Intercalating pyrene with polypeptide as a novel self-assembly nano-carrier for colon cancer suppression in vitro and in vivo

Lo, Pei Ying; Lee, Guang Yu; Zheng, Jia; Huang, Jen Hsien; Cho, Er Chieh; Lee, Kuen Chan

doi:10.1016/j.msec.2019.110593

Cited by 17 publications

(14 citation statements)

References 38 publications

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“…The tumor cells (1 × 10 6 tumor cells/mouse) were injected subcutaneously into the right thigh of the hind limb. After ten days of tumor cell inoculation, masses of A549 tumors began to appear, and the three inoculated groups were subsequently classified into a control group of A549 tumor cells without any treatment, a group inoculated with A549 cells and treated with the ethanolic crude extract of A. judaica L., and a group inoculated with A549 cells and treated with doxorubicin as a standard [ 36 ]. The third group was treated with a dose of 100 mg/Kg BW/IP/daily of A. judaica L. crude extract for seven days.…”

Section: Methodsmentioning

confidence: 99%

In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

et al. 2021

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Artemisia judaica L. (Family: Asteraceae) exhibited antioxidant, anti-inflammatory, and antiapoptotic effects. The in vitro cytotoxic activity of A. judaica ethanolic extract was screened against a panel of cancer cell lines. The results revealed its cytotoxic activity against a lung cancer (A549) cell line with a promising IC50 of 14.2 μg/mL compared to doxorubicin as a standard. This was confirmed through the downregulation of antiapoptotic genes, the upregulation of proapoptotic genes, and the cell cycle arrest at the G2/M phase. Further in vivo study showed that a solid tumor mass was significantly reduced, with a tumor inhibition ratio of 54% relative to doxorubicin therapy in a Xenograft model. From a chemical point of view, various classes of natural products have been identified by liquid chromatography combined with tandem mass spectrometry (LC-MS/MS). The docking study of the detected metabolites approved their cytotoxic activity through their virtual binding affinity towards the cyclin-dependent kinase 2 (CDK-2) and epidermal growth factor receptor (EGFR) active sites. Finally, A. judaica is a fruitful source of polyphenols that are well-known for their antioxidant and cytotoxic activities. As such, the previously reported polyphenols with anti-lung cancer activity were quantified by high-performance liquid chromatography coupled with a diode array detector (HPLC-DAD). Rutin, quercetin, kaempferol, and apigenin were detected at concentrations of 6 mg/gm, 0.4 mg/gm, 0.36 mg/gm, and 3.9 mg/gm of plant dry extract, respectively. It is worth noting that kaempferol and rutin are reported for the first time. Herein, A. judaica L. may serve as an adjuvant therapy or a promising source of leading structures in drug discovery for lung cancer treatment.

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Section: Methodsmentioning

confidence: 99%

In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

et al. 2021

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“…OD measurements were executed with an Eppendorf BioPhotometer plus. NMR spectra were recorded on a Bruker Avance 400 spectrometer (operating at 400 MHz for 1 H NMR and 101 MHz for 13 C NMR) in CHCl 3 -d with tetramethylsilane (TMS) as internal standard purchased by Carl Roth.…”

Section: Methodsmentioning

confidence: 99%

“…The following are available online at https://www.mdpi.com/article/10 .3390/biom12020153/s1, Figures S1-S6; HPLC profiles of fluorene, acenaphthene, 9-methylanthracene, azulene, pyrene, phenanthridine respectively, catalyzed by CYP3A4. Figures S7 and S8; 1 H and 13 C NMR Spectrum of fluorene. Figures S9 and S10; 1 H and 13 C NMR Spectrum of fluorenol.…”

Section: Supplementary Materialsmentioning

confidence: 99%

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Preparative Production of Functionalized (N- and O-Heterocyclic) Polycyclic Aromatic Hydrocarbons by Human Cytochrome P450 3A4 in a Bioreactor

et al. 2022

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Polycyclic aromatic hydrocarbons (PAHs) and their N- and O-containing derivatives (N-/O-PAHs) are environmental pollutants and synthetically attractive building blocks in pharmaceuticals. Functionalization of PAHs can be achieved via C-H activation by cytochrome P450 enzymes (e.g., P450 CYP3A4) in an environmentally friendly manner. Despite its broad substrate scope, the contribution of CYP3A4 to metabolize common PAHs in humans was found to be small. We recently showcased the potential of CYP3A4 in whole-cell biocatalysis with recombinant yeast Komagataella phaffii (Pichia pastoris) catalysts for the preparative-scale synthesis of naturally occurring metabolites in humans. In this study, we aimed at exploring the substrate scope of CYP3A4 towards (N-/O)-PAHs and conducted a bioconversion experiment at 10 L scale to validate the synthetic potential of CYP3A4 for the preparative-scale production of functionalized PAH metabolites. Hydroxylated products were purified and characterized using HPLC and NMR analysis. In total, 237 mg of fluorenol and 48 mg of fluorenone were produced from 498 mg of fluorene, with peak productivities of 27.7 μmol/L/h for fluorenol and 5.9 μmol/L/h for fluorenone; the latter confirmed that CYP3A4 is an excellent whole-cell biocatalyst for producing authentic human metabolites.

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“…Cell lines were seeded in 96 well plates for overnight, and then treated with different concentrations of the compounds for indicated time points. Cell viability was then analysed by MTT ((3–(4, 5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium-bromide) assay (Goldbio, St. Louis, MO) 27 with microplate spectrophotometer (BioTek Instruments, Winooski, VT). IC 50 was analysed and determined by SigmaPlot or Graphpad Prism software (GraphPad Software, La Jolla, CA).…”

Section: Methodsmentioning

confidence: 99%

Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors

Lin

Sung

Chao

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Bruton tyrosine kinase (BTK) is linked to multiple signalling pathways that regulate cellular survival, activation, and proliferation. A covalent BTK inhibitor has shown favourable outcomes for treating B cell malignant leukaemia. However, covalent inhibitors require a high reactive warhead that may contribute to unexpected toxicity, poor selectivity, or reduced effectiveness in solid tumours. Herein, we report the identification of a novel noncovalent BTK inhibitor. The binding interactions (i.e. interactions from known BTK inhibitors) for the BTK binding site were identified and incorporated into a structure-based virtual screening (SBVS). Top-rank compounds were selected and testing revealed a BTK inhibitor with >50% inhibition at 10 µM concentration. Examining analogues revealed further BTK inhibitors. When tested across solid tumour cell lines, one inhibitor showed favourable inhibitory activity, suggesting its potential for targeting BTK malignant tumours. This inhibitor could serve as a basis for developing an effective BTK inhibitor targeting solid cancers.

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Intercalating pyrene with polypeptide as a novel self-assembly nano-carrier for colon cancer suppression in vitro and in vivo

Cited by 17 publications

References 38 publications

In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

Preparative Production of Functionalized (N- and O-Heterocyclic) Polycyclic Aromatic Hydrocarbons by Human Cytochrome P450 3A4 in a Bioreactor

Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors

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