Compounds from rose (Rosa rugosa) flowers with human immunodeficiency virus type 1 reverse transcriptase inhibitory activity.

The aqueous extracts and ethanol precipitates of aqueous extracts of 18 medicinal herbs traditionally used in China were screened for their ability to inhibit human immunodeficiency virus type-1 reverse transcriptase (HIV-1 RT) in-vitro. Among the samples screened at a concentration of 500 μg mL -1 , dried rose (Rosa rugosa) flowers showed the strongest inhibition. The ethanol precipitate of the aqueous extract of R. rugosa was processed and two components (P 1 and P 2 ) were obtained after ion exchange chromatography on DEAE-cellulose. Then, P 1-a (Mr 150kDa) and P 1-b (Mr 8 kDa) were isolated from P 1 by gel filtration on Sephadex G-200. They inhibited the activity of HIV-1 RT with an IC50 of 158nM and 148.16μg mL -1 (18.5 μM ), respectively. Further structural analyses revealed that P 1-a was a polysaccharide-peptide complex, and P 1-b was a polymer consisting of acteoside and acteoside derivatives identified by Fourier transform infrared spectroscopy, nuclear magnetic resonance, assays of carbohydrate and protein contents and high-performance liquid chromatography electrospray ionization mass spectrometry.