Planta Med 2004; 70(12): 1161-1165
DOI: 10.1055/s-2004-835845
Original Paper
Biochemistry and Molecular Biology
© Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetic and Metabolic Studies of Retrojusticidin B, a Potential Anti-Viral Lignan, in Rats

Chen-Yu Wang1 , Shao-Wen Sun1 , Shoei-Sheng Lee1
  • 1School of Pharmacy, College of Medicine, National Taiwan University, Taipei, Taiwan 100, Republic of China
Further Information

Publication History

Received: February 23, 2004

Accepted: June 26, 2004

Publication Date:
10 January 2005 (online)

Abstract

The pharmacokinetics and metabolism of retrojusticidin B, an anti-HIV reverse transcriptase agent isolated from Phyllanthus myritifolius, were studied in rats. The phase II conjugated metabolites were characterized after solvolysis and enzymatic hydrolysis. The oral bioavailabilities of retrojusticidin B, suspended in Tween 80 and in corn oil, were found to be 22.1 % and 33.1 %, respectively. The elimination half-lives (T1/2) were 22.9 and 36.2 minutes, respectively. The T1/2, clearance, and the volume of distribution (Vz) of retrojusticidin B estimated from i. v. measurements were 24.5 min, 2.6 ± 0.4 L/min, and 90.6 ± 6.4 L, respectively. 9,9′-Secoretrojusticidin B was shown to be phase I metabolite.

Abbreviations

AUC:area under the plasma level-time curve

Vz:apparent volume of distribution of the central compartment

Cl:clearance

Cmax:maximum peak concentration

Tmax:the time to achieve Cmax

References

  • 1 Unander D W, Webster G L, Blumberg B S. Usage and bioassays in Phyllanthus (Euphorbiaceae) IV.  Clustering of antiviral uses and other effects, J Ethnopharmacol. 1995;  45 1-18
  • 2 Lin M T, Lee S S, Liu K CSC. Phyllamyricins A - C, three novel lignans from Phyllanthus myrtifolius .  J Nat Prod. 1995;  58 244-9
  • 3 Lee S S, Lin M T, Liu C L, Lin Y Y, Liu K CSC. Six lignans from Phyllanthus myrtifolius .  J Nat Prod. 1996;  59 1061-5
  • 4 Chang C W, Lin M T, Lee S S, Karin C SCL, Hsu F L, Lin J Y. Differential inhibition of reverse transcriptase and cellular DNA polymerase-α activities by lignans isolated from Chinese herbs, Phyllanthus myrtifolius Moon, and tannins from Lonicera japonica Thunb and Castanopsis hystrix .  Antiviral Res. 1995;  27 367-74
  • 5 Bhuchar V M, Agarwal A K. Evaluation of color changes of sulfamphthalein indicators: synthesis, purification, and characterization of phenol- and o-cresolsufamphthalein.  Indian J Chem Sect A. 1984;  23 262-4
  • 6 Sauter A, Hartung W. Radial transport of abscisic acid conjugates in maize roots: its implication for long distance stress signals.  J Exp Bot. 2000;  51 929-35
  • 7 Kostova I, Dinchev D, Rentsch G H, Dimitrov V, Ivanova A. Two new sulfated furostanol saponins from Tribulus terrestris. Z.  Naturforsch. 2002;  57c 33-8
  • 8 Sreekumar O, Hosono A. Immediate effect of Lactobacillus acidophilus on the intestinal flora and fecal enzymes of rats and the in vitro inhibition of Escherichia coli in coculture.  J Dairy Sci. 2000;  83 931-9
  • 9 Prueksaritanont T, Subramanian R, Fang X, Ma B, Qiu Y, Lin J H, Pearson P G, Baillie T A. Glucuronidation of statins in animals and humans: A novel mechanism of statin lactonization.  Drug Metab Dispos. 2002;  30 505-12

Dr. Shoei-Sheng Lee

School of Pharmacy

College of Medicine

National Taiwan University

Taipei 100

Taiwan

R.O.C.

Phone: +886-2-2312-3456 ext. 8405

Fax: +886-2-2321-1127

Email: shoeilee@ha.mc.ntu.edu.tw

    >