Search

L'isopropyl-4 anisole est traite a l'aide de l'acide trifluoroacetique deuterie. En plus de l'echange d'hydrogene aromatique attendu, les hydrogenes methyliques du groupe isopropyl sont echanges. La cinetique et le mecanisme de cette derniere reaction sont etudies

The steroid binding properties of the human pancreatic estrogen binding protein (hEBP) in cytosol were studied by equilibrium dialysis. A high ligand specificity of the protein was revealed. hEBP in cytosol binds unconjugated steroid estrogens with a medium affinity (Kd = 10−7M) but does not bind conjugated estrogens or unconjugated androgens, gestagens, glucocorticoids or cholesterol. Quantitation of hEBP by radioimmunoassay in subcellular fractions of human pancreatic tissue indicated that the protein is translocated into different subcellular compartments. Duodenal juice taken from patients following stimulation of pancreatic secretion by food ingestion (Lund's test) showed high hEBP concentrations, and the levels of hEBP changed concomitantly with the levels of pancreatic isoamylase, indicating that hEBP secretion was stimulated by food ingestion. The levels of hEBP in peripheral serum from healthy subjects showed no sex difference, but were positively correlated to age. Highly elevated (10–20-fold) hEBP levels were found in serum from patients wih acute pancreatitis, while normal serum hEBP values were found in other abdominal diseases. It is speculated that hEBP might have a specific role in the transport of estrogens from the peripheral circulation via the pancreas to the duodenum. The elevated hEBP levels in patients with acute pancreatitis indicate that this protein may be used as a marker of cellular damage in the pancreas.

A radioimmunoassay for quantitation of the human pancreatic estrogen binding protein (hEBP) was developed using polyclonal rabbit hEBP antiserum and iodinated purified hEBP. Parallel dose-response curves were obtained when serial dilutions of human serum and of cytosols obtained from human pancreas, prostate and colon were analyzed simultaneously with serial dilutions of purified hEBP standard. Very high levels of hEBP (500–1000 mg/kg wet weight) were found in normal pancreas. High as well as medium levels were found in pancreatic carcinoma tissue and medium values (0.1–1 mg/kg wet weight) in prostate, colon and ovarian tissue. Other tissues and serum from healthy volunteers showed low values, usually below 0.1 mg/kg. When serial dilutions of rat pancreatic cytosol were analyzed in the hEBP assay, [ 125 I]hEBP was displaced by the rat preparation, but the dose-response curves were not parallel to the standard curves, indicating similarity but non-identity between the estrogen binding proteins in human and in rat pancreas.

Etude des effets de la structure de diols, sur le comportement vis-a vis- de l'autooxydation de leurs ethers monoallyliques

A study was made of the effects of some agents on the stability of unphosphorylated pyruvate kinase type L, the enzyme phosphorylated with cyclic 3',5'-AMP-stimulated protein kinase and the subtilisin-modified enzyme form from which the phosphorylatable site had been removed. The phosphorylated pyruvate kinase was found to be the most labile of the enzyme forms at high temperature and in the presence of urea. The circular dichroism spectrum of the phosphorylated enzyme also differed from that of the unphosphorylated and proteolytically modified forms. All three forms of the enzyme showed a high degree of stability over a wide pH range. The unphosphorylated enzyme seemed, however, to be the most sensitive to differences in pH. Only 10% of its maximal activity remained after incubation at pH 10 and 30 degrees C for 30 min, compared with 30% and 75% for the phosphorylated and proteolytically modified forms of the enzyme, respectively. Of the three enzyme forms tested the subtilisin-modified pyruvate kinase was most rapidly inactivated by trypsin. These results taken together suggest that the phosphorylated enzyme has a less ordered structure than the other two enzyme forms studied.

