Investigation into the bioavailability of synthesized phytosterol esters in vitro and in vivo using Caco-2 cell model and Wistar rats

WANG, Shirang; YU, Dianyu; SHI, Yongge; JIANG, Lianzhou; YANG, Fuming; YU, Guoping

doi:10.1590/fst.68620

Acessibilidade / Reportar erro

Brasil

Food Science and Technology

Español English

Brasil

Español English

sumário « anterior atual seguinte »

Sumário

Original Article • Food Sci. Technol (Campinas) 42 • 2022 • https://doi.org/10.1590/fst.68620 copy

Investigation into the bioavailability of synthesized phytosterol esters in vitro and in vivo using Caco-2 cell model and Wistar rats

Authorship SCIMAGO INSTITUTIONS RANKINGS

Abstract

Phytosterols are bioactive components capable of reducing the level of cholesterol in serum. In this study, phytosterol acetic ester (PA), phytosterol oleate ester (PO) and phytosterol linoleic ester (PL) were synthesized from phytosterol (PS) and organic acid to improve the solubility of phytosterols in oil. The purities of PA, PO and PL were 98.4, 95.9 and 95.7%, respectively. Caco-2 cell monolayers and Wistar rats were used to research the bioavailability of synthesized esters (PE) in vitro and in vivo. Experiments using the Caco-2 cell monolayer model showed that the transport mechanism of phytosterol esters was passive transport. Experiments in vivo showed that the PS content in rat blood reached the highest level at 3 h, with a value of 21.82 μg/mL. PS content in the liver was the highest at 3 h, with a value of 43.65 μg/g. Bioavailability of PL is the highest, reaching a value as high as 19.57%. Acute study in the rats showed that the PS concentration in blood was at the safe level, and it had no side effects for health. In conclusion, the bioavailability of PL and PO is better than PS, PL and PO have more advantages in application.

Keywords:
phytosterol esters; cell model; in vivo absorption; bioavailability

Time (d)	Activity of alkaline phosphatase
Time (d)	Apical side	Basolateral side	AP/BL
0	0	0	----
5	16.2^c ± 0.22	11.8^c ± 0.18	1.37
15	40.5^b ± 0.32	13.9^b ± 0.21	2.91
21	68.1^a ± 0.78	15.3^a ± 0.23	4.45

propranolol hydrochloride (μg/mL)	P_app(×10^-5cm/s)
40	1.73 ± 0.19
60	1.71 ± 0.22
80	1.64 ± 0.15
100	1.57 ± 0.21

		1 h	2 h	3 h	4 h	5 h
PS	high dose	3.68^c ± 0.54	5.49^b ± 0.71	7.71^a ± 0.64	7.38^a ± 0.98	6.97^a ± 0.74
PS	middle dose	3.19^c ± 0.42	4.62^b ± 0.33	6.29^a ± 0.61	5.78^a ± 0.64	5.27^ab ± 0.72
PA	high dose	3.91^c ± 0.74	6.19^b ± 0.58	8.47^a ± 0.82	7.91^a ± 0.92	7.51^ab ± 0.49
PA	middle dose	4.01^c ± 0.57	5.29^b ± 0.75	7.12^a ± 0.82	6.51^ab ± 0.56	5.91^ab ± 0.62
PO	high dose	9.28^d ± 0.84	13.39^c ± 1.32	18.91^a ± 1.04	17.02^b ± 0.98	15.34^b ± 0.47
PO	middle dose	7.29^d ± 0.81	11.37^c ± 0.95	16.21^a ± 1.12	14.53^ab ± 0.83	13.86^b ± 0.98
PL	high dose	10.73^d ± 0.66	14.87^bc ± 1.29	21.82^a ± 1.36	18.03^b ± 0.87	16.26^b ± 0.75
PL	middle dose	8.73^d ± 0.77	13.89^c ± 1.26	19.48^a ± 1.17	17.18^b ± 1.25	15.67^bc ± 1.27

		heart	liver	spleen	lung	kidney
PS	high dose	14.17^b ± 0.49	16.35^a ± 0.64	11.13^c ± 0.53	9.02^d ± 0.38	8.31^d ± 0.42
PS	middle dose	12.03^b ± 0.44	13.25^a ± 0.48	9.84^c ± 0.29	7.93^d ± 0.47	6.84^e ± 0.31
PA	high dose	14.74^b ± 0.51	17.02^a ± 0.73	11.65^c ± 0.56	9.23^d ± 0.42	8.49^d ± 0.37
PA	middle dose	12.61^b ± 0.53	13.76^a ± 0.43	10.25^c ± 0.48	8.17^d ± 0.35	7.18^e ± 0.39
PO	high dose	34.21^b ± 1.71	38.72^a ± 1.33	26.74^c ± 0.83	20.12^d ± 0.38	19.22^d ± 0.78
PO	middle dose	30.47^a ± 1.82	32.11^a ± 1.51	24.28^b ± 0.97	18.33^c ± 0.42	17.19^c ± 0.54
PL	high dose	37.67^b ± 1.35	43.65^a ± 1.42	30.06^c ± 0.91	25.02^d ± 0.69	23.45^d ± 0.85
PL	middle dose	35.42^a ± 1.71	36.53^a ± 1.27	27.43^b ± 0.79	21.79^c ± 0.83	20.39^c ± 0.78

		PS content	PS excretion proportion	PE content	PE excretion proportion	total excretion proportion
PS	high dose	49.28^a ± 2.19	98.56^a ± 1.10	----	----	98.56^a ± 1.10
	middle dose	24.32^a ± 1.78	97.28^a ± 1.78	----	----	97.28^a ± 1.78
	low dose	2.40^a ± 0.27	95.91^a ± 2.72	----	----	95.91^a ± 2.72
PA	high dose	35.46^b ± 2.73	70.91^c ± 1.37	13.52^a ± 1.14	27.03^a ± 0.61	97.94^a ± 1.98
	middle dose	17.43^c ± 1.73	69.71^c ± 0.43	6.61 ± 0.84	26.42 ± 0.21	96.13^a ± 0.64
	low dose	2.02^a ± 0.21	80.79^b ± 0.21	0.37 ± 0.13	14.89 ± 0.13	95.68^a ± 0.34
PO	high dose	45.81^a ± 2.17	92.20^b ± 1.29	0.29^b ± 0.11	0.58^b ± 0.21	92.78^b ± 1.50
	middle dose	21.32^b ± 1.17	85.27^b ± 1.17	----	----	85.27^b ± 1.17
	low dose	2.08^a ± 0.27	83.12^b ± 2.74	----	----	83.12^b ± 2.74
PL	high dose	45.46^a ± 2.35	91.41^b ± 1.37	0.24^b ± 0.09	0.49^b ± 0.19	91.90^b ± 1.56
	middle dose	20.89^b ± 1.35	83.54^b ± 1.35	----	----	83.54^b ± 1.35
	low dose	2.01^a ± 0.39	80.43^b ± 1.89	----	----	80.43^b ± 1.89

Sociedade Brasileira de Ciência e Tecnologia de Alimentos Av. Brasil, 2880, Caixa Postal 271, 13001-970 Campinas SP - Brazil, Tel.: +55 19 3241.5793, Tel./Fax.: +55 19 3241.0527 - Campinas - SP - Brazil
E-mail: revista@sbcta.org.br

Acompanhe os números deste periódico no seu leitor de RSS

[1] *Corresponding author: yfmhj@163.com, yuguopingneau@hotmail.com