New Insights for the Use of Quercetin Analogs in Cancer Treatment

Iacopetta, Domenico; Grande, Fedora; Caruso, Anna; Mordocco, Roberta A.; Plutino, Maria Rosaria; Scrivano, Luca; Ceramella, Jessica; Muià, Noemi; Saturnino, Carmela; Puoci, Francesco; Rosano, Camillo; Sinicropi, Maria Stefania

doi:10.4155/fmc-2017-0118

Cited by 63 publications

(48 citation statements)

References 60 publications

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“…BCP, which is more than 25% of the essential oil from Pamburus missionis, has synergistic effect with two other important components of the essential oil, phytol (8) and aromadendrene oxide (9) (Figure 3), resulting in antitumor activity against A431 and HaCaT cell lines, by blocking the cell in phase G0/G1 or sub-G1. The mechanism of action is associated to ROS production [69] and the mitochondrial membrane potential loss, by increasing Bax expression and decreasing Bcl-2 expression. Bax and Bak oligomers form pores, which increase the permeability of the external mitochondrial membrane, releasing cytochrome c in the cytoplasm, which is an apoptosis characterizing event [70][71][72].…”

Section: β-Caryophyllene and Cancermentioning

confidence: 99%

“…In detail, in the latter cell line, the BCP determines a rise of the intracellular concentrations in the drug, probably by increasing the permeability of the cell membrane [13]. The mechanism of action is associated to ROS production [69] and the mitochondrial membrane potential loss, by increasing Bax expression and decreasing Bcl-2 expression. Bax and Bak oligomers form pores, which increase the permeability of the external mitochondrial membrane, releasing cytochrome c in the cytoplasm, which is an apoptosis characterizing event [70][71][72].…”

Section: β-Caryophyllene and Cancermentioning

confidence: 99%

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β-Caryophyllene: A Sesquiterpene with Countless Biological Properties

et al. 2019

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β-Caryophyllene (BCP), a natural bicyclic sesquiterpene, is a selective phytocannabinoid agonist of type 2 receptors (CB2-R). It isn’t psychogenic due to the absence of an affinity to cannabinoid receptor type 1 (CB1). Among the various biological activities, BCP exerts anti-inflammatory action via inhibiting the main inflammatory mediators, such as inducible nitric oxide synthase (iNOS), Interleukin 1 beta (IL-1β), Interleukin-6 (IL-6), tumor necrosis factor-alfa (TNF-α), nuclear factor kapp a-light-chain-enhancer of activated B cells (NF-κB), cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2). Peroxisome proliferator-activated receptors alpha (PPAR-α) effects are also mediated by the activation of PPAR-α and PPAR-γ receptors. In detail, many studies, in vitro and in vivo, suggest that the treatment with β-caryophyllene improves the phenotype of animals used to model various inflammatory pathologies, such as nervous system diseases (Parkinson’s disease, Alzheimer’s disease, multiple sclerosis, amyotrophic lateral sclerosis, stroke), atherosclerosis, and tumours (colon, breast, pancreas, lymphoma, melanoma and glioma cancer). Furthermore, pre-clinical data have highlighted that BCP is potentially useful in Streptococcus infections, osteoporosis, steatohepatitis, and exerts anticonvulsant, analgesic, myorelaxing, sedative, and antidepressive effects. BCP is non-toxic in rodents, with a Lethal dose, 50% (LD50) greater than 5000 mg/kg. Nevertheless, it inhibits various cytochrome P450 isoforms (above all, CYP3A4), which metabolise xenobiotics, leading to adverse effects, due to drug levels over therapeutic window. All the reported data have highlighted that both pharmacological and toxicological aspects need to be further investigated with clinical trials.

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Section: β-Caryophyllene and Cancermentioning

confidence: 99%

Section: β-Caryophyllene and Cancermentioning

confidence: 99%

β-Caryophyllene: A Sesquiterpene with Countless Biological Properties

et al. 2019

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“…Perhaps, the most important property of this flavonoid is its antioxidant effect. In addition, quercetin can be useful in cancer prevention (Iacopetta et al, ) and is known to have antiallergic, anti‐inflammatory, and antiviral activities (Y. Liu et al, ). Most importantly, quercetin impedes the propagation of various types of cancers, such as lung, prostate, liver, breast, colon, and cervical (Y. Liu et al, ); these anticancer properties are exerted through various mechanisms that involve cellular signaling and the ability to inhibit enzymes responsible for the activation of carcinogens.…”

