#312 - A masterclass in lactate: Its critical role as metabolic fuel, implications for diseases, and therapeutic potential from cancer to brain health and beyond | George A. Brooks, Ph.D.

Aug 5, 2024 Episode Page ↗
Overview

George Brooks, UC Berkeley Professor, discusses his groundbreaking "lactate shuttle" theory, clarifying lactate's role as a crucial fuel source. He explores its significance in metabolism, athletic performance, type 2 diabetes, cancer, and brain injuries.

At a Glance
15 Insights
2h 6m Duration
13 Topics
5 Concepts

Deep Dive Analysis

Introduction to Lactate Misconceptions and George Brooks' Work

Historical Understanding of Lactic Acid and Meyerhoff's Experiment

Fundamentals of Glucose Metabolism and ATP Production

Lactate as a Preferred Mitochondrial Fuel and Substrate Competition

Lactate's Role in Traumatic Brain Injury (TBI) Treatment

Lactate's Influence on Appetite Regulation

Metabolic Differences: Athletes vs. Insulin-Resistant Individuals

MCTs and Lactate Shuttling Between Muscle Fiber Types

Lactate's Role in Cancer and Exercise Benefits

Lactate in Sepsis and the Significance of D-Lactate

Enteric Glycolysis and Lactate Production from Oral Glucose

Lactate's Influence on Gene Expression (Lactylation)

Future Research Directions and Unanswered Questions

Lactate Shuttle Theory

Proposed by George Brooks, this theory posits that lactate is a crucial fuel source for muscles and other cells, actively produced and utilized, rather than merely an unfortunate byproduct of anaerobic metabolism. It highlights lactate's role in energy distribution and utilization throughout the body.

Monocarboxylate Transporters (MCTs)

These are proteins responsible for transporting monocarboxylates, including lactate and ketones, across cell membranes. Crucially, MCTs are found not only on the cell surface for export but also on mitochondrial membranes, facilitating lactate's entry into mitochondria for oxidation.

Cell-Cell Lactate Shuttle

This describes the process where fast glycolytic (Type 2) muscle fibers produce lactate and shuttle it to adjacent slow oxidative (Type 1) muscle fibers for consumption and oxidation. This allows efficient local utilization of lactate within muscle tissue, reducing its appearance in venous blood.

Warburg Effect

This phenomenon describes how cancer cells preferentially metabolize glucose to lactate, even in the presence of ample oxygen. While initially thought to indicate defective mitochondria, it's now understood that this metabolic pathway may be optimized for providing cellular building blocks for rapid replication, rather than just ATP efficiency.

Lactylation

A newly recognized epigenetic modification where lactate can directly and covalently bind to histones, similar to acetylation or methylation. This binding can influence gene expression, suggesting lactate acts as a potent signaling molecule beyond its metabolic role.

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What is the fundamental difference between lactate and lactic acid?

The body primarily produces lactate, which is an anion, not lactic acid. Lactic acid is formed when lactate is associated with a hydrogen ion, but the final step of glycolysis, which produces lactate, is actually an alkalizing step.

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Why was lactate historically misunderstood as a waste product or cause of fatigue?

Early 20th-century experiments, like Meyerhoff's with frog muscles in anaerobic conditions, observed lactate accumulation alongside acidosis and muscle fatigue. This led to the incorrect association of lactate with oxygen lack, acidosis, and fatigue.

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How does glucose enter cells and what are its initial metabolic fates?

Glucose enters cells via specific glucose transporters (e.g., GLUT4 in muscle and fat, activated by insulin or contraction). Once inside, it can either be stored as glycogen or enter the glycolytic pathway to be degraded for energy, primarily producing lactate.

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Does lactate serve as a direct fuel source for mitochondria?

Yes, lactate is transported into mitochondria via monocarboxylate transporters (MCTs) and is a preferred fuel for oxidative phosphorylation, where it is converted to pyruvate and then oxidized to generate ATP.

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Why does lactate appear to inhibit fatty acid metabolism?

Lactate metabolism generates acetyl-CoA, which inhibits the enzymes (CPT1 and CPT2) responsible for transporting fatty acids into mitochondria for oxidation. This prioritizes fast-acting carbohydrate fuel during high-demand, sympathetic states.

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What role does lactate play in traumatic brain injury (TBI)?

In an injured brain, glucose uptake can be impaired, leading to a metabolic crisis. Lactate, which can be transported into brain cells via MCTs, can serve as a preferred and vital fuel for neurons, potentially aiding in recovery from TBI.

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How does exercise training enhance lactate utilization and clearance?

Exercise training increases mitochondrial mass and the abundance of MCTs in muscle cells. This enhances the capacity to produce lactate, shuttle it between muscle fibers, and efficiently oxidize it within mitochondria or transport it to other tissues like the liver for gluconeogenesis.

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How does lactate influence appetite?

Elevated lactate levels, such as those achieved during moderate to intense exercise, can cross the blood-brain barrier and act on the hypothalamus to inhibit ghrelin secretion, thereby suppressing appetite and promoting satiety.

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What is the significance of lactate in sepsis, and why might standard measurements be incomplete?

Elevated lactate is a marker in sepsis, but common assays primarily measure L-lactate (the form the body typically produces). Microbes in the gut can produce D-lactate, which is neurotoxic and pro-inflammatory, and its presence might be a more significant, yet often unmeasured, contributor to sepsis pathophysiology.

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What happens metabolically immediately after consuming glucose?

Following an oral glucose tolerance test, lactate levels in arterial blood spike rapidly (within 5-15 minutes), often before glucose levels peak. This initial lactate production is primarily due to enteric glycolysis in enterocytes, which convert glucose to lactate for energy distribution.

