Essential oil from Saussurea costus inhibits proliferation and migration of Eca109 cells via mitochondrial apoptosis and STAT3 signaling

Objective: To investigate the effect and its underlying molecular mechanisms of essential oil from Saussurea costus in esophageal cancer cell line Eca109. Methods: The chemical composition of essential oil from Saussurea costus was investigated by gas chromatography-mass spectrometry (GC-MS). The anti-proliferative, anti-migrative, and apoptotic effects of essential oil from Saussurea costus against Eca109 cells were analyzed. Moreover, the expression of proteins associated with cell cycle, metastasis, and apoptosis was determined. Results: GC-MS analysis showed that essential oil from Saussurea costus was predominantly comprised of sesquiterpenes. Saussurea costus essential oil inhibited the viability of Eca109 cells in a dose-and time-dependent manner with IC 50 values of (24.29±1.49), (19.16±2.27) and (6.97±0.86) μg/mL at 12, 24, and 48 h, respectively. The expression levels of target proteins in the cell cycle (phase G 1 /S), including cyclin D1, p21, and p53, were affected by Saussurea costus essential oil. The essential oil also downregulated the expression of metastasis-related proteins MMP-9 and MMP-2. Moreover, it induced apoptosis of Eca109 cells through the mitochondrial pathway, as well as inhibition of STAT3 phosphorylation. Conclusions: The essential oil from Saussurea costus exhibited anti-proliferative, anti-migrative, and apoptotic effects on Eca109 cells, and could be further explored as a potential anti-esophageal cancer agent.

Explore the antiproliferative phytocompounds from ethanolic extracts of Citrus paradisi against liver cancer cell line by chemical analysis using TLC and FT-IR spectroscopy

Abstract The aim of the present study was to evaluate the in vitro antiproliferative activity of ethanolic extract of leaves and fruits Citrus paradisi plant on HepG-2 liver cell lines by MTT (3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-terazolium bromide) assay and to isolate and characterize the antiproliferative compounds by TLC (Thin layer chromatography) and FT-IR (Fourier transforms Infrared) spectroscopy. Qualitative phytochemical screening tests were performed to detect phytochemicals compounds from the crude extracts. Antioxidant activity of the plant extracts were characterized by using DPPH (2,2-Diphenyl-1-picrylhydrazyl) free radical scavenging method. The results showed that antioxidant activity using DPPH were found to be increased in a concentration dependent manner and decreased cell viability and cell growth inhibition in a dose dependent manner. The findings from this study indicated that fruit extract exhibited good antiproliferation and antioxidant potential. The seven functional groups of phytocompounds such as carboxylic acid, amine salt, aromatic compounds, cyclic alkene, aldehyde, fluoro compounds and alkene were detected by FT-IR which indicated that fruit extracts of Citrus paradisi possessed vast potential as a medicinal drug especially in liver cancer treatment.

Resumo O objetivo do presente estudo foi avaliar a atividade antiproliferativa in vitro do extrato etanólico de folhas e frutos da planta Citrus paradisi em linhagens de células hepáticas HepG-2 por MTT (3- (4, 5-dimetil-2-tiazolil) -2, Ensaio de brometo de 5-difenil-2H-terazólio) e isolar e caracterizar os compostos antiproliferativos por espectroscopia de TLC (cromatografia de camada fina) e FT-IR (infravermelho com transformadas de Fourier). Testes qualitativos de triagem fitoquímica foram realizados para detectar compostos fitoquímicos nos extratos brutos. A atividade antioxidante dos extratos vegetais foi caracterizada pelo método de eliminação de radicais livres DPPH (2,2-difenil-1-picrilhidrazil). Os resultados mostraram que a atividade antioxidante usando DPPH aumentou de uma maneira dependente da concentração e diminuiu a viabilidade celular e a inibição do crescimento celular de uma maneira dependente da dose. Os resultados deste estudo indicaram que o extrato de fruta exibiu bom potencial antiproliferação e antioxidante. Os sete grupos funcionais de fitocompostos, como ácido carboxílico, sal de amina, compostos aromáticos, alceno cíclico, aldeído, compostos de flúor e alceno, foram detectados por FT-IR, o que indicou que extratos de frutas de Citrus paradisi possuíam vasto potencial como medicamento, especialmente no tratamento de câncer do fígado.

