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Herbs > 10: Nootropics > Flashcards

10: Nootropics Flashcards

1
Q

NOOTROPIC
- used to do what?
- what are the 5 criteria to be considered a nootropic?

A
  • used to enhance memory or other cognitive function
    1. enhance memory and ability to learn/retain
    2. help brain function under disruptive conditions, such as hypoxia and electroconvulsive shock
    3. protect brain from chemical and physical assaults, such as anti-cholinergic drugs and barbituates
    4. increase efficacy of neuronal firing control mechanisms in cortical and sub-cortical regions of the brain
    5. possess few or no side effects and be virtually non-toxic
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2
Q
  • nootropic termed by which scientific in what year?
  • that scientist synthesized what? in what read?
  • mechanism of action ish?
  • acts on what?
A
  • Dr. Cornelie E. Giurgia in 1972
  • synthesized Piracetam in 1964
  • mechanism of action is not well understood, but it isn’t a sedative or stimulant –> it is a POSITIVE ALLOSTERIC MODULATOR OF THE GLUTAMATE AMPA RECEPTOR (BOLD) that is colocalized with cholinergic receptors
  • also acts on ion channels or ion carriers
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3
Q

what are 4 types of nootropics + examples

A
  1. RACETAMS
    - originals
    - piracetam, oxiracetams, phenylpiracetam, aniracetam
  2. CNS STIMULANTS
    - amphetamines (Adderall) (not natural)
    - methylphenidate (Ritalin) (not natural)
    - caffeine and nicotine (natural)
  3. HERBS
    - gingko biloba
    - panax ginseng
    - bacopa monnieri (bacopa)
    - hyperzia serrata (Huperzine A)
    - Plectranthus barbatus (Forskolin from indian coleus)
    - Hericium erinaceus (Lion’s mane mushroom)
  4. NUTRIENTS
    - phosphatidylserine
    - alpha-glycerophosphocholine
    - L-tyrosine
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4
Q

what are 6 ways nootropics work?

A
  1. brain energy
    - enhance metabolic activity and FA transport of/to mitochondria + enhance O2 and nutrient uptake
  2. brain chemicals:
    - supplies precursors, increases synthesis, receptor sensitivity and inhibits breakdown of neurotransmitters (ACh, DA, 5HT, NE, E, GABA)
  3. increase cerebral blood flow
    - promotes NO + vasodilation
    - inhibits homocysteine and oxidative damages to cells + AGEs
  4. brain waves:
    - 5 brain waves
    - some nootropics (L-theanine) can raise alpha brain waves (mild, meditative state for free-flowing creativity)
  5. neuroprotection
    - increase brain’s antioxidant capacity, help fight formation of irregular protein clusters, clearing brain tissue of neurotoxins, protecting brain against negative effects of stress
  6. brain regeneration
    - boost natural brain-boosting growth factors, provide raw neuronal building block materials, maintain brain cell membrane flexibility and plasticity
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5
Q

what are the main functions ish of the main neurotransmitters in brain?
ACh
DA
5HT
NE
EPI
GABA

A

ACh: memory, learning and basic thinking cognition
DA: mood and motivation, pleasure-reward pathway
5HT: relaxation and deep satisfaction (happy hormone)
NE: attention and intense focus
EPI: (adrenaline), intense energy
GABA: downer, sedation and calmness, inhibits excessive excitation

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6
Q

what are 3 categories of synthetic nootropics?

A
  1. RACETAMS
    - piracetam, oxiracetams, phenylpiracetam, aniracetam
  2. CNS STIMULANTS
    - amphetamines (Adderall)
    - methylphenidate (Ritalin)
  3. EUGEROICS
    - modafinil
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7
Q

Modafinil
- what?
- used to treat what due to (A) or (B)
- (A) is caused by what?
- improves (5)

A
  • nootropic! (eugeroic)
  • used to treat sleepiness due to narcolepsy or sleep apnea
  • narcolepsy is caused by a dysfunction in orexin peptides (bold), responsible for wakefulness and sleep suppressing
  • improves fatigue levels, motivation, reaction time, vigilance and brain function (in sleep deprived doctors)
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8
Q

what are 6 natural nootropics?

