RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Hyperuricemic nephropathy (HN) is a renal injury caused by hyperuricemia and is the main cause of chronic kidney disease and end-stage renal disease. ShiWeiHeZiSan, which is composed mainly of components of Terminalia chebula Retz. And is recorded in the Four Medical Tantras, is a typical traditional Tibetan medicinal formula for renal diseases. Although T. chebula has been reported to improve renal dysfunction and reduce renal cell apoptosis, the specific mechanism of the nephroprotective effects of T. chebula on HN is still unclear. AIM OF THE STUDY: This study was conducted to evaluate the effects and specific mechanism of T. chebula extract on HN through network pharmacology and in vivo and in vitro experiments. MATERIALS AND METHODS: Potassium oxalate (1.5 g/kg) and adenine (50 mg/kg) were combined for oral administration to establish the HN rat model, and the effects of T. chebula extract on rats in the HN model were evaluated by renal function indices and histopathological examinations. UPLC-Q-Exactive Orbitrap/MS analysis was also conducted to investigate the chemical components of T. chebula extract, and the potential therapeutic targets of T. chebula in HN were predicted by network pharmacology analysis. Moreover, the activation of potential pathways and the expression of related mRNAs and proteins were further observed in HN model rats and uric acid-treated HK-2 cells. RESULTS: T. chebula treatment significantly decreased the serum uric acid (SUA), blood urea nitrogen (BUN) and serum creatinine (SCr) levels in HN rats and ameliorated renal pathological injury and fibrosis. A total of 25 chemical components in T. chebula extract were identified by UPLC-Q-Exactive Orbitrap/MS analysis, and network pharmacology analysis indicated that the NF-κB pathway was the potential pathway associated with the therapeutic effects of T. chebula extract on HN. RTâPCR analysis, immunofluorescence staining and ELISA demonstrated that the mRNA and protein levels of TLR4 and MyD88 were significantly decreased in the renal tissue of HN rats after treatment with T. chebula extract at different concentrations, while the phosphorylation of P65 and the secretion of TNF-α and IL-6 were significantly inhibited. The results of in vitro experiments showed that T. chebula extract significantly decreased the protein levels of TLR4, MyD88, p-IκBα and p-P65 in uric acid-treated HK-2 cells and inhibited the nuclear translocation of p65 in these cells. In addition, the expression of inflammatory factors (IL-1ß, IL-6 and TNF-α) and fibrotic genes (α-SMA and fibronectin) was significantly downregulated by T. chebula extract treatment, while E-cadherin expression was significantly upregulated. CONCLUSION: T. chebula extract exerts nephroprotective effects on HN, such as anti-inflammatory effects and fibrosis improvement, by regulating the TLR4/MyD88/NF-κB axis, which supports the general use of T. chebula in the management of HN and other chronic kidney diseases.
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Hiperuricemia , Terminalia , Ratas , Animales , FN-kappa B/metabolismo , Hiperuricemia/tratamiento farmacológico , Hiperuricemia/metabolismo , Factor 88 de Diferenciación Mieloide/metabolismo , Ácido Úrico/farmacología , Receptor Toll-Like 4/metabolismo , Transducción de Señal , Factor de Necrosis Tumoral alfa/metabolismo , Interleucina-6/metabolismo , Terminalia/metabolismo , FibrosisRESUMEN
Ulcerative colitis (UC) is a chronic inflammatory disease significantly impacting patients' lives. This study aimed to elucidate the alleviating effect of ethyl acetate extract (TBEA) from Terminalia bellirica fruit on UC and to explore its mechanism. TBEA was the fraction with the best anti-inflammatory activity screened using in vitro anti-inflammatory assays, and HPLC initially characterized its composition. The mice model of ulcerative colitis was established after free drinking of 2.5% dextran sulfate sodium for six days, and the experimental group was treated with 50 mg/kg and 100 mg/kg TBEA for seven days. We found that TBEA significantly alleviated symptoms in UC mice, including a physiologically significant reduction in disease activity index and pathological damage to colonic tissue. TBEA dramatically slowed down oxidative stress and inflammatory process in UC mice, as evidenced by decreasing myeloperoxidase and malondialdehyde activities and increasing glutathione and catalase levels by reducing the concentrations of IL-6, IL-1ß, TNF-α, and NO in UC mice, as well as by regulating key proteins in the IL-6/JAK2/STAT3 pathway. Meanwhile, TBEA maintained intestinal homeostasis by regulating intestinal flora structure. Our study provides new ideas for developing TBEA into a new drug to treat UC.
