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1.
Biosci Biotechnol Biochem ; 84(1): 134-142, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31490096

RESUMO

Plumbagin (PLB), an alkaloid obtained from the roots of the plants of Plumbago genus, is an inhibitor of NADPH oxidase 4 (NOX4). This study aimed to investigate the beneficial effect of PLB against oxygen-glucose deprivation/reoxygenation (OGDR)-induced neuroinjury in human SH-SY5Y neuronal cultures. Our results showed that OGD/R stimulated NOX4 protein expression and reactive oxygen species (ROS) production in SH-SY5Y cells, whereas increased 4-hydroxynonenal (4-HNE) and malondialdehyde (MDA) production, resulting in the activation of the NLRP3 inflammasome. And PLB pretreatment reduced the ROS production by regulating the expression of NOX4 and downregulated NF-κB signaling which was induced by OGDR. Furthermore, PLB inhibited OGDR induced NLRP3 inflammasome activation but not PARP1. Overall, PLB improved OGDR induced neuroinjury by inhibiting NOX4-derived ROS-activated NLRP3 inflammasome.


Assuntos
Hipóxia Celular/efeitos dos fármacos , Glucose/deficiência , Inflamassomos/metabolismo , NADPH Oxidase 4/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Naftoquinonas/farmacologia , Neurônios/metabolismo , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Apoptose/efeitos dos fármacos , Isquemia Encefálica/metabolismo , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , NF-kappa B/antagonistas & inibidores , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas/química , Plumbaginaceae/química
2.
An Acad Bras Cienc ; 91(2): e20180468, 2019 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-31241699

RESUMO

This study evaluates the antibacterial, cytotoxic activities, and phytochemical composition, of Callistemon citrinus, Hibiscus rosa-sinensis and Plumbago auriculata leaves and flowers, three ornamental plants in Mexico. However, in other countries offers a range of other uses. Ethanol extracts of C. citrinus leaf and flower presented stronger antibacterial activity than the extracts obtained from the other two plants. C. citrinus leaf showed low cytotoxicity (LC50 <600 µg/mL) on the brine shrimp test, whereas the ethanol extracts of H. rosa-sinensis and P. auriculata leaves showed no cytotoxic activity. Flower extracts obtained from the three plants did no exhibit cytotoxicity. GC-MS analysis revealed that the ethanol extract of P. auriculata leaf contained lupeol triterpene and lupeol acetate, neither of them have been previously reported in this genus. Gamma sitosterol was present in the leaf and flower extracts of P. auriculata. Higher contents of linoleic and linolenic acids were found in extracts of H. rosa-sinensis leaves and flowers. The ability of the ethanol extracts of C. citrinus leaves and flowers to inhibit the growth of Gram-positive and Gram-negative bacteria indicates a potentially broad antimicrobial spectrum. Moreover, the absence of cytotoxicity suggests the potential use of this plant to treat microbial infections.


Assuntos
Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hibiscus/química , Myrtaceae/química , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Animais , Antibacterianos/toxicidade , Artemia/efeitos dos fármacos , México , Testes de Sensibilidade Microbiana , Extratos Vegetais/toxicidade , Testes de Toxicidade
3.
Lett Appl Microbiol ; 69(1): 41-49, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31044446

RESUMO

Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) is a bicyclic naphthoquinone, found in three major plant families viz. Plumbaginaceae, Ebenceae and Droseraceae. The phytochemical is reported to exhibit various pharmacological properties. In this study, plumbagin isolated from Plumbago zeylanica L. was investigated for its in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA). Against 100 MRSA isolates that included multi-drug-resistant phenotypes, plumbagin showed consistent activity with a narrow minimum inhibitory concentration (MIC) range of 4-8 µg ml-1 . The time-kill study revealed 99% kill of a reference MRSA strain, 8 h after exposure to plumbagin. In the combination MIC study using the reference MRSA strain, plumbagin showed synergistic effect with ciprofloxacin and piperacillin while additive or indifference effect with other commonly used antibiotics. The transmission electron micrograph of the reference MRSA strain treated with plumbagin confirmed cell wall and cytoplasmic changes. Our results demonstrated potent anti-MRSA activity of plumbagin which was not impacted by multi-drug resistance. This is a first ever study that evaluated in vitro anti-MRSA activity of plumbagin employing large number of MRSA isolates. The findings of this study support the need for the further investigation on this phytochemical agent for therapeutic application. SIGNIFICANCE AND IMPACT OF THE STUDY: This study revealed phytochemical plumbagin's potent and consistent in vitro antibacterial activity against clinically problematic methicillin-resistant Staphylococcus aureus (MRSA) including multi-drug-resistant (MDR) phenotypes. The study results support further research to assess the clinical scope of plumbagin.


