title: Antitumoral Activity of (20R)- and (20S)-Ginsenoside Rh2 on Transplanted Hepatocellular Carcinoma in Mice.
abstract: Hepatocellular carcinoma is one of the leading causes of malignancy-related death in China. Its therapy in clinics is a big challenge. Ginsenoside Rh2 is one of the most notable cancer-preventing components from red ginseng and it has been reported that ginsenoside Rh2 exhibited potent cytotoxicity against human hepatoma cells. Rh2 exists as two different stereoisomeric forms, (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2. Previous reports showed that the Rh2 epimers demonstrated different pharmacological activities and only (20S)-ginsenoside Rh2 showed potent proliferation inhibition on cancer cells in vitro. However, the in vivo anti-hepatoma activity of (20R)-ginsenoside Rh2 and (20S)-ginsenoside Rh2 has not been reported yet. This work assessed and compared the anti-hepatoma activities of (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 using H22 a hepatoma-bearing mouse model in vivo. In addition, hematoxylin and eosin staining, the deoxynucleotidyl transferase dUTP nick-end labeling assay, and the semiquantitative reverse transcriptase polymerase chain reaction method were used to further study the apoptosis of the tumors. The results showed that both (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 suppressed the growth of H22 transplanted tumors in vivo, and the highest inhibition rate could be up to 42.2 and 46.8 %, respectively (p < 0.05). Further, hematoxylin/eosin staining and the deoxynucleotidyl transferase dUTP nick-end labeling assay indicated that both (20R)-ginsenoside Rh2 and (20S)-ginsenoside Rh2 could induce H22 hepatoma tumor cell apoptosis, with apoptosis indexes of 3.87 %, and 3.80 %, respectively (p < 0.05). Moreover, this effect was accompanied by downregulating the level of Bcl-2 mRNA. In conclusion, both (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 can suppress the growth of H22 hepatomas without causing severe side effects, and this effect is associated with the induction of apoptosis.
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Qun
authors.initials: Q
authors.lastname: Lv
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Na
authors.initials: N
authors.lastname: Rong
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Li-Jia
authors.initials: LJ
authors.lastname: Liu
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Xiao-Lin
authors.initials: XL
authors.lastname: Xu
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Jian-Ting
authors.initials: JT
authors.lastname: Liu
authors.affiliation: School of Biological & Foodstuff Engineering, Dalian Institute of Light Industry, Dalian, China.
authors.forename: Feng-Xie
authors.initials: FX
authors.lastname: Jin
authors.affiliation: Department of Biological Pharmaceutics, School of Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Chun-Mei
authors.initials: CM
authors.lastname: Wang
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000627:therapeutic use*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000627:therapeutic use*; D005260:Female; D036145:Ginsenosides / Q000627:therapeutic use*; D007536:Isomerism; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy*; D051379:Mice; D005894:Panax / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004365:Drugs, Chinese Herbal; D036145:Ginsenosides; C055305:ginsenoside Rh2