Hypolipidemic Activity and Mechanism of Action of Sargassum fusiforme Polysaccharides.

Sargassum fusiforme polysaccharide (SFP) is a kind of biologically active macromolecule with biological functions. In this study, oxidative stress and high-fat HepG2 cell models were established to investigate its lipid-lowering activity and mechanism of action. It was found that SFP and its two isolated fractions had antioxidant effects on the cells. It was also found the polysaccharides decreased the content of total cholesterol and total triglyceride in the high-fat cells. RT-qPCR assays revealed that the three polysaccharides down-regulated the mRNA expression level of ACC, PPARγ, and SREBP-2. It could be concluded that the hypolipidemic effect of SFPs is achieved via multiple pathways, including the regulation on the expression level of lipid metabolism-related key enzymes and factors, and binding with bile acids. The hypolipidemic effect of SFPs could be partially due to their antioxidant activity. SFPs developed in the present work have potential as ingredients of functional foods with hypolipidemic effect.

Exopolysaccharide from Lactobacillus rhamnosus ZFM231 alleviates DSS-induced colitis in mice by regulating gut microbiota.

BACKGROUND: The exopolysaccharides (EPS) produced by Lactobacillus and other probiotics are associated with many benefits, such as immune regulation, antioxidant properties, antitumor effect, and regulation of intestinal microbe homeostasis. In the present study, the modulatory effect of EPS produced by Lactobacillus rhamnosus ZFM231 on the intestinal flora of mice with inflammatory bowel disease induced by dextran sulfate solution was investigated. RESULTS: Results indicated that weight loss, colonic length, the disease activity index score and colonic tissue damage in mice were significantly improved by EPS treatment. Compared with the model group, in the EPS-treated group, the diversity of and the composition of gut microbiota at both phylum and genus levels were found to recover to the levels of normal group, indicating the effective modulation on gut microbiota by EPS; short-chain fatty acids, including acetic acid, propionic acid and butyric acid produced by intestinal microbial metabolism, increased significantly; the level of anti-inflammatory factor transforning growth factor-ß significantly increased and the level of pro-inflammatory factor tumor necrosis factor-α significantly decreased in the colonic cells of EPS-treated mice. CONCLUSION: It is clear that EPS produced by L. rhamnosus ZFM231 could find application in functional foods with the property of anti-ulcerative colitis. The experimental results provide new insights into the probiotic effect of EPS. © 2022 Society of Chemical Industry.

Anti-inflammatory effect and component analysis of Chaihu Qingwen granules.

ETHNOPHARMACOLOGICAL RELEVANCE: As prevalent acute respiratory condition in clinical practice, acute lung injury has a quick start and severe symptoms which can harm patients physically. Chaihu Qingwen granules (CHQW) is a classic formula for the treatment of respiratory diseases. Clinical observation shows that CHQW has good efficacy in treating colds, coughs, and fevers. AIM OF THE STUDY: The aim of this study was to investigate the anti-inflammatory effect of CHQW on lipopolysaccharide (LPS)-induced acute lung injury (ALI) model in rats and to explore its potential mechanism, as well as to clarify its substance composition. MATERIALS AND METHODS: Male SD rats were randomly divided into the blank group, the model group, the ibuprofen group, the Lianhua Qingwen capsule group and the CHQW group (2, 4 and 8 g/kg, respectively). The LPS-induced acute lung injury (ALI) model in rats was established after pre-administration. The histopathological changes in the lung and the levels of inflammatory factors in bronchoalveolar lavage fluid (BALF) and serum of ALI rats were observed. The inflammation-related proteins toll-like receptor 4 (TLR4), inhibitory kappa B alpha (IκBα), phospho-IκBα (p-IκBα), nuclear-factor-kappa B (NF-κB), and NLR family pyrin domain containing 3(NLRP3) expression levels were measured by western blotting analysis and immunohistochemical analysis. The chemical composition of CHQW was identified by liquid chromatography-quadrupole-time of flight-mass spectrometry (LC-Q-TOF-MS). RESULTS: CHQW significantly ameliorated lung tissue pathological injury in LPS-induced ALI rats and decreased the release of inflammatory cytokines (interleukin-1ß, interleukin-17 and tumor necrosis factor-α) in BALF and serum. In addition, CHQW decreased the expression of TLR4, p-IκBα and NF-κB proteins, increased the level of IκBα, regulated the TLR4/NF-κB signaling pathway, and inhibited the activation of NLRP3. The chemical components of CHQW were analyzed by LC-Q-TOF-MS, and a total of 48 components were identified by combining information from the literature, mainly flavonoids, organic acids, lignans, iridoids and phenylethanoid glycosides. CONCLUSION: The results of this study showed that the pretreatment of CHQW had a strong protective effect on LPS-induced ALI in rats, reducing lung tissue lesions and decreasing inflammatory cytokines released in BALF and serum. The protective mechanism of CHQW may be related to the inhibition of the TLR4/NF-κB signaling pathway and NLRP3 activation. The main active ingredients of CHQW are flavonoids, organic acids, lignans, iridoids and phenylethanoid glycosides.

Purification, physico-chemical properties and antioxidant activity of polysaccharides from Sargassum fusiforme by hydrogen peroxide/ascorbic acid-assisted extraction.

