RESUMO
Objective To investigate the effect of Terminalia chebula water extract (TCWE) on the cellular immunity and PD-1/PD-L1 pathway in rats with collagen-induced arthritis (CIA). Methods SD rats were randomly divided into four groups: a control group, a CIA group, a TCWE group and a methotrexate (MTX) group, with 15 rats in each group. Except for the control group, SD rats in other groups were subcutaneously injected with type II collagen to establish the model of collagen-induced arthritis (CIA). The rats in the TCWE group were treated with 20 mg/(kg.d) TCWE and the rats in the MTX group were treated with 1.67 mg/(kg.d) MTX. After 14 days of treatment, the cartilage morphology was examined using hematoxylin-eosin (HE) staining, and splenic T lymphocyte apoptosis and Treg/Th17 cell ratio were detected by flow cytometry. The mRNA expressions of retinoid-related orphan nuclear receptor γt (RORγt), forkhead box P3 (FOXP3), PD-1 and PD-L1 in spleen were detected by reverse transcription PCR. The expression and localization of RORγt and FOXP3 were detected by immunohistochemical staining. The protein expressions of PD-1 and PD-L1 in splenic lymphocytes were detected by Western blot, and the levels of serum interleukin 17 (IL-17) and transforming growth factor ß (TGF-ß) in rats were detected by ELISA. Results Compared with CIA group, the pathological changes of cartilage and synovium were significantly alleviated in the TCWE group and the MTX group. Both the apoptosis rate of T lymphocytes in spleen and the ratio of Treg/Th17 cells increased. The expression of RORγt decreased, while the expressions of FOXP3, PD-1 and PD-L1 increased in spleen lymphocytes. The level of serum IL-17 decreased, while the level of serum TGF-ß increased. Conclusion TCWE treatment may activate PD-1/PD-L1 pathway in spleen cells to regulate cellular immunity, thus reducing cartilage injury in CIA rats.
Assuntos
Artrite Experimental , Antígeno B7-H1 , Receptor de Morte Celular Programada 1 , Ratos Sprague-Dawley , Baço , Terminalia , Animais , Artrite Experimental/imunologia , Artrite Experimental/tratamento farmacológico , Artrite Experimental/metabolismo , Baço/efeitos dos fármacos , Baço/imunologia , Baço/metabolismo , Antígeno B7-H1/genética , Antígeno B7-H1/metabolismo , Receptor de Morte Celular Programada 1/genética , Receptor de Morte Celular Programada 1/metabolismo , Ratos , Terminalia/química , Masculino , Imunidade Celular/efeitos dos fármacos , Regulação para Cima/efeitos dos fármacos , Extratos Vegetais/farmacologia , Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares/genética , Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares/metabolismo , Inflamação/tratamento farmacológico , Inflamação/imunologia , Inflamação/metabolismo , Linfócitos T Reguladores/imunologia , Linfócitos T Reguladores/efeitos dos fármacos , Linfócitos T Reguladores/metabolismo , Células Th17/imunologia , Células Th17/efeitos dos fármacos , Células Th17/metabolismoRESUMO
Alzheimer's disease (AD) and diabetes are non-communicable diseases with global impacts. Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are suitable therapies for AD, while α-amylase and α-glucosidase inhibitors are employed as antidiabetic agents. Compounds were isolated from the medicinal plant Terminalia macroptera and evaluated for their AChE, BChE, α-amylase, and α-glucosidase inhibitions. From 1H and 13C NMR data, the compounds were identified as 3,3'-di-O-methyl ellagic acid (1), 3,3',4'-tri-O-methyl ellagic acid-4-O-ß-D-xylopyranoside (2), 3,3',4'-tri-O-methyl ellagic acid-4-O-ß-D-glucopyranoside (3), 3,3'-di-O-methyl ellagic acid-4-O-ß-D-glucopyranoside (4), myricetin-3-O-rhamnoside (5), shikimic acid (6), arjungenin (7), terminolic acid (8), 24-deoxysericoside (9), arjunglucoside I (10), and chebuloside II (11). The derivatives of ellagic acid (1-4) showed moderate to good inhibition of cholinesterases, with the most potent being 3,3'-di-O-methyl ellagic acid, with IC50 values of 46.77 ± 0.90 µg/mL and 50.48 ± 1.10 µg/mL against AChE and BChE, respectively. The compounds exhibited potential inhibition of α-amylase and α-glucosidase, especially the phenolic compounds (1-5). Myricetin-3-O-rhamnoside had the highest α-amylase inhibition with an IC50 value of 65.17 ± 0.43 µg/mL compared to acarbose with an IC50 value of 32.25 ± 0.36 µg/mL. Two compounds, 3,3'-di-O-methyl ellagic acid (IC50 = 74.18 ± 0.29 µg/mL) and myricetin-3-O-rhamnoside (IC50 = 69.02 ± 0.65 µg/mL), were more active than the standard acarbose (IC50 = 87.70 ± 0.68 µg/mL) in the α-glucosidase assay. For α-glucosidase and α-amylase, the molecular docking results for 1-11 reveal that these compounds may fit well into the binding sites of the target enzymes, establishing stable complexes with negative binding energies in the range of -4.03 to -10.20 kcalmol-1. Though not all the compounds showed binding affinities with cholinesterases, some had negative binding energies, indicating that the inhibition was thermodynamically favorable.
