Base decomposition of erythromycin A methoxime.
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Biomedical subjects
Publications and source records attributed to X M Huang.
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From Oct 1992 to Dec 1993, 25 cases were done by VATS. They were: Wedge resection of the lung (5), biopsy of mediastinal mass (4), pleural biopsy (4), removal of mediastinal cyst (3), resection of pulmonary bullae and pleurodesis (2), removal of intrathoracic foreign body (2), lobectomy (2), removal of clotted blood of hemothorax (1), resection of malignant mesothelioma (1), and esophageal tumor (1). There was no severe complication. Three procedures of VATS needed to be converted to thoracotomy. All 25 patients were recovery well. The comment was done for indications and contraindications of VATS.
A recombinant retroviral vector was constructed which expressed antisense RNA of c-ets-2, c-myc and N-ras. The pseudotype virus was packaged and rescued by transfection in PA317 cells and used to infect human hepatoma cell line SMMC-7721. After selection with G418, resistant colonies were obtained. Stable integration of retrovirus in infectants was shown by Southern hybridization of genomic DNA and the presence of antisense RNA was detected by RNA dot blot hybridization. It was demonstrated that the antisense RNAs did inhibit the growth of human SMMC-7721 hepatoma cells. The ability to form colony in soft agar and tumorigenicity in nude mice of SMMC-7721 were significantly suppressed by the antisense RNAs. The result implicates the potential value in future cancer gene therapy.
The manometric studies of esophageal motility were performed on 30 normal subjects. Pressures were detected with a 3-microtransducer catheter following wet swallow. The measure, record and data processing were performed with the computer. The values obtained by us were compared with those reported by other laboratories. We consider that this method is simple, quick and accurate.
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Microsurgical tubocanalization was done in 412 patients. 278 women had the operation before the end of December 1987 and were followed up. The overall intrauterine pregnancy rate was 81.3% (92.86% for isthmus-isthmus anastomosis and 87.5% for ampulla-ampulla anastomosis). Two patients had ectopic pregnancy which was followed by term pregnancy subsequently. The factors affecting operative results were analyzed.
The (R)- and (S)-2-butylamides of d-lysergic acid were prepared and evaluated in behavioral and biochemical assays of 5-HT2 agonist activity. In rats trained to discriminate 0.08 mg/kg LSD tartrate from saline, both isomers completely substituted for the training stimulus. Similarly, both isomers were found to possess very high affinity in displacing [125I]-(R)-DOI ([125I]-(R)-1-(2,5-dimethoxy-4-iodophenyl)-2- aminopropane) from rat cortical homogenate 5-HT2 receptors and in displacing [3H]-8-OH-DPAT ([3H]-8-hydroxy-2-(di-n-propylamino)tetralin) from rat hippocampal 5-HT1A receptors. The difference in activity between the two isomeric amides was significant in both the behavioral and binding assays, with the R isomer possessing greater potency. Molecular mechanics were used to predict the active geometries of the subject compounds. It was found that the (R)-2-butylamide has a conformation quite similar to LSD, while the (S)-2-butylamide does not. These results suggest that stereochemical properties of the amide substituent of hallucinogenic lysergamides may exert a critical influence on activity. It is concluded that the conformation of the amide function may directly affect binding through stereoselective interactions with a hydrophobic region on the receptor, indirectly by inducing conformational changes elsewhere in the molecule, or by a combination of these two mechanisms.
alpha-Ethyltryptamine (Monase) is both an inhibitor of monoamine oxidase and a monoamine releasing agent. To determine whether alpha-ethyltryptamine induces serotonergic deficits similar to that of other monoamine releasing agents such as 3,4-methyl-enedioxymethamphetamine (MDMA) and para-chloroamphetamine (PCA), rats were given multiple doses (8 x 30 mg/kg s.c.) of alpha-ethyltryptamine acetate. Serotonin and 5-hydroxyindole acetic acid (5-HIAA) levels and the number of 5-HT uptake sites (determined from [3H]paroxetine binding) were significantly decreased in frontal cortex samples at one week killing. A significant decrease in 5-HT and 5-HIAA levels was also observed in rat hippocampal samples. The results provide evidence that alpha-ethyltryptamine may induce serotonin neurotoxicity similar to that of MDMA and PCA.
There is increasing evidence linking dopamine (DA) to the long-term serotonergic (5-HT) neurotoxic effects of certain substituted amphetamines such as 3,4-methylenedioxymethamphetamine (MDMA). The present study was undertaken to examine the importance of DA metabolism, uptake inhibition and release in the long-term effects of these drugs by combining various dopaminergic agents with an analogue of MDMA that had low neurotoxic liability, namely 5,6-methylenedioxy-2-aminoindan (MDAI). Monoamine and metabolite levels and the number of 5-HT uptake sites (using [3H]paroxetine binding) were determined 3 hours or 1 week after treatments. Combining the monoamine oxidase inhibitors, clorgyline (MAOA selective) or deprenyl (MAOB selective) with MDAI did not result in any long-term reductions of serotonergic markers. Similarly, combining the DA uptake inhibitor GBR-12909 with MDAI did not result in any long-term changes in monoamine levels at 1 week. In contrast, a single pretreatment of posttreatment with the nonvesicular DA releaser S-amphetamine and MDAI resulted in small but significant long-term changes in monoamine levels. More importantly, if a subacute dosing regimen (every 12 hours for 4 days) was utilized, the combination of S-amphetamine with MDAI resulted in a marked long-term decrease in the levels of cortical, hippocampal and striatal 5-HT, 5-HIAA and the number of 5-HT uptake sites. The results are discussed in terms of the significance of DA and especially nonvesicular DA release in the long-term effects of MDMA-like drugs.
