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Your search keyword '"Chai, Kequn"' showing total 5 results
Start Over Author "Chai, Kequn" Search Limiters Peer Reviewed Topic antineoplastic agents
5 results on '"Chai, Kequn"'

1. Myricanol induces apoptotic cell death and anti-tumor activity in non-small cell lung carcinoma in vivo.

Author

Dai G, Tong Y, Chen X, Ren Z, Ying X, Yang F, and Chai K

Subjects
Animals, Antineoplastic Agents chemistry, Antineoplastic Agents therapeutic use, Carcinoma, Non-Small-Cell Lung drug therapy, Carcinoma, Non-Small-Cell Lung metabolism, Carcinoma, Non-Small-Cell Lung pathology, Cell Line, Tumor, Diarylheptanoids chemistry, Diarylheptanoids therapeutic use, Humans, Hypoxia-Inducible Factor 1, alpha Subunit genetics, Hypoxia-Inducible Factor 1, alpha Subunit metabolism, Immunohistochemistry, Inhibitor of Apoptosis Proteins genetics, Inhibitor of Apoptosis Proteins metabolism, Lung Neoplasms drug therapy, Lung Neoplasms metabolism, Lung Neoplasms pathology, Mice, Mice, Nude, Polyethylene Glycols chemistry, Survivin, Up-Regulation drug effects, Vascular Endothelial Growth Factor A genetics, Vascular Endothelial Growth Factor A metabolism, Xenograft Model Antitumor Assays, bcl-2-Associated X Protein genetics, bcl-2-Associated X Protein metabolism, Antineoplastic Agents pharmacology, Apoptosis drug effects, Diarylheptanoids pharmacology
Abstract

This study explored the inhibiting effect and mechanism of myricanol on lung adenocarcinoma A549 xenografts in nude mice. Forty nude mice with subcutaneous A549 xenografts were randomly divided into five groups: high-dose myricanol (40 mg/kg body weight) group; middle-dose myricanol (20 mg/kg body weight) group; low-dose myricanol (10 mg/kg body weight) group; polyethylene glycol 400 vehicle group (1 mL/kg); and tumor model group. Nude mice were sacrificed after 14 days of treatment and the tumor inhibition rate (TIR, %) was then calculated. The relative mRNA expression levels of Bax, Bcl-2, VEGF, HIF-1α, and survivin in the tumor tissues were determined by real-time PCR. TUNEL assay was applied to determine cellular apoptosis, while IHC test was performed to detect the protein expression levels of Bax, Bcl-2, VEGF, HIF-1α, and survivin. The TIR of the three myricanol-treated groups ranged from 14.9% to 38.5%. The IHC results showed that the protein expression of Bcl-2, VEGF, HIF-1α, and survivin were consistently downregulated, whereas that of Bax was upregulated after myricanol treatment. Myricanol also significantly upregulated the mRNA expression of Bax and downregulated that of Bcl-2, VEGF, HIF-1α, and survivin in a dose-dependent manner (p < 0.05 to 0.001). These results are consistent with those of IHC. The TUNEL assay results indicated that apoptotic-positive cells significantly increased in the myricanol-treated tumor tissues compared with the cells of the vehicle control group (p < 0.01 to 0.001). These data suggest that myricanol could significantly decelerate tumor growth in vivo by inducing apoptosis.

Published
2015
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2. Myricanol 5-fluorobenzyloxy ether regulation of survivin pathway inhibits human lung adenocarcinoma A549 cells growth in vitro

Author

Xuan Chen, Yeling Tong, Ren Zeming, Chai Kequn, Dai Guanhai, and Chen-jie Dai

Subjects
Cell growth inhibition, Lung Neoplasms, Survivin, Poly ADP ribose polymerase, Population, Down-Regulation, Adenocarcinoma of Lung, Antineoplastic Agents, Cell Movement, Diarylheptanoids, Cell Line, Tumor, Humans, Human lung adenocarcinoma A549, education, Cytotoxicity, Cell Proliferation, Membrane Potential, Mitochondrial, A549 cell, education.field_of_study, Chemistry, Cell Cycle, Cell migration, lcsh:Other systems of medicine, Antitumor, Cell cycle, lcsh:RZ201-999, Myricanol 5-fluorobenzyloxy ether, Up-Regulation, Survivin pathway, Complementary and alternative medicine, A549 Cells, Apoptosis, Cancer research, Mitochondrial membrane potential, Research Article
Abstract

