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A surge in the number of anthropogenic pollutants has been caused by increasing industrial activities. Nanoplastics are spotlighted as a new aquatic pollutant that are a threat to microbes and larger organisms. Our previous study showed that the subinhibitory concentrations of aquatic pollutants such as phenol and formalin act as signaling molecules and modulate global gene expression and metabolism. In this study, we aimed to investigate the impact of a new type of anthropogenic contaminant, polystyrene (PS) nanoplastics, on the expression of key virulence factors in zoonotic pathogen Edwardsiella piscicida and the assessment of potential changes in the susceptibility of zebrafish as a model host. The TEM data indicated a noticeable change in the cell membrane indicating that PS particles were possibly entering the bacterial cells. Transcriptome analyses performed to identify the differentially expressed genes upon PS exposure revealed that the genes involved in major virulence factor type VI secretion system (T6SS) were down-regulated. However, the expression of T6SS-related genes was recovered from the PS adapted E. piscicida when nanoplastics are free. This demonstrated the hypervirulence of pathogen in infection assays with both cell lines and in vivo zebrafish model. Therefore, this study provides experimental evidence elucidating the direct regulatory impact of nanoplastics influx into aquatic ecosystems on fish pathogenic bacteria, notably influencing the expression of virulence factors.
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Edwardsiella , Contaminantes Ambientales , Enfermedades de los Peces , Animales , Virulencia/genética , Pez Cebra/genética , Pez Cebra/metabolismo , Microplásticos/toxicidad , Poliestirenos/toxicidad , Ecosistema , Factores de Virulencia/genética , Expresión Génica , Proteínas Bacterianas/metabolismoRESUMEN
We report herein the design and synthesis of a series of novel acridine-triazole and acridine-thiadiazole derivatives. The newly synthesized compounds and the key intermediates were all evaluated for their antitumor activities against human foreskin fibroblasts (HFF), human gastric cancer cells-803 (MGC-803), hepatocellular carcinoma bel-7404 (BEL-7404), large cell lung cancer cells (NCI-H460), and bladder cancer cells (T24). Most of the compounds exhibited high levels of antitumor activity against MGC-803 and T24 but low toxicity against human normal liver cells (LO2), and their effect was even better than the commercial anticancer drugs, 5-fluorouracil (5-FU) and cis-platinum. Further, pharmacological mechanisms such as topo I, cell cycle, cell apoptosis, and neovascularization were all evaluated. Only a few compounds exhibited potent topo I inhibitory activity at 100 µM. In addition, the most active compounds with an IC50 value of 5.52-8.93 µM were chosen, and they could induce cell apoptosis in the G2 stage of MGC-803 or mainly arrest T24 cells in the S stage. To our delight, most of the compounds exhibited lower zebrafish cytotoxicity but could strongly inhibit the formation of zebrafish sub-intestinal veins, indicating a potential for clinical application.
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Antineoplásicos , Fármacos Dermatológicos , Neoplasias , Tiadiazoles , Animales , Humanos , Pez Cebra , Triazoles/farmacología , Tiadiazoles/farmacología , Acridinas/farmacología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Antineoplásicos/farmacología , Fluorouracilo/farmacología , Apoptosis , Fármacos Dermatológicos/farmacología , Proliferación Celular , Relación Estructura-Actividad , Estructura Molecular , Neoplasias/tratamiento farmacológicoRESUMEN
Robustic acid is reported to be a bioactive compound, isolated from the medicinal plant Dalbergia benthamii Prain. Ten alkyl and benzyl derivatives (2a-2j) of robustic acid were designed and synthesized based on molecular docking approaches. The biological activities of most of the synthesized compounds (such as 2g, 2h, and 2i) were closely consistent with the docking results. In particular, 4-O-phenylpropyl substituted compound 2g displayed potent topoisomerase I inhibitory activity as well as cytotoxicity against SMMC-7721, HepG2, and HeLa cell lines. Further biological testing suggests that compound 2g acted mainly by an arrest of the tumor cells in G1 phase of the cell cycle and suppressed cell proliferation by inducing apoptosis. The findings of this study are encouraging with respect to potential utilization of these compounds as new topoisomerase I inhibitors.
