Prenylated flavonoid morusin protects against TNBS-induced colitis in rats

Vochyánová, Zora; Pokorná, Marie; Rotrekl, Dominik; Smékal, Václav; Fictum, P.; Suchý, Pavel; Gajdziok, Jan; Šmejkal, Karel; Hošek, Jan

doi:10.1371/journal.pone.0182464

Cited by 37 publications

(20 citation statements)

References 30 publications

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“…The inhibition of the matrix metalloproteinases gelatinases (MMP-2 and MMP-9) by morusin has also been described in literature. 20,24,25 Also, there is an elevation of these MMPs in colorectal cancer, pancreatic cancer, ovarian cancer and breast cancer as discussed previously. Thus, in order to check whether there was any interaction between morusin and MMPs, we performed molecular docking studies using Autodock tool.…”

Section: Docking Studiesmentioning

confidence: 79%

“…[22][23][24] In addition, morusin is also known to inhibit the expression of metalloproteinases (MMP-2 and MMP-9), which are elevated in the tumor microenvironment. 24,25 These evidences though support morusin as an effective natural anticancer drug; its full potential has not been explored mainly due to its poor aqueous solubility and bioavailability. Hydrophobicity of therapeutic moieties is a major issue in drug formulations, which results in rapid clearance by the reticuloendothelial system (RES) and poor bioavailability, restricting their full clinical potential.…”

Section: Introductionmentioning

confidence: 99%

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Formulation, characterization and evaluation of morusin loaded niosomes for potentiation of anticancer therapy

et al. 2018

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Morusin, a water-insoluble prenylated flavonoid is known for its numerous medicinal properties. It manifests its anticancer potential by suppression of genes involved in tumor progression. However, poor solubility of the drug results in low bioavailability and rapid degradation thus hindering its clinical utilization. In order to overcome this, we have synthesized a niosome system composed of non-ionic surfactant span 60 and cholesterol using a thin-layer evaporation technique to improve the aqueousphase solubility of the drug. Highly cytocompatible niosomes of 479 nm average size with smooth and uniform spherical morphology were synthesized in a facile manner. Unlike free morusin, nanomorusin was found to be freely dispersible in aqueous media. Having an extremely high drug entrapment efficiency (97%), controlled and sustained release of morusin resulting in enhanced therapeutic efficacy was observed in cancer cell lines of 4 different lineages. The results demonstrate that the morusinniosome system is a promising strategy for enhanced anti-cancer activity against multiple cancer types and could be an indispensable tool for future targeted chemotherapeutic strategies.

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Section: Docking Studiesmentioning

confidence: 79%

Section: Introductionmentioning

confidence: 99%

Formulation, characterization and evaluation of morusin loaded niosomes for potentiation of anticancer therapy

et al. 2018

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“…Soonthornsit et al reported that oxyresveratrol at concentrations of 5 and 10 μg/mL inhibited LPS-induced nitrite production and the expression of iNOS and COX-2 [12]. Morusin, a prenylated flavonoid, potentially has neuroprotective, anticancer, antioxidative, and ant-colitis activities [21][22][23][24]. In this study, the anti-inflammatory effect of ethanol extract from the dried root of M. australis (MRE) was evaluated in vitro and in vivo.…”

Section: Discussionmentioning

confidence: 94%

Protective Effects of Morus Root Extract (MRE) Against Lipopolysaccharide-Activated RAW264.7 Cells and CCl4-Induced Mouse Hepatic Damage

Tseng

Lin

Chang

et al. 2018

Cell Physiol Biochem

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Background/Aims: Inflammation is one of the main contributors to chronic diseases such as cancer. It is of great value to identify the potential activity of various medicinal plants for regulating or blocking uncontrolled chronic inflammation. We investigated whether the root extract of Morus australis possesses antiinflammatory and antioxidative stress potential and hepatic protective activity. Methods: The microwave-assisted extractionwere was used to prepare the ethanol extract from the dried root of Morus australis (MRE), including polyphenolic and flavonoid contents. Lipopolysaccharide (LPS)-stimulated RAW264.7 cells was examined the anti-inflammatory and anti-oxidative potential of MRE. CCl₄-induced mouse hepatic damage were performed to detect the hepatic protective potential in vivo. Immunohistochemistry (IHC) and western blot assays were used to detect target proteins. Results: MRE contained approximately 23% phenolic compounds and 3% flavonoids. The major flavonoid component of MRE was morusin. MRE and morusin inhibited lipopolysaccharide-induced production of nitrite and prostaglandin E2 in RAW264.7 cells. MRE and morusin also suppressed the formation of intracellular reactive oxygen species and the expression of iNOS and COX-2. In an in vivo study, a thiobarbituric acid reactive substances assay showed that MRE inhibited CCl₄-induced oxidative stress and expression of nitrotyrosine. MRE also decreased CCl₄-induced hepatic iNOS and COX-2 expression, as well as CCl₄-induced hepatic inflammation and necrosis in mice. Conclusion: MRE exhibited antiinflammatory and hepatic protective activity.

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“…Microscopic assessment criteria are as follows: the severity of inflammation was graded as 0-3 for the extent of inflammation (mucosa, submucosa, and transmural layers) and 0-4 for crypt damage. Then the three parts would be added up to make a total score [ 22 , 23 ].…”

Section: Methodsmentioning

confidence: 99%

Tou Nong San Attenuates Inflammation in TNBS‐IBD Model by Inhibiting NF‐κB Signaling Pathway

Yang

et al. 2018

Evidence-Based Complementary and Alternative Medicine

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The incidence of inflammatory bowel disease (IBD), which predominantly comprises Crohn's disease and ulcerative colitis, is increasing worldwide. However, the treatment of IBD still faces great challenges. The involved NF-κB is the main signaling pathway in human IBD and thus is a prime target. There is abundant evidence that Tou Nong San (TNS), which is a traditional Chinese medicinal decoction used for treating sores and carbuncles, has a positive effect on the inflammation. This study investigated the effects of oral administration of TNS on colitis induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) and the underlying mechanism(s). Quality control of the major compounds in TNS was performed by high-performance liquid chromatography, and six chemical constituents were identified in aqueous extracts. TNS led to improvements in weight loss and water and food intake in rats. The macroscopic and microscopic scores of rat tissues greatly decreased. Protein and mRNA levels of proinflammatory cytokines, including interleukin-17 (IL-17), tumour necrosis factor-α, IL-1β, and IL6, involved in the NF-κB signaling pathway were greatly reduced. The results suggest that the anti-inflammatory effect of TNS is associated with the regulation of the NF-κB signaling pathway, which contributes to the network pharmacological effect of TNS on human IBD in clinical practice.

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Prenylated flavonoid morusin protects against TNBS-induced colitis in rats

Cited by 37 publications

References 30 publications

Formulation, characterization and evaluation of morusin loaded niosomes for potentiation of anticancer therapy

Formulation, characterization and evaluation of morusin loaded niosomes for potentiation of anticancer therapy

Protective Effects of Morus Root Extract (MRE) Against Lipopolysaccharide-Activated RAW264.7 Cells and CCl4-Induced Mouse Hepatic Damage

Tou Nong San Attenuates Inflammation in TNBS‐IBD Model by Inhibiting NF‐κB Signaling Pathway

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