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1.
Pak J Biol Sci ; 26(7): 371-379, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37902078

RESUMO

<b>Background and Objective:</b> Isolation and investigation of plant growth promoting bacteria on potato plants can provide significant information for the application of beneficial bacteria in potato production. This study aims to isolate and characterize endophytic bacteria isolated from potato roots. In addition, the potential application of endophytes in promoting potato growth under <i>in vitro</i> conditions was also investigated. <b>Materials and Methods:</b> The roots from 15 healthy potato plants were excised and surface sterilized by NaOCl and finally rinsed by sterilized water. The confirmed surface-sterilized roots were then aseptically cut into small fragments and spread onto the isolation media, followed by incubation at 27°C for up to 3 days. Six isolates that showed differences in colony morphology were selected for further investigation. All isolates were screened for IAA production, nitrogen fixation, and phosphate solubilization. <b>Results:</b> Five of the isolates were identified as <i>Bacillus</i> and isolate 30 was identified as <i>Paenibacillus alvei</i>. All isolates exhibited good IAA production. While Iso-27 had no nitrogen fixation activity, Iso-28 showed the highest level of nitrogen fixation activity (3.59 mg L<sup>1</sup>), four isolates (Iso-9, Iso-10, Iso-11, Iso-28) could solubilize phosphate, ranging from 49.64 g L<sup>1</sup> to 67.98 mg L<sup>1</sup>. After being inoculated with <i>in vitro</i> potato plants, isolates 9, 10, 28, 30, improved the stalk length, root number, fresh mass and dried mass of the potato plants. <b>Conclusion:</b> The four isolates can potentially be applied in <i>in vitro</i> potato culture.


Assuntos
Bacillus , Solanum tuberosum , Ácidos Indolacéticos , Desenvolvimento Vegetal , Fosfatos
2.
Chemosphere ; 343: 139891, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37604337

RESUMO

Cynodon dactylon, an invasive species, exhibits its robust adaptability, reproduction and nutrient regime against the local species. Taking advantage of this harmful grass as a raw precursor to produce valuable materials for wastewater treatment has paid much attention. Herein, we report on the fabrication of Cynodom dactylon derived MgFe2O4@AC with a main goal of effective removal of ciprofloxacin antibiotic from water. Our findings showed that MgFe2O4@ACK1 composites attained mesoporous textures, high specific surface areas (884.3-991.6 m2 g-1), and MgFe2O4-20%@ACK1 was the most effective with a very high removal efficiency of 96.7%. The Elovich model was suitable for describing the kinetic of adsorption with (Radj)2 of 0.9988. Meanwhile, the isotherm data obeyed the Langmuir model corresponding to (Radj)2 of 0.9993. Qmax value of MgFe2O4-20%@ACK1 was determined at 211.67 mg g-1. The proposed adsorption mechanism primarily comprises five routes as follows, (i) pore-filling, (ii) π-π interaction, (iii) electrostatic interaction, (iv) hydrogen bonding, and (v) hydrophobic interaction. MgFe2O4-20%@ACK1 adsorbent could reuse with three cycles. We recommend that MgFe2O4/ACs derived from Cynodom dactylon could be high-efficiency adsorbents for the elimination of antibiotics.


Assuntos
Ciprofloxacina , Poluentes Químicos da Água , Cynodon , Poaceae , Carvão Vegetal/química , Poluentes Químicos da Água/análise , Antibacterianos , Adsorção , Cinética
3.
Chem Zvesti ; 76(9): 5655-5675, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35669698

RESUMO

Distichochlamys citrea M.F. Newman (commonly known as "Black Ginger") is an endemic plant to Vietnam and has been extensively exploited by folk medication for treatments of infection-related diseases and diabetes. In this work, its rhizomes were subjected to fractionated extraction, phytochemical examination, evaluation of antioxidant effect by DDPH free radical neutralization, and inhibitory activity toward α-glucosidase. The compositional components were subjected to in silico screening, including density functional theory calculation, molecular docking simulation, physicochemical analysis, and pharmacokinetic regression. In the trials, EtOAc fraction is found as the bioactive part of most effectiveness, regarding both antioxidant effect (IC50 = 90.27 µg mL-1) and α-glucosidase inhibitory activity (IC50 = 115.75 µg mL-1). Chemical determination reveals there are 13 components of its composition. DFT-based calculations find no abnormal constraints in their structures. Docking-based simulation provides order of inhibitory effectiveness: 3-P53341 > 12-P53341 > 7-P53341 > 4-P53341 > 11-P53341 > 10-P53341. QSARIS-based investigations implicate their biocompatibility. ADMET-based regressions indicate that all candidates are generally safe for medicinal applications. The findings would contribute to the basis for further studies on the chemical compositions of Distichochlamys citrea and their biological activities. Supplementary Information: The online version contains supplementary material available at 10.1007/s11696-022-02273-2.

