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1.
Acta Pharmaceutica Sinica B ; (6): 2765-2777, 2023.
Article in English | WPRIM | ID: wpr-982853

ABSTRACT

Oligoasthenospermia is the primary cause of infertility. However, there are still enormous challenges in the screening of critical candidates and targets of oligoasthenospermia owing to its complex mechanism. In this study, stem cell factor (SCF), c-kit, and transient receptor potential vanilloid 1 (TRPV1) biosensors were successfully established and applied to studying apoptosis and autophagy mechanisms. Interestingly, the detection limit reached 2.787 × 10-15 g/L, and the quantitative limit reached 1.0 × 10-13 g/L. Furthermore, biosensors were used to investigate the interplay between autophagy and apoptosis. Schisandrin A is an excellent candidate to form a system with c-kit similar to SCF/c-kit with a detection constant (KD) of 5.701 × 10-11 mol/L, whereas it had no affinity for SCF. In addition, it also inhibited autophagy in oligoasthenospermia through antagonizing TRPV1 with a KD of up to 4.181 × 10-10 mol/L. In addition, in vivo and in vitro experiments were highly consistent with the biosensor. In summary, high-potency schisandrin A and two potential targets were identified, through which schisandrin A could reverse the apoptosis caused by excessive autophagy during oligoasthenospermia. Our study provides promising insights into the discovery of effective compounds and potential targets via a well-established in vitro-in vivo strategy.

2.
Article in Chinese | WPRIM | ID: wpr-1018673

ABSTRACT

Objective To investigate the preventive effect of schisandrin(SCH)on fetal neural tube defects(NTDs)of mice and its mechanism.Methods C57BL/6 mice were mated with female and male at a ratio of 2:1.Pregnant female mice with vaginal plug after mating were randomly divided into control group,model group,SCH group,and folic acid group,with 9 mice in each group.The NTDs fetal mice model was induced by intraperitoneal injection of all-trans retinoic acid(atRA)(7.5 mg/kg)on embryonic day 7.5(E 7.5 d).During E 0.5 d-E 11.5 d,pregnant rats in folic acid group were given folic acid[61.0 μg/(kg·d)]by gavage once a day,and pregnant rats in SCH group were given SCH[8.0 mg/(kg·d)]by gavage once a day.Fetal mice were removed by cesarean section on E 11.5 d.PC12 cells were divided into control group,model group and SCH group.PC12 cells were treated with atRA(20 μmol/L)for 12 hours to establish cell damage model in model group,and treated with SCH(2.5 μmol/L)for 24 hours in SCH group.Fetuses were identified NTDs by stereoscopic microscopy.HE staining was used to observe the closure of the neural tube.The expression levels of p-PI3K,Akt and p-Akt molecules in PI3K/Akt signaling pathway were detected by Western Blotting.Results Compared with control group,the incidence of NTDs was significantly increased in mice of model group(P<0.01);compared with model group,the incidence of NTDs was decreased in folic acid group and SCH group(P<0.01);compared with folic acid group,SCH group had a lower incidence of NTDs(P<0.01).Western Blotting results showed that compared with control group,the expression of p-PI3K and p-Akt protein in fetal tissues of model group was significantly decreased(P<0.01,P<0.05);compared with model group,there was no significant difference in expression of p-PI3K and p-Akt in fetal tissues of folic acid group(P>0.05),while the expression of p-PI3K and p-Akt protein in SCH group was significantly higher(P<0.05).Compared with control group,PC12 cells in model group showed lower expression levels of p-PI3K and p-Akt(P<0.05);compared with model group,PC12 cells in SCH group showed higher expression levels of p-PI3K and p-Akt(P<0.05).Conclusions SCH can reduce the incidence of atRA-induced NTDs in fetal mice,and its preventive effect is better than folic acid,which may be related to the activation of the PI3K/Akt signaling pathway.

