[Prospective study of traditional Chinese medicine and Western medicine in acute abdomen].
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Abdomen, Acute↗
Biomedical subjects
X Z Wu
Publications and source records attributed to X Z Wu.
[Immune function and abdominal surgery in blood stasis syndrome in patients with gastrointestinal diseases].
52 Patients with Blood Stasis Syndrome (BSS) in abdominal surgical diseases were divided into 3 types according to their symptoms, signs and natures of diseases. Peripheral blood T lymphocyte subsets of these BSS patients and 12 healthy persons were studied with Flow Cytometry and monoclonal antibodies. The immunoglobulins and complements of these cases were also studied. There were no difference in T cell subsets, immunoglobulins and complements between Qizhi-BSS group and normal control. The Shire-BSS group showed that CD8 cell, IgG, IgM, and C1, C3c were increased. These results showed that the immune response increased in this type of BSS patients. In the Qixu-BSS group, the CD3 was nearly normal, and the CD4+, CD4+/CD8+ ratio, and CD16+ were statistically decreased. However, the CD8+ cells markedly increased, the IgG, IgM and IgD were also lowered significantly in this type. The marked morphologic abnormal changes in ultrastructures of T lymphocyte were found in 6 patients with Qixu-BSS group. These results showed that the Qixu type of Blood Stasis Syndrome patients were in the immuno-suppressive status.
Abdomen↗
[Determination of partially cellular and local immune function in patients with spleen deficiency syndrome].
The immune function status as reflected by the peripheral blood OKT system T cell subset classification and the lymphocyte in vitro interleukin 2 (IL2) secretory function were determined in 30 patients with Spleen deficiency syndrome and 20 normal subjects in this study. Experimental results decreased cellular immune function and disturbance of immune regulatory mechanism in the patients. Its manifestations were decreased number of total T lymphocytes and helper T cells (Th), relatively increased suppressor T cells (Ts), abnormal rate of Th to Ts, no marked change of IL2 secretory function of T cell in vitro, increased SIgA level before stimulating with acid but marked decreased SIgA level after stimulating. All these suggest the compensatory stage of local immune function.
Adult↗
Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand.
A series of compounds derived from phencyclidine (PCP) was examined in the sigma receptor and PCP receptor binding assays. The derivatives included compounds containing methylene, ethylene or carboxyl ethylene insertion between the cycloalkyl ring and the amine group of PCP. Various phenyl substitutions, cycloalkyl rings and amines of these derivatives were also examined. The methylene and ethylene insertions decreased the compounds' potencies at PCP receptors, whereas they increased the potencies at sigma receptors. The carboxyl ethylene insertion produced compounds with negligible potencies at PCP receptors while possessing high potencies for sigma receptors. One derivative (PRE-084; 2-(4-morpholino)ethyl 1-phenylcyclohexane-1-carboxylate hydrochloride) had an IC50 of 44 nM in the sigma receptor assay, an IC50 of more than 100,000 nM for PCP receptors and an IC50 higher than 10,000 nM in a variety of other receptor systems. In general, compounds with hydroxy-substituted phenyl groups tended to have decreased potency at sigma receptors, whereas methylphenyl and chlorophenyl substitutions increased potencies. Reduction of cycloalkyl ring size decreased potencies for sigma receptors and quaternized amine groups invariably lowered the compound's potencies. Conformational analysis indicated that PRE-084 fitted onto a pharmacophore model for the sigma ligands. The study describes a new, highly selective ligand for the sigma receptor. The results of this study also confirm distinctly different structural requirements for binding to sigma and PCP receptors and provide a new structural consideration for synthesizing sigma-selective compounds.
Animals↗
Electrophysiological and binding studies on intact NCB-20 cells suggest presence of a low affinity sigma receptor.