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Colitis Ulcerosa , Colitis , Microbioma Gastrointestinal , Terminalia , Animales , Ratones , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/tratamiento farmacológico , Colitis Ulcerosa/metabolismo , Citocinas/metabolismo , Terminalia/metabolismo , Mediadores de Inflamación/metabolismo , Interleucina-6/metabolismo , Frutas/metabolismo , Colon/metabolismo , Antiinflamatorios/uso terapéutico , Sulfato de Dextran/efectos adversos , Ratones Endogámicos C57BL , Modelos Animales de Enfermedad , Colitis/tratamiento farmacológicoRESUMEN
Acetylcholinesterase (AChE) is an important therapeutic target for the treatment of Alzheimer's disease (AD), and the development of natural AChE inhibitors as candidates has played a significant role in drug discovery. In this study, the inhibition mechanisms of four ellagitannins, punicalagin, chebulinic acid, geraniin and corilagin, from Terminalia chebula fruits on AChE were investigated systematically by a combination of inhibition kinetics, multi-spectroscopic methods and molecular docking. The kinetic results showed that punicalagin, chebulinic acid and geraniin exhibited strong reversible inhibitory effects on AChE in an uncompetitive manner with the IC50 values of 0.43, 0.50, and 0.51 mM, respectively, while corilagin inhibited AChE activity in a mixed type with the IC50 value of 0.72 mM. The results of fluorescence and UV-vis spectra and fluorescence resonance energy transfer (FRET) revealed that four ellagitannins could significantly quenched the intrinsic fluorescence of AChE though a static quenching along with non-radiative energy transfer. Thermodynamic analyses showed that values of ΔG, ΔH and ΔS were negative, indicating that all binding processes were spontaneous, and the hydrogen bonding and Van der Waals forces might make a great contribution to the formation of inhibitor-AChE complexes. The synchronous fluorescence, three-dimensional (3D) fluorescence, UV-vis, and FT-IR spectra studies suggested that four ellagitannins could lead to alterations in the micro-environment and secondary structure of AChE, and thus the conformational change of AChE. Moreover, molecular docking demonstrated that four ellagitannins could interacted with main amino acid residues of AChE with affinity energies ranging from -9.9 to -8.7 kJ/mol, and further confirmed the above experimental results. This study provided valuable findings for the potential application of four ellagitannins as promising candidates in the exploration of natural AChE inhibitors for the treatment of AD.
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Taninos Hidrolizables , Terminalia , Simulación del Acoplamiento Molecular , Taninos Hidrolizables/metabolismo , Acetilcolinesterasa/metabolismo , Terminalia/metabolismo , Unión Proteica , Sitios de Unión , Espectroscopía Infrarroja por Transformada de Fourier , Frutas/metabolismo , CinéticaRESUMEN
Current therapies for ischemic stroke are insufficient due to the lack of specific drugs. This study aimed to investigate the protective activity of polyphenol extracts from Terminalia chebula against cerebral ischemia-reperfusion induced damage. Polyphenols of ethyl acetate and n-butanol fractions were extracted from T. chebula. BV2 microglial cells exposed to oxygen-glucose deprivation/reoxygenation and mice subjected to middle cerebral artery occlusion/reperfusion were treated by TPE and TPB. Cell viability, cell morphology, apoptosis, mitochondrial membrane potential, enzyme activity and signaling pathway related to oxidative stress were observed. We found that TPE and TPB showed strong antioxidant activity in vitro. The protective effects of TPE and TPB on cerebral ischemia-reperfusion injury were demonstrated by enhanced antioxidant enzyme activities, elevated level of the nucleus transportation of nuclear factor erythroid 2-related factor 2 and expressions of antioxidant proteins, with a simultaneous reduction in cell apoptosis and reactive oxygen species level. In conclusion, TPE and TPB exert neuroprotective effects by stimulating the Nrf2 signaling pathway, thereby inhibiting apoptosis.
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Fármacos Neuroprotectores , Daño por Reperfusión , Terminalia , 1-Butanol/farmacología , Animales , Antioxidantes/metabolismo , Glucosa/farmacología , Ratones , Factor 2 Relacionado con NF-E2/metabolismo , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Estrés Oxidativo , Oxígeno/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Polifenoles/farmacología , Polifenoles/uso terapéutico , Especies Reactivas de Oxígeno/metabolismo , Daño por Reperfusión/tratamiento farmacológico , Daño por Reperfusión/metabolismo , Terminalia/metabolismoRESUMEN
Intestinal ischemia/reperfusion (II/R) injury is a common life-threatening complication with high morbidity and mortality. Chebulae Fructus Immaturus, the unripe fruit of Terminalia chebula Retz., also known as "Xiqingguo" or "Tibet Olive" in China, has been widely used in traditional Tibetan medicine throughout history. The phenolic acids' extract of Chebulae Fructus Immaturus (XQG for short) has exhibited strong antioxidative, anti-inflammation, anti-apoptosis, and antibacterial activities. However, whether XQG can effectively ameliorate II/R injuries remains to be clarified. Our results showed that XQG could effectively alleviate II/R-induced intestinal morphological damage and intestinal barrier injury by decreasing the oxidative stress, inflammatory response, and cell death. Transcriptomic analysis further revealed that the main action mechanism of XQG protecting against II/R injury was involved in activating PPARα and inhibiting the NF-κB-signaling pathway. Our study suggests the potential usage of XQG as a new candidate to alleviate II/R injury.
