Mechanism of 5-fluorouracil required resistance in human hepatocellular carcinoma cell line Bel_(7402)

AIM:To investigate the resistance mechanism of 5-fluorouracil(5-FU)in Bel7402/5-FU cells which was established in our lab by in vitro continuous stepwise exposure of human hepatocellular carnoma(HCC) cell line Bel7402 to 5-FU.

Identification of an epitope of SARS-coronavirus nucleocapsid protein

The nueleocapsid (N) protein of severe acute respiratory syndrome-coronavirus (SARS-CoV) is a major virion structural protein. In this study, two epitopes (Nl and N2) of the N protein of SARS-CoV were predicted by bioinformatics analysis. After immunization with two peptides, the peptides-specific antibodies were isolated from the immunized rabbits. The further experiments demonstrated that N1 peptide-induced polyclonal antibodies had a high affinity to bind to E. coli expressed N protein of SAR,S-CoV. Furthermore, it was confirmed that Nl peptide-specific IgG antibodies were detectable in the sera of severe acute respiratory syndrome (SARS) patients. The results indicated that an epitope of the N protein has been identified and N protein specific Abs were produced by peptide immunization, which will be useful for the study of SARS-CoV.

Two New Phloroglucinol Glycosides from Lysidice rhodostega Hance

Two new phloroglucinol glycosides, lysidiciside A (1) and lysidiciside B (2), were isolated from the roots of Lysidice rhodostega Hance. Their structures were determined as 1-[(3-methylbutyryl)phloroglucinol]-β-D- glucopyranoside (1), 1- [(3-methylbutyryl)phloro- glucinol]-β-D-glucopyranosyl-5-O-β-D-glucopyranoside (2) on the basis of chemical and spectral analysis .

Huperzine V,A New Lycopodium Alkaloid from Huperzia serrata

Huperzine V, a new Lycopodium alkaloid, was isolated from the whole plant of Huperzia serrata, and the absolute stereochemistry was determined by X-ray crystallographic analysis.

Anti-neoplastic efficacy of Haimiding on gastric carcinoma and its mechanisms

AIM:To study the anti-neoplastic effect of Haimiding and its mechanisms of action.METHODS:Experiments using MIT and colony formation were carried out to study the in vitro anti-neoplastic action of Haimiding, its in vivo anti-neoplastic action was studied by observing its effect on the weight of tumors in FC mice and S180, H22 tumor bearing mice, as well as their life spans.The effect of Haimiding on cell apoptosis and different stages of cell cycles in human gastric carcinoma cells were studied by flow cytometry. Its effect on [Ca^2+]i of human gastric carcinoma cells and the source of Ca^2+ during the change of [Ca^2+]i were observed by confocal laser scanning technique.RESULTS:Haimiding showed a definite cytotoxicity to 8 human tumor cell lines, which was most prominent against BGC-823, Eca-109 and HCT-8 tumor cells. It also exhibited an obvious inhibition on colony formation of the above tumor cell lines, which was most prominent in Eca-109 tumor cells. It showed obvious inhibition on the growth of tumor in FC mice and S180 bearing mice as well as prolonged the life span of H22 bearing mice. It was able to induce apoptosis and elevate intracellular [Ca^2+]i concentration of tumor cells.The source of Ca^2+ came from both extracellular Ca^2+ influx and intracellular Ca^2+ release.CONCLUSION:Haimiding is composed of a TCM preparation and 5-flurouracil.Its anti-neoplastic potency is highly enhanced by synergism as compared with either one of its components. Its mechanisms of anti-neoplastic action can be attributed to its action to initiate apoptosis of tumor cells by opening the membrane calcium channel and inducing intracellular Ca^2+ release to elevate [Ca^2+]i of the tumor cells.

