Affection of acupotomy lysis on leu-enkephalin (L-ENK) content in different parts of centrum of rats with knee osteoarthritis / 中国骨伤

<p><b>OBJECTIVE</b>To study the analgesia mechanism of needle-knife lysis in spinal cord and other parts of central nervous system by comparing the changes of Leu-Enkephalin (L-ENK) content in different parts of centrium of rats undergone needle-knife lysis and electro-acupuncture respectively.</p><p><b>METHODS</b>Sixty healthy SD rats were randomly devided into normal control group, model group, needle-knife lysis (NKL) group and electro-acupuncture (EA) group. 4% papain solution mixed with 0.3 mol/L cysteine solutin in the ratio of 1:1, paused for 0.5 h,injected the mixture, 20 microl each time,into the left knee joint cavities of rats in model, NKL, EA groups at the 1st, 4th, 7th day. After 4 weeks in NKL group and EA group were treated with needle-knife lysis and electro-acupuncture, respectively. Three weeks after treatment, samples of spinal cord of the swollen part of rat waists and rat brains were taken from and the content of L-ENK of medulla oblongata, midbrain, pituitary gland, and hippocampus were measured.</p><p><b>RESULTS</b>L-ENK content of model group increased higher than that of normal control group in spinal cord, hippocampus and midbrain (P < 0.01); there were no significant difference between normal control group and modle group on L-ENK in medulla oblongata and thalamus (P > 0.05). After intervening of NKL or EA, L-ENK content of NKL group increased higher in hippocampus than that of model group and EC group (P < 0.05); but L-ENK content of NKL group in midbrain was lower than that of model group (P < 0.05).</p><p><b>CONCLUSION</b>Needle-knife lysis has characteristic of regulation for the L-ENK content in different parts of central nervous system of rats with knee osteoarthritis, and analgesic effect of needle-knife was possibly related with regulation of center L-ENK.</p>

Surgical treatment of large cyst on the mandible by using saggital split ramus osteotomy

Plasma met-enkephalin, beta-endorphin and leu-enkephalin levels in human hepatic encephalopathy

To address the role of the opioid system in the pathogenesis of hepatic encephalopathy [HE] we measured plasma met- enkephalin, beta -endorphin and leu- enkephalin in patients with different grades of HE compared to control subjects and patients with cirrhosis. Plasma met- enkephalin levels were significantly higher in patients with cirrhosis and all grades of HE than controls. Plasma beta levels were similar in the 3 groups. Plasma leu- enkephalin levels were significantly higher -endorphin in HE grades II, III and IV than in controls, patients with cirrhosis and HE grade I patients. Our results support data on the involvement of met- enkephalin and leu- enkephalin in the pathogenesis of HE and provide a rationale for the use of opioid receptor antagonists in the treatment of HE

Vibrational dynamics of morphine in relation to Leu5--and Met5-enkephalins.

A complete normal coordinate analysis of morphine using Wilson's GF matrix method and Urey Bradley force field has been carried out to understand the dynamical behaviour of morphine in relation to Leu5- and Met5-enkephalins. In addition, charge distribution on different atoms of morphine, along with that of Leu5- and Met5-enkephalins using CNDO/2 method is also reported. The similarity in charge distribution on some of the sites of these molecules is indicative of the possible interactions at the same receptor site. It is surmised that the recognition and interaction of active sites with the receptor must be dynamical in nature and for this the modes involving the active sites should play an important role. It is found that the binding to receptors is not static, but a dynamic process.

