RESUMO
The supramolecular solvent (SUPRAS) has garnered significant attention as an innovative, efficient, and environmentally friendly solvent for the effective extraction and separation of bioactive compounds from natural resources. However, research on the use of a SUPRAS for the extraction of phenolic compounds from plants, which are highly valued in food products due to their exceptional antioxidant properties, remains scarce. The present study developed a green, ultra-sound-assisted SUPRAS method for the simultaneous determination of three phenolic acids in Prunella vulgaris using high-performance liquid chromatography (HPLC). The experimental parameters were meticulously optimized. The efficiency and antioxidant properties of the phenolic compounds obtained using different extraction methods were also compared. Under optimal conditions, the extraction efficiency of the SUPRAS, prepared with octanoic acid reverse micelles dispersed in ethanol-water, significantly exceeded that of conventional organic solvents. Moreover, the SUPRAS method demonstrated greater antioxidant capacity. Confocal laser scanning microscopy (CLSM) images revealed the spherical droplet structure of the SUPRAS, characterized by a well-defined circular fluorescence position, which coincided with the position of the phenolic acids. The phenolic acids were encapsulated within the SUPRAS droplets, indicating their efficient extraction capacity. Furthermore, molecular dynamics simulations combined with CLSM supported the proposed method's mechanism and theoretically demonstrated the superior extraction performance of the SUPRAS. In contrast to conventional methods, the higher extraction efficiency of the SUPRAS can be attributed to the larger solvent contact surface area, the formation of more types of hydrogen bonds between the extractants and the supramolecular solvents, and stronger, more stable interaction forces. The results of the theoretical studies corroborate the experimental outcomes.
Assuntos
Antioxidantes , Fenóis , Extratos Vegetais , Solventes , Solventes/química , Fenóis/química , Fenóis/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão/métodos , Química Verde , Simulação de Dinâmica Molecular , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificaçãoRESUMO
Prunella vulgaris, aptly named for its withering at the summer solstice, displays significant variation in quality arising from differing harvest time. However, research on the chemical composition changes of its spikes at various stages is limited, and the specific metabolites remain unclear. In order to elucidate the metabolites and metabolic pathways of the spikes of P. vulgaris, the current study deployed ultra-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) and targeted metabolomics to characterize the compound variability in the spikes of P. vulgaris across different periods. Multivariate statistical techniques such as principal component analysis(PCA) and orthogonal partial least squares-discriminant analysis(OPLS-DA) were used to identify the differences in metabolites, and relevant metabolic pathways were analyzed. A total of 602 metabolites were identified by metabolomics, of which organic acids and their derivatives were the most abundant, followed by flavonoids. Multiple differential metabolites, including p-hydroxybenzoic acids and gallic acids were identified based on variable importance in projection(VIP)>1 and P<0.05. The results of enrichment analysis suggested that isoflavonoids biosynthesis, aminobenzoate degradation, benzoate degradation, anthocyanins biosynthesis, metabolic pathways, microbial metabolism in different environments, secondary plant metabolite biosynthesis, tryptophan metabolism, and phenylpropanoid synthesis were the main metabolic pathways. These results intend to elucidate the dynamic changes of differential metabolites of P. vulgaris and provide a theoretical basis for further study of the harvesting mechanism of spikes of P. vulgaris.
