구조활성상관(QSAR)에 의한 피마엽(？麻葉) 추출물의 HIV-1 효소억제활성인자 예측
Inhibitory Effects of Ricinus communis on HIV-1 Essential Enzymes in vitro and Prediction of Inhibitory Factor Using QSAR in silico
1
조회
0
다운로드
1
인용
0
참고문헌
초록
Abstract
Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Ricinus communis were tested for their inhibitory effects on essential enzymes reverse transcriptase (RT), protease and alpha-glucosidase. Inhibition activity of major compounds of Ricinus communis were predicted from quantitative structure activity relationships (QSAR) in silico.Methods and Results : In the anti-HIV-1 RT using enzyme-linked oligonucleotide sorbent assay (ELOSA) method, water and methanol extracts (100ug/ml) of Ricinus communis showed strong activity of 94.2% and 82.7%, respectively. In the HIV-1 protease and alpha-glucosidase inhibition assay, neither water nor methanol extracts of Ricinus communis inhibited the activity of the enzyme to cleave any substrates as oligopeptides and oligosaccharides.Conclusions : We found that for these samples it is possible that the inhibition of the RT in vitro is due to the secondary metabolites of Ricinus communis such as ricinine and quercetin. It would beof great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agents up to date are RT inhibitors.
참고문헌 (17)
- "Natural product based anti HIV drug discovery and development facilitated by the NCI developmental therapeutics program", 64(2), pp.265~277 (2001)
- "Hattori Human Immunodeficiency Virus Type Ⅰ에 대한 수종 식물 추출물의 억제활성 검색", 29(4), pp.338~346 (1998)
- acridine marine alkaloids,
- "Inhibition of human immunodeficiency viral replication by tannins and related compounds", hata, pp.91~103 (1992)
- "Screening of various plant extracts used in ayurvedic medicine for inhibitory effects on human immunodeficiency virus type 1 HIV1 protease", 9, pp.180~184 (1995)
- "and flavonoids from Ricinus communis Journal of Natural Products" (1985)
- "Cellular distribution of HIV type Ⅰ nef protein Identification of domains in nef required for association with membrane and detergent-insoluble cellular matrix", pp.1003~10 (1994), Kaminchik
- "Mechanism of DNA strand transfer reactions catalyzed by HIV-1 reversetranscriptase", pp.1112~8 (1992)
- "Linker insertion mutagenesis of human immunodeficiency virus reversetranscriptase expressed in bacteria definition of the minimal polymerase domain", pp.3104~8 (1989)
- "Inhibition of alpha-glucosidase I of the glycoprotein-processing enzymes by 6-O-butanoyl castanospermine and its consequences in human immunodeficiency virus-infected T cells", pp.1780~28 1787 (1994)
- "Anti-AIDS drug development:challenges and strategies", 9(6), pp.703~14 (1992)
- "Inhibitory effect of tannins on reverse transcriptase from RNA tumor virus Journal of Natural Products", pp.614~21 (1985)
- "The V3 region of the envelope glycoprotein of human immunodeficiency virus type 1 binds sulfated polysaccharides and CD4-derived synthetic peptides Journal of Biological Chemistry", pp.6664~71 (1992)
- "The mannose-specific plants lectins from Cymvidium hybrid and Epipactis helleborine and the n-specific plant lectin from Urtica dioica are potent and selective inhibitors of human immunodeficiency virus and cytomegalovirus replication in vitro"
- "Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells", pp.3564~8 (1994)
- "Antiviral agents targeted to interact with viral capsid proteins and a possible application to human immunodeficiency virus", pp.4625~7 (1988)
- "Effects of flavonoids and alkaloids on reverse transcriptase", pp.240~54