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Chih-hsin Tang - One of the best experts on this subject based on the ideXlab platform.
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a novel Benzofuran Derivative acdb induces apoptosis of human chondrosarcoma cells through mitochondrial dysfunction and endoplasmic reticulum stress
Oncotarget, 2016Co-Authors: Chien-yu Chen, Chih-shiang Chang, Yi Sun, Yuanli Huang, Chunhao Tsai, Chih-hsin TangAbstract:// Chen-Ming Su 1, 2 , Chien-Yu Chen 3 , Tingting Lu 1 , Yi Sun 1 , Weimin Li 4 , Yuan-Li Huang 5 , Chun-Hao Tsai 6, 7 , Chih-Shiang Chang 3 , Chih-Hsin Tang 2, 5, 8 1 Department of Biomedical Sciences Laboratory, Affiliated Dongyang Hospital of Wenzhou Medical University, Dongyang, Zhejiang, China 2 Graduate Institute of Basic Medical Science, China Medical University, Taichung Taiwan 3 Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan 4 Department of Cardiology, Affiliated Dongyang Hospital of Wenzhou Medical University, Dongyang, Zhejiang, China 5 Department of Biotechnology, College of Health Science, Asia University, Taichung, Taiwan 6 School of Medicine, China Medical University, Taichung, Taiwan 7 Department of Orthopedic Surgery, China Medical University Hospital, Taichung, Taiwan 8 Department of Pharmacology, School of Medicine, China Medical University, Taichung, Taiwan Correspondence to: Chih-Shiang Chang, email: chihshiang3@gmail.com Chih-Hsin, Tang, email: chtang@mail.cmu.edu.tw Keywords: Benzofuran, chondrosarcoma, apoptosis, endoplasmic reticulum (ER) stress, mitochondrial dysfunction Received: August 25, 2016 Accepted: October 19, 2016 Published: November 07, 2016 ABSTRACT Chondrosarcoma is one of the bone tumor with high mortality in respond to poor radiation and chemotherapy treatment. Here, we analyze the antitumor activity of a novel Benzofuran Derivative, 2-amino-3-(2-chlorophenyl)-6-(4-dimethylaminophenyl)Benzofuran-4-yl acetate (ACDB), in human chondrosarcoma cells. ACDB increased the cell apoptosis of human chondrosarcomas without harm in chondrocytes. ACDB also enhanced endoplasmic reticulum (ER) stress, which was characterized by varieties in the cytosolic calcium levels and induced the expression of glucose-regulated protein (GRP) and calpain. Furthermore, the ACDB-induced chondrosarcoma apoptosis was associated with the upregulation of the B cell lymphoma-2 (Bcl-2) family members including pro- and anti-apoptotic proteins, downregulation of dysfunctional mitochondria that released cytochrome C, and subsequent activation of caspases-3. In addition, the ACDB-mediated cellular apoptosis was suppressed by transfecting cells with glucose-regulated protein (GRP) and calpain siRNA or treating cells with ER stress chelators and caspase inhibitors. Interestingly, animal experiments illustrated a reduction in the tumor volume following ACDB treatment. Together, these results suggest that ACDB may be a novel tumor suppressor of chondrosarcoma, and this study demonstrates that the novel antitumor agent, ACDB, induced apoptosis by mitochondrial dysfunction and ER stress in human chondrosarcoma cells in vitro and in vivo .
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bl 038 a Benzofuran Derivative induces cell apoptosis in human chondrosarcoma cells through reactive oxygen species mitochondrial dysfunction and the caspases dependent pathway
International Journal of Molecular Sciences, 2016Co-Authors: Ju-fang Liu, Chien-yu Chen, Hsien-te Chen, Chih-shiang Chang, Chih-hsin TangAbstract:Chondrosarcoma is a highly malignant cartilage-forming bone tumor that has the capacity to invade locally and cause distant metastasis. Moreover, chondrosarcoma is intrinsically resistant to conventional chemotherapy or radiotherapy. The novel Benzofuran Derivative, BL-038 (2-amino-3-(2,6-dichlorophenyl)-6-(4-methoxyphenyl)Benzofuran-4-yl acetate), has been evaluated for its anticancer effects in human chondrosarcoma cells. BL-038 caused cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353, but not in primary chondrocytes. Treatment of chondrosarcoma with BL-038 also induced reactive oxygen species (ROS) production. Furthermore, BL-038 decreased mitochondrial membrane potential (MMP) and changed mitochondrial-related apoptosis, by downregulating the anti-apoptotic activity members (Bcl-2, Bcl-xL) and upregulating pro-apoptotic members (Bax, Bak) of the B-cell lymphoma 2 (Bcl-2) family of proteins, key regulators of the apoptotic machinery in cells. These results demonstrate that in human chondrosarcoma cells, the apoptotic and cytotoxic effects of BL-038 are mediated by the intrinsic mitochondria-mediated apoptotic pathway, which in turn causes the release of cytochrome c, the activation of caspase-9 and caspase-3, and the cleavage of poly (ADP-ribose) polymerase (PARP), to elicit apoptosis response. Our results show that the Benzofuran Derivative BL-038 induces apoptosis in chondrosarcoma cells.
