Effect of 5,7-dimethoxyflavone on Bcrp1-mediated transport of sorafenib in vitro and in vivo in mice

Bae, Sohyun; D’Cunha, Ronilda; Shao, Jiahao; An, Guohua

doi:10.1016/j.ejps.2018.02.004

Cited by 12 publications

(9 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…5,7-Dimethoxyflavone ( 86 ) isolated from K. galanga was found to reduce cancer resistance to tyrosine kinase inhibitors (TKI) by inhibiting breast cancer resistance protein (BCRP), one of the efflux transporters that increased efflux of TKI out of cancer cells. This was observed both in vitro with a dose-dependent increase in the intracellular concentration of sorafenib in MDCK/BCRP1 breast cancer resistance cells, with an EC 50 of 8.78 μM as well as in vivo by increasing sorafenib AUC in mice tissues when co-administered with compound 88 , as reported by kinetic results [21]. The isolated methyl- β - D -galactopyranoside specific lectin from the rhizome of K. rotunda exhibited in vitro antitumor activity against Ehrlich ascites carcinoma cells at a pH between 6–9 and a temperature range between 30–80 °C.…”

Section: Biological Activitysupporting

confidence: 57%

Recent Advances in Kaempferia Phytochemistry and Biological Activity: A Comprehensive Review

et al. 2019

View full text Add to dashboard Cite

Background: Plants belonging to the genus Kaempferia (family: Zingiberaceae) are distributed in Asia, especially in the southeast region, and Thailand. They have been widely used in traditional medicines to cure metabolic disorders, inflammation, urinary tract infections, fevers, coughs, hypertension, erectile dysfunction, abdominal and gastrointestinal ailments, asthma, wounds, rheumatism, epilepsy, and skin diseases. Objective: Herein, we reported a comprehensive review, including the traditional applications, biological and pharmacological advances, and phytochemical constituents of Kaempheria species from 1972 up to early 2019. Materials and methods: All the information and reported studies concerning Kaempheria plants were summarized from library and digital databases (e.g., Google Scholar, Sci-finder, PubMed, Springer, Elsevier, MDPI, Web of Science, etc.). The correlation between the Kaempheria species was evaluated via principal component analysis (PCA) and agglomerative hierarchical clustering (AHC), based on the main chemical classes of compounds. Results: Approximately 141 chemical constituents have been isolated and reported from Kaempferia species, such as isopimarane, abietane, labdane and clerodane diterpenoids, flavonoids, phenolic acids, phenyl-heptanoids, curcuminoids, tetrahydropyrano-phenolic, and steroids. A probable biosynthesis pathway for the isopimaradiene skeleton is illustrated. In addition, 15 main documented components of volatile oils of Kaempheria were summarized. Biological activities including anticancer, anti-inflammatory, antimicrobial, anticholinesterase, antioxidant, anti-obesity-induced dermatopathy, wound healing, neuroprotective, anti-allergenic, and anti-nociceptive were demonstrated. Conclusions: Up to date, significant advances in phytochemical and pharmacological studies of different Kaempheria species have been witnessed. So, the traditional uses of these plants have been clarified via modern in vitro and in vivo biological studies. In addition, these traditional uses and reported biological results could be correlated via the chemical characterization of these plants. All these data will support the biologists in the elucidation of the biological mechanisms of these plants.

show abstract

Section: Biological Activitysupporting

confidence: 57%

Recent Advances in Kaempferia Phytochemistry and Biological Activity: A Comprehensive Review

et al. 2019

View full text Add to dashboard Cite

show abstract

“…Of particular interest are the helper effects against cancer therapy resistance by sensitizing malignant cells towards therapies. Those properties of flavonoids clearly demonstrated in preclinical studies are considered of particularly great clinical utility, when applied to anti-cancer therapies tailored to the personalized patient profile [48][49][50][51][52][53][54][55][56][57][58][59].…”