Assuntos
Antibacterianos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Naftoquinonas/farmacologia , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Parede Celular/efeitos dos fármacos , Ciprofloxacino/farmacologia , Citoplasma/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Staphylococcus aureus Resistente à Meticilina/isolamento & purificação , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/farmacologia , Piperacilina/farmacologia
4.
Chem Biodivers ; 16(7): e1900216, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31131525

RESUMO

A particular interest is nowadays given to natural antioxidants occurring in foods which can reduce the risk of several diseases through their protective effect. The genus Limonium is widely distributed in different salt regions of Tunisia and known in traditional medicine for the presence of highly effective viral and bacterial replication inhibitors. Limonium leaves have possible beneficial effects on human health for their antioxidant activities and free radical scavenging abilities. To exploit the potential of plants from extreme environments as new sources of natural antioxidants, we studied the extracts from leaves of eight Limonium species growing in extreme environments in Tunisia. Antioxidant molecules (polyphenols, flavonoids, flavonols, ascorbate, tocopherols), in vitro (DPPH, ORAC) and ex vivo antioxidant potential on human erythrocytes, antioxidant enzymes activities (superoxide dismutase, peroxidases, glutathione reductase) were evaluated to identify the species with the best antioxidant capacity. The results showed variability among the species considered in function of the environmental conditions of their natural biotopes, as for the antioxidants measured. In particular, L. vulgare from Oued Rane biotope, characterized by dryness and high temperatures, was the species with the highest enzymatic activity and antioxidant capacity, making it interesting as possible edible halophyte plant or as food complement.


Assuntos
Antioxidantes/farmacologia , Compostos Fitoquímicos/farmacologia , Plumbaginaceae/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Hemólise/efeitos dos fármacos , Capacidade de Absorbância de Radicais de Oxigênio , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Picratos/antagonistas & inibidores , Folhas de Planta/química , Análise de Componente Principal , Especificidade da Espécie , Tunísia
5.
Nat Prod Res ; 33(12): 1798-1803, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29397771

RESUMO

During our search for potential templates of HIV-1 reverse transcriptase (RT) and integrase (IN) dual inhibitors, the methanolic extract obtained from aerial parts of Limonium morisianum was investigated. Repeated bioassay-guided chromatographic purifications led to the isolation of the following secondary metabolites: myricetin, myricetin 3-O-rutinoside, myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside, (-)-epigallocatechin 3-O-gallate, tryptamine, ferulic and phloretic acids. The isolated compounds were tested on both HIV-1 RT-associated RNase H and IN activities. Interestingly, (-)-epigallocatechin-3-O-gallate and myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside potently inhibited both enzyme activities with IC50 values ranging from 0.21 to 10.9 µM. Differently, tryptamine and ferulic acid exhibited a significant inhibition only on the IN strand transfer reaction, showing a selectivity for this viral enzyme. Taken together these results strongly support the potential of this plant as a valuable anti HIV-1 drugs source worthy of further investigations.


Assuntos
Fármacos Anti-HIV/farmacologia , Inibidores de Integrase de HIV/farmacologia , Transcriptase Reversa do HIV/antagonistas & inibidores , Plumbaginaceae/química , Fármacos Anti-HIV/química , Flavonoides/química , Flavonoides/farmacologia , Galactose/análogos & derivados , Galactose/química , Galactose/farmacologia , Inibidores de Integrase de HIV/química , Itália , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Inibidores da Transcriptase Reversa/química , Inibidores da Transcriptase Reversa/farmacologia , Ribonuclease H/antagonistas & inibidores
6.
Biochemistry ; 57(44): 6367-6378, 2018 11 06.
Artigo em Inglês | MEDLINE | ID: mdl-30298725

RESUMO

Ebola virus (EBOV) is a filovirus that causes a severe and rapidly progressing hemorrhagic syndrome; a recent epidemic illustrated the urgent need for novel therapeutic agents because no drugs have been approved for treatment of Ebola virus. A key contribution to the high lethality observed during EBOV outbreaks comes from viral evasion of the host antiviral innate immune response in which viral protein VP35 plays a crucial role, blocking interferon type I production, first by masking the viral double-stranded RNA (dsRNA) and preventing its detection by the pattern recognition receptor RIG-I. Aiming to identify inhibitors of the interaction of VP35 with the viral dsRNA, counteracting the VP35 viral innate immune evasion, we established a new methodology for high-yield recombinant VP35 (rVP35) expression and purification and a novel and robust fluorescence-based rVP35-RNA interaction assay ( Z' factor of 0.69). Taking advantage of such newly established methods, we screened a small library of Sardinian natural extracts, identifying Limonium morisianum as the most potent inhibitor extract. A bioguided fractionation led to the identification of myricetin as the component that can inhibit rVP35-dsRNA interaction with an IC50 value of 2.7 µM. Molecular docking studies showed that myricetin interacts with the highly conserved region of the VP35 RNA binding domain, laying the basis for further structural optimization of potent inhibitors of VP35-dsRNA interaction.