A
  • gingko biloba (Gingko)
  • panax ginseng (ginseng)
  • bacopa monnieri (bacopa)
  • hyperzia serrata (Huperzine A)
  • Plectranthus barbatus (Forskolin from indian coleus)
  • Hericium erinaceus (Lion’s mane mushroom)
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9
Q

gingko (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: gingko biloba
  • PART USED: leaves and roots
  • MODE OF ADMINISTRATION: tincture, extract
  • BIOACTIVE COMPOUND: ginkgolides
  • COMPOUND CLASS: terepene lactone
  • USES: cognitive enhancer, anxiolytic, enhances blood flow (to brain!)
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10
Q

what are 4 mechanisms of action of gingko?

A
  1. cholinergic:
    - increase uptake and release of Ach = increase memory
  2. monoamine
    - increase uptake of serotonin
    - inhibits MAO
    - reduces b-adrenergic binding and activity
    - reverses age-related decline in a-adrenergic receptors
  3. GABA
    - elevates GABA levels
    - increases glutamic acid decarboxylase activity = degrades glutamate
  4. VASCULAR
    - platelet activation factor inhibitor
    - nitric oxide dependent vasodilation
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11
Q

describe gingko’s mechanism of action: cholinergic
- enhances what?
- where?
- increases what?
- short vs long term memory

A
  • gingko enhances release of ACh and alters cholinergic receptors
  • hippocampus: increased presynaptic uptake of choline!
  • increase in choline uptake due to increase in number of uptake transporters and rate of transport

SHORT-term memory tasks increase uptake of ACh
LONG-term memory reference memory tasks cause an acute increase followed by long-lasting decrease and inhibition (?)

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12
Q

describe gingko’s mechanism of action: monoamines
- 4 sub + describe

A
  • increase uptake of serotonin
  • inhibits MAO (MAO metabolizes NE, 5HT, DA)
  • reduces b-adrenergic binding and activity
  • reverses age-related decline in a-adrenergic receptors
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13
Q

gingko effect on adrenergic receptors?
- what are the effects of NE? (6)

A
  • gingko reduces b-adrenergic binding and activity
    1. mydriasis (dilation of pupils)
    2; decrease salivation
    3. bronchodilation
    4. tachycardia
    5. decrease digestion
    6. decrease urination
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14
Q

describe gingko’s mechanism of action: GABA
(2)

A
  • elevates GABA levels –> bilobalide (bold), a terpene lactone in Gingko, elevates GABA in hippocampus
  • increases glutamic acid decarboxylase activity = degrades glutamate

*glutamic acid decarbozylase catalyzes the decarboxylation of glutamate (exciting) into GABA (relaxing)

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15
Q

describe gingko’s mechanism of action: vascular
(4)

A
  1. inhibits platelet-activating factor –> PAF is a chemical messenger with many biological roles like aggregation of blood platelets
    - inhibit PAF improves microcirculation!
  2. nitric oxide dependent vasodilation
    - gingko improves sexual function by increasing NO production (involved in erections)
  3. potent antioxidant activity
    - flavonoid glycosides: kaempferol, quercetin, apigenin, luteolin, myrcetin
  4. cerebral blood flow: increases blood flow to multiple regions in brain
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16
Q

does gingko work?
- consistent or inconsistent findings?
- ability to reduce what?
- increases (2), reducing risk of what
- MAY help (3)

