Brazilin downregulates the expression of protein regulator of cytokinesis 1 in bladder cancer T24 cell and BIU87 cell and inhibits the cell proliferation / 肿瘤研究与临床

Objective:To investigate the inhibitory effect of brazilin on bladder cancer cells and its mechanism.Methods:Chemically synthesized brazilin was synthesized by chemical synthesis. Methyl thiazolyl tetrazolium (MTT) method was used to detect the inhibitory effect of synthetic brazilin on bladder cancer cells T24 and BIU87. Proteomic technique was used to detect the effect of brazilin on the level of protein in both cells. Real-time quantitative polymerase chain reaction (qRT-PCR) and Western blot methods were used to verify the effects of brazilin on the expression of protein regulator of cytokinesis 1 (PRC1) of both cells at gene and protein level.Results:MTT method showed that brazilin significantly inhibited the proliferation of bladder cancer cells T24 and BIU87, and its half inhibitory concentration ( IC50) of T24 cell and BIU87 cell was 9.9 μg/ml and 5.1 μg/ml,respectively. Proteomic results showed that brazilin could regulate the protein expression of PRC1 in both cells, which was verified by qRT-PCR and Western blot. Conclusion:Brazilin suppresses bladder cancer cell growth possibly by downregulating PRC1.

Effect of brazilin on apoptosis and autophagy of tongue cancer Tca8113 cells and its molecular mechanism / 南方医科大学学报

OBJECTIVE@#To investigate the effects of brazilin on the proliferation, apoptosis and autophagy of human tongue squamous cell carcinoma Tca8113 cells in vitro and explore its molecular mechanism.@*METHODS@#The changes in the proliferation, morphology and apoptosis of Tca8113 cells in response to brazilin treatment were detected using MTT assay, Hoechst33342 staining, and Annexin V/PI double staining, respectively. The expressions of apoptosis-related protein Bax, Bcl-2, cleaved caspase-3 and autophagy-related proteins p-AMPK, p-mTOR, LC3B, and p62 in the treated cells were detected using Western blotting. The effect of treatment with both the AMPK pathway inhibitor and brazilin on the expressions of the pathway-related proteins p-AMPK, p-mTOR, and LC3B was assessed.@*RESULTS@#MTT assay showed that brazilin significantly inhibited the proliferation of Tca8113 cells with an IC50 of 31.17 μmol/L at 24 h. Hoechst33342 staining showed that brazilin induced apoptotic morphological changes in Tca8113 cells in a concentration-dependent manner. Treatment with different concentrations of brazilin resulted in increased apoptosis in the cells. Brazilin obviously inhibited the expression of Bcl-2, p62 and p-mTOR and enhanced the expressions of Bax, cleaved caspase-3, LC3B and p-AMPK. The AMPK pathway inhibitor significantly inhibited the increase in p-AMPK and LC3B expressions and the decrease in p-mTOR expression induced by brazilin.@*CONCLUSIONS@#Brazilin can inhibit the proliferation and promote apoptosis in Tca8113 cells and at the same time induces autophagy in the cells through the AMPK/mTOR pathway.

Optimization of Caesalpinia sappan L. heartwood extraction procedure to obtain the highest content of brazilin and greatest antibacterial activity / 中西医结合学报

OBJECTIVE@#The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L. heartwood in order to maximize the brazilin content and antibacterial activity of the extract.@*METHODS@#Two independent factors were studied: extraction temperature (45-95 °C) and extraction time (30-60 min). In addition, five dependent factors were monitored, including extraction yield, brazilin content, and clear zones against Staphylococcus aureus TISTR 1466, Staphylococcus epidermidis TISTR 518 and Propionibacterium acnes DMST 14961. The brazilin content was quantified by high-performance liquid chromatography and antibacterial activity was determined by disk diffusion assay.@*RESULTS@#The high temperature provided high total extract yield as well as brazilin content, while extraction time had little effect on yield or brazilin content. Extraction time had a positive effect, while extraction temperature had little effect on clear zone against S. aureus. The largest clear zone against S. epidermidis was achieved at low extraction temperature and long extraction time. Conversely, short extraction time and high extraction temperature provided the largest clear zone against P. acnes. The optimal conditions providing the highest brazilin content was an extraction temperature and extraction time of 95 °C and 30 min, respectively. The same optimal conditions also provided the simultaneous greatest antibacterial activity against the three bacteria. Modeled optimal conditions were validated be conducting extraction using these values. Yield and antibacterial activity of the resulting extract demonstrated that the model had a low percentage error.@*CONCLUSION@#The optimal condition will be used as a standard condition for extraction of C. sappan heartwood to maximize brazilin content and antibacterial activity.

Brazilin and Caesalpinia sappan L. extract protect epidermal keratinocytes from oxidative stress by inducing the expression of GPX7 / 中国天然药物

Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various pharmacological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indicated that C. sappan L. extract reduced UVA-induced HO production via GPX7 activation. Moreover, brazilin exhibited antioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 (GPX7), suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin.