GKK1032B from endophytic Penicillium citrinum induces the apoptosis of human osteosarcoma MG63 cells through caspase pathway activation / 中国天然药物

Chemical investigation of the culture extract of an endophytic Penicillium citrinum from Dendrobium officinale, afforded nine citrinin derivatives (1-9) and one peptide-polyketide hybrid GKK1032B (10). The structures of these compounds were determined by spectroscopic methods. The absolute configurations of 1 and 2 were determined for the first time by calculation of electronic circular dichroism (ECD) data. Among them, GKK1032B (10) showed significant cytotoxicity against human osteosarcoma cell line MG63 with an IC50 value of 3.49 μmol·L-1, and a primary mechanistic study revealed that it induced the apoptosis of MG63 cellsvia caspase pathway activation.

Explore the antiproliferative phytocompounds from ethanolic extracts of Citrus paradisi against liver cancer cell line by chemical analysis using TLC and FT-IR spectroscopy / Explorar os fitocompostos antiproliferativos de extratos etanólicos de Citrus paradisi contra linhagem de células de câncer de fígado por análise química usando espectroscopia de TLC e FT-IR

The aim of the present study was to evaluate the in vitro antiproliferative activity of ethanolic extract of leaves and fruits Citrus paradisi plant on HepG-2 liver cell lines by MTT (3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2Hterazolium bromide) assay and to isolate and characterize the antiproliferative compounds by TLC (Thin layer chromatography) and FT-IR (Fourier transforms Infrared) spectroscopy. Qualitative phytochemical screening tests were performed to detect phytochemicals compounds from the crude extracts. Antioxidant activity of the plant extracts were characterized by using DPPH (2,2-Diphenyl-1-picrylhydrazyl) free radical scavenging method. The results showed that antioxidant activity using DPPH were found to be increased in a concentration dependent manner and decreased cell viability and cell growth inhibition in a dose dependent manner. The findings from this study indicated that fruit extract exhibited good antiproliferation and antioxidant potential. The seven functional groups of phytocompounds such as carboxylic acid, amine salt, aromatic compounds, cyclic alkene, aldehyde, fluoro compounds and alkene were detected by FT-IR which indicated that fruit extracts of Citrus paradisi possessed vast potential as a medicinal drug especially in liver cancer treatment.

O objetivo do presente estudo foi avaliar a atividade antiproliferativa in vitro do extrato etanólico de folhas e frutos da planta Citrus paradisi em linhagens de células hepáticas HepG-2 por MTT (3- (4, 5-dimetil-2-tiazolil) -2, Ensaio de brometo de 5-difenil-2H-terazólio) e isolar e caracterizar os compostos antiproliferativos por espectroscopia de TLC (cromatografia de camada fina) e FT-IR (infravermelho com transformadas de Fourier). Testes qualitativos de triagem fitoquímica foram realizados para detectar compostos fitoquímicos nos extratos brutos. A atividade antioxidante dos extratos vegetais foi caracterizada pelo método de eliminação de radicais livres DPPH (2,2-difenil-1-picrilhidrazil). Os resultados mostraram que a atividade antioxidante usando DPPH aumentou de uma maneira dependente da concentração e diminuiu a viabilidade celular e a inibição do crescimento celular de uma maneira dependente da dose. Os resultados deste estudo indicaram que o extrato de fruta exibiu bom potencial antiproliferação e antioxidante. Os sete grupos funcionais de fitocompostos, como ácido carboxílico, sal de amina, compostos aromáticos, alceno cíclico, aldeído, compostos de flúor e alceno, foram detectados por FT-IR, o que indicou que extratos de frutas de Citrus paradisi possuíam vasto potencial como medicamento, especialmente no tratamento de câncer do fígado.

