Isoprenoid flavonoids isolated from Sophora davidii and their activities induces apoptosis and autophagy in HT29 cells.

Four previously undescribed isoprenoid flavonoids (2-5) were isolated from Sophora davidii, along with five known analogues. The structures of the compounds were established through comprehensive analysis of spectroscopic data, including HRESIMS, 1D and 2D NMR, and absolute configurations determined by theoretical calculations, including ECD and NMR calculation. The cytotoxic effects of the isolated compounds on human HT29 colon cancer cells were evaluated using the MTT assay, compound 1 exhibited cytotoxicity against human HT29 colon cancer cells with an IC50 value of 8.39 ± 0.09 µM. Studies conducted with compound 1 in HT29 cells demonstrated that it may induce apoptosis and autophagy in HT29 by promoting the phosphorylation of P38 MAPK and inhibiting the phosphorylation of Erk MAPK.

Dihydrophenanthrenes and phenanthrenes from Dendrobium terminale.

Two previously undescribed dihydrophenanthrene derivatives (1 and 2) were isolated along with twelve known analogues from the whole plant of Dendrobium terminale. The structures of the new compounds were elucidated on the basis of detailed spectroscopic analysis. The NMR data of known phenanthrene derivatives (7 and 9) were revised by 2D NMR. The isolated compounds were evaluated for cytotoxicity against three kinds of tumor cell lines (sw1990, HCT-116, and HepG2). Especially compounds 11 and 14 showed stronger antitumor effects, and the structure-activity relationship of these compounds was discussed.

Glucosyloxybenzyl 2-isobutylmalates and phenolic glycosides from the flowers of Bletilla striata.

Four previously undescribed compounds, including three glucosyloxybenzyl 2-isobutylmalates (1-3), one phenolic glycoside (4), along with ten known compounds were isolated from the flowers of Bletilla striata. The structures and absolute configurations of the undescribed compounds were elucidated on the basis of HR-ESIMS, NMR spectroscopy, optical rotation value, and acid hydrolysis experiment. Cytotoxicity of the isolated compounds against A549, HCT-116, and SW1990 cells and protective effects of t-BHP-induced L02 cytotoxic were assayed. The antioxidant activities of the isolated compounds were also evaluated.

Analysis of the water-soluble polysaccharides from Camellia japonica pollen and their inhibitory effects on galectin-3 function.

Pollen has been defined as dietary supplement used to supplement the diet in many countries, but the primary structure and activity of Camellia japonica pollen polysaccharide remain unclear. In this study, the water-soluble polysaccharide extracted from Camellia japonica pollen (WCPP) was fractionated into one neutral fraction (WCPP-N) and two acidic fractions (WCPP-A1 and WCPP-A2) by DEAE-cellulose column, and WCPP-A2 was further fractionated into two homogeneous sub-fractions (WCPP-A2a and WCPP-A2b) by Sepharose CL-6B column. Monosaccharide composition results showed that WCPP-N might mainly contain starch-like glucan as well as some arabinogalactan, while WCPP-A1, WCPP-A2 and its sub-fractions might mainly composed of rhamnogalacturonan I (RG-I) pectic polysaccharide domain backbone with some different types of side chains, including arabinan, galactan, and/or arabinogalactan. The primary structure analysis of WCPP-A2a by NMR spectra analysis suggested that WCPP-A2a was an RG-I-like pectic polysaccharide, branched at the O-4 of Rha residues in the backbone, with α-(1 â†’ 3,5)-L-arabinan as well as type-II arabinogalactan side chain to which were attached. The results of galectin-3-mediated hemagglutination assay indicated that WCPP-A2a exhibited the strongest inhibitory effect on galectin-3 with MIC value around 0.27 µg/mL. These results suggested the potential use of Camellia japonica pollen polysaccharide as a galectin3 inhibitor in functional foods.

Ionic Liquid-Microwave-Based Extraction of Biflavonoids from Selaginella sinensis.

Selaginella sinensis (Desv.) Spring has been used for many years as traditional Chinese medicine (TCM) for many years. Recently, ionic liquids (ILs) have attracted great attentions in extraction and separation technology of TCM as a new green solvent. In this paper, microwave assisted extraction-IL (MAE-IL) that extracted amentoflavone (AME) and hinokiflavone (HIN) from Selaginella sinensis was reported for the first time. The contents of two biflavonoids were simultaneously determined by a high performance liquid chromatography (HPLC) method. After different ionic liquids were compared, it was found [C6mim]BF4 had a high selectivity and efficiency. Moreover, the important extraction conditions, including solid-liquid ratio, IL concentration, extraction time, microwave power and radiation temperature, were also investigated and optimized by response surface methodology (RSM) using AME and HIN yields as index. The results showed that the extraction yields of AME and HIN from S. sinensis were 1.96 mg/g and 0.79 mg/g, respectively, under the optimal process parameters (0.55 mmol/L, 300 W, 40 min, 1:11 g/mL and 48 °C). Compared with the conventional extraction methods, MAE-IL could not only achieve higher yield in shorter time, but also could reduce the consumption of solvent. This effective, rapid and green MAE-IL method was suitable for the extraction of AME and HIN.

