RESUMO
Dragon's Blood (DB) serves as a precious Chinese medicine facilitating blood circulation and stasis dispersion. Daemonorops draco (D. draco; Qi-Lin-Jie) and Dracaena cochinchinensis (D. cochinchinenesis; Long-Xue-Jie) are two reputable plant sources for preparing DB. This work was designed to comprehensively characterize and compare the metabolome differences between D. draco and D. cochinchinenesis, by integrating liquid chromatography/mass spectrometry and untargeted metabolomics analysis. Offline two-dimensional liquid chromatography/ion mobility-quadrupole time-of-flight mass spectrometry (2D-LC/IM-QTOF-MS), by utilizing a powerful hybrid scan approach, was elaborated for multicomponent characterization. Configuration of an XBridge Amide column and an HSS T3 column in offline mode exhibited high orthogonality (A0 0.80) in separating the complex components in DB. Particularly, the hybrid high-definition MSE-high definition data-dependent acquisition (HDMSE-HDDDA) in both positive and negative ion modes was applied for data acquisition. Streamlined intelligent data processing facilitated by the UNIFI™ (Waters) bioinformatics platform and searching against an in-house chemical library (recording 223 known compounds) enabled efficient structural elucidation. We could characterize 285 components, including 143 from D. draco and 174 from D. cochinchinensis. Holistic comparison of the metabolomes among 21 batches of DB samples by the untargeted metabolomics workflows unveiled 43 significantly differential components. Separately, four and three components were considered as the marker compounds for identifying D. draco and D. cochinchinenesis, respectively. Conclusively, the chemical composition and metabolomic differences of two DB resources were investigated by a dimension-enhanced analytical approach, with the results being beneficial to quality control and the differentiated clinical application of DB.
Assuntos
Quimiometria , Metaboloma , Extratos Vegetais , Espectrometria de Massas , Cromatografia Líquida , Cromatografia Líquida de Alta Pressão/métodosRESUMO
Chebulae Fructus (CF) is known as one of the richest sources of hydrolyzable tannins (HTs). In this study, ultra-performance liquid chromatography coupled with a photodiode array detector method was established for simultaneous determination of the 12 common phenolcarboxylic and tannic constituents (PTCs). Using this method, quantitative analysis was accomplished in CF and other four adulterants, including Terminaliae Belliricae Fructus, Phyllanthi Fructus, Chebulae Fructus Immaturus, and Canarii Fructus. Based on a quantitative analysis of the focused compounds, discrimination of CF and other four adulterants was successfully accomplished by hierarchical cluster analysis and principal component analysis. Additionally, the total contents of the 12 compounds that we focused on in this study were unveiled as 148.86 mg/g, 96.14 mg/g, and 18.64 mg/g in exocarp, mesocarp, and endocarp and seed of CF, respectively, and PTCs were witnessed to be the most abundant in the exocarp of CF. Noticeably, the HTs (chebulagic acid, chebulanin acid, chebulinic acid, and punicalagin) were observed to be ultimately degraded to chebulic acid, gallic acid, and ellagic acid during sunlight-drying of the fresh fruits. As a result, our study indicated that CF and its adulterants could be distinguished by the observed 12 PTCs, which were mainly distributed in the exocarp of the fruits. The HTs were prone to degrade into the three simple phenolcarboxylic acids during drying or processing, allowing us to obtain a more comprehensive understanding of the PTCs, with great significance in the improved quality of CF and related products.
