RESUMO
The most prevalent form of inflammatory bowel disease (IBD), ulcerative colitis (UC), is characterized by persistent inflammation of the colorectal mucosa. It is asymptomatic, whereas Crohn's disease (CD) causes patchy lesions in the gastrointestinal tract. Men and women suffer equally from ulcerative colitis, which usually strikes in the second and third decades of life and becomes more common in senior citizens. In the present study, we produced zinc oxide nanoparticles using the natural herbal plant, Cassia alata. Zinc oxide nanoparticles have remarkable antimicrobial and antitumor benefits in the field of biomedical science. Furthermore, the synthesized zinc oxide nanoparticles (ZnO NPs) were characterized using UV, XRD, FTIR, and SEM analyses. The XRD analysis confirmed the crystallite nature and purity of the synthesized nanoparticles. Zinc oxide nanoparticles with a uniform size and partially agglomerated morphology were verified by SEM analysis. We investigated the protective effects of environmentally friendly zinc oxide nanoparticles in dextran sodium sulfate-induced ulcerative colitis mouse models. Green synthesized Cassia alata zinc oxide nanoparticles (CA ZnO NPs) reversed weight loss, disease activity index, colon shortening, and colon histological damage. Zinc oxide nanoparticles reduce hypersensitivity, oxidative stress, and inflammation, and protect the mucosal layer. Green synthesized CA ZnO NPs demonstrated protection against dextran sodium sulfate-induced ulcerative colitis via anti-inflammatory activity.
Assuntos
Cassia , Colite Ulcerativa , Sulfato de Dextrana , Modelos Animais de Doenças , Nanopartículas Metálicas , Óxido de Zinco , Animais , Óxido de Zinco/química , Óxido de Zinco/farmacologia , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Camundongos , Cassia/química , Nanopartículas Metálicas/química , Nanopartículas/química , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
Urinary stones are a growing disease that results from pathological biomineralization. Cassia fistula Lin. is traditionally used to treat urinary stones. However, no scientific evidence is available to prove its antilithiatic effect. This study evaluates the antilithiatic potential of aqueous and ethanolic extract of Cassia fistula Lin. fruit (Cff) against calcium oxalate kidney stones. Forty-two male Wistar rats were divided into seven groups (n = 6/group): Group I (control), Group II (rats treated with ethylene glycol and ammonium chloride developed nephrolithiasis after 28 days), Group III (lithiatic rats receiving distilled water for 30 days), Group IV and V (lithiatic rats receiving aqueous extract of Cff at doses of 1 and 100 mg/kg body weight for 30 days, respectively) and Group VI and VII (lithiatic rats receiving ethanolic extract of Cff at doses of 1 and 100 mg/kg body weight for 30 days, respectively). Some parameters of urine and serum, and also renal oxidative stress and histopathology were used to determine the antilithiatic effect of aqueous and ethanolic extract of Cff. Therefore, the types of extracts of Cff improved abnormal levels of urine, serum, and renal oxidative stress and histopathology parameters. This antilithiatic effect of aqueous and ethanolic extracts of Cff, can be attributed to the anti-crystallization and antioxidant properties of the extracts and the ability to improve urine and serum biochemistry. RESEARCH HIGHLIGHTS: Ethylene glycol and ammonium chloride-induced urolithiasis, aggregation of calcium oxalate deposits, increase of some urinary and serum parameters, relative kidney weight, kidney size and MDA activity, decrease of some urinary parameters, relative body weight and SOD activity. Aqueous and ethanolic extracts of Cassia fistula Lin. lead to the treatment of urolithic rats by decreasing levels of urinary oxalate, phosphate, urea, serum urea, uric acid, creatinine, calcium, phosphate, MDA, kidney weight and kidney size, increasing levels of urinary calcium, creatinine, magnesium, citrate, body weight and SOD activity in the kidney, eliminating CaOx deposition (esp. ethanolic extract).
Assuntos
Cassia , Etilenoglicol , Frutas , Nefrolitíase , Estresse Oxidativo , Extratos Vegetais , Ratos Wistar , Animais , Masculino , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Frutas/química , Ratos , Nefrolitíase/induzido quimicamente , Nefrolitíase/tratamento farmacológico , Cassia/química , Estresse Oxidativo/efeitos dos fármacos , Rim/efeitos dos fármacos , Rim/patologia , Oxalato de Cálcio , Modelos Animais de DoençasRESUMO
Safety issues of the controversial anthraquinones from Cassia obtusifolia seed water extracts (CWEs) limit its application. This work aimed to remove the anthraquinones of CWEs by baking treatment (BT), stir-frying treatment (ST), and adsorption treatment (AT). Effects of these treatments on the chemical composition, physicochemical properties of polysaccharides, and antioxidant activities of CWEs were analyzed and compared. Results indicated that AT exhibited the best removal effect on the total anthraquinone among the three treatments. After AT, the contents of rhein, emodin, aloe-emodin, and aurantio-obtusin of the CWE were below the limit of detection. In addition, AT increased the contents of neutral sugars in CWEs in comparison to BT and ST. None of the treatments had an obvious influence on the structural characteristics of polysaccharides. However, AT decreased the antioxidant activity of CWEs due to their lower anthraquinone content. In summary, AT was considered as an efficient and simple method to remove anthraquinones, while retaining the features of polysaccharides.