Section: Focus Of the Current Study: Flavonoids As A Helper In Anti-cancer Therapymentioning

confidence: 99%

“…As stated above, the disadvantage of TKIs usage is resistance; important mechanisms of the development of resistance include enhanced TKI efflux through efflux transporters such as BCRP [54]. 5,7-dimethoxyflavone effectively inhibited BCRP-1-mediated sorafenib efflux in Madin-Darby Canine Kidney Type II wild-type cell subclones that were transfected with murine Bcrp1 (MDCK/Bcrp1); these results highlight an essential potential of 5,7-dimethoxyflavone as a chemosensitizing agent in BCRP-mediated drug resistance [54]. Further, the flavonol kaempferol enhanced the chemotherapeutic efficacy of sorafenib against HCC demonstrated in silico and in vitro (liver cancer HepG2 and N1S1 cells); also, kaempferol reversed MDR by decreasing P-gp overexpression [137].…”

Section: Flavonoids Enhance Effectiveness Of Targeted Anti-cancer Therapymentioning

confidence: 99%

“…TKIs are novel target-specific anti-cancer drugs. Nevertheless, the disadvantage of TKIs usage is the development of resistance [ 54 ]. The existence of EGFR mutations in NSCLC led to changes in the traditional lung cancer regimen from traditional cytotoxic chemotherapy to molecularly targeted agents.…”

Section: Resistance To Anti-cancer Treatmentsmentioning

confidence: 99%

“…Also, Saraswati et al demonstrated the capability of a chalcone phloretin to overcome sorafenib resistance in HCC as demonstrated through Src homology region 2 domain-containing phosphatase-1 (SHP-1)-mediated inhibition of STAT3 and Akt/VEGFR2 [ 136 ]. As stated above, the disadvantage of TKIs usage is resistance; important mechanisms of the development of resistance include enhanced TKI efflux through efflux transporters such as BCRP [ 54 ]. 5,7-dimethoxyflavone effectively inhibited BCRP-1-mediated sorafenib efflux in Madin-Darby Canine Kidney Type II wild-type cell subclones that were transfected with murine Bcrp1 (MDCK/Bcrp1); these results highlight an essential potential of 5,7-dimethoxyflavone as a chemosensitizing agent in BCRP-mediated drug resistance [ 54 ].…”

Section: Resistance To Anti-cancer Treatmentsmentioning

confidence: 99%

See 2 more Smart Citations

Flavonoids as an effective sensitizer for anti-cancer therapy: insights into multi-faceted mechanisms and applicability towards individualized patient profiles

et al. 2021

View full text Add to dashboard Cite

Cost-efficacy of currently applied treatments is an issue in overall cancer management challenging healthcare and causing tremendous economic burden to societies around the world. Consequently, complex treatment models presenting concepts of predictive diagnostics followed by targeted prevention and treatments tailored to the personal patient profiles earn global appreciation as benefiting the patient, healthcare economy, and the society at large. In this context, application of flavonoids as a spectrum of compounds and their nano-technologically created derivatives is extensively under consideration, due to their multi-faceted anti-cancer effects applicable to the overall cost-effective cancer management, primary, secondary, and even tertiary prevention. This article analyzes most recently updated data focused on the potent capacity of flavonoids to promote anti-cancer therapeutic effects and interprets all the collected research achievements in the frame-work of predictive, preventive, and personalized (3P) medicine. Main pillars considered are:- Predictable anti-neoplastic, immune-modulating, drug-sensitizing effects;- Targeted molecular pathways to improve therapeutic outcomes by increasing sensitivity of cancer cells and reversing their resistance towards currently applied therapeutic modalities.

show abstract

Efflux transporters in cancer resistance: Molecular and functional characterization of breast cancer resistance protein

Morris

2020

Drug Efflux Pumps in Cancer Resistance Pathways: From Molecular Recognition and Characterization to Possible Inhibition Strateg

View full text Add to dashboard Cite

Effect of 5,7-dimethoxyflavone on Bcrp1-mediated transport of sorafenib in vitro and in vivo in mice

Cited by 12 publications

References 34 publications

Recent Advances in Kaempferia Phytochemistry and Biological Activity: A Comprehensive Review

Recent Advances in Kaempferia Phytochemistry and Biological Activity: A Comprehensive Review

Flavonoids as an effective sensitizer for anti-cancer therapy: insights into multi-faceted mechanisms and applicability towards individualized patient profiles

Efflux transporters in cancer resistance: Molecular and functional characterization of breast cancer resistance protein

Contact Info

Product

Resources

About