ABSTRACT
Asiatic acid (AA) is a ursane pentacyclic triterpenoids, which possesses a wide range of pharmacological activities, such as anti-tumor, hypoglycemic, anti-inflammatory, anti-bacterial. Due to poor solubility and low bioavailability, clinical application of asiatic acid is limited. To address these defects, the structural modifications of AA have been carried out, and large numbers of AA-based derivatives with novel structure and eximious biological activity have been developed. In this paper, the research progress of structural modifications, biological activity, structure-activity relationship and mechanism studies in recent twenty years are reviewed, which provides reference for development of AA-related drugs.
ABSTRACT
Objective To establish a mouse model for short-term exposure to ambient PM and to investigate the impact on the Cytochrome P450 1A1(CYP1A1)and O6-methylguanine-DNA methyltransferase(MGMT)mRNA expression. Methods Twenty 6-week-old BALB/c mice were randomly assigned to one of two groups, each consisting of 5 male and 5 female animals. These mice were then housed in situ concurrently for 2 weeks in our lab located in urban area of Hangzhou. The first group was kept inside an individual ventilated caging(IVC)system equipped with a high-efficiency particulate-air(HEPA)filter, whereas the second was housed inside a IVC with HEPA filter removed. Then it's allowed flow-through of ambient air freely via a pipeline outside. Mice inside the HEPA filtration chamber were therefore protected from exposure to all airborne particulate. The other was in fact exposed to ambient air directly. After the exposure, the bronchoalveolar lavage(BAL)fiuid was collected for each animal and the differentials and percentages of BAL cells were determined. Paraffin sections of lungs of the mice were made and were examined for any inflammation changes. CYP1A1 and MGMT mRNA levels in the lungs were then detected by RT-qPCR. Results The mean concentration of PM2.5was(99.7±51.6)μg/m3in the exposure group. Weight increases were similar between the two groups(P>0.05). The number of total cells and macrophages in BALF from exposure mice was significantly greater than control.A mild inflammation was observed from light photomicrographs of the lung after PM exposure. CYP1A1 and MGMT mRNA levels were significantly up-regulated in the lung from the exposure group. Conclusion A mouse model for short-term exposure to ambient PM was established. CYP1A1 and MGMT may mediate the toxic effect of PM exposure.
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Objective To investigate the effects of dendrobium officinale leaves on sperm quality and testicular tissue morphology in parent(P)and offspring(F1、F2)rats.Methods P、F1、F2 rats were fed with dendrobium officinale leaves at the dose of 0,2.0,4.0,6.4g/kg·bw for two generation reproduction,and the testicular and epididymal viscera coefficients,the quantity and quality of sperm were examined and the histopathological assessment was carried out. Results There were no statistical differences in the testicular and epididymal viscera coefficients,sperm quantity,sperm motility rate and sperm malformation rate compared with the control group in P,F1,F2 rats(P>0.05). There were no differences between 0 and 6.4 g/kg·bw groups on the testicular and epididymal tissue morphology in P,F1,F2 rats. Conclusion Dendrobium officinale leaves didn't show obvious adverse effects on sperm quality and testicular tissue morphology in P,F1,F2 rats.
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Objective To study maternal toxicity, embryotoxicity and teratogenecity of Chimonanthus salicifolius S. Y. Hu in SD rats.Methods A total of 64 successfully mated female SD rats were randomly divided in to 4 groups (16 per group), in which 3 experimental groups were daily treated with 3.75, 7.5 and 15.0 g/kg. bw test substance by lavage from 7th to 16th day during gestation respectively. Body weight and general conditions of the pregnant rats were recorded during the study. On the 20th day in pregnancy, the rats were anatomized and examined grossly, the fetuses were removed and counted, weight, length, visceral and skeletal changes were then examined. Results There was no significant difference in the conception rate, total weight gain during the pregnancy and the number of living, dead and resorbed fetuses between each dosage groups and the control group (P>0.05) . The number of the rib, sternum, the fifth sternum punctated and the parietal bone which were ossified defectively all showed no difference among the four groups (P>0.05) . Conclusion Chimonanthus salicifolius S. Y. Hu extract had no obvious maternal toxicity, embryotoxicity and teratogenecity in SD rats under this experiment condition.
ABSTRACT
In recent years, iron has been regarded as a common pathological feature of many neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD) and Friedreich's ataxia (FRDA). A number of genes involved in iron transport, storage and regulation have been found associated with initiation and progression of neurodegeneration. However, whether iron abnormalities represent a primary or secondary event still remains unknown. Due to the limitation in transgenic rodent model construction and transfection systems, the progress in unraveling the pathogenic role of different iron-related proteins in neurodegenerative diseases has been slow. Drosophila melanogaster, a simple organism which has a shorter lifespan and smaller genome with many conserved genes, and captures many features of human nervous system and neurodegeneration, may help speed up the progress. The characteristics that spatial- and temporal-specific transgenic Drosophila can be easily constructed and raised in large quantity with phenotype easily determined turn Drosophila into an excellent in vivo genetic system for screening iron-related modifiers in different neurodegenerative conditions and hence provide a better picture about the pathogenic contribution of different iron-related protein abnormalities. It is believed that identification of important iron-related genes that can largely stop or even reverse degenerative process in Drosophila models may lead to development of novel therapeutic strategies against neurodegenerative diseases.