Cancer Chemopreventive and Therapeutic Potential of Guggulsterone

Almazari, Inas; Surh, Young‐Joon

doi:10.1007/128_2012_344

Cited by 9 publications

(5 citation statements)

References 119 publications

(191 reference statements)

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“…The exact mechanisms involved in the phytosterol-mediated protection against cancer are still poorly defined. Different potential anticancer mechanisms have been proposed, including those involving the inhibition of carcinogen production, cancer cell proliferation, invasion, and metastasis, as well as the induction of cell cycle arrest and apoptosis (reviewed in (3,4,22,66), thus conferring cancer chemopreventive and therapeutic potential. Apart from these, other mechanisms including the reduction of angiogenesis, invasion, and adhesion of cancer cells have been also suggested (Figure 1).…”

Section: Potential Cellular Mechanisms Of Anticancer Actionmentioning

confidence: 99%

“…The administration of another main phytosterol, campesterol, has been shown to prevent bFGF-induced endothelial cell proliferation and capillary-like tube formation as well as neovascularization in fertilized eggs (92). Guggulsterone has been recently reported to suppress capillary tube formation and the migration of endothelial vascular cells as well as matrix metalloproteinases release from the colon cancer cells (66). The anti-angiogenic activity of phytosterols, as one of the components of a dietary phytochemical conjugate, has been also demonstrated in vivo using a murine Lewis lung cancer model (93).…”

Section: Effect On Angiogenesismentioning

confidence: 99%

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Phytosterols in Cancer: From Molecular Mechanisms to Preventive and Therapeutic Potentials

Blanco‐Vaca

Cedó

Julve

2019

CMC

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Cancer is the second leading cause of death worldwide. Compelling evidence supports the hypothesis that the manipulation of dietary components, including plant compounds termed phytochemicals, demonstrates certain important health benefits in humans, including those in cancer. In fact, beyond their well-known cardiovascular applications, phytosterols may also possess anticancer properties, as has been demonstrated by several studies. Although the mechanism of action by which phytosterols (and derivatives) may prevent cancer development is still under investigation, data from multiple experimental studies support the hypothesis that they may modulate proliferation and apoptosis of tumor cells. Phytosterols are generally considered safe for human consumption and may also be added to a broad spectrum of food matrices; further, they could be used in primary and secondary prevention. However, few interventional studies have evaluated the relationship between the efficacy of different types and forms of phytosterols in cancer prevention. In this context, the purpose of this review was to revisit and update the current knowledge on the molecular mechanisms involved in the anticancer action of phytosterols and their potential in cancer prevention or treatment.

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Section: Potential Cellular Mechanisms Of Anticancer Actionmentioning

confidence: 99%

Section: Effect On Angiogenesismentioning

confidence: 99%

Phytosterols in Cancer: From Molecular Mechanisms to Preventive and Therapeutic Potentials

Blanco‐Vaca

Cedó

Julve

2019

CMC

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“…The crude ethyl acetate extract of gum guggul has been shown to suppress inflammatory mediators such as IFN-γ, IL-12, TNF-α and IL-1β. Recently, Guggulsterone E and Guggulsterone Z the active components from the gum guggul has been shown to exhibit anti-inflammatory activities by suppressing cytokines expression [107, 108] and inhibit tumor growth both in vitro and in vivo by modulating numerous survival and proapototic signaling cascades [107]. By affecting growth factors, growth factor receptors and several transcription factors implicated in inflammation like NF-κB, STAT1/3, C/EBPα, androgen and glucocorticoid receptors, guggulsterone (GS) modulates the expression of antiapoptotic proteins (IAP1, XIAP, Bcl-2, cFLIP, survivin), inhibits cell survival, cell proliferation associated proteins (cyclin D1, c-Myc), abrogates angiogenesis, and metastasis (MMP-9, COX-2, VEGF) in tumor cells [107].…”

