Antiproliferative Activity Against MCF‐7 Breast Cancer Cells by Diamino‐Triazaspirodiene Antifolates

Two triazaspirodienes, having similar phenoxy propyloxy side chain, were identified as potent mammalian dihydrofolate reductase inhibitors; one having a 6,5‐spiro bicyclic ring system (IC₅₀ = 2.3 nm ) and the other a 6,6‐spiro bicyclic system (IC₅₀ = 6.9 nm ). They also showed more than 50% antiproliferative activity against the MCF‐7 breast cancer cells at 20 μm . This study demonstrated the potential lead of the diamino‐triazaspirodienes in anticancer chemotherapeutical agents’ discovery.     

Association of the expressions of platelet-derived growth factor receptor and c-Fos with the biological characteristics of bladder cancer.

OBJECTIVE: To elucidate the relation of platelet-derived growth factor receptor (PDGFR) and c-Fos protein expressions with human bladder transitional epithelial cell carcinoma (BTCC). METHODS: The expressions of PDGFR and c-Fos were investigated in 11 normal bladder tissue samples, 14 adjacent non-carcinoma tissues and 43 BTCC tissues by means of SP immunohistochemical technique. RESULTS: The c-Fos expression was found in the cell nuclei and cytoplasm, and PDGFR in the nuclear membrane, cytoplasm, and cellular membrane. PDGFR and c-Fos were detected in 81.40% and 48.83% of the BTCC tissues respectively, at the rates both significantly higher than those in normal and adjacent non-carcinoma tissues (P<0.05). Correlation between the expression of c-Fos and the tumor grading was noted (P<0.05). The expressions of PDGFR and c-Fos in tumor blood vessels were significantly higher than those in normal vessels. CONCLUSIONS: The expressions of PDGFR and c-Fos might be involved in the development of BTCC, possibly related to the angiogenesis of the tumors. c-Fos expression can indicated the cell proliferative status of the BTCC.     

Ureteral obstruction caused by L-asparaginase-induced pancreatitis in a child with acute lymphoblastic leukemia.

L-asparaginase, an effective antileukemia and antilymphoma agent, is toxic to many organ systems. We report a case of ureteral obstruction caused by L-asparaginase via the inflammatory complication of acute pancreatitis. The patient was an 11-year-old boy with acute lymphoblastic leukemia. Six days after completing a 4-week induction therapy containing 9 doses of L-asparaginase, severe left abdominal pain developed. Abdominal computed tomography showed phlegmon formation anterior to the pancreatic head and in the left posterior pararenal space. The strands of inflammatory soft tissues encased the upper third of the left ureter, causing left hydroureter and left hydronephrosis. The ureteral obstruction resolved after insertion of a double-J catheter that remained in place for 66 days. This case suggests that L-asparaginase may play a role in the pathogenesis of ureteral obstruction in children receiving chemotherapy.     

重氮乳胶反向凝集试验与乳凝试验在血吸虫病临床诊断中的应用研究

本文应用日本血吸虫虫卵单克隆抗体及虫卵可溶性抗原，分别致敏新型免疫微球载体重氮基聚苯乙烯乳胶，制备出血吸虫反向乳凝试剂与乳凝试剂，并用于检测血吸虫病患者血清标本中的相应抗原和相应抗体，以此试验检测１９７份急慢性血吸虫病患者血清标本。结果反向乳凝试剂检出率为９０．４％，乳凝试剂检出率为９５．２％，均高于反向间接血凝法的８５．０％。反向乳凝试验与乳凝试验联合应用，既可早期诊断，又可判断疗效。试验采用玻片凝集法，３ｍｉｎ内即出结果，方法敏感．特异、简便和快速。     

Artificial bone of porous tricalcium phosphate ceramics and its preliminary clinical application

Summary The authors have prepared the artificial bone of porous tricalcium phosphate ceramics according to an appropriate formula and manufacturing technology. Physical and chemical testing shows that it possesses several distinguishing features: the communicating pores and macro/micropores; mean pore size, 380 μm (from 240 μm to 510 μm); porosity, 46.4 %; and compressive strength, 97.4 kg/cm². It consists of CaO (49.09 %) and P₂O₅ (48.84 %). The testing of its biocompatibility shows that it is devoid of systemic or local toxicity, and free of irritation or foreign body response in tissues, and it does not result in hemolysis or mutation. The new bone readily grows into its pores with direct contact to the implanted material. 11 cases of bone defects were treated with this artificial bone with satisfactory results.     

