Neuro-Anti Inflammatories and Antioxidants

Potent psychoactive and neuroactive chemicals that play key roles in modulating receptor sites, synaptic enzymes, membrane structures, cerebral perfusion, biogenic processes, neuroendocrine regulation and more.


Neuro-Anti Inflammatories - BioPQQ

BioPQQ

Overview:
PQQ is a quinone molecule with a potent anti-oxidant and neuroprotective effect. Studies indicate that PQQ can help prevent cognitive decline.

Scientific Name:
Pyrroloquinoline quinone

Mechanisms:

  • PQQ reduces oxidants and is continuously recycled into its active form by glutathione[1]
  • Increases the production of mitochondria and improves their efficiency – can act as a growth factor after prolonged intake[2]
  • Decreases the production of some anti-inflammatory molecules such as IL-6[3]
  • Regulates NMDA glutamate receptor activity – reduces excitoxicity and increases neuroprotection[4]
  • Increases NGF synthesis – promotes neuronal growth and survival[5]
  • Neuroprotective role in aged individuals – attenuates neurodegenerative and age-related cognitive decline[6]
  • Can improve sleep and decrease fatigue and stress[7]
References

[1] Mukai K, et al (2011). Kinetic study of the quenching reaction of singlet oxygen by Pyrroloquinolinequinol (PQQH(2), a reduced form of Pyrroloquinolinequinone) in micellar solution. J Agric Food Chem, 59(5):1705-12. doi: 10.1021/jf104420y
[2] Chowanadisai W, et al (2010). Pyrroloquinoline quinone stimulates mitochondrial biogenesis through cAMP response element-binding protein phosphorylation and increased PGC-1alpha expression. J Biol Chem, 285(1):142-52. doi: 10.1074/jbc.M109.030130
[3] Harris CB, et al (2013). Dietary pyrroloquinoline quinone (PQQ) alters indicators of inflammation and mitochondrial-related metabolism in human subjects. J Nutr Biochem, 24(12):2076-84. doi: 10.1016/j.jnutbio.2013.07.008
[4] Aizenman E, et al (1992). Interaction of the putative essential nutrient pyrroloquinoline quinone with the N-methyl-D-aspartate receptor redox modulatory site. J Neurosci, 12(6):2362-9. doi: 10.1074/jbc.M109.030130
[5] Yamaguchi K, et al (1993). Stimulation of nerve growth factor production by pyrroloquinoline quinone and its derivatives in vitro and in vivo. Biosci Biotechnol Biochem, 57(7):1231-3. doi: 10.1271/bbb.57.1231
[6] Itoh Y, et al (2016). Effect of the Antioxidant Supplement Pyrroloquinoline Quinone Disodium Salt (BioPQQ™) on Cognitive Functions. Adv Exp Med Biol, 876:319-25. doi: 10.1007/978-1-4939-3023-4_40
[7] Nakano M, et al (2012). Effects of Oral Supplementation with Pyrroloquinoline Quinone on Stress, Fatigue, and Sleep. Funct Foods Health Dis, 2(8) 307-324

Neuro-Anti Inflammatories - Quercetin

Quercetin

Overview:
Quercetin is a bioflavonoid found in fruits and vegetables, particularly in apples. Quercetin has antioxidant and neuroprotective effects contributing to a delayed cognitive decline.

Scientific Name:
3, 4, 5, 7-pentahydroxylflavone

Mechanisms:

  • Adenosine receptor antagonist – although more potent than caffeine, its lower bioavailability leads to a lower magnitude of effects[1]
  • Protects neurons from toxins, reactive oxygen species, and peroxides[2,3]
  • Decreases NO release by increasing heme-oxygenase-1 expression[4]
  • Anti-inflammatory action in the brain – decreases the production of some proinflammatory molecules, namely TNF-α and IL-1 α[5]
  • Can regulate estrogen and androgen levels[6]
References

[1] Olson CA, et al (2010). Effects of 2 adenosine antagonists, quercetin and caffeine, on vigilance and mood. J Clin Psychopharmacol, 30(5):573-8. doi: 10.1097/JCP.0b013e3181ee0f79
[2] Sasaki N, et al (2003). Protective effects of flavonoids on the cytotoxicity of linoleic acid hydroperoxide toward rat pheochromocytoma PC12 cells. Chem Biol Interact, 145(1):101-16. doi: 10.1016/S0009-2797(02)00248-X
[3] Shirai M, et al (2006). Effect of a conjugated quercetin metabolite, quercetin 3-glucuronide, on lipid hydroperoxide-dependent formation of reactive oxygen species in differentiated PC-12 cells. Free Radic Res, 40(10):1047-53. doi: 10.1080/10715760600794287
[4] Chen JC, et al (2005). Inhibition of iNOS gene expression by quercetin is mediated by the inhibition of IkappaB kinase, nuclear factor-kappa B and STAT1, and depends on heme oxygenase-1 induction in mouse BV-2 microglia. Eur J Pharmacol, 521(1-3):9-20. doi: 10.1016/j.ejphar.2005.08.005
[5] Bureau G, et al (2005). Resveratrol and quercetin, two natural polyphenols, reduce apoptotic neuronal cell death induced by neuroinflammation. J Neurosci Res, 86(2):403-10. doi: 10.1002/jnr.21503
[6] Rice S, et al (2006). Phytoestrogens and their low dose combinations inhibit mRNA expression and activity of aromatase in human granulosa-luteal cells. J Steroid Biochem Mol Biol, 101(4-5):216-25. doi: 10.1016/j.jsbmb.2006.06.021

