PAMPA Permeability, Acetylcholinesterase Inhibition and Antioxidant Activity of Pyranoisoflavones from<i>Polygala molluginifolia</i>(Polygalaceae)

Venzke, Dalila; Carvalho, Francieli Kanumfre de; Ruani, Ana Paula; Oliveira, Aldo Sena de; Brighente, Inês Maria Costa; Micke, Gustavo Amadeu; Barison, Andersson; Pizzolatti, Moacir Geraldo

doi:10.5935/0103-5053.20130249

Cited by 8 publications

(8 citation statements)

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“…The free radical scavenging activity of the samples was measured using DPPH (2,2-diphenyl-1-picrylhydrazyl) [28]. For this assay 1 mL of sample (in different concentrations) was added to 2 mL of a solution of DPPH in methanol (0.004%).…”

Section: Antioxidant Assaymentioning

confidence: 99%

Antioxidant and Antifungal Activity of Naphthoquinones Dimeric Derived from Lawsone

Oliveira¹,

Brighente²,

Lund³

et al. 2017

JBM

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This article reports the evaluation of antioxidant and antifungal activity from synthetic naphthoquinones derived from lawsone. The antifungal activity was carried out through the inhibition of exoenzymes produced by Candida albicans. The inhibition of phospholipase and the proteinase production by Candida was similar in all derivatives tested; however, the difference between the enzyme production of the control and test does not show statistical difference in any of the studied strains. Furthermore, the antioxidant activity using DPPH radical-scavenging assay showed an important activity for all naphtoquinone derivatives.

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Section: Antioxidant Assaymentioning

confidence: 99%

Antioxidant and Antifungal Activity of Naphthoquinones Dimeric Derived from Lawsone

Oliveira¹,

Brighente²,

Lund³

et al. 2017

JBM

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“…Specifically for Polygala molluginifolia , there is no data in the literature showing a clear phytochemical composition and biological effect. Recently, the 3′,4′‐dihydroxy‐6″,6″,6″′,6″′‐tetramethylbis(pyrano[2″,3″:5,6::2″′,3″′:7,8]isoflavone was isolated from the aerial parts of P. molluginifolia as reported by Venzke et al []. This compound exhibits an anti‐inflammatory effect by preventing the inflammation in the mouse pleurisy model through the inhibition of NF‐κB activation [Arruda‐Silva et al, ].…”

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confidence: 99%

Bis‐Pyrano Prenyl Isoflavone Improves Glucose Homeostasis by Inhibiting Dipeptidyl Peptidase‐4 in Hyperglycemic Rats

Altenhofen

Luz

Frederico

et al. 2016

J of Cellular Biochemistry

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Isoflavones widely distributed in plants prevent diabetes. This study investigated the in vivo and in vitro effect of 3',4'-dihydroxy-6″,6″,6″',6″'-tetramethylbis(pyrano[2″,3″:5,6::2″',3″':7,8]isoflavone (bis-pyrano prenyl isoflavone) on glucose homeostasis in hyperglycemic rats. The ethyl acetate fraction from aerial parts of Polygala molluginifolia that contain isoflavones was assayed on glucose tolerance, on in vitro maltase activity and on protein glycation. The isoflavone bis-pyrano prenyl isolated from this fraction was investigated on glucose homeostasis. The in vivo action of the isoflavone exhibits an anti-hyperglycemic effect by improving glucose tolerance, augmenting the liver glycogen, inhibiting maltase activity, and stimulating glucagon-like peptide-1 (GLP-1) and insulin secretion. The in vitro isoflavone inhibits dipeptidyl peptidase-4 (DPP-4) activity since the glucose tolerance was improved in the presence of the isoflavone as much as sitagliptin, an inhibitor of DPP-4. However, the co-incubation with isoflavone and sitagliptin exhibited an additive anti-hyperglycemic action. The isoflavone increased the GLP-1 faster than the positive hyperglycemic group, which shows that the intestine is a potential target. Thus, to clarify the main site of action in which isoflavone improves glucose balance, the in vitro mechanism of action of this compound was tested in intestine using calcium influx as a trigger for the signal pathways for GLP-1 secretion. The isoflavone stimulates calcium influx in intestine and its mechanism involves voltage-dependent calcium channels, phospholipase C, protein kinase C, and stored calcium contributing for GLP-1 secretion. In conclusion, the isoflavone regulates glycaemia by acting mainly in a serum target, the DPP-4 inhibitor. Furthermore, the long-term effect of isoflavone prevents protein glycation. J. Cell. Biochem. 118: 92-103, 2017. © 2016 Wiley Periodicals, Inc.