3.
Article in Chinese | WPRIM | ID: wpr-1014679

ABSTRACT

AIM: To explore schisandrin B (Sch B) pretreatment reduces intestinal ischemia reperfusion injury (IIRI) through inhibiting apoptosis by activation of Nrf2/HO-1 signing pathway in mice by network pharmacology and in vivo experiment. METHODS: (1) The targets of Sch B and IIRI were searched from online databases, Drawing Venn diagram to obtain the common target of them. Cytoscape software was imported to construct the protein-protein interaction (PPI) network to establish the "Drugs-Disease-core target gene" network. The mechanism of Sch B against IIRI was predicted through GO and KEGG enrichment analysis. (2) Thirty-six C57BL/6J mice were randomly divided into six groups (n = 6). The model of IIRI was established in four groups except the sham operation group. Three of the groups were pretreated with Sch B, Nrf2 inhibitor ML385, and Sch B + ML385, respectively. After the experiment, intestinal tissue samples were taken for HE staining, Chiu ' s score, apoptosis staining, immunohistochemistry (IHC), and immunoblotting (Western blot). RESULTS: A total of 412 Sch B related tar- gets, 2 166 IIRI related targets and 153 common targets were screened out through network pharmacology. There were 88 "Sch B-IIRI-core target gene" included NFE2L2 (Nrf2), HMOX1 (HO-1), BCL2, CASP3 (caspase 3), and so on. KEGG enrichment analysis screened 163 related pathways, apoptosis pathway ranked high showing that the pathway may play a key role in the treatment of IIRI by Sch B. The animal experiment had shown that Sch B reduced the Chiu's score and apoptotic while upregulating Nrf2, HO-1, Bcl-2 protein expression levels and Bcl-2/Bax, downregulating Bax, and cleaved caspase-3 expression levels, thereby reducing IIRI in mice, and that Nrf2 inhibitor ML385 reversed this process (P < 0.05). CONCLUSION: This study reveals that Sch B has the characteristics of multi-target and multi-pathway in the reduction of IIRI, and Sch B can reduce IIRI through inhibiting apoptosis by activation of Nrf2/ HO-1 pathway.

4.
Chin. j. integr. med ; Chin. j. integr. med;(12): 885-894, 2023.
Article in English | WPRIM | ID: wpr-1010300

ABSTRACT

OBJECTIVE@#To explore the effect and mechanism of schisandrin B (Sch B) in the treatment of cerebral ischemia in rats.@*METHODS@#The cerebral ischemia models were induced by middle cerebral artery occlusion (MCAO) and reperfusion. Sprague-Dawley rats were divided into 6 groups using a random number table, including sham, MCAO, MCAO+Sch B (50 mg/kg), MCAO+Sch B (100 mg/kg), MCAO+Sch B (100 mg/kg)+LY294002, and MCAO+Sch B (100 mg/kg)+wortmannin groups. The effects of Sch B on pathological indicators, including neurological deficit scores, cerebral infarct volume, and brain edema, were subsequently studied. Tissue apoptosis was identified by terminal transferase-mediated dUTP nick end-labeling (TUNEL) staining. The protein expressions involved in apoptosis, inflammation response and oxidative stress were examined by immunofluorescent staining, biochemical analysis and Western blot analysis, respectively. The effect of Sch B on phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) signaling was also explored.@*RESULTS@#Sch B treatment decreased neurological deficit scores, cerebral water content, and infarct volume in MCAO rats (P<0.05 or P<0.01). Neuronal nuclei and TUNEL staining indicated that Sch B also reduced apoptosis in brain tissues, as well as the Bax/Bcl-2 ratio and caspase-3 expression (P<0.01). Sch B regulated the production of myeloperoxidase, malondialdehyde, nitric oxide and superoxide dismutase, as well as the release of cytokine interleukin (IL)-1 β and IL-18, in MCAO rats (P<0.05 or P<0.01). Sch B promoted the phosphorylation of PI3K and AKT. Blocking the PI3K/AKT signaling pathway with LY294002 or wortmannin reduced the protective effect of Sch B against cerebral ischemia (P<0.05 or P<0.01).@*CONCLUSIONS@#Sch B reduced apoptosis, inflammatory response, and oxidative stress of MCAO rats by modulating the PI3K/AKT pathway. Sch B had a potential for treating cerebral ischemia.

5.
Chin. j. integr. med ; Chin. j. integr. med;(12): 594-602, 2022.
Article in English | WPRIM | ID: wpr-939784

ABSTRACT

OBJECTIVE@#To determine whether Schisandrin B (Sch B) attenuates early brain injury (EBI) in rats with subarachnoid hemorrhage (SAH).@*METHODS@#Sprague-Dawley rats were divided into sham (sham operation), SAH, SAH+vehicle, and SAH+Sch B groups using a random number table. Rats underwent SAH by endovascular perforation and received Sch B (100 mg/kg) or normal saline after 2 and 12 h of SAH. SAH grading, neurological scores, brain water content, Evan's blue extravasation, and terminal transferase-mediated dUTP nick end-labeling (TUNEL) staining were carried out 24 h after SAH. Immunofluorescent staining was performed to detect the expressions of ionized calcium binding adapter molecule 1 (Iba-1) and myeloperoxidase (MPO) in the rat brain, while the expressions of B-cell lymphoma 2 (Bcl-2), Bax, Caspase-3, nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing 3 (NLRP3), apoptosis-associated specklike protein containing the caspase-1 activator domain (ASC), Caspase-1, interleukin (IL)-1β, and IL-18 in the rat brains were detected by Western blot.@*RESULTS@#Compared with the SAH group, Sch B significantly improved the neurological function, reduced brain water content, Evan's blue content, and apoptotic cells number in the brain of rats (P<0.05 or P<0.01). Moreover, Sch B decreased SAH-induced expressions of Iba-1 and MPO (P<0.01). SAH caused the elevated expressions of Bax, Caspase-3, NLRP3, ASC, Caspase-1, IL-1β, and IL-18 in the rat brain (P<0.01), all of which were inhibited by Sch B (P<0.01). In addition, Sch B increased the Bcl-2 expression (P<0.01).@*CONCLUSION@#Sch B attenuated SAH-induced EBI, which might be associated with the inhibition of neuroinflammation, neuronal apoptosis, and the NLRP3 inflammatory signaling pathway.