Whole cell voltage clamp studies were performed on NCB-20 cells to examine physiological responses to drugs possessing affinities for sigma receptors. Those drugs [haloperidol, alpha-(4-fluoro-phenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutano l (BMY-14802), pentazocine, N-allylnormetazocine (SKF-10047), 3-(3-hydroxyphenyl)-N-(1-propyl)piperidine (3-PPP), phencyclidine, 1-[1-(2-thienyl)cyclohexyl]piperidine (TCP), (+)-5-methyl-10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5,10-imine maleate (MK-801)] caused an apparent inward current, which was due to blockade of a tonic, outward potassium current. The rank order of drug potencies in producing this effect generally resembled the rank orders of sigma-receptor affinities for the drugs, except that a reverse stereoselectivity was observed for several drugs. [3H](+)-SKF-10047 labeled two sites in intact NCB-20 cells (Kd = 49 nM, Bmax = 1.0 pmol/mg protein and Kd = 9.6 microM, Bmax = 69 pmol/mg protein). The high affinity site was similar pharmacologically to the sigma receptor assayed in membrane fragments from NCB-20 cells. However, the low affinity site showed a slightly different profile, highlighted by a reverse stereoselectivity. The rank order of drug potencies was as follows at the low affinity site: haloperidol greater than BMY-14802 greater than (-)-pentazocine greater than (+)-pentazocine greater than (-)-SKF-10047 greater than (-)-3-PPP greater than (+)-SKF-10047 greater than (+)-3-PPP greater than phencyclidine greater than TCP greater than MK-801.(ABSTRACT TRUNCATED AT 250 WORDS)
Animals↗
Protein kinase C in the promyelocytic leukemia cell differentiation of granulocytes.
When the leukemia cells in 14 patients with acute promyelocytic leukemia (APL) were induced by all-trans retinoic acid (RA) treatment, the activity of protein kinase C (PKC) increased with the differentiation. In the control cells, the activity of PKC was only 47 +/- 39.3 pmol.mg-1/min, while it was 149.3 +/- 150.1 pmol.mg-1/min after differentiation. There were 90.1 +/- 7.2% promyelocytes in the control group, and 8.9 +/- 5.6% in the induction group. Therefore, we think that there is a close correlation between PKC and the differentiation of promyelocytic leukemia cells.
Adult↗
[The status and role of integration of traditional Chinese and Western medicine in the development of Chinese medical sciences].
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China↗
[Da cheng qi tang on 45Ca content of the isolated colon smooth muscle from experimental colon obstruction rats].
Da Cheng Qi Tang (DCQT) is a classical prescription of Chinese medicine for treatment of acute intestinal obstruction. In this paper, the isolated colon smooth muscle from normal and experimental colon obstruction (CO) rats were used to study the effect of DCQT on 45Ca content. The results showed that the 45Ca content on isolated colon smooth muscle (microns/g wet tissue, mean +/- S) was 0.043 +/- 0.009 in the normal and 0.057 +/- 0.012 in those treated by DCQT respectively. The content of 45Ca in CO was higher than the normal, DCQT can reduce the content of 45Ca in CO. It is known that the higher level of intracellular CA++ is related to the formation and the development of acute intestinal obstruction. The inhibitory effect of DCQT on 45Ca content may play an important role in the treatment of acute colon obstruction.
Animals↗
Muscarinic regulation of Ca2+ mobilization in a human salivary myoepithelial cell line.
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Atropine↗
Guinea pig vas deferens contains sigma but not phencyclidine receptors.
Homogenates from guinea pig vas deferens were examined for possible existence of sigma receptor and phencyclidine (PCP) receptor using a radioligand binding assay. [3H](+)-SKF-10047 bound saturably in the homogenates to a single population of binding sites with a Kd of 311 and a Bmax of 1090 fmol/mg protein. IC50S of several representative sigma in displacing [3H](+)-SKF-10047 from this binding site were very much similar to the IC50S of those drugs in the brain sigma receptor binding assay. A correlation coefficient of 0.96 was obtained when IC50S from vas deferens were compared with those from the brain assay. Attempts to demonstrate PCP receptors in this tissue using [3H]TCP (N-[1-(2-thienyl)cyclohexyl]piperidine), however, yielded negative results. The results indicate that while guinea pig vas deferens contains sigma receptors, PCP receptors may be absent in this tissue.
Animals↗
The effect of N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) on muscarinic receptor-induced Ca2+ mobilization in a human salivary epithelial cell line.
