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Phytochemical research on an extract of Notopterygium incisum yielded twenty-four compounds (1 – 24), including four new compounds 7 , 10 , 13 and 17. The structures of new compounds were elucidated by spectroscopic analysis, and the absolute configuration of 5 were assigned via Mosher's method. In addition, compounds 2 , 9 , 19 and 24 were analyzed by single crystal X-ray analysis for the first time. The new compound 7 exhibited remarkable cytotoxic activity against the human pancreatic cancer cell lines PANC-1, CAPAN-2, CFPAC-1, and SW1990 with IC 50 values of 6.25 ± 0.54, 7.74 ± 1.12, 6.68 ± 1.11, and 5.35 ± 0.33 μM, respectively. The primary mechanistic study indicated that 7 caused cell death probably due to induced defects in the mitotic process. Moreover, compounds 2 and 7 - 9 effectively protected against H 2 O 2 -induced neurotoxicity in the SH-SY5Y cells, and 1 , 3 , 6 , 10 , 11 , 16 and 19 exhibited strong DPPH scavenging ability. [Display omitted] • Four undescribed and twenty known compounds were reported. • Compound 7 displayed cytotoxicity against four pancreatic cancer cell lines. • Coumarins protected against H 2 O 2 -induced neurotoxicity in the SH-SY5Y cells. [ABSTRACT FROM AUTHOR]

[Display omitted] • Three undescribed triterpenoids with rare skeletons (1 - 3) were reported. • One unreported gypenoside (4) was isolated. • The absolute configurations were determined by ECD analysis. • Their antiproliferative effects were evaluated in a variety of cell lines. Three undescribed dammarane-type triterpenoids with rare carbon skeletons (1 - 3), together with one unreported gypenoside (4), were isolated from a acid hydrolysis product of Gynostemma pentaphyllum (Thunb.) Makino. Their molecular structures were elucidated via a combination of spectroscopic and spectrometric data, while the absolute configurations of compounds 1 , 2 and 4 were determined by electronic circular dichroism (ECD) analyse. Notably, compounds 1 - 3 possess a 19(10→1)abeo structural moiety in the A ring. Saponin 4 possesses an unusual cyclopentenone side chain. Compounds 1 , 2 and 4 were screened for their antiproliferative effects against HepG2, MCF-7 and DU145 cell lines. [ABSTRACT FROM AUTHOR]

Many studies have so far confirmed the efficiency of phytochemicals in the treatment of prostate cancer. Eupatorin, a flavonoid with a wide range of phytomedical activities, suppresses proliferation of and induces apoptosis of multiple cancer cell lines. However, low solubility, poor bioavailability, and rapid degradation limit its efficacy. The aim of our study was to evaluate whether the use of mPEG-b-poly (lactic-co-glycolic) acid (PLGA) coated iron oxide nanoparticles as a carrier could enhance the therapeutic efficacy of eupatorin in DU-145 and LNcaP human prostate cancer cell lines. Nanoparticles were prepared by the co-precipitation method and were fully characterized for morphology, surface charge, particle size, drug loading, encapsulation efficiency and in vitro drug-release profile. The inhibitory effect of nanoparticles on cell viability was evaluated by MTT test. Apoptosis was then determined by Hoechest staining, cell cycle analysis, NO production, annexin/propidium iodide (PI) assay, and Western blotting. The results indicated that eupatorin was successfully entrapped in Fe 3 O 4 @mPEG-b-PLGA nanoparticles with an efficacy of (90.99 ± 2.1)%. The nanoparticle's size was around (58.5 ± 4) nm with a negative surface charge [(−34.16 ± 1.3) mV]. In vitro release investigation showed a 30% initial burst release of eupatorin in 24 h, followed by sustained release over 200 h. The MTT assay indicated that eupatorin-loaded Fe 3 O 4 @mPEG-b-PLGA nanoparticles exhibited a significant decrease in the growth rate of DU-145 and LNcaP cells and their IC50 concentrations were 100 μM and 75 μM, respectively. Next, apoptosis was confirmed by nuclear condensation, enhancement of cell population in the sub-G1 phase and increased NO level. Annexin/PI analysis demonstrated that eupatorin-loaded Fe 3 O 4 @mPEG-b-PLGA nanoparticles could increase apoptosis and decrease necrosis frequency. Finally, Western blotting analysis confirmed these results and showed that Bax/Bcl-2 ratio and the cleaved caspase-3 level were up-regulated by the designing nanoparticles. Encapsulation of eupatorin in Fe 3 O 4 @mPEG-b-PLGA nanoparticles increased its anticancer effects in prostate cancer cell lines as compared to free eupatorin. Based on these results, this formulation can provide a sustained eupatorin-delivery system for cancer treatment with the drug remaining active at a significantly lower dose, making it a suitable candidate for pharmacological uses. Schematic representation of eupatorin loaded Fe 3 O 4 @mPEG-b-PLGA nanoparticles synthesis, characterization and in vitro apoptosis detection test. Image 1 • In the current study, Eupatorin was efficiently encapsulated in mPEG-b-PLGA coated iron oxide nanoparticles. • The nanoparticles bypass the limitations and provide a sustained release of Eupatorin into the human prostate cancer cell. • The designed nanoparticles can be more effective in inhibiting cancer cell growth as compared to free form. [ABSTRACT FROM AUTHOR]