Subject(s)
Animals , Rats , Apoptosis , Brain/pathology , Brain Injuries/pathology , Caspase 3/metabolism , Cyclooctanes , Evans Blue , Inflammasomes/metabolism , Interleukin-18/metabolism , Lignans , NLR Family, Pyrin Domain-Containing 3 Protein/metabolism , Polycyclic Compounds , Proto-Oncogene Proteins c-bcl-2/metabolism , Rats, Sprague-Dawley , Subarachnoid Hemorrhage/drug therapy , Water , bcl-2-Associated X Protein/metabolism
6.
Article in Chinese | WPRIM | ID: wpr-1014796

ABSTRACT

AIM: To explore the protective effect and mechanism of schisandrin B (Sch B) on myocardial ischemia-reperfusion injury (MIRI) in rats. METHODS: Forty SD rats were randomly divided into control group, MIRI group, MIRI +30 mg/kg Sch B (MIRI + L-Sch B) group and MIRI +60 mg/kg Sch B (MIRI + H-Sch B) group, ten in each group, Sch B were intragastrically for 7 days. Ligation of the left anterior descending branch was used to establish MIRI model, control group rats only underwent sham operation. The ardiac function parameters of ejection fraction (EF), fractional shortening (FS), maximum rate of increase in left ventricular pressure (+ dp/dt

7.
China Pharmacy ; (12): 1173-1180, 2021.
Article in Chinese | WPRIM | ID: wpr-876883

ABSTRACT

OBJECTIVE:To prepare paclit axel and schisandrin B liposomes modified by cell penetrating peptide RPV ,and to preliminarily evaluate its anti-tumor activity in vitro . METHODS :RPV modified paclitaxel and schisandrin B liposomes were prepared by film dispersion method. Box-Benhken design-response surface methodology was used to optimize the prescription technology of RPV modified paclitaxel and schisandrin B liposomes using the amount of cholesterol and paclitaxel ,the time interval of ultrasound probe as factors ,average entrapment efficiency of paclitaxel and schisandrin B was used as the index. The liposomes prepared by the optimal technology were characterized. Sulfonylrhodamine B staining method was used to investigate in vitro toxicity of RPV modified blank liposomes ,paclitaxel and schisandrin B liposomes ,RPV modified paclitaxel and schisandrin B liposomes to human ovarian cancer cell SK-OV- 3. The effects of 3 kinds of liposomes on the migration and invasion ability of SK-OV-3 cells were investigated by cell scratch test and Transwell chamber invasion test. RESULTS :The optimal prescription technology was phospholipid 44 mg,cholesterol 8 mg,paclitaxel 0.64 mg,schisandrin B 1.5 mg,ultrasonic probe time interval 5 s,prescription dosage 5 mL. According to the optimal prescription technology ,the liposomes were spherical in shape ,and the particle size was (126.49±1.19)nm,Zeta-potential was (-4.83±0.61)mV,average entrapment efficiency of liposomes was (93.88±1.67)%. Compared with RPV modified blank liposomes ,after treated with paclitaxel and schisandrin B liposomes and RPV modified paclitaxel and schisandrin B liposomes ,the survival rate ,migration inhibition rate and invasion rate of SK-OV- 3 cells were significantly decreased (P<0.05). The effects of RPV modified paclitaxel and schisandrin B liposomes was better than those of paclitaxel and schisandrin B liposomes (P<0.05). CONCLUSIONS :RPV modified paclitaxel and schisandra B liposome are successfu lly prepared ,and they have certain antitumor activity in vitro .

