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1.
J Integr Med ; 22(2): 126-136, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38413255

ABSTRACT

BACKGROUND: Red yeast rice (RYR), a natural lipid-lowering agent, is widely used in clinical practice. However, the existing meta-analyses concerning the safety of RYR preparations have yielded inconsistent results, and the credibility of the evidence has not been quantified. OBJECTIVE: This study was designed to evaluate the existing evidence and offer a comprehensive understanding of the associations between the use of RYR preparations and various adverse health outcomes. SEARCH STRATEGY: Seven literature databases were searched from inception to May 5, 2023, using medical subject headings and free-text terms (e.g., "red yeast rice," "Xuezhikang," and "Zhibitai"). INCLUSION CRITERIA: Meta-analyses that investigated and quantitatively estimated associations between the use of RYR preparations and adverse health outcomes were included in this study. DATA EXTRACTION AND ANALYSIS: Two researchers independently extracted data using a standardized data collection table; any disagreements were resolved by consulting a third researcher. Based on the participant, intervention, comparator and outcome (PICO) framework in each eligible meta-analysis, a series of unique associations between the use of RYR preparations and adverse health outcomes were determined. The associations' effect estimates were re-evaluated using random-effect models. RESULTS: Fifteen meta-analyses, comprising 186 (164 unique) randomized controlled trials, were identified. Based on A MeaSurement Tool to Assess Systematic Reviews version 2, 3 (20%) and 12 (80%) of these meta-analyses had low and critically low confidence, respectively. A total of 61 unique associations between the use of RYR preparations and adverse health outcomes were extracted from eligible meta-analyses. Based on the random-effect models, 10 (16.4%) associations indicated a significant protective effect of RYR preparations against adverse health outcomes, while 5 (8.2%) indicated an increased risk of adverse health outcomes related to uric acid, alanine transaminase and aspartate transaminase levels. The other 46 (75.4%) associations showed no significant difference between the use of RYR preparations and control treatments. Regarding the credibility of the evidence, 21 (34.4%), 34 (55.7%) and 6 (9.8%) associations showed moderate, low and very low credibility, respectively. CONCLUSION: The evidence examined in this study suggests that RYR preparations are safe; however, the credibility of the evidence was not high. Further high-quality evidence is required. Please cite this article as: Ma ZY, Yang SP, Li Y, Xu TT, Yang YL, Yang HY, Li HB, Zhou LJ, Diao Y, Li SY. Associations between the use of red yeast rice preparations and adverse health outcomes: An umbrella review of meta-analyses of randomized controlled trials. J Integr Med. 2024; 22(2): 126-136.


Subject(s)
Biological Products , Humans , Randomized Controlled Trials as Topic , Biological Products/adverse effects
2.
J Sep Sci ; 45(3): 739-751, 2022 Feb.
Article in English | MEDLINE | ID: mdl-34865311

ABSTRACT

Trace amounts of components in traditional Chinese medicine are considered pharmacological active substances used for treating many serious diseases. However, purifying all the trace substances and making clear their structures are not easy. In this context, high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry based molecular networking was applied to investigate the chemical constituents of the roots of Aconitum kusnezoffii Reichb., which led to the identification of 33 nodes in different groups (N1-N33). Based on the excremental fragmentation pathway of known diterpenoid alkaloids (1-9) and comparisons of characteristic ions and characteristic loss of analogs in literature, the structures of unknown ions were deduced. This work lays a foundation for the evaluation of the clinical basis and mechanism of traditional Chinese medicine from the aspects of chemistry. In this paper, the method speculation of unknown natural products by means of molecular network method is expected to be applied in the discovery and change law of relevant active components in clinical pharmacology and the change of complex systems caused by trace active compounds.


Subject(s)
Aconitum , Alkaloids , Diterpenes , Drugs, Chinese Herbal , Aconitum/chemistry , Alkaloids/analysis , Chromatography, High Pressure Liquid , Chromatography, Liquid , Diterpenes/analysis , Drugs, Chinese Herbal/chemistry , Tandem Mass Spectrometry
3.
Int Wound J ; 19(1): 222-229, 2022 Jan.
Article in English | MEDLINE | ID: mdl-34129273

