Prospective role of lusianthridin in attenuating cadmium-induced functional and cellular damage in rat thyroid.

The thyroid represents the most prevalent form of head and neck and endocrine cancer. The present investigation demonstrates the anticancer effects of Lusianthridin against cadmium (Cd)-induced thyroid cancer in rats. Swiss Wistar rats were utilized in this experimental study. Cd was employed to induce thyroid cancer, and the rats were divided into different groups, receiving oral administration of Lusianthridin (20 mg/kg) for 14 days. Thyroid parameters, deiodinase levels, hepatic parameters, lipid parameters, and antioxidant parameters were respectively estimated. The mRNA expression was assessed using real-time reverse transcriptase polymerase chain reaction (RT-PCR). Lusianthridin significantly (P < 0.001) improved protein levels, T4, T3, free iodine in urine, and suppressed the level of TSH. Lusianthridin significantly (P < 0.001) enhanced the levels of FT3, FT4, and decreased the level of rT3. Lusianthridin significantly (P < 0.001) reduced the levels of D1, D2, D3, and enhanced the levels of hepatic parameters like AST, ALT. Lusianthridin remarkably (P < 0.001) altered the levels of lipid parameters such as LDL, total cholesterol, HDL, and triglycerides; antioxidant parameters viz., MDA, GSH, CAT, and SOD. Lusianthridin significantly altered the mRNA expression of Bcl-2, Bax, MEK1, ERK1, ERK2, p-eIf2α, GRP78, eIf2α, and GRP94. The results clearly state that Lusianthridin exhibits protective effects against thyroid cancer.

Natural compound chaetocin induced DNA damage and apoptosis through reactive oxygen species-dependent pathways in A549 lung cancer cells and in vitro evaluations.

There is an urgent need for potential pharmaceutics for lung cancer treatment due to the increased number of lung cancer deaths and the resistance of cancer cells to present therapeutics. The present work aims to discover the anticancer potential of the natural compound chaetocin as a therapeutic for lung cancer treatment. Results showed the significance of chaetocin-induced cell growth inhibition by the expression of G2 /M phase arrest and reactive oxygen species (ROS) dependent apoptosis in A549 lung cancer cells. Results concluded that chaetocin could produce ROS and nuclear damage against A549 lung cancer cells. Interestingly, chaetocin exhibits a significant level of CD47 that down-regulates the expression of CD47 at mRNA levels. PBMC biocompatibility study revealed that chaetocin is non-toxic to normal cells. Overall, experimental results suggested that chaetocin induces A549 cell apoptosis, by causing ROS and nuclear damage activation pathways. In the future, chaetocin might be an effective bio-safe anticancer agent for lung cancer treatments.

Preparation of carboxymethylcellulose / ZnO / chitosan composite hydrogel microbeads and its drug release behaviour.

In this study, a novel carboxymethylcellulose / ZnO / chitosan (CMC / ZnO / Cs) hydrogel microbeads loaded with crosslinked porous starch / curcumin (CPS / Cur) were designed and prepared to improve the encapsulation efficiency of curcumin for drug delivery to specific sites. It was found that the total pore volume of crosslinked porous starch (CPS) was increased by 1150 % when compared to the native starch (NS), and the adsorption ratio of curcumin by CPS was enhanced by 27 % when compared to NS. Secondly, the swelling ratio of composite hydrogel microbeads was within 25 % in an acidic environment at pH 1.2, and the swelling ratio of hydrogel microbeads sharply increased to 320 % ~ 370 % at pH 6.8 and 7.4. In addition, the results of in vitro simulated release experiments showed that the released amount of hydrogel microbeads loaded with NS/Cur and CPS/Cur in SGF were within 7 % in simulated gastric fluid (SGF). The highest released amount of curcumin was 65.26 % for hydrogel beads loaded with CPS/Cur, which was 26 % lower than that of hydrogel microbeads loaded with Cur in simulated intestinal fluid (SIF). In simulated colonic fluid (SCF), the released amount of hydrogel microbeads loaded with CPS/Cur and Cur were 73.96 % and 91.69 %, respectively. In conclusion, pH-sensitive drug delivery system with good drug stability and bioavailability were successfully prepared with carboxymethylcellulose / ZnO / chitosan bead, suitable targeting drug delivery to the small intestine.