Effect of cisapride on intestinal bacterial and endotoxin translocation in cirrhosis

AIM: To investigate the effects of cisapride on intestinal bacterial overgrowth (IBO), bacterial and endotoxin translocation, intestinal transit and permeability in cirrhotic rats.METHODS: All animals were assessed with variables including bacterial and endotoxin translocation, intestinal bacterial overgrowth, intestinal transit and permeability.Bacterial translocation (BT) was assessed by bacterial culture of MLN, liver and spleen, IBO by a jejunal bacterial count of the specific organism, intestinal permeability by determination of the 24-hour urinary 99mTc-DTPA excretion and intestinal transit by measurement of the distribution of 51Cr in the intestine.RESULTS: Bacterial translocation (BT) and IBO was found in 48 % and 80 % cirrhotic rats respectively and none in control rats. Urinary excretion of 99mTc-DTPA in cirrhotic rats with BT (22.2±7.8) was greater than these without BT (10.5±2.9). Intestinal transit (geometric center ratio) was significantly delayed in cirrhotic rats (0.31±0.06) and further more delayed in cirrhotic rats with BT (0.24±0.06) than these without BT (0.38±0.11). Cirrhotic rats with IBO had significantly higher rates of intestinal bacterial and endotoxin translocation, slower intestinal transit time and higher intestinal permeability than those without IBO. It was also found that BT was closely associated with IBO and the injury of intestinal barrier. Compared with the placebo group,cisapride-treated rats had lower rates of bacterial/endotoxin translocation and IBO, which was closely associated with increased intestinal transit and improved intestinal permeability by cisapride.CONCLUSION: These results indicate that endotoxin and bacterial translocation in cirrhotic rats may be attributed to IBO and increased intestinal permeability. Cisapride that accelerates intestinal transit and improve intestinal permeability might be helpful in preventing intestinal bacterial and endotoxin translocation.

Damaging Effect of Cigarette Smoke Extract on PrimaryCultured Human Umbilical Vein Endothelial Cells and Its Mechanism

Objective To investigate the cellular effects of cigarette smoke extract (CSE) on primarily cultured human umbilical vein endothelial cells (HUVEC). Methods The effects of CSE (5%-20%) and nicotine (10-4 mol/L) on HUVEC viability, proliferation, angiogenesis and apoptosis were observed. Results CSE decreased HUVEC survival rate and angiogenesis after 24 h as well as its proliferation after 48 h in a dose-dependent manner. Moreover, CSE induced apoptosis of HUVEC as indicated in condensation of nuclear chromatin and the presence of hypodiploid DNA. HUVEC incubated with CSE for 24 h gave a significant decrease in the expression of Bcl-2 as well as the decline in the Bcl-2/Bax ratio accompanied with the loss of mitochondrial membrane potential and excess cytosolic calcium. Our study also observed that p53 protein level decreased, rather than increased in cells treated with CSE. Nicotine had no discernible inhibitory effects on the above indices of HUVEC. Conclusion Exposure to CSE other than nicotine causes inhibition of viability, proliferation and differentiation of HUVEC. CSE-induced HUVEC injury is mediated in part through accelerated apoptosis but independent of p53 pathway. It appears that mitochondria have played a key role in the apoptosis of HUVEC induced by CSE.

Two New Bromophenols from Red Alga Rhodomela confervoides

Two new bromophenols were isolated from Rhodomela confervoides. Their structrues were elucidated as 2, 2', 3-tribromo-3', 4, 4', 5-tetrahydroxy-6'-hydroxymethyldiphenylmethane and 2, 2', 3-tribromo-3', 4,4', 5-tetrahydroxy-6'-ethyloxymethyldiphenylmethane by spectroscopie methods including IR, HREIMS, 1D and 2D NMR techniques.

A Morphinane Alkaloid from Meconopsis quintuplinervia

A new morphinane alkaloid named as mecoquitupline was isolated from Meconopsis quintuplinervia Regel. Its structure was elucidated to be 6-methoxy-17-methyl-2,3-[methylene bis(oxy)]-morphinan-5-en-7-one by spectroscopic techniques.

