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Utilization of Microemulsions from Rhinacanthus nasutus (L.) Kurz to Improve Carotenoid Bioavailability.

ABSTRACT: Carotenoids have been known to reduce the risk of several diseases including cancer and cardiovascular. However, carotenoids are unstable and susceptible to degradation. Rhinacanthus nasutus (L.) Kurz (R. nasutus), a Chinese medicinal herb rich in carotenoids, was reported to possess vital biological activities such as anti-cancer. This study intends to isolate carotenoids from R. nasutus by column chromatography, identify and quantify by HPLC-MS, and prepare carotenoid microemulsions for determination of absolute bioavailability in rats. Initially, carotenoid fraction was isolated using 250?mL ethyl acetate poured into an open-column packed with magnesium oxide-diatomaceous earth (1:3, w/w). Fourteen carotenoids including internal standard ?-apo-8'-carotenal were resolved within 62 min by a YMC C30 column and gradient mobile phase of methanol-acetonitrile-water (82:14:4, v/v/v) and methylene chloride. Highly stable carotenoid microemulsions were prepared using a mixture of Capryol(TM)90, Transcutol®HP, Tween 80 and deionized water, with the mean particle being 10.4?nm for oral administration and 10.7?nm for intravenous injection. Pharmacokinetic study revealed that the absolute bioavailability of carotenoids in microemulsions and dispersion was 0.45% and 0.11%, respectively, while a much higher value of 6.25% and 1.57% were shown for lutein, demonstrating 4-fold enhancement in bioavailability upon incorporation of R. nasutus carotenoids into a microemulsion system.

SUBMITTER: Ho NH

PROVIDER: S-EPMC4858739 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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Utilization of Microemulsions from Rhinacanthus nasutus (L.) Kurz to Improve Carotenoid Bioavailability.

Ho Nai-Hsing NH Inbaraj Baskaran Stephen BS Chen Bing-Huei BH

Scientific reports 20160506

Carotenoids have been known to reduce the risk of several diseases including cancer and cardiovascular. However, carotenoids are unstable and susceptible to degradation. Rhinacanthus nasutus (L.) Kurz (R. nasutus), a Chinese medicinal herb rich in carotenoids, was reported to possess vital biological activities such as anti-cancer. This study intends to isolate carotenoids from R. nasutus by column chromatography, identify and quantify by HPLC-MS, and prepare carotenoid microemulsions for determ ...[more]

PMID: 27150134

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Project description:Background:Oxidative 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. Objective:The 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 Methods:RRE 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. Results:On 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 ?g/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 ?g/mL, respectively, but higher than that of RD (IC50 of 50.4 ?g/mL), RN (IC50 of 89.5 ?g/mL), as well as the positive control, rutin (IC50 of 41.5 ?g/mL). Conclusions:The potent superoxide scavenging and albumin glycation inhibitory effect of RRE rationalized its therapeutic application in various chronic diseases, especially in the complications of diabetes. SUMMARY:Rhinacanthins-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

Utilization of Microemulsions from Rhinacanthus nasutus (L.) Kurz to Improve Carotenoid Bioavailability.

Publications

Utilization of Microemulsions from Rhinacanthus nasutus (L.) Kurz to Improve Carotenoid Bioavailability.

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