Comprehensive metabolic profiling of three plants of Ardisia based on UPLC-QTOF-MS coupled with bioactivity assays.

Ethnopharmacological Relevance: Ardisia is a large genus of Primulaceae, 734 accepted species worldwide, and most species are used as ethnomedicines for the treatment of bruises, rheumatism, tuberculosis, and various inflammatory diseases. According to our previous ethnobotanical survey, Ardisia gigantifolia Stapf, Ardisia hanceana Mez (Da-luo-san), and Ardisia crenata Sims (Xiao-luo-san) are commonly used in folk medicine for the treatment of rheumatism. Among them, A.

Gut microbiota and metabolomics unveil the mechanisms of in ameliorating visceral fat and serum lipids in high-fat diet-induced obese mice.

(LR) is a folk medicinal herb traditionally used as a lipid-lowering and anti-obesity agent; but its pharmacological mechanism is unclear. In this study, we assessed the alterations of LR on gut microbes and serum metabolites in obese mice and their associated mechanisms of modulation on visceral fat and serum lipid by integrating gut microbiota and metabolomics analyses. Mice were fed a high-fat diet (HFD) to generate obesity and were then given LR and Orlistat orally at different doses (0.

Metabolomics analysis reveals the effects of Bunge extract on ameliorating acute myocardial ischemia in rats induced by isoproterenol.

Salvia miltiorrhiza Bunge (SM) is a widespread herbal therapy for myocardial ischemia (MI). Nevertheless, the therapeutic signaling networks of SM extract on MI is yet unknown. Emerging evidences suggested that alterations in cardiac metabolite influences host metabolism and accelerates MI progression.

RNA-Seq Reveals Protective Mechanisms of Mongolian Medicine Molor-Dabos-4 on Acute Indomethacin-Induced Gastric Ulcers in Rats.

This study aimed to apply transcriptomics to determine how Molor-Dabos-4 (MD-4) protects healthy rats against indomethacin (IND)-induced gastric ulcers and to identify the mechanism behind this protective effect. Rats were pretreated with MD-4 (0.3, 1.

Metabolomics investigation on antiobesity effects of on high-fat high-sugar diet-induced obese rats.

Objective: (CB) is a well-used medicinal herb in Mongolian folk medicine and has been traditionally applied as an antiobesity agent. However, the evidence-based pharmacological effects of CB and its specific metabolic alterations in the obese model are not entirely understood. This study aimed to utilize untargeted metabolomic techniques to identify biomarkers and gain mechanistic insight into the serum metabolite alterations associated with weight loss and lipid metabolism in obese rats.

Usefulness of Noncontrast MRI-Based Radiomics Combined Clinic Biomarkers in Stratification of Liver Fibrosis.

Purpose: To develop and validate a radiomic nomogram based on texture features from out-of-phase T1W images and clinical biomarkers in prediction of liver fibrosis.

Materials And Methods: Patients clinically diagnosed with chronic liver fibrosis who underwent liver biopsy and noncontrast MRI were enrolled. All patients were assigned to the nonsignificant fibrosis group with fibrosis stage <2 and the significant fibrosis group with stage ≥2.

[Anti-obesity and lipid-lowering mechanism of Corydalis Bungeanae Herba: based on intestinal microflora and metabolomics].

This study aims to explore anti-obesity and lipid-lowering mechanism of Corydalis Bungeanae Herba(CB) based on intestinal microflora and metabolomics. Specifically, high-fat high-sugar diet(HFHS, 10 weeks) was used to induce obesity in rats. Then the model rats were randomized into the model group, low-dose(0.

Hepatoprotective Effects of on Nonalcoholic Fatty Liver Disease Induced by High-Fat Diet in Mice: An Integrated Gut Microbiota and Metabolomic Analysis.

(Thunb.) Nakai (IC) is a folk medicinal herb used in Mongolian medical clinics for the treatment of hepatitis and fatty liver diseases even though its pharmacological mechanism has not been well characterized. This study investigated the hepatoprotective mechanism of IC on mice with nonalcoholic fatty liver disease (NAFLD) by integrating gut microbiota and metabolomic analysis.

A rare case of duodenal spindle cell lipoma with gastrointestinal bleeding.

The manuscript reports a rare case of duodenal spindle cell lipoma (SCL), which is a rarely reported benign lipomatous neoplasm of the gastrointestinal tract. It is less commonly observed within the duodenum. Our patient presented with gastrointestinal bleeding, which is a rare symptom of lipomas.

Use of Texture Analysis on Noncontrast MRI in Classification of Early Stage of Liver Fibrosis.

e. To compare the diagnostic value of texture analysis- (TA-) derived parameters from out-of-phase T1W, in-phase T1W, and T2W images in the classification of the early stage of liver fibrosis. .

Clinical Study of the Prediction of Malignancy in Thyroid Nodules: Modified Score versus 2017 American College of Radiology's Thyroid Imaging Reporting and Data System Ultrasound Lexicon.

The clinical importance of thyroid nodules rests with the need to exclude thyroid cancer. In the present study, we developed a modified Thyroid Imaging Reporting and Data System (TI-RADS) score using gray-scale ultrasound, contrast-enhanced ultrasound (CEUS) and shear-wave elastography (SWE) images to predict malignancy of thyroid nodules and compared this modified score system with the subjective scoring criteria based on the Thyroid Imaging Reporting and Data System (TI-RADS, 2017 edition). The results revealed that by using SWE and CEUS (enhanced pattern) to downgrade TI-RADS category 4 and 5 nodules, the malignancy rate for TI-RADS category 4 and 5 nodules increased from 47.