Assuntos
Antivirais/farmacologia , Flavonoides/farmacologia , Fluorescência , Extratos Vegetais/farmacologia , RNA de Cadeia Dupla/antagonistas & inibidores , RNA Viral/antagonistas & inibidores , Proteínas Virais Reguladoras e Acessórias/antagonistas & inibidores , Ebolavirus/efeitos dos fármacos , Doença pelo Vírus Ebola/tratamento farmacológico , Doença pelo Vírus Ebola/virologia , Humanos , Simulação de Acoplamento Molecular , Plumbaginaceae/química , Conformação Proteica , RNA de Cadeia Dupla/genética , RNA de Cadeia Dupla/metabolismo , RNA Viral/genética , RNA Viral/metabolismo , Proteínas Virais Reguladoras e Acessórias/genética , Proteínas Virais Reguladoras e Acessórias/metabolismo
7.
Phytother Res ; 32(8): 1631-1635, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29672969

RESUMO

Plumbagin is a naphthoquinone found in the roots of Plumbago zeylanica. Here, we report an investigation to evaluate its antiobesity activity. The preliminary binding affinity of plumbagin to human pancreatic lipase (PL) was determined using molecular docking simulation. The in vitro PL inhibitory potential and the kinetics of inhibition were studied to validate and confirm the results obtained from molecular docking. The IC50 for PL was found to be 82.08 ± 9.47 µM, and the kinetics of inhibition was found to be of the mixed type. Further, the in vivo evaluation revealed that rats treated with plumbagin 1 mg/kg showed significant decrease in serum triglycerides (TG) and area under the curve of serum TG when compared with vehicle-treated rats. It was also seen that plumbagin possessed significant antiadipogenic effect as demonstrated by reduced oil red O staining and decreased TG contents. Thus, we conclude that plumbagin is a promising molecule to combat obesity and further optimization of plumbagin to yield plumbagin analogues will result in its improved activity profile.


Assuntos
Adipócitos/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Lipase/antagonistas & inibidores , Naftoquinonas/farmacologia , Obesidade/tratamento farmacológico , Células 3T3-L1 , Adipócitos/citologia , Animais , Humanos , Cinética , Lipase/metabolismo , Masculino , Camundongos , Simulação de Acoplamento Molecular , Raízes de Plantas/química , Plumbaginaceae/química , Ratos , Ratos Wistar , Triglicerídeos/sangue
8.
Inflammopharmacology ; 26(4): 983-991, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29569058

RESUMO

Plumbagin, a vitamin K3 analogue is the major active constituent in several plants including root of Plumbago indica Linn. This compound has been shown to exhibit a wide spectrum of pharmacological activities. The present investigation was to evaluate the ameliorative effects of plumbagin (PL) against severe malaria pathogenesis due to involvement of oxidative stress and inflammatory response in Plasmodium berghei infected malaria in mice. Malaria pathogenesis was induced by intra-peritoneal injection of P. berghei infected red blood cells into the Swiss albino mice. PL was administered orally at doses of 3, 10 and 30 mg/kg/day following Peter's 4 day suppression test. Oral administration of PL showed significant reduction of parasitaemia and increase in mean survival time. PL treatment is also attributed to significant increase in the blood glucose and haemoglobin level when compared with vehicle-treated infected mice. Significant inhibition in level of oxidative stress and pro-inflammation related markers were observed in PL treated group. The trend of inhibition in oxidative stress markers level after oral treatment of PL was MPO > LPO > ROS in organ injury in P. berghei infected mice. This study showed that plumbagin is able to ameliorate malaria pathogenesis by augmenting anti-oxidative and anti-inflammatory mechanism apart from its effect on reducing parasitaemia and increasing mean survival time of malaria-induced mice.