8.
Article in Chinese | WPRIM | ID: wpr-862491

ABSTRACT

Objective To improve the quality control of Dilong Shenmai oral liquid. Methods TLC was used for the qualitative identification of Astragali Radix, Ophiopogonis Radix and Schisandrae Chinensis Fructus in Dilong Shenmai oral liquid. HPLC was used to determine the contents of schisandrin and ethylparaben in the preparation. Wondasil C18 column (250 mm×4.6 mm, 5 μm) was used with acetonitrile-water as the mobile phase at the flow rate of 1.0 ml/min for gradient elution. The detection wavelength was set at 254 nm, and column temperature was 30 ℃. Results TLC spots were clear and well-separated without negative interference. The linear ranges of schisandrin and ethylparaben were 5.81−58.06 μg/ml (r=0.999 9) and 25.29−252.94 μg/ml (r=0.999 9). The average recoveries were 99.35% (RSD=1.02%) and 99.72% (RSD=0.76%). Conclusion This method is simple, quick and accurate. It can be used for effective quality control of Dilong Shenmai oral liquid.

9.
Article in Chinese | WPRIM | ID: wpr-904748

ABSTRACT

Objective To study the effects of schisandrin B (Sch B) on the apoptosis of human breast cancer MDA-MB-231 cells and its mechanism. Methods Cell counting reagent (CCK-8) was used to detect the effect of Sch B on the survival rate of MDA-MB-231 cells. MDA-MB-231 cells were treated with Sch B (10, 20, 40 μmol/L) for 24 hours. The cell death was detected by Annexin V-FITC/PI. The levels of intracellular reactive oxygen species (ROS) were detected by DCFA-DA fluorescent probe. Apoptosis and the expression of endoplasmic reticulum stress related proteins (Bcl-2、Bax、CHOP、GPR78、PERK、p-PERK、p-eIF2α、eIF2) were detected by Western blot. Results Compared with the blank group, the cell survival rate decreased significantly (P<0.01) with the increase of Sch B concentration, and its IC50 was 19.16 μmol/L. Compared with the control group, Sch B groups (10, 20, 40 μmol/L) inhibited cell clone formation in a dose-dependent manner (P<0.05). Sch B groups (10, 20, 40 μmol/L) induced apoptosis (P<0.05), significantly reduced the expression of anti-apoptotic protein Bcl-2 and significantly increased the expression of pro-apoptotic protein Bax (P<0.05). Sch B groups (10, 20, 40 μmol/L) significantly increased the level of intracellular ROS in a dose-dependent manner (P<0.05). Sch B groups (10, 20, 40 μmol/L) stimulated endoplasmic reticulum stress and increased the expressions of endoplasmic reticulum stress-related proteins CHOP, GPR78 and p-eIF2α in a dose-dependent manner (P<0.05). Conclusion Sch B induces apoptosis of MDA-MB-231 cells through ROS mediated endoplasmic reticulum stress.

10.
China Pharmacy ; (12): 1692-1697, 2021.
Article in Chinese | WPRIM | ID: wpr-882138

ABSTRACT

OBJECTIVE:To analyze the mass spectrometry fragmentation regularity of bicyclol ,bifendate and schisandrin C , and to identify the impurities of bicyclol raw material. METHODS :UHPLC-ESI-Q-TOF-MS method was adopted. Using electrospray ionization source ,in positive ion mode ,the excimer ion and characteristic fragments of bicyclol ,bifendate and schisandrin C were analyzed by means of TOF-MS. According to the mass change of fragments ,the possible fragmentation pathways were speculated ,and the fragmentation regularity were analyzed and summarized. Bicyclol raw material sample was first separated by liquid chromatography to find the impurity peaks in it ,and then the impurity peaks were analyzed by mass spectrometer;the impurity identification was conducted by combining with the fragmentation regularity. RESULTS :The 3 compounds all produced [M+H] + excimer ion in the positive ion mode. After collision-induced dissociation ,the C-O bond ,the simple rupture of the C-C bond and the ring-opening cleavage of the oxygen ring occurred ;with the loss of neutral fragments , mainly CH 2O,supplemented by CO 2,CO and CHO ,the dissociation was concentrated in the middle and high quality regions. C-C and C-O bonds of 3 compounds were simply broken only in the branched chain structure and/or oxygen ring structure ,but the structure of the biphenyl parent nucleus remained unchanged. Among them ,the bicyclol contained a benzyl alcohol structure ,so under acidic mobile phase conditions ,it would exist stably in the form of [M+H -H2O]+. Because schisandrin C contained 8-membered ring structure,ring opening first occurred under collision voltage ,and then neutral fragment loss occurred. The secondary mass spectra of impurity in bicyclol raw material were consistent with the mass spectra fragmentation of secondary fragments of bifendate. CONCLUSIONS:The study summarized mass spectrometry fragmentation regularity of 3 schisandrin derivatives. The impurity in bicyclol raw material may be bifendate.

11.
Chinese Pharmacological Bulletin ; (12): 698-702, 2020.
Article in Chinese | WPRIM | ID: wpr-856976

ABSTRACT

Aim To investigate the effects of schisandrin C on arterial inflammation and atherosclerosis of ApoE-/-mice fed with high-fat diet. Methods ApoE-/-mice were divided into high fat diet group (HFD) and high fat diet group + schisandrin group (HFD + Sch C). High fat diet and Sch C were given at the same time. After 12 weeks, mice were executed and arterial tissues were collected. RT-q PCR and Western blot were respectively used to detect the expressions of IL-6, TNF-α, ICAM-1, β-actin and the phosphorylation and expression of IκB-α in arteries. Oil red O staining and biochemical kit were respectively used to detect the lipid changes in aortic root and the blood lipid levels. Results Compared with HFD group, the area of atherosclerotic plaque in HFD + Sch C was reduced (P < 0. 05), but Sch C did not affect blood lipid levels. Compared with HFD group, the mRNA expression of TNF-α, IL-6 and ICAM-1 and the phosphorylation of IκB-α of arterial tissue in HFD + Sch Cgroup decreased (P < 0. 05). Conclusions Sch C could effectively alleviate atherosclerosis induced by high-fat diet in ApoE-/-mice, accompanied by alleviation of arterial inflammation.

12.
Article in Chinese | WPRIM | ID: wpr-845175

ABSTRACT

Objective: To establish HPLC fingerprints of Qiwei Tangmaishu tablet and simultaneously determine the contents of the six constituents, acteoside, martynoside, calycosin 7-O-β- D-glucopyranoside, schisandrin, formononetin and deoxyschizan- drin. Methods: The analysis of 50% methanol extract of this drug was performed on a 30℃ thermostatic Waters Symmetry C18 column, with the mobile phase comprising of acetonitrile(A)-0.2% formic acid solution(B)flowing at 1.0 ml/min in a gradient elution manner. The detection wavelength was set at 330 nm for acteoside and martynoside, 254 nm for calycosin 7-O-β-D-glucopyranoside, schisandrin, formononetin and deoxyschizandrin. Results: There were thirteen common peaks in the fingerprints of ten batches of samples with the similarities more than 0.9. Acteoside, martynoside, calycosin 7-O-β-D-glucopyranoside, schisandrin, formononetin and deoxyschizandrin showed good linear relationship within the ranges of 1.47-36.75, 0.66-16.50, 0.89-22.25, 2.58-64.50, 1.91-47.75 and 0.77-19.25 μg/ml(r≥0.9993), and their average recoveries were 97.57%, 99.22%, 96.69%, 100.01%, 98.79% and 96.77%, with the RSD of 0.79%, 1.54%, 0.61%, 0.64%, 0.83% and 0.36%, respectively. Conclusion: The established method is easily operable and repeatable, which could be used for quality control of Qiwei Tangmaishu tablet.

13.
Zhongcaoyao ; Zhongcaoyao;(24): 2467-2471, 2020.
Article in Chinese | WPRIM | ID: wpr-846457

ABSTRACT

Objective: To establish a method for determining the contents of schisandrin, schisandrol B, cryptotanshinone, tanshinone I and tanshinone IIA, γ-schisandrin in Zaoren Anshen Capsules (ZAC), and provide scientific method for quality control of ZAC. Methods: HPLC was used by using Thermo 120Å-C18 column, with the mobile phase consisted of acetonitrile and 0.1% acetic acid solution with gradient elution for simultaneous determination of six main index components. The detection wavelengths were set at 250 nm for schisandrin, schisandrol B, γ-schisandrin and 270 nm for cryptotanshinone, tanshinone I, and tanshinone IIA, flow rate was 1.0 mL/min, and column temperature was 30℃. Results: Schisandrin, schisandrol B, γ-schisandrin, cryptotanshinone, tanshinone I, and tanshinone IIA showed good the linear ranges relationships in the range of 4.7-3 153.6 ng (r = 0.999 9), 7.864-314.500 ng (r = 0.999 9), 14.4-1 256.9 ng (r = 0.999 9), 15.1-1 103.8 ng (r = 0.999 9), 15.3-1 532.0 ng (r = 0.999 9) and 6.134-204.500 ng (r = 0.999 9), respectively. The average recoveries were 100.4%, 98.7%, 99.4%, 100.0%, 99.3% and 100.2%, RSD were 1.4%, 2.7%, 2.2%, 2.2%, 2.5% and 2.1%, respectively. The contents of each index component in 8 batches of sample were schisandrin 1.545 7-1.909 9 mg/g, schisandrol B 0.129 8-0.235 1 mg/g, cryptotanshinone 0.508 4-0.523 4 mg/g, tanshinone I 0.111 7-0.122 3 mg/g, tanshinone IIA 0.755 8-0.874 4 mg/g, γ-schisandrin 0.120 2-0.190 1 mg/g. Conclusion: The established analytical method is highly sensitive with strong specificity and it can be used efficiently in the quality control of ZAC.

