Effect of Taraxerol in Inducing Autophagy in Breast Cancer Cells via mTOR Signaling Pathway / 中国实验方剂学杂志

Objective: To investigate the effect of taraxerol on autophagy of breast cancer MCF-7 cells in vitro, and explore the related mechanisms. Method: The effect of various doses of taraxerol (12.5, 25, 50, 100, 200 μmol·L-1) on proliferation of MCF-7 cells was detected by methye thiazolye telrazlium (MTT) assay. The autophagy-inducing effect of taraxerol was observed by acridine orange staining, transmission electron microscope (TEM) and immunofluorescence. The expressions of autophagy-related proteins and the changes of mammalian target of rapamycin (mTOR) signaling pathway were determined by Western blot analysis. Result: The viability of MCF-7 cells was significantly inhibited by taraxerol. Acridine orange staining indicated that the acidic lysosomes increased significantly after treatment with taraxerol in MCF-7 cells. The autophagic structure in the treated group was observed by TEM. Immunofluorescence showed that the expression of microtubule-associated protein 1 light chain 3 (LC3) in the cells of the drug group was increased. Western blot demonstrated that the protein expressions of LC3-Ⅱ and Beclin-1 were increased in taraxerol-treated MCF-7 cells (PP-1 taraxerol group, combination group (taraxerol + 3-methyladenine, 3-MA) showed the down-regulation of LC3-Ⅱ in the MCF-7 cells (PPPConclusion: Taraxerol can induce autophagy in MCF-7 cells, which may be related to the inhibition of mTOR signaling pathway.

Study on Chemical Constituents of Ethanol Extract from Euonymus amygdalifolius / 中国药房

OBJECTIVE:To study the chemical constituents of Euonymus amygdalifolius.METHODS:Silica gel column chromatogram,gel column chromatogram,TLC and semi-preparative HPLC were adopted to isolate and purify ethanol extract from E.amygdalifolius.The structure of compounds was analyzed and identified according to physical and chemical properties,spectral data (mass spectrurn,hydrogen spectrum and carbon spectrum).RESULTS:Ten compounds were isolated from ethanol extract of aerial part of E.amygdalifolius,i.e.taraxerol (1),sophoradiol (2),taraxerone (3),sorghumol (4),heptaecanoic acid (5),octadecenoic acid (6),β-Sitosterol (7),daucosterol (8),epifriedelinol (9) and friedelin (10).CONCLUSIONS:Above compounds are all isolated from E.amygdalifolius for the first time;compounds 1,2,4,5,6 are isolated and obtained from Euonymus A.for the first time.The study lay a foundation for quality evaluation of E.amygdalifolius.

Triterpenes and sterols from Hoya diversifolia Blume.

Chemical investigation of the dichloromethane extracts of Hoya diversifolia Blume led to the isolation of β-amyrin cinnamate (1), squalene (2), β-sitosterol (3), a mixture of β-amyrin (4a), α-amyrin (4b) and lupeol (4c) in a 4:2:1 ratio and saturated hydrocarbons from the leaves; and 2, taraxerol (5), lupeol cinnamate (6), and a mixture of 3 and stigmasterol (7) in a 2:1 ratio from the stems. The structures of 1-7 were identified by comparison of their NMR data with those reported in the literature.

Chemical Constituents of Hoya buotii Kloppenb.

Chemical investigation of the dichloromethane extracts of Hoya buotii Kloppenb. afforded taraxerone (1), taraxerol (2), a mixture of β-sitosterol (3a) and stigmasterol (3b) in about 2:1 ratio, and a mixture of α-amyrin cinnamate (4a) and β-amyrin cinnamate (4b) in about 1:2 ratio from the stems; 1, 2, and 3a from the roots; a mixture of 4a and 4b in about 3:2 ratio from the flowers; and 3a, squalene (5) and saturated hydrocarbons from the leaves. The structures of 1-5 were identified by comparison of their NMR data with those reported in the literature.

Effects of Lupenone, Lupeol, and Taraxerol Derived from Adenophora triphylla on the Gene Expression and Production of Airway MUC5AC Mucin / 결핵및호흡기질환

BACKGROUND: Adenophora triphylla var. japonica is empirically used for controlling airway inflammatory diseases in folk medicine. We evaluated the gene expression and production of mucin from airway epithelial cells in response to lupenone, lupeol and taraxerol derived from Adenophora triphylla var. japonica. METHODS: Confluent NCI-H292 cells were pretreated with lupenone, lupeol or taraxerol for 30 minutes and then stimulated with tumor necrosis factor alpha (TNF-alpha) for 24 hours. The MUC5AC mucin gene expression and production were measured by reverse transcription-polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. Additionally, we examined whether lupenone, lupeol or taraxerol affects MUC5AC mucin production induced by epidermal growth factor (EGF) and phorbol 12-myristate 13-acetate (PMA), the other 2 stimulators of airway mucin production. RESULTS: Lupenone, lupeol, and taraxerol inhibited the gene expression and production of MUC5AC mucin induced by TNF-alpha from NCI-H292 cells, respectively. The 3 compounds inhibited the EGF or PMA-induced production of MUC5AC mucin in NCI-H292 cells. CONCLUSION: These results indicated that lupenone, lupeol and taraxerol derived from Adenophora triphylla var. japonica regulates the production and gene expression of mucin, by directly acting on airway epithelial cells. In addition, the results partly explain the mechanism of of Adenophora triphylla var. japonica as a traditional remedy for diverse inflammatory pulmonary diseases.

