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1.
Molecules ; 26(19)2021 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-34641527

RESUMO

Toddalia asiatica (L.) Lam. (Rutaceae) has shown a broad spectrum of biological properties, such as anti-inflammatory, antioxidant, antimicrobial, anti-HIV, and anticancer properties. The present study is concerned with the separation of the main components with broad partition coefficients (KD values) from T. asiatica, using linear gradient high-speed counter-current chromatography (LGCCC) combined with an off-line two-dimensional (2D) mode. Similar to the binary gradient HPLC, the LGCCC mode is operated by the adjustment of the proportion between the mobile phase of 5:5:1:9 (v/v) (pump A) and 5:5:4.5:5.5 (v/v) (pump B) in an n-hexane/ethyl acetate/methanol/water solvent system. The off-line 2D-CCC mode was used in this study for the secondary separation of two similar KD value compounds with n-hexane/ethyl acetate/methanol/water (5:5:4:6, v/v). Notably, six coumarins, namely, tomentin (1), toddalolactone (2), 5,7,8-trimethoxycoumarin (3), mexoticin (4), isopimpinellin (5), and toddanone (6), were efficiently separated. The structures of the pure compounds were elucidated by spectral techniques and compared with the literature.


Assuntos
Cumarínicos/isolamento & purificação , Distribuição Contracorrente/métodos , Raízes de Plantas/química , Rutaceae/química , Cromatografia Líquida de Alta Pressão , Cumarínicos/química , Furocumarinas/isolamento & purificação , Estrutura Molecular , Solventes/química
2.
Molecules ; 26(15)2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34361817

RESUMO

Herein, a comprehensive review is given focusing on the chemical profiles of the essential oils (EOs), non-volatile compounds, ethnobotany, and biological activities of different Haplophyllum (Rutaceae family) species. To gather the relevant data, all the scientific databases, including Scopus, ISI-WOS (Institute of Scientific Information-Web of Science), and PubMed and highly esteemed publishers such as Elsevier, Springer, Taylor and Francis, etc., were systematically retrieved and reviewed. A wide array of valuable groups of natural compounds, e.g., terpenoids, coumarins, alkaloids, lignans, flavonoids, and organic acids have been isolated and subsequently characterized in different organic extracts of a number of Haplophyllum species. In addition, some remarkable antimicrobial, antifungal, anti-inflammatory, anticancer, cytotoxic, antileishmanial, and antialgal effects as well as promising remedial therapeutic properties have been well-documented for some species of the genus Haplophyllum.


Assuntos
Compostos Fitoquímicos/química , Fitoterapia , Rutaceae/química , Animais , Humanos , Medicina Tradicional , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico
3.
Fitoterapia ; 154: 105024, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34455037

RESUMO

The antimicrobial effects of essential oils are commonly cited within aromatherapeutic texts for use in respiratory tract infections. These essential oils are inhaled or applied to the skin to treat infections and manage symptoms associated with these conditions. A limited number of these essential oils have been scientifically studied to support these claims, specifically, against respiratory pathogens. This study reports on the minimum inhibitory concentration (MIC) of 49 commercial essential oils recommended for respiratory tract infections, and identifies putative biomarkers responsible for the determined antimicrobial effect following a biochemometric workflow. Essential oils were investigated against nine pathogens. Three essential oils, Amyris balsamifera (amyris), Coriandrum sativum (coriander) and Santalum austrocaledonicum (sandalwood) were identified as having greater activity (MIC value = 0.03-0.13 mg/ml) compared to the other essential oils investigated. The essential oil composition of all 49 oils were determined using Gas Chromatography coupled to Mass Spectroscopy (GC-MS) analysis and the GC-MS data analysed together with the antimicrobial data using chemometric tools. Eugenol was identified as the main biomarker responsible for antimicrobial activity in the majority of the essential oils. The ability of a chemometric model to accurately predict the active and inactive biomarkers of the investigated essential oils against pathogens of the respiratory tract was 80.33%.


