Blood-Brain Barrier Permeability of Asiaticoside, Madecassoside and Asiatic Acid in Porcine Brain Endothelial Cell Model

Hanapi, Nur Aziah; Arshad, Ahmad Saifuddin Mohamad; Abdullah, Jafri Malin; Muhammad, Tengku Sifzizul Tengku; Yusof, Siti R.

doi:10.1016/j.xphs.2020.09.015

Cited by 22 publications

(14 citation statements)

References 68 publications

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“…The apparent oral bioavailability of madecassoside and asiaticoside was less than 1% due to larger molecular sizes and the presence of sugar moiety in their structures [ 16 ]. A recent study showed that madecassoside, asiaticoside, and asiatic acid are highly BBB permeable towards in vitro BBB models from primary porcine brain endothelial cells (PBECs) [ 63 ]. However, there are no reported findings on C. asiatica extract and nanoemulsion formulation.…”

Section: Resultsmentioning

confidence: 99%

Development and Optimization of Nanoemulsion from Ethanolic Extract of Centella asiatica (NanoSECA) Using D-Optimal Mixture Design to Improve Blood-Brain Barrier Permeability

Jusril

Imran

Khalil

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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The evidence on the neuroprotective impact of Centella asiatica (C. asiatica) has been greatly documented in recent years. However, a major obstacle that remains to be overcome is the capacity of the active molecules in C. asiatica to cross the blood-brain barrier (BBB). In this study, we explored the possibilities of using a D-optimal mixture design to fabricate nanoemulsion of C. asiatica (NanoSECA) for better brain bioavailability. The parameters for optimization were the percentage of water (10–80% w/v) and virgin coconut oil (VCO) (10–80% w/v). Nanoemulsions were formulated using a high-pressure homogenization approach and were characterized for their physicochemical properties. The optimal VCO-based nanoemulsion (VBN: F2) conditions were found at 80% (w/v) of water and 10% (w/v) of VCO. Subsequently, viability tests were conducted on neuroblastoma (SH-SY5Y) and macrophage (RAW 264.7) cell lines. NanoSECA was distinguished for its antioxidant, acetylcholinesterase (AChE), anti-inflammatory, and parallel artificial membrane permeability assay (PAMPA) activities in vitro. The NanoSECA has a particle size of 127.833 ± 8.280 nm, zeta potential (ZP) of −24.9 ± 0.011 mV, polydispersity index (PDI) of 0.493 ± 4.681, percentage prediction error (PPE) of −12.02%, and pH of 6.0 ± 0.006 and is also stable under different storage conditions. Cell viability was improved in a dose-dependent manner on SH-SY5Y and RAW 264.7 cell lines. In addition, NanoSECA significantly reduced the AChE activity, suppressing the level of proinflammatory mediators and oxidative stress. Moreover, NanoSECA showed high BBB permeation with a high value of experimental permeability to cross the BBB. Thus, NanoSECA could efficiently potentiate the central nervous system (CNS) therapeutic activities through enhanced penetration of BBB. These nano-delivery systems are crucial to unlock the full potential of C. asiatica for treating numerous CNS disorders.

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Section: Resultsmentioning

confidence: 99%

Development and Optimization of Nanoemulsion from Ethanolic Extract of Centella asiatica (NanoSECA) Using D-Optimal Mixture Design to Improve Blood-Brain Barrier Permeability

Jusril

Imran

Khalil

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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“…AA was reported to have beneficiary effects on wound healing, cancer, and neurodegenerative diseases [ 146 ]. This substance can penetrate the BBB and enter the CNS [ 147 ]. AA has shown acceptable pharmacokinetics following oral or intraperitoneal administration [ 146 ].…”