Preparation and in vivo imaging of NIR-emissive carbonized polymer dots derived from biomass olive leaves with a quantum yield of 71.4.

The conversion of biomass materials into high value-added chemicals is receiving more and more attention. Herein, biomass olive leaves are converted into carbonized polymer dots (CPDs) through a simple hydrothermal reaction. The CPDs show near infrared light emission properties, and the absolute quantum yield reaches a record breaking value of 71.4% under the excitation wavelength of 413 nm. Detailed characterization determines that CPDs only contain three elements: carbon, hydrogen and oxygen, which is very different from most carbon dots which contain nitrogen atoms. Subsequently, NIR fluorescence imaging both in vitro and in vivo is performed to test their feasibility as fluorescence probes. The metabolic pathways of CPDs in the living body are inferred by studying the bio-distribution of CPDs in major organs. Their outstanding advantage is expected to further broaden the application field of this material.

Pulsed electric field-assisted esterification improves the freeze-thaw stability of corn starch gel by changing its molecular structure.

The influence of pulsed electric field (PEF) combined with octenyl succinic anhydride (OSA) on the freeze-thaw stability of corn starch gel was investigated. After five freeze-thaw cycles, the syneresis value of OSA starch treated with PEF-assisted esterification for 15 min was lower by 29.5 %, while that of OSA starch without PEF treatment was lower by 10.17 %, compared to that of native starch. Low-field nuclear magnetic resonance data showed that the introduction of OSA groups greatly increased the water-holding capacity of starch. Results from differential scanning calorimetry (DSC) and X-ray diffraction (XRD) showed that the PEF-assisted esterification markedly hindered the re-formation of the helical structure of starch during freeze-thaw cycles. Moreover, PEF-assisted esterification improved the viscoelastic properties of the starch gel. It is found that the freeze-thaw stability of the PEF-modified starch depends not only on the degree of substitution but also on the starch molecular fine structure. PEF-assisted OSA starch with a high degree of substitution, a low content of amylose, and a high content of short amylopectin chains were found to have high freeze-thaw stability. This study shows that PEF-assisted esterification is a promising technique that should be used for preserving the quality of frozen foods.

Succinylated whey protein isolate-chitosan core-shell composite particles as a novel carrier: Self-assembly mechanism and stability studies.

Single protein [whey protein isolate (WPI) or succinylated whey protein isolate (SWPI)] and composite particles of proteins with chitosan (CS) were tested for their ability to encapsulate and protect curcumin (CUR). Combining protein and CS resulted in changes in zeta-potential and surface hydrophobicity, particularly in the SWPI-H (high degree of succinylation, 90 %) and CS composite particle (H-CS). Furthermore, the secondary and tertiary structures were dramatically altered using Fourier transform infrared (FTIR), circular dichroism (CD), and X-ray diffraction (XRD). Scanning electron microscopy (SEM) and atomic force microscope (AFM) analyses revealed that H-CS exhibited a soft core-rigid shell morphology due to electrostatic interactions, hydrophobic interactions, and H-bond interactions. Fluorescence quenching results demonstrated that H-CS had a higher binding constant (K, 1.69 ×104 M-1) and encapsulation effectiveness (EE, 88.3 %) of CUR. Because of increased binding sites and steric hindrance, CUR was stabilized more effectively in H-CS in photostability and thermostability tests,. These results show that SWPI-CS composite particles can be utilized to build a protection system for water-insoluble nutritional supplements.

Sonosynthesis of nanobiotics with antimicrobial and antioxidant properties.

