Identification of BACE1 inhibitors from Panax ginseng saponins—An Insilco approach

Veerappan, Karpagam; Natarajan, Sathishkumar; Subramaniyam, Sathiyamoorthy; Rasappan, Periannan; Samuel, Shila; Kim, Yeon-Ju; Yang, Deok‐Chun

doi:10.1016/j.compbiomed.2013.05.009

Cited by 50 publications

(30 citation statements)

References 51 publications

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“…The diverse constituents and multiple actions of ginseng constituents in the CNS reviewed recently (Kim et al 2013a) will not be elaborated here. The in silco analysis of 12 ginsenosides (see Table 5.2) revealed those with potential interactions with the BACE1 receptor active site essential for enzyme inhibition (Karpagam et al 2013). Further studies included ADMET screening to find the drug-like ginsenosides with a specific ability to cross blood brain barrier (BBB), and to determine safety/toxicity.…”

Section: Ginsengmentioning

confidence: 99%

“…Enhanced the activity of protein phosphatase 2A (PP-2A) involved in tau dephosphorylation In silico approach for discovery of BACE1 inhibitors from Panax ginsenosides included Rb 1 , Rd, Rf, Re, Rg 1 , Rg 2 , Rg 3 , Ro, Rh 1 , Rh 2 , CK, and F1 Rh 1 , Rh 2 , CK, F1 passed the criteria of: molecular docking-evaluated interaction with BACE1 receptor proteins, complex stability, H-bond interactions, ADMET for BBB permeability, having no toxicity (Karpagam et al 2013) Ginsenoside Rg 5 effect on cognition and beta-amyloid deposition in STZ-induced memory impaired rats …”

Section: Ginsengmentioning

confidence: 99%

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Brain Food for Alzheimer-Free Ageing: Focus on Herbal Medicines

Hügel

2015

Advances in Experimental Medicine and Biology

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Healthy brain aging and the problems of dementia and Alzheimer's disease (AD) are a global concern. Beyond 60 years of age, most, if not everyone, will experience a decline in cognitive skills, memory capacity and changes in brain structure. Longevity eventually leads to an accumulation of amyloid plaques and/or tau tangles, including some vascular dementia damage. Therefore, lifestyle choices are paramount to leading either a brain-derived or a brain-deprived life. The focus of this review is to critically examine the evidence, impact, influence and mechanisms of natural products as chemopreventive agents which induce therapeutic outcomes that modulate the aggregation process of beta-amyloid (Aβ), providing measureable cognitive benefits in the aging process. Plants can be considered as chemical factories that manufacture huge numbers of diverse bioactive substances, many of which have the potential to provide substantial neuroprotective benefits. Medicinal herbs and health food supplements have been widely used in Asia since over 2,000 years. The phytochemicals utilized in traditional Chinese medicine have demonstrated safety profiles for human consumption. Many herbs with anti-amyloidogenic activity, including those containing polyphenolic constituents such as green tea, turmeric, Salvia miltiorrhiza, and Panax ginseng, are presented. Also covered in this review are extracts from kitchen spices including cinnamon, ginger, rosemary, sage, salvia herbs, Chinese celery and many others some of which are commonly used in herbal combinations and represent highly promising therapeutic natural compounds against AD. A number of clinical trials conducted on herbs to counter dementia and AD are discussed.

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Section: Ginsengmentioning

confidence: 99%

Section: Ginsengmentioning

confidence: 99%

Brain Food for Alzheimer-Free Ageing: Focus on Herbal Medicines

Hügel

2015

Advances in Experimental Medicine and Biology

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“…A β peptides resulted from the amyloid precursor protein (APP), cleaved by beta secretase (BACE1) and gamma secretase. Several studies have showed that ginseng and ginsenosides have the abilities to enhance the nonamyloidogenic processing of APP by increasing α secretase activities and decrease the amyloidogenic processing by decreasing BACE1 [68, 69]. …”

Section: Effects On the Central Nervous Systemmentioning

confidence: 99%

A Role of Ginseng and Its Constituents in the Treatment of Central Nervous System Disorders

Rokot

Kairupan

Cheng

et al. 2016

Evidence-Based Complementary and Alternative Medicine

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Ginseng, a perennial plant belonging to the Panax genus of the Araliaceae family, has been used in China, Korea, and Japan as a traditional herbal medicine for thousands of years. Ginseng is recorded to have exhibited a wide variety of beneficial pharmacological effects and has become a popular and worldwide known health supplement and drug. The protective effects of ginseng on central nervous system are discussed in this review. Ginseng species and ginsenosides and their intestinal metabolism and bioavailability are concisely introduced. The molecular mechanisms of the effects of ginseng on central nervous system, mainly focused on the neuroprotection properties of ginseng, memory, and learning enhanced properties, and the effects on neurodegenerative disorders are presented. Thus, ginseng and its constituents are of potential merits in the treatment of cerebral disorders.

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“…Rh 1 , Rh 2 , CK, F1 passed the criteria of: molecular docking-evaluated interaction with BACE1 receptor proteins, complex stability, H-bond interactions, ADMET for BBB permeability, having no toxicity (Karpagam et al 2013) Ginsenoside Rg 5 effect on cognition and beta-amyloid deposition in STZ-induced memory impaired rats Rg 5 (5, 10 and 20 mg/kg) improved cognitive dysfunction in rats which was related to attenuating neuro-inflammatory responses with decreased brain levels of inflammatory cytokines TNF-', IL-1"; Congo Red staining and Western blot analysis showed decreased A" deposits (Chu et al 2014 5.2 The structures of ginsenosides Rb 1 and its metabolic transformation product K, and those of Rh 1 , Rh 2 , F 1 inhibition, only the four monoglucosylated ginsenosides CK, Rh 1 , Rh 2 , and F 1 pass the BBB and possess satisfactory drug-like properties. BACE1 and ginseng inhibitor complex crystal structural data to describe their binding modes would provide an accurate picture of the number and length of hydrophobic and hydrogen bond ginsenoside-enzyme interactions.…”

Section: Ginsengmentioning

confidence: 99%

Natural Compounds as Therapeutic Agents for Amyloidogenic Diseases

Vassallo¹

2015

Advances in Experimental Medicine and Biology

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Identification of BACE1 inhibitors from Panax ginseng saponins—An Insilco approach

Cited by 50 publications

References 51 publications

Brain Food for Alzheimer-Free Ageing: Focus on Herbal Medicines

Brain Food for Alzheimer-Free Ageing: Focus on Herbal Medicines

A Role of Ginseng and Its Constituents in the Treatment of Central Nervous System Disorders

Natural Compounds as Therapeutic Agents for Amyloidogenic Diseases

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