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1.
Aussara Panya Nunghathai Sawasdee Pucharee Songprakhon Yingmanee Tragoolpua Siriphorn Rotarayanont Kiattawee Choowongkomon Pa-thai Yenchitsomanus 《Viruses》2020,12(11)
Dengue virus (DENV) infection has become a critically important globally prevalent infectious disease, especially in tropical and subtropical countries. Since neither currently exists, there is an urgent need for an effective vaccine to prevent, and a specific drug to treat DENV infection. Therapeutic peptides represent an attractive alternative for development into anti-DENV drugs due to their safety and their diverse biological and chemical properties. We recently reported novel bioactive peptides extracted from the Asian medicinal plant Acacia catechu that efficiently inhibited all four DENV serotypes. In this study, we investigated the anti-DENV activity of a synthetic bioactive peptide derived from this plant. The most effective peptide (designated Pep-RTYM) inhibited DENV infection with a half-maximal inhibition concentration value of 7.9 μM. Time-of-addition study demonstrated that Pep-RTYM interacted with DENV particles and inhibited cellular entry. Pep-RTYM at 50 μM significantly reduced DENV production in Vero-kidney epithelial cells about 1000-fold, but it could decrease the virus production in Huh7 hepatocyte cells approximately 40-fold. Binding of Pep-RTYM to DENV particles may prevent virus interaction with cellular receptor and subsequent virus entry. This finding suggests a potential role of Pep-RTYM in the development of a novel anti-DENV drug. 相似文献
2.
A Peptide Inhibitor Derived from the Conserved Ectodomain Region of DENV Membrane (M) Protein with Activity Against Dengue Virus Infection
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Aussara Panya Nunghathai Sawasdee Mutita Junking Chatchawan Srisawat Kiattawee Choowongkomon Pa‐thai Yenchitsomanus 《Chemical biology & drug design》2015,86(5):1093-1104
Dengue virus (DENV) infection is a public health problem worldwide; thus, the development of a vaccine and anti‐DENV drugs is urgently needed. It has been observed that low levels of viremia in DENV‐infected individuals are associated with mild disease outcomes; therefore, reduction of DENV load should offer therapeutic benefits. Disruption of protein–protein interactions on the surface of DENV by a peptide that mimics part of its structural protein may affect stability of the virion structure and inhibit viral entry into host cells. To test this hypothesis, we generated a novel peptide inhibitor that mimics the conserved ectodomain region of DENV membrane (M) protein, MLH40 peptide, for DENV inhibition assays. MLH40 inhibited all four serotypes of the virus (DENV1–4) at half maximal inhibition concentration of 24–31 μm . MLH40 at 100 μm blocked DENV2 attachment to cells by 80%. The inhibitory activity of MLH40 against DENV was consistently observed with different cell types, including Vero, A549, and Huh7 cells. Prediction of MLH40 binding by a molecular docking program indicated that its N‐terminal loop may interact with DENV envelope (E) proteins and alter their dimer conformation. Thus, MLH40 may serve as a lead‐peptide inhibitor for the development of an anti‐DENV drug. 相似文献
3.
Pattara Sawasdee Chalisa Sabphon Duangporn Sitthiwongwanit Udom Kokpol 《Phytotherapy research : PTR》2009,23(12):1792-1794
The rhizome of Kaempferia parviflora or kra‐chai‐dum (in Thai) is used traditionally as a folk medicine. The preliminary cholinesterase inhibitory screening of this plant extract exhibited significant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Thirteen known methoxyflavones (1–13) were isolated and their structures were completely elucidated based on NMR analysis and compared with literature reports. Minor compounds 12–13 were reported for the first time from this species. The cholinesterase inhibitory test results showed that the highest potential inhibitors toward AChE and BChE were 5,7,4′‐trimethoxyflavone (6) and 5,7‐dimethoxyflavone (7), respectively, with the percentage inhibitory activity varying over 43–85%. The structure‐activity relationship study led to the conclusion that compounds bearing 5,7‐dimethoxy groups and a free substituent at C‐3 had a significant inhibitory effect at a concentration of 0.1 mg/mL, but those bearing a 5‐hydroxyl group reduced the inhibitory potency. On the other hand, flavones bearing a 3′‐ or 5′‐methoxy group did not influence the inhibitory effect. Interestingly, 5,7‐dimethoxyflavone (7) exhibited strong selectivity for BChE over AChE which may be of great interest to modify as a treatment agent for Alzheimer's disease. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
4.
