結論 - 芝麻酚類成分之代謝動力學及清除自由基活性評估; Metabolic Pharmacokinetics of Sesame Phenols and Evaluation of Fre

ㄧ、口服以 PEG 400 溶解之芝麻酚並無原形分子存在，主要以其結合態代謝物存在於體循環中，且硫酸結合態代謝物濃度高於葡萄糖醛酸結合態代謝物，顯示芝麻酚硫酸結合態代謝物於體內發揮藥理活性之可能性不可忽略。

二、口服以蒸餾水溶解之芝麻酚，於投藥後一小時內有原形分子存在，

但主要仍以其結合態代謝物存在於體循環中，且硫酸結合態代謝物濃度高於葡萄糖醛酸結合態代謝物，顯示芝麻酚硫酸結合態代謝物於體內發揮藥理活性之可能性不可忽略。

三、芝麻酚溶於 PEG 400 及蒸餾水中會產生不同之代謝動力學行為，顯示溶媒對芝麻酚之代謝動力學產生影響。

四、芝麻酚及其結合態代謝物具清除 DPPH 自由基之活性。

五、芝麻酚對 AAPH 所誘導之紅血球溶血具抑制的作用，但其結合態代謝物卻不具此活性。

六、芝麻木酚素 sesaminol triglucoside 代謝動力學之初探顯示，其能被腸道菌所水解，但 sesaminol 未出現於血中。

Minutes Detector A (290nm)

2-15S

Detector A (290nm) 2-15G

Detector A (290nm) 2-15F

Fig. 1 HPLC chromatograms of (a) sesamol in serum (b) serum hydrolyzed with sulfatase (c) serum hydrolyzed with glucuronidase

(a) (b) (c) Sesamol

6,7-DMC

T im e (m in )

Fig. 2 (a):Mean (± S.E.) serum concentration-time profiles of sesamol (^▼), sesamol sulfate (^●), sesamol glucuronide (^○) after intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats.

(b): the semi-log diagram of (a).

T im e(m in)

0 200 400 600 800 1000 1200 1400 1600

Sesamolconcentration(nmol/mL)

0 20 40 60 80 100 120 140

S esam ol sulfate S esam ol glucuronide

(a)

T im e (m in)

0 2 00 4 00 6 00 8 00 100 0 120 0 1 40 0 16 00

Sesamolconcentration(nmol/mL)

0.1 1 1 0 10 0

1 00 0 S e sam o l s ulfa te

S e sam o l g lu cu ro nid e

(b)

Fig. 3 (a):Mean (± S.E.) serum concentration-time profiles of sesamol sulfate (^●), sesamol glucuronide (^○) after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats.

(b): the semi-log diagram of (a).

T im e(m in)

0 200 400 600 800 1000 1200 1400 1600

Sesamolconcentration(nmol/mL)

S esam ol sulfate S esam ol glucuronide S esam ol

(b)

Fig. 4 (a):Mean (± S.E.) serum concentration-time profiles of sesamol (^▼), sesamol sulfate (^●), sesamol glucuronide (^○) after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats.

(b): the semi-log diagram of (a).

T im e(m in)

Fig. 5 (a):Mean (± S.E.) serum concentration-time profiles of sesamol sulfate (^●),sesamol glucuronide (^○) after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats.

(b): the semi-log diagram of (a).

Tim e (m in)

0 200 400 600 800 1000 1200 1400 1600

Sesamolconcentration(nmol/mL)

0 100 200 300

400 S esam ol sulfate

S esam ol glucuronide S esam ol

(a)

Tim e (m in)

0 100 200 300 400 500 600

Sesamolconcentration(nmol/mL)

0.1 1 10 100

1000 S esam ol sulfate

S esam ol glucuronide S esam ol

(b)

Fig. 6 (a):Mean (± S.E.) serum concentration-time profiles of sesamol (^▼), sesamol sulfate (^●), sesamol glucuronide (^○) after intravenous administration of sesamol in water (10 mg/kg) to six rats.

(b): the semi-log diagram of (a).

Tim e (m in)

0 500 1000 1500 2000 2500 3000 3500

Sesamolconcentration(nmol/mL)

0 200 400 600 800

1000 Sesam ol sulfate

Sesam ol glucuronide Sesam ol

(a)

Tim e (m in)

0 200 400 600 800 1000 1200 1400 1600

Sesamolconcentration(nmol/mL)

1 10 100 1000 10000

Sesam ol sulfate Sesam ol glucuronide Sesam ol

(b)

Fig. 7 (a):Mean (± S.E.) serum concentration-time profiles of sesamol (^▼), sesamol sulfate (^●), sesamol glucuronide (^○) after oral

administration of sesamol in water (50 mg/kg) to six rats.

(b): the semi-log diagram of (a).

T im e (m in)

0 500 1000 1500 2000 2500 3000 3500

Sesamolconcentration(nmol/mL)

S esam ol sulfate S esam ol glucuronide S esam ol

Fig. 8 (a):Mean (± S.E.) serum concentration-time profiles of sesamol (^▼), sesamol sulfate (^●), sesamol glucuronide (^○) after oral

administration of seven doses of sesamol in water (50 mg/kg) to six rats.

(b): the semi-log diagram of (a).

Fig. 9 DPPH scavenging potential of (a) serum metabolites without SPE pretreatment (b) serum metabolites after SPE pretreatment

blank serum 1x

sulfate/glucuronide (310 μM/2 μM)

blank serum0.5x

sulfate/glucuronide (155 μM/1 μM)

blank serum 1x

sulfate/glucuronide (190 μM/1 μM)

blank serum0.5x

sulfate/glucuronide (95 μM/0.5 μM)

Fig. 10 DPPH scavenging potential of (a) serum metabolites without SPE pretreatment (b) serum metabolites after SPE pretreatment in various concentrations.

concentration

0.7 Blank serum

Serum metabolites

Fig. 11 Comparison of DPPH scavenging potential of sesamol and ascorbic acid in various concentrations to PBS.

Concentration(M)

Fig. 12 Effects of (a) serum metabolites without SPE pretreatment (b) serum metabolites with SPE pretreatment AAPH-induced hemolysis at various concentrations.