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BL-038, a Benzofuran Derivative, Induces Cell Apoptosis in Human Chondrosarcoma Cells through Reactive Oxygen Species/Mitochondrial Dysfunction and the Caspases Dependent Pathway
MDPI AG, 2016Co-Authors: Ju-fang Liu, Chien-yu Chen, Hsien-te Chen, Chih-shiang Chang, Chih-hsin TangAbstract:Chondrosarcoma is a highly malignant cartilage-forming bone tumor that has the capacity to invade locally and cause distant metastasis. Moreover, chondrosarcoma is intrinsically resistant to conventional chemotherapy or radiotherapy. The novel Benzofuran Derivative, BL-038 (2-amino-3-(2,6-dichlorophenyl)-6-(4-methoxyphenyl)Benzofuran-4-yl acetate), has been evaluated for its anticancer effects in human chondrosarcoma cells. BL-038 caused cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353, but not in primary chondrocytes. Treatment of chondrosarcoma with BL-038 also induced reactive oxygen species (ROS) production. Furthermore, BL-038 decreased mitochondrial membrane potential (MMP) and changed mitochondrial-related apoptosis, by downregulating the anti-apoptotic activity members (Bcl-2, Bcl-xL) and upregulating pro-apoptotic members (Bax, Bak) of the B-cell lymphoma 2 (Bcl-2) family of proteins, key regulators of the apoptotic machinery in cells. These results demonstrate that in human chondrosarcoma cells, the apoptotic and cytotoxic effects of BL-038 are mediated by the intrinsic mitochondria-mediated apoptotic pathway, which in turn causes the release of cytochrome c, the activation of caspase-9 and caspase-3, and the cleavage of poly (ADP-ribose) polymerase (PARP), to elicit apoptosis response. Our results show that the Benzofuran Derivative BL-038 induces apoptosis in chondrosarcoma cells
Alireza Khoshroo - One of the best experts on this subject based on the ideXlab platform.
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graphene sheet for improving the electrocatalytic activity of a Benzofuran Derivative modified electrode for determination of epinephrine in the presence of serotonin
Journal of Analytical Chemistry, 2017Co-Authors: Mohammad Mazloumardakani, Behnaz Brazesh, Laleh Hosseinzadeh, Alireza KhoshrooAbstract:A nanocomposite system based on coumarin Derivative and graphene sheet was used to prepare a new electrochemical sensor. The objective of the mentioned nanocomposite was to investigate novel electrochemical properties enabling the quantification of epinephrine (Ep). Cyclic voltammetry was used to study the redox properties of the mentioned modified electrode at different scan rates. Henceforward, the electrocatalytic oxidation of Ep at the surface of the modified electrode was considered. The data has shown excellent catalytic activity of the modified electrode for the electrooxidation of Ep, which leads to a reduction of overpotential for more than 238 mV. According to differential pulse voltammetry (DPV), the oxidation of Ep showed a dynamic range between 0.1 and 1000.0 μM and the detection limit (3s) of 0.011 μM. Besides, DPV was used for the determination of Ep at the mentioned modified electrode in the presence of serotonin.
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oxidized multi walled carbon nanotubes for improving the electrocatalytic activity of a Benzofuran Derivative modified electrode
Nanochemistry Research, 2016Co-Authors: Mohammad Mazloumardakani, Abolfazl Nasersadrabadi, Alireza KhoshrooAbstract:In the present paper, the use of a novel carbon paste electrode modified by 7,8-dihydroxy-3,3,6-trimethyl-3,4-dihydrodibenzo[b,d]furan-1(2H)-one (DTD) and oxidized multi-walled carbon nanotubes (OCNTs) is described for determination of levodopa (LD), acetaminophen (AC) and tryptophan (Trp) by a simple and rapid method. At first, the electrochemical behavior of DTD is studied, then, the mediated oxidation of LD at the modified electrode is investigated. At the optimum pH of 7.4, the oxidation of LD occurs at a potential about 330 mV less positive than that of an unmodified carbon paste electrode. Based on differential pulse voltammetry (DPV), the oxidation current of LD exhibits a linear range between 1.0 and 2000.0 μM of LD with a detection limit (3σ) of 0.36 μM. DPV was also used for simultaneous determination of LD, AC and Trp at the modified electrode. Finally, the proposed electrochemical sensor was used for determinations of these substances in human serum sample.
