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Low molecular weight mannogalactofucans (LMMGFs) prepared by enzymatic degradation of high molecular weight Undaria galactofucan (MF) were evaluated for their anti-cancer effects against human prostate cancer. Correlation NMR and linkage analyses confirmed that LMMGFs consist mainly of α-fucose and β-galactose units: α-fucose units are 1,3-linked; β-galactose units are terminal, 1,3- and/or 1,6-linked; both sugars are partially sulphated, fucose at positions O-2 and/or O-4 and galactose at O-3. Mannose residue, as a minor sugar, presents as the 1,4-linked terminal units. LMMGFs more significantly induced cell cycle arrest at the G0/G1 phase and cell death via suppression of the Akt/GSK-3β/β-catenin pathway than MF in human PC-3 prostate cancer cells. LMMGFs upregulated mRNA expression of death receptor-5 (DR-5), the ratio of Bax to Bcl-2, the cleavage of caspases and PARP, the depolarisation of mitochondrial membrane potential, and ROS generation. LMMGFs (200-400 mg/kg) effectively reduced both tumour volume and size in a xenografted mouse model. These results demonstrated that LMMGFs attenuate the growth of human prostate cancer cells both in vitro and in vivo, suggesting that LMMGFs can be used as a potent functional ingredient in health-beneficial foods or as a therapeutic agent to prevent or treat androgen-independent human prostate cancer. Graphical Abstract.

Glycosylation of natural flavonoids with various sugar moieties can affect their physicochemical and pharmacological properties. In this study, the plant flavonoids quercetin aglycon (Quer) and quercetin 3-O-glucoside (Q3G) were evaluated and compared for their potential anti-obesity effects. The Q3G dose-dependently reduced the TG contents and lipid accumulation in 3T3-L1 adipocyte cells, by 52% and 60% at 20μM, respectively, compared to differentiated control (100%), which were 1.6-fold and 2.4-fold higher reduction than Quer. The Q3G (20μM) also more significantly reduced the expression of adipogenic markers such as C/EBP-β, C/EBP-α, PPAR-γ, and aP2 than Quer, indicating that the Q3G suppresses both adipocyte differentiation and lipogenesis more effectively than Quer in vitro. Comparing to those in the high-fat diet (HFD) fed mice control group for 10 weeks, both the body and liver weights and the size of adipocytes in epididymal adipose tissues were significantly reduced in HFD mice fed with Q3G for another 6 weeks (30mg/kg body weight by oral administration), accompanied by the reductions of TG, total cholesterol, and HDL-cholesterol in serum. The Q3G also reduced the levels of the lipid metabolism-associated proteins, PPAR-γ, SREBP-1c, and FAS in the liver tissues. These results clearly demonstrated that Q3G exhibits a stronger anti-obesity effect than Quer and its anti-obesity effect is mediated via inhibition of adipocyte differentiation and lipogenesis, decreasing serum lipid levels by altering hepatic lipid metabolism, and reducing body weight gain. The results of this study suggest that the Q3G, but not Quer, can be a potent functional ingredient of beneficial health foods or a therapeutic agent to prevent or treat obesity.