Multi-omics approaches identify

Autophagy is a critical cellular homeostatic mechanism, and its dysfunction is linked to invasive breast carcinoma (BRCA). Recently, several omics methods have been applied to explore autophagic regulators in BRCA; however, more reliable and robust approaches for identifying crucial regulators and druggable targets remain to be discovered. Thus, we report here the results of multi-omics approaches to identify potential autophagic regulators in BRCA, including gene expression (EXP), DNA methylation (MET) and copy number alterations (CNAs) from The Cancer Genome Atlas (TCGA). Newly identified candidate genes, such as

Cytotoxic effects of Thai noni juice product ethanolic extracts against cholangiocarcinoma cell lines

Objective: To investigate the cytotoxic activity and molecular mechanism(s) of two Thai noni juice (TNJ) products ethanolic extracts against cholangiocarcinoma (CCA) cell lines and non-cancerous cells, and to explore phenolic acid compositions of TNJ products. Methods: Phenolic acid profiles of TNJ Chiangrai (TNJ-Cr) and TNJ Buasri (TNJ-Bs) ethanolic extracts were determined by HPLC. The cytotoxicity of TNJ ethanolic extracts on cancer and non-cancerous cells was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and trypan blue assays. Mechanism(s) underlying the anti-CCA activity of TNJ ethanolic extracts were determined by cell cycle, apoptosis, and reactive oxygen species (ROS) generation assays. The expression levels of proteins involved in apoptosis and ERK signaling were evaluated by Western blot analysis. Results: Phenolic acid profiles of both TNJ ethanolic extracts showed that the p-hydroxybenzoic, vanillic, and protocatechuic acids were the major phenolic acids in TNJ products. Cytotoxicity assays revealed that the TNJ-Cr and TNJ-Bs ethanolic extracts reduced viability of CCA cell lines through induction of apoptosis by up-regulation of p53 and Bax proapoptotic proteins. Both TNJ ethanolic extracts promoted ROS generation by activating the ERK1/2 signaling in well-differentiated CCA cells KKU-213B. Meanwhile, TNJ ethanolic extracts did not induce ROS production in poorly differentiated CCA cells KKU-100. Both TNJ ethanolic extracts showed no toxicity to human peripheral blood mononuclear cells. Conclusions: TNJ ethanolic extracts could inhibit CCA cell proliferation by inducing ROS generation and apoptosis and may be applicable for combination therapies in CCA treatment.

Phyllanthus fraternus manifests potent anti-proliferative activity on cultured Daudi cells

Objective: The aim of this study is to observe the apoptosis of Phyllanthus fraternus Webster against Daudi cells and to study its primary mechanism. Materials and Methods: Antiproliferative activity of cultured Daudi cells was evaluated using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay in a dose- and time-dependent manner after treatment with the hydroalcoholic extract of P. fraternus . Trypan blue viability assay was also performed. Apoptosis induction in the cells posttreatment was determined by DNA fragmentation assay, Agarose gel electrophoresis, and Acridine orange/Ethidium bromide dual staining. Protein isolation and analysis was carried out using the standard polyacrylamide gel electrophoresis protocols. Results: The extracts inhibited the growth and proliferation of Daudi cells through induced cell death, which was dose-dependent and time-dependent. The IC50 value was found to be 220 μg/ml after 72 h of treatment. The induction of DNA fragmentation and increase in a number of apoptotic cells posttreatment suggest the possibility of apoptosis induction. A significant decrease in protein level was also observed. Conclusion: The results raise the possibility that the hydroalcoholic extract of P. fraternus could be a potent chemotherapeutic agent for the treatment of various cancers. Further evaluation of its potency as a chemotherapeutic agent is imperative

Antiproliferation activity of God's crown fruit (Phaleria macrocarpa) extract and fractions against MCM-B2 breast cancer cells

