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ETHNOPHARMACOLOGICAL RELEVANCE: Corydalis decumbens (Thunb.) Pers. was used as stasis-eliminating medicine traditionally to treat cardiovascular disease potentially attributed to its antithrombotic effect, but lack of pharmacological research on it. AIM OF THE STUDY: To investigate the antithrombotic effect of C. decumbens and its preliminary mechanism. MATERIALS AND METHODS: A carrageenan-induced mouse thrombus model and adenosine diphosphate stimulated platelet aggregation of rabbits were used to confirm the inhibitory effect of C. decumbens extract and compounds on thrombosis in vivo. Then, H2O2-induced human umbilical vein endothelial cells (HUVECs) injury model was further adopted to verify the effects of bioactive compounds in vitro. Moreover, in silico network pharmacology analyses and molecular docking were performed to predict the underlying mechanisms, targets, and pathways, and which were further confirmed through western blotting assay. RESULTS: The administration of total extract (TE), total alkaloids (TA) and tetrahydropalmatine (TET) resulted in a significant reduction in black tail thrombus and congestion, along with a decreasing in platelet aggregation of rabbits. A superior antithrombotic effect indicated the bioactive fraction, and then the isolated bioactive compounds, TET and protopine (PRO) increased cell survival, and decreased reactive oxygen species (ROS) and lactate dehydrogenase (LDH) release in H2O2-induced HUVECs injury model. Moreover, the two alkaloids targeted 33 major proteins and influenced 153 pathways in network pharmacology prediction. Among these, HSP90AA1, COX-2, NF-κB/p65, MMP1 and HIF-1α were the key proteins and PI3K-Akt emerged as the major signaling pathway. Further western blotting results supported that five key proteins were downregulated by the two bioactive compounds in H2O2-stimulated HUVECs model. CONCLUSION: C. decumbens exerted protective effect on thrombosis through inhibiting PI3K-Akt pathway and related key proteins, which supported the traditional use and presented potential antithrombotic alkaloids for further investigation.
Subject(s)
Corydalis , Fibrinolytic Agents , Human Umbilical Vein Endothelial Cells , Plant Extracts , Proto-Oncogene Proteins c-akt , Signal Transduction , Thrombosis , Animals , Corydalis/chemistry , Rabbits , Humans , Human Umbilical Vein Endothelial Cells/drug effects , Proto-Oncogene Proteins c-akt/metabolism , Thrombosis/drug therapy , Plant Extracts/pharmacology , Mice , Signal Transduction/drug effects , Male , Fibrinolytic Agents/pharmacology , Phosphatidylinositol 3-Kinases/metabolism , Platelet Aggregation/drug effects , Molecular Docking Simulation , Berberine Alkaloids/pharmacology , Hydrogen Peroxide/toxicity , Disease Models, Animal , Carrageenan , Reactive Oxygen Species/metabolismABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: The roots and rhizomes of Bergenia purpurascens (Hook. f. et Thomson) Engl., was used as a sunscreen to protect against ultraviolet rays in Tibet of China historically, but its skin whitening constituents and pharmacological effects of this plant remained unknown. AIM OF THE STUDY: To investigate the anti-melanogenesis effect of B. purpurascens in vitro and in vivo, and then explore the preliminary mechanism. MATERIALS AND METHODS: An ultraviolet B (UVB)-induced skin injury model of mice was used to verify the ameliorative effect of B. purpurascens extract (BPE) on ultraviolet damage. Then, alpha-melanocyte stimulating hormone (α-MSH)-induced murine melanoma cell line (B16F10) melanin generation model was further adopted to approval the effects of BPE and its bioactive compound, cuscutin, in vitro. Moreover, α-MSH stimulated melanogenesis model in zebrafish was employed to confirm the anti-pigmentation effect of cuscutin. Then, proteins expressions associated with melanin production were observed using western blotting assay to explore preliminary mechanism. RESULTS: BPE inhibited UVB-induced mice injury and restored skin barrier function observably in vivo. BPE and cuscutin suppressed the overproduction of melanin in α-MSH induced B16F10 significantly, in which cuscutin exhibited better effect than well-known whitening agent α-arbutin at same 10 µg/mL concentration. Moreover, the pigmentation of zebrafish embryo was decreased by cuscutin. Finally, cuscutin showed significant downregulation of expressions of tyrosinase (TYR) and tyrosinase related protein-1 (TRP-1), TRP-2 and microphthalmia-associated transcription factor (MITF) in the melanogenic signaling pathway. CONCLUSION: B. purpurascens extract and its major bioactive constituent, cuscutin, showed potent anti-melanogenesis and skin-whitening effect by targeting TYR and TRP-2 proteins for the first time, which supported its traditional use.
