iridoids and morroniside

Morroniside and loganin are iridoid glycosides extracted from Cornus officinalis, a plant species widely used in traditional Chinese medicine. However, the anti-inflammatory effects of morroniside and loganin in colitis are barely understood. The aim of the present study was to explore the effects of morroniside and loganin on the dextran sodium sulfate (DSS)-induced murine model of colitis and an LPS-induced colorectal cancer (CRC) cell inflammation model, and to clarify the underlying mechanisms. We found that morroniside and loganin were able to ameliorate clinical features, including disease activity index (DAI), histological inflammation score and periodic acid-Schiff staining (PAS). In the mouse model, morroniside and loganin treatment increased expression of tight junction proteins (TJs) and decreased pro-inflammatory cytokine production. Moreover, our findings showed that the expression of p-STAT3 and p-p65 were suppressed compared to the disease group. In in vitro experiments, treatment with morroniside and loganin had no obvious effects on proliferative activity in HCT116 cells and HIEC-6 cells. Expression of pro-inflammatory cytokines was inhibited by morroniside and loganin treatment in comparison with the LPS-treated group. Taken together, morroniside and loganin have beneficial effects on colitis in vivo and are anti-inflammatory in vitro. Possible mechanisms of the anti-inflammatory response may include blockade of the STAT3/NF-κB pathway.

Topics: Animals; Anti-Inflammatory Agents; Cell Line; Colitis; Colitis, Ulcerative; Cornus; Dextran Sulfate; Disease Models, Animal; Glycosides; Humans; Iridoid Glycosides; Iridoids; Male; Medicine, Chinese Traditional; Mice; Mice, Inbred C57BL; NF-kappa B; Phosphorylation; Signal Transduction; STAT3 Transcription Factor

A wide variety of plant raw materials thought to promote health are used as herbal medicines as well as foods. However, there is no legal maximum or minimum concentration limit on any herbal compound when these plant raw materials are used in processed foods. Legally, these processed foods are regulated only for harmful substances, and there is no other guarantee of their contents. Therefore, the objective of this study was to determine the concentrations of 12 herbal compounds (nodakenin, decursin, decursinol angelate, morroniside, loganin, glycyrrhizic acid, liquiritigenin, puerarin, daidzin, schisandrin, gomisin A, gomisin N) in commonly used plant raw materials, such as "Angelica Gigas root", "Cornus Fruit", "Liquorice Root", "Pueraria Root", and "Schisandra Fruit"; and also in 45 processed foods, using high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Method validation was performed successfully using the parameters of specificity, linearity, limit of detection (LOD), limit of quantification (LOQ), accuracy, precision, matrix effect, extraction recovery, and stability. The 12 herbal compounds were determined to be present in all the foods advertised as containing each ingredient, although in very low concentrations in some cases. Three solid samples labelled as 100% pure material from one herbal species also contained herbal compounds found in others, so that intentional or unintentional adulteration was suspected.

Topics: Benzopyrans; Butyrates; Chromatography, Liquid; Coumarins; Cyclooctanes; Dioxoles; Flavanones; Food Analysis; Fruit; Glucosides; Glycosides; Glycyrrhizic Acid; Herbal Medicine; Iridoids; Isoflavones; Lignans; Plant Roots; Plants, Medicinal; Polycyclic Compounds; Tandem Mass Spectrometry

Alzheimer's disease (AD), also defined as a tauopathology, is a common neurodegenerative disease. Hyper-phosphorylation, cleavage or truncation, and aggregation of tau contribute to AD. Thus, targeting the post-translational modifications on tau may be a therapeutic strategy to treat AD. This study understood how cornel iridoid glycoside (CIG) affects tau post-translational modifications and synaptic abnormalities. The 10-month old P301S tau transgenic mice were given CIG at 100 and 200 mg/kg every day orally for 1 month. Hyperphosphorylated and truncated tau, synapse-associated proteins and glutamatergic receptors were all detected using Western blotting. The interactions between Morroniside (MOR) or Loganin (LOG) and tau were detected using Autodock and Surface Plasmon Resonance (SPR). The effects of CIG on the aggregation of tau were investigated using a cell-free system. CIG attenuated tau hyperphosphorylation at Thr205, Ser212, Ser262, Thr231 and Ser235 (AT180), but had no effect on tau truncation in the brains of 10-month old P301S mice. Binding free energies and interactions revealed that MOR and LOG bound with tau. We also found that CIG upregulated synapse-associated proteins such as PSD-95, syntaxin1A and synaptotagmin. In addition, CIG restored N-methyl-D-aspartic acid receptor and glutamate receptor levels. CIG improves post-translational modification of tau as well as synaptic abnormalities. The data presented here reveal that CIG may be used in the treatment of AD.