Transforming small-molecule antibiotics into carrier-free nanoantibiotics represents an opportunity for developing new multifunctional therapeutic agents. In this study, we demonstrate that acoustic cavitation produced by high-frequency ultrasound transforms the antibiotic doxycycline into carrier-free nanobiotics. Upon sonication for 1 h at 10-15 W cm-3, doxycycline molecules underwent hydroxylation and dimerization processes to ultimately self-assemble into nanoparticles of ∼100-200 nm in size. Micrometer sized particles can be also obtained by increasing the acoustic power to 20 W cm-3. The nanodrugs exhibited antioxidant properties, along with antimicrobial activity against both Gram-positive (S. aureus) and Gram-negative (E. coli) bacterial strains. Our results highlight the feasibility of the ultrasound-based approach for engineering drug molecules into a nanosized formulation with controlled and multiple bio-functionalities.

Quercetin attenuates the proliferation of arsenic-related lung cancer cells via a caspase-dependent DNA damage signaling.

Exposure to arsenic (As) mainly through contaminated drinking water enhances the lung tumor progression, invasion, and metastasis. The carcinogenic effect of As is due to the generation of reactive oxygen species (ROS) and DNA damage, and interference with DNA repair machinery. Herein, we investigated the potential therapeutic function of quercetin on As-treated lung cancer cells. Quercetin is a natural product with antioxidative, anti-inflammatory, and antiproliferative properties. We showed that quercetin induced cell death in the As-exposed lung cancer cells in a dose-dependent manner. Quercetin was able to significantly inhibit the proliferation of the As-treated cells over a period of 5 weeks. In addition, quercetin induced ROS-mediated DNA double-strand breaks in the As-treated lung cancer cells. We also showed that ROS generation induced by quercetin activated caspase-3 to a sufficient level to induce DNA damage but insufficient to induce death in As-treated lung cancer cells. Moreover, transient activation of caspase-2 was detected in quercetin- and As-cotreated cells. The flow cytometry-based cell cycle analysis showed that the antiproliferative function of quercetin was mediated by S-phase cell cycle arrest, which was associated with upregulation of the Ataxia Telangiectasia-mutated (ATM), but not ATM and RAD3-related. In conclusion, quercetin synergized the As-driven ROS generation and DNA damage, and induced the S-phase arrest, thus inhibiting the proliferation of As-exposed lung cancer cells. This data suggested that quercetin is an alternative reagent to chemo-drugs to prevent the growth of As-exposed lung cancer cells.

Inhibition of Biofilm Formation of Foodborne Staphylococcus aureus by the Citrus Flavonoid Naringenin.

Taking into consideration the importance of biofilms in food deterioration and the potential risks of antiseptic compounds, antimicrobial agents that naturally occurring are a more acceptable choice for preventing biofilm formation and in attempts to improve antibacterial effects and efficacy. Citrus flavonoids possess a variety of biological activities, including antimicrobial properties. Therefore, the anti-biofilm formation properties of the citrus flavonoid naringenin on the Staphylococcus aureus ATCC 6538 (S. aureus) were investigated using subminimum inhibitory concentrations (sub-MICs) of 5~60 mg/L. The results were confirmed using laser and scanning electron microscopy techniques, which revealed that the thick coating of S. aureus biofilms became thinner and finally separated into individual colonies when exposed to naringenin. The decreased biofilm formation of S. aureus cells may be due to a decrease in cell surface hydrophobicity and exopolysaccharide production, which is involved in the adherence or maturation of biofilms. Moreover, transcriptional results show that there was a downregulation in the expression of biofilm-related genes and alternative sigma factor sigB induced by naringenin. This work provides insight into the anti-biofilm mechanism of naringenin in S. aureus and suggests the possibility of naringenin being used in the industrial food industry for the prevention of biofilm formation.

Enhanced synthesis of succinylated whey protein isolate by pulsed electric field pretreatment.