The subdivisions of the intermediolateral nucleus in the sacral spinal cord of the cat

The subdivisions of the sacral intermediolateral nucleus (IML) of the cat have been studied by using a double-labeling technique of retrograde Fluoro-gold (FG) and wheat germ agglutinin-conjugated horseradish peroxidase (WGA-HRP) tracing. The parasympathetic preganglionic neurons (PGNs) that were labeled by the FG injected into the pelvic nerve formed a ‘V’-shaped column known as the sacral parasympathetic nucleus (SPN) in the sacral IML. The neurons that were labeled by the WGA-HRP applied to the lateral parabrachial nucleus (PBL) formed an elongated spindle-shaped column extending throughout the IML of the sacral segments. We designated it by the name of sacral visceral sensory nucleus (SVSN). These findings indicate that the sacral IML of the cat contain two distinct subdivisions, SPN and SVSN.     

DNA flow cytometry in stage IB and II cervical carcinoma

In a retrospective study the prognostic significance of nuclear DNA content was investigated, as measured by flow cytometry, of the tumor specimens from 212 women with nonpretreated FIGO stage IB and II cervical cancer. One-hundred and thirty cases (62%) were found to be diploid, whereas 82 (38%) were aneuploid. Univariate analysis of the follow-up data showed an increased relative risk (RR) for recurrence free survival (RFS) for stage II tumors (RR = 1.87, 95% CI: 1.13–3.10, P = 0.015) and for age (RR = 1.52, 95% CI: 0.66–3.52 and RR = 2.35, 95% CI: 1.19–4.65, P = 0.032). Ploidy showed a relative risk of 1.33 (95% CI: 0.83–2.13, NS). In addition, univariate analysis of overall survival (OS) revealed similar results. For the subgroup of patients with primary surgery ( n = 151), positive pelvic nodes (RR = 5.38, 95% CI: 2.70–10.71, P = 0.0001) and parametrial extension (RR = 2.53, 95% CI: 1.24–5.17, P = 0.011) were significant factors for OS after univariate analysis, the estimated effects on RFS were slightly smaller. Multivariate analysis of RFS for the whole study population showed age, histologic grade and stage with a slightly increased risk, but no effect was significant. Ploidy with an RR of 0.97 (95% CI: 0.58–1.62) seems to have no influence on prognosis. For the subgroup with primary surgery, ploidy again failed statistical significance with an RR of 1.20 (95% CI: 0.58–2.49). Our results suggest that abnormalities of the nuclear DNA content in this homogeneous group of patients are associated with clinical and morphological prognosticators, however, ploidy is not an independent prognostic factor for RFS, or for the whole study population or for the subgroup with primary surgery.     

Effect of Central Muscarine Receptor Blockade with DKJ-21 on the Blood Pressure and Heart Rate in Stress-Induced Hypertensive Rats

Da-Nian Zhu, Long-Mei Xue, Peng Li. Effect of central muscarine receptor blockade. with DKJ-21 on the blood pressure and heart rote in stress-induced hypertensive rats.

The experiments were performed on Wistar or Sprague-Dawley rats of both sexes divided at random into stress and control groups. The rats in the stress groups were put into cages and subjected to electric foot-shocks and noises for 9-15 days, which caused an increase in blood pressure (BP) and heart rate (HR). In hypertensive rats DKJ-21 (4mg/lml) was injected intravenously (i.v.), and 0.5-1.0h after administration the BP and HR dropped from the high level to normotensive level. In normotensive rats, however, administration of DKJ-21 had no effect on BP or HR. In separate groups of normotensive rats, pretreatment of DKJ-21 (4 mg/l ml, i.v.) blocked the pressor and tachycardiac effect induced by microinjection of physostigmine (0.4μg/0.1 /μl/site), corticosterone (40μg/0.1μl/site) or aldosterone (40 μg/0.1 μl/site) into the rostral ventrolateral medulla (rVLM). Furthermore, DKJ-21 also attenuated the enhancement of the pressor response to stimulation of the defense area in the midbrain, which was induced by microinjection of drugs (mentioned above) into the rVLM. These results indicate that i.v. DKJ-21 can selectively block the muscarinic receptors in the rVLM in stress-induced hypertensive rats, which suggests that abnormal enhancement of cholinergic mechanism in the rVLM may be related to hypertensive effects of corticoids in this area.     

手术治疗外展外旋力所致踝关节骨折

手术治疗外展外旋力引起的踝关节骨折３５例，平均随访２年半，满意率为８８．６％。效果不佳者与软组织损伤严重和关节软骨受损有关。恢复腓骨的长度对防止距骨移位与倾斜十分重要。用钢板固定外踝时要使其下端适应腓骨下段的外翻角。下胫腓联合不论是完全还是不全分离，都应用螺钉固定，以增加踝关节稳定性，早期练习活动。三角韧带断裂时，只要腓骨解剖复位与坚强固定，三角韧带可不予修复。对小于胫骨远端关节面２５％的后踝骨折可不予处理。