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Antineoplásicos/farmacología , ADN-Topoisomerasas de Tipo I/metabolismo , Diseño de Fármacos , Isoflavonas/farmacología , Simulación del Acoplamiento Molecular , Inhibidores de Topoisomerasa I/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Isoflavonas/síntesis química , Isoflavonas/química , Estructura Molecular , Relación Estructura-Actividad , Inhibidores de Topoisomerasa I/síntesis química , Inhibidores de Topoisomerasa I/químicaRESUMEN
In the present study, a series of 4-acyloxy robustic acid derivatives were synthesized and characterized for evaluation of their anti-cancer activity. The structures of these derivatives were elucidated by mass spectra (MS) nuclear magnetic resonance spectra (NMR). The single-crystal X-ray diffraction structure of one of these compounds was obtained, for further validation of the target compound structures. The anticancer activities of the target products were evaluated against human leukemic cells HL-60, human non-small cell lung carcinoma cells A-549, human hepatic carcinoma cells SMMC-7721, human hepatocellular carcinoma cells HepG2, and human cervical carcinoma cells Hela. Three compounds among them exhibited potent in-vitro cytotoxicity and excellent DNA topoisomerase I inhibitory activity, even at 0.1 mM concentrations. The most noteworthy observation was the minor toxicity of two of these compounds to normal cells, with an activity similar to the positive control in cancerous cells. A Surflex-Dock docking study was performed to investigate the topoisomerase I activity of all compounds. Of all the other compounds, the most sensitive compound was selected for further investigation of its effect on apoptosis induction and cell cycle regulation in HL-60 cells. Our results suggest that the anticancer effects of these compounds can be attributed to their pharmacological effects on topoisomerase I, cell apoptosis, and cell cycle. These findings suggest that robustic acid derivatives could be used as potential antitumor drugs.
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Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Isoflavonas/química , Piranocumarinas/síntesis química , Piranocumarinas/farmacología , Células A549 , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Células Cultivadas , ADN-Topoisomerasas de Tipo I/efectos de los fármacos , Dalbergia/química , Ensayos de Selección de Medicamentos Antitumorales , Células HL-60 , Células HeLa , Células Hep G2 , Humanos , Concentración 50 Inhibidora , Isoflavonas/farmacología , Simulación del Acoplamiento Molecular , Estructura Molecular , Piranocumarinas/química , Piranocumarinas/uso terapéutico , Inhibidores de Topoisomerasa I/síntesis química , Inhibidores de Topoisomerasa I/química , Inhibidores de Topoisomerasa I/farmacologíaRESUMEN
Background: Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of acridines. It is suggested that hybrid molecules may reduce the side effects and enhance the beneficial properties due to synergistic activity. The objectives of the present study are to synthesize and evaluate the anticancer and antimicrobial properties of new hybrids of acridine thiosemicarbazides derivatives. Results: The structures of the synthesized compounds 4a-4e were elucidated by MS and NMR spectra. In antimicrobial assay, Compound 4c exhibited potent antimicrobial activity compared to the other four compounds. In anticancer studies, we observed that compounds 4a, 4b, 4d and 4e exhibited high cytotoxicity against the MT-4 cell line, with IC50 values of 18.42 ± 1.18, 15.73 ± 0.90, 10.96 ± 0.62 and 11.63 ± 0.11 µM, respectively. The evaluation of anticancer effects, and the associated mechanism reveals that, the anticancer activities may be related to Topo I inhibitory activity, apoptosis and cell-cycle. Molecular docking studies revealed that the presence of planar naphtho-fused rings and a flexible thiourea group together, could improve DNA-intercalation and inhibition of DNA-Topo I activity. Conclusions: The results of this study demonstrate that the rational design of target derivatives as novel antimicrobial or antitumor leads is feasible.
