Discovery and synthesis of novel magnolol derivatives with potent anticancer activity in non-small cell lung cancer

Tang, Huan; Zhang, Yongguang; Li, Dan; Fu, Suhong; Tang, Minghai; Wan, Li; Chen, Kai; Liu, Zhuowei; Xue, Linlin; Peng, Aihua; Ye, Haoyu; Chen, Lijuan

doi:10.1016/j.ejmech.2018.06.048

Cited by 34 publications

(15 citation statements)

References 47 publications

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“…Diffusion and molecular matrix degradation of the Quercetin play an important role in the release of the Quercetin from the NP. Since the size of Quercetin is lower than the particle, Quercetin can easily diffuse from the surface or pores of the NP [34,35].…”

Section: Ee and Lc Of Np Including Quercetinmentioning

confidence: 99%

Assessment of mechanism involved in the apoptotic and anti-cancer activity of Quercetin and Quercetin-loaded chitosan nanoparticles

Doğan

2022

Med Oncol

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In prior studies, Quercetin was revealed to exhibit anticancer features in a variety of cancer cell lines.However, the impact of Quercetin on neuroblastoma is unknown. This study looked into the potential cytotoxic effects of Quercetin and Quercetin-loaded chitosan nanoparticles (NPs) on the SH-SY5Y cell line. In this study, NPs containing Quercetin was prepared and characterization studies were performed.The vitality of the cells was measured using the XTT test after 24 hours of treatment with various concentrations of Quercetin (0.5, 1, 2, 4, and 8 µg/mL). ELISA kits were used to detect the amounts of cleaved PARP, BCL-2, 8-Hydroxy-deoxyguanosine (8-oxo-dG), cleaved caspase 3, Bax, total oxidant, and total antioxidant in the cells. The results of the chitosan NPs characterization investigation revealed that the particle size, encapsulation effectiveness, and drug release pro le of NPs were all appropriate for cell culture studies. Quercetin and Quercetin-loaded chitosan NPs signi cantly reduced cell viability in SH-SY5Y cells at different concentrations (**p < 0.05). 2 µg/mL Quercetin and Quercetin-loaded chitosan NPs signi cantly enhanced the levels of 8-oxo-dG, cleaved caspase 3, Bax, cleaved PARP, and total oxidant in ELISA testing. However, treatment with 2 µg/mL of Quercetin and Quercetin-loaded chitosan NPs did not affect the amount of BCL-2 protein. Overall, Quercetin and Quercetin-loaded chitosan NPs caused signi cant cytotoxicity in SH-SY5Y cells via producing oxidative stress, DNA damage, and eventually apoptosis.

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Section: Ee and Lc Of Np Including Quercetinmentioning

confidence: 99%

Assessment of mechanism involved in the apoptotic and anti-cancer activity of Quercetin and Quercetin-loaded chitosan nanoparticles

Doğan

2022

Med Oncol

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“…Chemotherapeutics consist of a large group of drugs, including doxorubicin, docetaxel, camptothecin, 5-fluorouracil, paclitaxel, gemcitabine [ 85 ], bortezomib [ 86 ], and anastrozole [ 87 ]. Moreover, several natural compounds, such as magnolol [ 88 , 89 ] and curcumin [ 90 , 91 ], have proven their potential against cancer in preclinical studies.…”

Section: Supramolecular Hydrogels As Carriers For Biologically Active Substancesmentioning

confidence: 99%

From Supramolecular Hydrogels to Multifunctional Carriers for Biologically Active Substances

Skopińska-Wiśniewska

Flor

Kozłowska

2021

IJMS

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Supramolecular hydrogels are 3D, elastic, water-swelled materials that are held together by reversible, non-covalent interactions, such as hydrogen bonds, hydrophobic, ionic, host–guest interactions, and metal–ligand coordination. These interactions determine the hydrogels’ unique properties: mechanical strength; stretchability; injectability; ability to self-heal; shear-thinning; and sensitivity to stimuli, e.g., pH, temperature, the presence of ions, and other chemical substances. For this reason, supramolecular hydrogels have attracted considerable attention as carriers for active substance delivery systems. In this paper, we focused on the various types of non-covalent interactions. The hydrogen bonds, hydrophobic, ionic, coordination, and host–guest interactions between hydrogel components have been described. We also provided an overview of the recent studies on supramolecular hydrogel applications, such as cancer therapy, anti-inflammatory gels, antimicrobial activity, controlled gene drug delivery, and tissue engineering.

