A preclinical evaluation of cytarabine prodrug nanofibers assembled from cytarabine-lauric acid conjugate toward solid tumors

Liu, Ruiling; Jiang, Yue; Hu, Xu; Wu, Jilian; Jiang, Wei; Jin, Guoxia; Luan, Yuxia

doi:10.1016/j.ijpharm.2018.09.043

Cited by 14 publications

(3 citation statements)

References 41 publications

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“…Recent research has demonstrated that cytarabine is excreted in saliva by individuals taking large doses of the drug and that this directly and locally promotes the onset of oral mucositis. This finding therefore strongly implies a role for salivary cytarabine secretion in the emergence of cytarabine-associated oral mucositis [3] . Cytarabine is toxic to a variety of mammalian cells in vitro, showing specificity especially in the death of cells in the S phase, slowing the transition of cells from G1 to the S phase, and killing cells that are undergoing DNA synthesis [4] .…”

Section: Introductionmentioning

confidence: 60%

Histopathological Effects of Cytarabine on Rabbit Tongue Tissue and the Possibility of Treatment with Vitamin E.

Alshibib¹

2024

Egyptian Journal of Ear, Nose, Throat and Allied Sciences

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Introduction:This study aimed to investigate the possibility of treating the side effects of cytarabine on the tongue using vitamin E in rabbits. Material and Methods: Three-month-old rabbits weighing 1.5 to 2.0 kg were utilized in this investigation. A total of 18 rabbits were separated into 3 equal groups at random, with each group containing 6 rabbits. Vitamin E was administered orally, and cytarabine was administered intraperitoneally. Each treatment was administered daily for one week, following groups distilled water was administered parenterally to a control group, and A 50 mg/kg dosage of cytarabine was administered to the second group. The third group was given cytarabine 50 mg/kg, and then 5 hours later, it was given vitamin E at a dose of 800 IU. Results:The result revealed The tongue Cytarabine treated group showed hyperkeratosis with hyalinization, ballooning degeneration, necrosis of the epithelial cells degeneration, (Zenker's) of skeletal muscle cells with atrophy, oedema between it, inflammation, and congestion of blood vessels, while the Cytarabine with vitamin E treated group showing intact mucosa with filiform and epithelial cells, and longitudinal and transverse skeletal muscles, also showing mild hyperkeratosis, and degeneration of the epithelial cells and intact fungiform papillae. Conclusions:The conclusion from this study is that vitamin E is a promising treatment for cytarabine's side effects and that combining them has positive effects on treating rabbits' tongue lesions.

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Section: Introductionmentioning

confidence: 60%

Histopathological Effects of Cytarabine on Rabbit Tongue Tissue and the Possibility of Treatment with Vitamin E.

Alshibib¹

2024

Egyptian Journal of Ear, Nose, Throat and Allied Sciences

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“…To examine the sections under a microscope, the blocks were sectioned with a microtome at a thickness of 5 m. The sections were subjected to standard hematoxylin and eosin (H&E) staining procedures. Photomicrographs of each section were taken using a digital camera (canon, japan) using a light microscope to analyze the sections under examination (16).…”

Section: Sample Collection and Tissue Preparationmentioning

confidence: 99%

Histological study of L-carnitine effect against acute hepatotoxicity after cytarabine chemotherapy in male rats

Majed

Hassan

Mousa

et al. 2022

ijhs

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Hepatotoxicity is a common clinical manifestation associated with a wide range of anticancer therapies. Because of the inherent toxicity of anticancer therapies, oncologists must maintain a broad understanding of their effects on the body, including the liver. Therefore, the study was conducted to examine the effects of two doses of L-carnitine on damaged liver as a result of giving cytarabine. Twenty-four male rats were used in the experiment. The rats divided to four group each group with six rats,the first group injected normal saline intraperitoneally and set as control group(G1), the second group injected cytarabine 25 mg/kg/bw, intraperitoneally and set as (G2), the third group injected cytarabine 25 mg/kg/bw and 50 mg/kg/bw, L-carnitine intraperitoneally and set as (G3), the fourth group injected cytarabine 25 mg/kg/bw and 300 mg/kg/bw, L-carnitine intraperitoneally and set as (G4), the study showed that use of L-carnitine reduced the harmful effect of cytarabine in the body when compared to other groups that were injected only with cytarabine at level of (p-value <0.05).The rats treated with L-carnitine have shown significant elevation in CAT and SOD and reduction of the level of MDA.

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“…Compared with CP-4126, SZY-200 is assembled with LA not EA. Liu R et al [27] once synthesized a drug (LA-Ara) based on the conjugation of cytarabine (Ara-C) with LA. The LA increased the lipophilicity of Ara-C and protected its NH 2 group from the enzymatic attachment, thus markedly prolongs its plasma half-life.…”

Section: Szy-200 Could Arrest the Cell Cycle Induce Apoptosis And Signi Cantly Inhibit Bladder Cancer Cells Migrationmentioning

confidence: 99%

Anti-Tumor Activity and Mechanism of Gemcitabine Derivative SZY-200 Assembled from Gemcitabine-Lauric Acid Conjugate on Human Bladder Cancer Cells

Wang

Shao

et al. 2021

Preprint

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Gemcitabine is a first-line drug for the treatment of bladder cancer. One of the most important mechanisms of gemcitabine resistance is the low expression of cellular membrane transporter hENT1. Various derivatives containing fatty acid side chains have been developed in order to facilitate gemcitabine uptake and prolong its retention in cells, such as CP-4126. In this study, the anti-tumor effect and mechanism of a new derivative of gemcitabine named SZY-200 on bladder cancer cells was investigated. SZY-200 was assembled from gemcitabine-lauric acid conjugate. Our data showed that SZY-200 could inhibit the proliferation of bladder cancer cells by inducing cell cycle arrest and apoptosis. The inhibitory effects were comparable to gemcitabine and CP-4126. Importantly, SZY-200 was independent of the membrane transport system in bladder cancer cells. Moreover, we found that lauric acid could also inhibit the proliferation of bladder cancer cells. SZY-200 could downregulate the expressions of PPARG and PTGS2 which were related to the occurrence and development of bladder cancer. Overall, these results indicate that SZY-200 could be an ideal candidate drug for further in vivo investigation.

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A preclinical evaluation of cytarabine prodrug nanofibers assembled from cytarabine-lauric acid conjugate toward solid tumors

Cited by 14 publications

References 41 publications

Histopathological Effects of Cytarabine on Rabbit Tongue Tissue and the Possibility of Treatment with Vitamin E.

Histopathological Effects of Cytarabine on Rabbit Tongue Tissue and the Possibility of Treatment with Vitamin E.

Histological study of L-carnitine effect against acute hepatotoxicity after cytarabine chemotherapy in male rats

Anti-Tumor Activity and Mechanism of Gemcitabine Derivative SZY-200 Assembled from Gemcitabine-Lauric Acid Conjugate on Human Bladder Cancer Cells

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