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Antiinfecciosos/química , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Diseño de Fármacos , Semicarbacidas/química , Semicarbacidas/farmacología , Antiinfecciosos/síntesis química , Antineoplásicos/síntesis química , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Técnicas de Química Sintética , Humanos , Concentración 50 Inhibidora , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Estructura Molecular , Semicarbacidas/síntesis química , Análisis EspectralRESUMEN
In the present study, the extraction and isolation of Pelargonidin, an anthocyanin compound from stem bark of Ficus benghalensis are described. The study also involves evaluation of the effect of Pelargonidin on phenotypic variations in zebra fish embryos. Extraction and isolation of Pelargonidin were carried out by employing liquid-liquid extraction technique, phytochemical tests, column chromatography, UV and FT-IR. In the zebra fish embryo model, Paclitaxel was employed as a negative control. A series of phenotypic changes in different stages of embryonic development were studied with treatment concentrations of Pelargonidin between 3.0 and 20 ppm at 0-72-hour post-fertilization (hpf). The results of our studies indicate that, after exposure of zebra fish embryos to 3.3-20 ppm concentration of Pelargonidin for 72 h, a significant reduction in aortic development occurs. At the dose level of 0.5 ppm Paclitaxel and Pelargonidin in the dose range between 3.3 and 20 ppm, the zebra fish embryos were found to have bent tail, malformed eyes and developmental delays in vasculature. Based on the results obtained, we infer that Pelargonidin can exhibit phenotypic anti-angiogenic variations in embryonic stage of fish embryos and it can be applied in future for exploration of its anti-angiogenic potential. Furthermore, Pelargonidin could serve as a candidate drug for in vivo inhibition of angiogenesis and can be applied for the treatment of neovascular diseases and tumor.
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Swietenia macrophylla (SM) is a medicinally important plant found in tropical and subtropical regions of the world. The ethyl acetate fraction of the seeds of S. macrophylla (SMEAF) is reported to exhibit potent anticancer, antitumor, anti-inflammatory and antifeedant activities. Till date, there have been no studies reported on the acute oral toxicity profile of the ethyl acetate fraction of the seeds of SM. The objective of the present study was to determine the acute toxicity of SMEAF and evaluate the in-vitro neuroprotective activity of SMEAF using primary neuronal cell cultures. In acute oral toxicity study, the SMEAF did not produce any lethal signs of morbidity and mortality. Histo-pathological findings, support the safety of SMEAF, as there were no significant changes observed in any of the parameters studied. Based on the results obtained in MTT assay, we infer that SMEAF has a significant neuroprotective effect, as it increased the cell viability and exhibited protection to the neuronal cells against TBHP induced oxidative stress. Thus, SMEAF can be suggested for use in the development of herbal drug formulations with neuroprotective potential.
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Acorus calamus and its related species are of significant importance to the food and fragrance industries due to their varied applications. They are also a cause of critical concern due to their toxic ß-asarone content. Several toxicity cases have occurred due to high ß-asarone compositions in food products. Hence, limits for their use are strictly regulated by the Food and Drug Administration, the European Union, and legislations of different countries. The identification of species with a lower ß-asarone content is of great significance. In this report, the metabolite profiles and essential oil content of A. calamus and Acorus tatarinowii rhizomes were analysed and compared using UHPLC-QTOF-MS and GC-MS techniques. The metabolite profiles were similar; however, ß-asarone content was higher in A. calamus rhizomes. The developed methods can be applied for microscopic and macroscopic identification, and quality control of food products containing ß-asarone.
