Quercetin-Loaded Nanomedicine as Oncotherapy

Das, Sabya Sachi; Verma, Priya Ranjan Prasad; Kar, Sweta; Singh, Sandeep Kumar

doi:10.1007/978-981-15-1664-1_5

Cited by 16 publications

(10 citation statements)

References 109 publications

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“…Despite their low bioavailability, a proper delivery system such as nanoformulation may aid in their clinical applications. Nanotechnology offers multiple benefits in treating chronic human diseases by site-specific and target-oriented delivery of precise medicines, improving the efficacy of drugs and natural products [ 169 , 170 ]. For instance, phytochemical cyclodextrin complexes have the potential for transformation into drug delivery systems [ 171 ], and nanotechnology-based drug delivery for therapeutics are bioactive compounds from plant sources [ 172 ].…”

Section: Discussionmentioning

confidence: 99%

Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds

Chagas

Behrens²,

Tellis³

et al. 2022

Oxidative Medicine and Cellular Longevity

138

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Plant preparations have been used to treat various diseases and discussed for centuries. Research has advanced to discover and identify the plant components with beneficial effects and reveal their underlying mechanisms. Flavonoids are phytoconstituents with anti-inflammatory, antimutagenic, anticarcinogenic, and antimicrobial properties. Herein, we listed and contextualized various aspects of the protective effects of the flavonols quercetin, isoquercetin, kaempferol, and myricetin and the flavones luteolin, apigenin, 3 ′ ,4 ′ -dihydroxyflavone, baicalein, scutellarein, lucenin-2, vicenin-2, diosmetin, nobiletin, tangeretin, and 5-O-methyl-scutellarein. We presented their structural characteristics and subclasses, importance, occurrence, and food sources. The bioactive compounds present in our diet, such as fruits and vegetables, may affect the health and disease state. Therefore, we discussed the role of these compounds in inflammation, oxidative mechanisms, and bacterial metabolism; moreover, we discussed their synergism with antibiotics for better disease outcomes. Indiscriminate use of antibiotics allows the emergence of multidrug-resistant bacterial strains; thus, bioactive compounds may be used for adjuvant treatment of infectious diseases caused by resistant and opportunistic bacteria via direct and indirect mechanisms. We also focused on the reported mechanisms and intracellular targets of flavonols and flavones, which support their therapeutic role in inflammatory and infectious diseases.

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Section: Discussionmentioning

confidence: 99%

Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds

Chagas

Behrens²,

Tellis³

et al. 2022

Oxidative Medicine and Cellular Longevity

138

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“…Quercetin (QT), a natural flavonoid and anti-oxidant, has exhibited potential neuroprotective (anti-parkinsonism) [ 4 ] and chemotherapeutic (anticancer) [ 5 ] effects. QT potentially inhibits intracellular and mitochondrial ROS, leading to reduced oxidative stress in neuronal cells [ 1 ].…”

Section: Discussionmentioning

confidence: 99%

“…Quercetin (QT), a natural flavonoid and anti-oxidant, has exhibited potential neuroprotective (anti-parkinsonism) [4] and chemotherapeutic (anticancer) [5] effects. QT potentially inhibits intracellular and mitochondrial ROS, leading to reduced oxidative stress However, the presence of surfactant and oil in QNE could have increased the cytotoxic potential of pure QT against the treated human cancer cells.…”

Section: Discussionmentioning

confidence: 99%

“…Numerous studies have shown that QT exhibits multifaceted therapeutic applications in various NDDs and demonstrates potential pharmacological effects, including anticancer, antimicrobial, antiviral, cardiovascular diseases, and many others [ 2 , 3 ]. QT is one of the most potent natural antioxidants, which exhibits neuroprotective [ 4 ] and anticancer effects [ 5 ] due to its superior anti-oxidative properties, inhibitory actions against protein kinases, and regulatory action on several gene expressions. The anti-oxidative properties of QT assists in counteracting the excessive formation of ROS, leading to cellular oxidative stress, a pathological condition associated with cancer, and several ageing-mediated neurological diseases [ 6 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

