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1.
Mol Neurobiol ; 2023 Nov 21.
Artículo en Inglés | MEDLINE | ID: mdl-37987958

RESUMEN

Therapeutic options to contain seizures, a transitional stage of many neuropathologies, are limited due to the blood-brain barrier (BBB). Herbal nanoparticle formulations can be employed to enhance seizure prognosis. Bacoside A (BM3) and bacopaside I (BM4) were isolated from Bacopa monnieri and synthesized as nanoparticles (BM3NP and BM4NP, respectively) for an effective delivery system to alleviate seizures and associated conditions. After physicochemical characterization, cell viability was assessed on mouse neuronal stem cells (mNSC) and neuroblastoma cells (N2a). Thereafter, anti-seizure effects, mitochondrial membrane potential (MMP), apoptosis, immunostaining and epileptic marker mRNA expression were determined in vitro. The seizure-induced changes in the cortical electroencephalogram (EEG), electromyography (EMG), Non-Rapid Eye Movement (NREM) and Rapid Eye Movement (REM) sleep were monitored in vivo in a kainic acid (KA)-induced rat seizure model. The sizes of BM3NPs and BM4NPs were 165.5 nm and 689.6 nm, respectively. They were biocompatible and also aided in neuroplasticity in mNSC. BM3NPs and BM4NPs depicted more than 50% cell viability in N2a cells, with IC50 values of 1609 and 2962 µg/mL, respectively. Similarly, these nanoparticles reduced the cytotoxicity of N2a cells upon KA treatment. Nanoparticles decreased the expression of epileptic markers like fractalkine, HMGB1, FOXO3a and pro-inflammatory cytokines (P < 0.05). They protected neurons from apoptosis and restored MMP. After administration of BM3NPs and BM4NPs, KA-treated rats attained a significant reduction in the epileptic spikes, sleep latency and an increase in NREM sleep duration. Results indicate the potential of BM3NPs and BM4NPs in neutralizing the KA-induced excitotoxic seizures in neurons.

2.
J Ethnopharmacol ; 309: 116366, 2023 Jun 12.
Artículo en Inglés | MEDLINE | ID: mdl-36914036

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Sauropus androgynus is a medicinal shrub used for the treatment of fever in ethnomedical traditions in various Southeast Asian countries. AIM OF THE STUDY: This study was aimed to identify antiviral principles from S. androgynus against Chikungunya virus (CHIKV), a major mosquito-borne pathogen that re-emerged in the last decade, and to unravel their mechanism of action. MATERIALS AND METHODS: Hydroalcoholic extract of S. androgynus leaves was screened for anti-CHIKV activity using cytopathic effect (CPE) reduction assay. The extract was subjected to activity guided isolation and the resultant pure molecule was characterized by GC-MS, Co-GC and Co-HPTLC. The isolated molecule was further evaluated for its effect by plaque reduction assay, Western blot and immunofluorescence assays. In silico docking with CHIKV envelope proteins and molecular dynamics simulation (MD) analyses were used to elucidate its possible mechanism of action. RESULTS: S. androgynus hydroalcoholic extract showed promising anti-CHIKV activity and its active component, obtained by activity guided isolation, was identified as ethyl palmitate (EP), a fatty acid ester. At 1 µg/mL, EP led to 100% inhibition of CPE and a significant 3 log10 reduction in CHIKV replication in Vero cells at 48 h post-infection. EP was highly potent with an EC50 of 0.0019 µg/mL (0.0068 µM) and a very high selectivity index. EP treatment significantly reduced viral protein expression, and time of addition studies revealed that it acts at the stage of viral entry. A strong binding to the viral envelope protein E1 homotrimer during entry, thus preventing viral fusion, was identified as a possible mechanism by which EP imparts its antiviral effect. CONCLUSIONS: S. androgynus contains EP as a potent antiviral principle against CHIKV. This justifies the use of the plant against febrile infections, possibly caused by viruses, in various ethnomedical systems. Our results also prompt more studies on fatty acids and their derivatives against viral diseases.


