Anticancer activity of 3-demethylubiquinone Q2. In vivo experiments and probable mechanism of action.
BACKGROUND
3-Demethylubiquinone Q2 (3DMUbQ2), isolated from the ascidian Aplidium glabrum and later synthesized, is known as a natural product inhibiting EGF-induced malignant JB6 P+ Cl 41 cell transformation. However, its in vivo anticancer properties and probable mechanism of this action have not been studied.


METHODS
Preventive and curable effects of3DMUbQ2 on mice with inoculated Ehrlich carcinoma tumors were examined by magnetic resonance tomography. Capability to inhibit human tumor cell colony growth and induce their apoptosis was investigated using the anchorage-independent phenotype expression assay in soft agar and flow cytometry.


RESULTS
3DMUbQ2 inhibits the growth of the solid Ehrlich carcinoma in mice, especially using the prophylactic scheme of administration (50% inhibition). It inhibits the phenotype expression of HT-460, HCT-116 and SK-MEL-28 human tumor cells and induces apoptosis of these cell lines, as well as that of HL-60 and THP-1 tumor cells.


CONCLUSIONS
3DMUbQ2 and other related marine polyprenylquinones have potential for development of a new antitumor agent in cancer prophylactics and treatment and should be further investigated.
Fedorov
Sergey N
SN
Pacific Institute of Bioorganic Chemistry, Vladivostok 690022, Russian Federation.
Radchenko
Oleg S
OS
Shubina
Larisa K
LK
Balaneva
Nadezda N
NN
Agafonova
Irina G
IG
Bode
Ann M
AM
Jin
Jun-O
JO
Kwak
Jong-Young
JY
Dong
Zigang
Z
Stonik
Valentin A
VA
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D017209:Apoptosis; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051379:Mice; D010641:Phenotype; D014451:Ubiquinone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use
C509658:3-demethylubiquinone Q2; D000970:Antineoplastic Agents; D014451:Ubiquinone