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Magnolol, a hydroquinone containing an allyl side chain, is one of the major active components of magnolia for antioxidation and anti-aging. To enhance the anti-aging activity and improve the intramolecular hydrogen bonding of magnolol, magnolol was reacted with cinnamic acid to obtain 2-O-cinnamic acid magnolol by esterification. The anti-aging activity of magnolol 2-O-cinnamate was investigated based on Caenorhabditis elegans model. The results showed that 2-O-cinnamic acid magnolol can reduce lipofuscin accumulation in the nematode body, and the effect is better than that of magnolol. 2-O-Cinnamic acid magnolol can extend nematode lifespan, reduce ROS levels in nematodes during normal aging and oxidative stress and improve nematode stress resistance under heat stress and oxidative stress. 2-O-Cinnamic acid magnolol could induce DAF-16 translocation from the cytoplasm to the nucleus and upregulate the expression of the sod-3 gene encoding superoxide dismutase in the nematode TJ356 expressing DAF-16 fused with GFP. 2-O-Cinnamic acid magnolol did not improve the survival rate of hsp-16.2 gene deficient nematodes under oxidative stress, indicating that 2-O-cinnamic acid magnolol improves stress resistance of nematodes under oxidative stress may be associated with sod-3 and hsp-16.2. Moreover, 2-O-cinnamic acid magnolol did not extend the lifespan of daf-16 and age-1 mutants, indicating that age-1 and daf-16 are required for 2-O-cinnamic acid magnolol to delay aging. It showed that magnolol 2-O-cinnamic acid has the potential to improve antioxidant capacity and delay aging, and the mechanism may be related to the insulin/insulin-like growth factor signaling pathway.
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OBJECTIVE Right ventricular (RV) remodeling is one of the essential pathological features in pulmonary arterial hypertension (PAH). RV hypertrophy or fibrosis are the leading causes of RV remodeling. Magnolol is a com?pound isolated from Magnolia officinalis. It possesses multiple pharmacological activities, such as anti-oxidation and anti-inflammation. This study aims to evaluate the effects and underlying mechanisms of magnolol on RV remodeling in hypoxia-induced PAH. METHODS ① Male SD rats (220 g) were randomly divided into 5 groups (n=10): the normoxia group, the hypoxia group, the hypoxia plus Magnolol (10 and 20 mg·kg-1·d-1) group, and the vehicle group. Rats in the normoxia group were kept in a normoxia environment for 4 weeks, while rats in the hypoxia group were kept in a hypoxic chamber (10％ O2). The rats in the hypoxia plus magnolol groups were administered with magnolol at 10 or 20 mg·kg-1 (ip) once a day for 4 weeks. At the end of 4 weeks, the heart function was assessed by Doppler echocardiography, and then the rats were anesthetized with sodium pentobarbital (30 mg·kg-1, ip). The RVSP was measured by the right heart catheterization method. The heart tissues were collected and dissected to calculate the index of RV remodeling (RV/LV+IVS, RV/tibial length, or RV/body weight). Part of the RV samples was fixed with 4％paraformaldehyde for morphological analysis, while other samples were frozen at-80℃for molecular studies (measurements of ANP, BNP,α-SMA, and col?lagen Ⅰ/Ⅲ mRNA expression as well as p-JAK2/JAK2 and p-STAT3/STAT3 protein levels). ② To evaluate the effect of magnolol on hypoxia-induced myocardial hypertrophy and fibrosis, H9c2 or cardiac fibroblasts were divided into 7 groups: the control group, cells were cultured under normal conditions; the hypoxia group, cells were cultured under hypoxic condition (3％ O2);the hypoxia plus magnolol 10 mg·kg-1 group, magnolol10μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus magnolol 30 mg·kg-1 group, magnolol 20μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus TG-101348 group, TG-101348 (a specific inhibitor of JAK2) 1μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus JSI-124 group, JSI-124 (a specific inhibitor of JAK2) 1μmol·L-1 was added to the culture medium before the hypoxia treatment;and the hypoxia plus vehicle group, an equal volume of vehicle (DMSO) was added to the culture medium before the hypoxia treatment. At the end of the experiments, the cells were collected for morphological and molecular analysis. RESULTS In vivo, male Sprang-Daley rats were exposed to 10％ O2 for 4 weeks to establish an RV remodeling model, which showed hypertrophic and