Background This study aimed to explore the growth inhibitory effect of myricanol 5-fluorobenzyloxy ether (5FEM) and its underlying mechanisms in human lung adenocarcinoma A549 cells in vitro. Methods 5FEM was obtained by the chemical modification of myricanol with fluorobenzyloxy ether at the OH(5) position. The cytotoxicity, cell apoptosis, cell cycle, mitochondrial membrane potential (ΔΨm), scratch test, colony formation, and the expression levels of the key survivin pathway-related genes in A549 were evaluated. Results 5FEM could significantly inhibit A549 cell growth; induce cell apoptosis; increase G0/G1 population; reduce ΔΨm; inhibit cell migration and colony formation; upregulate caspase-9, P21, and Bax expression levels; and downregulate PARP, survivin, and Bcl-2 expression level. Conclusion These results enhanced our understanding of 5FEM and aid the discovery of novel myricanol derivatives as potential antitumor agents.

Published
2020

3. The mechanistic antitumor study of myricanol 5-fluorobenzyloxy ether in human leukemic cell HL-60

Author

Chen-Jie Fan, Zeming Ren, Zhen-Hua Li, Xuan Chen, Dai Guanhai, Xiao-Jing Nie, Chai Kequn, and Yeling Tong

Subjects
Cyclin-Dependent Kinase Inhibitor p21, 0301 basic medicine, Fas Ligand Protein, Cell, Population, Down-Regulation, Antineoplastic Agents, Apoptosis, HL-60 Cells, Biology, Ether, Fas ligand, 03 medical and health sciences, 0302 clinical medicine, Downregulation and upregulation, Diarylheptanoids, Drug Discovery, Survivin, medicine, Humans, fas Receptor, Cytotoxicity, education, bcl-2-Associated X Protein, Pharmacology, education.field_of_study, Leukemia, Cell cycle, Caspase 9, Up-Regulation, Cell biology, G2 Phase Cell Cycle Checkpoints, 030104 developmental biology, medicine.anatomical_structure, Proto-Oncogene Proteins c-bcl-2, 030220 oncology & carcinogenesis, Cancer research, M Phase Cell Cycle Checkpoints, Molecular Medicine
Abstract

Aim: The aim of the study was to explore the growth inhibitory effect of myricanol 5-fluorobenzyloxy ether (5FEM) and the underlying mechanism in human leukemic cells HL-60. Materials & methods: 5FEM was obtained by chemical modification of myricanol with fluorobenzyloxy ether at the OH(5) position. The cytotoxicity, cell apoptosis, cell cycle and the expression of key apoptosis-related genes in HL-60 were evaluated. Results & conclusion: 5FEM can significantly inhibited growth of HL-60 cells, increased the G2/M population and upregulated the expression of Bax, Fas, FasL, caspase-9 and p21 and downregulated that of Bcl-2 and survivin. The results enhance our understanding of 5FEM and aid the discovery of novel myricanol derivatives as potential antitumor agents.

Published
2017

4. Differential Metabolomics and Network Pharmacology Analysis of Silkworm Biotransformation between Mulberry Leaves and Silkworm Droppings.

Author

Li, Mingqian, Chen, Lin, Dai, Yuntao, Li, Jiacheng, Li, Fei, Li, Qun, Yu, Zhihong, Chai, Kequn, and Zhu, Yongqiang

Subjects
FECAL analysis, UNSATURATED fatty acids, HIGH performance liquid chromatography, PHARMACOLOGY, METABOLOMICS, ANIMAL experimentation, METABOLISM, ANTIVIRAL agents, ANTINEOPLASTIC agents, MOTHS, GAS chromatography, CELLULAR signal transduction, LEAVES, MASS spectrometry, GENES, LYSINE, BIOTRANSFORMATION (Metabolism), PEPTIDES
Abstract