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Carbon nanotube electrochemical sensor based on and Benzofuran Derivative as a mediator for the determination of levodopa, acetaminophen, and tryptophan
Ionics, 2015Co-Authors: Mohammad Mazloum-ardakani, Maryam Zokaie, Alireza KhoshrooAbstract:In this research, a (7,8-dihydroxy-3,3,6-trimethyl-3,4-dihydrodibenzo[b,d]furan-1(2H)-one] (DTDF) multi-walled carbon nanotube modified carbon paste electrode was constructed and used as an excellent electrocatalyst in the oxidation of levodopa (LD) in the presence of acetaminophen (AC) and tryptophan (TRP). In the first part of the work, we synthesized DTDF by electrochemically oxidizing the catechol Derivative in the presence of dimedone as a nucleophile in an aqueous solution. A modified carbon paste electrode based on this electrosynthesised compound (DTDF) and carbon nanotubes (CNTs) was prepared. Cyclic voltammetry was used to investigate the redox properties of this modified electrode at various scan rates. Next, the mediated oxidation of LD at the modified electrode was described. At the optimum pH of 7.0, the oxidation of LD occurs at a potential about 330 mV less positive than that of an unmodified carbon paste electrode. Based on differential pulse voltammetry (DPV), the oxidation of LD exhibited a dynamic range between 1.0 and 1000.0 μM and a detection limit of 0.46 μM. DPV was used for simultaneous determination of LD, AC, and TRP at the modified electrode and quantitation of LD, AC, and TRP in some real samples by the standard addition method.
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simultaneous determination of isoproterenol acetaminophen and folic acid using nanostructured electrochemical sensor based on Benzofuran Derivative and carbon nanotubes
Journal of the Brazilian Chemical Society, 2014Co-Authors: Mohammad Mazloumardakani, Seyyed Hamid Ahmadi, Zohal Safaei Mahmoudabadi, Alireza KhoshrooAbstract:No presente artigo, o uso de pasta de eletrodo de carbono modificada por nanotubos de carbono e derivados de Benzofurano (1-(4-(1,3-ditiolan-2-il)-6,7-dihidroxi-2-metil-6,7-dihidroBenzofuran-3-il) etanona) para a determinacao de isoproterenol (IP) foi descrito. O coeficiente de transferencia de carga, α, e a constante de transferencia de carga, ks, para a transferencia de eletrons entre o derivado de Benzofurano e a pasta de eletrodo de carbono foram calculados como 0,52 e 1,04 s-1, respectivamente. O potencial anodico do IP diminui cerca de 256 mV com esse eletrodo modificado. Picos de corrente de voltametria de pulso diferencial (DPV) do IP, acetaminofeno (AC) e acido folico (FA) aumentam linearmente com concentracoes na faixa de 0,05-2000 µmol L-1, 50,0-1200 µmol L-1 e 67,0-1600 µmol L-1, respectivamente e os limites de deteccao para IP, AC e FA foram 0,020 µmol L-1, 0,385 µmol L-1 e 0,690 µmol L-1, respectivamente.