Subject(s)
Melanoma, Experimental , Monophenol Monooxygenase , Animals , Mice , Melanins/metabolism , Zebrafish , alpha-MSH/pharmacology , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Microphthalmia-Associated Transcription Factor/metabolism , Cell Line, Tumor , Melanoma, Experimental/drug therapyABSTRACT
Introduction: The purpose of this study is to systematically evaluate the efficacy and safety of acupuncture combined with pelvic floor rehabilitation training in the treatment of postpartum stress urinary incontinence, and to promote the further promotion and application of acupuncture in the field of rehabilitation. Methods and analysis: Randomized controlled trials (RCTs) of acupuncture combined with pelvic floor rehabilitation in the treatment of postpartum stress urinary incontinence will be searched in PubMed, Web of Science (WOS), Cochrane Library, EMBASE, China National Knowledge Infrastructure (CNKI), Chinese Biomedical Literature Database (CBM), Wanfang (WF), and VIP databases. The clinical trial Registry (ClinicalTrials.gov and Chinese clinical trial Registry) will also be searched. The search period is limited to July 1, 2023, and the language limit of this systematic review is Chinese and English. The primary outcome is clinical effective rate. International Consultation on Incontinence Questionnaire-Short Form (ICI-Q-SF), 1-h pad test, pelvic floor muscle potential value, incidence of adverse events are secondary outcomes. A meta-analysis will be performed using RevMan 5.4 statistical software. If feasible, subgroup analysis and sensitivity analysis will be performed to address potential causes of inconsistency and heterogeneity. The risk of bias will be assessed using the approach recommended by Cochrane Handbook for Systematic Reviews of Interventions, and the quality of evidence will be assessed using GRADE. This Protocol has been developed in accordance with the guideline of Preferred Reporting Items for Systematic review and Meta-Analysis Protocols (PRISMA-P) 2015. Discussion: Acupuncture combined with pelvic floor rehabilitation training can effectively promote the rehabilitation of postpartum stress urinary incontinence patients, and provide a reference for the clinical application of integrated Chinese and Western medicine treatment in the field of rehabilitation. Systematic review registration: PROSPERO CRD42023455801.
ABSTRACT
Twelve lupanes including three new compounds named alstoscholarilups A-C (1: -3: ) were isolated from the leaves of Alstonia scholaris. Their structures were elucidated by spectroscopic analysis and ECD calculation. Structurally, compound 1: with a rare A ring-seco skeleton formed lactone and degraded C-3, while 2: with a 28-nor and 3: with a 29-nor-lupane skeleton supported the phytochemical diversity and novelty of the plant. Pharmacologically, compounds 4, 7: , and 10: reduced the serum uric acid (UA) levels of mice significantly.
