Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 512
Filtrar
1.
Viruses ; 14(7)2022 06 30.
Artigo em Inglês | MEDLINE | ID: mdl-35891417

RESUMO

Despite the success of combination antiretroviral therapy (cART), HIV persists in low- and middle-income countries (LMIC) due to emerging drug resistance and insufficient drug accessibility. Furthermore, cART does not target latently-infected CD4+ T cells, which represent a major barrier to HIV eradication. The "shock and kill" therapeutic approach aims to reactivate provirus expression in latently-infected cells in the presence of cART and target virus-expressing cells for elimination. An attractive therapeutic prototype in LMICs would therefore be capable of simultaneously inhibiting viral replication and inducing latency reversal. Here we report that Gnidia sericocephala, which is used by traditional health practitioners in South Africa for HIV/AIDS management to supplement cART, contains at least four daphnane-type compounds (yuanhuacine A (1), yuanhuacine as part of a mixture (2), yuanhuajine (3), and gniditrin (4)) that inhibit viral replication and/or reverse HIV latency. For example, 1 and 2 inhibit HIV replication in peripheral blood mononuclear cells (PBMC) by >80% at 0.08 µg/mL, while 1 further inhibits a subtype C virus in PBMC with a half-maximal effective concentration (EC50) of 0.03 µM without cytotoxicity. Both 1 and 2 also reverse HIV latency in vitro consistent with protein kinase C activation but at 16.7-fold lower concentrations than the control prostratin. Both 1 and 2 also reverse latency in primary CD4+ T cells from cART-suppressed donors with HIV similar to prostratin but at 6.7-fold lower concentrations. These results highlight G. sericocephala and components 1 and 2 as anti-HIV agents for improving cART efficacy and supporting HIV cure efforts in resource-limited regions.


Assuntos
Diterpenos , Infecções por HIV , HIV-1 , Plantas Medicinais , Thymelaeaceae , Linfócitos T CD4-Positivos , Cromatografia Líquida de Alta Pressão , Diterpenos/farmacologia , Diterpenos/uso terapêutico , HIV-1/fisiologia , Humanos , Leucócitos Mononucleares/metabolismo , Ativação Viral , Latência Viral
2.
Molecules ; 27(14)2022 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-35889407

RESUMO

As a valuable medicinal herb and spice, agarwood is widely used in the fields of daily chemistry, traditional medicine, religion and literary collection. It mainly contains sesquiterpenes and 2-(2-phenylethyl)chromones, which are often used to soothe the body and mind, relieve anxiety, act as an antidepressant and treat insomnia and other mental disorders, presenting a good calming effect. This paper reviews the chemical composition of the essential oils of different sources of agarwood, as well as the progress of research on the sedative and tranquilizing pharmacological activity and mechanism of action of agarwood essential oil (AEO), and then analyzes the current problems of AEO research and its application prospects in the treatment of mental diseases.


Assuntos
Óleos Voláteis , Distúrbios do Início e da Manutenção do Sono , Thymelaeaceae , Ansiedade/tratamento farmacológico , Depressão , Humanos , Óleos Voláteis/química , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Thymelaeaceae/química
3.
PLoS One ; 17(6): e0270167, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35709217

RESUMO

Recently, Qi-Nan germplasm, the germplasm of Aquilaria species that easily forms agarwood, has been widely cultivated in Guangdong and Hainan Provinces in China. Since the morphological characteristics of Qi-Nan germplasm are similar to those of Aquilaria species and germplasm is bred by grafting, it is difficult to determine the source species of this germplasm by traditional taxonomic characteristics. In this study, we performed a DNA barcoding analysis of 58 major Qi-Nan germplasms as well as Aquilaria sinensis, A. yunnanensis, A. crassna, A. malaccensis and A. hirta with 5 primers (nuclear gene internal transcribed spacer 2 (ITS2) and the chloroplast genes matK, trnH-psbA, rbcL and trnL-trnF). This field survey in the Qi-Nan germplasm plantations in Guangdong and Hainan Provinces aimed to accurately identify the source species of Qi-Nan germplasm. According to the results, ITS2 and matK showed the most variability and the highest divergence at all genetic distances. This ITS2+matK combination, screened for with TaxonDNA analysis, showed the highest success rate in species identification of the Qi-Nan germplasm. Clustering in the phylogenetic trees constructed with Bayesian inference and maximum likelihood indicated that the Qi-Nan germplasm was most closely related to A. sinensis and more distantly related to A. yunnanensis, A. crassna, A. malaccensis and A. hirta. Therefore, this study determined that the source species of the Qi-Nan germplasm is A. sinensis.