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Hidroxibenzoatos/farmacología , Daño por Reperfusión , Terminalia , Animales , Ratones , FN-kappa B/metabolismo , PPAR alfa , Extractos Vegetales , Daño por Reperfusión/tratamiento farmacológico , Terminalia/metabolismoRESUMEN
As a psychoactive substance abused worldwide, methamphetamine (METH) abuse leads to multiple neurodegenerative symptoms including memory deficits. Terminalia chebula retzius extracts (TREs) isolated by our lab have great antioxidant activity and its effect on METH-induced memory deficits has not been investigated yet. The present study was designed to investigate the protective effect of TREs on METH induced cell apoptosis in vitro and memory deficits in vivo. The results showed that TREs treatment attenuated free radical release and improved cell survival of primary hippocampal neurons after METH injury. In the Morris water maze task, TREs treatment reversed METH-induced learning and memory deficits in acquisition and retention. Moreover, TREs reduced oxidative stress in the serum and hippocampus of mice. Additionally, extracellular regulated protein kinases (ERK1/2) pathway and the nuclear factor E2-related factor 2 (Nrf2) pathway were inactivated after METH treatment, and were significantly activated after TREs pretreatment. These findings suggest that TREs may exert potent neuroprotective effect via activation of both ERK and Nrf2 pathways, thus providing a basis for its potential use for ameliorating memory deficits induced by METH.
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Metanfetamina , Terminalia , Animales , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , Metanfetamina/toxicidad , Ratones , Factor 2 Relacionado con NF-E2/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Terminalia/metabolismoRESUMEN
Anogeissus acuminata is used to treat wounds, diarrhoea, dysentery, and skin ailments. However, its hepatoprotective effect against ethanol-induced liver damage is yet to be reported. The phenolic-enriched ethyl acetate fraction of Anogeissus acuminata (AAE) was evaluated for hepatoprotective activity against ethanol-induced liver toxicity in rats. The intoxicated animals were treated with a phenolic-rich fraction of Anogeissus acuminata (AAE) (100 and 200 mg/kg) and silymarin (100 mg/kg). The antioxidant activity of AAE was analysed. Biochemical markers (ALT, AST, ALP, GGT, and TBL) for liver injury in ethanol-administered animals resulted in higher levels of key serum biochemical injury markers, as evidenced by increased levels of ALT (127.24 ± 3.95), AST (189.54 ± 7.56), ALP (263.88 ± 12.96), GGT (91.65 ± 3.96), and TBL (2.85 ± 0.12) compared to Group I ALT (38.67 ± 3.84), AST (64.45 ± 5.97), GGT (38.67 ± 3.84), and TBL (0.53 ± 064) (p < 0.05). AAE administration decreased serum biochemical liver injury markers as manifested in Group III animals' ALT (79.56 ± 5.16), AST (151.76 ± 6.16), ALP (184.67 ± 10.12), GGT (68.24 ± 4.05), TBL (1.66 ± 0.082) (p < 0.05), and Group IV ALT (55.54 ± 4.35), AST (78.79 ± 4.88), ALP (81.96 ± 9.43), GGT (47.32 ± 2.95), TBL (0.74 ± 0.075) (p < 0.05). Group IV exhibited the most significant reduction in serum biochemical markers as compared to Group III (p < 0.05) and close to silymarin-treated Group V ALT (44.42 ± 3.15), AST (74.45 ± 5.75), ALP (67.32 ± 9.14), GGT (42.43 ± 2.54), TBL (0.634 ± 0.077). Gene expression indices and histoarchitecture were evaluated to demonstrate the potential of AAE. The bioactive fraction of Anogeissus acuminata was rich in phenolics and flavonoid content. GC−MS analysis identified gallic acid, palmitic acid, cis-10-heptadecenoic acid, 9-octadecenoic acid, epigallocatechin, 2,5-dihydroxyacetophenone, and catechin. Oral administration of AAE (100 and 200 mg/kg) lowered the elevated levels of the biochemical markers and interleukin, and enhanced the level of enzymatic antioxidant. It also downregulated the expression level of proapoptotic genes and upregulated the expression level of the antiapoptotic gene along with improved liver histopathology.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Silimarina , Terminalia , Animales , Antioxidantes/química , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Etanol , Fenoles/farmacología , Fenoles/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Hojas de la Planta/metabolismo , Ratas , Silimarina/farmacología , Silimarina/uso terapéutico , Terminalia/metabolismoRESUMEN
This work reports an eco-friendly synthesis of silver nanoparticles (AgNPs) using endophytic bacteria, Cytobacillus firmus isolated from the stem bark of Terminalia arjuna. The synthesis of AgNPs was confirmed by visual observation as a change in color of the bacterial solution impregnated with silver. Further, the morphology of the AgNPs, average size, and presence of elemental silver were characterized by UV-Visible spectroscopy, scanning electron microscopy, and dynamic light scattering spectroscopy. The roles of endophytic secondary metabolites in the metal reduction, stabilization, and capping of silver nanoparticles were studied by qualitative FTIR spectral peaks. The antimicrobial ability of AgNPs was evaluated against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria and pearl millet blast disease-causing fungi (Magnoporthe grisea). The biosynthesized AgNPs showed good antibacterial and antifungal activities. AgNPs effectively inhibited the bacterial growth in a dose-dependent manner and presented as good antifungal agents towards the growth of Magnoporthe grisea.
