Activation of PPARγ by Metabolites from the Flowers of Purple Coneflower (<i>Echinacea purpurea</i>)

Christensen, Kathrine Bisgaard; Petersen, Rasmus Koefoed; Petersen, Sten; Kristiansen, Karsten; Christensen, Lars Porskjær

doi:10.1021/np900003a

Cited by 31 publications

(34 citation statements)

References 24 publications

(41 reference statements)

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“…A recent study showed that hexadeca-2E,9Z,12Z,14E-tetraenoic acid IBA (68) has the potential to manage insulin resistance and type-2 diabetes by activation of the peroxisome proliferator activated receptor gamma (PPARg) without stimulation of adipocyte differentiation (Christensen et al, 2009). NAAs with a C 16 to C 20 fatty acid chain length have the highest PPARg affinity.…”

Section: Othersmentioning

confidence: 99%

Alkamid database: Chemistry, occurrence and functionality of plant N-alkylamides

Boonen

Bronselaer

Nielandt

et al. 2012

Journal of Ethnopharmacology

126

109

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a b s t r a c tEthnopharmacological relevance: N-Alkylamides (NAAs) are a promising group of bioactive compounds, which are anticipated to act as important lead compounds for plant protection and biocidal products, functional food, cosmeceuticals and drugs in the next decennia. These molecules, currently found in more than 25 plant families and with a wide structural diversity, exert a variety of biologicalpharmacological effects and are of high ethnopharmacological importance. However, information is scattered in literature, with different, often unstandardized, pharmacological methodologies being used. Therefore, a comprehensive NAA database (acronym: Alkamid) was constructed to collect the available structural and functional NAA data, linked to their occurrence in plants (family, tribe, species, genus). Materials and methods: For loading information in the database, literature data was gathered over the period 1950-2010, by using several search engines. In order to represent the collected information about NAAs, the plants in which they occur and the functionalities for which they have been examined, a relational database is constructed and implemented on a MySQL back-end. Results: The database is supported by describing the NAA plant-, functional-and chemical-space. The chemical space includes a NAA classification, according to their fatty acid and amine structures. Conclusions: The Alkamid database (publicly available on the website http://alkamid.ugent.be/) is not only a central information point, but can also function as a useful tool to prioritize the NAA Q8 choice in the evaluation of their functionality, to perform data mining leading to quantitative structure-property relationships (QSPRs), functionality comparisons, clustering, plant biochemistry and taxonomic evaluations.

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Section: Othersmentioning

confidence: 99%

Alkamid database: Chemistry, occurrence and functionality of plant N-alkylamides

Boonen

Bronselaer

Nielandt

et al. 2012

Journal of Ethnopharmacology

126

109

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“…Crocus sativus Iridaceae C2C12 cells Enhances glucose uptake and the phosphorylation of AMPK/ACC and MAPKs [63] 32 Cryptolepis sanguinolenta Apocynaceae Type 2 diabetic mice Stimulates glucose uptake [64] 33 Curcuma comosa Zingiberaceae Ovariectomized rats Enhances insulin-mediated glucose uptake in skeletal muscle and increases muscle GLUT4 protein levels [65] 34 Cyclea peltata Menispermaceae Type 2 diabetic rats Improves glycogen in peripheral tissue such as skeletal muscle [66] 35 Dryopteris fragrans Dryopteridaceae Streptozotocin rats Improves glucose utilization and insulin resistance [67] 36 Echinacea purpurea Compositae Cultured adipocytes Activates PPARγ and increased insulin-stimulated glucose uptake [68] 37 Elaeis guineensis Arecaceae Healthy adults with pre-diabetes…”

Section: Cornus Officinalismentioning

confidence: 99%

“…[65] On the other hand, alkamide hexadeca-2E,9Z,12Z,14E-tetraenoic acid isobutylamide isolated from Echinacea purpurea was found to improve insulin sensitivity by activating PPARγ with no concurrent stimulation of adipocyte differentiation and increased insulin-stimulated glucose uptake. [68] Aromadendrin, a flavonoid isolated from Gleditsia sinensis has been shown to ameliorate insulin sensitivity in vivo. This compound significantly stimulated insulin-sensitive glucose uptake in both HepG2 cells and 3T3-L1 adipocytes.…”