Assuntos
Anti-Infecciosos/farmacologia , Óleos Voláteis/farmacologia , Óleos Vegetais/farmacologia , Coriandrum/química , Testes de Sensibilidade Microbiana , Infecções Respiratórias/tratamento farmacológico , Infecções Respiratórias/microbiologia , Rutaceae/química , Santalaceae/química , Relação Estrutura-Atividade
4.
Chin J Nat Med ; 19(8): 621-625, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34419261

RESUMO

Three new coumarins, integmarins A-C (1-3), and a new coumarin glycoside, integmaside A (4) were isolated from the leaves and stems of Micromelum integerrimum. Their structures were elucidated on the basis of 1D and 2D NMR and MS data, and their absolute configurations were assigned according to the ECD data of the in situ formed transition metal complexes and comparison of experimental and calculated ECD data. Compounds 1 and 2 are two rare coumarins with butyl and propyl moieties at the C-6 position; compound 3 is a novel coumarin with a highly oxidized prenyl group, and compound 4 is a rare bisdihydrofuranocoumarin glycoside.


Assuntos
Cumarínicos/química , Glicosídeos , Rutaceae , Cumarínicos/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química , Rutaceae/química
5.
Braz J Biol ; 83: e247071, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34431915

RESUMO

The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2´-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe2+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.


Assuntos
Diabetes Mellitus Experimental , Rutaceae , Animais , Glicemia , Diabetes Mellitus Experimental/tratamento farmacológico , Frutas , Pós , Ratos , Hormônios Tireóideos
6.
Phytochemistry ; 190: 112865, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34314905

RESUMO

The present article is a systematic and constructive review of the traditional medicinal uses, chemistry, pharmacology, toxicology, and formulation aspects of Glycosmis species. The genus Glycosmis comprise 51 accepted species broadly distributed in Australia, China, India, and South-East Asia. Traditionally, Glycosmis species are used in folk medicines to treat cancer, anaemia, rheumatism, fever, cough, liver-related problems, skin ailments, intestinal worm infections, wounds, and facial inflammation. This review aims to provide readers with the latest information highlighting chemical constituents isolated from the Glycosmis species, plant parts utilized for their isolation and their pharmacological activities. So far, 307 chemical constituents have been isolated and characterized from different species of the genus Glycosmis; among these constituents, alkaloids, flavonoids, terpenoids, phenolics, and sulphur-containing amides are the major bioactive compounds. Modern pharmacological studies have shown that the crude extracts and compounds isolated from this genus exhibit a broad spectrum of biological activities like anticancer, antimicrobial, anti-inflammatory, antipyretic, antidiabetic, antioxidant, larvicidal, insecticidal, hepatoprotective, wound healing, antiviral, antidiarrheal, and anxiolytic. The carbazole and acridone alkaloids from this genus have shown potential anticancer activity in various in vitro and in vivo studies. Rare scaffolds like dimeric carbazoles, dimeric acridone alkaloids, flavanocoumarins and sulphur-containing amides from this genus need further exploration for their potential bioactivity. This article also briefs about the toxicological screening and discusses various polyherbal and nano formulation aspects of Glycosmis species. Most of the pharmacological studies reported from this genus were carried out in vitro. An in-depth in vivo and toxicology evaluation of the crude extracts and isolated specialized compounds is required to explore the full therapeutic potential of this genus.


Assuntos
Rutaceae , Etnofarmacologia , Medicina Tradicional , Compostos Fitoquímicos , Fitoterapia , Extratos Vegetais
7.
Ann Bot ; 128(4): 497-510, 2021 09 03.
Artigo em Inglês | MEDLINE | ID: mdl-34250543

