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Acharaporn Duangjai Vatcharin Rukachaisirikul Yaowapa Sukpondma Chutima Srimaroeng Chatchai Muanprasat 《Molecules (Basel, Switzerland)》2021,26(18)
Antispasmodic agents are used for modulating gastrointestinal motility. Several compounds isolated from terrestrial plants have antispasmodic properties. This study aimed to explore the inhibitory effect of the pyrrolidine derivative, asperidine B, isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, on spasmodic activity. Isolated rat ileum was set up in an organ bath. The contractile responses of asperidine B (0.3 to 30 µM) on potassium chloride and acetylcholine-induced contractions were recorded. To investigate its antispasmodic mechanism, CaCl2, acetylcholine, Nω-nitro-l-arginine methyl ester (l-NAME), nifedipine, methylene blue and tetraethylammonium chloride (TEA) were tested in the absence or in the presence of asperidine B. Cumulative concentrations of asperidine B reduced the ileal contraction by ~37%. The calcium chloride and acetylcholine-induced ileal contraction was suppressed by asperidine B. The effects of asperidine B combined with nifedipine, atropine or TEA were similar to those treated with nifedipine, atropine or TEA, respectively. In contrast, in the presence of l-NAME and methylene blue, the antispasmodic effect of asperidine B was unaltered. These results suggest that the antispasmodic property of asperidine B is probably due to the blockage of the L-type Ca2+ channel and is associated with K+ channels and muscarinic receptor, possibly by affecting non-selective cation channels and/or releasing intracellular calcium. 相似文献
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Thongsri Oranich Srisuwan Sawitri Thaitalay Paritat Dangwiriyakul Rawee Aengchuan Prasert Chanlek Narong Talabnin Chutima Suksaweang Sanong Rattanachan Sirirat Tubsungnoen 《Journal of Sol-Gel Science and Technology》2021,98(3):441-451
Journal of Sol-Gel Science and Technology - Glass ionomer dental cement (GIC) is commonly used as a restorative material. The sol-gel synthesis of the ionomer glass is an alternative method, which... 相似文献
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Back Cover: Radical Cyclization/ipso‐1,4‐Aryl Migration Cascade: Asymmetric Synthesis of 3,3‐Difluoro‐2‐propanoylbicyclo[3.3.0]octanes (Angew. Chem. Int. Ed. 8/2014) 下载免费PDF全文
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Manat Pohmakotr Chutima Kuhakarn Vichai Reutrakul Darunee Soorukram 《Tetrahedron letters》2017,58(51):4740-4746
Furofurans are one of the largest sub-types of classical lignans which have been found to possess a broad range of important biological activities. Tremendous efforts have been directed to develop synthetic methodologies for the synthesis of furofurans, especially in a stereoselective manner, due to their interesting bioactivities associated with the structural and stereochemical complexity. This article summarizes the reports on asymmetric synthesis of furofurans disclosed during the period of 2004–2017. 相似文献
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Tipthida Pasachan Acharaporn Duangjai Atcharaporn Ontawong Doungporn Amornlerdpison Metee Jinakote Manussabhorn Phatsara Sunhapas Soodvilai Chutima Srimaroeng 《Molecules (Basel, Switzerland)》2021,26(5)
This study investigated the effects of Tiliacora triandra (Colebr.) Diels aqueous extract (TTE) on hepatic glucose production in hepatocellular carcinoma (HepG2) cells and type 2 diabetic (T2DM) conditions. HepG2 cells were pretreated with TTE and its major constituents found in TTE, epicatechin (EC) and quercetin (QC). The hepatic glucose production was determined. The in vitro data were confirmed in T2DM rats, which were supplemented daily with 1000 mg/kg body weight (BW) TTE, 30 mg/kg BW metformin or TTE combined with metformin for 12 weeks. Results demonstrate that TTE induced copper-zinc superoxide dismutase, glutathione peroxidase and catalase genes, similarly to EC and QC. TTE decreased hepatic glucose production by downregulating phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) and increasing protein kinase B and AMP-activated protein kinase phosphorylation in HepG2 cells. These results correlated with the antihyperglycemic, antitriglyceridemic, anti-insulin resistance, and antioxidant activities of TTE in T2DM rats, similar to the metformin and combination treatments. Consistently, impairment of hepatic gluconeogenesis in T2DM rats was restored after single and combined treatments by reducing PEPCK and G6Pase genes. Collectively, TTE could potentially be developed as a nutraceutical product to prevent glucose overproduction in patients with obesity, insulin resistance, and diabetes who are being treated with antidiabetic drugs. 相似文献
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Thitinan Aiebchun Panupong Mahalapbutr Atima Auepattanapong Onnicha Khaikate Supaphorn Seetaha Lueacha Tabtimmai Chutima Kuhakarn Kiattawee Choowongkomon Thanyada Rungrotmongkol 《Molecules (Basel, Switzerland)》2021,26(8)
Epidermal growth factor receptor (EGFR), overexpressed in many types of cancer, has been proved as a high potential target for targeted cancer therapy due to its role in regulating proliferation and survival of cancer cells. In the present study, a series of designed vinyl sulfone derivatives was screened against EGFR tyrosine kinase (EGFR-TK) using in silico and in vitro studies. The molecular docking results suggested that, among 78 vinyl sulfones, there were eight compounds that could interact well with the EGFR-TK at the ATP-binding site. Afterwards, these screened compounds were tested for the inhibitory activity towards EGFR-TK using ADP-Glo™ kinase assay, and we found that only VF16 compound exhibited promising inhibitory activity against EGFR-TK with the IC50 value of 7.85 ± 0.88 nM. In addition, VF16 showed a high cytotoxicity with IC50 values of 33.52 ± 2.57, 54.63 ± 0.09, and 30.38 ± 1.37 µM against the A431, A549, and H1975 cancer cell lines, respectively. From 500-ns MD simulation, the structural stability of VF16 in complex with EGFR-TK was quite stable, suggesting that this compound could be a novel small molecule inhibitor targeting EGFR-TK. 相似文献
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Manat Pohmakotr Supakeat Kambutong Patoomratana Tuchinda Chutima Kuhakarn 《Tetrahedron》2008,64(27):6315-6323
The synthetic utility of the intramolecular acylation of α-sulfinyl carbanions as an efficient and general synthetic approach for the preparation of (−)-pentenomycin I (1) and (−)-epipentenomycin I (5) and their enantiomers (ent-1 and ent-5), starting from chiral (2S,5S,6S)-ester 6 and ent-6, respectively, has been demonstrated. Easy accesses to pentenomycin analogs have also been demonstrated through the Pummerer, Suzuki-Miyaura, and Sonogashira reactions. 相似文献
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A new variation of the Pictet-Spengler reaction for the synthesis of 1-substituted tetrahydroisoquinoline derivatives has been developed. The reaction employs the reduction of N-acylcarbamates by DIBAL-H followed by simultaneous cyclization mediated by BF3·OEt2. The synthetic potential of this method has been illustrated by the synthesis of the tetrahydroisoquinoline alkaloids, (±)-xylopinine, (±)-laudanosine, (±)-8-oxo-O-methylbharatamine, and (±)-isoindoloisoquinolone. 相似文献