In Vitro Evaluation of the Phytopharmacological Potential of Sargassum incisifolium for the Treatment of Inflammatory Bowel Diseases

Abstract

Background: Comprised of Crohn’s disease and ulcerative colitis, inflammatory bowel diseases (IBD) are characterized by chronic inflammation of the gastro-intestinal tract, which often results in severe damage to the intestinal mucosa. This study investigated metabolites from the South African endemic alga, Sargassum incisifolium, as potential treatments for IBD. Phytochemical evaluation of S. incisifolium yielded prenylated toluhydroquinones and toluquinones, from which semi-synthetic analogs were derived, and a carotenoid metabolite. The bioactivities of S. incisifolium fractions, natural products, and semi-synthetic derivatives were evaluated using various in vitro assays. Methods: Sargahydroquinoic acid isolated from S. incisifolium was converted to several structural derivatives by semi-synthetic modification. Potential modulation of IBD by S. incisifolium crude fractions, natural compounds, and sargahydroquinoic acid analogs was evaluated through in vitro anti-inflammatory activity, anti-oxidant activity, cytotoxicity against HT-29 and Caco-2 colorectal cancer cells, and PPAR-γ activation. Results: Sargahydroquinoic acid acts on various therapeutic targets relevant to IBD treatment. Conclusions: Conversion of sargahydroquinoic acid to sarganaphthoquinoic acid increases peroxisome proliferator activated receptor gamma (PPAR-γ) activity, compromises anti-oxidant activity, and has no effect on cytotoxicity against the tested cell lines.

Peroxisome Proliferator-Activated Receptors: Experimental Targeting for the Treatment of Inflammatory Bowel Diseases

“…In this way, recent studies in DSS-induced colitis mice have shown the ability of natural compounds, such as magnolol, an active ingredient of Magnolia officinalis (Shen et al, 2018), and Portulaca oleracea extract (Kong et al, 2018), from traditional Chinese medicine, to counteract the expression of cytokines, such as TNF-a, IL-1b, and IL-12, via the regulation of NF-kB and PPARg pathways. Another natural compound, Sargahydroquinoic acid isolated from Sargassum incisifolium, and its semisynthetic derivatives have shown agonist activity of PPARg in in vitro assays (Nyambe et al, 2019). In addition, it presented dual anti-inflammatory and antioxidant effects when evaluated through in vitro cytotoxicity against HT-29 adenocarcinoma and Caco-2 colorectal cancer cells lines in addition to PPARg activation.…”

Cytotoxic, Cellular Antioxidant, and Antiglucuronidase Properties of the Ethanol Leaf Extract from Bulbine asphodeloides

“…Anti-Inflammatory Assay. Anti-inflammatory activity was performed as previously reported [18]. e murine peritoneal macrophage cells (RAW 267.4) were seeded in a 96-well plate at a density of 1 × 10 5 cells per well and allowed to attach overnight.…”

The effect of 1-deoxynojirimycin isolated from logging residue of Bagassa guianensis on an in vitro cancer model

“…This study zeroes in on 1-DNJ extracted from Tatajuba's timber waste, exploring its potential anticancer effects. Previous research has established 1-DNJ's antioxidant and anti-inflammatory capabilities, suggesting its suitability for anticancer therapy (Naik et al, 2015;George et al, 2017;Nyambe et al, 2019). For example, Morus nigra extract, rich in 1-DNJ, has been shown to have such effects and to inhibit carcinogenesis in prostate cancer models and prevent gastric ulcers in mice (Yatsunami et al, 2008;Turan et al, 2017;Piao et al, 2018).…”