Assuntos
Melhoramento Vegetal , Thymelaeaceae , Teorema de Bayes , China , Código de Barras de DNA Taxonômico/métodos , DNA de Plantas/genética , Filogenia , Thymelaeaceae/genética
4.
J Org Chem ; 87(12): 7643-7648, 2022 06 17.
Artigo em Inglês | MEDLINE | ID: mdl-35658440

RESUMO

Aquilarines A (1) and B (2), two unprecedented sesquiterpenoid-chromone heterohybrids, were isolated from Aquilaria sinensis agarwood. 1 is an alkaloid featuring an unusual pyridine nucleus, and 2 possesses a rare sesquiterpenoid-chromone skeleton via a C-C bond. A plausible biosynthetic pathway for 1 and 2 was proposed. Both 1 and 2 could significantly inhibit the expression of extracellular matrix components, and α-SMA at low concentrations in TGF-ß1 induced two types of kidney cells (NRK 52E and NRK 49F) featuring selective inhibition of Smad3 instead of Smad2 phosphorylation, showing their potential in renal fibrosis.


Assuntos
Sesquiterpenos , Thymelaeaceae , Cromonas , Fibrose , Humanos , Fosforilação , Sesquiterpenos/farmacologia , Proteína Smad3 , Thymelaeaceae/química
5.
ScientificWorldJournal ; 2022: 3992660, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35734014

RESUMO

Phaleria macrocarpa is a medicinal plant widely used in Indonesian folk medicine to treat several diseases, including cancer. However, the comparative evaluation of various plant parts of P. macrocarpa has not been studied for their anticancer properties on breast cancer. The study aimed to assess the antiproliferative activity of the ethanol extract of various parts of Phaleria macrocarpa against T47D human breast cancer cell lines. Several parts of P. macrocarpa, including pericarp, mesocarp, seed, and leaf, were used to determine the most potent plant part to inhibit the growth of T47D cells. The cytotoxic effects of each plant part were evaluated by WST-1 assay. The apoptotic level of T47D cells was determined by annexin V-FITC-PI and DNA fragmentation assay. Propidium iodide staining and the CFSE assay were used to examine the effect of each extract on cell cycle distribution and cell division, respectively. The relative number of caspase-3, Bax, and Bcl-2 was analyzed by flow cytometry technique. WST-1 assay revealed that P. macrocarpa leaves exhibited the most potent antiproliferative activity (p < 0.05) compared to other plant parts with selectivity only to T47D cells. P. macrocarpa leaves extract effectively induced apoptosis, inhibited proliferation, and arrested the cell cycle of T47D cells. The relative number of caspase-3 was significantly (p < 0.05) increased after being treated with P. macrocarpa leaf extract. P. macrocarpa leaf extract also leads to the dose-dependent accumulation in the Bax/Bcl-2 ratio due to upregulation of Bax and downregulation of Bcl-2. The overall results indicated that P. macrocarpa leaves could inhibit the proliferation of T47D cells and trigger apoptosis through caspase-3 activation and Bax/Bcl regulation. Therefore, P. macrocarpa leaves can be used for breast cancer therapy.


