Chiral phosphoric acid-catalyzed enantioselective phosphinylation of 3,4-dihydroisoquinolines with diarylphosphine oxides.

Chiral phosphorous-containing compounds are playing a more and more significant role in several different research fields. Here, we show a chiral phosphoric acid-catalyzed enantioselective phosphinylation of 3,4-dihydroisoquinolines with diarylphosphine oxides for the efficient and practical construction of a family of chiral α-amino diarylphosphine oxides with a diverse range of functional groups. The phosphine products are suitable for transforming to several kinds of chiral (thio)ureas, which might be employed as chiral ligands or catalysts with potential applications in asymmetric catalysis. Control and NMR tracking experiments show that the reaction proceeds via the tert-butyl 1-(tert-butoxy)-3,4-dihydroiso-quinoline-2(1H)-carboxylate intermediate, followed by C-P bond formation. Furthermore, computational studies elucidated that the hydrogen bonding strength between the phosphonate and isoquinolinium determines the stereoselectivity of the phosphinylation reaction.

In Situ Hypoiodite-Catalyzed Oxidative Rearrangement of Chalcones: Scope and Mechanistic Investigation.

It is highly desirable to avoid using rare or toxic metals for oxidative reactions in the synthesis of pharmaceuticals and fine chemicals. Hypervalent iodine compounds are environmentally benign alternatives, but their catalytic use has been quite limited. Herein, the protocol for in situ hypoiodite-catalyzed oxidative rearrangement of chalcones is first realized under mild and metal-free conditions, which provided a nontoxic, environmental-benign, and catalytic alternative to the thallium-based protocol. Also, the applicability and effectiveness of this catalytic protocol got well demonstrated via gram-scale synthesis and product derivatization. What is more, control and NMR tracking experiments were performed to figure out the possible catalytic species and intermediates.

Homogeneous Dearomative Hydrogenation with a Co/P4 N2 Catalyst: A Nucleophilic Approach.

Arene hydrogenation is the most straightforward method to prepare carbo- and heterocycles. However, the high resonance energy prevents aromatic substrates from hydrogenation. Herein the homogeneous, nucleophilic hydrogenation of less electron-rich arenes and heteroarenes is reported. The Co(P4 N2 )H species that has been demonstrated to be a strong hydride donor could deliver a hydride ion to the cyano (hetero)arene substrates. Deuterium labeling experiments supported a Michael-type reaction pathway. Theoretical analyses have been conducted to investigate the hydricity of the catalytically active CoH species and the electrophilicity of the arene substrates. An outlook for the synthesis of more challenging substituted benzenes was proposed based on the in silico modification of the CoH species.

Integration of Milstein Ru-PNN and Rh-Tribi/Tetrabi for Isomerization Linear Selective Hydroformylation of Far Internal Alkenes.

Converting cheap and abundant internal alkenes to value-added linear aldehydes is of great importance but not an addressed issue. In this paper, an integration of a Milstein-type Ru-PNN catalyst and our Rh-Tribi/Tetrabi catalyst was first demonstrated in highly improved isomerization linear selective hydroformylation of 2-, 3-, and 4-alkenes, yielding excellent linear selectivities and activities (linear selectivity improvements of 2.2-58%, up to 94.2-98.6%, and turnover numbers improvements of 61-335 TON, up to 385-851) compared to the Ru-PNN/Rh-Bisbi system.

Enantioselective Hydrogenation of Tetrasubstituted α,ß-Unsaturated Carboxylic Acids Enabled by Cobalt(II) Catalysis: Scope and Mechanistic Insights.

Chiral carboxylic acids are important compounds because of their prevalence in pharmaceuticals, natural products and agrochemicals. Asymmetric hydrogenation of α,ß-unsaturated carboxylic acids has been widely recognized as one of the most efficient synthetic approaches to afford such compounds. Although related asymmetric hydrogenation of di- and trisubstituted unsaturated acids with noble metals is well established, asymmetric hydrogenation of challenging tetrasubstituted α,ß-unsaturated carboxylic acids is rarely reported. We demonstrate enantioselective hydrogenation of cyclic and acyclic tetrasubstituted α,ß-unsaturated carboxylic acids via cobalt(II) catalysis. This protocol showed broad substrate scope and gave chiral carboxylic acids in good yields with excellent enantiocontrol (up to 98 % yield and 99 % ee). Combined experimental and computational mechanistic studies support a CoII catalytic cycle involving migratory insertion and σ-bond metathesis processes. DFT calculations reveal that enantioselectivity may originate from the steric effect between the phenyl groups of the ligand and the substrate.

