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Three new metal-organic coordination polymers, namely {[Cu(4,4'-bipy)(5-Hoipa)2](H2O)2}n (I, 5-H2oipa = 5-Hydroxyisophthalicacid, 4,4'-bipy = 4,4'-bipyridine), {[Cu2(4,4'-bipy)(tzb)2](DMF)3} (II, H2tzb = 4-(1H-Tetrazol-5-yl)benzoic acid), and {[Cu(cpdba)(2,2′—bpy)]}n (III, H2cpdba = 4-(4-carboxyphenylamino)-3,5-dinitrobenzoic acid, 2,2'-bipy = 2,2'-bipyridine), have been successfully prepared by using two similar pyridine ligands with different co-ligands under different reaction conditions (slow volatilization for II, solvothermal for I and III). Their structures have been unambiguously determined by both single-crystal X-ray study and elemental analysis. Additionally, the newly synthesized compounds were evaluated to identify the molecular characteristics contributing to their cytotoxicity. They were tested against three human gastric cancer cells (MGC-803, SGC-790 and MKN45) with the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. [ABSTRACT FROM AUTHOR]

Background: 70 years ago, it was put forward that the diseased liver was not a favorable soil for metastatic tumor cells. In addition, a few studies have demonstrated that rare occurrence of colorectal liver metastases among patients with fatty liver, cirrhosis or chronic hepatitis B and C virus infection. We performed a meta-analysis to verify the association between the incidences of colorectal liver metastases with chronically diseased livers. Methods: Relevant studies were identified by a search of electronic database PubMed, Cochrane Library, OVID, Web of Science and CNKI (up to February 24, 2014). Pooled odds ratio (OR) with 95% confidence interval (CI) was calculated using random- or fixed-effect models when appropriate. Meta-analysis and publication bias (Bgger's test) was evaluated with STATA 12.0. Results: A total of 10,349 colorectal cancer patients from 10 studies were included. The meta-analysis result showed there was a significant difference in the incidences of colorectal liver metastases between patients with normal and chronically diseased livers (OR = 0.32; 95% CI 95%: 0.26–0.38, P = 0.000 fixed-effects model). The result of Begg's test (Pr>|z| = 0.089; P>0.05) revealed no publication bias. Conclusions: The results of this meta-analysis demonstrated that patients with chronically diseased livers had significantly lower incidences of colorectal liver metastases than those with normal livers. [ABSTRACT FROM AUTHOR]

Abstract: Seven oleanane-type triterpenes and two 8-O-4′-neolignans, along with five known compounds (three 28-noroleanane-type triterpenes, one sarratane triterpene, and one neolignan), were isolated from roots of Nannoglottis carpesioides. Their structures were elucidated by spectroscopic methods, including 1D and 2D NMR, HRMS, and CD. The absolute configurations of two triterpenes were determined by experimental and calculated circular dichroism (CD) and optical rotation values. Ten compounds were evaluated for their cytotoxicity against human promyelocytic leukaemia (HL-60) and human hepatoma (Hep-G2) cells using the MTT assay. The antioxidant activities of these compounds were assessed by ABTS radical-scavenging assays. Among the tested compounds, three compounds exhibited moderate radical-scavenging activity against ABTS +, with IC50 values of 22.4, 17.4, and 23.2μM, respectively. [Copyright &y& Elsevier]

Skin cancer cells with donor genotype have been identified in allogeneic transplant patients; however, the donor contribution to the recipient's epithelial malignancy remains to be established. In this issue of the JCI, Verneuil et al. provide the first evidence for donor contribution to the malignant epithelium of skin squamous cell carcinoma in a kidney transplant recipient. This case report may have important implications for cancer research and clinical care of long-surviving kidney transplant patients. [ABSTRACT FROM AUTHOR]