Breast cancer is a disease caused by abnormal cell proliferation in the breast. God’s crown fruit (Phaleria macrocarpa)and its seed have potential as an antiproliferation of cancer cells. It contains active compounds such as flavonoids,alkaloids, polyphenols, and tannins. The sample of God’s crown fruit was obtained by extraction and fractionationusing the maceration method. Cytotoxicity of extracts and fractions was determined using Brine Shrimp Lethality Testmethod. Antiproliferation activity test of God’s crown fruit against MCM-B2 was performed using the hemacytometermethod. The God’s crown fruit sample consists of crude ethanol extract, n-hexane fraction, ethyl acetate fraction, andwater fraction. Lethal concentration 50 (LC50) values in crude ethanol extract, n-hexane fraction, ethyl acetate fraction,and water fraction were 13.72, 147.55, 405.81, and 149.55 ppm, respectively. The concentration of the test sample wasdirectly used for the antiproliferation activity test on MCM-B2 cells. God’s crown fruit can act as antiproliferation ofMCM-B2. The smallest concentration of those samples has inhibited MCM-B2 cell proliferation which is 3.5 ppmcrude ethanol extract lower than 100 ppm doxorubicin. The maximum percentage of the antiproliferation activity ofcrude ethanol extract (56 ppm) was able to inhibit MCM-B2 cell proliferation by 58.28% while doxorubicin (100 ppm)by 31.2%. This is due to the fact that crude ethanol extract has a lot of complex polar phytochemical content. The crudeethanol extract compounds inhibit MCM-B2 cell proliferation synergistically

Preparation and Properties of Rapamycin Sustained-release Film / 中山大学学报(医学科学版)

@#【Objective】To prepare rapamycin（RAPA）sustained-release film and to evaluate its dissolution.【Methods】RAPA sustained- release film was created by using polymer polyactioglyconic acid （PLGA），copolymer of polyactic acid（PLA）and polyglycolic acid（PGA）. Drug content of the sustained-release film was determined using specificity test，recovery，relative standard deviation（RSD）and stability test. Then，the dissolution of the sustained- release film was analyzed.【Results】The concentration of RAPA had a linear relationship with peak area，which ranged between 0.408 μg/mL and 40.8 μg/mL through the standard curve. The specificity test of the drug content determination indicated the excipient of the film and the solution with 0.3% sodium dodecyl sulfate（SDS）did not affect in determining the RAPA content. The recovery and RSD were excellent through drug content determination in blank films，which had three different levels of RAPA concentrations. The mean RAPA content of the sustained-release films was（112.6±10.1）μg（RSD 8.99%）through the drug content determination of the films，and the stability of RAPA with 0.3% SDS was good within 15 days. In addition，dissolution test of the sustained- release film indicated that the amount of drug release reached a high level and sustained up to 15 days.【Conclusion】 The RAPA sustained-release film with certain behavioral characteristic parameters had a stable drug content and favorable sustained-release property，and it may have certain application potential in anti-proliferation after glaucoma filtering surgery.

Effect of oxidative stress in SH-SY5Y cell injury induced by deguelin / 中国药理学通报

Aim To study the correlation between oxidative stress and neurotoxicity induced by deguelin, providing the mechanism basis for the structural modification and drug combination about deguelin. Methods SH-SY5Y cells were exposed to deguelin ranging from 1. 56-100 jimol • L"1 for 24 to 72 h, whose survival rate was determined by CCK-8 assay. The content of LDH, MDA levels, GPx and antioidant enzyme activities of SOD were determined using the assay kits ac-cording the manufacturer's protocol. And the content of ROS was determined by flow cytometry. The expressions of MEK, EGF, ERK and CREB were determined by immunoblotting. Results Deguelin obviously inhibited the growth of SH-SY5Y cells in a concentra-tion-and time-dependent manner ( P < 0. 05 ). After the cells were injured by deguelin, the content of ROS, LDH and MDA in SH-SY5Y cells increased obviously (P <0. 05), while the vitality of GPx and SOD decreased obviously ( P < 0. 05) in a dose-dependent manner. Furthermore, the protein expression levels of MEK, EGF, RAS and CREB in MAPK/ERK signaling pathway decreased obviously when treated with deguelin in a dose-dependent manner. (P < 0. 05). Conclusions The trauma of SH-SY5Y cells induced by deguelin is closely related to oxidative stress, in which MAPK/ERK signaling pathway may play a mediating role.