Brazilin and Caesalpinia sappan L. extract protect epidermal keratinocytes from oxidative stress by inducing the expression of GPX7 / 中国天然药物

Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various pharmacological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indicated that C. sappan L. extract reduced UVA-induced HO production via GPX7 activation. Moreover, brazilin exhibited antioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 (GPX7), suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin.

Brazilin from Caesalpinia sappan heartwood and its pharmacological activities: A review

Caesalpinia sappan L. (CS) is a plant of Leguminosae family, commonly known as Brazil or Sappan wood. CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverages and has a wide variety of medicinal properties. Higher extraction yield of CS wood was achieved with 95% ethanol for 2 h. Chemical constituent's investigation of sappan wood resulted in the isolation of various structural types of phenolic components including one xanthone, one coumarin, three chalcones, two flavones three homoisoflavonoids and brazilin. Brazilin [(6a S-cis)-7, 11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10(6H)- tetrol], a major and active compound found in CS heartwood. Most of the folkloric uses of brazilin were validated by the scientific studies such as antioxidant, antibacterial, anti-inflammatory, anti-photoaging, hypoglycemic, vasorelaxant, hepatoprotective and anti-acne activity. CS heartwood extract is safe and did not produce any acute or subacute toxicity in both male and female rats. Brazilin is the safe natural compound having potential to develop as a medicinal compound with application in food, beverage, cosmetics and pharmaceutical industries to screen its clinical use in modern medicine. The information gained could provide the important and potential approach for pharmaceutical researcher to implicate the knowledge of brazilin in the formulation of new drug and to reveal therapeutic and gaps requiring future research opportunities. More studies are needed to evaluate the potential application of brazilin as preservative and coloring agent in food processing industries.

Brazilin from Caesalpinia sappan heartwood and its pharmacological activities: A review

Caesalpinia sappan L. (CS) is a plant of Leguminosae family, commonly known as Brazil or Sappan wood. CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverages and has a wide variety of medicinal properties. Higher extraction yield of CS wood was achieved with 95% ethanol for 2h. Chemical constituent's investigation of sappan wood resulted in the isolation of various structural types of phenolic components including one xanthone, one coumarin, three chalcones, two flavones three homoisoflavonoids and brazilin. Brazilin [(6a S-cis)-7, 11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10(6H)- tetrol], a major and active compound found in CS heartwood. Most of the folkloric uses of brazilin were validated by the scientific studies such as antioxidant, antibacterial, anti-inflammatory, anti-photoaging, hypoglycemic, vasorelaxant, hepatoprotective and anti-acne activity. CS heartwood extract is safe and did not produce any acute or subacute toxicity in both male and female rats. Brazilin is the safe natural compound having potential to develop as a medicinal compound with application in food, beverage, cosmetics and pharmaceutical industries to screen its clinical use in modern medicine. The information gained could provide the important and potential approach for pharmaceutical researcher to implicate the knowledge of brazilin in the formulation of new drug and to reveal therapeutic and gaps requiring future research opportunities. More studies are needed to evaluate the potential application of brazilin as preservative and coloring agent in food processing industries.

Component analysis, and purification and characterization of active ingredients in aqueous extract from Sappan Lignum / 中草药

Objective: To investigate, purify, and characterize the active ingredients in the aqueous extract from Sappan Lignum (the dry heartwood of Caesalpinia sappan). Methods: HPLC-MS/MS was used in the analysis of the chemical constituents in the aqueous extract from Sappan Lignum. Then the inhibitory effect of the aqueous extract from Sappan Lignum on human bladder tumor cell line T24 in vitro was studied. The main chemical constituents were purified by column chromatography and their structures were characterized by NMR. Results: In the aqueous extract from Sappan Lignum, 16 compounds were separated and detected well by HPLC-MS/MS and 14 were identified. The main compounds were quercetin, brazilin, isoliquiritigeni, protosappanin B, brazil A, 3'-deoxysappanol, 4-O-hydroxybrazilin, sappanchalcone, and (αS)-α, 2', 4, 4'-tetrahydroxy dihydrochalcone. The killing rate of cancer cells was positively correlated to the concentration of the main component which was brazilin. At last, according to the purification by column chromatography and the structural characterization by NMR, we obtained the pure brazilin in the aqueous extract from Sappan Lignum. Conclusion: The research offers a new method for the identification of the components in the aqueous extract from Sappan Lignum and provides a basis for the medicinal functions of Sappan Lignum for future study.

