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    Synthesis and cytotoxicity study of gold(III) porphyrin complexes and their derivative in breast cancer cells
    (2021-12-01)
    Phromsatit, Tossapon
    ;
    Arpornmaeklong, Premjit
    ;
    Shirosaki, Yuki
    ;
    Teerawatananond, Thapong
    ;
    Rabablert, Jundee
    Gold(III) [Au(III)] complexes exhibit potential anticancer activities. A series of Au(III) porphyrin complexes containing different meso-substituent groups (phenyl, methoxyphenyl, butyloxyphenyl, octyloxyphenyl, and decyloxyphenyl) was synthesized. The synthesized compounds were characterized using mass spectrometry, infrared spectroscopy, UV–visible and fluorescence spectroscopy, and electron paramagnetic resonance spectroscopy. Moreover, the in vitro cytotoxicity of these Au(III) porphyrin complexes was investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide surrogate viability assay on an MCF7 human breast cancer cell line. The Au(III) complexes with 5,10,15,20-tetraphenylporphyrin (AuTPP) and 5,10,15,20-tetrakis(4-methyloxyphenyl)porphyrin (AuTOMPP) demonstrated high anticancer activity with IC<inf>50</inf> values against MCF7 cells at 4.30 and 25.35 µM, respectively. The toxicity of the Au(III) porphyrin complexes against the LLC-MK2 rhesus monkey kidney epithelial cell line, a representative normal cell line, was investigated. All the tested Au(III) porphyrin complexes were non-cytotoxic in LLC-MK2 cells. For AuTPP, more than 80% LLC-MK2 cell viability was observed at concentrations lower than 5 μM.
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    Biodiversity and bioactivity of stromatic xylariales collected from Mu Ko Chang National Park, Thailand
    (2020-01-01)
    Sutjaritvorakul, T.
    ;
    Chutipaijit, S.
    Ko Chang Island is a tropical rain forest island of Mu Ko Chang national park, Thailand, which has a wide variety of macro-fungi. The objective of this research was to study the biodiversity of Xylariales and to investigate the bioactive activity of ethyl acetate crude extracts. The fungi were collected from the forest area of the waterfalls all over the island. The crude extracts of selected fungi were tested for antibacterial activity by agar well diffusion method and the cancer cell viability was assessed using the MTT assay. Three genera of Xylariaceae and Hypoxylaceae were found including Xylaria, Daldinia and Hypoxylon. The crude extracts inhibited the growth of Gram positive bacteria more than that of Gram negative bacteria and showed broad spectrum inhibition to all cancer cell lines. The crude extract of Xylaria sp.3 showed the highest potential of antibacterial activity and selectively inhibited gastric carcinoma (Kato III) and T cell leukemia (Jurket) with the percentage survival of 26.12 ± 0.90% and 35.37 ± 0.40% respectively. The molecular identification of Xylaria sp.3 was identified as Xylaria sp.TP5BS101. These results show that these macromycetes are an excellent repertoire of antibacterial activity and exhibit anticancer activity against Kato III and Jurket by inducing DNA fragmentation.
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    Bioactive compounds from Mesua ferrea stems
    (2015-01-01)
    Keawsa-Ard, Sukanya
    ;
    Liawruangrath, Boonsom
    ;
    Kongtaweelert, Samart
    The chemical constituents and biological activities of Mesua ferrea Linn. were studied. The stems of M. ferrea were extracted with hexane, dichloromethane and methanol, respectively. The methanol extract exhibited the highest antibacterial activity against Escherichia coli with the MIC value of 31.25 μg/mL. The methanol extract and the dichloromethane extract exhibited the highest activity against Staphylococcus aureus with the MIC values of 31.25 μg/mL. The dichloromethane extract exhibited anticancer activities against KB-oral, MCF-7 and NCI-H187 cell lines with the IC<inf>50</inf>values of 18.01, 28.83 and 18.42 μg/mL, respectively. Friedelin, the mixture of α-amyrin and β-amyrin, lupeol and β-sitosterol were isolated from the active dichloromethane extract of the stems. Friedelin, the mixture of α-amyrin and β-amyrin, lupeol and β-sitosterol showed the antibacterial activity against E. coli with the MIC values of 250, 250, 250 and 1000 μg/mL, respectively. They also showed antibacterial activity against S. aureus with the MIC values of 250, 250, 500 and 1000 μg/mL, respectively. The mixture of α-amyrin and β-amyrin exhibited anticancer activity against MCF-7 cell line with the IC<inf>50</inf>value 28.45 μg/mL and lupeol exhibited anticancer activities against KB, MCF-7 and NCI-H187 cell lines with the IC<inf>50</inf>values of 30.12, 34.25 and 21.56 μg/mL, respectively. All the extracts and the isolated compounds were non-cytotoxic to Vero cells.
