An ethanolic extract of Arctium lappa L. leaves ameliorates experimental atherosclerosis by modulating lipid metabolism and inflammatory responses through PI3K/Akt and NF-κB singnaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Atherosclerosis (AS), a lipid-induced inflammatory condition of the arteries, is a primary contributor to atherosclerotic cardiovascular diseases including stroke. Arctium lappa L. leaf (ALL), an edible and medicinal herb in China, has been documented and commonly used for treating stroke since the ancient times. However, the elucidations on its anti-AS effects and molecular mechanism remain insufficient. AIM OF THE STUDY: To investigate the AS-ameliorating effects and the underlying mechanism of action of an ethanolic extract of leaves of Arctium lappa L. (ALLE). MATERIALS AND METHODS: ALLE was reflux extracted using with 70% ethanol. An HPLC method was established to monitor the quality of ALLE. High fat diet (HFD) and vitamin D3-induced experimental AS in rats were used to determine the in vivo effects; and oxidized low-density lipoprotein-induced RAW264.7 macrophage foam cells were used for in vitro assays. Simvatatin was used as positive control. Biochemical assays were implemented to ascertain the secretions of lipids and pro-inflammatory mediators. Haematoxylin-eosin (H&E) and Oil red O stains were employed to assess histopathological alterations and lipid accumulation conditions, respectively. CCK-8 assays were used to measure cytotoxicity. Immunoblotting assay was conducted to measure protein levels. RESULTS: ALLE treatment significantly ameliorated lipid deposition and histological abnormalities of aortas and livers in AS rats; improved the imbalances of serum lipids including total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C) and high-density lipoprotein cholesterol (HDL-C); notably attenuated serum concentrations of inflammation-associated cytokines/molecules including TNF-α, IL-6, IL-1ß, VCAM-1, ICAM-1and MMP-9. Mechanistic studies demonstrated that ALLE suppressed the phosphorylation/activation of PI3K, Akt and NF-κB in AS rat aortas and in cultured foam cells. Additionally, the PI3K agonist 740Y-P notably reversed the in vitro inhibitory effects of ALLE on lipid deposition, productions of TC, TNF-α and IL-6, and protein levels of molecules of PI3K/Akt and NF-κB singnaling pathways. CONCLUSIONS: ALLE ameliorates HFD- and vitamin D3-induced experimental AS by modulating lipid metabolism and inflammatory responses, and underlying mechanisms involves inhibition of the PI3K/Akt and NF-κB singnaling pathways. The findings of this study provide scientific justifications for the traditional application of ALL in managing atherosclerotic diseases.

Cucurbitane triterpenes from Hemsleya chinensis tubers and their anti-inflammatory activities.

Six new cucurbitane-type triterpenes, hemchinins A-F (1-6), together with thirteen known ones (7-19) were isolated from ethyl acetate extraction of Hemsleya chinensis tubers. Compounds 1-2 were a group of cucurbitane triterpenes possessing an infrequent pentacyclic framework. Their structures were established by comprehensive UV, IR, HRMS, 1D/2D NMR, and ECD analyses. Bioassay results showed that most isolated compounds exhibited anti-inflammatory actions, in which compounds 13 and 15 exhibited stronger activities at 6.25 µM, with NO inhibition rates of 49.00 ± 0.05% and 48.40 ± 0.10%, respectively.

Effect of Eucommia ulmoides leaves on hyperuricemia and kidney injury induced by a high-fat/high-fructose diet in rats.

