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Jian-Hua Xu

Publications and source records attributed to Jian-Hua Xu.

At least 19 recordsLinked to original sources

Curcumin synergistically augments bcr/abl phosphorothioate antisense oligonucleotides to inhibit growth of chronic myelogenous leukemia cells.

AIM: To investigate the growth inhibition effect of the combination of bcr/abl phosphorothioate antisense oligonucleotides (PS-ASODN) and curcumin (cur), and the possible mechanisms of cur on the chronic myelogenous leukemia cell line K562. METHODS: The K562 cell line was used as a P210( bcr/abl )-positive cell model in vitro and was exposed to different concentrations of PS-ASODN (0-20 micromol/L), cur (0-20 micromol/L), or a combination of both. Growth inhibition and apoptosis of K562 cells were assessed by MTT assay and AO/EB fluorescent staining, respectively. The expression levels of P210( bcr/abl ), NF-kappaB and heat shock protein 90 (Hsp90) were assessed by Western blot. RESULTS: Exposure to cur (5-20 micromol/L) and PSASODN (5-20 micromol/L) resulted in a synergistic inhibitory effect on cell growth. Growth inhibition was associated with the inhibition of the proliferation and induction of apoptosis. Western blot analysis showed that the drugs synergistically downregulated the level of P210( bcr/abl ) and NF-kappaB. Cur downregulated Hsp90, whereas no synergism was observed when cur was combined with PS-ASODN. CONCLUSION: PS-ASODN and cur exhibited a synergistic inhibitory effect on the cell growth of K562. The synergistic growth inhibition was mediated through different mechanisms that involved the inhibition of P210( bcr/abl ).

Antineoplastic Agents↗

Down-regulation of p210(bcr/abl) by curcumin involves disrupting molecular chaperone functions of Hsp90.

AIM: To investigate the effects of curcumin (Cur) on p210(bcr/abl) level in K562 cells, and the relationship between these effects and the molecular chaperone functions of heat shock protein 90 (Hsp90). METHODS: Flow cytometry and Western blot were used to examine the abundance of p210(bcr/abl), Hsp90, p23, Hsp70, and p60(Hop) in K562 cells treated with Cur. Reverse transcription polymerase chain reaction (RT-PCR) was used to determine the bcr-abl mRNA level in K562 cells treated with Cur. After co-immunoprecipitation of p210(bcr/abl) and its molecular chaperones, the immunoprecipitate was then subjected to Western blot analysis with anti-Hsp90, anti-Hsp70, anti-p23, and anti- p60(Hop)mAb. RESULTS: An exposure of K562 cells to Cur produced time-dependent down-regulation of p210(bcr/abl), the inhibition rate of p210(bcr/abl) in K562 cells determined by flow cytometry after treatment with Cur 27.2 micromol/L for 1 h, 6 h, 12 h and 24 h was 31.2%, 63.7%, 81.3% and 94.5%, respectively. In contrast, Cur had almost no influence on bcr-abl mRNA level. Treatment with Cur for 24 h reduced the association of p210(bcr/abl) with Hsp90/p23 complex, while increasing the association of p210(bcr/abl) with Hsp70/ p60(Hop) complex; however, the total protein abundance of Hsp90, p23, and p60(Hop) in K562 cells had no apparent change, while Hsp70 increased greatly. CONCLUSION: Down-regulation of p210(bcr/abl) by Cur involves dissociating the binding of p210(bcr/abl) with Hsp90/p23 complex. In contrast, the association of p210(bcr/abl) with Hsp70/ p60(Hop) complex increased.

Antineoplastic Agents↗

[VUV excited luminescence of LnZr(BO3)2 : Eu3+ (Ln = Ba, Sr)].

