Project Title Safe and Effective Next Generation Multi-Target Anti-inflammatory Drugs
Project Category Innovation
Abstract Inflammatory diseases such as asthma, atherosclerosis, inflammatory bowel disease and cancers are major health problems which are accountable for 38 million (68%) out of 56 million deaths reported in the world. The rising incidence of inflammatory conditions is expected to drive the market value of anti-inflammatory therapeutic agents to RM 446.88 billion globally. However, currently available anti-inflammatory agents were associated with severe adverse effects. Therefore, a safe and effective multitarget anti-inflammatory agent is desired. We used computational modelling approach to design new chemical compounds which inhibit 3 target proteins involved in the inflammatory pathways; the cyclooxygenase-2, 5-lipoxygenase and phosphodiesterase. We also ensure the chemical compounds fulfil the Lipinski Rule of 5 and have favorable ADME properties for oral administration. The chemical compounds are spared from binding with COX 1 and therefore does not have adverse effects exhibited by NSAIDs. The multitarget anti-inflammatory lead compound was synthesized. The inhibitory properties of the lead compound were confirmed using specific COX2, LOX-5 and PD4 inhibition assays. We further confirmed the anti-inflammatory effects of the lead compounds using lipopolysaccharides- induced macrophages cell model. As far as we know, this is the first time, novel multitarget anti-inflammatory lead compounds were successfully designed and synthesized.
Validation Status Validated
Validation Date 2018-01-31


Staff Status
Khong Heng Yen, Profesor, Dr Member
Nyotia ak Nyokat, Dr Leader


Event Name Event Date Event Level Achievement Event Venue
Invention, Innovation and Design Exposition (IIDEX) 2017 2018-09-28 National Silver DATC, UiTM Shah Alam