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1.
Molecules ; 28(15)2023 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-37570877

RESUMO

Aralia elata, a renowned medicinal plant with a rich history in traditional medicine, has gained attention for its potential therapeutic applications. However, the leaves of this plant have been largely overlooked and discarded due to limited knowledge of their biological activity and chemical composition. To bridge this gap, a comprehensive study was conducted to explore the therapeutic potential of the 70% ethanol extract derived from Aralia elata leaves (LAE) for the treatment of cardiovascular disease (CVD). Initially, the cytotoxic effects of LAE on human umbilical vein endothelial cells (HUVECs) were assessed, revealing no toxicity within concentrations up to 5 µg/mL. This suggests that LAE could serve as a safe raw material for the development of health supplements and drugs aimed at promoting cardiovascular well-being. Furthermore, the study found that LAE extract demonstrated anti-inflammatory properties in HUVECs by modulating the PI3K/Akt and MAPK signaling pathways. These findings are particularly significant as inflammation plays a crucial role in the progression of CVD. Moreover, LAE extract exhibited the ability to suppress the expression of adhesion molecules VCAM-1 and ICAM-1, which are pivotal in leukocyte migration to inflamed blood vessels observed in various pathological conditions. In conjunction with the investigation on therapeutic potential, the study also established an optimal HPLC-PDA-ESI-MS/MS method to identify and confirm the chemical constituents present in 24 samples collected from distinct regions in South Korea. Tentative identification revealed the presence of 14 saponins and nine phenolic compounds, while further analysis using PCA and PLS-DA allowed for the differentiation of samples based on their geographical origins. Notably, specific compounds such as chlorogenic acid, isochlorogenic acid A, and quercitrin emerged as marker compounds responsible for distinguishing samples from different regions. Overall, by unraveling its endothelial protective activity and identifying key chemical constituents, this research not only offers valuable insights for the development of novel treatments but also underscores the importance of utilizing and preserving natural resources efficiently.


Assuntos
Aralia , Espectrometria de Massas em Tandem , Humanos , Aralia/química , Fosfatidilinositol 3-Quinases , Extratos Vegetais/farmacologia , Extratos Vegetais/análise , Etanol/química , Células Endoteliais da Veia Umbilical Humana , Folhas de Planta/química
2.
Sci Rep ; 12(1): 20375, 2022 11 27.
Artigo em Inglês | MEDLINE | ID: mdl-36437256

RESUMO

Mulberry leaf (Mori Folium) extract (MLE) is known to have anti-obesity effects. In this study, the enhanced effects of MLE after bioconversion treatment using Pectinex (BMLE) on obesity were explored, and the underlying mechanisms were investigated using the active components, neochlorogenic acid (5-CQA) and cryptochlorogenic acid (4-CQA), whose amounts were increased by bioconversion of MLE. Both MLE and BMLE inhibited lipid accumulation in 3T3-L1 adipocytes without cytotoxicity and suppressed the expression of CCAAT/enhancer-binding protein alpha (C/EBPα). In addition, MLE and BMLE decreased high-fat diet-induced adipose tissue mass expansion. Notably, BMLE significantly increased antiadipogenic and anti-obesity effects compared to MLE in vitro and in vivo. The active ingredients increased by bioconversion, 5-CQA and 4-CQA, inhibited the protein levels of C/EBPα and the mRNA levels of stearoyl-CoA desaturase 1 (Scd1). These findings provide new insights into the therapeutic possibility of using bioconversion of MLE, by which upregulation of 5-CQA and 4-CQA potently inhibits adipogenesis.