Blank serum 1x Blank serum 0.5x

Sulfate/glucuronide (310M/2 M) Sulfate/glucuronide (156M/1 M) Without AAPH

0.8 Blank serum 1x

Blank serum 0.5x

Sulfate/glucuronide (190M/1 M) Sulfate/glucuronide (95M/ 0.5 M) Without AAPH

Fig. 13 Effects of sesamol (a) and ascorbic acid (b) on AAPH-induced hemolysis of rat erythrocytes in vitro. Data are expressed as mean ± S.D. of triplicates.

Time (h)

Minutes Detecto r A (290nm)

Blan k-1 Detecto r A (290nm)

1-1

14-(3)

Fig. 14-(1)~(6) Sesaminol triglucoside (ST) 與鼠便培養之層析指紋圖譜 Detector A (290nm)

10-1

Fig. 15 HPLC chromatogram of sesaminol in sesame extract

Fig. 16 Sesaminol triglucoside 之層析指紋圖譜

Minutes

Minutes Detecto r A (290nm)

芝麻 ST抽血時間點沒解 芝麻 ST抽血時間點沒解2-30.dat

Detector A (290n m) 芝麻 ST抽血時間點沒解 芝麻 ST抽血時間點沒解F2-30.dat

17-(3)

Fig. 17-(1)~(6) 餵食單次 sesaminol triglucoside 後各時間點血清以 sulfatase Detector A (290nm)

芝麻 ST抽血時間點沒解 芝麻 ST抽血時間點沒解2-2. dat

Detector A (290nm) 芝麻 ST抽血時間點沒解 Detector A (290nm)

芝麻 ST抽血時間點沒解 芝麻 ST抽血時間點沒解2-4. dat

Detector A (290nm) 芝麻 ST抽血時間點沒解 芝麻 ST抽血時間點沒解F2-4.dat

17-(6)

Minutes

Fig. 18-(1)~(4) 單次餵食 sesaminol 後各時間點血清以 sulfatase 水解後之層析圖 (1) 5 min; (2) 15 min; (3) 30 min; (4) 60 min Detector A (290nm)

芝麻跑 80-20%

18-(4)

Fig. 20-(1)~(4)餵食單次富含 sesaminol triglucoside 芝麻粉後各時間點血清 以 sulfatase 水解後之層析圖

(1) 15 min; (2) 30 min; (3) 60 min; (4) 120 min

Minut es

Fig. 21-(1)~(5) 餵食七次富含 sesaminol triglucoside 芝麻粉後各時間點血清以 sulfatase 水解後之層析圖

(1) 5 min; (2) 15 min; (3) 30 min; (4) 60 min (5) 120 min

Minut es

0 5 10 15 20 25 30 35 40 45 50

Volts

0.000 0.005 0.010 0.015 0.020 0.025 0.030

Volts

0.000 0.005 0.010 0.015 0.020 0.025 0.030 D etecto r A (290n m)

21-(5)

Fig. 22-(1)~(4) 餵食七次富含 sesaminol triglucoside 芝麻粉後各組織以 sulfatase 水解前(下線) 與水解後 (上線)之層析圖

(1) blank liver; (2) blank kidney; (3) liver; (4) kidney

0 5 1 0 1 5 2 0 2 5 3 0 3 5 4 0 4 5 5 0

D etector A (290nm) 1-K i dney-S

D etector A (290nm) 1-L iver -S

22-(3)

Minut es

Fig. 23-(1)~(8)餵食單次 sesamin 後各時間點血清 sulfatase 水解後之層析圖

(1) 5 min; (2) 15 min; (3) 30 min; (4) 60 min (5) 120 min; (6) 180 min; (7) 240 min; (8) 360 min 23-(5)

23-(8) 23-(7) 23-(6)

Fig. 24-(1)~(2) 餵食單次富含 sesamin 芝麻粉後各組織以 sulfatase 水解前(下線)與水解後 (上線)之層析圖

(1) liver; (2) kidney

Compound 1：R₁=H Compound 2：R₂=H Compound 3：R₁=CH₃ Compound 4：R₂=CH₃

(Nakai et al., 2003)

Minutes Detector A (290n m) 0.10

3-Ki dney-F

Detecto r A (290n m) 3-K idney-S

24-(2)

Table 1. Intra-run and inter-run analytical precision and accuracy of sesamol in rat

Table 2. Recovery (%) of sesamol from rat serum (n=3).

Conc.

Table 3. Concentration of sesamol (nmoL/mL) in serum after intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats

N.D.: not detectable

Table 4. Concentration of sesamol sulfate (nmoL/mL) in serum after

intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats

N.D.: not detectable Time

5 58.8 75.9 29.8 9.5 78.8 50.6±13.5

15 20.9 51.9 46.3 64.6 26.4 42.0±8.1

30 19.4 49.5 30.5 37.4 24.5 32.3±5.3

60 6.2 33.2 24.1 4.6 12.5 16.1±5.5

Table 5. Concentration of sesamol glucuronide (nmoL/mL) in serum after intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats

N.D.: not detectable Time

(min) 1 2 3 4 5 Mean±S.E.

5 1.9 N.D. 1.6 8.0 7.1 3.7±1.6

15 1.9 3.1 2.3 6.5 3.8 3.5±0.8

30 1.4 3.7 1.8 6.9 3.8 3.5±1.0

60 N.D. 6.5 1.4 3.4 1.5 2.6±1.1

120 N.D. 1.7 N.D. N.D. N.D. 0.3±0.3

240 N.D. N.D. 5.4 N.D. N.D. 1.1±1.1

480 N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 6. Pharmacokinetic parameters of sesamol sulfate in serum after intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats

Parameters 1 2 3 4 5 Mean±S.E.

T_max(min) 0 0 15 15 0 6.0±3.7

C_max(nmol/mL) 98.6 91.8 46.3 64.6 136.2 87.5±15.4

AUC_0-1440

(nmol．min/mL) 1806.3 5052.1 4794.3 2518.7 2537.3 3341.7±660.2

MRT_0-1440(min) 32.0 57.0 103.6 99.6 32.3 64.9±15.7

Table 7. Pharmacokinetic parameters of sesamol glucuronide in serum after intravenous administration of sesamol in PEG 400 (5 mg/kg) to five rats

Parameters 1 2 3 4 5 Mean±S.E.

