@article {824, title = {Cakile maritima Scop. Extracts Inhibit Caco2 and HeLa Human Carcinoma Cell Growth: GC-MS Analysis of an Anti-Proliferative Extract}, journal = {Pharmacognosy Journal}, volume = {11}, year = {2019}, month = {February 2019}, pages = {258-266}, type = {Original Article}, chapter = {258}, abstract = {

Introduction: Exposure to high levels of antioxidants has been linked to the treatment and prevention of some cancers. Although Cakile maritima has a high antioxidant capacity, it is yet to be tested for the ability to inhibit the proliferation of cancer cells. Methods: Solvent extracts prepared from C. maritima plant material were analysed for antioxidant capacity by the DPPH free radical scavenging assay. Anti-proliferative activities against Caco2 and HeLa cancer cells were determined by an MTS based cell proliferation assay. Toxicity was determined by the Artemia franciscana bioassay. The most potent anti-proliferative extract (hexane) was further investigated using non-targeted GC-MS headspace analysis. Results: Good DPPH radical scavenging activity was calculated for all C. maritima extracts. The methanolic and ethyl acetate extracts had particularly strong antioxidant activity (IC50 of 4.7 and 3.4 μg/mL respectively). Interestingly, the hexane extract which had the lowest DPPH radical scavenging activity (IC50 13.6 μg/mL), was the most potent inhibitor or Caco2 and HeLa carcinoma cell growth, with IC50{\textquoteright}s of 12 and 126 μg/mL respectively. The ethyl acetate extract was also a potent inhibitor of proliferation (IC50 values of 185 and 468 μg/mL against Caco2 and HeLa, respectively). The methanolic extract (IC50 values of 2261 and 2046 μg/mL against CaCo2 and HeLa respectively) displayed only moderate anti-proliferative activity, demonstrating that antioxidant activity did not correspond with anti-proliferative activity. All of the extracts were determined to be nontoxic in the Artemia franciscana bioassay, with LC50 values substantially \>1000 μg/mL. Non-biased GC-MS headspace analysis of the C. maritima hexane extract highlighted several interesting compounds that may contribute to the therapeutic bioactivities of the extract. Conclusion: The lack of toxicity and the anti-proliferative activity of the hexane and ethyl acetate C. maritima extracts against HeLa and Caco2 cancer cell lines indicates their potential in the treatment and prevention of some cancers.

}, keywords = {Anticancer activity, Antioxidant, Brassicaceae, CaCo2, European searocket, HeLa, Oxidative stress}, doi = {10.5530/pj.2019.11.40}, author = {Elsayed Omer and Abdelsamed Elshamy and Rihab Taher and Walaa El-Kashak and Joseph Shalom and Alan White and Ian Cock} } @article {620, title = {Pharmacophore Modelling of Brassicaceae Members as Potent HIF (Hypoxia Inducible Factor) Inhibitors Involved in Cancer Angiogenesis}, journal = {Pharmacognosy Journal}, volume = {10}, year = {2018}, month = {May 2018}, pages = {798-802}, type = {Original Article}, chapter = {798}, abstract = {

Angiogenesis is considered as an essential pathological feature of cancer due to its interplay between cancer and other diseases. Natural products found to act as antiangiogenic agents that mediate the angiogenic switch between pro and anti angiogenic factors. Among the different targets, HIF is an important and critical factor that stands as a key mediator between angiogenesis, inflammation and cancer. In our study different phytochemicals of Brassicaceae were analysed for their drug like properties and mapped for pharmacophore development. The developed pharmacophore was virtually screened and further subjected to Lipinski and ADMET filters. The molecular interaction studies of the 10 retrieved compounds were studied by binding with HIF. Among the compounds 1stdrug like molecule HTS 0115 (C15H21BrN2O3) was found to have best docked score and its interaction was further validated using dynamics simulation. The compound found to share the pharmacophoric features with progoitrin a biochemical form of glucosinolate with reported anticancer and anti thyroid activities. Thus the drug like compound HTS 0115 can be further optimised as a putative HIF inhibitor in tumor angiogenesis.

}, keywords = {Angiogenesis, Brassicaceae, HIF, Molecular docking, Pharmacophore, Simulation}, doi = {10.5530/pj.2018.4.135}, url = {http://fulltxt.org/article/673}, author = {Jeyavel Renukadevi and Ganesan Nandhinidevi and Muthiah Bavanilatha and Hemanath Tharani and Rajarajan Sathiyabama and Subramani Vasumathi} }