Ulcerative colitis (UC) is an inflammation of the colon that can progress to colorectal cancer if left untreated. No medication completely cures UC and natural products are sources of alternative approaches. This study aimed to determine the anti-inflammatory potential of Phyllanthus nivosus leaf extract and fractions in a rat model of ulcerative colitis and to identify the active ingredients. UC was induced in rats by intra-rectal infusion of 1ml of 4% acetic acid (AA) in normal saline. AA exposed groups of rats were treated with 100 mg/kg bodyweight of methanol extract, hexane, ethyl-acetate and butanol fractions orally for four days. Another group received the standard drug -Dexamethasone and control rats were given distilled water only. Some biochemical changes were evaluated and the active ingredients were identified using Gas Chromatography-Mass Spectrometry (GC-MS) followed by molecular docking against interleukin-1-beta converting enzyme (Caspase-1), beta-2 adrenergic receptor (ADRB2), cyclooxygenase-2 (COX-2) and tumour necrosis factor-alpha (TNF-α). Exposure of rat colon to acetic acid significantly altered (p < 0.05) serum levels of tumour necrosis factor-alpha (TNF-α), interleukin -6 (IL-6), nitric oxide (NO), lipid peroxidation product (malondialdehyde or MDA), reduced glutathione (GSH); and activities of superoxide dismutase (SOD) and catalase (CAT). These alterations were however restored in the rats treated with P. nivosus leaf with the ethyl-acetate fraction displaying the highest ameliorative activity. GC-MS analysis of the ethyl acetate fraction revealed the presence of 40 compounds which when subjected to molecular docking demonstrated varying degrees of binding affinities for the protein targets. Ethyl iso-allocholate demonstrated the highest binding affinity for caspase-1, cholest-22-ene-21-ol, 3,5-dehydro-6-methoxy-, pivalate for ADRB2 and TNF-α; and alpha-cadinol for COX-2. The anti-inflammatory potential of Phyllanthus nivosus leaf as a natural remedy and as a source of new drugs against ulcerative colitis is validated.
Aim: The aim of this study was to investigate and compare the antioxidative properties of the mistletoe plant obtained from three different host species namely Psidium guajava, Vernonia amygdalina and Moringa olifera lam. Study Design: Experimental Design Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences and Department of Biochemistry, College of Health Sciences, University of Jos, Nigeria. Methodology: Crude methanolic leaf extracts were studied for their antioxidative properties; Iron reducing and Iron-chelating activities, Nitric oxide (NO) radical and 2,2-diphenyl 1-picrylhydrazyl (DPPH) radical scavenging activities and the lipid peroxidation and thiobarbituric acid reaction (TBAR) methods. One way ANOVA was used for the result analysis with P<.05 for significant difference. Results: Mistletoes from Psidum guajava (MSPG) had significantly higher reducing property (0.16 – 0.20mg/mL); the chelating property of Mistletoes from Moringa olifera (MSMO) was significantly lower (45.7 – 58.9%); DPPH radical scavenging activity had no significant difference; and Nitric oxide scavenging activity was significantly higher in MSPG (72.1% in 75mg/mL) than the extracts from other hosts. MSPG had significantly higher TBAR inhibition using both FeSO4 (77.8% at 125µg/mL) and Sodium nitroprusside (61.6+1.0% at 125µg/mL) with an IC50 of 30.27µg/mL . Extract of Tapinanthus globiferus leaves from Psidium guajava had more antioxidative activities in the TBARs followed by Tapinanthus globiferus leaf extract from Vernonia amygdalina (MSVA). Conclusion: From the study, mistletoes from Psidium guajava had higher antioxidant activity compared to other hosts, which probably justifies its use for treatment of cancer in traditional medicinal practice.
Inflammatory bowel diseases (IBDs) comprising ulcerative colitis, Crohn’s disease and microscopic colitis are characterized by chronic inflammation of the gastrointestinal tract. IBD has spread around the world and is becoming more prevalent at an alarming rate in developing countries whose societies have become more westernized. Cell therapy, intestinal microecology, apheresis therapy, exosome therapy and small molecules are emerging therapeutic options for IBD. Currently, it is thought that low-molecular-mass substances with good oral bio-availability and the ability to permeate the cell membrane to regulate the action of elements of the inflammatory signaling pathway are effective therapeutic options for the treatment of IBD. Several small molecule inhibitors are being developed as a promising alternative for IBD therapy. The use of highly efficient and time-saving techniques, such as computational methods, is still a viable option for the development of these small molecule drugs. The computer-aided ( in silico ) discovery approach is one drug development technique that has mostly proven efficacy. Computational approaches when combined with traditional drug development methodology dramatically boost the likelihood of drug discovery in a sustainable and cost-effective manner. This review focuses on the modern drug discovery approaches for the design of novel IBD drugs with an emphasis on the role of computational methods. Some computational approaches to IBD genomic studies, target identification, and virtual screening for the discovery of new drugs and in the repurposing of existing drugs are discussed.
Over the years research findings have shown that free radicals are the basis for many diseases. This study sought to investigate the free radical scavenging and inhibition of lipid peroxidation activities of some three Northern Nigerian plant leaf; Boswellia dalzielii Hutch. (Burseraceae) (BDL), Detarium microcarpum Guill. and Perr. (DML), and Daniellia oliveiri (Rolfe) Hutch. & Dalz (DOL). The study investigated both qualitative and quantitative phytochemical screening, free radical scavenging activities of 1, 1-diphenyl-2-picrylhydrazyl DPPH, total antioxidant capacity ABTS, hydroxyl, reducing property and inhibition of lipid peroxidation. All the seven phytochemicals screened were all present in both BDL and DML plant extracts but saponins and glycosides were absent in DOL plant leaf. The result revealed that BDL methanolic extract had the highest total flavonoid and phenolic content while BDL methanolic extract had the highest alkaloid content. DOL methanolic extract had the least content in all the 3 phytochemicals quantified. BDL methanolic extract had the highest free radical scavenging activity in 1, 1-diphenyl-2-picrylhydrazyl (DPPH), Hydroxyl and reducing power assays. While DML methanolic extract, had the highest free radical scavenging ability in 2, 2-azino-bis(3-ethylbenzazoline-6-sulphonic acid (TEAC) assays. The IC50 of BDL extract (12.37 mg/mL) was not significantly different (p > 0.05) from DML extract (10.39 mg/mL) in the Fe 2+-induced lipid peroxidation assay. While, the IC50 of DML extract (14.83 mg/mL) was significantly higher (p < 0.05) than the BDL extract (19.92 mg/mL) in the SNP-induced lipid peroxidation. The DOL extract had the least scavenging and peroxidative inhibitory activity in all the assays carried out. We therefore concluded that the synergistic free radical scavenging activities and inhibition of lipid peroxidation of the three plants studied (especially, BDL and DML), provides a biochemical rationale for their usage as a medicinal plant.
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