The objective of this study was to investigate the feasibility of pulse electric field (PEF) as a pretreatment for whey protein isolate (WPI) before its succinylation. The degree of succinylation (DS) of WPI increased from 88.31% for native WPI to 93.45% for PEF-pretreated WPI (PWPI, initial pH 10.0) for the same succinic anhydride (SA) to WPI ratio (1:1). Fourier transform infrared spectroscopy and scanning electron microscopy analysis proved the successful succinylation of WPI. For PWPIs, the surface hydrophobicity, exposed sulphydryl, and total sulphydryl decreased, which indicates the occurrence of changes in protein structures with more hydrophilic groups and better protein dispersion. Moreover, PEF may expose more amino acid residues binding sites that are present inside the protein, which is more suitable for succinylation. Therefore, the PEF pretreatment of proteins can improve their efficient use that is expected to play a critical role in succinylation industry.

Pulsed electric field assisted modification of octenyl succinylated potato starch and its influence on pasting properties.

The physicochemical properties and structural changes of potato starch esterified with octenyl succinic anhydride (OSA) assisted with pulsed electric field (PEF) were investigated. Results showed that PEF treatment during esterification resulted in a significant modification of pasting properties. The pasting temperature at 2-6 kV/cm reduced by 7.6-15.1 °C for PEF-assisted OSA starches but only by 3 °C for OSA modified starch without PEF treatment as compared to that of native starch. PEF-assisted esterification could reduce the reaction time and improve the reaction efficiency over the control by 6.1-39.1 %. A novel schematic model on structure-functionality relationship for PEF-assisted OSA modified starch was proposed. Structural disorganizations of starch induced lower pasting temperature and paste viscosity. The results suggest that PEF could be a potential eco-friendly and cost-effective physical technique to prepare starch products with desired paste behaviors and to broaden its application area especially in papermaking and textile industries.

Impact of pulsed electric field treatment on drying kinetics, mass transfer, colour parameters and microstructure of plum.

The aim of the present study was to scrutiny the impact of pulsed electric field (PEF) as a pre-treatment method on the convective drying kinetics, cell disintegration, colours and microstructural changes of fresh plums. In this study, the PEF intensities of 1-3 kV/cm, pulses number 30 and 70 °C drying temperature was applied to detect the drying kinetics. The specific energy consumption generated by PEF treatment was 10-90 kJ/kg. It was explored that the cell disintegration index increased from 0.147 to 0.572 with increased electric field intensity from 1 to 3 kV/cm. Further, we found that high cell disintegration leads to increase in drying rate and shorten drying time. The rates of water diffusion coefficient also increase with increasing PEF intensity from 0.27 to 16.47 × 10-9 m2/s. PEF pre-treatment followed by convective drying results in enhanced lightness and chroma as compared to untreated plum. Furthermore, the microscopic analysis by scanning electron microscopy at 200 × revealed that the PEF treatment at 3 kV/cm had caused shrinkage in the plum tissues which might be responsible for higher diffusion rate of water in the plum. In this work was investigated that drying kinetics and mass transfer after PEF treatment to improve quality of dried plum.

Cinnamaldehyde inhibit Escherichia coli associated with membrane disruption and oxidative damage.

In this study, the antimicrobial mechanism of cinnamaldehyde (CIN) against Gram-negative Escherichia coli ATCC 25922 (E. coli) based on membrane and gene regulation was investigated. Treatment with low concentration (0, 1/8, 1/4, 3/8 MIC) of CIN can effectively suppress the growth of E. coli by prolonging its lag phase and Raman spectroscopy showed obvious distinction of the E. coli after being treated with these concentration of CIN. The determination of relative conductivity indicated that CIN at relatively high concentration (0, 1, 2, 4 MIC) can increase the cell membrane permeability, causing the leakage of cellular content. Besides, the content of malondialdehyde (MDA) and the activity of total superoxide dismutase (SOD) of E. coli increased with increasing treatment concentration of CIN, implying that CIN can cause oxidative damage on E. coli cell membrane and induce the increase of total SOD activity to resist this oxidative harm. Moreover, quantitative real-time RT-PCR (qRT-PCR) analysis revealed the relationship between expression of antioxidant genes (SODa, SODb, SODc) and treatment CIN concentration, suggesting that SOD, especially SODc, played a significant role in resistance of E. coli to CIN. The underlying inactivation processing of CIN on E. coli was explored to support CIN as a potential and natural antimicrobial agent in food industry.