Assuntos
Antraquinonas , Cassia , Extratos Vegetais , Sementes , Adsorção , Antraquinonas/química , Antioxidantes/análise , Cassia/química , Culinária/métodos , Emodina/análise , Extratos Vegetais/química , Polissacarídeos/análise , Sementes/químicaRESUMO
Green synthesised silver nanoparticles (AgNPs) have been identified as a promising new therapy pathway for cancer because of their anti-angiogenic potency. In the present study, CM-AgNPs were biosynthesized using aqueous leaf extract of Cassia marginata Roxb (CM) and were confirmed by spectral studies like UV-Visible and attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopic techniques. The structure and shape of the biosynthesized CM-AgNPs were confirmed by scanning electron microscope (SEM), energy-dispersive spectroscopy (EDX), and high-resolution transmission electron microscopy (HR-TEM) with selected area electron diffraction (SAED) studies. The antioxidant activity of the synthesized nanoparticles were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assay methods, and the IC50 values were found to be 19.58 ± 1.62 and 742.33 ± 14.57 µg, respectively. The anticancer activity of CM-AgNPs was evaluated against human breast cancer cell lines MCF-7 and MDA-MB-231 by 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay, and the IC50 values were found to be 21.02 ± 1.67 and 26.21 ± 0.33 µg/ml, respectively. These results provide promising information about the biosynthesized CM-AgNPs that can be used in the development of novel anticancer drugs.
Assuntos
Antineoplásicos , Cassia , Nanopartículas Metálicas , Humanos , Cassia/química , Prata/farmacologia , Prata/química , Nanopartículas Metálicas/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antineoplásicos/farmacologia , Antineoplásicos/química , Antioxidantes/farmacologia , Antioxidantes/química , Espectroscopia de Infravermelho com Transformada de Fourier , Antibacterianos/química , Química VerdeRESUMO
The Cassia (Leguminosae) genus has attracted a lot of attention as a prolific source of alkaloids and chromones with diverse structures and biological properties. The aim of this study is to screen the antiviral compounds from Cassia alata. The extract of the stem bark of this plant was separated using silica gel, MCI, ODS C18, and Sephadex LH-20 column chromatography, as well as semi-preparative HPLC. As a result, three new indole alkaloids, alataindoleins A-C (1-3); one new chromone, alatachromone A (4); and a new dimeric chromone-indole alkaloid, alataindolein D (5) were isolated. Their structures were determined by means of HRESIMS and extensive 1D and 2D NMR spectroscopic studies. Interestingly, alataindolein D (5) represents a new type of dimeric alkaloid with an unusual N-2-C-16' linkage, which is biogenetically derived from a chromone and an indole alkaloid via an intermolecular nucleophilic substitution reaction. Compounds 1-5 were tested for their anti-tobacco mosaic virus (TMV) and anti-rotavirus activities, and the results showed that compounds 2-4 showed high anti-TMV activities with inhibition rates of 44.4%, 66.5%, and 52.3%, respectively. These rates were higher than those of the positive control (with inhibition rate of 32.8%). Compounds 1 and 5 also showed potential anti-TMV activities with inhibition rates of 26.5% and 31.8%, respectively. In addition, compounds 1-5 exhibited potential anti-rotavirus activities with therapeutic index (TI) values in the range of 9.75~15.3. The successful isolation and structure identification of the above new compounds provided materials for the screening of antivirus drugs, and contributed to the development and utilization of C. alata.