RESUMO

BACKGROUND AND AIMS: Zanthoxylum is the only pantropical genus within Rutaceae, with a few species native to temperate eastern Asia and North America. Efforts using Sanger sequencing failed to resolve the backbone phylogeny of Zanthoxylum. In this study, we employed target-enrichment high-throughput sequencing to improve resolution. Gene trees were examined for concordance and sectional classifications of Zanthoxylum were evaluated. Off-target reads were investigated to identify putative single-copy markers for bait refinement, and low-copy markers for evidence of putative hybridization events. METHODS: A custom bait set targeting 354 genes, with a median of 321 bp, was designed for Zanthoxylum and applied to 44 Zanthoxylum species and one Tetradium species as the outgroup. Illumina reads were processed via the HybPhyloMaker pipeline. Phylogenetic inferences were conducted using coalescent and maximum likelihood methods based on concatenated datasets. Concordance was assessed using quartet sampling. Additional phylogenetic analyses were performed on putative single and low-copy genes extracted from off-target reads. KEY RESULTS: Four major clades are supported within Zanthoxylum: the African clade, the Z. asiaticum clade, the Asian-Pacific-Australian clade and the American-eastern Asian clade. While overall support has improved, regions of conflict are similar to those previously observed. Gene tree discordances indicate a hybridization event in the ancestor of the Hawaiian lineage, and incomplete lineage sorting in the American backbone. Off-target putative single-copy genes largely confirm on-target results, and putative low-copy genes provide additional evidence for hybridization in the Hawaiian lineage. Only two of the five sections of Zanthoxylum are resolved as monophyletic. CONCLUSIONS: Target enrichment is suitable for assessing phylogenetic relationships in Zanthoxylum. Our phylogenetic analyses reveal that current sectional classifications need revision. Quartet tree concordance indicates several instances of reticulate evolution. Off-target reads are proven useful to identify additional phylogenetically informative regions for bait refinement or gene tree based approaches.


Assuntos
Rutaceae , Zanthoxylum , Austrália , Hibridização Genética , Filogenia , Zanthoxylum/genética
8.
Planta Med ; 87(10-11): 827-835, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34293806

RESUMO

Haplophyllum tuberculatum is a plant commonly used in folk medicine to treat several diseases including vomiting, nausea, infections, rheumatism, and gastric pains. In the current study, H. tuberculatum essential oils, hydrosols, the pure compounds R-(+)-limonene, S-(-)-limonene, and 1-octanol, as well as their combinations R-(+)-limonene/1-octanol and S-(-)-limonene/1-octanol, were screened for their cytotoxicity on HEp-2 cells after 24, 48, and 72 h, and then tested for their activity against Coxsackievirus B3 and B4 (CV-B3 and CV-B4) at 3 different moments: addition of the plant compounds before, after, or together with virus inoculation. Results showed that the samples were more cytotoxic after 72 h than after 24 h or 48 h cell contact. However, the combinations R-(+)-limonene/1-octanol and S-(-)-limonene/1-octanol showed less effect on HEp-2 cells than pure R-(+)-limonene and S-(-)-limonene after 24 h, 48 h, and 72 h. 1-octanol exhibited the highest concentration causing 50% cytotoxicity (CC50) on HEp-2 cells after 24 h (CC50 = 93 µg/mL) and 48 h (CC50 = 83 µg/mL). The antiviral assays showed that the tested samples exhibited potent inhibition of CV-B. IC50 values ranged from 0.66 µg/mL to 28.4 µg/mL. In addition, CV-B3 was more sensitive than CV-B4. Both CV-B strains are more inhibited when cells were pretreated with the plant compounds. The hydrosols have no effect, neither on HEp-2 cells nor on the virus. 1-octanol, S-(-), and R-(+)-limonene/1-octanol had important selectivity indexes over time. Although essential oils had potent antiviral activity, they can be considered for application in the pretreatment of cells. However, 1-octanol and the combinations are within the safety limits, and thus, they can be used as an active natural antiviral agent for CV-B3 and CV-B4 inhibition.


