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1.
ISA Trans ; 135: 355-368, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37032567

RESUMEN

This paper proposes an intelligent control scheme for a two-stage integrated onboard electric vehicle (EV) battery charger connected to a single-phase household outlet which offers a close to ideal battery charging profile with power factor correction feature. Generally, the front-end AC-DC​ conversion stage is controlled by dual loop proportional-integral (PI) controllers, and tuning their gain constants is a difficult task. Furthermore, to achieve a close to ideal charging profile for an EV battery, the DC-DC conversion stage switches from constant current (CC) and constant voltage (CV) mode after a certain state of charge (SOC) which may lead to discontinuity in the charging current and voltage. This paper attempts to solve these issues by proposing an intelligent control scheme that includes the dynamic estimation of PI controller gain constants as well as provides a seamless mode transfer feature for battery charging. It is achieved by using fuzzy-PI-based control in the AC-DC conversion stage and Bayesian Regularization (BR) algorithm trained artificial neural network (ANN)-based control in the DC-DC conversion stage. The performance of the proposed control scheme is assessed both in steady-state and transient conditions in MATLAB® Simulink environment by comparing it against similar control schemes. The proposed intelligent control approach improves the dynamic response of DC link voltage, offers unity power factor operation and maintains the line current harmonics within IEEE 519 standards even during the switchover from CC to CV charging mode. Also, there is a decrease of 85% in the third harmonic component of the source current, 23.2% improvement in DC link voltage undershoot and 6.5% reduction in DC link voltage overshoot with reduced settling times using the proposed unified control scheme.

2.
Molecules ; 28(2)2023 Jan 04.
Artículo en Inglés | MEDLINE | ID: mdl-36677541

RESUMEN

The stem of Tinospora cordifolia has been traditionally used in traditional Indian systems of medicine for blood sugar control, without the knowledge of the underlying mechanism and chemical constitution responsible for the observed anti-diabetic effect. In the present study, Tinosporaside, a diterpenoid isolated from the stem of T. cordifolia, was investigated for its effects on glucose utilization in skeletal muscle cells, which was followed by determining the anti-hyperglycemic efficacy in our diabetic db/db mice model. We found that tinosporaside augmented glucose uptake by increasing the translocation of GLUT4 to the plasma membrane in L6 myotubes, upon prolonged exposure for 16 h. Moreover, tinosporaside treatment significantly increased the phosphorylation of protein kinase B/AKT (Ser-473) and 5' AMP-activated protein kinase (AMPK, Thr-172). These effects were abolished in the presence of the wortmannin and compound C. Administration of tinosporaside to db/db mice improved glucose tolerance and peripheral insulin sensitivity associated with increased gene expression and phosphorylation of the markers of phosphoinositide 3-kinases (PI3Ks) and AMPK signaling in skeletal muscle tissue. The findings revealed that tinosporaside exerted its antidiabetic efficacy by enhancing the rate of glucose utilization in skeletal muscle, mediated by PI3K- and AMPK-dependent signaling mechanisms.


Asunto(s)
Fosfatidilinositol 3-Quinasas , Tinospora , Ratones , Animales , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Quinasas Activadas por AMP/metabolismo , Músculo Esquelético/metabolismo , Glucosa/metabolismo , Fosfatidilinositol 3-Quinasa/metabolismo , Fibras Musculares Esqueléticas , Fosforilación , Transportador de Glucosa de Tipo 4/metabolismo
3.
Free Radic Biol Med ; 190: 339-350, 2022 09.
Artículo en Inglés | MEDLINE | ID: mdl-35998794

