Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Cyclamates”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 757 records · Page 42Linked to original sources
PubMed2001

Coreceptor usage of sequential isolates from cynomolgus monkeys experimentally Infected with simian immunodeficiency virus (SIVsm).

Sequential isolates from eight cynomolgus monkeys experimentally infected with simian immunodeficiency virus (SIVsm, of sooty mangabey origin) were tested for coreceptor use in the human osteosarcoma indicator cell line, GHOST(3), expressing CD4 and one or another of the chemokine receptors CCR3, CCR5, CXCR4, BOB, or the orphan receptor Bonzo. The indicator cell line carries the human immunodeficiency virus type 2 long terminal repeat-driven green fluorescence protein gene that becomes activated upon infection with HIV or SIV and fluorescence can be quantitated by flow cytometric analysis. The methodological details are described in the accompanying paper (Vödrös et al., 2001, Virology 290, in press). All SIVsm inoculum viruses and reisolates used CCR5 with a high level of efficiency. CCR5 use was stable over time. BOB and Bonzo use was less efficient than CCR5 use and, in particular, late isolates obtained at the time of immunodeficiency varied greatly in their coreceptor use and often could not establish a productive infection in BOB- or Bonzo-expressing cells. Unexpectedly, early reisolates obtained 12 days postinfection could infect the entire GHOST(3) panel including the parental cells. In one case this was due to use of CXCR4, either transfected or endogenously expressed on the GHOST(3) cells. Our results demonstrate the complex coreceptor use of SIVsm isolates. Moreover, they focus attention on the initial phase of virus replication when the availability of target cells may govern the replication pattern of the virus.

Animals↗
PubMed1987

Bladder cancer and the consumption of alcoholic beverages in Spain.

The relationship between bladder cancer and alcohol consumption was investigated in a case-control study conducted in 506 patients (453 males and 53 females) with diagnoses of papillary urothelial carcinoma during 1978-1982 at "La Paz" hospital (Madrid), and an equal number of controls matched for age, sex and date of admission to the hospital. The results showed that the risk of bladder cancer does not increase with the intake of beer, wine and spirit beverages. However, a high risk of bladder cancer was associated with consumption of wine mixed with "gaseosa" (a refreshment beverage consisting of carbonated water plus artificial sweeteners).

Age Factors↗
PubMed1976

[Cycloalkylsulfamic acids and their salts. V. (author's transl)].

3-Methyl-4-thia-cyclohexylsulfamic acid was synthesized, the degree of sweetness of its sodium salt was measured, and compared with that of the sodium salts of 3-methyl-cyclohexylsulfamic acid, 4-thia-cyclohexylsulfamic acid, and cyclohexylsulfamic acid.

Chemical Phenomena↗
PubMed1976

Heritable chromosome aberrations in mammals after exposure to chemicals.

The observation of dividing spermatocytes is routinely used to detect the induction of heritable chromosome aberrations such as reciprocal translocations in the treated animals or in their F1 offspring. 37 compounds have so far been tested for the induction of chromosome rearrangements in spermatogonia. Only 9 gave positive results. However, positive results were observed for all alkylating agents in the F1 test. From these observations it can be concluded that the spermatogonia which are the main germ cell type at risk represent a relatively safe germ cell stage.

Aflatoxins↗
PubMed1978

Ionic and metabolic requirements for the hydroosmotic response to antidiuretic hormone in toad urinary bladder.

A study has been conducted to determine the ionic and metabolic requirements for full expression of the hydroosmotic response to antidiuretic hormone in the toad urinary bladder. By appropriate manipulation of incubation conditions it can be shown that there is a pool of serosal sodium necessary for a full hormone response. This serosal sodium pool is not related to the transepithelial sodium transport pool A full hydroosmotic response also requires serosal potassium; however, no specific anion requirement was demonstrated. Additionally, anaerobic or aerobic metabolism support a full hydroosmotic response equally well.

Animals↗
PubMed2001

[Artificial sweeteners--are they potentially carcinogenic?].

BACKGROUND: Artificial sweeteners have rapidly evolved over the last 20 years and are added to a broad variety of food, drinks, drugs, and hygiene products. Since their introduction, especially mass media have reported about potential cancer risks, which has attributed to undermine the people's sense of security. It can be assumed that every citizen of the western countries is using artificial sweeteners--knowingly or not. A cancer-inducing activity of one of these substances would mean a health risk to an entire population. STUDIES: This article gives an overview about the most important publications dealing with the cancerogenic potential of artificial sweeteners.

