1,3,4-tri-O-galloyl-6-O-caffeoyl-β-D-glucopyranose, a new anti-proliferative ellagitannin, regulates the expression of microRNAs in HepG(2) cancer cells / 南方医科大学学报

<p><b>OBJECTIVE</b>MicroRNAs (miRNAs) play important roles in cell proliferation, differentiation and apoptosis. 1, 3, 4-tri-O-galloyl-6-O-caffeoyl-β-D-glucopyranose (BJA32515) is a new natural ellagitannin compound extracted from Balanophora Japonica MAKINO. The effect of BJA32515 on the expression of miRNAs in cancer cells has not yet been explored. Objective The present study was carried out to examine the changes in miRNA expression profiles in human HepG(2) hepatocarcinoma cells following BJA32515 exposure.</p><p><b>METHODS</b>The proliferation of BJA32515-exposed HepG(2) cells was assessed using a colorimetric assay (cell counting kit-8). The miRNA expression profile of the cancer cells was analyzed using a miRNA array and quantitative real-time PCR. Apoptosis was assessed by annexin V and propidium iodide staining.</p><p><b>RESULTS</b>BJA32515 inhibited the cell proliferation and increased apoptosis in HepG(2) cancer cells. The exposure to BJA32515 also caused alterations in the miRNA expression profile in the cells, with 33 miRNAs upregulated and 59 down-regulated. The up-regulation of let-7a and miR-29a and the down-regulation of miR-373 and miR-197 were verified by quantitative real-time PCR. CONCLSION: BJA32515-modifed miRNA expression may mediate the antiproliferative effect of this compound in HepG(2) cancer cells.</p>

Cough-relieving, analgesic and antibiotic effects of durian shell extracts: a study in mice / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the cough-relieving, analgesic and antibiotic effects of durian shell extract (DSE) in relieving cough and its analgesic and antibiotic effects.</p><p><b>METHODS</b>The effect of DSE in relieving cough was assessed in mice challenged with ammonia and SO(2) to induce coughing. The analgesic and antibiotic effects of DSE in mice were evaluated by hot plate test and twisting reaction induced by acetic acid, and by minimal inhibitory concentration (MIC) and disc-agar diffusion tests, respectively.</p><p><b>RESULTS</b>Compared with the control group, the mice treated with 300 and 900 mg/kg DSE showed significantly prolonged latency with decreased number of coughing induced by ammonia and SO(2), and the effect was dose-dependent. DSE markedly prolonged the latency and decreased the twisting number of the mice induced by acetic acid without affecting the pain threshold in hot plate test. DSE produced no significant inhibitory effects against Staphylococcus aureus, Staphylococcus epidermidis, or E. coli, and showed a week inhibition against Bacillus aeruginosus.</p><p><b>CONCLUSION</b>DSE shows obvious effect in relieving cough and produces better analgesic effect against chemical factor-induced pain than against physical agent-induced pain sensation. DSE has a moderate inhibitory effect against Bacillus aeruginosus.</p>

Naringin inhibits monocyte adhesion to high glucose-induced human umbilical vein endothelial cells / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the inhibitory effect of naringin on monocyte adhesion to high glucose-induced human umbilical vein endothelial cells (HUVECs).</p><p><b>METHODS</b>Cultured HUVECs isolated from human umbilical cords were pretreated with or without naringin and induced with high glucose (33 mmol/L) for 48 h. Human monocyte THP-1 cells, after labeling with BCECF-AM, were co-cultured with the HUVECs for 30 min. The labeled THP-1 cells adhering to HUVECs were observed under fluoroscence microscope, and the inhibitory effect of naringin on the cell adhesion was evaluated by measuring the adhering cell density. Western blot analysis was used to detect the expressions of the adhesion molecules in the HUVECs, and reactive oxygen species (ROS) production in the HUVECs was measured using an oxidation-sensitive fluorescent probe (DCFH-DA). The nuclear extracts of the HUVECs were prepared to examine the expression of nuclear factor-kappa B (NF-kappaB) in the cell nuclei by Western blotting.</p><p><b>RESULTS</b>HUVECs in high-glucose culture showed increased adhesion to THP-1 cells and enhanced expressions of the cell adhesion molecules, which were significantly attenuated by pretreatment with naringin (10-50 microg/ml). High glucose induced DCF-sensitive intracellular ROS production in the HUVECs, and this effect was inhibited by naringin pretreatment of the cells. Naringin also suppressed high glucose-induced increment of NF-kappaB expression in the cell nuclei of HUVECs.</p><p><b>CONCLUSION</b>Naringin can suppress high glucose-induced vascular inflammation possibly by inhibiting ROS production and NF-kappaB activation in HUVECs.</p>