Assuntos
Alcaloides , Cassia , Senna , Vírus do Mosaico do Tabaco , Alcaloides/farmacologia , Antivirais/química , Cassia/química , Cromonas/química , Alcaloides Indólicos , Casca de PlantaRESUMO
Traditional bioassay-guided investigation of bioactive compounds from natural products comprises critical steps, such as extraction, repeated column separation, and activity assay. Thus, the development of facile, rapid, and efficient technology is critically important. Here, a HepG2 cell-based extraction method was first developed to rapidly screen potential antitumor compounds from the seeds ofCassia obtusifolia. Then, an online extraction and enrichment-high-speed counter-current chromatography (HSCCC) strategy was fabricated to facilely and efficiently isolate target antitumor compounds, which included direct extraction from solid C. obtusifolia, removal of polar interferences, enrichment of target compounds, and preparative isolation by HSCCC using flow rate stepwise increasing mode. After further purification by Sephadex LH-20 column, five antitumor anthraquinones, aurantio-obtusin, 1-desmethylaurantio-obtusin, chryso-obtusin, obtusin, and questin, were obtained for structural characterization and bioassay verification. The results may not only provide new perspectives for facile and rapid investigation of bioactive compounds from complex natural products, but also offer a scientific basis for the potential applications of C. obtusifolia.
Assuntos
Cassia , Antraquinonas/química , Cassia/química , Distribuição Contracorrente , Extratos Vegetais/química , Sementes/químicaRESUMO
Aurantio-obtusin (AO) is a major anthraquinone (AQ) compound derived from Cassiae semen (CS). Although pharmacological studies have shown that the CS extracts can serve as effective agents in preclinical and clinical practice, AQ-induced hepatotoxicity in humans has attracted widespread attention. To explore whether AO induces hepatotoxicity and its underlying mechanisms, we exposed larval zebrafish and mice to AO. We found that AO delayed yolk sac absorption, and increased liver area and inflammation in the larval zebrafish. This inflammation was manifested as an increase in liver neutrophils and the up-regulated mRNA expression of interleukin-6 (Il-6) and tumor necrosis factor-α (Tnf-α) in the larval zebrafish. Furthermore, a pharmacokinetics study showed that AO was quickly absorbed into the blood and rapidly metabolized in the mice. Of note, AO induced hepatotoxicity in a gender-dependent manner, characterized by liver dysfunction, increased hepatocyte necrosis with inflammatory infiltration, and up-regulated mRNAs of Il-6, Tnf-α and monocyte chemotactic protein 1(Mcp1) in the female mice after 28-day oral administration. It also highlighted that AO triggered NOD-like receptor protein (NLRP) signaling in the female mice, as evidenced by the increased NLRP3, Caspase-1, pro-IL-1ß, IL-1ß and IL-18. Finally, we found that AO led to a significant increase in potassium calcium-activated channel, subfamily N, member 4 (KCNN4) and reactive oxygen species (ROS) levels, along with decreased nuclear factor kappa B p65 (NF-κB p65), in the female mouse livers. In conclusion, AO induced hepatotoxicity by activating NLRP3 inflammasome signaling, at least in part, through increased KCNN4 and ROS production, and NF-κB inhibition.
Assuntos
Antraquinonas/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Inflamassomos/metabolismo , Inflamação/induzido quimicamente , Inflamação/fisiopatologia , Peixe-Zebra/metabolismo , Animais , Cassia/química , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/toxicidade , Feminino , Humanos , Larva/efeitos dos fármacos , Camundongos , Transdução de Sinais/efeitos dos fármacosRESUMO
Here, we identified the mechanisms of action of antidiabetic activity of novel compounds isolated from Cassia fistula stem bark in STZ-diabetic animals. Novel triterpenoid compounds (C1, C2 and C3) were treated to STZ-administered diabetic animals at a concentration of 20mg/kg body weight orally for 60 days to assess their effects on plasma glucose, plasma insulin/C-peptide, serum lipid markers and the enzymes of carbohydrate metabolism, glucose oxidation and insulin signaling molecules. Oral administration of novel triterpenoid compounds to STZ-diabetic animals significantly decreased (p < 0.05) the plasma glucose concentration on the 7th, 15th, 30th, 45th and 60th daysin a duration-dependent manner (p < 0.05). Plasma insulin (p < 0.0001)/C-peptide (p < 0.0006), tissue glycogen (p < 0.0034), glycogen phosphorylase (p < 0.005), glucose 6-phosphatase (p < 0.0001) and lipid markers were significantly increased (p < 0.0001) in diabetic rats, whereas glucokinase (p < 0.0047), glycogen synthase (p < 0.003), glucose oxidation (p < 0.001), GLUT4 mRNA (p < 0.0463), GLUT4 protein (p < 0.0475) and the insulin-signaling molecules IR mRNA (p < 0.0195), IR protein (p < 0.0001), IRS-1 mRNA (p < 0.0478), p-IRS-1Tyr612 (p < 0.0185), Akt mRNA (p < 0.0394), p-AktSer473 (p < 0.0162), GLUT4 mRNA (p < 0.0463) and GLUT4 (p < 0.0475) were decreased in the gastrocnemius muscle. In silico analysis of C1-C3 with IRK and PPAR-γ protein coincided with in vivo findings. C1-C3 possessed promising antidiabetic activity by regulating insulin signaling mechanisms and carbohydrate metabolic enzymes.