Asunto(s)
Fiebre Chikungunya , Virus Chikungunya , Plantas Medicinales , Animales , Chlorocebus aethiops , Virus Chikungunya/fisiología , Células Vero , Línea Celular , Fiebre Chikungunya/tratamiento farmacológico , Fiebre Chikungunya/metabolismo , Replicación Viral , Antivirales/farmacología , Antivirales/uso terapéutico , Antivirales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Medicina Tradicional
3.
PLoS One ; 17(11): e0277341, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36383625

RESUMEN

Mast seeding and associated events in Melocanna baccifera, the largest fruit producing bamboo, is an enigma. So far there are no comprehensive accounts on its flowering phenology, fruiting dynamics and animal interactions. In this study, spanning over 13 years (2009 to 2022), we observed eight M. baccifera clumps in JNTBGRI Bambusetum from flowering initiation, fruiting to eventual death. Flowering phenology, floral characteristics, floret types, breeding system, bee visitation, pollination, fruit production and predators were recorded; predation patterns were correlated with fruit chemistry. Flowering duration of clumps ranged from 20 (March 2009-October 2010) to 120 (September 2012-August 2022) months. Bisexual florets are dichogamous and protogynous; and female duration (22-72 h) is many times higher than male duration (2-6 h). The highest ever fruit production for an individual bamboo clump (456.67 Kg) was recorded. Of the total fallen fruits (38371), 38.11% were predated, 43.80% good fruits (no predator hits) and 18.09% immature fruits. A positive correlation between reward (fruits) versus predation was observed, especially in short intervals of high fruit production. Pollen predators (Apis cerana indica, Halictus taprabonae, Braunsapis cupulifera, Trigona iridipennis), fruit predators, ranging from arthropods to mammals, viz., millipede (Spinotarsus colosseus), slug (Mariaella dussumieri), snails (Cryptozona bistrialis, Macrochlamys sp.), borers (Achroia grisella, Blattella germanica), mammals (monkeys Macaca radiata, rats Rattus rattus, porcupine Hystrix indica, wild boar Sus scrofa, palm civet Paradoxurus hermaphroditus), seedling predators (rabbit Lepus nigricollis, deer Axis axis), and insect/pest predators (ants Crematogaster biroi, Oecophylla smaragdina, mantis Euchomenella indica) were identified. Fruit predation is linked to its age and chemistry. Apart from new insights on flowering phenology, breeding system, pollination and fruiting dynamics, this study demonstrates the vibrant interaction between M. baccifera flowers/fruits and visitors/predators, and provides significant leads towards elucidating the cause of rat multiplication and other events associated with its gregarious flowering.


Asunto(s)
Ciervos , Frutas , Femenino , Masculino , Animales , Abejas , Ratas , Conejos , Fitomejoramiento , Flores , Polinización , Poaceae
4.
Sci Rep ; 12(1): 8177, 2022 05 17.
Artículo en Inglés | MEDLINE | ID: mdl-35581314

RESUMEN

Centellosides viz., asiatic acid, madecassic acid, asiaticoside, madecassoside, are the major bioactive molecules in Centella asiatica. In this study madecassic acid:asiatic acid, madecassoside:asiaticoside (C6-hydroxylation versus non-hydroxylation) and asiaticoside:asiatic acid, madecassoside:madecassic acid (C28-glycoside versus aglycone) ratios in 50 C. asiatica accessions originally collected from their natural habitats in south India and grown under identical ecological conditions for six generations were determined using validated HPTLC-densitometry protocols. Asiatic acid, madecassic acid, asiaticoside and madecassoside contents ranged from 0.00-0.29% (average 0.03 ± 0.06%; 28 accessions recorded asiatic acid content as zero), 0.02-0.72% (0.12 ± 0.13%), 0.04-2.41% (0.44 ± 0.52%) and 0.15-5.27% (1.59 ± 1.26%), respectively. Distinctly, C6-hydroxylated (madecassic acid:asiatic acid 4.00, madecassoside:asiaticoside 3.61) and C28-glycosylated (asiaticoside:asiatic acid 14.67, madecassoside: madecassic acid 13.25) centellosides dominated over the respective non-derivatized entities. Our results infer that both C6-hydroxylation by CYP450-dependent monooxygenases and C28-glycosylation by UDP-Glc glucosyltransferases are dominant bioconversion steps in C. asiatica. Besides, this study discovered six elite lines of C. asiatica, with their (asiaticoside + madecassoside) contents above the industrial benchmark (≥ 4%) from south India. Two elite clones with asiaticoside contents ≥ 2% were also identified. Standardization of the agrotechniques of these elite lines could lead to their industrial applications. Further, this study emphasizes the need for standardizing all four centellosides as biomarkers in C. asiatica raw drugs, pharmaceutical and cosmetic products.


