1.Effects and mechanism of galangin on hepatocyte apoptosis in rats with obstructive jaundice
Lin ZHAO ; Zuowu XI ; Shasha XU ; Xubiao PAN ; Weisheng GUO
China Pharmacy 2024;35(18):2246-2251
OBJECTIVE To investigate the effects and mechanism of galangin (GAL) on hepatocyte apoptosis in rats with obstructive jaundice (OJ) based on the Janus kinase 2 (JAK2)/signal transduction and activator of transcription 3 (STAT3) signaling pathway. METHODS Taking male SD rats as the object, the OJ model was established by double ligation of common bile duct, and 48 rats with successful modeling were randomly separated into OJ model group (model group), low-dose GAL group (GAL-L group), high-dose GAL group (GAL-H group) and high-dose GAL+JAK2 activator colivelin group (GAL-H+ colivelin group), with 12 rats in each group; another 12 SD rats with laparotomy/abdominal closure without ligation were selected as sham operation group (sham group). Each administration group was given relevant medicine intragastrically and/or intraperitoneally, once a day, for 7 consecutive days. After the last medication, the morphology of liver tissue in rats was observed; the serum levels of total bilirubin (TBIL), direct bilirubin (DBIL), alanine transaminase (ALT) and γ -glutamyltransferase (GGT), as well as the levels of superoxide dismutase (SOD) and malondialdehyde (MDA) in mail:guoweishengjcy@126.com liver tissue were detected. The apoptotic rate of liver tissue cells, the expression levels of signaling pathway-related proteins (phosphorylated JAK2, JAK2, phosphorylated STAT3, STAT3) and apoptosis-related proteins [B cell lymphoma 2 (Bcl-2), Bcl-2 related X protein (Bax)] were determined. RESULTS Compared with sham group, congestion of liver sinusoids, damage to liver lobules, disordered arrangement and swollen morphology of liver cells, the disappearance of nucleoli, and significant infiltration of inflammatory cells and fibrous tissue proliferation were observed in model group; the serum levels of TBIL, DBIL, ALT and GGT, the level of MDA in liver tissue, the apoptosis rate of liver cells, the protein expression of Bax, and the protein phosphorylation levels of JAK2 and STAT3 in liver tissue of model group were increased significantly (P<0.05); the level of SOD and the protein expression of Bcl-2 in liver tissue were decreased significantly (P<0.05). Compared with the model group, the pathological injuries of liver tissue were relieved in GAL-L group and GAL-H group, all quantitative indicators had significantly improved, and the effect of GAL-H group was more significant (P< 0.05). Colivelin could significantly reverse the improvement effects of GAL on liver injury and related indicators of OJ rats (P< 0.05). CONCLUSIONS GAL may inhibit liver cell apoptosis in OJ rats, improve liver function and alleviate oxidant stress, the mechanism of which may be associated with inhibiting JAK2/STAT3 signaling pathway.
2.2,3-Seco and 3-nor guaianolides fromAchillea alpina with antidiabetic activity.
Guimin XUE ; Chenguang ZHAO ; Jinfeng XUE ; Jiangjing DUAN ; Hao PAN ; Xuan ZHAO ; Zhikang YANG ; Hui CHEN ; Yanjun SUN ; Weisheng FENG
Chinese Journal of Natural Medicines (English Ed.) 2023;21(8):610-618
In this study, we presented the isolation and characterization of eight novel seco-guaianolide sesquiterpenoids (1-8) and two known guaianolide derivatives (9 and 10), from the aerial part of Achillea alpina L.. Compounds 1-3 were identified as guaianolides bearing an oxygen insertion at the 2, 3 position, while compounds 4-8 belonged to a group of special 3-nor guaianolide sesquiterpenoids. The structural elucidation of 1-8, including their absolute configurations, were accomplished by a combination of spectroscopic data analysis and quantum electronic circular dichroism (ECD) calculations. To evaluate the potential antidiabetic activity of compounds 1-10, we investigated their effects on glucose consumption in palmitic acid (PA)-mediated HepG2-insulin resistance (IR) cells. Among the tested compounds, compound 7 demonstrated the most pronounced ability to reverse IR. Moreover, a mechanistic investigation revealed that compound 7 exerted its antidiabetic effect by reducing the production of the pro-inflammatory cytokine IL-1β, which was achieved through the suppression of the NLRP3 pathway.
