The biological activities and molecular effects of pterostilbene.

Modes/treatments Model used Mechanism References
pterostilbene (1–10μM) 3T3-L1 & RAW 264.7 coculture ↓IL-6 & TNF-α secretion
↓COX-2, ↓iNOS, ↓IL-6, ↓TNF-α, ↓PAI-1, ↓CRP, ↓MCP-1, ↓resistin, ↓leptin,
↓Migration of macrophages toward adipocytes
Hsu et al, 2013 [1]
Pterostilbene (0.1–1μM) HUVECs ↓Monocyte binding, ↓sICAM1, ↓IL-8, ↓MCP-1, ↓sE-selectin, ↓p-eIF2α, ↓ICAM1, ↓MMP9, ↓CRP78 Liu et al, 2016 [2]
Breast cancer
Pterostilbene (40–80μM) MCF-7 ↓Cell viability, ↑Apoptosis, ↑Caspase-3, ↑Bax, ↓Bcl-2, ↑ROS generation, ↓MMP, ↑AMACR Chakraborty et al, 2010 [3]
Pterostilbene (50–100μM) MCF-7 & Bcap-37 ↓Cell viability, ↑Apoptosis, ↑PARP, ↑G1 phase arrest, ↓cyclin D1, ↓β-catenin, ↑autophagy, ↑LC3 II Wang et al, 2012 [4]
Pterostilbene (15–50μM) MCF-7 ↑Autophagy, ↑Beclin 1, ↑LC3 II, ↑ROS generation Chakraborty et al, 2012 [5]
Prostate cancer
Pterostilbene (1–25μM) LNCaP ↓Cell viability, ↑G1 phase arrest, ↑CDNK1A, ↑CDNK1B, ↓prostate-specific antigen Wang et al, 2010 [6]
Pterostilbene (40–80μM) PC-3 ↑Apoptosis, ↑caspase-3, ↑Bax, ↓Bcl-2, ↑ROS generation, ↓MMP, ↑AMACR Chakraborty et al, 2010 [7]
Pterostilbene (40–100μM) LNCaP ↓Cell viability, ↑G1 phase arrest, ↑p53, ↑p21, ↑p-AMPK, ↓fatty acid synthase, ↓acetyl CoA carboxylase Lin et al, 2012 [8]
Pterostilbene (40–100μM) PC-3 ↓Cell viability, ↑apoptosis, ↑caspase-3, ↑Caspase-9, ↑p-AMPK, ↓fatty acid synthase, ↓acetyl CoA carboxylase Lin et al, 2012 [8]
Colon cancer
Pterostilbene (1–30μM) HT-29 ↓Cell viability, ↓cyclin D1, ↓c-Myc, ↑PARP, ↓TNF -α, ↓IL-1β, ↓IFN-γ, ↓iNOS, ↓COX-2 Paul et al, 2009 [9]
Pterostilbene (0.004%) AOM-induced colonic carcinogenesis rat ↓Tumor multiplicity, ↓PCNA, ↓TNF-α, ↓IL-1β, ↓IL-4 Paul et al, 2010 [10]
Pterostilbene (50μM) HT-29 ↓β-catenin, ↓cyclin D1, ↓c-Myc, ↓IκBα,↓phosphorylation of p65 Paul et al, 2010 [10]
Pterostilbene (5–100μM) HCT-116, HT-29, & Caco-2 ↓Cell viability, ↓colony formation capacity, ↑apoptosis, ↑caspase-3, ↑PARP Nutakul et al, 2011 [11]
Pterostilbene (50 ppm & 250 ppm) AOM-induced colonic carcinogenesis mice ↓Aberrant crypt foci, lymphoid nodules & tumors, ↓NF-κB, ↓iNOS,↓COX-2, ↑heme oxygenase-1, ↑Glutathione reductase, ↑Nrf2 Chiou et al, 2011 [12]
Pterostilbene (5–50μM) COLO 205, HCT-116 & HT-29 ↑Apoptosis, ↑caspase-3, -8, -9, ↓mTOR/p70S6K, ↓PI3K/Akt, ↓MAPKs, ↓p-ERK1/2, ↓p-JNK1/2, ↑autophagy, ↑LC3 II Cheng et al, 2014 [13]
Pterostilbene (10 mg/kg BW) COLO 205 xenograft nude mice ↓Tumor volume, ↓tumor weight, ↓COX-2, ↓MMP-9, ↓VEGF, ↓cyclin D1, ↑caspase-3 Cheng et al, 2014 [13]
Pterostilbene (40 mg/kg BW) Diabetic rats ↓Blood glucose, ↓Glycosylated hemoglobin, ↑Hexokinase, ↓Glucose-6-phosphatase, ↓Fructose-1,6-bisphosphatase Pari et al, 2006 [14]
Pterostilbene (4μM & 8μM) INS-1E (insulin-secreting rat insulinoma) β-cell line ↑Nuclear Nrf2, ↑HO-1, ↑CAT, ↑SOD, ↑GPx, ↑Bcl-2, ↓Bax, ↓caspase-3 Bhakkiyalakshmi et al, 2014 [15]
Pterostilbene (15 mg/kg & 50 mg/kg BW) Wistar rats fed an obesogenic diet ↓HOMA-IR, ↑GLUT4, ↑p-Akt/total Akt ratio, ↑cardiotrophin-1, ↑glucokinase Gómez-Zorita et al, 2015 [16]
Pterostilbene (40 mg/kg BW) Streptozotocin-nicotinamide induced type II diabetes rats ↓VLDL-C, ↓LDL-C, ↑HDL-C, ↓triglycerides, ↓free fatty acids, ↓phospholipids Satheesh & Pari, 2008 [17]
Pterostilbene (15 mg/kg & 30 mg/kg BW) Wistar rats fed an obesogenic diet ↓ Adipose tissue weight, ↓ ME, ↓FAS, ↓G6PDH, ↓CPT-1a, ↓ACO Gómez-Zorita et al, 2014 [18]
Pterostilbene (10–50μM) H4IIEC3 cells PPARα ligand, ↑PPARα gene expression Rimando et al, 2015 [19]
Pterostilbene (0.004% or 0.016%) Aged male Fischer rats (19-mo-old) Cognitive behavioral deficits, ↓dopamine release, ↑pterostilbene levels in hippocampus, ↑working memory Joseph et al, 2008 [20]
Pterostilbene (120 mg/kg diet) SAMP8 mice ↓The number of errors over 2-day radial arm water maze test, ↑MnSOD, ↑PPAR-α, ↓phosphorylated JNK, ↓PHF Chang et al, 2012 [21]