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“…Studies reported that they exhibit anticancer properties by inhibiting proliferation, inducing differentiation and apoptosis, suppressing angiogenesis, countering metastasis, and reversing multidrug resistance. 9,[11][12][13][14] Although honokiol/magnolol showed antitumor activities against various tumor cells, their clinical use is limited by their insolubility, low bioavailability, and vascular irritation. Moreover, oral administration of honokiol/magnolol showed weak antitumor activity in vivo.…”

Section: Introductionmentioning

confidence: 99%

Honokiol/Magnolol-Loaded Self-Assembling Lecithin-Based Mixed Polymeric Micelles (lbMPMs) for Improving Solubility to Enhance Oral Bioavailability

Lin

Cheng

Chen

et al. 2021

IJN

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Objective This study was intended to utilize lecithin-based mixed polymeric micelles ( lb MPMs) for enhancing the solubility and bioavailability of honokiol and magnolol to resolve the hindrance of their extreme hydrophobicity on the clinical applications. Methods Lecithin was selected to increase the volume of the core of lb MPMs, thereby providing a greater solubilization capacity. A series of amphiphilic polymers (sodium deoxycholate [NaDOC], Cremophor ®, and Pluronic ® series) were included with lecithin for screening and optimization. Results After preliminary evaluation and subsequentially optimization, two lb MPMs formulations composed of honokiol/magnolol:lecithin:NaDOC ( lb MPMs[NaDOC]) and honokiol/magnolol:lecithin:PP123 ( lb MPMs[PP123]) in respective ratios of 6:2:5 and 1:1:10 were optimally obtained with the mean particle sizes of 80–150 nm, encapsulation efficacy (EEs) of >90%, and drug loading (DL) of >9.0%. These lb MPMs efficiently stabilized honokiol/magnolol in phosphate-buffered saline (PBS) at room temperature or 4 °C and in fetal bovine serum or PBS at 37 °C. PK study demonstrated that lb MPMs[NaDOC] showed much improvement in enhancing bioavailability than that by lb MPMs[PP123] for both honokiol and magnolol. The absolute bioavailability for honokiol and magnolol after intravenous administration of lb MPMs[NaDOC] exhibited 0.93- and 3.4-fold increases, respectively, compared to that of free honokiol and magnolol. For oral administration with lb MPMs[NaDOC], the absolute bioavailability of honokiol was 4.8%, and the absolute and relative bioavailability of magnolol were 20.1% and 2.9-fold increase, respectively. Conclusion Overall, honokiol/magnolol loaded in lb MPMs[NaDOC] showed an improvement of solubility with suitable physical characteristics leading to enhance honokiol and magnolol bioavailability and facilitating their wider application as therapeutic agents for treating human disorders.

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Discovery and synthesis of novel magnolol derivatives with potent anticancer activity in non-small cell lung cancer

Cited by 34 publications

References 47 publications

Assessment of mechanism involved in the apoptotic and anti-cancer activity of Quercetin and Quercetin-loaded chitosan nanoparticles

Assessment of mechanism involved in the apoptotic and anti-cancer activity of Quercetin and Quercetin-loaded chitosan nanoparticles

From Supramolecular Hydrogels to Multifunctional Carriers for Biologically Active Substances

Honokiol/Magnolol-Loaded Self-Assembling Lecithin-Based Mixed Polymeric Micelles (lbMPMs) for Improving Solubility to Enhance Oral Bioavailability

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