4.
Nat Prod Res ; 36(24): 6232-6239, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34989301

RESUMO

Using combined chromatographic separation techniques, three new triterpenoids named lycomclavatols A-C (1-3), a new natural product, methyl lycernuate-A (4), as well as seven known compounds (5-11), were isolated from the methanol extract of the whole plants of Lycopodium clavatum. Their chemical structures were established based on 1 D/2D NMR and HR-ESI-MS spectroscopic analyses. Among the isolates, compound 1 exhibited inhibitory activity on NO production in LPS-stimulated BV2 cells (IC50 = 36.0 µM). In addition, 1 was cytotoxic against both HepG2 and A549 cancer cell lines, with IC50 values of 40.7 and 87.0 µM, respectively. Compounds 10 and 11 showed cytotoxicity on only HepG2 and A549 cells, with IC50 values of 91.2 and 57.6 µM, respectively. Our results contribute to understanding more the secondary metabolites produced by L. clavatum and provide a scientific rationale for further investigations of anti-inflammatory and anticancer effects for this valuable medicinal plant.


Assuntos
Lycopodium , Plantas Medicinais , Triterpenos , Lycopodium/química , Triterpenos/farmacologia , Triterpenos/química , Óxido Nítrico/metabolismo , Plantas Medicinais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Concentração Inibidora 50
5.
Environ Res ; 208: 112683, 2022 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-35016870

RESUMO

This research was performed to evaluate the silver nanoparticles (AgNPs) fabricating potential of aqueous shoot extract of Aristolochia bracteolata and also assess the free radicals scavenging potential of synthesized AgNPs. The results obtained from this study showed that the aqueous shoot extract of A. bracteolata has the potential to synthesize the AgNPs and it was initially confirmed by color change in the reaction blend as yellow to dark brownish. Subsequently, a clear absorbance peak was found at 425 nm in UV-visible spectrum analysis. The functional groups involved in the capping and stabilization of AgNPs were confirmed by Fourier Transform-Infrared spectroscopy (FTIR) analysis and recorded about 10 sharp peaks 3688, 3401, 2980, 2370, 1948, 1642, 1480, 1280, 782, and 628 cm-1. The Scanning Electron Microscope (SEM) and Transmission Electron Microscope (TEM) observations revealed that the predominant shape of the AgNPs was spherical and size ranged from 41.43 to 60.51 nm. Interestingly, the green fabricated AgNPs showed significant free radicals scavenging activity and were confirmed with ferric reducing assay, 1, 1-diphenyl-2-picryl-hydrazyl (DPPH), H2O2 radicals, and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals scavenging activity. Thus, after a few in-vivo antioxidant studies, Aristolochia bracteolata-mediated AgNPs can be considered as an antioxidant agent.


Assuntos
Aristolochia , Nanopartículas Metálicas , Antioxidantes , Peróxido de Hidrogênio , Nanopartículas Metálicas/química , Extratos Vegetais , Prata/química , Espectroscopia de Infravermelho com Transformada de Fourier
6.
West J Nurs Res ; 43(6): 551-562, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-32942949

RESUMO

Interventions are needed to address physical and psychological health in middle-aged and older African Americans (AAs). The purpose of this pilot study was to evaluate the feasibility and potential benefits of an eight-week Qigong exercise on physical ability and function, balance, frailty, depression and anxiety, and spiritual well-being in AAs using a single-group design. Fifteen AAs with a mean age of 64 years received Qigong exercise over 16 semi-weekly, one-hour sessions. The majority were female (93.3%) and college-level educated (53.3%). Repeat chair stands, physical function, and spiritual well-being improved significantly (p < .05) with effect sizes ranging from .45 to .87. Over 52% of participants showed improved depression scores, fast gait speed, and standing balance. Nearly 42% demonstrated some frailty improvement over baseline. No adverse events were reported. Qigong exercise potentially improves the physical ability and function, and spiritual well-being of AAs and needs further testing in a randomized clinical trial.