Assuntos
Óleos Voláteis , Rutaceae , Antivirais/farmacologia , Limoneno , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia
9.
J Exp Bot ; 72(18): 6274-6290, 2021 09 30.
Artigo em Inglês | MEDLINE | ID: mdl-34125891

RESUMO

Carotenoids play vital roles in the coloration of plant tissues and organs, particularly fruits; however, the regulation of carotenoid metabolism in fruits during ripening is largely unknown. Here, we show that red light promotes fruit coloration by inducing accelerated degreening and carotenoid accumulation in kumquat fruits. Transcriptome profiling revealed that a NAC (NAM/ATAF/CUC2) family transcription factor, FcrNAC22, is specifically induced in red light-irradiated fruits. FcrNAC22 localizes to the nucleus, and its gene expression is up-regulated as fruits change color. Results from dual luciferase, yeast one-hybrid assays and electrophoretic mobility shift assays indicate that FcrNAC22 directly binds to, and activates the promoters of three genes encoding key enzymes in the carotenoid metabolic pathway. Moreover, FcrNAC22 overexpression in citrus and tomato fruits as well as in citrus callus enhances expression of most carotenoid biosynthetic genes, accelerates plastid conversion into chromoplasts, and promotes color change. Knock down of FcrNAC22 expression in transiently transformed citrus fruits attenuates fruit coloration induced by red light. Taken together, our results demonstrate that FcrNAC22 is an important transcription factor that mediates red light-induced fruit coloration via up-regulation of carotenoid metabolism.


Assuntos
Lycopersicon esculentum , Rutaceae , Carotenoides , Frutas/metabolismo , Regulação da Expressão Gênica de Plantas , Lycopersicon esculentum/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo
10.
Bull Environ Contam Toxicol ; 107(6): 1128-1135, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34159411

RESUMO

A pot experiment was conducted to investigate the effects of 0.5% and 1% alkaline, clay mineral and phosphorus amendments, as well as 2% and 5% organic amendments, on lead (Pb) soil bioavailability and Pb absorption by the low-Pb accumulator kumquat (Citrus japonica Thunb.) 'Cuipi' in two typical Pb-contaminated soils, Jiyuan and Yangshuo, from northern and southern China, respectively. The diethylenetriaminepentaacetic acid-extractable Pb soil concentration and Pb accumulation in kumquat significantly decreased with amendment additions. High amendment doses had greater inhibitory effects than low doses but no significant effects on the kumquat's biomass in the two typical soils. Alkaline, but not clay mineral, amendments greatly increased the soil pH level. Organic amendments effectively reduced Pb accumulation owing to their strong adsorptive capacities. Thus, using organic amendments combined with a low-Pb accumulator kumquat forms a suitable farming practice for producing safe fruit in the two common types of Pb-contaminated soils in China.


Assuntos
Rutaceae , Poluentes do Solo , Disponibilidade Biológica , Frutas/química , Chumbo , Solo , Poluentes do Solo/análise
11.
Food Chem ; 360: 129822, 2021 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-33984564

RESUMO

ß-Cryptoxanthin (BCX) possesses potential therapeutic and health benefits. However, BCX absorption is low because of its poor aqueous solubility. In this study, a complex between BCX and casein (Cas) was prepared to improve the water dispersibility and bioavailability of BCX. BCX was recovered quantitatively from freeze-dried kumquat powder through solid-liquid extraction and saponification. The complexation significantly improved the apparent solubility of BCX under acidic and neutral conditions. A cell membrane permeation test using a Caco-2 cell monolayer was performed to evaluate the bioavailability of the BCX-Cas complex. This complex and a blank sample were digested in vitro and added to the apical side of the Caco-2 cell membrane. The quantity of BCX that permeated using the BCX-Cas complex after 24 h was 22.7 times greater than that of the blank. Thus, complexation of BCX with Cas improved dramatically the bioavailability of BCX from a kumquat extract.


Assuntos
beta-Criptoxantina/química , Caseínas/química , Rutaceae/química , Células CACO-2 , Humanos , Permeabilidade , Extratos Vegetais/química , Solubilidade , Água/química
12.
PLoS One ; 16(5): e0251534, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33970960

