Natural products as a source of Alzheimer's drug leads

Williams, Philip G.; Sorribas, Analia; Howes, Melanie‐Jayne R.

doi:10.1039/c0np00027b

Cited by 358 publications

(242 citation statements)

References 384 publications

(616 reference statements)

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“…Several small molecules have been reported to exhibit inhibitory properties in neurodegeneration (Mandel et al, 2006;Ramassamy, 2006;Williams et al, 2011).…”

Section: Research Articlementioning

confidence: 99%

Bioactive compounds from endemic plants of Southwest Portugal: Inhibition of acetylcholinesterase and radical scavenging activities

Tavares¹,

Tyagi²,

Barata³

et al. 2011

Pharmaceutical Biology

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“…Several small molecules have been reported to exhibit inhibitory properties in neurodegeneration (Mandel et al, 2006;Ramassamy, 2006;Williams et al, 2011).…”

Section: Research Articlementioning

confidence: 99%

Bioactive compounds from endemic plants of Southwest Portugal: Inhibition of acetylcholinesterase and radical scavenging activities

Tavares¹,

Tyagi²,

Barata³

et al. 2011

Pharmaceutical Biology

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“…HPLC analysis results in the presence of phenolic acids, flavonoids and pentacyclic triterpenoid betulinic acid in the methanol extracts of stem and leaf of S. crenata in varied amounts. Similarly, Shih, Chan [86], Zhang, Cao [87], Lloret, Badia [88] recently reported several polyphenols such as phenolic acids, flavonoids, anthocyanins and vitamin E with strong antioxidant activity that play a crucial role in the prevention of neurodegenerative diseases pathophysiology.…”

Section: Discussionmentioning

confidence: 99%

Medicinal Plants Anti-cholinesterase Activity and the Potential for Alzheimer’s Disease Treatment

Usman¹

2017

JDMP

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Abstract:Alzheimer's disease (AD) is a slow and progressive neurodegenerative disease, leading to a breakdown in memory preservation and absence of cognitive reasoning and language skills. It is the most popular neurodegenerative disease worldwide, with nearly 20 million new incidences recorded every year. The enzymes, acetyl cholinesterase (AChE) and butyryl-cholinesterase (BChE) play important roles in the cholinergic deficit through enhanced degradation of the neurotransmitter, acetylcholine (ACh). In most cases, to improve neurotransmission and to alleviate cholinergic deficit, the focus is mainly on acetyl cholinesterase (AChE) and butyl cholinesterase (BCh). Currently, drugs for the treatment of AD (Rivastigmine, galanthamine, donepezil and Memantine) targets the later stages and implicated in the progression of the disease. Acetyl cholinesterase enzyme (AChE) is especially an attractive target for the rational drug design and for the discovery of mechanism based inhibitors; this is because of its role in the hydrolysis of neurotransmitter, acetylcholine. Many plants serve as potential source of AChE and BChE inhibitors, and useful compounds that could provide templates for the development of drugs for the treatment of AD. This paper provides a review of several medicinal plants tested for anti-AChE and or BChE, many of which contains promising bioactive compounds as potential anti-cholinesterase that could serve as candidates for the development of drugs to treat AD.

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“…[19] Among these compounds are found physostigmine (1), [20][21][22] Huperzine A (2), [23,24] and galanthamine (3). [25,26] Other AChEIs of relevance, but obtained by synthesis, are Tacrine (4), [27] donepezil (5) [28,29] and rivastigmine (6), [30] the latter being a semi-synthetic derivative of 1.…”

Section: Introductionmentioning

confidence: 99%

Study of the interaction of Huperzia saururus Lycopodium alkaloids with the acetylcholinesterase enzyme

Puiatti

Borioni

Vallejo

et al. 2013

Journal of Molecular Graphics and Modelling

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Abstract:In the present study, we describe and compare the binding modes of three Lycopodium alkaloids (sauroine, 6-hydroxylycopodine and sauroxine; isolated from Huperzia saururus) and huperzine A with the enzyme acetylcholinesterase. Refinement and rescoring of the docking poses (obtained with different programs) with an all atom force field helped to improve the quality of the protein-ligand complexes. Molecular dynamics simulations were performed to investigate the complexes and the alkaloid's binding modes. The combination of the latter two methodologies indicated that binding in the active site is favored for the active compounds. On the other hand, similar binding energies in both the active and the peripheral sites were obtained for sauroine, thus explaining its experimentally determined lack of activity. MM-GBSA predicted the order of binding energies in agreement with the experimental IC 50 values.

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Natural products as a source of Alzheimer's drug leads

Cited by 358 publications

References 384 publications

Bioactive compounds from endemic plants of Southwest Portugal: Inhibition of acetylcholinesterase and radical scavenging activities

Bioactive compounds from endemic plants of Southwest Portugal: Inhibition of acetylcholinesterase and radical scavenging activities

Medicinal Plants Anti-cholinesterase Activity and the Potential for Alzheimer’s Disease Treatment

Study of the interaction of Huperzia saururus Lycopodium alkaloids with the acetylcholinesterase enzyme

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