The Experts below are selected from a list of 6 Experts worldwide ranked by ideXlab platform
Yuh-ling Lin - One of the best experts on this subject based on the ideXlab platform.
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a study on inhibition mechanism of breast cancer cells by bis type Triaziquone
European Journal of Pharmacology, 2010Co-Authors: Yuh-ling Lin, B H ChenAbstract:Abstract The objectives of this study were to evaluate the antiproliferation effect of a synthetic quinone-containing compound bis-type Triaziquone (BTZQ) on breast cancer cells BC-M1 and MCF-7. At a dose of 0.42 and 0.79 μM, BTZQ showed a 50% inhibition on BC-M1 and MCF-7 cell growth after 24 h treatment, respectively, but reduced to 0.2 and 0.61 μM after 48 h. A low toxic effect was observed for skin fibroblast cell after BTZQ treatment for 48 h at a dose from 0.0625–0.25 μM. BTZQ was more effective in inhibiting growth of breast cancer cells than tamoxifen. Additionally, BTZQ-treated BC-M1 cells under hypoxia condition for 48 h exhibited a higher cytotoxicity than under aerobic condition. Cell cycle analysis revealed the arrest of BC-M1 cells at G2/M phase, with accumulation of apoptotic cells at the sub-G1 phase being enhanced following a rise in dose. The expression levels of caspase-3, caspase-8 and caspase-9 were elevated in both dose- and time-dependent responses. Western blot analysis indicated that BTZQ may up-regulate expression of cyclin B, p21, p53 and cytochrome c, but down-regulate cdk1 expression in a dose-dependent manner, leading to apoptosis of BC-M1 cells. All these results suggested that BTZQ may be a potential anti-breast cancer drug.
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Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives
MDPI AG, 2009Co-Authors: Yuh-ling Lin, Jia-wen Liu, Hsien-shou Kuo, Cheng Hua HuangAbstract:Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of Triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC50 value of 2.02 mM, and also weak cytotoxic activity against SF cells with an LC50 value over 10 mM for 24 hr treatment. Comparing the viability of normal fibroblast cells treated with compound 1a and TZQ, the LC50 value of the latter was 2.52 mM, indicating more toxicity than compound 1a. This significantly decreased cytotoxicity of compound 1a towards normal SF cells, while still maintaining the anticancer activity towards Hep2 cells is an interesting feature. Among the seven compounds synthesized, compound 1c has similar toxicity effects on the three cancer cell lines and SF normal cells as the TZQ monomer
Cheng Hua Huang - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives
MDPI AG, 2009Co-Authors: Yuh-ling Lin, Jia-wen Liu, Hsien-shou Kuo, Cheng Hua HuangAbstract:Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of Triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC50 value of 2.02 mM, and also weak cytotoxic activity against SF cells with an LC50 value over 10 mM for 24 hr treatment. Comparing the viability of normal fibroblast cells treated with compound 1a and TZQ, the LC50 value of the latter was 2.52 mM, indicating more toxicity than compound 1a. This significantly decreased cytotoxicity of compound 1a towards normal SF cells, while still maintaining the anticancer activity towards Hep2 cells is an interesting feature. Among the seven compounds synthesized, compound 1c has similar toxicity effects on the three cancer cell lines and SF normal cells as the TZQ monomer
B H Chen - One of the best experts on this subject based on the ideXlab platform.
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a study on inhibition mechanism of breast cancer cells by bis type Triaziquone
European Journal of Pharmacology, 2010Co-Authors: Yuh-ling Lin, B H ChenAbstract:Abstract The objectives of this study were to evaluate the antiproliferation effect of a synthetic quinone-containing compound bis-type Triaziquone (BTZQ) on breast cancer cells BC-M1 and MCF-7. At a dose of 0.42 and 0.79 μM, BTZQ showed a 50% inhibition on BC-M1 and MCF-7 cell growth after 24 h treatment, respectively, but reduced to 0.2 and 0.61 μM after 48 h. A low toxic effect was observed for skin fibroblast cell after BTZQ treatment for 48 h at a dose from 0.0625–0.25 μM. BTZQ was more effective in inhibiting growth of breast cancer cells than tamoxifen. Additionally, BTZQ-treated BC-M1 cells under hypoxia condition for 48 h exhibited a higher cytotoxicity than under aerobic condition. Cell cycle analysis revealed the arrest of BC-M1 cells at G2/M phase, with accumulation of apoptotic cells at the sub-G1 phase being enhanced following a rise in dose. The expression levels of caspase-3, caspase-8 and caspase-9 were elevated in both dose- and time-dependent responses. Western blot analysis indicated that BTZQ may up-regulate expression of cyclin B, p21, p53 and cytochrome c, but down-regulate cdk1 expression in a dose-dependent manner, leading to apoptosis of BC-M1 cells. All these results suggested that BTZQ may be a potential anti-breast cancer drug.
Jia-wen Liu - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives
MDPI AG, 2009Co-Authors: Yuh-ling Lin, Jia-wen Liu, Hsien-shou Kuo, Cheng Hua HuangAbstract:Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of Triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC50 value of 2.02 mM, and also weak cytotoxic activity against SF cells with an LC50 value over 10 mM for 24 hr treatment. Comparing the viability of normal fibroblast cells treated with compound 1a and TZQ, the LC50 value of the latter was 2.52 mM, indicating more toxicity than compound 1a. This significantly decreased cytotoxicity of compound 1a towards normal SF cells, while still maintaining the anticancer activity towards Hep2 cells is an interesting feature. Among the seven compounds synthesized, compound 1c has similar toxicity effects on the three cancer cell lines and SF normal cells as the TZQ monomer
Hsien-shou Kuo - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and Antitumor Evaluation of Novel Bis-Triaziquone Derivatives
MDPI AG, 2009Co-Authors: Yuh-ling Lin, Jia-wen Liu, Hsien-shou Kuo, Cheng Hua HuangAbstract:Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of Triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC50 value of 2.02 mM, and also weak cytotoxic activity against SF cells with an LC50 value over 10 mM for 24 hr treatment. Comparing the viability of normal fibroblast cells treated with compound 1a and TZQ, the LC50 value of the latter was 2.52 mM, indicating more toxicity than compound 1a. This significantly decreased cytotoxicity of compound 1a towards normal SF cells, while still maintaining the anticancer activity towards Hep2 cells is an interesting feature. Among the seven compounds synthesized, compound 1c has similar toxicity effects on the three cancer cell lines and SF normal cells as the TZQ monomer