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Acorus/química , Anisoles/análisis , Aceites Volátiles/química , Rizoma/química , Acorus/efectos adversos , Derivados de Alilbenceno , Anisoles/efectos adversos , Cromatografía de Gases y Espectrometría de Masas , Metaboloma , Aceites Volátiles/efectos adversos , Especificidad de la EspecieRESUMEN
Curcuma longa L. is recognized for its therapeutic and culinary uses both in Ayurveda and traditional Chinese medicine and is considered to be a boon to mankind. It has been extensively studied for its benefits and still continues to be an important drug with continued potential for further exploration and research. We studied the tissue-specific distribution of secondary metabolites to establish the validity of the use of rhizome samples from India and China, as substitutes for each other, based upon their metabolite profiles and curcumin contents. Laser microdissection was used for the isolation of microscopic tissues, such as cork, cortex and leaf-trace vascular bundles from rhizomes. Metabolite profiling was carried out by ultra-high performance liquid chromatography-quadrupole time of fight-mass spectrometry and curcumin content was estimated by a method validated as per the Harmonized Tripartite Guidelines. The cortex and cork revealed the presence of a higher number of secondary metabolites than in the leaf-trace vascular bundles. The curcumin contents in rhizome samples from both the countries, estimated with the help of a precise and accurate validated method, were found to be comparable. Based on the results, we conclude that turmeric rhizomes grown in India and China are qualitatively and quantitatively indistinguishable and therefore can be used as substitutes. The developed method can be widely applied for microscopic identification, authentication and analysis of the distribution of phytoconstituents in other botanical species of interest or of species with a significant commercial and therapeutic value.
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Cromatografía Líquida de Alta Presión/métodos , Curcuma/metabolismo , Captura por Microdisección con Láser/métodos , Metabolismo Secundario , Espectrometría de Masas en Tándem/métodos , China , Curcuma/química , Curcumina/análisis , India , Metabolómica/métodos , Especificidad de Órganos , Reproducibilidad de los Resultados , Rizoma/química , Rizoma/metabolismoRESUMEN
INTRODUCTION: Asparagus is esteemed in Traditional Chinese Medicine and Ayurveda, and it is commercially one of the most important drugs in the global herbal market. Comparative metabolite profiling of different species would help in determining the similarities and ascertain their validity for being used as substitutes for each other. Laser microdissection (LMD) facilitates identification of metabolites in specific tissues, and thus it can aid in exploration of metabolic pathways in target tissues. OBJECTIVE: To compare tissue-specific metabolites and protodioscin content of Asparagus cochinchinensis (Lour.) Merr. and Asparagus racemosus Willd. used in China and India. METHODS: Metabolite analysis of laser-dissected tissues was carried out using UHPLC-QTOF/MS and LC-MS/MS. The protodioscin contents were determined and the method was validated as per the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines. RESULTS: Metabolite analysis reveals that the velamen tissue, among other tissues such as cortex, vascular bundles and pith, contained maximum components, specifically those belonging to the steroidal saponin class. Although the metabolite profiles were similar, the content of protodioscin was found to be higher in Chinese than Indian species. CONCLUSION: The study provided a suitable methodology for metabolite profiling and protodioscin content determination of Asparagus by use of LMD, UHPLC-QTOF/MS and LC-MS/MS. The similarities in metabolite profiles indicate that Asparagus species from India and China can serve as substitute for each other in various therapeutic and pharmaceutical applications.
