scholarly journals In Vitro Antiviral Activity Against Zika Virus From a Natural Product of the Brazilian Brown Seaweed Dictyota menstrualis

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1985912 ◽  
Author(s):  
Claudio C. Cirne-Santos ◽  
Caroline de S. Barros ◽  
Max W. L. Gomes ◽  
Rafaela Gomes ◽  
Diana N. Cavalcanti ◽  
...  
Keyword(s):  
Natural Products ◽  
Zika Virus ◽  
Brown Seaweed ◽  
Health Concern ◽  
Dependent Manner ◽  
Dictyota Menstrualis ◽  
Crude Extracts ◽  
High Concentrations ◽  
Inhibitory Potential

Natural products isolated from seaweeds have shown great antiviral potential against numerous viruses such as human type 1 herpes, human immunodeficiency virus, and dengue. Diterpenes produced by the brown seaweeds Dictyota and Canistrocarpus, in particular, have shown antiviral or virucidal activity. Recently, the Zika virus (ZIKV) has become a major public health concern due to its widespread dissemination throughout the Americas. Since no vaccines are available, and no drugs have effectively treated recent cases of infection, our group evaluated products from Dictyota menstrualis for their antiviral potential, alone and in combination with Ribavirin. We first evaluated the compounds’ cytotoxicity at high concentrations, and then evaluated the inhibition of ZIKV replication by crude extracts and acetylated crude extracts and their fractions at 20 μg/mL. The F-6 and FAc-2 fractions, rich in cyclic diterpenes with aldehyde groupings, inhibited ZIKV replication by >74%, with inhibition behaving in a dose-dependent manner and the 50% effective concentration (EC50) values of 2.80 (F-6) and 0.81 (FAc-2) μg/mL. Regarding the mechanism of action, FAc-2 had strong virucidal potential, and F-6 inhibited viral adsorption. Associating FAc-2 with Ribavirin at suboptimal dosages produced a strong synergistic effect that completely inhibited viral replication. Our results indicate that these natural products have excellent inhibitory potential against ZIKV replication and may be promising for developing affective therapies.

scholarly journals Resveratrol affects Zika virus replication in vitro

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Azirah Mohd ◽  
Nurhafiza Zainal ◽  
Kim-Kee Tan ◽  
Sazaly AbuBakar
Keyword(s):  
Cell Cultures ◽  
Zika Virus ◽  
Copy Number ◽  
Virus Titer ◽  
Health Concern ◽  
Dependent Manner ◽  
Zikv Infection ◽  
Mrna Copy Number ◽  
Short Period

Abstract Zika virus (ZIKV) infection is a serious public health concern. ZIKV infection has been associated with increased occurrences of microcephaly among newborns and incidences of Guillain-Barré syndrome among adults. No specific therapeutics or vaccines are currently available to treat and protect against ZIKV infection. Here, a plant-secreted phytoalexin, resveratrol (RES), was investigated for its ability to inhibit ZIKV replication in vitro. Several RES treatment regimens were used. The ZIKV titers of mock- and RES-treated infected cell cultures were determined using the focus-forming assay and the Zika mRNA copy number as determined using qRT-PCR. Our results suggested that RES treatment reduced ZIKV titers in a dose-dependent manner. A reduction of >90% of virus titer and ZIKV mRNA copy number was achieved when infected cells were treated with 80 µM of RES post-infection. Pre-incubation of the virus with 80 µM RES showed >30% reduction in ZIKV titers and ZIKV mRNA copy number, implying potential direct virucidal effects of RES against the virus. The RES treatment reduced >70% virus titer in the anti-adsorption assay, suggesting the possibility that RES also interferes with ZIKV binding. However, there was no significant decrease in ZIKV titer when a short-period of RES treatment was applied to cells before ZIKV infection (pre-infection) and after the virus bound to the cells (virus internalization inhibition), implying that RES acts through its continuous presence in the cell cultures after virus infection. Overall, our results suggested that RES exhibited direct virucidal activity against ZIKV and possessed anti-ZIKV replication properties, highlighting the need for further exploration of RES as a potential antiviral molecule against ZIKV infection.

