Re-evaluation of antitumor activity of Cepharanthin.
The antitumor potential of Cepharanthin was re-evaluated. Cepharanthin, a biscoclaurin alkaloid extracted from Stephania cepharantha Hayata, dose-dependently reduced the viable cell number of both normal and tumor cells, showing no tumor-specific cytotoxic action. Cepharanthin synergistically enhanced the cytotoxic activity of vitamin K3 and epigallocatechin gallate. Cepharanthin induced internucleosomal DNA fragmentation only in the human promyelocytic leukemic cell line HL-60. ESR spectroscopy showed that Cepharanthin effectively scavenged the superoxide anion (produced by hypoxanthine-xanthine oxidase reaction), the hydroxyl radical (produced by Fenton reaction) and nitric oxide (NO) (produced by NOC-7 in the presence of C-PTIO). The radical scavenging activity of Cepharanthin suggests its possible anticarcinogenic action. Cepharanthin dose-dependently inhibited the production of nitric oxide, but not that of tumor necrosis factor by lipopoysaccharide-stimulated mouse macrophage-like cells Raw 264.7. These data present a cautionary note that the cytotoxic activity of Cepharanthin is more prominent than its immunopotentiating activity.
Terasaka
Hiroshi
H
Department of Oral Diagnosis, Meikai University School of Dentistry Saitama, Japan.
Machino
Mamoru
M
Saito
Masatoshi
M
Fujisawa
Seiichiro
S
Satoh
Kazue
K
Jiang
Yi
Y
Sakagami
Hiroshi
H
D000470:Alkaloids / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology* / Q000633:toxicity; D044182:Benzylisoquinolines; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D002470:Cell Survival / Q000187:drug effects; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D016166:Free Radical Scavengers / Q000494:pharmacology / Q000633:toxicity; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D009062:Mouth Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D009569:Nitric Oxide / Q000096:biosynthesis; D012468:Salivary Gland Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D014407:Tumor Cells, Cultured; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis; D052117:Benzodioxoles
D000470:Alkaloids; D000972:Antineoplastic Agents, Phytogenic; D044182:Benzylisoquinolines; D016166:Free Radical Scavengers; D008070:Lipopolysaccharides; D009569:Nitric Oxide; D014409:Tumor Necrosis Factor-alpha; C006947:cepharanthine; D052117:Benzodioxoles