Enhancement of rhubarb extract solubility and bioactivity by 2-hydroxypropyl-β-cyclodextrin.
Rhubarb is a traditional Chinese medicinal herb, and the ethanolic extract of rhubarb consists of active anthraquinones, which are hydrophobic and have antiproliferative effects on hepatoma cell lines. To increase the aqueous solubility of rhubarb and study the consequent bioavailability, the ethanolic extract of rhubarb was complexed with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), a cyclic oligosaccharide that has a hydrophilic outer surface and a hydrophobic central cavity, to form a rhubarb-HP-β-CD complex. This complex was characterized by performing nuclear magnetic resonance spectroscopy, two-dimensional rotating frame spectroscopy and thin layer chromatography to confirm the inclusion of anthraquinones from rhubarb extract in HP-β-CD (weight ratio of rhubarb extract:HP-β-CD=1:9). We investigated the effects of complexing rhubarb extract with HP-β-CD on the growth of Huh7 and HepG2 cells by performing cytotoxicity analysis, cellular uptake test, and colony formation assay. Our results showed that complexation of rhubarb extract with HP-β-CD increased the aqueous solubility and bioavailability of rhubarb and thus enhanced its effect on hepatoma cells.
School of Chinese Medicine, China Medical University, Taichung, Taiwan; Graduate Institute of Chinese Medicine, China Medical University, Taichung, Taiwan; Department of Medical Genetics, Pediatrics and Medical Research, China Medical University Hospital, Taichung, Taiwan.
Chin-Mu
CM
Hsu
Song-Cu
SC
Yu
Fuu-Jen
FJ
Tsai
Yuhsin
Y
Tsai
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000880:Anthraquinones / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology; D001682:Biological Availability; D001692:Biological Transport; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D000431:Ethanol; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D010936:Plant Extracts / Q000737:chemistry*; D012250:Rheum / Q000737:chemistry*; D012995:Solubility; D012997:Solvents; D047392:beta-Cyclodextrins / Q000737:chemistry*
D000880:Anthraquinones; D000972:Antineoplastic Agents, Phytogenic; D004365:Drugs, Chinese Herbal; D010936:Plant Extracts; D012997:Solvents; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000431:Ethanol
2-Hydroxypropyl-β-cyclodextrin; Complex; Hepatoma cell; Rhubarb; Traditional Chinese medicine