title: Luteolin nanoparticle in chemoprevention: in vitro and in vivo anticancer activity.
abstract: Cancer prevention (chemoprevention) by using naturally occurring dietary agents has gained immense interest because of the broad safety window of these compounds. However, many of these compounds are hydrophobic and poorly soluble in water. They frequently display low bioavailability, poor systemic delivery, and low efficacy. To circumvent this problem, we explored a novel approach toward chemoprevention using nanotechnology to deliver luteolin, a natural compound present in green vegetables. We formulated water-soluble polymer-encapsulated Nano-Luteolin from hydrophobic luteolin, and studied its anticancer activity against lung cancer and head and neck cancer. In vitro studies demonstrated that, like luteolin, Nano-Luteolin inhibited the growth of lung cancer cells (H292 cell line) and squamous cell carcinoma of head and neck (SCCHN) cells (Tu212 cell line). In Tu212 cells, the IC50 value of Nano-Luteolin was 4.13 μmol/L, and that of luteolin was 6.96 μmol/L. In H292 cells, the IC50 of luteolin was 15.56 μmol/L, and Nano-Luteolin was 14.96 μmol/L. In vivo studies using a tumor xenograft mouse model demonstrated that Nano-Luteolin has a significant inhibitory effect on the tumor growth of SCCHN in comparison to luteolin. Our results suggest that nanoparticle delivery of naturally occurring dietary agents like luteolin has many advantages and may have potential application in chemoprevention in clinical settings.
authors.affiliation: Department of Hematology and Medical Oncology, Winship Cancer Institute, Emory University School of Medicine, 1365 C Clifton Road, Atlanta, GA 30322. dmshin@emory.edu.
authors.forename: Debatosh
authors.initials: D
authors.lastname: Majumdar
authors.forename: Kyung-Ho
authors.initials: KH
authors.lastname: Jung
authors.forename: Hongzheng
authors.initials: H
authors.lastname: Zhang
authors.forename: Sreenivas
authors.initials: S
authors.lastname: Nannapaneni
authors.forename: Xu
authors.initials: X
authors.lastname: Wang
authors.forename: A R M Ruhul
authors.initials: AR
authors.lastname: Amin
authors.forename: Zhengjia
authors.initials: Z
authors.lastname: Chen
authors.forename: Zhuo G
authors.initials: ZG
authors.lastname: Chen
authors.forename: Dong M
authors.initials: DM
authors.lastname: Shin
mesh_terms: D000818:Animals; D016588:Anticarcinogenic Agents / Q000627:therapeutic use*; D002294:Carcinoma, Squamous Cell / Q000517:prevention & control; D045744:Cell Line, Tumor; D002470:Cell Survival; D018890:Chemoprevention / Q000379:methods*; D004032:Diet; D016503:Drug Delivery Systems; D006258:Head and Neck Neoplasms / Q000517:prevention & control*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D047311:Luteolin / Q000627:therapeutic use*; D051379:Mice; D008819:Mice, Nude; D053758:Nanoparticles / Q000737:chemistry*; D009368:Neoplasm Transplantation; D011108:Polymers / Q000737:chemistry; D012235:Rhodamines / Q000737:chemistry; D012995:Solubility; D000077195:Squamous Cell Carcinoma of Head and Neck; D014675:Vegetables
chemical_list: D016588:Anticarcinogenic Agents; D011108:Polymers; D012235:Rhodamines; C022027:lissamine rhodamine B; D047311:Luteolin