Powder samples of Ba(1-x) Sr(x)Zr(BO3)2 : Eu3+ (0 < or = x < or = 1) were prepared by the conventional solid state reaction method. The excitation spectrum shows a strong absorption in the VUV region with the broad absorption band edge at 130-170 nm due to the host and the f --> d transition of Eu3+, and another absorption band of charge-transfer state (CTS) of Eu3+ in the region of 230 nm. The absorption of the charge-transfer band of Eu3+ can be increased by incorporating Al3+ ion into Zr4+ ion lattice. The luminescence of Ba(1-x) Sr(x)Zr(BO3)2 : Eu3+ is also increased by incorporating Al3+ into the lattices. In Ba(1-x) Sr(x)Zr (BO3)2 : Eu3+, the intensity of the absorption band (130-170 nm) decreases, and the band shifts about 30 nm toward lower energy with x increasing. The emission spectra revealed an intense and sharp (616 nm) red color emission from Eu3+ (5 Do --> F2) transition under 147 nm VUV excitation.

English Abstract↗

New tumor-associated antigen SC6 in pancreatic cancer.

AIM: To examine the concentration of a new antigen SC6 (SC6-Ag) recognized by monoclonal antibody (MAb) in patients with pancreatic cancer and other malignant or benign diseases and to understand whether SC6-Ag has any clinical significance in distinguishing pancreatic cancer from other gastrointestinal diseases. METHODS: Six hundred and ninety-five serum specimens obtained from 115 patients with pancreatic cancer, 154 patients with digestive cancer and 95 patients with non-digestive cancer were used and classified in this study. Serum specimens obtained from 140 patients with benign digestive disease and 89 patients with non-benign digestive disease served as controls. Ascites was tapped from 16 pancreatic cancer patients, 19 hepatic cancer patients, 16 colonic cancer patients, 10 gastric cancer and 6 severe necrotic pancreatitis patients. The samples were quantitated by solid-phase radioimmunoassay. The cut-off values (CV) of 41, 80, and 118 U/mL were used. RESULTS: The average intra- and interassay CV detected by immunoradiometric assay of SC6-Ag was 5.4% and 8.7%, respectively. The sensitivity and specificity were 73.0% and 90.9% respectively. The levels in most malignant and benign cases were within the normal upper limit. Among the 16 pancreatic cancer cases, the concentration of SC6-Ag in ascites was over the normal range in 93.8% patients. There was no significant difference in the concentration of SC6-Ag. Decreased expression of SC6-Ag in sera was significantly related to tumor differentiation. The concentration of SC6-Ag was higher in patients before surgery than after surgery. The specificity of SC6-Ag and CA19-9 was significantly higher than that of ultrasound and computer tomography (CT) in pancreatic cancer patients. Higher positive predictive values were indicated in 92.3% SC6-Ag and 88.5% CA19-9, but lower in 73.8% ultrasound and 76.2% CT. CONCLUSION: The combined test of SC6-Ag and CA19-9 may improve the diagnostic rate of primary cancer. The detection of SC6-Ag is valuable in the diagnosis of pancreatic cancer before and after surgery.

Adult↗

Photoreactions of 1-acetylisatin with alkynes: regioselectivity in oxetene formation and easy access to 3-alkylideneoxindoles and dispiro[oxindole[3,2']furan[3',3' ']oxindole]s.

[reaction: see text] Photoinduced reactions of 1-acetylisatin (IS) with diphenylacetylenes 1a-c, 1-(p-methoxyphenyl)propyne 2, and 1,4-diphenyl-1,3-butadiyne 3 gave beta,beta-disubstituted 3-alkylidene oxindoles 6-12 respectively via [2+2] cycloaddition of 3IS* with the alkyne and subsequent oxetene ring opening. Photoreactions of IS with phenylacetylenes 4a-d and cyclopropylacetylene 5 furnished the dispiroindole[3,2']furan[3',3' ']indoles 13 and 14. Compounds 13 and 14 are formed in tandem reactions initiated by [2+2] cycloaddition of 3IS* with the alkynes to give spirooxetenes Va and Vb, which upon spontaneous ring opening gave the alpha,beta-unsaturated aldehydes IVa and IVb. It is proposed that hydrogen abstraction of 3IS* from the C(O)-H functionality in IV followed by dissociation of the triplet isatin ketyl (A)-aldehyde acyl (B) radical pair and an oxygenphilic attack of the acyl radical B at the C3 carbonyl oxygen atom of a neutral IS gave the 2:1 (IS:4) radical C, which took part in an intramolecular radical cyclization to give the dispiroindole[3,2']furan[3',3' ']indoles 13 and 14. The regioselectivity in the [2+2] photocycloadditions of IS with 4 to afford the oxetene Va depends on the intervening of the more stable 1,4-diradical intermediates VI, which have a linear alpha-phenyl-substituted vinyl radical where the phenyl provides spin delocalization of the radical center at the sp carbon atom.

