Que Zui tea ameliorates hepatic lipid accumulation and oxidative stress in high fat diet induced nonalcoholic fatty liver disease.

In this study, the protective effects of hot water (QW) and aqueous-ethanol extracts (QA) from Que Zui tea on non-alcoholic fatty liver disease (NAFLD) were investigated. Quantitative and qualitative analysis revealed that QW and QA were rich in polyphenols, especially 6'-O-caffeoylarbutin. Both QW and QA significantly reduced body weight and liver index, increased serum levels of high density lipoprotein cholesterol (HDL-C), and decreased the levels of total cholesterol (TC), triglyceride (TG), nonesterified free fatty acids (NEFA) and low density lipoprotein cholesterol (LDL-C) in NAFLD rats induced high fat diet. Furthermore, the contents of TC, TG, NEFA, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the liver tissues were inhibited after QW and QA administration. Histopathological examination showed that QW and QA significantly reduced liver lipid accumulation of NAFLD rats. In addition, QW and QA could enhance increase the activity of antioxidant (glutathione, superoxide dismutase and catalase) in the liver by regulation Nrf2 signaling pathway, thereby alleviating liver damage caused by lipid peroxidation. QW and QA activated AMPK/PPAR-α signaling pathway by increasing the expression of adiponectin and its receptor AdipoR2, thereby reducing fat production and enhancing fatty acid ß oxidation. These data suggested that QW and QA had the potential to in the prevention and treatment of NAFLD.

Phenolic Constituents, Antioxidant and Cytoprotective Activities, Enzyme Inhibition Abilities of Five Fractions from Vaccinium dunalianum Wight.

The bud of Vaccinium dunalianum Wight has been traditionally consumed as health herbal tea by "Yi" people in Yunnan Province, China, which was locally named "Que Zui tea". This paper studied the chemical constituents of five fractions from Vaccinium dunalianum, and their enzyme inhibitory effects of α-glucosidase and pancreatic lipase, antioxidant activity, and cytoprotective effects on H2O2-induced oxidative damage in HepG2 cells. The methanol extract of V. dunalianum was successively partitioned with petroleum ether (PF), chloroform (CF), ethyl acetate (EF), n-butanol (BF), and aqueous (WF) to obtain five fractions. The chemical profiling of the five fractions was analyzed by ultra-high-performance liquid chromatography coupled with a tandem mass spectrometry (UHPLC-MS/MS), and 18 compounds were tentatively identified. Compared to PF, CF, BF and WF, the EF revealed the highest total phenols (TPC) and total flavonoids (TFC), and displayed the strongest enzyme inhibition ability (α-glucosidase and pancreatic lipase) and antioxidant capacity (DPPH, ABTS and FRAP). Furthermore, these five fractions, especially EF, could effectively inhibit reactive oxygen species (ROS) production and cell apoptosis on H2O2-induced oxidative damage protection in HepG2 cells. This inhibitory effect might be caused by the up-regulation of intracellular antioxidant enzyme activity (CAT, SOD, and GSH). The flavonoids and phenolic acids of V. dunalianum might be the bioactive substances responsible for enzyme inhibitory, antioxidant, and cytoprotective activities.

6'-O-Caffeoylarbutin from Que Zui tea ameliorates acetaminophen-induced liver injury via enhancing antioxidant ability and regulating the PI3K signaling pathway.