Topics: Administration, Oral; Animals; Brain; Cell-Free System; Disease Models, Animal; Female; Glycosides; Humans; Iridoids; Male; Mice; Mice, Transgenic; Models, Molecular; Molecular Docking Simulation; Mutation; Phenotype; Protein Binding; Receptors, Glutamate; Receptors, N-Methyl-D-Aspartate; tau Proteins; Tauopathies; Treatment Outcome

Qiangshen tablet, an important prescription consisting of 14 kinds of Chinese herbal medicines, has been used for decades to treat kidney yang deficiency syndrome (KYDS) in China. Qiangshen tablet has been recorded in ChP (2015 edition) and possesses the effect of strengthening yang, invigorating qi and tonifying kidneys. In this research, a simple, reliable and specific method was established for simultaneous determination of stachydrine, psoralen, isopsoralen, morroniside, paeoniflorin and loganin in normal and KYDS rat plasma after intragastric administration of a Qiangshen tablet suspension by UPLC-MS/MS. Protein precipitation (PP) by acetonitrile and liquid-liquid extraction (LLE) by ethyl acetate - n-butanol (1: 1, v/v) were used for pretreatment of plasma samples. Chromatographic separation of two IS (Internal Standard) and six analytes was achieved using an ACQUITY UPLC® BEH C

Topics: Animals; Chromatography, High Pressure Liquid; Drug Monitoring; Drugs, Chinese Herbal; Ficusin; Furocoumarins; Glucosides; Glycosides; Iridoids; Male; Metabolome; Monoterpenes; Proline; Rats; Rats, Sprague-Dawley; Tablets; Tandem Mass Spectrometry; Yang Deficiency

Herbal medicines are widely used as therapeutic products in many countries. Fructus Corni, a traditional herb medicine, has been clinically used to cure chronic nephropathy for thousands of years. It could be converted by gut microflora in vivo to shape its pharmacological profiles. Thus, metabolic profiles of major active constituents in Fructus Corni extracts by gut microflora from rats in healthy and nephropathy state were firstly investigated in vitro by ultraperformance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) in this study. According to the features of protonated ions, five metabolites (M1, M2, M3, M5 and M6) were found and preliminarily authenticated. Intestinal bacteria were capable of converting N0 (loganin) to its aglycone M1 (loganetin). The latter was further hydrogenated to the corresponding M2 (hydrogenated loganetin) and subsequently to M3 (hydrogenated and demethylated loganetin) by demethylation; While M5 (demethylated morronisid aglycone) and M6 (dehydroxylated morronisid aglycone) were identified as the two metabolites of N4 (morronisid) through demethylation and dehydroxylation. Gut microflora from healthy and nephropathy rats could degrade loganin and morronisid to the above metabolites. However, healthy rat intestinal bacteria showed more powerful degradation and much more amounts of M1 and M6 were obtained in their samples. Additionally, this work demonstrated that UPLC-Q-TOF/MS approach connected with MetaboLynx™ analysis software was rapid and reliable for screening and authentication of natural product metabolites.

