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121.
PTT-119 is an antineoplastic agent in which an alkylating moiety, m-sarcolysine, is linked to two amino acid analogs. Previous studies showed a higher "in vitro" cytotoxicity of PTT-119 when compared to free m-sarcolysine; the mechanisms of this enhanced activity are not completely understood. In this study we incubated peripheral blood cells from 8 chronic lymphocytic leukemia patients with both m-sarcolysine and equimolar concentrations of PTT-119, measuring the intracellular concentration of the alkylating moiety. We observed a significantly higher intracellular concentration of m-sarcolysine in cells incubated with the peptide-bound drug than with the free drug (58.3 +/- 39.6 versus 4.4 +/- 1.9 ng/10(6) cells; P = 0.013). This observation could explain the higher cytotoxic activity of PTT-119 and the lack of cross-resistance with melphalan. 相似文献
122.
A TLC procedure which resolves two molecular species of ethanolamine plasmalogen, Pl-PE-1 and Pl-PE-2, was used to compare the ratio of these two species in myelin isolated from normal appearing white matter from brains of 17 multiple sclerosis (MS) patients, 17 normal (N) individuals, 1 patient with subacute sclerosing panencepha itis (SSPE) and 1 patient with a non-demyelinating neurological disease (OND). One of these species (Pl-PE-2) has been reported to be unique to myelin and has primarily 181 in both the 1 and 2 positions of glycerol. The other species (Pl-PE-1) is also present in other membranes and has primarily a saturated chain in the 1 position and a polyunsaturated chain in the 2 position. The Pl-PE-1 to Pl-PE-2 ratio was quantitated by scanning the plates with a densitometer. The ratio was similar to normal in most of the MS samples, 0.88±0.09, but was much less than normal in 4 of the MS samples and the SSPE sample. This is attributed to increased decomposition or hydrolysis of Pl-PE-1 relative to Pl-PE-2 at some stage, either during the disease process or due to post-mortem decomposition. Although the reason for the enhanced decomposition of Pl-PE-1 is not known it suggests that Pl-PE-2 is more stable chemically. This may be related to the unique occurrence of Pl-PE-2 in myelin. 相似文献
123.
Mario De Rosa Agata Gambacorta Barbara Nicolaus Salvatore Sodano J.D. BuLock 《Phytochemistry》1980,19(5):833-836
Individual di(biphytanyl) diglycerol tetraether lipids from thermoacidophile archaebacteria of the Caldariella series, with differently cyclized biphytanyl components, are separated and shown to have structures 8–12, with the glycerol and biphytanyl components demonstrably both antiparallel and with partial assignments of stereochemistry. Tetraethers with alternative arrangements of the components are absent. The structures allow previous observations on these and related lipids to be rationalized both biosynthetically and phyletically. 相似文献
124.
Ovatifolin and two new sesquiterpene lactones, deacetylovatifolin and arturin (1β-hydroxy-8β-angeloyloxy-eudesmane-4(15),11(13)-diene-6α,12-olide, have been isolated from stems and leaves of Podanthus mitiqui. Two of these compounds showed cytotoxic activity. 相似文献
125.
126.
Dr. Roberto Tosi Nobuyuki Tanigaki Rosa Sorrentino Peter van Mourik Pavol Ivanyi 《Immunogenetics》1982,16(3):187-199
An anti-I-Ek alloantiserum was shown to react with purified human Ia preparation. All Ia preparations tested were actively bound irrespective of their HLA-DR phenotypes. However, from a quantitative point of view, DR7 molecules were significantly less reactive. No reaction was observed with isolated Ia subunits. Only molecules carrying DR determinants, but not those carrying either DC1 or BR4X7 determinants, were bound. 相似文献
127.
