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羧甲基壳聚糖连接雷公藤内酯醇的口服给药的抗肿瘤作用。

antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration.

机构信息

Academy of Chinese Medicine Sciences, Henan University of Chinese Medicine, Zhengzhou, China.

School of Basic Medicine, Henan University of Chinese Medicine, Zhengzhou, China.

出版信息

Drug Deliv. 2020 Dec;27(1):848-854. doi: 10.1080/10717544.2020.1770370.

DOI:10.1080/10717544.2020.1770370
PMID:32508161
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8216443/
Abstract

The purpose of this study is to evaluate 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). cytotoxicity of CCTP conjugate was evaluated by CCK8 assay against human pancreatic cancer (PC) cell lines, showing comparable the half maximal inhibitory concentration (IC) 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.

摘要

本研究旨在评估雷公藤红素（TP）前药-羧甲基壳聚糖（CC）缀合物的抗肿瘤疗效和亚急性毒性。CCTP 缀合物中含有 4wt%的 TP，与天然 TP（17μg/mL）相比，具有优异的水溶性（5mg/mL）。用 CCK8 法检测 CCTP 缀合物对人胰腺癌细胞系的细胞毒性，其半数最大抑制浓度（IC）值与母体 TP 相当。在胰腺癌细胞（BxPC-3）的小鼠模型中，CCTP 缀合物口服给药（剂量低至 0.2mg TP 当量/公斤）在减少或消除异种移植瘤方面与相同剂量的 TP 相当，但表现出较低的亚急性毒性，如体重减轻和血液学毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/4dee03f43dd7/IDRD_A_1770370_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/064e8f03a1b4/IDRD_A_1770370_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/55448ac461fb/IDRD_A_1770370_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/b534a1010eea/IDRD_A_1770370_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/58dcaa1a5bfc/IDRD_A_1770370_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/854313ee673e/IDRD_A_1770370_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/307a41e194b2/IDRD_A_1770370_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/4dee03f43dd7/IDRD_A_1770370_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/064e8f03a1b4/IDRD_A_1770370_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/55448ac461fb/IDRD_A_1770370_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/b534a1010eea/IDRD_A_1770370_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/58dcaa1a5bfc/IDRD_A_1770370_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/854313ee673e/IDRD_A_1770370_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/307a41e194b2/IDRD_A_1770370_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10fd/8216443/4dee03f43dd7/IDRD_A_1770370_F0007_C.jpg

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