Acetylene↗

KAI1 inhibits anchorage-dependent and -independent pancreatic cancer cell growth.

Decreased expression of the tumor suppressor gene, KAI1, is associated with metastasis formation in pancreatic cancer. The aim of the present study was to investigate whether KAI1 influences pancreatic cancer cell growth and colony formation. A full-length KAI1 cDNA expression vector was stably transfected into Panc-1 and MiaPaCa-2 pancreatic cancer cell lines. Transfection was confirmed by Western blot analysis and immunohistochemistry. Tumor cell growth and cell cycle distribution were determined by MTT cell growth assays, colony formation assays, and flow cytometric analysis. KAI1-transfected, but not control-transfected pancreatic cancer cells displayed cytoplasmic KAI1 immunoreactivity. Cell proliferation decreased in the KAI1-transfected cells compared to parental and control cells together with a Go/G1-phase cell cycle arrest. Colony formation was reduced by 2.6- and 3.5-fold in the KAI1-transfected Panc-1 and MiaPaCa-2 pancreatic cancer cells, respectively, compared with parental cells. KAI1 blocks pancreatic cancer cell growth through cell cycle arrest and inhibits anchorage-independent cell growth. These findings support the premise that KAI1 functions as a tumor suppressor in this malignancy.

Antigens, CD↗

Photoinduced [4 + 4] cycloadditions of o-quinones with oxazoles.

[reaction: see text] Photocycloadditions of 9,10-phenanthraquinone (PQ) with oxazoles (1a and 1b) gave [4 + 4] products 2 with the O=C-C=O functionality in PQ and the 2-azadiene moiety in oxazole as 4pi addends. Photoreactions of 1-acetylisatin (IS) with 1a, 1c, and 1d gave [4 + 4] product A, which underwent further [2 + 2] reactions with another (3)IS to furnish 5. These regioselective and diastereoselective [4 + 4] photocycloadditions are rationalized by the intervening of the key conformers for ISC and bond formation of the most stable 1,6-diradical intermediates.

Journal Article↗

A copper- and amine-free sonogashira reaction employing aminophosphines as ligands.

An efficient Pd-catalyzed Sonogashira coupling reaction was achieved in the absence of a copper salt or amine with an inorganic base and easily prepared, air-stable aminophosphine ligands in commonly used organic solvents; good to excellent yields were obtained. Under optimized reaction conditions, the Sonogashira coupling reaction occurred selectively when an enyne substrate was employed and no Heck reaction product was detected; acetone-masked acetylene and trimethylsilylacetylene can also be efficiently coupled, providing a method to make terminal alkynes.

Journal Article↗

Reaction modes and mechanism in indolizine photooxygenation reactions.

