J Food Bioact

Journal of Food Bioactives, ISSN 2637-8752 print, 2637-8779 online

Journal website www.isnff-jfb.com

Original Research

Volume 2, Number , June 2018, pages 82-90

Absorption of polymethoxyflavones and their derivatives

Figures

Figure 1.
Caco-2 cell viability after treated with PMFs and their derivatives at a concentration of 20 μM.
Each bar was expressed as a mean ± SEM (n = 6). Cell viability was above 95% for all the PMFs and their derivatives at 20 μM concentration, meaning PMFs are not cytotoxic at this concentration. (NOB: nobiletin, known positive control).

Scheme 1.
Structures and preparation of polymethoxyflavones and related acetyl derivatives.

Figure 2.
Inhibitory effects of HeptaMF, 5-OHHeptaMF, and 5-AcHeptaMF on Caco-2 cells.
Each point represents mean ± SEM (n = 6). For all three compounds, the relative cell viability decreases as the concentration increases. 5-AcHeptaMF had the most outstanding inhibitory effect on human colon cancer cells.

Figure 3.
Permeability rates of PMFs and their derivatives as a function of time.
Each point represents mean ± SEM (n = 3). Data was presented in both apical to basolateral (AP-BL) and basolateral to apical (BL-AP) direction, which reflects absorption and efflux process respectively.

Figure 4.
Total permeability rates of 5-AcSIN and 5-AcHeptaMF with the amount of deacetylation adjusted.
Each point represents mean ± SEM (n = 3). Data indicates that 5-AcPMFs had better permeability than their corresponding 5-OHPMFs.

Tables

**Table 1.** Partition coefficient (log P) of PMFs and their derivatives
PMFs	SIN	5-OH-SIN	5-AcSIN	HeptaMF	5-OHHeptaMF	5-AcHeptaMF
Note: Each data represents mean ± SEM (n = 3). *Data is lacking due to either no peak detected in water layer or peak area in water layer under reliable range.
Partition coefficient (log P)	1.76 ± 0.22	NA*	NA*	1.97 ± 0.22	NA*	NA*

**Table 2.** Apparent permeability coefficient and efflux ratio of tested PMFs and their derivatives
	Papp (AP-BL) cm s⁻¹ × 10⁻⁷	Papp (BL-AP) cm s⁻¹ × 10⁻⁷	EfR
SIN	1,042	47	0.05
5-OHSIN	108	138	1.28
5-AcSIN	543	794	1.46
HeptaMF	1,091	320	0.29
5-OHHeptaMF	133	138	1.04
5-AcHeptaMF	132	190	1.44