Drug Designing: Open Access
Open Access
ISSN: 2169-0138
ISSN: 2169-0138
Weihui Hu, Gallant K L Chan, Huaiyou Wang, Michael Y T Cheng, Tina T X Dong Zhongyu Zhou and Karl W K Tsim
Hong Kong University of Science and Technology, China
Chinese Academy of Sciences, China
Posters & Accepted Abstracts: Drug Des
HerboChip is an array of different fractions deriving from herbal extracts, which could be applied in drug screening. Here, we aimed to identify effective components from traditional Chinese medicines (TCMs) that interact with vascular endothelial growth factor (VEGF) as a target using HerboChip. The extracts of TCMs were chemical standardized and fractionated by a standard HPLC profiling. The biotinylated-VEGF was hybridized with chips coated with different HPLC-separated fractions from the herbal extracts. Straptavidin-Cy5 was used to identify the VEGF-bound fractions. Over 100 chips were screened, and 8 positive hits were identified. The interaction of identified herbal extracts/phyto-compounds with VEGF was further confirmed in cultured human umbilical endothelial cells. As a result, the identified herbal extracts/compounds interfered (i.e. binding) with VEGF-induced cell proliferation and cell migration. The amounts of phosphorylated eNOS, phosphorylated Akt and phosphorylated ERK 1/2 were markedly altered in the co-application of the herbal extracts/compounds with VEGF. In addition, the phosphorylation of eNOS, Akt and ERK 1/2 could be modulated by the identified extracts/compounds. Six compounds from TCMs showed activating activities on the VEGF response, and two TCM compounds showed inhibiting activities. In conclusion, the current result supported the applicability of HerboChip for screening VEGF binding components from herbal extracts.