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Synthesis of curcumin

Taki Sato, Mayumi Hotsumi, Koki Makabe, Hiroyuki Konno
Amyloid β fibrillation is an early event in Alzheimer's disease, so its detection is important to understand its roles in Alzheimer's disease. Curcumin, which has poor water solubility, has been reported to have many pharmacological activities including potent anti-amyloid β fibril activity in Alzheimer's disease. In this study, we found that curcumin analogues with the fluorescence property instead of non-inhibition of amyloid β fibrils. The development of new curcumin analogue, Me-CUR (9), as fluorescent switchable probe to detect amyloid β fibrils is described...
October 3, 2018: Bioorganic & Medicinal Chemistry Letters
Amirah Adlia, Ilham Tomagola, Sophi Damayanti, Ardyanto Mulya, Heni Rachmawati
Conjugation of curcumin and gold with green chemistry is an approach to improve the effectiveness of curcumin as anti-fibrosis. In this work, curcumin and gold were conjugated to deliver curcumin to the liver. Curcumin-gold nanoparticles (cAuNPs) were prepared by varying curcumin pH and concentration. The successful of cAuNPs formation were identified by using UV-visible and FTIR spectrophotometers. The particle size and morphology were analyzed using particle size analyzer and cryo-TEM respectively. In vitro antioxidant assay was performed to determine the curcumin activity after conjugation...
September 21, 2018: Scientia Pharmaceutica
Yuzhen Hu, Miao Li, Mengmeng Zhang, Yiguang Jin
Idiopathic pulmonary fibrosis (IPF) is a progressive interstitial lung disease with high mortality and poor prognosis. Curcumin shows anti-inflammatory effect by suppressing pro-inflammatory cytokines and inhibiting NF-κB mediated inflammation. Here, we developed inhalable curcumin-loaded poly(lactic-co-glycolic)acid (PLGA) large porous microparticles (LPMPs) for the treatment of IPF. Curcumin LPMPs were rough and loose particles with many pores on the surfaces and channels in the inner spaces. The mean geometric diameter of them was larger than 10 µm while the aerodynamic diameter was only 3...
November 15, 2018: International Journal of Pharmaceutics
Marta Rui, Giacomo Rossino, Stefania Coniglio, Stefania Monteleone, Arianna Scuteri, Alessio Malacrida, Daniela Rossi, Laura Catenacci, Milena Sorrenti, Mayra Paolillo, Daniela Curti, Letizia Venturini, Dirk Schepmann, Bernhard Wünsch, Klaus R Liedl, Guido Cavaletti, Vittorio Pace, Ernst Urban, Simona Collina
In this manuscript we report on the design, synthesis and evaluation of dual Sigma 1 Receptor (S1R) modulators/Acetylcholinesterase (AChE) inhibitors endowed with antioxidant and neurotrophic properties, potentially able to counteract neurodegeneration. The compounds based on arylalkylaminoketone scaffold integrate the pharmacophoric elements of RRC-33, a S1R modulator developed by us, donepezil, a well-known AChE inhibitor, and curcumin, a natural antioxidant compound with neuroprotective properties. A small library of compounds was synthesized and preliminary in vitro screening performed...
September 8, 2018: European Journal of Medicinal Chemistry
Cihui Tian, Sajid Asghar, Yurui Xu, Zhipeng Chen, Jingwei Zhang, Qineng Ping, Yanyu Xiao
Redox-sensitive micelles based onhydrophilic hyaluronic acid-ss-hydrophobic curcumin conjugate were designed as a novel delivery system for gliomas targeting. Furthermore, the obtained micelles were further functionalized with Tween 80 (CUR-THSC) for better brain penetration. Dynamic light scattering experiment and in vitro release study showed that the synthetic disulfide-linked conjugate possessed redox-sensitivity under high glutathione conditions. Spherical micelles with a mean particle size of 74.2 nm, negative zeta potential (-30...
September 7, 2018: International Journal of Biological Macromolecules
Yogesh B Sutar, Vikas N Telvekar
The effective delivery of low potency anticancer drug is a major challenge. The present study introduces the novel chitosan-polylactic acid (CS-PLA)-drug conjugate and its transferrin receptor targeted polyelectrolyte complex nanoparticles (PEC Nps), encapsulating free drug to increase its potency and specificity. The model drug curcumin (CR) was used and incorporated in this system in both conjugated and encapsulated form. The synthesis of CS-PLA-CR copolymer was confirmed by 1 H NMR, FTIR, UV-visible spectrum, DSC thermogram and zeta potential...
