Design, synthesis, and discovery of stilbene derivatives based on lithospermic acid B as potent protein tyrosine phosphatase 1B inhibitors

Jung, Mankil; Lee, Yongnam; Park, Moonsoo; Kim, Hanjo; Kim, Heekyeong; Lim, Eunyoung; Tak, Jungae; Sim, Minjoo; Lee, Dong‐Eun; Namsoo, Park; Oh, Won Keun; Hur, Kyu Yeon; Kang, Eun Seok

doi:10.1016/j.bmcl.2007.06.016

Cited by 21 publications

(7 citation statements)

References 28 publications

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“…Furthermore, treatment with chrysophanol and physcion strongly enhanced insulin sensitivity, which was confirmed by an observation that treatment with these 2 compounds led to a dramatic increase in both tyrosine phosphorylation of the insulin receptor (IR) and Akt phosphorylation. Several stilbene derivatives showed potent PTP1B inhibitory activity (15). Because RU contains many kinds of anthranoids and stilbenes (9), its metabolic regulatory effects might be due to such compounds.…”

Section: Discussionmentioning

confidence: 99%

Anti-obesity and hypolipidemic effects of Rheum undulatum in high-fat diet-fed C57BL/6 mice through protein tyrosine phosphatase 1B inhibition

Lee¹,

Yoon²,

Hwang³

et al. 2012

BMB Reports

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Protein tyrosine phosphatase 1B (PTP1B) is important in the regulation of metabolic diseases and has emerged as a promising signaling target. Previously, we reported the PTP1B inhibitory activity of Rheum undulatum (RU). In the present study, we investigated the metabolic regulatory effects of RU in a high-fat diet (HFD) model. RU treatment significantly blocked body weight gain, which was accompanied by a reduction of feed efficiency. In addition, it led to a reduction of liver weight mediated by overexpression of PPARα and CPT1 in the liver, and an increase in the expression of adiponectin, aP2, and UCP3 in adipose tissue responsible for the reduction of total and LDL-cholesterol levels. Chrysophanol and physcion from RU significantly inhibited PTP1B activity and strongly enhanced insulin sensitivity. Altogether, our findings strongly suggest that 2 compounds are novel PTP1B inhibitors and might be considered as anti-obesity agents that are effective for suppressing body weight gain and improving lipid homeostasis. [BMB reports 2012; 45(3): 141-146]

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Section: Discussionmentioning

confidence: 99%

Anti-obesity and hypolipidemic effects of Rheum undulatum in high-fat diet-fed C57BL/6 mice through protein tyrosine phosphatase 1B inhibition

Lee¹,

Yoon²,

Hwang³

et al. 2012

BMB Reports

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“…PdCl 2 was purchased from Heraeus South Africa and used as received. [PdCl 2 (MeCN) 2 ], 22 3,5-di- tert -butylpyrazole, 23 3,5-diphenylpyrazole 24 and methyl-4-(chloromethyl)benzoate 25 were synthesized according to literature procedures.…”

Section: Methodsmentioning

confidence: 99%

Synthesis, characterization and evaluation of bulky bis(pyrazolyl)palladium complexes in Suzuki–Miyaura cross-coupling reactions

2018

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“…The organic layer was washed with saturated NaHCO 3 aq. and then brine, dried over Na 2 SO 4 and evaporated [49,50]. The residue was purified by silica gel column chromatography using n-hexane:AcOEt (3:1 and 1:1) as eluent to afford amides.…”

Section: General Syntheticmentioning

confidence: 99%

Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages

Gürkan¹,

Karabay²,

Büyükbingöl³

et al. 2011

European Journal of Medicinal Chemistry

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Design, synthesis, and discovery of stilbene derivatives based on lithospermic acid B as potent protein tyrosine phosphatase 1B inhibitors

Cited by 21 publications

References 28 publications

Anti-obesity and hypolipidemic effects of Rheum undulatum in high-fat diet-fed C57BL/6 mice through protein tyrosine phosphatase 1B inhibition

Anti-obesity and hypolipidemic effects of Rheum undulatum in high-fat diet-fed C57BL/6 mice through protein tyrosine phosphatase 1B inhibition

Synthesis, characterization and evaluation of bulky bis(pyrazolyl)palladium complexes in Suzuki–Miyaura cross-coupling reactions

Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages

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