Guggulsterone for Chemoprevention of Cancer

Shishodia, Shishir; Azu, Nkem O.; Rosenzweig, Jason A.; Jackson, Desiree A.

doi:10.2174/1381612822666151112153117

Cited by 33 publications

(19 citation statements)

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“…Thus, a critical evaluation of the binding interaction of ligands with GR was done and suggested that boswellic acid and withaferin A displayed better binding modes with GR compared with the other tested ligands, where withaferin A interacted with two active site amino acids similar to those that fluticasone interacted with and boswellic acid interacted with three active site amino acid residues, which was even better than fluticasone. Previous in silico and/or in vitro studies suggested that these plant steroids might interact with GR, including glycyrrhetinic acid [22], guggulsterone [23], boswellic acid [24], withaferin A [25], and diosgenin [26]. However, none of the previous studies compared more than one plant steroids or referred their effect to a standard GR ligand as fluticasone.…”

Section: Discussionmentioning

confidence: 99%

Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor

Morsy

Patel

El-Sheikh

et al. 2019

Mediators of Inflammation

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Despite the usefulness of glucocorticoids, they may cause hazardous side effects that limit their use. Searching for compounds that are as equally efficient as glucocorticoids, but with less side effects, the current study compared plant steroids, namely, glycyrrhetinic acid, guggulsterone, boswellic acid, withaferin A, and diosgenin with the classical glucocorticoid, fluticasone. This was approached both in silico using molecular docking against glucocorticoid receptor (GR) and in vivo in two different animal models. All tested compounds interacted with GR, but only boswellic acid and withaferin A showed docking results comparable to fluticasone, as well as similar in vivo anti-inflammatory effects, by significantly decreasing serum levels of interleukin-6 and tumor necrosis factor-α in cotton pellet-induced granuloma in rats. In addition, both compounds significantly decreased the percent of change in ear weight in croton oil-induced ear edema in mice and the granuloma weight in cotton pellet-induced granuloma in rats, to levels comparable to that of fluticasone. Both boswellic acid and withaferin A had no effect on adrenal index, but only withaferin A significantly increased the thymus index. In conclusion, boswellic acid may have comparable anti-inflammatory effects to fluticasone with fewer side effects.

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Section: Discussionmentioning

confidence: 99%

Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor

Morsy

Patel

El-Sheikh

et al. 2019

Mediators of Inflammation

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“…ex Stocks) Engl.). Guggulsterone is broadly utilized in Indian traditional medicine for the management of various diseases, including cancer [247][248][249]. It suppressed U266 cell proliferation by inducing apoptosis and cell cycle arrest at the sub-G 1 phase.…”

Section: Guggulsteronementioning

confidence: 99%

Targeting the JAK/STAT Signaling Pathway Using Phytocompounds for Cancer Prevention and Therapy

Bose¹,

Banerjee²,

Mondal³

et al. 2020

Cells

132

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Cancer is a prevalent cause of mortality around the world. Aberrated activation of Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling pathway promotes tumorigenesis. Natural agents, including phytochemicals, exhibit potent anticancer activities via various mechanisms. However, the therapeutic potency of phytoconstituents as inhibitors of JAK/STAT signaling against cancer has only come into focus in recent days. The current review highlights phytochemicals that can suppress the JAK/STAT pathway in order to impede cancer cell growth. Various databases, such as PubMed, ScienceDirect, Web of Science, SpringerLink, Scopus, and Google Scholar, were searched using relevant keywords. Once the authors were in agreement regarding the suitability of a study, a full-length form of the relevant article was obtained, and the information was gathered and cited. All the complete articles that were incorporated after the literature collection rejection criteria were applied were perused in-depth and material was extracted based on the importance, relevance, and advancement of the apprehending of the JAK/STAT pathway and their relation to phytochemicals. Based on the critical and comprehensive analysis of literature presented in this review, phytochemicals from diverse plant origins exert therapeutic and cancer preventive effects, at least in part, through regulation of the JAK/STAT pathway. Nevertheless, more preclinical and clinical research is necessary to completely comprehend the capability of modulating JAK/STAT signaling to achieve efficient cancer control and treatment.

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“…FXR antagonists are numerous and are both natural and synthetic [31]. Guggulsterone is a vegetal sterol derived from the resin of an Asian tree Commiphora wightii and has been consumed in traditional medicine for centuries to treat obesity, liver disorders and a large panel of tumors [45]. This molecule is often used in preclinical in vitro and in vivo studies and showed a decrease of FXR activity and the tumor size [46].…”

Section: Discussionmentioning

confidence: 99%

Farnesoid X receptor as marker of osteotropism of breast cancers through its role in the osteomimetism of tumor cells

et al. 2020

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Background: The skeleton is the first and most common distant metastatic site for breast cancer. Such metastases complicate cancer management, inducing considerable morbidities and decreasing patient survival. Osteomimetism is part of the complex process of osteotropism of breast cancer cells. Recent data indicate that Farnesoid X Receptor (FXR) is involved in the transformation and progression of breast cancer. Methods: The expression of FXR, Runt-related transcription factor 2 (RUNX2) and bone proteins were evaluated on two tumor cell lines (MCF-7 and MDA-MB-231) by immunohistochemistry, immunofluorescence and western blotting and quantified. Results: In a series of 81 breast cancer patients who developed distant metastases, we found a strong correlation between FXR expression in primary breast tumors and the development of bone metastases, especially in patients with histological grade 3 tumors. In in vitro studies, FXR activation by Chenodeoxycholic acid (CDCA) increased the expression of numerous bone proteins. FXR inhibition by lithocholic acid and z-guggulsterone decreased bone protein expression. Short Hairpin RNA (ShRNA) against FXR validated the involvement of FXR in the osteomimetism of breast cancer cells. Conclusion: Our experimental results point to a relationship between the expression of FXR in breast cancer cells and the propensity of these tumor cells to develop bone metastases. FXR induces the expression of RUNX2 which itself causes the synthesis of bone proteins by tumor cells.

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Guggulsterone for Chemoprevention of Cancer

Cited by 33 publications

References 0 publications

Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor

Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor

Targeting the JAK/STAT Signaling Pathway Using Phytocompounds for Cancer Prevention and Therapy

Farnesoid X receptor as marker of osteotropism of breast cancers through its role in the osteomimetism of tumor cells

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