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Yan-Chao Yin, Xiao-Dong Zhang, Zhi-Qiang Gao, Ting Hu, Ying Liu
Chalcone isomerase (CHI) is the second rate-limiting and the first reported enzyme involved in the biosynthetic pathway of flavonoids. It catalyzes the intramolecular cyclization reaction, converting the bicyclic chalcone into tricyclic (2S)-flavanone. In this paper, we obtained and analyzed 916 DNA sequences, 1310 mRNA sequences, and 2403 amino acid sequences of CHI registered in NCBI by Jan 2018. The full length of CHI DNA sequences ranges from 218 to 3758 bp, CHI mRNA sequences ranges from 265 to 1436 bp, and CHI amino acid sequences ranges from 35 to 465 amino acid residues...
October 15, 2018: Molecular Biotechnology
Roqia Bashary, Gopal L Khatik
Diabetes is the most prevalent metabolic disorder causing a high rate of mortality and morbidity. Recently alpha-amylase is reported to be good drug design target for the treatment of diabetes mellitus. We have designed 116 molecules based on aza-Michael adduct of trans-chalcone as 1,3 diaryl-3-(arylamino)propan-1-ones which were studied by molecular docking and among them best six derivatives were synthesized easily via aza-Michael addition on trans-chalcone using KOH as a catalyst and evaluated for alpha-amylase inhibition along with antioxidant activity...
October 9, 2018: Bioorganic Chemistry
Hao Jin, Hak Sung Kim, Geom Seog Seo, Sung Hee Lee
Chalcone (1,3-diphenyl-2-propen-1-one) derivatives exert anti-cancer activity by targeting key molecules that can lead to carcinogenesis. We synthesized the chalcone derivative 3-phenyl-1-(2,4,6-tris(methoxymethoxy)phenyl)prop-2-yn-1-one (KB-34) and previously reported its anti-inflammatory activity in macrophages. In this study, we examined the anti-metastatic activity of KB-34 against human colorectal cancer (CRC) cells and elucidated its underlying molecular mechanisms. KB-34 treatment significantly inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced migration, as well as the invasion and proliferation of CRC cells (HT-29 and SW620)...
October 12, 2018: European Journal of Pharmacology
Dian Alwani Zainuri, Ibrahim Abdul Razak, Suhana Arshad
The crystal structures of ( E )-1-(anthracen-9-yl)-3-(3 H -indol-2-yl)prop-2-en-1-one, C25 H17 NO, and ( E )-1-(anthracen-9-yl)-3-[4-(di-methyl-amino)-naphthalen-1-yl]prop-2-en-1-one, C29 H23 NO, are reported. In each case the anthracene ring system and pendant ring system are almost perpendicular to each other [dihedral angles = 75.57 (7)° and 70.26 (10)°, respectively]. In the extended structures, weak N-H⋯O, C-H⋯O and C-H⋯π inter-actions influence the centrosymmetric crystal packing. Density functional theory calculations were carried out using a 6-311 G++(d,p) basis set and the calculated structures are in good agreement with the crystal structures...
October 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
N R Sreenatha, B N Lakshminarayana, D P Ganesha, C R Gnanendra
The title chalcone derivative, C14 H10 Cl2 O3 , is almost planar, with a dihedral angle of 7.0 (2) ° between the 3,5-di-chloro-2-hy-droxy-phenyl and 5-methyl-furan rings. There is an intra-molecular O-H⋯O hydrogen bond present forming an S (6) ring motif. In the crystal, mol-ecules are linked by bifurcated C-H/H⋯O hydrogen bonds, enclosing an R 1 2 (6) ring motif, forming a 21 helix propagating along the b -axis direction. The inter-molecular inter-actions were qu-anti-fied using Hirshfeld surface analysis...
October 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
Dian Alwani Zainuri, Ibrahim Abdul Razak, Suhana Arshad
The structures of two new anthracenyl chalcones, namely ( E )-1-(anthracen-9-yl)-3-(4-nitro-phen-yl)prop-2-en-1-one, C23 H15 NO3 , and ( E )-1-(anthracen-9-yl)-3-(4-iodo-phen-yl)prop-2-en-1-one, C23 H15 IO are reported. A structural comparative study between the two chalcones was performed and some effects on the geometrical parameters, such as planarity and dihedral angles, are described. The mol-ecular geometry was determined by single-crystal X-ray diffraction, and density functional theory (DFT) at B3LYP with the 6-311++G(d,p) basis set was applied to optimize the ground-state geometry...
October 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
Aaditi B Deshmukh, Sagar S Datir, Yogesh Bhonde, Natasha Kelkar, Pawan Samdani, Vaijayanti A Tamhane
Oroxylum indicum (L.) Kurz is a medicinally important and rare tree species of the family Bignoniaceae. It is rich in flavonoid content and its mature roots are extensively used in Ayurvedic formulations. O. indicum specific flavonoids like oroxylin B, prunetin and oroxindin possess antibacterial, antiproliferative, antioxidant and anticancerous properties, signifying its importance in modern medicine. In the present study, de novo transcriptome analysis of O. indicum root was performed to elucidate the genes involved in flavonoid metabolism...