RESUMO

Melicope glabra (Blume) T. G. Hartley from the Rutaceae family is one of the richest sources of plant secondary metabolites, including coumarins and flavanoids. This study investigates the free radical scavenging and antibacterial activities of M. glabra and its isolated compounds. M. glabra ethyl acetate and methanol extracts were prepared using the cold maceration technique. The isolation of compounds was performed with column chromatography. The free radical scavenging activity of the extracts and isolated compounds were evaluated based on their oxygen radical absorbance capacity (ORAC) activities. The extracts and compounds were also subjected to antibacterial evaluation using bio-autographic and minimal inhibitory concentration (MIC) techniques against two oral pathogens, Enterococcus faecalis and Streptococcus mutans. Isolation of phytoconstituents from ethyl acetate extract successfully yielded quercetin 3, 5, 3'-trimethyl ether (1) and kumatakenin (2), while the isolation of the methanol extract resulted in scoparone (3), 6, 7, 8-trimethoxycoumarin (4), marmesin (5), glabranin (6), umbelliferone (7), scopoletin (8), and sesamin (9). The study is the first to isolate compound (1) from Rutaceae plants, and also the first to report the isolation of compounds (2-5) from M. glabra. The ORAC evaluation showed that the methanol extract is stronger than the ethyl acetate extract, while umbelliferone (7) exhibited the highest ORAC value of 24 965 µmolTE/g followed by glabranin (6), sesamin (9) and scopoletin (8). Ethyl acetate extract showed stronger antibacterial activity towards E. faecalis and S. mutans than the methanol extract with MIC values of 4166.7 ± 1443.4 µg/ml and 8303.3 ± 360.8 µg/ml respectively. Ethyl acetate extract inhibited E. faecalis growth, as shown by the lowest optical density value of 0.046 at a concentration of 5.0 mg/mL with a percentage inhibition of 95%. Among the isolated compounds tested, umbelliferone (7) and sesamin (9) exhibited promising antibacterial activity against S. mutans with both exhibiting MIC values of 208.3 ± 90.6 µg/ml. Findings from this study suggests M. glabra as a natural source of potent antioxidant and antibacterial agents.


Assuntos
Antibacterianos/farmacologia , Enterococcus faecalis/crescimento & desenvolvimento , Sequestradores de Radicais Livres/farmacologia , Casca de Planta/química , Extratos Vegetais/química , Rutaceae/química , Streptococcus mutans/crescimento & desenvolvimento , Antibacterianos/química , Sequestradores de Radicais Livres/química
13.
Molecules ; 26(6)2021 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-33799365

RESUMO

Dihydrofuranocoumarin, chalepin (1) and furanocoumarin, chalepensin (2) are 3-prenylated bioactive coumarins, first isolated from the well-known medicinal plant Ruta chalepensis L. (Fam: Rutaceae) but also distributed in various species of the genera Boenminghausenia, Clausena and Ruta. The distribution of these compounds appears to be restricted to the plants of the family Rutaceae. To date, there have been a considerable number of bioactivity studies performed on coumarins 1 and 2, which include their anticancer, antidiabetic, antifertility, antimicrobial, antiplatelet aggregation, antiprotozoal, antiviral and calcium antagonistic properties. This review article presents a critical appraisal of publications on bioactivity of these 3-prenylated coumarins in the light of their feasibility as novel therapeutic agents and investigate their natural distribution in the plant kingdom, as well as a plausible biosynthetic route.


Assuntos
Furocumarinas/biossíntese , Furocumarinas/farmacologia , Animais , Clausena/química , Cumarínicos/química , Humanos , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Ruta/química , Rutaceae/química
14.
Chem Biodivers ; 18(4): e2000999, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33738900

