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Angelo Antonio D'Archivio, Maria Anna Maggi
Response surface methodology, coupled to a full factorial three-level experimental design, was applied to investigate the combined influence of pH (between 7.0 and 8.6) and composition of methanol-water mixtures (between 30 and 70% v/v of methanol content) on the stability of curcumin and its analogues demethoxycurcumin and bisdemethoxycurcumin. The response plots revealed that addition of methanol noticeably improved the stability of curcuminoids, this effect being both pH- and structure-dependent. In the central point of the experimental domain, half-life times of curcumin, demethoxycurcumin and bisdemethoxycurcumin were 3...
March 15, 2017: Food Chemistry
Francielle Pelegrin Garcia, Jean Henrique da Silva Rodrigues, Zia Ud Din, Edson Rodrigues-Filho, Tânia Ueda-Nakamura, Rachel Auzély-Velty, Celso Vataru Nakamura
Leishmaniasis is a neglected tropical disease that affects millions of people worldwide. Current therapies mainly rely on antimonial drugs that are inadequate because of their high toxicity and increased drug resistance. An urgent need exists to discover new, more effective, more affordable, and more target-specific drugs. Pathways that are associated with apoptosis-like cell death have been identified in unicellular eukaryotes, including protozoan parasites. In the present study, we studied the mechanism of cell death that is induced by A3K2A3 against L...
October 19, 2016: Apoptosis: An International Journal on Programmed Cell Death
Liran Horev, Yuval Ramot, Laurent Klapholz
Yellow discoloration of the skin may be caused by several etiologies, including jaundice, hypervitaminosis, drug reaction or chemical exposure. Herein we describe a 68-year-old woman with a history of breast and thyroid carcinoma, presenting with a yellow discoloration of her soles, after ingestion of one capsule a day of turmeric root extract (Bluebonnet Turmeric Root, 500 mg, Vcap), taken for its anti-cancer properties, for 4 months. After drug cessation, the yellow hue disappeared completely. A Naranjo assessment score of 5 was obtained, indicating a probable relationship between the patient's symptom and her use of the drug...
December 2015: Drug Saf Case Rep
S Sanyal, A Painelli, S K Pati, F Terenziani, C Sissa
We present a theoretical investigation of small aggregates of quadrupolar (A-π-D-π-A or D-π-A-π-D) charge-transfer dyes, with attention focused on the role of intermolecular interactions in determining their optical properties. We tackle the theoretical issue by adopting essential-state models (ESMs), which describe an isolated molecule in terms of a minimal number of electronic states, corresponding to the resonance structures. ESMs quite naturally describe intermolecular interactions relaxing the dipolar approximation and accounting for molecular polarizabilities...
October 12, 2016: Physical Chemistry Chemical Physics: PCCP
Kok-Yong Chin
Osteoarthritis is a degenerative disease of the joint affecting aging populations worldwide. It has an underlying inflammatory cause, which contributes to the loss of chondrocytes, leading to diminished cartilage layer at the affected joints. Compounds with anti-inflammatory properties are potential treatment agents for osteoarthritis. Curcumin derived from Curcuma species is an anti-inflammatory compound as such. This review aims to summarize the antiosteoarthritic effects of curcumin derived from clinical and preclinical studies...
2016: Drug Design, Development and Therapy
Shuna Jin, Chengwu Song, Shuailong Jia, Sen Li, Yang Zhang, Cheng Chen, Yulin Feng, Yong Xu, Chaomei Xiong, Yi Xiang, Hongliang Jiang
Turmeric and curcuminoids are used as natural food coloring and functional food additives in various parts of the world. In this study, ninety-six curcuminoids were fully characterized using a targeted curcuminoid profile, which established by integrated use of two complementary LC-MS/MS platforms (liquid chromatography-quadrupole time of flight mass spectrometry (LC-QTOF-MS/MS) and liquid chromatography-quadrupole linear ion trap mass spectrometry (LC-QTRAP-MS/MS)). The curcuminoid profile was represented in the form of a multiple reaction monitoring (MRM) mode based on LC-QTRAP-MS/MS analysis...
September 27, 2016: Journal of Pharmaceutical and Biomedical Analysis
Ashapurna Sarma, Vishal P Sharma, Arindam B Sarkar, M Chandra Sekar, Karunakar Samuel, Michael E Geusz
BACKGROUND: Curcuminoids of the spice turmeric and their enhanced derivatives have much potential as cancer treatments. They act on a wide variety of biological pathways, including those regulating cell division and circadian rhythms. It is known that circadian clocks can modify cancer therapy effectiveness, according to studies aimed at optimizing treatments based on the circadian cycle. It is therefore important to determine whether treatments with curcumin or similar chemotherapeutic agents are regulated by circadian timing...
