Comparison of the metabolism of testosterone undecanoate and testosterone in the gastrointestinal wall of the rat in vitro and in vivo

The metabolism of testosterone undecanoate (TU) and testosterone (T) is studied in the gastrointestinal wall of the rat in vitro. A comparison is made with the in vivo metabolism of these compounds in the rat. The major metabolite first appearing during incubation of TU with the small intestine is T. Incubation of TU or T with the small intestine reveals a great similarity between the metabolite patterns obtained. This is also the case with the patterns derived from portal vein plasma upon oral administration of TU and T. Incubation of different parts of the gastrointestinal tract with TU or T shows that the greatest metabolic activity is located in the wall of the small intestine. Unlike T, TU is metabolized only to a small extent in the wall of the stomach and the large intestine.     

Hormone and mediator content in the blood of the adrenals and in the peripheral blood in hypertension]

The concentration of the fractions of corticosteroids, aldosterone, catecholamines, and cyclic nucleotides (cAMP and cGMP) in blood of the adrenal veins and the activity of renin in blood of the renal veins were studied in 22 patients with stages IIA and IIB hypertensive disease. At the same time the content of these substances in the peripheral blood was determined and compared with the level of steroid and catecholamine excretion in the daily urine. An increase in the content of free 11 OCS and F fractions in the peripheral blood and blood of the adrenal veins was revealed in all patients examined.     

Fluoro-fatty acids and the impairment of cardiac function in the rat in vivo and in vitro

Summary Dichapetalum toxicarium seeds contain long chain fluoro-fatty acids, particularly fluorooleic acid, which in doses as low as 10 mg/kg can cause death. We have used the rat heart both in vivo and in vitro to assess the cardiovascular effects of various doses of the fluoro-oleic acid extract of the seeds ofDichapetalum toxicarium. Intraperitoneal administration of 0.25 ml of seed extract solution/kg body weight (estimated to be equivalent to 10 mg fluoro-oleic acid/kg body weight) or 0.5 ml/kg body weight (equivalent to 20 mg fluoro-oleic acid/kg body weight) resulted in death in all animals (n–6 in each group). The mean time from administration to death was 36.4±4 h and 21.0±2 h, respectively. Death was attributable to severe bradycardia which developed progressively throughout the experiment. Thus, during the first 6 h, heart rate fell by 32.2% from 450±7 beats/min to 305±36 beats/min (p<0.01) in the 0.25 ml/kg group and by 66±10% to 150±20 beats/min (p<0.001) in the 0.5 ml/kg group. Administration of the extract solution alone or oleic acid alone (equivalent to 0.5 ml/kg seed extract) to control rats had no effect. Investigating the effects of the seed extract in vitro, hearts (n=6 in each group) were perfused with buffer containing 0.5 ml/l seed extract (equivalent to 20 mg fluoro-oleic acid/l) or with buffer containing extract solution alone. In control hearts, there were no changes in heart rate or LVEDP over 150 min of aerobic perfusion; there were small declines in coronary flow, LVDP and LVdP/dt_max. Perfusion with seed extract resulted in a progressive decline in heart rate which, over the first 60 min of perfusion, fell by 53±7% from its control value of 323±11 beats/min to 153±20 beats/min (p<0.001). Similarly, significant declines in coronaryflow (fell by 53±12% over 60 min), LVDP (fell by 61±12% over 60 min) and LVdP/dt_max (fell by 63±7% over 60 min) were observed. LVEDP began to increase after 30 min and by 60 min had increased to 2.8±0.4 kPa (control value=0 kPa). Perfusion with oleic acid (20 mg/l) alone had no adverse effect on cardiac contractile function. Metabolic studies showed that the administration of the seed extract resulted in a loss of myocardial high energy phosphates. Thus, ATP and creatine phosphate fell from their control values of 20.6±0.4 and 27.8±0.6 mol/g dry weight to 3.9±0.4 and 2.4±0.4 mol/g dry weight (p<0.001 in each instance), respectively. Lactic acid content increased from 1.4±0.2 to 21.7±1.4 mol/g dry weight (p<0.001). In conclusion, our results indicate that the fluoro-oleic acid-containing extract ofDichapetalum toxicarium exerts its toxic effects by severely reducing cardiac function. In vivo this can lead to death of the animal.     

