Molecular Targets Modulated by Fangchinoline in Tumor Cells and Preclinical Models

Mérarchi, Myriam; Sethi, Gautam; Fan, Li; Mishra, Srishti; Arfuso, Frank; Ahn, Kwang Seok

doi:10.3390/molecules23102538

Cited by 36 publications

(29 citation statements)

References 81 publications

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“…Interestingly, the anti-metastatic activity of fangchinoline in human gastric cancer cells was also found to implicate the suppression of MMP-2 and MMP-9, increase of TIMP1 and TIMP2 genes, and inhibition of AKT phosphorylation . Fangchinoline inhibits metastasis and migration of melanoma and glioma cells in vitro, as well as it suppresses in a dose-dependent manner the adhesion, migration, and invasion human gastric cancer cells (Mérarchi et al, 2018). Tetrandrine inhibits hepatocellular carcinoma cell invasion and migration by repressing the autophagy-dependent Wnt/β-catenin and metastatic tumor antigen 1 (MTA1) signaling pathways .…”

Section: Inhibition Of Cell Migration -Anti-metastatic and Antiatheromentioning

confidence: 99%

Cepharanthine: An update of its mode of action, pharmacological properties and medical applications

2019

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A B S T R A C TBackground: Cepharanthine (CEP) is a drug used in Japan since the 1950s to treat a number of acute and chronic diseases, including treatment of leukopenia, snake bites, xerostomia and alopecia. It is the only approved drug for Human use in the large class of bisbenzylisoquinoline alkaloids. This natural product, mainly isolated from the plant Stephania cephalantha Hayata, exhibits multiple pharmacological properties including anti-oxidative, anti-inflammatory, immuno-regulatory, anti-cancer, anti-viral and anti-parasitic properties. Purpose: The mechanism of action of CEP is multifactorial. The drug exerts membrane effects (modulation of efflux pumps, membrane rigidification) as well as different intracellular and nuclear effects. CEP interferes with several metabolic axes, primarily with the AMP-activated protein kinase (AMPK) and NFκB signaling pathways. In particular, the anti-inflammatory effects of CEP rely on AMPK activation and NFκB inhibition. Conclusion: In this review, the historical discovery and development of CEP are retraced, and the key mediators involved in its mode of action are presented. The past, present, and future of CEP are recapitulated. This review also suggests new opportunities to extend the clinical applications of this well-tolerated old Japanese drug.

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Section: Inhibition Of Cell Migration -Anti-metastatic and Antiatheromentioning

confidence: 99%

Cepharanthine: An update of its mode of action, pharmacological properties and medical applications

2019

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“…There has been considerable interest in the use of dietary compounds for various cancer prevention and therapy approaches [1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16]. Furanocoumarins are natural plant constituents present in many types of plants belonging to the Rutaceae and Umbelliferae families.…”

Section: Introductionmentioning

confidence: 99%

Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy

Arfuso

Sethi

et al. 2018

IJMS

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Cancer still remains one of the leading causes of death worldwide. In spite of significant advances in treatment options and the advent of novel targeted therapies, there still remains an unmet need for the identification of novel pharmacological agents for cancer therapy. This has led to several studies evaluating the possible application of natural agents found in vegetables, fruits, or plant-derived products that may be useful for cancer treatment. Bergamottin is a furanocoumarin derived from grapefruits and is also a well-known cytochrome P450 inhibitor. Recent studies have demonstrated potent anti-oxidative, anti-inflammatory, and anti-cancer properties of grapefruit furanocoumarin both in vitro and in vivo. The present review focuses on the potential anti-neoplastic effects of bergamottin in different tumor models and briefly describes the molecular targets affected by this agent.

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“…Fangchinoline, a bisbenzylisoquinoline alkaloid, can be obtained from the roots of Stephaniae tetrandra . The compound has been mainly showed to have anti-cancer effects such as preventing the proliferation and metastasis of malignant cells as well as promoting autophagy and apoptosis in tumor cells ( Mérarchi et al ., 2018 ). However, there are hardly any studies involving FAN and arthritis.…”

Section: Discussionmentioning

confidence: 99%

Fangchinoline Has an Anti-Arthritic Effect in Two Animal Models and in IL-1β-Stimulated Human FLS Cells

Villa

Kim

2020

Biomolecules & Therapeutics

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Fangchinoline (FAN) is a bisbenzylisoquinoline alkaloid that is widely known for its anti-tumor properties. The goal of this study is to examine the effects of FAN on arthritis and the possible pathways it acts on. Human fibroblast-like synovial cells (FLS), carrageenan/kaolin arthritis rat model (C/K), and collagen-induced arthritis (CIA) mice model were used to establish the efficiency of FAN in arthritis. Human FLS cells were treated with FAN (1, 2.5, 5, 10 μM) 1 h before IL-1β (10 ng/mL) stimulation. Cell viability, reactive oxygen species measurement, and western blot analysis of inflammatory mediators and the MAPK and NF-κB pathways were performed. In the animal models, after induction of arthritis, the rodents were given 10 and 30 mg/kg of FAN orally 1 h before conducting behavioral experiments such as weight distribution ratio, knee thickness measurement, squeaking score, body weight measurement, paw volume measurement, and arthritis index measurement. Rodent knee joints were also analyzed histologically through H&E staining and safranin staining. FAN decreased the production of inflammatory cytokines and ROS in human FLS cells as well as the phosphorylation of the MAPK pathway and NF-κB pathway in human FLS cells. The behavioral parameters in the C/K rat model and CIA mouse model and inflammatory signs in the histological analysis were found to be ameliorated in FAN-treated groups. Cartilage degradation in CIA mice knee joints were shown to have been suppressed by FAN. These findings suggest that fangchinoline has the potential to be a therapeutic source for the treatment of rheumatoid arthritis.

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Molecular Targets Modulated by Fangchinoline in Tumor Cells and Preclinical Models

Cited by 36 publications

References 81 publications

Cepharanthine: An update of its mode of action, pharmacological properties and medical applications

Cepharanthine: An update of its mode of action, pharmacological properties and medical applications

Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy

Fangchinoline Has an Anti-Arthritic Effect in Two Animal Models and in IL-1β-Stimulated Human FLS Cells

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