This paper was aimed to establish a new method for evaluating the anaphylactoid reaction of 15 batches of Zushima Injection from different manufacturers in vitro. Basophilic leukemia cell line RBL-2 H3 cells were cultured in vitro and Compound 48/80 was selected as positive drug. Real-time cell analysis(RTCA) system was used to detect the changes of cell index(CI) value after drug intervention. The degranulation of RBL-2 H3 cells was verified with the toluidine blue staining technology by observing the changes of cell morphology and skeleton. Clustering method was used to analyze the CI values of 15 batches of Zushima Injection on RBL-2 H3 cells. The results showed Compound 48/80(20 μg·mL~(-1)) significantly changed the cell morphology and cytoskeleton, with obvious degranulation. After adding Compound 48/80, CI value decreased rapidly within 30 minutes, then decreased slowly, suggesting that RTCA system can be used for rapid and sensitive evaluation of RBL-2 H3 cell degranulation. The results of cluster analysis showed that Zushima Injection from different manufacturers had different effects on RBL-2 H3 cells. S1-S8 and Compound 48/80 groups were grouped into one cluster, which suggesting that the sample might have potential clinical anaphylaxis. S9-S15 and the normal control group were grouped into one cluster, suggesting there was no anaphylactoid reaction in the sample. In this study, a rapid in vitro anaphylaxis evaluation technique based on RTCA system and pattern recognition method was established, which can be used for rapid in vitro evaluation of anaphylaxis for traditional Chinese medicine injection.
Anaphylaxis ; Cell Degranulation ; Humans ; Mast Cells ; Medicine, Chinese Traditional ; p-Methoxy-N-methylphenethylamine

<p>OBJECTIVETo evaluate the efficacy of 3 commonly used protocols for management of acute exacerbation of asthma in children.p><p>METHODSTotally 113 asthmatic children were randomized into 3 groups. In group A (53 cases), the children were treated with inhalation of nebulized budesonide suspension plus salbutamol and ipratropium bromide twice daily for 5 days; in group B (41 cases), budesonide plus salbutamol and ipratropium aerosol was administered, and in group C (29 cases), dexathmisone plus aminophylline injection was given once daily for 5 days. All the children received basic treatment with fluid infusion, antibiotics or/and anti-virus medications.p><p>RESULTSThe children in both groups A and C showed effectively controlled asthma attack, with significant differences in the therapeutic effects (P>0.05). In contrast, only a few children showed improvement in group B, suggesting the ineffectiveness of the treatment.p><p>CONCLUSIONNebulized medicine is one of the best means for management of acute asthma exacerbation in children, and inhalation of budesonide suspension plus salbutamol and ipratropium bromide can effectively relieve the asthmatic symptoms in these children with good compliance and convenient administration.p>
Acute Disease ; Adolescent ; Aerosols ; Albuterol ; administration & dosage ; therapeutic use ; Asthma ; drug therapy ; Bronchodilator Agents ; administration & dosage ; therapeutic use ; Budesonide ; administration & dosage ; therapeutic use ; Child ; Child, Preschool ; Drug Therapy, Combination ; Female ; Humans ; Infant ; Ipratropium ; administration & dosage ; therapeutic use ; Male ; Treatment Outcome

OBJECTIVES: This study investigated the optimal combination of 3-component photoinitiation system, consisting of CQ, p-octyloxy-phenyl-phenyl iodonium hexafluoroantimonate (OPPI), and 2-dimethylaminoethyl methacrylate (DMAEMA) to increase the degree of conversion of resin monomers, and analyze the effect of the ratio of the photoinitiator to the co-initiator. MATERIALS AND METHODS: Each photoinitiators (CQ and OPP) and co-initiator (DMAEMA) were mixed in three levels with 0.2 wt.% (low concentration, L), 1.0 wt.% (medium concentration, M), and 2.0 wt.% (high concentration, H). A total of nine groups using the Taguchi method were tested according to the following proportion of components in the photoinitiator system: LLL, LMM, LHH, MLM, MMH, MHL, HLH, HML, HHM. Each monomer was polymerized using a quartz-tungsten-halogen curing unit (Demetron 400, USA) for 5, 20, 40, 60, 300 sec and the degree of conversion (DC) was determined at each exposure time using FTIR. RESULTS: Significant differences were found for DC values in groups. MMH group and HHM group exhibited greater initial DC than the others. No significant difference was found with the ratio of the photoinitiators (CQ, OPPI) to the co-initiator (DMAEMA). The concentrations of CQ didn't affect the DC values, but those of OPPI did strongly. CONCLUSIONS: MMH and HHM groups seem to be best ones to get increased DC. MMH group is indicated for bright, translucent color and HHM group is good for dark, opaque colored-resin.
Ethylamines ; Methacrylates ; Polymers ; Terpenes