C 17 H 23 NOSSi cristallise dans P2 1 /c avec Z=4; affinement jusqu'a R=0,068. La chaine aminoethylthiomethyl est etendue au maximum et les molecules sont maintenues ensemble par liaisons hydrogene intermoleculaires O-H...N formant des dimeres cycliques

Preparation par cyclisation d'hydroxyacides (catalyse acide) ou de thioglycolate de β-halogenoethyle (catalyse basique); cinetique de l'hydrolyse des oxathianne-1,4ones-2

Etudes theoriques relatives a une reaction d'electrode A±e⇄B, suivie par des reactions homogenes de B

Stereochimie du transfert de proton-1,3 reversible du phenyl-3 o-tolyl-1 cyclohexene au phenyl-1 o-tolyl-3 cyclohexene en presence d'octahydro-1,2,3,4,4a,5,6,7 naphtyridine-1,8

Phospholipids which do not contain choline were found to solubilize Ni(II) in the chloroform phase resulting from the Folch extraction procedure. On the basis of this phenomenon a radioactive assay for such phospholipids was developed using 63Ni(II). This assay can be made rather sensitive by scaling down and can be performed relatively rapidly. The disadvantages are that it does not measure phosphatidyl chlorine or sphingomyelin and that different phospholipids bind different amounts of Ni(II). Alternatively, non-choline-containing phospholipids can be assayed colorimetrically on the basis of their ability to solubilize Cu(II) in the chloroform phase. The failure of phosphatidyl choline and sphingomyelin to bind divalent cations may be due to formation of an intramolecular salt between the negatively charged phosphate group and the positively charged nitrogen.

Synthese a partir de reactif de Grignard, par reaction avec CO 2 et le dichromate de tetrabutyl ammonium

Between 1980 and 1983, 373 patients with clinically resectable rectal adenocarcinoma entered a prospective randomized study aimed to evaluate the effect of short-term preoperative radiotherapy. Protocol violations were identified in 21 instances. Of the remaining 352 patients, 182 were randomized to surgical treatment only (S-group). Immediately, before surgery, 170 patients were irradiated to the pelvic region with 25 Gy (2500 rad) during a 5-day period (RT-group). Of these patients, 59% underwent abdominoperineal excision, 38% anterior resection, and 3% laparotomy only. At surgery distant metastases were discovered in 32 patients (9%). There were no significant differences between the groups in the distribution of age, sex, operative methods, and tumor stage according to the original Dukes' classification. During the follow-up time, ranging between 6 months and 3 years, tumor recurrence occurred in 35 patients, 19 in the S-group and 16 in the RT-group. Fifteen patients in the S-group had pelvic recurrence compared to 10 patients in the RT-group. Distant metastases occurred in six and eight patients, respectively. Two patients in each group had both pelvic and distant recurrence. There was no correlation between tumor recurrence and type of operation. Median time interval from diagnosis to pelvic recurrence was 10 months in the S-group and 16 months in the RT-group. Postoperative complications in the form of wound sepsis were slightly more common in the RT-group. In summary, the applied treatment regimen, is well-tolerated and apparently does not affect the Dukes' stage of the tumor. Although there is no statistically significant difference, there is a trend of less pelvic recurrence in patients receiving preoperative radiotherapy. Cancer 55:1182-1185, 1985.

Methoxylation electrochimique sur electrode de Pt dans le methanol-tetrafluoroborate d'ammonium, du formyl-1 prolinate de methyle. Etude de l'amidoalkylation du malonate de dimethyle et du mesitylene a l'aide du compose prepare

Since 1977 patients living in Stockholm with Stage I breast cancer fulfilling specific criteria are offered breast-conserving treatment. The treatment includes a partial mastectomy and a low-axillary dissection followed by radiotherapy, 5000 rad, to the remaining breast. Between 1977 and 1981, 262 patients underwent the breast conserving therapy. One hundred eighty-six patients had pathologic Stage I tumors. Radiotherapy was given to 158 of those patients. During the follow-up time (6 months to 5 years), 4 of 186 patients had recurrence to the breast. Two of those had not received radiotherapy. Recurrent tumor in regional lymph nodes occurred in 4/186, and distant metastases in 10/186 patients. Six patients have died of their disease. The cosmetic results were favorable overall, but often impaired when surgical complications occurred. A comparison between these results and those obtained in similar patients treated with modified radical mastectomy showed no significant differences in rate of local, regional, or distant recurrence. In selected patients a partial mastectomy with a low-axillar dissection followed by radiotherapy to the remaining breast seems to be an alternative treatment to modified radical mastectomy. Longer follow-up time is needed before final conclusions can be drawn. Cancer 53:1253-1255, 1984.

