Browsing by Author "Wandee Sirithana"

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    Molecular Docking Studies and Synthesis of Amino-oxy-diarylquinoline Derivatives as Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors
    (Georg Thieme Verlag, 2019) Arthit Makarasen; Mayuso Kuno; Suwicha Patnin; Nanthawan Reukngam; Panita Khlaychan; Sirinya Deeyohe; Pakamas Intachote; Busakorn Saimanee; Suchada Sengsai; Pornthip Boonsri; Apinya Chaivisuthangkura; Wandee Sirithana; Supanna Techasakul; S. Techasakul; Department of Chemistry, Laboratory of Organic Synthesis, Chulabhorn Research Institute, Laksi, Bangkok, 10210, Thailand; email: supanna@cri.or.th
    In this study, amino-oxy-diarylquinolines were designed using structure-guided molecular hybridization strategy and fusing of the pharmacophore templates of nevirapine (NVP), efavirenz (EFV), etravirine (ETV, TMC125) and rilpivirine (RPV, TMC278). The anti-HIV-1 reverse transcriptase (RT) activity was evaluated using standard ELISA method, and the cytotoxic activity was performed using MTT and XTT assays. The primary bioassay results indicated that 2-amino-4-oxy-diarylquinolines possess moderate inhibitory properties against HIV-1 RT. Molecular docking results showed that 2-amino-4-oxy-diarylquinolines 8(a-d) interacted with the Lys101 and His235 residue though hydrogen bonding and interacted with Tyr318 residue though �-� stacking in HIV-1 RT. Furthermore, 8a and 8d were the most potent anti-HIV agents among the designed and synthesized compounds, and their inhibition rates were 34.0% and 39.7% at 1 _M concentration. Interestingly, 8a was highly cytotoxicity against MOLT-3 (acute lymphoblastic leukemia), with an IC 50 of 4.63�0.62 _g/mL, which was similar with that in EFV and TMC278 (IC 50 7.76�0.37 and 1.57�0.20 _g/ml, respectively). Therefore, these analogs of the synthesized compounds can serve as excellent bases for the development of new anti-HIV-1 agents in the near future. � 2019 Georg Thieme Verlag. All rights reserved.
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    Selection of Potential Bacteria in Termite Nest and Gut for Sustainable Agriculture
    (Walailak University, 2024) Phanukit Kunhachan; Wandee Sirithana; Orapin Komutiban; Vassanasak Limkhuansuwan; Phanchai Menchai; Chanaporn Trakunjae; Thanasak Lomthong; Kriangsak Ruchusatsawat; Srisuda Samaimai; S. Samaimai; Faculty of Science and Technology, Suan Dusit University, Bangkok, 10700, Thailand; email: srisuda_sam@dusit.ac.th
    In this study, bacteria with the best abilities in cellulose degradation, siderophore production, phosphate solubility, and Pythium parasitica inhibition were selected from termite nests and guts. The isolate BTNASP 5-2, BTPK 5-3 and BTNA 5-1 from termite guts exhibited highest in siderophore production index (SPI) (4.16 ± 0.21), phosphate solubilizing index (PSI) (2.10 ± 0.14) and percentage inhibition of radial growth (PIRG) (67.07 ± 4.02 %), respectively. The BGNACMC 4-3 isolated from termite nest gave the highest cellulolytic index (CI) of 5.17 ± 0.24. Bacterial classification was performed using 16s rRNA gene sequencing. The isolates BTPK 5-3, BGNACMC 4-3 and BTNA 5-1 were found closely related to Bacillus cereus, whereas the bacterial isolate BTNASP 5-2 was closely related to Bacillus subtilis. It is also suggested that the Bacillus cereus exhibited a variety of biological activities, denoting the highest cellulase, phosphate-solubilizing and antifungal activities, while Bacillus subtilis produced only a siderophore. The results obtained suggest that the bacteria selected will be used to develop bio-compost to promote plant growth, leading to sustainable farming. © 2024, Walailak University. All rights reserved.
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    Trifluoroacetyl-Containing Scaffolds Assisted in Total Synthesis of Oxostephanine and Thailandine and Their Antimicrobial Activity
    (John Wiley and Sons Inc, 2024) Pongsit Vijitphan; Arthit Makarasen; Apisara Baicharoen; Suwicha Patnin; Nanthawan Reukngam; Panita Khlaychan; Wandee Sirithana; Supanna Techasakul; A. Makarasen; Department of Chemistry, Laboratory of Organic Synthesis, Chulabhorn Research Institute, Bangkok, 10210, Thailand; email: arthit@cri.or.th; S. Techasakul; Department of Chemistry, Laboratory of Organic Synthesis, Chulabhorn Research Institute, Bangkok, 10210, Thailand; email: supanna@cri.or.th
    This study is the first to fully synthesize oxostephanine (1) and thailandine (2), two aporphine alkaloids that were originally found in Stephania venosa (Blume) Spreng. The synthesis described in this study utilized commercially available starting materials, namely 2-bromo-6-methoxybenzaldehyde and 3,4-dihydroxybenzaldehyde. The B-ring moiety of aporphines was successfully synthesized through the utilization of the Bischler-Napieralski cyclization process. The synthesis of the C ring in oxoaporphine was accomplished using an order of crucial steps, namely biaryl coupling, incorporation of trifluoroacetyl-containing scaffolds, and palladium coupling, followed by oxidation using Fremy's salt. The synthesis of oxostephanine (1) and thailandine (2) was successfully achieved in 11 and 12 steps, respectively, resulting in equivalent overall yields of 11.7 %. This study aimed to increase amount of interested compounds and explore the biological activity of those compounds. In this study, both compounds were subjected to testing for antibacterial activity using the CLSI standard M100 guideline. Oxostephanine (1) has shown significant antibacterial efficacy against gram-positive bacteria and bacterial biofilms, as seen by minimum inhibitory concentration (MIC) values ranging from 7.8 to 125 _g/mL. Conversely, higher MIC values of 250 _g/mL indicated that thailandine (2) exhibited limited antimicrobial activity. © 2024 Wiley-VCH GmbH.