title: Synthesis and synergetic anti-tumor activity evaluation of dihydroartemisinin-organogermanium(IV) compound.
abstract: Dihydroartemisinin (DHA), a semi-synthetic derivative of the herb artemisinin, has shown commendable bioactivity. In this paper, a novel dihydroartemisinin-organogermanium (DHA-Ge) compound was synthesized, characterized and its potential anti-tumor activity was evaluated by various methods. MTT results demonstrated that DHA-Ge could effectively inhibit the proliferation of HepG2 cells and showed their dose-dependent properties. The IC50 value of inhibition effect on HepG2 cells of DHA-Ge was 10.23 μg/ml which was lower than 39.44 μg/ml of DHA. Flow cytometric results suggested that DHA-Ge could induce apoptosis of HepG2 cells and the apoptosis rate was 20.26% after 24h treatment with 56.8 μg/ml DHA-Ge concentration. Atomic force microscopy images showed that HepG2 cells were collapsed and the cell nucleus were fragmented after 24h treatment. All these results together showed that the DHA-Ge possessed desirable synergetic enhanced anti-tumor effects and could be developed as a suitable tumor therapeutic agent.
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Lu
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, China.
authors.forename: Shuguang
authors.initials: S
authors.lastname: Yao
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, China.
authors.forename: Jiye
authors.initials: J
authors.lastname: Cai
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, China. Electronic address: typh@jnu.edu.cn.
authors.forename: Pei-hui
authors.initials: PH
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D037621:Artemisinins / Q000737:chemistry*; D053938:DNA Fragmentation / Q000187:drug effects; D005857:Germanium / Q000737:chemistry; D056945:Hep G2 Cells; D006801:Humans; D018625:Microscopy, Atomic Force; D009942:Organometallic Compounds / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D009942:Organometallic Compounds; D005857:Germanium; C039060:artenimol
keywords: Dihydroartemisinin; Ge-132; Organogermanium; Synergetic anti-tumor activity