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Asparagus/química , Diosgenina/análogos & derivados , Medicamentos Herbarios Chinos/química , Microdisección/métodos , Raíces de Plantas/química , Saponinas/análisis , Asparagus/citología , China , Cromatografía Líquida de Alta Presión/métodos , Diosgenina/análisis , Diosgenina/química , Diosgenina/aislamiento & purificación , Medicamentos Herbarios Chinos/análisis , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicina Tradicional China , Raíces de Plantas/citología , Saponinas/química , Saponinas/aislamiento & purificación , Espectrometría de Masas en Tándem/métodosRESUMEN
The symbiotic community of microorganisms in the gut plays an important role in the health of the host. While many previous studies have been performed on the interactions between the gut microbiome and the host in mammals, studies in fish are still lacking. In this study, we investigated changes in the intestinal microbiome and pathogen susceptibility of zebrafish (Danio rerio) following chronic antibiotics exposure. The chronic antibiotics exposure assay was performed on zebrafish for 30 days using oxytetracycline (Otc), sulfamethoxazole/trimethoprim (Smx/Tmp), or erythromycin (Ery), which are antibiotics widely used in the aquaculture industry. The microbiome analysis indicated that Fusobacteria, Proteobacteria, Firmicutes, and Bacteroidetes were the dominant phyla in the gut microbiome of the zebrafish used in this study. However, in Smx/Tmp-treated zebrafish, the compositions of Fusobacteria and Proteobacteria were changed significantly, and in Ery-treated zebrafish, the compositions of Proteobacteria and Firmicutes were altered significantly. Although alpha diversity analysis showed that there was no significant difference in the richness, beta diversity analysis revealed a community imbalance in the gut microbiome of all chronically antibiotics-exposed zebrafish. Intriguingly, in zebrafish with dysbiosis in the gut microbiome, the pathogen susceptibility to Edwardsiella piscicida, a representative Gram-negative fish pathogen, was reduced. Gut microbiome imbalance resulted in a higher count of goblet cells in intestinal tissue and an upregulation of genes related to the intestinal mucosal barrier. In addition, as innate immunity was enhanced by the increased mucosal barrier, immune and stress-related gene expression in the intestinal tissue was downregulated. In this study, we provide new insight into the effect of gut microbiome dysbiosis on pathogen susceptibility.
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In this paper, a new amphiphilic mono-6-ß-cyclodextrin octadecylimine (6-ß-CD-N-ODMA) copolymer was synthesized based on ß-cyclodextrin and octadecylamine, which can self-assemble to form polymeric micelles. Drug-loaded micelles (a new drug carrier) were obtained using 6-ß-CD-N-ODMA and paclitaxel (PTX) by the dialysis method. Orthogonal experiments were used to optimize the preparation method of the drug-loaded micelles. The drug-loading content of the carrier prepared by the optimized method was 1.97%. The physicochemical properties of blank micelles and drug-loaded micelles were evaluated by the fluorescence probe method, infrared spectra, dynamic light scattering, and scanning electron microscopy. The release properties of the carrier were investigated. The carrier has good pH sensitivity and the cumulative release rate after 96 h was 88% in PBS (pH = 5.0). The Ritger-Peppas equation is the optimal model for PTX released at pH 5.0, implying that the hydrolysis effect of 6-ß-CD-N-ODMA is the main reason for PTX release. The results indicate that the developed carrier can increase the solubility of PTX and possess potential for increased clinical efficacy of PTX.
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Kava roots have been extensively studied in clinical trials as potential candidate anti-anxiety drugs. However, anti-convulsive properties of various tissues of stems of Kava have not been reported to date. The objective of the study was to evaluate the anti-convulsive potential of aqueous extracts prepared from specific tissues of Kava (Piper methysticum) stems in zebrafish, using the PTZ-induced seizure model. The potency of each extract was compared in terms of the intensity of seizure scores and onset time after pre-treating the zebrafish before the PTZ challenge. The results indicate that aqueous extract of Kava stems without peel after 45 min of pre-treatment exhibited anti-convulsive potential at the dose of 50 mg/L. This study provides evidence to the anti-convulsive properties of peeled Kava stems and its potential for investigation and design of candidate anti-convulsive drugs.
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Polypores are cosmopolitan mushrooms, widely investigated for their beneficial properties in combatting multidrug resistant pathogens. The present study focuses on the need for new, naturally sourced antimicrobial and antioxidant compounds from mushrooms. The antioxidant and antibacterial activity of the phenolic extract of strains of Trametes polyzona (Pers.) Justo, were investigated. Strains of T. polyzona were analyzed for total phenolic content, Trolox antioxidant equivalent, DPPH radical scavenging and antibacterial activities. The amplification of the ribosomal DNA-ITS fragments from DNA of selected mushrooms was carried out using ITS1 and ITS4 primers. The antibacterial activity of phenolic extracts of T. polyzona was comparable to the antibiotics, ceftazidime and erythromycin. T. polyzona extracts inhibited the growth of the different strains of K. pneumoniae, E. coli, S. aureus, and S. enterica tested in this study. The results of the study demonstrate that, T. polyzona can be a potential source of antimicrobial and antioxidant compounds.