Pyrazolone derivative C29 protects against HFD-induced obesity in mice via activation of AMPK in adipose tissue.

Beige adipocytes have been considered as a potential strategy in anti-obesity therapy because of its thermogenic capacity. AMP-activated protein kinase (AMPK) plays important roles in regulating adipose tissue function. C29 is a novel pyrazolone derivative with AMPK activity. In the current study, we investigated the role of C29 in the regulation of thermogenesis using differentiated adipocytes and diet-induced obese mice, and explored the mechanisms that might be involved in energy expenditure via adipocyte AMPK activation. We showed that treatment with C29 (2.5-10 µM) concentration-dependently increased thermogenesis in differentiated preadipocytes separated from inguinal white adipose tissue (iWAT), evidenced by increased expression levels of thermogenesis markers such as Ucp1, Pgc-1α, Dio2, Prdm16, Cox7a1, Cox8b, Elovl3, and Cidea, fatty acid oxidation (FAO) genes including Cpt1a, Lcad and Pparα, as well as beige-selective genes such as Cd137, Tmem26, Slc27a1, and Tbx1. In high-fat diet (HFD)-fed mice, oral administration of C29 (30 mg·kg-1·day-1) for 9 weeks alleviated HFD-induced obesity, promoted energy expenditure and modulated iWAT browning. However, these effects were not observed in adipose-specific AMPKα1/α2 knockout (AKO) mice following C29 administration. Together, this study demonstrates that C29 regulates energy balance via adipocyte AMPK. Our findings show that the discovery of AMPK activators that specifically target adipose tissue may have therapeutic potential for treating obesity-related metabolic diseases.

Cobalt-catalyzed highly enantioselective hydrogenation of α,ß-unsaturated carboxylic acids.

Asymmetric hydrogenation of α,ß-unsaturated acids catalyzed by noble metals has been well established, whereas, the asymmetric hydrogenation with earth-abundant-metal was rarely reported. Here, we describe a cobalt-catalyzed asymmetric hydrogenation of α,ß-unsaturated carboxylic acids. By using chiral cobalt catalyst bearing electron-donating diphosphine ligand, high activity (up to 1860 TON) and excellent enantioselectivity (up to >99% ee) are observed. Furthermore, the cobalt-catalyzed asymmetric hydrogenation is successfully applied to a broad spectrum of α,ß-unsaturated carboxylic acids, such as various α-aryl and α-alkyl cinnamic acid derivatives, α-oxy-functionalized α,ß-unsaturated acids, α-substituted acrylic acids and heterocyclic α,ß-unsaturated acids (30 examples). The synthetic utility of the protocol is highlighted by the synthesis of key intermediates for chiral drugs (6 cases). Preliminary mechanistic studies reveal that the carboxy group may be involved in the control of the reactivity and enantioselectivity through an interaction with the metal centre.

Diphyllin Improves High-Fat Diet-Induced Obesity in Mice Through Brown and Beige Adipocytes.

Brown adipose tissue (BAT) and beige adipose tissue dissipate metabolic energy and mediate nonshivering thermogenesis, thereby boosting energy expenditure. Increasing the browning of BAT and beige adipose tissue is expected to be a promising strategy for combatting obesity. Through phenotype screening of C3H10-T1/2 mesenchymal stem cells, diphyllin was identified as a promising molecule in promoting brown adipocyte differentiation. In vitro studies revealed that diphyllin promoted C3H10-T1/2 cell and primary brown/beige preadipocyte differentiation and thermogenesis, which resulted increased energy consumption. We synthesized the compound and evaluated its effect on metabolism in vivo. Chronic experiments revealed that mice fed a high-fat diet (HFD) with 100 mg/kg diphyllin had ameliorated oral glucose tolerance and insulin sensitivity and decreased body weight and fat content ratio. Adaptive thermogenesis in HFD-fed mice under cold stimulation and whole-body energy expenditure were augmented after chronic diphyllin treatment. Diphyllin may be involved in regulating the development of brown and beige adipocytes by inhibiting V-ATPase and reducing intracellular autophagy. This study provides new clues for the discovery of anti-obesity molecules from natural products.

Homogeneous Hydrogenation with a Cobalt/Tetraphosphine Catalyst: A Superior Hydride Donor for Polar Double Bonds and N-Heteroarenes.

