Byakangelicin

CN 103109822 A[P]. 2013.

Application of byakangelicin used as agricultural insect antifeedant and pesticide.[Reference: WebLink]

The invention discloses an application of Byakangelicin used as an agricultural pesticide and an insect antifeedant. The Byakangelicin has an obvious effect of preventing and controlling lepidopterous insects and homoptera when being used as the pesticide and the insect antifeedant, and also has the characteristics of low toxicity without any residues or pollutions when being used as the agricultural pesticide, so that environmental protection is favored.

Phytomedicine. 1998 Apr;5(2):121-7.

Effect of byakangelicin, an aldose reductase inhibitor, on galactosemic cataracts, the polyol contents and Na(+), K(+)ATPase activity in sciatic nerves of strepto-zotocin-induced diabetic rats.[Pubmed: 23195764]

Byakangelicin, a main furanocoumarin constituent isolated and characterized as an aldose reductase inhibitor from the roots of Angelica dahurica, was evaluated for usefulness in the treatment of galactosemic cataract and diabetic complications in animal experiments.
METHODS AND RESULTS:
Cataract formation and galactitol accumulation in the lenses of rats fed a 30% galactose diet were significantly prevented by intragastric (i.g.) administration of Byakangelicin at a dose of 100 mg/kg for 14 days. Administration of the drug for 18 days was found to suppress sorbitol accumulation and cause a significant reversal of depleted myo-inositol contents as well as Na(+),K(+)ATPase activity in the sciatic nerves of streptozotocin-induced diabetic rats.
CONCLUSIONS:
These results indicate that in rats, Byakangelicin is effective for the treatment of sugar cataracts and diabetic neuropathy and hence might be useful as a lead compound for the development of new type drugs for clinical use.

Br J Pharmacol. 2011 Jan;162(2):441-51.

Byakangelicin induces cytochrome P450 3A4 expression via transactivation of pregnane X receptors in human hepatocytes.[Pubmed: 20942813]

Byakangelicin is found in extracts of the root of Angelica dahurica, used in Korea and China as a traditional medicine to treat colds, headache and toothache. As Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones. Therefore, this study investigated the effects of Byakangelicin on the cytochrome P450 isoform cytochrome (CY) P3A4 in human hepatocytes.
METHODS AND RESULTS:
Cultures of human hepatocytes and a hepatoma cell line (Huh7 cells) were used. mRNA and protein levels were measured by quantitative reverse transcription-polymerase chain reaction and Western blot. Plasmid constructs and mutants were prepared by cloning and site-directed mutagenesis. Reporter (luciferase) activity was determined by transient co-transfection experiments. In human primary hepatocytes, Byakangelicin markedly induced the expression of CYP3A4 both at the mRNA level (approximately fivefold) and the protein level (approximately threefold) but did not affect expression of human pregnane X receptor (hPXR). In reporter assays, Byakangelicin activated CYP3A4 promoter in a concentration-dependent manner (EC₅₀ = 5 μM), and this activation was enhanced by co-transfection with hPXR. Further reporter assays demonstrated that the eNR4 binding element in the CYP3A4 promoter was required for the transcriptional activation of CYP3A4 by Byakangelicin.
CONCLUSIONS:
Byakangelicin induced expression and activity of CYP3A4 in human hepatocytes. This induction was achieved by the transactivation of PXR and not by increased expression of PXR. Therefore, Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions.

Indian J. Exp. Biology, 1967, 5(2):75-9.

Endocrinological studies on plant products: part 5. Effect of byakangelicin on female sex hormones and on fertility of rats.[Reference: WebLink]

The effect of Byakangelicin on female sex hormones and on fertility of rats and rabbits was investigated. Intact and castrate albino rats received sc injections of 1-3 mg/day/rat for 6 days 3 days alone and 3 days with 5 IU estradiol. Immature rabbits received im injections of 50 IU of estrogen for 3 days followed by 3-6 mg of Byakangelicin/day along with the same amount of hormone for 3 more days. The animals were sacrificed 24 hours after the last injection. Changes in gross uterine weight histological and histochemical examinations of tissues and vaginal smear test indicated that Byakangelicin partially blocked the uterotropic respones of exogenous estrogen. No effect on the progesterone response of the uterus was seen. Byakangelicin caused irregularity of estrous cycle delay in mating and a marked decrease in fertile mating and in number of offspring. It appeared that Byakangelicin might delay the sexual maturity of rats.

Arch Pharm Res. 2003 Aug;26(8):606-11.

Identification of new urinary metabolites of byakangelicin, a component of Angelicae dahuricae Radix, in rats.[Pubmed: 12967195]

Byakangelicin, 9-(2,3-dihydroxy-2-methylbutoxy)-4-methoxy-7H-furo[3,2-g][l]benzopyran-7-one (BKG), a component of Angelicae dahuricae Radix, is considered to be an inhibitor of aldose reductase for the treatment of diabetic cataract.
METHODS AND RESULTS:
An analytical method for the isolation of BKG developed by high-performance liquid chromatography has been reported. No literature on the metabolism of BKG, however, has been found. With the purpose of identifying new metabolites of BKG, BKG (100 mg/kg) was orally administered to Sprague-Dawley rats via a gavage. Using a metabolic cage, urine was collected for 24 h, and the urine samples were extracted by liquid-liquid extraction. For structural identification of new urinary metabolites of BKG, various instrumental analyses were conducted by gas-chromatography/mass spectrometry, high-performance liquid chromatography/diode array detector, liquid chromatography/mass spectroscopy with thermospray interface and 1H nuclear magnetic resonance spectroscopy. Two metabolites produced from the O-demethylation or O-dealkylation of BKG were newly identified, and another new but unknown metabolite was assumed to be the hydroxylated form of BKG.
CONCLUSIONS:
These results indicate that the major metabolic products of BKG are formed by O-demethylation or O-dealkylation of BKG side chains.