Assuntos
Antimaláricos/administração & dosagem , Malária/tratamento farmacológico , Naftoquinonas/administração & dosagem , Plasmodium berghei/efeitos dos fármacos , Administração Oral , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacologia , Antimaláricos/farmacologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Inflamação/tratamento farmacológico , Inflamação/parasitologia , Malária/parasitologia , Masculino , Camundongos , Naftoquinonas/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Plasmodium berghei/isolamento & purificação , Plumbaginaceae/química
9.
BMC Complement Altern Med ; 18(1): 89, 2018 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-29534723

RESUMO

BACKGROUND: This study aimed to explore the effects of plumbagin (PLB) on ARPE-19 cells and underlying mechanism. METHODS: Cultured ARPE-19 cells were treated with various concentrations (0, 5, 15, and 25 µM) of PLB for 24 h or with 15 µM PLB for 12, 24 and 48 h. Then cell viability was evaluated by MTT assay and DAPI staining, while apoptosis and cell cycle progression of ARPE cells were assessed by flow cytometric analysis. Furthermore, the level of main regulatory proteins was examinated by Western boltting and the expression of relative mRNA was tested by Real-Time PCR. RESULTS: PLB exhibited potent inducing effects on cell cycle arrest at G2/M phase and apoptosis of ARPE cells via the modulation of Bcl-2 family regulators in a concentration- and time-dependent manner. PLB induced inhibition of phosphatidylinositol 3-kinase (PI3K) and p38 mitogen-activated protein kinase (p38 MAPK) signaling pathways contributing to the anti-proliferative activities in ARPE cells. CONCLUSIONS: This is the first report to show that PLB could inhibit the proliferation of RPE cells through down-regulation of modulatory signaling pathways. The results open new avenues for the use of PLB in prevention and treatment of proliferative vitreoretinopathy.


Assuntos
Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Naftoquinonas/farmacologia , Plumbaginaceae/química , Epitélio Pigmentado da Retina/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Vitreorretinopatia Proliferativa/fisiopatologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Células Epiteliais/citologia , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/metabolismo , Humanos , Fosfatidilinositol 3-Quinases/genética , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/genética , Proteínas Proto-Oncogênicas c-akt/metabolismo , Epitélio Pigmentado da Retina/citologia , Epitélio Pigmentado da Retina/metabolismo , Serina-Treonina Quinases TOR/genética , Serina-Treonina Quinases TOR/metabolismo , Vitreorretinopatia Proliferativa/tratamento farmacológico , Vitreorretinopatia Proliferativa/genética , Vitreorretinopatia Proliferativa/metabolismo , Proteínas Quinases p38 Ativadas por Mitógeno/genética , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
10.
Environ Sci Pollut Res Int ; 25(1): 507-522, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29047057

RESUMO

This study surveyed three species of the genus Armeria Willd. from five ultramafic outcrops, two non-ultramafic (schist) soils, and one tailing heap of an abandoned iron-copper mine from Serbia. Similarities and differences among the three Armeria species growing on different geological substrates in the ability to control uptake and translocate nine metals were examined. Chemical characteristics of the soil and plant samples (concentrations of P2O5, K2O, Ca, Fe, Mn, Ni, Zn, Cu, Cr, Co, Cd, and Pb) are presented. In order to assess accumulative potential of these three Armeria species, biological concentration, accumulation, as well as translocation factors were used. Three investigated Armeria species growing on eight different localities showed large differences in heavy metal uptake, translocation, and accumulation. The differences were present among the plant samples of the same species and even more among three different Armeria species and were primarily the result of the different contents of available heavy metals in the investigated soils. Additionally, differences might be the consequence of diverse responses and possible presence of supplementary resistance mechanisms in the plants from the ultramafic soils. None of the three Armeria species showed shoot hyperaccumulative potential for any of the investigated heavy metals and they could be considered as root accumulators, considering their potential to accumulate medium to large amounts of Zn (BCF up to 134), Cr (BCF up to 148), and Cd (BCF up to 9) in their roots.


Assuntos
Monitoramento Ambiental/métodos , Metais Pesados/análise , Mineração , Plumbaginaceae/química , Poluentes do Solo/análise , Solo/química , Altitude , Plumbaginaceae/crescimento & desenvolvimento , Sérvia
11.
Nat Prod Res ; 32(18): 2127-2132, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28823173

RESUMO

Study of the chemical constituents of the roots of Plumbago zeylanica L. collected in Taiwan led to the isolation and identification of a new naphthoquinone dimer, plumzeylanone (1), along with eight known compounds (2-9). Nine naphthoquinones isolated from this plant were assayed for cell growth inhibition activity using NALM-6 (human B cell precursor leukaemia), A549 (human lung adenocarcinoma), Colo205 (human colorectal adenocarcinoma) and KB (human epidermoid carcinoma). Plumzeylanone (1), a novel plumbagin dimer, suppressed cell proliferation in only NALM-6 cells (IC50 3.98 µM). However, maritinone (9) showed strong inhibition of cell growth in all cell lines tested (0.12 < IC50 < 9.06 µM). This compound appeared to affect the cell cycle.