Asunto(s)
Centella , Triterpenos , Glucosiltransferasas , Glicósidos , Extractos Vegetales , Estándares de Referencia
5.
Comb Chem High Throughput Screen ; 25(10): 1672-1681, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-33568028

RESUMEN

BACKGROUND: Over the last few decades, there has been a stupendous change in the area of drug delivery using particulate delivery systems, with increasing focus on nanoparticles in recent times. Nanoparticles help to improve and alter the pharmacodynamic properties and pharmacokinetics of various types of drug molecules. These features help to protect the drug entity in the systemic circulation, access of the drug to the chosen sites, and to deliver the drug in a controlled and sustained rate at the site of action. OBJECTIVE: Nanoparticle based targeted delivery of anti-inflammatory drugs/signal modulatory agents to the cytoplasm or nuclei of the targeted cell can significantly enhance the precision and efficacy of intended therapeutic activity. To this end, we report ligand free, enhanced intra-nuclear delivery model of anti-inflammatory therapeutics via PDMS nanoparticles. METHODS: PDMS nanoparticles were prepared by sacrificial silica template-based approach and details of their characterization for suitability as a nanoparticle-based delivery material are detailed herein. RESULTS: Biological evaluation for compatibility was carried out and the results showed that the PDMS nanoparticle has no toxicity on RAW 264.7 cells in the concentration range of 10, 20, 40, 60, 80, 100 and 120 µg/mL in culture. Biocompatibility and absence of toxicity were determined by morphological examination and cell viability assays. Drug loading and release kinetics were carried out with the anti-inflammatory drug Diclofenac. CONCLUSION: In this paper, we clearly demonstrate the various aspects of nanoparticle articulation, characterization, effect of their characteristics and their applications as a non-toxic drug delivery molecule for its potential applications in therapeutic delivery of drugs for sustained release.


Asunto(s)
Nanopartículas , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Portadores de Fármacos , Sistemas de Liberación de Medicamentos/métodos , Nanopartículas/uso terapéutico , Preparaciones Farmacéuticas , Dióxido de Silicio
6.
Mini Rev Med Chem ; 21(10): 1237-1268, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33319669

RESUMEN

Breast cancer stands as the most prevalent cancer in women globally, and contributes to the highest percentage of mortality due to cancer-related deaths in women. Paclitaxel (PTX) is heavily relied on as a frontline chemotherapy drug in breast cancer treatment, especially in advanced metastatic cancer. Generation of resistance to PTX often derails clinical management and adversely affects patient outcomes. Understanding the molecular mechanism of PTX resistance is necessary to device methods to aid in overcoming the resistance. Recent studies exploring the mechanism of development of PTX resistance have led to unveiling of a range novel therapeutic targets. PTX resistance pathways that involve major regulatory proteins/RNAs like RNF8/Twist/ROR1, TLR, ErbB3/ErbB2, BRCA1- IRIS, MENA, LIN9, MiRNA, FoxM1 and IRAK1 have expanded the complexity of resistance mechanisms, and brought newer insights into the development of drug targets. These resistance-related targets can be dealt with synthetic/natural therapeutics in combination with PTX. The present review encompasses the recent understanding of PTX resistance mechanisms in breast cancer and possible therapeutic combinations to overcome resistance.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Resistencia a Antineoplásicos/efectos de los fármacos , Paclitaxel/farmacología , Antineoplásicos Fitogénicos/química , Neoplasias de la Mama/metabolismo , Femenino , Humanos , Paclitaxel/química
7.
PLoS One ; 15(6): e0235221, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32584888

RESUMEN

Ficus krishnae stem bark and leaves are used for diabetes treatment in traditional medicines. Stem bark of F. krishnae was sequentially extracted with hexane, methanol and water, and these extracts were tested for their antihyperglyceamic activity by oral glucose tolerance test (OGTT) in overnight fasted glucose loaded normal rats. Hexane extract showed significant glucose lowering activity in OGTT, and the triterpene alcohols (cycloartenol+24-methylenecycloartanol) (CA+24-MCA) were isolated together from it by activity guided isolation and characterized by NMR and mass spectroscopy. The ratio of the chemical constituents CA and 24-MCA in (CA+24-MCA) was determined as 2.27:1.00 by chemical derivatization and gas chromatographic quantification. (CA+24-MCA) in high fat diet-streptozotocin induced type II diabetic rats showed significant antidiabetes activity at 1 mg/kg and ameliorated derailed blood glucose and other serum biochemical parameters. Cytoprotective activity of (CA+24-MCA) from glucose toxicity was evaluated in cultured RIN-5F cells by MTT assay and fluorescent microscopy. (CA+24-MCA) in in vitro studies showed enhanced cell viability in RIN-5F cells and significant protection of beta cells from glucose toxicity. Both in in vivo and in vitro studies (CA+24-MCA) showed enhancement in insulin release from the beta cells. In short term toxicity studies in mice (CA+24-MCA) did not show any conspicuous toxic symptoms. The combination of the phytosterols (CA+24-MCA) obtained through activity guided isolation of the stem bark of F. krishnae showed significant activity, and therefore is a promising candidate for new generation antidiabetes drug development.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Ficus/química , Hipoglucemiantes/uso terapéutico , Fitosteroles/química , Triterpenos/química , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Diabetes Mellitus Experimental/inducido químicamente , Ficus/metabolismo , Prueba de Tolerancia a la Glucosa , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Insulina/metabolismo , Hígado/metabolismo , Masculino , Ratones , Conformación Molecular , Fitosteroles/aislamiento & purificación , Fitosteroles/uso terapéutico , Tallos de la Planta/química , Tallos de la Planta/metabolismo , Ratas , Ratas Wistar , Triterpenos/aislamiento & purificación , Triterpenos/uso terapéutico
8.
Curr Cancer Drug Targets ; 20(1): 33-46, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31560288