The biological activities of Sargassum fusiforme polysaccharides (SFP) were affected significantly by the extraction method. In order to screen the optimum extraction technology for SFP with high yield and biological activities, six extraction methods, including hot water extraction (HWE), acid-assisted extraction (ACAE), alkali-assisted extraction (ALAE), ultrasonic-assisted extraction (UAE), microwave-assisted extraction (MAE) and hydrogen peroxide/ascorbic acid-assisted extraction (HAE) were compared for the preparation of SFP. Based on the yield and in vitro antioxidant activity of the crude polysaccharides obtained by the six extraction methods, HAE was selected for the extraction of SFP. The SFP prepared by HAE (H-SFP) was purified by cellulose DEAE-52 ion-exchange chromatography, obtaining two purified fractions, namely H-SFP3 and H-SFP5. The analyses of their chemical composition, physico-chemical properties and the antioxidant capacity were performed. It was found that the crude SFP and the purified fractions possessed considerable ability to scavenge DPPH, hydroxyl and ABTS•+ radicals. These polysaccharide fractions were also found to effectively reduce the reactive oxygen species (ROS) level and increase the superoxide dismutase (SOD) activity in H2O2-induced oxidative stress RAW264.7 cells. The SFP prepared by the HAE has the potential as a natural non-toxic antioxidant and can be used as an ingredient in functional foods.

Physicochemical, structural and rheological properties of pectin isolated from citrus canning processing water.

In order to better utilize the citrus pectin (CP) resource, the crude citrus pectin (CCP), obtained from the citrus fruit canning processing waste water, was purified by cellulose DEAE-52 column, providing neutral polysaccharide CP0 and two acidic polysaccharides (CP1 and CP3). CP1 had the highest yield among the three fractions, being 44.29%. The chemical composition, structure and morphology of these pectin components were analyzed. Monosaccharide composition analysis revealed that arabinose was the most abundant composition in these pectin samples. CCP, CP1 and CP3 were mainly composed of rhamnogalacturonan-I (RG-I) regions. Compared with CP3, CCP and CP1 had longer side chains, which are mainly consisted of arabinose. FT-IR and NMR analysis indicated that α-type glycosidic bonds are the main linkage in the four pectin components. These CP samples were found to possess different conformation, but no triple-helical conformation was observed in all these CP fractions. Scanning electron microscopy revealed that CCP, CP1 and CP3 all had irregular sheet-like structures and partly porous structures. The four pectin components showed the characteristics of non-Newtonian fluids and possessed good viscoelasticity. Due to these properties, the pectin might have potential application in food industry as food thickening agent.

The first copper(I) complex of anthrahydrazone with potential ROS scavenging activity showed significant in vitro anticancer activity by inducing apoptosis and autophagy.

Based on the anticancer pharmacophore of anthrahydrazone and quinoline, a new quinolylanthrahydrazone ligand, 9-AQH (anthracene-9-quinolylhydrazone), was synthesized to further afford four metal complexes, [CoII(9-AQH)(NO3)2(H2O)] (1), [NiII(9-AQH)2(H2O)2]·2NO3 (2), [CuI(9-AQH)2]·NO3 (3), [ZnII(9-AQH)2(NO3)]·NO3 (4), determined by X-ray single crystal diffraction analysis. The reaction of Cu(NO3)2 with 9-AQH formed the stable and repeatable copper(I) complex 3. In vitro screening demonstrated only 3 showed significant and broad-spectrum anticancer activity, indicating that Cu(I) played a key role in exerting the anticancer activity. In solution, Cu(I) was not naturally oxidized to Cu(II) suggested by 1H-NMR (Nuclear Magnetic Resonance) and EPR (Electron Paramagnetic Resonance) analysis. The presence of 3 could also catalyze the H2O2 system to give hydroxyl free radicals, suggested by further EPR and electrophoresis assay. At the cellular level, although no obvious Cu(II) signals were detected and the total ROS (Reactive Oxygen Species) scavenging in the tumor cells treated with 3, the potential redox property between Cu(I)/Cu(II), as a key role, should not be denied for the significant anticancer activity of 3, considering the much complicated circumstance and other reductive substances in cells. The anticancer mechanism of 3 on the most sensitive MGC-803 cells pointed to significant cell apoptosis through mitochondrial pathway, rather than cell cycle arrest. While the autophagy observed in tumor cells treated by 3 suggested its complicated anticancer mechanism, and whether there was an intrinsic correlation still needed to be further investigated.

The copper(II) complexes of new anthrahydrazone ligands: In vitro and in vivo antitumor activity and structure-activity relationship.

Two new copper(II) complexes, 9-PMAH-Cu (1) and 9-FPMAH-Cu (2), of anthrahydrazone were synthesized and structurally characterized, in which 9-FPMAH (9-(4'-trifluoromethyl)-pyrimidine anthrahydrazone) is the 4'-CF3 derivative of 9-PMAH (9-pyrimidine anthrahydrazone). Both complexes 1 and 2 showed similar intercalative binding modes towards DNA and might compete with the typical DNA intercalator, GelRed, in the same binding site. They could also act as topoisomerase (type I) suppressor to effectively inhibit its activity, in which complex 1 was more effective than 2. The in vitro antitumor screening indicated that complex 1 displayed much higher antiproliferative ability than 2 and cisplatin towards all the tested tumor cell lines. On the other hand, complex 1 also showed high cytotoxicity against human normal liver cell line HL-7702, suggesting it is a potential high cytotoxic antitumor candidate. While it was also suggested that the loss of activity of complex 2 might be due to the presence of 4'-CF3 on the pyrimidine ring. Studies on the cellular level showed that complex 1 could arrest the cell cycle of the most sensitive T-24 cells at G2/M phase and induced cell apoptosis. Complex 1 further showed a significant suppression on the tumor growth on the T-24 tumor xenograft mouse model, but not reduced the body weight. Especially, complex 1 could retain its coordination state in H2O even in the presence of HSA. The results suggests that complex 1 is of enough safety to be considered as a promising anticancer candidate by combining the bioactive Cu(II) and the anthrahydrazone pharmacophore.