Assuntos
Qigong , Negro ou Afro-Americano , Idoso , Exercício Físico , Feminino , Humanos , Masculino , Saúde Mental , Pessoa de Meia-Idade , Projetos Piloto
7.
J Food Biochem ; 43(8): e12936, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31368557

RESUMO

Antrodia cinnamomea or Antrodia camphorata is a distinctive mushroom of Taiwan, which is being used as a traditional medicine to treat various health-related conditions. More than 78 compounds have been identified in A. cinnamomea. Large numbers of phytochemical studies have been carried out in A. cinnamomea due to the high amount of terpenoids. Besides that, the extracts and active components of A. cinnamomea were reported to have various biological activities including hepatoprotective, antihypertensive, antihyperlipidemic, anti-inflammatory, antioxidant, antitumor, and immunomodulatory activities. In this review article, we have summarized the recent findings of A. cinnamomea and its molecular mechanisms of action in various disease models. PRACTICAL APPLICATIONS: A. cinnamomea, medicinal fungus used in traditional medicine in Taiwan also possess high market value. Aim of the present review is to highlight the compounds present in A. cinnamomea and their different pharmacological activities in preventing/cure various diseases/disorders. A. cinnamomea can be potentially developed into health foods or drugs.


Assuntos
Agaricales/química , Antrodia/química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Taiwan
8.
BMC Pediatr ; 19(1): 53, 2019 02 11.
Artigo em Inglês | MEDLINE | ID: mdl-30744649

RESUMO

BACKGROUND: Prevalence of hemolytic neonatal hyperbilirubinemia (NHB) is not well characterized, and economic burden at the population level is poorly understood. This study evaluated the prevalence, clinical characteristics, and economic burden of hemolytic NHB newborns receiving treatment in U.S. real-world settings. METHODS: This cohort study used administrative claims from 01/01/2011 to 08/31/2017. The treated cohort had hemolytic NHB diagnosis and received phototherapy, intravenous immunoglobulin, and/or exchange transfusions. They were matched with non-NHB newborns who had neither NHB nor related treatments on the following: delivery hospital/area, gender, delivery route, estimated gestational age (GA), health plan eligibility, and closest date of birth within 5 years. Inferential statistics were reported. RESULTS: The annual NHB prevalence was 29.6 to 31.7%; hemolytic NHB, 1.8 to 2.4%; treated hemolytic NHB, 0.46 to 0.55%, between 2011 and 2016. The matched analysis included 1373 pairs ≥35 weeks GA. The treated hemolytic NHB cohort had significantly more birth trauma and hemorrhage (4.5% vs. 2.4%, p = 0.003), vacuum extractor affecting newborn (1.9% vs. 0.8%, p = 0.014), and polycythemia neonatorum (0.8% vs. 0%, p = 0.001) than the matched non-NHB cohort. The treated hemolytic NHB cohort also had significantly longer mean birth hospital stays (4.5 vs. 3.0 days, p < 0.001), higher level 2-4 neonatal intensive care admissions (15.7% vs. 2.4, 15.9% vs. 2.8 and 10.6% vs. 2.5%, respectively, all p < 0.001) and higher 30-day readmission (8.7% vs. 1.7%, p < 0.001). One-month and one-year average total costs of care were significantly higher for the treated hemolytic NHB cohort vs. the matched non-NHB cohort, $14,405 vs. $5527 (p < 0.001) and $21,556 vs. $12,986 (p < 0.001), respectively. The average costs for 30-day readmission among newborns who readmitted were $13,593 for the treated hemolytic NHB cohort and $3638 for the matched non-NHB cohort, p < 0.001. The authors extrapolated GA-adjusted prevalence of treated hemolytic NHB in the U.S. newborn population ≥ 35 weeks GA and estimated an incremental healthcare expenditure of $177.0 million during the first month after birth in 2016. CONCLUSIONS: The prevalence of treated hemolytic NHB was 4.6-5.5 patients per 1000 newborns. This high-risk hemolytic NHB imposed substantial burdens of healthcare resource utilization and incremental costs on newborns, their caregivers, and the healthcare system.