We have investigated the effect of W-7, a calmodulin (CaM) antagonist, on Ca2+ mobilization in a human salivary epithelial cell line, HSG-PA, after muscarinic receptor stimulation. In a medium containing 1.5 mmol/l Ca2+, W-7 reduced both the maximum peak increase in cytosolic Ca2+ [( Ca2+]i) which follows stimulation by carbachol (Cch, 100 mumol/l) and the sustained nature of the response. Using an experimental approach which allows separate visualization of the intracellular Ca2+ release and extracellular Ca2+ entry phases, W-7 was shown preferentially to inhibit Ca2+ release. At 100 mumol/l W-7, Cch-induced Ca2+ release was completely inhibited, but Cch-induced Ca2+ entry was partially (approximately 40%) maintained. This W-7 residual Ca2+ entry response was abolished when cells were depolarized with high K+ or gramicidin D. W-7 also substantially inhibited Cch-induced inositol trisphosphate (IP3) production (approximately 5%). W-5, a less potent CaM antagonist than W-7, had markedly smaller effects on Cch-induced Ca2+ mobilization and IP3 formation. W-7 (100 mumol/l) completely blocked (comparable to 10 mumol/l atropine) the binding of the muscarinic antagonist [3H] quinuclidinyl benzilate (QNB) to muscarinic receptors on cell membranes, whereas Cch (at 100 mumol/l) had minimal effects on ligand binding. W-7 and W-5 were equipotent in their ability to inhibit [3H] QNB binding. These results suggest that W-7 reduces Ca2+ mobilization in HSG-PA cells by a mechanism which likely involves the antagonism of a CaM regulatory step(s) but may also involve at least a partial blockade of the muscarinic receptor.
Calcium↗
Evidence for two modes of Ca2+ entry following muscarinic stimulation of a human salivary epithelial cell line.
We have investigated muscarinic receptor-operated Ca2+ mobilization in a salivary epithelial cell line. HSG-PA, using an experimental approach which allows independent evaluation of intracellular Ca2+ release and extracellular Ca2+ entry. The carbachol (Cch) dose response of intracellular Ca2+ release indicates the involvement of a single, relatively low-affinity, muscarinic receptor site (K0.5 approximately equal to 10 or 30 microM, depending on the method for [Ca2+]i determination). However, similar data for Ca2+ entry indicate the involvement of two Cch sites, one consistent with that associated with Ca2+ release and a second higher affinity site with K0.5 less than or equal to 2.5 microM. In addition, the Ca2+ entry response observed at lower concentrations of Cch (2.5 microM) was completely inhibited by membrane depolarization induced with high K+ (greater than 55 mM) or gramicidin D (1 microM), while membrane depolarization had little or no effect on Ca2+ entry induced by 100 microM Cch. Another muscarinic agonist, oxotremorine-M (100 microM; Oxo-M), like Cch, also induced an increase in the [Ca2+]i of HSG-PA cells (from 72 +/- 2 to 104 +/- 5 nM). This response was profoundly blocked (approximately 75%) by the inorganic Ca2+ channel blocker La3+ (25-50 microM) suggesting that Oxo-M primarily mobilizes Ca2+ in these cells by increasing Ca2+ entry. Organic Ca2+ channel blockers (verapamil or diltiazem at 10 microM, nifedipine at 1 microM), had no effect on this response. The Oxo-M induced Ca2+ mobilization response, like that observed at lower doses of Cch, was markedly inhibited (approximately 70-90%) by membrane depolarization (high K+ or gramicidin D).(ABSTRACT TRUNCATED AT 250 WORDS)
Calcium↗
[Exocrine function of the pancreas and pathological histology of the stomach in patients with stomach yin deficiency syndrome (SYDS) research on SYDS following abdominal operation or with severe acute abdominal diseases (Part 3)].