Assuntos
Frutas , Taninos Hidrolisáveis , Taninos Hidrolisáveis/química , Taninos Hidrolisáveis/análise , Frutas/química , Cromatografia Líquida de Alta Pressão , Terminalia/química , Taninos/análise , Taninos/química , Extratos Vegetais/química , Extratos Vegetais/análiseRESUMO
The microglia, displaying diverse phenotypes, play a significant regulatory role in the development, progression, and prognosis of Parkinson's disease. Research has established that glycolytic reprogramming serves as a critical regulator of inflammation initiation in pro-inflammatory macrophages. Furthermore, the modulation of glycolytic reprogramming has the potential to reverse the polarized state of these macrophages. Previous studies have shown that Levistilide A (LA), a phthalide component derived from Angelica sinensis, possesses a range of pharmacological effects, including anti-inflammatory, antioxidant, and neuroprotective properties. In our study, we have examined the impact of LA on inflammatory cytokines and glucose metabolism in microglia induced by lipopolysaccharide (LPS). Furthermore, we explored the effects of LA on the AMPK/mTOR pathway and assessed its neuroprotective potential both in vitro and in vivo. The findings revealed that LA notably diminished the expression of M1 pro-inflammatory factors induced by LPS in microglia, while leaving M2 anti-inflammatory factor expression unaltered. Additionally, it reduced ROS production and suppressed IκB-α phosphorylation levels as well as NF-κB p65 nuclear translocation. Notably, LA exhibited the ability to reverse microglial glucose metabolism reprogramming and modulate the phosphorylation levels of AMPK/mTOR. In vivo experiments further corroborated these findings, demonstrating that LA mitigated the death of TH-positive dopaminergic neurons and reduced microglia activation in the ventral SNpc brain region of the midbrain and the striatum. In summary, LA exhibited neuroprotective benefits by modulating the polarization state of microglia and altering glucose metabolism, highlighting its therapeutic potential.
Assuntos
Compostos Heterocíclicos de Anel em Ponte , Fármacos Neuroprotetores , Doença de Parkinson , Humanos , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/metabolismo , NF-kappa B/metabolismo , Fármacos Neuroprotetores/uso terapêutico , Microglia , Lipopolissacarídeos/farmacologia , Proteínas Quinases Ativadas por AMP/metabolismo , Reprogramação Metabólica , Anti-Inflamatórios/uso terapêutico , Serina-Treonina Quinases TOR/metabolismo , Glucose/metabolismoRESUMO
The objective was to report a relatively rare case of fulminant type 1 diabetes (FT1DM) complicated with acute pancreatitis (AP), to summarize the characteristics as well as experience of diagnosis and treatment, and to explore its pathogenesis. Clinical data of a case of FT1DM complicated with AP in the Department of Endocrinology of our hospital were analyzed retrospectively. A 66-year-old male presented with acute fever and abdominal pain, accompanying with the significantly elevated pancreatic enzymes, and his abdominal CT scan showed exudation around the pancreas. The clinical manifestations mentioned above were consistent with the diagnosis of AP. Five days after onset, the patient developed clinical symptoms, such as obvious thirst, polyuria, polyasthenia and fatigue. Meanwhile, his plasma glucose increased significantly and the diabetic ketoacidosis (DKA) occurred. The patient's fasting and postprandial 2 hours C peptide decreased significantly (all 0.02 µg/L), glycated hemoglobin level was not high (6%), and his islet-related autoantibodies were undetectable. Thus, the patient could be diagnosed with FT1DM. After the treatment of fasting, fluid replacement, anti-infection, somatostatin, anticoagulation and intravenous insulin sequential subcutaneous insulin pump, the patient gained the alleviation of pancreatitis, restoration of oral intake, and relatively stable blood glucose levels. Summarizing the characte-ristics of this case and reviewing the literature, FT1DM complicated with AP was relatively rare in FT1DM. Its common characteristics were described below: (1) Most cases started with AP and the blood glucose elevated within 1 week, or some cases had the simultaneously onset of AP and FT1DM. (2) The clinical course of AP was short and relieved no more than 1 week; Pancreatic imaging could completely return to normal within 1 to 4 weeks after onset. (3) The etiology of AP most was idiopathic; The elevation of pancreatic enzyme level was slight and the recovery was rapidly compared with AP of other etiologies. FT1DM could be complicated with AP, which was different from the physiological manifestations of pancreatic disease in general FT1DM patients. Virus infection mignt be the common cause of AP and FT1DM, and AP might be the early clinical manifestation of some FT1DM. The FT1DM patients developed with abdominal pain was easy to be missed, misdiagnosed and delayed, which should receive more attention in clinic.
