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Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers.
Curr Med Chem. 2016; 23(36):4151-4174.CM

Abstract

The central nervous system (CNS) is a mythical target for drug delivery. There is an ongoing debate over the brain accessibility of flavonoids, a group of plant-derived secondary metabolites widely known by their multifarious bioactivities achieved by distinct mechanisms. Recently, their applicability in the management of neurologic and psychiatric disorders, such as Alzheimer's and Parkinson's diseases, and major depression, has received particular attention. To reach their target, flavonoids must cross over the ultimate obstacle - the blood-brain barrier - at pharmacologically effective concentrations. This review addresses the low brain-bioavailability issue, based on in vitro and in vivo evidences. Besides the lipophilic character of the flavonoids, their permeability will depend upon the role of membrane transporters, especially those from the ABC superfamily. The enzymatic elements, namely β-glucuro-nidase, can induce a transient deconjugation process and affect permeability, as well. Novel drug delivery systems are successful strategies to overcome the low bioavailability issue, and redirect the native forms to CNS-targets. This work bridges a solid opinion over this hot topic of medicinal chemistry and natural products research.

Authors+Show Affiliations

Requimte/LAQV - Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, nº 228, Porto 4050-313, Portugal.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27516197

Citation

Andrade, Paula Branquinho, et al. "Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers." Current Medicinal Chemistry, vol. 23, no. 36, 2016, pp. 4151-4174.
Andrade PB, Grosso C, Valentao P, et al. Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers. Curr Med Chem. 2016;23(36):4151-4174.
Andrade, P. B., Grosso, C., Valentao, P., & Bernardo, J. (2016). Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers. Current Medicinal Chemistry, 23(36), 4151-4174.
Andrade PB, et al. Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers. Curr Med Chem. 2016;23(36):4151-4174. PubMed PMID: 27516197.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers. AU - Andrade,Paula Branquinho, AU - Grosso,Clara, AU - Valentao,Patrícia, AU - Bernardo,Joao, PY - 2016/05/20/received PY - 2016/07/22/revised PY - 2016/08/02/accepted PY - 2016/8/16/pubmed PY - 2017/2/9/medline PY - 2016/8/13/entrez SP - 4151 EP - 4174 JF - Current medicinal chemistry JO - Curr Med Chem VL - 23 IS - 36 N2 - The central nervous system (CNS) is a mythical target for drug delivery. There is an ongoing debate over the brain accessibility of flavonoids, a group of plant-derived secondary metabolites widely known by their multifarious bioactivities achieved by distinct mechanisms. Recently, their applicability in the management of neurologic and psychiatric disorders, such as Alzheimer's and Parkinson's diseases, and major depression, has received particular attention. To reach their target, flavonoids must cross over the ultimate obstacle - the blood-brain barrier - at pharmacologically effective concentrations. This review addresses the low brain-bioavailability issue, based on in vitro and in vivo evidences. Besides the lipophilic character of the flavonoids, their permeability will depend upon the role of membrane transporters, especially those from the ABC superfamily. The enzymatic elements, namely β-glucuro-nidase, can induce a transient deconjugation process and affect permeability, as well. Novel drug delivery systems are successful strategies to overcome the low bioavailability issue, and redirect the native forms to CNS-targets. This work bridges a solid opinion over this hot topic of medicinal chemistry and natural products research. SN - 1875-533X UR - https://www.unboundmedicine.com/medline/citation/27516197/Flavonoids_in_Neurodegeneration:_Limitations_and_Strategies_to_Cross_CNS_Barriers_ L2 - https://www.eurekaselect.com/144627/article DB - PRIME DP - Unbound Medicine ER -