A
  • inconsistent across all parameters of interest
  • ability to reduce inflammation caused by various conditions
  • increases blood flow to heart and brain, reducing risk of stroke
  • MAY help treat forms of dementia, improve mental performance in healthy people and help treat anxiety
17
Q

ginseng (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: panax ginseng
  • PART USED: root
  • MODE OF ADMINISTRATION: chewed, infusion, extract
  • BIOACTIVE COMPOUND: ginsengosides
  • COMPOUND CLASS: steroid glycosides (cholesterol backbone)
  • USES: cognitive enhance + adaptogen
18
Q

ginseng: 4 mechanisms of action

A
  1. cholinergic: increased ACh release and nicotinic binding
  2. MONOAMINES: turnover of DA, NE and 5HT is increased or decreased depending on dose and duration of use
  3. NO: enhances epithelial synthesis in heart, lungs and kidney
  4. NEUROTROPHIC: increase nerve growth factor (NGF) expression
  5. Ca2+ influx: inhibits calcium channels
19
Q

ginseng general effects
- lowers what?
- MAY do 5 things

A
  • lowers inflammation (too much electrons) due to antioxidant content
    MAY:
  • help improve memory, behaviour and mood
  • help protect against oxidative damage
  • improve symptoms of erectile dysfunction by decreasing oxidative stress
  • protect from cancer (ginsenosides help reduce inflammation and help prevent certain cancers)
  • help fight fatigue and enhance PA by lowering oxidative damage
20
Q

Bacopa (Brahmi) (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: bacopa monnieri
  • PART USED: leaves and stem
  • MODE OF ADMINISTRATION: juice
  • BIOACTIVE COMPOUND: bakosides
  • COMPOUND CLASS: triterpenoid saponin
  • USES: cognitive enhancer
21
Q

4 mechanisms of action of bacopa

A
  1. ANTIOXIDANT/ NEUROPROTECTION
    - prevent lipid peroxidation (involved in Alzheimer’s, Parkinson’s dementia…)
  2. CEREBRAL BLOOD FLOW AND VASODILATION
    - vasodilator by releasing NO in endothelium
  3. NEUROTRANSMITTER POTENTIATION
    - bacopa doubled levels of 5HT (can help enhance learning and memory). glutamate and ACh increased slightly. DA levels lowered
  4. ADHD:
    - 1 study showed bacopa reduced ADHD symptoms like restlessness, poor self control, inattention and impulsivity
22
Q

firmoss (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: Huperzia serrata
  • PART USED: clubmoss
  • MODE OF ADMINISTRATION: isolated compound
  • BIOACTIVE COMPOUND: Huperzine A
  • COMPOUND CLASS: sesquiterpene alkaloid
  • USES: cognitive enhancer
23
Q

Huperzine A (huperzia serrata)
- acts as (2) and crosses what?
used in china to treat what?

A
  • acts as acetylcholinesterase inhibitor AND NMDA antagonist that crosses blood brain barrier!
  • as an NMDA receptor (glutamate receptor) antagonist –> can help prevent neurons from cell death from excitotoxicity
  • China: swelling, fever, blood disorders
24
Q

indian coleus (monograph) (ON EXAM!)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: coleus foskolii (plectranthus barbatus)
  • PART USED: roots
  • MODE OF ADMINISTRATION: isolated compound
  • BIOACTIVE COMPOUND: forskolin
  • COMPOUND CLASS: labdane diterpene
  • USES: cognitive enhancer
25
Q

Forskolin
- from which plant?
- used for what?
- mechanism of action (2)
- synergistic with what?
- anti ___________ effects

A
  • from indian coleus (coleus foskolii)
  • used as weight loss –> may stimulate release of stored fat from fat cells (Dr. Oz lol)
    UNIQUE among nootropics:
    1. increases intracellular levels of cAMP through adenylate cyclase activation –> increased responsiveness to extracellular stimuli
    2. inhibits acetylcholinesterase –> increased ACh levels
  • synergistic with artichoke extract in increasing cAMP levels
  • anti-inflammatory effects
26
Q

why does _______ work better with artichoke extract? (4 steps ish)

A

forskolin! might work as a nootropic, but might work better as part of a “stack”
1. artichoke extract contains LUTEOLIN, a powerful phosphodiesterase (PDE4) inhibitor
2. excess PDE4 degrades cAMP (intracellular messenger within brain cells)
3. cAMP produces proteins needed for neuron and synapse growth, a process called long-term potentiation (LTP) (process where synaptic connections get stronger in response to electrical stimulation in brain
4. PDE4 inhibitor = no more degradation of cAMP = lots of cAMP for LTP!