Chickpea (Cicer arietinum L.) Lectin Exhibit Inhibition of ACE-I, α-amylase and α-glucosidase Activity

2019 ◽  
Vol 26 (7) ◽  
pp. 494-501 ◽  
Author(s):  
Sameer Suresh Bhagyawant ◽  
Dakshita Tanaji Narvekar ◽  
Neha Gupta ◽  
Amita Bhadkaria ◽  
Ajay Kumar Gautam ◽  
...  
Keyword(s):  
Biological Effects ◽  
Exchange Chromatography ◽  
Health Concern ◽  
Carbohydrate Binding ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ic50 Values ◽  
Chickpea Lectin

Background: Diabetes and hypertension are the major health concern and alleged to be of epidemic proportions. This has made it a numero uno subject at various levels of investigation. Glucosidase inhibitor provides the reasonable option in treatment of Diabetes Mellitus (DM) as it specifically targets post prandial hyperglycemia. The Angiotensin Converting Enzyme (ACE) plays an important role in hypertension. Therefore, inhibition of ACE in treatment of elevated blood pressure attracts special interest of the scientific community. Chickpea is a food legume and seeds contain carbohydrate binding protein- a lectin. Some of the biological properties of this lectin hitherto been elucidated. Methods: Purified by ion exchange chromatography, chickpea lectin was tested for its in vitro antioxidant, ACE-I inhibitory and anti-diabetic characteristic. Results: Lectin shows a characteristic improvement over the synthetic drugs like acarbose (oral anti-diabetic drug) and captopril (standard antihypertensive drug) when, their IC50 values are compared. Lectin significantly inhibited α-glucosidase and α-amylase in a concentration dependent manner with IC50 values of 85.41 ± 1.21 ҝg/ml and 65.05 ± 1.2 µg/ml compared to acarbose having IC50 70.20 ± 0.47 value of µg/ml and 50.52 ± 1.01 µg/ml respectively. β-Carotene bleaching assay showed antioxidant activity of lectin (72.3%) to be as active as Butylated Hydroxylanisole (BHA). In addition, lectin demonstrated inhibition against ACE-I with IC50 value of 57.43 ± 1.20 µg/ml compared to captopril. Conclusion: Lectin demonstrated its antioxidant character, ACE-I inhibition and significantly inhibitory for α-glucosidase and α-amylase seems to qualify as an anti-hyperglycemic therapeutic molecule. The biological effects of chickpea lectin display potential for reducing the parameters of medically debilitating conditions. These characteristics however needs to be established under in vivo systems too viz. animals through to humans.

Effects of polymethoxylated flavone metabolites on apoB100 secretion and MTP activity in Huh7.5 cells

2021 ◽  
Vol 18 ◽  
Author(s):  
Danielle R. Gonçalves ◽  
Thais B. Cesar ◽  
John A. Manthey ◽  
Paulo I. Costa
Keyword(s):  
Lipid Synthesis ◽  
Dependent Manner ◽  
Transfer Protein ◽  
Low Concentrations ◽  
Wide Range ◽  
Cell Assays ◽  
Polymethoxylated Flavones ◽  
High Concentrations

Background: Citrus polymethoxylated flavones (PMFs) reduce the synthesis of liver lipoproteins in animal and in vitro cell assays, but few studies have evaluated the direct effects of their metabolites on this highly regulated process. Objective: To investigate the effects of representative metabolites of PMF on the secretion of liver lipoproteins using the mammalian cell Huh7.5. Method: In this study, the influences of three PMFs and five previously isolated PMF metabolites on hepatic apoB-100 secretion and microsomal transfer protein (MTP) activity were evaluated. Tangeretin (TAN), nobiletin (NOB) and 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF), and their glucuronides (TAN-Gluc, NOB-Gluc and HMF-Gluc) and oxidatively demethylated metabolites (TAN-OH, NOB-OH, HMF-OH) were incubated with Huh7.5 cells to measure their inhibitory effects on lipid synthesis. Results: The results showed that TAN, HMF and TAN-OH reduced the secretion of apoB-100 in a dose-dependent manner, while NOB and the other tested metabolites showed no inhibition. MTP activity in the Huh7.5 cells was significantly reduced in the presence of low concentrations of TAN, and in high concentrations of NOB-OH. This study also showed that PMFs and PMF metabolites produced a wide range of effects on apoB-100 secretion and MTP activity. Conclusion: The results suggest that while PMFs and their metabolites control dyslipidemia in vivo, the inhibition of MTP activity cannot be the only pathway influenced by these compounds.

scholarly journals Antiobesity Effects of Extract from Spergularia marina Griseb in Adipocytes and High-Fat Diet-Induced Obese Rats

Nutrients ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 336 ◽  
Author(s):  
Yong-Hyun Park ◽  
Jae-Joon Lee ◽  
Hee-Kyoung Son ◽  
Bok-Hee Kim ◽  
Jaemin Byun ◽  
...  
Keyword(s):  
Ethanol Extract ◽  
Health Concern ◽  
Dependent Manner ◽  
High Fat ◽  
Proliferation And Differentiation ◽  
Obese Rats ◽  
Spergularia Marina ◽  
Natural Herb