老年甲状腺功能亢进症的诊治进展

老年甲状腺功能亢进症（简称甲亢）是常见的内分泌疾病。近年来,老年甲亢患病率有逐年增加趋势。但由于其临床表现不典型,容易被误诊或漏诊。由于老年患者伴随疾病多,老年甲亢的治疗方案应以使用抗甲状腺药物为主,且剂量宜偏小,也可采用放射性治疗,不推荐选择手术治疗。治疗时可同时辅以对症及支持疗法,并要密切监测甲状腺功能的变化。     

Difficulties and strategies in the control of schistosomiasis in the Philippines

Schistosomiasis japonica continues to remain a public health problem in the Philippines affecting 10 out of 16 regions with 6.7 million people at risk mostly farmers and fisher folks. Early efforts focused on snail control in the absence of an effective drug against the disease. Discovery of praziquantel shifted control focus from the expensive snail control to a more manageable one involving case detection and treatment. At present, the government's objective is to reduce morbidity by chemotherapy and supplemented with environmental sanitation, health education, and mollusciciding. In the past, external funds infused into government control programs helped a lot in bringing down prevalence rates of the disease in many highly endemic areas. The end of this foreign assistance has expectedly affected implementation of the programs bringing fears of a possible resurgence in many endemic areas. Such anxiety is also founded on the perennial problems of low disease awareness among people at risk, aggravated security problem, poverty and the negative effects of a devolved set-up in the health care delivery system. Experts suggest that the national health department should be more aggressive in dealing with the disease in terms of ensuring implementation and of continuously searching for better and more improved methods of control. Any new strategy should always consider the devolved set up of the health department.     

Calcitonin-like immunoreactivity and calcitonin gene expression in the placenta and in the mammary gland of the rat

Recently, the presence of monomeric CT in plasma and milk was reported by others in a lactating woman surgically thyroidectomized. Similarly, the placenta was thought to be a possible source of CT. Since such findings were based exclusively on immunological arguments, we have investigated the CT gene expression in these rat tissues. CT mRNAs were detected by dot-blot hybridization of total RNAs extracted from rat tissues with a 32P-labelled human CT cDNA probe. Subcellular fractions of each tissue were screened for CT-like immunoreactivity using two different antibodies. With one antibody, extracts of the mammary gland and placenta both produced full displacement of labelled human CT from the antiserum and serial dilutions of the extracts gave displacement curves parallel to that of synthetic human CT, which suggests immunological similarity. However, dilution curves were not parallel for the second antibody, and for both antisera, CT-like immunoreactivity was found in all subsellular fractions from nuclei to cytosols. Immunoprecipitation of translation products from poly (A)+RNAs of placenta showed two major bands around 30 kD. Under stringent conditions, the weak hybridization of placental RNAs seen by dot-blot under less stringent conditions disappeared. Northern analyses of total RNAs from the placenta failed to detect mRNA of 1 k base size like in thyroid glands, but hybridization under weak stringent conditions occurred with larger mRNAs (around 4.4 and 2.4 k bases). Immunoprecipitation of translation products from mRNAs of rat mammary glands showed three major bands around 46, 30 and 20 kD. Dot-blot hybridization of total RNAs extracted from mammary glands was also negative.(ABSTRACT TRUNCATED AT 250 WORDS)     

Peptidergic vasodilator nerves in the peripheral circulation and in the vascular beds of the heart and brain

This overview focusses on the ubiquitous presence of immunohistochemically visible peptidergic nerves with vasodilatory function. The nerve fibres are primarily related to the parasympathetic system (vasoactive intestinal polypeptide or VIP), the sympathetic system including the adrenal medulla (enkephalins) and to the sensory system (substance P as well as calcitonin gene-related peptide, CGRP). Substance P and probably also CGRP seem to be the mediators of antidromic vasodilatation. Enkephalins appear to be released both from nerve endings and from the adrenomedullary cells. The vasodilatory nerve fibres in the heart distribute both to the coronary vessels and to functionally important parts of the myocardium, where interesting relations exist between the peptidergic flow regulation and contractile force. In the brain the sensory and parasympathetic pathways for VIP and substance P/CGRP have recently been mapped in detail, and a new peptidergic intracranial ganglion has been discovered. The selective electrical stimulation of the sensory and postganglionic parasympathetic fibres, respectively, in the brain circulation has been found to evoke a pronounced flow increase which does not appear to involve cholinergic mediation. There is also experimental evidence that the mentioned systems of fibres may interact with each other and with the sympathetic nervous system by way of neuronal cross-talk.     

糖尿病大鼠主动脉超微结构和功能变化及氯沙坦对其影响

目的：探讨不同病程糖尿病大鼠主动脉超微结构和功能变化及血管紧张素II受体（ART）拮抗剂氯沙坦对其影响。方法：雄性SD大鼠随机分为正常对照组（NC），糖尿病对照组（DC），糖尿病治疗组（DL），造模后第5周起DL组每天予氯沙坦20mg/kg,于4，8，16周末测血糖，血浆内皮素（ET－1）和血管紧张素Ⅱ（Ang Ⅱ），8，16周末取主动脉作电镜,观察。结果：8周时，DC组内皮细胞有线粒体肿胀，空泡变，16周时DC组病变加重并内皮细胞广泛坏死脱落，但DL组病变明显减轻，各病程中DC组血浆Ang II均明显升高，ET－1在8周时明显升高，16周时明显降低，16周时DL组与DC组比较Ang II水平明显升高（P＜0．05），ET－1则降低，但P＞0．05，结论：糖尿病大鼠主动脉随病程不同而出现超微结构改变和功能异常，氯沙坦能明显改善这种病理变化，对糖尿病大鼠主动脉有一定保护作用。