RESUMEN

Targeted drug delivery systems gave newer dimensions for safer and more effective use of therapeutic drugs, thus helping in circumventing the issues of toxicity and unintended drug accumulation. These ongoing developments in delivery systems can, in turn, bring back drugs that suffered various limitations, Ellipticine (EPT) being a candidate. EPT derivatives witnessed entry into clinical settings but failed to survive in clinics citing various toxic side effects. A large body of preclinical data deliberates the potency of drug delivery systems in increasing the efficiency of EPT/derivatives while decreasing their toxic side effects. Recent developments in drug delivery systems provide a platform to explore EPT and its derivatives as good clinical candidates in treating tumors. The present review deals with delivery mechanisms of EPT/EPT derivatives as antitumor drugs, in vitro and in vivo, and evaluates the suitability of EPT-carriers in clinical settings.


Asunto(s)
Antineoplásicos/administración & dosificación , Sistemas de Liberación de Medicamentos , Elipticinas/administración & dosificación , Elipticinas/química , Elipticinas/farmacología , Humanos
9.
Nat Prod Res ; 34(16): 2319-2322, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-30475646

RESUMEN

Humboldtia unijuga Bedd., endemic to Agasthyamala in Western Ghats in India, is traditionally used by local Kani tribes for chicken pox, head ache and snake bite. This study reports the isolation of erythrodiol-3-acetate (HU-1) and 2,4-di-tert-butylphenol (HU-2) from H. unijuga roots and their anti-inflammatory and anticancer activities in macrophage, skin and breast cancer cell lines. Effects of HU-1 and HU-2 treatments (50, 100 µg/mL) on gene expression profiles of pro-inflammatory cytokines TNFα, IL-6 and IL-1ß, and apoptosis genes p53 and caspase 7 were studied. HU-2 exerted a significantly superior anti-inflammatory effect compared to HU-1 in all three pro-inflammatory genes. HU-2 showed a superior dose dependent anticancer effect through activation of p53 gene over HU-1 in MCF-7 cells. HU-1 exhibited a dose dependent effect on caspase 7 gene in both cell lines while HU-2 was more effective in A431. HU-2 has potential for development as a novel anti-inflammatory and anticancer agent.


Asunto(s)
Antiinflamatorios/farmacología , Anticarcinógenos/farmacología , Fabaceae/química , Ácido Oleanólico/análogos & derivados , Fenoles/aislamiento & purificación , Antiinflamatorios/aislamiento & purificación , Anticarcinógenos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Apoptosis/genética , Línea Celular Tumoral , Citocinas/efectos de los fármacos , Citocinas/metabolismo , Humanos , India , Macrófagos/efectos de los fármacos , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Fenoles/farmacología , Transcriptoma/efectos de los fármacos
10.
J Ethnopharmacol ; 236: 474-483, 2019 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-30872170

