RESUMEN
Hyperuricemia, an abnormally high level of blood uric acid, is a major risk factor for gout. Although xanthine oxidase inhibitors were clinically used to lower blood uric acid level, the concerned side effects restricted their utilization. In this study, strictinin, an abundant polyphenol in Pu'er tea, was evaluated for its preventive effects on hyperuricemia. The results showed that the xanthine oxidase activity, uric acid production, and inflammation in AML12 mouse hepatocytes treated with xanthine were significantly reduced by the supplementation of strictinin. Detailed analyses revealed that strictinin inhibited xanthine-induced NLRP3 inflammasome activation. Consistently, the elevated blood uric acid level and the enhanced xanthine oxidase activity in mice treated with potassium oxonate were effectively diminished by strictinin supplementation. Moreover, for the first time, strictinin was found to promote healthy gut microbiota. Overall, strictinin possesses a great potential to be utilized as a functional ingredient for the prevention of hyperuricemia.
RESUMEN
Teaghrelins were identified as unique acylated flavonoid tetraglycosides and firstly reported in Chin-shin oolong tea. In the present study, two new teaghrelin-like compounds (1 and 2) were purified and characterised from Assam tea varieties collected in Thailand. Their chemical structures were constructed by the spectroscopic and spectrometric analysis. These two teaghrelin-like compounds were also not supposed to exhibit significant ghrelin receptor affinity according to the structural comparison with those teaghrelin-like compounds previously reported. In addition, compounds 1 and 2 did not display notable anti-inflammatory activity in human neutrophils assay.[Formula: see text].
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Camellia sinensis , Flavonoides , Humanos , Receptores de Ghrelina , Té , TailandiaRESUMEN
A highly specific and sensitive proton nuclear magnetic resonance (1H-NMR) method has been developed for the quantification of ephedrine alkaloid derivatives in Ephedra herbal commercial prescriptions. At the region of δ 4.0 to 5.0 ppm in the 1H NMR spectrum, the characteristic signals are separated well from each other, and six analogues in total, methylephedrine (ME), ephedrine (EP), norephedrine (NE), norpseudoephedrine (NP), pseudoephedrine (PE), and methylpseudoephedrine (MP) could be identified. The quantities of these compounds are calculated by the relative ratio of the integral values of the target peak for each compound to the known concentrations of the internal standard anthracene. The present method allows for a rapid and simple quantification of ephedrine alkaloid derivatives in Ephedra-related commercial prescriptions without any preliminary purification steps and standard compounds, and accordingly it can be a powerful tool to verify different Ephedra species. In comparison to conventional chromatographic methods, the advantages of this method include the fact that no standard compounds are required, the quantification can be directly performed on the crude extracts, a better selectivity for various ephedrine alkaloid derivatives, and the fact that a very significant time-gain may be achieved.
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Alcaloides/análisis , Ephedra/química , Efedrina/análogos & derivados , Efedrina/análisis , Ephedra/clasificación , Estudios de Factibilidad , Humanos , Límite de Detección , Espectroscopía de Resonancia Magnética/métodos , Espectroscopía de Resonancia Magnética/estadística & datos numéricos , Medicina Tradicional China , Fenilpropanolamina/análisis , Preparaciones de Plantas/química , Seudoefedrina/análisis , Especificidad de la EspecieRESUMEN
Teaghrelins, identified originally in Chin-shin oolong tea, are unique acylated flavonoid tetraglycosides and proposed to be potential oral analogues of ghrelin. In the present study, two new teaghrelin-like compounds were characterized from tea cultivars (TTES No. 12), and their chemical structures were established by the spectroscopic and spectrometric analysis. However, due to the different location of rhamnose, these two teaghrelin-like compounds may not show significant ghrelin receptor affinity.[Figure: see text].
