ABSTRACT
The present study aims to assess the cytotoxic effect of the aqueous and protease inhibitors extracts of Sterculia striata on breast cancer cell lines. The in vitro results showed significant reductions in the highest concentrations from the S. striata seed extract for all cell lines. The aqueous extract reduced the viability by up to 35% in the MCF-7, 25% in the 4T1, and 35% in the MDA-MB-231 cell lines. Regarding the protease inhibitor extract, a 50% reduction in cell viability was observed in the MDA-MB-231 at concentration of 333 µg/mL. The aqueous and the protease inhibitor extracts showed mild reduction in the viability of macrophage cell lines. Chemical characterisation analysis revealed several polyphenols such as flavonoids, tannins, phenolic acids, and other secondary metabolites including terpenes, steroids, fatty acids, and organic acids, which may be related to the promising bioactivity observed. The S. striata showed antitumor activity, emphasising its pharmacological potential.
ABSTRACT
The objective of this research was to modify chicha gum with phthalic anhydride to obtain a new biologically active material. The chemical modification of the gum structure was proven through FTIR, elemental analysis, XRD, TG, and DSC. The derived materials demonstrated excellent inhibitory effect against P. aeruginosa and K. pneumoniae species (rating 100% inhibition) and could also inhibit Escherichia coli growth. The best antimicrobial activity observed for the derivatives suggests that chicha gum hydrophobization due to the addition of phthalic groups improved the interaction of these derivatives with bacterial cell wall components. On the other hand, the derivatives increased CC50 in macrophages but did not present acute toxicity or hemolytic activity, indicating that they are promising for use in prophylaxis or treatment of infections caused by Gram-negative bacteria.
Subject(s)
Anti-Bacterial Agents/pharmacology , Gram-Negative Bacteria/drug effects , Macrophages/drug effects , Phthalic Anhydrides/chemistry , Plant Gums/chemistry , Sterculia/chemistry , Animals , Cell Survival , Esterification , Female , Male , Mice , Mice, Inbred BALB C , Microbial Sensitivity TestsABSTRACT
Sterculia gums, as karaya and chicha gum, are complex branched and polydisperse heteropolysaccharides which can have their applications extended by improving their characteristics through chemical modifications. The objective of this work was to increase the antimicrobial activity of karaya and chicha gum through chemical modification with maleic anhydride. The incorporation of anhydride in the gum structure was confirmed by the characterization techniques. The derived biopolymers were synthesized and characterized by FTIR, X-ray diffraction, Thermogravimetric analysis and elemental analysis. Antimicrobial activity was evaluated against the Staphylococcus aureus strain (ATCC 25923). Mammalian cytotoxicity assays were also performed by MTT and hemolysis tests. The derivatives showed excellent antibacterial action inhibiting almost 100% of bacterial growth and did not present significant cytotoxicity in mammalian cells. The results showed that the derivatives are promising for biomedical applications aiming the control of infectious diseases caused by S. aureus.
Subject(s)
Anti-Bacterial Agents/pharmacology , Maleic Anhydrides/chemistry , Plant Gums/pharmacology , Sterculia/chemistry , Animals , Anti-Bacterial Agents/chemistry , Female , Karaya Gum/chemistry , Karaya Gum/pharmacology , Male , Mice , Microbial Sensitivity Tests , Microbial Viability/drug effects , Plant Gums/chemistry , Spectroscopy, Fourier Transform Infrared , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , Thermogravimetry , Toxicity Tests , X-Ray DiffractionABSTRACT
This work was aimed at the production and characterization of a new nanocarrier based on a Sterculia striata polysaccharide (SSP) modified via acylation reaction with propionic anhydride. Nanocapsules of propionated SSP (PSSP) were produced via spontaneous nanoemulsification process and tested as a potential amphotericin B (AMB) nanocarrier. Stable nanoparticles with a very low polydispersity index (0.08-0.29) and high zeta potential (ζ -42.7 to -53.8 mV) were obtained. Particle size was dependent on the degree of substitution and ranged from 205 to 286 nm. A nanocapsule with a degree of substitution (DS) of 2.53 (NCP 2.53) was selected for encapsulation, biocompatibility, and antifungal evaluation against Candida albicans strains. A maximum of 98.3% AMB encapsulation was achieved. Encapsulated AMB was in its monomeric form and showed good biocompatibility and antifungal activity against four C. albicans strains. Data indicate that PSSP has potential as a nanocarrier system for AMB.