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Antiinfecciosos/farmacología , Bacillaceae/metabolismo , Tecnología Química Verde , Nanopartículas del Metal/química , Plata/química , Terminalia/metabolismo , Plaquetas/citología , Supervivencia Celular , Eritrocitos/citología , Escherichia coli , Hemólisis , Humanos , Luz , Microscopía Electrónica de Rastreo , Microscopía Fluorescente , Corteza de la Planta , Pyricularia grisea , ARN Ribosómico 16S/metabolismo , Dispersión de Radiación , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de Fourier , Staphylococcus aureus , Difracción de Rayos XRESUMEN
Terminalia sericea is used throughout Africa for the treatment of a variety of conditions and has been identified as a potential commercial plant. The study was aimed at establishing a high-performance thin layer chromatography (HPTLC) chemical fingerprint for T. sericea root bark as a reference for quality control and exploring chemical variation within the species using HPTLC metabo3lomics. Forty-two root bark samples were collected from ten populations in South Africa and extracted with dichloromethane: methanol (1:1). An HPTLC method was optimized to resolve the major compounds from other sample components. Dichloromethane: ethyl acetate: methanol: formic acid (90:10:30:1) was used as the developing solvent and the plates were visualized using 10% sulfuric acid in methanol as derivatizing agent. The concentrations of three major bioactive compounds, sericic acid, sericoside and resveratrol-3-O-ß-rutinoside, in the extracts were determined using a validated ultra-performance liquid chromatography-photodiode array (UPLC-PDA) detection method. The rTLC software (written in the R-programming language) was used to select the most informative retardation factor (Rf) ranges from the images of the analysed sample extracts. Further chemometric models, including principal component analysis (PCA) and hierarchical cluster analysis (HCA), were constructed using the web-based high throughput metabolomic software. The rTLC chemometric models were compared with the models previously obtained from ultra-performance liquid chromatography coupled with mass spectrometry (UPLC-MS). A characteristic fingerprint containing clear bands for the three bioactive compounds was established. All three bioactive compounds were present in all the samples, although their corresponding band intensities varied. The intensities correlated with the UPLC-PDA results, in that samples containing a high concentration of a particular compound, displayed a more intense band. Chemometric analysis using HCA revealed two chemotypes, and the subsequent construction of a loadings plot indicated that sericic acid and sericoside were responsible for the chemotypic variation; with sericoside concentrated in Chemotype 1, while sericic acid was more abundant in Chemotype 2. A characteristic chemical fingerprint with clearly distinguishable features was established for T. sericea root bark that can be used for species authentication, and to select samples with high concentrations of a particular marker compound(s). Different chemotypes, potentially differing in their therapeutic potency towards a particular target, could be distinguished. The models revealed the three analytes as biomarkers, corresponding to results reported for UPLC-MS profiling and thereby indicating that HPTLC is a suitable technique for the quality control of T. sericea root bark.
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Fitoquímicos/análisis , Fitoquímicos/metabolismo , Terminalia/química , Terminalia/metabolismo , Cromatografía Líquida de Alta Presión/métodos , Cromatografía en Capa Delgada/métodos , Metaboloma , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Control de Calidad , Sudáfrica , Terminalia/clasificaciónRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia catappa L. (West Indian-Almond) is a medicinal plant used in traditional medicine for the treatment of infectious diseases. Moreover, various organic extracts prepared from this plant have been reported to exhibit antiplasmodial activity. AIM OF THE STUDY: The need for new antimalarials is still an urgency driven by the alarmingly high burden of malaria in endemic regions, with multitude of people dying annually. We have previously identified an endophytic fungus Aspergillus niger 58 harboured by T. catappa as having promising specialized secondary metabolites against the malaria parasites. In the present study, we report the antiplasmodial activity-guided chromatographic isolation of some metabolites secreted by this endophytic fungus. MATERIALS AND METHODS: The SYBR Green I-based fluorescence microtiter plate assay was used to monitor the growth of Plasmodium falciparum parasites in culture in the presence and absence of inhibitors and results were validated by microscopic analysis of Giemsa-stained culture smears. Giemsa-stain microscopy was also used to study the cell cycle stage-specific action of selected fractions. RESULTS: The results revealed that the multidimensional purification of the crude extract (IC50: 4.03 µg/mL) provided RPHPLC F17 (IC50: 0.09 µg/mL) and RPHPLC F18 (IC50: 0.1 µg/mL) with activity against P. falciparum 3D7 (Pf3D7) strain. Moreover, both fractions at IC99 (0.5 µg/mL) exhibited multi-stages action by targeting all the three stages of the life cycle of blood-stage Pf3D7. Two compounds, flavasperone (1) and aurasperone A (2) were isolated, of which aurasperone A exhibited good potency against Pf3D7 (IC50: 4.17 µM) and P. falciparum INDO (PfINDO) (IC50: 3.08 µM). CONCLUSION: Our study adds credence to the notion that endophytic extracts are potential storehouses for potent specialized secondary metabolites that can be harnessed to fight the malaria parasite and reduce the burden of this disease worldwide. An endophyte that can be cultured in laboratory with ability to secrete promising metabolites of medicinal value holds the promise of conserving Nature from the threat of annihilation of flora for medicinal purposes.