Assuntos
Diabetes Mellitus Tipo 1 , Pancreatite , Humanos , Masculino , Diabetes Mellitus Tipo 1/complicações , Idoso , Pancreatite/complicações , Pancreatite/etiologia , Pancreatite/diagnóstico , Doença Aguda , Cetoacidose Diabética/complicaçõesRESUMO
Maternal overnutrition can dramatically increase the susceptibility of offspring to metabolic diseases, whereas maternal exercise may improve glucose metabolism in offspring. However, the underlying mechanism programming the intergenerational effects of maternal exercise on the benefits of glucose metabolism has not been fully elaborated. C57BL/6 female mice were randomly assigned to four subgroups according to a diet and exercise paradigm before and during pregnancy as follows: NC (fed with normal chow diet and sedentary), NCEx (fed with normal chow diet and running), HF (fed with high-fat diet and sedentary), and HFEx (fed with high-fat diet and running). Integrative 16S rDNA sequencing and mass spectrometry-based metabolite profiling were synchronously performed to characterize the effects of maternal exercise on the gut microbiota composition and metabolite alterations in offspring. Maternal exercise, acting as a natural pharmaceutical intervention, prevented deleterious effects on glucose metabolism in offspring. 16S rDNA sequencing revealed remarkable changes in the gut microbiota composition in offspring. Metabolic profiling indicated multiple altered metabolites, which were enriched in butanoate metabolism signaling in offspring. We further found that maternal exercise could mediate gene expression related to intestinal gluconeogenesis in offspring. In conclusion, our study indicated that maternal running significantly improved glucose metabolism in offspring and counteracted the detrimental effects of maternal high-fat feeding before and during pregnancy. We further demonstrated that maternal voluntary wheel running could integratively program the gut microbiota composition and fecal metabolite changes and then regulate butanoate metabolism and mediate intestinal gluconeogenesis in offspring.
Assuntos
Microbioma Gastrointestinal , Camundongos , Gravidez , Animais , Feminino , Atividade Motora , Camundongos Endogâmicos C57BL , Dieta Hiperlipídica/efeitos adversos , Glucose/metabolismo , HomeostaseRESUMO
Cyperus rotundus L. has been widely used in the treatment and prevention of numerous diseases in traditional systems of medicine around the world, such as nervous, gastrointestinal systems diseases and inflammation. In traditional Chinese medicine (TCM), its rhizomes are frequently used to treat liver disease, stomach pain, breast tenderness, dysmenorrheal and menstrual irregularities. The review is conducted to summarize comprehensively the plant's vernacular names, distribution, phytochemistry, pharmacology, toxicology and analytical methods, along with the data mining for TCM prescriptions containing C. rotundus. Herein, 552 compounds isolated or identified from C. rotundus were systematically collated and classified, concerning monoterpenoids, sesquiterpenoids, flavonoids, phenylpropanoids, phenolics and phenolic glycosides, triterpenoids and steroids, diterpenoids, quinonoids, alkaloids, saccharides and others. Their pharmacological effects on the digestive system, nervous system, gynecological diseases, and other bioactivities like antioxidant, anti-inflammatory, anti-cancer, insect repellent, anti-microbial activity, etc. were summarized accordingly. Moreover, except for the data mining on the compatibility of C. rotundus in TCM, the separation, identification and analytical methods of C. rotundus compositions were also systematically summarized, and constituents of the essential oils from different regions were re-analyzed using multivariate statistical analysis. In addition, the toxicological study progresses on C. rotundus revealed the safety property of this herb. This review is designed to serve as a scientific basis and theoretical reference for further exploration into the clinical use and scientific research of C. rotundus. Supplementary Information: The online version contains supplementary materials available at 10.1007/s11101-023-09870-3.
