title: The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells.
abstract: Jesridonin, a small molecule obtained through the structural modification of Oridonin, has extensive antitumor activity. In this study, we evaluated both its in vitro activity in the cancer cell line EC109 and its in vivo effect on tumor xenografts in nude mice. Apoptosis induced by Jesridonin was determined using an MTT assay, Annexin-V FITC assay and Hoechest 33258 staining. Apoptosis via mitochondrial and death receptor pathways were confirmed by detecting the regulation of MDM2, p53, and Bcl-2 family members and by activation of caspase-3/-8/-9. In addition, vena caudalis injection of Jesridonin showed significant inhibition of tumor growth in the xenograft model, and Jesridonin-induced cell apoptosis in tumor tissues was determined using TUNEL. Biochemical serum analysis of alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST), gamma-glutamyl transferase (GGT), total protein (TP) and albumin (ALB) indicated no obvious effects on liver function. Histopathological examination of the liver, kidney, lung, heart and spleen revealed no signs of JD-induced toxicity. Taken together, these results demonstrated that Jesridonin exhibits antitumor activity in human esophageal carcinomas EC109 cells both in vitro and in vivo and demonstrated no adverse effects on major organs in nude mice. These studies provide support for new drug development.
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Cong
authors.initials: C
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Liping
authors.initials: L
authors.lastname: Jiang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Saiqi
authors.initials: S
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Hongge
authors.initials: H
authors.lastname: Shi
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Junwei
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Ran
authors.initials: R
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Yongmei
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Yinhui
authors.initials: Y
authors.lastname: Dou
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Guiqin
authors.initials: G
authors.lastname: Hou
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Ke
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
authors.forename: Hongmin
authors.initials: H
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D045786:Diterpenes, Kaurane / Q000494:pharmacology*; D004938:Esophageal Neoplasms / Q000378:metabolism / Q000473:pathology*; D006801:Humans; D051379:Mice; D009363:Neoplasm Proteins / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D045786:Diterpenes, Kaurane; D009363:Neoplasm Proteins; C000606573:jesridonin