ABSTRACT

Grade 4 peripheral intravenous infiltration with skin tears has seldom been reported. On 4 August 2020, a 35-year-old female patient was admitted to the emergency department of our hospital because of postprandial abdominal pain for 2 hours. She was diagnosed with a severe acute pancreatitis with type II diabetes mellitus. On 7 August, a vein detained needle was inserted into the dorsal vein of her right foot to infuse drugs. On 9 August, a grade 4 infiltration, discoloured and bruised skin with a swollen area of 11 cm × 9 cm around the infusion part of her right foot, was discovered. The infusion was stopped immediately and the residual drug was aspirated at the infusion site. When removing the vein detained needle, the skin surrounding the infusion site on the right foot was torn by the adhesive dressing. The size of the skin tears was 6 cm × 3 cm (type 3). The patient was provided with appropriate dressing, manual lymphatic drainage, and surgical intervention. Two months later, she was fully recovered with no functional impairment of the affected foot. Timely local wound interventions could lead to a satisfactory outcome for severe peripheral intravenous infiltration with skin tears.


Subject(s)
Diabetes Mellitus, Type 2 , Pancreatitis , Acute Disease , Adult , Emergency Service, Hospital , Humans
4.
Analyst ; 146(5): 1596-1603, 2021 Mar 08.
Article in English | MEDLINE | ID: mdl-33475624

ABSTRACT

Ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid (5F) is a diterpenoid that is isolated and purified from the Chinese herbal medicine Pteris semipinnata L., and is known to exert antitumour activity in several kinds of malignant cancer cells by leading cancer cells to apoptosis. However, the antitumour effect of 5F in vivo is rarely reported due to the complexity of the physiological environment and limitations of 5F as a small anticancer drug. In the present study, we utilized FITC-doped nanoparticles for the accumulation and delivery of 5F in nasopharyngeal carcinoma CNE2 tumours transplanted in nude mice by the enhanced permeation and retention (EPR) effect. In vivo studies demonstrated that nanoparticles could efficiently deliver 5F in CNE2 transplanted tumours, and the tumour growth was effectively inhibited by the drug-loaded nanoparticles with minimal side effects. The study indicated the benefits of combining well-studied nanoparticles with traditional herbal medicine treatment and establishes a delivery platform for 5F chemotherapy.


Subject(s)
Nanoparticles , Nasopharyngeal Neoplasms , Animals , Diterpenes , Mice , Mice, Nude , Nasopharyngeal Carcinoma/drug therapy , Nasopharyngeal Neoplasms/drug therapy , Silicon Dioxide
5.
J Ethnopharmacol ; 266: 113453, 2021 Feb 10.
Article in English | MEDLINE | ID: mdl-33039628

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Banxia Baizhu Tianma decoction (BBTD) is a classical representative prescription for expelling phlegm, extinguishing wind, strengthening the spleen and dissipating excessive fluid in traditional Chinese medicine (TCM). According to both TCM theory and about 300 years of clinical practice, BBTD is especially suitable for hypertensive patients of abdominal obesity and lacking physical activity. AIM OF THE STUDY: The present study tried to interpret the pharmacology of the ancient formula of BBTD. Herein, we focused on the plasma metabonomics of BBTD and evaluated the effect and targets of BBTD on endothelial protective effect. METHODS: Obesity-related hypertensive mice were induced by high-fat diet for 20 weeks. BBTD (17.8 g/kg) was administered intragastrically for 8 weeks, and telmisartan group (12.5 mg/kg) was used as positive drug. Body weight, blood pressure, triglyceride and cholesterol were recorded to evaluate the efficacy of BBTD in vivo. Lipid deposition in aortic roots was assessed by oil red O staining, while morphology of aortas was observed by HE staining. Ultra performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) was performed to study the plasma non-targeted metabonomics. According to the data of metabonomics, human aortic endothelial cells (HAECs) were treated by oxidized low-density lipoprotein (ox-LDL, 50 µg/mL) with/without BBTD (2, 1 or 0.5 mg/mL). Apoptosis rate (Annexin V-FITC/PI), migration (Transwell), cytoskeleton (Phalloidin) and density of VE-cadherin (Immunofluorescence staining) were used to investigate the effect of BBTD in vitro. Transcriptome sequencing was performed (2 mg/mL BBTD vs ox-LDL) to screen the possible targets of BBTD in endothelial protection against ox-LDL. RESULTS: BBTD effectively reduced the body weight and total cholesterol, and decreased 12.1 mmHg in SBP and 10.5 mmHg in DBP of obesity-related hypertensive mice (P < 0.05). BBTD attenuated lipid deposition in arterial roots and improved the morphology of aortas in vivo. Plasma metabolite profiles identified 94 differential metabolites and suggested BBTD mainly affected glycerophospholipids and fatty acyls. Bioinformatics analysis indicated sphingolipid metabolism and fluid shear stress and atherosclerosis were main pathways. Therefore, we focused on endothelial protective effect of BBTD against ox-LDL. In vitro, BBTD demonstrated endothelial protective effects, decreasing apoptosis rate, improving cell migration in dose-dependent manner and maintaining cell morphology. Transcriptome sequencing identified 251 downregulated and 603 upregulated mRNAs after 24h-BBTD treatment, which reversed 51.8% change in mRNAs (393 DE mRNAs) induced by ox-LDL. Bioinformatics analysis supported the potential of BBTD in hypertension and suggested that BBTD improved endothelial cells by targeting mainly on p53 and PPAR signaling pathways. CONCLUSIONS: BBTD attenuates obesity-related hypertension by regulating metabolism of glycerophospholipids and endothelial protection.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Hypertension/drug therapy , Metabolomics , Obesity/prevention & control , Animals , Aorta/cytology , Aorta/drug effects , Apoptosis/drug effects , Cells, Cultured , Diet, High-Fat , Disease Models, Animal , Dose-Response Relationship, Drug , Drugs, Chinese Herbal/administration & dosage , Endothelial Cells/drug effects , Endothelial Cells/metabolism , Humans , Hypertension/complications , Hypertension/metabolism , Lipoproteins, LDL/administration & dosage , Male , Mice , Mice, Inbred C57BL , Obesity/etiology , Obesity/metabolism
6.
J Altern Complement Med ; 27(3): 225-237, 2021 Mar.
Article in English | MEDLINE | ID: mdl-33252246