ABSTRACT
BACKGROUND: As one of the most commonly used folk medicines in "Dai" ethno-medicine system, Alstonia scholaris (l.) R. Br. has also been used for treat "water related diseases", such as chronic kidney disease. However, few study was reported for it on the intervention of chronic glomerulonephritis (CGN). PURPOSE: To investigate the effect and potential mechanism of indole alkaloids from A. scholaris leaves in ICR mice with adriamycin nephropathy, as well as providing experimental evidence for the further application. METHODS: ICR Mice were selected for injections of adriamycin (ADR) to induce the CGN model and administered total alkaloids (TA) and four main alkaloids continuously for 42 and 28 days, respectively. The pharmacological effects were indicated by serum, urine, and renal pathological observations. The targets and pathways of indole alkaloids on CGN intervention were predicted using the network pharmacology approach, and the immortalized mice glomerular podocyte (MPC5) cells model stimulated by ADR was subsequently selected to further verify this by western blotting and RT-qPCR methods. RESULTS: TA and four major compounds dramatically reduced the levels of urinary protein, serum urea nitrogen (BUN), and creatinine (CRE) in ADR - induced CGN mice, while increasing serum albumin (ALB) and total protein (TP) levels as well as ameliorating kidney damage. Moreover, four alkaloids effected on 33 major target proteins and 153 pathways in the CGN, among which, PI3K-Akt as the main pathway, an important pathway for kidney protection by network pharmacology prediction, and then the four target proteins - HRAS, CDK2, HSP90AA1, and KDR were screened. As a result, Val-and Epi can exert a protective effect on ADR-stimulated MPC5 cells injury at a concentration of 50 µM. Furthermore, the proteins and RNA expression of HRAS, HSP90AA1, and KDR were down-regulated, and CDK2 was up-regulated after the intervention of Val-and Epi, which were supported by Western blotting and RT-qPCR. Additionally, Val-and Epi inhibited ROS production in the MPC5 cells model. CONCLUSION: This study is the first to confirm the potential therapeutic effect of alkaloids from A. scholaris on CGN. TA with major bioactive components (vallesamine and 19epi-scholaricine) could exert protective effects against the ADR-induced CGN by regulating four key proteins: HRAS, CDK2, HSP90AA1, and KDR of the PI3K-Akt pathway.
Subject(s)
Alkaloids , Alstonia , Glomerulonephritis , Mice , Animals , Mice, Inbred ICR , Phosphatidylinositol 3-Kinases , Proto-Oncogene Proteins c-akt , Indole Alkaloids/pharmacology , Alkaloids/pharmacology , Alkaloids/therapeutic use , Glomerulonephritis/chemically induced , Glomerulonephritis/drug therapyABSTRACT
The Ganoderma lucidum mushroom, which has been used as a traditional medicine in China for more than 2000 years, is a source of many interesting natural product. In this study, the five undescribed minor meroterpenoids baoslingzhines F-J (1-5), containing a dihydropyran moiety, were isolated as racemic mixtures from the fruiting bodies of G. lucidum. These substances were structurally and stereochemically characterized by using spectroscopic and computational methods. Chiral HPLC was employed to separate the (+)- and (-)-antipodes. A survey of the activities against kidney fibrosis showed that both enantiomers of baoslingzhines F-J inhibit expression of renal fibrosis-related proteins, including fibronectin, collagen I and É-SMA in TGF-ß1-induced rat kidney proximal tubular cells.
Subject(s)
Ganoderma , Reishi , Rats , Animals , Terpenes/chemistry , Ganoderma/chemistry , Molecular Structure , Fibrosis , Fruiting Bodies, Fungal/chemistryABSTRACT
Aggregation-induced emission luminogens (AIEgens) are of great importance in optoelectronics and biomedical fields. However, the popular design philosophy by combining rotors with traditional fluorophores limits the imagination and structural diversity of AIEgens. Inspired by the fluorescent roots of the medicinal plant Toddalia asiatica, we discovered two unconventional rotor-free AIEgens, 5-methoxyseselin (5-MOS) and 6-methoxyseselin (6-MOS). Interestingly, a slight structural difference of the coumarin isomers leads to completely contrary fluorescent properties upon aggregation in aqueous media. Further mechanism investigation indicates that 5-MOS forms different extents of aggregates with the assistance of protonic solvents, leading to electron/energy transfer, which is responsible for its unique AIE feature, i.e., reduced emission in aqueous media but enhanced emission in crystal. Meanwhile, for 6-MOS, the conventional restriction of the intramolecular motion (RIM) mechanism is responsible for its AIE feature. More interestingly, the unique water-sensitive fluorescence property of 5-MOS enables its successful application for wash-free mitochondria imaging. This work not only demonstrates an ingenious tactic to seek new AIEgens from natural fluorescent species but also benefits the structure design and application exploration of next-generation AIEgens.
