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BackgroundPectins are a class of acidic polysaccharides with complex structures. Different pectin molecules are composed of different domains, which have an important impact on their biological activity.ObjectiveThis study aimed to determine the structural features and the antioxidant activities of the pectic polysaccharides isolated from Veronica peregrina L.MethodsThe polysaccharide was isolated from Veronica peregrina L by water extraction and fractionated by ion exchange chromatography and gel permeation chromatography. The structure features of the pectic polysaccharides were determined by Fourier transforminfrared spectroscopy (FT-IR) and Nuclear magnetic resonance (NMR). The antioxidant activities was evaluated by the DPPH, OH and ABTS radical scavenging ability.ResultsWVPP-A2b and WVPP-A3b, with molecular weights of 48.7 × 104 and 77.6 × 104 kDa, respectively, contained homogalacturonan (HG), rhamnogalacturonan I (RG-I), and rhamnogalacturonan II (RG-II) domains with a mass ratio of 2.08:2.64:1.00 and 3.87:4.65:1:00, respectively. The RG-I domain contained an arabinogalactan II backbone and arabinans consisting of t-Araf, (1→5)-α-Araf, and (1→3,5)-α-Araf. WVPP-A3b also contained short chains consisting of the [t-Araf-(1→5)-α-Araf-(1→] structural unit. WVPP-A3b showed stronger ability to scavenge DPPH, hydroxyl, and ABTS radicals, which was potentially associated with its high content of galacturonic acid and presence of the HG domain.ConclusionThe results provide information for enhancing knowledge of the structureactivity relationship of pectic polysaccharides from V. peregrina and their potential application in the healthcare food field.

Background: Malignant arrhythmias require drug therapy. However, most of the currently available antiarrhythmic drugs have significant side effects. Ginsenoside Rg2 exhibits excellent cardioprotective effects and appears to be a promising candidate for cardiovascular drug development. So far, the oral toxicity and antiarrhythmic effects of Rg2 have not been evaluated. Methods: Acute oral toxicity of Rg2 was assessed by the Limit Test method in mice. Subchronic oral toxicity was determined by repeated dose 28-day toxicity study in rats. Antiarrhythmic activities of Rg2 were evaluated in calcium chloride–induced arrhythmic rats. Antiarrhythmic mechanism of Rg2 was investigated in arrhythmic rats and H9c2 cardiomyocytes. Results: The results of toxicity studies indicated that Rg2 exhibited no single-dose (10 g/kg) acute oral toxicity. And 28-day repeated dose treatment with Rg2 (1.75, 3.5 and 5 g/kg/d) demonstrated minimal, if any, subchronic toxicity. Serum biochemical examination showed that total cholesterol in the high-dose cohort was dramatically decreased, whereas prothrombin time was increased at Day 28, suggesting that Rg2 might regulate lipid metabolism and have a potential anticoagulant effect. Moreover, pretreatment with Rg2 showed antiarrhythmic effects on the rat model of calcium chloride induced arrhythmia, in terms of the reduced duration time, mortality, and incidence of malignant arrhythmias. The antiarrhythmic mechanism of Rg2 might be the inhibition of calcium influx through L-type calcium channels by suppressing the phosphorylation of Ca2+/calmodulin-dependent protein kinase II. Conclusion: Our findings support the development of Rg2 as a promising antiarrhythmic drug with fewer side effects for clinical use.

Treatment of malignant brain tumors continues to challenge scientists and clinicians alike. Location of these tumors within the central nervous system (CNS), which is considered a "privileged" organ, can prevent the penetration of chemotherapeutic agents through the blood–brain barrier (BBB). To overcome this limitation, nanoparticles are taken up and transported by macrophage and then delivered directly into the CNS. In this study, we used macrophage to uptake the folate-targeted bifunctional micelles loaded with near-infrared (NIR) dye ICG-Der-01 and investigate the dynamic bio-distributions of macrophage after intravenous injection into tumor-bearing mice. In vitro cellular experiments by confocal microscopy indicated that the uptake of micelles in macrophage was greatly enhanced due to the folate receptor overexpression. Dynamic bio-distributions of macrophage showed a rapid clearing rate through the liver intestine pathway. In conclusion, macrophage could potentially be used as nanoparticle drug carriers and require further investigation.

