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Title:
CELL-PENETRATING RIBOFLAVIN COMPLEX AND APPLICATION THEREOF IN PREPARATION OF PHOTODYNAMIC THERAPY DRUG
Document Type and Number:
WIPO Patent Application WO/2023/092708
Kind Code:
A1
Abstract:
A cell-penetrating riboflavin complex and an application thereof in preparation of a photodynamic therapy drug. Riboflavin is coupled to a cell-penetrating peptide Arg8, (Cha-Arg)3, and a target small molecule triphenylphosphine (TPP), respectively; three complexes comprising Arg8-RF, (Cha-Arg)3-RF, and TPP-RF are designed, and by comparing the cell uptake efficiency and phototoxicity thereof, (Cha-Arg)3-RF can improve the uptake efficiency of tumor cells to riboflavin; meanwhile, the photodynamic therapy effect of riboflavin is enhanced. The riboflavin complex can be used to prepare a naturally derived anti-tumor photodynamic therapy drug. The drug has the advantages of being good in biocompatibility, low in toxicity, economical and readily available.

Inventors:
FANG LIJING (CN)
WU CHUNLEI (CN)
LI YANYAN (CN)
CHENG ZHEHONG (CN)
MA ZHILONG (CN)
Application Number:
PCT/CN2021/137632
Publication Date:
June 01, 2023
Filing Date:
December 13, 2021
Export Citation:
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Assignee:
SHENZHEN INST ADV TECH (CN)
International Classes:
A61K47/54; A61K41/00; A61K47/64; A61P35/00; C07K7/06
Foreign References:
US20050176624A12005-08-11
CN107936091A2018-04-20
CN104940950A2015-09-30
US20150374714A12015-12-31
Other References:
YONGDOO CHOI; JASON R. MCCARTHY; RALPH WEISSLEDER; CHING‐HSUAN TUNG: "Conjugation of a Photosensitizer to an Oligoarginine‐Based Cell‐Penetrating Peptide Increases the Efficacy of Photodynamic Therapy", CHEMMEDCHEM COMMUNICATIONS, vol. 1, no. 4, 24 January 2006 (2006-01-24), DE , pages 458 - 463, XP072419295, ISSN: 1860-7179, DOI: 10.1002/cmdc.200500036
MAHALINGAM SAKKARAPALAYAM M, ORDAZ JOSUE D., LOW PHILIP S: "Targeting of a Photosensitizer to the Mitochondrion Enhances the Potency of Photodynamic Therapy", ACS OMEGA, vol. 3, no. 6, 30 June 2018 (2018-06-30), US , pages 6066 - 6074, XP093069425, ISSN: 2470-1343, DOI: 10.1021/acsomega.8b00692
HORTON, K.L. ; STEWART, K.M. ; FONSECA, S.B. ; GUO, Q. ; KELLEY, S.O.: "Mitochondria-Penetrating Peptides", CHEMISTRY & BIOLOGY, vol. 15, no. 4, 21 April 2008 (2008-04-21), GB , pages 375 - 382, XP022613220, ISSN: 1074-5521, DOI: 10.1016/j.chembiol.2008.03.015
Attorney, Agent or Firm:
BEIJING ZHONG XUN TONG DA INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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