Pilot study for the evaluation of safety profile of a potential inhibitor of SARS-CoV-2 endocytosis.
Adult
Aged
Aged, 80 and over
Antiviral Agents
/ adverse effects
Betacoronavirus
COVID-19
Caco-2 Cells
Cell Culture Techniques
Coronavirus Infections
/ drug therapy
Endocytosis
/ drug effects
Female
Humans
Male
Middle Aged
Oral Sprays
Pandemics
Phenylethyl Alcohol
/ adverse effects
Pilot Projects
Pneumonia, Viral
/ drug therapy
SARS-CoV-2
Young Adult
alpha-Cyclodextrins
/ adverse effects
COVID-19 Drug Treatment
Journal
Acta bio-medica : Atenei Parmensis
ISSN: 2531-6745
Titre abrégé: Acta Biomed
Pays: Italy
ID NLM: 101295064
Informations de publication
Date de publication:
09 11 2020
09 11 2020
Historique:
received:
03
09
2020
accepted:
17
09
2020
entrez:
10
11
2020
pubmed:
11
11
2020
medline:
20
11
2020
Statut:
epublish
Résumé
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for the current pandemics of coronavirus disease. This virus is able to attack the cells of the airway epithelium by binding to the transmembrane angiotensin I converting enzyme 2 (ACE2). We developed an oral spray that could inhibit the SARS-CoV-2 endocytosis. The spray contains hydroxytyrosol for its anti-viral, anti-inflammatory and anti-oxidant properties, and α-cyclodextrin for its ability to deplete sphingolipids, that form the lipid rafts where ACE2 localizes. The aim of the present pilot multi-centric open non-controlled observational study was to evaluate the safety profile of the "Endovir Stop" spray. An MTT test was performed to evaluate cytotoxicity of the spray in two human cell lines. An oxygen radical absorbance capacity assay was performed to evaluate the antioxidant capacity of the spray. The spray was also tested on 87 healthy subjects on a voluntary basis. The MTT test revealed that the spray is not cytotoxic. The ORAC assay showed a good antioxidant capacity for the spray. Endovir Stop tested on healthy volunteers showed the total absence of side effects and drug interactions during the treatment. We demonstrated that Endovir Stop spray is safe. The next step would be the administration of the efficacy of the spray by testing it to a wider range of people and see whether there is a reduced infection rate of SARS-CoV-2 in the treated subjects than in the non-treated individuals.
Sections du résumé
BACKGROUND AND AIM OF THE WORK
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for the current pandemics of coronavirus disease. This virus is able to attack the cells of the airway epithelium by binding to the transmembrane angiotensin I converting enzyme 2 (ACE2). We developed an oral spray that could inhibit the SARS-CoV-2 endocytosis. The spray contains hydroxytyrosol for its anti-viral, anti-inflammatory and anti-oxidant properties, and α-cyclodextrin for its ability to deplete sphingolipids, that form the lipid rafts where ACE2 localizes. The aim of the present pilot multi-centric open non-controlled observational study was to evaluate the safety profile of the "Endovir Stop" spray.
METHODS
An MTT test was performed to evaluate cytotoxicity of the spray in two human cell lines. An oxygen radical absorbance capacity assay was performed to evaluate the antioxidant capacity of the spray. The spray was also tested on 87 healthy subjects on a voluntary basis.
RESULTS
The MTT test revealed that the spray is not cytotoxic. The ORAC assay showed a good antioxidant capacity for the spray. Endovir Stop tested on healthy volunteers showed the total absence of side effects and drug interactions during the treatment.
CONCLUSIONS
We demonstrated that Endovir Stop spray is safe. The next step would be the administration of the efficacy of the spray by testing it to a wider range of people and see whether there is a reduced infection rate of SARS-CoV-2 in the treated subjects than in the non-treated individuals.
Identifiants
pubmed: 33170175
doi: 10.23750/abm.v91i13-S.10583
pmc: PMC8023122
doi:
Substances chimiques
Antiviral Agents
0
Oral Sprays
0
alpha-Cyclodextrins
0
3,4-dihydroxyphenylethanol
10597-60-1
Phenylethyl Alcohol
ML9LGA7468
alpha-cyclodextrin
Z1LH97KTRM
Types de publication
Journal Article
Multicenter Study
Observational Study
Langues
eng
Sous-ensembles de citation
IM
Pagination
e2020009Références
J Biol Chem. 1996 Sep 20;271(38):23211-21
pubmed: 8798517
Front Nutr. 2014 Oct 27;1:18
pubmed: 25988120
Nutrition. 2014 Jul-Aug;30(7-8):936-8
pubmed: 24985014
Science. 1980 Jul 25;209(4455):497-9
pubmed: 6248960
Int J Mol Sci. 2019 Jul 25;20(15):
pubmed: 31349547
AIDS. 2016 Nov 28;30(18):2767-2776
pubmed: 27677167
J Biotechnol. 2020 Feb 10;309:29-33
pubmed: 31884046
J Med Virol. 2021 Jan;93(1):250-256
pubmed: 32592501
Colloids Surf B Biointerfaces. 2019 Jun 1;178:488-499
pubmed: 30925372
Biomedicines. 2018 Jan 26;6(1):
pubmed: 29373553
Molecules. 2020 Jun 24;25(12):
pubmed: 32599866
Nat Rev Immunol. 2020 Jun;20(6):363-374
pubmed: 32346093
Proc Natl Acad Sci U S A. 2016 Dec 6;113(49):14025-14030
pubmed: 27872310
Biomed Res Int. 2016;2016:7529521
pubmed: 27965980
Molecules. 2020 Jan 13;25(2):
pubmed: 31941100
Nature. 1979 Dec 6;282(5739):615-6
pubmed: 233137
Biochem Biophys Res Commun. 2007 Mar 23;354(4):872-8
pubmed: 17275783
Cell. 2020 Apr 16;181(2):271-280.e8
pubmed: 32142651
Antiviral Res. 2009 Jul;83(1):35-44
pubmed: 19501255