Novel leu-enkephalin analogue with anti-tumor activity

The goal of this study was to evaluate the anti-tumor activity of two Enkephalin analogues designed and synthesized using a conventional solution method. The anti-tumor activity of these two analogues was studied in-vitro following National cancer institute [NCI] protocol [USA]. The results confirmed that the synthesized Leu- Enkephalin analogue [analogue 1] have a positive effect on all cell lines tested indicating its effectiveness as anti-tumor compound on many cancers especially those of lungs, colon and breast. Met-Enkephalin analogue [ana1ogue II] showed no effect on any type of tumor cells tested. In conclusion analogue I can be considered as a novel promising anticancer compound

possible rolefor an enkephalinergic system in the internal defense mechanism of Biomphalaria alexandrina exposed to Schistosoma mansoni

The present study revealed that in Biomphalaria alexandrina, the coordinated responses to Schistosoma mansoni infection are modulated by receptor-mediated opioid signals. The comprehensive tests in susceptible and resistant snails demonstrated the presence of endogenous opioids in the snail hemolymph [in particular, Leu- enkephalin-like material]. The in vitro treatment of snail hemocytes with synthetic Leu-enkephalin analogue [DADLE] resulted in the modulation of cellular adherence and phagocytic activity. The addition of naloxone, either alone or in combination with DADLE, generally reduced the hemocyte activity indicating opioid-receptor- mediated mechanism. The presence of DADLE or naloxone modulated the level of IL-2-, TNF-gamma- and FNF-alpha-like molecules in S. Mansoni resistant and susceptible snails. Specifically, DADLE and DADLE in combination with naloxone, generally, were found to be capable of modulating the resistant snail hemocytes at concentrations of 10-6 and 10-8 M. Similar actions after incubation with the same concentrations were not detected in the susceptible snails

The postburn change in hypothalamic paraventricular beta-endorphin and the roles of delta-receptor in scalded rats / 中华烧伤杂志

<p><b>OBJECTIVE</b>To investigate the postburn change in hypothalamic paraventricular beta-endorphin and the roles of delta-receptor in scalded rats.</p><p><b>METHODS</b>Male Sprague-Dawley (SD) rats were randomly divided into 3 groups, i.e. ICI174864, DPDPE and control groups. The rats were inflicted with 20% TBSA of III degree scalding on the back by boiling (100 degrees ) water. The postburn change in the tissue content of the hypothalamic paraventricular beta-endorphin was determined by radioimmuno assay (RIA). The effects of delta-receptor in scalded shock rats were investigated by observing the change of the rats'survival time and cardiac indices after the micro-injection of delta-receptor agonist DPDPE or antagonist ICI174864 into the hypothalamic paraventricle.</p><p><b>RESULTS</b>(1) The tissue content of the hypothalamic paraventricular beta-endorphin increased significantly (P < 0.01) at 1, 2 and 4 postburn hours (PBHs) in the scalded rats. (2) When compared with that of control group, the ratio of the cardiovascular parameters [mean arterial pressure (MAP), dp/dt(max) and HR] were obviously increased at different time points in rats with pre-injection of ICI174864 whereas the ratio was decreased when DPDPE was used. Nevertheless, the change in the heart rate ratio was not obvious whether ICI174864 or DPDPE was used. (3) The average animal survival time in ICI174864 group was much longer than that in DPDPE group.</p><p><b>CONCLUSION</b>An excessive increase in hypothalamic paraventricular beta-endorphin was one of the factors leading to the aggravation of burn shock and earlier death. delta-receptor located in the tissue might have played important roles in the mediation of the action of hypothalamic paraventricular beta-endorphin. It is beneficial to antagonize the action of delta-receptor for the correction of burn shock and for the prolongation of the of life of animals.</p>

Pain-reducing Effect by Transplants of Isolated Xenogeneic Chromaffin Cells in Mouse

