Anti-tumorigenic activity of sophoflavescenol against Lewis lung carcinoma in vitro and in vivo.
This study examined the in vitro cytotoxic activity and in vivo antitumor activity as well as intracellular apoptotic capacities of a prenylated flavonol, sophoflavescenol from Sophora flavescens, to evaluate prospective anti-tumorigenic drugs, and antitumor potential. In addition, the in vitro antioxidant and anti-inflammatory capacities were evaluated. Despite the small effect on human breast adenocarcinoma (MCF-7), sophoflavescenol showed cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells. Interestingly, it also exerted potent in vivo antitumor activity by tumor growth inhibition in the LLC tumor model as well as apoptotic activity by caspase-3 activation in HL-60 cells. In addition, it exhibited potent antioxidant activities in 1,1-diphenyl-2-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radicals and lipid peroxidation assays. Sophoflavescenol exerted notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells. The findings show that the antioxidant, anti-inflammatory, and apoptotic activities of sophoflavescenol might contribute to the antitumor activity without severe side effects, highlighting its potential for chemoprevention and/or anticancer drugs due to multi-effective targets in almost all stages of tumorigenesis, including initiation, promotion, and progression.
Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju, 561-756, Korea.
Hyun Ah
HA
Jung
Seong Eun
SE
Jin
Ran Joo
RJ
Choi
Hung Tran
HT
Manh
Yeong Shik
YS
Kim
Byung-Sun
BS
Min
You Kyung
YK
Son
Bo Ra
BR
Ahn
Byung-Woo
BW
Kim
Hee Sook
HS
Sohn
Jae Sue
JS
Choi
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification* / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy*; D045744:Cell Line, Tumor; D005260:Female; D005419:Flavonoids / Q000302:isolation & purification* / Q000494:pharmacology / Q000627:therapeutic use*; D016166:Free Radical Scavengers / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D018517:Plant Roots / Q000737:chemistry; D051381:Rats; D029909:Sophora / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D005419:Flavonoids; D016166:Free Radical Scavengers; D010936:Plant Extracts; C117237:sophoflavescenol