西罗莫司纳米脂质载体固化制剂的制备

采用冷冻干燥法以微晶纤维素Avicel PH-101与聚乙烯吡咯烷酮(PVP)K30的混合物(4:1,w,%)为吸附性粉末固化西罗莫司纳米脂质载体分散液,并以再分散时间、平均粒径及分布、流动性和泄漏率等为指标,采用单因素试验优化固化处方。结果表明,3批按优化方法制备的西罗莫司纳米脂质载体固化制剂的休止角为(42.65±0.80)。,振实密度为(0.79±0.03)g/m1,且含量均匀度良好,再分散时间为(10.0±0.4)min,再分散液粒径(132.7+2.6)nm,分布系数0.297±0.01,ξ电位(-12.8±1.05)mV,冻干前后的泄漏率为(10.80±0.41)%。     

芹菜素对2型糖尿病合并非酒精性脂肪肝小鼠脂代谢紊乱的作用及机制研究

目的研究芹菜素对2型糖尿病合并非酒精性脂肪肝小鼠脂代谢紊乱的作用及机制。方法 8周龄雄性db/db小鼠随机分组分为模型组、芹菜素组(50 mg·kg~(-1)·d~(-1)),以雄性C57BL/6J小鼠为正常对照组。各干预8周后,检测小鼠体质量、空腹血糖(FBG)、总胆固醇(CHO)、三酰甘油(TG)、游离脂肪酸(FFA)、天门冬氨酸氨基转移酶(AST)、成纤维细胞生长因子-19(FGF-19)、空腹胰岛素水平(Fins)和胰岛素抵抗指数(HOMA-IR);肝组织HE染色观察肝细胞脂质蓄积; RT-PCR检测肝脏SREBP1c、FAS、Sirt1、PGC1α、CPT1基因表达; Western blot检测PPARα蛋白表达。结果与模型组比较,芹菜素组小鼠体质量、FBG、CHO、TG、FFA显著降低(P0.05,P0.01),FGF-19显著升高(P0.01); HE染色肝细胞脂肪变性程度减轻,胞内脂滴数量减少,细胞排列整齐;肝脏SREBP1c、FAS mRNA表达降低(P0.05,P0.01),Sirt1、PGC1α、CPT1αmRNA表达显著升高(P0.05); PPARα蛋白表达显著升高(P0.01)。结论芹菜素可以改善糖尿病合并非酒精性脂肪肝小鼠肝脏脂肪代谢紊乱,可能是通过下调肝脏SREBP1c、FAS mRNA表达,上调肝脏Sirt1、PGC1α、CPT1α、PPARα表达实现的。     

Dangers of reducing the range of food choice in developing countries

This article is based on a lecture, “Decreasing variety of plant foods used in developing countries” given at the Joint Congress of the Confoederatio Internationalis ad Qualitates Plantarum Edulium Perquirendas (CIQ) and Deutsche Gesellschaft fur Qualitatsforschung (Pflanzliche Nahrungsmittel) E. V. (DGQ) on The Role of Plant Foods in Preventive Medicine, 12–14th September, 1978 at Reading University. The lecture has been published in Qualitas Plantarum, 1979, Vol. 29, Nos. 1–2. Dr. W. Junk b.v. publishers. The Hague, Netherlands.     

Electrophysiological,biochemical and ultrastructural effects of radiotherapy on normal rat sciatic nerve

Abstract

Purpose: The aim of the present study was to evaluate the electrophysiological, biochemical and ultrastructural changes on the rat sciatic nerve after radiotherapy.

Material and Methods: Thirty male Wistar albino rats were divided into three groups as: Control group (n = 10), Group I: 3 months after radiotherapy (n = 10), and Group II: 6 months after radiotherapy (n = 10). Groups I and II were irradiated with a ⁶⁰Co gamma source. A dose of 20 Gy in 10 fractions was applied to Groups I and II. Compound motor action potentials (CMAP) were recorded in all groups. Superoxide dismutase (SOD) and catalase (CAT) activities and malondialdehyde (MDA) levels were measured in the sciatic nerve of rats using the biochemical methods. Ultrastructural changes were determined by electron microscopy.

