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Rhinacanthin-C but Not -D Extracted from Rhinacanthus nasutus (L.) Kurz Offers Neuroprotection via ERK, CHOP, and LC3B Pathways.

ABSTRACT: Neurodegenerative diseases present an increasing problem as the world's population ages; thus, the discovery of new drugs that prevent diseases such as Alzheimer's, and Parkinson's diseases are vital. In this study, Rhinacanthin-C and -D were isolated from Rhinacanthus nasustus, using ethyl acetate, followed by chromatography to isolate Rhinacanthin-C and -D. Both compounds were confirmed using NMR and ultra-performance-LCMS. Using glutamate toxicity in HT-22 cells, we measured cell viability and apoptosis, ROS build-up, and investigated signaling pathways. We show that Rhinacanthin-C and 2-hydroxy-1,4-naphthoquinone have neuroprotective effects against glutamate-induced apoptosis in HT-22 cells. Furthermore, we see that Rhinacanthin-C resulted in autophagy inhibition and increased ER stress. In contrast, low concentrations of Rhinacanthin-C and 2-hydroxy-1,4-naphthoquinone prevented ER stress and CHOP expression. All concentrations of Rhinacanthin-C prevented ROS production and ERK1/2 phosphorylation. We conclude that, while autophagy is present in HT-22 cells subjected to glutamate toxicity, its inhibition is not necessary for cryoprotection.

SUBMITTER: Rakkhittawattana V

PROVIDER: S-EPMC9145051 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

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Rhinacanthin-C but Not -D Extracted from <i>Rhinacanthus nasutus</i> (L.) Kurz Offers Neuroprotection via ERK, CHOP, and LC3B Pathways.

Rakkhittawattana Varaporn V Panichayupakaranant Pharkphoom P Prasanth Mani I MI Brimson James M JM Tencomnao Tewin T

Pharmaceuticals (Basel, Switzerland) 20220520 5

Neurodegenerative diseases present an increasing problem as the world's population ages; thus, the discovery of new drugs that prevent diseases such as Alzheimer's, and Parkinson's diseases are vital. In this study, Rhinacanthin-C and -D were isolated from <i>Rhinacanthus nasustus</i>, using ethyl acetate, followed by chromatography to isolate Rhinacanthin-C and -D. Both compounds were confirmed using NMR and ultra-performance-LCMS. Using glutamate toxicity in HT-22 cells, we measured cell viabi ...[more]

PMID: 35631453

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Project description:BackgroundOxidative stress and nonenzymatic protein glycation lead to serious diabetic complications that increase the risk of mortality. Rhinacanthus nasutus leaf crude extracts are previously reported for their antidiabetic, antiglycation, and antioxidant potential.ObjectiveThe present study was performed to prepare a standardized rhinacanthins-rich extract (RRE) and evaluate its superoxide scavenging and antiglycation effects as compared to its marker compounds, namely, rhinacanthin-C (RC), rhinacanthin-D (RD), and rhinacanthin-N (RN).Materials and methodsRRE was obtained by microwave-assisted green extraction along with a simple step of fractionation using Amberlite® column. RC, RD, and RN were isolated from the RRE using silica gel column chromatography. Superoxide scavenging activity was performed by cyclic voltammetry, and fructose-mediated human serum albumin glycation model was used for antiglycation activity. In silico studies were conducted to identify the structure-activity relationships of rhinacanthins.ResultsOn the basis of kinetic measurements, RRE exhibited the most potent antioxidant activity via ErCi mechanism, with a 50% inhibitory concentration (IC50) value of 8.0 μg/mL, antioxidant capacity of 39439 M-1, and binding constant of 45709 M-1. Antiglycation assay showed that RRE exhibited almost equivalent glycation inhibitory effect to that of RC, with IC50 values of 39.7 and 37.3 μg/mL, respectively, but higher than that of RD (IC50 of 50.4 μg/mL), RN (IC50 of 89.5 μg/mL), as well as the positive control, rutin (IC50 of 41.5 μg/mL).ConclusionsThe potent superoxide scavenging and albumin glycation inhibitory effect of RRE rationalized its therapeutic application in various chronic diseases, especially in the complications of diabetes.SummaryRhinacanthins-rich extract (RRE) exhibited potent superoxide scavenging activityRRE and rhinacanthin-C showed remarkable and comparable antiglycation effectRhinacanthins exhibited antiglycation activity by masking specific residues of albumin. Abbreviations used: RRE: Rhinacanthins-rich extract; RC: Rhinacanthin-C; RD: Rhinacanthin-D; RN: Rhinacanthin-N; IC50: 50% inhibitory concentration; Kao: Antioxidant activity coefficient; Kb: Binding constant; ErCi: Reversible electron transfer followed by an irreversible chemical reaction; DM: Diabetes mellitus; AGEPs: Advanced glycation end products; NMR: Nuclear magnetic resonance; HPLC: High-performance liquid chromatography; CV: Cyclic voltammetry; DMSO: Dimethyl sulfoxide; Ipa: Anodic peak current; Ipc: Cathodic peak current; HSA: Human serum albumin; MOE: Molecular operating environment; PASSonline: Online prediction of activity spectra for substances.

Dataset Information

Rhinacanthin-C but Not -D Extracted from Rhinacanthus nasutus (L.) Kurz Offers Neuroprotection via ERK, CHOP, and LC3B Pathways.

Publications

Rhinacanthin-C but Not -D Extracted from <i>Rhinacanthus nasutus</i> (L.) Kurz Offers Neuroprotection via ERK, CHOP, and LC3B Pathways.

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