November 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Amir Reza Ariamoghaddam, Bahman Ebrahimi-Hosseinzadeh, Ashrafalsadat Hatamian-Zarmi, Razi Sahraeian
Obesity as a dominant problem in developed countries which is known to be basic step of so many diseases is subjected to find a solution for in this work. Curcumin containing polyvinyl alcohol-gelatin nanofibers which ranging from 200 to 250 nm in diameter as a transdermal drug delivery system for declining volume of subcutaneous adipose tissue is investigated here. Morphology and synthesis method of nanofibers is designed and optimized by statistical software and a totally uniform and reproducible method of synthesis is used for preparation of a transdermal patch...
November 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Jigyasa, Jaspreet Kaur Rajput
Green, simple and quick melamine sensing assays for highly efficient detection of melamine down to nM level have been reported. Biopolyphenols (rutin & curcumin) were used as reducing and stabilizing agents for the synthesis of silver nanoparticles (AgNPs). The synthesis of AgNPs was confirmed by FTIR, UV-Visible, XRD and HRTEM-EDS analysis. The biopolyphenols reduced AgNPs were well dispersed and spherical in shape. However, the presence of melamine in the reaction medium disrupted their synthesis. This may be attributed to interaction of melamine with Ag+ ions and biopolyphenols...
November 30, 2018: Biosensors & Bioelectronics
Bo Ram Kim, Ji-Young Park, Hyung Jae Jeong, Hyung-Jun Kwon, Su-Jin Park, In-Chul Lee, Young Bae Ryu, Woo Song Lee
Sialidases are key virulence factors that remove sialic acid from the host cell surface glycan, unmasking receptors that facilitate bacterial adherence and colonisation. In this study, we developed potential agents for treating bacterial infections caused by Streptococcus pneumoniae Nan A that inhibit bacterial sialidase using Turmeric and curcumin analogues. Design, synthesis, and structure analysis relationship (SAR) studies have been also described. Evaluation of the synthesised derivatives demonstrated that compound 5e was the most potent inhibitor of S...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Mahsa Souri, Vahid Hoseinpour, Alireza Shakeri, Nasser Ghaemi
This study concerns the optimisation of green synthesis of manganese oxide nanoparticles (MnO NPs) with Dittrichia graveolens (L.) extract via response surface methodology (RSM). Central composite design was used to evaluate the effect of pH, time, and the extract to the metal ratio on the synthesised nanoparticles (NPs). Nine runs were designed to investigate the effect of each parameter while NPs were synthesised under different conditions. Considering the p -values ( p -value < 0.05), it is indicated that the extract to the metal ratio was the most effective parameter...
September 2018: IET Nanobiotechnology
Kenneth K Laali, William J Greves, Angela T Zwarycz, Sebastian J Correa Smits, Frederick J Troendle, Gabriela L Borosky, Sharoon Akhtar, Alak Manna, Aneel Paulus, Asher Chanan-Khan, Manabu Nukaya, Gregory D Kennedy
In a continuing search for curcuminoid (CUR) compounds with antitumor activity, a novel series of heterocyclic CUR-BF2 adducts and CUR compounds based on indole, benzothiophene, and benzofuran along with their aryl pyrazoles were synthesized. Computational docking studies were performed to compare binding efficiency to target proteins involved in specific cancers, namely HER2, proteasome, VEGFR, BRAF, and Bcl-2, versus known inhibitor drugs. The majority presented very good binding affinities, similar to, and even more favorable than those of known inhibitors...
September 19, 2018: ChemMedChem
Gejo George, Suja Bhargavan Sisupal, Teenu Tomy, Alaganandam Kumaran, Prabha Vadivelu, Vemparthan Suvekbala, Swaminathan Sivaram, Lakshminarayanan Ragupathy
The success of developing graphene based biomaterials depends on its ease of synthesis, use of environmentally benign methods and low toxicity of the chemicals involved as well as biocompatibility of the final products/devices. We report, herein, a simple, scalable and safe method to produce defect free few layers graphene using naturally available phenolics i.e. curcumin/tetrahydrocurcumin/quercetin, as solid-phase exfoliating agents with a productivity of ∼45 g/batch (D/G ≤ 0.54 and D/D' ≤ 1...
July 25, 2018: Scientific Reports
Stephen Bigelsen
Despite new and exciting research and renewed optimism about future therapy, current statistics of survival from pancreatic cancer remains dismal. Patients seeking alternative or complementary treatments should be warned to avoid the hype and instead look to real science. A variety of relatively safe and inexpensive treatment options that have shown success in preclinical models and/or retrospective studies are currently available. Patients require their physicians to provide therapeutic guidance and assistance in obtaining and administrating these various therapies...
