RESUMEN

Emerging antibiotic resistance in bacteria endorses the failure of existing drugs with chronic illness, complicated treatment, and ever-increasing expenditures. Bacteria acquire the nature to adapt to starving conditions, abiotic stress, antibiotics, and our immune defense mechanism due to its swift evolution. The intense and inappropriate use of antibiotics has led to the development of multidrug-resistant (MDR) strains of bacteria. Phytochemicals can be used as an alternative for complementing antibiotics due to their variation in metabolic, genetic, and physiological fronts as well as the rapid evolution of resistant microbes and lack of tactile management. Several phytochemicals from diverse groups, including alkaloids, phenols, coumarins, and terpenes, have effectively proved their inhibitory potential against MDR pathogens through their counter-action towards bacterial membrane proteins, efflux pumps, biofilms, and bacterial cell-to-cell communications, which are important factors in promoting the emergence of drug resistance. Plant extracts consist of a complex assortment of phytochemical elements, against which the development of bacterial resistance is quite deliberate. This review emphasizes the antibiotic resistance mechanisms of bacteria, the reversal mechanism of antibiotic resistance by phytochemicals, the bioactive potential of phytochemicals against MDR, and the scientific evidence on molecular, biochemical, and clinical aspects to treat bacterial pathogenesis in humans. Moreover, clinical efficacy, trial, safety, toxicity, and affordability investigations, current status and developments, related demands, and future prospects are also highlighted.

Asunto(s)

Infecciones Bacterianas , Fitoquímicos , Antibacterianos/uso terapéutico , Bacterias/genética , Infecciones Bacterianas/microbiología , Proteínas Bacterianas/metabolismo , Biopelículas , Farmacorresistencia Bacteriana Múltiple , Humanos , Pruebas de Sensibilidad Microbiana , Fitoquímicos/química

RESUMEN

Liver cancer is one of the most malignant cancers worldwide with poor prognosis. Intracellular mediators like microvesicles (MVs) and cancer stem cells (CSCs) are considered as potential candidates in liver cancer progression. CSCs receive stimuli from the tumor microenvironment to initiate tumor formation in which it's secreted MVs play a noteworthy role. The phenotypic conversion of tumor cells during epithelial-to-mesenchymal transition (EMT) is a key step in tumor invasion and metastasis which indicates that the diverse cell populations within the primary tumor are in a dynamic balance and can be regulated by cell to cell communication via secreted microvesicles. Thus, in this review, we aim to highlight the evidences that suggest CSCs are crucial for liver cancer development where the microvesicles plays an important part in the maintenance of its stemness properties. In addition, we summarize the existing evidences that support the concept of microvesicles, the tiny particles have a big role behind the rare immortal CSCs which controls the tumor initiation, propagation and metastasis in liver cancer. Identifying interactions between CSCs and microvesicles may offer new insights into precise anti-cancer therapies in the future.

Asunto(s)

Neoplasias Hepáticas/terapia , Células Madre Neoplásicas , Transición Epitelial-Mesenquimal , Humanos , Neoplasias Hepáticas/etiología , Microambiente Tumoral

RESUMEN

The present study was aimed to evaluate the effect of apigenin 8-C-glucoside (Vitexin) and chlorogenic acid on epileptic mice induced by pilocarpine and explored its possible mechanisms. Intraperitonial administration of pilocarpine (85mg/kg) induced seizure in mice was assessed by behavior observations, which is significantly (p>0.05) reduced by apigenin 8-C-glucoside (AP8CG) (10mg/kg) and chlorogenic acid (CA) (5mg/kg), similar to diazepam. Seizure was accompanied by an imbalance in the levels of Gamma-aminobutyric acid (GABA) and glutamate in the pilocarpine administered group. Moreover, convulsion along with reduced acetylcholinesterase, increased monoamine oxidase and oxidative stress was observed in epileptic mice brain. AP8CG and CA significantly restored back to normal levels even at lower doses. Further, increased lipid peroxidation and nitrite content was also significantly attenuated by AP8CG and CA. However, CA was found to be more effective when compared to AP8CG. In addition, the mRNA expression of N-methyl-d-aspartate receptor (NMDAR), mGluR1 and mGlu5 was significantly (P≤0.05) inhibited by AP8CG and CA in a lower dose. The mRNA expression of GRIK1 did not differ significantly in any of the group and showed a similar pattern of expression. Our result shows that AP8CG and CA selectively inhibit NMDAR, mGluR1 and mGlu5 expression. Modification in the provoked NMDAR calcium response coupled with neuronal death. Hence, these findings underline that the polyphenolics, AP8CG and CA have exerted antiepileptic and neuroprotective activity by suppressing glutamate receptors.