Chemical constituents from barks of Quercus mongolica / 中草药

Objective: To study the chemical constituents from the barks of Quercus mongolica. Methods: The chemical constituents were isolated and purified on the base of silica gel column chromatography and HPLC method. The structural elucidation was performed according to the physicochemical properties and spectral analysis. Results: Twenty compounds were isolated and identified as taraxerone (1), taraxerol (2), 20β-hydroxydammara-23-en-3-one (3), 20 (S), 24 (S)-dihydroxydammara-26-en-3-one (4), ursotic acid acetate (5), lupeol (6), β-sitosterone (7), isofouquierol (8), gallic acid (9), 5, 6, 7, 4'-tetrahydroxyflavanone (10), taxifolin (11), scopoletin (12), kaempferol (13), β-sitosterol (14), secoisolariciresinol (15), erythrodiol (16), (-)-epicatechin (17), daucosterol (18), (-)-epipinoresinol (19), and salicylic acid (20). Conclusion: Compounds 1, 2, 5, 6, and 11 are isolated from this plant for the first time, and compounds 4, 7, and 8 are isolated from the plants of Quercus L. for the first time.

Effect of bioactive compounds extracted from euphorbious plants on hematological and biochemical parameters of Channa punctatus / Efeito de compostos bioativos extraídos de plantas eufórbicas sobre os parâmetros hematológicos e bioquímicos da Channa punctatus

Channa punctatus was exposed to four different concentrations of Rutin, Taraxerol and Apigenin. Changes in some hematological parameters of Channa punctatus were assessed to determine the influence of these compounds on test fish. Fish were exposed to sublethal concentrations (80 percent of LC50 of 24h) of these compounds for one week. Control fish were also administered for one week. Thereafter, blood samples were obtained from the control and experimental fish. Blood was assayed for selected hematological parameters (hematocrit, hemoglobin, red blood cell count, white blood cell count total plasma protein and plasma glucose concentration). The derived hematological indices of mean corpuscular hemoglobin concentration (MCHC), mean corpuscular hemoglobin (MCH) and mean corpuscular volume (MCV) were calculated. Sublethal concentrations of these compounds caused a dose dependent decrease in hemoglobin values coupled with a decrease in hematocrit values and red blood cell counts are an obvious indication of anemia. The total white blood cell counts and the differential white blood cell counts were decreased except for the lymphocytes, where there was a slight increase. Plasma protein and glucose were also lower in exposed fish when compared with control. The hematological indices MCH, MCHC, MCV were also lowered. The result from this study reveals high mortality rate and deleterious consequences on the health of fish subjected to acute exposure of Rutin, Taraxerol and Apigenin and therefore, should not be used directly in aquaculture without having the proper knowledge.

Channa punctatus foi exposta a quatro diferentes concentrações de Rutina, Taraxerol e Apigenina. Alterações de alguns parâmetros hematológicos da Channa punctatus foram acessados para determinar a influência destes compostos no peixe teste. Peixes foram expostos a concentrações sub-letais (80 por cento 0f LC50 em 24h) destes compostos por uma semana. Os peixes controles foram também expostos durante uma semana. A seguir, amostras de sangue foram obtidas do peixe controle e do experimental. O sangue foi estudado por parâmetros hematológicos selecionados (hematócrito, hemoglobina, contagem de células vermelhas e brancas, proteína plasmática total e concentração de glucose plasmática). Os índices hematológicos derivados da média da concentração corpuscular da hemoglobina (MCHC), a média de hemoglobina corpuscular (MCH) e a média de volume corpuscular (MCV), foram calculados. Concentrações sub-letais destes compostos causaram decréscimo dose-dependente dos valores da hemoglobina unidos a decréscimo de valores de hematócrito e das contagens de células sanguíneas vermelhas o que caracteriza indicação óbvia de anemia. As contagens totais de células brancas e a contagem diferencial destas células estavam diminuídas exceto pelos linfócitos que mostraram leve aumento. A proteína plasmática e a glicose estavam também baixas nos peixes expostos quando comparados com o controle. Os índices hematológicos MCH, MCHC, MCV estavam também diminuídos. Os resultados deste estudo revelam alto percentual de mortalidade e conseqüências deletérias à saúde de peixes submetidos à exposição aguda de Rutina, Talaxerol e Apigenina e portanto eles não devem ser usados diretamente em aquacultura sem conhecimento apropriado.

A new prenylated flavanone from Mallotus apelta / 中草药

Objective To study the chemical constituents in the leaves of Mallotus apelta. Methods Constituents isolation and purification were carried out on silica gel and polyamide column. Their structures were identified by physicochemical properties and spectral analysis. Results Five compounds were isolated and elucidated as taraxerol (Ⅰ), ?-sitosterol (Ⅱ), 5, 7-dihydroxy-6-prenyl-4′-methoxy-flavanone (Ⅲ), apigenin (Ⅳ), and apigenin-7-O[WTBZ]-?-D-glucoside (Ⅴ). Conclusion Compound Ⅲ is a new compound named as mallotusin. Compounds Ⅰ and Ⅲ-Ⅴ are isolated from the leaves of M. apelta for the first time.