Assuntos
Neoplasias da Mama , Thymelaeaceae , Apoptose , Neoplasias da Mama/metabolismo , Caspase 3/farmacologia , Linhagem Celular Tumoral , Proliferação de Células , Feminino , Humanos , Extratos Vegetais/farmacologia , Proteína X Associada a bcl-2/farmacologia
6.
Molecules ; 27(11)2022 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-35684324

RESUMO

Agarwood, popularly known as oudh or gaharu, is a fragrant resinous wood of high commercial value, traded worldwide and primarily used for its distinctive fragrance in incense, perfumes, and medicine. This fragrant wood is created when Aquilaria trees are wounded and infected by fungi, producing resin as a defense mechanism. The depletion of natural agarwood caused by overharvesting amidst increasing demand has caused this fragrant defensive resin of endangered Aquilaria to become a rare and valuable commodity. Given that instances of natural infection are quite low, artificial induction, including biological inoculation, is being conducted to induce agarwood formation. A long-term investigation could unravel insights contributing toward Aquilaria being sustainably cultivated. This review will look at the different methods of induction, including physical, chemical, and biological, and compare the production, yield, and quality of such treatments with naturally formed agarwood. Pharmaceutical properties and medicinal benefits of fragrance-associated compounds such as chromones and terpenoids are also discussed.


Assuntos
Perfumes , Thymelaeaceae , Odorantes , Perfumes/análise , Resinas Vegetais/análise , Thymelaeaceae/química , Árvores , Madeira/química
7.
Phytochemistry ; 201: 113275, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35718134

RESUMO

Five undescribed sesquiterpenoids stellerasespenes A‒E and four reported congeners were isolated from the roots of Stellera chamaejasme. The structures were elucidated by comprehensive spectroscopic analyses together with X-ray single crystal diffraction and theoretical calculations. The structure of holosericin B was revised. All the isolated compounds were evaluated for NO production in murine microglial BV2 cells induced by LPS. Stellerasespene A showed better inhibitory activity than the positive control minocycline, inhibiting NO production and overexpression of pro-inflammatory cytokine IL-1ß in LPS-activated BV2 cells.


Assuntos
Sesquiterpenos , Thymelaeaceae , Animais , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Raízes de Plantas/química , Sesquiterpenos/química , Thymelaeaceae/química
8.
Microsc Res Tech ; 85(8): 2904-2912, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35491427

RESUMO

Agarwood, a non-timber fragrant wood, is derived from wounded Aquilaria trees (Thymelaeaceae) and is widely used in traditional medicine, incense and perfume. Agarwood-like substances and programmed cell death (PCD) can be induced by wounding signals in the suspension cells and aerial roots of Aquilaria sinensis. In this study, the dynamic process of wound-induced agarwood formation in stems of A. sinensis was observed, and the occurrence of PCD was synchronously detected using techniques such as 4',6-diamidino-2-phenylindole and dUTP nick-end labeling staining. The results showed that the wounding was a induce signal for agarwood resin formation, meanwhile might induce PCD. Interxylary phloem and xylem ray were the main sites of agarwood resin formation and PCD occurrence. There might be a relationship between the spatiotemporal pattern of PCD and agarwood resin formation: more severe PCD corresponded to a higher rate of resin formation but a shorter resin formation time; conversely, slower PCD progression corresponded to a lower rate of resin formation but a longer resin formation time. Our findings are the first to demonstrate that PCD might occur in the process of wound-induced agarwood formation at the tree level, and the spatiotemporal pattern is closely related to the formation of agarwood resin. This study provides valuable insight for further studies on the relationship between PCD and agarwood formation. HIGHLIGHTS: Programmed cell death (PCD) might occur in the process of wound-induced agarwood formation at the tree level. Interxylary phloem and xylem ray were the main sites of agarwood resin formation and PCD occurrence. Spatiotemporal pattern of PCD might have a strong impact on agarwood resin formation.