Assuntos
Metabolômica , Prunella , Espectrometria de Massas em Tandem , Prunella/química , Prunella/metabolismo , Espectrometria de Massas em Tandem/métodos , Cromatografia Líquida de Alta Pressão , Metabolômica/métodos , Espectrometria de Massa com Cromatografia LíquidaRESUMO
Numerous studies show that Lonicera macranthoides and L. japonica have significant differences in organic matter. However, there is still a lack of research on inorganic elements between them. In this study, a non-targeted elemental metabolomics method was established by inductively coupled plasma mass spectrometry(ICP-MS), so as to compare the overall differences of inorganic elements between L. macranthoides and L. japonica. In addition, the differential markers were screened, and these differential markers were quantitatively analyzed by the targeted method. The non-targeted elemental metabolomics showed that the established mathematical model could reflect the difference in element content between L. macranthoides and L. japonica. Four inorganic elements such as ~(55)Mn, ~(209)Bi, ~(111)Cd, and ~(85)Rb were confirmed as the differential markers of L. macranthoides and L. japonica based on the screening principles of variable importance in the projection(VIP) value>2.0, P<0.01 and fold change(FC) value>1.2 or <0.80. The targeted quantitative results showed that the content of ~(209)Bi in L. japonica was significantly higher than that in L. macranthoides, while ~(55)Mn, ~(111)Cd, and ~(85)Rb in L. macranthoides were significantly higher than that in L. japonica. The non-targeted and targeted elemental metabolomics methods based on ICP-MS can significantly reflect the overall differences in inorganic elements between L. macranthoides and L. japonica. Exploring the differences between them from the perspective of elements can partly reflect the differences in their drug properties and lay a foundation for further study on the quality control mode of inorganic elements in L. macranthoides and L. japonica and their pharmacological effects.
Assuntos
Lonicera , Espectrometria de Massas , Metabolômica , Controle de Qualidade , Lonicera/química , Espectrometria de Massas/métodos , Metabolômica/métodos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/análiseRESUMO
BACKGROUND: To develop a new modality of colorectal cancer screening based on chronic disease management (CDM) to improve the participation rate of screening, and maximize the benefits of limited resources. METHODS: Patients under CDM were assigned to screening intervention group (SI) and screening control group1 (SC1), residents from natural community were assigned to screening control group2 (SC2). A parallel controlled community intervention study was performed. Only SI would achieve "one-to-one" intervention services. Meanwhile, 200 subjects were selected from each of the three groups for the Knowledge-Attitude-Practice (KAP) questionnaire before and after intervention, named questionnaire intervention group(QI), questionnaire control group1(QC1) and questionnaire control group2(QC2). The outcome of the intervention was evaluated using the difference-in-differences method and multiple regression analysis. RESULTS: The preliminary screening participation rate was 43.63%(473/1084) in SI, 14.32%(132/922) in SCI, and 5.87%(105/1789) in SC2. The baseline questionnaire showed low knowledge scores in the three questionnaire groups with no statistically significant differences, while attitude scores in QI and QC1 were significantly higher than QC2. The differences between baseline and terminal showed QI increased larger in knowledge and attitude scores than QC1 and QC2, while no difference was detected between QC1 and QC2. CONCLUSION: The colorectal cancer screening model based on chronic disease management effectively improved the screening participation rate, and the "one-to-one" intervention and the inherent characteristics of the patient population under CDM were the core elements of the new modality.
Assuntos
Neoplasias Colorretais , Detecção Precoce de Câncer , Humanos , Detecção Precoce de Câncer/métodos , Neoplasias Colorretais/epidemiologia , Conhecimentos, Atitudes e Prática em Saúde , Análise Multivariada , Gerenciamento Clínico , Programas de RastreamentoRESUMO
The virtual machine (VM) scheduling problem in cloud brokers that support cloud bursting is fraught with uncertainty due to the on-demand nature of Infrastructure as a Service (IaaS) VMs. Until a VM request is received, the scheduler does not know in advance when it will arrive or what configurations it demands. Even when a VM request is received, the scheduler does not know when the VM's lifecycle expires. Existing studies begin to use deep reinforcement learning (DRL) to solve such scheduling problems. However, they do not address how to guarantee the QoS of user requests. In this paper, we investigate a cost optimization problem for online VM scheduling in cloud brokers for cloud bursting to minimize the cost spent on public clouds while satisfying specified QoS restrictions. We propose DeepBS, a DRL-based online VM scheduler in a cloud broker which learns from experience to adaptively improve scheduling strategies in environments with non-smooth and uncertain user requests. We evaluate the performance of DeepBS under two request arrival patterns which are respectively based on Google and Alibaba cluster traces, and the experiments show that DeepBS has a significant advantage over other benchmark algorithms in terms of cost optimization.
RESUMO
Catalyst deactivation is a problem of great concern for many heterogeneous reactions. Here, an urchin-like LaPO4 catalyst was easily developed for pentane-2,3-diol dehydration; it has an impressive ability to restore the activity inâ situ by itself during the reaction, accounting for its high stability. This facilitates the efficient production of renewable penta-1,3-diene from pentane-2,3-dione via a novel approach, where penta-2,3-diol was obtained as an intermediate in 95 % yield under mild conditions.
