Punicalagin inhibits hepatic lipid deposition in obese mice via AMPK/ACC pathway / 中国中药杂志

Hepatic lipid deposition is one of the basic manifestations of obesity, and nowadays pharmacological treatment is the most important tool. Punicalagin(PU), a polyphenol derived from pomegranate peel, is a potential anti-obesity substance. In this study, 60 C57BL/6J mice were randomly divided into a normal group and a model group. After establishing a model of simple obesity with a high-fat diet for 12 weeks, the successfully established rat models of obesity were then regrouped into a model group, an orlistat group, a PU low-dose group, a PU medium-dose group, and a PU high-dose group. The normal group was kept on routine diet and other groups continued to feed the high-fat diet. The body weight and food intake were measured and recorded weekly. After 8 weeks, the levels of the four lipids in the serum of each group of mice were determined by an automatic biochemical instrument. Oral glucose tole-rance and intraperitoneal insulin sensitivity were tested. Hemoxylin-eosin(HE) staining was applied to observe the hepatic and adipose tissues. The mRNA expression levels of peroxisome proliferators-activated receptor γ(PPARγ) and C/EBPα were determined by real-time quantitative polymerase chain reaction(Q-PCR), and the mRNA and protein expression levels of adenosine 5'-monophosphate-activated protein kinase(AMPK), anterior cingulate cortex(ACC), and carnitine palmitoyltransferase 1A(CPT1A) were determined by Western blot. Finally, the body mass, Lee's index, serum total glyceride(TG), serum total cholesterol(TC), and low-density lipoprotein cholesterol(LDL-C) levels were significantly higher and high-density lipoprotein cholesterol(HDL-C) levels were significantly lower in the model group as compared with the normal group. The fat deposition in the liver was significantly increased. The mRNA expression levels of hepatic PPARγ and C/EBPα and the protein expression level of ACC were increased, while the mRNA and protein expression levels of CPT-1α(CPT1A) and AMPK were decreased. After PU treatment, the above indexes of obese mice were reversed. In conclusion, PU can decrease the body weight of obese mice and control their food intake. It also plays a role in the regulation of lipid metabolism and glycometabolism metabolism, which can significantly improve hepatic fat deposition. Mechanistically, PU may regulate liver lipid deposition in obese mice by down-regulating lipid synthesis and up-regulating lipolysis through activation of the AMPK/ACC pathway.

Two new isoquinoline alkaloids from Corydalis hendersonii / 中国中药杂志

Corydalis hendersonii(CH) is a Tibetan folk medicine with the functions of clearing heat, detoxifying, cooling blood, checking diarrhea, and lowering blood pressure. It is often used to treat high altitude polycythemia, vasculitis, peptic ulcer, and diarrhea. Nine compounds were separated from the ethanol extract of CH by silica gel, ODS, Sephadex LH-20 chromatography and semi-preparative HPLC. Their structures were identified as hendersine H(1),hendersine I(2), dehydrocheilanthifoline(3), protopine(4), izmirine(5), 6,7-methylenedioxy-1(2H)-isoquinolinone(6), icariside D_2(7), ethyl 4-(β-D-glucopyranosyloxy)-3-methoxybenzoate(8), 3-hydroxy-4-methoxybenzoic acid(9), respectively, by the spectroscopic data analysis and comparison with those in the literature. Among them, compounds 1 and 2 are new isoquinoline alkaloids, and compounds 7-9 are reported the first time for Corydalis. The hypoglycemic model of H9c2 cardiomyocytes and the inflammatory model of H9c2 cardiomyocytes induced by conditional supernatant were employed to determine the activities of the above compounds. The results showed that 20 μmol·L~(-1) compound 1 had a protective effect on H9c2 cardiomyocytes and 10 μmol·L~(-1) compounds 4 and 5 inhibited H9c2 cardiomyocyte inflammation induced by conditional supernatant.

Research progress on in vitro models of cardiomyocyte injury / 中国中药杂志

Cardiovascular diseases seriously endanger human health and life. The accompanying myocardial injury has been a focus of attention in society. Chinese medicine,serving as a natural and precious reservoir for the research and development of new drugs,is advantageous in resisting myocardial injury due to its multi-component,multi-pathway,and multi-target characteristics. In recent years,with the extensive application of culture method for isolated cardiomyocytes,a cost-effective,controllable in vitro model of cardiomyocyte injury with uniform samples is becoming a key tool for mechanism research on cardiomyocyte injury and drug development.A good in vitro model can reduce experimental and manpower cost,and also accurately stimulate clinical changes to reveal the mechanism. Therefore,the selection and establishment of in vitro model are crucial for the in-depth research. This study summarized the modeling principles,evaluation indicators,and application of more than ten models reflecting different clinical conditions,such as injuries induced by hypoxia-reoxygenation,hypertrophy,oxidative stress,inflammation,internal environmental disturbance,and toxicity. Furthermore,we analyzed advantages and technical difficulties,aiming to provide a reference for in-depth research on myocardial injury mechanism and drug development.