ABSTRACT
BACKGROUND: Nonalcoholic fatty liver disease (NAFLD), peculiarly nonalcoholic steatohepatitis (NASH), has become the main cause of liver transplantation and liver-related death. However, the US Food and Drug Administration has not approved a specific medication for treating NASH. Neferine (NEF), a natural bisbenzylisoquinoline alkaloid separated from the traditional Chinese medicine Nelumbinis plumula, has a variety of pharmacological properties, especially on metabolic diseases. Nevertheless, the anti-NASH effect and mechanisms of NEF remain unclear. PURPOSE: This study aimed to investigate the amelioration of NEF on NASH and the potential mechanisms. STUDY DESIGN: HepG2 cells, hepatic stellate cells (HSCs) and high-fat diet (HFD)+carbon tetrachloride (CCl4) induced C57BL/6 mice were used to observe the effect of NEF against NASH and investigate the engaged mechanism. METHODS: HSCs and HepG2 cells stimulated by oleic acid (OA) were treated with NEF. C57BL/6 mice were fed with HFD+CCl4 to induce NASH mouse model and treated with or without NEF (5 mg/kg or 10 mg/kg, once daily, i.p) for 4 weeks. RESULTS: NEF significantly attenuated the accumulation of lipid droplets, intracellular triglyceride (TG) levels and hepatocytes apoptosis in OA-exposed HepG2 cells. NEF not only enhanced the AMPK and ACC phosphorylation in OA-stimulated HepG2 cells, but also reduced inflammatory response and fibrosis in lipopolysaccharide (LPS)-stimulated HepG2 and in LX-2, respectively. In HFD+CCl4-induced NASH mice, pathological staining confirmed NEF treatment mitigated hepatic lipid deposition, inflammatory cell infiltration as well as hepatic fibrosis. Furthermore, the liver weight, serum and hepatic TG and total cholesterol (TC) and aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were decreased compared with the model group. HFD+CCl4 also induced the upregulation of specific proteins and genes associated to inflammation (ILs, TNF-α, NLRP3, ASC, CCL2 and CXCL10) and hepatic fibrosis (collagens, α-SMA, TGF-ß and TIPM1), which were also suppressed by NEF treatment. CONCLUSION: Our results demonstrated that NEF played a protective role in hepatic steatosis via the regulation of AMPK pathways, which may serve as an attractive candidate for a potential novel strategy on prevention and treatment of NASH.
Subject(s)
Benzylisoquinolines , Non-alcoholic Fatty Liver Disease , Mice , Animals , Non-alcoholic Fatty Liver Disease/drug therapy , AMP-Activated Protein Kinases/metabolism , Mice, Inbred C57BL , Liver , Benzylisoquinolines/pharmacology , Liver Cirrhosis/drug therapy , Diet, High-FatABSTRACT
Zanthoxylum plants (ZPs), including multiple Chinese prickly ash species, are dual-purpose functional foods favored by the general population around the world in foods, cosmetics, and traditional medicines and have antipruritic, insecticidal, and fungicidal bioactivities. For the first time, the anti-roundworm bioactivity of ZPs and the active ingredients were compared and investigated. Through nontarget metabolomics following targeted quantitative analysis, qinbunamides, sanshools, sanshooel, asarinin, and sesamin were found to be the main different components of Zanthoxylum species. Coincidentally, the 12 chemical components were also the dominant anti-roundworm ingredients of ZP extracts. The extracts of three species of Chinese prickly ash (1 mg/mL) decreased the hatchability of roundworm eggs significantly, and the ChuanJiao seed killed roundworms (insecticidal rate 100%) and alleviated the symptoms of pneumonia in mice. Furthermore, retention time-accurate mass-tandem mass spectrometry-ion ratio (RT-AM-MS/MS-IR) were modeled by assaying 108 authentic compounds of ZP extracts, and 20 metabolites were confidently identified in biological samples from ZP extract-treated mice by analyzing the m/z values and the empirical substructures. This study provides a good reference for the proper application of ZPs.