14.
China Pharmacy ; (12): 2725-2730, 2020.
Article in Chinese | WPRIM | ID: wpr-829973

ABSTRACT

OBJECTIVE:To study the pr otective effect of schisandrin A (SA)on CCl 4-induced liver fibrosis model mice and its mechanism. METHODS :Mice were randomly divided into blank control group ,model group ,silymarin group (positive control,100 mg/kg),SA low-dose and high-dose groups (20,40 mg/kg),with 10 mice in each group. Except for blank control group,other groups were given CCl 4 subcutaneously to induce liver fibrosis model. After successful modeling ,administration groups were given relevant medicine intragastrically ,once a day ,for consecutive 6 weeks;blank control group and model group were given constant volume of 0.5%sodium carboxymethyl cellulose solution intragastrically by the same way. HE staining was used to observe the pathological changes of liver tissue in mice. UV spectrophotometry and ELISA assay were adopted to detect the serum levels of liver injury indexes (ALT and AST )and the contents of inflammatory factors (TNF-α,IL-1β,IL-6). Western blotting assay was used to detect the expression of NOD like receptor protein 3(NLRP3)/NF-κB and TGF-β/Smad signaling pathway protein. RESULTS :Compared with blank control group ,obvious pathological changes of liver fibrosis were observed in model group. The serum levels of liver injury indexes and contents of inflammatory factors were significantly increased (P<0.01). The expression of NLRP 3,apoptosis associated spot-like protein ,Caspase-1 and IL- 1β,TGF-β1 and ratios ofp-NF-κB p65/NF-κB p65,p-IκBα/IκBα,p-Samd3/Smad3 were increased significantly (P<0.01). Compared with model group ,SA could significantly relieve hepatic fibrosis in mice ,reduce serum levels of liver injury indexes and contents of inflammatory factors ,as well as the expression of NLRP 3/NF-κB and TGF-β/Smad signaling pathway protein and phosphorylation level(P<0.01). CONCLUSIONS : SA can effectively relieve liver injury and inflammation of CCl 4-induced hepatic fibrosis model mice ,which may be through the regulation of NLRP 3/NF-κB and TGF-β/Smad3 signaling pathways ,thus inhibiting the process of liver fibrosis.

15.
Zhongguo Zhong Yao Za Zhi ; (24): 5177-5183, 2020.
Article in Chinese | WPRIM | ID: wpr-878803

ABSTRACT

In the current study, schisandrin B(SchB)-loaded F127 modified lipid-polymer hybrid nanoparticles(SchB-F-LPNs) were developed to improve the inhibition of breast cancer lung metastasis. Modified nanoprecipitation method was used to prepare SchB-F-LPNs. The nanoparticles were spherical in shape with shell-core structure by TEM observation. SchB-F-LPNs showed a mean particle size of(234.60±6.11) nm with zeta potential of(-5.88±0.49) mV. XRD results indicated that SchB existed in the nanoparticles in an amorphous state. The apparent permeability coefficient through porcine mucus of F-LPNs was 1.43-fold of that of LPNs as shown in the in vitro mucus penetration study. The pharmacokinetics study showed that the C_(max) of SchB was(369.06±146.94) μg·L~(-1),(1 121.34±91.65) μg·L~(-1) and(2 951.91±360.53) μg·L~(-1) respectively in SchB suspensions group, SchB-LPNs group and SchB-F-LPNs group after oral administration in rats. With SchB suspensions as the reference formulation, the relative bioavailability of SchB-F-LPNs was 568.60%. SchB-F-LPNs inhibited the morphological change during transforming growth factor-β1(TGF-β1)-induced epithelial-mesenchymal transition. In addition, SchB-F-LPNs significantly decreased the number of metastatic pulmonary nodules in 4 T1 tumor-bearing mice, suggesting that SchB-F-LPNs may inhibit the metastasis of breast cancer. These results reveal the promising potential of SchB-F-LPNs in treatment of breast cancer lung metastasis.


