A new naphthalene glycoside from Chimaphila umbellata inhibits the RANKL-stimulated osteoclast differentiation.

A new naphthalene glycoside was isolated from the leaves and stems of Chimaphila umbellata Barton. Its chemical structure was elucidated to be 2,7-dimethyl-1,4-dihydroxynaphthalene-1-O-ß-D-glucopyranoside (DMDHNG), based on spectroscopic evidence. DMDHNG significantly inhibited the receptor activator of nuclear factor-κB ligand (RANKL)-induced tartrate-resistant acid phosphatase (TRAP) activity and the formation of multinucleated osteoclasts in a dose-dependent manner. In addition, the new glycoside inhibited the RANKL-induced mRNA expression of osteoclast-associated genes that encode TRAP, cathepsin K, and another transcription factor-nuclear factor of activated T-cells c1. We believe that the inhibitory effects of DMDHNG on the osteoclast differentiation may be exploited for a therapeutic benefit.

Rapid identification and characterization of antioxidants from Ligularia fischeri.

The objectives of this study were to investigate the radical-scavenging activity of Ligularia fischeri on oxidative damage by the radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) and to rapidly identify the active components using the bioassay-linked fractionation method. The MeOH extract and fractions of CH(2)Cl(2), BuOH, and H(2)O from L. fischeri showed DPPH radical-scavenging effects in a dose-dependent manner (p < 0.01). In particular, the BuOH fraction had the most effective (p < 0.05) antioxidative capacity. The active constituents from the BuOH fraction of L. fischeri were rapidly isolated by bioassay-linked HPLC method and identified as hyperoside and 2''-acetylhyperoside with potent antioxidant effects against the DPPH radical, with IC(50) values of 1.31 and 7.09 microg/mL, respectively. They have not been reported from L. fischeri yet.

[Study on antioxidant activity of constituents from mulberry leaf].

OBJECTIVE: To study the chemical constituents with antioxidant activity from mulberry leaf. METHODS: Siliga gel column chromatography was used to isolate, and their structures were identified by spectras. METHODS: Isolated constituents were tested in vitro for antioxidant activity against 1, 1-diphenyl -2-picrylhydrazyl (DPPH) and 2, 2' -azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS+) radicals. RESULTS: Four known flavonoids were isolated from mulberry leaf and their structures were identified as kaempferol-3-O-beta-D-glucopyranoside (I), quercetin-3-O-beta-D-glucopyranoside (II), quercitrin (III), morin-3-O-beta-D-glucopyranoside (IV). All these compounds showed DPPH and ABTS+ radicals scavenging activity. CONCLUSION: Compound IV has the strongest ABTS+ radicals scavenging effects.

Pharmacokinetics and pharmacodynamics of sterylglucoside-modified liposomes for levonorgestrel delivery via nasal route.

For emergency contraceptive, the rapid delivery of levonorgestrel (LNG) to plasma is desirable, furthermore, a sustained delivery of LNG along with rapid absorption will be necessary. The pharmacokinetics and pharmacodynamics of LNG entrapped in different kinds of liposome formulations via nasal administration in rats were evaluated and compared with LNG suspension via the oral route. The relative bioavailabilities of these liposome formulations via nasal administration were 100% or higher than 100%. The Cmax and Tmax values of sterylglucoside (SG) and chitosan-contained formulations by nasal administration were 416.84 ng/mL and 1.02 hr, 227.97 ng/mL and 2.02 hr, respectively, compared with that of 334.94 ng/mL and 1.89 hr of oral suspension. Fully 100% contraception was observed for all the formulations. SG could promote the absorption of LNG via the nasal route and may provide a rapid onset of action of LNG for emergency contraception. Chitosan could retain LNG in the nasal cavity for long contact time to sustain delivery of LNG. The rapid onset and sustained delivery of LNG can be achieved via the nasal route using liposomes as the vehicle.

Antioxidative and acute antiinflammatory effects of Torreya grandis.

The present study was undertaken to investigate the antioxidative and antiinflammatory activities of the ethanolic extract of seeds of Torreya grandis (EST). Exposure of human dermal fibroblasts to the extract at 50 and 250 microg/ml showed significant protective effect against hydrogen peroxide (300 microM). EST not only protected cell survival from H(2)O(2)-induced toxicity, but also inhibited the H(2)O(2)-induced LDH release significantly. It was also found that EST at 100 and 1000 microg/ml showed scavenging activities of radicals and reactive oxygen species with 29.8% and 100.0% of inhibition against DPPH radical and 41.2% and 98.4% against superoxide radicals in the xanthine/xanthine oxidase system, respectively. Topically applied EST dose-dependently inhibited arachidonic acid (AA)- and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema in mice.

Aloe emodin-induced apoptosis in t-HSC/Cl-6 cells involves a mitochondria-mediated pathway.

The aim of our study was to clarify the apoptosis pathway induced by aloe emodin, an hydroxyanthraquinone present in aloe vera leaves, in rat hepatic stellate cells transformed by simian virus 40 (t-HSC/Cl-6), which retain the features of activated rat stellate cells. Apoptosis was determined by DNA fragmentation, caspase activity assay and western blotting analysis. Treatment of t-HSC/Cl-6 cells with 12.5, 25, or 50 microM aloe emodin inhibited t-HSC/Cl-6 cell viability in a dose- and time-dependent manner. The induction of apoptosis by aloe emodin was confirmed by typical DNA ladder formation and annexin v-propidium iodide flow-cytometric analysis. Aloe emodin treatment of t-HSC/Cl-6 cells caused activation of caspase-3 and caspase-9, detected with a caspase activity assay, although no change was observed in caspase-8 activity. Western blotting showed caspase-3 and caspase-9 active forms and the subsequent proteolytic cleavage of poly(ADP-ribose) polymerase. Aloe emodin induced mitochondrial membrane depolarization. Our data also show that cytochrome c increased in the cytosol but decreased in the mitochondria in a time-dependent manner. Increased Bax and unchanged Bcl-2 levels resulted in an increased Bax/Bcl-2 ratio. Thus, our research provides evidence that aloe emodin-induced apoptosis involves a mitochondria-associated apoptosis pathway.