Assuntos
Efeitos Psicossociais da Doença , Hiperbilirrubinemia Neonatal/economia , Hiperbilirrubinemia Neonatal/epidemiologia , Adulto , Cuidados Críticos/economia , Transfusão Total/estatística & dados numéricos , Utilização de Instalações e Serviços , Feminino , Idade Gestacional , Custos de Cuidados de Saúde/estatística & dados numéricos , Humanos , Hiperbilirrubinemia Neonatal/terapia , Imunoglobulinas Intravenosas/uso terapêutico , Recém-Nascido , Cobertura do Seguro , Unidades de Terapia Intensiva Neonatal/economia , Tempo de Internação/economia , Masculino , Readmissão do Paciente/economia , Fototerapia/estatística & dados numéricos , Prevalência , Estudos Retrospectivos , Estados Unidos/epidemiologia
9.
Nat Prod Res ; 33(6): 796-802, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29210295

RESUMO

This study describes the chemical constituents of Oldenlandia pinifolia (Wall. Ex G. Don) Kuntze (synonym Hedyotis pinifolia Wall. Ex G. Don) and discusses their anti-proliferative activities. Thirteen compounds were isolated from the n-hexane, ethyl acetate and n-butanol extracts of whole plants O. pinifolia by chromatography method. Their structures were elucidated using MS and NMR analysis and compared with reported data. They are three anthraquinones, a carotenoid, two triterpenes, four iridoid glycosides and three flavonoid glycosides. Among them, 2-methyl-1,4,6-trihydroxy-anthraquinone is a new one, and three compounds were found for the first time in this genus. MTT assay resulted that the n-butanol extract and four isolated compounds inhibited the proliferation of chronic myelogenous leukaemia cells. The results from Hoechst 33343 staining and caspase 3-inducing exhibited that those four tested compounds induced apoptosis and activated caspase 3 (p < 0.05). One of them, isorhamnetin-3-O-ß-rutinoside showed the most activity with IC50 value of 394.68 ± 25.12 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Dissacarídeos/farmacologia , Flavonoides/farmacologia , Oldenlandia/química , Extratos Vegetais/química , Antraquinonas/isolamento & purificação , Antraquinonas/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Dissacarídeos/isolamento & purificação , Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Humanos , Células K562 , Células KB , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Vietnã
10.
Front Pharmacol ; 9: 220, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29593542

RESUMO

Flavonoids, present in fruits, vegetables and traditional medicinal plants, show anticancer effects in experimental systems and are reportedly non-toxic. This is a favorable property for long term strategies for the attenuation of lymph node metastasis, which may effectively improve the prognostic states in breast cancer. Hence, we studied two flavonoids, apigenin and luteolin exhibiting strong bio-activity in various test systems in cancer research and are readily available on the market. This study has further advanced the mechanistic understanding of breast cancer intravasation through the lymphatic barrier. Apigenin and luteolin were tested in a three-dimensional (3-D) assay consisting of MDA-MB231 breast cancer spheroids and immortalized lymph endothelial cell (LEC) monolayers. The 3-D model faithfully resembles the intravasation of breast cancer emboli through the lymphatic vasculature. Western blot analysis, intracellular Ca2+ determination, EROD assay and siRNA transfection revealed insights into mechanisms of intravasation as well as the anti-intravasative outcome of flavonoid action. Both flavonoids suppressed pro-intravasative trigger factors in MDA-MB231 breast cancer cells, specifically MMP1 expression and CYP1A1 activity. A pro-intravasative contribution of FAK expression in LECs was established as FAK supported the retraction of the LEC monolayer upon contact with cancer cells thereby enabling them to cross the endothelial barrier. As mechanistic basis, MMP1 caused the phosphorylation (activation) of FAK at Tyr397 in LECs. Apigenin and luteolin prevented MMP1-induced FAK activation, but not constitutive FAK phosphorylation. Luteolin, unlike apigenin, inhibited MMP1-induced Ca2+ release. Free intracellular Ca2+ is a central signal amplifier triggering LEC retraction through activation of the mobility protein MLC2, thereby enhancing intravasation. FAK activity and Ca2+ levels did not correlate. This implicates that the pro-intravasative contribution of FAK and of Ca2+ release in LECs was independent of each other and explains the better anti-intravasative effects of luteolin in vitro. In specific formulations, flavonoid concentrations causing significant anti-intravasative effects, can certainly be achieved in vivo. As the therapeutic strategy has to be based on permanent flavonoid treatment both the beneficial and adverse effects have to be investigated in future studies.

