• Title, Summary, Keyword: opioid peptides

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The Relationships of the Opioid-peptides to Hope of the Cancer Patients (암환자에서 희망과 아편양 펩타이드의 관련성 연구)

  • Kim, Dal-Sook
    • Asian Oncology Nursing
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    • v.1 no.2
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    • pp.157-167
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    • 2001
  • Purpose : This study was 1) to determine the relationship between endogenous opioid-peptides and hope 2) to evaluate the availability of the opioid- peptides, known as biochemicals of emotion in psychoneuroimmunology, as a variable to explain hope. Method : blood sampling for 20 cancer patients' (age range 18-73, 13 men and 7 women, having mild pain or no pain, can do ADL) were made under approval from the doctors in a university hospital at 8 A.M. and quantitative analysis of opioid peptides were done by the internal standard method. In 10min after blood sampling, hope was measured using Kim and Lee's hope scale which had acceptable reliabilities and validity after making consent about interviewing. Blood was sampled from the seven normal adults for comparing the degrees of the opioids. None-parametric statistical analysis was used. Results : There was a significant difference in leucine enkephalin between normal adults and cancer patients. And significant positive relationship existed between chemotherapy and leucine enkephalin. So, the relationships between hope and the endogenous opioids in the patients before chemotherapy were re-tested, excluding the effect of chemotherapy on opioids. As a result, a significant negative relationship between hope and beta- endorphin(r=-.841<.05) showed. And there were highly negative relationships between leucine enkephalin and methionine enkephalin and hope, but not significant statistically. Conclusions : This results implies endogenous opioids can be used as a biological variable to explain hope. More researches in sophisticated design would be needed ,especially in human model.

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Vector-Mediated Delivers of $^{125}I$-labeled Opioid Peptide, $[Lys^7$]dermorphin (K7DA), through the Blood-Brain Barrier (진통 펩타이드 K7DA의 혈액-뇌 관문을 통한 Vector-Mediated Delivery)

  • 강영숙
    • Biomolecules & Therapeutics
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    • v.5 no.1
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    • pp.53-58
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    • 1997
  • $[Lys^7$]dermorphin, abbreviated K7DA, which has structural features similar to a metabolically stable $\mu$-opioid peptide agonist $[D-Arg^2, Lys^4$]dermorphin analogue (DALDA), but is intrinsically more potent with respect to binding to the $\mu$-opioid peptide receptor. The present studies report on attempts to enhance brain uptake of systemically administered K7DA by conjugation to a complex of streptavidin (SA) and the OX26 murine monoclonal antibody to the rat transferrin receptor, which undergoes receptor-mediated transcytosis through the blood-brain barrier (BBB). SA-OX26 conjugate mediates BBB transport of biotinylated therapeutics. The K7DA is monobiotinylated at the $\varepsilon$-amino group of the $[Lys^7$] residue with cleavable linker using NHS-SS-biotin. The brain uptake of $^{125}I$ labeled biotinylated K7DA ($^{125}I$-bio-SSa-K7DA) was very small and rapidly metabolized after intravenous injection. The brain uptake, expressed as percent of injected dose delivered per gram of brain, of the $^{125}I$-bio-55-K7DA bound to the SA-OX26 conjugate $^{125}I$-bio-SS-K7DA/SA-OX26) was 0.14$\pm$0.01, a level that is 2-fold greater than the brain uptake of morphine. The cleavability of the disulfide linker in vivo in rat plasma and brain was assessed with gel filtration HPLC and intravenous injection of labeled opioid chimeric peptides. The disulfide linker is stable in plasma in vivo but is cleaved in rat brain in vivo. In conclusion, these studies show that delivery of these potential opioid peptides to the brain may be improved by coupling them to vector-mediated BBB drug delivery system.

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Physiological Effects of Casein-derived Bioactive Peptides (카제인 유래 생리활성 Peptide의 체내 효과)

  • Jung, Ho-Jung;Min, Bock-Ki;Kwak, Hae-Soo
    • Food Science of Animal Resources
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    • v.29 no.6
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    • pp.659-667
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    • 2009
  • Casein is considered to be the main source of protein in milk; therefore, many studies have been conducted to identify casein-derived bioactive peptides and their physiological effects. Casein is inactive within the parent protein but can be liberated by various proteases and enzymatic hydrolysis during microbial fermentation and gastrointestinal digestion. Once absorbed, casein exhibits different bioavailabilities in the body. Specifically, casein-derived peptides function as angiotensin converting enzyme (ACE) inhibitor in the cardiovascular system; thus, they are expected to reduce and prevent hypertension. Additionally, casein-derived peptides behave as opioid-like peptides in the nervous system, which impacts relaxation. These peptides are also expected to modulate various aspects of immune functions. Finally, caseinophosphopeptide (CPP) and glycomacropeptide (GMP) may exhibit a number of nutritional effects such as the absorption of calcium, iron or zinc. Many studies have been conducted to evaluate casein-derived peptides due to their multifunctional properties and the results of these studies have contributed to the development of a wide variety of functional dairy products. The purpose of this paper was to review the generation of bioactive peptides, their absorption and metabolism, and their specific bioactive effects.

Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?

  • Ok, Hwoe Gyeong;Kim, Su Young;Lee, Su Jung;Kim, Tae Kyun;Huh, Billy K;Kim, Kyung Hoon
    • The Korean Journal of Pain
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    • v.31 no.2
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    • pp.73-79
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    • 2018
  • All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to ${\mu}$ opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia, while the ${\beta}$-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the ${\beta}$-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the ${\mu}$ receptor G protein pathway selective (${\mu}$-GPS) modulation. Even though adverse reactions (ADRs) are significantly attenuated, while the analgesic effect is augmented, the some residual ADRs persist. Consequently, a G protein biased ${\mu}$ opioid ligand, oliceridine, improves the therapeutic index owing to increased analgesia with decreased adverse events. This review article provides a brief history, mechanism of action, pharmacokinetics, pharmacodynamics, and ADRs of oliceridine.