Que Zui tea (QT), a traditional herbal tea in China, has a significant hepatoprotective effect. 6'-O-Caffeoylarbutin (CA) is the most abundant chemical compound in the QT. However, the hepatoprotective effect of CA has not been investigated. This study is aimed to evaluate the protective effect of CA on acetaminophen (APAP) induced hepatotoxicity in vivo and in vitro and its possible underlying mechanism. In APAP-induced HepG-2 cells, CA inhibited intracellular ROS accumulation and cell apoptosis, and improved the expression of antioxidants including SOD, CAT and GSH. In APAP-administrated mice, CA pretreatment remarkably ameliorated the histopathological damage and inflammatory response, and antioxidant enzyme activity in the serum and liver tissues. Moreover, the immunohistochemistry and immunofluorescence assay results revealed that the CA markedly reduced ROS production and apoptosis, and activated antioxidant transcription factor Nrf2 in the liver. Meanwhile, molecular docking results showed that the strong binding force of CA and PI3K was due to the higher number of hydrogen- and π-bonds with active site residues. Notably, CA pretreatment significantly regulated the expression of PI3K, Akt, Nrf2, NQO1, HO-1, Bcl-2, Bax, caspase-3, and caspase-9 proteins in APAP-treated liver tissues. These data demonstrated that CA had a protective effect against APAP-induced hepatotoxicity via regulating the PI3K/Akt and Nrf2 signaling pathway.

Hypoglycemic and hypolipidemic effects of Epigynum auritum in high fat diet and streptozotocin-induced diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Epigynum auritum is mainly distributed in Southwest China, and has been used as a "dai" folk medicine with promising Besides, the leaves and barks of E. auritum have detoxifying, analgesic and relieving swelling effects. Previous studies evidenced that E. auritum was rich in pregnanes and their glycosides. However, the hypoglycemic and hypolipidemic effects of the extract from E. auritum (EAE) and its molecular mechanism are still not studied. AIM OF THE STUDY: The aim of this study is to investigate the hypoglycemic and hypolipidemic effects of EAE on high-fat diet and streptozocin-induced type 2 diabetic rats. MATERIALS AND METHODS: The high-fat diet and streptozocin induced type 2 diabetic model was established. The diabetic rats were treated with 70% ethanol extract of E. auritum (100 and 300 mg/kg/d) or metformin (DMBG, 100 mg/kg/d) every day for 4 weeks. Fasting blood glucose was recorded weekly. The phenotypic changes were evaluated by the measurement of biochemical indexes and immunohistochemical. The expressions of signaling-related proteins were explored by western blotting. RESULTS: EAE could effectively regulate the metabolism of glucose and lipids in diabetic rats by increasing insulin sensitivity. In addition, EAE ameliorated the oxidative stress damage and further mitigated the liver, kidney, and pancreatic damage. Mechanism research results show that EAE treatment increased the phosphorylation of Akt, AMPK and GSK-3ß, up-regulated the expression of GLUT-2, GLUT-4 and PPAR-α, and reduced PPAR-γ and FAS expressions. CONCLUSION: EAE exhibited significant hypoglycemic and hypolipidemic effects in HFD/STZ-induced diabetes rats. The mechanism may be related to the effective upregulation of AMPK/Akt/GSK-3ß pathway and the decreased expression of PPAR-γ and FAS. It could be a promising natural product with potential value for the development of drugs to prevent or treat type 2 diabetic.

Anti-leukemic effect and molecular mechanism of 11-methoxytabersonine from Melodinus cochinchinensis via network pharmacology, ROS-mediated mitochondrial dysfunction and PI3K/Akt signaling pathway.

Melodinus cochinchinensis (Lour.) Merr. is a Yunnan endemic folk medicine. Our previous study showed that 11-methoxytabersonine (11-MT) isolated from M. cochinchinensis has strong cytotoxicity on human T-ALL cells, but its molecular mechanism has not been studied. In current study, the cytotoxicity and possible mechanism of 11-MT on T-cell acute lymphoblastic leukemia was explored using network pharmacology and molecular biology techniques. 11-MT significantly inhibited the cell proliferations on different four human T-ALL cells (MOLT-4, Jurkat, CCRF-CEM, and CEM/C1 cells). 11-MT triggered ROS accumulation, calcium concentration and cell apoptosis, and decreased the mitochondrial membrane potential (MMP) in human T-ALL cells, especially MOLT-4 cells. Western blot analysis showed that it can induce MOLT-4 cell apoptosis by up-regulating PI3K/Akt signaling pathway. Therefore, 11-MT induces human T-ALL cells apoptosis via up-regulation of ROS-mediated mitochondrial dysfunction and down-regulation of PI3K/Akt/mTOR signaling pathway.