Assessing cytotoxicity and antiproliferation effects of Sida rhombifolia against MCA-B1 and A549 cancer cells

This research aims to determine the cytotoxicity and antiproliferation activities of Sida rhombifolia leavesextract against cancer cells MCA-B1, A549, and normal Vero cells. Sida rhombifolia leaves were extractedwith ethanol using ultrasonication method and fractionated using n-hexane, ethyl acetate, and water. The testedsamples were ethanol extract and n-hexane fraction based on the results of cytotoxicity using the Brine ShrimpLethality Test. The antiproliferation activity test by using Trypan Blue Dye method and the cells harvested afterconfluence on the third or fourth day and the total cells were calculated by using the Neubauer Hemocytometer.The result showed that the inhibitory activity of ethanol extract at a concentration of 500 ppm is 69.44% withIC50 202.556 ppm on MCA-B1 cancer cells and 69.44% with IC50 276.836 ppm on A549 cancer cells, whilethe n-hexane fraction at a concentration of 1,000 ppm was 64.13% with IC50 425.969 ppm in MCA-B1 cancercells and 57.18% with IC50 786.617 ppm on A549 cancer cells. After being tested on normal Vero cells, theinhibition of normal Vero cells proliferation is not more than 1%. This indicates that ethanol extracts andn-hexane fraction are safe for normal cells and analysis by using LC-MS/MS showed a benzazepine compoundin the ethanol extract of S. rhombifolia is known for its role as antiproliferation. These results indicate thatS. rhombifolia leaves extract has the potential to be developed as anticancer compounds..

Antiproliferative and apoptotic effects of the natural alkaline water (Zamzam) in breast cancer cell line MCF-7

Background: Zamzam water (ZW) is a natural alkaline water that contains several minerals that may represent a powerful tool for cancer therapy. Objectives: In this research, in vitro antiproliferative and apoptotic effects of ZW were investigated in the human breast cancer cell line MCF-7. Materials and Methods: This study was conducted between January 2015 and February 2016. The effects of ZW on the morphology and the cell viability of human breast cancer cell line MCF-7 were determined. The cell death type and cell cycle changes were investigated using flow cytometry. Finally, reactive oxygen species (ROS) were also measured by fluorometric technique. Results: MCF-7 cells treated with either ZW with adjusted pH at 7.2 or unadjusted pH at 8 showed reduced cell viability of cancerous cells. The cell death occurred through the apoptosis pathway under both treatment conditions. The treated MCF-7 cells were arrested in the G2/M phase and decreased in the G1 phase. Only the unadjusted pH ZW sample demonstrated an increase in the production of both cytoplasmic and mitochondrial ROS in MCF-7 cells. Conclusion: All the results in the present study indicated, for the first time, that ZW might have anticancer and apoptotic effects on breast cancer cell line

Synthesis of nitro-substituted curcumin analogs and their apoptosis-inducing activity on hepatocellular cancer cells / 国际药学研究杂志

Objective:To design and synthesize mono-carbonyl curcumin analogs with tumor suppressor activi- ty using substituted benzaldehyde and acetone as the raw material. Methods: Acetone and substituted benzaldehyde were used as starting compounds to synthesize the target compounds via aldol condensation reaction. The antiproliferation activity and apoptosis-inducing activity of target compounds against HepG2 cells were evaluated by MTT assay and flow cytometry, respectively. The medicinal chemical properties of the compounds were calculated online from the website: www.molinspiration.com. Results: Six compounds were synthesized and their structures were verified by the 1H NMR, 13C NMR and MS data. Compound 1 exhibited more potent antiproliferative and apoptosis-inducing activity against HepG2 cells than curcumin. The medicinal chemical properties of 1 were more consistent with Lipinski’s Rule of Five and it was ea sier for 1 to penetrate cell membranes than other compounds. Conclusion: The introduction of nitro group into the ortho-position of aromatic rings in mono-carbonyl curcumin analogs could enhance the anticancer activity, which is of great significance for the design and synthesis of mono-carbonyl curcumin analogs with better anticancer activity.