ACO=acetyl-coA carboxylase; AMACR=a-methylacyl-CoA recemase; Bcl-2=B-cell leukemia/lymphoma 2; CAT=catalase; CDNK1A=cyclin-dependent kinase inhibitor 1A; CDNK1B=cyclin-dependent kinase inhibitor 1B; COX-2=cyclooxygenase-2; CPT-1a=carnitine palmitoyl-transferase 1a; CRP=C-reactive protein; FAS=fatty acid synthase; G6PDH=glucose-6-phosphate dehydrogenase; GLUT4=glucose transporter4; GPx=glutathione peroxidase; HDL-C=high density lipoprotein cholesterol; HO-1=heme oxygenase-1; HOMA-IR=homeostatic modelassessment-insulin resistance; IFN-g=interferon gamma; IkBa=inhibitor of kappa B; IL-1b=interleukin 1 beta; IL-4=interleukin 4; IL-6=interleukin 6; IL-8=interleukin 8; iNOS=inducible nitric oxide synthase; LC3 II=autophagy-related protein light chain 3 II; LDL-C=low densitylipoprotein cholesterol; MAPKs=mitogen-activated protein kinases; MCP-1=monocyte chemoattractant protein-1; ME=malic enzyme; MMP=matrix metallopeptidase; mTOR=mammalian target of rapamycin; Nrf2=NF-E2-related factor 2; p70S6K=70 kDa ribosomal protein S6kinase; PAI-1=plasminogen activator inhibitor-1; p-AMPK=phosphorylated adenosine monophosphate activated protein kinase; PARP=polyADP-ribose polymerase; PCNA=proliferating cell nuclear antigen; p-eIF2a=phospho-eIF2a; p-ERK1/2=phosphorylated-extracellular signal-regulated kinase 1/2; PHF=paired helical filaments; PI3K=phosphatidylinositol 3-kinase; p-JNK1/2=phospho-JNK1/2; sICAM1=solubleintercellular adhesion molecule-1; PPARa=peroxisome proliferator activated receptor alpha; ROS=reactive oxygen species; SOD=superoxidedismutase; TNF-a=tumor necrosis factor-a; VEGF=vascular endothelial growth factor; VLDL-C=very low density lipoprotein cholesterol.

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