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Your search keyword '"Pei, Shaomeng"' showing total 2 results
Start Over Author "Pei, Shaomeng" Topic antineoplastic agents
2 results on '"Pei, Shaomeng"'

1. Synthesis and in vitro and in vivo antitumour activity study of 11-hydroxyl esterified bergenin/cinnamic acid hybrids.

Author

Liang C, Pei S, Ju W, Jia M, Tian D, Tang Y, and Mao G

Subjects
Animals, Antineoplastic Agents pharmacology, Apoptosis drug effects, Benzopyrans pharmacology, Caspase 3 metabolism, Caspase 9 metabolism, Cinnamates pharmacology, Esterification, Female, G2 Phase, Hep G2 Cells, Humans, Liver metabolism, Liver pathology, Liver Neoplasms metabolism, Liver Neoplasms pathology, Mice, Proto-Oncogene Proteins c-akt metabolism, Proto-Oncogene Proteins c-bcl-2 metabolism, Antineoplastic Agents chemistry, Antineoplastic Agents therapeutic use, Benzopyrans chemistry, Benzopyrans therapeutic use, Cinnamates chemistry, Cinnamates therapeutic use, Liver drug effects, Liver Neoplasms drug therapy
Abstract

Fourteen bergenin/cinnamic acid hybrids were synthesized, characterized and evaluated for their antitumour activity both in vitro and in vivo. The most potent compound, 5c, arrested HepG2 cells (IC 50  = 4.23 ± 0.79 μM) in the G2/M phase and induced cellular apoptosis. Moreover, compound 5c was also found to suppress the tumour growth in Heps xenograft-bearing mice with low toxicity. In the mechanistic study, 5c administration ignited a mitochondria-mediated apoptosis pathway of HepG2 cell death. Furthermore, 5c activated Akt-dependent pathways and further decreased the expression of the Bcl-2 family of proteins. The downstream mitochondrial p53 translocation was also significantly activated, accompanied by an increase of the caspase-9, caspase-3 activation. These data imply that bergenin/cinnamic acid hybrids could serve as novel Akt/Bcl-2 inhibitors for further preclinical studies., (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)

Published
2017
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2. Synthesis and in vitro and in vivo antitumour activity study of 11-hydroxyl esterified bergenin/cinnamic acid hybrids

Author

Pei Shaomeng, Tang Yonghong, Ju Weihui, Tian Danni, Liang Chengyuan, Gennian Mao, and Jia Minyi

Subjects
G2 Phase, 0301 basic medicine, Antineoplastic Agents, Apoptosis, Chromosomal translocation, 01 natural sciences, Cinnamic acid, Mice, 03 medical and health sciences, chemistry.chemical_compound, In vivo, Drug Discovery, Animals, Humans, Benzopyrans, Protein kinase B, Pharmacology, Esterification, Low toxicity, Caspase 3, 010405 organic chemistry, Liver Neoplasms, Organic Chemistry, Bergenin, Hep G2 Cells, General Medicine, Caspase 9, In vitro, 0104 chemical sciences, 030104 developmental biology, Liver, Proto-Oncogene Proteins c-bcl-2, chemistry, Biochemistry, Cinnamates, Female, Proto-Oncogene Proteins c-akt
Abstract

Fourteen bergenin/cinnamic acid hybrids were synthesized, characterized and evaluated for their antitumour activity both in vitro and in vivo. The most potent compound, 5c, arrested HepG2 cells (IC50 = 4.23 ± 0.79 μM) in the G2/M phase and induced cellular apoptosis. Moreover, compound 5c was also found to suppress the tumour growth in Heps xenograft-bearing mice with low toxicity. In the mechanistic study, 5c administration ignited a mitochondria-mediated apoptosis pathway of HepG2 cell death. Furthermore, 5c activated Akt-dependent pathways and further decreased the expression of the Bcl-2 family of proteins. The downstream mitochondrial p53 translocation was also significantly activated, accompanied by an increase of the caspase-9, caspase-3 activation. These data imply that bergenin/cinnamic acid hybrids could serve as novel Akt/Bcl-2 inhibitors for further preclinical studies.

Published
2017

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