Decreased B16F10 melanoma growth and impaired tumour vascularization in BDF1 mice with quercetin-cyclodextrin binary system

Rajendrakumar, Kale; Saraf, M. N.; Juvekar, Aarti; Tayade, Pralhad

doi:10.1211/jpp.58.10.0008

Cited by 38 publications

(29 citation statements)

References 17 publications

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“…Accordingly, many studies analyzed possible complexes able to transport Qu to various tissues [152, 153]. Promising studies have been obtained with polyethylene glycol (PEG) and sulfobutyl ether-7beta-cyclodextrin (SBE7betaCD) [154, 155]. The association of Qu to PEG (Q-PEGL) has been tested in different mouse models through intravenous injections.…”

Section: In Vivo Studies and Their Problemsmentioning

confidence: 99%

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Quercetin and Cancer Chemoprevention

Gibellini

Pinti

Nasi

et al. 2011

Evidence-Based Complementary and Alternative Medicine

391

243

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Several molecules present in the diet, including flavonoids, can inhibit the growth of cancer cells with an ability to act as “chemopreventers”. Their cancer-preventive effects have been attributed to various mechanisms, including the induction of cell-cycle arrest and/or apoptosis as well as the antioxidant functions. The antioxidant activity of chemopreventers has recently received a great interest, essentially because oxidative stress participates in the initiation and progression of different pathological conditions, including cancer. Since antioxidants are capable of preventing oxidative damage, the wide use of natural food-derived antioxidants is receiving greater attention as potential anti-carcinogens. Among flavonoids, quercetin (Qu) is considered an excellent free-radical scavenging antioxidant, even if such an activity strongly depends on the intracellular availability of reduced glutathione. Apart from antioxidant activity, Qu also exerts a direct, pro-apoptotic effect in tumor cells, and can indeed block the growth of several human cancer cell lines at different phases of the cell cycle. Both these effects have been documented in a wide variety of cellular models as well as in animal models. The high toxicity exerted by Qu on cancer cells perfectly matches with the almost total absence of any damages for normal, non-transformed cells. In this review we discuss the molecular mechanisms that are based on the biological effects of Qu, and their relevance for human health.

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Section: In Vivo Studies and Their Problemsmentioning

confidence: 99%

“…Qu-SBE7betaCD complex significantly improved anti-cancer activity of Qu, with decreased density of the microvessel within the melanoma [154]. …”

Section: In Vivo Studies and Their Problemsmentioning

confidence: 99%

Quercetin and Cancer Chemoprevention

Gibellini

Pinti

Nasi

et al. 2011

Evidence-Based Complementary and Alternative Medicine

391

243

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“…6,8 In another approach, a water-soluble derivative of quercetin has been synthesized, but a bioavailability of only 20% was obtained. 15 Various techniques have also been used to improve quercetin's aqueous solubility via complexation with cyclodextrins 16 for example. In addition, liposomal formulations have previously been reported.…”

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confidence: 99%

Polyethylene Glycol Conjugated Polymeric Nanocapsules for Targeted Delivery of Quercetin to Folate-Expressing Cancer Cellsin Vitroandin Vivo

et al. 2014

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In this work we describe the formulation and characterization of chemically modified polymeric nanocapsules incorporating the anticancer drug, quercetin, for the passive and active targeting to tumors. Folic acid was conjugated to poly(lactide-co-glycolide) (PLGA) polymer to facilitate active targeting to cancer cells. Two different methods for the conjugation of PLGA to folic acid were employed utilizing polyethylene glycol (PEG) as a spacer. Characterization of the conjugates was performed using FTIR and (1)H NMR studies. The PEG and folic acid content was independent of the conjugation methodology employed. PEGylation has shown to reduce the size of the nanocapsule; moreover, zeta-potential was shown to be polymer-type dependent. Comparative studies on the cytotoxicity and cellular uptake of the different formulations by HeLa cells, in the presence and absence of excess folic acid, were carried out using MTT assay and Confocal Laser Scanning Microscopy, respectively. Both results confirmed the selective uptake and cytotoxicity of the folic acid targeted nanocapsules to the folate enriched cancer cells in a folate-dependent manner. Finally, the passive tumor accumulation and the active targeting of the nanocapsules to folate-expressing cells were confirmed upon intravenous administration in HeLa or IGROV-1 tumor-bearing mice. The developed nanocapsules provide a system for targeted delivery of a range of hydrophobic anticancer drugs in vivo.

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“…(19) While the precise role of ATRA in the carcinogenic process is still not clear, our studies have shown that the use of ATRA can lead to a significant reduction in solid tumor formation (B16F10 mouse melanoma cells) in a Balb/c mouse model. However, as has been shown in studies with BDF1 (C57Bl/6 × DBA/2 cross; H-2 b/d ) (20) or B 6 C 3 F 1 (C57Bl/6 × DBA/2 cross; H-2 b/k ) (21)(22)(23)(24) mice, a lack of '100% purity' at the H-2 allele is not a limiting factor for use of the B16F10 model in assessment of immunotoxicologic endpoints. In fact, Picaud et al (25) clearly showed that B16F10-induced tumors readily formed in C3H (H-2 k ) mice.…”

Section: Discussionmentioning

confidence: 80%

Evaluation of immunomodulatory and antitumor activity of alltransretinoic acid (ATRA) in solid tumor bearing mice

Siddikuzzaman

Grace

2012

Immunopharmacology and Immunotoxicology

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Natural or synthetic agents can modify the immune system and, in some cases, impart a therapeutic benefit. Cancer, a disease of uncontrolled growth and spread of abnormal cells, is a major cause of death. The Vitamin A metabolite all-trans retinoic acid (ATRA) and its other active derivatives are potent modulators of cell growth and differentiation, and because it has an influence on cancer, it can be used as a chemotherapeutic and -preventive agent. To evaluate the immunomodulatory activity of ATRA, the impact of treatment on various parameters, e.g. delayed-type hypersensitivity (DTH), bone marrow cellularity, hematology, and levels of esterase-positive cells, was assessed in Balb/c mice. To evaluate antitumor effects of ATRA, tumor volume and host survival rate were monitored in B16F10 melanoma cell-injected mice. The results showed that administration of ATRA (0.60 mg/kg/dose, IP) caused a decrease in DTH (footpad thickness) in response to challenge with sheep red blood cells (SRBC) in SRBC-sensitized hosts. ATRA also caused increases in WBC counts and bone marrow cell numbers. In tumor-inoculated mice, ATRA caused tumor growth suppression and gave rise to a heightened survival rate. It was also found that ATRA had differential effects on serum levels of reduced glutathione (GSH) and nitric oxide (NO) was reduced in serum. Based on these results, we conclude that ATRA has a potent immunomodulatory potential but also could significantly impact upon solid tumor growth and prolong host survival.

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Decreased B16F10 melanoma growth and impaired tumour vascularization in BDF1 mice with quercetin-cyclodextrin binary system

Cited by 38 publications

References 17 publications

Quercetin and Cancer Chemoprevention

Quercetin and Cancer Chemoprevention

Polyethylene Glycol Conjugated Polymeric Nanocapsules for Targeted Delivery of Quercetin to Folate-Expressing Cancer Cellsin Vitroandin Vivo

Evaluation of immunomodulatory and antitumor activity of alltransretinoic acid (ATRA) in solid tumor bearing mice

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