The development of catalysts based on earth abundant metals in place of noble metals is becoming a central topic of catalysis. We herein report a cobalt/tetraphosphine complex-catalyzed homogeneous hydrogenation of polar unsaturated compounds using an air- and moisture-stable and scalable precatalyst. By activation with potassium hydroxide, this cobalt system shows both high efficiency (up to 24 000 TON and 12 000 h-1 TOF) and excellent chemoselectivities with various aldehydes, ketones, imines, and even N-heteroarenes. The preference for 1,2-reduction over 1,4-reduction makes this method an efficient way to prepare allylic alcohols and amines. Meanwhile, efficient hydrogenation of the challenging N-heteroarenes is also furnished with excellent functional group tolerance. Mechanistic studies and control experiments demonstrated that a CoIH complex functions as a strong hydride donor in the catalytic cycle. Each cobalt intermediate on the catalytic cycle was characterized, and a plausible outer-sphere mechanism was proposed. Noteworthy, external inorganic base plays multiple roles in this reaction and functions in almost every step of the catalytic cycle.

Redetermination of the Structure of a Water-Soluble Hypervalent Iodine(V) Reagent AIBX and Its Synthetic Utility in the Oxidation of Alcohols and Synthesis of Isoxazoline N-Oxides.

The structure of a water-soluble hypervalent iodine(V) reagent AIBX is re-examined through its single-crystal X-ray analysis and theoretical calculations including Mayer bond order and localized orbital locator (LOL) and AIBX is believed to be a pseudocyclic iodylarene because of the strong electron-withdrawing nature of the trimethylammonium cation on its phenyl ring, which would decrease the electron density of carboxylic anion and make the ortho-carboxyl oxygen anion incapable to form hypervalent bond with iodine atom. However, the cyclic benziodoxole structure of AIBX could be obtained by adding a Brønsted acid, which was supported by the calculation result including the increase of Mayer bond order and the shortening of the I-O bond length. Moreover, the fact that the system of AIBX and TFA could oxidize various alcohols to their corresponding carbonyl compounds would indicate that AIBX constitutes a cyclic benziodoxole structure under acidic conditions. In addition, an efficient method has been developed for the synthesis of isoxazoline N-oxides via AIBX-induced dehydrogenative cyclization using ß-keto esters as substrates and methyl nitroacetate as a nucleophile.

Malonylginsenosides with Potential Antidiabetic Activities from the Flower Buds of Panax ginseng.

LC-MS-guided phytochemical isolation of malonylginsenosides, featuring neutral elimination of CO2 and C3H2O3 by the negative mode collision-induced dissociation, from the flower buds of Panax ginseng led to the isolation of 19 malonyl-substituted triterpenoid saponins. They include 15 new malonylginsenosides, malonylfloralginsenosides-Re1-Re3 (1-3), -Rb1 and -Rb2 (4, 5), -Rd1-Rd6 (6-11), and -Rc1-Rc4 (12-15), and the known m-Rb1, m-Rc, m-Rb2, and m-Rd (16-19). Compound 11 represents the first dimalonyl saponin isolated from the Panax genus, while 2-4, 9, and 10 are five ginsenosides with single malonylation at the C-20 sugar chain. The antidiabetic activities of nine of these malonyl-substituted ginsenosides (1, 3, 4, 8, 13, and 16-19) and five of the corresponding non-malonyl ginsenosides (Re, Rb1, Rb2, Rc, and Rd) were evaluated by L6 myotubes' glucose consumption and AMPKα2ß1γ1 activation. Ginsenoside Rb2, 1, and 18 promoted glucose consumption of differentiated L6 myotubes, while ginsenosides Rb1, Rb2, and Rd and the malonylginsenosides 4, 8, 13, 16, 17, and 19 activated AMPKα2ß1γ1 (EC50: 0.0168-2.8 µM, fold: 1.7-4.7).

Recyclable Hypervalent-Iodine-Mediated Dehydrogenative Cyclopropanation under Metal-Free Conditions.

A method is developed for the synthesis of cyclopropanes from the C(sp2)-C(sp3) single bonds of ß-keto esters with activated methylene compounds under metal-free conditions in the presence of 5-trimethylammonio-1,3-dioxo-1,3-dihydro-1λ5-benzo[d][1,2]iodoxol-1-ol anion (AIBX), a recyclable water-soluble hypervalent iodine(V) reagent developed by our group. This mild, efficient method has a wide substrate scope and good functional group tolerance and is complementary to existing cyclopropanation strategies. The method can be used to construct polysubstituted ring-fused cyclopropanes and is amenable to further synthetic transformations for construction of complex biologically active molecules as well as asymmetric cyclopropanes (90% de) when a chiral ester auxiliary is used.

