Director: Associate Professor Dr. Supanna Techasakul
The emergence or re-emergence of both infectious and non-communicable diseases has signified the importance and power of organic synthesis for the discovery and development of drug-like candidates towards novel efficacious drugs of future. Microbial infections as well as morbidities such as hypertension, diabetes, cancer, and Alzheimer’s have been associated as the cause of mortality, especially in the elderly. In 2020, while over 19 million new cases of cancer have been reported, more than 400 million people are living with diabetes worldwide. In addition, it has been estimated that more than 150 million people have been affected by Alzheimer’s and a new case of dementia occurs every 3.2 seconds.
These have become major public health issues as Thailand rely virtually solely on importing all active pharmaceutical ingredients (APIs) of small molecule drugs, thereby rendering the health crisis not only non-cost effective but also prone to be uncontrollable. Thus, establishing a viable program in drug discovery and development is an important element to ensure the drug security of our country. In addition, developing new prototypes for medical device using synthetic polymers is also a key to address medical needs for some treatments.
Our laboratory has established an integrative approach to practically bring bench-top discoveries to bed-side cares; this can be classified into three main areas:
Over the years, through the integrative approach as well as collaborations both nationally and internationally with universities and research institutions, our laboratory has exemplified how to best translate knowledge from basic research into pragmatic development for research utilization. As a consequence, patents ranging from potent novel anti-HIV agents to innovative medical devices have been successfully filed.These patents not only reflect successful research translation from laboratory discoveries to industry but also represent important intellectual properties for future profitable commercialization.
Previous Next Our laboratory has emphasized on the importance of research utilization in the areas of polymer sciences for medical devices and standardized preparation of Kratom extracts as well as essential oils, with an ultimate aim for their applications in the industry. Standardized herbal extracts and essential oils such as those from mangosteen peels, galanga, betel vine, white turmeric, and white ginger have been developed on a lab/pre-pilot scale. Double-layered wound dressing from biopolymer mixed with Thai herbal extracts has been formulated. The first layer of bacterial cellulose raised with coconut juice provides not only moisture during the healing process, thereby reducing irritation upon peeling it off, but also matrix to absorb exudates from the wound. The second layer consists of polylactic acid nanofiber prepared via electrospinning process; it also contains antioxidants from rice extracts and antibacterial essential oils from Crofton weed. This wound dressing also exhibits good safety profile toward human skin as both rice extracts and essential oils are non-cytotoxic against human dermal fibroblasts and human keratinocytes. The development has relied on local materials, thereby reducing the costs of imports and strengthening the local industry in wound dressing to effectively cater to the patients’ needs. The eggshell-derived hydroxyapatite-incorporated fibroin-alginate composite injectable hydrogel has been fabricated as scaffold for bone...
Compounds of natural/semi-synthetic/fully synthetic origins have been screened for their biological activities including but not limited to cytotoxicity with an emphasis against a panel of cancer cell lines, antimicrobial, anti-inflammatory, and antiviral activities. More importantly, advanced techniques in computational chemistry such as molecular docking have been employed to gain insights and understanding of interactions between the biomolecular target(s) and the small molecule drug compounds which could lead to designing more efficacious drug-like candidates with fewer adverse side effects. Moreover, in order to ascertain new candidates with safer drug-like profiles, toxicity against relevant normal cell types has been determined. The ratios of efficacy over general toxicity, namely therapeutic indices (TI) or selectivity indices (SI), are also derived. These values are pivotal for candidate selection since a number of potential drug-like compounds may not advance to further stages including clinical trials because of the inherent general toxicity. Therefore, evaluating both efficacy and toxicity is important in advancing drug candidates through successful drug discovery process.
Previous Next The typical first stage of rational drug design involves the search for molecular templates from which more desirable candidates can be accessed via direct structural modifications orde novosynthesis. On the basis of herbal or folk medicines worldwide, natural products, with their unimaginably complex novel skeletons, have served as both concrete entities and inspiration to learn from as well as to design the better analogs with an aid of modern computational chemistry techniques. Various clinically used herbal remedies with their known bioactive components have been our focus to establish the fully integrated approach for herbs, featuring the development of simplified and efficient isolation processes suitable for industrial applications. Advanced technologies and instrumentation have enabled the quantitative determination of the natural abundance of major bioactive compounds and the preparation of compound standards for commercialization. In addition, our laboratory has also employed some of these naturally occurring compounds as starting materials for direct derivatizations. As an example, mitragynine, the major alkaloid component inMitragyna speciosa, locally known as Kratom, has been obtained through this approach and employed to prepare the bioactive metabolite, 7-hydroxymitragynine, along with other semi-synthetic analogs. As a crucial alternative to access bioactive natural compounds with low natural abundance, simplified and efficient synthetic methods have also been devised for heterocycles frequently encountered as pharmacophores. Structural...
Name : Mister Pongsit Vijitphan (Research Scientist) Office Address : Room : R303A Laboratory of Organic Synthesis 54 Kamphaeng Phet 6 Talat Bang Khen, Lak Si, Bangkok 10210, Thailand Tel : +66 2553 8555 (ext. 3017) Email : pongsit@cri.or.th Research Interests Synthesis of heterocyclic compounds Total synthesis of natural products Isolation of natural prodcuts Education 2016 – 2019 M.Sc. Chemistry, Faculty of Science, Prince of Songkhla University, Thailand 2012 – 2016 B.Sc. Chemistry, Faculty of Science, Prince of Songkhla University, Thailand Work Experiences 2020 – present Research Scientist, Chulabhorn Research Institute, Thailand Publications Selected Publications Vijitphan, P.; Makarasen, A.; Patnin, S.; Baicharoen, A.; Techasakul, S. In Vitro Cytotoxic Activity, Molecular Docking Study, and Chemical Composition of Zingiber cassumunar root oil. ScienceAsia 2022, 48, 596-604. Patnin, S; Makarasen, A.; Kuno, M.; S. Techasakul; Vijitphan, P.; Baicharoen, A. Computational Screening of Phenylamino-phenoxy-quinoline Derivatives against the Main Protease of SARS-COV-2 Using Molecular Docking and the ONIOM Method. Molecules 2022, 27, 1793. Makarasen, A.; Patnin, S.; Vijitphan, P.; Reukngam, N.; Khlaychan, P.; Techasakul, S. Structural Basis of 2-Phenylamino-4-phenoxyquinoline Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. Molecules 2022, 27, 461. Other Publications Vijitphan, P.; Rukachaisirikul, V,; Muanprasat, C.; Iawsipo, P.; Panprasert, J.; Tadpetch, K. Unified Synthesis and Cytotoxic Activity of 8-O-Methylfusarubin and its Analogues. Org. Biomol. Chem. 2019, 17, 7078–7087.
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