Topics: Animals; Chromatography, High Pressure Liquid; Cornus; Gastrointestinal Microbiome; Glycosides; Iridoids; Mass Spectrometry; Plant Extracts; Rats; Renal Insufficiency, Chronic

Cornus officinalis-Rehmannia glutinosa herb couple is widely used herb medicine in clinical practice to treat chronic kidney disease (CKD). However, the in vivo integrated metabolism of its main bioactive components in CKD rats remains unknown. In this study, UPLC-Q-TOF/MS technique combined with Metabolynx

Topics: Administration, Oral; Animals; Case-Control Studies; Chromatography, High Pressure Liquid; Cornus; Feces; Glucosides; Glycosides; Iridoid Glucosides; Iridoids; Male; Phenols; Plant Extracts; Rats; Rehmannia; Renal Insufficiency, Chronic; Tandem Mass Spectrometry

Fructus Corni has been used for nourishing liver and kidney in clinical practice for many years. However, the in vivo integrated metabolism profile of its bioactive components remains unknown. In the present study, ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry coupled with the MetaboLynxTM software was established for screening and identification of the metabolites of the loganin and the morroniside in normal and chronic kidney disease (CKD) rat plasma, urine and feces after oral administration of Fructus Corni extract. The results showed that 11 metabolites including taurine and glucuronide conjugates, deglycosylated, dehydrated, (de)hydroxylated, (de)methylated, acetylated products were tentatively detected in normal rat samples while only eight metabolites were obtained in the model samples. Two parent compounds were both absorbed into the blood circulation of the normal and CKD rats. However, the compounds in the CKD rat showed lower metabolic capability. Few kinds and minor amounts of the metabolites were appeared in the CKD rat plasma, urine and feces. While considerable amounts of the parent compounds were detected in the CKD plasma. This helped maintain a high blood drug concentration which might be beneficial for the treatment of CKD. These results will be helpful for the further investigation of the pharmacokinetic study of Fructus Corni in vivo.

Topics: Administration, Oral; Animals; Biomarkers; Chromatography, High Pressure Liquid; Cornus; Glycosides; Iridoids; Male; Metabolome; Metabolomics; Plant Extracts; Rats; Rats, Sprague-Dawley; Renal Insufficiency, Chronic; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

Hypoglycemic activity-guided separation of ethanol extracts from the fruits of Cornus officinalis Sieb. et Zucc (CO) led to the isolation of loganin, morroniside, and ursolic acid. The antidiabetic capacity of CO extracts and related compounds was further investigated in diabetes mellitus mice. The results suggested that both CO extracts and pure compounds could ameliorate diabetes-associated damages and complications. Oral administration of loganin and morroniside decreased fasting blood glucose levels in diabetes mellitus mice. Ursolic acid exhibited the highest reactive oxygen species scavenging activity and α-glucosidase inhibitory activity. Notably, we noticed an interesting synergistic effect between loganin and ursolic acid. Given these favorable hypoglycemic properties, C. officinalis, a food and medicinal plant in China, may be used as a valuable food supplement for the treatment of diabetes mellitus.

Topics: alpha-Glucosidases; Animals; China; Cornus; Diabetes Mellitus, Experimental; Free Radical Scavengers; Fruit; Glycosides; Hep G2 Cells; Humans; Hypoglycemic Agents; Iridoids; Male; Mice; Plant Extracts; Plants, Medicinal; Reactive Oxygen Species; Triterpenes; Ursolic Acid

A sensitive and rapid method for determination of loganin, morroniside, catalpol and acteoside in rat plasma after oral administration of Rehmannia glutinosa Libosch and Cornus officinalis Sieb drug pair based on ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS). Chromatographic separation was achieved using an Acquity UPLC BEH C18 column (100mm×2.1mm, 1.7μm) at a flow rate of 0.4mL/min, using gradient mode containing 0.1% formic acid in water and acetonitrile were used as the mobile phase A and B. Loganin, morroniside, catalpol, acteoside and the internal standard (chloramphenicol) were detected by selected reaction monitoring in the negative ion mode with the mass transition of m/z 451.0→179.0 (morroniside), m/z 435.0→227.0 (loganin), m/z 407.1→199.1 (catalpol), m/z 623.2→161.0 (acteoside) and m/z 320.8→151.9 (chloramphenicol), respectively. All calibration curves showed good linearity (r>0.991). The precision was evaluated by intra-day and inter-day assays and the RSD% were all within 9.58%. The recovery ranged from 67.62 to 80.14%. The method was successfully applied to pharmacokinetic study of the analytes in normal and doxorubicin-induced chronic kidney disease rat plasma.

