1.Effective components and signaling pathways of Epimedium brevicornumbased on network pharmacology.
Run-Tong ZHANG ; Hai-Ning WU ; Gui-Hong YU ; Yuan-Li ZHOU ; Xiao-Bin JIA ; Liang FENG
China Journal of Chinese Materia Medica 2018;43(23):4709-4717
The aim of this paper was to find out the active components of Epimedium brevicornum using network pharmacology, and find the potential targets and mechanisms. The TCMSP database was used to screen the active ingredients, and TTD and DrugBank databases were used to predict the potential targets with the literature mining. The pathway annotation was used to enrich and analyze the active ingredients and potential targets of E. brevicornum. The results showed that E. brevicornum had34 potential target active ingredients, including 21 flavones components, such as icariin, epimedin A, epimedin B, epimedin C, Yinyanghuo A, Yinyanghuo C and so on, 2 lignans involved in (+)-cycloolivil and olivil, 3 sterols consisting of sitosterol, 24-epicampesterol and poriferast-5-en-3beta-ol. The main predicted targets included Ptgs2, NCOA6, RANK, OPG, WNT9B, PTH1R, BMPs, SMAD4A and so on. There were 88 signaling pathways involved in 10 signaling pathways which was related to inflammation, such as NF-kappa B signaling pathway, T cell receptor signaling pathway, IL-17 signaling pathway and 10 pathways which was related to cancer included breast cancer, bladder cancer, pancreatic cancer and so on, and estrogen related signaling pathways included estrogen signaling pathway. This laid the foundation for the discovery of the active components of Epimedium and the study on its mechanism of action.
Epimedium
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classification
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metabolism
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Estrogens
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Flavonoids
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Signal Transduction
2.Variation of icariin and total flavonoid of Epimedium acuminatum in different parts and habitats.
Tao ZHOU ; Xiaobo ZHANG ; Lanping GUO ; Ge LIN ; Weike JIANG ; Qiang AI ; Chenggang ZHANG
China Journal of Chinese Materia Medica 2012;37(13):1917-1921
OBJECTIVEThrough comparative study on contents of icariin and total flavonoid of Epimedium acuminatum in different habitats and parts, the distribution and correlation of the two components were observed.
METHODTwenty-four sample spots in four habitats were set up, and the whole plant of these samples was divided as following: leaf, root, stem and rhizome. Total flavonoid and icariin of samples were determined by using the UV method and the HPLC, respectively. The data was analyzed by SPSS 17.0.
RESULTThe distribution of icariin in different parts had the pattern: leaf > root > stem > rhizome, the total flavonoid content was higher in leaf, but it showed no difference in other parts. Habitat had certain effect on icariin accumulation in E. acuminatum. The significant differences of total flavonoid content in E. acuminatum from different parts were not observed.
CONCLUSIONThe distribution of icariin from different parts and habitats has high selectivity. Metabolism and accumulation of flavonoid content in each part have no difference. Flavonoid content is less affected by environment. Considering the distribution of icariin and flavonoid content in every part and the growth strategy in different habitats comprehensively, it is reasonable to harvest the aerial part for the sustainable utilization of E. acuminatum.
Drugs, Chinese Herbal ; chemistry ; metabolism ; Ecosystem ; Epimedium ; chemistry ; metabolism ; Flavonoids ; analysis ; metabolism ; Plant Structures ; chemistry ; metabolism
3.Research on growth state and physiological changes of Epimedium wushanense under different shade conditions.
Hui WANG ; Yunxiang LI ; Qiumei QUAN ; Gang ZHAO ; Yayun TONG ; Yong NIE
China Journal of Chinese Materia Medica 2010;35(20):2669-2673
OBJECTIVETo study the growth state and physiological changes of Epimedium wushanense under different light conditions (100%, 80%, 60%, 40%, 20%), and investigate its adaptation mechanism to shade environment so that it can provide theoretical basis for cultivation and production.
METHODThe growth index, the content of photosynthetic pigments, proline content, MDA content, soluble sugar content, soluble protein content and antioxidant enzymy activity of E. wushanense under different shade conditions were measured.
RESULTExcept for length/width, the other form index of E. wushanense changed significantly. The E. wushanense grew well between light intensity 80%-40%, besides, the biomass above the earth was relatively high. The chlorophyll a, chlorophyll b, total chlorophyll content and carotenoids cotent were enhanced after shaded, the values of chlorophyll a\chlorophyll b increased between light intensity 100% -60% and reduced between light intensity 60% -20%. The proline and MDA content decreased after shading, the soluble sugar and soluble protein content increased respectively between light intensity 100% -60%, 100% -40% and reduced respectively between light intensity 60% -20%, 40% -20%. The SOD activity, CAT activity decreased after shading, and the POD activity, APX activity reduced between light intensity 60% -40%, raised under 20% treatment.