Tmax(min) 0 60 15 0 0 15.0±11.6

Cmax(nmol/mL) 2.0 6.5 2.3 8.8 9.7 5.9±1.6

AUC0-1440

(nmol．min/mL) 53.7 462.9 100.8 368.7 231.7 243.6±77.6

MRT0-1440(min) 13.9 57.6 28.9 24.9 21.0 29.3±7.5

Table 8. Comparison of pharmacokinetic parameters of sesamol sulfate and glucuronide after intravenous administration of sesamol in PEG 400 (5

mg/kg) to five rats

Parameters Sulfate Glucuronide

Tmax(min) 6.0±3.7 15.0±11.6

Cmax(nmol/mL) 87.5±15.4 ** 5.9±1.6

AUC0-1440

(nmol．min/mL) 3341.7±660.2 ** 243.6±77.6

MRT0-1440(min) 64.9±15.7 29.3±7.5

Data expressed as Mean±S.E. **p<0.01

Table 9. Concentration of sesamol sulfate (nmoL/mL) in serum after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats

N.D.: not detectable

Table 10. Concentration of sesamol glucuronide (nmoL/mL) in serum after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats

N.D.: not detectable Time

(min) 1 2 3 4 5 Mean±S.E.

5 200.9 120.0 67.0 101.9 31.5 104.3±28.5

15 71.0 170.1 53.7 66.4 20.8 76.4±25.0

30 76.5 71.8 44.9 36.3 34.7 52.9±8.9

60 32.0 99.4 125.5 22.2 8.7 57.6±23.1

120 53.9 65.3 165.5 25.1 5.3 63.0±27.7

240 35.2 11.1 52.8 38.9 15.5 30.7±7.7

480 11.4 N.D. 9.3 2.1 12.0 7.0±2.5

720 16.5 N.D. N.D. N.D. 4.5 4.2±3.2

1440 2.6 N.D. N.D. N.D. 3.0 1.1±0.7

Time

(min) 1 2 3 4 5 Mean±S.E.

5 19.4 4.2 2.0 2.9 3.6 6.4±3.3

15 7.1 4.0 6.4 0.0 1.8 3.9±1.3

30 8.1 2.9 4.1 6.3 1.7 4.6±1.2

60 5.5 10.0 6.9 2.5 N.D. 5.0±1.7

120 8.0 11.3 8.8 9.7 N.D. 7.6±2.0

240 2.2 3.6 2.2 4.6 N.D. 2.5±0.8

480 N.D. N.D. N.D. 1.5 N.D. 0.3±0.3

720 N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 11. Pharmacokinetic parameters of sesamol sulfate in serum after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats

Parameters 1 2 3 4 5 Mean±S.E.

T_max(min) 5 15 120 5 30 35.0±21.7

C_max(nmol/mL) 200.9 170.1 165.5 101.9 34.7 134.6±29.7 AUC_0-1440

(nmol．min/mL) 26870.5 16334.8 33647.4 12427.0 10559.8 19967.9±4434.8

MRT_0-1440(min) 381.9 94.9 156.2 162.1 482.4 255.5±74.8

Table 12. Pharmacokinetic parameters of sesamol glucuronide in serum after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats

Parameters 1 2 3 4 5 Mean±S.E.

Tmax(min) 5 120 120 120 5 74.0±28.2

Cmax(nmol/mL) 19.4 11.3 8.8 9.7 3.6 10.6±2.6

AUC0-1440

(nmol．min/mL) 1359.8 1856.2 1327.5 2053.2 62.3 1331.8±347.0

MRT0-1440(min) 90.4 138.6 108.9 208.4 13.8 112.0±31.7

Table 13. Comparison of pharmacokinetic parameters of sesamol sulfate and

glucuronide after oral administration of sesamol in PEG 400 (30 mg/kg) to five rats

Parameters Sulfate Glucuronide

Tmax(min) 35.0±21.7 74.0±28.2

Cmax(nmol/mL) 134.6±29.7 * 10.6±2.6

AUC0-1440

(nmol．min/mL) 19967.9±4434.8 * 1331.8±347.0

MRT_0-1440(min) 255.5±74.8 112.0±31.7

Data expressed as Mean±S.E. *p<0.05

Table 14. Concentration of sesamol (nmoL/mL) in serum after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

N.D.: not detectable

Table 15. Concentration of sesamol sulfate (nmoL/mL) in serum after

intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

N.D.: not detectable Time

5 95.5 168.8 98.6 137.5 116.2 16.2 88.4 103.0±17.9

15 95.4 132.6 57.8 70.2 80.0 33.7 78.4 78.3±11.7

30 69.3 108.0 70.5 74.6 60.0 48.0 38.3 67.0±8.4

60 40.5 66.4 49.2 32.8 42.7 22.8 10.1 37.8±6.9

120 8.7 34.3 8.6 5.8 7.4 8.8 4.1 11.1±3.9

240 1.3 3.9 11.6 N.D. 2.0 1.9 2.6 3.3±1.5

480 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 16. Concentration of sesamol glucuronide (nmoL/mL) in serum after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 7 Mean±S.E.

5 8.7 6.1 35.7 17.8 3.1 5.2 2.8 11.3±4.5

15 3.3 10.2 5.5 3.5 6.2 3.0 8.2 5.7±1.0

30 N.D. 26.8 6.0 7.7 7.0 7.4 6.7 8.8±3.2

60 1.5 23.6 6.0 3.6 3.8 9.8 1.8 7.2±2.9

120 N.D. 4.4 2.7 N.D. 1.4 1.5 N.D. 1.4±0.6

240 N.D. N.D. 1.2 N.D. N.D. N.D. N.D. 0.2±0.2

480 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 17. Pharmacokinetic parameters of sesamol sulfate in serum after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

Parameters 1 2 3 4 5 6 7 Mean±S.E.

T_max(min) 0 0 0 0 0 30 0 4.3±4.3

C_max(nmol/mL) 95.6 190.5 128.7 192.4 140.2 48.0 93.9 127.0±20.0

AUC_0-1440

(nmol．min/mL) 6394.0 12132.0 7050.0 5720.0 6279.0 3554.3 3725.0 6407.8±1080.2

MRT_0-1440(min) 45.5 58.4 64.4 31.2 45.3 62.7 41.3 49.8±4.7

Table 18. Pharmacokinetic parameters of sesamol glucuronide in serum after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

Parameters 1 2 3 4 5 6 7 Mean±S.E.