Network pharmacology study of Tibetan medicine Corydalis Herba against acute myocardial ischemia / 中国中药杂志

In this study, the compound search was completed through SciFinder and CNKI databases, and the drug-like properties were screened in FAFdrugs4 and SEA Search Server databases. In addition, based on the target sets related to acute myocardial ischemia(AMI) searched in disease target databases such as OMIM database, GeneCards database and DrugBank, a network diagram of chemical component-target-pathway-disease was established via Cytoscape to predict the potential active components of Corydalis Herba, a traditional Tibetan herbal medicine which derived from the aerial parts of Corydalis hendersonii and C. mucronifera against AMI. A protein-protein interaction(PPI) network was constructed through the STRING database and the core targets in the network were predicted. And the enrichment analyses of core targets were completed by DAVID database and R software. Furthermore, a molecular docking method was used to verify the binding of the components with core targets using softwares such as Autodock Vina. The present results showed that there were 60 compounds related to AMI in Corydalis Herba, involving 73 potential targets. The GO functional enrichment analysis obtained 282 biological processes(BP), 49 cell components(CC) and 78 molecular functions(MF). KEGG was enriched into 85 pathways, including alcoholism pathway, endocrine resistance pathway, calcium signaling pathway, cAMP signaling pathway, vascular endothelial growth factor signaling pathway and adrenergic signaling transduction pathway of myocardial cells. The results of network topology analysis showed that the key components of anti-AMI of Corydalis Herba might be tetrahydropalmatine, etrahydrocolumbamine, N-trans-feruloyloctopamine, N-cis-p-coumaroyloctopamine, N-trans-p-coumaroylnoradrenline and N-trans-p-coumaroyloctopamine, and their core targets might be CDH23, SCN4 B and NFASC. The results of molecular docking showed that the key components of Corydalis Herba had stable binding activity with the core targets. This study provides reference for further elucidation of the pharmacological effects of Corydalis Herba against AMI, subsequent clinical application, and development.

Research Process on Pharmacological Effects and Clinical Applications of Commonly Used Medicinal Plants of Genus Ilex / 中国实验方剂学杂志

Four commonly used medicinal plants of genus Ilex, including I. pubescens, I. asprella, I. rotunda, and I. latifolia, have been extensively used in clinic. The Ilex plants contain triterpenes and their glycosides, flavones, phenols and other compositions, and their have the pharmacological activities of anti-inflammatory, antibacterial, antithrombosis, cardiovascular and cerebrovascular protection, etc. Among them, I. pubescens has significant pharmacological activities in cardiovascular and cerebrovascular diseases, but there are few studies on clinical application. There are a few literature reports on the anti-inflammatory, lowering blood lipids, anti-oxidation, anti-bacterial and anti-viral activities of I. asprella, which is clinically used in the treatment of upper respiratory diseases and infectious diseases. I. rotunda has strong activities of antithrombosis and anti-inflammatory, it is clinically used for the treatment of chronic pelvic inflammatory disease. I. latifolia shows activities of hypolipidemic, antitumor, antibacterial and antioxidant, and its leaves are often used in the treatment of hypertension. This review summarized the research progress on the pharmacological effects and clinical applications of commonly used medicinal plants of this genus in recent years, in order to provide basis for their clinical applications, and provide useful reference for the further development of the research direction and the development of medicines and health products.

Chemical and pharmacological progress on a Tibetan folk medicine formula Bawei Chenxiang Powder / 中国中药杂志

Bawei Chenxiang Powder is a traditional Tibetan folk medicine formula, consisting of resinous wood of Aquilaria sinensis, kernel of Myristica fragrans, fruit of Choerospondias axillaris, travertine, resin of Boswellia carterii or B. bhaw-dajiana, stem of Aucklandia lappa, fruit of Terminalia chebula(roasted), and flower of Gossampinus malabarica. It has the function of clearing heart heat, nourishing heart, tranquilizing mind, and inducing resuscitation, which has been used for the treatment of coronary heart disease and angina pectoris. Modern research shows that the medicine materials of this formula mainly contain terpenoids like sesquiterpenes and triterpenes and polyphenols like flavonoids, lignans, and tannins, displaying some pharmacological activities such as anti-myocardial ischemia, anti-cerebral ischemia, and spatial learning and memory promotion. This review summaries the traditional uses, chemical constituents, and pharmacological activities research progress, hopefully to provide a reference for clarification of its pharmacological active ingredients.

Advances on anti-tumor mechanisms of zerumbone / 中国中药杂志

Zerumbone(ZER), one of humulane-type sesquiterpenoids, showed its unique advantage against tumor activities. The main underlying mechanisms include inhibiting the growth and proliferation of cancer cells, inducing apoptosis of cancer cells and differentiation of cancer cells, regulating immune function, inhibiting invasion and metastasis of cancer cells, and reversing multidrug resistance of cancer cells. Studies on ZER focusing its cytotoxic or anti-tumor is one of hot topic. Currently, with the increasing studies on ZER, the clarified mechanisms are getting rich. The present paper describes a summary of its anti-tumor mechanism of action and helps to provide significant reference to more in-depth research.