Recyclable Hypervalent-Iodine-Mediated Dehydrogenative α,ß'-Bifunctionalization of ß-Keto Esters Under Metal-Free Conditions.

We have developed a method for recyclable hypervalent-iodine-mediated direct dehydrogenative α,ß'- bifunctionalization of ß-ketoesters and ß-diketones under metal-free conditions, which affords a straightforward way to synthesize benzo-fused 2,3-dihydrofurans. This efficient, mild method, which has a wide substrate scope and good functional-group tolerance, was used for the multistep synthesis of the protected aglycone of a naturally occurring phenolic glycoside. A mechanism involving Michael addition to an enone intermediate and subsequent oxidative cyclization is proposed.

Electrochemiluminescence properties of [Pt2Ag4(C≡CC6H4R)8]n (R = CH3, n = 1; R = H, n = 1 and 2) with amine (TPrA and DBAE) as the coreactant and determination of Sudan I.

Two hexanuclear clusters, [Pt(2)Ag(4)(C≡CC(6)H(4)R)(8)] (R = CH(3), 1; R = H, 2), together with dimer [Pt(2)Ag(4)(C≡CC(6)H(5))(8)](2) (3), have been synthesized and characterized by elemental analyses, electrospray ionization mass spectrometry, and (1)H NMR spectroscopy and by X-ray crystallography for 1 and 3. A considerable enhancement of photoluminescence (PL) and a notable red shift in the emission maximum of 1 (λ(max) 600 nm) relative to 2 (λ(max) 545 nm) are observed. Electrogenerated chemiluminescence (ECL) of 1 and 2 in the absence or presence of coreactant tri-n-propylamine (TPrA) or 2-(dibutylamino)ethanol (DBAE) at different working electrodes in different solvents (CH(2)Cl(2), CH(2)ClCH(2)Cl, or CH(3)CN) has been studied. The ECL spectra are identical with the PL spectra, indicating that ECL emissions are also due to a MLM'CT [Pt(d)/π (C≡CC(6)H(4)R-4) → Pt(p(z))/Ag(sp)/π* (C≡CC(6)H(4)R-4)] state modified by Pt···Ag and Ag···Ag contacts. ECL of 1- and 2/amine systems in CH(2)ClCH(2)Cl was produced at the potentials of 1.14-1.19 V vs SCE, notably negatively shifted by about 0.38 V compared to those of the Ru(bpy)(3)(2+)/amine system. In all cases, ECL quantum efficiencies of 2 are higher than those of 1 and on the same order of magnitude as that of the [Ru(bpy)(3)](PF(6))(2)/amine system. It is noted that Sudan I tends to decrease the ECL intensity of the 1/DBAE system in CH(2)ClCH(2)Cl at a platinum working electrode. A new ECL method for the determination of Sudan I was developed with a linear range of 2.5 × 10(-5)-1.0 × 10(-3) M and a detection limit of 8.0 × 10(-6) M based on 3 times the ratio of signal-to-noise.

Mono- and dinuclear Ru(II) complexes of 1,4-bis(3-(2-pyridyl)pyrazol-1-ylmethyl)benzene): synthesis, structure, photophysical properties and electrochemiluminescent determination of diuretic furosemide.

Mononuclear ruthenium complex 1 and dinuclear complex 2 were synthesized by reaction of the appropriate bidentate pyrazolyl-pyridyl-based ligand L (L = 1,4-bis(3-(2-pyridyl)pyrazol-1-ylmethyl)benzene) with cis-Ru(bipy)(2)Cl(2)·2H(2)O. They were characterized by elemental analyses, ESI-MS, (1)H spectroscopy, and X-ray crystallography for 2. Compounds 1 and 2 both emit strongly in solid states and in solutions at 298 K with the lifetimes in the microsecond range. Electrogenerated chemiluminescence (ECL) of complexes 1 and 2 in the absence or presence of coreactant tri-n-propylamine (TPrA) or 2-(dibutylamino)ethanol (DBAE) at different working electrodes in acetonitrile and phosphate buffer solutions (PBS, pH 7.5) was studied. The ECL spectra are identical to the photoluminescence spectra, indicating that the ECL emissions are due to the metal to ligand charge transfer (MLCT). In all cases, ECL quantum efficiencies of dinuclear complex 2 are higher than those of mononuclear complex 1, and ECL quantum efficiencies of complexes 1 and 2/TPrA system are higher than those of DBAE system. It is noted that diuretic furosemide tends to decrease the ECL intensity of complex 2/TPrA system in PBS (pH 7.5) at GC working electrode. A novel ECL method for the determination of diuretic furosemide was developed with a linear range between 2.0 × 10(-7) mol L(-1) and 1.0 × 10(-6) mol L(-1), and a detection limit of 1.2 × 10(-8) mol L(-1) based on 3 times the ratio of signal-to-noise.