October 11, 2018: Phytochemistry
Lívia C Silva, Bruno J Neves, Marcelo N Gomes, Cleber C Melo-Filho, Célia Ma Soares, Carolina H Andrade, Maristela Pereira
AIM: The shape-based virtual screening was used for the identification of new compounds anti-paracoccidioidomycosis (PCM). MATERIALS & METHODS: The study was performed according to the following steps: collection and curation of a dataset of quinolinyl N-oxide chalcones with anti-PCM activity, development and validation of shape-based models, application of the best model for virtual screening, and experimental validation. RESULTS & CONCLUSION: Among 31 computational hits, eight compounds showed potent antifungal activity and low cytotoxicity for mammalian cells...
October 12, 2018: Future Microbiology
Adrian P Mansini, Estanislao Peixoto, Sujeong Jin, Seth Richard, Sergio A Gradilone
Cholangiocytes, the epithelial cells lining the biliary tree in the liver, express primary cilia that can detect several kinds of environmental signals and then transmit this information into the cell. We have previously reported that cilia are significantly reduced in cholangiocarcinoma (CCA) and that the experimental deciliation of normal cells induces a malignant-like phenotype with increased proliferation, anchorage independent growth, invasion and migration. Here, we tested the hypothesis that the chemosensory function of cholangiocyte primary cilia acts as a mechanism for tumor suppression...
October 9, 2018: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
Adnan Ashraf, Syeda Abida Ejaz, Shafiq Ur Rahman, Waseeq Ahmad Siddiqui, Muhammad Nadeem Arshad, Joanna Lecka, Jean Sévigny, Mohie E Moustafa Zayed, Abdullah M Asiri, Jamshed Iqbal, Christian G Hartinger, Muhammad Hanif
Chalcones and 1,2-benzothiazines are two important classes of bioactive compounds, each scaffold endowed with diverse pharmacological activities. Combining both of these pharmacophores in a single molecule was aimed to yield multi-modal agents. Herein, we report a series of hybrid compounds 3a-3o derived from chalcones and 1,2-benzothiazine cores. They were synthesized from commercially available sodium saccharin, and the resulting 1,2-benzothiazine-derived ketone was then condensed with aromatic aldehydes in an aldol condensation to obtain the respective chalcones...
November 5, 2018: European Journal of Medicinal Chemistry
Yunsheng Xue, Yunping Liu, Qingquan Luo, Han Wang, Ran Chen, Yin Liu, Ya Li
In view of their multifunctional features of coumarins and chalcones, coumarin-chalcone hybrids have attracted much attention in recent years. Herein, the free radical scavenging activities of a series of coumarin-chalcone hybrids were investigated using the density functional theory (DFT) method. Three main reaction mechanisms were explored: hydrogen atom transfer (HAT), electron transfer followed by proton transfer (SET-PT) and sequential proton loss electron transfer (SPLET). Thermodynamic descriptors associated with these mechanisms were calculated in gas phase and solvents...
October 8, 2018: Journal of Physical Chemistry. A
Geoffrey Liou, Ying-Chih Chiang, Yi Wang, Jing-Ke Weng
Flavonoids are important polyphenolic natural products, ubiquitous in land plants, that play diverse functions in plants' survival in their ecological niches, including UV protection, pigmentation for attracting pollinators, symbiotic nitrogen fixation, and defense against herbivores. Chalcone synthase (CHS) catalyzes the first committed step in plant flavonoid biosynthesis and is highly conserved in all land plants. In several previously reported crystal structures of CHSs from flowering plants, the catalytic cysteine is oxidized to sulfinic acid, indicating enhanced nucleophilicity in this residue associated with its increased susceptibility to oxidation...
October 5, 2018: Journal of Biological Chemistry
Md Zakir Hossain, Yasuhiro Ishiga, Naoki Yamanaka, Eri Ogiso-Tanaka, Yuichi Yamaoka
Asian soybean rust (ASR), caused by the obligate biotrophic fungus Phakopsora pachyrhizi, is responsible for severe yield losses of up to 90% in all soybean producing countries. Till today, eight resistance to Phakopsora pachyrhizi (Rpp) loci have been mapped in soybean. Their resistance mechanism is race specific but largely unknown. The transcriptomes of susceptible BRS184 and Rpp3 with ASR isolates T1-2 at 24 h after inoculation (hai) and without ASR inoculation (mock) were annotated by similarity searching with different databases...
September 23, 2018: Plant Physiology and Biochemistry: PPB
Sonia Rocha, Daniela Ribeiro, Eduarda Fernandes, Marisa Freitas
The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse side effects. Thus, entirely new interventions, addressing the underlying etiopathogenesis of type 2 diabetes mellitus, are required. Chalcones, secondary metabolites of terrestrial plants and precursors of the flavonoids biosynthesis, have been used for a long time in the traditional medicine due to their wide-range of biological activities, from which the anti-diabetic activity stands out...