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Centella asiatica (CA) is a medicinal herb traditionally used as a brain tonic in Ayurvedic medicine. Various ethnomedical leads revealed the effective use of CA in the treatment of symptoms associated to oxidative stress and inflammation. AIM OF THE STUDY: The aim of this study was to evaluate the therapeutic ability of CA methanol extract (CAM) in protecting mouse brain and astrocytes from oxidative stress and inflammation induced by Paracetamol, and thus to substantiate the allied traditional/ethnomedical claims of CA. MATERIALS AND METHODS: Chemical profiling of CAM and quantification of its major constituents were carried out by HPTLC-densitometry. Mice were administered with CAM and Paracetamol in various combinations, and oxidative stress parameters (lipid peroxidation, radical scavenging) as well as nitric oxide stress were estimated from isolated mouse brain. Cellular toxicity was investigated by apoptosis/necrosis in primary astrocytes isolated from brain tissues of mouse (which was challenged by CAM/Paracetamol) by flow cytometry and fluorescent microscopy. Expression of inflammatory cytokine mediators (monocyte chemo attractant protein 1, interleukin 1, interferon γ, tumor necrosis factor ß, interleukin 10 and mitogen activated protein kinase 14 gene) in CAM/Paracetamol administered mouse brain tissues was analyzed by real time PCR. Mouse brain tissues challenged by CAM/Paracetamol were also assessed for gross and histopathology. In addition, staining with acridine orange was carried out in C6 cell lines treated with CAM, and viewed under fluorescent microscopy. RESULTS: Paracetamol elicited reactive oxygen species generation was revealed through Ferric Reducing Antioxidant Power (FRAP) activity. CAM reversed the Paracetamol induced free radical and reactive nitrogen species production and increased the scavenging activity which was more pronounced at the higher dose (80 mg/kg b.wt). CAM negated the Paracetamol-induced damage by inhibiting expression of pro-inflammatory cytokines (MCP 1, IL 1, TNF ß), and increasing the expression of the anti-inflammatory cytokine (IL 10) profoundly. Interestingly, MAPK 14 gene expression was decreased gradually and became same as normal control with increase in the dose of CAM. Also, it was evident that CAM protected mouse primary astrocytes from Paracetamol by maintaining a normal morphology. Similarly, apoptosis of primary astrocytes (treated with Paracetamol/CAM) decreased with the increase in CAM dose (80 mg/kg b.wt.) which was evident from flow cytometric data. Severe brain damage in the form of lesions was apparent from the histology of Paracetamol alone treated mouse brain. Whereas, CAM treated together with Paracetamol upturned these lesions. Surprisingly, CAM alone proved to be cytotoxic to C6 Glioma cells. CONCLUSIONS: CAM showed antioxidant and anti-inflammatory effects (which were pronounced at higher doses) against Paracetamol-induced oxidative stress and associated inflammation in mouse brain. The underlying mechanisms may be mediated by inhibiting the pro-inflammatory cytokines TNF ß, IL 1 and MCP 1 via regulation of the antioxidant mediated INF γ and MAPK 14 gene signalling pathways. The major bioactive constituents in CAM are the triterpenoid saponins, asiaticoside and madecassoside. The present results provide pharmacological evidence that CAM acts as an antioxidant and anti-inflammatory agent. Furthermore, this study validates the use of CA as an antioxidant and anti-inflammatory agent in ethnomedicine.


Asunto(s)
Sobredosis de Droga/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Fármacos Neuroprotectores/farmacología , Extractos Vegetales/farmacología , Triterpenos/farmacología , Acetaminofén/toxicidad , Animales , Astrocitos/efectos de los fármacos , Astrocitos/patología , Conducta Animal/efectos de los fármacos , Encéfalo/citología , Encéfalo/efectos de los fármacos , Encéfalo/patología , Células Cultivadas , Centella/química , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Sobredosis de Droga/complicaciones , Sobredosis de Droga/etiología , Humanos , Inflamación/etiología , Inflamación/patología , Masculino , Medicina Ayurvédica , Metanol/química , Ratones , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/uso terapéutico , Cultivo Primario de Células , Triterpenos/aislamiento & purificación
11.
Curr Neuropharmacol ; 17(5): 438-446, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-29676230

RESUMEN

Bacopa monnieri, commonly known as Brahmi, has been extensively used as a neuromedicine for various disorders such as anxiety, depression and memory loss. Chemical characterization studies revealed the major active constituents of the herb as the triterpenoid saponins, bacosides. Bacoside A, the vital neuroprotective constituent, is composed of four constituents viz., bacoside A3, bacopaside II, jujubogenin isomer of bacopasaponin C (bacopaside X) and bacopasaponin C. B. monnieri extracts as well as bacosides successfully establish a healthy antioxidant environment in various tissues especially in the liver and brain. Free radical scavenging, suppression of lipid peroxidation and activation of antioxidant enzymes by bacosides help to attain a physiological state of minimized oxidative stress. The molecular basis of neuroprotective activity of bacosides is attributed to the regulation of mRNA translation and surface expression of neuroreceptors such as AMPAR, NMDAR and GABAR in the various parts of the brain. Bioavailability as well as binding of neuroprotective agents (such as bacosides) to these receptors is controlled by the Blood Brain Barrier (BBB). However, nano conversion of these drug candidates easily resolves the BBB restriction and carries a promising role in future therapies. This review summarizes the neuroprotective functions of B. monnieri extracts as well as its active compounds (bacoside A, bacopaside I) and the molecular mechanisms responsible for these pharmacological activities.