RESUMO

Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Despite its frequent use in traditional medicine, there is still a paucity of scientific information on T. asiatica growing on the tropical island of Mauritius. Therefore, the present study was designed to appraise the pharmacological and phytochemical profile of extracts (methanol, ethyl acetate and water) and essential oil obtained from aerial parts of T. asiatica. Biological investigation involved the evaluation of in vitro antioxidant and enzyme inhibitory potentials. The chemical profile of the EO was determined using gas chromatography coupled to mass spectrometry (GC/MS) analysis, while for the extracts, the total phenolic (TPC) and flavonoid content were quantified as well as their individual phenolic compounds by LC/MS/MS. Quinic acid, fumaric acid, chlorogenic acid, quercitrin and isoquercitrin were the main compounds in the extracts. Highest total phenolic (82.5±0.94 mg gallic acid equivalent (GAE/g)) and flavonoid (43.8±0.31 mg rutin equivalent (RE/g)) content were observed for the methanol extract. The GC/MS analysis has shown the presence of 26 compounds with linalool (30.9 %), linalyl acetate (20.9 %) and ß-phellandrene (7.9 %) being most abundant components in the EO. The extracts and EO showed notable antioxidant properties, with the methanol extract proved to be superior source of antioxidant compounds. Noteworthy anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE) effects were recorded for the tested samples, while only the methanol and ethyl acetate extracts were active against tyrosinase. With respect to antidiabetic effects, the extracts and EO were potent inhibitors of α-glucosidase, while modest activity was recorded against α-amylase. Docking results showed that linalyl acetate has the highest affinity to interact with the active site of BChE with docking score of -6.25 kcal/mol. The findings amassed herein act as a stimulus for further investigations of this plant as a potential source of bioactive compounds which can be exploited as phyto-therapeutics.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Rutaceae/química , Acetilcolinesterase/metabolismo , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Butirilcolinesterase/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Medicina Tradicional , Modelos Moleculares , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais/química , Espécies Reativas de Oxigênio/metabolismo , Ácidos Sulfônicos/antagonistas & inibidores , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
15.
Biomed Pharmacother ; 138: 111490, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33773465

RESUMO

This study was aimed to explore the mechanism of rutaecarpine (RUT) on ethanol-induced gastric ulcer (GU) in mice by integrated approaches. At first, the efficacy was determined through the macroscopic and microscopic state of stomach tissue and the expression levels of GU-related factors. Then, the serum metabolomics method based on UPLC-Q-TOF/MS was used to explore the specific metabolites and metabolic pathways. Finally, the upstream key protein targets of these specific metabolites were analyzed by network pharmacology and verified by PCR to explore the potential mechanism. RUT alleviated the histological and pathological damage of gastric tissue caused by ethanol, and could remarkably ameliorate the level of GU-related factors. Subsequently, a total of 7 potential metabolites involved in 9 metabolic pathways were identified by metabolomics analysis. Then, a 'component-targets-metabolites' interaction network was constructed, and therefore 4 key target proteins (PLA2G1B, PDE5A, MIF and SRC) that may regulate the specific metabolites were obtained. This case was further verified by the results of PCR. ALL the above results strongly demonstrated that RUT exerted a gastroprotective effect against GU. And it is the first time to combine metabolomics combined with network pharmacology to elucidate the mechanism of RUT on GU, which may be related to the regulation of energy metabolism, oxidative stress, and inflammation, and these pathways may be regulated through the upstream protein PLA2G1B, PDE5A, MIF and SRC.


Assuntos
Etanol/toxicidade , Alcaloides Indólicos/uso terapêutico , Metabolômica/métodos , Quinazolinas/uso terapêutico , Rutaceae , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/metabolismo , Animais , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Alcaloides Indólicos/farmacologia , Masculino , Camundongos , Quinazolinas/farmacologia , Úlcera Gástrica/induzido quimicamente
16.
Phytochemistry ; 186: 112744, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33780702

RESUMO

Two previously undescribed indole alkaloids, 3-prenyl-5(3-keto-but-1-enyl) indole and 3-prenyl-indole-5-carbaldehyde, the structurally-related 3,5-diprenyl indole and four known alkaloids were isolated from the leaves of Ravenia spectabilis Engl. Structures were elucidated based on nuclear magnetic resonance (1D and 2D NMR) spectroscopic and mass spectrometric analysis. The previously undescribed compounds isolated were subsequently screened against the HeLa (human cervical cancer), MIA PaCa-2 (human pancreatic adenocarcinoma) and A549 (lung cancer) cell lines. Among the isolated compounds, 3,5-diprenyl indole was the most cytotoxic across all three cell lines (MIA PaCa-2 IC50 = 9.5 ± 2.2 µM). Molecular modelling studies suggested DNA intercalation as the mode of action of these compounds.