Tmax(min) 0 30 0 0 30 0 15 10.7±5.4

Cmax(nmol/mL) 14.0 26.8 91.3 40.0 7.0 7.0 8.2 27.8±11.6

AUC0-1440

(nmol．min/mL) 163.1 1967.6 1283.6 503.7 471.3 746.0 301.4 776.7±241.3

MRT0-1440(min) 13.8 50.7 53.7 19.3 45.3 50.3 25.9 37.0±6.3

Table 19. Comparison of pharmacokinetic parameters of sesamol sulfate and

glucuronide after intravenous administration of sesamol in PEG 400 (10 mg/kg) to seven rats

Parameters Sulfate Glucuronide

Tmax(min) 4.3±4.3 10.7±5.4

Cmax(nmol/mL) 127.0±20.0 ** 27.8±11.6

AUC0-1440

(nmol．min/mL) 6407.8±1080.2 *** 776.7±241.3

MRT0-1440(min) 49.8±4.7 ** 37.0±6.3

Data expressed as Mean±S.E. **p<0.01 ***p<0.001

Table 20. Concentration of sesamol sulfate (nmoL/mL) in serum after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats

N.D.: not detectable

Table 21. Concentration of sesamol glucuronide (nmoL/mL) in serum after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 7 Mean±S.E.

5 80.7 192.5 137.4 169.4 9.3 191.3 199.7 140.0±26.9 15 61.2 300.0 51.5 31.1 55.8 130.4 139.7 110.0±35.3 30 13.8 170.0 58.0 76.7 28.0 139.2 93.8 82.8±21.4

60 15.4 76.7 26.7 99.3 8.6 144.2 53.3 60.6±18.7

120 21.9 145.7 27.5 74.6 31.0 196.3 68.8 80.8±25.1

240 12.0 61.2 27.0 47.2 7.7 42.7 43.8 34.5±7.4

480 52.3 1.6 27.3 7.9 10.1 19.2 11.0 18.5±6.4

720 5.4 2.7 4.8 1.6 3.2 4.4 2.9 3.6±0.5

1440 3.0 2.2 8.6 6.1 N.D. 2.4 N.D. 3.2±1.2

Time

(min) 1 2 3 4 5 6 7 Mean±S.E.

5 1.7 5.3 3.1 10.4 N.D. 6.5 5.8 4.7±1.3

15 N.D. 11.4 N.D. 8.0 1.0 9.8 3.2 4.8±1.8

30 N.D. 10.0 3.3 3.8 N.D. 8.7 2.5 4.0±1.5

60 N.D. 3.7 N.D. 6.2 1.4 8.7 N.D. 2.9±1.3

120 3.4 8.5 1.4 6.5 N.D. 13.5 N.D. 4.8±1.9

240 N.D. 4.3 1.3 1.9 3.1 3.3 N.D. 2.0±0.6

480 1.5 N.D. 5.2 N.D. 1.3 1.4 N.D. 1.3±0.7

720 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 22. Pharmacokinetic parameters of sesamol sulfate in serum after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats

Parameters 1 2 3 4 5 6 7 Mean±S.E.

T_max(min) 5 15 5 5 15 120 5 24.3±16.1

C_max(nmol/mL) 80.7 299.8 137.4 169.4 55.8 196.3 200.0 162.8±30.9

AUC_0-1440

(nmol．min/mL) 22742.5 39048.8 23478.6 27913.3 11991.0 45612.6 24831.0 27945.4±4216.4

MRT_0-1440(min) 451.3 175.3 463.0 280.0 497.0 207.1 177.1 321.5±54.5

Table 23. Pharmacokinetic parameters of sesamol glucuronide in serum after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats

Parameters 1 2 3 4 5 6 7 Mean±S.E.

Tmax(min) 120 15 480 5 240 120 5 140.7±65.2

Cmax(nmol/mL) 3.4 11.4 5.2 10.4 3.1 13.5 6.0 7.6±1.6

AUC0-1440

(nmol．min/mL) 495.6 1592.0 1082.3 1238.0 782.8 2727.0 103.0 1145.8±322.0

MRT0-1440(min) 248.2 108.3 345.1 95.6 270.9 145.9 13.4 175.3±44.0

Table 24. Comparison of pharmacokinetic parameters of sesamol sulfate and

glucuronide after oral administration of sesamol in PEG 400 (50 mg/kg) to seven rats

Parameters Sulfate Glucuronide

Tmax(min) 24.3±16.1 140.7±65.2

Cmax(nmol/mL) 162.8±30.9 ** 7.6±1.6

AUC0-1440

(nmol．min/mL) 27945.4±4216.4 *** 1145.8±322.0

MRT0-1440(min) 321.5±54.5 ** 175.3±44.0

Data expressed as Mean±S.E. **p<0.01 ***p<0.001

Table 25. The regression equations, concentration ranges and correlation coefficients of sesamol in water.

Constituents Regression equations Conc. range(g/mL) r

Sesamol y=0.09540x-0.00153 0.16~200.00 0.998

Table 26. Recovery (%) of sesamol from rat serum (n=3).

Conc.

(μg/mL) 1 2 3 Mean±S.D.

100.0 20.0

2.5

92.2 107.5 102.3

97.2 101.8 102.8

91.9 100.3 102.2

93.8±3.0 103.2±3.8 102.4±0.4

Table 27. Concentration of sesamol (nmoL/mL) in serum after intravenous administration of sesamol in water (10 mg/kg) to six rats

N.D.: not detectable

Table 28. Concentration of sesamol sulfate (nmoL/mL) in serum after

intravenous administration of sesamol in water (10 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 50.6 53.0 70.6 87.9 36.4 77.7 62.7±8.6

15 50.4 17.2 26.0 78.3 18.2 36.2 37.7±10.5

30 25.7 8.4 11.6 27.9 3.2 9.0 14.3±4.5

5 88.5 247.0 239.3 118.1 179.7 221.3 182.3±29.6 15 219.2 241.0 454.4 226.4 223.2 476.2 306.7±55.1 30 261.0 358.0 451.1 170.6 208.9 277.3 287.8±45.8 60 140.7 304.1 257.0 292.9 75.7 180.6 208.5±40.8