Etude de l'oxyamination de l'(allyl phenyl) ether et hexene-1 en presence d'un complexe de Pd coordine a la (dimethyl phenyl-1 ethyl) amine

The estrogen binding protein in human pancreas has been purified from pancreatic cytosol by chromatography on Concanavalin-A-Sepharose and hydroxyl-apatite followed by ion-exchange chromatography carried out using a fast-protein liquid chromatography apparatus (FPLC). The purified protein, still able to bind labelled [3H]estradiol, appeared as one single band corresponding to 31 K in SDS-gel electrophoresis. Total amino acid analysis revealed high levels of histidine, glutamic acid and leucine. The capacity of the purified protein to bind estrogens could be increased more than 4-fold by addition of a cytosolic factor, probably being a small peptide, that is present in crude cytosol, but lost during the purification procedure. The iodinated protein does not bind to DNA-cellulose or phosphocellulose, and shows no similarities to estrogen receptor proteins.

Sucrose gradient centrifugation analysis was used to measure estradiol receptor levels in 35 patients with inoperable or recurrent mammary carcinomas that were subsequently treated with the antiestrogen tamoxifen (Nolvadex ICI). Carcinomas from eighteen patients demonstrated specific estradiol binding. Twelve of these patients responded to therapy. Seventeen patients had tumors without measurable estradiol binding. One of these responded to therapy. Tumors binding less than approximately 0.1 fmole of estradiol per μg DN.1 demonstrated a low response rate to tamoxifen (126). Electrofocusing of the estradiol receptor at pH 6.6 in polyacrylamide gel was found to be a quantitative and very sensitive method for the measurement of the estradiol receptor content in mammary carcinoma. Sixteen patients had their tumors analyzed with electrofocusing and all demonstrated some specific estradiol binding. The amount of estradiol binding in tumors from responders to tamoxifen or ovariectomy was approximately 20 times greater than the amount bound in tumors from non-responders. We conclude that there exists a positive correlation between the amount of specific estradiol binding in human mammary carcinomas and their response to subsequent antiestrogen therapy.

Blood and tissue concentrations of doxorubicin (DOX) were assayed after an intraoperative IV test dose of either free DOX 10 mg or its DNA complex 10 mg to patients with gastrointestinal cancer. After administration of the free drug, blood DOX levels decreased in an at least biphasic way, while DOX-DNA gave higher blood concentrations, which decreased slowly with no clear inflexion point on the concentration-time curve within the first hour. Tissue concentrations of DOX did not differ significantly after the two forms of the drug, liver being the tissue with the highest levels, followed by lymph node metastases, tumor tissue, muscle, and normal intestinal mucosa. If skeletal muscle can be used as a substitute for myocardium, lower cardiotoxicity of DOX-DNA than of DOX is not likely to be due to a difference in tissue uptake and retention between the two forms of DOX.

Synthese d'[hydroxy-4' methoxy-3' phenyl]-2 dihydro-2,3 benzofurannemethanol-3 a partir de benzyloxy-2 methoxy-3 benzaldehyde et de benzyloxy-4' methoxy-3' acetophenone

Between November 1, 1976 and December 31, 1981, 826 post-menopausal females with operable breast cancer were included into a trial comparing tamoxifen 40 mg daily for 2 years with no endocrine treatment. Patients without axillary lymph node metastases and tumors less than 30 mm received no other treatment whilst those with more advanced disease were in addition superrandomised to receive postoperative irradiation or 12 courses of CMF. With a mean follow-up of 44 months tamoxifen significantly reduced the incidence of recurrence. There was no significant interaction between the effect of tamoxifen and any other treatment or prognostic subgroup.

L'oxydation des α-hydroxyacides conduit a des aldehydes (si la fonction alcool est secondaire) et a des cetones (si la fonction alcool est tertiaire) ayant un carbone de moins que les hydroxyacides de depart