Anticancer Compounds from Chinese Medicines: Drug Leads Discovery, Chemical Modifications and Formulations

Professor Che, Chi Ming   (Project Coordinator (PC))

Professor Lee Victor Ho Fun   (Co-Investigator)

Dr Sy Lai King   (Co-Investigator)

Dr Fung Eva Yi Man   (Co-Investigator)

Dr Liu Yungen   (Co-Investigator)

Dr Lok Chun Nam   (Co-Investigator)

18

2017-09-01

2019-02-28

1394950

Anticancer Compounds from Chinese Medicines: Drug Leads Discovery, Chemical Modifications and Formulations

Anticancer, Chemical Modifications, Chinese Medicines, Drug Leads Discovery, Formulations

Chemical Sciences

Physical Sciences (P)

ITS/345/16

Innovation and Technology Support Programme (Tier 3)

2017

Completed

Natural compounds from Chinese herbal medicines are rich resources for anticancer drug discovery, but only a select few from the numerous purportedly anticancer active compounds have been developed for clinical use. The main challenges in converting a herbal medicine into a clinical pharmaceutical are 1) the lack of a proper anticancer formulation with favorable pharmacology and 2) the obscurity of the molecular targets, which are necessary for further optimization. We have identified several distinct natural compounds which exhibit effective in vitro and in vivo anticancer activities and have chemical properties amenable to modifications into drug-like derivatives. In the proposed study, we will chemically modify these compounds into biocompatible forms, such as esterification of polar compounds, conjugation with cleavable water soluble motifs to improve solubility or incorporation of tumor-targeting groups to enhance bioavailability and targeting efficiency. The compounds disposition and metabolites will be analyzed in animal models by high performance mass spectrometry. Furthermore, the molecular targets and mechanisms will be elucidated by unbiased, high throughput strategies, including transcriptomic and proteomic analyses. The proposed project will exploit the valuable resources present in Chinese medicines for therapeutic applications using advanced synthetic chemistry and chemical biology strategies.