Assuntos
Acetilcolinesterase , Inibidores da Colinesterase , Hipoglicemiantes , Simulação de Acoplamento Molecular , Extratos Vegetais , Terminalia , alfa-Amilases , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Acetilcolinesterase/metabolismo , Acetilcolinesterase/química , Terminalia/química , Humanos , Butirilcolinesterase/metabolismo , alfa-Glucosidases/metabolismo , alfa-Glucosidases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Estrutura MolecularRESUMO
Chebulae Fructus (CF) is known as one of the richest sources of hydrolyzable tannins (HTs). In this study, ultra-performance liquid chromatography coupled with a photodiode array detector method was established for simultaneous determination of the 12 common phenolcarboxylic and tannic constituents (PTCs). Using this method, quantitative analysis was accomplished in CF and other four adulterants, including Terminaliae Belliricae Fructus, Phyllanthi Fructus, Chebulae Fructus Immaturus, and Canarii Fructus. Based on a quantitative analysis of the focused compounds, discrimination of CF and other four adulterants was successfully accomplished by hierarchical cluster analysis and principal component analysis. Additionally, the total contents of the 12 compounds that we focused on in this study were unveiled as 148.86 mg/g, 96.14 mg/g, and 18.64 mg/g in exocarp, mesocarp, and endocarp and seed of CF, respectively, and PTCs were witnessed to be the most abundant in the exocarp of CF. Noticeably, the HTs (chebulagic acid, chebulanin acid, chebulinic acid, and punicalagin) were observed to be ultimately degraded to chebulic acid, gallic acid, and ellagic acid during sunlight-drying of the fresh fruits. As a result, our study indicated that CF and its adulterants could be distinguished by the observed 12 PTCs, which were mainly distributed in the exocarp of the fruits. The HTs were prone to degrade into the three simple phenolcarboxylic acids during drying or processing, allowing us to obtain a more comprehensive understanding of the PTCs, with great significance in the improved quality of CF and related products.
Assuntos
Frutas , Taninos Hidrolisáveis , Taninos Hidrolisáveis/química , Taninos Hidrolisáveis/análise , Frutas/química , Cromatografia Líquida de Alta Pressão , Terminalia/química , Taninos/análise , Taninos/química , Extratos Vegetais/química , Extratos Vegetais/análiseRESUMO
This study aims to explore the correlation between intestinal toxicity and composition changes of Euphorbia ebracteolata before and after Terminalia chebula soup(TCS) processing. Intragastric administration was performed on the whole animal model. By using fecal water content, inflammatory causes, and pathological damage of different parts of the intestinal tract of mice as indexes, the differences in intestinal toxicity of dichloromethane extraction of raw E. ebracteolata(REDE), dichloromethane extraction of TCS, and dichloromethane extraction of E. ebracteolata after simulated TCS processing(STREDE) were compared, so as to investigate the effect of TCS processing on the intestinal toxicity of E. ebracteolata. At the same time, the component databases of E. ebracteolata and T. chebula were constructed, and the composition changes of diterpenoids, tannins, and phenolic acids in the three extracted parts were analyzed by HPLC-TOF-MS. HPLC was used to compare the content of four diterpenoids including ent-11α-hydroxyabicta-8(14), 13(15)-dien-16, 12-olide(HAO), jolkinolide B(JNB), fischeria A(FA), and jolkinolide E(JNE) in the E. ebracteolata before and after processing and the residue of container wall after processing, so as to investigate the effect of TCS processing on the content and structure of the diterpenoids. The results showed that the REDE group could significantly increase the fecal water content and the release levels of TNF-α and IL-1ß from each intestinal segment, and intestinal tissue damage was accompanied by significant infiltration of inflammatory cells. However, compared with the REDE group, the intestinal tissue damage in the STREDE group was alleviated, and the infiltration of inflammatory cells decreased. The intestinal toxicity significantly decreased. Mass spectrometry analysis showed that there was no significant difference in the content of diterpenoids of REDE before and after simulated TCS processing, but a large number of tannins and phenolic acids were added. The results of HPLC showed that the content of four diterpenoids of E. ebracteo-lata decreased to varying degrees after TCS processing, ranging from-0.35% to-19.74%, and the decreased part mainly remained in the container wall, indicating that the structure of toxic diterpenoids of E. ebracteolata was not changed after TCS processing. The antagonistic effect of tannic and phenolic acids in the TCS may be the main reason for the reduced intestinal toxicity of E. ebracteolata after TCS processing. The TCS processing for E. ebracteolata is scientific.
