In vitro mutagenicity of valepotriates

Valepotriates are epoxide-bearing triesters of the monoterpene alcohol 4,7-dimethylcyclopenta-(c)-pyrane isolated from the roots of several Valerianacae species. They are regarded as the main tranquilizing constituents of these drugs.Although the valepotriates valtrate/isovaltrate (VAL) and dihydrovaltrate (DH-VAL) showed a strong alkylating activity against the nucleophilic agent 4-(p-nitrobenzyl)-pyridine (NBP), they were not clearly mutagenic for the strains TA98, TA100, TA1535, and TA1537 of Salmonella typhimurium or for the strains WP2 and WP2 uvrA^– of Escherichia coli in the absence of a metabolic activation system (S9-mix). However, the valepotriates were mutagenic for TA100, WP2 and WP2 uvrA^– at concentrations up to about 1.0 mole/plate when S9-mix was added to the test system. With more than 1 mole/plate the valepotriates were toxic in the presence of a metabolic activation system for all strains tested. The mutagenicity of the valepotriates was inversely related to the protein content of the S9-mix used. The mutagenicity and toxicity of the valepotriates could be inhibited when the S9-mix was preincubated with the esterase inhibitor paraoxon (1 mM) for 5 min before the test compounds and bacteria were added. Therefore, bioactivation of the valepotriates by an enzymatic hydrolysis of their ester groups is considered. This could be proven by activating the valepotriates with purified esterase.Parts of this paper were presented at the Congress, Fortschritte in der Arzneimittelforschung, April 17–20, 1983 in Munich     

新洁尔灭对小白鼠抗早孕的病理组织学观察

本文报告用不同剂量的新洁尔灭和同体积生理盐水注入怀孕5天小白鼠的宫腔内,3天后杀死,观察其蜕膜、胚泡、宫内膜腺体和卵巢黄体病理学改变。实验表明:对照组无改变。实验组小白鼠的蜕膜细胞全部退变坏死。病变随着给药量的递增而渐趋严重;同时胚泡亦有退变和坏死。提示:新洁尔灭对早期妊娠小白鼠是有抗早孕效果的。根据实验结果,我们认为新洁尔灭对小白鼠抗早孕的机制,很可能是一个综合因素,有直接的,也有间接的。作者强调在抗早孕机制诸因素中,蜕膜退变坏死是一个重要的因素。     

Ejaculatory incompetence: a theoretical formulation and case illustration

Three theoretical formulations of ejaculatory incompetence have been proposed in the literature. They include: (1) aversive conditioned inhibition of the ejaculatory reflex, (2) an "autosexual" orientation associated with discrepant levels in the cognitive and physiological dimensions of sexual arousal, and (3) a discriminative learning model. These three models are discussed in relation to their theoretical and therapeutic implications. Clinical data supporting the discriminative view is presented.     

Comparison of α-Tocopherol, α-Tocopherol Acetate,and α-Tocopheryl Polyethylene Glycol Succinate 1000 Absorption by Caco-2 TC7 Intestinal Cells

(1) Background: vitamin E is often supplemented in the form of tocopherol acetate, but it has poor bioavailability and can fail to correct blood tocopherol concentrations in some patients with severe cholestasis. In this context, α-tocopheryl polyethylene glycol succinate 1000 (TPGS) has been of value, but very little is known about the mechanisms of its absorption. The aim of our work was to evaluate the mechanisms of absorption/secretion of TPGS compared to tocopherol acetate (TAC) and α-tocopherol by human enterocyte-like Caco-2 TC7 cells. (2) Methods: two weeks post-confluence Caco-2 cells were incubated with tocopherol- or TAC- or TPGS-rich mixed micelles up to 24 h and, following lipid extraction, TAC and tocopherol amounts were measured by high performance liquid chromatography (HPLC) in apical, cellular, and basolateral compartments. (3) Results: at equivalent concentrations of tocopherol in the apical side, the amounts of tocopherol secreted at the basolateral pole of Caco-2 cells are (i) significantly greater when the tocopherol is in the free form in the micelles; (ii) intermediate when it is in the TAC form in the micelles (p < 0.001); and (iii) significantly lower with the TPGS form (p < 0.0001). Interestingly, our results show, for the first time, that Caco-2 cells secrete one or more esterified forms of the vitamin contained in TPGS at the basolateral side.     

亚急性联合变性的临床分析

目的探讨亚急性联合变性(SCD)的临床特点、发病机制及电生理和磁共振成像的诊断价值.方法对14例SCD患者的临床资料进行回顾性分析.结果发现所有SCD患者发病均由维生素B12缺乏所引起.肢体感觉异常,深感觉减退,共济失调及痉挛性轻瘫是SCD常见的症状和体征.该病早期易误诊,电生理检查有极高的敏感性,磁共振成像可以确定脱髓鞘的部位.结论血清维生素B12浓度测定,体感诱发电位及磁共振对诊断和治疗有重要作用.     

The effects of vitamin B12, vitamin D,ferritin level,neutrophil/monocyte ratio and some blood parameters on genital warts presence,the number of lesions,and recurrence rates

The relationships between cancer caused by HPV and some vitamins, as well as leucocytes and their ratios, have been investigated in the literature. Our aim is to evaluate these relationships at the level of genital wart in terms of the investigated parameters and lesion numbers. Data were obtained from 98 and 94 patients for groups one and two, including warts patients and healthy people respectively. The Neutrophil/Monocyte ratio and lesion numbers in the warts patients were reported and analysed in terms of vitamin B12 and D, ferritin and leucocytes. A correlation was established between lesion numbers, age and midcorpuscular volume (p <0.05). There was no correlation between lesion numbers and recurrence. According to the comparative analysis, there were differences in terms of ferritin, neutrophil, monocyte, haemoglobin, midcorpuscular volume and neutrophil/monocyte ratio between groups. The cut-off values for neutrophil, monocyte and N/M ratios were 56.45, 4.91 and 7.825 respectively. While our study showed that wart development may be affected by blood ferritin levels and in this situation, midcorpuscular volume, neutrophil, monocyte and N/M ratios may change, a relation was found between lesion numbers and age and mean midcorpsucular volume values only. However, further studies are needed to clarify this issue.     

The effect of vitamin E on sperm motility and viability in asthenoteratozoospermic men: In vitro study

Induction of oxidative stress during the sperm preparation process for assisted reproductive techniques (ART) in men can weaken sperm parameters. Vitamin E (VE) is considered a factor in boosting male fertility. This experimental study (in vitro) aimed to assess the impact of VE supplementation on sperm quality and lipid peroxidation during sperm sampling at different times. For this mention, semen samples were collected from 50 asthenoteratozoospermic men. Samples were divided into control and test groups for 2, 4 and 6 hr that the test group was incubated with VE (2 mM). In two groups, total motility, progressive motility and viability based on the WHO 2010 criteria were assessed. Moreover, malondialdehyde (MDA) levels were evaluated in each group. In the control group, total and progressive motility and sperm viability were decreased significantly after 2 hr; however, MDA levels were increased significantly after 6 hr. Also, in the test group, sperm parameters were increased significantly after 2 hr, and MDA levels were decreased significantly after 6 hr compared to the control group. In outcome, in vitro VE supplementation may protect spermatozoa from the adverse effect of oxidative stress during sperm preparation via preservation antioxidant processes in normal condition.