title: Rapid screening of bioactive compounds from natural products by integrating 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays.
abstract: A high throughput method was developed for rapid screening and identification of bioactive compounds from traditional Chinese medicine, marine products and other natural products. The system, integrated with five-channel chromatographic separation and dual UV-MS detection, is compatible with in vitro 96-well microplate based bioassays. The stability and applicability of the proposed method was validated by testing radical scavenging capability of a mixture of seven known compounds (rutin, dihydroquercetin, salvianolic acid A, salvianolic acid B, glycyrrhizic acid, rubescensin A and tangeretin). Moreover, the proposed method was successfully applied to the crude extracts of traditional Chinese medicine and a marine sponge from which 12 bioactive compounds were screened and characterized based on their anti-oxidative or anti-tumor activities. In particular, two diterpenoid derivatives, agelasine B and (-)-agelasine D, were identified for the first time as anti-tumor compounds from the sponge Agelas mauritiana, showing a considerable activity toward MCF-7 cells (IC50 values of 7.84±0.65 and 10.48±0.84 μM, respectively). Our findings suggested that the integrated system of 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays can be a versatile and high efficient approach for the discovery of active compounds from natural products.
authors.affiliation: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Zhang
authors.forename: Shun
authors.initials: S
authors.lastname: Xiao
authors.forename: Lijuan
authors.initials: L
authors.lastname: Sun
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Ge
authors.forename: Fengkai
authors.initials: F
authors.lastname: Fang
authors.forename: Wen
authors.initials: W
authors.lastname: Zhang
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
authors.forename: Yiyu
authors.initials: Y
authors.lastname: Cheng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology; D001681:Biological Assay / Q000379:methods*; D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002853:Chromatography, Liquid; D004354:Drug Screening Assays, Antitumor; D004355:Drug Stability; D018922:HL-60 Cells; D006801:Humans; D013058:Mass Spectrometry; D011161:Porifera / Q000737:chemistry; D015203:Reproducibility of Results; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D001688:Biological Products