Topics: Administration, Oral; Animals; Chromatography, High Pressure Liquid; Cornus; Drugs, Chinese Herbal; Glucosides; Glycosides; Iridoid Glucosides; Iridoids; Limit of Detection; Male; Mass Spectrometry; Phenols; Rats; Rats, Sprague-Dawley; Rehmannia; Renal Insufficiency, Chronic

We evaluated the major active components isolated from Corni Fructus: loganin, morroniside, and 7-O-galloyl-D-sedoheptulose as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) for use in Alzheimer's disease treatment. These compounds exhibited predominant cholinesterase (ChEs) inhibitory effects with IC50 values of 0.33, 3.95, and 10.50 ± 1.16 µM, respectively, for AChE, and 33.02, 37.78, and 87.94 ± 4.66 µM, respectively, for BChE. Kinetics studies revealed that loganin and 7-O-galloyl-D-sedoheptulose inhibited AChE with characteristics typical of mixed inhibitors, while morroniside was found to be a noncompetitive inhibitor against AChE and also exerted mixed BChE inhibitory activities. For BACE1, loganin showed noncompetitive type inhibitory effects, while morroniside and 7-O-galloyl-D-sedoheptulose were found to be mixed inhibitors. Furthermore, these compounds exhibited dose-dependent inhibitory activity with ONOO(-)-mediated protein tyrosine nitration. Molecular docking simulation of these compounds demonstrated negative binding energies for ChEs, and BACE1, indicating high affinity and tighter binding capacity for the active site of the enzyme. Loganin was the most potent inhibitor against both ChEs and BACE1. The data suggest that these compounds together can act as a triple inhibitor of AChE, BChE, and BACE1, providing a preventive and therapeutic strategy for Alzheimer's disease treatment.

Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid Precursor Protein Secretases; Aspartic Acid Endopeptidases; Butyrylcholinesterase; Cholinesterase Inhibitors; Cornus; Drug Discovery; Glycosides; Heptoses; Iridoids; Kinetics; Molecular Docking Simulation; Protein Binding

Pharmacokinetic studies on traditional Chinese medicine are useful to evaluate and predict the drug efficacy and safety. The renal impairment may affect drug clearance and other pharmacokinetic processes which can increase toxicity and drug to drug interactions or cause ineffective therapy. Pharmacokinetic studies in pathological status rats might be meaningful for revealing the action mechanism and improving clinical medication of the herb medicine.. A highly sensitive and rapid ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) method with multiple-reaction monitoring (MRM) mode was developed and validated for simultaneous quantitation of morroniside and loganin in normal and doxorubicin-induced chronic kidney disease (CKD) rat plasma after oral administration of Shanzhuyu (fruit of Cornus officinalis) extract.. Both calibration curves gave satisfactory linearity (r>0.99) at linear range of 1.96-1962.5ngmL(-1) for morroniside, 1.53-1531.25ngmL(-1) for loganin. The precision and accuracy of the in vivo study were assessed by intra-day and inter-day assays. The percentages of relative standard deviation (RSD) were all within 9.58% and the accuracy (RE) was in the -6.02% to 8.11% range. The extraction recoveries of morroniside, loganin and internal standard (IS) were all >67.62% and the matrix effects ranged from 95.07% to 102.75%.. The pharmacokinetic behavior of morroniside and loganin in normal and CKD rat plasma was determined in this paper. The significant different pharmacokinetic parameters might partly result from the changes of P-glycoprotein and metabolic enzymes in the pathological state. The pharmacokinetic research in the pathological state might provide more useful information to guide the clinical usage of the herb medicine.

Topics: Administration, Oral; Animals; Chromatography, Liquid; Cornus; Fruit; Glycosides; Iridoids; Male; Plant Extracts; Rats, Sprague-Dawley; Renal Insufficiency, Chronic; Tandem Mass Spectrometry

The methanolic extract of the fruits of Cornus officinalis S et Z. (Cornaceae) showed the significant neuroprotective activity against glutamate-induced toxicity in HT22 hippocampal cells. Chemical profile of n-BuOH fraction of the methanolic extract of C. officinalis fruits, which showed the most potent activity, was established using HPLC-diode array detector-electrospray-MS (HPLC-DAD-ESI-MS). Through bioactivity-guided isolation, five iridoid glycosides including one new compound, 7-O-butylmorroniside (1), loganin (2), morroniside (3), 7R-O-methylmorroniside (4), 7S-O-methylmorroniside (5) were isolated from the n-BuOH fraction. The protective activities of the isolated compounds, themselves, were not statistically significant. However, the hydrolyzed products of compounds 1, 4 and 5 significantly protected glutamate-injured HT22 cells up to 78±2.2%, 60±3.2% and 59±2.5% of non-treated control, respectively.