Asunto(s)
Fármacos Neuroprotectores/farmacología , Saponinas/farmacología , Triterpenos/farmacología , Animales , Antioxidantes/farmacología , Bacopa/química , Humanos , Estrés Oxidativo/efectos de los fármacos , Saponinas/química , Triterpenos/química
12.
Nat Prod Res ; 33(1): 122-125, 2019 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29446995

RESUMEN

Phytochemistry of fruits and leaves of the unique bamboo Melocanna baccifera resulted in the isolation of 27 secondary metabolites, including 4-Oxabicyclo[3.2.2]nona-1(7),5,8-triene and Verbacine. Biological activity studies of Verbacine revealed it as an inhibitor of acetylcholinesterase and as cytotoxic against C6 cancer cells.


Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Inhibidores de la Colinesterasa/aislamiento & purificación , Poaceae/metabolismo , Línea Celular Tumoral , Frutas/química , Frutas/metabolismo , Humanos , Fitoquímicos/análisis , Hojas de la Planta/química , Hojas de la Planta/metabolismo , Poaceae/química
13.
Phytomedicine ; 50: 231-237, 2018 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-30466983

RESUMEN

BACKGROUND: Citrus comprises the largest fruit sector worldwide, and its fruit peels are the dominant 'residue' of the industry. Though not profitable, Citrus peels are industrially used for making some byproducts (cattle feed, molasses, ethanol, fiber) and for the extraction of bioactives (flavonoids, essential oils, d-limonene). Still huge amounts of peels are wasted by Citrus industries, juice and other vending sectors. PURPOSE: The biological potentials of these unutilized or 'wasted' Citrus peels are least exploited. Here we tested the anticancer potentials of Citrus medica (2 morphotypes), C. sinensis, C. maxima, C. limon and C. reticulata peels by in vitro assays and in vivo cancer models. METHODS: Chemical profiles of Citrus peel oils and peel extracts were analyzed by gas chromatographic techniques (GC-FID, GC-MS) and HPTLC-densitometry, respectively. Anticancer potentials of Citrus peels (Citrus medica 2 morphotypes, C. sinensis, C. maxima, C. limon and C. reticulata) were evaluated by various in vitro assays (MTT assay, morphological observations, fast halo assay, flow cytometric analysis) and in vivo cancer models. RESULTS: C. reticulata peels (extracts, essential oils) showed significant activity against DLA cell line in MTT assay. We found C. reticulata peel water extract inducing cell cycle arrest of DLA in G0/G1 phase followed by nuclear condensation, membrane blebbing, formation of apoptotic bodies and DNA damage leading to apoptosis. In in vivo experiments, C. reticulata peel extract pre-treated mice were significantly (50%) protected from DLA compared to post-treated mice (33%), without any conspicuous toxic symptoms. Citrus peels have volatiles (essential oils, limonoids) and non-volatiles (mainly polymethoxy flavones) as their bioactive/anticancer constituents. CONCLUSION: Our results encourage the use of Citrus peels, which is wasted in huge amounts, as cancer preventive food additives and as anticancer agents.


Asunto(s)
Antineoplásicos/farmacología , Citrus/química , Frutas/química , Neoplasias Experimentales/tratamiento farmacológico , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Animales , Línea Celular Tumoral , Flavonoides/farmacología , Cromatografía de Gases y Espectrometría de Masas , Limoneno/farmacología , Masculino , Ratones
14.
Nat Prod Res ; 32(22): 2657-2662, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-28925289

RESUMEN

Uvaria narum has been used for gastrointestinal problems, jaundice, fever and skin diseases in traditional and ethnomedical practices. Our preliminary antifungal screening of various leaf extracts of U. narum revealed very good antifungal activity for its acetone extract. Active principle of U. narum leaf acetone extract was isolated by bioactivity-guided fractionation and characterised as a new molecule, 2-E-(2″-oxo-5″-acetoxy cyclopent-3″-en-1″-ylidene) ethyl benzoate, by NMR, IR and mass spectroscopic analyses. This active isolate showed very good activity against the fungal pathogen, Colletotrichum gloeosporioides.