11.
Food Chem Toxicol ; 111: 114-124, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29129665

RESUMO

Mechanisms how colorectal cancer (CRC) cells penetrate blood micro-vessel endothelia and metastasise is poorly understood. To study blood endothelial cell (BEC) barrier breaching by CRC emboli, an in vitro assay measuring BEC-free areas underneath SW620 cell spheroids, so called "circular chemorepellent induced defects" (CCIDs, appearing in consequence of endothelial retraction), was adapted and supported by Western blotting, EIA-, EROD- and luciferase reporter assays. Inhibition of ALOX12 or NF-κB in SW620 cells or BECs, respectively, caused attenuation of CCIDs. The FDA approved drugs vinpocetine [inhibiting ALOX12-dependent 12(S)-HETE synthesis], ketotifen [inhibiting NF-κB], carbamazepine and fenofibrate [inhibiting 12(S)-HETE and NF-κB] significantly attenuated CCID formation at low µM concentrations. In the 5-FU-resistant SW620-R/BEC model guanfacine, nifedipine and proadifen inhibited CCIDs stronger than in the naïve SW620/BEC model. This indicated that in SW620-R cells formerly silent (yet unidentified) genes became expressed and targetable by these drugs in course of resistance acquisition. Fenofibrate, and the flavonoids hispidulin and apigenin, which are present in medicinal plants, spices, herbs and fruits, attenuated CCID formation in both, naïve- and resistant models. As FDA-approved drugs and food-flavonoids inhibited established and acquired intravasative pathways and attenuated BEC barrier-breaching in vitro, this warrants testing of these compounds in CRC models in vivo.


Assuntos
Neoplasias Colorretais/patologia , Células Endoteliais/fisiologia , Endotélio Vascular/fisiologia , Flavonoides/farmacologia , Esferoides Celulares/fisiologia , Araquidonato 12-Lipoxigenase/genética , Araquidonato 12-Lipoxigenase/metabolismo , Bloqueadores dos Canais de Cálcio/farmacologia , Feminino , Regulação da Expressão Gênica/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica , Humanos , NF-kappa B/genética , NF-kappa B/metabolismo , Metástase Neoplásica/fisiopatologia , Preparações Farmacêuticas
12.
Plant Biotechnol (Tokyo) ; 35(4): 341-348, 2018 Dec 25.
Artigo em Inglês | MEDLINE | ID: mdl-31892821

RESUMO

Grey mangrove (Avicennia marina) is a traditional medicine used for the treatment of various diseases, including rheumatism and ulcers; however, the compounds responsible for its curative effects remain largely unknown. Triterpenoids are a diverse group of plant-specialized metabolites derived from a common precursor, 2,3-oxidosqualene. Triterpenoids are potentially responsible for the beneficial effects of A. marina; however, the chemical profiles of triterpenoids in A. marina and their biosynthetic genes have not been identified. Cytochrome P450 monooxygenases (P450s) have key roles in the structural diversification of plant triterpenoids by catalyzing site-specific oxidation of triterpene scaffolds. Recent studies have revealed that the CYP716 family represents the most common clade of P450s involved in triterpenoid biosynthesis. In this study, we performed triterpenoid profiling and RNA sequencing of A. marina leaves. Mining of CYP716 family genes and enzymatic activity assays of encoded proteins revealed that CYP716A259 catalyzed oxidation at the C-28 position of the pentacyclic triterpene skeletons of ß-amyrin, α-amyrin, and lupeol to produce oleanolic acid, ursolic acid, and betulinic acid, respectively. The other functionally defined P450, CYP716C53, catalyzed the C-2α hydroxylation of oleanolic acid and ursolic acid to produce maslinic acid and corosolic acid, respectively. The possible involvement of CYP716A259 and CYP716C53 in the biosynthesis of these health-benefiting compounds in A. marina leaves, and the possible contribution of the resulting compounds to the reported bioactivities of A. marina leaf extract, are discussed.

