A New Flavonol Glycoside Gallate Ester from Acer okamotoanum and Its Inhibitory Activity against Human Immunodeficiency Virus-1 (HIV-1) Integrase

Abstract

Bioassay-directed chromatographic fractionation of an ethyl acetate extract of the leaves of Acer okamotoanum using HIV-1 integrase afforded a new acylated flavonol glycoside, quercetin 3-O-(2",6"-O-digalloyl)-beta-D-galactopyranoside (1), together with six known flavonol glycosides and three known phenolic compounds. The structure of the new compound was determined by spectroscopic methods. The most active compounds were quercetin 3-O-(2"-galloyl)-alpha-L-arabinopyranoside (6) and 1, which exhibited IC50 values of 18.1 +/- 1.3 and 24.2 +/- 6.6 micrograms/mL, respectively, against HIV-1 integrase.

Anti-hyperglycaemic effects of the Japanese red maple Acer pycnanthum and its constituents the ginnalins B and C

“…A. pycnanthum is also used as a folk medicine for eye care [13]. Other pharmacological effects of Acer genus have also been reported [14,15]. However, the phytochemical constituents of A. pycnanthum and their biological activities have not yet been reported.…”

Flavonoids That Mimic Human Ligands from the Whole Plants of Euphorbia lunulata

“…7,9,10) Compounds 1 and 2 showed proliferation activity for BAF/InsR. Stimulation with 1 or 2 was dose-dependent and The proliferative activity for BAF/IL10R was observed in 1, 2, 4 and 5, although the activity of 1 and 2 was weaker than that of 4 and 5.…”

Beauvericin and enniatins H, I and MK1688 are new potent inhibitors of human immunodeficiency virus type-1 integrase

“…9 For the in vitro 3¢-processing reaction, two 20-mer oligonucleotides the sequences of which resemble those of the end of HIV-1 U5-LTR were synthesized at Takara: K16 (U5-LTR, + strand), 5¢-TGTGGAAAATCTCTAG CAGT-3¢; and K17 (U5-LTR, À strand), 5¢-ACTGCTAGAGATTTTCCACA-3¢. Oligonucleotide K16 (15 pmol) was labeled at the 5¢-end using 250 mCi [g-32 P]-ATP (Amersham, Richmond, VA, USA) and 10 units of T4 polynucleotide kinase (New England Biolabs, Beverly, MA, USA) in a 40 ml reaction buffer (70 mM Tris-HCl (pH 7.6), 10 mM MgCl 2 and 5 mM dithiothreitol) for 60 min at 37 1C.…”