Choochai Nettuwakul Nunghathai Sawasdee Pa-thai Yenchitsomanus 《Clinical biochemistry》2010,43(4-5):497-504
ObjectiveThe objective of this study is to develop and evaluate a high-resolution melting (HRM) method for detection of SLC4A1 mutations and polymorphisms.Design and methodsThe HRM method was optimized for detection of 18 known SLC4A1 variants. It was then used for analysis of 16 blind DNA samples highly enriched with two common mutations, Southeast Asian ovalocytosis (SAO) and band 3 Bangkok 1 (G701D), to compare the results with that of the conventional procedures.ResultsThe HRM method was able to detect all 18 SLC4A1 variants. In the samples in which homozygous wild-type and homozygous variant could not be distinguished by difference plots, they were spiked with a sample carrying known homozygous genotype, resulting in their clear differentiation. The HRM method had 100% efficiency for detection of mutations in the blind DNA samples, when compared with that of the conventional techniques.ConclusionsThe developed HRM method is efficient and reproducible for detection of SLC4A1 mutations and polymorphisms. 相似文献
5.
Cholinesterase (ChE) inhibitory activities of three coumarins (mansorins A–C) and five naphthoquinones (mansonone C, E, G and H) were evaluated to determine the relationships between the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects and the core structures of these compounds. Among the tested compounds, mansonone E exhibited the highest ChE inhibitory activities, with IC50 values in the low micromolar levels. In addition to revealing the ChE inhibitory activities of naphthoquinones for the first time, the results also revealed structure–activity relationship information that could be useful for further modification. Furthermore, the study also supports the hypothesis that mansonones are the active component in Thespesia populnea, a plant that previously has been shown to enhance memory activity in an in vivo study. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
6.
Suchai Sritippayawan Sombat Borvornpadungkitti Atchara Paemanee Chagkrapan Predanon Wattanachai Susaengrat Duangporn Chuawattana Nunghathai Sawasdee Sirintra Nakjang Suttikarn Pongtepaditep Choochai Nettuwakul Nanyawan Rungroj Somkiat Vasuvattakul Prida Malasit Pa-thai Yenchitsomanus 《Urological research》2009,37(3):141-146
Genetic factor may play a role in the pathogenesis of kidney stone that is found in the northeastern (NE) Thai population.
Herein, we report initial evidence suggesting genetic contribution to the disease in this population. We examined 1,034 subjects
including 135 patients with kidney stone, 551 family members, and 348 villagers by radiography of kidney–ureter–bladder (KUB)
and other methods, and also analyzed stones removed by surgical operations. One hundred and sixteen of 551 family members
(21.05%) and 23 of the 348 villagers (6.61%) were affected with kidney stone. The relative risk (λR) of the disease among family members was 3.18. Calcium stones (whewellite, dahllite, and weddellite) were observed in about
88% of stones analyzed. Our data indicate familial aggregation of kidney stone in this population supporting that genetic
factor should play some role in its pathogenesis. Genetic and genomic studies will be conducted to identify the genes associated
with the disease. 相似文献
7.
