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Constituents from Cistus salvifolius (Cistaceae) Activate Peroxisome Proliferator-Activated Receptor-γ but Not -δ and Stimulate Glucose Uptake by Adipocytes.
MedLine Citation:
PMID:  20922652     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
A number of medicinal/culinary herbs have been reported to improve glucose metabolism and to yield hypoglycemic effects in patients with diabetes. Since stimulation of insulin sensitivity appears to be a potential mechanism, peroxisome proliferator-activated receptor (PPAR) γ is a likely target molecule for small lipophilic compounds derived from endogenous metabolism and nutrition. Functionally, PPAR γ integrates the control of energy, lipid, and glucose homeostasis. In addition, PPAR δ activity is involved in energy expenditure. Therefore the aim of this study was to investigate whether PPAR γ and PPAR δ as well as the stimulation of glucose uptake is activated by botanical products. CISTUS SALVIFOLIUS (Cistaceae) has been identified as a candidate botanical in a preliminary screening of extracts from medicinal plants of Greek flora. In a bioguided approach, crude extracts, fractions and in the end purified compounds have been evaluated for PPAR γ and PPAR δ specific activities using cell-based transactivation assays. Glucose uptake was measured by nonradioactive 2-[ N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxyglucose (2-NBDG) uptake. Concerning PPAR γ several extracts induced reporter gene activity, and clear dose-response patterns (0.1-100 µg/mL) could be established in the case of the cyclohexane and dichloromethane extracts. Isolation of individual compounds from the cyclohexane extract revealed that at least 6 out of 7 compounds isolated were active with TRANS-cinnamic acid showing a clear dose-response pattern. In contrast, they were found to be inactive on PPAR δ. The same compounds, however, were also active in stimulating glucose uptake into 3T3-L1 adipocytes. In summary, the bioguided fractionation of CISTUS SALVIFOLIUS yields PPAR γ stimulating metabolites with differing chemical natures. In conclusion, PPAR γ represents a candidate molecule for the mediation of improvement of glucose metabolism by botanical/nutritional products.
Authors:
Claudia Kühn; Niki Eliza Arapogianni; Maria Halabalaki; Jana Hempel; Nicole Hunger; Jannette Wober; Alexios Leandros Skaltsounis; Günter Vollmer
Publication Detail:
Type:  Journal Article     Date:  2010-10-04
Journal Detail:
Title:  Planta medica     Volume:  77     ISSN:  1439-0221     ISO Abbreviation:  Planta Med.     Publication Date:  2011 Mar 
Date Detail:
Created Date:  2011-03-08     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0066751     Medline TA:  Planta Med     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  346-53     Citation Subset:  IM    
Copyright Information:
© Georg Thieme Verlag KG Stuttgart · New York.
Affiliation:
Molecular Cell Physiology & Endocrinology, Technische Universität Dresden, Dresden, Germany.
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