Exocrine function of pancreas (BT-PABA test) in 13 patients with SYDS was examined and gastric membrane in 5 cases with SYDS other than gastric diseases was observed under light- and electro-microscopy. The results were as follows: urine rate of recovery of PABA in SYDS was 35. 42 +/- 14.33% and that in the control with same age was 64.70 +/- 10.55%. The rate in SYDS was decreased obviously (P less than 0.001). Under light microscopy gastric mucosa of patients with SYDS showed slight gland degenerative atrophy, smaller cytoplasm, eosinophilic decrease of parietal cells and infiltration of inflammatory cells in interstitial tissue. Under electro-microscopy, the main changes of the gastric mucosa with SYDS were severe mitochondria damage, inflating rough endoplasmic pools and large vacuole at which membrane major particles of ribosomes disappeared, degenerated secretory vessels and formation of myelin figure in parietal cells, decrease of secretory particles in main cells, degeneration in some degree and decrease of nervous secretory particles in G cells and damaged interstitial capillaries. The results in this study suggested that the exocrine function of pancreas in patients with SYDS after abdominal operation or with severe acute abdominal diseases was decreased and there were some damages in energy supply and protein manufacturing systems of the gastric mucosa and functional disturbances of main cells, parietal cells and G cells in patients with SYDS.
4-Aminobenzoic Acid↗
Enhanced sensitivity to behavioral effects of naltrexone in rats.
Rats were trained on a fixed-ratio schedule under which every 30th response produced food reinforcement. Five 3-min periods of fixed-ratio reinforcement were each preceded by a 10-min time-out in which responding had no scheduled consequence. Cumulative dose-effect functions for naltrexone were determined once per week by administering increasing doses during each successive time-out. Initially, only a dose of 100 mg/kg suppressed fixed-ratio responding. After eight exposures to cumulative naltrexone, however, a dose of 10 mg/kg suppressed responding. This shift to the left of the dose-effect function, or supersensitivity, persisted for at least 10-wk when naltrexone was not injected. Pretreatment with either morphine (3.0 mg/kg) or ethylketocyclazocine (0.1 and 1.0 mg/kg) partially prevented the naltrexone-induced decreases in response rates. Neither chlordiazepoxide nor [D-pen2, D-pen5]enkephalin pretreatments appreciably altered the effects of naltrexone. When cumulative doses of 1.0-10.0 mg/kg naltrexone were followed by two saline injections instead of the higher doses of naltrexone, over 8 wk, the naltrexone dose-effect function shifted back to the right. The return to normal naltrexone sensitivity after elimination of the two highest doses suggests that a reliable association between the lower and higher doses in a cumulative dosing procedure can result in conditioned effects to the lower doses. Similar observations of salivation elicited by cumulative naltrexone injections further support the hypothesis that the present naltrexone supersensitivity may involve conditioning processes.
Animals↗
Beta-adrenergic control of cell volume and chloride transport in an established rat submandibular cell line.
Rat submandibular cells treated with methylcholanthrene are able to be propagated in continuous culture while retaining beta-adrenergic responsiveness. A specific clone, RSMT-A5, has been isolated and studied in detail. RSMT-A5 cells possess beta-adrenergic receptors (BARS) as judged by [3H]-dihydroalprenolol ([3H]-DHA) binding studies. [3H]-DHA binds to RSMT-A5 membranes in a specific and saturable manner with respect to time and [3H]-DHA concentration. Specific binding is saturable within three min of incubation, and a Scatchard analysis reveals a single class of high affinity binding sites with an equilibrium dissociation constant of 0.62 +/- 0.03 nM and a receptor density of 101 +/- 4 fmole/mg protein. Antagonist competition studies indicate that the BARs are primarily of the beta 2-subtype. The BARs are functional since isoproterenol stimulation results in an increased intracellular cAMP content, marked morphological change, and decreased cell volume and chloride content. These same responses can be evoked by treating RSMT-A5 cells with 8-bromo-cAMP. Ion transport inhibitors such as bumetanide (an inhibitor of Na/K/Cl cotransport), SITS and DIDS (inhibitors of chloride-bicarbonate exchange), amiloride (an inhibitor of Na-H exchange), ouabain (an inhibitor of Na/K-ATPase), and dipyridamole and 9-anthracene carboxylic acid (chloride channel blockers) fail to inhibit the isoproterenol-stimulated change in chloride content. The effects of either isoproterenol or 8-bromo-cAMP on both chloride content and cell volume can be inhibited by the chloride channel blocker N-phenylanthranilic acid, however. Taken together, our results indicate that RSMT-A5 cells possess a beta-adrenergic receptor system which controls intracellular volume and chloride content by modulating transport processes that are 1) cAMP-responsive and 2) inhibitable by the putative chloride channel blocker N-phenylanthranilic acid.