fibrotic features (increases of RV remodeling index, cellular size, hypertrophic and fibrotic marker expression), accompanied by an elevation in phosphorylation levels of JAK2 and STAT3;these changes were attenuated by treating rats with magnolol. In vitro, the cultured H9c2 cells or cardiac fibroblasts were exposed to 3％ O2 for 48 h to induce hypertrophy or fibrosis, which showed hypertrophic (increases in cellular size as well as the expression of ANP and BNP) or fibrotic features (increases in the expression of collagenⅠ, collagenⅢandα-SMA). Administration of mag?nolol and TG-101348 or JSI-124 (JAK2 selective inhibitors) could prevent the process of myocardial hypertrophy and fibrosis, accompanied by the decrease in the phosphorylation level of JAK2 and STAT3. CONCLUSION Magnolol can attenuate RV hypertrophy and fibrosis in hypoxia-induced PAH rats through a mechanism involving inhibition of the JAK2/STAT3 signaling pathway.
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Mitochondria as a signaling platform play crucial roles in deciding cell fate. Many classic anticancer agents are known to trigger cell death through induction of mitochondrial damage. Mitophagy, one selective autophagy, is the key mitochondrial quality control that effectively removes damaged mitochondria. However, the precise roles of mitophagy in tumorigenesis and anticancer agent treatment remain largely unclear. Here, we examined the functional implication of mitophagy in the anticancer properties of magnolol, a natural product isolated from herbal
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Objective: To optimize the supercritical CO2 extraction process of active ingredients from Magnoliae Officinalis Cortex (MOC) and explore the antioxidant activity of the extracts. Methods: The content of magnolol and honokiol of the supercritical CO2 extracts of MOC was determined by HPLC, and the extraction process was optimized by orthogonal experiment. The antioxidant activities of the extracts were determined by MTT. Results: The optimum extraction pressure of magnolol was 25 MPa, the extraction temperature was 55 ℃, the amount of CO2 was 30 kg, and the optimum extraction parameters mentioned above of honokiol were 15 MPa, 50 ℃, and 25 kg, respectively. Conclusion: Under the optimum extraction conditions, magnolol and honokiol have high extraction efficiency, good repeatability, stability and feasibility, and the extract have good antioxidant activity.
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Objective: To prepare magnolol solid dispersions (Mag-SD), magnolol phospholipids complex (Mag-PC) and magnolol solid lipid nanoparticles (Mag-SLN), and compare their effects on the pharmacokinetics in vivo. Methods: Solvent evaporation method was used to prepare Mag-SD and Mag-PC. Their existential state of Mag in Mag-SD and Mag-PC were analyzed by X-ray power diffraction (XRPD). High pressure homogenization method was employed to prepare Mag-SLN, its particle size and Zeta potential were also studied. The dissolution in vitro of Mag-SD, Mag-PC and Mag-SLN were also studied compared to magnolol suspension. SD rats in each group were administered intragastrically with magnolol, Mag-SD, Mag-PC and Mag-SLN, respectively. The concentration of magnolol in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. The pharmacokinetic behavior and bioavailability of magnolol, Mag-SD, Mag-PC and Mag-SLN were also compared. Results: The results of XRPD indicated that magnolol showed an amorphous state in Mag-SD and Mag-PC. The average particle size and Zeta potential of Mag-SLN was (161.37 ± 3.77) nm and (-29.16 ± 1.83) mV, respectively. The results of dissolution in vitro indicated that the cumulative dissolution of magnolol was 30.6% within 12 h. Mag-SD, Mag-PC and Mag-SLN enhanced its cumulative dissolution to 96.3%, 76.4% and 45.9%, respectively. The results of pharmacokinetics in vivo showed that Cmax, AUC0-t and AUC0-∞ of Mag-SD, Mag-PC and Mag-SLN were enhanced greatly compared to magnolol suspension. Mag-PC, Mag-SD and Mag-SLN increased its Cmax from (429.67 ± 53.12) ng/mL to (533.62 ± 59.01), (721.73 ± 103.44) and (1 063.21 ± 108.22) ng/mL, respectively. The bioavailability of Mag-SD, Mag-PC and Mag-SLN were enhanced to 1.38, 2.12 and 3.45 times, respectively. Conclusion: Mag-SD, Mag-PC and Mag-SLN could promote the absorption of magnolol in SD rats notably. In addition, Mag-SLN could give a better effect on the bioavailability.