Assuntos
Cassia/química , Diabetes Mellitus Tipo 1/tratamento farmacológico , Diabetes Mellitus Tipo 1/metabolismo , Hipoglicemiantes/farmacologia , Insulina/metabolismo , Triterpenos/farmacologia , Animais , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Peptídeo C/sangue , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/genética , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 1/genética , Glucoquinase/metabolismo , Glucose-6-Fosfatase/metabolismo , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Insulina/sangue , Proteínas Substratos do Receptor de Insulina/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Simulação de Acoplamento Molecular , Estrutura Molecular , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/metabolismo , PPAR gama/metabolismo , Casca de Planta/química , Plantas Medicinais/química , Canais de Potássio Corretores do Fluxo de Internalização/metabolismo , Proteínas Proto-Oncogênicas c-akt/genética , Proteínas Proto-Oncogênicas c-akt/metabolismo , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos , Ratos Wistar , Transdução de Sinais/efeitos dos fármacos , Triterpenos/química , Triterpenos/isolamento & purificaçãoRESUMO
Cassia obtusifolia L., of the Leguminosae family, is used as a diuretic, laxative, tonic, purgative, and natural remedy for treating headache, dizziness, constipation, tophobia, and lacrimation and for improving eyesight. It is commonly used in tea in Korea. Various anthraquinone derivatives make up its main chemical constituents: emodin, chrysophanol, physcion, obtusifolin, obtusin, au rantio-obtusin, chryso-obtusin, alaternin, questin, aloe-emodin, gluco-aurantio-obtusin, gluco-obtusifolin, naphthopyrone glycosides, toralactone-9-ß-gentiobioside, toralactone gentiobioside, and cassiaside. C. obtusifolia L. possesses a wide range of pharmacological properties (e.g., antidiabetic, antimicrobial, anti-inflammatory, hepatoprotective, and neuroprotective properties) and may be used to treat Alzheimer's disease, Parkinson's disease, and cancer. In addition, C. obtusifolia L. contributes to histamine release and antiplatelet aggregation. This review summarizes the botanical, phytochemical, and pharmacological features of C. obtusifolia and its therapeutic uses.
Assuntos
Cassia/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitoterapia , Plantas Medicinais/química , Animais , Antraquinonas/química , Antraquinonas/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Etnofarmacologia , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Medicina Tradicional Coreana , Mosquitos Vetores/efeitos dos fármacos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Compostos Fitoquímicos/uso terapêutico , República da CoreiaRESUMO
Medicinal plant species contain vast and unexploited riches of chemical substances with high medical potential making these plant species valuable as biomedicine sources. Cassia fistula L is an important medicinal plant used in many traditional medicinal systems including Ayurveda and Chinese Traditional Medicine. It is a deciduous medium sized tree with elongated and rod-shaped fruits having pulp and have bright yellow flowers, earning the name 'Yellow Shower'. The present review provides a version of updated information on its botanical description and pharmacological properties including antioxidant, antimicrobial, anti-inflammatory, antidiabetic, antitumor, hepatoprotective among other activities. Pharmacological reviews on medicinal plants will provide valuable information; thus, Cassia fistula L can provide important discoveries of valuable bioactive natural products facilitating in developing novel pharmaceuticals products.
Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Cassia , Fármacos Gastrointestinais/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antitussígenos/isolamento & purificação , Antitussígenos/farmacologia , Cassia/química , Fármacos Gastrointestinais/isolamento & purificação , Humanos , Compostos Fitoquímicos/isolamento & purificação , Fitoterapia , Extratos Vegetais/isolamento & purificação , Cicatrização/efeitos dos fármacosRESUMO
BACKGROUND: Inflammation is a key element in tumor progression, over time, persistent inflammation causes damage to DNA and leads to cancer. The relationship between chronic inflammation and tumor development is well established, blocking of which can help in cancer prevention and treatment in the future. OBJECTIVE: Hence, with this background, the present study aims to evaluate the anti-inflammatory and anticancer potential of Cassia auriculata (CA) solvent fractions through in silico and in vitro means, respectively. METHODS: Generally, inflammatory mediators play a key task in chronic inflammation, following its inflection was chosen for their interactions with nine structurally varied phytoconstituents of CA identified through GCMS. The ethanolic extract of CA was assessed for its apoptotic effects on A549 lung cancer cells by 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, JC-10 staining, DNA fragmentation assay and quantitative Real-Time Polymerase Chain Reaction (qRT-PCR). RESULTS: The interactions between bioactive components and target protein revealed that important molecules like 5,7-dihydroxy-2-[2-nethoxyphenyl]- 4H-1-Benzopyran-4-one, a flavonoid, and three other components can bind target interleukin 1-beta associated with lung cancer. In vitro data also confirmed that the diverse active components of CA extract might follow the intrinsic mitochondrial pathway to provoke cancer cell death. CONCLUSION: Hence, these findings strongly propose that Cassia auriculata (CA) solvent fractions could be exploited in the future to design ligands for obtaining novel leads for treating chronic inflammation linked with lung cancer, and also the extracts of CA can be recommended as a potential agent for lung cancer chemotherapy.
Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Cassia/química , Flavonoides/farmacologia , Inflamação/tratamento farmacológico , Interleucina-1beta/antagonistas & inibidores , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Células A549 , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Flavonoides/química , Flavonoides/isolamento & purificação , Humanos , Inflamação/metabolismo , Inflamação/patologia , Interleucina-1beta/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: According to ethnobotanical surveys, Cassia sieberiana DC. (1825) is a particularly reputed species in African folk Medicine, namely due to the application of its leaves and roots for the treatment of diseases and symptomatology that appear to be related with an inflammatory background. In contrast with the roots of the plant, the leaves remain to be investigated, which prompted us to further detail mechanisms underlying their anti-inflammatory properties, by using in vitro models of disease. AIM OF THE STUDY: Considering its use in the amelioration and treatment of conditions that frequently underlie an inflammatory response, C. sieberiana leaves extract was prioritized amongst a collection of extracts obtained from plants collected in Guinea-Bissau. As such, this work aims to deliver experimental data on the anti-inflammatory properties of C. sieberiana leaf and to establish possible associations with its chemical composition, thus providing a rationale on its use in folk Medicine. MATERIALS AND METHODS: The chemical profile of an hydroethanol extract obtained from the leaves of the plant was established by HPLC-DAD-ESI/MSn in order to identify bioactives. The extract and its main compound were tested towards a series of inflammatory mediators, both in enzymatic and cell-based models. The capacity to interfere with the eicosanoid-metabolizing enzymes 5-lipoxygenase (5-LOX), cyclooxygenase-1 (COX-1) and -2 (COX-2) was evaluated in cell-free systems, while the effects in interleukin 6 (IL-6) and tumour necrosis factor-α (TNF-α) levels produced by THP-1 derived macrophages were assessed through ELISA. RESULTS: HPLC-DAD-ESI/MSn analysis of the extract elucidated a chemical profile qualitatively characterized by a series of anthraquinones, particularly rhein derivatives, and nine flavonols, most of which 3-O-glycosylated. Considering the concentrations of the identified compounds, quercetin was detached as the main component. Effects of the hydroethanol extract obtained from C. sieberiana leaves against key enzymes of the arachidonic acid cascade were recorded, namely a concentration-dependent inhibition against 5-LOX, at concentrations ranging from 16 to 250 µg mL-1 and a selective inhibitory action upon COX-2 (IC50 = 3.58 µg mL-1) in comparison with the isoform COX-1 (IC50 = 9.10 µg mL-1). Impact on inflammatory cytokines was also noted, C. sieberiana leaf extract significantly decreasing IL-6 levels in THP-1 derived macrophages at 250 and 500 µg mL-1. In contrast, TNF-α levels were found to be increased in the same model. Quercetin appears to partially account for the observed effects, namely due to the significant inhibitory effects on the activity of the arachidonic acid metabolizing enzymes COX-2 and 5-LOX. CONCLUSIONS: The anti-inflammatory effects herein reported provide a rationale for the use of C. sieberiana leaves in African folk practices, such as in the treatment of arthritis, rheumatism and body aches. Considering the occurrence of flavonoidic and anthraquinonic constituents, as well as the observed anti-inflammatory properties of quercetin, recorded effects must be related with the presence of several bioactives.
