Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines

Abstract Background Phytochemicals and plant extracts are showing promising anticancer potentials. In the current study, the volatile faction (essential oil) of Nigella sativa seeds was evaluated against some hepatocellular carcinoma (HCC). The essential oil was extracted and characterized by chroma...

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Autores principales:	Ahmed A. Abd-Rabou, Amr E. Edris
Formato:	article
Lenguaje:	EN
Publicado:	BMC 2021
Materias:	Apoptosis Cytotoxicity Nigella sativa Essential oil nanoemulsion HepG2 Huh-7 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/5599eacd028642f4ac4875f76a75e6bf
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spelling	oai:doaj.org-article:5599eacd028642f4ac4875f76a75e6bf2021-11-07T12:18:37ZCytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines10.1186/s12645-021-00101-y1868-69581868-6966https://doaj.org/article/5599eacd028642f4ac4875f76a75e6bf2021-11-01T00:00:00Zhttps://doi.org/10.1186/s12645-021-00101-yhttps://doaj.org/toc/1868-6958https://doaj.org/toc/1868-6966Abstract Background Phytochemicals and plant extracts are showing promising anticancer potentials. In the current study, the volatile faction (essential oil) of Nigella sativa seeds was evaluated against some hepatocellular carcinoma (HCC). The essential oil was extracted and characterized by chromatographic techniques to reveal its chemical composition, especially thymoquinone. Then, the oil was fabricated in two nanoemulsion formulations (F1 and F2), which differ in their composition of surfactants. The cytotoxicity and apoptotic activities of the essential oil and its nanoemulsions were evaluated in vitro against HepG2 and Huh-7 cell lines. Normal WI-38 cell line was also included in that evaluation to study the selectivity and safety of the different formulations on normal cells. Results Gas chromatographic analysis indicated that the essential oil is composed mainly of p-cymene (40.0%), thymoquinone (31.2%) and trans-α-thujene (12.8%). Particle size of the nanoemulsions ranged between 9.4 and 119.7 nm depending on the type of surfactant used in the formulation process. The pure essential oil and its two nanoemulsions (F1 and F2) showed dose-dependent antiproliferative activity against both HCC cells. This activity reached its highest cell inhibition in the case of nanoemulsion (F2) where the proliferation percentage was only 21.9% and 9.2% against HepG2 and Huh-7 cells, respectively. The same nanoemulsion (F2) also showed the lowest IC50 values (55.7 and 35.5 µg/ml) against both HepG2 and Huh-7 cells, respectively, compared to 100 µg/ml for the reference drug Doxorubicin. Flow cytometric analysis also confirmed that nanoemulsion (F2) has the highest apoptotic activity compared to nanoemulsion (F1) and the pure unformulated essential oil. Genetic expressions of pro-apoptotic (Bax) and the anti-apoptotic (Bcl-2) gene markers evaluation revealed that nanoemulsion (F2) has better activity in upregulating (Bax) and down-regulate (Bcl-2) with the highest Bax/Bcl-2 ratio (69) was found against Huh-7 cells. All N. sativa nanoemulsions showed minimal cytotoxicity on the normal WI-38 cell, indicating wide safety margins due to selective properties. Conclusion Overall, the study revealed the potentials of N. sativa essential oil, after formulation in specially tailored nanoemulsion for application as potential adjuvant liver anticancer agent. Graphical AbstractAhmed A. Abd-RabouAmr E. EdrisBMCarticleApoptosisCytotoxicityNigella sativaEssential oil nanoemulsionHepG2Huh-7Neoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancer Nanotechnology, Vol 12, Iss 1, Pp 1-23 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Apoptosis Cytotoxicity Nigella sativa Essential oil nanoemulsion HepG2 Huh-7 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	Apoptosis Cytotoxicity Nigella sativa Essential oil nanoemulsion HepG2 Huh-7 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Ahmed A. Abd-Rabou Amr E. Edris Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
description	Abstract Background Phytochemicals and plant extracts are showing promising anticancer potentials. In the current study, the volatile faction (essential oil) of Nigella sativa seeds was evaluated against some hepatocellular carcinoma (HCC). The essential oil was extracted and characterized by chromatographic techniques to reveal its chemical composition, especially thymoquinone. Then, the oil was fabricated in two nanoemulsion formulations (F1 and F2), which differ in their composition of surfactants. The cytotoxicity and apoptotic activities of the essential oil and its nanoemulsions were evaluated in vitro against HepG2 and Huh-7 cell lines. Normal WI-38 cell line was also included in that evaluation to study the selectivity and safety of the different formulations on normal cells. Results Gas chromatographic analysis indicated that the essential oil is composed mainly of p-cymene (40.0%), thymoquinone (31.2%) and trans-α-thujene (12.8%). Particle size of the nanoemulsions ranged between 9.4 and 119.7 nm depending on the type of surfactant used in the formulation process. The pure essential oil and its two nanoemulsions (F1 and F2) showed dose-dependent antiproliferative activity against both HCC cells. This activity reached its highest cell inhibition in the case of nanoemulsion (F2) where the proliferation percentage was only 21.9% and 9.2% against HepG2 and Huh-7 cells, respectively. The same nanoemulsion (F2) also showed the lowest IC50 values (55.7 and 35.5 µg/ml) against both HepG2 and Huh-7 cells, respectively, compared to 100 µg/ml for the reference drug Doxorubicin. Flow cytometric analysis also confirmed that nanoemulsion (F2) has the highest apoptotic activity compared to nanoemulsion (F1) and the pure unformulated essential oil. Genetic expressions of pro-apoptotic (Bax) and the anti-apoptotic (Bcl-2) gene markers evaluation revealed that nanoemulsion (F2) has better activity in upregulating (Bax) and down-regulate (Bcl-2) with the highest Bax/Bcl-2 ratio (69) was found against Huh-7 cells. All N. sativa nanoemulsions showed minimal cytotoxicity on the normal WI-38 cell, indicating wide safety margins due to selective properties. Conclusion Overall, the study revealed the potentials of N. sativa essential oil, after formulation in specially tailored nanoemulsion for application as potential adjuvant liver anticancer agent. Graphical Abstract
format	article
author	Ahmed A. Abd-Rabou Amr E. Edris
author_facet	Ahmed A. Abd-Rabou Amr E. Edris
author_sort	Ahmed A. Abd-Rabou
title	Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
title_short	Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
title_full	Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
title_fullStr	Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
title_full_unstemmed	Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
title_sort	cytotoxic, apoptotic, and genetic evaluations of nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines
publisher	BMC
publishDate	2021
url	https://doaj.org/article/5599eacd028642f4ac4875f76a75e6bf
work_keys_str_mv	AT ahmedaabdrabou cytotoxicapoptoticandgeneticevaluationsofnigellasativaessentialoilnanoemulsionagainsthumanhepatocellularcarcinomacelllines AT amreedris cytotoxicapoptoticandgeneticevaluationsofnigellasativaessentialoilnanoemulsionagainsthumanhepatocellularcarcinomacelllines
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Cytotoxic, apoptotic, and genetic evaluations of Nigella sativa essential oil nanoemulsion against human hepatocellular carcinoma cell lines

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