RESUMO
Chemical investigation on the water-soluble constituents of Stemona tuberosa Lour. resulted in the isolation of a previously undescribed furfural derivative namely (S)-5-((R)-hydroxy(5-(hydroxymethyl)furan-2-yl)methyl)-5-methylfuran-2(5H)-one and twenty-five known compounds from the water decoction of the dried root tubers. Their structures were determined by analysis of the extensive spectroscopic data, including 1D/2D NMR, HR-ESI-MS, and ORD, as well as the ECD simulation and comparison. Most of them were phenolic and among them, four compounds were isolated from Stemona plants for the first time. This study uncovers diverse constituents from water decoction of S. tuberosa dedicated for its quality control and allows for the exploitation of chemical markers with potential significance for discrimination of Stemona plants.
Assuntos
Alcaloides , Stemonaceae , Alcaloides/química , Stemonaceae/química , Furaldeído/análise , Tubérculos/química , Espectroscopia de Ressonância Magnética , Estrutura MolecularRESUMO
Four undescribed steroidal compounds along with twenty known compounds were isolated from n-butanol extracted fraction of the whole plants of Solanum lyratum Thunb (SLNF). Their structures were assigned based on analyses of the extensive spectroscopic data (including MS, 1D/2D NMR, and ECD) or comparisons of the NMR data with those reported. Among the knowns, three compounds were isolated from Solanum plants for the first time, while one compound was isolated from S. lyratum for the first time. In addition, the cytotoxicities of these isolates against human colon SW480 and hepatoma Hep3B cells were evaluated by a MTT assay. And, nine of them and SLNF exhibited significant activities against both SW480 and Hep3B cells, while twelve of them significantly inhibited the activities of SW480 cells. This study allows for the exploitation of chemical markers with potential significance in discrimination of Solanum plants, and uncovers the diverse steroidal constituents from S. lyratum dedicated for its future application in cancer treatment.
Assuntos
Saponinas , Solanum , Humanos , Solanum/química , Saponinas/farmacologia , Esteroides/farmacologia , Estrutura MolecularRESUMO
Nardosinone, a predominant bioactive product from Nardostachys jatamansi DC, is well-known for its promising therapeutic applications, such as being used as a drug on anti-inflammatory, antidepressant, cardioprotective, anti-neuroinflammatory, anti-arrhythmic, anti-periodontitis, etc. However, its stability under varying environmental conditions and its degradation products remain unclear. In this study, four main degradation products, including two previously undescribed compounds [2-deoxokanshone M (64.23%) and 2-deoxokanshone L (1.10%)] and two known compounds [desoxo-narchinol A (2.17%) and isonardosinone (3.44%)], were firstly afforded from the refluxed products of nardosinone in boiling water; their structures were identified using an analysis of the extensive NMR and X-ray diffraction data and the simulation and comparison of electronic circular dichroism spectra. Compared with nardosinone, 2-deoxokanshone M exhibited potent vasodilatory activity without any of the significant anti-neuroinflammatory activity that nardosinone contains. Secondly, UPLC-PDA and UHPLC-DAD/Q-TOF MS analyses on the degradation patterns of nardosinone revealed that nardosinone degraded more easily under high temperatures and in simulated gastric fluid compared with the simulated intestinal fluid. A plausible degradation pathway of nardosinone was finally proposed using nardosinonediol as the initial intermediate and involved multiple chemical reactions, including peroxy ring-opening, keto-enol tautomerization, oxidation, isopropyl cleavage, and pinacol rearrangement. Our findings may supply certain guidance and scientific evidence for the quality control and reasonable application of nardosinone-related products.