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Antimaláricos/metabolismo , Antimaláricos/farmacología , Aspergillus niger/metabolismo , Plasmodium falciparum/efectos de los fármacos , Terminalia/metabolismo , Antimaláricos/aislamiento & purificación , Aspergillus niger/aislamiento & purificación , Células HEK293 , Humanos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacología , Plasmodium falciparum/fisiologíaRESUMEN
Ultrahigh-performance liquid chromatography quadrupole-time-of-flight mass spectrometry (UHPLC-QToF-MS) profiling was used for the identification of marker compounds and generation of metabolic patterns that could be interrogated using chemometric modeling software. UHPLC-QToF-MS was used to generate comprehensive fingerprints of three botanicals (Hoodia, Terminalia, and chamomile), each having different classes of compounds. Detection of a broad range of ions was carried out in full scan mode in both positive and negative modes over the range m/z 100-1700 using high-resolution mass spectrometry. Multivariate statistical analysis was used to extract relevant chemical information from the data to easily differentiate between Terminalia species, chamomile varieties, and quality control of Hoodia products. Using nontargeted analysis, identification of 37 compounds contributed to the differences between Terminalia species, 26 flavonoids were identified to show the differences between German and Roman chamomile, and 43 pregnane glycosides were identified from Hoodia gordonii samples. The UHPLC-QToF-MS-based chemical fingerprinting with principal component analysis was able to correctly distinguish botanicals and their commercial products. This work can be used as a basis to assure the quality of botanicals and commercial products.
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Manzanilla/metabolismo , Hoodia/metabolismo , Preparaciones de Plantas/normas , Terminalia/metabolismo , Manzanilla/química , Cromatografía Líquida de Alta Presión , Suplementos Dietéticos/normas , Hoodia/química , Espectrometría de Masas , Metaboloma , Metabolómica , Preparaciones de Plantas/química , Control de Calidad , Terminalia/químicaRESUMEN
Kidney stone formation during hyperoxaluric condition is inherently dependent on the interaction between renal epithelial cells and calcium oxalate (CaOx) crystals. Although modern medicine has progressed in terms of removal of these stones, recurrence and persistent side effects restricts their use. Strategies involving plant based agents which could be used as adjunct therapy is an area which needs to be explored. Plant proteins having antilithiatic activity is a hitherto unexplored area and therefore, we conducted a detailed identification and characterization of antilithiatic proteins from Terminalia arjuna (T. arjuna). Proteins were isolated from the dried bark of T. arjuna and those having molecular weights > 3 kDa were subjected to anion exchange chromatography followed by gel filtration chromatography. Four proteins were identified exhibiting inhibitory activity against CaOx crystallization and crystal growth kinetics The cytoprotective and anti-apoptotic efficacy of these purified proteins was further investigated on oxalate injured renal epithelial cells (MDCK and NRK-52E) wherein, injury due to oxalate was significantly attenuated and led to a dose dependent increase in viability of these cells. These proteins also prevented the interaction of the CaOx crystals to the cell surface and reduced the number of apoptotic cells. Identification of these 4 anionic proteins from the bark of T. arjuna was carried out by Matrix-assisted laser desorption/ionization-time of flight Mass spectrometry (MALDI-TOF MS). This was followed by database search with the MASCOT server and sequence similarity was found with Nuclear pore anchor, DEAD Box ATP-dependent RNA helicase 45, Lon protease homolog 1 and Heat shock protein 90-3. These novel proteins isolated from T. arjuna have the potential to inhibit CaOx crystallization and promote cell survival and therefore, offer novel avenues which need to be explored further for the medical management of urolithiasis.
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Corteza de la Planta/metabolismo , Proteínas de Plantas/metabolismo , Proteómica/métodos , Terminalia/metabolismo , Animales , Aniones , Apoptosis/efectos de los fármacos , Oxalato de Calcio/química , Oxalato de Calcio/metabolismo , Línea Celular , Cromatografía en Gel , Cromatografía por Intercambio Iónico , Cristalización , Perros , Células Epiteliales/citología , Células Epiteliales/efectos de los fármacos , Células Epiteliales/metabolismo , Túbulos Renales Colectores/citología , Células de Riñón Canino Madin Darby , Fitoterapia/métodos , Proteínas de Plantas/aislamiento & purificación , Proteínas de Plantas/farmacología , Ratas , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción , Urolitiasis/tratamiento farmacológicoRESUMEN
The objective of the present study was to assess the in vitro anticancer activity of 70% methanolic extract of Terminalia belerica (TBME) against human lung (A549) and human breast (MCF-7) carcinoma and its possible mechanism. TBME showed significant cytotoxicity to both A549 and MCF-7 cells, whereas, no cytotoxicity was found in non-malignant WI-38 cells. Flow cytometric analysis was then performed and 100 µg/ml of TBME was selected as the effective concentration inducing apoptosis in A549 and MCF-7. At this concentration, TBME caused DNA fragmentation pattern of apoptosis. Furthermore, mechanism of apoptosis induction was demonstrated using western blotting and Bax/Bcl-2 ratio in both types of the cells was found increased, which leads to the activation of caspase cascade along with the cleavage of PARP. These results suggested that TBME is able to induce anticancer effects on both lung and breast cancer cell lines through the modulation of Bcl-2 family proteins.