2018: Cancer Management and Research
Jie Quan Wang, Xiaobin Wang, Yang Wang, Wen Jian Tang, Jing Bo Shi, Xin Hua Liu
In this study, twenty curcumin analogue hybrids as potential anticancer agents through regulation protein of TrxR were designed and synthesized. Results of anticancer activity showed that 5,7-dimethoxy-3-(3-(2-((1E, 4E)-3-oxo-5-(pyridin-2-yl)penta-1,4-dien-1- yl)phenoxy)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one (compound 7d) could induce gastric cancer cells apoptosis by arresting cell cycle, break mitochondria function and inhibit TrxR activity. Meanwhile, western blot revealed that this compound could dramatically up expression of Bax/Bcl-2 ratio and high expression of TrxR oxidation...
August 5, 2018: European Journal of Medicinal Chemistry
Puneet Khandelwal, Aftab Alam, Arpankumar Choksi, Samit Chattopadhyay, Pankaj Poddar
Gold nanoparticles (Au NPs) have been thoroughly investigated for anti-cancer therapy. However, their undesired high gold content remains a problem when injected into the body for drug delivery applications. In this report, we made an effort to conjugate the curcumin molecules on the surface of gold quantum clusters (Au QCs) by a novel in situ synthesis method which provides an alternative route to not only reduce the metallic content but also increase the water solubility of curcumin and the loading efficiency...
May 31, 2018: ACS Omega
Amanda N Abraham, Tarun K Sharma, Vipul Bansal, Ravi Shukla
The rapid formation of the protein corona on to the nanoparticle (NP) surface is the key that confers biological identity to NPs and subsequently dictates their fate both in vitro and in vivo. Despite significant efforts, the inability to control the spontaneous interaction of serum proteins with the administered NPs remains a major constraint in clinical translation of nanomedicines. The ligands present on the NP surface offer promise in controlling their biological interactions; however, their influence on the NP-protein interaction is not well-understood...
February 28, 2018: ACS Omega
Tathagata Pal, Shanid Mohiyuddin, Gopinath Packirisamy
Early detection is the critical phase in the prognostic strategy of various life-threatening maladies like infectious diseases and cancer. The mortality rate caused by these diseases could be considerably reduced if they were diagnosed in the early stages of disease development. Carbon dots (C-dots), a relatively new and promising candidate in the fluorescent nanomaterial category, possess a perceptible impact on various bioapplications. Herein, we report a one-step facile hydrothermal synthesis that yields a novel surface-passivated carbon dot (CDP) from curcumin (as a green substrate) displaying high aqueous solubility...
January 31, 2018: ACS Omega
Eneko Larrañeta, Mikel Imízcoz, Jie X Toh, Nicola J Irwin, Anastasia Ripolin, Anastasia Perminova, Juan Domínguez-Robles, Alejandro Rodríguez, Ryan F Donnelly
Lignin is the second most abundant biopolymer on the planet. It is a biocompatible, cheap, environmentally friendly and readily accessible material. It has been reported that these biomacromolecules have antimicrobial activities. Consequently, lignin (LIG) has the potential to be used for biomedical applications. In the present work, a simple method to prepare lignin-based hydrogels is described. The hydrogels were prepared by combining LIG with poly(ethylene glycol) and poly(methyl vinyl ether- co -maleic acid) through an esterification reaction...
July 2, 2018: ACS Sustainable Chemistry & Engineering
Miri Lee, Kyoung-Sook Kim, Abekura Fukushi, Dong-Hyun Kim, Cheorl-Ho Kim, Young-Choon Lee
Curcumin, a natural polyphenolic compound isolated from the plant Curcuma longa , is known to induce autophagy in various cancer cells, including lung cancer. In the present study, we also confirmed by LC3 immunofluorescence and immunoblotting analyses that curcumin triggers autophagy in the human lung adenocarcinoma A549 cell line. In parallel with autophagy induction, the gene expression of human GD3 synthase (hST8Sia I) responsible for ganglioside GD3 synthesis was markedly elevated in response to curcumin in the A549 cells...
July 2, 2018: International Journal of Molecular Sciences
Raymond E Borg, Maryam Hatamimoslehabadi, Stephanie Bellinger, Jeffrey La, Farha Mithila, Chandra Yelleswarapu, Jonathan Rochford
The synthesis, photophysical and photoacoustic characterization for a series of nine π-extended quadrupolar curcumin dyes is presented. A systematic evaluation of the π-bridging unit including the p-phenyl, naphth-4-yl, thien-2-yl and hybrid 4-naphthathien-2-yl groups is presented. Furthermore, evaluation of the strongly donating donor-π-acceptor-π-donor quadrupolar dimethylamino terminated derivatives is also included. Select dyes exhibit excited state absorption at increased laser fluence which translates to the production of a nonlinear enhanced photoacoustic response...
July 10, 2018: Photochemistry and Photobiology
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