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Camellia sinensis/química , Flavonoides/química , Acilación , Flavonoides/metabolismo , Ghrelina/química , Ghrelina/farmacología , Espectroscopía de Resonancia Magnética , Simulación del Acoplamiento Molecular , Estructura Molecular , Extractos Vegetales/química , Receptores de Ghrelina/metabolismo , Espectrometría de Masa por Ionización de Electrospray , Té/químicaRESUMEN
A new dimeric quaternary protoberberine alkaloid, bispalmatrubine (1), and thirteen known compounds (2-14) were purified from the tubers of Tinospora dentata. Their structures were determined by spectroscopic and spectrometric analytical methods. Among the isolates, eight compounds were examined for their in vitro anti-inflammatory potential and several tested alkaloids displayed moderate inhibitory effects of N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release.
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Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Tinospora/química , Alcaloides/química , Alcaloides/farmacología , Alcaloides de Berberina/química , Citocalasina B/farmacología , Humanos , Estructura Molecular , N-Formilmetionina Leucil-Fenilalanina/farmacología , Neutrófilos/efectos de los fármacos , Neutrófilos/metabolismo , Elastasa Pancreática/metabolismo , Tubérculos de la Planta/química , Plantas Medicinales/química , Superóxidos/metabolismoRESUMEN
Sesamin (SSM) and sesamolin (SesA) are the two major furofuran lignans of sesame oil and they have been previously noticed to exert various biological actions. However, their modulatory actions on different types of ionic currents in electrically excitable cells remain largely unresolved. The present experiments were undertaken to explore the possible perturbations of SSM and SesA on different types of ionic currents, e.g., voltage-gated Na+ currents (INa), erg-mediated K+ currents (IK(erg)), M-type K+ currents (IK(M)), delayed-rectifier K+ currents (IK(DR)) and hyperpolarization-activated cation currents (Ih) identified from pituitary tumor (GH3) cells. The exposure to SSM or SesA depressed the transient and late components of INa with different potencies. The IC50 value of SSM needed to lessen the peak or sustained INa was calculated to be 7.2 or 0.6 µM, while that of SesA was 9.8 or 2.5 µM, respectively. The dissociation constant of SSM-perturbed inhibition on INa, based on the first-order reaction scheme, was measured to be 0.93 µM, a value very similar to the IC50 for its depressant action on sustained INa. The addition of SSM was also effective at suppressing the amplitude of resurgent INa. The addition of SSM could concentration-dependently inhibit the IK(M) amplitude with an IC50 value of 4.8 µM. SSM at a concentration of 30 µM could suppress the amplitude of IK(erg), while at 10 µM, it mildly decreased the IK(DR) amplitude. However, the addition of neither SSM (10 µM) nor SesA (10 µM) altered the amplitude or kinetics of Ih in response to long-lasting hyperpolarization. Additionally, in this study, a modified Markovian model designed for SCN8A-encoded (or NaV1.6) channels was implemented to evaluate the plausible modifications of SSM on the gating kinetics of NaV channels. The model demonstrated herein was well suited to predict that the SSM-mediated decrease in peak INa, followed by increased current inactivation, which could largely account for its favorable decrease in the probability of the open-blocked over open state of NaV channels. Collectively, our study provides evidence that highlights the notion that SSM or SesA could block multiple ion currents, such as INa and IK(M), and suggests that these actions are potentially important and may participate in the functional activities of various electrically excitable cells in vivo.