Results: In Groups I and II, the amplitude of CMAP was significantly lower and the latency was significantly higher than that of the control group. There were no significant differences between Groups I and II regarding the CMAP amplitude and latency. The MDA levels were significantly increased, whereas the SOD and CAT activities were significantly decreased in experimental groups when compared with the control group. However, there were no significant changes in these parameters between Groups I and II. Degeneration in myelinated nerve fibers was observed ultrastructurally only in the experimental groups. Significant changes were observed between the control group and experimental groups in terms of ultrastructural myelin grading score and axonal damage score. No significant differences were found between Groups I and II.

Conclusions: These findings indicated that the dose of 20 Gy in 10 fractions radiotherapy caused neuropathic damages in normal rat sciatic nerve 3 and 6 months after irradiation.     

Biochemical characterization of stallion prostasomes and comparison to their human counterparts

Release of nanometer-sized prostasomes into human and equine semen suggests essential functions in their relationships with sperm cells and the fertilization process. The two types of prostasomes displayed ultrastructural similarities, albeit the human prostasomes were somewhat larger than the stallion prostasomes. A high ratio of saturated fatty acids was characteristic for the two prostasome types. Electrophoretic separation systems revealed an equine prostasomal pattern different from that of human. The 21 distinctive low molecular weight protein spots in the 2D-gel (with no counterparts in human prostasomes) were identified via peptide mass fingerprinting, several of which may be different isoforms. Out of the three high molecular weight bands characteristic for human prostasomes (CD10, CD13, and CD26), CD10 and CD13 were retrieved in equine prostasomes. We present some new proteins of horse prostasomes not found in their human counterparts. Further studies are warranted to reveal the function of these proteins.     

Peripheral artery disease: therapeutic advances

Peripheral arterial disease (PAD), usually caused by atherosclerosis, is defined as an obstructive arterial disease of the lower extremities that reduces arterial flow during exercise or, in advanced stages, at rest. It affects more than 8.5 million people in the USA. PAD may appear as an asymptomatic arterial disease with abnormal noninvasive test results, or as a symptomatic disease presenting with atypical limb pain, classic intermittent claudication, or critical limb ischemia. The spectrum of PAD is not a continuum. Patients who present with critical limb ischemia may have experienced minimum symptoms. PAD results in limitation of exercise and walking ability, described as intermittent claudication. Patients with PAD are physically impaired and have a higher risk of cardiovascular events; therefore, the treatment goals are aimed at decreasing their cardiovascular risk, as well as improving exercise and daily functional performance. Apart from supervised exercise, which is a major treatment modality for patients with PAD, as of yet there have been very few significant pharmacological breakthroughs in the treatment of PAD that increases blood flow to the ischemic limb. Although percutaneous intervention has markedly improved the treatment of PAD, bypass surgery continues to play an important role. For the most part medical therapy for PAD is designed as a secondary prevention for cardiovascular risk. These include antiplatelet therapy, statins, ACE-inhibitors, smoking cessation and possibly antihypertensive therapy. Revascularization is most beneficial for patients with lifestyle limiting symptoms, acute or chronic limb ischemia with resting pain or nonhealing ulcers. In the following review article we will try to explore the clinical role of some of the latest developments in this field.     

Adiponectin: linking the metabolic syndrome to its cardiovascular consequences

Obesity and its related disorders, glucose intolerance, hypertension and hyperlipidemia, collectively named the metabolic syndrome, result in substantial cardiovascular morbidity and mortality. Recent data point to several underlying regulatory mechanisms through which obesity links these various outcomes. Adipose tissue is now understood to function not merely as a passive energy storage depot but as an active endocrine organ, producing a variety of bioactive substances termed adipocytokines. Adiponectin, an adipocytokine first described as the most abundant protein produced by adipocytes, appears to serve as a central regulatory protein in many of the physiologic pathways controlling lipid and carbohydrate metabolism, and to mediate various vascular processes. Adiponectin displays both anti-inflammatory and antiatherogenic properties. Unlike other adipocytokines, its levels are paradoxically decreased in obesity and insulin-resistance states including metabolic syndrome and diabetes, as well as hypertension and coronary artery disease. This review will detail the relationship of adiponectin to various features of obesity and insulin-resistance syndromes, as well as its relationship to the cardiovascular complications of these disorders.     