Photooxygenations of 1,2-, 1,3-, and 2,3-di- and 1,2,3-trisubstituted indolizines 1a-1f under different reaction conditions in methanol and acetonitrile have been investigated to establish the general reaction pattern and mechanism in indolizine photooxygenation in view of the influence of the ring substituents and substitution pattern. Photooxygenations of 1-acyl-2-phenylindolizines 1a and 1b and 1,3-dibenzoyl-2-phenylindolizine (1d) are self-sensitized, while those of 1-(p-nitrobenzoyl)-2-phenylindolizine (1c) and 2-phenyl-3-(p-chlorobenzoyl)indolizine (1e) need to be sensitized by rose bengal (RB) or methylene blue (MB). These reactions proceed via a singlet oxygen mechanism yet follow different pathways in methanol and in acetonitrile, with peroxidic zwitterion D (in methanol) and dioxetane E across the indolizine C2-C3 bond (in acetonitrile) as the intervening intermediates. Methanol trapping of the peroxidic zwitterion results in C3-N bond cleavage and pyrrole ring opening to give the corresponding (E)- and (Z)-3-(2-pyridinyl)-3-benzoylpropenoic acid methyl esters (2 and 3) and 4-(2-pyridinyl)-3-phenyl-5-aryl-5-hydroxyfuran-2-one (4) as products in methanol, while O-O bond homolysis of the dioxetane furnishes 3-(2-pyridinyl)-3-benzoyl-2-phenyloxirane-2-carboxaldehyde (6) and 1-(6-methyl-2-pyridinyl)-2-phenylethanedione (5) as products in acetonitrile. 3-Benzoyl-1-indolizinecarboxylic acid methyl ester (1f) is unreactive toward singlet oxygen; however, it could be photooxygenated under electron transfer conditions with 9,10-dicyanoanthracene (DCA) as a sensitizer. This reaction takes place by the combination of the indolizine cation radical with the superoxide anion radical (or molecular oxygen) to give the pyridine ring oxidized methyl 3-benzoyl-5-methoxy-8-hydroxy-1-indolizinecarboxylate (9f), dimethyl 2-(2-pyridinyl)fumarate (8f), and dimethyl 2-(2-pyridinyl)maleate (7f) as products.

Journal Article↗

[A new method for phylogenic analysis].

With ESTs from porcine fatty tissue and cDNA sequences from human, bovine and mouse in non-reduncdant database and dbEST in GenBank,we sampled cDNA sequences of 70 function-known genes in four species on the base of randomly sampling method, analyzed the mutation pattern of 70 x 150 bp linking sequences between them, and established an integrated phylogenic analysis method. The results showed that 391 single bases mutations were found in 70 x 150 bp linking sequences alignment among four species. The number of mutation bases between them were greatly exceeded the 1/1000 predicted in the human genome analysis. C/T(T/C) and A/G (G/A) transitions were the major types of single base mutation. The genetic relationship between pig and bovine who are both Artiodactylous is the nearest, the next is human, and the farthest is mouse. The differentiation sequence taken place in four species from the same ancestor is that mouse is the earliest one, and the latter human, and pig and bovine are the latest.

Animals↗

Inhibitory effect of curcumin on proliferation of K562 cells involves down-regulation of p210(bcr/abl) initiated Ras signal transduction pathway.

AIM: To investigate the effects of curcumin (Cur) on proliferation of K562 cells and the relationship between these effects and Ras signal transduction pathway activated by p210bcr/abl. METHODS: K562 cell line was used as a p210bcr/abl-positive cell system and HL-60 cell line as a p210bcr/abl-negative control; etoposide (VP-16), which has no influence on p210bcr/abl and has resistance to K562 cells[1], was used as an anticancer drug control to compare with curcumin. MTT was used to determine the proliferative effects of drugs on K562 and HL-60 cells. Western blot and flow cytometry were used to examine the abundance of signal protein molecules expressed in tumor cells. RESULTS: An exposure of K562 cells or HL-60 cells to Cur produced both concentration- and time-dependent increase in the anti-proliferative rate. Moreover, both cell lines had the same sensitivity to Cur (P>0.05). In contrast, HL-60 cells had more sensitivity to VP-16 than K562 cells in anti-proliferative effect (P<0.01). The abundance of p210bcr/abl as well as MEK-1 and c-JUN proteins were strongly down-regulated in curcumin-treated p210bcr/abl-positive K562 cells while c-JUN and MEK-1 proteins were only slightly down-regulated in p210bcr/abl-negative HL-60 cells. CONCLUSION: Curcumin inhibited the proliferation of K562 cells and the inhibitory effect was correlated with down-regulation of the abundance of p210bcr/abl, which may ultimately lead to retard the Ras signal transduction pathway. Curcumin might be worthy of being evaluated as a potential chemotherapeutic agent to CML.