ABSTRACT

Background: Coronavirus disease 2019 (COVID-19) has become a pandemic with no specific and widely accepted effective drug or vaccine. However, studies have shown that Traditional Chinese Medicine (TCM) may play a significant role as an auxiliary treatment for COVID-19. Objective: This study aimed to assess the effects of TCM as an auxiliary treatment for COVID-19 through a systematic review of randomized-controlled trials (RCTs). Methods: Four English and three Chinese language databases were searched from December 1, 2019, to June 30, 2020. RCTs comparing TCM in combination with Western medicine (WM) with the same WM therapies alone for confirmed COVID-19 patients were included. The outcome measures were cure rate, lowering of body temperature, cough relief, improvement in chest computed tomography (CT) images, deterioration of condition, and adverse effects. Methodological quality was assessed using the Cochrane risk-of-bias tool. A series of meta-analyses were conducted for selected outcomes using RevMan 5.3 software. The quality of evidence was appraised using the grading of recommendation, assessment, development, and evaluation (GRADE) recommendations. Results: Ten RCTs with a total of 1,285 patients were included. Compared with WM alone in treating COVID-19, WM with auxiliary treatment by TCM appears to have increased the cure rate (risk ratio [RR] 1.15 [95% confidence interval (CI) 1.04-1.26]), relieved cough (RR 1.32 [95% CI 1.15-1.52]), improved chest CT images (RR 1.23 [95% CI 1.11-1.37]), and reduced the number of cases transitioning from a moderate to severe condition (RR 0.58 [95% CI 0.43-0.77]). The authors are uncertain whether TCM combined WM has effects on fever normalization (RR 1.10 [95% CI 0.94-1.29]) or adverse effects (RR 0.81 (95% CI 0.42-1.57]). Although they evaluated the certainty of evidence for lowering body temperature and adverse effects as very low, and low for cure rate, certainty was evaluated as moderate for improvement in chest CT images, cough relief, and deterioration of condition. Conclusion: TCM may be an effective auxiliary treatment for COVID-19 patients, which is likely to help improve the main symptoms and reduce disease progression. However, due to the limited number of studies and apparent heterogeneity among them, a more definitive conclusion on the effect of TCM on lowering body temperature and adverse effects cannot be drawn at this time.


Subject(s)
COVID-19 Drug Treatment , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Adult , Aged , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/therapeutic use , Female , Humans , Male , Middle Aged , Pandemics , Randomized Controlled Trials as Topic , SARS-CoV-2 , Treatment Outcome
7.
Fitoterapia ; 142: 104501, 2020 Apr.
Article in English | MEDLINE | ID: mdl-32058050

ABSTRACT

A phytochemical investigation on the leaves of Tripterygium wilfordii Hook. F. was conducted, leading to the isolation of five undescribed dihydro-ß-agarofuran sesquiterpenoids (1-5) and one known analogue (6). Their structures were determined by comprehensive spectroscopic analyses. The absolute configurations of the compounds were determined by comparison of the experimental ECD with the calculated data. In addition, all the compounds were evaluated for their neuroprotective activities against H2O2-induced cell injury in human neuroblastoma SH-SY5Y cells, and 3 showed the better protective effect with 76.63% cell viability comparing with the positive control Trolox (69.84%) at 12.5 µM.