Subject(s)
Animals , Mice , Rats , Cyclooctanes , Lignans , Lipids , Lung Neoplasms/drug therapy , Nanoparticles , Polycyclic Compounds , Polyethylenes , Polymers , Polypropylenes , Swine
16.
Chinese Journal of Immunology ; (12): 176-180, 2019.
Article in Chinese | WPRIM | ID: wpr-744629

ABSTRACT

Objective: To evaluate the protective effect and underlying mechanism of schisandrin B ( SB) on streptozotocin ( STZ) induced-diabetic reinopathy ( DR) in rats. Methods: Following STZ injection, rats received gavage of SB for 9 months subsequently. TUNEL assay was performed for apoptosis. The levels of SOD, MDA and LDH were determined by kits. To calculate the levels of inflammatory cytokines, ELISA assay was carried out. And western blot was performed for protein levels. Results: In STZ induced-DR rats, glucose level was makedly increased. SB inhibited STZ-induced apoptosis as demonstrated by increased apoptotic body. SB significantly increased the level of SOD and decreased the levels of MDA and LDH. Meanwhile, SB notably inhibited STZ induced-inflammation by decreasing IL-6, TNF-α and IL-1β. Furthermore, SB partly abolished STZ' s effects on the expressions of VEGF, Cdc42 and pp38. Conclusion: SB attenuates STZ induced-DR via Cdc42/p38 signaling pathway.

17.
Chinese Journal of Neuromedicine ; (12): 325-330, 2019.
Article in Chinese | WPRIM | ID: wpr-1034997

ABSTRACT

Objective To investigate the effect of schisandrin (SCH) treatment on learning and memory abilities and their mechanism in APP/PS1 dual transgenic dementia mice,and explore the effect of Chinese medicine on Alzheimer's disease (AD).Methods Thirty-five APP/PS1 dementia mouse models were randomly assigned into APP/PS1 model group (n=17) and APP/PS1+SCH group (n=18);another 10 male C57BL/6J mice were chosen as blank control group.The mice in the APP/PS1+SCH group were given intragastric administration of SCH at 2.6 mg/(kg· d) for 30 d;the mice in the APP/PS1 model group and blank control group were treated with distilled water for 30 d.The learning and memory abilities of these APP/PS1 mice (n=7) were detected by Morris water maze.Mice from the three groups were sacrificed;Nissl staining was used to observe Nissl bodies of neurons in brain tissues;real-time fluorescence quantitative PCR (qPCR) was used to detect the mRNA content of terminal glycosylationend products receptor (RAGE) in brain tissues;Western blotting was used to detect the expressions of RAGE and phosphorylated P38 mitogen-activated protein kinase (p-p38) in brain tissues.Results (1) The results of water maze space exploration experiment showed that the times of crossing the platform area in the three groups were statistically significant (P<0.05);as compared with the APP/PS1 modelgroup,the times of crossing the platform area in the APP/PS1+SCH group were significantly increased (P<0.05).(2) Nissl staining results showed that the contents of Nissl bodies in the hippocampal CA1 area and cortical neurons of the APP/PS 1 model group were significantly reduced,with light staining and cell body atrophy;the lesions in mice of the APP/PS1+SCH group were less severe than those of APP/PS1 model group,some neurons were atrophic,and the content of the neuronal nileite bodies in the hippocampal CA1 region was relatively abundant.(3) The qPCR results showed that there were statistically significant differences in RAGE mRNA expression levels in the cortex and hippocampus of the three groups (P<0.05);as compared with the APP/PS1 model group,the APP/PS1+SCH group had significantly reduced RAGE mRNA expression in the hippocampal area (P<0.05).(4) Western blotting results showed that RAGE and p-p38 protein expression levels in two parts of mice of APP/PS1+SCH group were significantly reduced as compared with those in the APP/PS1 model group (P<0.05).Conclusion SCH may improve the functional status of hippocampal and cortical neurons and improve the spatial exploratory memory ability of APP/PS1 mice by down regulating the RAGE and P38 expressions.

