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Kamphaeng Phet, Thailand

Pingaew R.,Srinakharinwirot University | Prachayasittikul S.,Srinakharinwirot University | Ruchirawat S.,Chulabhorn Research Institute | Ruchirawat S.,Chulabhorn Graduate Institute
Molecules | Year: 2010

Thiosemicarbazone analogs of papaveraldine and related compounds 1-6 were synthesized and evaluated for cytotoxic and antimalarial activities. The cytotoxic activity was tested against HuCCA-1, HepG2, A549 and MOLT-3 human cancer cell lines. Thiosemicarbazones 1-5 displayed cytotoxicity toward all the tested cell lines, while compounds 2-5 selectively showed potent activity against the MOLT-3 cell lines. Significantly, N(4)-phenyl-2-benzoylpyridine thiosemicarbazone 4 exhibited the most potent activity against HuCCA-1, HepG2, A549 and MOLT-3 cell lines with IC50 values of 0.03, 4.75, 0.04 and 0.004 μg/mL, respectively. In addition, 2-benzoylpyridine thiosemicarbazones 3 and 4 showed antimalarial activity against Plasmodium falciparum with IC 50 of 10-7 to < 10-6 M. The study demonstrates the quite promising activity of analog 4 as a lead molecule for further development. © 2010 by the authors.

Pornmuttakun D.,Mahidol University | Pornmuttakun D.,Queen Saovabha Memorial Institute | Ratanabanangkoon K.,Chulabhorn Research Institute | Ratanabanangkoon K.,Chulabhorn Graduate Institute
Toxicon | Year: 2014

An in vitro potency assay of antivenom against Malayan pit viper (Calloselasma rhodostoma, CR) has been developed. The assay is based on the neutralizing activity of the antivenom against the coagulant activity of the venom. The minimum coagulant dose (MCD) of CR venom was 22.12 ± 0.25 μg/ml. The coagulation time induced by 2MCD of the venom was used as the control for calculating the neutralizing activity of each batch of antivenom. The in vitro potency of antivenom, expressed as effective dose (ED), was the antivenom/venom ratio at which the coagulation time was increased three fold of that induced by 2MCD of the venom. Eleven batches of the antivenom were assayed for their lethality neutralizing activity (ED50) by the in vivo assay using mice as well as the developed in vitro assay. The correlation coefficient (r) between the in vitro neutralizing activities (ED) and in vivo neutralizing activities (ED50) was 0.957, (p value < 0.001). This simple and rapid in vitro assay of C. rhodostoma antivenom should be a good alternative method for the assessment of antivenom potency during the immunization program and fractionation process. The assay should be adaptable for use with antivenoms against other similar procoagulant venoms. © 2013 Elsevier Ltd. All rights reserved.

Robinson L.N.,Harvard-MIT Division of Health Sciences and Technology | Artpradit C.,Chulabhorn Graduate Institute | Raman R.,Harvard-MIT Division of Health Sciences and Technology | Shriver Z.H.,Harvard-MIT Division of Health Sciences and Technology | And 3 more authors.
Electrophoresis | Year: 2012

Glycans, or complex carbohydrates, are a ubiquitous class of biological molecule which impinge on a variety of physiological processes ranging from signal transduction to tissue development and microbial pathogenesis. In comparison to DNA and proteins, glycans present unique challenges to the study of their structure and function owing to their complex and heterogeneous structures and the dominant role played by multivalency in their sequence-specific biological interactions. Arising from these challenges, there is a need to integrate information from multiple complementary methods to decode structure-function relationships. Focusing on acidic glycans, we describe here key glycomics technologies for characterizing their structural attributes, including linkage, modifications, and topology, as well as for elucidating their role in biological processes. Two cases studies, one involving sialylated branched glycans and the other sulfated glycosaminoglycans, are used to highlight how integration of orthogonal information from diverse datasets enables rapid convergence of glycan characterization for development of robust structure-function relationships. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Athikomkulchai S.,Srinakharinwirot University | Awale S.,University of Toyama | Ruangrungsi N.,Chulalongkorn University | Ruchirawat S.,Chulabhorn Research Institute | And 2 more authors.
Fitoterapia | Year: 2013

Phytochemical investigation on the constituents of Thai propolis led the isolation of a new phenylallylflavanone, (7″S)-8-[1-(4′-hydroxy- 3′-methoxyphenyl)prop-2-en-1-yl]-(2S)-pinocembrin (1) and (E)-cinnamyl-(E)-cinnamylidenate (2) from methanolic extract of Thai propolis. Their structures were determined on the basis of extensive NMR spectroscopic analysis. In addition to this, 19 compounds (3-21) belonging to flavonoids and phenolic esters were isolated and identified. © 2013 Elsevier B.V.

Tummatorn J.,Chulabhorn Research Institute | Ruchirawat S.,Chulabhorn Research Institute | Ruchirawat S.,Chulabhorn Graduate Institute | Ploypradith P.,Chulabhorn Research Institute | Ploypradith P.,Chulabhorn Graduate Institute
Chemistry - A European Journal | Year: 2010

(Figure Presented) Five and six: 3, 4-Cyclopentyl- and cyclohexyl-fused 2-arylchromans could be readily prepared from the intramolecular hetero-Diels-Alder reactions of the corresponding ortho-quinone methide (o-QM) precursors tethered to the styrenes under mild reaction conditions. The products were obtained with good to excellent diastereoselectivity (up to > 99:1 dr; see scheme; MOM = methoxymethyl). © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

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