Adrenergic beta-Agonists↗
Muscarinic receptor regulation of Ca2+ mobilization in a human salivary cell line.
We have studied receptor-mediated Ca2+ mobilization in an established exocrine epithelial cell line (HSG-PA) derived from a human submandibular gland. These cells possess a single class of high-affinity muscarinic cholinergic receptors identified using [3H]-quinuclidinyl-benzilate (Kd = 0.17 +/- 0.07 nmol/l; Bmax = 37 +/- 2 fmol/mg protein; n = 3). The muscarinic agonist carbachol elicits a concentration dependent increase of [3H]-inositol trisphosphate in HSG-PA cells (100 mumol/l; greater than 2 fold by 30 s). Carbachol also results in a rapid, approximately 5-fold increase in cytosolic [Ca2+]. This response is made up of two components, one arising from the release of intracellular Ca2+ (La3+ insensitive; independent of extracellular [Ca2+]), the other from the entry of extracellular Ca2+ (La3+ sensitive; dependent on extracellular [Ca2+]). These Ca2+ mobilizing mechanisms are completely blocked by the muscarinic antagonist atropine (10 mumol/l) but unaffected by several voltage-dependent Ca2+ channel antagonists (verapamil, nifedipine, diltiazem) and by membrane depolarization (incubation in 55 mmol/l KCl). These results demonstrate that HSG-PA cells respond to muscarinic stimulation by mobilizing Ca2+ from an intracellular store and via a receptor-operated Ca2+ entry pathway.
Calcium↗
Studies on the relationship between protein kinase C and differentiation of human promyelocytic leukemia cells induced by retinoic acid.
We studied the differentiation of acute promyelocytic leukemia (APL) cells in 14 patients with APL. After the induction by retinoic acid (RA) the mature cells rose to 60 +/- 11.8% compared to 0.7 +/- 1% of the control, while the promyelocytes declined to 8.7 +/- 6.4% (93.3 +/- 5.6% in the control group). Protein kinase C (PKC) activity was significantly increased to 149.3 +/- 156.2 pmol/mg per min compared to 47 +/- 40.9 of the control (p less than 0.01). In HL-60 cells, the activity of PKC increased also from 52.3 +/- 35 to 129.2 +/- 64.6 pmol/mg per min (n = 10, p less than 0.01) after the induction of differentiation with RA. If the leukemia cells were pretreated with a kind of PKC inhibitor such as trifluoperazine, the increase of PKC activity was inhibited, and the rate of nitroblue tetrazolium reduction decreased from 89.9 +/- 7.7% to 62 +/- 25% (n = 6, p less than 0.01) and the mature cells reduced from 63.1 +/- 11.7% to 19.7 +/- 12.2% (p less than 0.01). We presumed that the activity of PKC is closely related to the differentiation of human promyelocytic leukemia cells induced by all-trans-retinoic acid.
Adult↗
Characteristics of alpha 1-adrenergic receptors in a rat salivary cell line, RSMT-A5.
1. Membrane preparations obtained from RSMT-A5, an established rat submandibular cell line, possess alpha 1-adrenergic receptors as judged by [3H]prazosin binding studies. Scatchard analysis reveals a single class of binding sites with an equilibrium dissociation constant (Kd) of 0.052 nM and a receptor density (Bmax) of 104 fmol/mg protein. 2. These receptors are functional since stimulation by epinephrine results in an increased rate of phosphatidylinositol turnover which is blocked by both phentolamine and phenoxybenzamine. 3. Phenoxybenzamine (10(-5) M) irreversibly blocks 95% of the receptors within 2 min. A kinetic analysis shows that the receptors subsequently reappear at a rate of 6 fmol/mg protein/h. The calculated rate constant for receptor clearance (Kc) is 0.027 hr-1, and the half life (t 1/2) of the receptor is 26 hr. 4. These results are comparable to those reported for alpha 1-adrenergic receptors in the BC3H-1 smooth muscle cell line and suggest that alpha 1-adrenergic receptors in cultured cells, from diverse tissues, display similar characteristics.
Animals↗