Asunto(s)

Anticonvulsivantes/uso terapéutico , Apigenina/uso terapéutico , Ácido Clorogénico/uso terapéutico , Epilepsia/tratamiento farmacológico , Epilepsia/genética , Receptores de N-Metil-D-Aspartato/genética , Animales , Anticonvulsivantes/farmacología , Antioxidantes/metabolismo , Apigenina/química , Apigenina/farmacología , Conducta Animal/efectos de los fármacos , Ácido Clorogénico/química , Ácido Clorogénico/farmacología , Regulación de la Expresión Génica/efectos de los fármacos , Ácido Glutámico/metabolismo , Glutatión/metabolismo , Hipocampo/efectos de los fármacos , Hipocampo/enzimología , Hipocampo/patología , Masculino , Ratones , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Óxido Nítrico/metabolismo , Pilocarpina , Receptores de N-Metil-D-Aspartato/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo , Ácido gamma-Aminobutírico/metabolismo

RESUMEN

PURPOSE: Pergularia daemia Forsk. (Asclepiadaceae) is a traditionally reported medicinal herb used to treat joint pain and arthritis. However, there are no scientific reports about anti-arthritic activity of P. daemia methanolic extract on rats as animal model. This study identifies bioactive compounds present in the P. daemia methanolic extract and evaluates its anti-arthritic potential in CFA induced arthritic rats. METHODS AND RESULTS: Phytoconstituents of P. daemia extract were examined using LC-ESI/MS method. Anti-arthritic activity of P. daemia extract was determined by various biochemical experiments (RF, ESR and CRP), ultrasonography and histological analysis. LC-ESI/MS analysis resulted in the identification of major flavonoids compounds such as formononetin, qurecetin, chrysoeriol, taxifolin and naringenin. Serum biomarker analysis, after the treatment with PDME (500mg/kg b.w.) revealed that the hemoglobin (11.84±0.42g/dL) and RBC (8.38±0.67million/mm(3)) levels were significantly increased whereas WBC (8.91±0.38thousands/mm(3)), RF (17.94±0.45IU/mL), ESR (7.91±0.12mm/h) and CRP (22.56±0.26mg/L) levels were decreased when compared with the CFA induced arthritic control group. Histology results revealed that treatment with PDME has resulted in significant prevention against bony destruction by decreasing soft tissue swelling and narrowing of joint spaces (250 and 500mg/kg b.w.). CONCLUSION: Anti-arthritic effect of P. daemia might be due to the presence of these bioactive flavonoids. These findings lend pharmacological support to the reported folkloric use of P. daemia in the treatment and management of painful, arthritic inflammatory conditions.

Asunto(s)

Apocynaceae/química , Artritis Experimental/tratamiento farmacológico , Flavonoides/uso terapéutico , Extractos Vegetales/uso terapéutico , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Artritis Experimental/sangre , Artritis Experimental/diagnóstico por imagen , Artritis Experimental/patología , Biomarcadores/metabolismo , Peso Corporal/efectos de los fármacos , Cromatografía Liquida , Extremidades/patología , Femenino , Flavonoides/química , Flavonoides/farmacología , Adyuvante de Freund , Hemoglobinas/metabolismo , Mediadores de Inflamación/metabolismo , Espectrometría de Masas , Fitoquímicos/análisis , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoterapia , Extractos Vegetales/farmacología , Ratas Wistar

RESUMEN

Pouteria campechiana (Kunth) Baehni. is used as a remedy for coronary trouble, liver disorders, epilepsy, skin disease, and ulcer. Therefore, the present study aims to investigate the antioxidant and hepatoprotective effect of polyphenolic-rich P. campechiana fruit extract against acetaminophen-intoxicated rats. Total phenolic and flavonoid contents of egg fruit were estimated followed by the determination of antioxidant activities. Treatment with P. campechiana fruit extract effectively scavenged the free radicals in a concentration-dependent manner within the range of the given concentrations in all antioxidant models. The presence of polyphenolic compounds were confirmed by high-performance thin-layer chromatography (HPTLC). The animals were treated with acetaminophen (250 mg/kg body weight; p.o.) thrice at the interval of every 5 days after the administration of P. campechiana aqueous extract and silymarin (50 mg/kg). Acetaminophen treatment was found to trigger an oxidative stress in liver, leading to an increase of serum marker enzymes. However, treatment with P. campechiana fruit extract significantly reduced the elevated liver marker enzymes (aspartate transaminase, alanine transaminase, and alkaline phosphatase) and increased the antioxidant enzymes (viz., superoxide dismutase and catalase) and glutathione indicating the effect of the extract in restoring the normal functional ability of hepatocytes. These results strongly suggest that P. campechiana fruit extract has strong antioxidant and significant hepatoprotective effect against acetaminophen-induced hepatotoxicity

