Blood-Brain Barrier Study Notes
Blood-Brain Barrier Overview
Source: Alahmari (2021). Neural Plasticity – Review Article
Related Course: MCB5130 – DVM2029 – Block 3
Brain Functions
Blood vessels provide essential resources to the brain:
Oxygen
Nutrients
Energy
Metabolites
Blood vessels also remove metabolic waste products such as CO2.
Neurovascular coupling (also known as functional hyperemia):
Refers to rapid changes in local blood perfusion that respond to neuronal activity, resulting in increases in:
Blood supply
Oxygen
Introduction of the Blood-Brain Barrier (BBB), also referred to as the hematoencephalic barrier.
Overview of the Blood-Brain Barrier (BBB)
Definition: The BBB is a dynamic, semipermeable, and highly selective system existing within the cerebral microvessels of most vertebrates.
Historical Background
Paul Ehrlich (Late 19th century): Conducted experiments involving the injection of aniline dyes into the blood of experimental animals, observing that all organs were stained except for the brain, indicating the presence of a barrier.
Other historical figures mentioned:
Edwin Goldmann
Lina Stern
Structural Features of the BBB
The BBB is characterized by a selective and semi-permeable membrane separating the blood from the interstitial fluid (extracellular fluid) in the brain.
Regulates the movement of molecules and ions between the blood (microvasculature) and the brain.
Essential for proper neuronal function.
Maintains a stable environment for the brain:
Neurons do not regenerate.
Environment is evolutionarily conserved across vertebrates.
Mechanism of Action of the BBB
Components of the BBB include:
Endothelial cells
Pericytes
Capillary basement membrane (basal lamina)
Astrocyte end-feet
Microglia
These components collectively protect the brain from:
Toxins
Drugs
Microorganisms
They also provide nutrients and help maintain a homeostatic internal environment within the central nervous system (CNS).
Neurovascular Unit (NVU)
Key components of the NVU:
Neurons
Pericytes
Astrocytes
Blood capillaries
Tight junctions formed by endothelial cells
Basement membrane
Detailed Characteristics of Endothelial Cells
Origin: Derived from mesoderm.
Unique features related to the BBB include:
Absence of fenestrations.
Luminal/abluminal polarization.
Extensive tight junctions that limit the flux of hydrophilic molecules across the BBB.
Sparse pinocytic vesicular transport.
Rich mitochondria supporting a unique and active metabolism that changes the cellular environment.
Function is regulated by neighboring cells with intercellular communication.
Signaling is facilitated through a diverse array of proteins.
Tight Junctions (Zonula Occludens)
Endothelial cells in the brain exhibit:
A high density of tight junctions, markedly up to 100 times that found in somatic endothelial cells.
Highly selective diffusion barrier that prevents blood substances from entering the brain.
Blocks the paracellular aqueous diffusion pathways between adjacent endothelial cells.
Limits the paracellular flux of hydrophilic molecules and the passive diffusion of proteins and polar solutes to/from the CNS.
Composition:
Composed of a branching network of sealing strands that are independent from one another.
Efficient structure with each strand formed from transmembrane proteins embedded in plasma membranes, where extracellular domains interact directly.
Major proteins involved are Claudins and Occludins, which anchor to strands of Actin.
Junction adhesion molecules (e.g., JAM 1,3) have potential roles that are yet to be fully elucidated.
Interrelation of Cell Components in the BBB
Major components illustrated:
Tight junctions are crucial to the functionality of the BBB, providing required structural integrity.
The apical plasma membrane supports interaction with the actin cytoskeleton, including proteins such as cingulin, ZO-1, catenins, vinculin, claudin-5, and occludin.
Role of Astrocytes in BBB Regulation
Astrocytes are a subtype of glial cells and are the most abundant cells in the CNS.
Key functions include:
Providing structural support.
Metabolic regulation.
Signaling, growth, and homeostatic maintenance.
Control of blood flow and biochemical maintenance of the BBB.
Discusses the foot processes of astrocytes and their impact on the BBB structure and function:
A1 astrocyte phenotype: Pro-inflammatory effects (harmful).
A2 astrocyte phenotype: Involved in healing (anti-inflammatory).
Potential therapeutic implications of astrocyte phenotypic states.