Assuntos
Morus , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta , Obesidade/tratamento farmacológico , Obesidade/genética , Frutas , Proteína alfa Estimuladora de Ligação a CCAAT/genética
3.
Plants (Basel) ; 11(17)2022 Aug 24.
Artigo em Inglês | MEDLINE | ID: mdl-36079577

RESUMO

Migraines are a common neurological disorder characterized by desperate throbbing unilateral headaches and are related to phonophobia, photophobia, nausea, and vomiting. The Angelica dahurica Radix and Ligusticum chuanxiong Rhizoma herb pair (ALHP) has been used to treat migraines for centuries in traditional Chinese medicine (TCM). However, the physiological mechanisms of migraine treatment have not yet been elucidated. In this study, a total of 50 hub targets related to the effect of 28 bioactive compounds in ALHP on anti-migraine were obtained through network pharmacology analysis. GO and KEGG analyses of the hub targets demonstrated that ALHP treatment of migraines significantly involved the G-protein-coupled receptor signaling pathway, chemical synaptic transmission, inflammatory response, and other biological processes. According to the degree of gene targets in the network, ACE, SLC3A6, NR3CI, MAPK1, PTGS2, PIK3CA, RELA, GRIN1, GRM5, IL1B, and DRD2 were found to be the core gene targets. The docking results showed a high affinity for docked conformations between compounds and predicted targets. The results of this study suggest that ALHP could treat migraines by regulating immunological functions, diminishing inflammation, and improving immunity through different physiological pathways, which contributes to the scientific base for more in-depth research as well as for a more widespread clinical application of ALHP.

4.
Int J Mol Sci ; 23(18)2022 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-36142265

RESUMO

The root of Pueraria lobata (Willd.) is used commercially in different products, including dietary supplements, cosmetics, and teas, but its stem part is rarely used and studied. Therefore, this study evaluated the antioxidant and anti-melanogenesis activities of the bioactive fraction of P. lobata stem and investigated whether the activated carbon decolorization technique would have an impact on its activity and chemical composition. We observed that the dichloromethane fraction of P. lobata stem (DCM-PLS) has excellent antioxidant and anti-melanin synthesis activity at a concentration of 50 µg/mL. For the investigation of the anti-melanogenesis mechanism, we evaluated the mRNA expression of tyrosinase, which was depressed by the DCM-PLS. Daidzin was identified as the main active ingredient in DCM-PLS by using a high-performance liquid chromatography-diode array detector-hyphenated with tandem mass spectrometry. In addition, the activated carbon decolorization technology has no negative impact on the main components and bioactivity of DCM-PLS. DCM-PLS also did not induce any skin response in the human skin safety test. Collectively, DCM-PLS could be used as a natural type of skin-whitening agent in skin care products.


Assuntos
Clareadores , Pueraria , Preparações Clareadoras de Pele , Antioxidantes/farmacologia , Carvão Vegetal , Humanos , Cloreto de Metileno , Monofenol Mono-Oxigenase , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Pueraria/química , RNA Mensageiro , Preparações Clareadoras de Pele/farmacologia
5.
Molecules ; 27(14)2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35889504

RESUMO

In contrast to the stem and fruit of Akebia quinata, A. quinata leaves as a source rich in phenolic compounds with potentially beneficial pharmacological activities have been largely overlooked. To develop and use A. quinata leaves as a resource, we evaluated its potential as a cardiovascular-protective agent. Herein, we investigated the effects and potential mechanisms of A. quinata leaves extract on lipopolysaccharide (LPS)-induced inflammatory responses in human umbilical vein endothelial cells. We found that A. quinata leaves extract pretreatment of 10 µg/mL significantly attenuated LPS-induced protein expression of intercellular adhesion molecule-1, vascular cell adhesion molecule-1. Furthermore, this extract also suppressed LPS-induced phosphorylation of nuclear factor-κB p65. In order to elucidate the chemical profiles of the samples, the HPLC fingerprint was established, and prominent peaks were identified via HPLC-electrospray ionization-mass spectrometry. Multivariate statistical analyses, including hierarchical cluster analysis, principal component analysis, and partial least-squares discriminant analysis, were performed to evaluate the clustering of the samples. It was found that isochlorogenic acid C was a key marker for the classification of A. quinata leaves from the Gongju and Muju city in Korea. Collectively, this study not only suggested the potential of A. quinata leaves as a novel therapeutic candidate for inflammatory cardiovascular disease but also developed a quality control method for A. quinata leaves, which could help to expand the application of A. quinata.