Synthesis, structure, photophysical and electrochemiluminescence properties of Re(I) tricarbonyl complexes incorporating pyrazolyl-pyridyl-based ligands.

Three rhenium carbonyl complexes 1-3 were synthesized by reaction of the appropriate bidentate pyrazolyl-pyridyl-based ligand L1, L2 (L1 = 2-[1-{4-(bromomethyl)benzyl}-1H-pyrazol-3-yl]pyridine; L2 = 1,4-bis(3-(2-pyridyl)pyrazol-1-ylmethyl)benzene) with [Re(CO)(5)Cl] in toluene. They were characterized by elemental analyses, ESI-MS, (1)H spectroscopy, and X-ray crystallography for 1 and 2. Compounds 1-3 exhibit bright yellow-green luminescence in the solid state and in solution at 298 K with the lifetimes in the microsecond range. It is noteworthy that the luminescent quantum efficiencies of compounds 1-3 are between 0.040 and 0.051, which are much higher than that of the [Re(bpy)(CO)(3)Cl] complex (= 0.019) (M. M. Richter et al., Anal. Chem., 1996, 68, 4370; J. Van Houten et al., J. Am. Chem. Soc., 1976, 98, 4853). Electrogenerated chemiluminescence (ECL) was observed in solutions of these complexes in the absence or presence of coreactant tri-n-propylamine (TPrA) or 2-(dibutylamino)ethanol (DBAE) by stepping the potential of a Pt disk working electrode. The ECL spectra are identical to the photoluminescence spectra, indicating that the chemical reactions following electrochemical oxidation or reduction form the same (3)MLCT excited states as that generated in the photoluminescence experiments. In most cases, the ECL quantum efficiencies of complexes 1-3 are comparable to that of the [Re(L)(CO)(3)Cl] (L = bpy or phen) system. Oxygen tends to substantially decrease ECL intensities of the three rhenium complexes-TPrA system, which could allow them to be used as oxygen sensors.

Association of vascular endothelial growth factor gene polymorphisms with susceptibility to epithelial ovarian cancer.

BACKGROUND: Vascular endothelial growth factor (VEGF) is a major angiogenic factor involved in a number of pathological processes, including neovascularization, a crucial step in the development of solid malignancies. The aim of this study was to investigate the association of polymorphisms in the VEGF gene with susceptibility to epithelial ovarian cancer (EOC). METHODS: This case-control study included 303 EOC patients and 303 healthy controls. Genotyping of the VEGF gene polymorphisms at j460C/T, j1154G/A, j2578C/A, and +936C/T were performed by polymerase chain reaction and restriction fragment length polymorphism analysis. RESULTS: No significant difference was found in allele and genotype distributions of the -460C/T, +936C/T, and -2578C/A polymorphisms between patients and controls. However, the frequencies of -1154G/A genotype and allele were significantly different between the two groups (P = 0.037, P = 0.013). Compared with the G/A + A/A genotype, the G/G genotype could significantly increase the risk of developing EOC (odds ratio, 1.64; 95% confidence interval, 1.12Y2.39). The haplotype analysis suggested that the -460T/ -1154A/ -2578C haplotype exhibited a decrease in the risk of developing EOC compared with the -460T/ -1154G/ -2578C haplotype (odds ratio, 0.644; 95% confidence interval, 0.415-0.999). CONCLUSIONS: The study suggested a possible association between the VEGF -1154G/A polymorphism with susceptibility to EOC, but there is no support for an association of the VEGF -460C/T, +936C/T, and -2578C/A polymorphisms with the risk for EOC.

Polymorphisms in promoter region of FAS and FASL gene and risk of cardia gastric adenocarcinoma.