RESUMEN

Glucocorticoid-induced osteoporosis (GIOP) is a common clinical consequence that arises due to the extensive usage of glucocorticoids. Cladrin (Clad), a methoxylated isoflavone has been reported to have a bone protecting effect by enhancing osteoblast proliferation and differentiation. However, its consequences on GIOP are not reported yet. This study investigates whether Clad protects against the deleterious effects of Dexamethasone (Dex) on osteoblast and bone. Mice calvarial osteoblasts were treated with Clad and then exposed to Dex to study the effect on osteoblast differentiation, proliferation, and survival. Further, GIOP mice were treated with Clad (5 and 10 mg/kg) doses along with reference standard alendronate (ALN 3 mg/kg) for evaluation of bone protecting effect of Clad. We analyzed bone and vertebral microarchitecture, mechanical strength, and biochemical parameters. We observed that Clad at 10 nM concentration mitigated Dex-induced cytotoxicity and defend osteoblasts against apoptosis. Subsequent results demonstrate that Clad suppressed apoptosis of osteoblast in the presence of Dex by enhancing autophagy in a way that was reliant on the AMP-activated protein kinase (AMPK) and mammalian target of rapamycin (mTOR) pathway. Furthermore, micro-CT scanning, eco MRI results, and serum CTX levels revealed that 12 weeks of Clad treatment prevented bone loss and preserved trabecular bone mass in GIOP animals. We also observed that Clad treated osteoblasts had a lower rate of apoptosis and a greater LC3-II/LC3-I ratio than the Dex group. Our findings show that Clad can protect osteoblasts against glucocorticoids by inducing autophagy via the AMPK/mTOR pathway.


Asunto(s)
Isoflavonas , Osteoporosis , Proteínas Quinasas Activadas por AMP/genética , Proteínas Quinasas Activadas por AMP/metabolismo , Animales , Apoptosis , Autofagia , Dexametasona/farmacología , Glucocorticoides/farmacología , Isoflavonas/metabolismo , Isoflavonas/farmacología , Isoflavonas/uso terapéutico , Mamíferos/metabolismo , Ratones , Osteoblastos , Osteogénesis , Osteoporosis/inducido químicamente , Osteoporosis/tratamiento farmacológico , Osteoporosis/metabolismo , Serina-Treonina Quinasas TOR/genética , Serina-Treonina Quinasas TOR/metabolismo
4.
Omega (Westport) ; : 302228221108544, 2022 Jun 10.
Artículo en Inglés | MEDLINE | ID: mdl-35686845

RESUMEN

Death awareness and near-death experiences initiate shifts in awareness, priorities, and relationships. This narrative inquiry explored the stories of four individuals who had near-death experiences. Participants shared their experiences before and after the experiences. Findings include considerations of how mortality awareness connects with life experiences. Resonant threads across narratives included Interactions with Death, Life after Death, and Meaning in Life after Death. Specifically, findings explore near-death experiences, how life was changed following interactions with death, and the meaning-making process through death awareness. Findings and discussion explore the impact of death awareness as well as considerations for those in death and trauma-related fields.

5.
Environ Sci Pollut Res Int ; 29(11): 15432-15489, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34997510

RESUMEN

Particulate matter (PM) emitted from compression ignition (CI) engines (diesel engines) has a detrimental effect on human health and the environment. The physical and chemical characteristics of PM emitted from CI-engines are influenced by engine operating conditions and fuel properties. The morphology, nanostructure, and chemical composition of PM affect its toxicity and interaction with the environment. From automotive industry perspective, these parameters influence the design of diesel particulate filters. This study presents a review of the physical and chemical characteristics of particulate emissions from the CI-engine. The present study commences with a brief description about the composition of PM emitted from CI-engine and the PM formation mechanism in CI-engine. Later on, the detailed review of PM's physical and chemical characteristics and the effect of engine operating parameters and alternative fuels on the particle number concentration, morphology, nano-structure, and oxidative reactivity of PM is presented. Online and offline methods of diesel particulate characterization and emerging chemical characterization techniques such as X-ray photoelectron spectroscopy and X-ray absorption fine structure (EXAFS) are also discussed briefly. Correlation between physical and chemical properties, and oxidative reactivity of PM is also discussed. It was found that engine operating parameters affect the physical and chemical properties of PM. Use of alternative fuels changes the diesel particulate morphology, nanostructure, and chemical composition which enhances the oxidative reactivity of PM.


