RESUMEN
Sambucus adnata Wall.(SAW) has been used to treat osteoarthritis by the Yi nationality in China. The present study established an overall identification strategy based on ultra-high performance liquid chromatography-tandem Q-Exactive Orbitrap mass spectrometry (UPLC-Q-Exactive Orbitrap/MS) method to characterize the multiple chemical constituents of SAW before and after percutaneous penetration. Nineteen compounds, including triterpenoids, fatty acids, lignans, flavonoid, and amide, were tentatively identified in the dichloromethane extract of SAW, while fourteen ingredients penetrated the skin. Among them, eleven components were reported for the first time in SAW.
Asunto(s)
Medicamentos Herbarios Chinos , Cloruro de Metileno , Absorción Cutánea , Espectrometría de Masas/métodos , Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/químicaRESUMEN
Toosendanin (TSN) is a natural anti-cancer compound that is isolated from the traditional Chinese herbal Melia toosendan Sieb et Zucc. However, the research effect of TSN in the treatment of Triple negative breast cancer (TNBC) is still far from ideal. In this work, we investigated TSN and its derivatives in terms of their actions against MDA-MB-231 and HCC1806 TNBC cell lines. The results indicated that TSN and its derivative 11 showed excellent antitumor activity. Preliminary mechanistic studies showed that both compounds TSN and 11 induced S-phase arrest and G2/M phase cell number decrease in HCC1806 cells. Also, TSN and 11 significantly reduced the protein level of the well-known cancer suppressor gene p53, reduced the phosphorylation of AKT and ERK, and also induced the accumulation of phosphorylated p38 and p21.
Asunto(s)
Medicamentos Herbarios Chinos , Neoplasias de la Mama Triple Negativas , Humanos , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Apoptosis , Medicamentos Herbarios Chinos/farmacología , Línea Celular , Línea Celular Tumoral , Proliferación CelularRESUMEN
Six previously undescribed cycloartane triterpenes glycosides, cimimanols A-F (1-6), together with thirteen known analogues (7-19) were isolated from the rhizomes of Cimicifuga foetida. Among them, cimimanol A (1) was the first example of cycloartane triterpene glycoside featuring a unique cyclic carbonate, and cimimanol B (2) was a rare trinortriterpene glycoside. The chemical structures and absolute configurations of new compounds were determined on the basis of comprehensive spectroscopic analysis, chemical method, and X-ray crystal diffraction, as well as quantum chemistry calculations. Finally, all these compounds were evaluated for their lipid-lowering effect on 3T3-L1 adipocytes. Compounds 1-3, 6-10, 12-16, 18-19 could significantly reduce the fat accumulation in 3T3-L1 adipocytes, especially compounds 8, 9, 14, and 15 exhibited strong lipid-lowering effect at the concentration of 10 µM, with inhibition rates ranging from 8.35% to 12.07%.
Asunto(s)
Cimicifuga/química , Glicósidos/farmacología , Hipolipemiantes/farmacología , Triterpenos/farmacología , Células 3T3-L1 , Adipocitos/efectos de los fármacos , Animales , Diferenciación Celular/efectos de los fármacos , China , Glicósidos/aislamiento & purificación , Hipolipemiantes/aislamiento & purificación , Ratones , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Rizoma/química , Triterpenos/aislamiento & purificaciónRESUMEN
Five new aromatic compounds, designed as lucidumins A-D (1-4) and lucidimine E (9), along with seven known aromatic compounds (5-8, 10-12) were isolated from Ganoderma lucidum. Their structures were determined by spectroscopic method. Bioactive evaluation showed that compounds 2-4 and 6-10 displayed remarkable neuroprotective activities against corticosterone-induced PC12 cell damage, with the cell viability ranging from 69.99% to 126.00%; and compounds 1-4, 9 and 10 exhibited significant anti-inflammatory activities against LPS-induced nitric oxide (NO) production in RAW264.7 macrophages, with IC50 values ranging from 4.68 to 15.49⯵M. In particular, compound 10 showed remarkable neuroprotection with EC50 value of 2.49⯱â¯0.12⯵M, and potent anti-inflammation with IC50 value of 4.68⯱â¯0.09⯵M.
Asunto(s)
Antiinflamatorios/farmacología , Ganoderma/química , Fármacos Neuroprotectores/farmacología , Animales , Supervivencia Celular , China , Cuerpos Fructíferos de los Hongos/química , Ratones , Estructura Molecular , Óxido Nítrico/metabolismo , Células PC12 , Células RAW 264.7 , RatasRESUMEN
One new 15,16-seco-cycloartane triterpene (1: ), three new cycloartane triterpene glycosides (2: -4: ), and five known compounds (5: -9: ) were isolated from the aerial parts of Actaea heracleifolia. The chemical structures of these compounds were determined on the basis of NMR analysis, HRTOF-ESIMS data, and other spectroscopic methods. Selected compounds were evaluated for their cytotoxicity against human tumor cell lines (HL-60, SMMC-7721, A549, MCF-7, and SW480) in vitro. Compounds 3: and 4: showed weak activity against the HL-60, A-549, and MCF-7 cell lines with IC50 values ranging from 21.34 to 36.98 µM.