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electrocatalytic properties of functionalized carbon nanotubes with titanium dioxide and Benzofuran Derivative ionic liquid for simultaneous determination of isoproterenol and serotonin
Electrochimica Acta, 2014Co-Authors: Mohammad Mazloumardakani, Alireza KhoshrooAbstract:In this paper we report synthesis and application of functionalized multiwalled carbon nanotubes (CNTs) with titanium dioxide nanoparticles (TiO2), 9-(1,3-dithiolan-2-yl)-6,7-dihydroxy-3,3-dimethyl-3,4-dihydrodibenzo[b,d]furan-1(2H)-one (Benzofuran Derivative (DDF)) and 1-butyl-3-methylimidazolium tetrafluoroborate (IL) as high sensitive sensors for simultaneous determination of isoproterenol (IP) and serotonin (5-HT) using glassy carbon electrode. The modified electrode was characterized by different methods including a scanning electron microscope (SEM), electrochemical impedance spectroscopy (EIS) and voltammetry. A pair of well-defined redox peaks of DDF was obtained at the modified glassy carbon electrode by direct electron transfer between the DDF and the electrode. Dramatically enhanced electrocatalytic activity was exemplified at the modified electrode, as an electrochemical sensor to study the electro oxidation of IP and 5-HT. The differential pulse voltammetry data showed that the obtained anodic peak currents were linearly dependent on the IP and 5-HT concentrations in the range of 0.1–1300.0 and 1.0–650.0 μM, respectively. The applicability of the modified electrode was demonstrated by simultaneous determination of IP and 5-HT in human serum.
Sherif S. Ebada - One of the best experts on this subject based on the ideXlab platform.
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Chemistry and Biology of Rocaglamides (= Flavaglines) and Related Derivatives from Aglaia Species (Meliaceae)
Progress in the chemistry of organic natural products, 2011Co-Authors: Sherif S. Ebada, Neil J. Lajkiewicz, John A. Porco, Min Li-weber, Peter ProkschAbstract:Rocaglamide (1) is the parent cyclopenta[b]Benzofuran Derivative which was first identified as an antileukemic agent from the dried roots and stems of Aglaia elliptifolia Merr. (family Meliaceae) in 1982. Based on these findings, phytochemical interest in this genus increased sharply and up to date, more than 100 rocaglamide-type (= flavagline) compounds and structurally related Derivatives have been identified from over 30 Aglaia species. Rocaglamide-type compounds show pronounced pharmacological activities including primarily (but not exclusively) antiproliferative and anti-inflammatory activity. The molecular mechanisms underlying these activities have been elucidated in recent years and established rocaglamide and several of its Derivatives as interesting candidates for drug development especially in the field of anti-cancer research. Due to their unique structural features and promising pharmacological activities, several strategies leading to total synthesis of enantiomeric rocaglamide Derivatives were developed and optimized. This chapter reviews the chemistry and biology of the rocaglamide-type Derivatives and related compounds, with emphasis on their structural diversity, biosynthesis, pharmacological significance and total synthesis.
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chemistry and biology of rocaglamides flavaglines and related Derivatives from aglaia species meliaceae
Progress in the chemistry of organic natural products, 2011Co-Authors: Neil J. Lajkiewicz, Sherif S. Ebada, John A. Porco, Min Liweber, Peter ProkschAbstract:Rocaglamide (1) is the parent cyclopenta[b]Benzofuran Derivative which was first identified as an antileukemic agent from the dried roots and stems of Aglaia elliptifolia Merr. (family Meliaceae) in 1982. Based on these findings, phytochemical interest in this genus increased sharply and up to date, more than 100 rocaglamide-type (= flavagline) compounds and structurally related Derivatives have been identified from over 30 Aglaia species. Rocaglamide-type compounds show pronounced pharmacological activities including primarily (but not exclusively) antiproliferative and anti-inflammatory activity. The molecular mechanisms underlying these activities have been elucidated in recent years and established rocaglamide and several of its Derivatives as interesting candidates for drug development especially in the field of anti-cancer research. Due to their unique structural features and promising pharmacological activities, several strategies leading to total synthesis of enantiomeric rocaglamide Derivatives were developed and optimized. This chapter reviews the chemistry and biology of the rocaglamide-type Derivatives and related compounds, with emphasis on their structural diversity, biosynthesis, pharmacological significance and total synthesis.
Peter Proksch - One of the best experts on this subject based on the ideXlab platform.
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Chemistry and Biology of Rocaglamides (= Flavaglines) and Related Derivatives from Aglaia Species (Meliaceae)
Progress in the chemistry of organic natural products, 2011Co-Authors: Sherif S. Ebada, Neil J. Lajkiewicz, John A. Porco, Min Li-weber, Peter ProkschAbstract:Rocaglamide (1) is the parent cyclopenta[b]Benzofuran Derivative which was first identified as an antileukemic agent from the dried roots and stems of Aglaia elliptifolia Merr. (family Meliaceae) in 1982. Based on these findings, phytochemical interest in this genus increased sharply and up to date, more than 100 rocaglamide-type (= flavagline) compounds and structurally related Derivatives have been identified from over 30 Aglaia species. Rocaglamide-type compounds show pronounced pharmacological activities including primarily (but not exclusively) antiproliferative and anti-inflammatory activity. The molecular mechanisms underlying these activities have been elucidated in recent years and established rocaglamide and several of its Derivatives as interesting candidates for drug development especially in the field of anti-cancer research. Due to their unique structural features and promising pharmacological activities, several strategies leading to total synthesis of enantiomeric rocaglamide Derivatives were developed and optimized. This chapter reviews the chemistry and biology of the rocaglamide-type Derivatives and related compounds, with emphasis on their structural diversity, biosynthesis, pharmacological significance and total synthesis.
