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Fucoidan and deep-sea water (DSW) are attractive marine resources for treating type 2 diabetes (T2DM). In this study, the regulation and mechanism associated with the co-administration of the two were first studied using T2DM rats, induced by a high fat diet (HFD) and streptozocin (STZ) injection. Results demonstrate that, compared to those with DSW or FPS alone, the orally administered combination of DSW and FPS (CDF), especially the high dose (H-CDF), could preferably inhibit weight loss, decrease levels of fasting blood glucose (FBG) and lipids, and improve hepatopancreatic pathology and the abnormal Akt/GSK-3β signaling pathway. The fecal metabolomics data show that H-CDF could regulate the abnormal levels of metabolites mainly through the regulation of linoleic acid (LA) metabolism, bile acid (BA) metabolism, and other related pathways. Moreover, H-CDF could adjust the diversity and richness of bacterial flora and enrich bacterial groups, such as Lactobacillaceae and Ruminococcaceae UCG-014. In addition, Spearman correlation analysis illustrated that the interaction between the gut microbiota and BAs plays an essential role in the action of H-CDF. In the ileum, H-CDF was verified to inhibit activation of the farnesoid X receptor (FXR)–fibroblast growth factor 15 (FGF15) pathway, which is regulated by the microbiota–BA–axis. In conclusion, H-CDF enriched Lactobacillaceae and Ruminococcaceae UCG-014, thereby changing BA metabolism, linoleic acid metabolism, and other related pathways, as well as enhancing insulin sensitivity and improving glucose and lipid metabolism. [ABSTRACT FROM AUTHOR]

One rare diterpenoid which was an unusual phorbol derivative possessing a 5-ene-7-oxo functional group, wallichiioid A (1), and 17 known compounds (2–18) were isolated from the aerial parts of Euphorbia wallichii. The structures and relative configuration of these compounds were elucidated on the basis of extensive spectroscopic interpretation. All the known compounds were isolated from E. wallichii for the first time. Diterpenoids 1–5 were tested for their cytotoxicity against five cancer cell lines (A-549, MCF-7, Hep G2, HeLa, and P388) and showed IC50 values in the range of 8.19–29.72 μg/mL. The antiangiogenic activities of diterpenoids 1–5 were also evaluated using a zebrafish model. [ABSTRACT FROM AUTHOR]

Three new prenylated flavonoids, macarindicins A–C ( 1–3 ), as well as seven known compounds ( 4–10 ) were isolated from the twigs of Macaranga indica . Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 2 and 3 enriched the diversity of prenyl moiety in genus Macaranga especially in the aspect of various lengths of prenyl chain. All the known compounds were isolated from M. indica for the first time and this plant was found to contain large number of ellagic acid. Compounds 1–10 were tested for their cytotoxicity against four cancer cell lines (MCF-7, Hep G2, Hela and P388) and showed IC 50 values in the range of 2.61–20.35 μ g/mL. [ABSTRACT FROM AUTHOR]

The in vitro metabolism of two novel phosphate prodrugs of glycyrrhetic acid (GA) was studied by the method of incubation in the rat liver microsome and the in vivo plasma pharmacokinetics after injecting intravenously (i.v.) into six rats was investigated, respectively. The prodrugs diminished gradually with time and most of the parent drugs were released in 30 min in vitro. In this paper, the in vivo plasma concentration data were analyzed by compartmental modeling. Both the prodrugs and the corresponding released parent drugs could be described by a two-compartment model, which existed for 48 h in rats. The t1/2 increases remarkably after i.v. administration to rats when compared with injecting the parent drugs directly. [ABSTRACT FROM AUTHOR]

Two new neo-clerodane diterpenoid alkaloids, scutebarbatine O (1) and 6-O-nicotinoylscutebarbatine G (2), were isolated from the whole plant of Scutellaria barbata. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR analyses. In vitro, compounds 1 and 2 showed cytotoxic activities against three human tumor cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 2.1-5.7 μM. [ABSTRACT FROM AUTHOR]