RESUMO
This study aims to explore the biological actions of circular RNA (circRNA) ArfGAP with SH3 domain, ankyrin repeat and PH domain 2 (circ_ASAP2, circ_0006089) in cisplatin (DDP) resistance of gastric cancer. Circ_ASAP2, ecto-5'-nucleotidase (NT5E) and miR-330-3p were quantified by quantitative real-time PCR or western blot. The measurements of the IC50 value and cell proliferation were done using 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) assay. Cell colony formation, cell cycle distribution, apoptosis, migration and invasion were evaluated by the colony formation, flow cytometry and transwell assays. Dual-luciferase reporter assay was performed to confirm the targeted relationship between different molecules. The role of circ_ASAP2 in tumor growth was gauged by in vivo animal studies. Circ_ASAP2 and NT5E were overexpressed in DDP-resistant gastric cancer tissues and cells. Knockdown of circ_ASAP2 promoted DDP sensitivity, apoptosis and repressed proliferation, migration and invasion of DDP-resistant gastric cancer cells in vitro and diminished tumor growth in vivo. Moreover, NT5E was a downstream effector of circ_ASAP2 in regulating cell DDP sensitivity and functional behaviors. Mechanistically, circ_ASAP2 directly bound to miR-330-3p to promote NT5E expression. Furthermore, circ_ASAP2 modulated cell DDP sensitivity and functional behaviors by targeting miR-330-3p. Knockdown of circ_ASAP2 promoted DDP sensitivity and suppressed malignant behaviors of DDP-resistant gastric cancer cells through targeting the miR-330-3p/NT5E axis.
Assuntos
Antineoplásicos/farmacologia , Cisplatino/farmacologia , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , MicroRNAs/metabolismo , RNA Circular/metabolismo , Neoplasias Gástricas/patologia , 5'-Nucleotidase/metabolismo , Animais , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Feminino , Proteínas Ligadas por GPI/metabolismo , Proteínas Ativadoras de GTPase/metabolismo , Humanos , Concentração Inibidora 50 , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos NusRESUMO
In this study, silica-polydopamine hybrids (SPDA) were fabricated by a facile and one-step heating method using dopamine and (3-aminopropyl)triethoxysilane (APTES) as the reaction reagents. It was firstly found that light illuminated-SPDA could oxidize colorless 3,3',5,5'-tetramethylbenzidine (TMB) to produce blue ox-TMB. The coloration process was quenched very efficiently via the addition of Cu2+. The presence of pyrophosphate ion (PPi) in the solution of light-illuminated SPDA-Cu2+-TMB induced the recovery of the coloration process. The recovery occurred because PPi coordinated with Cu2+, effectively sequestering the ion from SPDA. A calibration curve was developed that is related to the extent of absorption recovery to [PPi], making the SPDA-Cu2+-TMB system a sensitive and selective turn-on sensor for PPi detection. The limit-of-detection (LOD) for PPi was 0.06 µmol L-1 (S/N = 3) with a linear dynamic range of 0.1-30 µmol L-1 and the calibration curve of linear equation is given as: y = 0.00146x + 0.05096 (r = 0.9974). The proposed method has been successfully applied to the detection of PPi in human serum with satisfactory recovery. The simplicity, low cost, high sensitivity, good reproducibility and excellent selectivity of the PPi detection platform based on the light-induced oxidase mimicking property of SPDA makes it promising for further applications of SPDA in chemo/biosensing.
RESUMO
An enantiomeric pair of rare cyperane-type sesquiterpenoids, (+)- and (-)-gracilistones C (1a, 1b), together with a novel norsesquiterpenoid, gracilistone D (2), bearing a bicyclic lactone system were isolated from the root bark of Acanthopanax gracilistylus using LC-MS-IT-TOF analyses. The structures and absolute configurations of 1a, 1b, and 2 were elucidated by 1D and 2D NMR spectroscopy, X-ray diffraction, and ECD spectroscopic methods. Intermediate 1b suggests a possible biosynthesis process involving compound 2. The bioassay results showed that compounds 1a, 1b, and 2 exhibited significant inhibitory effects against lipopolysaccharide-induced nitric oxide production in RAW 264.7 cells, with IC50 values of 7.7 ± 0.6, 6.8 ± 1.5, and 2.6 ± 0.4 µM, respectively. Additional docking analyses provided some perspective of this activity in human inducible nitric oxide synthase.
