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Anthranilate deteriorates the structure of Pseudomonas aeruginosa biofilms and antagonizes the biofilm-enhancing indole effect.
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Anthranilate and indole are alternative degradation products of tryptophan, depending on the bacterial species. While indole enhances the biofilm formation of Pseudomonas aeruginosa, we found that anthranilate, the tryptophan degradation product of P. aeruginosa, had an opposite effect on P.
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
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A noninvasive topical ocular therapy for the treatment of neovascular or "wet" age-related macular degeneration would provide a patient administered alternative to the current standard of care, which requires physician administered intravitreal injections. This manuscript describes a novel strategy
DISTURBANCES OF INDOLE METABOLISM IN HEPATOLENTICULAR DEGENERATION.
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Molecular cloning and analysis of strictosidine beta-D-glucosidase, an enzyme in terpenoid indole alkaloid biosynthesis in Catharanthus roseus.
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Strictosidine beta-D-glucosidase (SGD) is an enzyme involved in the biosynthesis of terpenoid indole alkaloids (TIAs) by converting strictosidine to cathenamine. The biosynthetic pathway toward strictosidine is thought to be similar in all TIA-producing plants. Somewhere downstream of strictosidine
The effect of reduced neopterin on the synthesis of several methylated indoles in the pineal gland of adult male golden hamsters, kept under standardized conditions.
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In the present study the effect was tested of reduced neopterin (RN) on the methylating capacity of the pineal gland of adult, male golden hamsters, housed under standardized conditions throughout the year. An effect of RN on the synthesis of a number of methylated compounds was, indeed,
Lu 35-138 ((+)-(S)-3-{1-[2-(1-acetyl-2,3-dihydro-1H-indol-3-yl)ethyl]-3,6-dihydro-2H-pyridin-4-yl}-6-chloro-1H-indole), a dopamine D4 receptor antagonist and serotonin reuptake inhibitor: characterisation of its in vitro profile and pre-clinical antipsychotic potential.
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The present study describes the pharmacological profile of the putative antipsychotic drug Lu 35-138 ((+)-(S)-3-{1-[2-(1-acetyl-2,3-dihydro-1H-indol-3-yl)ethyl]-3,6-dihydro-2H-pyridin-4-yl}-6-chloro-1H-indole). The in vitro receptor profile of Lu 35-138 revealed high affinity (K(i)=5 nM) and
Role of melatonin in reducing water avoidance stress-induced degeneration of the gastrointestinal mucosa.
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We investigated the role of melatonin on water avoidance stress (WAS)-induced degeneration of the gastric, ileal and colonic mucosa. Wistar albino rats were exposed to acute WAS (aWAS group) or chronic WAS (cWAS group). Before exposing animals to acute (aWAS + mel group) or chronic WAS (cWAS + mel
Indole-pyruvic acid treatment reduces damage in striatum but not in hippocampus after transient forebrain ischemia in the rat.
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The effects of treatment with indole-pyruvic acid, an endogenous metabolite of tryptophan converted into kynurenic acid in the brain, were studied in rats after transient forebrain ischemia induced by the 4-vessel occlusion procedure. The histological analysis showed a significant protective effect
Weight loss effects of quaternary salts of 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles; structure-activity relationships.
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Quaternary salt analogues based on the DNA minor groove binder and adenine N3 alkylating agent 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indole (aminoCBI) show remarkable effects on the body weight of mice (a long-term failure to gain weight relative to matched controls with no loss of appetite
Carcinogenicity of a mutagenic compound from food, 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeA alpha C), in male F344 rats.
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Carcinogenicity of 2-amino-3-methyl-9H-pyrido[2,3-b]-indole (MeA alpha C) was investigated at dietary levels of 0 (control), 0.01, 0.02, 0.04 and 0.08% using male F344/DuCrj rats. The administration of MeA alpha C was continued for 100 experimental weeks for the control, 0.01 and 0.02% groups, but
SSR180575 (7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide), a peripheral benzodiazepine receptor ligand, promotes neuronal survival and repair.
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In the present study, we have investigated the potential neuroprotective effects of a novel peripheral benzodiazepine binding site (PBR) ligand, 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide (SSR180575), in models of central and peripheral
A study of indoles which inhibit pineal antigonadotrophic activity in male hamsters.
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Blinding adult male golden hamsters led to involution of the testes and accessory sex organs (seminal vesicles and coagulating glands) and to a regression in pituitary prolactin levels within 8 weeks. The subcutaneous implantation of either melatonin or 6-hydroxymelatonin (1 mg/wk in beeswax)
Development of pre-implantation mouse embryos under the influence of pineal indoles.
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The developmental toxicity of pineal hormones on mouse embryos was examined both in vitro and in vivo. Pregnant ICR mice were divided into groups which received at 1.5 days post-coitum (p.c.) and again at 2.5 days p.c. a subcutaneous injection of one of the following pineal indoles:
Effects of pineal indoles and parachlorophenylalanine on seasonal reproduction in the pigeon
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The effect of melatonin, methoxytryptophol (ML), methoxytryptamine (MT) and parachlorophenylalanine (p-CPA) on the mass and histology of the testes and the adrenal and thyroid glands and on serum thyroid hormone levels have been studied in the recrudescent phase of the feral pigeon Columba livia.
[Influence of indole-3-alkanecarboxylic acids on glucose utilization in rats].
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The influence of various indole-3-alkane-carboxylic acids (indole-3-propionic acid, indole-3-butyric acid and derivatives of this substance) on some parameters of carbohydrate, fat and insulin metabolism were studied in normal and experimentally induced diabetic rats. Earlier it had been shown, by
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