A Garnier-Suillerot J P Albertini L Tosi 《Biochemical and biophysical research communications》1981,102(1):499-506
Co(II) interacts with bleomycin in aqueous solution, in the presence of air, to give a short lived mononuclear superoxo-Co(III) complex (I) identified previously, by Sugiura, by electron paramagnetic resonance measurements. This complex rapidly releases O2 to yield the dinuclear μ-peroxo-Co(III) complex (II), but is stabilized by the presence of DNA yielding a new superoxo long lived species (I′). The absorption and circular dichroism spectra of the three species (I,I′,II) have been characterized. 相似文献
128.
Giuliano Gazzotti Enrico Garattini Mario Salmona 《Chemico-biological interactions》1981,35(3):311-318
Apparent Km- and Vmax-values of nuclear styrene 7,8-oxide hydrolase were determined at different protein concentrations. In the protein concentrations range used no significant differences in the apparent Km-values were observed. The influence of the incubation with different modifiers (i.e. SKF-525A, metyrapone, 1,2-epoxy-3,3,3 trichloropropane, cyclohexene oxide) at two different concentrations on this enzyme activity was also determined. Cyclohexene oxide and 1,2-epoxy-3,3,3-trichloropropane, two well known inhibitors of the microsomal epoxide hydrolase(s) caused a marked inhibition, metyrapone had a strong activating effect whereas SKF-525A had no effect. In vivo pretreatment with phenobarbital significantly induced the nuclear epoxide hydrolase whereas β-naphthoflavone caused a lower degree of induction. This pattern is quantitatively different but qualitatively very similar to the microsomal one. Moreover a toxifying to detoxifying enzymatic activity balance is attempted for the metabolization of the alkenic double bond of styrene, taking into account the ratio between the styrene monooxygenase (toxifying enzyme) and the styrene 7,8-oxide hydrolase (detoxifying enzyme) after the above mentioned pretreatments, both in the microsomal and nuclear fractions. 相似文献
129.
Byung K. Kim Manfred Steiner Mario G. Baldini 《Biochemical and biophysical research communications》1980,97(3):1227-1232
The receptor site for antithrombin III (AT III) was investigated in normal human platelets. [125I] iodinated AT III was utilized as tracer for the binding assay. Equilibrium of AT III binding was reached within 2 min. The binding capacity was pH-dependent with the optimum around pH 7.0. Binding specificity was demonstrated by inhibition of [125I] AT III ligation using an excess amount of non-labeled AT III. The AT III·heparin complex did not supress [125I] AT III binding. Analysis of binding data by Scatchard plot revealed a single class of binding sites with Kd of 3.2 × 10?7 M and binding capacity of 3840 per platelet. 相似文献
130.
De Moraes DJ Abilio FM Cunha M Feitosa LA Aragão E Cysne E Vieira R Glavam HC Zaniolo W Netto MS Villela RD Labrunie P 《Cardiovascular diseases》1979,6(2):144-152
Thirteen patients were submitted to direct myocardial revascularization (saphenous vein graft) without the use of an artificial oxygenator. The perfusion was done by a left ventricle-to-aorta bypass and autogenous oxygenation. Most patients had three grafts implanted plus endarterectomy of the distal right coronary artery. There was one hospital death that was apparently not related to the method used. Perfusion time ranged from 45 minutes to 4 hours. Body temperature during perfusion was kept between 25 and 30 degrees C. Perfusion flow was maintained between 25 to 50 ml per kg of body weight per minute. Ischemic, hypothermic cardiac arrest was employed. We demonstrated for the first time that perfusion for this kind of heart surgery could be done with no artificial oxygenators and, apparently, is safer for the patients. There were no bleeding problems even in perfusions as long as 4 hours. There was no respiratory dysfunction, and artificial respiration was used for only 6 to 12 hours. The patients awoke at the end of surgery with no signs or symptoms of central nervous system damage, and vasopressor drugs were rarely used after surgery. Although the experience is very small, it suggests that many postoperative problems, especially those related to bleeding and respiratory dysfunction may be reduced or eliminated by this new method. 相似文献