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Preparation of a Camptothecin‐conjugated Molecular Carrier and its Cytotoxic Effect Toward Human Colorectal Carcinoma In Vitro
Author(s) -
Jeong Dongjun,
Pal Tarun,
Kim Hyungjoo,
Kim Tae Wan,
Biswas Goutam,
Lee Daeun,
Singh Tejinder,
Murthy Akula S. N.,
Kim Wanil,
Kim KyongTai,
Im Jungkyun
Publication year - 2018
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11611
Subject(s) - camptothecin , in vivo , conjugate , chemistry , viability assay , apoptosis , topoisomerase , in vitro , bioavailability , mtt assay , pharmacology , efflux , cytotoxicity , colorectal cancer , cell culture , cytotoxic t cell , cancer research , biochemistry , biology , cancer , medicine , mathematical analysis , genetics , microbiology and biotechnology , mathematics
Camptothecin (CPT) and its derivatives are the only chemical class that targets the enzymatic activity of DNA topoisomerase I, which is involved in DNA damage and subsequent cell apoptosis. Despite CPT's advantages, its use has been restricted due to extremely poor solubility, drug resistance by several efflux pumps, short half‐life, and poor bioavailability. To overcome these limitations, we designed and synthesized a water‐soluble CPT‐conjugated molecular transporter that successfully and rapidly delivered CPT into cells. The conjugate had affinity toward mitochondria inside cells and it was distributed mainly to kidney, lung, and spleen. MTT assay confirmed that the CPP‐conjugate decreased cell viability of colon cancer cell lines to a much greater extent than the parent drug. This novel approach has the potential of improving CPT efficacy for future in vivo applications, especially for colon cancer therapy.