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Discovery and resupply of pharmacologically active plant-derived natural products: A review
While the intrinsic complexity of natural product-based drug discovery necessitates highly integrated interdisciplinary approaches, the reviewed scientific developments, recent technological advances, and research trends clearly indicate that natural products will be among the most important sources of new drugs in the future. Expand
Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review
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Leoligin, the Major Lignan from Edelweiss (Leontopodium nivale subsp. alpinum), Promotes Cholesterol Efflux from THP-1 Macrophages
It is suggested that leoligin induces cholesterol efflux in THP-1-derived macrophages by upregulating ABCA1 and ABCG1 expression, a novel activity that suggests leolIGin as a promising candidate for further studies addressing a possible preventive or therapeutic application in the context of atherosclerosis. Expand
Piperine inhibits ABCA1 degradation and promotes cholesterol efflux from THP‐1‐derived macrophages
Piperine promotes ChE in THP‐1‐derived macrophages by upregulation of ABCA1, which might be mediated by inhibition of calpain activity, and makes the dietary constituent piperine a good candidate to be further explored for therapeutic or preventive applications in the context of atherosclerosis. Expand
Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents.
Through a structure-based molecular hybridization approach, a series of novel benzothiazole derivatives bearing indole-based moiety were designed, synthesized and screened for in vitro antitumorExpand
The Dietary Constituent Falcarindiol Promotes Cholesterol Efflux from THP-1 Macrophages by Increasing ABCA1 Gene Transcription and Protein Stability
Falcarindiol increasesABCA1 protein level by two complementary mechanisms, i.e., promoting ABCA1 gene expression and inhibiting ABCA 1 protein degradation, which lead to enhanced cholesterol efflux. Expand
Part of the Special Issue: Metabolism 2014 - Alterations of metabolic pathways as therapeutic targets Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARg): a review
This work presents a meta-analyses of the chiral stationary phase of Na6(CO3(CO4)(SO4)2, Na2SO4, and its two major racemates, Pioglitazone and Magnolol, which show stationary phase-dependent CHBAs of Na2CO4 and Na2O2 respectively. Expand
Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives as potential c-met inhibitors.
Six series of novel 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives conjugated with aza-aryl formamide/amine scaffords were designed and synthesized through a structure-based molecular hybridization approach and indicated that a 1H-benzo [e] [1,3,4]thiadiazine-3-carboxamide-4,4-dioxide moiety contributed to the antitumor potency. Expand
Novel interactomics approach identifies ABCA1 as direct target of evodiamine, which increases macrophage cholesterol efflux
Using a novel interactomics approach, the Nematic Protein Organisation Technique (NPOT), the identification of ATP-binding cassette transporter A1 (ABCA1), a key membrane transporter contributing to cholesterol efflux (ChE), as a direct binding target of evodiamine is reported. Expand
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.
The discovery of a potent c-Met inhibitor 23n, bearing 2-hydroxy-3-allylphenyl group at R(2) moiety, as a valuable lead molecule, which possessed remarkable cytotoxicity and high selectivity against A549 and HT-29 cell lines with IC50 values of 11 nM and 27 nM clearly indicated that compound 23n is a potent and highly selective c- Met inhibitor. Expand