Flavonoids and stilbenoids with COX-1 and COX-2 inhibitory activity from Dracaena loureiri 总被引:1,自引:0,他引:1
Fom the stem wood of Dracaena loureiri, a new homoisoflavanone named loureiriol (1) and eight known flavonoid and stilbenoid derivatives, including 5,7-dihydroxy-3-(4-hydroxybenzyl)-4-chromanone (2), 4,4'-dihydroxy-2,6-dimethoxydihydrochalcone (3), 2,4'-dihydroxy-4,6-dimethoxydihydrochalcone (4), 4'-hydroxy-2,4,6-trimethoxydihydrochalcone (5), 4,6,4'-trihydroxy-2-methoxydihydrochalcone (6), 4,3',5'-trihydroxystilbene (7), 4,3'-dihydroxy-5'-methoxystilbene (8) and 4-hydroxy-3',5'-dimethoxystilbene (9) were isolated. These compounds were evaluated for their inhibitory activity against the enzymes cyclooxygenase-1 and cyclooxygenase-2. Potent but non-selective activity was found for the stilbenoids 7-9 (IC(50) 1.29 - 4.92 microM) whereas weak or no activity was observed for the flavonoids 1-6. 相似文献
8.
Kangsadalampai S Yenchitsomanus P Chelvanayagam G Sawasdee N Laosombat V Board P 《European journal of haematology》2000,65(4):279-284
The molecular defects of the factor XIII A subunit gene were studied in a patient with factor XIII deficiency. Mutation analysis was performed on amplified DNA from each exon of this gene by single-strand conformation polymorphism (SSCP) and DNA sequencing techniques. A substitution of guanine by adenine at nucleotide 1258 in exon 10 of the coagulation factor XIII A subunit gene has been identified in the patient. The mutation results in the replacement of Gly420 by Ser in the core domain of the enzyme. Restriction enzyme analysis of amplified exon 10 DNA confirmed that the patient was homozygous for this mutation. A family study revealed that the mutation was inherited from both parents, who were first cousins. The potential effects of the mutation were predicted by molecular modeling of the amino acid substitution within the coordinates of the crystal structure. The substitution occurred within the core domain of the enzyme at a residue completely conserved among all known members of the transglutaminase family. The model of the mutant protein suggests that although the substitution of Gly420 by Ser causes only minor readjustment of the residues and does not appear to be particularly deleterious in terms of structure, the mutation is, however, likely to decrease the molecule's ability to undergo the conformational change that is thought to be required for full transglutaminase activity. Our data strongly support the previously published information about the functional significance of the residues surrounding, but not forming, the catalytic pocket in the A subunit of factor XIII. 相似文献
9.
Temkitthawon P Hinds TR Beavo JA Viyoch J Suwanborirux K Pongamornkul W Sawasdee P Ingkaninan K 《Journal of ethnopharmacology》2011,137(3):1437-1441
Aim of the study
A number of medicinal plants are used in traditional medicine to treat erectile dysfunction. Since cyclic nucleotide PDEs inhibitors underlie several current treatments for this condition, we sought to show whether these plants might contain substantial amounts of PDE5 inhibitors.Materials and methods
Forty one plant extracts and eight 7-methoxyflavones from Kaempferia parviflora Wall. ex Baker were screened for PDE5 and PDE6 inhibitory activities using the two-step radioactive assay. The PDE5 and PDE6 were prepared from mice lung and chicken retinas, respectively. All plant extracts were tested at 50 μg/ml whereas the pure compounds were tested at 10 μM.Results
From forty one plant extracts tested, four showed the PDE5 inhibitory effect. The chemical constituents isolated from rhizomes of Kaempferia parviflora were further investigated on inhibitory activity against PDE5 and PDE6. The results showed that 7-methoxyflavones from this plant showed inhibition toward both enzymes. The most potent PDE5 inhibitor was 5,7-dimethoxyflavone (IC50 = 10.64 ± 2.09 μM, selectivity on PDE5 over PDE6 = 3.71). Structure activity relationship showed that the methoxyl group at C-5 position of 7-methoxyflavones was necessary for PDE5 inhibition.Conclusions
Kaempferia parviflora rhizome extract and its 7-methoxyflavone constituents had moderate inhibitory activity against PDE5. This finding provides an explanation for enhancing sexual performance in the traditional use of Kaempferia parviflora. Moreover, 5,7-dimethoxyflavones should make a useful lead compound to further develop clinically efficacious PDE5 inhibitors. 相似文献10.