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Adenocarcinoma/tratamiento farmacológico , Apoptosis/efectos de los fármacos , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias Pulmonares/tratamiento farmacológico , Extractos Vegetales/farmacología , Terminalia/metabolismo , Adenocarcinoma del Pulmón , Caspasa 3/biosíntesis , Caspasa 3/metabolismo , Caspasa 8/biosíntesis , Caspasa 8/metabolismo , Caspasa 9/biosíntesis , Caspasa 9/metabolismo , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Fragmentación del ADN/efectos de los fármacos , Femenino , Humanos , Células MCF-7 , Poli(ADP-Ribosa) Polimerasas/metabolismo , Proteínas Proto-Oncogénicas c-bcl-2/biosíntesis , Proteínas Proto-Oncogénicas c-bcl-2/genética , Proteína X Asociada a bcl-2/biosíntesis , Proteína X Asociada a bcl-2/genéticaRESUMEN
CONTEXT: Subcutaneous mycoses are chronic infections caused by slow growing environmental fungi. Latin American plants are used in folk medicine to treat these afflictions. Moreover, the potential of the rich Latin American biodiversity for this purpose has not been fully explored. OBJECTIVES: The aim of the study was to screen Latin American plant extracts against two species of subcutaneous fungi: Sporothrix schenckii and Fonsecaea pedrosoi. MATERIALS AND METHODS: One hundred ninety-five organic extracts from 151 Latin American plants were screened against two subcutaneous fungi by the agar dilution method at a concentration of 100 µg/mL, and minimum inhibitory concentrations (MICs) of active extracts were determined. Positive (amphothericin B) and negative (50% ethanol) controls were used. RESULTS AND DISCUSSION: Twenty eight extracts showed activity at ≤100 µg/mL. Of these, four extracts from Gnaphalium gaudichaudianum DC (Asteraceae), Plumeria rubra L (Apocynaceae), Tecoma stans (L.) Juss. ex Kunth. (Bignoniaceae), and Trichostigma octandum (L.), H. Walter showed activity against F. pedrosoi at MIC 12.5 µg/mL; and, four extracts from Bourreria huanita (Lex.) Hemsl. (Boraginaceae), Phytolacca bogotensis Kunth (Phytolaccaceae), Monnina xalapensis Kunth (Polygalaceae) and Crataegus pubescens (C. Presl) C. Presl (Rosaceae) against S. schenckii. This is the first report on antifungal activity of the Latin American plants against these two subcutaneous fungi. CONCLUSION: S. schenkii and F. pedrosoi were inhibited by B. huanita (MIC: 12.5 and 25 µg/mL), G. gaudichaudianum (MIC: 50 and 12.5 µg/mL) and T. triflora (MIC: 25 µg/mL).
Asunto(s)
Antifúngicos/farmacología , Ascomicetos/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Micosis/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/farmacología , Sporothrix/efectos de los fármacos , Anfotericina B/farmacología , Antifúngicos/análisis , Antifúngicos/uso terapéutico , Etanol/farmacología , Hongos/efectos de los fármacos , Humanos , América Latina , Medicina Tradicional , Pruebas de Sensibilidad Microbiana , Hongos Mitospóricos/efectos de los fármacos , Extractos Vegetales/análisis , Extractos Vegetales/uso terapéutico , Terminalia/química , Terminalia/metabolismoRESUMEN
Five woody plants species (i.e. Terminalia arjuna, Prosopis juliflora, Populus alba, Eucalyptus tereticornis and Dendrocalamus strictus) were selected for phytoremediation and grow on tannery sludge dumps of Common Effluent Treatment Plant (CETP), Unnao (Uttar Pradesh), India. Concentration of toxic metals were observed high in the raw tannery sludge i.e. Fe-1667>Cr-628>Zn-592>Pb-427>Cu-354>Mn-210>Cd-125>Ni-76 mg kg(-1) dw, respectively. Besides, physico-chemical properties of the raw sludge represented the toxic nature to human health and may pose numerous risks to local environment. The growth performances of woody plants were assessed in terms of various growth parameters such as height, diameter at breast height (DBH) and canopy area of plants. All the plant species have the capabilities to accumulate substantial amount of toxic metals in their tissues during the remediation. The ratio of accumulated metals in the plants were found in the order Fe>Cr>Mn>Pb>Zn>Cu>Cd>Ni and significant changes in physico-chemical parameters of tannery sludge were observed after treatment. All the woody plants indicated high bioconcentration factor for different metals in the order Fe>Cr>Mn>Ni>Cd>Pb>Zn>Cu. After one year of phytoremediation, the level of toxic metals were removed from tannery sludge up to Cr (70.22)%, Ni (59.21)%, Cd (58.4)%, Fe (49.75)%, Mn (30.95)%, Zn (22.80)%, Cu (20.46)% and Pb (14.05)%, respectively.