Hydroxyl-related differences for three dietary flavonoids as inhibitors of human purine nucleoside phosphorylase.

In this work, the hydroxyl-related differences of binding properties and inhibitory activities of dietary flavonoids, namely chrysin, baicalein and apigenin against purine nucleoside phosphorylase (PNP) were investigated. It was found that the hydroxylation on position C4' of chrysin (→apigenin) mildly decreased the binding affinities for PNP, whereas on the position C6 of chrysin (→baicalein) significantly increased binding affinities. Comparatively, the hydroxylation on position C4' and C6 greatly improved their PNP inhibitory effects. The IC50 values of apigenin and baicalein were 6.09 × 10-5 M and 8.94 × 10-5 M, respectively, which is significantly lower than that of chrysin (2.13 × 10-4 M). Results from molecular modeling revealed that there are two binding sites, i.e. active site (major) and tryptophan site (minor) on PNP, and the binding of these flavonoids might induce a serious conformational destabilization of PNP as a result of altering the micro-environment and morphology by flavonoids.

Metabolic profiling of antioxidants constituents in Artemisia selengensis leaves.

This study aimed to evaluate the antioxidant potential of Artemisia selengensis Turcz (AST) leaves, a byproduct when processing AST stalk, and identify the antioxidant constituents by using HPLC-QTOF-MS(2). The total phenolics content (TPC), total flavonoids content (TFC) and antioxidant abilities of fractions resulted from the successively partition of chloroform, ethyl acetate and n-butanol were compared. Ethyl acetate fraction (EAF) exhibited the highest TFC (65.44 mg QuE/g fraction), n-butanol fraction (nBuF) showed the highest TPC (384.78 mg GAE/g fraction) and the best DPPH scavenging ability, ABTS(+) scavenging ability and reducing power. Totally, 57 compounds were identified or tentatively identified in nBuF and EAF, 40 of them were reported in AST for the first time. The major constituents in EAF were flavonoids, and the major constituents in nBuF were phenolic acids and organic acids. Thus, AST leaves might be a potential low-cost resource of natural antioxidants.

Response surface optimization and physicochemical properties of polysaccharides from Nelumbo nucifera leaves.

Dynamic high pressure microfluidization (DHPM)-assisted extraction (DHPMAE) of lotus (Nelumbo nucifera) leaves polysaccharides (LLPs) was optimized by response surface methodology. The optimal extraction conditions were: liquid/solid ratio of 35:1 (v/m, mL/g), processing pressure of 180 MPa, processed two times, extraction temperature of 76°C, extraction time of 50 min. Under the optimal extraction conditions, DHPMAE produced a higher polysaccharides yield (6.31%) than leaching (2.95%). Scanning electron microscope (SEM) analysis revealed that DHPM could reduce the particles size and make the surface more unconsolidated. The LLPs prepared by both methods showed similar FT-IR spectrum, and were consisted of the same monosaccharides, including rhamnose, fucose, arabinose, xylose, mannose, glucose and galactose. The content of each monosaccharide in extracts, however, was quite different. The average molecular weight of LLPs prepared by DHPMAE is 550 kDa, smaller than 578 kDa obtained by leaching. The LLPs prepared by DHPMAE exhibited stronger DPPH scavenging ability (IC50 value of 0.38 mg/mL), HO scavenging ability (IC50 value of 0.61 mg/mL) and reducing power. Therefore, DHPMAE can be a promising alternative to traditional extraction techniques for polysaccharides from plants, and lotus leaves might be a potential resource of natural antioxidants.

[Comparison between antitumor effect and chemical constituents of Huanglian Jiedu decoction and that of serum containing Huanglian Jiedu decoction].