Assuntos
Lipopolissacarídeos , Extratos Vegetais , Frutas , Células Endoteliais da Veia Umbilical Humana , Humanos , Molécula 1 de Adesão Intercelular , NF-kappa B , Fenóis/farmacologia , Extratos Vegetais/química , Folhas de Planta
6.
Prep Biochem Biotechnol ; 52(2): 144-153, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33950798

RESUMO

Ginseng flower bud (GFB), as an inexpensive part of Panax ginseng, attracted significant attention as a beneficial functional food with medicinal potentials due to its high content of ginsenosides. A few studies focused on the utilization of heat treatment and citric acid treatment to process ginseng flowers, converting its polar ginsenosides into rare ginsenosides to improve its biological activities. Thus, in this study, we compared the changes of ginsenosides in GFB after citric acid and heat treatment by HPLC method. The results revealed that less-polar ginsenoside, Rg6 and F4, increased to 1.01 and 0.27% by heat treatment, respectively. Further, ginsenoside F2 increased to 1.13% with 1 M citric acid treatment. Furthermore, based on the combination of these two processing methods for the first time, the conversion rate of less-polar ginsenosides surged to 80%. The content of ginsenoside Rg3(s) and Rg5 increased to 1.509 and 1.871%, respectively, by simultaneous heat and citric acid treatment. Therefore, a processing approach that simultaneously performs heat and citric acid treatments has been proposed, and this considerably inexpensive and convenient processing method could be applied to the processing of GFBs and produce less-polar ginsenosides.


Assuntos
Ácido Cítrico/farmacologia , Flores/metabolismo , Ginsenosídeos/metabolismo , Temperatura Alta , Panax/metabolismo , Cromatografia Líquida de Alta Pressão
7.
Plants (Basel) ; 10(12)2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34961245

RESUMO

Herbal and plant extracts exhibit various types of properties and activities that have been applied in the medicinal field to treat diseases and achieve better health [...].

8.
Antioxidants (Basel) ; 10(9)2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34572971

RESUMO

Isatis indigotica leaf is an oriental herbal medicine that has been known for various pharmacological effects. However, its anti-wrinkle activity has not been fully evaluated. Therefore, we evaluated the anti-wrinkle effect of I. indigotica leaf extract on human skin. The purified extract inhibited 85.4% of 2,2-diphenyl-1-1picrylhydrazyl and 72.2% of 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radicals at a concentration of 1 mg/mL. Nitrite production was reduced by 30% after treatment with 50 µg/mL of extract. Three fractions from the extract downregulated the mRNA expression of matrix metalloproteinase-1 and -3 and upregulated the expression of interleukin 4. Among the three fractions, fraction 2 exhibited the highest activity. The major component of the extract was identified as 3,4,5-trimethoxycinnamic acid by liquid chromatography coupled with mass spectrometry. Molecular docking was conducted to predict the binding mechanism of 3,4,5-trimethoxycinnamic with matrix metalloproteinase-1 and -3, and their binding energies were -5.20 and -4.89 kcal/mol, respectively. In a clinical trial, five roughness values of visiometer and visual score were significantly reduced in treated groups compared with the placebo group after 8 weeks. I. indigotica leaf extract inhibits wrinkle formation, and could be a potential anti-wrinkle agent. This is the first clinical trial demonstrating its anti-wrinkle activity.

9.
Int J Mol Sci ; 22(15)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34360871

RESUMO

The root of Pueraria lobata (Willd.) is a widely used herbal medicine worldwide, whereas the stem of the plant is discarded or used as feed for livestock. To reuse and exploit the stem of P. lobata as a resource, we investigated its potential as a skin-whitening agent. We found that the developed, enriched P. lobata stem (PLS) extract significantly inhibited melanin production in the 3-isobutyl-1-methylxanthine-induced B16/F10 cells at a concentration of 50 µg/mL. To further confirm the mechanism of the antimelanogenic effect of the enriched PLS extracts, we examined the mRNA expression of tyrosinase, which was suppressed by the extracts. To standardize and implement effective quality control of the enriched PLS extracts, its major chemical constituents were identified by high-performance liquid chromatography-photodiode array-electrospray ionization-mass spectrometry. In total, 12 constituents were identified. In silico analysis showed that the main constituents, puerarin and daidzin, had excellent binding affinities for human tyrosinase. Collectively, our results suggest that the PLS extracts could be used as anti-pigmentation agents.