Asunto(s)
Residuos Industriales/análisis , Magnoliopsida/metabolismo , Metales/metabolismo , Árboles/metabolismo , Contaminantes Químicos del Agua/metabolismo , Bambusa/crecimiento & desarrollo , Bambusa/metabolismo , Biodegradación Ambiental , Eucalyptus/crecimiento & desarrollo , Eucalyptus/metabolismo , Cinética , Magnoliopsida/crecimiento & desarrollo , Metales/análisis , Metales/química , Populus/crecimiento & desarrollo , Populus/metabolismo , Prosopis/crecimiento & desarrollo , Prosopis/metabolismo , Curtiembre , Terminalia/crecimiento & desarrollo , Terminalia/metabolismo , Árboles/crecimiento & desarrollo , Contaminantes Químicos del Agua/análisis , Contaminantes Químicos del Agua/químicaRESUMEN
An experiment was conducted to study the potential of chromium (Cr) phytoaccumulatory capabilities of four tree species viz., Anogeissus latifolia, Terminalia arjuna, Tecomella undulata, and Salvadora persica Possibility of enhancement of Cr uptake by citric acid and vesicular arbuscular mycorrhizal fungi (VAM) amendments were also tried. Cr is a major pollutant of the environment. Chromium can exist in oxidation states from III to VI, but the most stable and common forms of Cr are trivalent and hexavalent species. Cr(VI) was more toxic to the tree growth in terms of collar diameter (CD) increment in all the tree species than Cr(lll). Roots accumulated more Cr than shoots in all the tree species. There was more than 10 fold increase in root Cr content in comparison with shoot Cr content in all the trees at all the concentration of Cr and all sources of Cr. Citric acid significantly increased the Cr content in the tissues of roots in all the species under both speciation of Cr. The highest increase in Cr content brought by 20 mM citric acid addition was in A. latifolia Results suggest that Anogeissus latifolia is a potential Cr accumulator with citric acid as soil amendment.
Asunto(s)
Carcinógenos Ambientales/metabolismo , Cromo/metabolismo , Micorrizas/metabolismo , Plantones/metabolismo , Árboles/metabolismo , Ácido Cítrico/metabolismo , Ácido Cítrico/farmacología , Clima Desértico , India , Hojas de la Planta/metabolismo , Raíces de Plantas/metabolismo , Brotes de la Planta/metabolismo , Salvadoraceae/metabolismo , Salvadoraceae/microbiología , Especificidad de la Especie , Terminalia/metabolismo , Terminalia/microbiología , Árboles/microbiologíaRESUMEN
Effects of Aspergillus niger-fermented Terminalia catappa seed meal-based diet on the activities of alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST) and gamma-glutamate transferase (gamma-GT) in the crop, small intestine, gizzard, heart, liver and serum of broiler chicks were investigated. Milled T. catappa seed was inoculated with spores of A.niger (2.21 x 10(4) spores per ml) for 3 weeks. Forty-five day-old broiler chicks weighing between 27.62 and 36.21 g, were divided into three groups. The first group was fed soybean-based (control) diet; the second on raw T. catappa seed meal-based diet; and the third on A. niger-fermented T. catappa seed meal-based diet for 7 weeks. The results revealed a significantly increased (p<0.05) activity of ALP in the tissues. Contrarily, there were significant reductions (p<0.05) in the activities of ALP, ALT, AST and gamma-GT in the liver and heart of the broilers fed the raw T. catappa seed meal-based diet while there were significant increase (p<0.05) in the activities of these enzymes in the serum of the broilers in this group. The data obtained showed that A. niger-fermented T. catappa seed meal reduced the toxic effects of the raw seed meal on the tissues of broiler chicks.