Humans
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Hypoglycemic Agents/pharmacology*
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Circular Dichroism
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Cytokines
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Glucose
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Hep G2 Cells
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Insulin Resistance
3.Establishment of the fingerprint of Cnidium monnieri and a method for the content determination of 4 kinds of coumarins
Xiaojun PAN ; Weisheng LYU ; Wenhui YANG ; Yuqin LUO ; Yueyi LIANG ; Mei WEI ; Dongmei SUN ; Xiangdong CHEN ; Wenjie HUO ; Zhenyu LI
China Pharmacy 2022;33(2):185-190
OBJECTIVE To establi sh the fingerprint of Cnidium monnieri and a method for the content determination of 4 kinds of coumarins. METHODS Ultra-high performance liquid chromatography (UPLC) method was adopted to establish the fingerprints of 21 batches of C. monnieri ; their similarities were evaluated with Similarity Evaluation System of TCM Chromatographic Fingerprint (2012 edition);common peaks were identification by comparison with reference substance. Using 10 common peak areas as variables ,cluster analysis was performed for 21 batches of C. monnieri by the method of between groups. The relative correction factors of xanthotoxin ,bergapten and imperatorin were calculated by the same UPLC method with osthole as the internal reference. The contents of them were calculated by quantitative analysis of multi-components by single marker (QAMS),and compared with the results of external standard method. RESULTS Totally 10 common peaks were identified in the fingerprints of 21 batches of C. monnieri ;the similarities ranged from 0.997 to 1.000. Peak 4 was identified as xanthotoxin ,peak 8 as bergapten ,peak 9 as imperatorin and peak 10 as osthole. A total of 21 batches of samples were divided into 3 categories,of which S 7 was clustered into one category ,S14 was clustered into one category ,and the other 19 batches were clustered into one category. The relative deviations of the contents of xanthotoxin ,bergapten and imperatorin determined by QAMS and external standard method were in the range of 0.88% -1.07% ,2.22% -2.29% ,0.67% -2.93% ,respectively. CONCLUSIONS UPLC fingerprint of C. monnieri is successfully established ,and QAMS method for content determination of 4 coumarins is also established.
4.Expert Consensus for Thermal Ablation of Pulmonary Subsolid Nodules (2021 Edition).
Xin YE ; Weijun FAN ; Zhongmin WANG ; Junjie WANG ; Hui WANG ; Jun WANG ; Chuntang WANG ; Lizhi NIU ; Yong FANG ; Shanzhi GU ; Hui TIAN ; Baodong LIU ; Lou ZHONG ; Yiping ZHUANG ; Jiachang CHI ; Xichao SUN ; Nuo YANG ; Zhigang WEI ; Xiao LI ; Xiaoguang LI ; Yuliang LI ; Chunhai LI ; Yan LI ; Xia YANG ; Wuwei YANG ; Po YANG ; Zhengqiang YANG ; Yueyong XIAO ; Xiaoming SONG ; Kaixian ZHANG ; Shilin CHEN ; Weisheng CHEN ; Zhengyu LIN ; Dianjie LIN ; Zhiqiang MENG ; Xiaojing ZHAO ; Kaiwen HU ; Chen LIU ; Cheng LIU ; Chundong GU ; Dong XU ; Yong HUANG ; Guanghui HUANG ; Zhongmin PENG ; Liang DONG ; Lei JIANG ; Yue HAN ; Qingshi ZENG ; Yong JIN ; Guangyan LEI ; Bo ZHAI ; Hailiang LI ; Jie PAN
Chinese Journal of Lung Cancer 2021;24(5):305-322
"The Expert Group on Tumor Ablation Therapy of Chinese Medical Doctor Association, The Tumor Ablation Committee of Chinese College of Interventionalists, The Society of Tumor Ablation Therapy of Chinese Anti-Cancer Association and The Ablation Expert Committee of the Chinese Society of Clinical Oncology" have organized multidisciplinary experts to formulate the consensus for thermal ablation of pulmonary subsolid nodules or ground-glass nodule (GGN). The expert consensus reviews current literatures and provides clinical practices for thermal ablation of GGN. The main contents include: (1) clinical evaluation of GGN, (2) procedures, indications, contraindications, outcomes evaluation and related complications of thermal ablation for GGN and (3) future development directions.