Subject(s)
Neuroprotective Agents/isolation & purification , Sesquiterpenes/chemistry , Tripterygium/chemistry , Cell Line, Tumor , Drug Evaluation, Preclinical , Humans , Neuroprotective Agents/chemistry , Plant Leaves/chemistry
8.
Chin J Integr Med ; 26(1): 46-53, 2020 Jan.
Article in English | MEDLINE | ID: mdl-31388973

ABSTRACT

OBJECTIVE: To evaluate the effects of combination of Radix Astragali (RA) and Radix Salviae Miltiorrhizae (RS) on kidney of spontaneously hypertensive rats (SHRs) and renal intrinsic cells. METHODS: SHRs were intragastrically administrated with RA (5.09 g/kg) and RS (2.55 g/kg) either alone or with combination for 4 weeks; valsartan (13.35 mg/kg) was used as a positive control. Blood pressure and renal ultrasonography were monitored periodically. The biomarkers [microalbumin (mALB), cystatin ^C, angiotensin II (Ang II), interleukin-1 beta (IL-1ß), and ß2-microglobulin (ß2-Mg), etc.] in serum and urine were measured by enzyme-linked immunosorbent assay (ELISA). The protein expressions [phosphorylated adenosine 5'-monophosphate-activated protein kinase-α1 (p-AMPKα1), sestrin-ß, calcium/calmodulin-dependent protein kinase kinase-ß (CaMKK-ß), phosphoinositide 3-kinases (PI3K), serine-threonine protein kinase 1 (AKT1), and vascular endothelial growth factor receptor 2 (VEGFR2)] in renal cortex were determined by Western blot. In vitro, the hypertensive cellular model was established by applying 2×10-6 mol/L Ang ^II. The primary human podocytes, human glomerular endothelial cells (HRGECs), and human proximal tubular epithelial cells (HK-2s) were pre-incubated with sulfotanshinone sodium (Tan, 10 µg/mL) and/or calycosin-7-O-ß-D-glucoside (Cal, 5 µg/mL). The cellular viability and apoptosis were assayed by 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and Annexin V/PI staining, respectively. The level of endothelial nitric oxide synthase (eNOS) in culture supernatant was determined by ELISA. RESULTS: RA+RS signifificantly decreased the diastolic blood pressure, renal vascular resistance index, and parenchymal thickness, increased 24 h urinary volume as well as lowered the levels of urine mALB and serum cystatin ^C, IL-1ß and ß2-Mg of SHRs (P <0.05 vs. SHRs). The decreased protein levels of p-AMPKα1, sestrinß and CaMKK-ß and the increased protein levels of PI3K, AKT1 and VEGFR2 in renal cortex of SHRs were normalized after RA+RS treatment (P <0.05). In vitro, Tan and Cal attenuated the Ang II-induced abnormal proliferation and increased the apoptosis of HRGECs and HK-2s and improved the level of eNOS in culture supernatant. Whereas, neither of them showed powerful effect on podocyte. CONCLUSION: The combination of RA and RS had potential effects on alleviating the renal damages of SHRs and the renoprotection was independent of blood pressure level.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Hypertension/drug therapy , Kidney/drug effects , Kidney/metabolism , Salvia miltiorrhiza/chemistry , Angiotensin II , Animals , Astragalus propinquus , Biomarkers/blood , Biomarkers/urine , Blotting, Western , Cells, Cultured , Kidney/cytology , Male , Nitric Oxide Synthase Type III/metabolism , Rats , Rats, Inbred SHR , Rats, Inbred WKY
9.
Chemistry ; 26(25): 5583-5591, 2020 May 04.
Article in English | MEDLINE | ID: mdl-31880368

ABSTRACT

As newly emerged crystalline porous materials, covalent organic frameworks (COFs) possess fascinating structures and some specific features such as modularity, crystallinity, porosity, stability, versatility, and biocompatibility. Besides adsorption/separation, sensing, catalysis, and energy applications, COFs have recently shown a promise in biomedical applications. This contribution provides an overview of the recent developments of COF-based medicines in cancer therapeutics, including drug delivery, photodynamic therapy (PDT), photothermal therapy (PTT), and combined therapy. Furthermore, the major challenges and developing trends in this field are also discussed. These recent developments are summarized and discussed to help encourage further contributions in this emerging and promising field.


