Chain length, size, composition, surface charge, and other properties of polymeric materials affect their recognition and uptake by cells and must be optimized to deliver polymers selectively to their target. However, it is often not possible to precisely modify selected properties without changing other parameters. To overcome these difficulties, well‐defined poly(pentafluorostyrene)‐based polymers are prepared that can be grafted via thiol/para‐fluorine “click” reaction with 1‐thio‐β‐D ‐glucose and 1‐thio‐β‐D ‐galactose. Fluorescence microscopy and flow cytometry show that nanoparticles are taken up by HepG2 cells to a higher degree than the respective water‐soluble polymers, and that internalization of both galactosylated homo‐ and nanoprecipitated block copolymers is enhanced.
Two novel rare earth tungstosilicic polyoxometalate containing 5-fluorouracil,K26(C4H4FN2O2)8Pr(SiW11O39)4·10H2O(FPSW) and K26(C4H4FN2O2)8Sm(SiW11O39)4·9H2O(FSSW),were synthesized and their structure were characterized by using elemental analysis,FTIR spectra,X-ray powder diffraction and TG.The antitumor activity tests of the compounds FPSW and FSSW were carried out by the methyl thiazolyl tetrazolium method in hepatocellular carcinoma cell HepG-2.The results showed that FPSW and FSSW could inhibit the HepG-2 cells in vitro significantly.The EC50 of FPSW and FSSW is 1.94×10-5 and 1.32×10-5 mol·L-1 respectively.The therapeutic index of FPSW and FSSW is 0.76 and 1.58 respectively. 相似文献
To develop new radiopharmaceuticals for the interventional radionuclide therapy of recurrent hepatocellular carcinoma, poly(HPMA)-APMA-DTPA[HPMA=N-(2-hydroxypropyl) methacrylamide; APMA=N-(3-aminopro-pyl)methacrylamide; DTPA=diethylenetriaminepentaacetic acid] was synthesized by free radical precipitation polymerization in acetone/dimethylsulfoxide with N,N′-azobis(isobutyronitrile) as the initiator. The copolymers were characterized with nuclear magnetic resonance(NMR) spectroscopy and gel permeation chromatography(GPC, Mn=2.2×104, Mw/Mn=1.38). Subsequently, poly(HPMA)-APMA-DTPA was conjugated with 99mTc radionuclide. Prolonged retention of poly(HPMA)-APMA-DTPA conjugate within the tumor tissues was demonstrated by single-photon emission computed tomography computed tomography(SPECT-CT) at 1, 2, 4 and 24 h following intra-tumoral injection of the conjugate to hepatocellular carcinoma xenografts in mice. DTPA-99mTc was also synthesized and characterized for comparison. The data suggest that the poly(HPMA)-APMA-DTPA conjugates might be useful for the interventional radionuclide therapy of recurrent hepatocellular carcinoma in humans. 相似文献
To assess the predictability of the response to radiotherapy of uterine carcinoma, this study retrospectively analyzed dynamic contrast-enhanced magnetic resonance images (DCE-MRI) taken before radiotherapy.
Materials and Methods
Forty-two patients with uterine carcinoma were studied, of whom 22 had adenocarcinoma and 20 had squamous cell carcinoma (SCC). In DCE-MRI analysis, two parameters, SIe and Rdown, were measured. SIe is a median value for the degree of signal intensity change in all selected pixels in the tumor at 1–2 min after contrast agent injection. Rdown is the ratio of the number of down-sloped pixels to that of all selected pixels 3–7 min after injection. The tumor volume reduction rate (TVRR) was measured by MRI-based volumetry in pre- and post-radiotherapy transverse T2-weighted images.
Results
Overall, TVRR was significantly correlated to both SIe (r=0.37, P=.015) and Rdown (r=0.73, P<.0001). In the separate patient groups, SIe but not Rdown was significantly different between the adenocarcinoma and SCC patients (t=3.64, P<.001). TVRR was not correlated to SIe in any group. TVRR was significantly correlated to Rdown in adenocarcinoma patients (r=0.78, P<.001) but not in SCC patients.
Conclusion
SIe may reflect differences in histological characteristics. Rdown may be useful for predicting the response to radiotherapy of uterine carcinoma. 相似文献
The DNA of P3 promoter region of IGF-Ⅱ gene was obtained by means of PCR technique. The examination of DNA polymorphism by restriction endonuclease BstE Ⅱ and the examination of AFP by bioluminescence immunoassay technique were carried out. The results have a significant difference(P<0.005). But the positive rate of AFP is higher than that of DNA polymorphism. The experimental result shows that the change of the DNA polymorphism of IGF-Ⅱis not the only carcinogenic factor. The suggested unite examination is the best method for the diagnosis of the primary hepatocellular carcinoma. 相似文献
Abstract A new series of xanthone derivatives against the oral human epidermoid carcinoma (KB) cancer cell line is examined to determine
the relationship between the structural properties and the biological activity of these compounds—the 3-D quantitative structure–activity
relationship (3D-QSAR)—using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis
(CoMSIA). The best CoMFA and CoMSIA models were obtained using the atom-based alignment of 33 compounds, 22 training compounds
and 11 tested compounds, and these give desirable statistics; those for the CoMFA standard model were: rcv2 = 0.691, r2 = 0.998, Spress = 0.178, s = 0.014 and F = 1080.765, while CoMSIA combined steric, electrostatic, hydrophobic and hydrogen-bond acceptor fields: rcv2 = 0.600, r2 = 0.988, Spress = 0.206, s = 0.034 and F = 284.433. The 3D-QSAR models calculated satisfactory test set activities. The 3D-QSAR contour plots correlated strongly
with the experimental data for the binding topology. For this reason, these results would be beneficial for predicting affinities
with the compounds of interest, and they are advantageous for guiding the design and synthesis of new and more effective anticancer
agents.
Graphical abstract
A new and more effective anticancer agent of xanthone derivatives against the oral human epidermoid carcinoma (KB) cell line,
as investigated by CoMFA and CoMSIA analysis 相似文献
Peptidyl‐prolyl cis‐trans isomerase Pin1 plays a crucial role in the development of human cancers. Recently, we have disclosed that Pin1 regulates the biogenesis of miRNA, which is aberrantly expressed in HCC and promotes HCC progression, indicating the therapeutic role of Pin1 in HCC therapy. Here, 7‐(benzyloxy)‐3,5‐dihydroxy‐2‐(4‐methoxyphenyl)‐8‐(3‐methylbut‐2‐en‐1‐yl)‐4H‐chromen‐4‐one ( AF‐39 ) was identified as a novel Pin1 inhibitor. Biochemical tests indicate that AF‐39 potently inhibits Pin1 activity with an IC50 values of 1.008 μm , and also displays high selectivity for Pin1 among peptidyl prolyl isomerases. Furthermore, AF‐39 significantly suppresses cell proliferation of HCC cells in a dose‐ and time‐dependent manner. Mechanistically, AF‐39 regulates the subcellular distribution of XPO5 and increases miRNAs biogenesis in HCC cells. This work provides a promising lead compound for HCC treatment, highlighting the therapeutic potential of miRNA‐based therapy against human cancer. 相似文献