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Adenoma/tratamiento farmacológico , Dioxoles/farmacología , Activación del Canal Iónico , Lignanos/farmacología , Neoplasias Hipofisarias/tratamiento farmacológico , Canales de Potasio con Entrada de Voltaje/metabolismo , Aceite de Sésamo/química , Canales de Sodio Activados por Voltaje/metabolismo , Adenoma/metabolismo , Adenoma/patología , Animales , Antioxidantes/farmacología , Neoplasias Hipofisarias/metabolismo , Neoplasias Hipofisarias/patología , Ratas , Células Tumorales CultivadasRESUMEN
Mulberry (Morus alba) leaf is traditionally consumed as a functional tea with remedial effects, such as preventing aging-related diseases. Two similar compounds, quercetin 3-O-malonylglucoside, and kaempferol 3-O-malonylglucoside, were detected in mulberry leaves and found to be structural recombinant composites of teaghrelin and emoghrelin, two classes of non-peptidyl compounds functionally identified as analogs of ghrelin. Molecular modeling showed that these two mulberry compounds were able to enter and interact with the ghrelin receptor and theoretical calculation revealed that they were similar to emoghrelin but slightly weaker than teaghrelin in terms of interaction with the receptor. The relatively abundant compound, quercetin 3-O-malonylglucoside was subjected to a bioactivity assay, and the result confirmed that it was able to increase the growth hormone secretion of rat anterior pituitary cells. It seems that quercetin 3-O-malonylglucoside is also a functional analog of ghrelin and presumably a key ingredient for the anti-aging activity of mulberry leaves. PRACTICAL APPLICATIONS: According to this study, quercetin 3-O-malonylglucoside and kaempferol 3-O-malonylglucoside are suggested to serve as active ingredients in tea products prepared from mulberry leaves. Contents of these two compounds might be used as key factors for breeding or screening mulberry varieties for commercial cultivation. Moreover, water extract of mulberry leaves containing these compounds can be used as an adequate supplement for functional food.
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Morus , Animales , Ghrelina , Glucósidos , Extractos Vegetales/farmacología , Hojas de la Planta , Quercetina/farmacología , RatasRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Kucha tea plant (Camellia assamica var. kucha Chang et Wang) is regarded as a mutant variety of wild Pu'er tea plant found in few mountain areas of Yunnan, China. Its fresh young leaves and shoots are picked by the indigenous aborigines in these local areas to prepare an herbal tea for the treatment of common cold empirically. MATERIALS AND METHODS: Two extra compounds of relative abundance were detected in Kucha tea in comparison with Pu'er tea, and their chemical structures were identified as chlorogenic acid and theacrine. These two compounds as well as two major compounds, strictinin and caffeine, in Kucha tea were evaluated for their cytotoxicity and inhibitory effects on human influenza virus A/Puerto Rico/8/34 by analyzing viral protein expression and progeny production. RESULTS: No or low cytotoxicity was detected for the four Kucha compounds when their concentrations were below 100 µM. Expression of viral NS1 protein was significantly inhibited by chlorogenic acid, theacrine or strictinin, but not caffeine at a concentration of 100 µM. The relative inhibitory potency was detected as chlorogenic acid < theacrine < strictinin, and both theacrine and strictinin displayed significant inhibition at a concentration of 50 µM. According to a plaque assay, viral progeny production was significantly reduced by theacrine or strictinin, but not by chlorogenic acid or caffeine under the same concentration of 100 µM. CONCLUSION: It is suggested that theacrine and strictinin are two major ingredients responsible for the anti-influenza activity of Yunnan Kucha tea traditionally used for the treatment of common cold.
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Alphainfluenzavirus/efectos de los fármacos , Antivirales/farmacología , Camellia sinensis , Fenoles/farmacología , Tés de Hierbas , Ácido Úrico/análogos & derivados , Animales , Antivirales/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Perros , Humanos , Alphainfluenzavirus/fisiología , Células de Riñón Canino Madin Darby , Fenoles/aislamiento & purificación , Hojas de la Planta , Ácido Úrico/aislamiento & purificación , Ácido Úrico/farmacologíaRESUMEN
Croton is an extensive flowering plant genus in the spurge family, Euphorbiaceae. Three croton compounds with the common ent-kaurane skeleton have been purified from Croton tonkinensis. METHODS: We examined any modifications of croton components (i.e., croton-01 [ent-18-acetoxy-7α-hydroxykaur-16-en-15-one], croton-02 [ent-7α,14ß-dihydroxykaur-16-en-15-one] and croton-03 [ent-1ß-acetoxy-7α,14ß-dihydroxykaur-16-en-15-one] on either hyperpolarization-activated cation current (Ih) or erg-mediated K+ current identified in pituitary tumor (GH3) cells and in rat insulin-secreting (INS-1) cells via patch-clamp methods. RESULTS: Addition of croton-01, croton-02, or croton-03 effectively and differentially depressed Ih amplitude. Croton-03 (3 µM) shifted the activation curve of Ih to a more negative potential by approximately 11 mV. The voltage-dependent hysteresis of Ih was also diminished by croton-03 administration. Croton-03-induced depression of Ih could not be attenuated by SQ-22536 (10 µM), an inhibitor of adenylate cyclase, but indeed reversed by oxaliplatin (10 µM). The Ih in INS-1 cells was also depressed effectively by croton-03. CONCLUSION: Our study highlights the evidence that these ent-kaurane diterpenoids might conceivably perturb these ionic currents through which they have high influence on the functional activities of endocrine or neuroendocrine cells.
