꽃치자나무 추출물의 HIV-1 효소 억제 활성과 QSAR에 의한 활성인자 예측

Inhibitory Effects of Gardenia jasminoides var. radicans Makino on HIV-1 Enzymes and Prediction of Inhibitory Factor by QSAR

꽃치자나무 추출물의 HIV-1 reverse transcriptase, protease 및 alpha-glucosidase 에 대한 억제활성실험을 실시하였다. ELOSA 방법으로 실험한 역전사효소 억제활성 실험에서는 꽃치자나무 잎 MeOH 추출물 100 ㎍ /ml 농도에서 13.4% 의 약한 억제활성이 관찰되었고, 줄기의 메탄올추출물에서는 32.5% 의높은 HIV-1 protease 억제활성과 줄기의 메탄올 추출물에서는26.1% 의 alpha-glucosidase 억제활성이 관찰되었다. 그리고 HIV-1 복제 억제활성은 MT-4 세포에 대한 HIV-1 유도 세포변성억제를 광학현미경으로 관찰하여 살펴본 결과 잎과 줄기의 모든 추출물에서 HIV-1 바이러스 증식억제에 억제활성이 관찰되지 않았다. In silico 실험결과 주요성분인 crocetin 이 81.8% 의 높은 역전사 효소활성이 예측되었으며, genipin 이 55.39%, geniposidic acid aglycone이 64.5% 역전사효소 활성이 예측되었다. 주로 aglycone 의 활성이 높게 예측되었으며 배당체의 경우 활성이 현저하게 저하되는 것으로 나타났다.

In this study, we conducted the anti- HIV-1 enzymes assay in vitro and its active components were predicted by QSAR in silico for the elucidation of action mechanism on anti-HIV of natural resources. The extracts of Gardenia jasminoides var. radicans Makino were tested for their inhibitory effects on the reverse transcriptase (RT), protease and α- glucosidase. In the enzyme inhibition assay, the methanol extracts of Gardenia jasminoides var. radicans Makino stem showed a strong activity of 32.5% on the enzyme activity to cleave an oligopeptide, resembling one of the cleavage sites in the viral polyprotein which can only be processed by HIV-1 protease. Moreover the methanol extracts of stem exhibited alpha-glucosidase inhibitory activities of 26.1%. The methanol extracts (100 μ g/ml) of stem showed a weak activity of 13.4% on anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method. However, all extracts of leaf and stem didn’t exhibit the HIV-1-induced cytopathic effects with IC (inhibitory concentration) of 100 μ g/ml in HIV-1-infected human T-cell line. From these results, it is suggested that Gardenia jasminoides var. radicans Makino extracts may possibly be involved in the inhibition of reverse transcriptase, protease and alpha-glucosidase but can’t vitally concerned with the viral replication in vitro.