120 59.7 50.3 37.0 254.6 9.2 34.6 74.2±40.3

240 10.6 10.1 9.8 57.2 5.2 4.9 16.3±9.0

480 N.D. N.D. N.D. 6.7 4.9 N.D. 1.9±1.4

720 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 29. Concentration of sesamol glucuronide (nmoL/mL) in serum after intravenous administration of sesamol in water (10 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 N.D. 21.4 N.D. N.D. 6.9 N.D. 4.7±3.9

15 1.8 32.2 23.8 N.D. 15.2 10.1 13.9±5.6

30 26.9 44.7 70.5 N.D. 8.3 6.3 26.1±12.2

60 10.8 32.1 7.8 5.8 9.8 33.6 16.7±5.7

120 6.5 6.8 3.3 36.1 N.D. 10.3 10.5±5.8

240 N.D. N.D. N.D. 6.2 N.D. N.D. 1.0±1.1

480 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 30. Pharmacokinetic parameters of sesamol in serum after intravenous administration of sesamol in water (10 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

C_max(nmol/mL) 50.7 92.9 116.4 93.1 51.6 113.9 86.4±13.0

AUC_0-2880

(nmol．min/mL) 1865.1 1110.8 1496.5 2728.7 653.2 1387.7 1540.3±317.1

MRT_0-2880(min) 20.2 14.0 13.9 18.5 8.4 8.5 13.9±2.2

Table 31. Pharmacokinetic parameters of sesamol sulfate in serum after intravenous administration of sesamol in water (10 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

Tmax(min) 30 0 15 60 15 15 22.5±9.2

Cmax(nmol/mL) 261.0 250.1 454.4 292.9 223.2 476.2 326.3±49.3 AUC0-2880

(nmol．min/mL) 21621.0 32363.0 33103.5 54738.0 14594.5 25384.4 30300.7±6182.2

MRT0-2880(min) 64.7 55.8 49.3 119.8 68.6 47.9 67.7±12.0

Table 32. Pharmacokinetic parameters of sesamol glucuronide in serum after intravenous administration of sesamol in water (10 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

Tmax(min) 30 30 30 120 15 60 47.5±17.2

Cmax(nmol/mL) 26.9 44.7 70.5 36.1 15.2 33.6 37.8±8.4

AUC0-2880

(nmol．min/mL) 1304.9 3216.5 2335.5 3878.1 574.1 2090.8 2233.3±541.0

MRT0-2880(min) 54.2 46.1 36.4 127.4 30.5 64.2 59.8±15.8

Table 33. Comparison of pharmacokinetic parameters of sesamol, sesamol sulfate, and sesamol glucuronide after intravenous administration of sesamol in water (10 mg/kg) to six rats

Parameters Tmax

(min)

Cmax

(nmol/mL)

AUC0-2880

(nmol．min/mL) MRT_0-2880(min)

sesamol — ^a 86.4±13.0^a 1540.3±317.1^a 13.9±2.2

sesamol sulfate 22.5±9.2^{a b} 326.3±49.3 30300.7±6182.2 67.7±12.0^a sesamol glucuronide 47.5±17.2^b 37.8±8.4^a 2233.3±541.0^a 59.8±15.8^a Data expressed as Mean±S.E. Means in a row without a common superscript differ P< 0.05

Table 34. Concentration of sesamol (nmoL/mL) in serum after oral administration of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable

Table 35. Concentration of sesamol sulfate (nmoL/mL) in serum after oral administration of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 134.0 426.0 208.3 212.5 79.1 36.8 182.8±61.7

15 25.1 231.5 84.5 100.0 38.5 52.5 88.7±33.7

30 5.8 66.9 22.9 33.1 8.3 12.7 25.0±10.2

60 2.0 4.7 8.5 21.0 4.4 7.2 8.0±3.0

5 513.9 395.8 512.5 442.4 380.4 425.8 445.1±25.5 15 624.6 739.0 776.2 675.2 315.2 481.0 601.9±77.9 30 607.0 1131.5 901.0 783.4 316.2 390.0 688.2±139.2 60 263.4 544.3 319.1 358.7 222.3 333.7 340.3±49.9

120 136.5 73.4 88.3 131.8 82.4 120.2 105.4±12.2

240 123.4 63.1 39.7 48.8 87.5 45.2 68.0±14.4

480 10.6 19.7 36.5 21.4 8.7 4.6 16.9±5.2

720 2.8 N.D. N.D. 4.5 10.4 2.5 3.4±1.7

1440 3.3 N.D. N.D. 4.2 8.7 3.7 3.3±1.4

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 36. Concentration of sesamol glucuronide (nmoL/mL) in serum after oral administration of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 6.4 N.D. N.D. N.D. 9.3 63.6 13.2±11.2

15 32.8 44.1 19.1 53.3 9.0 N.D. 26.4±9.2

30 25.4 66.6 53.5 139.0 52.6 22.4 59.9±19.0

60 9.7 59.4 21.6 101.6 33.3 48.4 45.7±14.6

120 8.2 10.6 7.5 45.9 6.5 12.6 15.2±6.8

240 4.9 N.D. N.D. 9.8 4.2 2.6 3.6±1.6

480 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 37. Pharmacokinetic parameters of sesamol in serum after oral administration of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

T_max(min) 5 5 5 5 5 15 6.7±1.8

C_max(nmol/mL) 134.0 426.0 208.3 212.5 79.1 52.5 185.4±60.2

AUC_0-2880

(nmol．min/mL) 1478.7 7665.4 3261.1 3904.6 1326.6 1325.4 3160.3±1103.0

MRT_0-2880(min) 10.4 14.2 14.3 17.4 14.9 19.8 15.2±1.4

Table 38. Pharmacokinetic parameters of sesamol sulfate in serum after oral administration of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

Tmax(min) 15 30 30 30 5 15 20.8±4.8

Cmax(nmol/mL) 624.6 1131.5 901.0 783.4 380.4 481.0 717.0±124.5 AUC0-2880

(nmol．min/mL) 76981.2 82476.0 67658.2 75325.4 57277.3 55563.0 69213.5±4918.6

MRT0-2880(min) 156.3 85.3 94.7 153.3 256.4 140.2 147.7±27.3

Table 39. Pharmacokinetic parameters of sesamol glucuronide in serum after oral administration of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