Assuntos
Melaninas/biossíntese , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Caules de Planta/química , Pueraria/química , Preparações Clareadoras de Pele/farmacologia , Linhagem Celular Tumoral , Humanos , Isoflavonas/farmacologia , Melanoma Experimental , Monofenol Mono-Oxigenase/metabolismo
10.
Prep Biochem Biotechnol ; 51(4): 395-404, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32940554

RESUMO

Stachys sieboldii MiQ (SSM) is an important food and medicinal herb in Korea, used to improve memory of patients with senile dementia and cardiovascular diseases. However, little information on bioactive components from SSM or standardized extraction methods for these components is available. This study isolated and purified major components from SSM for the first time, and assessed their ability to inhibit soluble epoxide hydrolase (sEH). The results showed that acteoside is the most potent inhibitor of sEH, with an IC50 of 33.5 ± 0.5 µM. Additional active components, including harpagide, tryptophan, and 8-acetate-harpagide, along with acteoside, were tentatively identified using high-performance liquid chromatography photodiode array tandem mass spectrometry (HPLC-PDA-MS/MS) and quantified using an ultraviolet detector at 210 nm. Further, an ultrasonic-assisted extraction technique for extraction of four bioactive compounds in SSM was developed and optimized using response surface methodology (RSM). The optimal extraction conditions were: extraction time, 30.46 minutes; extraction temperature, 67.95 °C, and methanol concentration 53.85%. The prediction model of RSM was validated with laboratory experiments. The similarity between predicted and actual values was 97.84%. The extraction method is thus a rapid, environment-friendly, energy-saving method can be applied to extract bioactive components from SSM in large quantities.


Assuntos
Epóxido Hidrolases/antagonistas & inibidores , Epóxido Hidrolases/química , Extração Líquido-Líquido/métodos , Modelos Estatísticos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Stachys/química , Cromatografia Líquida de Alta Pressão/métodos , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Concentração Inibidora 50 , Glicosídeos Iridoides/isolamento & purificação , Glicosídeos Iridoides/farmacologia , Metanol/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Piranos/isolamento & purificação , Piranos/farmacologia , Solubilidade , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos , Temperatura , Triptofano/isolamento & purificação , Triptofano/farmacologia , Ondas Ultrassônicas
11.
Molecules ; 25(16)2020 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-32823787

RESUMO

Stauntonia hexaphylla (Lardizabalaceae) has been used as a traditional herbal medicine in Korea and China for its anti-inflammatory and analgesic properties. As part of a bioprospecting program aimed at the discovery of new bioactive compounds from Korean medicinal plants, a phytochemical study of S. hexaphylla leaves was carried out leading to isolation of two oleanane-type triterpene saponins, 3-O-[ß-d-glucopyranosyl (1→2)-α-l-arabinopyranosyl] oleanolic acid-28-O-[ß-d-glucopyranosyl (1→6)-ß-d-glucopyranosyl] ester (1) and 3-O-α-l-arabinopyranosyl oleanolic acid-28-O-[ß-d-glucopyranosyl (1→6)-ß-d-glucopyranosyl] ester (2). Their structures were established unambiguously by spectroscopic methods such as one- and two-dimensional nuclear magnetic resonance and infrared spectroscopies, high-resolution electrospray ionization mass spectrometry and chemical reactions. Their anti-inflammatory activities were examined for the first time with an animal model for the macrophage-mediated inflammatory response as well as a cell-based assay using an established macrophage cell line (RAW 264.7) in vitro. Together, it was concluded that the saponin constituents, when they were orally administered, exerted much more potent activities in vivo than their sapogenin core even though both the saponins and the sapogenin molecule inhibited the RAW 264.7 cell activation comparably well in vitro. These results imply that saponins from S. hexaphylla leaves have a definite advantage in the development of oral medications for the control of inflammatory responses.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Ranunculales/química , Animais , Glicosilação , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Saponinas/química , Relação Estrutura-Atividade
12.
Pharmaceutics ; 12(1)2020 01 07.
Artigo em Inglês | MEDLINE | ID: mdl-31936070