Assuntos
Thymelaeaceae , Apoptose , Resinas Vegetais , Thymelaeaceae/metabolismo , Madeira
9.
Sci Rep ; 12(1): 7194, 2022 05 03.
Artigo em Inglês | MEDLINE | ID: mdl-35505005

RESUMO

The basic helix-loop-helix (bHLH) transcription factors are involved in several biological processes both in plant development and stress responses. Agarwood, a major active and economical product, is only induced and accumulated when the roots, stems, or branches are wounded in Aquilaria sinensis. Although genome-wide comprehensive analyses of the bHLH family have been identified in many plants, no systematic study of the genes in this family has been conducted in A. sinensis. In this study, 105 bHLH genes were identified in A. sinensis through genome-wide analysis and named according to their chromosomal locations. Based on a phylogenetic tree, AsbHLH family proteins were classified into 18 subfamilies. Most of them were distributed on eight chromosomes, with the exception of two genes. Based on the tissue-specific expression characteristics and expression patterns in response to methyl jasmonate (MeJA) treatment, seven AsbHLH genes were likely involved in wound-induced agarwood formation. The results provide comprehensive information on AsbHLHs that can be used to elucidate the molecular functions and physiological roles of these proteins in A. sinensis.


Assuntos
Fatores de Transcrição Hélice-Alça-Hélice Básicos , Thymelaeaceae , Fatores de Transcrição Hélice-Alça-Hélice Básicos/metabolismo , Genoma de Planta , Família Multigênica , Filogenia , Thymelaeaceae/genética , Thymelaeaceae/metabolismo
10.
Molecules ; 27(9)2022 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-35566388

RESUMO

The inflammatory response is a central aspect of the human immune system that acts as a defense mechanism to protect the body against infections and injuries. A dysregulated inflammatory response is a major health concern, as it can disrupt homeostasis and lead to a plethora of chronic inflammatory conditions. These chronic inflammatory diseases are one of the major causes of morbidity and mortality worldwide and the need for them to be managed in the long term has become a crucial task to alleviate symptoms and improve patients' overall quality of life. Although various synthetic anti-inflammatory agents have been developed to date, these medications are associated with several adverse effects that have led to poor therapeutic outcomes. The hunt for novel alternatives to modulate underlying chronic inflammatory processes has unveiled nature to be a plentiful source. One such example is agarwood, which is a valuable resinous wood from the trees of Aquilaria spp. Agarwood has been widely utilized for medicinal purposes since ancient times due to its ability to relieve pain, asthmatic symptoms, and arrest vomiting. In terms of inflammation, the major constituent of agarwood, agarwood oil, has been shown to possess multiple bioactive compounds that can regulate molecular mechanisms of chronic inflammation, thereby producing a multitude of pharmacological functions for treating various inflammatory disorders. As such, agarwood oil presents great potential to be developed as a novel anti-inflammatory therapeutic to overcome the drawbacks of existing therapies and improve treatment outcomes. In this review, we have summarized the current literature on agarwood and its bioactive components and have highlighted the potential roles of agarwood oil in treating various chronic inflammatory diseases.


Assuntos
Qualidade de Vida , Thymelaeaceae , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Humanos , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Madeira
11.
Curr Microbiol ; 79(5): 151, 2022 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-35397007

RESUMO

Aquilaria malaccensis, the resinous agarwood, is highly valued in the perfumery and medicinal industry. The formation of fragrant agarwood resin inconsistently by various fungi is still not clearly understood. The current study investigated the agarwood quality and fungal diversity in artificially inoculated and naturally infected A. malaccensis. The chemical analysis of volatile compounds of agarwood was performed using the Solid Phase Micro Extraction (SPME) method, and the identification of fungi was made through a morphological observation using a light microscope. Gas chromatography analysis revealed the presence of essential compounds related to high-quality agarwood, such as 4-phenyl-2-butanone, ß-selinene, α-bulnesene, and agarospirol in both artificially inoculated and naturally infected agarwood but with some differences in the abundance. Further studies on the fungi associated with agarwood volatile compounds formation showed a total of ten fungal group isolates, which were identified based on morphological and molecular studies. The study revealed that agarwood from both artificial and natural sources were naturally infected with Fusarium, Botryosphaeria, Aspergillus, Schizophyllum, Phanerochaete, Lasiodiplodia, Polyporales, and Ceriporia species. This study has offered a potential opportunity to research further the promising development of fungal strains for artificial inducement of high-quality agarwood formation from A. malaccensis trees.