CONCLUSION80% 40% irradiance treatment was favorable to the growth of E. wushanense.
Catalase ; metabolism ; Epimedium ; chemistry ; physiology ; Light ; Peroxidase ; metabolism ; Superoxide Dismutase ; metabolism
4.Analysis on biotransformation of Epimedium brevicornu flavonoids.
Xia GAO ; Xuan LIU ; Yan CHEN ; Ying WANG ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2013;38(23):4079-4083
This study aims to investigate the biotransformation of Epimedium brevicornu flavonoids under the effect of hydrolytic enzymes in vitro. Snailase was mainly used to hydrolyze E. brevicornu flavonoids, and HPLC was used to determine the content of the main flavonoids in E. brevicornu flavonoids. The data results showed that the main known flavonoids included icariin, epimedin A, epi-mendin B and epimendin C, which were completely transformed into baohuoside I, sagittatoside A, sagittatoside B and 2"-O-rhamnosyl-icariside II in 1-2 h, respectively. Their transformed products were continuously hydrolyzed over time. In conclusion, snailase could transform E. brevicornu flavonoids into secondary glycoside or aglycone under 37 degrees C in pH 6.0 HBSS balanced salt solution in 2 h. Moreover, its enzymatic hydrolysates were consistent with intestinal metabolites.
Biotransformation
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Epimedium
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chemistry
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Flavonoids
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metabolism
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Hydrogen-Ion Concentration
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Hydrolases
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metabolism
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Hydrolysis
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Temperature
5.Morphological character of growth cycle for Epimedium acuminatim and icariin content analysis.
Tao ZHOU ; Hou-Xi XIONG ; Ge LIN ; Wei-Ke JIANG ; Lan-Ping GUO ; Min LEI ; Chuan-Yi CHEN ; Xiao-Bo ZHANG
China Journal of Chinese Materia Medica 2014;39(1):48-51
OBJECTIVETo study the relationship between morphological characteristics of growth cycle for Epimedium acuminatium and accumulation level of secondary metabolites.
METHODAfter making habitat clear, methods of morphology observation, specimen preparation, organism charting were applied to record morphological characteristics of E. acuminatium at different stages. HPLC was employed to detect icariin content of different parts of the plant at the stage of vegetative growth and sexual reproduction.
RESULTThe growth cycle of E. acuminatium was divided into vegetative growth stage and sexual and asexual reproduction coexistence stage. Seven to eight years were needed for the plants flowering and seeding of E. acuminatimcan in open land of forest edge, but within good nutrition conditions, growth cycle is shortened into three to four years. The difference of icariin content in two growth stages was not significant.
CONCLUSIONMorphological change of lower and foliar organ can be utilized to estimate growth age. But after applying sexual propagation for both root and stem of grown plants, it's been difficult to determine their growth year. If individual biomass or yield is economical, plants can be harvested in both vegetative growth and sexual reproduction stages.
Biomass ; Chromatography, High Pressure Liquid ; methods ; Epimedium ; growth & development ; metabolism ; Flavonoids ; metabolism ; Plant Roots ; growth & development ; metabolism ; Reproduction ; Seedlings ; metabolism
6.New prenylated flavonoid glycosides derived from Epimedium wushanense by β-glucosidase hydrolysis and their testosterone production-promoting effects.
Xin-Guang SUN ; Xu PANG ; Hai-Zhen LIANG ; Jie ZHANG ; Bei WANG ; Qi LI ; Jie WANG ; Xiao-Juan CHEN ; Bao-Lin GUO ; Bai-Ping MA
Chinese Journal of Natural Medicines (English Ed.) 2022;20(9):712-720
Six new prenylated flavonoid glycosides, including four new furan-flavonoid glycosides wushepimedoside A-D (1-4) and two new prenyl flavonoid derivatives wushepimedoside E-F (5-6), and one know analog epimedkoreside B (7) were isolated from biotransformation products of the aerial parts of Epimedium wushanense. Their structures were elucidated according to comprehensive analysis of HR-MS and NMR spectroscopic data, and the absolute configurations were assigned using experimental and calculated electronic circular dichroism (ECD) data. The regulatory activity of compounds 1-7 on the production of testosterone in primary rat Leydig cells were investigated, and 4 and 5 exhibited testosterone production-promoting activities. Molecular docking analysis suggested that bioactive compounds 4 and 5 showed the stable binding with 3β-HSD and 4 also had good affinity with Cyp17A1, which suggested that these compounds may regulate testosterone production through stimulating the expression of the above two key proteins.
Animals
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Epimedium/chemistry*
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Flavonoids/chemistry*
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Furans
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Glycosides/chemistry*
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Hydrolysis
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Male
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Molecular Docking Simulation
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Molecular Structure
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Rats
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Testosterone
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beta-Glucosidase/metabolism*
7.Distribution and influencing factors of magnoflorine in Epimedium.
