Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles.

Pimsumon Jiamboonsri,Song Gao,Rapepol Bavovada,Ming Hu,Pimolpan Pithayanukul,Taijun Yin,Jiraporn Leanpolchareanchai

doi:10.3390/molecules201219759

Pimsumon Jiamboonsri, Song Gao + Show 5 more

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https://doi.org/10.3390/molecules201219759

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Abstract

Mango seed kernel extract (MSKE) and its key components (gallic acid, GA; methyl gallate, MG; and pentagalloyl glucopyranose, PGG) have generated interest because of their pharmacological activities. To develop the potential use of the key components in MSKE as natural therapeutic agents, their pharmacokinetic data are necessary. Therefore, this study was performed to evaluate the factors affecting their oral bioavailability as pure compounds and as components in MSKE. The in vitro chemical stability, biological stability, and absorption were evaluated in Hanks’ Balanced Salt Solution, Caco-2 cell and rat fecal lysates, and the Caco-2 cell model, respectively. The in vivo oral pharmacokinetic behavior was elucidated in Sprague-Dawley rats. The key components were unstable under alkaline conditions and in Caco-2 cell lysates or rat fecal lysates. The absorptive permeability coefficient followed the order MG > GA > PGG. The in vivo results exhibited similar pharmacokinetic trends to the in vitro studies. Additionally, the co-components in MSKE may affect the pharmacokinetic behaviors of the key components in MSKE. In conclusion, chemical degradation under alkaline conditions, biological degradation by intestinal cell and colonic microflora enzymes, and low absorptive permeability could be important factors underlying the oral bioavailability of these polyphenols.

Highlights

Mango (Mangifera indica L.) belongs to the family Anacardiaceae and is one of the most popular edible fruits around the world because of its unique taste and nutritional value
At concentrations of 2 and 20 μM, all three individual standard phenolic compounds decomposed in Hanks’ Balanced Salt Solution (HBSS) at pH 8 within 4 h, whereas they were stable in HBSS at pH 6 for 8 h (Figure 1A,B)
Because Mango seed kernel extract (MSKE) has been reported to Mbeolecaulseso2u0r1c5e, 20o,fpahgieg–hpamgeolecular weight hydrolyzable tannins, such as hexa, hepta, octa, nona, and deca-O-galloylglucose, which are known to be degraded into smaller molecules [20], itnhcereiansceredasreedcorveecroievseroiefsGoAf G, MA,GM, Gan,danPdGPGGmG amyahyahvaevbeebeenena arerseuslutltofofththeeddeeggrraaddaatitoionnooff ootthheerr uunniiddeennttiiffiieedd ccoonnssttiittuueennttss iinn MMSSKKEE

Summary

Introduction

Mango (Mangifera indica L.) belongs to the family Anacardiaceae and is one of the most popular edible fruits around the world because of its unique taste and nutritional value. Mango is an excellent source of antioxidants, including phenolic compounds, carotenoids, and vitamin C [1]. Oils and starches, other phytochemical compounds such as tannins, coumarin, ellagic acid, vanillin, mangiferin, ferulic acid, and cinnamic acid have been observed and characterized in mango kernels [2,3]. Mango seed kernel extract (MSKE) and its major phenolic constituents have been shown to exert interesting pharmacological activities both in vitro and in vivo, including in vitro anti-methicillin-resistant Staphylococcus aureus activity [5], potent free radical scavenging and antioxidant, anti-inflammatory [4], and anti-enzymatic (e.g., tyrosinase, phospholipase and hyaluronidase) activities [6,7,8] and in vivo anti-hepatotoxicity activity against liver damage induced by carbon tetrachloride [4]

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