Asunto(s)

Animales , Ratas , Antioxidantes/farmacocinética , Pouteria , Acetaminofén/efectos adversos , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Modelos Animales de Enfermedad , Medicamento Fitoterápico , Sustancias Protectoras/farmacocinética

RESUMEN

Pouteria campechiana (Kunth) Baehni. is used as a remedy for coronary trouble, liver disorders, epilepsy, skin disease, and ulcer. Therefore, the present study aims to investigate the antioxidant and hepatoprotective effect of polyphenolic-rich P. campechiana fruit extract against acetaminophen-intoxicated rats. Total phenolic and flavonoid contents of egg fruit were estimated followed by the determination of antioxidant activities. Treatment with P. campechiana fruit extract effectively scavenged the free radicals in a concentration-dependent manner within the range of the given concentrations in all antioxidant models. The presence of polyphenolic compounds were confirmed by high-performance thin-layer chromatography (HPTLC). The animals were treated with acetaminophen (250 mg/kg body weight; p.o.) thrice at the interval of every 5 days after the administration of P. campechiana aqueous extract and silymarin (50 mg/kg). Acetaminophen treatment was found to trigger an oxidative stress in liver, leading to an increase of serum marker enzymes. However, treatment with P. campechiana fruit extract significantly reduced the elevated liver marker enzymes (aspartate transaminase, alanine transaminase, and alkaline phosphatase) and increased the antioxidant enzymes (viz., superoxide dismutase and catalase) and glutathione indicating the effect of the extract in restoring the normal functional ability of hepatocytes. These results strongly suggest that P. campechiana fruit extract has strong antioxidant and significant hepatoprotective effect against acetaminophen-induced hepatotoxicity.

Asunto(s)

Acetaminofén/toxicidad , Analgésicos no Narcóticos/toxicidad , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Depuradores de Radicales Libres/farmacología , Extractos Vegetales/farmacología , Pouteria/química , Animales , Benzotiazoles/química , Compuestos de Bifenilo/química , Catalasa/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Cromatografía en Capa Delgada , Citoprotección , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Frutas/química , Hepatocitos/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Masculino , Óxido Nítrico/química , Estrés Oxidativo , Picratos/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Polifenoles/aislamiento & purificación , Polifenoles/farmacología , Ratas , Ratas Wistar , Ácidos Sulfónicos/química , Superóxido Dismutasa/metabolismo

RESUMEN

In this present study, we investigated thio glycolic acid-capped cadmium telluride quantum dots (TGA-CdTe QDs) as nano carrier to study the antiarthritic activity of quercetin on adjuvant induced arthritic Wistar rats. The free radical scavenging activity of QDs-QE complex was evaluated by 2,2'-azinobis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and superoxide anion scavenging assays. Fifteen days after adjuvant induction, arthritic rats received QDs-QE complex orally at the dose of 0.2 and 0.4mg/kg daily for 3 weeks. Diclofenac sodium (DF) was used as a reference drug. Administration of QDs-QE complex showed a significant reduction in inflammation and improvement in cartilage regeneration. Treatment with QDs-QE complex significantly (P<0.05) reduced the expressions lipid peroxidation and showed significant (P<0.05) increase in activities of antioxidant enzymes such as superoxide dismutase (SOD), reduced glutathione (GSH), glutathione peroxidase (GPx) catalase (CAT) levels in paw tissue. C-reactive protein (CRP), rheumatoid factor (RF), red blood cells (RBC) and white blood cells (WBC) count and erythrocyte sedimentation rate (ESR) of experimental animals were also estimated. Histology of hind limb tissue in experimental groups confirmed the complete cartilage regeneration in arthritis induced rats treated with QDs-QE complex. Based on our findings, we suggest that the QDs act as nano carrier for the drugs used in the treatment of various degenerative diseases.

Asunto(s)

Artritis Experimental/tratamiento farmacológico , Compuestos de Cadmio/química , Puntos Cuánticos/química , Quercetina/administración & dosificación , Telurio/química , Tioglicolatos/química , Animales , Antioxidantes/administración & dosificación , Artritis Experimental/sangre , Artritis Experimental/patología , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Femenino , Tamaño de la Partícula , Puntos Cuánticos/ultraestructura , Ratas , Ratas Wistar , Espectrofotometría

RESUMEN

Oxygen is the most essential molecule for life; since it is a strong oxidizing agent, it can aggravate the damage within the cell by a series of oxidative events including the generation of free radicals. Antioxidative agents are the only defense mechanism to neutralize these free radicals. Free radicals are not only generated internally in our body system but also trough external sources like environmental pollution, toxic metals, cigarette smoke, pesticides, etc., which add damage to our body system. Inhaling these toxic chemicals in the environment has become unavoidable in modern civilization. Antioxidants of plant origin with free radical scavenging properties could have great importance as therapeutic agents in several diseases caused by environmental pollution. This review summarizes the generation of reactive oxygen species and damage to cells by exposure to external factors, unhealthy lifestyle, and role of herbal plants in scavenging these reactive oxygen species.

