Synthesis and biological activity of phthalimide‐based polymers containing 5‐fluorouracil

The attachment of anticancer agents to polymers is a promising approach towards reducing the toxic side‐effects and retaining the potent antitumour activity of these agents. A new tetrahydrophthalimido monomer containing 5‐fluorouracil (ETPFU) and its homopolymer and copolymers with acrylic acid (AA) and with vinyl acetate (VAc) have been synthesized and spectroscopically characterized. The ETPFU contents in poly(ETPFU‐co‐AA) and poly(ETPFU‐co‐VAc) obtained by elemental analysis were 21 mol% and 20 mol%, respectively. The average molecular weights of the polymers determined by gel permeation chromatography were as follows: M_n = 8900 g mol^?1, M_w = 13 300 g mol^?1, M_w/M_n = 1.5 for poly(ETPFU); M_n = 13 500 g mol^?1, M_w = 16 600 g mol^?1, M_w/M_n = 1.2 for poly(ETPFU‐co‐AA); M_n = 8300 g mol^?1, M_w = 11 600 g mol^?1, M_w/M_n = 1.4 poly(ETPFU‐co‐VAc). The in vitro cytotoxicity of the compounds against FM3A and U937 cancer cell lines increased in the following order: ETPFU > 5‐FU > poly(ETPFU) > poly(ETPFU‐co‐AA) > poly(ETPFU‐co‐VAc). The in vivo antitumour activities of all the polymers in Balb/C mice bearing the sarcoma 180 tumour cell line were greater than those of 5‐FU and monomer at the highest dose (800 mg kg^?1). © 2002 Society of Chemical Industry     

Syntheses and biological activities of polymers containing methacryloyl‐2‐oxy‐1,2,3‐propanetricarboxylic acid or 5‐fluorouracil

A series of novel copolymers, poly(methacryloyl‐2‐oxy‐1,2,3‐propanetricarboxylic acid‐co‐exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalic acid) [poly(MTCA‐co‐ETAc)], poly(methacryloyl‐2‐oxy‐1,2,3‐propanetricarboxylic acid‐co‐hydrogenethyl‐exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalate) [poly(MTCA‐co‐HEET)], and poly(methacryloyl‐2‐oxy‐1,2,3‐propanetricarboxylic acid‐co‐α‐ethoxy‐exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthaloyl‐5‐fluorouracil) [poly(MTCA‐co‐EETFU)], were prepared from corresponding monomers by photopolymerizations at 25°C for 48 h. The polymers were identified by FTIR, ¹H‐NMR, and ¹³C‐NMR spectroscopies. The number‐average molecular weights of the fractionated polymers determined by GPC were in the range from 9400 to 14,900 and polydispersity indices were 1.2–1.4. The in vitro IC₅₀ values of polymers against mouse mammary carcinoma (FM3A), mouse leukemia (P388), and human histiocytic lymphoma (U937) as cancer cell lines and mouse liver cells (AC2F) as a normal cell line were much higher compared to that of 5‐fluorouracil (5‐FU). The in vivo antitumor activities of monomers and polymers against mice bearing sarcoma 180 tumor cell line were better than those of 5‐FU. The inhibition of DNA replication and antiangiogenesis activities of MTCA and copolymers were better compared to those of 5‐FU. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 94: 57–64, 2004     

Synthesis and biological activity of medium range molecular weight polymers containing exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalimidocaproic acid

A new monomer, exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalimidocaproic acid (ETCA), was prepared by reaction of maleimidocaproic acid and furan. The homopolymer of ETCA and its copolymers with acrylic acid (AA) or with vinyl acetate (VAc) were obtained by photopolymerizations using 2,2‐dimethoxy‐2‐phenylacetophenone as an initiator at 25 °C. The synthesized ETCA and its polymers were identified by FTIR, ¹H NMR and ¹³C NMR spectroscopies. The apparent average molecular weights and polydispersity indices determined by gel permeation chromatography (GPC) were as follows: M_n = 9600 g mol^?1, M_w = 9800 g mol^?1, M_w/M_n = 1.1 for poly(ETCA); M_n = 14 300 g mol^?1, M_w = 16 200 g mol^?1, M_w/M_n = 1.2 for poly(ETCA‐co‐AA); M_n = 17 900 g mol^?1, M_w = 18 300 g mol^?1, M_w/M_n = 1.1 for poly(ETCA‐co‐VAc). The in vitro cytotoxicity of the synthesized compounds against mouse mammary carcinoma and human histiocytic lymphoma cancer cell lines decreased in the following order: 5‐fluorouracil (5‐FU) ≥ ETCA > polymers. The in vivo antitumour activity of the polymers against Balb/C mice bearing sarcoma 180 tumour cells was greater than that of 5‐FU at all doses tested. © 2001 Society of Chemical Industry     