Animals↗
PubMed2006

The chemokine (C-X-C motif) receptor 4 inhibitor AMD3100 accelerates blood flow restoration in diabetic mice.

AIMS/HYPOTHESIS: Bone marrow cell mobilisation potently induces vascular growth in ischaemic tissue, possibly by mobilising endothelial cell progenitors. Thus, mobilising agents might not be therapeutic when endothelial cell progenitors are dysfunctional, as in diabetes mellitus. Local injection of autologous endothelial cell progenitors also stimulates vascular growth in ischaemic tissue, but endothelial cell progenitors from people with multiple cardiovascular risk factors and from obese diabetic mice are marginally therapeutic or inhibitory. We sought to identify possible strategies to improve vascularisation in patients with diabetes mellitus by determining if (1) mobilisation accelerates neovascularisation in diabetic animals, and (2) mobilised cells from a non-diabetic source accelerate vascularisation in diabetic animals. METHODS: We tested whether systemic administration of the chemokine (C-X-C motif) receptor 4 inhibitor AMD3100 or local injection of human CD34(+) circulating cells mobilised by AMD3100 could speed or enhance blood flow restoration in ischaemic limbs of diabetic mice. The small-molecule-mobilising drug AMD3100 was selected because mobilisation and apheresis can be done on the same day. RESULTS: Systemic administration of AMD3100 and local injection of cells mobilised by AMD3100 greatly accelerated the restoration of blood flow to ischaemic limbs of diabetic mice. CD34(+) cells mobilised by AMD3100 appeared to be more potent growth stimulators than their unmobilised counterparts. CONCLUSIONS/INTERPRETATION: Unlike other mobilising agents requiring multi-day mobilisation, AMD3100 enables mobilised donors to undergo mobilisation and apheresis on the same day. The combination of excellent therapeutic benefits as well as ease of use indicates that AMD3100 could be a powerful tool to ameliorate tissue ischaemia in the diabetic environment.

Animals↗
PubMed2002

New potent agents binding to a poly(dT) sequence in double-stranded DNA: bis(Zn(2+)-cyclen) and tris(Zn(2+)-cyclen) complexes.

In an effort to search for mechanistically new and more potent agents than conventional drugs that target AT-rich sequences in double-stranded DNA, we have tested multi(Zn(2+)-cyclen) complexes. Indeed, they selectively bound to poly(dT) sequences to melt the A-T hydrogen bonds; only 2.5 microM or 4 microM of the p-tris(Zn(2+)-cyclen) complex were required to completely melt a 50 microM nucleobase of double-stranded poly(dA) x poly(dT) or poly(dA-dT)(2) at 25 degrees C. The region with seven consecutive T's in native DNA (150 bp) was protected from micrococcal nuclease hydrolysis, as revealed by footprinting assays, with IC(50) values of 2 microM for p-bis(Zn(2+)-cyclen) and 0.5 microM for p-tris(Zn(2+)-cyclen). The high affinity to AT-rich sequences of these Zn(2+)-cyclen complexes matches or surpasses those of the conventional AT-binding drugs distamycin A (IC(50)=2 microM) and DAPI (5 microM). Moreover, the p-tris(Zn(2+)-cyclen) complex selectively binds to the TATA box sequence of the SV40 early promoter to inhibit the binding of the TATA binding protein as effectively as distamycin A, with an IC(50) value of 0.4 microM. In vitro transcription of poly(dA) x poly(dT) using Escherichia coli RNA polymerase was effectively inhibited by p-tris(Zn(2+)-cyclen). The [(3)H]-ATP incorporation into RNA was more strongly blocked (IC(50)=0.8 microM) than the [(3)H]-UTP incorporation (IC(50)=40 microM), a fact indicating that the p-tris(Zn(2+)-cyclen) complex interacts only with the poly(dT) strand in the double-stranded DNA template.

Base Sequence↗
PubMed1999

Natural and synthetic double-stranded DNA binding studies of macrocyclic tetraamine zinc(II) complexes appended with polyaromatic groups.