Asunto(s)

Exposición a Riesgos Ambientales/efectos adversos , Estilo de Vida , Estrés Oxidativo/efectos de los fármacos , Consumo de Bebidas Alcohólicas/efectos adversos , Antioxidantes/análisis , Antioxidantes/farmacología , Dieta , Exposición a Riesgos Ambientales/análisis , Fabaceae/química , Radicales Libres/análisis , Humanos , Metales Pesados/análisis , Metales Pesados/toxicidad , Oxígeno/análisis , Oxígeno/metabolismo , Plaguicidas/análisis , Plaguicidas/toxicidad , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Especies Reactivas de Oxígeno/metabolismo , Especies Reactivas de Oxígeno/toxicidad , Fumar/efectos adversos , Estrés Fisiológico/efectos de los fármacos , Rayos Ultravioleta/efectos adversos , Verduras/química

RESUMEN

This study was undertaken to evaluate the antioxidant potential of an aqueous extract from Merremia emarginata leaves because this plant has a very high flavonoid and phenol content. The in vitro antioxidant activity was measured by diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid (ABTS), superoxide anion scavenging assay and lipid peroxidation activity; the total reducing capability of the plant extract indicates that this plant is a source for natural antioxidants. Furthermore, we investigated thio glycolic acid-capped cadmium telluride quantum dots (TGA-CdTe QDs) as fluorescent probes to study the antioxidant activity of the M. emarginata extract through fluorescence quenching. The antimicrobial activity was also investigated using a disc diffusion method and fluorescence microscopy. The TGA-CdTe QDs and M. emarginata complex could provide antimicrobial activity through a reactive oxygen species pathway and/or microbial endocytosis through an electrostatic attraction. Based on our findings, we suggest that the QDs act as potential probes for the in vitro antioxidant and antimicrobial activities. In addition, their cooperative effect with the plant extract indicates that QDs could be used as nanocarriers to enhance the antimicrobial capability. Further in vivo studies on the photolabelling of antioxidants with QDs will provide insights into the mechanistic pathways of secondary metabolites against various degenerative diseases.

Asunto(s)

Antibacterianos/farmacología , Antioxidantes/farmacología , Compuestos de Cadmio/química , Convolvulaceae/química , Puntos Cuánticos , Telurio/química , Tioglicolatos/química , Benzotiazoles/química , Compuestos de Bifenilo/química , Difusión , Escherichia coli/efectos de los fármacos , Flavonoides/análisis , Indicadores y Reactivos , Peroxidación de Lípido/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Nanopartículas , Fenoles/análisis , Picratos/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Espectrometría de Fluorescencia , Ácidos Sulfónicos/química , Superóxidos/química

RESUMEN

The methanolic extract of the aerial part of Hedyotis corymbosa (L.) Lam. (Rubiaceae) was screened for antioxidant activity using 1,1-diphenyl-2-picryl hydroxyl (DPPH) quenching assay, 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid (ABTS) cation decolorization test, ferric reducing power (FRP), scavenging capacity towards hydroxyl ion (OH*) radicals and nitric oxide (NO) radical inhibition activity using established assay procedures. Total phenolics and total flavonoid contents were, also determined. The plant yielded 210 mg gallic acid equivalent/100 g phenolic content and 55 mg quercetin equivalent/100 g flavonoid content. The extract exhibited high antiradical activity against DPPH, ABTS, nitric oxide and hydroxyl radicals with EC50 value of 82, 150, 130, and 170 microg/ml, respectively. The FRP increased with increasing concentration of the sample. The antioxidant activity of the extract was comparable with that of the standard butylated hydroxyl toluene (BHT). High correlation between total phenolic/flavonoid contents and scavenging potential of different reactive oxygen species (R2 = 0.785-0.998) indicated the polyphenols as the main antioxidants.

Asunto(s)

Antioxidantes/farmacología , Extractos Vegetales/farmacología , Rubiaceae/química , Depuradores de Radicales Libres/farmacología , Técnicas In Vitro , Especies Reactivas de Oxígeno/metabolismo