Obesity has recently risen and become a serious health concern in Korea according to the westernized diet and altered lifestyle. Hence, there is a growing interest in the supplementation of phytochemicals to find a safe and effective functional ingredient to treat obesity. Spergularia marina Griseb (SM) has traditionally been used as a natural herb against chronic diseases in Korea. In this study, we investigated the antiobesity effects of SM in vitro and in vivo. SM ethanol extract (SME) inhibited proliferation and differentiation in murine adipocytes and primary porcine pre-adipocytes in a dose-dependent manner. In the in vivo study, supplementation of SM powder (SMP) remarkably attenuated fat accumulation in HFD-induced obese rats. In addition, SMP supplementation improved lipid profiles in the serum and tissues of high-fat induced obese rats. Collectively, these data indicated that SME exhibited antiobesity effects by modulating adipogenesis and lipolysis. Furthermore, SMP could be developed as an obesity-induced metabolic syndrome treatment.

scholarly journals Impact of Phytomediated Zinc Oxide Nanoparticles on Growth and Oxidative Stress Response of In Vitro Raised Shoots of Ochradenus arabicus

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Fahad Al-Qurainy ◽  
Salim Khan ◽  
Saleh Alansi ◽  
Mohammad Nadeem ◽  
Aref Alshameri ◽  
...  
Keyword(s):  
Zinc Oxide ◽  
Zinc Oxide Nanoparticles ◽  
Shoot Growth ◽  
System Response ◽  
Oxide Nanoparticles ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Shoot Number ◽  
High Concentrations

Biogenic nanoparticles have potential roles in the growth and development of plants and animals as they are ecofriendly and free of chemical contaminants. In this study, we assessed the effects of phytomediated zinc oxide nanoparticles (ZnONPs) on shoot growth, biochemical markers, and antioxidant system response in Ochradenus arabicus, which is a medicinal plant. The shoot length and fresh and dry weights were found to be higher in groups with 5 and 10 mg/L ZnONPs than in the control. At high concentrations of ZnONPs (50, 100, and 300 mg/L), biomass was decreased in a concentration-dependent manner. The shoot number was observed to be highest at 50 mg/L among all applied concentrations of ZnONPs. The levels of the stress markers proline and TBARS were found to be higher in shoots treated with 100 and 300 mg/L ZnONPs than in the control as well as NP-treated shoots. The levels of antioxidant enzymes were significantly increased at high concentrations of nanoparticles compared with the control. Thus, synthesized phytomediated ZnONPs from shoots of O. arabicus and their application to the same organ of O. arabicus in vitro were found to be effective as a low concentration of nanoparticles promoted shoot growth, resulting in high biomass accumulation. Thus, using green nanotechnology, such endemic plants could be conserved in vitro and multiple shoots could be produced by reducing the phytohormone concentration for multiple uses, such as the production of potential secondary metabolites.

scholarly journals Effects of storage and solvent type in a lipophylic chemical profile of the seaweed Dictyota menstrualis

2008 ◽  
Vol 56 (1) ◽  
pp. 51-57 ◽  
Author(s):  
Diana Negrão Cavalcanti ◽  
Marcelo Augusto Vasconcelos Gomes ◽  
Angelo Cunha Pinto ◽  
Claudia Moraes de Rezende ◽  
Renato Crespo Pereira ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Chemical Analysis ◽  
Bioactive Compounds ◽  
Mass Production ◽  
Brown Seaweed ◽  
Selective Extraction ◽  
Chemical Profile ◽  
Dictyota Menstrualis ◽  
Crude Extracts ◽  
Solvent Type

Crude extracts from specimens of the brown seaweed Dictyota menstrualis, known to produce diterpenes as their major secondary metabolites, were analyzed according to storage procedures before extraction, and the solvent types used to obtain the crude extracts. The specimens of D. menstrualis were submitted to three types of storage procedures, such as wet, dry, and frozen and were extracted with a mixture of dichloromethane:methanol (2:1) and acetone. Qualitative differences were not observed by GC/MS analyses of all crude extracts containing mainly the diterpenes pachydictyol A (I), 6-hydroxy-dichotoma-3,14-diene-1,17-dial (II), 6-hydroxy-2,7-cycloxenia-3,14-diene-1,17-dial (III), and 6-acetoxy-dichotoma-3,14-diene-1,17-dial (IV). The most efficient and selective extraction of the compounds with intermediate polarity produced by D. menstrualis was obtained using acetone, but with less mass production. In general, the storage procedures produced very similar results, but the frozen samples furnished low amount of total diterpenes. According to these results on chemical analysis of crude extracts of seaweeds, the choice of solvent to extraction should be considered as important aspect to better screening bioactive compounds.