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BACKGROUND: Kava is an important neuroactive medicinal plant. While kava has a large global consumer footprint for its clinical and recreational use, factors related to its use lack standardization and the tissue-specific metabolite profile of its neuroactive constituents is not well understood. RESULTS: Here we characterized the metabolomic profile and spatio-temporal characteristics of tissues from the roots and stems using cross-platform metabolomics and a 3D imaging approach. Gas chromatography-mass spectrometry and liquid chromatography-mass spectrometry revealed the highest content of kavalactones in crown root peels and lateral roots. Infrared matrix-assisted laser desorption electrospray ionization (IR-MALDESI) imaging revealed a unique tissue-specific presence of each target kavalactone. X-ray micro-computed tomography analysis demonstrated that lateral roots have morphological characteristics suitable for synthesis of the highest content of kavalactones. CONCLUSIONS: These results provide mechanistic insights into the social and clinical practice of the use of only peeled roots by linking specific tissue characteristics to concentrations of neuroactive compounds.
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Kava , Imagenología Tridimensional , Lactonas , Metabolómica , Microtomografía por Rayos XRESUMEN
Serenoa repens (saw palmetto) berries are one of the most consumed medicinal herbs in the United States and the wild green variety is used in the initial therapy of benign prostatic hyperplasia (BPH), globally. Use of saw palmetto is approved by the German Commission E, and several clinical trials are underway for evaluation of its efficacy. Exploitation of its habitats and over foraging imperil this plant, which only grows in the wild. This is the first study, to propose the use of the S. repens forma glauca (silver variety) as a qualitative substitute for the wild variety, to support its conservation. We compared tissue microstructures and lipid and water distribution through spatial imaging and examined metabolite distribution of three tissue domains and whole berries. This combined approach of 3D imaging and metabolomics provides a new strategy for studying phenotypic traits and metabolite synthesis of closely related plant varieties.
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Conservación de los Recursos Naturales , Frutas/metabolismo , Serenoa/metabolismo , Frutas/anatomía & histología , Frutas/química , Humanos , Metabolismo de los Lípidos , Lípidos/análisis , Masculino , Metabolómica , Fitoterapia/métodos , Extractos Vegetales/uso terapéutico , Plantas Medicinales/anatomía & histología , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Hiperplasia Prostática/tratamiento farmacológico , Metabolismo Secundario , Serenoa/química , Análisis Espacial , Agua/análisis , Agua/metabolismoRESUMEN
Dietary phenols are antioxidants with diverse physiological functions that are beneficial for human health. The objective of this research work was to investigate antioxidant activity of p-coumaric acid (p-CA) using four in vitro methods, the protective effects against oxidative stress in PC12 cells, and hypolipidemic effects on High fat-diet (HFD) mice model. The p-CA exhibited moderate antioxidant activity in the selected in vitro assay. The highest chelating activity of p-CA at 50 µg/mL was found to be 52.22%. Pretreatment with p-CA significantly enhanced cell viability of PC12 cell and suppressed AAPH-induced intracellular ROS generation and AAPH-induced LDH release. The hypolipidemic effects of p-CA (100 mg/kg BW) was directly linked to the increased expression of nuclear factor erythroid 2-related factor (Nrf2) by 2.0-fold, Glutathione peroxidase (Gpx) by 3.8-fold, Superoxide dismutase (SOD-1) by 1.6-fold, Heme oxygenase (HO-1) by 1.72-fold and NAD(P)H Quinone Dehydrogenase 1 (NQO-1) by 1.5-fold compared with HFD group. In addition to these effects, p-CA decreased total cholesterol and atherosclerosis index levels, and increased catalase (CAT) level in serum, total antioxidant capacity (T-AOC) and glutathione peroxidase (GSH-Px) levels in liver as compared HFD group. Administration of p-CA also promoted the recovery of hyperlipidemia steatohepatitis in mice by ameliorating lipid peroxidation. These results suggested that p-CA is a potent antioxidant with potential therapeutic efficacy for treating hyperlipidemia symptoms.
