scholarly journals Cytotoxic effect of Leurius quinquestratus (scorpion) venom in different human cancer cell lines in vitro

2022 ◽  
Vol 20 (2) ◽  
pp. 345-350
Author(s):  
Wesam M. Salama ◽  
Sabry A. El-Naggar

Purpose: In this study, the cytotoxicity of scorpion Leurius quinquestratus crude venom (LQCV) was evaluated in vitro in selected human cancer cell lines. Methods: Breast (MCF-7), hepatocellular (HepG-2), colon (CaCo-2), cervix (HeLa) and alveolar (A-549) adenocarcinoma cell lines were tested. MTT assay and median inhibition concentration (IC50), apoptotic assay, caspase 3, P53, Bcl-2 proteins and cell cycle were determined. Results: 24 hrs post-treatment, CaCo-2 represented the most sensitive cell line (IC50 of 4.12 μg/mL). Due to the exposure to 1/10 IC50 of LQCV, the percentage of the apoptotic cells, caspase 3, and P53 proteins were increased significantly (P<0.05) while Bcl-2 was decreased in comparison to untreated cells. Treatment with LQCV induced cell cycle arrest at G1 and G2/M phases. Conclusion: LQCV displays potent cytotoxicity against selected human cell lines in vitro. Thus, the material could become a potent agent for the management of some cancers.

2003 ◽  
Vol 106 (1) ◽  
pp. 125-137 ◽  
Author(s):  
Wen-Sen Lee ◽  
Rong-Jane Chen ◽  
Ying-Jan Wang ◽  
How Tseng ◽  
Jiiang-Huei Jeng ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.


Author(s):  
Suguru Fukahori ◽  
Hirohisa Yano ◽  
Jun Akiba ◽  
Sachiko Ogasawara ◽  
Seiya Momosaki ◽  
...  

RSC Advances ◽  
2016 ◽  
Vol 6 (94) ◽  
pp. 91386-91393 ◽  
Author(s):  
Jianfa Zong ◽  
Dongxu Wang ◽  
Weiting Jiao ◽  
Liang Zhang ◽  
Guanhu Bao ◽  
...  

Oleiferasaponin C6 was isolated from Camellia oleifera Abel. and inhibits proliferation through inducing cell-cycle arrest and apoptosis on cancer cell lines in vitro.


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