Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats

The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO(2) (0.3%), albendazole 2-aminosulfone (ABZ-SO(2)NH(2)) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7).     

Pharmacokinetics,disposition, and plasma concentrations of dimethyl sulfoxide (DMSO) in the horse following topical,oral, and intravenous administration

Compartmental models were used to investigate the pharmacokinetics of intravenous (i.v. ), oral (p.o. ), and topical (TOP ) administration of dimethyl sulfoxide (DMSO ). The plasma concentration–time curve following a 15‐min i.v. infusion of DMSO was described by a two‐compartment model. Median and range of alpha (t _1/2α) and beta (t _1/2β) half‐lives were 0.029 (0.026–0.093) and 14.1 (6.6–16.4) hr, respectively. Plasma concentration–time curves of DMSO following p.o. and TOP administration were best described by one‐compartment absorption and elimination models. Following the p.o. administration, median absorption (t _1/2ab) and elimination (t _1/2e) half‐lives were 0.15 (0.01–0.77) and 15.5 (8.5–25.2) hr, respectively. The plasma concentrations of DMSO were 47.4–129.9 μg/ml, occurring between 15 min and 4 hr. The fractional absorption (F ) during a 24‐hr period was 47.4 (22.7–98.1)%. Following TOP administrations, the median t _1/2ab and t _1/2e were 1.2 (0.49–2.3) and 4.5 (2.1–11.0) hr, respectively. Plasma concentrations were 1.2–8.2 μg/ml occurring at 2–4 hr. Fractional absorption following TOP administration was 0.48 (0.315–4.4)% of the dose administered. Clearance (Cl) of DMSO following the i.v. administration was 3.2 (2.2–6.7) ml hr^?1 kg^?1. The corrected clearances (Cl_F ) for p.o. and TOP administrations were 2.9 (1.1–5.5) and 4.5 (0.52–18.2) ml hr^?1 kg^?1.     

A morphological classification proposal for curimba (Prochilodus lineatus) sperm damages after cryopreservation

The present study evaluated some cryoprotectants and concentrations for curimba (Prochilodus lineatus) semen preservation from a simple methodology of analysis of sperm morphology. Semen of nine males was diluted (1:4) into eight cryosolutions, all of them containing 5% of BTS^? Minitüb, still comprising methanol or dimethyl sulphoxide (DMSO) at four concentrations: 5%, 7.5%, 10% and 12.5%. Morphological sperm analysis was performed on an optical microscope at × 1000 magnification. Damages on the head, midpiece and tail rest (the main and terminal portions) were investigated and classified as primary or secondary, according to the assumed influence on fertilization. There was a linear reduction in the total damages with an increase in the cryoprotectant concentration. Samples with DMSO showed the lowest percentage of fractured tails and tail stumps. The cryopreservation protocol retained the fertilizing potential of the sperm after freezing and both methanol 5% and DMSO 7.5% conferred adequate protection to the curimba sperm cells. Sperm morphology, as pointed out here, must be incorporated into routine fish sperm (cryopreserved or not) analysis once sperm defects influence fertilization directly. To the best of our knowledge, this was the first report on curimba sperm damages after cryopreservation by optical microscopy. The classification model presented in this study can be adequate to tackle fish sperm damages.     

吖啶橙和二甲基亚枫对蚕胚胎发育影响的分析

蚕种解除滞育后,对不同发育阶段的蚕卵涂抹吖啶橙或二甲基亚枫溶液后保护至孵化,调查对蚕胚胎发育的影响,结果蚕胚胎在其发育进程中对吖啶橙涂抹卵表面有2个特别敏感的时期,一是在转青期(催青经过第8天)最敏感,处理区的孵化率只有51.22%,二是在催青的第3天,孵化率为56.40%。提取药物处理过的蚕卵蛋白,经SDS-PAGE电泳,转青期的蚕卵蛋白出现某些蛋白泳带的减少或条带染色有颜色深浅的差异。经双向电泳分析,处理区与对照区有4个蛋白质点的差异。     

缩节胺（DPC）对干旱区杂交棉冠层结构及群体光合生产的调节

 在干旱气候生态条件下,设置常规化调和轻量化调2种方式,以常规棉品种为对照,研究了不同剂量缩节胺（DPC）对杂交棉品种冠层结构及群体光合生产的影响。结果表明,轻量化调下,杂交种标杂A₁和石杂2号棉株主茎第6及以上节间长度明显增加,叶面积指数增大且生育后期下降较缓,光截获量增加;植株叶倾角增大,叶片较直立,冠层开度较大,透光良好,群体光合速率峰值高且高值持续期较长,光合物质积累量明显增加,皮棉产量显著提高。常规棉花品种新陆早13号和新陆早36号第6及以上节间长度变化不大,叶面积指数峰值高但生育后期下降较快,生育后期漏光损失严重,群体光合速率下降,产量显著降低。因此,采用轻量化调,有助于杂交种形成高光效冠层结构,增强群体光合生产能力,发挥其生长优势,提高产量。     