Assuntos
Medicamentos de Ervas Chinesas , Euphorbia , Terminalia , Euphorbia/química , Animais , Terminalia/química , Camundongos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/toxicidade , Masculino , Intestinos/efeitos dos fármacos , Intestinos/química , Cromatografia Líquida de Alta Pressão , HumanosRESUMO
Chronic restraint stress induces cognitive abnormalities through changes in synapses and oxidant levels in the amygdala and hippocampus. Given the neuroprotective effects of fruit of Terminalia chebula (Halileh) in different experimental models, the present investigation aimed to address whether Terminalia chebula is able to reduce chronic restraint stress-induced behavioral, synaptic and oxidant markers in the rat model. Thirty-two male Wistar rats were randomly divided into four groups as follows: control (did not receive any treatment and were not exposed to stress), stress (restraint stress for 2â¯h a day for 14 consecutive days), Terminalia chebula (received 200â¯mg/kg hydroalcoholic extract of Terminalia chebula), and stress + Terminalia chebula groups (received 200â¯mg/kg extract of Terminalia chebula twenty minutes before stress) (n = 8 in each group). We used the shuttle box test to assess learning and memory, Golgi-Cox staining to examine dendritic spine density in the dentate gyrus region of the hippocampus and the basolateral and central nuclei of the amygdala, and total antioxidant capacity (TAC) and total oxidant status (TOS) in the brain. The shuttle box test results demonstrated that Terminalia chebula treatment had a profound positive effect on memory parameters, including step-through latency (STL) and time spent in the dark room, when compared to the stress group. Daily oral treatment with Terminalia chebula effectively suppressed the loss of neural spine density in the dentate gyrus region of the hippocampus and the basolateral and central nuclei of the amygdala caused by chronic restraint stress, as demonstrated by Golgi-Cox staining. Additionally, the results indicate that Terminalia chebula significantly reduced the TOS and increased TAC in the brain compared to the stress group. In conclusion, our results suggest that Terminalia chebula improved memory impairment and synaptic loss in the dentate gyrus of the hippocampus and the basolateral and central nuclei of the amygdala induced by restraint stress via inhibiting oxidative damage.
Assuntos
Giro Denteado , Transtornos da Memória , Estresse Oxidativo , Extratos Vegetais , Ratos Wistar , Restrição Física , Estresse Psicológico , Terminalia , Animais , Terminalia/química , Masculino , Estresse Psicológico/metabolismo , Ratos , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/fisiologia , Giro Denteado/metabolismo , Extratos Vegetais/farmacologia , Sinapses/efeitos dos fármacos , Sinapses/metabolismo , Sinapses/patologia , Hipocampo/metabolismo , Hipocampo/patologia , Hipocampo/efeitos dos fármacos , Complexo Nuclear Basolateral da Amígdala/metabolismo , Complexo Nuclear Basolateral da Amígdala/efeitos dos fármacos , Núcleo Central da Amígdala/metabolismo , Núcleo Central da Amígdala/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Espinhas Dendríticas/efeitos dos fármacos , Tonsila do Cerebelo/metabolismoRESUMO
Malaria is a mosquito-borne infectious disease that is caused by the Plasmodium parasite. Most of the available medication are losing their efficacy. Therefore, it is crucial to create fresh leads to combat malaria. Green silver nanoparticles (AgNPs) have recently attracted a lot of attention in biomedical research. As a result, green mediated AgNPs from leaves of Terminalia bellirica, a medicinal plant with purported antimalarial effects, were used in this investigation. Initially, cysteine-rich proteins from Plasmodium species were studied in silico as potential therapeutic targets. With docking scores between -9.93 and -11.25 kcal/mol, four leaf constituents of Terminalia bellirica were identified. The green mediated silver nanoparticles were afterward produced using leaf extract and were further examined using UV-vis spectrophotometer, DLS, Zeta potential, FTIR, XRD, and FESEM. The size of synthesized TBL-AgNPs was validated by the FESEM results; the average size of TBL-AgNPs was around 44.05 nm. The zeta potential study also supported green mediated AgNPs stability. Additionally, Plasmodium falciparum (3D7) cultures were used to assess the antimalarial efficacy, and green mediated AgNPs could effectively inhibit the parasitized red blood cells (pRBCs). In conclusion, this novel class of AgNPs may be used as a potential therapeutic replacement for the treatment of malaria.