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Objective:To study the anti-colon cancer effect and mechanism of magnolol analogue CT2-3， in order to lay a foundation for the application of CT2-3 in anti-colon cancer area. Method:Colon cancer cells SW480 and LoVo were cultured in vitro. Different concentrations （10， 20， 40， 80 μmol·L-1） of CT2-3 and magnolol were used to stimulate colon cancer cells for 24， 48 h. The effect of CT2-3 and magnolol on the cell viability of colon cancer cells was detected by cell counting kit （CCK-8）. Colony formation assay was used to detect the colony formation capacity of CT2-3 on colon cancer cells. Flow cytometry and Western blot were used to determine the effect of CT2-3 on the apoptosis of colon cancer cells and the expression of DNA damage marker phosphorylated histone H2AX （γH2AX）. Reactive oxygen species （ROS） generation was measured by ROS assay kit. Real time quantitative polymerase chain reaction （Real-time PCR） was used to detect the effect of CT2-3 on expressions of mitochondrial apoptosis-related genes B-cell lymphoma-2 （Bcl-2） and Bcl-2-associated X （Bax） in colon cancer cells. Result:The half maximal inhibitory concentration （IC50） of magnolol in two kinds of colon cancer cells after treatment for 24， 48 h were both higher than 80 μmol·L-1. While the IC50 of CT2-3 in SW480 cells after treatment for 24， 48 h were （54.59±1.73） μmol·L-1 and （29.82±1.13） μmol·L-1， respectively. The IC50 of CT2-3 in LoVo cells after treatment for 24，48 h were （66.68±2.11） μmol·L-1 and （46.70±1.81） μmol·L-1， respectively. Compared with the blank group， the colony formation capacity of colon cancer cells in CT2-3 groups （20， 40 μmol·L-1） was significantly decreased in a dose-dependent manner （P<0.01）， apoptotic colon cancer cells were significantly increased （P<0.01）， relative expression of DNA damage marker γH2AX was significantly increased （P<0.01）， ROS was significantly increased （P<0.01）. In addition， relative mRNA expression of Bcl-2 was significantly decreased （P<0.01）， while relative mRNA expression of Bax was significantly increased （P<0.01）. Conclusion:CT2-3 can remarkably inhibit colon cancer cells， and the underlying mechanism might be that CT2-3 promotes mitochondria dysfunction and ROS generation by regulating expressions of mitochondrial apoptosis-related genes， so as to further induce DNA damage and finally lead to apoptosis.
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Objective@#To simultaneously determinate 4 effective components in Fructus Cannabis Bolus by high performance liquid chromatography (HPLC).@*Methods@#The column was ALLTIMA-C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase was methanol (A)-0.1% phosphoric acid aqueous solution (B) in gradient elution program. The flow rate was 1.0 ml/min, the column temperature was 30℃, and the injection volume was 10 μl. The detection wavelength was set at 254 nm.@*Results@#The linear ranges of 4 effective components of emodin, chrysophanol, parietic acid, and magnolol were 9.05-81.26 μg (r=0.999 8), 13.28-119.3 μg (r=0.997 6), 8.30-75.40 μg (r=0.998 7), 6.30-61.79 μg (r=0.996 5), respectively; the average recoveries and RSDs of emodin, chrysophanol, parietic acid, and magnolol were 99.25%, 99.46%, 99.51%, 99.86%, respectively. The RSDs of emodin, chrysophanol, parietic acid, and magnolol were 2.04%, 3.23%, 1.84%, and 2.42%, respectively.@*Conclusions@#The HPLC can be used as an effective and feasible method for the determination of emodin, chrysophanol, parietic acid, and magnolol in Fructus Cannabis Bolus. The method is simple, quick, and reproducible, and can be used for the quality control of Fructus Cannabis Bolus.