Assuntos
Sesquiterpenos , Sesquiterpenos/química , Temperatura , Sesquiterpenos Policíclicos , Anti-InflamatóriosRESUMO
BACKGROUND: To investigate the effect of lactic acid (LA) on the progression of bone metastasis from colorectal cancer (CRC) and its regulatory effects on primary CD115 (+) osteoclast (OC) precursors. METHODS: The BrdU assay, Annexin-V/PI assay, TRAP staining and immunofluorescence were performed to explore the effect of LA on the proliferation, apoptosis and differentiation of OC precursors in vitro and in vivo. Flow cytometry was performed to sort primary osteoclast precursors and CD4(+) T cells and to analyze the change in the expression of target proteins in osteoclast precursors. A recruitment assay was used to test how LA and Cadhein-11 regulate the recruitment of OC precursors. RT-PCR and Western blotting were performed to analyze the changes in the mRNA and protein expression of genes related to the PI3K-AKT pathway and profibrotic genes. Safranin O-fast green staining, H&E staining and TRAP staining were performed to analyze the severity of bone resorption and accumulation of osteoclasts. RESULTS: LA promoted the expression of CXCL10 and Cadherin-11 in CD115(+) precursors through the PI3K-AKT pathway. We found that CXCL10 and Cadherin-11 were regulated by the activation of CREB and mTOR, respectively. LA-induced overexpression of CXCL10 in CD115(+) precursors indirectly promoted the differentiation of osteoclast precursors through the recruitment of CD4(+) T cells, and the crosstalk between these two cells promoted bone resorption in bone metastasis from CRC. On the other hand, Cadherin-11 mediated the adhesion between osteoclast precursors and upregulated the production of specific collagens, especially Collagen 5, which facilitated fibrotic changes in the tumor microenvironment. Blockade of the PI3K-AKT pathway efficiently prevented the progression of bone metastasis caused by lactate. CONCLUSION: LA promoted metastatic niche formation in the tumor microenvironment through the PI3K-AKT pathway. Our study provides new insight into the role of LA in the progression of bone metastasis from CRC. Video Abstract.
Assuntos
Neoplasias Ósseas/metabolismo , Neoplasias Colorretais/metabolismo , Ácido Láctico/metabolismo , Animais , Neoplasias Ósseas/genética , Neoplasias Ósseas/secundário , Linfócitos T CD4-Positivos , Caderinas/genética , Caderinas/metabolismo , Adesão Celular , Diferenciação Celular , Movimento Celular , Células Cultivadas , Quimiocina CXCL10/genética , Quimiocina CXCL10/metabolismo , Técnicas de Cocultura , Colágeno/genética , Colágeno/metabolismo , Neoplasias Colorretais/genética , Neoplasias Colorretais/patologia , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Osteoclastos , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Serina-Treonina Quinases TOR/metabolismo , Microambiente TumoralRESUMO
Prunus cerasoides (PC) products contain relatively high levels of flavones and isoflavones and may be potential sources of phytoestrogens for postmenopausal symptom relief. We assessed the PC extract (PCE) and its representative constituents in vitro with assays for estrogen receptor alpha binding, estrogen response element transcriptional activity, cell proliferation, and gene expression changes for pS2 in MCF-7 cells. PCE and its compounds showed strong estrogen receptor binding affinities and estrogen response element induction. A previously undescribed compound (designated as compound 18), now identified as being gentisic acid, 5-O-ß-D-(6'-O-trans-4-coumaroyl)-glucopyranoside, also showed potent estrogenic properties and induced proliferation of MCF-7 cells. PCE was evaluated for its in vivo uterotrophic effects in immature female rats as well as for its lipid lowering effects in estrogen-deprived animals. For ovariectomized rats and aged female mice, PCE-treated groups had lower plasma triglyceride levels compared with control and, for the same comparison, had reduced serum levels of liver stress/damage markers. Our results point to strong estrogenic activities and beneficial metabolic effects for PCE, with properties that put PC and its extracts as promising sources of phytoestrogens for symptom relief in menopausal and postmenopausal cases.
