title: Antitumor activity of rhein lysinate against human glioma U87 cells in vitro and in vivo.
abstract: In previous studies, we demonstrated that rhein lysinate (RHL), the salt of rhein and lysine that is easily dissolved in water, inhibited the growth of tumor cells derived from breast and ovarian cancer, hepatocellular carcinoma, cervical cancer and lung carcinoma. Based on these observations, human glioma U87 cells and a xenograft model in BALB/c nude mice were used to examine the antitumor activity of RHL against human glioma. Notably, RHL statistically significantly suppressed the growth of human glioma U87 xenografts in BALB/c nude mice. In vitro, there was a significant reduction in cell proliferation after treatment with RHL in a dose- and time-dependent manner. The overall growth inhibition was correlated with the increase in reactive oxygen species (ROS) production and cell apoptosis. The apoptosis- and cell cycle-related proteins including BAX and Bim were increased, whereas Bcl-2 and cyclin D were decreased in the RHL-treated cells. The results demonstrated that RHL is highly effective against the growth of human glioma U87 xenografts in BALB/c nude mice. The potent antitumor activity of RHL may be mediated through downregulation of Bcl-2 and cyclin D expression and upregulation of BAX and Bim expression.
authors.affiliation: College of Life Sciences, Beijing Normal University, Beijing 100875, P.R. China.
authors.forename: Jin
authors.initials: J
authors.lastname: Liu
authors.affiliation: Oncology Department, Rizhao City People's Hospital, Rizhao, Shandong 276800, P.R. China.
authors.forename: Ke
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Key Laboratory for Chronic Diseases of Hebei Province, Key Laboratory for Preclinical and Basic Research on Chronic Diseases of Tangshan City, School of Basic Medical Sciences, North China University of Science and Technology, Tangshan, Hebei 063000, P.R. China.
authors.forename: Yong-Zhan
authors.initials: YZ
authors.lastname: Zhen
authors.affiliation: The Key Laboratory of Geriatrics, Beijing Hospital and Beijing Institute of Geriatrics, Chinese Ministry of Health, Beijing 100730, P.R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Wei
authors.affiliation: The Key Laboratory of Geriatrics, Beijing Hospital and Beijing Institute of Geriatrics, Chinese Ministry of Health, Beijing 100730, P.R. China.
authors.forename: Gang
authors.initials: G
authors.lastname: Hu
authors.affiliation: Key Laboratory for Chronic Diseases of Hebei Province, Key Laboratory for Preclinical and Basic Research on Chronic Diseases of Tangshan City, School of Basic Medical Sciences, North China University of Science and Technology, Tangshan, Hebei 063000, P.R. China.
authors.forename: Jun-Ling
authors.initials: JL
authors.lastname: Gao
authors.affiliation: Key Laboratory for Chronic Diseases of Hebei Province, Key Laboratory for Preclinical and Basic Research on Chronic Diseases of Tangshan City, School of Basic Medical Sciences, North China University of Science and Technology, Tangshan, Hebei 063000, P.R. China.
authors.forename: Yan-Xia
authors.initials: YX
authors.lastname: Tian
authors.affiliation: The Key Laboratory of Geriatrics, Beijing Hospital and Beijing Institute of Geriatrics, Chinese Ministry of Health, Beijing 100730, P.R. China.
authors.forename: Ya-Jun
authors.initials: YJ
authors.lastname: Lin
mesh_terms: D000818:Animals; D000880:Anthraquinones / Q000008:administration & dosage*; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage; D017209:Apoptosis / Q000187:drug effects; D051017:Apoptosis Regulatory Proteins / Q000096:biosynthesis*; D000072224:Bcl-2-Like Protein 11; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056741:Cyclin D / Q000096:biosynthesis*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D005910:Glioma / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D006801:Humans; D008239:Lysine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D008565:Membrane Proteins / Q000096:biosynthesis*; D051379:Mice; D011518:Proto-Oncogene Proteins / Q000096:biosynthesis*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000096:biosynthesis*; D017382:Reactive Oxygen Species; D023041:Xenograft Model Antitumor Assays; D051028:bcl-2-Associated X Protein / Q000096:biosynthesis*
chemical_list: D000880:Anthraquinones; D000972:Antineoplastic Agents, Phytogenic; D051017:Apoptosis Regulatory Proteins; C000606775:BCL2L11 protein, human; D000072224:Bcl-2-Like Protein 11; C000606776:Bcl2l11 protein, mouse; D056741:Cyclin D; D008565:Membrane Proteins; D011518:Proto-Oncogene Proteins; D019253:Proto-Oncogene Proteins c-bcl-2; D017382:Reactive Oxygen Species; D051028:bcl-2-Associated X Protein; C583741:rhein lysinate; D008239:Lysine