Extensive phytochemical investigation of the polar constituents of Diospyros bipindensis Gürke traditionally used by Baka pygmies

Cesari, I.; Queiroz, Emerson Ferreira; Favre-Godal, Quentin; Marcourt, Laurence; Caccialanza, Gabriele; Moundipa, Paul Fewou; Brusotti, Gloria; Wolfender, Jean‐Luc

doi:10.1016/j.phytochem.2013.09.005

Cited by 10 publications

(5 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In this context, an ethnobotanical survey was conducted by our research group among the pygmies Baka, a community living in the south of Cameroon and possessing a consolidated vernacular knowledge in the field of traditional medicine through the use of medicinal plants. Some of these medicinal plants were selected as candidates to validate their traditional use 19–23 . Among them, Diospyros bipindensis was identified as the most interesting plant for possible activity on PPARs receptors.…”

Section: Introductionmentioning

confidence: 99%

Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis

Brusotti

Montanari

Capelli

et al. 2017

Sci Rep

Self Cite

View full text Add to dashboard Cite

PPAR antagonists are ligands that bind their receptor with high affinity without transactivation activity. Recently, they have been demonstrated to maintain insulin-sensitizing and antidiabetic properties, and they serve as an alternative treatment for metabolic diseases. In this work, an affinity-based bioassay was found to be effective for selecting PPAR ligands from the dried extract of an African plant (Diospyros bipindensis). Among the ligands, we identified betulinic acid (BA), a compound already known for its anti-inflammatory, anti-tumour and antidiabetic properties, as a PPARγ and PPARα antagonist. Cell differentiation assays showed that BA inhibits adipogenesis and promotes osteogenesis; either down-regulates or does not affect the expression of a series of adipogenic markers; and up-regulates the expression of osteogenic markers. Moreover, BA increases basal glucose uptake in 3T3-L1 adipocytes. The crystal structure of the complex of BA with PPARγ sheds light, at the molecular level, on the mechanism by which BA antagonizes PPARγ, and indicates a unique binding mode of this antagonist type. The results of this study show that the natural compound BA could be an interesting and safe candidate for the treatment of type 2 diabetes and bone diseases.

show abstract

Section: Introductionmentioning

confidence: 99%

Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis

Brusotti

Montanari

Capelli

et al. 2017

Sci Rep

Self Cite

View full text Add to dashboard Cite

show abstract

“…The number of natural products included in drug discovery programs decreased in the past decades when automated high throughput platforms were introduced due to the compatibility problems of complex extracts with bioassays, and laborious identification processes of the active principles following the activity profiling. In this context, HPLC-based activity profiling (Cesari et al 2013;Queiroz et al 2014) which can further be coupled with hyphenated spectroscopic methods for dereplication (Queiroz et al 2002(Queiroz et al , 2005 provides a valuable tool for drug discovery of bioactive compounds from complex natural extracts. On the contrary, the field of antimicrobial drug discovery has lacked sensitive assays compatible with automated environments.…”

Section: Resultsmentioning

confidence: 99%

Cell-based bioreporter assay coupled to HPLC micro-fractionation in the evaluation of antimicrobial properties of the basidiomycete fungus Pycnoporus cinnabarinus

Järvinen

Nybond

Marcourt

et al. 2016

Pharmaceutical Biology

Self Cite

View full text Add to dashboard Cite

show abstract

“…Other compounds found included xanthotoxin ( 5) 28 , bothrioclinin ( 6 ) 29 , nodakenin ( 7 ) 30 , and gerberinside ( 8 ) 31 .…”

Section: Resultsmentioning

confidence: 99%

Coumarin derivatives from Ainsliaea fragrans and their anticoagulant activity

Lei

Xue

Liu

et al. 2015

Sci Rep

View full text Add to dashboard Cite

Coumarin derivatives are an important class of C6–C3 plant metabolites that show a variety of bioactivities. Currently, most clinical anticoagulant agents are coumarins, such as warfarin, dicoumarol and acenocoumarol, and patients taking these drugs must be monitored for adverse reactions. In a search for safe and effective anticoagulant compounds from Chinese herbal medicine, a screening procedure on the whole plant of Ainsliaea fragrans was performed. The phytochemical investigation of this plant afforded five new coumarin derivatives, including a pair of natural 4-hydroxycoumarin enantiomers (1), a pair of coumarin enantiomers with a rare polycyclic pyrano[3-2c] carbon skeleton (2) and a 7-hydroxycoumarin derivative (3), together with 5 known biogenetically related compounds (4–8). Enantioseparation of 1 and 2 produced optically pure compounds 1a, 1b, 2a and 2b. The absolute configurations of the new compounds were confirmed by single-crystal X-ray diffraction analysis. In addition, we evaluated the anticoagulant activity of all isolates via activated partial thromboplastin time (APTT), thrombin time (TT) and prothrombin time (PT) assays in vitro and in vivo. Of note, compound 3 displayed potent anticoagulant activity and no significant hepatic or renal toxicity, which could make it a promising agent for further preclinical evaluation for preventing abnormal blood clotting.

show abstract

Extensive phytochemical investigation of the polar constituents of Diospyros bipindensis Gürke traditionally used by Baka pygmies

Cited by 10 publications

References 21 publications

Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis

Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis

Cell-based bioreporter assay coupled to HPLC micro-fractionation in the evaluation of antimicrobial properties of the basidiomycete fungus Pycnoporus cinnabarinus

Coumarin derivatives from Ainsliaea fragrans and their anticoagulant activity

Contact Info

Product

Resources

About