Asunto(s)
Ácido Benzoico/farmacología , Colletotrichum/efectos de los fármacos , Fungicidas Industriales/farmacología , Extractos Vegetales/química , Uvaria/química , Ácido Benzoico/aislamiento & purificación , Ésteres/aislamiento & purificación , Ésteres/farmacología , Fungicidas Industriales/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Hojas de la Planta/química
15.
Sci Rep ; 7(1): 11281, 2017 09 12.
Artículo en Inglés | MEDLINE | ID: mdl-28900277

RESUMEN

Carnivorous plants of the genus Nepenthes supplement their nutrient deficiency by capturing arthropods or by mutualistic interactions, through their leaf-evolved biological traps (pitchers). Though there are numerous studies on these traps, mostly on their prey capture mechanisms, the gas composition inside them remains unknown. Here we show that, Nepenthes unopened pitchers are CO2-enriched 'cavities', when open they emit CO2, and the CO2 gradient around open pitchers acts as a cue attracting preys towards them. CO2 contents in near mature, unopened Nepenthes pitchers were in the range 2500-5000 ppm. Gas collected from inside open N. khasiana pitchers showed CO2 at 476.75 ± 59.83 ppm. CO2-enriched air-streaming through N. khasiana pitchers (at 619.83 ± 4.53 ppm) attracted (captured) substantially higher number of aerial preys compared to air-streamed pitchers (CO2 at 412.76 ± 4.51 ppm). High levels of CO2 dissolved in acidic Nepenthes pitcher fluids were also detected. We demonstrate respiration as the source of elevated CO2 within Nepenthes pitchers. Most unique features of Nepenthes pitchers, viz., high growth rate, enhanced carbohydrate levels, declined protein levels, low photosynthetic capacity, high respiration rate and evolved stomata, are influenced by the CO2-enriched environment within them.


Asunto(s)
Dióxido de Carbono/análisis , Conducta Predatoria , Sarraceniaceae/química , Animales , Carbono/análisis , Nitrógeno/análisis , Compuestos Orgánicos/análisis , Presión Parcial , Sarraceniaceae/ultraestructura
16.
Nat Prod Res ; 31(8): 890-895, 2017 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-27817202

RESUMEN

A new quinolinone alkaloid, Melicodenine I (1), along with five known compounds, bergapten (2), isoevodionol methyl ether (3), isoevodionol (4), ternatin (5), ß-sitosteryl-3-O-ß-D-glucopyranoside (6) and a mixture of ß-sitosterol and stigmasterol were isolated from Melicope denhamii leaves, and their structures were elucidated using 1H NMR, 13C NMR, 2D NMR and UPLC-qToF-MS.


Asunto(s)
Hojas de la Planta/química , Quinolonas/química , Rutaceae/química , 5-Metoxipsoraleno , Alcaloides/química , Alcaloides/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Metoxaleno/análogos & derivados , Metoxaleno/química , Metoxaleno/aislamiento & purificación , Estructura Molecular , Plantas Medicinales/química , Quinolonas/aislamiento & purificación , Sitoesteroles/química , Sitoesteroles/aislamiento & purificación , Estigmasterol/química , Estigmasterol/aislamiento & purificación
17.
Sci Rep ; 6: 26135, 2016 05 19.
Artículo en Inglés | MEDLINE | ID: mdl-27194218

RESUMEN

Melocanna baccifera is a unique bamboo which produces the largest fruits in the grass family. Its gregarious flowering once in 45-50 years in north east India and adjacent regions is a botanical enigma, resulting in a glut of fruits. Proper utilization of M. baccifera fruits is not extant, and huge quantities of fruits are left underexploited due to lack of scientific information on their chemical composition and nutritional potential. Here we report the nutritional properties of M. baccifera fruits, and the ecological significance of its fruiting. This pear-shaped, fleshy bamboo fruit is rich in amino acids (lysine, glutamic acid), sugars (sucrose, glucose, fructose) and phenolics (ferulic acid). Protein content (free, bound) in M. baccifera fruits is very low. Fruits are rich in saturated fatty acids (palmitic acid), minerals (potassium), and only B series vitamins (B3) are detected in them. Rat feeding experiments showed that M. baccifera fruit alone is not a complete food, but with other protein supplements, it is a valuable food additive. This study could lead to better utilization of M. baccifera fruits during future flowering/fruiting events. These results could also help in the successful management of rodent outbreaks and other ecological problems associated with M. baccifera fruiting.


