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In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration

The purpose of this study is to evaluate in vitro and in vivo antitumor efficacy and subacute toxicity of triptolide (TP) prodrug, a conjugate between TP and carboxymethyl chitosan (CC). The CCTP conjugate contained 4∼ wt % TP and displayed excellent aqueous solubility (5 mg/mL) as compared to the n...

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Autores principales: Zeng, Huahui, Zhu, Xin, Tian, Qikang, Yan, Yinyin, Zhang, Lan, Yan, Min, Li, Ruiqin, Li, Xiaofang, Wang, Guoqiang, Ma, Jinlian, Su, Yufang, Zhang, Xiangbo, Ma, Linyu, Zhang, Zhenqiang, Wu, Xiangxiang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8216443/
https://www.ncbi.nlm.nih.gov/pubmed/32508161
http://dx.doi.org/10.1080/10717544.2020.1770370
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author Zeng, Huahui
Zhu, Xin
Tian, Qikang
Yan, Yinyin
Zhang, Lan
Yan, Min
Li, Ruiqin
Li, Xiaofang
Wang, Guoqiang
Ma, Jinlian
Su, Yufang
Zhang, Xiangbo
Ma, Linyu
Zhang, Zhenqiang
Wu, Xiangxiang
author_facet Zeng, Huahui
Zhu, Xin
Tian, Qikang
Yan, Yinyin
Zhang, Lan
Yan, Min
Li, Ruiqin
Li, Xiaofang
Wang, Guoqiang
Ma, Jinlian
Su, Yufang
Zhang, Xiangbo
Ma, Linyu
Zhang, Zhenqiang
Wu, Xiangxiang
author_sort Zeng, Huahui
collection PubMed
description The purpose of this study is to evaluate in vitro and in vivo antitumor efficacy and subacute toxicity of triptolide (TP) prodrug, a conjugate between TP and carboxymethyl chitosan (CC). The CCTP conjugate contained 4∼ wt % TP and displayed excellent aqueous solubility (5 mg/mL) as compared to the native TP (17 μg/mL). In vitro cytotoxicity of CCTP conjugate was evaluated by CCK8 assay against human pancreatic cancer (PC) cell lines, showing comparable the half maximal inhibitory concentration (IC(50)) values to the parent TP. In a mouse model of PC (BxPC-3), the CCTP conjugate administered orally (at dose levels as low as 0.2 mg TP equivalent/kg) showed comparable efficacy in reducing or eliminating xenograft tumor to the same dose of TP, but exhibited much lower subacute toxicity as seen in body weight loss and hematological toxicity.
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spelling pubmed-82164432021-07-06 In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration Zeng, Huahui Zhu, Xin Tian, Qikang Yan, Yinyin Zhang, Lan Yan, Min Li, Ruiqin Li, Xiaofang Wang, Guoqiang Ma, Jinlian Su, Yufang Zhang, Xiangbo Ma, Linyu Zhang, Zhenqiang Wu, Xiangxiang Drug Deliv Article The purpose of this study is to evaluate in vitro and in vivo antitumor efficacy and subacute toxicity of triptolide (TP) prodrug, a conjugate between TP and carboxymethyl chitosan (CC). The CCTP conjugate contained 4∼ wt % TP and displayed excellent aqueous solubility (5 mg/mL) as compared to the native TP (17 μg/mL). In vitro cytotoxicity of CCTP conjugate was evaluated by CCK8 assay against human pancreatic cancer (PC) cell lines, showing comparable the half maximal inhibitory concentration (IC(50)) values to the parent TP. In a mouse model of PC (BxPC-3), the CCTP conjugate administered orally (at dose levels as low as 0.2 mg TP equivalent/kg) showed comparable efficacy in reducing or eliminating xenograft tumor to the same dose of TP, but exhibited much lower subacute toxicity as seen in body weight loss and hematological toxicity. Taylor & Francis 2020-06-08 /pmc/articles/PMC8216443/ /pubmed/32508161 http://dx.doi.org/10.1080/10717544.2020.1770370 Text en © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Article
Zeng, Huahui
Zhu, Xin
Tian, Qikang
Yan, Yinyin
Zhang, Lan
Yan, Min
Li, Ruiqin
Li, Xiaofang
Wang, Guoqiang
Ma, Jinlian
Su, Yufang
Zhang, Xiangbo
Ma, Linyu
Zhang, Zhenqiang
Wu, Xiangxiang
In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title_full In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title_fullStr In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title_full_unstemmed In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title_short In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
title_sort in vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8216443/
https://www.ncbi.nlm.nih.gov/pubmed/32508161
http://dx.doi.org/10.1080/10717544.2020.1770370
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