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5.Quality Evaluation of Polygonum cuspidatum by UPLC Fingerprint and QAMS
Hui LIANG ; Xiaojun PAN ; Wenhui YANG ; Weisheng LYU ; Yuqin LUO ; Jiaxuan WU ; Mei WEI ; Xueren CHENG ; Xiaoyong LAN ; Zhenyu LI
China Pharmacy 2021;32(15):1842-1848
OBJECTIVE:To establish the UPLC fingerprint of Polygonum cuspidatum ,and to determine the contents of four active ingredients and to provide reference for the quality evaluation of P. cuspidatum . METHODS :The determination was performed on Waters BEH C 18 column(100 mm×2.1 mm,1.7 μm)with mobile phase consisted of acetonitrile- 0.2% formic acid (gradient elution )at flow rate of 0.4 mL/min. The column temperature was 40 ℃,and detection wavelength was 290 nm. The sample size was 1 μL. The fingerprints were evaluated by similarity calculation,cluster analysis and orthogonal partial least square discriminant analysis (OPLS-DA). Using polydatin as internal standard ,relative calibration factors of resveratrol ,emodin-8-O- β-D-glucoside and emodin were determined to develop a method of QAMS. The contents of 4 above components in 15 batches of P. cuspidatum were calculated by relative calibration factors. The results of QAMS were compared with those of external standard. RESULTS:UPLC fingerprints of 15 batches of P. cuspidatum were established ,and 12 common peaks were confirmed. Five components were identified ,i.e. polydatin ,resveratrol,emodin-8-O-β-D-glucoside,emodin,emodin methyl ether. The fingerprint similarity of 15 batches of P. cuspidatum was in the range of 0.865-0.976. According to cluster analysis ,15 batches of P. cuspidatum were classified into 4 categories,showing certain regularity of origin. Seven markers were identified by OPLS-DA method. The order of difference significance was peak 7>emodin-8-O-β-D-glucoside>resveratrol>peak 8>polydatin>peak 1> peak 10. The relative deviation among the contents of resveratrol ,emodin-8-O-β-D-glucoside and emodin in 15 batches of P. cuspidatum determined by QAMS and external standard method was less than 5.0%,indicating that there was no significant difference between the two methods. CONCLUSIONS :UPLC fingerprint combined with QAMS method is convenient and reliable for the quality evaluation of P. cuspidatum ;the quality of P. cuspidatum produced in Chongqing and Anhui province is better.
6.Fingerprint Establishment of Rhizoma Ligustici from Different Origins and Their Chemometrics Analysis
Hui LIANG ; Xiaojun PAN ; Weisheng LYU ; Wenhui YANG ; Yuqin LUO ; Liye PAN ; Wenjie HUO ; Zhenyu LI
China Pharmacy 2021;32(19):2358-2362
OBJECTIVE:To establish UPLC fingerpri nt of Ligusticum sinense ,Ligusticum jeholense and Conioselinum vaginatium,and to conduct their chemometrics analysis so as to provide reference for the identification of Rhizoma Ligustici from different origins. METHODS :UPLC method combined with Similarity Evaluation System of TCM Chromatographic Fingerprints (2012 edition) were used to establish the fingerprints of Rhizoma Ligustici from different origins. Chromatographic peak identification and similarity evaluation were carried out. Cluster analysis (CA),principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA)were performed to analyze Rhizoma Ligustici from different origins,and screen differential components. RESULTS :Totally 13,11,11 characteristic peaks were identified in UPLC fingerprints of L. sinense ,L. jeholense and C. vaginatium ,respectively. Similarity evaluation showed that the similarity between C. vaginatium and L. jeholense were 0.312-0.541;that between C. vaginatium and L. sinense were 0.324-0.682;that between L. sinense and L. jeholense were 0.312-0.671,indicating there was great difference among Rhizoma Ligustici from different origins. CA,PCA and OPLS-DA showed that Rhizoma Ligustici from different origins were clustered into each category respectively ; chemical components represented by peak 10,peak 13,peak 12,peak 7 and peak 6 were differential components for Rhizoma Ligustici from 3 origins. CONCLUSIONS :The study establishes UPLC fingerprint of Rhizoma Ligustici from different origins , and screens 5 differential components ,which can be used to identify Rhizoma Ligustici from different origins.