Asunto(s)
Alimentación Animal , Aspergillus niger/metabolismo , Sistema Digestivo/efectos de los fármacos , Corazón/efectos de los fármacos , Semillas/efectos adversos , Terminalia/metabolismo , Animales , Pollos , Buche de las Aves/efectos de los fármacos , Buche de las Aves/enzimología , Sistema Digestivo/enzimología , Femenino , Fermentación , Tracto Gastrointestinal/efectos de los fármacos , Tracto Gastrointestinal/enzimología , Molleja de las Aves/efectos de los fármacos , Molleja de las Aves/enzimología , Hígado/efectos de los fármacos , Hígado/enzimología , Masculino , Miocardio/enzimología , Semillas/metabolismo , Semillas/microbiología , Terminalia/microbiologíaRESUMEN
Nine esters of a naturally occurring triterpenoid, arjunolic acid (from Terminalia arjuna), with alkyl chains have been synthesized, and their self-assembly has been studied in organic liquids. All of the esters examined were found to be excellent gelators. No birefringence was detected in optical micrographs of the transparent toluene gels with 5% (w/w) ethyl arjunolate or 5% (w/w) p-nitrobenzyl arjunolate as the gelator, but a spherulitic-type pattern was seen for a gel of 1.2% (w/w) p-nitrobenzyl arjunolate in 1/1 (w/w) chloroform/cyclohexane. Electron microscope images revealed self-assembled fibrillar network (SAFIN) structures with right-handed helical ribbons in some gels. With increasing concentration of the gelators, the gel-to-sol transition temperature (T(gel)) increased and then approached plateau values. Differential scanning thermograms demonstrated that the heats for transition from transparent gels to sols of ethyl arjunolate or p-nitrobenzyl ajunolate in toluene are very small. Powder X-ray diffractograms revealed that the molecular packing in the SAFIN of the 5% (w/w) ethyl aijunoate in the toluene gel was amorphous and similar to the diffractogram recorded for the neat gelator. Although the diffractogram of neat p-nitrobenzyl arjunolate consisted of broad peaks, suggesting disordered packing, the low-angle peaks of the corresponding toluene gel were much sharper; these results indicate more crystalline packing in the SAFIN than in the neat gelator. The kinetics and growth of the transformation of sols of p-nitrobenzyl arjunolate in 1/1 (w/w) chloroform/cyclohexane to their gels have been investigated at different incubation temperatures by circular dichroism spectroscopy. The data have been analyzed to probe the mechanism of SAFIN formation and the relationship between the molecular structures of the esters of arjunolic acid and their abilities to function as gelators of a wide variety of organic liquids.
Asunto(s)
Química/métodos , Geles , Triterpenos/química , Cloroformo/química , Dicroismo Circular , Ciclohexanos/química , Relación Dosis-Respuesta a Droga , Ésteres , Cinética , Microscopía Electrónica/métodos , Modelos Químicos , Propiedades de Superficie , Temperatura , Terminalia/metabolismo , Difracción de Rayos XRESUMEN
The present study was undertaken to investigate the effect of aqueous and ethanolic extracts of T. bellirica on depression in mice using forced swim test (FST) and tail suspension test (TST). The extracts were administered orally for 10 successive days in separate groups of Swiss young male albino mice. Aqueous extract (50, 100 and 200 mg/kg) in a dose-dependent manner and ethanolic extract (100 mg/kg) significantly reduced the immobility time of mice in both FST and TST. The extracts were without any significant effect on locomotor activity of mice. The efficacies of aqueous extract (200 mg/kg) and ethanolic extract (100 mg/kg) were found to be similar to that of imipramine (15 mg/kg, po) and fluoxetine (20 mg/kg, po) administered for 10 successive days. Both extracts reversed reserpine-induced extension of immobility period of mice in FST and TST. Prazosin (62.5 microg/kg, ip; an alpha1-adrenoceptor antagonist), sulpiride (50 mg/kg, ip; a selective D2 receptor antagonist) and p-chlorophenylalanine (100 mg/kg, ip; an inhibitor of serotonin synthesis) significantly attenuated the aqueous and ethanolic extract-induced antidepressant-like effect in TST. Thus, both the aqueous and ethanolic extracts of T. bellirica elicited a significant antidepressant-like effect in mice by interaction with adrenergic, dopaminergic and serotonergic systems.
Asunto(s)
Antidepresivos/farmacología , Conducta Animal/efectos de los fármacos , Extractos Vegetales/farmacología , Reserpina/farmacología , Terminalia/metabolismo , Animales , Química Farmacéutica/métodos , Depresión/tratamiento farmacológico , Evaluación Preclínica de Medicamentos , Etanol/química , Etanol/farmacología , Concentración de Iones de Hidrógeno , Masculino , Ratones , Reserpina/metabolismo , Natación , Agua/químicaRESUMEN
Coupled gas chromatography-electroantennogram detection (GC-EAD) analysis of volatiles from tropical almond fruit, Terminalia catappa L., revealed 22 compounds that were detected by antennae of oriental fruit fly females, Bactrocera dorsalis (Hendel). Both solid-phase microextraction (SPME) and Porapak Q were used for sampling odors in fruit headspace, with SPME collections producing larger EAD responses from a greater number of compounds. Geranyl acetate and methyl eugenol elicited the largest EAD responses. A synthetic blend containing SPME collected, EAD stimulatory compounds showed female-biased attraction in laboratory wind tunnel bioassays, but heavily male-biased trap captures in a larger olfactometer arena. A nine-component subset of compounds eliciting relatively small EAD responses (EAD minor) and consisting of equal parts ethanol, ethyl acetate, ethyl hexanoate, hexyl acetate, linalyl acetate, ethyl nonanate, nonyl acetate, ethyl cinnamate, and (E)-beta-farnesene, attracted mainly females. This EAD minor blend was as attractive to females and much less attractive to males when compared to torula yeast in field cage experiments using glass McPhail traps. Similar results were obtained with outdoor rotating olfactometer tests in which the EAD minor blend was almost completely inactive for males.