Assuntos
Adenocarcinoma , Antineoplásicos Fitogênicos , Neoplasias Pancreáticas , Rutaceae , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Humanos , Alcaloides Indólicos/farmacologia , Estrutura Molecular , Neoplasias Pancreáticas/tratamento farmacológico , Folhas de Planta
17.
Molecules ; 26(4)2021 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-33671156

RESUMO

The objective of this paper is to compare conventional, ultrasound, microwave, and French press methods for the extraction of antioxidant compounds from Decatropis bicolor in an aqueous medium. This plant is widely used in Mexican traditional medicine for breast cancer treatment. Despite that, there are few studies on D. bicolor. Two response surface designs were applied to establish the best conditions of the liberation of antioxidants from D. bicolor, which were determined by DPPH• and Ferric Reducing Antioxidant Power (FRAP) techniques. The total phenolic content was evaluated by the Folin-Ciocalteu method. The results showed that D. bicolor is a source of antioxidants (669-2128 mg ET/100 g and 553-1920 mg EFe2+/100 g, respectively) and phenolic compounds (2232-9929 mg EGA/100 g). Among the physical factors that were analyzed, the temperature was the determinant factor to liberate the compounds of interest by using low concentrations of the sample and short times of extraction. The French press was the most efficient method, obtaining values of antioxidant activity and phenolic compounds even higher than those reported by using extraction methods with solvents such as methanol.


Assuntos
Antioxidantes/isolamento & purificação , Bioquímica/métodos , Rutaceae/química , Água/química , Antioxidantes/análise , Compostos de Bifenilo/química , Ferro/química , Micro-Ondas , Fenóis/análise , Picratos/química , Ultrassom
18.
J Ethnopharmacol ; 271: 113887, 2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-33539951

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Melicope accedens (Blume) Thomas G. Hartley is a plant included in the family Rutaceae and genus Melicope. It is a native plant from Vietnam that has been used for ethnopharmacology. In Indonesia and Malaysia, the leaves of M. accedens are applied externally to decrease fever. AIM OF THE STUDY: The molecular mechanisms of the anti-inflammatory properties of M. accedens are not yet understood. Therefore, we examined those mechanisms using a methanol extract of M. accedens (Ma-ME) and determined the target molecule in macrophages. MATERIALS AND METHODS: We evaluated the anti-inflammatory effects of Ma-ME in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and in an HCl/EtOH-triggered gastritis model in mice. To investigate the anti-inflammatory activity, we performed a nitric oxide (NO) production assay and ELISA assay for prostaglandin E2 (PGE2). RT-PCR, luciferase gene reporter assays, western blotting analyses, and a cellular thermal shift assay (CETSA) were conducted to identify the mechanism and target molecule of Ma-ME. The phytochemical composition of Ma-ME was analyzed by HPLC and LC-MS/MS. RESULTS: Ma-ME suppressed the production of NO and PGE2 and the mRNA expression of proinflammatory genes (iNOS, IL-1ß, and COX-2) in LPS-stimulated RAW264.7 cells without cytotoxicity. Ma-ME inhibited NF-κB activation by suppressing signaling molecules such as IκBα, Akt, Src, and Syk. Moreover, the CETSA assay revealed that Ma-ME binds to Syk, the most upstream molecule in the NF-κB signal pathway. Oral administration of Ma-ME not only alleviated inflammatory lesions, but also reduced the gene expression of IL-1ß and p-Syk in mice with HCl/EtOH-induced gastritis. HPLC and LC-MS/MS analyses confirmed that Ma-ME contains various anti-inflammatory flavonoids, including quercetin, daidzein, and nevadensin. CONCLUSIONS: Ma-ME exhibited anti-inflammatory activities in vitro and in vivo by targeting Syk in the NF-κB signaling pathway. Therefore, we propose that Ma-ME could be used to treat inflammatory diseases such as gastritis.


