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Abstract The extract of Belamcanda chinensis (L.) leaves (BCLE) is a traditional Chinese herbal medicine for the treatment of hyperglycemia in Hainan province, South China. In this study, the effects of BCLE on obese diabetes were investigated using the KK-Ay mice. The component F2 of BCLE alleviate hyperglycemia and insulin resistance, as indicated by decreased levels of FBG, AUC, GSP, LDH and insulin. High levels of hepatic G6Pase and PEPCK in KK-Ay mice were markedly attenuated by F2. The inhibitory effect of F2 on GSK-3β and the enhancement effect on liver glycogen demonstrated that F2 could significantly inhibit hepatic gluconeogenesis and glycogen accumulation. The higher PPAR γ showed F2 may prevent insulin resistance by PI3K signal transduction pathway. In addition, the component F1 of BCLE prevented cell degeneration and reduced pathological tissue injury in pancreas tissue. These findings suggest that F2 exhibited high hypoglycemic activities and could be explored as possible therapeutic agents for type 2 diabetes mellitus. [ABSTRACT FROM AUTHOR]

Dregea sinensis Hemsl is an important herbal medicine in the Dai nationality of China. Its prominent clinical application has generated interest in the polyoxypregnane glycosides of the plant. This paper describes an extension of previous research on the polyoxypregnane di- and triglycosides of D. sinensis , aiming at identifying related tetraglycosides. On the basis of HPLC-ESI-MS n analysis in positive mode, twenty-five previously undescribed polyoxypregnane tetraglycosides were characterized (regarding molecular masses and fragmentation in MS n ) from an ethyl acetate fraction that was not previously investigated. Guided by MS n fragmentation and known structures of related di- and triglycosides from D. sinensis , tentative structures were predicted from the MS data. In order to test the predictions, eight of the glycosides were isolated and their structures were elucidated by 1D and 2D NMR methods, confirming the tentative predictions. Finally, the cytotoxicity of the isolates was evaluated on several human cell lines with little effect in general, even though slight inhibitory effects of four polyoxypregnane glycosides were detected at 10 μM against the human leukemia cell line HL-60. [ABSTRACT FROM AUTHOR]

Purpose Dragon's blood (DB), a Chinese traditional herb, was shown to have certain protective effects on radiation-induced bone marrow injury due to the presence of several phenolic compounds. The 50% ethanol extracts (DBE) were separated from DB by the methods of alcohol extracting-water precipitating. The protective effects of DBE on hematopoiesis were studied, particularly on megakaryocytes. Materials and methods In this study, we investigated the in vivo radioprotective effects of DBE on hematopoiesis and pathological changes using an irradiated-mouse model. Moreover, the protective effects and potential molecular mechanisms of DBE on megakaryocytopoiesis in vitro were explored in GM-CSF depletion-induced Mo7e cell model. Results DBE significantly promoted the recovery of peripheral blood cells in irradiated mice. Histology bone marrow confirmed the protective effect of DBE, as shown by an increased number of hematopoietic cells and a reduction of apoptosis. In a megakaryocytic apoptotic model, DBE (50 µg/mL) markedly alleviated GM-CSF withdrawal-induced apoptosis and cell-cycle arrest of Mo7e cells. DBE (50 µg/mL) also significantly decreased the ratio of Bax to Bcl-2 expression, inhibited the active caspase-3 expression. In addition, DBE could induce ERK1/2 phosphorylation in GM-CSF-depleted Mo7e cell, but not Akt. Conclusions Our data demonstrated that DBE could effectively accelerate the recovery of peripheral blood cells, especially platelet. DBE attenuated cell apoptosis and cell cycle arrest through the decrease of Bax/Bcl-2 ratio and the reduction of active caspase-3 expression. The effect of DBE on Mo7e cells survival and proliferation is likely associated with the activation of ERK, but not Akt. [ABSTRACT FROM AUTHOR]

Absract The phytochemical investigation of the roots of Dregea sinensis Hemsl yielded six new polyhydroxy steroidal glycosides (1–6). The chemical structures have been elucidated on the basis of extensive one- and two-dimensional NMR spectroscopy, as well as by mass spectrometry. The cytotoxic activity of these compounds were evaluated in vitro while compounds 3 and 4 showed weak activity against human leukemia cells (HL-60) with IC 50 values of 14.10 μM and 19.16 μM, respectively. [ABSTRACT FROM AUTHOR]