Tmax(min) 15 30 30 30 30 5 23.3±4.8

Cmax(nmol/mL) 32.8 67.0 53.5 139.0 52.6 64.0 68.2±16.4

AUC0-2880

(nmol．min/mL) 2497.0 5040.0 2640.0 13086.0 3703.0 4449.0 5235.8±1776.2

MRT0-2880(min) 83.7 49.9 47.4 77.6 69.8 72.3 66.8±6.6

Table 40. Comparison of pharmacokinetic parameters of sesamol, sesamol sulfate, and sesamol glucuronide after oral administration of sesamol in water (50 mg/kg) to six rats

Parameters Tmax

(min)

Cmax

(nmol/mL)

AUC0-2880

(nmol．min/mL) MRT_0-2880(min)

sesamol 6.7±1.8^a 185.4±60.2^a 3160.3±1103.0^a 15.2±1.4^a

sesamol sulfate 20.8±4.8^{a b} 717.0±124.5 69213.5±4918.6 147.7±27.3 sesamol glucuronide 23.3±4.8^b 68.2±16.4^a 5235.8±1776.2^a 66.8±6.6^a Data expressed as Mean±S.E. Means in a row without a common superscript differ P< 0.05

Table 41. Comparison of pharmacokinetic parameters of sesamol sulfate and glucuronide after intravenous administration of sesamol in PEG 400 and water (10 mg/kg).

Parameters Sesamol in PEG 400 Sesamol in water Sesamol sulfate

Tmax(min) 4.3±4.3 22.5±9.2

Cmax(nmol/mL) 127.0±20.0 326.3±49.3 ***

AUC0-t

(nmol．min/mL) 6407.8±1080.2 30300.7±6182.2 ***

MRT0-t(min) 49.8±4.7 67.7±12.0

Sesamol glucuronide

Tmax(min) 10.7±5.4 47.5±17.2 *

Cmax(nmol/mL) 27.8±11.6 37.8±8.4

AUC0-t

(nmol．min/mL)

776.7±241.3 2233.3±541.0 *

MRT0-t(min) 37.0±6.3 59.8±15.8

Data expressed as Mean±S.E. *p<0.05 ***p<0.001

Table 42. Comparison of pharmacokinetic parameters of sesamol sulfate and glucuronide after oral administration of sesamol in PEG 400 and water (50 mg/kg).

Parameters Sesamol in PEG 400 Sesamol in water Sesamol sulfate

T_max(min) 24.3±16.1 20.8±4.8

C_max(nmol/mL) 162.8±30.9 717.0±124.5 ***

AUC_0-t

(nmol．min/mL) 27945.4±4216.4 69213.5±4918.6 ***

MRT_0-t(min) 321.5±54.5 * 147.7±27.3

Sesamol glucuronide

Tmax(min) 140.7±65.2 23.3±4.8

Cmax(nmol/mL) 7.6±1.6 68.2±16.4 ***

AUC0-t

(nmol．min/mL) 1145.8±322.0 5235.8±1776.2 *

MRT0-t(min) 175.3±44.0 * 66.8±6.6

Data expressed as Mean±S.E. *p<0.05 ***p<0.001

Table 43. Concentration of sesamol (nmoL/mL) in serum after oral administration of seven doses of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable

Table 44. Concentration of sesamol sulfate (nmoL/mL) in serum after oral administration of seven doses of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 29.3 23.5 12.7 17.0 12.9 23.2 19.8±3.0

15 11.0 8.4 3.6 14.2 10.8 3.8 8.6±1.9

5 288.6 188.8 316.1 266.6 376.8 247.6 280.8±28.5 15 238.9 229.8 149.4 583.7 278.2 202.8 280.5±69.1 30 461.4 291.5 469.7 716.0 297.0 206.1 407.0±82.0

60 226.0 95.7 466.3 511.1 86.3 100.4 247.6±86.8

120 65.3 78.0 103.3 176.8 71.7 50.9 91.0±20.3

240 92.5 114.9 72.8 116.8 51.6 19.8 78.1±17.0

480 34.8 34.8 43.9 21.2 40.8 7.8 30.6±6.1

720 10.5 14.8 9.3 4.5 11.1 11.0 10.2±1.5

1440 17.6 7.2 16.2 9.1 23.6 13.7 14.6±2.7

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 45. Concentration of sesamol glucuronide (nmoL/mL) in serum after oral administration seven doses of sesamol in water (50 mg/kg) to six rats

N.D.: not detectable Time

(min) 1 2 3 4 5 6 Mean±S.E.

5 1.0 N.D. 4.9 2.7 9.8 N.D. 3.1±1.7

15 41.4 14.8 19.5 0.6 7.2 12.9 16.1±6.3

30 51.8 15.2 9.5 19.6 12.0 10.4 19.8±7.2

60 6.4 15.6 20.5 49.2 11.5 9.7 18.8±7.0

120 8.5 14.3 11.2 19.9 4.3 5.8 10.7±2.6

240 5.2 8.5 4.0 N.D. N.D. N.D. 3.0±1.6

480 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

720 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

1440 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

2880 N.D. N.D. N.D. N.D. N.D. N.D. 0.0±0.0

Table 46. Pharmacokinetic parameters of sesamol in serum after oral administration seven doses of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

T_max(min) 5 5 5 30 5 5 9.2±4.6

C_max(nmol/mL) 29.3 23.5 12.7 18.9 12.9 23.2 20.1±2.9

AUC_0-2880

(nmol．min/mL) 515.9 795.7 197.0 1224.3 269.8 237.0 540.0±180.7

MRT_0-2880(min) 18.8 42.6 14.5 40.8 13.5 8.6 23.1±6.6

Table 47. Pharmacokinetic parameters of sesamol sulfate in serum after oral administration seven doses of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

Tmax(min) 30 30 30 30 5 5 21.7±5.8

Cmax(nmol/mL) 461.4 291.5 469.7 716.0 376.8 247.6 427.2±74.7 AUC0-2880

(nmol．min/mL) 68299.2 61451.1 79596.6 96116.2 56577.8 33646.5 65947.9±9493.9

MRT0-2880(min) 329.0 318.5 285.2 184.0 427.9 402.3 324.5±39.0

Table 48. Pharmacokinetic parameters of sesamol glucuronide in serum after oral administration seven doses of sesamol in water (50 mg/kg) to six rats

Parameters 1 2 3 4 5 6 Mean±S.E.