Assuntos
Estrogênios/uso terapêutico , Extratos Vegetais/química , Prunus/química , Animais , Modelos Animais de Doenças , Estrogênios/farmacologia , Feminino , Humanos , Células MCF-7/metabolismo , Camundongos , RoedoresRESUMO
Four sesquiterpenoid-chalcone hybrids (nardochalaristolones A-D, 1-4), a pair of epimeric sesquiterpenoid-flavonone hybrids ((2'S)- and (2'R)-nardoflavaristolone A, 5 and 6), and a sesquiterpenoid dimer (dinardokanshone F, 7), all sharing a kanshone C-derived sesquiterpenoid unit, were isolated from the underground parts of Nardostachys jatamansi (D.Don) DC. Their structures were elucidated by analysis of the extensive spectroscopic data, and the absolute configurations were established by analysis of 2D NMR spectroscopic data including NOESY data, combined with comparisons of experimental and calculated electronic circular dichroism spectra. Further, the plausible biosynthetic pathways for these compounds were proposed. And the results of SERT activity assay revealed that nardochalaristolones C-D (3 and 4) and nardoflavaristolone A (5 and 6) significantly enhanced SERT activity, while other compounds didn't show any SERT regulatory activities.
Assuntos
Chalcona/isolamento & purificação , Nardostachys/química , Sesquiterpenos/isolamento & purificação , Chalcona/química , Estrutura Molecular , Sesquiterpenos/químicaRESUMO
Nardostachys jatamansi is a well-documented herbal agent used to treat digestive and neuropsychiatric disorders in oriental medicinal systems. However, few simple, rapid, and comprehensive methods were reported for quality assessment and control of N. jatamansi. Herein, a UPLC with photodiode array detection method was developed for both fingerprint investigation of N. jatamansi and simultaneous quantitative analysis of the six serotonin transporter modulatory constituents in N. jatamansi. For chromatographic fingerprinting, 24 common peaks were selected as characteristic peaks to assess the consistency of N. jatamansi samples from different retail sources. Six of the common peaks (5, 7, 12: , and 16: â-â18: ) were identified as desoxo-narchinol A, buddleoside, isonardosinone, nardosinone, kanshone H, and (-)-aristolone, respectively, by phytochemical investigation. Five of the six compounds significantly either enhanced or inhibited serotonin transporter activity, while (-)-aristolone (18: ) didn't show any serotonin transporter activity. In quantitative analysis, the six compounds showed good linearity (r > 0.999) within test ranges. The precision, expressed as relative standard deviation, was in the range of 0.25â-â2.77%, and the recovery of the method was in the range of 92â-â105%. The UPLC-photodiode array detection-based fingerprint analysis and quantitative methods reported here could be used for routine quality control of N. jatamansi.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Nardostachys/química , Controle de QualidadeRESUMO
Sakuranetin (SKN), found in cherry trees and rice, is a flavanone with various pharmacological activities. It is biosynthesized from naringenin in rice or cherry trees, and the metabolism of SKN has been studied in non-human species. The present study aimed to investigate the metabolic pathways of SKN in human liver microsomes and identify the phase I and phase II metabolites, as well as evaluate the potential for drugâ»herb interactions through the modulation of drug metabolizing enzymes (DMEs). HPLC-DAD and HPLC-electrospray mass spectrometry were used to study the metabolic stability and identify the metabolites from human liver microsomes incubated with SKN. The potential of SKN to inhibit the DMEs was evaluated by monitoring the formation of a DME-specific product. The cytochrome P450 2B6 and 3A4-inductive effects were studied using promoter reporter assays in human hepatocarcinoma cells. The major pathways for SKN metabolism include B-ring hydroxylation, 5-O-demethylation, and conjugation with glutathione or glucuronic acid. The phase I metabolites were identified as naringenin and eriodictyol. SKN was found to be a UDP-glucuronosyltransferases (UGT) 1A9 inhibitor, whereas it induced transactivation of the human pregnane X receptor-mediated cytochrome P450 (CYP) 3A4 gene.