Subject(s)
Lignans , Zanthoxylum , Humans , Mice , Animals , Zanthoxylum/chemistry , Tandem Mass Spectrometry , Lignans/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , PhytochemicalsABSTRACT
Two unique windmill-like aziridine-containing indole alkaloids, possessing an unprecedented 6/5/5/6/6/5/3 rigid ring system and an unusual azabicyclo[3.1.0]hexane core, were isolated from Alstonia scholaris. Their structures were established by spectroscopy, X-ray diffraction, and electronic circular dichroism calculations. The novel compounds exhibited significant anti-inflammatory bioactivity in vitro and alleviated LPS-induced acute lung injury in mice.
Subject(s)
Alstonia , Plants, Medicinal , Mice , Animals , Alstonia/chemistry , Indole Alkaloids , Anti-Inflammatory Agents , X-Ray Diffraction , Molecular Structure , Plant Leaves/chemistryABSTRACT
Benign prostatic hyperplasia (BPH) is a chronic disease that affects the quality of life of older males. Sinomenine hydrochloride (SIN) is the major bioactive alkaloid isolated from the roots of the traditional Chinese medicinal plant Sinomenium acutum Rehderett Wilson. We wondered if the SIN administration exerted a regulatory effect on BPH and its potential mechanism of action. Mice with testosterone propionate-induced BPH subjected to bilateral orchiectomy were employed for in vivo experiments. A human BPH cell line (BPH-1) was employed for in vitro experiments. SIN administration inhibited the proliferation of BPH-1 cells (p < 0.05) by regulating the expression of androgen-related proteins (steroid 5-alpha reductase 2 (SRD5A2), androgen receptors, prostate-specific antigen), apoptosis-related proteins (B-cell lymphoma 2 (Bcl-2), Bcl-2-associated X protein (Bax)) and proliferation-related proteins (proliferating cell nuclear antigen (PCNA), mammalian target of rapamycin, inducible nitric oxide synthase) in vitro. SIN administration decreased the prostate-gland weight coefficient (p < 0.05) and improved the histological status of mice suffering from BPH. The regulatory effects of SIN administration on SRD5A2, an apoptosis-related protein (Bcl-2), and proliferation-related proteins (PCNA, matrix metalloproteinase-2) were consistent with in vitro data. SIN exerted a therapeutic effect against BPH probably related to lowering the SRD5A2 level and regulating the balance between the proliferation and apoptosis of cells. Our results provide an important theoretical basis for the development of plant medicines for BPH therapy.
Subject(s)
Prostatic Hyperplasia , Animals , Humans , Male , Mice , Apoptosis , Cell Proliferation , Cholestenone 5 alpha-Reductase/metabolism , Matrix Metalloproteinase 2 , Membrane Proteins , Plant Extracts/pharmacology , Proliferating Cell Nuclear Antigen , Prostatic Hyperplasia/drug therapy , Prostatic Hyperplasia/metabolism , Proto-Oncogene Proteins c-bcl-2/metabolism , Quality of Life , Testosterone/pharmacologyABSTRACT
Veratrazine A (1), a steroidal alkaloid with a unique 6/5/5 triheterocyclic scaffold as the side chain, was isolated from Veratrum stenophyllum, and its structure was established via spectroscopic analyses and X-ray diffraction. A plausible biosynthetic pathway for 1 is proposed. Bioassy exhibits moderate anti-inflammatory activities in vitro and in vivo.
