scholarly journals The Small Molecule Fractions of Floccularia luteovirens Induce Apoptosis of NSCLC Cells through Activating Caspase-3 Activity

2021 ◽  
Vol 22 (19) ◽  
pp. 10609
Author(s):  
Shuying Li ◽  
Jie Gao ◽  
Lizhen Hou ◽  
Yaxin Gao ◽  
Jing Sun ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Molecule ◽  
Caspase 3 ◽  
Tibet Plateau ◽  
Western Blot Assay ◽  
Molecular Weights ◽  
Medicinal Fungus ◽  
Potential Resource ◽  
Induced Apoptosis ◽  
Qinghai Tibet Plateau

Floccularia luteovirens is a rare wild edible and medicinal fungus endemic to the Qinghai-Tibet Plateau. In this study, the hollow fiber membranes with molecular weights of 50 kDa, 6 kDa and 3 kDa were used to extract different fractions of F. luteovirens, which were named as #1, #2 and #3. Then the antitumor activity of these fractions on NSCLC cell lines, PC9 and NCI-H460, were investigated by using MTT assay, flow cytometry analysis and Western blot assay. The results indicated that the #2 and #3 fractions showed obviously inhibitory activities on PC9 and NCI-H460 tumor cells and proved that these small molecule fractions induced apoptosis of NSCLC cells by activating caspase-3. Finally, a total of 15 components, including six amino acids, two nucleosides, two glycosides, two terpenoids, one phenylpropanoid, one ester and one alkaloid, were identified in #2 and #3 fractions. This is the first evidence that the small molecule components of F. luteovirens were able to inhibit lung cancer by inducing apoptosis in a caspase-3 manner. The present study indicated the benefits of F. luteovirens in lung cancer treatment, which might be a potential resource of functional food and drugs.

Overexpression of Smac Promotes Cisplatin-Induced Apoptosis by Activating Caspase-3 and Caspase-9 in Lung Cancer A549 Cells

2013 ◽  
Vol 28 (2) ◽  
pp. 177-182 ◽  
Author(s):  
Sida Qin ◽  
Chengcheng Yang ◽  
Xifang Wang ◽  
Chongwen Xu ◽  
Shuo Li ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Caspase 3 ◽  
A549 Cells ◽  
Caspase 9 ◽  
Induced Apoptosis

scholarly journals Screening for Caspase-3 Inhibitors: A New Class of Potent Small-Molecule Inhibitors of Caspase-3

2006 ◽  
Vol 11 (3) ◽  
pp. 277-285 ◽  
Author(s):  
Ilya Okun ◽  
Sergei Malarchuk ◽  
Elena Dubrovskaya ◽  
Alexander Khvat ◽  
Sergey Tkachenko ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput Screening ◽  
Caspase 3 ◽  
Small Molecule Inhibitors ◽  
High Potency ◽  
New Class ◽  
Mechanistic Analysis ◽  
Compound Collection ◽  
Induced Apoptosis

From the authors'650,000 compound collection, they have selected approximately 15,000 potential small-molecule protease inhibitors, which were subjected to high-throughput screening against caspase-3. The screening yielded a series of hits that belong to 11 different scaffolds. Based on the structure of one of the hits, a new class of the small-molecule inhibitors with a double electrophilicwarhead, 8-sulfonyl-pyrrolo[3,4-c]quinoline-1,3-diones (SPQ), was synthesized and tested in follow-up mechanistic and antiapoptosis assays. Mechanistic analysis of a representative compound of this class, CD-001-0011, showed that the compound exhibited a high potency (IC 50 = 130 nM), was reversible though noncompetitive, and had a broad selectivity profile to other caspases belonging to groups I to III. The compound was effective in preventing staurosporineinduced apoptosis in a few cell lines and retinoic acid–induced apoptosis in zebrafish.

