루파리엘롤라이드 유도체의 분리,합성과 항균효과 평가

Title
루파리엘롤라이드 유도체의 분리,합성과 항균효과 평가
Alternative Title
Isolation and synthesis of luffariellolide derivatives and evaluation of anti-bacterial activities against Gram-nagative bateria
Author(s)
이지훈; 신아영; 이희승
KIOST Author(s)
Lee, Jihoon(이지훈)Shin, A Young(신아영)Lee, Hyi Seung(이희승)
Publication Year
2018-08-19
Abstract
Luffariellolide, an anti-inflammatory sesterterpene, was originally isolated as a major metabolite from the hexane extract of the Palauan sponge Luffariella variabilis. Initially, luffariellolide has been reported to exhibit reversible inhibitory activity against phospholipase A (PLA ), which is a mediator for inflammation.

During the course of our research to identify marine invertebrates producing pharmacologically useful metabolites, luffariellolide was isolated from the marine sponge Suberea sp., which was collected offshore of the Philippines. Chemical diversification on the g-hydroxylbutenolide core of luffariellolide revealed that pyridazinone-type derivatives can enhance the antimicrobial activity toward K. pneumonia up to 32 times (MIC = 0.002 mg/mL), compared to that of the natural product (MIC > 0.064 mg/mL). Also, N-pyridinyl pyridazinone analogue exhibited selective anti-cancer activity against A375SM with an EC50 value of 0.0063 mM/mL (luffariellolide, EC50 = 0.024 mg/mL), while luffariellolide showed non-selective cytotoxicity against most of cancer cell lines.bitory activity against phospholipase A (PLA ), which is a mediator for inflammation.

During the course of our research to identify marine invertebrates producing pharmacologically useful metabolites, luffariellolide was isolated from the marine sponge Suberea sp., which was collected offshore of the Philippines. Chemical diversification on the g-hydroxylbutenolide core of luffariellolide revealed that pyridazinone-type derivatives can enhance the antimicrobial activity toward K. pneumonia up to 32 times (MIC = 0.002 mg/mL), compared to that of the natural product (MIC > 0.064 mg/mL). Also, N-pyridinyl pyridazinone analogue exhibited selective anti-cancer activity against A375SM with an EC50 value of 0.0063 mM/mL (luffariellolide, EC50 = 0.024 mg/mL), while luffariellolide showed non-selective cytotoxicity against most of cancer cell lines.
URI
https://sciwatch.kiost.ac.kr/handle/2020.kiost/23165
Bibliographic Citation
American Chemical Society 256th National Meeting, pp.1, 2018
Publisher
American Chemical Society
Type
Conference
Language
English
Publisher
American Chemical Society
Related Researcher
Research Interests

Marine Natural Products,Organic Chemistry,해양천연물,유기화학

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