Depletion of H3K79 methyltransferase Dot1L promotes cell invasion and cancer stem-like cell property in ovarian cancer.

DOT1-like protein (Dot1L) is the sole methyltransferase for methylation of lysine 79 in histone H3. Dot1L-dependent H3K79 methylation is involved in many biological processes, including telomeric silencing, cell cycle regulation, transcriptional activation and DNA repair. Genome-wide sequencing studies have revealed recurrent deletion and mutations of Dot1L gene in many types of human malignancies including ovarian cancer, however the role of Dot1L in ovarian cancer are largely unknown.

A potential biomarker hsa-miR-200a-5p distinguishing between benign thyroid tumors with papillary hyperplasia and papillary thyroid carcinoma.

Papillary thyroid carcinoma (PTC) is the most common endocrine cancer with a significantly increase of the incidence recently. Several cytokines, such as thyroid peroxidase (TPO), cluster of differentiation 56 (CD56), Galectin-3, mesothelial cell (MC), cytokeratin 19 (CK19) and BRAF (B-raf) were recommended to be tested by immunohistochemistry (IHC) for a definitive diagnosis, but were still limited in clinical use because of their relative lower sensitivity and specificity. MicroRNA (miRNA), as a new molecular biomarkers, however, has not been reported yet so far.

Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex.

Our previous study demonstrated that the retention of drug in the hydrophobic core of Soluplus micelle greatly impeded drug absorption from gastrointestinal tract. Using supersaturated polymeric micelles can improve drug release, however, insufficient maintaining of supersaturation of drug is still unfavorable for drug absorption. Here, we report adding small amount of small molecule, sodium dodecyl sulfate (SDS), to Soluplus solution can form a Soluplus-SDS complex.

Lipid-Based Formulations for Oral Drug Delivery: Effects on Drug Absorption and Metabolism.

The application of lipid-based drug delivery systems on the industrial scale has successfully demonstrated their therapeutic and manufacturing advantages. Recently, various lipid-based formulations were successfully prepared for oral delivery of compounds that are difficult to administer. Nevertheless, an improved understanding of how these formulations affect drug absorption and metabolism is required to support the rapid and successful completion of drug development programs.

Supersaturated polymeric micelles for oral cyclosporine A delivery.

Polymeric micelles provide a promising platform for improving oral absorption of poorly soluble drugs. However, improved understanding of how drug retention within the hydrophobic micelle core can reduce drug absorption is required. We designed supersaturated polymeric micelles (Super-PMs) to increase molecularly dissolved drug concentration and gain an insight into the effect of the degree of supersaturation on oral absorption of cyclosporine A (CsA) in rats.

Comparative study of Pluronic(®) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats.

Liposomes modified using cationic and hydrophilic nonionic polymers are 2 popular carriers for improving oral drug absorption. Cationic polymer-modified liposomes can adhere to the intestinal wall mucus (mucoadhesive type), while liposomes modified using hydrophilic nonionic polymers can penetrate across the mucus barrier (mucus-penetrating type). Chitosan-modified liposomes (CS-Lip, mucoadhesive type) and Pluronic(®) F127-modified liposomes (PF127-Lip, mucus-penetrating type) were engineered to investigate the differences between these mucoadhesive and mucus-penetrating systems in oral absorption of a poorly soluble drug, cyclosporine A (CyA).

An examination of the potential effect of lipids on the first-pass metabolism of the lipophilic drug anethol trithione.

In this study, an examination of the potential effect of lipids on the first-pass metabolism of anethol trithione (ATT) was investigated. ATT is metabolized rapidly and extensively in liver into 4-hydroxy-anethole trithione (ATX), which was confirmed using the rat intestinal perfusion with the mesenteric cannulation model. Male Sprague-Dawley rats were orally administered of the lipid-based formulations (prepared by medium chain triglycerides (MCT)), the cyclodextrin formulation and the suspension formulation, respectively.

Absorption enhancement of adefovir dipivoxil by incorporating MCT and ethyl oleate complex oil phase in emulsion.

Aim: To improve the oral absorption of adefovir dipivoxil (ADV) by employing MCT and the esterase inhibitor ethyl oleate (EO) as a complex oil phase in emulsion.

Methods: EO was used as the esterase inhibitor, and its inhibitory effect on esterase activity was assessed in rat intestinal homogenates. ADV emulsions with or without EO were prepared.

Reversible inhibitory effects of saturated and unsaturated alkyl esters on the carboxylesterases activity in rat intestine.

This study was conducted to investigate the relationship between the carbon chain length/double bonds of alkyl esters and their inhibitory potency/mechanism on carboxylesterases (CESs). CESs activity was evaluated by inhibition of adefovir dipivoxil (ADV) metabolism in rat intestinal homogenates. Furthermore, the inhibitory effect of BNPP and ethyl (E)-hex-2-enoate (C8:1) on drug absorption was evaluated in situ intestinal perfusion model.

Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: effects of lipid composition and formulation.

This study has explored the use of lipid-based formulations to enhance the oral bioavailability of the poorly water-soluble drug anethol trithione (ATT), and compared the performance of different formulations. Two groups of lipid-based formulations, sub-microemulsion (SME) and oil solution, were prepared using short (SCT), medium (MCT) and long (LCT) chain triglycerides respectively; aqueous suspension was used as the reference formulation. In vitro and in vivo studies were conducted to investigate the impact of lipid composition and formulation on drug absorption.