Assuntos
Antimaláricos , Química Verde , Nanopartículas Metálicas , Extratos Vegetais , Folhas de Planta , Plasmodium falciparum , Prata , Terminalia , Prata/química , Prata/farmacologia , Antimaláricos/química , Antimaláricos/farmacologia , Antimaláricos/síntese química , Nanopartículas Metálicas/química , Terminalia/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plasmodium falciparum/efeitos dos fármacos , Simulação de Acoplamento Molecular , HumanosRESUMO
BACKGROUND: A study carried out by World Health Organization revealed that around 80% of individuals globally depends on herbal forms of medication with 40% of pharmaceutical products being sourced from medicinal plants. The study objective was to evaluate the phytochemicals composition, in vitro antimicrobial and antioxidant properties of the leaves of Terminalia catappa L. aqueous and methanolic extracts. METHODS: Antimicrobial activity was analyzed by disk diffusion, the minimum inhibitory concentration in-vitro assays with ciprofloxacin as the standard for antibacterial assay while nystatin for antifungal assay. Ferric reducing antioxidant power and 2,2-diphenyl-1-picryl-hydrazyl-hydrate assays were used for the evaluation of antioxidant properties of the crude extracts while the groups responsible for this activity identified using Fourier transform infrared spectrophotometer. RESULTS: The study found that the leaves of Terminalia catappa contained alkaloids, tannins, steroids, cardiac glycosides, flavonoids, phenols, saponins, and coumarins, but terpenoids were absent. Presence of functional groups associated with this class of compounds such as OH vibrational frequencies were observed in IR spectrum of the crude extracts. Methanolic extract from Terminalia catappa exhibited greater antibacterial properties against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus, whereas aqueous extract displayed greater antibacterial activity against Bacillus subtilis for all concentrations tested. The amount of the sample that scavenged 50 percent of DPPH (IC50) was found to be 8.723, 13.42 and 13.04 µg/mL for L-ascorbic acid, Terminalia catappa L. methanolic and aqueous extracts respectively. The antimicrobial and antioxidant activities varied with the extract concentration and solvent used in extractions. CONCLUSION: Terminalia catappa L. leaves are prospective for use as a source of therapeutic agents that could lead to the advancement of new antimicrobial and antioxidant products.
Assuntos
Anti-Infecciosos , Terminalia , Humanos , Antioxidantes/química , Metanol , Terminalia/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Estudos Prospectivos , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , ÁguaRESUMO
Plants have a history of being employed in managing breast cancer. However, no scientific evidence supports the idea that these plants can effectively reduce the level of HER2 expression. In this study, extracts from 10 medicinal plants were evaluated for their anticancer properties against HER2-positive breast cancer cells through various methods, including the SRB assay, comet assay, annexin V-FITC dual staining, and immunoblotting. All extracts exerted antiproliferative activity against HER2-positive breast cancer cells. Furthermore, Terminalia chebula (T. chebula), Berberis aristata (B. aristata), and Mucuna pruriens (M. pruriens) reduced HER2 expression in tested cell lines. In addition, an increased Bax/Bcl-2 ratio was observed after the treatment. A comparative proteomics study showed modulation in the proteome profile of breast cancer cells after treatment with T. chebula, B. aristata, Punica granatum, M. pruriens, and Acorus calamus. Metabolic profiling of lead plants revealed the existence of multiple anticancer compounds. Our study demonstrates the considerable potential of the mentioned plants as innovative therapies for HER2-positive breast cancer.
Assuntos
Neoplasias da Mama , Proliferação de Células , Regulação para Baixo , Extratos Vegetais , Plantas Medicinais , Receptor ErbB-2 , Humanos , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Neoplasias da Mama/genética , Receptor ErbB-2/metabolismo , Receptor ErbB-2/genética , Plantas Medicinais/química , Feminino , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Linhagem Celular Tumoral , Regulação para Baixo/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Terminalia/química , Mucuna/químicaRESUMO
Based on their high antioxidant capacity and noteworthy phytochemistry, Terminalia ferdinandiana fruit and leaves have attracted considerable recent interest for their therapeutic potential. Whilst those studies have reported a variety of therapeutic properties for the fruit, the anti-inflammatory potential of T. ferdinandiana has been largely neglected and the leaves have been almost completely ignored. This study investigated the immune-modulatory and anti-inflammatory properties of T. ferdinandiana fruit and leaf extracts by evaluating their inhibition of multiple pro- and anti-inflammatory cytokines and chemokines secretion in lipopolysaccharide (LPS)-stimulated and unstimulated RAW 264.7 macrophages using multiplex bead immunoassays and ELISA assays. The methanolic extracts were particularly good immune-modulators, significantly inhibiting the secretion of all the cytokines and chemokines tested. Indeed, the methanolic extracts completely inhibited IL-10, IFN-γ, IL-1ß, IL-6, MCP-1, and MIP-2a secretion, and almost completely inhibited the secretion of TNF-α. In addition, the methanolic T. ferdinandiana extracts also significantly inhibited cytosolic COX-2 levels (by 87-95%) and the synthesis of the PGE2 (by ~ 98%). In contrast, the methanolic extracts stimulated LTB4 secretion by ~ 60-90%, whilst the aqueous extracts significantly inhibited LTB4 secretion (by ~ 27% each). Exposure of RAW 264.7 cells to the methanolic T. ferdinandiana extracts also significantly down-regulated the cytosolic levels of NF-κB by 33-44%, indicating that the immune-modulatory and anti-inflammatory properties of the extracts may be regulated via a decrease in NF-κB transcription pathways. Taken together, these results demonstrate potent anti-inflammatory properties for the extracts and provide insights into their anti-inflammatory mechanisms.