27
Q

schéma steps of how forskolin and luteolin can increase protein phosphorylation and LTP!

A
  1. agonist of ACh binds to receptor –> activates metabotropic receptor/G-protein (leads to activation of adenylate cyclase)
  2. Forskolin activates AC –> convers ATP to cAMP
  3. luteolin inhibits PDE (PDE usually converts cAMP to 5’AMP)
  4. more cAMP = more PKA = more protein phosphorylation + Long term potentiation!
28
Q

lion’s mane (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:

A
  • SCIENTIFIC NAME: nericium erinaceus
  • PART USED: fruit body
  • MODE OF ADMINISTRATION: whole plant extract
  • BIOACTIVE COMPOUND: hericenon/erinacine
  • COMPOUND CLASS: cyanthin diterpenoids
  • USES: cognitive enhancer
29
Q

mechanism of action of lion’s mane

A
  • nericenones and erinacines isolated from cultured mycelia of lion’s mane ENHANCES NERVE GROWTH FACTOR (NGF) in vitro
  • NGF is a protein that is essential tin the maintenance, survival and regeneration of neurons

*Lion’s mane could regenerate damaged nerve cells –> form new pathways, neuroplasticity

30
Q

summary slide on natural nootropics
- name common name, compound, mechanism (1 to 3)
GINGKO BILOBA
PANAX GINSENG
BACOPA MONNIERI
HYPERZIA SERRATA
PLECTRANTHUS BARBATUS
HERICIUM ERINACEUS
- lion’s mane mushroom)

A

GINGKO BILOBA
- Gingko, ginkgosides
1. increase uptake and release of ACh
2. increases uptake of 5HT
3. reverses age related decline in a adrenergic receptors

PANAX GINSENG
- ginseng, ginsengosides
1. increase uptake and release of ACh
2. increases nerve growth factor

BACOPA MONNIERI
- Bacopa, bacosides
- releases NO and promotes vasodilation and increased cerebral blood flow

HYPERZIA SERRATA
- Firmoss, Huperzine A
- Actylcholinesterase inhibitor –> increases ACh

PLECTRANTHUS BARBATUS
- Indian coleus, Foskolin (with the help of luteolin!)
1. increases cAMP levels
2. inhibits acetylcholinesterase

HERICIUM ERINACEUS
- lion’s mane, hericenone, erinacine
1. increases nerve growth factor

31
Q

what are BDNFs? + found where?
- helps support what? + encourages (2) of (2)
- active in brain areas responsible for (3)
- BDNF clears which neurotransmitter from synaptic cleft –> consequence?

A

brain-derived neurotropic factor –> protein related to nerve growth factor (NDG) and found in brain and PNS
- helps support nerve health and encourages growth and specialization or new nerves (neurogenesis) and synapses (synaptogenesis)
- active in brain areas responsible for learning, memory and higher thinking
- clears GABA from synaptic cleft –> GABA is shuttled into neighbouring astrocytes via adenosine A2A receptor –> consequence: nerve pathways become more excitatory

32
Q

DEFINITIONS:
- used to enhance memory or other cognitive function
- relating to the growth of nervous tissue
- also known as wakefulness-promoting agents and wakefulness-promoting drugs. are a class of drugs that promote wakefulness and alertness

A
  • nootropic
  • Neurotrophic
  • eugeroics
33
Q

Definitions
- nootropic
- Neurotrophic
- eugeroics

A
  • used to enhance memory or other cognitive function
  • relating to the growth of nervous tissue
  • also known as wakefulness-promoting agents and wakefulness-promoting drugs. are a class of drugs that promote wakefulness and alertness

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