Induction of sub-G arrest and apoptosis by seed extract of Moringa peregrina (Forssk.) Fiori in cervical and prostate cancer cell lines / 中西医结合学报

OBJECTIVE@#This study investigated cytotoxicity and induction of apoptosis in human cervical cancer cells (HELA) and prostate cancer cells (PC-3) using the most active fraction of Moringa peregrina seed extract.@*METHODS@#Dried and powdered seeds were extracted using 95% ethanol. The total ethanolic extract was further dissolved in distilled water and separated into petroleum ether, chloroform, ethyl acetate and aqueous extracts. Based on the results of in vitro anticancer studies of all extracts, the most highly active extract was selected for evaluation of apoptosis induction and cell cycle analysis on HELA and PC-3 cells at its half maximal inhibitory concentration using flow cytometry; DNA fragmentation by agarose gel electrophoresis and the expression of protein were measured by Western blot.@*RESULTS@#The chloroform fraction from the ethanolic extract of M. peregrina (CFEE) was the most active antitumor fraction. The selectivity index, determined using the normal Vero cell line, indicated that CFEE had a high degree of selectivity against HELA and PC-3 cells. CFEE induced apoptosis, confirmed by cell cycle arrest at sub-G phase and DNA fragmentation. CFEE induced an increase in mRNA expression of caspase-3, a decrease in Bcl-2 mRNA expression, and decreased ATP levels. CFEE increased protein expression of caspase-3 and decreased protein expression of poly-ADP-ribose polymerase-1 (PARP-1). Flow cytometric analysis showed an appreciable increase in the number of cells in the early apoptotic stage in CFEE-treated HELA and PC-3 cells. CFEE treatment significantly increased lipid peroxidation (malondialdehyde level) in HELA and PC-3 cells.@*CONCLUSION@#Seed extract of M. peregrina displayed a significant antitumor effect through apoptosis induction in HELA and PC-3 cells.

Phytochemical Screening and Synergistic Anti-proliferative Activity against Selected Cancer Cell Lines of Moringa oleifera and Indigofera arrecta Leaf Extracts

Medicinal plants present a plausible source for anticancer agents. Combination of plant extracts and plant-derived compounds with the currently used cancer drugs has shown a marked improvement of the conventional drugs' efficacy and reduced toxicity. This study evaluated; phytochemical screening, antiproliferative activity and drug interaction potentials of Moringa oleifera and Indigofera arrecta leaf extracts with 5-fluoro uracil against selected cancer cell lines. Phytochemical screening was done using standard procedures. The common 3– (4, 5-dimethylthiazol-2-yr) -2, 5-diphenyltetrazolium (MTT) assay was used to determine the growth inhibitory potential of the extracts towards cancer cells. Drug interaction assays were done using constant ratio combination method. Alkaloids, terpenoids, tannins, flavonoids, glycosides, phenols and saponins were found to be present in the plant's extracts. M. oleifera and I. arrecta methanol-dichloromethane extracts had the highest activity compared to water extracts. All the extracts showed antiproliferative activities towards; HCC 1395 (breast), DU145 (prostate) and Hela (cervical) cancer cell lines. The extracts were not cytotoxic towards Vero cells (IC50>1000 µg/ml). I. arrecta and M. oleifera inhibited DU145 the most with IC50 values of 111.110 µg/ml and 66.290 µg/ml respectively. The plant extracts synergistically inhibited the growth of cancer cells (CI<1). Combination of the plant extracts and 5-Fluorouracil depicted that the concentration of the conventional drug could be reduced and yet achieve the same desired effect against cancerous cells (Dose reduction index (DRI) >1). Further studies to isolate the bioactive compounds and deduce the probable mechanisms of action are recommended.