Abstract: Belamcanda chinensis (Iridaceae) belongs to the family of iridaceae and its rhizoma has been widely used for the treatment of throat ailment. Here we report a new pharmacological activity of B. chinensis leaf extract (BCL), that is, the hypoglycemic effect in normal and STZ-induced diabetic rats. Animals either healthy or STZ-induced diabetic show significantly lowered fasting blood glucose levels after treatment with BCL. The serum insulin concentration in normal rats is also enhanced. Additionally, the increase in blood glucose levels after administration of various carbohydrates in normal rats is significantly decreased and the oral glucose tolerance (OGTT) of STZ-induced diabetic rats is largely improved by BCL treatment. However, co-administration of BCL with Nifedipine, a Ca2+ ion channel blocker, or Nicorandil, an ATP-sensitive K+ ion channel opener thoroughly abolishes the hypoglycemic effect of BCL. HPLC analysis and compound identification showed that several isoflavone glycosides with antidiabetic activities were contained in BCL while pharmacological experiment showed that the polysaccharide fraction of BCL had no significant hypoglycemic effect on normal rats. Therefore, the isoflavone glycosides but not polysaccharides might be the active fraction of BCL in diabetes treatment. [Copyright &y& Elsevier]

Liver fibrosis is a dynamic and highly integrated pathological process resulting from repeated liver injury healing accompanied by inflammation and extracellular matrix deposition. Treatment is necessary at the early stage of reversible liver fibrosis to prevent further deterioration to liver cirrhosis and liver cancer. Currently, the inhibition of liver fibrosis are mainly focused on prevention the activation of hepatic stellate cells and inhibition of inflammatory pathways involved in liver fibrosis. Previous research in our lab found that natural phenanthrenes derived from Traditional Chinese Medicine Baiyangjie could inhibit liver fibrosis through inhibiting TGF-β1, TNF-α and promoting the secretion of MMP-9. Herein, in order to optimize the structure of phenanthrenes to maximize their anti-fibrosis activities, a series of phenanthrene derivatives were designed and synthesized in an expeditious manner. Their ability to inhibit LPS-initiated cellular liver fibrosis in HSC-T6 cells were examined and the results indicated that compounds A-1 and B-1 provided the best cellular anti-fibrosis activities. Further studies implied that they inhibited the LPS-initiated cellular liver fibrosis through inhibition the secretion of TNF-α, IL-1β, TGF-β1 and α-SMA. From these data, a picture emerges wherein a novel idea using phenanthrenes A-1 and B-1 as potential candidates to treat liver fibrosis for further animal studies. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: An efficient chemoenzymatic route for the synthesis of enantiopure (R)-salsolinol through the use of Candida antarctica lipase A (CALA) was developed. Different parameters, including the acyl agent, the solvent, the temperature, and the amount of enzyme and substrates used, were investigated in order to establish the optimal reaction conditions for the enzymatic kinetic resolution of secondary amines. The combination of CALA with phenyl allyl carbonates in toluene allowed the isolation of amines with high conversion (50%) and ee (98%) values. [Copyright &y& Elsevier]

Torreya grandis (Taxaceae) was studied for antinociceptive and anti-inflammatory effects. Leaves were extracted with 80% ethanol at 80°C for 3h and fractionated with petroleum ether, chloroform, ethylacetate and n-butanol. The aqueous ethanolic extract (aq.EE), ethylacetate fraction (EaF) and butanol fraction (BtF) at the doses of (100 and 200mg/kg, i.g.) body weight were used for study. Evaluation of antinociceptive activity was carried out by acetic acid-induced writhing response and formalin-induced paw licking time in the first and second phases of mice. The paw edema induced by formalin- and xylene-induced ear edema were used to assess anti-inflammatory activity. It was found that Torreya grandis extract and fractions at the doses of (100 and 200mg/kg, i.g.) were significantly attenuated the writhing responses induced by acetic acid and second phase of pain response induced by subplantar injection of formalin in mice. In addition, these extract and fractions inhibiting the formaldehyde-induced arthritis as well as xylene-induces edema prolifically. From acute oral toxicity studies no mortality was pragmatic even at highest dose (2500mg/kg, i.g.). Furthermore, our phytochemical studies indicated that the aq. ethanolic extract of leaves contains alkaloids, flavonoids, tannins, terpenoids and saponins. The results provide justification for the folkloric uses of Torreya grandis in the treatment of analgesic and inflammatory-based diseases across the China. [Copyright &y& Elsevier]

