生物活性

• 描述Resveratrol inhibits the activity of Cyclooxygenase, lipooxygenase, PKCs and p56, ERK1, JNK1, p38, IKK β, Src, STAT3, Ribonucleotide Reductase, DNA polymerases α and δ, PKD, PKC α, Quinone reductase 2, and Aromatase with IC50 of 0.035-60 μM. Resveratrol is also an activator of Adenylyl cyclase and AMPK with EC50 of 0.8 μM and 50 μM, respectively. The roles of Resveratrol as inhibitor or activator enable its effects on decreasing cell inflammatory associated behaviors, growth inhibition and induction of apoptosis in cancer cells, reversal of endothelin-1 stimulated cell responses, inhibition of phorbol ester-induced expression of COX-2, inhibition of DNA synthesis in cell, resistance to menadione-induced cell death, and improvement of cell mitochondrial function and glucose/lipid metabolism.
  Resveratrol is also an activator of sirtuins. Resveratrol lowers the Michaelis constant of SIRT1 for both the acetylated substrate and NAD, and increases cell survival by stimulating SIRT1-dependent deacetylation of p53. In yeast, Resveratrol mimics calorie restriction by stimulating Sir2, increasing DNA stability and extending lifespan.
  Resveratrol is effective at protecting isolated rat hearts against ischemia/reperfusion injury via its antioxidant activity, with improved recovery of developed pressure and aortic flow, reduction of malondialdehyde concentrations and reduction of infarct size.^[1][2]
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  HEK293 cells	-	Function assay	48 h	Inhibition of TNF-alpha-induced NF-kappaB activity expressed in HEK293 cells after 48 hrs by luciferase reporter gene assay, IC50=0.173 μM	20527891
  HEK293T cells	-	Function assay	-	Inhibition of TNF-alpha-induced NF-kappaB activation in HEK293T cells, IC50=20 μM	17125270
  human 293 cells	-	Function assay	24 h	Inhibition of TNFalpha induced NF-kappaB activation in human 293 cells after 24 hrs by luciferase reporter gene assay, IC50=16.1 μM	18487053

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• 动物研究
  剂量	Rat: 10 mg/kg, 100 mg/kg[7] (i.g.) Mice: 1 mg/kg - 5 mg/kg[7] (i.p.), 150 mg/kg[7] (p.o.) Nude Mice: 25 mg/kg[7] (i.p.)
  给药途径	i.g., p.o., i.p.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00920556	Multiple Myeloma	Phase 2	Terminated(Study terminated.24... more >> subjects enrolled;provided adequate data for decision making.) Collapse <<	-	Denmark ... more >> GSK Investigational Site Vejle, Denmark, 7100 United Kingdom GSK Investigational Site Sutton, Surrey, United Kingdom, SM2 5NG GSK Investigational Site Birmingham, United Kingdom, B15 2TH GSK Investigational Site Leeds, United Kingdom, LS9 7TF GSK Investigational Site London, United Kingdom, EC1A 7BE Collapse <<
  NCT00654667	Insulin Resistance	Phase 2	Withdrawn(no participant enrol... more >>lment) Collapse <<	-	United States, California ... more >> University of California San Francisco, California, United States, 94143-0608 Collapse <<
  NCT02256540	Endothelial Dysfunction	Not Applicable	Active, not recruiting	January 2019	United States, Colorado ... more >> University of Colorado Anschutz Medical Campus Aurora, Colorado, United States, 80045 Collapse <<

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• 参考文献

• [1] Pirola L, Frojdo S. Resveratrol: one molecule, many targets. IUBMB Life. 2008 May;60(5):323-32.

  [2] Howitz KT, Bitterman KJ, et al. Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan. Nature. 2003 Sep 11;425(6954):191-6.

  [3] Zunino SJ, Storms DH, et al. Resveratrol given intraperitoneally does not inhibit the growth of high-risk t(4;11) acute lymphoblastic leukemia cells in a NOD/SCID mouse model. Int J Oncol. 2012;40(4):1277-84.

  [4] Thirunavukkarasu M, Penumathsa SV, et al. Resveratrol alleviates cardiac dysfunction in streptozotocin-induced diabetes: Role of nitric oxide, thioredoxin, and heme oxygenase. Free Radic Biol Med. 2007;43(5):720-9.

  [5] Harper CE, Cook LM, et al. Genistein and resveratrol, alone and in combination, suppress prostate cancer in SV-40 tag rats. Prostate. 2009;69(15):1668-82.

  [6] Singh M, Parent S, et al. Resveratrol modulates the expression of PTGS2 and cellular proliferation in the normal rat endometrium in an AKT-dependent manner. Biol Reprod. 2011;84(5):1045-52.

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