13.
Phytother Res ; 30(12): 2044-2052, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27654887

RESUMO

Aging-related neurodegenerative diseases, such as Parkinson's disease (PD) or related disorders, are an increasing societal and economic burden worldwide. Δ9-Tetrahydrocannabinol (THC) is discussed as a neuroprotective agent in several in vitro and in vivo models of brain injury. However, the mechanisms by which THC exhibits neuroprotective properties are not completely understood. In the present study, we investigated neuroprotective mechanisms of THC in glutamate-induced neurotoxicity in primary murine mesencephalic cultures, as a culture model for PD. Glutamate was administered for 48 h with or without concomitant THC treatment. Immunocytochemistry staining and resazurin assay were used to evaluate cell viability. Furthermore, superoxide levels, caspase-3 activity, and mitochondrial membrane potential were determined to explore the mode of action of this compound. THC protected dopaminergic neurons and other cell types of primary dissociated cultures from glutamate-induced neurotoxicity. Moreover, THC significantly counteracted the glutamate-induced mitochondrial membrane depolarization and apoptosis. SR141716A, a CB1 receptor antagonist, concentration-dependently blocked the protective effect of THC in primary mesencephalic cultures. In conclusion, THC exerts anti-apoptotic and restores mitochondrial membrane potential via a mechanism dependent on CB1 receptor. It strengthens the fact that THC has a benefit on degenerative cellular processes occurring, among others, in PD and other neurodegenerative diseases by slowing down the progression of neuronal cell death. Copyright © 2016 John Wiley & Sons, Ltd.


Assuntos
Potencial da Membrana Mitocondrial/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Receptor CB1 de Canabinoide/uso terapêutico , Animais , Morte Celular , Feminino , Camundongos , Doença de Parkinson , Gravidez , Receptor CB1 de Canabinoide/administração & dosagem
14.
Bioorg Med Chem Lett ; 26(16): 3913-7, 2016 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-27423477

RESUMO

Five new compounds, named ancistronaphtosides A and B (1 and 2), anciscochine (3), anciscochine 6-O-ß-d-glucopyranoside (4), and 4'-methoxy-5-epi-ancistecrorine A1 (5), together with tortoside A (6) and 4-hydroxy-2-methoxyphenyl-6-O-syringoyl-ß-d-glucopyranoside (7) were isolated from the methanolic extract of Ancistrocladus cochinchinensis. Their chemical structures were established using HR-ESI-MS, NMR spectroscopic, and chiroptical methods. Compound 5 significantly exhibited anti-proliferation against HL-60, LU-1, and SK-MEL-2 cells with IC50 values of 5.0±1.2, 6.5±1.6, and 6.8±2.0µg/mL, respectively.


Assuntos
Alcaloides/química , Antineoplásicos Fitogênicos/química , Isoquinolinas/química , Magnoliopsida/química , Naftalenos/química , Alcaloides/isolamento & purificação , Alcaloides/toxicidade , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/toxicidade , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Células HL-60 , Humanos , Espectroscopia de Ressonância Magnética , Magnoliopsida/metabolismo , Conformação Molecular , Naftalenos/isolamento & purificação , Naftalenos/toxicidade , Neoplasias/metabolismo , Neoplasias/patologia , Extratos Vegetais/química , Espectrometria de Massas por Ionização por Electrospray
15.
Phytomedicine ; 22(9): 862-74, 2015 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-26220634

RESUMO

BACKGROUND: The t(2;5)(p23;q35) chromosomal translocation results in the expression of the fusion protein NPM/ALK that when expressed in T-lymphocytes gives rise to anaplastic large cell lymphomas (ALCL). In search of new therapy options the dichloromethane extract of the ethnomedicinal plant Neurolaena lobata (L.) R.Br. ex Cass was shown to inhibit NPM/ALK expression. PURPOSE: Therefore, we analysed whether the active principles that were recently isolated and found to inhibit inflammatory responses specifically inhibit growth of NPM/ALK+ ALCL, leukaemia and breast cancer cells, but not of normal cells, and the intravasation through the lymphendothelial barrier. METHODS: ALCL, leukaemia and breast cancer cells, and normal peripheral blood mononuclear cells (PBMCs) were treated with isolated sesquiterpene lactones and analysed for cell cycle progression, proliferation, mitochondrial activity, apoptosis, protein and mRNA expression, NF-κB and cytochrome P450 activity, 12(S)-HETE production and lymphendothelial intravasation. RESULTS: In vitro treatment of ALCL by neurolenin B suppressed NPM/ALK, JunB and PDGF-Rß expression, inhibited the growth of ALCL cells late in M phase, and induced apoptosis via caspase 3 without compromising mitochondrial activity (as a measure of general exogenic toxicity). Moreover, neurolenin B attenuated tumour spheroid intravasation probably through inhibition of NF-κB and CYP1A1. CONCLUSION: Neurolenin B specifically decreased pro-carcinogenic NPM/ALK expression in ALK+ ALCL cells and, via the inhibition of NF-kB signalling, attenuated tumour intra/extravasation into the lymphatics. Hence, neurolenin B may open new options to treat ALCL and to manage early metastatic processes to which no other therapies exist.


