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Márcia Rodrigues Trein, Lígia Rodrigues E Oliveira, Graziela Vargas Rigo, Mayara Aparecida Rocha Garcia, Brenda Petro-Silveira, Danielle da Silva Trentin, Alexandre José Macedo, Luis Octávio Regasini, Tiana Tasca
Trichomoniasis is the most common non-viral sexually transmitted disease worldwide and can lead to serious consequences in reproductive health, cancer, and HIV acquisition. The current approved treatment present adverse effects and drug resistance data on this neglected parasitic infection is underestimated. Chalcones are a family of molecules that present biological applications, such as activity against many pathogenic organisms including protozoan pathogens. Chalcone (1) and three amino-analogues (2-4) were synthesized by Claisen-Schmidt condensation reaction and had their activity evaluated against the parasitic protozoan Trichomonas vaginalis...
December 7, 2018: Parasitology Research
Wenlong Li, Feijie Xu, Wen Shuai, Honghao Sun, Hong Yao, Cong Ma, Shengtao Xu, Hequan Yao, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Jinyi Xu
A series of novel quinoline-chalcone derivatives were designed, synthesized and evaluated for their antiproliferative activity. Among them, compound 24d exhibited the most potent activity with IC50 values ranging from 0.009 to 0.016 μM in a panel of cancer cell lines. Compound 24d also displayed a good safety profile with LD50 value of 665.62 mg/kg by intravenous injection, and its hydrochloride salt 24d-HCl significantly inhibited tumor growth in H22 xenograft models without observable toxic effects, which was more potent than that of CA-4...
December 11, 2018: Journal of Medicinal Chemistry
Yunlin Cao, Linfeng Xie, Yingyue Ma, Chuanhong Ren, Mengyun Xing, Zishan Fu, Xinyue Wu, Xueren Yin, Changjie Xu, Xian Li
Flavonoids are major polyphenol compounds in plants and contribute substantially to the health-promoting benefits of fruit and vegetables. Peach is rich in polyphenols with flavonols as the main flavonoids. To investigate the regulation of flavonol biosynthesis in peach fruit, two R2R3-MYB transcription factor (TF) genes, PpMYB15 and PpMYBF1, were isolated and characterized. Sequence analysis revealed that the PpMYB15 and PpMYBF1 proteins are members of the flavonol clade of the R2R3-MYB family. Real-time quantitative PCR analysis showed that PpMYB15 and PpMYBF1 transcript levels correlated well with the flavonol content and the expression of flavonol synthase (PpFLS1) in different fruit samples...
December 7, 2018: Journal of Agricultural and Food Chemistry
Gurjaspreet Singh, Aanchal Arora, Pooja Kalra, Indresh Kumar Maurya, Cristobal Espinosa Ruizc, M Angeles Estebanc, Shweta Sinha, Kapil Goyal, Rakesh Sehgal
A series of ferrocene appended chalcone allied triazole coupled organosilatranes (FCTSa 7-FCTSa 12) were synthesised with the aim of amalgamating the pharmacological action of the constituting moieties into a single molecular scaffold. All the synthesised silatranes were well characterized by various spectroscopic techniques like IR, 1 H NMR, 13 C NMR and elemental analysis. Organosilatranes were then evaluated for their biological alacrity against bacterial and fungal strains compared with the standard drugs Rifampicin and Amphotericin B respectively...
November 28, 2018: Bioorganic & Medicinal Chemistry
Bhupendra Koul, Pooja Taak, Arvind Kumar, Anil Kumar, Indraneel Sanyal
ETHNOPHARMACOLOGICAL RELEVANCE: The genus Psoralea (Fabaceae) harbours 105 accepted species that are extensively used by local peoples and medicinal practitioners of China, India, and other countries for treatment of tooth decay, psoriasis, leucoderma, leprosy, kidney problems, tuberculosis, indigestion, constipation and impotence. Presently, pharmacological research reports are available on only few species namely Bituminaria bituminosa (Syn: P. bituminosa), P. canescens, P. corylifolia, P...
December 3, 2018: Journal of Ethnopharmacology
Arun Kumaran Anguraj Vadivel, Kevin Krysiak, Gang Tian, Sangeeta Dhaubhadel
BACKGROUND: Soybean is a paleopolyploid that has undergone two whole genome duplication events. Gene duplication is a type of genomic change that can lead to novel functions of pre-existing genes. Chalcone synthase (CHS) is the plant-specific type III polyketide synthase that catalyzes the first committed step in (iso)flavonoid biosynthesis in plants. RESULTS: Here we performed a genome-wide search of CHS genes in soybean, and identified 21 GmCHS loci containing 14 unique GmCHS (GmCHS1-GmCHS14) that included 5 newly identified GmCHSs (GmCHS10-GmCHS14)...