One rare flavonoid–diterpene heterodimer, denticulatain C ( 1 ), one modified geranyl-type side chain substituted flavonoid, denticulatain D ( 2 ) and one geranylated flavonoid, denticulatain E ( 3 ), as well as 11 known compounds ( 4 – 14 ) were isolated from the fronds of Macaranga denticulata . Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 4 and 8 inhibited the proliferation of A-549 cell line with IC 50 values of 48.6 and 20.2 μ g/mL, respectively. Compounds 3 , 6 , and 8 exhibited significant antiangiogenic activity on a zebrafish model with IC 50 values of 9.78, 0.34, and 2.55 μ g/mL, respectively. [ABSTRACT FROM AUTHOR]

One unique prenylated bibenzyl, kurzphenol A ( 1 ), two new prenylated flavonoids, kurzphenols B and C ( 2 and 3 ), as well as fourteen known compounds ( 4 – 17 ) were isolated from the twigs of Macaranga kurzii . Compound 1 was the first example of prenylated bibenzyl which possesses a benzofuran ring. All the known compounds were isolated from M. kurzii for the first time. Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 1 – 17 were tested for their cytotoxicity against A-549 and Hep G2 cancer cell lines and showed IC 50 values in the range of 9.76–30.14 μ g/mL. [ABSTRACT FROM AUTHOR]

Background: There is an urgent need for a vaccine that is effective against the 2009 pandemic influenza A (H1N1) virus. Methods: A split-virus, inactivated candidate vaccine against the 2009 H1N1 virus was manufactured, and we evaluated its safety and immunogenicity in a randomized clinical trial. Subjects were between 3 and 77 years of age, stratified into four age groups. The immunization schedule consisted of two vaccinations, 21 days apart. Subjects were injected with placebo or with vaccine, with or without alum adjuvant, at doses of 7.5 μg, 15 μg, or 30 μg. Serologic analysis was performed at baseline and on days 21 and 35. Results: A total of 2200 subjects received one dose, and 2103 (95.6%) received the second dose, of vaccine or placebo. No severe adverse side effects associated with the vaccine were noted. In the nonadjuvanted-vaccine groups, injection-site or systemic reactions, most mild in nature, were noted in 5.5 to 15.9% of subjects. Among the subjects receiving 15 μg of nonadjuvanted vaccine, a hemagglutination-inhibition titer of 1:40 or more was achieved by day 21 in 74.5% of subjects between 3 and 11 years of age, 97.1% of subjects between 12 and 17 years, 97.1% of subjects between 18 and 60 years, and 79.1% of subjects 61 years of age or older; by day 35, the titer had been achieved in 98.1%, 100%, 97.1%, and 93.3% of subjects, respectively. The proportion with a titer of 1:40 or more was generally highest among the subjects receiving 30 μg of vaccine, with or without adjuvant. Vaccine without adjuvant was associated with fewer local reactions and greater immune responses than was vaccine with adjuvant. Conclusions: These data suggest that a single dose of 15 μg of hemagglutinin antigen without alum adjuvant induces a typically protective immune response in the majority of subjects between 12 and 60 years of age. Lesser immune responses were seen after a single dose of vaccine in younger and older subjects. (ClinicalTrials.gov number, NCT00975572.) N Engl J Med 2009;361:2414-23. [ABSTRACT FROM AUTHOR]

A new binuclear zinc(II) complex bridged by μ-oxalate, and end-capped with 2,2'-bipyridine (bpy), [Zn2(ox)(bpy)4](ClO4)2 · H2O, has been synthesized and characterized by elemental analyses, molar conductance, IR, and electronic spectra and single-crystal X-ray diffraction. The single-crystal X-ray analysis reveals that the [Zn2(ox)(bpy)4]2+ cation has two zinc(II) centers bridged by a planar bis(bidentate) oxalate group with Zn···Zn distance of 5.482(3) Å; each zinc(II) is in a distorted octahedral environment. The crystal structure is stabilized by non-classical C-H···O hydrogen bonds and π-π stacking interactions to form a 3-D supramolecular structure. The interaction of the complex with calf-thymus DNA (CT-DNA) was explored by using electronic and fluorescence spectra and viscosity measurements. The results reveal that the complex intercalates with CT-DNA with intrinsic binding constant of 4.1 × 104 M-1. [ABSTRACT FROM AUTHOR]