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Antioxidantes/uso terapéutico , Hiperlipidemias/prevención & control , Peroxidación de Lípido/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Propionatos/uso terapéutico , Animales , Antioxidantes/farmacología , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Ácidos Cumáricos , Dieta Alta en Grasa/efectos adversos , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Depuradores de Radicales Libres/farmacología , Depuradores de Radicales Libres/uso terapéutico , Hiperlipidemias/metabolismo , Peroxidación de Lípido/fisiología , Masculino , Ratones , Estrés Oxidativo/fisiología , Células PC12 , Propionatos/farmacología , Ratas , Resultado del TratamientoRESUMEN
Achyranthes bidentata and Achyranthes aspera are saponin and steroid rich medicinal plants, used extensively for therapeutic treatments in Traditional Chinese Medicine (TCM) and Ayurveda. A. bidentata is reported to be one of the rare and extensively exploited medicinal plant species that face the issue of being endangered. Finding qualitative substitute with identical phyto-constituents contributing to similar composition and pharmacological benefits will help in reducing the burden of exploitation of the natural habitats of such plants. In the present study, a comparative metabolite analysis of the whole drug and specific tissues isolated by laser micro-dissection (LMD) was carried out for both the selected species, by use of ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-QTOF MS). The results of the study indicate that the cortex and the medullary ray tissues are rich in their content of steroidal and saponin constituents such as (25S)-inokosterone-20,22-acetonide, ginsenoside Ro, bidentatoside II and achyranthoside B. Metabolite profiling of the whole tissues of both the species indicates presence of identical constituents. Thus, it is inferred that A. bidentata and A. aspera can be used as qualitative substitutes for each other.
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Ayurveda is considered as one of the oldest of the traditional systems of medicine (TSMs) accepted worldwide. The ancient wisdom in this traditional system of medicine is still not exhaustively explored. The junction of the rich knowledge from different traditional systems of medicine can lead to new avenues in herbal drug discovery process. The lack of the understanding of the differences and similarities between the theoretical doctrines of these systems is the major hurdle towards their convergence apart from the other impediments in the discovery of plant based medicines. This review aims to bring into limelight the age old history and the basic principles of Ayurveda. This would help the budding scholars, researchers and practitioners gain deeper perspicuity of traditional systems of medicine, facilitate strengthening of the commonalities and overcome the challenges towards their global acceptance and harmonization of such medicinal systems.
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ETHNOPHARMACOLOGICAL RELEVANCE: China and India have a long history in the therapeutic application of botanical drugs in traditional medicine. Traditional Chinese Medicine (TCM) and Ayurveda are considered as two of the most ancient systems of medicine, with history of more than two millennia. Medicinal plants are the principal medicinal materials used in both these systems. AIM OF THE REVIEW: This review discusses about the histories of Ayurveda and TCM, the common medicinal plants species, the drug processing strategies used, and the current statuses of these traditional systems of medicine (TSM). Through the views presented in this article, we aim to provide a new perspective to herbal drug researchers for expanding and improving the utilization of botanical drugs and their therapeutic applications. METHODS: A bibliographic investigation of Chinese and Indian pharmacopoeias, monographs and official websites was performed. Furthermore, information was obtained from scientific databases on ethnobotany and ethno medicines. RESULTS: The review of Ayurveda and TCM ethno medicine indicates that both these systems have many medicinal materials in common. The studies carried out by the authors for comparison of plants from same genus from both these TSM's have been discussed to further bring focus to the utilization of "qualitatively" similar species which can be utilized and substituted for endangered or economically valued species. The overview of ancient literature and scientific findings for drugs in both these systems suggests that, the botanical drugs used in common and their processing methods can be explored further for extensive utilization in traditional medicine. CONCLUSION: This review describes the histories, common medicinal plant species, their processing methods and therapeutic applications in Ayurveda and TCM. The insights provided through this article may be used by herbal drug researchers and pharmacologists for further exploration of botanical drugs from these two traditional systems of medicine.