Synthesis of trifluoromethyl-substituted mono-carbonyl curcumin analogs and evaluation of their anti-proliferation activity on lung cancer cells / 国际药学研究杂志

Objective To synthesize trifluoromethyl-substituted mono-carbonyl curcumin analogs and investigate their effects on the proliferation of human lung cancer cells A549 and NCI-H460. Methods Six mono-carbonyl curcumin analogs 1a-1f were synthesized via Aldol condensation using commercially available 2-trifluoromethyl benzadehyde and different ketones (actone, cyclopentanone, cyclohexanone, piperid-4-one, and 1-methylpiperid-4-one). MTT method was used to test the effect of 1a-1f on the proliferation of A549 and NCI-H460 cells. Results Compared with curcumin, most of the mono-carbonyl curcumin analogs 1a-1f exhibited anti-proliferation activity on the A549 cells. The values of IC50 were lower than that of curcumin (P＜0.01), and 1a and 1f showed much better activities both on the A549 and NCI-H460 cells, with their IC50 values were much lower than that of curcumin (P＜0.01).Among them, 1f showed better medicinal chemical properties, with the relative molecular mass less than 500, cLogP 5.25, and the polar surface area (PSA) 37.38, which was more better accorded with the Lipinski′s five rules. Conclusion Six mono-carbonyl curcumin analogs 1a-1f were synthesized, and 1f showed much better anti-proliferation activity on A549 and NCI-H460 cells.

Study on relationship between IGFBP-5/p53 axis and anti-proliferation effect of tetrandrine in MCF-7 cells / 中国药理学通报

Aim To study the effect of tetrandrine ( Tet ) on proliferation of MCF-7 breast cancer cells and the possible mechanism underlying this biological process. Methods CCK-8, flow cytometric and Western blot were introduced to analyze the effect of Tet on proliferation and apoptosis in MCF-7 cells.Re-al-time PCR and/or Western blot assay were employed to detect the effect of Tet on expression of IGFBP-5 , p53 and MDM2.CCK-8 and recombinant adenovirus were utilized to determine the effect of IGFBP-5 on the proliferation inhibitory effect of Tet .Western blot assay was introduced to evaluate the effect of IGFBP-5 on p53 which was induced by Tet .Results Tet inhibited the proliferation , arrested cell cycle at G 1 phase and decreased the expression of PCNA concentration dependently in MCF-7 cells.Meanwhile, Tet increased the percentage of apoptotic cells , the level of Bad and reduced the level of Bcl-2.Tet increased the expres-sion of IGFBP-5 either mRNA or protein , over-expres-sion of IGFBP-5 enhanced the anti-proliferation activity of Tet in MCF-7 cells, but knockdown of IGFBP-5 at-tenuated this effect of Tet .Tet increased the level of p53 and decreased that of MDM2, and exogenous IG-FBP-5 enhanced the effect of Tet on p53 and MDM2, respectively .Conclusion Tet can inhibit the prolifer-ation of MCF-7 cells, and this activity is partly media-ted by increasing the function of p 53 signal , which may be triggered by the Tet-induced IGFBP-5.

Inhibitory growth effect of honokiol and BMP7 in human colon cancer cells / 中国药理学通报

