The Role of Fructose in Public Health and Obesity

We are in the so-called nutritional transition, in which obesity and its comorbidities have emerged as an important research topic, and the information on food composition is fundamental to promote nutritional safety. Fructose is the sweetest carbohydrate, and this sweetness, along with its low cost, is the key factor for its use in commercial drinks and sweets. The global average consumption of fructose per capita has increased from 56 g/day in 1986 to 65 g/day in 2007. Experimental models associate high fructose intake with the development of obesity and induced insulin resistance. In recent studies, diabetic patients have been reported to use fructose more frequently than glucose. Fructose acts differently in the hypothalamus and generates less satiety than glucose;thus, fructose has a high lipogenic potential. Replacing fructose with another isocaloric carbohydrate is associated with better glycemic control.

Gracilaria fisheri oligosaccharides ameliorate inflammation and colonic epithelial barrier dysfunction in mice with acetic acid-induced colitis

Objective:To investigate the effect of Gracilaria fisheri oligosaccharides(GFO)on inflammation and colonic epithelial barrier dysfunction in colitis mice.Methods:The animals were treated by oral gavage with distilled water,1000 mg/kg inulin,100,500,or 1000 mg/kg GFO for 14 d,or treated with 50 mg/kg mesalamine for 5 d after colitis induction(on day 10).Histopathology,inflammatory cytokines,colonic permeability,and tight junction proteins were investigated by hematoxylin and eosin staining,immunohistochemical staining,Ussing chamber technique,and Western blotting assays,respectively.Results:GFO ameliorated histological damage in colitis mice when compared to untreated colitis mice.Treatments with 100,500,and 1000 mg/kg GFO reduced TNF-αexpression,while IL-1βwas significantly reduced in colitis mice treated with 500 and 1000 mg/kg.Compared to untreated colitis mice,GFO increased transepithelial electrical resistance,reduced fluorescein isothiocyanate-dextran paracellular flux,and modulated tight junction proteins(occludin and claudin 2)in colitis mice.Conclusions:GFO has anti-inflammatory activity and could modulate colonic epithelial barrier dysfunction in acetic acid-induced colitis mice.Furthermore,GFO could modulate the expression of tight junction proteins that play important roles in colonic barrier function.

Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidinesubstituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs

In this report,a series of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket(NNIBP)by incorporating an aromatic moiety to the left wing of the lead K-5 a2.The newly synthesized compounds were evaluated for anti-HIV potency in MT-4 cells and inhibitory activity to HIV-1 reverse transcriptase(RT).Most of the synthesized compounds exhibited broad-spectrum activity toward wild-type and a wide range of HIV-1 strains carrying single non-nucleoside reverse transcriptase inhibitors(NNRTI)-resistant mutations.Especially,compound 26 exhibited the most potent activity against wild-type and a panel of single mutations(L1001,K103 N,Y181 C,Y188 L and E138 K)with an EC50 ranging from 6.02 to 23.9 nmol/L,which were comparable to those of etravirine(ETR).Moreover,the RT inhibition activity,preliminary structure-activity relationship and molecular docking were also investigated.Furthermore,26 exhibited favorable pharmacokinetics(PK)profiles and with a bioavailability of 33.8%.Taken together,the results could provide valuable insights for further optimization and compound 26 holds great promise as a potential drug candidate for the treatment of HIV-1 infection.