BACKGROUND: We developed an ethanol extract of peanut sprouts (EPS), a peanut sprout-derived natural product, which contains a high level of trans-resveratrol (176.75 microg/ml) and was shown to have potent antioxidant activity. OBJECTIVE: We evaluated the potential anti-inflammatory activity of EPS by measuring its antioxidant potential in skin. METHODS: The anti-inflammatory activity of EPS was tested using two models of skin inflammation: oxazolone (OX)-induced contact dermatitis in mice and compound 48/80-treated HaCaT cells. As biomarkers of skin inflammation, cyclooxygenase-2 (COX-2) and nerve growth factor (NGF) levels were measured. RESULTS: OX-induced contact dermatitis was suppressed markedly in mice that were treated with an ointment containing 5% EPS as evidenced by a decrease in the extent of scaling and thickening (p<0.05) and supported by a histological study. COX-2 (messenger RNA [mRNA] and protein) and NGF (mRNA) levels, which were upregulated in the skin of OX-treated mice, were suppressed markedly in the skin of OX+EPS-treated mice. Consistent with this, compound 48/80-induced expression of COX-2 (mRNA and protein) and NGF (mRNA) in HaCaT cells were suppressed by EPS treatment in a dose-dependent manner. As an inhibitor of NF-kappaB, IkappaB protein levels were dose-dependently upregulated by EPS. Fluorescence-activated cell sorting (FACS) analysis revealed that EPS scavenged compound 48/80-induced reactive oxygen species (ROS) in HaCaT cells. CONCLUSION: EPS exerts a potent anti-inflammatory activity via its anti-oxidant activity in both mouse skin and compound 48/80-treated HaCaT cells in vitro. Compound 48/80-treated HaCaT cells are a useful new in vitro model of skin inflammation.
Animals ; Biomarkers ; Cyclooxygenase 2 ; Dermatitis, Contact* ; Ethanol* ; Flow Cytometry ; Inflammation ; Mice* ; Nerve Growth Factor ; NF-kappa B ; Oxazolone ; p-Methoxy-N-methylphenethylamine ; Reactive Oxygen Species ; RNA ; Skin

Phendimetrazine is a medication currently being used to help patients with weight loss. It shares a chemical structure with amphetamines. As such, it shares some of the same toxicities, which can include psychosis. Two cases present good examples of phendimetrazine-induced psychotic disorder. A 30-year old female was admitted to emergency room with visual hallucination, auditory hallucination and aberrant behavior. Another 38-year old housewife was accompanied by her family to evaluate mood swing, auditory hallucination and behavioral change to psychiatric clinic. After evaluation in psychiatric ward, they were confirmed to have causal relation with prescription diet pills. These case reports demonstrate the potential dangers of amphetamine based diet pills. There have been several cases of cardiomyopathies and pulmonary hypertension related to phendimetrazine, but psychosis is something that is rarely recognized in an outpatient setting. Two cases showed the importance of obtaining a careful medication history in all patients and specially recognizing diet pills with an amphetamine base causing psychosis.
Amphetamine ; Amphetamines ; Cardiomyopathies ; Diet ; Emergencies ; Female ; Hallucinations ; Humans ; Hypertension, Pulmonary ; Morpholines ; Outpatients ; Prescriptions ; Psychotic Disorders ; Weight Loss

Contribution of histamine H1- and H2-receptors to the effect of compound 48/80, a potent histamine releaser, upon asphyxiation and body temperature in mice was investigated in the present experiments. Compound 48/80 showed an apparent protective potency against hypoxia and significantly prolonged the latencies for convulsions and death in a dose-dependent manner. Compound 48/80 also decreased the body temperature, which was in relation with the antihypoxic effect. Both the H1-receptor antagonist, dimethindene, and the H2-receptor antagonist, ranitidine, attenuated the hypothermic effect of compound 48/80, indicating the involvement of central histamine through both the H1- and H2-receptors. Ranitidine had no effect on the protective effect of compound 48/80 against hypoxia-induced lethality, whereas dimethindene completely antagonized it. These results suggest that the protective effect of compound 48/80 against hypoxia is mediated through histamine H1-receptors and is not related to its ability to induce hypothermia.
Animal ; Anoxia/*drug therapy/physiopathology ; Body Temperature/*drug effects ; Convulsions/prevention & control ; Male ; Mice ; Mice, Inbred BALB C ; Receptors, Histamine H1/*physiology ; Receptors, Histamine H2/*physiology ; p-Methoxy-N-methylphenethylamine/*pharmacology