Health Functional Peptides From Milk Products (유제품의 기능성 펩타이드)

  • Lee, Hyong-Joo
    • 한국유가공학회:학술대회논문집
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    • pp.22-29
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    • 1998
  • Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides (CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These results suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

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Health Functional Peptides from Milk Products (유제품의 기능성 펩타이드)

  • Lee, Hyong-Joo
    • Journal of Dairy Science and Biotechnology
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    • v.16 no.2
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    • pp.98-105
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    • 1998
  • Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides(CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These result suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

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Bioactive Components in Milk (우유의 생리활성 물질)

  • Kim, Geun-Bae
    • Journal of Dairy Science and Biotechnology
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    • v.28 no.1
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    • pp.43-52
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    • 2010
  • In addition to the nutritional values, milk has a wide range of bioactive compounds which have been found to be increasingly important for physiological and biochemical functions on human metabolism and health. Bioactive components in milk comprise specific proteins, peptides, lipids and carbohydrates. Especially, milk proteins are known to exert a wide range of nutritional, functional, and biological activities. And milk proteins are considered the most important source of bioactive peptides, including antihypertensive, antithrombotic, antimicrobial, antioxidative, immunomodulatory, and opioid peptides. Many ingredients containing specific bioactive peptides derived from milk protein hydrolysates have been launched on the market and are currently under development. In future studies more emphasis should be given to the health-promoting effect in the well-defined human clinical studies for the successful development of function foods based on the milk-derived bioactive components.

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Bioactive Peptides in Milk and Dairy Products: A Review

  • Park, Young Woo;Nam, Myoung Soo
    • Food Science of Animal Resources
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    • v.35 no.6
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    • pp.831-840
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    • 2015
  • Functionally and physiologically active peptides are produced from several food proteins during gastrointestinal digestion and fermentation of food materials with lactic acid bacteria. Once bioactive peptides (BPs) are liberated, they exhibit a wide variety of physiological functions in the human body such as gastrointestinal, cardiovascular, immune, endocrine, and nervous systems. These functionalities of the peptides in human health and physiology include antihypertensive, antimicrobial, antioxidative, antithrombotic, opioid, anti-appetizing, immunomodulatory and mineral-binding activities.

BIOACTIVE PEPTIDES DERIVED FROM FOOD PROTEINS AND PREVENTION OF LIFE-STYLE RELATED DISEASES

  • Yoshikawa Masaaki
    • Proceedings of the Korean Society of Food Science and Nutrition Conference
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    • pp.69-73
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    • 2001
  • Two opioid peptides, YPLDL and YPLDLF, were isolated from enzymatic digests of spinach ribulose-1, 5-bisphosphate carboxylase/oxygenase (RuBisCO) and named rubiscolin-5 and -6, respectively. These peptides were selective for delta-receptor and the latter was about 3 times more potent than the former. After oral administration in mice at the dose of 100 mg/kg, rubiscolin-6 showed analgesic activity in tail pinch test. It also stimutated learning performance at the same dose in passive avoidance experiment using step-through apparatus. An immunostimulating peptide, MITLAIPVNKPGR, was isolated from a trypsin digest of soybean protein and named soymetide. Immunostimulating activy of soymetide was mediated by fMLP receptor. Interestingly, after oral administration in rats at a dose of 300 mg/kg (po.), soymetide-4 (MITL) protected alopecia (hair-loss) induced by etoposide, a cancer chemotherapy agent. Stimulation of IL-1 release by the peptide was involved in the mechanism. Ovokinin(2-7), RADHPF, is a vasorelaxing peptide released from ovalbumin by the action of chymotrypsin. It lowered blood pressure of spontaneously hypersensive rats (SHR) after oral administration at a dose of 10 mg/kg. RPLKPW, which was designed by replacing 4 amino acid residues in ovokinin(2-7), exhibited hypotensive activity at a dose of 0.1 mg/kg (po.). This peptides was introduced into 3 homologous sites in soybean beta-conglycinin alpha' subunit by site-directed mutagenesis of the cDNA and expressed in E. coli. The minimum effective dose for hypotensive activity of the genetically modified beta-conglycinin alpha' subunit was 10 mg/kg (po.), which is about 1/200 that of ovalbumin.

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The Recent Study on Pain Modulation of Acupuncture (침의 통증 조절에 관한 최근 연구 동향)

  • Kim, Jong-Yoon;Koh, Hyeong-Gyun;Nam, Sang-Soo
    • Journal of Acupuncture Research
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    • v.23 no.1
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    • pp.145-154
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    • 2006
  • Objectives : To research the recent trends of study related to pain modulation of acupuncture. Methods : We searched the resent study related to pain modulation of acupuncture. Results & Conclusion : 1) Early studies demonstrated that the analgesic effects of acupuncture are mediated by opioid peptides in the periaqueductal gray. Recent evidences show that nitric oxide plays an important role in mediating the cardiovascular responses to acupuncture stimulation through gracile nucleus-thalamic pathway. 2) Recent evidences show that acupuncture stimulate gene expression related to pain. 3) By using functional magnetic resonance and positron emission tomography, recent study suggest that acupuncture has regionally specific, quantifiable effects on pain-relevant brain structures.

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