December 4, 2018: BMC Plant Biology
Mohammad Shahidul Islam, Hussien Mansur Ghawas, Fardous F El-Senduny, Abdullah Mohammed Al-Majid, Yaseen A M M Elshaier, Farid A Badria, Assem Barakat
Anticancer therapeutics with profiles of high potency, low toxicity, and low resistance is of considerable interest. A new series of functionalized spirooxindole linked with 3-acylindole scaffold is reported, starting from chalcones derived from 3-acetyl indole with isatin, and l-4-thiazolidinecarboxylic acid. The reactions proceeded regioselectivity, stereoselectivity, without side products in high yield (71-89%). The new spirooxindole hybrids have been evaluated in vitro for their antiproliferative effects against colon cancer (HCT-116), hepatocellular carcinoma (HepG2) and prostate cancer (PC-3)...
October 23, 2018: Bioorganic Chemistry
Mohd Usman Mohd Siddique, Tabassum Khair Barbhuiya, Barij Nayan Sinha, Venkatesan Jayaprakash
Phytoestrogens are class of natural compounds that shares structural similarity with estrogen and has the capacity to alter the fertilization in mammals. Till early 1990s, the natural phytoestrogens as well as their synthetic analogues were explored for their fertility modulating activity. During late 1990s, two findings renewed the interest on phytoestrogens as means to control hormone induced cancer: (i) revelation of overexpression of CYP1B1 in breast & ovarian cancer and (ii) protection offered by alphanapthoflavone (ANF) against hormone induced cancer...
November 17, 2018: European Journal of Medicinal Chemistry
Jamaluddin Mahar, Aamer Saeed, Kevin D Belfield, Fayaz Ali Larik, Pervaiz Ali Channar, Mehar Ali Kazi, Qamar Abbas, Mubashir Hassan, Hussain Raza, Sung-Yum Seo
A novel series of silyl-yne containing chalcone derivatives 5a-5j was synthesized by exploiting Sonogashira coupling reaction and Claisen-Schimdt condensation reaction. The synthesized derivative were characterized by spectroscopic and elemental analysis. The selective inhibition of carbonic anhydrases is considered critical in the field of medicinal chemistry because carbonic anhydrases exits in several isoforms. Synthesized compounds were subjected to carbonic anhydrase -II assay. Except 5j, the other derivatives exhibited better potential than standard acetazolamide...
November 24, 2018: Bioorganic Chemistry
Marwa Ali A Fathi, Amer Ali Abd El-Hafeez, Dalia Abdelhamid, Samar H Abbas, Monica M Montano, Mohamed Abdel-Aziz
A new series of 1,3,4-oxadiazole/chalcone hybrids was designed, synthesized, identified with different spectroscopic techniques and biologically evaluated as inhibitors of EGFR, Src, and IL-6. The synthesized compounds showed promising anticancer activity, particularly against leukemia, with 8v being the most potent. The synthesized compounds exhibited strong to moderate cytotoxic activities against K-562, KG-1a, and Jurkat leukemia cell lines in MTT assays. Compound 8v showed the strongest cytotoxic activity with IC50 of 1...
November 22, 2018: Bioorganic Chemistry
L Carmona, B Alquézar, S Tárraga, L Peña
A protein analysis in the pulp of Moro blood oranges (Citrus sinensis L. Osbeck) at the onset and after 30 days of storage at either 4 or 9 °C was performed. All differential proteins belonged to different functional classes (sugar, amino acid and secondary metabolism, defense, stress response, oxidative process, transport and cellular component biogenesis), displaying a differential accumulation in those Moro oranges kept at 9 versus 4 °C, and in those stored at 4 °C versus onset. Anthocyanin biosynthesis structural proteins chalcone synthases and flavonone 3-hydroxylase and different glutathione S-transferases related with their vacuolar transport were up-accumulated in fruits kept at 9 versus 4 °C and versus the onset...
March 30, 2019: Food Chemistry
Raedeh Saraei, Faroogh Marofi, Adel Naimi, Mehdi Talebi, Mahnaz Ghaebi, Naser Javan, Omid Salimi, Ali Hassanzadeh
Flavonoids are a varied family of phytonutrients (plant chemicals) usually are detected in fruits and vegetables. In this big family, there exist more than 10,000 members that is separated into six chief subtypes: isoflavonols, flavonoenes, flavones, flavonols, anthocyanins, and chalcones. The natural compounds, such as fruits, have visible positive effects in regulating of survival involved signaling pathways that performance as the regulator of cell survival, growth, and proliferation. Researchers have established that commonly consumption up flavonoids decreases incidence and development risk of certain cancers, especially leukemia...
November 30, 2018: Journal of Cellular Physiology
Nurmirza Begmatov, Jun Li, Khayrulla Bobakulov, Sodik Numonov, Haji Akber Aisa
Seventeen compounds were isolated from the capitula of Coreopsis tinctoria Nutt. with various column chromatographic methods and semi-preparative HPLC. Their structures were identified by the spectroscopic data and comparison with literatures as 2'-hydroxy-4,4'-dimethoxy-chalcone; (1), isoliquiritigenin (2), eriodictyol (3), naringenin (4), maritimetin (5), butin (6), taxifolin (7), luteolin (8), 7,3',4'-trihydroxyflavone (9), 8,3',4'-trihydroxyflavone-7-O-β-d-glucoside (10), quercetin (11), quercetagitin-7-O-β-d-glucoside (12), quercetin-7-O-β-d-glucoside (13), 3,4-dihydroxybenzoic acid (14), caffeic acid (15), coreoside B (16), and myo-inositol (17)...
