Insights Into the Molecular Aspects of Neuroprotective Bacoside A and Bacopaside I

Abstract

Bacopa monnieri, commonly known as Brahmi, has been extensively used as a neuromedicine for various disorders such as anxiety, depression and memory loss. Chemical characterization studies revealed the major active constituents of the herb as the triterpenoid saponins, bacosides. Bacoside A, the vital neuroprotective constituent, is composed of four constituents viz., bacoside A3, bacopaside II, jujubogenin isomer of bacopasaponin C (bacopaside X) and bacopasaponin C. B. monnieri extracts as well as bacosides successfully establish a healthy antioxidant environment in various tissues especially in liver and brain. Free radical scavenging, suppression of lipid peroxidation and activation of antioxidant enzymes by bacosides help to attain a physiological state of minimized oxidative stress. The molecular basis of neuroprotective activity of bacosides is attributed to the regulation of mRNA translation and surface expression of neuroreceptors such as AMPAR, NMDAR and GABAR in the various parts of the brain. Bioavailability as well as binding of neuroprotective agents (such as bacosides) to these receptors is controlled by the Blood Brain Barrier (BBB). However, nano conversion of these drug candidates easily resolves the BBB restriction and carries a promising role in future therapies. This review summarizes the neuroprotective functions of the B. monnieri extracts as well as its active compounds (bacoside A, bacopaside I) and the molecular mechanisms responsible for these pharmacological activities.

Characterization of Metabolites in Plasma, Urine and Feces of Healthy Participants after Taking Brahmi Essence for Twelve Weeks Using LC-ESI-QTOF-MS Metabolomic Approach

“…As shown in Figure S1a,b , the five saponins glycosides (bacoside A 3 , bacopaside II, bacopaside X, bacopaside I, and bacopasaponin C) were present in the Brahmi essence, but not in the placebo. These compounds have been reported to be responsible for the pharmacological effect of Brahmi [ 19 , 20 ]. As mulberry is the ingredient of both placebo and Brahmi essence, some chemical constituents of mulberry—such as cyanidin 3-O-rutinoside, cyanidin 3-O-glucoside and rutin—were found in both Brahmi essences and placebo ( Figure S1a and b and Table S1, Supplementary Material ).…”

“…The phytosterols (stigmasterol, β-sitosterol) and flavonoids (apigenin and luteolin) were also reported from Bacopa [ 15 , 18 ]. Bacoside A—which is a mixture of bacoside A 3 , bacopaside II, bacopasaponin C, and bacopaside X—has been reported for nootropic and neuroprotective activities [ 19 , 20 ].…”

Potential Herb–Drug Interactions in the Management of Age-Related Cognitive Dysfunction

“…In fact, inflammation plays an important role in age-related cognitive disorders [50] and, as such, antioxidative molecules and the inhibitors of pro-inflammatory enzymes or cytokines, present in many (58%) of the plants considered, may improve cognition. As examples, Bacopa monnieri [51] has been associated with a reduction of radical oxygen associated inflammation and plants, such as Foeniculum vulgare [52] and Centella asiatica [53], inhibit the production of phospholipase A2. Crocin from Crocus sativus suppressed formation of brain inflammatory mediators, such as interleukin-1 and tumor necrosis factor-α [54].…”

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“…The bacoside establish a healthy anti-oxidant environment in liver and brain. The neuroprotective activity is attributed to the regulation of mRNA translation & surface expression of neuroreceptors such as AMPAR, NMDAR, and GABAR in the various parts of the brain 19 .…”