Epigallocatechin gallate (EGCG) is a principle phenolic antioxidant found in a variety of plants, including green and black tea. The anti-allergic effect of EGCG is unknown. The purpose of this study is to investigate the effects of EGCG on compound 48/80-induced mast cell activation and passive cutaneous anaphylaxis. For this, the influences of EGCG on the compound 48/80-induced cutaneous reaction were measured in vivo and the effects of EGCG on the compound 48/80-induced mast cell activations were examined in vitro. Results are below: as 1) EGCG significantly inhibited compound 48/80-induced passive cutaneous anaphylaxis, 2) the compound 48/80-induced degranulation, calcium influx and histamine release of rat peritoneal mast cells (RPMCs) were significantly inhibited by the pretreatment with EGCG, and 3) the compound 48/80-mediated inhibition of cAMP level in RPMCs was significantly increased by the pretreatment with EGCG. These results suggested that EGCG, the most abundant polyphenol in green tea, inhibits the compound 48/80-induced mast cell activation and the increase of vascular permeability, and potentially serve as effective therapeutic tools for allergic diseases.
Animals ; Antioxidants/*pharmacology ; Catechin/*analogs & derivatives/pharmacology ; Cyclic AMP/metabolism ; Histamine Release/*drug effects ; Mast Cells/*drug effects/metabolism ; Passive Cutaneous Anaphylaxis/*drug effects ; Rats ; Research Support, Non-U.S. Gov't ; p-Methoxy-N-methylphenethylamine/*antagonists & inhibitors

Animals ; Cromolyn Sodium ; administration & dosage ; Disease Models, Animal ; Intestines ; blood supply ; Mast Cells ; drug effects ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; mortality ; pathology ; p-Methoxy-N-methylphenethylamine ; administration & dosage

<p>BACKGROUNDStudy of the relationship between mast cells and atherosclerosis is mostly dependent on pathological observation and cytology experiments. To investigate the effects of mast cells degranulation on plaque and their possible mechanisms we used apolipoprotein E knockout mice which had been placed perivascular common carotid collar with mast cells degranulator compound 48-80.p><p>METHODSForty apolipoprotein E knockout mice were fed a western-type diet and operated on with placement of perivascular right common carotid collar. Four weeks after surgery, the mice were intraperitoneally injected with compound 48-80 (0.5 mg/kg) or D-Hanks every other day for 4 times. The serum lipids and activity of tryptase were measured. Tissue sections were stained with hematoxylin and eosin. Corresponding sections were stained with toluidine blue and immunohistochemically with antibodies against macrophage-specific antigen, alpha-smooth muscle actin, interleukin-1beta and von Willebrand factor. Simultaneously, basic fibroblast growth factor was detected by in situ hybridization and immunofluorescence.p><p>RESULTSNo pathological change was observed in common carotid non-collar placement but atherogenesis in common carotid collar placement of both groups. There was a significant increase in plaque area ((5.85+/-0.75) x 10(4) vs (0.86+/-0.28) x 10(4) microm(2), P<0.05), the degree of lumen stenosis ((81+/-15)% vs (41+/-12)%, P<0.05), the activity of tryptase in serum ((0.57+/-0.13) U/L vs (0.36+/-0.10) U/L, P<0.05), and the percentage of degranulated mast cells ((80.6+/-17.8)% vs (13.5+/-4.1)%, P<0.05). The expressions of macrophage-specific antigen, alpha-smooth muscle actin, interleukin-1beta, basic fibroblast growth factor and the density of neovessel in plaque were more in the compound 48-80 group than in the control group.p><p>CONCLUSIONSPerivascular common carotid collar placement can promote atherosclerotic plaque formation in apolipoprotein E knockout mice. Compound 48-80 increases plaque area and the degree of lumen stenosis by the mechanism that compound 48-80 promotes proliferation of smooth muscle cells and aggregation of macrophages. Compound 48-80 promotes angiogenesis in plaque. The mechanism is potentially that compound 48-80 increases the expressions of basic fibroblast growth factor mRNA and protein in plaque. Compound 48-80 enhances the expression of interleukin-1beta in plaque.p>
Animals ; Apolipoproteins E ; genetics ; Atherosclerosis ; chemically induced ; genetics ; metabolism ; pathology ; Carotid Arteries ; drug effects ; pathology ; Fluorescent Antibody Technique ; Immunohistochemistry ; In Situ Hybridization ; In Vitro Techniques ; Male ; Mast Cells ; drug effects ; metabolism ; Mice ; Mice, Knockout ; p-Methoxy-N-methylphenethylamine ; pharmacology

Ongoing effort to find novel antiasthmatic drugs led to the design and synthesis of a series of compounds bearing phenyl tetrazole group based on the SAR study. The important intermediate 3-(1H-tetrazol-5-yl) benzenamine was synthesized from m-nitroaniline via cyclization and hydrogenation. Followed by amidation, eight new target compounds were obtained. The structures of these compounds were confirmed with 1H NMR, ESI-MS and elemental analysis. Their non-specific and specific anti-histamine effects in the mast cell were determined. Compound NP03 could inhibit non-specific histamine release induced by compound 48/80 in mast cell of SD rats.
Animals ; Anti-Asthmatic Agents ; chemical synthesis ; chemistry ; pharmacology ; Histamine Release ; drug effects ; Mast Cells ; drug effects ; metabolism ; Molecular Structure ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; Tetrazoles ; chemical synthesis ; chemistry ; pharmacology ; p-Methoxy-N-methylphenethylamine ; pharmacology