Subject(s)
Amphotericin B/pharmacology , Drug Carriers/chemistry , Nanoparticles/chemistry , Polysaccharides/chemistry , Propionates/chemistry , Sterculia/chemistry , Antifungal Agents/pharmacology , Biocompatible Materials/chemistry , Candida albicans/drug effects , Drug Liberation , Hemolysis/drug effects , Humans , Microbial Sensitivity Tests , Nanocapsules/chemistry , Particle Size , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform InfraredABSTRACT
Stable oil nanocapsules based on acetylated Sterculia striata polysaccharide (ASSP) were produced without the use of a surfactant, and derivatives of ASSP with four different degrees of substitution (DS) were synthesised. The data revealed that only derivatives with high DS were able to produce nanocapsules (NC), which exhibited monomodal size distribution profiles with a Z-average particle size, ζ-potential, and polydispersity index (PDI) that were dependent on ASSP DS and concentration. Nanocapsules were loaded with amphotericin B (AMB) with encapsulation efficiencies (EE%) that were dependent on drug and ASSP concentrations and DS. A maximum EE% value of 99.2% was achieved, and the loaded AMB was found to be in a monomeric form, even with a concentration one hundredfold higher than that usually observed for commercial AMB aqueous solutions. Loaded nanocapsules show an in vitro controlled release of AMB. As the monomeric AMB state decreased drug toxicity, ASSP nanocapsules loaded with AMB (NC1.68) have potential for use as a drug delivery system. AMB loaded NC 1.68 keeps its activity against 5 strains of Candida albicans tested.
Subject(s)
Amphotericin B/administration & dosage , Antifungal Agents/administration & dosage , Nanocapsules/chemistry , Polysaccharides/chemistry , Sterculia/chemistry , Acetylation , Biocompatible Materials , Drug Carriers/chemistry , Drug Delivery Systems , Drug Liberation , Humans , Materials Testing , Microbial Sensitivity Tests , Microscopy, Atomic Force , Spectrum AnalysisABSTRACT
Nanoparticles are produced by means of polyelectrolyte complexation (PEC) of oppositely charged polycationic chitosan (CH) with polyanionic polysaccharide extracted from Sterculia striata exudates (rhamnogalacturonoglycan (RG)-type polysaccharide). The nanoparticles formed with low-molar-mass CH are larger than those formed with high-molar-mass CH. This behavior is in contrast with that previously observed for other systems and may be attributed to different mechanisms related to the association of CH with RG of higher persistence length chain than that of CH. Nanoparticles harnessed with a charge ratio (n(+)/n(-)) of <1 are smaller than particles with an excess of polycations. Particles with hydrodynamic sizes smaller than 100nm are achieved using a polyelectrolyte concentration of 10(-4)gmL(-1) and charge ratio (n(+)/n(-)) of <1. The CH/RG nanoparticles are associated with chloroquine (CQ) with an efficiency of 28% and release it for up to â¼60% within â¼10h, whereas in the latter, only â¼40% of the CQ was released after 24h. The main factor that influenced drug release rate is the nanoparticle charge ratio.
Subject(s)
Chitosan/chemistry , Chloroquine/chemistry , Delayed-Action Preparations , Karaya Gum/chemistry , Nanoparticles/chemistry , Sterculia/chemistry , Drug Compounding , Drug Liberation , Hydrogen-Ion Concentration , Karaya Gum/isolation & purification , Molecular Weight , Nanoparticles/ultrastructure , Particle Size , Static ElectricityABSTRACT
The present work reports the anti-inflammatory and antinociceptive activities of the ethanol extract obtained from the stem bark of Sterculia striata A. St.-Hil. & Naudin (Ss-EtOH) in the experimental models of edema induced by carrageenan, dextran, or histamin and nociception induced by chemical stimuli, such as acetic acid, formalin, capsaicin, or glutamate. The Ss-EtOH (50 mg/kg) promoted a marked inhibition on the hind paw edema induced by carrageenan or dextran (30% and 73%, respectively). Besides, Ss-EtOH (25 mg/kg) exhibited a slight activity (30%) on the hind paw edema induced by histamin. The Ss-EtOH (12.5 and 25 mg/kg) showed the antinociceptive activity on chemical stimuli induced by acetic acid (65.59% and 38.37%, respectively), formalin, in the initial (35.08% and 31.5%, respectively) and late phases (44.09% and 83.57%, respectively), capsaicin (43.77% and 51.31%, respectively), or glutamate (36.6% and 52.12%, respectively). Regarding the possible mechanism involved in the antinociceptive effect, Ss-EtOH (12.5 mg/kg) showed a decrease in the antinociceptive effect (65.8%) in the acetic acid model after pretreatment with naloxone. Thus, opioid mechanisms might be underlying this response.
