Combination of Paclitaxel and PXR Antagonist SPA70 Reverses Paclitaxel-Resistant Non-Small Cell Lung Cancer

Niu, Xiaxia; Wu, Ting; Yin, Qishuang; Gu, Xinsheng; Li, Gege; Zhou, Changlong; Ma, Mei; Li, Su; Tang, Shu; Yan, Tian; Yang, Mingming; Cui, Hongmei

doi:10.3390/cells11193094

Cited by 9 publications

(3 citation statements)

References 57 publications

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“…The cells were treated with drugs and incubated for 24 h. The width of the scratch closure was measured and recorded. The cell migration distances were calculated by ImageJ software. , …”

Section: Methodsmentioning

confidence: 99%

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Imperatorin-Loaded RH60/mPEG–PLLA Micelles for Reversing Tamoxifen Resistance in Breast Cancer

Li,

Zhao,

et al. 2024

ACS Appl. Nano Mater.

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Imperatorin (IMP) has demonstrated potential in reversing drug resistance in various tumor cells; however, its limited clinical application and development are attributed to its poor water solubility and low bioavailability. The current work is intended to enhance the oral bioavailability of IMP and its efficacy in overcoming tamoxifen (TAM) resistance in breast cancer cells. We employed mPEG−PLLA and Cremophor RH60 (RH60) to prepare imperatorin nanomicelles (IMP-RH60/mPEG−PLLA). The freeze-dried powder of IMP-RH60/mPEG−PLLA demonstrated a porous structure, and upon reconstitution, the resulting solution exhibited clarity and transparency. The particle size was measured to be 25.48 ± 0.92 nm, with a zeta potential of −5.50 ± 1.06 mV. The encapsulation efficiency was determined to be 85.78 ± 0.84%, while the drug loading was found to be 2.66 ± 0.03%. In comparison to the active pharmaceutical ingredients (APIs) of IMP, IMP-RH60/mPEG−PLLA exhibited a significant increase in in vitro release, improved bioavailability in rats, and enhanced uptake by MCF-7/TAM cells. The coadministration of IMP-RH60/mPEG−PLLA and TAM effectively inhibited the proliferation, colony formation, migration, and invasion of MCF-7/TAM cells. This outcome could potentially be attributed to the downregulation of GST-π and MDR1 drug resistance genes, consequently augmenting the susceptibility of MCF-7/TAM cells to TAM. An experimental model of BALB/c nude xenograft, consisting of human breast cancer cells resistant to tamoxifen (TAM), was established in order to assess the potential in vivo reversal of TAM resistance through the use of IMP-RH60/mPEG−PLLA. The growth of xenografts was inhibited by IMP-RH60/mPEG−PLLA, and it induced apoptosis in tumor tissues through the downregulation of K i -67, GST-π, and MDR1 gene expression. The findings indicated that the utilization of IMP-RH60/mPEG− PLLA micelles resulted in an enhancement of IMP's bioavailability and its efficacy in overcoming TAM resistance.

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“…The cells were treated with drugs and incubated for 24 h. The width of the scratch closure was measured and recorded. The cell migration distances were calculated by ImageJ software. , …”

Section: Methodsmentioning

confidence: 99%

“…The cell migration distances were calculated by ImageJ software. 24,25 100 μL of Matrigel (diluted with a ratio of 1:8 with MEM) was deposited in the upper chamber. After incubating at 37 °C for 3 h, the residual liquid was removed.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

Imperatorin-Loaded RH60/mPEG–PLLA Micelles for Reversing Tamoxifen Resistance in Breast Cancer

Li,

Zhao,

et al. 2024

ACS Appl. Nano Mater.

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“…Additionally, treatment with SPA70 and paclitaxel led to cells acquiring morphological features typical of necrotic ells, making it a promising treatment option for paclitaxel‐resistant NSCLC because it triggers necrosis (Table 6). 152 …”

Section: Small‐molecule Compounds Targeting Other Types Of Rcd For Th...mentioning

confidence: 99%

Targeted therapy for non‐small‐cell lung cancer: New insights into regulated cell death combined with immunotherapy

Li,

Wang,

et al. 2023

Immunological Reviews

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SummaryNon‐small‐cell lung cancer (NSCLC), which has a high rate of metastatic spread and drug resistance, is the most common subtype of lung cancer. Therefore, NSCLC patients have a very poor prognosis and a very low chance of survival. Human cancers are closely linked to regulated cell death (RCD), such as apoptosis, autophagy, ferroptosis, pyroptosis, and necroptosis. Currently, small‐molecule compounds targeting various types of RCD have shown potential as anticancer treatments. Moreover, RCD appears to be a specific part of the antitumor immune response; hence, the combination of RCD and immunotherapy might increase the inhibitory effect of therapy on tumor growth. In this review, we summarize small‐molecule compounds used for the treatment of NSCLC by focusing on RCD and pharmacological systems. In addition, we describe the current research status of an immunotherapy combined with an RCD‐based regimen for NSCLC, providing new ideas for targeting RCD pathways in combination with immunotherapy for patients with NSCLC in the future.

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Discovery of novel small molecules targeting the USP21/JAK2/STAT3 axis for the treatment of triple-negative breast cancer

Long,

Xu,

et al. 2024

European Journal of Medicinal Chemistry

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Combination of Paclitaxel and PXR Antagonist SPA70 Reverses Paclitaxel-Resistant Non-Small Cell Lung Cancer

Cited by 9 publications

References 57 publications

Imperatorin-Loaded RH60/mPEG–PLLA Micelles for Reversing Tamoxifen Resistance in Breast Cancer

Imperatorin-Loaded RH60/mPEG–PLLA Micelles for Reversing Tamoxifen Resistance in Breast Cancer

Targeted therapy for non‐small‐cell lung cancer: New insights into regulated cell death combined with immunotherapy

Discovery of novel small molecules targeting the USP21/JAK2/STAT3 axis for the treatment of triple-negative breast cancer

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