Ginseng saponins are a type of important active substances in the ginseng genus plants. They have notable pharmacological activities of antineoplastic, neuroprotective, and hepatoprotective activities, which have been drawn more attention to obtain minor ginsenosides by all kinds of methods. In this review, we discussed the latest progress for enrichment of minor ginsenosides by biological transformation of major ginsenosides. At the same time, we have a brief outlook of the research at bioconversion of ginseng saponins.
Bacteria ; metabolism ; Biotransformation ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Ginsenosides ; chemistry ; metabolism ; Panax ; chemistry ; metabolism

Animals ; Animals, Newborn ; Hypoxia-Ischemia, Brain ; metabolism ; Neuroprotective Agents ; pharmacology ; Nitric Oxide ; biosynthesis ; Nitric Oxide Synthase Type II ; metabolism ; Progesterone ; pharmacology ; Rats ; Rats, Wistar

OBJECTIVETo observe the effect of Shenluotong Decoction (SD) on serum levels of aldosterone, monocyte chemoattractant protein-1 (MCP-1), α-smooth muscle protein (α-SMA), and nuclear factor-KB (NF-κB) in obstructive nephropathy rats, and to explore the initial mechanism of SD for inhibiting renal interstitial fibrosis.

METHODSTotally 48 healthy Wistar rats were randomly divided into the sham-operation group (n =12) and the model group (n =36). Renal interstitial fibrosis rat model was established by unilateral ureteral obstruction (UUO). After successful modeling, 36 rats were randomly divided into the model group, the Chinese medicine group, and the Western medicine group, 12 in each group. Eplerenone was added in the forage at the daily dose of 100 mg/kg for rats in the Western medicine group. Chinese medicine was added in the forage at the daily dose of 26 g/kg for rats in the Chinese medicine group. Equal volume of normal saline was administered to rats in the sham-operation group and the model group. All medication was performed once daily. The obstructive kidneys were extracted ten days after medication. The pathomorphological changes were observed. The contents of serum aldosterone and MCP-1, and the protein or mRNA expression of MCP-1, α-SMA, and NF-KB were detected.

RESULTSCompared with the sham-operation group, infiltration of a large amount of inflammatory cells and collagen deposition significantly increased, serum contents of aldosterone and MCP-1 obviously increased (P < 0.01), the expression of MCP-1 mRNA and protein were significantly up-regulated (P <0.01), the protein expression of α-SMA and NF-KB were significantly enhanced in the model group (P <0.01). Com- pared with the model group, infiltration of inflammatory cells and renal collagen deposition were attenua- ted in the Chinese medicine group and the Western medicine group, the serum MCP-1 level were reduced, and the mRNA and protein expression of MCP-1 were significantly down-regulated (P <0.01), the protein expression of α-SMA and NF-KB were obviously inhibited (P <0. 01). At the same time, serum aldosterone level was reduced in the Chinese medicine group (P <0.01).

CONCLUSIONSinflammatory lesions of the renal tissue could promote the progress of interstitial fibrosis in rats with obstructive nephropathy. SD could attenuate interstitial fibrosis through reducing serum contents of aldosterone and MCP-1, down-regulating MCP-1/ NF-KB, and inhibiting the expression of α-SMA.

Animals ; Chemokine CCL2 ; drug effects ; metabolism ; Down-Regulation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Fibrosis ; Kidney ; drug effects ; Kidney Diseases ; drug therapy ; genetics ; NF-kappa B ; drug effects ; metabolism ; RNA, Messenger ; biosynthesis ; Rats, Sprague-Dawley ; Ureteral Obstruction ; drug therapy ; genetics

Objective:To explore the different functional connectivity of right caudate nucleus between adults with high myopia and normal vision controls.Methods:The resting-state functional magnetic resonance imaging(fMRI) data were collected from twenty-five high myopia(HM group) and twenty-seven normal vision subjects(NC group). Right caudate nucleus and their subregions(anterior and posterior subregions included) were used as seeds to perform seed-based functional connectivity (FC)analyses at group level under three different frequency bands: convention (0.010~0.080 Hz), slow-5(0.010~0.027 Hz) and slow-4(0.027~0.073 Hz).Results:(1)Compared with NC group, FC of right caudate nucleus with left middle occipital gyrus(MNI: x=-48, y=-84, z=9), left fusiform gyrus(MNI: x=-30, y=-63, z=-12), and right middle frontal gyrus(MNI: x=39, y=12, z=39) were stronger in HM group(all P<0.05, Alphasim Corrected). (2)In HM group, these changed FC were mainly detected in the anterior subregion of right caudate nucleus.(3)The increased FC of right caudate nucleus and its anterior subregion with left middle occipital in HM group were mainly reflected in the frequency band of slow-4(all P<0.05, Alphasim Corrected). Conclusion:The right caudate nucleus in adults with high myopia may play compensatory roles in visual perception and visual attention by enhancing its functional connectivity with visual and visual attentional brain areas.

Asian Continental Ancestry Group ; China ; Diabetes Mellitus, Type 2 ; ethnology ; genetics ; Genetic Variation ; Genotype ; Humans ; Insulin Receptor Substrate Proteins ; Intracellular Signaling Peptides and Proteins ; Phosphoproteins ; genetics

OBJECTIVETo investigate the impact of depression on clinical outcome of patients undergoing revascularization.

METHODSSelf-rating depression scale (SDS) assessment was made before and after coronary artery bypass grafting (CABG, n = 345) and percutaneous coronary intervention (PCI, n = 308) procedure. Patients were divided into depression and non-depression group. All patients were followed up for 12 months after procedure for the occurrence of rehospitalization and major adverse cardiovascular events (MACE) including all-cause mortality, nonfatal myocardial infarction or target lesion revascularization.