Topics: Animals; Cell Line, Transformed; Chemical Fractionation; Chromatography, High Pressure Liquid; Cornus; Fruit; Glutamic Acid; Glycosides; Hippocampus; Hydrolysis; Iridoids; Methanol; Mice; Molecular Structure; Neuroprotective Agents; Plant Extracts; Spectrometry, Mass, Electrospray Ionization

To research the chemical constituents from stems and leaves of Lonicera macranthoides.. Various column chromatographies were employed to isolate and purify the constituents. Their structures were elucidated by spectral analysis (IR, MS, 1H-NMR, 13 C-NMR) and chemical evidence.. Nine constituents were obtained and identified as loganin (I), loganic acid (II), morroniside (III),7-O-ethyl-morroniside (IV), scopoletin (V), caffeic acid (VI), chlorogenic acid (VII), beta-sitosterol (VIII), daucosterol (IX).. Compounds I-VI are isolated from the plant for the first time. All the compounds are found for the first time from the stems and leaves of Lonicera macranthoides.

Topics: Caffeic Acids; Glycosides; Iridoids; Lonicera; Molecular Structure; Plant Leaves; Plant Stems; Plants, Medicinal; Scopoletin

Liuweidihuang wan (LW), initially a well-known formula for curing "wu chi wu ruan", is commonly used nowadays for clinical treatment of postmenopausal osteoporosis (PO), but the identity of the effective substance(s) remains unclear. The present study was designed to evaluate the effects of morroniside and loganin isolated from LW on the proliferation, differentiation and apoptosis of MC3T3-E1 cells, as well as the possible mechanism of action. Morroniside and loganin had no effects on the proliferation of MC3T3-E1 cells, but both susbtances could improve the activity of alkaline phosphatase (ALP), and increase the contents of collagen type I and osteocalcin. Simultaneously, the mRNA expression of caspase-3, capase-9, RANKL was down-regulated and that of bcl-2 was up-regulated, which partially explains the anti-osteoporosis mechanism in MC3T3-E1 cells. In conclusion, morroniside and loganin may directly promote the differentiation and inhibit the apoptosis of MC3T3-E1 cells, and accordingly indirectly reduce bone resorption, which makes them promising natural drugs leads for treating PO in the near future.

Topics: 3T3 Cells; Animals; Cell Proliferation; Drugs, Chinese Herbal; Female; Glycosides; Humans; Iridoids; Male; Mice; Osteoporosis, Postmenopausal

To investigate the effects of four original constituents (Loganin, Morroniside, Peoniflorin, Paeonol) of Liu-wei Di-huang pills on the proliferation and differentiation of rat preadipocyte, and optimize the best concentration by the orthogonal test.. The rat preadipocytes were cultured, then above four original constituents according to 4 factors and 3 levels to make L9 (3(4)) orthogonal test, and the control was performed at the same time. The proliferation of preadipocytes was determined by MTT method, and the accumulation of cellular lipid was determined by Oil Red O staining, the differences between factors and variances were compared by the value of absorbance.. The combination of four original constituents of Liu-wei Di-huang pills could stimulate rat preadipocyte proliferation and inhibited its lipid accumulation. Both the effects were highly significant (P < 0.01) with the combination of A3 B1 C3 D2; Compared with the monosomic group, the effects of the A3 B1 C3 D2 was highly significant (P < 0.01).. Compared with the monosomic group, the effects of the combination of the four original constituents of Liu-wei Di-huang pills on the proliferation and differentiation of rat preadipocyte were highly significant. This combination consists of Loganin, morroniside with high doses, Paeonol, Peoniflorin with mid-dose and low-dose, respectively. Regnesent the overall regulatory role of synergy and officiencg.