scholarly journals In vitro and in vivo antioxidant potentials of the methanolic crude extract from Inula glomerata Oliv. & Hiern (Asteraceae) and Salacia kraussii (Harv.) Harv (Celastraceae)

2021 ◽  
Vol 20 (4) ◽  
pp. 416-426
Author(s):  
Michael C Ojo ◽  
◽  
Foluso O Osunsanmi ◽  
Nkosinathi D Cele ◽  
Godfrey E Zharare ◽  
...  
Keyword(s):  
Erectile Dysfunction ◽  
Antioxidant Properties ◽  
Therapeutic Modality ◽  
Total Phenolic ◽  
Phytochemical Analysis ◽  
Dependent Manner ◽  
Plant Materials ◽  
Crude Extracts

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitro as well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerata and S. kraussii possess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.

scholarly journals Inhibitory Effect of Ocimum gratissimum Leaf Extract on Postprandial Increase of Blood Glucose

2019 ◽  
Vol 14 (10) ◽  
pp. 1934578X1988372
Author(s):  
Hiroaki Shimada ◽  
Chiaki Kuma ◽  
Taichi Iseri ◽  
Shin-ichi Matsumura ◽  
Atsushi Kawase ◽  
...  
Keyword(s):  
Blood Glucose ◽  
Glucose Transporter ◽  
Inhibitory Effect ◽  
Glucose Absorption ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ocimum Gratissimum ◽  
Inhibitory Potential ◽  
Hyperglycemic Effect

The tea of Ocimum gratissimum (OG) leaves has been commonly consumed by people living in Ishigaki Island, Okinawa prefecture, Japan, and is considered to be effective for improving diabetes mellitus. In this study, we aimed to clarify the inhibitory potential of OG leaves extract (OG-ext) on gastrointestinal glucose absorption and to provide theoretical evidence for the anti-hyperglycemic effect of OG-ext. The increase of blood glucose after oral administration of α-starch and glucose in mice was suppressed by co-administration of OG-ext. An in vitro enzymatic assay suggested that amylase and maltase were inhibited weakly by the addition of OG-ext. In Caco-2 cells, a human intestinal epithelial model, the sodium-dependent glucose transporter (SGLT) 1-mediated uptake of fluorescence glucose analog was inhibited significantly by the addition of OG-ext in a concentration-dependent manner. These results indicate that the inhibitory effect on SGLT1 is one of the mechanisms of the anti-hyperglycemic effect of the tea of OG leaves.

Pelle kinase is activated by autophosphorylation during Toll signaling in Drosophila

Development ◽  
2002 ◽  
Vol 129 (8) ◽  
pp. 1925-1933 ◽  
Author(s):  
Baohe Shen ◽  
James L. Manley
Keyword(s):  
Dependent Manner ◽  
Loss Of Function ◽  
Concentration Dependent Manner ◽  
Downstream Target ◽  
Toll Signaling ◽  
Early Embryos ◽  
High Concentrations ◽  
L2 Cells

The Drosophila Pelle kinase plays a key role in the evolutionarily conserved Toll signaling pathway, but the mechanism responsible for its activation has been unknown. We present in vivo and in vitro evidence establishing an important role for concentration-dependent autophosphorylation in the signaling process. We first show that Pelle phosphorylation can be detected transiently in early embryos, concomitant with activation of signaling. Importantly, Pelle phosphorylation is enhanced in a gain-of-function Toll mutant (Toll10b), but decreased by loss-of-function Toll alleles. Next we found that Pelle is phosphorylated in transfected Schneider L2 cells in a concentration-dependent manner such that significant modification is observed only at high Pelle concentrations, which coincide with levels required for phosphorylation and activation of the downstream target, Dorsal. Pelle phosphorylation is also enhanced in L2 cells co-expressing Toll10b, and is dependent on Pelle kinase activity. In vitro kinase assays revealed that recombinant, autophosphorylated Pelle is far more active than unphosphorylated Pelle. Importantly, unphosphorylated Pelle becomes autophosphorylated, and activated, by incubation at high concentrations. We discuss these results in the context of Toll-like receptor mediated signaling in both flies and mammals.

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