Potent immunosuppressive and anti-inflammatory bisindole alkaloids from Melodinus fusiformis.

Phytochemical investigation of Melodinus fusiformis led to a new aspidosperma-aspidosperma bisindole alkaloid (BIA), bis-19ß-hydroxyvenalstonidine (1), together with three known BIAs (2-4). The structures were established by extensive analysis of their HRESIMS, NMR data, and comparing with the reported data. BIA 1 is an almost symmetrical structure, linked by C3-C14' bond, while BIAs 2-4 are reported for the first time from the plant. The cytotoxic, immunosuppressive and anti-inflammatory activities of BIAs 1-4 were evaluated in vitro. BIAs 1, 3 and 4 showed good toxicity against MOLT-4 cell lines with IC50 values in the range of 1.5-17.5 -M. BIA 2 exhibited the strongest inhibitory effect against MCF-7 cell lines with an IC50 value of 7.1 µM. BIA 1 significantly inhibited Con A-stimulated mice splenocytes proliferation equal to that of the positive control (DXM) in a concentration-dependent manner. BIAs 1 and 2 were able to decrease the NO production in LPS-induced RAW 264.7 cells at 30 µM concentration. BIA 2 showed similar inhibition of nitric oxide release, compared to that of DXM. Furthermore, BIA 2 remarkably inhibited the levels of IL-6 and TNF-α compared to the LPS induced group. Interestingly, BIA 2 displayed an inhibitory effect on TNF-α production similar to that of dexamethasone at a concentration of 20 µM.

The effect of ultra-high pretreatment on free, esterified and insoluble-bound phenolics from mango leaves and their antioxidant and cytoprotective activities.

Ultra-high pressure (UHP) is a novel non-thermal pretreatment method in food processing for improving the extraction yield of polyphenols and functional properties. The present work investigated the phenolic profiles, antioxidant activities, and cytoprotective effects of the free, esterified, and insoluble-bound phenolic fractions from mango leaves before and after ultra-high pressure (UHP) treatment. UHPLC-Q-Orbitrap-MS/MS analysis resulted in the identification of 42 phenolic compounds in the different phenolic forms. UHP pretreatment could significantly influence the contents of total phenols, total flavonoids and individual compounds in the different phenolic fractions (p < 0.05). After UHP pretreatment, these phenolic fractions exhibited greater antioxidant activity, and inhibited reactive oxygen species production and cell apoptosis (p < 0.05). Meanwhile, IBP were the most potential antioxidative and cytoprotective ingredients. Therefore, UHP pretreated mango leaves with enhanced bioactivity could be used as biological agents in the health food industry to improve its application and economic values.

Phenolic constituents, antioxidant activity and neuroprotective effects of ethanol extracts of fruits, leaves and flower buds from Vaccinium dunalianum Wight.

Vaccinium dunalianum Wight is an important healthy tea resource in China with health benefits. The chemical compositions and the possible bioactive substances in its fruits, leaves and flower buds extracts (FE, LE and FBE) were identified and characterized by UHPLC-HRMS/MS. Consequently, FE, LE and FBE were rich in phenolic and flavonoid compounds. Among them, 21 compounds were identified, and the main components were chlorogenic acid, quinic acid and 6'-O-caffeoylarbutin. Furthermore, their neuroprotection and mechanism on H2O2-induced neurotoxicity in PC12 cells were investigated. All the different concentrations of FE, LE and FBE were apparently inhibited the H2O2-induced ROS generation and apoptosis on PC12 cells. FBE showed stronger neuroprotective activity against H2O2-induced PC12 cell damage than those of FE and LE. The mechanism of neuroprotective effect might be related to the upregulation of endogenous antioxidant enzymes expressions and activation of the Nrf2/HO-1 signaling pathway.