OBJECTIVE: Adrenal medullary chromaffin cells are known to release analgesic substances such as opioides and catecholamines. Transplantation of them is a novel method that challenges current approaches in treating chronic pain. The transplantation of xenogeneic chromaffin cells into the central nervous system(CNS) supply antinociception in animals. In this study, we investigated the analgesic effects of rat adrenal medullary chromaffin cells transplanted into the CNS of the mouse. To study the antinociceptive efficacy of transplanted chromaffin cells, the survival of rat adrenal medullary chromaffin cells transplanted into the CNS of mouse was determined. METHODS: The adrenal medullary chromaffin cells isolated from rat were transplanted into the striatum of mouse. These cells were confirmed of the release of Met-enkephalin and Leu-enkephalin by HPLC, and immunoblots for tyrosine hydroxylase(TH). Two weeks after transplantation, we performed immunohistochemistry for TH to determine the survival of implanted cells and assessed pain sensitivity at the same time. RESULTS: The isolated rat adrenal medullary chromaffin cells were positive for anti-TH antibody and released Met-enkephalin and Leu-enkephalin more than rat endothelial cells. Transplanted rat chromaffin cells were stained with anti-TH antibody in striatum of mouse after 2 weeks. Pain sensitivity was reduced on the chromaffin cell-transplanted mouse compared to endothelial cell-transplanted mouse by the hot plate test. CONCLUSION: These results suggest that the rat chromaffin cells were suitably transplanted into the CNS of mouse. This approach could be used as a therapy for reducing of chronic pain induced by cancer or neuronal injury.

Serum butyrylcholinesterase of non-human primate shows amine sensitive aryl acyl amidase and metallopeptidase activities and characteristics similar to those of the human serum enzyme.

Butyrylcholinesterase (BChE) was purified from monkey serum and the catalytic activities were examined. The enzyme has a molecular mass of approximately equal to 74 kDa as seen by SDS-gel electrophoresis. Monkey serum BChE also exhibits an amine sensitive aryl acylamidase (AAA) and a metallocarboxypeptidase activity. The tyramine activation of the aryl acylamidase activity and the metal chelator inhibition of the peptidase activity were characteristics similar to those of the human enzyme. Studies on 65Zn2+ binding and zinc chelate Sepharose chromatography showed that monkey serum BChE and human serum BChE have similar characteristics. Limited alpha chymotrypsin digestion of monkey serum BChE followed by Sephadex gel chromatography cleaved the enzyme into a 36 kDa fragment exhibiting peptidase activity. However the 20 kDa fragment corresponding to cholinesterase and aryl acylamidase activity was not detectable possibly due to the unstable nature of the fragment. Immunological studies showed that a polyclonal antibody against human serum BChE cross reacted with monkey serum BChE. The identical nature of the catalytic activities of human serum BChE and monkey serum BChE supports the postulate that all three catalytic activities co-exist in the same enzyme. This is the first time that purification and characterisation of the monkey serum BChE which has the highest sequence identity and immunological identity with that of human serum BChE, is being reported.

Ontogeny, glycosylation and modulation by dialysis, sodium and nucleotides of the rat brain delta opioid receptor studied with anti-idiotypic antibodies to anti-leucine enkephalin.

Ontogeny of the rat brain delta opioid receptor in 1-60 days old animals has been studied with anti-idiotypic antibodies to anti-leucine enkephalin. It is found that delta opioid receptors are present in rats from birth and attain adult levels by 28 days and these receptors are glycosylated and inhibited by Na+, GTP, ATP and CTP at all ages. Adult membrane-bound and solubilized delta opioid receptors are inhibited to similar extents by Na+ (100 mM), GTP, ATP and CTP (50 microM). Dialysis of the adult membrane-bound receptor led to 81% loss in binding which was restored by 100 mM Na+, 50 microM GTP, ATP and CTP to 77, 72, 87 and 94% respectively and by 100 mM NH4+, Mg2+, Ca2+ and Mn2+ to 63, 43, 57 and 73% respectively. Dialysis of the solubilized receptor resulted in 23% loss in binding with Na+ (100 mM), GTP and ATP (50 microM) inhibiting receptor binding to 46, 62 and 54% respectively, while CTP (50 microM) restored binding to 88%. These studies indicate that the delta opioid receptor can be probed with anti-idiotypic antibodies to anti-leucine enkephalin, that functional, glycosylated receptors are present at birth in rats and that the adult membrane-bound and solubilized receptors are modulated differently by dialysis.

Dynamics of Met5- and Leu5-enkephalin and their receptor binding activity in relation to morphine.