Asunto(s)
Contaminantes Atmosféricos , Nanoestructuras , Contaminantes Atmosféricos/análisis , Polvo , Gasolina/análisis , Humanos , Material Particulado/análisis , Emisiones de Vehículos/análisis
6.
J Ethnopharmacol ; 282: 114315, 2022 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-34116187

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Dalbergia sissoo DC. (Indian rosewood or Sheesham) is a traditional medicinal plant, reported since time immemorial for its analgesic, anti-nociceptive, anti-inflammatory, and immuno-modulatory properties. D. sissoo DC (DS). is being used traditionally to cure joint inflammation and joint pain. AIM: To study the potential of DS leaves and its derived novel compound CAFG to treat the clinical symptoms of osteoarthritis (OA) and its underlying mechanism. METHODS: The chemical profile of DS extract (DSE) with isoflavonoids and isoflvaonoid glycosides from the DS was established by UHPLC-PDA and UHPLC-MS/MS. Monosodium iodoacetate (MIA) was injected into the knee joint to develop the OA model in rats. DSE was given orally for 28 days daily at 250 and 500 mg.kg-1day-1. For in-vitro experiments, chondrocytes isolated from joint articular cartilage were negatively induced with interleukin-1ß (IL-1ß) and CAFG was given to the cells as a co-treatment. RESULTS: Chondrocytes undergo apoptosis following inflammation and proteoglycan synthesis affected in MIA injected knees. DSE administration prevented these effects as assessed by H&E and Toluidine blue staining. Micro-CT analysis showed that subchondral bone loss was restored. DSE decreased elevated serum levels of cartilage-bone degradation (CTX-I, CTX-II, and COMP), inflammation markers IL-1ß, and matrix-degrading MMP-3 and 13. The effects of IL-1ß on gene expression of chondrocytes were reversed by CAFG treatment at 1 µM. CONCLUSION: Data showed that DSE protected joint cartilage and deterioration in subchondral bone in vivo while in in-vitro, its active ingredient CAFG prevented interleukin-1ß induced effects and inhibited OA. This finding suggest that DSE and CAFG could be used as a possible therapeutic to treat osteoarthritis.


Asunto(s)
Artralgia/tratamiento farmacológico , Dalbergia , Glicósidos/farmacología , Isoflavonas/farmacología , Osteoartritis/tratamiento farmacológico , Administración Oral , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Cartílago Articular/efectos de los fármacos , Células Cultivadas , Condrocitos/efectos de los fármacos , Modelos Animales de Enfermedad , Flavonoides/farmacología , Fitoterapia/métodos , Extractos Vegetales/farmacología , Ratas , Resultado del Tratamiento
7.
Eur J Pharmacol ; 913: 174634, 2021 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-34785210

RESUMEN

Previously, we established adiponectin receptors (AdipoRs) as osteoanabolic target. To discover small molecule agonists of AdipoRs, we studied apigenin and apigenin-6C-glucopyranose (isovitexin) that induced osteoblast differentiation. In-silico, in vitro and omics-based studies were performed. Molecular docking using the crystal structures of AdipoRs showed different interaction profiles of isovitexin and apigenin. In osteoblasts, isovitexin but not apigenin rapidly phosphorylated AMP-activated protein kinase (pAMPK) which is downstream of AdipoRs and a master regulator of cellular energy metabolism, and upregulated expression of AdipoRs. Blocking AMPK abolished the osteogenic effect of isovitexin and its effect on AdipoR expression. Isovitexin upregulated the expression of peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), the mitochondrial biogenesis factor in osteoblasts, and the effect was blocked by AMPK inhibition. Upregulation of PGC-1α by isovitexin was accompanied by increased mitochondrial membrane proteins and mitochondrial DNA (mtDNA). Isovitexin via AdipoRs and PGC-1α induced oxidative phosphorylation (OxPhos) and ATP synthesis that resulted in osteoblast differentiation. Isovitexin had no agonistic/antagonistic activity and stimulatory/inhibitory effect in screening platforms for G protein-coupled receptors and kinases, respectively. In vivo, isovitexin upregulated AdipoRs and osteogenic genes, and increased mtDNA in rat calvarium. We conclude that isovitexin selectively via AdipoRs induced osteoblast differentiation that was fuelled by mitochondrial respiration.


