Introduction: Benzimidazole analogues are bicyclic compounds that had been synthesized comprising the fusion of benzene and imidazole. It gains interest in research as it poses numerous therapeutic potential such as anti-ulcer, anti-malarial, anti-helminthic, anti-fungal, anti-inflammatory, and anti-cancer. Hence, this work aims to screen novel benzimidazole analogues using MTT assay for potential anti-proliferation activities on gastric cancer, which is the second cause of cancer-related death. Methods: MTT assay was conducted following standard protocol on HGT-1 gastric cancer cells. Cells were seeded and allowed to attach overnight before being introduced with various con-centration of benzimidazole analogues up to 72 hours and the optical density of the MTT was recorded using 560 nm wavelength. Two-Way ANOVA was used to analyse all data, followed by post-hoc Tukey test and the structure analysis relationship was analysed using MTT result. Results: From five analogues, only compound 4 showed an-ti-proliferation activity with IC50 8.212 ± 0.813 μM at 72 hours. Compound 4 had hydroxyl group at ortho- and para- position and remarkably, compound 2 which contained the hydroxyl group at ortho- and meta- position together with compound 5 which contained the combination of meta- and para- induced proliferation on gastric cancer. Conclusion: Different position of hydroxyl group on the benzene ring gives different activities on gastric cancer and from the experiment, only compound 4 had the anti-proliferative activity.
Plants have been a good source of therapeutic agents for thousands of years;
an impressive number of modern drugs used for treating human diseases are derived from
natural sources. The Theobroma cacao tree, or cocoa, has recently garnered increasing
attention and become the subject of research due to its antioxidant properties, which are
related to potential anti-cancer effects. In the past few years, identifying and developing
active compounds or extracts from the cocoa bean that might exert anti-cancer effects
have become an important area of health- and biomedicine-related research. This review
provides an updated overview of T. cacao in terms of its potential anti-cancer compounds
and their extraction, in vitro bioassay, purification, and identification. This article also
discusses the advantages and disadvantages of the techniques described and reviews the
processes for future perspectives of analytical methods from the viewpoint of anti-cancer
compound discovery.
A cationic Schiff base ligand, TSB (L) and its Zn (II) complex (1) were synthesized and characterized by using CHN, (1)H-NMR, FT-IR, UV, LC-MS, and X-ray methods. Their ability to inhibit topoisomerase I, DNA cleavage activities, and cytotoxicity were studied. X-ray diffraction study shows that the mononuclear complex 1 is four coordinated with distorted tetrahedral geometry. The singly deprotonated Schiff base ligand L acts as a bidentate ON-donor ligand. Complexation of L increases the inhibitory strength on topoisomerase I activity. Complex 1 could fully inhibit topoisomerase I activity at 250 μM, while L did not show any inhibitory effect on topoisomerase I activity. In addition, L and complex 1 could cleave pBR322 DNA in a concentration and time dependent profile. Surprisingly, L has better DNA cleavage activity than complex 1. The cleavage of DNA by complex 1 is altered in the presence of hydrogen peroxide. Furthermore, L and complex 1 are mildly cytotoxic towards human ovarian cancer A2780 and hepatocellular carcinoma HepG2.