The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and,...The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and, in some cases, prevent the development of the human hypernephroma in the cheek pouch of golden hamsters. The effect of enteropathgenic proteims may possibly consist in inducing the production of endogenous immune interferon which activates the host immune system and enhances the rejection of heterologous tumour cells.展开更多
Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the mol...Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the molecular weight of chitosan supports.展开更多
Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was ...Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was proved by IR ^(13)CNMR spectroscopy.展开更多
Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ...Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ethanol media. The compounds were characterized by elemental analyses, molecular weight, IR and 1 H NMR spectroscopy. The results indicate that n Bu 2 SnL 2 have distorted trans octahedral structure. The antitumor activity in vitro against human A 549 tumor cells and P388 leukemia was presented, and their structure activity relationship was discussed.展开更多
The diorganotin(Ⅳ) complexes of N-(3,5-dibromosalicylidene)-α-amino acid, R2Sn(2-O-3,5-Br2C6H2CH= NCHRCOO)(where R=H, Me, i-Pr, Bz; R'=n-Bu, Cy), were synthesized by the reactions of diorganotin dichlorides...The diorganotin(Ⅳ) complexes of N-(3,5-dibromosalicylidene)-α-amino acid, R2Sn(2-O-3,5-Br2C6H2CH= NCHRCOO)(where R=H, Me, i-Pr, Bz; R'=n-Bu, Cy), were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-(3,5-dibromosalicylidene)-α-amino acid and characterized by elemental analysis, IR and NMR (^1H, ^13C and ^119Sn) spectra. The crystal structures of n-Bu2Sn(2-O-3,5-Br2C6H2CH= NCHRCOO)(R=i-Pr, Bz) and Cy2Sn(2-O-3,5-Br2C6H2CH=NCHRCOO)(R=Me, Bz) were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.展开更多
A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety(7a--7r) were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 (human breast cancer), H460(human ...A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety(7a--7r) were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 (human breast cancer), H460(human lung cancer) and HT-29(human colon cancer) cell lines by standard 3-(4,5-dimethylthiazae-2-yl)-2,5-diphenyltetrazo- lium bromide(MTT) assay. Representative compounds(Td, 7k, 7m, 7p) with higher cytotoxicity were further examined against one normal cell line(WI-38, human fetal lung fibroblasts). The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC5o values of 0.78, 0.056 and 0.018 μmol/L, respectively. The potency is much higher than that of Sunitinib(IC50=3.46 μmol/L against MDA-MB-231, IC50=2.59 μmol/L against H460, IC50=1.50 μmol/L against HT-29) by 4.4, 46.3 and 83.3 fold.展开更多
文摘The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and, in some cases, prevent the development of the human hypernephroma in the cheek pouch of golden hamsters. The effect of enteropathgenic proteims may possibly consist in inducing the production of endogenous immune interferon which activates the host immune system and enhances the rejection of heterologous tumour cells.
基金This work was supported by the National Natural Science Foundation of China (grant No. 29977014) and China Capital Investment, Ltd., in Shanghai.
文摘Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the molecular weight of chitosan supports.
文摘Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was proved by IR ^(13)CNMR spectroscopy.
基金ProjectsupportedbytheNationalNaturalScienceFoundationofChina (No .2 97710 2 3)andtheNaturalScienceFoundationofShanxiProvince
文摘Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ethanol media. The compounds were characterized by elemental analyses, molecular weight, IR and 1 H NMR spectroscopy. The results indicate that n Bu 2 SnL 2 have distorted trans octahedral structure. The antitumor activity in vitro against human A 549 tumor cells and P388 leukemia was presented, and their structure activity relationship was discussed.
基金Project supported by the Natural Science Foundation of Shandong Province (No. Z2002F01), the State Key Laboratory of Crystal Materials (No. 2005B 103) and the Scientific Research Foundation of Qufu Normal University.
文摘The diorganotin(Ⅳ) complexes of N-(3,5-dibromosalicylidene)-α-amino acid, R2Sn(2-O-3,5-Br2C6H2CH= NCHRCOO)(where R=H, Me, i-Pr, Bz; R'=n-Bu, Cy), were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-(3,5-dibromosalicylidene)-α-amino acid and characterized by elemental analysis, IR and NMR (^1H, ^13C and ^119Sn) spectra. The crystal structures of n-Bu2Sn(2-O-3,5-Br2C6H2CH= NCHRCOO)(R=i-Pr, Bz) and Cy2Sn(2-O-3,5-Br2C6H2CH=NCHRCOO)(R=Me, Bz) were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.
基金Supported by the Program for Innovative Research Team of the Ministry of Education of China and the Program for Liaoning Innovative Research Team in University, China(No.IRT1073), and the National Natural Science Foundation of China (No.81202405)
文摘A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety(7a--7r) were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 (human breast cancer), H460(human lung cancer) and HT-29(human colon cancer) cell lines by standard 3-(4,5-dimethylthiazae-2-yl)-2,5-diphenyltetrazo- lium bromide(MTT) assay. Representative compounds(Td, 7k, 7m, 7p) with higher cytotoxicity were further examined against one normal cell line(WI-38, human fetal lung fibroblasts). The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC5o values of 0.78, 0.056 and 0.018 μmol/L, respectively. The potency is much higher than that of Sunitinib(IC50=3.46 μmol/L against MDA-MB-231, IC50=2.59 μmol/L against H460, IC50=1.50 μmol/L against HT-29) by 4.4, 46.3 and 83.3 fold.