Water-dispersible unadulterated α-mangostin particles for biomedical applications

Abstract

α-Mangostin, the extract from pericarp of Garcinia mangostana L . or mangosteen fruit, has been applied in various biomedical products because of its minimal skin irritation, and prominent anti-inflammatory, antimicrobial and immune-modulating activities. Owing to its low water solubility, the particle formulations are necessary for the applications of α-mangostin in aqueous media. The particle formulations are usually prepared using surfactants and/or polymers, usually at a larger amount of these auxiliaries than the amount of α-mangostin itself. Here, we show the self-assembly of α-mangostin molecules into water-dispersible particles without a need of any polymers/surfactants. Investigations on chemical structure, crystallinity and thermal properties of the obtained α-mangostin particles, in comparison to the conventional α-mangostin crystalline solid, confirm no formation of the new compound during the particle formation and suggest changes in intermolecular interactions among α-mangostin molecules and significantly more hydroxyl functionality positioned at the particles' surface. The ability of the water suspension of the α-mangostin to inhibit the growth of Propionibacterium acnes , the acne-causing bacteria, is similar to that of the solution of the conventional α-mangostin in 5% dimethyl sulfoxide. Moreover, at 12.7 ppm in an aqueous environment of RAW 264.7 cell culture, α-mangostin suspension exhibits five times higher anti-inflammatory activity than the conventional α-mangostin solution, with the same acceptable cytotoxicity of less than 20% cell death.

Alpha-glucosidase inhibitory activity of the combination of Caesalpinia sappan L. and Garcinia mangostana extract

“…This study also analyzed the presence of mangostin, a xanthone compound that is major in Gm pericarp. Mangostin is poorly soluble in water (Bumrung et al, 2020). This study revealed that mangostin was only detected in ethanol extract of Gm (Fig.…”

Nanoformulations of α-Mangostin for Cancer Drug Delivery System

“…α-mangostin (Figure 3) is a metabolite of 1,3,6,7-tetrahydroxy-2,8-di(3-methyl-2-butenyl) xanthones isolated from mangosteen pericarps [23,[40][41][42]. α-mangostin is soluble in methanol and has a water solubility of 2.03 × 10 −4 mg/L at 25 • C (Table 1) [43,44]. The low solubility of α-mangostin in water causes low bioavailability.…”

In Silico Study: Combination of α-Mangostin and Chitosan Conjugated with Trastuzumab against Human Epidermal Growth Factor Receptor 2

“…α-mangostin was known to have anticancer activity through the mechanism of the inhibition of the fatty acid synthase (FAS) and the induction of apoptosis in the cell signaling pathway (FAK, ERK1/2 and AKT) against MCF-7 and MDA-MB-231 cell lines [11]. However, α-mangostin has drawbacks in terms of solubility, as well as selectivity to target cancer cells [12][13][14].…”