Synthesis and biological activity of medium molecular weight polymers containing 3,6‐endo‐methylene‐1,2,3,6‐tetrahydrophthalimidobutanoyl‐5‐fluorouracil

A new monomer, 3,6‐endo‐methylene‐1,2,3,6‐tetrahydrophthalimidobutanoyl‐5‐fluorouracil (ETBFU), was synthesized by reaction of 3,6‐endo‐methylene‐1,2,3,6‐tetrahydrophthalimidobutanoyl chloride and 5‐fluorouracil. The homopolymer of ETBFU and its copolymers with acrylic acid (AA) or vinyl acetate (VAc) were prepared by photopolymerization using 2,2‐dimethoxy‐2‐phenylacetophenone as an initiator at 25 °C. The synthesized ETBFU and its polymers were identified by FTIR, ¹H NMR and ¹³C NMR spectroscopies. The ETBFU content in poly(ETBFU‐co‐AA) and poly(ETBFU‐co‐VAc) was 43 and 14 mol%, respectively. The apparent number‐average molecular weight (M_n) of the polymers determined by GPC ranged from 8400 to 11 300. The in vitro cytotoxicity of the samples against mouse mammary carcinoma (FM3A), mouse leukaemia (P388), and human histiocytic lymphoma (U937) cancer cell lines decreased in the order 5‐FU ≥ ETBFU > poly(ETBFU) > poly(ETBFU‐co‐AA) > poly(ETBFU‐co‐VAc). The in vivo antitumour activity of the polymers against Balb/C mice bearing sarcoma 180 tumour cells was greater than that of 5‐fluorouracil at all doses tested. © 2000 Society of Chemical Industry     

WTO与中国农产品的处理技术:食品加工与包装

从1985年起,世界人口增长率超过食品的增长率,可耕地面积和谷物生产率每年都在减少.因此,21世纪我们面临的严重的危机之一是食物短缺.为了解决严重的食品缺乏问题,除努力生产更多食品外,还应发展快速收割技术、食品加工技术以及包装技术,从而减少浪费并充分利用已产出的农产品.     

Synthesis and antitumour and antiangiogenesis activity of polymers containing methacryloyl‐2‐oxy‐1,2,3‐propane tricarboxylic acid

A new monomer, methacryloyl‐2‐oxy‐1,2,3‐propane tricarboxylic acid (MTCA), was synthesized from citric acid and methacrylic anhydride. Poly(methacryloyl‐2‐oxy‐1,2,3‐propane tricarboxylic acid) and poly(methacryloyl‐2‐oxy‐1,2,3‐propane tricarboxylic acid)‐co‐(maleic anhydride) were prepared by radical polymerizations. Terpoly(methacryloyl‐2‐oxy‐1,2,3‐propane tricarboxylic acid–maleic anhydride–furan) was obtained by in situ terpolymerization of MTCA and exo‐3,6‐epoxy‐1,2,3,6‐tetrahydrophthalic anhydride. The synthesized samples were identified by FTIR, ¹H NMR and ¹³C NMR spectroscopies. The number‐average molecular weights of the fractionated polymers determined by GPC were in the range 14 900–16 600 and polydispersity indices were less than 1.14. The in vitro IC₅₀ values of the monomer and polymers against cancer and normal cell lines were much higher than those of 5‐fluorouracil (5‐FU). The in vivo antitumour activities of the synthesized samples at a dosage of 0.8 mg kg⁻¹ against mice bearing the sarcoma 180 tumour cell line decreased in the order terpoly(MTCA‐MAH‐FUR) > poly(MTCA‐co‐MAH) > poly(MTCA) > MTCA > 5‐FU. The synthesized samples inhibited DNA replication and angiogenetic activity more than did 5‐FU. © 2001 Society of Chemical Industry     