Topics: Acetophenones; Adipocytes; Animals; Benzoates; Bridged-Ring Compounds; Cell Differentiation; Cell Proliferation; Cells, Cultured; Drug Combinations; Drug Synergism; Drugs, Chinese Herbal; Fats; Glucosides; Glycosides; Iridoids; Male; Monoterpenes; Plants, Medicinal; Rats; Rats, Wistar

The aim of this study was to investigate the effects of cornel iridoid glycoside (CIG), an ingredient extracted from a traditional Chinese herb Cornus officinalis, on neurological function and neurogenesis after ischemic stroke. CIG was intragastrically administered to rats in doses of 20, 60 and 180 mg/kg/day, starting 3 h after the onset of middle cerebral artery occlusion (MCAO). The behavioral test was performed by using the modified neurological severity score (mNSS). Rats were sacrificed 7, 14, or 28 days after ischemia occurred. Neurogenesis and angiogenesis were detected by using immunofluorescence staining. The messenger ribonucleic acid (mRNA) expression of vascular endothelial growth factor (VEGF) and its receptor Flk-1 was measured by RT-PCR, and the protein expression of VEGF was determined by Western blotting analysis. The treatment with CIG at the doses of 60 and 180 mg/kg/day significantly improved neurological function, and increased the number of bromodeoxyuridine (BrdU)-positive cells and nestin-positive cells in the subventricular zone of rats 7, 14 and 28 days after ischemia. The number of newly mature neurons and blood vessels in striatum, as indicated by BrdU/NeuN and vWF immunoreactivity, respectively, was also increased in CIG-treated rats 28 days after stroke. CIG treatment obviously enhanced the mRNA expression of VEGF and its receptor Flk-1 and the protein expression of VEGF 7 and 28 days after ischemia. The results indicated that CIG promoted neurogenesis and angiogenesis and improved neurological function after ischemia in rats, and the mechanism might be related to CIG's increasing VEGF and Flk-1 in the brain.

Topics: Angiogenesis Inducing Agents; Animals; Brain; Cognition; Cornus; Drugs, Chinese Herbal; Glycosides; Infarction, Middle Cerebral Artery; Iridoids; Male; Neurogenesis; Neurons; Neuroprotective Agents; Neuropsychological Tests; Phytotherapy; Random Allocation; Rats; Rats, Sprague-Dawley; RNA, Messenger; Vascular Endothelial Growth Factor A; Vascular Endothelial Growth Factor Receptor-2

A simple and rapid HPLC method was established for simultaneously determining six active components in Fructus Corni. The six components were separated on an Agilent Zorbax Extend C18 column (250 mmx4.6 mm, 5 microm) and detected by diode array detector (DAD). Mobile phase was composed of (A) aqueous phosphoric acid (0.1%, v/v) and (B) acetonitrile phosphoric acid (0.1%, v/v) using a gradient elution. Analyses were performed at 30 degrees C with a flow rate of 1.0 mL/min and UV detection at 218 nm, 240 nm and 284 nm. All calibration curves showed good linear regression (r2>or=0.9999) within tested ranges. The LOD and LOQ were 0.11-1.69 microg/mL and 1.48-16.60 microg/mL, respectively. Overall intra-day and inter-day variations were less than 4.72%, and the average recoveries were 97.97-102.51% for the analytes. The developed method can be applied to the intrinsic quality control of Fructus Corni.

Topics: Biological Assay; Calibration; Chromatography, High Pressure Liquid; Cornus; Drugs, Chinese Herbal; Furaldehyde; Gallic Acid; Glucosides; Glycosides; Iridoid Glucosides; Iridoids; Molecular Structure; Pyrans; Reproducibility of Results; Time Factors

To elucidate the promoting effect of the constituents in plasma after oral administration of Liuwei Dihuangwan on proliferation of rat osteoblast.. To add the constituents in plasma after oral administration of Liuwei Dihuangwan with rational concentration into culture solution of rat osteoblast, later using MT method for determining the proliferation rate of rat osteoblast.. The Mixed group including morroniside, sweroside and loganin with different dose all significantly promoted proliferation of rat osteoblast.. This study preliminarily elucidated the constituents such as morroniside, sweroside and loganin in plasma after oral administration of Liuwei Dihuangwan were main biological constituents which contributed to anti-osteoporosis bioactivity of Liuwei Dihuangwan.