Effect of brazilin on proliferation and apoptosis of bladder carcinoma T24 cell line / 肿瘤研究与临床

Objective To observe the effects of brazilin on proliferation and apoptosis in T24 cells.Methods Trypan blue exclusion test was performed to detect the inhibition of brazilin on the growth of T24 cell lines in vitro cultured within different time.After exposure to different concentrations of brazilin,homogeneous bioluminescence assay was used to detect the inhibitory action of brazilin,Caspase-3 and Caspase-9 activity on T24 cells.Cellular apoptosis was measured by flow cytometry (FCM) and observed by laser scanning confocal microscope.Results Brazilin could significantly inhibit the proliferation of T24 cells after 8 hours,the inhibitory rates of the brazilin at concentration of 25,50,100,200 μg/ml against T24 cells respectively were 43.19 ％,60.73 ％,86.38 ％ and 93.89 ％ (P ＜ 0.05).After exposured to 50 μg/ml of brazilin,the inhibition ration to T24 cells increased with time prolonging (52.72 ％ in 4 h,60.73 ％ in 8 h,91.77 ％ in 24 h,96.41％ in 48 h) (P ＜ 0.05).The activity of Caspase-3 and Caspase-9 increased slightly when brazilin was at 25 μg/ml,but there was no statistical differences compared with that in the control group (P ＞ 0.05).When cells were treated with an increase of the concentration of brazilin from range of 7.5-60 μg/ml for 16 hours,the apoptosis ratio in turn showed a upward trend of 0.15 ％,1.35 ％,2.91％,34.76 ％.It could be seen by laser scanning confocal microscope that the apoptosis occurred in the cells.Conclusion Brazilin can effectively inhibit the proliferation of T24 cells and induce apoptosis in a dose and time dependent manner.

A produção do conhecimento na psicologia social brasileira: um estudo descritivo a partir da Revista Psicologia & Sociedade, 1986-1992 / Knowledge production in Brazilian social psychology: a descriptive study from the Journal of Psychology & Society, 1986-1992

Com o intuito de auxiliar na compreensão da história recente da Psicologia Social brasileira, apresentamos a primeira parte de pesquisa que objetivou descrever alguns aspectos que perpassam sua organização científica e social, o que se deu a partir de um dos seus principais veículos de comunicação, o periódico Psicologia & Sociedade: Revista da Associação Brasileira de Psicologia Social (ABRAPSO). Para isso, analisamos os trabalhos publicados entre os anos de 1986 e 1992. Assim, o total de 277 trabalhos, distribuídos em 10 revistas, constituiu nossa fonte de pesquisa. A origem institucional e geográfica dos autores, o padrão de autoria, o tipo e as temáticas dos trabalhos publicados, a metodologia e os locais de realização das investigações e intervenções, foram as informações examinadas. Por fim, a identificação tanto das transformações quanto de padrões de funcionamento da área, e alguns de seus possíveis determinantes, são apresentados.

With the objective of helping the comprehension of the recent Brazilian Social Psychology history, we present the first part of the survey, aimed at describing some aspects that go through its scientific and social organization, which happened from one of its main means of communication, the periodical Psicologia & Sociedade (Psychology & Society): a magazine from the Brazilian Association of Social Psychology (ABRAPSO). For that, we analyzed the works published between the years 1986 and 1992. Thus, the total of 277 works, distributed in 10 magazines, constituted our survey source. The institutional and geographic origin of the authors, the authorship pattern, the type and themes of the published works, the methodology and the places where investigations and interventions took place were examined. Finally, the identification of the transformations as well as the patterns of the area functioning, and some of its determiners, are presented.

Study on anticancer active principle in lignum Caesalpinia sappan / 肿瘤研究与临床

Objective To search for the anticancer active substance from Caesalpinia sappan wood extractions. Methods Crude extracts were extracted from Caesalpinia sappan wood with different solvents.Liquid chromatography was applied to analyze the content of each essential component in the extraction fractions. Trypan blue exclusion test was performed to detect the growth suppression rate of human bladder carcinoma cell line T24 treated by the extraction fractions at different time course (20,40,60,80,100 min).The main component positively correlated with the cell suppression rate was separated out using repeated chromatography, thus the anticancer active monomer was obtained, with purity over 98 ％. The chemical constitution was determined using NMR (nuclear magnetic resonance), mass spectrum and infrared spectrum methods. T24 cell line, human ovarian cancer cell line SKOV3, mice sarcoma S180 and hepatic carcinoma H22 cell were chosen as target subjects, with mitomycin, hydroxycamptothecin as positive control drug, the inhibitory activity of the monomer was tested by trypan blue chromophobia method. Results Among the extraction fractions, R12 has a positive correlation with the cell suppression rate (r100 min=0.941, P＜0.001).Brazilin is the key component in R12.The inhibition rate of brazilin could reach 90.89 ％,98.65 ％,99.82 ％ and 100.00 ％ on T24,SKOV3,S180 and H22 respectively in 40 min at the concentration of 1.2 mg/ml,and its effect is much superior to that of the control drug mitomycin and hydroxycamptothecin. Conclusion Brazilin is one of the essential anticancer principles in Caesalpinia sappan wood.