September 29, 2016: BMC Cancer
Trong Tuan Dao, Pankaj Sehgal, Truong Thanh Tung, Jesper Vuust Møller, John Nielsen, Michael Palmgren, Søren Brøgger Christensen, Anja Thoe Fuglsang
P-type ATPases catalyze the active transport of cations and phospholipids across biological membranes. Members of this large family are involved in a range of fundamental cellular processes. To date, a substantial number of P-type ATPase inhibitors have been characterized, some of which are used as drugs. In this work a library of natural compounds was screened and we first identified curcuminoids as plasma membrane H+-ATPases inhibitors in plant and fungal cells. We also found that some of the commercial curcumins contain several curcuminoids...
2016: PloS One
Kazim Sahin, Ragip Pala, Mehmet Tuzcu, Oguzhan Ozdemir, Cemal Orhan, Nurhan Sahin, Vijaya Juturu
PURPOSE: Exercise (Ex) increases reactive oxygen species and impairs antioxidant defense systems. Recent data suggest that curcumin (CW) possesses peroxisome proliferator-activated receptor gamma activity and anti-inflammatory properties. Therefore, this study was designed to investigate the effects of CW supplementation on Ex performance, endurance, and changes in serum and muscle proteins in rats after exhaustive Ex. MATERIALS AND METHODS: Twenty-eight (28) male Wistar rats (age: 8 weeks and body weight: 180±20 g) were divided into four treatment groups: 1) control (C; no Ex), 2) C + CW (no Ex + CW), 3) C + Ex, and 4) C + Ex + CW (Ex + CW)...
2016: Journal of Inflammation Research
Sara Rubagotti, Stefania Croci, Erika Ferrari, Michele Iori, Pier C Capponi, Luca Lorenzini, Laura Calzà, Annibale Versari, Mattia Asti
Curcumin derivatives labelled with fluorine-18 or technetium-99m have recently shown their potential as diagnostic tools for Alzheimer's disease. Nevertheless, no study by exploiting the labelling with gallium-68 has been performed so far, in spite of its suitable properties (positron emitter, generator produced radionuclide). Herein, an evaluation of the affinity for synthetic β-amyloid fibrils and for amyloid plaques of three (nat/68)Ga-labelled curcumin analogues, namely curcumin curcumin (CUR), bis-dehydroxy-curcumin (bDHC) and diacetyl-curcumin (DAC), was performed...
2016: International Journal of Molecular Sciences
Erika Ferrari, Rois Benassi, Monica Saladini, Giulia Orteca, Zuzana Gazova, Katarina Siposova
Curcumin and its derivatives have attracted great interest in the prevention and treatment of Alzheimer's disease (AD), thanks both to the ability to hinder the formation of amyloid-beta (Aβ) aggregates and the ability to bind Cu (II) ion. In this article, we explore the ability of curcumin derivatives of K2T series to affect amyloid Aβ1-40 aggregation. These derivatives were obtained by introducing the t-butyl ester group through a methylenic spacer on the central carbon atom of the β-diketo moiety of curcumin frame...
August 29, 2016: Chemical Biology & Drug Design
Jacek W Morzycki, Lucie Rárová, Jiři Grúz, Tomasz Sawczuk, Urszula Kiełczewska, Leszek Siergiejczyk, Agnieszka Wojtkielewicz
Natural retinoids and curcuminoids are known for their broad spectrum of biological properties, such as antioxidant, anti-inflammatory, antitumor, and so forth. In this work, a convenient synthesis of aromatic retinoids and curcuminoids from vinyl or allyl ketones, and the corresponding alcohols, using olefin metathesis as a key reaction, was elaborated. The best yields and diastereoselectivities were obtained from allylic or homoallylic alcohols by employing the two-step cross-metathesis/oxidation procedure...
August 2016: ChemistryOpen
Rob De Vreese, Charlotte Grootaert, Sander D'hoore, Atiruj Theppawong, Sam Van Damme, Maarten Van Bogaert, John Van Camp, Matthias D'hooghe
Curcuminoids are high-potential drugs targeting multiple components of vital signaling pathways without being toxic, and are therefore considered to be valuable lead structures in medicinal chemistry. Unfortunately, most curcuminoids poorly reach their site of action because of low bioavailability issues, (partly) associated with the labile β-diketo structure. In that respect, curcumin derivatives bearing a central β-enaminone fragment may have improved solubility and intestinal stability, and therefore may represent a new class of analogs with higher bioactivity...
November 10, 2016: European Journal of Medicinal Chemistry
Jing-Jing Xu, Qin Li, Jun Cao, Elisa Warner, Mingrui An, Zhijing Tan, Shu-Ling Wang, Li-Qing Peng, Xun-Gao Liu
A green and economical method for the extraction and preconcentration of natural pigments (curcumin, demethoxycurcumin and bisdemethoxycurcumin) was developed using ultrasound-assisted extraction combined with dispersive micro solid-phase extraction. In this work, Ionic liquids (ILs) were used for the pre-extraction of natural pigments. The pure chitosan nanoparticles (CS NPs) were then used as a sorbent for the microextraction mode. The method involves the use of ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry...