Section: Tlrs and Pdmentioning

confidence: 99%

The role of Toll-like receptors and neuroinflammation in Parkinson’s disease

Heidari

Yazdanpanah

Rezaei

2022

J Neuroinflammation

127

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Background Parkinson’s disease (PD) is the second most prevalent neurodegenerative disorder, characterized by motor and non-motor symptoms, significantly affecting patients’ life. Pathologically, PD is associated with the extensive degeneration of dopaminergic neurons in various regions of the central nervous system (CNS), specifically the substantia nigra. This neuronal loss is accompanied by the aggregation of misfolded protein, named α-synuclein. Main text Recent studies detected several clues of neuroinflammation in PD samples using postmortem human PD brains and various PD animal models. Some evidence of neuroinflammation in PD patients included higher levels of proinflammatory cytokines in serum and cerebrospinal fluid (CSF), presence of activated microglia in various brain regions such as substantia nigra, infiltration of peripheral inflammatory cells in affected brain regions, and altered function of cellular immunity like monocytes phagocytosis defects. On the other side, Toll-like receptors (TLRs) are innate immune receptors primarily located on microglia, as well as other immune and non-immune cells, expressing pivotal roles in recognizing exogenous and endogenous stimuli and triggering inflammatory responses. Most studies indicated an increased expression of TLRs in the brain and peripheral blood cells of PD samples. Besides, this upregulation was associated with excessive neuroinflammation followed by neurodegeneration in affected regions. Therefore, evidence proposed that TLR-mediated neuroinflammation might lead to a dopaminergic neural loss in PD patients. In this regard, TLR2, TLR4, and TLR9 have the most prominent roles. Conclusion Although the presence of inflammation in acute phases of PD might have protective effects concerning the clearance of α-synuclein and delaying the disease advancement, the chronic activation of TLRs and neuroinflammation might lead to neurodegeneration, resulting in the disease progression. Therefore, this study aimed to review additional evidence of the contribution of TLRs and neuroinflammation to PD pathogenesis, with the hope that TLRs could serve as novel disease-modifying therapeutic targets in PD patients in the future.

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“…[93][94][95][96][97][98] In addition, it is also known as an anti-inflammatory, cardioprotector, and neuroprotector. [99][100][101][102][103][104] The ECa233 standardized extract containing the four triterpenoid compounds has been tested for safety. 105 Asiaticoside (Figure3A) has been studied to have properties as an anti-inflammatory, lung protector, neuroprotector, and antiresorptive agent on the bone (bone protector).…”

Section: Figure 3: Compouds Isolated From C Asiatica (L)): (A) Asiati...mentioning

confidence: 99%

Indonesian Medicinal Plants with Anti-inflammatory Properties and Potency as Chronic Obstructive Pulmonary Disease (COPD) Herbal Medicine

Rahminiwati¹,

Trivadila²,

Iswantini³

et al. 2022

Pharmacogn. J.

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Indonesia is a tropical country with mega-biodiversity. Several medicinal plants locally have been recognized for their anti-inflammatory properties and are traditionally used to help treat respiratory diseases. Chronic obstructive pulmonary disease (COPD) is one of the diseases known as the high cause of death globally, and one of the treatment efforts is by using anti-inflammatory drugs. In developing alternative remedies for COPD, this review summarizes the potential of Indonesian medicinal plants and their ingredients known to have an anti-inflammatory activity to develop alternative remedies for COPD. Primarily, we focus on the medicinal plants that have been scientifically proven to pose some biological activities, such as legetan warak (Adenostemma lavenia), celery (Apium graveolens), pegagan (Centella asiatica), kenikir (Cosmos caudatus), and kersen (Muntingia calabura). This review is expected to provide more information about Indonesian medicinal plants and their potencies to be developed as COPD herbal medicine and, further, as a treatment to help patients suffering from coronavirus disease (COVID-19).

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Blood-Brain Barrier Permeability of Asiaticoside, Madecassoside and Asiatic Acid in Porcine Brain Endothelial Cell Model

Cited by 22 publications

References 68 publications

Development and Optimization of Nanoemulsion from Ethanolic Extract of Centella asiatica (NanoSECA) Using D-Optimal Mixture Design to Improve Blood-Brain Barrier Permeability

Development and Optimization of Nanoemulsion from Ethanolic Extract of Centella asiatica (NanoSECA) Using D-Optimal Mixture Design to Improve Blood-Brain Barrier Permeability

The role of Toll-like receptors and neuroinflammation in Parkinson’s disease

Indonesian Medicinal Plants with Anti-inflammatory Properties and Potency as Chronic Obstructive Pulmonary Disease (COPD) Herbal Medicine

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