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Croton/química , Diterpenos de Tipo Kaurano/farmacología , Canales Regulados por Nucleótidos Cíclicos Activados por Hiperpolarización/antagonistas & inhibidores , Neoplasias Hipofisarias/tratamiento farmacológico , Adenilil Ciclasas/genética , Animales , Línea Celular Tumoral , Modelos Animales de Enfermedad , Diterpenos de Tipo Kaurano/química , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , Canales Regulados por Nucleótidos Cíclicos Activados por Hiperpolarización/química , Canales Regulados por Nucleótidos Cíclicos Activados por Hiperpolarización/genética , Estructura Molecular , Neoplasias Hipofisarias/genética , Neoplasias Hipofisarias/patología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , RatasRESUMEN
INTRODUCTION: Recently, the fresh leaves of Aquilaria trees have been processed as food products such as agarwood tea due to its beneficial medicinal properties. However, there have not been any reported analytical methods to quantify the bioactive principles in the processed products. OBJECTIVE: A rapid and sensitive ultrahigh-performance liquid chromatography (UHPLC) coupled with electrospray ionisation (ESI) tandem mass spectrometry (MS/MS) method was developed and validated for the simultaneous determination of 10 bioactive components in Aquilaria leaf tea. METHODS: The UHPLC-MS/MS was used for quantification operated in multiple reaction monitoring (MRM) mode. The optimised chromatographic parameters were conducted on a Shim-pack XR-ODS II column and mobile phases consisted of acetonitrile and 0.1% formic acid in water. RESULTS: All the samples were analysed within 20 min. The established method showed excellent linearity (R2 > 0.9988), good repeatability with all the relative standard deviation values lower than 3.27%, and satisfactory recovery (79.72-119.22%). The matrix effect factors ranged from 87.65 to 97.27% in the examination. The developed method was applied to the determination of 10 bioactive principles (1-10) in six different Aquilaria leaf tea samples. Among the analytes, mangiferin (1) and iriflophenone 2-O-α-l-rhamnopyranoside (2) were the most abundant compounds in the extracts of Aquilaria leaf tea, and it indicated that these biotech products may possess laxative effects. CONCLUSION: This proposed method appeared to be a useful tool for the quality control of commercial products of Aquilaria leaf tea and thus provided an analytical reference for herbal drinks.
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Espectrometría de Masas en Tándem , Thymelaeaceae , Cromatografía Líquida de Alta Presión , Hojas de la Planta , Reproducibilidad de los Resultados , TéRESUMEN
Teaghrelins are unique acylated flavonoid tetraglycosides originally identified in Chin-shin oolong tea, and proposed to be potential oral analogs of ghrelin. Two acylated flavonoid tetraglycosides were isolated from Shy-jih-chuen oolong tea, and their chemical structures were determined to be quercetin and kaempferol 3-O-[α-L-arabinopyranosyl(1 â 3)][2"-O-(E)-p-coumaroyl] [ß-D-glucopyranosyl(1 â 3)-α-L-rhamnopyranosyl(1 â 6)]-ß-D-glucoside. These two compounds were extremely similar to the two teaghrelins (teaghrelin-1 and teaghrelin-2) in Chin-shin oolong tea by simply replacing a glucopyranosyl group with an arabinopyranosyl group. Molecular modeling showed that the two putative teaghrelins identified in Shy-jih-chuen docked to and interacted with the ghrelin receptor as well as teaghrelin-1 and teaghrelin-2. Mixture of these two putative teaghrelins was shown to enhance the release of growth hormone from primary anterior pituitary cells of rats. The results suggest that two teaghrelins, named teaghrelin-3 and teaghrelin-4, are present in Shy-jih-chuen oolong tea and possess biological activities analogous to teaghrelins in Chin-shin oolong tea. PRACTICAL APPLICATIONS: According to this study, teaghrelin-3 and teaghrelin-4 may be regarded as active ingredients for the quality control of Shy-jih-chuen oolong tea. The content of teaghrelins may serve as a key factor for the farmers to select new tea plants in their next propagation of Shy-jih-chuen cultivar. Crude water extract of Shy-jih-chuen oolong tea containing teaghrelins is considered to be an adequate food supplement or additive in functional food products.