Assuntos
Ascomicetos , Fusarium , Polyporales , Thymelaeaceae , Odorantes , Thymelaeaceae/microbiologia
12.
Prog Chem Org Nat Prod ; 118: 47-100, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35416517

RESUMO

The phytochemistry of the fragrant infected heartwood of Aquilaria and Gyrinops species, agarwood (oud), is critically reviewed, highlighting the use of this remarkable natural raw material in perfumery. The chemistry of the two main groups of constituents of agarwood (sesquiterpenoids and chromones) is discussed, focusing particularly on the former structural type. The identities of the main key odorants of agarwood essential oil and of the smoke produced by heating the wood of agarwood are also discussed.


Assuntos
Sesquiterpenos , Thymelaeaceae , Cromonas/análise , Cromonas/química , Odorantes/análise , Sesquiterpenos/química , Thymelaeaceae/química , Madeira/química
13.
J Tradit Chin Med ; 42(2): 187-193, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35473338

RESUMO

OBJECTIVE: To observe the effects of the flower of Edgeworthia gardneri (Wall.) Meisn (EWM) on glucose and lipid metabolism in KK/upj-Ay/J (KKAy) mice and investigate the possible mechanism of EWM in the liver of KKAy mice by transcriptome analysis. METHODS: Forty KKAy mice were fed a high-sugar and high-fat diet for 3 weeks to establish the animal model of metabolic syndrome. After 5 weeks of continuous administration of EWM, serum high-density lipoprotein (HDL), low-density lipoprotein (LDL), triglycerides (TG), total cholesterol (TC), and free fatty acids (FFA) were detected by radioimmunoassay. Serum fasting insulin (Fins) and adiponectin levels were measured by enzyme-linked immunosorbent assay. Liver tissue fixed with paraformaldehyde was stained with hematoxylin-eosin and oil red O. Transcriptome analysis was used to evaluate the liver tissue. The expressions of lipoprotein lipase (LPL), peroxisome proliferator-activated receptor-γ (PPARγ), adenosine 5'-monophosphate-activated protein kinase (AMPK), sterol regulatory element binding protein-1c (SREBP-1c), and fatty acid synthase (Fas) mRNA and protein in liver tissue were detected by reverse transcription-polymerase chain reaction (RT-PCR) and Western blot analysis. RESULTS: EWM slightly reduced FBG and Fins in KKAy mice. Furthermore, EWM was able to downregulate serum LDL, TG, TC, and FFA and upregulate the expression of serum HDL and adiponectin. Transcriptome analysis revealed the following differential pathways: the peroxisome proliferator-activated receptor (PPAR) signaling pathway and the AMPK signaling pathway. RT-PCR and western blot analysis detected the associated genes and proteins. In addition, EWM was able to upregulate the expression of AMPK and downregulate the expression of PPARγ, SREBP1c, and Fas mRNA and protein and upregulate the expression of LPL mRNA. CONCLUSIONS: EWM can alleviate lipid metabolism disorders and to some extent improve glucose metabolism disorders in KKAy mice. These effects may be related to regulating PPARγ/LPL and activating the AMPK/SREBP1c/Fas pathway.


Assuntos
Metabolismo dos Lipídeos , Thymelaeaceae , Proteínas Quinases Ativadas por AMP/metabolismo , Adiponectina/metabolismo , Animais , Flores , Glucose , Humanos , Camundongos , PPAR gama/genética , RNA Mensageiro/metabolismo , Proteína de Ligação a Elemento Regulador de Esterol 1/genética , Proteína de Ligação a Elemento Regulador de Esterol 1/metabolismo , Thymelaeaceae/metabolismo , Triglicerídeos
14.
Eur J Med Chem ; 237: 114397, 2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35472851

RESUMO

2-(2-Phenylethyl)chromones (PECs) are a group of naturally occurring compounds, which are characterized as phenylethyl substituent at the C2 position of chromone. They have been isolated mainly from Aquilaria sinensis (Lour.) Gilg. This type of natural compound is correlative with anti-diabetes, anticancer, antioxidant, antibacterial, anticancer, and anti-inflammatory activities. Due to the versatile activities of PECs, more and more researchers use different improved methods to synthesize them and their derivatives. This review mainly focuses on the natural occurrence, chemical synthesis, and biological activities of PECs, which were published up until 2020.