Subject(s)
Metal-Organic Frameworks , Neoplasms/drug therapy , Photochemotherapy/methods , Adsorption , Catalysis , Humans , Porosity
10.
Fitoterapia ; 139: 104403, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31676396

ABSTRACT

Ailanthus altissima Swingle is a deciduous tree, belonging to the Simaroubaceae family. Phytochemical investigation of the root barks of A. altissima showed the presence of eight pairs of enantiomeric 8,4'-type oxyneolignans (1a/1b-8a/8b) including nine undescribed compounds (1b, 2a, 3a/3b, 4a/4b, 5b, 7b, 8a). Their structures were elucidated by comprehensive spectroscopic analyses, and their absolute configurations were determined by comparison of the experimental and quantum chemical calculations of electronic circular dichroism (ECD) curves. In addition, their neuroprotective effects against H2O2-induced oxidative stress in human neuroblastoma SH-SY5Y cells were investigated. Among them, 4a, 4b, and 8b exhibited moderate neuroprotective activity.


Subject(s)
Ailanthus/chemistry , Lignans/pharmacology , Neuroprotective Agents/pharmacology , Oxidative Stress/drug effects , Cell Line, Tumor , China , Humans , Hydrogen Peroxide , Lignans/isolation & purification , Molecular Structure , Neuroblastoma , Neuroprotective Agents/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Bark/chemistry , Plant Roots/chemistry , Stereoisomerism
11.
J Nat Prod ; 82(10): 2696-2706, 2019 10 25.
Article in English | MEDLINE | ID: mdl-31556299

ABSTRACT

Fifteen new dihydro-ß-agarofuran-type sesquiterpenoids, tripterfordins A-O, were obtained from the aqueous EtOH extracts of the leaves of Tripterygium wilfordii. These constituted a class of highly oxygenated tricyclic sesquiterpenoid polyesters with a cinnamoyloxy group at C-1. The assignments of their structures were conducted via extensive analyses of the spectroscopic data and comparison of experimental and calculated ECD data. The absolute configurations of compounds 1, 4, 9, and 10 were established via single-crystal X-ray diffraction data. Additionally, compounds 1, 4, 9, 10, and 13 exhibited pronounced inhibitory effects on nitric oxide production in RAW 264.7 murine macrophages stimulated by lipopolysaccharide with IC50 values ranging from 11.9 to 31.0 µM.


Subject(s)
Sesquiterpenes/isolation & purification , Tripterygium/chemistry , Animals , Mice , Nitric Oxide/biosynthesis , Plant Extracts/analysis , Plant Leaves/chemistry , RAW 264.7 Cells , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology
12.
Nat Prod Res ; 33(17): 2446-2452, 2019 Sep.
Article in English | MEDLINE | ID: mdl-29521116

ABSTRACT

Two new sesquineolignans, hawthornsesquinins K and L (1 and 2), were isolated from the seeds of Crataegus pinnatifida. Their structures were determined by spectroscopic analyses, including 1D, 2D NMR and HRESIMS data. All isolated compounds were tested for their ß-amyloid aggregation inhibitory activity and neuroprotective effects against H2O2-induced damage in SH-SY5Y cells. The results indicated that compound 1 showed prominent inhibition of Aß1-42 aggregation and significant neuroprotective effect on H2O2-induced cellular damage in SH-SY5Y cells.


Subject(s)
Amyloid beta-Peptides/antagonists & inhibitors , Crataegus/chemistry , Lignans/chemistry , Lignans/pharmacology , Neuroprotective Agents/pharmacology , Peptide Fragments/antagonists & inhibitors , Amyloid beta-Peptides/metabolism , Cell Line , Drug Evaluation, Preclinical/methods , Humans , Hydrogen Peroxide/toxicity , Magnetic Resonance Spectroscopy , Molecular Structure , Neurons/drug effects , Neurons/metabolism , Neuroprotective Agents/chemistry , Peptide Fragments/metabolism , Seeds/chemistry , Spectrometry, Mass, Electrospray Ionization
13.
J Cell Biochem ; 120(3): 4291-4300, 2019 03.
Article in English | MEDLINE | ID: mdl-30260039

