3 Some Pyrimidines of Biological and Medicinal Interest—I

Cheng, G.C.

doi:10.1016/s0079-6468(08)70197-8

Cited by 50 publications

(4 citation statements)

References 528 publications

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“…The rats were either untreated (control group injected with saline 0•9% NaCl) or intravenously injected with alloxan (dissolved in saline solution, pH 7) at a dose of 40 mg/kg body weight, after an overnight fasting period as previously described (Otton et al 2002a). Alloxan is a potent generator of reactive oxygen species, which can mediate -cell toxicity (Cheng & Roth 1971, Elsner et al 2002. We chose the model of alloxan-induced diabetes because alloxan-diabetic rats present low plasma levels of insulin with no change in the activation state of the immune cells.…”

Section: Induction Of Diabetesmentioning

confidence: 99%

Diabetes induces apoptosis in lymphocytes

Otton¹,

Soriano²,

Verlengia³

et al. 2004

Journal of Endocrinology

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The occurrence of DNA fragmentation in lymphocytes obtained from alloxan-induced diabetic rats and diabetic patients was investigated. A high proportion of apoptotic lymphocytes in diabetic states may explain the impaired immune function in poorly controlled diabetic patients. Rat mesenteric lymph node lymphocytes were analysed for DNA fragmentation by using flow cytometry and agarose gel, and for chromatin condensation by Hoescht 33342 staining under different situations. Immediately after being obtained, the proportion of lymphocytes with fragmented DNA was twofold higher in alloxan-induced diabetic rats than in cells from control rats. After 48 h in culture, the occurrence of DNA fragmentation was also higher (81%) in cells from diabetic rats. Hoescht staining and fragmented DNA visualized in agarose gel were also higher in lymphocytes from alloxan-induced diabetic rats than in control cells. To investigate if this phenomenon also occurs in humans, blood lymphocytes from 14 diabetic subjects were examined. Similar results to those of rat lymphocytes were found in cells from diabetic patients immediately after being obtained and after 48 h in culture. The high occurrence of apoptosis in lymphocytes was accompanied by a reduced number of blood-circulating lymphocytes in diabetic patients. The involvement of low insulinaemia for the occurrence of apoptosis in lymphocytes was also examined. Insulin treatment markedly reduced the proportion of lymphocytes with fragmented DNA in alloxan-induced diabetic rats.

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Section: Induction Of Diabetesmentioning

confidence: 99%

Diabetes induces apoptosis in lymphocytes

Otton¹,

Soriano²,

Verlengia³

et al. 2004

Journal of Endocrinology

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“…Pyrimethamine which induces apoptosis and matrix metalloproteinases (MMP) and potent telomerase inhibition in the prostate cell line is considered to be a chemopreventative agent in cancer [77][78][79]. Lately, it has been found that the "T-oligo", an oligonucleotide which has the homology sequence to the terminal telomeric DNA, is a telomerase inhibitor and has shown cytotoxic effects in multiple cancers and destruction of the T-loop structure followed by the DNA damage response likely pathway [80].…”

Section: Small-molecule Telomerase Inhibitorsmentioning

confidence: 99%

Telomere and Telomerase as Targets for Cancer Therapy

Tian

Chen

Liu

2009

Appl Biochem Biotechnol

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Telomere maintenance and telomerase reactivation is essential for the transformation of most human cancer cells. Telomere shortening to the threshold length, mutations of the telomere-associated proteins, and/or telomerase RNA lead to telomeric dysfunction and therefore genomic instability. Telomerase up-regulation in 85% of human cancer cells has become a hallmark of cancers, hence a promising target for anticancer therapy. In this review, we discuss the mechanism of cancer due to telomere dysfunction and the resulting biological effects, the control of telomerase activity, and the new developments in cancer therapies targeting telomere and telomerase.

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“…Pyrimidine thiones and their nucleosides are of considerable biological importance (Cheng, 1969). Various analogues of pyrimidine thiones possess effective antibacterial, antifungal, antiviral, insecticidal, and miticidal activities (Akkurt and Hiller, 1993;Ajitkumar and Cherayil, 1988).…”

Section: Introductionmentioning

confidence: 99%

Antiviral and Antischistosomal Evaluation of Newly Synthesized Thioglycosides and their Acyclic Analogues

Ael-H²,

Sm³

et al. 2009

Zeitschrift Für Naturforschung C

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The pyrimidine thione derivatives 2a -d were prepared by the reaction of thiourea, ethyl cyanoacetate and several aromatic aldehydes. The acyclic thioglycosides 4a -7d were prepared by the reaction of the synthesized pyrimidine thiones 2a -d with different alkyl halides, whereas the reaction of 2a -d with 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl bromide afforded the cyclic thioglycosides 8a -d whose deprotection afforded 9a -d. The obtained compounds were tested for their antischistosomal and antiviral activity against hepatitis B virus (HBV). Compounds 5a, 5d, 7a showed high activity against HBV using the MTT assay; moreover compounds 5c, 6d, 7a, 9a, 9c exhibited high activity as antischistosomal agents.

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3 Some Pyrimidines of Biological and Medicinal Interest—I

Cited by 50 publications

References 528 publications

Diabetes induces apoptosis in lymphocytes

Diabetes induces apoptosis in lymphocytes

Telomere and Telomerase as Targets for Cancer Therapy

Antiviral and Antischistosomal Evaluation of Newly Synthesized Thioglycosides and their Acyclic Analogues

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