Min GAO ; Changzhen FU ; Jingjing LIU ; Baolin GUO ; Xiangbo YANG ; Debin CHEN ; Li LI
China Journal of Chinese Materia Medica 2011;36(18):2475-2478
Eighty samples of Epimedium from 29 species and were determined in this study. The content of magnoflorine in leaves range between 0. 003% and 2. 603%. The results showed that the content of magnoflorine was quite stable within species except E. wushanense, E. acuminatum, E. hunanense. Genetic factors might be the main influencing ones. The contents of different parts and different collecting time of the medicinal materials were variable.
Aporphines
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chemistry
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metabolism
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Breeding
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Drugs, Chinese Herbal
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chemistry
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metabolism
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Environment
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Epimedium
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chemistry
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classification
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metabolism
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Plant Leaves
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chemistry
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metabolism
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Species Specificity
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Tissue Distribution
8.Protective effect of total flavonoids of epimedium on the kidney in experimental diabetic rats.
Hong QIAN ; Jun-Jie YANG ; Ding-Yi PAN ; Wen-Tao TANG ; Ke-Jia XU ; Min-You QI
Chinese Journal of Applied Physiology 2014;30(4):314-317
OBJECTIVETo investigate the influence of total flavonoids of epimedium (TFE) on the streptozocin (STZ)-induced kidney injury in diabetic rats and discuss the possible mechanism.
METHODSDiabetes was produced by a single injection of streptozocin (40 mg/kg, iv) in male SD rats. The rats were randomly divided into three groups (n = 10): control group, model group and TFE group (100 mg/kg, ig). Animals were sacrificed 12 weeks later. The level of blood glucose, blood urea nitrogen (BUN) and creatinine (Cr) as well as the renal index were determined. Detect the specific biochemical of renal tissue: superoxide dismutase (SOD), malondialdehyde (MDA). Use masson staining to observe the morphology of the renal tissue. Immunohistochemistry was employed to determine the protein levels of transforming growth factor-beta1 (TGF-beta1).
RESULTSCompared to control group, the enhancement of blood glucose, renal index, BUN and Cr was found in model group, which was significantly attenuated by treatment with TFE. Meanwhile, elevated MDA level in renal tissue as well as decreased SOD activities in renal tissue were significantly remitted by TFE. Furthermore, TFE decreased the expression of TGF-beta1.
CONCLUSIONTFE can evidently relieve renal damage in rats with diabetic nephropathy induced by STZ, which might be related to antioxidation and modulating the expression of TGF-beta1 protein.
Animals ; Diabetes Mellitus, Experimental ; metabolism ; Diabetic Nephropathies ; metabolism ; prevention & control ; Epimedium ; chemistry ; Flavonoids ; pharmacology ; Kidney ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley
10.Absorption and metabolism of flavonoids in Herba Epimedii via rat intestinal perfusion model.
Yan CHEN ; Xiaobin JIA ; Xiaobin TAN ; Chenyi FAN ; Ming HU
China Journal of Chinese Materia Medica 2009;34(22):2928-2931
OBJECTIVETo study the absorption and metabolism of five flavonoids of Herba Epimedii (icariin, epimedin A, epi-medin B, epimedin C and baohuoside I) in rat intestine.
METHODUsing the rat intestinal perfusion model, the contents of the five flavonoids in perfusates were measured by HPLC and the permeability coefficients in different intestines were calculated.
RESULTThe permeabilities of five flavonoids in duodenum, jejunum, ileum, colon according to the sequence were as: icariin: 6.365, 5.349, 1.004, 0.601, epimedinA: 4.120, 3.397, 0.401, 0.257, epimedin B: 3.645, 3.135, 0.990 7, 0.434, epimedin C: 3.114, 2.882, 0.688, 0.470, baohuoside I: 2.324, 2.398, 1.529, 1.045, respectively. The analysis of the perfusates showed that icariin, epimedin A, epimedin B, epimedin C could be hydrolyzed in intestine. Icariin had two hydrolytic metabolites, whereas epimedin A, B, C only had one hydrolytic metabolite, respectively.
CONCLUSIONThe results indicated that the absorption of all the five flavonoids was significantly different in different intestinal segments, and the permeability in ileum and colon was significantly lower than that of the duodenum and jejunum. The metabolites of icariin, epimedin A, epimedin B, epimedin C were related with their structures and enzymes in intestine, and the metabolites were more in duodenum, jejunum, whereas were less in ileum and colon.
Absorption ; Animals ; Epimedium ; chemistry ; Flavonoids ; metabolism ; pharmacokinetics ; Intestines ; drug effects ; physiology ; Male ; Models, Animal ; Perfusion ; Plant Extracts ; metabolism ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley