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Review
. 2022 Jul 13;27(14):4490.
doi: 10.3390/molecules27144490.

Evaluation of Biological Activity of Natural Compounds: Current Trends and Methods

Carlos Barba-Ostria  1 , Saskya E Carrera-Pacheco  2 , Rebeca Gonzalez-Pastor  2 , Jorge Heredia-Moya  2 , Arianna Mayorga-Ramos  2 , Cristina Rodríguez-Pólit  2 , Johana Zúñiga-Miranda  2 , Benjamin Arias-Almeida  2 , Linda P Guamán  2
Affiliations
Review

Evaluation of Biological Activity of Natural Compounds: Current Trends and Methods

Carlos Barba-Ostria et al. Molecules. .

Abstract

Natural compounds have diverse structures and are present in different forms of life. Metabolites such as tannins, anthocyanins, and alkaloids, among others, serve as a defense mechanism in live organisms and are undoubtedly compounds of interest for the food, cosmetic, and pharmaceutical industries. Plants, bacteria, and insects represent sources of biomolecules with diverse activities, which are in many cases poorly studied. To use these molecules for different applications, it is essential to know their structure, concentrations, and biological activity potential. In vitro techniques that evaluate the biological activity of the molecules of interest have been developed since the 1950s. Currently, different methodologies have emerged to overcome some of the limitations of these traditional techniques, mainly via reductions in time and costs. These emerging technologies continue to appear due to the urgent need to expand the analysis capacity of a growing number of reported biomolecules. This review presents an updated summary of the conventional and relevant methods to evaluate the natural compounds' biological activity in vitro.

Keywords: antimicrobial; antioxidant; bioactive compounds; natural product.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
High-tech in vitro models to assess cytotoxicity in cultured mammalian cells. (A) Dual chamber, test compound, and metabolites diffuse through the microporous barrier toward target cells. (B) Three-dimensional cellular models based on multicellular spheroids or organoids consisting of target cells or the co-cultivation of several types of cells on extracellular matrix (ECM). (C) Organotypic cultures, whereby cells, organ slices, or whole organs are cultured on a tissue culture insert that is either submerged in medium or maintained at an air–liquid interface to ensure sufficient oxygen supply. (D) Microfluidic system based on a mixture of cells and matrix collected in the central channel and medium flowing from the lateral channels that keeps particles in homogenous suspension.
Figure 2
Figure 2
Strategies employed to assess anti-inflammatory activity in vitro. Nitric oxide (NO), lipopolysaccharide (LPS), interferon-gamma (IFN-γ), nuclear factor kappa B (NF-κB).
Figure 3
Figure 3
Sites in the rat brain tissue, where both opiate antagonists and agonists compete for the same receptors, opiate potencies, and antagonists in displacing 3H-naloxone binding parallel to their pharmacological potencies.
Figure 4
Figure 4
The activation of coagulation factors in vitro for clot formation by adding the test compound as a possible therapeutic agent.
Figure 5
Figure 5
Strategies employed to assess analgesic activity in vitro. TT: thrombin time; aPTT: activated partial thromboplastin; PT: prothrombin time; PRP: platelet-rich plasma.
Figure 6
Figure 6
The inhibition of angiotensin-converting enzyme. Calcium (Ca2+), angiotensin-converting enzyme (ACE), angiotensin-converting enzyme inhibitors (ACEi), atypical protein kinase C (aPKC), myosin-light-chain kinase (MLCK), nitric oxide (NO).
Figure 7
Figure 7
Summary of the most relevant antimicrobial activity methods.
See this image and copyright information in PMC

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