nutrients
Article
L-Carnitine Tartrate Downregulates the ACE2 Receptor and
Limits SARS-CoV-2 Infection
Aouatef Bellamine
1,
*, Tram N. Q. Pham
2
, Jaspreet Jain
2
, Jacob Wilson
3
, Kazim Sahin
4
, Frederic Dallaire
2
,
Nabil G. Seidah
2
, Shane Durkee
1
, Katarina Radoševi´ c
5
and Éric A. Cohen
2,6,
*
Citation: Bellamine, A.; Pham,
T.N.Q.; Jain, J.; Wilson, J.; Sahin, K.;
Dallaire, F.; Seidah, N.G.; Durkee, S.;
Radoševi´ c, K.; Cohen, É.A.
L-Carnitine Tartrate Downregulates
the ACE2 Receptor and Limits
SARS-CoV-2 Infection. Nutrients 2021,
13, 1297. https://doi.org/10.3390/
nu13041297
Academic Editor: Carlo Agostoni and
Gregorio Paolo Milani
Received: 15 March 2021
Accepted: 12 April 2021
Published: 14 April 2021
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4.0/).
1
Lonza Consumer Health, Morristown, NJ 07960, USA; shane.durkee@lonza.com
2
Institut de Recherche Clinique de Montreal, Montreal, QC H2W1R7, Canada;
Tram.Pham@ircm.qc.ca (T.N.Q.P.); Jaspreet.Jain@ircm.qc.ca (J.J.); frederic.dallaire@ircm.qc.ca (F.D.);
Nabil.Seidah@ircm.qc.ca (N.G.S.)
3
Applied Science and Performance Institute, Tampa, FL 33607, USA; jwilson@theaspi.com
4
Department of Animal Nutrition, Faculty of Veterinary Medicine, Firat University, Elazig 23119, Turkey;
nsahinkm@yahoo.com
5
Biologics R&D, Lonza Pharma & Biotech, 4057 Basel, Switzerland; katarina.radosevic@lonza.com
6
Departmentof Microbiology, Infectiology and Immunology, Université de Montréal,
Montreal, QC H3T 1J4, Canada
* Correspondence: aouatef.bellamine@lonza.com (A.B.); eric.Cohen@ircm.qc.ca (É.A.C.)
Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been responsible for
one of the worst pandemics in modern history. Several prevention and treatment strategies have
been designed and evaluated in recent months either through the repurposing of existing treatments
or the development of new drugs and vaccines. In this study, we show that L-carnitine tartrate
supplementation in humans and rodents led to significant decreases of key host dependency factors,
notably angiotensin-converting enzyme 2 (ACE2), transmembrane protease serine 2 (TMPRSS2),
and Furin, which are responsible for viral attachment, viral spike S-protein cleavage, and priming
for viral fusion and entry. Interestingly, pre-treatment of Calu-3, human lung epithelial cells, with
L-carnitine tartrate led to a significant and dose-dependent inhibition of the infection by SARS-CoV-2.
Infection inhibition coincided with a significant decrease in ACE2 mRNA expression levels. These
data suggest that L-carnitine tartrate should be tested with appropriate trials in humans for the
possibility to limit SARS-CoV-2 infection.
Keywords: L-carnitine; SARS-CoV-2; COVID-19; exercise; inflammation; ACE-2; Furin; TMPRSS2
1. Introduction
Severe acute respiratory syndrome coronavirus (SARS-CoV-1 and SARS-CoV-2) is
responsible for the SARS epidemic from 2002 to 2004 and more recently for the coronavirus
disease 2019 (COVID-19) pandemic outbreak initially detected in December 2019 in Wuhan
China [1]. The rapid spread of the disease has affected more than 120 million people and
caused over 2.6 million deaths in 220 countries as per mid-March of 2021 [2]. SARS-CoV-2
is an airborne virus that affects mainly the lungs and the upper respiratory system [2],
leading ultimately to lung injury, respiratory distress, and death in severe cases.
According to recent data released, there are 237 known vaccine candidates globally,
of which 64 are in clinical evaluation and nine are in their phase III clinical stage [3,4]. A
few vaccines starting with Pfizer-BioNTech and Moderna’s mRNA-based vaccines and
more recently Johnson & Johnson’s single-shot adenovirus vector-based vaccine have
been approved for adult use [5]. As a result of the urgency of the situation, accelerated
clinical development paths have been followed [3,6] and resulted in decreased vaccine
acceptance [6]. In addition to the vaccines, there are a number of other preventive and
therapeutic strategies being developed, including antibodies [7,8] and antiviral drugs [9,10].
Nutrients 2021, 13, 1297. https://doi.org/10.3390/nu13041297 https://www.mdpi.com/journal/nutrients