RESUMO

Diabetes mellitus (DM) has become a major health problem in most countries of the world. DM causes many complications, including hyperglycemia, diabetic ketoacidosis, and death. In Asia, mulberry has been used widely in the treatment of DM. Combination of drugs with herbal medicine may reduce the unwanted side effects caused by drugs. In this study, the influence of extended mulberry leaves extract (MLE) intake on metformin (Met) was evaluated in terms of pharmacokinetics and pharmacodynamics in DM-induced rats. Three week-treatment of MLE alone produced the anti-hyperglycemic effect (around 24%) if compared to the control. Interestingly, Met administration after MLE treatment for 3 weeks enhanced about 49% of the anti-hyperglycemic effect of Met. In addition, the extended intake of MLE potentiated the anti-hyperglycemic effect of Met on various concentrations. This potentiated anti-hyperglycemic effect of Met appears to be due to the pharmacokinetic change of Met. In this study, 3 week-treatment of MLE reduced the elimination of Met in DM-induced rats. In addition, MLE reduced the human organic cation transporter 2 (hOCT2) activity in a concentration-dependent manner. Thus, these findings suggest that MLE lowered the elimination of Met via inhibiting the hOCT2.

13.
BMC Complement Altern Med ; 19(1): 55, 2019 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-30841887

RESUMO

BACKGROUND: Mulberry is a Korean medicinal herb that shows effective prevention and treatment of obesity and diabetes. Bioconversion is the process of producing active ingredients from natural products using microorganisms or enzymes. METHODS: In this study, we prepared bioconverted mulberry leaf extract (BMLE) with Viscozyme L, which we tested in insulin-sensitive cells (i.e., skeletal muscle cells and adipocytes) and insulin-secreting pancreatic ß-cells, as well as obese diabetic mice induced by co-administration of streptozotocin (100 mg/kg, IP) and nicotinamide (240 mg/kg, IP) and feeding high-fat diet, as compared to unaltered mulberry leaf extract (MLE). RESULTS: BMLE increased the glucose uptake in C2C12 myotubes and 3 T3-L1 adipocytes and increased glucose-stimulated insulin secretion in HIT-T15 pancreatic ß-cells. The fasting blood glucose levels in diabetic mice treated with BMLE or MLE (300 and 600 mg/kg, PO, 7 weeks) were significantly lower than those of the vehicle-treated group. At the same concentration, BMLE-treated mice showed better glucose tolerance than MLE-treated mice. Moreover, the blood concentration of glycated hemoglobin (HbA1C) in mice treated with BMLE was lower than that in the MLE group at the same concentration. Plasma insulin levels in mice treated with BMLE or MLE tended to increase compared to the vehicle-treated group. Treatment with BMLE yielded significant improvements in insulin resistance and insulin sensitivity. CONCLUSION: These results indicate that in the management of diabetic condition, BMLE is superior to unaltered MLE due to at least, in part, high concentrations of maker compounds (trans-caffeic acid and syringaldehyde) in BMLE.


Assuntos
Glicemia/efeitos dos fármacos , Hipoglicemiantes/farmacologia , Morus/química , Extratos Vegetais/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/metabolismo , Dieta Hiperlipídica , Hipoglicemiantes/metabolismo , Resistência à Insulina/fisiologia , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/metabolismo , Folhas de Planta/química
14.
J Pharm Biomed Anal ; 168: 1-12, 2019 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-30776566

