Purification Of Inhibitors Against HIV-1 Reverse Transcriptase And Protease From Edible Mushrooms

Acquired Immunodeficiency Syndrome (AIDS) is a deadly pandemic disease caused by a retrovirus known as human immunodeficiency virus type 1(HIV-1). Reverse transcriptase (RT), protease (PR), and integrase (IN) are three essential enzymes to the life cycle of the HIV. The chemotherapeutic strategies have been directed at the development of inhibitors of these HIV enzymes. One of the major obstacles to the long-term treatment of AIDS is the remarkable mutation of HIV to most, if not all, of clinically used chemotherapeutic agents. Therefore, it is an ongoing need for new, structurally diverse anti-HIV agents, which are less toxic and affordable to all AIDS patients. In this study, we firstly screened the ethanol extracts from edible mushrooms on inhibition of HIV-1 RT activity. Among the mushroom ethanol extracts examined, the extract of Poria cocos exhibited over 97.4% inhibition at Img/ml. Then this crude ethanol extract was fractionated through DEAE-cellulose anion-exchange chromatography, CM-cellulose cation-exchange chromatography, and FPLC Superdex 75 gel filtration respectively, which result in the isolation of an active polysaccharide-peptide with five amino acids of AENGG in N-terminal, named SI 2. On the other hand, we also examined these extracts' inhibitory effects on HIV-1 PR. The results showed that Lactarius camphorates, which could inhibit HIV-1 PR by 80.9%, was the only sample exhibited over 80% inhibition on PR at 0.5mg/ml.