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    Anticancer and antibacterial activities of the isolated compounds from Solanum spirale Roxb. leaves
    (2012-01-01)
    Keawsa-Ard, Sukanya
    ;
    Natakankitkul, Surapol
    ;
    Liawruangrath, Saisunee
    ;
    Teerawutgulrag, Aphiwat
    ;
    Trisuwan, Kongkiat
    The isolations of active anticancer compounds from Solanum spirale Roxb., collected from Phayao Province, Thailand are rarely reported. The anticancer activities of hexane and methanol extracts of the leaves were investigated. The chloroform extract possessed anticancer activities against KB-Oral cavity cancer, MCF-7 breast cancer cell and NCI-H187-Small cell lung cancer with the IC<inf>50</inf> values of 42.73, 17.90, and 36.74 μg/ mL, respectively. But the hexane extract did not inhibit significant anticancer activity against three cancer cell lines. Lupeol, protocatechuic acid and trans-cinnamic acid have been isolated from the chloroform extract of this medicinal plants. Their structures were characterized on the basis of spectroscopic analysis. The anticancer activities of the isolated compounds were also evaluated in vitro against three cancer cell lines. Only lupeol compound inhibited significant anticancer activity against KB-Oral cavity cancer with the IC<inf>50-</inf> value of 26.73 μg/mL, whereas protocatechuic acid and trans-cinnamic acid did not exhibit anticancer activity. The hexane, chloroform extracts and the isolated compounds did not show cytotoxic activity against the African green monkey kidney cell line. The hexane and chloroform extracts also inhibited antibacterial activity against Escherichia coli and Staphylococcus aureus with the MIC values were in the range between 375-1500 μg/mL. All isolated compounds showed equal antibacterial activity against E. coli with the MIC of 250 μg/mL, and trans-cinnamic acid showed better antibacterial activity against S. aureus with the MIC of 250 μg/mL than lupeol and protocatechuic acid. This is the first report decribes the isolation and structure elucidation of lupeol, protocatechuic acid and trans-cinnamic acid together with their anticancer, cytotoxic and antibacterial activities from this medicinal plant.
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    Antioxidant, antibacterial, anticancer activities and chemical constituents of the essential oil from Mesua ferrea leaves
    (2012-01-01)
    Keawsa-Ard, Sukanya
    ;
    Kongtaweelert, Samart
    Essential oil from leaves of Mesua ferrea L. was isolated by hydrodistillation and analyzed by means of GC and GC-MS. The yield of obtained essential oil was at 0.064% and it was appearred as yellow liquid. Thirty-five constituents were identified, constituting 81.4% of the total volatile components. The major constituents were trans-caryophyllene (30.9%), β-caryophyllene oxide (17.9%), α-humulene (6.0%), δ-cadinene (4.1%), γ-muurolene (3.5%), γ-cadinene (2.3%), β-selinene (1.9%), germacrene D (1.8%) and β-bisabolene (1.6%). Antioxidant activity of the essential oi l was evaluated by using the DPPH (1,1-diphenyl-2-picrylhydrazyl) radicals scavenging assay. The essential oil showed antioxidant activity with the IC<inf>50</inf> of 31.67 mg/mL. In addition, the essential oil exhibited significant antibacterial activity against Escherichia coli and Staphylococcus aureus with the MIC values of 250 and 125 mg/mL, respectively. This oil also exhibited anticancer activities against KB, MCF-7 and NCI-H187 cell lines with the IC<inf>50</inf> values of 24.02, 16.19, and 20.32 μg/mL, respectively, but it was non-cytotoxic to Vero cell line.