Efficient extraction and purification of benzo[ c ]phenanthridine alkaloids from Macleaya cordata (Willd) R. Br. by combination of ultrahigh pressure extraction and pH‐zone‐refining counter‐current chromatography with anti‐breast cancer activity in vitro

2020 ◽  
Author(s):  
Iftikhar Ali ◽  
Jingchao Li ◽  
Li Cui ◽  
Hongwei Zhao ◽  
Qiuxia He ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Ultrahigh Pressure ◽  
Zone Refining ◽  
Extraction And Purification ◽  
Pressure Extraction ◽  
Efficient Extraction ◽  
Macleaya Cordata ◽  
Counter Current ◽  
Cancer Activity

Coumarin-Fatty Acid Conjugates as Potential ERα/AKT-1 Antagonists for ER Positive Breast Cancer

2020 ◽  
Vol 20 (4) ◽  
pp. 437-449
Author(s):  
Jubie Selvaraj ◽  
Jameera B.A. John ◽  
Nanjan M. Joghee ◽  
Justin Antony ◽  
Ashish Wadhwani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Gene Expression ◽  
Fatty Acid ◽  
Binding Assay ◽  
Uterine Cancer ◽  
Design Development ◽  
Structure Based Drug Design ◽  
Ic50 Values ◽  
Cancer Activity

Background: : Current drugs used for the treatment of hormone-dependent breast cancer function as anti-estrogens in the breast, in addition to Estrogen Receptor (ER) agonists in the uterus, thus elevate a woman’s risk of developing uterine cancer. This is due to the lack of selective binding and partial agonistic effect of these drugs towards estrogen receptors. In recent years, therefore, researchers have turned their attention towards antiestrogens devoid of these agonist properties and thus have a mechanism of action different from the existing drugs. Objective:: In this context, we report here the design, development and in vitro evaluation of some novel pharmacophores containing coumarin and fatty acid scaffolds for their anti-breast cancer activity. Methods: : A library of coumarin-fatty acid conjugates was designed using structure-based drug design approach. The conjugates which have shown good in silico results were then synthesized, characterized and evaluated for their anti-breast cancer activity by MTT assay, Apoptotic assay, Cell proliferation assay, Estrogen binding assay and Gene expression study. Results: Out of the fifteen compounds screened, two compounds, SAC-2 and LNAC-2, showed good activity with IC50 values 22µg/ml, 25μg/ml, respectively. These compounds suppressed the proliferation of ER overexpressed MCF-7 cells, increased ERα degradation and hence inactivate the ERα pathway. ER binding assay and gene expression RT-PCR study reveal that SAC-2 downregulated the expression of ERα receptor and AKT-1 gene. Conclusion:: Compound SAC-2 is a good antagonist to ER and hence has a potential for treating breast cancer and other cancers where AKT plays an important role.

scholarly journals Synthesis and biological evaluation of (E)-4-(3-arylvinyl-1H-indazol-6-yl)pyrimidin-2-amine derivatives as PLK4 inhibitors for the treatment of breast cancer

RSC Advances ◽  
2017 ◽  
Vol 7 (44) ◽  
pp. 27737-27746 ◽  
Author(s):  
Zhihao Liu ◽  
Qian Lei ◽  
Wei Wei ◽  
Lu Xiong ◽  
Yaojie Shi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Biological Evaluation ◽  
Amine Derivative ◽  
Synthesis And Biological Evaluation ◽  
Cancer Activity

SAR explorations identified (E)-4-(3-arylvinyl-1H-indazol-6-yl)pyrimidin-2-amine derivative14ias a potential PLK4 inhibitor with significant anti-breast cancer activityin vitroandin vivo.

Synthetic NRG-1 functionalized DNA nanospindels towards HER2/neu targets for in vitro anti-cancer activity assessment against breast cancer MCF-7 cells

2020 ◽  
Vol 182 ◽  
pp. 113133 ◽  
Author(s):  
Mirza Muhammad Faran Ashraf Baig ◽  
Wing-Fu Lai ◽  
Reyaj Mikrani ◽  
Mehreen Jabeen ◽  
Muhammad Naveed ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Activity Assessment ◽  
Anti Cancer ◽  
Cancer Activity ◽  
Mcf 7

Anti-cancer activity of a novel palladium(II) complex on human breast cancer cells in vitro and in vivo

2011 ◽  
Vol 46 (10) ◽  
pp. 4957-4963 ◽  
Author(s):  
Engin Ulukaya ◽  
Ferda Ari ◽  
Konstantinos Dimas ◽  
Elif Ilkay Ikitimur ◽  
Emel Guney ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Human Breast Cancer ◽  
Breast Cancer Cells ◽  
Human Breast Cancer Cells ◽  
Human Breast ◽  
Anti Cancer ◽  
Cancer Activity

scholarly journals In Vitro Anti-Cancer Alkaloid and Flavonoid Extracted from the Erythrina variegata (Leguminoseae) Plant

2011 ◽  
Vol 2 (3) ◽  
pp. 286
Author(s):  
Tati Herlina ◽  
Unang Supratman ◽  
Anas Subarnas ◽  
Supriyatna Sutardjo ◽  
Suseno Amien ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Methanol Extract ◽  
Stem Bark ◽  
Erythrina Variegata ◽  
Anti Cancer ◽  
Cancer Agent ◽  
Cancer Activity

Erythrina plants, locally known as “dadap ayam”, are higher plant species and have been used as a folk medicine for treatment of cancer. To prove the effectiveness of the leaves and stem bark of E. variegata as an anti-cancer agent, the assay in this research was focused on in vitro test towards breast cancer cell T47D. In the course of our continuing search for novel anti-cancer agent from Erythrina plants, the methanol extract of the leaves and stem bark of E. variegata showed significant anti-cancer activity against breast cancer cell T47D in vitro using the Sulphorhodamine B (SRB) assay. By using the anti-cancer activity to follow the separations, the methanol extract was separated by combination of column chromatography. The chemical structure of an anti-cancer compounds were determined on the basis of spectroscopic evidence and comparison with the previously reported and identified as an erythrina alkaloid (1) and isoflavonoid (2). Compounds (1-2) showed anti-cancer activity against breast cancer cell T47D used with IC50 of  1.0 and 3.3 µg/mL, respectively. This results strongly suggested that E. variegata is promising sources for anti-cancer agents. Keywords: Anti-cancer, Erythrina variegata, Leguminoseae

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