7.Variations of Chemical Components in Inula japonica by UPLC-MS/MS before and after Honey-frying
Weisheng LYU ; Cuijie WEI ; Xiaojun PAN ; Wenhui YANG ; Minyou HE ; Xiangdong CHEN ; Dongmei SUN ; Mei WEI ; Zhenyu LI
China Pharmacy 2021;32(20):2478-2484
OBJECTIVE:To compare the c hemical components differences of Inula japonica before and after honey-frying. METHODS:UPLC-MS/MS method was adopted. The determination was performed on Waters ACQUITY UPLC BEH C 18 column with mobile phase consisted of 0.1% formic acid-acetonitrile (gradient elution )at the flow rate of 0.3 mL/min. The column temperature was set at 30 ℃,and sample size was 5 µL. The electrospray ion source was scanned by positive ion mode. The first order mass spectrometry scanning range was m/z 70-1 050,the second order mass spectrometry scanning range was m/z 50-1 050, and the normalized collision energy was 40,60 eV ;mass spectrum type was the peak figure ,the flow rate of sheath gas was 35 arb,the auxiliary airflow speed was 10 arb,the spray voltage was 3.80 kV,the S-lens voltage was 50 V,the heating temperature was 350 ℃,and the capillary temperature was 350 ℃. The components were identified by Qual Browser 4.1.39.1 software, referring to the online high-resolution database mzCloud and local database OTCML of high-resolution mass spectrometry of TCM , and combined with relevant literature. The principal component analysis (PCA)and orthogonal partial least squared-discriminant analysis(OPLS-DA)of I. japonica before and after honey-fried were performed by using SIMCA 14.1 statistical software ,and variable importance projection (VIP)value greater than 1 was used as the standard to screen the differential components before and after honey-frying. RESULTS :A total of 29 common chemical components were identified from I. japonica and honey-fried I. japonica,including 5 phenolic acids as 1-caffeoylquinic acid ,chlorogenic acid and 3,5-dicaffeoylquinic acid ,12 flavonoids as quercetin,luteolin and evamectin ,as well as 12 sesquiterpene lactones as 1-O-acetylinula diester ,inula bicolor lactone B and 1-O-acetyl-6-O-isobutyryl inulin. The results of PCA showed that I. japonica and honey-fried I. japonica were located on both sides of the score diagram respectively. The results of OPLS-DA showed that the VIP values of 7 components were greater than 1,which were peak 19(britanin),peak 6(quercetagitrin),peak 1(1-caffeoylquinic acid ),peak 21(vitexicarpin),peak 20(tomentosin), peak 13(spinacetin)and peak 3(daphnetin). CONCLUSIONS :After honey-fried ,the content of chemical components of I. japonica changed and decreased to a certain extent. Britanin ,quercetagitrin,1-caffeoylquinic acid ,tomentosin,vitexicarpin, spinacetin and daphnetin may be the differential components of I. japonica and honey-fried I. japonica .