Function and Importance of Pericytes
Pericytes are contracting cells located at intervals along capillaries:
Important for angiogenesis and maintain structural integrity, differentiation of microvessels, and formation of endothelial tight junctions.
Help sustain brain blood flow by relaxing.
A role in phagocytosis, but not deeply understood.
Linked to microvascular instability when malfunctioning.
Basement Membrane as Part of the BBB
Role: Connects cells and intervenes in cellular communication, providing a barrier to chemicals and cells (including inflammatory cells).
Offers physical space for various interactions and is composed of extracellular matrix (ECM) proteins.
Extracellular Matrix Proteins
Key proteins include:
Collagen type IV
Laminin
Fibronectin
Proteoglycans
Functions of ECM proteins:
Provide structural scaffolding and biochemical cues for cell adhesion, differentiation, and polarization.
Facilitate tight junction formation and enhance barrier integrity while reducing permeability.
Subject to degradation by metalloproteinases, which are crucial for tissue remodeling, wound healing, and angiogenesis.
Types of Neuroglia
In the Central Nervous System (CNS):
Ependymal cells
Oligodendrocytes
Astrocytes
Microglia
In the Peripheral Nervous System:
Satellite cells
Schwann cells
Microglia Characteristics
Types of microglia mentioned:
Microglia (ameboid, active, endocytosis)
Enteric glia (with subtypes depending on location)
Microglia play a critical role in regulating tight junction expression in the BBB.
Presence of BBB Across Various Structures
Not universally present; absent in areas such as:
Pineal gland
Neurohypophysis (Pituitary)
Subcommissural organ (CSF)
Subfornical organ (CSF)
Organum vasculosum of the lamina terminalis (CSF)
Area postrema (vomiting center)
Molecules That Can Cross the BBB
Characteristics include:
Lipophilic, positively charged molecules with low molecular weight (less than 400 to 600 Da) can cross.
Examples of diffusible substances:
Water
Sodium (Na)
Potassium (K)
Chloride (Cl)
Oxygen (O2)
Carbon dioxide (CO2)
Anesthetics
Barbiturates
Ethanol
Nicotine
Caffeine
Role of the BBB is to prevent alterations in concentrations of blood ions, amino acids, peptides, and other elements, including inflammatory cells.
Mechanisms of Transmission Across the BBB
Various mechanisms include:
Paracellular diffusion
Transcellular diffusion
Transporter protein-mediated transcytosis
Receptor-mediated transcytosis
Adsorptive-mediated transcytosis
Cell-mediated transcytosis
Efflux Transport at the BBB
Substances involved:
Oxygen (O2)
Carbon dioxide (CO2)
Sodium (Na)
Potassium (K)
Hydroxide ions (OH-)
Various peptidases
Carriers for drugs
Cell surface adsorptive proteins like GLUTS (for glucose)
Detailed Explanation of Paracellular Transport
Definition: Passive movement of water, ions, and small molecules between adjacent epithelial cells via tight junctions.
The paracellular barrier restricts this movement.
Facilitates the transmission of dissolved molecules through an area between two neighboring endothelial cells driven by a negative concentration gradient from the bloodstream to cerebral tissue.
Only small water-soluble molecules can cross this area.
Explanation of Transcellular Transport
Definition: Movement of solute substances across endothelial cells.
Lipid-soluble agents such as oxygen, carbon dioxide, anesthetics, and alcohol can pass through this method.
Lipid-soluble substances cross by dissolving in the lipids of endothelial cell plasma membranes.
Additional barrier systems exist to safeguard against the harmful lipid-soluble compounds which may permeate directly out of vessel walls, known as efflux pumps.
Key Efflux Transport Proteins at the BBB
P-glycoprotein (P-gp/ABCB1): Restricts the uptake of numerous lipid-soluble drugs.
Breast Cancer Resistance Protein (BCRP/ABCG2): Exports toxins and drugs along with P-glycoprotein.
Multidrug Resistance-associated Proteins (MRPs/ABCCs) and Solute Carrier (SLC) Transporters: Facilitate the efflux of various organic anions.
Molecules Capable of Passing Through the BBB
Examples of transport mechanisms:
Receptor-mediated transcytosis: Insulin, leptin, IgG, transferrin, TNF-alpha.