Assuntos
Anti-Inflamatórios , Ciclo-Oxigenase 2 , Citocinas , Dinoprostona , Regulação para Baixo , NF-kappa B , Extratos Vegetais , Folhas de Planta , Terminalia , Camundongos , Animais , NF-kappa B/metabolismo , Células RAW 264.7 , Extratos Vegetais/farmacologia , Dinoprostona/metabolismo , Citocinas/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Terminalia/química , Regulação para Baixo/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Folhas de Planta/química , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Lipopolissacarídeos/farmacologia , Frutas/químicaRESUMO
1,3,6-Trigalloylglucose is a natural compound that can be extracted from the aqueous extracts of ripe fruit of Terminalia chebula Retz, commonly known as "Haritaki". The potential anti-Helicobacter pylori (HP) activity of this compound has not been extensively studied or confirmed in scientific research. This compound was isolated using a semi-preparative liquid chromatography (LC) system and identified through Ultra-high-performance liquid chromatography-MS/MS (UPLC-MS/MS) and Nuclear Magnetic Resonance (NMR). Its role was evaluated using Minimum inhibitory concentration (MIC) assay and minimum bactericidal concentration (MBC) assay, scanning electron microscope (SEM), inhibiting kinetics curves, urea fast test, Cell Counting Kit-8 (CCK-8) assay, Western blot, and Griess Reagent System. Results showed that this compound effectively inhibits the growth of HP strain ATCC 700392, damages the HP structure, and suppresses the Cytotoxin-associated gene A (Cag A) protein, a crucial factor in HP infection. Importantly, it exhibits selective antimicrobial activity without impacting normal epithelial cells GES-1. In vitro studies have revealed that 1,3,6-Trigalloylglucose acts as an anti-adhesive agent, disrupting the adhesion of HP to host cells, a critical step in HP infection. These findings underscore the potential of 1,3,6-Trigalloylglucose as a targeted therapeutic agent against HP infections.
Assuntos
Helicobacter pylori , Terminalia , Extratos Vegetais/química , Terminalia/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , ÁguaRESUMO
Terminalia canescens DC. Radlk. (family: Combretaceae) is native to northern Australia. Species of the genus Terminalia are widely used as traditional medicines to treat diverse ailments, including bacterial infections. However, we were unable to find any studies that had examined the antimicrobial activity of T. canescens. In this study, T. canescens was screened against a panel of bacterial pathogens, including multi-antibiotic-resistant strains. Solvents with different polarities were used to extract different complements of phytochemicals from T. canescens leaves. Methanolic and aqueous extracts exhibited substantial antimicrobial activity against various pathogens, including those that are multidrug-resistant strains. When combined with some selected clinical antibiotics, some extracts potentiated the antibacterial inhibitory activity. This study identified two synergistic, eleven additive, eleven non-interactive and eight antagonistic interactions. The toxicities of the plant extracts were examined in the Artemia franciscana nauplii assay and were found to be non-toxic, except the aqueous extract, which showed toxicity. Metabolomic liquid chromatography-mass spectrometry (LC-MS) analyses highlighted and identified several flavonoids, including vitexin, quercetin, orientin and kaempferol, as well as the tannins ellagic acid and pyrogallol, which may contribute to the antibacterial activities observed herein. The possible mechanism of action of these extracts was further explored in this study.
Assuntos
Antibacterianos , Terminalia , Antibacterianos/farmacologia , Terminalia/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Bactérias , beta-Lactamas , Testes de Sensibilidade MicrobianaRESUMO
Diabetes mellitus (DM) is a chronic and progressive metabolic disorder that can stimulate neuroinflammation and increase oxidative stress in the brain. Therefore, the present study was aimed to assess the efficacy of ethanolic Terminalia chebula extract against the neurochemical and histopathological changes induced in the brains of diabetic rats. The study clarified the reduction in oxidative stress induced in the brains of diabetic rats by the significant (P ≤ 0.05) increase in levels of the antioxidants with decreasing the peroxidation products via ethanolic T. chebula extract at both doses (400 and 600 mg/kg). Moreover, T. chebula extract improved the brain integrity by lowering levels of interleukin-1ß (IL-1ß), tumor necrosis factor-α (TNF-α), ß-amyloid (Aß) content, monocyte chemoattractant protein-1 (MCP-1) and acetylcholine esterase (ACHE) significantly (P ≤ 0.05) in a dose dependent manner compared to brain of diabetic rats. Severe nuclear pyknosis and degeneration were noticed in neurons of the cerebral cortex, hippocampus and striatum in brains of diabetic rats. The severity of these alterations decreased with T. chebula extract at a dose of 600 mg/kg compared to the other treated groups. The different electrophoretic protein and isoenzyme assays revealed that the lowest similarity index (SI%) values exist in the brains of diabetic rats compared to the control group. The quantity of the most native proteins and isoenzyme types increased significantly (P ≤ 0.05) in the brains of diabetic rats, and these electrophoretic variations were completely diminished by T. chebula extract. The study concluded that T. chebula extract ameliorated the biochemical, histopathological and electrophoretic abnormalities induced in the brains of diabetic rats when administered at a dose of 600 mg/kg.