Synthesis of 5-Alkynyltetrandrine Derivatives and Evaluation of their Anticancer Activity on A549 Cell Lines

2019 ◽  
Vol 19 (12) ◽  
pp. 1454-1462 ◽  
Author(s):  
Nana Niu ◽  
Tingli Qu ◽  
Jinfang Xu ◽  
Xiaolin Lu ◽  
Graham J. Bodwell ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Caspase 3 ◽  
Human Lung ◽  
A549 Cells ◽  
Human Lung Cancer ◽  
Coupling Reactions ◽  
Apoptotic Pathway ◽  
Future Design ◽  
Cyt C ◽  
Induced Apoptosis

Background: Lung cancer is one of the most prevalent malignancies and thus the development of novel therapeutic agents for managing lung cancer is imperative. Tetrandrine, a bis-benzyltetrahydroisoquinoline alkaloid isolated from Stephania tetrandra S. Moore, has been found to exert cytotoxic effects on cancerous cells. Methods: A series of 5-alkynyltetrandrine derivatives was synthesized via the Sonogashira cross-coupling reactions and evaluated as potential anti-tumor agents. The anti-tumor activities of 12 compounds on lung cancer cells (A549) were evaluated using the MTT method. The population of apoptotic cells was measured using a TUNEL assay. Real-time PCR quantified the gene expression levels of Bcl-2, Bax, survivin and caspase-3. The content of Cyt-C was detected using a Human Cyt-C ELISA kit. Results: Most of these compounds exhibited better activities than tetrandrine itself on A549 cells. Among them, compound 7 showed the highest cytotoxicity among the tested compounds against human lung adenocarcinoma A549 cells with an IC50 of 2.94 µM. Preliminary mechanistic studies indicated that compound 7 induced apoptosis of human lung cancer A549 cells and increased the level of the proapoptotic gene Bax, release of Cyt-C from mitochondria and activation of caspase-3 genes. Conclusion: The results suggest that compound 7 exerts its antitumor activity against A549 cells through the induction of the intrinsic (mitochondrial) apoptotic pathway. These findings will contribute to the future design of more effective anti-tumor agents in lung cancer therapy.

scholarly journals Involvement of Bim in Photofrin-Mediated Photodynamically Induced Apoptosis

2015 ◽  
Vol 35 (4) ◽  
pp. 1527-1536 ◽  
Author(s):  
Xianwang Wang ◽  
Xiaobing He ◽  
Shujuan Hu ◽  
Anbang Sun ◽  
Chengbiao Lu
Keyword(s):  
Lung Adenocarcinoma ◽  
Caspase 3 ◽  
Photodynamic Treatment ◽  
Western Blot Assay ◽  
Noninvasive Technique ◽  
Human Cancers ◽  
Confocal Scanning ◽  
Potential Strategy ◽  
Induced Apoptosis ◽  
In Cells

Background/Aims: Photodynamic therapy (PDT) is a promising noninvasive technique, which has been successfully applied to the treatment of human cancers. Studies have shown that the Bcl-2 family proteins play important roles in PDT-induced apoptosis. However, whether Bcl-2-interacting mediator of cell death (Bim) is involved in photodynamic treatment remains unknown. In this study, we attempt to determine the effect of Bim on Photofrin photodynamic treatment (PPT)-induced apoptosis in human lung adenocarcinoma ASTC-a-1 cells. Methods: The translocation of Bim/Bax of the cells were monitored by laser confocal scanning microscope. The levels of Bim protein and activated caspase-3 in cells were detected by western blot assay. Caspase-3 activities were measured by Caspase-3 Fluorogenic Substrate (Ac-DEVD-AFC) analysis. The induction of apoptosis was detected by Hoechst 33258 and PI staining as well as flow cytometry analysis. The effect of Bim on PPT-induced apoptosis was determined by RNAi. Results: BimL translocated to mitochondria in response to PPT, similar to the downstream pro-apoptotic protein Bax activation. PPT increased the level of Bim and activated caspase-3 in cells and that knockdown of Bim by RNAi significantly protected against caspase-3 activity. PPT-induced apoptosis were suppressed in cells transfected with shRNA-Bim. Conclusion: We demonstrated the involvement of Bim in PPT-induced apoptosis in human ASTC-a-1 lung adenocarcinoma cells and suggested that enhancing Bim activity might be a potential strategy for treating human cancers.

