scholarly journals Synthesis and potent cytotoxic activity of diosgenin derivative FZU-0021-194-P2 and its phytosomes against non-small-cell lung cancer cells

2019 ◽  
Author(s):  
Liang Xu ◽  
Dekang Xu ◽  
Ziying Li ◽  
Yu Gao ◽  
Haijun Chen
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Water Solubility ◽  
Antitumor Agents ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Cytotoxic Activities ◽  
Small Cell Lung

Diosgenin (Di), a steroidal sapogenin derived from plants, has been shown to exert anti-cancer effects in preclinical studies. Using Di as a starting material, various Di derivatives were designed and synthesized, aiming to discover new steroid-based antitumor agents. In this work, we synthesized several Di derivatives and screened FZU-0021-194-P2 (P2), which showed more potent cytotoxic activities against human non-small-cell lung cancer A549 and PC9 cells. Considering that Di has a unique sterol structure similarly to cholesterol, P2 phytosomes (P2P) were prepared to further improve the water solubility of P2. P2P exhibited a particle size of 53.6 ± 0.3 nm with oval shape and a zeta potential of −4.0 ± 0.7 mV. P2P could inhibit the proliferation of lung cancer cells more efficiently than Di phytosomes with 72-h incubation time through the mechanism of inducing cell cycle arrest and apoptosis. The results indicated that P2P could be a promising anticancer formulation for non-small-cell lung cancer.

scholarly journals Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells

2019 ◽  
Vol 10 ◽  
pp. 1933-1942 ◽  
Author(s):  
Liang Xu ◽  
Dekang Xu ◽  
Ziying Li ◽  
Yu Gao ◽  
Haijun Chen
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Water Solubility ◽  
Antitumor Agents ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Cytotoxic Activities ◽  
Small Cell Lung

Diosgenin (Di), a steroidal sapogenin derived from plants, has been shown to exert anticancer effects in preclinical studies. Using Di as a starting material, various Di derivatives were designed and synthesized, aiming to discover new steroid-based antitumor agents. In this work, we synthesized several Di derivatives and screened FZU-0021-194-P2 (P2), which showed more potent cytotoxic activities against human non-small-cell lung cancer A549 and PC9 cells. Considering that Di has a unique sterol structure similarly to cholesterol, P2 phytosomes (P2Ps) were prepared to further improve the water solubility of P2. The P2Ps exhibited a particle size of 53.6 ± 0.3 nm with oval shape and a zeta potential of −4.0 ± 0.7 mV. P2Ps could inhibit the proliferation of lung cancer cells more efficiently than Di phytosomes after 72 h of incubation time by inducing cell cycle arrest and apoptosis. The results indicated that P2Ps could be a promising anticancer formulation for non-small-cell lung cancer.

scholarly journals Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells

2021 ◽  
Vol 36 (1) ◽  
pp. 987-999
Author(s):  
Mohammad M. Al-Sanea ◽  
Ghada H. Al-Ansary ◽  
Zainab M. Elsayed ◽  
Raed M. Maklad ◽  
Eslam B. Elkaeed ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Antitumor Agents ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Small Cell Lung

Paeonol Inhibits Migration, Invasion and Bone Adhesion of Small Cell Lung Cancer Cells

2015 ◽  
Vol 10 (2) ◽  
pp. 126-130
Author(s):  
Yong Tian ◽  
Cong Chen ◽  
Yu Zhang ◽  
Zhen Zhang ◽  
Haiyan Xie
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Small Cell Lung

scholarly journals Melatonin Downregulates PD-L1 Expression and Modulates Tumor Immunity in KRAS-Mutant Non-Small Cell Lung Cancer

2021 ◽  
Vol 22 (11) ◽  
pp. 5649
Author(s):  
Yi-Chun Chao ◽  
Kang-Yun Lee ◽  
Sheng-Ming Wu ◽  
Deng-Yu Kuo ◽  
Pei-Wei Shueng ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Tumor Immunity ◽  
Cell Lung Cancer ◽  
Kras Mutation ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Small Cell Lung ◽  
Syngeneic Mouse Model

Non-small cell lung cancer (NSCLC) patients harboring a KRAS mutation have unfavorable therapeutic outcomes with chemotherapies, and the mutation also renders tolerance to immunotherapies. There is an unmet need for a new strategy for overcoming immunosuppression in KRAS-mutant NSCLC. The recently discovered role of melatonin demonstrates a wide spectrum of anticancer impacts; however, the effect of melatonin on modulating tumor immunity is largely unknown. In the present study, melatonin treatment significantly reduced cell viability accompanied by inducing cell apoptosis in KRAS-mutant NSCLC cell lines including A549, H460, and LLC1 cells. Mechanistically, we found that lung cancer cells harboring the KRAS mutation exhibited a higher level of programmed death ligand 1 (PD-L1). However, treatment with melatonin substantially downregulated PD-L1 expressions in both the presence and absence of interferon (IFN)-γ stimulation. Moreover, KRAS-mutant lung cancer cells exhibited higher Yes-associated protein (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ) levels, and PD-L1 expression was positively correlated with YAP and TAZ in lung cancer cells. Treatment with melatonin effectively suppressed YAP and TAZ, which was accompanied by downregulation of YAP/TAZ downstream gene expressions. The combination of melatonin and an inhibitor of YAP/TAZ robustly decreased YAP and PD-L1 expressions. Clinical analysis using public databases revealed that PD-L1 expression was positively correlated with YAP and TAZ in patients with lung cancer, and PD-L1 overexpression suggested poor survival probability. An animal study further revealed that administration of melatonin significantly inhibited tumor growth and modulated tumor immunity in a syngeneic mouse model. Together, our data revealed a novel antitumor mechanism of melatonin in modulating the immunosuppressive tumor microenvironment by suppressing the YAP/PD-L1 axis and suggest the therapeutic potential of melatonin for treating NSCLC.

miR‐155‐5p and miR‐760 mediate radiation therapy suppressed malignancy of non‐small cell lung cancer cells

BioFactors ◽  
2019 ◽  
Vol 45 (3) ◽  
pp. 393-400 ◽  
Author(s):  
Lin Zhu ◽  
Feng Xue ◽  
Ying Cui ◽  
Shanshan Liu ◽  
Gen Li ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Radiation Therapy ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Small Cell Lung
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