Assuntos
Diabetes Mellitus Experimental , Terminalia , Ratos , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Isoenzimas , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Terminalia/química , Encéfalo , Epigênese Genética , FrutasRESUMO
Terminalia bellirica (T. bellirica) (Gaertn.) Roxb. is a well-known traditional medicinal plants that show promising treatment because of fewer side effects in humans. In the present study, the total phenol, flavonoid, condensed and hydrolyzable tannins extracted and analyzed from cold macerated (CM) T. bellirica (Gaertn.) Roxb. fruit (TBF) and leaves (TBL) extract with the identification of bioactive compounds using GC-MS/MS technique. The highest amount of bioactive content was found in ethanolic extract than toluene. Current experimental data of TBF extract shows the maximum and significant biological activity like free radical scavenging activity against DPPH and FRAP assays with IC50 values of 51.07 ± 0.52 µg/ml and 63.14 ± 0.59 µg/ml respectively. However, IC50 cytotoxicity values of TBF extract on MCF-7 cells for 24 hrs was found to be 6.34 ± 0.72 µg/ml. Minimum inhibitory concentration (MIC) for infectious pathogens Escherichia coli and Bacillus cereus was >12.5 µg/ml and >100 µg/ml respectively, however, anti-inflammatory activity was demonstrated as an IC50 value of 509.1 ± 1.72 µg/ml. Cold macerated fruit extract revealed threatening inhibitory potential against the α-amylase and α-glucosidase enzymes, with IC50 of 50.98 ± 0.23 µg/ml and 46.70 ± 1.38 µg/ml respectively. Finally, the outcome of this study showed that T. bellirica (Gaertn.) Roxb. fruit extract could be an effective source of bioactives with efficient biomedical properties.
Assuntos
Frutas , Extratos Vegetais , Terminalia , Terminalia/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Frutas/química , Humanos , Células MCF-7 , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Antibacterianos/farmacologia , Antibacterianos/isolamento & purificação , Antibacterianos/química , Testes de Sensibilidade Microbiana , Escherichia coli/efeitos dos fármacos , Bacillus cereus/efeitos dos fármacos , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/química , Folhas de Planta/química , Temperatura BaixaRESUMO
ABSTRACT BACKGROUND Leathery Murdah, Terminalia coriacea (Roxb.) Wight & Arn. from family Combretaceae is used in Ayurveda and Siddha traditional systems of medicine to heal ulcers. OBJECTIVE The present study was conducted to assess the gastroprotective effect and understand the fundamental mechanism of action of Leathery Murdah, Terminalia coriacea (Roxb.) Wight & Arn. Leaf Methanolic Extract. METHODS The test extract was screened for anti-ulcer activity by Aspirin induced ulcerogenesis in pyloric ligation and ethanol induced gastric ulcers at three doses - 125, 250, and 500 mg/kg, p.o. using Ranitidine 50 mg/kg and Misoprostol 100 μg/kg as standard drug in respective models. Seven parameters were carefully examined, that is, ulcer index, total protein, mucin, catalase, malondialdehyde, and superoxide dismutase levels and histopathology. High Performance Liquid Chromatographic - Ultra Violet profiling and Liquid Chromatography - Mass Spectral analysis of crude Terminalia coriacea leaves methanolic extract were carried out as a part of chemical characterization to identify bioactive compounds. RESULTS All the test doses exhibited significant gastroprotective function, particularly the higher doses demonstrated improved action. The results revealed a significant increase in the levels of catalase, superoxide dismutase, and Mucin with reduction in ulcer index, the levels of total protein, and malondialdehyde. Histopathological observations also illustrated the gastroprotective effect of Terminalia coriacea leaves methanolic extract. CONCLUSION Terminalia coriacea leaves methanolic extract exhibited strong anti-oxidant and anti-secretory activities mediated gastroprotection besides inducing the gastric mucosal production. The observed pharmacological response can be attributed to the flavonoidal compounds namely - Quercetin-3-O-rutinoside, Luteolin-7-O-glucoside, Myricetin hexoside, Quercetin-3-O-glucoside, Isorhamnetin-3-O-rhamnosylglucoside and Isorhamnetin-3-O-glucoside identified in the extract for the first time with High Performance Liquid Chromatographic - Ultra Violet and Liquid Chromatography - Mass Spectral analysis.