4,21-Secovincanol, a Novel Immunosuppressive Monoterpenoid Indole Alkaloid from Kopsia Hainanensis.

4,21-Secovincanol (1), a novel C-21/N-4 cleavage monoterpenoid indole alkaloid, along with four analogs (2-5), were obtained from the aerial parts of Kopsia hainanensis. Structurally, compound 1 might be a derivative of epivincanol (2) via C-21/N-4 cleavage. Their structures were confirmed by means of comprehensive spectroscopic data analysis and comparison with the reported data. All isolates significantly inhibited Con A-stimulated mice splenocytes proliferation at 10-40 µM in a dose-dependent manner in vitro. Especially, compound 3 exhibited potent activities comparable to positive control (Dexamethasone, DXM).

Structural characterization and immunosuppressive activity of a new pregnane glycoside from Epigynum cochinchinensis.

Phytochemical investigation on the ethyl acetate fraction of the leaves of Epigynum cochinchinensis led to the isolation of a new C21 pregnane glycoside, epigycoside B (1), together with three known analogues. Their structures were elucidated on the basis of extensive spectroscopic techniques, including UV, MS, and NMR experiments, as well as the chemical methods. Compound 1 displayed in vitro immunosuppressive activity against concanavalin A (Con A)/Lipopolysaccharides (LPS)-stimulated proliferation of mice splenocyte. The activity was significant as compared with control group at 50 µM concentration.

A new immunosuppressive pregnane glycoside from aqueous fraction of Epigynum cochinchinensis.

Chemical investigation on the aqueous fraction of the stems of Epigynum cochinchinensis led to the isolation of a new pregnane glycoside named as epigycoside A (1) along with three known analogues (2-4). The structure of compound 1 was elucidated by means of spectroscopic techniques, including HRESIMS, and 1D and 2D NMR experiments. The immunosuppressive activity of 1 was evaluated by an in vitro model of concanavalin A-induced mice splenocytes proliferation. Compound 1 showed significant inhibitory activity in a dose-dependent manner, closer to the efficacy of positive control, dexamethasone, at a concentration of 50 µM.

Novel immunosuppressive pregnane glycosides from the leaves of Epigynum auritum.

Phytochemical investigation on the leaves of Epigynum auritum led to the isolation of three novel C21 pregnane glycosides, epigynosides, E-G (1-3), together with two known pregnane glycosides, epigynosides A (4) and C (5). Their structures were elucidated based on extensive spectroscopic data (MS, IR, 1D and 2D NMR) analysis, as well as comparison with the reported data. The immunological activities of the new compounds was evaluated against concanavalin A (Con A)-stimulated proliferation of mice splenocyte in vitro. Compounds 1-3 displayed significant immunosuppressive activities, close to the efficacy of the positive control (dexamethasone) at the concentration of 50µM.

Seco-pregnane glycosides from the stems of Epigynum auritum.

Chemical investigation of the stems of Epigynum auritum led to the isolation and identification of a novel 16,17-seco pregnane glycoside, epigynoside D, along with other three known compounds (2-4). The structure of compound 1 was elucidated by means of spectroscopic analysis, including HRESIMS, 1D and 2D NMR experiments. All isolated compounds were tested for their in vitro cytotoxic, immunological and anti-acetylcholinesterase activities.

Good interrater reliability of a new grading system in detecting traumatic bone marrow lesions in the knee by dual energy CT virtual non-calcium images.