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Camellia sinensis/química , Ghrelina/química , Extractos Vegetales/química , Flavonoides/química , Hojas de la Planta/química , Receptores de Ghrelina/química , Té/químicaRESUMEN
Two new sesquiterpenoids peltopterins A and B (compounds 1 and 2) and fifty-two known compounds were isolated from the methanol extract of P. pterocarpum and their chemical structures were established through spectroscopic and mass spectrometric analyses. The isolates 40, 43, 44, 47, 48, 51 and 52 exhibited potential inhibitory effects of superoxide anion generation or elastase release.
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Fabaceae/química , Sesquiterpenos/aislamiento & purificación , Espectrometría de Masas , Estructura Molecular , Elastasa Pancreática/metabolismo , Extractos Vegetales/análisis , Hojas de la Planta/química , Sesquiterpenos/química , Superóxidos/metabolismoRESUMEN
The Machilus genus (Lauraceae) had been extensively utilized in folk medicine due to its broad range of bioactivities. In the present study, a series of chromatographic separations of the methanol extract of stems of M. philippinensis led to the identification of thirty eight compounds totally. Among these, biscinnamophilin (1), machilupins A-C (2-4), machilutone A (5), and machilusoxide A (6) were new compounds reported for the first time. In addition, 5 was characterized with a unprecedented carbon skeleton. Other known compounds, including the major compounds cinnamophilin (7) and meso-dihydroguaiaretic acid (8), are identified by comparison of their physical and spectroscopic data with reported values. One of the reported compounds, cinnamophilin A (10), should be revised as dehydroguaiaretic acid (9) after careful comparison of all the 1H and 13C NMR data. Moreover, the neuroprotective activity of cinnamophilin (7) was examined in a primary cortical neuron culture and the results indicated that 7 was effective against glutamate induced excitotoxicity.
RESUMEN
Fifty-five compounds were isolated from the fresh stems of Cissus assamica, including 14 benzenoids, 11 triterpenes, nine steroids, five tocopherols, five chlorophylls, four flavonoids, two benzoquinones, two tannins, and three other compounds. Their structures were constructed by 1D and 2D nuclear magnetic resonance (NMR) and mass spectral data, and were also identified by a comparison of their spectral data with those reported in the literature. Among these isolates, 1,2-bis-(5--tocopheryl) ethane (51) was reported for the first time from natural sources. Some purified compounds were examined for their anti-inflammatory and anticancer bioactivities. The results indicated that betulinic acid (16) exhibited strong inhibition of superoxide anion generation with IC50 value of 0.2 ± 0.1 µM, while betulinic acid (16) and pheophytin-a (47) inhibited elastase release with IC50 value of 2.7 ± 0.3 and 5.3 ± 1.0 µM, respectively. In addition, betulinic acid (16) and epi-glut-5(6)-en-ol (18) exhibited potential cytotoxicity to non-small-cell lung carcinoma (NCI-H226) and colon cancer (HCT-116) cell lines with IC50 values in the range of 1.6 to 9.1 µM.