Antineoplastic Agents, Phytogenic↗

11-Methyl-12a-phenyl-9a,12a-dihydrophenanthro[9',10':5,6][1,4]dioxino[2,3-d]oxazole and 9a-(10-hydroxyphenanthren-9-yl)-11,12a-diphenyl-9a,12a-dihydrophenanthro[9',10':5,6][1,4]dioxino[2,3-d]oxazole.

In the title compounds, C(24)H(17)NO(3), (I), and C(43)H(27)NO(5), (II), the dioxine ring is not planar and tends toward a boat conformation. The oxazoline ring adopts a twisted conformation in molecule (I) but is essentially planar in molecule (II). The configuration of the dioxine-oxazoline system is determined by the sp(3) state of the two shared atoms. The phenanthrene moiety is nearly coplanar with the dioxine ring, while the phenyl ring is perpendicular to the attached oxazole ring. The triclinic unit cell of (II) contains two crystallographically independent molecules related by a pseudo-inversion centre.

Journal Article↗

1-Acetyl-3'-(4-bromophenyl)-3'-chlorospiro[3H-indole-3,2'-oxetan]-2(1H)-one.

In the title compound, C(18)H(13)BrClNO(3), the heterocyclic ring of the indole is distorted from planarity towards an envelope conformation. The orientations of the indole, oxetane, chloro and bromophenyl substituents are conditioned by the sp(3) states of the spiro-junction and the Cl-attached C atoms.

Journal Article↗

1-Acetyl-3-[1-(4-methoxyphenyl)-2-oxopropylidene]-1H-indol-2(3H)-one: a twinned crystal.

The crystal of the title compound, C(20)H(17)NO(4), which was used for collecting intensity data was twinned. Each of the two crystallographically independent molecules in the asymmetric unit has a planar indole moiety perpendicular to a planar oxopropyl moiety. The distribution of the bonds at the central C atom joining the oxopropyl, phenyl and indole substituents is also planar. The packing is stabilized by intermolecular C-H* * *O interactions, as well as by dipole-dipole and van der Waals interactions.

Journal Article↗

Syn- and anticlinal isomers of 2a'-acetoxy-1,7'-diacetyl-7',7a'-dihydro-2-oxospiro[1H-indole-3(2H),2'(2a'H)-oxeto[3,2-b]indole].

In the syn- and anticlinal isomers of the title compound, C(22)H(18)N(2)O(6), the indole moiety is not completely planar, with the pyrrolidine ring being distorted very slightly towards a conformation intermediate between half-chair and envelope. The molecular and packing structures in the crystals of these isomers are stabilized by C-H...O interactions.

Journal Article↗

Effect of bax, bcl-2 and bcl-xL on regulating apoptosis in tissues of normal liver and hepatocellular carcinoma.

AIM: To investigate the expression of bax, bcl-2 and bcl-xL mRNA in the tissues of normal liver and hepatocellular carcinoma (HCC), and analyze the relationship between the expression of bax, bcl-2 and bcl-xL mRNA and clinical parameters of HCC patients. METHODS: The expression of bax, bcl-2 and bcl-xL mRNA of normal liver and HCC was measured by Northern blot. Statistical analyses were made by t test and correlation analysis. RESULTS: A very low mRNA level was indicated at bax, bcl-2 and bcl-xL in the HCC tissues in contrast to the tissues of normal liver by Northern blot analysis. The analyses of mRNA level revealed that HCC tissues exhibited a mean 7.6-fold decrease in bax, 4.2-fold in bcl-2 and 3.5-fold in bcl-xL in comparison with normal control tissues, respectively. Positive correlation was found between bax and bcl-xL (r=0.7061, P<0.01). There was no significance between the mRNA expression of these three genes and age, gender, tumor differentiation and tumor stage of HCC patients. CONCLUSION: The results are consistent with the fact that apoptosis rarely occurs in normal livers but increases in HCC, indicating that bcl-2 and bcl-xL may play a very important role in regulating the apoptosis of normal liver and HCC.

Adult↗