Assuntos
Araliaceae/química , Óxido Nítrico/antagonistas & inibidores , Casca de Planta/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Animais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Células RAW 264.7 , Difração de Raios XRESUMO
OBJECTIVE: The aim of this study was to estimate the clinical effects of allogeneic acellular dermal matrix (ADM) in the surgical therapy of anterior urethral stricture (AUS). METHODS: We retrospectively collected the clinical data of 49 patients with AUS who underwent urethral repair surgery with ADM in the Department of Urology of the Peking University People's Hospital, and in the First Affiliated Hospital of the People's Liberation Army, from September 2015 to January 2019. The changes in urine flow rate and conditions of urethral mucosal coverage were observed as well as complications and outcomes, and statistical analysis was performed. RESULTS: The average maximum urine flow rates at the 1st, 6th, and 12th month post-surgery were 16.3 ± 1.5, 15.0 ± 1.9, and 14.6 ± 2.1 mL/s, respectively. These values were significantly higher than the preoperative maximum urine flow rate, 1.3 ± 0.5 mL/s (p < 0.05). Cystoscopy was performed in 11 patients 12 months after surgery, with microscopic assessment revealing good urethral epithelial mucosal coverage. Only 2 patients developed infection 2-4 weeks after surgery, while 7 patients developed noninfective urethral restricture 6-10 months after surgery and 1 patient developed urinary fistula 5 months after surgery. All of these statuses improved after receiving appropriate treatment. CONCLUSIONS: Use of ADM represents a new option for the surgical management of AUS repair and reconstruction, with positive clinical effects. In addition, it has the advantages of convenient for operation procedures and access, with no need for additional sampling surgery.
Assuntos
Derme Acelular , Estreitamento Uretral/cirurgia , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Resultado do Tratamento , Estreitamento Uretral/patologia , Procedimentos Cirúrgicos Urológicos Masculinos/métodosRESUMO
There has been a lot of research on flight delays. But it is more useful and difficult to estimate the departure delay time especially three hours before the scheduled time of departure, from which passengers can reasonably plan their travel time and the airline and airport staff can schedule flights more reasonably. In this paper, we develop a Spatio-temporal Graph Dual-Attention Neural Network (SGDAN) to learn the departure delay time for each flight with real-time conditions at three hours before the scheduled time of departure. Specifically, it first models the air traffic network as graph sequences, what is, using a heterogeneous graph to model a flight and its adjacent flights with the same departure or arrival airport in a special time interval, and using a sequence to model the flight and its previous flights that share the same aircraft. The main contributions of this paper are using heterogeneous graph-level attention to learn the influence between the flight and its adjacent flight together with sequence-level attention to learn the influence between the flight and its previous flight in the flight sequence. With aggregating features from the learned influence from both graph-level and sequence-level attention, SGDAN can generate node embedding to estimate the departure delay time. Experiments on a real-world large-scale data set show that SGDAN produces better results than state-of-the-art models in the accurate flight delay time estimation task.
RESUMO
Although there are many algorithms to track people that are walking, existing methods mostly fail to cope with occluded bodies in the setting of multi-person tracking with one camera. In this paper, we propose a method to use people's shadows as a clue to track them instead of treating shadows as mere noise. We introduce a novel method to track multiple people by fusing shadow data from the RGB image with skeleton data, both of which are captured by a single RGB Depth (RGB-D) camera. Skeletal tracking provides the positions of people that can be captured directly, while their shadows are used to track them when they are no longer visible. Our experiments confirm that this method can efficiently handle full occlusions. It thus has substantial value in resolving the occlusion problem in multi-person tracking, even with other kinds of cameras.