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Cissus/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Tallos de la Planta/química , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Supervivencia Celular/efectos de los fármacos , Células HCT116 , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Neutrófilos/efectos de los fármacos , Neutrófilos/inmunología , Neutrófilos/metabolismo , Fitoquímicos/química , Fitoquímicos/farmacología , Extractos Vegetales/aislamiento & purificaciónRESUMEN
Lycii Fructus, a solanaceous drug, is widely used as functional foods and in Traditional Chinese Medicine. Samples collected from different regions of China have been found to be not identical in chemical compositions which might affect the biological activities. Although many chromatographic and spectrometric methods have been reported to determine the concentration of betaine and other bioactive amino acids, disturbance resulted from other polar substances with low UV-absorbance and expensive mass facilities reduced the applicability of these techniques. In the present study, the strong cation exchange solid phase extraction procedure incorporated with 1H NMR was successfully developed as a rapid and reliable method that can simultaneously determine betaine, citric acid, threonine, alanine, and proline in various Lycii Fructus. In addition, ERETIC 2 method based on PULCON principle was also applied and compared with conventional method. This feasible and practical method offers a very powerful tool for the quality control of commercial Lycii Fructus from different sources.
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Medicamentos Herbarios Chinos/química , Lycium/química , Espectroscopía de Protones por Resonancia Magnética/métodos , Aminoácidos/química , China , Frutas/química , Control de CalidadRESUMEN
Low bioavailability and high binding affinity to plasma proteins led to the difficulty for the quantitative detection of lithospermate B (LSB) in plasma. This study aimed to develop a protocol for detecting LSB in plasma. A method was employed to quantitatively detect LSB of 5-500 ng/mL by LC/MS spectrometry in multi reaction monitoring mode via monitoring two major fragments with m/z values of 519 and 321 in the MS2 spectrum. To set up an adequate extraction solution to release LSB captured by plasma proteins, recovery yields of LSB extracted from rat plasma acidified by formic acid or HCl in the presence or absence of EDTA and caffeic acid were detected and compared using the above quantitative method. High recovery yield (â¼90%) was achieved when LSB (5-500 ng/mL) mixed in rat plasma was acidified by HCl (5 M) in the presence of EDTA (0.5 M) and caffeic acid (400 µg/mL). The lower limit of detection and the lower limit of quantification for LSB in the spiked plasma were calculated to be 1.8 and 5.4 ng/mL, respectively. Good accuracy (within ±10%) and precision (less than 10%) of intra- and inter-day quality controlled samples were observed. Oral bioavailability of LSB in rat model was detected via this optimized extraction method, and the maximum plasma concentration (Cmax) was found to be 1034.3 ± 510.5 µg/L at tmax around 10 min, and the area under the plasma concentration-time curve (AUC) was 1414.1 ± 851.2 µg·h/L.
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Cromatografía Liquida , Medicamentos Herbarios Chinos/farmacocinética , Espectrometría de Masas , Administración Oral , Animales , Disponibilidad Biológica , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/química , Masculino , Estructura Molecular , Unión Proteica , Ratas , Reproducibilidad de los ResultadosRESUMEN
BACKGROUND: The flavor and quality of tea are widely believed to be associated with the pot in which the tea is made. However, this claim is mostly by experiences and lacks solid support from scientific evidence. The current study investigated and compared the chemical compositions of oolong tea made with six different teapot materials, namely Zisha, Zhuni, stainless steel, ceramic, glass and plastic. RESULTS: For each tea sample, polyphenols and caffeine were examined by HPLC-UV, volatile compounds by GC/MS, amino acids by LC/MS and minerals by ICP-MS. The results suggested that tea infusions from Zisha and Zhuni pots contain higher levels of EGC, EGCG and total catechins and less caffeine than those from ceramic, glass and plastic pots and tend to have the lowest total mineral contents, potassium and volatile compounds in tea soup. The statistical differences were not all significant among Zisha, Zhuni and stainless steel pots. CONCLUSION: Based on the overall chemical composition of the tea infusion, Yixing clay pots (Zisha and Zhuni) produce tea infusions that are presumably less bitter and more fragrant and tend to contain more healthful compounds than tea infusions from other pots. The results could partially explain why Yixing clay pots are among the most popular teapots. The beneficial effects of long-term repeated use of these teapots warrants further study. © 2017 Society of Chemical Industry.