The characteristic binding mode of zinc(II) complexes of macrocyclic tetraamines (1,4,7,10-tetraazacyclododecane, cyclen) appended with one or two arylmethyl group(s) [(4-quinolyl)methyl-, 1,7-bis(4-quinolyl)methyl-, (1-naphthyl)methyl-, 1,7-bis(1-naphthyl)methyl-, and (9-acridinyl)methyl-cyclen] to double-stranded calf thymus DNA and synthetic DNAs [poly(dA)-poly(dT), poly(dA-dT)2, poly(dI).poly(dC), poly(dI-dC)2, poly(dG) poly(dC), and poly(dG-dC)2] has been examined by spectrophotometric methods, Tm measurement, and inhibition of these DNA-directed transcriptions in vitro. Various hypochromic and bathochromic effects on the pendant aromatic absorption spectra of the complexes were observed in titration with the native and synthetic DNA. The binding constants Kapp (=[bound cyclen derivatives]/[unbound cyclen derivatives][DNA phosphates] M(-1)), at 25 degrees C in 10 mM EPPS (pH 8.0) containing 0.1 M Na+, were determined and compared with those of the corresponding Zn2+ -free ligands. The results showed that the Zn2+ -cyclen complexes interact with the DNA more strongly than the corresponding diprotonated ligands, leading to a stronger stacking of the pendant aromatic rings. The binding of Zn2+ -(9-acridinyl)methyl-cyclen to calf thymus DNA was competed by an AT-selective, minor groove binder, distamycin, but not by a major groove binder, methyl green. In an unusual interaction of excess Zn2+ -(9-acridinyl)methyl-cyclen with poly(dA).poly(dT), the Zn2+ -cyclen moiety went into the minor groove to make coordination bonds with the deprotonated imides of the thymines, resulting in disruption of the poly(dA).poly(dT) duplex. Thymine-containing DNA-directed transcription with Escherichia coli RNA polymerase in vitro was inhibited by the Zn2+ -(9-acridinyl)methyl-cyclen. The 50% inhibition concentrations of the transcription (IC50) were 22-45 microM with poly(dA).poly(dT) or poly(dA-dT)2 as templates, while with poly(dG-dC)2 as a template the IC50 value was 110 microM.

Amines↗
PubMed2003

Cyclen substitution with urea-containing dendrimeric branches. Theoretical study considering the concept of collectivity.

Equilibrium structures of novel dendrimeric compounds consisting of 1,4,7,10-tetraazacyclododecane (cyclen) mono- to tetra-substituted with four different dendrimeric branches have been studied. It has been shown using molecular dynamics (MD) that, even in the presence of the macrocycle cyclen, the most stable conformations are those with a globular shape due to close contact interactions between poly-functional branches. No collapse of cyclen occurred, making this cavity available for metal complexation. Terminal branches A=NHCOOtBu, B=OSi(Me)2tBu, C=Imidazole and D=CN have different molecular volumes in the decreasing order: B>A>C>D. This conclusion is in accord with the long range interaction energies, showing that the larger the volume the less the steric hindrance. Considering these energy values, the stability of the systems follows exactly the same tendency as observed for the molecular volume. More polar groups like A=NHCOOtBu and D=CN impart extra stability due to long range interactions between atoms separated by exactly three chemical bonds. The negative charge inside the cyclen cavity increases with the volume of the branches. Besides cyclen, urea groups located at the middle of the branches represent another independent point of negative charge for eventual interaction with small molecules. These compounds show a sum of small contributions of the functionalities in a collective fashion.

Computer-Aided Design↗
PubMed2001

Increase of R5 HIV-1 infection and CCR5 expression in T cells treated with high concentrations of CXCR4 antagonists and SDF-1.

The chemokine receptors CXCR4 and CCR5 are considered to be potential targets for the inhibition of HIV-1 replication. We found that the synthetic peptides T134 and T140 (see text for full names) inhibited X4 HIV-1 infection with selectivity and low toxicity because they acted as CXCR4 antagonists. However, high concentrations of T134, T140, and ALX40-4C (see text for full name) increased the expression of CCR5 and R5 HIV-1 infection, as did stromal cell-derived factor 1 (SDF-1). In contrast to CXCR4 antagonists and SDF-1, viral monocyte inflammatory protein (vMIP) II inhibited not only anti-CXCR4 monoclonal antibody (MAb) but also inhibited anti-CCR5 MAb binding to human peripheral blood mononuclear cells, and inhibited both X4 and R5 HIV-1 strains. T134, T140, ALX40-4C, and SDF-1 increased viral transcription in the treated cells. In addition, ALX40-4C and SDF-1 also increased nuclear transcription factor (NF)-kappaB. However, the mechanisms of action of T134 and T140 are different from those of clinically used anti-HIV drugs. Thus, synergistic activities were observed in the concomitant treatment with T134 and reverse transcriptase inhibitors or protease inhibitors. Our findings, presented here, are noteworthy in regard to the potential clinical use of these agents as drugs for the treatment of AIDS.

Animals↗