RESUMO CONTEXTO Leathery Murdah, Terminalia coriacea (Roxb.) Wight & Arn. da família Combretaceae é usada nos tradicionais sistemas da medicina Ayurveda e Siddha para cicatrização de úlceras. OBJETIVOS O presente estudo foi realizado para avaliar o efeito gastroprotetor e para esclarecer o mecanismo fundamental da ação do extrato metanólico de folhas de Leathery Murdah, Terminalia coracea (Roxb.) Wight & Arn. MÉTODOS O extrato teste foi testado para ação antiulcerogênica induzida pela Aspirina através da ligação pilórica e úlceras gástricas induzidas por etanol em três doses - 125, 250 e 500 mg/kg, via oral, utilizando-se Ranitidina 50 mg/kg e Misoprostol 100 μg/kg como drogas padrão nos respectivos modelos. Sete parâmetros foram cuidadosamente analisados tais como índice ulcerogênico, níveis de proteínas totais, de mucina, de catalase, de malondialdeído e de superoxido dismutase, além da histopatologia. A análise do perfil espectroscópico pela Cromatografia Líquida de Alta Eficiência - Ultravioleta e análise crua pela Cromatografia Líquida - Espectrometria de Massas foram realizadas como parte da caracterização química para identificar os componentes bioativos. RESULTADOS Todas as doses utilizadas exibiram função gastroprotetora, em particular as doses mais elevadas. Os testes revelaram aumentos significantes de catalase, superóxido dismutase e mucina, com diminuição do índice ulcerogênico, dos níveis de proteínas totais, e de malondialdeído. As observações histopatológicas também ilustraram o efeito gastroprotetor do extrato metanólico de folhas de Terminalia coracea. CONCLUSÃO O extrato metanólico de folhas de Terminalia coracea mostrou forte atividade antioxidante e antissecretória além de induzir a produção de mucosa gástrica. A resposta farmacológica observada pode ser atribuída aos compostos flavonoides denominados Quercetin-3-O-rutinosideo, Luteolin-7-O-glucosideo, Myricetin hexosideo, Quercetin-3-O-glucosideo, Isorhamnetin-3-O-rhamnosylglucosideo e Isorhamnetin-3-O-glucosideo, identificados no extrato pela primeira vez pelas análises de Cromatografia Líquida de Alta Eficiência - Ultravioleta e Cromatografia Líquida - Espectrometria de Massas.
Assuntos
Animais , Masculino , Ratos , Úlcera Gástrica/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Terminalia/química , Antiulcerosos/administração & dosagem , Úlcera Gástrica/induzido quimicamente , Anti-Inflamatórios não Esteroides , Aspirina , Ratos Wistar , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Mucosa Gástrica/efeitos dos fármacosRESUMO
ABSTRACT Purpose: For most cases, urolithiasis is a condition where excessive oxalate is present in the urine. Many reports have documented free radical generation followed by hyperoxaluria as a consequence of which calcium oxalate (CaOx) deposition occurs in the kidney tissue. The present study is aimed to exam the antilithiatic potency of the aqueous extract (AE) of Terminalia arjuna (T. arjuna). Materials and Methods: The antilithiatic activity of Terminalia arjuna was investigated in vitro nucleation, aggregation and growth of the CaOx crystals as well as the morphology of CaOx crystals using the inbuilt software ‘Image-Pro Plus 7.0’ of Olympus upright microscope (BX53). Antioxidant activity of AE of Terminalia arjuna bark was also determined in vitro. Results: Terminalia arjuna extract exhibited a concentration dependent inhibition of nucleation and aggregation of CaOx crystals. The AE of Terminalia arjuna bark also inhibited the growth of CaOx crystals. At the same time, the AE also modified the morphology of CaOx crystals from hexagonal to spherical shape with increasing concentrations of AE and reduced the dimensions such as area, perimeter, length and width of CaOx crystals in a dose dependent manner. Also, the Terminalia arjuna AE scavenged the DPPH (2, 2-diphenyl-1-picrylhydrazyl) radicals with an IC50 at 13.1µg/mL. Conclusions: The study suggests that Terminalia arjuna bark has the potential to scavenge DPPH radicals and inhibit CaOx crystallization in vitro. In the light of these studies, Terminalia arjuna can be regarded as a promising candidate from natural plant sources of antilithiatic and antioxidant activity with high value.
Assuntos
Antioxidantes/farmacologia , Oxalato de Cálcio/química , Extratos Vegetais/farmacologia , Terminalia/química , Cálculos Urinários/prevenção & controle , Análise de Variância , Compostos de Bifenilo/química , Cristalização , Sequestradores de Radicais Livres/farmacologia , Fitoterapia , Picratos/química , Valores de Referência , Reprodutibilidade dos Testes , Cálculos Urinários/químicaRESUMO
PURPOSE: Kidney stone is one of the most prevalent diseases worldwide. Calcium oxalate (CaOx) has been shown to be the main component of the majority of stones formed in the urinary system of the patients with urolithiasis. The present study evaluates the antilithiatic properties of Terminalia chebula commonly called as "harad" which is often used in ayurveda to treat various urinary diseases including kidney stones. MATERIALS AND METHODS: The antilithiatic activity of Terminalia chebula was investigated on nucleation and growth of the calcium oxalate crystals. The protective potency of the plant extract was also tested on oxalate induced cell injury of both NRK-52E and MDCK renal epithelial cells. RESULTS: The percentage inhibition of CaOx nucleation was found 95.84% at 25µg/mL of Terminalia chebula aqueous extract which remained almost constant with the increasing concentration of the plant extract; however, plant extract inhibited CaOx crystal growth in a dose dependent pattern. When MDCK and NRK-52E cells were injured by exposure to oxalate for 48 hours, the aqueous extract prevented the injury in a dose-dependent manner. On treatment with the different concentrations of the plant extract, the cell viability increased and lactate dehydrogenase release decreased in a concentration dependent manner. CONCLUSION: Our study indicates that Terminalia chebula is a potential candidate for phytotherapy against urolithiasis as it not only has a potential to inhibit nucleation and the growth of the CaOx crystals but also has a cytoprotective role.