A complete normal coordinate analysis of Met5- and Leu5-enkephalins using Wilson's GF matrix method and Urey Bradley force field has been carried out to understand the dynamical behaviour of enkephalins. In addition, the charge distributions on different atoms of the two enkephalins and morphine using CNDO/2 method are also reported. The similarity in the charge distribution on the part of these two molecules is indicative of the possible interactions at the same receptor site as that of morphine and its derivatives. Apart from the topographical features and charge distribution, binding onto receptor site is not a static but a dynamic process and low frequency modes must play an important role in the recognition process. The significance of the out-of-plane amide VII band and other skeletal modes as characteristic of conformational states of Met5- and Leu5-enkephalins are discussed.

Papel del óxido nítrico en las alteraciones de la hemodinámica sistémica y esplácnica en un modelo experimental de hipertensión portal / Role of nitric oxide in the alterations of the systemic and splanchnic hemodynamics in a experimental model of portal hypertension

Se evaluó el efecto de la Nw-Nitro-L-arginina (L-NNA), un inhibidor específico de la síntesis de óxido nítrico, sobre la hemodinámica sistémica y esplácnica en un modelo experimental de hipertensión portal (ligadura parcial de la vena porta). La administración de L-NNA en los animales con hipertensión portal ocasionó un aumento significativo de la presión arterial media, una reducción del gasto cardíaco y un aumento de la resistencia vascular periférica. A nível de la hemodinámica esplácnica la L-NNA ocasionó un marcado incremento de la resistencia vascular esplácnica con la consecuente disminución del flujo sanguíneo portal. No se observaron cambios singnificativos en la presión portal. El pretratamiento con L-arginina inhibió los efectos hemodinámicos de la L-NNA. Similares niveles plasmáticos de endotoxina se detectaron en ambos grupos de animales. En el grupo control La L-NNA produjo un aumento de la presión arterial media; sin embargo, y a diferencia de lo observado en los animales on hipertensión portal, la administración de L-NNA no se acompaño de cambios significativos en el gasto cardíaco, flujo sanguíneo portal ni resistencia vascular esplácnica. Nuestros resultados sugieren que las alteraciones, tanto de la hemodinámica sistémica como esplácnica, asociadas a la hipertensión portal, pueden ser atenuadas mediante la administración de L-NNA. Asimismo, el aumento de la síntesis de óxido nítrico puede jugar un papel importante en la fisiopatogenia de estos trastornos hemodinámicos

The rat brain delta opioid receptor studied with anti-idiotypic antibodies to anti-leucine enkephalin.

Anti-idiotypic antibodies to anti-leucine enkephalin raised in rabbits immunized with leucine enkephalin conjugated to BSA, were purified and characterized for their ability to mimic leucine enkephalin in binding to the rat brain delta opioid receptor. An ELISA was standardized to assay the delta opioid receptor using these antibodies. The rat brain receptor was purified to 308 fold with a yield of 1.5% using these antibodies for assay. The receptor, probed with these anti-idiotypic antibodies, was characterized with respect to binding parameters, molecular weight and effect of divalent cations.

Plasma enkephalins in hepatosplenic bilharziasis with and without ascites

This study included 50 patients with pure bilharziasis and mixed liver cirrhosis at different clinical stages. They were selected from Inpatient Medical Department, Mansoura University Hospital. Ten healthy individuals were selected as a control group Leucine- and Methionine - enkephalins plasma levels were estimated in all the participants and after their classification into the following groups: group of intestinal billharziasis [10 patients], non - ascetic group [10 BHF patients + 12 patients with mixed cirrhosis] and ascetic group [8 BHF patients + 12 patients with mixed cirrhosis]. This study was shown that plasma enkephalins level is significantly increased in ascetic than in non- ascetic group of patients and this increase is proportional to the degree of derangement of hepatic function

Efeitos das encefalinas sobre o aparelho digestivo / Enkephalins effects on digestive system

A identificaçäo, localizaçäo e propriedades digestivas das encefalina-metionina e encefalina-leucina säo discutidas neste artigo. Interaçöes sinérgicas e antagônicas säo também apresentadas.