RESUMO

Syzygium formosum (SF) leaves have been used for thousands of years in traditional Vietnamese medicine for the treatment of allergy or skin rash. However, the role of the phytochemical profile of SF leaves on their activities is poorly understood. Additionally, there is currently no quality control method for this herbal material, which is required by the pharmaceutical industry. Therefore, this study aimed to investigate chemical profile of SF leaves using high-performance liquid chromatography-photodiode array-tandem mass spectrometry (HPLC-PDA-ESI-MS/MS) and establish a simple and efficient HPLC method for controlling major bioactive compounds. The characterization of 28 components, including eleven flavonoids, thirteen triterpene acids, and four phenolic acids, was achieved on the basis of their maximum ultraviolet wavelength values and MS fragmentation pathways. An HPLC-evaporate light scattering detector (HPLC-ELSD) method over 35 min of analysis time for quality control of SF leaves was proposed. Using response surface methodology based on a Box-Behnken design and Derringer's desirability function, the optimal conditions for extracting the main bioactive compounds in SF leaves were determined. The content of marker compounds within SF leaves decreased in the order asiatic acid > corosolic acid > betulinic acid > maslinic acid. The developed HPLC-ELSD method is appropriate for quality control testing of SF leaves.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/química , Syzygium/química , Espectrometria de Massas em Tandem/métodos , Folhas de Planta , Controle de Qualidade
15.
J Chromatogr B Analyt Technol Biomed Life Sci ; 1102-1103: 152-158, 2018 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-30391729

RESUMO

Nardostachyos Radix et Rhizoma (NR) is a valuable medicinal herb widely used in Korea, India, and China for the treatment of many diseases. Desoxo-narchinol A (DA) and nardosinonediol (ND) are the two main bioactive compounds belonging to the sesquiterpene group. Desoxo-narchinol A possesses anti-inflammatory activity while ND exhibits anti-depressant and cardioprotective activities. A pharmacokinetic study is important to decide whether the isolated compounds or the NR extract have better pharmacological activity. Hence, we developed an analytical method for studying the pharmacokinetics of DA and ND after oral administration of the pure compounds and herbal extract. An optimized liquid chromatography-mass spectrometry method (LC-MS/MS) with solid-phase extraction (SPE) for sample preparation was developed. A ZORBAX Extend C18 column (2.1 × 50 mm, 3.5 µm) was used under gradient elution with acetonitrile and 0.1% formic acid in water as the mobile phase. Validation experiments assessing accuracy, precision, and stability were satisfactory; the lower limit of quantification was 5 ng/mL. For the pharmacokinetic study, three groups of rats were administrated pure DA, pure ND, or NR extract orally. Concentrations of DA and ND in their plasma were determined by the developed method. Pharmacokinetic parameters, including the time to achieve maximum plasma concentration (Tmax) and the area under the plasma concentration curve from time zero to infinity (AUC0-∞), were compared for the herbal extract and pure compounds. The Tmax of the pure compound and the NR extract for DA was 7.50 and 8.33 min, respectively, compared to 5.00 and 5.83 min for the pure compound and the NR extract for ND, respectively. The AUC0-∞ of the pure compound and the NR extract for DA was 156.34 and 133.90 µg min/mL, respectively, and that for the NR extract for ND was 6.42 and 4.15 µg min/mL, respectively. LC-MS/MS was used to determine DA and ND in rat plasma. The pharmacokinetic profile of each pure compound and those in the extract were characterized and compared.


Assuntos
Naftóis/farmacocinética , Nardostachys , Extratos Vegetais/farmacocinética , Sesquiterpenos/farmacocinética , Administração Oral , Animais , Cromatografia Líquida/métodos , Estabilidade de Medicamentos , Modelos Lineares , Naftóis/sangue , Naftóis/química , Extratos Vegetais/administração & dosagem , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Sesquiterpenos/sangue , Sesquiterpenos/química , Espectrometria de Massas em Tandem/métodos
16.
Molecules ; 23(10)2018 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-30297610