Assuntos
Sistema Enzimático do Citocromo P-450/metabolismo , Flavonoides/metabolismo , Glucuronosiltransferase/metabolismo , Fígado/metabolismo , Animais , Cromatografia Líquida de Alta Pressão , Inibidores das Enzimas do Citocromo P-450/farmacologia , Sistema Enzimático do Citocromo P-450/genética , Células Hep G2 , Humanos , Fígado/efeitos dos fármacos , Desintoxicação Metabólica Fase I , Desintoxicação Metabólica Fase II , Metaboloma , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/metabolismo , NADP/metabolismo , Receptor de Pregnano X , Regiões Promotoras Genéticas/genética , Receptores de Esteroides/metabolismo , Ativação Transcricional/genética , Uridina Difosfato Ácido Glucurônico/metabolismoRESUMO
Nardonaphthalenones A and B (1-2), one new apo-α-carotenone (3) and four new monoterpenoids (4, 8-9 and 11), along with six known compounds (5-7, 10, 12-13) were isolated from the dried roots and rhizomes of Nardostachys chinensis Batal. Their structures were elucidated by analysis of the spectroscopic data including NMR, HRESIMS and circular dichroism data. Furthermore, the serotonin transporter (SERT)-regulating activities of these isolates were evaluated, among them compound 3 showed the strongest enhancement activity while compound 12 showed a moderate inhibition activity on SERT.
Assuntos
Monoterpenos/química , Naftalenos/química , Nardostachys/química , Expressão Gênica/efeitos dos fármacos , Células HEK293 , Humanos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Monoterpenos/isolamento & purificação , Monoterpenos/farmacologia , Naftalenos/isolamento & purificação , Naftalenos/farmacologia , Nardostachys/metabolismo , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Rizoma/química , Rizoma/metabolismo , Proteínas da Membrana Plasmática de Transporte de Serotonina/química , Proteínas da Membrana Plasmática de Transporte de Serotonina/genética , Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismoRESUMO
Four new iridoids, 2'-O-(E)-coumaroylshanzhiside (1), 6'-O-(E)-coumaroylshanzhiside (2), 8α-butylgardenoside B (3), 6α-methoxygenipin (4), and one new phenylpropanoid glucoside, 5-(3-hydroxypropyl)-2-methoxyphenyl ß-d-glucopyranoside (5), together with sixteen known compounds, were isolated from the edible flowers of wild Gardenia jasminoides J.Ellis. Their chemical structures were characterized by extensive spectroscopic techniques, including 1D- and 2D-NMR, HR-ESI-MS, and CD experiments. The absolute configurations of the new isolates' sugar moiety were assigned by HPLC analysis of the acid hydrolysates. Furthermore, the antioxidant activities of those isolates were preliminarily evaluated by DPPH scavenging experiment. And comparison of 1 H-NMR spectra for the EtOH extract of G. jasminoides J.Ellis, gardenoside B and geniposide revealed that the flowers of this plant have a considerable content of gardenoside B instead of geniposide in the fruits, indicating different activities and applications in people's daily life.
Assuntos
Gardenia/química , Extratos Vegetais/análise , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Flores/química , Frutas/química , Iridoides/isolamento & purificação , Estrutura Molecular , Extratos Vegetais/química , Análise EspectralRESUMO
The existing antidepressants demonstrated delayed onset of clinical effects, so fast-onset antidepressants are required. Essential oil of herbs showed potentials fast-onset antidepressant potential. First, its aromatic odor can directly activate olfactory nerves; its high lipophilicity causes a high blood-brain barrier penetration rate; and its high volatility is suitable for nasal-brain targeting and inhalation delivery. Therefore, essential oils can rapidly regulate brain functions by multiple ways, suggesting a fast-onset antidepressant potential. Second, the advance of studies on chemistry and pharmacology of antidepressant essential oils demonstrated chemical substances, antidepressant effects and possible action mechanisms of antidepressant essential oils. Third, the effect of essential oils' antidepressant components on fast-onset antidepressant targets was investigated. It was found that chemical constituents of essential oils antagonized NMDA receptor activities, suggesting that essential oils have fast-onset antidepressant effect. Finally, characteristics of essential oils, fast-onset antidepressant targets and drug delivery methods are integrated to give full play to essential oils' fast-onset antidepressant advantage and provide a new direction for new drug discovery.
