• Journal of Life Science
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• v.34 no.4
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• pp.215-226
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• 2024

Aralia continentalis is widely distributed in Far East Asian countries such as Korea, China, and Japan. A. continentalis has traditionally been used as an herbal remedy for various conditions, including analgesia, headache, inflammation, lameness, lumbago, rheumatism, and dental diseases in Korea. Previously, epi-continentalic acid, continentalic acid, and kaurenoic acid as major active biological compounds belonging to the diterpenoid class were identified. To synthesize diterpenoid derivatives with enhanced bioavailability, Fusarium fujikuroi was employed to biotransform diterpenoids due to its known antibacterial activity. This yielded two derivatives of kaurenoic acid, namely 16α-hydroxyent-kauran-2-on-19-oic acid and 2β, 16α-dihydroxy-ent-kauran-19-oic acid, with their chemical structures elucidated via NMR analysis. These derivatives exhibited increased polarity compared to kaur- enoic acid, as evidenced by their retention time on preparative HPLC using the ODS-A column and structural modifications. Evaluation of their antidiabetic activity targeting PTP1B, a negative regulator of the insulin signaling pathway, revealed inhibitory activities of 30.8% and 27.6%, respectively, at a concentration of 4 ㎍/ml. Additionally, both derivatives demonstrated low cytotoxicity, with an IC50 value 18 times higher than kaurenoic acid. Therefore, the augmented water solubility and reduced toxicity of 16α-hydroxy-ent-kauran-2-on-19-oic acid and 2β, 16α-dihydroxy-ent-kauran-19-oic acid, resulting from biotransformation by F. fujikuroi, render them promising candidates for industrial applications.

• Herbal Formula Science
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• v.30 no.4
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• pp.249-257
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• 2022

Objectives : Aquilaria crassna is a traditional herbal medicine, which is used to treat allergies, diabetes, neurological diseases. Recently, Aquilaria crassna extracts have been reported in anti-bacterial and anti-inflammatory activities. In this study, various solvents fraction of Aquilaria crassna were investigated on various physiological activities. Methods : According to the polarity, the solvents fraction of Aquilaria crassna were confirmed through TLC, and the activities of the extracts were confirmed in anti-diabetes, anti-obesity, whitening, anti-gout, and anti-inflammation. Results : TLC results showed that ACM and ACM/E have similar patterns and most of the components were transferred to ACM/E. Treatment with ACM and ACM/E fraction were significantly decreased the generation of NO in lipopolysaccharide (LPS)-stimulated macrophage cells. Analysis of biological activities such as α-glucosidase, protein tyrosine phosphatase (PTP1B), tyrosinase, xanthine oxidase (XO) and pancreatic lipase inhibition, showed that ACM and ACM/E have more inhibitory effects than other fractions. Conclusions : Therefore, the results of the present study clearly demonstrate that Aquilaria crassna and its constituents might be beneficial in the prevention or treatment of immune-regulating effects.