A novel near-infrared light responsive microcapsule system, gold nanorod-covered DOX-loaded hollow CaCO3 microcapsule (AuNR-HM-DOX) is developed for cancer therapy. The hollow CaCO3 microcapsules were prepared based on the self-assembly between chitosan and sodium alginate on CaCO3 particles via layer-by-layer technique, and then covered with gold nanorods to obtain the microcapsule system. Upon near-infrared (NIR) irradiation, microcapsule with gold nanorods can convert the absorbed NIR light into heat. Meanwhile, doxorubicin (DOX), a chemotherapy drug, is loaded into the microcapsule system via electrostatic adsorption for combined photothermal therapy and chemotherapy. Properties of AuNR-HM-DOX including grain diameter, optical spectra were characterized. Confocal fluorescence imaging was performed to observe the morphology of the capsules and existence of DOX in the core, confirming the successful loading of DOX. The release of DOX from the capsules under continuous NIR irradiation was investigated to evaluate the temperature responsiveness of AuNR-HM-DOX. Results indicate that AuNR-HM-DOX microcapsules possess uniform particle size and high light responsiveness. The combination of chemical and physical therapy of AuNR-HM-DOX features great potential as an adjuvant therapeutic alternative material for combined cancer therapy.

Polysaccharides display poor cell adhesion due to the lack of cell binding domains. This severely limits their applications in regenerative medicine. This study reports novel cross-linked pectin nanofibers with dramatically enhanced cell adhesion. The nanofibers are prepared by at first oxidizing pectin with periodate to generate aldehyde groups and then cross-linking the nanofibers with adipic acid dihydrazide to covalently connect pectin macromolecular chains with adipic acid dihydrazone linkers. The linkers may act as cell binding domains. Compared with traditional Ca2+-cross-linked pectin nanofibers, the pectin nanofibers with high oxidation/cross-linking degree exhibit much enhanced cell adhesion capability. Moreover, the cross-linked pectin nanofibers exhibit excellent mechanical strength (with Young's modulus ~10 MPa) and much enhanced body degradability (degrade completely in 3 weeks or longer time). The combination of excellent cell adhesion capability, mechanical strength, and body degradability suggests that the cross-linked pectin nanofibers are promising candidates for in vivo applications such as tissue engineering and wound healing. This cross-linking strategy may also be used to improve the cell adhesion capability of other polysaccharide materials. [ABSTRACT FROM AUTHOR]

Adriamycin (ADM) has been effective against many types of solid tumors in clinical applications. However, its use is limited because of systemic toxicities, primarily cardiotoxicity, and multidrug resistance. In this study, a new active receptor-mediated complex, ADM conjugated with 2-amino-2-deoxy-D-glucose and succinic acid (2DG-SUC-ADM), was designed to target tumor cells through glucose transporter 1 (GLUT1). MTT assay and confocal images showed that the complex had better inhibition rate to tumor cells and low toxicity to normal cells. Most importantly, the complex displayed a potential to reverse overcome multidrug resistance in cancer cells, with more complex transported into the nucleus of tumor cells. Our in vivo experiments also showed that this new complex could significantly decrease organ toxicity and enhance the antitumor efficacy compared with free ADM, indicating a promising drug of 2DG-SUC-ADM for targeted cancer therapy. [ABSTRACT FROM AUTHOR]

CdHgTe-folate conjugates, acting as novel active-targeting fluorescence probes, were prepared by covalent conjugation of CdHgTe QDs and folic acid. Their characteristics, such as optical spectra, stability and cancer cell targeting were investigated in detail. The fluorescence wavelength of CdHgTe-folate conjugates was 790 nm and a full width at half-maximum (FWHM) of them was 50-70 nm. Their fluorescence stability could satisfy the need of long and continuous fluorescence imaging. The in vivo dynamic bio-distribution of CdHgTe-folate conjugates in S180 tumor beard mouse model was monitored by a NIR imaging system. The resultes indicated that CdHgTe-folate conjugates targeted to tumor effectively. The high fluorescence intensity together with targeting effect makes CdHgTe-folate conjugates promising candidates for imaging, monitoring and early diagnosis of cancer at molecular and cell level. [ABSTRACT FROM AUTHOR]