Silkworm droppings are the product of mulberry leaves digested by silkworm intestines, which are an important medicinal resource in traditional Chinese medicine (TCM). The contents of total fat, fat acids, crude protein, amino acids, and secondary metabolites of obtained mulberry leaves and silkworm droppings were analyzed by HPLC, GC-MS, and UHPLC-Q-TOF MS. The target genes and enriched pathways related to significantly changed compositions between mulberry leaves and silkworm droppings were analyzed by network pharmacology. High unsaturated C18 : 3 fatty acids were transformed to low unsaturated C18 : 1 from mulberry leaves to silkworm droppings. Only lysine and 17 mini-peptides had significantly higher content in silkworm droppings than in mulberry leaves. There were 36 common target genes or the different compounds between mulberry leaves and silkworm droppings. The main pathways of mulberry leaf were enriched in antivirus and anticancer properties, while the pathways of silkworm droppings were enriched in hormone regulation and signal transduction. [ABSTRACT FROM AUTHOR]

Published
2021
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5. Myricanol Induces Apoptotic Cell Death and Anti-Tumor Activity in Non-Small Cell Lung Carcinoma in Vivo

Author

Xuhua Ying, Feng Yang, Xuan Chen, Zeming Ren, Dai Guanhai, Yeling Tong, and Chai Kequn

Subjects
Vascular Endothelial Growth Factor A, Lung Neoplasms, Survivin, Apoptosis, Inhibitor of Apoptosis Proteins, Polyethylene Glycols, lcsh:Chemistry, Mice, Carcinoma, Non-Small-Cell Lung, lcsh:QH301-705.5, Spectroscopy, bcl-2-Associated X Protein, TUNEL assay, biology, General Medicine, respiratory system, Immunohistochemistry, Computer Science Applications, Up-Regulation, Vascular endothelial growth factor A, Adenocarcinoma, Mice, Nude, Antineoplastic Agents, anticancer, Catalysis, Article, Inorganic Chemistry, Bcl-2-associated X protein, In vivo, Diarylheptanoids, Cell Line, Tumor, medicine, myricanol, Animals, Humans, Physical and Theoretical Chemistry, Molecular Biology, Organic Chemistry, medicine.disease, Hypoxia-Inducible Factor 1, alpha Subunit, Molecular biology, A549 xenograft, Xenograft Model Antitumor Assays, respiratory tract diseases, lcsh:Biology (General), lcsh:QD1-999, biology.protein
Abstract

This study explored the inhibiting effect and mechanism of myricanol on lung adenocarcinoma A549 xenografts in nude mice. Forty nude mice with subcutaneous A549 xenografts were randomly divided into five groups: high-dose myricanol (40 mg/kg body weight) group, middle-dose myricanol (20 mg/kg body weight) group, low-dose myricanol (10 mg/kg body weight) group, polyethylene glycol 400 vehicle group (1 mL/kg), and tumor model group. Nude mice were sacrificed after 14 days of treatment and the tumor inhibition rate (TIR, %) was then calculated. The relative mRNA expression levels of Bax, Bcl-2, VEGF, HIF-1α, and survivin in the tumor tissues were determined by real-time PCR. TUNEL assay was applied to determine cellular apoptosis, while IHC test was performed to detect the protein expression levels of Bax, Bcl-2, VEGF, HIF-1α, and survivin. The TIR of the three myricanol-treated groups ranged from 14.9% to 38.5%. The IHC results showed that the protein expression of Bcl-2, VEGF, HIF-1α, and survivin were consistently downregulated, whereas that of Bax was upregulated after myricanol treatment. Myricanol also significantly upregulated the mRNA expression of Bax and downregulated that of Bcl-2, VEGF, HIF-1α, and survivin in a dose-dependent manner (p &lt, 0.05 to 0.001). These results are consistent with those of IHC. The TUNEL assay results indicated that apoptotic-positive cells significantly increased in the myricanol-treated tumor tissues compared with the cells of the vehicle control group (p &lt, 0.01 to 0.001). These data suggest that myricanol could significantly decelerate tumor growth in vivo by inducing apoptosis.

Published
2015

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