Ganoderic acid DM, a natural triterpenoid, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells

Ganoderic acid DM (GADM) is a triterpenoid isolated from Ganoderma lucidum, a well-known edible medicinal mushroom. In the present study, we found that GADM effectively inhibited cell proliferation and colony formation in MCF-7 human breast cancer cells, which was much stronger than that of MDA-MB-231 breast cancer cells. GADM both concentration- and time-dependently mediated G1 cell cycle arrest and significantly decreased the protein level of CDK2, CDK6, cycle D1, p-Rb and c-Myc in MCF-7 cells. Moreover, GADM obviously induced DNA fragmentation and cleavage of PARP which are the characteristics of apoptosis and decreased the mitochondrial membrane potential in MCF-7 cells. Besides, we also showed that GADM elicited DNA damage as measured by comet assay which is a sensitive method for DNA damage detection. γ-H2AX, a marker of DNA damage, was also slightly up-regulated after treated with GADM for 6h, suggesting that the G1 cell cycle arrest and apoptosis induced by GADM may be partially resulted from GADM-induced DNA damage. These results have advanced our current understandings of the anti-cancer mechanisms of GADM.     

Study on Freezing Storage of Human Dermal Papilla Cells

To explore a safety method of freezing storage of human dermal papilla cells not influencing its biological activity. The enormous dermal papillae isolated newly were freezed with cryoprotective agent including dimathyl sulfoxide and storaged in liquid nitrogen after sinking gradually. At the 1 month, 2 month and 6 month after submersing in liquid nitrogen, the freezing dermal papillaes got revivfication after thawing, inoculated and raised in Dulbecco's Modified eagle's medium. The rate of dermal papillaes attaching to the wall and the cell growth behaviour were observed. Similar to that of islated newly, the rates of dermal papillaes attaching to the wall at 2 days after culture were 90 percents to 95 percents after freezing for 1 month, 2 months and 6 months. The dermal papillae also can culture for dermal papilla cell which exhibites a polygonal cellular morphology and a tendency to form pre-confluent multi-layered cluster after restored in liquid nitrogen. It was approximately 15 days to approach cell fusion in culture bottle. Conclusion It is suggested that freezing storage of human dermal papillaes has no side-effect in their biological characteristics and is worth application in the series experiment of DPC .     

Effect of certain herbicides on growth and pathogenicity of take-all fungus on wheat (Triticum aestivum L.)

Summary The effects of Spray Seed (diquat + paraquat), Roundup (glyphosate), Banvel-D (dicamba), Treflan (trifluralin), Glean (chlorsulfuron) and Dacthal (chlorthal dimethyl) at concentrations of 0–500 ppm product on the vegetative growth, vigour and pathogenicity of Gaeumannomyces graminis var. tritici (Ggt) on wheat were examined. All herbicides with the exception of dicamba and chlorsulfuron inhibited fungal growth on potato dextrose agar (PDA) at concentrations 10–500-fold of rates recommended for use in the field. The vegetative growth of the pathogen growing out of straw colonized on PDA supplemented with 100 ppm diquat + paraquat or glyphosate was reduced by 47.4% and 42.4%, respectively. When portions of these colonies were subcultured onto unamended PDA, their growth and the pathogenicity of straw pieces colonized by these subcultures were found to be unaltered. Straw colonized by Ggt on agar amended with concentrations of diquat + paraquat or at all concentrations of glyphosate produced less root disease in wheat seedlings in comparison to those colonized on unamended agar. It is proposed that the reduced pathogenicity of inocula prepared on agar amended with these two herbicides is due to poor colonization by the pathogen of straw on these media, and that a similar effect on saprophytic colonization in the field could lead to a reduction in the field inocula of the pathogen.     

富马酸二甲酯对汉中柑橘贮藏品质的影响

为了研究新型防霉剂富马酸二甲酯(DMF)对采后汉中柑橘果实贮藏品质的影响,确定DMF在柑橘防腐保鲜方面的效果。笔者分析测定了DMF处理后在常温贮藏的柑橘果实的失重率、呼吸强度、可溶性总糖和维生素C含量的变化。结果表明,DMF处理的柑橘果实在贮藏156天内呼吸强度、失重率显著低于对照组;可溶性总糖含量和Vc含量均大于对照组。表明DMF处理在柑橘保鲜方面有效,可延缓果实的可溶性总糖和Vc的下降,有效抑制柑橘呼吸强度的上升,提高柑橘的贮藏品质。