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Objective To simultaneously determinate 4 effective components in Fructus Cannabis Bolus by high performance liquid chromatography (HPLC). Methods The column was ALLTIMA-C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase was methanol (A)-0.1% phosphoric acid aqueous solution (B) in gradient elution program. The flow rate was 1.0 ml/min, the column temperature was 30℃, and the injection volume was 10 μl. The detection wavelength was set at 254 nm. Results The linear ranges of 4 effective components of emodin, chrysophanol, parietic acid, and magnolol were 9.05-81.26 μg (r=0.999 8), 13.28-119.3 μg (r=0.997 6), 8.30-75.40 μg (r=0.998 7), 6.30-61.79 μg (r=0.996 5), respectively; the average recoveries and RSDs of emodin, chrysophanol, parietic acid, and magnolol were 99.25%, 99.46%, 99.51%, 99.86%, respectively. The RSDs of emodin, chrysophanol, parietic acid, and magnolol were 2.04%, 3.23%, 1.84%, and 2.42%, respectively. Conclusions The HPLC can be used as an effective and feasible method for the determination of emodin, chrysophanol, parietic acid, and magnolol in Fructus Cannabis Bolus. The method is simple, quick, and reproducible, and can be used for the quality control of Fructus Cannabis Bolus.
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Allergic asthma, is a common chronic inflammatory disease of the airway presenting with airway hyperresponsiveness and airway remodelling. T helper cells-derived cytokines are critically associated with asthma pathogenesis. Janus kinase-signal transduction and activation of transcription (JAK/STAT) signaling is found to be involved in asthma. Magnolol is a plant-derived bioactive compound with several pharmacological effects. The study aimed to assess the effects of magnolol in ovalbumin (OVA)-induced asthmatic model. BALB/c mice were sensitized and challenged with OVA. Magnolol (12.5, 25, or 50 mg/kg body weight) was administered to separate groups of animals. Dexamethasone was used as the positive control. Cellular infiltration into the bronchoalveolar lavage fluid (BALF) were reduced on magnolol treatment. The levels of Th2 and Th17 cytokines were reduced with noticeably raised levels of interferon gamma. Lung function was improved effectively along with restoration of bronchial tissue architecture. OVA-specific immunoglobulin E levels in serum and BALF were decreased by magnolol. Magnolol reduced Th17 cell population and effectively modulated the JAK-STAT and Notch 1 signaling. The results suggest the promising use of magnolol in therapy for allergic asthma.
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Animals , Mice , Airway Remodeling , Asthma , Bronchoalveolar Lavage Fluid , Cytokines , Dexamethasone , Immunoglobulin E , Immunoglobulins , Interferons , Lung , Ovalbumin , Ovum , Th17 CellsABSTRACT
Objective: To establish the grade evaluation standard for Magnoliae Officinalis Cortex processed with ginger juice by combining traditional morphology evaluation with modern intrinsic quality evaluation. Method: The morphological parameters and contents of intrinsic pharmacodynamic index components of 28 batches of Magnoliae Officinalis Cortex processed with ginger juice were determined, and the relative quality constants were calculated. Assuming that the average relative quality constant was 100%, more than 120%of the samples were classified as the first grade, 60%to 120%as the second grade, the remaining as the third grade. Result: The relative quality constant of Magnoliae Officinalis Cortex processed with ginger juice ranged from 0.09 to 1.78. The relative quality constant of the first grade was ≥ 0.64, the second grade was 0.32-0.64, while the third grade was ≤ 0.32. Conclusion: Relative quality constant combines external indexes of traditional morphology and internal indexes of pharmacodynamic components, which can objectively, reasonably and scientifically classify the grade of Magnoliae Officinalis Cortex processed with ginger juice, and provide reference for establishing and improving the grade evaluation standard of this decoction pieces.