September 9, 2016: Journal of Chromatography. A
Thi Thanh Hanh Nguyen, Jinbeom Si, Choongil Kang, Byoungsang Chung, Donghwa Chung, Doman Kim
Curcuminoids from rhizomes of Curcuma longa possess various biological activities. However, low aqueous solubility and consequent poor bioavailability of curcuminoids are major limitations to their use. In this study, curcuminoids extracted from turmeric powder using stevioside (Ste), rebaudioside A (RebA), or steviol glucosides (SG) were solubilized in water. The optimum extraction condition by Ste, RebA, or SG resulted in 11.3, 9.7, or 6.7mg/ml water soluble curcuminoids. Curcuminoids solubilized in water showed 80% stability at pH from 6...
January 1, 2017: Food Chemistry
Hoang Van Nong, Le Xuan Hung, Pham Nam Thang, Vu Duc Chinh, Le Van Vu, Phan Tien Dung, Tran Van Trung, Pham Thu Nga
In this report, we present the research results on using the conventional method and microwave technology to extract curcuminoid from turmeric roots originated in different regions of Northern Vietnam. This method is simple, yet economical, non-toxic and still able to achieve high extraction performance to get curcuminoid from turmeric roots. The detailed results on the Raman vibration spectra combined with X-ray powder diffraction and high-performance liquid chromatography/mass spectrometry allowed the evaluation of each batch of curcumin crystalline powder sample received, under the conditions of applied fabrication technology...
2016: SpringerPlus
Gary N Asher, Ying Xie, Ruin Moaddel, Mitesh Sanghvi, Katina S S Dossou, Angela D M Kashuba, Robert S Sandler, Roy L Hawke
Curcumin is poorly absorbed driving interest in new preparations. However, little is known about pharmacokinetics and tissue bioavailability between formulations. In this randomized, crossover study we evaluated the relationship between steady-state plasma and rectal tissue curcuminoid concentrations using standard and phosphatidylcholine curcumin extracts. There was no difference in the geometric mean plasma AUCs when adjusted for the 10-fold difference in curcumin dose between the two formulations. Phosphatidylcholine curcumin extract yielded only 20-30% plasma demethoxycurcumin and bisdemethoxycurcumin conjugates compared to standard extract, yet yielded 20-fold greater hexahydrocurcumin...
August 9, 2016: Journal of Clinical Pharmacology
Emma R Veldman, Zhisheng Jia, Christer Halldin, Marie M Svedberg
The presence of β-amyloid (Aβ) containing plaques in the brain is a hallmark of Alzheimer's disease (AD) and serves as a biomarker for confirmation of diagnosis postmortem. Early diagnosis is of great importance for optimal treatment and for monitoring disease progression in the brain. Highly specific and sensitive biomarkers are thus greatly needed to assess therapeutic efficacy, not only clinically, but also in terms of clearance of histopathological lesions and decelerated neurodegeneration. The objective of the present study was to give more insight into the binding of curcumin analogues, curcuminoids, to Aβ containing plaques in postmortem tissue from AD patients...
September 6, 2016: Neuroscience Letters
Alvaro Etcheverry-Berríos, Ignacio Olavarría, Mickael L Perrin, Raúl Díaz-Torres, Domingo Jullian, Ingrid Ponce, José H Zagal, Jorge Pavez, Sergio O Vásquez, Herre S J van der Zant, Diana Dulić, Núria Aliaga-Alcalde, Monica Soler
We studied the electronic and conductance properties of two thiophene-curcuminoid molecules, 2-thphCCM (1) and 3-thphCCM (2), in which the only structural difference is the position of the sulfur atoms in the thiophene terminal groups. We used electrochemical techniques as well as UV/Vis absorption studies to obtain the values of the HOMO-LUMO band gap energies, showing that molecule 1 has lower values than 2. Theoretical calculations show the same trend. Self-assembled monolayers (SAMs) of these molecules were studied by using electrochemistry, showing that the interaction with gold reduces drastically the HOMO-LUMO gap in both molecules to almost the same value...
August 26, 2016: Chemistry: a European Journal
Juan Wang, Xiao-Hui Wang, Xiao Liu, Jun Li, Xiao-Ping Shi, Yue-Lin Song, Ke-Wu Zeng, Le Zhang, Peng-Fei Tu, She-Po Shi
A curcuminoids, benzalacetone-, and quinolone-producing type III polyketide synthase (HsPKS3) from Huperzia serrata uniquely catalyzes the formation of unnatural 2-substituted quinolones and 1,3-diketones via head-to-head condensation of two completely different substrates. The broad range of substrate tolerance of HsPKS3 facilitates accessing structurally diverse 2-substituted quinolones and 1,3-diketones.
August 5, 2016: Organic Letters
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