Table 2.
The biological activities and molecular effects of pterostilbene.
| Modes/treatments | Model used | Mechanism | References |
|---|---|---|---|
| Inflammation | |||
| 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 [67] |
| Pterostilbene (0.1–1μM) | HUVECs | ↓Monocyte binding, ↓sICAM1, ↓IL-8, ↓MCP-1, ↓sE-selectin, ↓p-eIF2α, ↓ICAM1, ↓MMP9, ↓CRP78 | Liu et al, 2016 [68] |
| Breast cancer | |||
| Pterostilbene (40–80μM) | MCF-7 | ↓Cell viability, ↑Apoptosis, ↑Caspase-3, ↑Bax, ↓Bcl-2, ↑ROS generation, ↓MMP, ↑AMACR | Chakraborty et al, 2010 [69] |
| 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 [18] |
| Pterostilbene (15–50μM) | MCF-7 | ↑Autophagy, ↑Beclin 1, ↑LC3 II, ↑ROS generation | Chakraborty et al, 2012 [70] |
| Prostate cancer | |||
| Pterostilbene (1–25μM) | LNCaP | ↓Cell viability, ↑G1 phase arrest, ↑CDNK1A, ↑CDNK1B, ↓prostate-specific antigen | Wang et al, 2010 [71] |
| Pterostilbene (40–80μM) | PC-3 | ↑Apoptosis, ↑caspase-3, ↑Bax, ↓Bcl-2, ↑ROS generation, ↓MMP, ↑AMACR | Chakraborty et al, 2010 [69] |
| Pterostilbene (40–100μM) | LNCaP | ↓Cell viability, ↑G1 phase arrest, ↑p53, ↑p21, ↑p-AMPK, ↓fatty acid synthase, ↓acetyl CoA carboxylase | Lin et al, 2012 [25] |
| Pterostilbene (40–100μM) | PC-3 | ↓Cell viability, ↑apoptosis, ↑caspase-3, ↑Caspase-9, ↑p-AMPK, ↓fatty acid synthase, ↓acetyl CoA carboxylase | Lin et al, 2012 [25] |
| 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 [19] |
| Pterostilbene (0.004%) | AOM-induced colonic carcinogenesis rat | ↓Tumor multiplicity, ↓PCNA, ↓TNF-α, ↓IL-1β, ↓IL-4 | Paul et al, 2010 [63] |
| Pterostilbene (50μM) | HT-29 | ↓β-catenin, ↓cyclin D1, ↓c-Myc, ↓IκBα,↓phosphorylation of p65 | Paul et al, 2010 [63] |
| Pterostilbene (5–100μM) | HCT-116, HT-29, & Caco-2 | ↓Cell viability, ↓colony formation capacity, ↑apoptosis, ↑caspase-3, ↑PARP | Nutakul et al, 2011 [15] |
| 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 [79] |
| 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 [28] |
| 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 [28] |
| Diabetes | |||
| Pterostilbene (40 mg/kg BW) | Diabetic rats | ↓Blood glucose, ↓Glycosylated hemoglobin, ↑Hexokinase, ↓Glucose-6-phosphatase, ↓Fructose-1,6-bisphosphatase | Pari et al, 2006 [66] |
| 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 [72] |
| 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 [73] |
| Dyslipidemia | |||
| 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 [74] |
| 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 [75] |
| Pterostilbene (10–50μM) | H4IIEC3 cells | PPARα ligand, ↑PPARα gene expression | Rimando et al, 2015 [76] |
| Aging | |||
| 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 [77] |
| 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 [78] |
ACO = acetyl-coA carboxylase; AMACR = α-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 transporter 4; GPx = glutathione peroxidase; HDL-C = high density lipoprotein cholesterol; HO-1 = heme oxygenase-1; HOMA-IR = homeostatic model assessment-insulin resistance; IFN-γ = interferon gamma; IκBα = inhibitor of kappa B; IL-1β = 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 density lipoprotein 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 S6 kinase; PAI-1 = plasminogen activator inhibitor-1; p-AMPK = phosphorylated adenosine monophosphate activated protein kinase; PARP = poly ADP-ribose polymerase; PCNA = proliferating cell nuclear antigen; p-eIF2α = phospho-eIF2α; 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 = soluble intercellular adhesion molecule-1; PPARα = peroxisome proliferator activated receptor alpha; ROS = reactive oxygen species; SOD = superoxide dismutase; TNF-α = tumor necrosis factor-α; VEGF = vascular endothelial growth factor; VLDL-C = very low density lipoprotein cholesterol.