Fakulti Farmasi | Faculty of Pharmacy, UKM

 Menerajui Farmasi Untuk Kesihatan | Advancing Pharmacy For Health



Centre for Drug and
Herbal Development

Drug Discovery

 

CURRENT ACTIVE PROJECTS:

A/Prof Juriyati Jalil

Anti-inflammatory effect of phytochemicals from selected Annonaceae species through inhibition of PGE2, COX-2 and cytokines production.

  • This research project aims to isolate and identify the active constituents from selected Annonaceae species using various chromatographic and spectroscopic techniques and to determine their anti-inflammatory activity through inhibition of PGE2, COX-2 and cyctokines production in human plasma using radioimmunoassay and ELISA techniques. The findings from this study could lead to the identification of new anti-inflammatory agents for drug discovery and development.

A/ Prof Khairana Hussain

Inhibitory effects of a novel α,β- unsaturated carbonyl-based compound on NF-kB, MAPK and PI3K-Akt signaling pathways in U937 macrophages, histamine and β- hexosaminidase release in RBL-2H3 cells.

  • We aim to demonstrate the anti-inflammatory activity of synthetic curcumin analogue and its molecular mechanism using LPS-activated U937 macrophages and its anti-allergic effect based on release of histamine and beta-hexosaminidase from monoclonal mouse anti-DNP immunoglobulin E-treated basophilic leukemia 2H3 (RBL-2H3) cells in vitro.
Mechanistic studies on anti-allergic activity of Anaxagorea javanica Blume extracts and their isolated compounds their isolated compounds.
 
  • In this study, we aim to isolate and identify the bioactive constituents from the leaves of Anaxagorea javanica with significant anti-allergic effects based on in vitro bioassays using rat basophilic leukemia (RBL-2H3) cell line as well as to determine their mechanisms through inhibition of effects on beta-hexosaminidase release, histamine release, histamine H1 receptors and cyctokines (TNF-alfa and IL-4) production.

Anti-allergic effects of the standardized extract of Phyllanthus amarus and its biomarker(s) using mast cells.

  • It is our interest to isolate and identify the biomarker compounds with significant anti-allergic effects based on in vitro bioassay using rat basophilic leukemia (RBL-2H3) cell line as well as to determine the inhibit effect on ligand binding to histamine H1 receptors particularly for skin allergic.

A/Prof Lam Kok Wai

 

Design and synthesis of Bcl-2 inhibitors to enhance the sensitivity of triple-negative human breast cancer cells to doxorubicin.

  • Breast cancer is the most frequent cancer among women. In Malaysia, 7593 of new breast cancer cases occurred in both sexes, which constituted about 17.3% of all new cases in 2018. It has been shown that downregulation or inhibition of Bcl-2 improves the effects of chemotherapeutic agents such as doxorubicin in human breast cancer cells. In this project, the designed compounds (based on the chromone structure) could potentially inhibit Bcl-2 activity and improve response to doxorubicin therapy in TNBC breast cancer patients.

 

Synthesis and biological evaluation of KWF101 derivatives as potential adjuvants to paclitaxel chemotherapy in TLR4-positive breast cancer cells.

  • Breast cancer is a major global health problem and the leading cause of death among women of all ethnic backgrounds with an estimated 1.6 million new cases are diagnosed worldwide. A total of 560 thousands of women will die of breast cancer each year. Preclinical models of breast cancer have shown that acquired chemoresistance and metastasis events to the widely used drug Paclitaxel (PTX) can be mediated by the activation of TLR4/MD2 in cancer cells. Our previous studies (in the literature review) showed that KWF101, a small organic molecule can potentially target the activation of TLR-4/MD2 by binding to MD-2 specifically. KWF101 was derived from curcumin which showed potent anti-inflammatory activity in human U937 cells and has good metabolic stability. 

 

 

 

 

 

 

 

 

Triple negative breast cancer cells has little HER2 protein expression and no expression of estrogen or progesterone receptors. These cells tend to grow and spread faster. Cells are stained with cytokeratins 14 (green) and 19 (red). Photo courtesy: Bill Schmitt.

EXTERNAL COLLABORATORS:

PROUDLY SPONSORED BY: