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Effects of acetylsalicylic acid and a new pyrazine derivative PD-101 on sister chromatid exchange frequency and cell kinetics in cultured human lymphocytes

100%

Wozniak A., Limon J., Petrusewicz J., Kaliszan R.

Journal of Applied Genetics

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1998

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tom 39

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nr 3

Acetylsalicylic acid (ASA) and α-2-pyrazylidene-α-cyano N-butyl acetamide (PD-101), a new antiaggregatory pyrazine derivative were tested for their genotoxicity in human lymphocytes in vitro using the sister chromatid exchange (SCE) technique. Both compounds were found to be inactive in inducing SCE in concentration from 1 µM up to 1000 µM. The agents displayed inhibitory effect on cell kinetics.

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Synthesis and biological properties of new chimeric galanin analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2

76%

Ruczynski J., Konstanski Z., Cybal M., Petrusewicz J., Wojcikowski C., Rekowski P., Kaminska B.

Journal of Physiology and Pharmacology

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2005

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tom 56

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nr 2

Several chimeric peptides consisting of the N-terminal fragment of galanin (GAL) and C-terminal fragments of other bioactive peptides (e.g. substance P, bradykinin, neuropeptide Y, mastoparan) have been synthesized and reported as high-affinity galanin receptor antagonists. Recently we have synthesized a new chimeric peptide, GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2, consisting of the N-terminal fragment of GAL and the C-terminal fragment of endothelin-1 (ET-1) analogue. This chimera was previously shown to be a moderate-affinity ligand to hypothalamic galanin receptors with a KD value of 205 nM. However, its biological action has been unknown so far. In our studies we characterized the biological properties of this new chimeric analogue, investigating its action on rat isolated gastric smooth muscles and influence on insulin secretion from rat isolated islets of Langerhans. Data acquired in the course of our studies suggest that analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2 does not seem to be a potent galanin receptor antagonist in the gastrointestinal tract.

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New galanin(1-15) analogues modified in positions 9,10 and 11 act as galanin antagonists on glucose-induced insulin secretion

76%

Olkowicz M., Ruczynski J., Cybal M., Konstanski Z., Petrusewicz J., Kaminska B., Rekowski P.

Journal of Physiology and Pharmacology

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2007

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tom 58

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nr 4

Galanin (GAL) is a 29-amino-acid residue peptide originally isolated from porcine upper small intestine. GAL exhibits various physiological activities, such as effects on hormones release, smooth muscles contractions, gastric acid secretion, neurons degeneration and feeding. One of the biological actions of GAL is the inhibition of insulin secretion from the pancreatic ß-cells. In our studies we have designed several new 15-amino-acid-residue galanin fragment analogues modified in positions: 6, 8, 9, 10, 11 and tested for their effects on glucose-induced insulin secretion from isolated rat pancreatic islets of Langerhans. In vitro insulin secretion was studied during static incubation. All peptides were tested at two concentrations: 0.1 µM and 1 µM. Among the analogues derived from GAL(1-15)NH2 peptide: [Phe9]GAL(1-15)NH2 and [Pro11]GAL(1-15)NH2 were found to be the potent antagonists against the inhibitory effect of GAL on glucose-induced insulin secretion from the isolated rat pancreas. These analogues block the GAL-mediated inhibition of insulin secretion. The present studies have shown that analogues: [Phe9]GAL(1-15)NH2 and [Pro11]GAL(1-15)NH2 may be a key compounds for developing a more potent GAL antagonists.

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Sources of activator Ca2plus for galanin-induced contractions of rat gastric fundus, jejunum and colon

76%

Korolkiewicz R. P., Konstanski Z., Rekowski P., Ruczynski J., Szyk A., Korolkiewicz K. Z., Petrusewicz J.

Journal of Physiology and Pharmacology

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2000

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tom 51

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nr 4,2

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Actions of several substituted short analogues of porcine galanin on isolated rat fundus strips: a structure-activity relationship

64%

Korolkiewicz R. P., Konstanski Z., Rekowski P., Ruczynski J., Szyk A., Grzybowska M., Korolkiewicz K. Z., Petrusewicz J.

Journal of Physiology and Pharmacology

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2001

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tom 52

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nr 1

Ograniczanie wyników

4 Journal of Physiology and Pharmacology

1 Journal of Applied Genetics

5 Petrusewicz J.

4 Konstanski Z.

4 Rekowski P.

4 Ruczynski J.

2 Cybal M.

2 Kaminska B.

2 Korolkiewicz K. Z.

2 Korolkiewicz R. P.

2 Szyk A.

1 Grzybowska M.

1 Kaliszan R.

1 Limon J.

1 Olkowicz M.

1 Wojcikowski C.

1 Wozniak A.

1 2007

1 2005

1 2001

1 2000

1 1998

Effects of acetylsalicylic acid and a new pyrazine derivative PD-101 on sister chromatid exchange frequency and cell kinetics in cultured human lymphocytes

Synthesis and biological properties of new chimeric galanin analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2

New galanin(1-15) analogues modified in positions 9,10 and 11 act as galanin antagonists on glucose-induced insulin secretion

Sources of activator Ca2plus for galanin-induced contractions of rat gastric fundus, jejunum and colon

Actions of several substituted short analogues of porcine galanin on isolated rat fundus strips: a structure-activity relationship