Objective: To establish an HPLC method for detecting the contents of seven compounds in total flavonoids from Scutellariae Barbatae Herba

and further study the antitumor activity of total flavonoids and seven compounds from Scutellariae Barbatae Herba. Method: The contents of scutellarin

apigenin-5-O-β-D-glucopyranoside

suctellarein

isoscutellarein 8-glucuronide

luteolin

4'-hydroxywogonin

and apigenin were detected by HPLC. The antitumor activity of total flavonoids and the seven compounds were assayed in human hepatocellular carcinoma cells (Hep3B)

human gastric cancer cells (AGS)

human lung cancer cells (A549)

mouse melanoma cells (B16) and mouse breast cancer cells (4T1) by using MTT assat. Result: The HPLC method was established to detect the contents of above seven compounds. The linear range was 9.98-249.60

1.06-26.50

2.16-54.00

2.56-64.05

1.16-29.10

0.52-13.00 and 1.18-29.50 mg·L-1 respectively for the above 7 components

with an average recovery rate of 103.47%

96.15%

98.66%

98.91%

98.25%

102.67% and 102.32% respectively

and RSD of 2.1%

1.1%

1.7%

3.2%

2.1%

1.8%

and 1.9%. The total flavonoids (300 mg·L-1) showed obvious inhibitory effect on the proliferation of Hep3B

AGS

A549 and B16 cells (the inhibitory rate was >50% for the 4 kinds of cells). Luteolin and 4'-hydroxywogonin showed significant anti-tumor activity (IC50 26.64-36.97 mmol·L-1 and 20.14-36.97 mmol·L-1

respectively). Conclusion: The method is simple

rapid

accurate and is suitable for the determination of effective compounds in total flavonoids from Scutellariae Barbatae Herba. The total flavonoids have certain inhibitory effect

while luteolin and 4'-hydroxywogonin have significant inhibitory effect on the proliferation of Hep3B

AGSA549

B16 and 4T1 cells. All these results indicated that the total flavonoids are the main active fraction in Scutellariae Barbatae Herba for anti-tumor effect

and luteolin and 4'-hydroxywogonin are the main active ingredient.