Two 2,3-dihydrobenzofuran analogues of hallucinogenic amphetamines were prepared and evaluated for activity in the two-lever drug-discrimination paradigm in rats trained to discriminate saline from LSD tartrate (0.08 mg/kg) and for the ability to displace [125I]-(R)-DOI [( 125I]-(R)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane) from rat cortical homogenate 5-HT2 receptors. The compounds, 1-(5-methoxy-2,3-dihydrobenzofuran-4-yl)-2-aminopropane (6a) and its 7-brominated analogue 6b, possessed activity comparable to their conformationally flexible counterparts 1-(2,5-dimethoxyphenyl)-2-aminopropane (3) and its 4-bromo derivative DOB (5), respectively. The results suggest that the dihydrofuran ring in 6a and 6b models the active conformation of the 5-methoxy groups in 3 and 5. Free energy of binding, derived from radioligand displacement KA values, indicated that addition of the bromine in either series contributes 2.4-3.2 kcal/mol of binding energy. On the basis of surface area of the bromine atom, this value is 2-3 times higher than would be expected on the basis of hydrophobic binding. Thus, hydrophobicity of the para substituent alone cannot account for the dramatic enhancement of hallucinogenic activity. Although this substituent may play a minor role in orienting the conformation of the 5-methoxy group in derivatives such as 4 and 5, there appears to be some other, as yet unknown, critical receptor interaction.
The effects of acupuncture and moxibustion on 376 cases of chemotherapy-induced leukocytopenia was observed in patients with malignant tumors in the intermediary and advanced stages. Findings revealed that the total effect in 121 cases (88.4%) occurred in the group treated with acupuncture and moxibustion with warming needle; while the total effect in 221 cases (90.9%) was in the group treated with moxibustion with ignited moxa cone. A comparison made between the 2 groups showed no significant difference (P greater than 0.05). The total effective rate was 38.2% when compared with the control group using batylalcohol and pentoxyl and so the difference was significant (P less than 0.01). Analysis found that with patients having higher basic WBC value, the effect would be higher. Conversely, those who had lower basic value in their WBCs, the expected effect would be lower. These findings suggest that acupuncture and moxibustion in raising the effect on the white cells were influenced by the extent to which the bone marrow was inhibited, having no relevance to the kind of disease, the chemotherapy regime, and the treatment course which the patient was in.
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The present set of experiments was designed to examine the effects of extension of the alpha-methyl of p-chloroamphetamine (PCA) to an alpha-ethyl. Therefore, the alpha-ethyl homologue of PCA, 1-(4-chlorophenyl)-2-aminobutane (CAB), was compared to PCA in a number of pharmacological assays. CAB was 2-fold less potent than PCA at inhibiting synaptosomal uptake of [3H]5-hydroxytryptamine ([3H]5-HT), and 5-fold less potent at inhibiting uptake of [3H]dopamine ([3H]DA). In drug discrimination assays, CAB was approximately 3-fold less potent than PCA in animals trained to discriminate 3,4-methylenedioxymethamphetamine (MDMA) or its alpha-ethyl homologue, S-(+)-N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (S-(+)-MBDB), from saline. Monitoring with in vivo microdialysis, 10 mg/kg of PCA caused a large increase in extracellular DA and a significant decrease in 3,4-dihydroxyphenylacetic acid (DOPAC) in the striatum. In contrast, 11 mg/kg CAB caused no increase and 22 mg/kg CAB caused only a slight increase in extracellular DA. Both doses of CAB caused a decrease in extracellular DOPAC. The potential 5-HT neurotoxicity of CAB was examined by measuring monoamine and metabolite levels and [3H]paroxetine binding at one week following acute doses. A 10 mg/kg dose of PCA caused an 80% decrease in cortical and hippocampal serotonergic markers, while an equimolar dose of CAB decreased only hippocampal 5-HT and 5-hydroxyindoleacetic acid (5-HIAA) levels. However, 22 mg/kg of CAB produced a 20-40% decrease in all serotonergic markers. Thus, extension of the alpha-alkyl significantly decreases the dopaminergic effects of PCA. The similar decrease in relative 5-HT neurotoxicity and the decreased ability to alter dopaminergic systems in vivo and in vitro supports the involvement of DA in the neurotoxicity of PCA.
A new sesquiterpene lactone named gweicurculactone, along with beta-sitosterol, germacrone, daucosterin and palmitic acid, was isolated from Curcuma kwangsiensis. Its structure has been confirmed by means of spectral and X-ray diffraction analysis.
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