Adsorption and desorption characteristics of CF<Subscript>4</Subscript> on fixed bed column

Adsorption and desorption characteristics of CF₄, which is considered a significant global warming compound, were experimentally investigated. Dynamic behavior of feed gas mixture of CF₄ and N₂ was observed by breakthrough curve. Effects of CF₄ concentrations in the feed gas were investigated, and three pressurization methods were compared. Desorption experiments were carried out using vacuum blowdown and purge. Desorption curves with various N₂ flow rates, feed compositions, and purge time were obtained. The enrichment factor was high for low concentration of CF₄. However, the time required for complete desorption was independent of CF₄ concentration. In the operation of separate vacuum blowdown and purge steps, a short period of vacuum blowdown followed by the purge step was effective.     

Efficiency evaluation of data warehouse operations

We evaluate an efficiency model for data warehouse operations using data from USA and non-USA-based (mostly Korean) organizations. The analysis indicates wide dispersions in operational efficiency, industry and region differences, large differences in labor budgets between efficient and inefficient firms, few organizations efficient in both refresh processing and query production, and difficulty of providing some variables. Follow-up interviews provide insights about the value of efficiency comparisons of information technology organizations and suggestions to improve the model. Using this analysis, we propose a framework containing data warehouse characteristics and firm characteristics to explain IT operational efficiency at the subfirm level.     

The potential micro-hydropower projects in Nakhon Ratchasima province,Thailand

At present, fossil fuel energy is commonly used in developing countries, including Thailand. The tendency to use fossil fuel energy is continuously increasing, and the price of fossil fuels is rising. Thus, renewable energy is of interest. Hydropower is one of the oldest renewable energy forms known and one of the best solutions for providing electricity to rural communities. The present paper aims to determine the potential micro-hydropower sites that could provide more than 50 kW but not over 10 MW in Nakhon Ratchasima Province, Thailand. Both reservoir and run-of-the-river schemes are considered for the assessment of potential micro-hydropower sites. For the reservoir scheme, the discharge in the reservoir is employed for generating micro-hydropower electricity. This installation can be carried out without major modifications to the dam. The run-of-the-river scheme diverts water flow from the river mainstream to the intake via a pressure pipe or an open canal, which is then conveyed to the turbine via a penstock to generate electricity. The results showed that there are 6 suitable projects for the reservoir scheme and 11 suitable projects for the run-of-the-river. The maximum power load was 6000 kW and 320 kW for the reservoir and the run-of-the-river schemes, respectively. Hydropower from the run-of-the-river scheme is more suitable than hydropower from the reservoir scheme because of the many mountains in this province. The designed head for the run-of-the-river scheme is thus generally higher than that for the reservoir scheme. Because stream flow during the dry season is very low, electricity can only be produced in the wet season. This research is a pilot study to determine the potential sites of micro-hydropower projects.     

The Influences of Steeping Duration and Temperature on the α‐ and β‐Amylase Activities of Six Thai Rice Malt Cultivars (Oryza sativa L. Indica)

A preliminary study of malting conditions for six Thai rice cultivars was conducted. Three non‐glutinous rice cultivars (KDML105, PT60, and WR) and three glutinous rice cultivars (SPT, RD6, and KND) were selected. The steeping durations (24, 48, and 72 h) and temperatures (20, 25 and 30°C) were investigated for their effect on α‐ and β‐amylase, the key enzymes for malt quality evaluation. During steeping, the production of both enzymes was lower than at the germination process. The longer the steeping duration, the lower the maximum β‐amylase activity obtained. The contradictory effect was observed for α‐amylase activity, near the end of the germination time. Additionally, temperature influenced the water absorption content as well as the amylolytic enzyme activity. Particularly at 30°C, the maximum β‐amylase activity (6.7 unit/mg protein) was found in KND malt steeped for 24 h, and maximum α‐amylase activity (20 unit/mg protein) was found in PT60 malt steeped for 72 h. The amount of enzyme production depended on the variety rather than the amylose content in the rice. The optimal condition for malting rice regarding β‐amylase activity and α‐amylase activity was analyzed at 30°C, with steeping for 24 h and germination for 4–5 days.