Abstract Taking sophoridine as a lead compound, 58 sophoridine derivatives were designed, synthesized and evaluated for their antiproliferative activity in the HepG2 cancer cell line. Among the 58 compounds, 33 compounds showed potent antiproliferative activity with IC 50 less than 10 μM. Compound 5w showed the most potent anti-proliferative activity in the HepG2 cancer cell line. Thus, we further extended our characterization of the antiproliferative activity of 5w in six cancer cell lines (HepG2, SMMC-7721, Hela, CNE1, CNE2 and MCF7). The representative compound 5w displayed robust anti-proliferative activities in all the tested cell lines with IC 50 values in range of 0.93–1.89 μM which were much lower than that of sophoridine. Here, we report the structure–activity relationships (SAR) in a sophoridine series of compounds, which indicated that introduction of N-benzyl indole group on the 14-carbon atom of sophoridine can significantly enhance the antiproliferative activity. By molecular docking and enzymatic assay, compound 5w was found to be able to inhibit the activity of DNA Topo I. Furthermore, apoptosis assay displayed that compound 5w could significantly induce the apoptosis of HepG2 cells in a dose-dependent manner by activating caspase-3, increasing expression of cleaved caspase-3 and reducing the ratio of Bcl-2/Bax. The in vivo antitumor assay demonstrated that 5w suppressed the growth of HepG2 xenografts in nude mice without any obvious side effects. Graphical abstract Image 1 Highlights • 58 sophoridine derivatives were designed, synthesized and evaluated. • 5w exhibited potent antitumor activity in vitro. • 5w inhibited the activity of DNA Topo I. • 5w arrested tumor growth in vivo. [ABSTRACT FROM AUTHOR]

Using matrine ( 1 ) as the lead compound, a series of new 14-( N -substituted-2-pyrrolemethylene) matrine and 14-( N -substituted-indolemethylene) matrine derivatives was designed and synthesized for their potential application as anticancer agents. The structure of these compounds was characterized by 1 H NMR, 13 C NMR and ESI-MS spectral analyses. The target compounds were evaluated for their in vitro cytotoxicity against three human cancer cell lines (SMMC-7721, A549 and CNE2). The results revealed that compound A6 and B21 displayed the most significant anticancer activity against three cancer cell lines with IC 50 values in range of 3.42–8.05 μM, which showed better activity than the parent compound (Matrine) and positive control Cisplatin. Furthermore, the Annexin V-FITC/PI dual staining assay revealed that compound A6 and B21 could significantly induce the apoptosis of SMMC-7721 and CNE2 cells in a dose-dependent manner. The cell cycle analysis also revealed that compound A6 could cause cell cycle arrest of SMMC-7721 and CNE2 cells at G2/M phase. [ABSTRACT FROM AUTHOR]

Two triterpenoid acids, betulinic acid and ursolic acid, were purified from the ethanol extract ofEngelhardtia serrataBl. by bioassay-guided isolation. Their cytotoxic and apoptosis-inducing activities on the K562 cell line were evaluated by MTT and flow cytometric analysis. Betulinic acid and ursolic acid inhibited the growth of K562 tumor cell line with IC 50 values of 6.25 and 12.5  μg/ml and also induced 35%and 13%apoptosis at 25  μg/ml, respectively. [ABSTRACT FROM AUTHOR]

The title compound, 4-(3-amino-4-morpholino-1H-indazole-1-carbonyl)benzonitrile was synthesised by condensation of 4-cyanobenzoic acid with 4-morpholino-1H-indazol-3-amine, which was prepared from 2,6-difluorobenzonitrile by amination with morpholine and then cyclisation with hydrazine hydrate. The crystal structure of the title compound was determined and the crystals belong to the monoclinic system, space group P21/c. In addition, the compound showed some inhibition of the proliferation of some cancer cell lines. [ABSTRACT FROM AUTHOR]

Tumor cell adhesion to the microvessel wall is a critical step during tumor metastasis. Vascular endothelial growth factor (VEGF), a secretion of tumor cells, can increase microvessel permeability and tumor cell adhesion in the microvessel. To test the hypothesis that inhibiting permeability increase can reduce tumor cell adhesion, we used in vivo fluorescence microscopy to measure both microvessel permeability and adhesion rates of human mammary carcinoma MDA-MB-231 cells in post-capillary venules of rat mesentery under the treatment of VEGF and a cAMP analog, 8-bromo-cAMP, which can decrease microvessel permeability. By immunostaining adherens junction proteins between endothelial cells forming the microvessel wall, we further investigated the structural mechanism by which cAMP abolishes VEGF-induced increase in microvessel permeability and tumor cell adhesion. Our results demonstrate that 1) Pretreatment of microvessels with cAMP can abolish VEGF-enhanced microvessel permeability and tumor cell adhesion; 2) Tumor cells prefer to adhere to the endothelial cell junctions instead of cell bodies; 3) VEGF increases microvessel permeability and tumor cell adhesion by compromising endothelial junctions while cAMP abolishes these effects of VEGF by reinforcing the junctions. These results suggest that strengthening the microvessel wall integrity can be a potential approach to inhibiting hematogenous tumor metastasis. [ABSTRACT FROM AUTHOR]