Subject(s)
Alkaloids , Antineoplastic Agents , Veratrum , Alkaloids/pharmacology , Alkaloids/chemistry , Plant Extracts/chemistry , Veratrum/chemistry , Steroids/pharmacology , Anti-Inflammatory Agents , Molecular StructureABSTRACT
Four novel epimeric meroterpenoids, ganadone A (1), 3',10'-di-epi-ganadone A (2), 10'-epi-ganadone A (3), and 3'-epi-ganadone A (4) as well as another pairs of epimers, ganadone B (5) and 10'-epi-ganadone B (6), with a same basic skeleton compound ganadone C (7), together with two lactonized meroterpenoids, ganadones D and E (8 and 9) were isolated from the fruiting bodies of Ganoderma cochlear. Compounds 1-7 were constructed with fascinating adjacent 6',7'-bifuran ring system. Fortunately, we have revised our previously reported structure cochlearol Q, which was proposed pyrano[6',7'-b]pyran ring system into 6',7'-bifuran motif. All the isolates were characterized by analysis of HRESIMS, NMR spectroscopy and 1 was supported by X-ray crystallography analysis. The absolute stereochemistry of 1-9 were assigned by quantum chemical calculations. Biological evaluation of 1-9 showed that 5, 6, and 9 have significant anti-inflammatory potentials.
Subject(s)
Ganoderma , Terpenes , Terpenes/chemistry , Molecular Structure , Cyclooxygenase 2 , Fruiting Bodies, Fungal/chemistry , Ganoderma/chemistryABSTRACT
The concept of ethnic medicine is divided into a broad sense and a narrow sense. The broad concept refers to the traditional medicine of the Chinese nation, and the narrow concept refers to the traditional medicine of Chinese ethnic minorities. The external medicine is one of the main forms of ethnic medicine, and it is also the important content of ethnic medicine for external use, which is widely used in clinical practice. As the theory of ethnic medicine is unique, the application methods have certain characteristics, which are the key technical parts of clinical practice. However, the existing traditional Chinese medicine consensus formulation me-thods cannot meet the needs of the consensus formulation of the external ethnic medicine. Therefore, the methods suitable for expert consensus on external ethnic medicine are required. This article took Expert opinion on clinical application of Baimai Ointment as an exa-mple, and explorde a reasonable, effective, multi-dimensional, and multi-stage method to formulate expert consensus on the external ethnic medicine. In this research, three-dimensional sources of information, including ancient classics, clinical research evidence, and expert application experiences, were systematically and scientifically collected. After organization and analysis, the information was formed into comprehensive evidence. In a formal consensus meeting, part of the recommendations reached consensus. As to the issues that did not reach agreement, in-depth interviews were used to explore the reasons for the differences and resolve the disagreements. Finally, unanimous recommendations were reached. There are common problems during the formulation process of Expert opinion on clinical application of Baimai Ointment. This study is expected to provide references for the formulation of expert consensus on other external ethnic medicine.
Subject(s)
Humans , Biological Products , Consensus , Drugs, Chinese HerbalABSTRACT
Objective:To re-evaluate the reliability of the conclusions of the systematic reviews (SR)/meta-analysis (MA) of Traditional Chinese Medicine (TCM) in the treatment of functional dyspepsia (FD).Methods:CNKI, CBM, WanFang Data, VIP, PubMed, Cochrane Library, and Embase were searched from the establishment of the database to March 30, 2022. Two researchers independently screened literature and extracted data, and included SRs/MAs in the treatment of FD with TCM. The AMSTAR 2 and GRADE tools were used to evaluate the included the study carried out methodological quality evaluation, outcome evidence quality grading, and descriptive analysis of the main outcome.Results:A total of 28 SRs/MAs were included, with 34 outcome indicators. According to the AMSTAR 2 evaluation results, 21 SRs/MAs were of medium quality, and 7 SRs/MAs were of low quality. The GRADE quality of evidence grading results showed that of the 100 evidence bodies, 13 were of high quality, 58 were of moderate quality, 24 were of low quality, and 5 were of very low quality.Conclusion:TCM in the treatment of FD can improve the clinical efficiency, improve the cure rate, reduce the recurrence rate, and improve the clinical symptoms, but the methodological quality and evidence quality of related SRs/MAs have certain defects, so this conclusion should be treated with caution.