18.
Zhongcaoyao ; Zhongcaoyao;(24): 1947-1951, 2019.
Article in Chinese | WPRIM | ID: wpr-851204

ABSTRACT

Objective: To establish an HPLC method for the simultaneous content determination of seven constituents in Compound Yi’anning Pills (CYP). Methods: The determination was performed on Shim-pack GIST C18 column with mobile phase consisted of acetonitrile-0.1% phosphoric acid (gradient elution: 0-5 min, 5% acetonitrile; 5-12 min, 5%-12% acetonitrile; 12-17 min, 12%-20% acetonitrile; 17-30 min, 20% acetonitrile; 30-36 min, 20%-50% acetonitrile; 36-45 min, 50%-80% acetonitrile; 45-70 min, 80% acetonitrile) at the flow rate of 1.0 mL/min. The detection wavelength was set at 203 nm for notoginsenoside R1, ginsenoside Rg1, and ginsenoside Rb1, 220 nm for schisantherrin A, 250 nm for schisandrin, 268 nm for salvianolic acid B, and 270 nm for tanshinone IIA. The column temperature was set at 35 ℃ and the injection volume was 10 μL. Results: The linear range of detection concentration was 0.015-0.150 mg/mL for notoginsenoside R1, 0.077-0.766 mg/mL for schisandrin, 0.006-0.062 mg/mL for salvianolic acid B, 0.009-0.092 mg/mL for buddleodide, 0.050-0.503 mg/mL for ginsenoside Rg1, 0.067-0.670 mg/mL for ginsenoside Rb1, and 0.011-0.108 mg/mL for tanshinone IIA. Average recoveries respectively were 99.5%, 99.8%, 99.2%, 98.9%, 96.9%, 98.8%, and 97.1%. Conclusion: The method is simple, effective, and accurate, which can be used for simultaneous determination of seven active constituents in CYP.

19.
Chinese Pharmacological Bulletin ; (12): 833-839, 2019.
Article in Chinese | WPRIM | ID: wpr-857235

ABSTRACT

Aim: To evaluate the mouse model of hypertriglyceridemia (hTG) induced by schisandrin B (Sch B) using lipid metabolomics technology. Methods: Male ICR mice weighing 23 ~ 27 g were randomly divided into four groups: (1) mice fed with normal diet (ND group) (2) mice fed with ND and treated with Sch B(ND +Sch B group); (3) mice fed with high fat/fructose diet(HFFD group; fat, 10%; fructose, 10%; w/w), and (4) mice fed with HFFD and treated with Sch B (HFFD + Sch B group). Based on our previous research, Sch B at a single dose of 2 g · kg-1 was orally administered to the animals in the current study. Forty-eight hours later, serum samples were obtained from the orbital vein. Serum triglyceride (TG) and total cholesterol (TC) were analyzed by biochemical method. The metabolic fingerprint spectrum of serum in all groups were obtained and analyzed using ultra-performance liquid chromatography quadrupole-time-of-flight mass spectrometry (UPLC-Q/TOF-MS) method. The differences of metabolic spectra in every two groups were compared via the multivariate statistical methods. Results: Compared with ND group, three kinds (27 markers) of differential metabolites were identified in ND +Sch B group, including 18 TG, 7 phosphatidylcholine (PC), and 2 phosphatidylethano-lamine(PE). Compared with ND group, five kinds(27 markers) of differential metabolites were screened in HFFD group, including 6 sphingomyelin (SM), 13 PC, 2 cholesteryl ester(CE), 5 TG and 1 phosphati-dylinositol (PI). Compared with HFFD group, four kinds (25 markers) of differential metabolites were found in HFFD + Sch B group, involving 14 TG, 1 CE, 6 PC and 4 PE. Conclusion: These findings suggest that the animal model of hypertriglyceridemia established by Sch B involves the alteration of serum lipid metabolomics.

20.
China Pharmacist ; (12): 973-976, 2018.
Article in Chinese | WPRIM | ID: wpr-705641

ABSTRACT

Objective: To assess the anti-inflammatory and immunomodulatory activities of schisandrin B in mice. Methods: Kun-ming mice were randomly divided into 6 groups: the blank control group, the model control group, the positive control group( dexam-ethasone hydrochloride 5 mg·kg-1,levamisole hydrochloride 30 mg·kg-1), schisandrin B low (100 mg·kg-1), medium (200 mg ·kg-1) and high (400 mg·kg-1) dose groups. The inflammatory mice were induced by xylene and the immunosuppressed mice were induced by cyclophosphamide. The ear edema experiment, carbon clearance experiment and serum hemolysin experiment were per-formed with the swelling rate, swelling inhibition rate, carbon clearance index, phagocytic index, half hemolytic value, spleen index and thymus index as the investigation factors. Results: High dose and medium dose schisandrin B groups had significant inhibitory effect on mice ear edema when compared with the model control group(P<0. 05);There were significant differences between the high dose group and the positive group and there were significant differences in clearance index and phayxyitc index between high dose group and low dose group(P<0. 05), and high dose schisandrin B group had increased clearance index and phagocytic index in low immune function mice when compared with the model control group (P<0.05). Schisandrin B significantly increased HC50in low immune function mice when compared with the model control group (P<0. 01). Schisandrin B significantly increased the spleen index and thy-mus index in low immune function mice when compared with the model control group ( P<0. 01,and in a dose-dependent manner. Conclusion: Schisandrin B has significant anti-inflammatory and immune function enhancing effects.

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