Two undescribed dammarane-type saponins were isolated from Gynostemma pentaphyllum. Their anti-Alzheimer's Disease (AD) activity was evaluated on a transgenic fly AD model. This study provided two potential candidates for anti-AD agents. • Gynostemma pentaphyllum is a traditional medicinal and edible plant in China. • Two undescribed dammarane-type saponins were isolated. • The relative configurations were determined. • Anti-AD activity was evaluated on a transgenic fly AD model. • This study provided two potential candidates for anti-AD agents. To search for potential candidate anti-AD agents, the gypenosideson the aerial parts of Gynostemma pentaphyllum were phytochemically investigated, yielding two undescribed (1 - 2) and five known (3 - 7) dammarane saponins. Their molecular structures were unambiguously elucidated via spectroscopic analyses (1D and 2D NMR, HR-ESI-MS, IR, and optical rotation) chemical transformations. All of the compounds possessed a 21- O - n -butyl-20,21-dihydroxy-21,23-epoxydammar-24-ene moiety in their structures. The short-term memory assay on a transgenic fly Alzheimer's disease (AD) model revealed that all of the compounds displayed potential anti-AD activity. Of the compounds, 1 and 6 at 10 μM showed comparable short-term memory rescue ability to memantine, the positive control, at 100 μM. This study revealed the potent antagonistic effect of dammarane-type saponins 1 and 6 against Alzheimer's disease. [ABSTRACT FROM AUTHOR]

Abstract: Purpose: There is an increasing amount of experimental evidence that oxidative stress has a central role in the neuropathology of neurodegenerative diseases. It has been suggested that the loss of cell function results from the increased oxidative damage to proteins and DNA. Herein, we investigated the effect of a natural neuroprotective flavonoid, calycopterin, on H2O2-induced disruption of phase II detoxifying enzyme system and cAMP response element binding protein (CREB) phosphorylation. Methods: PC12 cells were treated with 25, 50 and 100μM of calycopterin for 3h, followed by adding H2O2 (150μM) for 24h. The extent of apoptosis was assessed by comet assay. The level of phosphorylated CREB, nuclear factor erythroid 2-related factor 2 (Nrf2), glutamylcysteine synthetase (γ-GCS) and heme oxygenase 1 (HO-1) were measured by western blot method. The concentration of glutathione (GSH) was determined in whole cell lysate using dithionitrobenzoic acid method. Superoxide dismutase (SOD) activity was measured by colorimetric assay. Result: Morphological analysis of protection induced by calycopterin, determined by comet assay, showed that calycopterin reduced DNA in tail. We found that H2O2 decreased mitochondrial membrane potential (MMP), while, calycopterin prevented this decrease in MMP in presence of H2O2. In H2O2-treated cells, calycopterin also suppressed cytochrome C release to cytosol that is necessary for maintaining mitochondrial homeostasis in survived cells. Moreover, calycopterin, in presence of H2O2 inhibited the decrease caused by oxidative stress in stress-sensing transcription factors, CREB and Nrf2, which play an important role in antioxidant capacity of the cell. There was also an increase in γ-GCS and HO-1 levels in calycopterin pretreated cells. In the presence of H2O2, calycopterin inhibited decrease in GSH level and SOD activity. Conclusion: We provided documentation of neuroprotective effect of a natural flavone, calycopterin, against H2O2-induced oxidative stress in differentiated PC12 cells by modulating the level of CREB phosphorylation and Nrf2 pathway. [Copyright &y& Elsevier]

In this paper, graphene-based nanoadsorbent is designed and synthesized through the functionalization of magnetic graphene oxide by aminoguanidine (denoted AGu@mGO(R)). The graphene oxide (GO) was first fabricated from rice husk biomasses and modified Hammer's method. Then, co-precipitation of Fe2+ and Fe3+ onto GO in primary media resulted in magnetic graphene oxide (mGO), which was subsequently functionalized by aminoguanidine to form AGu@mGO(R) nanoparticles. The fabricated graphene-based nanoadsorbent was characterized by several techniques, including scanning electron microscopy (SEM), transmission electron microscopy (TEM), atomic force microscopy (AFM), dynamic light scattering (DLS), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), and vibrating sample magnetometer (VSM) analysis. AGu@mGO(R) efficiency was evaluated in removing chlorpyrifos, one of the most widely used pesticides from water and cucumber juice, as an actual sample. Different variables, including pH, concentration, temperature, exposure time, and amount of the adsorbent, were optimized on the efficiency of the adsorption activity of AGu@mGO(R) to obtain the most efficient pesticide removal. Isotherm, kinetic and thermodynamic of the adsorption processes were also evaluated. The chlorpyrifos desorption efficiency from AGu@mGO(R) was quantified by the HPLC-MS/MS method. The results showed the effective absorbent activity of AGu@mGO(R) on the removal of chlorpyrifos. Hence, this nonabsorbent would be used for the removal of the remained pesticide in agricultural wastewater. Additionally, the AGu@mGO(R) might be used for the quantification of pesticide residues in samples. [Display omitted] • Magnetic graphene-based nanoadsorbent was designed, synthesized, and characterized. • The nanoadsorbent was evaluated for removal and extraction of chlorpyrifos residues from water. • The cucumber was used as real sample for validation of the efficiency of nanoadsorbent in extraction of chlorpyrifos. • The chlorpyrifos removal was quantified by the HPLC-MS/MS method. [ABSTRACT FROM AUTHOR]