A Cascade-Targeting Nanocapsule for Enhanced Photothermal Tumor Therapy with Aid of Autophagy Inhibition.

Autophagy is a homeostatic lysosome-dependent metabolic process to eliminate damaged or dysfunctional cellular organelles, which is closely associated with tumor progression. Indocyanine green (ICG) can convert NIR light energy to localized heat for cancer cell and tissue ablation. However, the effect of autophagy modulation on ICG-mediated photothermal therapy remains unknown. In this study, it is found that primaquine (PQ) suppresses autophagy flux at a late stage through the impeding fusion of the autophagosome with the lysosome to form an autophagolysosome, leading to cell apoptosis or necrosis. This autophagosome-lysosome fusion inhibitory effect and the autophagosome accumulation are more evident in the photothermal therapy combined with autophagy inhibition. Motivated by this notable effect, a cascade-targeting nanocapsule (HCP) is constructed using an organic solvent-free strategy to coencapsulate PQ and ICG. By targeting the cluster designation 44 molecule and sequentially enhancing the cell-penetrating peptide-mediated endocytosis, the codelivery of PQ/ICG by HCP achieves selective recognition and reinforces the internalization by MCF-7 cells to exert a synergistic therapeutic effect on MCF-7 cells both in vitro and in vivo. The HCP system for the photothermal and autophagy inhibition combination therapy represents a novel strategy for the treatment of breast cancer.

New Triterpenoid Saponins from the Herb Hylomecon japonica.

Background: Hylomecon japonica, a plant of the Papaveraceae family which is well-known for the alkaloids they produce, is a perennial plant widely distributed in the northeast, central and east regions of China. Although a variety of chemical constituents, including alkaloids, flavonoids, and megastigmoids, have been isolated from H. japonica, the investigation of saponins in H. japonica has not been reported until now. Methods: Various separation techniques, including polyporous resin column chromatography, silica gel column chromatography and hemi-preparative HPLC were applied to the isolation of triterpenoid saponins, and chemical methods such as acid hydrolysis and spectroscopic methods including HRESIMS and NMR were applied to their structure elucidation, and the XTT reduction method was used to assay cytotoxicity. Results: Two new triterpenoid saponins, named hylomeconoside A (1) and B (2) which were identified as 3-O-ß-d-galactopyranosyl-(1→2)-ß-d-glucuronopyranosyl-gypsogenin-28-O-ß-d-xylopyranosyl-(1→3)-ß-d-xylopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→2)-ß-d-quinovopyranoside (1) and 3-O-ß-d-galactopyranosyl-(1→2)-ß-d-glucuronopyranosyl-gypsogenin-28-O-ß-d-xylopyranosyl-(1→3)-ß-d-xylopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→2)-α-l-arabinopyranoside (2), and two known triterpenoid saponins identified as dubioside C (3) and lucyoside P (4) on the basis of spectroscopic and chemical evidence, were isolated from H. japonica. Compound 1 exhibited moderate cytotoxicity on MGC-803 and HL-60 cells, with IC50 values of 43.8 and 32.4 µg·mL-1, respectively. Conclusions: Compounds 1 and 2 are new saponins, and 1 is considered to be one of the antitumor principles in this plant. This is the first time that triterpenoid saponins have been isolated from plants of the Papaveraceae family.

Anti-hyperglycemic and anti-oxidative activities of ginseng polysaccharides in STZ-induced diabetic mice.

Neutral (WGPN) and acidic (WGPA) polysaccharides were fractionated from ginseng polysaccharide. WGPN and WGPA decreased fasting blood glucose by different manners of administration. Intra-gastric administration of WGPA showed a marked hypoglycemic effect, which may be related to its anti-oxidative activity. The results indicated that WGPA may have anti-diabetic potential.

The effective mechanism of the polysaccharides from Panax ginseng on chronic fatigue syndrome.

