scholarly journals Anti-Cancer Activity of Cayratia Auriculata Ethanolic Extracts Against Cancer Cell Line A549 An In Vitro Analysis

2020 ◽  
Vol 13 (2) ◽  
pp. 495-499
Author(s):  
Lalitha S Lalitha ◽  
Anusha D Anusha ◽  
Yogeshkumar Murkunde ◽  
Viji Devanand ◽  
Maheshkumar K Maheshkumar
2021 ◽  
Vol 21 (2) ◽  
pp. 59-69
Author(s):  
Priscilla Ardianto ◽  
Ade Arsianti ◽  
Khaerunissa Anbar Isti ◽  
Fadilah Fadilah

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Kotaro Sakamoto ◽  
Teruaki Masutani ◽  
Takatsugu Hirokawa

AbstractRas mutations (e.g., occur in K-Ras, N-Ras, and H-Ras) are one of the most desirable and promising drug targets in chemotherapy treatments for cancer. However, there are still no approved drugs directly targeting mutated Ras. In 2017, an artificial cyclic peptide, KRpep-2d, was discovered as the first selective inhibitor of K-Ras(G12D), the most frequent K-Ras mutation. Here, we report the generation of KS-58, a KRpep-2d derivative that is identified as a bicyclic peptide and possess unnatural amino acid structures. Our in vitro data and molecular dynamics simulations suggest that KS-58 enters cells and blocks intracellular Ras–effector protein interactions. KS-58 selectively binds to K-Ras(G12D) and suppresses the in vitro proliferation of the human lung cancer cell line A427 and the human pancreatic cancer cell line PANC-1, both of which express K-Ras(G12D). Moreover, KS-58 exhibits anti-cancer activity when given as an intravenous injection to mice with subcutaneous or orthotropic PANC-1 cell xenografts. The anti-cancer activity is further improved by combination with gemcitabine. To the best of our knowledge, this is the first report of K-Ras(G12D)-selective inhibitory peptide presenting in vivo anti-cancer activity. KS-58 is an attractive lead molecule for the development of novel cancer drugs that target K-Ras(G12D).


PLoS ONE ◽  
2013 ◽  
Vol 8 (6) ◽  
pp. e64388 ◽  
Author(s):  
Chanel E. Smart ◽  
Brian J. Morrison ◽  
Jodi M. Saunus ◽  
Ana Cristina Vargas ◽  
Patricia Keith ◽  
...  

2018 ◽  
Vol 16 (1) ◽  
pp. 591-604 ◽  
Author(s):  
Lucia Pirvu ◽  
Amalia Stefaniu ◽  
Georgeta Neagu ◽  
Bujor Albu ◽  
Lucia Pintilie

AbstractThis study aimed to compare in vitro cell cytotoxicity and antiproliferative potency of three standardized ethanolic extracts (5mg GAE/mL sample) from quince flower petals, leaves and fruit pellet on four cell lines (L-929, and HepG2, Caco-2 and BT-20 respectively). Comparative analytical qualitative studies (HPTLC) indicated that if quince leaf extracts (Col40) mainly contain quercetin and kaempferol derivates, the flower petal extracts (Cof40) contain caffeoylquinic acid derivates, while the fruit pellet extracts (Cop40) are comprised of quercetin and caffeoylquinic acid derivates. Pharmacological studies demonstrated the lack of toxicity of test extracts; the most important antiproliferative effects were observed on the hepatic cancer cell line HepG2 (up to 75%, 53% and 70% inhibition in the case of Col40, Cof40 and Cop40 test extracts), followed by the colon cancer cell line Caco-2 (up to 69%, 77% and 40% inhibition) and breast cancer cell line BT-20 (up to 54%, 61% and 19% inhibition). The docking simulations on hyperoside, isoquercitrin, astragalin, and quercetin and kaempferol compared to the synthetic co-crystallized LI0 A1000 ligand (a strong inhibitor of anti-apoptotic protein Bcl-2) indicated astragalin as the most feasible protein inhibitor, but quercetin and kaempferol respected all the parameters involved in the Lipinski rule, making them the most promising antiproliferative candidates.


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