ABSTRACT

Artemisinin (Art) is isolated from Artemisia annua L. and known as the most effective antimalaria drugs. Previous studies demonstrated that it could exert an immune-regulatory effect on autoimmune diseases. In this study, we first investigated its potential role in tubulointerstitial inflammation and fibrosis in rats with 5/6 nephrectomy. Subtotal nephrectomized (SNx) rats were orally administered Art (100 mg·kg -1 ·d - 1) for 16 weeks. Blood and urine samples were collected for biochemical examination. Kidney tissues were collected for immunohistochemistry and Western blot analyses. Ang II-induced injury of the human kidney 2 (HK-2) cells was used for in vitro study. It was shown that Art could significantly attenuate the renal function decline in SNx rats compared with control. More importantly, Art treatment significantly reduced the tubulointerstitial inflammation and fibrosis, as demonstrated by the evaluation of renal pathology. Furthermore, Art inhibited the activation of NLRP3 inflammasome and NF-κB in the kidneys. In in vitro study, Art pretreatment could significantly prevent the activation of NLRP3 inflammasome and NF-κB in Ang II-treated HK-2 cells, while BAY11-7082 (an inhibitor of NF-κB) significantly inhibited Ang II-induced NLRP3 inflammasome activation. This study suggested that Art could provide renoprotective role by attenuating the tubulointerstitial inflammation and fibrosis in SNx rats by downregulating the NF-κB/NLRP3 signaling pathway.


Subject(s)
Anti-Inflammatory Agents/therapeutic use , Artemisinins/therapeutic use , NF-kappa B/metabolism , NLR Family, Pyrin Domain-Containing 3 Protein/metabolism , Nephrectomy/adverse effects , Nephritis, Interstitial/drug therapy , Nephritis, Interstitial/etiology , Animals , Anti-Inflammatory Agents/pharmacology , Artemisia/chemistry , Artemisinins/pharmacology , Cell Line , Epithelial Cells/drug effects , Epithelial Cells/metabolism , Fibrosis , Humans , Inflammasomes/drug effects , Inflammasomes/metabolism , Kidney/cytology , Kidney/pathology , Male , Plant Extracts/therapeutic use , Rats , Rats, Sprague-Dawley , Signal Transduction/drug effects
14.
Bioorg Chem ; 80: 64-69, 2018 10.
Article in English | MEDLINE | ID: mdl-29883933

ABSTRACT

Four new dihydrobenzofuran neolignans 1a/1b and 2a/2b were isolated from the fruit of Rubus ideaus. 1a/1b and 2a/2b as two pairs of enantiomers were separated on a chiral chromatographic column. Their structures were determined using a suite of techniques including 1D and 2D NMR, HRESIMS, together with theoretical electronic circular dichroism (ECD) calculation. All compounds were evaluated for their inhibition of self-induced Aß1-42 aggregation. Compounds 1b and 2a exhibited optimal Aß1-42 aggregation inhibition capability, with an inhibition potency of 81.6% and 83.4% at 20 µM, respectively. Additionally, molecular docking was performed to identify the possible factor responsible for the enantioselectivity in the anti-Aß1-42 aggregation activity.


Subject(s)
Amyloid beta-Peptides/metabolism , Benzofurans/chemistry , Lignans/chemistry , Peptide Fragments/metabolism , Rubus/chemistry , Amyloid beta-Peptides/antagonists & inhibitors , Binding Sites , Circular Dichroism , Fruit/chemistry , Fruit/metabolism , Lignans/isolation & purification , Lignans/metabolism , Magnetic Resonance Spectroscopy , Molecular Conformation , Molecular Docking Simulation , Peptide Fragments/antagonists & inhibitors , Plant Extracts/chemistry , Protein Structure, Tertiary , Rubus/metabolism , Stereoisomerism
15.
Fitoterapia ; 128: 169-174, 2018 Jul.
Article in English | MEDLINE | ID: mdl-29787805

ABSTRACT

Seven new N-acylanthranilic acid derivatives (1-3, 4a/4b, 5a/5b) including two pairs of enantiomers (4a/4b and 5a/5b) were isolated from the leaves of Isatis indigotica Fortune. Their chemical structures were elucidated by extensive spectroscopic data analyses. The absolute configurations of compounds 4a/4b and 5a/5b were determined by comparison of the experimental and calculated ECD spectra. All compounds were tested for their anti-Aß1-42 aggregation activity. As a result, compounds 1 (72.1%), 2 (79.8%) and 5a (81.8%) showed stronger inhibitory activity than the positive control curcumin (67.0%). By the comparison between 5a (81.8%) and 5b (63.1%), it was found that stereochemical configurations may affect Aß1-42 aggregation activity, which was discussed through the molecular docking results of compounds 5a and 5b.