OBJECTIVE: To evaluate the capacity of dual-energy computed tomography (DECT) virtual non-calcium (VNCa) images in detecting post-traumatic bone marrow lesions (BMLs) in the knee with a new grading system. METHODS: DECT and magnetic resonance (MR) imaging were used to examine acute trauma of the knee in 32 patients. VNCa images were generated by dual-energy subtraction of calcium, and the lower end of the femur and upper end of the tibia each were divided into six regions for grading of bone marrow by two musculoskeletal radiologists using a four-grading system (Grade 4, very obvious lesions; Grade 3, relatively obvious lesions; Grade 2, slight or suspicious lesion on VNCa image and mild lesion on MR image; Grade 1, normal bone marrow). CT values were obtained in the BMLs. MR images were used as the reference standard. Grade 3-4 bone marrow was regarded as a positive result to evaluate the performance of VNCa images in detecting traumatic BMLs in the knee, and receiver operating characteristic (ROC) curve analysis of VNCa images for detection of knee BMLs was performed based on CT value of the bone marrow. RESULTS: Bone marrow rating by the two radiologists showed very good consistency (κ=0.850 and 0.869 for VNCa and MR images, respectively). VNCa and MR images had good consistency (κ=0.799 for lower end of the femur; κ=0.659 for upper end of the tibia). When Grade 3-4 bone marrow was regarded as a positive result, the sensitivity, specificity, positive predictive value, and negative predictive value of VNCa images for detection of BMLs in the lower end of the femur were 73.5%, 98.6%, 94.7%, and 91.6%, respectively, and the values in the upper end of the tibia were 91.0%, 100.0%, 100.0%, and 95.4%, respectively. The CT values of bone marrow were (-52.5 ± 31.3) HU in positive area and (-91.2 ± 16.9) HU in negative area for the lower end of the femur, and those were (-51.3 ± 30.2) HU in positive area and (-104.7 ± 17.5) HU in negative area for the upper end of the tibia (all p values<0.0001). The areas under the ROC curve of VNCa images for detection of BMLs were 0.875 for the lower end of the femur and 0.939 for the upper end of the tibia. CONCLUSION: Good interrater reliability of this new grading system in detecting traumatic BMLs in the knee by VNCa images of DECT can be obtained with good diagnostic predictive values.

Radiation and contrast agent doses reductions by using 80-kV tube voltage in coronary computed tomographic angiography: a comparative study.

OBJECTIVE: To investigate the effects of 80-kilovoltage (kV) tube voltage coronary computed tomographic angiography (CCTA) with a reduced amount of contrast agent on qualitative and quantitative image quality parameters and on radiation dose in patients with a body mass index (BMI) <23.0 kg/m(2). METHODS: One hundred and twenty consecutive patients with a BMI <23.0 kg/m(2) and a low calcium load undergoing retrospective electrocardiogram (ECG)-gated dual-source CCTA were randomized into two groups [standard-tube voltage (120-kV) vs. low-tube voltage (80-kV)]. The injection flow rate of contrast agent (350 mg I/mL) was adjusted to body weight of each patient (4.5-5.5 mL/s in the 120-kV group and 2.8-3.8 mL/s in the 80-kV group). Radiation and contrast agent doses were evaluated. Quantitative image quality parameters and figure of merit (FOM) of coronary artery were evaluated. Each coronary segment was evaluated for image quality on a 4-point scale. RESULTS: Compared with the 120-kV group, effective dose and amount of contrast agent in the 80-kV group were decreased by 57.8% and 30.5% (effective dose:2.7 ± 0.5 vs. 6.4 ± 1.3 mSv; amount of contrast agent:57.1 ± 3.2 vs. 82.1 ± 6.1 mL; both p<0.0001), respectively. Image noise was 22.7 ± 2.1HU for 120-kV images and 33.2 ± 5.2 HU for 80-kV images (p<0.0001). Signal-to-noise ratio (SNR) and contrast-to-noise ratio (CNR) in the proximal right coronary artery (RCA) and left main coronary artery (LMA) were all lower in 80-kV than 120-kV images (SNR in the proximal RCA: 16.5 ± 1.8 vs. 19.4 ± 2.8; SNR in the LMA: 16.3 ± 2.0 vs.19.6 ± 2.7; CNR in the proximal RCA: 19.4 ± 2.3 vs.22.9 ± 3.0; CNR in the LMA: 18.8 ± 2.4 vs. 22.7 ± 2.9; all p<0.0001). FOM were all significantly higher in 80-kV than 120-kV images (proximal RCA: 146.7 ± 45.1 vs. 93.4 ± 32.0; LMA: 139.1 ± 47.2 vs. 91.6 ± 31.1; all p<0.0001). There was no significant difference in image quality score between the two groups (3.3 ± 0.8 vs. 3.3 ± 0.8, p=0.068) despite decreased SNR and CNR of coronary artery in the 80-kV group. CONCLUSION: The 80-kV protocol significantly reduces radiation and contrast agent doses in CCTA in patients with a low BMI <23.0 kg/m(2) and a low calcium load while maintaining image quality.

