
10
6
CFU, respectively.
Caesalpinia ferrea fruit extract can inhibit
in vitro growth of oral pathogens in planktonic and biofilm models supporting its use for oral infections.
The project proposes three innovative intervention techniques (treadmill training, mobility training with virtual reality and transcranial direct current stimulation that can be safely administered ...to children with cerebral palsy. The combination of transcranial stimulation and physical therapy resources will provide the training of a specific task with multiple rhythmic repetitions of the phases of the gait cycle, providing rich sensory stimuli with a modified excitability threshold of the primary motor cortex to enhance local synaptic efficacy and potentiate motor learning.
A prospective, double-blind, randomized, controlled, analytical, clinical trial will be carried out.Eligible participants will be children with cerebral palsy classified on levels I, II and III of the Gross Motor Function Classification System between four and ten years of age. The participants will be randomly allocated to four groups: 1) gait training on a treadmill with placebo transcranial stimulation; 2) gait training on a treadmill with active transcranial stimulation; 3) mobility training with virtual reality and placebo transcranial stimulation; 4) mobility training with virtual reality and active transcranial stimulation. Transcranial direct current stimulation will be applied with the anodal electrode positioned in the region of the dominant hemisphere over C3, corresponding to the primary motor cortex, and the cathode positioned in the supraorbital region contralateral to the anode. A 1 mA current will be applied for 20 minutes. Treadmill training and mobility training with virtual reality will be performed in 30-minute sessions five times a week for two weeks (total of 10 sessions). Evaluations will be performed on four occasions: one week prior to the intervention; one week following the intervention; one month after the end of the intervention;and 3 months after the end of the intervention. The evaluations will involve three-dimensional gait analysis, analysis of cortex excitability (motor threshold and motor evoked potential), Six-Minute Walk Test, Timed Up-and-Go Test, Pediatric Evaluation Disability Inventory, Gross Motor Function Measure, Berg Balance Scale, stabilometry, maximum respiratory pressure and an effort test.
This paper offers a detailed description of a prospective, double-blind, randomized, controlled, analytical, clinical trial aimed at demonstrating the effect combining transcranial stimulation with treadmill and mobility training on functionality and primary cortex excitability in children with Cerebral Palsy classified on Gross Motor Function Classification System levels I, II and III. The results will be published and will contribute to evidence regarding the use of treadmill training on this population.
ReBEC RBR-9B5DH7.
The adequate control of asthma includes the absence of nocturnal symptoms, minimal use of medication, normal or nearly normal lung function and no limitations to physical activity. The choice of a ...more sedentary lifestyle can lead to physical de-conditioning, thereby aggravating asthma symptoms and increasing the risk of obesity.
This study aimed at performing a battery of function-related assessments in patients with asthma and comparing them to a healthy control group. A prospective, transversal and case-control study was designed. It was set up at Santa Casa de Misericórdia Hospital -Sao Paulo and Nove de Julho University on a population of outpatients. Subjects of the study were patients affected by moderate to severe asthma. A case-control study was carried out involving 20 patients with moderate to severe asthma and 15 healthy individuals (control group). All participants underwent body composition analysis (BMI and BIA) and a controlled walk test (Shuttle test), resistance muscle test (1RM) and answered a physical activity questionnaire (IPAQ). The group with asthma also answered a questionnaire addressing the clinical control of the illness (ACQ).
In comparison to the control group (unpaired Student's t-test), the patients with asthma had a significantly higher BMI (31.09 ± 5.98 vs. 26.68 ± 7.56 kg/m(2)) and percentage of body fat (38.40 ± 6.75 vs. 33.28 ± 8.23%) as well as significantly lower values regarding distance traveled on the walk test (369 ± 110 vs. 494 ± 85 meters) and metabolic equivalents (3.74 ± 0.87 vs. 4.72 ± 0.60). A strong correlation was found between the distance completed and peripheral muscle strength (r: 0.57, p < 0.05) and METs (Metabolic equivalents - minutes/week) and peripheral muscle strength of 1RM (r: 0.61, p = 0.009).
The individuals with asthma had lower functional capacity and levels of physical activity as well as a higher percentage of body fat compared to healthy individuals. This suggests that such patients have a reduced physical performance stemming from a sedentary lifestyle. Despite the existence of few studies reporting moderate to severe asthmatic patients and functional capacity assessment, it is clear that the assessment presented in the current study is a valid and accessible tool in clinical practice.