Subject(s)
Amyloid beta-Peptides/antagonists & inhibitors , Isatis/chemistry , Peptide Fragments/antagonists & inhibitors , Plant Leaves/chemistry , ortho-Aminobenzoates/isolation & purification , Molecular Docking Simulation , Stereoisomerism
16.
Phytochemistry ; 149: 132-139, 2018 May.
Article in English | MEDLINE | ID: mdl-29499466

ABSTRACT

Six undescribed alkaloids, indiforine A-F, together with four known ones, were isolated from the leaves of Isatis indigotica Fortune. Their structures were elucidated on the basis of extensive spectroscopic analyses. The absolute configurations of indiforine A and B were determined by comparison of the experimental and calculated electronic circular dichroism spectra, as well as experimental and calculated optical rotations. The isolated alkaloids were evaluated for their neuroprotective activities against H2O2-induced cell injury in human neuroblastoma SH-SY5Y cells. The results showed that in H2O2-induced SH-SY5Y cell injury models, indiforine A and B exhibited potent neuroprotective activities. Further investigation of the most potent indiforine A by Hoechst 33258 staining and Annexin V/PI analysis demonstrated that it could protect SH-SY5Y cells from oxidative damage through inhibiting cell apoptosis.


Subject(s)
Drugs, Chinese Herbal/isolation & purification , Drugs, Chinese Herbal/pharmacology , Indole Alkaloids/isolation & purification , Isatis/chemistry , Neuroprotective Agents/isolation & purification , Neuroprotective Agents/pharmacology , Plant Leaves/chemistry , Apoptosis/drug effects , China , Drugs, Chinese Herbal/chemistry , Humans , Hydrogen Peroxide/pharmacology , Indole Alkaloids/chemistry , Indole Alkaloids/pharmacology , Molecular Structure , Neuroprotective Agents/chemistry , Plant Roots/chemistry
17.
Fitoterapia ; 127: 301-307, 2018 Jun.
Article in English | MEDLINE | ID: mdl-29534982

ABSTRACT

Eight new phenylpropanoids (1a/1b, 2-4, 5a/5b and 6) including two pairs of enantiomers (1a/1b and 5a/5b), along with a known analogue (7) were isolated from the fruit of Crataegus pinnatifida. Their structures were elucidated using comprehensive spectroscopic methods. Compounds 1a/1b and 5a/5b were separated successfully by chiral chromatographic column. The absolute configurations of enantiomers were determined by comparison between the experimental and calculated electronic circular dichroism (ECD) spectra. The in vitro antitumor activities of the isolates were evaluated against two human hepatocellular carcinoma HepG2 and Hep3B cells. Five compounds (1a/1b, 2-4) exhibited more potent cytotoxicity and their structure-activity relationships were also discussed. Annexin V-FITC/PI staining using flow cytometry was carried out to examine cell apoptosis, and the results showed that compounds 3-4 with the presence of two methoxy groups substituted at C-3' significantly induced apoptosis in HepG2 cells.


Subject(s)
Apoptosis/drug effects , Crataegus/chemistry , Fruit/chemistry , Propanols/isolation & purification , Hep G2 Cells , Humans , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Propanols/pharmacology , Stereoisomerism
18.
Biol Trace Elem Res ; 185(2): 364-374, 2018 Oct.
Article in English | MEDLINE | ID: mdl-29468613

ABSTRACT

This study was conducted to investigate effects of dietary zinc oxide nanoparticles (nano-ZnOs) on growth, diarrhea rate, mineral deposition (Zn, Fe, and Mn), intestinal morphology, and barrier of weaned piglets. A total of 384 weaned piglets (Duroc × Landrace × Yorkshire) in 4 groups were fed a basal diet supplemented with 0, 400, and 800 mg/kg nano-ZnOs or 3000 mg/kg ZnO for 14 days. Compared with the control group, 800 mg/kg nano-ZnOs and 3000 mg/kg ZnO significantly increased average daily gain and decreased diarrhea rate of weaned piglets. There was no significant difference among ZnO and nano-ZnO groups. ZnO and nano-ZnOs did not affect serum activities of glutamic oxalacetic transaminase, glutamic-pyruvic transaminase, and lactate dehydrogenase. However, ZnO and 800 mg/kg nano-ZnOs significantly increased zinc concentrations in plasma, liver, pancreas, and tibia, without affecting Fe and Mn concentrations. Compared with the control group, 800 mg/kg nano-ZnOs significantly reduced plasma diamine oxidase activity, decreased total aerobic bacterial population in mesenteric lymph node, enhanced mRNA expressions of occludin, ZO-1, IL-1ß, IL-10, TNF-α, and ki67 in ileal mucosa, and increased villous height, width, crypt depth, and surface area. Compared to ZnO group, 800 mg/kg nano-ZnOs significantly decreased aerobic bacterial population, enhanced mRNA expressions of occludin, IL-1ß, IL-10, and TNF-α, and reduced fecal zinc concentration. These results indicated that 800 mg/kg nano-ZnOs might be a potential substitute for 3000 mg/kg ZnO in diets of weaned piglets.