November 30, 2018: Natural Product Research
Jianhua Li, Chenfei Tian, Yuhui Xia, Ishmael Mutanda, Kaibo Wang, Yong Wang
Baicalein and scutellarein are bioactive flavones found in the medicinal plant Scutellaria baicalensis Georgi, used in traditional Chinese medicine. Extensive previous work has demonstrated the broad biological activity of these flavonoids, such as antifibrotic, antiviral and anticancer properties. However, their supply from plant material is insufficient to meet demand. Here, to provide an alternative production source and increase production levels of these flavones, we engineered an artificial pathway in an Escherichia coli cell factory for the first time...
November 26, 2018: Metabolic Engineering
Silvia Marquina, Maritza Maldonado-Santiago, Jessica Nayelli Sánchez-Carranza, Mayra Antúnez-Mojica, Leticia González-Maya, Rodrigo Said Razo-Hernández, Laura Alvarez
Eleven 4'-alkoxy chalcones were synthesized and biologically evaluated for their antiproliferative activity against four human tumor cell lines (PC-3, MCF-7, HF-6, and CaSki). Compounds 3a-3d and 3f were selective against PC-3, with IC50 values ranging from 8.08 to 13.75 μM. In addition, chalcones 3a-3c did not affect the normal fibroblasts BJ cells. The most active and selective compounds were further evaluated for their effect on the progression of cell cycle in PC-3 cells, and chalcones 3a and 3c induced a G2/M phase arrest...
November 10, 2018: Bioorganic & Medicinal Chemistry
Sourav Sekhar Bera, Md Raja Sk, Modhu Sudan Maji
Weakly coordinating, ketone-directed, regioselective mono-amidation of aromatic ketones, chalcone, carbazole, and benzophenones are achieved employing high-valent cobalt- and rhodium-catalysis to access numerous biologically important molecular building blocks. This amidation proceeds smoothly with varieties of ketones as well as with several amidating partners. The application of the products to the syntheses of heterocycles acridones, indoles, quinoline, quinolones, quinolinones, and quinazolines is also described...
November 26, 2018: Chemistry: a European Journal
Xue Han, Bin Peng, Bei-Bei Xiao, S-Li Cao, Chao-Rui Yang, Wen-Zhu Wang, Fu-Cheng Wang, Hong-Yun Li, Xiao-Li Yuan, Ruifeng Shi, Ji Liao, Hailong Wang, Jing Li, Xingzhi Xu
The chalcone motif can be found in many molecules that contribute to essential biological processes, and many chalcone-containing compounds exhibit potent anti-cancer activity. Here, we synthesized two series of chalcone analogues (3a-s and 6a-s) based on substituting the chalcone B-ring or A-ring with a 4-oxoquinazolin-2-yl group, and then evaluated them for cytotoxic activity in human colorectal HCT-116 and breast cancer MCF-7 cell lines. Compounds 3a-s (in which a 4-oxoquinazolin-2-yl group functioned as the B-ring) were markedly more cytotoxic than compounds 6a-s (in which 4-oxoquinazolin-2-yl group functioned as the A-ring), based on their IC50 values to inhibit proliferation...
November 16, 2018: European Journal of Medicinal Chemistry
Ines L Paraiso, Layhna S Plagmann, Liping Yang, Ryszard Zielke, Adrian F Gombart, Claudia S Maier, Aleksandra E Sikora, Paul R Blakemore, Jan F Stevens
SCOPE: The intestinal microbiota transforms a wide range of available substrates, including polyphenols. Microbial catabolites of polyphenols can contribute in significant ways to the health promoting properties of their parent polyphenols. This work aimed to identify intestinal metabolites of xanthohumol (XN), a prenylated flavonoid found in hops (Humulus lupulus) and beer, as well as to identify pathways of metabolism of XN in the gut. METHODS AND RESULTS: To investigate intestinal metabolism, XN and related prenylated flavonoids, isoxanthohumol (IX) and 8-prenylnaringenin (8PN) were added to growing cultures of intestinal bacteria, Eubacterium ramulus and E...
November 24, 2018: Molecular Nutrition & Food Research
Richard M Beteck, Lesetje J Legoabe, Michelle Isaacs, Heinrich C Hoppe
Human African trypanosomiasis is a neglected infectious disease that affects mostly people living in the rural areas of Africa. Current treatment options are limited to just four drugs that have been in use of four to nine decades. The life-threatening toxic side-effects associated with the use of these drugs are disconcerting. Poor efficacy, low oral bioavailability, and high cost are other shortcomings of current HAT treatments. Evaluating the potentials of known hits for other therapeutic areas may be a fast and convenient method to discover new hit compounds against alternative targets...
November 16, 2018: Drug Research
Della Grace Thomas Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa Elizabeth Mathew, Sanal Dev, B Lakshminarayanan, Omnia Magdy Hendawy, Bijo Mathew
Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD). The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated. Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively...
November 18, 2018: Central Nervous System Agents in Medicinal Chemistry
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