OBJECTIVE: To make a comparison between the antitumor effect and the chemical constituents of Huanglian Jiedu decoction (HLJDT) and that of serum containing HLJDT. METHOD: Based on the established chromatographic fingerprint of HLJDT, analysis and comparison were made between the HPLC fingerprints of rat serum samples obtained after orally taking HLJDT and those of control rat serum samples. The different effects on NCI-H446 and Bel-74024 cancer cells from human were investigated in vitro using HLJDT and its serum. The inhibitory effects of HLJDT and its serum were observed by MTT assay. RESULT: Ten compounds of HLJDT and some metabolites were detected after oral administration of HLJDT, and however some main compounds of HLJDT were not detected in serum. Both HLJDT and its serum in different dosage groups could inhibit the proliferation of NCI-H446 and Bel-7402 cancer cells from human in a dose-dependent manner, but inhibitory grade was different in the two cancer cell lines. HLJDT had more inhibitory effect on Bel-7402 than on NCI-H446, on the other hand serum containing HLJDT had the same inhibitory effect on Bel-7402 and NCI-H446. CONCLUSION: The reason for inhibitory grade change was that the proportion of concentration of many compounds in serum containing HLJDT was different to that in HLJDT, which should be subject to thorough investigation so as to illuminate the pharmacology and active mechanism of HLJDT.

[Study on antitumor activities of huanglian jiedu decoction].

OBJECTIVE: To study the antitumor activity of Huanglian Jiedu decoction (HLJDT). METHOD: Antitumor activities were tested in mice with experimental tumor H22 in vivo, and the thymus index, spleen index and tumor inhibitory rate were evaluated. The effects on cancer cells from human were investigated in vitro using serum pharmacological approach. Swille, SPC-A-1, SGC-7901 and MCF-7 cancer cells were incubated in culture media containing serum from mice medicated with HLJDT. The inhibitory effects of HLJDT serum were observed by MTT assay. RESULT: HLJDT showed significant antitumor activities on H22 in mice. All of the HLJDT serum in different dosage groups could highly inhibit the proliferation of 4 cancer cell lines from human. CONCLUSION: The HLJDT can significantly inhibit the tumor H22 in mice in a dose-dependent manner, the drug serum has obvious anticancer effects against Swille, SPC-A-1, SGC-7901 and MCF-7.

[Qualitative and quantitative determination of the main components of huanglianjiedu decoction by HPLC-UV/MS].

AIM: To establish a comprehensive HPLC analytical method of Huanglianjiedu decoction. METHODS: This study was performed by HPLC-UV/MS to identify the chemical constituents of the whole and individual herbs of the "Huanglianjiedu decoction". Zorbax Extend C18 (150 mm x 4. 6 mm ID, 5 microm) column was used; the mobile phase was composed of acetonitrile (A) and water (B, with 0.5% acetic acid) with gradient elution; the flow rate was 1.0 mL x min(-1) and the column temperature was setup at 25 degrees C. The detection wavelength was 254 nm. RESULTS: The chromatogram of Huanglianjiedu decoction showed 21 main peaks. Peaks 1, 2, 5 and 18 were from Gardenia jasminoides Ellis, Peaks 8, 13, 14, 15, 16, 17, 19 and 21 from Scutellaria baicalensis Georgi. While 10 from Coptis chinensis Franch and 20 from Phellodendron amurense Rupr., Peaks 3, 4, 6, 9, 11 and 12 came from them together. Peak 7 presented in the chromatograms of the herbs except Gardenia jasminoides Ellis. By comparison of the retention time, the on-line UV spectra and MS spectra, 11 peaks were identified as 5 (geniposide), 9 (jatrorrhizine), 10 (coptisine), 11 (palmatine), 12 (berberine), 13 (baicalin), 15 (oroxin A), 17 (wogonoside), 19 (baicalein), 20 (obaculactone), 21 (wogonin), then eight of them were quantified by HPLC-UV. CONCLUSION: The method could represent the characteristics of Huanglianjiedu decoction, and it could be used to evaluate the quality and quantity of Huanglianjiedu decoction. It distinguished between Coptis chinensis Franch and Phellodendron amurense Rupr. by HPLC for the first time.