Asunto(s)
Apigenina/farmacología , Osteoblastos/efectos de los fármacos , Osteogénesis/efectos de los fármacos , Receptores de Adiponectina/agonistas , Adenosina Trifosfato/metabolismo , Animales , Animales Recién Nacidos , Diferenciación Celular/efectos de los fármacos , Células Cultivadas , Metabolismo Energético/efectos de los fármacos , Ratones , Mitocondrias/efectos de los fármacos , Mitocondrias/metabolismo , Osteoblastos/metabolismo , Fosforilación Oxidativa/efectos de los fármacos , Cultivo Primario de Células , Receptores de Adiponectina/metabolismo , Regulación hacia Arriba/efectos de los fármacos
8.
Phytomedicine ; 93: 153750, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34662767

RESUMEN

BACKGROUND: Osteoporosis is an asymptomatic bone disorder leading to altered bone microarchitecture, mineralization and strength. Musa paradisiaca has been reported to have antioxidant and anti-inflammatory effects in various diseases. Its impact on postmenopausal osteoporosis has not been investigated yet. PURPOSE: The intention of the current study was to evaluate the bone regeneration and osteoprotective potential of extract and fraction of M. paradisiaca flower in ovariectomized (Ovx) Sprague Dawley (SD) rats, a model of post-menopausal bone loss. The study also aims to identify osteogenic compounds from active fraction. METHODS: Ethanolic extract (MFE) and butanolic fraction (MFE-Bu) from flower of M. paradisiaca were prepared and their efficacy was tested in rat femur osteotomy model at different doses. Effective dose from both extract (250 mg/kg) and fraction (50 mg/kg) were taken for study in osteopenic bone loss model. PTH was taken as reference standard (20 µg/kg/twice a week). Bones were harvested at autopsy for dynamic and static histomorphometry. Serum was collected for ELISA. Pure compounds were isolated from butanolic fraction (MFE-Bu), and were assessed for their osteogenic effect. RESULTS: MFE and MFE-Bu were observed for their potential in bone healing and prevention of bone loss. Both MFE and MFE-Bu promoted new bone regeneration at injury site as assessed by microCT and calcein dye labeling studies. These also led to restoration of bone microarchitecture deteriorated as a result of osteopenia and improved bone biomechanical properties. Extract as well as the fraction exhibited dual bone anabolic and anti-resorptive properties where they elevated serum procollagen type I N-terminal propeptide (P1NP), a bone formation marker and suppressed serum C-telopeptide of type I collagen (CTX-1), a bone resorption marker. As many as four osteogenic compounds were isolated from MFE-Bu. Oleracein-E was found to be the most potent osteogenic agent based on osteoblast differentiation, mineralization assays, qPCR and protein expression studies. CONCLUSION: Our studies demonstrates that ethanolic extract from the flower of M. paradisiaca and its butanolic fraction exhibit dual osteogenic and anti-resorptive potential, and have an advantage over PTH which though promotes bone formation but is also bone catabolic in nature.


Asunto(s)
Enfermedades Óseas Metabólicas , Musa , Animales , Densidad Ósea , Flores , Humanos , Osteogénesis , Ovariectomía , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-Dawley
9.
Molecules ; 26(11)2021 May 24.
Artículo en Inglés | MEDLINE | ID: mdl-34073781