ABSTRACT
Objective: To investigate the effect of oxidative stress caused by heat exposure on the blood pressure increase of treadmill rats and the intervention of antioxidants. Methods: In June 2021, Twenty-four healthy SD male rats were randomly divided into four groups: normal temperature feeding, normal temperature treadmill, high temperature treadmill and high temperature treadmill supplementation with vitamin C groups, 6 rats in each group. The rats run on the platform in normal temperature or heat exposure environment for 30 min in the morning and in the afternoon daily, 6 days per week. The daily vitamin C supplement dose of high temperature treadmill supplementation with vitamin C group was 10 mg/kg. BP recordings were done at the end of the week. The rat vascular lipofuscin (LF) was detected by ELISA, the rat serum nitric oxide (NO) was detected by nitrate reductase method, the serum malondialdehyde (MDA) was detected by thibabituric acid method, the serum glutathione peroxidase (GPx) and superoxide dismutase (SOD) were detected by chemiluminescence method, and the serum catalase (CAT) was detected by ammonium molybdate method. The total antioxidant capacity (T-AOC) of serum was measured by iron reduction/antioxidant capacity method, and the content of nuclear erythroid 2-related factor 2 (Nrf2) in vascular tissue was measured by Western blot. The intra-group mean was compared by repeated measurement analysis of variance, and the inter-group mean was compared by single-factor analysis of variance and post-event LSD-t test. Results: Compared with the previous time point, the systolic BP and diastolic BP of the high temperature treadmill group were significantly increased at 7, 14 and 21 d, and decreased at 28 d which were higher than the initial level (P<0.05), and the systolic BP and diastolic BP values at each experimental time point were significantly higher than those of normal temperature treadmill group (P<0.001). The changes of thickening of the artery wall, no smoothing of the endodermis and irregular arrangement of muscle cells in high temperature treadmill group were observed. Compared with the normal temperature treadmill group, the content of MDA in serum, and LF in vascular tissue were significantly increased, the activities of SOD, CAT, T-AOC, the content of NO in serum, and the expression of Nrf2 in vascular tissue were significantly decreased in high temperature treadmill group (P<0.05). Compared with the high temperature treadmill group, the systolic BP and diastolic BP values at 7, 14, 21 and 28 d, the content of serum MDA and LF in vascular tissue were significantly decreased, the activities of CAT and T-AOC, and the expression of Nrf2 in vascular tissue significantly increased (P<0.05), the histopathological changes of the artery wall improved in high temperature treadmill supplementation with vitamin C group. Conclusion: Heat exposure has effect on oxidative stress, which may be related to the increase of BP. Vitamin C as an anti-oxidative enhancer can prevent those negative effects, which could alleviate the pathological changes of vessel intima in heat-exposed rats. And the Nrf2 may be a regulated factor to vascular protection.
Subject(s)
Male , Animals , Rats , Ascorbic Acid , Antioxidants/pharmacology , Blood Pressure , Hot Temperature , NF-E2-Related Factor 2 , Oxidative Stress , FeverABSTRACT
The basic constituent elements of ancient acupuncture prescriptions and moxibustion prescriptions for migraine and headache are extracted and summarized. The frequency and proportion of each element are counted and its characteristics are analyzed. The basic constituent elements of ancient acupuncture and moxibustion prescriptions includes five aspects: disease symptoms (main symptoms, concurrent symptoms, etiology and pathogenesis), disease type, acupuncture and moxibustion site (acupoint name, site name, meridian name), manipulation method (acupuncture method, reinforcing and reducing method, blood pricking method, moxibustion method) and curative effect. Acupuncture and moxibustion prescriptions are essential for recording the disease symptoms, while the acupuncture and moxibustion site and manipulation methods are the two core elements of ancient acupuncture and moxibustion prescriptions, which are also the premise to ensure that acupuncture and moxibustion prescriptions have good reference value.