Assuntos
Reconhecimento Automatizado de Padrão , Fotografação/instrumentação , Algoritmos , Humanos , Movimento (Física) , Fatores de TempoRESUMO
Bladder cancer has high morbidity and mortality rates worldwide. Its incidence is high in western countries and has shown an increasing trend in China. While radical cystectomy combined with pelvic lymph node dissection (PLND) is the standard treatment for bladder cancer,the optimal range of PLND remains controversial. In addition,the prognostic value of lymph node factors is also unclear. This article reviews research advances in PLND.
Assuntos
Excisão de Linfonodo , Neoplasias da Bexiga Urinária/diagnóstico , China , Humanos , Linfonodos , PelveRESUMO
Ginkgo biloba L., well known as living fossil, have various pharmacological activities. Eighteen compounds were isolated from Ginkgo male flowers including a novel matsutake alcohol glycoside, Ginkgoside A (1), and 17 known compounds-calaliukiuenoside (2), benzylalcohol O-α-l-arabinopyranosyl-(1 â 6)-ß-d-glucopyranoside (3), amentoflavone (4), sciadopitysin (5), bilobetin (6), isoginkgetin (7), olivil 4-O-ß-d-glucopyranoside (8), dihydrodehydrodiconiferyl alcohol-4-O-ß-d-glucoside (9), (+)-cyclo-olivil-6-O-ß-d-glucopyranoside (10), (-)-isolariciresinol 4-O-ß-d-glucopyranoside (11), coniferin (12), trans-cinnamic acid-4-O-ß-d-glucopyranoside (13), p-coumaryl alchol glucoside (14), stroside B (15), methylconiferin (16), cis-p-coumaric acid 4-O-ß-d-glucopyranoside (17), and cis-coniferin (18). Thirteen of these compounds had not previously found in Ginkgo. All extractive fractions and isolated compounds were evaluated for their anti-inflammatory ability in the lipopolysaccharide-induced RAW264.7 macrophages. The ethanol extract of Ginkgo flowers and the chloroform and ethyl acetate fractions can significantly decrease nitric oxide (NO), interleukin-6 (IL-6), and prostaglandin E2 (PGE2 ) production at 100 µg/ml. The most effective compounds, bilobetin (6) and isoginkgetin (7), elevated the NO inhibition ratios to 80.19% and 82.37% at 50 µM, respectively. They also exhibited significant dose-dependent inhibitory effects on tumor necrosis factor-α, IL-6, PGE2 , inducible NO synthase mRNA, and cyclooxygenase-2 mRNA levels. So they can be promising candidates for the development of new anti-inflammatory agents.
Assuntos
Anti-Inflamatórios/farmacologia , Ginkgo biloba/química , Inflamação/prevenção & controle , Macrófagos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Pólen/química , Animais , Ciclo-Oxigenase 2/metabolismo , Flores/química , Inflamação/induzido quimicamente , Inflamação/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Despite having played a significant role in the Industry 4.0 era, the Internet of Things is currently faced with the challenge of how to ingest large-scale heterogeneous and multi-type device data. In response to this problem we present a heterogeneous device data ingestion model for an industrial big data platform. The model includes device templates and four strategies for data synchronization, data slicing, data splitting and data indexing, respectively. We can ingest device data from multiple sources with this heterogeneous device data ingestion model, which has been verified on our industrial big data platform. In addition, we present a case study on device data-based scenario analysis of industrial big data.
RESUMO
C-boivinopyranosyl flavones have rarely been isolated from nature. In the search for anti-HBV (hepatitis b virus) constituents of Alternanthera philoxeroides, two new compounds, luteolin-6-C-ß-D-boivinopyranosyl-3'-O-ß-D-glucopyranoside (1) and chrysoeriol-6-C-ß-D-boivinopyranosyl-4'-O-ß-D-glucopyranoside (2), along with three known C-boivinopyranosyl flavones (compounds 3-5) were isolated. Their structures were determined by spectroscopic analyses including 1D and 2D NMR, HR-ESI-MS, IR spectra. Compounds 1, 2 and 3 showed significant anti-HBV activities through specifically inhibiting the secretion of HBsAg in HepG2.2.15.