RESUMEN

Estrogenic molecules have been reported to regulate glucose homeostasis and may be beneficial for diabetes management. Here, we investigated the estrogenic effect of ß-sitosterol-3-O-D-glucopyranoside (BSD), isolated from the fruits of Cupressus sempervirens and monitored its ability to regulate glucose utilization in skeletal muscle cells. BSD stimulated ERE-mediated luciferase activity in both ERα and ERß-ERE luc expression system with greater response through ERß in HEK-293T cells, and induced the expression of estrogen-regulated genes in estrogen responsive MCF-7 cells. In silico docking and molecular interaction studies revealed the affinity and interaction of BSD with ERß through hydrophobic interaction and hydrogen bond pairing. Furthermore, prolonged exposure of L6-GLUT4myc myotubes to BSD raised the glucose uptake under basal conditions without affecting the insulin-stimulated glucose uptake, the effect associated with enhanced translocation of GLUT4 to the cell periphery. The BSD-mediated biological response to increase GLUT4 translocation was obliterated by PI-3-K inhibitor wortmannin, and BSD significantly increased the phosphorylation of AKT (Ser-473). Moreover, BSD-induced GLUT4 translocation was prevented in the presence of fulvestrant. Our findings reveal the estrogenic activity of BSD to stimulate glucose utilization in skeletal muscle cells via PI-3K/AKT-dependent mechanism.


Asunto(s)
Glucosa/metabolismo , Imitación Molecular , Músculo Esquelético/metabolismo , Fitoestrógenos/farmacología , Sitoesteroles/farmacología , Transportador de Glucosa de Tipo 4/metabolismo , Células HEK293 , Humanos , Células MCF-7 , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Músculo Esquelético/citología , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal , Sitoesteroles/química
11.
Food Funct ; 11(9): 8273-8285, 2020 Sep 23.
Artículo en Inglés | MEDLINE | ID: mdl-32901645

RESUMEN

Osteoarthritis (OA) is an aging disorder characterized by degenerated cartilage and sub-chondral bone alteration in affected knee joints. Globally, millions of people suffer from this disease. However, there is a lack of safe and promising therapeutics, making the exploration and development of leads from natural sources urgent. Accordingly, food as medicine may be the most suitable approach for the treatment of this degenerative disease. Herein, we elucidated the protective role of Spinacia oleracea extract (SOE) in an anterior cruciate ligament transection (ACLT) model of osteoarthritis as a mimic of the human condition. ACL transection was done in the tibio-femoral joints of rats. SOE was orally administered at the dosage of 125 and 250 mg kg-1 day-1 for four weeks. It was shown that the animals with SOE treatment had better joint morphology than the ACLT animals, as evident by the shiny appearance of their cartilage. Hematoxylin and safranin-o staining showed that the number of chondrocytes was significantly reduced in the OA model, which was prevented with SOE treatment. The reduction in the cartilage thickness was well observed by toluidine blue staining. The reduced stain by safranin-o and toluidine blue, indicated proteoglycan loss in the ACLT-induced osteoarthritis model. The proteoglycan content and cartilage thickness were restored in the SOE group upon treatment at an SOE dosage of 125 and 250 mg kg-1 day-1. The micro-CT parameters of subchondral bone (SCB) and cartilage degradation markers in the serum corroborated our findings of the protective effects of SOE. In summary, our study suggests that SOE has therapeutic potential, which if taken regularly as a food supplement, can have beneficial effects.


Asunto(s)
Ligamento Cruzado Anterior/cirugía , Osteoartritis/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Spinacia oleracea/química , Animales , Huesos/metabolismo , Huesos/fisiopatología , Cartílago Articular/crecimiento & desarrollo , Cartílago Articular/fisiopatología , Modelos Animales de Enfermedad , Femenino , Humanos , Articulación de la Rodilla/metabolismo , Articulación de la Rodilla/fisiopatología , Osteoartritis/metabolismo , Osteoartritis/fisiopatología , Ratas , Ratas Sprague-Dawley
12.
Sci Rep ; 10(1): 195, 2020 01 13.
Artículo en Inglés | MEDLINE | ID: mdl-31932603

