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1.
Pharmaceutics ; 14(10)2022 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-36297575

RESUMEN

The family of nuclear peroxisome proliferator-activated receptors (PPARα, PPARß/δ, and PPARγ) is a set of ligand-activated transcription factors that regulate different functions in the body. Whereas activation of PPARα is known to reduce the levels of circulating triglycerides and regulate energy homeostasis, the activation of PPARγ brings about insulin sensitization and increases the metabolism of glucose. On the other hand, PPARß when activated increases the metabolism of fatty acids. Further, these PPARs have been claimed to be utilized in various metabolic, neurological, and inflammatory diseases, neurodegenerative disorders, fertility or reproduction, pain, and obesity. A series of different heterocyclic scaffolds have been synthesized and evaluated for their ability to act as PPAR agonists. This review is a compilation of efforts on the part of medicinal chemists around the world to find novel compounds that may act as PPAR ligands along with patents in regards to PPAR ligands. The structure-activity relationship, as well as docking studies, have been documented to better understand the mechanistic investigations of various compounds, which will eventually aid in the design and development of new PPAR ligands. From the results of the structural activity relationship through the pharmacological and in silico evaluation the potency of heterocycles as PPAR ligands can be described in terms of their hydrogen bonding, hydrophobic interactions, and other interactions with PPAR.

2.
Curr Top Med Chem ; 22(24): 2045-2067, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35524663

RESUMEN

BACKGROUND: All currently available antimalarial drugs are developed from natural product lineages that may be traced back to herbal medicines, including quinine, lapachol, and artemisinin. Natural products that primarily target free radicals or reactive oxygen species, play an important role in treating malaria. OBJECTIVES: This review analyses the role of antioxidative therapy in treating malaria by scavenging or countering free radicals and reviews the importance of natural plant extracts as antioxidants in oxidative therapy of malaria treatment. METHODS: The search for natural antioxidants was conducted using the following databases: ResearchGate, ScienceDirect, Google Scholar, and Bentham Science with the keywords malaria, reactive oxygen species, natural antioxidants, and antiplasmodial. CONCLUSION: This study reviewed various literature sources related to natural products employed in antimalarial therapy directly or indirectly by countering/scavenging reactive oxygen species published between 2016 till date. The literature survey made it possible to summarize the natural products used in treating malaria, emphasizing botanical extracts as a single component and in association with other botanical extracts. Natural antioxidants like polyphenols, flavonoids, and alkaloids, have a broad range of biological effects against malaria. This review is pivoted around natural antioxidants obtained from food and medicinal plants and explores their application in restraining reactive oxygen species (ROS). We anticipate this article will provide information for future research on the role of antioxidant therapy in malaria infection.


Asunto(s)
Antimaláricos , Productos Biológicos , Malaria , Plantas Medicinales , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Especies Reactivas de Oxígeno/uso terapéutico , Antimaláricos/farmacología , Antimaláricos/uso terapéutico , Malaria/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico
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