Mechanistic studies of ipomoeassin F for its cell growth inhibition activity

Study of the chemical constituents of the stems of Garcinia schomburgkiana Pierre (Guttiferae), collected in Thailand, led to the isolation and identification of five known compounds and two new biphenyl derivatives, schomburgbiphenyl A (1) and B (2). Six phenolic compounds isolated from this plant were screened for their cell growth inhibition activity using several human leukemia cell lines. One compound, oblongifolin C (7), showed significant cytotoxic activity towards Jurkat, NALM6, K562 and HPB-ALL cells.

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One-pot, multi-component synthesis of novel 2-amino-[1,2,4]triazolo[1,5-a] pyrimidine-6-carboxamide derivatives as antiproliferative agents

10.21203/rs.3.rs-182311/v1 ◽

2021 ◽

Author(s):

Xian-Sen Huo ◽

Yu-Feng Ma ◽

Zhi-Ru Chen ◽

Li-Li Yuan ◽

Xiao-Lan Zheng ◽

...

Keyword(s):

Cell Growth ◽

Cancer Cells ◽

Anticancer Agents ◽

Inhibition Activity ◽

Cell Growth Inhibition ◽

Cancer Cell Growth ◽

One Pot ◽

Antiproliferative Agents ◽

Heterocyclization Reaction ◽

Growth Inhibition Activity

Abstract A novel series of 2-amino-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxamide derivatives has been achieved successfully via an efficient one-pot three-component Biginelli-like heterocyclization reaction between different benzaldehydes, 1H-1,2,4-triazole-3,5-diamine, and N-substituted acetoacetamides in the presence of p-toluenesulfonic acid as a catalyst. Moreover, the effects of different conditions on the reaction were well investigated. In addition, cancer cell growth inhibition activity for these target compounds was also explored, and analogue 5l demonstrated the most potent cytotoxic activity against different cancer cells. These finds indicat that 2-amino-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxamide core could be well worth further optimization as a potential scaffold for development of anticancer agents.

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Jab1-siRNA Induces Cell Growth Inhibition and Cell Cycle Arrest in Gall Bladder Cancer Cells via Targeting Jab1 Signalosome

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190725122400 ◽

2020 ◽

Vol 19 (16) ◽

pp. 2019-2033 ◽

Cited By ~ 2

Author(s):

Pratibha Pandey ◽

Mohammad H. Siddiqui ◽

Anu Behari ◽

Vinay K. Kapoor ◽

Kumudesh Mishra ◽

...

Keyword(s):

Cell Cycle ◽

Bladder Cancer ◽

Cell Growth ◽

Gall Bladder ◽

Growth Inhibition ◽

Cell Cycle Arrest ◽

Gall Bladder Cancer ◽

Cell Growth Inhibition ◽

Cycle Arrest ◽

Apoptotic Induction

Background: The aberrant alteration in Jab1 signalosome (COP9 Signalosome Complex Subunit 5) has been proven to be associated with the progression of several carcinomas. However the specific role and mechanism of action of Jab1 signalosome in carcinogenesis of gall bladder cancer (GBC) are poorly understood. Objective: The main objective of our study was to elucidate the role and mechanism of Jab1 signalosome in gall bladder cancer by employing siRNA. Methods: Jab1 overexpression was identified in gall bladder cancer tissue sample. The role of Jab1-siRNA approach in cell growth inhibition and apoptotic induction was then examined by RT-PCR, Western Blotting, MTT, ROS, Hoechst and FITC/Annexin-V staining. Results: In the current study, we have shown that overexpression of Jab1 stimulated the proliferation of GBC cells; whereas downregulation of Jab1 by using Jab1-siRNA approach resulted incell growth inhibition and apoptotic induction. Furthermore, we found that downregulation of Jab1 induces cell cycle arrest at G1 phase and upregulated the expression of p27, p53 and Bax gene. Moreover, Jab1-siRNA induces apoptosis by enhancing ROS generation and caspase-3 activation. In addition, combined treatment with Jab1-siRNA and gemicitabine demonstrated an enhanced decline in cell proliferation which further suggested increased efficacy of gemcitabine at a very lower dose (5μM) in combination with Jab1-siRNA. Conclusion: In conclusion, our study strongly suggests that targeting Jab1 signalosome could be a promising therapeutic target for the treatment of gall bladder cancer.

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Structural and multifunctional properties of cardiac fatty acid-binding protein: from fatty acid binding to cell growth inhibition

Biochemical Society Transactions ◽

10.1042/bst0200806 ◽

1992 ◽

Vol 20 (4) ◽

pp. 806-811 ◽

Cited By ~ 12

Author(s):

F. Spener ◽

T. Börchers

Keyword(s):

Fatty Acid ◽

Cell Growth ◽

Growth Inhibition ◽

Fatty Acid Binding Protein ◽

Binding Protein ◽

Cell Growth Inhibition ◽

Fatty Acid Binding ◽

Acid Binding Protein ◽

Multifunctional Properties

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Effect of β-carotene-rich tomato lycopene β-cyclase (tlcy-b) on cell growth inhibition in HT-29 colon adenocarcinoma cells

British Journal Of Nutrition ◽

10.1017/s0007114508169902 ◽

2008 ◽

Vol 102 (2) ◽

pp. 207-214 ◽

Cited By ~ 15

Author(s):

Paola Palozza ◽

Diana Bellovino ◽

Rossella Simone ◽

Alma Boninsegna ◽

Francesco Cellini ◽

...

Keyword(s):

Cell Growth ◽

Growth Inhibition ◽

Colon Adenocarcinoma ◽

Human Colon ◽

Cell Growth Inhibition ◽

Adenocarcinoma Cells ◽

Ht 29 ◽

Colon Adenocarcinoma Cells ◽

Β Carotene

Lycopene β-cyclase (tlcy-b) tomatoes, obtained by modulating carotenogenesis via genetic engineering, contain a large amount of β-carotene, as clearly visible by their intense orange colour. In the present study we have subjected tlcy-b tomatoes to an in vitro simulated digestion and analysed the effects of digestate on cell proliferation. To this aim we used HT-29 human colon adenocarcinoma cells, grown in monolayers, as a model. Digested tomatoes were diluted (20 ml, 50 ml and 100 ml/l) in culture medium and added to the cells for different incubation times (24 h, 48 h and 72 h). Inhibition of cell growth by tomato digestate was dose-dependent and resulted from an arrest of cell cycle progression at the G0/G1 and G2/M phase and by apoptosis induction. A down-regulation of cyclin D1, Bcl-2 and Bcl-xl expression was observed. We also found that heat treatment of samples before digestion enhanced β-carotene release and therefore cell growth inhibition. To induce with purified β-carotene solubilised in tetrahydrofuran the same cell growth inhibition obtained with the tomato digestate, a higher amount of the carotenoid was necessary, suggesting that β-carotene micellarised during digestion is utilised more efficiently by the cells, but also that other tomato molecules, reasonably made available during digestion, may be present and cooperate with β-carotene in promoting cell growth arrest.

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