RESUMEN
BACKGROUND: Autologous fat grafting is a common method for soft tissue defect repair. However, the high absorption rate of transplanted fat is currently a bottleneck in the process. Excessive inflammation is one of the main reasons for poor fat transplantation. Salvianolic acid B (Sal-B) is a herbal medicine that shows promise for improving the effectiveness of fat transplantation. OBJECTIVE: The aim of this study was to improve fat graft survival by injecting Sal-B into fat grafts locally. METHODS: In vivo, 0.2 mL of Coleman fat was transplanted into nude mice along with Sal-B. The grafts were evaluated by histologic analysis at 2, 4, and 12 weeks posttransplantation and by microcomputed tomography at 4 weeks posttransplantation. In vitro ribonucleic acid sequencing, cell proliferation assays, anti-inflammatory activity assays, molecular docking studies, and kinase activity assays were performed in RAW264.7 cells to detect the potential mechanism. RESULTS: Sal-B significantly improved fat graft survival and attenuated adipose tissue fibrosis and inflammation. Sal-B also inhibited the polarization of M1 macrophages in fat grafts. In vitro, Sal-B inhibited the proliferation and activation of inflammatory pathways in RAW264.7 cells. In addition, Sal-B had an inhibitory effect on NF-κB (nuclear factor κ light polypeptide gene enhancer in B cells) signaling. This bioactivity of Sal-B may result from its selective binding to the kinase domain of the inhibitor of NF-κB kinase subunit ß. CONCLUSIONS: Sal-B could serve as a promising agent for improving the effect of fat transplantation by inhibiting the polarization of M1 macrophages through NF-κB signaling.
Asunto(s)
Inflamación , FN-kappa B , Ratones , Animales , FN-kappa B/genética , FN-kappa B/metabolismo , Ratones Desnudos , Simulación del Acoplamiento Molecular , Microtomografía por Rayos X , Macrófagos/metabolismoRESUMEN
The neuroprotective properties of ginsenosides have been found to reverse the neurological damage caused by oxidation in many neurodegenerative diseases. However, the distribution of ginsenosides in different tissues of the main root, which was regarded as the primary medicinal portion in clinical practice was different, the specific parts and specific components against neural oxidative damage were not clear. The present study aims to screen and determine the potential compounds in different parts of the main root in ginseng. Comparison of the protective effects in the main root, phloem and xylem of ginseng on hydrogen peroxide-induced cell death of SH-SY5Y neurons was investigated. UPLC-Q-Exactive-MS/MS was used to quickly and comprehensively characterize the chemical compositions of the active parts. Network pharmacology combined with a molecular docking approach was employed to virtually screen for disease-related targets and potential active compounds. By comparing the changes before and after Content-Effect weighting, the compounds with stronger anti-nerve oxidative damage activity were screened out more accurately. Finally, the activity of the selected monomer components was verified. The results suggested that the phloem of ginseng was the most effective part. There were 19 effective compounds and 14 core targets, and enriched signaling pathway and biological functions were predicted. After Content-Effect weighting, compounds Ginsenosides F1, Ginsenosides Rf, Ginsenosides Rg1 and Ginsenosides Rd were screened out as potential active compounds against neural oxidative damage. The activity verification study indicated that all four predicted ginsenosides were effective in protecting SH-SY5Y cells from oxidative injury. The four compounds can be further investigated as potential lead compounds for neurodegenerative diseases. This also provides a combined virtual and practical method for the simple and rapid screening of active ingredients in natural products.
Asunto(s)
Ginsenósidos , Neuroblastoma , Panax , Humanos , Espectrometría de Masas en Tándem/métodos , Ginsenósidos/química , Panax/química , Simulación del Acoplamiento Molecular , Floema/metabolismo , Estrés Oxidativo , Cromatografía Líquida de Alta Presión/métodosRESUMEN
A rapid and simple method has been developed for the screening and identification of natural antioxidants from the leaves of Acer ginnala Maxim (AG). The process is that upon reaction with 1,1-diphenyl-2-picrylhydrazyl (DPPH), the white yellow spots of compounds with potential antioxidant effects will be significantly observed on the thin-layer chromatography (TLC), and possible structures will be presumed by the ESI/MS technique. Using the improved approach, 6 compounds in the AG extract were found to possess a potential antioxidant activity. They were speculated as quercetin-3-O-α-L-(3"-galloyl)-rhamnoside (1), quercetin-3-O-α-L-(2"-galloyl)-rhamnoside (2), quercetin-3-O-α-L-(2"-galloyl)-arabinopyranoside (3), acertannin (4), gallic acid (5), and methyl gallate (6). In addition, we were still found that compounds 2, 3, and 5 had favorable antioxidant activity from the scannogram of the DPPH reaction plate. As a result, the isolated 6 compounds structures were in accordance with the presumed structures. Furthermore, the free radical scavenging capacities of the available identified compounds were also investigated. Compounds 2, 3, and 5 showed significant DPPH.Scavenging capacities, with IC50 values of 2.83 µg/mL, 2.34 µg/mL, and 1.86µg/mL, respectively. The results indicated that this newly improved method could be widely applied for rapid screening and identification of natural antioxidants from Chinese herbal medicines.