RESUMEN

We recently reported that a butanol soluble fraction from the stem of Cassia occidentalis (CSE-Bu) consisting of osteogenic compounds mitigated methylprednisone (MP)-induced osteopenia in rats, albeit failed to afford complete protection thus leaving a substantial scope for further improvement. To this aim, we prepared an oral formulation that was a lipid-based self-nano emulsifying drug delivery system (CSE-BuF). The globule size of CSE-BuF was in the range of 100-180 nm of diluted emulsion and the zeta potential was -28 mV. CSE-BuF enhanced the circulating levels of five osteogenic compounds compared to CSE-Bu. CSE-BuF (50 mg/kg) promoted bone regeneration at the osteotomy site and completely prevented MP-induced loss of bone mass and strength by concomitant osteogenic and anti-resorptive mechanisms. The MP-induced downregulations of miR29a (the positive regulator of the osteoblast transcription factor, Runx2) and miR17 and miR20a (the negative regulators of the osteoclastogenic cytokine RANKL) in bone was prevented by CSE-BuF. In addition, CSE-BuF protected rats from the MP-induced sarcopenia and/or muscle atrophy by downregulating the skeletal muscle atrogenes, adverse changes in body weight and composition. CSE-BuF did not impact the anti-inflammatory effect of MP. Our preclinical study established CSE-BuF as a prophylactic agent against MP-induced osteopenia and muscle atrophy.


Asunto(s)
Enfermedades Óseas Metabólicas/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Glucocorticoides/toxicidad , Atrofia Muscular/tratamiento farmacológico , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Senna/química , Animales , Enfermedades Óseas Metabólicas/inducido químicamente , Enfermedades Óseas Metabólicas/patología , Butanoles/química , Emulsiones , Masculino , Atrofia Muscular/inducido químicamente , Atrofia Muscular/patología , Fitoterapia , Extractos Vegetales/química , Tallos de la Planta/química , Sustancias Protectoras/química , Ratas , Ratas Sprague-Dawley
13.
RSC Adv ; 10(8): 4579-4588, 2020 Jan 24.
Artículo en Inglés | MEDLINE | ID: mdl-35495260

RESUMEN

Cassia occidentalis L. stem extract is used as a purgative, febrifuge, and diuretic, and in the treatment of flu, fever, fracture and bone diseases. Pharmacological studies prove the osteogenic and antiresorptive effects of Cassia occidentalis L. ethanolic extract (COEE), which may be due to apigenin, apigenin-6-C-glucopyranoside, luteolin, 3',4',7-trihydroxyflavone and emodin. The objectives of this study was to develop a selective and sensitive LC-MS/MS method and validate for the simultaneous determination of the above five biomarkers in rat plasma after oral administration of COEE at a dose of 500 mg kg-1. The analytes were separated on a Phenomenex Luna C18 column (4.6 × 150 mm, 3.0 µm) with an isocratic mobile phase consisting of methanol-10 mM ammonium acetate buffer (95 : 05, v/v). Run time was for 5.5 min with LLOQ of 1 ng mL-1 for all the analytes. The mass spectrometer was operating in negative ionization mode for quantification of the analytes. The calibration curves were linear (r 2 > 0.99) for all the analytes. The intra- and inter-day precisions were less than 8.17% and the relative error was between -8.57% and 7.28%. Analytes were rapidly absorbed in the oral pharmacokinetic study. The biomarkers were stable in simulated gastric and intestinal fluids but underwent metabolism in rat liver microsomes. This is the first report on in vivo oral pharmacokinetics and in vitro stability studies of osteogenic compounds present in COEE. These results will be helpful for further understanding of pharmacodynamic behaviour of COEE and the bioanalytical method will be useful for further preclinical/clinical trials.

15.
Neurotoxicology ; 73: 100-111, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-30857974

RESUMEN

Extract of Ulmus wallichiana is being used as traditional medicine used for the treatment of fractured bones however the effect of its individual flavonols is not known. The present study was conducted to investigate the effect of its novel flavonol, (2S, 3S)-(+)-30, 40, 5, 7-tetrahydroxydihydroflavonol-6-C-b-d-glucopyranoside named as Ulmoside A (UA), on lipopolysaccharides (LPS) treated neurons. LPS treatment to neuronal cells caused significant cytotoxicity, reactive oxygen species generation, depletion in glutathione and mitochondrial impairment which were significantly inhibited with UA treatment. LPS treatment also caused significant translocation of cytochrome-c, decreased level of Bcl2, increased level of Bax and cleaved caspase-3 in neuronal cells reflecting the involvement of intrinsic apoptotic pathway in neuronal death which was attenuated with UA treatment. Since LPS is a well known pro-inflammatory agent it also offered the significant increase in proinflammatory cytokines (tumor necrosis factors-α & interleukin 1-beta) however, UA treatment did not exhibit significant inhibition against LPS induced inflammatory response. LPS also caused the augmented level of inducible nitric oxide synthase (iNOS) which was also not inhibited with co treatment of UA. We have also observed the significant DNA fragmentation and augmented level of cleaved Poly (ADP-Ribose) polymerase 1 after LPS treatment which was significantly reverted with UA treatment. Findings suggested that UA acts through mitochondria and exhibited its anti-oxidative and anti-apoptotic activities in neuronal cells while no significant anti-inflammatory activity and effect on iNOS were observed.