佛甲草对实验性肝纤维化大鼠脂质过氧化的影响

目的:探讨佛甲草提取液(SLT)对实验性肝纤维化大鼠脂质过氧化的影响。方法:雄性SD大鼠随机分为正常对照组、模型组、阳性对照组(Col,0.1 mg·kg-1)、SLT低剂量组(SLT,4 g·kg-1)、SLT高剂量组(SLT,8 g·kg-1)。采用50%的CCl4花生油溶液灌服制备大鼠肝纤维化模型,期间给予灌服SLT(4,8 g·kg-1)、Col(0.1 mg·kg-1)进行干预,共9周。9周后处死大鼠取固定部位肝组织及血清标本,光镜下观察肝细胞结构和肝纤维化程度,分光光度法检测肝组织匀浆、血清中丙二醛(MDA)含量以及超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px)活性的变化。结果:光镜下可见模型组大鼠肝细胞严重变性、坏死,胶原纤维明显增加;肝组织、血清中MDA含量增高,SOD、GSH-Px活力显著下降。SLT预防给药明显改善大鼠肝细胞结构,减轻肝纤维化程度;明显降低肝纤维化大鼠肝脏及血清MDA含量,显著升高SOD、GSH-Px活性。结论:佛甲草提取液对大鼠肝纤维化有一定的防治作用,其机制可能与抗脂质过氧化损伤有关。     

辣木叶水提物对油酸钠-钠棕榈酸酯诱导的HepG2细胞脂质代谢及抗氧化能力的影响

目的 探讨辣木叶水提物（MOLAE）对脂肪堆积人HepG2细胞的调节作用。方法 制备MOLAE冻干粉;通过CCK-8法检测油酸钠-钠棕榈酸酯（O-P）对HepG2细胞活力的影响、油红O染色检测O-P对细胞脂质堆积的影响、试剂盒法检测O-P对细胞三酰甘油（TG）、总胆固醇（TC）水平的影响,筛选O-P诱导HepG2细胞脂质代谢异常模型的作用浓度及时间;CCK-8法检测辛伐他汀、MOLAE对HepG2细胞活力的影响,筛选安全作用浓度;设立对照组、模型组、辛伐他汀（阳性药,15 μmol·L^-1）组和MOLAE（3.125、6.250、12.500、25.000、50.000 μg·mL^-1）组,除对照组外,其他各组均给予0.4-0.2 mmol·L^-1的O-P诱导细胞脂质沉积,诱导3 h后开始给药,干预24 h后,CCK-8法检测细胞活性,油红O染色观察细胞中脂滴形成情况,试剂盒法测定细胞中TG、TC、谷胱甘肽（GSH）、超氧化物歧化酶（SOD）及丙二醛（MDA）水平。结果 确定造模方式为：0.4-0.2 mmol·L^-1的O-P作用HepG2细胞3 h后开始给药;10、15 μmol·L^-1的辛伐他汀和3.125～100.000 μg·mL^-1的MOLAE作用于HepG2细胞24、48 h后,不影响细胞活力。与模型组比较,不同浓度的MOLAE（3.125、6.250、12.500、25.000、50.000 μg·mL^-1）均能降低TG、TC、MDA水平（P<0.05、0.01）,显著升高GSH、SOD水平（P<0.05、0.01）。油红O染色结果表明,辛伐他汀组和MOLAE组（12.5、25.0 μg·mL^-1）脂滴堆积现象均较模型组有明显改善。结论 MOLAE能够降低O-P诱导的HepG2细胞中TG、TC水平,提高GSH、SOD水平和降低MDA水平,减少细胞中脂质堆积的现象。