Assuntos
Anti-Inflamatórios/farmacologia , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Rutaceae/química , Quinase Syk/metabolismo , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Ciclo-Oxigenase 2/genética , Dinoprostona/metabolismo , Modelos Animais de Doenças , Etanol/toxicidade , Gastrite/induzido quimicamente , Gastrite/tratamento farmacológico , Gastrite/patologia , Células HEK293 , Humanos , Ácido Clorídrico/toxicidade , Inflamação/genética , Interleucina-1beta/genética , Lipopolissacarídeos/toxicidade , Masculino , Metanol/química , Camundongos , Camundongos Endogâmicos ICR , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos
19.
Food Chem Toxicol ; 149: 112031, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33529679

RESUMO

Hepatocellular carcinoma (HCC) is one of the most common fatal malignant tumors. Glycosmis pentaphylla is used by traditional medical practitioners worldwide to treat various diseases. We isolated and identified a chemical component with potential anti-hepatocellular carcinoma (HCC) effects. Methylgerambullin is a sulfur containing amine and has significant antihepatoma activity in vitro and in vivo. Methylgerambullin was significantly cytotoxic to HCC cells and induces apoptosis in HCC cells. In addition, methylgerambullin is able to inhibit the growth of transplanted tumors in nude mice without significant toxicity. Regarding the anti-cancer mechanism of methylgerambullin, treatment with methylgerambullin increased the expression of caspase-3, caspase-9 and Bax in vitro and in vivo and reduce the expression of B-cell lymphoma-2 (Bcl-2). Simultaneously, methylgerambullin can also affect ERS-related proteins, inhibit Protein Kinase B (Akt) activity, cause dephosphorylation of downstream Bad, and inhibit the expression of the Signal Transducer and Activator of Transcription 3 (STAT3) protein to inhibit HCC cells proliferation. Overall, these results suggest that methylgerambullin can inhibit HCC cells proliferation by inducing mitochondrial apoptosis, activating ERS signaling pathways and inhibiting the Akt and STAT3 pathways.


Assuntos
Amidas/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Rutaceae/química , Compostos de Enxofre/farmacologia , Amidas/administração & dosagem , Amidas/química , Animais , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , Camundongos Nus , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Folhas de Planta , Distribuição Aleatória , Compostos de Enxofre/administração & dosagem , Compostos de Enxofre/química
20.
Proc Natl Acad Sci U S A ; 118(6)2021 02 09.
Artigo em Inglês | MEDLINE | ID: mdl-33526689

RESUMO

Citrus Huanglongbing (HLB), caused by a vector-transmitted phloem-limited bacterium Candidatus Liberibacter asiaticus (CLas), is the most devastating citrus disease worldwide. Currently, there are no effective strategies to prevent infection or to cure HLB-positive trees. Here, using comparative analysis between HLB-sensitive citrus cultivars and HLB-tolerant citrus hybrids and relatives, we identified a novel class of stable antimicrobial peptides (SAMPs). The SAMP from Microcitrus australiasica can rapidly kill Liberibacter crescens (Lcr), a culturable Liberibacter strain, and inhibit infections of CLas and CL. solanacearum in plants. In controlled greenhouse trials, SAMP not only effectively reduced CLas titer and disease symptoms in HLB-positive trees but also induced innate immunity to prevent and inhibit infections. Importantly, unlike antibiotics, SAMP is heat stable, making it better suited for field applications. Spray-applied SAMP was taken up by citrus leaves, stayed stable inside the plants for at least a week, and moved systemically through the vascular system where CLas is located. We further demonstrate that SAMP is most effective on α-proteobacteria and causes rapid cytosol leakage and cell lysis. The α-helix-2 domain of SAMP is sufficient to kill Lcr Future field trials will help determine the efficacy of SAMP in controlling HLB and the ideal mode of application.


Assuntos
Citrus/efeitos dos fármacos , Doenças das Plantas/prevenção & controle , Proteínas Citotóxicas Formadoras de Poros/farmacologia , Rutaceae/química , Citrus/microbiologia , Resistência à Doença/genética , Liberibacter/efeitos dos fármacos , Liberibacter/patogenicidade , Doenças das Plantas/genética , Doenças das Plantas/microbiologia , Folhas de Planta/microbiologia , Proteínas Citotóxicas Formadoras de Poros/química , Proteínas Citotóxicas Formadoras de Poros/genética
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