Assuntos
Anti-Inflamatórios/farmacologia , Cassia/química , Inibidores Enzimáticos/farmacologia , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Antraquinonas/química , Anti-Inflamatórios/química , Ciclo-Oxigenase 1/efeitos dos fármacos , Ciclo-Oxigenase 2/efeitos dos fármacos , Citocinas/antagonistas & inibidores , Eicosanoides/metabolismo , Inibidores Enzimáticos/química , Flavonoides/química , Flavonoides/farmacologia , Guiné-Bissau , Humanos , Inflamação/induzido quimicamente , Lipopolissacarídeos/toxicidade , Medicina Tradicional , Fenóis/química , Extratos Vegetais/química , Folhas de Planta/química , Células THP-1RESUMO
A novel antioxidative film was prepared by drying a film-forming solution containing the Flos Sophorae Immaturus extract (FSIE) (0-3.5%) and cassia gum (CG). Scanning electron microscopy (SEM) showed that FSIE was successfully compounded with CG. Although the addition of FSIE slightly increased the water vapor permeability (WVP) and O2 permeability (OP) of the film, it also improved its ability to block ultraviolet light significantly. The appropriate amounts of FSIE increased the tensile strength (TS) from 20.9 MPa to 30.2 MPa but reduced the elongation at break (EB) from 38.7% to 27.6%. The films doped with FSIE exhibited strong antioxidative activity and high rates of free radical scavenging. Total phenols exhibited a positive trend as the amount of FSIE increased in 50% of ethanol. The practical application of these composite films was investigated by evaluating the quality of lard wrapped in the films. After 25 d, the acid value (XAV) and peroxide value (POV) of lard packaged in CG/FSIE2% were lower than the values for lard packaged in CG/FSIE0% and plastic bag. These results showed that the CG/FSIE film had superior antioxidative activity compared to films made from plastic and pure CG.
Assuntos
Antioxidantes/química , Cassia/química , Embalagem de Alimentos/métodos , Extratos Vegetais/química , Gomas Vegetais/química , Sophora/química , Filmes Comestíveis , Temperatura Alta , Microscopia Eletrônica de Varredura , Oxigênio , Permeabilidade , Fenóis/análise , Extratos Vegetais/análise , Gomas Vegetais/análise , Espectroscopia de Infravermelho com Transformada de Fourier , Vapor/análise , Resistência à Tração , Raios Ultravioleta , Difração de Raios XRESUMO
BACKGROUND: Multidrug-resistant (MDR) bacteria remain a major cause of morbidity and mortality globally. The present study was designed to investigate the in vitro antibacterial activities of crude methanol extract and constituents isolated by Column Chromatography (CC) from Cassia sieberiana bark (CSB) against ten MDR Gram-negative bacteria, as well as the mechanisms of action of the most active sample. METHODS: The antibacterial activity of the tested samples (extract, the fractions and their compounds isolated by CC and the structures obtained by exploiting 1H and 13C Nuclear magnetic resonance (NMR) spectra) in the presence and absence of an efflux pumps inhibitor, phenylalanine-arginine ß-naphthylamide (PAßN), was evaluated using the micro-dilution method. The effects of the most active sample were evaluated on the cell growth kinetic and on the bacterial H+-ATPase proton pumps. RESULTS: Phytochemical composition of the crude extract showed a rather selective distribution of secondary metabolites (presence of polyphenols, tannins, steroids, triterpenes, flavonoids, alkaloids, saponins and absence of anthocyanins, anthraquinones). The tested samples displayed different antibacterial activities with minimal inhibitory concentrations (MICs) ranging from 64 to 512 µg/mL. Crude extract (CS) and fraction CSc showed the highest inhibitory spectra, both inhibiting all of the studied bacteria except Enterobacter aerogenes EA27 strain. Fraction CSc exerted bactericidal effects on most bacteria meanwhile, crude extract (CS) and sub-fraction CSc2 exerted bacteriostatic effects. Compounds 1 (spectaline) and 2 (iso-6-cassine) inhibited the growth of 70% (Escherichia coli ATCC8739 and AG102, Klebsiella pneumoniae ATCC11296, Enterobacter aerogenes ATCC13048 and EA27, Providencia stuartii ATCC29916, Pseudomonas aeruginosa PA01) and 60% (Escherichia coli ATCC8739, Klebsiella pneumoniae ATCC11296 and KP55, Providencia stuartii ATCC29916, Pseudomonas aeruginosa PA01 and PA124) of bacteria respectively with MICs ranging from 128 to 512 µg/mL. In the presence of PAßN, the activities of crude extract CS, fraction CAc and sub-fraction CSc2 strongly increased on most bacteria strains as their MICs significantly decreased. Sub-fraction CSc2 inhibited the H+-ATPase proton pumps and altered growth kinetic of Escherichia coli ATCC8739. CONCLUSION: The overall results justify the traditional use of C. sieberiana for the treatment of bacterial infections.