Objectives: To investigate the protective and preventive treatment effects of Eucommia ulmoides leaves on a rat model of high-fat and high-fructose diet (HFFD) induced hyperuricemia and renal injury. Materials and Methods: Network pharmacology and molecular-docking methods were used to predict the effects and action mechanisms of the major components of E. ulmoides leaves on hyperuricemia. Combining literature collection, we used SciFinder and the Traditional Chinese Medicine Systems Pharmacology Database (TCMSP) and Analysis Platform to collect E. ulmoides leaf flavonoid and iridoid components. Swiss Target Prediction, Similarity ensemble approach (SEA), GeneCards, and the Online Mendelian Inheritance in Man (OMIM) database were used to obtain core targets, and the Search Tool for Recurring Instances of Neighbouring Genes (STRING) protein database was used as core target for gene ontology enrichment Set and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses. Molecular docking was applied to predict the pathways regulating the metabolism of uric acid. The selected targets and targeting efficacy were validated using a rat model of hyperuricemia and renal injury induced by a high-fat and high-fructose diet. Results: A total of 32 chemical components with effective targets, which regulated the PI3K-AKT pathway and endocrine resistance, were collected. Molecular docking results showed that iridoids and flavonoids are bound to proteins related to inflammation and uric acid metabolism. In addition, it was verified via animal experiments that an E. ulmoides leaf extract ameliorated hyperuricemia, renal injury, and inflammation, which are closely related to the targets Interleukin- 6 (IL-6), Tumor necrosis factor-α (TNF-α), Toll-Like Receptor 4 (TLR4), and Glucose transporter 9 (GLUT9). Conclusion: E. ulmoides leaf flavonoids and iridoids ameliorate hyperuricemia and uric-acid-induced inflammation through a multi-component, multi-target, and multi-pathway mechanism, which provides a theoretical basis for the development of therapeutics from E. ulmoides leaf components.

[Short-term curative effect and safety on female abdominal obesity and defecation function treated with acupoint embedding therapy at different layers under B ultrasound].

OBJECTIVE: To investigate the short-term effect and safety on female abdominal obesity and defecation function in treatment with acupoint embedding therapy at different abdominal layers under B ultrasound. METHODS: A total of 102 female patients with abdominal obesity were randomly divided into 3 groups, i.e. a deep embedding group (34 cases, 1 case dropped out), a shallow embedding group (34 cases, 3 cases dropped out) and a sham-embedding group (34 cases, 6 cases dropped out). Finally, 92 cases were included in the three groups. Under B ultrasound, in the deep embedding group, the absor-bable surgical suture were embedded in subcutaneous fat layer and muscle layer. In the shallow embedding group, the absorbable surgical suture was embedded in the fat layer and in the sham-embedding group, no suture was embedded. The acupoints for embedding therapy included Zhongwan (CV12), Guanyuan (CV4), bilateral Guanmen (ST22), bilateral Tianshu (ST25), bilateral Daimai (GB26) and bilateral Shuidao (ST28). The acupoint embedding therapy was exerted once every two weeks, for 4 times totally. Before and after treatment, the changes in abdominal obesity indicators (waist circumference ï¼»WCï¼½, body fat rate ï¼»BFRï¼½, body mass index ï¼»BMIï¼½, abdominal subcutaneous fat thickness ï¼»ASFTï¼½) and defecation function indicators (spontaneous bowel movement times ï¼»SBMsï¼½ and Bristol stool scale ï¼»BSSï¼½) were observed and the safety indicators were assessed. RESULTS: After treatment, WC, BFR, BMI and ASFT were lower than those before treatment in both the deep embedding group and the shallow embedding group (P<0.05), those values in the deep embedding group were reduced more obviously as compared with the shallow embedding group (P<0.05). SBMs and BSS after treatment were increased as compared with those before treatment in both the deep embedding group and the shallow embedding group (P<0.05) and the increase in the deep embedding group was more obvious than in the shallow embedding group (P<0.05). The abdominal obesity indicators and defecation function indicators after treatment were not different statistically as compared with those before treatment in the sham-embedding group (P>0.05). The pain score of acupuncture in either the deep embedding group or the shallow embedding group was higher than in the sham-embedding group (P<0.05). The acceptance was more than 2 points in all of the three groups and there was no statistical significance among groups (P>0.05). CONCLUSION: Acupoint embedding therapy in both the deep and the shallow subcutaneous layers under B ultrasound may regulate the indicators of female abdominal obesity safely. The acupoint embedding therapy in the deep layer is more effective on abdominal obesity and defecation improvement as compared with that exerted in the shallow layer.