Topics: Administration, Oral; Animals; Cell Proliferation; Cells, Cultured; Drugs, Chinese Herbal; Glucosides; Glycosides; Iridoid Glucosides; Iridoids; Osteoblasts; Plasma; Rats; Rats, Wistar

A micellar electrokinetic chromatography (MEKC) method for the simultaneous determination of four bioactive constituents (morroniside, loganin, paeoniflorin and paeonal) in the Chinese patent medicine Liuwei Dihuang Pills is established. A carrier composed of 0.2M boric acid, 0.02 M sodium dodecyl sulfate (SDS) and 5% acetonitrile (pH was adjusted to 10.5 with 0.1 M NaOH) is found to be the most suitable electrolyte for this separation. The four constituents in Liuwei Dihuang Pills can be easily determined within 16 min. Optimization of separation is realized with the univariate approach by studying the effects of four factors relevant to run buffer on migration times.

Topics: Acetonitriles; Benzoates; Boric Acids; Bridged-Ring Compounds; Buffers; Chloramphenicol; Chromatography, Micellar Electrokinetic Capillary; Drug Carriers; Drugs, Chinese Herbal; Glucosides; Glycosides; Humans; Hydrogen-Ion Concentration; Iridoids; Molecular Structure; Monoterpenes; Reference Standards; Reproducibility of Results; Sodium Dodecyl Sulfate; Time Factors

To gain a clear idea on function of getting fid of cores of Cornus officinalis Sieb. et Zucc. and elect a suitable processing method and technics of Crnus officinalis Sieb. et Zucc. in producing area.. The contents of loganin and morroniside were determined in the cores and sarocarp of Cornus officinalis Sieb. et Zucc.; Using pathogonal method, the methods which Cornus officinalis sieb. et Zuee. were warmed or poached were isolated by determining quantitively loganin from Cornus officinalis Sieb. et Zucc. by HPLC.. There was a bit loganin and morroniside in the cores of Cornus officinalis Sieb. et Zuecc.; There were three aspects that were marked influence to extracted account of loganin which were hot temperature of poach, adding water and time of warming. The best suitable extracting technology was warmed in 60 degrees C by 10 min and then getted rid of cores.. Clearing the non-medicinal positon is the function of getting rid of cores of Cornus officinalis Sieb. et Zucc. and warming is better than poach.

Topics: Chromatography, High Pressure Liquid; Cornus; Drugs, Chinese Herbal; Fruit; Glycosides; Iridoids; Plants, Medicinal; Quality Control; Technology, Pharmaceutical; Time Factors

Advanced glycation end products (AGE) are involved in the alterations of renal mesangial cell (MCs) growth, a feature of early stages of diabetic nephropathy (DN). We postulate that morroniside and loganin, 2 components extracted from Cornus officinalis, may ameliorate the detrimental effects of AGE-induced MCs proliferation by preventing oxidative stress. Rat MCs cultured in AGE milieu were treated with morroniside and loganin. Results showed that morroniside and loganin inhibited AGE-induced MC proliferation as measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Fluorescence microscopy revealed that the morroniside and loganin improved the morphological changes of MCs. Flow cytometric analysis showed that morroniside and loganin inhibited the cell cycle of rat MCs. Furthermore, the level of reactive oxygen species was significantly reduced, and the activities of superoxide dismutase and glutathione peroxidase were markedly increased, whereas the level of malondialdehyde was not significantly reduced. These results suggest that morroniside and loganin regulate MC growth by preventing oxidative stress. Thus, this study provides a molecular basis for the use of morroniside and loganin in the early stages of DN.

Topics: Animals; Antioxidants; Cell Cycle; Cell Line; Cell Proliferation; Cell Shape; Cornus; Diabetic Nephropathies; Flow Cytometry; Glutathione Peroxidase; Glycation End Products, Advanced; Glycosides; Iridoids; Malondialdehyde; Mesangial Cells; Microscopy, Fluorescence; Oxidative Stress; Rats; Reactive Oxygen Species; Superoxide Dismutase