Preparation, characterization, and cytotoxicity evaluation of self-assembled nanoparticles of diosgenin-cytarabine conjugate

Ai-Mei Liao; Ying Zhang; Yinchen Hou; Ji-Hong Huang; Ming Hui; Kyung-Ku Lee; Kwang Youl Lee; ChangJu Chun

doi:10.1016/j.fct.2021.112101

Preparation, characterization, and cytotoxicity evaluation of self-assembled nanoparticles of diosgenin-cytarabine conjugate

Food Chem Toxicol. 2021 May:151:112101. doi: 10.1016/j.fct.2021.112101. Epub 2021 Mar 5.

Authors

Ai-Mei Liao¹, Ying Zhang², Yinchen Hou³, Ji-Hong Huang⁴, Ming Hui⁵, Kyung-Ku Lee⁶, Kwang Youl Lee⁷, ChangJu Chun⁸

Affiliations

¹ College of Biological Engineering, Henan University of Technology, Zhengzhou, 450001, China; College of Pharmacy, Chonnam National University, Gwangju, 61186, Republic of Korea.
² Department of Cell Biology, School of Medicine, Jiangsu University, Zhenjiang, Jiangsu, 212013, China.
³ College of Food and Biological Engineering, Henan University of Animal Husbandry and Economy, Zhengzhou, 450046, China.
⁴ College of Biological Engineering, Henan University of Technology, Zhengzhou, 450001, China; Henan Provincial Key Laboratory of Biological Processing and Nutritional Function of Wheat, Zhengzhou, 450001, PR China.
⁵ College of Biological Engineering, Henan University of Technology, Zhengzhou, 450001, China.
⁶ Testing and Evaluation Center for Dental Devices, Chonnam National University Dental Hospital, Gwangju, 61186, Republic of Korea.
⁷ College of Pharmacy, Chonnam National University, Gwangju, 61186, Republic of Korea. Electronic address: kwanglee@chonnam.ac.kr.
⁸ College of Pharmacy, Chonnam National University, Gwangju, 61186, Republic of Korea; Henan Provincial Key Laboratory of Biological Processing and Nutritional Function of Wheat, Zhengzhou, 450001, PR China. Electronic address: cchun1130@jnu.ac.kr.

PMID: 33684518
DOI: 10.1016/j.fct.2021.112101

Abstract

Diosgenin (DG) isolated from yam roots revealed various bioactivities and applications as drug carrier. In the present study, a conjugate of DG with cytarabine (Ara-C) was used to prepare the self-assembled nanoparticles (NPs) of DG-Ara-C by a nanoprecipitation method. Dynamic light scattering (DLS) as well as transmission electron microscopy (TEM) were employed to analyze the size and the morphology of NPs, respectively. The stability and absorption of DG-Ara-C NPs were measured. Additionally, the cytotoxicity of the NPs was determined via MTT assay. The results indicated that the average particle size of DG-Ara-C NPs was around 190 nm with a narrow size distribution (PDI = 0.1). TEM showed that DG-Ara-C NPs had a spherical morphology. Compared to free DG or Ara-C, the self-assembled DG-Ara-C NPs exhibited a better anti-tumor activity against solid tumor cells as well as leukemia cells. In conclusion, DG possesses dual role in the self-assembled NPs of DG-Ara-C conjugate, being as a promising anticancer drug and drug carrier.

Keywords: Anti-tumor activity; Cytarabine; Diosgenin; Diosgenin-cytarabine conjugate; Self-assembled nanoparticle.

MeSH terms

Antimetabolites, Antineoplastic / administration & dosage
Antimetabolites, Antineoplastic / chemistry*
Antimetabolites, Antineoplastic / pharmacology
Cell Line, Tumor
Cell Survival / drug effects*
Cytarabine / administration & dosage
Cytarabine / chemistry*
Cytarabine / pharmacology
Diosgenin / administration & dosage
Diosgenin / chemistry*
Diosgenin / pharmacology
Drug Carriers
Drug Screening Assays, Antitumor
Humans
Nanoparticles / chemistry*

Substances

Antimetabolites, Antineoplastic
Drug Carriers
Cytarabine
Diosgenin