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“…Other applications of PAMPA such as the prediction of protein binding, lipophilicity determination, and pH profiling have also been reported [10,12,21,22]. Despite the rapid industrial success of PAMPA in the last decade, papers mentioning the use of this HTS technique for studying the passive permeability potential of NPs are sparse [23][24][25][26][27]. The applicability of a modified version of the PAMPA-BBB technique was recently reported in the frame of a CNS-based HTS campaign in order to screen a library of chemically diverse plant extracts [18].…”

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confidence: 99%

Prediction of the Passive Intestinal Absorption of Medicinal Plant Extract Constituents with the Parallel Artificial Membrane Permeability Assay (PAMPA)

et al. 2016

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At the early drug discovery stage, the high-throughput parallel artificial membrane permeability assay is one of the most frequently used in vitro models to predict transcellular passive absorption. While thousands of new chemical entities have been screened with the parallel artificial membrane permeability assay, in general, permeation properties of natural products have been scarcely evaluated. In this study, the parallel artificial membrane permeability assay through a hexadecane membrane was used to predict the passive intestinal absorption of a representative set of frequently occurring natural products. Since natural products are usually ingested for medicinal use as components of complex extracts in traditional herbal preparations or as phytopharmaceuticals, the applicability of such an assay to study the constituents directly in medicinal crude plant extracts was further investigated. Three representative crude plant extracts with different natural product compositions were chosen for this study. The first extract was composed of furanocoumarins (Angelica archangelica), the second extract included alkaloids (Waltheria indica), and the third extract contained flavonoid glycosides (Pueraria montana var. lobata). For each medicinal plant, the effective passive permeability values Pe (cm/s) of the main natural products of interest were rapidly calculated thanks to a generic ultrahigh-pressure liquid chromatography-UV detection method and because Pe calculations do not require knowing precisely the concentration of each natural product within the extracts. The original parallel artificial membrane permeability assay through a hexadecane membrane was found to keep its predictive power when applied to constituents directly in crude plant extracts provided that higher quantities of the extract were initially loaded in the assay in order to ensure suitable detection of the individual constituents of the extracts. Such an approach is thus valuable for the high-throughput, cost-effective, and early evaluation of passive intestinal absorption of active principles in medicinal plants. In phytochemical studies, obtaining effective passive permeability values of pharmacologically active natural products is important to predict if natural products showing interesting activities in vitro may have a chance to reach their target in vivo.

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PAMPA Permeability, Acetylcholinesterase Inhibition and Antioxidant Activity of Pyranoisoflavones fromPolygala molluginifolia(Polygalaceae)

Cited by 8 publications

References 1 publication

Antioxidant and Antifungal Activity of Naphthoquinones Dimeric Derived from Lawsone

Antioxidant and Antifungal Activity of Naphthoquinones Dimeric Derived from Lawsone

Bis‐Pyrano Prenyl Isoflavone Improves Glucose Homeostasis by Inhibiting Dipeptidyl Peptidase‐4 in Hyperglycemic Rats

Prediction of the Passive Intestinal Absorption of Medicinal Plant Extract Constituents with the Parallel Artificial Membrane Permeability Assay (PAMPA)

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