Bioequivalence evaluation of orally disintegrating tablet of pentoxyverine citrate / 南方医科大学学报

<p><b>OBJECTIVE</b>To evaluate the bioequivalence of orally disintegrating tablets of pentoxyverine citrate (tested preparation) in healthy male volunteers.</p><p><b>METHODS</b>A single oral dose of the tested and reference preparations at 25 mg were given to 20 healthy volunteers in a randomized two-period cross-over design. Plasma pentoxyverine citrate concentrations were determined by HPLC-MS/ESI+ method. The pharmacokinetic parameters were calculated and the bioequivalence of the two preparations were evaluated using DAS program.</p><p><b>RESULTS</b>The Tmax, Cmax, AUC0 15 and AUC0infinity of tested and reference preparations were 1.62-/+0.75 h and 2.52-/+1.21 h, 62.28-/+33.06 microg/L and 59.72-/+33.25 microg/L, 234.44-/+130.01 microg.h.L(-1) and 228.77-/+129.24 microg.h.L(-1), 246.80-/+136.19 microg.h.L(-1) and 244.11-/+140.73 microg.h.L(-1), respectively. The 90% confidence interval of C(max), AUC0 15 and AUC0infinity of tested preparations were 81.4%-138.4%, 86.0%-123.3% and 86.5%-121.2%, respectively.</p><p><b>CONCLUSION</b>The tested and reference preparations are bioequivalent.</p>

Hydrocamptothecin promotes the mRNA expression of Wnt signaling inhibitor DKK-1 / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effects of hydrocamptothecin on the expression of Wnt signaling pathway inhibitor DKK-1 in tumor cells.</p><p><b>METHODS</b>Human HepG2, Hep3B, LoVo and U251 cells were treated with the antitumor drug Hydrocamptothecin. DKK-1 mRNA expression in the cells was detected with RT-PCR, and beta-catenin expression was measured by fluorescence-activated cell sorting (FACS).</p><p><b>RESULTS</b>DKK mRNA in Hep3B, HepG2, LoVo and U251 cells was significantly increased after hydrocamptothecin treatment for 24 h, and the percentage of beta-catenin-positive cells and fluorescence intensity for beta-catenin expression was lowered in the cells after the treatment.</p><p><b>CONCLUSION</b>Hydrocamptothecin promotes mRNA expression of Wnt signaling pathway inhibitor DKK-1 in Hep3B, HepG2, LoVo and U251 cells.</p>

Inhibitory effect of polysaccharides on the six-alpha-helix bundle formation of HIV gp41 protein / 南方医科大学学报

<p><b>OBJECTIVE</b>To compare the in vitro inhibitory effect of expolysaccharides from Streptomyces, polysaccharides of Ganoderma lucidum and rice bran on six-alpha-helix bundle formation of HIV gp41 protein.</p><p><b>METHODS</b>The amount of six-alpha-helix bundle formed in the presence of N36 and C34 was tested by ELISA in response to treatments with different doses of polysaccharides.</p><p><b>RESULTS</b>Expolysaccharides from Streptomyces potentially inhibited six-alpha-helix bundle formation with the effective concentration (IC(50)) of 145.48-/+7.25 mg /L. Polysaccharides of Ganoderma lucidum and rice bran showed no effect on the six-alpha-helix bundle formation.</p><p><b>CONCLUSION</b>Expolysaccharides from Streptomyces can inhibit the six-alpha-helix bundle formation of HIV gp41, whereas polysaccharides of Ganoderma lucidum and rice bran do not exhibit such activity.</p>