ASSESSMENT OF BIOLOGY ACTIVITY OF THE PEELING SUBSTANCES BY THE
PHYSICOCHEMICAL APPROACHES ON THE SPIROSTOMUM AMBIGUUM CELL MODEL
Original Article
USPENSKAYA E. V.,
*
Peoples Friendship University of Russia (RUDN University), Department of Pharmaceutical and Toxicological Chemistry, 6, Miklukho-
Maklaya St, Moscow, 117198, Russian Federation
*Email:
PLETENEVA T. V., PHAM MY HANH, KAZIMOVA I. V.
uspenskaya75@mail.ru
Received: 28 Apr 2021, Revised and Accepted: 01 Jun 2021
ABSTRACT
Objective: To evaluate the biological activity of chemical peeling substances based on enzymatic and Arrhenius kinetics using Spirostomum
ambiguum as an alternative approach to animal experiments.
Methods: The Spirotox method was used to analyze the mechanism of «xenobiotic-cell» interaction, similar to the Michaelis-Menten enzymatic
kinetics. The Hill-Langmuir equation was used to determine the degree of cooperativity in the binding of xenobiotics to cellular receptors. Using the
Arrhenius kinetics, the observed activation energy obsEa of cell death in the model solutions of glycolic and carbolic acids was determed, which will
allow predicting the toxicity parameters of any peeling substances.
Results: The relationship Spirostomum ambiguum lifetime t L- lgC concentration of peeling compound solution made it possible to characterize the
moment of cellular transition from the intermediate state C•L n to the dead state DC, characterized by irreversible structural and functional changes
in the cell/death. The values were 5.3 mmol•l
-1
for glycolic acid solutions and 2.8 mmol•l
-1
for carbolic acid solutions. Equilibrium constants Keq of
complexation, the rate of infusoria death f m, and the degree of ligand cooperativity n were calculated. The activation energy °
bs
E a of cell death was
determined in Arrhenius coordinates, which were 210±0.39 kJ·mol
-1
and 108±0.09 kJ·mol
-1
for glycolic and carbolic acids respectively. The
correlation between the values of activation energy and DL 50
Conclusion: The obtained kinetic parameters made it possible, without animals and humans testing, to characterize the mechanisms of interaction
of peeling substances with the living cell.
of mammals (rats) was discovered.
Keywords: Peeling, Glycolic acid, Phenol, Spirotox method, Biological activity, Animal-free test
© 2021 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
DOI: https://dx.doi.org/10.22159/ijpps.2021v13i7.41927. Journal homepage: https://innovareacademics.in/journals/index.php/ijpps.
INTRODUCTION
Chemical peeling (сhemexfoliation) stimulates the appearance of
controlled keratocoagulation and denaturing proteins in the
epidermis and dermis, the release of pro-inflammatory cytokines
and chemokines, and the production of new skin collagen and elastin
[1-5]. The clinical effectiveness of chemical peeling, as well as the risk
of various complications, depends on many factors: the properties of
chemicals, concentration, regimen, and the number of uses, skin type,
dermatological condition, and cumulative dose [6, 7]. Despite available
reviews about the traumatic nature of this procedure, chemical peeling
ranks third in the frequency of non-invasive cosmetic procedures in
the USA [8]. Since the use of cosmetic products is not associated with
an urgent need for the life and health of consumers, there is the
number of advocates of alternative in vitro approaches to animal
experiments, for example, when checking the safety of cosmetics [9-
14]. Cosmetic animal testing is banned in a few countries [15]. For the
testing of cosmetics, programs are being developed to enable the
cosmetics industry to conduct safety assessments [16, 17]. To date,
testing methods without the use of animals have been selected,
including cell lines [18].
Alternative models use various cellular cultures, specialized moving
cells, bacteria, single-celled organisms, primitive crustaceans and
other hydrobionts. Methods based on the reactions of the simplest
animals are of paramount importance in today's environment, as
they allow determining the possible range of properties in a short
period the substance under study and making recommendations on
whether to investigate it further. For example, there are approaches
to describing the kinetics of the development of cellular population
under the influence of inhibitors and promoters [19]. It is also
important that biological research methods using protozoa
significantly reduce the time required to study the properties of
substances and are characterized by a relatively low cost. Replacing
warm-blooded animals with unicellular ones reduces the time of
toxicological and pharmaceutical studies from one year to a month,
and the cost of their implementation decreases in ten times [20]. The
goal is to directly replace animal testing with non-animal methods.
Advances in cell and molecular biology and informatics need to be
leveraged to develop new specific preclinical testing strategies that
are applicable to specific human situations [21].
This work aims to evaluate the biological activity of chemical peeling
substances using enzymatic and Arrhenius kinetics for a single-cell
model Spirostomum ambiguum as an alternative approach to animal
experiments.
MATERIALS AND METHODS
Cell model
The test culture Spirostomum ambiguum (Sp. ambiguum) has been
cultured in the laboratory to carry out studies of individual and
combined biological activity of medicines.
The protozoan ciliate Sp. ambiguum is characterized by tape-shaped,
dorsal body shape (1-3 mm long), has a macronucleus clear-shaped
and mouth apparatus up to the back third of the body (fig. 1).
Compared to other objects of biological testing, Sp. ambiguum have
several advantages, since they are eukaryotic organisms. The
statistically reliable sensitivity to toxicants makes it possible to
compare the response of protozoa with that of humans [23, 24].
Under favorable conditions in a low-mineralized environment, cells
do not die for a period exceeding their cell cycle (about 20 h).
When incubated into a toxicant solution, cells die over time, which is
a function of both concentration and temperature. Kinetic scheme of
ligand-induced death of Sp. ambiguum includes the reversible
reaction with the formation of an intermediate product (C • L n ) and
the state of transition to cell death (DC) (fig. 2).
International Journal of Pharmacy and Pharmaceutical Sciences
Print ISSN: 2656-0097 | Online ISSN: 0975-1491 Vol 13, Issue 7, 2021