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Silicatos de Aluminio/química , Cerámica/química , Vidrio/química , Plásticos/química , Acero Inoxidable/química , Té/química , Arcilla , Hojas de la Planta/químicaRESUMEN
Investigation of the chemical constituents from the fruits of Citrus medica L. var. sarcodactylis Swingle has led to the characterization of a new sesquiterpene 1 along with thirty-two known compounds. The structure of 1 was established on the basis of 2D NMR spectroscopic and mass spectrometric analyses, and the known compounds were identified by comparison of their physical and spectroscopic data with those reported in the literature. In addition, most of the isolated compounds were evaluated for the activity assayed by the in vitro inhibition of superoxide anion generation and elastase release by human neutrophils. The results showed that only 6,7-dimethoxycoumarin (5) exhibited significant inhibition of superoxide anion generation, with IC50 value of 3.8 ± 1.4 µM.
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Citrus/enzimología , Cumarinas/farmacología , Frutas/enzimología , Elastasa Pancreática/metabolismo , Superóxidos/metabolismo , Adulto , Espectroscopía de Resonancia Magnética con Carbono-13 , Humanos , Neutrófilos/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Espectroscopía de Protones por Resonancia Magnética , Adulto JovenRESUMEN
BACKGROUND: It has been reported that royal jelly would reduce melanin synthesis and inhibit the expression of melanogensis related proteins and genes. In this study, we evaluate the anti-melanogenic and depigmenting activity of 10-hydroxy-2-decenoic acid (10-HDA) from royal jelly of Apis mellifera. METHODS: In this study, we assesses the 10-HDA whitening activity in comparison with the changes in the intracellular tyrosinase activity, melanin content and melanin production related protein levles in B16F1 melanoma cells after treating with 10-HDA. Furthermore, the skin whitening effect was evaluated by applying a cream product containing with 0.5%, 1% and 2% of 10-HDA onto the skin of mice (C57BL/6 J) for 3 week to observe the effect of DL*-values. RESULTS: The results showed that 10-HDA inhibited the MITF protein expression (IC50 0.86 mM) in B16F1 melanoma cells. Western blot analysis revealed that 10-HDA inhibited the activity of tyrosinase and the expression of tyrosinase-related protein 1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor (MITF) in B16F1 melanoma cells. In addition, the 10-HDA was applied on the skin of mice show significantly increased the average skin-whitening index (L value). CONCLUSIONS: The validation data indicated the potential of 10-HDA for use in suppressing skin pigmentation. The 10-HDA is proposed as a candidate to inhibit melanogenesis, thus it could be developed as cosmetics skin care products.
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Ácidos Grasos Monoinsaturados/farmacología , Ácidos Grasos/farmacología , Melaninas/biosíntesis , Pigmentación de la Piel/efectos de los fármacos , Piel/efectos de los fármacos , Animales , Línea Celular Tumoral , Cosméticos , Regulación hacia Abajo , Ácidos Grasos/química , Oxidorreductasas Intramoleculares/metabolismo , Ratones Endogámicos C57BL , Factor de Transcripción Asociado a Microftalmía/metabolismo , Monofenol Monooxigenasa/metabolismo , Oxidorreductasas/metabolismoRESUMEN
Four A-type flavan-3-ol-dihydroretrochalcone dimers, dragonins A-D (1-4), were characterized from the traditional Chinese medicine Sanguis Draconis. The structures of 1-4 were elucidated by spectroscopic and spectrometric analyses. Compounds 1 and 2 exhibited significant inhibition of fMLP/CB-induced superoxide anion and elastase. The signaling pathways accounting for the inhibitory effects of compound 2 were also elucidated. These purified A-type flavan-3-ol-dihydroretrochalcones are new potential leads for the development of anti-inflammatory drugs.