RESUMEN
Lepidium meyenii is now widely consumed as a functional food and medicinal product, which is known as an enhancer of reproductive health. However, the specific chemical composition and mechanism of action for improving sexual function are unclear. The present study aims at screening and determining the potential compounds, which promote mouse leydig cells (TM3) proliferation. The partial least squares analysis (PLS) was employed to reveal the correlation between common peaks of high performance liquid chromatography (HPLC) fingerprint of L. meyenii and the proliferation activity of TM3. The results suggested that three compounds had good activities on the proliferation of TM3 and promoting testosterone secretion, there were N-benzyl-hexadecanamide, N-benzyl-(9z,12z)-octadecadienamide and N-benzyl-(9z,12z,15z)-octadecatrienamide which might be the potential bioactive markers related to the enhancing sexual ability functions of L. meyenii. The first step in testosterone synthesis is the transport of cholesterol into the mitochondria, and the homeostasis of mitochondrial function is related to cyclophilin D (CypD). In order to expound how bioactive ingredients lead to promoting testosterone secretion, a molecular docking simulation was used for further illustration in the active sites and binding degree of the ligands on CypD. The results indicated there was a positive correlation between the binding energy absolute value and testosterone secretion activity. In addition, in this study it also provided the reference for a simple, quick method to screen the promoting leydig cell proliferation active components in traditional Chinese medicine (TCM).
Asunto(s)
Lepidium/química , Células Intersticiales del Testículo/citología , Fitoquímicos/análisis , Fitoquímicos/farmacología , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en Tándem , Animales , Línea Celular , Proliferación Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Enlace de Hidrógeno , Interacciones Hidrofóbicas e Hidrofílicas , Análisis de los Mínimos Cuadrados , Células Intersticiales del Testículo/efectos de los fármacos , Ligandos , Masculino , Ratones , Simulación del Acoplamiento Molecular , Análisis Multivariante , Fitoquímicos/química , Testosterona/metabolismoRESUMEN
OBJECTIVE: To study the alkaloids of Cervi Cornu Pantotrichum and its effect on murine splenocytes proliferation. METHODS: The constituents isolation and purification from Cervi Cornu Pantotrichum was carried out by reported column chromatography including Sephadex LH-20 and MCI (CHP20P) and their structures were elucidated on the basis of spectral compounds. The method of MTT was used to examine the effects of eight alkaloids and total alkaloids content (TAC) of Cervi Cornu Pantotrichum on murine splenocytes proliferation. RESULTS: Eleven compounds were isolated from Cervi Cornu Pantotrichum, and their structures were identified as follows: uracil (1), hypoxanthine (2), uridine (3) inosine (4), guanosine (5), 2'-deoxyguanosine (6), guanine (7), thymidine (8), thymine (9), cytidine (10) and adenosine (11). By the experiment of murine splenocytes proliferation activity in vitro, the results showed that the total alkaloids, uracil and adenosine had significantly promoted the proliferation of mouse spleen cells. CONCLUSION: Compounds 4 - 11 are isolated from Cervi Cornu Pantotrichum for the first time. The total alkaloids is one of the material basis of immunomodulatory effects of Cervi Cornu Pantotrichum, and uracil and adenosine are the most active.
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Alcaloides/química , Alcaloides/farmacología , Ciervos , Cuernos/química , Materia Medica/farmacología , Medicina Tradicional China , Adenosina/química , Adenosina/aislamiento & purificación , Adenosina/farmacología , Alcaloides/aislamiento & purificación , Animales , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Femenino , Masculino , Materia Medica/química , Materia Medica/aislamiento & purificación , Ratones , Bazo/citología , Uracilo/química , Uracilo/aislamiento & purificación , Uracilo/farmacologíaRESUMEN
OBJECTIVE: To study the antioxidant constituents from the root of Rubus crataegifolius. METHOD: The constituents isolation and purification from the root of R. crataegifolius was carried by reported column chromatography including silica gel, toyopearl, and their structures were elucidated on the basis of spectral compounds. DPPH method was used to evaluate the free radical scavenging activity of the isolated compounds. RESULT: Nine compounds were isolated from the root of R. crataegifolius, and their structures were identified as follow: euscaphic acid (1), kaempferol-3-O-beta-D-galactopyranoside (2), tormentic acid (3), 2alpha, 19alpha, 24-trihydroxyurs-12-ene-3-oxo-28-acid (4) , 2alpha-hydroxy-oleanolic acid (5), ursolic acid (6), daucosterol (7), beta-sitosterol (8) and polydatin (9). By experiment of antioxidant activity, the result showed compounds 2 and 9 revealed DPPH free radical scavenging rates were 95.60% and 75.23% at the concentration of 50 mg x L(-1). CONCLUSION: Compounds 1-8 were isolated from this plant for the first time, and compounds 2 and 9 showed the significant antioxidant activity.
