TY - JOUR
T1 - Bioactivity of Natural Polyphenols as Antiparasitic Agents and their Biochemical Targets
AU - Soto-Sánchez, Jacqueline
N1 - Publisher Copyright:
© 2022 Bentham Science Publishers.
PY - 2022/11
Y1 - 2022/11
N2 - Background: Leishmaniasis and trypanosomiasis are diseases that affect public health worldwide due to their high incidence, morbidity, and mortality. Available treatments are costly, prolonged, and toxic, not to mention the problem of parasite resistance. The development of alternative treatments is justified and polyphenols show promising activity. Objective: The main aim of this mini-review was to analyze the most promising phenolic compounds with reported antileishmanial and antitrypanosomal activity as well as their mechanisms of action. Results: We found that the mode of action of these natural compounds, mainly lignans, neolignans, and flavonoids depends on the organism they act on and includes macrophage activation, induction of morphological changes such as chromatin condensation, DNA fragmentation, accumulation of acidocalcisomes, and glycosomes, Golgi damage and mitochondrial dysfunction as well as negative regulation of mitochondrial enzymes and other essential enzymes for parasite survival such as arginase. This gives a wide scope for future research toward the rational development of anti-kinetoplastid drugs. Conclusion: Although the specific molecular targets, bioavailability, route of administration, and dosages of some of these natural compounds need to be determined, polyphenols and their combinations represent a very promising and safe strategy to be considered for use against Leishmania spp and Trypanosoma spp. In addition, these compounds may provide a scaffold for developing new, more potent, and more selective antiprotozoal agents.
AB - Background: Leishmaniasis and trypanosomiasis are diseases that affect public health worldwide due to their high incidence, morbidity, and mortality. Available treatments are costly, prolonged, and toxic, not to mention the problem of parasite resistance. The development of alternative treatments is justified and polyphenols show promising activity. Objective: The main aim of this mini-review was to analyze the most promising phenolic compounds with reported antileishmanial and antitrypanosomal activity as well as their mechanisms of action. Results: We found that the mode of action of these natural compounds, mainly lignans, neolignans, and flavonoids depends on the organism they act on and includes macrophage activation, induction of morphological changes such as chromatin condensation, DNA fragmentation, accumulation of acidocalcisomes, and glycosomes, Golgi damage and mitochondrial dysfunction as well as negative regulation of mitochondrial enzymes and other essential enzymes for parasite survival such as arginase. This gives a wide scope for future research toward the rational development of anti-kinetoplastid drugs. Conclusion: Although the specific molecular targets, bioavailability, route of administration, and dosages of some of these natural compounds need to be determined, polyphenols and their combinations represent a very promising and safe strategy to be considered for use against Leishmania spp and Trypanosoma spp. In addition, these compounds may provide a scaffold for developing new, more potent, and more selective antiprotozoal agents.
KW - Polyphenols
KW - biological activity
KW - flavonoids
KW - leishmaniasis
KW - molecular targets
KW - trypanosomiasis
UR - http://www.scopus.com/inward/record.url?scp=85138460013&partnerID=8YFLogxK
U2 - 10.2174/1389557522666220404090429
DO - 10.2174/1389557522666220404090429
M3 - Artículo de revisión
C2 - 35379147
AN - SCOPUS:85138460013
SN - 1389-5575
VL - 22
SP - 2661
EP - 2677
JO - Mini-Reviews in Medicinal Chemistry
JF - Mini-Reviews in Medicinal Chemistry
IS - 20
ER -