Assuntos
Antibacterianos/farmacologia , Cassia/química , Dipeptídeos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/metabolismo , Proteínas de Bactérias/antagonistas & inibidores , Proteínas de Bactérias/metabolismo , Farmacorresistência Bacteriana Múltipla , Bactérias Gram-Negativas/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Casca de Planta/química , Extratos Vegetais/química , ATPases Translocadoras de Prótons/antagonistas & inibidores , ATPases Translocadoras de Prótons/metabolismoRESUMO
Two structurally unique polyphenols, alatains A (1) and B (2), were isolated from the bark of Cassia alata. Their structures were elucidated on the basis of spectroscopic analysis. Compounds 1 and 2 represent a new type of hetero-dimeric polyphenols with a C-14-C-5' linkage, biogenetically formed by an unusual intermolecular oxidative phenol-coupling reaction between a chromone unit and an isocoumarin moiety. Moreover, compounds 1 and 2 showed significant anti-tobacco mosaic virus (anti-TMV) inhibition IC50 values of 18.8 and 11.4 µM, respectively. Alatains A and B also exhibited promising protective effects on TMV infection of the host plants (Nicotiana tabacum) with the inhibition rates of 54.6% and 69.7% at the concentration of 20 µM, respectively. The results provided a new structural template for potential anti-TMV agent discovery.
Assuntos
Antivirais/farmacologia , Cassia/química , Polifenóis/farmacologia , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antivirais/isolamento & purificação , China , Cromonas , Isocumarinas , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Polifenóis/isolamento & purificação , Nicotiana/virologiaRESUMO
UPLC-MS/MS profiling of Cassia glauca leaves extract revealed the identification of 10 flavonoids. Kaempferol 3-O-ß-D-rutinoside was isolated and studied for its cytotoxic activity. It showed high cytotoxic effects against MCF-7 (IC50 of 4.6±0.038 µg/ml) and HepG-2 (IC50 of 8.2±0.024 µg/ml) cancer cell lines, compared to the leaves extracts, their Ag nanoparticles, and doxorubicin. Moreover, Kaempferol 3-O-ß-D-rutinoside exerted a synergistic cytotoxic effect with doxorubicin on MCF-7 cell lines. It was discovered as kinases and aldose reductase inhibitor while rationalizing its cytotoxic activity through molecular docking study. Thus, it is expected that the cardiotoxic effects of doxorubicin can be also decreased by using Kaempferol 3-O-ß-D-rutinoside due to its aldose reductase inhibitory effect. These findings suggested that Kaempferol 3-O-ß-D-rutinoside could be used in combination with chemotherapeutic drugs to increase the sensitivity to their cytotoxic activity and protect against their side effects.
Assuntos
Aldeído Redutase/antagonistas & inibidores , Cassia/química , Inibidores Enzimáticos/química , Nanopartículas Metálicas/química , Simulação de Acoplamento Molecular , Prata/química , Aldeído Redutase/metabolismo , Sítios de Ligação , Cassia/metabolismo , Domínio Catalítico , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Doxorrubicina/farmacologia , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Quempferóis/farmacologia , Nanopartículas Metálicas/toxicidade , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Espectrometria de Massas em TandemRESUMO
Natural products are used as alternative drugs in traditional medicine to treat infection and inflammation and relieve pain. Heartwood of Cassia garettiana Craib has been investigated as an ingredient in Thai traditional medicine for anti-HIV protease, but there is no report on its antibacterial and anti-inflammatory activities. The objectives of this study were to investigate the anti-inflammatory and antibacterial activities, time-kill profile, and main active constituents of an ethanolic extract of C. garettiana heartwood. The study followed the generally accepted experimental design. All tests were investigated in triplicate. The heartwood of C. garettiana was extracted by maceration with 95% EtOH. The antibacterial activity of the extract and its chemical constituents were determined by their MIC values using resazurin as an indicator. Time-kill profile was determined at 0, 2, 4, 6, 8, 10, 12, and 24 hrs and expressed as log CFU/mL. The anti-inflammatory activity of the extract and its chemical components was investigated by their inhibiting effect on IL-6 and TNF-α production by ELISA. The ethanolic extract was analyzed for its chemical constituents by HPLC technique. The ethanolic extract showed both dose- and time-dependent bactericidal effects against Staphylococcus aureus, methicillin-resistance Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Salmonella Typhi, Salmonella Typhimurium, Klebsiella pneumoniae, and Shigella dysenteriae with MIC values of 312.5, 312.5, 312.5, 1,250, 2,500, 625, 625, 2,500, and 625 µg/mL, respectively. It showed an inhibiting effect on IL-6 production at concentrations of 12.5 to 100 µg/mL. The main active chemical constituent of C. garettiana was piceatannol that showed antibacterial activity against all test bacteria except P. aeruginosa. C. garettiana showed a broad spectrum of antibacterial activity against both Gram-negative and Gram-positive bacteria. Piceatannol and resveratrol from the plant strongly inhibited IL-6 production. Based on these results, we concluded that the ethanolic extract of C. garettiana showed both an antibacterial activity and inhibition of IL-6. Piceatannol is the active constituent of the extract and showed anti-inflammatory and antibacterial activities against Gram-negative and Gram-positive bacteria.
