Differential expression of LHRH-receptor in bovine nasal tissue and its role in deslorelin delivery

Sneha Sundaram, Shyamal K Roy, Uday B. Kompella

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Deslorelin, a luteinizing hormone releasing hormone (LHRH) agonist, is transported via the LHRH-receptor (LHRH-R) and exhibits regional variation as follows: inferior turbinate posterior (ITP) > medium turbinate posterior (MTP) > medium turbinate anterior (MTA) of the bovine nasal mucosa. Differential LHRH-R expression in various regions of the nose is a potential explanation for regional variation in deslorelin transport. Thus, the objective was to determine whether LHRH-R expression exhibits regional variation in bovine nasal mucosa. LHRH-R density (Bmax) and affinity constant (Kd) were determined by saturation experiments using 0.5 mg tissue in the presence of increasing amounts of I125-deslorelin (100-100,000 cpm) at 4 °C for 4 h. The 50% inhibitory concentration (IC50) was determined by competition experiments using various amounts of unlabelled deslorelin (0.01-3000 ng) at 4 °C for 4 h. LHRH-R mRNA and protein expressions were determined using real-time PCR and Western blot analysis, respectively. LHRH-R Bmax and Kd varied between the regions of excised bovine nasal mucosa: ITP > MTP > MTA. The inhibition experiments yielded two IC50 concentrations which exhibited trends similar to Bmax and Kd. Real-time PCR and Western blot analysis indicated that LHRH-R expression exhibits similar trends: ITP > MTP > MTA. We identified two deslorelin binding sites in the nasal tissues, with high affinity sites representing approximately 60-70% of the total sites available. In summary, regional differences in nasal deslorelin transport correlate with regional differences in LHRH-R expression, with LHRH-R expression, peptide binding, and transport being the highest in the inferior turbinate posterior region of the nose.

Original languageEnglish (US)
Pages (from-to)351-358
Number of pages8
JournalPeptides
Volume30
Issue number2
DOIs
StatePublished - Feb 1 2009

Fingerprint

LHRH Receptors
Turbinates
Nose
Gonadotropin-Releasing Hormone
Tissue
Nasal Mucosa
Inhibitory Concentration 50
Real-Time Polymerase Chain Reaction
Western Blotting
deslorelin
Experiments
Binding Sites
Messenger RNA
Peptides

Keywords

  • Deslorelin
  • LHRH-receptor (LHRH-R)
  • Luteinizing hormone releasing hormone (LHRH)
  • Nasal turbinates

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

Cite this

Differential expression of LHRH-receptor in bovine nasal tissue and its role in deslorelin delivery. / Sundaram, Sneha; Roy, Shyamal K; Kompella, Uday B.

In: Peptides, Vol. 30, No. 2, 01.02.2009, p. 351-358.

Research output: Contribution to journalArticle

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abstract = "Deslorelin, a luteinizing hormone releasing hormone (LHRH) agonist, is transported via the LHRH-receptor (LHRH-R) and exhibits regional variation as follows: inferior turbinate posterior (ITP) > medium turbinate posterior (MTP) > medium turbinate anterior (MTA) of the bovine nasal mucosa. Differential LHRH-R expression in various regions of the nose is a potential explanation for regional variation in deslorelin transport. Thus, the objective was to determine whether LHRH-R expression exhibits regional variation in bovine nasal mucosa. LHRH-R density (Bmax) and affinity constant (Kd) were determined by saturation experiments using 0.5 mg tissue in the presence of increasing amounts of I125-deslorelin (100-100,000 cpm) at 4 °C for 4 h. The 50{\%} inhibitory concentration (IC50) was determined by competition experiments using various amounts of unlabelled deslorelin (0.01-3000 ng) at 4 °C for 4 h. LHRH-R mRNA and protein expressions were determined using real-time PCR and Western blot analysis, respectively. LHRH-R Bmax and Kd varied between the regions of excised bovine nasal mucosa: ITP > MTP > MTA. The inhibition experiments yielded two IC50 concentrations which exhibited trends similar to Bmax and Kd. Real-time PCR and Western blot analysis indicated that LHRH-R expression exhibits similar trends: ITP > MTP > MTA. We identified two deslorelin binding sites in the nasal tissues, with high affinity sites representing approximately 60-70{\%} of the total sites available. In summary, regional differences in nasal deslorelin transport correlate with regional differences in LHRH-R expression, with LHRH-R expression, peptide binding, and transport being the highest in the inferior turbinate posterior region of the nose.",
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AB - Deslorelin, a luteinizing hormone releasing hormone (LHRH) agonist, is transported via the LHRH-receptor (LHRH-R) and exhibits regional variation as follows: inferior turbinate posterior (ITP) > medium turbinate posterior (MTP) > medium turbinate anterior (MTA) of the bovine nasal mucosa. Differential LHRH-R expression in various regions of the nose is a potential explanation for regional variation in deslorelin transport. Thus, the objective was to determine whether LHRH-R expression exhibits regional variation in bovine nasal mucosa. LHRH-R density (Bmax) and affinity constant (Kd) were determined by saturation experiments using 0.5 mg tissue in the presence of increasing amounts of I125-deslorelin (100-100,000 cpm) at 4 °C for 4 h. The 50% inhibitory concentration (IC50) was determined by competition experiments using various amounts of unlabelled deslorelin (0.01-3000 ng) at 4 °C for 4 h. LHRH-R mRNA and protein expressions were determined using real-time PCR and Western blot analysis, respectively. LHRH-R Bmax and Kd varied between the regions of excised bovine nasal mucosa: ITP > MTP > MTA. The inhibition experiments yielded two IC50 concentrations which exhibited trends similar to Bmax and Kd. Real-time PCR and Western blot analysis indicated that LHRH-R expression exhibits similar trends: ITP > MTP > MTA. We identified two deslorelin binding sites in the nasal tissues, with high affinity sites representing approximately 60-70% of the total sites available. In summary, regional differences in nasal deslorelin transport correlate with regional differences in LHRH-R expression, with LHRH-R expression, peptide binding, and transport being the highest in the inferior turbinate posterior region of the nose.

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