Asunto(s)
Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Flavonoides/farmacología , Glicósidos/farmacología , Neuronas/efectos de los fármacos , Fármacos Neuroprotectores/farmacología , Estrés Oxidativo/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Ulmus , Animales , Antioxidantes/aislamiento & purificación , Proteínas Reguladoras de la Apoptosis/metabolismo , Línea Celular Tumoral , Citocinas/metabolismo , Flavonoides/aislamiento & purificación , Glutatión/metabolismo , Glicósidos/aislamiento & purificación , Mediadores de Inflamación/metabolismo , Lipopolisacáridos/toxicidad , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ratones , Mitocondrias/efectos de los fármacos , Mitocondrias/metabolismo , Mitocondrias/patología , Neuronas/metabolismo , Neuronas/patología , Fármacos Neuroprotectores/aislamiento & purificación , Óxido Nítrico Sintasa de Tipo II/metabolismo , Transducción de Señal , Ulmus/química
16.
J Ethnopharmacol ; 235: 8-18, 2019 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-30703497

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Cassia occidentalis L., a synonym of Senna occidentalis (belongs to Caesalpiniaceae family) is an annual plant. Pursuing a lead from a folk practice prevalent since the late nineteenth century in Andhra Pradesh, a Southern state of India, of use of Cassia occidentalis leaf and stem for treating patients with fracture and bone diseases, we have not only confirmed its fracture healing activity but also demonstrated efficacy in preventing glucocorticoid-induced osteoporosis (GIO), the commonest form of medication-induced bone loss caused chiefly due to impairment of bone formation. AIM OF THE STUDY: In the present work, the effects of extract and fraction of leaf and stem of Cassia occidentalis was investigated in fracture healing and GIO models of rat. The study also aimed to identify osteogenic compounds from this plant. MATERIALS AND METHODS: Ethanolic extracts from leaf and stem of Cassia occidentalis were prepared and their efficacy tested in rat femur osteotomy (fracture healing) model. Subsequently, a butanolic fraction was prepared and osteogenic efficacy compared with the ethanolic extract, and upon finding the former to be more potent, its osteogenic effect was studied in details in GIO model. Chemical finger-printing and isolation of ten pure compounds were done to assess their osteogenic effect in rat primary osteoblast cultures. RESULTS: Ethanolic extract of stem was more effective than the leaf extract in enhancing bone regeneration at the site of osteotomy. Further, butanolic fraction of the ethanolic extract of stem was more effective than the later in bone regeneration at the femur osteotomy site and in preventing bone loss in GIO model. The mechanism of skeletal preservation involved stimulation of new bone formation and inhibition of bone resorption. As many as six osteogenic compounds were isolated out of which apigenin-6C-glucopyranoside was most effective in vitro. CONCLUSION: Our study found that a standardized extract of an ethanolic extract and its butanolic fraction from the stem of Cassia occidentalis has osteogenic as well as anti-resorptive effects, resulting in the protection against glucocorticoid-induced bone loss. Our results contribute towards validation of the traditional use of Cassia occidentalis in fracture healing and also suggest its beneficial use in GIO for which clinical trials are warranted.