Assuntos
Antibacterianos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Cassia/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Antibacterianos/química , Anti-Inflamatórios não Esteroides/química , Bactérias/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Etanol/química , Interleucina-6/metabolismo , Lipopolissacarídeos/toxicidade , Camundongos , Testes de Sensibilidade Microbiana , Células RAW 264.7 , Resveratrol/análise , Estilbenos/análise , Fator de Necrose Tumoral alfa/metabolismoRESUMO
The present study is an attempt to evaluate the in vitro anti-inflammatory and in silico anticancer potentials of the plant Cassia auriculata (CA). The aerial parts of CA were subjected to solvent extraction, and the extracts were fractionised by gas chromatography and mass spectrometry analysis for its phytochemical content. The antiinflammatory activity of the extracts were confirmed by the IC50 value of 125.02â µg/ml for red blood cell membrane stabilisation and 195.7â µg/ml for inhibition of protein denaturation activity. The interaction of bioactive compounds of CA ethanol extract with target protein was predicted through molecular docking studies, serine/threonine-protein kinase B (AKT1), responsible for development and progression of lung cancer using AutoDock tools. Extensive studies have been carried out on a range of kinase inhibitors targeting Akt, but obtaining promising results is a challenge yet due to its toxicity and resistance issues. Yohimbine, undecanoic acid 10-methyl-ethyl ester and chrysin significantly bind to the target protein with least binding energy. Hence, the present paper establishes the anti-inflammatory and anticancer capacities of CA ethanol extract as an alternative to the existing therapeutic approach to inflammation and cancer through a systematic in vitro and in silico approaches supplementing the findings.
Assuntos
Cassia/química , Compostos Fitoquímicos , Extratos Vegetais , Anti-Inflamatórios/química , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Simulação por Computador , Membrana Eritrocítica/efeitos dos fármacos , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/metabolismo , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Proteínas Proto-Oncogênicas c-akt/química , Proteínas Proto-Oncogênicas c-akt/metabolismoRESUMO
Aloe-emodin is a naturally anthraquinone derivative and an active ingredient of Chinese herbs, such as Cassia occidentalis, Rheum palmatum L., Aloe vera, and Polygonum multiflorum Thunb. Emerging evidence suggests that aloe-emodin exhibits many pharmacological effects, including anticancer, antivirus, anti-inflammatory, antibacterial, antiparasitic, neuroprotective, and hepatoprotective activities. These pharmacological properties lay the foundation for the treatment of various diseases, including influenza virus, inflammation, sepsis, Alzheimer's disease, glaucoma, malaria, liver fibrosis, psoriasis, Type 2 diabetes, growth disorders, and several types of cancers. However, an increasing number of published studies have reported adverse effects of aloe-emodin. The primary toxicity among these reports is hepatotoxicity and nephrotoxicity, which are of wide concern worldwide. Pharmacokinetic studies have demonstrated that aloe-emodin has a poor intestinal absorption, short elimination half-life, and low bioavailability. This review aims to provide a comprehensive summary of the pharmacology, toxicity, and pharmacokinetics of aloe-emodin reported to date with an emphasis on its biological properties and mechanisms of action.
Assuntos
Antraquinonas/farmacologia , Antraquinonas/farmacocinética , Antraquinonas/toxicidade , Aloe/química , Animais , Cassia/química , Fallopia multiflora/química , Humanos , Rheum/químicaRESUMO
In this study, we determined the antimicrobial activity of ten essential oils (EOs)-oregano, thyme, clove, arborvitae, cassia, lemongrass, melaleuca, eucalyptus, lavender, and clary sage-against drug-resistant microorganisms previously isolated from patients with skin infections. The essential oil compositions were determined using gas chromatography coupled to mass spectrometry (GC/MS). The assayed bacteria included Pseudomonas aeruginosa, Proteus vulgaris, Citrobacter koseri, and Klebsiella pneumoniae. Two drug-resistant yeasts (Candida albicans and Candida parapsilosis) were also involved in our survey. Oregano, thyme, cassia, lemongrass and arborvitae showed very strong antibacterial and antifungal activity against all tested strains. These results show that these essential oils may be effective in preventing the growth of the drug-resistant microorganisms responsible for wound infections. In this study, the genotoxic effects of tested essential oils on healthy human keratinocytes HaCaT were evaluated using the comet assay for the first time. These results revealed that none of the essential oils induced significant DNA damage in vitro after 24 h. Moreover, the treatment of HaCaT cells with essential oils increased the total antioxidant status (TAS) level. The obtained results indicate that EOs could be used as a potential source of safe and potent natural antimicrobial and antioxidant agents in the pharmaceutical and food industries.