Phytochemicals for the Management of Melanoma

Pal, Harish C.; Hunt, Katherine M.; Diamond, Ariana C.; Elmets, Craig A.; Afaq, Farrukh

doi:10.2174/1389557516666160211120157

Cited by 63 publications

(49 citation statements)

References 313 publications

(343 reference statements)

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“…The flavone apigenin is another phytoestrogen that received growing attention as a potential chemopreventive agent and suppressor of cancer growth (155, 179–182). In A375 human melanoma cells, apigenin was reported to induce apoptosis through accumulation of reactive oxygen species in mitochondria, upregulation of Bax, caspase 3, 9, and PARP and downregulation of Bcl-2, thus triggering the mitochondrial apoptotic pathway (183).…”

Section: Natural Erβ Ligands and Melanomamentioning

confidence: 99%

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

et al. 2016

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Cutaneous melanoma is an aggressive tumor; its incidence has been reported to increase fast in the past decades. Melanoma is a heterogeneous tumor, with most patients harboring mutations in the BRAF or NRAS oncogenes, leading to the overactivation of the MAPK/ERK and PI3K/Akt pathways. The current therapeutic approaches are based on therapies targeting mutated BRAF and the downstream pathway, and on monoclonal antibodies against the immune checkpoint blockade. However, treatment resistance and side effects are common events of these therapeutic strategies. Increasing evidence supports that melanoma is a hormone-related cancer. Melanoma incidence is higher in males than in females, and females have a significant survival advantage over men. Estrogens exert their effects through estrogen receptors (ERα and ERβ) that affect cancer growth in an opposite way: ERα is associated with a proliferative action and ERβ with an anticancer effect. ERβ is the predominant ER in melanoma, and its expression decreases in melanoma progression, supporting its role as a tumor suppressor. Thus, ERβ is now considered as an effective molecular target for melanoma treatment. 17β-estradiol was reported to inhibit melanoma cells proliferation; however, clinical trials did not provide the expected survival benefits. In vitro studies demonstrate that ERβ ligands inhibit the proliferation of melanoma cells harboring the NRAS (but not the BRAF) mutation, suggesting that ERβ activation might impair melanoma development through the inhibition of the PI3K/Akt pathway. These data suggest that ERβ agonists might be considered as an effective treatment strategy, in combination with MAPK inhibitors, for NRAS mutant melanomas. In an era of personalized medicine, pretreatment evaluation of the expression of ER isoforms together with the concurrent oncogenic mutations should be considered before selecting the most appropriate therapeutic intervention. Natural compounds that specifically bind to ERβ have been identified. These phytoestrogens decrease the proliferation of melanoma cells. Importantly, these effects are unrelated to the oncogenic mutations of melanomas, suggesting that, in addition to their ERβ activating function, these compounds might impair melanoma development through additional mechanisms. A better identification of the role of ERβ in melanoma development will help increase the therapeutic options for this aggressive pathology.

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Section: Natural Erβ Ligands and Melanomamentioning

confidence: 99%

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

et al. 2016

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“…It is known from the earlier report that the photophysical properties of PRO are dependent on the surrounding local environment. [30,31] Fluorescence of PRO originates from locally excited (LE) Franck-Condon state and an ICT excited state in which electron density is transferred from the electrondonating -NMe 2 group to the electron-accepting carbonyl group at 6-position of naphthalene unit (see Figure 1 for the charge transfer process). [28,31] It is also well established that the emission from PRO comes from LE state, which does not get much influenced by the surrounding environment.…”

Section: Resultsmentioning

confidence: 99%

“…[33] Further, a new emission band (~435 nm) was observed, which was very different from both the LE and CT emission. [28,30] Most of the earlier reports either believed that the new fluorescent maximum was originated from synthetic impurity or was actually developed due to the aggregation of PRO only after a certain concentration. [34][35][36] This drastically different emission maximum from the aggregated PRO is only observable in "bad" solvents like water (at pH 9.0) above a concentration of 10 mM at ambient temperature.…”

Section: Resultsmentioning

confidence: 99%

“…Initially, the host-guest complexation analysis of neutral PRO (above pH 7.5) with individual host molecules (b-CD, DOM-b-CD, g-CD and CB7) was investigated in details. Fluorescencebased binding titration of PRO in aqueous solution at pH 9.0 (to minimize the effect of ionic strength and the protonation of PRO; pK a = 3.4 [30] and ca. 3.5 unit shift in pK a value with CB7.…”

Section: Resultsmentioning

confidence: 99%

“…Similarly, a 1:2 complex between g-CD PRO was characterized. [26,28,30] Herein, we report a competitive disassembling of a selfassembled g-CD * (PRO) 2 host-guest complex by DOM-b-CD and CB7 in water to achieve novel optical properties of the encapsulated guest. This method has potential application for tuning properties of any guest molecule with a sizeable binding affinity towards multiple hosts.…”

Section: Introductionmentioning

confidence: 99%

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Tailoring Emission Properties Using Macrocyclic Nanocavities via Guest Interplay in Aqueous Solution

2016

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The non‐covalent approach of tuning photophysical properties via competitive disassembling of a host‐guest complex using same or different classes of the water‐soluble macrocyclic molecule is demonstrated. Cucurbit[7]uril, a pumpkin‐shaped, and heptakis‐(2,6‐di‐O‐methyl)‐β‐cyclodextrin, a toroid‐shaped water‐soluble organic macrocycle are used as competitor host molecule for disassembling another host‐guest assembly. This competitive process has been monitored using various spectroscopic and microscopic techniques. This competitive fluorescence‐based guest interplay allows us to modulate the emissive properties of encapsulated guest and can be applied for the development of novel fluorescent assay and fluorescent materials.

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Nutraceuticals: Formulations and Commercialization

Zaman

Milani

Bhatt

et al. 2019

Kirk-Othmer Encyclopedia of Chemical Technology

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Nutraceuticals are currently growing alternative option for prevention as well as treatment for many acute and chronic illnesses. At some stage where a single pharmaceutical drug acts as a solo performer to treat the illness, the herbal remedy provides group of ingredients together to eradicate the disease. Many of the pharmaceutical drugs are from herbal origin and acts as a potent solo performer against the disease or disorder. While on the other side group of active ingredients present in herbal remedy may stimulate the effect of main active constituent to treat the disease. The resulting effect of course depends on how each of the ingredient are interacting with each other to stimulate the actions of each other. Though there is vast research going on development of nutraceuticals, the challenges associated with nutraceuticals such as variation in active ingredient content, difficulty in purification, lack of appropriate nomenclature, lack of confine regulations, formulation related challenges as well as solubility problems leads researchers as well as formulators in a direction to find out unmet need to overcome these challenges. The concept of solo and concert performance in regards to nutraceuticals and challenges related to nutraceuticals are described here in this article.

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Phytochemicals for the Management of Melanoma

Cited by 63 publications

References 313 publications

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

Tailoring Emission Properties Using Macrocyclic Nanocavities via Guest Interplay in Aqueous Solution

Nutraceuticals: Formulations and Commercialization

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