Neuro-Anti Inflammatories - Curcumin

Curcumin

Overview:
Curcumin is a polyphenolic compound extracted from turmeric (Curcuma long), with potent anti-inflammatory and neuroprotective effects. There are indications that curcumin may improve memory and delay aging.

Scientific Name:
Diferuloylmethane

Mechanisms:

  • Curcumin’s bioavailability is enhanced by piperine[1]
  • Reduces COX-2 production induced by inflammatory cytokines – potent anti-inflammatory effect[2]
  • Anti-aging properties – diminishes oxidative stress, upregulates antioxidant genes and downregulates age-related genes[3]
  • Reduces the production of iNOS, Lysiyl oxidase (LOX), and Phospholipase A2[2,4,5]
  • Can act on TrkB receptors and protects neurons from glutamate excitotoxicity[6]
  • Interacts with dopamine receptors and increases dopamine levels – antidepressant activity[7]
  • Can increase BDNF levels[6]
  • Can significantly reduce chronic pain[8]
References

[1] Shoba G, et al (1998). Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med, 64(4):353-6. doi: 10.1055/s-2006-957450
[2] Camacho-Barquero L, et al (2007). Curcumin, a Curcuma longa constituent, acts on MAPK p38 pathway modulating COX-2 and iNOS expression in chronic experimental colitis. Int Immunopharmacol, 7(3):333-42. doi: 10.1016/j.intimp.2006.11.006
[3] Wu A, et al (2006). Dietary curcumin counteracts the outcome of traumatic brain injury on oxidative stress, synaptic plasticity, and cognition. Exp Neurol, 197(2):309-17. doi: 10.1016/j.expneurol.2005.09.004
[4] Huang CS, et al (2013). Long-term ethanol exposure-induced hepatocellular carcinoma cell migration and invasion through lysyl oxidase activation are attenuated by combined treatment with pterostilbene and curcumin analogues. J Agric Food Chem, 61(18):4326-35. 10.1021/jf4004175
[5] Dileep KV, et al (2013). Molecular docking studies of curcumin analogs with phospholipase A2. Interdiscip Sci, 3(3):189-97. doi: 10.1007/s12539-011-0090-9
[6] Wang R, et al (2008). Curcumin protects against glutamate excitotoxicity in rat cerebral cortical neurons by increasing brain-derived neurotrophic factor level and activating TrkB. Brain Res. 2008 May 19;1210:84-91. doi: 10.1016/j.brainres.2008.01.104
[7] Chang XR, et al (2016). Analysis of anti-depressant potential of curcumin against depression induced male albino wistar rats. Brain Res, pii: S0006-8993(16)30135-4. doi: 10.1016/j.brainres.2016.03.010
[8] Belcaro G, et al (2010). Efficacy and safety of Meriva®, a curcumin-phosphatidylcholine complex, during extended administration in osteoarthritis patients. Altern Med Rev, 15(4):337-44. PMID: 21194249

Neuro-Anti Inflammatories - Algal DHA

Algal DHA

Overview:
DHA is a structural omega-3 fatty acid with neuroprotective and nootropic effects. DHA has been shown to improve executive function, memory and learning..

Scientific Name:
Docosahexaenoic acid extracted from algae

Mechanisms:

  • DHA is the most abundant omega-3 fatty acid in the brain – main structural component of the neuronal cell membrane[1]
  • Modulates the levels of dopamine, adrenaline and noradrenaline in the brain and downregulates the HPA axis – antidepressant effect[1,2]
  • DHA modulates the transport of choline, glycine, and taurine, the function of some potassium channels, and the function of rhodopsin in synaptic vesicles[3]
  • Decreases neuronal susceptibility to oxidative stress[4]
  • Decreases the production of proinflammatory molecules and increases the levels of anti-inflammatory molecules and neuroprotectins[5]
  • Slows the rate of telomere shortening – chromosomic marker of aging[5]
  • Increased protection from neurodegeneration and decreased age-related memory loss[5]
References