Assuntos
Medicamentos de Ervas Chinesas , Thymelaeaceae , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/química , Cromonas/química , Cromonas/farmacologia , Medicamentos de Ervas Chinesas/química , Flavonoides/química , Estrutura Molecular , Thymelaeaceae/química
15.
Arch Insect Biochem Physiol ; 110(3): e21892, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35478464

RESUMO

To explore the toxicity mechanisms of neochamaejasmin B (NCB) extracted from Stellera chamaejasme L., we first evaluated its cytotoxicity in neuronal cells of Helicoverpa zea (AW1 cells). NCB inhibited cell growth and was cytotoxic to AW1 cells in a dose-dependent manner. Further, transmission electron microscopy (TEM) was used to analyze the microstructure, and typical apoptotic characteristics were observed in AW1 cells treated with NCB. Moreover, the NCB-induced apoptosis was dose dependent. Subsequently, we explored the mechanism of apoptosis. A decline in the mitochondrial membrane potential (MMP) was found. Also, the levels of Bax were increased with increases in drug concentration, but there was no statistical difference in Bcl-2 levels at different NCB doses. Caspase-3 and caspase-10 activity was increased. These findings confirmed that NCB induced apoptosis in AW1 cells through a caspase-10-dependent mechanism. The results provide the basic information needed for understanding the toxicity and mechanisms of action of NCB, which could potentially be used to develop NCB as a new insecticide.


Assuntos
Thymelaeaceae , Animais , Apoptose , Biflavonoides , Caspase 10/metabolismo , Insetos , Thymelaeaceae/química , Thymelaeaceae/metabolismo
16.
J Sep Sci ; 45(13): 2394-2405, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35461190

RESUMO

A novel strategy of performing ligand fishing with enzyme-modified open tubular microchannel was proposed for screening bioactive components present in medicinal plants. Monoamine oxidase B was immobilized onto the surface of the microchannel for the first time to specifically extract its ligands when the plant's extracts solution flows through the channel. The thermal and the storage stability of immobilized monoamine oxidase B were significantly enhanced after immobilization. Crocin I and Ⅱ were extracted from Crocus sativus, and tiliroside was extracted from Edgeworthia gardneri. All the three compounds were inhibitors of the enzyme with the half-maximal inhibitory concentration values of 26.70 ±â€¯0.91, 19.88 ±â€¯2.78, and 15.65 ± 0.85 µM, respectively. The enzyme inhibition kinetics and molecular docking were investigated. This is the first report on the inhibitory effects of tiliroside and crocin Ⅱ. The novel ligand fishing method proposed in this work possesses advantages of rapidness, high efficiency, and tiny sample consumption compared to routine ligand fishing, with promising potential for screening active natural products in complex mixtures.


Assuntos
Crocus , Thymelaeaceae , Caça , Ligantes , Simulação de Acoplamento Molecular , Monoaminoxidase , Extratos Vegetais/farmacologia
17.
Fitoterapia ; 158: 105171, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35288211

RESUMO

Sixteen guaiane-type sesquiterpenoids were isolated from Stellera chamaejasme L. Among them, chamaejasnoids A-F (1-5) are new compounds. 1 represents the first example of 2,3-seco-guaiane sesquiterpenoid with a 5/6/7 bridged ring system. 2 is a unique 2-nor-guaiane sesquiterpenoid. A plausible biosynthetic pathway for 1 was proposed, involving a Baeyer-Villiger oxidation and a non-enzymatic intramolecular transesterification. 5 exhibited a selective cytotoxicity against HCT8 cell line with an IC50 of 11.82 ± 2.89 µM.