Assuntos
Asteraceae/química , Lactonas/farmacologia , Linfoma Anaplásico de Células Grandes/patologia , NF-kappa B/metabolismo , Proteínas Tirosina Quinases/metabolismo , Sesquiterpenos de Germacrano/farmacologia , Sesquiterpenos/farmacologia , Apoptose , Ciclo Celular , Linhagem Celular Tumoral/efeitos dos fármacos , Proliferação de Células , Humanos , Leucócitos Mononucleares/efeitos dos fármacos , Estrutura Molecular , Plantas Medicinais/química , Transdução de Sinais
16.
Mutat Res ; 777: 79-90, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25989051

RESUMO

Pluchea odorata is ethno pharmaceutically used to treat inflammation-associated disorders. The dichloromethane extract (DME) was tested in the carrageenan-induced rat paw oedema assay investigating its effect on inflammation that was inhibited by 37%. Also an in vitro anti-neoplastic potential was reported. However, rather limited information about the bio-activity of purified compounds and their cellular mechanisms are available. Therefore, two of the most abundant eudesmanes in P. odorata were isolated and their anti-neoplastic and anti-intravasative activities were studied. HL-60 cells were treated with P. odorata compounds and metabolic activity, cell number reduction, cell cycle progression and apoptosis induction were correlated with relevant protein expression. Tumour cell intravasation through lymph endothelial monolayers was measured and potential causal mechanisms were analyzed by Western blotting. Compound PO-1 decreased the metabolic activity of HL-60 cells (IC50 = 8.9 µM after 72 h) and 10 µM PO-1 induced apoptosis, while PO-2 showed just weak anti-neoplastic activities at concentrations beyond 100 µM. PO-1 arrested the cell cycle in G1 and this correlated with induction of JunB expression. Independent of this mechanism 25 µM PO-1 decreased MCF-7 spheroid intravasation through the lymph endothelial barrier. Hence, PO-1 inhibits an early step of metastasis, impairs unrestricted proliferation and induces apoptosis at low micromolar concentrations. These results warrant further testing in vivo to challenge the potential of PO-1 as novel lead compound.


Assuntos
Apoptose/efeitos dos fármacos , Asteraceae/química , Proliferação de Células/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sesquiterpenos de Eudesmano/farmacologia , Animais , Antineoplásicos Fitogênicos/farmacologia , Ciclo Celular/efeitos dos fármacos , Células HL-60 , Humanos , Concentração Inibidora 50 , Masculino , Ratos , Ratos Sprague-Dawley , Saponinas/farmacologia , Espirostanos/farmacologia
17.
PLoS Pathog ; 3(10): 1530-9, 2007 Oct 26.
Artigo em Inglês | MEDLINE | ID: mdl-17967062

RESUMO

The development of multidrug-resistant viruses compromises antiretroviral therapy efficacy and limits therapeutic options. Therefore, it is an ongoing task to identify new targets for antiretroviral therapy and to develop new drugs. Here, we show that an indole derivative (IDC16) that interferes with exonic splicing enhancer activity of the SR protein splicing factor SF2/ASF suppresses the production of key viral proteins, thereby compromising subsequent synthesis of full-length HIV-1 pre-mRNA and assembly of infectious particles. IDC16 inhibits replication of macrophage- and T cell-tropic laboratory strains, clinical isolates, and strains with high-level resistance to inhibitors of viral protease and reverse transcriptase. Importantly, drug treatment of primary blood cells did not alter splicing profiles of endogenous genes involved in cell cycle transition and apoptosis. Thus, human splicing factors represent novel and promising drug targets for the development of antiretroviral therapies, particularly for the inhibition of multidrug-resistant viruses.