Assuntos
Amaranthaceae/química , Antivirais/química , Antivirais/farmacologia , Flavonas/química , Flavonas/farmacologia , Vírus da Hepatite B/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
Objective: To study the chemical constituents of Rubus stans. Methods: The chemical constituents were isolated and purified by silica gel and Sephadex LH-20 column chromatography. The structures were identified on the basis of spectroscopic analysis and physicochemical properties. Results: Eleven compounds were isolated and purified from the ethanol extract of Rubus stans. They were identified as ß-sitosterol( 1),betulinic acid( 2),euscaphic acid( 3),ursolic acid( 4),corosolic acid( 5),kaempferol( 6),quercetin( 7),2α,3ß,19α,23-tetrahydroxy-urs-12-en-28-oic acid( 8),ß-daucosterol( 9),quercetin-3-O-ß-D-glucoside( 10) and kaempferol-3-O-ß-D-6-O-( p-hydroxycinnamoyl)-glucopyranoside( 11). Conclusion: All the compounds are isolated from this plant for the first time.
Assuntos
Rubus , Quempferóis , Triterpenos Pentacíclicos , Sitosteroides , Triterpenos , Ácido Betulínico , Ácido UrsólicoRESUMO
Objective: To study the chemical constituents from the whole plant of Delphinium caeruleum. Methods: The chemical constituents were isolated and purified by silica gel and Sephadex LH-20 column chromatography. The structures of the isolated compounds were elucidated by spectroscopic analysis and physicochemical properties. Results: Twelve compounds were isolated and purified from the ethanol extract of Delphinium caeruleum. They were identified as ß-sitosterol( 1),kaempferol( 2),quercetin( 3),isovanillic acid( 4),apigenin( 5),luteolin( 6),8-methoxy-5,7,3',4'-tetrahydroxy-flavone( 7),ß-daucosterol( 8),kaempferol-3-O-ß-D-glucoside( 9),3,5-dihydroxy-4'-methoxyflavone-7-yl-O-ß-D-glucopyranosyl-( 1â4)-α-L-rhamnopyranoside( 10),rutin( 11) and sucrose( 12). Conclusion: Compounds 1 ~ 12 are isolated from this plant for the first time.
Assuntos
Delphinium , Apigenina , Glucosídeos , Quempferóis , Luteolina , Quercetina , Rutina , SitosteroidesRESUMO
Chemical investigation of the ethanol extract of the whole plant of Megacodon stylophorus led to the isolation and identification of two new seco-hopane triterpenoids, 2,3-seco-22(29)-hopene-2-carboxyl-3-aldehyde (1) and 2,3-seco-4(23),22(29)-hopene-2-carboxyl-3-aldehyde (2), along with 10 known compounds, 3-12. All the isolates were reported from this plant for the first time. The structures of compounds 1 and 2 were determined by detailed analysis of their spectral data including 1D and 2D NMR. In addition, compound 1 was further analyzed by X-ray crystallography. Compounds 1-3 were evaluated for their in vitro anti-proliferative activities on HeLa, MCF-7, and Hep-G2 tumor cell lines. Compound 2 was active against the three cell lines with IC50 values of 3.6, 7.5, and 13.6 µM, respectively, while compound 1 exhibited cytotoxicity on MCF-7 (IC50 14.0 µM) and HeLa (IC50 18.2 µM) cell lines. Antimicrobial activities of compounds 1-2 (minimum inhibitory concentration values in the range of 3.12-12.50 mg/mL) were also observed.
Assuntos
Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Gentianaceae/química , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Cristalografia por Raios X , Feminino , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Triterpenos/química , Triterpenos/isolamento & purificaçãoRESUMO
Two new coumarins, (E)-2-(4-hydroxy-3-methoxybenzylidene)-5-methoxy-2H-[1,4]dioxino[2,3-h]chromene-3,9-dione (indicumin E, 1) and 7-hydroxy-6,8-dimethoxy-3-(4'-hydroxy-3'-methoxyphenyl)-coumarin (2), together with two known coumarins isofraxidin (3) and fraxetin (4), were isolated from the Solanum indicum seeds. Their structures were established on the basis of 1D and 2D spectroscopic data. Compound 1 was the rarest coumarinolignoid known to date.