Assuntos
Oxalato de Cálcio/síntese química , Cálculos Renais/induzido quimicamente , Fitoterapia , Extratos Vegetais/farmacologia , Terminalia/química , Análise de Variância , Sobrevivência Celular , Citoproteção , Relação Dose-Resposta a Droga , Células Epiteliais/efeitos dos fármacos , Cálculos Renais/tratamento farmacológico , Rim/citologia , Modelos Biológicos , Extratos Vegetais/uso terapêuticoRESUMO
Infecções de ouvido representam uma das doenças mais comuns do mundo. Diferentes agentes etiológicos são responsáveis por tais infecções. OBJETIVO: Avaliar o potencial antimicrobiano de extratos de folhas e da casca de Terminalia arjuna contra Staphylococcus aureus, Acinetobacter sp., Proteus mirabilis, Escherchia coli, Pseudomonas aeruginosa e Candida albicans - patógenos que causam infecções de ouvido e como esses extratos se comparam às medicações tópicas atualmente disponíveis. MATERIAIS E MÉTODOS: Metanol, etanol, acetona, extratos aquosos (quentes e frios) de folhas e casca da T. arjuna foram testados para avaliação de suas atividades antimicrobianas. RESULTADOS: Dos três solventes orgânicos avaliados, o extrato acetônico das folhas foi o que teve o melhor resultado contra S. aureus. O extrato orgânico da casca exibiu quase o mesmo grau de ação antimicrobiana entre todas as bactérias gram-negativas, exceto contra P. aeruginosa. Entretanto, o extrato aquoso da casca de T. arjuna exibiu boa atividade contra S. aureus. Nenhum dos extratos exibiu atividade antifúngica. CONCLUSÃO: O extrato orgânico obtido a partir da casca e folhas de T. arjuna pode ser usado para tratar infecções bacterianas de ouvido, especialmente aquelas causadas por S. aureus, que exibiu maiores zonas de inibição do que gotas herbáceas; entretanto, ainda necessitamos de estudos mais detalhados - como ensaios in vivo e avaliações de propriedades farmacocinéticas para avaliarmos sua utilidade terapêutica no tratamento de infecções de ouvido.
Ear infection is one of the common diseases occurring throughout the world. Different etiological agents are responsible for ear infections. AIM: To assess the antimicrobial potential of Terminalia arjuna leaves and bark extracts against Staphylococcus aureus, Acinetobacter sp., Proteus mirabilis, Escherchia coli, Pseudomonas aeruginosa and Candida albicans, pathogens causing ear infections and their comparison with locally available ear drops. MATERIALS AND METHODS: Methanol, ethanol, acetone, aqueous (hot and cold) extracts from the leaves and bark of T. arjuna were tested for their antimicrobial activity. RESULTS: Of the three organic solvents evaluated, acetonic leaf extract was found to be best against S. aureus. Organic bark extract showed almost equal inhibition of all tested Gram negative bacteria except P. aeruginosa. However, aqueous extract of T. arjuna bark exhibited good activity against S. aureus. All the extracts were unable to exhibit any antifungal activity. CONCLUSION: Organic extract obtained from the T. arjuna bark and leaves may be used to treat the bacterial ear pathogens especially S. aureus, which has shown greater inhibition zones than the herbal drops, however, we still need more detailed studies as in vivo testing and pharmacokinetics properties for their therapeutic utility in treating ear infections.
Assuntos
Humanos , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Terminalia/química , Bactérias Gram-Negativas/genética , Bactérias Gram-Positivas/genética , Testes de Sensibilidade Microbiana , Dados de Sequência Molecular , Otite/microbiologiaRESUMO
Methanolic extracts of different parts of five medicinal plants, Ferula assafoetidaL. resin, Grewia asiaticaL. leaves, Ipomoea hederaceaJacq. seeds, Lepidium sativumL. seeds and Terminalia chebulaRetz. fruits were tested in vitrofor their cytotoxic, phytotoxic, insecticidal, nematicidal and anthelmintic activities. Ipomoea hederaceashowed very significant phytotoxic and cytotoxic activity, with 100% inhibition of Lemna minorgrowth and 100% death of Artemia salinaat concentrations of 1000 and 100 µg mL-1. Grewia asiaticaexhibited very weak activities while Lepidium sativumand Ferula assafoetidashowed moderate to good potential in all three bioassays. The results suggest screening of Ipomoea hederaceaseeds further for isolation of bioactive compounds that may be responsible for its toxic potential.