Section: Natural Products Modulating Mucin Expression: Potential Thermentioning

confidence: 99%

Emerging potential of natural products for targeting mucins for therapy against inflammation and cancer

Macha

Krishn

Jahan

et al. 2015

Cancer Treatment Reviews

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Deregulated mucin expression is a hallmark of several inflammatory and malignant pathologies. Emerging evidence suggests that, apart from biomarkers, these deregulated mucins are functional contributors to pathogenesis in inflammation and cancer. Both overexpression and downregulation of mucins in various organ systems is associated with pathobiology of inflammation and cancer. Restoration of mucin homeostasis has become an important goal for therapy and management of such disorders and has fueled the quest for selective mucomodulators. With improved understanding of mucin regulation and mechanistic insights into their pathobiological roles, there is optimism to find selective non-toxic agents capable of modulating mucin expression and function. Recently, natural compounds derived from dietary sources have drawn attention due to their anti-inflammatory and anti-oxidant properties and low toxicity. Considerable efforts have been directed towards evaluating dietary natural products as chemopreventive and therapeutic agents; identification, characterization and synthesis of their active compounds; and improving their delivery and bioavailability. We describe the current understanding of mucin regulation, rationale for targeting mucins with natural products and discuss some natural products that modulate mucin expression and functions. We further discuss the approaches and parameters that should guide future research to identify and evaluate selective natural mucomodulators for therapy.

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“…The therapeutic benefits of C. wightii have been reported in the treatment of various diseases including tumors, malignant sores, ulcers, obesity, and liver and intestinal problems; hence, it has been widely used in Ayurveda for thousands of years [ 57 ]. Besides, GS has also gained importance due to its chemopreventive and therapeutic properties against various cancers and their hallmarks [ 63 , 64 ]. This plant metabolite was first recognized as an antagonist for the nuclear receptor, farnesoid X receptor (FXR) [ 57 ].…”

Section: Introductionmentioning

confidence: 99%

Potential of guggulsterone, a farnesoid X receptor antagonist, in the prevention and treatment of cancer

Girisa

Dey

Harsha

et al. 2020

Exploration of Targeted Anti-Tumor Therapy

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Cancer is one of the most dreadful diseases in the world with a mortality of 9.6 million annually. Despite the advances in diagnosis and treatment during the last couple of decades, it still remains a serious concern due to the limitations associated with currently available cancer management strategies. Therefore, alternative strategies are highly required to overcome these glitches. The importance of medicinal plants as primary healthcare has been well-known from time immemorial against various human diseases, including cancer. Commiphora wightii that belongs to Burseraceae family is one such plant which has been used to cure various ailments in traditional systems of medicine. This plant has diverse pharmacological properties such as antioxidant, antibacterial, antimutagenic, and antitumor which mostly owes to the presence of its active compound guggulsterone (GS) that exists in the form of Z- and E-isomers. Mounting evidence suggests that this compound has promising anticancer activities and was shown to suppress several cancer signaling pathways such as NF-κB/ERK/MAPK/AKT/STAT and modulate the expression of numerous signaling molecules such as the farnesoid X receptor, cyclin D1, survivin, caspases, HIF-1α, MMP-9, EMT proteins, tumor suppressor proteins, angiogenic proteins, and apoptotic proteins. The current review is an attempt to summarize the biological activities and diverse anticancer activities (both in vitro and in vivo) of the compound GS and its derivatives, along with its associated mechanism against various cancers.

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Cancer Chemopreventive and Therapeutic Potential of Guggulsterone

Cited by 9 publications

References 119 publications

Phytosterols in Cancer: From Molecular Mechanisms to Preventive and Therapeutic Potentials

Phytosterols in Cancer: From Molecular Mechanisms to Preventive and Therapeutic Potentials

Emerging potential of natural products for targeting mucins for therapy against inflammation and cancer

Potential of guggulsterone, a farnesoid X receptor antagonist, in the prevention and treatment of cancer

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