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황기, 지치 복합물의 연골세포에서의 Matrix Metalloproteinases 저해 효과 및 유효성분의 분석

Inhibitory Effect of Mixed Extracts Obtained from Astragali Radix and Lithospermi Radix on Matrix Metalloproteinases in IL-1β-induced SW1353 Cells and Quantitative Analysis of Active Compound

한국약용작물학회지 2019년 27권 4호 p.247 ~ 258
최두진 ( Choi Doo-Jin ) - 농촌진흥청 국립원예특작과학원 인삼특작부

최보람 ( Choi Bo-Ram ) - 농촌진흥청 국립원예특작과학원 인삼특작부
이대영 ( Lee Dae-Young ) - 농촌진흥청 국립원예특작과학원 인삼특작부
 ( Choi Soo-Im ) - 덕성여자대학교 식물자원연구소
이영섭 ( Lee Young-Seob ) - 농촌진흥청 국립원예특작과학원 인삼특작부
김금숙 ( Kim Geum-Soog ) - 농촌진흥청 국립원예특작과학원 인삼특작부

Abstract


Background: Astragali radix (A) and Lithospermi radix (L) have long been used as traditional medicines due to their known antiinflammatory effects. This study aimed at evaluating, their optimal mixing ratio and their functional compounds by investigating the inhibitory effects of mixed extracts of A and L and their active compounds on matrix metalloproteinases (MMPs).

Methods and Results: A and L extracts were obtained by extraction at 80℃ using 50% and 70% fermented alcohol, respectively, and then mixed at a ratio of 5 : 5, 6 : 4, 7 : 3 and 8 : 2 (w/w). The activities of MMP-1, MMP-3, and MMP-13 were evaluated in interleukin-1beta (IL-1β)-induced SW1353 cells. The extract mixtures showed synergistic inhibitory effects on MMP-3 and MMP13, higher than the effects of the individual A and L extracts. The 7 : 3 mixture (ALM16) showed the most effective MMPs inhibitory activity, while among the active ingredients, calycosin-7-O-β-D-glucoside and lithospermic acid exhibited excellent MMPs inhibitory activity. Additionally, an HPLC method was established for simultaneous quantification of the effective components of the extract mixtures, and validated by measuring the linearity, precision and accuracy of the limit of detection (LOD) and limit of quantification (LOQ).

Conclusions: ALM16 showed the most effective MMPs inhibitory activity. Calycosin-O-β-D-glucoside, calycosin and lithospermic acid were identified as useful candidates, as they were the major functional compounds in the MMP inhibitory activity. Summarily, ALM16 might be a highly effective in osteoarthritis management, owing to its because it exhibits a protective effect on cartilage via excellent inhibition of MMPs.

키워드

Astragali Radix; Lithospermi Radix; Matix Metalloproteinases (MMPs)
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