October 1, 2018: Current Medicinal Chemistry
Vinícius R D Pereira, Ismael J Alves Junior, Lígia S da Silveira, Reinaldo B Geraldo, Priscila de F Pinto, Fernanda S Teixeira, Maria C Salvadori, Marcos P Silva, Lara A Alves, Priscila V S Z Capriles, Ayla das C Almeida, Elaine S Coimbra, Pedro L S Pinto, Mara R C Couri, Josué de Moraes, Ademar Alves Da Silva Filho
In this study, we evaluated the in vitro and in vivo schistosomicidal activities of chalcones against Schistosoma mansoni worms. In vitro assays revealed that chalcones 1 and 3 were the most active compounds, without affecting significantly mammalian cells. Confocal laser scanning microscopy and scanning electron microscopy studies revealed reduction on the numbers of tubercles and morphological alterations in the tegument of S. mansoni worms after in vitro incubation with chalcones 1 and 3. In a mouse model of schistosomiasis, the oral treatment (400 mg/kg) with chalcone 1 or 3 significantly caused a total worm burden reduction in mice...
October 1, 2018: Chemistry & Biodiversity
Neha Pandey, Niraj Goswami, Deepika Tripathi, Krishna Kumar Rai, Sanjay Kumar Rai, Shilpi Singh, Shashi Pandey-Rai
UV-B-induced flavonoid biosynthesis is epigenetically regulated by site-specific demethylation of AaMYB1, AaMYC, and AaWRKY TF-binding sites in AaPAL1 promoter-causing overexpression of AaPAL gene in Artemisia annua. The present study was undertaken to understand the epigenetic regulation of flavonoid biosynthesis under the influence of ultraviolet-B radiation using Artemisia annua L. as an experimental model. In-vitro propagated and acclimatized plantlets were treated with UV-B radiation (2.8 W m-2 ; 3 h), which resulted in enhanced accumulation of total flavonoid and phenolics content as well as eleven individual flavonoids measured through HPLC-DAC...
September 28, 2018: Planta
Yuanfeng Zhou, Ming Li, Xinyou Yu, Ting Liu, Tian Li, Li Zhou, Wenbin Liu, Wei Li, Feng Gao
Aurora B is aberrantly expressed in various tumors and shown to be a promising target for cancer therapy. Butein, a chalcone isolated from Rhus cerniciflua, has demonstrated antitumor activities in different cancers. In this study, we aimed to validate whether Aurora B kinase was the direct target of butein to exhibit its potency in hepatocellular carcinoma (HCC). Comparing with the normal cell line and tissue, Aurora B was overexpressed in all tested HCC cells and the majority of tumor tissue. Knocking down of Aurora B with shRNA substantially inhibited HCC cell proliferation, colony formation and delayed tumor growth in nude mice...
2018: International Journal of Biological Sciences
Jonathan I Watkinson, Peter A Bowerman, Kevin C Crosby, Sherry B Hildreth, Richard F Helm, Brenda S J Winkel
Plant flavonoid metabolism has served as a platform for understanding a range of fundamental biological phenomena, including providing some of the early insights into the subcellular organization of metabolism. Evidence assembled over the past three decades points to the organization of the component enzymes as a membrane-associated complex centered on the entry-point enzyme, chalcone synthase (CHS), with flux into branch pathways controlled by competitive protein interactions. Flavonoid enzymes have also been found in the nucleus in a variety of plant species, raising the possibility of alternative, or moonlighting functions for these proteins in this compartment...
2018: PeerJ
Yidan Zhang, Yoav S Zvi, Brian Batko, Nikolas Zaphiros, Edmond F O'Donnell, Jichuan Wang, Kenji Sato, Rui Yang, David S Geller, Pratistha Koirala, Wendong Zhang, Xiuquan Du, Sajida Piperdi, Yang Liu, Deyou Zheng, Michael Roth, Jonathan Gill, Jinghang Zhang, Tingting Ren, Richard Gorlick, Xiaolin Zi, Bang H Hoang
Osteosarcoma (OS), the most common primary cancer of bone, exhibits a high propensity for local invasion and distant metastasis. This study sought to elucidate the role of S phase kinase-associated protein (Skp2) in osteosarcoma invasion and metastasis and to explore flavokawain A (FKA), a natural chalcone from kava extract, as a potential Skp2 targeting agent for preventing osteosarcoma progression. Skp2 was found to be overexpressed in multiple osteosarcoma cell lines, including 5 standard and 8 primary patient-derived cell lines...
September 24, 2018: Scientific Reports
Elizabeth Varghese, Samson Mathews Samuel, Mariam Abotaleb, Sohaila Cheema, Ravinder Mamtani, Dietrich Büsselberg
Among the different types of breast cancers, triple-negative breast cancers (TNBCs) are highly aggressive, do not respond to conventional hormonal/human epidermal growth factor receptor 2 (HER2)-targeted interventions due to the lack of the respective receptor targets, have chances of early recurrence, metastasize, tend to be more invasive in nature, and develop drug resistance. The global burden of TNBCs is increasing regardless of the number of cytotoxic drugs being introduced into the market each year as they have only moderate efficacy and/or unforeseen side effects...
September 21, 2018: Cancers
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