ENT-ABIETANE DITERPENES FROM Euphorbia phosphorea (EUPHORBIACEAE). Phytochemical study of the roots of Euphorbia phosphorea Mart. (Euphorbiaceae) was carried out through chromatographic techniques, ...resulting in the isolation of a new ent-abietane diterpene named 11β,12β-dihydroxy-ent-abieta-8(14),13(15)-dien-16,12α-olide (1), and of nine known ent-abietane diterpenes jolkinolide A (2), jolkinolide E (3), euphorin H (4), euphopilolide (5) jolkinolide F (6), ent-12-hydroxy-12R-abieta8(14),13(15)-dien-16,12-olide (7), ent-11α-hydroxyabieta-8(14),13(15)-dien-16,12α-olide (8), 17-hydroxyjolkinolide B (9) and caudicifolin (10). The structures of all compounds were established using spectroscopic techniques such as 1D and 2D NMR, and the structure of the compound 1 was established also with MS, IR and ECD. All compounds were submitted to an in silico study through of a predictive model and then submitted to in vitro tests against Mycobacterium tuberculosis and M. smegmatis for evaluation of their antimycobacterial activity. Compounds 5 and 9 showed mycobacterial growth inhibition with MIC values of 62.5 μM against M. tuberculosis and M. smegmatis, respectively.
One new diterpene (4R,7R,14S)-4α,7α-diacetoxy-10-one-14α-hydroxydolasta-1(15),8-diene (1), and five known compounds (4R,7R,14S)-4α,7α-diacetoxy-14α-hydroxydolasta-1(15),8-diene (2), ...(4R,14S)-4α,14α-dihydroxydolasta-1(15),8-diene (3), (4S,9R,14S)-4α-acetoxy-9β,14α-dihydroxydolasta-1(15),7-diene (4), 4-acetoxy-14-hydroxydolasta-1(15),7,9-triene (5) and isolinearol (6), were isolated from Canistrocarpus cervicornis. In this study, dolastane diterpenes were isolated from the alga C. cervicornis and evaluated as modifiers of antibiotic activity in Staphylococcus aureus: SA-1199B, which overexpresses the norA gene RN-4220, which encodes for the protein efflux of macrolides (MRSA), and IS-58 which has the gene encoding the protein TetK. The minimum inhibitory concentrations (MICs) for norfloxacin, tetracycline and erythromycin were determined by the microdilution broth nutrient in the absence and presence of diterpenes at a sub-inhibitory concentration (MIC/4). The extracts of C. cervicornis and isolated diterpenes showed no antibacterial activity, but showed modulatory activity, decreasing the MIC of antibiotics by 4-256 fold. The results indicate that seaweed extracts and diterpenes are potential sources of antibiotic adjuvant, acting as potential inhibitors of efflux pump.
The study aimed to investigate the chemical composition of Paliavana tenuiflora Mansf., an endemic Brazilian species that belongs to Gesneriaceae family. By chromatographic, spectroscopic and ...cheminformatics techniques it was possible to isolate and elucidate eleven compounds: a new naphthoquinone named as tenuiflorone (1), besides known compounds 7-metoxy-8-hydroxy-α-dunnione (2), tectoquinone (3), 2-(p-hydroxyphenyl) ethyl hexacosanoate (4), 2-(3′,4′-dihydroxyphenyl) ethyl hexacosanoate (5), caffeic acid (6), presilphiperfolan-9-ol (7), β-sitosterol (8), stigmasterol (9), β-sitosterol-3-O-d-glucopyranoside (10) and stigmasterol-3-O-d-glucopyranoside (11). This is the first time that secondary metabolites were isolated from species belonging to Paliavana genus, with the isolation of a new naphthoquinone named as tenuiflorone. The results obtained contribute to the chemotaxonomy of the Gesneriaceae family.
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Xylopia langsdorfiana A. St.-Hil. &Tul. (Annonaceae) is popularly known in the northeast of Brazil as 'pimenteira da terra', and an essential oil (XL-OE) was extracted from its leaves. Since Xylopia ...species are cited in folk medicine and diterpenes from X. langsdorfiana have spasmolytic activity, this study aimed to investigate a possible spasmolytic action of XL-OE on smooth muscle models. XL-OE (243 and 729 μg/mL) showed low pharmacologic efficacy on guinea pig trachea and rat aorta and uterus. However, in guinea pig ileum, XL-OE (27-729 μg/mL) inhibited carbachol or histamine-induced phasic contractions (1 μM) in a significant and concentration-dependent manner. In addition, XL-OE (81 μg/mL) reduced fluorescence intensity in ileal myocytes stimulated by histamine, indicating a decrease in cytosolic calcium concentration, which could explain the spasmolytic activity. Thus, XL-OE proved to be a promising natural product to be used in gastrointestinal diseases acting by modulating the cytosolic calcium concentration.
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