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Evaluation of cyclooxygenase (COX) inhibition in rosemary extract

로즈마리 추출물의 cyclooxygenase (COX) 효소 및 유전자 발현에 미치는 영향

  • Sehee Lee (Department of Food Science and Technology, Seoul National University of Science and Technology) ;
  • Soo-yeon Park (Department of Food Science and Technology, Seoul National University of Science and Technology) ;
  • Kyeong Jin Kim (Department of Nano Bio Engineering, Seoul National University of Science and Technology) ;
  • Sonwoo Kim (CJ CheilJedang Food & Nutrition Tech) ;
  • Yanghoon P. Jung (CJ CheilJedang Food & Nutrition Tech) ;
  • Ji Yeon Kim (Department of Food Science and Technology, Seoul National University of Science and Technology)
  • Received : 2023.01.31
  • Accepted : 2023.03.10
  • Published : 2023.12.31

Abstract

Selective cyclooxygenase (COX)-2 inhibition is a novel strategy to reduce the risk of gastrointestinal side effects caused by conventional nonsteroidal anti-inflammatory drugs. However, some selective COX-2 inhibitors have become apparent to increase the risk of severe cardiovascular disease. The aim of this study was to examine the anti-inflammatory effect of rosemary extract (RE) and confirm the safety of cardiovascular side effects. Inhibition of COX enzyme activity was assessed, and the levels of COX-2 and prostaglandin E2 (PGE2) and COX-1 and thromboxane B2 (TXB2) were evaluated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. The 40% RE group showed increased COX-2 inhibition activity in a dose-dependent manner, whereas the 50% RE group only exhibited at 100 ㎍/mL. In a cell-based study, COX-2 mRNA expression was similar in both RE groups and PGE2 levels tended to decrease in the 40% RE group compared to the LPS group in the LPS pretreatment condition. In the LPS posttreatment condition, the COX-2 mRNA expression decreased in the 40% RE group, and PGE2 levels were increased in the 40 and 50% RE groups. In both conditions, there was no significant difference in COX-1 and TXB2 levels. In conclusion, 40 and 50% RE showed significant COX-2 inhibition, similar to the positive control group. It was confirmed that the inhibition of the COX-2 expression, but the effect did not affect the balance between prostacyclin and TXB2. These results indicate that rosemary showed COX-2 inhibition activity with a low risk of cardiovascular diseases.

선택적 cyclooxygenase (COX)-2 억제제는 기존의 비스테로이드성 소염제의 위장 부작용을 줄일 수 있는 새로운 대체제이다. 하지만, 최근 혈전을 일으켜 심혈관 질환의 위험을 증가시킨다는 보고가 있다. 따라서 본 연구에서는 유효성분인 ursolic acid를 각각 40, 50%로 극대화한 로즈마리 추출물(RE)의 항염증 효과와 이에 따른 심혈관 부작용의 안전성을 확인하였다. RE의 COX 효소 활성 저해 평가 결과 40, 50% RE는 100 ㎍/mL에서 양성 대조군인 celecoxib 및 rofecoxib와 비슷한 COX-2 저해 활성을 보였고, COX-1 저해 활성은 미미하였다. 이후 Lipopoly-saccharide (LPS)를 조건에 따라 처리한 RAW 264.7 세포에 40, 50% RE 1 ㎍/mL를 처리하여 COX-2, COX-1 유전자 발현, 세포 배양액의 prostaglandin E2 (PGE2), thromboxane B2 (TXB2) 농도를 확인하였다. 실험 결과 COX-2 유전자 발현은 40% RE가 LPS를 24시간 후처리한 조건에서 감소하였고, 40, 50% RE는 COX-1 유전자 발현 및 PGE2, TXB2 농도에는 유의한 영향을 주지 않는 것으로 확인되었다. 따라서 RE는 혈전 생성에 관여하는 prostaglandins의 균형에 영향을 주지 않아 심혈관 혈전 생성의 위험성이 적을 것으로 사료된다.

Keywords

Acknowledgement

본 연구는 CJ제일제당의 지원을 받아 수행되었으며 이에 감사드립니다.

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