scholarly journals β-Elemene Triggers ROS-dependent Apoptosis in Glioblastoma Cells Through Suppressing STAT3 Signaling Pathway

2021 ◽  
Vol 27 ◽  
Author(s):  
Shi-zhong Cai ◽  
Qian-wei Xiong ◽  
Li-na Zhao ◽  
Yi-ting Ji ◽  
Zheng-xiang Luo ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Caspase 3 ◽  
Treatment Strategies ◽  
Oxygen Species ◽  
Glioblastoma Cells ◽  
Western Blot Assay ◽  
Stat3 Signaling ◽  
Stat3 Signaling Pathway ◽  
Apoptotic Activity ◽  
Induced Apoptosis

Glioblastoma is one of the most aggressive primary brain tumors with few treatment strategies. β-Elemene is a sesquiterpene known to have broad spectrum antitumor activity against various cancers. However, the signaling pathways involved in β-elemene induced apoptosis of glioblastoma cells remains poorly understood. In this study, we reported that β-elemene exhibited antiproliferative activity on U87 and SHG-44 cells, and induced cell death through induction of apoptosis. Incubation of these cells with β-elemene led to the activation of caspase-3 and generation of reactive oxygen species (ROS). Western blot assay showed that β-elemene suppressed phosphorylation of STAT3, and subsequently down-regulated the activation of p-JAK2 and p-Src. Moreover, pre-incubation of cells with ROS inhibitor N-acetyl-L-cysteine (NAC) significantly reversed β-elemene-mediated apoptosis effect and down-regulation of JAK2/Src-STAT3 signaling pathway. Overall, our findings implied that generation of ROS and suppression of STAT3 signaling pathway is critical for the apoptotic activity of β-elemene in glioblastoma cells.

Involvement of Caspase-3 Activity and Survivin Downregulation in Cinobufocini-Induced Apoptosis in A 549 Cells

2009 ◽  
Vol 234 (5) ◽  
pp. 566-572 ◽  
Author(s):  
Juyong Wang ◽  
Ye Jin ◽  
Zhenye Xu ◽  
Zhan Zheng ◽  
Su Wan
Keyword(s):  
Caspase 3 ◽  
Human Lung ◽  
Water Soluble ◽  
Dependent Manner ◽  
Survivin Mrna ◽  
Toad Skin ◽  
Western Blot Assay ◽  
Human Lung Fibroblast ◽  
Caspase 7 ◽  
Induced Apoptosis

Cinobufocini injection is a preparation containing water-soluble components of the toad skin. The aim of the present study was to investigate the apoptosis of human lung adenocarcinoma cell line A 549 induced by cinobufocini. A 549 or HLF-1(human lung fibroblast) cells were treated with cinobufocini at different concentrations for 24 and 48 h, respectively. The proliferation of cells was detected with the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay. Morphology of cells was carried out with scanning electronic microscopy (SEM) and Hoechst 33258 staining. The apoptosis rate was examined by flow cytometry. The expression of survivin was examined with RT-PCR and Western blot assay. The caspase-3 and caspase-7 activities were detected with caspase colorimetric protease assay. We found that cinobufocini significantly inhibited tumor growth of A 549 cells in a dose- and time-dependent manner without damaging non-cancerous cells (HLF-1) and induced granular apoptotic bodies of A 549 cells. Next, cinobufocini increased the percentage of cells in G1 phase and decreased the percentage of cells in S phase in A 549 cells. Furthermore, cinobufocini downregulated the expression of survivin mRNA and protein. Finally, cinobufocini upregulated caspase-3 activity. We concluded that cinobufocini induces apoptosis of A 549 cells, which is associated with the decreasing expression of survivin mRNA and protein, increasing caspase-3 activity of A 549 cells.

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