Ginseng acidic polysaccharide WGPA isolated from the root of Panax ginseng C. A. Meyer was fractionated into WGPA-A and WGPA-N by anion-exchange chromatography. The antifatigue activity of ginseng acidic polysaccharide WGPA has been reported in our previous research. This present study was designed to identify its active component and elucidate the mechanism for preventing chronic fatigue syndrome (CFS). WGPA, WGPA-A and WGPA-N were orally administered to mice once daily for 15 days. The effects of these compounds on physiological biomarkers of oxidative stress and on the morphology of the mitochondria in striated skeletal muscle were assessed. The results of forced swimming test-induced indicated that WGPA and WGPA-A could lengthen the swimming time, while WGPA-N could not. In addition, malondialdehyde and lactate dehydrogenase levels in serum were enhanced; while those of superoxide dismutase and glutathione peroxidase were lowered. Interestingly, the structural degeneration of mitochondria were all ameliorated. These findings suggested that WGPA-A is the active component of WGPA, it might have potential therapeutic effects for CFS and the oxidative stress might be involved in the pathogenesis. Our results also provided essential data for a better understanding of the antifatigue effects of P. ginseng extracts.

Neuroprotective effects of ginseng pectin through the activation of ERK/MAPK and Akt survival signaling pathways.

In this study, we investigated the neuroprotective activities of ginseng pectin (GP) against hydrogen peroxide (H2O2)-induced neuronal toxicity in different neuronal cells. GP selectively attenuated H2O2-induced damage up to 26% in primary cortical neuron cells and human glioblastoma U87 cells. Following H2O2 exposure, DAPI staining and neuron-specific ß-tubulin antibody probing indicated that GP maintained cell integrity and decreased nuclei condensation. Data from western blot analysis revealed that pre-treatment with GP increased the phosphorylation of both the extracellular signal-regulated kinases 1 and 2 (ERK1/2) and Akt in cortical neuron cells. However, the phosphorylation of ERK1/2 was increased, but that of Akt was decreased in U87 cells. These results suggest that the protective effects of GP against H2O2-induced apoptosis may be due to the activation of the phosphorylation of ERK1/2 and Akt; however, the mechanisms involved differ depending on the cell line. This neuroprotective property indicates that GP could serve as a potential therapeutic agent for neurodegenerative diseases.

In vivo antimalarial activity of ginseng extracts.

CONTEXT: Novel antimalarial agents are in demand due to the emergence of multidrug resistant strains. Ginseng, a medicinal plant with antiparasitic activity, contains components that can be used to treat the tropical disease malaria. OBJECTIVE: Ginsenosides and polysaccharides are active components of ginseng. This study aimed to elucidate the ability of these compounds to inhibit the replication of Plasmodium yoelii in an attempt to determine whether the medicinal uses of ginseng are supported by pharmacological effects. New antimalarial compounds may be developed from ginsenosides and water-soluble ginseng polysaccharides (WGP). MATERIALS AND METHODS: Ginsenosides and ginseng polysaccharides were prepared from ginseng. Antimalarial activities were examined by 4-day tests and repository tests. Macrophage phagocytosis was tested in normal and malaria-bearing mice. RESULTS: Ginseng polysaccharides could inhibit residual malaria infection. After a 6-day treatment, the parasitemia reductions of WGP and acidic ginseng polysaccharide (WGPA) were 55.66% and 64.73% at 200 mg/kg/day, respectively. Ginsenosides showed significant antimalarial activity on early infection. Protopanaxadiol-type ginsenosides caused 70.97% chemosuppression at 50 mg/kg/day, higher than 52.8% of total ginsenosides at the same dose. DISCUSSION AND CONCLUSION: Protopanaxadiol-type ginsenosides have remarkably suppressive activity during early infection, while acidic ginseng polysaccharides have significant prophylactic activity against malaria by stimulating the immune system. We propose that the activity of ginsenosides is dependent upon non-specific carbohydrate interactions and that the activity of ginseng polysaccharides is due to immunological modulation. Ginsenosides and ginseng polysaccharides might have a potential application in antimalarial treatments.

Preparation of a glucan from the roots of Rubus crataegifolius Bge. and its immunological activity.

A water-soluble glucan (RCP-1) was prepared from the roots of Rubus crataegifolius Bge. by extraction with hot-water, deproteination by Sevag reagent, alpha-amylase treatment and ultrafiltration. RCP-1 consisted of only glucose, and its molecular weight was determined to be approximately 7KD by high performance gel permeation chromatography (HPGPC). Fourier transform infra-red spectroscopy (FT-IR), nuclear magnetic resonance spectroscopy (NMR), methylation and periodate oxidation analyses indicated that RCP-1 was an alpha-d-glucan. Its main chains were composed of (1-->4)- and (1-->6)-linked alpha-glucopyranosyls, and side chains were single alpha-glucopyranosyl residues attached to the O-6 of glucosyls in the main chains. RCP-1 could increase both cytotoxic activity against B16 melanoma cells and the production of nitric oxide (NO) of macrophages in vitro. Furthermore, in vivo bioassay tests indicated that RCP-1 could remarkably enhance T and B lymphocyte proliferations, augment the phagocytosis of macrophages and increase the tumour necrosis factor-alpha (TNF-alpha) levels in serum.