8.Study on Essential Oil in the Seeds ofDescurainia Sophia (L.) Webb ex Prantl by GC-MS Analysis
Jianhong GONG ; Yanli ZHANG ; Weisheng FENG ; Haixu KUANG ; Xiaoke ZHENG ; Mengke DONG ; Bei PAN
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(9):1942-1945
The analysis of essential oil in seeds ofDeseurainia sophia provided an experimental basis for further research on essential oil activity test at the first time. Essential oil was extracted by steam distillation method. Analysis and identification were made by gas chromatography-mass spectrometry (GC-MS) technology in combination with retention indices. A total of 33 components in seeds ofD. sophia were detected by GC-MS and 28 compounds were identified by MS in combination with Kovats retention index. The compounds with high contents were as follows: 3-methylene-nonane (68.14%), 1,3-diazine (29.32%), 2-n-butylacrolein (0.58%), methyl nipecotate (0.43%), 4-oxo-butanenitrile (0.31%), 8-chloro-neoisol-ongifolene (0.25%) and so on. It was concluded that 28 volatile components were identified by GC-MS combined with retention indices. The total detected components were 99.91%. This method was able to improve the accuracy of qualitative detection results.
9.Relationship between BGP with glucose and lipids metabolism in elderly men
Xiaojing CHEN ; Lu ZHOU ; Yanhong GAO ; Yongyu PAN ; Yan WANG ; Weisheng LU ; Zhihong PAN ; Shuyan CHEN
Journal of Chinese Physician 2014;(z1):11-13
Objective To study the relationship between serum osteocalcin and parameters of glucose and lipid metabolism in elderly men.Methods The bone metabolism index such as serum osteocalcin was measured by electrochemiluminescence immunoas -say in 206 old male patients , incluiding 69 patients with type 2 diabetes mellitus .The parameters of glucose and lipid metabolism were also measured and the correlation between the parameters and serum BGP were analyzed .Results Serum BGP and beta-CTx concen-trations were significantly lower in patients with type 2 diabetes than those in normal glucose tolerance group [ ( 9.57 ±4.74 )μg/L vs (13.22 ±10.35)μg/L, P <0.05;(0.25 ±0.19)μg/L vs (0.35 ±0.29)μg/L, P <0.05].Compared with the group in low level of BGP, fasting blood glucose and HbA1c were reduced in high-level-BGP group[(5.89 ±2.10)mmol/L vs (5.28 ±1.38)mmol/L, P<0.01;6.30%±1.03% vs 5.98%±0.61%, P <0.01].Triglyceride (TG) was positively correlated with serum BGP ( r =0.146, P =0.032).Stepwise multiple regression analysis showed that TG and HbA 1c were independently associated with serum BGP level(β=1.995, P <0.01;β=-1.483, P <0.05).Conclusions Serum TG and HbA1c are independent factors related to serum BGP in elderly men .
10.Correlation analyses of serum levels of homocysteine and hypersensitivity C-reactive protein in elderly patients with cerebral infarction
Huimin YUAN ; Jiangrong ZHANG ; Zhihong PAN ; Weisheng LU ; Jing CHANG
Journal of Chinese Physician 2012;14(7):901-903
Objective To observe the serum levels of homocysteine (Hcy) and hypersensitivity C-reactive protein(hs-CRP) in elderly patients with cerebral infarction and to investigate their relationship and clinical significance by National Institutes of Health Stroke Scale (NIHSS).Methods The serum levels of Hcy and hs-CRP were by enzymatic cycling method and scattering turbidimetry in the elderly patients ( 116 cases with cerebral infarction and 100 cases of healthy control).Those 116 cases with cerebral infarction were divided into three groups by the degree of NIHSS.The three groups were compared with each other.Results The levels of serum Hcy and hs-CRP in elderly patients with cerebral infarction were significantly higher than that of healthy control group ( t =6.97,P <0.01 ; t =14.96,P <0.01 ).There has significant difference among those three groups with cerebral infarction by comparing with each other( F =23.49,P <0.05; F =28.19,P <0.05).A positive correlation was found between Hcy and degree of NIHSS( r=0.54,P <0.05),and between hs-CRPand degree of NIHSS( r =0.58,P <0.05).Conclusions Serum levels of Hcy and hs-CRP are correlated with the occurrence of cerebral infarction and its severity.There has positive clinical significance to evaluate the effect of cerebral infarction by measuring the serum levels of Hcy and hs-CRP dynamic.

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