Subject(s)
Humans , Moxibustion , Acupuncture Therapy , Meridians , Acupuncture Points , Headache/therapy , Migraine Disorders/therapyABSTRACT
Viscum coloratum (Kom.) Nakai is a well-known medicinal plant. However, the optimal harvest time for V. coloratum is unknown. Few studies were performed to analyze compound variation during storage and to improve post-harvest quality control. Our study aimed to comprehensively evaluate the quality of V. coloratum in different growth stages, and determine the dynamic variation of metabolites. Ultra-performance liquid chromatography tandem mass spectrometry was used to quantify 29 compounds in V. coloratum harvested in six growth periods, and the associated biosynthetic pathways were explored. The accumulation of different types of compounds were analyzed based on their synthesis pathways. Grey relational analysis was used to evaluate the quality of V. coloratum across different months. The compound variation during storage was analyzed by a high-temperature high-humidity accelerated test. The results showed that the quality of V. coloratum was the hightest in March, followed by November, and became the lowest in July. During storage, compounds in downstream steps of the biosynthesis pathway were first degraded to produce the upstream compounds and some low-molecular-weight organic acids, leading to an increase followed by a decrease in the content of some compounds, and resulted in a large gap during the degradation time course among different compounds. Due to the rapid rate and large degree of degradation, five compounds were tentatively designated as "early warning components" for quality control. This report provides reference for better understanding the biosynthesis and degradation of metabolites in V. coloratum and lays a theoretical foundation for rational application of V. coloratum and better quality control of V. coloratum during storage.
Subject(s)
Viscum/chemistry , Plants, Medicinal/chemistry , Chromatography, Liquid , Mass Spectrometry , MetabolomicsABSTRACT
Baoslingzhines A-E (1-5), five new meroterpenoids were isolated from the fruiting bodies of Ganoderma lucidum. The structures including their absolute configurations were characterized by using spectroscopic and computational methods. Compound 1 is a novel trinormeroterpenoid featuring the presence of an unusual dihydronaphthalene representing an unprecedented meroterpenoid skeleton. Compounds 2-4 are mononormeroterpenoids characteristic of a large conjugated system. Among them, racemic 3 and 4 were separated by HPLC on chiral phase. Biological evaluation toward kidney fibrosis found that compounds 2 and (+)-3 could inhibit the expression of fibronectin and collagen I dose dependently in TGF-ß1-induced rat kidney proximal tubular cells (NRK-52e). Additionally, (+)-3 could also down regulate É-SMA in a concentration dependent manner. Further investigation showed that 2 could inhibit Smad2 phosphorylation.
Subject(s)
Ganoderma , Reishi , Animals , Fibrosis , Ganoderma/chemistry , Molecular Structure , Rats , Terpenes/chemistry , Terpenes/pharmacology , Transforming Growth Factor beta1/pharmacologyABSTRACT
Ganoderma mushrooms are a renowned Chinese medicine and functional food used worldwide. Seven undescribed spiro Ganoderma meroterpenoids spiroganodermaines A-G were isolated from Ganoderma species. Their structures were characterized by using spectroscopic, computational and X-ray diffraction methods. Biological studies showed that (+)-spiroganodermaine G significantly activates glucose uptake and IRS1 phosphorylation in insulin resistance C2C12 cells. Furthermore, (-)-spiroganodermaine G inhibits the expressions of fibronectin and α-SMA in TGF-ß1 induced NRK-52E cells. These findings demonstrate the potential of Ganoderma meroterpenoids as medicines and dietary supplements.