Research progress on terpenes and pharmacological effects of Saussurea lappa / 中国中药杂志

Saussurea lappa originates in India, and now mainly grow in Yunnan, Sichuan and other places in China. It is one of the commonly used traditional herbal medicines in Tibet and other minority regions, with effects in regulating qi to relieve pain and invigo-rating spleen to promote food. It has been used in clinic for gastrointestinal diseases, such as Qi stagnation syndrome of spleen and stomach, diarrhea and tenesmus. More than 200 compounds have been identified from S. lappa. Among them, sesquiterpenoids attracted much attention. In terms of the number of compounds, eudesmanetype is dominant, guaiane and germacranetypes have also been reported frequently. Pharmacological studies have involved extracts, volatile oils and monomeric components represented by dehydrocostus lactone. Anti-tumor, anti-inflammatory and anti-bacterial effects on digestive system have attracted great attention. However, due to the complex sources of S. lappa and widely used in clinical practice, there is few research progress on relevant chemical constituents and pharmacological activities. This paper systematically summarizes terpenes and the pharmacological effects of S. lappa, in order to provide basis for further studies and clinical applications.

Seroepidemiology of varicella among the healthy population aged 1-19 years in Harbin, China / 中国当代儿科杂志

OBJECTIVE@#To investigate the level of IgG antibody to varicella in the healthy population aged 1-19 years in Harbin, China.@*METHODS@#Random sampling was performed to select 1 203 healthy individuals aged 1-19 years in Harbin. According to age, they were divided into ≥1 years group (n=240), ≥4 years group (n=396), ≥7 years group (n=364) and 14-19 years group (n=203). Enzyme-linked immunosorbent assay was used to measure the concentration of varicella-zoster virus (VZV)-IgG antibody in serum, and a concentration of VZV-IgG antibody of ≥100 mIU/mL was considered positive, suggesting that the subject had the ability to resist VZV infection.@*RESULTS@#The overall positive rate of VZV-IgG antibody was 71.49% (860/1 203), and the concentration of VZV-IgG antibody was 447±17 mIU/mL. The concentration of VZV-IgG antibody tended to increase with age (P<0.05). The positive rate of VZV-IgG antibody in the urban population was significantly higher than that in the rural population (P<0.05). There was significant difference in the positive rate of VZV-IgG antibody between the populations with different doses of varicella vaccination (P<0.05), and the population with 2 doses of vaccination had the highest positive rate of VZV-IgG antibody. There was a significant difference in the concentration of VZV-IgG antibody between the populations with different medical histories (P<0.05), and the population with a past history of varicella had the highest concentration.@*CONCLUSIONS@#Among the healthy population aged 1-19 years in Harbin, there is a significant difference in the level of VZV-IgG antibody between the urban and rural populations, as well as between different age groups. Varicella vaccination should be strengthened in areas with a low vaccination rate and the population aged <14 years.

Anti-inflammatory Effect of Chinese Agarwood Essential Oil Via Inhibiting p-STAT3 and IL-1β/IL-6 / 中国药学杂志

OBJECTIVE: Eaglewood is a commonly used precious herbal medicine. Due to the multiple drug effects and shortage of medicinal resources, it is currently a hot research topic. Chinese agarwood essential oil (CEEO) is the main active ingredient of eaglewood. To investigate the anti-inflammatory effect and mechanism of CEEO. METHODS: The anti-inflammatory effect of CEEO was evaluated on xylene-induced ear edema in mice and carrageenan-induced paw swelling in rats. The production and transcription levels of pro-inflammatory cytokines IL-1β and IL-6 were detected by ELISA or quantitative RT-PCR in LPS-activated RAW264.7 macrophages. The protein levels of p-transducer and activator of transcription 3 (STAT3) and p-IκBα/p-NF-κBp65 were detected by Western blot analysis. The chemical profiles of CEEO were identified by GC-MS. RESULTS: Intragastric administration with CEEO (60-960 mg•kg-1 in mice and 680 mg•kg-1 in rats) produced significant anti-inflammatory effect in vivo, the highest inhibition percentages were 73% and 51%, respectively (P<0.001). After treatment with CEEO (10, 5, and 2.5 μg•mL-1), ELISA and RT-PCR analysis showed that the production and mRNA level of IL-1β and IL-6 were attenuated by 68% and 39%, 64% and 52% (P<0.001), respectively, at the highest concentration. Western blot analysis showed that CEEO (680 mg•kg-1, ig) significantly restrained the phosphorylation of STAT3 by 21% (P<0.05). Totally 117 compounds were identified in CEEO by GC-MS analysis and the chemical analysis revealed that sesquiterpenoids were the major compounds (68.83%). CONCLUSION: This study shows for the first time that intragastric administration of CEEO has significant anti-inflammatory effect, which may be due to the suppression of pro-inflammatory cytokines IL-1β and IL-6 by reducing the overexpression of p-STAT3, thereby inhibiting the occurrence and development of inflammation. The anti-inflammatory effect of CEEO may be related to the primary component sesquiterpenoids.