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chemistry and biology of rocaglamides flavaglines and related Derivatives from aglaia species meliaceae
Progress in the chemistry of organic natural products, 2011Co-Authors: Neil J. Lajkiewicz, Sherif S. Ebada, John A. Porco, Min Liweber, Peter ProkschAbstract:Rocaglamide (1) is the parent cyclopenta[b]Benzofuran Derivative which was first identified as an antileukemic agent from the dried roots and stems of Aglaia elliptifolia Merr. (family Meliaceae) in 1982. Based on these findings, phytochemical interest in this genus increased sharply and up to date, more than 100 rocaglamide-type (= flavagline) compounds and structurally related Derivatives have been identified from over 30 Aglaia species. Rocaglamide-type compounds show pronounced pharmacological activities including primarily (but not exclusively) antiproliferative and anti-inflammatory activity. The molecular mechanisms underlying these activities have been elucidated in recent years and established rocaglamide and several of its Derivatives as interesting candidates for drug development especially in the field of anti-cancer research. Due to their unique structural features and promising pharmacological activities, several strategies leading to total synthesis of enantiomeric rocaglamide Derivatives were developed and optimized. This chapter reviews the chemistry and biology of the rocaglamide-type Derivatives and related compounds, with emphasis on their structural diversity, biosynthesis, pharmacological significance and total synthesis.
Chien-yu Chen - One of the best experts on this subject based on the ideXlab platform.
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a novel Benzofuran Derivative acdb induces apoptosis of human chondrosarcoma cells through mitochondrial dysfunction and endoplasmic reticulum stress
Oncotarget, 2016Co-Authors: Chien-yu Chen, Chih-shiang Chang, Yi Sun, Yuanli Huang, Chunhao Tsai, Chih-hsin TangAbstract:// Chen-Ming Su 1, 2 , Chien-Yu Chen 3 , Tingting Lu 1 , Yi Sun 1 , Weimin Li 4 , Yuan-Li Huang 5 , Chun-Hao Tsai 6, 7 , Chih-Shiang Chang 3 , Chih-Hsin Tang 2, 5, 8 1 Department of Biomedical Sciences Laboratory, Affiliated Dongyang Hospital of Wenzhou Medical University, Dongyang, Zhejiang, China 2 Graduate Institute of Basic Medical Science, China Medical University, Taichung Taiwan 3 Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan 4 Department of Cardiology, Affiliated Dongyang Hospital of Wenzhou Medical University, Dongyang, Zhejiang, China 5 Department of Biotechnology, College of Health Science, Asia University, Taichung, Taiwan 6 School of Medicine, China Medical University, Taichung, Taiwan 7 Department of Orthopedic Surgery, China Medical University Hospital, Taichung, Taiwan 8 Department of Pharmacology, School of Medicine, China Medical University, Taichung, Taiwan Correspondence to: Chih-Shiang Chang, email: chihshiang3@gmail.com Chih-Hsin, Tang, email: chtang@mail.cmu.edu.tw Keywords: Benzofuran, chondrosarcoma, apoptosis, endoplasmic reticulum (ER) stress, mitochondrial dysfunction Received: August 25, 2016 Accepted: October 19, 2016 Published: November 07, 2016 ABSTRACT Chondrosarcoma is one of the bone tumor with high mortality in respond to poor radiation and chemotherapy treatment. Here, we analyze the antitumor activity of a novel Benzofuran Derivative, 2-amino-3-(2-chlorophenyl)-6-(4-dimethylaminophenyl)Benzofuran-4-yl acetate (ACDB), in human chondrosarcoma cells. ACDB increased the cell apoptosis of human chondrosarcomas without harm in chondrocytes. ACDB also enhanced endoplasmic reticulum (ER) stress, which was characterized by varieties in the cytosolic calcium levels and induced the expression of glucose-regulated protein (GRP) and calpain. Furthermore, the ACDB-induced chondrosarcoma apoptosis was associated with the upregulation of the B cell lymphoma-2 (Bcl-2) family members including pro- and anti-apoptotic proteins, downregulation of dysfunctional mitochondria that released cytochrome C, and subsequent activation of caspases-3. In addition, the ACDB-mediated cellular apoptosis was suppressed by transfecting cells with glucose-regulated protein (GRP) and calpain siRNA or treating cells with ER stress chelators and caspase inhibitors. Interestingly, animal experiments illustrated a reduction in the tumor volume following ACDB treatment. Together, these results suggest that ACDB may be a novel tumor suppressor of chondrosarcoma, and this study demonstrates that the novel antitumor agent, ACDB, induced apoptosis by mitochondrial dysfunction and ER stress in human chondrosarcoma cells in vitro and in vivo .