T_max(min) 30 60 60 60 30 15 42.5±8.9

C_max(nmol/mL) 51.8 15.6 20.5 49.2 12.0 12.9 27.0±8.3

AUC_0-2880

(nmol．min/mL) 3045.9 3019.5 2663.2 3281.1 1081.0 1005.0 2349.3±461.2

MRT_0-2880(min) 74.3 109.6 91.7 66.4 52.2 56.2 75.1±9.8

Table 49. Comparison of pharmacokinetic parameters of sesamol, sesamol sulfates, and sesamol glucuronides after oral administration seven doses of sesamol in water (50 mg/kg) to six rats

Parameters T_max

(min)

C_max (nmol/mL)

AUC_0-2880

(nmol．min/mL) MRT0-2880(min)

sesamol 9.2±4.6^a 20.1±2.9^a 540.0±180.7^a 23.1±6.6^a

sesamol sulfate 21.7±5.8^{a b} 427.2±74.7 65947.9±9493.9 324.5±39.0 sesamol glucuronide 42.5±8.9^b 27.0±8.3^a 2349.3±461.2^a 75.1±9.8^a Data expressed as Mean±S.E. Means in a row without a common superscript differ P< 0.05

Table 50. Comparison of pharmacokinetic parameters of sesamol, sesamol sulfate and glucuronide after oral administration of single and seven doses of sesamol in water (50 mg/kg) to six rats

Parameters Single dose Seven doses

Sesamol

Tmax(min) 6.7±1.8 9.2±4.6

Cmax(nmol/mL) 185.4±60.2 20.1±2.9 *

AUC0-2880

(nmol．min/mL) 3160.3±1103.0 540.0±180.7 *

MRT0-2880(min) 15.2±1.4 23.1±6.6

Sesamol sulfate

Tmax(min) 20.8±4.8 21.7±5.8

Cmax(nmol/mL) 717.0±124.5 427.2±74.7

AUC0-2880

(nmol．min/mL)

69213.5±4918.6 65947.9±9493.9

MRT0-2880(min) 147.7±27.3 324.5±39.0 **

Sesamol glucuronide

Tmax(min) 23.3±4.8 42.5±8.9

Cmax(nmol/mL) 68.2±16.4 27.0±8.3 *

AUC0-2880

(nmol．min/mL)

5235.8±1776.2 2349.3±461.2

MRT0-2880(min) 66.8±6.6 75.1±9.8

Data expressed as Mean±S.E. *p<0.05 **p<0.01

Table 51. DPPH radical scavenging potential of blank serum and sesamol conjugates without SPE pretreatment.

1 2 3 Mean±S.D.

1 X 0.375 0.400 0.392 0.389±0.013

Blank serum

0.5 X 0.456 0.459 0.436 0.450±0.013

312 μM 0.258 0.226 0.227 0.237±0.018

A 156 μM 0.350 0.372 0.349 0.357±0.013

Data expressed as absorbance at 517 nm

A: Sesamol conjugates without solid-phase extraction pretreatment

Table 52. DPPH radical scavenging potential of blank serum and sesamol conjugates with SPE.

1 2 3 Mean±S.D.

1 X 0.400 0.416 0.411 0.409±0.008

Blank serum (SPE)

0.5 X 0.401 0.416 0.421 0.413±0.010

191 μM 0.293 0.318 0.312 0.308±0.013

B 96 μM 0.451 0.446 0.433 0.443±0.009

Data expressed as absorbance at 517 nm

B: Sesamol conjugates with solid-phase extraction pretreatment

Table 53. DPPH radicals scavenging potential of blank serum and sesamol conjugates without SPE.

1 2 3 Mean±S.D.

1 X 0.524 0.525 0.475 0.508±0.029

0.8 X 0.482 0.466 0.470 0.473±0.008

0.6 X 0.474 0.501 0.459 0.478±0.021

0.5 X 0.564 0.504 0.488 0.519±0.040

Blank serum

0.4 X 0.552 0.558 0.529 0.546±0.015

1 X (312 μM) 0.334 0.329 0.322 0.328±0.006 ***

0.8 X (250 μM) 0.353 0.353 0.339 0.348±0.008 ***

0.6 X (187 μM) 0.435 0.446 0.449 0.443±0.007 0.5 X (156 μM) 0.496 0.521 0.551 0.523±0.028 A

0.4 X (125 μM) 0.545 0.552 0.596 0.564±0.028 Data expressed as absorbance at 517 nm ***p<0.001

A: Sesamol metabolites without solid-phase extraction pretreatment

Table 54. DPPH radicals scavenging potential of blank serum and sesamol conjugates with SPE.

1 2 3 Mean±S.D.

1 X 0.630 0.648 0.626 0.635±0.012

0.8 X 0.655 0.637 0.644 0.645±0.009

0.6 X 0.627 0.631 0.669 0.642±0.023

0.5 X 0.668 0.634 0.674 0.659±0.022

Blank serum

0.4 X 0.648 0.614 0.673 0.645±0.030

1 X (191 μM) 0.415 0.434 0.451 0.433±0.018 ***

0.8 X (153 μM) 0.479 0.468 0.494 0.480±0.013 ***

0.6 X (115 μM) 0.557 0.650 0.596 0.601±0.047

0.5 X (96 μM) 0.594 0.622 0.629 0.615±0.019

0.4 X (76 μM) 0.651 0.640 0.680 0.657±0.021

Data expressed as absorbance at 517 nm ***p<0.001

B: Sesamol metabolites with solid-phase extraction pretreatment

Table 55. Comparison of the DPPH radical scavenging potential of PBS, sesamol and ascorbic acid.

Concentration (M) 1 2 3 Mean±S.D.

