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.
The genus Macaranga comes from the family of Euphorbiaceae and it is the only genus in the subtribe Macaranginae that have a large genus with 300 species of which 27 species were found in Peninsular Malaysia. This plant grows as shrubs or trees that can grow up to 15 m tall and known for their mutual associations with ants. Fresh or dried leaves of some Macaranga species were used by traditional healers to treat swellings, cuts, sores, boils and bruises. The isolation of chemical constituent from this genus has been shown to produce numerous results of phenolic compounds, such as flavonoids and stilbenoids. In this paper, we report the isolation of a prenylated flavonol, glyasperin A (1), together with a simple flavone apigenin (2) from the methanolic extract of the leaves of Macaranga gigantea. The structure of both compounds has been elucidated based on its spectroscopic data, including mass spectroscopy (MS), infrared (IR), ultraviolet-visible (UV-Vis), 1D and 2D nuclear magnetic resonance (NMR) spectra and comparison with the previous literature.