The biological damage caused by the environmental factors such as radiation and its control methods are one of the frontiers of life science research that has received widespread attention. Ionizing radiation can directly interact with target molecules (such as DNA, proteins and lipids) or decomposed by radiation from water, leading to changes in oxidative events and biological activities in cells. Liver is a radiation-sensitive organ, and its radiosensitivity is second only to bone marrow, lymph, gastrointestinal tissue, gonads, embryos and kidneys. In addition, as a key organ of mammals, liver performs a series of functions, including the production of bile, the metabolism of nutrients, the elimination of waste, the storage of glycogen, and the synthesis of proteins. Therefore, liver is prone to various pathophysiological changes. In this review, the effects of radiation on liver injury, its pathogenesis, bystander effect and the natural traditional Chinese medicine to protect the radiation induced liver damage are discussed. [ABSTRACT FROM AUTHOR]

Radiation and microgravity exert different biological effects on the human brain during space flight. Studies rarely focus on the two combined. The central nervous system (CNS) is among the most crucial systems in the human brain. Inflammatory activation of glial cells is the principal sign of damage to nerve function. Therefore, the present study established in vitro models of radiation, simulated microgravity, and a combination of the two, in order to explore the resultant biological changes occurring in human glial cells. Experiments were performed on U-87 MG cells to study the release of inflammatory factors, changes in autophagy, and the transcription level of a key regulatory factor of histone methyltransferase enhancer of zeste 2 (EZH2). The results demonstrated that a simulated space environment significantly impacted cell growth and morphology. Neurons released cytokines that recruited monocytes, invoking an inflammatory response. Both radiation and microgravity activated cell autophagy. Finally, the meta-transcriptomics of glial cells were comprehensively analyzed, focusing on changes in the transcription of genes regulating autophagy. The results indicated that transcription levels of EZH2, the critical dual regulator of inflammation and autophagy, decreased in a simulated space environment, suggesting that U-87 MG cells inhibit EZH2 expression in such conditions. The down-regulation of EZH2 induced autophagy through activation of the mTOR pathway. Changes in levels of autophagy activated NF-κB and induced the release of the inflammatory factor IL-6. The interaction between NF-κB and EZH2 may also, in turn, affect the expression of EZH2, creating a U-87 MG cell inflammatory activation cycle. In summary, the results indicate that EZH2 may be a dual-regulator of inflammatory activation and autophagy in a simulated space environment, helping to explain the biological damage observed in the CNS in a space environment due to neuroinflammation, providing molecular targets for the health protection of astronauts during long-term space flight. • Glial cells occur inflammatory activation under simulated space environment. • Autophagy was activated in glial cells under simulated space environment. • EZH2 related signaling pathway may be critical regulatory factors of autophagy related inflammation. [ABSTRACT FROM AUTHOR]

Cyclocarya paliurus is essential and only living specie of the genus Cyclocarya Iljinskaja. The leaves of this plant have been extensively used as food in the form of tea and green vegetable. Many compounds have been isolated from this plant, and their useful aspects explored, including the polysaccharides. Studies conducted on leaves show that different methods of extraction have been used, as well as a combination of different techniques that have been applied to isolate polysaccharides from the leaves. Their structure has been elucidated because the activity of polysaccharides mainly depends upon their composition. It has been reported that different activities exhibited by the isolated crude, purified as well as modified polysaccharides include, anticancer, anti-inflammatory, antioxidant, antimicrobial, anti-hyperlipidemic and anti-diabetic activities. In some studies, a comparison of crude extract, as well as purified polysaccharide, has been performed. In this review, we have summarized all the available literature available on the methods of extraction, structure, and biological activities of polysaccharides from the leaves of C. paliurus and indicated the potential research areas that should be focused on future studies. We believe that this review will provide an up to date knowledge regarding polysaccharides of C. paliurus for the researchers. [ABSTRACT FROM AUTHOR]

