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Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives.

ABSTRACT: This study investigated the antioxidant activity DPPH, ABTS, and Folin-Ciocalteu methods of betulin (compound 1) and its derivatives (compounds 2-11). Skin permeability and accumulation associated with compounds 1 and 8 were also examined. Identification of the obtained products (compound 2-11) and betulin isolated from plant material was based on the analysis of ¹H- NMR and ¹³C-NMR spectra. The partition coefficient was calculated to determine the lipophilicity of all compounds. In the next stage, the penetration through pig skin and its accumulation in the skin were evaluated of ethanol vehicles containing compound 8 (at a concentration of 0.226 mmol/dm³), which was characterized by the highest antioxidant activity. For comparison, penetration studies of betulin itself were also carried out. Poor solubility and the bioavailability of pure compounds are major constraints in combination therapy. However, we observed that the ethanol vehicle was an enhancer of skin permeation for both the initial betulin and compound 8. The betulin 8 derivative showed increased permeability through biological membranes compared to the parent betulin. The paper presents the transformation of polycyclic compounds to produce novel derivatives with marked antioxidant activities and as valuable intermediates for the pharmaceutical industry. Moreover, the compounds contained in the vehicles, due to their mechanism of action, can have a beneficial effect on the balance between oxidants and antioxidants in the body, minimizing the effects of oxidative stress. The results of this work may contribute to knowledge regarding vehicles with antioxidant potential. The use of vehicles for this type of research is therefore justified.

SUBMITTER: Gunther A

PROVIDER: S-EPMC8201114 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Dermal aging is characterized by states of oxidative stress, chronic inflammation, and abnormal proteolytic degradation due to the action of hydrogen peroxide, superoxide, 5-lipoxygenase, and elastase, respectively. Noteworthy elastase inhibition has previously been reported, and so this study aimed to investigate the ability of Myrsine africana and myrsinoside B to reduce the activity of hydrogen peroxide, superoxide, and 5-lipoxygenase as supplementary mechanisms of action by which M. africana may reduce the appearance of wrinkles. The use of maltose microneedles were also investigated as a means to enhance the delivery of myrsinoside B into the skin as this is a crucial aspect to investigate when characterizing the efficacy of an active ingredient. Myrsine africana has traditionally been used for skin allergies, boils, and to purify blood (as an astringent) and was selected for this study based on it use in skincare. The crude extract exhibited IC50's of 56.08 ± 2.88 and 132.74 ± 1.64 µg/ml against the hydrogen peroxide and superoxide radicals, while myrsinoside B exhibited IC50's of 52.19 ± 4.16 and 192.14 ± 3.52 µg/ml, respectively. The IC50 of the extract and compound against 5-lipoxygenase was 29.65 ± 2.92 and 29.33 ± 3.08 µg/ml, respectively. No toxicity was observed in vitro at the highest concentration tested. Microneedle treatment increased the permeation of the active through the skin after 24 h to 12.46 ± 5.14 µg/cm2 compared to the passive group (1.30± 0.85 µg/cm2). The amount of active retained in the epidermis and dermis was 8.97 ± 0.90 and 6.98 ± 0.73 µg/cm2 respectively, greater than the retention observed in the passive group (3.24 ± 1.41 and 3.27 ± 1.47 µg/cm2, respectively). M. africana and myrsinoside B showed promising antioxidant and anti-inflammatory activity thus supporting the potential of M. africana and myrsinoside B as anti-wrinkle agents. Further, treatment of dermatomed human skin with maltose microneedles facilitated topical delivery of myrsinoside B and provided an effective means for compound delivery to ensure maximum effect.

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Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives.

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