Assuntos
Antineoplásicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Naftoquinonas/farmacologia , Plumbaginaceae/química , Antineoplásicos/farmacologia , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Dimerização , Humanos , Naftoquinonas/química , Naftoquinonas/isolamento & purificação , Raízes de Plantas/química , Taiwan
12.
Indian J Cancer ; 54(1): 253-256, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29199700

RESUMO

BACKGROUND: Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) derived from Plumbago species is a potential anti-tumour agent. Plumbagin has been tested for anti-cancer activity in vitro and in vivo using mice model. AIM: To study the tumour suppressing efficacy of plumbagin using zebrafish model. MATERIALS AND METHODS: Human Non-small lung cancer cell line were cultured in vitro and transplanted in to zebrafish. The development of tumour was confirmed by performing histology. The tumour was then allowed to progress in vivo and the fishes were administered with plumbagin orally for three continuous days. The tumour suppression capacity was monitored subsequently using transcriptosome analysis. STATISTICAL METHODS: The pixel integrated density obtained was converted into relative gene expression using IBM SPSS. RESULTS: The administration of plumbagin had an ability to suppress tumour and the size of the tumour were relatively lesser when compared with the control sample; it has also increased p53 gene expression. CONCLUSION: The study helps to conclude that plumbagin is an effective anti-tumour agent against human cancer cells based on the study in vivo in zebrafish.


Assuntos
Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Naftoquinonas/administração & dosagem , Proteína Supressora de Tumor p53/genética , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Carcinoma Pulmonar de Células não Pequenas/genética , Carcinoma Pulmonar de Células não Pequenas/patologia , Linhagem Celular Tumoral , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , Naftoquinonas/química , Plumbaginaceae/química , Transdução de Sinais/efeitos dos fármacos , Transplante Heterólogo , Peixe-Zebra/genética
13.
Zhongguo Zhong Yao Za Zhi ; 42(15): 2989-2994, 2017 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-29139268

RESUMO

Models were established in mice with warfarin sodium method, and their bleeding time and hemostasis time were measured by tail cutting method and slide method respectively. Rats were administered for 15 consecutive days to measure their recalcification time, plasma viscosity, platelet adhesion rate, platelet aggregation rate and other blood indexes. As compared with the blank group, the bleeding time was prolonged in model groupn(P<0.05). As compared with the model group, the results showed that the positive vitamin K, the leaching type water decoction and the sediment type decoction could significantly shorten the bleeding time (P<0.01); positive vitamin K significantly (P<0.01) shortened clotting time, and the leaching type water decoction, the sediment type water decoction and the sediment type powder could also shorten the clotting time (P<0.05). As compared with blank group, low dose, medium dose of leaching type water decoction, medium dose of powder, high dose of sediment type decoction and low dose of drug residues could reduce plasma viscosity (P<0.05), and high dose of leaching powder and low dose of water decoction could significantly reduce (P<0.01) plasma viscosity. As compared with blank group, Limonitum leaching type decoction high dose group could significantly reduce the platelet adhesion rate (P<0.05), while sediment type water decoction could significantly increase the platelet adhesion rate (P<0.05); the high dose of leaching type water decoction, high dose of drug residues, low dose of leaching type powder and low dose of drug residues could decrease the platelet aggregation rate (P<0.05), while high dose of leaching type water decoction and high dose of the powder could increase the platelet aggregation rate (P<0.05). Analysis of mineral compositions was conducted by polarized light microscopy and X-ray diffraction (XRD). The results of the both methods showed that Limonitum mineral compositions contained goethite, quartz, and kaolinite, and sedimentary type also contained illite and albite. Sediment type of Limonitum showed better hemostatic effect, which may be related to the high content of goethite and illite.


Assuntos
Medicamentos de Ervas Chinesas/química , Hemostáticos/farmacologia , Plumbaginaceae/química , Animais , Hemostasia , Camundongos , Minerais , Agregação Plaquetária , Ratos
14.
Biol Pharm Bull ; 40(11): 1856-1865, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29093332