Assuntos
Sesquiterpenos , Thymelaeaceae , Estrutura Molecular , Sesquiterpenos/farmacologia , Sesquiterpenos de Guaiano
18.
Fitoterapia ; 159: 105177, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35302005

RESUMO

Seven new 2-(2-Phenethyl) chromone derivatives (1-7), including four 2-(2-Phenethyl) chromones (1-4), one 6, 7, 8 trihydroxy-2-(2-Phenethyl) chromone (5), one acetylated 5, 6, 7, 8-tetrahydroxy-2-(2-Phenethyl) chromone (6), and one chlorine-containing 5, 6, 7, 8-tetrahydro-2-(2-Phenethyl) chromone (7), along with eight known compounds (8-15), were isolated from agarwood originating from Aquilaria agallocha Roxb.. Their structures were determined mainly by high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) and nuclear magnetic resonance (NMR) analysis. The absolute configurations of 3-7 were resolved by electronic circular dichroism (ECD) calculations. Nearly all compounds were evaluated for their anti-inflammatory activities in RAW264.7 cells. Compounds 1 and 7-11 displayed significant anti-inflammatory activities with IC50 values ranging from 3.71 to 32.04 µM.


Assuntos
Cromonas , Thymelaeaceae , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Cromonas/química , Cromonas/farmacologia , Flavonoides/química , Estrutura Molecular , Óxido Nítrico , Thymelaeaceae/química
19.
Fitoterapia ; 158: 105162, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35217119

RESUMO

Six new 2-(2-phenylethyl)chromone dimers (1-6) were isolated from ethyl ether extract of red soil agarwood of Aquilaria crassna from Vietnam by LC-MS-guided fractionation procedure. Their structures were unambiguously elucidated based on HRESIMS, 1D and 2D NMR spectra. The absolute configuration of 2-(2-phenylethyl)chromone dimers was determined by comparison of the experimental and computed ECD spectra. Compound 6 displayed cytotoxicity against the human myeloid leukemia cell line (K562) with an IC50 value of 39.49 µM.


Assuntos
Cromonas , Thymelaeaceae , Cromatografia Líquida , Cromonas/química , Flavonoides/química , Humanos , Estrutura Molecular , Solo , Espectrometria de Massas em Tandem , Thymelaeaceae/química , Madeira/química
20.
Molecules ; 27(3)2022 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-35163893

RESUMO

Aquilaria sinensis (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of A. sinensis flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and PPARγ), liver X receptor (LXR), glucose uptake, and lipid accumulation (adipogenesis). Activation of PPARα, PPARγ and LXR was determined in hepatic (HepG2) cells by reporter gene assays. Glucose uptake was determined in differentiated muscle (C2C12) cells using 2-NBDG (2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]-D-glucose). Adipogenesis was determined in adipocytes (3T3-L1 cells) by Oil red O staining. At a concentration of 50 µg/mL, AF caused 12.2-fold activation of PPARα and 5.7-fold activation of PPARγ, while the activation of LXR was only 1.7-fold. AF inhibited (28%) the adipogenic effect induced by rosiglitazone in adipocytes and increased glucose uptake (32.8%) in muscle cells at 50 µg/mL. It was concluded that AF acted as a PPARα/γ dual agonist without the undesired effect of adipogenesis and exhibited the property of enhancing glucose uptake. This is the first report to reveal the PPARα/γ dual agonistic action and glucose uptake enhancing property of AF along with its antiadipogenic effect, indicating its potential in ameliorating the symptoms of metabolic syndrome.


Assuntos
Síndrome Metabólica , Thymelaeaceae , Células 3T3-L1 , Adipogenia , Animais , Flores/metabolismo , Síndrome Metabólica/tratamento farmacológico , Camundongos , PPAR gama/metabolismo , Extratos Vegetais/farmacologia , Thymelaeaceae/metabolismo
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...