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Antioxidantes/química , Medicamentos Herbarios Chinos/química , Rosaceae/química , Antioxidantes/aislamiento & purificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Raíces de Plantas/químicaRESUMEN
OBJECTIVE: To study the chemical constituents of the aerial part of Ligusticum jeholense. METHODS: The constituents were isolated by sillica gel column chromatography, Sephadex LH-20 column chromatography and their structures were elucidated by spectral analysis. RESULTS: Seven compounds were separated from the EtOH extracts. Their structures were identified as psoralen (1), beta-sitosterol (2), daucosterol (3), kaempferol-3-O-(2",4"-di-E-p-coumaroyl)-alpha-L-rhamnoside (4), kaempferol-3-O-beta-D-galactoside (5), quercetin-3-O-beta-D-galactoside (6), sucrose (7). CONCLUSION: Compounds 1, 4, 5 and 6 are isolated from the genus for the first time. Compounds 2, 3 and 7 are isolated from the aerial part of the plant for the first time.
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Ficusina/aislamiento & purificación , Ligusticum/química , Plantas Medicinales/química , Quercetina/análogos & derivados , Sitoesteroles/aislamiento & purificación , Etanol , Ficusina/química , Quempferoles/química , Quempferoles/aislamiento & purificación , Estructura Molecular , Monosacáridos/química , Monosacáridos/aislamiento & purificación , Componentes Aéreos de las Plantas/química , Quercetina/química , Quercetina/aislamiento & purificación , Sitoesteroles/química , Sacarosa/química , Sacarosa/aislamiento & purificaciónRESUMEN
OBJECTIVE: To study the chemical constituents of the root and rhizoma of Ligusticum jeholense. METHODS: The constituents were isolated by silica gel column chromatography, Sephadex LH-20 column chromatography and their structures were elucidated through spectral analysis. RESULTS: Seven compounds were separated from the EtOH extracts. Their structures were identified as levistolide A (1), xiongterpene (2), linoleic acid (3), sucrose (4), daucosterol (5), ferulic acid (6) and beta-sitosterol (7). CONCLUSION: Compounds 1-5 are isolated from the genus for the first time.
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Benzofuranos/aislamiento & purificación , Ligusticum/química , Ácido Linoleico/aislamiento & purificación , Plantas Medicinales/química , Terpenos/aislamiento & purificación , Benzofuranos/química , Ácidos Cumáricos/química , Ácidos Cumáricos/aislamiento & purificación , Ácido Linoleico/química , Estructura Molecular , Raíces de Plantas/química , Rizoma/química , Sitoesteroles/química , Sitoesteroles/aislamiento & purificación , Sacarosa/química , Sacarosa/aislamiento & purificación , Terpenos/químicaRESUMEN
OBJECTIVE: To investigate the chemical constituents in stem and leaves of Jasminum lanceolarium. METHOD: The constituents of the EtOAc-soluble portion of the 95% ethanol extractive were isolated and purified by means of column chromatographic methods. Compounds were identified by their physical characteristics and spectral features. RESULT: Eight compounds were isolated and identified as 5, 7, 3', 5'-tetrahydroxyflavanone (1), (2S)-5, 7, 3', 4'-tetrahydroxyflavan-5-O-beta-D-glucopyranosie (2), mannitol (3), nonacosane (4), trans-p-coumaric acid (5), cis-p-coumaric acid (6), ferulic acid (7) and, trans-cinnamic acid (8). CONCLUSION: Compounds 14 were isolated from this genus for the first time. And compounds 5 and 6 were isolated from this plant for the first time.
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Jasminum/química , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Hojas de la Planta/química , Tallos de la Planta/químicaRESUMEN
OBJECTIVE: To make qualitative analysis on alkaliod in Lobelia sessilifolia. METHOD: The ESI-MS(n) method was used for qualitative analysis. RESULT: The structures of two alkaliods in plant extract of L. sessilifolia were successfully analyzed and identified as norlobelanine and 8, 10-diethyllobelidione by electrospray ionization multistage mass spectrometry in positive mode. Then the fragmentation mechanisms were explored. CONCLUSION: SPE and ESI-MS(n) could simply and rapidly provide qualitative examination of alkaliods in L. sessilifolia.