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Liposomal quercetin efficiently suppresses growth of solid tumors in murine models.
Clin Cancer Res. 2006 May 15; 12(10):3193-9.CC

Abstract

PURPOSE

Quercetin is a potent chemotherapeutic drug. Clinical trials exploring different schedules of administration of quercetin have been hampered by its extreme water insolubility. To overcome this limitation, this study is aimed to develop liposomal quercetin and investigate its distribution in vivo and antitumor efficacy in vivo and in vitro.

EXPERIMENTAL DESIGN

Quercetin was encapsulated in polyethylene glycol 4000 liposomes. Biodistribution of liposomal quercetin i.v. at 50 mg/kg in tumor-bearing mice was detected by high-performance liquid chromatography. Induction of apoptosis by liposomal quercetin in vitro was tested. The antitumor activity of liposomal quercetin was evaluated in the immunocompetent C57BL/6N mice bearing LL/2 Lewis lung cancer and in BALB/c mice bearing CT26 colon adenocarcinoma and H22 hepatoma. Tumor volume and survival time were observed. The mechanisms underlying the antitumor effect of quercetin in vivo was investigated by detecting the microvessel density, apoptosis, and heat shock protein 70 expression in tumor tissues.

RESULTS

Liposomal quercetin could be dissolved in i.v. injection and effectively accumulate in tumor tissues. The half-time of liposomal quercetin was 2 hours in plasma. The liposomal quercetin induced apoptosis in vitro and significantly inhibited tumor growth in vivo in a dose-dependent manner. The optimal dose of liposomal quercetin resulted in a 40-day survival rate of 40%. Quantitative real-time PCR showed that liposomal quercetin down-regulated the expression of heat shock protein 70 in tumor tissues. Immunohistochemistry analysis showed that liposomal quercetin inhibited tumor angiogenesis as assessed by CD31 and induced tumor cell apoptosis.

CONCLUSIONS

Our data indicated that pegylated liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be a potential application in the treatment of tumor.

Authors+Show Affiliations

State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16707620

Citation

Yuan, Zhi-ping, et al. "Liposomal Quercetin Efficiently Suppresses Growth of Solid Tumors in Murine Models." Clinical Cancer Research : an Official Journal of the American Association for Cancer Research, vol. 12, no. 10, 2006, pp. 3193-9.
Yuan ZP, Chen LJ, Fan LY, et al. Liposomal quercetin efficiently suppresses growth of solid tumors in murine models. Clin Cancer Res. 2006;12(10):3193-9.
Yuan, Z. P., Chen, L. J., Fan, L. Y., Tang, M. H., Yang, G. L., Yang, H. S., Du, X. B., Wang, G. Q., Yao, W. X., Zhao, Q. M., Ye, B., Wang, R., Diao, P., Zhang, W., Wu, H. B., Zhao, X., & Wei, Y. Q. (2006). Liposomal quercetin efficiently suppresses growth of solid tumors in murine models. Clinical Cancer Research : an Official Journal of the American Association for Cancer Research, 12(10), 3193-9.
Yuan ZP, et al. Liposomal Quercetin Efficiently Suppresses Growth of Solid Tumors in Murine Models. Clin Cancer Res. 2006 May 15;12(10):3193-9. PubMed PMID: 16707620.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Liposomal quercetin efficiently suppresses growth of solid tumors in murine models. AU - Yuan,Zhi-ping, AU - Chen,Li-juan, AU - Fan,Lin-yu, AU - Tang,Ming-hai, AU - Yang,Guang-li, AU - Yang,Han-su, AU - Du,Xiao-bo, AU - Wang,Guo-qing, AU - Yao,Wen-xiu, AU - Zhao,Qu-mei, AU - Ye,Bin, AU - Wang,Rui, AU - Diao,Peng, AU - Zhang,Wei, AU - Wu,Hong-bin, AU - Zhao,Xia, AU - Wei,Yu-quan, PY - 2006/5/19/pubmed PY - 2006/7/27/medline PY - 2006/5/19/entrez SP - 3193 EP - 9 JF - Clinical cancer research : an official journal of the American Association for Cancer Research JO - Clin. Cancer Res. VL - 12 IS - 10 N2 - PURPOSE: Quercetin is a potent chemotherapeutic drug. Clinical trials exploring different schedules of administration of quercetin have been hampered by its extreme water insolubility. To overcome this limitation, this study is aimed to develop liposomal quercetin and investigate its distribution in vivo and antitumor efficacy in vivo and in vitro. EXPERIMENTAL DESIGN: Quercetin was encapsulated in polyethylene glycol 4000 liposomes. Biodistribution of liposomal quercetin i.v. at 50 mg/kg in tumor-bearing mice was detected by high-performance liquid chromatography. Induction of apoptosis by liposomal quercetin in vitro was tested. The antitumor activity of liposomal quercetin was evaluated in the immunocompetent C57BL/6N mice bearing LL/2 Lewis lung cancer and in BALB/c mice bearing CT26 colon adenocarcinoma and H22 hepatoma. Tumor volume and survival time were observed. The mechanisms underlying the antitumor effect of quercetin in vivo was investigated by detecting the microvessel density, apoptosis, and heat shock protein 70 expression in tumor tissues. RESULTS: Liposomal quercetin could be dissolved in i.v. injection and effectively accumulate in tumor tissues. The half-time of liposomal quercetin was 2 hours in plasma. The liposomal quercetin induced apoptosis in vitro and significantly inhibited tumor growth in vivo in a dose-dependent manner. The optimal dose of liposomal quercetin resulted in a 40-day survival rate of 40%. Quantitative real-time PCR showed that liposomal quercetin down-regulated the expression of heat shock protein 70 in tumor tissues. Immunohistochemistry analysis showed that liposomal quercetin inhibited tumor angiogenesis as assessed by CD31 and induced tumor cell apoptosis. CONCLUSIONS: Our data indicated that pegylated liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be a potential application in the treatment of tumor. SN - 1078-0432 UR - https://www.unboundmedicine.com/medline/citation/16707620/Liposomal_quercetin_efficiently_suppresses_growth_of_solid_tumors_in_murine_models_ L2 - http://clincancerres.aacrjournals.org/cgi/pmidlookup?view=long&pmid=16707620 DB - PRIME DP - Unbound Medicine ER -