Subject(s)
Analgesics/therapeutic use , Anti-Inflammatory Agents/therapeutic use , Inflammation/drug therapy , Pain/drug therapy , Phytotherapy , Plant Extracts/therapeutic use , Sterculia , Acetic Acid , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Capsaicin , Carrageenan , Dextrans , Edema/chemically induced , Edema/drug therapy , Formaldehyde , Glutamic Acid , Histamine , Inflammation/chemically induced , Male , Mice , Naloxone/pharmacology , Plant Bark , Plant Extracts/pharmacology , Plant Stems , Rats, WistarABSTRACT
OBJETIVO: Analisar os componentes químicos e antinutrientes antes e após torrefação da amêndoa de chichá da espécie Sterculia striata A. St. Hill & Naudin, oriunda de Corrente, Piauí. MÉTODOS: Foram realizadas análises: centesimal, perfil de ácidos graxos, antinutrientes (taninos, inibidor de tripsina, inibidor de amilase, lectina, fitatos), compostos fenólicos e atividade de peroxidase e polifenoloxidase. RESULTADOS: Os resultados da análise centesimal da amêndoa crua e torrada foram: lipídeos de 25,1 por cento e 26,2 por cento, carboidratos de 44,4 por cento e 45,6 por cento, proteína de 20,8 por cento e 22,1 por cento, cinzas de 3,7 por cento e 4,0 por cento, fibra alimentar total de 12,3 por cento e 10,4 por cento, respectivamente. Nas amêndoas cruas e torradas não foram encontradas lectinas, taninos, inibidores de tripsina e alfa-amilase. Verificou-se a ausência de peroxidase e polifenoloxidase e conteúdo de compostos fenólicos de 107,7mg/100g e 108,9mg/100g para amêndoas cruas e torradas, respectivamente. CONCLUSÃO: A torrefação realizada a 205ºC por 11 minutos diminuiu o teor de fitatos de 10,6mg/g para 5,5mg/g. Por fim, as amêndoas de chichá, cruas e torradas, apresentam alto teor de proteínas, fibras, ácidos graxos monoinsaturados e saturados.
OBJECTIVE: This study analyzed the chemical components and antinutrients present in raw and roasted chichá almonds from the species Sterculia striata A. St. Hill & Naudin harvested in Corrente, Piauí. METHODS: The following were determined: percent composition, fatty acid profile, antinutrients (tannins, trypsin inhibitor, amylase inhibitor, lectin, phytates), phenolic compounds and peroxidase and polyphenol oxidase activities. RESULTS: The percentage composition of the raw and lipid almonds were respectively: 25.1 percent and 26.2 percent fats, 44.4 percent and 45.6 percent carbohydrates, 20.8 percent and 22.1 percent protein, 3.7 percent and 4.0 percent ashes, and 12.3 percent and 10.4 percent total fiber. Neither raw nor roasted almonds contained lectins, tannins, trypsin inhibitors, alpha-amylase, peroxidase and polyphenol oxidase. Contents of phenolic compounds were 107.7mg/100g and 108.9mg/100 for the raw and roasted almonds, respectively. CONCLUSION: Roasting at 205ºC for 11 minutes reduced phytate content from 10.6mg/g to 5.5mg/g. Raw and roasted chichá almonds have a high content of proteins, fibers and monounsaturated and saturated fatty acids.
Subject(s)
Food Composition , Prunus/chemistryABSTRACT
A investigação fitoquímica das cascas do caule de Sterculia striata St. Hil. et Naudin, através de métodos cromatográficos, conduziu ao isolamento dos esteróides sitosterol, estigmasterol e sitosterol-3-O-ß-D-glicopiranosídeo, além de quatro triterpenóides pentacíclicos, o lupeol, 3-ß-O-acil lupeol, lupenona e ácido betulínico. As estruturas desses compostos foram identificadas por análise dos espectros de RMN ¹H e 13C e comparações com dados da literatura. Para determinação do teor de fenóis totais do extrato etanólico de S. striata utilizou-se o reativo Folin Ciocalteu, enquanto na avaliação da atividade antioxidante empregou-se o radical livre DPPH. Este é o primeiro trabalho descrevendo o estudo químico com as cascas do caule desta espécie.
The phytochemical investigation of the stem bark of Sterculia striata St. Hil. et Naudin by chromatographic methods led to the isolation of sitosterol, stigmasterol and sitosterol-3-O-ß-D-glucopyranoside, besides pentacyclic triterpenoids, lupeol, 3-ß-O-acyl-lupeol, lupenone and betulinic acid. The structures of these compounds were identified by ¹H and 13C NMR spectral data analysis and comparison with literature data. For determining of the phenolic content of the etanolic extract of Sterculia striata we used the Folin Ciocalteu reagent, and for the evaluation of antioxidant activity, we utilized the DPPH free radical. This is the first work reporting the chemical study with the stem bark of this species.
