Epimedin B

Acta Physiol Plant, 2013, 35(11):3271-5.

Light stress suppresses the accumulation of epimedins A, B, C, and icariin in Epimedium, a traditional medicinal plant.[Reference: WebLink]

Epimedium is well-known in China and East Asia due to high content of flavonoid derivatives, including icariin, epimedin A, Epimedin B, and epimedin C, hereafter designated as bioactive components, which have been extensively utilized to cure many diseases. So far, the molecular mechanism of the bioactive components biosynthesis remains unclear.
METHODS AND RESULTS:
In the present study, the effect of light stress (24 h illumination) on the accumulation of bioactive components and the expression of flavonoid genes in Epimedium was investigated. Under light stress, the structural genes CHS1, CHI1, F3H, FLS, DFR1, DFR2, and ANS were remarkably up-regulated while CHS2 and F3′H were significantly down-regulated. For transcription factors, the expression of Epimedium MYB7 and TT8 were increased while Epimedium GL3, MYBF, and TTG1 expression were depressed. Additionally, the content of bioactive components was significantly decreased under light stress.
CONCLUSIONS:
Our results suggested that the decrease of bioactive compounds may be attributed to transcripts of late genes (DFRs and ANS) increased to a higher level than that of early genes (FLS and CHS1).

Drug Metab Dispos . 2015 Aug;43(8):1181-9.

Ginsenosides Regulate PXR/NF-κB Signaling and Attenuate Dextran Sulfate Sodium-Induced Colitis[Pubmed: 25986850]

Abstract Pregnane X receptor (PXR) activation exhibits anti-inflammatory effects via repressing nuclear factor-κB (NF-κB); however, its overactivation may disrupt homeostasis of various enzymes and transporters. Here we found that ginsenosides restore PXR/NF-κB signaling in inflamed conditions without disrupting PXR function in normal conditions. The effects and mechanisms of ginsenosides in regulating PXR/NF-κB signals were determined both in vitro and in vivo. Ginsenosides significantly inhibited NF-κB activation and restored the expression of PXR target genes in tumor necrosis factor-α-stimulated LS174T cells. Despite not being PXR agonists, ginsenosides repressed NF-κB activation in a PXR-dependent manner. Ginsenosides significantly increased the physical association between PXR and the NF-κB p65 subunit and thereby decreased the nuclear translocation of p65. Ginsenoside Rb1 and compound K (CK) were major bioactive compounds in the regulating PXR/NF-κB signaling. Consistently, ginsenosides significantly attenuated dextran sulfate sodium-induced experimental colitis, which was associated with restored PXR/NF-κB signaling. This study indicates that ginsenosides may elicit anti-inflammatory effects via targeting PXR/NF-κB interaction without disrupting PXR function in healthy conditions. Ginsenoside Rb1 and CK may serve as leading compounds in the discovery of new drugs that target PXR/NF-κB interaction in therapy for inflammatory bowel disease. Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics.

Oxid Med Cell Longev . 2015;2015:843721.

Ginsenoside Rb1 Treatment Attenuates Pulmonary Inflammatory Cytokine Release and Tissue Injury following Intestinal Ischemia Reperfusion Injury in Mice[Pubmed: 26161243]

Abstract Objective. Intestinal ischemia reperfusion (II/R) injury plays a critical role in remote organ dysfunction, such as lung injury, which is associated with nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) signaling pathway. In the present study, we tested whether ginsenoside Rb1 attenuated II/R induced lung injury by Nrf2/HO-1 pathway. Methods. II/R injury was induced in male C57BL/6J mice by 45 min of superior mesenteric artery (SMA) occlusion followed by 2 hours of reperfusion. Ginsenoside Rb1 was administrated prior to reperfusion with or without ATRA (all-transretinoic acid, the inhibitor of Nrf2/ARE signaling pathway) administration before II/R. Results. II/R induced lung histological injury, which is accompanied with increased levels of malondialdehyde (MDA), interleukin- (IL-) 6, and tumor necrosis factor- (TNF-) α but decreased levels of superoxide dismutase (SOD) and IL-10 in the lung tissues. Ginsenoside Rb1 reduced lung histological injury and the levels of TNF-α and MDA, as well as wet/dry weight ratio. Interestingly, the increased Nrf2 and HO-1 expression induced by II/R in the lung tissues was promoted by ginsenoside Rb1 treatment. All these changes could be inhibited or prevented by ATRA. Conclusion. Ginsenoside Rb1 is capable of ameliorating II/R induced lung injuries by activating Nrf2/HO-1 pathway.

National Symposium on Chinese medicine and natural medicine. 2014.

Study on Different Factors Affecting the Bionic Enzymatic Hydrolysis of Icariin,Epimedin A,Epimendin B,Epimendin C and Eplmedium Flavonolds.[Reference: WebLink]

Flavonoids were the main active ingredient in Epimedium and mainly included icariin,epimedin A,epimendin B,epimendin C and baohuoside.Modern pharmacological studies have shown that Epimedium flavone had clear anti-osteoporosis effect. In order to obtain an improved absorption,transformation to secondary glycosides by intestinal enzymes and intestinal bacteria is necessary after the oral administration[1].However,intestinal enzymes and intestinal bacteria were unstable and could be affected by race,age,diet and medication[2].To screen effective and safe hydrolase in vitro and add it to epimedium flavone preparation could promote oral absorption of epimedium flavonoids,increase its bioavailability and improve its efficacy.
METHODS AND RESULTS:
This study aims to screen effective and safe hydrolase,investgate different factors which affect the bionic enzymatic hydrolysis of epimedium flavonoids and optimize the reaction conditions for building a novel bionic enzymolysis drug delivery system.To simulate the environment in vivo,37 °C was set as the temperature and artificial intestinal juice and gastric juice was selected as the buffer solutions.Taking the conversion of epimedium flavonoids as index,the effects of the kinds of enzyme,the ratio of enzyme and substrate,substrate concentration,reaction time,pancreatin were investigated.
CONCLUSIONS:
The results show the conversion of epimedium flavonoids was highest and their enzymolysis products was accordant with the intestinal metabolites by using snailase in artificial intestinal juice.Moreover,the main flavonoids could be completely transformed into the secondary glycoside or aglycone during 2~6 h.

Nat Prod Res. 2015;29(2):185-8.

Simultaneous enrichment and separation of flavonoids from Herba Epimedii by macroporous resins coupled with preparative chromatographic method.[Pubmed: 25277166]

METHODS AND RESULTS:
An efficient, feasible enrichment and separation method of epimedin A,Epimedin B,epimedin C and icariin from Herba Epimedii was developed by the combination of microwave-assisted extraction, macroporous resins and preparative HPLC. WDX-5 macroporous resin shows better recoveries at 96.2%, 97.0%, 98.2% and 97.1% for epimedins A, B, C and icariin than other macroporous resins used in the experiments. As a result, epimedins A (5.1 mg),Epimedin B (15.3 mg),epimedin C (7.6 mg) and icariin (14.3 mg) were obtained from 6.0 g crude Herba Epimedii with the recoveries at 70.8%, 68.9%, 66.7% and 95.3%, respectively.
CONCLUSIONS:
The method developed in this study may provide scientific references for the enrichment and separation of flavonoids from Herba Epimedii.