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Food-Grade Quercetin-Loaded Nanoemulsion Ameliorates Effects Associated with Parkinson’s Disease and Cancer: Studies Employing a Transgenic C. elegans Model and Human Cancer Cell Lines

et al. 2022

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A nanosized food-grade quercetin-loaded nanoemulsion (QNE) system comprising capmul MCM NF (oil) and cremophor RH 40 (surfactant) was developed using a high-speed homogenization technique. The developed QNE was studied for its significant neuroprotective (anti-Parkinsonism) and cytotoxicity (anticancer) effects against Caenorhabditis elegans (C. elegans) strains and human cancer cells, respectively. HR-TEM studies revealed that the QNE was spherical with a mean globule size of ~50 nm. Selected area electron diffraction (SAED) studies results demonstrated that QNE was amorphous. In vivo results show that QNE potentially reduced the α-Syn aggregation, increased mitochondrial and fat content, and improved the lifespan in transgenic C. elegans strain NL5901. QNE significantly downregulated the reactive oxygen species (ROS) levels in wild-type C. elegans strain N2. In vitro results of the MTT assay show that QNE significantly exhibited chemotherapeutic effects in all treated human cancer cells in an order of cytotoxicity: HeLa cells > A549 cells > MIA PaCa-2 cells, based on the IC50 values at 24 h. Conclusively, the QNE showed improved solubility, targetability, and neuroprotective effects against the PD-induced C. elegans model, and also cytotoxicity against human cancer cells and could be potentially used as an anti-Parkinson’s or anticancer agent.

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“…In this context, quercetin (QT; 3,3′,4′,5,7-pentahydroxyflavanone) is one of the most studied dietary flavonoids (subclass of polyphenols), which exhibits a significant role as a prominent target when conducting investigations on alternative therapy against Leishmania infections. QT is widely found in medicinal plants, fruits, vegetables, and other green sources. , It has been reported to have diverse therapeutic activities, including antioxidant, anti-inflammatory, antibacterial, antiviral, iron chelating, anticancer, antiproliferative, and others. Moreover, the in vitro antileishmanial activity of QT against promastigote forms of L.…”

Section: Introductionmentioning

confidence: 99%

Therapeutic Potential of Quercetin-Loaded Nanoemulsion against Experimental Visceral Leishmaniasis: In Vitro/Ex Vivo Studies and Mechanistic Insights

et al. 2022

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Visceral leishmaniasis (VL) is one of the most fatal and neglected tropical diseases caused by Leishmania donovani (L. donovani). The applications of currently available chemotherapy (amphotericin B, miltefosine, and others) in VL treatment have been limited due to their poor bioavailability, unfavorable toxicity profile, and prolonged parenteral dosing. Quercetin (QT), a potent natural antioxidant, is a prominent target when conducting investigations on alternative therapies against L. donovani infections. However, the therapeutic applications of QT have been restricted due to its low solubility and bioavailability. In the present study, we developed and evaluated the antileishmanial activity (ALA) of quercetin-loaded nanoemulsion (QTNE) against L. donovani clinical strains. In vitro anti-promastigote assay results demonstrated that QTNE (IC50 6.6 μM, 48 h) significantly inhibited the growth of parasites more efficiently than the pure QT suspension in a dose- and time-dependent manner. Results of the anti-amastigote assay revealed that the infected macrophages (%) of QTNE were significantly more than those of the pure QT suspension at all concentrations (6.6, 26.4, and 52.8 μM; p < 0.05, p < 0.01 compared to the control). Moreover, the results of in vitro and ex vivo studies assisted in determining the mechanistic insights associated with the ALA of QTNE. The overall findings suggested that QTNE exhibited potential ALA by enhancing the intracellular ROS and nitric oxide levels, inducing distortion of membrane integrity and phosphatidylserine release (AV/PI), rupturing the parasite DNA (late apoptosis/necrosis process), and upregulating the immunomodulatory effects (IFN-γ and IL-10 levels). Additionally, QTNE showed superior biocompatibility against all of the treated healthy cells (PBMCs, PECs, and BMCs) as compared to the control. In conclusion, QTNE acts as a potential antileishmanial agent targeting both promastigote and intracellular amastigote forms of L. donovani, which thus opens a new avenue for the use of QTNE in VL therapy.

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Quercetin-Loaded Nanomedicine as Oncotherapy

Cited by 16 publications

References 109 publications

Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds

Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds

Food-Grade Quercetin-Loaded Nanoemulsion Ameliorates Effects Associated with Parkinson’s Disease and Cancer: Studies Employing a Transgenic C. elegans Model and Human Cancer Cell Lines

Therapeutic Potential of Quercetin-Loaded Nanoemulsion against Experimental Visceral Leishmaniasis: In Vitro/Ex Vivo Studies and Mechanistic Insights

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