PBS 0.224 0.228 0.228 0.227±0.002

2.4 0.255 0.308 0.272 0.278±0.027

4.9 0.276 0.311 0.283 0.290±0.019

9.8 0.261 0.283 0.260 0.268±0.013

19.5 0.337 0.255 0.262 0.285±0.045

Ascorbic acid

39.0 0.226 0.244 0.241 0.237±0.010

2.4 0.227 0.239 0.218 0.228±0.011

4.9 0.209 0.246 0.218 0.224±0.019

9.8 0.196 0.223 0.204 0.208±0.014

19.5 0.141 0.148 0.153 0.147±0.006 ***

Sesamol

39.0 0.125 0.130 0.125 0.127±0.003 ***

Data expressed as Mean±S.D. of absorbance at 517 nm ***p<0.001

Table 56. Comparison of the DPPH radical scavenging potential of PBS, sesamol and ascorbic acid.

Concentration (M) 1 2 3 Mean±S.D.

PBS 0.224 0.228 0.228 0.227±0.002

40.0 0.174 0.332 0.186 0.231±0.088

80.0 0.195 0.208 0.214 0.206±0.010

160.0 0.221 0.251 0.251 0.241±0.017

240.0 0.287 0.295 0.297 0.293±0.005

320.0 0.262 0.286 0.297 0.282±0.018

Ascorbic acid

400.0 0.345 0.358 0.352 0.352±0.007

40.0 0.100 0.098 0.101 0.100±0.002 ***

80.0 0.088 0.088 0.090 0.089±0.001 ***

160.0 0.088 0.082 0.084 0.085±0.003 ***

240.0 0.072 0.074 0.078 0.075±0.003 ***

320.0 0.082 0.077 0.081 0.080±0.003 ***

Sesamol

400.0 0.083 0.084 0.092 0.086±0.005 ***

Data expressed as Mean±S.D. of absorbance at 517 nm ***p<0.001

Table 57. Inhibition of sesamol conjugates without SPE on AAPH-induced hemolysis of rat erythrocytes

concentration

Blank serum A

Time (h)

control 1X control 0.5X 312M 156M Without AAPH

0 0.105±0.013 0.128±0.043 0.122±0.009 0.108±0.002 0.109±0.002 1 0.091±0.002 0.065±0.003 0.161±0.032 ** 0.071±0.002 0.099±0.003 3 0.564±0.023 0.185±0.018 0.652±0.021 0.433±0.067 *** 0.099±0.005 5 0.793±0.068 0.427±0.045 0.829±0.084 0.673±0.020 ** 0.099±0.003 7 0.829±0.035 0.603±0.045 0.878±0.033 0.833±0.030 *** 0.102±0.001 9 0.695±0.047 0.739±0.095 0.747±0.062 0.653±0.199 0.106±0.002 Data expressed as absorbance at 540 nm **p<0.01 ***p<0.001

A: Sesamol conjugates without Solid-Phase extraction

Table 58. Inhibition of sesamol conjugates with SPE on AAPH-induced hemolysis of rat erythrocytes

concentration

Blank serum (SPE) B

Time (h)

control 1X control 0.5X 191M 96M Without AAPH 0 0.095±0.006 0.095±0.005 0.092±0.002 0.094±0.003 0.109±0.002 1 0.063±0.004 0.055±0.002 0.052±0.002 * 0.056±0.005 0.099±0.003 3 0.081±0.002 0.091±0.005 0.075±0.008 0.087±0.002 0.099±0.005 5 0.189±0.020 0.244±0.030 0.194±0.042 0.251±0.001 0.099±0.003 7 0.325±0.033 0.405±0.023 0.325±0.016 0.402±0.030 0.102±0.001 9 0.532±0.190 0.467±0.051 0.518±0.155 0.496±0.006 0.106±0.002 Data expressed as absorbance at 540 nm *p<0.05

B: Sesamol conjugates with Solid-Phase extraction

Table 59. Comparison the inhibition of PBS and sesamol on AAPH-induced hemolysis of rat erythrocytes concentration

Sesamol Time

(h)

PBS control 0.2M 1.0M 4.9M 24.4M 122.0M

0 0.061±0.001^a 0.073±0.002^b 0.072±0.001^b 0.071±0.001^b 0.071±0.003^b 0.072±0.005^b 1 0.048±0.005 0.050±0.001 0.051±0.001 0.051±0.000 0.051±0.003 0.054±0.001 3 0.106±0.006^a 0.084±0.001^b 0.079±0.001^b 0.063±0.003^b 0.050±0.001^b 0.052±0.001^b 5 0.321±0.006^a 0.226±0.003^b 0.198±0.009^b 0.134±0.005^b 0.052±0.001^b 0.050±0.002^b 7 0.543±0.023^a 0.349±0.006^b 0.325±0.010^b 0.239±0.023^b 0.053±0.001^b 0.053±0.001^b 9 0.683±0.063^a 0.393±0.013^b 0.340±0.037^b 0.302±0.015^b 0.064±0.004^b 0.058±0.003^b Data expressed as absorbance at 540 nm

Data expressed as Mean±S.E. Means in a row without a common superscript differ P< 0.05

Table 60. Comparison the inhibition of PBS and ascorbic acid on AAPH-induced hemolysis of rat erythrocytes

concentration Vitamin C Time

(h)

PBS control 0.2M 1.0M 4.9M 24.4M 122.0M

0 0.061±0.001^a 0.069±0.003 0.071±0.001^b 0.072±0.001^b 0.072±0.001^b 0.073±0.001^b 1 0.048±0.005^a 0.060±0.001^b 0.065±0.004^b 0.054±0.001 0.055±0.004 0.061±0.001^b 3 0.106±0.006^a 0.077±0.013^b 0.083±0.006^b 0.084±0.003^b 0.065±0.002^b 0.052±0.002^b 5 0.321±0.006^a 0.215±0.006^b 0.221±0.013^b 0.210±0.009^b 0.166±0.013^b 0.072±0.003^b 7 0.543±0.023^a 0.344±0.008^b 0.341±0.008^b 0.340±0.003^b 0.292±0.007^b 0.133±0.015^b 9 0.683±0.063^a 0.401±0.023^b 0.404±0.002^b 0.406±0.009^b 0.353±0.005^b 0.205±0.010^b Data expressed as absorbance at 540 nm

Data expressed as Mean±S.E. Means in a row without a common superscript differ P< 0.05

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在文檔中芝麻酚類成分之代謝動力學及清除自由基活性評估; Metabolic Pharmacokinetics of Sesame Phenols and Evaluation of Free Radical-scavenging Effect (頁 85-150)