RESUMO

Halophyte Limonium tetragonum has recently been of interest in Korea for its nutritional value and salty taste which made it an ideal vegetable. In this study, the potential of L. tetragonum preventing excess weight gain, obesity and the related health problem has been evaluated in vitro and in vivo. The treatment with 100 mg/kg of L. tetragonum EtOAc soluble fraction (EALT) apparently prevented the body weight gain, adipose tissue weight gain, and the increase of triglyceride and total cholesterol level in mice fed a high-fat diet for 8 weeks. In addition, both glucose tolerance and insulin resistance in dietary obese mice were improved by EALT administration. A marked decrease in adipocyte differentiation was observed in the EALT (50 µg/mL)-treated 3T3-L1 cells, which was mediated by the suppression of adipogenesis-related transcription factors including peroxisome proliferator-activated receptor (PPAR) γ, CCAAT/enhancer binding protein (C/EBP)α, and Sterol regulatory element binding protein-1 (SREBP-1) and adipocyte-specific proteins such as fatty acid synthase (FAS), lipoprotein lipase (LPL), and adipocyte fatty acid-binding protein (aP2). The major components contained in EALT were identified as (-)-epigallocatechin-3-(3″-O-methyl) gallate, (-)-epigallocatechin-3-gallate, and myricetin-3-O-ß-D-galactopyranoside based on its phytochemical analysis. Results suggested that EALT might be available as functional crop and bioactive diet supplement for the prevention and/or treatment of obesity.


Assuntos
Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/uso terapêutico , Obesidade/prevenção & controle , Extratos Vegetais/uso terapêutico , Plumbaginaceae/química , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Fármacos Antiobesidade/farmacologia , Glicemia , Dieta Hiperlipídica/efeitos adversos , Suplementos Nutricionais , Modelos Animais de Doenças , Teste de Tolerância a Glucose , Humanos , Resistência à Insulina , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/sangue , Obesidade/etiologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/farmacologia , República da Coreia , Triglicerídeos/sangue , Ganho de Peso/efeitos dos fármacos
15.
Molecules ; 22(9)2017 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-28872626

RESUMO

Overproduction and stimulation of tyrosinase result in increased melanogenesis of which several skin disorders such as freckles, spots, and hyperpigmentation appear as complications. Limonium tetragonum is a halophyte well-known for its antioxidative properties. This study investigated the anti-melanogenic effects of solvent-partitioned L. tetragonum extracts (LTEs) and its bioactive constituents, two isolated flavonoid glycosides. Current study followed a set of experiments on B16-F10 mouse melanoma cell model with a focus on tyrosinase activity and production. The anti-melanogenic capacity of LTEs was confirmed by their tyrosinase inhibitory effects, prevention of DOPA oxidation, and suppression of melanin production. The inhibition of tyrosinase and DOPA oxidation by LTEs was suggested to be related with the downregulation of microphthalmia-associated transcription factor, tyrosinase, tyrosinase-related protein-1, and tyrosinase-related protein-2, verified with mRNA and protein expression levels. Among all tested LTEs, 85% aq. MeOH and n-BuOH were found to be the most active fractions which later yielded the two known compounds, myricetin 3-galactoside and quercetin 3-O-ß-galactopyronaside. The anti-melanogenic potential of the compounds were confirmed by their tyrosinase inhibitory effects. These results suggested that L. tetragonum may serve as a potential source of bioactive substances with effective anti-melanogenesis properties.


Assuntos
Flavonoides/farmacologia , Glicosídeos/farmacologia , Oxirredutases Intramoleculares/antagonistas & inibidores , Melaninas/antagonistas & inibidores , Monofenol Mono-Oxigenase/antagonistas & inibidores , Oxirredutases/antagonistas & inibidores , Plumbaginaceae/química , Animais , Linhagem Celular Tumoral , Regulação para Baixo , Flavonoides/química , Expressão Gênica , Glicosídeos/química , Oxirredutases Intramoleculares/metabolismo , Melanoma Experimental , Camundongos , Oxirredutases/metabolismo
16.
Biomed Pharmacother ; 95: 1404-1411, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28946188

RESUMO

Limoniastrum guyonianum is used in several regions of North Africa as a folk medicine. The objective of this study was to determine the in vitro antioxidant activities of L. guyonianum roots and their cytoprotective action on H2O2-challenged rat small intestine epithelial cells (IEC-6 cells). To assess the cytoprotective effect of L. guyonianum extract (LGE), IEC-6 cells were pre-incubated with different LGE concentrations. Then, IEC-6 cultures were exposed to 40µM H2O2 during 4h. Modulation of endogenous antioxidant system including SOD, CAT, MDA, GSH and the expression of possibly involved MAPKs was evaluated. Main results reported that L. guyonianum was rich in polyphenols and exhibited an important antioxidant activity as revealed by different tests (DPPH Assay, IC50=1.6µg/mL; ABTS+ test, IC50=27µg/mL; Fe-reducing power, EC50=44µg/mL). HPLC analysis showed that quercetin, catechin, and isorhamnetin-3-O-rutinoside were major phenolics. The exposure of IEC-6 cells to 40µM H2O2 during 4h resulted in oxidative stress manifested by (i) over 70% cell mortality, (ii) over-activity of CAT (246%), (iii) decrease in GSH level (10.4nmol/mg), (iv) excess in MDA content (18.4nmol/mg), and (v) a trigger of JNK phosphorylation. Pretreatment with LGE, especially at 0.25µg/mL, restored cell viability to 100%, and normal cell morphology in H2O2-chalenged cells. In addition, this extract maintained a high CAT activity, enhanced SOD capacity (120%) and increased GSH level (45.5nmol/mg). Furthermore, reducing cell death seems to be due to dephosphorylated JNK MAPK exerted by L. guyonianum bioactive compounds. In all, L. guyonianum components provided a cross-talk between regulatory pathways, implying their role as cytoprotector against oxidative stress.