Aim To investigate the anti-proliferation effect of honokial on human colon cancer cells HCT116 and the possible mechanism. Methods Crystal stai-ning and flow cytometry assay were introduced to test the proliferation inhibitory and cell cycle arrested effect of honokial on HCT116 cells. Western blot was used to analyse the expression of PCNA and induction effect of apoptosis. Western blot and PCR assay were conducted to assess the change of BMP7. Via exogenous adenovi-ruses of BMP7 and its antibody combined with honoki-al,crystal violet staining and Western blot were used to analyse the effect on HCT116 cells. Results Honoki-al inhibited the growth of HCT116 in a time-and con- centration-dependent way,induced apoptosis and arres-ted at G2 phase; Western blot assay showed honokial up-regulated the level of PCNA and BMP7,and down-regulated the expression of Bcl-2; Western blot result also showed that exogenous adenoviruses of BMP7 en-hanced the effect of honokial on proliferation inhibition and apoptosis, while BMP7 antibody reversed such effects of honokial. Conclusion Honokial can inhibit the proliferation and induce apoptosis on HCT116 cells,which may be mediated by the up-regulation of BMP7.

Anti-proliferation activity of terpenoids isolated from Euphorbia kansui in human cancer cells and their structure-activity relationship / 中国天然药物

Euphorbia kansui is a commonly used traditional Chinese medicine for the treatment of edema, pleural effusion, and asthma, etc. According to the previous researches, terpenoids in E. kansui possess various biological activities, e.g., anti-virus, anti-allergy, antitumor effects. In this work, twenty five terpenoids were isolated from E. kansui, including thirteen ingenane- and eight jatrophane-type diterpenoids (with two new compounds, kansuinin P and Q) and four triterpenoids. Eighteen of them were analyzed by MTS assay for in vitro anticancer activity in five human cancer cell lines. Structure-activity relationship for 12 ingenane-type diterpenoids in colorectal cancer Colo205 cells were preliminary studied. Significant anti-proliferation activities were observed in human melanoma cells breast cancer MDA-MB-435 cells and Colo205 cells. More than half of the isolated ingenane-type diterpenoids showed inhibitory activities in MDA-MB-435 cells. Eight ingenane- and one jatrophane-type diterpenoids possessed much lower IC values in MDA-MB-435 cells than positive control staurosporine. Preliminary structure-activity relationship analysis showed that substituent on position 20 was important for the activity of ingenane-type diterpenoids in Colo205 cells and substituent on position 3 contributed more significant biological activity of the compounds than that on position 5 in both MDA-MB-435 and Colo205 cells.

Anti-proliferative effect of terpenes on human prostate cancer cells: Natural sources and their potential role as chemopreventive agents / Efecto anti-proliferativo de los terpenos en células de cáncer de próstata humana: Fuentes naturales y su rol potencial como agentes quimiopreventivos

ABSTRACT Prostate cancer is one of the neoplastic diseases with the highest morbidity and mortality in the world. The diversity of available treatments and side effects related to therapeutic treatments are severe and affect a patient's quality of life. Thus, to creating new therapeutic alternatives to reduce morbidity and creating safe and effective therapies is a constant challenge. Recently, the use of traditional medicine and chemoprevention has gained importance. Several clinical and epidemiological studies suggest that a high-terpenoid compound-based diet is associated with a reduced risk of prostate cancer. This review is focused on the anti-proliferative effects of different terpenoids isolated from natural sources on human prostate cancer cells, with the aim of setting the basis to use these compounds as phytotherapeutic, nutraceutical and functional ingredients.

RESUMEN El cáncer de próstata es una de las neoplasias que produce gran morbilidad y mortalidad en el mundo. Los tratamientos y los efectos secundarios de la terapia son severos y afectan la calidad de vida del paciente. Por esto, es necesario crear nuevas alternativas terapéuticas para reducir la morbilidad y generar terapias seguras y efectivas es un desafío permanente. En los últimos años, el uso de la medicina tradicional y agentes quimiopreventivos han adquirido importancia. Estudios clínicos y epidemiológicos sugieren que una dieta basada en altas dosis de terpenoides se asocia a una reducción en el riesgo de presentar cáncer de próstata. Esta revisión se centra en los efectos anti-proliferativos sobre las células de cáncer de próstata en humanos de diferentes terpenoides aislados de fuentes naturales, con el objetivo de establecer las bases para utilizar estos compuestos como ingredientes fitoterapéuticos, nutracéuticos y funcionales.