Asunto(s)
Análisis de los Alimentos , Frutas/química , Poaceae/química , Aminoácidos/análisis , Ácidos Grasos/análisis , India , Minerales/análisis , Fenoles/análisis , Proteínas/análisis , Azúcares/análisis , Vitaminas/análisis
18.
Nat Prod Res ; 30(19): 2197-203, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-26979490

RESUMEN

A new pentacyclic triterpenoid fatty acid ester, lupan-20-ol-3(ß)-yl hexadecanoate (1), together with lupan-20-ol-3(ß)-yl acetate (2), olean-18-en-3(ß)-yl hexadecanoate (3), dotriacontanoic acid (4), stigmasterol (5), rubiadin (6), nonadecanoic acid (7), palmitic acid (8) and camptothecin (9) were isolated from the hexane and chloroform extracts of Ophiorrhiza shendurunii from South India. Structures of the isolates were determined by (1)H, (13)C, (13)C DEPT, (1)H-(1)H COSY, HMBC, HSQC, NOESY NMR, FT-IR, DART-MS, ESI-MS, alkaline hydrolysis, derivatisation, GC-MS and HPTLC analyses. O. shendurunii hexane and chloroform extracts showed significant activities against Candida albicans and Fusarium oxysporum. Compounds 1 to 3 showed only moderate antiyeast/antifungal activities.


Asunto(s)
Antifúngicos/aislamiento & purificación , Rubiaceae/química , Triterpenos/aislamiento & purificación , Antifúngicos/farmacología , Evaluación Preclínica de Medicamentos/métodos , Ácidos Grasos/química , Cromatografía de Gases y Espectrometría de Masas , Hexanos/química , Hidrólisis , India , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Espectrometría de Masa por Ionización de Electrospray , Espectroscopía Infrarroja por Transformada de Fourier , Triterpenos/química , Triterpenos/farmacología
19.
Nat Prod Res ; 30(17): 1965-8, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26456637

RESUMEN

Volatile oil from fresh rhizomes of Zingiber anamalayanum was isolated by hydrodistillation and characterised by GC-FID and GC-MS. Twenty-one out of 24 constituents comprising 99.47% of the oil were identified. Major components in Z. anamalayanum rhizome oil were δ-2-carene (52.83%), camphene (9.83%), endo-fenchol (9.42%), iso-dihydrocarveol (6.44%) and cis-p-mentha-2,8-dien-1-ol (5.19%). Monoterpene hydrocarbons in the rhizome oil were 65.81%, followed by oxygenated monoterpenes (23.78%) and sesquiterpene hydrocarbons (9.87%). Physical parameters of rhizome oil were [Formula: see text] 1.4031, [Formula: see text] - 16.097(o) (c = 1, CHCl3) and [Formula: see text] 0.9202. Z. anamalayanum rhizome oil showed significant anti-Dalton's Lymphoma Ascitic activity.


Asunto(s)
Aceites Volátiles/farmacología , Rizoma/química , Zingiberaceae , Antioxidantes/química , Monoterpenos Bicíclicos , Canfanos , Proliferación Celular/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Humanos , India , Linfoma/patología , Monoterpenos/análisis , Norbornanos/análisis , Aceites Volátiles/química , Sesquiterpenos/análisis , Terpenos/análisis
20.
Sci Rep ; 5: 11078, 2015 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-26058043

RESUMEN

Mucuna pruriens is the best known natural source of L-dopa, the gold standard for treatment of Parkinsonism. M. pruriens varieties are protein rich supplements, and are used as food and fodder worldwide. Here, we report L-dopa contents in seeds of fifty six accessions of four M. pruriens varieties, M. pruriens var. pruriens, M. pruriens var. hirsuta, M. pruriens var. utilis and M. pruriens var. thekkadiensis, quantified by HPTLC-densitometry. L-dopa contents varied between 0.58 to 6.42 (%, dr. wt.). High and low L-dopa yielding genotypes/chemotypes of M. pruriens could be multiplied for medicinal and nutritional purposes, respectively. HPTLC profiles of M. pruriens seeds on repeated extraction (24 h) in 1:1 formic acid-alcohol followed by development in butanol:acetic acid:water (4:1:1, v/v) showed consistent degradation of L-dopa (Rf 0.34 ± 0.02) into a second peak (Rf 0.41 ± 0.02). An average of 52.11% degradation of L-dopa was found in seeds of M. pruriens varieties. Since M. pruriens seeds and/or L-dopa are used for treatment of Parkinson's disease and as an aphrodisiac both in modern and/or traditional systems of medicine, the finding of high level of L-dopa degradation (in pure form and in M. pruriens extracts) into damaging quinones and ROS is very significant.


Asunto(s)
Levodopa/metabolismo , Mucuna/metabolismo , Biodegradación Ambiental , Cromatografía en Capa Delgada , Hidrólisis
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