A series of new antitumor compounds having indolecarbazole structures were designed and synthesized. The methoxy substituted indolecarbazole parent nucleus, which was firstly synthesized, is condensed with bromine sub...A series of new antitumor compounds having indolecarbazole structures were designed and synthesized. The methoxy substituted indolecarbazole parent nucleus, which was firstly synthesized, is condensed with bromine substituted amino acid methyl ester to produce the target compounds. The target compounds were performed with methylthiazolyldiphenyl-tetrazolium bromide（MTT） in vitro cytotoxin activity test and the results showed that compounds CZ-1, CZ-3 and CZ-6 have higher activity against human colon cancer（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared to the positive control JDC-108.展开更多
A series of antitumor compounds with indolecarbazole structure modified by amino acid and piperidine were designed and synthesized. The indolecarbazole parent nucleus was firstly synthesized, condensed with bromine su...A series of antitumor compounds with indolecarbazole structure modified by amino acid and piperidine were designed and synthesized. The indolecarbazole parent nucleus was firstly synthesized, condensed with bromine substituted amino acid methyl ester, then hydrolyzed and condensed with piperidine to produce the target compounds. In vitro cytotoxin activity test was performed against 7 target compounds with methylthiazolyldiphenyl-tetrazolium bromide（MTT）, and the results showed that compounds CZ-2, CZ-3 and CZ-5 have higher activity against human colon cancers（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared with the positive control JDC-108.展开更多
BACKGROUND In recent years,associations between specific virulence markers of Helicobacter pylori(H.pylori)and gastrointestinal disorders have been suggested.AIM To investigate the presence of virulence factors includ...BACKGROUND In recent years,associations between specific virulence markers of Helicobacter pylori(H.pylori)and gastrointestinal disorders have been suggested.AIM To investigate the presence of virulence factors including vacuolating cytotoxin A genotypes(s1m1,s1m2,s2m1,and s2m2),cytotoxin-associated gene A(CagA),and urease activity in H.pylori strains isolated from Arab and Jewish populations in northern Israel and to assess associations between these factors and patients’demographics and clinical outcomes.METHODS Patients(n=108)who underwent gastroscopy at the Baruch Padeh Medical Center,Poriya due to symptomatic gastroduodenal pathologies as part of H.pylori diagnosis were enrolled in the study.Gastric biopsy specimens were collected from the antrum of the stomach.Clinical condition was assessed by clinical pathology tests.Bacteria were isolated on modified BD Helicobacter Agar(BD Diagnostics,Sparks,MD,United States).Bacterial DNA was extracted,and PCR was performed to detect CagA and vacuolating cytotoxin A genes.Urease activity was assessed using a rapid urease test.RESULTS A significant correlation was found between disease severity and patient ethnicity(P=0.002).A significant correlation was found between CagA presence and the s1m1 genotype(P=0.02),which is considered the most virulent genotype.Further,a higher level of urease activity was associated with isolates originating from the Jewish population.Moreover,higher urease activity levels were measured among CagA-/s1m1 and CagA-/s2m2 isolates.CONCLUSION Our study highlights the importance of incorporating molecular methods for detection of virulence markers of H.pylori in order to tailor optimal treatments for each patient.Further investigation should be performed regarding associations between H.pylori virulence factors and ethnicity.展开更多
基金supported by the science and technology support project of Jiangsu Province(No.BY2015057-03)
文摘A series of new antitumor compounds having indolecarbazole structures were designed and synthesized. The methoxy substituted indolecarbazole parent nucleus, which was firstly synthesized, is condensed with bromine substituted amino acid methyl ester to produce the target compounds. The target compounds were performed with methylthiazolyldiphenyl-tetrazolium bromide（MTT） in vitro cytotoxin activity test and the results showed that compounds CZ-1, CZ-3 and CZ-6 have higher activity against human colon cancer（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared to the positive control JDC-108.
基金Supported by the opening project of Jiangsu Key Laboratory of Biochemistry and Biotechnology of Marine Wetland(No.K2016-11)
文摘A series of antitumor compounds with indolecarbazole structure modified by amino acid and piperidine were designed and synthesized. The indolecarbazole parent nucleus was firstly synthesized, condensed with bromine substituted amino acid methyl ester, then hydrolyzed and condensed with piperidine to produce the target compounds. In vitro cytotoxin activity test was performed against 7 target compounds with methylthiazolyldiphenyl-tetrazolium bromide（MTT）, and the results showed that compounds CZ-2, CZ-3 and CZ-5 have higher activity against human colon cancers（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared with the positive control JDC-108.
基金The study was reviewed and approved by the Helsinki Committee of the Baruch Padeh Medical Center,Poriya(Approval No.POR 0007-20).
文摘BACKGROUND In recent years,associations between specific virulence markers of Helicobacter pylori(H.pylori)and gastrointestinal disorders have been suggested.AIM To investigate the presence of virulence factors including vacuolating cytotoxin A genotypes(s1m1,s1m2,s2m1,and s2m2),cytotoxin-associated gene A(CagA),and urease activity in H.pylori strains isolated from Arab and Jewish populations in northern Israel and to assess associations between these factors and patients’demographics and clinical outcomes.METHODS Patients(n=108)who underwent gastroscopy at the Baruch Padeh Medical Center,Poriya due to symptomatic gastroduodenal pathologies as part of H.pylori diagnosis were enrolled in the study.Gastric biopsy specimens were collected from the antrum of the stomach.Clinical condition was assessed by clinical pathology tests.Bacteria were isolated on modified BD Helicobacter Agar(BD Diagnostics,Sparks,MD,United States).Bacterial DNA was extracted,and PCR was performed to detect CagA and vacuolating cytotoxin A genes.Urease activity was assessed using a rapid urease test.RESULTS A significant correlation was found between disease severity and patient ethnicity(P=0.002).A significant correlation was found between CagA presence and the s1m1 genotype(P=0.02),which is considered the most virulent genotype.Further,a higher level of urease activity was associated with isolates originating from the Jewish population.Moreover,higher urease activity levels were measured among CagA-/s1m1 and CagA-/s2m2 isolates.CONCLUSION Our study highlights the importance of incorporating molecular methods for detection of virulence markers of H.pylori in order to tailor optimal treatments for each patient.Further investigation should be performed regarding associations between H.pylori virulence factors and ethnicity.
