Effect of Oligopeptides-Homologues of the Fragment of ACTH<sub>15-18</sub> on Morphogenetic Markers of Stress in the Adrenal Glands on the Model of Acute Cold Injury in Rats

Article

Author: Kudina, Olesia ; Larjanovska, Yulia ; Shtrygol, Sergii

ObjectivesAim of the current study was to evaluate the stress-protective effect of oligopeptides-homologues of the adrenocorticotropic hormone (ACTH) fragment 15-18 on morphogenetic signs of stress reaction of the adrenal glands under acute cold exposure (CE) in rats.Materials and MethodsThe acute cold stress was reproduced by placing random-bred male rats in a freezer at a temperature of -18°C for 2 hours. The peptides-homologous of ACTH_15-18 acetyl-(D-Lys)-Lys-Arg-Arg-amide (KK-1) and acetyl-(D-Lys)-Lys-(D-Arg)-Arg-amide (KK-5) and the reference medicine (Sema) were administered intranasally in a dose of 20 mg/kg 30 minutes before and after CE. Rectal temperature was measured before and 10 min after CE. Zona glomeruloza, zona fasciculata, zona reticularis, and the area of cells and nuclei of adrenocorticocytes of the zona fasciculata were measured.ResultsKK-1 significantly prevented structural changes in the adrenal cortex and medulla and stabilized the secretory activity of glucocorticoid-producing cells. However, the congestion of the capillaries of the zona fasciculata and zona reticularis remained in some locations. Zona fasciculata cells had a marked tendency to decrease, and the area of nuclei significantly decreased (p<0.05) recovering the width to control animals' markers. KK-5 had a more marked recovery of the adrenal glands (a greater saturation of cytoplasm of adrenocorticocytes of zona glomerulosa and zona fasciculata). The number of chromaffin cells at rest was increased in the adrenal medulla. KK-5 statistically significantly normalized both the area of cells (p<0.05) and the area of nuclei (p<0.05) of the zona fasciculata, unlike KK-1, which reliably restored only the marker of the nuclei area. Some morphometric parameters of acute stress hypertrophy remained in the adrenal glands of rats receiving Sema.ConclusionKK-1 and KK-5 prevented the manifestation of acute stress reactions in the adrenal cortex of rats. KK-5 had a more marked stress-protective effect compared with the peptide KK-1. Both study substances exceeded the reference medicine Sema. KK-5 is a promising stres-sprotector and frigoprotector.

01 Feb 2013·ChemosphereQ2 · ENVIRONMENTAL SCIENCE & ECOLOGY

Significance of autochthonous Bacillus sp. KK1 on biomineralization of lead in mine tailings

Q2 · ENVIRONMENTAL SCIENCE & ECOLOGY

Article

Author: Kui-Jae Lee ; Jae Su Kim ; Byung-Taek Oh ; Muthusamy Govarthanan ; Seralathan Kamala-Kannan ; Min Cho

The aim of the study was to isolate and characterize potential autochthonous bacteria for biomineralization of Pb in mine tailings. A total of four bacteria were isolated from the soil samples and assayed for tolerance to Pb and other heavy metals. Isolate KK1 exhibited maximum Pb resistance and was subsequently identified as Bacillus sp. based on the partial 16S rRNA gene sequences. The isolate KK1 reduced the Pb ions and did not harbor pbrT gene. Selective sequential extraction of bioaugmented soil revealed that the isolate significantly reduced (26%) the exchangeable fraction and increased (38%) the carbonate fraction of Pb. X-ray diffraction studies confirmed the role of bacterially induced calcite precipitation in the bioremediation of mine tailings. A significant increase in the urease (334%), DHO (dehydrogenase) (14%), and phosphatase (37%) activity was observed in the bioaugmented mine soil.

01 Mar 2005·NeuropharmacologyQ2 · MEDICINE

In vivo behavioral effects of stable, receptor-selective neurotensin[8?13] analogues that cross the blood?brain barrier

Q2 · MEDICINE

Article

Author: Ronald E. See ; Kimber L. Price ; Kyle P. Kokko ; M. Kyle Hadden ; Kevin S. Orwig ; Thomas A. Dix

A set of neurotensin[8-13] (NT[8-13]) analogues (KK1-19) has been evaluated in various pre-clinical assays relevant for further development of these compounds as potential antipsychotics. Initial screening of these compounds for induction of hypothermia following systemic (I.V.) injection in rats, an indirect method commonly utilized to measure the central nervous system (CNS) activity of NT[8-13] analogues, identified three peptides, KK1, KK13 and KK14, capable of crossing the blood-brain barrier (BBB). KK1 features 2(S)-azido-7-aminoheptanoic acid (AAHA) in the Arg(8) position and represents the first monosubstituted NT[8-13] analogue that crosses the BBB. KK13 and KK14 both feature AAHA in the Arg(8) position and tert-Leu in the Ile(12) position while KK14 includes a Trp substituted for Tyr(11). When I.P. administered, only the latter two analogues induced a significant hypothermic response. KK13 (1mg/kg) inhibited amphetamine-induced hyperlocomotion after I.P. injection; this assay is highly predictive for potential antipsychotics. Chronic dosing (5mg/kg) of this compound over 5 consecutive days failed to induce hypothermic tolerance while the same dose failed to induce measurable catalepsy. KK13 is thus the first NT[8-13] analogue described to date that demonstrates inhibition of amphetamine-induced hyperlocomotion without inducing catalepsy while maintaining day-to-day hypothermic potency.

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 1	-	Xiamen Nanxun Co., Ltd	-

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