Assuntos
Células Epiteliais/enzimologia , Células Epiteliais/patologia , Glutationa/metabolismo , Peróxido de Hidrogênio/toxicidade , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Animais , Antioxidantes/farmacologia , Linhagem Celular , Forma Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Epiteliais/efeitos dos fármacos , Malondialdeído/metabolismo , Fenóis/análise , Fosforilação/efeitos dos fármacos , Raízes de Plantas/química , Ratos
17.
J Biomater Sci Polym Ed ; 28(16): 1847-1858, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28697688

RESUMO

In the present work, silver nanoparticles have been biosynthesized by utilizing the alcoholic extract of Plumbago auriculata. The optimization of reaction conditions was carried out by monitoring the reactions with the help of UV-Visible absorption spectroscopy. The characterization of AgNP was carried out by infrared spectroscopy, transmission electron microscopy and X-Ray diffraction (XRD) studies. The biogenic AgNPs were tested against Mycobacterium tuberculosis using Microplate Almar Blue assay (MABA) and their antioxidant activity was also evaluated. The silver nanoparticles were also assessed for their reducing activity against organic dyes. The AgNPs were spherical in shape with size ranging from 15 to 45 nm with face centered cubic geometry as revealed by XRD analysis. The AgNPs possessed good antitubercular activity with MIC value of 1.6 µg/ml and these also exhibited promising antioxidant activity with IC50 value of 28.2. Furthermore, AgNPs also reduced congo red within 2 h and malachite green was degraded within 40 min. The present work demonstrated the utilization of P. auriculata for biosynthesis of AgNP which could be a potential candidate for antitubercular drug development and it could also be used as an antioxidant agent. The application of AgNP in reducing agent can be further extended and evaluated for purification of effluent water from textile industries.


Assuntos
Corantes/química , Nanopartículas Metálicas/química , Mycobacterium tuberculosis/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plumbaginaceae/química , Prata/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Antituberculosos/química , Antituberculosos/isolamento & purificação , Antituberculosos/farmacologia , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Poluentes Químicos da Água/química
18.
J Nat Med ; 71(4): 650-658, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28550653

RESUMO

Members of the genus Limonium are widely used as medicinal herbs due to their health-promoting effects, such as an ability to improve blood circulation by inhibiting angiotensin I converting enzyme (ACE). While the potential of L. michelsonii Lincz. (a medicinal plant endemic to Kazakhstan) to inhibit ACE has been demonstrated, the inhibitory activities of its secondary metabolites have not been explored. In this work, the principal phenolic compounds (1-20) among these metabolites were isolated to determine the components responsible for ACE inhibition. The natural abundances of the active constituents within the target plant were characterized by UPLC-Q-TOF/MS analysis. All of the isolated compounds except for gallates 10-12 were found to significantly inhibit ACE, with IC50 values of between 7.1 and 138.4 µM. Unexpectedly, the flavonol glycosides 16-20 were observed to be more potent than the corresponding aglycones 4 and 5. For example, quercetin (4) had IC50 = 30.3 µM, whereas its glycosides (16, 17) had IC50 = 10.2 and 14.5 µM, respectively. A similar trend was observed for myricetin (5) and its glycosides (18-20). In a kinetic study, the flavonols 3-5 and 16-20 and the dihydroflavonols 8 and 9 behaved as competitive inhibitors, whereas other flavones (1, 2, 13-15) and flavanones (6, 7) performed noncompetitive inhibition.


