Quantitative LC/MS/MS method and pharmacokinetic studies of columbin, an anti-inflammation furanoditerpen isolated from Radix Tinosporae.
Columbin is an important component isolated from Radix Tinosporae. It has been demonstrated to possess many pharmacological activities, including anti-inflammation, antitumor and inhibition of enzyme activity in vivo. The purpose of the present study was to examine in vivo pharmacokinetics and bioavailability of columbin in rats using a high-performance liquid chromatography coupled with tandem mass spectrometry quantitative detection method. The columbin was extracted from rat plasma samples by methyl tert-butyl ether, evaporated and reconstituted in 100 microL methanol prior to analysis. The separation was performed using a Luna reversed-phase analytical column (5 microm, 100 x 2.0 mm) and an SB-C18 guard column (5 microm, 20 x 4.0 mm). The mobile phase was a mixture of methanol and water containing 25 mmoL/L NH(4)Ac (80:20, v/v). The method was validated within the concentration range of 5-5000 ng/mL, and the calibration curves were linear with correlation coefficients (r) >0.999. It was further applied to assess pharmacokinetics and oral bioavailability of columbin after i.v. and oral administration to rats. The oral bioavailability of columbin was only 3.18%, which indicated that columbin had poor absorption or underwent extensive first-pass metabolism.
Shi
Qirong
Q
Department of Natural Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, People's Republic of China.
Liang
Mingjin
M
Zhang
Weidong
W
Zhang
Chuan
C
Liu
Runhui
R
Shen
Yunheng
Y
Li
Huiliang
H
Wang
Xiaolin
X
Wang
Xiangwei
X
Pan
Qiongqun
Q
Chen
Chunlin
C
D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004224:Diterpenes / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D007783:Lactones / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000378:metabolism; D018517:Plant Roots / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods; D013056:Spectrophotometry, Ultraviolet / Q000379:methods; D053719:Tandem Mass Spectrometry / Q000379:methods*; D031610:Tinospora / Q000737:chemistry* / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D004224:Diterpenes; D007783:Lactones; D010936:Plant Extracts; C062514:columbin