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Objective To study the dry extract rate, determination and transfer rate of maker compounds, and fingerprint of standard decoction of ginger juice Magnoliae Officinalis Cortex (GJMOC) and provide a reference for the preparation and quality assessment of its dispensing granules by establishing 16 batches of standard decoction of GJMOC. Methods A total of 16 batches of GJMOC standard decoctions were prepared following literature requirements. The quantitative analysis method of magnolol and honokiol was according to Chinese Pharmacopoeia (2015 edition). The transfer rate of total magnolol and honokiol and extraction rate were calculated. the pH value was determined and HPLC fingerprint was established under a flow rate of 1 mL/min and eluted with a mobile phase of acetonitrile (A)-0.1% phosphoric acid solution (B) in a gradient mode (0-15 min, 12%-16% A; 15-30 min, 16%-28% A; 30-42 min, 28%-74% A; 42-55 min, 74%-80% A). The column temperature was set at 40℃ and the detection wavelength was 294 nm. Results By measuring the of 16 batches of standard decoction, the transfer rate of the sum of magnolol and honokiol ranged from 6.5% to 12.0%, the extraction rate was at a range of 3.41% to 7.14% and pH value was 4.63 to 5.43. The Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine (2012A) was used to analyze and compare the fingerprints, and seven common peaks were determined and four were identified including magnoloside B (peak 1), magnoloside A (peak 2), honokiol (peak 6), and magnolol (peak 7). The similarity among 16 batches of standard decoction of GJMOC was evaluated, and the similarity was all greater than 0.69. Moreover, this study established an HPLC fingerprint analysis method of GJMOC standard decoction. Conclusion The preparation method established in this study is stable and feasible, and the analysis method shows good precision, stability, and repeatability in fingerprint analysis and it is suitable for evaluating the quality of standard decoction of GJMOC.
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Objective: Hot-melt extrusion technique was applied to prepare magnolol solid dispersions, which can improve the in vitro solubility of magnolol and the in vivo bioavailability in rats. Methods: Four kinds of excipients, such as PS-630, HPC, EPO, and Soluplus, which were compatible with magnolol were used to prepare solid dispersions of different drug loadings by solubility parameter calculation. The prepared solid dispersion was characterized by differential scanning calorimetry (DSC), X-ray diffraction analysis (XRPD) and infrared spectroscopy (IR) using in vitro dissolution as an indicator; UPLC-MS/MS was used to evaluate the pharmacokinetic behavior of rats after oral administration of magnolol solid dispersion. Results: The in vitro dissolution test showed that the solid dispersion prepared by the 1:6 drug loading of PS-630, HPC, and EPO can significantly improve the dissolution of magnolol, and the drug was dispersed in the carrier in an amorphous state. The in vivo bioavailability test showed that the Cmax of magnolol in the solid dispersion prepared by PS-630 and HPC was about five times and 2.3 times that of the monomer, respectively, and the AUC0-t was increased about 37.22% and 70.88%, respectively. There was no increase in the EPO system. Conclusion: Hot melt extrusion technology can be successfully applied to improve the in vitro dissolution and in vivo bioavailability of the poorly soluble drug magnolol.
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OBJECTIVE： To prepare Magnolol nano-crystal suspension （MAG-NS）， and to conduct quality evaluation. METHODS： The preparation technology of MAG-NS was optimized by central composite design-response surface methodology with OD value of particle size and polydispersity coefficient as evaluation indexes， using volume ratio of organic phase to water phase， ratio of excipient to drug， concentration of magnolol as factors and conduct validation tests. The quality of MAG-NS prepared optimal technology was evaluated. RESULTS： Optimized technology included that the volume ratio of organic phase to water phase was 1 ∶ 5， mass ratio of excipient to drug was 4 ∶ 1， concentration of magnolol was 2 mg/mL. In 3 times of validation tests， average OD value was 0.940 0 （RSD＝0.08％）， relative error of which to predicted value 0.977 7 was 3.86％. magnolol nano-crystals of MAG-NS prepared by the optimal technology were spherical， uniform in size， smooth in surface， with particle size of （34.88±0.33） nm， polydispersity coefficient of 0.032±0.001 and drug loading amount of （17.83±0.92）％. CONCLUSIONS： Established preparation method is simple and feasible. Prepared MAG-NS is in line with quality requirements. It can provide reference for further development and utilization of MAG-NS.