Assuntos
Inibidores da Enzima Conversora de Angiotensina/farmacologia , Flavonoides/farmacologia , Glicosídeos/farmacologia , Peptidil Dipeptidase A/metabolismo , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Inibidores da Enzima Conversora de Angiotensina/isolamento & purificação , Animais , Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Pulmão/metabolismo , Fenóis/isolamento & purificação , Compostos Fitoquímicos , Extratos Vegetais/química , Plantas Medicinais/química , Coelhos
19.
Am J Chin Med ; 45(3): 423-441, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28359198

RESUMO

It has been shown that plumbagin, a bioactive naphthoquinone isolated from three major plant families viz. Plumbaginaceae, Ebenceae and Droseraceae, definitively exhibits anticancer potential in diverse cancer cells both in vitro and in vivo. Plumbagin shows antineoplastic effects via multi-channel molecular mechanisms, including the induction of apoptosis and autophagy, the disruption of the cell cycle, the inhibition of invasion and metastasis, and anti-angiogenesis. Plumbagin inhibits the growth of cancer cells mainly through the modulation of the signals of PI3K/Akt/mTOR, AMPK, Ras, and so on. The pharmaceutical applications of plumbagin combined with nanocarriers to achieve better therapeutic efficiency are discussed in this review Among them, liposomes, nanoparticles, microspheres, micelles, and nisosomes are used in cancer treatment. The anticancer study of plumbagin in vivo is also summarized in this review. On the whole, we aim to review the research progress of plumbagin both in pharmacological and pharmaceutical filed, which may provide some reference for further research of plumbagin.


Assuntos
Antineoplásicos Fitogênicos , Naftoquinonas/farmacologia , Naftoquinonas/uso terapêutico , Neoplasias/tratamento farmacológico , Fitoterapia , Transdução de Sinais/efeitos dos fármacos , Proteínas Quinases Ativadas por AMP , Animais , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Droseraceae/química , Ebenaceae/química , Genes ras , Humanos , Técnicas In Vitro , Camundongos , Naftoquinonas/isolamento & purificação , Neoplasias/genética , Neoplasias/patologia , Fosfatidilinositol 3-Quinase/metabolismo , Plumbaginaceae/química , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/genética , Serina-Treonina Quinases TOR/metabolismo
20.
Bioorg Med Chem Lett ; 27(9): 1914-1918, 2017 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-28359791

RESUMO

Lung cancer is the second most commonly diagnosed cancer and the leading cause of cancer deaths in both men and women in the United States. It has been recently demonstrated that osteopontin (OPN) effectively inhibits cofilin activity through the focal adhesion kinase (FAK)/AKT/Rho-associated kinase (ROCK) pathway to induce the invasion of human non-small cell lung cancer (NSCLC) cells. Plumbagin was isolated from the roots of the medicinal plant Plumbago zeylanica L. and has been reported to possess anticancer activities. However, the molecular mechanisms by which plumbagin inhibits the invasion of cancer cells is still unclear. In this study, the anti-invasive and anti-metastatic mechanisms of plumbagin were investigated in OPN-treated NSCLC A549 cells. OPN effectively induced the motility and invasion of NSCLC A549 cells and H1299 cells, which was strongly suppressed by plumbagin with no evidence of cytotoxicity. In addition, lamellipodia formation at the leading edge of cells by OPN was dramatically decreased in plumbagin-treated cells. Plumbagin caused an effective inhibition in OPN-induced the expression of ROCK1 as well as the phosphorylation of LIM kinase 1 and 2 (LIMK1/2), and cofilin. OPN-induced the phosphorylation of FAK and AKT was impaired without affecting their total forms by plumbagin treatment. OPN facilitated metastatic lung colonization, which was effectively suppressed in plumbagin-treated mice. Taken together, these results suggest that plumbagin reduces OPN-induced the invasion of NSCLC A549 cells, which resulted from inhibiting the ROCK pathway mediated by the FAK/AKT pathway and suppresses lung metastasis in vivo.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Neoplasias Pulmonares/tratamento farmacológico , Naftoquinonas/uso terapêutico , Osteopontina/metabolismo , Inibidores de Proteínas Quinases/uso terapêutico , Quinases Associadas a rho/antagonistas & inibidores , Células A549 , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Carcinoma Pulmonar de Células não Pequenas/metabolismo , Carcinoma Pulmonar de Células não Pequenas/patologia , Movimento Celular/efeitos dos fármacos , Humanos , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Pulmão/patologia , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patologia , Masculino , Camundongos Endogâmicos BALB C , Camundongos Nus , Naftoquinonas/química , Naftoquinonas/farmacologia , Invasividade Neoplásica/patologia , Invasividade Neoplásica/prevenção & controle , Plumbaginaceae/química , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacologia , Transdução de Sinais/efeitos dos fármacos , Quinases Associadas a rho/metabolismo
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