Section: Xanthium Strumarium Compositae Streptozotocin Diabetic Ratsmentioning

confidence: 99%

“…Alkamide hexadeca-2E,9Z,12Z,14E-tetraenoic acid isobutylamide [68] 9 Gleditsia sinensis Aromadendrin [75] 10 Glycyrrhiza foetida Amorfrutins [39] 11 Hedysarum polybotrys Polysaccharide [76] 12 Schisandra chinensis Lignan [72,122] 13 Lindera aggregate Secoaggregatalactone A [86] 14 Liriope spicata Polysaccharides [87] 15 Litsea coreana Flavonoids [88] 16…”

Section: Echinacea Purpureamentioning

confidence: 99%

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Antidiabetic plants improving insulin sensitivity

Eddouks¹,

Bidi²,

Bouhali³

et al. 2014

Journal of Pharmacy and Pharmacology

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Background Globally, the prevalence of diabetes mellitus is increasing at an alarming rate. This chronic pathology gravely troubled the human health and quality of life. Both insulin deficiency and insulin resistance are involved in the pathophysiology of diabetes mellitus. Moreover, insulin resistance is being diagnosed nowadays in a growing population of diabetic and obese patients, especially in industrialized societies. There are lots of conventional agents available to control and to treat diabetes, but total recovery from this disorder has not been reported up to this date. Plants provided a potential source of hypoglycemic drugs and are widely used in several traditional systems of medicine to prevent diabetes. A few reviews with less attention paid to mechanisms of action have been published on antidiabetic plants. Objectives The present review focuses on the various plants that have been reported to be effective in improving insulin sensitivity associated with diabetes. Key findings In this work, an updated systematic review of the published literature has been conducted to review the antidiabetic plants improving insulin sensitivity and 111 medicinal plants have been reported to have a beneficial effect on insulin sensitivity using several in-vitro and in-vivo animal models of diabetes. Conclusion The different metabolic and cellular effects of the antidiabetic plants improving insulin sensitivity are reported indicating the important role of medicinal plants as potential alternative or complementary use in controlling insulin resistance associated with diabetes mellitus.

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“…Pharmacophore-based virtual screening has only recently been used for the identification of novel ligands of PPARc of synthetic [17,18] or natural [19] origin. Experimentally validated PPARc agonists from plants are hitherto few and include structurally diverse compounds from various sources such as fruits, vegetables, and medicinal plants [20][21][22][23]. Considering that plants have a long history in the traditional treatment of many diseases, including diabetes [24], natural product libraries represent a very promising source of novel PPARc ligands.…”

Section: Introductionmentioning

confidence: 99%

Pharmacophore-driven identification of PPARγ agonists from natural sources

Petersen

Christensen

Assimopoulou

et al. 2010

J Comput Aided Mol Des

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In a search for more effective and safe anti-diabetic compounds, we developed a pharmacophore model based on partial agonists of PPARγ. The model was used for the virtual screening of the Chinese Natural Product Database (CNPD), a library of plant-derived natural products primarily used in folk medicine. From the resulting hits, we selected methyl oleanonate, a compound found, among others, in Pistacia lentiscus var. Chia oleoresin (Chios mastic gum). The acid of methyl oleanonate, oleanonic acid, was identified as a PPARγ agonist through bioassay-guided chromatographic fractionations of Chios mastic gum fractions, whereas some other sub-fractions exhibited also biological activity towards PPARγ. The results from the present work are two-fold: on the one hand we demonstrate that the pharmacophore model we developed is able to select novel ligand scaffolds that act as PPARγ agonists; while at the same time it manifests that natural products are highly relevant for use in virtual screening-based drug discovery.

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Activation of PPARγ by Metabolites from the Flowers of Purple Coneflower (Echinacea purpurea)

Cited by 31 publications

References 24 publications

Alkamid database: Chemistry, occurrence and functionality of plant N-alkylamides

Alkamid database: Chemistry, occurrence and functionality of plant N-alkylamides

Antidiabetic plants improving insulin sensitivity

Pharmacophore-driven identification of PPARγ agonists from natural sources

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