Sung Han Kim

Comparative Effect of Gromwell (Lithospermum erythrorhizon) Extract and Borage Oil on Reversing Epidermal Hyperproliferation in Guinea Pigs

To compare the systemic efficacy of borage oil (Borago officinalis: BO) and gromwell (Lithospermum erythrorhizon), two plant species of the Boraginaceae family, epidermal hyperproliferation was induced in guinea pigs by a hydrogenated coconut oil diet for 8 weeks. Subsequently, guinea pigs were fed diets of BO (group HBO), organic extract (group HGO), or water extract (group HGW) of gromwell for 2 weeks. In groups HGO and HGW, proliferation scores and the level of ceramides, the major lipid maintaining epidermal barrier, were similar with those in normal control group BO fed BO diet for 10 weeks. Despite accumulation of 15-hydroxyeicosatrienoic acid (15-HETrE), the potent anti-proliferative metabolite of γ-linolenic acid (GLA: major polyunsaturated fatty acid in BO), the reversal of epidermal hyperproliferation and the ceramide level of group HBO were less than those of groups HGO and HGW. Taken together, our data demonstrate that gromwell is more effective in reversing epidermal hyperproliferation with a marked increase in ceramides.

Oral supplementation of Lithospermum erythrorhizon prevents the development of atopic dermatitis with reducing ceramide degradation in the epidermis of NC/Nga mice.

Lithospermum erythrorhizon Sieb. et Zucc. (LE) is widely used in the treatment of abnormal skin conditions, but its systemic efficacy, especially in atopic dermatitis (AD), is not clear. To examine the systemic efficacy of LE on the clinical manifestation of AD‐like skin lesions, NC/Nga mice, a murine model of AD, were fed a control diet (group CA: atopic control) or a diet with a 70% ethanol extract from 5% LE (group LE) for 10 weeks. In group LE, the clinical manifestation of AD‐like skin lesions was prevented as the level of serum IgE, epidermal hyperproliferation, and the number and duration of scratching episodes, which were greater in group CA, were significantly reduced to a similar level of the normal control group of BALB/c mice (group C). In addition, the level of ceramides, the major lipid maintaining the epidermal barrier, in the epidermis of group LE was increased, and was inversely associated with a decreased protein level of ceramidase, an enzyme of ceramide degradation. However, the mRNA and the protein levels of serine palmitoyl transferase (enzyme for de novo ceramide synthesis) in groups C, CA and LE did not differ. It was demonstrated that oral supplementation with LE extract prevented the development of atopic dermatitis with reducing ceramide degradation coupled with a low expression of ceramidase protein. Copyright

The Effect of Gromwell (Lithospermum erythrorhizon) Extract on the Stratum Corneum Hydration and Ceramides Content in Atopic Dermatitis Patients

BACKGROUND A disruption of the balance between the water content of the stratum corneum (SC) and skin surface lipids may lead to the clinical manifestation of dryness of skin in patients with atopic dermatitis (AD). OBJECTIVE To determine whether supplementation of gromwell (Lithospermum erythrorhizon), one of herbs used in East Asia in remedies for various abnormal skin conditions, may improve the SC level of hydration and ceramides, major lipid in SC in patients with AD. METHODS A total of 28 subjects with AD were randomly assigned into two groups: either gromwell group received dextrose contained capsules with 1.5 g of gromwell extracts or placebo group received only dextrose contained capsules for 10 weeks. RESULTS In contrast to no alteration of SC hydration and ceramides in placebo group, the SC hydration in gromwell group was significantly increased in parallel with an increase of SC ceramides. Furthermore, % increase of SC hydration in gromwell group bore a positive correlation with the clinical severity, which suggests that the increase of SC hydration in gromwell group was more effective as AD was more severe. CONCLUSION Supplementation of gromwell improves SC hydration in parallel with an increase of ceramides in part.

Synthesis of 2′,3′-dideoxyisoguanosine from guanosine

Abstract2′,3′-dideoxyisoguanosine was synthesized from guanosinevia intermediate 6-[(4-methylphenyl)thio]-2-oxo-9-(2′,3′,5′-tri-O-acetyl-β-D-ribofuranosyl)-2,3-dihydropurine (4). The 2-oxo, 6-amino and 5′-hydroxy triprotected isoguanosine derivative was utilized to reduce high polarity and promote poor solubility of intermediates. The protecting groups for oxo and 6-amino were easily removed in reduction of olefin in ribose without additional reaction steps. 2′,3′-Vicinal diol in ribose sugar moiety was transformed to olefin with Bu3SnH by radical reactionvia bisxanthate. Removing 5′-O-TBDMS protecting group gave final product, 2′,3′-dideoxyisoguanosine (12) in a 10% overall yield.