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다래나무 추출물의 HIV-1 효소억제활성과 구조활성상관(QSAR)예측
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  • 다래나무 추출물의 HIV-1 효소억제활성과 구조활성상관(QSAR)예측
저자명
유영법,Yu. Young-Beob
간행물명
大韓本草學會誌
권/호정보
2006년|21권 4호|pp.115-121 (7 pages)
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Actinidia arguta were tested for their inhibitory effects on essential enzymes as the reverse transcriptase (RT), protease and ${alpha}-;glucosidase$. And we predicted inhibition activity of major compounds of Actinidia arguta using Quantitative Structure Activity Relationships (QSAR). Methods : In this assay the activity of HIV-1 reverse transcriptase is measured as the formation of a strand of copy-DNA (cDNA) using RNA as a template. The activity of HIV-1 protease is measured as the cleavage of an oligopeptide by HIV-1 protease. Results : In the anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method, water extracts (100ug/ml) of stem and leaf showed strong activity of 93.9% and 91.9%, respectively. In the HIV-1 protease inhibition assay, aqueous stem extract inhibited the activity of the enzyme to cleave an oligopeptide, resembling one of the cleavage sites in the viral polyprotein which can only be processed by HIV-1 protease with 56.8%. In the ${alpha}-glucosidase$ inhibition assay, aqueous stem extract showed activity of 73.1%. Conclusion : We found out this result, for these samples it is possible that the inhibition of the viral replication in vitro is due to the inhibition at least one of RT and ${alpha}-glucosidase$. It would be of great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agent up to date are RT, PR and ${alpha}-glucosidase$ inhibitors.