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AIM To investigate the pharmacokinetic behaviors of four constituents in Huanglian Xiangru Decoction in rat plasma.METHODS The rats intragastrically administered with diluted drug (9 g/kg) had their blood collected for the determination of plasma concentration by HPLC,after which pharmacokinetic parameters were calculated by 3p97 software.RESULTS The plasma concentration-time curves for berberine hydrochloride,apigenin,honokiol,magnolol accorded with open one compartment model,with the Tpeak values of (1.436 5 ± 0.311 9),(2.049 5 ±0.705 5),(1.359 0 ±0.343 4),(1.195 9 ±0.334 6) h,AUC values of (1.477 8 ± 0.4840),(1.063 0±0.452 1),(0.863 5±0.2697),(7.0105 ±2.584 7) μg/(mL· h),Cmax values of (0.245 9 ±0.019 4),(0.129 6 ±0.016 7),(0.180 9 ±0.021 3),(0.966 7 ±0.042 0) μg/mL,respectively.CONCLUSION Compared with the other three constituents in Huanglian Xiangru Decoction,magnolol demonstrates better in vivo absorption and higher bioavailability.
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Objective:To establish a GC method for the imultaneous determination of cinnamaldehyde, bornyl acetate, costunol-ide,dehydrocostus lactone,magnolol and honokiol in Dutong pills. Methods: The determination was performed on an HP-5 column (30 m ×0.32 mm,0.25 μm) with programmed temperature. The carrier gas was nitrogen with the flow rate of 2.0 ml·min-1. The injection volumn was 1 μl and the sample split ratio was 5:1. The inlet temperature was 280 ℃. The detector was a flame ionization detector with temperature at 300 ℃. Results:The linear ranges were 32.28-516.40 μg·ml-1for cinnamaldehyde(r=0.999 3), 27.06-433.00 μg·ml-1for bornyl acetate(r=0.999 2),25.65-410.40 μg·ml-1for costunolide(r=0.999 3),26.10-417.60 μg ·ml-1for dehydrocostus lactone(r=0.999 3),24.01-384.20 μg·ml-1for magnolol(r=0.999 0) and 18.32-293.10 μg·ml-1 for honokiol(r=0.999 4). The average recovery was 99.71%(RSD=0.67%),99.34%(RSD=1.18%),100.16%(RSD=0. 34%),100.40%(RSD=0.39%),99.32%(RSD=1.22%) and 99.58%(RSD=0.58%)(n=6),respectively. Conclusion:The method is simple,sensitive and accurate,can be used to supplement the insufficient quality control of Dutong pills.
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Objective The quality evaluation of the Shuwei mixture was determined by the content of the six components of sinapine cyanide sulfonate, magnolol, honokiol, hesperidin, naringin and neohesperidin. Methods RP-HPLC method was used.The separation was performed on a Agilent ZORBAX Eclispse SB-C18column (4.6 mm×250 mm,5 mm),the mobile phase consisted of acetonitrile(A)-0.1% phosphoric acid with gradient elution at the flow rate of 1.0 mL·min-1.The detection wavelength was 326 nm ( sinapine cyanide sulfonate ), 294 nm ( magnolol, honokiol ) and 283 nm ( naringin, neohesperidin).The column temperature was kept at 30 ℃. Results The sinapine cyanide sulfonate, magnolol, honokiol, hesperidin,naringin and neohesperidin all had good linear relationship in the ranges of 0.049 6-1.24,0.048 2-1.205,0.060 5-1.512 5,0.187 2-4.68,0.131 6-3.29,0.197-4.925 μg.The average recoveries were 100.66%, 99.86%, 101.37%, 102.41%, 99.01%, 102.05%, respectively, RSD were 0.82%, 1.89%, 2.56 %, 0.74%, 1.54%, 0.99%, respectively. Conclusion The method is simple,accurate,reproducible and nice to the separation,and can be used for the quality evaluation of Shuwei mixture.