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Antidepressivos/farmacologia , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Administração por Inalação , Encéfalo/efeitos dos fármacos , HumanosRESUMO
To explore the associated risk factors of symptomatic knee osteonecrosis (KON) in patients with systemic lupus erythematosus (SLE), we conducted a retrospective case-control study to compare the clinical and laboratory features between SLE patients with and without symptomatic KON matched by age and gender. Univariate and multivariate regression analyses were used to evaluate possible associated risk factors. Twenty (one male, nineteen females) out of 3941 lupus patients were identified as symptomatic KON, which was confirmed by magnetic resonance imaging. The mean age at KON onset was 34.4 (range 12-67) years, and the median course of lupus at KON onset was 72.5 (range 8-123) months. Univariate and multivariate analyses identified that the prevalence of cutaneous vasculitis (OR 5.23; 95 % CI 1.11-24.70), hyperfibrinogenemia (OR 4.75; 95 % CI 1.08-20.85), and elevated IgG levels (OR 6.05; 95 % CI 1.58-23.16) were statistically higher in KON group, and hydroxychloroquine (HCQ) usage was statistically lower in KON group (OR 0.27; 95 % CI 0.07-0.97). Glucocorticoid usage, in terms of maximal dose, duration of treatment, and the percentage of receiving methylprednisolone pulse therapy, did not show statistical difference between the two groups (p > 0.05). Symptomatic KON is a relatively rare complication of SLE. Cutaneous vasculitis, hyperfibrinogenemia, and elevated IgG levels are possible risk factors, whereas HCQ may provide a protective effect. Our results suggest that lupus activity as well as hypercoagulation status may play a role in the pathogenesis of KON in lupus.
Assuntos
Articulação do Joelho/diagnóstico por imagem , Lúpus Eritematoso Sistêmico/complicações , Osteonecrose/complicações , Adolescente , Adulto , Idoso , Estudos de Casos e Controles , Criança , Feminino , Humanos , Lúpus Eritematoso Sistêmico/diagnóstico por imagem , Imageamento por Ressonância Magnética , Masculino , Pessoa de Meia-Idade , Osteonecrose/diagnóstico por imagem , Adulto JovemRESUMO
A new saponin, isonarthogenin 3-O-ß-d-glucopyranosyl-(1â4)-ß-d-galactopyranoside (1), together with twelve known compounds, were isolated from the rhizomes of Polygonatum sibiricum. The structures of these compounds were elucidated by analysis of their 1D/2D NMR and MS data. Among them, phenol compounds 4-7 and 9-10 showed significant inhibitions against the formation of advanced glycosylation end products, with IC50 values of 0.091 ± 0.0021, 0.10 ± 0.041, 0.014 ± 0.0027, 0.11 ± 0.011, 0.13 ± 0.045, and 0.055 ± 0.019 µM, respectively. The results will promote exploiting potential medicinal use of these compounds in the prevention of diabetic complications and supporting Polygonatum sibiricum as a functional food for healthy and medicinal diet.
Assuntos
Produtos Finais de Glicação Avançada/antagonistas & inibidores , Polygonatum/química , Saponinas/isolamento & purificação , Saponinas/farmacologia , Medicamentos de Ervas Chinesas/química , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Rizoma/química , Saponinas/químicaRESUMO
A new caffeate compound, (E)-erythro-syringylglyceryl caffeate (1), was isolated from the roots and rhizomes of Nardostachys chinensis Batal., together with nine known phenolic compounds, including (+)-licarin A (2), naringenin 4', 7-dimethyl ether (3), pinoresinol-4-O-ß-D-glucoside (4), caraphenol A (5), Z-miyabenol C (6), protocatechuic acid (7), caffeic acid (8), gallic acid (9) and vanillic acid (10). Their chemical structures were elucidated on the basis of spectroscopic data and physicochemical properties. Furthermore, this is the first report of compounds 2, 5 and 6 from Nardostachys genus.