Assuntos
Antirretrovirais/farmacologia , Farmacorresistência Viral/genética , HIV/efeitos dos fármacos , Indóis/farmacologia , Isoquinolinas/farmacologia , Precursores de RNA/efeitos dos fármacos , Splicing de RNA/efeitos dos fármacos , Carbazóis/farmacologia , Avaliação Pré-Clínica de Medicamentos , Ensaio de Imunoadsorção Enzimática , HIV/genética , Humanos , Leucócitos Mononucleares/virologia , Macrófagos/virologia , RNA Viral/efeitos dos fármacos , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Replicação Viral/efeitos dos fármacos
18.
J Ethnopharmacol ; 81(3): 337-42, 2002 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-12127234

RESUMO

A chromogenic bioassay was utilized to determine the antithrombin activity of the methylene chloride and methanol extracts prepared from forty-five plants of Russia. Mouse leukemia cells (L1210) were utilized to screen these extracts for activity against cancer. The results indicated that eight plant extracts demonstrated 90% or higher activity in the inhibition of thrombin. Also, nine methanol extracts demonstrated activity of 90% or higher in the inhibition of mouse leukemia L1210 cells. The methanol extracts of Quercus robur and Sanguisorba officinalis demonstrated high activity against both thrombin and cancer.


Assuntos
Anticoagulantes/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Leucemia/patologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Trombina/antagonistas & inibidores , Animais , Metanol , Cloreto de Metileno , Camundongos , Fitoterapia , Plantas Medicinais/classificação , Federação Russa , Trombina/metabolismo , Células Tumorais Cultivadas
19.
Food Nutr Bull ; 23(2): 133-42, 2002 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12094663

RESUMO

Vitamin A deficiency is one of the major nutritional deficiencies in Vietnam. The first survey, conducted in 1985-1988 showed that the prevalence of severe xerophthalmia was seven times higher than the cutoff point established by the World Health Organization (WHO) to define vitamin A deficiency as a public health problem. The result of this survey strongly convinced the government to launch a program to control vitamin A deficiency, which started in 1988. The program strategies included nutrition education, universal distribution of high-dose vitamin A capsules to children aged 6 to 36 months in combination with national immunization days, and promotion of production and consumption of vitamin A-rich foods at the family level. The implementation network was set up based on the existing preventive health structure at all administrative levels. Organizations such as the women's union and other social sectors have participated actively in the program. Surveys conducted in 1994 and 1998 showed that the prevalence of clinical xerophthalmia was significantly lower than that identified in the baseline survey and below the WHO criteria for a public health problem. The achievements of our program have demonstrated that an effective vitamin A supplementation program can be implemented successfully by the preventive health network with active community participation. In the coming years, it will be important for our program to develop approaches other than vitamin A supplementation in order to maintain the past achievements.


Assuntos
Planejamento em Saúde/tendências , Deficiência de Vitamina A/tratamento farmacológico , Vitamina A/administração & dosagem , Xeroftalmia/tratamento farmacológico , Adulto , Pré-Escolar , Suplementos Nutricionais , Feminino , Humanos , Lactente , Masculino , Leite Humano , Vietnã/epidemiologia , Vitamina A/sangue , Deficiência de Vitamina A/epidemiologia , Xeroftalmia/epidemiologia
20.
J Ethnopharmacol ; 81(2): 277-80, 2002 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-12065163

RESUMO

A chromogenic bioassay was utilized to determine the antithrombin activity of methylene chloride and methanol extracts prepared from 30 plants of central Florida. Extracts of Ardisia crenata, Tetrapanax papyriferus, Lagerstroemia indica, Callistemon lanceolatus, Antigonon Leptopus, Magnolia virginiana, and Myrica cerifera demonstrated activity of 80% or higher in this bioassay system.


Assuntos
Fibrinolíticos/farmacologia , Plantas Medicinais , Trombina/antagonistas & inibidores , Fibrinolíticos/isolamento & purificação , Fibrinolíticos/uso terapêutico , Florida , Magnolia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Trombina/metabolismo
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