RESUMO

The individual parts of Morus alba L. including root bark, branches, leaves, and fruits are used as a cosmetic ingredient in many Asian countries. This study identified several anti-melanogenesis constituents in a 70% ethanol extract of M. alba leaves. The ethyl acetate fraction of the initial ethanol extract decreased the activity of tyrosinase, a key enzyme in the synthetic pathway of melanin. Twelve compounds were isolated from this fraction and their structures were identified based on spectroscopic spectra. Then, the authors investigated the anti-melanogenesis effects of the isolated compounds in B16-F10 mouse melanoma cells. Compounds 3 and 8 significantly inhibited not only melanin production but also intracellular tyrosinase activity in alpha-melanocyte-stimulating-hormone (α-MSH)-induced B16-F10 cells in a dose-dependent manner. These same compounds also inhibited melanogenesis-related protein expression such as microphthalmia-associated transcription factor (MITF), tyrosinase, and tyrosinase-related protein-1 (TRP-1). Compound 3 modulated the cAMP-responsive element-binding protein (CREB) and p38 signaling pathways in α-MSH-activated B16-F10 melanoma cells, which resulted in the anti-melanogenesis effects. These results suggest that compound 3, isolated from M. alba leaves, could be used to inhibit melanin production via the regulation of melanogenesis-related protein expression.


Assuntos
Melaninas/biossíntese , Monofenol Mono-Oxigenase/antagonistas & inibidores , Morus/química , Extratos Vegetais/farmacocinética , Animais , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/genética , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Relação Dose-Resposta a Droga , Melaninas/metabolismo , Melanoma Experimental/metabolismo , Camundongos , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , alfa-MSH/genética
17.
Arch Pharm Res ; 41(5): 490-496, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29721815

RESUMO

Ten compounds (1-10) isolated from the seeds of Cassia tora were evaluated for tyrosinase inhibition. Compounds 3, 4, and 7 inhibited tyrosinase enzymatic activity in a dose-dependent manner, with IC50 values of 3.0 ± 0.8, 7.0 ± 0.4, and 9.2 ± 3.4 µM, respectively. Kinetic analyses revealed a mechanism consistent with competitive inhibition. In silico molecular docking showed that compounds 3 and 4 docked in the active site of tyrosinase, whereas 7 interacted with Ala246 and Val248 at outside of the active site, and His244 and Glu256 at inside. Additionally, compounds 3, 4, and 7 suppressed melanogenesis in α-MSH-treated B16F10 melanoma cells at a concentration of 10 µM.


Assuntos
Cinnamomum aromaticum/química , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Sementes/química , Animais , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade , Células Tumorais Cultivadas
18.
Int Immunopharmacol ; 54: 286-295, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29175507

RESUMO

While an anti-allergic effect of Chaga mushroom (Inonotus obliquus) has been indicated, its therapeutic effect on allergy and immunoregulatory mechanisms and chemical constituents directly responsible for that are hardly known. We examined the effect of 70% ethanol extract of Chaga mushroom (EE) and its dichloromethane (DF) and aqueous (AF) fractions using a mouse model of chicken ovalbumin (cOVA)-induced food allergy, and found that only EE and DF ameliorated allergy symptoms to a significant extent. The in vivo mast cell-stabilizing activity was also found only in EE and DF whereas the activities to suppress Th2 and Th17 immune responses and cOVA-specific IgE production in the small intestine were observed in all three treatment regimens, implying that inhibition of the mast cell function by lipophilic compounds was vital for the therapeutic effect. Results also indicated that inotodiol, a triterpenoid predominantly present in DF, played an active role as a mast cell stabilizer.


Assuntos
Antialérgicos/uso terapêutico , Hipersensibilidade Alimentar/tratamento farmacológico , Lanosterol/análogos & derivados , Mastócitos/imunologia , Células Th17/imunologia , Células Th2/imunologia , Animais , Basidiomycota/imunologia , Modelos Animais de Doenças , Etanol , Feminino , Humanos , Imunoglobulina E/sangue , Lanosterol/uso terapêutico , Cloreto de Metileno , Camundongos , Camundongos Endogâmicos BALB C , Ovalbumina/imunologia
19.
J Ethnopharmacol ; 211: 171-179, 2018 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-28943447

