A Potent Anticancer Agent of Shikonin Derivative Targeting Tubulin

In this study, a shikonin ester derivative, compound 3g , was selected to evaluate its anticancer activities and we found that compound 3g exhibited better antitubulin activities against the human HepG2 cell line with an IC₅₀ value of 1.097 μM. Furthermore, the inhibition of tubulin polymerization results indicated that compound 3g demonstrated the most potent antitubulin activity (IC₅₀ = 13.88), which was compared with shikonin and colchicine as positive controls (IC₅₀ = 25.28 μM and 22.56 μM), respectively. Compound 3g was simulated to have good binding site with tubulin and arrested the cell cycle at G2/M phase, which also induces apoptosis in HepG2 cells, in which P53 and members of Bcl‐2 protein family were both involved in the progress of apoptosis revealed by western blot. Confocal microscopy observations revealed compound 3g targeted tubulin and altered its polymerization by interfering with microtubule organization. Based on these results, compound 3g functions as a potent anticancer agent targeting tubulin. Chirality 27:274–280, 2015.. © 2015 Wiley Periodicals, Inc.     

The brown seaweed Sargassum hemiphyllum exhibits α-amylase and α-glucosidase inhibitory activity and enhances insulin release in vitro

Diabetes is one of the most prevalent chronic diseases globally. In this study, major polyphenols (17.35 ± 0.93–36.66 ± 2.01 mg/g) and minor fucoxanthin (non detected 15.12 ± 0.09 mg/g) were isolated from water, ethanol, and acetone extracts (WES, EES, and AES, respectively) of Sargassum hemiphyllum. Inhibition of α-amylase, α-glucosidase, sucrose, and maltase activities and stimulation of insulin secretion was greater with AES than with WES or EES and correlated with polyphenol and fucoxanthin concentrations in extracts. Moreover, 250 μg/ml EES and AES significantly increased insulin secretion in the presence of 25 mg/ml glibenclamide to higher levels than those obtained with 50 mg/ml glibenclamide. None of the extracts exhibited cytotoxicity, exacerbated the side effects of glibenclamide, or inhibited glibenclamide-induced insulin secretion. These results suggested that the S. hemiphyllum extracts WES, EES, and AES could be used as pharmaceuticals and functional foods to reduce dosages of synthetic diabetes drugs.     

Effects of Spirogyra arcta on biomass and structure of submerged macrophyte communities

The presence of algae can greatly reduce the amount of light that reaches submerged macrophytes, but few experimental studies have been conducted to examine the effects of algae on biomass and structure of submerged macrophyte communities. We constructed communities with four submerged macrophytes (Hydrilla verticillata, Egeria densa, Ceratophyllum demersum, and Chara vulgaris) in three environments in which 0 (control), 50 and 100% of the water surface was covered by Spirogyra arcta. Compared to the control treatment, the 100% spirogyra treatment decreased biomass of the submerged macrophyte communities and of all the four macrophytes except C. demersum. Compared to the control and 50% treatments, the 100% treatment significantly increased relative abundance of C. demersum and decreased that of E. densa. Therefore, the presence of S. arcta can greatly affect the productivity and alter the structure of submerged macrophyte communities. To restore submerged macrophyte communities in conditions with abundant algae, assembling communities consisting of C. demersum or similar species may be a good practice.     

Population genetic structure of Oryza rufipogon and Oryza nivara: implications for the origin of O. nivara

Ecological speciation plays a primary role in driving species divergence and adaptation. Oryza rufipogon and Oryza nivara are two incipient species at the early stage of speciation with distinct differences in morphology, life history traits and habitat preference, and therefore provide a unique model for the study of ecological speciation. However, the population genetic structure of the ancestral O. rufipogon has been controversial despite substantial study, and the origin of the derivative O. nivara remains unclear. Here, based on sequences of 10 nuclear and two chloroplast loci from 26 wild populations across the entire geographic ranges of the two species, we conducted comprehensive analyses using population genetics, phylogeography and species distribution modelling (SDM) approaches. In addition to supporting the two previously reported major subdivisions, we detected four genetically distinct groups within O. rufipogon and found no correlation between the genetic groups and either species identity or geographical regions. The SDM clearly showed substantial change in the distribution range of O. rufipogon in history, demonstrating that the repeated extinction and colonization of local populations due to multiple glacial–interglacial cycles during the Quaternary was most likely the main factor shaping the confounding population genetic structure of O. rufipogon. Moreover, we found significant differences between the two species in climate preferences, suggestive of an important role for climatic factors in the adaptation, persistence and expansion of O. nivara. Finally, based on the genetic pattern and dynamics of the O. nivara populations, we hypothesize that O. nivara might have independently originated multiple times from different O. rufipogon populations.     

苦荞转录因子基因FtbHLH4的克隆及其对非生物胁迫的应答

根据苦荞花期转录组数据,克隆得到1个苦荞bHLH类转录因子基因,命名为FtbHLH4。采用实时荧光定量PCR技术,分析了非生物胁迫对苦荞芽期FtbHLH4基因表达的影响。序列分析表明,苦荞FtbHLH4基因DNA全长1 852bp,由7个外显子和6个内含子构成,符合GT-AG剪接原则;cDNA序列包含1个1 062bp的开放阅读框,编码353个氨基酸,具有bHLH类蛋白典型的螺旋-环-螺旋保守结构域。在脱落酸(ABA)、NaCl和PEG模拟干旱胁迫下,苦荞芽期FtbHLH4基因表达量均持续上升,至48h时达最大,分别为胁迫前的11.3倍、12.0倍和6.1倍。而在冷胁迫和UV-B胁迫下,苦荞芽期FtbHLH4基因表达量迅速下降,分别于6h和12h降低至胁迫前的24%和23%。研究推测FtbHLH4基因以不同机制参与了苦荞对非生物胁迫的应答过程。     

棉花纤维发育相关基因GhPRP10的克隆及其功能分析

利用电子序列拼接结合RT-PCR技术,从12DPA(开花后天数)棉纤维中克隆到1个编码富含脯氨酸蛋白(PRPs)基因,命名为GhPRP10(登录号KP036633)。GhPRP10基因开放阅读框为684bp,编码228个氨基酸,其中脯氨酸(Pro)含量为34.6%。序列分析发现GhPRP10蛋白具有N端信号肽和富含脯氨酸区域,属于第一类PRPs。实时荧光定量PCR(RT-PCR)结果显示,GhPRP10在棉纤维组织中优势表达,在纤维发育过程中的表达量呈现先升高后降低的趋势,在18DPA纤维中表达量最高。利用Gateway技术构建植物过量表达载体,转入烟草BY-2悬浮细胞,表型观察和细胞长度测量结果显示,转GhPRP10基因细胞比野生型细胞显著增长。根据该基因的组织表达特征和转基因细胞表型分析,推测GhPRP10基因在纤维伸长和次生壁合成过程中发挥作用。