[1] Lauritzen L, et al (2001). The essentiality of long chain n-3 fatty acids in relation to development and function of the brain and retina. Prog Lipid Res, 40(1-2):1-94. doi: 10.1016/S0163-7827(00)00017-5
[2] Jiang LH, et al (2012). Pure docosahexaenoic acid can improve depression behaviors and affect HPA axis in mice. Eur Rev Med Pharmacol Sci, 16(13):1765-73. PMID: 23208960
[3] Spector AA (1999). Essentiality of fatty acids. Lipids, 34 Suppl:S1-3. doi: 10.1007/BF02562220
[4] North JA, et al (1994). Cell fatty acid composition affects free radical formation during lipid peroxidation. Am J Physiol, 267(1 Pt 1):C177-88. PMID: 8048478
[5] Bazan NG, et al (2011). Docosahexaenoic acid signalolipidomics in nutrition: significance in aging, neuroinflammation, macular degeneration, Alzheimer’s, and other neurodegenerative diseases. Annu Rev Nutr, 31:321-51. doi: 10.1146/annurev.nutr.012809.104635

Neuro-Anti Inflammatories - Green Tea Extract

Green Tea Extract

Overview:
Green tea extract is rich in polyphenols with neuroprotective and nootropic effects. Green tea extract can enhance memory and learning abilities and delay aging.

Scientific Name:
EGCG – Epigallocatechin-3-gallate from Camellia Sinensis

Mechanisms:

  • Polyphenols in green tea include catechins, theaflavins, tannins, and flavonoids, all with antioxidant and anti-inflammatory properties – anti-aging effect[1]
  • Synergistic with quercetin – increased bioavailability of catechins[2]
  • Synergistic with L-Theanine in inhibiting acetylcholinesterase and enhancing cognitive effects[3]
  • The catechin EGCG is the most abundant and potent polyphenol in green tea[4]
  • EGCG can improve cognitive function by increasing the production of neural progenitor cells[5]
  • Increases blood flow[6]
  • May reduce anxiety and fatigue[7,8]
References

[1] Khan N & Mukhtar H (2013). Tea and health: studies in humans. Curr Pharm Des, 19(34):6141-7. doi: 10.2174/1381612811319340008
[2] Wang P, et al (2012). Quercetin increased bioavailability and decreased methylation of green tea polyphenols in vitro and in vivo. Food Funct, 3(6):635-42. doi: 10.1039/c2fo10254d
[3] Kim TI, et al (2008). Improvement of Memory Impairment by the Combination of Green Tea Extract and L-Theanine through Inhibition of Acetylcholinesterase Activity in Mice (link)
[4] Bhagwat S, et al (2011). USDA Database for the Flavonoid Content of Selected Foods, Release 3. Agricultural Research Service, U.S. Department of Agriculture. (link)
[5] Wang Y, et al (2012). Green tea epigallocatechin-3-gallate (EGCG) promotes neural progenitor cell proliferation and sonic hedgehog pathway activation during adult hippocampal neurogenesis. Mol Nutr Food Res, 56(8):1292-303. doi: 10.1002/mnfr.201200035
[6] Ras RT, et al (2011). Tea consumption enhances endothelial-dependent vasodilation; a meta-analysis. PLoS One, 6(3):e16974. doi: 10.1371/journal.pone.0016974
[7] Vignes M, et al (2006). Anxiolytic properties of green tea polyphenol (-)-epigallocatechin gallate (EGCG). Brain Res, 1110(1):102-15. doi: 10.1016/j.brainres.2006.06.062
[8] Sachdeva AK, et al (2010). Protective effect of epigallocatechin gallate in murine water-immersion stress model of chronic fatigue syndrome. Basic Clin Pharmacol Toxicol, 106(6):490-6. doi 10.1111/j.1742-7843.2009.00525.x

Neuro-Anti Inflammatories - Bioperine

Bioperine

Overview:
Piperine is an alkaloid found in black pepper (Piper nigrum) with anti-inflammatory and nootropic effects. Piperine can boost memory and focus and improve executive function.

Scientific Name:
Pentadienoyl-2-piperidine from Piper nigrum

Mechanisms:

  • Increases the absorption and bioavailability of a number of nutrients, including vitamin C, vitamin B6 and EGCG[1]
  • Highly synergistic with curcumin – enhances its bioavailability and its anti-inflammatory effects[2]
  • Increases serotonin and dopamine levels – antidepressant effects[3]
  • Analgesic properties – activates TRPV1 ion channels on nociceptive (pain-sensing) neurons[4]
  • Increases motivation, attention and reasoning skills – productivity enhancer[5]
References

[1] Lambert JD, et al (2004). Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice. J Nutr, 134(8):1948-52. PMID: 15284381
[2] Shoba G, et al (1998). Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med, 64(4):353-6. doi: 10.1055/s-2006-957450
[3] Li S, et al (2007). Antidepressant-like effects of piperine and its derivative, antiepilepsirine. J Asian Nat Prod Res, 9(3-5):421-30. PMID: 17701559
[4] McNamara FN, et al (2005). Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1). Br J Pharmacol, 144(6):781-90. doi: 10.1038/sj.bjp.0706040
[5] Wattanathorn J, et al (2008). Piperine, the potential functional food for mood and cognitive disorders. Food Chem Toxicol, 46(9):3106-10. doi: 10.1016/j.fct.2008.06.014