Juliflorine: A potent natural peripheral anionic-site-binding inhibitor of acetylcholinesterase with calcium-channel blocking potential, a leading candidate for Alzheimer’s disease therapy

Choudhary, M. Iqbal; Nawaz, Syed Junaid; Ul-Haq, Zaheer; Azim, M. Kamran; Ghayur, Muhammad Nabeel; Lodhi, Muhammad Arif; Jalil, Saima; Khalid, Asaad; Khalid, Asaad; Rode, Bernd M.; Atta-ur-Rahman, _; Gilani, Anwarul Hassan; Ahmad, Viqar Uddin

doi:10.1016/j.bbrc.2005.05.068

Cited by 82 publications

(48 citation statements)

References 35 publications

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“…Interestingly, the presence of a unique combination of activities (ACE inhibitory and calcium antagonist) was found in Sarcococca saligna with active chemicals identified Gilani et al, 2005b). Similarly, juliflorine from Prosopis juliflora and Withanolides from Withania somnifera were found to possess this unique combination of activities (Choudhary et al, 2005(Choudhary et al, , 2005a. These studies points towards the therapeutic potential of such plants, or their active chemicals (with dual action) in AD.…”

Section: Synergistic And/or Side-effects Nullifying Combinations In Pmentioning

confidence: 85%

Trends in ethnopharmacology

Gilani

Atta-ur-Rahman

2005

Journal of Ethnopharmacology

429

275

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Section: Synergistic And/or Side-effects Nullifying Combinations In Pmentioning

confidence: 85%

Trends in ethnopharmacology

Gilani

Atta-ur-Rahman

2005

Journal of Ethnopharmacology

429

275

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“…7. Structures of AChE inhibitors colleagues reported a new biological activity of juliflorine as an inhibitor of AChE and butyrylcholinesterase enzymes (Choudhary et al, 2005b).…”

Section: Inhibitors Of Acetylcholinesterase (Ache)mentioning

confidence: 99%

Potential therapeutic agents against Alzheimer’s disease from natural sources

Park

2010

Arch. Pharm. Res.

106

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The average human life span in developed countries has increased to more than 80 years following rapid breakthrough and developments in modern medicine and science, resulting in prolonged life expectancy and increase in the population counts of the geriatric age group. This translates into a dramatic increase in disease burden of elderly patients suffering from senile disorders including neurodegenerative diseases, particularly Alzheimer's disease (AD). AD is characterized by the death of nerve cells in the cerebral cortex and is the most common subtype of dementia that affected 25 million people worldwide in 2000 and is expected to increase to 114 million by 2050. Despite the exponential growth in the number of AD patients, only acetylcholinesterase (AChE) inhibitors are being currently used to treat AD. It is well known that AChE inhibitors can alleviate the symptoms of AD but not halt the disease progression. Consequently, therapeutic agents against AD acting at various pathologic levels are needed. In the recent decade, natural products with anti-AD properties have attracted much attention. But very few natural products have been investigated in a scientifically justifiable method for these biological activities. Following a detailed research process, it is certain that natural products have a strong potential to develop biologically active compounds with new chemical structures. Many studies have been carried out to identify the naturally occurring anti-AD agents. This review article describes the molecular targets aiming at developing the anti-AD agents including the inhibition of AChE, inhibition of Aβ production by enhancing α-secretase (non-amyloidogenic pathway) or inhibiting β- and γ-secretases (amyloidogenic pathway), alleviating Aβ-induced neurotoxicity or reducing Aβ-induced neuroinflammation. In addition, this paper summarizes the potential of some of the natural products that might inhibit specific molecular targets and slow the progression of this disease.

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“…A further initial binding is thought to occur at the outer rim of the gorge, at the peripheral anionic site (PAS [16]). Ligands of the PAS as well as compounds with gorge-spanning binding modes, reaching from the PAS to the active site, have been reported [17][18][19].…”

Section: Introductionmentioning

confidence: 99%

Applications of Integrated Data Mining Methods to Exploring Natural Product Space for Acetylcholinesterase Inhibitors

Schuster

Kern²,

Hristozov³

et al. 2010

CCHTS

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Nature, especially the plant kingdom, is a rich source for novel bioactive compounds that can be used as lead compounds for drug development. In order to exploit this resource, the two neural network-based virtual screening techniques novelty detection with self-organizing maps (SOMs) and counterpropagation neural network were evaluated as tools for efficient lead structure discovery. As application scenario, significant descriptors for acetylcholinesterase (AChE) inhibitors were determined and used for model building, theoretical model validation, and virtual screening. Top-ranked virtual hits from both approaches were docked into the AChE binding site to approve the initial hits. Finally, in vitro testing of selected compounds led to the identification of forsythoside A and (+)-sesamolin as novel AChE inhibitors.

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Juliflorine: A potent natural peripheral anionic-site-binding inhibitor of acetylcholinesterase with calcium-channel blocking potential, a leading candidate for Alzheimer’s disease therapy

Cited by 82 publications

References 35 publications

Trends in ethnopharmacology

Trends in ethnopharmacology

Potential therapeutic agents against Alzheimer’s disease from natural sources

Applications of Integrated Data Mining Methods to Exploring Natural Product Space for Acetylcholinesterase Inhibitors

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