Section: Introductionmentioning

confidence: 99%

Anticancer potential of quercetin: A comprehensive review

Rauf

Imran

Khan

et al. 2018

Phytotherapy Research

503

276

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Diet plays a key role to maintaining healthy life. Many natural products present in our diet, such as flavonoids, can prevent the progression of cancer. Quercetin, a distinctive bioactive flavonoid, is a dietary component that has attracted the attention of dietitians and medicinal chemists due to its numerous health-promoting effects. It is an outstanding antioxidant that has a well-documented role in reducing different human cancers. Quercetin exhibits direct proapoptotic effects on tumor cells and thus can inhibit the progress of numerous human cancers. The anticancer effect of quercetin has been documented in numerous in vitro and in vivo studies that involved several cell lines and animal models. On the other hand, the high toxic effect of quercetin against cancer cells is accompanied with little or no side effects or harm to normal cells. Accordingly, this review presents an overview of recent developments on the use of quercetin against different types of cancer along with mechanisms of action. In addition, the present review summarizes the literature pertaining to quercetin as an anticancer agent and provides an assessment of the potential utilization of this natural compound as a complimentary or alternative medicine for preventing and treating cancer.

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“…The primary mechanism of action of these compounds is their anti/pro-oxidant effect [14][15][16]. Some examples of polyphenols with anti cancer effect are flavonoids such as quercetin, kaempferol, fisetin, myricetin (Myr), and phenolic acids such as gallic acid (GA), protocatechuic acid and rosmarinic acid [6,8,10,17]. Recent studies have demonstrated that Myr and GA particularly, could have interesting applications in the treatment of cancer [18,19].…”

Section: Introductionmentioning

confidence: 99%

Effect of Gallic acid and Myricetin on ovarian cancer models: a possible alternative antitumoral treatment

Varela-Rodríguez

Sánchez‐Ramírez

Hernández‐Ramírez

et al. 2020

BMC Complement Med Ther

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Background: Ovarian cancer is the leading cause of mortality among malignant gynecological tumors. Surgical resection and chemotherapy with intravenous platinum/taxanes drugs are the treatments of choice, with little effectiveness in later stages and severe toxicological effects. Therefore, this study aimed to evaluate the antineoplastic activity of gallic acid (GA) and myricetin (Myr) administrated peritumorally in Nu/Nu mice xenotransplanted with SKOV-3 cells. Methods: Biological activity of GA and MYR was evaluated in SKOV-3 and OVCAR-3 cells (ovarian adenocarcinomas) by confocal/transmission electron microscopy, PI-flow cytometry, H 2-DCF-DA stain, MTT, and Annexin V/PI assays. Molecular targets of compounds were determined with ACD/I-Labs and SEA. Antineoplastic activity was performed in SKOV-3 cells subcutaneously xenotransplanted into female Nu/Nu mice treated peritumorally with 50 mg/kg of each compound (2 alternate days/week) for 28 days. Controls used were paclitaxel (5 mg/kg) and 20 μL of vehicle (0.5% DMSO in 1X PBS). Tumor lesions, organs and sera were evaluated with NMR, USG, histopathological, and paraclinical studies. Results: In vitro studies showed a decrease of cell viability with GA and Myr in SKOV-3 (50 and 166 μg/mL) and OVCAR-3 (43 and 94 μg/mL) cells respectively, as well as morphological changes, cell cycle arrest, and apoptosis induction due to ROS generation (p ≤ 0.05, ANOVA). In silico studies suggest that GA and MYR could interact with carbonic anhydrase IX and PI3K, respectively. In vivo studies revealed inhibitory effects on tumor lesions development with GA and MYR up to 50% (p ≤ 0.05, ANOVA), with decreased vascularity, necrotic/fibrotic areas, neoplastic stroma retraction and apoptosis. However, toxicological effects were observed with GA treatment, such as leukocyte infiltrate and hepatic parenchyma loss, hypertransaminasemia (ALT: 150.7 ± 25.60 U/L), and hypoazotemia (urea: 33.4 ± 7.4 mg/dL), due to the development of chronic hepatitis (p ≤ 0.05, ANOVA).

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New Insights for the Use of Quercetin Analogs in Cancer Treatment

Abstract: The studied compounds represent suitable leads for the development of innovative anticancer drugs. [Formula: see text].

Cited by 63 publications

References 60 publications

β-Caryophyllene: A Sesquiterpene with Countless Biological Properties

β-Caryophyllene: A Sesquiterpene with Countless Biological Properties

Anticancer potential of quercetin: A comprehensive review

Effect of Gallic acid and Myricetin on ovarian cancer models: a possible alternative antitumoral treatment

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