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Objective To investigate the effect and mechanism of magnolol on hippocampal neuroplasticity in depression model rats. Methods In this study, depression model rats were prepared with unpredictable chronic mild stress (UCMS), and was given different doses of magnolol (20, 40 mg/kg) for 28 d. The rats in the positive control group were given fluoxetine (20 mg/kg) for 28 d. The ameliorative effects of magnolol on symptom of depression were investigated through behavior tests including open-field test, sucrose preference test, and forced-swimming test. The mRNA levels of Map-2, Gap43, and SYP in the hippocampus, cortex and striatum of rats in each group were detected by qRT-PCR, and the localization and expression of MAP-2, GAP43, and SYP in the hippocampus were observed by immunohistochemical staining analysis. The quantitative analysis of MAP-2, p-MAP-2, and p-ERK in hippocampus of rats in each group were further analyzed by Western blotting. Results UCMS was able to decrease the sucrose preference index, reduce locomotor activity and increase the immobility time in the forced swimming test. Compared with model group, magnolol significantly increased the spontaneous activity of rats, increased the consumption of sugar and water, and decreased the immobility time of chronic stress rats in forced swimming (P < 0.05, 0.01). Magnolol reversed MAP-2 mRNA and protein level in the hippocampus, increased phosphorylated MAP-2 expression in the hippocampus (P < 0.05), and significantly restored the p-ERK expression (P < 0.05). Conclusion Magnolol can affect the phosphorylation of MAP-2 through ERK pathway and increase the expression of MAP-2, thus affecting the neuronal plasticity and exerting its antidepressant effect.
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Lignans which are polymerized by two or more phenylpropanoids derivatives were mostly found in the xylem and resin of plants. Modern pharmacological studies have shown that lignans have extensive biological activities, such as anti-tumor, anti-HIV, antidiabetics, anti-oxidant, cardiovascular and liver protections and so on. However, owing to the poor solubility of structures, its clinical application is still limited. Therefore, chemical modification methods are usually used by domestic and overseas researchers in order to improve their solubility. In this paper, a series of typical lignans such as arctigenin, podophyllotoxin, schisandrin, magnolol, and honokiol were taken as examples to summarize their structural modification methods and different biological activities, aiming to provide scientific basis for further exploitation and studies of lignans.
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Based on the chemical structures of magnolol and honokiol,a series of small molecular derivatives were designed for the treatment of Alzheimer's disease.Through the Discovery Studio,five compounds (6a-6e) exhibited the inhibitory activity against Aβ and Tau proteins in all of the designed compounds.Then the five compounds are chemically synthesized and their biological activities were tested by thioflavin T.The result showed that compound 6a had inhibitory effect on the aggregation of two kinds of target proteins at the concentration of 100 μmol/L,which deserves further research.
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Objective:To establish a method for simultaneously determining 3 components ( hesperidin, magnolol and honokiol) in Xiaoji Huachong powder by UPLC. Methods: The experiments were performed on a Thermo Accucore C18 column ( 150 mm × 4. 6 mm, 2. 6 μm). The mobile phase was methanol-0. 5% glacial acetic acid in water with gradient elution, the flow rate was 0. 7 ml ·min-1 , the column temperature was maintained at 30 ℃,the detection wavelength was set at 283 nm and the injection volume was 2μl. Results:The 3 constituents showed a good linear relationship within the range of 4. 707-28. 242 μg·ml-1(r=0. 9994) for hes-peridin, 5. 085-30. 510 μg·ml-1(r=0. 9997) for magnolol and 10. 651-63. 908 μg·ml-1(r=0. 9995) for honokiol. The average recovery was 101. 2%,104. 8% and 99. 4% with the RSDs of 1. 11%,1. 68% and 1. 49% (n=6), respectively. Conclusion: The experiment provides a simple and effective method that can be used to evaluate the quality of Xiaoji Huachong powder.