- NOVEL CARBONATE ANALOGUES BEARING PTEROSTILBENE AMINO ACIDS FOR THE TREATMENT OF NON-ALCOHOLIC FATTY LIVER DISEASE AND NON-ALCOHOLIC STEATOHEPATITIS
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A series of novel analogs of water soluble pterostilbene amino acid bearing carbonates were synthesized, which show activities in treating a non-alcoholic fatty liver disease and a nonalcoholic steatohepatitis (NASH).
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Page/Page column 30; 33
(2021/12/31)
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- Syntheses of resveratrol and its hydroxylated derivatives as radical scavenger and tyrosinase inhibitor
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Eight hydroxylated stilbene derivatives including resveratrol, desoxyrhapontigenin and piceatannol as potential radical scavenger and tyrosinase inhibitor are synthesized using optimized Wittig-Horner reaction for excellent trans-selectivity in good yields. Antioxidant activity was tested against ABTS radical and tyrosinase inhibitory activity was performed with L-tyrosine as the substrate based on previous procedure with some modification. In general, catecholic stilbenes showed stronger activity against ABTS radical and resorcinolic moiety showed stronger tyrosinase inhibitory activity. Synthetic piceatannol which containing both catecholic and resorcinolic moieties showed the strongest activity in both as ABTS radical scavenger and tyrosinase inhibitor with IC50 values of 4.1 and 8.6 μM, respectively.
- Lee, Hyun Suck,Lee, Byung Won,Kim, Mi Ran,Jun, Jong-Gab
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experimental part
p. 971 - 975
(2010/10/21)
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- Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents
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Resveratrol 1 (3,4′,5-trihydroxy-trans-stilbene), a phytoalexin present in grapes and other food products, has recently been suggested as a potential cancer chemopreventive agent based on its striking inhibitory effects on cellular events associated with cancer initiation, promotion, and progression. This triphenolic stilbene has also displayed in vitro growth inhibition in a number of human cancer cell lines. In this context, a series of cis- and trans-stilbene-based resveratrols were prepared with the aim of discovering new lead compounds with clinical potential. All the synthesized compounds were tested in vitro for cell growth inhibition and the ability to induce apoptosis in HL60 promyelocytic leukemia cells. The tested trans-stilbene derivatives were less potent than their corresponding cis isomers, except for trans-resveratrol, whose cis isomer was less active. The best results were obtained with compounds 11b and 7b, the cis-3,5-dimethoxy derivatives of rhapontigenin 10a (3,5,3′-trihydroxy-4′methoxy-transstilbene) and its 3′-amino derivative 10b, respectively, which showed apoptotic activity at nanomolar concentrations. The corresponding trans isomers 12b and 8b were less active both as antiproliferative and as apoptosis-inducing agents. Of interest, 11b and 7b were active toward resistant HL60R cells and their activity was higher than that of several classic chemotherapeutic agents. The flow cytometry assay showed that at 50 nM compounds 7b or 11b were able to recruit almost all cells in the apoptotic sub-G0-G1 peek, thus suggesting that the main mechanism of cytotoxicity of these compounds could be the activation of apoptosis. These data indicate unambiguously that structural alteration of the stilbene motif of resveratrol can be extremely effective in producing potent apoptosis-inducing agents.
- Roberti, Marinella,Pizzirani, Daniela,Simoni, Daniele,Rondanin, Riccardo,Baruchello, Riccardo,Bonora, Caterina,Buscemi, Filippo,Grimaudo, Stefania,Tolomeo, Manlio
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p. 3546 - 3554
(2007/10/03)
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- Studies on Rhubarb (Rhei Rhizoma). XIV. Isolation and Characterization of Stilbene Glucosides from Chinese Rhubarb
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Two major stilbene glucosides (1 and 2) have been newly isolated from Chinese rhubarb (commercial name: Gaoh, second grade), and characterized on the basis of chemical and spectroscopic evidence as piceatannol 4'-O-β-D-glucopyranoside (1) and its 6''-O-gallate (2).In addition, high-performance liquid chromatographic analysis has led to the characterization of minor components including sennoside, anthraquinones, and other stilbenes.Keywords- rhubarb; Polygonaceae; stilbene glucoside; stilbene glucoside gallate; piceatannol; chemical evaluation; HPLC
- Kashiwada, Yoshiki,Nonaka, Gen-Ichiro,Nishioka, Itsuo,Nishizawa, Makoto,Yamagishi, Takashi
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p. 1545 - 1549
(2007/10/02)
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