An iridoid glycoside with diverse biological activities
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Genipin 1-gentiobioside is an iridoid glycoside that has been found in G. jasminoides and has diverse biological activities.1,2,3 It inhibits acetylcholinesterase (AChE) by 60.23% when used at a concentration of 25 ?g/ml.1 Genipin 1-gentiobioside (50-500 ?g/ml) is cytotoxic to BRL 3A rat liver fibroblasts.2 It inhibits the germination of G. jasminoides and N. offinicale seeds and the growth of B. rapa roots.3 Genipin 1-gentiobioside (2.5 mg/kg) prevents scopolamine-induced increases in escape latency in the Morris water maze in mice.1
1.Kwak, J.H., and Lee, D.-U.Structure–antiamnesic activity relationship of iridoid glycosides from gardenia fruitsChem. Lett.44(6)837-839(2017) 2.Li, C., Lan, M., Lv, J., et al.Screening of the hepatotoxic components in Fructus Gardeniae and their effects on rat liver BRL-3A cellsMolecules24(21)3920(2019) 3.Shimomura, H., Sashida, Y., Nakata, H., et al.Germination and growth inhibitors in fruits of Gardenia jasminoidesPlant Cell Physiol.24(1)123-126(1983)
Animal experiment: | Rats[1]Twelve male rats are divided randomly into normal and acute cholestatic liver injury (CLI) group, with 6 rats in each. The rats are kept in an air-conditioned environment at a temperature of 22-24°C and a relative humidity of 50±10%, with access to the standard laboratory food and water. After fasted for 12 h, the rats are given Zhi-Zi-Da-Huang decoction (ZZDHD) at a dose of 8 g/kg (crude drug/body weight, equivalent to 35.9 mg/kg geniposide, 11.4 mg/kg Genipin 1-β-D-gentiobioside, 2.50 mg/kg Rhein, 0.23 mg/kg Emodin, 11.2 mg/kg Isonaringin, 83.5 mg/kg Naringin, 12.4 mg/kg Hesperidin and 79.6 mg/kg Neohesperidin) by oral administration. Blood samples (approximately 0.3 mL) are collected from the fosse orbital vein using heparinized 1.5 mL polythene tubes before the dose and at 0.08, 0.17, 0.33, 0.67, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 h after dosing, and then centrifuged immediately at 13,000 rpm for 5 min. Plasma is transferred into clean tubes and stored at -80°C until analysis[1]. |
参考文献: [1]. Zhu H, et al. Simultaneous determination of two iridoid glycosides, two anthraquinones and four flavonoid glycosides of Zhi-Zi-Da-Huang decoction in rat plasma by UFLC-MS/MS: application to a comparative pharmacokinetic study in normal and cholestatic liver injury rats. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Jun 1;960:116-25. |
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