Subject(s)
Diarrhea/drug therapy , Dietary Supplements , Intestines/anatomy & histology , Intestines/drug effects , Minerals/metabolism , Nanoparticles/chemistry , Zinc Oxide/pharmacology , Animals , Apoptosis/drug effects , Apoptosis/genetics , Cell Proliferation/drug effects , Cell Proliferation/genetics , Diarrhea/metabolism , Dose-Response Relationship, Drug , Intestinal Mucosa/anatomy & histology , Intestinal Mucosa/drug effects , Intestinal Mucosa/metabolism , Nanoparticles/administration & dosage , Particle Size , Swine , Weaning , Zinc Oxide/administration & dosage , Zinc Oxide/chemistry
19.
Fitoterapia ; 127: 56-61, 2018 Jun.
Article in English | MEDLINE | ID: mdl-29371160

ABSTRACT

Rubus ideaus L., a member of the Rosaceae family, is popular for its distinctive flavor and attractive red color. In order to explore the functional factors possibly presented in the fruit, seven new benzofuran neolignans (1a/1b-3a/3b and 4b), together with one known neolignan 4a, were isolated from the fruit of R. ideaus. Compounds 1a/1b-4a/4b as four pairs of enantiomers were separated on a chiral chromatographic column. Their structures including absolute configurations were elucidated by extensive spectroscopic data analyses, including UV, IR, HRESIMS, NMR, and comparing their experimental electronic circular dichroism (ECD) spectra with calculated ECD spectra. Additionally, all these enantiomeric compounds were evaluated for their antioxidant, neuroprotective, and anti-Aß1-42 aggregation activities.


Subject(s)
Benzofurans/chemistry , Fruit/chemistry , Lignans/chemistry , Rubus/chemistry , Amyloid beta-Peptides/chemistry , Cell Line, Tumor , Circular Dichroism , Free Radical Scavengers/chemistry , Humans , Magnetic Resonance Spectroscopy , Molecular Structure , Peptide Fragments/chemistry , Stereoisomerism
20.
Eur J Nutr ; 57(8): 2735-2745, 2018 Dec.
Article in English | MEDLINE | ID: mdl-28936696

ABSTRACT

PURPOSE: The present study investigated whether dietary methionine supplementation might protect against intrauterine growth retardation (IUGR)-induced damage in the intestine of piglets. METHODS: Thirty normal birth weight (NBW) female piglets and sixty same-sex IUGR piglets were weaned at 21 days of postnatal age and fed the control diet (4.0 g methionine per kg of feed, NBW-CON, and IUGR-CON groups) or the methionine-supplemented diet (5.2 g methionine per kg of feed, IUGR-MET group) for 28 days (n = 6). RESULTS: Piglets in the IUGR-CON group showed decreased average daily feed intake and average daily gain and an increased feed conversion ratio than those in the NBW-CON group. Compared with NBW-CON piglets, IUGR-CON piglets had decreased villus height (VH) and villus height-to-crypt depth ratio in both the jejunum and ileum. In addition, in comparison with the NBW-CON piglets, IUGR increased the concentration of malondialdehyde (MDA) and the index of apoptosis, while it decreased the concentrations of methionine and reduced glutathione (GSH), the ratio of reduced glutathione/oxidized glutathione (GSH/GSSG), and the protein expression of occludin (OCLN) in both the jejunum and ileum. Dietary methionine supplementation decreased the MDA and protein carbonyl concentrations and the apoptotic index, while it increased the VH level, methionine and GSH concentrations, GSH/GSSG ratio, and the OCLN protein expression in the jejunum of IUGR-MET piglets. CONCLUSIONS: Methionine may have beneficial effects in improving intestinal integrity and oxidative status in IUGR weanling piglets.


Subject(s)
Dietary Supplements , Fetal Growth Retardation/pathology , Intestinal Mucosa/physiology , Methionine/pharmacology , Oxidative Stress , Animal Feed , Animals , Apoptosis , Female , Gene Expression Regulation , Glutathione/metabolism , Male , Malondialdehyde/metabolism , Occludin/genetics , Occludin/metabolism , Oxidation-Reduction , Swine , Weaning
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