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Antimicrobial activity of oleanolic and ursolic acids: an update.

Jesus JA, Lago JH, Laurenti MD, Yamamoto ES, Passero LF - Evid Based Complement Alternat Med (2015)

Bottom Line: Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids.These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now.Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, via in vivo studies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Patologia de Moléstias Infecciosas, Departamento de Patologia, Faculdade de Medicina da Universidade de São Paulo, Avenue Dr. Arnaldo 455, 06780-210 Cerqueira César, SP, Brazil ; Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Professor Artur Riedel 275, 09972-270 Diadema, SP, Brazil.

ABSTRACT
Triterpenoids are the most representative group of phytochemicals, as they comprise more than 20,000 recognized molecules. These compounds are biosynthesized in plants via squalene cyclization, a C30 hydrocarbon that is considered to be the precursor of all steroids. Due to their low hydrophilicity, triterpenes were considered to be inactive for a long period of time; however, evidence regarding their wide range of pharmacological activities is emerging, and elegant studies have highlighted these activities. Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids. These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now. Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, via in vivo studies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

No MeSH data available.


Related in: MedlinePlus

Ultrastructural alterations induced by 10.96 μg of UA on promastigote forms of L. (L.) amazonensis. (a) Control parasites showed a normal morphology of the cell membranes, nucleus, and kinetoplast (20.000x). (b) Parasites treated with UA presented with evident external and internal alterations, such as mitochondrial swelling (arrowhead) and a pyknotic nucleus (short arrow) (10.000x); (c) Blebs (arrows) were detected in the nucleus and kinetoplast (40.000x); and (d) membranes were detected inside vacuoles, as indicated by the arrow (20.000x).
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fig2: Ultrastructural alterations induced by 10.96 μg of UA on promastigote forms of L. (L.) amazonensis. (a) Control parasites showed a normal morphology of the cell membranes, nucleus, and kinetoplast (20.000x). (b) Parasites treated with UA presented with evident external and internal alterations, such as mitochondrial swelling (arrowhead) and a pyknotic nucleus (short arrow) (10.000x); (c) Blebs (arrows) were detected in the nucleus and kinetoplast (40.000x); and (d) membranes were detected inside vacuoles, as indicated by the arrow (20.000x).

Mentions: In addition, our group demonstrated, through ultrastructural studies, that L. (L.) amazonensis promastigote forms treated with 10.96 μg of UA presented with irreversible morphological changes after 18 hours of incubation. Control parasites presented with normal membrane morphology, cytoplasm, nucleus, mitochondrion, and flagellum (Figure 2(a)). Otherwise, treated parasites presented with rounded-shape morphology, and the intracellular environment presented with vacuoles, suggesting organelle degradation (Figure 2(b)) and swelling of the mitochondrion, and a pyknotic nucleus was detected (Figure 2(b)); blebs were also visualized in the nucleus and in the kinetoplast (Figure 2(c)). In addition, intracellular vacuoles presented with fragments of membranes (Figure 2(d)), suggesting degradation of the organelles. Taken together, these results suggest that, in promastigote forms of L. (L.) amazonensis, UA induces a mechanism of death associated to apoptosis or even autophagy. This is the first study that depicted the possible mechanism of action of UA on L. (L.) amazonensis promastigote forms.


Antimicrobial activity of oleanolic and ursolic acids: an update.

Jesus JA, Lago JH, Laurenti MD, Yamamoto ES, Passero LF - Evid Based Complement Alternat Med (2015)

Ultrastructural alterations induced by 10.96 μg of UA on promastigote forms of L. (L.) amazonensis. (a) Control parasites showed a normal morphology of the cell membranes, nucleus, and kinetoplast (20.000x). (b) Parasites treated with UA presented with evident external and internal alterations, such as mitochondrial swelling (arrowhead) and a pyknotic nucleus (short arrow) (10.000x); (c) Blebs (arrows) were detected in the nucleus and kinetoplast (40.000x); and (d) membranes were detected inside vacuoles, as indicated by the arrow (20.000x).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4352472&req=5

fig2: Ultrastructural alterations induced by 10.96 μg of UA on promastigote forms of L. (L.) amazonensis. (a) Control parasites showed a normal morphology of the cell membranes, nucleus, and kinetoplast (20.000x). (b) Parasites treated with UA presented with evident external and internal alterations, such as mitochondrial swelling (arrowhead) and a pyknotic nucleus (short arrow) (10.000x); (c) Blebs (arrows) were detected in the nucleus and kinetoplast (40.000x); and (d) membranes were detected inside vacuoles, as indicated by the arrow (20.000x).
Mentions: In addition, our group demonstrated, through ultrastructural studies, that L. (L.) amazonensis promastigote forms treated with 10.96 μg of UA presented with irreversible morphological changes after 18 hours of incubation. Control parasites presented with normal membrane morphology, cytoplasm, nucleus, mitochondrion, and flagellum (Figure 2(a)). Otherwise, treated parasites presented with rounded-shape morphology, and the intracellular environment presented with vacuoles, suggesting organelle degradation (Figure 2(b)) and swelling of the mitochondrion, and a pyknotic nucleus was detected (Figure 2(b)); blebs were also visualized in the nucleus and in the kinetoplast (Figure 2(c)). In addition, intracellular vacuoles presented with fragments of membranes (Figure 2(d)), suggesting degradation of the organelles. Taken together, these results suggest that, in promastigote forms of L. (L.) amazonensis, UA induces a mechanism of death associated to apoptosis or even autophagy. This is the first study that depicted the possible mechanism of action of UA on L. (L.) amazonensis promastigote forms.

Bottom Line: Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids.These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now.Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, via in vivo studies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Patologia de Moléstias Infecciosas, Departamento de Patologia, Faculdade de Medicina da Universidade de São Paulo, Avenue Dr. Arnaldo 455, 06780-210 Cerqueira César, SP, Brazil ; Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Professor Artur Riedel 275, 09972-270 Diadema, SP, Brazil.

ABSTRACT
Triterpenoids are the most representative group of phytochemicals, as they comprise more than 20,000 recognized molecules. These compounds are biosynthesized in plants via squalene cyclization, a C30 hydrocarbon that is considered to be the precursor of all steroids. Due to their low hydrophilicity, triterpenes were considered to be inactive for a long period of time; however, evidence regarding their wide range of pharmacological activities is emerging, and elegant studies have highlighted these activities. Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids. These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now. Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, via in vivo studies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

No MeSH data available.


Related in: MedlinePlus