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911.
912.
RITA PEREGO LUIGIA GOZZINI EMANUELE ARLANDINI GIORGIO BOLIS ROBERTO DE CASTIGLIONE 《Chemical biology & drug design》1995,46(5):341-345
Endothelin-1 (ET), the most potent vasoconstrictor yet discovered, is a peptide containirig 21 amino acids with two intrachain disulfide bridges. With the aim of obtaining two-chain derivatives, Et was submitted to chemical and enzymatic treatments. Reaction of ET with CNBr in 70% HCOOH gave, in addition to the expected [Hse7 lactone]-7,8-seco-ET and unreacted material, a by-product whose molecular weight was 25 m.u. greater than that of ET. When the reaction mixture, after lyophilisation, was immediately quenched with NH3-saturated dry MeOH, two products could be recovered in a 5:1 ratio, both obtained by nucleophilic attack of the homoserine lactone: the expected [Hse7-NH2]-7,8-seco-ET and [Hse7]ET, resulting from competitive intramolecular reaction of the deprotonated α-amino group of the Asp8 residue. The Lys9-Glu10 bond turned out to be very resistant to enzymatic attack both by Lys-C-endopeptidase and trypsin. The 9,10-seco-ET derivative could be obtained by treatment with Lys-C-endopeptidase only by using a high enzyme/ET ratio and after a prolonged incubation time. Cleavage of the Lys9-Glu10 bond could not be achieved by treatment with trypsin, even with a high enzyme/substrate ratio. The main product was 13, 14-seco-ET, deriving from the action of chymotripsin (present as an impurity in the trypsin preparation) on Tyr13. The structure of these peptides was confirmed by amino-acid sequence analysis and fast atom bombardment mass spectrometry (FAB-MS). Nicking of the ET structure at different positions had different impact on the biological properties of the resulting derivatives. © Munksgaard 1995. 相似文献
913.
Abstract Nitric oxide (NO) plays an important physiological role in regulating gastrointestinal motility. Involvement of endogenous NO was evaluated in the response to non-adrenergic, non-cholinergic (NANC) nerve stimulation of the dog sphincter muscle of Oddi. Transmural electrical stimulation (TES), nicotine (10?5M) and K+ (10 mM) produced only a relaxation in the sphincter muscle strips contracted with substance P, which was not potentiated by atropine. The TES-induced relaxation was abolished by tetrodotoxin (3 times 10?7 M) and oxyhaemoglobin (1.6 times 10?5 M), but not affected by atropine (10?7 M), propranolol (10?7 M), phentolamine (10?7 M), indomethacin (10?6 M), chole-cystokinin (CCK, 10?8 M) and vasoactive intestinal polypeptide (VIP, 10?8 M). The relaxation was also abolished by treatment with NG-nitro-L-arginine (L-NA, 10?5 M), an NO synthase inhibitor. Nicotine produced a transient relaxation, which was abolished by tetrodotoxin, hexamethonium (10?5 M) and L-NA, but not affected by atropine and NG-nitro-D-arginine (D-NA, 10?5 M). The addition of K+ elicited a transient relaxation, which was abolished by tetrodotoxin and L-NA. The inhibitory effects of L-NA were antagonized by L-arginine (10?3 M). The presence of neurons containing nicotinamide adenine dinucleotide phosphate (NADPH)-diaphorase was histochemically demonstrated in the sphincter of Oddi. These findings may indicate that TES, nicotine and K+ liberate NO from NANC inhibitory nerve which is involved in the relaxation of the dog sphincter of Oddi. The muscular tone does not seem to be regulated by cholinergic nerves under the experimental conditions used. 相似文献
914.
915.
916.
917.
采用扫描电镜、透射电镜及光镜免疫金银法观察了31例慢性扁桃体炎患者和8例胎儿的扁桃体隐窝上皮结构及其中细胞的分布。电镜观察发现隐窝上皮表面存在三种类型微隐窝开口,其腔内有浸润细胞、异物及细菌。有三种特化上皮细胞(M细胞)覆盖于Ⅲ型微隐窝开口处,其结构与肠道M细胞相似,其数量随扁桃体炎的反复发作而减少。形态表明微隐窝是浸润细胞和外来抗原的出入口。M细胞与抗原的摄取及传递有关。光镜免疫金银法观察证明上皮浸润细胞中多数为OKT_s~+细胞,其中OKT_4~+者又占多数而OKT_s~+细胞较少,这些细胞是隐窝上皮参于免疫应答的结构基础。 相似文献
918.
The edema-producing activity of NNAVPLA2, an acidic phospholipase A2 (PLA2) enzyme from Naja naja atra venom (NNAV), was less potent than that of TMVPLA2 II, a basic PLA; from Trimeresurus mucrosquamatus venom (TMV). These edema-forming effects were greatly suppressed by pretreatment of rats with diphenhydramine/ methysergide or compound 48/80, which reduced the tissue content of histamine and serotonin. Heparin abolished and suppressed the paw edema caused by protamine and TMVPLA2 II, respectively, but had no effect on the NNAVPLA2-induced response. In isolated rat peritoneal mast cells, both PLA2 concentration dependently induced the release of histamine and β-glueuronidase. Again, TMVPLA2 II was more potent than NNAVPLA2. This degranulation effect of mast cells caused by TMVPLA2 II and protamine was inhibited by heparin, while that caused by NNAVPLA2 was unaffected. The edema-forming and mast cell degranulation effects were greatly decreased in both PBPB-modified NNAVPLA2 and PBPB-modified TMVPLA2 II, in which the catalytic activity of the enzymes was completely lost. PBPB-modified TMVPLA2 II-induced paw edema was also suppressed by heparin. Furthermore, this edematous response was totally reversed in rat pretreated with aspirin in combination with diphenhydramine and methysergide. These results suggest that the edema-forming effect of PLA2 is probably dependent on the presence of catalytic, positive charge and pharmacological sites on its molecule. 相似文献
919.
920.
Seishi Inoue Tadayasu Shono Mieko Shono Masayuki Azuma Toshiaki Hirabayashi Oshi Inagaki Hidetaro Mori Yoshikazu Fujita 《Journal of bone and mineral metabolism》1990,8(3):19-23
A case of polycythemia vera complicated by chronic renal failure under maintenance hemodialysis requiring parathyroidectory
(PTH) for secondary hyperparathyroidism (2° HPT) is reported.
A 62 year old female presented with 75000 white blood cells (WBC)/μl, 703×104 red blood cells (RBC)/μl, 23×104 platelets (PLT)/μl, hyperuricemia and hypertension in 1970 and the diagnosis of polycythemia vera was made. Hemodialysis
was started in October 1974 for chronic renal failure. Blood cells in peripheral blood rapidly decreased in number after the
beginning of dialysis, reaching the level of 10000∼20000 WBC/μl, and 150∼250×104RBC/μl. In August 1988, marked bone resorption in X-ray picture and high serum alkaline phosphatase and parathyroid hormone
(PTH) noted along with 17400 WBC/μl, 370×104RBC/μl and 35.9×104PLT/μl.
After subtotal PTX removing 3.21g parathyroid gland, serum PTH rapidly fell. At 3 months after PTX, WBC rose to 23600/μl,
RBC 372×104/μl and PLT 94.0×104/μl. At 6 months, WBC was to 31000/μl, RBC 429×104/μl and PLT 78.0×104/μl, suggesting an inhibitory action of PTH on not only RBC, but also WBC and PLT. 相似文献