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Anti-inflammatory activity and toxicity of the compound K produced by bioconversion

생물전환에 의해 생성된 Compound K의 항염증 및 독성 효과

  • Kim, MooSung (Macrocare Co., Ltd) ;
  • Shin, Hyun Young (Department of Integrated Biomedical and Life Science, Graduate School, Korea University, Transdisciplinary major in Learning Health System) ;
  • Kim, Hyun-Gyeong (Division of Food Science and Biotechnology, KNUT) ;
  • Kang, Ji Sung (Division of Food Science and Biotechnology, KNUT) ;
  • Jung, Kyung-Hwan (Division of Food Science and Biotechnology, KNUT) ;
  • Yu, Kwang-Won (Division of Food Science and Biotechnology, KNUT) ;
  • Moon, Gi-Seong (Division of Food Science and Biotechnology, KNUT) ;
  • Lee, Hyang-Yeol (Division of Food Science and Biotechnology, KNUT)
  • 김무성 (마크로케어) ;
  • 신현영 (고려대학교 대학원 의생명융합과학과 러닝헬스시스템융합전공) ;
  • 김현경 (한국교통대학교 식품생명학부) ;
  • 강지성 (한국교통대학교 식품생명학부) ;
  • 정경환 (한국교통대학교 식품생명학부) ;
  • 유광원 (한국교통대학교 식품생명학부) ;
  • 문기성 (한국교통대학교 식품생명학부) ;
  • 이향렬 (한국교통대학교 식품생명학부)
  • Received : 2021.11.23
  • Accepted : 2021.12.15
  • Published : 2021.12.30

Abstract

Compound K (20-O-β-(D-glucopyranosyl)-20(S)-protopanaxadiol) is an active ingredient of ginsenosides. Compound K has been known to produce from biotransformation by β-glucosidase action of human intestinal microbes after oral admistration of ginseng. We have investigated the cytotoxicity of compound K obtained from bio-converted ginseng extract. As a result, compound K showed no significant cytotoxicity in the concentration of 0.001 to 1 ㎍/mL and inhibited the production of TNF-α, MCP-1, IL-6 and NO in RAW 264.7 cells induced by LPS inflamation. In the same concentration, HaCaT cells induced by inflammation with TNF-α and IFN-γ decreased IL-8 production due to compound K treatment. In the brine shrimp lethality assay, the LC50 of compound K was 0.37 mg/mL indicating some toxicity, but the bioconverted product containing 35% compound K showed relatively low toxicity with an LC50 of 0.87 mg/mL. These results suggest that the compound K enriched extract is a potential functional material for acne relief cosmetic products.

Compound K (20-O-β-(D-glucopyranosyl)-20(S)-protopanaxadiol)는 진세노사이드의 활성성분이다. Compound K는 경구 투여 후 Rb1, Rb2 및 Rc가 사람의 장내 미생물의 β-glucosidase에 의해 생물전환 과정을 거쳐 생성된다고 알려져 있다. 본 연구는 생물전환된 인삼농축액에서 얻은 compound K를 이용해 항염증 및 독성을 조사하였다. 세포독성평가 결과, compound K는 0.001~1 ㎍/mL의 농도범위에서 유의적인 세포독성은 나타나지 않았으며, LPS로 염증이 유발된 RAW 264.7 세포에서 TNF-α, MCP-1, IL-6 및 NO의 생성을 억제하는 것으로 확인되었다. 동일 농도범위에서 TNF-α 및 IFN-γ로 염증이 유발된 HaCaT 세포는 compound K의 처리로 인해 IL-8의 생성을 감소시키는 것으로 나타났지만, IL-6의 경우 일부 농도에서 생성을 감소시켰으나, 통계적인 유의성은 나타나지 않았다. Brine shrimp를 이용한 치사율 검정법에서 compound K의 LC50는 0.37mg/mL로 다소의 독성을 함유하고 있는 것으로 나타났으나 compound K가 35% 고함유된 생물전환물은 LC50가 0.87mg/mL로 나타나 상대적으로 낮은 독성을 보였다. 따라서 이 생성물은 향후 여드름 완화용 화장품 개발에 사용할 수 있는 매우 우수한 기능성 소재가 될 수 있을 것으로 기대된다.

Keywords

Acknowledgement

이 논문은 2021년도 정부(교육부)의 재원으로 한국연구재단의 지원을 받아 수행된 기초연구지원사업(No. 2021R1A6A1A03046418)이며, 또한 2021년도 교육부의 재원으로 한국연구재단의 지원을 받아 수행된 지자체-대학 협력기반 지역혁신 사업의 결과입니다(No. 2021RIS001).

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