Abstract In addition to amyloid cascade hypothesis, ferroptosis – a recently identified cell death pathway associated with the accumulation of lipid hydroperoxides – was hypothesized as one of the main forms of cell death in Alzheimer's disease. Herein, a series of hydroxylated chalcones were designed and synthesized as dual-functional inhibitors to inhibit amyloid-β peptide (Aβ) aggregation as well as ferroptosis simultaneously. Thioflavin-T assay indicated trihydroxy chalcones inhibited Aβ aggregation better. In human neuroblastoma SH-SY5Y cells, cytoprotective chalcones 14a-c with three hydroxyl substituents exhibited a significant neuroprotection against Aβ 1-42 aggregation induced toxicity. In addition, chalcones 14a-c were found to be good inhibitors of ferroptosis induced by either pharmacological inhibition of the hydroperoxide-detoxifying enzyme Gpx4 using (1S, 3R)-RSL4 or cystine/glutamate antiporter system X c − inhibition by erastin through lipid peroxidation inhibition mechanism. Trihydroxy chalcone 14a was also able to completely subvert lipid peroxidation induced by Aβ 1-42 aggregation in SH-SY5Y cells indicating that they can reduce the neurotoxicity involved with oxidative stress. Compound 14a-c showed good ADMET properties and blood-brain barrier penetration in silico simulation software. From these data, a picture emerges wherein trihydroxy chalcones are potential candidates for the treatment of Alzheimer's disease by simultaneously inhibition of Aβ 1-42 aggregation and ferroptosis. Graphical abstract Image 1 Highlights • Hydroxylated chalcones were synthesized as dual-functional inhibitors. • Chalcones 14a-c inhibited amyloid-β aggregation at micromolar concentrations. • Chalcones 14a-c protected neural cells against Aβ aggregation induced toxicity. • Chalcones 14a-c protected cells from ferroptosis at micromolar concentrations. [ABSTRACT FROM AUTHOR]

During spaceflight, the negative effects of space microgravity on astronauts are becoming more and more prominent, and especially, of which on the nervous system is urgently to be solved. For this purpose tissue blocks and primary cells of nervous tissues obtained from glioma of patients were cultivated after culturing for about 7 days, explanted tissues and cells were then randomly divided into two groups, one for static culture (control group, C), and the other for rotary processing for 1 day, 3 days, 5 days, 7 days and 14 days (experiment group, E). Figures captured by inverted microscope revealed that, with short time rotating for 1 day or 3 days, morphology changes of tissue blocks were not obvious. When the rotary time was extended to 7 days or 14 days, it was found that cell somas is significantly larger and the ability of adhesion is declined in comparison with that in control group. Additionally, the arrangement of cells migrated from explanted tissues was disorganized, and the migration distance became shorter. In immunofluorescence analysis, β-tubulin filaments in control group appeared to organize into bundles. While in experiment group, β-tubulin was highly disorganized. In conclusion, simulated microgravity treatment for a week affected the morphology of nervous tissue, and caused highly disorganized distribution of cytoskeleton and the increase of cell apoptosis. These morphological changes might be one of the causes of apoptosis induced by simulated microgravity. [ABSTRACT FROM AUTHOR]

Artemisia sphaerocephala Krasch (ASK) is an important member of Compositae (Asteraceae) family. Its seeds have been widely used as traditional medicine and to improve the quality of food. Water soluble and water insoluble polysaccharides are found in the seeds of this plant. Research has been conducted on the extraction of polysaccharides, their modification and determination of their structure. To date different techniques for extraction purposes have been applied which are reviewed here. Antioxidant, antidiabetic, anti-obesogenic, antitumor, and immunomodulatory activities have been explored using in vivo and in vitro methods. Moreover, these polysaccharides have been used as packaging material and as a sensing component for monitoring the freshness of packaged food. Some experimental results have shown that the quality of foods is also improved by using them as a food additive. We have also indicated some of the potential areas that are needed to be explored. [ABSTRACT FROM AUTHOR]