BACKGROUND AND AIM: The FAS and FASL system play an important role in regulating apoptotic cell death. This study was designed to investigate the correlation of FAS-1377 G/A, -670 A/G and FASL-844 T/C polymorphisms with susceptibility to gastric cardiac adenocarcinoma in a population of a high-incidence region of Hebei Province. METHODS: FAS-1377 G/A, -670 A/G and FASL-844 T/C polymorphisms were genotyped by polymerase chain reaction-restriction fragment length polymorphism analysis in 262 gastric cardiac carcinoma (GCA) patients and 524 healthy controls. RESULTS: Family history of upper gastrointestinal cancer (UGIC) might increase the risk of developing GCA (age- and sex-adjusted odds ratio [OR] = 1.38, 95% confidence interval [CI] = 1.02-1.86). The overall allelotype and genotype distributions of FAS-1377 G/A, and FASL-844 T/C polymorphisms in GCA patients did not significantly differ from that in healthy controls (P > 0.05). Compared with individuals with a FAS-670 A/A genotype, individuals with an A/G genotype in a smoker group had a lower risk of developing GCA (age, sex, and family history of UGIC adjusted OR = 0.55, 95% CI = 0.34-0.88). When the genotypes of FAS and FASL single nucleotide polymorphisms (SNP) were combined to analyze, no significant correlation was found between these SNP and the risk for GCA development. CONCLUSION: In the high-incidence region of Hebei Province, FAS-1377 G/A and FASL-844 T/C polymorphisms were not associated with the risk of GCA. However, the FAS-670 A/G genotype might decrease the risk of GCA for smoker individuals.

Association of functional polymorphisms in MMPs genes with gastric cardia adenocarcinoma and esophageal squamous cell carcinoma in high incidence region of North China.

The aim of the present study was to investigate the association of single nucleotide polymorphisms (SNPs) in matrix metalloproteinase (MMPs) with the risk of gastric cardia adenocarcinoma (GCA) and esophageal squamous cell carcinoma (ESCC). Genotypes were analyzed by polymerase chain reaction-restriction fragment-length polymorphism method in 592 patients and 624 healthy individuals. Significant differences in allele and genotype distributions of MMP-2 -1306C --> T SNP were observed between ESCC and controls (P = 0.02 and 0.01, respectively). Compared with the C/T + T/T genotypes, C/C genotype significantly increased the risk of ESCC (OR = 1.57, 95% CI = 1.10-2.23), especially in individuals in smoker group and in the group with positive family history. The stratification analysis showed there were risk changes of GCA for -735C/C genotype carrier in nonsmoker, for MMP-12 -82G allele and MMP-13 -77A/G genotype carrier in smoker. Our study indicated that these four functional polymorphisms might play roles in developing ESCC and GCA in high incidence region of North China.

[CDH1 polymorphism and its association with the risk of cervical cancer].

OBJECTIVE: To investigate the effect of CDH1 3'-UTR + 54C/T single nucleotide polymorphism (SNP) on expression of luciferase reporter gene and its association with susceptibility to cervical cancer. METHODS: The luciferase gene expression vectors containing CDH1 3'-UTR+54C/T SNP C or T allelotype were constructed. The effect of CDH1 3'-UTR+54C/T SNP on expression of luciferase reporter gene in 293 T cells were tested by daul luciferase reporter assay system. The CDH1 3'-UTR+54C/T SNP was genotyped by polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) analysis in 280 cervical cancer patients and 330 healthy controls. RESULTS: The luciferase activity analysis showed that the relative luciferase activity (RLA) of 293T cells with C allelotype was 1.46, which was significantly lower than that of the 293 T cells with T allelotype (3.01; t = 2.94, P = 0.042). There was no significant difference in age distribution between the cervical cancer patients and the healthy controls. The genotype frequency distribution of CDH1 3'-UTR+54C/T SNP in healthy controls did not significantly differ from that expected by Hardy-Weinberg equilibrium (P > 0.05). The C allelotype frequency of CDH1 in cervical cancer patients was 80.%, which was significantly higher than that in healthy controls (74.5%; chi2 = 6.59, P = 0.010). The T/T, T/C and C/C genotype frequencies of cervical cancer patients and healthy controls were 4.3%, 30.0%, 65.7% and 5.8%, 39.4%, 54.8%, respectively, which were significantly different (chi2 = 7.45, P = 0.024). Compared with individuals with T/T or T/C genotype, individuals with C/C genotype had significantly higher risks of developing cervical cancer (OR = 1.578, 95% CI = 1.136 - 2.191). CONCLUSION: The C allelotype of CDH1 3'-UTR + 54C/T SNP might decrease the expression of luciferase reporter gene and the C/C genotype might be a potential risk for cervical cancer development