Branched chain amino Acids as in vitro and in vivo Anti-Oxidation Compounds

Background and aims: Branched chain amino acids (BCAAs) can be tightly connected to metabolism syndrome (MetS) which can be counted as a metabolic indicator in the case of insulin resistance (IR). The aim of this study was to assess the potential role of these acids under oxidative stress. Material and Methods: the in vitro antioxidant activity of BCAAs was assessed using free radical 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) scavenging assays. For further check, a qRT-PCR technique was madefor detection the extent of alterations in gene expression of antioxidative enzymes (catalase and glutathione peroxidase (Gpx)) in lipopolysaccharides (LPS(-induced macrophages RAW 264.7 cell line. Additionally, BCAAs antioxidant activity was evaluated based on plasma H2O2 levels and xanthine oxidase (XO) activity in prooxidative LPS-treated mice. Results: Different concentrations of BCAAs affected on DPPH radical scavenging activity but to lesser extent than the ascorbic acid. Besides, BCAAs obviously upregulated the gene expression levels of catalases and Gpx in LPS-modulated macrophage RAW 264.7 cell line. In vivo BCAAs significantly minimized the level of plasma H2O2 as well as the activity of XO activity under oxidative stress. Conclusion: our current findings suggest that BCAAs supplementation may potentially serve as a therapeutic target for treatment of oxidative stress occurs with atherosclerosis, IR-diabetes, MetS and tumorigenesis.

Lipidated Methotrexate Microbubbles: A Promising Rheumatoid Arthritis Theranostic Medicine Manipulated via Ultrasonic Irradiation

De novo designed lipidated methotrexate was synthesized and self-assembled into microbubbles for targeted rheumatoid arthritis theranostic treatment. Controlled lipidatedmethotrexate delivery was achieved by ultrasound-targetedmicrobubble destruction technique. Methotrexate was dissociated inflammatory microenvironment of synovial cavity, owing to representive low pH and enriched leucocyte esterase. We first manipulated methotrexate controlled release with RAW 264.7 cell line in vitro and further verified with rheumatoid arthritis rabbits in vivo. Results showed that lipidated methotrexate microbubbles precisely affected infection focus and significantly enhanced rheumatoid arthritis curative effect comparing with dissociative methotrexate. This study indicates that lipidated methotrexate microbubbles might be considered as a promising rheumatoid arthritis theranostics medicine.

A New Phenylpropanoid from the Roots of Solanum melongena L. and Evaluation of Anti-inflammatory Activity

Fifteen phenylpropanoids were isolated from the ethanol extract of the roots of Solanum melongena L., including a new compound, melongenapanoid A (1), together with fourteen known compounds (2-15). Their chemical structures were elucidated by 1D and 2D NMR and HR-MS data according to those values of the literatures. The fourteen known compounds (2-15) were all firstly isolated from this plant. While, the isolates were evaluated for the inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 cell line. Compounds 2, 4 and 5 showed moderate inhibition of NO production with IC50 values of 28.7, 24.4 and 32.6 μM, respectively.

HPLC-UV-Based Simultaneous Determination of Canthin-6-One Alkaloids, Quassinoids, and Scopoletin: The Active Ingredients in Eurycoma Longifolia Jack and Eurycoma Harmandiana Pierre, and Their Anti-Inflammatory Activities

Background Quassinoids and canthin-6-one alkaloids are bioactive markers of Eurycoma longifolia (EL) and E. harmandiana (EH) and have been commercially utilized to treat inflammation and male infertility. Objectives This study aims to reveal the contents of bioactive compounds and compare anti-inflammatory activities of these two species. Methods HPLC methods coupled with UV-Vis detection were developed and validated for the simultaneous analysis of the chemical profiles and their contents in EL and EH. The anti-inflammatory activities of both species were investigated using RAW 264.7 cell line. Results The HPLC methods provided a sensitivity (LOD) of 0.02–0.05 µg/mL for the eight bioactive compounds (canthin-6-one alkaloids, quassinoids, and scopoletin) with high precision (% relative standard deviation (RSD) ≤6.48) and recoveries between 80.0 and 120%. The chaparrinone: eurycomanone ratio was high in EH, whereas EL had a higher ratio of eurycomanone: chaparrinone than EH. The contents of total canthin-6-one alkaloids, quassinoids, and scopoletin were 0.01–0.75, 0.19–1.54, and 0.01–0.28 mg/g, respectively, in EL roots and 0.12–1.80, 7.05–9.26, and 0.02 mg/g, respectively, in EH roots. The anti-inflammatory effects of EL and EH extracts varied among the samples due to the variation in their chemical constituents. Conclusions In summary, our study indicated that chaparrinone was the major compound in EH. EH exhibited anti-inflammatory activity to the same extent as EL. Highlights EH and EL extracts were analyzed using developed HPLC-UV methods, revealing a high concentration of chaparrinone in EH, and an anti-inflammatory assay indicated that EH had a potency comparable to that of EL.

In vitro Evaluation of the Antiproliferative Effect, Cytotoxicity and Proinflammatory Activity of the Food Additive Monosodium Glutamate on RAW 264.7 Cell Line

Monosodium glutamate (E-621, abbreviated MSG) is a food additive widely used in the food domain as a flavor and taste enhancer. The present study aims to evaluate in vitro the effects of increased concentrations of MSG, using the RAW 264.7 murine macrophage line. The study was conducted in 3 complementary directions: first, establishing the ability of monosodium glutamate to induce cell mortality, by using the MTT assay to determine cell viability; second, establishing by its oxidizing activity if MSG is toxic for cells inducing oxidative stress, measured by the Griess test for determination of extracellular NO; third, to observe whether MSG presence induces an immune response quantified by the secretion of proinflammatory cytokines, TNFα in this case, measured through the immunoenzymatic ELISA technique.

The Health-Benefits and Phytochemical Profile of Salvia apiana and Salvia farinacea var. Victoria Blue Decoctions

Salvia apiana and Salvia farinacea var. Victoria Blue decoctions were screened for diverse bioactivities, including the ability to counteract oxidative and inflammatory events, as well as to act as cytotoxic and antimicrobial agents. Both extracts showed good activities and that of S. apiana origin was particularly effective regarding the ability to prevent lipid peroxidation and to prevent nitric oxide (NO●) production in lipopolysaccharide (LPS)-activated murine macrophage RAW 264.7 cell line (EC50 = 50 μg/mL). Moreover, it displayed high cytotoxic capacity against hepatocellular carcinoma HepG2, cervical carcinoma HeLa, and breast carcinoma cells MCF-7, but comparatively low effects in porcine liver primary cells, which highlights its selectivity (GI50 = 41–60 μg/mL vs. 362 μg/mL, respectively). Further, it exhibited inhibitory and lethal potential against a panel of Gram-positive and Gram-negative bacteria. It is possible that the bioactive properties of the two Salvia extracts are associated to their phenolic components and, in the particular case of S. apiana, to its richness in phenolic terpenes, namely in rosmanol, hydroxycarnosic acid and a derivative of sageone, which were found in the extract.