Effect of chitosan film incorporated with tea polyphenol on quality and shelf life of pork meat patties.

The objective of this study was to investigate the effect of chitosan (CH) film incorporated with tea polyphenol (TP) on quality and shelf life of pork meat patties stored at 4±1 °C for 12 days. The microbiological, physicochemical (pH, thiobarbituric acid-reactive substances (TBARS) values, and metmyoglobin (MetMb)), and sensory qualities were measured on all the samples. A microbiological shelf-life extension of 6 days was achieved for CH and CH-TP treatment groups when compared to the control group. Wrapping with CH-TP composite film tended to retard the increases in TBARS values and MetMb content. CH-TP composite film maintained acceptable sensory quality of pork meat patties throughout the storage. The results indicated that CH-TP composite film could be a promising material as a packaging film for extending the shelf life of pork meat patties.

Progress of pharmacological studies on alkaloids from Apocynaceae.

Alkaloid was a kind of biological active ingredient. There were various types of alkaloids in Apocynaceae. This paper reviewed the progress on alkaloids from Apocynaceae, which contained origin, structure, and pharmacological activity.

A new 8-O-4' neolignan glycoside from Tetracentron sinense.

A new 8-O-4' neolignan glycoside was isolated from the stem bark of Tetracentron sinense. Its structure was elucidated as erythro 4',5',7, 9, 9'-pentahydroxy-3-methoxy 8-O-4'-neolignan 3'-O-beta-glucopyranoside on the basis of spectral evidence (MS, IR, 1D and 2D NMR).

[Studies on chemical constituents from roots of Mirabilis jalapa].

OBJECTIVE: To investigate the anti-HIV constituents from the root of Mirabilis jalapa. METHOD: The compounds were isolated by column chromatography on silica gel, Sephadex LH - 20, MCI-gel CHP-20P and RP-18. The structure were identified by means of NMR and MS analyses (1H-NMR, 13C-NMR, MS). RESULT: Eleven compounds were isolated and identified as astragaloside II (1), astragaloside II (2), astragaloside IV (3), astragaloside VI (4), flazin (5), 4'-hydroxy-2, 3-dihydroflavone 7-beta-D-glucopyranoside (6), gingerglycolipid A (7), 3, 4-dihydroxybenzaldehyd (8), p-hydroxybenzaldehyde (9), beta-sitosterol (10) and daucosterol (11). CONCLUSION: Compounds 1-9 were obtained from this genus for the first time.

[Determination of flavones in Elsholtzia bodinieri by HPLC].

OBJECTIVE: To develop an HPLC method for the measurement of flavones in Elsholtzia bodinieri. METHOD: Analysis was carried out on Shimadzu LC-2010A HPLC system. The separation was performed on Agilent Extend-RP C18 column (4. 6 mm x 250 mm, 5 microm), with methanol-acetonitrile-0.2% phosphoric acid as mobile phase, and the flow rate was 1.0 mL min(-1) and the detective wavelength was 280 nm. RESULT: A good linear relationship and the mean recovery was found within the range. CONCLUSION: This method is rapid, simple and accurate.