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Can lactate directly influence gene expression?

Yes, lactate can act as a signaling molecule by directly binding to histones, a process known as lactylation. This epigenetic modification can affect gene expression, potentially playing a role in cellular adaptations like mitochondrial biogenesis.

1. Double Mitochondrial Mass via Training

Engage in consistent training over several weeks to months, as this can double mitochondrial mass in muscle, enhancing the body’s energy delivery system and improving metabolic capacity.

2. Exercise to Suppress Appetite

Engage in exercise intense enough to raise lactate levels to around 3-4 millimolar, as this can cross the blood-brain barrier, inhibit ghrelin secretion, and suppress appetite for several hours post-exercise.

3. Increase MCT Density with Training

Train consistently to increase the abundance of monocarboxylate transporters (MCTs) in muscle cells, which facilitates both the export of lactate and its uptake into mitochondria for oxidation.

4. Enhance Lactate Clearance for Cancer

Increase your body’s lactate clearance capacity through regular exercise, as effective removal of lactate may lessen the chance for carcinogenesis if lactate is indeed carcinogenic.

5. Generate Endogenous Lactate for Biogenesis

To stimulate mitochondrial biogenesis, focus on generating high levels of endogenous lactate through exercise, as this appears to be a more effective signal than simply infusing exogenous lactate.

6. Exercise for Brain Health, Neurogenesis

Engage in physical exercise to promote brain health, as it can stimulate neurogenesis in the dentate gyrus and improve brain blood flow and substrate delivery, contributing to the development of new brain cells.

7. Exercise Boosts Cognition

Engage in exercise that raises lactate levels, as this can temporarily improve scores on cognitive tests and fuel the brain, suggesting a direct link between physical activity and enhanced executive function.

8. Administer Lactate for TBI

For brain-injured individuals, consider intravenous lactate infusion, as early clinical trials suggest it may serve as a preferred fuel source for injured neurons and could lead to better outcomes.

9. Use ‘Lactate,’ Not ‘Lactic Acid’

Refer to the molecule as ’lactate’ rather than ’lactic acid,’ as the body produces lactate, and this distinction corrects a century-old historical mistake in understanding its role.

10. Recognize Lactate as Fuel

Understand that lactate is an integral participant in powering muscle and all cells, serving as a crucial fuel source rather than merely an unfortunate byproduct or waste product of exercise.

11. Metformin’s Lactate: A Good Thing

If taking metformin, understand that the associated rise in lactate levels may be a beneficial outcome, as the drug could be encouraging enterocytes to produce lactate as a valuable carbohydrate energy form.

12. Distinguish Lactate from pH in Sepsis

In septic patients, differentiate between elevated lactate and low pH; while a low pH requires intervention, a high lactate level in the absence of a significant pH change may not warrant aggressive treatment for acidosis.

13. Recognize Enteric Glycolysis

Understand that enteric glycolysis, occurring in the gut, is an initial and rapid process of carbohydrate energy distribution, producing lactate that appears in arterial blood even before glucose levels significantly rise after a meal.

14. Liver Sequestering Glucose Load

Understand that the liver plays a key role in glucose disposal, sequestering approximately 80% of an oral glucose load and gradually releasing it over time, rather than immediate muscle uptake.

15. Lactate Signals Gene Expression

Recognize that lactate is a potent signaling molecule that can directly bind to genes (lactylation) and affect gene expression, potentially influencing mitochondrial biogenesis and other physiological adaptations.

The body does not make lactic acid. It makes lactate.

George Brooks

We've been teaching glycolysis wrong for a hundred years.

George Brooks

Lactate basically shuts the door, blocks fatty acid metabolism.

George Brooks

Lactate is a preferred fuel over glucose in the brain and muscle, wherever.

George Brooks

Lactate is there to moderate. It's a strain response. It's helping to protect you.

George Brooks

If you just take muscles, put them in a muscle cells in a dish, you had lactate, you activate 500 genes.

George Brooks
Up to 100% (doubling)
Mitochondrial mass increase with training Observed over several weeks in rats and in athletes compared to average individuals.
10-15%
VO2 max increase with training Potential increase in individuals through training.
4 millimolar
Lactate concentration for TBI infusion (UCLA study) Target concentration for intravenous lactate infusion in a stage two clinical trial for traumatic brain injury patients.
Up to 8 millimolar
Lactate concentration for TBI infusion (Switzerland) Concentration of hypertonic lactate preferentially given to TBI patients by a group in Switzerland.
Approximately 20 minutes
Half-life of Carbon-11 Radioisotope used in PET scans for lactate, requiring rapid synthesis and use.
75-80%
Lactate oxidation rate Percentage of lactate that is oxidized in the body, as observed in tracer studies.
500 genes
Genes activated by lactate in muscle cells Observed in in vitro experiments where muscle cells in a dish were exposed to lactate.
$2.5 million
Cost for a basic research grant (RO1) Estimated funding needed to begin definitive experiments on lactate flux and disposal.
75 grams
Standard oral glucose tolerance test (OGTT) glucose load Amount of glucose given in a typical OGTT.
5 minutes (peaking at 15 minutes)
Time for lactate spike after OGTT Observed rapid increase in arterial lactate after oral glucose intake, preceding glucose peak.
30 minutes
Time for glucose spike after OGTT Typical time for blood glucose levels to peak after an oral glucose tolerance test.
Approximately 80%
Liver sequestration of oral glucose load Percentage of an oral glucose load that the liver initially sequesters before doling it out over time.