Efficacy of a functional food ingredient from Ensete superbum Roxb. Cheesman peel in reducing the severity of ulcerative colitis in a murine model.

Ulcerative colitis is a recurrent inflammatory illness of the colon with an elevated risk of developing colon cancer. The drugs presently used to treat UC cause adverse effects and are limited to symptomatic treatments. To overcome these constraints, naturally derived novel alternative therapies are being tested. Ensete superbum Roxb. Cheesman (wild banana) is used as a folk medicinal plant to treat stomach aches, diarrhea, and dysentery. Previous research has shown that a peel dioxane (PD) fraction obtained from a ripe peel aqueous extract of E. superbum Roxb. Cheesman possesses in vitro antioxidant, anti-inflammatory and anti-colon cancer effects. Furthermore, it has been shown to alleviate 2,4,6-trinitrobenzene sulfonic acid (TNBS) induced ulcerative colitis (UC) in rats. The current study intended to evaluate its efficacy as a functional dietary component added to cold pressed orange juice in colitic rats, and deduce the molecular processes involved in UC amelioration. The PD fraction in orange juice ameliorated colitis by modulating the oxidative stress and inflammatory parameters in the damaged tissue with improved healing activity as indicated by a lower disease activity index (DAI) score. The ameliorative effect was related to the inhibition of the nuclear factor-κB (NF-κB) signaling pathway by downregulating the expression levels of NFκBp65, TNF-α, IL-6 and IL-1ß, followed by the recovery of epithelial barrier integrity. The ameliorating effects were statistically similar (p > 0.05) to those of the standard sulfasalazine treated population. The results suggest that PD fractions can be used as a new functional food and as an adjuvant to prevent IBDs due to their anti-colitic effect; however, it needs to be confirmed in clinical trials.

Anti-proliferative activity of Ensete superbum Roxb. Cheesman extract and its active principles on human colorectal cancer cell lines.

Ensete superbum Roxb. Cheesman (wild banana) is a plant traditionally used for the treatment of fever and diarrhea. On a preliminary screening, the ripe peel aqueous extract (PA) exhibited higher cytotoxicity (cell viability of 49% against HCT-15 at 75 µg/ml; and 46% against Caco2 at 50 µg/ml), superior anti-inflammatory (IC50 of 0.49 µg/ml), and greater anti-mutagenic activity at 500 µg/plate compared to the aqueous extracts of seed (SA), flower (FA) and bract (BA). Therefore, we further evaluated the anti-proliferative activity of PA and its fractions. The ability to inhibit the growth of cell lines (HCT-15 and Caco2) was used for the bio-guided fractionation and isolation of active compounds in PA using chromatographic techniques. Multiple extractions of the PA yielded the peel dioxane fraction (PD), and column fractionation of PD yielded eight compounds, of which three (Compound D-PDD, Compound E-PDE, and Compound G-PDG) possessed higher cytotoxic activity. At 10 µg/ml, the cell viability of HCT-15 was 50.1%, 46.5%, and 61.9%, respectively; Caco2 was 98.2%, 62.9%, and 64.7%, respectively, for PDD, PDE, and PDG. These compounds also showed apoptotic effect as evidenced by measuring the mitochondrial membrane potential, dual staining (acridine orange/ethidium bromide), DNA fragmentation, and the ROS status in colorectal cell lines. The UPLC-HRMS/MS, FTIR, and NMR data revealed the active compounds as quercetin-3-O-rutinoside, 3,5-dimethoxy-4-hydroxybenzoic acid, and 4',5,7-trihydroxyflavone. These findings indicate the anti-proliferative potential of PA, and warrant further investigation of its active principles in the amelioration of colorectal cancer in in vivo models. PRACTICAL APPLICATION: The potential of an underutilized crop as a source of therapeutic agents for colon cancer was established, as the study showed a high cytotoxic activity of wild bananas against HCT-15 and Caco2 cell lines. Bioactivity guided fractionation of peel fraction identified the active compounds present in wild banana, and their anticancer activity was attributed to the induction of cell death. The study indicated that wild banana has the potential to inhibit the growth of colon cancer cells.

Hyperlipidemia Downregulate Brain Antioxidant Defense Enzymes and Neurotrophins in Rats: Assessment of the Modulatory Potential of EPA+DHA and Zerumbone.

BACKGROUND: Oxidative stress (OS) plays a vital role in the pathogenesis of cognitive disorders. In this study, brain antioxidant defense dysregulation as a consequence of hyperlipidemia, and the efficacy of eicosapentaenoic acid (EPA) + docosahexaenoic acid (DHA), and zerumbone (Z) in their modulation are assessed. METHODS AND RESULTS: Male Wistar rats are fed control, high-fat (HF), HF + fish oil (HF+F), HF + zerumbone (HF+Z), and HF + fish oil + zerumbone (HF+F+Z) diet for 60 days. Markers of OS, antioxidant enzymes, monoamine oxidase, nuclear factor (erythroid-derived 2)-like 2 (NRF-2), nitric oxide-2 (NOS-2), inter cellular adhesion molecule-1 (ICAM-1), and neurotrophins are measured. Hyperlipidemia increases OS, decreases antioxidant enzyme activity, increases monoamine oxidase activity, increases NOS-2 and ICAM-1 expression, decreases NRF-2 activation, decreases nerve growth factor (NGF), and brain-derived neurotrophic factor (BDNF) levels in the brain compared to control. While EPA+DHA and zerumbone significantly (p < 0.05) restores the perturbations induced by hyperlipidemia. CONCLUSION: It is concluded that hyperlipidemia cause OS by decreasing the activity of brain antioxidant enzymes via the downregulation of NRF-2. The reduced brain neurotrophins in hyperlipidemia indicate its potential risk on cognitive attributes. EPA+DHA, together with zerumbone, positively modulates hyperlipidemia induced brain dysfunction thereby offering promising therapeutic strategy.

Structure-function activity of dehydrozingerone and its derivatives as antioxidant and antimicrobial compounds.

Dehydrozingerone, structural half analogue of curcumin, is a phenolic compound isolated from ginger (Zingiber officinale) rhizomes. Dehydrozingerone and several of its derivatives such as glucopyranosides and its tetra acetate derivative and 4-O-acetyl and methyl derivatives of dehydrozingerone were synthesized in the present study. Dehydrozingerone, synthesised with improved yield was used for the synthesis of Dehydrozingerone 4-O-ß-D-glucopyranoside (first time report) by modified Koenigs-Knorr-Zemplén method. Structures of all the compounds have been established using spectroscopic methods. These compounds were tested for radical scavenging activity by DPPH and FRAP method as well as for antibacterial and antifungal activities. The parent molecule exhibited better scavenging activity as compared to its derivatives indicating the significance of free phenolic hydroxyl group. Also, Dehydrozingerone and its derivatives exhibited antibacterial as well as antifungal activity due to the conjugation system present, which includes α,ß-unsaturated carbonyl (C = O) group. This study gave an insight into structural requirements for dehydrozingerone activity.