Extraction and Crystal Structure of Karounidiol

The title compound of karounidiol (C30H48O2), a main active triterpene component of snakegourd seed, was isolated from unsaponifiable matter of the seed oil of Trichosanthes kirilowii Maxim., and characterized by X-ray diffraction analysis. It crystallizes in orthorhombic system, space group P212121 with C30H48O2CH3OHH2O (C31H54O4), a = 7.515(1), b = 14.407(1), c = 27.799(2) , V = 3009.8(5) 3, Z = 4, Dx = 1.087 g/cm3, Mr = 490.77, F(000) = 1088 and = 0.086 mm-1. The final R = 0.0840 and wR = 0.2289 for 2752 observed reflections (|F|2 ≥ 2|F|2). The molecular crystal structure of karounidiol shows relative stereochemistry of (3,13,14, 20)-3,29-dihydroxy-13-methyl-26-norolean-7,9(11)-diene. The molecule is composed of five six- membered rings with ring junctures of A/B trans, C/D trans and D/E cis.

Toxicity of novel anti-hepatitis drug bicyclol: A preclinical study

AIM: To study the toxicity of bicyclol to animals. METHODS: Acute toxicity test was performed in Kunming strain mice that were orally given bicyclol at the doses of 3 and 5 g/kg body weight, respectively. Wistar rats were orally administered bicyclol at a dose of 5 g/kg body weight. Death and clinical symptoms of animals were recorded within 7 d. Sub-acute toxicity test was carried out in rats that were treated with various doses of bicyclol (150, 300, 600 mg/kg) once daily for 14 d. Animal behaviors, blood biochemical markers, blood and urine pictures were examined. Chronic toxicity test was conducted in 80 Wistar rats of both sexes. The animals were orally administered with various doses of bicyclol [150, 300, 600 mg/kg, 100-400 folds corresponding to the proposed therapeutic dose (1.5 mg/(kg·d)) of bicyclol for patients] once daily for 6 mo except for Sunday. The control group was given the same volume of 0.2% sodium carboxyl methylcellulose (Na-CMC). Twenty-one beagle dogs received bicyclol (25, 75, 225 mg/kg, 16.6, 50, 150 folds corresponding to the proposed therapeutic dose of bicyclol for patients) once a day for 6 mo except for Sunday. The body weight, food intake, urine and feces, blood picture, blood biochemical markers, and pathological examination of main organs were determined. Mutagenicity and teratogenicity were determined. Mutagenicity assay included Ames's test, chromosome aberration test in CHL cells and micronucleus test in mice. For the teratogenicity assay, pregnant Wistar rats weighing 200-250 g were treated with 0.2,1.0 g/kg bicyclol once daily from the 7th d of gestation for 10 d. RESULTS: The oral LD50 of bicyclol was over 5 g/kg in mice and rats. No noticeable alterations in subacute and chronic toxicity of rats and dogs were demonstrated. No mutagenicity and teratogenicity of bicyclol were found. CONCLUSION: Bicyclol has no detectable chronic toxicity as well as mutagenicity and teratogenicity in animals.

A New Halogenated Biindole and A New Apo-carotenone from Green Alga Chaetomorpha basiretorsa Setchell

A new halogenated biindole and a new apo-carotenone have been isolated from the ethanolic extract of the green alga Chaetomorpha basiretorsa Sethcell. On the basis of chemical and spectroscopic methods including 2D NMR technique, their structures have been elucidated as 4,4′-dichloro-5,5′-dibromo-7,7′-dimethoxy-2,2′-bi-1H-indole and 1′S*,4′R*-8-(4′-hydroxy-2′,6′,6′- trimethylcyclohex-2-enyl)-6-methyloct-3E,5E,7E-trien-2-one, respectively.

Triterpenoids from Erythrophleum fordii

A phytochemical investigation of the bark of Erythroph/eum fordii Oliv. furnished five compounds.One is a new triterpenoid, namely 20S, 24S-epoxy-23S, 25-dihydroxy-dammarane-3-one (1), and four areknown, identified to be 20S, 25-epoxy-24R-hydroxydammarane-3-one (2), 20S, 24S-epoxydammarane-3β,25-diol (3), betulinic acid (4), morolic acid acetate (5). All the known compounds were isolated from thespecies for the first time. The structure of compound 1 was elucidated on the basis of spectroscopicanalyses.

