A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase

Garro, Hugo Alejandro; García, Celina; Martı́n, Victor S.; Tonn, Carlos E.; Pungitore, Carlos Rodolfo

doi:10.1016/j.bmcl.2014.12.052

Cited by 14 publications

(9 citation statements)

References 16 publications

(22 reference statements)

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“…Consistent with our findings, VB was shown to suppress cell proliferation in gastric cancer . Hugo et al demonstrated that VB was protective against prostate cancer, acting to reduce the levels of reactive oxygen species in cancer cells . Zhou et al similarly found that VB up‐regulated colorectal cancer cell apoptosis by activating the HIPK2‐p53 signalling pathway .…”

Section: Discussionsupporting

confidence: 90%

“…32 Hugo et al demonstrated that VB was protective against prostate cancer, acting to reduce the levels of reactive oxygen species in cancer cells. 33 Zhou et al similarly found that VB up-regulated colorectal cancer cell apoptosis by activating the HIPK2-p53 signalling pathway. 25 Notably, our in vitro experiments indicated that VB could down-regulate PKC, a Wnt pathway-related gene, by modulating the expression of let-7g-5p.…”

Section: Discussionmentioning

confidence: 96%

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Verbascoside inhibits progression of glioblastoma cells by promoting Let‐7g‐5p and down‐regulating HMGA2 via Wnt/beta‐catenin signalling blockade

Jia

Zhu

Yang

et al. 2020

J Cellular Molecular Medi

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Glioblastoma (GBM) continues to show a poor prognosis despite advances in diagnostic and therapeutic approaches. The discovery of reliable prognostic indicators may significantly improve treatment outcome of GBM. In this study, we aimed to explore the function of verbascoside (VB) in GBM and its effects on GBM cell biological processes via let‐7g‐5p and HMGA2. Differentially expressed GBM‐related microRNAs (miRNAs) were initially screened. Different concentrations of VB were applied to U87 and U251 GBM cells, and 50 µmol/L of VB was selected for subsequent experiments. Cells were transfected with let‐7g‐5p inhibitor or mimic, and overexpression of HMGA2 or siRNA against HMGA2 was induced, followed by treatment with VB. The regulatory relationships between VB, let‐7g‐5p, HMGA2 and Wnt/β‐catenin signalling pathway were determined. The results showed that HMGA2 was a direct target gene of let‐7g‐5p. VB treatment or let‐7g‐5p overexpression inhibited HMGA2 expression and the activation of Wnt/β‐catenin signalling pathway, which further inhibited cell viability, invasion, migration, tumour growth and promoted GBM cell apoptosis and autophagy. On the contrary, HMGA2 overexpression promoted cell viability, invasion, migration, tumour growth while inhibiting GBM cell apoptosis and autophagy. We demonstrated that VB inhibits cell viability and promotes cell autophagy in GBM cells by up‐regulating let‐7g‐5p and down‐regulating HMGA2 via Wnt/β‐catenin signalling blockade.

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Section: Discussionsupporting

confidence: 90%

Section: Discussionmentioning

confidence: 96%

Verbascoside inhibits progression of glioblastoma cells by promoting Let‐7g‐5p and down‐regulating HMGA2 via Wnt/beta‐catenin signalling blockade

Jia

Zhu

Yang

et al. 2020

J Cellular Molecular Medi

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“…The regioselective silylation of secondary saccharide alcohols can also be achieved either taking advantage of the inherent difference of reactivity among the hydroxy functions [24–32] or exploiting the activation effect of boron complexes [33]. …”

Section: Introductionmentioning

confidence: 99%

Orthogonal protection of saccharide polyols through solvent-free one-pot sequences based on regioselective silylations

Traboni¹,

Bedini²,

Iadonisi³

2016

Beilstein J. Org. Chem.

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tert-Butyldimethylsilyl (TBDMS) and tert-butyldiphenylsilyl (TBDPS) are alcohol protecting groups widely employed in organic synthesis in view of their compatibility with a wide range of conditions. Their regioselective installation on polyols generally requires lengthy reactions and the use of high boiling solvents. In the first part of this paper we demonstrate that regioselective silylation of sugar polyols can be conducted in short times with the requisite silyl chloride and a very limited excess of pyridine (2–3 equivalents). Under these conditions, that can be regarded as solvent-free conditions in view of the insolubility of the polyol substrates, the reactions are faster than in most examples reported in the literature, and can even be further accelerated with a catalytic amount of tetrabutylammonium bromide (TBAB). The strategy proved also useful for either the selective TBDMS protection of secondary alcohols or the fast per-O-trimethylsilylation of saccharide polyols. In the second part of the paper the scope of the silylation approach was significantly extended with the development of unprecedented “one-pot” and “solvent-free” sequences allowing the regioselective silylation/alkylation (or the reverse sequence) of saccharide polyols in short times. The developed methodologies represent a very useful and experimentally simple tool for the straightforward access to saccharide building-blocks useful in organic synthesis.

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“…As part of a programme to determine biological activities of natural products and derivatives (Pungitore 2008; Martin et al 2011; Garro et al 2015), 17 alkaloids previously reported were tested as biofilm forming inhibitors (Fig. 1) (Di Marco et al 2019).…”

Section: Methodsmentioning

confidence: 99%

Aporphinoid alkaloids inhibit biofilm formation of Yersinia enterocolitica isolated from sausages

Marco

Pungitore

Estrada

2020

J. Appl. Microbiol.

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Aims of the study The ability of Yersinia enterocolitica strains to form biofilms and the capacity of different alkaloids to inhibit biofilm formation were investigated. Methods and Results The capacity to form biofilm on polystyrene of 31 Y. enterocolitica strains was evaluated. Biofilm and quorum sensing (QS) inhibition of 17 alkaloids were assayed; furthermore, minimum biofilm inhibitory concentration (MBIC) was determined. The capacity to form biofilms among the examined strains seemed to be a strain‐related feature. The best biofilm inhibitors at 100 µmol l−1 were oliverine (1), guatterine (3), liriodenine (4), oliveridine (5) and pachypodanthine (6), which showed biofilm inhibition higher than 87%. Pachypodanthine (6) was the most effective compound with MBIC value of 12·5 µmol l−1 at subinhibitory concentration and also was able to inhibit QS system and reduce yenR expression at this concentration. Conclusion This is the first study to demonstrate that oliverine, liriodenine, and pachypodanthine are able to inhibit biofilm formation of Y. enterocolitica without critically disturbing its growing capacity. At MBIC, pachypodanthine inhibited biofilm formation and QS. Significance and Impact of the Study The use of aporphinoid alkaloids as biofilms inhibitory agents might potentially be useful to treat biofilm‐associated infections in the future.

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A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase

Cited by 14 publications

References 16 publications

Verbascoside inhibits progression of glioblastoma cells by promoting Let‐7g‐5p and down‐regulating HMGA2 via Wnt/beta‐catenin signalling blockade

Verbascoside inhibits progression of glioblastoma cells by promoting Let‐7g‐5p and down‐regulating HMGA2 via Wnt/beta‐catenin signalling blockade

Orthogonal protection of saccharide polyols through solvent-free one-pot sequences based on regioselective silylations

Aporphinoid alkaloids inhibit biofilm formation of Yersinia enterocolitica isolated from sausages

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