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: As documented in a Vietnamese traditional medical encyclopedia, Syzygium formosum (Wall.) Masam leaves have been routinely used among indigenous Vietnamese people for treatment of various allergy-like symptoms including dermatitis and rhinitis. AIM OF THE STUDY: Anti-allergic activity of S. formosum leaves was examined with a mouse model of chicken ovalbumin (cOVA)-induced food allergy, and mechanisms underlying the anti-allergic effect were explored. MATERIAL AND METHODS: BALB/c mice were administered i.p. cOVA (20µg) plus alum (2mg) twice on day 0 and 14 for sensitization (immunization). Two weeks after the second immunization, the mice were administered cOVA (50mg) p.o. 5 times every 3 days to induce food allergy symptoms (i.e., anaphylaxis, diarrhea, and drop in the body temperature). Ethanol extract of dried leaves of S. formosum (80mg/kg or 200mg/kg body weight) was administered p.o. daily during the induction (challenge) period. RESULTS: Treatment with the S. formosum leaves ethanol extract ameliorated the allergic symptoms to a significant extent and in a dose-dependent manner. The treatment also resulted in a significant improvement in the inflammatory lesion in the small intestine and reduction in the numbers of mast cells and eosinophils recruited to the lesion. The treatment also brought about a significant reduction in the levels of Th2 cytokines produced by the mesenteric lymph node cells cultured ex vivo with cOVA. The passive anaphylaxis experiment also showed that the extract treatment impaired the mast cell function. CONCLUSION: Our study provides a scientific basis for the traditional (indigenous) use of the S. formosum leaves extract for the treatment of various allergy symptoms in Vietnam. In addition, the results show that the extract has activities to suppress antigen-specific Th2 T cell immune responses and the mast cell function, which are directly related with its anti-allergic effect.


Assuntos
Antialérgicos/uso terapêutico , Hipersensibilidade Alimentar/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Syzygium , Alérgenos , Compostos de Alúmen , Animais , Antialérgicos/análise , Antialérgicos/farmacologia , Quimases/sangue , Citocinas/imunologia , Etanol/química , Feminino , Flavonoides/análise , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Hipersensibilidade Alimentar/sangue , Hipersensibilidade Alimentar/imunologia , Imunoglobulina E/sangue , Imunoglobulina G/sangue , Linfonodos/citologia , Camundongos Endogâmicos BALB C , Ovalbumina , Fitoterapia , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Folhas de Planta/química , Solventes/química , Triterpenos/análise , Triterpenos/farmacologia , Triterpenos/uso terapêutico
20.
Bioorg Med Chem Lett ; 27(23): 5149-5153, 2017 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-29100799

RESUMO

Panax ginseng has been the subject of extensive research on potential medicinal materials. The goal of this study was search the chemical constituents and biological activities of processed Panax ginseng, Korean red ginseng. Our efforts led to the isolation eleven compounds (1-11) including two new compounds 1 and 2 from Korean red ginseng using various chromatographic techniques. Chemical structures of isolated compounds were demonstrated by spectroscopic methods (1D-, 2D-NMR, and HR-ESI-MS). The anti-inflammatory effects of the compounds were investigated by inhibiting IL-6 and TNF-α secretion in LPS-activated RAW264.7 cells. Additionally, the effects of the compounds on the expression of COX-2 and iNOS were examined by Western blotting. Compound 1 significantly reduced the level of proinflammatory cytokines IL-6 and TNF-α secretion in LPS-activated RAW264.7 cells and the expression of COX-2 and iNOS inflammatory enzymes in the cells. These results suggested that compound 1, a new ginsenoside might useful in treatment of inflammation.


Assuntos
Anti-Inflamatórios/química , Panax/química , Saponinas/química , Triterpenos/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Quimiocinas/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Citocinas/metabolismo , Expressão Gênica/efeitos dos fármacos , Lipopolissacarídeos/toxicidade , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Espectroscopia de Ressonância Magnética , Camundongos , Conformação Molecular , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Panax/metabolismo , Células RAW 264.7 , República da Coreia , Saponinas/isolamento & purificação , Saponinas/farmacologia , Damaranos
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