Two New C-glucoside Flavonoids from Leaves of Crataegus pinnatifida Bge.var.major N.E.Br.

Two new C-glucoside flavonoids, namely 8-C-b-D-(2-O-acetyl) glucofuranosyl apigenin and 3-O-acetylvitexin, were isolated from leaves of Crataegus pinnatifida Bge. var. major N. E. Br.. Their structures were elucidated by the spectroscopic means and chemical evidence.

A New Brominated Phenylpropylaldehyde and its Dimethyl Acetal from Red Alga Rhodomela confervoides

A new brominated phenylpropylaldehyde and its dimethyl acetal together with a new natural brominated phenol were isolated from Rhodomela confervoides. Their structrues were elucidated as 2-methyl-3-(2,3-dibromo-4,5-dihydroxyphenyl)propylaldehyde, 2-methyl-3-(2,3-di-bromo-4,5-dihydroxyphenyl) propylaldehyde dimethyl acetal and 3-bromo-4,5-dihydroxybenzoic acid methyl ester by spectroscopic techniques including IR, HRFABMS, ID and 2DNMR experiments.

Effect of Haimiding on the functioning of red cell membrane of FC and H_(22) tumor-bearing mice

AIM: To study the effect of Haimiding on the functioning of red cell membrane of FC and H22 tumor-bearing mice. METHODS: The membrane fluidity of red cells is measured with DPH fluorescence probe as a marker; the amount of red cell membrane proteins is measured using polyacrylamide gel electrophoresis; the amount of sialic acid (SA) on the surface of red cell membrane and the scalability of these cells are measured using colorimetric analysis. RESULTS: Haimiding can lower the membrane fluidity of red cells in tumor-bearing mice and the amount of their membrane proteins, while increasing the amount of sialic acid in the membrane of red cells in these mice and enhancing the ability of the membrane of their red cells to reseal. CONCLUSION: The anti-tumor effect of Haimiding on tumor-bearing mice is due to its ability to improve and restore the functions of the membrane of their red cell and to enhance the immune effect of the organisms.

A New Diterpene from Suregada glomerulate(Blume) Baill

A new diterpene with an abietane skeleton, 3β-hydroxy-8α,14α-epoxyabieta-11,13(15)- dien-16,12-olide, was isolated from the root of Suregada glomerulate(Blume) Baill. Its structure was elucidated on the basis of spectroscopic and X-ray crystallographic analysis.

Segetoside L, A New Triterpenoid Saponin from Vaccaria segetalis

A new triterpenoid saponin, named segetoside L, was isolated from the seeds of Vaccaria segetalis. On the basis of spectral data and chemical reaction, its structure was established as 28-O-b-D-glucopyranosyl-(16)-b-D-glucopyranosyl oleanolic acid 3-O-b-D- glucopyranosyl-(13)-[b-D-galactopyranosyl-(12)]-b-D-galactopyranoside.

Oldhamioside, A New Phenolic Glucoside from Daphniphyllum oldhamii

Further phytochemical investigation of the ethyl acetate extract of the stem of Daphniphyllum oldhamii afforded a new phenolic glucoside, named oldhamioside 1, together with eleven known compounds, koaburaside 2, betulin, 28-hydroxyl-3-lupenone, pineresinol, syringaresinol, 4-O-methyl- cedrusin, narigenin, eriodictyol, apigenin, loureirin C, and asperuloside. The structures of new and known compounds were characterized by detailed spectroscopic analysis and comparison of their spectral data with reported values.

Oxypregnane-oligoglycosides from the Stems of Stephanotis mucronata (Asclepiadaceae)

Four new oxypregnane-oligoglycosides, mucronatosides A (1), B (2), C (3), and D (4), together with one known stephanoside E (5) were isolated from the stems of Stephanotis mucronata (Blanco) Merr.. Their chemical structures were determined on the basis of chemical and extensive spectroscopic methods including one-dimensional and two-dimensional NMR.