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bl 038 a Benzofuran Derivative induces cell apoptosis in human chondrosarcoma cells through reactive oxygen species mitochondrial dysfunction and the caspases dependent pathway
International Journal of Molecular Sciences, 2016Co-Authors: Ju-fang Liu, Chien-yu Chen, Hsien-te Chen, Chih-shiang Chang, Chih-hsin TangAbstract:Chondrosarcoma is a highly malignant cartilage-forming bone tumor that has the capacity to invade locally and cause distant metastasis. Moreover, chondrosarcoma is intrinsically resistant to conventional chemotherapy or radiotherapy. The novel Benzofuran Derivative, BL-038 (2-amino-3-(2,6-dichlorophenyl)-6-(4-methoxyphenyl)Benzofuran-4-yl acetate), has been evaluated for its anticancer effects in human chondrosarcoma cells. BL-038 caused cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353, but not in primary chondrocytes. Treatment of chondrosarcoma with BL-038 also induced reactive oxygen species (ROS) production. Furthermore, BL-038 decreased mitochondrial membrane potential (MMP) and changed mitochondrial-related apoptosis, by downregulating the anti-apoptotic activity members (Bcl-2, Bcl-xL) and upregulating pro-apoptotic members (Bax, Bak) of the B-cell lymphoma 2 (Bcl-2) family of proteins, key regulators of the apoptotic machinery in cells. These results demonstrate that in human chondrosarcoma cells, the apoptotic and cytotoxic effects of BL-038 are mediated by the intrinsic mitochondria-mediated apoptotic pathway, which in turn causes the release of cytochrome c, the activation of caspase-9 and caspase-3, and the cleavage of poly (ADP-ribose) polymerase (PARP), to elicit apoptosis response. Our results show that the Benzofuran Derivative BL-038 induces apoptosis in chondrosarcoma cells.
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BL-038, a Benzofuran Derivative, Induces Cell Apoptosis in Human Chondrosarcoma Cells through Reactive Oxygen Species/Mitochondrial Dysfunction and the Caspases Dependent Pathway
MDPI AG, 2016Co-Authors: Ju-fang Liu, Chien-yu Chen, Hsien-te Chen, Chih-shiang Chang, Chih-hsin TangAbstract:Chondrosarcoma is a highly malignant cartilage-forming bone tumor that has the capacity to invade locally and cause distant metastasis. Moreover, chondrosarcoma is intrinsically resistant to conventional chemotherapy or radiotherapy. The novel Benzofuran Derivative, BL-038 (2-amino-3-(2,6-dichlorophenyl)-6-(4-methoxyphenyl)Benzofuran-4-yl acetate), has been evaluated for its anticancer effects in human chondrosarcoma cells. BL-038 caused cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353, but not in primary chondrocytes. Treatment of chondrosarcoma with BL-038 also induced reactive oxygen species (ROS) production. Furthermore, BL-038 decreased mitochondrial membrane potential (MMP) and changed mitochondrial-related apoptosis, by downregulating the anti-apoptotic activity members (Bcl-2, Bcl-xL) and upregulating pro-apoptotic members (Bax, Bak) of the B-cell lymphoma 2 (Bcl-2) family of proteins, key regulators of the apoptotic machinery in cells. These results demonstrate that in human chondrosarcoma cells, the apoptotic and cytotoxic effects of BL-038 are mediated by the intrinsic mitochondria-mediated apoptotic pathway, which in turn causes the release of cytochrome c, the activation of caspase-9 and caspase-3, and the cleavage of poly (ADP-ribose) polymerase (PARP), to elicit apoptosis response. Our results show that the Benzofuran Derivative BL-038 induces apoptosis in chondrosarcoma cells