Synthesis and biological evaluation of novel bisphosphonates with dual activities on bone in vitro

In an effort to generate novel anti-osteoporosis agents, new bisphosphonates with various benzoyl groups on side chains have been synthesized and evaluated for activities on both bone resorption and bone formation in vitro. Several candidates showed distinct dual activities: promoting bone formation and inhibiting bone resorption.     

MiR-101a-3p Attenuated Pilocarpine-Induced Epilepsy by Downregulating c-FOS

This study aimed to explore the effects and function of microRNA-101a-3p (miR-101a-3p) in epilepsy. Rat model of pilocarpine-induced epilepsy was established and the seizure frequency was recorded. Expression of miR-101a-3p and c-Fos in hippocampus tissues of Rat models were detected by qRT-PCR and western blot. Besides, we established a hippocampal neuronal culture model of acquired epilepsy using Mg²⁺ free medium to evaluate the effects of miR-101a-3p and c-Fos in vitro. Cells were transfected with miR-101a-3p mimic, si-c-FOS, miR-101a-3p?+?c-FOS and its corresponding controls. MTT assay was used to detect cell viability upon transfection. Flow cytometry was performed to determine the apoptosis rate. Western blot was performed to measure the protein expression of apoptosis-related proteins (Bcl-2, Bax, and cleaved caspase 3), autophagy-related proteins (LC3 and Beclin1) and c-FOS. The targeting relationship between miR-101a-3p and c-FOS was predicted and verified by TargetScan software and dual-luciferase reporter assay. The role of miR-101a-3p was validated using epilepsy rat models in vivo. Another Rat models of pilocarpine-induced epilepsy with miR-NC or miR-101a-3p injection were established to evaluate the effect of miR-101a-3p overexpression on epilepsy in vivo. MiR-101a-3p was downregulated while c-FOS was increased in hippocampus tissues of Rat model of pilocarpine-induced epilepsy. Overexpression of miR-101a-3p or c-FOS depletion promoted cell viability, inhibited cell apoptosis and autophagy. C-FOS was a target of miR-101a-3p and miR-101a-3p negatively regulated c-FOS expression to function in epilepsy. Overexpression of miR-101a-3p attenuated pilocarpine-induced epilepsy in Rats in vivo. This study indicated that miR-101a-3p could attenuate pilocarpine-induced epilepsy by repressing c-Fos expression.

     

Efficacy of transgenic rice expressing Cry1Ac and CpTI against the rice leaffolder, Cnaphalocrocis medinalis (Guenée)

Detached leaf bioassays, open field tests and cage tests were conducted to evaluate the control efficacy of two transgenic rice lines, expressing Cry1Ac and CpTI, against Cnaphalocrocis medinalis (Guenée) during 2005-2006 in Fuzhou, China. Bioassay results showed that cumulative feeding areas of C. medinalis on transgenic lines were significantly lower than that on control rice lines at different developmental stages. The corrected mortalities at 96 h after infestation on transgenic lines during six rice growth stages were >90% and 100% during experiments conducted in 2005 and 2006, respectively. In the open field test, there was no significant difference in egg density between transgenic and control lines during early days of infestation, but significant differences were detected in late season, due to serious damage on control lines. Larval densities on control lines were significantly higher than the low larval populations observed on transgenic lines during both seasons. The percentages of plants with folded leaves and percentages of folded leaves on transgenic lines were significantly lower than that on control lines with and without insecticide applications, during the entire season. In cage tests the cumulative numbers of C. medinalis adults derived from transgenic lines were significantly lower than that from control lines with and without insecticide treatments. The high level of efficacy of the two transgenic rice lines against C. medinalis may provide an important basis for reduced insecticide applications, an expansion of alternative pest-control strategies and insect resistance management of Bt rice in the future.     

棉铃虫的飞翔活动

实验研究表明,棉铃虫初羽化个体极少活动,１日龄以后活动趋于频繁。个体日活动以２０：００￣２１：００和３：００￣５：００为２个高峰期,１￣３日龄主要以交配和觅食为主,４日龄以后多表现产卵活动。３￣６日龄成虫的飞翔能力最强,连续吊飞第６日龄个体,其平均累计飞行时间达４１．３０ｈ,平均飞行距离２３９．７ｋｍ,个体最远飞行距离３１１．２９ｋｍ,最长飞行时间５９．６８ｈ,最大飞行速度３．２１ｍ／ｓ。棉铃虫在     

Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents

A series of 4,5-disubstitute-1,2,3-thiadiazole compounds were designed and synthesized as potent anticancer agents, some of them exhibited excellent in vitro and in vivo inhibitory activity.     

Cytotoxicity and binding profiles of activated Cry1Ac and Cry2Ab to three insect cell lines

While Cry1Ac has been known to bind with larval midgut proteins cadherin, APN (amino peptidase N), ALP (alkaline phosphatase) and ABCC2 (adenosine triphosphate‐binding cassette transporter subfamily C2), little is known about the receptors of Cry2Ab. To provide a clue to the receptors of Cry2Ab, we tested the baseline cytotoxicity of activated Cry1Ac and Cry2Ab against the midgut and fat body cell lines of Helicoverpa zea and the ovary cell line of Spodoptera frugiperda (SF9). As expected, the descending order of cytotoxicity of Cry1Ac against the three cell lines in terms of 50% lethal concetration (LC₅₀) was midgut (31.0 μg/mL) > fat body (59.0 μg/mL) and SF9 cell (99.6 μg/mL). By contrast, the fat body cell line (LC₅₀ = 7.55 μg/mL) was about twice more susceptible to Cry2Ab than the midgut cell line (16.0 μg/mL), the susceptibility of which was not significantly greater than that of SF9 cells (27.0 μg/mL). Further, ligand blot showed the binding differences between Cry1Ac and Cry2Ab in the three cell lines. These results indicated that the receptors of Cry2Ab were enriched in fat body cells and thus largely different from the receptors of Cry1Ac, which were enriched in midgut cells.     

棉铃虫蛹和成虫形态特征的数值分析

通过对棉铃虫Helicoverpa armigera(Hubner)及其近缘种的蛹和成虫进行了形态特征变异的数值分析,结果表明：棉铃虫种群内个体变异较大,但种群间相对分化较小,无明显的地理分化,也没有发现棉铃虫种群有稳定变异的地理特征;但发现雄性抱器冠的长、宽、抱器瓣长宽比及抱器瓣长与冠宽比4个特征与纬度有一定的相关性,其相关系数分别为：-0.612,-0.699,0.693和0.691。尽管如此,棉铃虫还是相对比较单一的一个种,而近缘种在阳茎刺和抱器瓣的形态及阳茎端囊上的大刺数等方面有明显而稳定的差异和间断。     

纳米金对PCR扩增效率影响的机制探讨

近年来,纳米金粒子对聚合酶链式反应（polymerasechainreaction,PCR）的增效作用倍受关注,但是其具体的机制仍未明确提出。研究发现在PCR反应中,纳米粒子的增效作用是存在最佳浓度的,增加DNA聚合酶或者小牛血清蛋白（BSA）可以消除纳米金粒子导致的抑制。我们认为,纳米金粒子可能起到了类似于聚合酶B亚基的作用,提高了DNA聚合酶的延伸能力;而过量纳米金对PCR的抑制作用可能与纳米金结合单链DNA产生的位阻效应有关。