Adsorptive-mediated transcytosis: Albumin, histones.
Transporter-mediated pathway: Glucose, creatine, lactate, pyruvate, and large neutral amino acids.
Drug Delivery to the Brain Challenges
Most drugs cannot pass the BBB effectively.
Overcoming challenges through invasive techniques:
Intra-cerebral-ventricular and intrathecal infusions or injections.
Transient disruption of the BBB via:
Ultrasound
Noxious agents
Hyperosmotic solutions
Bradykinin and histamine (vasoactive drugs that increase capillary permeability).
Non-Invasive Techniques for Drug Delivery
Strategies to enhance drug delivery include:
Enhanced transcellular transport.
Intranasal delivery utilizing neural pathways connecting the nasal mucosa to the brain.
Use of transport/carrier systems.
Nanoparticle-based technologies allowing controlled drug release while protecting drugs from metabolism.
Transforming water-soluble molecules into lipid-soluble by chemical modifications (e.g. replacing OH- with COO-).
Inhibition of efflux transporters that restrict drug delivery.
Examples of Therapeutic Agents Accessible via BBB
Types of drugs that can cross include:
Anticonvulsants
Sedatives
Anesthetics
Nonsteroidal anti-inflammatory drugs (NSAIDs)
Some antibiotics (e.g., chloramphenicol, fluoroquinolones, doxycycline, sulfas/trimethoprim).
Influences to consider: molecular size, polarity, lipophilicity, plasma protein binding, and affinity to active transport systems.
Factors Altering the BBB Environment
Elements altering this condition include:
Astrocytes secreting substances like glutamate, aspartate, taurine, ATP, nitrogen monoxide (NO), TNF-alpha, and IL-beta.
Other cells releasing: Bradykinin, histamine, thrombin, and free radicals.
Pathological conditions such as inflammation, hypoxia, degeneration, edema, neoplasia, hemorrhage, and necrosis affect the BBB.
External factors like microwaves are also noted.
Encephalitis
Definition: Inflammation of the brain.
Associated Infectious agents:
Viruses
Bacteria
Fungi
Parasites
Infectious Encephalitis in Various Species
Observations of infectious agents affecting several animal species including horses, dogs, cats, cows, and birds.
Dynamics of Infectious Encephalitis
Infections of the brain are rare but can be severe.
Reliance on the innate immune system for the brain and CNS immune response as the BBB inhibits antibody and B cell passage.
The limited effect of adaptive immune response in CNS follows inflammation increasing BBB permeability.
Some bacteria may traverse the barrier utilizing endolysins to disrupt it, such as Treponema spp. and Borrelia spp.
West Nile Virus Impact on the BBB
Clinical signs in horses include:
Weakness
Ataxia
Paresis
Head tremors
Vestibular syndrome
Head tilt and pressing
Seizures
Anorexia, fever
Potential abortion
Lip droop/paralysis
The virus increases BBB permeability and utilizes leukocyte transport for entry.
Detection of WNV ds RNA by TLR3 triggers an inflammatory cytokine response (TNF-alpha and IL-6).
Mechanisms for Viral Entry into the CNS
Viruses can infect endothelial cells, compromising BBB integrity (West Nile virus is an example).
Binding proteins and specific receptors expressed in neurons confer neurotropism.
Utilize 'trojan horses' via infected white blood cells, access through cerebral spinal fluid (CSF) via ependymal cells, or axonal transport mechanisms (e.g., rabies and herpes viruses).
Biomarkers of BBB Disruption
Definition: A measurable substance in an organism indicating disease, infection, or environmental exposure with potential for diagnosis.
Essential features of a biomarker include:
High sensitivity and specificity
Reliability
Quick response
Biomarkers include:
Occludin (tight junction component)
Fibronectin (basal membrane component)
Metalloproteinases (extracellular proteases)
CSF/Serum albumin ratio
Biomarker indicators from brain microvascular endothelial cells.
Summary of Biomarkers of BBB Disruption
Reiterated features of molecular biomarkers include their sensitivity, reliability, and diagnostic applicability in the context of BBB integrity assessment.
Questions / Discussion Section
A segment reserved for participant queries.