Asunto(s)
Enfermedades Óseas Metabólicas/prevención & control , Glucocorticoides/toxicidad , Extractos Vegetales/farmacología , Senna/química , Animales , Células Cultivadas , Modelos Animales de Enfermedad , Etanol/química , Curación de Fractura/efectos de los fármacos , India , Osteoblastos/efectos de los fármacos , Osteoblastos/metabolismo , Osteogénesis/efectos de los fármacos , Ratas , Ratas Sprague-Dawley
17.
Nat Prod Res ; 33(2): 233-238, 2019 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29488392

RESUMEN

Phytochemical investigation of Cissus quadrangularis stems led to the isolation of one new phenolic glycoside (1) and two new lignan glycosides (7 & 8) along with twelve known compounds (2-6 & 9-15). Their chemical structures were determined on the basis of extensive spectroscopic analysis using 1D, 2D NMR, and mass spectrometric analysis. Among the known compounds, 4-6, 9 and 12 were isolated for the first time from the genus Cissus whereas compounds 10, 11 and 13 for the first time from this plant.


Asunto(s)
Cissus/química , Glicósidos/aislamiento & purificación , Lignanos/aislamiento & purificación , Glicósidos/farmacología , Lignanos/farmacología , Espectroscopía de Resonancia Magnética , Estructura Molecular , Fenoles , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Tallos de la Planta/química
18.
Nat Prod Res ; 33(15): 2253-2256, 2019 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-30259760

RESUMEN

Spinacia oleracea L. (Spinach) is a leafy vegetable which is considered to have a high nutritional value. Flavonoids in spinach were reported to act as antimutagenic property. Rapid detection of these flavonoids in Spinach was achieved by using HPLC-ESI-QTOF-MS/MS. Thirty six compounds were tentatively identified based on their retention times, accurate mass and MS/MS spectra. The fragmentation patterns of known compounds were applied to elucidate the structure of their corresponding derivatives having the same basic skeleton. Out of thirty six peaks, three peaks were assigned as patuletin and six peaks were assigned as spinacetin derivatives. Twelve compounds were first time identified following the fragmentation pattern of known compounds. Five of the identified compounds i.e., spinacetin, 5,3',4'-trihydroxy-3-methoxy-6,7-methylenedioxyflavone, protocatechuic acid, ferulic acid and coumaric acid were simultaneously quantified in spinach leaves by a validated UPLC-ESI-MS/MS method under MRM mode.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Flavonoides/aislamiento & purificación , Spinacia oleracea/química , Espectrometría de Masas en Tándem/métodos , Flavonoides/química , Extractos Vegetales/análisis , Hojas de la Planta/química
19.
J Chromatogr Sci ; 56(8): 738-745, 2018 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-29800074

RESUMEN

An ultra performance liquid chromatography coupled with hybrid triple-quadrupole linear ion trap tandem mass spectrometry (UPLC-ESI-QqQLIT-MS-MS) method in multiple reaction monitoring mode was developed for identification and simultaneous determination of potential osteogenic compounds in ethanol extracts of different plant parts of Butea monosperma collected from different geographical regions. The chromatographic separation was carried out on an Acquity UPLC CSH C18 column (1.7 µm, 2.1 × 100 mm) with 0.1% (v/v) formic acid in water and methanol as mobile phase under gradient conditions in 8 min. The developed method was validated according to the guidelines of international conference on harmonization. The correlation coefficients of all the calibration curves were ≥0.9995 and recoveries ranged from 95.2 to 105.8% (RSD ≤ 1.95%). Relative standard deviations of intra-day, inter-day precisions and stability were ≤1.74, 1.84 and 2.8%, respectively. The quantitative results showed remarkable differences in the content of all potential osteogenic compounds in different parts of the plant as well as samples from different geographical regions. Quantitative variations studied from principal component analysis indicated tentative markers for B. monosperma cultivars which can discriminate sample of different geographical regions.


Asunto(s)
Butea/química , Cromatografía Líquida de Alta Presión/métodos , Fitoquímicos/análisis , Extractos Vegetales/química , Espectrometría de Masas en Tándem/métodos , Límite de Detección , Análisis de Componente Principal , Espectrometría de Masa por Ionización de Electrospray/métodos
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