RESULTSDepression was present in 40.9% (n = 141) of patients after CABG, which was significantly higher than before procedure (24.3%, P < 0.01). The MACE rate was significantly higher in patients with post-procedure depression [8.5% (12/141)] than in patients without depression [2.9% (6/204), P < 0.05] and the incidences of target lesion revascularization and rehospitalization were also significantly higher in depression patients than in non-depression patients during the 12 months follow-up (all P < 0.05). Depression was present in 36.4% (n = 112) of patients after PCI, which was significantly higher than that before procedure (28.6%, P < 0.05). The MACE rate [8.0% (9/112) vs. 2.0% (4/196)] and rehospitalization rate [12.5% (14/112) vs. 4.6% (9/196)] were significantly higher in depression patients than in patients without depression during the 12 months follow-up (P < 0.05). There was no significant difference on SDS score between the PCI and CABG before the procedure. However, after the procedure, the SDS score for patients undergoing CABG was significantly higher than in patients undergoing PCI (48.9 ± 9.8 vs. 45.7 ± 10.5 P = 0.01). The level of serum IL-6 was significantly higher in depression patients than in patients without depression (P < 0.05).

CONCLUSIONPrevalence of depression is high in patients treated with revascularization procedures and is linked with poor post-procedure prognosis.

Aged ; Angioplasty, Balloon, Coronary ; Coronary Artery Bypass ; Coronary Disease ; diagnosis ; psychology ; therapy ; Coronary Stenosis ; Depression ; etiology ; Female ; Humans ; Male ; Middle Aged ; Prognosis ; Treatment Outcome

In order to develop potent antidiabetic agents that have inhibitory effect to a-glucosidase, twelve β-acetamido ketone derivatives such as N-{[(substituted-4-oxo-thiochroman-3-yl)phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by 1H NMR, 13C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-41 were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol x L(-1). The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.
Acetamides ; Glycoside Hydrolase Inhibitors ; chemical synthesis ; pharmacology ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Molecular Docking Simulation ; Structure-Activity Relationship ; alpha-Glucosidases ; metabolism

OBJECTIVETo study the value of ROI A value in the strain ratio and the elasticity scores by the 4-score system in ultrasonic elastography in differential diagnosis of benign and malignant thyroid nodules.

METHODSA total of 124 patients with 166 thyroid nodules underwent examinations with real-time ultrasonic elastography to obtain the elasticity score and the ROI A value in strain ratio. Receiver operating characteristic (ROC) curves were used to assess the diagnostic value of ROI A value, and the best cutoff point was determined. The results of diagnosis based on ROI A value, elasticity scores, and their combination were compared with the results of pathological diagnosis.

RESULTSThe area under the ROC curve (Az) of ROI A value for differentiating benign and malignant thyroid nodules was 0.825. The best diagnostic cut-off point of ROI A value was 0.00165. In differentiating benign and malignant thyroid nodules, the sensitivity, specificity, accuracy and odds ratio were 82.93%, 72.80%, 75.30%, and 13.0 for ROI A value, 87.80%, 80.00%, 81.93%, and 28.8 for the elasticity scores, and 73.17%, 91.20%, 86.75%, and 32.1 for their combination, respectively. The odds ratio of the combined diagnosis was the highest, and the accuracy of the combined diagnosis was significantly higher than that of ROI A value (χ(2)=19.31, P<0.05) and the elasticity scores (χ(2)=12.03, P<0.05).

CONCLUSIONROI A value has moderate diagnostic value and clinical practicability in differentiating thyroid nodules. The diagnostic accuracy of ROI A value can be improved by combining with the elasticity scores.

Adolescent ; Adult ; Aged ; Child ; Child, Preschool ; Diagnosis, Differential ; Elasticity Imaging Techniques ; methods ; Female ; Humans ; Male ; Middle Aged ; ROC Curve ; Thyroid Nodule ; diagnostic imaging ; Young Adult

OBJECTIVETo investigate the synergistic effects of carnosic acid (CA) with arsenic trioxide (As₂O₃) on proliferation and apoptosis in HL-60 human myeloid leukemia cells, and the major cellular signaling pathway involved in these effects.

METHODSHL-60 cellular proliferation was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) analysis. Cell cycle distribution and apoptosis were monitored by flow cytometry. The activation of casepase-9, Bcl-2-associated agonist of cell death (BAD), p-BAD, p27, phosphatase and tensin homolog deleted on chromosome ten (PTEN), Akt, p-Akt was assessed by Western blot analysis. The expression of PTEN mRNA was tested by reverse transcription polymerase chain reaction (RT-PCR) analysis.

RESULTSCA reduced HL-60 cell viability in a dose- and time-dependent manner, and induced G1 arrest and apoptosis. Moreover, CA upregulated PTEN expression, blocked the Akt signaling pathway, subsequently inhibited phosphorylation of BAD, reactivated caspase-9, and elevated levels of p27. CA also augmented these effects of As₂O₃.

CONCLUSIONCA might be a novel candidate of the combination therapy for leukemia treatment; these effects were apparently associated with the modulation of PTEN/Akt signaling pathway.

Apoptosis ; drug effects ; Arsenicals ; pharmacology ; Base Sequence ; Blotting, Western ; Cell Cycle ; drug effects ; DNA Primers ; Diterpenes, Abietane ; pharmacology ; Drug Synergism ; HL-60 Cells ; Humans ; Leukemia, Myeloid, Acute ; metabolism ; pathology ; Oxides ; pharmacology ; PTEN Phosphohydrolase ; metabolism ; Plant Extracts ; pharmacology ; Proto-Oncogene Proteins c-akt ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; Signal Transduction ; drug effects

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